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US4382094A Expired / Lapsed US ⏱️ 0.0 years remaining

Reduced naphthalenes, their preparation and use

Assignee: Beecham Group PLC
•
Filing: 1981-07-29
•
Granted: 1983-05-03
•
Expires: 2001-07-29
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Abstract

Abstract A compound of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: Ar is phenyl, optionally substituted by one or more C 1-4 alkyl, C 1-4 alkoxy, halogen, cyano, nitro, hydroxy, CONH 2 , CO 2 W wherein W is C 1-6 alkyl or C 1-4 alkylphenyl which phenyl may be substituted by one or more C 1-4 alkyl, C 1-4 alkoxy or halogen, NR 1 R 2 wherein R 1 and R 2 are selected from hydrogen or C 1-6 alkyl, NHCO C 1-6 alkyl or C 1-6 alkylcarbonyloxy; phenyl disubstituted on adjacent carbon atoms by methylenedioxy; furyl or thienyl; the dotted lines represent an optionally present double bond; and X is CO or CR 1 OH wherein R 1 is hydrogen or C 1-4 alkyl, having useful pharmacological activity, processes for their preparation and their use.

Inventors

  • 👤 Alexander C. Goudie
  • 👤 Josephine M. Cox

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 17:09
CPC Classifications
C; C07; C07D; C07D339/00; C07D339/02; C07D339/06; A; A61; A61K; A61K31/00; A61K31/12; C07C; C07C205/00; C07C205/45; C07C255/00; C07C45/00; C07C45/56; C07C45/567; C07C45/61; C07C45/67; C07C45/673; C07C45/68; C07C49/00; C07C49/587; C07C49/657; C07C49/683; C07C49/687; C07C49/697; C07C49/703; C07C49/747; C07C49/753; C07C65/00; C07C65/32; C07C65/38; C07D307/00; C07D307/02; C07D307/34; C07D307/38; C07D307/40; C07D307/46; C07D317/00; C07D317/08; C07D317/44; C07D317/46; C07D317/48; C07D317/50; C07D317/54; C07D333/00; C07D333/02; C07D333/04; C07D333/06; C07D333/22

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 76 words
A compound of formula (I): ##STR35## wherein: Ar is phenyl, optionally substituted by one or more C 1-4 alkyl, C 1-4 alkoxy, halogen, nitro, hydroxy or NR 1 R 2 wherein R 1 and R 2 are selected from hydrogen or C 1-6 alkyl; the dotted lines represent an optionally present double bond; and X is CO or CR 1 OH wherein R 1 is hydrogen or C 1-4 alkyl; or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim 76 words
A compound of formula (I): ##STR35## wherein: Ar is phenyl, optionally substituted by one or more C 1-4 alkyl, C 1-4 alkoxy, halogen, nitro, hydroxy or NR 1 R 2 wherein R 1 and R 2 are selected from hydrogen or C 1-6 alkyl; the dotted lines represent an optionally present double bond; and X is CO or CR 1 OH wherein R 1 is hydrogen or C 1-4 alkyl; or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim 50 words
A compound according to claim 1 wherein Ar is phenyl, optionally substituted by C 1-4 alkyl, C 1-4 alkoxy or halogen; the dotted line in formula (I) represents an optionally present double bond; and X is CO or CR 1 OH wherein R 1 is hydrogen or C 1-4 alkyl.
Claim 4
Dependent Claim 50 words
A compound according to claim 1 of the formula (IV) ##STR36## wherein Ar 1 is phenyl optionally substituted by one or more C 1-4 alkyl, C 1-4 alkoxy, halogen, nitro, hydroxy, or NR 1 R 2 wherein R 1 and R 2 are selected from hydrogen or C 1-6 alkyl.
Claim 5
Dependent Claim 27 words
A compound according to claim 3 of the formula (V): ##STR37## wherein Ar 111 is phenyl or phenyl substituted by methyl, ethyl, methoxy, chlorine, bromine, or nitro.
Claim 6
Dependent Claim 40 words
A compound according to claim 3 of the formula (VI): ##STR38## wherein Ar 1V is phenyl substituted by hydroxy, or NR 1 1 R 2 1 wherein R 1 1 and R 1 2 are selected from hydrogen and methyl.
Claim 7
Dependent Claim 15 words
A compound according to claim 1, characterised in that the exocyclic double bond is present.
Claim 8
Dependent Claim 3 words
2-(4-Dimethylaminobenzylidene)-3,4,8,8a-tetrahydro-8a-methyl-1,6(2H,7H)-naphthalenedione, or 2-(3-hydroxybenzylidene)-3,4,8,8a-tetrahydro-8a-methyl-1,6(2H,7H)-napthalenedione.
Claim 9
Dependent Claim 3 words
2-(4-Dimethylaminobenzylidene)-3,4,8,8a-tetrahydro-8a-methyl-1,6(2H,7H)-naphthalenedione, or 2-(3-hydroxybenzylidene)-3,4,8,8a-tetrahydro-8a-methyl-1,6(2H,7H)-napthalenedione.
Claim 10
Dependent Claim 32 words
An anti-inflammatory pharmaceutical composition adapted for topical administration which comprises an effective amount of a compound according to claim 1 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier therefor.
Claim 11
Dependent Claim 35 words
A method of treatment or prophylaxis of inflammation in mammals including man which comprises the topical administration of a therapeutically effective amount of a compound according to claim 1 or a pharmaceutically acceptable salt thereof.

References Cited (Backward Citations)

US4201869A Cited
US3833726A Cited
US3843665A Cited
US4177271A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1986-05-02 1986-11-01 1987-05-03 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1990-05-02 1990-11-01 1991-05-03 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1994-05-02 1994-11-01 1995-05-03 $7700.00 Window Closed / Lapsed

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