YU73702A - Karbamatni inhibitori kaspaze i njihova upotreba - Google Patents

Karbamatni inhibitori kaspaze i njihova upotreba

Info

Publication number
YU73702A
YU73702A YU73702A YUP73702A YU73702A YU 73702 A YU73702 A YU 73702A YU 73702 A YU73702 A YU 73702A YU P73702 A YUP73702 A YU P73702A YU 73702 A YU73702 A YU 73702A
Authority
YU
Yugoslavia
Prior art keywords
caspase inhibitors
inhibitors
carbamate
caspase
carbamate caspase
Prior art date
Application number
YU73702A
Other languages
English (en)
Inventor
David Bebbington
Jean-Damien Charrier
David Kay
Ronald Knegtel
Julian Golec
Michael Mortimore
John Studley
Original Assignee
Vertex Pharmaceuticals Incorporated
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 Vertex Pharmaceuticals Incorporated filed Critical Vertex Pharmaceuticals Incorporated
Publication of YU73702A publication Critical patent/YU73702A/sh

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • A61P31/04—Antibacterial agents
    • A61P31/06—Antibacterial agents for tuberculosis
    • 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
    • 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
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/82—Carbazoles; Hydrogenated carbazoles
    • C07D209/86—Carbazoles; Hydrogenated carbazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/06—Ring systems of three rings
    • C07D221/10—Aza-phenanthrenes
    • C07D221/12—Phenanthridines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/18—Dibenzazepines; Hydrogenated dibenzazepines
    • C07D223/22—Dibenz [b, f] azepines; Hydrogenated dibenz [b, f] azepines
    • C07D223/24—Dibenz [b, f] azepines; Hydrogenated dibenz [b, f] azepines with hydrocarbon radicals, substituted by nitrogen atoms, attached to the ring nitrogen atom
    • C07D223/26—Dibenz [b, f] azepines; Hydrogenated dibenz [b, f] azepines with hydrocarbon radicals, substituted by nitrogen atoms, attached to the ring nitrogen atom having a double bond between positions 10 and 11
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/18—Dibenzazepines; Hydrogenated dibenzazepines
    • C07D223/22—Dibenz [b, f] azepines; Hydrogenated dibenz [b, f] azepines
    • C07D223/24—Dibenz [b, f] azepines; Hydrogenated dibenz [b, f] azepines with hydrocarbon radicals, substituted by nitrogen atoms, attached to the ring nitrogen atom
    • C07D223/28—Dibenz [b, f] azepines; Hydrogenated dibenz [b, f] azepines with hydrocarbon radicals, substituted by nitrogen atoms, attached to the ring nitrogen atom having a single bond between positions 10 and 11
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/14—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems
    • C07D279/18—[b, e]-condensed with two six-membered rings
    • C07D279/22—[b, e]-condensed with two six-membered rings with carbon atoms directly attached to the ring nitrogen atom
    • C07D279/30—[b, e]-condensed with two six-membered rings with carbon atoms directly attached to the ring nitrogen atom with acyl radicals attached to the ring nitrogen atom

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Pulmonology (AREA)
  • Molecular Biology (AREA)
  • Addiction (AREA)
  • Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Biotechnology (AREA)

Abstract

Ovaj pronalazak daje inhibitore kaspaze formule (I) gde Z predstavlja kiseonik ili sumpor, R1 je vodonik, -CHN2R, -CH2OR, -CH2SR ili -CH2Y; Y je elektronegativna odlazeća grupa; R2 je CO2H, CH2CO2H ili njihov estar, amid ili izoster; R3 je grupa koja može da se smesti na S2 sub-mesto enzima kaspaze; R4 i R5, uzeti zajedno sa medjuatomom azota, formiraju heterociklični prsten; i R je opisano u ovoj prijavi. Ova jedinjenja su efikasni inhibitori apoptoze i izlučivanja IL-1ГЎ.[This invention provides caspase inhibitors of formula (I): wherein Z is oxygen or sulfur; R1 is hydrogen, -CHN2,R, CH2OR, CH2SR, or -CH2Y; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 and R5 are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1ГЎ secretion.
YU73702A 2000-03-29 2001-03-29 Karbamatni inhibitori kaspaze i njihova upotreba YU73702A (sh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US19282600P 2000-03-29 2000-03-29

