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31. 发明申请

WO2011146371A1 DIAZENIUMDIOLATE CYCLOHEXYL DERIVATIVES 审中-公开
标题翻译：二氮杂环丁烷衍生物
公开(公告)号：WO2011146371A1
公开(公告)日：2011-11-24
申请号：PCT/US2011/036607
申请日：2011-05-16
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , YAN, Lin , HUO, Pei , NARGUND, Ravi
发明人： ALI, Amjad , YAN, Lin , HUO, Pei , NARGUND, Ravi
IPC分类号： A01N33/26 , A61K31/13 , A61K31/15
CPC分类号： C07C291/02 , C07B59/001 , C07C2601/14
摘要： A compound having the structure (I) or a pharmaceutically acceptable salt thereof, wherein R 3 is hydrogen, deuterium, -OH, -OC 1-6 alkyl, or halogen; R 8 is hydrogen, deuterium, or C 1-6 alkyl; R 11 and R 12 are independently hydrogen, -C 1-6 alkyl, -OH, -OC 1-6 alkyl, or halogen; R 13 and R 14 are independently -C 1-6 alkyl, -(CH 2 ) 1-2 OH, or -OC 1-6 alkyl, or, together with the nitrogen atom to which they are attached, form a 4- to 7-membered heterocyclic ring containing one nitrogen atom and 0 or 1 oxygen atoms, wherein said ring is unsubstituted or mono-, di- or tri-substituted with halogen or -C 1-6 alkyl; R 15 is (CR 1 R 2 ) n C(O)OR 16 , wherein n is 0, 1 or 2, -C(O)NHCH(R 17 )OR 16 , or -C(O)NHCH(R 17 )C(O)NHCH(R 18 )C(O)OR 16 ; R 16 is hydrogen, C 1-6 alkyl, or (CH 2 ) 1-2 N+R 19 R 20 R 21 ; R 1 , R 2 , R 4 , R 5 , R 6 , R 7 , R 9 , R 10 , R 17 , R 18 , R 19 , R 20 , and R 21 are independently hydrogen or -C 1-6 alkyl; and stereoisomers thereof, and pharmaceutically acceptable salts thereof, and pharmaceutically acceptable salts of stereoisomers thereof.
摘要翻译：具有结构（I）的化合物或其药学上可接受的盐，其中R 3是氢，氘，-OH，-OC 1-6烷基或卤素; R8是氢，氘或C1-6烷基; R 11和R 12独立地是氢，-C 1-6烷基，-OH，-OC 1-6烷基或卤素; R 13和R 14独立地为C 1-6烷基， - （CH 2）1-2 OH或-OC 1-6烷基，或者与它们所连接的氮原子一起形成含有一个氮的4-至7-元杂环原子和0或1个氧原子，其中所述环是未取代的或被卤素或-C 1-6烷基单取代，二取代或三取代; R15是（CR1R2）nC（O）OR16，其中n是0,1或2，-C（O）NHCH（R17）OR16或-C（O）NHCH（R17）C（O）NHCH（R18）（O）OR 16; R16是氢，C1-6烷基或（CH2）1-2N + R19R20R21; R 1，R 2，R 4，R 5，R 6，R 7，R 9，R 10，R 17，R 18，R 19，R 20和R 21独立地为氢或-C 1-6烷基; 其立体异构体及其药学上可接受的盐及其立体异构体的药学上可接受的盐。

32. 发明申请

WO2010062415A1 NITROOXY CYCLOALKANE DERIVATIVES 审中-公开
公开(公告)号：WO2010062415A1
公开(公告)日：2010-06-03
申请号：PCT/US2009/051794
申请日：2009-07-27
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , BAKER, Robert, K. , RUPPRECHT, Kathleen, M. , LO, Michael, Man-Chu , WHITEHEAD, Brent
发明人： ALI, Amjad , BAKER, Robert, K. , RUPPRECHT, Kathleen, M. , LO, Michael, Man-Chu , WHITEHEAD, Brent
IPC分类号： A01N37/08 , A61K31/19 , A61K31/557
CPC分类号： C07D257/04 , C07D249/12
摘要： A compound having the structure wherein Y is selected from the group consisting of –C(O)OR 2 , -C(O)NHR 8 , -C(CH 2 ) 1-2 OR3, OH, and or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
摘要翻译：具有结构的化合物，其中Y选自-C（O）OR 2，-C（O）NHR 8，-C（CH 2）1-2OR 3，OH及其药学上可接受的盐，以及使用该化合物治疗高血压。

