DE69432176T2 - Verfahren zur herstellung von hiv protease inhibitoren - Google Patents

Verfahren zur herstellung von hiv protease inhibitoren

Info

Publication number
DE69432176T2
DE69432176T2 DE69432176T DE69432176T DE69432176T2 DE 69432176 T2 DE69432176 T2 DE 69432176T2 DE 69432176 T DE69432176 T DE 69432176T DE 69432176 T DE69432176 T DE 69432176T DE 69432176 T2 DE69432176 T2 DE 69432176T2
Authority
DE
Germany
Prior art keywords
hiv protease
protease inhibitors
producing hiv
intermediates
chem
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
DE69432176T
Other languages
English (en)
Other versions
DE69432176D1 (de
Inventor
David Askin
Paul Reider
Kai Rossen
J Varsolona
M Wells
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck and Co Inc
Original Assignee
Merck and 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 and Co Inc filed Critical Merck and Co Inc
Publication of DE69432176D1 publication Critical patent/DE69432176D1/de
Application granted granted Critical
Publication of DE69432176T2 publication Critical patent/DE69432176T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D303/00Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02Compounds containing oxirane rings
    • C07D303/36Compounds containing oxirane rings with hydrocarbon radicals, substituted by nitrogen atoms
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • 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
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Epoxy Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
DE69432176T 1993-07-16 1994-07-11 Verfahren zur herstellung von hiv protease inhibitoren Expired - Fee Related DE69432176T2 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US9262793A 1993-07-16 1993-07-16
PCT/US1994/007695 WO1995002583A1 (en) 1993-07-16 1994-07-11 Process for making hiv protease inhibitors

Publications (2)

Publication Number Publication Date
DE69432176D1 DE69432176D1 (de) 2003-04-03
DE69432176T2 true DE69432176T2 (de) 2003-11-27

Family

ID=22234214

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69432176T Expired - Fee Related DE69432176T2 (de) 1993-07-16 1994-07-11 Verfahren zur herstellung von hiv protease inhibitoren

Country Status (20)

Country Link
US (4) US5693803A (de)
EP (2) EP0708763B1 (de)
JP (1) JPH09500131A (de)
KR (2) KR100362800B1 (de)
CN (1) CN1046715C (de)
AT (1) ATE233249T1 (de)
AU (1) AU679770B2 (de)
CA (1) CA2167408C (de)
CZ (1) CZ13096A3 (de)
DE (1) DE69432176T2 (de)
ES (1) ES2191683T3 (de)
FI (1) FI960206A (de)
HU (1) HUT76789A (de)
IL (1) IL110255A (de)
NZ (1) NZ269400A (de)
RO (3) RO117176B1 (de)
RU (1) RU2134263C1 (de)
UA (1) UA45317C2 (de)
WO (1) WO1995002583A1 (de)
ZA (1) ZA945194B (de)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE116640T1 (de) * 1992-03-13 1995-01-15 Bio Mega Boehringer Ingelheim Substituierte pipecoline-säurederivate als hiv- protease-hemmer.
US5734055A (en) * 1993-11-22 1998-03-31 Koei Chemical Co. Ltd. Process for preparing N-tert-butyl-2-pyrazinecarboxamide and N-tert-butyl-2-piperazinecarboxamide
ES2116029T3 (es) * 1994-11-04 1998-07-01 Yamakawa Chemical Ind Procedimiento para preparar derivados de piperazina opticamente activos e intermedios para prepararlos.
ATE209190T1 (de) * 1995-05-23 2001-12-15 Lonza Ag Verfahren zur herstellung von optisch aktiven 2- piperazincarbonsäurederivaten
EP1125930A1 (de) * 1995-05-23 2001-08-22 Lonza Ag Optisch aktive 2-Piperazincarbonsäurederivate und Verfahren zu ihrer Herstellung
CA2201218C (en) * 1996-04-23 2004-09-28 Rudolf Fuchs Process for the preparation of optically active piperazine-2-carboxylic acid derivatives
US5981759A (en) * 1997-06-20 1999-11-09 Merck & Co., Inc. Process for indinavir intermediate
GB9808069D0 (en) * 1998-04-16 1998-06-17 Vanguard Medica Ltd Novel processes
JP2003514910A (ja) 1999-11-24 2003-04-22 メルク エンド カムパニー インコーポレーテッド Hivプロテアーゼ阻害剤としてのガンマ−ヒドロキシ−2−(フルオロアルキルアミノカルボニル)−1−ピペラジンペンタンアミド類
US7781478B2 (en) 2004-07-14 2010-08-24 Ptc Therapeutics, Inc. Methods for treating hepatitis C

