- (PYRIDIN-2-YL)AMINE DERIVATIVES AS TGF-BETA R1 (ALK5) INHIBITORS FOR THE TREATMENT OF CANCER
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The present invention relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder associated with ΤGFβR1 activity, such as a cancer or fibrosis. The invention provides compounds of Formula (I) and Formula (II) as further described herein having an acidic moiety that enhances tissue specificity for targeted tissues and organs. The invention includes pharmaceutical compositions, pharmaceutical combinations, and methods of use of these compounds for treating conditions including cancer or fibrosis.
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Paragraph 00357
(2020/07/15)
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- RORGAMMA MODULATORS AND USES THEREOF
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The present invention provides novel compounds of formula (la) that are modulators of RORgamma. These compounds, and pharmaceutical compositions comprising the same, are suitable means for treating any disease wherein the modulation of RORgamma has therapeutic effects, for instance in autoimmune diseases, autoimmune-related diseases, inflammatory diseases, metabolic diseases, fibrotic diseases, or cholestatic diseases. (formula Ia)
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Page/Page column 38
(2018/09/02)
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- RORGAMMA MODULATORS AND USES THEREOF
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The present invention provides novel compounds of formula (la) that are modulators of RORgamma. These compounds, and pharmaceutical compositions comprising the same, are suitable means for treating any disease wherein the modulation of RORgamma has therapeutic effects, for instance in autoimmune diseases, autoimmune-related diseases, inflammatory diseases, metabolic diseases, fibrotic diseases, or cholestatic diseases.
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Page/Page column 41; 42
(2018/08/20)
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- HETEROCYCLIC COMPOUNDS AND COMPOSITIONS AS C-KIT AND PDGFR KINASE INHIBITORS
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The invention provides a novel class of compounds of Formula I: (I) pharmaceutical compositions comprising such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFRα and PDGFRβ kinases.
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Page/Page column 37; 39
(2009/10/18)
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- COMPOSITIONS AND METHODS FOR MODULATING C-KIT AND PDGFR RECEPTORS
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The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit, PDGFR , PDGFR , CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGF , SRC, EGFR, trkB, FGFR3, FLT3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2 , BRK, KDR, c-raf or b-raf kinase, or mutant forms thereof.
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Page/Page column 33; 34
(2008/12/05)
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- COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
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The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, CSK, JNK1, JNK2, PDGF-R, p38, p70S6K, TGF beta , SRC, EGFR, c-Kit, trkB, FGFR3, Fes, Lck, Syk, RAF, MKK4, MKK6 and SAPK2 beta kinases.
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Page/Page column 42
(2008/06/13)
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- Leaving group effects in reductively triggered fragmentation of 4-nitrobenzyl carbamatesf
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The rates and extent of release of a series of substituted anilines from 4-nitrobenzyl carbamates, following nitro group reduction by radiolytic, enzymic and chemical methods, are reported. The yield of released anilines decreased over the pH range 4-7, b
- Sykes, Bridget M.,Hay, Michael P.,Bohinc-Herceg, Dubravka,Helsby, Nuala A.,O'Connor, Charmian J.,Denny, William A.
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p. 1601 - 1608
(2007/10/03)
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