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公开(公告)号：EP2651882B1
公开(公告)日：2018-11-14
申请号：EP11804528.5
申请日：2011-12-12
IPC分类号： C07C319/06 , C07C323/40 , C07C327/30 , C07D277/64
CPC分类号： A61K31/16 , A61K31/167 , C07C319/06 , C07C327/30 , C07C327/34 , C07C2601/14 , C07D277/64 , C07C323/40
摘要： The present invention relates to a process for the preparation of S-[2-[1-(2-ethylbutyl)cyclohexylcarbonylamino]-phenyl]2-methylthiopropionate which is useful as a pharmaceutically active compound.
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公开(公告)号：EP2616433B1
公开(公告)日：2015-12-09
申请号：EP11758183.5
申请日：2011-09-13
IPC分类号： C07C253/30 , C07C51/06 , C07C51/08 , C07C51/60 , C07C61/08 , C07C319/06 , C07C319/22 , C07C327/06 , C07C255/46 , C07C321/28
CPC分类号： C07C253/30 , C07C51/06 , C07C51/08 , C07C51/60 , C07C231/02 , C07C231/06 , C07C231/12 , C07C319/06 , C07C319/22 , C07C327/30 , C07C2601/14 , C07C255/46 , C07C323/40 , C07C61/08
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3.发明公开DERIVATIVES OF CYCLOALKYL- AND CYCLOALKENYL-1,2-DICARBOXYLIC ACID COMPOUNDS HAVING FORMYL PEPTIDE RECEPTOR LIKE-1 (FPRL-1) AGONIST OR ANTAGONIST ACTIVITY 审中-公开衍生的大肠杆菌 - 环丙基-1,2-DICARBONSÄUREVERBINDUNGENMIT FORMYLPEPTIDREZEPTOR-LIKE-1（FPRL-1）-AGONISTISCHER ODER ANTAGONISTISCHER WIRKUNG
公开(公告)号：EP2585054A1
公开(公告)日：2013-05-01
申请号：EP11729858.8
申请日：2011-06-23
申请人： Allergan, Inc.
IPC分类号： A61K31/167 , A61K31/192 , A61K31/216 , A61K31/44 , C07C233/45 , A61P27/02 , A61P27/06 , A61P29/00
CPC分类号： C07C323/40 , A61K31/16 , A61K31/167 , A61K31/192 , A61K31/195 , A61K31/215 , A61K31/216 , A61K31/4035 , A61K31/44 , C07C233/58 , C07C233/59 , C07C311/46 , C07C2603/94 , C07D213/75 , C07D493/08
摘要： The invention provides well defined compounds having FPRL-1 agonist or antagonist activity. As such, the compounds of the invention are useful for treating a variety of ocular disorders.
摘要翻译： 本发明提供具有FPRL-1激动剂或拮抗剂活性的明确定义的化合物。 因此，本发明的化合物可用于治疗各种眼部疾病。
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公开(公告)号：EP1249233B9
公开(公告)日：2009-08-05
申请号：EP00976387.1
申请日：2000-11-21
申请人： SHIONOGI & CO., LTD.
发明人： KAWANISHI, Yasuyuki Shionogi & Co., Ltd. , TAKENAKA, Hideyuki Shionogi & Co., Ltd. , HANASAKI, Kohji Shionogi & Co., Ltd. , OKADA, Tetsuo Shionogi & Co., Ltd.
