ZA949127B - Prodrugs of an inhibitor of HIV protease - Google Patents

Prodrugs of an inhibitor of HIV protease

Info

Publication number
ZA949127B
ZA949127B ZA949127A ZA949127A ZA949127B ZA 949127 B ZA949127 B ZA 949127B ZA 949127 A ZA949127 A ZA 949127A ZA 949127 A ZA949127 A ZA 949127A ZA 949127 B ZA949127 B ZA 949127B
Authority
ZA
South Africa
Prior art keywords
prodrugs
inhibitor
hiv protease
hiv
protease
Prior art date
Application number
ZA949127A
Other languages
English (en)
Inventor
Jose Alexander
Dilbir Bindra
Bruce D Dorsey
Arnold J Repta
Joseph P Vacca
Original Assignee
Merck & Co Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of ZA949127B publication Critical patent/ZA949127B/xx

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36Radicals substituted by singly-bound nitrogen atoms
    • C07D213/38Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Plant Substances (AREA)
ZA949127A 1993-11-18 1994-11-17 Prodrugs of an inhibitor of HIV protease ZA949127B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US15420493A 1993-11-18 1993-11-18

Publications (1)

Publication Number Publication Date
ZA949127B true ZA949127B (en) 1996-05-17

Family

ID=22550424

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA949127A ZA949127B (en) 1993-11-18 1994-11-17 Prodrugs of an inhibitor of HIV protease

Country Status (17)

Country Link
US (1) US5733907A (xx)
EP (1) EP0729467A1 (xx)
JP (1) JPH09505303A (xx)
KR (1) KR960705809A (xx)
CN (1) CN1139432A (xx)
AU (1) AU687128B2 (xx)
CA (1) CA2174649A1 (xx)
CZ (1) CZ140696A3 (xx)
FI (1) FI962073A0 (xx)
HU (1) HUT76270A (xx)
IL (1) IL111584A0 (xx)
NO (1) NO962000D0 (xx)
NZ (1) NZ276622A (xx)
PL (1) PL314486A1 (xx)
SK (1) SK61496A3 (xx)
WO (1) WO1995014016A1 (xx)
ZA (1) ZA949127B (xx)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6458772B1 (en) 1909-10-07 2002-10-01 Medivir Ab Prodrugs
US20040122000A1 (en) 1981-01-07 2004-06-24 Vertex Pharmaceuticals Incorporated. Inhibitors of aspartyl protease
US6878728B1 (en) 1999-06-11 2005-04-12 Vertex Pharmaceutical Incorporated Inhibitors of aspartyl protease
MY126358A (en) * 1996-03-22 2006-09-29 Glaxo Group Ltd Compositions comprising vx478 and a water soluble tocopherol derivative such as vitamin e-tpgs
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
FR2773994B1 (fr) * 1998-01-23 2002-10-11 Univ Nice Sophia Antipolis Prodrogues issues d'anti-proteases inhibitrices du virus de l'immunodeficience humaine (vih) pour l'amelioration de leur biodisponibilite, de leur tropisme vers et/ou de leur delivrance dans le systeme nerveux central
WO1999065870A2 (en) 1998-06-19 1999-12-23 Vertex Pharmaceuticals Incorporated Sulfonamide inhibitors of aspartyl protease
US6319946B1 (en) 1999-02-12 2001-11-20 Vertex Pharmaceuticals Incorporated Inhibitors of aspartyl protease
IL150929A0 (en) * 2000-01-28 2003-06-24 Rohm & Haas Pharmaceutical compounds comprising a pharmaceutically active moiety and a moiety comprising a substituent that enhances its properties
US6818787B2 (en) 2001-06-11 2004-11-16 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
US7202092B2 (en) * 2001-07-13 2007-04-10 Roche Diagnostics Operations, Inc. Indinavir derivatives useful in immunoassay
WO2003077902A1 (en) 2002-02-19 2003-09-25 Xenoport, Inc. Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
US8603949B2 (en) * 2003-06-17 2013-12-10 California Institute Of Technology Libraries of optimized cytochrome P450 enzymes and the optimized P450 enzymes
US7662987B2 (en) * 2003-07-15 2010-02-16 Xenoport, Inc. Methods for synthesis of acyloxyalkyl compounds
PT1660440E (pt) 2003-08-20 2012-05-15 Xenoport Inc Pró-fármacos de aciloxialquilcarbamato, métodos de síntese e utilização
WO2005066122A2 (en) 2003-12-30 2005-07-21 Xenoport, Inc. Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US541168A (en) * 1895-06-18 Frank e
GB1338169A (en) * 1971-03-09 1973-11-21 Smith Kline French Lab Ureas thioureas and guanidines
US4144346A (en) * 1977-01-31 1979-03-13 Janssen Pharmaceutica N.V. Novel 1-(1,3-dioxolan-2-ylmethyl)-1H-imidazoles
US4661473A (en) * 1984-03-27 1987-04-28 Merck & Co., Inc. Renin inhibitors containing peptide isosteres
WO1989003842A1 (en) * 1987-10-21 1989-05-05 The Upjohn Company Renin inhibitors containing a (1-amino-2-hydroxy-2-heterocyclic) ethyl moiety
DK24089D0 (da) * 1989-01-20 1989-01-20 Hans Bundgaard Novel prodrug derivatives of biologically active agents containing hydroxyl groups or nh-acidic groups
US5218114A (en) * 1991-04-10 1993-06-08 Merck & Co., Inc. Cholecystokinin antagonists
US5169952A (en) * 1991-07-02 1992-12-08 Merck & Co., Inc. Stereoselective production of hydroxyamide compounds from chiral α-amino epoxides
US5413999A (en) * 1991-11-08 1995-05-09 Merck & Co., Inc. HIV protease inhibitors useful for the treatment of AIDS
IL103613A (en) * 1991-11-08 1999-05-09 Merck & Co Inc VIH protease inhibitors, and the process of preparing intermediates and pharmaceutical preparations containing them.
US5463067A (en) * 1993-07-16 1995-10-31 Merck & Co., Inc. Process for making HIV protease inhibitors
CZ293953B6 (cs) * 1993-07-16 2004-08-18 Mercká@Áco@Źáinc Způsob výroby meziproduktů pro výrobu inhibitorů HIV@proteázy a příslušné meziprodukty
WO1995010281A1 (en) * 1993-10-13 1995-04-20 Merck & Co., Inc. Combination therapy for hiv infection
US5455351A (en) * 1993-12-13 1995-10-03 Abbott Laboratories Retroviral protease inhibiting piperazine compounds

Also Published As

Publication number Publication date
EP0729467A1 (en) 1996-09-04
HUT76270A (en) 1997-07-28
KR960705809A (ko) 1996-11-08
PL314486A1 (en) 1996-09-16
FI962073A (fi) 1996-05-15
US5733907A (en) 1998-03-31
IL111584A0 (en) 1995-01-24
SK61496A3 (en) 1996-11-06
CN1139432A (zh) 1997-01-01
NZ276622A (en) 1997-09-22
WO1995014016A1 (en) 1995-05-26
HU9601340D0 (en) 1996-07-29
JPH09505303A (ja) 1997-05-27
CA2174649A1 (en) 1995-05-26
FI962073A0 (fi) 1996-05-15
NO962000L (no) 1996-05-15
NO962000D0 (no) 1996-05-15
AU1096095A (en) 1995-06-06
AU687128B2 (en) 1998-02-19
CZ140696A3 (en) 1996-12-11

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