NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS

Title:

NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS

Document Type and Number:

WIPO Patent Application WO2003097644

Kind Code:

A3

Abstract:

Compounds represented by formula (I), wherein R<2> is selected from the group consisting of H, (C1-4)alkyl, halo, haloalkyl, OH, (C1-6)alkoxy, NH(C1-4alkyl) or N(C1-4alkyl)2; R<4> is H or Me; R<5> is H or Me; R<11> is H, (C1-4)alkyl, (C3-4)cycloalkyl and (C1-4)alkyl-(C3-4)cycloalkyl; A is a connecting chain of (C1-3)alkyl; B is O or S; n is 0 or 1; wherein when n is 0: Ring C is 6- or 10-membered aryl or 5- or 6-membered heterocycle having from 1 to 4 heteroatoms selected from the group consisting of O, N, and S, said aryl and said heterocycle being optionally substituted; and E is CONR<12>R<13> ; CONHNR<14>R<15>; NR<16>COR<17>; NR<18>SO2(C1-6)alkyl; SO2NR<19>R<20>; or SO2R<21>; or when n is 1: Ring C is as defined above and E is a single bond or a connecting group; and Ring D is 6- or 10-membered aryl or 5- or 6-membered heterocycle having from 1 to 4 heteroatoms selected from the group consisting of O, N, and S, said aryl and said heterocycle being optionally substituted with from 1 to 5 substituents; or a salt or a prodrug thereof are provided as inhibitors of HIV reverse transcriptase.

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Inventors:

SIMONEAU BRUNO (CA)
LANDRY SERGE (CA)
MALENFANT ERIC (CA)
NAUD JULIE (CA)
O'MEARA JEFFREY (CA)
THAVONEKHAM BOUNKHAM (CA)
YOAKIM CHRISTIANE (CA)

Application Number:

PCT/CA2003/000718

Publication Date:

February 05, 2004

Filing Date:

May 14, 2003

Export Citation:

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Assignee:

BOEHRINGER INGELHEIM INT (DE)
SIMONEAU BRUNO (CA)
LANDRY SERGE (CA)
MALENFANT ERIC (CA)
NAUD JULIE (CA)
O'MEARA JEFFREY (CA)
THAVONEKHAM BOUNKHAM (CA)
YOAKIM CHRISTIANE (CA)

International Classes:

A61K31/551; A61P31/18; A61P43/00; C07D471/14; (IPC1-7): C07D471/14; A61K31/55; A61P31/18; C07D471/14

Domestic Patent References:

WO2003011862A1	2003-02-13
WO2002076982A2	2002-10-03

Foreign References:

US5705499A	1998-01-06
US20020028807A1	2002-03-07

Other References:

CYWIN, CHARLES L. ET AL: "Novel Nonnucleoside Inhibitors of HIV-1 Reverse Transcriptase. 8. 8-Aryloxymethyl- and 8-Arylthiomethyldipyridodiazepinones", JOURNAL OF MEDICINAL CHEMISTRY (1998), 41(16), 2972-2984, XP002181340

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