No data available that match "benzothiepins"


Enhancement of osteogenesis in vitro and in vivo by a novel osteoblast differentiation promoting compound, TAK-778. (1/16)

TAK-778 [(2R,4S)-(-)-N-(4-diethoxyphosphorylmethylphenyl)-1,2,4, 5-tetrahydro-4-methyl-7, 8-methylenedioxy-5-oxo-3-benzothiepin-2-carboxyamide; mw 505.53], a novel osteoblast differentiation promoting compound, was characterized in vitro and in vivo models. TAK-778 at doses of 10(-6) M and higher promoted potently bone-like nodule formation in the presence of dexamethasone in rat bone marrow stromal cell culture. This was accompanied by increases in cellular alkaline phosphatase activity, soluble collagen release, and osteocalcin secretion. Under the culture conditions, TAK-778 also stimulated the secretion of transforming growth factor-beta and insulin-like growth factor-I, indicating that TAK-778 may exert regulatory effects on osteoblast differentiation via autocrine/paracrine mechanisms. Furthermore, the in vivo osteogenic potential of TAK-778 was studied in bony defect and osteotomy animal models, using sustained release microcapsules consisted of a biodegradable polymer, poly (dl-lactic/glycolic) acid (PLGA). Single local injection of TAK-778/PLGA-microcapsules (PLGA-MC) (0.2-5 mg/site) to rat skull defects resulted in a dose-dependent increase in new bone area within the defects after 4 weeks. When the pellet containing TAK-778/PLGA-MC (4 mg/pellet) was packed into place to fill the tibial segmental defect in rabbit, this pellet induced osseous union within 2 months, whereas the placebo pellet did not. In addition, single local application of TAK-778/PLGA-MC (10 mg/site) to rabbit tibial osteotomy site enhanced callus formation accompanied by an increase in breaking force after 30 days. These results reveal for the first time that a nonendogenous chemical compound promotes potently osteogenesis in vitro and enhances new bone formation during skeletal regeneration and bone repair in vivo and should be useful for the stimulation of fracture healing.  (+info)

Effects of histamine H1 antagonist dithiaden on acetic acid-induced colitis in rats. (2/16)

To assess the possible involvement of mast cells and/or their mediators in inflammatory bowel diseases, the effect of the histamine H1 antagonist Dithiaden was studied on a model of acetic acid-induced colitis in rats. Dithiaden pretreatment by intracolonic administration was found to reduce the extent of acute inflammatory colonic injury. This was manifested by a decrease in the score of gross mucosal injury, by lowered colonic wet weight and by diminished myeloperoxidase activity reflecting reduced leukocyte infiltration. Vascular permeability and gamma-glutamyl transpeptidase activity, elevated by acetic acid exposure, were decreased after Dithiaden pretreatment. The results indicate that locally administered Dithiaden may protect the colonic mucosa against an acute inflammatory attack by interfering with the action of the major mast cell mediator histamine.  (+info)

Synthesis of 1-benzothiepine and 1-benzazepine derivatives as orally active CCR5 antagonists. (3/16)

Quaternary ammonium benzocycloheptene compound 1 has previously been reported as a clinical candidate for an injectable CCR5 antagonist. In order to develop an orally active CCR5 antagonist, derivatives of tertiary amine benzocycloheptene 2, the chemical precursor to 1, were investigated. The benzocycloheptene ring was converted to benzothiepine and benzazepine rings and it was found that these changes could enhance the potency of tertiary amine derivatives. In particular, the 1-benzothiepine-1,1-dioxide 11b and the N-methyl-1-benzazepine 18 showed increased activity and good preliminary pharmacokinetic properties. The synthesis of 1-benzothiepine and 1-benzazepine derivatives and their activity are described.  (+info)

KW-7158 [(2S)-(+)-3,3,3-trifluoro-2-hydroxy-2-methyl-N-(5,5,10-trioxo-4,10-dihydrothieno[ 3,2-c][1]benzothiepin-9-yl)propanamide] enhances A-type K+ currents in neurons of the dorsal root ganglion of the adult rat. (4/16)

Recent studies revealed that a new compound, KW-7158 [(2S)-(+)-3,3,3-trifluoro-2-hydroxy-2-methyl-N-(5,5,10-trioxo-4,10-dihydrothieno[ 3,2-c][1]benzothiepin-9-yl)propanamide], can depress the excitability of afferent pathways from the urinary bladder and reduce bladder overactivity induced by chemical irritation of the urinary tract with xylene, an agent that sensitizes capsaicin-sensitive, C-fiber afferent nerves. In the present experiments, we examined the mechanisms that might underlie the depressant effect of KW-7158 on primary afferent neurons by studying the actions of the compound on ion channels and firing in dissociated dorsal root ganglion (DRG) cells from adult rats using whole cell patch-clamp techniques. KW-7158 increased transient, A-type K+ currents at concentrations ranging from 50 nM to 1 microM (20-50% increases). Similar effects were seen in fast blue identified bladder afferent neurons. Low concentrations of KW-7158 shortened the action potential duration, produced a 5- to 10-mV hyperpolarization, and inhibited repetitive firing induced by either 4-AP (50 microM) or substance P (0.5 microM) in phasic firing DRG neurons. Above 1 microM, KW-7158 elicited a smaller enhancement of A-type K+currents and in high concentrations inhibited the currents. Tetraethylammonium (5-60 mM) and verapamil (50 microM), which block noninactivating K+ currents, did not prevent the facilitatory effects of KW-7158. High concentrations of 4-AP (5 mM) inhibited A-type K+ currents and prevented the facilitatory effect of KW-7158 on the remaining currents. These data suggest that KW-7158 enhances A-type K+ currents in DRG neurons. Because A-type K+ channels regulate afferent neuron excitability and firing properties, KW-7158 is a promising new compound for treatment of hyper-reflexic bladder conditions.  (+info)

Orally active CCR5 antagonists as anti-HIV-1 agents: synthesis and biological activity of 1-benzothiepine 1,1-dioxide and 1-benzazepine derivatives containing a tertiary amine moiety. (5/16)

The search for orally active CCR5 antagonists was performed by chemical modification of the 1-benzothiepine 1,1-dioxide 3 and 1-benzazepine 4 lead compounds containing a tertiary amine moiety. Replacement of methyl group with a 2-(C(2-4) alkoxy)ethoxy group at the 4-position on the 7-phenyl group of the 1-benzothiepine ring resulted in both enhanced activity and significant improvement in the pharmacokinetic properties upon oral administration in rats. Introduction of C(2-4) alkyl, phenyl or (hetero)arylmethyl groups as the 1-substituent on the 1-benzazepine ring together with the 2-(butoxy)ethoxy group led to further increase of activity. Among the 1-benzazepine derivatives, the isobutyl (6i), benzyl (6o) or 1-methylpyrazol-4-ylmethyl (6s) compounds were found to exhibit highly potent inhibitory effects, equivalent to the injectable CCR5 antagonist 1, in the HIV-1 envelope-mediated membrane fusion assay. In particular, compound 6s showed the most potent CCR5 antagonistic activity (IC(50)=2.7 nM) and inhibitory effect (IC(50)=1.2 nM) on membrane fusion, together with good pharmacokinetic properties in rats. The synthesis of 1-benzothiepine 1,1-dioxide and 1-benzazepine derivatives and their biological activity are described.  (+info)

