专利检索 ap:"Travis Matthew STAMS" 第 1 页

1.

发明授权
1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and compositions thereof for inhibiting the activity of SHP2 有权

公开(公告)号：US10093646B2

公开(公告)日：2018-10-09

申请号：US15110498

申请日：2015-01-16

申请人： Christine Hiu-Tung Chen , Zhuoliang Chen , Jorge Garcia Fortanet , Denise Grunenfelder , Rajesh Karki , Mitsunori Kato , Matthew J. LaMarche , Lawrence Blas Perez , Travis Matthew Stams , Sarah Williams

发明人： Christine Hiu-Tung Chen , Zhuoliang Chen , Jorge Garcia Fortanet , Denise Grunenfelder , Rajesh Karki , Mitsunori Kato , Matthew J. LaMarche , Lawrence Blas Perez , Travis Matthew Stams , Sarah Williams

IPC分类号： C07D401/04 , C07D409/14 , C07D471/04 , C07D403/04 , C07D401/14 , C07D487/04

摘要： The present invention relates to compounds of formula I: in which m, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a and R5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

2.

发明申请
5-Substituted 1,1-Dioxo- 1,2,5- Thiadiazolidin-3-One Derivatives 审中-公开
标题翻译： 5-取代的1,1-二氧-1,2,5-噻二唑烷-3-酮衍生物

公开(公告)号：US20080139576A1

公开(公告)日：2008-06-12

申请号：US11860034

申请日：2007-09-24

申请人： Gary Mark Coppola , John William Davies , Charles Francis Jewell , Yu-Chin Li , James Richard Wareing , Donald Mark Sperbeck , Travis Matthew Stams , Sidney Wolf Topiol , Isidoros Vlattas

发明人： Gary Mark Coppola , John William Davies , Charles Francis Jewell , Yu-Chin Li , James Richard Wareing , Donald Mark Sperbeck , Travis Matthew Stams , Sidney Wolf Topiol , Isidoros Vlattas

IPC分类号： A61K31/497 , C07D285/10 , C07D403/02 , A61K31/47 , A61P3/00 , C07D215/00 , A61K31/41

CPC分类号： C07D285/10 , C07D417/06 , C07D417/10 , C07K5/06078

摘要： Compounds of the formula provide pharmacological agents which are inhibitors of PTPases, in particular, the compounds of formula I inhibit PTP-1B and TC PTP, and thus may be employed for the treatment of conditions associated with PTPase activity. The compounds of the present invention may also be employed for inhibition of other enzymes with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula I may be employed for prevention or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels. The compounds of the present invention may also be employed in the treatment, prevention or control of a number of conditions that accompany Type 2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.

摘要翻译： 式的化合物提供作为PTPase抑制剂的药理学试剂，特别是式I化合物抑制PTP-1B和TC PTP，因此可用于治疗与PTPase活性相关的病症。本发明的化合物也可用于抑制具有磷酸酪氨酸结合区的其它酶，例如SH2结构域。因此，式I化合物可用于预防或治疗与肥胖，葡萄糖不耐受，糖尿病，高血压和大血管和小血管缺血性疾病相关的胰岛素抵抗。本发明的化合物还可用于治疗，预防或控制伴随2型糖尿病的多种病症，包括高脂血症，高甘油三酯血症，动脉粥样硬化，血管再狭窄，肠易激综合征，胰腺炎，脂肪细胞瘤和癌。作为脂肪肉瘤，血脂异常和其他指示胰岛素抵抗的疾病。此外，本发明的化合物可用于治疗或预防癌症，骨质疏松症，神经变性和感染性疾病以及涉及炎症和免疫系统的疾病。