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-9815816-B2 优先权日:2005-09-30 标 题 :Chemical process for the synthesis of 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline 发明人:BLIXT JORGEN; GOLDEN MICHAEL DAVID; HOGAN PHILIP JOHN; MARTIN DAVID MICHAEL GLANVILLE; MONTGOMERY FRANCIS JOSEPH; PATEL ZAKARIYA; PITTAM JOHN DAVID; SEPENDA GEORGE JOSEPH; SQUIRE CHRISTOPHER JOHN; WRIGHT NICHOLAS CARTWRIGHT ALEXANDER 权利人:ASTRAZENECA AB; GENZYME CORP 摘要:The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilizing said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline.
专利号:US-8399502-B2 优先权日:2008-09-17 标 题 :Analogs of indole-3-carbinol and their use as agents against infection 发明人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN 权利人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN; STANFORD RES INST INT 摘要:Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2′-diindolylmethane, 2′,3-diindolylmethane, and 3,3′-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.
专利号:US-2019263782-A1 优先权日:2005-09-30 标 题 :Chemical Process for the Synthesis of 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline
专利号:US-2025188083-A1 优先权日:2021-06-25 标 题:Modulators of Histone Acetyltransferase 1 and Methods of Treatment Thereof 发明人:GRUBER JOSHUA JAMES; LIPCHIK ANDREW; SNYDER MICHAEL P; SCHOW STEVEN R 权利人:UNIV LELAND STANFORD JUNIOR 摘要:Small molecules compounds and methods of their synthesis are provided. Small molecules identified can inhibit histone acetyltransferase 1 activity. Formulations and medicaments are also provided that are directed to the treatment of human disorders and conditions, such as, for example, neoplasms, cancers, viral, fungal, and parasitic infections, and aging. Therapeutics are also provided containing a therapeutically effective dose of one or more small molecule compounds, present either as pharmaceutically effective salt or in pure form, including, but not limited to, formulations for oral, intravenous, or intramuscular administration.
专利号:US-7645754-B2 优先权日:2001-12-20 标题 :Pyrrolopyrimidine A2B selective antagonist compounds, their synthesis and use 发明人:CASTELHANO ARLINDO; MCKIBBEN BRYAN; STEINIG ARNO 权利人:OSI PHARM INC 摘要:The subject invention provides compounds having the structure: n n n n n n n n n n n n wherein,n R 1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(â•?O)NR a R b , —NR a R b , —NR a C(â•?O)NR a R b , —NR a C(â•?O)OR a , —OC(â•?O)NR a R b , or —NHC(â•?O) R a ; R 2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(â•?O)NR a R b , —NR a R b , —NR a C(â•?O)NR a R b , —NR a C(â•?O)OR a , —OC(â•?O)NR a R b , or —NHC(â•?O)R a , or R 1 , R 2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with —(CH 2 ) 2 OH or —CH 2 C(â•?O)OH; R 3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C 1 -C 15 )alkyl, (C 1 -C 15 )alkoxy, or —NR a R b ; R 4 is hydrogen or substituted or unsubstituted (C 1 -C 15 )alkyl; R 5 is —(CH 2 ) m OR 6 , —CHNOR 7 , —C(â•?O)NR 8 R 9 , —(CH 2 ) m C(â•?O)OR 10 , —(CH 2 ) k C(â•?O)NR 11 R 12 ;n wherein R 6 is a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 3 -C 10 )cycloalkyl, or an aryl, heteroaryl or 4-8 membered heterocyclic ring; R 7 is hydrogen, or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 1 -C 30 )alkylaryl; R 8 and R 9 are each independently hydrogen, or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 1 -C 30 )alkylaryl, (C 1 -C 30 )alkylamino, (C 1 -C 30 )alkoxy, or a saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic ring, or R 8 , N, and R 9 together form a substituted or unsubstituted 4-8 membered heterocyclic ring; R 10 is hydrogen or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 3 -C 10 )cycloalkyl, or an aryl, heteroaryl or heterocyclic ring; R 11 , N and R 12 together form a 4-8 membered heterocyclic ring; R a and R b are each independently hydrogen or alkyl; m is 0, 1, 2 or 3; and k is 1, 2 or 3,n nor a specific enantiomer thereof, or a specific tautomer thereof, or a pharmaceutically acceptable salt thereof, and a method for treating a disease associated with the A 2b adenosine receptor in a sbject in need of such treatment comprising administering to the subject a therapeutically effective amount of the compounds of the invention.
[参考文献]: Hideki Kubota, Et Al. Synthesis And Pharmacological Evaluation Of Piperidinoalkanoyl-1,2,3,4-Tetrahydroisoquinoline Derivatives As Novel Specific Bradycardic Agents. Bioorg Med Chem Lett. 2004 Jun 21;14(12):3049-52.
合成参考文献
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