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51. 发明申请

WO2012099770A3 DIAZENIUMDIOLATE DERIVATIVES 审中-公开
标题翻译： DIAZENIUMDOLATE DERIVATIVES
公开(公告)号：WO2012099770A3
公开(公告)日：2012-11-15
申请号：PCT/US2012021048
申请日：2012-01-12
申请人： MERCK SHARP & DOHME , ALI AMJAD , LO MICHAEL MAN-CHU , METZGER EDWARD , SHAH SHRENIK K , DELLUREFICIO JAMES
发明人： ALI AMJAD , LO MICHAEL MAN-CHU , METZGER EDWARD , SHAH SHRENIK K , DELLUREFICIO JAMES
IPC分类号： C07C245/04 , A61K31/04 , A61P9/12 , C07C243/06
CPC分类号： C07C291/02 , A61K45/06 , C07C291/08
摘要： A compound having the structure (I) useful for treating hypertension, pulmonary arterial hypertension, 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，充血性心力衰竭，由过度保水，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，骨质疏松症或肾病引起的病症的结构（I）的化合物。

52. 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。

53. 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。

54. 发明申请

WO2011053519A1 DIURETICS 审中-公开
标题翻译：利尿剂
公开(公告)号：WO2011053519A1
公开(公告)日：2011-05-05
申请号：PCT/US2010/053680
申请日：2010-10-22
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , NARGUND, Ravi , LO, Michael Man-Chu , YAN, Lin , HUO, Pei , FRANKLIN, Christopher
发明人： ALI, Amjad , NARGUND, Ravi , LO, Michael Man-Chu , YAN, Lin , HUO, Pei , FRANKLIN, Christopher
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： C07D491/048
摘要： A compound having the structure (I) wherein R is selected from the group consisting of 1) and 2), or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
摘要翻译：具有结构（I）的化合物，其中R选自1）和2）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。

55. 发明申请

WO2010065432A1 NITROOXY DERIVATIVES AS ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
标题翻译： NITROOXY衍生物作为血管紧张素II受体拮抗剂
公开(公告)号：WO2010065432A1
公开(公告)日：2010-06-10
申请号：PCT/US2009/066041
申请日：2009-11-30
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , LO, Michael Man-Chu , NARGUND, Ravi, P.
发明人： ALI, Amjad , LO, Michael Man-Chu , NARGUND, Ravi, P.
IPC分类号： C07D235/08 , C07D257/04 , C07D403/10 , C07D409/06 , A61K31/164 , A61K31/4178 , A61K31/4184
CPC分类号： C07D403/10 , C07D235/08 , C07D257/04 , C07D409/06
摘要： A compound having the structure wherein R is an angiotensin receptor antagonist active group, and Y is Y is selected from the group consisting of R1 is selected from the group consisting of -O-C 1-6 alkyl, -O-aryl, -O-heteroaryl, -O-C 3-8 cycloalkyl, -C 1-6 alkyl, -aryl, -heteroaryl, and -C 3-8 cycloalkyl; R 2 and R 3 are independently selected from the group consisting of hydrogen and C1-4 alkyl, or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
摘要翻译：具有结构的化合物，其中R是血管紧张素受体拮抗剂活性基团，Y是Y选自由R 1选自-OC 1-6烷基，-O-芳基，-O-杂芳基，-OC 3-8环烷基，-C 1-6烷基， - 芳基， - 杂芳基和-C 3-8环烷基; R2和R3独立地选自氢和C 1-4烷基，或其药学上可接受的盐或水合物，其可用于治疗高血压。

56. 发明申请

WO2009094242A1 ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
标题翻译： ANGIOTENSIN II受体拮抗剂
公开(公告)号：WO2009094242A1
公开(公告)日：2009-07-30
申请号：PCT/US2009/030382
申请日：2009-01-08
申请人： MERCK & CO., INC. , ALI, Amjad , FRANKLIN, Christopher , LO, Michael Man-chu , WHITEHEAD, Brent, R.
发明人： ALI, Amjad , FRANKLIN, Christopher , LO, Michael Man-chu , WHITEHEAD, Brent, R.
IPC分类号： A01N43/64 , A61K31/41 , C07D257/00
CPC分类号： C07D403/10 , C07D235/20 , C07D257/04 , C07D401/14 , C07D409/06
摘要： A compound having the structure (I) wherein R is an angiotensin receptor antagonist active group, Y is selected from the group consisting of (II), and 2) -C(R 1 H)OC(O)X((CR 12 R 13 )-(CHR 10 )m-(CH 2 )n-Zp-(CH 2 )q-(CHR 11 )r-(CR 16 R 17 ))-R 5 ; Z is O- or (CR 14 R 15 )-; m, n, p, q, and r are independently selected from the group consisting of 0 and 1; X is O- or (CR 18 R 19 )-; R 1 is selected from the group consisting of hydrogen, C 1-4 alkyl, aryl and C 1-4 alkylaryl; R 5 is -O-N=N(O)-NR 3 R 4 ; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
摘要翻译：具有结构（I）的化合物，其中R是血管紧张素受体拮抗剂活性基团，Y选自（II）和2）-C（R 1 H）OC（O）X（（CR 12 R 13） - （CHR 10））间 - （CH 2）N-ZP-（CH 2）Q - （CHR11）R-（CR 16 R 17）） - R 5; Z是O-或（CR14R15） - ; m，n，p，q和r独立地选自0和1组成的组; X为O-或（CR 18 R 19） - ; R1选自氢，C1-4烷基，芳基和C1-4烷基芳基; R5是-O-N = N（O）-NR3R4; 或其药学上可接受的盐或水合物，其可用于治疗高血压。

