专利号:US-7126025-B2 优先权日:2003-01-21 标 题 :Synthesis of 4-(amino)-2-butenoyl chlorides and their use in the preparation of 3-cyano quinolines 发明人:CONSIDINE JOHN LEO; DAIGNEAULT SYLVAIN; CHEW WARREN; IERA SILVIO; DUNCAN SCOTT MASON; REN JIANXIN 权利人:WYETH CORP 摘要:This invention provides a compound of Formula (I): n nwhereinn S 1 and S 2 are each independently, hydrogen, alkyl, alkenyl, alkynyl, aralkyl, substituted or unsubstituted aryl, and S 1 and S 2 together with the nitrogen to which they are attached form a nitrogen containing heteroaryl and a pharmaceutically acceptable salt thereof; a method of preparing the compound of Formula (I), and use of the compound of Formula (I) in the preparation of 3-cyano quinolines.
专利号:US-10550127-B1 优先权日:2017-02-08 标题:Indanylaminoazadihydrobenzofuranylacetic acids, pharmaceutical compositions for the treatment of diabetes 发明人:ECKHARDT MATTHIAS; WAGNER HOLGER; PETERS STEFAN 权利人:BOEHRINGER INGELHEIM INT 摘要:The present invention relates to compounds of general formula I, n nwherein the groups R, R 1 , R 2 , m and n are defined herein, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
专利号:US-2004162442-A1 优先权日:2003-01-21 标 题 :Synthesis of 4-(amino)-2-butenoyl chlorides and their use in the preparation of 3-cyano quinolines
专利号:US-8981092-B2 优先权日:2008-09-19 标题 :Substituted 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-ones as modulators of protein kinase activity 发明人:MIRIZZI DANILO; CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; FERGUSON RON; CASUSCELLI FRANCESCO 权利人:MIRIZZI DANILO; CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; FERGUSON RON; CASUSCELLI FRANCESCO; NERVIANO MEDICAL SCIENCES SRL 摘要:Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, n nor pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
专利号:WO-2004066919-A2 优先权日:2003-01-21 标 题:Synthesis of 4amino-2-butenoyl chlorides and their use in the preparation of 3-cyano quinolines
专利号:WO-2008022467-A1 优先权日:2006-08-25 标 题 :2-substituted azain doles and 2 substituted thienopyrroles, their precursors and novel processes for the preparation thereof 发明人:LAUTENS MARK; YUEN JOSEPHINE; FANG YUANQING 权利人:LAUTENS MARK; YUEN JOSEPHINE; FANG YUANQING 摘要:The present invention relates generally to processes for the chemical synthesis of azaindole and thienopyrrole compounds, in particular azaindole and thienopyrrole compounds that are substituted at the 2-position of the azaindole or thienopyrrole ring, and optionally at additional locations of the azaindole or thienopyrrole ring such as the 1- and/or 3-position, compounds prepared by such processes, and synthetic precursors of such processes. More particularly, the present invention relates to the preparation of 2- substituted azaindoles from an ortho-gem-dihalovinylaminopyridine or from an ortho- gem-dihalovinylaminopyridine N-oxide compound and an organoboron reagent using a palladium metal pre-catalyst, base and a ligand. The present invention also relates to the preparation of 2-substituted thienopyrroles from an ortho-gem-dihalovinylthiophene compound and an organoboron reagent using a palladium metal pre-catalyst, base and a ligand. The present invention also relates to processes for the production of ortho-gem- dihalovinylaminopyridines which are useful as starting materials in the production of 2- substituted azaindoles, and novel compounds prepared by the processes. The present invention also relates to processes for the production of ortho-gem-dihalovinylthiophenes which are useful as starting materials in the production of 2-substituted thienopyrroles, and novel compounds prepared by the processes. Formulae (V) and (VII).