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US4464375A
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4-Anilinoquinazoline compounds and pharmaceutical compositions thereof
Assignee: Sankyo Co Ltd
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Filing: 1981-08-03
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Granted: 1984-08-07
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Expires: 2001-08-03
Abstract
Abstract 4-Anilinoquinazoline derivatives of formula (I): <IMAGE> (I) (in which: R1 represents a hydrogen atom, a halogen atom, a trifluoromethyl group or a nitro group; R2 represents a hydrogen atom, a C1-C4 alkyl group, an alkoxy group or a halogen atom; and R3 represents a hydrogen atom cr a C1-C4 alkyl group) and pharmaceutically acceptable salts thereof are, except where R1 represents a hydrogen atom or a chlorine atom in the 6- position when R2 and R3 both represent hydrogen atoms, new compounds and have been found to possess valuable analgesic and anti-inflammatory activities. These compounds can be prepared by heating the appropriate 4-haloquinazoline with an appropriate aniline or aniline derivative.
Inventors
- 👤 Shinsaku Kobayashi
- 👤 Katsuo Kamoshita
- 👤 Shigeki Nagai
- 👤 Takeo Honda
- 👤 Kiroku Oda
- 👤 Katsutoshi Fujii
- 👤 Takashi Kobayashi
- 👤 Mikio Kojima
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 16:51
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/70; C07D239/72; C07D239/86; C07D239/94; A; A61; A61P; A61P25/00; A61P25/04; A61P29/00
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
63 words
Compounds of formula (I): ##STR9## in which: R 1 represents a halogen atom, or a trifluoromethyl group; R 2 represents a hydrogen atom, a C 1 -C 4 alkyl group, a C 1 -C 4 alkoxy group or a halogen atom; and R 3 represents a hydrogen atom or a C 1 -C 4 alkyl group; and pharmacologically acceptable acid addition salts thereof.
Claim 2
Dependent Claim
63 words
Compounds of formula (I): ##STR9## in which: R 1 represents a halogen atom, or a trifluoromethyl group; R 2 represents a hydrogen atom, a C 1 -C 4 alkyl group, a C 1 -C 4 alkoxy group or a halogen atom; and R 3 represents a hydrogen atom or a C 1 -C 4 alkyl group; and pharmacologically acceptable acid addition salts thereof.
Claim 3
Dependent Claim
56 words
Compounds as claimed in claim 1, wherein: R 1 represents a chlorine atom, or a trifluoromethyl group; R 2 represents a hydrogen atom or it represents a methyl group, an ethyl group, a methoxy group, an ethoxy group or a chlorine atom at the 4'-position; and R 3 represents a methyl group or an ethyl group.
Claim 4
Dependent Claim
53 words
Compounds of formula (Ia): ##STR10## in which: R 1a represents a halogen atom or a trifluoromethyl group; and R 2 represents a hydrogen atom, a C 1 -C 4 alkyl group, an alkoxy group having a C 1 -C 4 -alkyl moiety or a halogen atom; and pharmacologically acceptable acid addition salts thereof.
Claim 5
Dependent Claim
53 words
Compounds of formula (Ia): ##STR10## in which: R 1a represents a halogen atom or a trifluoromethyl group; and R 2 represents a hydrogen atom, a C 1 -C 4 alkyl group, an alkoxy group having a C 1 -C 4 -alkyl moiety or a halogen atom; and pharmacologically acceptable acid addition salts thereof.
Claim 6
Dependent Claim
46 words
Compounds as claimed in claim 3, wherein: R 1a represents a chlorine atom or a trifluoromethyl group; and R 2 represents a hydrogen atom, a C 1 -C 4 alkyl group, an alkoxy group having a C 1 -C 4 alkyl moiety or a halogen atom.
Claim 7
Dependent Claim
34 words
Compounds as claimed in claim 3, wherein: R 1a represents a chlorine atom or a trifluoromethyl group; and R 2 represents a hydrogen atom, a methyl group, a methoxy group or a chlorine atom.
Claim 8
Dependent Claim
12 words
4-Anilino-7-chloroquinazoline and pharmaceutically acceptable salts thereof of the formula of claim 1.
Claim 9
Dependent Claim
12 words
4-Anilino-7-trifluoromethylquinazoline and pharmaceutically acceptable salts thereof of the formula of claim 1.
Claim 10
Dependent Claim
12 words
7-Chloro-4-(N-methylanilino)quinazoline and pharmaceutically acceptable salts thereof of the formula of claim 1.
Claim 11
Dependent Claim
12 words
4-(N-Methylanilino)-7-trifluoromethylquinazoline and pharmaceutically acceptable salts thereof of the formula of claim 1.
Claim 12
Dependent Claim
7 words
4-Anilino-7-chloroquinazoline of the formula of claim 1.
Claim 13
Dependent Claim
7 words
4-anilino-7-trifluoromethylquinazoline of the formula of claim 1.
Claim 14
Dependent Claim
7 words
7-chloro-4-(N-methylanilino)quinazoline of the formula of claim 1.
Claim 15
Dependent Claim
7 words
4-(N-methylanilino)-7-trifluoromethylquinazoline of the formula of claim 1.
Claim 16
Dependent Claim
88 words
A pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and an analgesic and anti-inflammatory effective amount of at least one compound of formula (I): ##STR11## in which: R 1 represents a halogen atom, or a trifluoromethyl group; R 2 represents a hydrogen atom, a C 1 -C 4 alkyl group, an alkoxy group having a C 1 -C 4 alkyl moiety or a halogen atom; and R 3 represents a hydrogen atom or a C 1 -C 4 alkyl group; and pharmacologically acceptable acid addition salts thereof.
Claim 17
Dependent Claim
88 words
A pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and an analgesic and anti-inflammatory effective amount of at least one compound of formula (I): ##STR11## in which: R 1 represents a halogen atom, or a trifluoromethyl group; R 2 represents a hydrogen atom, a C 1 -C 4 alkyl group, an alkoxy group having a C 1 -C 4 alkyl moiety or a halogen atom; and R 3 represents a hydrogen atom or a C 1 -C 4 alkyl group; and pharmacologically acceptable acid addition salts thereof.
Claim 18
Dependent Claim
15 words
The pharmaceutical composition of claim 14 containing an analgesic and anti-inflammatory effective amount of 4-anilino-7-chloroquinazoline.
Claim 19
Dependent Claim
15 words
The pharmaceutical composition of claim 14 containing an analgesic and anti-inflammatory effective amount of 4-anilino-7-trifluoromethylquinazoline.
Claim 20
Dependent Claim
15 words
The pharmaceutical composition of claim 14 containing an analgesic and anti-inflammatory effective amount of 7-chloro-4-(N-methylanilino)quinazoline.
Claim 21
Dependent Claim
15 words
The pharmaceutical composition of claim 14 containing an analgesic and anti-inflammatory effective amount of 4-(N-methylanilino)-7-trifluoromethylquinazoline.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-08-07 | 1988-02-06 | 1988-08-07 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-08-07 | 1992-02-06 | 1992-08-07 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-08-07 | 1996-02-06 | 1996-08-07 | $7700.00 | Window Closed / Lapsed |