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公开(公告)号:US5026705A
公开(公告)日:1991-06-25
申请号:US530520
申请日:1990-05-30
申请人: Helmut Prucher , Rochus Jonas , Jaime Piulats , Michael Klockow
发明人: Helmut Prucher , Rochus Jonas , Jaime Piulats , Michael Klockow
IPC分类号: A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/50 , A61P7/02 , A61P9/04 , A61P9/08 , C07D237/00 , C07D333/00 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
CPC分类号: C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要: New benzimidazolylpyridazinones of the formula I ##STR1## in which R.sup.1 is a styryl or mononculear of binuclear heteroaryl radical which contains 1-4 heteroatoms, each of which is unsubstituted or singly or multiply substituted by alkyl, alkoxy, alkylthio, halogen, OH, SH, amino, alkylamino, dialkylamino, acylamino having 1-8 C atoms, nitro, COOH, COOalkyl and/or CN,R.sup.2 R.sup.3, R.sup.4 and R.sup.5 are each H or alkyl andR.sup.6 and R.sup.7 are each H, or together are a C--C bond, and in which the alkyl and alkoxy groups each contain 1-4 C atoms,and their salts, show positive inotropic, vasodilating and antithrombotic actions.
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公开(公告)号:US4923869A
公开(公告)日:1990-05-08
申请号:US830781
申请日:1986-02-19
申请人: Helmut Prucher , Rochus Jonas , Jaime Piulats , Michael Klockow
发明人: Helmut Prucher , Rochus Jonas , Jaime Piulats , Michael Klockow
IPC分类号: A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/50 , A61P7/02 , A61P9/04 , A61P9/08 , C07D237/00 , C07D333/00 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
CPC分类号: C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要: New benzimidazolylpyridazinones of the formula I ##STR1## in which R.sup.1 is a styryl or mononuclear of binuclear heteroaryl radial which contains 1-4 heteroatoms, each of which is unsubstituted or singly or multiply substituted by alkyl, alkoxy, alkylthio, halogen, OH, SH, amino, alkylamino, dialkylamino, acylamino having 1-8 C atoms, nitro, COOH, COOalkyl and/or CN,R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each H or alkyl, andR.sup.6 and R.sup.7 are each H, or together are a C--C bond,and in which the alkyl and alkoxy groups each contain 1-4 C atoms,and their salts, show positive inotropic, vasodilating and antithrombotic actions.
摘要翻译: 式Ⅰ的新的苯并咪唑基哒嗪酮其中R 1是含有1-4个杂原子的双杂芳基杂环的苯乙烯基或单核,其各自是未被取代的或被烷基,烷氧基,烷硫基,卤素,OH, SH,氨基,烷基氨基,二烷基氨基,具有1-8个C原子的酰氨基,硝基,COOH,COO烷基和/或CN,R2,R3,R4和R5各自为H或烷基,R6和R7各自为H, CC键,其中烷基和烷氧基各自含有1-4个C原子,并且它们的盐显示正性肌力,血管扩张和抗血栓形成作用。
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公开(公告)号:US4916128A
公开(公告)日:1990-04-10
申请号:US202294
申请日:1988-06-06
IPC分类号: A61K31/54 , A61K31/55 , A61P7/02 , A61P9/00 , A61P9/08 , C07D417/04 , C07D417/14
CPC分类号: C07D417/04 , C07D417/14
摘要: Thiadiazinones of the formula I ##STR1## wherein A is --CHR.sup.4 --CHR.sup.5 --, --CH.sub.2 --CR.sup.4 R.sup.5 --, --CR.sup.4 R.sup.5 --CH.sub.2 --, --CHR.sup.4 --CHR.sup.5 --CH.sub.2 --, --CHR.sup.4 --CH.sub.2 --CHR.sup.5 --, --CH.sub.2 --CHR.sup.4 --CHR.sup.5 --, --CR.sup.4 R.sup.5 --CH.sub.2 CH.sub.2 --, --CH.sub.2 --CR.sup.4 R.sup.5 --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --CR.sup.4 R.sup.5 --,R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each independently H, C.sub.1-5 -alkyl, C.sub.2-5 -alkenyl or C.sub.2-5 -alkinyl,R.sup.3 is also C.sub.1-15 -acyl,R.sup.6 is H, alkyl, alkoxyl, OH, F, Cl, Br or I andZ is (H, H), (H, alkyl), (alkyl, alkyl) or O,the alkyl, alkenyl, alkinyl and/or alkoxy groups in each case containing up to 5 C atoms, but wherein, if A is --CH.sub.2 CH.sub.2 -- and Z is O, one of the radicals R.sup.1, R.sup.2, R.sup.3 and R.sup.6 must be other than H,and salts thereof demonstrate positive inotropic action and are suitable for combating cardiovascular diseases.
