Details for Patent: 9,839,637

Title:	Piperazine-substituted benzothiophenes for treatment of mental disorders
Abstract:	The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
Inventor(s):	Yamashita; Hiroshi (Tokushima, JP), Ito; Nobuaki (Tokushima, JP), Miyamura; Shin (Tokushima, JP), Oshima; Kunio (Tokushima, JP), Matsubara; Jun (Tokushima, JP), Kuroda; Hideaki (Tokushima, JP), Takahashi; Haruka (Tokushima, JP), Shimizu; Satoshi (Tokushima, JP), Tanaka; Tatsuyoshi (Tokushima, JP)
Assignee:	OTSUKA PHARMACEUTICAL CO., LTD. (Tokyo, JP)
Filing Date:	Sep 06, 2017
Application Number:	15/697,196
Claims:	1. A pharmaceutical composition comprising a heterocyclic compound or a salt thereof represented by formula (1): ##STR00176## wherein ring Q is a bicyclic group selected from the group consisting of: ##STR00177## wherein the ring Q may have 1 to 3 substituents selected from the group consisting of a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a hydroxy group, a lower alkoxy group, a halogenated lower alkyl group, a phenyl group, a phenyl lower alkyl group, a naphthyl lower alkyl group, a phenyl lower alkoxy group, a naphthyl lower alkoxy group, a benzoyl group, a lower alkenyloxy group, a lower alkanoyl group, a lower alkanoyloxy group, a cyclo C.sub.3-C.sub.8 alkyl group, a cyclo C.sub.3-C.sub.8 alkyl lower alkyl group, a halogen atom, a carbamoyl group which may have a lower alkyl group, a carboxy group, a lower alkoxycarbonyl group, an amino group which may have a lower alkanoyl group, a nitro group, a hydroxy lower alkyl group, an amino lower alkyl group which may have a lower alkyl group, a thienyl group, and a pyrrolidinyl lower alkyl group; R.sub.2 represents a hydrogen atom or a lower alkyl group; and A represents --O-A.sub.1-, wherein A.sub.1 is a C.sub.1-C.sub.6 alkylene group; and a pharmaceutically acceptable carrier. 2. A pharmaceutical composition comprising a heterocyclic compound or a salt thereof represented by formula (1): ##STR00178## wherein ring Q is a bicyclic group selected from the group consisting of: ##STR00179## wherein the carbon-carbon between the 3-position and 4-position of the bicyclic heterocyclic skeleton represents a single bond or a double bond; wherein the ring Q may have 1 to 3 substituents selected from the group consisting of a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a hydroxy group, a lower alkoxy group, a halogenated lower alkyl group, a phenyl group, a phenyl lower alkyl group, a naphthyl lower alkyl group, a phenyl lower alkoxy group, a naphthyl lower alkoxy group, a benzoyl group, a lower alkenyloxy group, a lower alkanoyl group, a lower alkanoyloxy group, a cyclo C.sub.3-C.sub.8 alkyl group, a cyclo C.sub.3-C.sub.8 alkyl lower alkyl group, a halogen atom, a carbamoyl group which may have a lower alkyl group, a carboxy group, a lower alkoxycarbonyl group, an amino group which may have a lower alkanoyl group, a nitro group, a hydroxy lower alkyl group, an amino lower alkyl group which may have a lower alkyl group, a thienyl group, and a saturated 5- to 6-membered heteromonocyclic group containing 1 to 2 nitrogen atoms-substituted lower alkyl group; R.sub.2 represents a hydrogen atom or a lower alkyl group; and A represents --O-A.sub.1-, wherein A.sub.1 is a C.sub.1-C.sub.6 alkylene group; and a pharmaceutically acceptable carrier. 3. A pharmaceutical composition comprising 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one and a pharmaceutically acceptable carrier. 4. The pharmaceutical composition according to claim 3, wherein the 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one is present in the pharmaceutical composition in an amount ranging from 1% to 70% by weight. 5. The pharmaceutical composition according to claim 3, wherein the 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one is present in the pharmaceutical composition in an amount ranging from 1% to 30% by weight. 6. The pharmaceutical composition according to claim 3, wherein the composition contains from 1 mg to 200 mg of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one. 7. The pharmaceutical composition according to claim 3, wherein the composition contains about 1 mg of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one. 8. The pharmaceutical composition according to claim 6, wherein the pharmaceutical composition is in the form of a tablet. 9. A method for treating major depression comprising administering a pharmaceutical composition according to claim 3. 10. A method for treating schizophrenia comprising administering a pharmaceutical composition according to claim 3. 11. A pharmaceutical composition comprising a pharmaceutically acceptable salt of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-- 2-one and a pharmaceutically acceptable carrier. 12. The pharmaceutical composition according to claim 11, wherein the pharmaceutically acceptable salt of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one is present in the pharmaceutical composition in an amount ranging from 1% to 70% by weight. 13. The pharmaceutical composition according to claim 11, wherein the pharmaceutically acceptable salt of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one is present in the pharmaceutical composition in an amount ranging from 1% to 30% by weight. 14. The pharmaceutical composition according to claim 11, wherein the composition contains from 1 mg to 200 mg of the pharmaceutically acceptable salt of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one. 15. The pharmaceutical composition according to claim 11, wherein the composition contains about 1 mg of the pharmaceutically acceptable salt of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one- . 16. The pharmaceutical composition according to claim 14, wherein the pharmaceutical composition is in the form of a tablet. 17. A method for treating major depression comprising administering a pharmaceutical composition according to claim 11. 18. A method for treating schizophrenia comprising administering a pharmaceutical composition according to claim 11.