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1. 发明授权

US5464788A Tocolytic oxytocin receptor antagonists 失效
标题翻译：溶血性催产素受体拮抗剂
公开(公告)号：US5464788A
公开(公告)日：1995-11-07
申请号：US217270
申请日：1994-03-24
申请人： Mark G. Bock , Ben E. Evans , J. Christopher Culberson , Kevin F. Gilbert , Kenneth E. Rittle , Peter D. Williams
发明人： Mark G. Bock , Ben E. Evans , J. Christopher Culberson , Kevin F. Gilbert , Kenneth E. Rittle , Peter D. Williams
IPC分类号： A61K31/435 , A61K31/4427 , A61K31/445 , A61K31/451 , A61K31/495 , A61P7/02 , A61P7/10 , A61P9/08 , A61P9/12 , A61P43/00 , C07D211/46 , C07D221/20 , C07D235/06 , C07D241/04 , C07D241/08 , C07D295/096 , C07D401/12 , C07D401/14 , C07D403/12 , C07D273/00 , C07D413/00 , C07D451/00
CPC分类号： C07D221/20 , C07D235/06 , C07D241/04 , C07D241/08 , C07D295/096 , C07D401/12 , C07D401/14 , C07D403/12
摘要： Compounds of the formula X--Y--R, or the pharmaceutically acceptable salts and esters thereof, wherein X is ##STR1## Y is --SO.sub.2 --, --(CH.sub.2).sub.p -- or --CO--(CH.sub.2).sub.p --; R is unsubstituted or substituted phenyl where said substitutents are one or more of R.sup.5, R.sup.6 or R.sup.7 ; R.sup.1 is hydrogen, cyano, phenyl,--CONHR.sup.2, --CONR.sup.2 R.sup.2, --(CH.sub.2).sub.m --OR.sup.2, --(CH.sub.2).sub.p --S(O).sub.r --R.sup.2, --(CH.sub.2).sub.m --CO.sub.2 R.sup.2, --(CH.sub.2).sub.m --N.sub.3, --(CH.sub.2).sub.m --NH.sub.2 or --(CH.sub.2).sub.m --NR.sup.2 R.sup.2 ; R.sup.2 is hydrogen, C.sub.3-8 cycloalkyl or C.sub.1-5 alkyl; R.sup.5 and R.sup.6 are each independently selected from hydrogen, C.sub.1-5 alkoxy, halogen or --(CH.sub.2).sub.n --N(R.sup.2)--C(O)--R.sup.18 ; R.sup.7 is hydrogen or ##STR2## R.sup.11 is selected from hydrogen, C.sub.1-5 alkylcarbonyl, ##STR3## or substituted C.sub.1-5 alkyl wherein said alkyl substituent is unsubstituted, mono-, di- or tri-substituted pyridyl wherein said substitutents on said pyridyl are independently selected from halogen, C.sub.1-5 alkyl or C.sub.1-5 alkoxyl; R.sup.13 is unsubstituted or substituted C.sub.1-10 alkyl wherein the substituent is selected from --N(R.sup.2).sub.2, --NHR.sup.2 or imidazolyl; R.sup.14 and R.sup.15 are each independently selected from C.sub.1-5 alkyl, C.sub.1-5 alkoxy or halogen; R.sup.16 is hydrogen or oxo; R.sup.18 is C.sub.1-5 alkoxyl, unsubstituted or substituted C.sub.1-5 alkyl where said substituent is Het, unsubstituted or substituted C.sub.2-5 alkenyl where said subsituent is Het or Het; Het is benzimidazolyl, carboxymethyl-substituted benzimidazolyl or indolyl; m is an integer of from 1 to 5; p is an integer of from 1 to 3; and r is an integer of from 0 to 2. Such compounds as useful as oxytocin and vasopressin receptor antagonists.
摘要翻译：式X-Y-R化合物或其药学上可接受的盐和酯，其中X为Y是-SO 2 - ， - （CH 2）p - 或-CO-（CH 2）p - ; R是未取代或取代的苯基，其中所述取代基是R5，R6或R7中的一个或多个; R 1是氢，氰基，苯基，-CONHR 2，-CONR 2 R 2， - （CH 2）m OR 2， - （CH 2）pS（O）r -R 2， - （CH 2）m -CO 2 R 2， - （CH 2）m -N 3， - （CH 2）m -NH 2或 - （CH 2）m -NR 2 R 2; R2是氢，C3-8环烷基或C1-5烷基; R 5和R 6各自独立地选自氢，C 1-5烷氧基，卤素或 - （CH 2）n -N（R 2）-C（O）-R 18; R 7是氢或者R 11选自氢，C 1-5烷基羰基，或者被取代的C 1-5烷基，其中所述烷基取代基是未被取代的，一取代，二取代或三取代的吡啶基，其中所述吡啶基独立地选自卤素，C 1-5烷基或C 1-5烷氧基; R 13是未取代的或取代的C 1-10烷基，其中取代基选自-N（R 2）2，-NHR 2或咪唑基; R 14和R 15各自独立地选自C 1-5烷基，C 1-5烷氧基或卤素; R 16是氢或氧代; R 18为C 1-5烷氧基，未取代或取代的C 1-5烷基，其中所述取代基为Het，未取代或取代的C2-5烯基，其中所述取代基为Het或Het; Het是苯并咪唑基，羧甲基取代的苯并咪唑基或吲哚基; m为1〜5的整数， p为1〜3的整数，并且r是0至2的整数。用作催产素和加压素受体拮抗剂的这类化合物。

