HIV inhibiting pyrimidines derivatives

HIV replication inhibitors having formula (I) defined herein are disclosed. Pharmaceutical compositions containing the HIV replication inhibitors; the use of the HIV replication inhibitors in the treatment of HIV; and processes for preparing the HIV replication inhibitors are also disclosed.

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Main Authors Guillemont, Jérôme Emile Georges, Palandijian, Patrice, De Jonge, Marc René, Koymans, Lucien Maria Henricus, Vinkers, Hendrik Maarten, Daeyaert, Frederik Frans Desiré, Heeres, Jan, Van Aken, Koen Jeanne Alfons, Lewi, Paulus Joannes, Janssen, Paul Adriaan Jan
Format Patent
LanguageEnglish
Published 20.12.2011
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Abstract HIV replication inhibitors having formula (I) defined herein are disclosed. Pharmaceutical compositions containing the HIV replication inhibitors; the use of the HIV replication inhibitors in the treatment of HIV; and processes for preparing the HIV replication inhibitors are also disclosed.
AbstractList HIV replication inhibitors having formula (I) defined herein are disclosed. Pharmaceutical compositions containing the HIV replication inhibitors; the use of the HIV replication inhibitors in the treatment of HIV; and processes for preparing the HIV replication inhibitors are also disclosed.
Author Koymans, Lucien Maria Henricus
Daeyaert, Frederik Frans Desiré
Lewi, Paulus Joannes
Guillemont, Jérôme Emile Georges
De Jonge, Marc René
Heeres, Jan
Janssen, Paul Adriaan Jan
Vinkers, Hendrik Maarten
Palandijian, Patrice
Van Aken, Koen Jeanne Alfons
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  givenname: Marc René
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  givenname: Paul Adriaan Jan
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References Supuran, et al., J. of Enzyme Inhibition (2000), 15(4), 391-401.
Squires, K., "An Introduction to Nucleoside and Nucleotide Analogues", Antiviral Therapy, 6 Suppl.3, XP 009042950 pp. 1-14 2001.
(WO0027825) 20000500
Bethiel et al. (6949544) 20050900
(WO 01/23362) 20010400
International Search Report, mailing date Feb. 7, 2005, for corresponding Application No. PCT/EP2004/052028 (related subject matter).
Supuran, Cl., et al. "Carbonic Anhyddrase Inhibitors: Synthesis of Sulfonamides Incorporating 2,4,6-Trisubstituted-Pyridinium-Ethylcarboxamido Moieties Possessing Membrane-Impermeability and In Vivo Selectively for the Membrane-Bound (CA IV) Versus the Cytosolic (CA 1 and CA II) Isozymes", Journal of Enzyme Inhibitor and Medicinal Chemistry vol. 15, pp. 381-340 (2000).
Gennaro, AR "Remington Pharmacy", 19th edition, Medica Panmericana, 1995, pp. 230-235, 245, and 2226-2234. English translation and Certfication attached.
Andries et al. (6197779) 20010300
International Preliminary Examination Report dated Dec. 3, 2003 for corresponding Appln. No. PCT/EP2002/08953.
(2341) 19790600
(2324919) 19991000
(WO 01/60816) 20010800
Young, B., "Can Abacavir Be Given Once-A-Day?" the 43rd Interscience Conference on Antimicrobial Agents and Chemotherapy XP-002274551 Sep. 16, 2003.
Ludovici, D., et al. "Evolution of Anti-HIV Drug Candidates. Part 3: Diarylpyrimidine (DAPY) Analogues", Bioorganic & Medicinal Chemistry Letters, vol. 11 pp. 2235- 2239 (2001).
International Preliminary Examination Report dated Nov. 30, 2004 for corresponding Appin. No. PCT/EP2003/50366.
(WO 01/22938) 20010400
International Search report, mailing date Nov. 26, 2002, for corresponding Application No. PCT/EP2002/08953.
Guillemont et al. (7125879) 20061000
(WO 03/016306) 20030200
(WO 00/27825) 20000500
Schils et al. (7399856) 20080700
(2000-35628) 20000200
Miles, Community Pract., vol. 78, Aug. 2005, pp. 292-294 ( Medline abstract), 2005.
(WO 00/53610) 20000900
(WO 00/78731) 20001200
Denton, et al. "Antiretroviral Pre-Exposure Prophylaxis Prevents Vaginal Transmission of HIV-1 in Humanized BLT Mice", PLoS Medicine (Jan. 14, 2008).
(WO 02/70470) 20020900
International Search Report dated Nov. 6, 2003 for related International Application No. PCT/EP2003/50366.
(1002795) 20000500
Davis et al. (5958935) 19990900
Pease et al. (6838464) 20050100
(WO 97/18839) 19970500
(19945982) 19990900
(WO 97/24350) 19970700
(WO 00/62778) 20001000
Larock, R. C. "Interconversion of Nitriles Casiooxylic Acids and Derivatives", John Wiley & Sons, Inc. pp. 1983-1985 1999.
(WO 02/08226) 20020100
Mayo Clinic, HIV Infection Symptoms According to Infection Stage, www.mayoclinic.com/health/hiv-aids/DS00005/DSECTION-symptoms (Nov. 2, 2009).
(WO 00/12485) 20000300
(WO 01/85700) 20011100
Pauletti et al. (6982091) 20060100
(19945982) 20010300
Ludocici, et al., Bioorg. & Med. Chem. Letters (2001), 11(17), 2235-2239.
Mayo Clinic, HIV infection symptoms according to infection stage; <http://www.mayoclinic.com/health/hiv-aids/DS00005/DSECTION=symptoms>, updated Jun. 20, 2008, downloaded Feb. 27, 2009.
Gilead Press Release XP-002314669 Oct. 24, 2005.
Pavia, A., "Abacavir/Lamiviudne in Connection With Efavirenz, Amprenavir/Ritonavir or Stavudine", XP 002274550, The XIV International AIDS Conference Jul. 9, 2002.
(1002795) 19990500
Hantke et al. (2009/0148531) 20090600
Gramera et al. (3459731) 19690800
Arien et al. (2006/0034797) 20060200
Denton, et al., PLoS Medicine, Jan. 14, 2008.
(0945443) 19990900
(WO 99/50250) 19991000
Buckman et al. (5691364) 19971100
Singh et al. (7060827) 20060600
Office Action dispatched May 12, 2009 for corresponding Japanese Patent Application No. 521229/03.
(WO 98/41512) 19980900
(WO 01/64654) 20010900
(WO 2004/50058) 20040600
D'Auria, M., et al. "Photochemical Dimerization in Solution of Arylacrylonitrile Derivatives", Tetrahedron, vol. 53, No. 51, pp. 17307-17316 (1997).
(WO 97/19065) 19970500
(WO 2004/16581) 20030200
Koyanagi, Y., et al. "Selective Cytotoxicity of Aids Virus Infection Towards HTLV1-Transformed Cell Lines", Int. J. Cancer: 36, pp. 445-451 (1985).
European Search Report dated Dec. 5, 2001 for corresponding Application No. EP 01203090.4.
Canadian Search Report dated Feb. 19, 2007 for corresponding Application No. CA 2,452,217.
Miles, K., "The Growing HIV Pandemic", HIV Diagnoses: Community Practitioner (2005) vol. 78, No. 8 pp. 292-294.
(WO 2005/021001) 20050300
(0002341) 19820100
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  ident: 2324919
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