公开(公告)号：EP1692128A1

公开(公告)日：2006-08-23

申请号：EP04811774.1

申请日：2004-11-19

申请人： Signal Pharmaceuticals LLC

发明人： BHAGWAT, Shripad, S. ,  SATOH, Yoshitaka ,  SAKATA, Steven, T. ,  BUHR, Chris, A. ,  ALBERS, Ronald ,  SAPIENZA, John ,  PLANTEVIN, Veronique ,  CHAO, Qi ,  SAHASRABUDHE, Kiran ,  FERRY, Rachel ,  NARLA, Rama, K.

IPC分类号： C07D403/04 ,  C07D401/14 ,  C07D403/14 ,  C07D403/12 ,  A61K31/416 ,  A61K31/4196

CPC分类号： C07D403/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14

摘要： This invention is directed to Indazole Compounds or pharmaceutically acceptable salts, solvates and hydrates thereof. The Indazole Compounds have utility in the treatment or prevention of a wide range of diseases and disorders that are responsive to the inhibition, modulation or regulation of kinases, such as inflammatory diseases, abnormal angiogenesis and diseases related thereto, cancer, atherosclerosis, a cardiovascular disease, a renal disease, an autoimmune condition, macular degeneration, disease-related wasting, an asbestos-related condition, pulmonary hypertension, diabetes, obesity, pain and others. Thus, methods of treating or preventing such diseases and disorders are also disclosed, as are pharmaceutical compositions comprising one or more of the Indazole Compounds. This invention is based, in part, upon the discovery of a novel class of 5-triazolyl substituted indazole molecules that have potent activity with respect to the modulation of protein kinases. Thus, the invention encompasses orally active molecules as well as parenterally active molecules which can be used at lower doses or serum concentrations for treating diseses or disorders associated with protein kinase signal transduction.

公开(公告)号：EP3736268A1

公开(公告)日：2020-11-11

申请号：EP20178220.8

申请日：2014-12-19

申请人： Signal Pharmaceuticals, LLC

发明人： CASHION, Daniel Kurt ,  MORTENSEN, Deborah ,  HUANG, Dehua ,  TORRES, Eduardo ,  PARNES, Jason ,  SAPIENZA, John ,  HANSEN, Joshua ,  LEFTHERIS, Katerina ,  CORREA, Matthew ,  DELGADO, Maria Mercedes ,  RAHEJA, Raj ,  PAPA, Patrick ,  BAHMANYAR, Sogole ,  HEGDE, Sayee ,  NORRIS, Stephen Tyson ,  PLANTEVIN-KRENITSKY, Veronique ,  CALABRESE, Andrew Antony ,  CATHERS, Brian Edwin ,  WHITEFIELD, Brandon Wade ,  BENNETT, Brydon

IPC分类号： C07D239/48 ,  C07D403/06 ,  A61K31/506 ,  A61P3/00 ,  A61P11/00 ,  A61P11/06 ,  A61P17/00 ,  A61P19/00 ,  A61P21/00 ,  A61P37/06 ,  C07D405/14 ,  A61K31/505 ,  A61K31/5377 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04

摘要： The invention provides a method for preparing a compound of formula (I):

comprising contacting a compound of formula (Ia)

or a compound of formula (Ic)

with R 1 -L-NH 2 , in an organic solvent, in the presence of a base, under conditions as defined herein. Also provided are reaction intermediates involved in said method as defined herein.

公开(公告)号：EP3660020A1

公开(公告)日：2020-06-03

申请号：EP20152165.5

申请日：2009-10-27

申请人： Signal Pharmaceuticals, LLC

发明人： PERRIN-NINKOVIC, Sophie ,  HARRIS, Roy L. ,  SAPIENZA, John ,  SHEVLIN, Graziella I. ,  PAPA, Patrick ,  LEE, Branden ,  PACKARD, Garrick ,  ZHAO, Jingjing ,  RIGGS, Jennifer ,  PARNES, Jason ,  MORTENSEN, Deborah ,  ELSNER, Jan

IPC分类号： C07D487/04

摘要： Provided herein is a method for preparing a compound of formula (II):

wherein the method comprising contacting a compound of formula (VI):

with R 1 -Y in a solvent, in the presence of a palladium catalyst, wherein said contacting occurs in the presence of a base, wherein R 1 , R 2 , R 3 and Y are as defined herein.