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4097490A (en) * 1975-09-25 1978-06-27 Merck & Co., Inc. Pyroglutamic acid salts of t-butylamino-2,3-dihydroxypropane
US5026853A (en) * 1987-04-01 1991-06-25 Janssen Pharmaceutica N.V. 4-substituted-2(or 3)aminocarbonyl-1-piperazineacetamide
CA1340588C (en) * 1988-06-13 1999-06-08 Balraj Krishan Handa Amino acid derivatives
US5075337A (en) * 1989-07-26 1991-12-24 G. D. Searle & Co. Alpha-deuterated 2-alkylaminoacetamide derivatives having reduced toxicity for treatment of CNS disorders
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
CA2072237A1 (en) * 1991-07-02 1993-01-03 Merck & Co., Inc. Stereoselective production of hydroxyamide compounds from chiral –-amino epoxides
SG52731A1 (en) * 1991-11-08 1998-09-28 Merck & Co Inc Hiv protease inhibitors useful for the treatment of aids
US5484926A (en) * 1993-10-07 1996-01-16 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
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
US5461154A (en) * 1994-02-02 1995-10-24 Eli Lilly And Company Intermediate and process for making
TW472047B (en) * 1994-02-04 2002-01-11 Merck & Co Inc Process for making HIV protease inhibitors

Also Published As

Publication number Publication date
AU679770B2 (en) 1997-07-10
EP1310495A2 (de) 2003-05-14
ZA945194B (en) 1995-02-15
ATE233249T1 (de) 2003-03-15
CN1046715C (zh) 1999-11-24
UA45317C2 (uk) 2002-04-15
EP0708763B1 (de) 2003-02-26
FI960206A (fi) 1996-03-14
AU7326794A (en) 1995-02-13
US5637711A (en) 1997-06-10
KR100362800B1 (ko) 2002-11-29
FI960206A0 (fi) 1996-01-16
IL110255A0 (en) 1994-10-21
HU9600078D0 (en) 1996-03-28
RO117019B1 (ro) 2001-09-28
KR960703879A (ko) 1996-08-31
US5618939A (en) 1997-04-08
NZ269400A (en) 1997-11-24
RO117175B1 (ro) 2001-11-30
JPH09500131A (ja) 1997-01-07
RU2134263C1 (ru) 1999-08-10
EP1310495A9 (de) 2003-07-23
EP1310495A3 (de) 2003-05-21
DE69432176D1 (de) 2003-04-03
ES2191683T3 (es) 2003-09-16
HUT76789A (en) 1997-11-28
US5693803A (en) 1997-12-02
CA2167408C (en) 2003-09-16
CZ13096A3 (en) 1996-06-12
EP0708763A1 (de) 1996-05-01
CN1130905A (zh) 1996-09-11
KR100325279B1 (ko) 2002-07-22
CA2167408A1 (en) 1995-01-26
IL110255A (en) 1998-12-06
WO1995002583A1 (en) 1995-01-26
RO117176B1 (ro) 2001-11-30
US5861512A (en) 1999-01-19

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Legal Events

Date Code Title Description
8364 No opposition during term of opposition
8339 Ceased/non-payment of the annual fee