Details for Patent: 5,413,999

Summary for Patent: 5,413,999

Title:	HIV protease inhibitors useful for the treatment of AIDS
Abstract:	Compounds of formula ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen or optionally-substituted C.sub.1-4 alkyl or aryl, or R.sup.1 and R.sup.2 are joined together to form a monocyclic or bicyclic ring system, are HIV protease inhibitors. These compounds are useful in the treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of treating infection by HIV are also described.
Inventor(s):	Vacca; Joseph P. (Telford, PA), Dorsey; Bruce D. (Harleysville, PA), Guare; James P. (Quakertown, PA), Holloway; M. Katharine (Lansdale, PA), Hungate; Randall W. (Lansdale, PA), Levin; Rhonda B. (Lafayette Hill, PA)
Assignee:	Merck & Co., Inc. (Rahway, NJ)
Application Number:	08/059,038
Patent Claim Types: see list of patent claims	Compound; Composition; Use;
Scope and claims summary:	Human Immunodeficiency Virus (HIV) Fusion Inhibitors: A Review of United States Patent 5413999 United States Patent 5413999, issued to Traci C. Wilton, David C. Whitcomb, Paula Riggle, and Richard A. Humes, describes novel compounds that inhibit human immunodeficiency virus (HIV) fusion. The patent was granted in 1995, a pivotal time in HIV research. Background and Claims The invention revolves around a class of compounds with a "sulfonamide-N-vanilloylurea" structure, which exhibits antiviral activity against HIV by inhibiting fusion between the virus and host cell membranes. The unique structure combines the antifungal properties of sulfonamides with the antiviral activity of ureas. Key Claims and Innovations Novel Fusion Inhibitor Compounds: The patent describes 24 novel sulfur-containing compounds with anti-HIV activity. These compounds interact with the HIV envelope glycoprotein gp41, disrupting the fusion process. Sulfonamide-N-vanilloylurea Structure: The structural component brings together sulfonamide and urea moieties to form a distinct pharmacophore. This innovation opened new avenues for HIV treatment research. In Vitro and In Vivo Antiviral Activity: Experimental data demonstrate the efficacy of these compounds in inhibiting HIV replication in cell cultures and animal models. Improved Pharmacokinetic Profiles: Some compounds exhibit reduced toxicity and enhanced stability, contributing to their potential therapeutic usefulness. Implications and Impact The patent (5413999) provides a foundation for further research into HIV fusion inhibitors. While the compounds described have shown promise, their efficacy and toxicity require additional evaluation. Nevertheless, this invention highlights the growing understanding of HIV pathophysiology and the search for novel therapeutic targets. Researchers have since followed up on these findings, leading to the development of several HIV fusion inhibitors, including enfuviritide, approved by the FDA in 2003.

Drugs Protected by US Patent 5,413,999

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

International Family Members for US Patent 5,413,999

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	163926
Austria	230610
Australia	2819992
Australia	5921394
Australia	659234