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1. 发明授权

US4069336A (2-Oxo-pyrrolidines)-acetic hydrazides 失效
标题翻译：（2-氧代吡咯烷） - 甲基水合物
公开(公告)号：US4069336A
公开(公告)日：1978-01-17
申请号：US661138
申请日：1976-02-25
申请人： Fritz-Walter Lange , Haireddin Jacobi , Jens Muller
发明人： Fritz-Walter Lange , Haireddin Jacobi , Jens Muller
IPC分类号： C07D207/26 , C07D207/27 , A61K31/40 , C07D403/12
CPC分类号： C07D207/27
摘要： The present invention pertains to novel (2-oxo-pyrrolidine-1)-acetic hydrazides, methods for preparation and subsequent treatment therewith, and pharmaceutical preparations containing the same.
摘要翻译：本发明涉及新型（2-氧代 - 吡咯烷-1） - 乙酰肼，其制备方法和随后的处理方法以及含有该方法的药物制剂。

2. 发明授权

US4123548A (2-Oxo-pyrrolidines)-acetic hydrazides 失效
标题翻译：（2-氧代 - 吡咯烷）乙酸酰肼
公开(公告)号：US4123548A
公开(公告)日：1978-10-31
申请号：US842908
申请日：1977-10-17
申请人： Fritz-Walter Lange , Haireddin Jacobi , Jens Muller
发明人： Fritz-Walter Lange , Haireddin Jacobi , Jens Muller
IPC分类号： C07D207/26 , C07D207/27 , A61K31/40
CPC分类号： C07D207/27
摘要： The present invention pertains to novel (2-oxo-pyrrolidine-1)-acetic hydrazides, methods for preparation and subsequent treatment therewith, and pharmaceutical preparations containing the same.

3. 发明授权

US4241207A Organonitrogen derivatives of 2-benzopyranone 失效
标题翻译： 2-苯并吡喃酮的有机氮衍生物
公开(公告)号：US4241207A
公开(公告)日：1980-12-23
申请号：US963652
申请日：1978-11-24
申请人： Karl-Heinz Boltze , Peter-Rudolf Seidel , Haireddin Jacobi , Helmut Schwarz
发明人： Karl-Heinz Boltze , Peter-Rudolf Seidel , Haireddin Jacobi , Helmut Schwarz
IPC分类号： A61K31/37 , A61P9/08 , A61P9/10 , C07D311/16 , C07D311/08 , C07D407/14
CPC分类号： C07D311/16 , Y10S514/929
摘要： Novel 2-benzopyranone compounds of the formula ##STR1## wherein X is a 3,4,5-trimethoxybenzoyl group or a 3,4,5-trimethoxycinnamoyl group; and eachR individually is selected from the group consisting of alkylamino and dialkylamino in which one carbon atom in the alkyl moiety may be replaced by an oxygen atom and one hydrogen atom may be replaced by a hydroxyl group which may in turn be esterified with a 3,4,5-trimethoxybenzoyl or 3,4,5-trimethoxycinnamoyl group; amino substituted once or twice by alkenyl, aralkyl, or cycloalkyl; ora 4- to 7-membered N-containing heterocyclic ring linked through a nitrogen atom and which contains up to 3 hetero atoms, which heterocyclic ring may be substituted by phenyl, alkyl or hydroxyalkyl, wherein the hydroxy group may be esterfied by a 3,4,5-trimethoxy benzoyl or 3,4,5-trimethoxy cinnamoyl group;or a salt of each compound with a physiologically acceptable acid; possess outstanding activity as coronary dilators. Processes for producing such compounds are also disclosed.
摘要翻译：新颖的2-苯并吡喃酮化合物，其中X是3,4,5-三甲氧基苯甲酰基或3,4,5-三甲氧基肉桂酰基; 并且每个R各自选自烷基氨基和二烷基氨基，其中烷基部分中的一个碳原子可以被氧原子代替，一个氢原子可以被羟基代替，羟基可以依次用3 ，4,5-三甲氧基苯甲酰基或3,4,5-三甲氧基肉桂酰基; 氨基被烯基，芳烷基或环烷基取代一次或两次; 或通过氮原子连接并含有至多3个杂原子的4至7元含氮杂环，该杂环可被苯基，烷基或羟烷基取代，其中羟基可被3 ，4,5-三甲氧基苯甲酰基或3,4,5-三甲氧基肉桂酰基; 或每种化合物与生理上可接受的酸的盐; 作为冠状动脉扩张器具有突出的活性。还公开了用于生产这些化合物的方法。