Protein kinase Cbeta is a critical regulator of dopamine transporter trafficking and regulates the behavioral response to amphetamine in mice. (6/16)

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The novel neuropeptide Y Y5 receptor antagonist Lu AA33810 [N-[[trans-4-[(4,5-dihydro[1]benzothiepino[5,4-d]thiazol-2-yl)amino]cyclohexyl]me thyl]-methanesulfonamide] exerts anxiolytic- and antidepressant-like effects in rat models of stress sensitivity. (7/16)

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Persistent (current) in the face of adversity ... a new class of cardiac anti-ischaemic compounds on the horizon? (8/16)

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1-Methyl-4-[3-[(2-methyltetrazol-5-yl)methyl]-5,6-dihydrobenzo[b][1]benzothiepin-5-yl]piperazine | C22H26N6S | CID 49781890 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
Read about the chemical and physical properties of (2R,3R)-2-(1-(2-((S)-1-amino-2-methylpropyl)-4-methylphenyl)piperazine-4-carbonyl)-3-(4-chlorophenyl)-N,N-dimethylpyrrolidine-1-carboxamide. Get (2R,3R)-2-(1-(2-((S)-1-amino-2-methylpropyl)-4-methylphenyl)piperazine-4-carbonyl)-3-(4-chlorophenyl)-N,N-dimethylpyrrolidine-1-carboxamide molecular formula, CAS number, boiling point, melting point, applications, synonyms and more here.
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Representative natural products containing benzoxa[3.2.1]octane skeleton and approaches to it.(a) Selected bioactive natural products having benzoxa[3.2.1]octan
Products list acetic acid, copper salt Aluminum, di m fluorotetrafluorodi 6 methyl 4 oxo 5,6 dihydrothieno 2,3 b thiopyran 2 sulfonamide 2 methylquinoline 6 carboxylic acid 1 methoxy 4 4 propylcyclohexyl benzene
Methyl 6-[4-(2-methylpropyl)piperazin-1-yl]pyridine-3-carboxylate | C15H23N3O2 | CID 14987938 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
Buy high quality N-[(1S)-1-(Aminocarbonyl)-2-methylpropyl]-1-[(3-fluorophenyl)methyl]-1H-indazole-3-carboxamide 1185282-19-2 from toronto research chemicals Inc.
51734-37-3 - KGGIFQOTGCPQAV-UHFFFAOYSA-N - 2-Propanol, 1-(bis(2-methylpropyl)amino)-3-(diethylamino)-, benzoate (ester), dihydrochloride - Similar structures search, synonyms, formulas, resource links, and other chemical information.
Comprehensive supplier list for Butanenitrile, 2-[(1-cyano-1-methylethyl)azo]-2-methyl-,Butanenitrile, 2-[(1-cyano-1-methylpropyl)azo]-2,3-dimethyl-
110-19-0 Isobutyl acetate testing. Laboratory testing for CAS number 110-19-0. Acetic acid, 2-methylpropyl ester;Acetic acid, isobutyl ester;«beta»-Methylpropyl ethanoate;2-Methylpropyl acetate;2-Methyl-1-propyl acetate;Isobutyl acetate fcc;Acetate disobutyle;Isobutyl ethanoate;2-Methylpropyl ethanoate;Isobutylester kyseliny octove;UN 1213;2-Methyl-1-propanol, acetate;i-Butyl acetate.
3-Methyl-6-phenyl-2-thioxo-2,3-dihydrothieno[3,2-d]pyrimidin- 4(1H)-one (2), on treatment with phosphorous oxychoride, affored 4-chloro-3-methyl-6-phenyl -thieno[3,2-d]pyrimidine- 2(3H)-thione (3). A series of novel 6-phenyl-thieno[3,2-d]pyrimidine derivatives 4-9 bearing different functional groups were synthesized via treatment of compound 3 with different reagents. On the other hand, compound 2 was used to synthesize ethyl-[(3-methyl-6-phenyl-2-thioxo-2,3-dihydrothieno[ 3,2-d]pyrimidin-4-yl)-oxy]acetate (10), 2-hydrazinyl- -3-methyl-6-phenyl-thieno[3,2-d]pyrimidin-4(3H)-one (11), 3-methyl-2-(methyl-sulfanyl)-6-phenyl-thieno[3,2-d]pyrimidin- 4(3H)-one (12) and N-(phenyl)/4-chlorophenyl or methoxy- phenyl)-2-[(3-methyl-4-oxo-6-phenyl-3,4-dihydrothieno[ 3,2-d]pyrimidin-2-yl)-sulfanyl]-acetamide (13a-c ...
Find quality suppliers and manufacturers of 220119-17-5(Avermectin A1a,25-cyclohexyl-4-O-de(2,6-dideoxy-3-O-methyl-a-L-arabino-hexopyranosyl)-5-demethoxy-25-de(1-methylpropyl)-22,23-dihydro-5-(hydroxyimino)-,(5Z)-) for price inquiry. where to buy 220119-17-5(Avermectin A1a,25-cyclohexyl-4-O-de(2,6-dideoxy-3-O-methyl-a-L-arabino-hexopyranosyl)-5-demethoxy-25-de(1-methylpropyl)-22,23-dihydro-5-(hydroxyimino)-,(5Z)-).Also offer free database of 220119-17-5(Avermectin A1a,25-cyclohexyl-4-O-de(2,6-dideoxy-3-O-methyl-a-L-arabino-hexopyranosyl)-5-demethoxy-25-de(1-methylpropyl)-22,23-dihydro-5-(hydroxyimino)-,(5Z)-) including MSDS sheet(poisoning, toxicity, hazards and safety),chemical properties,Formula, density and structure, solution etc.
4-methyl-N-(4-methylphenyl)-N-phenylaniline 20440-95-3 NMR spectrum, 4-methyl-N-(4-methylphenyl)-N-phenylaniline H-NMR spectral analysis, 4-methyl-N-(4-methylphenyl)-N-phenylaniline C-NMR spectral analysis ect.
4H-Indolo[4,3-fg][3,1]benzoxazine,6,6a,7,8,10,- 10a-hexahydro-7,8-dimethyl-10-(1-methylethenyl)-,(6aR,8R,10R,10aR)- 1,3-bis(2-methylprop-2-enyl)-2-prop-2-enoxy-benzene Benzeneacetic acid, alpha-methyl-4-(4-oxo-2-(propylthio)-3(4H)-quinazolinyl)-, methyl ester 4-methyl-6-(2,2,3,3,4,4,5,5-octafluoropentoxy)pyrimidin-2-amine 2-Propanol, 1-((1-methylpropyl)thio)-3-(6,7,10,11-tetramethoxyemetan-2-yl)-, 2HCl Benzyl (3S-(2(R*),3alpha,8abeta))-1-(3-benzylhexahydro-1,4-dioxopyrrolo(1,2-a)pyrazin-2(1H)-yl)-1-oxopropane-2-carbamate 4-(4,5-dichloro-6-oxo-pyridazin-1-yl)benzenesulfonamide 3-(benzyl-methyl-amino)-1-naphthalen-2-yl-propan-1-one 4-amino-4-methyl-pentanoic acid 6-amino-5H-purine-2-sulfonamide
Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...
Diazotization of 4-fluoroanthranilic acid (V) and the following reaction with sodium disulfide gave the dithio diacid VII which was reduced with lithium aluminium hydride to 4-fluoro-2-mercaprobenzyl alcohol (XI). Its reaction with 2-chloro-5-iodothiophene afforded the alcohol XIII which was transformed via the chloride XIV and the nitrile XV to [2-(5-chloro-2-thienylthio)-4-fluorophenyl]acetic acid (XVI). Cyclization with phosphorus pentoxide in toluene resulted in 2-chloro-8-fluorothieno[2,3-b]-1-benzothiepin-4(5H)-one (XVIII) which was converted via the alcohol XIX to the chloro derivative XX. The substitution reaction with 1-methylpiperazine led to the title compound IV which is a long-acting and very potent tranquillizer but did not reveal, in the animal tests performed, the properties of a neuroleptic agent.. ...
