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1. 发明授权

US4727189A Substituted tyrosyl alanine dipeptide amides 失效
标题翻译：取代的酪氨酰丙氨酸二肽酰胺
公开(公告)号：US4727189A
公开(公告)日：1988-02-23
申请号：US851834
申请日：1986-04-14
申请人： Donald W. Hansen, Jr. , Robert H. Mazur , Daniel R. Pilipauskas
发明人： Donald W. Hansen, Jr. , Robert H. Mazur , Daniel R. Pilipauskas
IPC分类号： A61K38/00 , C07K5/065 , C07C103/20 , C07C68/00
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.sub.1 represents straight or branched lower alkyl having 1 to 4 carbons;R.sub.2 represents hydrogen, hydroxy, --OCO.sub.2 R.sub.1 substituent or lower alkyl having 1 to 4 carbons;R.sub.3 represents a hydrogen or lower alkyl having 1 to 6 carbons;R.sub.4 and R.sub.5 may be the same or different and represent hydrogen or lower alkyl having 1 to 6 carbons;n is 1 to 6;X represents a hydrogen, hydroxy or OCO.sub.2 R.sub.1 substituent;A represents a cyclohexyl, phenyl or phenyl substituted with one or more lower alkyls containing 1 to 6 carbons, one or more amino, hydroxy, halogen, nitro or lower alkoxy substituent having 1 to 6 carbons;V represents the asymmetric carbon that may be racemic or have the D or L configuration;W represents the asymmetric carbon when R.sub.4 and R.sub.5 are not the same that may optionally be racemic or have the D or L configuration.These compounds are useful as analgesic and/or antihypertensive agents.
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R1代表具有1-4个碳原子的直链或支链低级烷基; R2代表氢，羟基，-OCO2R1取代基或具有1至4个碳原子的低级烷基; R3表示氢或具有1至6个碳的低级烷基; R 4和R 5可以相同或不同，表示氢或具有1至6个碳的低级烷基; n为1至6; X表示氢，羟基或OCO 2 R 1取代基; A表示被一个或多个含有1至6个碳的低级烷基，一个或多个具有1-6个碳原子的氨基，羟基，卤素，硝基或低级烷氧基取代基取代的苯基或苯基; V表示可以是外消旋或具有D或L构型的不对称碳; 当R4和R5不相同时，W表示不对称碳，其可任选地是外消旋的或具有D或L构型。这些化合物可用作止痛剂和/或抗高血压药物。

2. 发明授权

US4599325A Substituted tyrosyl alanine dipeptide amides 失效
公开(公告)号：US4599325A
公开(公告)日：1986-07-08
申请号：US692611
申请日：1985-01-22
申请人： Donald W. Hansen, Jr. , Robert H. Mazur , Daniel R. Pilipauskas
发明人： Donald W. Hansen, Jr. , Robert H. Mazur , Daniel R. Pilipauskas
IPC分类号： A61K38/00 , C07K5/065 , A61K37/24 , C07K7/12
CPC分类号： C07K5/06078 , A61K38/00 , Y10S514/809
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.sub.1 represents straight or branched lower alkyl having 1 to 4 carbons;R.sub.2 represents hydrogen, hydroxy, --OCO.sub.2 R.sub.1 substituent or lower alkyl having 1 to 4 carbons;R.sub.3 represents a hydrogen or lower alkyl having 1 to 6 carbons;R.sub.4 and R.sub.5 may be the same or different and represent hydrogen or lower alkyl having 1 to 6 carbons;n is 1 to 6;X represents a hydrogen, hydroxy or OCO.sub.2 R.sub.1 substituent;A represents a cyclohexyl, phenyl or phenyl substituted with one or more lower alkyls containing 1 to 6 carbons, one or more amino, hydroxy, halogen, nitro or lower alkoxy substituent having 1 to 6 carbons;V represents the asymmetric carbon that may be racemic or have the D or L configuration;W represents the asymmetric carbon when R.sub.4 and R.sub.5 are not the same that may optionally be racemic or have the D or L configuration. These compounds are useful as analgesic and/or antihypertensive agents.

