- Discovery of a potent G-protein-coupled receptor 119 agonist for the treatment of type 2 diabetes
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The ever-growing prevalence of Type-2 diabetes in the world has an urgent need for multiple orally effective agents that can regulate glucose homeostasis. G-Protein coupled receptor 119 (GPR 119) agonists have demonstrated the glucose-dependent insulin secretion and showed beneficial effects on glycemic control in humans and/or relevant animal models. Herein, we describe our efforts towards identification of a potent and oral GPR 119 agonist 13c (ZY-G19), which showed in vitro potency in the cell-based assay and in vivo efficacy without exerting any significant signs of toxicity in relevant animal models.
- Pola, Suresh,Shah, Shailesh R.,Pingali, Harikishore,Zaware, Pandurang,Thube, Baban,Makadia, Pankaj,Patel, Hoshang,Bandyopadhyay, Debdutta,Rath, Akshyaya,Giri, Suresh,Patel, Jitendra H.,Ranvir,Sundar,Patel, Harilal,Kumar, Jeevan,Jain, Mukul R.
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- TETRAHYDROISOQUINOLINE DERIVED PRMT5-INHIBITORS
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A compound of formula I wherein: n is 1 or 2: p is 0 or 1; R1 is optionally one or more halo or methyl groups; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R3a and R3b are independently selected from H and Me; R4 is either H or Me; R5 is either H or Me; R6a and R6b are independently selected from H and Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C5-12 heteroaryl.
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Page/Page column 105-106
(2016/03/19)
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- INDOLYLPYRIMIDINES AS MODULATORS OF GPR119
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The present invention relates to compounds of Formula (I) that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions modulated by GPR119 receptor activity. The invention also relates to the process for preparation of the compounds, pharmaceutical compositions thereof. The invention further relates to methods of treating, preventing and/or managing diseases, disorders syndromes or conditions associated with the modulation of GPR119 receptor by using either alone or in combinations of Formula (I).
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Page/Page column 30
(2012/03/26)
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- 2, 7 -NAPHTHYRIDIN- 1 -ONE DERIVATIVES AS SYK KINASE INHIBITORS
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Provided herein area 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 Syk kinase activity.
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Page/Page column 118
(2011/02/24)
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- PYRIMIDYL INDOLINE COMPOUND
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It is intended to provide a pyrimidyl indoline compound which structurally differs from compounds used as active ingredients in conventional oral hypoglycemic agents and has excellent hypoglycemic effect. The present invention provides a compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof:
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Page/Page column 48
(2010/08/07)
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- BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF
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The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a c
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Page/Page column 36, 37
(2010/07/09)
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- NEW COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS RELATING THERETO
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New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein X1, X2, X3, X4, Y1
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Page/Page column 34; 35
(2011/01/12)
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- SUBSTITUTED ARYL AND HETEROARYL DERIVATIVES AS MODULATORS OF METABOLISM AND THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO
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The present invention relates to certain substituted aryl and heteroaryl derivative of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and complicati
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Page/Page column 148
(2008/06/13)
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- Peptide compounds
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The present invention relates to a compound of the formula (I)wherein R1 is benzofuranyl substituted by halogen, or styryl substituted by halogen; R2 is substituted hydroxy, substituted mercapto or substituted sulfonyl; and X is or pharmaceutically acceptable salts thereof. The compound (1) of the present invention and pharmaceutically acceptable salts thereof possess a strong inhibitory activity on the production of nitric oxide (NO), and are useful for prevention and/or treatment of NO-mediated diseases in human being and animals.
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