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Generated: January 21, 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 ➤ Subscribe ➤ Subscribe Y Y TREATMENT OF HIV INFECTION ➤ Subscribe
Janssen Prods EDURANT rilpivirine hydrochloride TABLET;ORAL 202022-001 May 20, 2011 RX Yes Yes ➤ Subscribe ➤ Subscribe 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 ➤ Subscribe
Janssen Prods EDURANT rilpivirine hydrochloride TABLET;ORAL 202022-001 May 20, 2011 RX Yes Yes ➤ Subscribe ➤ Subscribe 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 ➤ Subscribe
Janssen Prods EDURANT rilpivirine hydrochloride TABLET;ORAL 202022-001 May 20, 2011 RX Yes Yes ➤ Subscribe ➤ Subscribe 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 ➤ Subscribe
Gilead Sciences Inc ODEFSEY emtricitabine; rilpivirine hydrochloride; tenofovir alafenamide fumarate TABLET;ORAL 208351-001 Mar 1, 2016 RX Yes Yes ➤ Subscribe ➤ Subscribe Y Y TREATMENT OF HIV INFECTION ➤ Subscribe
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
8,841,310 Combinations of a pyrimidine containing NNRTI with RT inhibitors ➤ Subscribe
7,638,522 Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl- ]amino] benzonitrile ➤ Subscribe
7,956,063 Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl- ]amino]benzonitrile ➤ Subscribe
9,580,392 HIV replication inhibiting pyrimidines ➤ Subscribe
8,101,629 Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl- ]amino]benzonitrile ➤ Subscribe
8,080,551 HIV inhibiting pyrimidines derivatives ➤ Subscribe
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
Canada 2577273 ➤ Subscribe
Canada 2577288 ➤ Subscribe
China 1541215 ➤ Subscribe
China 100509801 ➤ Subscribe
China 101056673 ➤ Subscribe
China 101060844 ➤ Subscribe
China 101068597 ➤ Subscribe
Cyprus 1112249 ➤ Subscribe
Cyprus 1112331 ➤ Subscribe
Cyprus 1116565 ➤ Subscribe
Country Document Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration

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Serving leading biopharmaceutical companies globally:

Teva
Chubb
Cipla
Boehringer Ingelheim
Farmers Insurance
Covington
Colorcon
Merck
Medtronic

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