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61. 发明授权

US06653305B2 Bicyclic heterocycles, pharmaceutical compositions containing them, their use, and processes for preparing them 有权
标题翻译：双环杂环，含有它们的药物组合物，它们的用途和制备它们的方法
公开(公告)号：US06653305B2
公开(公告)日：2003-11-25
申请号：US09929931
申请日：2001-08-15
申请人： Frank Himmelsbach , Elke Langkopf , Birgit Jung , Stefan Blech , Flavio Solca
发明人： Frank Himmelsbach , Elke Langkopf , Birgit Jung , Stefan Blech , Flavio Solca
IPC分类号： A61K31535
CPC分类号： C07D405/12 , A61K31/505 , C07D239/94 , C07D413/12 , C07D413/14
摘要： A compound of formula (I) wherein: Ra is a benzyl or 1-phenylethyl group or a phenyl group substituted by the groups R1 and R2, wherein: R1 is a hydrogen, fluorine, chlorine, or bromine atom, or a methyl, trifluoromethyl, cyano, or ethynyl group, and R2 is a hydrogen or fluorine atom; Rb is an R3O—CO—CH2—N—CH2—CH2—OH group optionally substituted at the methylene groups by 1 or 2 methyl or ethyl groups, wherein R3 is a hydrogen atom or a C1-4-alkyl group, a 2-oxomorpholin-4-yl group optionally substituted by 1 or 2 methyl or ethyl groups, or a N-[(1,3-dioxolan-2-yl)methyl]methylamino group; Rc is a hydrogen atom, or a methoxy, ethoxy, 2-methoxyethoxy, 2-ethoxyethoxy, cyclobutyloxy, cyclopentyloxy, cyclohexyloxy, cyclopropylmethoxy, cyclobutylmethoxy, cyclopentylmethoxy, cyclohexylmethoxy, tetrahydrofuran-3-yloxy, tetrahydropyran-3-yloxy, tetrahydropyran-4-yloxy, tetrahydrofuranylmethoxy, or tetrahydropyranylmethoxy group; and n is 1, 2, or 3, the tautomers, stereoisomers, and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.
摘要翻译：式（I）的化合物，其中：R a是苄基或1-苯基乙基或被基团R 1和R 2取代的苯基，其中：R 1是氢，氟，氯或溴原子，或甲基，三氟甲基，氰基或乙炔基，R 2是氢或氟原子; R b是任选在亚甲基被1或2个甲基或乙基取代的R3O-CO-CH2-N-CH2-CH2-OH基团，其中R3是氢原子或C1-4烷基，任选被1或2个甲基或乙基取代的2-氧代吗啉-4-基，或N - [（1,3-二氧戊环-2-基）甲基] 甲基氨基; R c是氢原子，或甲氧基，乙氧基，2-甲氧基乙氧基，2-乙氧基乙氧基，环丁氧基，环戊氧基，环己氧基，环丙基甲氧基，环丁基甲氧基，环戊基甲氧基，环己基甲氧基，四氢呋喃-3-基氧基，四氢吡喃-3-基氧基，四氢吡喃 -4-基氧基，四氢呋喃基甲氧基或四氢吡喃基甲氧基; andn为1,2或3，互变异构体，立体异构体及其盐，特别是其与具有有价值药理学性质的无机或有机酸或碱的生理上可接受的盐，它们在治疗疾病尤其是肿瘤疾病和疾病中的用途的肺和气道，以及其制备。

