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1.发明授权2-[(Aminophenyl and amidophenyl)amino]-1-azacycloalkanes having antidiarrheal activity 失效2 - 具有止泻活性的[（氨基苯基和氨基苯基）氨基] -1-氮杂环烷烃
公开(公告)号：US4533739A
公开(公告)日：1985-08-06
申请号：US433922
申请日：1982-10-12
IPC分类号： A61K31/445 , A61K31/55 , A61P1/12 , C07C67/00 , C07C231/00 , C07C233/43 , C07D207/22 , C07D207/40 , C07D211/72 , C07D223/12 , C07D207/18
CPC分类号： C07D211/72 , C07D207/22 , C07D223/12 , Y10S514/867
摘要： This invention relates to the novel use of certain aromatic substituted amidines as antidiarrheals.
摘要翻译： 本发明涉及某些芳族取代的脒类作为止泻药的新用途。
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公开(公告)号：US4579951A
公开(公告)日：1986-04-01
申请号：US590663
申请日：1984-03-19
IPC分类号： A61K31/40 , A61K31/445 , A61P1/12 , C07C67/00 , C07C213/00 , C07C217/86 , C07D207/22 , C07D211/72 , C07D407/12 , C07D211/56 , C07D207/14
CPC分类号： C07D407/12 , C07D207/22
摘要： This invention relates to novel substituted (azacycloalk-2-yl)iminophenols that are useful in the treatment of diarrhea.
摘要翻译： 本发明涉及可用于治疗腹泻的新的取代的（氮杂环烷-2-基）亚氨基酚。
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公开(公告)号：US4758675A
公开(公告)日：1988-07-19
申请号：US14339
申请日：1987-02-13
IPC分类号： A61K38/00 , C07K5/065 , C07D333/22
CPC分类号： C07K5/06078 , A61K38/00
摘要： This invention relates to novel 3-thiophene-substituted tryosyl dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable addition salts thereof, wherein R.sup.1 is --OH, benzyloxy, or --OCH.sub.3 ; wherein R.sub.2 and R.sub.3 may be the same or different and represent lower alkyl of 1-6 carbon atoms; wherein R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 may be the same or different and represent hydrogen or lower alkyl of 1-6 carbon atoms; wherein "v" represents an asymmetric carbon atom that may be racemic or that may have the D or L configuration; and wherein "w" represents an asymmetric carbon atom that has the D configuration. These compounds are useful as analgesic agents.
摘要翻译： 本发明涉及下式的新型3-噻吩取代的甜蛋白二肽酰胺及其药学上可接受的加成盐，其中R1是-OH，苄氧基或-OCH3; 其中R2和R3可以相同或不同，代表1-6个碳原子的低级烷基; 其中R4，R5，R6，R7，R8和R9可以相同或不同，代表氢或1-6个碳原子的低级烷基; 其中“v”表示可以是外消旋的或可具有D或L构型的不对称碳原子; 并且其中“w”表示具有D构型的不对称碳原子。 这些化合物可用作止痛剂。
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公开(公告)号：US4933325A
公开(公告)日：1990-06-12
申请号：US145953
申请日：1988-01-20
CPC分类号： C07K5/06078 , A61K38/00
摘要： The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is hydrogen, lower alkyl, hydroxy, --OCO.sub.2 lower alkyl, lower alkoxy, --O(CH.sub.2).sub.n -phenyl with the phenyl optionally substituted by halogen, --NO.sub.2, --CN, --NH.sub.2 or lower alkyl wherein n is 1 to 4; R.sup.2 and R.sup.3 represent lower alkyl, halogen, or lower alkoxy, or either one of R.sup.2 or R.sup.3 is hydrogen and the other is lower alkyl, lower alkoxy or halogen; R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 may be the same or different and represent hydrogen or lower alkyl; R.sup.10 is selected from the gorup consisting of--(ALK)Xwhere ALK represents alkylene, thioalkylene, oxyalkylene, having 1 to 5 carbon atoms; alkenylene and alkynylene having 2 to 4 carbon atoms; and X represents pyridyl, pyrimidinyl, 9H-fluoren-9-yl, diphenylmethyl, thienyl, carboxy, lower alkoxy carbonyl, substituted phenyl wherein the phenyl substituent is amino, hydroxy, halogen, nitro, methylenedioxy, lower alkyl, carboxy, lower alkoxycarbonyl, lower alkoxy, carboxamide, diloweralkylamino or X represents phenyl when ALK is not alkylene; or R.sup.10 is ##STR2## where p and q are independently 1 to 4; or R.sup.9 and R.sup.10 together with N is ##STR3## where r and t are independently 1 to 4;v represents an asymmetric carbon that may be racemic or have the D or L configuration;w represents an asymmetric carbon when R.sup.7 and R.sup.8 are not the same that may be racemic or have the D or L configuration.These compounds are useful as analgesic and/or antihypertensive compounds.