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Structure, properties, spectra, suppliers and links for: N-(1-Cycloheptyl-3-piperidinyl)-3-(5-methyl-1H-pyrazol-1-yl)propanamide.
You are viewing an interactive 3D depiction of the molecule n-{[4-(5-methyl-3-phenyl-1,2-oxazol-4-yl)phenyl]sulfonyl}propanamide (C19H18N2O4S) from the PQR.
Structure, properties, spectra, suppliers and links for: 3-Methyl-N-{4-[4-(2-methyl-2-butanyl)phenoxy]phenyl}-2-thiophenecarboxamide.
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11 trihydroxy 9 2 hydroxyacetyl 4 methoxy 8,10 dihydro 7H tetracene 5,
12 dione 3 O methyl 5 O 2 methylpropyl
2,6 dimethyl 4 2 nitrophenyl 1,4 dihydropyridine 3,5 dicarboxylate
The National Institute of Standards and Technology (NIST) uses its best efforts to deliver a high quality copy of the Database and to verify that the data contained therein have been selected on the basis of sound scientific judgment. However, NIST makes no warranties to that effect, and NIST shall not be liable for any damage that may result from errors or omissions in the Database ...
The National Institute of Standards and Technology (NIST) uses its best efforts to deliver a high quality copy of the Database and to verify that the data contained therein have been selected on the basis of sound scientific judgment. However, NIST makes no warranties to that effect, and NIST shall not be liable for any damage that may result from errors or omissions in the Database ...
0033]Starting materials of formula (III) of the present invention are available commercially or from known methods in the art as disclosed in the following list: [0034]2,5-dimethyl-3(2H)-furanone, from Ryan Scientific Product List. [0035]4-(1,1-dimethylethyl)-2,5-dimethyl-3(2H)-furanone, from JP10036259. [0036](S)-2,5-dimethyl-3(2H)-furanone and (R)-2,5-dimethyl-(2H)-furanone, from Eghbaldar et al., Parfums, Cosmetiques, Aromes (1992), 104, 71-8. [0037](R)-5-hexyl-2-methyl-3(2H)-furanone and (S)-5-hexyl-2-methyl-3(2H)-furanone, from Mosandl et al. Journal of High Resolution Chromatography (1990), 13(9), 660-2. [0038]2-methyl-4-(2-methylpropyl)-3(2H)-furanone and 2-methyl-4-pentyl-3(2H)-furanone, from Baraldi et al. Tetrahedron (1987), 43(1), 235-42. [0039]2-methyl-5-(2-methylpropyl)-3(2H)-furanone, 2-methyl-5-phenyl-3(2H)-furanone, and 2-methyl-5-pentyl-3(2H)-furanone, from Baraldi et al. Tetrahedron Letters (1984), 25(38), 4313-16. [0040]5-hexyl-2-methyl-3(2H)-furanone, from Winkler et al. ...
IN CONNECTION WITH A STUDY OF POLYMERS CONTAINING HIGH-ENERGY GROUPS, POLY( -nitro-2-methylpropyl methacrylate) was prepared in both the isotactic (m.p. above 300 C.) and the atactic (m.p. 280 C.) forms. Isotactic poly(2-nitro-2methylpropyl methacrylate) was prepared by adding the monomer to a relatively large amount of toluene containing phenylmagnesium bromide as a catalyst. Atactic poly(2-ni ro-2-met ylpropyl m h cryl ) AS PREP RED BY A CONVENTIO AL FREE RADICAL-TYP POLYMERIZATION USING AZOBISISOBUTYRONITRILE. Similarly, isotactic poly(methyl methacrylate) (m.p. 140-160 C.) was prepared and compared with a commercially available sample of atactic poly(methyl methacrylate) (m.p. 120125 C.). Contrary to previous observations that the isotactic form of a polymer had higher mechanical strength than the atactic form, a actic poly(methyl methacrylate) had a higher tensile strength than the isotactic modification. (Author)*ACRYLIC RESINS
1,2,4-Trifluoro-5-nitrobenzene 2105-61-5 route of synthesis, 1,2,4-Trifluoro-5-nitrobenzene chemical synthesis methods, 1,2,4-Trifluoro-5-nitrobenzene synthetic routes ect.
88133-19-1 - KIGWLQJAJQIKNY-PLCQNAAUSA-N - alpha-Cyano-9,10-didehydro-6-methyl-ergoline-8-propanamide, (8beta)- - Similar structures search, synonyms, formulas, resource links, and other chemical information.
US EPA PC Code ); 012303 (US EPA PC Code Text ); 5-Bromo-3-sec-butyl-6-methyluracil, sodium salt; 5-Bromo-6-methyl-3-(1-methylpropyl)-2,4(1H,3H)-pyrimidinedione, sodium salt; 69484-12-4 (CAS number); 69484124; 69484124 (CAS number without hyphens); 842 (CA DPR Chem Code) ); Bromacil, sodium salt; BROMACIL, SODIUM SALT (CA DPR Chem Code Text ); Bromacilsodiumsalt; Uracil, 5-bromo-3-sec-butyl-6-methyl-, sodium ...
SIDDHARTH INTERCHEM PVT. LTD. - Exporter, Manufacturer & Supplier of Itraconazole Intermediate 1-(4-Methoxyphenyl)-4-(4 -nitrophenyl) piperazine (IT - 1),2,4-Dihydro-4-[4-[4-(4-hydroxyphenyl]-1-piperazinyl]-phenyl]-2-(1-methylpropyl)-3H-1,2,4-triazol-3-one (IT - 7),1-(4-Methoxyphenyl) piperazine,Cis Bromo Benzoate,Cis Mesylate, India
The expression of P-glycoprotein (P-gp) in tumor cells causes a multidrug resistance (MDR) phenotype. P-gp has been shown to mediate the transport of structurally dissimilar drugs across the cell membrane in an energy-dependent manner. In this report, we show that BIBW22 BS, a phenylpteridine analog, reverses the MDR phenotype of CEM human lymphoma cells in a dose-dependent fashion. Using a photoactive analog of BIBW22 BS {[3H]azido-4-[N-(2-hydroxy-2-methylpropyl)-ethanolamino]-2, 7-bis(cis-2,6-dimethyl-morpholino)-6-phenylpteridine}, we show the photoaffinity labeling of a 170-kDa protein in drug-resistant cells immunoprecipitated with P-gp-specific monoclonal antibodies. The photolabeling of P-gp by [3H]azido-BIBW22 BS was specific and saturable. Furthermore, BIBW22 BS, vinblastine, and verapamil, but not colchicine, inhibited the photolabeling of P-gp by [3H]azido-BIBW22 BS. Drug binding studies showed that membranes from MDR cells bound more BIBW22 BS than parental drug-sensitive cells, and ...
The present invention relates to novel carbamate intermediate of formula (II), process for its preparation and process for its conversion into 3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl]phen
sec-Butanol, sec-Butanol Product Name: sec-Butanol Synonyms: (R,S)-Butan-2-ol;(RS)-2-butanol;1-Methyl propanol;1-methylpropanol;1-Methylpropyl alcohol;1-methylpropylalcohol;2-butanol,DL-;Alcool butylique sec, Auto Classifieds.
Picaridin Icaridin 119515-38-7 97% In stock suppliers TCCS9 - Tocopharm Products Made In China, China Manufacturer. Icaridin Product Name: Icaridin Cas No: 119515-38-7 ; 107133-36-8 Synonyms: KBR 3023;Picaridin;1-(1-methyl-propoxycarbonyl)-2-(2-hydroxyethyl)-piperidine;1-(1-methylpropoxycarbonyl)-2-(2-hydroxyethyl)piperidine;1-methylpropyl2-(2-hydroxyethyl)-1-piperidinecarboxylate