摘要翻译: 其中A是-CHR 4 -CHR 5 - , - CH 2 - CR 4 R 5 - , - CR 4 R 5 -CH 2 - , - CHR 4 -CHR 5 -CH 2 - , - CHR 4 -CH 2 - CHR 5 - , - CH 2 CHR 4 - CHR5-,-CR4R5-CH2CH2-,-CH2-CR4R5-CH2-或-CH2CH2-CR4R5-,R1,R2,R3,R4和R5各自独立地为H,C1-5烷基,C2-5-烯基或C2 -5-炔基,R 3还为C 1-15酰基,R 6为H,烷基,烷氧基,OH,F,Cl,Br或I,Z为(H,H),(H,烷基) )或O,每种情况下的烷基,烯基,炔基和/或烷氧基含有至多5个C原子,但其中,如果A是-CH 2 CH 2 - 并且Z是O,基团R 1,R 2,R 3和R 6中的一个 必须不是H,其盐表现出正性肌力作用,并且适用于对抗心血管疾病。
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公开(公告)号:US5137885A
公开(公告)日:1992-08-11
申请号:US811212
申请日:1991-12-20
CPC分类号: C07D417/04
摘要: Thiadiazinones of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the meaning given in claim 1, show positively inotropic and vasodilating action and are suitable for combating cardiovascular diseases.
摘要翻译: 其中R 1,R 2,R 3,R 4和R 5具有权利要求1中给出的含义的式I的噻二嗪酮显示出正的肌力和血管舒张作用,并且适用于对抗心血管疾病。
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公开(公告)号:US5869516A
公开(公告)日:1999-02-09
申请号:US648951
申请日:1996-05-16
IPC分类号: C12N9/99 , A61K31/415 , A61K31/4152 , A61K31/4155 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/496 , A61K31/535 , A61K31/5377 , A61K31/63 , A61P7/02 , A61P9/00 , A61P9/10 , A61P9/12 , A61P43/00 , C07D231/20 , C07D231/22 , C07D231/24 , C07D231/26 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D413/12 , C07F9/6503
CPC分类号: C07D401/04 , C07D231/20 , C07D403/04
摘要: 5-Pyrazolinone derivatives of the general formula I: ##STR1## in which the R.sup.1 -R.sup.3 variables are as defined herein and the physiologically acceptable salts thereof; processes for the preparation of these compounds, and in particular their use as selective inhibitors of cGMP-specific phosphodiesterase (cGMP PDE), thus as pharmaceutically active compounds.
摘要翻译: 通式I的5-吡唑啉酮衍生物:其中R1-R3变量如本文所定义,及其生理上可接受的盐; 这些化合物的制备方法,特别是其作为cGMP特异性磷酸二酯酶(cGMP PDE)的选择性抑制剂的用途,因此作为药物活性化合物。
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公开(公告)号:US5747489A
公开(公告)日:1998-05-05
申请号:US592659
申请日:1996-01-26
申请人: Rochus Jonas , Michael Wolf , Michael Klockow
发明人: Rochus Jonas , Michael Wolf , Michael Klockow
IPC分类号: A61K31/54 , A61K31/549 , A61P11/00 , A61P11/06 , A61P29/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D285/16 , C07D417/04 , C07D285/18
CPC分类号: C07D285/16
摘要: Arylalkyl-thiadiazinone derivatives of the formula I ##STR1## and physiologically unobjectionable salts thereof in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and Q have the meanings given in claim 1, exhibit phosphodiesterase IV inhibition and can be used for the therapy of asthmatic disorders.
摘要翻译: 其中R 1,R 2,R 3,R 4,R 5和Q具有权利要求1中给出的含义的式I化合物的芳基烷基 - 噻二嗪酮衍生物及其生理上无关的盐表现出磷酸二酯酶IV抑制,并且可用于治疗 哮喘性疾病
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公开(公告)号:US5434149A
公开(公告)日:1995-07-18
申请号:US220657
申请日:1994-03-31
IPC分类号: A61K31/54 , A61P9/08 , A61P11/00 , A61P25/24 , A61P25/26 , A61P25/28 , A61P29/00 , A61P43/00 , C07D285/16 , C07D285/18 , C07D417/04 , C07D417/06
CPC分类号: C07D285/16 , C07D417/04
摘要: The present invention relates to thiadiazinones of the formula I ##STR1## having a phosphodiesterase-inhibiting action and which are suitable for combating cardiovascular and asthmatic disorders.
