Back to results
US 2004/0024019 A1Published application
Drug composition antagonistic to both pgd2/txa2 receptors
AssigneeShionogi & Co., Ltd.
InventorsNorihiko Tanimoto, Akinori Arimura
Life of this patent
Estimating the term…
Abstract
A compound of the formula (I): 1 wherein A is alkylene optionally having an unsaturated bond; R is —C(═O)—R1; R1 is hydroxy or the like; m is 0 or 1; p is 0 or 1; X1 and X3 are each independently optionally substituted aryl or optionally substituted heteroaryl or the like; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(═O)—, or the like, having a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor is found.
Claims24
A compound of the formula (I):
- 583
- A is alkylene optionally intervened with a heteroatom, optionally having an oxo group, optionally substituted with halogen and/or optionally having an unsaturated bond;
- R is —C(═O)—R1, —CH2—R1, or tetrazolyl;
- R1 is hydroxy, alkyloxy, or optionally substituted amino;
- m is 0 or 1;
- provided that combinations wherein m is 1, A is —CH═CH—CH2—CH2—CH2— and R is —C(═O)—R1 (R1 is hydroxy or alkyloxy) and wherein A is —CH2—CH═CH—CH2—CH2—CH2— and R is —C(═O)—R1 wherein R1 is hydroxy or alkyloxy are excluded, p is 0 or 1, provided that when p=0, X1 is not bonded to X3 via X4;
- X1 and X3 are each independently optionally substituted aryl, optionally substituted heteroaryl or optionally substituted non-aromatic heterocyclyl;
- X2 is a bond, —CH2—, —CH2—CH2—, —C(═O)—, —O—, —S—, —SO—, —SO2—, —NH—, —N(CH3)—, —C(═N—O—CH3)—, —N═N—, —CH═CH—, —(C═O)—NH—, —NH—(C═O)—, —CH2—NH—, —NH—CH2—, —CH2—O—, —O—CH2—, —CH2—, —S—CH2—, —CH2—SO2—, —SO2—CH2—, —SO2—NH—, —NH—SO2—, —C(═CH2)—, —SO2N(Me)—, —CH2NHSO2—, —CH2NH—(C═O)—, —NH—C(═O)—NH or —NH—C(═O)—N(Me)—;
- X4 is —CH2—, —CH2—CH2—, —C(═O)—, —SO—, —SO2—, —(C═O)—NH—, —NH—(C═O)—, —CH2—NH—, —NH—CH2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, —CH2—SO2—, —SO2—CH2—, —SO2—NH— or —NH—SO2—,
- provided that a combination wherein
- 584
- A is —CH═CH—CH2—CH2—CH2—, R is —COOH, m is 1, p is 0, X1 and X3 are phenyl, and X2 is —N═N—, is excluded
- and provided that when
- 585
- X1 and X3 are phenyl, X2 is —CH═CH—, —O—, or —S—, m is 0, and p is 0, a compound wherein A is —CH═CH—CH2—CH2—CH2—C(CH3)2— and R is COOH, A is —CH2—C(═O)—CH2—CH2—CH2—CH2— and R is COOH, A is —CH2—CH2—CH2—CH2—CH2— and R is —COOH, or A is —CH═CH—CH2—CH2—CH2— and R is —CH2OH,
- is excluded,
- a prodrug, a pharmaceutically acceptable salt or a solvate thereof.
14 more elements
A compound of the formula:
- X3—X2—X1—COOH wherein X3 is pyrrolyl optionally substituted with alkyl, alkyloxy or halogen, indolyl optionally substituted with alkyl, alkyloxy or halogen, indolinyl optionally substituted with alkyl, alkyloxy or halogen, or 1,2,3,4-tetrahydroquinolyl optionally substituted with alkyl, alkyloxy or halogen;
- X2 is —SO2—, —S— or —CH2—;
- X1 is thienyl, or a salt thereof.
Dependencies are inferred from the claim text.