专利号:US-9795613-B2 优先权日:2014-12-10 标题 :GLP-1 receptor modulators 发明人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM R; BRAHMACHARY ENUGURTHI; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; KNAGGS MICHAEL; GLYNN DANIEL; MILLS MARK 权利人:CELGENE INT II SÀRL 摘要:Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “ â€? represents either or both the R and S form of the compound): n nwhere A, B, C, Y 1 , Y 2 , Z, R 1 , R 2 , R 3 , R 4 , R 5 , W 1 , n, p and q are as defined herein.
专利号:US-9187522-B2 优先权日:2011-12-12 标题 :GLP-1 receptor modulators 发明人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM R; BRAHMACHARY ENUGURTHI; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; KNAGGS MICHAEL 权利人:RECEPTOS INC 摘要:The invention relates to compounds that modulate the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds are act as modulators or potentiators of GLP-1 receptor on their own, or with receptor ligands including GLP-1 peptides GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “ â€? represents either or both the R and S form of the compound): n nwhere A, B, C, Y 1 , Y 2 , Z, R 1 , R 2 , R 3 , R 4 , R 5 , W 1 , n, p and q are as defined herein.
专利号:US-9598430-B2 优先权日:2013-06-11 标 题 :GLP-1 receptor modulators 发明人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM R; BRAHMACHARY ENUGURTHI; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; KNAGGS MICHAEL 权利人:RECEPTOS INC; CELGENE INT II SÀRL 摘要:Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “ â€? represents either or both the R and S form of the compound): n nwhere A, B, C, Y 1 , Y 2 , Z, R 1 , R 2 , R 3 , R 4 , R 5 , W 1 , n, p and q are as defined herein.
参考标题:Design And Synthesis Of Poly(Adp-Ribose) Polymerase Inhibitors: Impact Of Adenosine Pocket-Binding Motif Appendage To The 3-Oxo-2,3-Dihydrobenzofuran-7-Carboxamide On Potency And Selectivity 作者:Uday Kiran Velagapudi,Marie-France Langelier,Cristina Delgado-Martin,Morgan E. Diolaiti,Sietske Bakker,Alan Ashworth,Bhargav A. Patel,Xuwei Shao,John M. Pascal,Tanaji T. Talele |发布日期:2019.6.13 摘要:Poly(Adenosine 5'-Diphosphate-Ribose) Polymerase (Parp) Inhibitors Are A Class Of Anticancer Drugs That Block The Catalytic Activity Of Parp Proteins. Optimization Of Our Lead Compound 1 (( Z)-2-Benzylidene-3-Oxo-2,3-Dihydrobenzofuran-7-Carboxamide; Parp-1 Ic50 = 434 Nm) Led To A Tetrazolyl Analogue (51, Ic50 = 35 Nm) With Improved Inhibition. Isosteric Replacement Of The Tetrazole Ring With A Carboxyl