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Last Updated: March 29, 2024

Claims for Patent: 7,897,635


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Summary for Patent: 7,897,635
Title:HIV protease inhibitors
Abstract: Compounds useful for inhibiting HIV protease are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating wild-type HIV and of multidrug-resistant strains of HIV, also are disclosed.
Inventor(s): Ghosh; Arun K. (River Forest, IL), Bilcer; Geoffrey M. (Chicago, IL), Devasamudram; Thippeswamy (Chicago, IL)
Assignee: The Board of Trustees of the University of Illinois (Urbana, IL)
Application Number:11/593,665
Patent Claims:1. A compound having a formula ##STR00216## wherein R.sup.1 is ##STR00217## or ##STR00218## R.sup.2 is ##STR00219## wherein X is NH optionally substituted with oxo(=O); R.sup.3 is ##STR00220## R.sup.4 is hydrogen; Rd is selected from the group consisting of C.sub.1-4alkyl, C.sub.2-6alkenyl, C.sub.1-3alkyleneC.sub.3-8heterocycloalkyl, OR.sup.e, C.sub.1-3alkyleneOR.sup.e, N(R.sup.e).sub.2, SR.sup.e, halo, nitro, CHO, cyano, NC, C(.dbd.O)R.sup.e, OC(.dbd.O)R.sup.e, C(.dbd.O)OR.sup.e, C(.dbd.O)N(R.sup.e).sub.2, CH.dbd.NOH, CH.dbd.CHCH.sub.2OH, N(R.sup.e)COR.sup.e, and C.sub.1-3alkyleneN(R.sup.e).sub.2; R.sup.e is selected from the group consisting of hydro, C.sub.1-6alkyl, C.sub.2-6alkenyl, aryl, heteroaryl, C.sub.3-8cycloalkyl, THP, Ts, Boc, and C.sub.3-8heterocycloalkyl; q is 0 through 3; or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 wherein R.sup.d, independently, is selected from the group consisting of CH.sub.2OH, NH.sub.2, OH, CH.sub.3, CH.sub.2CH.sub.3, CH.sub.2NH.sub.2, CHO, Cl, F, nitro, OTHP, OCH.sub.3, CH.sub.2NHCH.sub.3, CH.dbd.N--OH, and CH.sub.2OCH.sub.3.

3. A compound of claim 1 selected from the group consisting of, ##STR00221## ##STR00222##

4. A composition comprising a compound of claim 1 and a pharmaceutically acceptable diluent or carrier.

5. A method of treating a male or female mammal suffering from a condition wherein inhibition of HIV-1 protease provides a therapeutic benefit comprising administering to said mammal a therapeutically effective amount of a compound of claim 1.

6. The method of claim 5 wherein the mammal is a human.

7. A method of treating a male or female mammal suffering from a condition wherein inhibition of HIV-1 protease provides a therapeutic benefit comprising administering to said mammal an effective amount of a pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable diluent or carrier.

8. A method of treating a male or female mammal suffering from a condition where inhibition of HIV-1 protease provides a therapeutic benefit comprising administering a therapeutically effective amount of (a) a compound of claim 1, and (b) a second therapeutically active ingredient useful in treatment of the condition.

9. The method of claim 8 wherein (a) and (b) are administered simultaneously, separately, or sequentially.

10. The method of claim 8 wherein the second therapeutically active agent is selected from the group consisting of a second HIV protease inhibitor, an antiviral agent, an immunomodulator, a nucleoside analog, a tat antagonist, a glycosidase inhibitor, and mixtures thereof.

11. The method of claim 10 wherein the second therapeutically active ingredient is selected from the group consisting of Ro 31-859, KNI-272, AZT, DDI, DDC, 3TC, D4T, PMEA, Ro 5-3335, Ro 24-7429, indinavir, ritonavir, saquinavir, nelfinavir, amprenavir, abacavir, castanospremine, castanospermine 6-butryl ester, N-butyl-1-deoxynojirimycin, N-butyl-1-deoxynojirimycin per-butryl ester, 097, acemannan, acyclovir, AD-439, AD-519, adefovir clipivoxil, AL-721, alpha interferon, ansamycin, beta-fluoro-ddA, BMS-232623, BMS-234475, CI-1012, cidofovir, delaviridine, EL-10, efaviren, famciclovir, FTC, hypericin, Compound Q, ISIS 2922, lobucavir, nevirapine, novapren, peptide T, octapeptide, PNU-140690, probacol, stavudine, valaciclovir, virazole, zalcitabine, ABT-378, bropirimine, gamma interferon, interleukin-2, TNF, etanercept, infliximab, fluconalzole, piritrexim, trimetrexate, daunorubicin, leukotriene B4 receptor antagonist, and analogs and prodrugs thereof.

Details for Patent 7,897,635

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Janssen Biotech, Inc. REMICADE infliximab For Injection 103772 08/24/1998 ⤷  Try a Trial 2022-03-12
Immunex Corporation ENBREL etanercept For Injection 103795 11/02/1998 ⤷  Try a Trial 2022-03-12
Immunex Corporation ENBREL etanercept For Injection 103795 05/27/1999 ⤷  Try a Trial 2022-03-12
Immunex Corporation ENBREL etanercept Injection 103795 09/27/2004 ⤷  Try a Trial 2022-03-12
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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