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公开(公告)号：US09051265B2
公开(公告)日：2015-06-09
申请号：US13490342
申请日：2012-06-06
申请人： Theodore Mark Kamenecka , Patrick R. Griffin , Marcel Koenig , Alice Asteian , Anne-Laure Blayo , Yuanjun He , Youseung Shin
发明人： Theodore Mark Kamenecka , Patrick R. Griffin , Marcel Koenig , Alice Asteian , Anne-Laure Blayo , Yuanjun He , Youseung Shin
IPC分类号： C07D209/08 , C07D405/12 , C07D409/12 , C07D401/06 , C07D403/12 , C07D413/12 , A61K31/4439 , A61K31/497 , A61K31/41 , A61K31/4245 , C07D209/42 , C07D209/04 , C07D413/10 , C07D419/12 , A61K31/404
CPC分类号： C07D209/42 , A61K31/404 , C07D209/04 , C07D401/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/10 , C07D419/12
摘要： The invention provides molecular entities that bind with high affinity to PPARG (PPARγ), and inhibit kinase-mediated (e.g., cdk5-mediated) phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. Side effects such as significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, can be avoided in the mammal receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.
摘要翻译： 本发明提供了以高亲和力结合PPARG（PPARγ）并抑制PPARG的激酶介导的（例如cdk5介导的）磷酸化的分子实体，但不对PPARG发挥激动作用。 本发明的化合物可用于治疗其中PPARG起作用的患者中的病症，例如糖尿病，胰岛素抵抗，葡萄糖耐量降低，前期糖尿病，高血糖症，高胰岛素血症，肥胖症或炎症。 在接受化合物的哺乳动物中可以避免副作用，例如显着的体重增加，水肿，骨生长或形成的损害，或心脏肥大，或其任何组合。 还提供了制备化合物的方法，用于评价本发明的化合物作为非激动性PPARG结合化合物的生物测定方法和药物组合物。
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公开(公告)号：US20120309757A1
公开(公告)日：2012-12-06
申请号：US13490324
申请日：2012-06-06
申请人： Theodore Mark Kamenecka , Patrick R. Griffin , Marcel Koenig , Alice Asteian , Anne-Laure Blayo , Yuanjun He , Youseung Shin
发明人： Theodore Mark Kamenecka , Patrick R. Griffin , Marcel Koenig , Alice Asteian , Anne-Laure Blayo , Yuanjun He , Youseung Shin
IPC分类号： A61K31/404 , C07D403/10 , C07D401/10 , A61K31/4439 , C07D405/12 , C07D413/12 , A61K31/5377 , C07D401/12 , A61K31/4709 , A61K31/454 , C07D413/10 , A61K31/4245 , A61P3/10 , A61P3/04 , A61P29/00 , C07D209/12
CPC分类号： C07D209/42 , C07D401/10 , C07D401/12 , C07D403/10 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/12 , C07D471/04 , C07D493/04
摘要： The invention provides molecular entities that bind with high affinity to PPARG (PPARγ), inhibit kinase-mediated, e.g., cdk5-mediated, phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. In methods of treatment of these conditions using a compound of the invention, the compound can avoid producing side effects of significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, in the patient receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.
摘要翻译： 本发明提供了以高亲和力结合PPARG（PPARγ），抑制激酶介导的，例如cdk5介导的PPARG磷酸化，但不对PPARG发挥激动作用的分子实体。 本发明的化合物可用于治疗其中PPARG起作用的患者中的病症，例如糖尿病，胰岛素抵抗，葡萄糖耐量降低，前期糖尿病，高血糖症，高胰岛素血症，肥胖症或炎症。 在使用本发明化合物治疗这些病症的方法中，化合物可以避免在接受化合物的患者中产生显着的体重增加，水肿，骨生长或形成的损害或心脏肥大或其任何组合的副作用 。 还提供了制备化合物的方法，用于评价本发明的化合物作为非激动性PPARG结合化合物的生物测定方法和药物组合物。
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公开(公告)号：US08957093B2
公开(公告)日：2015-02-17
申请号：US13490324
申请日：2012-06-06
申请人： Theodore Mark Kamenecka , Patrick R. Griffin , Marcel Koenig , Alice Asteian , Anne-Laure Blayo , Yuanjun He , Youseung Shin
发明人： Theodore Mark Kamenecka , Patrick R. Griffin , Marcel Koenig , Alice Asteian , Anne-Laure Blayo , Yuanjun He , Youseung Shin
IPC分类号： A61K31/404 , C07D209/42 , C07D401/10 , C07D401/12 , C07D403/10 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/12 , C07D471/04 , C07D493/04
CPC分类号： C07D209/42 , C07D401/10 , C07D401/12 , C07D403/10 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/12 , C07D471/04 , C07D493/04
摘要： The invention provides molecular entities that bind with high affinity to PPARG (PPARγ), inhibit kinase-mediated, e.g., cdk5-mediated, phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. In methods of treatment of these conditions using a compound of the invention, the compound can avoid producing side effects of significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, in the patient receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.
