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公开(公告)号:US20120238608A1
公开(公告)日:2012-09-20
申请号:US13483213
申请日:2012-05-30
申请人: Amjad Ali , Michael Man-chu Lo , Iyassu K. Sebhat , Chris Franklin , Nicoletta Almirante , Silvia Stefanini , Stefano Biondi , Ennio Ongini
发明人: Amjad Ali , Michael Man-chu Lo , Iyassu K. Sebhat , Chris Franklin , Nicoletta Almirante , Silvia Stefanini , Stefano Biondi , Ennio Ongini
IPC分类号: A61K31/4178 , A61P9/12 , C07D493/04
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-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。
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公开(公告)号:US20110065765A1
公开(公告)日:2011-03-17
申请号:US12992300
申请日:2009-05-06
申请人: Amjad Ali , Michael Man-chu Lo , Iyassu K. Sebhat , Chris Franklin , Nicoletta Almirante , Silvia Stefanini , Stefano Biondi , Ennio Ongini
发明人: Amjad Ali , Michael Man-chu Lo , Iyassu K. Sebhat , Chris Franklin , Nicoletta Almirante , Silvia Stefanini , Stefano Biondi , Ennio Ongini
IPC分类号: A61K31/41 , C07D403/14 , A61P9/12
CPC分类号: C07D403/10 , C07D235/20 , C07D257/04 , C07D409/06 , C07D493/04
摘要: A compound having the structure R—Y 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: 具有结构R-Y的化合物,其中R为例如Y选自1)R 5,R 2,R 2,R 2,R 3,R 3,R 3, R1R2)-O-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)(OR6)-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。
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公开(公告)号:US20110052674A1
公开(公告)日:2011-03-03
申请号:US12866688
申请日:2009-02-19
申请人: Nicoletta Almirante , Alessia Nicotra , Valentino Mandelli , Stefano Biondi , Silvia Stefanini , Iyassu K. Sebhat , Michael Man-Chu Lo
发明人: Nicoletta Almirante , Alessia Nicotra , Valentino Mandelli , Stefano Biondi , Silvia Stefanini , Iyassu K. Sebhat , Michael Man-Chu Lo
IPC分类号: A61K9/127 , C07D403/10 , A61K31/41 , C07D403/14 , C07D471/04 , A61K31/519 , C07D257/04 , A61K31/4184 , C07D409/06 , A61K31/4178 , A61K9/12 , A61K9/28 , A61K9/48 , A61P9/00 , A61P13/12 , A61P27/06 , A61P25/00
CPC分类号: C07D403/10 , C07D403/14 , C07D405/14
摘要: New angiotensin II receptor blocker nitroderivatives of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof: and their use for treating cardiovascular, renal and chronic liver diseases, inflammatory processes and metabolic syndromes.
摘要翻译: 通式(I)的新型血管紧张素II受体阻断剂硝基衍生物及其药学上可接受的盐或立体异构体及其用于治疗心血管,肾脏和慢性肝脏疾病,炎症过程和代谢综合征的用途。
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公开(公告)号:US08207208B2
公开(公告)日:2012-06-26
申请号:US12992300
申请日:2009-05-06
申请人: Amjad Ali , Michael Man-chu Lo , Iyassu K. Sebhat , Chris Franklin , Nicoletta Almirante , Silvia Stefanini , Stefano Biondi , Ennio Ongini
发明人: Amjad Ali , Michael Man-chu Lo , Iyassu K. Sebhat , Chris Franklin , Nicoletta Almirante , Silvia Stefanini , Stefano Biondi , Ennio Ongini
IPC分类号: A61K31/41 , A61K31/405 , C07D209/00 , C07D257/04
CPC分类号: C07D403/10 , C07D235/20 , C07D257/04 , C07D409/06 , C07D493/04
摘要: A compound having the structure R—Y 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: 具有结构R-Y的化合物,其中R为例如Y选自1)R 5,R 2,R 2,R 2,R 3,R 3,R 3, R1R2)-O-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)(OR6)-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。
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公开(公告)号:US20110077279A1
公开(公告)日:2011-03-31
申请号:US12995640
申请日:2009-05-18
IPC分类号: A61K31/4184 , C07D493/04 , A61P9/12
CPC分类号: C07D493/04 , C07D403/10
摘要: A compound having the structure wherein R is an angiotensin II receptor antagonist selected from the group consisting of (IIa)-(IIh); A is wherein R1 and R2 are independently selected from the group consisting of hydrogen and C1-4 alkyl. Y is X0—Z wherein X0 is selected from the group consisting of: —O—, —O—CO—, —OCOO—, —OCONH— and —OSO2—; Z is a nitric oxide releasing moiety, or a pharmaceutically acceptable salt thereof.
