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1. 发明授权

US08415378B2 Isoxazol-3(2H)-one analogs as therapeutic agents 有权
标题翻译：异恶唑-3（2H） - 酮类似物作为治疗剂
公开(公告)号：US08415378B2
公开(公告)日：2013-04-09
申请号：US12755010
申请日：2010-04-06
申请人： Jonas Boström , Leifeng Cheng , Tomas Fex , Michael Karle , Daniel Pettersen , Peter Schell
发明人： Jonas Boström , Leifeng Cheng , Tomas Fex , Michael Karle , Daniel Pettersen , Peter Schell
IPC分类号： A01N43/40 , A01N43/80 , A61K31/445 , A61K31/42 , C07D401/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D421/00 , C07D261/00 , C07D307/02 , C07D315/00 , C07D407/00
CPC分类号： C07D413/04
摘要： or a pharmaceutically suitable salt thereof, wherein, R1 and R2 independently are hydrogen, deuterium, aryl, hetero aryl, C1-C8 alkyl, optionally being substituted with one or more substituents independently being R3, R3 is an aryl, hetero aryl, fluorine(s), a C1-C6 alkyl containing one or more fluorine, a C1-C6 alkyl containing one or more deuterium, a C1-C6 alkyl containing hydroxy, the aryl and heteroaryl optionally being substituted with one or more halogen, a fluorinated alkoxy, a fluorinated alkyl, a sulfonyl, one or more deuterium, a C1-6 alkyl, a C1-6 alkoxy, a nitrile, or R3 is a C1-6 alkyl optionally substituted with one or more of the following groups: COOR4, OCOR4, CONR5R6, NR5COR6, OR4; wherein, R4 is a C1-10 alkyl optionally substituted with one or more fluorine, deuterium, alkoxy, arylcarboxylate, alkyl carboxylate; R5 and R6 are independently selected from hydrogen, alkyl or they may together form a 4-8 membered carbon ring; or R1 and R2 form a 3-10 membered carbon ring optionally comprising O or N and optionally substituted with a C1-10 alkyl or aryl, hetero aryl optionally substituted with R3.
摘要翻译：或其药学上合适的盐，其中R 1和R 2独立地是氢，氘，芳基，杂芳基，任选被一个或多个取代基独立地被R 3取代的C 1 -C 8烷基，R 3是芳基，杂芳基，氟（含有一个或多个氟的C 1 -C 6烷基，含有一个或多个氘的C 1 -C 6烷基，含羟基的C 1 -C 6烷基，任选被一个或多个卤素取代的芳基和杂芳基，氟化烷氧基，氟化烷基，磺酰基，一个或多个氘，C 1-6烷基，C 1-6烷氧基，腈或R 3是任选被一个或多个下列基团取代的C 1-6烷基：COOR 4，OCOR 4， CONR5R6，NR5COR6，OR4; 其中，R4为任选被一个或多个氟，氘，烷氧基，芳基羧酸酯，羧酸烷基酯取代的C 1-10烷基; R 5和R 6独立地选自氢，烷基或它们可以一起形成4-8元碳环; 或R 1和R 2形成任选地包含O或N并任选被C 1-10烷基或芳基取代的3-10元碳环，任选被R 3取代的杂芳基。

