NO328122B1 - Bredspektrede heterocyklisk substituerte fenylinneholdende sulfonamid-HIV-proteaseinhibitorer - Google Patents
Bredspektrede heterocyklisk substituerte fenylinneholdende sulfonamid-HIV-proteaseinhibitorer Download PDFInfo
- Publication number
- NO328122B1 NO328122B1 NO20043114A NO20043114A NO328122B1 NO 328122 B1 NO328122 B1 NO 328122B1 NO 20043114 A NO20043114 A NO 20043114A NO 20043114 A NO20043114 A NO 20043114A NO 328122 B1 NO328122 B1 NO 328122B1
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- Prior art keywords
- alkyl
- amino
- compound
- compounds
- halogen
- Prior art date
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 title claims description 21
- 125000000623 heterocyclic group Chemical group 0.000 title description 6
- 239000004030 hiv protease inhibitor Substances 0.000 title description 5
- 229940124530 sulfonamide Drugs 0.000 title description 5
- 150000003456 sulfonamides Chemical class 0.000 title description 5
- 238000001228 spectrum Methods 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims description 201
- 239000000203 mixture Substances 0.000 claims description 86
- -1 hexahydrofurophenyl Chemical group 0.000 claims description 68
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 50
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- 238000002360 preparation method Methods 0.000 claims description 32
- 229910052736 halogen Inorganic materials 0.000 claims description 29
- 150000002367 halogens Chemical group 0.000 claims description 29
- 125000000217 alkyl group Chemical group 0.000 claims description 27
- 125000001424 substituent group Chemical group 0.000 claims description 23
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- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 15
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- 229910052757 nitrogen Inorganic materials 0.000 claims description 11
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
- C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
- C07C311/18—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms, not being part of nitro or nitroso groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D233/88—Nitrogen atoms, e.g. allantoin
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/38—Nitrogen atoms
- C07D277/40—Unsubstituted amino or imino radicals
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/38—Nitrogen atoms
- C07D277/42—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/38—Nitrogen atoms
- C07D277/44—Acylated amino or imino radicals
- C07D277/46—Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2603/00—Systems containing at least three condensed rings
- C07C2603/02—Ortho- or ortho- and peri-condensed systems
- C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
- C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
- C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
- C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
- C07C2603/18—Fluorenes; Hydrogenated fluorenes
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- Chemical & Material Sciences (AREA)
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- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
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- Pharmacology & Pharmacy (AREA)
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- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Thiazole And Isothizaole Compounds (AREA)
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Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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EP01205115 | 2001-12-21 | ||
PCT/EP2002/014839 WO2003053435A1 (en) | 2001-12-21 | 2002-12-20 | Broadspectrum heterocyclic substituted phenyl containing sulfonamide hiv protease inhibitors |
Publications (2)
Publication Number | Publication Date |
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NO20043114L NO20043114L (no) | 2004-09-20 |
NO328122B1 true NO328122B1 (no) | 2009-12-14 |
Family
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Family Applications (1)
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NO20043114A NO328122B1 (no) | 2001-12-21 | 2004-07-20 | Bredspektrede heterocyklisk substituerte fenylinneholdende sulfonamid-HIV-proteaseinhibitorer |
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US (1) | US7763641B2 (ja) |
EP (1) | EP1463502B1 (ja) |
JP (1) | JP4578101B2 (ja) |
KR (1) | KR100942743B1 (ja) |
CN (1) | CN100448444C (ja) |
AP (1) | AP1922A (ja) |
AR (1) | AR037976A1 (ja) |
AT (1) | ATE516029T1 (ja) |
AU (1) | AU2002361235B2 (ja) |
BR (1) | BR0215260A (ja) |
CA (1) | CA2470964C (ja) |
EA (1) | EA009556B1 (ja) |
HK (1) | HK1070001A1 (ja) |
HR (1) | HRP20040662B1 (ja) |
HU (1) | HUP0500164A3 (ja) |
IL (2) | IL162574A0 (ja) |
MX (1) | MXPA04006201A (ja) |
MY (1) | MY138657A (ja) |
NO (1) | NO328122B1 (ja) |
NZ (1) | NZ533665A (ja) |
PL (1) | PL216539B1 (ja) |
TW (1) | TWI336621B (ja) |
WO (1) | WO2003053435A1 (ja) |
ZA (1) | ZA200405784B (ja) |
Families Citing this family (10)
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CN100364531C (zh) * | 2002-12-18 | 2008-01-30 | 西托维亚公司 | 3,5-二取代-[1,2,4]-二唑及类似物和其用途 |
US20080234288A1 (en) * | 2003-09-30 | 2008-09-25 | Kenneth Alan Simmen | Hcv Inhibiting Sulfonamides |
EP2422781A1 (en) * | 2004-05-07 | 2012-02-29 | Sequoia Pharmaceuticals, Inc. | Resistance-repellent retroviral protease inhibitors |
