- FUSED PYRIMIDINE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF FIBROTIC DISEASES
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The present invention discloses compounds according to Formula I: Wherein A, B, R1, R2, and Cy are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, pain, and/or abnormal angiogenesis associated diseases by administering the compounds of the invention.
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Paragraph 0380-0381
(2021/02/25)
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- THIAZOLIDINONE COMPOUNDS AND USE THEREOF
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A pharmaceutical composition containing a compound of Formula (I) for treating an opioid receptor-associated condition. Also disclosed is a method for treating an opioid receptor-associated condition using such a compound. Further disclosed are two sets of thiazolidinone compounds of formula (I): (i) compounds each having an enantiomeric excess greater than 90% and (ii) compounds each being substituted with deuterium.
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Paragraph 0175-0176
(2017/09/21)
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- PYRAZOLE COMPOUNDS AS CRTH2 ANTAGONISTS
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The present invention relates to pyrazole compounds of formula (I) and pharmaceutically acceptable salts thereof having CRTH2-activity, wherein W, L1, L2, X, L3, Y, R1 and R2 are as defined in the spe
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Page/Page column 44
(2012/02/06)
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- Insecticidal 4-phenyl-1H-pyrazoles
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The present invention relates to novel 4-phenyl-1H-pyrazoles and their use as insecticides and/or parasiticides and also to processes for their preparation and to compositions comprising such phenylpyrazoles.
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Page/Page column 28
(2011/08/08)
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- PYRAZOLE COMPOUNDS AS CRTH2 ANTAGONISTS
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The present invention relates to pyrazole compounds of formula (I) and pharmaceutically acceptable salts thereof having CRTH2-activity, wherein W, L1, L2, X, L3, Y, R1 and R2 are as defined in the spe
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Page/Page column 76
(2011/08/21)
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- INDOLE DERIVATIVES USEFUL AS PPAR ACTIVATORS
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There is provided according to the invention novel compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof: (I) useful as PPAR activators.
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Page/Page column 29
(2009/05/30)
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- Rational design of the first small-molecule antagonists of NHERF1/EBP50 PDZ domains
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This report describes the first small-molecule antagonists that specifically target the ligand-binding pocket of PDZ domains of NHERF1 multi-functional adaptor protein. Comparison of the peptide sequence homology between the native ligand of NHERF1 PDZ do
- Mayasundari, Anand,Ferreira, Antonio M.,He, Liwen,Mahindroo, Neeraj,Bashford, Don,Fujii, Naoaki
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p. 942 - 945
(2008/09/18)
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- Indole-2-amide based biochemical antagonist of Dishevelled PDZ domain interaction down-regulates Dishevelled-driven Tcf transcriptional activity
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We designed and synthesized a series of indole-2-amide-based compounds that antagonize interaction between the Dishevelled (Dvl) PDZ domain and a peptide derived from the natural PDZ ligand Frizzled-7 (Fz7). These compounds inhibit Tcf-mediated transcript
- Mahindroo, Neeraj,Punchihewa, Chandanamali,Bail, Allison M.,Fujii, Naoaki
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p. 946 - 949
(2008/09/20)
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- BICYCLIC COMPOUNDS USEFUL AS CATHEPSIN S INBHIBITORS
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Compounds of formula (I), wherein R1, R2, R3, Ra and E are are defined within, and pharmaceutically acceptable salts, solvates, hydrates and N-oxides thereof having utility in the treatment of disorders mediated by cathepsin S.
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Page/Page column 46
(2010/11/29)
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- SMALL MOLECULE INHIBITION OF A PDZ-DOMAIN INTERACTION
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Novel compounds that have been found effective in inhibiting PDZ domain interactions, and particularly interactions of PDZ domains in MAGIs with the oncogenic (tumor suppressor) protein PTEN and interactions between the PDZ domain in the Dishevelled (Dvl)
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Page/Page column 24
(2008/06/13)
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- CATHEPSIN S INHIBITORS
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Compounds of the formula (I) where R1 is C1-C4 straight or branched alkyl, optionally substituted with up to three substituents selected from halo and hydroxy; R2 is halo, hydroxy, methyloxy, or C1-C2 alkyl, which alkyl is optionally substituted with up to three halogens or an hydroxy or a methyloxy; D is - C3-C7 alkylene-, thereby defining a cycloalkyl ring; E is -C(=O)-, -S(=O)m-, -NRdS(=O)m-, -NRaC(=O)-, -OC(=O)-, R3 is an optionally substituted carbocyclic or heterocyclic ring R10 is H, ORc, SRc or together with the gem H is =O or (ORc)2; Ra is independently selected from H, C1-C4 alkyl; have utility in the inhibition of cathepsin S and are thus useful pharmaceuticals against disorders such as autoimmune disorders and chronic pain.
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Page/Page column 117
(2010/11/08)
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- NOVEL ANTITHROMBOTIC SUBSTITUTED PYRROLIDINONES, THE PRODUCTION AND USE THEREOF IN THE FORM OF MEDICAMENTS
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The invention relates to novel substituted pyrrolidines of general formula (I), wherein A, X, B and R1 to R9 are such as defined in the claim 1, and to the tautomers, enantiomers, diastereomers, mixtures and the salts thereof, in par
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Page/Page column 99
(2008/06/13)
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- SUBSTITUTED THIOPHEN-CARBOXYLIC ACID AMIDES, THE PRODUCTION AND THE USE THEREOF IN THE FORM OF A DRUG
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The invention relates to novel substituted thiophen-2-carboxylic acid amides of general formula (I), wherein A and R1 to R8 are defined as specified in the claim 1, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, in particular the salts thereof which are physiologically compatible with inorganic or organic acids or bases and exhibit interesting properties.
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Page/Page column 156-157
(2010/02/14)
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