专利号:US-2016153015-A1 优先权日:2013-06-27 标 题 :Synthesis method for l-heterocyclic amino acid and pharmaceutical composition having thereof 发明人:HONG HAO; ZHENG CHANGSHENG; GUO LINA 权利人:ASYMCHEM LAB TIANJIN CO LTD; ASYMCHEM LIFE SCIENCE TIANJIN CO LTD; TIANJIN ASYMCHEM PHARMACEUTICAL CO LTD; ASYMCHEM LAB FUXIN CO LTD; JILIN ASYMCHEM LAB CO LTD 摘要:A synthesis method for an L-heterocyclic amino acid and a pharmaceutical composition having the said amino acid are provided in the present disclosure. The synthesis method comprises: step A: preparing a heterocyclic keto acid, wherein the heterocycle in the heterocyclic keto acid is selected from any one of a five-membered heterocycle, a six-membered heterocycle, a seven-membered heterocycle, an alkyl-substituted five-membered heterocycle, an alkyl-substituted six-membered heterocycle, and an alkyl-substituted seven-membered heterocycle, and the keto acid group in the heterocyclic keto acid has a structural formula of n n n n n n n n n n and is located on any one of the carbon positions of the heterocycle, and step B: mixing the heterocyclic keto acid with ammonium formate, a phenylalanine dehydrogenase, a formate dehydrogenase and a coenzyme NAD + , and carrying out a reductive amination reaction to generate L-heterocyclic amino acid, wherein the amino acid sequence of the phenylalanine dehydrogenase is SEQ ID No. 1.
专利号:US-11267820-B2 优先权日:2015-09-09 标 题 :Tricyclic fused pyridin-2-one derivatives and their use as BRD4 inhibitors 发明人:VADIVELU SARAVANAN; RAJAGOPAL SRIDHARAN; RAMAIAH MANJUNATHA M; GONDRALA PAVAN KUMAR; CHINNAPATTU MURUGAN; SIVANANDHAN DHANALAKSHMI; PARIKH PAYAL KIRAN; MULAKALA CHANDRIKA 权利人:JUBILANT BIOSYS LTD 摘要:The present disclosure describes heterocyclic compounds of Formula I or, its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms and pharmaceutically active derivatives thereof and pharmaceutical compositions containing them as the active ingredient. The present disclosure also describes the synthesis and characterization of aforementioned compounds to exhibit high anticancer activity. The compounds of the present disclosure are useful as medicaments and their use in the manufacture of medicaments for treatment, prevention, or suppression of diseases, an conditions mediated b one or more BET family of bromodomains.
专利号:US-9957277-B2 优先权日:2015-11-25 标题 :eIF4A-inhibiting compounds and methods related thereto 发明人:ERNST JUSTIN T; REICH SIEGFRIED H; SPRENGELER PAUL A; TRAN CHINH VIET; PACKARD Garrick Kenneth; XIANG ALAN X; NILEWSKI CHRISTIAN; MICHELS THEO 权利人:EFFECTOR THERAPEUTICS INC 摘要:The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. n nFor Formula I compounds X, Y, R 1 , R 2 , R 3a , R 3b , R 4a , R 4b and R 5 are as defined in the specification. The inventive Formula I compounds are inhibitors of eIF4A and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.