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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: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: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: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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公开(公告)号:US07491742B2
公开(公告)日:2009-02-17
申请号:US10750878
申请日:2004-01-05
IPC分类号: A61K31/415
CPC分类号: C07D491/04 , C07D495/04
摘要: Imidazole derivatives of the formula I in which R1 is H, A, benzyl, indan-5-yl, 1,2,3,4-tetrahydronaphthalen-5-yl, dibenzothien-2-yl, or phenyl which is unsubstituted or mono-, di- or trisubstituted by Hal, A, A-CO—NH, benzyloxy, alkoxy, COOH or COOA, R2 is H or A, X is O or S, Hal is F, Cl, Br or I, A is alkyl with 1 to 6 C atoms, and the physiologically acceptable salts and/or solvates thereof as phosphodiesterase VII inhibitors and the use thereof for producing a pharmaceutical.
摘要翻译: 式I的咪唑衍生物,其中R 1是H,A,苄基,茚满-5-基,1,2,3,4-四氢萘-5-基,二苯并噻吩-2-基或未取代或单 - ,Hal,A,A-CO-NH,苄氧基,烷氧基,COOH或COOA二取代或三取代,R 2为H或A,X为O或S,Hal为F,Cl,Br或I, 1至6个C原子,以及其作为磷酸二酯酶VII抑制剂的生理学上可接受的盐和/或溶剂合物及其用于制备药物的用途。
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公开(公告)号:US06376493B1
公开(公告)日:2002-04-23
申请号:US09830957
申请日:2001-05-03
申请人: Rochus Jonas , Michael Wolf , Franz-Werner Kluxen
发明人: Rochus Jonas , Michael Wolf , Franz-Werner Kluxen
IPC分类号: A61K3150
CPC分类号: C07D237/04
摘要: A group of compounds of, the preparation of, and the methods of use of benzoylpyridazine derivatives and the physiologically acceptable salts and solvates thereof, which have valuable pharmacological properties while well tolerated. They selectively inhibit phosphodiesterase IV with an intracellular increase in the CAMP level, and have an inhibitory effect on the formation of tumor necrosis factor.
摘要翻译: 苯甲酰基哒嗪衍生物的一组化合物,其制备方法和使用方法及其生理上可接受的盐和溶剂合物,其具有有价值的药理学性质,同时具有良好的耐受性。 它们选择性抑制磷酸二酯酶IV,细胞内CAMP水平升高,对肿瘤坏死因子的形成具有抑制作用。
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公开(公告)号:US06399611B1
公开(公告)日:2002-06-04
申请号:US08634830
申请日:1996-04-19
申请人: Rochus Jonas , Michael Wolf , Norbert Beier
发明人: Rochus Jonas , Michael Wolf , Norbert Beier
IPC分类号: C07D23704
CPC分类号: C07D237/04
摘要: Aralkylpyridazinone derivatives of the formula I and their physiologically acceptable salts in which R1, R2, R3, R4, R5 and Q have the meanings indicated in claim 1, show inhibition of phosphodiesterase IV and can be employed for the treatment of inflammatory processes and of allergies, asthma and autoimmune disorders.
摘要翻译: 式I的芳烷基哒嗪酮衍生物及其生理上可接受的盐,其中R 1,R 2,R 3,R 4,R 5和Q具有权利要求1所示的含义,表示磷酸二酯酶IV的抑制,并且可用于治疗炎症过程和过敏性哮喘 和自身免疫性疾病。
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公开(公告)号:US06884800B1
公开(公告)日:2005-04-26
申请号:US10129629
申请日:2000-10-31
IPC分类号: A61K31/5383 , A61K31/542 , A61P1/04 , A61P3/10 , A61P7/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/10 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/18 , A61P35/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D498/06 , C07D513/06 , A61K31/538 , A61K31/5415 , C07D413/02 , C07D417/02
CPC分类号: C07D513/06
摘要: Imidazole compounds of the formula I in which R1 and R2, independently of one another, each denote A1, OA1, SA1 or Hal, A1 denotes H, A, alkenyl, cycloalkyl or alkylenecycloalkyl, A denotes alkyl having 1-10 carbon atoms, Hal denotes F, Cl, Br or I, and X denotes O, S, SO or SO2, and their physiologically acceptable salts and/or solvates, as phosphodiesterase VII inhibitors, and their use for the preparation of a medicament.
摘要翻译: 其中R 1和R 2彼此独立的式I的咪唑化合物各自表示A 1,A 1, 或者Hal,A 1表示H,A,链烯基,环烷基或亚烷基环烷基,A表示具有1-10个碳原子的烷基,Hal表示F ,Cl,Br或I,X表示O,S,SO或SO 2,以及它们的生理学上可接受的盐和/或溶剂化物,作为磷酸二酯酶VII抑制剂,及其用于制备药物 。
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9.
公开(公告)号:US06531498B1
公开(公告)日:2003-03-11
申请号:US10129270
申请日:2002-05-03
IPC分类号: C07D26106
CPC分类号: A61K31/42
摘要: The invention relates to compounds of formula I and to their physiologically acceptable salts and solvates which act as phosphodiesterse VII inhibitors and are thus useful for the treatment of allergic disorders, asthma, chronic bronchitis, atopic dermatitis, psoriasis and other skin disorders, inflammatory disorders, autoimmune diseases, rheumatoid arthritis, multiple sclerosis, Crohn's disease, diabetes mellitus or ulcerative colitis, osteoporosis, transplant rejection reactions, cachexia, tumor growth, tumor metastases, sepsis, memory disturbances, atherosclerosis and AIDS.
摘要翻译: 本发明涉及式I化合物及其作为磷酸二酯VII抑制剂的生理上可接受的盐和溶剂合物,因此可用于治疗过敏性疾病,哮喘,慢性支气管炎,特应性皮炎,牛皮癣和其他皮肤病,炎症性疾病, 自身免疫疾病,类风湿性关节炎,多发性硬化,克罗恩病,糖尿病或溃疡性结肠炎,骨质疏松症,移植排斥反应,恶病质,肿瘤生长,肿瘤转移,败血症,记忆障碍,动脉粥样硬化和艾滋病。
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公开(公告)号:US06737436B1
公开(公告)日:2004-05-18
申请号:US10129261
申请日:2002-05-03
IPC分类号: A61K31402
CPC分类号: C07D207/34
摘要: Compounds of the formula I in which R1 and R2, independently of one another, each denote H, A, OA, SA or HaI, R3 denotes H or A, R4 denotes A or NH2, R5 denotes H, NH2, NHA or NA2, A denotes alkyl having 1 to 10 carbon atoms, alkenyl, cycloalkyl or alkylenecycloalkyl, Hal denotes F, Cl, Br or I, and their physiologically acceptable salts and/or solvates, as phosphodiesterase VII inhibitors.
摘要翻译: R 1和R 2彼此独立的式Iin的化合物各自表示H,A,OA,SA或HaI,R 3表示H或A,R 4表示A或NH 2, R 5表示H,NH 2,NHA或NA 2,A表示具有1至10个碳原子的烷基,烯基,环烷基或亚烷基环烷基,Hal表示F,Cl,Br或I及其生理学上可接受的盐和/或溶剂化物, 磷酸二酯酶VII抑制剂。
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