NO932813L - Peptider som er i stand til aa inhibere aktiviteten av HIV protease, deres fremstilling og deres terapeutiske anvendelse - Google Patents

Peptider som er i stand til aa inhibere aktiviteten av HIV protease, deres fremstilling og deres terapeutiske anvendelse

Info

Publication number
NO932813L
NO932813L NO932813A NO932813A NO932813L NO 932813 L NO932813 L NO 932813L NO 932813 A NO932813 A NO 932813A NO 932813 A NO932813 A NO 932813A NO 932813 L NO932813 L NO 932813L
Authority
NO
Norway
Prior art keywords
inhibiting
activity
hiv protease
hydrogen
alkyl
Prior art date
Application number
NO932813A
Other languages
English (en)
Other versions
NO932813D0 (no
Inventor
Susumu Higashida
Mitsuya Sakurai
Yuichiro Yabe
Takashi Nishigaki
Tomoaki Komai
Hiroshi Handa
Original Assignee
Sankyo 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 Sankyo Co filed Critical Sankyo Co
Publication of NO932813D0 publication Critical patent/NO932813D0/no
Publication of NO932813L publication Critical patent/NO932813L/no

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/273—2-Pyrrolidones 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 other ring carbon atoms
    • C07D207/277—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D207/28—2-Pyrrolidone-5- carboxylic acids; Functional derivatives thereof, e.g. esters, nitriles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • C07D405/02—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
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—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
    • C07K5/0202—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-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • 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)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Virology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Analytical Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic 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)

Abstract

Forbindelser av formel (I): [hvori: R1 er hydrogen, alkyl, aralkyl, -COR", -CORb, -CSR", -CSRb, -S02Rb, -CONHRb, -CSNHR", -CONRbRb eller -CSNR"Rb; R2 er hydrogen eller alkyl; R3 er hydrogen, alkyliden, substituert alkyl, eller Rb; R* er eventuelt substi- tuert alkyl, sykloalkyl eller aryl; R5 er RbO-, RbRbN-, RbHN-, aralkyloksykar- bonyloksy eller aralkyloksykarbonyl- amino, eller R5 er -(CH2 )p-D-(CH2)r- [hvori D er en enkeltbinding, karbonyl, oksygen, svovel, -NH-, -(CH2=CH2)- eller -NHCO-; og E og E er hver O eller et helt tall fra l til 5]; A er -(CH2)m-B- ¿ (CH2)n- [hvori B er en enkeltbinding, karbonyl, oksygen, svovel, -NH-, -(CH2=CHj)- eller -NHCO-; og m og n er hver O eller et helt tall fra l til 5]; R* er alkoksy, aralkyloksy, aryloksy eller alkoksykarbonyl; Rb er eventuelt substituert alkyl, sykloalkyl, hetero- syklisk, aryl eller arylalkenyl]; og farmasøytisk akseptable salter og estere derav og prolegemidler derfor, har evne til å inhibere aktiviteten av HIV-protease og kan således anvendes for behandling og profylakse av AIDS.
NO932813A 1992-08-07 1993-08-06 Peptider som er i stand til aa inhibere aktiviteten av HIV protease, deres fremstilling og deres terapeutiske anvendelse NO932813L (no)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP21174692 1992-08-07

Publications (2)

Publication Number Publication Date
NO932813D0 NO932813D0 (no) 1993-08-06
NO932813L true NO932813L (no) 1994-02-08

Family

ID=16610902

Family Applications (1)

Application Number Title Priority Date Filing Date
NO932813A NO932813L (no) 1992-08-07 1993-08-06 Peptider som er i stand til aa inhibere aktiviteten av HIV protease, deres fremstilling og deres terapeutiske anvendelse

Country Status (16)

