发明名称 S1P receptors modulators and their use thereof
摘要 The invention relates to novel compounds that have SIP receptor modulating activity. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate SIP receptor modulating activity or expression, for example, autoimmune response. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate SIP receptor modulating activity or expression such as autoimmune response.
申请公布号 US9193716(B2) 申请公布日期 2015.11.24
申请号 US201314066276 申请日期 2013.10.29
申请人 Akaal Pharma PTY LTD. 发明人 Gill Gurmit S.;Grobelny Damian W.
分类号 A61K31/00;C07D413/04;A61K31/16;A61K31/18;A61K31/343;A61K31/382;A61K31/397;A61K31/403;A61K31/41;A61K31/4164;C07C33/26;C07C215/10;C07C215/14;C07C215/16;C07C229/16;C07C275/24;C07C275/28;C07C281/06;C07D205/04;C07D209/04;C07D209/08;C07D215/18;C07D233/32;C07D241/12;C07D257/04;C07D295/104;C07D307/79;C07D307/81;C07D311/22;C07D333/04;C07D333/20;C07D413/10;C07D413/14;C07F9/09;C07F9/6558 主分类号 A61K31/00
代理机构 Cooley LLP 代理人 Cooley LLP ;Erlacher Heidi A.;Ouyang Lian
主权项 1. A method of modulation of S1P receptor activity and/or expression by the administration of an effective amount of a compound of formula (II) or a stereoisomer and/or isotopic form or a pharmaceutically acceptable salt or derivative thereof, to a subject in need thereof wherein B′ is a five-membered heterocyclic ring selected from one of the following: the asterisks indicating the attachment within formula (II); G represents R is selected from hydrogen, deuterium, alkylamino, CH2OH, alkoxy, a C1-5 alkyl chain optionally containing one or more of deuterium, O, NR′R″, S, and halogen, heterocycle, amide, sulphonamide, COOH, —OPO3H2, and —PO3H2,represents an optional bridging group; A ring is phenyl or pyridinyl; R2 independently is selected from halogen, hydrogen, deuterium, CN, amino, alkylamino, alkoxy, CF3, and a C1-4 alkyl chain optionally containing one or more of deuterium, OH, NR′R″, S, SO, SO2, a carbon-carbon double bond, a carbon-carbon triple bond, a carbon-heteroatom double bond, a carbon-hetero atom triple bond, carbocycle, heterocycle, amide, and sulphonamide; J and D each are independently selected from hydrogen, deuterium, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylamino, halogen, amino, hydroxy, cyano, aryl, heterocycle, carbocycle, and a C1-10 alkyl chain optionally containing a carbon-carbon multiple bond or a carbon-hetero multiple bond wherein one or more carbon atoms are optionally independently replaced with oxygen, sulphur, SO, SO2, NR′, carbocycle or heterocycle; and R′ and R″ each are independently selected from alkyl, cycloalkyl, aryl, and heterocycle.
地址 Bundoora AU