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1. 发明专利

IL280182D0 Pyridin-2-one compounds useful as smarca2 antagonists 未知
公开(公告)号：IL280182D0
公开(公告)日：2021-03-01
申请号：IL28018221
申请日：2021-01-14
申请人： EPIZYME INC , HARVEY DARREN MARTIN , MORADEI OSCAR , LAMPE JOHN W , CAMPBELL JOHN EMMERSON , DUNCAN KENNETH WILLIAM , MUNCHHOF MICHAEL JOHN
发明人： HARVEY DARREN MARTIN , MORADEI OSCAR , LAMPE JOHN W , CAMPBELL JOHN EMMERSON , DUNCAN KENNETH WILLIAM , MUNCHHOF MICHAEL JOHN
IPC分类号： A61P35/00
摘要： This disclosure generally relates to pyridine-2-one compounds of formula (I) and methods of using them in the treatment of a disorder, such as cancer or a SMARCA2-associated disorder, including as antagonists (e.g., inhibitors) of SMARCA2. The present disclosure provides treatment modalities, e.g., strategies, treatment methods, patient stratification methods, compounds, combinations, and compositions that are useful for the treatment of disorders, e.g., proliferative disorders, such as certain cancers. Some aspects of this disclosure provide treatment modalities, methods, strategies, compounds, compositions, combinations, and dosage forms for the treatment of cell proliferative disorders, e.g., cancers with decreased activity or function, or loss of function, of SMARCA4 with a SMARCA2 antagonist.

2. 发明专利

CA2029651A1 TRICYCLIC PTERIDINONES AND A PROCESS FOR THEIR PREPARATION 未知
公开(公告)号：CA2029651A1
公开(公告)日：1991-05-18
申请号：CA2029651
申请日：1990-11-09
申请人： DAVEY DAVID D , LAMPE JOHN W
发明人： DAVEY DAVID D , LAMPE JOHN W
IPC分类号： A61K31/505 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , C07D487/14

3. 发明申请

WO2016089833A1 NOVEL TRICYCLIC COMPOUNDS AS INHIBITORS OF MUTANT IDH ENZYMES 审中-公开
标题翻译：新型三聚体化合物作为突变体酶的抑制剂
公开(公告)号：WO2016089833A1
公开(公告)日：2016-06-09
申请号：PCT/US2015/063131
申请日：2015-12-01
申请人： MERCK SHARP & DOHME CORP. , FISCHER, Christian , BOGEN, Stephane, L. , CHILDERS, Matthew, L. , LLINAS, Francesc Xavier Fradera , KIM, Alexander, J. , LAMPE, John, W. , MACHACEK, Michelle, R. , MCMASTERS, Daniel, R. , PARKER, Dann, L., Jr. , SUN, Wanying , SCIAMMETTA, Nunzio , SHAO, Pengcheng, P. , SLOMAN, David, L. , UJJAINWALLA, Feroze , HUANG, Chunhui
发明人： FISCHER, Christian , BOGEN, Stephane, L. , CHILDERS, Matthew, L. , LLINAS, Francesc Xavier Fradera , KIM, Alexander, J. , LAMPE, John, W. , MACHACEK, Michelle, R. , MCMASTERS, Daniel, R. , PARKER, Dann, L., Jr. , SUN, Wanying , SCIAMMETTA, Nunzio , SHAO, Pengcheng, P. , SLOMAN, David, L. , UJJAINWALLA, Feroze , HUANG, Chunhui
IPC分类号： A01N43/00
CPC分类号： A61K31/5513 , A01N43/00 , A61K31/551 , A61K45/06 , A61P35/00 , C07D471/04 , C07D471/14 , C07D519/00 , A61K2300/00
摘要： The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I); wherein A is -C(R1)= or -N=; and X is selected from the group consisting of: (II-i), (II-ii), (II-iii), and (II-iv). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
摘要翻译：本发明涉及作为一种或多种突变体IDH酶抑制剂的式（I）的三环化合物：（I）; 其中A是-C（R 1）=或-N =; X选自：（II-i），（II-ii），（II-iii）和（II-iv）。本发明还涉及本文所述的三环化合物在潜在的治疗或预防涉及一种或多种突变体IDH酶的癌症中的用途。本发明还涉及包含这些化合物的组合物。本发明还涉及这些组合物在这种癌症的潜在预防或治疗中的用途。

