Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
1999-08-30
2001-06-12
Shah, Mukund J. (Department: 1624)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
C514S254040, C514S254090, C544S368000, C544S376000, C544S358000, C548S469000, C548S503000, C548S212000, C548S214000
Reexamination Certificate
active
06245765
ABSTRACT:
BACKGROUND OF THE INVENTION
The invention is directed to the mesylate dihydrate salts of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6chloro-1,3-dihydro-2H-indol-2-one (hereafter “ziprasidone mesylate dihydrates”), pharmaceutical compositions containing one or both of the ziprasidone mesylate dihydrates, and methods of administering the ziprasidone mesylate dihydrates to treat psychotic diseases. Ziprasidone is a potent antipsychotic agent and is therefore useful for treating various disorders including schizophrenia, anxiety and migraine pain. U.S. Pat. No. 5,312,925 refers to ziprasidone hydrochloride monohydrate, and states that ziprasidone hydrochloride monohydrate is substantially hygroscopically stable, which alleviates potential problems associated with weight changes of the active ingredient during the manufacture of capsules or tablets. U.S. Pat. No. 5,312,925 is herein incorporated by reference in its entirey. Ziprasidone hydrochloride monohydrate, however, has low aqueous solubility and, as a result, is more appropriate for capsule or tablet formulation than for injectable dosage forms.
The ziprasidone mesylate dihydrates also possess hygroscopic stability. The ziprasidone mesylate dihydrates have the added advantage of having significantly greater aqueous solubility than the hydrochloride monohydrate, which makes the mesylate dihydrates more suitable for injectable dosage forms than the hydrochloride monohydrate.
SUMMARY OF THE INVENTION
The present invention relates to the mesylate dihydrate salts of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-chloro-1,3-dihydro-2H-indol-2-one.
This invention also relates to a pharmaceutical composition for the treatment of a psychotic disorder, such as schizophrenia, anxiety or migraine pain, comprising an amount of the mesylate dihydrate salts of 5-(2-(4-(1,2-benzisothiazol-3yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydro-2H-indol-2-one that is effective in treating said psychotic disorder, and a pharmaceutically acceptable carrier.
This invention also relates to a method of treating a psychotic disorder, such as schizophrenia, anxiety or migraine pain, in a mammal, including a human, comprising administering to said mammal an amount of the mesylate dihydrate salts of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)chloro-1,3-dihydro-2H-indol-2-one that is effective in treating said disorder.
REFERENCES:
patent: 5312925 (1994-05-01), Allen et al.
patent: 0281309 A1 (1988-09-01), None
patent: 0584903 A1 (1994-03-01), None
patent: 0586191 A1 (1994-03-01), None
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Howard H. R., et al., (1996) 3-Benzisothiazolylpiperazine Derivatives as Potential Atypical Antipsychotic Agents, Journal of Medicinal Chemistry, vol. 39, pp. 143-148.
Busch Frank R.
Rose Carol A.
Shine Russell J.
Ginsburg Paul H.
Konstas Kristina L.
Patel Sudhaker B.
Pfizer Inc
Richardson Peter C.
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