摘要翻译： 本发明提供了以高亲和力结合PPARG（PPARγ），抑制激酶介导的，例如cdk5介导的PPARG磷酸化，但不对PPARG发挥激动作用的分子实体。 本发明的化合物可用于治疗其中PPARG起作用的患者中的病症，例如糖尿病，胰岛素抵抗，葡萄糖耐量降低，前期糖尿病，高血糖症，高胰岛素血症，肥胖症或炎症。 在使用本发明化合物治疗这些病症的方法中，化合物可以避免在接受化合物的患者中产生显着的体重增加，水肿，骨生长或形成的损害或心脏肥大或其任何组合的副作用 。 还提供了制备化合物的方法，用于评价本发明的化合物作为非激动性PPARG结合化合物的生物测定方法和药物组合物。
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公开(公告)号：US20120309769A1
公开(公告)日：2012-12-06
申请号：US13490342
申请日：2012-06-06
申请人： Theodore Mark Kamenecka , Patrick R. Griffin , Marcel Koenig , Alice Asteian , Anne-Laure Blayo , Yuanjun He , Youseung Shin
发明人： Theodore Mark Kamenecka , Patrick R. Griffin , Marcel Koenig , Alice Asteian , Anne-Laure Blayo , Yuanjun He , Youseung Shin
IPC分类号： C07D209/08 , C07D405/12 , C07D409/12 , C07D401/06 , A61K31/4439 , C07D403/12 , A61K31/497 , A61K31/41 , C07D413/12 , A61K31/4245 , A61P3/10 , A61P3/08 , A61P3/04 , A61P29/00 , A61K31/404
CPC分类号： C07D209/42 , A61K31/404 , C07D209/04 , C07D401/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/10 , C07D419/12
摘要： The invention provides molecular entities that bind with high affinity to PPARG (PPARγ), and inhibit kinase-mediated (e.g., cdk5-mediated) phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. Side effects such as significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, can be avoided in the mammal receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.
摘要翻译： 本发明提供了以高亲和力结合PPARG（PPARγ）并抑制PPARG的激酶介导的（例如cdk5介导的）磷酸化的分子实体，但不对PPARG发挥激动作用。 本发明的化合物可用于治疗其中PPARG起作用的患者中的病症，例如糖尿病，胰岛素抵抗，葡萄糖耐量降低，前期糖尿病，高血糖症，高胰岛素血症，肥胖症或炎症。 在接受化合物的哺乳动物中可以避免副作用，例如显着的体重增加，水肿，骨生长或形成的损害，或心脏肥大，或其任何组合。 还提供了制备化合物的方法，用于评价本发明的化合物作为非激动性PPARG结合化合物的生物测定方法和药物组合物。
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公开(公告)号：US20140187554A1
公开(公告)日：2014-07-03
申请号：US14118116
申请日：2012-05-16
申请人： Theodore Mark Kamenecka , Patrick R. Griffin , Youseung Shin , Yuanjun He , Anne-Laure Blayo , Brent R. Lyda , Marcel Koenig , Naresh Kumar , Thomas Burris
发明人： Theodore Mark Kamenecka , Patrick R. Griffin , Youseung Shin , Yuanjun He , Anne-Laure Blayo , Brent R. Lyda , Marcel Koenig , Naresh Kumar , Thomas Burris
IPC分类号： C07D317/50 , A61K31/496 , C07D295/096 , A61K45/06 , C07D295/185 , A61K31/5375 , A61K31/5377 , C07D213/36 , A61K31/495
CPC分类号： C07D317/50 , A61K31/495 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K45/06 , C07D207/09 , C07D209/14 , C07D211/22 , C07D213/36 , C07D213/61 , C07D213/64 , C07D213/74 , C07D213/82 , C07D215/12 , C07D233/61 , C07D277/28 , C07D277/64 , C07D295/096 , C07D295/185 , C07D295/205 , C07D295/215 , C07D295/26 , C07D307/24 , C07D317/58 , C07D319/20 , C07D333/20 , C07D333/34 , C07D401/12
摘要： The invention provides small molecule modulators of retinoic acid receptor-related orphan receptors such as RORα, RORβ, or RORγ. Compounds of the invention can be effective modulators at concentrations ineffective to act on LXR receptors, or on other nuclear receptors, or other biological targets. Methods of modulation the RORs and methods of treating metabolic disorders, immune disorders, cancer, and CNS disorders wherein modulation of an ROR is medically indicated are also provided.
