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21. 发明申请

WO2012099770A2 DIAZENIUMDIOLATE DERIVATIVES 审中-公开
标题翻译： DIAZENIUMOOLOLA衍生物
公开(公告)号：WO2012099770A2
公开(公告)日：2012-07-26
申请号：PCT/US2012/021048
申请日：2012-01-12
申请人： MERCK SHARP & DOHME CORP. , 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 , C07C243/06 , A61K31/04 , A61P9/12
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：具有结构（I）的化合物，其可用于治疗高血压，肺动脉高压，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，骨质疏松症或肾病。

22. 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。

23. 发明申请

WO2009070241A2 ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
标题翻译：血管紧张素II受体拮抗剂
公开(公告)号：WO2009070241A2
公开(公告)日：2009-06-04
申请号：PCT/US2008/012984
申请日：2008-11-21
申请人： MERCK & CO., INC. , NICOX S.A. , ALI, Amjad , LO, Michael Man-Chu , FRANKLIN, Chris , ALMIRANTE, Nicoletta , STEFANINI, Silvia , STORONI, Laura , BIONDI, Stefano , ONGINI, Ennio
发明人： ALI, Amjad , LO, Michael Man-Chu , FRANKLIN, Chris , ALMIRANTE, Nicoletta , STEFANINI, Silvia , STORONI, Laura , BIONDI, Stefano , ONGINI, Ennio
IPC分类号： C07D403/10 , A61K31/41 , A61P9/12
CPC分类号： C07D403/10
摘要： A compound having the structure (A) wherein R is an angiotensin receptor antagonist active group, and Y is 1) -(CH 2 ) 3 R 5 , 2) -C(O)(CH 2 ) 2 R 5 , 3) -C(R 1 R 2 )OC(O)O(CH 2 ) n R 5 , wherein n is 1 or 2, 4) -C(R 1 R 2 )OC(O)CH 2 CH 2 R 5 , 5) -C(R 1 R 2 )OC(O)OCH 2 CH 2 C(R 3 R 4 )R 5 , Formula (B), and Formula (C) provided that when Y is -C(O)(CH 2 ) 2 R 5 , then R is Formula (D) R 1 , R 2 , R 3 and R 4 are independently selected from the group consisting of hydrogen and C 1-4 alkyl; R 5 is CH(ONO 2 )CH(ONO 2 )R 6 ; R 6 is selected from CH 3 , CH 2 CH 3 and CH(CH 3 ) 2 ; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
摘要翻译：具有结构（A）的化合物，其中R是血管紧张素受体拮抗剂活性基团，Y是1） - （CH 2）3 2）-C（O）（CH 2）2 2 R 5，3） - C（R ^{1 - [R ^{2 ）OC（O）O（CH <子> 2 ）<子>名词ř^{5 其中n是1或2，4）-C（R 1 R 2）OC（O）CH 2 CH 5）-C（R 1）R 2）OC（O）OCH 2，其中R 1，R 2，（B），（B），（B），（B），（B），和式（C）条件是当Y为-C（O）（CH 2）2 R 5时，则R为式（D ）R 1，R 2，R 3和R 4独立地选自氢和C 1-4烷基，其中R 1，R 2，R 3和R 4独立地选自氢和 C 1-4烷基; R 5 = CH（ONO 2）CH（ONO 2）R 6 = R 6选自CH 3，CH 2，CH 3和CH（CH 3）3，子>）<子> 2 ; 或其药学上可接受的盐或水合物，其可用于治疗高血压。}}}

