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1. 发明授权

US5137904A Thiohydantoin inhibitors of collagen-induced and ADP-induced platelet aggregation 失效
标题翻译：胶原诱导的血友病素抑制剂和ADP诱导的血小板聚集
公开(公告)号：US5137904A
公开(公告)日：1992-08-11
申请号：US359003
申请日：1989-05-30
申请人： John S. Baran , Tom Lindberg , Robert H. Mazur , Alan E. Moorman , Doug Steinman
发明人： John S. Baran , Tom Lindberg , Robert H. Mazur , Alan E. Moorman , Doug Steinman
IPC分类号： C07D233/86
CPC分类号： C07D233/86
摘要： A series of ethers and thioethers of 5-methanol thiohydantoins, unsubstituted at the number one position heterocyclic nitrogen atom of the thiohydantoin ring, useful in reversing the effects of collagen and ADP-induced platelet aggregation.
摘要翻译：一系列5-甲基硫代乙内酰脲的醚和硫醚，其在硫代乙内酰脲环的杂环氮原子的第一位未被取代，可用于逆转胶原和ADP诱导的血小板聚集的作用。

2. 发明授权

US4025551A 3-Amino-N-substituted succinamic acids 失效
标题翻译： 3-氨基-N-取代的琥珀酰胺酸
公开(公告)号：US4025551A
公开(公告)日：1977-05-24
申请号：US642890
申请日：1975-12-22
申请人： Arthur H. Goldkamp , Robert H. Mazur , James M. Schlatter
发明人： Arthur H. Goldkamp , Robert H. Mazur , James M. Schlatter
IPC分类号： A23L27/30 , C07D209/16 , C07D307/52 , C07C101/72 , C07C101/02 , C07C101/10 , C07C101/16
CPC分类号： C07D307/52 , A23L27/32 , C07D209/16 , Y02P20/55 , Y10S426/804
摘要： 3-Amino-N-substituted succinamic acids, prepared by coupling of a protected L-aspartic acid derivative with the appropriate amine followed by cleavage of the protecting groups, are potent sweetening agents and also exhibit pharmacological, e.g. anti-inflammatory, properties.
摘要翻译：通过将受保护的L-天冬氨酸衍生物与适当的胺偶联，然后裂解保护基团制备的3-氨基-N-取代的琥珀酰胺酸是有效的甜味剂，并且也表现出药理学的，例如，抗炎，性质。

3. 发明授权

US4012367A Anti-ulcer polypeptides containing L-aspartic acid and intermediates thereto 失效
标题翻译：含有L-天冬氨酸的抗溃疡多肽及其中间体
公开(公告)号：US4012367A
公开(公告)日：1977-03-15
申请号：US655338
申请日：1976-02-05
申请人： Robert H. Mazur
发明人： Robert H. Mazur
IPC分类号： C07K5/10 , A61K38/00 , A61P1/00 , C07K1/113 , C07K5/117 , C07K14/575 , C07K14/595 , C07C103/52 , A61K37/00
CPC分类号： C07K14/5955 , C07K5/1024 , A61K38/00 , Y02P20/55
摘要： This invention encompasses novel tetrapeptide amides and their intermediates containing an L-aspartic acid residue. These peptides are inhibitors of gastric acid secretion and therefore useful in the treatment of ulcers.
摘要翻译：本发明包括新的四肽酰胺及其含有L-天冬氨酸残基的中间体。这些肽是胃酸分泌的抑制剂，因此可用于治疗溃疡。

4. 发明授权

US3975365A Inhibitory octapeptides angiotensin II 失效
标题翻译：抑制性八肽血管紧张素II
公开(公告)号：US3975365A
公开(公告)日：1976-08-17
申请号：US544128
申请日：1975-01-27
申请人： Robert H. Mazur
发明人： Robert H. Mazur
IPC分类号： C07K14/81 , A61K38/00 , C07K1/113 , C07K5/083 , C07K7/06 , C07K7/14 , C07C103/52 , A61K37/00
CPC分类号： C07K7/14 , C07K5/0808 , A61K38/00
摘要： Octapeptide derivatives characterized by an oxygen or sulfur-containing moiety in the C-terminal position are potent inhibitors of the pharmacological effects of Angiotensin and possess the additional advantage of a favorable antagonist/agonist ratio.
摘要翻译：以C末端位置的含氧或含硫部分为特征的八肽衍生物是血管紧张素的药理作用的有效抑制剂，并具有有利的拮抗剂/激动剂比例的另外的优点。

5. 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。

6. 发明授权

US4603121A Enkephalin analogs 失效
标题翻译：脑啡肽类似物
公开(公告)号：US4603121A
公开(公告)日：1986-07-29
申请号：US650145
申请日：1984-09-14
申请人： Donald W. Hansen, Jr. , David A. Jones, Jr. , Robert H. Mazur , James M. Schlatter
发明人： Donald W. Hansen, Jr. , David A. Jones, Jr. , Robert H. Mazur , James M. Schlatter
IPC分类号： C07K5/107 , A61K37/24 , C07K7/12
CPC分类号： C07K5/1016 , Y10S514/809
摘要： The invention relates to novel enkephalin analogs of the formula: ##STR1## which are useful as analgesic agents.
摘要翻译：本发明涉及新的脑啡肽类似物，其具有下式：可用作止痛剂的 + TR 。

7. 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.