摘要翻译： 本发明提供了视黄酸受体相关的孤儿受体如RORα，ROR和bgr或RORγ的小分子调节剂。 本发明的化合物可以是无效作用于LXR受体或其它核受体或其他生物靶标的有效调节剂。 还提供调节ROR的方法和治疗代谢紊乱，免疫疾病，癌症和中枢神经系统疾病的方法，其中医学指示ROR的调节。
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公开(公告)号：US09586928B2
公开(公告)日：2017-03-07
申请号：US14118116
申请日：2012-05-16
申请人： Theodore Mark Kamenecka , Patrick R. Griffin , Youseung Shin , Yuanjun He , Anne-Laure Blayo , Brent R. Lyda , Marcel Koenig , Naresh Kumar , Thomas Burris
发明人： Theodore Mark Kamenecka , Patrick R. Griffin , Youseung Shin , Yuanjun He , Anne-Laure Blayo , Brent R. Lyda , Marcel Koenig , Naresh Kumar , Thomas Burris
IPC分类号： C07D213/74 , C07D213/36 , C07D295/096 , C07D295/185 , C07D295/195 , C07D295/26 , C07D277/64 , C07D207/09 , C07D211/22 , C07D233/61 , C07D317/50 , C07D213/82 , C07D215/12 , C07D317/58 , C07D319/20 , C07D333/20 , C07D333/34 , C07D401/12 , C07D277/28 , C07D209/14 , C07D295/205 , C07D295/215 , C07D213/61 , C07D213/64 , C07D307/24 , A61K31/495 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K45/06
CPC分类号： C07D317/50 , A61K31/495 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K45/06 , C07D207/09 , C07D209/14 , C07D211/22 , C07D213/36 , C07D213/61 , C07D213/64 , C07D213/74 , C07D213/82 , C07D215/12 , C07D233/61 , C07D277/28 , C07D277/64 , C07D295/096 , C07D295/185 , C07D295/205 , C07D295/215 , C07D295/26 , C07D307/24 , C07D317/58 , C07D319/20 , C07D333/20 , C07D333/34 , C07D401/12
摘要： The invention provides small molecule modulators of retinoic acid receptor-related orphan receptors such as RORα, RORβ, or RORγ, of formula with the variable atoms as defined herein and R1 comprising a hydroxyl- or alkoxyl-substituted fluoroalkyl group. Compounds of the invention can be effective modulators at concentrations ineffective to act on LXR receptors, or on other nuclear receptors, or other biological targets. Methods of modulation the RORs and methods of treating metabolic disorders, immune disorders, cancer, and CNS disorders wherein modulation of an ROR is medically indicated are also provided.
