ATE159728T1 - Cis-epoxide derivate, verwendbar als irreversible hiv-protease inhibitoren und verfahren und zwischenprodukte zu ihrer herstellung - Google Patents

Cis-epoxide derivate, verwendbar als irreversible hiv-protease inhibitoren und verfahren und zwischenprodukte zu ihrer herstellung

Info

Publication number
ATE159728T1
ATE159728T1 AT93119458T AT93119458T ATE159728T1 AT E159728 T1 ATE159728 T1 AT E159728T1 AT 93119458 T AT93119458 T AT 93119458T AT 93119458 T AT93119458 T AT 93119458T AT E159728 T1 ATE159728 T1 AT E159728T1
Authority
AT
Austria
Prior art keywords
cis
production
methods
protease inhibitors
intermediate products
Prior art date
Application number
AT93119458T
Other languages
English (en)
Inventor
Sung Chun Kim
Nakyen Choy
Chang Sun Lee
Young Chan Son
Hoill Choi
Jong Sung Koh
Heungsik Yoon
Chi Hyo Park
Sang Soo Kim
Original Assignee
Lucky Ltd
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
Priority claimed from KR1019920023089A external-priority patent/KR960000078B1/ko
Priority claimed from KR1019920023088A external-priority patent/KR960000077B1/ko
Priority claimed from KR1019930010811A external-priority patent/KR970011577B1/ko
Priority claimed from KR1019930021300A external-priority patent/KR0134497B1/ko
Priority claimed from KR1019930021299A external-priority patent/KR960011580B1/ko
Priority claimed from KR1019930021298A external-priority patent/KR0125104B1/ko
Application filed by Lucky Ltd filed Critical Lucky Ltd
Application granted granted Critical
Publication of ATE159728T1 publication Critical patent/ATE159728T1/de

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Classifications

    • 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
    • C07D303/38—Compounds containing oxirane rings with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • 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
    • A61P31/12—Antivirals
    • 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
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/02—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C217/04—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C217/06—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted
    • C07C217/08—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/20—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • 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
    • 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
    • C07D303/38—Compounds containing oxirane rings with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D303/46—Compounds containing oxirane rings with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals by amide or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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 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
    • C07D493/08—Bridged systems
    • 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
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02—Linear peptides containing at least one abnormal peptide link
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Veterinary Medicine (AREA)
  • Communicable Diseases (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epoxy Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
AT93119458T 1992-12-02 1993-12-02 Cis-epoxide derivate, verwendbar als irreversible hiv-protease inhibitoren und verfahren und zwischenprodukte zu ihrer herstellung ATE159728T1 (de)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
KR1019920023089A KR960000078B1 (ko) 1992-12-02 1992-12-02 인간 면역 결핍 바이러스 프로테아제의 억제 화합물 및 그의 제조방법
KR1019920023088A KR960000077B1 (ko) 1992-12-02 1992-12-02 인간 면역 결핍 바이러스 프로테아제의 억제 화합물 및 그의 제조방법
KR1019930010811A KR970011577B1 (ko) 1993-06-14 1993-06-14 항 에이즈(aids) 효과를 갖는 신규한 인간 면역 결핍 바이러스 프로테아제의 억제 화합물 및 그의 제조방법
KR1019930021300A KR0134497B1 (ko) 1993-10-14 1993-10-14 비가역적 에이치아이브이 프로테아제 억제제
KR1019930021299A KR960011580B1 (ko) 1993-10-14 1993-10-14 비가역적 에이치아이브이(hiv) 프로테아제 억제제의 중간체
KR1019930021298A KR0125104B1 (ko) 1993-10-14 1993-10-14 신규 인간 면역 결핍 바이러스(hiv) 프로테아제 억제 화합물 및 그의 제조방법

Publications (1)

Publication Number Publication Date
ATE159728T1 true ATE159728T1 (de) 1997-11-15

Family

ID=27555058

Family Applications (1)

Application Number Title Priority Date Filing Date
AT93119458T ATE159728T1 (de) 1992-12-02 1993-12-02 Cis-epoxide derivate, verwendbar als irreversible hiv-protease inhibitoren und verfahren und zwischenprodukte zu ihrer herstellung

Country Status (8)

