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    • 3. 发明申请
    • NOVEL COMPOUNDS, THEIR USE AND PREPARATION
    • 新化合物,其使用和制备
    • WO0076984A3
    • 2001-02-08
    • PCT/SE0001017
    • 2000-05-19
    • PHARMACIA & UPJOHN ABNILSSON BJOERNTEJBRANT JANPELCMAN BENJAMINRINGBERG ERIKTHOR MARKUSNILSSON JONASJOENSSON MATTIAS
    • NILSSON BJOERNTEJBRANT JANPELCMAN BENJAMINRINGBERG ERIKTHOR MARKUSNILSSON JONASJOENSSON MATTIAS
    • A61K31/497A61K31/498A61K31/517A61K31/5377A61K31/551A61P3/04A61P13/00A61P15/00A61P25/00A61P25/04A61P25/18A61P25/22A61P25/24A61P25/28A61P43/00C07D241/18C07D241/20C07D241/54C07D401/12C07D403/04C07D403/12C07D405/12C07D405/14C07D409/12C07D413/12C07D417/12C07D491/04
    • C07D401/12C07D241/18C07D241/20C07D403/12C07D405/12C07D413/12C07D417/12C07D491/04
    • The invention relates to compounds of general formula (I) wherein Ar is optionally substituted aryl or heteroaryl; A is (i) -O-, -S-, -SO2-, -NH-, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is -C(R4)(R5)-, -OC(R4)(R5)-, -N(R6)C(R4)(R5)-, -N(R6)-O-, -S- or -SO2-; R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl; R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group -[C(R4)(R5)]xN(R2a)(R3a)]; R2a, R3a, R4, R5, R6 and x are as defined in the claims, and n is 0 or 1; and pharmaceutically acceptable salts, hydrates and prodrug forms thereof. The compounds may be prepared by per se conventional methods and can be used for treating a human or animal subject suffering from a serotonin-related disorder, such as eating disorders, especially obesity, memory disorders, schizophrenia, mood disorders, anxiety disorders, pain, sexual dysfunctions, and urinary disorders. The invention also relates to such use as well as to pharmaceutical compositions comprising a compound of formula (I).
    • 本发明涉及通式(I)的化合物,其中Ar为任选取代的芳基或杂芳基; A是(ⅰ)-O - , - S - , - SO 2 - , - NH - ,(ⅱ)C 1-4 - 烷基 - 或C 1-6 - 酰基取代的氮原子或(ⅲ) 亚烷基链或具有2至8个链原子的杂亚烷基链,其任选地包含至少一个不饱和键,并且其可以被取代和/或含有桥以形成具有3-8个环成员的饱和或部分或完全不饱和的环; B是-C(R4)(R5) - ,-OC(R4)(R5) - , - N(R6)C(R4)(R5) - ,-N(R6)-O - , - S-或 - SO2-; R是任选取代的C 3-8 - 环烷基,芳基或杂芳基; R1是(i)饱和或不饱和的氮杂环或氨基氮杂环,或具有4-7个环成员的饱和二氮环或氨基二氮环,或具有7至10个环成员的饱和氨基氮杂双环,氮杂双环或二氮杂双环,其任选地 在一个或多个位置被取代,或基团 - [C(R 4)(R 5)] x N(R 2a)(R 3a)]; R2a,R3a,R4,R5,R6和x如权利要求中所定义,n为0或1; 及其药学上可接受的盐,水合物和前药形式。 化合物可以通过本身的常规方法制备,并且可以用于治疗患有5-羟色胺相关病症的人或动物受试者,例如进食障碍,特别是肥胖症,记忆障碍,精神分裂症,情绪障碍,焦虑症,疼痛, 性功能障碍和尿失调。 本发明还涉及这样的用途以及包含式(I)化合物的药物组合物。
    • 5. 发明申请
    • NOVEL COMPOUNDS, THEIR USE AND PREPARATION
    • 新化合物,它们的用途和制备
    • WO0076984A8
    • 2001-07-19
    • PCT/SE0001017
    • 2000-05-19
    • PHARMACIA ABNILSSON BJOERNTEJBRANT JANPELCMAN BENJAMINRINGBERG ERIKTHOR MARKUSNILSSON JONASJOENSSON MATTIAS
    • NILSSON BJOERNTEJBRANT JANPELCMAN BENJAMINRINGBERG ERIKTHOR MARKUSNILSSON JONASJOENSSON MATTIAS
    • A61K31/497A61K31/498A61K31/517A61K31/5377A61K31/551A61P3/04A61P13/00A61P15/00A61P25/00A61P25/04A61P25/18A61P25/22A61P25/24A61P25/28A61P43/00C07D241/18C07D241/20C07D241/54C07D401/12C07D403/04C07D403/12C07D405/12C07D405/14C07D409/12C07D413/12C07D417/12C07D491/04
    • C07D401/12C07D241/18C07D241/20C07D403/12C07D405/12C07D413/12C07D417/12C07D491/04
    • The invention relates to compounds of general formula (I) wherein Ar is optionally substituted aryl or heteroaryl; A is (i) -O-, -S-, -SO2-, -NH-, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is -C(R4)(R5)-, -OC(R4)(R5)-, -N(R6)C(R4)(R5)-, -N(R6)-O-, -S- or -SO2-; R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl; R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group -[C(R4)(R5)]xN(R2a)(R3a)]; R2a, R3a, R4, R5, R6 and x are as defined in the claims, and n is 0 or 1; and pharmaceutically acceptable salts, hydrates and prodrug forms thereof. The compounds may be prepared by per se conventional methods and can be used for treating a human or animal subject suffering from a serotonin-related disorder, such as eating disorders, especially obesity, memory disorders, schizophrenia, mood disorders, anxiety disorders, pain, sexual dysfunctions, and urinary disorders. The invention also relates to such use as well as to pharmaceutical compositions comprising a compound of formula (I).
