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1. 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。

2. 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。

3. 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。

4. 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。

5. 发明授权

US4539323A N-[1-(4-Amino-6,7-dialkoxy-2-quinazolinyl)-4-piperidy l]-oxazolidine-2,4-diones 失效
标题翻译： N- [1-（4-氨基-6,7-二烷氧基-2-喹唑啉基）-4-哌啶基] - 恶唑烷-2,4-二酮
公开(公告)号：US4539323A
公开(公告)日：1985-09-03
申请号：US531842
申请日：1983-09-14
申请人： Anton Mentrup , Ernst-Otto Renth , Kurt Schromm , Wolfgang Hoefke , Wolfram Gaida
发明人： Anton Mentrup , Ernst-Otto Renth , Kurt Schromm , Wolfgang Hoefke , Wolfram Gaida
IPC分类号： C07D239/95 , A61K31/505 , A61K31/517 , A61P9/08 , A61P9/12 , A61P25/02 , C07D263/44 , C07D401/14 , C07D413/04 , C07D413/14 , C07D491/056
CPC分类号： C07D413/04 , C07D413/14
摘要： Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2, which may be identical to or different from each other, are each independently hydrogen, straight or branched alkyl of 1 to 8 carbon atoms or arylmethyl; orR.sub.1 and R.sub.2, together with each other, are --(CH.sub.2).sub.4 or --(CH.sub.2).sub.5 --; andR.sub.3 and R.sub.4, which may be identical to or different from each other, are each independently hydrogen, straight or branched alkyl of 1 to 4 carbon atoms or arylmethyl; orR.sub.3 and R.sub.4, together with each other, are --CH.sub.3 -- or --CH.sub.2 --CH.sub.2 --;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful for the treatment of cardiovascular diseases, especially hypertension.
摘要翻译：其中R 1和R 2可以相同或不同，各自独立地为氢，1至8个碳原子的直链或支链烷基或芳基甲基; 或R 1和R 2彼此一起为 - （CH 2）4或 - （CH 2）5 - ; 并且可以相同或不同的R 3和R 4各自独立地为氢，1至4个碳原子的直链或支链烷基或芳基甲基; 或R 3和R 4彼此一起为-CH 3 - 或-CH 2 -CH 2 - ; 和无毒的，药学上可接受的酸加成盐。化合物及其盐可用于治疗心血管疾病，特别是高血压。

6. 发明授权

US4720496A Pyridotriazoloquinazolines and triazolopyridoquinazolines useful as antiallergics 失效
标题翻译：吡唑并三唑喹唑啉和三唑并吡啶喹唑啉可用作抗过敏药
公开(公告)号：US4720496A
公开(公告)日：1988-01-19
申请号：US870365
申请日：1986-06-04
申请人： Kurt Schromm , Anton Mentrup , Ernst-Otto Renth , Armin Fugner
发明人： Kurt Schromm , Anton Mentrup , Ernst-Otto Renth , Armin Fugner
IPC分类号： C07D487/04 , A61K31/505 , A61K31/517 , A61P9/08 , A61P11/00 , A61P11/08 , A61P37/08 , C07D471/14
CPC分类号： C07D471/14
摘要： Compounds of the formula ##STR1## wherein (a)R.sub.1 is hydrogen, lower alkyl, lower alkoxy or 8-halo;R.sub.2 is hydrogen, lower alkyl, lower alkoxy or a fused benzene ring; andR.sub.3 and R.sub.4, together with each other, are --N.dbd.N--NH--; or(b)R.sub.1 and R.sub.2, together with each other, are --N.dbd.N--NH--;R.sub.3 is hydrogen, lower alkyl, lower alkoxy, 2-halo, 3-halo or 4-halo; andR.sub.4 is hydrogen, lower alkyl, lower alkoxy or a fused benzene ring;and non-toxic, pharmacologically acceptable salts thereof formed with an inorganic or organic base. The compounds as well as their salts are useful as antiallergics.
摘要翻译：式（Ia）的化合物，其中（a）R 1是氢，低级烷基，低级烷氧基或8-卤素; R2是氢，低级烷基，低级烷氧基或稠合苯环; 并且R 3和R 4彼此一起是-N = N-NH-; 或（b）R 1和R 2彼此一起为-N = N-NH-; R3是氢，低级烷基，低级烷氧基，2-卤代，3-卤代或4-卤素; R4为氢，低级烷基，低级烷氧基或稠合苯环; 和与无机或有机碱形成的无毒的，药学上可接受的盐。化合物及其盐可用作抗过敏药。

