PT2270005E - Pró-fármaco de um inibidor de ice - Google Patents

Pró-fármaco de um inibidor de ice Download PDF

Info

Publication number
PT2270005E
PT2270005E PT101775377T PT10177537T PT2270005E PT 2270005 E PT2270005 E PT 2270005E PT 101775377 T PT101775377 T PT 101775377T PT 10177537 T PT10177537 T PT 10177537T PT 2270005 E PT2270005 E PT 2270005E
Authority
PT
Portugal
Prior art keywords
prodrug
ice inhibitor
inhibitor
ice
Prior art date
Application number
PT101775377T
Other languages
English (en)
Inventor
Marion W Wannamaker
Robert J Davies
Original Assignee
Vertex Pharma
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 Pharma filed Critical Vertex Pharma
Publication of PT2270005E publication Critical patent/PT2270005E/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/14Drugs for genital or sexual disorders; Contraceptives for lactation disorders, e.g. galactorrhoea
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • 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
    • 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
    • A61P31/16Antivirals for RNA viruses for influenza or rhinoviruses
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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
    • C07D207/10Heterocyclic 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
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D477/00Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring
    • C07D477/02Preparation
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D477/00Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring
    • C07D477/10Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2
    • C07D477/12Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2 with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached in position 6
    • C07D477/16Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2 with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached in position 6 with hetero atoms or carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 3
    • C07D477/20Sulfur atoms
    • 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
    • C07K5/0202Peptides 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06191Dipeptides containing heteroatoms different from O, S, or N
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
PT101775377T 2000-05-19 2001-05-18 Pró-fármaco de um inibidor de ice PT2270005E (pt)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US20543900P 2000-05-19 2000-05-19

Publications (1)

Publication Number Publication Date
PT2270005E true PT2270005E (pt) 2015-10-21

Family

ID=22762189

Family Applications (2)

Application Number Title Priority Date Filing Date
PT01939230T PT1286989E (pt) 2000-05-19 2001-05-18 Pró-fármaco de um inibidor de ice
PT101775377T PT2270005E (pt) 2000-05-19 2001-05-18 Pró-fármaco de um inibidor de ice

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PT01939230T PT1286989E (pt) 2000-05-19 2001-05-18 Pró-fármaco de um inibidor de ice

Country Status (23)

