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公开(公告)号：US06090805A
公开(公告)日：2000-07-18
申请号：US095232
申请日：1998-06-10
申请人： Peter D. Williams , Michelle A. Sparks , Ian Bell , Debra S. Perlow , Kenneth Stauffer , Roger M. Freidinger
发明人： Peter D. Williams , Michelle A. Sparks , Ian Bell , Debra S. Perlow , Kenneth Stauffer , Roger M. Freidinger
IPC分类号： C07D413/04 , C07D413/14 , A61K31/535 , A61K31/47 , C07D215/16 , C07D265/12
CPC分类号： C07D413/04 , C07D413/14
摘要： This invention relates to certain novel benzoxazinone compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor in mammals, especially humans. The ability of the compounds to relax uterine contractions in mammals also makes them useful for treating dysmenorrhea and stopping labor prior to cesarean delivery.
摘要翻译： 本发明涉及某些新的苯并恶嗪酮化合物及其衍生物，其合成及其作为催产素受体拮抗剂的用途。 这些化合物的一种应用是在哺乳动物，特别是人类中治疗早产。 化合物放松哺乳动物子宫收缩的能力也使它们可用于治疗痛经并在剖宫产分娩前停止劳动。
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公开(公告)号：US5726172A
公开(公告)日：1998-03-10
申请号：US779296
申请日：1997-01-06
IPC分类号： C07D413/04 , C07D413/14 , C07D417/14 , C07D451/06 , C07D265/12 , A61K31/535
CPC分类号： C07D451/06 , C07D413/04 , C07D413/14 , C07D417/14
摘要： This invention relates to certain novel benzoxazinone compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor. The ability of the compounds to relax uterine contractions in mammals also makes them useful for treating dysmenorrhea and stopping labor prior to cesarean delivery. A typical compound is as follows: ##STR1##
摘要翻译： 本发明涉及某些新的苯并恶嗪酮化合物及其衍生物，其合成及其作为催产素受体拮抗剂的用途。 这些化合物的一种应用是治疗早产。 化合物放松哺乳动物子宫收缩的能力也使它们可用于治疗痛经并在剖宫产分娩前停止劳动。 典型的化合物如下：
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公开(公告)号：US5968938A
公开(公告)日：1999-10-19
申请号：US86107
申请日：1998-05-29
IPC分类号： C07D211/46 , C07D211/96 , C07D213/74 , C07D235/06 , C07D239/42 , C07D241/20 , C07D295/185 , A61K31/495 , C07D401/12 , C07D403/12
CPC分类号： C07D213/74 , C07D211/46 , C07D211/96 , C07D235/06 , C07D239/42 , C07D241/20 , C07D295/185
摘要： This invention relates to certain novel piperazine compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor in mammals, especially humans. The ability of the compounds to relax uterine contractions in mammals also makes them useful for treating dysmenorrhea and stopping labor prior to cesarean delivery.
摘要翻译： 本发明涉及某些新的哌嗪化合物及其衍生物，其合成及其作为催产素受体拮抗剂的用途。 这些化合物的一种应用是在哺乳动物，特别是人类中治疗早产。 化合物放松哺乳动物子宫收缩的能力也使它们可用于治疗痛经并在剖宫产分娩前停止劳动。
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公开(公告)号：US5648352A
公开(公告)日：1997-07-15
申请号：US451779
申请日：1995-05-26
申请人： Mark G. Bock , Jill M. Erb , Doug W. Hobbs , James B. Hoffman , Joseph M. Pawluczyk , Debra S. Perlow , Daniel F. Veber , Peter D. Williams
发明人： Mark G. Bock , Jill M. Erb , Doug W. Hobbs , James B. Hoffman , Joseph M. Pawluczyk , Debra S. Perlow , Daniel F. Veber , Peter D. Williams
IPC分类号： C07B59/00 , C07D207/16 , C07D207/26 , C07D207/277 , C07D211/58 , C07D211/60 , C07D211/62 , C07D213/38 , C07D213/74 , C07D233/54 , C07D241/08 , C07D295/26 , C07D303/34 , C07D309/14 , C07D335/02 , C07D403/12 , C07D453/02 , A61K31/495 , C07D401/12 , C07D405/12
CPC分类号： C07D207/277 , C07B59/00 , C07D207/16 , C07D211/58 , C07D211/60 , C07D211/62 , C07D213/38 , C07D213/74 , C07D233/64 , C07D241/08 , C07D295/26 , C07D303/34 , C07D309/14 , C07D335/02 , C07D403/12 , C07D453/02 , C07C2103/66
摘要： The invention is directed to a series of novel piperazinylcamphorsulfonyl compounds where the camphor ring is substituted by amides, amines, alkanes, alkenes, alkylamines, halogens, hydroxy, carboxy, alkoxycarbonyl and heterocyclic tings. Such compounds are oxytocin antagonists useful in the treatment of preterm labor, dysmenorrhea and for the stoppage of labor preparatory to cesarean delivery.
