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公开(公告)号:US20100152258A1
公开(公告)日:2010-06-17
申请号:US12312225
申请日:2007-12-11
IPC分类号: A61K31/4178 , C07D403/10 , A61P9/12
CPC分类号: C07D209/10 , C07C65/21 , C07C215/82 , C07C217/92 , C07D209/12 , C07D307/80 , C07D319/18 , C07D401/06 , C07D403/10 , C07D405/04 , C07D409/04
摘要: A compound having the structure (Formula I), wherein Y is —Y1, —Y2, —Y3, —Y4, —Y5; Y1 is C(O) or C(R1R2); Y2 is O, C(O), P(O)(OH) or CH2, provided that when Y1 is C(O), Y2 is not C(O); R1 is selected from the group consisting of hydrogen and C1-4 alkyl; R2 is selected from the pup consisting of hydrogen, C1-4 alkyl, and —OC(O)C1-4 alkyl; Y3 is O, C(O) or CH2, provided that when Y2 is C(O), then Y3 is not C(O), and further provided that when Y2 is O, then Y3 is not O; Y4 is O or CH2 or is absent, provided that when Y3 is O, then Y4 is not O; 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 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-Y1,-Y2,-Y3,-Y4,-Y5; Y1是C(O)或C(R1R2); Y2是O,C(O),P(O)(OH)或CH2,条件是当Y1是C(O)时,Y2不是C(O); R 1选自氢和C 1-4烷基; R2选自由氢,C 1-4烷基和-OC(O)C 1-4烷基组成的小鼠; Y3为O,C(O)或CH2,条件是当Y2为C(O)时,Y3不为C(O),进一步规定,当Y2为O时,Y3不为O; Y4为O或CH2或不存在,条件是当Y 3为O时,Y 4不为O; 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,其可用于治疗高血压。
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公开(公告)号:US08293777B2
公开(公告)日:2012-10-23
申请号:US12629419
申请日:2009-12-02
申请人: Michael Man-Chu Lo , Amjad Ali , Ravi P. Nargund
发明人: Michael Man-Chu Lo , Amjad Ali , Ravi P. Nargund
IPC分类号: A61K31/34 , A61K31/41 , C07D249/00 , C07D409/02
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—C1-6 alkyl, —O-aryl, —O-heteroaryl, —O—C3-8 cycloalkyl, —C1-6 alkyl, -aryl, -heteroaryl, and —C3-8 cycloalkyl; R2 and R3 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: 具有其中R为血管紧张素受体拮抗剂活性基团且Y为Y的结构的化合物选自R 1选自-O-C 1-6烷基,-O-芳基,-O- 杂芳基,-O-C 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。
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公开(公告)号:US07834042B2
公开(公告)日:2010-11-16
申请号:US12312225
申请日:2007-12-11
IPC分类号: A61K31/41 , C07D257/04
CPC分类号: C07D209/10 , C07C65/21 , C07C215/82 , C07C217/92 , C07D209/12 , C07D307/80 , C07D319/18 , C07D401/06 , C07D403/10 , C07D405/04 , C07D409/04
摘要: A compound having the structure (Formula I), wherein Y is —Y1—Y2—Y3—Y4—Y5—; Y1 is C(O) or C(R1R2); Y2 is O, C(O), P(O)(OH) or CH2, provided that when Y1 is C(O), Y2 is not C(O); R1 is selected from the group consisting of hydrogen and C1-4 alkyl; R2 is selected from the pup consisting of hydrogen, C1-4 alkyl, and —OC(O)C1-4 alkyl; Y3 is O, C(O) or CH2, provided that when Y2 is C(O), then Y3 is not C(O), and further provided that when Y2 is O, then Y3 is not O; Y4 is O or CH2 or is absent, provided that when Y3 is O, then Y4 is not O; 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 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-Y1-Y2-Y3-Y4-Y5-; Y1是C(O)或C(R1R2); Y2是O,C(O),P(O)(OH)或CH2,条件是当Y1是C(O)时,Y2不是C(O); R 1选自氢和C 1-4烷基; R2选自由氢,C 1-4烷基和-OC(O)C 1-4烷基组成的小鼠; Y3为O,C(O)或CH2,条件是当Y2为C(O)时,Y3不为C(O),进一步规定,当Y2为O时,Y3不为O; Y4为O或CH2或不存在,条件是当Y 3为O时,Y 4不为O; 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,其可用于治疗高血压。
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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:US07880014B2
公开(公告)日:2011-02-01
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: C07D257/00 , C07D403/00
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-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-OC(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。
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公开(公告)号:US20100152259A1
公开(公告)日:2010-06-17
申请号:US12516482
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: C07D403/10 , A61K31/4184 , A61P9/12
CPC分类号: C07D403/10
摘要: A compound having the structure (Formula I), wherein R 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为血管紧张素受体拮抗剂活性基团,Y为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。
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公开(公告)号:US20100144810A1
公开(公告)日:2010-06-10
申请号:US12629419
申请日:2009-12-02
申请人: Michael Man-Chu Lo , Amjad Ali , Ravi P. Nargund
发明人: Michael Man-Chu Lo , Amjad Ali , Ravi P. Nargund
IPC分类号: A61K31/4178 , C07D403/10 , C07D257/04 , C07D409/06 , A61K31/41 , A61K31/4184 , A61P9/12
