专利号:US-5218089-A 优先权日:1988-12-23 标 题 :Retro-inverso analogues of thymopentin and the method for their synthesis 发明人:MARIOTTI SABINA; SISTO ALESSANDRO; NENCIONI LUCIANO; VILLA LUIGI; VERDINI ANTONIO S 权利人:SCLAVO SPA 摘要:New analogues of thymopentin (TP5) and of its tetrapeptide fragment (TP51-4) containing two non-contiguous retro-inverted bonds in the peptide chain are described which are of the general formula (I) (I) where R is hydrogen or an acyl radical, and R1 is an -OR2 group or an group where R2 is a hydrogen atom or a hydrocarbon radical, and R3 is a hydrogen atom or a hydroxyl group, and the corresponding pharmaceutically acceptable salts of acid or basic addition, possess immunomodulating activity.
专利号:US-8338565-B2 优先权日:2008-08-20 标 题 :Macrocyclic compounds for inhibition of tumor necrosis factor alpha 发明人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P 权利人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P; ENSEMBLE THERAPEUTICS CORP 摘要:Disclosed herein are macrocyclic compounds and methods for their synthesis and use. In particular, macrocyclic compounds are disclosed that modulate the activity of tumor necrosis factor alpha and/or are useful in the treatment of medical conditions, such as, rheumatoid arthritis, psoriasis, and asthma.
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-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.
专利号:EP-0375058-B1 优先权日:1988-12-23 标 题 :New retro-inverso analogues of trymopentin, the method for their synthesis and their use in the preparation of pharmaceutical compositions