ES2193589T3 - Aldehido del acido n-(2-(5-benciloxicarbonil-amino-6-oxo-2-(4-fluorofenil)-1,6-dihidro-1-pirimidinil)acetoxil)-l-aspartico como un inhibidor (in vivo) del enzima de conversion de la interleucina-1beta. - Google Patents

Aldehido del acido n-(2-(5-benciloxicarbonil-amino-6-oxo-2-(4-fluorofenil)-1,6-dihidro-1-pirimidinil)acetoxil)-l-aspartico como un inhibidor (in vivo) del enzima de conversion de la interleucina-1beta.

Info

Publication number
ES2193589T3
ES2193589T3 ES98958672T ES98958672T ES2193589T3 ES 2193589 T3 ES2193589 T3 ES 2193589T3 ES 98958672 T ES98958672 T ES 98958672T ES 98958672 T ES98958672 T ES 98958672T ES 2193589 T3 ES2193589 T3 ES 2193589T3
Authority
ES
Spain
Prior art keywords
inhibitor
interleucina
benciloxicarbonil
aspartico
acetoxil
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
ES98958672T
Other languages
English (en)
Inventor
Gerald Paul Schielke
Aurash Shahripour
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.)
Abbott GmbH and Co KG
Warner Lambert Co LLC
Original Assignee
Abbott GmbH and Co KG
Warner Lambert Co LLC
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 Abbott GmbH and Co KG, Warner Lambert Co LLC filed Critical Abbott GmbH and Co KG
Application granted granted Critical
Publication of ES2193589T3 publication Critical patent/ES2193589T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous 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
    • A61P25/28—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
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Peptides Or Proteins (AREA)

Abstract

El compuesto **(Fórmula)** y los estereoisómeros y sales, ésteres, amidas y pro-fármacos del mismo farmacéuticamente aceptables. El compuesto 1 muestra una actividad in vivo como inhibidor de ICE inesperadamente superior a la de los inhibidores de ICE de técnicas anteriores. De hecho, este es el primer inhibidor de ICE que muestra actividad in vivo en un modelo animal de ataque después de su administración periférica. Compuestos de técnicas anteriores tales como el compuesto 2 no presentan esta actividad.
ES98958672T 1998-01-20 1998-11-20 Aldehido del acido n-(2-(5-benciloxicarbonil-amino-6-oxo-2-(4-fluorofenil)-1,6-dihidro-1-pirimidinil)acetoxil)-l-aspartico como un inhibidor (in vivo) del enzima de conversion de la interleucina-1beta. Expired - Lifetime ES2193589T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US7191898P 1998-01-20 1998-01-20

Publications (1)

Publication Number Publication Date
ES2193589T3 true ES2193589T3 (es) 2003-11-01

Family

ID=22104428

Family Applications (1)

Application Number Title Priority Date Filing Date
ES98958672T Expired - Lifetime ES2193589T3 (es) 1998-01-20 1998-11-20 Aldehido del acido n-(2-(5-benciloxicarbonil-amino-6-oxo-2-(4-fluorofenil)-1,6-dihidro-1-pirimidinil)acetoxil)-l-aspartico como un inhibidor (in vivo) del enzima de conversion de la interleucina-1beta.

Country Status (11)

Country Link
EP (1) EP1049703B1 (es)
JP (1) JP2002509153A (es)
AT (1) ATE232536T1 (es)
AU (1) AU1466399A (es)
CA (1) CA2309546A1 (es)
DE (1) DE69811404T2 (es)
DK (1) DK1049703T3 (es)
ES (1) ES2193589T3 (es)
PT (1) PT1049703E (es)
WO (1) WO1999036426A1 (es)
ZA (1) ZA99369B (es)

