Composition of a 5-HT2A serotonin receptor modulator useful for the treatment of disorders related thereto
First Claim
1. A pharmaceutical composition comprising:
- a. Form II of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea; and
wherein said Form II of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea has an x-ray powder diffraction pattern comprising a peak expressed in terms of 2θ
, at about 8.2°
, about 11.5°
, about 12.3°
, about 19.9°
, about 20.4°
, about 24.6°
, and about 24.7°
b. an excipient selected from;
PVP and coPVPwherein Form II of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea and said excipient are present in a ratio of between about 1;
20 and about 1;
1 by weight, andwherein the composition comprises less than 0.9 mole % of 1-(2,4-difluorophenyl)-3-(4-methoxy-3-(1-methyl-1H-pyrazol-5-yl)phenyl)urea.
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Abstract
The present invention relates to certain compositions of a 5-HT2A serotonin receptor modulator and methods for their preparation. The compositions disclosed herein are useful for increasing slow wave sleep, improving sleep consolidation, improving sleep maintenance and improving sleep quality, and for treating insomnia and related sleep disorders, dyssomnias, parasomnias and nonrestorative sleep and the like. The compositions disclosed herein are further useful for treating platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, thrombosis, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette'"'"'s syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders and progressive multifocal leukoencephalopathy and the like.
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Citations
22 Claims
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1. A pharmaceutical composition comprising:
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a. Form II of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea; and
wherein said Form II of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea has an x-ray powder diffraction pattern comprising a peak expressed in terms of 2θ
, at about 8.2°
, about 11.5°
, about 12.3°
, about 19.9°
, about 20.4°
, about 24.6°
, and about 24.7°b. an excipient selected from;
PVP and coPVPwherein Form II of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea and said excipient are present in a ratio of between about 1;
20 and about 1;
1 by weight, andwherein the composition comprises less than 0.9 mole % of 1-(2,4-difluorophenyl)-3-(4-methoxy-3-(1-methyl-1H-pyrazol-5-yl)phenyl)urea. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17)
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18. A method for treating agitation or a symptom thereof in an individual in need thereof comprising administering to the individual a therapeutically effective amount of a pharmaceutical composition comprising Form II of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea and an excipient selected from the group consisting of PVP and coPVP.
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19. A method for treating agitation or a symptom thereof in an individual in need thereof, where the individual is a cognitively intact elderly patient, comprising administering to the individual a therapeutically effective amount of a pharmaceutical composition comprising Form II of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea and an excipient selected from the group consisting of PVP and coPVP.
- 20. A method for the treatment of agitation or a symptom thereof in an individual in need thereof suffering from dementia comprising administering to the individual a therapeutically effective amount of a pharmaceutical composition comprising Form II of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea and an excipient selected from the group consisting of PVP and coPVP.
Specification