Product Number: C5716 CAS number: 755038-65-4 Synonyms: N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy-benzamide. ...
You are viewing an interactive 3D depiction of the molecule (9r,21r)-1-[(2r,3s,4r,5r)-5-(6-amino-9h-purin-9-yl)-4-hydroxy-3-(phosphonooxy)tetrahydro-2-furanyl]-3,5,9,21-tetrahydroxy-n,n,n,8,8-pentamethyl-10,14,19-trioxo-2,4,6-trioxa-18-thia-11,15-diaza-3,5-diphosphadocosan-22-aminium 3,5-dioxide (C28H28N8O18P3S+) from the PQR.
Trimetazidine is an anti-ischaemic agent with direct cardioprotective effects. It has been developed by the French company Servier for the prophylactic
Compare the utility of different models and approaches 2- Describe and explain the rationale behind the current pharmacological treatment of pulmonary arterial hypertension, Also, based on what is known about the pathophysiology of this condition, propose two additional mechanisms, not currently exploited, which might be targeted in order to treat it.. Type of service-Academic paper ...
A method for the prophylaxis and treatment of irritable bowel syndrome, which comprises administering a pharmaceutically effective amount of at least one compound selected from the group consisting of ( )-2-(4-chlorophenyl)-5,6-dihydro-[1]benzothiepino [5,4-c]pyridazin-3(2H)-one 7-oxide, optical isomers thereof and 2-(4-chlorophenyl)-5,6-dihydro-[1]benzothiepino[5,4-c]pyridazin-3(2H)-one 7,7-dioxide to a subject in need of such prophylaxis or treatment.
Ceballos, Cesar C., Antonio C. Roque, and Ricardo M. Leão. A negative slope conductance of the persistent sodium current prolongs subthreshold depolarizations. Biophysical journal 113.10 (2017): 2207-2217.
M. F. Shuba, "Pathways and mechanisms of transmembrane entry of Ca ions, responsible for activation of contraction, into the smooth muscle cells,"Fiziol. Zh.,27, No. 4, 533-540 (1981).PubMedGoogle Scholar ...
Wear a self-contained breathing apparatus in pressure-demand, MSHA/NIOSH (approved or equivalent), and full protective gear. During a fire, irritating and highly toxic gases may be generated by thermal decomposition or combustion. Extinguishing media: Use agent most appropriate to extinguish fire. In case of fire use water spray, dry chemical, carbon dioxide, or appropriate foam ...
Corticobasal degeneration (CBD) is a neurodegenerative parkinsonian disorder of unknown cause that shows considerable clinical heterogeneity. In CBD, activated microglia have been shown to be associated closely with the extensive tau pathology found in the affected basal ganglia, brainstem nuclei, and cortical regions. We report on the use of [(11)C](R)-(1-[2-chlorophenyl]-N-methyl-N-[1-methylpropyl]-3-isoquinoline ...
TABLE-US-00006 Structure and Example # Chemical name, Analytical data and comments ##STR00077## 3-[(2-cyanopyridin-2-yl)amino]-6,6-dimethyl-N- [trans-2-phenylcyclopropyl]-4,6-dihydropyrrolo[3,4- c]pyrazole-5(1H)-carboxamide 1H NMR (CD3OD) δ: 1.03-1.15 (m, 2 H), 1.66 (s, 6 H), 1.75-2.01 (m, 1 H), 2.51-2.75 (m, 1 H), 4.59 (s, 2 H), 6.81-6.96 (b, 1 H), 7.00-7.07 (m, 3 H), 7.10-7.17 (m, 2 H), 8.20 (d, J = 6.06 Hz, 1 H). LCMS (APCl, M + H.sup.+): 415.1. HPLC-UV Detection: ,95% purity Method of Example 31 using 4-chloropyrimidine-2- carbonitrile in place of 31c. ##STR00078## 6,6-dimethyl-3-[(2-methyl-6-morpholin-4-ylpyrimidin-4- yl)amino]-N-[trans-2-phenylcyclopropyl]-4,6- dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide 1H NMR (400 MHz, DMSO) δ: 1.04-1.21 (m, 2 H), 1.63 (s, 6 H), 2.42 (s, 3 H), 2.75 (m, 1 H), 4.28 (m, 2 H), 6.05 (s, 1 H), 6.31 (m, 1H) 7.09-7.27 (m, 5H). Anal. (C26H32N8O8•1.6TFA•2.2H2O) C, H, N. APCl- MS: [M + H] 489. Method of Example 31 using 4-chloro-2-methyl-6- ...
Guzei IA, Spencer LC, Lin Q, Blackwell HE. N-{(Aminocarbonyl) (S)-4-nitrobenzyl methyl}-N-{ (R)-cyclohexyl (cyclohe xylaminocarbonyl)methyl}propanamide methanol solvate. Acta Crystallographica Section E-Structure Reports Online. 2007 ;63:O1892-O1894. ...
WZ4003;1214265-58-3;N-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]propanamide;ABP001164.Active Biopharma Corp
Fosamprenavir BASE CAS 226700-79-4 [(1S,2R)-3-[[(4-Aminophenyl)sulfonyl](2-methylpropyl)amino]-1-(phenylmethyl)-2-(phosphonooxy)propyl]carbamic acidC-[(3S)-tetrahydro-3-furanyl] ester Additional Names: (3S)-tetrahydro-3-furyl [(aS)-a-[(1R)-1-hydroxy-2-(N1-isobutylsulfanilamido)ethyl]phenethyl]carbamate dihydrogen phosphate (ester) Manufacturers Codes: VX-175 Molecular Formula: C25H36N3O9PS Molecular Weight: 585.61 Percent Composition: C 51.27%, H 6.20%, N 7.18%, O 24.59%, P 5.29%, S 5.48% WO 9933815 PRODUCT PATENT Fosamprenavir Systematic (IUPAC) name {[(2R,3S)-1-[N-(2-methylpropyl)(4-aminobenzene)sulfonamido]-3-({[(3S)-oxolan-3-yloxy]carbonyl}amino)-4-phenylbutan-2-yl]oxy}phosphonic acid Clinical data Trade names Lexiva AHFS/Drugs.com monograph…
Compounds. Compound I [IUPAC name: N-(3-fluoro-4-((7-methoxy-4-quinolinyl)oxy)phenyl)-1-(2-hydroxy-2-methylpropyl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide] was synthesized at Amgen, Inc. The MAPK/extracellular signal-regulated kinase (ERK) kinase 1/2 (MEK1/2) inhibitor U0126 was obtained from Calbiochem.. Cells. KATOIII (gastric), PC3 (prostate), HT-29 (colorectal), Colo205 (colorectal), BxPC3 (pancreatic), and U-87 MG (glioblastoma) cancer cell lines were obtained from the American Type Culture Collection. NIH3T3 TPR-Met or NIH3T3 RON cells were generated by stable transfection of TPR-Met, a constitutively active, ligand-independent form of c-Met ( 31) or wild-type RON in NIH3T3 cells. Cells were grown as monolayers using standard cell culture conditions.. Antibodies and reagents. Antibodies against c-Met (C-12), RON (C-20), and actin (1615-R) were acquired from Santa Cruz Biotechnology. Antibodies against phospho-c-Met (Y1234/1235), phospho-Gab1 (Y627), phospho-ERK1/2 ...
Analogues of (phenoxymethyl)benzene for sale. 4-[(3,4-dichlorophenyl)methoxy]-3-ethoxybenzaldehyde to {[4-(benzyloxy)phenyl]methyl}(2-methylpropyl)amine
