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41.发明公开
公开(公告)号：EP0934257A1
公开(公告)日：1999-08-11
申请号：EP97936050.0
申请日：1997-07-16
发明人： ANTANE, Madelene, Miyoko , HERBST, David, Richard , McFARLANE, Geraldine, Ruth , GUNDERSEN, Eric, Gould , HIRTH, Bradford, Hammond , QUAGLIATO, Dominick, Anthony , GRACEFFA, Russell, Francis , BUTERA, John, Anthony , GILBERT, Adam, Matthew
CPC分类号： C07C225/20 , C07C233/41 , C07C255/58 , C07C271/24 , C07C2601/04 , C07C2601/08
摘要： The compounds of formula (I) wherein R1, R2, R3 and A are as defined herein are useful, via potassium channel modulation, in the treatment of disorders associated with smooth muscle contraction. Such disorders include, but are not limited to, urinary incontinence, hypertension, asthma, premature labor, irritable bowel syndrome, congestive heart failure, angina and cerebral vascular disease.
摘要翻译： 下式的化合物：其中R 1，R 2，R 3和A如本文所定义，通过钾通道调节可用于治疗与平滑肌收缩相关的疾病。 这些疾病包括但不限于尿失禁，高血压，哮喘，早产，肠易激综合征，充血性心力衰竭，心绞痛和脑血管疾病。
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公开(公告)号：EP0927034A1
公开(公告)日：1999-07-07
申请号：EP97942538.0
申请日：1997-09-17
CPC分类号： A61K31/00 , A61K9/0034 , A61K31/137 , A61K31/192 , A61K31/215 , A61K31/221 , A61K31/277 , A61K31/352 , A61K31/4025
摘要： This invention provides a method of treating urinary incontinence in a female mammal which comprises administering to said mammal an effective amount of an anti-incontinent agent intravaginally or rectally.
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公开(公告)号：EP0730598B1
公开(公告)日：1999-06-09
申请号：EP95903559.3
申请日：1994-11-18
IPC分类号： C07D498/18 , A61K31/435 , A61K31/71
CPC分类号： C07D498/18
摘要： A compound of structure (I) wherein R and R1 are each, independently, (A), (B), or hydrogen; R?2 and R3¿ are each, independently, alkyl, arylalkyl, or R?2 and R3¿ may be taken together to form a cycloalkyl ring; R4 is a heterocyclic radical which may be optionally substituted; R5 is alkyl or arylalkyl; R?6 and R7¿ are taken together to form a saturated heterocyclic ring which may be optionally substituted; k=0-1; m=0-1; n=1-6; with the proviso that R and R1 are not both hydrogen, or a pharmaceutically acceptable salt thereof, which is useful as an immunosuppresive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
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公开(公告)号：EP0745063B1
公开(公告)日：1999-03-24
申请号：EP95908671.1
申请日：1995-01-25
IPC分类号： C07C235/42 , C07C243/38 , C07C255/54 , C07C217/80 , C07C251/44 , C07C251/48 , C07C275/32 , C07C235/34 , C07C259/10 , C07D237/30 , C07C65/21
CPC分类号： C07D237/32 , C07C43/235 , C07C43/247 , C07C45/68 , C07C47/575 , C07C49/755 , C07C49/84 , C07C65/26 , C07C69/94 , C07C217/80 , C07C233/25 , C07C235/42 , C07C243/38 , C07C251/44 , C07C251/48 , C07C255/54 , C07C259/10 , C07C275/34 , C07C2601/08 , C07C2602/10
摘要： A compound of structure (I), wherein, when R8 = H: R1 = alkyl, cycloalkyl, arylalkyl, aryl; R2 = cycloalkyl, aryl, C3-C10 alkyl; X, Y = O, S(O)n, NH; Z = CH2OH, NHSO2R3, CHO, CO2R3, CONHR4R5, CN, COR6, H, halo, NHCN, NHCONR4R5, CONR4OR5, CONR4NR5R6, 1-tetrazole, S(O)nOH, S(O)nNR3R4, C=NOH, C(=N(OH)NH2, OCONR7R6, P(O)(OR4)2, NH2, SH, OH, OS(O)2R3, C(O)CO2R3, C(O)CONR3R4, CH(OH)CO2R3, CHFCO2R3, CF2CO2R3, CH(OH)CONR3R4, CF2CONR3R4, C=NNH2, C(=NOC(=O)R3)R4, C(=NNHC(=O)R3)R4, C(=NOH)R3, C(=NNR3)R4, NHC(=O)R6 or C(O)CONH2; R3, R4, R5, R6, R7 = hydrogen, alkyl, aryl, aryalkyl, cycloalkyl, or fluoroalkyl; or a compound of Structure I, wherein: R1 = alkyl, cycloalkyl, aryalkyl, or aryl; R2 = cycloalkyl, aryl, or alkyl; X, Y = CH2, O, S(O)n), or NH; R3, R4, R5, R6, R7 are each, independently, hydrogen, alkyl, aryl, aryalkyl, cycloalkyl, or fluoroalkyl; R8 = CO2R3, CONR3, or R8 and Z are concatenated such that R8Z = C(O)NHNHC(O), (CH2)mC(=W), V(CH2)mC(=W), or VnCH=CH(CH2)nC(=W); where V = O, S(O)n, NH; W = O, NOH, NHNH2, NOC(O)CH3, or NNHC(O)CH3; halo = Cl, Br, or I; fluoroalkyl = CF3CHF2, CH2F, CH2CF3, C2F5; cycloalkyl = C3-C6 cycloalkyl; aryalkyl = C1-C4 aryl; aryl = phenyl, furanyl, thienyl, or pyridyl; n = 0-2; and m = 2-4 or pharmaceutically acceptable salts thereof, useful in the treatment of asthma, or allergic or inflammatory diseases, as well as methods of treatment and pharmaceutical compositions utilizing the same.
