专利号:US-6033882-A 优先权日:1994-07-07 标题:Chiral synthesis of 2-hydroxy carboxylic acids with a dehydrogenase 发明人:HOLBROOK JOSEPH JOHN; WILLIS CHRISTINE LOUISE; JOHNSEN KEYJI; HATELEY MARTIN JOHN 权利人:GENZYME CORP 摘要:PCT No. PCT/EP95/02692 Sec. 371 Date May 29, 1997 Sec. 102(e) Date May 29, 1997 PCT Filed Jul. 7, 1995 PCT Pub. No. WO96/01892 PCT Pub. Date Jan. 25, 1996Inter alia, an enzyme, a 2-hydroxy carboxylic acid dehydrogenase, characterised in that it is obtainable from Lactobacillus delbrueckii ssp. Bulgaricus and in that it catalyses the production of (R)-hydroxy derivatives of 2-keto acids, which are unsubstituted in the 3-position, but which may be substituted in the 4-position or beyond is disclosed.
专利号:US-2016319312-A1 优先权日:2013-07-29 标 题 :Synthesis method for l-cyclic alkyl amino acid and pharmaceutical composition having thereof 发明人:HONG HAO; ZHENG CHANGSHENG; GUO LINA 权利人:ASYMCHEM LABORATORIES (TIANJIN) CO LTD; ASYMCHEM LIFE SCIENCE (TIANJIN) CO LTD; TIANJIN ASYMCHEM PHARMACEUTICAL CO LTD; ASYMCHEM LABORATORIES (FUXIN) CO LTD; JILIN ASYMCHEM LABORATORIES CO LTD 摘要:A synthesis method for L-cyclic alkyl amino acid and a pharmaceutical composition having the said amino acid are provide in the present disclosure provides. The synthesis method comprises: step A.) preparing a cyclic alkyl keto acid or a cyclic alkyl keto acid salt having Structural Formula (I) or Structural Formula (II), and step B.) mixing the cyclic alkyl keto acid or the cyclic alkyl keto acid salt with ammonium formate, a leucine dehydrogenase, a formate dehydrogenase and a coenzyme NAD + , and carrying out a reductive amination reaction to generate the L-cyclic alkyl amino acid, wherein the Structural Formula (I) is n n n n n n n n n n where n 1 ≧1, m 1 ≧0 and the M 1 is H or a monovalent cation; the Structural Formula (II) is n n n n n n n n n n where n 2 ≧0, m 2 ≧0, the M 2 is H or a monovalent cation, an amino acid sequence of the leucine dehydrogenase is SEQ ID No.1.
专利号:US-9861636-B2 优先权日:2014-04-29 标题 :Polyfluorinated compounds acting as bruton tyrosine kinase inhibitors 发明人:HE WEI 权利人:HE WEI; ZHEJIANG DTRM BIOPHARMA CO LTD 摘要:Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton's tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.