公开(公告)号：EP2105442A1

公开(公告)日：2009-09-30

申请号：EP07850951.0

申请日：2007-12-20

申请人： Astellas Pharma Inc. ,  Kotobuki Pharmaceutical Co., Ltd.

发明人： KOMENOI, Kousuke ,  NAKAMURA, Atsushi ,  KASAI, Makoto ,  IMAMURA, Masakazu ,  SHIRAKI, Ryota ,  NAKANISHI, Keita

IPC分类号： C07D409/10 ,  A61K31/381 ,  A61P3/10 ,  C07D333/54

CPC分类号： C07D409/10 ,  C07D333/54

摘要： The present invention provides a method for producing a C-glycoside derivative, which can produce the C-glycoside derivative at a high yield and at a low cost, which conforms to environmental protection, and which is applicable industrially. The C-glycoside derivative is useful for treating and preventing diabetes such as insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes) and the like and various diabetes-related diseases including insulin-resistant diseases and obesity.

摘要翻译： 本发明提供一种可以以高产率和低成本生产符合环境保护并且在工业上可应用的C-糖苷衍生物的方法。 C-糖苷衍生物可用于治疗和预防糖尿病如胰岛素依赖性糖尿病（1型糖尿病），非胰岛素依赖型糖尿病（2型糖尿病）等，以及各种糖尿病相关疾病，包括胰岛素抵抗性疾病和 肥胖。

公开(公告)号：EP2894152A1

公开(公告)日：2015-07-15

申请号：EP13835562.3

申请日：2013-09-06

申请人： Astellas Pharma Inc.

发明人： KIKUCHI, Takashi ,  YOSHIDA, Shinya ,  NAKAMURA, Atsushi ,  AKIBA, Takahiro ,  YOSHINO, Toshitaka ,  NAKAGAWA, Shuichi ,  SATO, Kiichi

IPC分类号： C07D235/12 ,  C07D309/12 ,  C07D405/12

CPC分类号： C07D235/12 ,  C07B2200/13 ,  C07D235/14 ,  C07D309/06 ,  C07D309/12 ,  C07D405/12

摘要： Provided are a method for producing a sulfonyl amidine compound, which has an excellent gonadotropin releasing hormone receptor antagonism and is useful as a therapeutic agent for gonadotropin-dependent diseases (for example, prostate cancer, breast cancer, endometriosis, uterine fibroid, prostatic hyperplasia, or the like) or a salt thereof, and a synthesis intermediate useful in the production method. The production method of the present invention controls formation of a by-product which is hardly removed unless column purification is conducted and racemization of a target compound, thereby obtaining the target compound with a high purity, and therefore, the production method is suitable for industrial production.

摘要翻译： 本发明提供促进促性腺激素释放激素受体拮抗作用优异，作为促性腺激素依赖性疾病（例如前列腺癌，乳腺癌，子宫内膜异位症，子宫肌瘤，前列腺增生症等）的治疗剂有用的磺酰脒化合物的制造方法。 或类似物）或其盐，以及用于该生产方法的合成中间体。 本发明的制造方法，在不进行塔精制和目标化合物的外消旋化而得到高纯度的目标化合物的情况下，控制难以除去的副产物的生成，因此适合于工业上的制造方法 生产。