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公开(公告)号：US20080312235A1
公开(公告)日：2008-12-18
申请号：US11572533
申请日：2005-07-12
IPC分类号： A61K31/5377 , C07D401/12 , A61P25/00
CPC分类号： C07D213/81 , C07D401/12
摘要： The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain.
摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐和溶剂合物，其制备方法，用于制备的中间体和含有这些化合物的组合物以及这些化合物用于治疗疼痛的用途 。
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公开(公告)号：US07053122B2
公开(公告)日：2006-05-30
申请号：US10636406
申请日：2003-08-07
IPC分类号： A61K31/135 , A61K31/137 , A61K31/13
CPC分类号： C07D271/07 , A61K31/195 , C07C227/22 , C07D209/44 , C07D209/46
摘要： The compounds of formula (I) are useful in the treatment of faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, neuropathic pain, neuropathological disorders and sleep disorders. Processes for the preparation of the final products and intermediates useful in the process are included. Pharmaceutical compositions containing one or more of the compounds are also included.
摘要翻译： 式（I）化合物可用于治疗微弱发作，运动功能减退，颅内疾病，神经变性疾病，抑郁症，焦虑症，恐慌症，神经性疼痛，神经病理学障碍和睡眠障碍。 包括用于制备在该方法中有用的最终产物和中间体的方法。 还包括含有一种或多种化合物的药物组合物。
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公开(公告)号：US07649004B2
公开(公告)日：2010-01-19
申请号：US11572533
申请日：2005-07-12
IPC分类号： A61K31/5377 , A61K31/44 , C07D401/12 , C07D413/12
CPC分类号： C07D213/81 , C07D401/12
摘要： The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain.
摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐和溶剂合物，其制备方法，用于制备的中间体和含有这些化合物的组合物以及这些化合物用于治疗疼痛的用途 。
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公开(公告)号：US06586439B2
公开(公告)日：2003-07-01
申请号：US10189680
申请日：2002-07-03
IPC分类号： A61K31495
CPC分类号： C07D473/30
摘要： There is provided compounds of formula IA and of formula IB, wherein R1, R2, R3, Het1 and X have meanings given in the description, which are useful in the curative and prophylactic treatment of medical conditions for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.
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公开(公告)号：US06440982B1
公开(公告)日：2002-08-27
申请号：US09650848
申请日：2000-08-29
IPC分类号： A61K3152
CPC分类号： C07D473/30
摘要： There is provided compounds of formula IA and of formula IB, wherein R1, R2, R3, Het1 and X have meanings given in the description, which are useful in the curative and prophylactic treatment of medical conditions for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.
摘要翻译： 提供式IA和式IB的化合物，其中R1，R2，R3，Het1和X具有描述中给出的含义，其可用于治疗和预防性治疗环状鸟苷3' ，需要5'-单磷酸磷酸二酯酶（例如cGMP PDE5）。
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公开(公告)号：US06756373B1
公开(公告)日：2004-06-29
申请号：US09684228
申请日：2000-10-06
申请人： Charlotte Moira Norfor Allerton , Christopher Gordon Barber , Graham Nigel Maw , David James Rawson
发明人： Charlotte Moira Norfor Allerton , Christopher Gordon Barber , Graham Nigel Maw , David James Rawson
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： There is provided a compound of formula I: wherein X represents O or NR5 R4 represents H, halo, cyano, nitro, halo(loweralkyl), OR6, OC(O)R7, C(O)R8, C(O)OR9, C(O)NR10R11, NR12R13, NR16Y(O)R17, N[Y(O)R17]2, SOR18, SO2R19, C(O)AZ, lower alkyl, lower alkenyl, lower alkynyl, Het, alkylHet, aryl, alkylaryl (which latter seven groups are all optionally substituted with one or more substituents selected from halo, cyano, nitro, lower alkyl, halo(loweralkyl), OR6, OC(O)R7, C(O)R8, C(O)OR9, C(O)NR10R11, NR12R13 and SO2NR14R15) which are useful in the curative and prophylactic treatment of a medical condition for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g., cGMP PDE5) is desired.
摘要翻译： 提供式I化合物：其中X代表O或NR 5 R 4表示H，卤素，氰基，硝基，卤素（低级烷基），OR 6，OC（O）R 7，C （O）R 8，C（O）OR 9，C（O）NR 10 R 11，NR 12 R 13，NR 16 Y（O）R 17 >，N [Y（O）R 17] 2，SOR 18，SO 2 R 19，C（O）AZ，低级烷基，低级烯基，低级炔基，Het，烷基Het，芳基，烷基芳基 七个基团都可以被一个或多个选自卤素，氰基，硝基，低级烷基，卤代（低级烷基），OR 6，OC（O）R 7，C（O）R 8， C（O）OR 9，C（O）NR 10 R 11，NR 12 R 13和SO 2 NR 14 R 15），其可用于治疗和预防性治疗 需要抑制环鸟嘌呤3'，5'-单磷酸磷酸二酯酶（例如cGMP PDE5）的医学病症。
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公开(公告)号：US06593332B2
公开(公告)日：2003-07-15
申请号：US10189655
申请日：2002-07-03
IPC分类号： A61K3152
CPC分类号： C07D473/30
摘要： There is provided compounds of formula IA and of formula IB, wherein R1, R2, R3, Het1 and X have meanings given in the description, which are useful in the curative and prophylactic treatment of medical conditions for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.
