公开(公告)号：US09725450B2

公开(公告)日：2017-08-08

申请号：US14918655

申请日：2015-10-21

申请人： Signal Pharmaceuticals, LLC

发明人： Steven Clareen ,  Veronique Plantevin-Krenitsky ,  Moorthy Palanki ,  Yoshitaka Satoh

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

CPC分类号： C07D473/32 ,  A61K31/52

摘要： Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.

公开(公告)号：US09593120B2

公开(公告)日：2017-03-14

申请号：US14385329

申请日：2013-03-15

申请人： ALGENIS SPA

发明人： Max Rutman ,  Jean-Jacques Pilorget ,  Jimmy Stehberg ,  Wolfgang Vanscheidt ,  Constanza Sigala

IPC分类号： A01N43/54 ,  A61K31/505 ,  C07D237/36 ,  C07D473/32 ,  A61K31/519 ,  A61K31/4741 ,  A61K31/4748 ,  A61K9/00 ,  A61K47/12 ,  A61K47/14 ,  A61K47/18 ,  A61K9/06 ,  A61K47/32 ,  A61K47/44 ,  A61K31/52 ,  A61K45/06

CPC分类号： C07D473/32 ,  A61K9/0009 ,  A61K9/0014 ,  A61K9/06 ,  A61K31/4741 ,  A61K31/4748 ,  A61K31/519 ,  A61K31/52 ,  A61K45/06 ,  A61K47/12 ,  A61K47/14 ,  A61K47/186 ,  A61K47/32 ,  A61K47/44

摘要： The invention concerns a paralytic shellfish poison for the treatment of itching in a human being or another mammal.

摘要翻译： 本发明涉及用于治疗人或其他哺乳动物的瘙痒的麻痹贝类毒物。

公开(公告)号：US20160129122A1

公开(公告)日：2016-05-12

申请号：US14996669

申请日：2016-01-15

申请人： Catabasis Pharmaceuticals, Inc.

发明人： Jill C. Milne ,  Michael R. Jirousek ,  Chi B. Vu ,  Allison Wensley ,  Amal Ting

IPC分类号： A61K47/48 ,  A61K31/685 ,  C07C233/52 ,  A61K31/215 ,  C07C237/24 ,  A61K31/16 ,  A61K31/197 ,  C07D309/28 ,  A61K31/351 ,  C07D473/30 ,  A61K31/522 ,  C07D405/04 ,  A61K31/655 ,  C07D411/04 ,  C07D473/32 ,  C07D471/04 ,  A61K31/4745 ,  C07D493/04 ,  A61K31/34 ,  C07H19/10 ,  A61K31/7072 ,  C07F9/6558

CPC分类号： A61K31/7072 ,  A61K31/16 ,  A61K31/197 ,  A61K31/215 ,  A61K31/34 ,  A61K31/351 ,  A61K31/4745 ,  A61K31/522 ,  A61K31/655 ,  A61K31/685 ,  A61K47/54 ,  A61K47/542 ,  C07C233/52 ,  C07C237/24 ,  C07D309/28 ,  C07D405/04 ,  C07D411/04 ,  C07D471/04 ,  C07D473/30 ,  C07D473/32 ,  C07D487/04 ,  C07D493/04 ,  C07F9/65586 ,  C07H19/10

摘要： The invention relates to fatty acid antiviral conjugates; compositions comprising an effective amount of a fatty acid antiviral conjugate; and methods for treating or preventing a viral infection comprising the administration of an effective amount of a fatty acid antiviral conjugate.

公开(公告)号：US09181221B2

公开(公告)日：2015-11-10

申请号：US14085660

申请日：2013-11-20

申请人： Infinity Pharmaceuticals, Inc.

发明人： Pingda Ren ,  Yi Liu ,  Liansheng Li ,  Katrina Chan ,  Alfredo C. Castro ,  Catherine A. Evans

IPC分类号： A01N43/90 ,  A61K31/52 ,  C07D401/14 ,  A61K31/47 ,  C07D473/16 ,  C07D473/32 ,  C07D487/04

CPC分类号： C07D473/34 ,  A61K31/47 ,  A61K31/52 ,  C07D401/14 ,  C07D473/16 ,  C07D473/32 ,  C07D487/04 ,  Y02A50/414 ,  Y02A50/463

摘要： Substituted isoquinolinone compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.

摘要翻译： 本文描述了取代的异喹啉酮化合物和调节激酶活性（包括PI3激酶活性）的药物组合物，以及化合物，药物组合物和治疗与激酶活性（包括PI3激酶活性）相关的疾病和病症的方法。

公开(公告)号：US09138437B2

公开(公告)日：2015-09-22

申请号：US14271486

申请日：2014-05-07

申请人： VERASTEM, INC.