2. 发明授权

US5756504A Tocolytic oxytocin receptor antagonists 失效
标题翻译：溶血性催产素受体拮抗剂
公开(公告)号：US5756504A
公开(公告)日：1998-05-26
申请号：US718415
申请日：1996-09-23
申请人： Mark G. Bock , Ben E. Evans , J. Christopher Culberson , Kevin F. Gilbert , Kenneth E. Rittle , Peter D. Williams
发明人： Mark G. Bock , Ben E. Evans , J. Christopher Culberson , Kevin F. Gilbert , Kenneth E. Rittle , Peter D. Williams
IPC分类号： A61K31/435 , A61K31/4427 , A61K31/445 , A61K31/451 , A61K31/495 , A61P7/02 , A61P7/10 , A61P9/08 , A61P9/12 , A61P43/00 , C07D211/46 , C07D221/20 , C07D235/06 , C07D241/04 , C07D241/08 , C07D295/096 , C07D401/12 , C07D401/14 , C07D403/12
CPC分类号： C07D221/20 , C07D235/06 , C07D241/04 , C07D241/08 , C07D295/096 , C07D401/12 , C07D401/14 , C07D403/12
摘要： Compounds of the formula X--Y--R, or the pharmaceutically acceptable salts and esters thereof, wherein X is ##STR1## Y is --SO.sub.2 --, --(CH.sub.2).sub.p -- or --CO--(CH.sub.2).sub.p --; R is unsubstituted or substituted phenyl where said substitutents are one or more of R.sup.5, R.sup.6 or R.sup.7 ; R.sup.1 is hydrogen, cyano, phenyl, --CONHR.sup.2, --CONR.sup.2 R.sup.2, --(CH.sub.2).sub.m --OR.sup.2, --(CH.sub.2).sub.p --S(O).sub.r --R.sup.2, --(CH.sub.2).sub.m --CO.sub.2 R.sup.2, --(CH.sub.2).sub.m --N.sub.3, --(CH.sub.2).sub.m --NH.sub.2 or --(CH.sub.2).sub.m --NR.sup.2 R.sup.2 ; R.sup.2 is hydrogen, C.sub.3-8 cycloalkyl or C.sub.1-5 alkyl; R.sup.5 and R.sup.6 are each independently selected from hydrogen, C.sub.1-5 alkoxy, halogen or --(CH.sub.2).sub.n --N(R.sup.2)--C(O)--R.sup.18 ; R.sup.7 is hydrogen or ##STR2## R.sup.11 is selected from hydrogen, C.sub.1-5 alkyl-carbonyl, --Z--R.sup.13, ##STR3## or substituted C.sub.1-5 alkyl wherein said alkyl substituent is unsubstituted, mono-, di- or tri-substituted pyridyl wherein said substitutents on said pyridyl are independently selected from halogen, C.sub.1-5 alkyl or C.sub.1-5 alkoxyl; R.sup.13 is unsubstituted or substituted C.sub.1-10 alkyl wherein the substituent is selected from --N(R.sup.2).sub.2, --NHR.sup.2 or imidazolyl; R.sup.14 and R.sup.15 are