AU2006217922B2 (en) | 2005-02-25 | 2012-04-05 | Janssen Sciences Ireland Uc | Protease inhibitor precursor synthesis |
WO2008004100A2 (en) | 2006-07-05 | 2008-01-10 | Pfizer Products Inc. | Therapeutic compounds |
US20120316161A1 (en) | 2009-12-23 | 2012-12-13 | Katholieke Universiteit Leuven | Novel antiviral compounds |
US8563597B2 (en) * | 2010-09-02 | 2013-10-22 | Purdue Research Foundation | Fused tricyclic ether carbamates and their use |
CA2817896A1 (en) | 2010-11-15 | 2012-05-24 | Viiv Healthcare Uk Limited | Inhibitors of hiv replication |
EP2640705A2 (en) | 2010-11-15 | 2013-09-25 | Katholieke Universiteit Leuven | Novel antiviral compounds |
EP3192794A4 (en) * | 2014-09-11 | 2018-06-27 | Shionogi & Co., Ltd. | Sustained hiv protease inhibitor |
Family Cites Families (21)
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US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
PH30929A (en) | 1992-09-03 | 1997-12-23 | Janssen Pharmaceutica Nv | Beads having a core coated with an antifungal and a polymer. |
US5723490A (en) * | 1992-09-08 | 1998-03-03 | Vertex Pharmaceuticals Incorporated | THF-containing sulfonamide inhibitors of aspartyl protease |
DE69415326T2 (de) | 1993-08-24 | 1999-06-02 | G.D. Searle & Co., Chicago, Ill. | Hydroxyaminosulfonamide verwendbar als inhibitoren retroviraler proteasen |
IL111080A (en) | 1993-10-01 | 1999-08-17 | Astra Ab | Method for treating a finely divided powder medicament |
JP4014220B2 (ja) | 1995-01-20 | 2007-11-28 | ジー.ディー.サール アンド カンパニー | ビス−スルホンアミドヒドロキシエチルアミノ レトロ ウイルスプロテアーゼインヒビター |
US5756533A (en) | 1995-03-10 | 1998-05-26 | G.D. Searle & Co. | Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
US6150556A (en) | 1995-03-10 | 2000-11-21 | G. D. Dearle & Co. | Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
US5705500A (en) | 1995-03-10 | 1998-01-06 | G.D. Searle & Co. | Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
RU2174519C2 (ru) | 1995-03-10 | 2001-10-10 | Джи. Ди. Сирл Энд Ко. | Гидроксиэтиламино сульфонамиды гетероциклокарбонил аминокислоты, ингибирующие ретровирусную протеазу |
JPH09124630A (ja) * | 1995-10-26 | 1997-05-13 | Kissei Pharmaceut Co Ltd | カルバミン酸テトラヒドロフリルエステル誘導体の製造方法 |
WO1997018205A1 (en) | 1995-11-15 | 1997-05-22 | G.D. Searle & Co. | Substituted sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
CN1165291C (zh) | 1996-05-20 | 2004-09-08 | 詹森药业有限公司 | 具有改进的生物利用度的抗真菌组合物 |
HU224217B1 (hu) | 1997-03-26 | 2005-06-28 | Janssen Pharmaceutica N.V. | Gombaellenes hatóanyaggal és polimerrel bevont magrészt tartalmazó pelletek |
AU2010299A (en) | 1997-12-24 | 1999-07-19 | Vertex Pharmaceuticals Incorporated | Prodrugs os aspartyl protease inhibitors |
BR9814484A (pt) | 1997-12-24 | 2000-10-10 | Vertex Pharma | "pró-drogas de inibidores de aspartil protease" |
US6436989B1 (en) | 1997-12-24 | 2002-08-20 | Vertex Pharmaceuticals, Incorporated | Prodrugs of aspartyl protease inhibitors |
AU2012199A (en) | 1997-12-24 | 1999-07-19 | Vertex Pharmaceuticals Incorporated | Prodrugs of aspartyl protease inhibitors |
DK1086076T3 (da) * | 1998-06-19 | 2005-03-29 | Vertex Pharma | Sulfonamidinhibitorer af aspartylprotease |
WO1999067417A2 (en) | 1998-06-23 | 1999-12-29 | The United States Of America, Represented By The Secretary, Department Of Health And Human Services | Fitness assay and associated methods |
WO1999067254A2 (en) | 1998-06-23 | 1999-12-29 | The United States Of America Represented By The Secretary, Department Of Health And Human Services | Multi-drug resistant retroviral protease inhibitors and use thereof |
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2002
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- 2002-12-20 IL IL16257402A patent/IL162574A0/xx unknown
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- 2002-12-20 EP EP02796754A patent/EP1463502B1/en not_active Expired - Lifetime
- 2002-12-20 MX MXPA04006201A patent/MXPA04006201A/es active IP Right Grant
- 2002-12-20 WO PCT/EP2002/014839 patent/WO2003053435A1/en active IP Right Grant
- 2002-12-20 MY MYPI20024811A patent/MY138657A/en unknown
- 2002-12-20 US US10/499,221 patent/US7763641B2/en not_active Expired - Fee Related
- 2002-12-20 AP APAP/P/2004/003083A patent/AP1922A/en active
- 2002-12-20 EA EA200400828A patent/EA009556B1/ru not_active IP Right Cessation
- 2002-12-20 HU HU0500164A patent/HUP0500164A3/hu unknown
- 2002-12-20 TW TW091136901A patent/TWI336621B/zh not_active IP Right Cessation
- 2002-12-20 KR KR1020047009850A patent/KR100942743B1/ko not_active IP Right Cessation
- 2002-12-20 PL PL370801A patent/PL216539B1/pl unknown
- 2002-12-20 AR ARP020105066A patent/AR037976A1/es not_active Application Discontinuation
- 2002-12-20 AT AT02796754T patent/ATE516029T1/de not_active IP Right Cessation
- 2002-12-20 CN CNB028281667A patent/CN100448444C/zh not_active Expired - Fee Related
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- 2002-12-20 JP JP2003554192A patent/JP4578101B2/ja not_active Expired - Fee Related
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2004
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- 2004-07-19 HR HRP20040662AA patent/HRP20040662B1/hr not_active IP Right Cessation
- 2004-07-20 NO NO20043114A patent/NO328122B1/no not_active IP Right Cessation
- 2004-07-20 ZA ZA2004/05784A patent/ZA200405784B/en unknown
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