公开(公告)号：US20070149571A1

公开(公告)日：2007-06-28

申请号：US11704665

申请日：2007-02-09

申请人： Bernd Stein ,  John Westwick ,  Bruce Ennis

发明人： Bernd Stein ,  John Westwick ,  Bruce Ennis

IPC分类号： A61K31/454

CPC分类号： A61K31/704 ,  A61K31/337 ,  A61K31/416 ,  A61K31/4196 ,  A61K31/454 ,  A61K31/4745 ,  A61K31/505 ,  A61K31/513 ,  A61K31/675 ,  A61K33/24 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention relates to methods and compositions designed for the treatment, management or prevention of cancer. The methods of the invention comprise the administration of an effective amount of one or more inhibitors of JNK in combination with the administration of an effective amount of one or more other agents useful for cancer therapy. The invention also provides pharmaceutical compositions comprising one or more inhibitors of JNK in combination with one or more other agents useful for cancer therapy. In particular, the invention is directed to methods of treatment and prevention of cancer by the administration of an effective amount of one or more inhibitors of JNK in combination with standard and experimental chemotherapies, hormonal therapies, bone marrow transplants, stem cell replacement therapies, biological therapies/immunotherapies and/or radiation therapies for treatment or prevention of cancer. Also included are methods of treatment of cancer by the administration of one or more inhibitors of JNK in combination with surgery, alone or in further combination with standard and experimental chemotherapies, hormonal therapies, bone marrow transplants, stem cell replacement therapies, biological therapies/immunotherapies and/or radiation therapies.

摘要翻译： 本发明涉及设计用于治疗，管理或预防癌症的方法和组合物。 本发明的方法包括施用有效量的一种或多种JNK抑制剂与施用有效量的一种或多种其它可用于癌症治疗的试剂的组合。 本发明还提供包含一种或多种JNK抑制剂与一种或多种其它可用于癌症治疗的试剂组合的药物组合物。 特别地，本发明涉及通过给予有效量的一种或多种JNK抑制剂与标准和实验化学疗法，激素疗法，骨髓移植物，干细胞替代疗法，生物学方法，治疗和预防癌症的方法 用于治疗或预防癌症的治疗/免疫治疗和/或放射疗法。 还包括通过单独或与标准和实验化疗，激素治疗，骨髓移植，干细胞替代疗法，生物疗法/免疫疗法单独或进一步组合的一种或多种JNK抑制剂的给药来治疗癌症的方法 和/或放射疗法。

公开(公告)号：US07148252B2

公开(公告)日：2006-12-12

申请号：US10261198

申请日：2002-09-30

申请人： Jerome B. Zeldis

发明人： Jerome B. Zeldis

IPC分类号： A61K31/35 ,  A61P35/04

CPC分类号： A61K31/5377 ,  A61K31/37 ,  A61K31/4025 ,  A61K31/4178 ,  A61K31/4433

摘要： This invention relates to methods for using benzopyranones, or their pharmaceutically acceptable salts, for treating or preventing a primary brain cancer or a brain metastasis. The benzopyranones have the formula: wherein R1, R2, R3, n and p are as defined herein.

摘要翻译： 本发明涉及使用苯并吡喃酮或其药学上可接受的盐治疗或预防原发性脑癌或脑转移的方法。 苯并吡喃酮具有下式：其中R 1，R 2，R 3，n和p如本文所定义。

公开(公告)号：US07129242B2

公开(公告)日：2006-10-31

申请号：US10004645

申请日：2001-12-04

申请人： Yoshitaka Satoh ,  Shripad S. Bhagwat

发明人： Yoshitaka Satoh ,  Shripad S. Bhagwat

IPC分类号： A61K31/50 ,  A61K31/497

CPC分类号： C07D239/42 ,  A61K31/496 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D487/08 ,  C07D491/10 ,  A61K2300/00

摘要： Compounds having activity as inhibitors of the JNK pathway are disclosed. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R1 through R6 are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to inhibition of the JNK pathway. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.

摘要翻译： 公开了具有JNK途径抑制剂活性的化合物。 本发明的化合物是具有以下结构的苯胺基嘧啶衍生物：其中R 1至R 6如本文所定义。 这些化合物可用于治疗对抑制JNK通路有反应的广泛的条件。 因此，还公开了治疗这些病症的方法，以及含有一种或多种上述化合物的化合物的药物组合物。

公开(公告)号：US07037936B2

公开(公告)日：2006-05-02

申请号：US10463009

申请日：2003-06-16

申请人： Jeffrey McKenna ,  Frank Mercurio ,  Veronique Plantevin ,  Weilin Xie ,  Michele Pagano

发明人： Jeffrey McKenna ,  Frank Mercurio ,  Veronique Plantevin ,  Weilin Xie ,  Michele Pagano

IPC分类号： A61K31/35

CPC分类号： A61K31/351 ,  A61K31/135 ,  A61K31/4025

摘要： The present invention generally relates to compounds and compositions useful for the modulation of ligase activity. The invention further relates to Compounds of the Invention, compositions thereof, and methods for treating or preventing cancer, a neoplastic disorder, acute or chronic renal failure, an inflammatory disorder, an immune disorder, a cardiovascular disease, an effect of aging or an infectious disease comprising administering an effective amount of a Compound of the Invention. The invention further relates to the use of a Compound of the Invention as a preservative of a cell, blood, tissue or an organ or as an agent to modulate stem cells.