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US6716838B1 (en) 1999-05-19 2004-04-06 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents
US6458952B1 (en) 1999-05-19 2002-10-01 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
US6664255B1 (en) 1999-05-19 2003-12-16 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
US7015230B1 (en) 1999-05-19 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
US6750342B1 (en) 1999-05-19 2004-06-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US6653316B1 (en) 1999-05-19 2003-11-25 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US6867217B1 (en) 1999-05-19 2005-03-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade
US6808902B1 (en) 1999-11-12 2004-10-26 Amgen Inc. Process for correction of a disulfide misfold in IL-1Ra Fc fusion molecules
US6660885B2 (en) 2000-03-13 2003-12-09 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade
WO2001077079A2 (en) 2000-04-05 2001-10-18 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyridones useful for selective inhibition of the coagulation cascade
US20020022604A1 (en) 2000-04-05 2002-02-21 South Michael S. Polycyclic aryl and heteroaryl substituted 4-pyrones useful for selective inhibition of the coagulation cascade
CA2405684A1 (en) 2000-04-17 2001-10-25 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 1,4-quinones useful for selective inhibition of the coagulation cascade
WO2001087851A1 (en) * 2000-05-18 2001-11-22 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
PE20011350A1 (es) 2000-05-19 2002-01-15 Vertex Pharma PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE)
CA2416248A1 (en) * 2000-07-18 2002-01-24 Neurogen Corporation 5-substituted 2-aryl-4-pyrimidinones
US7119094B1 (en) 2000-11-20 2006-10-10 Warner-Lambert Company Substituted polycyclic aryl and heteroarpyl pyrazinones useful for selective inhibition of the coagulation cascade
US7015223B1 (en) 2000-11-20 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl 1,2,4-triazinones useful for selective inhibition of the coagulation cascade
US6624180B2 (en) 2000-11-20 2003-09-23 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade
US7364736B2 (en) 2001-06-26 2008-04-29 Amgen Inc. Antibodies to OPGL
JP2005519866A (ja) 2001-10-03 2005-07-07 ファルマシア・コーポレーション 凝固カスケードの選択阻害に有用な６員複素環式化合物
MXPA04003170A (es) 2001-10-03 2004-07-08 Pharmacia Corp Compuestos policiclicos, sustituidos, provisto de 5 miembros, utiles para la inhibicion selectiva de la cascada de coagulacion.
TWI289668B (en) 2002-09-06 2007-11-11 Amgen Inc Therapeutic human anti-IL-1R1 monoclonal antibody
WO2005117846A2 (en) 2004-05-27 2005-12-15 Vertex Pharmaceuticals Incorporated Ice inhibitors for the treatment of autoinflammatory diseases
HUE024556T2 (hu) 2004-03-12 2016-02-29 Vertex Pharma Eljárások és intermedierek aszparagin acetál kapszáz inhibitorok elõállítására
US20060128696A1 (en) 2004-05-15 2006-06-15 Annamaria Vezzani Treating seizures using ice inhibitors
WO2007015931A2 (en) 2005-07-28 2007-02-08 Vertex Pharmaceuticals Incorporated Caspase inhibitor prodrugs
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
EP3836954A1 (en) 2018-08-13 2021-06-23 Iltoo Pharma Combination of interleukin-2 with an interleukin 1 inhibitor, conjugates and therapeutic uses thereof
WO2023222565A1 (en) 2022-05-16 2023-11-23 Institut National de la Santé et de la Recherche Médicale Methods for assessing the exhaustion of hematopoietic stems cells induced by chronic inflammation

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5441960A (en) * 1992-04-16 1995-08-15 Zeneca Limited 1-pyrimidinylacetamide human leukocyte elastate inhibitors
CN1118458C (zh) * 1994-03-31 2003-08-20 弗特克斯药品有限公司 作为白细胞介素抑制剂的嘧啶基衍生物

Also Published As

Publication number Publication date
AU1466399A (en) 1999-08-02
JP2002509153A (ja) 2002-03-26
CA2309546A1 (en) 1999-07-22
EP1049703A1 (en) 2000-11-08
DE69811404D1 (de) 2003-03-20
DE69811404T2 (de) 2003-12-04
PT1049703E (pt) 2003-06-30
ZA99369B (en) 1999-07-20
ATE232536T1 (de) 2003-02-15
EP1049703B1 (en) 2003-02-12
WO1999036426A1 (en) 1999-07-22
DK1049703T3 (da) 2003-06-02

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