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    • 2. 发明授权
    • Process for producing blocked isocyanate compound
    • 封端异氰酸酯化合物的制备方法
    • US07504518B2
    • 2009-03-17
    • US11666696
    • 2005-10-27
    • Hideo MiyataMasatoshi MurakamiKatsutoshi Ohno
    • Hideo MiyataMasatoshi MurakamiKatsutoshi Ohno
    • C07D231/00C07D231/10
    • C07D231/32C07D231/12
    • Disclosed is a process for producing a blocked isocyanate compound represented by general formula (III): wherein R1, R2, Q1, and Q2 are as defined in the specification, characterized by comprising reacting a pyrazole compound (I) with an ethylenically unsaturated group-containing isocyanate compound (II) at a temperature in the range of 0° C. to 90° C. The production process can efficiently produce a high-purity blocked isocyanate compound without substantially producing by-products. In the production process, unlike the prior art technique, since there is no need to use any inert solvent such as toluene or xylene, safety to the human body and environment is excellent and the production processes and equipment can be simplified. The blocked isocyanate compound produced by the production process contains no residual inert solvent and is suitable for use in extensive fields such as various coating agents, adhesives, and molding materials.
    • 公开了一种制备由通式(III)表示的封端异氰酸酯化合物的方法:其中R1,R2,Q1和Q2如说明书中所定义,其特征在于包括使吡唑化合物(I)与烯属不饱和基团 - 含有异氰酸酯化合物(II)的温度在0℃〜90℃的范围内。制造方法可以有效地制造高纯度的封端异氰酸酯化合物而基本不产生副产物。 在生产过程中,与现有技术不同,由于不需要使用甲苯或二甲苯等惰性溶剂,因此对人体和环境的安全性优异,可以简化生产方法和设备。 通过生产方法生产的封端异氰酸酯化合物不含残留的惰性溶剂,适用于各种涂料,粘合剂和成型材料等广泛领域。
    • 3. 发明申请
    • Pyrazole derivative, drug composition containing the same and production intermediate therefor
    • 吡唑衍生物,含有它们的药物组合物及其制备中间体
    • US20070060531A1
    • 2007-03-15
    • US10561217
    • 2004-06-15
    • Norihiko KikuchiHideki FujikuraShigeki TazawaTokuhisa YamatoMasayuki Isaji
    • Norihiko KikuchiHideki FujikuraShigeki TazawaTokuhisa YamatoMasayuki Isaji
    • A61K31/7052C07H15/00
    • C07D231/32A61K31/7056A61K31/706C07D231/52Y10S514/866
    • The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl, etc.; one of Q and T represents a group selected from the following: , and the other represents -Z-Ar wherein Z represents —O—, —S—, etc.; Ar represents an optionally substituted C6-10 aryl, etc.; R represents an optionally substituted C3-8 cycloalkyl, an optionally substituted C6-10 aryl, etc., pharmaceutically acceptable salts thereof, and prodrugs thereof, which exhibit an excellent inhibitory activity in human sodium/glucose cotransporter (SGLT) and are useful as agents for the prevention, inhibition of progression or treatment of a disease associated with the excess uptake of at least a kind of carbohydrates selected from glucose, fructose and mannose (diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, etc.), and pharmaceutical compositions containing the same, medicinal uses thereof and intermediates for production therefor.
    • 本发明提供由以下通式表示的吡唑衍生物:其中R 1表示H,任选取代的C 1-6烷基等; Q和T中的一个表示选自以下的基团:另一个表示-Z-Ar,其中Z表示-O-,-S-等; Ar表示任选取代的C 6-10芳基等; R表示任选取代的C 3-8环烷基,任选取代的C 6-10芳基等,其药学上可接受的盐及其前药,其表现出优异的 在人钠/葡萄糖协同转运蛋白(SGLT)中的抑制活性,并且可用作预防,抑制与选自葡萄糖,果糖和甘露糖中的至少一种碳水化合物的过量摄取相关的疾病的进展或治疗的药剂(糖尿病, 餐后高血糖,葡萄糖耐量降低,糖尿病并发症等),含有该组合物的药物组合物,其医药用途和用于其生产的中间体。