Medical definition of tertiary amine: an amine (as trimethylamine or nicotine) having three organic groups attached to the nitrogen in place of three hydrogen atoms.
Learn more about n-4-4-methylphenyl-1-3-thiazol-2-yl-guanidine. We enable science by offering product choice, services, process excellence and our people make it happen.
Learn more about 2-phenyl-1-3-thiazol-5-yl-methyl-amine-hydrochloride. We enable science by offering product choice, services, process excellence and our people make it happen.
Trifluoromethylbenzene / Nitrobenzene / Anilide / Phenoxy compound / Nitroaromatic compound / N-arylamide / Phenol ether / Alkyl aryl ether / Fluorobenzene / HalobenzeneAryl fluoride / Aryl halide / Tertiary alcohol / Carboxamide group / Secondary carboxylic acid amide / C-nitro compound / Organic nitro compound / Carboxylic acid derivative / Ether / Organic 1,3-dipolar compound / Propargyl-type 1,3-dipolar organic compound / Allyl-type 1,3-dipolar organic compound / Organic oxoazanium / Alkyl halide / Alkyl fluoride / Hydrocarbon derivative / Organic nitrogen compound / Alcohol / Organic oxide / Carbonyl group / Organopnictogen compound / Organohalogen compound / Organic oxygen compound / Organofluoride / Organonitrogen compound / Organooxygen compound / Organic zwitterion / Aromatic homomonocyclic compound ...
It is shown that the 3-benzoyl-2-isopropyl-4-alkyloxazolidin-5-ones (12), derived from isobutyraldehyde and ?-amino acids are as efficient as, but more economical than, the corresponding tert-butyl compounds (9), as sources of enantiopure ?,?-dialkylated ?-amino acids (e.g., 21-23). In the absence of alkylating agents, the anions of (2R,4S)-12 and its enantiomer undergo a fragmentation-recombination process to generate (1S,2R,4S)-N-[1-(3-benzoyl- 2-isopropyl-4-methyl-5-oxo-oxazolidin-4-yl)-2-methylpropyl]benzamide ((1S, 2R,4S)-20), and its enantiomer. Acidic methanolysis of these condensation products provides access to ?,?-dialkylated ?,?-diaminopropionic acids [e.g., (2S,3S)-2,3-bisbenzoylamino-2,4-dimethylpentanoic acid methyl ester ((2S,3S)-24)). ...
Other names: 4-Methyl-2-pentanone, Isopropylacetone, Hexone, Isobutyl methyl ketone, 2-Methylpropyl methyl ketone, 4-Methyl-2-oxopentane, MIK, Isobutylmethyl ketone, MIBK, Isohexanone
This paper shows that persistent sodium current critically contributes to the subthreshold nonlinear dynamics of CA1 pyramidal neurons and promotes rapidly reversible conversion between place-cell and silent-cell in the hippocampus. A simple model built with realistic axo-somatic voltage-gated sodium channels in CA1 (Carter et al., 2012; Neuron 75, 1081-1093) demonstrates that the biophysics of persistent sodium current is sufficient to explain the synaptic amplification effects. A full model built previously (Grienberger et al., 2017; Nature Neuroscience, 20(3): 417-426) with detailed morphology, ion channel types and biophysical properties of CA1 place cells naturally reproduces the steep voltage dependence of synaptic responses ...
Propyl-ammonium 4,4,4-trifluoro-1-(naphthalen-2-yl)butane-1,3-dionate.: The title salt, C(3)H(10)N(+)·C(14)H(8)F(3)O(2) (-), constitutes the first organic cryst
Polysarcosine (M-n = 3650-20 000 g mol(-1), D similar to 1.1) was synthesized from the air and moisture stable N-phenoxycarbonyl-N-methylglycine. Polymerization was achieved by in situ transformation of the urethane precursor into the corresponding N-methylglycine-N-carboxyanhydride, when in the presence of a non-nucleophilic tertiary amine base and a primary amine initiator.
Cardiovascular drugs attenuated myocardial resistance against ischaemia-induced and reperfusion-induced injury in a rat model of repetitive occlusion ...
Pharmaceutical drug precursors China, Piroxicam Cas No 36322 90 4, Synonyms: PIROXICAM;PIROXICAMUM;2H-1, 2-Benzothiazine-3-carboxamide, 4-hydroxy-2-methyl-N-2-pyridinyl-, 1, 1-dioxide;2h-...
All participants were asked to take one capsule at the same time each day throughout the study.. This single-center trial was conducted in the United States. The overall time to participate in this study was approximately 7 weeks. Participants made 2 visits to the clinic, including 18 days confinement to the clinic, and were contacted by telephone 1 day and 27 days after leaving confinement for a follow-up assessment. ...
DI-fusion, le Dépôt institutionnel numérique de lULB, est loutil de référencementde la production scientifique de lULB.Linterface de recherche DI-fusion permet de consulter les publications des chercheurs de lULB et les thèses qui y ont été défendues.
Tacrolimus 8-Propyl Analog (USP) ;. Dihydro Tacrolimus ;. Dihydro FK-506 ;. Tsukubamycin B ;. CAS # 104987-30-6 ;. C44H71NO12 ;. MW: 806.03 ;. ...
Find information about Kinston, NC physics department options. Check with each technical school below for assistance with atomic physics certificate program requirements, degree prerequisites, and class registration. Are you are considering an associates degree in electronics engineering, or a bachelor of science in mechanical or civil engineering?
This asymmetrical dress unexpectedly and originally reinterprets the classic and feminine lines so dear to women who love discreet elegance. The high neck and the skirt that falls in soft waves make this dress highly refined and chic.
Cleavage of 3,3,4-trifluoro-2,2-dimethyloxetane (I) in an aqueous solution of sulphuric acid, phosphoric acid, hydrogen chloride, or hydrogen bromide gave a mixture of 2,2-difluoro-3-methyl-3-butenal (II) and 5,5-difluoro-2-(1,1-difluoro-2-hydroxy-2-methylpropyl)-4-hydroxy-6,6-dimethyl-1,3-dioxane (VIa); in the cleavage effected by hydrochloric or hydrobromic acid the mixture also contained 3-chloro- or 3-bromo-2,2-difluoro-3-methyl-1,1-butanediol (Vb or Vc). In alcoholic solutions of the mineral acids the cleavage afforded the corresponding acetals of butenal II and 2,2-difluoro-3-hydroxy-3-methylbutanal (IIIa). The action of sulphuric acid in the presence of acetyl chloride or acetanhydride led to 1-chloro-2,2-difluoro-3-methyl-3-butenyl acetate (IVd) or 2,2-difluoro-3-methyl-3-butenylidene diacetate (IVe), as the main product. Butenal II was a sole product of the cleavage of oxetane I by polyphosphoric acid at 150-160 °C in the gaseous phase. At temperatures above 180 °C there were also ...
