专利号:US-7626045-B2 优先权日:2005-01-14 标题:Synthesis of himbacine analogs 发明人:THIRUVENGADAM TIRUVETTIPURAM K; WANG TAO; LIAO JING; CHIU JOHN S; TSAI DAVID J S; LEE HONG-CHANG; WU WENXUE; FU XIAOYONG 权利人:SCHERING CORP 摘要:The present invention relates to an improved process for preparing himbacine analogs. The compounds are useful as thrombin receptor antagonists. The improved process may allow for at least one of easier purification by crystallization, easier scalability, and improved process yield on the desired enantiomer. n An example of a step in the synthesis of such a himbacine analog is as follows:
专利号:EP-1853592-B1 优先权日:2005-01-14 标题:Synthesis of himbacine analogs 发明人:THIRUVENGADAM TIRUVETTIPURAM K; WANG TAO; LIAO JING; CHIU JOHN S; TSAI DAVID J S; LEE HONG-CHANG; WU WENXUE; FU XIAOYONG 权利人:SCHERING CORP 摘要:The present invention relates to an improved process for preparing imbacine analogs. The compounds are useful as thrombin receptor antagonists. The improved process may allow for at least one of easier purification by crystallization, easier scalability, and improved process yield on the desired enantiomer. An example of a step in the synthesis of such a himbacine analog is as follows: Formula (I)
专利号:US-8188113-B2 优先权日:2006-09-14 标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases 发明人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C 权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC 摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.
专利号:US-8329905-B2 优先权日:2006-06-30 标 题 :Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate 发明人:YONG KELVIN H; ZAVIALOV ILIA A; YIN JIANGUO; FU XIAOYONG; THIRUVENGADAM THIRUVETTIPURAM K 权利人:YONG KELVIN H; ZAVIALOV ILIA A; YIN JIANGUO; FU XIAOYONG; THIRUVENGADAM THIRUVETTIPURAM K; MERCK SHARP & DOHME 摘要:This application discloses a novel process for the preparation of phosphonate esters useful as intermediates in the preparation of himbacine analogs, themselves useful as thrombin receptor antagonists. The chemistry taught herein can be exemplified by the following scheme: n nwherein R 9 is selected from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms, and R 11 is selected independently for each occurrence from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms and hydrogen, X 2 is Cl, Br, or I; X 3 is selected from Cl and Br; and PdL n is a supported palladium metal catalyst or a soluble heterogeneous palladium catalyst. The L-derivatizing reagent is a moiety which converts the alcohol functional group of compound 137D to any leaving group which can be displaced by a triorgano-phosphite phosphonating agent.
专利号:US-8618314-B2 优先权日:2005-01-14 标 题 :Exo- and diastereo-selective synthesis of himbacine analogs 发明人:WU GEORGE G; SUDHAKAR ANANTHA; WANG TAO; XIE JI; CHEN FRANK X; POIRIER MARC; HUANG MINGSHENG; SABESAN VIJAY; KWOK DAW-LONG; CUI JIAN; YANG XIAOJING; THIRUVENGADAM TIRUVETTIPURAM K; LIAO JING; ZAVIALOV ILIA; NGUYEN HOA N; LIM NGIAP KIE 权利人:WU GEORGE G; SUDHAKAR ANANTHA; WANG TAO; XIE JI; CHEN FRANK X; POIRIER MARC; HUANG MINGSHENG; SABESAN VIJAY; KWOK DAW-LONG; CUI JIAN; YANG XIAOJING; THIRUVENGADAM TIRUVETTIPURAM K; LIAO JING; ZAVIALOV ILIA; NGUYEN HOA N; LIM NGIAP KIE; MERCK SHARP & DOHME 摘要:This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following:
专利号:US-9732097-B2 优先权日:2015-05-11 标 题:Process for the synthesis of a phosphoinositide 3-kinase inhibitor 发明人:ZHOU JIACHENG; QIAO LEI; WENG LINGKAI 权利人:INCYTE CORP 摘要:The present application is directed to processes and intermediates for making (S)-7-(1-((9H-purin-6-yl)amino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one, which is an inhibitor of phosphoinositide 3-kinases (PI3Ks), useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.