[EN] SUBSTITUTED 4,5,6,7-TETRAHYDRO-PYRAZOLO[1,5-a]PYRAZINE DERIVATIVES AND 5,6,7,8-TETRAHYDRO-4H-PYRAZOLO[1,5-a][1,4]DIAZEPINE DERIVATIVES AS ROS1 INHIBITORS<br/>[FR] DÉRIVÉS 4,5,6,7-TÉTRAHYDRO-PYRAZOLO[1,5-A]PYRAZINE SUBSTITUÉS ET DÉRIVÉS 5,6,7,8-TÉTRAHYDRO-4H-PYRAZOLO[1,5-A][1,4]DIAZÉPINE UTILISÉS COMME INHIBITEURS DE ROS1
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2015144799A1
公开(公告)日:2015-10-01
The present invention relates to substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyrazine derivatives and 5,6,7,8-tetrahydro-4H-pyrazolo[1,5-a][1,4]diazepine derivatives of formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as ROS 1 inhibitors. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
本发明涉及取代的4,5,6,7-四氢吡唑并[1,5-a]吡嗪衍生物和5,6,7,8-四氢-4H-吡唑并[1,5-a][1,4]二氮杂环衍生物的公式(I)中的变量具有权利要求中定义的含义。根据本发明的化合物可用作ROS 1抑制剂。本发明还涉及制备这种新化合物的方法,包含所述化合物作为活性成分的药物组合物,以及将所述化合物用作药物的用途。
Novel compounds for the management of aging-related and diabetic vascular complications, process for their preparation and therapeutic uses thereof
申请人:——
公开号:US20010018524A1
公开(公告)日:2001-08-30
Novel compounds of the pyridinium series useful for the management of diabetes and aging-related vascular complications, including kidney disease, nerve damage, atherosclerosis, retinopathy, dermatological disorders and discoloration of teeth, by breaking preformed AGE, of the general formula I, or pharmaceutically acceptable salts thereof,
1
wherein, R
1
, R
2
, R
3
, X and m are as defined in the specification. Also disclosed is a method for preparation of the compounds of general formula (I) and pharmaceutical composition containing one or more compounds as defined above as active ingredients. Also disclosed is a method of treatment of a diabetic patient by administering the compounds as defined above, either singly or in combination with drugs for antidiabetic therapy.
本发明涉及一系列新的吡啶系列化合物,可用于管理糖尿病和与衰老相关的血管并发症,包括肾脏疾病、神经损伤、动脉硬化、视网膜病变、皮肤疾病和牙齿变色,通过破坏预先形成的AGE,其通式为I,或其药学上可接受的盐,其中,R1、R2、R3、X和m如规范中所定义。本发明还公开了一种制备通式(I)化合物的方法和含有一种或多种上述化合物作为活性成分的制药组合物。本发明还公开了一种通过单独或与抗糖尿病治疗药物联合使用上述化合物治疗糖尿病患者的方法。