摘要翻译： 本发明涉及一系列新颖的哌嗪基樟脑磺酰化合物，其中樟脑环被酰胺，胺，烷烃，烯烃，烷基胺，卤素，羟基，羧基，烷氧基羰基和杂环取代。 这些化合物是催产素拮抗剂，可用于治疗早产，痛经和停止为剖宫产分娩的劳动。
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公开(公告)号：US5356904A
公开(公告)日：1994-10-18
申请号：US957491
申请日：1992-10-07
IPC分类号： A61K31/47
CPC分类号： A61K31/47 , Y10S514/807 , Y10S514/935
摘要： A method of inhibiting oxytocin from acting at its receptor site by administering oxytocin receptor antagonist compounds of the formula ##STR1## wherein X is oxygen or sulfur; Y is hydrogen or lower alkyl; R.sup.A is ##STR2##
摘要翻译： 一种抑制催产素通过施用式（IMAGE）的催产素受体拮抗剂化合物在其受体位点起作用的方法，其中X为氧或硫; Y是氢或低级烷基; RA是
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公开(公告)号：US5225528A
公开(公告)日：1993-07-06
申请号：US628986
申请日：1990-12-17
IPC分类号： C07K7/16
CPC分类号： C07K7/16
摘要： Disclosed are cyclic hexapeptides of the formula: ##STR1## These compounds are antagonists of oxytocin and are useful in the treatment of preterm labor and dysmenorrhea, and for stoppage of labor prepatory to Caesarian delivery. Also disclosed are pharmaceutical compositions containing the compounds of formula I and methods of preparing these compounds.
摘要翻译： 公开的是下式的环状六肽：这些化合物是催产素的拮抗剂，可用于治疗早产和痛经，并且用于停止用于切片分娩的预备剂。 还公开了含有式I化合物的药物组合物和制备这些化合物的方法。
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公开(公告)号：US5756497A
公开(公告)日：1998-05-26
申请号：US807307
申请日：1997-02-27
IPC分类号： C07D413/14 , C07D265/18 , A61K31/535
CPC分类号： C07D413/14
摘要： This invention relates to certain novel benzoxazinone compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor in mammals, especially humans. The ability of the compounds to relax uterine contractions in mammals also makes them useful for treating dysmenorrhea and stopping labor prior to cesarean delivery.
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8.发明授权Benzoxazinone and benzopyrimidinone piperidinyl tocolytic oxytocin receptor antagonists 失效苯并恶嗪酮和苯并嘧啶酮哌啶基溶血性催产素受体拮抗剂
公开(公告)号：US5665719A
公开(公告)日：1997-09-09
申请号：US470693
申请日：1995-06-06
申请人： Mark G. Bock , Ben E. Evans , Peter D. Williams , Roger M. Freidinger , Douglas J. Pettibone , Doug W. Hobbs , Paul S. Anderson
发明人： Mark G. Bock , Ben E. Evans , Peter D. Williams , Roger M. Freidinger , Douglas J. Pettibone , Doug W. Hobbs , Paul S. Anderson
IPC分类号： A61K31/4427 , A61K31/445 , A61K31/47 , A61K31/535 , A61K31/54 , A61K31/55 , A61P7/02 , A61P7/10 , A61P9/08 , A61P9/12 , A61P43/00 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D495/04 , C07D498/04 , C07D521/00 , C07F9/6558 , C07D401/02 , A61K31/545 , C07D403/02
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D495/04 , C07F9/65583
摘要： Compounds of the formula ##STR1## X is --O--, --NH-- and --NR.sup.8 --; Y is --CH.sub.2 --, --CHR.sup.8 -- and --C(R.sup.8).sub.2 --; R.sup.1 is camphor-10-yl, C.sub.1-5 alkoxyl, styryl, hydroxystyryl, furyl, unsubstituted or substituted thienyl, naphthyl, indolyl, tetrahydronaphthyl, unsubstituted, mono- or di-substituted pyridyl, pyrazinyl, unsubstituted or substituted cyclohexyl where the substituent is R.sup.4, and unsubstituted or substituted phenyl where the substituents on phenyl are R.sup.5, R.sup.6 and R.sup.7 ; R.sup.2 is hydrogen, C.sub.1-5 alkoxy, C.sub.1-5 alkyl, amino, C.sub.1-5 alkylcarbonylamino, nitro or halogen; R.sup.3 is hydrogen, C.sub.1-5 alkoxycarbonyl, cyano or carbamoyl; R.sup.4 is one to two of hydrogen, oxo, hydroxy, C.sub.1-5 alkoxy, C.sub.1-5 alkoxycarbonylamino-C.sub.1-5 alkyl and amino-C.sub.1-5 alkyl; R.sup.5, R.sup.6 are each independently selected from hydrogen, halogen, C.sub.1-5 alkyl, hydroxyl and C.sub.1-5 alkoxy; R.sup.7 is ##STR2## W is CO or SO.sub.2 ; and m is an integer from 0 to 1. Such compounds as useful as oxytocin and vasopressin receptor antagonists.
