Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1999-06-23
2003-07-15
Huang, Evelyn Mei (Department: 1625)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C546S080000
Reexamination Certificate
active
06593335
ABSTRACT:
SUMMARY OF THE INVENTION
In its principle embodiment, the present invention discloses compounds having formula I:
or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof wherein,
n is 0-2;
R
1
is selected from the group consisting of alkyl and haloalkyl;
R
2
is selected from the group consisting of optionally substituted aryl and optionally substituted heteroaryl;
A is selected from the group consisting of hydrogen, alkyl, haloalkyl, cyano, heteroaryl, nitro and —XR
3
;
X is selected from the group consisting of C(O) and S(O)
p
;
p is 1-2;
R
3
is selected from the group consisting of alkyl, haloalkyl, and hydroxy;
R
4
is selected from the group consisting of hydrogen, alkoxyalkoxyalkyl, alkoxyalkyl, alkyl, arylalkoxyalkyl, aryloxyalkyl, haloalkyl, heteroarylalkoxyalkyl, heteroaryloxyalkyl, (NZ
1
Z
2
)alkoxyalkyl, and (NZ
1
Z
2
)alkyl wherein Z
1
and Z
2
are independently selected from the group consisting of hydrogen, alkoxycarbonyl, alkyl, alkylcarbonyl, alkylsulfonyl, aminocarbonyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, formyl, heteroaryl, and heteroarylalkyl or Z
1
, Z
2
and the nitrogen atom to which they are attached form a 3, 4, 5, 6, 7, or 8 membered ring; or
R
3
and R
4
together form a ring selected from the group consisting of a 5-, 6-, or 7-membered carbocyclic ring with 1-2 double bonds and 0-4 substituents selected from the group consisting of alkenyl, alkoxy, alkoxyalkoxy, alkoxyalkyl, alkyl, alkynyl, arylalkoxy, amino, aminoalkoxy, aminoalkyl, haloalkenyl, haloalkyl, halogen, hydroxy, hydroxyalkenyl, hydroxyalkyl, and oxo, and a 5-, 6- or 7-membered sulfur-containing ring with 1-2 double bonds and 0-4 substituents selected from the group consisting of alkenyl, alkoxy, alkoxyalkoxy, alkoxyalkyl, alkyl, alkynyl, arylalkoxy, amino, aminoalkoxy, aminoalkyl, haloalkenyl, haloalkyl, halogen, hydroxy, hydroxyalkenyl, hydroxyalkyl, and oxo; and
R
5
is selected from the group consisting of hydrogen, alkyl and haloalkyl; or R
1
and R
5
together with the ring to which they are attached form a 5-, 6- or 7-membered sulfur-containing ring with 1-2 double bonds and 0-4 substituents selected from the group consisting of alkenyl, alkoxy, alkoxyalkoxy, alkoxyalkyl, alkyl, alkynyl, arylalkoxy, amino, aminoalkoxy, aminoalkyl, haloalkenyl, haloalkyl, halogen, hydroxy, hydroxyalkenyl, hydroxyalkyl, and oxo;
provided that at least one of R
1
and R
5
or R
3
and R
4
forms a ring.
Another embodiment of the present invention relates to pharmaceutical compositions comprising a therapeutically effective amount of a compound of formula I or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof in combination with a pharmaceutically acceptable carrier.
Another embodiment of the invention relates to a method of treating male sexual dysfinction including, but not limited, to male erectile dysfunction and premature ejaculation.
Another embodiment of the invention relates to a method of treating female sexual dysfunction including, but not limited to, female anorgasmia, clitoral erectile insufficiency, vaginal engorgement, dyspareunia, and vaginismus.
Yet another embodiment of the invention relates to a method of treating asthma, epilepsy, hypertension, Raynaud's syndrome, migraine, pain, eating disorders, urinary incontinence, functional bowel disorders, neurodegeneration and stroke comprising administering a therapeutically effective amount of a compound of formula I or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof.
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Carroll William A.
Chen Yiyuan
Drizin Irene
Holladay Mark W.
Kort Michael E.
Abbott Laboratories
Donner B. Gregory
Huang Evelyn Mei
Ward Michael J.
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