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81.
公开(公告)号:US6037377A
公开(公告)日:2000-03-14
申请号:US460961
申请日:1995-06-05
申请人: Ralf Anderskewitz , Kurt Schromm , Ernst-Otto Renth , Frank Himmelsbach , Franz Birke , Armin Fugner
发明人: Ralf Anderskewitz , Kurt Schromm , Ernst-Otto Renth , Frank Himmelsbach , Franz Birke , Armin Fugner
IPC分类号: C07C257/18 , A61K31/155 , A61K31/34 , A61K31/343 , A61K31/35 , A61K31/352 , A61K31/357 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/44 , A61P1/04 , A61P11/00 , A61P11/06 , A61P17/06 , A61P29/00 , A61P37/08 , C07C303/40 , C07C311/29 , C07C315/04 , C07C317/18 , C07C317/22 , C07C317/44 , C07C319/20 , C07C323/18 , C07C323/20 , C07C323/32 , C07C323/62 , C07D213/78 , C07D231/00 , C07D263/32 , C07D277/00 , C07D307/78 , C07D307/79 , C07D311/22 , C07D317/66 , C07D319/18 , C07D333/00 , C07D333/38
CPC分类号: C07D213/78 , C07C257/18 , C07C317/18 , C07C317/22 , C07C317/44 , C07C323/20 , C07C323/62 , C07D307/79 , C07D311/22
摘要: Compounds of the formula ##STR1## which is explained more fully in the specification, may be prepared by conventional methods and used therapeutically in conventional galenic preparations.
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82.Pyrimido�5,4!-dipyrimidines, pharmaceuticals containing them, their use and processes for the preparation thereof 失效
标题翻译: 嘧啶并[5,4] - 二嘧啶,含有它们的药物,其用途和制备方法公开(公告)号:US5821240A
公开(公告)日:1998-10-13
申请号:US811907
申请日:1997-03-05
IPC分类号: A61K31/00 , A61K31/505 , A61K31/519 , A61K31/529 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61K31/541 , A61K31/55 , A61K31/551 , A61P17/00 , A61P17/06 , A61P35/00 , A61P37/00 , A61P43/00 , C07D487/04 , C07D519/00
CPC分类号: C07D487/04
摘要: Pyrimido�5,4-d!pyrimidines of the general formula ##STR1## which have an inhibitory effect on signal transduction mediated by tyrosine kinases, their use for the treatment of disorders, in particular of oncoses, and their preparation. Exemplary compounds are: 4-�(3-Chloro-4-fluorophenyl)amino!-6-�1-methyl-4-piperidinylamino!pyrimido�5,4-d!pyrimidine, and 4-�(3-Chloro-4-fluorophenyl)amino!-6-�trans-4-dimethyl-aminocycohexylamino!pyrimido�5,4-d!pyrimidine.
摘要翻译: 对通过酪氨酸激酶介导的信号转导具有抑制作用的通式为(IMA)的吡啶并[5,4-d]嘧啶,其用于治疗疾病,特别是肿瘤的用途及其制备。 示例性的化合物是:4 - [(3-氯-4-氟苯基)氨基] -6- [1-甲基-4-哌啶基氨基]吡啶并[5,4-d]嘧啶和4 - [(3-氯 - 4-氟苯基)氨基] -6- [反式-4-二甲基 - 氨基胞嘧啶]嘧啶并[5,4-d]嘧啶。
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83.Biphenyl derivatives, pharmaceutical compositions containing these compounds and processes for preparing them 失效
标题翻译: 联苯衍生物,含有这些化合物的药物组合物及其制备方法公开(公告)号:US5736559A
公开(公告)日:1998-04-07
申请号:US691107
申请日:1996-08-01
申请人: Frank Himmelsbach , Helmut Pieper , Volkhard Austel , Gunter Linz , Thomas Muller , Wolfgang Eisert , Johannes Weisenberger
发明人: Frank Himmelsbach , Helmut Pieper , Volkhard Austel , Gunter Linz , Thomas Muller , Wolfgang Eisert , Johannes Weisenberger