2,2,2-trifluoro-1-propan-2-yloxy-ethanimine Altechromone B 4-methyl-N-[2-methyl-4-oxo-3-[(4-oxo-3,5-ditert-butyl-1-cyclohexa-2,5-dienylidene)amino]oxy-5-propan-2-yl-1-cyclohexa-2,5-dienylidene]benzenesulfonamide 2-(3-(N-Methylacetamido)-2,4,6-triiodophenoxy)propionic acid see 1,3-Dioxolane,2-(8-nonynyl)- 3-(3-chloro-2-methyl-phenyl)-2-tert-butyl-1-(1,3-thiazol-2-yl)guanidine 2-Propenoic acid, 2-methyl-, polymer with butyl 2-propenoate, ethenyl acetate and 2-ethylhexyl 2-propenoate N-(3-methylphenyl)-2,4-dinitro-aniline 4-methoxy-4-phenyl-hexan-3-one 2-Methyltetradecanoic acid
Insecticidal neurotoxin that modulates the insect Nav channel (DmNaV1/tipE (para/tipE)) in a unique manner, with both the activation and inactivation processes being affected. The voltage dependence of activation is shifted toward more hyperpolarized potentials (analogous to site 4 toxins) and a non-inactivating persistent sodium current is induced (site 3-like action). Interestingly, both effects take place in a voltage-dependent manner, producing a bell-shaped curve between -80 and 0 mV.
A dispersant derivatized from a functionalized hydrocarbon and a polyamine having one primary amine and 1-10, preferably 3-8 secondary or tertiary amines; preferably where said functionalized hydrocarbon is a Koch-derived hydrocarbon.
Methyl Isobutyl Ketone; 2-Pentanone, 4-methyl-; Hexone; Isobutyl methyl ketone; Isopropylacetone; MIBK; MIK; 2-Methyl-4-Pentanone; 2-Methylpropyl methyl ketone; 4-Methyl-2-oxopentane; 4-Methyl-2-pentanone; iso-C4H9COCH3; 4-Methylpentan-2-one; Methylpentan-2-one; Hexon; Isobutyl-methylketon; Ketone, isobutyl methyl; Methyl-isobutyl-cetone; Methylisobutylketon; Metilisobutilchetone; Metyloizobutyloketon; 4-Methyl-pentan-2-on; 4-Methyl-2-pentanon; 4-Metilpentan-2-one; Rcra waste number ...
Rovatirelin Hydrate, S-0373, Rovatirelin, RN: 204386-76-5 UNII: 9DL0X410PY (4S,5S)-5-methyl-N-((2S)-1-((2R)-2-methylpyrrolidin-1-yl)-1-oxo-3-((1,3-thiazol-4-yl)methyl)propan-2-yl)-2-oxo-1,3-oxazolidine-4-carboxamide (4S,5S)-5-methyl-N-((S)-1-((R)-2-methylpyrrolidin-1-yl)-1-oxo-4-(thiazol-4-yl)butan-2-yl)-2-oxooxazolidine-4-carboxamide4-Oxazolidinecarboxamide, 5-methyl-N-[2-(2-methyl-1-pyrrolidinyl)-2-oxo-1-(4-thiazolylmethyl)ethyl]-2-oxo-, [4S-[4α[R*(S*)],5α]]- Phase III A thyrotropin-releasing hormone potentially for the treatment of spinocerebellar ataxia. CAS No.204386-76-5(Rovatirelin) 879122-87-9(Rovatirelin Hydrate) C17H24N4O4S Exact Mass: 380.1518 Rovatirelin is a novel synthetic agent that mimics the actions of thyrotropin-releasing hormone (TRH). Rovatirelin binds to the human TRH receptor with higher affinity (Ki=702nM) than taltirelin (Ki=3877nM).…
Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...
Huang WS, Metcalf CA, Sundaramoorthi R, Wang Y, Zou D, Thomas RM, Zhu X, Cai L, Wen D, Liu S, Romero J, Qi J, Chen I, Banda G, Lentini SP, Das S, Xu Q, Keats J, Wang F, Wardwell S, Ning Y, Snodgrass JT, Broudy MI, Russian K, Zhou T, Commodore L, Narasimha (2010). Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including th J Med Chem, 53 (12), 4701-4719 DOI: 10.1021/jm100395q ...
Quick Search Product Directory Listing in Alphabetical Index9 on Drugdu.com for 2 3 Dihydro 1 4 dioxino 2 3 b pyridin 7 yl methanol|||1016579053663842304|||hairuichem, 6 Bromo 7 methyl 1H indole|||1016579052862730240|||hairuichem, 2 3 5 dichlorophenyl ethanol|||1016579052053229568|||hairuichem and more.
1,3-isoquinolinedione / 2,3-dihydroisoquinoline-1,4-dione / Isoquinolone / Benzyloxycarbonyl / Phenylacetamide / Tetrahydroisoquinoline / Aryl ketone / N-arylamide / Chlorobenzene / HalobenzeneAryl chloride / Aryl halide / Monocyclic benzene moiety / Benzenoid / Carboxylic acid imide / Vinylogous amide / Dicarboximide / Carboxylic acid imide, n-unsubstituted / Ketone / Secondary carboxylic acid amide / Carboxamide group / Carboxylic acid ester / Monocarboxylic acid or derivatives / Azacycle / Carboxylic acid derivative / Organonitrogen compound / Organic nitrogen compound / Organic oxygen compound / Carbonyl group / Organooxygen compound / Hydrocarbon derivative / Organic oxide / Organopnictogen compound / Organohalogen compound / Organochloride / Aromatic heteropolycyclic compound ...
Starting up at: $0.95 $one.08 Save: 12% Temaril-P(R) Tablets (trimeprazine with prednisolone) The special Temaril-P method combines the antipruritic and antitussive action of trimeprazine with the anti-inflammatory action of prednisolone. Product Technical specs: To be used: Dogs Producer: Pfizer Animal Wellbeing Dosage: Use as Directed by your Veterinarian COMPOSITION: Each and every pill contains trimeprazine tartrate (USP) ten-[three-(Dimethylamino)-2-methylpropyl] phenothiazine tartrate (two:one) comparable to trimeprazine five mg and prednisolone two mg. Tips To be used: one. Antipruritic: Temaril-P is usually recommended to the relief of itching irrespective of cause. Its usefulness has become demonstrated for the relief of itching and also the reduction of inflammation generally related with most skin disorders of dogs including the eczema caused by interior Ailments otitis and dermatitis (allergic parasitic pustular and nonspecific). It usually relieves pruritis which will not reply to ...
We investigated the effect of proteases, widely used for neuron isolation in electrophysiological studies, on the amplitude and kinetic characteristics of persistent sodium current (INaP) in hippocampal CA1 pyramidal neurons. Properties of INaP were studied on neurons isolated by mechanical treatment (control group) and by mechanical and enzymatic treatment using pronase E (from Streptomyces griseus) or protease type XXIII (from Aspergillus oryzae). We show that in neurons isolated with pronase E kinetic of activation and density of INaP was unaltered. Enzymatic treatment with protease type XXIII did not alter INaP activation but result in significant decrease in INaP density. Our data indicates that enzymatic treatment using pronase E for neuron isolation is preferable for investigation of INaP ...
