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1.发明公开PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING SECRETED FRIZZLED RELATED PROTEIN 审中-公开分泌型卷曲相关蛋白的药物组合物含有及其用途
公开(公告)号：EP1212355A2
公开(公告)日：2002-06-12
申请号：EP00960097.4
申请日：2000-09-13
IPC分类号： C07K14/00
CPC分类号： A01K67/0276 , A01K2227/105 , A01K2267/03 , A61K38/00 , C07K14/71
摘要： Pharmaceutical compositions and methods of use in regulation of mammalian bone forming activities of SFRPs (secreted frizzled-related proteins) are disclosed. SFRPs are secreted receptors for Wnts that are important polypeptide growth factors that are known to regulate fundamental biological processes like tissue polarity, embryonic development and tumorigenesis. A SFRP was isolated in human osteoblast cells and identified as SFRP-1 (also known as SARP-2) and shown to be regulated by osteogenic agents in the HOB cells in a differentiation selective manner modulating the life of osteoblasts/preosteocytes.
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公开(公告)号：EP1198231A1
公开(公告)日：2002-04-24
申请号：EP00950508.2
申请日：2000-07-20
发明人： ZASK, Arie , HAUZE, Diane, Barbara,Apartment 3B , KEES, Kenneth, Lewis , COGHLAN, Richard, Dale , YARDLEY, John
IPC分类号： A61K31/195 , A61K31/4704 , A61P19/10 , C07D239/14 , C07D215/22
CPC分类号： C07D215/227 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/537 , A61K31/5377 , A61K31/54 , A61K31/541 , C07D215/26 , C07D239/14
摘要： This invention provides novel bicyclic compounds of Formula (I): wherein u, v, m, Y, G, A-B, R?1, R1a, R2, R4, R5, R5a, and R5b¿ are defined in the specification which compounds exhibit activity as inhibitors of bone resorption and compounds of Formula (II) wherein u, v, m, Y, G, D, A-B, R?1, R1a, R2, R3, R4, R5, R5a, and R5b¿ are defined in the specification which compounds exhibit activity as inhibitors of bone resorption.
摘要翻译： 本发明提供了新的式（I）双环化合物：其中u，v，m，Y，G，AB，R 1，R 1，R 2，R 4，R 5，R 5a和R 5b定义于说明书中， 作为骨吸收抑制剂的活性和其中u，v，m，Y，G，D，AB，R 1，R 1a，R 2，R 3，R 4，R 5，R 5a和R 5b定义于式 该化合物表现出作为骨吸收抑制剂的活性。
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3.发明公开CONTRACEPTIVE COMPOSITIONS CONTAINING CYCLIC CARBAMATES AND AMIDE DERIVATIVES 审中-公开避孕组合物环状氨基甲酸酯，坐落于包衍生物
公开(公告)号：EP1173253A1
公开(公告)日：2002-01-23
申请号：EP00935851.6
申请日：2000-05-01
发明人： GRUBB, Gary, S. , ZHI, Lin , JONES, Todd, K. , SANTILLI, Arthur, A. , TEGLEY, Christopher, M. , VIET, Andrew Q, , ZHANG, Puwen, , FENSOME, Andrew, , WROBEL, Jay, E. , EDWARDS, James P.
IPC分类号： A61P15/18 , A61K45/06 , A61K31/57 , A61K31/565
CPC分类号： A61K31/56 , A61K31/40 , A61K31/445 , A61K31/535 , A61K31/565 , A61K45/06 , A61K2300/00
摘要： This invention relates to cyclic combination therapies and regimens utilizing, in combination with progestins, substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure:where A and B are independent substituents selected from S, CH or N; provided that when A is S, B is CH or N; and when B is S, A is CH or N; and A and B cannot both be CH; and when A and B both equal N, one N may be optionally substituted with an C1 to C6 alkyl group; R1 and R2 are independent substituents selected from the group of H, C1 to C6 alkyl, substituted C1 to C6 alkyl, C2 to C6 alkenyl, substituted C2 to C6 alkenyl, C2 to C6 alkynyl, substituted C2 to C6 alkynyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, substituted aryl, heterocyclic, substituted heterocyclic, CORA, or NRBCORA; or R1 and R2 are fused to form optionally substituted 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic ring, the heterocyclic ring containing one to three heteroatoms selected from the group of O, S and N; or pharmaceutically useful salts thereof. These methods of treatment may be used for contraception.