摘要翻译： 本发明提供了视黄酸受体相关的孤儿受体如RORα，ROR和bgr或RORγ的小分子调节剂。 本发明的化合物可以是无效作用于LXR受体或其它核受体或其他生物靶标的有效调节剂。 还提供调节ROR的方法和治疗代谢紊乱，免疫疾病，癌症和中枢神经系统疾病的方法，其中医学指示ROR的调节。
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公开(公告)号：US20140249196A1
公开(公告)日：2014-09-04
申请号：US13811969
申请日：2012-11-20
IPC分类号： C07D235/06 , C07D405/12 , A61K45/06 , A61K31/4184
CPC分类号： C07D235/06 , A61K31/4184 , A61K45/06 , C07D235/08 , C07D401/12 , C07D405/12 , C07D417/12
摘要： The invention provides molecular entities that bind with high affinity to PPARG (PPARγ), inhibit cdk5-mediated phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes or obesity. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.
摘要翻译： 本发明提供了以高亲和力结合PPARG（PPARγ），抑制cdk5介导的PPARG磷酸化，但不对PPARG发挥激动作用的分子实体。 本发明的化合物可用于治疗其中PPARG起作用的患者中的病症，例如糖尿病或肥胖症。 还提供了制备化合物的方法，用于评价本发明的化合物作为非激动性PPARG结合化合物的生物测定方法和药物组合物。
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公开(公告)号：US20140288090A1
公开(公告)日：2014-09-25
申请号：US13811973
申请日：2012-11-20
IPC分类号： C07D231/56 , C07D403/06 , C07D401/06 , C07D405/06 , C07D405/12 , C07D403/10
CPC分类号： C07D231/56 , A61K45/06 , C07D401/06 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/06 , C07D405/12
摘要： The invention provides molecular entities that bind with high affinity to PPARG (PPARγ), inhibit cdk5-mediated phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes or obesity. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.
摘要翻译： 本发明提供了以高亲和力结合PPARG（PPARγ），抑制cdk5介导的PPARG磷酸化，但不对PPARG发挥激动作用的分子实体。 本发明的化合物可用于治疗其中PPARG起作用的患者中的病症，例如糖尿病或肥胖症。 还提供了制备化合物的方法，用于评价本发明的化合物作为非激动性PPARG结合化合物的生物测定方法和药物组合物。
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公开(公告)号：US09018205B2
公开(公告)日：2015-04-28
申请号：US13766075
申请日：2013-02-13
申请人： Theodore Mark Kamenecka , Rong Jiang , Xinyi Song , Philip LoGrasso , Michael Darin Cameron , Derek R. Duckett
发明人： Theodore Mark Kamenecka , Rong Jiang , Xinyi Song , Philip LoGrasso , Michael Darin Cameron , Derek R. Duckett
IPC分类号： A61K31/505 , A61K31/506 , A61K31/4196 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/4965 , A61K31/5377 , C07D239/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/12 , C07D491/10
CPC分类号： C07D239/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/12 , C07D491/10
摘要： The present invention provides novel substituted pyrimidinyl-amines that are useful as inhibitors of protein kinases, especially c-Jun N-terminal kinases (JNK) and pharmaceutical compositions thereof and methods of using the same for treating conditions responsive to the inhibition of the JNK pathway.
摘要翻译： 本发明提供了可用作蛋白激酶抑制剂，特别是c-Jun N-末端激酶（JNK）的新型取代的嘧啶基胺及其药物组合物，以及用于治疗对抑制JNK途径有反应的病症的方法 。
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公开(公告)号：US20130231336A1
公开(公告)日：2013-09-05
申请号：US13766075
申请日：2013-02-13
申请人： Theodore Mark Kamenecka , Rong Jiang , Xinyi Song , Philip LoGrasso , Michael Darin Cameron , Derek R. Duckett
发明人： Theodore Mark Kamenecka , Rong Jiang , Xinyi Song , Philip LoGrasso , Michael Darin Cameron , Derek R. Duckett
IPC分类号： C07D239/42 , C07D403/14 , C07D413/12 , C07D403/12 , C07D401/14
CPC分类号： C07D239/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/12 , C07D491/10
摘要： The present invention provides novel substituted pyrimidinyl-amines that are useful as inhibitors of protein kinases, especially c-Jun N-terminal kinases (JNK) and pharmaceutical compositions thereof and methods of using the same for treating conditions responsive to the inhibition of the JNK pathway.
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