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21. 发明授权

US5541229A Benzimidazoles and medicaments containing these compounds 失效
标题翻译：苯并咪唑和含有这些化合物的药物
公开(公告)号：US5541229A
公开(公告)日：1996-07-30
申请号：US227291
申请日：1994-04-13
申请人： Berthold Narr , Andreas Bomhard , Norbert Hauel , Jacques Van Meel , Wolfgang Wienen , Michael Entzeroth
发明人： Berthold Narr , Andreas Bomhard , Norbert Hauel , Jacques Van Meel , Wolfgang Wienen , Michael Entzeroth
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/425 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/5355 , A61P1/00 , A61P3/10 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P13/02 , A61P13/10 , A61P15/00 , A61P27/02 , A61P27/06 , C07D235/02 , C07D235/04 , C07D235/06 , C07D235/08 , C07D235/12 , C07D235/16 , C07D235/18 , C07D235/24 , C07D235/26 , C07D235/28 , C07D235/30 , C07D401/04 , C07D403/04 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D417/04 , C07D417/12 , C07D487/04 , C07D495/14 , C07D513/04 , C07D521/00 , A61K31/41
CPC分类号： C07D235/02 , C07D231/12 , C07D233/56 , C07D235/06 , C07D235/08 , C07D235/12 , C07D235/18 , C07D235/24 , C07D235/26 , C07D235/28 , C07D235/30 , C07D249/08 , C07D401/04 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/12 , C07D417/04 , C07D417/12 , C07D487/04 , C07D513/04
摘要： The invention relates to benzimidazoles of the formula ##STR1## in which R.sub.1 to R.sub.2 are as defined in claim 1,1 and 3 isomer mixtures thereof and addition salts thereof which have valuable properties.In particular, the novel compounds are angiotensin II antagonists.
摘要翻译：本发明涉及式（I）的苯并咪唑，其中R1至R2如权利要求1,1,3和3所述的异构体混合物及其加成盐具有有价值的性质。特别地，新化合物是血管紧张素II拮抗剂。

22. 发明授权

US5175157A Cyclic amine derivatives, pharmaceutical compositions containing these compounds and methods for preparing them 失效
标题翻译：环胺衍生物，含有这些化合物的药物组合物及其制备方法
公开(公告)号：US5175157A
公开(公告)日：1992-12-29
申请号：US725855
申请日：1991-07-03
申请人： Manfred Psiorz , Joachim Heider , Andreas Bomhard , Manfred Reiffen , Norbert Hauel , Klaus Noll , Berthold Narr , Christian Lillie , Walter Kobinger , Jurgen Dammgen
发明人： Manfred Psiorz , Joachim Heider , Andreas Bomhard , Manfred Reiffen , Norbert Hauel , Klaus Noll , Berthold Narr , Christian Lillie , Walter Kobinger , Jurgen Dammgen
IPC分类号： C07D223/16 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D491/04
CPC分类号： C07D223/16 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D491/04
摘要： Disclosed are new cyclic amine derivatives of the formula I ##STR1## wherein the substituents are defined in the specification. These compounds are useful as for treating sinus tachycardia.
摘要翻译：公开了式I（I）的新的环胺衍生物，其中取代基在说明书中定义。这些化合物可用于治疗窦性心动过速。

23. 发明授权

US5116986A Heteroaromatic amine derivatives 失效
标题翻译：异构胺衍生物
公开(公告)号：US5116986A
公开(公告)日：1992-05-26
申请号：US696677
申请日：1991-05-07
申请人： Andreas Bomhard , Joachim Heider , Manfred Psiorz , Norbert Hauel , Berthold Narr , Klaus Noll , Christian Lillie , Walter Kobinger , Willi Diederen
发明人： Andreas Bomhard , Joachim Heider , Manfred Psiorz , Norbert Hauel , Berthold Narr , Klaus Noll , Christian Lillie , Walter Kobinger , Willi Diederen
IPC分类号： A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/472 , A61P9/00 , A61P9/08 , A61P9/10 , C07D209/44 , C07D209/46 , C07D209/48 , C07D217/04 , C07D217/08 , C07D217/14 , C07D217/22 , C07D217/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D491/04 , C07D491/056
CPC分类号： C07D209/48 , C07D209/44 , C07D209/46 , C07D217/14 , C07D217/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D491/04
摘要： The present invention relates to new heteroaromatic amine derivatives of general formula ##STR1## wherein the substituents are defined hereinbelow, which have valuable pharmacological properties, particularly a heart rate lowering activity and a positive inotropic activity.

