USPatentGranted
B2Tenofovir alafenamide hemifumarate
Granted 15 Apr 2014 · 2 office actions
Assignee: Gilead Sciences
Law firm: Law firm · Log in to unlock
Attorney: Attorney · Log in to unlock
Inventors: Richard Hung Chiu Yu, Dazhan Liu, Bing Shi, Fang Wang · Examiner: James D Anderson · AU 1629 · TC 1600
Application
13/586,358
filed 15 Aug 2012
Publication
US 20130065856
published 14 Mar 2013
Patent· this page
US 8,697,675
granted 15 Apr 2014
31
Claims
4 independent
56
File wrapper
transactions
2032
20-year term
term adjustment not held
none
Litigation
checked
5
Classifications
C07D473/34, C07F9/6561
11
Citations
11 cites · 0 cited by
Life of the patent
4 dated events⤢ drag to zoom
Prosecutionhover for detail · click to open
Abstract
A hemifumarate form of 9-[(R)-2-[[(S)-[[(S)-1-(isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine (tenofovir alafenamide), and antiviral therapy using tenofovir alafenamide hemifumarate (e.g., anti-HIV and anti-HBV therapies).
Claims
31 · 4 independent · depth 431 granted claims
›1.independentTenofovir alafenamide hemifumarate.+23
›2.↳ 1The hemifumarate of claim 1 that has a differential scanning calorimetry (DSC) onset endotherm of 131±2° C.d2+1
›3.↳ 2The hemifumarate of claim 2 that has a DSC onset endotherm of 131±1° C.d3
›6.↳ 1A composition comprising tenofovir alafenamide hemifumarate according to claim 1, wherein the ratio of fumaric acid to tenofovir alafenamide in said c…d2+7
›7.↳ 6The composition of claim 6, wherein the ratio of fumaric acid to tenofovir alafenamide is 0.5±0.05.d3+1
›14.↳ 7The composition of claim 7, which is a solid.d4
›8.↳ 6The composition of claim 6, wherein the ratio of fumaric acid to tenofovir alafenamide is 0.5±0.01.d3+1
›15.↳ 8The composition of claim 8, which is a solid.d4
›9.↳ 6The composition of claim 6, wherein the ratio of fumaric acid to tenofovir alafenamide is about 0.5.d3+1
›16.↳ 9The composition of claim 9, which is a solid.d4
›10.↳ 6The composition of claim 6, which is a solid.d3
›11.↳ 1A pharmaceutical composition comprising the hemifumarate of claim 1 and a pharmaceutically acceptable excipient.d2+4
›12.↳ 11The pharmaceutical composition of claim 11, further comprising an additional therapeutic agent.d3+1
›13.↳ 12The pharmaceutical composition of claim 12, wherein the additional therapeutic agent is selected from the group consisting of human immunodeficiency v…d4
›18.↳ 11A method for treating an HIV infection comprising administering to a subject in need thereof a therapeutically effective amount of the pharmaceutical …d3
›21.↳ 11A method for treating an HBV infection comprising administering to a subject in need thereof a therapeutically effective amount of the pharmaceutical …d3
›17.↳ 1A method for treating a human immunodeficiency virus (HIV) infection comprising administering to a subject in need thereof a therapeutically effective…d2+3
›19.↳ 17The method for treating an HIV infection of claim 17, further comprising administering to the subject one or more additional therapeutic agents select…d3
›22.↳ 17The method for treating an HIV infection of claim 17, wherein the hemifumarate is administered in multiple daily doses.d3
›23.↳ 17The method for treating an HIV infection of claim 17, wherein the hemifumarate is administered in a single daily dose.d3
›20.↳ 1A method for treating a hepatitis B virus (HBV) infection comprising administering to a subject in need thereof a therapeutically effective amount of …d2+2
›24.↳ 20The method for treating an HBV infection of claim 20, wherein the hemifumarate is administered in multiple daily doses.d3
›25.↳ 20The method for treating an HBV infection of claim 20, wherein the hemifumarate is administered in a single daily dose.d3
›26.↳ 1A method for preparing a pharmaceutical composition comprising combining the hemifumarate of claim 1 and a pharmaceutically acceptable excipient to pr…d2
›4.independentTenofovir alafenamide hemifumarate, having an X-ray powder diffraction (XRPD) pattern comprises 2theta values of 6.9±0.2° and 8.6±0.2°.+1
›5.↳ 4The hemifumarate of claim 4, wherein the XRPD pattern comprises 2theta values of 6.9±0.2°, 8.6±0.2°, 11.0±0.2°, 15.9±0.2°, and 20.2±0.2°.d2
›27.independentA method for preparing tenofovir alafenamide hemifumarate comprising admixing a) aprotic organic solvent; b) fumaric acid; c) tenofovir alafenamide; a…+2
›28.↳ 27The method of claim 27, wherein the solvent comprises acetonitrile.d2
›29.↳ 27The method of claim 27, wherein the solution is subjected to a temperature in the range of from about 0° C. to about 75° C.d2
›30.independentA method for preparing tenofovir alafenamide hemifumarate, comprising the steps of:nadmixing a) a solvent comprising water, isopropyl alcohol, acetone…+1
›31.↳ 30The method of claim 30, wherein the solvent comprises acetonitrile and up to about 50% by volume methylene chloride.d2
Classifications
5 codesIPC · International Patent Classification
Section A — Human necessities
- A61K31/685
Section C — Chemistry; metallurgy
- C07D473/34
- C07F9/6561
USPC · US Patent Classification
514/81544/244
Claim changes
SoonComing soonHow the claims changed between publication and grant
See which claims were amended, added or cancelled during examination, with every added and removed word marked.
AmendedAddedCancelledUnchanged
The published claims of this patent are not paired with the granted ones in what we hold.
File wrapper
Pendency
1.7 y
608 days filing → grant
Office actions
1
non-final + final
Responses
1
no RCE
Examiner
James D Anderson
art unit 1629 · TC 1600
Law firm
Citations: 11 back · 0 forward
See the full prosecution history — every USPTO and applicant action on this file, in order.
Log in to unlockTerm & fees
See the term timeline — pendency span, in-force span, the maintenance fees paid and both computed expiry dates.
Log in to unlockPriority chain
2 priority documentsPriority
16 Aug 2011
earliest claimed
›Priority documents — 2
| Type | Document | Date |
|---|---|---|
| provisional | US 61524224 | 16 Aug 2011 |
| related publication | US 20130065856 A1 | 14 Mar 2013 |
Validity challenges
See the validity challenges on record — reexaminations, IPRs and PGRs, with their institution decisions and outcomes.
Log in to unlockCitations
See every patent this one cites and every patent that cites it back — publication, assignee, and how each one was found.
Log in to unlock