摘要:
This invention provides the compounds of formula (I): or a pharmaceutically acceptable ester or salt thereof, wherein R1 and R2 independently represent hydrogen or the like; R3 represents aryl or the like; —X—Y— represents —CH2O— or the like, and n represents 0, 1 or 2. These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.
摘要翻译:本发明提供式(I)化合物或其药学上可接受的酯或盐,其中R 1和R 2独立代表氢或类似物; R 3表示芳基等; -X-Y-表示-CH 2 O 2等,n表示0,1或2.这些化合物具有ORL1-受体拮抗剂活性; 因此,可用于治疗诸如疼痛,各种CNS疾病等疾病或病症。
摘要:
This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y1, Y2, Y3 and Y4 are independently selected from N, CH, etc.; R1 is H, C1-8 alkyl, etc.; Q1 is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 4 heteroatoms selected from O, N and S, etc.; A is a 5-6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; B is C1-6 alkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; R2 is H, C1-4 alkyl, etc.; Z is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; L is halo, C1-4 alkyl, etc.; m is 0, 1 or 2; R3 and R4 are independently selected from H and C1-4 alkyl ; R5 is H, C1-4 alkyl, etc.; Q2 is a 5-12 membered monocyclic or bicyclic aromatic ring or tricyclic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc. These compounds are useful for the treatment of medical conditions mediated by prostaglamadin such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译:本发明提供式(I)化合物或其药学上可接受的盐,其中Y 1,Y 2,Y 3和 Y 4独立地选自N,CH等; R 1是H,C 1-8烷基等; Q 1是5-12元单环或双环芳族环,任选地含有至多4个选自O,N和S的杂原子等; A是任选含有至多3个选自O,N和S的杂原子的5-6元单环芳环等; B是任选被氧代基取代的C 1-6亚烷基等; W是NH,O等; R 2是H,C 1-4烷基等; Z是任选地含有至多3个选自O,N和S的杂原子的5-12元单环或双环芳环等; L为卤素,C 1-4烷基等; m为0,1或2; R 3和R 4独立地选自H和C 1-4烷基; R 5是H,C 1-4烷基等; Q 2是5-12元单环或双环芳族环或三环,任选地含有至多3个选自O,N和S的杂原子等。这些化合物可用于治疗介导的医学病症 通过前列腺炎如疼痛,发热或炎症等。本发明还提供包含上述化合物的药物组合物。
摘要:
This invention provides the compounds of formula (I): or a pharmaceutically acceptable ester of such compound, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 independently represent a hydrogen atom or the like; R3 represents an aryl group having from 6 to 10 ring atoms or the like; X represents an oxygen atom, or the like; Y represents an oxygen atom or the like; and n represents an integer 0, 1 or 2. These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.
摘要翻译:本发明提供式(I)化合物或其药学上可接受的酯或其药学上可接受的盐,其中R 1和R 2独立地表示 氢原子等; R 3表示具有6至10个环原子等的芳基; X表示氧原子等; Y表示氧原子等; 并且n表示整数0,1或2.这些化合物具有ORL1-受体拮抗剂活性; 因此,可用于治疗诸如疼痛,各种CNS疾病等疾病或病症。
摘要:
This invention provides the compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 and R2 independently represent hydrogen or the like; R3 and R4 independently represents hydrogen or the like; R5 represents aryl or the like; —X—Y— represents —CH2O— or the like; and n represents 0, 1 or 2. These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.
摘要翻译:本发明提供式(I)化合物或其药学上可接受的盐,其中R 1和R 2独立代表氢或类似物; R 3和R 4独立地表示氢等; R 5表示芳基等; -X-Y-表示-CH 2 O-等; 并且n表示0,1或2.这些化合物具有ORL1受体拮抗剂活性; 因此,可用于治疗诸如疼痛,各种CNS疾病等疾病或病症。
摘要:
This invention provides the compounds of formula (I): or a pharmaceutically acceptable ester of such compound, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 independently represent a hydrogen atom or the like; R3 represents an aryl group having from 6 to 10 ring atoms or the like; X represents an oxygen atom, or the like; Y represents an oxygen atom or the like; and n represents an integer 0, 1 or 2. These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.