24. 发明授权

US4714698A 8-alkylthio-2-piperazino-pyrimido[5,4-d]-pyrimidines 失效
标题翻译： 8-烷硫基-2-哌嗪基 - 嘧啶并[5,4-d] - 嘧啶
公开(公告)号：US4714698A
公开(公告)日：1987-12-22
申请号：US745095
申请日：1985-06-17
申请人： Josef Roch , Armin Heckel , Josef Nickl , Erich Muller , Berthold Narr , Rainer Zimmermann , Johannes Weisenberger
发明人： Josef Roch , Armin Heckel , Josef Nickl , Erich Muller , Berthold Narr , Rainer Zimmermann , Johannes Weisenberger
IPC分类号： A61K31/505 , A61K31/55 , A61P7/02 , A61P9/10 , A61P35/00 , C07D487/04 , C07D471/04
CPC分类号： C07D487/04
摘要： The invention relates to new compounds of general formula ##STR1## wherein R.sub.1 represents an alkyl group,R.sub.2 represents a hydrogen atom, an alkyl group optionally substituted (except at the .alpha. carbon atom) by a hydroxy group, or represents a cycloalkyl group or an allyl, phenyl or benzyl group,R.sub.3 represents an allyl group, an alkyl group optionally substituted (except at the .alpha. carbon atom) by a hydroxy group, or represents a cycloalkyl group orR.sub.2 and R.sub.3 together with the nitrogen atom between them represent a straight-chained alkyleneimino group,the acid addition salts thereof, particularly the acid addition salts thereof with physiologically acceptable inorganic or organic acids which have valuable pharmacological properties, particularly a metastasis-inhibiting effect based on their selective tumour-PDE inhibiting effect, and pharmaceutical compositions containing these compounds or the physiologically acceptable acid addition salts thereof.The new compounds may be prepared according to methods known for analogous compounds.
摘要翻译：本发明涉及通式（I）的新化合物，其中R 1表示烷基，R 2表示氢原子，任选被羟基取代的烷基（除了在α碳原子上），或表示环烷基基团或烯丙基，苯基或苄基，R 3表示烯丙基，任选被羟基取代的烷基（除了在α碳原子上），或表示环烷基或R 2和R 3以及它们之间的氮原子代表直链亚烷基亚氨基，其酸加成盐，特别是其酸加成盐与具有有价值的药理学性质的生理上可接受的无机或有机酸，特别是基于其选择性肿瘤-PDE抑制作用的转移抑制作用，以及含有这些化合物的药物组合物或其生理上可接受的酸加成盐。新化合物可以根据类似化合物已知的方法制备。

25. 发明授权

US4629733A Indolinones and pharmaceutical compositions containing same 失效
标题翻译：含吲哚酮和含有它们的药物组合物
公开(公告)号：US4629733A
公开(公告)日：1986-12-16
申请号：US625020
申请日：1984-07-27
申请人： Erich Muller , Josef Nickl , Josef Roch , Berthold Narr
发明人： Erich Muller , Josef Nickl , Josef Roch , Berthold Narr
IPC分类号： C07D209/12 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/4427 , A61P7/02 , C07D209/34 , C07D401/12
CPC分类号： C07D209/34
摘要： The present invention relates to novel indolinones of the general formula ##STR1## wherein R represents an aryl group having from 6 to 10 carbon atoms, unsubstituted or mono- or disubstituted by alkyl groups having from 1 to 5 carbon atoms, hydroxyl groups, alkoxy groups having from 1 to 3 carbon atoms, or halogen atoms, whereby the substituents may be the same or different and whereby the phenyl nucleus of the aryl group may also be substituted by an amino group, a hydroxyl group, or an alkanoylamino group with altogether from 1 to 3 carbon atoms; an aryl group having from 6 to 10 carbon atoms, substituted by 3 or 4 alkyl groups having from 1 to 5 carbon atoms each; a phenyl group substituted by a phenyl, halogenphenyl, or cycloalkyl group with 5 to 7 carbon atoms; an aralkyl group having from 7 to 11 carbon atoms; or a pentamethylphenyl, pyridyl, or quinolyl group; m represents the number 0, 1, or 2; and n represents the number 2, 3, 4, 5, or 6.
摘要翻译：本发明涉及通式为“IMAGE”的新的二氢吲哚酮，其中R代表具有6至10个碳原子的芳基，未被取代或被具有1至5个碳原子的烷基单羟基或二取代，羟基，烷氧基具有1至3个碳原子或卤素原子，其中取代基可以相同或不同，由此芳基的苯基也可以被氨基，羟基或烷酰基氨基取代，其总共从 1至3个碳原子; 具有6至10个碳原子的芳基，被3或4个具有1至5个碳原子的烷基取代; 被苯基，卤素苯基或具有5至7个碳原子的环烷基取代的苯基; 具有7至11个碳原子的芳烷基; 或五甲基苯基，吡啶基或喹啉基; m表示数字0，1或2; n表示数字2,3,4,5或6。