each independently selected from C.sub.1-5 alkyl, C.sub.1-5 alkoxy or halogen; R.sup.16 is hydrogen or oxo; R.sup.18 is C.sub.1-5 alkoxyl, unsubstituted or substituted C.sub.1-5 alkyl where said substituent is Het, unsubstituted or substituted C.sub.2-5 alkenyl where said subsituent is Het or Het; Het is benzimidazolyl, carboxymethyl-substituted benzimidazolyl or indolyl; m is an integer of from 1 to 5; p is an integer of from 1 to 3; and r is an integer of from 0 to 2. Such compounds as useful as oxytocin and vasopressin receptor antagonists.
摘要翻译： PCT No.PCT / US95 / 03738 Sec。 371日期1996年9月23日 102（e）1996年9月23日PCT 1995年3月23日PCT公布。 WO95 / 25443 PCT出版物日期为1995年9月28日，式X-Y-R或其药学上可接受的盐和酯的化合物，其中X为Y 2 - ， - （CH 2）p - 或-CO-（CH 2）p - ; R是未取代或取代的苯基，其中所述取代基是R5，R6或R7中的一个或多个; R 1是氢，氰基，苯基，-CONHR 2，-CONR 2 R 2， - （CH 2）m OR 2， - （CH 2）pS（O）r -R 2， - （CH 2）m -CO 2 R 2， - （CH 2）m -N 3， - （CH 2）m -NH 2或 - （CH 2）m -NR 2 R 2; R2是氢，C3-8环烷基或C1-5烷基; R 5和R 6各自独立地选自氢，C 1-5烷氧基，卤素或 - （CH 2）n -N（R 2）-C（O）-R 18; R 7是氢或R 11选自氢，C 1-5烷基 - 羰基，-Z-R 13，取代基是未取代的，一取代，二取代或三取代的吡啶基，其中所述吡啶基上的所述取代基独立地选自卤素，C 1-5烷基或C 1-5烷氧基; R 13是未取代的或取代的C 1-10烷基，其中取代基选自-N（R 2）2，-NHR 2或咪唑基; R 14和R 15各自独立地选自C 1-5烷基，C 1-5烷氧基或卤素; R 16是氢或氧代; R 18是C 1-5烷氧基，未取代或取代的C 1-5烷基，其中所述取代基是Het，未取代或取代的C2-5烯基，其中所述取代基是Het或Het; Het是苯并咪唑基，羧甲基取代的苯并咪唑基或吲哚基; m为1〜5的整数， p为1〜3的整数，并且r是0至2的整数。用作催产素和加压素受体拮抗剂的这类化合物。

3. 发明授权

US5665719A Benzoxazinone and benzopyrimidinone piperidinyl tocolytic oxytocin receptor antagonists 失效
标题翻译：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。

4. 发明授权

US5206237A Benzodiazepine analogs 失效
标题翻译：苯并嗪类似物
公开(公告)号：US5206237A
公开(公告)日：1993-04-27
申请号：US699849
申请日：1991-05-14
申请人： Roger M. Freidinger , Mark G. Bock , Ben E. Evans
发明人： Roger M. Freidinger , Mark G. Bock , Ben E. Evans
IPC分类号： A61K31/55 , A61K31/551 , A61P25/04 , A61P25/20 , A61P25/30 , A61P27/02 , A61P35/00 , C07D243/14 , C07D401/12 , C07D403/04
CPC分类号： A61K31/55
摘要： Pharmaceutical compositions containing benzodiazepines of the formula: ##STR1## are disclosed which are useful in the treatment of panic disorder or anxiety disorder.

