Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2002-07-30
2004-10-26
Padmanabhan, Sreeni (Department: 1617)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S250000, C514S214010, C514S296000
Reexamination Certificate
active
06809112
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention is a method of treating sexual disturbances using the compounds of U.S. Pat. No. 5,273,975.
2. Description of the Related Art
There are a number of diseases/conditions which directly affect the sexual lives of humans and animals. These include orgasmic disorders, lack of interest in sex and erectile dysfunction in males. In addition there are a number of diseases/conditions which indirectly affect the sexual lives of humans. There are a few pharmaceutical agents to treat this diseases/conditions and others in clinical development.
U.S. Pat. No. 5,273,975 discloses that the compounds (A) of the present invention are useful to stimulate sexual activity and to alleviate impotence. The useful dosage range disclosed in U.S. Pat. No. 5,273,975 is “at least 10 mg up to about 1200 mg per day”. The operable dosage range in the present invention is considerably lower. The compounds of U.S. Pat. No. 5,273,975 have been used in clinical trials to prove their usefulness in treating Parkinson's disease at a dose of 30 mg/person. Compounds (A) of the present invention are used at a dose of less than 8 mg in treating the sexual disturbances of the present invention. U.S. Pat. No. 5,273,975 generically discloses compounds where the variable substituent “A” can be either a carbonyl group (—CO—) or a thiocarbonyl (—CS—).
U.S. Pat. No. 5,250,534 discloses sildenafil (VIAGRA®). The compounds (A) of the present invention are quite different chemically than sildenafil. International Publication WO94/282902 discloses the use of sildenafil for treating male impotence.
U.S. Pat. No. 4,127,118 discloses the intracavernosal injection of a vasodilator for enhancing an erection of the penis. PGE1 is a vasodilator and is sold as CAVERJECT® to treat male erectile dysfunction. The compounds (A) of the present invention are not prostaglandins and are not injected into the penis.
International Journal of Impotence Research,
10 (Supplement 3), August 1998, Abstracts #417 and 419 disclose that apomorphine, which is available in a number of countries to treat Parkinson's Disease, is in late-stage development as a sublingual formulation for treating male erectile dysfunction. The compounds (A) used in the present invention are not apomorphine analogs. U.S. Pat. No. 5,770,606 discloses sublingual use of apomorphine for treating erectile dysfunction.
U.S. Pat. No. 5,541,211 discloses that yohimbine can be used to treat erectile dysfunction. The compounds of formula (A) are quite different chemically as compared to yohimbine.
U.S. Pat. No. 4,801,587 discloses that phentolamine (VASOMAX®) which is available in a number of countries for treating hypertension is also useful for treating erectile dysfunction. The compounds of formula (A) are quite different chemically as compared to phentolamine. In addition, the compounds of formula (A) are not applied either topically to the penis nor intra-urethrally.
U.S. Pat. No. 5,773,020 discloses that intraurethral PGE1 (MUSE) is useful for treating erectile dysfunction. Compounds (A) are not prostaglandins and are not administered intraurethrally.
Brain Research,
55, 383-389 (1973) reports on the sexually stimulating effect of L-DOPA given to male rats and conjuctures that it may be the reason that hypersexuality occasionally is seen in patients with Parkinson's syndrome during L-DOPA treatment.
