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Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Quality Control of Isothiazole-4-carboxylic acid, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 822-82-2, in my other articles.

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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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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

 

Discovery of Isothiazole-4-carboxylic acid

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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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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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SUBSTITUTED DIHYDROTHIENOPYRIMIDINES AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS

The present invention relates to novel substituted dihydrothienopyrimidines with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions.

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

 

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ETHYLDIAMINE OREXIN RECEPTOR ANTAGONISTS

The present invention is directed to ethyldiamne 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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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Synthesis, Identification, and Structure-Activity Relationship Analysis of GATA4 and NKX2-5 Protein-Protein Interaction Modulators

Transcription factors GATA4 and NKX2-5 directly interact and synergistically activate several cardiac genes and stretch-induced cardiomyocyte hypertrophy. Previously, we identified phenylisoxazole carboxamide 1 as a hit compound, which inhibited the GATA4-NKX2-5 transcriptional synergy. Here, the chemical space around the molecular structure of 1 was explored by synthesizing and characterizing 220 derivatives and structurally related compounds. In addition to the synergistic transcriptional activation, selected compounds were evaluated for their effects on transcriptional activities of GATA4 and NKX2-5 individually as well as potential cytotoxicity. The structure-activity relationship (SAR) analysis revealed that the aromatic isoxazole substituent in the southern part regulates the inhibition of GATA4-NKX2-5 transcriptional synergy. Moreover, inhibition of GATA4 transcriptional activity correlated with the reduced cell viability. In summary, comprehensive SAR analysis accompanied by data analysis successfully identified potent and selective inhibitors of GATA4-NKX2-5 transcriptional synergy and revealed structural features important for it.

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

 

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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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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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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Agonist lead identification for the high affinity niacin receptor GPR109a

A strategy for lead identification of new agonists of GPR109a, starting from known compounds shown to activate the receptor, is described. Early compound triage led to the formulation of a binding hypothesis and eventually to our focus on a series of pyrazole acid derivatives. Further elaboration of these compounds provided a series of 5,5-fused pyrazoles to be used as lead compounds for further optimization.

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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