IPC分类号: C07C211/44 , A61K38/00 , C07C211/48 , C07C211/50 , C07C211/53 , C07C233/65 , C07C237/36 , C07C237/38 , C07C243/22 , C07C255/54 , C07C255/56 , C07C255/57 , C07C255/58 , C07C255/59 , C07C255/60 , C07C257/18 , C07C271/64 , C07C275/28 , C07C275/32 , C07C275/38 , C07C275/42 , C07C279/18 , C07C307/10 , C07C309/11 , C07C311/04 , C07C311/06 , C07C311/08 , C07C311/11 , C07C311/16 , C07C311/19 , C07C311/21 , C07C311/29 , C07C317/14 , C07C317/44 , C07C317/46 , C07C321/24 , C07C323/60 , C07C323/62 , C07D207/08 , C07D207/26 , C07D211/34 , C07D211/60 , C07D211/62 , C07D211/70 , C07D257/04 , C07D295/192 , C07F9/40 , C07K5/06 , A61K31/445 , A61K31/40 , A61K31/495 , C07D211/06 , C07D295/185
CPC分类号: C07D295/192 , C07C237/36 , C07C237/38 , C07C243/22 , C07C255/56 , C07C255/57 , C07C255/59 , C07C255/60 , C07C257/18 , C07C271/64 , C07C275/42 , C07C307/10 , C07C309/11 , C07C311/04 , C07C311/06 , C07C311/08 , C07C311/19 , C07C311/21 , C07C311/29 , C07C317/44 , C07C317/46 , C07C323/60 , C07C323/62 , C07D211/34 , C07D211/60 , C07D211/62 , C07D211/70 , C07K5/06026 , A61K38/00 , C07C2101/14
摘要: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.
摘要翻译: 本发明涉及通式为(I)的联苯衍生物,其中A至E和X如权利要求1所定义,其立体异构体包括它们的混合物及其盐,特别是其与无机或有机物的生理上可接受的盐 酸或碱,其具有有价值的性质,优选聚集抑制作用,含有这些化合物的药物组合物及其制备方法。
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84.Piperazine derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them 失效
标题翻译: 哌嗪衍生物,含有这些化合物的药物组合物,其用途和制备方法公开(公告)号:US5700801A
公开(公告)日:1997-12-23
申请号:US572256
申请日:1995-12-13
申请人: Helmut Pieper , Volkhard Austel , Frank Himmelsbach , Gunter Linz , Brian Guth , Johannes Weisenberger
发明人: Helmut Pieper , Volkhard Austel , Frank Himmelsbach , Gunter Linz , Brian Guth , Johannes Weisenberger
IPC分类号: C07D295/18 , A61K31/495 , A61P7/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D211/34 , C07D211/58 , C07D213/74 , C07D213/78 , C07D401/12 , C07D211/18
CPC分类号: C07D213/74 , C07D211/34 , C07D211/58 , C07D401/12
摘要: Piperazine derivatives useful in the treatment or prevention of inflammation, bone degradation, thrombosis and tumor metastasis. Exemplary species are: (a) �4-trans-�3-�4-(4-Pyridyl)-piperazin-1-yl!propionyl!amino!-cyclohexanecarboxylic acid, (b) 3-�4-trans-�4-(4-Pyridyl)-piperazin-1-yl!carbonylamino!-cyclohexylpropionic acid, (c) 3-�4-trans-�4-(4-Pyridyl)-piperazin-1-yl!malonylamino!cyclohexylcarboxylic acid, (d) Methyl �4-trans-�3-�4-(4-pyridyl)-piperazin-1-yl!-propionyl!-amino!cyclohexane carboxylate, (e) Methyl 3-�4-trans-�4-(4-pyridyl)-piperazin-1-yl!-carbonylamino!cyclohexyl propionate, (f) Methyl �4-trans-�4-(4-pyridyl)-piperazin-1-yl!-malonylamino!-cyclohexyl carboxylate, (g) Cyclohexyl �4-trans-��4-(4-pyridyl)-piperazin-1-yl!-acetyl!-amino!-cyclohexane carboxylate, and (h) Isobutyl �4-trans-��4-(4-pyridyl)-piperazin-1-yl!-acetyl!-amino!-cyclohexane carboxylate.
