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Details for Patent: 5,202,333

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Patent 5,202,333 protects ALOXI and is included in one NDA. There are four tentative approvals for the compound protected by this patent. Additional details are available via the generic ingredient links below.

Protection for ALOXI has been extended six months for pediatric studies, as indicated by the *PED designation in the table below.

This patent has thirty-four patent family members in twenty-two countries.

Summary for Patent: 5,202,333

Title: Tricyclic 5-HT.sub.3 receptor antagonists
Abstract:The present invention is directed to 5-HT.sub.3 receptor antagonist compounds of formula I: ##STR1## in which the dashed line denotes an optional double bond; n is 1, 2 or 3; p is 0, 1, 2 or 3; q is 0, 1 or 2; each R.sup.1 is independently selected from halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, amino carbonyl, (lower alkyl)amino, di(lower alkyl)amino, and (lower alkanoyl)amino; each R.sup.2 is lower alkyl; and R.sup.3 is a group selected from Formulae (a), (b), (c) and (d): ##STR2## in which u is 0 or 1; z is 1, 2 or 3; and R.sup.4 is C.sub.1-7 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.1-2 alkyl, or a group (CH.sub.2).sub.t R.sup.5 where t is 1 or 2 and R.sup.5 is thienyl, pyrrolyl, or furyl, each optionally further substituted by one or two substituents selected from C.sub.1-6 alkyl, C.sub.1-6 alkoxy, trifluoromethyl or halogen, or is phenyl optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy, and C.sub.1-4 alkyl optionally substituted by hydroxy, C.sub.1-4 alkoxy, carboxy, esterified carboxy or in vivo hydrolyzable acyloxy; and the pharmaceutically acceptable salts, individual isomers, mixtures of isomers, processes for preparation, compositions, and methods of use thereof.
Inventor(s): Berger; Jacob (Los Altos Hills, CA), Clark; Robin D. (Palo Alto, CA), Eglen; Richard M. (Mountain View, CA), Smith; William L. (Sunnyvale, CA), Weinhardt; Klaus K. (San Francisco, CA)
Assignee: Syntex (U.S.A.) Inc. (Palo Alto, CA)
Application Number:07/704,565
Patent Claim Types:
see list of patent claims
Compound; Use; Composition;

Applicant Tradename Generic Name Dosage NDA Approval Date Type RLD Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use
Helsinn Hlthcare
ALOXI
palonosetron hydrochloride
INJECTABLE;INTRAVENOUS021372-002Feb 29, 2008RXYes5,202,333*PED► subscribe
Helsinn Hlthcare
ALOXI
palonosetron hydrochloride
INJECTABLE;INTRAVENOUS021372-001Jul 25, 2003RXYes5,202,333*PED► subscribe
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International Patent Family for Patent: 5,202,333

Country Document Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Austria124698► subscribe
Australia642178► subscribe
Australia6696390► subscribe
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The estimated expiration dates shown above are derived by simply adding 20 years to the priority date.
Due to the complexity of determining patent expirations even in a single country, compounded by the diversity of global patent laws, it is advisable to have patent counsel verify freedom to operate.

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