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91. 发明公开

EP2651916A2 C-17-HETEROARYL STEROIDAL COMPOUNDS AS INHIBITORS OF CYP11B, CYP17, AND/OR CYP21 审中-公开
标题翻译：甾体C-17的杂芳基作为CYP11B，CYP17和/或CYP21抑制剂
公开(公告)号：EP2651916A2
公开(公告)日：2013-10-23
申请号：EP11808473.0
申请日：2011-12-16
申请人： BioMarin Pharmaceutical Inc.
发明人： CHU, Daniel , WANG, Bing , YE, Tao
IPC分类号： C07D401/08 , C07D403/08 , C07D405/08 , C07D413/08 , C07D471/04 , C07J43/00 , C07J61/00 , C07J63/00 , C07J73/00 , A61P5/26 , A61P5/42 , A61P5/46 , A61P35/00 , A61K31/56
CPC分类号： C07J73/008 , C07D401/08 , C07D403/08 , C07D405/08 , C07D413/08 , C07D471/04 , C07J1/0011 , C07J13/005 , C07J21/005 , C07J31/006 , C07J43/003 , C07J61/00 , C07J63/002 , C07J73/003 , C07J73/005
摘要： Provided herein are inhibitors of CYP11B, CYP17, and/or CYP21 enzymes of Formula (Z), (IX), (X), (XI), (XII), (XIII), (XIV), (XV), (XVI), or (XVII). Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions. Formula (Z)

92. 发明公开

EP2077262A1 IMINOPYRIDINE DERIVATIVE AND USE THEREOF 审中-公开
标题翻译：维也纳国际货币基金组织
公开(公告)号：EP2077262A1
公开(公告)日：2009-07-08
申请号：EP07830315.3
申请日：2007-10-22
申请人： Takeda Pharmaceutical Company Limited
发明人： YOSHIDA, Masato , SUZAKI, Tomohiko , KOHARA, Yasuhisa , KUNO, Haruhiko , NAGABUKURO, Hiroshi , SAIKAWA, Reiko , OKABE, Yuuichi , IMAI, Shigemitsu
IPC分类号： C07D213/82 , A61K31/4545 , A61K31/455 , A61K31/497 , A61K31/5377 , A61P1/00 , A61P1/02 , A61P1/08 , A61P1/12 , A61P1/14 , A61P1/16 , A61P1/18 , A61P3/00 , A61P3/02 , A61P3/04 , A61P3/10 , A61P5/00 , A61P5/24 , A61P5/40 , A61P5/42 , A61P7/00
CPC分类号： C07D213/82 , C07D401/06 , C07D405/06 , C07D409/06
摘要： Provided are an iminopyridine derivative having a selective α 1D adrenergic receptor antagonistic action and useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like, and a screening method for a compound having an α 1D adrenergic receptor antagonistic action. An α 1D adrenergic receptor antagonist containing a compound represented by the formula:

wherein each symbol is as defined in the specification, or a salt thereof, and a method of screening for an agent having an α 1D adrenergic receptor antagonistic action for the prophylaxis or treatment of a lower urinary tract disease, which includes measuring the bladder smooth muscle tension of rats with bladder outlet obstruction.
摘要翻译：提供具有选择性±1D肾上腺素能受体拮抗作用并可用作预防或治疗下尿路疾病等的试剂的亚氨基吡啶衍生物和具有±1D肾上腺素能受体拮抗作用的化合物的筛选方法。一种含有由下式表示的化合物的±1D肾上腺素受体拮抗剂：其中每个符号如本说明书中所定义，或其盐，以及筛选具有±1D肾上腺素能受体拮抗作用的药物用于预防或治疗的方法的下尿路疾病，其中包括测量膀胱出口阻塞的大鼠膀胱平滑肌张力。

93. 发明公开

EP1957489A2 BIS-HETEROCYCLIC IMIDAZOLYL COMPOUNDS 审中-公开
标题翻译：双杂环咪唑基化合物
公开(公告)号：EP1957489A2
公开(公告)日：2008-08-20
申请号：EP06830466.6
申请日：2006-12-08
申请人： Speedel Experimenta AG
发明人： HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , QUIRMBACH, Michael , MARTI, Christiane , STOJANOVIC, Aleksandar , STUTZ, Stefan
IPC分类号： C07D471/04 , A61P5/42 , A61K31/437
CPC分类号： C07D471/04
摘要： The patent application relates to new heterocyclic compounds of the general formula (I) in which R, R1, R2, R3, R4 and n have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldosterone synthase inhibitors.
摘要翻译：该专利申请涉及新的通式（I）的杂环化合物，其中R，R 1，R 2，R 3，R 4和n具有在说明书中更详细阐述的定义，涉及制备它们的方法以及这些化合物作为药物，特别是作为醛固酮合酶抑制剂。