4. 发明授权

US4332819A Antiphlogistic agent and its use 失效
标题翻译：消炎药及其用途
公开(公告)号：US4332819A
公开(公告)日：1982-06-01
申请号：US241146
申请日：1981-03-06
申请人： Eugen Etschenberg , Haireddin Jacobi , Wolfgang Opitz
发明人： Eugen Etschenberg , Haireddin Jacobi , Wolfgang Opitz
IPC分类号： A61K9/12 , A61K31/10 , A61K31/21 , A61K31/265 , A61P29/00 , C07C327/20
CPC分类号： A61K31/265 , C07C327/00
摘要： The invention relates to compositions containing S-benzyl 3-benzylthiopropionothioate for the treatment of inflammatory processes. Also included in the invention are methods for combating illnesses caused by inflammatory, processes, which methods involve use of medicaments containing said S-benzyl 3-benzylthiopropionothioate.
摘要翻译：本发明涉及含有S-苄基3-苄硫基丙硫杆酸酯用于治疗炎症过程的组合物。本发明还包括用于对抗由炎症，过程引起的疾病的方法，该方法涉及使用含有所述S-苄基-3-硫代丙酸硫酸酯的药物。

5. 发明授权

US4285935A Dehydropeptide compounds, their production and their medical use 失效
标题翻译：脱氢肽化合物，其生产和医疗用途
公开(公告)号：US4285935A
公开(公告)日：1981-08-25
申请号：US114468
申请日：1980-01-23
申请人： Eugen Etschenberg , Haireddin Jacobi , Wolfgang Opitz
发明人： Eugen Etschenberg , Haireddin Jacobi , Wolfgang Opitz
IPC分类号： C07K1/113 , A61K38/00 , A61P7/02 , A61P43/00 , C07K5/06 , C07K5/065 , A61K37/00 , C07C103/52
CPC分类号： C07K5/06078 , A61K38/00
摘要： This invention relates to dehydropeptides containing a tryptophan moiety useful as tumour-resolving and/or histolytic medicaments. Also included in the invention are methods for the preparation of said dehydropeptides, compositions containing said dehydropeptides and methods for the use of said dehydropeptides and dehydropeptide compositions.
摘要翻译：本发明涉及含有可用作肿瘤分解和/或组织溶解药物的色氨酸部分的脱氢肽。本发明还包括制备所述脱氢肽的方法，含有所述脱氢肽的组合物和使用所述脱氢肽和脱氢肽组合物的方法。

