ES2145282T3 - Inhibidores de enzimas. - Google Patents

Inhibidores de enzimas.

Info

Publication number
ES2145282T3
ES2145282T3 ES95924405T ES95924405T ES2145282T3 ES 2145282 T3 ES2145282 T3 ES 2145282T3 ES 95924405 T ES95924405 T ES 95924405T ES 95924405 T ES95924405 T ES 95924405T ES 2145282 T3 ES2145282 T3 ES 2145282T3
Authority
ES
Spain
Prior art keywords
enzyme inhibitors
protecting group
amidino
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 - Lifetime
Application number
ES95924405T
Other languages
English (en)
Inventor
Harold Francis Dson
Richard M J Palmer
David Alan Sawyer
Richard Graham Knowles
Karl Witold Franzmann
Martin James Drysdale
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.)
Wellcome Foundation Ltd
Original Assignee
Wellcome Foundation 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 GBGB9509774.7A external-priority patent/GB9509774D0/en
Application filed by Wellcome Foundation Ltd filed Critical Wellcome Foundation Ltd
Application granted granted Critical
Publication of ES2145282T3 publication Critical patent/ES2145282T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/60—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C07C317/48—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • 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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Saccharide Compounds (AREA)
  • Steroid Compounds (AREA)
  • Immobilizing And Processing Of Enzymes And Microorganisms (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

SE DESCRIBE UN COMPUESTO DE FORMULA (I), DONDE R 1 ES UN GRUPO ALQUILO C{SUB,1-6}, LINEAL O RAMIFICADO, UN GRUPO ALQUENILO C{SUB,2-6}, UN GRUPO ALQUINILO C{SUB,2-6}, UN GRUPO CICLOALQUILO C{SUB,3-6}, O UN GRUPO CICLOALQUIL C{SUB,3-6} ALQUILO C{SUB,1-6}, CADA UNO OPCIONALMENTE SUSTITUIDO POR DOS O TRES GRUPOS, SELECCIONADOS INDEPENDIENTEMENTE ENTRE: -CN, -NO{SUB,2}; UN GRUPO -COR{SUP,2}, DONDE R{SUP,2} ES HIDROGENO, ALQUILO C{SUB,1-6}, -OR{SUP,3}, DONDE R{SUP,3} ES HIDROGENO O ALQUILO C{SUB,1-6}, O NR{SUP,4}R{SUP,5}, DONDE R{SUP,4} Y R{SUP,5} SON SELECCIONADOS INDEPENDIENTEMENTE ENTRE HIDROGENO O ALQUILO C{SUB,1-6}; UN GRUPO -S(O){SUB,M}R{SUP,6}, DONDE M ES 0, 1, O 2, R{SUP,6} ES HIDROGENO, ALQUILO C{SUB,1-6}, HIDROXI O NR{SUP,7}R{SUP,8}, DONDE R{SUP,7} Y R{SUP,8} SON, INDEPENDIENTEMENTE, HIDROGENO O UN GRUPO ALQUILO C{SUB,1-6}; UN GRUPO PO(OR{SUP,9}){SUB,2}, DONDE R{SUP,9} ES HIDROGENO O UN GRUPO ALQUILO C{SUB,1-6}; UN GRUPO NR{SUP,11}R{SUP,12}, DONDE R{SUP,11} Y R{SUP,12} SE SELECCIONAN INDEPENDIENTEMENTE ENTRE HIDROGENO, ALQUILO C{SUB,1-6}, O -S(O){SUB,M''}R{SUP,13}, DONDE M'' ES 0, 1, O 2 Y R{SUP,13} ES HIDROGENO, ALQUILO C{SUB,1-6}; HALO; O UN GRUPO -COR{SUP,14}, DONDE R{SUP,14} ES HIDROGENO, ALQUILO C{SUB,1-6} SUSTITUIDO CON DE UNO A TRES HALOATOMOS, ARILO C{SUB,6-10} O -COR{SUP,15}, DONDE R{SUP,15} ES HIDROGENO O ALQUILO C{SUB,1-6}; P ES 2 O 3; Q ES 1 O 2; Y N ES 0 O 1. TAMBIEN SE DESCRIBEN TODAS LAS SALES, ESTERES, AMIDAS Y PRECURSORES DE MEDICAMENTOS FISIOLOGICAMENTE ACEPTABLES; UTILIZACIONES FARMACEUTICAS; Y PROCEDIMIENTOS PARA LA PREPARACION DE LOS MISMOS.
ES95924405T 1994-06-15 1995-06-14 Inhibidores de enzimas. Expired - Lifetime ES2145282T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP94304314 1994-06-15
GBGB9509774.7A GB9509774D0 (en) 1995-05-15 1995-05-15 Enzyme inhibitors