摘要翻译： 本发明一般涉及可用于调节连接酶活性的化合物和组合物。 本发明还涉及本发明的化合物，其组合物，以及用于治疗或预防癌症，肿瘤性疾病，急性或慢性肾功能衰竭，炎症性疾病，免疫疾病，心血管疾病，衰老或感染性的影响的方法 疾病，包括施用有效量的本发明化合物。 本发明还涉及本发明的化合物作为细胞，血液，组织或器官的防腐剂或作为调节干细胞的药剂的用途。

公开(公告)号：US11492332B2

公开(公告)日：2022-11-08

申请号：US17195814

申请日：2021-03-09

申请人： Signal Pharmaceuticals, LLC

发明人： Hon-Wah Man ,  Mohit Atul Kothare

IPC分类号： C07D239/48 ,  C07B59/00

摘要： Provided herein are isotopologues of Compound A, which are enriched with isotopes such as, for example, deuterium. Pharmaceutical compositions comprising the isotope-enriched compounds, and methods of using such compounds are also provided.

公开(公告)号：US20220273650A1

公开(公告)日：2022-09-01

申请号：US17496433

申请日：2021-10-07

申请人： Signal Pharmaceuticals, LLC

发明人： Shuichan XU ,  Kristen Mae HEGE ,  Antonia LOPEZ-GIRONA ,  Heather RAYMON ,  Rama K. NARLA ,  Rajesh CHOPRA

IPC分类号： A61K31/4985 ,  C07D471/04 ,  C07D473/00 ,  C07D498/04 ,  A61K31/4166 ,  A61K31/4188 ,  A61P35/00 ,  C07D487/04

摘要： Provided herein are methods for treating or preventing a solid tumor, non-Hodgkin lymphoma or multiple myeloma in a patient, comprising administering an effective amount of a TOR kinase inhibitor to a patient having a solid tumor, non-Hodgkin lymphoma or multiple myeloma.

公开(公告)号：US20210221772A1

公开(公告)日：2021-07-22

申请号：US17195814

申请日：2021-03-09

申请人： Signal Pharmaceuticals, LLC

发明人： Hon-Wah MAN ,  Mohit Atul KOTHARE

IPC分类号： C07D239/48 ,  C07B59/00

摘要： Provided herein are isotopologues of Compound A, which are enriched with isotopes such as, for example, deuterium. Pharmaceutical compositions comprising the isotope-enriched compounds, and methods of using such compounds are also provided.

公开(公告)号：US10940152B2

公开(公告)日：2021-03-09

申请号：US16846503

申请日：2020-04-13

申请人： Signal Pharmaceuticals, LLC

发明人： Matthew Alexander ,  Sogole Bahmanyar ,  John Frederick Boylan ,  Joshua Hansen ,  Dehua Huang ,  Robert Hubbard ,  Brandon Jeffy ,  Jim Leisten ,  Mehran Moghaddam ,  Raj K. Raheja ,  Heather Raymon ,  Kimberly Schwarz ,  Marianne Sloss ,  Eduardo Torres ,  Tam Minh Tran ,  Shuichan Xu ,  JingJing Zhao

IPC分类号： A61K31/52 ,  C07D473/32 ,  A61P35/00 ,  A61K31/5377

摘要： Provided herein are Aminopurine Compounds having the following structures: wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.

公开(公告)号：US10683298B2

公开(公告)日：2020-06-16

申请号：US16186883

申请日：2018-11-12

申请人： SIGNAL PHARMACEUTICALS, LLC

发明人： Jan Elsner ,  Roy L. Harris ,  Branden Gingsee Lee ,  Deborah Mortensen ,  Garrick K. Packard ,  Patrick Papa ,  Jason Parnes ,  Sophie Perrin-Ninkovic ,  Jennifer Riggs ,  John Sapienza ,  Graziella I. Shevlin ,  Lida Tehrani ,  Jingjing Zhao

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

摘要： Provided herein are Heteroaryl Compounds having the following structure: 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. Further provided herein are methods for the preparation of substituted pyrazino[2,3-b]pyrazines of formula (II): the method comprising contacting a compound of formula (VI): the method further comprising cyclizing a compound of formula (VII) in a second solvent, in the presence of a second base, or an acid, wherein said cyclization occurs under conditions suitable to provide a compound of formula (VI), with R1-Y in a solvent, in the presence of a palladium catalyst, wherein said contacting occurs in the presence of a base, wherein R1-R3, Y, the palladium catalyst and the base are as defined herein.

公开(公告)号：US10052322B2

公开(公告)日：2018-08-21

申请号：US15790177

申请日：2017-10-23

申请人： SIGNAL PHARMACEUTICALS, LLC

发明人： Anil Menon ,  Darshan K. Parikh ,  Dora Visky ,  Nathan Boersen ,  Thomas Lee ,  Xiaozhang Liang

IPC分类号： A61K31/4985 ,  A61K9/48 ,  A61K9/20 ,  C07D471/04 ,  C07D487/04

CPC分类号： A61K31/4985 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/4858 ,  A61P35/00 ,  C07D471/04 ,  C07D487/04

摘要： Provided herein are formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one.