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参考文献: Prolyl Hydroxylase Inhibitors[fr] Inhibiteurs De Prolyle Hydroxylase
标题: Prolyl Hydroxylase Inhibitors[fr] Inhibiteurs De Prolyle Hydroxylase
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2912110000-甲醛
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专利信息
专利号:US-2012053350-A1
优先权日:2009-04-30
标题 :Preparation of alkyl esters of n-protected oxo-azacycloalkylcarboxylic acids
发明人:MANGION IAN; HUFFMAN MARK A; RUCK REBECCA T; LYNCH JOSEPH; CHUNG JOHN Y L; MARCUNE BENJAMIN
权利人:MANGION IAN; HUFFMAN MARK A; RUCK REBECCA T; LYNCH JOSEPH; CHUNG JOHN Y L; MARCUNE BENJAMIN
摘要:A process for the preparation of alkyl esters of N-protected oxo-azacycloalkylcarboxylic acids of Formula III: comprises contacting a ketosulfoxonium ylide of Formula II: with an iridium catalyst to obtain Compound III, wherein P G1 is an amine protective group; k is 0, 1, or 2; and R U , R 1 , R 2 , and R 3 are defined herein. An embodiment of the process further com rises contacting a compound of Formula I: with a sulfoxonium halide of formula (R U ) 3 S(O)Z, wherein Z is halide, in the presence of a strong base to obtain Compound II. Additional embodiments add a series of process steps leading to the synthesis of 7-oxo-1,6-diazabicyclo[3.2.1]octanes suitable for use as β-lactamase inhibitors.
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-9839642-B2
优先权日:2014-05-09
标 题:Beta-tetrazolyl-propionic acids as metallo-beta-lactamase inhibitors
发明人:TANG HAIFENG; YANG SHU-WEI; MANDAL MIHIR; SU JING; LI GUOQING; PAN WEIDONG; TANG HAIQUN; DEJESUS REYNALDA; PAN JIANPING; HAGMANN WILLIAM; DING FA-XIANG; XIAO LI; PASTERNAK ALEXANDER; HUANG YUHUA; DONG SHUZHI; YANG DEXI
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula I that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
专利号:US-8791131-B2
优先权日:2008-09-30
标题 :Imidazo[1,5]naphthyridine compounds, their pharmaceutical use and compositions
发明人:CHENG HENGMIAO; JOHNSON TED WILLIAM; HOFFMAN JACQUI ELIZABETH; GUO LISA CHEN; LIU ZHENGYU
权利人:CHENG HENGMIAO; JOHNSON TED WILLIAM; HOFFMAN JACQUI ELIZABETH; GUO LISA CHEN; LIU ZHENGYU; PFIZER
摘要:The present invention is directed to compounds of Formula (I), n nand to salts thereof, their synthesis, and their use as PI3-Kα inhibitors and/or PI3-Kα/mTOR dual inhibitors.