← Back to Patent Explorer
US4076818A Expired / Lapsed US ⏱️ 0.0 years remaining

Pyrazolo [1,5-C]quinazoline derivatives and related compounds

Assignee: ER Squibb and Sons LLC
•
Filing: 1976-07-02
•
Granted: 1978-02-28
•
Expires: 1996-07-02
📄 Original PDF 🌐 Google Patents 🔄 Sync Now

Abstract

Abstract Compounds are provided having the structure ##STR1## wherein R 1 and R 2 may be the same or different and R 1 is hydrogen, alkyl of 1-3 carbons, phenyl optionally substituted by R 4 or ##STR2## hydrogen, lower alkyl or phenyl optionally substituted by R 4 with the proviso that at least one of R 1 and R 2 is ##STR3## R 3 is hydrogen, lower alkyl, benzyl or phenyl optionally substituted by R 4 ; and R 4 and R 5 are the same or different and represent hydrogen, lower alkyl, lower alkoxy, alkanoyloxy, benzyloxy, hydroxy, halogen (Cl, Br and F), nitro, and trifluoromethyl; R 6 is hydrogen, lower alkyl, alkanoyl, aroyl, aralkanoyl, aralkyl or phenyl; and R 7 , R 8 , m and n are as defined hereinafter. These compounds are useful as anti-allergics.

Inventors

  • 👤 B. Richard Vogt

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-02 18:35
CPC Classifications
C; C07; C07D; C07D487/00; C07D487/02; C07D487/04; A; A61; A61P; A61P29/00; A61P3/00; A61P37/00; A61P37/08; C07C; C07C45/00; C07C45/27; C07C45/29; C07C45/292; C07C49/00; C07C49/76; C07C49/794; C07D209/00; C07D209/02; C07D209/04; C07D209/30; C07D209/40