4. 发明申请

WO2016089830A1 NOVEL TRICYCLIC COMPOUNDS AS INHIBITORS OF MUTANT IDH ENZYMES 审中-公开
标题翻译：新型三聚体化合物作为突变体酶的抑制剂
公开(公告)号：WO2016089830A1
公开(公告)日：2016-06-09
申请号：PCT/US2015/063127
申请日：2015-12-01
申请人： MERCK SHARP & DOHME CORP. , FISCHER, Christian , BOGEN, Stephane, L. , CHILDERS, Matthew, L. , LLINAS, Francesc Xavier Fradera , ELLIS, J. Michael , ESPOSITE, Sara , HOFFMAN, Dawn, M. , HUANG, Chunhui , KATTAR, Solomon , KIM, Alexander, J. , LAMPE, John, W. , MACHACEK, Michelle, R. , MCMASTERS, Daniel, R. , PARKER, Dann, L., Jr. , REUTERSHAN, Michael , SCIAMMETTA, Nunzio , SHAO, Pengcheng, P. , SLOMAN, David, L. , SUN, Wanying , UJJAINWALLA, Feroze , WU, Zhicai , YU, Yang , GIBEAU, Craig
发明人： FISCHER, Christian , BOGEN, Stephane, L. , CHILDERS, Matthew, L. , LLINAS, Francesc Xavier Fradera , ELLIS, J. Michael , ESPOSITE, Sara , HOFFMAN, Dawn, M. , HUANG, Chunhui , KATTAR, Solomon , KIM, Alexander, J. , LAMPE, John, W. , MACHACEK, Michelle, R. , MCMASTERS, Daniel, R. , PARKER, Dann, L., Jr. , REUTERSHAN, Michael , SCIAMMETTA, Nunzio , SHAO, Pengcheng, P. , SLOMAN, David, L. , SUN, Wanying , UJJAINWALLA, Feroze , WU, Zhicai , GIBEAU, Craig
IPC分类号： A01N43/00
CPC分类号： C07D471/04 , C07D471/14 , C07D519/00
摘要： The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes (I); wherein A is -C(R 1 )= or -N=; and X is selected from the group consisting of: (II-i), and (II-ii). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
摘要翻译：本发明涉及作为一种或多种突变体IDH酶（I）的抑制剂的式（I）的三环化合物; 其中A是-C（R 1）=或-N =; 并且X选自：（II-i）和（II-ii）。本发明还涉及本文所述的三环化合物在潜在的治疗或预防涉及一种或多种突变体IDH酶的癌症中的用途。本发明还涉及包含这些化合物的组合物。本发明还涉及这些组合物在这种癌症的潜在预防或治疗中的用途。