33. 发明申请

WO2013043518A1 IMIDAZOPYRIDYL COMPOUNDS AS ALDOSTERONE SYNTHASE INHIBITORS 审中-公开
标题翻译：作为阿糖胞苷合成酶抑制剂的咪唑吡啶化合物
公开(公告)号：WO2013043518A1
公开(公告)日：2013-03-28
申请号：PCT/US2012/055694
申请日：2012-09-17
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , BENNETT, D. Jonathan , CAI, Jaiqiang , CARSWELL, Emma , COOKE, Andrew , HOYT, Scott, B. , LO, Michael , LONDON, Clare , MACLEAN, John , PARK, Min, K. , RATCLIFFE, Paul , TAYLOR, Jerry Andrew , WHITEHEAD, Brent , XIONG, Yusheng
发明人： ALI, Amjad , BENNETT, D. Jonathan , CAI, Jaiqiang , CARSWELL, Emma , COOKE, Andrew , HOYT, Scott, B. , LO, Michael , LONDON, Clare , MACLEAN, John , PARK, Min, K. , RATCLIFFE, Paul , TAYLOR, Jerry Andrew , WHITEHEAD, Brent , XIONG, Yusheng
IPC分类号： A01N43/42
CPC分类号： C07D471/04 , A61K31/437 , C07D487/04
摘要： This invention relates to imidazopyridyl compounds of the structural formula: I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.
摘要翻译：本发明涉及结构式为I或其药学上可接受的盐的咪唑并吡啶基化合物，其中该变量在本文中定义。本发明化合物选择性地抑制醛固酮合酶。本发明还提供包含式I化合物或其盐的药物组合物，以及潜在的治疗，改善或预防可通过抑制醛固酮合酶治疗的病症的方法。

34. 发明申请

WO2012151114A1 DIAZENIUMDIOLATE CYCLOHEXYL DERIVATIVES 审中-公开
标题翻译：二氮杂环丁烷衍生物
公开(公告)号：WO2012151114A1
公开(公告)日：2012-11-08
申请号：PCT/US2012/035318
申请日：2012-04-27
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , LO, Michael, Man-Chu , YAN, Lin
发明人： ALI, Amjad , LO, Michael, Man-Chu , YAN, Lin
IPC分类号： A01N33/24 , A61K31/15 , C07C243/00
CPC分类号： C07C247/06 , C07B2200/07 , C07C245/24 , C07C291/08 , C07C2601/14 , C07D231/12 , C07D249/04 , C07D317/72
摘要： The present invention includes diazeniumdiolate cyclohexyl derivatives, such as a compound having the structure of formula (I) wherein R 1 -R 13 are as defined herein, including various pharmaceutically acceptable salts and hydrates thereof, and pharmaceutical formulations comprising the diazeniumdiolate cyclohexyl derivatives. The invention also includes a method for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy, comprising administering a compounds of the invention to a patient having such a condition, or being at risk to having such condition.
摘要翻译：本发明包括二氮烯二硫酸酯环己基衍生物，例如具有式（I）结构的化合物，其中R 1 -R 13如本文所定义，包括其各种药学上可接受的盐和水合物，以及包含二氮烯二硫酸环己基衍生物的药物制剂。本发明还包括治疗高血压，肺动脉高压（PAH），充血性心力衰竭，过度保水，心血管疾病，糖尿病，氧化应激，内皮功能障碍，肝硬化，先兆子痫，骨质疏松症或肾病的病症的方法，包括将具有这种病症或有风险患有这种病症的患者给予本发明的化合物。

