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1. 发明申请

WO2014200682A1 BIDENTATE-BINDING MODULATORS OF LRRK2 AND JNK KINASES 审中-公开
标题翻译： LRRK2和JNK KINASES的双相结合调节剂
公开(公告)号：WO2014200682A1
公开(公告)日：2014-12-18
申请号：PCT/US2014/039190
申请日：2014-05-22
申请人： THE SCRIPPS RESEARCH INSTITUTE , FENG, Yangbo , LOGRASSO, Philip
发明人： FENG, Yangbo , LOGRASSO, Philip
IPC分类号： A61K31/416 , C07D405/12 , C07D319/16
CPC分类号： C07K5/06026 , A61K31/416 , A61K38/00 , C07D231/56 , C07D405/12 , C07K5/101 , C07K7/06
摘要： Both JNK and LRRK2 are associated with Parkinson's disease (PD), myocardial infarction (Ml), and other medical disorders. Here we report a reasonably selective and potent kinase inhibitors (e.g., compounds 6 and 10) that bound to both JNK and LRRK2 (a dual inhibitor). A bidentate-binding strategy that simultaneously utilized the ATP hinge binding and a unique protein surface site outside of the ATP pocket was applied to the design and identification of this kind of inhibitor. Compound 6 was a potent JNK3 and modest LRRK2 dual inhibitor with an enzyme IC50 value of 12 nM and 99 nM (LRRK2-G2019S), respectively. 6 also exhibited good cell potency, inhibited LRRK2:G2019S induced mitochondrial dysfunction in SHSY5Y cells, and was demonstrated to be reasonably selective against a panel of 116 kinases from representative kinase families.
摘要翻译： JNK和LRRK2均与帕金森病（PD），心肌梗死（M1）和其他医学疾病有关。在这里，我们报告了结合JNK和LRRK2（双重抑制剂）的合理选择性和有效的激酶抑制剂（例如，化合物6和10）。同时使用ATP铰链结合和ATP口袋外的独特蛋白质表面位点的二齿结合策略被应用于这种抑制剂的设计和鉴定。化合物6是分别具有12nM和99nM（LRRK2-G2019S）的酶IC 50值的有效的JNK3和适度的LRRK2双重抑制剂。 6也表现出良好的细胞效能，抑制LRRK2：G2019S诱导SHSY5Y细胞的线粒体功能障碍，并且被证明对来自代表性激酶家族的116个激酶的组合是合理选择性的。

