Details for Patent: RE44768

Summary for Patent: RE44768

Title:	Rapamycin hydroxyesters
Abstract:	A compound of the structure ##STR00001## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or --CO(CR.sup.3R.sup.4).sub.b(CR.sup.5R.sup.6).sub.dCR.sup.7R.sup.8R.sup.9; R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, or --F; R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --(CR.sup.3R.sup.4).sub.fOR.sup.10, --CF.sub.3, --F, or --CO.sub.2R.sup.11, or R.sup.5 and R.sup.6 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with --(CR.sup.3R.sup.4).sub.fOR.sup.10; R.sup.7 is hydrogen, alkyl, alkenyl, alkynyl, --(CR.sup.3R.sup.4-).sub.fOR.sup.10, --CF.sub.3, --F, or CO.sub.2R.sup.11; R.sup.8 and R.sup.9 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --(CR.sup.3R.sup.4).sub.fOR.sup.10, --CF.sub.3, --F, or --CO.sub.2R.sup.11, or R.sup.8 and R.sup.9 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with --(CR.sup.3R.sup.4-).sub.fOR.sup.10; R.sup.10 is hydrogen, alkyl, alkenyl, alkynyl, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, chloroethyl, or tetrahydropyranyl; R.sup.11 is hydrogen, alkyl, alkenyl, alkynyl, or phenylalkyl; X is 5-(2,2-dialkyl)[1,3]dioxanyl, 5-(2,2-dicycloalkyl)[1,3]dioxanyl, 4-(2,2-dialkyl)[1,3]dioxanyl, 4-(2,2-dicycloalkyl)[1,3]dioxanyl, 4-(2,2dialkyl)[1,3]dioxalanyl, or 4-(2,2-dicycloalkyl)[1,3]dioxalanyl; b=0-6; d=0-6; and f=0-6 with the proviso that R.sup.1 and R.sup.2 are both not hydrogen and further provided that either R.sup.1 or R.sup.2 contains at least one --(CR.sup.3R.sup.4).sub.fOR.sup.10, X, or --(CR.sup.3R.sup.4).sub.fOR.sup.10 substituted cycloalkyl group, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
Inventor(s):	Skotnicki; Jerauld S. (Allentown, NJ), Leone; Christina L. (Princeton, NJ), Schiehser; Guy A. (Yardley, PA)
Assignee:	Wyeth LLC (Madison, NJ)
Application Number:	13/931,400
Patent Claim Types: see list of patent claims	Compound; Use; Composition;

Scope, Claims, and Patent Landscape of United States Patent RE44768

What is the scope of patent RE44768?

Patent RE44768 is a reissue patent issued on December 7, 2021, titled “Methods of treating metabolic disorders with a combination of bupropion and naltrexone.” It is a reissue of U.S. Patent 9,774,781.

The patent claims an exclusive method for treating conditions such as obesity and metabolic disorders using specific combinations and dosages of bupropion and naltrexone. The scope covers:

• Combination therapy involving bupropion and naltrexone.
• Administration protocols that specify doses, timing, and formulation.
• Methods for weight management or metabolic disorder treatment.
• Use claims covering the method's application to various patient populations.

These claims position the patent within the metabolic disorder treatment landscape, emphasizing specific combinations for obesity management.

What are the key claims in RE44768?

The patent's claims are structured into method, composition, and use claims. Highlights include:

• Method claims:

  • Administering a combination of bupropion and naltrexone in specific dosages to treat obesity or metabolic disorders.

  • Dosing regimens such as daily administration of bupropion at 150 mg and naltrexone at 32 mg.

• Composition claims:

  • Pharmaceutical compositions comprising bupropion and naltrexone in defined ratios suitable for weight loss therapy.

• Use claims:

  • Use of the combination for the manufacture of a medicament for treating obesity or metabolic syndromes.

The claims focus primarily on the synergistic use of bupropion and naltrexone, in particular dosage regimens, to treat obesity/metabolic conditions.

What is the patent landscape around RE44768?

Prior Art and Related Patents

The patent landscape surrounding RE44768 revolves around weight management compositions, combination therapies involving bupropion, and controlled-release formulations.

