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US4379783A Expired / Lapsed US ⏱️ 0.0 years remaining

Trialkylsilicon-containing phenylcycloalkane analgesics

Assignee: Pfizer Inc
•
Filing: 1982-05-24
•
Granted: 1983-04-12
•
Expires: 2002-05-24
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Abstract

Abstract A compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: G is hydroxymethylene or carbonyl; R is hydrogen or alkanoyl having from one to seven carbon atoms; R 1 and R 2 are each methyl or ethyl; R 3 is an alkyl of from five to seven carbon atoms; m is 0 or 1; and n is 1, 2 or 3. A preferred compound is one in which m is zero, n is one or G is hydroxymethylene. Also preferred are compounds in which R 1 and R 2 are methyl. Additional preferred compounds include those where R is hydrogen or acetyl. A preferred compound is Z-3-(4'-(dimethyl-n-hexylsilyl)-2'-hydroxyphenyl)cyclohexanol. The invention further comprises pharmaceutical compositions containing these compounds. In accordance with the present invention, these compounds when administered in an effective amount to mammals are useful as CNS agents including analgesics, tranquilizers, sedatives, anticonvulsants, antidiarrheals, antiemetics and antianxiety agents.

Inventors

  • 👤 Lawrence S. Melvin, Jr.
  • 👤 Michael R. Johnson

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-03 19:50
CPC Classifications
C; C07; C07F; C07F7/00; C07F7/02; C07F7/08; C07F7/0803; C07F7/081; A; A61; A61P; A61P25/00; A61P25/04; A61P25/20

Claims Analysis

Total Claims: 12
Claim 1
Independent Claim 63 words
A compound having the formula ##STR8## or a pharmaceutically acceptable salt thereof, wherein: G is hydroxymethylene or carbonyl; R is hydrogen or alkanoyl having from one to seven carbon atoms; R 1 and R 2 are methyl or ethyl; R 3 is an alkyl of from five to seven carbon atoms; m is 0 or 1; and n is 1, 2 or 3.
Claim 2
Dependent Claim 63 words
A compound having the formula ##STR8## or a pharmaceutically acceptable salt thereof, wherein: G is hydroxymethylene or carbonyl; R is hydrogen or alkanoyl having from one to seven carbon atoms; R 1 and R 2 are methyl or ethyl; R 3 is an alkyl of from five to seven carbon atoms; m is 0 or 1; and n is 1, 2 or 3.
Claim 3
Dependent Claim 10 words
A compound according to claim 1 wherein m is zero.
Claim 4
Dependent Claim 10 words
A compound according to claim 1 wherein n is 1.
Claim 5
Dependent Claim 10 words
A compound according to claim 1 wherein G is hydroxymethyl.
Claim 6
Dependent Claim 14 words
A compound according to claim 1 wherein R 1 and R 2 are methyl.
Claim 7
Dependent Claim 10 words
A compound according to claim 1 wherein R is hydrogen.
Claim 8
Dependent Claim 10 words
A compound according to claim 1 wherein R is acetyl.
Claim 9
Dependent Claim 27 words
A compound according to claim 1 wherein m is zero, n is 1, R 1 and R 2 are methyl, R is hydrogen and G is hydroxymethylene.
Claim 10
Dependent Claim 14 words
A compound according to claim 1 or claim 8 wherein R 3 is n-hexyl.
Claim 11
Dependent Claim 31 words
A pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and an analgesic, tranquilizer, sedative, antianxiety, anticonvulsant, antidiarrheal or antiemetic effective amount of a compound of claim 1 or claim 2.
Claim 12
Dependent Claim 24 words
A method for producing analgesia in a mammal which comprises administering thereto an analgesia-producing quantity of a compound of claim 1 or claim 2.

References Cited (Backward Citations)

US3558683A Cited
US3491137A Cited
US3586705A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1986-04-11 1986-10-11 1987-04-12 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1990-04-11 1990-10-11 1991-04-12 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1994-04-11 1994-10-11 1995-04-12 $7700.00 Window Closed / Lapsed

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