2. 发明申请

WO2010056758A1 QUINAZOLINE DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：喹诺酮衍生物作为激酶抑制剂
公开(公告)号：WO2010056758A1
公开(公告)日：2010-05-20
申请号：PCT/US2009/064048
申请日：2009-11-11
申请人： FENG, Yangbo , LOGRASSO, Philip , BANNISTER, Thomas , SCHROETER, Thomas , FANG, Xingang , YIN, Yan , CHEN, Yen Ting , SESSIONS, Hampton , CHOWDHURY, Sarwat , LUO, Jun-Li , VOJKOVSKY, Tomas
发明人： FENG, Yangbo , LOGRASSO, Philip , BANNISTER, Thomas , SCHROETER, Thomas , FANG, Xingang , YIN, Yan , CHEN, Yen Ting , SESSIONS, Hampton , CHOWDHURY, Sarwat , LUO, Jun-Li , VOJKOVSKY, Tomas
IPC分类号： A01N43/54 , A61K31/517
CPC分类号： A61K31/517 , A61K38/217 , A61K45/06 , C07D403/04 , C07D403/14 , C07D405/14 , C07D473/00 , C07D487/04 , A61K2300/00
摘要： The invention is directed to quinazoline compounds that can inhibit the bioactivity of one or more kinase enzymes, including a Rho kinase, an AKT kinase, a p70S6K kinase, a LIM kinase, an IKK kinase, a Fit kinase, an Aurora kinase, or a Src kinase, or any combination thereof; to methods of use of those compounds; and to methods of preparation of those compounds. The inventive compounds can be used in the treatment of malconditions including cardiovascular disease, neurogenic pain, hypertension, atherosclerosis, angina, stroke, arterial obstruction, peripheral arterial disease, erectile dysfunction, acute and chronic pain, dementia, Alzheimer's disease, Parkinson's disease, neuronal degeneration, asthma, amyotrophic lateral sclerosis, spinal cord injury, rheumatoid arthritis, osteoarthritis, osteoporosis, psoriasis, cerebral vasospasm, open angle glaucoma, multiple sclerosis, pulmonary hypertension, acute respiratory distress syndrome, inflammation, diabetes, urinary organ diseases and benign prostatic hypertrophy (BPH), metastasis, cancer, glaucoma, ocular hypertension, retinopathy, autoimmune disease, viral infection, or myocardial pathology.
摘要翻译：本发明涉及可抑制一种或多种激酶的生物活性的喹唑啉化合物，包括Rho激酶，AKT激酶，p70S6K激酶，LIM激酶，IKK激酶，Fit激酶，Aurora激酶或 Src激酶或其任何组合; 使用这些化合物的方法; 以及这些化合物的制备方法。本发明化合物可用于治疗包括心血管疾病，神经源性疼痛，高血压，动脉粥样硬化，心绞痛，中风，动脉阻塞，外周动脉疾病，勃起功能障碍，急性和慢性疼痛，痴呆，阿尔茨海默病，帕金森病，神经元变性，哮喘，肌萎缩性侧索硬化，脊髓损伤，类风湿性关节炎，骨关节炎，骨质疏松症，银屑病，脑血管痉挛，开角型青光眼，多发性硬化，肺动脉高压，急性呼吸窘迫综合征，炎症，糖尿病，尿器官疾病和良性前列腺肥大（BPH），转移，癌症，青光眼，高眼压症，视网膜病变，自身免疫性疾病，病毒感染或心肌病理学。

3. 发明申请

WO2009079009A1 ANILIDES AND ANALOGS AS RHO KINASE INHIBITORS 审中-公开
标题翻译：抗氧化剂和类似物作为RHO激酶抑制剂
公开(公告)号：WO2009079009A1
公开(公告)日：2009-06-25
申请号：PCT/US2008/013851
申请日：2008-12-18
申请人： FENG, Yangbo , LOGRASSO, Philip , BANNISTER, Thomas , SCHROETER, Thomas , FANG, Xingang , CHEN, Yen, Ting , YIN, Yan , SMOLINSKI, Michael, P. , YAO, Lei , WANG, Bo , SESSIONS, Hampton
发明人： FENG, Yangbo , LOGRASSO, Philip , BANNISTER, Thomas , SCHROETER, Thomas , FANG, Xingang , CHEN, Yen, Ting , YIN, Yan , SMOLINSKI, Michael, P. , YAO, Lei , WANG, Bo , SESSIONS, Hampton
IPC分类号： A01N43/56
CPC分类号： C07D405/12 , C07D405/14 , C07D409/14 , C07D471/04 , C07D487/04
摘要： Compounds useful as Rho kinase inhibitors of formula (I): wherein variable are as defined herein are provided. Methods of treatment of malconditions mediated by Rho kinase, and methods of preparation of the compounds, are also provided.
摘要翻译：可用作式（I）的Rho激酶抑制剂的化合物：其中变量如本文所定义。还提供了由Rho激酶介导的病症治疗方法和化合物的制备方法。

4. 发明申请

WO2009032861A1 SUBSTITUTED PYRIMIDINYL-AMINES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的取代的吡咯烷
公开(公告)号：WO2009032861A1
公开(公告)日：2009-03-12
申请号：PCT/US2008/075151
申请日：2008-09-03
申请人： THE SCRIPPS RESEARCH INSTITUTE , KAMENECKA, Theodore, Mark , JIANG, Rong , SONG, Xinyi , LOGRASSO, Philip , CAMERON, Michael, Darin
发明人： KAMENECKA, Theodore, Mark , JIANG, Rong , SONG, Xinyi , LOGRASSO, Philip , CAMERON, Michael, Darin
IPC分类号： A01N43/04 , A61K31/70
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）及其药物组合物的新型取代的嘧啶基胺，以及用于治疗响应于JNK通路抑制的病症的方法。