摘要翻译:本发明提供式(I)化合物或其药学上可接受的酯或其药学上可接受的盐,其中R 1和R 2独立地表示 氢原子等; R 3表示具有6至10个环原子等的芳基; X表示氧原子等; Y表示氧原子等; 并且n表示整数0,1或2.这些化合物具有ORL1-受体拮抗剂活性; 因此,可用于治疗诸如疼痛,各种CNS疾病等疾病或病症。
摘要:
This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y1, Y2, Y3 and Y4 are independently selected from N, CH, etc.; R1 is H, C1-8 alkyl, etc.; Q1 is a 5–12 membered monocyclic or bicyclic aromatic ring optionally containing up to 4 heteroatoms selected from O, N and S, etc.; A is a 5–6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; B is C1-6 alkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; R2 is H, C1-4 alkyl, etc.; Z is a 5–12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; L is halo, C1-4 alkyl, etc.; m is 0, 1 or 2; R3 and R4 are independently selected from H and C1-4 alkyl; R5 is H, C1-4 alkyl, etc.; Q2 is a 5–12 membered monocyclic or bicyclic aromatic ring or tricyclic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc. These compounds are useful for the treatment of medical conditions mediated by prostaglamndin such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译:本发明提供式(I)化合物或其药学上可接受的盐,其中Y 1,Y 2,Y 3和 Y 4独立地选自N,CH等; R 1是H,C 1-8烷基等; Q 1是5-12元单环或双环芳族环,任选地含有至多4个选自O,N和S的杂原子等; A是任选含有至多3个选自O,N和S的杂原子的5-6元单环芳环等; B是任选被氧代基取代的C 1-6亚烷基等; W是NH,O等; R 2是H,C 1-4烷基等; Z是任选地含有至多3个选自O,N和S的杂原子的5-12元单环或双环芳环等; L为卤素,C 1-4烷基等; m为0,1或2; R 3和R 4独立地选自H和C 1-4烷基; R 5是H,C 1-4烷基等; Q 2是5-12元单环或双环芳族环或三环,任选地含有至多3个选自O,N和S的杂原子等。这些化合物可用于治疗介导的医学病症 通过前列腺素如疼痛,发烧或炎症等。本发明还提供了包含上述化合物的药物组合物。
摘要:
This invention provides the compounds of formula (I): or its a pharmaceutically acceptable ester or amide of such compound, or a pharmaceutically acceptable salt thereof, wherein X1 is NH; R1, R2, R4 through R6 and R7 through R11 are all hydrogen; R3 is hydroxy; X2 and X3 are methylene; X4 is a bond; and X5 is a carbon atom, and the like. These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.
摘要翻译:本发明提供式(I)化合物或其药学上可接受的这类化合物的酯或酰胺或其药学上可接受的盐,其中X 1是NH; R 1,R 2,R 4,R 4和R 7通过R 6和R 7通过 R 11都是氢; R 3是羟基; X 2和X 3是亚甲基; X 4是一个键; 和X 5是碳原子等。 这些化合物具有ORL1受体拮抗剂活性; 因此,可用于治疗诸如疼痛,各种CNS疾病等疾病或病症。
摘要:
This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y1, Y2, Y3 and Y4 are independently selected from N, CH, etc.; R1 is H, C1-8 alkyl, etc.; Q1 is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 4 heteroatoms selected from O, N, and S, etc.; A is 5-6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected form O, N and S, etc.; B is C1-6 alkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; R2 is H, C1-4 alkyl, etc.; Z is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected form O, N and S, etc.; L is halo, C1-4 alkyl, etc.; m is 0, 1 or 2; R3 and R4 are independently selected from H and C1-4 alkyl; R5 is H, C1-4 alkyl; etc.; Q2 is a 5-12 membered monocyclic or bicyclic aromatic ring or tricyclic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc. These compounds are useful for the treatment of medical conditions mediated by prostaglamndin such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译:本发明提供式(I)化合物或其药学上可接受的盐,其中Y 1,Y 2,Y 3和Y 4独立地选自N,CH等; R 1是H,C 1-8烷基等; Q 1是任选地含有至多4个选自O,N和S的杂原子的5-12元单环或双环芳环等; A是任选含有至多3个选自O,N和S的杂原子的5-6元单环芳环等; B是任选被氧代基取代的C 1-6亚烷基等; W是NH,O等; R 2是H,C 1-4烷基等; Z是任选地含有至多3个选自O,N和S等的杂原子的5-12元单环或双环芳环; L是卤素,C 1-4烷基等; m为0,1或2; R 3和R 4独立地选自H和C 1-4烷基; R 5是H,C 1-4烷基; 等等。; Q 2是任选地含有至多3个选自O,N和S的杂原子的5-12元单环或双环芳族环或三环,这些化合物可用于治疗由前列腺素介导的医学病症如疼痛 ,发热或炎症等。本发明还提供包含上述化合物的药物组合物。
摘要:
This invention provides the compounds of formula (I): or a pharmaceutically acceptable ester of such compound, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 independently represent a hydrogen atom or the like; R3 represents a hydrogen atom, or the like; R4 represents a hydrogen atom or the like; represents one of the following or the like; R5 represents an aryl group having from 6 to 10 ring atoms or the like; X represents an oxygen atom, or the like; Y represents an oxygen atom or the like and n represents an integer 0, 1 or 2. These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.
摘要翻译:本发明提供式(I)化合物或其药学上可接受的酯或其药学上可接受的盐,其中R 1和R 2独立地表示 氢原子等; R 3表示氢原子等; R 4表示氢原子等; 代表以下之一或类似物; R 5表示具有6至10个环原子等的芳基; X表示氧原子等; Y表示氧原子等,n表示0,1或2的整数。这些化合物具有ORL1-受体拮抗剂活性; 因此,可用于治疗诸如疼痛,各种CNS疾病等疾病或病症。
摘要:
This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y1, Y2, Y3 and Y4 are independently selected from N, CH, etc.; R1 is H, C1-8 alkyl, etc.; Q1 is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 4 heteroatoms selected from O, N and S, etc.; A is a 5-6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; B is C1-6 alkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; R2 is H, C1-4 alkyl, etc.; Z is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; L is halo, C1-4 alkyl, etc.; m is 0, 1 or 2; R3 and R4 are independently selected from H and C1-4 alkyl ; R5 is H, C1-4 alkyl, etc.; Q2 is a 5-12 membered monocyclic or bicyclic aromatic ring or tricyclic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc. These compounds are useful for the treatment of medical conditions mediated by prostaglamadin such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.