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1. 发明授权

US07960380B2 Non-anilinic 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1,1-二氧化物的非苯胺衍生物作为肝X受体调节剂
公开(公告)号：US07960380B2
公开(公告)日：2011-06-14
申请号：US12725669
申请日：2010-03-17
申请人： Anders Broo , Robert Judkins , Lanna Li , Eva-Lotte Lindstedt-Alstermark , Pernilla Sandberg , Marianne Swanson , Lars Weidolf , Kay Brickmann , Patrik Holm
发明人： Anders Broo , Robert Judkins , Lanna Li , Eva-Lotte Lindstedt-Alstermark , Pernilla Sandberg , Marianne Swanson , Lars Weidolf , Kay Brickmann , Patrik Holm
IPC分类号： A61K31/5355 , A61K31/501 , A61K31/4523 , A61K31/4427 , A61K31/427 , A61K31/4255 , C07D275/02 , C07D233/54 , C07D413/02 , C07D401/02 , C07D239/02 , C07D211/00 , C07D417/02
CPC分类号： C07D275/03 , C07D417/12 , C07D417/14
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）的某些新型化合物，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bgr; （NR1H2）和治疗和/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。

2. 发明申请

US20100227847A1 Non-Anilinic Derivatives Of Isothiazol-3(2H)-one 1,1-Dioxides As Liver X Receptor Modulators 失效
标题翻译：异噻唑啉-3（2H） - 酮1,1-二氧化物的非苯胺衍生物作为肝X受体调节剂
公开(公告)号：US20100227847A1
公开(公告)日：2010-09-09
申请号：US12725669
申请日：2010-03-17
申请人： Anders Broo , Robert Judkins , Lanna Li , Eva-Lotte Lindstedt-Alstermark , Pernilla Sandberg , Marianne Swanson , Lars Weidolf , Kay Brickmann , Patrik Holm
发明人： Anders Broo , Robert Judkins , Lanna Li , Eva-Lotte Lindstedt-Alstermark , Pernilla Sandberg , Marianne Swanson , Lars Weidolf , Kay Brickmann , Patrik Holm
IPC分类号： A61K31/427 , A61P3/10 , A61P3/06 , A61P9/10 , A61P25/28 , A61K31/425 , A61K31/4439 , A61K31/4545 , A61K31/454 , A61K31/5377
CPC分类号： C07D275/03 , C07D417/12 , C07D417/14
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）的某些新型化合物，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bgr; （NR1H2）和治疗和/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。

3. 发明授权

US07723333B2 Non-anilinic 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1,1-二氧化物的非苯胺衍生物作为肝X受体调节剂
公开(公告)号：US07723333B2
公开(公告)日：2010-05-25
申请号：US11813470
申请日：2006-01-09
申请人： Anders Broo , Robert Judkins , Lanna Li , Eva-Lotte Lindstedt-Alstermark , Pernilla Sandberg , Marianne Swanson , Lars Weidolf , Kay Brickmann , Patrik Holm
发明人： Anders Broo , Robert Judkins , Lanna Li , Eva-Lotte Lindstedt-Alstermark , Pernilla Sandberg , Marianne Swanson , Lars Weidolf , Kay Brickmann , Patrik Holm
IPC分类号： A61K31/5355 , A61K31/501 , A61K31/4523 , A61K31/4427 , A61K31/427 , A61K31/4155 , C07D275/02 , C07D233/54 , C07D413/02 , C07D401/02 , C07D239/02 , C07D211/00 , C07D417/02
CPC分类号： C07D275/03 , C07D417/12 , C07D417/14
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）的某些新型化合物，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bgr; （NR1H2）和治疗和/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

US20090005353A1 Non-Anilinic Derivatives of Isothiazol-3(2H)-one 1,1-Dioxides as Liver X Receptor Modulators 失效
标题翻译：异噻唑啉-3（2H） - 酮1,1-二氧化物的非苯胺衍生物作为肝X受体调节剂
公开(公告)号：US20090005353A1
公开(公告)日：2009-01-01
申请号：US11813470
申请日：2006-01-09
申请人： Anders Broo , Robert Judkins , Lanna Li , Eva-Lotte Lindstedt-Alstermark , Pernilla Sandberg , Marianne Swanson , Lars Weidolf , Kay Brickmann , Patrik Holm
发明人： Anders Broo , Robert Judkins , Lanna Li , Eva-Lotte Lindstedt-Alstermark , Pernilla Sandberg , Marianne Swanson , Lars Weidolf , Kay Brickmann , Patrik Holm
IPC分类号： A61K31/397 , C07D275/02 , A61K31/425 , C07D417/02 , A61K31/4439 , C07D211/06 , A61K31/4545 , A61K31/501 , A61P29/00 , A61P25/00 , A61P9/00 , C07D403/14 , A61K31/454 , C07D401/14 , A61K31/506 , C07D295/00 , A61K31/5377
CPC分类号： C07D275/03 , C07D417/12 , C07D417/14
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。

