Organic compounds
AssigneeIntra-Cellular Therapies, Inc.
InventorsPeng LI, Robert DAVIS
Life of this patent
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Abstract
The invention relates to particular substituted deuterated heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.
Claims22
The method according to claim 11, wherein the compound administered is the compound of formula I:
- wherein at least one of R1 and R2, or both, is D, in free or pharmaceutically acceptable salt form.
The method according to claim 11, wherein the compound administered is the compound of formula II:
- wherein at least one of R1 and R2, or both, is D, in free or pharmaceutically acceptable salt form.
The method according to claim 11, wherein the compound administered is the compound of formula III:
- wherein at least one of R1 and R2, or both, is D, in free or pharmaceutically acceptable salt form
(canceled)
The method according to claim 11, wherein R1 is H and R2 is D.
The method according to claim 11, wherein R1 and R2 are both D.
The method according to claim 11, wherein said compound is in pharmaceutically acceptable salt form.
The method according to claim 11, wherein the compound has substantially greater than natural incorporation of deuterium at the indicated deuterium positions of the structure.
The method according to claim 11, wherein the method comprises the administration of a pharmaceutical composition comprising the compound, in free or pharmaceutically acceptable salt form, in combination or association with a pharmaceutically acceptable diluent or carrier.
A method for the treatment of a central nervous system disorder comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula I,
- wherein at least one of R1 and R2, or both, is D;
- or
- a compound of formula II,
- wherein at least one of R1 and R2, or both, is D;
- or
- a compound of formula III,
- wherein at least one of R1 and R2, or both, is D;
- each in free or pharmaceutically acceptable salt form;
- wherein said central nervous system disorder is selected from a group consisting of anxiety, depression, psychosis, schizophrenia, sleep disorders agitation, agitation in dementia, agitation in autism and related autistic disorders, post-traumatic stress disorder, impulse control disorders, and intermittent explosive disorder.
(canceled)
Dependencies are inferred from the claim text.