3. 发明授权

US4797470A O-substituted tyrosyl dipeptide amides 失效
标题翻译： N-末端取代的酪氨酰丙氨酸
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
IPC分类号： A61K38/00 , C07K5/065 , C07K5/08
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。

4. 发明授权

US5536869A Process for the preparation of ethyl 3S-[4-[[4-(aminoiminomethyl)phenyl]amino]-1,4-dioxobutyl]amino]-4-pentyn oate 失效
标题翻译：制备3S- [4 - [[4-（氨基亚氨基甲基）苯基]氨基] -1,4-二氧代丁基]氨基] -4-戊酸乙酯的方法
公开(公告)号：US5536869A
公开(公告)日：1996-07-16
申请号：US502054
申请日：1995-07-14
申请人： Kevin A. Babiak , Srinivasan Babu , James R. Behling , Mark L. Boys , Kimberly J. Cain-Janicki , Wendel W. Doubleday , Payman Farid , Timothy J. Hagen , E. Ann Hallinan , Donald W. Hansen, Jr. , Donald E. Korte , Kathleen T. McLaughlin , John R. Medich , Sean T. Nugent , Vlasdislav Orlovski , Jung M. Park , Karen B. Peterson , Daniel R. Pilipauskas , Barnett S. Pitzele , Sofya Tsymbalov , Glenn L. Stahl
发明人： Kevin A. Babiak , Srinivasan Babu , James R. Behling , Mark L. Boys , Kimberly J. Cain-Janicki , Wendel W. Doubleday , Payman Farid , Timothy J. Hagen , E. Ann Hallinan , Donald W. Hansen, Jr. , Donald E. Korte , Kathleen T. McLaughlin , John R. Medich , Sean T. Nugent , Vlasdislav Orlovski , Jung M. Park , Karen B. Peterson , Daniel R. Pilipauskas , Barnett S. Pitzele , Sofya Tsymbalov , Glenn L. Stahl
IPC分类号： C07C227/02 , C07B61/00 , C07C227/12 , C07C227/34 , C07C229/08 , C07C257/18 , C07C229/24
CPC分类号： C07C227/12 , C07C227/34 , C07C257/18
摘要： The present invention relates to a novel process for the preparation of ethyl 3S-[[4-[[4-(aminoiminomethyl)phenyl]amino]-1,4-dioxobutyl]amino]-4-pentynoate and pharmaceutically acceptable acid addition salt thereof which comprises treating (trimethylsilyl)acetylene sequentially with n-butyllithium and 4-formylmorpholine followed by acid hydrolysis to give 3-(trimethylsilyl)-2-propynal; treating 3-(trimethylsilyl)-2-propynal with lithium bis(trimethylsilyl)amide to give in situ N,3-bis(trimethylsilyl)-2-propyn-1-imine; condensation of N,3-bis(trimethylsilyl)-2-propyn-1-imine with lithium t-butyl acetate to give (.+-.)1,1-dimethylethyl 3-amino-5-(trimethylsilyl)-4-pentynoate; treating (.+-.)1,1-dimethylethyl 3-amino-5-(trimethylsilyl)-4-pentynoate- with p-toluenesulfonic acid to give (.+-.)1,1-dimethylethyl 3-amino-5-(trimethylsilyl)-4-pentynoate, mono p-toluenesulfonic acid salt, treatment of resulting salt with ethanol in the presence of p-toluenesulfonic acid to give (.+-.)ethyl 3-amino-5-(trimethylsilyl)-4-pentynoate; desilylation of (.+-.)ethyl 3-amino-5-(trimethylsilyl)-4-pentynoate to give in situ (.+-.)ethyl 3-amino-4-pentynoate; resolution of (.+-.)ethyl 3-amino-4-pentynoate using (R)-(-)-mandelic acid and treatment of the resolved product with gaseous hydrochloric acid to give ethyl 3S-amino-4-pentynoate, monohydrochloride; coupling the ethyl 3S-amino-4-pentynoate, monohydrochloride to 4-[[4-(aminoiminomethyl)phenyl]amino]-4-oxobutanoic acid, monohydrochloride in the presence of isobutyl chloroformate and N-methylmorpholine to give ethyl 3S-[[4-[[4-(aminoiminomethyl)phenyl]amino]-1,4-dioxobutyl]amino]-4-pentynoate, monohydrochloride.
摘要翻译：本发明涉及制备3S - [[4 - [[4-（氨基亚氨基甲基）苯基]氨基] -1,4-二氧代丁基]氨基] -4-戊酸乙酯及其药学上可接受的酸加成盐的新方法其包括用正丁基锂和4-甲酰基吗啉依次处理（三甲基甲硅烷基）乙炔，然后酸水解，得到3-（三甲基甲硅烷基）-2-丙炔醛; 用双（三甲基甲硅烷基）氨基锂处理3-（三甲基甲硅烷基）-2-丙炔醛，得到原位N，3-双（三甲基甲硅烷基）-2-丙炔-1-亚胺; N，3-二（三甲基甲硅烷基）-2-丙炔-1-亚胺与乙酸叔丁酯的缩合得到3-氨基-5-（三甲基甲硅烷基）-4-戊炔酸（+/-）1,1-二甲基乙酯; 用对甲苯磺酸处理（+/-）3-氨基-5-（三甲基甲硅烷基）-4-戊酸乙酯（+/-）1,1-二甲基乙基酯，得到3-氨基-5-（三甲基甲硅烷基）-4-戊酸酯，单对甲苯磺酸盐，在对甲苯磺酸存在下用乙醇处理所得的盐，得到（+/-）3-氨基-5-（三甲基甲硅烷基）-4-戊酸乙酯; （+/-）乙基3-氨基-5-（三甲基甲硅烷基）-4-戊酸乙酯脱甲硅烷基，得到原位（+/-）3-氨基-4-戊酸乙酯; 使用（R） - （ - ） - 扁桃酸分解（+/-）乙基3-氨基-4-戊炔酸，并用气态盐酸处理分离产物，得到3S-氨基-4-戊酸乙酯，一盐酸盐; 将3S-氨基-4-戊酸乙酯，一盐酸盐在氯甲酸异丁酯和N-甲基吗啉存在下，将4 - [[4-（氨基亚氨基甲基）苯基]氨基] -4-氧代丁酸单盐酸盐偶合，得到3S- [ 4 - [[4-（氨基亚氨基甲基）苯基]氨基] -1,4-二氧代丁基]氨基] -4-戊酸乙酯，一盐酸盐。