62. 发明授权

US06627634B2 Bicyclic heterocycles, pharmaceutical compositions containing them, their use, and processes for preparing them 有权
标题翻译：双环杂环，含有它们的药物组合物，它们的用途和制备它们的方法
公开(公告)号：US06627634B2
公开(公告)日：2003-09-30
申请号：US09816003
申请日：2001-03-23
申请人： Frank Himmelsbach , Elke Langkopf , Birgit Jung , Stefan Blech , Flavio Solca
发明人： Frank Himmelsbach , Elke Langkopf , Birgit Jung , Stefan Blech , Flavio Solca
IPC分类号： A61K31517
CPC分类号： C07D401/14 , C07D405/12 , C07D413/14 , C07D491/04
摘要： Bicyclic heterocycles of general formula wherein: Ra to Rd, A to C and X are as defined herein, the tautomers, the stereoisomers and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, diseases of the lungs and respiratory tract, and the preparation thereof.
摘要翻译：一般形式的双环杂环：R a至R d，A至C和X如本文所定义，具有有价值的药理学性质的互变异构体，立体异构体及其盐，特别是其与无机或有机酸或碱的生理上可接受的盐，特别是对由酪氨酸激酶介导的信号转导的抑制作用，其用于治疗疾病，特别是肿瘤疾病，肺和呼吸道疾病的用途及其制备。

63. 发明授权

US09492436B2 Azabenzimidazole derivatives 有权
标题翻译：偶氮苯并咪唑衍生物
公开(公告)号：US09492436B2
公开(公告)日：2016-11-15
申请号：US14331359
申请日：2014-07-15
申请人： Frank Himmelsbach , Elke Langkopf , Holger Wagner , Nobert Redemann
发明人： Frank Himmelsbach , Elke Langkopf , Holger Wagner , Nobert Redemann
IPC分类号： C07D471/02 , A61K31/437 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/541 , A61K45/06 , C07D493/04 , C07D519/00
CPC分类号： A61K31/437 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/541 , A61K45/06 , C07D493/04 , C07D519/00
摘要： The present invention relates to compounds of general formula I, wherein the group R1, R2, X and Y are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the AMP-activated protein kinase (AMPK) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
摘要翻译：本发明涉及通式I的化合物，其中R1，R2，X和Y基团如权利要求1中所定义，其具有有价值的药理学性质，特别是结合AMP活化蛋白激酶（AMPK）并调节其活动。该化合物适用于治疗和预防可受该受体影响的疾病，如代谢疾病，特别是2型糖尿病。

64. 发明授权

US06972288B1 4-amino-quinazoline and quinoline derivatives having an inhibitory effect on signal transduction mediated by tyrosine kinases 有权
标题翻译：对酪氨酸激酶介导的信号转导具有抑制作用的4-氨基 - 喹唑啉和喹啉衍生物
公开(公告)号：US06972288B1
公开(公告)日：2005-12-06
申请号：US09914323
申请日：2000-02-24
申请人： Frank Himmelsbach , Elke Langkopf , Birgit Jung , Thomas Metz , Flavio Solca , Stefan Blech
发明人： Frank Himmelsbach , Elke Langkopf , Birgit Jung , Thomas Metz , Flavio Solca , Stefan Blech
IPC分类号： A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/496 , A61K31/517 , A61P35/00 , C07D215/42 , C07D215/54 , C07D239/94 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D413/12
CPC分类号： C07D401/12 , A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/496 , A61K31/517 , C07D215/54 , C07D239/94 , C07D403/12 , C07D405/12 , C07D413/12
摘要： The present invention relates to bicyclic heterocycles of general formula wherein Ra to Rd, A to G and X are defined as in claim 1, the tautomers, the steroisomers and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, particularly an inhibiting effect on signal transduction mediated by tyrosine kinases, their use for treating diseases, particularly tumoral diseases, diseases of the lungs and respiratory tract, and the preparation thereof.
摘要翻译：本发明涉及通式的双环杂环，其中R a至R d，A至G和X如权利要求1所定义，互变异构体，立体异构体和其盐，特别是其具有有价值的药理学性质的无机或有机酸或碱的生理上可接受的盐，特别是对由酪氨酸激酶介导的信号转导的抑制作用，其用于治疗疾病，特别是肿瘤疾病，肺和呼吸道疾病道及其制备。