35. 发明申请

WO2012148808A1 ALDOSTERONE SYNTHASE INHIBITORS 审中-公开
公开(公告)号：WO2012148808A1
公开(公告)日：2012-11-01
申请号：PCT/US2012/034417
申请日：2012-04-20
申请人： MERCK SHARP & DOHME CORP. , ElexoPharm GmbH , HOYT, Scott, B. , PETRILLI, Whitney Lane , LONDON, Clare , XIONG, Yusheng , TAYLOR, Jerry Andrew , ALI, Amjad , LO, Michael , HENDERSON, Timothy, J. , HU, Qingzhong , HARTMANN, Rolf , YIN, Lina , HEIM, Ralf , BEY, Emmanuel , SAXENA, Rohit , SAMANTA, Swapan Kumar , KULKARNI, Bheemashankar, A.
发明人： HOYT, Scott, B. , PETRILLI, Whitney Lane , LONDON, Clare , XIONG, Yusheng , TAYLOR, Jerry Andrew , ALI, Amjad , LO, Michael , HENDERSON, Timothy, J. , HU, Qingzhong , HARTMANN, Rolf , YIN, Lina , HEIM, Ralf , BEY, Emmanuel , SAXENA, Rohit , SAMANTA, Swapan Kumar , KULKARNI, Bheemashankar, A.
IPC分类号： A01N43/64 , A61K31/41
CPC分类号： C07D487/04 , A61K31/41 , A61K45/06 , C07D471/04 , C07D519/00 , A61K2300/00
摘要： This invention relates to tricyclic triazole analogues of the formula I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthetase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthetase.
摘要翻译：本发明涉及式I的三环三唑类似物或其药学上可接受的盐，其中该变量在本文中定义。本发明化合物选择性地抑制醛固酮合成酶。本发明还提供包含式I化合物或其盐的药物组合物，以及用于治疗，改善或预防可通过抑制醛固酮合成酶治疗的病症的方法。

36. 发明申请

WO2013151876A1 ALDOSTERONE SYNTHASE INHIBITORS 审中-公开
公开(公告)号：WO2013151876A1
公开(公告)日：2013-10-10
申请号：PCT/US2013/034517
申请日：2013-03-29
申请人： MERCK SHARP & DOHME CORP. , ELEXOPHARM GMBH , ALI, Amjad , BEY, Emmanuel , HARTMANN, Rolf , HU, Qungzhong , YIN, Lina
发明人： ALI, Amjad , BEY, Emmanuel , HARTMANN, Rolf , HU, Qungzhong , YIN, Lina
IPC分类号： A01N43/64 , A61K31/41
CPC分类号： A61K31/4745 , A61K45/06 , C07D471/04
摘要： This invention relates to tricyclic triazole compounds or their pharmaceutically acceptable salts. The inventive compounds selectively inhibit aldosterone synthetase. This invention also provides for pharmaceutical compositions comprising the above-cited compounds or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthetase.
摘要翻译：本发明涉及三环三唑化合物或其药学上可接受的盐。本发明化合物选择性地抑制醛固酮合成酶。本发明还提供了包含上述化合物或其盐的药物组合物，以及潜在地用于治疗，改善或预防可通过抑制醛固酮合成酶治疗的病症的方法。

37. 发明申请

WO2011043914A1 DIURETICS 审中-公开
标题翻译：利尿剂
公开(公告)号：WO2011043914A1
公开(公告)日：2011-04-14
申请号：PCT/US2010/049425
申请日：2010-09-20
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , LO, Michael, Man-Chu , YAN, Lin
发明人： ALI, Amjad , LO, Michael, Man-Chu , YAN, Lin
IPC分类号： A61K31/535
CPC分类号： C07D491/04
摘要： A compound having the structure formula (I) or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
摘要翻译：具有结构式（I）的化合物或其药学上可接受的盐，以及使用该化合物治疗高血压的方法。