7. 发明授权

US4558061A Bronchospasmolytic 1-(3-methanesulfonamido-4-hydroxyphenyl)-2-[(3-(4-acyl-aminophenyl)-imid azolidin-2-one-1-yl)-alkylamino]-ethanols 失效
标题翻译：支气管痉挛性1-（3-甲磺酰氨基-4-羟基苯基）-2 - [（3-（4-酰基 - 氨基苯基） - 咪唑烷-2-酮-1-基） - 烷基氨基] - 乙醇
公开(公告)号：US4558061A
公开(公告)日：1985-12-10
申请号：US628383
申请日：1984-07-06
申请人： Anton Mentrup , Kurt Schromm , Ernst-Otto Renth , Gojko Muacevic , Armin Fugner
发明人： Anton Mentrup , Kurt Schromm , Ernst-Otto Renth , Gojko Muacevic , Armin Fugner
IPC分类号： C07D233/34 , A61K31/415 , A61K31/4166 , A61P9/08 , A61P11/00 , A61P11/08 , A61P25/24 , A61P25/26 , C07D233/30 , C07D233/36
CPC分类号： C07D233/36
摘要： Compounds of the formula ##STR1## wherein n is 1 or 2, R.sub.1 is hydrogen, --CO--R.sub.2 or --SO.sub.2 R.sub.3,R.sub.2 is hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or (alkyl of 1 to 4 carbon atoms)amino, andR.sub.3 is alkyl of 1 to 4 carbon atoms,and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as bronchospasmolytics.
摘要翻译：其中n为1或2，R1为氢，-CO-R2或-SO2R3，R2为氢，1至4个碳原子的烷基，1至4个碳原子的烷氧基的化合物或（1〜4个碳原子的烷基）氨基，R3为1〜4个碳原子的烷基，以及无毒的药学上可接受的酸加成盐。化合物及其盐可用作支气管痉挛溶解剂。

8. 发明授权

US4460581A (1-Hydroxy-2-amino-alkyl)-substituted benzoxazinones and benzoxazolinones 失效
标题翻译：（1-羟基-2-氨基 - 烷基）取代的苯并恶嗪酮和苯并恶唑啉酮
公开(公告)号：US4460581A
公开(公告)日：1984-07-17
申请号：US433681
申请日：1982-10-12
申请人： Kurt Schromm , Anton Mentrup , Ernst-Otto Renth , Armin Fugner
发明人： Kurt Schromm , Anton Mentrup , Ernst-Otto Renth , Armin Fugner
IPC分类号： C07D263/58 , C07D265/36 , C07D413/12 , A61K31/47
CPC分类号： C07D263/58 , C07D265/36 , C07D413/12
摘要： Compounds of the formula ##STR1## wherein A is a single bond, ##STR2## R.sub.1 is --OH, --0--acyl, chlorine or hydrogen; R.sub.2 is hydrogen, methyl or ethyl;R.sub.3 is ##STR3## m is 2, 3 or 4; n is 1, 2 or 3;R.sub.4 is hydrogen or lower alkyl;R.sub.5 is hydrogen, lower alkyl or, when R.sub.4 is hydrogen, also phenyl;R.sub.6, R.sub.7 and R.sub.8 are each hydrogen or methyl;R.sub.9 is hydrogen, --Ar, --OAr or --NH--CO--Ar;Ar is ##STR4## R.sub.10, R.sub.11 and R.sub.12 which may be identical to or different from each other, are each hydrogen, hydroxyl, methyl, methoxy, halogen, methylenedioxy, --NH--R.sub.13 or --CONH.sub.2 ; andR.sub.13 is hydrogen, acyl or lower alkylsulfonyl;and non-toxic, pharmaceutically acceptable acid addition salts thereof; the compounds as well as their salts are useful for the treatment of asthma, bronchitis, urticaria, conjunctivities, hay fever, colds and cardiovascular disorders, and for relaxation of the uterine musculature.
摘要翻译：其中A是单键的式“IMAGE”的化合物，R 1是-OH，-O-酰基，氯或氢; R2是氢，甲基或乙基; R3为 m为2,3或4; n为1,2或3; R4是氢或低级烷基; R5是氢，低级烷基，或当R4是氢时也是苯基; R6，R7和R8各自为氢或甲基; R9是氢，-Ar，-OAr或-NH-CO-Ar; Ar可以相同或不同，分别是氢，羟基，甲基，甲氧基，卤素，亚甲二氧基，-NH-R13或-CONH 2; R 1，R 2，和R 13是氢，酰基或低级烷基磺酰基; 和无毒的药学上可接受的酸加成盐; 化合物及其盐可用于治疗哮喘，支气管炎，荨麻疹，结膜炎，花粉症，感冒和心血管疾病，以及用于放松子宫肌肉组织。