Country Link
US (8) US7417029B2 (pt)
EP (3) EP1286989B1 (pt)
JP (2) JP4890719B2 (pt)
KR (1) KR100863144B1 (pt)
AP (1) AP2002002406A0 (pt)
AT (1) ATE543814T1 (pt)
AU (1) AU2001264770A1 (pt)
CA (1) CA2379972C (pt)
CY (1) CY1112448T1 (pt)
DK (2) DK1286989T3 (pt)
ES (2) ES2380915T3 (pt)
HK (1) HK1060881A1 (pt)
MX (1) MXPA02000751A (pt)
NO (1) NO324354B1 (pt)
NZ (1) NZ516703A (pt)
PE (1) PE20011350A1 (pt)
PL (1) PL207575B1 (pt)
PT (2) PT1286989E (pt)
SK (1) SK287070B6 (pt)
TR (1) TR200200769T1 (pt)
TW (1) TWI285642B (pt)
WO (1) WO2001090063A2 (pt)
ZA (1) ZA200200610B (pt)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2274642C2 (ru) 1998-03-19 2006-04-20 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы каспаз
EP2332579A3 (en) * 2000-02-10 2011-09-21 Abbott Laboratories Antibodies that bind human interleukin-18 and methods of making and using
PE20011350A1 (es) 2000-05-19 2002-01-15 Vertex Pharma PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE)
AU2003211052A1 (en) * 2002-02-11 2003-09-04 Vertex Pharmaceuticals Incorporated Phospholipids as caspase inhibitor prodrugs
SI1487541T1 (sl) 2002-03-22 2009-02-28 Serono Lab Uporaba inhibitorjev il-18 za zdravljenje in /alipreventivo bolezni perifernega oĺ˝ilja
CA2545733A1 (en) * 2003-11-10 2005-05-26 Vertex Pharmaceuticals Incorporated Methods for monitoring il-18
US7968684B2 (en) 2003-11-12 2011-06-28 Abbott Laboratories IL-18 binding proteins
WO2005053665A1 (en) * 2003-12-01 2005-06-16 Vertex Pharmaceuticals Incorporated Treating infectious diseases using ice inhibitors
CA2820541A1 (en) * 2004-02-27 2005-09-15 Vertex Pharmaceuticals Incorporated Caspase inhibitors and uses thereof
JP2007525503A (ja) 2004-02-27 2007-09-06 バーテックス ファーマシューティカルズ インコーポレイテッド カスパーゼインヒビターおよびそれらの使用
AU2011226946B2 (en) * 2004-02-27 2012-05-03 Vertex Pharmaceuticals Incoporated Caspase Inhibitors and Uses Thereof
US7381827B2 (en) 2004-03-12 2008-06-03 Vertex Pharmaceuticals Incorporated Processes and intermediates
JP4848367B2 (ja) * 2004-05-15 2011-12-28 バーテックス ファーマシューティカルズ インコーポレイテッド Iceインヒビターを使用した発作の処置
CN1980658A (zh) * 2004-05-27 2007-06-13 沃泰克斯药物股份有限公司 治疗自身炎性疾病的ice抑制剂
CA2610691C (en) 2005-06-03 2015-12-01 Laboratoires Serono S.A. Use of il-18bp isoforms for the treatment and/or prevention of neurological inflammatory diseases
ATE529430T1 (de) * 2005-07-28 2011-11-15 Vertex Pharma Caspase-hemmer-propharmaka
JP2009538912A (ja) * 2006-05-31 2009-11-12 バーテックス ファーマシューティカルズ インコーポレイテッド インターロイキン−1β変換酵素阻害剤の経口制御放出剤形
MX2009005252A (es) * 2006-11-17 2009-05-28 Abbott Lab Aminopirrolidinas como antagonistas del receptor de quimiocina.
CN101772577A (zh) 2007-08-03 2010-07-07 塞诺菲-安万特股份有限公司 半胱天冬蛋白酶成像探针
US20100158905A1 (en) 2008-12-19 2010-06-24 Nuon Therapeutics, Inc. Combination therapy of arthritis with tranilast
WO2011094426A1 (en) 2010-01-29 2011-08-04 The United State Of America, As Represented By The Secretary, Department Of Health & Human Services Caspase inhibitors
EP2635906A4 (en) 2010-11-05 2014-04-02 Univ Brandeis ICE INHIBITING COMPOUNDS AND USES THEREOF
ES2665301T3 (es) 2011-04-15 2018-04-25 Genesis Technologies Limited Inhibidores selectivos de cisteína proreasa y usos de los mismos
US9956260B1 (en) 2011-07-22 2018-05-01 The J. David Gladstone Institutes Treatment of HIV-1 infection and AIDS
EP2848696A1 (en) 2013-09-13 2015-03-18 Sanofi-Aventis Deutschland GmbH Caspase-1 imaging probes
JP7213555B2 (ja) 2016-12-23 2023-01-27 シーエーエスピー-エイド インク. 神経学的状態の予防および治療のためのカスパーゼ1の阻害およびその使用
ES2769975B2 (es) * 2018-12-27 2020-12-04 Univ Murcia Inhibidores de caspasa 1 para el tratamiento de anemia
WO2021011500A2 (en) * 2019-07-16 2021-01-21 Rush University Medical Center Use of a benzoate containing composition to treat neurodegenerative disorders
MX2022013549A (es) 2020-05-01 2023-01-16 Medstar Health Inc Metodos para tratar la covid-19.
WO2022074134A1 (en) 2020-10-07 2022-04-14 Etienne Jacotot Treatments of coronavirus infections, cytokine release syndrome, cytokine storm syndrome, or diseases associated with excessive activation of inflammasomes by the use of inhibitors of inflammatory caspases
FR3114741A1 (fr) 2020-10-07 2022-04-08 Etienne Jacotot Traitements des infections à coronavirus, du syndrome de libération de cytokine, du syndrome de la tempête de cytokines ou des maladies associées à l'activation excessive des inflammasomes par l'utilisation d'inhibiteurs des caspases inflammatoires.
WO2023006645A1 (en) * 2021-07-28 2023-02-02 F. Hoffmann-La Roche Ag Haloacethydrazides useful as aep inhibitors