Claims Analysis

Total Claims: 12
Claim 1
Independent Claim 319 words
A compound of the structure ##STR537## wherein R 1 and R 2 are the same or different, and R 1 is selected from the group consisting of hydrogen, lower alkyl, phenyl, phenyl having an R 4 substituent, or ##STR538## R 2 is selected from the group consisting of ##STR539## hydrogen, lower alkyl, phenyl or phenyl having an R 2 substitutent, with the proviso that at least one of R 1 and R 2 is ##STR540## R 6 is selected from the group consisting of ##STR541## having 1 to 8 carbons in the alkyl group, ##STR542## having 1 to 8 carbons in the alkyl group or ##STR543## wherein phenyl includes unsubstituted phenyl, mono-, or di-lower-alkylphenyl, or halophenyl; R 3 is selected from the group consisting of hydrogen, lower alkyl, benzyl, phenyl, or phenyl having an R 4 sustituent; R 4 and R 5 are the same or different and are selected from the group consisting of hydrogen, alkyl of 1 to 4 carbons, alkoxy of 1 to 4 carbons, lower alkanoyloxy of 1 to 4 carbons, nitro, benzyloxy, benzyloxy having a lower alkoxy, halogen, hydroxy, or trifluoromethyl substituent; R 7 and R 8 may be the same or different and are selected from the group consisting of hydrogen, alkyl of 1 to 3 carbons, phenyl, phenyl having a lower alkoxy substituent, benzyl, or benzyl having a lower alkoxy substituent, or R 7 and R 8 taken together is a single cycloalkyl ring of 3 to 7 carbons; (CH 2 ) m and (CH 2 ) n represent straight chain alkylene radicals or mono- or di-alkyl substituted alkylene radicals wherein the alkyl group has 1 to 8 carbons, m and n are integers which represent the number of carbon atoms in the longest normal chains and may be the same or different and are 0 to 10, with the proviso that m + n ≦ 10, and physiologically acceptable salts thereof.
Claim 2
Dependent Claim 319 words
A compound of the structure ##STR537## wherein R 1 and R 2 are the same or different, and R 1 is selected from the group consisting of hydrogen, lower alkyl, phenyl, phenyl having an R 4 substituent, or ##STR538## R 2 is selected from the group consisting of ##STR539## hydrogen, lower alkyl, phenyl or phenyl having an R 2 substitutent, with the proviso that at least one of R 1 and R 2 is ##STR540## R 6 is selected from the group consisting of ##STR541## having 1 to 8 carbons in the alkyl group, ##STR542## having 1 to 8 carbons in the alkyl group or ##STR543## wherein phenyl includes unsubstituted phenyl, mono-, or di-lower-alkylphenyl, or halophenyl; R 3 is selected from the group consisting of hydrogen, lower alkyl, benzyl, phenyl, or phenyl having an R 4 sustituent; R 4 and R 5 are the same or different and are selected from the group consisting of hydrogen, alkyl of 1 to 4 carbons, alkoxy of 1 to 4 carbons, lower alkanoyloxy of 1 to 4 carbons, nitro, benzyloxy, benzyloxy having a lower alkoxy, halogen, hydroxy, or trifluoromethyl substituent; R 7 and R 8 may be the same or different and are selected from the group consisting of hydrogen, alkyl of 1 to 3 carbons, phenyl, phenyl having a lower alkoxy substituent, benzyl, or benzyl having a lower alkoxy substituent, or R 7 and R 8 taken together is a single cycloalkyl ring of 3 to 7 carbons; (CH 2 ) m and (CH 2 ) n represent straight chain alkylene radicals or mono- or di-alkyl substituted alkylene radicals wherein the alkyl group has 1 to 8 carbons, m and n are integers which represent the number of carbon atoms in the longest normal chains and may be the same or different and are 0 to 10, with the proviso that m + n ≦ 10, and physiologically acceptable salts thereof.
Claim 3
Dependent Claim 27 words
The compound of claim 1 wherein R 1 is hydrogen or ##STR544## wherein R 6 is ##STR545## and R 2 is ##STR546## wherein R 6 is ##STR547##
Claim 4
Dependent Claim 33 words
The compound of claim 2 wherein R 3 is hydrogen or lower alkyl, R 4 and R 5 are hydrogen, or one of R 4 and R 5 is halogen or lower alkoxy.
Claim 5
Dependent Claim 21 words
The compound of claim 2 wherein R 1 is hydrogen and R 2 is selected from the group consisting of ##STR548##
Claim 6
Dependent Claim 37 words
The compound of claim 4 wherein R 3 is hydrogen, and R 5 is 7-, 8-, 9- or 10-Cl, 7-, 8-, 9- or 10--OCH 3 , or 8- or 9--CH 3 , 9-F, or 7-CF 3 .
Claim 7
Dependent Claim 18 words
The compound as defined in claim 5 wherein R 5 is 7-OCH 3 and R 4 is 10-Cl.
Claim 8
Dependent Claim 23 words
The compound as defined in claim 4 having the structure ##STR549## wherein R 6' is alkyl of 1 to 4 carbons or hydrogen.
Claim 9
Dependent Claim 11 words
The compound as defined in claim 7 wherein alkyl is methyl.
Claim 10
Dependent Claim 13 words
The compound as defined in claim 7 wherein alkyl is ethyl or propyl.
Claim 11
Dependent Claim 23 words
A pharmaceutical composition for use in treating allergic conditions comprising a compound as defined in claim 1 and a pharmaceutically acceptable carrier therefor.
Claim 12
Dependent Claim 26 words
A method for treating allergic conditions in mammals, which comprises administering to the mammalian host a therapeutic amount of a compound as defined in claim 1.

References Cited (Backward Citations)

US3171740A Cited
US3810894A Cited
US4002755A Cited
US3890324A Cited
US3895027A Cited
US3897434A Cited
US3899508A Cited
US3903106A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1981-02-27 1981-08-29 1982-02-28 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1985-02-27 1985-08-29 1986-02-28 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1989-02-27 1989-08-29 1990-02-28 $7700.00 Window Closed / Lapsed

Assigned Categories & Tags

No categories assigned to this patent yet.

Assign Category Tag