专利号:US-8772301-B2 优先权日:2009-12-18 标题 :Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof 发明人:HARDY LARRY WENDELL; HEFFERNAN MICHELE L R; WU FRANK XINHE; SPEAR KERRY L; SARASWAT LAKSHMI D 权利人:HARDY LARRY WENDELL; HEFFERNAN MICHELE L R; WU FRANK XINHE; SPEAR KERRY L; SARASWAT LAKSHMI D; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
专利号:US-2008269233-A1 优先权日:2005-08-04 标 题:Piperidinoyl-Pyrrolidine and Piperidinoyl-Piperidine Compounds 发明人:ANDREWS MARK DAVID; BROWN ALAN DANIEL; SEBASTIEN DAVID; LANSDELL MARK IAN 权利人:ANDREWS MARK DAVID; BROWN ALAN DANIEL; SEBASTIEN DAVID; LANSDELL MARK IAN 摘要:The present invention relates to a class of compounds of general formula (I) n n n n n n n n n n and the salts, hydrates, solvates, polymorphs and prodrugs wherein n, R 6 , R 7 and R 10 are as defined herein and especially to MCR4 agonist compounds of formula (I), to their use in medicine, particularly in the treatment of sexual dysfunction and obesity, to intermediates useful in their synthesis and to compositions containing them.
专利号:EP-1641453-B1 优先权日:2003-06-25 标题 :Product containing at least one phosphatase cdc25 inhibitor combined with at least one other anticancer agent 发明人:PREVOST GREGOIRE; BREZAK PANNETIER MARIE-CHRISTINE; DIOLEZ CHRISTIAN 权利人:IPSEN PHARMA 摘要:The invention relates to a product containing at least one phosphatase Cdc25 inhibitor combined with at least one other anticancer agent for simultaneous, separate or staggered therapeutic use during treatment for cancer. According to the invention, the other anticancer agent is preferably selected from: DNA base analogs such as 5-fluorouracil; inhibitors of type I and/or type II topoisomerases, such as camptothecin and the analogs thereof, doxorubicin or amsacrine; compounds interacting with the cellular spindle, for example, paclitaxel (Taxol); compounds acting on the cytoskeleton, such as vinblastine; inhibitors of the transduction of the signal passing via the heterotrimeric G proteins; prenyltransferase inhibitors, and especially farnesyltransferase inhibitors; cyclin-dependent kinase (CDKs) inhibitors; alkylating agents such as cisplatin; folic acid antagonists such as methotrexate; and inhibitors of DNA synthesis and cellular division, such as mitomycin C. The invention also relates to (1R)-1-[({(2R)-2-amino--3-[(8S)-8-(cyclohexylmethyl)-2-phenyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]--3-oxopropyl}dithio)methyl]-2-[(8S)-8-(cyclohexylmethyl)-2-phenyl--5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]-2-oxoethylamine, or the pharmaceutically acceptable salts thereof, that can be used as anticancer agents.