94. 发明授权

EP1306089B1 Combination of benzimidazoles having angiotensin-II antagonistic activity with diuretics 失效
标题翻译：血管紧张素II与利尿剂拮抗苯并咪唑的组合
公开(公告)号：EP1306089B1
公开(公告)日：2007-09-05
申请号：EP03001570.5
申请日：1994-06-07
申请人： Takeda Pharmaceutical Company Limited
发明人： Inada, Yoshiyuki , Kubo, Keiji
IPC分类号： A61K31/4184 , A61K31/585 , A61P9/12 , A61P9/04 , A61P9/10 , A61P13/12 , A61P5/42 , A61P17/00 , A61P25/28 , A61P25/24 , A61P25/22 , A61P25/18 , A61P27/06
CPC分类号： A61K45/06 , A61K31/495 , A61K2300/00

95. 发明公开

EP1505072A3 Eplerenone crystalline form exhiniting enhanced dissolution rate 审中-公开
标题翻译：依普利酮的晶体形式具有改善的溶出速率
公开(公告)号：EP1505072A3
公开(公告)日：2006-06-21
申请号：EP04020121.2
申请日：2000-12-04
申请人： Pharmacia Corporation
发明人： Barton, Kathleen , Borchardt, Thomas B. , Carlos, Marlon, V. , Desai, Subhash , Ferro, Leonard, J. , Gaud, Henry, T. , Ganser, Scott , Little, Clay, R. , Mudipalli, Partha S. , Pietz, Mark, A. , Pilipauskas, Daniel R. , Sing, Yuen-Lung, L. , Stahl, Glenn, L. , Wieczorek, Joseph, J. , Yan, Chris Y.
IPC分类号： C07J71/00 , A61K31/58 , A61P5/42
CPC分类号： C07J71/0015
摘要： A novel crystalline form (Form H) of the aldosterone receptor antagonist drug eplerenone is provided having a relatively rapid dissolution rate in aqueous media. Also provided are novel solvated crystalline forms of eplerenone that, when desolvated, can yield Form H eplerenone. Also provided is amorphous eplerenone. Pharmaceutical compositions are provided comprising Form H eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form H eplerenone and for preparing compositions comprising Form H eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form H eplerenone.

96. 发明申请

WO2012083112A3 C- 17 -HETEROARYL STEROIDAL COMPOUNDS AS INHIBITORS OF CYP11B, CYP17, AND/OR CYP21 审中-公开
公开(公告)号：WO2012083112A3
公开(公告)日：2012-06-21
申请号：PCT/US2011/065362
申请日：2011-12-16
申请人： BIOMARIN PHARMACEUTICAL INC. , CHU, Daniel , WANG, Bing , YE, Tao
发明人： CHU, Daniel , WANG, Bing , YE, Tao
IPC分类号： C07D401/08 , C07D403/08 , C07D405/08 , C07D413/08 , C07D471/04 , C07J43/00 , C07J61/00 , C07J63/00 , C07J73/00 , A61P5/26 , A61P5/42 , A61P5/46 , A61P35/00 , A61K31/56
摘要： Provided herein are inhibitors of CYP11B, CYP17, and/or CYP21 enzymes of Formula (Z), (IX), (X), (XI), (XII), (XIII), (XIV), (XV), (XVI), or (XVII). Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions. Formula (Z)

