专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

EP0136720B1 Enkephalin analogs 有权
标题翻译：脑啡肽类似物
公开(公告)号：EP0136720B1
公开(公告)日：1989-09-20
申请号：EP84111914.2
申请日：1984-10-04
申请人： G.D. Searle & Co.
发明人： Hansen, Donald Willis, Jr. , Jones, David Ackley, Jr. , Mazur, Robert Henry , Schlatter, James Myron
IPC分类号： C07K5/10 , A61K37/02
CPC分类号： C07K5/1016 , Y10S514/809

2. 发明授权

EP0081838B1 Cyclohexyl and phenyl substituted enkephalins 有权
标题翻译：环己酮和苯基取代的环丙沙星
公开(公告)号：EP0081838B1
公开(公告)日：1988-04-27
申请号：EP82111547.4
申请日：1982-12-13
申请人： G.D. Searle & Co.
发明人： Mazur, Robert Henry , Tyner, David Anson , Hallinan, Eleanor Ann
IPC分类号： C07K5/10 , C07K5/06 , C07K5/08 , C07K1/06 , A61K31/02
CPC分类号： C07K5/1016

3. 发明公开

EP0136720A2 Enkephalin analogs 有权
标题翻译：脑啡肽类似物。
公开(公告)号：EP0136720A2
公开(公告)日：1985-04-10
申请号：EP84111914.2
申请日：1984-10-04
申请人： G.D. Searle & Co.
发明人： Hansen, Donald Willis, Jr. , Jones, David Ackley, Jr. , Mazur, Robert Henry , Schlatter, James Myron
IPC分类号： C07K5/10 , A61K37/02
CPC分类号： C07K5/1016 , Y10S514/809
摘要： The invention relates to novel enkephalin analogs of the formula:
which are useful as analgesic agents.

4. 发明公开

EP0154234A3 Substituted tyrosil alanine dipeptide amides 失效
标题翻译：取代的酪氨酸丙氨酸二肽酰胺
公开(公告)号：EP0154234A3
公开(公告)日：1987-05-27
申请号：EP85101690
申请日：1985-02-15
申请人： G.D. Searle & Co.
发明人： Hansen, Donald Willis , Mazur, Robert Henry , Pilipauskas, Daniel Richard
IPC分类号： C07K05/06 , A61K37/02
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:
and the pharmaceutically acceptable acid addition salts thereof wherein
R, represents straight or branched lower alkyl having 1 to 4 carbons; R 2 represent hydrogen, hydroxy, -OCO 2 R 1 substituent or lower alkyl having 1 to 4 carbons; R 3 represents a hydrogen or lower alkyl having 1 to 6 carbons; R 4 and R 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 2 R 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 4 and R 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的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代表具有1至4个碳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个碳的低级烷基; R3代表氢或具有1至6个碳的低级烷基; R4和R5可以相同或不同，表示氢或具有1至6个碳的低级烷基; n是1至6; X代表氢，羟基或OCO 2 R 1取代基; A代表环己基，苯基或被一个或多个含有1至6个碳原子的低级烷基，一个或多个氨基，羟基，卤素，硝基或具有1至6个碳原子的低级烷氧基取代基取代的苯基; V代表可以是外消旋的或具有D或L构型的不对称碳; 当R4和R5不相同时，W代表不对称碳，其可以任选地是外消旋的或具有D或L构型。这些化合物可用作镇痛剂和/或抗高血压剂。

5. 发明公开

EP0154234A2 Substituted tyrosil alanine dipeptide amides 失效
标题翻译：取代基酪氨酰 - 丙氨酸 - 二肽 - 酰胺。
公开(公告)号：EP0154234A2
公开(公告)日：1985-09-11
申请号：EP85101690.7
申请日：1985-02-15
申请人： G.D. Searle & Co.
发明人： Hansen, Donald Willis , Mazur, Robert Henry , Pilipauskas, Daniel Richard
IPC分类号： C07K5/06 , A61K37/02
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:
and the pharmaceutically acceptable acid addition salts thereof wherein