5. 发明授权

US4767744A Substituted tyrosyl methionyl dipeptide amides 失效
标题翻译：取代的酪氨酰甲硫氨酰二肽酰胺
公开(公告)号：US4767744A
公开(公告)日：1988-08-30
申请号：US14329
申请日：1987-02-13
申请人： Donald W. Hansen, Jr. , Daniel R. Pilipauskas , Michael Clare
发明人： Donald W. Hansen, Jr. , Daniel R. Pilipauskas , Michael Clare
IPC分类号： A61K38/00 , C07D333/20 , C07D333/38 , C07D333/48 , C07D335/02 , C07K5/065 , A61K37/02 , C07C103/20 , C07D207/00 , C07K5/06
CPC分类号： C07D333/48 , C07D333/20 , C07D333/38 , C07D335/02 , C07K5/06078 , A61K38/00
摘要： This invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable addition salts thereof, wherein R.sup.1 is --OH, --OCH.sub.3 or lower alkoxy of 1-6 carbon atoms; wherein R.sup.2 and R.sup.3 may be the same or different and represent straight or branched chain lower alkyl of 1-6 carbon atoms; wherein R.sup.4, R.sup.5 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 R.sup.6 represents hydrogen, or straight or branched chain lower alkyl of 1-6 carbon atoms, or R.sup.6 may act together with N.sup.6, C.sup.w and either R.sup.7 R.sup.8 to form a cycloamine of the formula: ##STR2## such that between R.sup.7 and R.sup.8, when one acts to form said cycloamine, the other is hydrogen, or straight or branched chain lower alkyl of 1-6 carbon atoms; wherein when neither R.sup.7 nor R.sup.8 is acting to form said cycloamine, R.sup.7 R.sup.8 act together with C.sup.w to form a cycloalkyl of the formula: ##STR3## where n=3, 4, 5; wherein C.sup.w represents 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 represents an asymmetric carbon atom that may be racemic or that may hve the D or L configuration.These compounds are useful because they possess analgesic activity in mammals.
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加成盐，其中R1是-OH，-OCH3或1-6个碳原子的低级烷氧基; 其中R2和R3可以相同或不同，表示1-6个碳原子的直链或支链的低级烷基; 其中R4，R5 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; 其中R6表示氢或1-6个碳原子的直链或支链低级烷基，或R6可以与N6，Cw和R7R8一起起作用以形成下式的环胺：使得在R 7和R 8之间，当一个作用形成所述环胺时，另一个是氢或1-6个碳原子的直链或支链的低级烷基; 其中当R7和R8都不起作用形成所述环胺时，R 7 R8与Cw一起作用以形成下式的环烷基：其中n = 3,4,5; 其中当R 7和R 8不相同时，Cw表示不对称碳原子，可以是外消旋的或具有D或L构型; 并且其中Cv表示可以是外消旋的或可以是D或L构型的不对称碳原子。这些化合物是有用的，因为它们在哺乳动物中具有止痛活性。