摘要翻译: 哌嗪衍生物可用于治疗或预防炎症,骨退化,血栓形成和肿瘤转移。 示例性物质是:(a)[4-反式 - [3- [4-(4-吡啶基) - 哌嗪-1-基]丙酰基]氨基] - 环己烷甲酸,(b)3- [4-反式 - [4 - (4-吡啶基) - 哌嗪-1-基]羰基氨基] - 环己基丙酸,(c)3- [4-反式 - [4-(4-吡啶基) - 哌嗪-1-基]丙二酰氨基]环己基羧酸, d)[4-反式 - [3- [4-(4-吡啶基) - 哌嗪-1-基] - 丙酰基] - 氨基]环己烷羧酸甲酯,(e)3- [4-反式 - [4- 4-吡啶基) - 哌嗪-1-基] - 羰基氨基]环己基丙酸酯,(f)[4-反式 - [4-(4-吡啶基) - 哌嗪-1-基] - 丙酰基氨基] )[4-反式 - [[4-(4-吡啶基) - 哌嗪-1-基] - 乙酰基] - 氨基] - 环己烷羧酸环己酯和(h)[4-反式 - [[4- 吡啶基) - 哌嗪-1-基] - 乙酰基] - 氨基] - 环己烷羧酸酯。
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85.Cyclic imino derivatives, processes for preparing them and pharmaceutical compositions containing these compounds 失效
标题翻译: 环状亚氨基衍生物,其制备方法和含有这些化合物的药物组合物公开(公告)号:US5576444A
公开(公告)日:1996-11-19
申请号:US53037
申请日:1993-04-26
申请人: Frank Himmelsbach , Austel Volkhard , Helmut Pieper , Guenter Linz , Johannes Weisenberger , Thomas Mueller
发明人: Frank Himmelsbach , Austel Volkhard , Helmut Pieper , Guenter Linz , Johannes Weisenberger , Thomas Mueller
IPC分类号: A61K31/40 , A61K31/34 , A61K31/4015 , A61K31/4025 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/535 , A61K31/675 , A61P7/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D207/08 , C07D207/26 , C07D207/267 , C07D207/27 , C07D207/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07F9/24 , C07F9/572
CPC分类号: C07D207/26 , C07D401/12 , C07D405/12 , C07F9/5727
摘要: Cyclic imino derivatives of the formulaB--X.sub.2 --X.sub.1 --A--Y--E (I)wherein A, B, E, X.sub.1, X.sub.2 and Y are as defined herein, the stereoisomers, tautomers, mixtures and addition salts thereof, pharmaceutical compositions containing these compounds and processes for preparing them. The cyclic imino derivatives are useful as inhibitors of cell-cell and cell-matrix interactions, e.g., thrombocyte aggregation.
摘要翻译: 其中A,B,E,X 1,X 2和Y如本文所定义的式B-X2-X1-AYE(I)的环亚胺衍生物,其立体异构体,互变异构体,其混合物和加成盐,含有这些化合物的药物组合物和方法 准备他们 环状亚氨基衍生物可用作细胞 - 细胞和细胞 - 基质相互作用的抑制剂,例如凝血细胞聚集。
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公开(公告)号:US5563268A
公开(公告)日:1996-10-08
申请号:US375084
申请日:1995-01-19
申请人: Guenter Linz , Helmut Pieper , Frank Himmelsbach , Volkhard Austel , Thomas Mueller , Johannes Weisenberger , Elke Seewaldt-Becker
发明人: Guenter Linz , Helmut Pieper , Frank Himmelsbach , Volkhard Austel , Thomas Mueller , Johannes Weisenberger , Elke Seewaldt-Becker
IPC分类号: A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4425 , A61K31/4427 , A61K31/445 , A61K31/495 , A61K31/50 , A61K31/505 , A61P7/02 , A61P29/00 , A61P35/00 , C07D213/75 , C07D213/81 , C07D237/14 , C07D237/20 , C07D237/24 , C07D239/28 , C07D239/34 , C07D239/36 , C07D241/20 , C07D401/06 , C07D401/12 , C07D417/12 , C07F9/40 , C07F9/6509 , C07D403/02
CPC分类号: C07D239/36 , C07D237/14 , C07D237/20 , C07D237/24 , C07D401/06 , C07D401/12 , C07F9/650941
摘要: Heterobiaryl derivatives of the formulaR.sub.1 NH--X.sub.1 --X.sub.2 --X.sub.3 --Y.sub.1 --Y.sub.2 --Y.sub.3 --Y.sub.4 --E (I)whereinR.sub.1, X.sub.1 to X.sub.3 and Y.sub.1 to Y.sub.4 are as defined herein, the tautomers, stereoisomers and mixtures thereof, and the salts, particularly the physiologically acceptable salts, thereof with organic or inorganic acids or bases. The derivatives have valuable pharmacological properties, such as inhibiting cell-cell aggregation and cell-matrix interactions.
