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Generated: April 23, 2018

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Details for Patent: 7,125,879

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Summary for Patent: 7,125,879
Title:HIV inhibiting pyrimidines derivatives
Abstract:This invention concerns HIV replication inhibitors of formula (I) the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a.sup.1=a.sup.2-a.sup.3=a.sup.4--and -b.sup.1=b.sup.2-b.sup.3=b.sup.4represents pheynl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R.sup.1 is hydrogen; aryl; formyl; C.sub.1-6alkylcarbonyl; C.sup.1-6alkyl; C.sub.1-6alkyloxycarbonyl, substituted C.sub.1-6alkyl, C.sub.1-6alkylcarbonyl; R.sup.2 is hydroxy, halo, optionally substituted C.sub.1-6alkyl, C.sub.3-7cycloalkyl, optionally substituted C.sub.2-6alkenyl, optionally substituted C.sub.2-6alkynyl, C.sub.1-6alkyloxy, C.sub.1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C.sub.1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, --S(.dbd.O).sub.pR.sup.6, --NH--S(.dbd.O).sub.pR.sup.6, --C(.dbd.O)R.sup.6, --NHC(.dbd.O)H, --C(.dbd.O)NHNH?2?, --NHC(.dbd.O)R.sup.6, --C(.dbd.NH)R.sup.6 or a 5-membered hetrocycl; X.sub.1 is --NR.sup.5--, --NH--NH--, --N.dbd.N--, --O--, --C(.dbd.O)--, C.sub.1-4alkanediyl, --CHOH--, --S--, --S(.dbd.O).sub.p--, --X.sub.2--C.sub.1-4alkanediyl- or --C.sub.1-4alkanediyl-X.sub.2--; R.sup.3 is NHR.sup.13, NR.sup.13R.sup.14; --C(.dbd.O)--NHR.sup.13; --C(.dbd.O)--NR.sup.13R.sup.14; --C(.dbd.O)--R.sup.15; --CH.dbd.N--NH--C(.dbd.O)--R.sup.16; substituted C.sub.1-6alkyl; optionally substituted C.sub.1-6alkyloxyC.sub.1-6alkyl; substituted C.sub.2-6alkenyl; substituted C.sub.2-6alkynyl; substituted C.sub.2-6alkylenyl; C.sub.1-6alkyl substituted with hydroxy and a second substituent; --C(.dbd.N--O--R.sup.8)--C.sub.1-4alkyl; R.sup.7; or --X.sub.3--R.sup.7; R.sup.4 is halo, hydroxy, C.sub.1-6alkyl, C.sub.3-7cycloalkyl, C.sub.1-6alkyloxy, cyano, nitro, polyhaloC.sub.1-6alkyl, polyhaloC.sub.1-6alkyloxy, aminocarbonyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkylcarbonyl, formyl, amino, mono- or di(C.sub.1-4alkyl) amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them ##STR00001##
Inventor(s): Guillemont; Jeo (Ande, FR), Palandjian; Patrice (Louviers, FR), de Jonge; Marc Rene (Tilburg, NL), Koymans; Lucien Maria Henricus (Retie, BE), Vinkers; Hendrik Maarten (Antwerp, BE), Daeyaert; Frederik Frans Desire (Beerse, BE), Heeres; Jan (Vosselaar, BE), Van Aken; Koen Jeanne Alfons (Kortrijk, BE), Lewi; Paulus Joannes (Turnhout, BE), Arts, legal representative; Frank Xavier Josef Herwig (Beerse, BE), Janssen, deceased; Paul Adriaan Jan (Turnhout, BE)
Assignee: Janssen Pharmaceutica N.V. (Beerse, BE)
Application Number:10/485,636
Patent Claim Types:
see list of patent claims
Compound; Composition; Process; Use; Dosage form;

Drugs Protected by US Patent 7,125,879

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Patent Submitted
Gilead Sciences Inc COMPLERA emtricitabine; rilpivirine hydrochloride; tenofovir disoproxil fumarate TABLET;ORAL 202123-001 Aug 10, 2011 RX Yes Yes ➤ Try a Free Trial ➤ Try a Free Trial Y Y TREATMENT OF HIV INFECTION ➤ Try a Free Trial
Janssen Prods EDURANT rilpivirine hydrochloride TABLET;ORAL 202022-001 May 20, 2011 RX Yes Yes ➤ Try a Free Trial ➤ Try a Free Trial Y Y IN COMBINATION WITH OTHER ANTIRETROVIRAL AGENTS, IS INDICATED FOR THE TREATMENT OF HUMAN IMMUNODEFICIENCY VIRUS TYPE 1 (HIV-1) INFECTION IN ANTIRETROVIRAL TREATMENT-NAIVE ADULT PATIENTS, AS SET FORTH IN THE LABELING, INCLUDING I&U SECTION ➤ Try a Free Trial
Janssen Prods EDURANT rilpivirine hydrochloride TABLET;ORAL 202022-001 May 20, 2011 RX Yes Yes ➤ Try a Free Trial ➤ Try a Free Trial Y Y IN COMBINATION WITH OTHER ANTIRETROVIRAL AGENTS FOR THE TREATMENT OF HIV-1 INFECTION IN TREATMENT-NAIVE ADULT PATIENTS WITH HIV-1 RNA LESS THAN OR EQUAL TO 100,000 AT THE START OF THERAPY ➤ Try a Free Trial
Janssen Prods EDURANT rilpivirine hydrochloride TABLET;ORAL 202022-001 May 20, 2011 RX Yes Yes ➤ Try a Free Trial ➤ Try a Free Trial Y Y IN COMBINATION WITH OTHER ANTIRETROVIRAL AGENTS FOR THE TREATMENT OF HIV-1 INFECTION IN TREATMENT-NAIVE PATIENTS WITH HIV-1 RNA LESS THAN OR EQUAL TO 100,000 AT THE START OF THEARPY ➤ Try a Free Trial
Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Patent Submitted

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Foreign Priority and PCT Information for Patent: 7,125,879

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
01203090Aug 13, 2001
02077748Jun 10, 2002
PCT Information
PCT FiledAugust 09, 2002PCT Application Number:PCT/EP02/08953
PCT Publication Date:February 27, 2003PCT Publication Number: WO03/016306

Non-Orange Book US Patents Family Members for Patent 7,125,879

For Orange Book-listed patents (shown in the main table above) generic applications must certify that the listed patents are expired, invalid, or will not be infringed by generic entry.

The non-Orange Book patents listed below do not require formal certifications, so they do not automatically impede generic entry. Instead, they represent potential opportunities for branded firms to block generic entry through patent infringment challenges.

Patent No. Title Estimated Patent Expiration
8,080,551 HIV inhibiting pyrimidines derivatives ➤ Try a Free Trial
8,101,629 Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl- ]amino]benzonitrile ➤ Try a Free Trial
7,638,522 Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl- ]amino] benzonitrile ➤ Try a Free Trial
9,580,392 HIV replication inhibiting pyrimidines ➤ Try a Free Trial
Patent No. Title Estimated Patent Expiration

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International Patents Family Members for US Patent 7,125,879

Country Document Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
African Regional IP Organization (ARIPO) 1610 ➤ Try a Free Trial
African Regional IP Organization (ARIPO) 2109 ➤ Try a Free Trial
African Regional IP Organization (ARIPO) 2296 ➤ Try a Free Trial
African Regional IP Organization (ARIPO) 2487 ➤ Try a Free Trial
Country Document Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration

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Serving hundreds of leading biopharmaceutical companies globally:

Chubb
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Chinese Patent Office
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Covington
Cantor Fitzgerald
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