6. 发明授权

US4144336A 2-Benzopyranone derivatives, process for their production, their use as medicaments, more especially as coronary dilators 失效
标题翻译： 2-苯并吡喃酮衍生物，其制备方法，用作药物，更特别地作为冠状动脉扩张剂
公开(公告)号：US4144336A
公开(公告)日：1979-03-13
申请号：US703340
申请日：1976-07-08
申请人： Karl-Heinz Boltze , Peter-Rudolf Seidel , Haireddin Jacobi , Helmut Schwarz
发明人： Karl-Heinz Boltze , Peter-Rudolf Seidel , Haireddin Jacobi , Helmut Schwarz
IPC分类号： A61K31/37 , A61P9/08 , A61P9/10 , C07D311/16 , C07D407/14
CPC分类号： C07D311/16 , Y10S514/929
摘要： Novel 2-benzopyranone compounds of the formula ##STR1## wherein X is a 3,4,5-trimethoxybenzoyl group or a 3,4,5-trimethoxycinnamoyl group; and eachR individually is selected from the group consisting of alkylamino and dialkylamino in which one carbon atom in the alkyl moiety may be replaced by an oxygen atom and one hydrogen atom may be replaced by a hydroxyl group which may in turn be esterified with a 3,4,5-trimethoxybenzoyl or 3,4,5-trimethoxycinnamoyl group; amino substituted once or twice by alkenyl, aralkyl, or cycloalkyl; or a 4- to 7-membered N-containing heterocyclic ring linked through a nitrogen atom and which contains up to 3 hetero atoms, which heterocyclic ring may be substituted by phenyl, alkyl or hydroxyalkyl, wherein the hydroxy group may be esterified by a 3,4,5-trimethoxy benzoyl or 3,4,5-trimethoxy cinnamoyl group;Or a salt of each compound with a physiologically acceptable acid; possess outstanding activity as coronary dilators. Processes for producing such compounds are also disclosed.
摘要翻译：新颖的2-苯并吡喃酮化合物，其中X是3,4,5-三甲氧基苯甲酰基或3,4,5-三甲氧基肉桂酰基; 并且每个R各自选自烷基氨基和二烷基氨基，其中烷基部分中的一个碳原子可以被氧原子代替，一个氢原子可以被羟基代替，羟基可以依次用3 ，4,5-三甲氧基苯甲酰基或3,4,5-三甲氧基肉桂酰基; 氨基被烯基，芳烷基或环烷基取代一次或两次; 或通过氮原子连接并含有至多3个杂原子的4至7元含氮杂环，该杂环可以被苯基，烷基或羟烷基取代，其中羟基可以被3 ，4,5-三甲氧基苯甲酰基或3,4,5-三甲氧基肉桂酰基; 或每种化合物的盐与生理上可接受的酸; 作为冠状动脉造影器的不可忽视的活动。还公开了用于生产这些化合物的方法。

7. 发明授权

US4539402A Quinazolinone derivatives 失效
标题翻译：喹唑啉酮衍生物
公开(公告)号：US4539402A
公开(公告)日：1985-09-03
申请号：US492775
申请日：1983-05-09
申请人： Wolfgang Opitz , Haireddin Jacobi , Bernhard Pelster
发明人： Wolfgang Opitz , Haireddin Jacobi , Bernhard Pelster
IPC分类号： A61K31/505 , A61P25/04 , A61P25/20 , A61P29/00 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to quinazolinone derivatives and of formula (I) as defined herein and processes for the production of said derivatives. Also included in the invention are pharmaceutical compositions containing a compound of said formula (I) as active ingredient and the use of said compounds and compositions as anti-inflammatory agents.
摘要翻译：本发明涉及喹唑啉酮衍生物和本文所定义的式（I）和用于制备所述衍生物的方法。本发明还包括含有所述式（I）化合物作为活性成分的药物组合物和所述化合物和组合物作为抗炎剂的用途。

8. 发明授权

US4370342A S-Alkyl 3-alkylthiopropionothioate compounds, their production and their medicinal use 失效
标题翻译： S-烷基3-烷硫基丙硫醇化合物，其生产及其药用
公开(公告)号：US4370342A
公开(公告)日：1983-01-25
申请号：US241147
申请日：1981-03-06
申请人： Haireddin Jacobi , Wolfgang Opitz
发明人： Haireddin Jacobi , Wolfgang Opitz
IPC分类号： A61K31/255 , A61K31/21 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61P29/00 , C07C67/00 , C07C325/00 , C07C327/20 , C07C327/22 , C07D213/32 , C07D307/38 , C07D307/64 , C07D333/18 , C07D333/34 , C07C153/00 , C07D333/24
CPC分类号： C07D307/38 , C07C327/00 , C07D213/32 , C07D333/18
摘要： The invention relates to S-alkyl 3-alkylthiopropionothioates of Formula (I) as defined herein. Also included in the invention are methods for the manufacture of said S-alkylthiopropionothioates, compositions containing them and the use of said compounds and compositions for the treatment of inflammatory processes.
摘要翻译：本发明涉及如本文所定义的式（I）的3-烷基-3-烷基硫代丙酸硫酸酯。本发明还包括制备所述S-烷基硫代丙硫杆酸酯的方法，含有它们的组合物以及所述化合物和组合物用于治疗炎症过程的用途。

