专利号:EP-3091007-A1 优先权日:2015-05-08 标 题 :Process for the preparation of piperidine compounds 发明人:ATTOLINO EMANUELE; RIZZO ELISABETH; ROSSI DAVIDE 权利人:DIPHARMA FRANCIS SRL 摘要:The present invention relates to a process for the preparation of intermediates useful in the synthesis of efinaconazole and their use in the synthesis of efinaconazole.
专利号:US-11299484-B2 优先权日:2018-10-10 标 题 :Inhibiting fatty acid synthase (FASN) 发明人:MARTIN MATTHEW W; ZABLOCKI MARY-MARGARET; MENTE SCOT; DINSMORE CHRISTOPHER; WANG ZHONGGUO; ZHENG XIAOZHANG 权利人:FORMA THERAPEUTICS INC 摘要:The present disclosure is directed to inhibitors of FASN. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of FASN. For instance, the disclosure is concerned with compounds and compositions for inhibition of FASN, methods of treating, preventing, or ameliorating diseases or disorders associated with the inhibition of FASN, and methods of synthesis of these compounds.
专利号:US-7501407-B2 优先权日:2001-12-20 标题 :Pyrimidine A2B selective antagonist compounds, their synthesis and use 发明人:CASTELHANO ARLINDO; MCKIBBEN BRYAN; STEINIG ARNO; COLLINGTON ERIC 权利人:OSI PHARM INC 摘要:The subject invention provides compounds having the structure: n nwherein R 1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R 2 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R 3 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R 2 and R 3 are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R 3 is oxygen; R 4 and R 5 are each independently substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R 4 NR 5 together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl moiety containing from 1 to 6 heteroatoms;n R 12 is hydrogen, alkyl, halogen or cyano; and n is 0, 1, 2, 3 or 4, or an enantiomer, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the A 2b adenosine receptor by administering a therapeutically effective amount of the compounds of the invention.
专利号:WO-2012069566-A1 优先权日:2010-11-24 标 题 :Synthesis of n-heterocycles by reductive alkylation of cyan derivatives
专利号:US-11286268-B1 优先权日:2019-07-02 标题:EIF4E-inhibiting compounds and methods 发明人:SPERRY SAMUEL; XIANG ALAN X; ERNST JUSTIN T; REICH SIEGFRIED H; SPRENGELER PAUL A; SHAGHAFI MIKE; MICHELS THEO; NILEWSKI CHRISTIAN; TRAN CHINH VIET; PACKARD Garrick Kenneth; GRUBBS ALAN; URKALAN KAVERI; MUKAIYAMA TAKASUKE 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 n n n n n n n n n For Formula I compounds X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , Q, L 1 , L 2 , Y, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and rings A, B and C are as defined in the specification. The inventive Formula I compounds are inhibitors of eIF4e and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
专利号:WO-2018089904-A1 优先权日:2016-11-11 标 题 :Heterocyclic modulators of lipid synthesis