首页> 外国专利> 4 - oxo - thiazole Derivatives, Pharmaceutical composition, method of preparing the same and their use in the manufacture of a Medicament for the treatment of diseases Modulated by Estrogen Related Receptor Alpha.

4 - oxo - thiazole Derivatives, Pharmaceutical composition, method of preparing the same and their use in the manufacture of a Medicament for the treatment of diseases Modulated by Estrogen Related Receptor Alpha.

机译:4-氧代噻唑衍生物,药物组合物,其制备方法及其在制备用于治疗由雌激素相关受体α调节的疾病的药物中的用途。

摘要

4-oxo-tiazol derivatives, pharmaceutical ingredients and methods of preparation and use of drugs used to treat diseases, including but not limited to peritonitis, water poison bacilli, arthritis (such as rheumatoid arthritis, infectious arthritis, ninez arthritis, psychoarthritis) Reactive arthritisBone related diseases (including those related to bone formation)Breast cancer (including breast cancer without estrogen therapy), cardiovascular disease, cartilage related diseases (such as cartilage damage / loss, cartilage degeneration) and cartilage formation related diseases,Condom, condom, chronic back injury, chronic bronchitis, chronic road inflammation, chronic obstructive pulmonary disease, diabetes, hypertension, gout, wig, lipid disorder, metabolic syndrome, multiple myeloma, obesity, skeletal inflammation, Incomplete osteoporosis, osteoporosis, osteoporosis, osteoporosis, Babbitt's disease, periodic disease, rheumatic multimite, Reiter syndrome, recurrent stress, hyperglycemia, hyperglycemia and insulin resistance. Item 1: a formula compound (1), wherein X is s or O, R1 is halogen,C1-4 alkyl optionally substituted, C1-4 alkoxy optionally substituted, or hydroxyl; R2 is selected from C1-3alkyl substituted by halo, cyano, halo, -C (O) NH2, and -C (O) O-C1-4alkyl, or alternatively R2 is attached together with R3 to form an aryl fused to the phenyl ring to which R2 and R3 are shown attached; R3 is H, or alternatively R3 is attached together with R2 to form an aryl fused to the phenyl ring to which R3 and R2 are shown attached; R4 is halo, cyano, C1-3 alkyl substituted by halo, -CsCH, -C (O) O-C1-4 alkyl, -C (O) NH2 or -S (O2) -C1-4 alkyl; and R5 and R6 are independently selected from H, optionally substituted C1-4 alkyl,Heteromorphic substitutes, isomerized substitutes or substitutes R5 and R6 are connected with N atom, and connected with N atom to form an isomerization, which contains alternative substitutes; or an optical isomer, dwarf, cholesterol, isomer, racemato, From a pharmaceutical point of view, acceptable salts or aquifers.
机译:4-氧-噻唑衍生物,药物成分以及用于治疗疾病的药物的制备和使用方法,包括但不限于腹膜炎,水毒杆菌,关节炎(如类风湿性关节炎,感染性关节炎,尼兹氏关节炎,精神性关节炎)反应性关节炎相关疾病(包括与骨形成有关的疾病)乳腺癌(包括未经雌激素治疗的乳腺癌),心血管疾病,与软骨相关的疾病(例如软骨损伤/丢失,软骨变性)和与软骨形成相关的疾病,避孕套,避孕套,慢性背损伤,慢性支气管炎,慢性道路炎症,慢性阻塞性肺疾病,糖尿病,高血压,痛风,假发,脂质疾病,代谢综合征,多发性骨髓瘤,肥胖症,骨骼炎症,不完全骨质疏松症,骨质疏松症,骨质疏松症,骨质疏松症,巴比特氏病,周期性疾病,风湿性多螨,雷特综合征,反复发作的压力,高血糖症,高血糖和胰岛素抵抗。第1项:式X化合物,其中X为s或O,R 1为卤素,任选取代的C 1-4烷基,任选取代的C 1-4烷氧基或羟基; R 2选自被卤素,氰基,卤素,-C(O)NH 2和-C(O)O-C 1-4烷基取代的C 1-3烷基,或者R 2与R 3一起连接以形成与苯基稠合的芳基R2和R3所连接的环; R3是H,或R3与R2连接在一起形成与R3和R2连接的苯环稠合的芳基。 R4是卤素,氰基,被卤素取代的C1-3烷基,-CsCH,-C(O)O-C1-4烷基,-C(O)NH 2或-S(O2)-C1-4烷基; R 5和R 6独立地选自H,任选取代的C 1-4烷基,亚同构取代基,异构化取代基或取代基R5和R6与N原子连接,并与N原子连接形成异构化,其包含备选取代基;或旋光异构体,侏儒,胆固醇,异构体,消旋体。从药学角度考虑,可接受的盐或含水层。

著录项

  • 公开/公告号AR065657A1

    专利类型

  • 公开/公告日2009-06-24

    原文格式PDF

  • 申请/专利权人 JANSSEN PHARMACEUTICA N.V.;

    申请/专利号AR2008P100964

  • 发明设计人

    申请日2008-03-07

  • 分类号C07D277/42;C07D417/04;A61K31/427;A61K31/496;A61K31/4523;A61P3/04;A61P3/10;A61P19/02;A61P19/10;A61P35/00;

  • 国家 AR

  • 入库时间 2022-08-21 19:28:40

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