摘要:
The invention relates to compounds of Formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.
摘要:
The present invention provides for compounds of formula (I) which are a class of dopamine agonists, more particularly a class of agonists that are selective for D3 over D2. These compounds are useful for the treatment and/or prevention of sexual dysfunction, for example female sexual dysfunction (FSD), in particular female sexual arousal disorder (FSAD), hypoactive sexual desire disorder (HSDD; lack of interest in sex), female orgasmic disorder (FOD; inability to achieve orgasm); and male sexual dysfunction, in particular male erectile dysfunction (MED). Male sexual dysfunction as referred to herein is meant to include ejaculatory disorders such as premature ejaculation, anorgasmia (inability to achieve orgasm) or desire disorders such as hypoactive sexual desire disorder (HSDD; lack of interest in sex). These compounds are also useful in treating neuropsychiatric disorders and neurodegenerative disorders.
摘要:
Disclosed are compounds of Formula (I): (I) which are useful as bromodomain inhibitors. Pharmaceutical compositions containing compounds of Formula (I) and the use of compounds of Formula (I) to treat diseases or disorders that are bromodomain-dependent are also disclosed. Methods for preparing and using these compounds are further described.
摘要:
The present invention provides for compounds of formula (I), (la) and (lb) Wherein: A is selected from C-X and N, B is selected from C-Y and N, R 1 is selected from H and (C 1 -C 6 )alkyl R 2 is selected from H and (C 1 -C 6 )alkyl, X is selected from H, HO, C(O)NH 2 , NH 2 Y is selected from H HO,, NH 2 , Br, Cl and F Z is selected from H, HO, F, CONH2 and CN; And pharmaceutically acceptable salts, solvates and prodrugs thereof; With the provisos that: for a compound of formula (I), (la) or (lb), when A is C-X, B is C-Y, at least one of X, Y and Z must be OH; for a compound of formula (I), when A is C-X and B is C-Y, Y is H, Z is H, R 1 is H and R 2 is H, then X cannot be OH; these compounds are useful as dopamine agonists for the treatment of i.a. secual dysfunction.
摘要:
The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R 1 is optionally substituted C 1-6 alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C 1-6 alkoxy, -NR 2 R 3 or - NR 4 SO 2 R 5 ; X is the linkage -(CH 2 ) n - or -(CH 2 ) q -O- (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C 1-4 alkoxy; hydroxy; hydroxy(C 1-3 alkyl); C 3-7 cycloalkyl; carbocyclyl; heterocyclyl; or by C 1-4 alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6, or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R 8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.
摘要翻译:本发明涉及用于治疗例如性功能障碍的式(I)化合物,其中R 1是任选取代的C 1-6烷基,任选取代的碳环基,任选取代的杂环基,氢,C 1-6烷氧基,-NR 2 R 3或 NR 4 SO 2 R 5; X是连接 - (CH 2)n - 或 - (CH 2)q -O-(其中Y连接到氧上); 其中连接X中的一个或多个氢原子可以被C 1-4烷氧基独立地取代; 羟基; 羟基(C 1-3烷基); 3-7环烷基; 碳环; 杂环; 或被任选被一个或多个氟或苯基取代的C 1-4烷基; n为3,4,5,6或7; q为2,3,4,5或6; Y为苯基或吡啶基,各自可以被取代; 或相邻碳原子上的两个R 8基团与互连碳原子一起可以形成稠合的任选取代的5或6元碳环或杂环基。
摘要:
The invention relates to compounds of Formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.
摘要:
PC26133A The present invention provides for compounds of formula (I) wherein A, R 1 , R 2 , R 3 , R 4 and R 5 are defined herein. The compounds of formula (I) are a class of dopamine agonists, more particularly a class of agonists that are selective for D3 over D2. These compounds are useful for the treatment and/or prevention of neuropsychiatric disorders, neurodegenerative disorders, pain and sexual dysfunction.
摘要:
PC26133A The present invention provides for compounds of formula (I) wherein A, R 1 , R 2 , R 3 , R 4 and R 5 are defined herein. The compounds of formula (I) are a class of dopamine agonists, more particularly a class of agonists that are selective for D3 over D2. These compounds are useful for the treatment and/or prevention of neuropsychiatric disorders, neurodegenerative disorders, pain and sexual dysfunction.
摘要:
The use of a composition comprising a selective dopamine D3 receptor agonist, wherein said dopamine D3 receptor agonist is at least about 15-times more functionally selective for a dopamine D3 receptor as compared with a dopamine D2 receptor when measured using the same functional assay, in the preparation of a medicament for the treatment and/or prevention of sexual dysfunction.
摘要:
The use of a composition comprising a selective dopamine D3 receptor agonist, wherein said dopamine D3 receptor agonist is at least about 15-times more functionally selective for a dopamine D3 receptor as compared with a dopamine D2 receptor when measured using the same functional assay, in the preparation of a medicament for the treatment and/or prevention of sexual dysfunction.