公开(公告)号：EP3103803A1

公开(公告)日：2016-12-14

申请号：EP16171709.5

申请日：2009-10-27

申请人： Signal Pharmaceuticals, LLC

发明人： PERRIN-NINKOVIC, Sophie ,  HARRIS, Roy L. ,  SAPIENZA, John ,  SHEVLIN, Graziella I. ,  PAPA, Patrick ,  LEE, Branden ,  PACKARD, Garrick

IPC分类号： C07D487/04 ,  C07F5/05 ,  C07F7/22 ,  C07D241/20

摘要： Provided herein is a compound having the formula:

or a salt, tautomer or stereoisomer thereof, wherein X is halogen, B(OR + ) 2 or Sn(R ++ ) 3 ; R 2 and R 3 are as defined herein. This compound is used as interemdiate in the snythesis of mTOR kinase inhibitors. Also provided are reaction intermediates for preparing said compound.

摘要翻译： 本文提供具有下式的化合物或其盐，互变异构体或立体异构体，其中X为卤素，B（OR +）2或Sn（R + +）3; R 2和R 3如本文所定义。 该化合物在mTOR激酶抑制剂的使用中被用作互连。 还提供了用于制备所述化合物的反应中间体。

公开(公告)号：EP3082819A1

公开(公告)日：2016-10-26

申请号：EP14871136.9

申请日：2014-12-19

申请人： Signal Pharmaceuticals, LLC

发明人： CASHION, Daniel ,  MORTENSEN, Deborah ,  HUANG, Dehua ,  TORRES, Eduardo ,  PARNES, Jason ,  SAPIENZA, John ,  HANSEN, Joshua ,  LEFTHERIS, Katerina ,  CORREA, Matthew ,  DELGADO, Maria, Mercedes ,  RAHEJA, Raj ,  PAPA, Patrick ,  BAHMANYAR, Sogole ,  HEGDE, Sayee ,  NORRIS, Stephen Tyson ,  PLANTEVIN-KRENITSKY, Veronique ,  CALABRESE, Andrew, Antony ,  CATHERS, Brian, Edwin ,  WHITEFIELD, Brandon, Wade ,  BENNETT, Brydon

IPC分类号： A61K31/506 ,  C07D239/48

CPC分类号： C07D239/48 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04

摘要： Provided herein are diaminopyrimidyl Compounds having the following structures: wherein X, L, R1, and R2 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidyl Compound, and methods for treating or preventing PKC-theta-mediated disorders, or a condition treatable or preventable by inhibition of a kinase, for example, PKC-theta.

摘要翻译： 本文提供具有以下结构的二氨基嘧啶化合物：其中X，L，R 1和R 2如本文所定义，包含有效量的二氨基嘧啶基化合物的组合物，以及治疗或预防PKC-θ介导的病症的方法或病症 可通过抑制激酶例如PKC-θ治疗或预防。

公开(公告)号：EP2344494B1

公开(公告)日：2016-04-20

申请号：EP09789271.5

申请日：2009-09-08

申请人： Signal Pharmaceuticals, LLC

发明人： BAHMANYAR, Sogole ,  BATES, R.J. ,  BLEASE, Kate ,  CALABRESE, Andrew, Antony ,  DANIEL, Thomas, Oran ,  DELGADO, Mercedes ,  ELSNER, Jan ,  ERDMAN, Paul ,  FAHR, Bruce ,  FERGUSON, Gregory ,  LEE, Branden ,  NADOLNY, Lisa ,  PACKARD, Garrick ,  PAPA, Patrick ,  PLANTEVIN-KRENITSKY, Veronique ,  RIGGS, Jennifer ,  ROHANE, Patricia ,  SANKAR, Sabita ,  SAPIENZA, John ,  SATOH, Yoshitaka ,  SLOAN, Victor ,  STEVENS, Randall ,  TEHRANI, Lida ,  TIKHE, Jayashree ,  TORRES, Eduardo ,  WALLACE, Andrew ,  WHITEFIELD, Brandon, Wade ,  ZHAO, Jingjing

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P35/00 ,  A61P5/00 ,  A61P25/00 ,  A61P9/00 ,  A61P19/00 ,  A61P29/00

CPC分类号： C07D471/04 ,  C07D519/00

公开(公告)号：EP2493472A1

公开(公告)日：2012-09-05

申请号：EP10827343.4

申请日：2010-10-22

申请人： Signal Pharmaceuticals, LLC

发明人： HARRIS, Roy, L. ,  SAPIENZA, John ,  SHEVLIN, Graziella ,  PAPA, Patrick ,  LEE, Branden, Gingsee ,  PACKARD, Garrick ,  ZHAO, Jingjing ,  JOKIEL, Patrick, Anthony ,  MORTENSEN, Deborah ,  RIGGS, Jennifer ,  GAMBOA, Juan, Antonio ,  BEAUCHAMPS, Marie, Georges ,  KREILEIN, Matthew, Michael ,  KOTHARE, Mohit, Atul ,  PERRIN-NINKOVIC, Sophie ,  PYE, Philip ,  LEONG, William, Wei-Hwa ,  ELSNER, Jan ,  CHOUDHURY, Anusuya

