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1. 发明授权

EP0533244B1 Amide-substituted derivatives of spiroindanylcamphorsulfonyl oxytocin antagonists 失效
标题翻译：通过酰胺基团取代Spiroindanylcamphorsulfonylderivate催产素拮抗剂
公开(公告)号：EP0533244B1
公开(公告)日：1997-12-17
申请号：EP92202724.8
申请日：1992-09-08
申请人： Merck & Co., Inc.
发明人： Bock, Mark G. , Gilbert, Kevin , Evans, Ben E. , Hobbs, Doug W. , Freidinger, Roger M. , Hoffman, James B. , Lundell, George F. , Pettibone, Douglas J.
IPC分类号： C07D401/12 , A61K31/445 , C07D401/14 , C07D221/20
CPC分类号： C07D221/20 , C07D401/12 , C07D401/14

2. 发明公开

EP0533241A3 Substituted alkyl derivatives of piperazinylcamphorsulfonyl oxytocin antagonists 失效
标题翻译：哌嗪类黄嘌呤氧合蛋白拮抗剂的取代烷基衍生物
公开(公告)号：EP0533241A3
公开(公告)日：1993-09-29
申请号：EP92202721.4
申请日：1992-09-08
申请人： MERCK & CO. INC.
发明人： Erb, Jill M. , Hoffman, James B. , Perlow, Debra S. , Williams, Peter D.
IPC分类号： C07D295/22 , C07D207/26 , C07D233/54 , C07D453/02 , C07D303/34 , C07D211/60 , C07D207/16 , A61K31/495
CPC分类号： C07D207/277 , C07C2603/66 , 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
摘要： Compounds of the formula:
where R is substituted or unsubstituted alkyl; are oxytocin antagonists useful in the treatment of preterm labor, dysmenorrhea and for the stoppage of labor preparatory to cesarean delivery. Also disclosed are pharmaceutical compositions containing these compounds, methods of their use and methods of their preparation.
摘要翻译：下式的化合物：其中R是取代或未取代的烷基; 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力。还公开了含有这些化合物的药物组合物，其使用方法及其制备方法。

3. 发明公开

EP0533241A2 Substituted alkyl derivatives of piperazinylcamphorsulfonyl oxytocin antagonists 失效
标题翻译：取代基烷基化催化剂哌嗪酰基甘油衍生物催产素拮抗剂。
公开(公告)号：EP0533241A2
公开(公告)日：1993-03-24
申请号：EP92202721.4
申请日：1992-09-08
申请人： MERCK & CO. INC.
发明人： Erb, Jill M. , Hoffman, James B. , Perlow, Debra S. , Williams, Peter D.
IPC分类号： C07D295/22 , C07D207/26 , C07D233/54 , C07D453/02 , C07D303/34 , C07D211/60 , C07D207/16 , A61K31/495
CPC分类号： C07D207/277 , C07C2603/66 , 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
摘要： Compounds of the formula:
where R is substituted or unsubstituted alkyl; are oxytocin antagonists useful in the treatment of preterm labor, dysmenorrhea and for the stoppage of labor preparatory to cesarean delivery. Also disclosed are pharmaceutical compositions containing these compounds, methods of their use and methods of their preparation.
摘要翻译：下式的化合物：其中R是取代或未取代的烷基; 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力。还公开了含有这些化合物的药物组合物，其使用方法及其制备方法。

4. 发明公开

EP0533244A1 Amide-substituted derivatives of spiroindanylcamphorsulfonyl oxytocin antagonists 失效
标题翻译： Durch eine Amide-Gruppe取代物Spiroindanylcamphorsulfonylderivate als催产素 - 拮抗剂。
公开(公告)号：EP0533244A1
公开(公告)日：1993-03-24
申请号：EP92202724.8
申请日：1992-09-08
申请人： MERCK & CO. INC.
发明人： Bock, Mark G. , Gilbert, Kevin , Evans, Ben E. , Hobbs, Doug W. , Freidinger, Roger M. , Hoffman, James B. , Lundell, George F. , Pettibone, Douglas J.
IPC分类号： C07D401/12 , A61K31/445 , C07D401/14 , C07D221/20
CPC分类号： C07D221/20 , C07D401/12 , C07D401/14
摘要： Compounds of the formula:

where R¹ is hydrogen or hydroxy and R² is a substituted amino group, a substituted heterocyclic ring or a substituted alkyl; are oxytocin and vasopressin antagonists useful in the treatment of preterm labor, dysmenorrhea and for the stoppage of labor preparatory to cesarean delivery, timing of parturition, uterine hyperactivity, endometriosis, hypertension, congestive heart failure, hyponatremia and cognitive disorders. Also disclosed are pharmaceutical compositions containing these compounds, methods of their use and methods of their preparation.
摘要翻译：式：其中R 1是氢或羟基，R 2是取代的氨基，取代的杂环或取代的烷基的式：CHEM的化合物; 是催产素和加压素拮抗剂，可用于治疗早产，痛经和停止为剖宫产分娩，分娩时间，子宫多动症，子宫内膜异位症，高血压，充血性心力衰竭，低钠血症和认知障碍的劳动。还公开了含有这些化合物的药物组合物，其使用方法及其制备方法。