We performed a meta-analysis of RCT evaluating the effect of trimetazidine compared with placebo control on cardiac function variables, clinical symptoms and major adverse events in patients with chronic HF. We found trimetazidine treatment resulted in better cardiac function for ischaemic and non-ischaemic HF, and improved clinical symptoms. More importantly, trimetazidine was associated with a significant reduction in the RR for mortality, cardiovascular events and hospitalisation.. Trimetazidine is initially used as an anti-ischaemic or cytoprotective agent through a metabolic pathway: switching cardiac metabolism from FFA to glucose oxidation, which is efficient in terms of oxygen consumption and energy production. Because FFA inhibitors can act as metabolic modulators in protecting the ischaemic myocardium, the effects of trimetazidine on HF have previously been assessed mainly in patients with ischaemic HF. The results of several small RCT have revealed improved cardiac function with ...
In vitro stress assays are commonly used to study responses of plants to abiotic stress and to assess stress tolerance. A literature review reveals that most studies use very high stress levels, and measure criteria such as germination, plant survival, or development of visual symptoms such as bleaching. However, we show that these parameters are indicators of very severe stress, and such studies thus only provide incomplete information about stress sensitivity. Similarly, transcript analysis revealed that typical stress markers are only induced at high stress levels in young seedlings. Therefore, tools are needed to study the effects of mild stress. We found that the commonly used stress-inducing agents mannitol, sorbitol, NaCl and H2O2 impact shoot growth in a highly specific and dose-dependent way. Therefore, shoot growth is a sensitive, relevant and easily measured phenotype to assess stress tolerance over a wide range of stress levels. Finally, our data suggest that care should be taken ...
Think the paper was decent. I think that I found the majority of it OK. I know for certain that I have lost two marks stupidly, however: I said that you could reduce a carboxylic acid for the last question. Can you add a halogenoalkane to the NH group in paracetamol? I wasnt sure, so I put it anyway, in other words, it would form a tertiary amine?? And yes, I said NaOH would react with both, but yes it would form two productS ...
The major finding in this study is that an increase in the inward sodium current INaP plays an important role in causing long QT syndrome in murine models of diabetes. Previous studies suggested that the cardiac repolarization defect in diabetes is due mainly to a decrease in outward potassium currents. Using streptozotocin-induced diabetic rats as a model of type 1 diabetes, it was concluded that APD prolongation is due to reductions in the 4-AP-sensitive transient outward current Ito and a 4-AP-insensitive steady-state current referred to as IK (19-21). A decrease in the inward L-type calcium current ICaL was also seen in streptozotocin-induced diabetic rats (21) and Ins2Akita mice (18), but this would tend to shorten the APD. APD prolongation and suppression of outward potassium currents and ICaL were also seen in cardiac myocytes from type 2 diabetic db/db mice (22-25). The affected potassium currents in db/db mice were not extensively characterized, but were probably equivalent to Ito and ...
Introduction: Despite hundreds of training models for microsurgery being available in the literature, very few of them are scientifically validated. We chose to validate our low-fidelity training model on flower petals by comparing it headto-head with a moderate fidelity training model, the anastomosis on chicken leg femoral artery. Materials and methods: A total of 16 participants of different levels of expertise were randomized into 2 groups, 1 training on flower petals and 1 on chicken leg femoral arteries. The groups were evaluated on performing a rat femoral artery anastomosis using the validated Stanford Microsurgical Assessment (SMaRT) Scale. The Mann-Whitney U test was used to check for statistically significant differences between the groups. The flower petal sutures were also evaluated and Pearson correlation was used to check for associations between better petal anastomosis scores and better final SMaRT results. Results: After 6 weeks of flower petal training, microsurgical trainees ...
The invention provides aqueous, solvent based, and solvent-free curable coating compositions which include (A) the reaction product of epoxy resin, acid, and tertiary amine; (B) reactive diluent, and, optionally, (C) curing agent. The compositions are useful for forming cured coated substrates, that are especially suitable for food and beverage packaging.
N-[4-(3-methyl-1,2,4-oxadiazol-5-yl)-1,3-thiazol-2-yl]guanidine - C7H8N6OS, synthesis, structure, density, melting point, boiling point
Incorporates a phase consisting of a 2,3,6-tri-O-methyl derivative of beta-cyclodextrin. This phase exhibits broad chiral selectivity and is good for terpenes and tertiary amines.
Reaction products between monomeric epichlorohydrin and a tertiary amine when applied to the surface of a substrate, such as paper, produce an electroconductive surface useful in electrographic image reproduction. Both a coated paper product and a process of producing it are provided.
Lu AA21004 was discovered by H. Lundbeck A/S, and is under co-development by H. Lundbeck A/S and Takeda for the treatment of major depressive disorder and general anxiety disorder.. Major depressive disorder (MDD) is a chronic, recurring disease with considerable morbidity in the general population. The estimated lifetime prevalence of major depression in the adult population is 5 to 25%, with approximately 2-fold higher prevalence in women than in men. The hallmark of the disease is a depressed mood, with additional symptoms including sleep disturbances, psychomotor agitation or retardation, sexual dysfunction, weight loss, concentration difficulties and delusional ideas. In addition to direct ill effects, MDD causes suicide or job loss and exerts indirect influence on social economy.. This long-term extension study will assess the safety and efficacy of 52-week treatment with Lu AA21004 in participants with major depressive disorder after completion of the 8-week double-blind treatment period ...