IPC分类号： A61K31/18 , C07C311/06 , C07C311/20 , C07C311/46 , C07C323/40 , C07D207/12 , C07D209/08 , C07D209/48 , C07D209/88 , C07D211/58 , C07D213/75 , C07D215/36 , C07D217/04 , C07D219/10 , C07D231/16 , C07D231/56 , C07D233/68 , C07D239/42 , C07D277/56 , C07D285/06 , C07D295/12 , C07D307/68 , C07D307/91 , C07D311/16 , C07D317/66 , C07D333/38 , C07D333/72 , A61P3/00
CPC分类号： C07D249/08 , A61K31/00 , A61K31/18 , A61K31/341 , A61K31/351 , A61K31/357 , A61K31/37 , A61K31/381 , A61K31/4015 , A61K31/402 , A61K31/4035 , A61K31/41 , A61K31/4196 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/433 , A61K31/44 , A61K31/4409 , A61K31/4453 , A61K31/451 , A61K31/495 , A61K31/4965 , A61K31/505 , A61K31/5375 , A61K31/63 , A61K31/635 , C07C311/06 , C07C311/07 , C07C311/08 , C07C311/14 , C07C311/20 , C07C311/21 , C07C311/46 , C07C323/40 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/44 , C07C2603/18 , C07D207/09 , C07D207/12 , C07D207/16 , C07D209/08 , C07D209/48 , C07D209/88 , C07D211/58 , C07D211/62 , C07D213/75 , C07D213/82 , C07D215/36 , C07D215/38 , C07D217/04 , C07D219/10 , C07D231/12 , C07D231/16 , C07D231/56 , C07D233/56 , C07D233/68 , C07D239/42 , C07D277/56 , C07D277/70 , C07D285/06 , C07D295/135 , C07D307/68 , C07D307/91 , C07D311/16 , C07D317/66 , C07D333/38 , C07D333/72
摘要： NPYY5 receptor antagonists which contain compounds represented bygeneral formula (I), prodrugs thereof, pharmaceutically acceptable salts thereof or solvates of the same wherein R1 represents lower alkyl, cycloalkyl, etc.; R2 represents hydrogen, lower alkyl, etc.; n is 1 or 2; X represents lower alkylene, lower alkenylene, arylene, cycloalkylene, etc.; Y represents CONR?7, CSNR7, NR7CO, NR7¿CS, etc. (wherein R7 represents hydrogen or lower alkyl); and Z represents lower alkyl, an optionally substituted hydrocarbon cycle, an optionally substituted heterocycle, etc.
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公开(公告)号：EP2035129A1
公开(公告)日：2009-03-18
申请号：EP07726181.6
申请日：2007-07-02
申请人： Merck Patent GmbH
发明人： HIERSE, Wolfgang , IGNATYEV, Nikolai (Mykola) , SEIDEL, Martin , MONTENEGRO, Elvira , KIRSCH, Peer , BATHE, Andreas
IPC分类号： B01F17/00
CPC分类号： C07C381/00 , B01F17/0035 , B01F17/005 , B01F17/0057 , C07C17/12 , C07C17/16 , C07C17/18 , C07C17/25 , C07C205/11 , C07C205/37 , C07C211/29 , C07C211/52 , C07C215/68 , C07C217/84 , C07C229/60 , C07C233/64 , C07C323/09 , C07C323/20 , C07C323/36 , C07C323/40 , C07C323/62 , C07C25/13 , C07C22/08
摘要： The invention relates to the use of Y terminal groups, wherein Y represents (formula I), Rf represents CF3-(CH2)r-, CF3-(CH2)r-O-, CF3-(CH2)r-S-, CF3CF2-S-, SF5- (CH2)r-, [CF3-(CH2)r]2N-, [CF3-(CH2)r]NH- or (CF3)2N-(CH2)r-, B represents a single bond, O, NH, NR, CH2, C(O)-O, C(O), S, CH2-O, O-C(O), N-C(O), C(O)-N, O-C(O)-N, N-C(O)-N, O-SO2 or SO2-O, R represents alkyl having 1 to 4 C-atoms, b represents 0 or 1 and c represents 0 or 1, q represents 0 or 1, at least one radical from b and q represents 1, and r represents 0, 1, 2, 3, 4 or 5, as a terminal group in the surface-active compounds. The invention also relates to corresponding compounds and to a method for producing said compounds.