Family Cites Families (124)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6204261B1 (en) 1995-12-20 2001-03-20 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β Converting enzyme inhibitors
US5874424A (en) * 1995-12-20 1999-02-23 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
US4465679A (en) * 1983-01-31 1984-08-14 Usv Pharmaceutical Corporation 1,2-Diaza-3-one compounds, their use in treating hypertension and pharmaceutical compositions thereof
IL72523A (en) 1983-08-12 1988-06-30 Takeda Chemical Industries Ltd 3-amino-4-oxo-2,3,4,5-tetrahydro-1,5-benzoxazepine derivatives,their production and pharmaceutical compositions containing them
US5055451A (en) * 1986-12-22 1991-10-08 Syntex Inc. Aryloxy and arylacyloxy methyl ketones as thiol protease inhibitors
US5158936A (en) * 1986-12-22 1992-10-27 Syntex (U.S.A.) Inc. Aryloxy and arylacyloxy methyl ketones as thiol protease inhibitors
US5008245A (en) * 1988-10-27 1991-04-16 University Of Kentucky Research Foundation Novel peptidyl carbamate inhibitors of the enzyme elastase
ZA905737B (en) 1989-07-26 1991-05-29 Merrell Dow Pharma Novel peptidase inhibitors
NZ235155A (en) 1989-09-11 1993-04-28 Merrell Dow Pharma Peptidase substrates in which the carboxy terminal group has been replaced by a tricarbonyl radical
US5416013A (en) * 1990-04-04 1995-05-16 Sterling Winthrop Inc. Interleukin 1β protease and interleukin 1β protease inhibitors
AU7775991A (en) 1990-04-04 1991-10-30 Immunex Corporation Interleukin 1beta protease
ATE172713T1 (de) 1991-03-15 1998-11-15 Hoechst Ag Verfahren zur diastereoselektiven reduktiven pinakol-kupplung von homochiralen alpha- aminoaldehyden
DE69226820T2 (de) 1991-06-21 1999-05-12 Merck & Co Inc Peptidylderivate als Inhibitoren von Interleukin-1B-konvertierenden Enzymen
JP3190431B2 (ja) 1991-07-01 2001-07-23 三菱化学株式会社 ケトン誘導体
US6348570B1 (en) 1991-08-16 2002-02-19 Merck & Co., Inc. Chromophore containing compounds and their use in determining interleukin-1β convertase activity
US5278061A (en) 1991-08-16 1994-01-11 Merck & Co., Inc. Affinity chromatography matrix useful in purifying interleukin-1β converting enzyme
DE69229252T2 (de) 1991-08-16 1999-12-16 Merck & Co Inc DNS, welche das Interleukin-1B-Vorläufer-Converting-Enzym kodiert
EP0533226A3 (en) 1991-08-16 1993-08-18 Merck & Co. Inc. Novel chromophore containing compounds
CA2111100C (en) 1991-08-30 2004-11-02 Roy A. Black Interleukin-1 beta protease and interleukin-1 beta protease inhibitors
EP0541946B1 (de) * 1991-10-07 1996-07-17 Hoechst Aktiengesellschaft Verfahren zur diastereoselektiven reduktiven Pinakol-Kupplung von homochiralen alpha-Aminoaldehyden
GB9123326D0 (en) 1991-11-04 1991-12-18 Sandoz Ltd Improvements in or relating to organic compounds
WO1993012076A1 (en) 1991-12-13 1993-06-24 Corvas International Inc. Reagents for automated synthesis of peptide analogs
EP0547699A1 (en) 1991-12-19 1993-06-23 Merck & Co. Inc. Peptidyl derivatives as inhibitors of interleukin-1B converting enzyme
AU3479593A (en) 1992-01-31 1993-09-01 Merck & Co., Inc. Peptidyl derivatives as inhibitors of interleukin-1beta converting enzyme