26. 发明授权

US4560685A 2-Piperazino-pteridines useful as antithrombotics and antimetastatics 失效
标题翻译： 2-Piperazino-pteridines可用作抗血栓形成和抗转移
公开(公告)号：US4560685A
公开(公告)日：1985-12-24
申请号：US621438
申请日：1984-06-18
申请人： Josef Roch , Josef Nickl , Erich Muller , Berthold Narr , Johannes Weisenberger , Rainer Zimmermann , Walter Haarmann
发明人： Josef Roch , Josef Nickl , Erich Muller , Berthold Narr , Johannes Weisenberger , Rainer Zimmermann , Walter Haarmann
IPC分类号： C07D475/06 , C07D475/08 , A61K31/505
CPC分类号： C07D475/06 , C07D475/08
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is phenylalkylamino, alkylamino, dialkylamino, piperidino, morpholino, thiomorpholino or 1-oxido-thiomorpholino;R.sub.2 is dialkylamino, piperidino, morpholino, thiomorpholino or 1-oxido-thiomorpholino; andR.sub.3 is halogen, alkoxy, alkylthio, phenylalkoxy or phenylalkylthio;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antithrombotics and antimetastatics.
摘要翻译：其中R 1是苯基烷基氨基，烷基氨基，二烷基氨基，哌啶子基，吗啉代，硫代吗啉代或1-氧代硫代吗啉代; R2是二烷基氨基，哌啶子基，吗啉代，硫代吗啉代或1-氧代硫代吗啉代; R3是卤素，烷氧基，烷硫基，苯基烷氧基或苯基烷硫基; 和无毒的，药学上可接受的酸加成盐。化合物及其盐可用作抗血栓形成和抗转移酶。

27. 发明授权

US4551464A Antithrombotic sulfoximino carbostyrils 失效
标题翻译：抗血栓形式的磺酰亚胺喹诺酮类
公开(公告)号：US4551464A
公开(公告)日：1985-11-05
申请号：US573964
申请日：1984-01-26
申请人： Erich Muller , Josef Nickl , Berthold Narr , Josef Roch , Walter Haarmann , Johannes M. Weisenberger
发明人： Erich Muller , Josef Nickl , Berthold Narr , Josef Roch , Walter Haarmann , Johannes M. Weisenberger
IPC分类号： A61K31/40 , A61K31/455 , A61K31/47 , C07D209/34 , C07D215/22 , C07D215/227 , C07D401/02 , C07D401/12 , C07D409/02 , C07D409/12
CPC分类号： C07D215/227 , C07D209/34 , C07D401/12 , C07D409/12
摘要： Compounds of the formula ##STR1## wherein n is 0 or 1;A is methylene, vinylene or ethylene optionally substituted by lower alkyl;B is alkylene;R.sub.1 is an optionally substituted alkyl, phenyl or naphthyl group, or a cycloalkyl or pyridyl group; andR.sub.2 is hydrogen or acyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antithrombotics.
摘要翻译：其中n为0或1的式（I）的化合物; A是任选被低级烷基取代的亚甲基，亚乙烯基或乙烯基; B是亚烷基; R1是任选取代的烷基，苯基或萘基，或环烷基或吡啶基; 并且R 2是氢或酰基; 和无毒的，药学上可接受的酸加成盐。化合物及其盐可用作抗血栓形成剂。