R, represents straight or branched lower alkyl having 1 to 4 carbons;
R 2 represent hydrogen, hydroxy, -OCO 2 R 1 substituent or lower alkyl having 1 to 4 carbons;
R 3 represents a hydrogen or lower alkyl having 1 to 6 carbons;
R 4 and R 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 2 R 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 4 and R 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：式（I）和酸加成盐的二肽是新的。（其中R1 = 1-4C烷基，R2 = H，OH，OCO2R1或1-4C烷基; R3 = H或1-6C烷基，R4，R5 = H或1-6C烷基，n = 1-6，X = H，OH，OCO 2 R 1，A =环己基或苯基取代，具有1个或多个1-6C烷基，一个或多个NH 2，OH，卤素，NO 2或C 1-6烷氧基，v表示不对称C，其可以是外消旋的或具有D或L配置，当R4和R5不相同时，w表示不对称C，或者具有D或L配置）。几个cpds。（I）。 2,6-二甲基酪氨酰基N-（3-苯基丙基）-D-丙氨酸甘氨酸盐酸盐（Ia）和2,6-二甲基酪氨酰-N-（3-苯基 - 丙基）是椭圆酰胺单盐酸盐。 -

6. 发明公开

EP0136720A3 Enkephalin analogs 有权
标题翻译：脑啡肽类似物
公开(公告)号：EP0136720A3
公开(公告)日：1987-05-06
申请号：EP84111914
申请日：1984-10-04
申请人： G.D. Searle & Co.
发明人： Hansen, Donald Willis, Jr. , Jones, David Ackley, Jr. , Mazur, Robert Henry , Schlatter, James Myron
IPC分类号： C07K05/10 , A61K37/02
CPC分类号： C07K5/1016 , Y10S514/809
摘要： The invention relates to novel enkephalin analogs of the formula:
which are useful as analgesic agents.
摘要翻译：本发明涉及下式的新型脑啡肽类似物：其可用作止痛剂。

7. 发明公开

EP0081838A1 Cyclohexyl and phenyl substituted enkephalins 有权
标题翻译：环己基和苯基取代的脑啡肽。
公开(公告)号：EP0081838A1
公开(公告)日：1983-06-22
申请号：EP82111547.4
申请日：1982-12-13
申请人： G.D. Searle & Co.
发明人： Mazur, Robert Henry , Tyner, David Anson , Hallinan, Eleanor Ann
IPC分类号： C07K5/10 , C07K5/06 , C07K5/08 , C07K1/06 , A61K31/02
CPC分类号： C07K5/1016
摘要： The invention relates to novel cyclohexyl and phenyl substituted enkephalins of Formula I which are useful as analgesic agents.
wherein R 1 is:

(a) hydrogen; or
(b) alkyl of 1 to 6 carbon atoms, inclusive;

wherein R 2 and R 8 are:

(a) hydrogen; or
(b) alkyl of 1 to 6 carbon atoms, inclusive; R 2 and R 8 each being the same or different;

wherein R 3 is:

(a) alkyl of 1 to 6 carbon atoms, inclusive;
(b) -C 4 H 9 ;
(c) alkylthioalkyl, having 2 to 6 carbon atoms, inclusive;
(d) alkylsulfinylalkyl, having 2 to 6 carbon atoms inclusive; or
(e) alkoxyalkyl, having 2 to 6 carbon atoms inclusive;

wherein X is:
wherein R 4 is:

(a) hydrogen; or
(b) alkyl of 1 to 6 carbon atoms, inclusive;

wherein R 5 is:
wherein R 6 is:

(a) cyclohexyl; substituted 2, 3, or 4 by R 7 ; or
(b) phenyl; substituted ortho, meta or para by R 7 ;

wherein R 7 is:

(a) hydrogen;
(b) CO 2 -alkyl having 1 to 6 carbon atoms inclusive; or
(c) hydroxy alkyl of one to six carbon atoms inclusive.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式