Publications (1)

Publication Number Publication Date
YU73702A true YU73702A (sh) 2006-03-03

Family

ID=22711181

Family Applications (1)

Application Number Title Priority Date Filing Date
YU73702A YU73702A (sh) 2000-03-29 2001-03-29 Karbamatni inhibitori kaspaze i njihova upotreba

Country Status (32)

Country Link
US (2) US6689784B2 (sh)
EP (1) EP1268425B1 (sh)
JP (2) JP4298200B2 (sh)
KR (1) KR100858640B1 (sh)
CN (2) CN100358869C (sh)
AR (1) AR027993A1 (sh)
AT (1) ATE384695T1 (sh)
AU (2) AU2001249619B2 (sh)
BG (1) BG107136A (sh)
BR (1) BR0109588A (sh)
CA (1) CA2403959A1 (sh)
CZ (1) CZ20023227A3 (sh)
DE (1) DE60132567T2 (sh)
DK (1) DK1268425T3 (sh)
EA (1) EA005740B1 (sh)
EE (1) EE200200550A (sh)
ES (1) ES2296742T3 (sh)
HK (1) HK1052355B (sh)
HR (1) HRP20020782A2 (sh)
HU (1) HUP0301472A3 (sh)
IL (2) IL151829A0 (sh)
MX (1) MXPA02009633A (sh)
NO (1) NO325062B1 (sh)
NZ (1) NZ521639A (sh)
PE (1) PE20011267A1 (sh)
PL (1) PL201081B1 (sh)
PT (1) PT1268425E (sh)
SK (1) SK13922002A3 (sh)
TW (1) TWI318207B (sh)
WO (1) WO2001072707A2 (sh)
YU (1) YU73702A (sh)
ZA (1) ZA200207483B (sh)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2369619A1 (en) 1999-04-09 2000-10-19 Cytovia, Inc. Caspase inhibitors and the use thereof
CA2383002A1 (en) 1999-08-27 2001-03-08 Cytovia, Inc. Substituted .alpha.-hydroxy acid caspase inhibitors and the use thereof
ATE384695T1 (de) * 2000-03-29 2008-02-15 Vertex Pharma Carbamat caspase inhibitoren und deren verwendung
PE20011350A1 (es) 2000-05-19 2002-01-15 Vertex Pharma PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE)
US20040192889A1 (en) * 2001-03-30 2004-09-30 Dale Bredesen Cytotoxic peptides and peptidomimetics based thereon, and methods for use thereof
EP1392289A2 (en) 2001-05-23 2004-03-03 Vertex Pharmaceuticals Incorporated Caspase inhibitors and uses thereof
US7410956B2 (en) 2002-02-11 2008-08-12 Vertex Pharmaceuticals Incorporated Caspase inhibitor prodrugs
WO2003088917A2 (en) * 2002-04-19 2003-10-30 Vertex Pharmaceuticals Incorporated Regulation of tnf-alpha
EP1447093A1 (en) 2003-02-14 2004-08-18 Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts Inhibition of the CD95 ligand/receptor system for the treatment of neurological disorders and injuries
US20060217299A1 (en) * 2003-02-24 2006-09-28 Hirofumi Doi Degradation inhibitor for hepatitis b virus x interacting protein
AU2003902704A0 (en) * 2003-05-29 2003-06-19 Crc For Waste Management And Pollution Control Limited Of Unsw Process for producing a nanoscale zero-valent metal
EP1725548B1 (en) * 2004-03-12 2015-01-14 Vertex Pharmaceuticals Incorporated Processes and intermediates for the preparation of aspartic acetal caspase inhibitors
US7544855B2 (en) * 2004-04-23 2009-06-09 Buck Institute Transgenic mouse whose genome comprises an APP having a mutation at amino acid 664
CN102362867A (zh) * 2004-05-15 2012-02-29 沃泰克斯药物股份有限公司 使用ice抑制剂治疗癫痫发作
KR100619440B1 (ko) 2004-05-20 2006-09-08 한기종 포름아마이드 유도체 제조방법