8. 发明授权

US4273704A N-Adamantane-substituted tetrapeptide amides 失效
标题翻译： N-金刚烷取代的四肽酰胺
公开(公告)号：US4273704A
公开(公告)日：1981-06-16
申请号：US099765
申请日：1979-12-03
申请人： Robert H. Mazur
发明人： Robert H. Mazur
IPC分类号： C07K5/10 , A61K38/00 , A61P25/04 , C07K5/02 , C07K5/06 , C07K5/103 , C07K5/107 , C07K7/02 , C07K14/575 , C07K14/655 , C07C103/52
CPC分类号： C07K5/06026 , C07K5/0205 , C07K5/1005 , C07K5/1016 , C07K7/02 , A61K38/00
摘要： N-Adamantane-substituted tetrapeptide amides and the pharmacologically acceptable salts thereof are disclosed herein. These compounds are analogs of enkephalin wherein the methionine or leucine of position 5 has been substituted by an adamantyl amide and the glycine of position 2 has been substituted by various amino acid residues. Optionally the tyrosine of position 1 and the phenylalanine of position 4 may be substituted by various amino acid residues. These compounds exhibit agonist activity at opiate receptor sites and are useful as analgesics.
摘要翻译：本文公开了N-金刚烷取代的四肽酰胺及其药理学上可接受的盐。这些化合物是脑啡肽的类似物，其中位置5的甲硫氨酸或亮氨酸已经被金刚烷基酰胺取代，并且位置2的甘氨酸被各种氨基酸残基取代。任选地，位置1的酪氨酸和位置4的苯丙氨酸可以被各种氨基酸残基取代。这些化合物在阿片受体位点表现出激动剂活性，可用作镇痛药。

9. 发明授权

US4495178A Enkephalin analogs 失效
标题翻译：脑啡肽类似物
公开(公告)号：US4495178A
公开(公告)日：1985-01-22
申请号：US539458
申请日：1983-10-06
申请人： Donald W. Hansen, Jr. , David A. Jones, Jr. , Robert H. Mazur , James M. Schlatter
发明人： Donald W. Hansen, Jr. , David A. Jones, Jr. , Robert H. Mazur , James M. Schlatter
IPC分类号： C07K14/655 , A61K38/00 , A61K38/22 , A61P25/04 , C07K5/107 , C07K14/575 , C07K14/70 , A61K37/00 , C07C103/52
CPC分类号： C07K5/1016 , Y10S514/809
摘要： The invention relates to novel enkephalin analogs of the formula: ##STR1## which are useful as analgesic agents.
摘要翻译：本发明涉及新的脑啡肽类似物，其具有下式：作为止痛剂有用的。

10. 发明授权

US4407746A Cyclohexyl and phenyl substituted enkephalins 失效
标题翻译：环己基和苯基取代的脑啡肽
公开(公告)号：US4407746A
公开(公告)日：1983-10-04
申请号：US330614
申请日：1981-12-14
申请人： Robert H. Mazur , David A. Tyner , Eleanor A. Hallinan
发明人： Robert H. Mazur , David A. Tyner , Eleanor A. Hallinan
IPC分类号： C07K14/655 , A61K38/00 , A61K38/22 , A61P25/04 , C07K5/10 , C07K5/107 , C07K14/575 , C07K14/70 , C07C103/52 , A61K37/00
CPC分类号： C07K5/1016
摘要： The invention discloses cyclohexyl and phenyl substituted enkephalin derivatives of the formula: ##STR1## Where R.sub.1, R.sub.2, R.sub.4, and R.sub.8 is hydrogen or alkyl of R.sub.3 is alkylthioalkyl or alkylsulfinylalkyl, X is: ##STR2## R.sub.5 is cyclohexylmethyl, phenylmethyl, optionally substituted by --NO.sub.2, R.sub.6 is cyclohexyl or phenyl optionally substituted by R.sub.7 and R.sub.7 is hydrogen, an alkyl ester of carboxylic acid or hydroxyalkyl and the pharmaceutically acceptable salts, which are useful as analgesic agents.
摘要翻译：本发明公开了下式的环己基和苯基取代的脑啡肽衍生物：其中R1，R2，R4和R8是氢或R3的烷基是烷硫基烷基或烷基亚磺酰基烷基，X是：环己基甲基，苯甲基，通过-NO 2，R 6是任选被R 7取代的环己基或苯基，R 7是氢，羧酸或羟烷基的烷基酯和药学上可接受的盐，其可用作止痛剂。

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