Title:
USE OF NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITOR (MNI) FOR THE TREATMENT OF HIV INFECTION
Document Type and Number:
WIPO Patent Application WO/2000/056736
Kind Code:
A2
Abstract:
Use of a compound of the formula (I), wherein x can be selected one of: 2,5-OMe; o-F; m-F, p-F; and o-C1. For treatment of HIV invection.
Inventors:
UCKUN FATIH M
Application Number:
PCT/US2000/006806
Publication Date:
September 28, 2000
Filing Date:
March 16, 2000
Export Citation:
Assignee:
PARKER HUGHES INST (US)
International Classes:
A61K31/17; A61P31/18; (IPC1-7): C07D493/00
Domestic Patent References:
| WO1999047501A2 | 1999-09-23 | |||
| WO1993003022A1 | 1993-02-18 |
Other References:
D'CRUZ, OSMOND J. ET AL: "Novel derivatives of phenethyl-5-bromopyridylthiourea and dihydroalkoxybenzyl-oxopyrimidine are dual-function spermicides with potent anti-human immunodeficiency virus activity" BIOL. REPROD. (1999), 60(6), 1419-1428 , XP000886878
VIG, RAKESH ET AL: "Rational design and synthesis of phenethyl-5-bromopyridyl thiourea derivatives as potent non-nucleoside inhibitors of HIV reverse transcriptase" BIOORG. MED. CHEM. (1998), 6(10), 1789-1797 , XP000974972 cited in the application
MAO, CHEN ET AL: "Structure-based design of N-[2-(1-piperidinylethyl)Ü-N'-[2-(5- bromopyridyl)Üthiourea and N-[2-(1-piperazinylethyl)Ü-N'-[2-(5- bromopyridyl)Üthiourea as potent non-nucleoside inhibitors of HIV -1 reverse transcriptase" BIOORG. MED. CHEM. LETT. (1998), 8(16), 2213-2218 , XP004132801
VIG, RAKESH ET AL: "Rational design and synthesis of phenethyl-5-bromopyridyl thiourea derivatives as potent non-nucleoside inhibitors of HIV reverse transcriptase" BIOORG. MED. CHEM. (1998), 6(10), 1789-1797 , XP000974972 cited in the application
MAO, CHEN ET AL: "Structure-based design of N-[2-(1-piperidinylethyl)Ü-N'-[2-(5- bromopyridyl)Üthiourea and N-[2-(1-piperazinylethyl)Ü-N'-[2-(5- bromopyridyl)Üthiourea as potent non-nucleoside inhibitors of HIV -1 reverse transcriptase" BIOORG. MED. CHEM. LETT. (1998), 8(16), 2213-2218 , XP004132801
Attorney, Agent or Firm:
Daignault, Ronald A. (MN, US)
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Claims:
WE CLAIM:
| 1. | A method for the treatment of HIV infection comprising: administering to a patient an effective dose of a compound of the formula: wherein x can be a selected one of : 2,5OMe; oF; mF; pF; and oCl. |
| 2. | The method of claim 1, wherein said compound is selected from the group of formulas consisting of :. |
| 3. | A method for the treatment of HIV strains having mutations in the Wing 2 region of the RT NNI binding site, comprising contacting said mutant HIV strain with DDE236 or DDE240. |
| 4. | A method for the treatment of multidrug resistant HIV comprising administering DDE236 or DDE240. |
Description:
INTERNATIONALSEARCHREPORT lntei tal Application No PCT/US00/06806 C.(Continuation)DOCUMENTSCONSIDEREDTOBERELEVANT Calegory ° Cilationofdocument,withindication,whereappropriate,oftherele
vantpassagesRelevanttoclaimNo. XWO9303022A(MEDIVIRAB)1-3 18February1993(1993-02-18) page24,line19-22 page22-23;claims41,42,63-65 page20,line2-11 page10,line9-24 XVIG,RAKESHETAL:"Rationaldesignand1-4 synthesisofphenethyl-5-bromopyridyl thioureaderivativesaspotent non-nucleosideinhibitorsofHIVreverse transcriptase" BIOORG.MED.CHEM.(1998),6(10), 1789-1797, XP000974972 citedintheapplication thewholedocument AMAO,CHENETAL:"Structure-baseddesign1 ofN-'2- (l-piperidinylethyl) !-N'-'2- (5- bromopyridyl)!thioureaand N-'2- (1-piperazinylethyl) !-N'-'2- (5- bromopyridyl) ! thioureaaspotent non-nucleosideinhibitorsofHIV-1 reversetranscriptase" BIOORG.MED.CHEM.LETT.(1998),8(16), 2213-2218, XP004132801 page2214-5 INTERNATIONAL SEARCH REPORT Inte d Appllcatfon No wnormation on patent family members Patent document Publication Patent family Publication citedinsearchreportdate member(s)date WO9947501A23-09-1999US 5998411 A 07-12-1999 AU 3186499 A 11-10-1999 US 6124307 A 26-09-2000 US 6124307 A 26-09-2000 WO9303022A18-02-1993AP 384 A 15-05-1995 AP 388 A 15-05-1995 AU 657978 B 30-03-1995 AU 2045192 A 11-03-1993 AU 2407492 A 02-03-1993 BG 98623 A 31-05-1995 CA 2075173 A 03-02-1993 CN 1069882 A 17-03-1993 CZ 282900 B 12-11-1997 EP 0540143 A 05-05-1993 ES 2051641 A 16-06-1994 FI 923443 A 03-02-1993 HU 9500395 A 28-09-1995 IL 102548 A 16-08-1998 JP 5320138 A 03-12-1993 MX 9204454 A 30-06-1994 NO 922949 A 03-02-1993 NO 931337 A 03-02-1993 NO 931338 A 03-02-1993 NO 931339 A 03-02-1993 NO 931340 A 03-02-1993 NZ 260293 A 26-05-1997 OA 9914 A 15-08-1994 RU 2106341 C 10-03-1998 US 5593993 A 14-01-1997 US 5714503 A 03-02-1998 US 5658907 A 19-08-1997 ZA 9205663 A 28-01-1994
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