6. 发明授权

US4760180A N-terminally substituted dipeptide amides 失效
标题翻译： N-末端取代的二肽酰胺
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。

7. 发明授权

US5631399A Process for the preparation of ethyl 3S-[[4-[[4-(aminoiminomethyl)phenyl]amino]-1,4-dioxobutyl]amino]-4-penty noate 失效
标题翻译：制备3S - [[4 - [[4-（氨基亚氨基甲基）苯基]氨基] -1,4-二氧代丁基]氨基] -4-戊酸乙酯的方法
公开(公告)号：US5631399A
公开(公告)日：1997-05-20
申请号：US647514
申请日：1996-05-14
申请人： Kevin A. Babiak , Srinivasan Babu , James R. Behling , Mark L. Boys , Kimberly J. Cain-Janicki , Wendel W. Doubleday , Payman Farid , Timothy J. Hagen , E. A. Hallinan , Donald W. Hansen, Jr. , Donald E. Korte , Kathleen T. Mc Laughlin , John R. Medich , Sean T. Nugent , Vlasdislav Orlovski , Jung M. Park , Karen B. Peterson , Daniel R. Pilipauskas , Barnett S. Pitzele , Sofya Tsymbalov , Glenn L. Stahl
发明人： Kevin A. Babiak , Srinivasan Babu , James R. Behling , Mark L. Boys , Kimberly J. Cain-Janicki , Wendel W. Doubleday , Payman Farid , Timothy J. Hagen , E. A. Hallinan , Donald W. Hansen, Jr. , Donald E. Korte , Kathleen T. Mc Laughlin , John R. Medich , Sean T. Nugent , Vlasdislav Orlovski , Jung M. Park , Karen B. Peterson , Daniel R. Pilipauskas , Barnett S. Pitzele , Sofya Tsymbalov , Glenn L. Stahl
IPC分类号： C07C227/02 , C07B61/00 , C07C227/12 , C07C227/34 , C07C229/08 , C07C257/18 , C07C229/30
CPC分类号： C07C227/12 , C07C227/34 , C07C257/18
摘要： The present invention relates to a novel process for the preparation of ethyl 3S-[[4-[[4-(aminoiminomethyl)phenyl]amino]-1,4-dioxobutyl]amino]-4-pentynoate and pharmaceutically acceptable acid addition salt thereof.
摘要翻译：本发明涉及制备3S - [[4 - [[4-（氨基亚氨基甲基）苯基]氨基] -1,4-二氧代丁基]氨基] -4-戊酸乙酯及其药学上可接受的酸加成盐的新方法。

