摘要:
The present invention relates to novel piperazine-piperidine compounds. The compounds are useful as 5-HT1A binding agents, particularly as 5-HT1A receptor antagonists and agonists. These compounds are useful in treating central nervous system disorders, such as cognition disorders, anxiety disorders, depression and sexual dysfunction. The invention relates to compounds and pharmaceutically acceptable salts of formula (I′): wherein R1-R16, Ra, Rb, and n are set forth in the specification. The invention also relates to pharmaceutical compositions comprising compounds and pharmaceutically acceptable salts of formula (I′).
摘要:
Benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives and compositions containing such compounds are disclosed. Methods of using benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives and compositions containing such composition in the treatment and/or prevention of serotonin-related disorders, such as depression and anxiety, are also disclosed. In addition, processes for the preparation of benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives are disclosed.
摘要:
Benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives and compositions containing such compounds are disclosed. Methods of using benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives and compositions containing such composition in the treatment and/or prevention of serotonin-related disorders, such as depression and anxiety, are also disclosed. In addition, processes for the preparation of benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives are disclosed. Benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives of Formula I are disclosed:
摘要:
The present invention relates to novel piperazine-piperidine compounds. The compounds are useful as 5-HT1A binding agents, particularly as 5-HT1A receptor antagonists and agonists. These compounds are useful in treating central nervous system disorders, such as cognition disorders, anxiety disorders, depression and sexual dysfunction.
摘要:
The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.
摘要:
Compounds are provided which are useful for the treatment of serotonin-affected neurological disorders which comprise Wherein: R1, R2 and R3 are each, independently, hydrogen, halogen, CF3, alkyl, alkoxy, MeSO2, or together can form a 5-7 membered carbocyclic or heterocyclic ring; R4 is hydrogen, halogen, or alkyl; R5 is hydrogen, alkyl, alkylaryl, or aryl; R6 is hydrogen, halogen, CF3, CN, carbamide, or alkoxy; X1, X2 and X3 are each carbon or one of X1, X2 or X3 may be nitrogen; Y is carbon or nitrogen; and Z is carbon or nitrogen; or pharmaceutically acceptable salts thereof.
摘要翻译:提供了可用于治疗受5-羟色胺影响的神经系统疾病的化合物,其包括:R 1,R 2和R 3各自独立地为氢,卤素,CF 3,烷基,烷氧基,MeSO 2或一起可以形成5-7元碳环 或杂环; R 4为氢,卤素或烷基; R 5为氢,烷基,烷基芳基或芳基; R 6为氢,卤素,CF 3,CN,脲或烷氧基; X 1,X 2和X 3为碳或 X1,X2或X3可以是氮; Y是碳或氮; Z为碳或氮; 其药学上可接受的盐。
摘要:
Compounds of the formula R1 and R2 are independently alkyl of 1 to 6 carbon atoms, allyl, or substituted allyl of 3 to 6 carbon atoms; R3 is hydrogen, alkyl of 1 to 6 carbon atoms, or cycloalkyl of 3 to 10 carbon atoms; and R4 is phenyl or naphthyl substituted with alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms or NR5R6; substituted or unsubstituted phenylalkyl wherein the alkyl group contains 1 to 6 carbon atoms; substituted or unsubstituted 5 to 10 membered heteroaryl having 1 to 3 heteroatoms selected from N, S and O; substituted or unsubstituted cycloalkyl of 3 to 10 carbon atoms; or substituted or unsubstituted cycloalkylalkyl of 4 to 10 carbon atoms; provided that phenyl or naphthyl is substituted with NR5R6 when R1 and R2 is alkyl, are useful in the treatment of various disorders associated bone loss by increased transcription and elevation of plasma calcitonin levels. Such disorders include, but are not limited to: Paget's Disease, post menopausal osteoporosis, senile osteoporosis, and glucocorticoid-induced osteoporosis.
摘要:
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of a CNS disorder related to or affected by the 5-HT6 receptor.
摘要:
This invention provides novel compounds and pharmaceutical compositions and methods of using the compounds in the treatment of central nervous system disorders, such as anxiety and depression, the compounds having the formula I: wherein: X is N—R, O, S(O)m; m is 0 to 2; n is 0 to 4; Ar is an aryl group of 6 to 12 carbon atoms optionally substituted with 1 to 3 R3 groups, or a heteroaryl group of 4 to 10 carbon atoms optionally substituted with 1 to 3 R3 groups; R and R2 are independently H, straight chain alkyl of 1 to 6 carbon atoms, branched alkyl of 3 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, alkoxycarbonyl of 1 to 6 carbon atoms, alkylcarbonyl of 1 to 6 carbon atoms, aminocarbonyl, or alkylaminocarbonyl of 1 to 4 carbon atoms; R1 and R3 are independently H, straight chain alkyl of 1 to 4 carbon atoms, branched alkyl of 3 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, halo, alkoxy group of 1 to 4 carbon atoms, haloalkyl of 1 to 4 carbon atoms, OH, nitro, amino, sulfonyl, CN, carboxy, alkoxycarbonyl of 1 to 4 carbon atoms, alkylcarbonyl of 1 to 4 carbon atoms, aminocarbonyl, or alkylaminocarbonyl of 1 to 4 carbon atoms; or a pharmaceutically acceptable salt thereof.
摘要翻译:本发明提供了新的化合物和药物组合物和使用该化合物治疗中枢神经系统疾病如焦虑和抑郁的方法,具有式I的化合物:其中:X是N-R,O,S(O)m; m为0〜2; n为0〜4; Ar是任选被1至3个R 3基团取代的6至12个碳原子的芳基或任选被1至3个R 3基团取代的4至10个碳原子的杂芳基; R 2和R 2独立地是H,直链烷基 1至6个碳原子,3至6个碳原子的支链烷基,3至6个碳原子的环烷基,1至6个碳原子的烷氧基羰基,1至6个碳原子的烷基羰基,氨基羰基或1至4个碳原子的烷基氨基羰基; R 1和R 3独立地为H,1至4个碳原子的直链烷基,3至6个碳原子的支链烷基,3至8个碳原子的环烷基,卤素,1至4个碳原子的烷氧基,1至4个卤代烷基 碳原子,OH,硝基,氨基,磺酰基,CN,羧基,1至4个碳原子的烷氧基羰基,1至4个碳原子的烷基羰基,氨基羰基或1至4个碳原子的烷基氨基羰基;或其药学上可接受的盐。
摘要:
The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.