发明人： DiZhong Chen ,  Meredith Williams

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

CPC分类号： C07D473/32 ,  A61K31/5377 ,  C07D487/04 ,  C12N9/12 ,  C12N9/1205 ,  C12Y207/01137 ,  C12Y207/11001 ,  Y02A50/401 ,  Y02A50/414

摘要： The present invention relates to a purine compound useful as a kinase inhibitor. The compound has the structure: or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及可用作激酶抑制剂的嘌呤化合物。 该化合物具有以下结构：或其药学上可接受的盐。

公开(公告)号：US09096600B2

公开(公告)日：2015-08-04

申请号：US13329532

申请日：2011-12-19

申请人： Yun-Long Li ,  Andrew P. Combs ,  Eddy W. Yue ,  Thomas P. Maduskuie, Jr. ,  Richard B. Sparks

发明人： Yun-Long Li ,  Andrew P. Combs ,  Eddy W. Yue ,  Thomas P. Maduskuie, Jr. ,  Richard B. Sparks

IPC分类号： C07D473/34 ,  C07D473/32

CPC分类号： C07D473/34 ,  A61K31/52 ,  A61K31/5377 ,  A61K45/06 ,  C07D473/32

摘要： The present invention provides N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines derivatives that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.

摘要翻译： 本发明提供了调节磷酸肌醇3-激酶（PI3K）活性的N-（1-（取代苯基）乙基）-9H-嘌呤-6-胺衍生物，可用于治疗与 PI3Ks包括例如炎症性疾病，基于免疫的疾病，癌症和其它疾病。

公开(公告)号：US20150038494A1

公开(公告)日：2015-02-05

申请号：US14518480

申请日：2014-10-20

申请人： Piet Herdewijn ,  Steven De Jonghe ,  Ling-Jie Gao ,  Mi-Yeon Jang ,  Bart Vanderhoydonck ,  Mark Jozef Albert Waer ,  Yuan Lin ,  Jean Ferdinand Herman ,  Thierry Andre Michel Louat

发明人： Piet Herdewijn ,  Steven De Jonghe ,  Ling-Jie Gao ,  Mi-Yeon Jang ,  Bart Vanderhoydonck ,  Mark Jozef Albert Waer ,  Yuan Lin ,  Jean Ferdinand Herman ,  Thierry Andre Michel Louat

IPC分类号： C07D473/32 ,  A61K31/5513 ,  C07D473/18 ,  A61K31/5377 ,  A61K31/517 ,  A61K45/06

CPC分类号： C07D473/32 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5513 ,  A61K45/06 ,  C07D473/18 ,  C07D513/04

摘要： The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1. The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections.

摘要翻译： 本发明涉及式I，II，III或IV化合物和/或其药学上可接受的加成盐和/或其立体异构体和/或其溶剂合物，其中R1，R2，R3，R4，R5， R6，R7，R8，R9，R11和R12如权利要求1中所定义。本发明还涉及其制备方法及其药物组合物。 本发明还涉及所述化合物作为生物活性成分的用途，更具体地说，作为用于治疗疾病和病理状况的药物，例如但不限于免疫和自身免疫病症，器官和细胞移植排斥。

公开(公告)号：US08946282B2

公开(公告)日：2015-02-03

申请号：US13855916

申请日：2013-04-03

申请人： Annji Pharmaceutical Co., Ltd.

发明人： Ji-Wang Chern ,  Ajit Dhananjay Jagtap ,  Hsiao-Chun Wang ,  Grace Shiahuy Chen

IPC分类号： C07D209/34 ,  C07D403/06 ,  C07D401/06 ,  A61K38/45 ,  C07D401/14 ,  C07D409/06 ,  C07D405/06 ,  C07D403/14 ,  A61K31/522 ,  C07D473/32 ,  C07D209/00

CPC分类号： C07D209/34 ,  A61K31/522 ,  A61K38/45 ,  C07D209/00 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/06 ,  C07D409/06 ,  C07D473/32