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公开(公告)号：EP0796243B1
公开(公告)日：1999-01-27
申请号：EP95935742.7
申请日：1995-10-03
发明人： ANTANE, Madelene, Miyoko , BUTERA, John, Anthony , HIRTH, Bradford, Hammond , ANTANE, Schuyler, Adam
IPC分类号： C07C255/60 , A61K31/275 , C07C271/24 , C07D217/22 , A61K31/44 , C07D213/74
CPC分类号： C07D213/75 , C07C233/41 , C07C255/60 , C07C271/28 , C07C311/08 , C07C2601/04 , C07C2601/14 , C07C2602/42 , C07D217/02
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46.发明授权ALKYLIDENE ANALOGS OF 1'-AMINOSPIRO-[ISOQUINOLINE- 4(1H),3'-PYRROLIDINE]-1,2',3,5'(2H)-TETRONES USEFUL AS ALDOSE REDUCTASE INHIBITORS IN VIVO 失效1'-AMINOSPIRO- [异喹啉-4（1H），3'-吡咯烷〕-1,2”，3,5' （2H）的ALKYLIDENANALOGE -tetrones，有用的作为体内醛糖还原酶抑制剂
公开(公告)号：EP0555327B1
公开(公告)日：1999-01-13
申请号：EP91919785.5
申请日：1991-10-10
IPC分类号： C07D471/10 , A61K31/47
CPC分类号： C07D471/10
摘要： This invention relates to alkylidene analogs of 1'-aminospiro[isoquinoline-4(1H),3'-pyrrolidine]-1,2',3,5'(2H)-tetrones (I), to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes mellitus associated complications.
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公开(公告)号：EP0628052B1
公开(公告)日：1998-12-09
申请号：EP93906093.5
申请日：1993-02-19
IPC分类号： C07J31/00 , A61K31/565 , C07J1/00
CPC分类号： C07J1/0059 , C07J31/006
摘要： This invention presents alkali metal salts of 8,9-dehydroestrone, salts of its sulfate ester, and stable compositions thereof, as well as processes for their production and use in estrogen replacement therapy and cardiovascular protection.
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公开(公告)号：EP0879238A1
公开(公告)日：1998-11-25
申请号：EP97901369.0
申请日：1997-01-07
IPC分类号： C07F9
CPC分类号： C07F9/65068 , C07F9/4006
摘要： This invention provides a process for the preparation of a compound of formula (I), wherein R?1 and R2¿ are each, independently, hydrogen, alkyl, alkoxy, trifluoromethyl, trifluoromethoxy, methanesulfonylamino, acetylamino, halo, cyano, nitro, or when taken together R?1 and R2¿ represent a methylenedioxy or ethylenedioxy moiety; or a pharmaceutically acceptable salt thereof.
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49.发明授权1'-AMINOSPIRO-[ISOQUINOLINE-4(1H),3'-PYRROLIDINE]- 1,2',3,5'(2H)-TETRONES AND ANALOGS THEREOF USEFUL AS ALDOSE REDUCTASE INHIBITORS IN VIVO 失效1'-AMINOSPIRO- [异喹啉-4（1H），3'-吡咯烷] - 1,2”，3,5' - （2H）-tetrones和类似化合物作为醛糖还原酶的体内抑制剂
公开(公告)号：EP0553263B1
公开(公告)日：1998-08-05
申请号：EP91920029.5
申请日：1991-10-10
IPC分类号： C07D471/10
CPC分类号： C07D471/10
摘要： This invention relates to 1'-aminospiro[isoquinoline-4(1H),3'-pyrrolidine]-1,2',3,5'(2H)-tetrones and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes mellitus associated complications.
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50.发明公开PHENOXY ACETIC ACIDS AS ALDOSE REDUCTASE INHIBITORS AND ANTIHYPERGLYCEMIC AGENTS 失效苯氧ALS还原酶抑制剂和中等ANTIHYPERGLYZEMISCHE
公开(公告)号：EP0847379A1
公开(公告)日：1998-06-17
申请号：EP96926208.0
申请日：1996-08-01
CPC分类号： C07C69/712 , C07C45/68 , C07C47/575 , C07C59/74
摘要： This invention relates to 4-formyl-2-(naphthalenylmethyl)phenoxyacetic acids and pharmaceutically acceptable salts thereof according to formula (I), pharmaceutically compositions thereof, a method of treating hyperglycemia due to non-insulin dependent diabetes mellitus, and a method of prevention or treatment of complications associated with diabetes. In said formula the group A is selected from the group consisting of 1-naphthyl, 2-naphthyl, optionally substituted with alkyl of from one to six carbon atoms, fluorine, chlorine, bromine, iodine, trifluoromethyl, alkoxy of from one to six carbon atoms; R1 is hydrogen or alkyl of from one to six carbon atoms; R2 is selected from hydrogen, fluorine, chlorine, bromine, iodine, alkyl of from one to six carbon atoms, alkoxy of from one to six carbon atoms, and hydroxyl; or a pharmaceutically acceptable metal salt thereof.
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