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US5397802A Expired / Lapsed US ⏱️ 0.0 years remaining

Gem-dichlorocyclopropanes as antitumor agents

Assignee: University of Oklahoma
•
Filing: 1993-02-22
•
Granted: 1995-03-14
•
Expires: 2013-02-22
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Abstract

Abstract Gem-Dichlorocyclopropanes (Analog II derivatives) which demonstrate antiproliferative activity toward MCF-7 cells, in vitro and are generally not reversed by estradiol or having intrinsic estrogenicity (except the hydroxyphenyl derivative Compound 30). In general the cyclopropane compounds have the formula: <IMAGE> or any pharmaceutically acceptable salt thereof. X is selected from a group consisting of hydrogen and halogen atoms. The group R1 may be a hydrogen atom, an alkyl group, an acyl group, or an arylalkyl group. The group R2 may be a hydrogen atom, an unsubstituted aryl group or a substituted aryl group. The group R3 may be a hydrogen atom, an alkyl group, a cycloalkyl group, a substituted aryl group or an unsubstituted aryl group. The group R4 may be a hydrogen atom, an unsubstituted aryl group or a substituted aryl group. The R4 is absent when R3 is a cycloalkyl group having a first position carbon and a terminal position carbon bonded to the same carbon of the cyclopropane. Further, no more than any two of R2, R3 and R4 has an aryl group.

Inventors

  • 👤 Robert A. Magarian
  • 👤 Joseph T. Pento
  • 👤 May T. Griffin

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-24 14:30
CPC Classifications
C; C07; C07D; C07D295/00; C07D295/04; C07D295/08; C07D295/084; C07D295/088; A; A61; A61K; A61K31/00; A61K31/02; A61K31/025; A61K31/03; C07C; C07C217/00; C07C217/02; C07C217/04; C07C217/06; C07C217/14; C07C217/18; C07C309/00; C07C309/63; C07C309/64; C07C309/65; C07C309/66; C07C2601/00; C07C2601/02

Claims Analysis

Total Claims: 9
Claim 1
Independent Claim 62 words
A cyclopropane compound having the formula: ##STR23## or any pharmaceutically acceptable salt thereof, in which X is a halogen atom; R 1 is a hydrogen; R 2 is a hydroxyphenyl; and R 3 is a cyclopentyl group having the first position carbon and the fifth position carbon bonded to the same carbon of the cyclopropane wherein the R 4 group is absent.
Claim 2
Dependent Claim 62 words
A cyclopropane compound having the formula: ##STR23## or any pharmaceutically acceptable salt thereof, in which X is a halogen atom; R 1 is a hydrogen; R 2 is a hydroxyphenyl; and R 3 is a cyclopentyl group having the first position carbon and the fifth position carbon bonded to the same carbon of the cyclopropane wherein the R 4 group is absent.
Claim 3
Dependent Claim 10 words
The compound of claim 1 in which X is chlorine.
Claim 4
Dependent Claim 78 words
A composition of matter comprising a compound having the formula: ##STR24## or any pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier of sufficient quantity to solubilize the compound, in which: X is a halogen atom; R 1 is a hydrogen; R 2 is a hydroxyphenyl; and R 3 is a cyclopentyl group having the first position carbon and the fifth position carbon bonded to the same carbon of the cyclopropane wherein the R 4 group is absent.
Claim 5
Dependent Claim 78 words
A composition of matter comprising a compound having the formula: ##STR24## or any pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier of sufficient quantity to solubilize the compound, in which: X is a halogen atom; R 1 is a hydrogen; R 2 is a hydroxyphenyl; and R 3 is a cyclopentyl group having the first position carbon and the fifth position carbon bonded to the same carbon of the cyclopropane wherein the R 4 group is absent.
Claim 6
Independent Claim 76 words
A method of increasing uterine growth in a mammal comprising administering to the mammal an effective amount of one or more of the compounds having the formula: ##STR25## or any pharmaceutically acceptable salt thereof, in which X is a halogen atom; R 1 is a hydrogen; R 2 is a hydroxyphenyl; and R 3 is a cyclopentyl group having the first position carbon and the fifth position carbon bonded to the same carbon of the cyclopropane.
Claim 7
Independent Claim 76 words
A method of increasing uterine growth in a mammal comprising administering to the mammal an effective amount of one or more of the compounds having the formula: ##STR25## or any pharmaceutically acceptable salt thereof, in which X is a halogen atom; R 1 is a hydrogen; R 2 is a hydroxyphenyl; and R 3 is a cyclopentyl group having the first position carbon and the fifth position carbon bonded to the same carbon of the cyclopropane.
Claim 8
Dependent Claim 10 words
The method of claim 4 in which X is chlorine.
Claim 9
Dependent Claim 21 words
The method of claim 4 wherein the compound further comprises a pharmaceutically acceptable carrier of sufficient quantity to solubilize the compound.

References Cited (Backward Citations)

No citation records indexed.

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1998-03-13 1998-09-12 1999-03-14 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 2002-03-13 2002-09-12 2003-03-14 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2006-03-13 2006-09-12 2007-03-14 $7700.00 Window Closed / Lapsed

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