摘要翻译: 本发明涉及具有磷酸二酯酶抑制作用并且适于对抗心血管和哮喘病症的式I的噻二嗪酮。
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公开(公告)号:US5378702A
公开(公告)日:1995-01-03
申请号:US89485
申请日:1993-07-16
申请人: Rochus Jonas , Ingeborg Lues , Klaus-Otto Minck , Michael Klockow
发明人: Rochus Jonas , Ingeborg Lues , Klaus-Otto Minck , Michael Klockow
IPC分类号: A61K31/54 , A61P9/00 , A61P9/06 , C07D207/09 , C07D211/26 , C07D215/14 , C07D223/24 , C07D285/08 , C07D417/04 , C07D417/14 , C07D417/02
CPC分类号: C07D417/04 , C07D417/14
摘要: Thiadiazinones of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n have the meaning given in claim 1, show antiarrhythmic action and are suitable for the control of cardiovascular disorders.
摘要翻译: 其中R 1,R 2,R 3,R 4,R 5和n具有权利要求1中给出的含义的式I的噻二嗪酮显示抗心律失常作用并且适合于控制心血管疾病。
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公开(公告)号:US5276027A
公开(公告)日:1994-01-04
申请号:US964686
申请日:1992-10-22
申请人: Rochus Jonas , Michael Klockow , Joachim Leibrock , Hans-Jochen Schliep , Christoph Seyfried , Michael Wolf
发明人: Rochus Jonas , Michael Klockow , Joachim Leibrock , Hans-Jochen Schliep , Christoph Seyfried , Michael Wolf
IPC分类号: A61K31/54 , A61K31/549 , A61P9/04 , A61P9/08 , A61P11/00 , A61P11/06 , A61P25/24 , A61P25/26 , A61P25/28 , A61P29/00 , A61P43/00 , C07D285/16
CPC分类号: C07D285/16
摘要: Compounds of formula I ##STR1## in which R.sup.1 and R.sup.2 are each independently of one another H or A,R.sup.3 is H, OA or O--C.sub.m H.sub.2m+1-n X.sub.n,R.sup.4 is --O--C.sub.m H.sub.2m+1-n X.sub.n,X is F or Cl,A is alkyl having 1-6 C atoms,m is 1, 2, 3, 4, 5 or 6 andn is 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12 or 13, and their salts have positive ionitropic activity and vasodilating action, and promote circulation. In addition, the compounds can be employed for the treatment of asthmatic disease and memory disorders, and have anti-depressive and anti-inflammatory properties.
摘要翻译: 其中R1和R2各自独立地为H或A,R3为H,OA或O-CmH2m + 1-nXn,R4为-O-CmH2m + 1-nXn的式I化合物,其中X为 F或Cl,A是具有1-6个C原子的烷基,m是1,2,3,4,5或6,n是1,2,3,4,5,6,7,8,9,10, 11,12或13,其盐具有阳离子活性和血管扩张作用,促进循环。 此外,该化合物可用于治疗哮喘病和记忆障碍,并具有抗抑郁和抗炎特性。
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公开(公告)号:US6025354A
公开(公告)日:2000-02-15
申请号:US8812
申请日:1998-01-20
申请人: Rochus Jonas , Michael Wolf , Michael Klockow
发明人: Rochus Jonas , Michael Wolf , Michael Klockow
IPC分类号: A61K31/54 , A61K31/549 , A61P11/00 , A61P11/06 , A61P29/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D285/16 , C07D417/04
CPC分类号: C07D285/16
摘要: Arylalkyl-thiadiazinone derivatives of the formula I ##STR1## and physiologically unobjectionable salts thereof in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and Q have the meanings given in claim 1, exhibit phosphodiesterase IV inhibition and can be used for the therapy of asthmatic disorders.
摘要翻译: R 1,R 2,R 3,R 4,R 5和Q具有权利要求1中给出的含义的式I的芳基烷基 - 噻二嗪酮衍生物及其生理上无反应的盐表现出磷酸二酯酶IV抑制,并且可用于治疗哮喘性疾病。
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