CA2567080A1 (en) 2004-05-27 2005-12-15 Vertex Pharmaceuticals Incorporated Ice inhibitors for the treatment of autoinflammatory diseases
KR100619439B1 (ko) 2004-05-27 2006-09-08 한기종 포밀기 도입된 아민유도체의 제조방법
US8012751B2 (en) * 2005-03-31 2011-09-06 Wisconsin Alumni Research Foundation Differentiation of pluripotent embryonic stem cells
KR20080038369A (ko) * 2005-07-28 2008-05-06 버텍스 파마슈티칼스 인코포레이티드 카스파제 억제제 프로드럭
WO2007043388A1 (ja) * 2005-10-07 2007-04-19 Matsushita Electric Industrial Co., Ltd. 音響信号処理装置および音響信号処理方法
AU2006349611A1 (en) 2005-11-30 2008-05-02 Massachusetts Institute Of Technology Pathogen-detecting cell preservation systems
EP2049139A4 (en) * 2006-04-24 2009-06-24 Gloucester Pharmaceuticals Inc TREATMENT OF TUMORS EXPRESSING RAS
EP2043672A4 (en) * 2006-07-07 2009-10-21 Univ Leland Stanford Junior SELECTIVE CASPASE INHIBITORS
WO2008021745A2 (en) * 2006-08-16 2008-02-21 Itherx Pharmaceuticals, Inc. Hepatitis c virus entry inhibitors
EP2054076A2 (en) * 2006-08-21 2009-05-06 United Therapeutics Corporation Combination therapy for treatment of viral infections
WO2008106167A1 (en) * 2007-02-28 2008-09-04 Conatus Pharmaceuticals, Inc. Combination therapy comprising matrix metalloproteinase inhibitors and caspase inhibitors for the treatment of liver diseases
WO2008137567A1 (en) * 2007-05-01 2008-11-13 Cedars-Sinai Medical Center Caspase inhibitors in the treatment of infection-associated preterm delivery
KR101009588B1 (ko) * 2008-06-04 2011-01-20 거진산업주식회사 미세여과막을 이용한 부유고형물 처리장치
JP2012051804A (ja) * 2008-12-26 2012-03-15 Kyoto Univ Ｅｇ５阻害剤
KR101010350B1 (ko) * 2009-03-26 2011-01-25 삼성중공업 주식회사 역세척 여과장치
JP6006908B2 (ja) 2010-11-05 2016-10-12 ブランダイス ユニバーシティＢｒａｎｄｅｉｓ Ｕｎｉｖｅｒｓｉｔｙ Ｉｃｅ阻害化合物およびその使用
TW201236239A (en) * 2010-11-16 2012-09-01 Solvay Rechargeable metal or metal-ion cell
EP2490021A1 (en) 2011-02-18 2012-08-22 Biotempt B.V. Modulators of PRR and GPCR signalling
US9956260B1 (en) 2011-07-22 2018-05-01 The J. David Gladstone Institutes Treatment of HIV-1 infection and AIDS
MX2016014731A (es) 2014-05-12 2017-05-04 Conatus Pharmaceuticals Inc Tratamiento de las complicaciones de la enfermedad cronica del higado con enfermedades de caspasa.
WO2017079566A1 (en) 2015-11-05 2017-05-11 Conatus Pharmaceuticals, Inc. Caspase inhibitors for use in the treatment of liver cancer
RU2018127752A (ru) 2015-12-31 2020-01-31 Конатус Фармасьютикалз Инк. Способы применения ингибиторов каспаз при лечении заболеваний печени
BR112019005985A2 (pt) 2016-10-05 2019-06-25 Novartis Ag composições de combinação compreendendo agonistas de fxr para tratar ou prevenir uma doença ou distúrbio fibrótico, cirrótico
US20200277647A1 (en) * 2017-05-24 2020-09-03 Ramot At Tel-Aviv University Ltd. Chemiluminescent probes for imaging/detection of proteases
WO2022123062A1 (en) 2020-12-11 2022-06-16 INSERM (Institut National de la Santé et de la Recherche Médicale) Blocking caspase and/or fasl for preventing fatal outcome in covid-19 patients

