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N6 -tricyclic adenosines

Assignee: Warner Lambert Co LLC
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Filing: 1984-10-26
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Granted: 1986-06-03
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Expires: 2004-10-26
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Abstract

Abstract N 6 -Tricyclic adenosines and pharmaceutically acceptable acid addition salts having highly desirable central nervous system and cardiovascular properties, processes for their manufacture and pharmaceutical compositions and methods for using said compounds and compositions are described.

Inventors

  • 👤 James A. Bristol
  • 👤 Walter Moos
  • 👤 Bharat K. Trivedi

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-25 08:38
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/16; A; A61; A61P; A61P25/00; A61P25/04; A61P25/20; A61P9/00; A61P9/12

Claims Analysis

Total Claims: 13
Claim 1
Independent Claim 198 words
A compound of the formula: ##STR6## wherein R 6a is hydrogen or lower alkyl; R 6b is hydrogen, hydroxy, lower alkyl, lower alkanoyloxy- or benzoyloxy; R 6c and 6d are each independently hydrogen or one or more substituents selected from halogen, hydroxy, lower alkoxy, lower alkanoyloxy, benzoyloxy, lower S(O)n-alkyl in which n is 0, 1, or 2, sulfonamide, trifluoromethyl, lower alkyl, lower mono- or dialkylamino, nitro or sulfhydryl; X is a valence bond or a straight or branched alkylene of 1 to 8 carbon atoms; Y is a valence bond, oxygen, sulfur, NR in which R is hydrogen, lower alkyl, lower alkanoyl or benzoyl, --(CH 2 )n-- in which n is 1 or 2 or --CH═CH--; R 2 is hydrogen, halogen, NR i R ii , or i or SR i in which R i and R ii are each independently hydrogen, lower alkyl or phenyl, lower alkyl; R 2' , R 3' , and R 5' are each independently hydrogen, lower alkanoyl, benzoyl, benzoyl substituted by lower alkyl, lower alkoxy, halogen or trifluoromethyl, or R 2' and R 3' may be bonded together to form a lower alkylidene group, on a pharmaceutically acceptable acid form salt thereof.
Claim 2
Dependent Claim 198 words
A compound of the formula: ##STR6## wherein R 6a is hydrogen or lower alkyl; R 6b is hydrogen, hydroxy, lower alkyl, lower alkanoyloxy- or benzoyloxy; R 6c and 6d are each independently hydrogen or one or more substituents selected from halogen, hydroxy, lower alkoxy, lower alkanoyloxy, benzoyloxy, lower S(O)n-alkyl in which n is 0, 1, or 2, sulfonamide, trifluoromethyl, lower alkyl, lower mono- or dialkylamino, nitro or sulfhydryl; X is a valence bond or a straight or branched alkylene of 1 to 8 carbon atoms; Y is a valence bond, oxygen, sulfur, NR in which R is hydrogen, lower alkyl, lower alkanoyl or benzoyl, --(CH 2 )n-- in which n is 1 or 2 or --CH═CH--; R 2 is hydrogen, halogen, NR i R ii , or i or SR i in which R i and R ii are each independently hydrogen, lower alkyl or phenyl, lower alkyl; R 2' , R 3' , and R 5' are each independently hydrogen, lower alkanoyl, benzoyl, benzoyl substituted by lower alkyl, lower alkoxy, halogen or trifluoromethyl, or R 2' and R 3' may be bonded together to form a lower alkylidene group, on a pharmaceutically acceptable acid form salt thereof.
Claim 3
Dependent Claim 17 words
A compound as claimed in claim 1, wherein R 6 a and R 6 b are hydrogen.
Claim 4
Dependent Claim 26 words
A compound as claimed in claim 1, wherein R 6 a , R 6 b , R 6 c , and R 6 d are hydrogen.
Claim 5
Dependent Claim 24 words
A compound as claimed in claim 3, where X is a valence bond, methylene or ethylene and Y is a valence bond or oxygen.
Claim 6
Dependent Claim 12 words
A compond as claimed in claim 4, wherein R 2 is hydrogen.
Claim 7
Dependent Claim 19 words
A compound as claimed in claim 5, wherein R 2' , R 3' , and R 5' are hydrogen.
Claim 8
Dependent Claim 12 words
A compound as claimed in claim 6, and being N 6 -fluorenyladenosine.
Claim 9
Dependent Claim 12 words
A copound as claimed in claim 6, and being N 6 -fluorenylmethyladenosine.
Claim 10
Dependent Claim 12 words
A compound as claimed in claim 6, and being N 6 -fluorenylethyladenosine.
Claim 11
Dependent Claim 12 words
A compound as claimed in claim 6, and being N 6 -(xanthene-9-methylamino)adenosine.
Claim 12
Dependent Claim 25 words
A pharmaceutical composition for treating psychosis comprising an antipsychotic effective amount of a compound as claimed in claim 1 together with a pharmaceutically acceptable carrier.
Claim 13
Dependent Claim 31 words
A method of treating psychosis in a mammal suffering therefrom comprising administering to such mammal an antipsychotic effective amount of a compound as claimed in claim 1 in unit dosage form.

References Cited (Backward Citations)

US3551409A Cited
DE2139107A1 Cited
US3901876A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1989-06-02 1989-12-02 1990-06-03 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1993-06-02 1993-12-02 1994-06-03 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1997-06-02 1997-12-02 1998-06-03 $7700.00 Window Closed / Lapsed

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