- BICYCLIC HETEROCYCLES AS FGFR INHIBITORS
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The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR enzyme and are useful in the treatment of FGFR-associated diseases such as cancer. Formula (I)
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Page/Page column 131
(2021/04/23)
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- AZAINDOLE INHIBITORS OF WILD-TYPE AND MUTANT FORMS OF LRRK2
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Disclosed are compounds that possess inhibitory activity against LRRK2. Also disclosed are pharmaceutical compositions containing the compounds and methods of using the compounds to treat diseases and disorders including neurodegenerative diseases and dis
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Paragraph 0192; 0191
(2020/05/21)
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- QUINAZOLINONES AS PARP14 INHIBITORS
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The present invention relates to quinazolinones and related compounds which are inhibitors of PARP14 and are useful, for example, in the treatment of cancer and inflammatory diseases.
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Paragraph 0298; 0838; 0840
(2019/07/10)
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- 5-HETEROARYL SUBSTITUTED INDAZOLE-3-CARBOXAMIDES AND PREPARATION AND USE THEREOF
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Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., tendinopathy, dermatitis, psoriasis, morphea, ichthyosis, Raynaud's syndrome, Darier's disease, scleroderma, cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as neurological conditions/disorders/diseases linked to overexpression of DYRK1A.
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Paragraph 0715; 0716
(2019/09/06)
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- N-ACYLPIPERIDINE ETHER TROPOMYOSIN-RELATED KINASE INHIBITORS
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The present invention relates to compounds of Formula (I) described herein and their pharmaceutically acceptable salts, and their use in medicine, in particular as Trk antagonists.
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Page/Page column 178
(2015/07/07)
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- TETRAHYDROQUINOLINE COMPOSITIONS AS BET BROMODOMAIN INHIBITORS
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The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula (I): wherein W, X, Y, Z, R1, R2, R5, and R8 are as described herein.
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Paragraph 0744
(2015/06/03)
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- COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF MEK
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The present invention relates to compounds of formula I: in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.
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- COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF MEK
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The present invention relates to compounds of formula I in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.
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- Tetraaza-cyclopenta[a]indenyl derivatives
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The present invention provides compounds of Formula (I) as M1 receptor positive allosteric modulators for the treatment of diseases mediated by the muscarinic M1 mediator.
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- Discovery of a novel class of imidazo[1,2-a ]pyridines with potent PDGFR activity and oral bioavailability
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The in silico construction of a PDGFRβ kinase homology model and ensuing medicinal chemistry guided by molecular modeling, led to the identification of potent, small molecule inhibitors of PDGFR. Subsequent exploration of structure-activity relationships
- Hicken, Erik J.,Marmsater, Fred P.,Munson, Mark C.,Schlachter, Stephen T.,Robinson, John E.,Allen, Shelley,Burgess, Laurence E.,Delisle, Robert Kirk,Rizzi, James P.,Topalov, George T.,Zhao, Qian,Hicks, Julie M.,Kallan, Nicholas C.,Tarlton, Eugene,Allen, Andrew,Callejo, Michele,Cox, April,Rana, Sumeet,Klopfenstein, Nathalie,Woessner, Richard,Lyssikatos, Joseph P.
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supporting information
p. 78 - 83
(2014/02/14)
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- TETRAAZA-CYCLOPENTA[A]INDENYL DERIVATIVES
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The present invention provides compounds of Formula (I) as M1 receptor positive allosteric modulators for the treatment of diseases mediated by the muscarinic M1 mediator.
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Page/Page column 121; 122
(2015/01/09)
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- PYRIMIDINE PYRAZOLYL DERIVATIVES
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The present invention provides compounds of Formula (I) for the treatment of cancer, rheumatoid arthritis and other diseases (I).
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Page/Page column 117; 118
(2014/02/15)
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- IMIDAZO[1,2-A]PYRIDINE COMPOUNDS AS RECEPTOR TYROSINE KINASE INHIBITORS
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Compounds of Formula I: in which A, B, R1, R1a, R2, R3, R4, R5 R6, R7 and R8 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by class 3 and class 5 receptor tyrosine kinases. Particular compounds of this invention have also been found to be inhibitors of Pim-1.
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