US2023055376A1PendingUtilityA1
5-ht2c receptor agonists and compositions and methods of use
Est. expiryJul 31, 2035(~9 yrs left)· nominal 20-yr term from priority
A61P 25/08A61P 3/04A61K 31/55C07D 491/052C07D 223/16A61K 2121/00A61P 25/32A61P 3/10C07D 223/32C07D 491/06
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Claims
Abstract
Provided in some embodiments are compounds of Formula A, as defined herein, that modulate the activity of 5-HT2C receptor. Also provided in some embodiments are methods, such as, for weight management, inducing satiety, and decreasing food intake, and for preventing and treating obesity, antipsychotic-induced weight gain, type 2 diabetes, Prader-Willi syndrome, tobacco/nicotine dependence, drug addiction, alcohol addiction, pathological gambling, reward deficiency syndrome, and sex addiction), obsessive-compulsive spectrum disorders and impulse control disorders (including nail-biting and onychophagia), sleep disorders (including insomnia, fragmented sleep architecture, and disturbances of slow-wave sleep), urinary incontinence, psychiatric disorders (including schizophrenia, anorexia nervosa, and bulimia nervosa), Alzheimer disease, sexual dysfunction, erectile dysfunction, epilepsy, movement disorders (including parkinsonism and antipsychotic-induced movement disorder), hypertension, dyslipidemia, nonalcoholic fatty liver disease, obesity-related renal disease, and sleep apnea.
Claims
exact text as granted — not AI-modified1 .- 50 . (canceled)
51 . A method selected from the group consisting of decreasing food intake in an individual in need thereof, inducing satiety in an individual in need thereof, treating obesity in an individual in need thereof, and weight management in an individual in need thereof, the method comprising administering to the individual a therapeutically acceptable amount of a compound selected from the following compounds and pharmaceutically acceptable salts, solvates, and hydrates thereof:
Com-
pound
No.
Chemical Structure
Chemical Name
102
6,6′-dimethyl-2′,3′,4′,4a′,5′,6′- hexahydro-1′H- spiro[cyclopropane-1,7′- naphtho[1,8-cd]azepine]
103
(S)-6,6′-dimethyl- 2′,3′,4′,4a′,5′,6′-hexahydro- 1′H-spiro[cyclopropane-1,7′- naphtho[1,8-cd]azepine]
104
(R)-6′,6′-dimethyl- 2′,3′,4′,4a′,5′,6′-hexahydro- 1′H-spiro[cyclopropane-1,7′- naphtho[1,8-cd]azepine]
105
8′-fluoro-2′,3′,4′,4a′,5′- pentahydro-1′H- dispiro[cyclopropane-1,6′- cyclopropane-7′,1″- naphtho[1,8-cd]-azepine]
110
(S)-7,7-dimethyl- 1,2,3,4,4a,5,6,7- octahydronaphtho[1,8- cd]azepine
113
(R)-2′,3′,4′,4a′,5′-pentahydro- 1′H-dispiro[cyclopropane-1,6′- cyclopropane-7′,1″- naphtho[1,8-cd]-azepine]
114
(S)-2′,3′,4′,4a′,5′-pentahydro- 1′H-dispiro[cyclopropane-1,6′- cyclopropane-7′,1″- naphtho[1,8-cd]-azepine]
122
(R)-7,7-dimethyl- 1,2,3,4,4a,5,6,7- octahydronaphtho[1,8- cd]azepine
123
(S)-2′,3′,4′,4a′,5′,6′- hexahydro-1′H- spiro[cyclopropane-1,7′- naphtho[1,8-cd]azepine]
128
2′,3′,4′,4a′,5′,6′- hexahydro-1′H- spiro[cyclopropane-1,7′- naphtho[1,8-cd]azepine]
130
2′,3′,4′,4a′,5′-pentahydro-1′H- dispiro[cyclopropane-1,6′- cyclopropane-7′,1″- naphtho[1,8-cd]-azepine]
133
(R)-8′-fluoro- 2′,3′,4′,4a′,5′-pentahydro-1′H- dispiro[cyclopropane-1,6′- cyclopropane-7′,1″- naphtho[1,8-cd]-azepine]
134
(S)-8′-fluoro- 2′,3′,4′,4a′,5′-pentahydro-1′H- dispiro[cyclopropane-1,6′- cyclopropane-7′,1″- naphtho[1,8-cd]-azepine]
135
7,7-dimethyl-1,2,3,4,4a,5,6,7- octahydronaphtho[1,8- cd]azepine
136
(R)-2′,3′,4′,4a′,5′,6′-hexahydro- 1′H-spiro[cyclopropane-1,7′- naphtho[1,8-cd]azepine].
52 . The method of claim 51 , wherein said individual is an obese patient with an initial body mass index ≥30 kg/m 2 .
53 . The method of claim 51 , wherein said individual is an overweight patient with an initial body mass index ≥27 kg/m 2 in the presence of at least one weight related co-morbid condition.
54 . The method of claim 53 , wherein said weight related co-morbid condition is selected from: hypertension, dyslipidemia, cardiovascular disease, glucose intolerance and sleep apnea.
55 . The method of claim 51 , wherein the method is for decreasing food intake in the individual in need thereof.
56 . The method of claim 51 , wherein the method is for inducing satiety in the individual in need thereof.
57 . The method of claim 51 , wherein the method is for the treatment of obesity in the individual in need thereof.
58 . The method of claim 51 , wherein the method is for weight management in the individual in need thereof.
59 . A method selected from the group consisting of treating type 2 diabetes in an individual in need thereof, treating drug and alcohol addiction in an individual in need thereof, and treating a seizure disorder in an individual in need thereof, wherein said seizure disorder is epilepsy or Dravet syndrome, the method comprising administering to the individual a therapeutically effective amount of a compound selected from the following compounds and pharmaceutically acceptable salts, solvates, and hydrates thereof:
Com-
pound
No.
