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1. 发明授权

US4647563A Heterocyclic compounds 失效
标题翻译：杂环化合物
公开(公告)号：US4647563A
公开(公告)日：1987-03-03
申请号：US806692
申请日：1985-12-09
申请人： Kurt Schromm , Anton Mentrup , Ernst-Otto Renth , Armin Fugner , Ilse Streller
发明人： Kurt Schromm , Anton Mentrup , Ernst-Otto Renth , Armin Fugner , Ilse Streller
IPC分类号： A61K31/41 , A61K31/415 , A61K31/4166 , A61K31/4184 , A61K31/42 , A61K31/496 , A61K31/505 , A61K31/517 , A61K31/535 , A61K31/5355 , A61P1/04 , A61P1/06 , A61P9/00 , A61P9/06 , A61P9/12 , A61P11/00 , A61P11/08 , A61P13/02 , A61P15/00 , A61P25/24 , A61P25/26 , A61P27/02 , A61P27/14 , A61P37/08 , C07D233/36 , C07D233/54 , C07D233/58 , C07D233/61 , C07D235/06 , C07D235/08 , C07D235/18 , C07D239/88 , C07D239/90 , C07D239/96 , C07D249/18 , C07D413/12 , C07D521/00
CPC分类号： C07D233/64 , C07D231/12 , C07D233/36 , C07D233/56 , C07D235/06 , C07D235/08 , C07D235/18 , C07D239/88 , C07D239/96 , C07D249/08 , C07D249/18 , Y10S514/821 , Y10S514/826 , Y10S514/849 , Y10S514/906 , Y10S514/914
摘要： Compounds of the formula ##STR1## wherein Het is ##STR2## n is an integer from 1 to 4, inclusive, preferably 2 or 3, R.sub.1 is H or acyl,R.sub.2 is H, R.sub.1 O, --NHSO.sub.2 R.sub.7, --NHCOR.sub.8, --NHCONHR.sub.8, --NH--CH.sub.2 --C.sub.6 H.sub.4 --R.sub.9, --CH.sub.2 OH, --CH.sub.2 SO.sub.2 R.sub.7, --CONHR.sub.8, halogen or --CN,R.sub.3 is H, halogen, R.sub.7 or --OR.sub.7,R.sub.2 and R.sub.3 together with each other are ##STR3## R.sub.4 is H, --CH.sub.3 or --C.sub.2 H.sub.5, R.sub.5 and R.sub.6 are each H or --CH.sub.3,R.sub.7 is C.sub.1 -C.sub.4 alkyl,R.sub.8 is H or C.sub.1 -C.sub.4 alkyl,R.sub.9 is H, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy optionally interrupted by oxygen,R.sub.10 and R.sub.12 are each H, CH.sub.3, Cl or OCH.sub.3, or together methylenedioxy,X is ##STR4## or N, and Z is --CH.sub.2 or --CO;in the form of racemates, enantiomers, diastereoisomeric antipode pairs, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as the salts are useful as bronchospasmolytics, spasmolytics, muscle-relaxants, antiallergics and hypotensives.
摘要翻译：其中Het为+4 的化合物，n为1〜4的整数，优选2或3，R 1为H或酰基，R 2为H，R 10，-NHSO 2 R 7， NHCOR 8，-NHCONHR 8，-NH-CH 2 -C 6 H 4 -R 9，-CH 2 OH，-CH 2 SO 2 R 7，-CONHR 8，卤素或-CN，R 3是H，卤素，R 7或-OR 7，R 2和R 3彼此是 R4是H，-CH3或-C2H5，R5和R6分别是H或-CH3，R7是C1-C4烷基，R8是H或C1-C4烷基，R9是H，C1-C4烷基或C1-C4烷氧基被氧中断，R 10和R 12各自为H，CH 3，Cl或OCH 3，或一起亚甲二氧基，X为或N，Z为-CH 2或-CO; 以外消旋物，对映异构体，非对映异构体对映体对及其无毒的药学上可接受的酸加成盐的形式存在。化合物和盐可用作支气管解痉药，解痉药，肌肉松弛剂，抗过敏药和低血压药。

