ATE141265T1 - Verfahren zur herstellung von intermediaten in der synthese von retroviralen protease inhibitoren - Google Patents

Verfahren zur herstellung von intermediaten in der synthese von retroviralen protease inhibitoren

Info

Publication number
ATE141265T1
ATE141265T1 AT93911369T AT93911369T ATE141265T1 AT E141265 T1 ATE141265 T1 AT E141265T1 AT 93911369 T AT93911369 T AT 93911369T AT 93911369 T AT93911369 T AT 93911369T AT E141265 T1 ATE141265 T1 AT E141265T1
Authority
AT
Austria
Prior art keywords
substituted
alkyl
arylalkyl
synthesis
protease inhibitors
Prior art date
Application number
AT93911369T
Other languages
English (en)
Inventor
John S Ng
Claire A Przybyla
Richard A Mueller
Michael L Vazquez
Daniel P Getman
Original Assignee
Searle & Co
Monsanto Co
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 Searle & Co, Monsanto Co filed Critical Searle & Co
Application granted granted Critical
Publication of ATE141265T1 publication Critical patent/ATE141265T1/de

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C213/02—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C213/08—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/04—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms
    • C07C275/20—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
    • C07C275/22—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings other than six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/04—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms
    • C07C275/20—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
    • C07C275/24—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02—Compounds containing oxirane rings
    • C07D303/36—Compounds containing oxirane rings with hydrocarbon radicals, substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Epoxy Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
AT93911369T 1992-05-20 1993-05-20 Verfahren zur herstellung von intermediaten in der synthese von retroviralen protease inhibitoren ATE141265T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US88655892A 1992-05-20 1992-05-20

Publications (1)

Publication Number Publication Date
ATE141265T1 true ATE141265T1 (de) 1996-08-15

Family

ID=25389250

Family Applications (1)

Application Number Title Priority Date Filing Date
AT93911369T ATE141265T1 (de) 1992-05-20 1993-05-20 Verfahren zur herstellung von intermediaten in der synthese von retroviralen protease inhibitoren

Country Status (11)

Country Link
EP (1) EP0641333B1 (de)
JP (3) JP3492362B2 (de)
KR (1) KR100290516B1 (de)
AT (1) ATE141265T1 (de)
AU (2) AU676479B2 (de)
CA (1) CA2131182C (de)
DE (1) DE69304051T2 (de)
DK (1) DK0641333T3 (de)
ES (1) ES2091000T3 (de)
GR (1) GR3020814T3 (de)
WO (2) WO1993023388A1 (de)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
KR100336699B1 (ko) 1992-08-25 2002-05-13 윌리암스 로저 에이 레트로바이러스 프로테아제 저해제로서 유용한히드록시에틸아미노 술폰아미드
US7141609B2 (en) 1992-08-25 2006-11-28 G.D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
US5723490A (en) * 1992-09-08 1998-03-03 Vertex Pharmaceuticals Incorporated THF-containing sulfonamide inhibitors of aspartyl protease
IS2334B (is) 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
US5783701A (en) * 1992-09-08 1998-07-21 Vertex Pharmaceuticals, Incorporated Sulfonamide inhibitors of aspartyl protease
CA2163456C (en) 1993-05-21 2009-06-23 Franco Lori New procedure to block the replication of reverse transcriptase dependent viruses by the use of inhibitors of deoxynucleotides synthesis
WO1995006061A1 (en) * 1993-08-20 1995-03-02 G.D. Searle & Co. Retroviral protease inhibitors and combinations thereof
US6093702A (en) * 1993-12-20 2000-07-25 The United States Of America As Represented By The Department Of Health And Human Services Mixtures of dideoxy-nucleosides and hydroxycarbamide for inhibiting retroviral spread
DE69512220T2 (de) * 1994-03-07 2000-03-16 Vertex Pharma Sulfonamidderivate als aspartylprotease-inhibitoren
US5475138A (en) * 1994-07-07 1995-12-12 Pharm-Eco Laboratories Incorporated Method preparing amino acid-derived diaminopropanols
CA2137406C (en) * 1994-12-06 2005-09-13 Pierre Louis Beaulieu Process for key intermediates for hiv protease inhibitors
US5481011A (en) * 1994-12-13 1996-01-02 Bristol-Myers Squibb Company Process for preparing N-protected amino acid α-halomethyl ketones and alcohols from N-protected amino acid esters
US5831117A (en) 1995-01-20 1998-11-03 G. D. Searle & Co. Method of preparing retroviral protease inhibitor intermediates
WO1996022287A1 (en) * 1995-01-20 1996-07-25 G.D. Searle & Co. Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors
US5691372A (en) * 1995-04-19 1997-11-25 Vertex Pharmaceuticals Incorporated Oxygenated-Heterocycle containing sulfonamide inhibitors of aspartyl protease
US5693847A (en) * 1995-04-19 1997-12-02 Vertex Pharmaceuticals Incorporated Heteroatom functionalized α-methyl ketones
US6004957A (en) * 1995-06-07 1999-12-21 Vertex Pharmaceuticals, Incorporated Sulfonamide inhibitors of aspartyl protease
US6037157A (en) 1995-06-29 2000-03-14 Abbott Laboratories Method for improving pharmacokinetics
US6063963A (en) * 1995-07-05 2000-05-16 Pharm-Eco Laboratories, Inc. Amino acid-derived diaminopropanols
CA2237936A1 (en) * 1995-11-16 1997-05-22 G.D. Searle & Co. N-protected/n-substituted-beta-amino hydroxy sulfonates
CA2190570C (en) * 1995-11-17 2005-05-03 Yutaka Honda Process for producing 3-amino-2-oxo-1-halogenopropane derivatives
US5914332A (en) 1995-12-13 1999-06-22 Abbott Laboratories Retroviral protease inhibiting compounds
US5919956A (en) * 1996-10-18 1999-07-06 Roche Vitamins Inc. Process for the C1 -homologization of protected phorenol
ZA9710071B (en) * 1996-11-21 1998-05-25 Abbott Lab Pharmaceutical composition.
US6232333B1 (en) 1996-11-21 2001-05-15 Abbott Laboratories Pharmaceutical composition
US6127556A (en) * 1996-12-31 2000-10-03 G. D. Searle & Co. Epoxide formation by continuous in-situ synthesis process
US6436989B1 (en) 1997-12-24 2002-08-20 Vertex Pharmaceuticals, Incorporated Prodrugs of aspartyl protease inhibitors
AP1717A (en) 1998-06-19 2007-01-30 Vertex Pharma Sulfonamide inhibitors of aspartyl protease.
ES2676151T3 (es) 2000-01-19 2018-07-17 Abbvie Inc. Formulaciones farmacéuticas mejoradas
FR2820136A1 (fr) * 2001-01-26 2002-08-02 Aventis Pharma Sa Nouveaux derives de l'uree, leur procede de preparation, leur application a titre de medicaments, compositions pharmaceutiques et nouvelle utilisation
FR2885129B1 (fr) 2005-04-29 2007-06-15 Proskelia Sas Nouveaux derives de l'ureee substituee parun thiazole ou benzothiazole, leur procede de preparation, leur application a titre de medicaments, les compositions pharmaceutiques les renfermant et utilisation.
AU2006316705B2 (en) 2005-11-25 2011-09-29 Galapagos Sas Urea derivatives useful as calcium receptor modulators
CN102816111B (zh) 2007-03-12 2014-08-06 尼克塔治疗公司 低聚物-蛋白酶抑制剂偶联物
US9095620B2 (en) 2008-03-12 2015-08-04 Nektar Therapeutics Reagents
US20120108501A1 (en) 2009-06-12 2012-05-03 Nektar Therapeutics Protease Inhibitors
CN112546969B (zh) * 2020-12-07 2022-12-23 安徽贝克制药股份有限公司 催化加氢连续生产装置和利托那韦中间体的制备方法

