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Last Updated: November 25, 2020

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Claims for Patent: 7,638,536

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Summary for Patent: 7,638,536
Title:2-Acylaminothiazole derivative or salt thereof
Abstract: A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia.
Inventor(s): Sugasawa; Keizo (Tsukuba, JP), Watanuki; Susumu (Tsukuba, JP), Koga; Yuji (Tsukuba, JP), Nagata; Hiroshi (Tsukuba, JP), Obitsu; Kazuyoshi (Tsukuba, JP), Wakayama; Ryutaro (Tsukuba, JP), Hirayama; Fukushi (Tsukuba, JP), Suzuki; Ken-ichi (Tsukuba, JP)
Assignee: Astellas Pharma Inc. (Chuo-Ku, Tokyo, JP)
Application Number:10/500,964
Patent Claims: 1. A 2-acylaminothiazole derivative compound represented by the following Formula (V), or a pharmaceutically acceptable salt thereof: ##STR00114## wherein the symbols have the following meanings: Ar.sup.2: substituted or unsubstituted phenyl or monocyclic aromatic heterocycle; R.sup.3: a substituted or unsubstituted thienyl; R.sup.4: a group represented by Formula II: ##STR00115## wherein X is C(R.sup.27)R.sup.28 or NR.sup.26 and m=n=2; wherein CR.sup.20R.sup.21 and CR.sup.22R.sup.23 can be identical or different; and wherein each of R.sup.20, R.sup.21, R.sup.22, R.sup.23, R.sup.26, R.sup.27, and R.sup.28 can be the same or different and can be selected from the group consisting of H; --OH; --O-lower alkyl; a substituted or unsubstituted lower alkyl; a substituted or unsubstituted cycloalkyl; a substituted or unsubstituted aryl; a substituted or unsubstituted arylalkyl; a substituted or unsubstituted aromatic heterocycle; a substituted or unsubstituted aromatic heterocyclic alkyl; a substituted or unsubstituted nonaromatic heterocycle; lower alkenyl; lower alkylidene; --COOH; --COO-lower alkyl; --COO-lower alkenyl; --COO-lower alkylene-aryl; --COO-lower alkylene-aromatic heterocycle; carbamoyl or amino, each of which can be substituted with one or more groups selected from the group consisting of lower alkyl which can be substituted with halogen, --OH, --O-lower alkyl, or --O-aryl; --NHCO-lower alkyl; and oxo.

2. The compound according to claim 1, wherein Ar.sup.2 is phenyl or pyridyl, each of which can be substituted.

3. The compound according to claim 1, wherein R.sup.3 is a thienyl which is substituted with 1 to 3 halogen atoms, which can be identical or different.

4. The compound according to claim 3, wherein R.sup.4 is 4-(piperidin-1-yl)piperidin-1-yl, 4-propylpiperidin-1-yl, 4-cyclohexylpiperazin-1-yl, or 4-propylpiperazin-1-yl.

5. The compound according to claim 4, wherein Ar.sup.2 is phenyl which is unsubstituted at 2- and 6-positions, substituted with --H, --F, --Cl, or --Br at 3-position, substituted with --F, --Cl, or --Br at 5-position, and substituted at 4-position; or pyridin-3-yl which is unsubstituted at 2- and 4-positions, substituted with --F, --Cl, or --Br at 5-position, and substituted at 6-position.

6. The compound according to claim 5, wherein Ar.sup.2 is phenyl which is substituted at 4-position with a group selected from the group consisting of --O--R.sup.Y, --NH--R.sup.Y, a substituted or unsubstituted piperidin-1-yl and a substituted or unsubstituted piperazin-1-yl; or pyridin-3-yl which is substituted at 6-position with a group selected from the group consisting of --O--R.sup.Y, --NH--R.sup.Y, a substituted or unsubstituted piperidin-1-yl and a substituted or unsubstituted piperazin-1-yl, wherein R.sup.Y is lower alkyl which can be substituted with one or more groups selected from the group consisting of --OH, --O-lower alkyl, amino which can be substituted with one or two lower alkyl, --CO.sub.2H, --CO-lower alkyl, carbamoyl which can be substituted with one or two lower alkyl, cyano, aryl, aromatic heterocycle, nonaromatic heterocycle and halogen.

7. The compound according to any one of claims 1-6 wherein the pharmaceutically acceptable salt is a maleate salt.

8. A compound selected from the group consisting of: 1-(3-chloro-5-{[4-(4-chlorothiophen-2-yl)-5-(4-cyclohexylpiperazin-1-yl)t- hiazol-2-yl]carbamoyl}-2-pyridyl)piperidine-4-carboxylic acid, and pharmaceutically acceptable salts thereof.

9. The compound of claim 8, wherein the pharmaceutically acceptable salt is the maleic acid salt.

10. A pharmaceutical composition comprising a therapeutically effective amount of any one of the pharmaceutical compounds of claims 1-6 and a pharmaceutically acceptable carrier.

11. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 7 and a pharmaceutically acceptable carrier.

12. The pharmaceutical composition according to claim 10, wherein the pharmaceutical composition is formulated for oral administration.

13. The pharmaceutical composition according to claim 11, wherein the pharmaceutical composition is formulated for oral administration.

14. A pharmaceutical composition for treating thrombocytopenia, the composition comprising: a therapeutically effective amount of a compound selected from the group consisting of ##STR00116## and pharmaceutically acceptable salts thereof; and a pharmaceutically acceptable carrier.

15. The pharmaceutical composition of claim 14, wherein the compound is: ##STR00117##

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