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6.发明公开COMPOSITIONS AND METHODS FOR THE TREATMENT OF DISEASE ASSOCIATED WITH TRP-P8 EXPRESSION 审中-公开组合物和方法用于治疗TRP-P8相关疾病的表达
公开(公告)号：EP1663962A4
公开(公告)日：2007-08-22
申请号：EP04781589
申请日：2004-08-20
申请人： DENDREON CORP
发明人： NATARAJAN SATEESH K , MORENO OFIR , GRADDIS THOMAS J , DUNCAN DAVID , LAUS REINER , CHEN FENG
IPC分类号： A61K31/498 , A61K31/517 , A61K45/06 , A61P35/00 , C07C311/20 , C07C311/37 , C07C323/40 , C07C323/44 , C07C333/06 , C07D207/06 , C07D207/09 , C07D207/32 , C07D207/325 , C07D209/08 , C07D209/14 , C07D209/20 , C07D209/48 , C07D213/40 , C07D215/04 , C07D215/08 , C07D215/46 , C07D217/06 , C07D231/12 , C07D231/14 , C07D231/56 , C07D235/18 , C07D235/26 , C07D239/42 , C07D241/18 , C07D241/44 , C07D251/54 , C07D263/34 , C07D263/56 , C07D263/57 , C07D279/12 , C07D295/096 , C07D295/135 , C07D295/26 , C07D307/52 , C07D317/66 , C07D333/34 , C07D401/04 , C07D405/12 , C07D413/04 , C07D413/12 , C07D417/04 , C07D471/04 , C07D487/04 , C07D493/08 , C07D495/04 , C07D513/04 , G01N33/68
CPC分类号： C07C233/60 , A61K31/498 , A61K31/517 , A61K45/06 , C07C233/58 , C07C243/36 , C07C243/38 , C07C311/20 , C07C311/37 , C07C323/40 , C07C323/44 , C07C333/06 , C07C2601/14 , C07C2601/18 , C07C2602/42 , C07D207/06 , C07D207/09 , C07D207/325 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/20 , C07D209/48 , C07D211/06 , C07D213/40 , C07D215/04 , C07D215/08 , C07D215/46 , C07D217/06 , C07D223/04 , C07D231/12 , C07D231/14 , C07D231/56 , C07D235/18 , C07D235/26 , C07D239/42 , C07D241/18 , C07D241/44 , C07D241/54 , C07D251/54 , C07D263/34 , C07D263/57 , C07D279/12 , C07D295/096 , C07D295/135 , C07D295/155 , C07D295/26 , C07D307/52 , C07D311/16 , C07D317/66 , C07D333/34 , C07D401/04 , C07D403/14 , C07D405/12 , C07D413/04 , C07D413/12 , C07D417/04 , C07D471/04 , C07D487/04 , C07D493/08 , C07D495/04 , C07D513/04 , G01N33/5011 , G01N33/6872 , G01N2500/10 , A61K2300/00
摘要： Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Tip-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.
摘要翻译： 本发明提供小分子Trp-p8调节剂，包括TRP-P8激动剂和Trp-p8的拮抗剂，和组合物包含小分子Trp-p8的激动剂，以及用于鉴定和表征新型小分子Trp-p8调节剂和方法的方法 降低活力和/或抑制TRP-P8的生长表达细胞，用于激活方法的Trp-p8的介导的阳离子内流，用于刺激细胞凋亡和/或坏死，以及相关的方法，用于治疗疾病，包括癌症的方法：如肺，乳腺 ，结肠癌和/或前列腺癌以及其他疾病，良性前列腺增生：如，没与TRP-P8表达相关。
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7.发明公开COMPOSITIONS AND METHODS FOR THE TREATMENT OF DISEASE ASSOCIATED WITH TRP-P8 EXPRESSION 审中-公开组合物和方法用于治疗TRP-P8相关疾病的表达
公开(公告)号：EP1663962A2
公开(公告)日：2006-06-07
申请号：EP04781589.9
申请日：2004-08-20
申请人： DENDREON CORPORATION , Natarajan, Sateesh K. , Moreno, Ofir , Graddis, Thomas J. , Duncan, David , Laus, Reiner , Chen, Feng
发明人： NATARAJAN, Sateesh K. , MORENO, Ofir , GRADDIS, Thomas J. , DUNCAN, David , LAUS, Reiner , CHEN, Feng
IPC分类号： C07C303/00 , C07C321/00 , C07C69/95 , C07C69/76 , C07C35/08 , C07C31/12 , C07D345/00
CPC分类号： C07C233/60 , A61K31/498 , A61K31/517 , A61K45/06 , C07C233/58 , C07C243/36 , C07C243/38 , C07C311/20 , C07C311/37 , C07C323/40 , C07C323/44 , C07C333/06 , C07C2601/14 , C07C2601/18 , C07C2602/42 , C07D207/06 , C07D207/09 , C07D207/325 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/20 , C07D209/48 , C07D211/06 , C07D213/40 , C07D215/04 , C07D215/08 , C07D215/46 , C07D217/06 , C07D223/04 , C07D231/12 , C07D231/14 , C07D231/56 , C07D235/18 , C07D235/26 , C07D239/42 , C07D241/18 , C07D241/44 , C07D241/54 , C07D251/54 , C07D263/34 , C07D263/57 , C07D279/12 , C07D295/096 , C07D295/135 , C07D295/155 , C07D295/26 , C07D307/52 , C07D311/16 , C07D317/66 , C07D333/34 , C07D401/04 , C07D403/14 , C07D405/12 , C07D413/04 , C07D413/12 , C07D417/04 , C07D471/04 , C07D487/04 , C07D493/08 , C07D495/04 , C07D513/04 , G01N33/5011 , G01N33/6872 , G01N2500/10 , A61K2300/00
摘要： Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Tip-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.