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4.发明公开CONTRACEPTIVE COMPOSITIONS CONTANING INDOLONE DERIVATIVES AND PROGESTATIONAL AGENTS 审中-公开EMPFÄNGNISVERHUTENDE组合物，其吲哚酮衍生物激素和孕CONTAIN
公开(公告)号：EP1173212A1
公开(公告)日：2002-01-23
申请号：EP00930287.8
申请日：2000-05-01
发明人： GRUBB, Gary, S. , ZHI, Lin , JONES, Todd, K. , TEGLEY, Christopher, M. , FENSOME, Andrew , MILLER, Lori, L. , ULLRICH, John, W. , BENDER, Reinhold, H., W. , ZHANG, Puwen , WROBEL, Jay, E. , EDWARDS, James, P.
CPC分类号： A61K45/06 , A61K31/535 , A61K31/56 , A61K31/57 , A61K2300/00
摘要： This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having general structure (1), wherein R?1 and R2¿ may be single substituents or fused to form spirocyclic rings, in combination with progestins, estrogens, or both. These methods of treatment may be used for contraception or for the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or minimization of side effects or cyclic menstrual bleeding. Additional uses of the invention include stimulation of food intake.
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公开(公告)号：EP1171439A1
公开(公告)日：2002-01-16
申请号：EP00923540.9
申请日：2000-04-20
IPC分类号： C07D471/04 , A61K31/437 , A61P25/24
CPC分类号： C07D471/04
摘要： Compounds useful in the treatment of diseases affected by disorders of the serotonin-affected neurological systems, such as depression and anxiety, are provided having formula (I) wherein: R1 and R2 form a carbocyclic or heterocyclic ring of 5 to 7 atoms, wherein said ring may be saturated or unsaturated; and X is independently hydrogen, cyano, carbamoyl, halogen or alkoxy; or pharmaceutically acceptable salts thereof.
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6.发明授权Use of rapamycin in the manufacture of a medicament for preventing and heating hyperproliferactive vascular diseases, eventually in combination with mycophenolic acid 失效使用雷帕霉素的用于过度增殖性Gefässerkrankheiten，弓和治疗的药物中的用途可能与麦考酚酸组合
公开(公告)号：EP0691130B1
公开(公告)日：2001-12-19
申请号：EP95303150.7
申请日：1995-05-10
IPC分类号： A61K31/395
CPC分类号： A61K31/706 , A61K31/436 , A61K31/70 , A61K45/06 , A61K31/365 , A61K2300/00
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公开(公告)号：EP0678027B1
公开(公告)日：2001-11-28
申请号：EP94906461.2
申请日：1993-12-22
IPC分类号： A61K31/56
CPC分类号： A61K31/56 , A61K31/565
摘要： A method for the treatment of atherosclerosis by administering to a patient in need of anti-atherosclerotic treatment, an effective amount of 17 alpha-dihydroequilin, a C2-C6 alkanoyloxy ester thereof or a pharmaceutically acceptable salt of its sulfate or phosphate ester, in the absence of naturally occurring estrogenic steroids. A pharmaceutical composition containing 17 alpha-dihydroequilin, a C2-C6 alkanoyloxy ester thereof or a pharmaceutically acceptable salt of its sulfate or phosphate ester, in the absence of naturally occurring estrogenic steroids, and a pharmaceuticallly acceptable carrier therefor.
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公开(公告)号：EP0572542B9
公开(公告)日：2001-11-21
申请号：EP92907399.7
申请日：1992-02-21
IPC分类号： A61K35/74 , A61K31/44 , A61K31/445
CPC分类号： A61K31/70
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公开(公告)号：EP0879238B1
公开(公告)日：2001-11-14
申请号：EP97901369.5
申请日：1997-01-07
IPC分类号： C07F9/6506 , C07F9/40
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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10.发明公开
公开(公告)号：EP1151990A1
公开(公告)日：2001-11-07
申请号：EP01119663.1
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
IPC分类号： C07C255/58 , A61K31/275 , C07C225/20 , C07C233/41 , A61K31/16 , A61P9/12
CPC分类号： C07C225/20 , C07C233/41 , C07C255/58 , C07C271/24 , C07C2601/04 , C07C2601/08
摘要： The compounds of the formula:
wherein R 1 , R 2 , R 3 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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