57. 发明申请

WO2008076246A3 NITRODERIVATIVES AS ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2008076246A3
公开(公告)日：2009-01-15
申请号：PCT/US2007025232
申请日：2007-12-11
申请人： MERCK & CO INC , NICOX SA , SEBHAT IYASSU K , LO MICHAEL MAN-CHU , NARGUND RAVI P , ALI AMJAD , FRANKLIN CHRIS , ALMIRANTE NICOLETTA , STORONI LAURA , STEFANINI SILVIA
发明人： SEBHAT IYASSU K , LO MICHAEL MAN-CHU , NARGUND RAVI P , ALI AMJAD , FRANKLIN CHRIS , ALMIRANTE NICOLETTA , STORONI LAURA , STEFANINI SILVIA
IPC分类号： C07D403/10 , A61K31/41 , A61P9/12
CPC分类号： C07D403/10
摘要： A compound having the structure (Formula I), wherein R is an angiotensin receptor antagonist active group, Y is -Y1-Y2-Y3-Y4-Y5.; Y1 is C(R1R2); R1 is selected from the group consisting of hydrogen and C1-4 alkyl; R2 is selected from the group consisting of hydrogen, C1-4 alkyl, and -0C(0)C1-4 alkyl; Y2 is O or CH2; Y3 is C(O) or CH2; Y4 is O or CH2; Y5 is -(CH2) 1-2-(X)0-1-(CH2)0-1- or is absent; X is -O- or -CR3R4-; and R3 and R4 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
摘要翻译：具有结构（式I）的化合物，其中R是血管紧张素受体拮抗剂活性基团，Y是-Y1-Y2-Y3-Y4-Y5。 Y1是C（R1R2）; R 1选自氢和C 1-4烷基; R 2选自氢，C 1-4烷基和-C（O）C 1-4烷基; Y2是O或CH2; Y 3是C（O）或CH 2; Y4是O或CH2; Y 5是 - （CH 2）1-2 - （X）0-1 - （CH 2）0-1-或不存在; X是-O-或-CR 3 R 4 - ; 并且R 3和R 4独立地选自氢和C 1 -C 4烷基; 或其药学上可接受的盐或水合物，其可用于治疗高血压。

58. 发明申请

WO2008076245A3 NITRODERIVATIVES AS ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2008076245A3
公开(公告)日：2008-09-12
申请号：PCT/US2007025231
申请日：2007-12-11
申请人： MERCK & CO INC , SEBHAT IYASSU K , LO MICHAEL MAN-CHU , NARGUND RAVI P , ALI AMJAD
发明人： SEBHAT IYASSU K , LO MICHAEL MAN-CHU , NARGUND RAVI P , ALI AMJAD
IPC分类号： C07D403/10 , A61K31/41 , A61P9/12
CPC分类号： C07D403/10
摘要： A compound having the structure (Formula I), wherein Y is -Y 1 -Y 2 -Y 3 -Y 4 -Y 5 -; Y 1 is C(O) or C(R 1 R 2 ); Y 2 is O, C(O), P(O)(OH) or CH 2 , provided that when Y 1 is C(O), Y 2 is not C(O); R 1 is selected from the group consisting of hydrogen and C 1-4 alkyl; R 2 is selected from the group consisting of hydrogen, C 1-4 alkyl, and -OC(O)C 1-4 alkyl; Y 3 is O, C(O) or CH 2 , provided that when Y 2 is C(O), then Y 3 is not C(O), and further provided that when Y 2 is O, then Y 3 is not O; Y 4 is O or CH 2 or is absent, provided that when Y 3 is O, then Y 4 is not O; Y5 is -(CH 2 ) 1-2 -(X) 0- l -(CH 2 ) 0-l - or is absent; X is -O- or -CR 3 R 4 -; and R 3 and R 4 are independently selected from the group consisting of hydrogen and C 1 -C 4 alkyl; or a pharmaceutically acceptable salt thereof, which is useful for treating hypertension.
摘要翻译：具有结构（式I）的化合物，其中Y为-Y 1 -Y 2 -Y 3 -Y 4 - / SUP> -Y ^{5 - ; Y 1是C（O）或C（R 1 R 2）2）。 Y 2是O，C（O），P（O）（OH）或CH 2，条件是当Y 1是C（ O），Y 2不是C（O）; R 1选自氢和C 1-4烷基; R 2选自氢，C 1-4烷基和-OC（O）C 1-4烷基; Y 3是O，C（O）或CH 2，条件是当Y 2是C（O）时，则Y 3不是C（O），并且进一步地，当Y 2为O时，Y 3不为O; Y 4是O或CH 2或不存在，条件是当Y 3为O时，则Y 4为O，不是O Y 5是 - （CH 2）2 - （X）0-1 - （CH 2）2 - 0-1 - 或不存在; X是-O-或-CR 3 R 4 - 。和R 3和R 4独立地选自氢和C 1 -C 4烷基 ; 或其药学上可接受的盐，其可用于治疗高血压。}

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