EP0627926B1 (en) * 1992-02-21 1998-08-05 Merck & Co., Inc. (a New Jersey corp.) PEPTIDYL DERIVATIVES AS INHIBITORS OF INTERLEUKIN-1$g(b) CONVERTING ENZYME
AU4634993A (en) 1992-06-24 1994-01-24 Merck & Co., Inc. Dna encoding precursor interleukin 1beta converting enzyme
DE69319432T2 (de) 1992-07-31 1998-10-29 Pfizer Peptide aus Derivaten der 4-Amino-2.2.-Difluoro-3-Oxo-1.6-Hexandisäure als Wirkstoffe gegen Entzündungen
CA2109646C (en) * 1992-11-24 2000-03-07 Gaston O. Daumy Para-nitroanilide peptides
EP0618223A3 (en) 1993-03-08 1996-06-12 Sandoz Ltd Peptides, the release of Interleukin 1-Bêta, useful as anti-inflammatory agents.
TW494094B (en) 1993-04-29 2002-07-11 Vertex Pharma Peptide analogs as irreversible interleukin-1β protease inhibitors and pharmaceutical compositions comprising the same
US5462939A (en) * 1993-05-07 1995-10-31 Sterling Winthrop Inc. Peptidic ketones as interleukin-1β-converting enzyme inhibitors
US5411985A (en) * 1993-05-17 1995-05-02 Merck & Co., Inc. Gamma-pyrone-3-acetic acid as an inhibitor or interleukin-1 β inventory enzyme
JPH0789951A (ja) 1993-06-03 1995-04-04 Sterling Winthrop Inc インターロイキン−1β転換酵素阻害剤
JPH0725887A (ja) 1993-06-04 1995-01-27 Sterling Winthrop Inc インターロイキン−1β転換酵素阻害剤
JPH08511690A (ja) 1993-06-24 1996-12-10 ザ・ジェネラル・ホスピタル・コーポレーション プログラムされた細胞死遺伝子及びタンパク質
EP0739506B1 (en) 1993-06-30 1999-01-13 Ford Motor Company Limited Method and system for controlling an automotive hvac system
WO1995005192A1 (en) 1993-08-13 1995-02-23 Merck & Co., Inc. SUBSTITUTED KETONE DERIVATIVES AS INHIBITORS OF INTERLEUKIN-1β CONVERTING ENZYME
US5714484A (en) 1993-12-08 1998-02-03 Prototek, Inc. α-(1,3-dicarbonylenol ether) methyl ketones as cysteine protease inhibitors
US5486623A (en) * 1993-12-08 1996-01-23 Prototek, Inc. Cysteine protease inhibitors containing heterocyclic leaving groups
ES2210289T3 (es) 1994-03-31 2004-07-01 Vertex Pharmaceuticals Incorporated Derivados de pirimidinilo como inhibidores de interleuquinas.
EP0758891A4 (en) 1994-04-29 1997-12-03 Sanofi Winthrop Inc HALOMETHYL AMIDES USED AS IL-1-g (b) PROTEASE INHIBITORS.
BE1008343A3 (nl) 1994-05-06 1996-04-02 Dsm Nv Bidentaat fosfineligand
US5492824A (en) 1994-05-12 1996-02-20 Basf Ag Ice and ice-like compositions and methods of making same
US5552400A (en) * 1994-06-08 1996-09-03 Sterling Winthrop Inc. Fused-bicyclic lactams as interleukin-1β converting enzyme inhibitors
US5716929A (en) * 1994-06-17 1998-02-10 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US5756466A (en) * 1994-06-17 1998-05-26 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US6420522B1 (en) 1995-06-05 2002-07-16 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
US5847135A (en) 1994-06-17 1998-12-08 Vertex Pharmaceuticals, Incorporated Inhibitors of interleukin-1β converting enzyme
US6057119A (en) 1994-06-17 2000-05-02 Vertex Pharmaceuticals, Incorporated Crystal structure and mutants of interleukin-1β converting enzyme
US5565430A (en) 1994-08-02 1996-10-15 Sterling Winthrop Inc. Azaaspartic acid analogs as interleukin-1β converting enzyme inhibitors