IPC分类号： A61K31/497

CPC分类号： C07D471/04 ,  C07D241/20 ,  C07D487/04 ,  C07D498/14 ,  C07D519/00

摘要： Provided herein are methods to prepare Heteroaryl Compounds having the following structure: Forumula (I) or Formula (II): wherein R
1 -R
4 are as defined herein. The Heteroaryl compounds are useful for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions.

公开(公告)号：EP2344494A1

公开(公告)日：2011-07-20

申请号：EP09789271.5

申请日：2009-09-08

申请人： Signal Pharmaceuticals, LLC

发明人： BAHMANYAR, Sogole ,  BATES, R.J. ,  BLEASE, Kate ,  CALABRESE, Andrew, Antony ,  DANIEL, Thomas, Oran ,  DELGADO, Mercedes ,  ELSNER, Jan ,  ERDMAN, Paul ,  FAHR, Bruce ,  FERGUSON, Gregory ,  LEE, Branden ,  NADOLNY, Lisa ,  PACKARD, Garrick ,  PAPA, Patrick ,  PLANTEVIN-KRENITSKY, Veronique ,  RIGGS, Jennifer ,  ROHANE, Patricia ,  SANKAR, Sabita ,  SAPIENZA, John ,  SATOH, Yoshitaka ,  SLOAN, Victor ,  STEVENS, Randall ,  TEHRANI, Lida ,  TIKHE, Jayashree ,  TORRES, Eduardo ,  WALLACE, Andrew ,  WHITEFIELD, Brandon, Wade ,  ZHAO, Jingjing

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P35/00 ,  A61P5/00 ,  A61P25/00 ,  A61P9/00 ,  A61P19/00 ,  A61P29/00

CPC分类号： C07D471/04 ,  C07D519/00

摘要： Provided herein are Heteroaryl Compounds of formula (I): wherein R
1 and R
2 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing inflammatory conditions or cancer, and conditions treatable or preventable by inhibition of a kinase or a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a subject in need thereof.

公开(公告)号：EP3103803B1

公开(公告)日：2020-03-11

申请号：EP16171709.5

申请日：2009-10-27

申请人： Signal Pharmaceuticals, LLC

发明人： PERRIN-NINKOVIC, Sophie ,  HARRIS, Roy L. ,  SAPIENZA, John ,  SHEVLIN, Graziella I. ,  PAPA, Patrick ,  LEE, Branden ,  PACKARD, Garrick ,  ZHAO, Jingjing ,  RIGGS, Jennifer ,  PARNES, Jason ,  MORTENSEN, Deborah ,  ELSNER, Jan

IPC分类号： C07D487/04 ,  C07F5/05 ,  C07F7/22

公开(公告)号：EP2358718A1

公开(公告)日：2011-08-24

申请号：EP09759827.0

申请日：2009-10-27

申请人： Signal Pharmaceuticals, LLC

发明人： ELSNER, Jan ,  HARRIS, Roy, L. ,  LEE, Branden ,  MORTENSEN, Deborah ,  PACKARD, Garrick ,  PAPA, Patrick ,  PERRIN-NINKOVIC, Sophie ,  RIGGS, Jennifer ,  SANKAR, Sabita ,  SAPIENZA, John ,  SHEVLIN, Graziella ,  TEHRANI, Lida ,  XU, Weiming ,  ZHAO, Jingjing ,  PARNES, Jason ,  MADAKAMUTIL Loui ,  FULTZ Kimberly ,  NARLA, Rama K.

IPC分类号： C07D487/04 ,  A61K31/4985 ,  A61P35/00

CPC分类号： C07D487/04 ,  C07D241/20 ,  C07D471/04 ,  C07D471/14 ,  C07D487/10 ,  C07D487/14 ,  C07D498/14

摘要： Provided herein are Heteroaryl Compounds having the following structure: R2 N (I) or (II) wherein R1 -R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.

摘要翻译： 提供在杂芳基是具有下列结构的化合物：worin R 1〜R 3的定义相同，有效量的杂芳基化合物和杂芳基化合物中的内容提供了一种用于使用在治疗或预防癌症，炎性病症的方法的组合物，包含， 免疫病症，神经退行性疾病，糖尿病，肥胖病，神经系统疾病，老年性疾病，或心血管疾病。