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公开(公告)号：EP1249233A4
公开(公告)日：2005-04-13
申请号：EP00976387
申请日：2000-11-21
申请人： SHIONOGI & CO
IPC分类号： A61K20060101 , A61K31/00 , A61K31/18 , A61K31/341 , A61K31/351 , A61K31/357 , A61K31/37 , A61K31/381 , A61K31/4015 , A61K31/402 , A61K31/4035 , A61K31/41 , A61K31/415 , A61K31/4196 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/433 , A61K31/44 , A61K31/4409 , A61K31/4453 , A61K31/451 , A61K31/495 , A61K31/4965 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/63 , A61K31/635 , A61P20060101 , A61P3/04 , A61P43/00 , C07C20060101 , C07C311/06 , C07C311/07 , C07C311/08 , C07C311/14 , C07C311/20 , C07C311/21 , C07C311/46 , C07C323/40 , C07D20060101 , C07D207/09 , C07D207/12 , C07D207/16 , C07D209/08 , C07D209/48 , C07D209/88 , C07D211/08 , C07D211/58 , C07D211/62 , C07D213/75 , C07D213/82 , C07D215/36 , C07D215/38 , C07D217/04 , C07D219/10 , C07D231/12 , C07D231/16 , C07D231/56 , C07D233/68 , C07D239/42 , C07D241/02 , C07D261/08 , C07D265/30 , C07D277/46 , C07D277/56 , C07D277/70 , C07D285/06 , C07D295/135 , C07D307/02 , C07D307/68 , C07D307/91 , C07D311/16 , C07D317/66 , C07D333/38 , C07D333/72 , C07D521/00 , A61P3/00 , C07D295/12
CPC分类号： C07D249/08 , A61K31/00 , A61K31/18 , A61K31/341 , A61K31/351 , A61K31/357 , A61K31/37 , A61K31/381 , A61K31/4015 , A61K31/402 , A61K31/4035 , A61K31/41 , A61K31/4196 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/433 , A61K31/44 , A61K31/4409 , A61K31/4453 , A61K31/451 , A61K31/495 , A61K31/4965 , A61K31/505 , A61K31/5375 , A61K31/63 , A61K31/635 , C07C311/06 , C07C311/07 , C07C311/08 , C07C311/14 , C07C311/20 , C07C311/21 , C07C311/46 , C07C323/40 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/44 , C07C2603/18 , C07D207/09 , C07D207/12 , C07D207/16 , C07D209/08 , C07D209/48 , C07D209/88 , C07D211/58 , C07D211/62 , C07D213/75 , C07D213/82 , C07D215/36 , C07D215/38 , C07D217/04 , C07D219/10 , C07D231/12 , C07D231/16 , C07D231/56 , C07D233/56 , C07D233/68 , C07D239/42 , C07D277/56 , C07D277/70 , C07D285/06 , C07D295/135 , C07D307/68 , C07D307/91 , C07D311/16 , C07D317/66 , C07D333/38 , C07D333/72
摘要： NPYY5 receptor antagonists which contain compounds represented bygeneral formula (I), prodrugs thereof, pharmaceutically acceptable salts thereof or solvates of the same wherein R1 represents lower alkyl, cycloalkyl, etc.; R2 represents hydrogen, lower alkyl, etc.; n is 1 or 2; X represents lower alkylene, lower alkenylene, arylene, cycloalkylene, etc.; Y represents CONR?7, CSNR7, NR7CO, NR7¿CS, etc. (wherein R7 represents hydrogen or lower alkyl); and Z represents lower alkyl, an optionally substituted hydrocarbon cycle, an optionally substituted heterocycle, etc.