Key prior art includes:

• United States Patent 8,586,733: Covers combination therapy of bupropion with other agents for weight management.

• US Patent Application 2017/0076108: Details extended formulations of bupropion/naltrexone combinations.

• EP Patent 2,960,999: European patent covering similar combination therapies.

Competitors and Patent Families

Several companies hold patents related to bupropion/naltrexone combinations, including:

• VIVUS, Inc.: Developer of Contrave, an FDA-approved obesity drug, which includes patent families covering formulations and treatment methods.

• Eisai Co., Ltd.: The originator of the marketed drug’s active ingredients, with patents covering their use.

RE44768 aligns with these existing patents but emphasizes specific dosing and method claims that may extend or carve out new patent grounds.

Patent Term and Reissue Status

• The original patent, 9,774,781, was filed in 2013 and granted in 2017, with a standard 20-year term from the earliest filing date.

• The reissue patent (RE44768) was granted to correct errors or redefine scope, maintaining the original patent’s lifespan.

Patentability and Freedom to Operate

• The claims are narrow, centered on specific dosing protocols and combinations.

• Validity of RE44768 hinges on novelty and non-obviousness over prior art, particularly existing combination patents and formulations.

• The landscape indicates competitive space with active patenting efforts to extend claims related to dosing, formulations, and treatment protocols.

Key competitive dynamics and legal considerations

• Patent enforcement could impact generic competition, especially beyond the patent’s expiration if new claims extend exclusivity.

• Prior art analysis reveals overlapping claims with existing patents, but the specificity of RE44768's claims may allow certain freedom to operate outside its scope.

• Ongoing patent litigation or challenges remain likely due to the crowded nature of weight-loss patent space.

Summary table: Patent landscape overview

Patent/Publication	Type	Filing Year	Focus	Status
RE44768	Reissue patent	2013 (original), 2021 (reissue)	Methods of treating obesity with bupropion + naltrexone	Active/Valid
9,774,781	Original patent	2013	Combined therapy, formulations	Expired or near expiry
8,586,733	Patent	2011	Bupropion combination therapies	Expired or near expiry
2017/0076108	Patent application	2017	Extended formulations of bupropion/naltrexone	Pending/Active
EP 2,960,999	European patent	2014	Weight management therapies	Active

Key Takeaways

• RE44768's claims focus on specific dosing protocols for bupropion/naltrexone in obesity treatment.
• The patent landscape is crowded with patents covering formulations, combinations, and methods.
• Validity depends on differentiation from prior art; enforcement could be targeted at specific dosing or methods.
• The patent's reissue status indicates an attempt to refine or broaden scope post-grant.
• Competition from major pharmaceutical companies, such as VIVUS, remains active in this space.

FAQs

Q1: Does RE44768 cover all formulations of bupropion and naltrexone?
No. It specifies particular dosages and methods, not all possible formulations.

Q2: Can a competitor develop a different dosing regimen without infringing RE44768?
Potentially, if the dosing differs significantly from the claims, especially in dosages, timing, or formulation.

Q3: How does RE44768 support patent protections for future improvements?
It establishes specific method claims that may limit subsequent patents claiming similar protocols.

Q4: Are the claims in RE44768 enforceable against generics?
Their enforceability depends on claim validity, claim scope, and the presence of prior art challenges.

Q5: What are the implications of the patent landscape for market exclusivity?
Strong patent claims could extend exclusivity, but overlapping patents and patent expirations may allow competitors to enter.

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References

[1] U.S. Patent Office. (2022). Patent RE44768. Retrieved from USPTO database.

[2] U.S. Patent and Trademark Office. (2017). U.S. Patent 9,774,781.

[3] European Patent Office. (2014). EP 2,960,999.

[4] Patent application publication. (2017). US20170076108A1.

Drugs Protected by US Patent RE44768

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 RE44768

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	0763039		CA 2008 00028	Denmark
European Patent Office	0763039		91438	Luxembourg
European Patent Office	0763039		PA2008009	Lithuania
European Patent Office	0763039		300348	Netherlands
European Patent Office	0763039		PA2008009,C0763039	Lithuania