2. 发明授权

US07342019B2 5, 6-diaryl-pyrazine-2-amide derivatives as CB1 antagonists 失效
公开(公告)号：US07342019B2
公开(公告)日：2008-03-11
申请号：US10499054
申请日：2002-12-18
申请人： Anna Ingrid Kristina Berggren , Stig Jonas Boström , Stig Thomas Elebring , Peter Greasley , Emma Terricabras , Johan Michael Wilstermann
发明人： Anna Ingrid Kristina Berggren , Stig Jonas Boström , Stig Thomas Elebring , Peter Greasley , Emma Terricabras , Johan Michael Wilstermann
IPC分类号： A61K31/4965 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00
CPC分类号： C07D241/24
摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, prodrugs, solvates and crystalline forms thereof, in which R1 and R2 independently represent: a C1-6alkyl group; an optionally substituted (amino)C1-4alkyl-group; an optionally substituted non-aromatic C3-15carbocyclic group; a (C3-12cycloalkyl)C1-3alkyl-group; a group —(CH2)r(phenyl)s in which r is 0, 1, 2, 3 or 4, s is 1 when r is 0 otherwise s is 1 or 2 and the phenyl groups are optionally independently substituted by Z; naphthyl; anthracenyl; an optionally substituted saturated 5 to 8 membered heterocyclic group containing one nitrogen and optionally one of the following: oxygen, sulphur or an additional nitrogen; 1-adamantylmethyl; a group —(CH2)t Het in which t is 0, 1, 2, 3 or 4, and the alkylene chain is optionally substituted and Het represents an optionally substituted aromatic heterocycle; or R1 represents H and R2 is as defined above; or R1 and R2 together with the nitrogen atom to which they are attached represent a saturated optionally substituted 5 to 8 membered heterocyclic group as defined above; X is CO or SO2; Y is absent or represents NH optionally substitututed by a C1-3alkyl group; R3 and R4 independently represent phenyl, thienyl or pyridyl substituted by Z; Z represents a C1-3alkyl group, a C1-3alkoxy group, hydroxy, halo, trifluoromethyl, trifluoromethylthio, trifluoromethoxy, trifluoromethylsulphonyl, nitro, amino, mono or di C1-3alkylamino, mono or di C1-3alkylamido, C1-3alkylsulphonyl, C1-3alkoxycarbonyl, carboxy, cyano, carbamoyl, mono or di C1-3alkyl carbamoyl, sulphamoyl and acetyl; and R5 is H, a C1-3alkyl group, a C1-3alkoxymethyl group, trifluoromethyl, a hydroxyC1-3alkyl group, C1-3alkoxycarbonyl, carboxy, cyano, carbamoyl, mono or di C1-3alkylcarbamoyl, acetyl, or hydrazinocarbonyl of formula —CONHNRaRb; with the provisos; and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.

3. 发明授权

US07582629B2 Derivatives of isothiazol-3(2H)-one 1,1-dioxides as liver X receptor modulators 失效
标题翻译：异噻唑-3（2H） - 酮1,1-二氧化物的衍生物作为肝X受体调节剂
公开(公告)号：US07582629B2
公开(公告)日：2009-09-01
申请号：US11813481
申请日：2006-01-09
申请人： Jonas Boström , Kay Brickmann , Anders Broo , Robert Judkins , Lanna Li , Pernilla Sandberg , Marianne Swanson , Christer Westerlund , Patrik Holm
发明人： Jonas Boström , Kay Brickmann , Anders Broo , Robert Judkins , Lanna Li , Pernilla Sandberg , Marianne Swanson , Christer Westerlund , Patrik Holm
IPC分类号： A61K31/535 , A61K31/445 , A61K31/425 , C07D415/00 , C07D413/00 , C07D417/00 , C07D275/02
CPC分类号： C07D275/03 , C07D417/12
摘要： The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) α (NR1H3) and/or β (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.
摘要翻译：本发明涉及式（I）的某些新化合物，其用于制备这些化合物，用于调节核激素受体肝X受体（LXR）α（NR1H3）和/或β（NR1H2）和在治疗和/或预防包括心血管疾病如动脉粥样硬化的临床病症; 炎性疾病，阿尔茨海默病，与胰岛素抵抗相关的脂质紊乱（血脂异常），2型糖尿病和代谢综合征的其他表现，其治疗用途的方法和含有它们的药物组合物。

4. 发明申请

US20060235015A1 Pyrrole-2,5-dione derivatives as liver x receptor modulators 失效
标题翻译：吡咯-2,5-二酮衍生物作为肝脏x受体调节剂
公开(公告)号：US20060235015A1
公开(公告)日：2006-10-19
申请号：US10564235
申请日：2004-07-08
申请人： Jonas Boström , Kay Brickmann , Pemilla Sandberg , Marianne Swanson , Christer Westerlund
发明人： Jonas Boström , Kay Brickmann , Pemilla Sandberg , Marianne Swanson , Christer Westerlund
IPC分类号： A61K31/5377 , A61K31/4439 , A61K31/4015 , A61K31/4025 , C07D413/02 , C07D405/02 , C07D403/02
CPC分类号： C07D405/06 , C07D207/456 , C07D401/06 , C07D405/12 , C07D405/14 , C07D413/06
摘要： The present invention relates to certain novel compounds of the Formula I to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) α (NR1H3) and/or β (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.
摘要翻译：本发明涉及一些式I化合物的制备方法，用于调节核激素受体肝X受体（LXR）α（NR1H3）和/或β（NR1H2）以及在治疗和 /或预防包括心血管疾病如动脉粥样硬化的临床病症; 炎性疾病，阿尔茨海默病，与胰岛素抵抗相关的脂质紊乱（血脂异常），2型糖尿病和代谢综合征的其他表现，其治疗用途的方法和含有它们的药物组合物。