5. 发明申请

WO2009079008A8 BENZOPYRANS AND ANALOGS AS RHO KINASE INHIBITORS 审中-公开
标题翻译：苯并噻唑和类似物作为RHO激酶抑制剂
公开(公告)号：WO2009079008A8
公开(公告)日：2010-07-08
申请号：PCT/US2008013844
申请日：2008-12-18
申请人： SCRIPPS RESEARCH INST , FENG YANGBO , LOGRASSO PHILIP , BANNISTER THOMAS , SCHROETER THOMAS , CHEN YEN TING , YIN YAN , SESSIONS HAMPTON , SMOLINSKI MICHAEL P , YAO LEI , WANG BO , FRACKOWIAK-WOJTASEK BOZENA
发明人： FENG YANGBO , LOGRASSO PHILIP , BANNISTER THOMAS , SCHROETER THOMAS , CHEN YEN TING , YIN YAN , SESSIONS HAMPTON , SMOLINSKI MICHAEL P , YAO LEI , WANG BO , FRACKOWIAK-WOJTASEK BOZENA
IPC分类号： A61K31/535
CPC分类号： C07D405/12 , C07D405/14 , C07D409/14 , C07D471/04 , C07D487/04
摘要： Compounds useful as Rho kinase inhibitors of formula (I) wherein the variables are as defined herein are provided. Methods of treatment of malconditions mediated by Rho kinase, and methods of preparation of the compounds, are also provided.
摘要翻译：提供了可用作式（I）的Rho激酶抑制剂的化合物，其中变量如本文所定义。还提供了由Rho激酶介导的病症治疗方法和化合物的制备方法。

6. 发明申请

WO2009079008A1 BENZOPYRANS AND ANALOGS AS RHO KINASE INHIBITORS 审中-公开
标题翻译：苯并噻唑和类似物作为RHO激酶抑制剂
公开(公告)号：WO2009079008A1
公开(公告)日：2009-06-25
申请号：PCT/US2008/013844
申请日：2008-12-18
申请人： FENG, Yangbo , LOGRASSO, Philip , BANNISTER, Thomas , SCHROETER, Thomas , CHEN, Yen, Ting , YIN, Yan , SESSIONS, Hampton , SMOLINSKI, Michael, P. , YAO, Lei , WANG, Bo , FRACKOWIAK-WOJTASEK, Bozena
发明人： FENG, Yangbo , LOGRASSO, Philip , BANNISTER, Thomas , SCHROETER, Thomas , CHEN, Yen, Ting , YIN, Yan , SESSIONS, Hampton , SMOLINSKI, Michael, P. , YAO, Lei , WANG, Bo , FRACKOWIAK-WOJTASEK, Bozena
IPC分类号： A61K31/535
CPC分类号： C07D405/12 , C07D405/14 , C07D409/14 , C07D471/04 , C07D487/04
摘要： Compounds useful as Rho kinase inhibitors of formula (I) wherein the variables are as defined herein are provided. Methods of treatment of malconditions mediated by Rho kinase, and methods of preparation of the compounds, are also provided.
摘要翻译：提供了可用作式（I）的Rho激酶抑制剂的化合物，其中变量如本文所定义。还提供了由Rho激酶介导的病症治疗方法和化合物的制备方法。

