HRP20150844T1 - Spojevi piruvamida kao inhibitori alergena peptidaze od kuä†nih grinja skupine 1 - Google Patents

Spojevi piruvamida kao inhibitori alergena peptidaze od kuä†nih grinja skupine 1 Download PDF

Info

Publication number
HRP20150844T1
HRP20150844T1 HRP20150844TT HRP20150844T HRP20150844T1 HR P20150844 T1 HRP20150844 T1 HR P20150844T1 HR P20150844T T HRP20150844T T HR P20150844TT HR P20150844 T HRP20150844 T HR P20150844T HR P20150844 T1 HRP20150844 T1 HR P20150844T1
Authority
HR
Croatia
Prior art keywords
asthma
piperizino
compound according
optionally substituted
independently
Prior art date
Application number
HRP20150844TT
Other languages
English (en)
Inventor
Clive Robinson
Jihui Zhang
David Ronald Garrod
Trevor Robert Perrior
Gary Karl Newton
Kerry Jenkins
Rebekah Elisabeth Beevers
Meriel Ruth MAYOR
Mark Richard Stewart
Original Assignee
St. George's Hospital Medical School
The University Of Manchester
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 St. George's Hospital Medical School, The University Of Manchester filed Critical St. George's Hospital Medical School
Publication of HRP20150844T1 publication Critical patent/HRP20150844T1/hr

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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N37/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
    • A01N37/44—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing at least one carboxylic group or a thio analogue, or a derivative thereof, and a nitrogen atom attached to the same carbon skeleton by a single or double bond, this nitrogen atom not being a member of a derivative or of a thio analogue of a carboxylic group, e.g. amino-carboxylic acids
    • A01N37/46—N-acyl derivatives
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/02—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms
    • A01N43/04—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom
    • A01N43/14—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom six-membered rings
    • A01N43/16—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom six-membered rings with oxygen as the ring hetero atom
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/02—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms
    • A01N43/24—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with two or more hetero atoms
    • A01N43/26—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with two or more hetero atoms five-membered rings
    • A01N43/28—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with two or more hetero atoms five-membered rings with two hetero atoms in positions 1,3
    • A01N43/30—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with two or more hetero atoms five-membered rings with two hetero atoms in positions 1,3 with two oxygen atoms in positions 1,3, condensed with a carbocyclic ring
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/34—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
    • A01N43/36—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom five-membered rings
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/34—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
    • A01N43/36—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom five-membered rings
    • A01N43/38—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom five-membered rings condensed with carbocyclic rings
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/34—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
    • A01N43/40—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/34—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
    • A01N43/40—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
    • A01N43/42—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/48—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/48—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with two nitrogen atoms as the only ring hetero atoms
    • A01N43/60—1,4-Diazines; Hydrogenated 1,4-diazines
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/72—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/72—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms
    • A01N43/84—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms as ring hetero atoms six-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07—Tetrapeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • 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
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/14—Ectoparasiticides, e.g. scabicides
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0827—Tripeptides containing heteroatoms different from O, S, or N
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Veterinary Medicine (AREA)
  • Dentistry (AREA)
  • Plant Pathology (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Pest Control & Pesticides (AREA)
  • Agronomy & Crop Science (AREA)
  • Environmental Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Otolaryngology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Virology (AREA)

Claims (31)