摘要翻译： 本发明涉及下式的新型取代的酪氨酰丙氨酸二肽酰胺及其药学上可接受的酸加成盐，其中R 1是氢，低级烷基，羟基，-OCO 2低级烷基，低级烷氧基，-O（CH 2）n - 苯基，其中任选被卤素取代的苯基，-NO 2，-CN，-NH 2或其中n为1至4的低级烷基; R2和R3表示低级烷基，卤素或低级烷氧基，或R2或R3中的任一个为氢，另一个为低级烷基，低级烷氧基或卤素; R 4，R 5，R 6，R 7，R 8和R 9可以相同或不同，表示氢或低级烷基; R10选自 - （ALK）X，其中ALK表示亚烷基，硫代亚烷基，氧化烯，具有1至5个碳原子; 具有2至4个碳原子的亚烯基和亚炔基; 羟基，卤素，硝基，亚甲二氧基，低级烷基，羧基，低级烷氧基羰基，低级烷氧基羰基，低级烷氧基羰基， 低级烷氧基，甲酰胺，二低级烷基氨基或X代表苯基，当ALK不是亚烷基时; 或R10为
，其中p和q独立地为1至4; 或R 9和R 10与N一起为 ，其中r和t独立地为1至4; v表示可以是外消旋或具有D或L构型的不对称碳; 当R7和R8不相同时，w表示不对称碳，可以是外消旋的或具有D或L构型。 这些化合物可用作镇痛和/或抗高血压化合物。 -
5.发明授权Fluorenyl substituted tyrosyl dipeptide amides which are useful in treating pain 失效可用于治疗疼痛的芴基取代的酪氨酰二肽酰胺
公开(公告)号：US4847241A
公开(公告)日：1989-07-11
申请号：US145954
申请日：1988-01-20
CPC分类号： C07K5/06078 , A61K38/00
摘要： The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is hydrogen, lower alkyl, hydroxy, --OCO.sub.2 lower alkyl, lower alkoxy, --O(CH.sub.2).sub.n --phenyl with the phenyl optionally substituted by halogen, --NO.sub.2, --CN, --NH.sub.2 or lower alkyl wherein n is 1 to 4; R.sup.2 and R.sup.3 represent lower alkyl, halogen, or lower alkoxy, or either one of R.sup.2 or R.sup.3 is hydrogen and the other is lower alkyl, lower alkoxy or halogen; R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 may be the same or different and represent hydrogen or lower alkyl; R.sup.10 is selected from the group consisting of--(ALK)Xwhere ALK represents alkylene, thioalkylene, oxyalkylene, having 1 to 5 carbon atoms; alkenylene and alkynylene having 2 to 4 carbon atoms; and X represents pyridyl, pyrimidinyl, 9H-fluoren-9-yl, diphenylmethyl, thienyl, carboxy, lower alkoxy carbonyl, substituted phenyl wherein the phenyl substitutent is amino, hydroxy, halogen, nitro, methylenedioxy, lower alkyl, carboxy, lower alkoxycarbonyl, lower alkoxy, carboxamide, diloweralkylamino or X represents phenyl when ALK is not alkylene; or R.sup.10 is ##STR2## where p and q are independently 1 to 4; or R.sup.9 and R.sup.10 together with N is ##STR3## where r and t are independently 1 to 4; v represents an symmetric carbon that may be racemic or have the D or L configuration; w represents an asymmetric carbon when R.sup.7 and R.sup.8 are not the same that may be racemic or have the D or L configuration. These compounds are useful as analgesic and/or antihypertensive compounds.
