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US 2002/0058652 A1Published application
Pharmaceutical compositions and methods for use
AssigneeTargacept, Inc.
InventorsGary Maurice Dull, Jeffrey Daniel Schmitt, Balwinder Singh Bhatti, Craig Harrison Miller
Life of this patent
Estimating the term…
Abstract
The present invention relates to aryl olefinic azacyclic compounds and aryl acetylenic azacyclic compounds, including pyridyl olefinic cycloalkylamines and pyridyl acetylenic cycloalkylamines. The present invention also relates to prodrug derivatives of the compounds of the present invention.
Claims75
A compound of the formula:
- 3
- where each of X and X′ are individually nitrogen, nitrogen bonded to oxygen or carbon bonded to a substituent species characterized as having a sigma m value between about −0.3 and about 0.75;
- m is an integer and n is an integer such that the sum of m plus n is 0, 1, 2 or 3;
- E, EI, EII and EIII individually represent hydrogen or a suitable non-hydrogen substituent;
- and Q is selected from:
- 4
- where Z′ represents hydrogen or lower alkyl, acyl, alkoxycarbonyl, or aryloxycarbonyl;
- Z″ is hydrogen or lower alkyl;
- and Z′″ is a non-hydrogen substituent;
- the dotted line indicates a carbon-carbon single bond or a carbon-carbon double bond;
- p is 0, 1 or 2;
- q is 0, 1, 2 or 3;
- and j is an integer from 0 to 3.
10 more elements
A compound of the formula:
- 6
- where each of X, X′ and X″ are individually nitrogen, nitrogen bonded to oxygen or carbon bonded to a substituent species characterized as having a sigma m value between about −0.3 and about 0.75;
- A is O, C═O or a covalent bond;
- D is a suitable non-hydrogen substituent species characterized as having a sigma m value between about −0.3 and about 0.75;
- k is 0, 1 or 2;
- Cx is selected from a group consisting of aryl, substituted aryl, heteroaryl, substituted heteroaryl, non-aromatic heterocyclyl, substituted non-aromatic heterocyclyl, non-aromatic heterocyclylalkyl and substituted non-aromatic hetero-cyclylalkyl;
- m is an integer and n is an integer such that the sum of m plus n is 0, 1, 2 or 3;
- E, EI, EII and EIII individually represent hydrogen or a suitable non-hydrogen substituent;
- and Q is selected from:
- 7
- where Z′ represents hydrogen or lower alkyl, acyl, alkoxycarbonyl, or aryloxycarbonyl;
- Z″ is hydrogen or lower alkyl;
- and Z′″ is a non-hydrogen substituent;
- the dotted line indicates a carbon-carbon single bond or a carbon-carbon double bond;
- p is 0, 1 or 2;
- q is 0, 1, 2 or 3;
- and j is an integer from 0 to 3.
14 more elements
A pharmaceutical composition incorporating a compound of:
- 9
- where each of X and X′ are individually nitrogen, nitrogen bonded to oxygen or carbon bonded to a substituent species characterized as having a sigma m value between about −0.3 and about 0.75;
- m is an integer and n is an integer such that the sum of m plus n is 0, 1, 2 or 3;
- E, EI, EII and EIII individually represent hydrogen or a suitable non-hydrogen substituent;
- and Q is selected from:
- 10
- where Z′ represents hydrogen or lower alkyl, acyl, alkoxycarbonyl, or aryloxycarbonyl;
- Z″ is hydrogen or lower alkyl;
- and Z′″ is a non-hydrogen substituent;
- the dotted line indicates a carbon-carbon single bond or a carbon-carbon double bond;
- p is 0, 1 or 2;
- q is 0, 1, 2 or 3;
- and j is an integer from 0 to 3.
10 more elements
A pharmaceutical composition incorporating a compound of the formula:
- 12
- where each of X, X′ and X″ are individually nitrogen, nitrogen bonded to oxygen or carbon bonded to a substituent species characterized as having a sigma m value between about −0.3 and about 0.75;
- A is O, C═O or a covalent bond;
- D is a suitable non-hydrogen substituent species characterized as having a sigma m value between about −0.3 and about 0.75;
- k is 0, 1 or 2;
- Cx is selected from a group consisting of aryl, substituted aryl, heteroaryl, substituted heteroaryl, non-aromatic heterocyclyl, substituted non-aromatic heterocyclyl, non-aromatic heterocyclylalkyl and substituted non-aromatic hetero-cyclylalkyl;
- m is an integer and n is an integer such that the sum of m plus n is 0, 1, 2 or 3;
- E, EI, EII and EIII individually represent hydrogen or a suitable non-hydrogen substituent;
- and Q is selected from:
- 13
- where Z′ represents hydrogen or lower alkyl, acyl, alkoxycarbonyl, or aryloxycarbonyl;
- Z″ is hydrogen or lower alkyl;
- and Z′″ is a non-hydrogen substituent;
- the dotted line indicates a carbon-carbon single bond or a carbon-carbon double bond;
- p is 0, 1 or 2;
- q is 0, 1, 2 or 3;
- and j is an integer from 0 to 3.
14 more elements
A method for treating a central nervous system disorder, said method comprising administering an effective amount of a compound having the formula:
- 15
- where each of X and X′ are individually nitrogen, nitrogen bonded to oxygen or carbon bonded to a substituent species characterized as having a sigma m value between about −0.3 and about 0.75;
- m is an integer and n is an integer such that the sum of m plus n is 0, 1, 2 or 3;
- E, EI, EII and EIII individually represent hydrogen or a suitable non-hydrogen substituent;
- and Q is selected from:
- 16
- where Z′ individually represent hydrogen or lower alkyl, acyl, alkoxycarbonyl, or aryloxycarbonyl;
- Z″ is hydrogen or lower alkyl;
- and Z′″ is a non-hydrogen substituent;
- the dotted line indicates a carbon-carbon single bond or a carbon-carbon double bond;
- p is 0, 1 or 2;
- q is 0, 1, 2 or 3;
- and j is an integer from 0 to 3.
10 more elements
A method for treating a central nervous system disorder, said method comprising of the administration of an effective amount of a compound having the formula:
- 18
- where each of X, X′ and X″ are individually nitrogen, nitrogen bonded to oxygen or carbon bonded to a substituent species characterized as having a sigma m value between about −0.3 and about 0.75;
- A is O, C═O or a covalent bond;
- D is a suitable non-hydrogen substituent species characterized as having a sigma m value between about −0.3 and about 0.75;
- k is 0, 1 or 2;
- Cx is selected from a group consisting of aryl, substituted aryl, heteroaryl, substituted heteroaryl, non-aromatic heterocyclyl, substituted non-aromatic heterocyclyl, non-aromatic heterocyclylalkyl and substituted non-aromatic hetero-cyclylalkyl;
- m is an integer and n is an integer such that the sum of m plus n is 0, 1, 2 or 3;
- E, EI, EII and EIII individually represent hydrogen or a suitable non-hydrogen substituent;
- and Q is selected from:
- 19
- where Z′ individually represent hydrogen or lower alkyl, acyl, alkoxycarbonyl, or aryloxycarbonyl;
- Z″ is hydrogen or lower alkyl;
- and Z′″ is a non-hydrogen substituent;
- the dotted line indicates a carbon-carbon single bond or a carbon-carbon double bond;
- p is 0, 1 or 2;
- q is 0, 1, 2 or 3;
- and j is an integer from 0 to 3.
14 more elements
Dependencies are inferred from the claim text.