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    • 7. 发明申请
    • ADRENERGIC RECEPTOR ANTAGONISTS
    • WO2005113498A1
    • 2005-12-01
    • PCT/IB2004/001641
    • 2004-05-19
    • RANBAXY LABORATORIES LIMITEDSALMAN, MohammadSHARMA, SomeshKAPKOTI, Gobind, SinghANAND, NityaCHUGH, Anita
    • SALMAN, MohammadSHARMA, SomeshKAPKOTI, Gobind, SinghANAND, NityaCHUGH, Anita
    • C07D207/40
    • C07D207/408C07D207/448C07D209/48
    • This invention relates to α 1a and/or α 1d adrenergic receptor antagonists. Compounds disclosed herein can function as α 1a and/or α 1d adrenergic receptor antagonist and can be used for the treatment of diseases or disorder mediated through α 1a and/or α 1d adrenergic receptors. Compounds disclosed herein can be used for the treatment of benign prostatic hyperplasia and the related symptoms thereof. Compounds disclosed herein can be used for the treatment of lower urinary tract symptoms associated with or without benign prostatic hyperplasia. Processes for the preparation of compounds disclosed herein, pharmaceutical compositions containing the compounds disclosed herein, and methods of treating benign prostatic hyperplasia or related symptoms thereof are also provided. Formula (I) Its pharmaceutically acceptable acid addition salts,pharmaceutically acceptable solvates, enantiomers, diastereomers, N-oxides, polymorphs or metabolites,wherein; A represents a Formula (F.a or ,F.b or F.c wherein) N represents 1 or 2; Y represents cycloalkyl (C 5- C 7 ) group; optionally substituted with halogen atom(s) or lower alkyl (C 1- C 4 ) group; and R is selected from optionally substituted non_aromatic or aromatic monocyclic or bicyclic ring system having 0 to 4 heteroatom(s),the substituent(s) may be selected from the group consisting of halogen, lower alkyl (C 1- C 4 ),halogenated lower alkyl (C 1- c 4 ),cyano, hydroxy, lower alkoxy (C 1- C 4 ),cycloalkoxy (C 3- C 6 ),amino,lower alkylamino (C 1- C 4 ) and lower alkylamino (C 1- C 4 ) carbonyl group.
    • 本发明涉及α1a和/或α1d肾上腺素能受体拮抗剂。 本文公开的化合物可用作α1a和/或α1肾上腺素能受体拮抗剂,并且可用于治疗通过α1a和/或α1肾上腺素能受体介导的疾病或病症。 本文公开的化合物可用于治疗良性前列腺增生及其相关症状。 本文公开的化合物可用于治疗与或不伴有良性前列腺增生相关的下尿路症状。 还提供了制备本文公开的化合物的方法,含有本文公开的化合物的药物组合物,以及治疗良性前列腺增生或其相关症状的方法。 式(I)其药学上可接受的酸加成盐,药学上可接受的溶剂合物,对映异构体,非对映异构体,N-氧化物,多晶型物或代谢物,其中; A表示式(F.a或F.b或F.c,其中N表示1或2; Y代表环烷基(C5-C7)基团; 任选被卤素原子或低级烷基(C 1 -C 4)基团取代; 并且R选自具有0至4个杂原子的任选取代的非芳族或芳族单环或双环体系,所述取代基可以选自卤素,低级烷基(C 1 -C 4),卤代低级烷基 (C1-C4),氰基,羟基,低级烷氧基(C1-C4),环烷氧基(C3-C6),氨基,低级烷基氨基(C1-C4)和低级烷基氨基(C1-C4)羰基。