    • 本发明涉及通式(I)的化合物,其中Ar是任选取代的芳基或杂芳基; A为(i)-O - , - S - , - SO2 - , - NH-,(ii)C1-4-烷基 - 或C1-6-酰基取代的氮原子或(iii)C1-8- 亚烷基链或具有2-8个链原子的杂亚烷基链,其任选地含有至少一个不饱和键,并且其可以被取代和/或含有桥以形成具有3-8个环成员的饱和或部分或完全不饱和的环; (R 4)(R 5) - , - O(R 4)(R 5) - , - N(R 6)C SO2-; R是任选取代的C 3-8 - 环烷基,芳基或杂芳基; R1为(i)饱和或不饱和的氮杂环或氨基氮杂环或饱和的二氮杂环或氨基二氮杂环,其具有4至7个环成员,或具有7至10个环成员的饱和氨基氮杂二环,氮杂二环或二氮杂双环, 在一个或多个位置被取代,或基团 - [C(R4)(R5)] xN(R2a)(R3a)]; R2a,R3a,R4,R5,R6和x如权利要求中所定义,且n为0或1; 及其药学上可接受的盐,水合物和前药形式。 这些化合物可以通过本身常规方法制备,并且可以用于治疗患有血清素相关病症的人或动物对象,例如进食障碍,尤其是肥胖症,记忆障碍,精神分裂症,心境障碍,焦虑症,疼痛, 性功能障碍和泌尿系统疾病。 本发明还涉及这种用途以及包含式(I)化合物的药物组合物。
    • 6. 发明申请
    • NOVEL COMPOUNDS, THEIR USE AND PREPARATION
    • 新化合物,其使用和制备
    • WO00076984A2
    • 2000-12-21
    • PCT/SE2000/001017
    • 2000-05-19
    • A61K31/497A61K31/498A61K31/517A61K31/5377A61K31/551A61P3/04A61P13/00A61P15/00A61P25/00A61P25/04A61P25/18A61P25/22A61P25/24A61P25/28A61P43/00C07D241/18C07D241/20C07D241/54C07D401/12C07D403/04C07D403/12C07D405/12C07D405/14C07D409/12C07D413/12C07D417/12C07D491/04
    • C07D401/12C07D241/18C07D241/20C07D403/12C07D405/12C07D413/12C07D417/12C07D491/04
    • The invention relates to compounds of general formula (I) wherein Ar is optionally substituted aryl or heteroaryl; A is (i) -O-, -S-, -SO2-, -NH-, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is -C(R4)(R5)-, -OC(R4)(R5)-, -N(R6)C(R4)(R5)-, -N(R6)-O-, -S- or -SO2-; R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl; R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group -[C(R4)(R5)]xN(R2a)(R3a)]; R2a, R3a, R4, R5, R6 and x are as defined in the claims, and n is 0 or 1; and pharmaceutically acceptable salts, hydrates and prodrug forms thereof. The compounds may be prepared by per se conventional methods and can be used for treating a human or animal subject suffering from a serotonin-related disorder, such as eating disorders, especially obesity, memory disorders, schizophrenia, mood disorders, anxiety disorders, pain, sexual dysfunctions, and urinary disorders. The invention also relates to such use as well as to pharmaceutical compositions comprising a compound of formula (I).
    • 本发明涉及通式(I)的化合物,其中Ar为任选取代的芳基或杂芳基; A是(ⅰ)-O - , - S - , - SO 2 - , - NH - ,(ⅱ)C 1-4 - 烷基 - 或C 1-6 - 酰基取代的氮原子或(ⅲ) 亚烷基链或具有2至8个链原子的杂亚烷基链,其任选地包含至少一个不饱和键,并且其可以被取代和/或含有桥以形成具有3-8个环成员的饱和或部分或完全不饱和的环; B是-C(R4)(R5) - ,-OC(R4)(R5) - , - N(R6)C(R4)(R5) - ,-N(R6)-O - , - S-或 - SO2-; R是任选取代的C 3-8 - 环烷基,芳基或杂芳基; R1是(i)饱和或不饱和的氮杂环或氨基氮杂环,或具有4-7个环成员的饱和二氮环或氨基二氮环,或具有7至10个环成员的饱和氨基氮杂双环,氮杂双环或二氮杂双环,其任选地 在一个或多个位置被取代,或基团 - [C(R 4)(R 5)] x N(R 2a)(R 3a)]; R2a,R3a,R4,R5,R6和x如权利要求中所定义,n为0或1; 及其药学上可接受的盐,水合物和前药形式。 化合物可以通过本身的常规方法制备,并且可以用于治疗患有5-羟色胺相关病症的人或动物受试者,例如进食障碍,特别是肥胖症,记忆障碍,精神分裂症,情绪障碍,焦虑症,疼痛, 性功能障碍和尿失调。 本发明还涉及这样的用途以及包含式(I)化合物的药物组合物。