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—C1-6 alkyl, —O-aryl, —O-heteroaryl, —O—C3-8 cycloalkyl, —C1-6 alkyl, -aryl, -heteroaryl, and —C3-8 cycloalkyl; R2 and R3 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: 具有其中R为血管紧张素受体拮抗剂活性基团且Y为Y的结构的化合物选自R 1选自-O-C 1-6烷基,-O-芳基,-O- 杂芳基,-O-C 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。
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公开(公告)号:US20100029678A1
公开(公告)日:2010-02-04
申请号:US12509698
申请日:2009-07-27
申请人: Amjad ALI , Iyassu K. Sebhat , Cristopher L. Franklin , Kathleen M. Rupprecht , Robert K. Baker , Ravi P. Nargund , Lin Yan , Pei Huo , Dong-Ming Shen , Nicoletta Almirante , Stefano Biondi , Massimiliano Ferrario , Alessia Nicotra
发明人: Amjad ALI , Iyassu K. Sebhat , Cristopher L. Franklin , Kathleen M. Rupprecht , Robert K. Baker , Ravi P. Nargund , Lin Yan , Pei Huo , Dong-Ming Shen , Nicoletta Almirante , Stefano Biondi , Massimiliano Ferrario , Alessia Nicotra
IPC分类号: A61K31/496 , C07D491/02 , A61K31/4355 , C07D241/04 , A61P9/12
CPC分类号: C07D491/04 , C07D519/00
摘要: A compound having the structure wherein X is selected from the group consisting of: a bond, —NHCH2(CH2)nCH2OC(O)—, —CH2NHC(O)CH2NHC(O)—, —CH2OC(O)—, —OCH(CH3)OC(O)—, —OCH2OC(O)—, —O—, —NR1—, —CR1R3—, —(CH2)p—, —(CH2)qNR1C(O)—, —CHR5NR2C(O)—, —(CH2)qC(O)—, —(CH2)qC(O)—, —(CH2)qC(O)NR1—, 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X选自:-NHCH 2(CH 2)n CH 2 OC(O) - , - CH 2 NHC(O)CH 2 NHC(O) - , - CH 2 OC(O) - , - OCH CH 3)OC(O) - , - OCH 2 OC(O) - , - O - , - NR 1 - ,CR 1 R 3 - , - (CH 2)p - , - (CH 2)q NR1C , - (CH2)qC(O) - , - (CH2)qC(O) - , - (CH2)qC(O)NR1-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:US08119806B2
公开(公告)日:2012-02-21
申请号:US12509698
申请日:2009-07-27
申请人: Amjad Ali , Iyassu K. Sebhat , Christopher L. Franklin , Kathleen M. Rupprecht , Robert K. Baker , Ravi P. Nargund , Lin Yan , Pei Huo , Dong-Ming Shen , Nicoletta Almirante , Stefano Biondi , Massimiliano Ferrario , Alessia Nicotra
发明人: Amjad Ali , Iyassu K. Sebhat , Christopher L. Franklin , Kathleen M. Rupprecht , Robert K. Baker , Ravi P. Nargund , Lin Yan , Pei Huo , Dong-Ming Shen , Nicoletta Almirante , Stefano Biondi , Massimiliano Ferrario , Alessia Nicotra
IPC分类号: A61K31/4355 , C07D491/048
CPC分类号: C07D491/04 , C07D519/00
摘要: A compound having the structure wherein X is selected from the group consisting of: a bond, —NHCH2(CH2)nCH2OC(O)—, —CH2NHC(O)CH2NHC(O)—, —CH2OC(O)—, —OCH(CH3)OC(O)—, —OCH2OC(O)—, —O—, —NR1—, —CR1R3—, —(CH2)p—, —(CH2)qNR1C(O)—, —CHR5NR2C(O)—, —(CH2)qC(O)—, —(CH2)qC(O)NR1—, 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X选自:-NHCH 2(CH 2)n CH 2 OC(O) - , - CH 2 NHC(O)CH 2 NHC(O) - , - CH 2 OC(O) - , - OCH CH 3)OC(O) - , - OCH 2 OC(O) - , - O - , - NR 1 - ,CR 1 R 3 - , - (CH 2)p - , - (CH 2)q NR1C , - (CH 2)q C(O) - , - (CH 2)q C(O)NR 1 - 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:US20160251407A1
公开(公告)日:2016-09-01
申请号:US15025912
申请日:2014-10-02
申请人: Songnian LIN , Lin YAN , Ahmet KEKEC , Yuping ZHU , David N. HUNTER , Pei HUO , Danqing FENG , Ravi P. NARGUND , Christopher R. MOYES , Zhiqiang ZHAO , Brenda PIPIK , Dimitri PISSARNITSKI , Joseph L. DUFFY , Erin N. GUIDRY , MERCK SHARP & DOHME CORP.
发明人: Songnian Lin , Lin Yan , Ahmet Kekec , Yuping Zhu , David N. Hunter , Pei Huo , Danqing Feng , Ravi P. Nargund , Christopher R. Moyes , Zhiqiang Zhao , Brenda Pipik , Dmitri Pissarnitski , Joseph L. Duffy , Erin Guidry
CPC分类号: A61K47/61 , A61K38/28 , A61K47/549 , A61K47/64 , C07K14/62
摘要: Insulin conjugates comprising an insulin molecule covalently attached to at least one bi-dentate linker having two arms, each arm independently attached to a ligand comprising a saccharide and wherein at least one ligand of the linker is fucose are disclosed. The insulin conjugates display a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose even when administered to a subject in need thereof in the absence of an exogenous multivalent saccharide-binding molecule such as Con A.
摘要翻译: 胰岛素缀合物包含共价连接到具有两个臂的至少一个双齿连接体的胰岛素分子,每个臂独立地连接到包含糖的配体,并且其中至少一个连接体的配体是岩藻糖。 胰岛素缀合物显示药代动力学(PK)和/或药效学(PD)谱,其对糖类如葡萄糖或α-甲基甘露糖的全身浓度有反应,即使在不存在外源多价的情况下施用于有需要的受试者时 糖结合分子如Con A.
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