5. 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。

6. 发明申请

US20100016321A1 DERIVATIVES OF ISOTHIAZOL-3(2H)-ONE 1,1-DIOXIDES AS LIVER X RECEPTOR MODULATOR 审中-公开
标题翻译：异硫氰酸-3（2H） - 酮-1,1-二氧化物作为肝脏X受体调节剂的衍生物
公开(公告)号：US20100016321A1
公开(公告)日：2010-01-21
申请号：US12507924
申请日：2009-07-23
申请人： Jonas Bostrom , Kay Brickmann , Anders Broo , Robert Judkins , Lanna Li , Pernilla Sandberg , Marianne Swanson , Christer Westerlund , Patrik Holm
发明人： Jonas Bostrom , Kay Brickmann , Anders Broo , Robert Judkins , Lanna Li , Pernilla Sandberg , Marianne Swanson , Christer Westerlund , Patrik Holm
IPC分类号： A61K31/5377 , A61P3/00 , A61P25/00
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 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，用于制备这些化合物的方法，用于调节核激素受体肝X受体（LXR）α（NR1H3）和/或β（NR1H2）和治疗和/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。

7. 发明申请

US20080255122A1 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） - 一种1,1-二氧化物作为肝X受体调节剂的衍生物
公开(公告)号：US20080255122A1
公开(公告)日：2008-10-16
申请号：US11813481
申请日：2006-01-09
申请人： Jonas Bostrom , Kay Brickmann , Anders Broo , Robert Judkins , Lanna Li , Pernilla Sandberg , Marianne Swanson , Christer Westerlund , Patrik Holm
发明人： Jonas Bostrom , Kay Brickmann , Anders Broo , Robert Judkins , Lanna Li , Pernilla Sandberg , Marianne Swanson , Christer Westerlund , Patrik Holm
IPC分类号： A61K31/5355 , C07D275/03 , A61K31/425 , A61P25/00 , C07D401/02 , A61K31/497 , A61K31/4725 , C07D413/14 , A61K31/454 , C07D417/02
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。

8. 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。

9. 发明申请

US20060247439A1 Mchir antagonists 审中-公开
公开(公告)号：US20060247439A1
公开(公告)日：2006-11-02
申请号：US10520372
申请日：2003-07-04
申请人： Asim Ray , Emma Evertsson , Anna Stina Linusson Jonsson , Pernilla Sandberg , Tord Ingiiardt , Anette Svensson , Kay Brickmann
发明人： Asim Ray , Emma Evertsson , Anna Stina Linusson Jonsson , Pernilla Sandberg , Tord Ingiiardt , Anette Svensson , Kay Brickmann
IPC分类号： A61K31/4709 , A61K31/4706 , C07D409/02 , C07D405/02 , C07D401/02
CPC分类号： C07D215/38 , C07D401/12 , C07D405/12 , C07D407/12 , C07D409/12
摘要： The present invention provides compounds of formula (I), wherein R1 represents a C1-4 alkoxy group optionally substituted by one or more fluoro or a C1-4alkyl group optionally substituted by one or more fluoro; n represents 0 or 1; R2 represents a C1-4alkyl group optionally substituted by one or more fluoro or a C1-4alkoxy group optionally substituted by one or more fluoro; m represents 0 or 1; R3 represents H or a C1-4alkyl group; L1 represents an alkylene chain (CH2)r in which r represents 2 or 3 or L1 represents a cyclohexyl group wherein the two nitrogens bearing R3 and R4, respectively, are linked to the cyclohexyl group either via the 1,3 or the 1,4 positions of the cyclohexyl group or L1 represents a cyclopentyl group wherein the two nitrogens bearing R3 and R4, respectively, are linked to the cyclopentyl group via the 1,3 position of the cyclopentyl group and additionally when R5 represents 9,10-methanoanthracen-9(10H)-yl the group -L1-N(R4)— together represents a piperidyl ring which is linked to L2 through the piperidinyl nitrogen and to N—R3 via the 4 position of the piperidyl ring with the proviso that when R5 represents 9,10-methanoanthracen-9(10H)-yl then r is only 2; R4 represents H or a C1-4alkyl group optionally substituted by one or more of the following: an aryl group or a heteroaryl group; L2 represents a bond or an alkylene chain (CH2), in which s represents 1, 2 or 3 wherein the alkylene chain is optionally substituted by one or more of the following: a C1-4alkyl group, phenyl or heteroaryl; R5 represents aryl, a heterocyclic group or a CH3-8cycloalkyl group which is optionally fused to a phenyl or to a heteroaryl group; as well as optical isomers and racemates thereof as well as pharmaceutically acceptable salts, thereof; with provisos, processes for preparing such compounds, their use in the treatment of obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and related conditions, and neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea and Alzheimer's disease and pain related disorders and to pharmaceutical compositions containing them.

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