US5704001A (en) 1994-08-04 1997-12-30 Qualcomm Incorporated Sensitivity weighted vector quantization of line spectral pair frequencies
GB2292149A (en) 1994-08-09 1996-02-14 Ferring Res Ltd Peptide inhibitors of pro-interleukin-1beta converting enzyme
US5498616A (en) * 1994-11-04 1996-03-12 Cephalon, Inc. Cysteine protease and serine protease inhibitors
TW394764B (en) 1995-02-14 2000-06-21 Mitsubishi Chemcal Corp Oxygen-containing heterocyclic derivatives
KR0144921B1 (ko) * 1995-02-17 1998-07-01 김광호 반도체 메모리소자의 커패시터 구조 및 그 제조방법
JPH09165360A (ja) 1995-03-31 1997-06-24 Takeda Chem Ind Ltd システインプロテアーゼ阻害剤
WO1996030395A2 (en) 1995-03-31 1996-10-03 Takeda Chemical Industries, Ltd. Cysteine protease inhibitor
US5798442A (en) 1995-04-21 1998-08-25 Merck Frosst Canada, Inc. Peptidyl derivatives as inhibitors of pro-apoptotic cysteine proteinases
EP0859779A4 (en) 1995-08-31 2000-04-12 Smithkline Beecham Corp INTERLEUKIN CONVERSION ENZYME AND APOPTOSIS
EP0851760A4 (en) 1995-08-31 1998-11-25 Smithkline Beecham Corp INTERLEUKIN CONVERSION ENZYME AND APOPTOSIS
US5744451A (en) 1995-09-12 1998-04-28 Warner-Lambert Company N-substituted glutamic acid derivatives with interleukin-1 β converting enzyme inhibitory activity
EP0761680A3 (en) * 1995-09-12 1999-05-06 Ono Pharmaceutical Co., Ltd. Tetrazole compounds having Interleukin-1beta converting enzyme inhibitory activity
US5843904A (en) 1995-12-20 1998-12-01 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1βconverting enzyme
EP0900791A1 (en) * 1995-12-27 1999-03-10 Ono Pharmaceutical Co., Ltd. Tetrazole derivatives and drugs containing the same as the active ingredient
WO1998001133A1 (fr) 1996-07-08 1998-01-15 Yamanouchi Pharmaceutical Co., Ltd. Inhibiteurs de la resorption osseuse
WO1998004539A1 (fr) 1996-07-29 1998-02-05 Mitsubishi Chemical Corporation Derives heterocycliques oxygenes
IL125190A (en) 1996-09-12 2003-01-12 Idun Pharmaceuticals Inc Tricyclic compounds for the inhibition of the ice/ced-3 protease family of enzymes and pharmaceutical compositions containing the same
US5869519A (en) * 1996-12-16 1999-02-09 Idun Pharmaceuticals, Inc. C-terminal modified (n-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases
EP0920444B1 (en) 1996-09-12 2002-12-18 Idun Pharmaceuticals, Inc. C-TERMINAL MODIFIED (N-SUBSTITUTED)-2-INDOLYL DIPEPTIDES AS INHIBITORS OF THE ICE/ced-3 FAMILY OF CYSTEINE PROTEASES
US6200969B1 (en) 1996-09-12 2001-03-13 Idun Pharmaceuticals, Inc. Inhibition of apoptosis using interleukin-1β-converting enzyme (ICE)/CED-3 family inhibitors
EP0874850B1 (en) 1996-09-12 2002-04-10 Idun Pharmaceuticals, Inc. Novel tricyclic compounds for the inhibition of the ice/ced-3 protease family of enzymes
US5968927A (en) 1996-09-20 1999-10-19 Idun Pharmaceuticals, Inc. Tricyclic compounds for the inhibition of the ICE/ced-3 protease family of enzymes
WO1998016502A1 (en) 1996-10-11 1998-04-23 Warner-Lambert Company ASPARTATE ESTER INHIBITORS OF INTERLEUKIN-1β CONVERTING ENZYME
KR20000049047A (ko) 1996-10-11 2000-07-25 로즈 암스트롱, 크리스틴 에이. 트러트웨인 술폰아미드 인터루킨-1β 전환 효소 억제제
