专利号:WO-03031376-A1 优先权日:2001-10-12 标 题 :Solid phase synthesis of substituted 1,5-benzodiazepine-2-one and 1,5-benzothiazepine-2-one 发明人:MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 权利人:AVENTIS PHARMA INC; MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 摘要:A solid phase synthetic method for making substituted 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one. The method is useful for synthesis of large numbers of compounds through automated parallel synthesis or combinatorial library generation and is thus important to rapid discovery or new therapeutic agents containing the base structure of 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one.
专利号:US-12240835-B2 优先权日:2018-09-18 标题:Substituted benzamides as intermediates in the synthesis of inhibitors of tyrosine kinase enzymatic activity 发明人:ROMERO F ANTHONY; KIRSCHBERG THORSTEN A; HALCOMB RANDALL; XU YINGZI 权利人:TERNS PHARMACEUTICALS INC 摘要:Provided herein are compounds, preferably compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, compositions thereof, and methods of their preparation, and methods of inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, and methods for treating diseases wherein modulation of BCR-ABL1 activity prevents, inhibits, or ameliorates the pathology and/or symptomology of the disease. Intermediates such as compounds of Formula (S23), which are useful in the synthesis of compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, are also provided.
专利号:US-2005100968-A1 优先权日:2000-02-23 标题 :Self-encoded combinatorial synthesis of compound multiplets 发明人:GALLOP MARK A; DOWER WILLIAM J; BARRETT RON W 权利人:XENOPORT INC 摘要:The present invention provides a variety of methods for synthesizing, encoding and decoding compounds in a combinatorial library. One step or cycle in the synthetic methods of the invention is a self-encoding step in which different pairs of components, each pair with a known and different molecular weight difference, are reacted with supports, whereby two compounds differing in molecular weight are formed on each support. The molecular weight difference between the two compounds on the support encodes for a particular component pair. Libraries of compounds formed according to the methods of the invention are also provided.
专利号:US-2006122240-A1 优先权日:2002-11-05 标题 :Benzotriazoles and methods of prophylaxis or treatment of metabolic-related disorders thereof 发明人:SEMPLE GRAEME; SKINNER PHILIP J; CHERRIER MARTIN C; WEBB PETER; TAMURA SUSAN Y 权利人:ARENA PHARM INC 摘要:The present invention relates to certain benzotriazole carboxylic acid or ester derivatives of Formula (I), pharmaceutically acceptable salts and solvates thereof, which exhibit useful pharmaceutical properties, for example, as agonists for the GPCR referred to as hRUP38. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the prophylaxis or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of -glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.
专利号:US-10112955-B2 优先权日:2015-10-29 标题 :Isoindoline, azaisoindoline, dihydroindenone and dihydroazaindenone inhibitors of Mnk1 and Mnk2 发明人:SPRENGELER PAUL A; REICH SIEGFRIED H; ERNST JUSTIN T; WEBBER STEPHEN E; SHAGHAFI MIKE; MURPHY DOUGLAS; TRAN CHINH 权利人:EFFECTOR THERAPEUTICS INC 摘要:The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. n nFor Formula I compounds A 1 , A 2 , A 3 , A 4 , A 5 , W 1 , Y, R 1 , R 2 , R 3 , R 4 , R 5 , R 6a , R 6b , R 7 , R 8 , R 8a , R 8b , R 9 , R 9a , R 9b , and R 10 and subscript “nâ€? are as defined in the specification. The inventive Formula I compounds are inhibitors of Mnk and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
专利号:US-9217012-B2 优先权日:2009-04-08 标题 :Inhibitors of protein tyrosine phosphatases 发明人:ZHANG ZHONG-YIN; ZHANG SHENG 权利人:ZHANG ZHONG-YIN; ZHANG SHENG; UNIV INDIANA RES & TECH CORP 摘要:Disclosed herein are compounds that selectively inhibit members of the PTP family of enzymes. Synthesized compounds demonstrated selective inhibition of TC-PTP. Also provided are methods of using the compounds and formulations containing the compounds. Also described is a fluorescence-tagged combinatorial library synthesis and screening method. And methods of using these compounds to effect enzyme activity both in cells and in vitro as well as method of using these compounds to treat diseases in human and animals.
[参考文献]: Chih-Hau Chen, Et Al. Regioselective, Unconventional Pictet-Spengler Cyclization Strategy Toward The Synthesis Of Benzimidazole-Linked Imidazoquinoxalines On A Soluble Polymer Support. Chem Asian J. 2011 Jun 6;6(6):1557-65. [参考文献]: D L Ladd, Et Al. Reagents For The Preparation Of Chromophorically Labeled Polyethylene Glycol-Protein Conjugates. Anal Biochem. 1993 May 1;210(2):258-61. [参考文献]: Gérard Klein, Et Al. Parallel Solid-Phase Synthesis Of Trisubstituted Triazinobenzimidazolediones. J Comb Chem. 2002 Jul-Aug;4(4):345-51. [参考文献]: J C Wijkmans, Et Al. Solid Phase Synthesis Of Functionalized Biaryl Ethers: Versatile Scaffolds For Combinatorial Chemistry. Mol Divers. 1997;3(2):117-20. [参考文献]: Wen-Bing Yeh, Et Al. Combinatorial Synthesis Of Biheterocyclic Benzimidazoles By Microwave Irradiation. Comb Chem High Throughput Screen. 2004 May;7(3):251-5.