Chemical Structure
Chemical Name
102
6,6′-dimethyl-2′,3′,4′,4a′,5′,6′- hexahydro-1′H- spiro[cyclopropane-1,7′- naphtho[1,8-cd]azepine]
103
(S)-6,6′-dimethyl- 2′,3′,4′,4a′,5′,6′-hexahydro- 1′H-spiro[cyclopropane-1,7′- naphtho[1,8-cd]azepine]
104
(R)-6′,6′-dimethyl- 2′,3′,4′,4a′,5′,6′-hexahydro- 1′H-spiro[cyclopropane-1,7′- naphtho[1,8-cd]azepine]
105
8′-fluoro-2′,3′,4′,4a′,5′- pentahydro-1′H- dispiro[cyclopropane-1,6′- cyclopropane-7′,1″- naphtho[1,8-cd]-azepine]
110
(S)-7,7-dimethyl- 1,2,3,4,4a,5,6,7- octahydronaphtho[1,8- cd]azepine
113
(R)-2′,3′,4′,4a′,5′-pentahydro- 1′H-dispiro[cyclopropane-1,6′- cyclopropane-7′,1″- naphtho[1,8-cd]-azepine]
114
(S)-2′,3′,4′,4a′,5′-pentahydro- 1′H-dispiro[cyclopropane-1,6′- cyclopropane-7′,1″- naphtho[1,8-cd]-azepine]
122
(R)-7,7-dimethyl- 1,2,3,4,4a,5,6,7- octahydronaphtho[1,8- cd]azepine
123
(S)-2′,3′,4′,4a′,5′,6′-hexahydro-1′H-spiro[cyclopropane-1,7′- naphtho[1,8-cd]azepine]
128
2′,3′,4′,4a′,5′,6′-hexahydro- 1′H-spiro[cyclobutane-1,7′-naphtho[1,8-cd]azepine]
130
2′,3′,4′,4a′,5′-pentahydro-1′H- dispiro[cyclopropane-1,6′- cyclopropane-7′,1″- naphtho[1,8-cd]-azepine]
133
(R)-8′-fluoro-2′,3′,4′,4a′,5′- pentahydro-1′H- dispiro[cyclopropane-1,6′- cyclopropane-7′,1″- naphtho[1,8-cd]-azepine]
134
(S)-8′-fluoro-2′,3′,4′,4a′,5′- pentahydro-1′H- dispiro[cyclopropane-1,6′- cyclopropane-7′,1″- naphtho[1,8-cd]-azepine]
135
7,7-dimethyl-1,2,3,4,4a,5,6,7- octahydronaphtho[1,8- cd]azepine
136
(R)-2′,3′,4′,4a′,5′,6′-hexahydro- 1′H-spiro[cyclopropane-1,7′- naphtho[1,8-cd]azepine].
60 . The method of claim 59 , wherein the method is for the treatment of type 2 diabetes in the individual in need thereof.
61 . The method of claim 59 , wherein the method is for the treatment of drug and alcohol addiction in the individual in need thereof.
62 . The method of claim 59 , wherein the method is for the treatment of a seizure disorder in the individual in need thereof, wherein said seizure disorder is epilepsy or Dravet syndrome.
63 . A method selected from the group consisting of decreasing food intake in an individual in need thereof, inducing satiety in an individual in need thereof, treating obesity in an individual in need thereof, and weight management in an individual in need thereof, the method comprising administering to the individual a therapeutically acceptable amount of the following compound and pharmaceutically acceptable salts, solvates, and hydrates thereof: (R)-8′-fluoro-2′,3′,4′,4a′,5′-pentahydro-1′H-dispiro[cyclopropane-1,6′-cyclopropane-7′,1″-naphtho[1,8-cd]-azepine] (Compound 133).
64 . The method of claim 63 , wherein the individual is an obese patient with an initial body mass index ≥30 kg/m 2 .
65 . The method of claim 63 , wherein the individual is an overweight patient with an initial body mass index ≥27 kg/m 2 in the presence of at least one weight related co-morbid condition.
66 . The method of claim 65 , wherein the weight related co-morbid condition is selected from: hypertension, dyslipidemia, cardiovascular disease, glucose intolerance and sleep apnea.
67 . The method of claim 63 , wherein the method is for decreasing food intake in the individual in need thereof.
68 . The method of claim 63 , wherein the method is for inducing satiety in the individual in need thereof.
69 . The method of claim 63 , wherein the method is for the treatment of obesity in the individual in need thereof.
70 . The method of claim 63 , wherein the method is for weight management in the individual in need thereof.
71 . A method selected from the group consisting of treating type 2 diabetes in an individual in need thereof, treating drug and alcohol addiction in an individual in need thereof, and treating a seizure disorder in an individual in need thereof, wherein said seizure disorder is epilepsy or Dravet syndrome, the method comprising administering to the individual a therapeutically effective amount of the following compound and pharmaceutically acceptable salts, solvates, and hydrates thereof: (R)-8′-fluoro-2′,3′,4′,4a′,5′-pentahydro-1′H-dispiro[cyclopropane-1,6′-cyclopropane-7′,1″-naphtho[1,8-cd]-azepine] (Compound 133).
72 . The method of claim 71 , wherein the method is for the treatment of type 2 diabetes in the individual in need thereof.
73 . The method of claim 71 , wherein the method is for the treatment of drug and alcohol addiction in the individual in need thereof.
74 . The method of claim 71 , wherein the method is for the treatment of a seizure disorder in the individual in need thereof, wherein said seizure disorder is epilepsy or Dravet syndrome.Join the waitlist — get patent alerts
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