9. 发明授权

US4332802A 11-Oxo-11H-pyrido[2,1-b]quinazoline-2-carboxylic acid and salts thereof, antiallergic compositions containing it and methods of suppressing allergic reactions with it 失效
标题翻译： 11-氧代-11H-吡啶并[2,1-b]喹唑啉-2-羧酸及其盐，含有它的抗过敏组合物和抑制其过敏反应的方法
公开(公告)号：US4332802A
公开(公告)日：1982-06-01
申请号：US204226
申请日：1980-11-05
申请人： Kurt Schromm , Anton Mentrup , Ernst-Otto Renth , Armin Fugner
发明人： Kurt Schromm , Anton Mentrup , Ernst-Otto Renth , Armin Fugner
IPC分类号： C07D239/88 , A61K31/505 , A61K31/517 , A61K31/519 , A61P9/08 , A61P11/08 , A61P37/08 , C07D471/02 , C07D471/04 , C07D487/04 , C07D513/04
CPC分类号： C07D471/04 , C07D513/04 , Y10S514/826 , Y10S514/861 , Y10S514/912
摘要： This invention relates to the novel compound 11-oxo-11H-pyrido[2,1-b]quinazoline-2-carboxylic acid of the formula ##STR1## and non-toxic, pharmacologically acceptable salts thereof, as well as to pharmaceutical composition containing these compounds as active ingredients, and methods of using them as antiallergics.
摘要翻译：本发明涉及具有式“IMAGE”的新型化合物11-氧代-11H-吡啶并[2,1-b]喹唑啉-2-羧酸及其无毒的药理学上可接受的盐，以及含有这些化合物作为活性成分，以及将其用作抗过敏药物的方法。

10. 发明授权

US4241068A 2-(Pyridyl-amino)-benzoic acids and salts thereof 失效
标题翻译： 2-（吡啶基 - 氨基） - 苯甲酸及其盐
公开(公告)号：US4241068A
公开(公告)日：1980-12-23
申请号：US64355
申请日：1979-08-07
申请人： Kurt Schromm , Anton Mentrup , Ernst-Otto Renth , Armin Fugner , Volker Jacobi
发明人： Kurt Schromm , Anton Mentrup , Ernst-Otto Renth , Armin Fugner , Volker Jacobi
IPC分类号： A61K31/44 , A61K31/4402 , A61K31/4427 , A61K31/445 , A61K31/455 , A61K31/47 , A61K31/495 , A61K31/505 , A61P7/08 , A61P37/08 , C07D213/74 , C07D213/75 , C07D213/80 , C07D215/38 , C07D239/42 , C07D401/04 , C07D401/12 , C07D403/04
CPC分类号： C07D213/74 , C07D213/75 , C07D213/80 , C07D215/38 , C07D239/42
摘要： Compounds of the formula ##STR1## wherein A is .dbd.CH-- or .dbd.N--;R.sub.1 is (a) hydrogen, lower alkyl, lower alkoxy or a fused benzene ring, or (b) --CO--R.sub.4, tetrazol-5-yl or cyano in the 4- or 5-position;R.sub.2 is --CO--R.sub.4, tetrazol-5-yl, cyano or, when R.sub.1 has one of the meanings included in (b), also hydrogen, lower alkyl, lower alkoxy or a fused benzene ring;R.sub.3 is hydrogen or lower alkanoyl; andR.sub.4 is hydroxyl, amino, hydroxy-amino, tetrazol-5-yl-amino or lower alkoxy;internal salts thereof, and non-toxic salts thereof formed with a basic substance. The compounds as well as their salts are useful as antiallergics.
摘要翻译：式（Ⅰ）化合物，其中A为= CH-或= N-; R1是（a）氢，低级烷基，低级烷氧基或稠合苯环，或（b）在4-或5-位的-CO-R4，四唑-5-基或氰基; R 2为-CO-R 4，四唑-5-基，氰基，或者当R 1具有（b）中所述含义之一时，还有氢，低级烷基，低级烷氧基或稠合苯环; R3是氢或低级烷酰基; 和R4是羟基，氨基，羟基 - 氨基，四唑-5-基氨基或低级烷氧基; 其内盐和与碱性物质形成的无毒盐。化合物及其盐可用作抗过敏药。

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