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1991015577A1 (en) 1990-04-04 1991-10-17 Black, Roy, A. INTERLEUKIN 1'beta' PROTEASE
EP0600880B1 (en) 1991-08-30 2004-01-07 Vertex Pharmaceuticals Incorporated Interleukin 1- beta protease and interleukin 1-beta protease inhibitors
EP0618223A3 (en) 1993-03-08 1996-06-12 Sandoz Ltd Peptides, the release of Interleukin 1-Bêta, useful as anti-inflammatory agents.
CA2215211A1 (en) 1995-03-31 1996-10-03 Takeda Chemical Industries, Ltd. Cysteine protease inhibitor
US6136834A (en) * 1995-12-27 2000-10-24 Ono Pharmaceutical Co., Ltd. Tetrazole compounds and pharmaceutical agents containing such derivative
KR20000036056A (ko) 1996-09-12 2000-06-26 아이디유엔 파마슈티칼즈, 인코포레이티드 인터루킨-1β 전환 효소 및 관련 프로테아제의 억제제로서의 Ｃ-말단 변형된 (Ｎ-치환된)-2-인돌릴 디펩티드
KR20000049047A (ko) * 1996-10-11 2000-07-25 로즈 암스트롱, 크리스틴 에이. 트러트웨인 술폰아미드 인터루킨-1β 전환 효소 억제제
BR9712530A (pt) 1996-10-11 1999-10-19 Warner Lambert Co Inibidores de ésteres de asparato de enzima de conversão de interleucina-1beta
CA2306692C (en) * 1997-10-10 2010-09-21 Cytovia, Inc. Dipeptide apoptosis inhibitors and the use thereof
US6184210B1 (en) 1997-10-10 2001-02-06 Cytovia, Inc. Dipeptide apoptosis inhibitors and the use thereof
EP1076563B1 (en) 1998-03-16 2005-05-11 Cytovia, Inc. Dipeptide caspase inhibitors and the use thereof
US6242422B1 (en) 1998-10-22 2001-06-05 Idun Pharmacueticals, Inc. (Substituted)Acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases
KR20010110667A (ko) 1999-03-16 2001-12-13 추후보정 치환 2-아미노벤즈아미드 카스파제 저해제 및 그것의 용도
CA2369619A1 (en) 1999-04-09 2000-10-19 Cytovia, Inc. Caspase inhibitors and the use thereof
CA2383002A1 (en) * 1999-08-27 2001-03-08 Cytovia, Inc. Substituted .alpha.-hydroxy acid caspase inhibitors and the use thereof
ATE384695T1 (de) * 2000-03-29 2008-02-15 Vertex Pharma Carbamat caspase inhibitoren und deren verwendung