摘要翻译： 式X的化合物是-O - ， - NH-和-NR 8 - ; Y是-CH 2 - ， - CHR 8 - 和-C（R 8）2 - ; R 1是樟脑-10-基，C 1-5烷氧基，苯乙烯基，羟基苯乙烯基，呋喃基，未取代的或取代的噻吩基，萘基，吲哚基，四氢萘基，未取代的，单或二取代的吡啶基，吡嗪基，未取代或取代的环己基， R4和未取代或取代的苯基，其中苯基上的取代基是R5，R6和R7; R2是氢，C1-5烷氧基，C1-5烷基，氨基，C1-5烷基羰基氨基，硝基或卤素; R3是氢，C1-5烷氧基羰基，氰基或氨基甲酰基; R 4是氢，氧代，羟基，C 1-5烷氧基，C 1-5烷氧基羰基氨基-C 1-5烷基和氨基-C 1-5烷基中的一个到两个; R 5，R 6各自独立地选自氢，卤素，C 1-5烷基，羟基和C 1-5烷氧基; R 7是CO或SO 2; m为0至1的整数。用作催产素和加压素受体拮抗剂的化合物。
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公开(公告)号：US06528503B2
公开(公告)日：2003-03-04
申请号：US10171708
申请日：2002-06-14
申请人： Peter D. Williams , Terry A. Lyle , Matthew M. Morrissette , Lekhanh O. Tran , Donnette D. Staas
发明人： Peter D. Williams , Terry A. Lyle , Matthew M. Morrissette , Lekhanh O. Tran , Donnette D. Staas
IPC分类号： A61K31397
CPC分类号： C07D401/06 , A61K38/00 , C07D205/04 , C07D207/16 , C07D403/12 , C07K5/06078 , C07K5/06139 , C07K5/06191
摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, e.g. 1-(3(S)-Cyclopropyl-2(R)-hydroxybutanoyl)azetidine-2(S)-N-(2-aminomethyl-5-chlorobenzyl)carboxamide, and 1-(3-Cyclopropyl-3-methyl-2(R)-hydroxybutanoyl)azetidine-2(S)-N-(2-aminomethyl-5-chlorobenzyl)carboxamide.
摘要翻译： 本发明的化合物可用于抑制具有以下结构的凝血酶和相关的血栓闭塞：或其药学上可接受的盐，例如， 1-（3-（S） - 环丙基-2（R） - 羟基丁酰基）氮杂环丁烷-2（S）-N-（2-氨基甲基-5-氯苄基）甲酰胺和1-（3-环丙基-3-甲基-2 （R） - 羟基丁酰基）氮杂环丁烷-2（S）-N-（2-氨基甲基-5-氯苄基）甲酰胺。
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公开(公告)号：US6087373A
公开(公告)日：2000-07-11
申请号：US157964
申请日：1998-09-21
申请人： Craig Coburn , Joseph P. Vacca , Peter D. Williams
发明人： Craig Coburn , Joseph P. Vacca , Peter D. Williams
IPC分类号： A61P9/10 , C07D471/04 , A61K31/4375
CPC分类号： C07D471/04
摘要： A compound which inhibits human thrombin and which has the general structure ##STR1##
摘要翻译： 一种抑制人凝血酶并具有一般结构的化合物
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