97. 发明申请

WO2010042626A1 1-PHENYLPYRROLE COMPOUNDS 审中-公开
标题翻译： 1-苯基吡咯烷酮化合物
公开(公告)号：WO2010042626A1
公开(公告)日：2010-04-15
申请号：PCT/US2009/059852
申请日：2009-10-07
申请人： EXELIXIS, INC. , Daiichi Sankyo Company, Limited , NUSS, John , WILLIAMS, Matthew , MOHAN, Raju , MARTIN, Richard , WANG, Tie-lin , TSURUOKA, Hiroyuki , AOKI, Kazumasa , HONZUMI, Masatoshi , ASOH, Yusuke , SAITO, Keiji , HOMMA, Tsuyoshi
发明人： NUSS, John , WILLIAMS, Matthew , MOHAN, Raju , MARTIN, Richard , WANG, Tie-lin , TSURUOKA, Hiroyuki , AOKI, Kazumasa , HONZUMI, Masatoshi , ASOH, Yusuke , SAITO, Keiji , HOMMA, Tsuyoshi
IPC分类号： C07D207/335 , A61K31/405 , A61P9/12 , A61P9/10 , A61P13/12 , A61P5/42 , A61P7/10
CPC分类号： C07D207/34
摘要： The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases, nephropathy, fibrosis, primary aldosteronism or edema. The compound is of the following general formula (I): wherein R 1 represents a C1 -C3 alkyl group; R 2 represents a hydroxy -C1 -C4 alkyl group and the like; R 3 represents a halogeno group, a halogeno-C1 -C3 alkyl group and the like; R 4 represents a hydrogen atom, a halogeno group and the like,- R 5 represents a sulfamoyl group or a C1-C3 alkylsulf onyl group; R 6 represents a hydrogen atom, a halogeno group and the like] or an N-oxide, atropisomer of the foregoing, or pharmaceutically acceptable salt of the foregoing.
摘要翻译：本发明包括用于预防和/或治疗心血管疾病，肾病，纤维化，原发性醛固酮增多症或水肿的化合物。该化合物具有以下通式（I）：其中R1表示C1-C3烷基; R 2表示羟基-C 1 -C 4烷基等; R 3表示卤代基，卤代-C 1 -C 3烷基等; R4代表氢原子，卤代基等，R5表示氨磺酰基或C1-C3烷基亚磺酰基; R6表示氢原子，卤代基等]或上述的N-氧化物，阻转异构体或上述的药学上可接受的盐。

98. 发明申请

WO2007025780A3 ALDOSTERONE RECEPTOR ANTAGONISTS 审中-公开
标题翻译：醛固酮受体拮抗剂
公开(公告)号：WO2007025780A3
公开(公告)日：2007-07-26
申请号：PCT/EP2006008593
申请日：2006-09-01
申请人： RECORDATI IRELAND LTD , RECORDATI CHEM PHARM
发明人： LEONARDI AMEDEO , RIVA CARLO , TAVECCHIA PAOLO , SIRONI GIORGIO
IPC分类号： C07J21/00 , A61K31/58 , A61P5/42 , C07J31/00 , C07J41/00 , C07J43/00 , C07J53/00 , C07J71/00
CPC分类号： C07J21/003 , C07J21/00 , C07J31/006 , C07J41/0038 , C07J43/006 , C07J53/001 , C07J71/00 , C07J71/0015
摘要： Compounds of the formula (I), (R 1 is one of a wide range of substituents; R 2 = H, halogen and R 3 = H, hydroxymethyl or CR 2 R 3 = cyclopropyl ring; CR 4 R 5 is one of formula (II), formula (III) and formula (IV) R a and R b are a bond between carbons 9 and 11 or an -O-, -S-, -CH 2 - or -CF 2 - bridge; R 6 is H, alkyl, -CH 2 OR x , -CH 2 SR x , -CH 2 SO-alkyl, -CH 2 SO 2 -alkyl, -CH 2 NHR x , -CH 2 N(alkyl)(R x ), -C(=O)O-alkyl, -C(=O)-alkyl, -C(=O)NHR x or -C(=O)N(alkyl)(R x ); R 7 = R 8 = H or CR 7 R 8 is a cyclopropyl ring; R 9 and R 9' are H, halogen, alkyl or alkoxycarbonyl or a bond between carbons 22 and 23; R 10 is H or -C(=O)OR x ; R x is H, alkyl or acyl; R y is H, alkyl; R z is H, alkyl) are provided. They are aldosterone receptor antagonists, useful for the treatment of aldosteronism including hypertension, cardiovascular disease, renal dysfunction, edema, cerebrovascular disease and insulinopathies.
摘要翻译：式（I）化合物，（R 1是一系列取代基中的一种; R 2 = H，卤素和R 3 = = H，羟甲基或CR 2 R 3 =环丙基环; CR 4 R 5是式（ II），式（III）和式（IV）中，R a和R b是碳9和碳11之间的键或-O - ， - S - ， - CH 2 - 或-CF 2 - 桥; R 6是H，烷基，-CH 2，OR 2， CH 2，SO 2 CH 2，SO 2 CH 2，SO 2 CH 2，SO 2 CH 2，（烷基）（R 2）， - （C 1 -C 4）烷基， - （C 1 -C 4）（= O）O-烷基，-C（= O） - 烷基，-C（= O）NHR x x或-C（= O））N（烷基）（R xx）; R 7 = R 8 = H或CR 7 R 9，其中R 9和R 9'为H，卤素，烷基或烷氧基羰基或碳22和碳23之间的键; R 9和R 9'为H，卤素，烷基或烷氧基羰基或碳22和23之间的键; R 其中R 10为H或-C（= O）OR x; R x为H，烷基或酰基; 其中Y是H，烷基; R z是H，烷基）。它们是醛固酮受体拮抗剂，可用于治疗醛固酮增多症，包括高血压，心血管疾病，肾功能不全，水肿，脑血管疾病和胰岛素病。