24. 发明申请

WO2008076247A2 ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
标题翻译： ANGIOTENSIN II受体拮抗剂
公开(公告)号：WO2008076247A2
公开(公告)日：2008-06-26
申请号：PCT/US2007/025233
申请日：2007-12-11
申请人： MERCK & CO., INC. , NICOX S.A. , SEBHAT, Iyassu, K. , LO, Michael, Man-Chu , NARUGUND, Ravi, P. , ALI, Amjad , FRANKLIN, Chris , ALMIRANTE, Nicoletta , STORONI, Laura , STEFANINI, Silvia
发明人： SEBHAT, Iyassu, K. , LO, Michael, Man-Chu , NARUGUND, 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 -Y 1 -Y 2 -Y 3 -Y 4 -Y 5 .; Y 1 is C(R 1 R 2 ); 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 -0C(0)C 1-4 alkyl; Y 2 is O or CH 2 ; Y 3 is C(O) or CH 2 ; Y 4 is O or CH 2 ; Y5 is -(CH2) 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 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-Y 1 -Y 2 -Y 3， SUP> -Y ^{4 -Y ^{5 .; Y 1是C（R 1 R 2）2）。 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; Y 2是O或CH 2; Y 3是C（O）或CH 2 O 2; Y 4是O或CH 2; Y 5是 - （CH 2）n 1-2 - （X）0-1 - （CH 2）2 - SUB> - 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或水合物，其可用于治疗高血压。}}

25. 发明申请

WO2008076246A2 ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
标题翻译： ANGIOTENSIN II受体拮抗剂
公开(公告)号：WO2008076246A2
公开(公告)日：2008-06-26
申请号：PCT/US2007/025232
申请日：2007-12-11
申请人： MERCK & CO., INC. , NICOX S.A. , 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 -Y 1 -Y 2 -Y 3 -Y 4 -Y 5 .; Y 1 is C(R 1 R 2 ); 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 -0C(0)C 1- 4 alkyl; Y 2 is O or CH 2 ; Y 3 is C(O) or CH 2 ; Y 4 is O or CH 2 ; Y5 is -(CH2) 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 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-Y 1 -Y 2 -Y 3， SUP> -Y ^{4 -Y ^{5 .; Y 1是C（R 1 R 2）2）。 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 -}}

26. 发明申请

WO2008076245A2 ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
标题翻译： ANGIOTENSIN II受体拮抗剂
公开(公告)号：WO2008076245A2
公开(公告)日：2008-06-26
申请号：PCT/US2007/025231
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。}

27. 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。

28. 发明申请

WO2009140111A1 ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
标题翻译： ANGIOTENSIN II受体拮抗剂
公开(公告)号：WO2009140111A1
公开(公告)日：2009-11-19
申请号：PCT/US2009/042951
申请日：2009-05-06
申请人： MERCK & CO., INC. , NICOX S.A. , ALI, Amjad , LO, Michael, Man-chu , SEBHAT, Iyassu, K. , FRANKLIN, Chris , ALMIRANTE, Nicoletta , STEFANINI, Silvia , BIONDI, Stefano , ONGINI, Ennio
发明人： ALI, Amjad , LO, Michael, Man-chu , SEBHAT, Iyassu, K. , FRANKLIN, Chris , ALMIRANTE, Nicoletta , STEFANINI, Silvia , BIONDI, Stefano , ONGINI, Ennio
IPC分类号： A01N43/40 , A01N43/50 , A61K31/445
CPC分类号： C07D403/10 , C07D235/20 , C07D257/04 , C07D409/06 , C07D493/04
摘要： A compound having the structure wherein R is, for example, Y is selected from the group consisting of 1) R5, 2) -C(R1R2)(C(R3R4))0-1Y1R5, and 3) -C(R1R2)-O-Y1R5; R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is; Y1 is selected from the group consisting of C(O)-O- and P(O)(OR6)-O-; and R6 is hydrogen or CH3, or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
摘要翻译：具有其中R为例如Y的结构的化合物选自1）R5，2）-C（R1R2）（C（R3R4））0-1Y1R5和3）-C（R1R2） - O型Y1R5; R 1，R 2，R 3和R 4独立地选自氢和C 1-4烷基; R5是 Y1选自C（O）-O-和P（O）（OR 6）-O-; R6为氢或CH3，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。