38. 发明申请

WO2012154518A1 BIPYRIDYLAMINOPYRIDINES AS SYK INHIBITORS 审中-公开
标题翻译： BIPYRIDYLAMINOPYRIDINES作为SYK抑制剂
公开(公告)号：WO2012154518A1
公开(公告)日：2012-11-15
申请号：PCT/US2012/036419
申请日：2012-05-04
申请人： MERCK SHARP & DOHME CORP. , MERCK CANADA INC. , DESCHENES, Denis , ALTMAN, Michael, D. , ELLIS, John Michael , FISCHER, Christian , HAIDLE, Andrew, M. , KATTAR, Solomon, D. , NORTHRUP, Alan, B. , SCHELL, Adam, J. , SMITH, Graham, F. , TAOKA, Brandon, M. , BIENSTOCK, Corey , DI FRANCESCO, Maria Emilia , DONOFRIO, Anthony , PETERSON, Scott , SPENCER, Kerrie, B. , JEWELL, James Patrick , ALI, Amjad , BENNETT, David Jonathan , DANG, Qun , WAI, John
发明人： DESCHENES, Denis , ALTMAN, Michael, D. , ELLIS, John Michael , FISCHER, Christian , HAIDLE, Andrew, M. , KATTAR, Solomon, D. , NORTHRUP, Alan, B. , SCHELL, Adam, J. , SMITH, Graham, F. , TAOKA, Brandon, M. , BIENSTOCK, Corey , DI FRANCESCO, Maria Emilia , DONOFRIO, Anthony , PETERSON, Scott , SPENCER, Kerrie, B. , JEWELL, James Patrick , ALI, Amjad , BENNETT, David Jonathan , DANG, Qun , WAI, John
IPC分类号： A01N43/40 , A61K31/44 , C07D213/04
CPC分类号： C07D401/14 , C07D401/12 , C07D409/14 , C07D417/14 , C07D471/04
摘要： The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, or are prodrugs thereof, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis and cancer.
摘要翻译：本发明提供了式I的新型嘧啶胺，其是脾脏酪氨酸激酶的有效抑制剂，或其前药，并且可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD和类风湿性关节炎和癌症。

39. 发明申请

WO2012122077A1 PRIMARY AMINE DIAZENIUMDIOLATE HETEROCYCLIC DERIVATIVES 审中-公开
标题翻译：主要的氨基二氮杂环戊烷杂环衍生物
公开(公告)号：WO2012122077A1
公开(公告)日：2012-09-13
申请号：PCT/US2012/027658
申请日：2012-03-05
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , LO, Michael Man-Chu , WHITEHEAD, Brent , SHAH, Shrenik, K. , HENDERSON, Timothy, J. , YAN, Lin , GUO, Zhiqiang
发明人： ALI, Amjad , LO, Michael Man-Chu , WHITEHEAD, Brent , SHAH, Shrenik, K. , HENDERSON, Timothy, J. , YAN, Lin , GUO, Zhiqiang
IPC分类号： C07D207/12 , C07D207/48 , C07D211/46 , C07D211/96 , C07D223/08 , C07D309/12 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/12 , C07D207/273 , A61K31/445
CPC分类号： C07D211/46 , C07D207/12 , C07D207/273 , C07D207/48 , C07D211/96 , C07D223/08 , C07D309/12 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/12
摘要： A compound having the structure (I) useful for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy.
摘要翻译：具有用于治疗高血压，肺动脉高压（PAH），充血性心力衰竭，由过度保水引起的病症，心血管疾病，糖尿病，氧化应激，内皮功能障碍，肝硬化，先兆子痫，骨质疏松或骨质疏松症的化合物肾病。