5. 发明申请

WO2012015760A1 METHOD FOR TREATING OPHTHALMIC DISEASES USING KINASE INHIBITOR COMPOUNDS IN PRODRUG FORMS 审中-公开
标题翻译：使用激素抑制剂化合物治疗原发性疾病的方法
公开(公告)号：WO2012015760A1
公开(公告)日：2012-02-02
申请号：PCT/US2011/045244
申请日：2011-07-25
申请人： INSPIRE PHARMACEUTICALS, INC. , LAMPE, John W. , SHAVER, Sammy R. , WATSON, Paul S.
发明人： LAMPE, John W. , SHAVER, Sammy R. , WATSON, Paul S.
IPC分类号： A01N43/34
CPC分类号： C07D401/12 , A61K9/0048 , C07D401/14 , C07D403/12
摘要： This invention is directed to prodrugs of rho kinase (ROCK) inhibitors. These prodrugs are in general the ester or the amide derivatives of the parent compounds. These prodrugs are often weak inhibitors of ROCK, but their parent compounds have good activities. Upon instillation into the eyes, the ester or the amide group of these prodrugs is rapidly hydrolyzed into alcohol, amine, or acid, and the prodrugs are converted into the active base compounds. The prodrugs of ROCK inhibitors provide several advantages such as delivery of higher concentrations of the active species into the target site and reduction of ocular discomfort. The invention is also directed to a method of treating ophthalmic diseases such as glaucoma, allergic conjunctivitis, macular edema, macular degeneration, and blepharitis, by administering an effective amount of a ROCK prodrug compound of Formula (I) to the eyes of the patient in need of.
摘要翻译：本发明涉及rho激酶（ROCK）抑制剂的前药。这些前药通常是母体化合物的酯或酰胺衍生物。这些前药通常是ROCK的弱抑制剂，但它们的母体化合物具有良好的活性。滴入眼中时，这些前体药物的酯或酰胺基被快速水解成醇，胺或酸，并将前体药物转化成活性碱化合物。 ROCK抑制剂的前药提供了几个优点，例如将较高浓度的活性物质递送到靶位点和减少眼部不适。本发明还涉及通过向患者的眼睛施用有效量的式（I）的ROCK前药化合物，治疗眼部疾病如青光眼，过敏性结膜炎，黄斑水肿，黄斑变性和睑炎，需要。

6. 发明申请

WO2008077057A3 CYTOSKELETAL ACTIVE RHO KINASE INHIBITOR COMPOUNDS, COMPOSITION AND USE 审中-公开
标题翻译： CYTOSKELETAL活性RHO激酶抑制剂化合物，组合物和用途
公开(公告)号：WO2008077057A3
公开(公告)日：2008-08-21
申请号：PCT/US2007087973
申请日：2007-12-18
申请人： INSPIRE PHARMACEUTICALS INC , LAMPE JOHN W , WATSON PAUL S , SLADE DAVID J , PETERSON WARD M , CREAN CHRISTOPHER S , VITTITOW JASON L , DECAMP JONATHAN BRYAN , PELZ NICHOLAS F
发明人： LAMPE JOHN W , WATSON PAUL S , SLADE DAVID J , PETERSON WARD M , CREAN CHRISTOPHER S , VITTITOW JASON L , DECAMP JONATHAN BRYAN , PELZ NICHOLAS F
IPC分类号： A61K31/505 , A61K31/47
CPC分类号： C07D401/12 , A61F9/00781 , A61K9/0048 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14
摘要： The present invention is directed to synthetic cytoskeletal active compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or Formula II, wherein said amount is effective to influence the actomyosin interactions, for example by leading to cellular relaxation and alterations in cell-substratum adhesions.
摘要翻译：本发明涉及作为ρ相关蛋白激酶抑制剂的合成细胞骨架活性化合物。本发明还涉及包含这些化合物和药学上可接受的载体的药物组合物。本发明还涉及预防或治疗与细胞骨架重组有关的疾病或病症的方法。在本发明的一个实施例中，该方法治疗增加的眼内压，例如原发性开角型青光眼。该方法包括向受试者施用治疗有效量的式I或式II的细胞骨架活性化合物，其中所述量有效影响肌动球蛋白相互作用，例如通过导致细胞松弛和细胞 - 基质粘连的改变。