29. 发明申请

WO2009106470A2 ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
标题翻译： ANGIOTENSIN II受体拮抗剂
公开(公告)号：WO2009106470A2
公开(公告)日：2009-09-03
申请号：PCT/EP2009/051942
申请日：2009-02-19
申请人： NICOX S.A. , MERCK & CO. INC. , ALMIRANTE, Nicoletta , NICOTRA, Alessia , STEFANINI, Silvia , BIONDI, Stefano , ONGINI, Ennio , ALI, Amjad , LO, Michael Man-chu
发明人： ALMIRANTE, Nicoletta , NICOTRA, Alessia , STEFANINI, Silvia , BIONDI, Stefano , ONGINI, Ennio , ALI, Amjad , LO, Michael Man-chu
IPC分类号： C07D257/04 , C07D403/10 , C07D409/06 , A61P9/12
CPC分类号： C07D257/04 , C07D403/10 , C07D409/06
摘要： The present invention relates to nitrooxyderivatives of angiotensin II receptor antagonist having the general formula (I): where in R is selected f rom the group consisting of (IIa) - (IIk): when R is selected from (Ilk), Y is selected from the group consisting of: 1) -C(O) (CH 2 ) n R 5 ; 2) -C(O)(CH 2 n -O-CH 2 -R 5 ; 3) -C(O)-R 6 wherein R 6 is the following group: when R is selected from (IIa)-(IIh), Y is selected from the group consisting of: 4) -C(R 1 R 2 )OC(O)-(CH 2 ) n R 5 ; 5) -C(R 1 R 2 )OC(O)O-(CH 2 ) n R 5 ; 6) C(R 1 R 2 )OC(O)(CH 2 ) n -O-CH 2 -R 5 ; 7) C(R 1 R 2 )OC(O)O(CH 2 ) n -O-CH 2 -R 5 ; 8) -C(R 1 R 2 )OC(O)-R 6 wherein R 6 is as above defined; R 1 and R 2 are independently selected from the group consisting of hydrogen and C 1-4 alkyl; R 5 is -CH(ONO 2 )R 7 ; R 7 is CH 3 or C 1-4 alkyl; n is an integer from 1 to 4; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及具有通式（I）的血管紧张素II受体拮抗剂的硝基氧基衍生物：其中R选自（IIa） - （IIk）组：当R选自（IIk）时，选择Y 由以下组成：1）-C（O）（CH 2）n R 5; 2）-C（O）（CH 2 nO-CH 2 -R 5; 3）-C（O）-R 6，其中R 6是下列基团：当R选自（IIa） - （IIh）时，Y选自由以下组成：4）-C（R 1 R 2）OC（O） - （CH 2）n R 5; 5）-C（R 1 R 2）OC（O）O-（CH 2）n R 5; 6）C（R 1 R 2）OC（O）（CH 2）n -O-CH 2 -R 5; 7）C（R 1 R 2）OC（O）O（CH 2）n -O-CH 2 -R 5; 8）-C（R 1 R 2）OC（O）-R 6，其中R 6如上所定义; R 1和R 2独立地选自氢和C 1-4烷基; R5是-CH（ONO2）R7; R7是CH3或C1-4烷基; n是1至4的整数; 或其药学上可接受的盐。

30. 发明申请

WO2009099853A3 ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2009099853A3
公开(公告)日：2009-08-13
申请号：PCT/US2009/032323
申请日：2009-01-29
申请人： MERCK & CO., INC. , ALI, Amjad , LO, Michael Man-chu
发明人： ALI, Amjad , LO, Michael Man-chu
IPC分类号： A61K31/497
摘要： A compound having the structure (I) wherein R is an angiotensin receptor blocking group Y is -(CR 1 R 20 ) 1-7 R 5 , or - C(O)(CR 1 R 20 ) 1-7 R 5 ; R 1 and R 20 are independently selected from the group consisting of hydrogen or C 1-4 alkyl; R 5 is -O-N=N(O)-NR 3 R 4 ; and R 3 and R 4 are independently selected from the group consisting of CH 2 CH 2 OH, -CH 2 CH 2 OCH 3 , -C 1-4 alkyl, unsubstituted or substituted C 1-6 alkenyl, unsubstituted or substituted morpholino, amino, unsubstituted or substituted benzyl, unsubstituted or substituted phenyl, unsubstituted or substituted arylC 1-4 alkyl, or R 3 and R 4 together with the nitrogen atom to which they are attached, form a ring selected from the group consisting of (II); or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of the stereoisomer thereof, which is useful for treating hypertension.

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