99. 发明申请

WO2007065942A2 BIS-HETEROCYCLIC IMIDAZOLYL COMPOUNDS 审中-公开
标题翻译：双杂环咪唑基化合物
公开(公告)号：WO2007065942A2
公开(公告)日：2007-06-14
申请号：PCT/EP2006/069462
申请日：2006-12-08
申请人： SPEEDEL EXPERIMENTA AG , HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , QUIRMBACH, Michael , MARTI, Christiane , STOJANOVIC, Aleksandar , STUTZ, Stefan
发明人： HEROLD, Peter , MAH, Robert , TSCHINKE, Vincenzo , QUIRMBACH, Michael , MARTI, Christiane , STOJANOVIC, Aleksandar , STUTZ, Stefan
IPC分类号： C07D471/04 , A61K31/437 , A61P5/42
CPC分类号： C07D471/04
摘要： The patent application relates to new heterocyclic compounds of the general formula (I) in which R, R 1 , R 2 , R 3 , R 4 and n have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldosterone synthase inhibitors.
摘要翻译：该专利申请涉及通式（I）的新的杂环化合物，其中R，R 1，R 2，R 4，R 5， R 3和R 4具有在说明书中更详细阐述的定义，涉及它们的制备方法以及这些化合物作为药物的用途，特别是作为醛固酮合酶抑制剂

100. 发明申请

WO02000653A2 FUSED CYCLIC MODULATORS OF NUCLEAR HORMONE RECEPTOR FUNCTION 审中-公开
标题翻译：核激素受体功能的融合循环调节剂
公开(公告)号：WO02000653A2
公开(公告)日：2002-01-03
申请号：PCT/US2001/019663
申请日：2001-06-20
IPC分类号： C07D487/08 , A61K31/00 , A61K31/407 , A61K31/4188 , A61K31/423 , A61K31/53 , A61K31/655 , A61K31/675 , A61K45/00 , A61P1/04 , A61P1/14 , A61P1/16 , A61P3/00 , A61P3/04 , A61P3/10 , A61P5/24 , A61P5/26 , A61P5/30 , A61P5/38 , A61P5/40 , A61P5/42 , A61P5/44 , A61P5/46 , A61P7/00 , A61P7/04 , A61P7/08 , A61P9/00 , A61P9/04 , A61P9/14 , A61P11/00 , A61P11/06 , A61P13/08 , A61P13/12 , A61P15/00 , A61P15/04 , A61P15/08 , A61P15/10 , A61P15/12 , A61P15/16 , A61P15/18 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P21/00 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/28 , A61P25/30 , A61P27/00 , A61P27/16 , A61P29/00 , A61P31/04 , A61P31/18 , A61P35/00 , A61P37/00 , A61P37/02 , A61P37/06 , A61P43/00 , C07D207/12 , C07D471/18 , C07D487/18 , C07D491/08 , C07D491/18 , C07D491/22 , C07D495/18 , C07D519/00 , C07K14/72 , C12N5/10 , C12Q1/66 , C07D471/00
CPC分类号： C07D487/08 , A61K31/00 , A61K31/407 , A61K31/655 , A61K31/675 , C07D207/12 , A61K2300/00
摘要： Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.
摘要翻译：稠合的环状化合物，使用这些化合物治疗核激素受体相关病症如癌症和免疫疾病的方法，以及含有这些化合物的药物组合物。

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