28. 发明授权

US4260621A 3-Amino-4-phenyl-6-piperidino-1H-pyrazolo[3,4-b]-pyridines and salts thereof 失效
标题翻译： 3-氨基-4-苯基-6-哌啶子基-1H-吡唑并[3,4-b] - 吡啶及其盐
公开(公告)号：US4260621A
公开(公告)日：1981-04-07
申请号：US75100
申请日：1979-09-13
申请人： Josef Roch , Erich Muller , Berthold Narr , Josef Nickl , Walter Haarmann
发明人： Josef Roch , Erich Muller , Berthold Narr , Josef Nickl , Walter Haarmann
IPC分类号： A61K31/435 , A61P7/02 , A61P29/00 , C07D213/85 , C07D471/04 , A61K31/445
CPC分类号： C07D471/04 , C07D213/85 , Y10S514/822
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is unsubstituted, mono-substituted or di-substituted piperidino, where the substituents are selected from the group consisting of methyl, hydroxymethyl, hydroxyl, phenyl and benzyl;R.sub.2 is hydrogen, methyl or benzyl; andR.sub.3 is hydrogen, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 3 carbon atoms;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antiphlogistics and antithrombotics.
摘要翻译：其中R 1是未取代的，单取代的或二取代的哌啶子基，其中取代基选自甲基，羟甲基，羟基，苯基和苄基; R2是氢，甲基或苄基; R3为氢，卤素，1〜3个碳原子的烷基或1〜3个碳原子的烷氧基; 和无毒的，药学上可接受的酸加成盐。化合物及其盐可用作消炎和抗血栓形成。

29. 发明授权

US4191776A Biphenyl derivatives 失效
标题翻译：联苯衍生物
公开(公告)号：US4191776A
公开(公告)日：1980-03-04
申请号：US852714
申请日：1977-11-18
申请人： Josef Nickl , Erich Muller , Berthold Narr , Walter Haarmann , Wolfgang Schroter , Rudolf Kadatz
发明人： Josef Nickl , Erich Muller , Berthold Narr , Walter Haarmann , Wolfgang Schroter , Rudolf Kadatz
IPC分类号： C07C67/00 , C07C69/76 , C07C313/00 , C07C315/04 , C07C317/10 , C07C317/18 , C07C317/24 , C07C317/44 , C07C323/16 , C07C323/45 , C07C323/52 , C07C323/60 , C07C323/65 , C07D213/30 , C07D295/185 , C07C147/107 , A61K31/235 , A61K31/44 , C07C147/14
CPC分类号： C07D213/30 , C07C317/10 , C07C317/18 , C07C317/24 , C07C317/44 , C07C323/16 , C07C323/45 , C07C323/52 , C07C323/60 , C07C323/65 , C07D295/185 , Y10S514/822
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, fluorine, chlorine, bromine, methyl, methoxy, methylthio or cyano;R.sub.2 is hydrogen or fluorine;R.sub.3 is carboxyl, (alkoxy of 1 to 6 carbon atoms)-carbonyl, methoxy-(alkoxy of 1 to 6 carbon atoms)-carbonyl, (alkenyloxy of 2 to 6 carbon atoms)-carbonyl, (aralkoxy of 7 to 12 carbon atoms)-carbonyl, phenoxy-carbonyl or pyridyl-methoxy-carbonyl,A is (alkyl of 1 to 3 carbon atoms)-methylene,m is 1 or 2; andn is 0, 1, 2 or 3;and, when R.sub.3 is carboxyl, non-toxic salts thereof formed with an inorganic or organic base. The compounds as well as the salts are useful as antithrombotics, anticholesteremics and anticoagulants.
摘要翻译：其中R 1是氢，氟，氯，溴，甲基，甲氧基，甲硫基或氰基的式 R2是氢或氟; R 3为羧基，（碳原子数1〜6的烷氧基） - 羰基，甲氧基 - （1〜6个碳原子的烷氧基） - 羰基，（2〜6个碳原子的烯氧基） - 羰基，（碳原子数为7〜12）） - 羰基，苯氧基 - 羰基或吡啶基 - 甲氧基 - 羰基，A是（1至3个碳原子的烷基） - 亚甲基，m是1或2; 并且n为0,1,2或3; 并且当R 3为羧基时，其无毒盐与无机或有机碱形成。化合物以及盐可用作抗血栓形成剂，抗胆固醇剂和抗凝剂。

