专利号:US-6268499-B1 优先权日:1998-08-10 标 题 :Process and intermediates for preparation of substituted piperidine-epoxides 发明人:GUELLER ROLF; LOHRI BRUNO; SCHMID RUDOLF 权利人:HOFFMANN LA ROCHE 摘要:The present invention concerns intermediates useful in and a process for the preparation of a compound of formula 1 or a salt thereof n comprisingepoxidation of a compound of formula 2 or a salt thereof n wherein A, R 1 and R 2 are as herein defined. These compounds are useful in the synthesis of renin inhibitors.
专利号:US-8067460-B2 优先权日:2004-10-04 标 题 :5-phenoxyalkoxypsoralens and methods for selective inhibition of the voltage gated Kv1.3 potassium channel 发明人:WULFF HEIKE; SANKARANARAYANAN ANANTHAKRISHNAN; HAENSEL WOLFRAM; SCHMITZ ALEXANDER; SCHMIDT-LASSEN KRISTINA 权利人:WULFF HEIKE; SANKARANARAYANAN ANANTHAKRISHNAN; HAENSEL WOLFRAM; SCHMITZ ALEXANDER; SCHMIDT-LASSEN KRISTINA; UNIV CALIFONIA 摘要:Compositions of matter comprising 5-phenoxyalkoxypsoralen compounds and their method of synthesis and use. The compounds are useable to treat diseases or disorders in human or animal subjects, including autoimmune diseases. The compounds inhibit potassium channels, including the Kv1.3 channel and at least some of the therapeutic effects of such compounds may be due at least in part to potassium channel inhibition. In some embodiments, the compounds are more selective for certain potassium channels (e.g., Kv1.3 channels) than other potassium channels (e.g., Kv1.5 channels).
专利号:EP-1399406-B1 优先权日:2001-01-04 标题:Novel estrogen receptor ligands and methods i 发明人:KOEHLER KONRAD; HENSSEN CECILIA; NILSSON MARITA; GILLNER MIKAEL; LIU YE; SANIN ANDREI; WILKENING ROBERT R; RATCLIFFE RONALD W; WENSBO DAVID 权利人:KAROBIO AB; MERCK & CO INC 摘要:The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant inventive are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynecomastia, autoimmune disease, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer of the lung, colon, breast, uterus, and prrostate.
专利号:US-9133224-B2 优先权日:2010-11-29 标 题:Macrocyclic kinase inhibitors 发明人:CREW ANDREW P; DONG HANQING; FERRARO CATERINA; SHERMAN DAN; SIU KAM W 权利人:CREW ANDREW P; DONG HANQING; FERRARO CATERINA; SHERMAN DAN; SIU KAM W; OSI PHARMACEUTICALS LLC 摘要:Compounds of Formula (I): wherein variables are defined herein, and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers for which FAK inhibition is beneficial.
[参考文献]: Alexander Schmitz, Et Al. Design Of Pap-1, A Selective Small Molecule Kv1.3 Blocker, For The Suppression Of Effector Memory T Cells In Autoimmune Diseases. Mol Pharmacol. 2005 Nov;68(5):1254-70.
合成参考文献
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