# US 4,397,849 A · Benzothiazine derivatives

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- Number: US 4,397,849 A
- Document ID: US4397849A
- Status: Granted
- Kind: A
- Application number: 06/329,862
- Filed: 1981-12-11
- Granted: 1983-08-09
- Earliest claimed: 1980-12-30
- Assignees: Fujisawa Pharmaceutical Co., Ltd.
- Inventors: Tsutomu Teraji; Teruo Oku; Youichi Shiokawa
- Web page: https://patentgrep.com/patent/US4397849A

## CPC

- C07D 279/16: condensed with one six-membered ring
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

This invention relates to novel benzothiazine derivatives having therapeutic effect on autoimmune diseases, to processes for preparation of such derivatives, and to pharmaceutical compositions containing such derivatives, the derivatives having the formula: ##STR1## wherein R.sup.1 is lower alkyl which may have one or more substituents selected from carboxy, aryl and carboxy(lower)cycloalkyl; aryl which may have one or more substituents selected from halogen, lower alkyl, halo(lower)alkyl and lower alkoxy; haloarylamino; or heterocyclic group; R.sup.2 is hydrogen, lower alkyl, lower alkylamino(lower)alkyl, aryl or ar(lower)alkyl; R.sup.3 is hydrogen, halogen, lower alkyl or lower alkoxy; and n is an integer 0 to 2.

## Claims

### Claim 1

A compound of the formula or its pharmaceutically acceptable salt: ##STR7## wherein R.sup.1 is lower alkyl which may have one or more substituents selected from carboxy, phenyl and carboxy(lower)cycloalkyl;
phenyl which may have one or more substituents selected from halogen, lower alkyl, halo(lower)alkyl and lower alkoxy;
halophenylamino; or
5- or 6-membered heterocyclic group containing at least one hetero atom selected from oxygen, nitrogen and sulfur;
R.sup.2 is hydrogen, lower alkyl, lower alkylamino(lower)alkyl, phenyl or phenyl(lower)alkyl;
R.sup.3 is hydrogen, halogen, lower alkyl or lower alkoxy; and
n is an integer 0 to 2.

### Claim 2 (depends on 1)

A compound according to claim 1, wherein
R.sup.1 is lower alkyl which may have one or more substituents selected from carboxy, phenyl and carboxy(lower)cycloalkyl; phenyl which may have one or more substituents selected from halogen, lower alkyl, halo(lower)alkyl and lower alkoxy; halophenylamino; or 5 or 6 membered heterocyclic group containing at least one hetero atom selected from oxygen, nitrogen and sulfur
R.sup.2 is hydrogen, lower alkyl or lower alkylamino(lower)alkyl;
R.sup.3 is hydrogen, halogen or lower alkoxy; and
n is an integer 0 or 2.

### Claim 3 (depends on 2)

A compound according to claim 2, wherein
R.sup.1 is mono- or di- halophenyl, R.sup.2 is lower alkyl, R.sup.3 is hydrogen and n is an integer of 2.

### Claim 4 (depends on 3)

A compound according to claim 3, wherein
R.sup.1 is mono or di-halophenyl, and
R.sup.2, R.sup.3 and n are each as defined in claim 3.

### Claim 5 (depends on 4)

A compound according to claim 4, wherein
R.sup.1 is 3,4-dichlorophenyl, R.sup.2 is methyl, R.sup.3 is hydrogen and n is an integer of 2.

### Claim 6 (depends on 1)

A pharmaceutical composition for inhibition of contact hypersensitivity comprising as an active ingredient an effective amount of a compound of claim 1 or its pharmaceutically acceptable salt in admixture with a pharmaceutically acceptable carrier.