8. 发明授权

US4757153A Sulfide, sulfinyl and sulfone dipeptide amides 失效
标题翻译：硫化物，亚磺酰基和砜二肽酰胺
公开(公告)号：US4757153A
公开(公告)日：1988-07-12
申请号：US882796
申请日：1986-07-14
申请人： Donald W. Hansen, Jr. , Daniel R. Pilipauskas , Michael Clare
发明人： Donald W. Hansen, Jr. , Daniel R. Pilipauskas , Michael Clare
IPC分类号： A61K38/00 , C07D333/20 , C07D333/38 , C07D333/48 , C07D335/02 , C07K5/065 , C07D337/00 , C07C103/00 , C07D331/04 , C07D333/36 , C07K7/12
CPC分类号： C07D333/48 , C07D333/20 , C07D333/38 , C07D335/02 , 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, 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, and R.sup.9 may be the same or different and represent hydrogen, lower alkyl, cycloalkyl having 3 to 8 carbons, unsaturated lower alkyl, or --(CH.sub.2).sub.m cycloalkyl with the cycloalkyl having 3 to 8 carbons and m is 1 to 4; R.sup.10 is hydrogen or --(CH.sub.2).sub.p phenyl or with the phenyl optionally substituted with --NH.sub.2, --OH, halogen, --NO.sub.2, or lower alkyl or --(CH.sub.2).sub.p thienyl wherein p is 1 to 4; one of R.sup.7 or R.sup.8 is --(CH.sub.2).sub.f --S(O).sub.z --(CH.sub.2).sub.q --CH.sub.3 where f is 1 to 3 and q is 0 to 3, z is 0, 1 or 2 and the other is hydrogen or lower alkyl, or R.sup.7 and R.sup.8 together with carbon w is ##STR2## where x and y are independently 1 to 3 and z is 0, or 2. V represents an asymmetric carbon that may be recemic 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 recemic or have the D or L configuration.The compounds of this invention are useful as analgesic and/or antihypertensive agents.
摘要翻译：本发明涉及下式的新型取代的酪氨酸丙氨酸二肽酰胺及其药学上可接受的酸加成盐，其中R1是氢，低级烷基，羟基，低级烷氧基，-O（CH2）n-苯基，其中苯基任选被卤素，-NO 2，-CN，-NH 2或低级烷基，其中n为1至4; 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和R 9可以相同或不同，表示氢，低级烷基，具有3-8个碳原子的环烷基，不饱和低级烷基或 - （CH 2）m环烷基，环烷基具有3至8个碳原子，m是1 到4; R 10是氢或 - （CH 2）p苯基或与-NH 2，-OH，卤素，-NO 2或低级烷基或 - （CH 2）p噻吩基取代的苯基，其中p为1至4; R 7或R 8中的一个为 - （CH 2）f S（O）z - （CH 2）q -CH 3，其中f为1至3，q为0至3，z为0,1或2，而另一个为氢或低级烷基或者R 7和R 8与碳w一起为，其中x和y独立地为1〜3，z为0或2.V表示可以是接受或具有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，其可以是可接受的或具有D或L构型。本发明的化合物可用作镇痛药和/或抗高血压药。

9. 发明申请

US20090149431A1 Eplerenone Drug Substance Having High Phase Purity 审中-公开
标题翻译：具有高相纯度的依普利酮药物
公开(公告)号：US20090149431A1
公开(公告)日：2009-06-11
申请号：US12388228
申请日：2009-02-18
申请人： Kathleen P. Barton , Thomas B. Borchardt , Marlow V. Carlos , Subhash Desai , Leonard J. Ferro , Henry T. Gaud , Scott S. Ganser , Clay R. Little , Partha S. Mudipalli , Mark A. Pietz , Daniel R. Pilipauskas , Yuen-Lung L. Sing , Glenn L. Stahl , Joseph J. Wieczorek , Chris Y. Yan
发明人： Kathleen P. Barton , Thomas B. Borchardt , Marlow V. Carlos , Subhash Desai , Leonard J. Ferro , Henry T. Gaud , Scott S. Ganser , Clay R. Little , Partha S. Mudipalli , Mark A. Pietz , Daniel R. Pilipauskas , Yuen-Lung L. Sing , Glenn L. Stahl , Joseph J. Wieczorek , Chris Y. Yan
IPC分类号： C07J71/00 , A61K31/58 , A61P5/00
CPC分类号： C07J71/0015
摘要： A novel crystalline form (Form L) of the aldosterone receptor antagonist drug eplerenone is provided having relatively high physical stability at normal temperatures of storage and use. Pharmaceutical compositions are also provided comprising Form L eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form L eplerenone and for preparing compositions comprising Form L eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form L eplerenone.
摘要翻译：提供醛固酮受体拮抗剂药物依普利酮的新型结晶形式（形式L），其在常规储存和使用温度下具有相对较高的物理稳定性。还提供药物组合物，其包含任选伴随有一种或多种其它固体形式的依普利酮的甲基泼尼龙，总单位剂量为约10至约1000mg的依普利酮，并且还包含一种或多种药学上可接受的赋形剂。提供了用于制备L-赖康孕酮的方法和用于制备包含L-赖普肾素的组合物。还提供了一种用于预防和/或治疗醛固酮介导的病症或病症的方法，其包括向受试者施用治疗有效量的依普利酮，其中至少一部分所述的依普利酮是勃立普仑。

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