专利号:US-4375545-A 优先权日:1981-06-22 标 题 :Process for the synthesis of the nicotinyl ester of 6-aminonicotinic acid 发明人:WARNER JR PAUL L; LUBER JR EDWARD J; SOMERVILLE WILLIAM A; ZUSI F CHRISTOPHER 权利人:WESTWOOD PHARMACEUTICALS INC 摘要:6-Aminonicotinic acid is reacted with an alkali carbonate selected from the group consisting of sodium carbonate and potassium carbonate. The reaction is carried out at elevated temperature and in dimethylformamide. The 6-aminonicotinic acid alkali salt so produced is reacted with 3-chloromethylpyridine hydrochloride. The reaction is carried out at elevated temperature and in dimethylformamide. The desired nicotinyl ester is thus produced.
专利号:US-10308595-B2 优先权日:2013-02-15 标 题:Albicidin derivatives, their use and synthesis 发明人:SUESSMUTH RODERICH; KRETZ JULIAN; SCHUBERT VIVIEN; PESIC ALEXANDER; HUEGELLAND MANUELA; ROYER MONIQUE; COCIANCICH STEPHANE; ROTT PHILIPPE; KERWAT DENNIS; GRAETZ STEFAN 权利人:UNIV BERLIN TECH 摘要:Antibiotically active compounds characterized by general formula (I), wherein X1, BB, BC, BD, BE and X2 are building blocks with D1, D2, D3, D4 or D5 being linkers which include carbon, sulphur, nitrogen, phosphor and/or oxygen atoms and which are covalently connecting the moities BA and BB, BB and BC, BC and BD, BD and BE and BE and BF, respectively, and wherein in particular the building block BC comprises an amino acid derivative. The compounds for use in a method of treatment of diseases, in particular for use in a method of treatment of bacterial infections are also disclosed.
专利号:US-11731956-B2 优先权日:2018-10-22 标 题:Substituted 1,2,4-triazoles as intermediates in the synthesis of TYK2 inhibitors
专利号:US-9700543-B2 优先权日:2011-05-31 标题 :GLP-1 receptor stabilizers and modulators 发明人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; BRAHMACHARY ENUGURTHI; YEAGER ADAM RICHARD 权利人:CELGENE INT II SÀRL 摘要:Compounds that bind the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, methods of their therapeutic and/or prophylactic use, and methods of their use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor are provided. Certain compounds may have activity as modulators or potentiators with respect to glucagon receptor, GIP receptor, GLP-1 and GLP-2 receptors, and PTH receptor on their own or in the presence of receptor ligands such as GIP(1-42), PTH(1-34), Glucagon(1-29), GLP-2(1-33), GLP-1(7-36), GLP-1(9-36), oxyntomodulin and exendin variants.
专利号:US-11530205-B2 优先权日:2017-04-28 标题:GLP-1 receptor modulators 发明人:TAMIYA JUNKO; TURNBULL PHILIP; ENUGURTHI BRAHMACHARY; HUANG LIMING; YEAGER ADAM R; FOWLER THOMAS; IACOBINI GREG P; CRITTALL MATTHEW RICHARD 权利人:RECEPTOS LLC 摘要:Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as products containing such compounds, and methods of their use and synthesis. Such compounds have the structure of Formula (I) below: (I) or pharmaceutically acceptable salts thereof, wherein A, J, W 1 , Y, Z, R 1 , R 2 , R 3 and R 4 are as defined herein.
专利号:US-8518952-B2 优先权日:2008-08-06 标题 :6 substituted 2-heterocyclylamino pyrazine compounds as CHK-1 inhibitors 发明人:BRAGANZA JOHN FREDERICK; COLLINS MICHAEL RAYMOND; KATH JOHN CHARLES; NINKOVIC SACHA; LI HUI; RICHTER DANIEL TYLER 权利人:BRAGANZA JOHN FREDERICK; COLLINS MICHAEL RAYMOND; KATH JOHN CHARLES; NINKOVIC SACHA; LI HUI; RICHTER DANIEL TYLER; PFIZER 摘要:The present invention is directed to compounds of formula (I), n nand pharmaceutically acceptable salts thereof, their synthesis, and their use as CHK-1 inhibitors.