摘要翻译： 本发明涉及下式的新型取代的酪氨酰丙氨酸二肽酰胺及其药学上可接受的酸加成盐，其中R 1是氢，低级烷基，羟基，-OCO 2低级烷基，低级烷氧基，-O（CH 2）n - 苯基，其中任选被卤素取代的苯基，-NO 2，-CN，-NH 2或其中n为1至4的低级烷基; R2和R3表示低级烷基，卤素或低级烷氧基，或R2或R3中的任一个为氢，另一个为低级烷基，低级烷氧基或卤素; R 4，R 5，R 6，R 7，R 8和R 9可以相同或不同，表示氢或低级烷基; R 10选自 - （ALK）X，其中ALK表示亚烷基，硫代亚烷基，氧化烯，具有1至5个碳原子; 具有2至4个碳原子的亚烯基和亚炔基; 羟基，卤素，硝基，亚甲二氧基，低级烷基，羧基，低级烷氧基羰基，低级烷氧基羰基，低级烷氧基羰基， 低级烷氧基，甲酰胺，二低级烷基氨基或X代表苯基，当ALK不是亚烷基时; 或R10为
，其中p和q独立地为1至4; 或R 9和R 10与N一起为 ，其中r和t独立地为1至4; v表示可以是外消旋或具有D或L构型的对称碳; 当R7和R8不相同时，w表示不对称碳，可以是外消旋的或具有D或L构型。 这些化合物可用作镇痛和/或抗高血压化合物。 -
公开(公告)号：US4822775A
公开(公告)日：1989-04-18
申请号：US882794
申请日：1986-07-14
IPC分类号： A61K38/00 , C07K5/065 , A61K31/34 , C07D317/54 , C07D317/58 , C07K5/06
CPC分类号： C07K5/06078 , A61K38/00
摘要： The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is hydrogen, lower alkyl, hydroxy, --OCO.sub.2 lower alkyl, lower alkoxy, --O(CH.sub.2).sub.n -phenyl with the phenyl optionally substituted by halogen, --NO.sub.2, --CN, --NH.sub.2 or lower alkyl wherein n is 1 to 4; R.sup.2 and R.sup.3 represent lower alkyl, halogen, or lower alkoxy, or either one of R.sup.2 or R.sup.3 is hydrogen and the other is lower alkyl, lower alkoxy or halogen; R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 may be the same or different and represent hydrogen or lower alkyl; R.sup.10 is selected from the group consisting of--(ALK)Xwhere ALK represents alkylene, thioalkylene, oxyalkylene, having 1 to 5 carbon atoms; alkenylene and alkynylene having 2 to 4 carbon atoms; and X represents pyridyl, pyrimidinyl, 9H-fluoren-9-yl, diphenylmethyl, thienyl, carboxy, lower alkoxy carbonyl, substituted phenyl wherein the phenyl substituent is amino, hydroxy, halogen, nitro, methylenedioxy, lower alkyl, carboxy, lower alkoxycarbonyl, lower alkoxy, carboxamide, diloweralkylamino or X represents phenyl, when ALK is not alkylene; or R.sup.10 is ##STR2## where p and q are independently 1 to 4; or R.sup.9 and R.sup.10 together with N is ##STR3## where r and t are independently 1 to 4;v represents an asymmetric carbon that may be racemic or have the D or L configuration;w represents an asymmetric carbon when R.sup.7 and R.sup.8 are not the same that may be racemic or have the D or L configuration.These compounds are useful as analgesic and/or antihypertensive compounds.
摘要翻译： 本发明涉及下式的新型取代的酪氨酰丙氨酸二肽酰胺及其药学上可接受的酸加成盐，其中R 1是氢，低级烷基，羟基，-OCO 2低级烷基，低级烷氧基，-O（CH 2）n - 苯基，其中任选被卤素取代的苯基，-NO 2，-CN，-NH 2或其中n为1至4的低级烷基; R2和R3表示低级烷基，卤素或低级烷氧基，或R2或R3中的任一个为氢，另一个为低级烷基，低级烷氧基或卤素; R 4，R 5，R 6，R 7，R 8和R 9可以相同或不同，表示氢或低级烷基; R 10选自 - （ALK）X，其中ALK表示亚烷基，硫代亚烷基，氧化烯，具有1至5个碳原子; 具有2至4个碳原子的亚烯基和亚炔基; 羟基，卤素，硝基，亚甲二氧基，低级烷基，羧基，低级烷氧基羰基，低级烷氧基羰基，低级烷氧基羰基， 当ALK不是亚烷基时，低级烷氧基，羧酰胺，二低级烷基氨基或X代表苯基; 或R10为
，其中p和q独立地为1至4; 或R 9和R 10与N一起为 ，其中r和t独立地为1至4; v表示可以是外消旋或具有D或L构型的不对称碳; 当R7和R8不相同时，w表示不对称碳，可以是外消旋的或具有D或L构型。 这些化合物可用作镇痛和/或抗高血压化合物。 -
公开(公告)号：US4797470A
公开(公告)日：1989-01-10
申请号：US14340
申请日：1987-02-13
申请人： Barnett S. Pitzele , Donald W. Hansen, Jr. , Robert W. Hamilton , Daniel R. Pilipauskas , Michael Clare
发明人： Barnett S. Pitzele , Donald W. Hansen, Jr. , Robert W. Hamilton , Daniel R. Pilipauskas , Michael Clare
CPC分类号： C07K5/06078 , A61K38/00
摘要： This invention relates to compounds of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is ##STR2## where X is oxygen or sulfur, Y is oxygen or nitrogen, and R.sup.11 represents straight or branched chain lower alkenyl having 2-6 carbon atoms, or phenyl, benzyl, and their equivalents such as nitro, halogen, or lower alkyl or lower alkoxy substituted phenyl or benzyl; wherein R.sup.2 and R.sup.3 may be the same or different and represent straight or branched chain lower alkyl having 1-6 carbon atoms, wherein R.sup.4 -R.sup.9 may be the same or different and represent hydrogen, or straight or branched chain lower alkyl having 1-6 carbon atoms; wherein C.sub.w is an asymmetric carbon atom when R.sup.7 and R.sup.8 are not the same and may be racemic or have the D or L configuration; and wherein C.sup.v is an asymmetric carbon atom and may be racemic or may have the D or L configuration.The compounds of this invention are useful because they possess analgesic activity in mammals.