40. 发明申请

WO2011100384A1 DIAZENIUMDIOLATE CYCLOPENTYL DERIVATIVES 审中-公开
标题翻译：二氮杂环戊烷衍生物
公开(公告)号：WO2011100384A1
公开(公告)日：2011-08-18
申请号：PCT/US2011/024275
申请日：2011-02-10
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , LO, Michael Man-Chu , METZGER, Edward , YAN, Lin
发明人： ALI, Amjad , LO, Michael Man-Chu , METZGER, Edward , YAN, Lin
IPC分类号： A01N51/00
CPC分类号： C07C291/00 , C07C291/08 , C07C2601/08 , C07D249/04
摘要： A compound having the structure or a pharmaceutically acceptable salt thereof, wherein R 1 is hydrogen, -OH, -O-C 1 - 6 alkyl, =O, or halogen;R 2 is hydrogen, C(O)OR 8 , C 6 H 5 C(O)OR 8 , (CH 2 ) 1-2 OH, CR 9 R 10 OH, C(O)O(CH 2 ) 0-2 aryl, C(O)NR 9 R 10 , C(O)SO 2 NR 9 R 10 , C 6 H 5 OR 9 , W-C(O)OR 8 , W-OR 9 , Y, or P(O)(OR 9 )(ORlO); R 3 is hydrogen or -C 1-6 alkyl; R 4 is hydrogen, -OH or -C(O)OR 9 ; R 5 is hydrogen or deuterium; R 6 and R 7 are independently-C 1-6 alkyl, fluoro-substituted -C 1-6 alkyl, deutero-substituted -C 1-6 alkyl or -(CH 2 ) 1-2 R 11 , wherein any carbon atom of the fluoro-substituted -C 1-6 alkyl is mono- or di-substituted with fluoro, and any carbon atom of the deutero-substituted -C 1-6 alkyl is mono- or di-substituted with fluoro; R 8 , in each instance in which it occurs, is independently hydrogen, -C 1-6 alkyl, or -(CH 2 ) 2 N + (CH 3 ) 3 ; R 9 and R 10 , in each instance in which they occur, are independently -C 1-6 alkyl; R 11 is -OH, -O-C 1-6 alkyl, -0CD3, -OC(O)OC 1-6 alkyl, -NH 2 , -C 6 H 5 , -N 3 , or W; W is an unsubslituted 5- or 6-raembered heteroaryl ring having 1, 2, or 3 nitrogen atoms, or a substituted 5- or 6-membered heteroaryl ring having 1, 2, or 3 nitrogen atoms that is mono- or di-substituted at any carbon atom with R 6 or R 7 ; Y is a 5- or 6-membered heterocyclic ring having 1, 2, 3 or 4 heteroatoms which are N, O or S or stereoisomers thereof, or pharmaceutically acceptable salts thereof, or pharmaceutically acceptable salts of stereoisomers thereof, and methods of using the compounds for treating hypertension.
摘要翻译：具有结构或其药学上可接受的盐的化合物，其中R 1是氢，-OH，-O-C 1-6烷基，= O或卤素; R 2是氢，C（O）OR 8，C 6 H 5 C（O）OR 8，（O）OR 2，C（O）O（CH 2）0-2芳基，C（O）NR 9 R 10，C（O）SO 2 NR 9 R 10，C 6 H 5 OR 9，WC（O）OR 8，W-OR 9，Y或P （O）（OR 9）（ORlO）; R3是氢或-C 1-6烷基; R4是氢，-OH或-C（O）OR9; R5是氢或氘; R 6和R 7独立地是C 1-6烷基，氟取代的C 1-6烷基，取代的C 1-6烷基或 - （CH 2）1-2 R 11，其中氟取代的-C 1-6的任何碳原子烷基被氟单取代或二取代，并且取代的C 1-6烷基的任何碳原子被氟单取代或二取代; 在其每次发生的情况下，R 8独立地为氢，-C 1-6烷基或 - （CH 2）2 N +（CH 3）3; 在其各自出现的情况下，R 9和R 10独立地为-C 1-6烷基; R 11是-OH，-O-C 1-6烷基，-CD 3，-OC（O）OC 1-6烷基，-NH 2，-C 6 H 5，-N 3或W; W是具有1,2或3个氮原子的未取代的5-或6-元杂芳基环，或具有1,2或3个氮原子的取代的5-或6-元杂芳基环，其被单取代或二取代在任何具有R6或R7的碳原子上; Y是具有1,2,3或4个杂原子的5或6元杂环，其为N，O或S或其立体异构体，或其药学上可接受的盐，或其立体异构体的药学上可接受的盐，以及使用用于治疗高血压的化合物。

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