US5919790A (en) 1996-10-11 1999-07-06 Warner-Lambert Company Hydroxamate inhibitors of interleukin-1β converting enzyme
ZA979327B (en) 1996-10-18 1998-05-11 Vertex Pharma Inhibitors of serine proteases, particularly hepatitis C virus NS3 protease.
US6184244B1 (en) 1996-12-16 2001-02-06 Idun Pharmaceuticals, Inc. C-terminal modified (N-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases
US5877197A (en) * 1996-12-16 1999-03-02 Karanewsky; Donald S. C-terminal modified (N-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases
US6054487A (en) 1997-03-18 2000-04-25 Basf Aktiengesellschaft Methods and compositions for modulating responsiveness to corticosteroids
HUP9700816A3 (en) 1997-04-28 1999-06-28 Gyogyszerkutato Intezet 3(r)-3-amino-4-carboxy-butiraldehyde derivatives inhibiting release of interleukin-1-beta
FR2766188B1 (fr) 1997-07-15 2000-02-11 Hoechst Marion Roussel Inc Nouveau procede de preparation de derives amines d'alkyloxy furanone, composes issus de ce procede et utilisation de ces composes
US6184210B1 (en) 1997-10-10 2001-02-06 Cytovia, Inc. Dipeptide apoptosis inhibitors and the use thereof
US6054470A (en) 1997-12-18 2000-04-25 Boehringer Ingelheim Pharmaceuticals, Inc. Src family SH2 domain inhibitors
AU1466399A (en) 1998-01-20 1999-08-02 Basf Aktiengesellschaft N-(2-(5-benzyloxycarbonyl-amino-6-oxo-2-(4-fluorophenyl)-1,6 -dihydro-1-pyrimidinyl)aceto- xyl)-l-aspartic acid aldehyde as an (in vivo) inhibitor of interleukin-1beta converting enzyme (ice)
RU2274642C2 (ru) 1998-03-19 2006-04-20 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы каспаз
US6197750B1 (en) 1998-07-02 2001-03-06 Idun Pharmaceuticals, Inc. C-terminal modified oxamyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases
US6323180B1 (en) 1998-08-10 2001-11-27 Boehringer Ingelheim (Canada) Ltd Hepatitis C inhibitor tri-peptides
US6242422B1 (en) 1998-10-22 2001-06-05 Idun Pharmacueticals, Inc. (Substituted)Acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases
WO2000055127A1 (en) 1999-03-16 2000-09-21 Merck Frosst Canada & Co. Gamma-ketoacid dipeptides as inhibitors of caspase-3
DE60030097T2 (de) 1999-03-16 2007-03-08 Cytovia, Inc., San Diego Substituierte 2-aminobenzamin caspase inhibitoren und ihre verwendung
EP1177168B1 (en) 1999-04-09 2007-05-30 Cytovia, Inc. Caspase inhibitors and the use thereof
AU773317B2 (en) 1999-07-19 2004-05-20 Merck Canada Inc. Pyrazinones, compositions containing such compounds
ES2219381T3 (es) 1999-08-06 2004-12-01 Vertex Pharmaceuticals Incorporated Inhibidores de caspasa y usos de los mismos.
US6442565B1 (en) 1999-08-13 2002-08-27 Hiddenmind Technology, Inc. System and method for transmitting data content in a computer network
KR20020033777A (ko) 1999-08-27 2002-05-07 추후보정 치환된 α-히드록시 산 카스파제 억제제 및 이의 용도
AR026748A1 (es) 1999-12-08 2003-02-26 Vertex Pharma Un compuesto inhibidor de caspasas, una composicion farmaceutica que lo comprende, un metodo para la sintesis del mismo y un compuesto intermediario paradicha sintesis
EA005740B1 (ru) 2000-03-29 2005-06-30 Вертекс Фармасьютикалз Инкорпорейтед Карбаматные ингибиторы каспазы и их использование