65. 发明授权

US06617329B2 Aminoquinazolines and their use as medicaments 有权
标题翻译：氨基喹唑啉及其作为药物的用途
公开(公告)号：US06617329B2
公开(公告)日：2003-09-09
申请号：US09938314
申请日：2001-08-23
申请人： Frank Himmelsbach , Elke Langkopf , Birgit Jung , Stefan Blech , Flavio Solca
发明人： Frank Himmelsbach , Elke Langkopf , Birgit Jung , Stefan Blech , Flavio Solca
IPC分类号： C07D23994
CPC分类号： C07D405/12 , A61K31/505 , A61K31/517 , C07D405/14 , C07D413/12 , C07D413/14
摘要： Compounds of the formula having an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and air-ways, and the preparation thereof.
摘要翻译：该化合物对由酪氨酸激酶介导的信号转导具有抑制作用，其用于治疗疾病，特别是肿瘤疾病以及肺和空气疾病以及其制备。

66. 发明申请

US20100130557A1 SUBSTITUTED ARYLSULPHONYLGLYCINES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS 有权
标题翻译：取代的氨基磺酰胺，其制备方法及其作为药物组合物的用途
公开(公告)号：US20100130557A1
公开(公告)日：2010-05-27
申请号：US12530507
申请日：2008-03-14
申请人： Holger Wagner , Elke Langkopf , Matthias Eckhardt , Ruediger Streicher , Corinna Schoelch , Annette Schuler-Metz , Alexander Pautsch
发明人： Holger Wagner , Elke Langkopf , Matthias Eckhardt , Ruediger Streicher , Corinna Schoelch , Annette Schuler-Metz , Alexander Pautsch
IPC分类号： A61K31/404 , A61K31/4439 , A61K31/403 , C07D401/12 , C07D209/82 , C07D209/04 , A61P3/10
CPC分类号： C07D209/08 , C07D209/18 , C07D209/42 , C07D209/88 , C07D231/56 , C07D235/06 , C07D235/26 , C07D277/64 , C07D333/68 , C07D333/70 , C07D401/12 , C07D403/06 , C07D403/12 , C07F7/0812
摘要： The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
摘要翻译：本发明涉及通式（I）的取代芳基磺酰基甘氨酸，其中R，X，Y和Z如权利要求1所定义，其互变异构体，对映异构体，非对映体，其混合物及其盐具有有价值的药理学性质，特别是抑制的糖原磷酸化酶a与糖原相关蛋白磷酸酶1（PP1）的GL亚基的相互作用，以及它们作为药物组合物的用途。

67. 发明申请

US20100093703A1 SUBSTITUTED ARYLSULPHONYLGLYCINES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译：取代的氨基磺酰胺，其制备方法及其作为药物组合物的用途
公开(公告)号：US20100093703A1
公开(公告)日：2010-04-15
申请号：US12527249
申请日：2008-02-15
申请人： Holger Wagner , Elke Langkopf , Ruediger Streicher , Matthias Eckhardt , Annette Schuler-Metz , Alexander Pautsch , Corinna Schoelch
发明人： Holger Wagner , Elke Langkopf , Ruediger Streicher , Matthias Eckhardt , Annette Schuler-Metz , Alexander Pautsch , Corinna Schoelch
IPC分类号： A61K31/404 , C07D403/04 , C07D401/04 , C07D403/14 , C07D413/14 , C07D417/14 , A61K31/506 , A61K31/4178 , A61K31/4439 , A61K31/496 , A61K31/501 , A61K31/53 , A61K31/5377 , A61K31/541 , A61K31/551 , A61P3/10
CPC分类号： C07D209/04 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14
摘要： The present invention relates to substituted arylsulphonylglycines of general formula wherein R, R4, X, Y, Z and m are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
摘要翻译：本发明涉及通式其中R，R 4，X，Y，Z和m如权利要求1中定义的取代芳基磺酰基甘氨酸，其互变异构体，对映异构体，非对映异构体，其混合物及其盐，其具有有价值的药理学性质，抑制糖原磷酸化酶a与糖原相关蛋白磷酸酶1（PP1）的GL亚基的相互作用，以及它们作为药物组合物的用途。

