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:
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:
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。
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。
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。
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:
Certain novel substituted diazepine sulfonamides are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.
摘要:
Certain novel substituted diazepine sulfonamides are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.
摘要:
Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
摘要:
Certain novel substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment and control of obesity, diabetes, and sexual dysfunction, including erectile dysfunction and female sexual dysfunction.