SUMMARY OF INVENTION
Disclosed is a method of treating sexual disturbances in a human who is in need of such treatment which comprises administering a sexually therapeutically effective amount of a compound of the formula (A)
where
R
1
, R
2
and R
3
are the same or different and are: —H, C
1
-C
6
alkyl, C
3
-C
5
alkenyl, C
3
-C
5
alkynyl, C
3
-C
5
cycloalkyl, C
4
-C
10
cycloalkyl, phenyl substituted C
1
-C
6
alkyl, —NR
1
R
2
where R
1
and R
2
are cyclized with the attached nitrogen atom to produce pyrrolidiyl, piperidinyl, morphoninyl, 4-methyl piperazinyl or imidazolyl;
X is: —H, C
1
-C
6
alkyl, —F, —Cl, —Br, —I, —OH, C
1
-C
6
alkoxy, cyano, carboxamide, carboxyl, (C
1
-C
6
alkoxy)carbonyl;
A is: CH, CH
2
, CH-(halogen) where halogen is —F, —Cl, —Br, —I, CHCH
3
, C═O, C═S, C—SCH
3
, C═NH, C—NH
2
, C—NHCH
3
, C—NHCOOCH
3
, C—NHCN, SO
2
, N;
B is: CH
2
, CH, CH-(halogen) where halogen is as defined above, C═O, N, NH, N—CH
3
,
D is: CH, CH
2
, CH-(halogen) where halogen is as defined above, C═O, O, N, NH. N—CH
3
, and n is 0 or 1, and where
is a single or double bond, with the provisos:
(1) that when n is 0, and
A is CH
2
, CH-(halogen) where halogen is as defined above, CHCH
3
, C═O, C═S, C═NH, SO
2,
; then
D is CH
2
, CH-(halogen) where halogen is as defined above, C═O, O, NH, N—CH
3
;
(2) that when n is 0, and
A is CH, C—SCH
3
, C—NH
2
, C—NHCH
3
, C—NHCOOCH
3
, C—NHCN, N; then
D is CH, N;
(3) that when n is 1, and
A is CH
2
, CH-(halogen) where halogen is as defined above, CHCH
3
, C═O, C═S, C═NH, SO
2
; and
B is CH
2
, CH-(halogen) where halogen is as defined above, C═O, NH, N—CH
3
; then
D is CH
2
, C═O, O, NH, N—CH
3
;
(4) that when n is 1, and
A is CH, C—SCH
3
, C—NH
2
, C—NHCH
3
, C—NHCOOCH
3
, C—NHCN, N; and
B is CH, N; then
D is CH
2
, C═O, O, NH, N—CH
3
;
(5) that when n is 1, and
A is CH
2
, CHCH
3
, C═O, C═S, C═NH, SO
2
, and
B is CH, N; then
D is CH, N; and pharmaceutically acceptable salts thereof to the human.
Also disclosed is a method of inducing mating a non-human mammal which comprises administering a sexually mating amount of a compound of the formula (A) and pharmaceutically acceptable salts thereof.
Further disclosed is a method of treating a sexual deficiency state in a human who has epilepsy, craniopharyngioma, hypogonadism or who has had a hysterectomyoophorectomy, hysterectomy or oophorectomy which comprises administering a sexually therapeutically effective amount of a compound of the formula (A) and pharmaceutically acceptable salts thereof.
Additionally disclosed is a method of increasing sexual desire, interest or performance in a human who is desirous thereof which comprises administering a sexually useful effective amount of a compound of the formula (A) and pharmaceutically acceptable salts thereof.
Disclosed is (5R)-5-(methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinoline-2(1H)-thione and pharmaceutically acceptable salts thereof.
REFERENCES:
patent: 4127118 (1978-11-01), Latorre
patent: 4801587 (1989-01-01), Voss et al.
patent: 5250534 (1993-10-01), Bell et al.
patent: 5273975 (1993-12-01), Moon et al.
patent: 5541211 (1996-07-01), Pertovaara et al.
patent: 5770606 (1998-06-01), El-Rashidy et al.
patent: 5773020 (1998-06-01), Place et al.
patent: WO94/282902 (1994-12-01), None
Clark et al., Science, Aug. 24, 1984; 225(4664):847-849.*
International Journal of Impotence Research, 10 (Supplement), Aug. 1998, Abstracts #417 and 419Brain Research, 55, 383-389 (1973).
Diagnostic and Statistical Manual of Mental Disorders, FourthEdition, (DSM-IV), American Psychiatric Association, Washington DC (1994).
DSM-IV Guidebook, American Psychiatric Press, Inc., Washington DC 1995.
McCall Robert B.
Meglasson Martin Durham
Hui San-ming
McDonnell Boehnen & Hulbert & Berghoff LLP
Padmanabhan Sreeni
Pharmacia & Upjohn Company
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