Therapeutic compounds and methods of use
View Patent ↗The invention relates to protein binding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C disorders, including diseases and disorders mediated by GPCRs.
1. A method of treating a GPCR-mediated disorder in a subject comprising administering to the subject identified as in need thereof a APT compound of the formula:
wherein,
R 1 is independently 3-halophenyl, 3-haloalkylphenyl or 3-alkoxyphenyl, wherein the 3-halophenyl, 3-haloalkylphenyl, or 3-alkoxyphenyl are each optionally substituted with 1, 2, or 3 independent halo, alkoxy, or CF 3 ;
R 2 is H;
or salt thereof.
2. The method of claim 1 , wherein the APT compound is a compound of Table 1 or salt thereof:
TABLE 1
Compounds:
Formula I
APT-type PAT #
R 1
R 2
33 (CF 3 -5APT)
m-CF 3 —C 6 H 4
H
34 (OCH 3 -5APT)
m-OCH 3 —C 6 H 4
H
35 (Cl-5APT)
m-Cl—C 6 H 4
H.
3. The method of claim 1 , wherein the disorder is a neuropsychiatric disorder, obesity, addiction, anxiety, depression, schizophrenia, sleep disorder, a neurodegenerative disorder, Parkinson's Disease, Alzheimer's Disease, a neurological disorder, epilepsy, a cardiovascular disorder, hypertension, a gastrointestinal disorder, irritable bowel syndrome, a genitor-urinary tract disorder, or bladder control disorder.
4. The method of claim 1 , wherein the disorder is cocaine addiction.
5. The method of claim 1 , wherein the disorder is obesity.
6. The method of claim 1 , wherein R 1 is substituted 3-halophenyl, 3-haloalkylphenyl or 3-alkoxyphenyl, wherein the 3-halophenyl, 3-haloalkylphenyl, or 3-alkoxyphenyl are each substituted with 1, 2, or 3 independent halo, alkoxy, or CF 3 ; and R 2 is H.
7. A method of treating obesity in a subject comprising administering to the subject identified as in need thereof a APT compound of the formula:
wherein,
R 1 is independently 3-halophenyl, 3-haloalkylphenyl or 3-alkoxyphenyl, wherein the 3-halophenyl, 3-haloalkylphenyl, or 3-alkoxyphenyl are each optionally substituted with 1, 2, or 3 independent halo, alkoxy, or CF 3 ;
R 2 is H;
or salt thereof.
8. The method of claim 7 , wherein the APT compound is a compound of Table 1 or salt thereof:
TABLE 1
Compounds:
APT-type PAT #
R 1
R 2
33 (CF 3 -5APT)
m-CF 3 —C 6 H 4
H
34 (OCH 3 -5APT)
m-OCH 3 —C 6 H 4
H
35 (Cl-5APT)
m-Cl—C 6 H 4
H.
9. The method of claim 7 , wherein R 1 is 3-halophenyl, 3-haloalkylphenyl or 3-alkoxyphenyl, wherein the 3-halophenyl, 3-haloalkylphenyl, or 3-alkoxyphenyl are each substituted with 1, 2, or 3 independent halo, alkoxy, or CF 3 ; and R 2 is H.