68. 发明授权

US08927726B2 N-cyclopropyl-N-piperidinyl-amide derivatives, pharmaceutical compositions containing them and uses thereof 有权
标题翻译： N-环丙基-N-哌啶基 - 酰胺衍生物，含有它们的药物组合物及其用途
公开(公告)号：US08927726B2
公开(公告)日：2015-01-06
申请号：US13947200
申请日：2013-07-22
申请人： Frank Himmelsbach , Elke Langkopf , Neil J. Ashweek , Nicole Harriott
发明人： Frank Himmelsbach , Elke Langkopf , Neil J. Ashweek , Nicole Harriott
IPC分类号： A61K31/445 , C07D401/00 , C07D413/12 , A61K31/454 , A61K31/4545 , A61K31/497 , A61K31/506 , A61K45/06 , C07D401/12 , C07D401/14
CPC分类号： C07D413/12 , A61K31/454 , A61K31/4545 , A61K31/497 , A61K31/506 , A61K45/06 , C07D401/12 , C07D401/14
摘要： The present invention relates to compounds of general formula I, wherein R1, LP, (Het)Ar1, (Het)Ar2 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的化合物，其中R1，LP，（Het）Ar1，（Het）Ar2和n如本申请中所定义，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动。

69. 发明授权

US08586608B2 Quinazoline derivatives and pharmaceutical compositions containing them 有权
标题翻译：喹唑啉衍生物和含有它们的药物组合物
公开(公告)号：US08586608B2
公开(公告)日：2013-11-19
申请号：US12563340
申请日：2009-09-21
申请人： Frank Himmelsbach , Elke Langkopf , Stefan Blech , Birgit Jung , Anke Baum , Flavio Solca
发明人： Frank Himmelsbach , Elke Langkopf , Stefan Blech , Birgit Jung , Anke Baum , Flavio Solca
IPC分类号： A61K31/47 , A01N43/42
CPC分类号： C07D405/12 , C07D239/94
摘要： A compound of general formula I wherein: Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetra-hydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetra-hydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and Rc is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.
摘要翻译：通式I的化合物，其中：R a是苄基，1-苯乙基或3-氯-4-氟苯基; Rb是二甲基氨基，N-甲基-N-乙基氨基，二乙基氨基，N-甲基-N-异丙基氨基，N-甲基-N-环丙基氨基，N-甲基-N-（2-甲氧基乙基）氨基，N-乙基-N- （2-甲氧基乙基）氨基，双（2-甲氧基乙基）氨基，吗啉代，N-甲基-N-（四氢呋喃-3-基）氨基，N-甲基-N-（四氢呋喃-2-基甲基）氨基，N - 甲基-N-（四氢呋喃-3-基甲基）氨基，N-甲基-N-（四氢吡喃-4-基）氨基或N-甲基-N-（四氢吡喃-4-基甲基）氨基; Rc为环丙基甲氧基，环丁氧基，环戊氧基，四氢呋喃-3-基氧基，四氢呋喃-2-基甲氧基，四氢呋喃-3-基甲氧基，四氢吡喃-4-基氧基或四氢吡喃-4-基甲氧基，或互变异构体，立体异构体或盐特别是其具有有价值的药理学特性的无机或有机酸或碱的生理上可接受的盐，特别是对由酪氨酸激酶介导的信号转导的抑制作用，它们在治疗疾病尤其是肿瘤疾病和肺疾病中的用途和气道及其制备。

70. 发明申请

US20060100223A1 Quinazoline derivatives and pharmaceutical compositions containing them 审中-公开
公开(公告)号：US20060100223A1
公开(公告)日：2006-05-11
申请号：US11313304
申请日：2005-12-21
申请人： Frank Himmelsbach , Elke Langkopf , Stefan Blech , Birgit Jung , Anke Baum , Flavio Solca
发明人： Frank Himmelsbach , Elke Langkopf , Stefan Blech , Birgit Jung , Anke Baum , Flavio Solca
IPC分类号： A61K31/517 , C07D405/02 , C07D239/84
CPC分类号： C07D405/12 , C07D239/94
摘要： A compound of general formula I wherein: Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetrahydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetrahydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and Rc is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.

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