NO963254L - Makrocykliske difluorstatonderivater som er anvendbare som antivirale midler - Google Patents

Makrocykliske difluorstatonderivater som er anvendbare som antivirale midler

Info

Publication number
NO963254L
NO963254L NO963254A NO963254A NO963254L NO 963254 L NO963254 L NO 963254L NO 963254 A NO963254 A NO 963254A NO 963254 A NO963254 A NO 963254A NO 963254 L NO963254 L NO 963254L
Authority
NO
Norway
Prior art keywords
alkyl
hydrogen
piperazinyl
hydroxy
phenyl
Prior art date
Application number
NO963254A
Other languages
English (en)
Other versions
NO963254D0 (no
Inventor
Robert Allan Farr
Brent Ludvick Podlogar
Original Assignee
Merrell Pharma 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 Merrell Pharma Inc filed Critical Merrell Pharma Inc
Publication of NO963254L publication Critical patent/NO963254L/no
Publication of NO963254D0 publication Critical patent/NO963254D0/no

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0205Peptides 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)3-C(=0)-, e.g. statine or derivatives thereof
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Biochemistry (AREA)
  • Communicable Diseases (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Engineering & Computer Science (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Foreliggende oppfinnelse tilveie- bringer nye makrocykliske difluor- statonderivater som er anvendbare som . antivirale midler. Nærmere spesifikt 1 er disse nye forbindelser anvendbare l som inhibitorer av retrovirale prote- iaser som er nødvendige for replikasjon, i særdeleshet HIV-1 og HIV-2 virale ,proteaser, ved forhindring eller behandling av infeksjon med humant 1immunosvekkelsesvirus (HIV), og ved behandling av påfølgende patologiske tilstander slik som det ervervede immunosvekkelsessyndrom (AIDS) i pattedyr som er i stand til å bli i infisert med HIV-virus. foi Dir.::- ai ^v :o»melen: (CH2),-0 ! og stereoisomerer, hydrater og £armas«ytislc akseptable salter derav hvori P2 er C, ,-a)k'/l, cykJopentyJ, hydroxy C,6-aJJcyl, fenyj, benzyl eJler 3-tetrahydrofuryJ; P-. er valgt fra gruppen bestående av hydrogen, -CHj, -Cfl(CH3)j, -CH2Ca(Ca])j, -CH(CH])(CH2CHj), -CHjSH, -CHjCSjSCHj, -CHjOH, -CS(CHj)OB, -CH2(CHj)]NH2, -CH,(CHj)2NHC(=NH)NHj, -CH2COjH, -CH2CHjCO2H, -CHjCONH2, -CHjCH2CONHj, -'benzyl. -CH2 . hydrogen, C. j.-alkyJ, hydfoxy C^j.-a CH([ {Cli2)d-0-C!:2) f-R;l alkyJen] -OR,, CHIY) IZ) , l , POL, -( hvori PDL ei -ICH2)a-2-, 3- el)er 4-pyridyJ; Y er hydroxy C^jj-aJkyl, Cl.6-alkyl eller (CHj) e-C6H4- (v) e , ; 2 er (CHj) - 0-CHO, Ci_5-alkylen-0-(CH2ld-(0-CH2-CH2)e-o-C1_6-aJkyl, r.HO . 4, CONHR4, (CH)-0-(CH eJJer (CHjJ, hvori V er OR. eller hydroxy C, ,-aJkylen; forutsatt at d* *> 2 når RS er piperazinyl, substituert piperazinyl, piperidyl eller tnorfolinyl; R, er som definert for R,, forutsatt at R, er forskjelJig fra hydrogen når R, er hydrogen, eller R. og R, tatt sammen med nitrogenatomet tiJ hvilket de er bundet, er valgt fra gruppen bestående av: (O (i) R4 er hydrogen, c,_g-aJkyJ, fenyl eJJer benzyj; R5 er piperazinyl, substituert pipcrazinyl, piperidyj, morfoJinyJ, pyridyl, pyrazinyl, pyrimidinyj eJJer fenyl, hvori substituert piperazinyj er piperazinyl substituert med ett nifogenatom derav med CHO, C (O) NHH., c, -alkvl eller rn D . 4 1-4 r R-, er pyrimidyl, pyridyl, pyrazinyj eller fenyJ; R8 er C1_6-alkylen, hydroxy C, ,-alkyl eller c._,-alkyl; a er null, l, 2 eller 3; b er null eller 1; d og d' er hver uavhengig l eller 2; e og e1 er hver uavhengig null, l eJler 2; \ f er null elJer en; og x er l, 2, 3 eller 4.
NO963254A 1994-02-04 1996-08-02 Makrocykliske difluorstatonderivater som er anvendbare som antivirale midler NO963254D0 (no)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US19208094A 1994-02-04 1994-02-04
PCT/US1994/013711 WO1995021186A1 (en) 1994-02-04 1994-11-28 Macrocyclic difluorostatone derivatives useful as antiviral agents