Country Link
US (3) US5587388A (de)
EP (1) EP0601486B1 (de)
JP (2) JP2916359B2 (de)
AT (1) ATE159728T1 (de)
DE (1) DE69314911T2 (de)
DK (1) DK0601486T3 (de)
ES (1) ES2111700T3 (de)
GR (1) GR3025968T3 (de)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2565745B2 (ja) * 1988-08-03 1996-12-18 新明和工業株式会社 垂直循環式駐車装置
US5587388A (en) * 1992-12-02 1996-12-24 Lucky Limited Irreversible HIV protease inhibitors, intermediates, compositions and processes for the preparation thereof
US5670517A (en) * 1993-11-30 1997-09-23 Lg Chemical Limited Irreversible HIV protease inhibitors, compositions containing same and process for the preparation thereof
US5696134A (en) * 1993-11-30 1997-12-09 Lg Chemical Limited Irreversible HIV protease inhibitors, intermediates, compositions and processes for the preparation thereof
EP0812839A1 (de) * 1994-12-08 1997-12-17 LG Chemical Limited Irreversible HIV-Protease-Inhibitoren und diese enthaltende Zusammensetzungen und Verfahren zu ihrer Herstellung
EP0812857A1 (de) * 1994-12-08 1997-12-17 LG Chemical Limited Irreversible Inhibitoren der HIV-Protease, sie enthaltende Zubereitungen und Verfahren zu ihrer Herstellung
KR0125117B1 (ko) * 1994-06-15 1997-12-05 성재갑 항 에이즈(aids)효과를 갖는 신규한 인간 면역 결핍 바이러스(hiv)프로테아제 억제 화합물 및 그의 제조방법
US5679687A (en) * 1993-11-30 1997-10-21 Lg Chemical Limited Irreversible HIV protease inhibitors, compositions containing same and process for the preparation thereof
KR0159652B1 (ko) * 1995-10-26 1998-12-01 성재갑 항 에이즈 효과를 갖는 비가역적 인간 면역 결핍 바이러스 프로테아제 저해제 및 그의 제조방법
DE19641691A1 (de) 1996-10-10 1998-04-16 Bayer Ag Substituierte 2-Amino-4-alkylamino-1,3,5-triazine
JP2004525109A (ja) 2001-02-15 2004-08-19 キング・ファーマシューティカルズ・インコーポレイティッド 安定化された甲状腺ホルモン医薬組成物、及びその製法
US7101569B2 (en) 2001-08-14 2006-09-05 Franz G Andrew Methods of administering levothyroxine pharmaceutical compositions
PT2328875E (pt) 2008-07-17 2015-02-04 Univ Pittsburgh Agentes de nitróxido dirigidos
GB201814067D0 (en) * 2018-08-29 2018-10-10 Univ Edinburgh Compounds for the inhibition of cyclophilins
EP3932902B1 (de) * 2019-02-26 2026-01-28 Mitsubishi Gas Chemical Company, Inc. Aminzusammensetzung, aminverbindung, herstellungsverfahren und anwendung davon

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5142056A (en) * 1989-05-23 1992-08-25 Abbott Laboratories Retroviral protease inhibiting compounds
IE70080B1 (en) * 1989-02-16 1996-10-30 Sankyo Co Peptides having renin inhibitory activity their preparation and use
US5114937A (en) * 1989-11-28 1992-05-19 Warner-Lambert Company Renin inhibiting nonpeptides
EP0492136A3 (en) * 1990-12-20 1993-05-26 American Cyanamid Company Retroviral protease inhibitors derived from 3-chloro-2-chloromethyl-1-propene
US5268361A (en) * 1991-06-07 1993-12-07 Sri International Hydroxyazido derivatives and related compounds as renin inhibitors
US5587385A (en) * 1991-12-24 1996-12-24 Farmitalia Carlo Erba S.R.L. Arylidene-heterocyclic derivatives and process for their preparation
US5587388A (en) * 1992-12-02 1996-12-24 Lucky Limited Irreversible HIV protease inhibitors, intermediates, compositions and processes for the preparation thereof

Also Published As

Publication number Publication date
JPH072820A (ja) 1995-01-06
DK0601486T3 (da) 1998-07-20
EP0601486B1 (de) 1997-10-29
DE69314911D1 (de) 1997-12-04
JPH1081653A (ja) 1998-03-31
EP0601486A1 (de) 1994-06-15
JP2916359B2 (ja) 1999-07-05
JP2978848B2 (ja) 1999-11-15
DE69314911T2 (de) 1998-04-09
US5744621A (en) 1998-04-28
US5587388A (en) 1996-12-24
US5763631A (en) 1998-06-09
GR3025968T3 (en) 1998-04-30
ES2111700T3 (es) 1998-03-16

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