5. 发明公开

EP0532097A1 Piperazinyl(sulfon)amide derivatives of camphor as oxytocin antagonists 失效
标题翻译：哌嗪基（磺酰基）酰胺衍生物冯·坎培尔·奥斯汀催产素 - 拮抗剂。
公开(公告)号：EP0532097A1
公开(公告)日：1993-03-17
申请号：EP92202689.3
申请日：1992-09-05
申请人： MERCK & CO. INC.
发明人： Bock, Mark G. , Erb, Jill M. , Hobbs, Doug W. , Hoffman, James B. , Perlow, Debra S. , Pawluczyk, Joseph M. , Veber, Daniel F. , Williams, Peter D.
IPC分类号： C07D295/22 , C07D403/12 , C07D471/08 , C07D401/12 , C07D403/10 , C07D401/04 , A61K31/495
CPC分类号： C07D207/277 , C07B59/00 , C07C2603/66 , 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
摘要： Compounds of the formula:

Compounds according to the structural formula, wherein R¹ is

(1) hydrogen,
(2) alkoxycarbonyl or
(3) unsubstituted or substituted alkyl wherein said substituent is hydroxyl, alkoxyl, carboxyl, carboxyalkyl., alkylsulfonyl or alkoxycarbonyl; and
R² is

(1) hydrogen,
(2) alkoxyl,
(3) aralkoxyl,
(4) alkoxycarbonyl,
(5) alkoxycarbonylamino,
(6) unsubstituted or substituted cycloalkyl, wherein said substituent is carboxyl,
(7) unsubstituted or substituted phenyl wherein said substituent is one or more of carboxyl, carboxyalkyl or SO₃H,
(8) unsubstituted or substituted amino, wherein said substituent is unsubstituted or substituted alkyl where said substituent is one or more of carboxyl, alkylsulfonyl or unsubstituted 5-membered heterocyclic rings having 1 or 2 heteroatoms, where said heteroatom is N,
(9) unsubstituted or substituted rings of the formulae
where said substituents are one or more of alkyl, carboxyl, carboxyalkyl, carboxyaralkyl, aralkylcarbonyl, aralkoxycarbonyl, alkoxycarbonyl, alkoxycarbonylalkyl, alkoxycarbonylaminoalkylcarbonyl, oxo or unsubstituted or substituted amino wherein said substituent is one or more of alkyl, carboxylalkyl, alkoxycarbonyl or alkoxycarbonylalkyl or
(10) unsubstituted or substituted alkyl, wherein said substituent is one or more of hydroxyl, carboxyl, carboxyalkylphenyl, alkylsulfonyl, aminocarbonyl, alkylaminocarbonyl, aralkyl, aralkoxycarbonyl, halogen, alkoxycarbonyl, alkoxycarbonylalkyl, Het or unsubstituted or substituted amino, wherein said substituent is one or more of alkyl, alkylcarbonyl, alkylsulfonyl, carboxyalkyl, Cyc, alkoxycarbonyl, alkoxycarbonylalkyl, aralkoxycarbonyl, aminocarbonylalkyl, alkylaminocarbonyl, phenalkyl or unsubstituted or substituted alkylcarbonyl, where said substituent is a 5-membered heterocyclic ring having 1 or 2 heteroatoms and where said hetero atom is N, where Het is defined as for the above heterocyclic rings and where Cyc is defined as substituted or unsubstituted cycloalkyl wherein said substituent is selected from the group consisting of alkoxycarbonyl, carboxyl, hydroxyl, oxo or spiro-dioxolinyl . 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：下式化合物：其中R 1为（1）氢，（2）烷氧基羰基或（3）未取代或取代的烷基，其中所述取代基为羟基，烷氧基，羧基，羧基烷基。，烷基磺酰基或烷氧基羰基; 并且R 2是（1）氢，（2）烷氧基，（3）芳烷氧基，（4）烷氧基羰基，（5）烷氧羰基氨基，（6）未取代或取代的环烷基，其中所述取代基是羧基，（7）取代的苯基，其中所述取代基是羧基，羧基烷基或SO 3 H中的一个或多个，（8）未取代或取代的氨基，其中所述取代基是未取代的或取代的烷基，其中所述取代基是羧基，烷基磺酰基或未取代的5元杂环中的一个或多个具有1或2个杂原子，其中所述杂原子是N，（9）未取代的或取代的式CHEM的环，其中所述取代基是烷基，羧基，羧基烷基，羧基烷基，芳烷基羰基，芳烷氧基羰基，烷氧基羰基，烷氧基羰基烷基，烷氧基羰基氨基烷基羰基，氧代或未取代或取代的氨基，其中所述取代基是烷基，羧基烷基，烷氧基羰基或烷氧基羰基烷基中的一个或多个或（10）未取代或未取代的烷基，其中所述取代基是羟基，羧基，羧基烷基苯基，烷基磺酰基，氨基羰基，烷基氨基羰基，芳烷基，芳烷氧基羰基，卤素，烷氧基羰基，烷氧基羰基烷基，Het或未取代或取代的氨基中的一个或多个，其中所述取代基是一个或多个烷基，烷基羰基，烷基磺酰基，羧基烷基，环烷基，烷氧基羰基，烷氧基羰基烷基，芳烷氧基羰基，氨基羰基烷基，烷基氨基羰基，苯烷基或未取代或取代的烷基羰基，其中所述取代基是具有1或2个杂原子的5元杂环，其中所述杂原子是N，定义为上述杂环，其中Cyc被定义为取代或未取代的环烷基，其中所述取代基选自烷氧基羰基，羧基，羟基，氧代或螺 - 二氧杂环戊烯基。这些化合物是催产素拮抗剂，可用于治疗早产，痛经和停止为剖腹产分娩的劳动。 [R

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