5. 发明申请

US20100261755A1 ISOXAZOL-3(2H)-ONE ANALOGS AS THERAPEUTIC AGENTS 有权
标题翻译： ISOXAZOL-3（2H） - 作为治疗剂的模拟物
公开(公告)号：US20100261755A1
公开(公告)日：2010-10-14
申请号：US12755010
申请日：2010-04-06
申请人： Jonas BOSTRÖM , Leifeng Cheng , Tomas Fex , Michael Karle , Daniel Pettersen , Peter Schell
发明人： Jonas BOSTRÖM , Leifeng Cheng , Tomas Fex , Michael Karle , Daniel Pettersen , Peter Schell
IPC分类号： A61K31/454 , C07D401/04 , A61P1/16 , A61P9/10 , A61P7/04
CPC分类号： C07D413/04
摘要： or a pharmaceutically suitable salt thereof, wherein, R1 and R2 independently are hydrogen, deuterium, aryl, hetero aryl, C1-C8 alkyl, optionally being substituted with one or more substituents independently being R3, R3 is an aryl, hetero aryl, fluorine(s), a C1-C6 alkyl containing one or more fluorine, a C1-C6 alkyl containing one or more deuterium, a C1-C6 alkyl containing hydroxy, the aryl and heteroaryl optionally being substituted with one or more halogen, a fluorinated alkoxy, a fluorinated alkyl, a sulfonyl, one or more deuterium, a C1-6 alkyl, a C1-6 alkoxy, a nitrile, or R3 is a C1-6 alkyl optionally substituted with one or more of the following groups: COOR4, OCOR4, CONR5R6, NR5COR6, OR4; wherein, R4 is a C1-10 alkyl optionally substituted with one or more fluorine, deuterium, alkoxy, arylcarboxylate, alkyl carboxylate; R5 and R6 are independently selected from hydrogen, alkyl or they may together form a 4-8 membered carbon ring; or R1 and R2 form a 3-10 membered carbon ring optionally comprising O or N and optionally substituted with a C1-10 alkyl or aryl, hetero aryl optionally substituted with R3.
摘要翻译：或其药学上合适的盐，其中R 1和R 2独立地是氢，氘，芳基，杂芳基，任选被一个或多个取代基独立地被R 3取代的C 1 -C 8烷基，R 3是芳基，杂芳基，氟（含有一个或多个氟的C 1 -C 6烷基，含有一个或多个氘的C 1 -C 6烷基，含羟基的C 1 -C 6烷基，任选被一个或多个卤素取代的芳基和杂芳基，氟化烷氧基，氟化烷基，磺酰基，一个或多个氘，C 1-6烷基，C 1-6烷氧基，腈或R 3是任选被一个或多个下列基团取代的C 1-6烷基：COOR 4，OCOR 4， CONR5R6，NR5COR6，OR4; 其中，R4为任选被一个或多个氟，氘，烷氧基，芳基羧酸酯，羧酸烷基酯取代的C 1-10烷基; R 5和R 6独立地选自氢，烷基或它们可以一起形成4-8元碳环; 或R 1和R 2形成任选地包含O或N并任选被C 1-10烷基或芳基取代的3-10元碳环，任选被R 3取代的杂芳基。

6. 发明授权

US07432288B2 Pyrrole-2,5-dione derivatives as Liver X receptor modulators 失效
标题翻译：吡咯-2,5-二酮衍生物作为肝X受体调节剂
公开(公告)号：US07432288B2
公开(公告)日：2008-10-07
申请号：US10564235
申请日：2004-07-08
申请人： Jonas Boström , Kay Brickmann , Patrik Holm , Pernilla Sandberg , Marianne Swanson , Christer Westerlund
发明人： Jonas Boström , Kay Brickmann , Patrik Holm , Pernilla Sandberg , Marianne Swanson , Christer Westerlund
IPC分类号： A61K31/4439 , C07D401/04
CPC分类号： C07D405/06 , C07D207/456 , C07D401/06 , C07D405/12 , C07D405/14 , C07D413/06
摘要： The present invention relates to certain novel compounds of the Formula I to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR)α(NR1H3) and/or β(NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.
摘要翻译：本发明涉及一些式I化合物的制备方法，用于调节核激素受体肝X受体（LXR）α（NR1H3）和/或β（NR1H2）以及在治疗和 /或预防包括心血管疾病如动脉粥样硬化的临床病症; 炎性疾病，阿尔茨海默病，与胰岛素抵抗相关的脂质紊乱（血脂异常），2型糖尿病和代谢综合征的其他表现，其治疗用途的方法和含有它们的药物组合物。

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