Patent ID: 7241757
Filing Date: 2007-07-10
Classification: A61P,C07D

Abstract:
1. A compound of formula I, wherein R R R R R R R q represents 0, 1 or 2; R wherein the dotted lines independently represent optional bonds; A and E independently represent CH; D represents —CH═CH—; X A Z represents S(O) R R R R R R R Y represents CH R n represents 0,1, 2, 3 or 4; and B represents a structural fragment of formula IIIa or IIIc wherein X R R R one of D R R A R R A Het represents, at each occurrence, a five- to ten-membered heteroaryl group, which may be aromatic in character, containing one or more nitrogen, oxygen or sulphur atoms in the ring system; n and r independently represent 0 or 1; X X R R m represents, at each occurrence, 0, 1 or 2; or a pharmaceutically acceptable salt thereof; provided that: (a) when A (b) when A (c) when A (d) the compound is not: (S)- or (R)-1-hydroxy-7-methoxytetralin-1-yl-C(O)-Pro-Pab; (R)- or (S)-1-hydroxy-7-methoxytetralin-1-yl-C(O)-Pro-Pab; (S)- or (R)-1-hydroxy-7-methoxytetralin-1-yl-C(O)-Aze-Pab×HOAc; (R)- or (S)-1-hydroxy-7-methoxytetralin-1-yl-C(O)-Aze-Pab; 1-hydroxy-5-methoxytetralin-1-yl-C(O)-Aze-Pab×HOAc; 1-hydroxy-5,7-dimethyltetralin-1-yl-C(O)-Aze-Pab×HOAc; 1-hydroxy-7-aminotetralin-1-yl-C(O)-Aze-Pab×HOAc; 1-hydroxytetralin-1-yl-C(O)-Aze-Pab×HOAc; 7-methoxytetralin-1-yl-C(O)-Aze-Pab×HOAc; (R)- or (S)-7-methoxy-1-methyltetralin-1-yl-C(O)-Aze-Pab; 4-hydroxy-6-methoxychroman-4-yl-C-(O)Aze-Pab×OAc; (S)- or (R)-1-hydroxy-4-methoxyindan1-yl-C(O)-Aze-Pab; 1-hydroxy-5-methoxytetralin-1-yl-C(O)-Aze-Pab(OH); (S)- or (R)-1-hydroxy-7-methoxytetralin-1-yl-C(O)-Aze-Pab(OH); 4-hydroxy-6-methoxychroman-yl-C(O)-Aze-Pab(OH); 4-hydroxy-6-methoxychroman-4-yl-C(O)-Aze-Pab(OMe); (S)- or (R)-1-hydroxy-7-methoxytetralin-1-yl-C(O)-Aze-Pab-(C(O)OCH (S)- or (R)-1-hydroxy-7-methoxytetralin-1-yl-C(O)-Aze-Pab-(C(O)OCH 7-methoxy-1-allyltetralin-1-yl-C(O)-Aze-Pab×HOAc; (S)- or (R)-1-hydroxy-7-chlorotetralifl-1-yl-C(O)-Pro-Pab; 1-n-propyl-7-methoxytetralin-1-yl-C(O)-Aze-Pab×HOAc; 6-chloro-4-hydroxychroman-4-yl-C(O)-Aze-Pab×HOAc; 4-hydroxychroman-4-yl-C(O)-Aze-Pab×HOAc; 6,8-dichloro-4-hydroxychroman-4-yl-C(O)-Aze-Pab×HOAc; 6-fluoro-4-hydroxychroman-4-yl-C(O)-Aze-Pab×HOAc; 4-hydroxy-6-methylchroman-4-yl-C(O)-Aze-Pab×HOAc; 8-chloro-4-hydroxy-6-methoxychroman-4-yl-C(O)-Aze-Pab×HOAc; 6-chloro-4-hydroxy-8-methylcbroman-4-yl-C(O)Aze-Pab×HOAc; (S)- or (R)-1-hydroxy-7-methoxytetralin-1-yl-C(O)-Aze-Pab(O—C(O)-i-Pr); (S)- or (R)-1-hydroxy-7-methoxytetralin-1-yl-C(O)-Aze-Pab(O—C(O)-Et); (S)- or (R)-1-hydroxy-7-methoxytetralin-1-yl-C(O)-Aze-Pab(O—C(O)—Ch); (S)- or (R)-1-hydroxy-7-methoxytetralin-1-yl-C(O)-Aze-Pab(O-allyl); (S)- or (R)-1-hydroxy-7-methoxytetralin-1-yl-C(O)-Aze-Pab(O-Bzl); (S)- or (R)-1-hydroxy-7-methoxytetralin-1-yl-C(O)-Aze-Pab-(CO—O-methallyl); 1-hydroxy-7-aminotetralin-1-yl-C(O)-Aze-Pab(OH); (S)- or (R)-1-hydroxy-7-methoxytetralin-1-yl-C(O)-Aze-Pab(O-Val); (S)- or (R)-1-hydroxy-7-methoxytetralin-1-yl-C(O)-Aze-(Me)Pab; or 9-hydroxyfluoren-9-yl-C(O)-Aze-Pab×HOAc.