2. 发明授权

US4871760A Use of 2-(N-2,6-dichlorophenyl-N-allylamino)-2-imidazoline as cytoprotective agent 失效
标题翻译：使用2-（N-2,6-二氯苯基-N-烯丙基氨基）-2-咪唑啉作为细胞保护剂
公开(公告)号：US4871760A
公开(公告)日：1989-10-03
申请号：US63617
申请日：1987-06-18
申请人： Dietrich Arndts , Gunter Schingnitz , Ilse Streller , Alexander Walland
发明人： Dietrich Arndts , Gunter Schingnitz , Ilse Streller , Alexander Walland
IPC分类号： C07D233/50 , A61K31/41 , A61K31/415 , A61P43/00
CPC分类号： A61K31/41
摘要： The invention relates to the use of 2-[N-(2,6-dichlorophenyl)-N-allylamino]-2-imidazoline as a cytoprotective agent.
摘要翻译：本发明涉及2- [N-（2,6-二氯苯基）-N-烯丙基氨基] -2-咪唑啉作为细胞保护剂的用途。

3. 发明授权

US4341778A 3,1 Benzoxazin-2-ones and use thereof 失效
标题翻译： 3，苯并恶嗪-2-酮及其用途
公开(公告)号：US4341778A
公开(公告)日：1982-07-27
申请号：US280349
申请日：1981-07-06
申请人： Anton Mentrup , Kurt Schromm , Ernst-Otto Renth , Wolfgang Hoefke , Wolfram Gaida , Ilse Streller , Armin Fugner
发明人： Anton Mentrup , Kurt Schromm , Ernst-Otto Renth , Wolfgang Hoefke , Wolfram Gaida , Ilse Streller , Armin Fugner
IPC分类号： C07D265/16 , A61K31/535 , A61K31/536 , A61P9/00 , A61P9/08 , A61P9/12 , A61P11/08 , A61P13/02 , A61P15/00 , C07D265/18 , C07D265/22
CPC分类号： C07D265/18
摘要： The invention relates to compounds of general formula I ##STR1## (wherein R.sub.1 and R.sub.2, which may be the same or different, each represents a hydrogen atom or a (C.sub.1 -C.sub.4) alkyl group;R.sub.3 and R.sub.4, which may be the same or different, each represents a hydrogen, fluorine or chlorine atom or a hydroxy, methyl, ethyl or (C.sub.1 -C.sub.4) alkoxy group, or R.sub.3 together with R.sub.4 represents a methylenedioxy group;R.sub.5 and R.sub.6, which may be the same or different, each represents a hydrogen atom or a methyl group;R.sub.7 represents a group of formula ##STR2## R represents a hydrogen atom or a (C.sub.1 -C.sub.4) alkyl group; R.sub.8 represents a fluorine or chlorine atom or a (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkylthio, hydroxymethyl, CONHR.sub.11, SO.sub.2 NHR.sub.11, OR.sub.12, methoxycarbonyl, ethoxycarbonyl or NHSO.sub.2 CH.sub.3 group;R.sub.9 represents a hydrogen, fluorine or chlorine atom or a OR.sub.12 group;R.sub.10 represents a hydrogen or chlorine atom or an amino, methyl or methoxy group;R.sub.11 represents a hydrogen atom or a methyl, ethyl or hydroxyethyl group;R.sub.12 represents a hydrogen atom or a (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkyl-CO, aryl-CH.sub.2 or aryl-CO group; andn represents 1, 2 or 3) and acid addition salts thereof as well as to processes for their preparation and pharmaceutical compositions containing them. The compounds of the invention possess interesting pharmacological properties in particular displaying hypotensive and selective tocolytic effects.
摘要翻译：本发明涉及通式I（I）的化合物（其中R 1和R 2可以相同或不同，各自表示氢原子或（C 1 -C 4）烷基; R 3和R 4可以相同或不同，各自表示氢，氟或氯原子或羟基，甲基，乙基或（C1-C4）烷氧基，或R3与R4一起代表亚甲二氧基; R5和R6可以相同或不同的，各自表示氢原子或甲基; R 7表示下式的基团：R表示氢原子或（C 1 -C 4）烷基; R 8表示氟或氯原子或（C 1 -C 4））烷基，（C1-C4）烷硫基，羟甲基，CONHR11，SO2NHR11，OR12，甲氧基羰基，乙氧基羰基或NHSO2CH3基; R9表示氢，氟或氯原子或OR12基团; R10表示氢或氯原子或氨基，甲基或甲氧基; R11表示氢原子或甲基，乙基或羟乙基; R12表示a 氢原子或（C 1 -C 4）烷基，（C 1 -C 4）烷基-CO，芳基-CH 2或芳基-CO基团; 和n表示1,2或3）及其酸加成盐以及其制备方法和含有它们的药物组合物。本发明的化合物具有特别显示降血压和选择性溶瘤作用的有趣的药理学性质。