5. 发明授权

US5204349A Amide-substituted derivatives of spiroindanylcamphorsulfonyl oxytocin antagonists 失效
标题翻译：螺旋体丹参酮氧基氧化物拮抗剂的酰胺取代衍生物
公开(公告)号：US5204349A
公开(公告)日：1993-04-20
申请号：US760284
申请日：1991-09-16
申请人： Mark G. Bock , Ben E. Evans , Roger M. Freidinger , Kevin Gilbert , Doug W. Hobbs , James B. Hoffman , George F. Lundell , Douglas J. Pettibone
发明人： Mark G. Bock , Ben E. Evans , Roger M. Freidinger , Kevin Gilbert , Doug W. Hobbs , James B. Hoffman , George F. Lundell , Douglas J. Pettibone
IPC分类号： A61K31/435 , A61K31/495 , A61P13/02 , A61P15/00 , C07D221/20 , C07D401/12 , C07D401/14
CPC分类号： C07D221/20 , C07D401/12 , C07D401/14
摘要： Compounds of the formula: ##STR1## where R.sup.1 is hydrogen or hydroxy and R.sup.2 is a substituted amino group, a substituted heterocyclic ring or a substituted alkyl. These compounds 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.

6. 发明授权

US5166151A 2-Benzazepines with 5- and 6-membered heterocyclic rings, compositions and medical methods of use thereof 失效
标题翻译：具有5-和6-元杂环的2-苯并氮杂，其组合物和医用方法
公开(公告)号：US5166151A
公开(公告)日：1992-11-24
申请号：US668353
申请日：1991-03-11
申请人： Roger M. Freidinger , Ben E. Evans , Mark G. Bock
发明人： Roger M. Freidinger , Ben E. Evans , Mark G. Bock
IPC分类号： C07D487/04 , C07D498/04 , C07D513/04
CPC分类号： C07D487/04 , C07D513/04
摘要： Aromatic 2-benzazepines with fused 5- or 6-membered heterocyclic rings which are antagonists of cholecystokinins and/or gastrin, and are useful in the treatment or prevention of CCK-related and/or gastrin-related disorders of the gastrointestinal, central nervous and appetite regulatory systems; compositions comprising these compounds; and methods of treatment of mammals or of increasing food intake of animals employing these compounds.
摘要翻译：具有作为缩胆囊素和/或胃泌素拮抗剂的稠合的5-或6-元杂环的芳族2-苯并吖庚因，可用于治疗或预防胃肠道，中枢神经和/或胃肠激素的CCK相关和/或胃泌素相关疾病食欲调节系统; 包含这些化合物的组合物; 哺乳动物的治疗方法或使用这些化合物的动物的食物摄入量增加。