摘要翻译: 具有以下结构的化合物,其中R是选自(IIa) - (IIh)的血管紧张素II受体拮抗剂; A是其中R 1和R 2独立地选自氢和C 1-4烷基。 Y是X0-Z,其中X0选自:-O - , - O-CO-,-OCOO-,-OCONH-和-OSO 2 - ; Z是一氧化氮释放部分或其药学上可接受的盐。
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公开(公告)号:US20100311800A1
公开(公告)日:2010-12-09
申请号:US12867050
申请日:2009-02-19
申请人: Nicoletta Almirante , Alessia Nicotra , Silvia Stefanini , Stefano Biondi , Ennio Ongini , Amjad Ali , Michael Man-chu Lo
发明人: Nicoletta Almirante , Alessia Nicotra , Silvia Stefanini , Stefano Biondi , Ennio Ongini , Amjad Ali , Michael Man-chu Lo
IPC分类号: A61K31/41 , C07D257/04 , A61P9/12
CPC分类号: C07D257/04 , C07D403/10 , C07D409/06
摘要: The present invention relates to nitrooxyderivatives of angiotensin II receptor antagonists.
摘要翻译: 本发明涉及血管紧张素II受体拮抗剂的硝基氧基衍生物。
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公开(公告)号:US20100273845A1
公开(公告)日:2010-10-28
申请号:US12743402
申请日:2008-11-21
申请人: Amjad Ali , Michael Man-Chu Lo , Chris Franklin , Nicoletta Almirante , Silvia Stefanini , Laura Storoni , Stefano Biondi , Ennio Ongini
发明人: Amjad Ali , Michael Man-Chu Lo , Chris Franklin , Nicoletta Almirante , Silvia Stefanini , Laura Storoni , Stefano Biondi , Ennio Ongini
IPC分类号: A61K31/4184 , C07D403/10 , A61P9/12 , A61K31/4178
CPC分类号: C07D403/10
摘要: A compound having the structure wherein R is an angiotensin receptor antagonist active group, and Y is 1) —(CH2)3R5, 2) —C(O)(CH2)2R5, 3) —C(R1R2)OC(O)O(CH2)nR5, wherein n is 1 or 2, 4) —C(R1R2)OC(O)CH2CH2R5, 5) —C(R1R2)OC(O)OCH2CH2C(R3R4)R5, provided that when Y is —C(O)(CH2)2R5, then R is R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is —CH(ONO2)CH(ONO2)R6; R6 is selected from CH3, CH2CH3 and CH(CH3)2; 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,其中n为1或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) O)(CH 2)2 R 5,则R 1是R 1,R 2,R 3和R 4独立地选自氢和C 1-4烷基; R5是-CH(ONO2)CH(ONO2)R6; R 6选自CH 3,CH 2 CH 3和CH(CH 3)2; 或其药学上可接受的盐或水合物,其可用于治疗高血压。
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公开(公告)号:US20100249189A1
公开(公告)日:2010-09-30
申请号:US12744168
申请日:2009-01-15
IPC分类号: A61K31/34 , C07D493/04 , A61K31/4525 , A61P29/00 , A61P9/00 , A61P3/10 , A61P9/12 , A61P1/00 , A61P27/02 , A61P27/06 , A61P31/00 , A61P21/00 , A61P7/02 , A61P11/00 , A61P25/00 , A61P35/00
CPC分类号: C07D493/04
摘要: The invention relates to nitric oxide donors of the formula (I) and pharmaceutically acceptable salts or stereoisomers thereof: wherein A and A′ are independently selected from the group consisting of H and —(X)S—Y with the proviso that at least one of A or A′ is not H; wherein s is 0 or 1; X is selected from the group consisting of: —CO—, —COO—, —CONH— and —SO2— or Y is straight or branched C1-C20 alkyl chain, preferably C1-C10 alkyl chain, substituted with one or two —ONO2; or C1-C6 alkylenoxy-C1-C5 alkyl wherein the alkyl group is substituted by one or two —ONO2 groups. The invention also provides novel compositions comprising at least one compound of the invention and at least one therapeutic agent.