Also Published As

Publication number Publication date
BG107136A (bg) 2003-05-30
HRP20020782A2 (en) 2004-12-31
HUP0301472A2 (hu) 2003-08-28
KR100858640B1 (ko) 2008-09-17
CZ20023227A3 (cs) 2003-01-15
PL201081B1 (pl) 2009-03-31
NO20024661D0 (no) 2002-09-27
HK1052355A1 (en) 2003-09-11
JP2008266348A (ja) 2008-11-06
NO20024661L (no) 2002-11-26
ATE384695T1 (de) 2008-02-15
MXPA02009633A (es) 2003-03-10
IL151829A0 (en) 2003-04-10
TWI318207B (en) 2009-12-11
HK1052355B (zh) 2008-06-27
ZA200207483B (en) 2003-09-18
US7074782B2 (en) 2006-07-11
CN100358869C (zh) 2008-01-02
EE200200550A (et) 2004-02-16
US6689784B2 (en) 2004-02-10
PE20011267A1 (es) 2001-12-15
EP1268425B1 (en) 2008-01-23
AR027993A1 (es) 2003-04-23
WO2001072707A2 (en) 2001-10-04
NO325062B1 (no) 2008-01-28
US20040053920A1 (en) 2004-03-18
EP1268425A2 (en) 2003-01-02
NZ521639A (en) 2004-05-28
DK1268425T3 (da) 2008-05-05
BR0109588A (pt) 2003-02-04
JP2003528855A (ja) 2003-09-30
PL358430A1 (en) 2004-08-09
SK13922002A3 (sk) 2003-09-11
KR20020086711A (ko) 2002-11-18
CN1994298A (zh) 2007-07-11
AU2001249619B2 (en) 2006-08-17
DE60132567D1 (de) 2008-03-13
IL151829A (en) 2012-03-29
ES2296742T3 (es) 2008-05-01
CA2403959A1 (en) 2001-10-04
AU4961901A (en) 2001-10-08
EA200201030A1 (ru) 2003-02-27
PT1268425E (pt) 2008-04-01
JP4298200B2 (ja) 2009-07-15
EA005740B1 (ru) 2005-06-30
HUP0301472A3 (en) 2005-04-28
CN1422253A (zh) 2003-06-04
DE60132567T2 (de) 2009-01-22
US20020028803A1 (en) 2002-03-07
WO2001072707A3 (en) 2002-05-23

Similar Documents

Publication Publication Date Title
YU73702A (sh) Karbamatni inhibitori kaspaze i njihova upotreba
WO2002094263A3 (en) Caspase inhibitors and uses thereof
PT1178958E (pt) N-cianometilamidas como inibidores de proteases
YU83602A (sh) Derivati fenilglicina
DE60022508D1 (de) Inhibitoren von serin proteasen
NZ335981A (en) Ketobenzamides as calpain inhibitors
WO2003047512A3 (en) Compounds derived from an amine nucleus and pharmaceutical compositions comprising same
DE69835532D1 (de) Quinolin-enthaltende alpha-ketoamid-basierte inhibitoren von cystein- und serin protease
MXPA03011907A (es) Fluoropirrolidinas como inhibidores de dipeptidil peptidasa.
MX9804262A (es) Inhibidores derivados de d-aminoacidos de proteasas de cisteina y serina.
ATE326454T1 (de) Neue bernsteinsäure derivative als cysteine- protease-inhibitoren
NO20005261L (no) Nye heterocyklisk substituerte amider med cystein-protease- inhiberende virkning
MXPA02012160A (es) Composiciones medicinales las cuales contienen derivados de propenona.
TR200102912T2 (tr) Trombin ihtibit”rlerinin ”n ila‡larì.
MXPA03000223A (es) Derivados de pirrolidina como inhibidores de la enzima conversor de endotelina.
CA2342985A1 (en) Hydroxamate-containing cysteine and serine protease inhibitors
MXPA03000368A (es) Derivados de pirrolidina como inhibidores de metalproteasa.
MXPA03003942A (es) Compuestos bis-heterociclicos con actividad antitumoral y quimiosensibilizante.
ATE373636T1 (de) Amidderivate als inhibitoren der enzymatischen aktivität von renin
DE60108495D1 (en) Thrombin inhibitoren
EP1923386A3 (en) Carbamate caspase inhibitors and uses thereof
TR200102914T2 (tr) Trombin önleyicilerinin önilaçları
WO2003107317A8 (en) REMANENCE COMPENSATION FOR PLASMA DISPLAY PANELS
WO2003103574A3 (en) PROTEASE INHIBITORS
AR044258A1 (es) Intermedios utiles en la sintesis de los inhibidores de las proteasas de vih y procedimientos para preparar los mismos