Country Link
US (1) US5629406A (no)
EP (1) EP0587311A1 (no)
KR (1) KR0177838B1 (no)
CN (1) CN1091432A (no)
AU (1) AU662434B2 (no)
CA (1) CA2103536A1 (no)
CZ (1) CZ161993A3 (no)
FI (1) FI933472A (no)
HU (1) HUT64774A (no)
IL (1) IL106600A (no)
MX (1) MX9304837A (no)
NO (1) NO932813L (no)
NZ (1) NZ248332A (no)
PH (1) PH31249A (no)
RU (1) RU2106357C1 (no)
ZA (1) ZA935697B (no)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6313094B1 (en) 1990-12-11 2001-11-06 Japan Energy Corporation β-amino-α-hydroxycarboxylic acid derivatives and HIV protease inhibitors
DE69524527D1 (de) * 1994-10-14 2002-01-24 Japan Energy Corp AIDS-hemmende Arzneizubereitung und Verfahren
DE19512484A1 (de) 1995-04-04 1996-10-17 Bayer Ag Kohlenhydratmodifizierte Cytostatika
US6008228A (en) * 1995-06-06 1999-12-28 Hoffman-La Roche Inc. Pharmaceutical compositions containing proteinase inhibitors
CA2179935C (en) * 1995-06-30 2010-09-07 Ryohei Kato Novel dipeptide compound or pharmaceutically acceptable salt thereof and medical use thereof
US6222043B1 (en) 1995-06-30 2001-04-24 Japan Energy Corporation Methods of preparing novel dipeptide compounds or pharmaceutically acceptable salts thereof
US6291432B1 (en) 1996-12-27 2001-09-18 Japan Energy Corporation Tripeptide compounds and anti-AIDS medicine
JP4006058B2 (ja) 1997-03-11 2007-11-14 第一三共株式会社 多臓器不全予防及び／又は治療剤
DK0950416T3 (da) 1997-03-14 2007-02-26 Daiichi Seiyaku Co Anvendelse af TCF-II til behandling af cancerrelateret tab af kropsvægt, anæmi og TNF-forhöjelse
WO1998051295A1 (fr) * 1997-05-14 1998-11-19 Nissui Pharmaceutical Co., Ltd. Inhibiteur de la protease du vih-1, leur procede de production, et compositions medicinales
ES2147162B1 (es) 1999-01-27 2001-03-16 Lacer Sa "s-nitrosotioles como agentes para el tratamiento de disfunciones circulatorias".
SE9902987D0 (sv) 1999-08-24 1999-08-24 Astra Pharma Prod Novel compounds
CO5300399A1 (es) 2000-02-25 2003-07-31 Astrazeneca Ab Heterocicliocs que contienen nitrogeno, proceso para su preparacion y composiciones farmaceuticas que los contienen
AR028948A1 (es) 2000-06-20 2003-05-28 Astrazeneca Ab Compuestos novedosos
US7005439B2 (en) 2000-06-20 2006-02-28 Astrazeneca Ab Compounds
GB0104050D0 (en) 2001-02-19 2001-04-04 Astrazeneca Ab Chemical compounds
AR035230A1 (es) 2001-03-19 2004-05-05 Astrazeneca Ab Compuestos de bencimidazol, proceso para su preparacion, composicion farmaceutica, proceso para la preparacion de dicha composicion farmaceutica, y usos de estos compuestos para la elaboracion de medicamentos
GB0107228D0 (en) 2001-03-22 2001-05-16 Astrazeneca Ab Chemical compounds
SE0101038D0 (sv) 2001-03-23 2001-03-23 Astrazeneca Ab Novel compounds
WO2002081454A1 (en) * 2001-04-09 2002-10-17 Dr. Reddy's Laboratories Ltd. Derivatives of aryl acids, their use in medicine, process for their preparation and pharmaceutical compositions containing them
CN100350036C (zh) 2001-04-27 2007-11-21 宝洁公司 用于控制生物膜的装置和方法
US7094909B2 (en) * 2001-06-11 2006-08-22 Agouron Pharmaceuticals, Inc. HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis
US7169932B2 (en) * 2001-06-11 2007-01-30 Pfizer Inc. HIV protease inhibitors, compositions containing the same, their pharmaceutical uses, material for their synthesis
HN2002000136A (es) * 2001-06-11 2003-07-31 Basf Ag Inhibidores de la proteasa del virus hiv, compuestos que contienen a los mismos, sus usos farmaceuticos y los materiales para su sintesis
SE0103818D0 (sv) 2001-11-15 2001-11-15 Astrazeneca Ab Chemical compounds
KR20040068240A (ko) 2001-12-14 2004-07-30 노보 노르디스크 에이/에스 호르몬 민감성 리파아제의 활성을 감소시키기 위한 화합물및 그들의 사용
SE0301369D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Chemical compounds
EP1692104A1 (en) * 2003-12-04 2006-08-23 Pfizer Inc. Methods of preparing compounds useful as protease inhibitors
JP2007513142A (ja) * 2003-12-04 2007-05-24 ファイザー インコーポレイテッド プロテアーゼ阻害剤として有用な化合物の製造法
WO2005121094A1 (en) * 2004-06-09 2005-12-22 Pfizer Limited Piperazine and piperidine derivatives as anti-hiv-agents
TW200738634A (en) 2005-08-02 2007-10-16 Astrazeneca Ab New salt
FR2904317A1 (fr) 2006-07-27 2008-02-01 Inst Nat Sante Rech Med Analogues d'halogenobenzamides marques a titre de radiopharmaceutiques
EP2085390A1 (en) 2008-01-31 2009-08-05 Institut National De La Sante Et De La Recherche Medicale (Inserm) Labelled analogues of halobenzamides as multimodal radiopharmaceuticals and their precursors

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CA2056911C (en) * 1990-12-11 1998-09-22 Yuuichi Nagano Hiv protease inhibitors
AU647239B2 (en) * 1991-02-08 1994-03-17 Sankyo Company Limited New beta-amino- alpha-hydroxycarboxylic acids and their use

Also Published As

Publication number Publication date
EP0587311A1 (en) 1994-03-16
CN1091432A (zh) 1994-08-31
ZA935697B (en) 1994-03-10
AU4443893A (en) 1994-02-10
IL106600A0 (en) 1993-12-08
KR0177838B1 (ko) 1999-04-01
HU9302286D0 (en) 1993-10-28
AU662434B2 (en) 1995-08-31
CA2103536A1 (en) 1994-02-08
US5629406A (en) 1997-05-13
FI933472A (fi) 1994-02-08
IL106600A (en) 1997-09-30
KR940003965A (ko) 1994-03-14
NO932813D0 (no) 1993-08-06
CZ161993A3 (en) 1994-02-16
PH31249A (en) 1998-06-18
NZ248332A (en) 1995-01-27
FI933472A0 (fi) 1993-08-05
MX9304837A (es) 1994-05-31
RU2106357C1 (ru) 1998-03-10
HUT64774A (en) 1994-02-28

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