7. 发明申请

WO02090524A3 ISOLATED NUCLEIC ACID MOLECULES ENCODING A NOVEL HUMAN SIGNAL TRANSDUCING KINASE-MAPKAP-2; ENCODED PROTEINS, CELLS TRANSFORMED THEREWITH AND USES THEREOF 审中-公开
标题翻译：分离的核酸分子编码新的人类信号转导激酶MAPKAP-2; 编码的蛋白质，其转化的细胞及其用途
公开(公告)号：WO02090524A3
公开(公告)日：2003-05-08
申请号：PCT/US0205670
申请日：2002-02-25
申请人： MERCK & CO INC , LOGRASSO PHILIP , HAWKINS JULIO , LISNOCK JEAN MARIE
发明人： LOGRASSO PHILIP , HAWKINS JULIO , LISNOCK JEAN MARIE
IPC分类号： G01N33/50 , A61K38/45 , A61P1/04 , A61P9/10 , A61P11/06 , A61P19/02 , A61P25/28 , A61P29/00 , A61P31/04 , A61P37/02 , A61P37/06 , A61P37/08 , C07K16/40 , C12N1/21 , C12N5/10 , C12N9/12 , C12N15/09 , C12Q1/02 , C12Q1/48 , C12Q1/68 , G01N33/15 , G01N33/53 , G01N33/566 , G01N33/573 , C07H21/04 , A61K38/51 , C07H21/02 , C07K1/00 , C12N1/20 , C12N5/00 , C12N15/00
CPC分类号： C12N9/1205
摘要： Disclosed herein are two newly identified enzymes - mitogen-activated protein kinase-activated protein kinase-2, each comprising a sequence of nucleotides as set forth in SEQ ID NOs: 1 and 3. Each of the herein disclosed enzymes is a serine/threonine signal transduction kinase that is phosphorylated and activated by Erks and p38 MAPK in vitro. Also disclosed, inter alia, are cells containing the recombinant nucleic acid molecules; antisense constructs thereto; antibodies specific for each of the disclosed proteins; methods for using the novel nucleic acid molecules and their gene products including kits containing the same.
摘要翻译：本文公开了两种新鉴定的酶 - 丝裂原活化蛋白激酶活化蛋白激酶-2，每个酶包含如SEQ ID NO：1和3所示的核苷酸序列。本文公开的每一种酶是丝氨酸/苏氨酸信号通过Erks和p38 MAPK在体外磷酸化和活化的转导激酶。还公开了特别是含有重组核酸分子的细胞; 反义构建体; 对于每个所公开的蛋白质具有特异性的抗体; 使用新型核酸分子及其基因产物的方法，包括含有该核酸分子的试剂盒。

8. 发明申请

WO2015084936A1 NOVEL COMPOUNDS AS JNK KINASE INHIBITORS 审中-公开
标题翻译：新型化合物作为JNK激酶抑制剂
公开(公告)号：WO2015084936A1
公开(公告)日：2015-06-11
申请号：PCT/US2014/068333
申请日：2014-12-03
申请人： THE SCRIPPS RESEARCH INSTITUTE , FENG, Yangbo , LOGRASSO, Philip , ZHENG, Ke , PARK, Chul Min
发明人： FENG, Yangbo , LOGRASSO, Philip , ZHENG, Ke , PARK, Chul Min
IPC分类号： A01N43/56
CPC分类号： C07D231/40 , C07D231/54 , C07D239/47 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present invention is directed to modulators, such as inhibitors, of JNK isoform 2 (JNK2) or isoform 3 (JNK3) comprising compounds of formula (I) or formula (II) as described herein. Compounds of the invention can be used for treatment of a medical disorder in a patient wherein modulation of JNK3 is medically indicated, such as when the disorder is Parkinsons disease (PD) Alzheimer's disease (AD), Huntington's disease (HD), amyotrophic lateral sclerosis (ALS), multiple sclerosis (MS), myocardial infarction (MI), glaucoma, obesity, diabetes, cancer, rheumatoid arthritis, fibrotic disease, pulmonary fibrosis, kidney disease, liver inflammation, Crohns disease, hearing loss, Prader Willi syndrome, or a condition where modification of feeding behavior is medically indicated.
摘要翻译：本发明涉及包含本文所述的式（I）或式（II）化合物的JNK同种型2（JNK2）或同种型3（JNK3）的调节剂，例如抑制剂。本发明的化合物可用于治疗患有医学上指示JNK3调节的患者的医学病症，例如当疾病是帕金森病（PD）阿尔茨海默病（AD），亨廷顿病（HD），肌萎缩性侧索硬化症（ALS），多发性硬化症（MS），心肌梗塞（MI），青光眼，肥胖症，糖尿病，癌症，类风湿性关节炎，纤维化疾病，肺纤维化，肾脏疾病，肝脏炎症，克罗恩病，听力损失，Prader Willi综合征或在医疗上指示进食行为改变的条件。