30. 发明授权

US3993683A Biphenylyl derivatives 失效
标题翻译：联苯衍生物
公开(公告)号：US3993683A
公开(公告)日：1976-11-23
申请号：US577169
申请日：1975-05-14
申请人： Josef Nickl , Erich Muller , Berthold Narr , Walter Haarmann , Wolfgang Schroter , Rudolf Kadatz
发明人： Josef Nickl , Erich Muller , Berthold Narr , Walter Haarmann , Wolfgang Schroter , Rudolf Kadatz
IPC分类号： C07C67/00 , C07C69/76 , C07C313/00 , C07C315/04 , C07C317/10 , C07C317/18 , C07C317/24 , C07C317/44 , C07C323/16 , C07C323/45 , C07C323/52 , C07C323/60 , C07C323/65 , C07D213/30 , C07D295/185 , C07C149/40
CPC分类号： C07D213/30 , C07C317/10 , C07C317/18 , C07C317/24 , C07C317/44 , C07C323/16 , C07C323/45 , C07C323/52 , C07C323/60 , C07C323/65 , C07D295/185 , Y10S514/822
摘要： Compounds of the formula ##SPC1##WhereinR.sub.1 is hydrogen, fluorine, bromine, methyl, methoxy, methylthio, nitro, cyano or, when A is other than methylene, R.sub.2 is hydrogen, R.sub.3 is carboxyl, m is 2 and n is 0, also chlorine;R.sub.2 is hydrogen or fluorine;R.sub.3 is hydrogen, methyl, hydroxymethyl, carboxyl, (alkoxy of 1 to 6 carbon atoms)-carbonyl, methoxy-(alkoxy of 1 to 6 carbon atoms)-carbonyl, (alkenyloxy of 2 to 6 carbon atoms)-carbonyl, (aralkoxy of 7 to 12 carbon atoms)-carbonyl, phenoxy-carbonyl, pyridylmethoxy-carbonyl, amino-carbonyl, (alkyl of 1 to 3 carbon atoms-amino)-carbonyl, (dialkyl of 1 to 3 carbon atoms-amino)-carbonyl, phenylamino-carbonyl, morpholino-carbonyl, piperidino-carbonyl, thiomorpholino-carbonyl, (1-oxidothiomorpholino)-carbonyl or (1,1-dioxido-thiomorpholino)-carbonyl;A is methylene, (alkyl of 1 to 3 carbon atoms)-methylene, di-(alkyl of 1 to 3 carbon atoms)-methylene, hydroxymethyl-methylene, hydroxymethylene or carbonyl;m is 1 or 2; andn is 0, 1, 2 or 3;And, when R.sub.3 is carboxyl, non-toxic salts thereof formed with an inorganic or organic base. The compounds as well as the salts are useful as antithrombotics, anticholesteremics and anticoagulants.
摘要翻译：式A的化合物是氢，氟，溴，甲基，甲氧基，甲硫基，硝基，氰基，或当A不是亚甲基时，R 2是氢，R 3是羧基，m是2，n是0，也是氯; R2是氢或氟; R 3是氢，甲基，羟甲基，羧基，（1至6个碳原子的烷氧基） - 羰基，甲氧基 - （1至6个碳原子的烷氧基） - 羰基，（2至6个碳原子的链烯氧基） - 羰基 7至12个碳原子的羰基，苯氧基 - 羰基，吡啶基甲氧羰基，氨基 - 羰基，（1至3个碳原子的烷基 - 氨基） - 羰基，（1至3个碳原子的二烷基 - 氨基） - 羰基，苯基氨基羰基，吗啉代羰基，哌啶子基 - 羰基，硫代吗啉代羰基，（1-氧硫基吗啉代）羰基或（1,1-二氧化硫代吗啉代）羰基。 A是亚甲基，（1至3个碳原子的烷基） - 亚甲基，二（1至3个碳原子的烷基） - 亚甲基，羟甲基 - 亚甲基，羟基亚甲基或羰基; M IS 1 OR 2; 和N是0,1,2或3; 当R 3为羧基时，其无机盐与无机或有机碱形成。化合物以及盐可用作抗血栓形成剂，抗胆固醇剂和抗凝剂。

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