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6,5-BICYCLIC OCTAHYDROPYRROLOPYRIDINE OREXIN RECEPTOR ANTAGONISTS

The present invention is directed to 6,5-bicyclic octahydropyrrolopyridine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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OXAZOLE OREXIN RECEPTOR ANTAGONISTS

The present invention is directed to oxazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the oxazole compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Electric Literature of 822-82-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.822-82-2, Name is Isothiazole-4-carboxylic acid, molecular formula is C4H3NO2S. In a Patent£¬once mentioned of 822-82-2

HETERO-1,5,6,7-TETRAHYDRO-4H-INDOL-4-ONES

Compounds of formula (I) as described herein, processes for their production and their use as pharmaceuticals.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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RESORCINOL N-ARYL AMIDE COMPOUNDS, FOR USE AS PYRUVATE DEHYDROGENASE KINASE INHIBITORS

A compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: Y is ?CONR1- or optionally substituted arylene or optionally substituted heteroarylene; R1 is H, Cl, F, CH3 or CF3; 10 each R4 is independently H, CH3 or F; R5 is H or CH3; and each R2 and R6 is independently (Alk)n-Rn-(Alk)n-Rn-(Alk)n-X; The compounds of the invention are useful as resorcinol N-aryl amide (NAA) compounds, which are suitable for use as PDK inhibitors, for example for 15 inhibition of cancer cell proliferation.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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TRIAZOLE BETA CARBOLINE DERIVATIVES AS ANTIDIABETIC COMPOUNDS

Beta-carboline derivatives of structural formula (I) are selective antagonists of the somatostatin subtype receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Electric Literature of 822-82-2, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 822-82-2, molcular formula is C4H3NO2S, introducing its new discovery.

Substituted phenyl compounds

STR1Compounds of formula (I) are described wherein R 1 is hydrogen, -(lower alkyl) q (CO 2 R 6 or OH), –CN, –C(R 7) NOR 8, NO 2, –O(lower alkyl)R 9, –C C–R 10, –CR 11 C(R 12)(R 13), –C( O)CH 2 C( O)CO 2 H, –CO(R 14), alkylthio, alkylsulphinyl, alkylsulphonyl, carbamoyl, thiocarbamoyl, substituted carbamoyl, substituted thiocarbamoyl, sulphamoyl or an optionally substituted nitrogen-containing ring, m, n, o and p are independently zero or 1 and R 2, R 3, R 4 and R 5 are various groups; and physiologically acceptable salts, N-oxides and prodrugs thereof. The compounds have endothelin antagonist activity and are useful as pharmaceuticals.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Substituted Indoles

The invention provides for compounds of formula (I) wherein R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by SUV420H1. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 822-82-2, molcular formula is C4H3NO2S, introducing its new discovery. 822-82-2

Substituted Indoles

The invention provides for compounds of formula (I) wherein R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by SUV420H1. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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BENZAZEPIN-2(1H)-ONE DERIVATIVES

Compounds of formula (I) and pharmaceutically acceptable salts thereof are agonists at the beta-2 adrenoceptor. They are useful as feed additives for livestock animals.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

Application of (S)-(1-Ethylpyrrolidin-2-yl)methanamine

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It is a common heterocyclic compound, the isothiazole compound, Isothiazole-4-carboxylic acid, cas is 822-82-2 its synthesis route is as follows.

Intermediate G Step 1 : 5-Bromo-isothiazole-4-carboxylic acid (Gl) To a solution of isothiazole-4-carboxylic acid (1.70 g, 12.98 mmol) in THF (17 ml) was added i-BuLi (29.95 mL) at -78 C, and then a solution of CBr4 (8.62 g, 25.96 mmol) in THF (10 ml) was added dropwise. The mixture was stirred at -78 C for 2 h, quenched with addition of saturated aqueous NH4C1 solution and extracted with EtOAc (50 mL x 3). The aqueous layer was adjusted to ~pH =1.5 by addition of HC1 and extracted with EtOAc (50 mL x 3). The combined organic layers were dried over MgS04, filtered, and concentrated in vacuo to provide the title compound, which was used without further purification.

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Reference£º
Patent; MERCK SHARP & DOHME CORP.; KIM, Ronald; KUDUK, Scott, D.; LIVERTON, Nigel; ZHUO, Gang; (116 pag.)WO2016/100161; (2016); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com