摘要翻译: 本发明涉及式(I)的一氧化氮供体及其药学上可接受的盐或立体异构体:其中A和A'独立地选自H和 - (X)S-Y,条件是至少一个 A或A'不是H; 其中s为0或1; X选自:-CO - , - COO - , - CONH-和-SO 2 - ,或Y是被一个或两个-ONO 2取代的直链或支链C 1 -C 20烷基链,优选C 1 -C 10烷基链 ; 或其中烷基被一个或两个-ONO 2基团取代的C 1 -C 6亚烷基氧基-C 1 -C 5烷基。 本发明还提供包含至少一种本发明化合物和至少一种治疗剂的新型组合物。
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公开(公告)号:US20080194660A1
公开(公告)日:2008-08-14
申请号:US12000247
申请日:2007-12-11
申请人: Iyassu K. Sebhat , Michael Man-chu Lo , Ravi P. Nargund , Amjad Ali , Chris Franklin , Nicoletta Almirante , Laura Storoni , Silvia Stefanini
发明人: Iyassu K. Sebhat , Michael Man-chu Lo , Ravi P. Nargund , Amjad Ali , Chris Franklin , Nicoletta Almirante , Laura Storoni , Silvia Stefanini
IPC分类号: A61K31/41 , C07D257/04 , A61P9/12
CPC分类号: C07D403/10
摘要: A compound having the structure 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 —OC(O)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: 具有其中R是血管紧张素受体拮抗剂活性基团的结构的化合物,Y是-Y 1 -Y 2 -Y 3 -Y 3, SUP> 4 u> u> u> 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-OC(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; (CH 2)2 - (X)0-1 - (CH 3) 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或水合物,其可用于治疗高血压。
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公开(公告)号:US08003811B2
公开(公告)日:2011-08-23
申请号:US12744168
申请日:2009-01-15
申请人: Nicoletta Almirante , Silvia Stefanini , Laura Storoni , Fabio Nicoli , Julio Lazaro Padron , Stefano Biondi
发明人: Nicoletta Almirante , Silvia Stefanini , Laura Storoni , Fabio Nicoli , Julio Lazaro Padron , Stefano Biondi
IPC分类号: C07D493/00 , A61K31/45
CPC分类号: C07D493/04
摘要: The invention relates to nitric oxide donors of the formula (I) and pharmaceutically acceptable salts or stereoisomers thereof: wherein A and A′ are independently selected from the group consisting of H and —(X)s—Y with the proviso that at least one of A or A′ is not H; wherein s is 0 or 1; X is selected from the group consisting of: —CO—, —COO—, —CONH— and —SO2— or Y is straight or branched C1-C20 alkyl chain, preferably C1-C10 alkyl chain, substituted with one or two —ONO2; or C1-C6 alkylenoxy-C1-C5 alkyl wherein the alkyl group is substituted by one or two —ONO2 groups. The invention also provides novel compositions comprising at least one compound of the invention and at least one therapeutic agent.
摘要翻译: 本发明涉及式(I)的一氧化氮供体及其药学上可接受的盐或立体异构体:其中A和A'独立地选自H和 - (X)s-Y,条件是至少一个 A或A'不是H; 其中s为0或1; X选自:-CO - , - COO - , - CONH-和-SO 2 - ,或Y是被一个或两个-ONO 2取代的直链或支链C 1 -C 20烷基链,优选C 1 -C 10烷基链 ; 或其中烷基被一个或两个-ONO 2基团取代的C 1 -C 6亚烷基氧基-C 1 -C 5烷基。 本发明还提供包含至少一种本发明化合物和至少一种治疗剂的新型组合物。
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