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1297631C (en) * 1985-12-23 1992-03-17 Sesha I. Natarajan Ureido renin inhibitors
DE3635907A1 (de) * 1986-10-22 1988-04-28 Merck Patent Gmbh Hydroxy-aminosaeurederivate
GB2200115B (en) * 1987-01-21 1990-11-14 Sandoz Ltd Novel peptide derivatives, their production and use
USH725H (en) * 1987-02-26 1990-01-02 E. R. Squibb & Sons, Inc. Ureido amino and imino acids, compositions and methods for use
DE3711911A1 (de) * 1987-04-08 1988-10-20 Bayer Ag Optisch aktive (alpha)-aminoaldehyde, verfahren zu ihrer herstellung und ihre verwendung zur stereoselektiven herstellung optisch aktiver ss-aminoalkohole
EP0374097A3 (de) * 1988-12-15 1991-06-12 Ciba-Geigy Ag Verwendung von Peptidisosteren als retrovirale Proteasehemmer
ATE164839T1 (de) * 1990-11-19 1998-04-15 Monsanto Co Retrovirale proteaseinhibitoren

Also Published As

Publication number Publication date
WO1993023368A1 (en) 1993-11-25
AU676479B2 (en) 1997-03-13
DE69304051T2 (de) 1997-01-23
EP0641333B1 (de) 1996-08-14
AU4253193A (en) 1993-12-13
DK0641333T3 (da) 1996-09-02
KR100290516B1 (ko) 2001-09-17
EP0641333A1 (de) 1995-03-08
DE69304051D1 (de) 1996-09-19
GR3020814T3 (en) 1996-11-30
WO1993023388A1 (en) 1993-11-25
JP3492362B2 (ja) 2004-02-03
ES2091000T3 (es) 1996-10-16
JP2003160545A (ja) 2003-06-03
AU4253093A (en) 1993-12-13
JP2003192648A (ja) 2003-07-09
JPH07508041A (ja) 1995-09-07
CA2131182A1 (en) 1993-11-25
KR950700893A (ko) 1995-02-20
CA2131182C (en) 2005-04-26

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Legal Events

Date Code Title Description
UEP Publication of translation of european patent specification
REN Ceased due to non-payment of the annual fee