380893-73-2Relevant articles and documents
Derivatives of hexahydrobenzofuranone useful for the treatment of (inter alia) auto-immune or inflammatory disorders
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, (2016/03/04)
Heterocyclic-substituted compounds of formula (I) or a pharmaceutically acceptable salt thereof, are disclosed, wherein: Z is - (CH2)n-; (a); (b), wherein R 10 is absent; or, (c) wherein R 3 is absent; the single dotted line represents an optional double bond; the double dotted line represents an optional single bond; n is 0-2; Het is an optionally substituted mono-, bi- or tri-cyclic heteroaromatic group; B is -(CH 2 ) n3 -. wherein n 3 is 0-5, -CH 2 -O-, -CH 2 S-, -CH 2 -NR 6 -, -C(O)NR 6 -. -NR 6 C(O)-, (d), optionally substituted alkenyl or optionally substituted alkynyl; X is -O- or -NR 6 - when the double dotted line represents a single bond, or X is H, -OH or -NHR 20 when the bond is absent; Y is =O, =S, (H, H), (H, OH) or (H, C 1 -C 6 alkoxy) when the double dotted line represents a single bond or when the bond is absent, Y is =O, =NOR 17 (H, H). (H, OH), (H, SH), (H, C 1 -C 6 alkoxy) or (H, substituted-amino); R 22 and R 23 are independently -OH, -OC(O)R 30 , OC(O)NR 30 R 31 , or optionally substituted alkyl, alkenyl, alkynyl, heterocycloalkyl, aryl, cycloalkyl, cycloalkenyl, carbonyl, amino, alkoxy, alkenyloxy, alkynyloxy, heterocycloalkyloxy, cycloalkyloxy, or cycloalkenyloxy; or R 22 and R 10 , or R 23 and R 11 , can form a carbocyclic or heterocyclic ring; and the remaining variables are as described in the specification, Also disclosed are pharmaceutical compositions containing said compounds and their use as thrombin receptor antagonists and blinders to cannabinoid receptors.
Heterotricyclic himbacine analogs as potent, orally active thrombin receptor (protease activated receptor-1) antagonists
Chelliah, Mariappan V.,Chackalamannil, Samuel,Xia, Yan,Eagen, Keith,Clasby, Martin C.,Gao, Xiaobang,Greenlee, William,Ahn, Ho-Sam,Agans-Fantuzzi, Jacqueline,Boykow, George,Hsieh, Yunsheng,Bryant, Matthew,Palamanda, Jairam,Chan, Tze-Ming,Hesk, David,Chintala, Madhu
, p. 5147 - 5160 (2008/03/14)
Pursuing our earlier efforts in the himbacine-based thrombin receptor antagonist area, we have synthesized a series of compounds that incorporate heteroatoms in the C-ring of the tricyclic motif. This effort has resulted in the identification of several p