7. 发明申请

WO2016089797A1 NOVEL TRICYCLIC COMPOUNDS AS INHIBITORS OF MUTANT IDH ENZYMES 审中-公开
标题翻译：新型三聚体化合物作为突变体酶的抑制剂
公开(公告)号：WO2016089797A1
公开(公告)日：2016-06-09
申请号：PCT/US2015/063061
申请日：2015-12-01
申请人： MERCK SHARP & DOHME CORP. , FISCHER, Christian , BOGEN, Stephane, L. , CHILDERS, Matthew, L. , LLINAS, Francesc Xavier Fradera , ELLIS, J. Michael , ESPOSITE, Sara , HONG, Qingmei , HUANG, Chunhui , KIM, Alexander, J. , LAMPE, John, W. , MACHACEK, Michelle, R. , MCMASTERS, Daniel, R. , OTTE, Ryan, D. , PARKER, Dann, L., Jr. , REUTERSHAN, Michael , SCIAMMETTA, Nunzio , SHAO, Pengcheng, P. , SLOMAN, David, L. , UJJAINWALLA, Feroze , WHITE, Catherine , WU, Zhicai , YU, Yang , ZHAO, Kake , GIBEAU, Craig , BIFTU, Tesfaye , BIJU, Purakkattle , CHEN, Lei , CLOSE, Joshua , FULLER, Peter, H. , HUANG, Xianhai , PARK, Min, K. , SIMOV, Vladimir , WITTER, David, J. , ZHANG, Hongjun
发明人： FISCHER, Christian , BOGEN, Stephane, L. , CHILDERS, Matthew, L. , LLINAS, Francesc Xavier Fradera , ELLIS, J. Michael , ESPOSITE, Sara , HONG, Qingmei , HUANG, Chunhui , KIM, Alexander, J. , LAMPE, John, W. , MACHACEK, Michelle, R. , MCMASTERS, Daniel, R. , OTTE, Ryan, D. , PARKER, Dann, L., Jr. , REUTERSHAN, Michael , SCIAMMETTA, Nunzio , SHAO, Pengcheng, P. , SLOMAN, David, L. , UJJAINWALLA, Feroze , WHITE, Catherine , WU, Zhicai , ZHAO, Kake , GIBEAU, Craig , BIFTU, Tesfaye , BIJU, Purakkattle , CHEN, Lei , CLOSE, Joshua , FULLER, Peter, H. , HUANG, Xianhai , PARK, Min, K. , SIMOV, Vladimir , WITTER, David, J. , ZHANG, Hongjun
IPC分类号： A01N43/00
CPC分类号： C07D498/08 , A01N43/00 , C07D471/04 , C07D471/08 , C07D498/04 , C07D498/10
摘要： The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
摘要翻译：本发明涉及作为一种或多种突变体IDH酶的抑制剂的式（I）的三环化合物：（I）。本发明还涉及本文所述的三环化合物在潜在的治疗或预防涉及一种或多种突变体IDH酶的癌症中的用途。本发明还涉及包含这些化合物的组合物。本发明还涉及这些组合物在这种癌症的潜在预防或治疗中的用途。

8. 发明申请

WO2011075415A1 BRIDGED BICYCLIC RHO KINASE INHIBITOR COMPOUNDS, COMPOSITION AND USE 审中-公开
标题翻译： BRIDGED BICYCLIC RHO激酶抑制剂化合物，组合物和用途
公开(公告)号：WO2011075415A1
公开(公告)日：2011-06-23
申请号：PCT/US2010/059926
申请日：2010-12-10
申请人： INSPIRE PHARMACEUTICALS, INC. , LAMPE, John, W. , WATSON, Paul, S. , SLADE, David, J.
发明人： LAMPE, John, W. , WATSON, Paul, S. , SLADE, David, J.
IPC分类号： A01N43/00 , A61K31/55
CPC分类号： C07D451/04 , A61K31/46 , A61K31/4725 , C07D401/12 , C07D403/12 , C07D413/12 , C07D453/06 , C07D471/08 , C07D487/08
摘要： The present invention is directed to synthetic bridged bicyclic compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. The method comprises administering to a subject a therapeutically effective amount of a Rho kinase inhibitory compound of Formula I, wherein said amount is effective to influence the actomyosin interactions, for example, by leading to cellular relaxation and alterations in cell-substratum adhesions. In one embodiment, the method treats increased intraocular pressure, such as primary open-angle glaucoma. In another embodiment, the method treats diseases or conditions of the lung associated with excessive cell proliferation, remodeling, inflammation, vasoconstriction, bronchoconstriction, airway hyperreactivity and edema.
摘要翻译：本发明涉及作为rho相关蛋白激酶抑制剂的合成桥联双环化合物。本发明还涉及包含这些化合物和药学上可接受的载体的药物组合物。本发明另外涉及预防或治疗与细胞骨架重组相关的疾病或病症的方法。该方法包括向受试者施用治疗有效量的式I的Rho激酶抑制性化合物，其中所述量有效地影响肌动球蛋白相互作用，例如通过导致细胞松弛和细胞 - 基底粘连的改变。在一个实施方案中，该方法治疗增加的眼内压，例如原发性开角型青光眼。在另一个实施方案中，该方法治疗与过度细胞增殖，重塑，炎症，血管收缩，支气管收缩，气道高反应性和水肿相关的肺的疾病或病症。