Publications (2)

Publication Number Publication Date
NO963254L true NO963254L (no) 1996-08-02
NO963254D0 NO963254D0 (no) 1996-08-02

Family

ID=22708156

Family Applications (1)

Application Number Title Priority Date Filing Date
NO963254A NO963254D0 (no) 1994-02-04 1996-08-02 Makrocykliske difluorstatonderivater som er anvendbare som antivirale midler

Country Status (20)

Country Link
US (1) US5969132A (no)
EP (1) EP0742791B1 (no)
JP (1) JP3574455B2 (no)
KR (1) KR100367379B1 (no)
CN (1) CN1142830A (no)
AT (1) ATE198602T1 (no)
AU (1) AU684875B2 (no)
CA (1) CA2182476C (no)
DE (1) DE69426574T2 (no)
DK (1) DK0742791T3 (no)
ES (1) ES2155515T3 (no)
FI (1) FI963073A0 (no)
GR (1) GR3035623T3 (no)
HU (1) HUT74384A (no)
IL (1) IL112514A0 (no)
NO (1) NO963254D0 (no)
NZ (1) NZ277410A (no)
PT (1) PT742791E (no)
WO (1) WO1995021186A1 (no)
ZA (1) ZA95756B (no)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1633774T3 (da) 2003-06-18 2010-05-25 Tranzyme Pharma Inc Makrocykliske motilinreceptorantagonister

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH672792A5 (no) * 1985-02-19 1989-12-29 Sandoz Ag
FI865196A7 (fi) * 1985-04-19 1986-12-18 Upjohn Co Halostatiinisubstituoituja reniini-inhibiittoreita.
FI910084A7 (fi) * 1988-07-08 1991-01-07 Smithkline Beckman Corp Retroviraalisia proteaaseja sitovia peptidejä
US5071837A (en) * 1990-11-28 1991-12-10 Warner-Lambert Company Novel renin inhibiting peptides
EP0565631B1 (en) * 1991-01-02 1996-09-18 Merrell Pharmaceuticals Inc. Anti-viral compounds
AU711035B2 (en) * 1994-07-15 1999-10-07 Merrell Pharmaceuticals Inc. Difluorostatone antiviral agents

Also Published As

Publication number Publication date
CN1142830A (zh) 1997-02-12
ATE198602T1 (de) 2001-01-15
KR100367379B1 (ko) 2003-04-11
HUT74384A (en) 1996-12-30
WO1995021186A1 (en) 1995-08-10
PT742791E (pt) 2001-06-29
FI963073L (fi) 1996-08-02
EP0742791A1 (en) 1996-11-20
EP0742791B1 (en) 2001-01-10
JP3574455B2 (ja) 2004-10-06
ES2155515T3 (es) 2001-05-16
GR3035623T3 (en) 2001-06-29
AU684875B2 (en) 1998-01-08
FI963073A7 (fi) 1996-08-02
US5969132A (en) 1999-10-19
NO963254D0 (no) 1996-08-02
AU1262295A (en) 1995-08-21
NZ277410A (en) 1997-02-24
HU9602158D0 (en) 1996-09-30
JPH09508417A (ja) 1997-08-26
FI963073A0 (fi) 1996-08-02
DK0742791T3 (da) 2001-04-02
CA2182476C (en) 2000-12-26
DE69426574D1 (de) 2001-02-15
DE69426574T2 (de) 2001-08-09
IL112514A0 (en) 1995-05-26
ZA95756B (en) 1995-10-05

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