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公开(公告)号：US5696146A
公开(公告)日：1997-12-09
申请号：US553589
申请日：1995-11-16
IPC分类号： A61K31/405 , A61K31/41 , A61P5/00 , A61P13/02 , A61P15/00 , A61P17/00 , A61P35/00 , A61P43/00 , C07D405/06 , C07D405/14 , A61K31/40
CPC分类号： C07D405/06
摘要： Compounds of formula (I) ##STR1## and the pharmaceutically acceptable base salts thereof, wherein R is --CO.sub.2 H or tetrazol-5 yl; R.sup.1 is C.sub.3 -C.sub.8 alkyl optionally substituted by fluoro; and R.sup.2 is C.sub.2 -C.sub.4 alkyl, together with compositions containing, uses of, process for the preparation of, and intermediates used in the preparation of, such compounds. The compounds have steroid 5.alpha.-reductase inhibitory activity and are useful for treating a disease such as benign prostatic hypertrophy.
摘要翻译： PCT No.PCT / EP94 / 01760 Sec。 371日期：1995年11月16日 102（e）日期1995年11月16日PCT 1994年5月26日PCT PCT。 WO94 / 27990 PCT公开 日期1994年12月8日，式（I）的化合物及其药学上可接受的碱式盐，其中R为-CO 2 H或四唑-5-基; R 1是任选被氟取代的C 3 -C 8烷基; 以及R2是C2-C4烷基，以及含有制备方法的用途的组合物和用于制备这些化合物的中间体。 该化合物具有类固醇5α-还原酶抑制活性，可用于治疗良性前列腺肥大等疾病。
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9.发明授权Pyrazolopyrimidinone CGMP PDE5 inhibitors for the treatment of sexual dysfunction 失效吡唑并嘧啶酮CGMP PDE5抑制剂治疗性功能障碍公开(公告)号：US06333330B1
公开(公告)日：2001-12-25
申请号：US09426554
申请日：1999-10-22
申请人： Mark Edward Bunnage , John Paul Mathias , Graham Nigel Maw , David James Rawson , Stephen Derek Albert Street , Anthony Wood
发明人： Mark Edward Bunnage , John Paul Mathias , Graham Nigel Maw , David James Rawson , Stephen Derek Albert Street , Anthony Wood
IPC分类号： A61K31505
CPC分类号： C07D401/12 , C07D231/14 , C07D487/04
摘要： There is provided compounds of formula IA and of formula IB, wherein R1, R2, R3, R4 and A have meanings given in the description, which are useful in the curative and prophylactic treatment of medical conditions for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.
摘要翻译： 提供式IA和式IB的化合物，其中R 1，R 2，R 3，R 4和A具有在描述中给出的含义，其可用于治疗和预防治疗环状鸟苷3' ，需要5'-单磷酸磷酸二酯酶（例如cGMP PDE5）。
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公开(公告)号：US5922747A
公开(公告)日：1999-07-13
申请号：US982735
申请日：1997-12-02
IPC分类号： A61K31/405 , A61K31/41 , A61P5/00 , A61P13/02 , A61P15/00 , A61P17/00 , A61P35/00 , A61P43/00 , C07D405/06 , C07D405/14 , A61K31/40
CPC分类号： C07D405/06
摘要： A method of treatment of a human to inhibit a steroid 5.alpha.-reductase, particularly a testosterone 5.alpha.-reductase, which comprises treating said human with an effective amount of a compound of the formula (I) ##STR1## or a pharmaceutically acceptable base salt thereof, wherein R is --CO.sub.2 H or tetrazol-5-yl;R.sup.1 is C.sub.3 -C.sub.8 alkyl optionally substituted by fluoro; andR.sup.2 is C.sub.2 -C.sub.4 alkylor with a pharmaceutically acceptable base salt or composition thereof. Conditions which are treatable by such inhibition include acne vulgaris, alopecia, seborrhoea, female hirsutism, benign prostatic hypertropy, male pattern baldness and human prostate adenocarcinomas.
摘要翻译： 一种治疗人类以抑制类固醇5α-还原酶，特别是睾丸激素5α-还原酶的方法，其包括用有效量的式（I）化合物或其药学上可接受的碱盐处理所述人， 其中R是-CO 2 H或四唑-5-基; R1是任选被氟取代的C3-C8烷基; 并且R 2是C 2 -C 4烷基或其药学上可接受的碱盐或组合物。 通过这种抑制可治疗的病症包括寻常痤疮，脱发，皮脂溢，女性多毛症，良性前列腺肥大，男性型秃发和人类前列腺腺癌。
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