9. 发明申请

WO2006104897A3 CYTOSKELETAL ACTIVE COMPOUNDS, COMPOSITION AND USE 审中-公开
标题翻译： CYTOSKELETAL活性化合物，组合物和用途
公开(公告)号：WO2006104897A3
公开(公告)日：2007-06-14
申请号：PCT/US2006010817
申请日：2006-03-23
申请人： INSPIRE PHARMACEUTICALS INC , LAMPE JOHN W , PLOURDE ROBERT JR , SHE JIN , VITTITOW JASON L , WATSON PAUL S , CRIMMINS MICHAEL T , SLADE DAVID J
发明人： LAMPE JOHN W , PLOURDE ROBERT JR , SHE JIN , VITTITOW JASON L , WATSON PAUL S , CRIMMINS MICHAEL T , SLADE DAVID J
IPC分类号： C07D493/08 , A61K31/427 , A61P27/02 , C07D417/04 , C07D491/08 , C07D498/08
CPC分类号： C07D491/08 , C07D277/06 , C07D277/14 , C07D277/16 , C07D277/34 , C07D277/56 , C07D417/04 , C07D493/08 , C07D497/18
摘要： The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with actin polymerization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or II, wherein said amount is effective to influence the cytoskeleton, for example by inhibiting actin polymerization.
摘要翻译：本发明涉及与天然的秋水仙素A或梭菌素B相关的合成细胞骨架活性化合物。本发明还涉及包含这些化合物和药学上可接受的载体的药物组合物。本发明另外涉及预防或治疗与肌动蛋白聚合相关的疾病或病症的方法。在本发明的一个实施方案中，该方法治疗增加的眼内压，例如原发性开角型青光眼。该方法包括向受试者施用治疗有效量的式I或II的细胞骨架活性化合物，其中所述量有效影响细胞骨架，例如通过抑制肌动蛋白聚合。

10. 发明申请

WO2006104897A2 CYTOSKELETAL ACTIVE COMPOUNDS, COMPOSITION AND USE 审中-公开
标题翻译： CYTOSKELETAL活性化合物，组合物和用途
公开(公告)号：WO2006104897A2
公开(公告)日：2006-10-05
申请号：PCT/US2006/010817
申请日：2006-03-23
申请人： INSPIRE PHARMACEUTICALS, INC. , LAMPE, John W. , PLOURDE, Robert Jr. , SHE, Jin , VITTITOW, Jason L. , WATSON, Paul S. , CRIMMINS, Michael T. , SLADE, David J.
发明人： LAMPE, John W. , PLOURDE, Robert Jr. , SHE, Jin , VITTITOW, Jason L. , WATSON, Paul S. , CRIMMINS, Michael T. , SLADE, David J.
IPC分类号： C07D493/08 , C07D498/08 , C07D491/08 , C07D417/04
CPC分类号： C07D491/08 , C07D277/06 , C07D277/14 , C07D277/16 , C07D277/34 , C07D277/56 , C07D417/04 , C07D493/08 , C07D497/18
摘要： The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with actin polymerization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or II, wherein said amount is effective to influence the cytoskeleton, for example by inhibiting actin polymerization.
摘要翻译：本发明涉及与天然的秋水仙素A或梭菌素B相关的合成细胞骨架活性化合物。本发明还涉及包含这些化合物和药学上可接受的载体的药物组合物。本发明另外涉及预防或治疗与肌动蛋白聚合相关的疾病或病症的方法。在本发明的一个实施方案中，该方法治疗增加的眼内压，例如原发性开角型青光眼。该方法包括向受试者施用治疗有效量的式I或II的细胞骨架活性化合物，其中所述量有效影响细胞骨架，例如通过抑制肌动蛋白聚合。

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