摘要翻译: 式R1NH-X1-X2-X3-Y1-Y2-Y3-Y4-E(Ⅰ)的杂芳基衍生物其中R1,X1至X3和Y1至Y4如本文所定义,互变异构体,立体异构体及其混合物,以及 盐,特别是其生理上可接受的盐与有机或无机酸或碱反应。 该衍生物具有有价值的药理学性质,例如抑制细胞 - 细胞聚集和细胞 - 基质相互作用。
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87.Cyclic imino derivatives, pharmaceutical compositions containing these compounds and processes preparing them 失效
标题翻译: 环状亚氨基衍生物,含有这些化合物的药物组合物和制备它们的方法公开(公告)号:US5489693A
公开(公告)日:1996-02-06
申请号:US52877
申请日:1993-04-26
申请人: Guenter Linz , Volkhard Austel , Frank Himmelsbach , Johannes Weisenberger , Thomas Mueller , Helmut Pieper , Elke Seewaldt-Becker
发明人: Guenter Linz , Volkhard Austel , Frank Himmelsbach , Johannes Weisenberger , Thomas Mueller , Helmut Pieper , Elke Seewaldt-Becker
IPC分类号: A61K31/40 , A61K31/4015 , A61K31/44 , A61K31/4427 , A61K31/495 , A61K31/505 , A61K31/535 , A61P7/02 , C07D207/24 , C07D207/26 , C07D207/36 , C07D207/38 , C07D207/40 , C07D207/416 , C07D401/04 , C07D403/04
CPC分类号: C07D207/26 , C07D207/38
摘要: Cyclic imino derivatives of the formula ##STR1## wherein X and R.sub.a to R.sub.g are as defined herein, useful for their inhibitory effects on aggregation, pharmaceutical compositions containing the compounds and processes for preparing them.
摘要翻译: 其中X和R a至R g如本文所定义的式(I)的环亚胺衍生物可用于其对聚集的抑制作用,含有该化合物的药物组合物及其制备方法。
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88.5-membered heterocyclic compounds, processes for preparing them and pharmaceutical compositions containing these compounds 失效
标题翻译: 5元杂环化合物,其制备方法和含有这些化合物的药物组合物公开(公告)号:US5463071A
公开(公告)日:1995-10-31
申请号:US148724
申请日:1993-11-08
申请人: Frank Himmelsbach , Guenter Linz , Volkhard Austel , Helmut Pieper , Thomas Mueller , Johannes Weisenberger , Elke Seewaldt-Becker
发明人: Frank Himmelsbach , Guenter Linz , Volkhard Austel , Helmut Pieper , Thomas Mueller , Johannes Weisenberger , Elke Seewaldt-Becker
IPC分类号: A61K31/41 , A61K31/415 , A61K31/433 , A61P7/02 , A61P43/00 , C07D233/54 , C07D233/64 , C07D233/66 , C07D249/08 , C07D249/12 , C07D257/04 , C07D263/32 , C07D271/10 , C07D277/20 , C07D277/30 , C07D285/12 , C07D307/68 , C07D401/04 , C07D403/04 , C07F9/6506 , C07D257/02 , C07D257/06
CPC分类号: C07D233/64 , C07D249/08 , C07D257/04 , C07D263/32 , C07D271/10 , C07D277/30 , C07D285/12 , C07D307/68 , C07D401/04 , C07D403/04 , C07F9/65067
摘要: Compounds of the formula ##STR1## wherein X.sub.1 to X.sub.5 are as defined herein, the tautomers, the stereoisomers including the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases. The compounds are useful for inhibiting undesirable cell aggregation.