摘要： A novel class of indoline-2-one derivatives are disclosed. These compounds are protein kinase inhibitors which are useful for treating hyperproliferative diseases such as cancer. In one aspect, the invention relates to a compound a compound of Formula A: or a pharmaceutically acceptable salt thereof, wherein: Ra is hydrogen, (C6-C18)aryl, halo(C6-C18)aryl, or (C1-C6)alkoxy(C6-C18)aryl; Rb is hydrogen, (C3-C18)heteroaryl, (C1-C6)alkoxy(C3-C18)heteroaryl; (C1-C6)alkyl(C3-C18)heteroaryl, (C1-C6)alkyl(C1-C6)alkoxy(C3-C18)heteroaryl, (C1-C6)alkyl(C1-C6)carboxyalkyl(C3-C18)heteroaryl; (C1-C6)alkyl(C1-C6)alkylamino(C1-C6)alkylcarbamoyl)(C3-C18)heteroaryl, (C1-C6)alkyl(C1-C18)aryl(C3-C18)heteroaryl, (C1-C6)alkyl(C1-C6)alkoxycarbonyl)(C3-C18)heteroaryl, (C1-C6)alkyl(C1-C6)alkoxy(C1-C6)oxyalkyl(C3-C18)heteroaryl, (C1-C6)alkyl(C3-C6)heterocyclylcarbonyl(C3-C18)heteroaryl, (C1-C6)alkyl(C3-C6)heterocyclyl(C1-C6)oxyalkyl(C3-C18)heteroaryl, or (C1-C6)alkyl((C3-C6)heterocyclyl(C1-C6)alkylcarbamoyl)(C3-C18)heteroaryl; Rc is hydrogen, (C1-C6)alkoxybenzoylureido, or halo(C6-C18)aryl(C3-C18)heteroarylamido; Rd is hydrogen, halogen, (C1-C6)alkoxybenzoylureido, or halo(C6-C18)aryl(C3-C18)heteroarylamido; Re is-hydrogen, benzoylureido, halobenzoylureido, halo(C1-C6)alkoxybenzoylureido, (C1-C6)alkoxybenzoylureido, (C1-C6)alkylaminobenzoylureido, (C1-C6)alkylbenzoylureido, nitrobenzoylureido, (C1-C6)haloalkylbenzoylureido, (C1-C6)haloalkylhalobenzoylureido, halo(C6-C18)arylcarbomylacetamido, (C1-C6)alkoxy(C6-C18)arylcarbomylacetamido, (C1-C6)alkoxy(C6-C18)arylcarbamoyl(C3-C6)cycloalkylamido, halo(C6-C18)aryl(C3-C18)heteroarylcarbonylamino, (C3-C6)cycloalkyl(C3-C18)heteroarylcarbonylamino, (C1-C6)alkylamino(C6-C18)aryl(C3-C18)heteroarylcarbonylamino, halo(C1-C6)alkoxy(C6-C18)aryl(C3-C18) heteroarylcarbonylamino, (C1-C6)alkoxy(C6-C18)aryl(C3-C18)heteroarylcarbonylamino, (C1-C6)alkyl(C3-C18)heteroarylcarbonylamino, aryl(C3-C18)heteroarylcarbonylamino, (C1-C6)haloalkylhalo(C6-C18)aryl(C3-C6)heterocyclylcarbonylamino, (C1-C6)haloalkyl(C6-C18)aryl(C3-C18)heteroarylcarbonylamino, halo(C6-C18)aryl(C3-C18)heteroarylamido, (C1-C6)oxyalkyl(C3-C6)heterocyclylamido, (C1-C6)alkoxy(C1-C6)alkyl(C3-C18)heteroarylamido, (C6-C18)aryl(C3-C18)heteroarylamido, (C1-C6)alkyl(C1-C18)aryl(C3-C18)heteroarylamido, (C1-C6)haloalkyl(C6-C18)aryl(C3-C18)heteroarylamido, (C1-C6)alkyl(C3-C18)heteroarylamido, or (C1-C6)alkoxy(C6-C18)aryl(C3-C18)heteroarylamido; and Rf is hydrogen, (C1-C6)alkoxybenzoylureido, or halo(C6-C18)aryl(C3-C18)heteroarylamido.

公开(公告)号：US20150011545A1

公开(公告)日：2015-01-08

申请号：US14331302

申请日：2014-07-15

申请人： AstraZeneca AB

发明人： Audrey DAVIES ,  Stephanos IOANNIDIS ,  Michelle Laurae LAMB ,  Mei SU ,  Tao WANG ,  Hai-Jun ZHANG

IPC分类号： C07D471/04 ,  C07D473/18 ,  C07D473/16 ,  C07D473/32

CPC分类号： C07D471/04 ,  C07D471/22 ,  C07D473/16 ,  C07D473/18 ,  C07D473/32 ,  C07D491/22 ,  C07D498/22

摘要： The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer.

摘要翻译： 本发明涉及式（I）化合物及其药物组合物及其使用方法。 这些化合物提供骨髓增生性疾病和癌症的治疗。

公开(公告)号：US08759360B2

公开(公告)日：2014-06-24

申请号：US13072843

申请日：2011-03-28

申请人： Adam Jan Sanderson ,  Peter Charles Astles ,  Rossella Guidetti ,  Sean Patrick Hollinshead

发明人： Adam Jan Sanderson ,  Peter Charles Astles ,  Rossella Guidetti ,  Sean Patrick Hollinshead

IPC分类号： A61K31/52 ,  C07D473/32

CPC分类号： C07D487/04

摘要： A compound of the formula: and pharmaceutical compositions for the treatment or prevention of pain.

摘要翻译： 一种下式的化合物：用于治疗或预防疼痛的药物组合物。