您的位置: 首页 > 农业专利 > 详情页

CRYSTALLINE FORMS OF [(S)-1-CARBAMOYL-2-(PHENYLPYRIMIDIN-2-YLAMINO)ETHYL]AMIDE 2-(2-METHYLAMINOPYRIMIDIN-4-YL)-1H-INDOLE-5-CARBONIC ACID
专利权人:
SANOFI
发明人:
RITTSELER Olaf (DE),РИТЦЕЛЕР Олаф (DE),MONIKKE Mandi (DE),МОНИККЕ Манди (DE),BILLEN Gyunter (DE),БИЛЛЕН Гюнтер (DE),BAUMGARTNER Bruno (DE),БАУМГАРТНЕР Бруно (DE),BREKELMANN Martin (DE),БРЕКЕЛЬМАНН Мар,RITTSELER Olaf,РИТЦЕЛЕР Олаф,MONIKKE Mandi,МОНИККЕ Манди,BILLEN Gyunter,БИЛЛЕН Гюнтер,BAUMGARTNER Bruno,БАУМГАРТНЕР Бруно,BREKELMANN Martin,БРЕКЕЛЬМАНН Мартин,NAGEL Norbert,НАГЕЛЬ Норберт
申请号:
RU2014127478
公开号:
RU0002631320C2
申请日:
2012.12.04
申请国别(地区):
RU
年份:
2017
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: invention relates to the novel polymorph 1 ((S)-1-carbamoyl-2-(phenylpyrimidin-2-ylamino)ethyl]amide 2-(2-methylaminopyrimidin-4-yl)-1H-indole-5-carboxylic acid and method for its preparation. Polymorph 1 of the compound has the properties of IkB kinase inhibitors and can be used for the treatment of inflammatory, immunologically or metabolically mediated acute and chronic arthritis, arthropathies, rheumatoid arthritis, degenerative joint diseases, spondylosis, diabetes II type, inflammatory bowel disease, loss of cartilage following joint trauma or a relatively long period of joint immobilization after meniscus or patella injuries or torn ligaments, or diseases of the connective tissue, m algy or disorders of bone metabolism, and also for the treatment of pain, including acute pain and chronic pain. Polymorph 1 has characteristic reflections in a powder X-ray diffraction pattern using CuK-alpha1 radiation in the reflection mode at 2 theta angles (in degrees) of 14.9±0.2, 19.4±0.2, 19.7±0.2, 20.0±0.2, 22.3±0.2, 25.0±0.2. The method of producing polymorph 1 involves heating the polymorph 2 of mentioned compound in a mixture of acetone and water to a temperature of 50 to 60°C, cooling the mixture to a temperature of 20 to 25°C and precipitate precipitation. In this case polymorph 2 has a characteristic x-ray powder reflection using CuK-Alpha1 radiation reflection mode with 2 Theta angles (degrees): 5.8±0.2, 6.7±0.2, 9.3±0.2, 11.2±0.2, 16.5±0.2, 18.1±0.2, 19.4±0.2, 22.1±0.2, as well as indicators of DSC peaks 222.1±1; 248.1±1; 251±1 at heating rate 10°C/minute.EFFECT: polymorphic form 1 is thermodynamically stable, has low hygroscopicity and stability.8 cl, 2 tbl, 5 dwgНастоящее изобретение относится к новому полиморфу 1 [(S)-1-карбамоил-2-(фенилпиримидин-2-иламино)этил]амида 2-(2-метиламинопиримидин-4-ил)-1Н-индол-5-карбоновой кислоты и способу его получения. Полиморф 1 указанного соединения обладает свойствами ингибитора IkB киназы и может
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

意 见 箱

匿名:登录

个人用户登录

找回密码

第三方账号登录

忘记密码

个人用户注册

必须为有效邮箱
6~16位数字与字母组合
6~16位数字与字母组合
请输入正确的手机号码

信息补充