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9.发明公开
公开(公告)号：EP1472214A2
公开(公告)日：2004-11-03
申请号：EP03737732.2
申请日：2003-02-10
IPC分类号： C07C237/10 , C07C323/29 , C07C323/40 , C07C323/41 , C07C323/42 , C07C323/44 , C07C323/49 , C07C323/52 , C07C323/60 , C07C335/18 , C07D207/32 , C07D213/38 , C07D213/70 , C07D213/73 , C07D213/81
CPC分类号： C07D207/335 , C07C45/46 , C07C45/673 , C07C205/56 , C07C211/29 , C07C229/34 , C07C233/11 , C07C237/10 , C07C237/14 , C07C317/44 , C07C323/29 , C07C323/40 , C07C323/41 , C07C323/42 , C07C323/44 , C07C323/49 , C07C323/52 , C07C323/60 , C07C335/18 , C07C2601/02 , C07C2601/14 , C07D211/24 , C07D211/96 , C07D213/38 , C07D213/70 , C07D213/73 , C07D213/81 , C07D213/82 , C07D231/14 , C07D233/20 , C07D233/64 , C07D271/06 , C07D277/28 , C07D277/64 , C07D295/185 , C07D413/12 , C07C49/83
摘要： Compounds, compositions and methods for altering insulin secretion, particularly in the context of treatment of subjects having, or suspected of being at risk for having, diabetes mellitus. The compounds have the following struture (I): (I)including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein W1, W2, X, R1, R2, R3, R4, m and n are defined herein.
摘要翻译： 化合物，组合物和用于改变胰岛素分泌，特别是在治疗的受试者具有，或用于具有被怀疑处于危险，糖尿病的上下文中的方法。 所述化合物具有以下结构（I）：包括其立体异构体，前药和药学上可接受的盐，worinW¯¯ 1 ，W 2 ，X，R 1 ，R 2 ，R 3 ，R 4 ，m和n中所定义。
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10.发明公开ABCA-1 ELEVATING COMPOUNDS AGAINST CORONARY ARTERY DISEASE OR ATHEROSCLEROSIS 审中-公开ABCA-1表达 - 刺激素VERBINDUNGEN GEGEN KORONARARTERIEN-ERKRANKUNGEN ODER ATHEROSCLOSE
公开(公告)号：EP1379517A2
公开(公告)日：2004-01-14
申请号：EP01995408.0
申请日：2001-12-06
IPC分类号： C07D319/08
CPC分类号： C07D319/08 , A61K31/53 , A61K45/06 , C07C237/06 , C07C237/22 , C07C237/40 , C07C275/26 , C07C311/20 , C07C323/36 , C07C323/40 , C07C323/60 , C07C327/42 , C07C327/48 , C07C2601/08 , C07C2601/14 , C07C2602/10 , C07C2602/40 , C07C2602/42 , C07C2603/74 , C07D251/16 , C07D251/52 , C07D409/12 , A61K2300/00
摘要： The present invention provides compounds that elevate cellular expression of the ABCA-1 gene, promoting cholesterol efflux from cells and increasing HDL levels in the plasma of a mammal, in particular humans. The compounds are useful for treating coronary artery disease.
摘要翻译： 本发明提供了提高ABCA-1基因的细胞表达，促进来自细胞的胆固醇流出并增加哺乳动物，特别是人的血浆中的HDL水平的化合物。 该化合物可用于治疗冠状动脉疾病。
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