4. 发明授权

US4378361A Heterocyclic compounds 失效
标题翻译：杂环化合物
公开(公告)号：US4378361A
公开(公告)日：1983-03-29
申请号：US285713
申请日：1981-07-22
申请人： Kurt Schromm , Anton Mentrup , Ernst-Otto Renth , Armin Fugner , Ilse Streller
发明人： Kurt Schromm , Anton Mentrup , Ernst-Otto Renth , Armin Fugner , Ilse Streller
IPC分类号： A61K31/41 , A61K31/415 , A61K31/4166 , A61K31/4184 , A61K31/42 , A61K31/496 , A61K31/505 , A61K31/517 , A61K31/535 , A61K31/5355 , A61P1/04 , A61P1/06 , A61P9/00 , A61P9/06 , A61P9/12 , A61P11/00 , A61P11/08 , A61P13/02 , A61P15/00 , A61P25/24 , A61P25/26 , A61P27/02 , A61P27/14 , A61P37/08 , C07D233/36 , C07D233/54 , C07D233/58 , C07D233/61 , C07D235/06 , C07D235/08 , C07D235/18 , C07D239/88 , C07D239/90 , C07D239/96 , C07D249/18 , C07D413/12 , C07D521/00 , C07D239/72
CPC分类号： C07D233/64 , C07D231/12 , C07D233/36 , C07D233/56 , C07D235/06 , C07D235/08 , C07D235/18 , C07D239/88 , C07D239/96 , C07D249/08 , C07D249/18 , Y10S514/821 , Y10S514/826 , Y10S514/849 , Y10S514/906 , Y10S514/914
摘要： Compounds of the formula ##STR1## wherein Het is ##STR2## n is an integer from 1 to 4, inclusive, preferably 2 or 3, R.sub.1 is H or acyl,R.sub.2 is H, R.sub.1 O, --NHSO.sub.2 R.sub.7, --NHCOR.sub.8, --NHCONHR.sub.8, --NH--CH.sub.2 --C.sub.6 H.sub.4 --R.sub.9, --CH.sub.2 OH, --CH.sub.2 SO.sub.2 R.sub.7, --CONHR.sub.8, halogen or --CN,R.sub.3 is H, halogen, R.sub.7 or --OR.sub.7,R.sub.2 and R.sub.3 together with each other are ##STR3## R.sub.4 is H, --CH.sub.3 or --C.sub.2 H.sub.5, R.sub.5 and R.sub.6 are each H or --CH.sub.3,R.sub.7 is C.sub.1 -C.sub.4 alkyl,R.sub.8 is H or C.sub.1 -C.sub.4 alkyl,R.sub.9 is H, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy optionally interrupted by oxygen,R.sub.10 and R.sub.12 are each H, CH.sub.3, Cl or OCH.sub.3, or together methylenedioxy,X is ##STR4## or N, and Z is --CH.sub.2 or --CO;in the form of racemates, enantiomers, diastereoisomeric antipode pairs, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as the salts are useful as bronchospasmolytics, spasmolytics, muscle-relaxants, antiallergics and hypotensives.
摘要翻译：其中Het为1至4的整数，包括端值，优选2或3，R 1为H或酰基，R 2为H，R 1 O - ， - NHSO2R7，-NHCOR8，-NHCONHR8，-NH-CH2-C6H4-R9，-CH2OH，-CH2SO2R7，-CONHR8，卤素或-CN，R3是H，卤素，R7或-OR7，R2和R3彼此是 R4是H，-CH3或-C2H5，R5和R6分别是H或-CH3，R7是C1-C4烷基，R8是H或C1-C4烷基，R9是H，C1-C4烷基或C1- 任选被氧中断的C 4烷氧基，R 10和R 12各自为H，CH 3，Cl或OCH 3，或一起为亚甲二氧基，X为N或N，并且Z为-CH 2或-CO; 以外消旋物，对映异构体，非对映异构体对映体对及其无毒的药学上可接受的酸加成盐的形式存在。化合物和盐可用作支气管解痉药，解痉药，肌肉松弛剂，抗过敏药和低血压药。

