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NADPH OXIDASE 4 INHIBITORS

The invention relates to 2,5-disubstituted benzoxazole and benzothiazole derivatives of Formula (I) Formula (I) wherein L, X, Y, and ring (A) are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds may be useful for the prevention or treatment of diseases or disorders associated with impaired reactive oxygen species (ROS) production, and/or for the prevention or treatment of various fibrotic diseases.

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A thiophene and pyrimidine derivatives, its preparation process and its use in medicine (by machine translation)

The invention discloses a thiophene and pyrimidine derivatives, its preparation process and its application in medicine. Said derivatives are having the general formula I or formula II or the compounds of the general formula III: In the above-mentioned formula: Ar is phenyl, halogen substituted phenyl, C 1-6 alkyl substituted phenyl, biphenyl, halogen-substituted biphenyl, naphthyl, pyridyl, thienyl, halogen-substituted thienyl, C 1-3 alkyl substituted thienyl, furanyl, halogen substituted furyl, C 1-3 alkyl substituted furyl in any one of; A, D, respectively E is carbon atom or a nitrogen atom, but A, D, different E is carbon atom; for R R 1-NH-, The present invention provides thieno miazines has obvious and inhibit EGFR inhibitory activity of A431 cell activity, is expected to develop for the tyrosine kinase inhibitor, it has broad application prospects and medicinal value. (by machine translation)

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MODULATORS FOR AMYLOID BETA

The invention relates to compounds of formula wherein the substituents are as described in claim 1. Compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of beta-amyloid in the brain, in particular Alzheimer”s disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.

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Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice

A series of trisubstituted hydroxylactams was identified as potent enzymatic and cellular inhibitors of human lactate dehydrogenase A. Utilizing structure-based design and physical property optimization, multiple inhibitors were discovered with <10 muM lactate IC50 in a MiaPaca2 cell line. Optimization of the series led to 29, a potent cell active molecule (MiaPaca2 IC50 = 0.67 muM) that also possessed good exposure when dosed orally to mice. One of the oldest and most widely used commercial enzyme inhibitors is aspirin, SDS of cas: 39093-93-1, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 39093-93-1

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DIAZACARBAZOLES AND METHODS OF USE

The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chkl) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

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PYRROLIDINE DERIVATIVES AS DUAL NK1/NK3 RECEPTOR ANTAGONISTS

The invention relates to pyrrolidine derivatives of formulawherein R1,R2,R3,n, and o are defined in the specification and to pharmaceutically active acid-addition salts thereof. Compounds of formula I have a high affinity simultaneously to both the NK1 and the NK3 receptors (dual NK1/NK3 receptor antagonists), useful in the treatment of schizophrenia.

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AZAINDAZOLE COMPOUNDS AS INHIBITORS OF T790M CONTAINING EGFR MUTANTS

This invention relates to novel compounds of formula (I), which are inhibitors of T790M containing EGFR mutants, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of cancer.

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N-SULFONYLATED PYRAZOLO[3,4-B]PYRIDIN-6-CARBOXAMIDES AND METHOD OF USE

The present 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 CFTR, including cystic fibrosis, Sjoegren’s syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

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Synthesis of N-methyl-6-heterocyclic-1-oxoisoindoline derivatives by microwave assisted buchwald-hartwig amination

An rapid and efficient microwave assisted Pd(II) catalyzed protocol for the preparation of N-methyl-6-heterocyclic-1-oxoisoindoline derivatives by Buchwald-Hartwig amination with an overall yield 68-85% has been described.

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beta-N-Biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors: Part 2. Optimization of alpha-amino substituents

The introduction and the optimization of an alpha-amino substituent based on a series of alpha-hydroxy-beta-N-biaryl ether sulfonamide hydroxamates is described. The modification leads to a new series of MMP-2/MMP-9 inhibitors with enhanced inhibitory activities and improved ADME properties. An efficacy study on reducing the ischemia-induced brain edema in the rat transient middle cerebral artery occlusion (tMCAo) model is also demonstrated.

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