Publications (1)

Publication Number Publication Date
ES2145282T3 true ES2145282T3 (es) 2000-07-01

Family

ID=26137155

Family Applications (2)

Application Number Title Priority Date Filing Date
ES95924405T Expired - Lifetime ES2145282T3 (es) 1994-06-15 1995-06-14 Inhibidores de enzimas.
ES99116304T Expired - Lifetime ES2189322T3 (es) 1994-06-15 1995-06-14 Intermediarios utiles en la preparacion de inhibidores de encimas.

Family Applications After (1)

Application Number Title Priority Date Filing Date
ES99116304T Expired - Lifetime ES2189322T3 (es) 1994-06-15 1995-06-14 Intermediarios utiles en la preparacion de inhibidores de encimas.

Country Status (29)

Country Link
US (2) USRE39576E1 (es)
EP (2) EP0765308B1 (es)
JP (2) JP2989010B2 (es)
KR (1) KR100430207B1 (es)
CN (1) CN1070849C (es)
AT (2) ATE229001T1 (es)
AU (1) AU692892B2 (es)
BR (1) BR9507995A (es)
CA (1) CA2192668A1 (es)
CY (2) CY2238B1 (es)
DE (2) DE69516141T2 (es)
DK (2) DK0957087T3 (es)
ES (2) ES2145282T3 (es)
FI (1) FI965019A (es)
GR (1) GR3033746T3 (es)
HK (1) HK1003935A1 (es)
HU (1) HUT77407A (es)
IL (2) IL114142A (es)
IS (1) IS4384A (es)
MX (1) MX9606136A (es)
MY (1) MY115437A (es)
NO (1) NO308655B1 (es)
NZ (1) NZ289157A (es)
PT (2) PT765308E (es)
RU (1) RU2162841C2 (es)
SI (2) SI0957087T1 (es)
TW (1) TW442453B (es)
WO (1) WO1995034534A1 (es)
ZA (1) ZA954940B (es)

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CN116194114A (zh) 2020-03-26 2023-05-30 葛兰素史密斯克莱知识产权发展有限公司 用于防止或治疗病毒感染的组织蛋白酶抑制剂

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GB9127376D0 (en) * 1991-12-24 1992-02-19 Wellcome Found Amidino derivatives
DE4310202A1 (de) 1992-03-30 1993-10-07 Ciba Geigy µ-Ketoimidoester als Stabilisatoren für chlorhaltige Polymerisate
FR2727111B1 (fr) * 1994-11-21 1997-01-17 Hoechst Lab Nouveaux analogues soufres d'aminoacides, leur procede de preparation et leurs applications comme medicaments

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RU2162841C2 (ru) 2001-02-10
PT765308E (pt) 2000-09-29
SI0765308T1 (en) 2000-08-31
NO965379L (no) 1996-12-13
USRE39576E1 (en) 2007-04-17
JP3614711B2 (ja) 2005-01-26
DK0957087T3 (da) 2003-03-24
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NO308655B1 (no) 2000-10-09
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EP0765308A1 (en) 1997-04-02
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ATE191470T1 (de) 2000-04-15
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CN1155276A (zh) 1997-07-23
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IL128717A0 (en) 2000-01-31
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EP0765308B1 (en) 2000-04-05
PT957087E (pt) 2003-04-30
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