ATE297946T1 (de) 2000-04-03 2005-07-15 Vertex Pharma Inhibitoren von serin proteasen, speziell der hepatitis-c-virus ns3-protease
CA2402128A1 (en) 2000-04-24 2001-11-01 Vertex Pharmaceuticals Incorporated Process and intermediates for making substituted aspartic acid acetals
TWI291462B (en) 2000-04-25 2007-12-21 Daiichi Sankyo Co Ltd Hydrate crystal of neuraminic acid compound
PE20011350A1 (es) 2000-05-19 2002-01-15 Vertex Pharma PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE)
TR200200767T1 (tr) 2000-05-23 2002-09-23 Vertex Pharmaceuticals Incorporated Kaspaz engelleyiciler ve kullanımları
AU7527901A (en) 2000-06-07 2001-12-17 Vertex Pharma Caspase inhibitors and uses thereof
DK1385870T3 (da) 2000-07-21 2010-07-05 Schering Corp Peptider som inhibitorer af NS3-serinprotease fra hepatitis C-virus
JP2004509120A (ja) 2000-09-13 2004-03-25 バーテックス ファーマシューティカルズ インコーポレイテッド カスパーゼ阻害剤およびそれらの用途
US6846806B2 (en) 2000-10-23 2005-01-25 Bristol-Myers Squibb Company Peptide inhibitors of Hepatitis C virus NS3 protein
ATE359274T1 (de) 2000-11-21 2007-05-15 Vertex Pharma Imidazol- und benzimidazol- caspase inhibitoren und deren verwendung
GB0107924D0 (en) 2001-03-29 2001-05-23 Angeletti P Ist Richerche Bio Inhibitor of hepatitis C virus NS3 protease
EP1381602A1 (en) 2001-04-19 2004-01-21 Vertex Pharmaceuticals Incorporated Heterocyclyldicarbamides as caspase inhibitors
EP1392289A2 (en) 2001-05-23 2004-03-03 Vertex Pharmaceuticals Incorporated Caspase inhibitors and uses thereof
KR100926244B1 (ko) 2001-07-11 2009-11-12 버텍스 파마슈티칼스 인코포레이티드 브릿지된 바이사이클릭 세린 프로테아제 억제제
EP1436248A2 (en) 2001-10-09 2004-07-14 Vertex Pharmaceuticals Incorporated Process for synthesizing aspartic and glutamic acid derivatives and diazoketone intermediates thereof
AU2003211052A1 (en) 2002-02-11 2003-09-04 Vertex Pharmaceuticals Incorporated Phospholipids as caspase inhibitor prodrugs
AU2003225088A1 (en) 2002-04-19 2003-11-03 Vertex Pharmaceuticals Incorporated Regulation of tnf-alpha
US7001899B2 (en) 2002-06-10 2006-02-21 The Procter & Gamble Company Interleukin converting enzyme inhibitors
US7138395B2 (en) 2002-06-10 2006-11-21 The Procter & Gamble Company Interleukin-1β converting enzyme inhibitors
US7041696B2 (en) 2002-06-17 2006-05-09 The Procter & Gamble Company Interleukin-1β converting enzyme inhibitors
AR040350A1 (es) 2002-06-28 2005-03-30 Vertex Pharma Inhibidores de caspasa y usos de los mismos
TW200500343A (en) 2002-12-20 2005-01-01 Vertex Pharma Caspase inhibitors and uses thereof
PE20050159A1 (es) 2003-05-27 2005-04-19 Vertex Pharma Derivados de acido 3-[2-(3-amino-2-oxo-2h-piridin-1-il)-acetilamino]-4-oxo-pentanoico como inhibidores de caspasa
CA2545733A1 (en) 2003-11-10 2005-05-26 Vertex Pharmaceuticals Incorporated Methods for monitoring il-18
JP2007525503A (ja) 2004-02-27 2007-09-06 バーテックス ファーマシューティカルズ インコーポレイテッド カスパーゼインヒビターおよびそれらの使用
US7381827B2 (en) 2004-03-12 2008-06-03 Vertex Pharmaceuticals Incorporated Processes and intermediates
CN1980658A (zh) 2004-05-27 2007-06-13 沃泰克斯药物股份有限公司 治疗自身炎性疾病的ice抑制剂