9. 发明申请

WO2011050245A1 BICYCLIC HETEROARYLS AS KINASE INHIBITORS 审中-公开
标题翻译：双相异构体作为激酶抑制剂
公开(公告)号：WO2011050245A1
公开(公告)日：2011-04-28
申请号：PCT/US2010/053690
申请日：2010-10-22
申请人： FENG, Yangbo , CHEN, Yen Ting , SESSIONS, Hampton , MISHRA, Jitendra K. , CHOWDHURY, Sarwat , YIN, Yan , LOGRASSO, Philip , LUO, Jun-Li , BANNISTER, Thomas , SCHROETER, Thomas
发明人： FENG, Yangbo , CHEN, Yen Ting , SESSIONS, Hampton , MISHRA, Jitendra K. , CHOWDHURY, Sarwat , YIN, Yan , LOGRASSO, Philip , LUO, Jun-Li , BANNISTER, Thomas , SCHROETER, Thomas
IPC分类号： A01N43/38 , A61K31/40
CPC分类号： A61K31/4025 , A61K31/416 , A61K31/506
摘要： The invention is directed to heteroaryl compounds useful as inhibitors of various kinase enzymes. In various embodiments, the invention provides a heteroaryl compound having inhibitory bioactivity with respect to a Rho kinase, an AKT kinase, a p70S6K kinase, a LIM kinase, an IKK kinase, a Flt kinase, an Aurora kinase, or a Src kinase, or any combination thereof. Compounds of the invention include bicyclic heteroaryl compounds of formula (I), which can contain a bridging nitrogen atom at a ring junction. The invention further provides methods of synthesis of compounds of the invention, pharmaceutical compositions, pharmaceutical combinations, and methods of treatment of malconditions using compounds of the invention.
摘要翻译：本发明涉及可用作各种激酶的抑制剂的杂芳基化合物。在各种实施方案中，本发明提供了相对于Rho激酶，AKT激酶，p70S6K激酶，LIM激酶，IKK激酶，Flt激酶，极光激酶或Src激酶具有抑制生物活性的杂芳基化合物，或其任何组合。本发明的化合物包括式（I）的双环杂芳基化合物，其可以在环结上含有桥连氮原子。本发明进一步提供了使用本发明化合物合成本发明化合物，药物组合物，药物组合以及治疗病症的方法。

10. 发明申请

WO2010036316A1 UREA AND CARBAMATE COMPOUNDS AND ANALOGS AS KINASE INHIBITORS 审中-公开
标题翻译：尿素和碳酸酯化合物和类似物作为激酶抑制剂
公开(公告)号：WO2010036316A1
公开(公告)日：2010-04-01
申请号：PCT/US2009/005177
申请日：2009-09-17
申请人： FENG, Yangbo , LOGRASSO, Philip , SCHROETER, Thomas , YIN, Yan
发明人： FENG, Yangbo , LOGRASSO, Philip , SCHROETER, Thomas , YIN, Yan
IPC分类号： A01N47/28 , A61K31/56
CPC分类号： A61K31/56
摘要： The invention is directed to compounds that can inhibit the bioactivity of one or more kinases such as any of Rho kinases, PKB (Akt) kinases, p70S6K kinase, LIM kinases, or IKK kinases, to methods of use of those compounds, and to methods of preparation of those compounds The inventive compounds can be used In the treatment of a variety of medical malconditions.
摘要翻译：本发明涉及可以抑制一种或多种激酶（例如任何Rho激酶，PKB（Akt）激酶，p70S6K激酶，LIM激酶或IKK激酶）的生物活性的化合物，以及使用这些化合物的方法这些化合物的制备本发明化合物可用于治疗各种医疗条件。

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