287193-07-1Relevant academic research and scientific papers
C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators
Du, Xiaohui,Hinklin, Ronald J.,Xiong, Yumei,Dransfield, Paul,Park, Jaehyeon,Kohn, Todd J.,Pattaropong, Vatee,Lai, Sujen,Fu, Zice,Jiao, Xianyun,Chow, David,Jin, Lixia,Davda, Jasmine,Veniant, Murielle M.,Anderson, Deborah A.,Baer, Brian R.,Bencsik, Josef R.,Boyd, Steven A.,Chicarelli, Mark Joseph,Mohr, Peter J.,Wang, Bin,Condroski, Kevin R.,Dewolf, Walter E.,Conn, Marion,Tran, Thanhvien,Yang, Jerry,Aicher, Thomas D.,Medina, Julio C.,Coward, Peter,Houze, Jonathan B.
supporting information, p. 1284 - 1289 (2015/02/02)
Glucokinase (GK) activators represent a class of type 2 diabetes therapeutics actively pursued due to the central role that GK plays in regulating glucose homeostasis. Herein we report a novel C5-alkyl-2-methylurea-substituted pyridine series of GK activators derived from our previously reported thiazolylamino pyridine series. Our efforts in optimizing potency, enzyme kinetic properties, and metabolic stability led to the identification of compound 26 (AM-9514). This analogue showed a favorable combination of in vitro potency, enzyme kinetic properties, acceptable pharmacokinetic profiles in preclinical species, and robust efficacy in a rodent PD model.
IRAK INHIBITORS AND USES THEREOF
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Paragraph 001250, (2013/07/25)
The present invention provides thieno[2,3-d]pyrimidine derivative compounds, and pharmaceutical compositions thereof. The invention also includes methods inhibiting an IRAK protein kinase in a patient by administering the thieno[2,3-d]pyrimidine derivative compound. The invention also includes methods of treating an IRAK-mediated disorder, disease, or condition in a patient by administering the thieno[2,3-d]pyrimidine derivative compound.
SERINE/THREONINE KINASE INHIBITORS
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Paragraph 00288, (2013/09/12)
Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
Modulators of Protein Tyrosine Phosphatases (PTPases)
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Page/Page column 72, (2010/10/20)
Disclosed are novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds of Formula 1 are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPases) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like, wherein n, m, X, Y, R1, R2, R3, R4, R5 and R6 are defined more fully in the description. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, and other diseases.
Method of inhibiting protein tyrosine phosphatase 1B and/or T-cell protein tyrosine phosphatase 4 and/or other PTPases with an Asp residue at position 48
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Page/Page column 85-87, (2010/11/23)
The present invention provides a method of inhibiting a member of a family of Protein Tyrosine Phosphatases (PTPases, PTPs) such as PTP1B, TC-PTP, CD45, SHP-1, SHP-2, PTPα, PTPε, PTPμ, PTPδ, PTPσ, PTPζ, PTPβ, PTPD1, PTPD2, PTPH1, PTP-MEG1, PTP-LAR, and HePTP by exposing said Ptpase member by administration to a host or otherwise to at least one compound with certain structural, physical and spatial characteristics that allow for the interaction of said compound with specific residues of the active site of PTP1B and/or TC-PTP. These compounds are indicated in the management or treatment of a broad range of diseases such as autoimmune diseases, acute and chronic inflammation, osteoporosis, various forms of cancer and malignant diseases, and type I diabetes and type II diabetes, as well as in the isolation of PTPases and in elucidation or further elucidation of their biological function.
MODULATORS OF PROTEIN TYROSINE PHOSPHATASES (PTPases)
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Page/Page column 49-50, (2010/02/14)
Disclosed are novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds of Formula 1 are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPases) such as PTP1B, CD45, SHP-1, SHP-2, PTPalpha, LAR and HePTP or the like, wherein n, m, X, Y, R1, R2, R3, R4, R5 and R6 are defined more fully in the description. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, and other diseases.
Substituted bicyclic derivatives useful as anticancer agents
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, (2008/06/13)
The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein A, X, R1, R3and R4are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals with administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.