Also Published As

Publication number Publication date
ES2380915T3 (es) 2012-05-21
US20020013278A1 (en) 2002-01-31
EP1396492B1 (en) 2012-02-01
SK1022002A3 (en) 2002-07-02
PE20011350A1 (es) 2002-01-15
US9156880B2 (en) 2015-10-13
JP2003534320A (ja) 2003-11-18
US20110301096A1 (en) 2011-12-08
EP2270005A1 (en) 2011-01-05
PT1286989E (pt) 2012-03-22
TR200200769T1 (tr) 2002-09-23
EP1396492A1 (en) 2004-03-10
CA2379972A1 (en) 2001-11-29
WO2001090063A3 (en) 2002-02-21
US20170022249A1 (en) 2017-01-26
ZA200200610B (en) 2003-01-23
DK2270005T3 (en) 2015-09-21
DK1286989T3 (da) 2012-02-27
PL365171A1 (en) 2004-12-27
EP2270005B1 (en) 2015-07-08
EP1286989B1 (en) 2012-02-01
AP2002002406A0 (en) 2002-03-31
US20090012149A1 (en) 2009-01-08
US7417029B2 (en) 2008-08-26
US8022041B2 (en) 2011-09-20
JP4890719B2 (ja) 2012-03-07
US20200048306A1 (en) 2020-02-13
US20130331310A1 (en) 2013-12-12
EP1286989A2 (en) 2003-03-05
PL207575B1 (pl) 2011-01-31
US20150284426A1 (en) 2015-10-08
AU2001264770A1 (en) 2001-12-03
US8329662B2 (en) 2012-12-11
NO20020287L (no) 2002-03-19
KR20020025199A (ko) 2002-04-03
NZ516703A (en) 2004-07-30
JP5285130B2 (ja) 2013-09-11
JP2011236235A (ja) 2011-11-24
SK287070B6 (sk) 2009-11-05
US9994613B2 (en) 2018-06-12
TWI285642B (en) 2007-08-21
US9487555B2 (en) 2016-11-08
US20180327449A1 (en) 2018-11-15
ATE543814T1 (de) 2012-02-15
NO324354B1 (no) 2007-09-24
CY1112448T1 (el) 2015-12-09
NO20020287D0 (no) 2002-01-18
ES2548869T3 (es) 2015-10-21
WO2001090063A2 (en) 2001-11-29
CA2379972C (en) 2009-07-21
HK1060881A1 (en) 2004-08-27
KR100863144B1 (ko) 2008-10-14
MXPA02000751A (es) 2002-07-22

Similar Documents

Publication Publication Date Title
PT2270005E (pt) Pró-fármaco de um inibidor de ice
GB0025782D0 (en) Use of inhibitors
SI1686119T1 (sl) Derivati pirimidin-5-ona kot inhibitorji ldl-pla2
AU2001258771A1 (en) -secretase inhibitors
IL153633A0 (en) Lipid-rich plaque inhibitors
AU3467101A (en) Mucin synthesis inhibitors
AP2002002593A0 (en) Protease inhibitors
HUP0300061A3 (en) Use of il-18 inhibitors
AU8323701A (en) Inhibitors of p38
AU2002222627A1 (en) Tak1 inhibitors
IL153421A0 (en) Protease inhibitors
AU3955101A (en) Apoptosis inhibitor
AU2002214038A1 (en) Inhibitors of transglutaminases
IL151087A0 (en) Protease inhibitors
HUP0301964A3 (en) Protease inhibitors
AU1212002A (en) Use of lipase inhibitors
AU2002221882A1 (en) Use of 3-hydroxyl-3-methylglutaryl-coenzyme-a-reductase inhibitors
AU2001290852A1 (en) Inhibitors of rho c
GB0004895D0 (en) Inhibitor
GB0005017D0 (en) Inhibitor
AU2001268051A1 (en) Spla2 inhibitors
GB0000829D0 (en) Growth inhibitor
AU2001263003A1 (en) Carboxyalkylether-acat inhibitor combinations
GB0029730D0 (en) Inhibitors
GB0015996D0 (en) Inhibitors