5. 发明授权

US5607941A Useful for treating neurodegenerative diseases 失效
标题翻译：用于治疗神经退行性疾病
公开(公告)号：US5607941A
公开(公告)日：1997-03-04
申请号：US463798
申请日：1995-06-05
申请人： Herbert Merz , Enzio Mueller , Werner Stransky , Ilse Streller
发明人： Herbert Merz , Enzio Mueller , Werner Stransky , Ilse Streller
IPC分类号： C07D221/26 , A61K31/445 , A61K31/44 , C07D221/22
CPC分类号： A61K31/439 , C07D221/26
摘要： Novel benzomorphan derivatives of the formula ##STR1## wherein R.sup.1 -R.sup.8 are as defined herein. The benzomorphan derivatives are useful for treating cerebral ischaemia of various origins, epilepsy and neurodegenerative diseases.
摘要翻译：新颖的式（I）的苯并吗啉衍生物，其中R 1 -R 8如本文所定义。苯并吗啉衍生物可用于治疗各种起源，癫痫和神经退行性疾病的脑缺血。

6. 发明授权

US5008273A Amino acid derivatives and their pharmaceutical use 失效
标题翻译：氨基酸衍生物及其药物用途
公开(公告)号：US5008273A
公开(公告)日：1991-04-16
申请号：US403628
申请日：1989-09-06
申请人： Gerd Schnorrenberg , Otto Roos , Walter Losel , Ingrid Wiedemann , Wolfram Gaida , Wolfgang Hoefke , Dietrich Arndts , Ilse Streller
发明人： Gerd Schnorrenberg , Otto Roos , Walter Losel , Ingrid Wiedemann , Wolfram Gaida , Wolfgang Hoefke , Dietrich Arndts , Ilse Streller
IPC分类号： C07K14/81 , A61K31/198 , A61K31/381 , A61K31/435 , A61K38/00 , A61K38/55 , A61P9/00 , A61P9/12 , A61P43/00 , C07D471/04 , C07D491/048 , C07D495/04 , C07K1/113 , C07K5/02 , C07K5/06
CPC分类号： C07K5/0222 , C07K5/06086 , A61K38/00
摘要： Amino acid derivatives of general formula ##STR1## (the definitions of the various symbols being explained in the specification) are suitable for treating high blood pressure and for cardioprotection. The new compounds are prepared and used in the usual way.
摘要翻译：通式（I）的氨基酸衍生物（说明书中解释的各种符号的定义）适用于治疗高血压和心脏保护。新化合物以常规方式制备和使用。

7. 发明授权

US5731318A Benzomorphan derivatives 失效
标题翻译：苯并吗啉衍生物
公开(公告)号：US5731318A
公开(公告)日：1998-03-24
申请号：US691220
申请日：1996-08-01
申请人： Adrian Carter , Helmut Ensinger , Matthias Grauert , Franz Josef Kuhn , Herbert Merz , Enzio Mueller , Werner Stransky , Ilse Streller
发明人： Adrian Carter , Helmut Ensinger , Matthias Grauert , Franz Josef Kuhn , Herbert Merz , Enzio Mueller , Werner Stransky , Ilse Streller
IPC分类号： C07D221/26 , A61K31/44 , C07D221/12
CPC分类号： A61K31/439 , C07D221/26
摘要： Novel benzomorphan derivatives of the formula ##STR1## wherein R.sup.1 -R.sup.8 are as defined herein. The benzomorphan derivatives are useful for treating cerebral ischaemia of various origins, epilepsy and neurodegenerative diseases.
摘要翻译：新颖的式（I）的苯并吗啉衍生物，其中R 1 -R 8如本文所定义。苯并吗啉衍生物可用于治疗各种起源，癫痫和神经退行性疾病的脑缺血。