9. 发明授权

US4229453A Substituted 5,6-dimethylpyrrolo[2,3-d]pyrimidine compounds, their production and their medicinal use 失效
标题翻译：取代的5,6-二甲基吡咯并[2,3-d]嘧啶化合物，其生产及其药用
公开(公告)号：US4229453A
公开(公告)日：1980-10-21
申请号：US28028
申请日：1979-04-06
申请人： Hermann J. Roth , Kurt Eger , Sedika Issa , Haireddin Jacobi
发明人： Hermann J. Roth , Kurt Eger , Sedika Issa , Haireddin Jacobi
IPC分类号： A61K31/505 , A61P21/02 , A61P25/04 , A61P25/08 , A61P25/20 , A61P29/00 , C07D207/34 , C07D487/04 , A61K31/495
CPC分类号： C07D487/04 , C07D207/34
摘要： The invention includes 5,6-dimethylpyrrolo [2,3-d]-pyrimidines (and method for their manufacture) of the formula ##STR1## or an acid-addition salt thereof, in which R is amino or hydroxy,R.sub.1 is halogen, nitro, C.sub.1 --C.sub.6 alkyl or alkoxy or CF.sub.3 and, where R is hydroxy, is also hydrogen,R.sub.2 is hydrogen, halogen or C.sub.1 --C.sub.6 -alkyl or alkoxy, andn is 1 or 2.Also included in the invention are pharmaceutical compositions containing said pyrrolo [2,3-d]-pyrimidines and the use of said compounds and compositions for treating CNS illnesses or inflammations.
摘要翻译：本发明包括式（I）的5,6-二甲基吡咯并[2,3-d] - 嘧啶（及其制备方法）或其酸加成盐，其中R为氨基或羟基，R1 是卤素，硝基，C 1 -C 6烷基或烷氧基或CF 3，并且其中R是羟基，也是氢，R 2是氢，卤素或C 1 -C 6烷基或烷氧基，n是1或2.也包括在本发明中是含有所述吡咯并[2,3-d] - 嘧啶的药物组合物，以及所述化合物和组合物用于治疗CNS疾病或炎症的用途。

10. 发明授权

US4349543A Histolytic agents and their use 失效
标题翻译：组织溶解剂及其用途
公开(公告)号：US4349543A
公开(公告)日：1982-09-14
申请号：US108315
申请日：1979-12-31
申请人： Haireddin Jacobi , Wolfgang Opitz , Eugen Etschenberg
发明人： Haireddin Jacobi , Wolfgang Opitz , Eugen Etschenberg
IPC分类号： A61K38/00 , A61P35/00 , C07K5/06 , C07K5/065 , A61K37/02 , A61K37/00
CPC分类号： C07K5/06078 , A61K38/00
摘要： The invention relates to pharmaceutical compositions containing as an active ingredient a dipeptide or an acid salt or a base addition salt thereof or a stereoisomer thereof, said dipeptide being those of the formulaR--Phe--Trp--R.sub.1in whichPhe denote the radical ##STR1## Trp denotes the radical ##STR2## R denotes a hydrogen atom or a C.sub.1 to C.sub.6 optionally substituted alkanoyl group andR.sub.1 denotes a hydroxyl, C.sub.1 to C.sub.4 alkoxy, amino, C.sub.1 to C.sub.4 alkylamino or di-C.sub.1 to C.sub.4 alkylamino group.
摘要翻译：本发明涉及含有作为活性成分二肽或其酸盐或其碱加成盐或其立体异构体的药物组合物，所述二肽是式R-Phe-Trp-R1的二肽，其中Phe表示基团 Trp表示基团R 1表示氢原子或C 1〜C 6任选取代的烷酰基，R 1表示羟基，C 1〜C 4烷氧基，氨基，C 1〜C 4烷基氨基或二-C 1〜C 4烷基氨基。

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