The synthesis of a small library of dihydrouracils spiro-fused to pyrrolidines is described. These compounds are synthesized from b-aryl pyrrolidines, providing products with the 2-arylethyl amine moiety, a structural feature often encountered in compounds active in the central nervous system. The b-aryl pyrrolidines are synthesized through a three-step methodology that includes a Knoevenagel condensation reaction, a 1,3-dipolar cycloaddition reaction, and a nitrile reduction.
The salts of the present invention can be easily obtained by mixing hydroxide or a suitable salt of the desired metal with a solution or slurry of the compound of formula I in one of the above mentioned slightly polar aprotic solvents. Alternatively, when the hydroxide or salt of the desired metal is not soluble enough to start the reaction a small amount of water can be added to the solution or slurry In the organic solvent and the water can be removed by azeotropic destination. In that case an apoiar aprotic solvent which forms an azeotrope with water has to be selected. For metals that have a highly insoluble hydroxide the metal can be added in the form of an ethoxide (e.g. Mg(OEt)2) or as a mixed hydroxide/carbonate (3Zn(OH)2.2ZnC03).The preferred solvent for the above method Is methyl tertiairy methyl ether or ethyl acetate. When the salt has been obtained in solution it can be isolated by first removing the water mat is still available by azeotropic distillation, followed by mixing with a ...
The process you describe is absolutely correct. The process has been practiced for decades and markets have been found (and still exist) for every distillation fraction. Just about nothing goes to waste. Also, given that it appears the key step in this Akzo process involves nucleophilic ring-opening it is not clear to me that it will or should be selective either - once nitrogen is alkylated it becomes a better nucleophile and thus gives secondary and tertiary amines. Profit margins in the ethyleneamines/ethanolamines business are quite healthy. Youd have to have a very significant change in economics to enter this market and compete.. Delete ...
This protein is involved in the oxidative metabolism of a variety of xenobiotics such as drugs and pesticides. Form I catalyzes the N-oxygenation of secondary and tertiary amines.
Benzothiepins at the US National Library of Medicine Medical Subject Headings (MeSH). ...
BENZOTHIEPINS (75-85); RN given refers to parent cpd without isomeric designation ... minor descriptor (75-85); on-line & Index Medicus search DIBENZOTHIEPINS (69-74) & BENZOTHIEPINS (75-85); RN given refers to ...
Benzothiepins at the US National Library of Medicine Medical Subject Headings (MeSH). ...
4-Phenyl-2,3,4,5-tetrahydro-1-benzothiepins and some related compounds. 1972, Vol. 37, Issue 11, pp. 3808-3816 [Abstract] ...
4-Phenyl-2,3,4,5-tetrahydro-1-benzothiepins and some related compounds. 1972, Vol. 37, Issue 11, pp. 3808-3816 [Abstract] ...
Benzothiepins (0) * beta-Lactams (0) * Cyclic S-Oxides (0) * Isothiocyanates (0) * Organothiophosphorus Compounds (0) ...
Bohula EA, Scirica BM, Inzucchi SE, McGuire DK, Keech AC, Smith SR, Kanevsky E, Murphy SA, Leiter LA, Dwyer JP, Corbalan R, Hamm C, Kaplan L, Nicolau JC, Ophuis TO, Ray KK, Ruda M, Spinar J, Patel T, Miao W, Perdomo C, Francis B, Dhadda S, Bonaca MP, Ruff CT, Sabatine MS, Wiviott SD. Effect of lorcaserin on prevention and remission of type 2 diabetes in overweight and obese patients (CAMELLIA-TIMI 61): a randomised, placebo-controlled trial. Lancet. 2018 11 24; 392(10161):2269-2279 ...
Biddlestone-Thorpe L, Sajjad M, Rosenberg E, Beckta JM, Valerie NC, Tokarz M, Adams BR, Wagner AF, Khalil A, Gilfor D, Golding SE, Deb S, Temesi DG, Lau A, OConnor MJ, Choe KS, Parada LF, Lim SK, Mukhopadhyay ND, Valerie K. ATM kinase inhibition preferentially sensitizes p53-mutant glioma to ionizing radiation. Clin Cancer Res. 2013 Jun 15; 19(12):3189-200 ...
Staszewski S, Morales-Ramirez J, Tashima KT, Rachlis A, Skiest D, Stanford J, Stryker R, Johnson P, Labriola DF, Farina D, Manion DJ, Ruiz NM. Efavirenz plus zidovudine and lamivudine, efavirenz plus indinavir, and indinavir plus zidovudine and lamivudine in the treatment of HIV-1 infection in adults. Study 006 Team. N Engl J Med. 1999 Dec 16; 341(25):1865-73 ...
Benzothiepins D3.438.197 D3.633.100.197 Benzoxazines D3.438.209 D3.633.100.209 Benzoxazoles D3.438.221 D3.633.100.221 ...
Comparative Study 2009; 30(Suppl 1): 133-136 PubMed PMID: 20027159 Keywords: Benzothiepins:pharmacology, Brompheniramine: ...
Comparative Study 2009; 30(Suppl 1): 133-136 PubMed PMID: 20027159 Keywords: Benzothiepins:pharmacology, Brompheniramine: ...
This is a multicentre, extension study of LUM001 in children diagnosed with Alagille Syndrome who have completed participation in a core LUM001 treatment
Townsend EC, Murakami MA, Christodoulou A, Christie AL, Köster J, DeSouza TA, Morgan EA, Kallgren SP, Liu H, Wu SC, Plana O, Montero J, Stevenson KE, Rao P, Vadhi R, Andreeff M, Armand P, Ballen KK, Barzaghi-Rinaudo P, Cahill S, Clark RA, Cooke VG, Davids MS, DeAngelo DJ, Dorfman DM, Eaton H, Ebert BL, Etchin J, Firestone B, Fisher DC, Freedman AS, Galinsky IA, Gao H, Garcia JS, Garnache-Ottou F, Graubert TA, Gutierrez A, Halilovic E, Harris MH, Herbert ZT, Horwitz SM, Inghirami G, Intlekoffer AM, Ito M, Izraeli S, Jacobsen ED, Jacobson CA, Jeay S, Jeremias I, Kelliher MA, Koch R, Konopleva M, Kopp N, Kornblau SM, Kung AL, Kupper TS, LaBoeuf N, LaCasce AS, Lees E, Li LS, Look AT, Murakami M, Muschen M, Neuberg D, Ng SY, Odejide OO, Orkin SH, Paquette RR, Place AE, Roderick JE, Ryan JA, Sallan SE, Shoji B, Silverman LB, Soiffer RJ, Steensma DP, Stegmaier K, Stone RM, Tamburini J, Thorner AR, van Hummelen P, Wadleigh M, Wiesmann M, Weng AP, Wuerthner JU, Williams DA, Wollison BM, Lane AA, Letai ...
Benzothiepins *Benzoxazine *Benzoxazoles *Benzoxepins *Benzoyl *Benzoyl chloride *Benzoyl hydrate *Benzoyl peroxide *Benzoyl ...

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