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1. 发明申请

US20140187554A1 MODULATORS OF THE NUCLEAR HORMONE RECEPTOR ROR 有权
标题翻译：核激素受体ROR的调节剂
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。

2. 发明授权

US09586928B2 Modulators of the nuclear hormone receptor ROR 有权
标题翻译：核激素受体ROR的调节剂
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。

3. 发明授权

US09051265B2 N-benzylindole modulators of PPARG 有权
标题翻译： PPARG的N-苄基吲哚调节剂
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。

4. 发明申请

US20120309757A1 N-BIPHENYLMETHYLINDOLE MODULATORS OF PPARG 有权
标题翻译： PPARG的N-二苯基甲基咪唑调节剂
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。

5. 发明授权

US08957093B2 N-biphenylmethylindole modulators of PPARG 有权
标题翻译： PPARG的N-联苯甲基吲哚调节剂
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。

6. 发明申请

US20120309769A1 N-BENZYLINDOLE MODULATORS OF PPARG 有权
标题翻译： PPARG的N-苄基吲哚调节剂
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。

7. 发明授权

US08501763B2 Inhibitors of focal adhesion kinase 有权
标题翻译：粘着斑激酶抑制剂
公开(公告)号：US08501763B2
公开(公告)日：2013-08-06
申请号：US12531010
申请日：2008-03-10
申请人： Congxin Liang , Marcel Koenig , Yuanjun He , Par Holmberg
发明人： Congxin Liang , Marcel Koenig , Yuanjun He , Par Holmberg
IPC分类号： A01N43/42 , A61K31/44 , A61K31/4965 , A61K31/535 , C07D295/00 , C07D265/30
CPC分类号： C07D491/113 , C07D213/72 , C07D213/74 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions.
摘要翻译：本发明提供了粘着斑激酶抑制剂，其是参与将细胞的细胞骨架与细胞外基质连接的酶，其涉及细胞迁移，细胞增殖和细胞存活等过程。抑制剂是5-取代的2,4-二氨基吡啶的衍生物，其中取代基如本文所定义。本发明还提供了一种使用抑制剂治疗癌症的方法，以及通过使用偶联反应制备抑制剂的方法。

8. 发明申请

US20110046121A1 INHIBITORS OF FOCAL ADHESION KINASE 有权
标题翻译：焦糖粘连激酶抑制剂
公开(公告)号：US20110046121A1
公开(公告)日：2011-02-24
申请号：US12531010
申请日：2008-03-10
申请人： Congxin Liang , Marcel Koenig , Yuanjun He , Par Holmberg
发明人： Congxin Liang , Marcel Koenig , Yuanjun He , Par Holmberg
IPC分类号： A61K31/5377 , C07D413/14 , C07D417/12 , A61K31/541
CPC分类号： C07D491/113 , C07D213/72 , C07D213/74 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions.
摘要翻译：本发明提供了粘着斑激酶抑制剂，其是参与将细胞的细胞骨架与细胞外基质连接的酶，其参与诸如细胞迁移，细胞增殖和细胞存活的过程。抑制剂是5-取代的2,4-二氨基吡啶的衍生物，其中取代基如本文所定义。本发明还提供了一种使用抑制剂治疗癌症的方法，以及通过使用偶联反应制备抑制剂的方法。

9. 发明申请

US20090033036A1 GAS TURBINE WITH ANNULAR HEAT SHIELD 审中-公开
标题翻译：具有环形热风罩的气体涡轮机
公开(公告)号：US20090033036A1
公开(公告)日：2009-02-05
申请号：US12189976
申请日：2008-08-12
申请人： Peter Marx , James Robert Wise , Marcel Koenig
发明人： Peter Marx , James Robert Wise , Marcel Koenig
IPC分类号： F01D11/00
CPC分类号： F01D11/005 , F01D11/00 , F05D2240/57 , F05D2250/70 , F16J15/0887
摘要： A gas turbine includes a supporting structure which concentrically surrounds a hot gas path and is shielded with respect to the hot gas path by an annular heat shield (15′), which heat shield (15′) includes a multiplicity of segments which are arranged one behind the other in a circumferential direction and which in each case butt against one another in the circumferential direction so as to form a gap, seals (16′), being arranged for sealing off the gaps between the segments butting against one another, the seals having thin elongate sealing strips (23), which are accommodated in corresponding sealing slots (19), delimited transversely with respect to the longitudinal direction by a wall (25), in the mutually opposite end faces of the segments of the heat shield (15′) which butt against one another. Vibrationally-induced rubbing through of the wall is inhibited or prevented by the frictional surface between the wall (25) and the sealing strips (23) being markedly enlarged with respect to the end face (22) of the sealing strip (23).
摘要翻译：一种燃气轮机包括一个支撑结构，该支撑结构同心地围绕热气体路径，并通过一个环形隔热罩（15'）相对于热气路径进行屏蔽，该隔热罩（15'）包含多个段，在圆周方向上彼此相对并且在每个情况下在圆周方向上彼此对接以形成间隙，密封件（16'）被设置用于密封彼此对接的部分之间的间隙，密封件具有细长的密封条（23），其被容纳在相应的密封槽（19）中，在隔热件（15）的段的相互相对的端面中通过壁（25）横向相对于纵向方向限定 '）彼此对接。通过壁（25）和密封条（23）之间的摩擦表面相对于密封条（23）的端面（22）显着地增大，可以抑制或阻止振动引起的壁的摩擦。

10. 发明授权

US07122548B2 Triazolotriazine compounds and uses thereof 失效
标题翻译：三唑并三嗪化合物及其用途
公开(公告)号：US07122548B2
公开(公告)日：2006-10-17
申请号：US10874743
申请日：2004-06-24
申请人： Fang-Jie Zhang , Tomas Vojkovsky , Ping Huang , Congxin Liang , Steven Huy Do , Marcel Koenig , Jingrong Cui
发明人： Fang-Jie Zhang , Tomas Vojkovsky , Ping Huang , Congxin Liang , Steven Huy Do , Marcel Koenig , Jingrong Cui
IPC分类号： C07D487/04 , A61K31/53 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of the Formula (I), and their pharmaceutically acceptable salts. These compounds modulate the activity of c-Met and are therefore expected to be useful in the prevention and treatment of c-Met related disorders such as cancer
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐。这些化合物调节c-Met的活性，因此预期可用于预防和治疗c-Met相关疾病如癌症

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