摘要翻译： 本发明涉及下式的化合物及其药学上可接受的酸加成盐，其中R 1为X，其中X为氧或硫，Y为氧或氮，R11为直链或支链低级烯基，其具有2 -6个碳原子，或苯基，苄基及其等同物如硝基，卤素或低级烷基或低级烷氧基取代的苯基或苄基; 其中R2和R3可以相同或不同，表示具有1-6个碳原子的直链或支链低级烷基，其中R4-R9可以相同或不同，表示氢，或具有1-6个碳原子的直链或支链低级烷基 碳原子 其中当R 7和R 8不相同时，C w是不对称碳原子，并且可以是外消旋的或具有D或L构型; 并且其中Cv是不对称碳原子并且可以是外消旋的或可以具有D或L构型。 本发明的化合物是有用的，因为它们在哺乳动物中具有止痛活性。
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公开(公告)号：US4880829A
公开(公告)日：1989-11-14
申请号：US146006
申请日：1988-01-20
CPC分类号： C07K5/06078 , A61K38/00
摘要： The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is hydrogen, lower alkyl, hydroxy, --OCO.sub.2 lower alkyl, lower alkoxy, --O(CH.sub.2).sub.n --phenyl with the phenyl optionally substituted by halogen, --NO.sub.2, --CN, --NH.sub.2 or lower alkyl wherein n is 1 to 4; R.sup.2 and R.sup.3 represent lower alkyl, halogen, or lower alkoxy, or either one of R.sup.2 or R.sup.3 is hydrogen and the other is lower alkyl, lower alkoxy or halogen; R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 may be the same or different and represent hydrogen or lower alkyl; R.sup.10 is selected from the group consisting of--(ALK)Xwhere ALK represents alkylene, thioalkylene, oxyalkylene, having 1 to 5 carbon atoms; alkenylene and alkynylene having 2 to 4 carbon atoms; and X represents pyridyl, pyrimidinyl, 9H-fluoren-9-yl, diphenylmethyl, thienyl, carboxy, lower alkoxy carbonyl, substituted phenyl wherein the phenyl substituent is amino, hydroxy, halogen, nitro, methylenedioxy, lower alkyl, carboxy, lower alkoxycarbonyl, lower alkoxy, carboxamide, diloweralkylamino or X represents phenyl when ALK is not alkylene; or R.sup.10 is ##STR2## where p and q are independently 1 to 4; or R.sup.9 and R.sup.10 together with N is ##STR3## where r and t are independently 1 to 4;v represents an asymmetric carbon that may be racemic or have the D or L configuration;w represents an asymmetric carbon when R.sup.7 and R.sup.8 are not the same that may be racemic or have the D or L configuration.These compounds are useful as analgesic and/or antihypertensive compounds.