7. 发明授权

US5004741A Methods of antagonizing CCK or gastrin with benzodiazepine analogs 失效
标题翻译：用苯并二氮杂类似物拮抗CCK或胃泌素的方法
公开(公告)号：US5004741A
公开(公告)日：1991-04-02
申请号：US269212
申请日：1988-11-09
申请人： Ben E. Evans , Mark G. Bock , Roger M. Freidinger
发明人： Ben E. Evans , Mark G. Bock , Roger M. Freidinger
IPC分类号： A61K31/55 , A61K38/00 , C07C271/22 , C07D209/20 , C07D209/48 , C07D243/16 , C07D243/20 , C07D243/22 , C07D243/24 , C07D243/26 , C07D243/28 , C07D243/36 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07K5/06 , C07K5/065 , C07K5/078 , C07K5/097
CPC分类号： C07C271/22 , C07D209/20 , C07D209/48 , C07D243/16 , C07D243/20 , C07D243/22 , C07D243/24 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07K5/06078 , C07K5/06139 , C07K5/06191 , C07K5/0821 , A61K38/00 , Y10S514/925 , Y10S514/926 , Y10S514/927
摘要： Methods of antagonizing gastrin and/or cholecystokinin (CCK) with benzodiazepine analogs are disclosed, as well as related pharmaceutical compositions, which are useful in treating disorders of the gastrointestinal tract, central nervous system, and of the appetite.
摘要翻译：公开了用苯并二氮杂类似物拮抗胃泌素和/或胆囊收缩素（CCK）的方法，以及可用于治疗胃肠道疾病，中枢神经系统和食欲的相关药物组合物。

8. 发明授权

US4847248A 1,4-Benzodiazepines with 5- and 6-membered heterocyclic rings and their use as cholecystokinins and gastrin antagonists 失效
标题翻译：具有5-和6-元杂环的1,4-苯并二氮杂类及其作为缩胆囊素和胃泌素拮抗剂的用途
公开(公告)号：US4847248A
公开(公告)日：1989-07-11
申请号：US141435
申请日：1988-01-06
申请人： Roger M. Freidinger , Ben E. Evans , Mark G. Bock
发明人： Roger M. Freidinger , Ben E. Evans , Mark G. Bock
IPC分类号： C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： Aromatic 1,4-benzodiazepines with fused 5- or 6-membered heterocyclic rings which are antagonists of cholecystokinins and/or gastrin, and are useful in the treatment or prevention of CCK-related and/or gastrin-related disorders of the gastrointestinal, central nervous and appetite regulatory systems; compositions comprising these compounds; and methods of treatment employing these compounds.
摘要翻译：具有稠合的5-或6-元杂环的芳族1,4-苯并二氮杂，其是缩胆囊素和/或胃泌素的拮抗剂，并且可用于治疗或预防胃肠道，中枢的CCK相关和/或胃泌素相关疾病紧张和食欲调节系统; 包含这些化合物的组合物; 和使用这些化合物的治疗方法。

9. 发明授权

US5210082A 2-benzazepines with 5- and 6-membered heterocyclic rings to treat pain and anxiety disorders 失效
标题翻译：具有5-和6-成员的杂环环的2-苯并嗪治疗疼痛和恶心病
公开(公告)号：US5210082A
公开(公告)日：1993-05-11
申请号：US701275
申请日：1991-05-16
申请人： Mark G. Bock , Ben E. Evans , Roger M. Freidinger
发明人： Mark G. Bock , Ben E. Evans , Roger M. Freidinger
IPC分类号： C07D487/04 , A61K31/55 , A61P25/20 , A61P43/00 , C07D498/04 , C07D513/04
CPC分类号： A61K31/55
摘要： Pharmaceutical compositions containing aromatic 2-benzazepines with fused 5- or 6-membered heterocyclic rings are disclosed which are useful in the treatment of panic disorder or anxiety disorder.

10. 发明授权

US5206234A Benzolactam analogs as antagonists of CCK 失效
标题翻译：作为CCK的拮抗剂的BENZOLACTAM类似物
公开(公告)号：US5206234A
公开(公告)日：1993-04-27
申请号：US718075
申请日：1991-06-20
申请人： Mark G. Bock , Roger M. Freidinger , Ben E. Evans
发明人： Mark G. Bock , Roger M. Freidinger , Ben E. Evans
IPC分类号： A61K31/55 , A61K38/00 , A61P1/00 , A61P25/04 , A61P25/20 , A61P27/02 , A61P35/00 , C07D223/16 , C07D403/12 , C07K5/078
CPC分类号： C07D223/16 , C07K5/06139 , A61K38/00
摘要： Benzolactam analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).

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