摘要翻译: 其中X1至X5如本文所定义的式(I)化合物,互变异构体,立体异构体包括其混合物及其盐,特别是其与无机或有机酸或碱的生理学上可接受的盐。 该化合物可用于抑制不期望的细胞聚集。
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89.Cyclic urea derivatives, pharmaceutical compositions containing these compounds and methods of using the same 失效
标题翻译: 环状脲衍生物,含有这些化合物的药物组合物及其使用方法公开(公告)号:US5276049A
公开(公告)日:1994-01-04
申请号:US849557
申请日:1992-03-11
申请人: Frank Himmelsbach , Helmut Pieper , Volkhard Austel , Guenter Linz , Thomas Mueller , Johannes Weisenberger , Wolfgang Eisert
发明人: Frank Himmelsbach , Helmut Pieper , Volkhard Austel , Guenter Linz , Thomas Mueller , Johannes Weisenberger , Wolfgang Eisert
IPC分类号: A61K31/41 , A61K31/415 , A61K31/4166 , A61K31/4184 , A61K31/433 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/535 , A61K31/5355 , A61K31/54 , A61K31/541 , A61K31/675 , A61P7/02 , A61P9/00 , A61P9/10 , A61P11/00 , A61P29/00 , A61P35/00 , C07D211/58 , C07D233/30 , C07D233/32 , C07D233/36 , C07D233/70 , C07D233/72 , C07D233/74 , C07D233/76 , C07D235/26 , C07D239/10 , C07D239/36 , C07D249/12 , C07D285/10 , C07D309/12 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/10 , C07D471/04 , C07F9/6506
CPC分类号: C07D285/10 , C07D211/58 , C07D233/32 , C07D233/70 , C07D233/72 , C07D235/26 , C07D239/10 , C07D239/36 , C07D249/12 , C07D309/12 , C07D401/04 , C07D403/04 , C07D471/04 , C07F9/65061
摘要: The invention relates to cyclic urea derivatives of general formula ##STR1## wherein R.sub.a, R.sub.b, X and Y are as defined herein, pharmaceutical compositions containing the derivatives and processes for preparing them.
摘要翻译: 本发明涉及通式为(I)的环脲衍生物,其中Ra,Rb,X和Y如本文所定义,含有衍生物的药物组合物及其制备方法。
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90.N-cyclopropyl-N-piperidinyl-amide derivatives, pharmaceutical compositions and uses thereof 有权
标题翻译: N-环丙基-N-哌啶基 - 酰胺衍生物,药物组合物及其用途公开(公告)号:US08921398B2
公开(公告)日:2014-12-30
申请号:US13489557
申请日:2012-06-06
申请人: Armin Heckel , Frank Himmelsbach , Elke Langkopf , Bernd Nosse , Neil J. Ashweek , Nicole Harriott
发明人: Armin Heckel , Frank Himmelsbach , Elke Langkopf , Bernd Nosse , Neil J. Ashweek , Nicole Harriott
IPC分类号: C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , A61K31/4468 , A61K31/497 , C07D401/12 , C07D401/14
CPC分类号: C07D413/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , Y10S514/866 , Y10S514/909
摘要: The present invention relates to compounds of general formula I, wherein R1, LP, HetAr, Ar, and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
摘要翻译: 本发明涉及通式Ⅰ化合物,其中R1,LP,HetAr,Ar和n如申请中所定义,其具有有价值的药理学性质,特别是与GPR119受体结合并调节其活性。
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