摘要翻译： 本发明涉及下式的新型取代的酪氨酰丙氨酸二肽酰胺及其药学上可接受的酸加成盐，其中R 1是氢，低级烷基，羟基，-OCO 2低级烷基，低级烷氧基，-O（CH 2）n - 苯基，其中任选被卤素取代的苯基，-NO 2，-CN，-NH 2或其中n为1至4的低级烷基; R2和R3表示低级烷基，卤素或低级烷氧基，或R2或R3中的任一个为氢，另一个为低级烷基，低级烷氧基或卤素; R 4，R 5，R 6，R 7，R 8和R 9可以相同或不同，表示氢或低级烷基; R 10选自 - （ALK）X，其中ALK表示亚烷基，硫代亚烷基，氧化烯，具有1至5个碳原子; 具有2至4个碳原子的亚烯基和亚炔基; 羟基，卤素，硝基，亚甲二氧基，低级烷基，羧基，低级烷氧基羰基，低级烷氧基羰基，低级烷氧基羰基， 低级烷氧基，甲酰胺，二低级烷基氨基或X代表苯基，当ALK不是亚烷基时; 或R10为
，其中p和q独立地为1至4; 或R 9和R 10与N一起为 ，其中r和t独立地为1至4; v表示可以是外消旋或具有D或L构型的不对称碳; 当R7和R8不相同时，w表示不对称碳，可以是外消旋的或具有D或L构型。 这些化合物可用作镇痛和/或抗高血压化合物。 -
公开(公告)号：US4760180A
公开(公告)日：1988-07-26
申请号：US882795
申请日：1986-07-14
申请人： Barnett S. Pitzele , Donald W. Hansen, Jr. , Robert W. Hamilton , Daniel R. Pilipauskas , Michael Clare
发明人： Barnett S. Pitzele , Donald W. Hansen, Jr. , Robert W. Hamilton , Daniel R. Pilipauskas , Michael Clare
IPC分类号： A61K38/00 , C07K5/065 , C07C103/20
CPC分类号： C07K5/06078 , A61K38/00
摘要： This invention encompasses compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is lower alkoxy or --O--(CH.sub.2).sub.n -phenyl where the phenyl may be optionally substituted with halogen, --NO.sub.2, --CN, --NH.sub.2 or lower alkyl wherein n is 1 to 4; R.sup.2 and R.sup.3 represent lower alkyl, halogen, lower alkoxy or one of R.sup.2 or R.sup.3 is hydrogen and the other is lower alkyl, lower alkoxy, or halogen; R.sup.4, R.sup.5, R.sup.7, R.sup.8, and R.sup.9 represent hydrogen or lower alkyl, R.sup.6 represents hydrogen, lower alkyl, lower alkenyl, or --(CH.sub.2).sub.m -cycloalkyl wherein m is 1 to 4 and the cycloalkyl has 3 to 8 carbon atoms; R.sup.10 is --(CH.sub.2).sub.p -phenyl wherein p is 1 to 4; and v represents an asymmetric carbon that may be racemic or have the D or L Configuration; w represents an asymmetric carbon when R.sup.7 and R.sup.8 are not the same that may be racemic or have the D or L configuration. This invention also encompasses compounds where R.sup.1 is hydroxy, provided at least one of R.sup.4, R.sup.5, R.sup.6 or R.sup.9 is lower alkyl. The compounds of this invention are useful analgesic agents.
摘要翻译： 本发明包括式IMA的化合物及其药学上可接受的酸加成盐，其中R 1是低级烷氧基或-O-（CH 2）n - 苯基，其中苯基可以任选地被卤素，-NO 2，-CN， NH 2或其中n为1至4的低级烷基; R2和R3表示低级烷基，卤素，低级烷氧基或R2或R3中的一个为氢，另一个为低级烷基，低级烷氧基或卤素; R 4，R 5，R 7，R 8和R 9表示氢或低级烷基，R 6表示氢，低级烷基，低级烯基或 - （CH 2）m - 环烷基，其中m为1至4，环烷基具有3至8个碳原子; R 10为 - （CH 2）p - 苯基，其中p为1至4; v表示可以是外消旋的或具有D或L构型的不对称碳; 当R7和R8不相同时，w表示不对称碳，可以是外消旋的或具有D或L构型。 本发明还包括R1为羟基的化合物，只要R4，R5，R6或R9中的至少一个为低级烷基。 本发明的化合物是有用的止痛剂。
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公开(公告)号：US4388308A
公开(公告)日：1983-06-14
申请号：US157693
申请日：1980-06-09
IPC分类号： A61K31/52 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61P9/12 , C07D473/34 , C07H19/16 , C07H19/167
CPC分类号： C07H19/16 , C07D473/34
摘要： N.sup.6 -2-hydroxypropylaryl-substituted adenosines and adenines represented by the formula ##STR1## wherein R.sub.1 is selected from the group consisting of naphthyl, phenyl, substituted phenyl or biphenyl; and R.sub.2 is hydrogen or 1-.beta.-ribosyl; and the pharmaceutically acceptable salts thereof. The compounds are anti-hypertensive agents.
摘要翻译： 由下式表示的N6-2-羟基丙基芳基取代的腺苷和腺嘌呤：其中R 1选自萘基，苯基，取代的苯基或联苯基; R2是氢或1-β-核糖; 及其药学上可接受的盐。 这些化合物是抗高血压药。
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