8. 发明授权

US4581367A 1-phenyl-2-(heterocyclyl-alkyl-amino)-ethanols 失效
标题翻译： 1-苯基-2-（杂环基 - 烷基 - 氨基） - 乙醇
公开(公告)号：US4581367A
公开(公告)日：1986-04-08
申请号：US443912
申请日：1982-11-23
申请人： Kurt Schromm , Anton Mentrup , Ernst-Otto Renth , Armin Fugner , Ilse Streller
发明人： Kurt Schromm , Anton Mentrup , Ernst-Otto Renth , Armin Fugner , Ilse Streller
IPC分类号： A61K31/41 , A61K31/415 , A61K31/4166 , A61K31/4184 , A61K31/42 , A61K31/496 , A61K31/505 , A61K31/517 , A61K31/535 , A61K31/5355 , A61P1/04 , A61P1/06 , A61P9/00 , A61P9/06 , A61P9/12 , A61P11/00 , A61P11/08 , A61P13/02 , A61P15/00 , A61P25/24 , A61P25/26 , A61P27/02 , A61P27/14 , A61P37/08 , C07D233/36 , C07D233/54 , C07D233/58 , C07D233/61 , C07D235/06 , C07D235/08 , C07D235/18 , C07D239/88 , C07D239/90 , C07D239/96 , C07D249/18 , C07D413/12 , C07D521/00 , C07D235/00
CPC分类号： C07D233/64 , C07D231/12 , C07D233/36 , C07D233/56 , C07D235/06 , C07D235/08 , C07D235/18 , C07D239/88 , C07D239/96 , C07D249/08 , C07D249/18 , Y10S514/821 , Y10S514/826 , Y10S514/849 , Y10S514/906 , Y10S514/914
摘要： Compounds of the formula whereinHet is a heterocycle;n is an integer from 1 to 4, inclusive, preferably 2 or 3;R.sub.1 is H or acyl;R.sub.2 is H, R.sub.1 O, --NHSO.sub.2 R.sub.7, --NHCOR.sub.8, --NHCONHR.sub.8, --NH--CH.sub.2 --C.sub.6 H.sub.4 --R.sub.9, --CH.sub.2 OH, --CH.sub.2 SO.sub.2 R.sub.7, --CONHR.sub.8, halogen or --CN;R.sub.3 is H, halogen, R.sub.7 or --OR.sub.7 ; orR.sub.2 and R.sub.3, together with each other, are ##STR1## N.sub.4 is H, --CH.sub.3 or --C.sub.2 H.sub.5 ; R.sub.5 and R.sub.6 are each H or --CH.sub.3 ;R.sub.7 is C.sub.1 -C.sub.4 alkyl;R.sub.8 is H or C.sub.1 -C.sub.4 alkyl; andR.sub.9 is H, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy optionally interrupted by oxygen;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as the salts are useful as bronchospasmolytics, spasmolytics, muscle-relaxants, antiallergics and hypotensives.
摘要翻译：其中Het是杂环的式“IMAGE”的化合物; n为1〜4的整数，优选为2或3; R1是H或酰基; R2是H，R1O，-NHSO2R7，-NHCOR8，-NHCONHR8，-NH-CH2-C6H4-R9，-CH2OH，-CH2SO2R7，-CONHR8，卤素或-CN; R3是H，卤素，R7或-OR7; 或R 2和R 3彼此一起是H，-CH 3或-C 2 H 5; R5和R6各自为H或-CH3; R7是C1-C4烷基; R8是H或C1-C4烷基; 并且R 9为H，任选被氧中断的C 1 -C 4烷基或C 1 -C 4烷氧基; 和无毒的，药学上可接受的酸加成盐。化合物和盐可用作支气管解痉药，解痉药，肌肉松弛剂，抗过敏药和低血压药。

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