1. Spoj, naznačen time, da je odabran od spojeva sljedeće formule, i njegove farmaceutski prihvatljive soli, njegovi hidrati i solvati: [image] -R1 je neovisno -H ili -R1A; -R1A je zasićeni alifatski C1-6alkil, te je po želji supstituiran s jednim ili više supstituenata -RX1; -R2 je -H; -R3 je neovisno -H ili -R3A; -R3A je zasićeni alifatski C1-3alkil; -R4 je -R4A; -R4A je -Me; -R5 je -H; -R6 je -H ili -R6A; -R6A je zasićeni alifatski C1-3alkil; -R7 je -H, -R7A, ili -R7B; -R7A je zasićeni alifatski C1-6alkil; -R7B je zasićeni -L7B1-R7BB, ili -R7BB; -L7B1- je zasićeni alifatski C1-3alkilen; -R7BB je neovisno -R7BB1, -R7BB2, -R7BB3, ili -R7BB4; -R7BB1 je neovisno fenil ili naftil, te je po želji supstituiran s jednim ili više supstituenata -RX3; -R7BB2 je C5-10heteroaril, te je po želji supstituiran s jednim ili više supstituenata -RX3; -R7BB3 je C3-7cikloalkil, te je po želji supstituiran s jednim ili više supstituenata -RX2, ili je po želji staljen na benzen-prsten koji je po želji supstituiran s jednim ili više supstituenata -RX3; -R7BB4 je zasićeni premošteni C5-10cikloalkil, te je po želji supstituiran s jednim ili više supstituenata -RX2; -R8 je -H; -R9 je neovisno -H ili -R9A; -R9A je zasićeni alifatski C1-4alkil; -R10 je neovisno -R10A, -R10B, -R10C, ili -R10D; -R10A je neovisno fenil ili naftil, te je po želji supstituiran s jednim ili više supstituenata -RX3; -R10B je C5-10heteroaril, te je po želji supstituiran s jednim ili više supstituenata -RX3; -R10C je zasićeni C3-7cikloalkil, te je po želji supstituiran s jednim ili više supstituenata -RX2; -R10D je nearomatski C3-10heterociklil, te je po želji supstituiran s jednim ili više supstituenata -RX2; ili -R9 i -R10, kada se uzimaju zajedno s atomom dušika ili atomom ugljika na koje su priključeni, tvore nearomatski C5-7heterociklički laktam-prsten koji je po želji supstituiran s jednim ili više supstituenata -RX2, ili koji je po želji stavljen na benzen-prsten koji je po želji supstituiran s jednim ili više supstituenata -RX3; -R11 je neovisno -H, -R11A, ili -R11B; -R11A je neovisno -RZ1, -RZ2, -RZ3, -RZ4, -RZ5, -LZ-RZ2, -LZ-RZ3, -LZ-RZ4, ili -LZ-RZ5; -RZ1 je zasićeni alifatski C1-6alkil, te je po želji supstituiran s jednim ili više supstituenata -RX1; svaki -RZ2 je zasićeni C3-7cikloalkil, te je po želji supstituiran s jednim ili više supstituenata -RX2; svaki -RZ3 je neovisno -RZ3A, ili -RZ3B; svaki -RZ3A je nearomatski C3-7heterociklil, te je po želji supstituiran s jednim ili više supstituenata -RX2; svaki -RZ3B je zasićeni premošteni C5-10heterociklil, te je po želji supstituiran s jednim ili više supstituenata -RX2; svaki -RZ4 je neovisno fenil ili naftil, te je po želji supstituiran s jednim ili više supstituenata -RX3; svaki -RZ5 je C5-10heteroaril, te je po želji supstituiran s jednim ili više supstituenata -RX3; svaki -LZ- je zasićeni alifatski C1-4alkilen; -R11B je -CRJ1RJ2-C(=O)-NRJ3RJ4; -RJ1 je neovisno -H, ili zasićeni alifatski C1-4alkil; -RJ2 je neovisno -H, ili zasićeni alifatski C1-4alkil; -RJ3 je neovisno -H, zasićeni alifatski C1-4alkil, fenil, ili benzil; -RJ4 je neovisno -H, zasićeni alifatski C1-4alkil, fenil, ili benzil; ili -NRJ3RJ4 je C3-10heterociklil-skupina, te je po želji supstituiran s jednim ili više supstituenata -RX2; -R12 je neovisno -H, ili -R12A; -R12A je zasićeni alifatski C1-4alkil; pri čemu je svaki -RX1 neovisno odabran od sljedećih: -F, -Cl, -Br, -I, fenil, -CF3, -OH, -ORS, -OCF3, -NH2, -NHRS, -NRS2, pirolidino, piperidino, morfolino, piperizino, N-(C1-4alkil)-piperizino, -NHC(=O)RS, -NRSC(=O)RS, -C(=O)RS, -C(=O)OH, -C(=O)ORS, -C(=O)NH2, -C(=O)NHRS, -C(=O)NRS2, -C(=O)-pirolidino, -C(=O)-piperidino, -C(=O)-morfolino, -C(=O)-piperizino, -C(=O)-{N-(C1-4alkil)-piperizino}-, -SRS, -S(=O)RS, i -S(=O)2RS; gdje je svaki -RS neovisno zasićeni alifatski C1-6alkil, fenil, ili -CH2-fenil; pri čemu je svaki fenil po želji supstituiran s jednom ili više skupina odabranih od sljedećih: -F, -Cl, -Br, -I, -RSS, -CF3, -OH, -ORSS, ili -OCF3, gdje je svaki -RSS zasićeni alifatski C1-4alkil; i gdje je svaki -RX2 neovisno odabran od sljedećih: -F, -Cl, -Br, -I, -RT, fenil, -OH, -ORT, -C(=O)RT, -NH2, -NHRT, -NRT2, pirolidino, piperidino, morfolino, piperizino, N-(C1-4alkil)-piperizino, -NHC(=O)RT, i -NRTC(=O)RT; dok je svaki -RT neovisno zasićeni alifatski C1-6alkil, fenil, ili -CH2-fenil; pri čemu je svaki fenil po želji supstituiran s jednom ili više skupina odabranih od sljedećih: -F, -Cl, -Br, -I, -RTT, -CF3, -OH, -ORTT, ili -OCF3, gdje je svaki -RTT zasićeni alifatski C1-4alkil; te gdje je svaki -RX3 neovisno odabran od sljedećih: -F, -Cl, -Br, -I, -RV, -CH=CH2, -C=CH, ciklopropil, -CF3, -CHF2, -OCF3, -OCHF2, -CN, -NO2, -OH, -ORV, -LV-OH, -LV-ORV, -O-LV-OH, -O-LV-ORV, -NH2, -NHRV, -NRV2, pirolidino, piperidino, morfolino, piperizino, N-(C1-4alkil)-piperizino, LV-NH2, -LV-NHRV, -LV-NRV, -LV-pirolidino, -LV-piperidino, -LV-morfolino, -LV-piperizino, -LV-{N-(C1-4alkil)-piperizino}, -LV-imidazol-2-il, -LV-{N-(C1-4alkil)-imidazol-2-il}, -O-LV-NH2, -O-LV-NHRV, -O-LV-NRV2, -O-LV-pirolidino, -O-LV-piperidino, -O-LV-morfolino, -O-LV-piperizino, -O-LV-{N-(C1-4alkil)-piperizino}, -O-LV-imidazol-2-il, -O-LV-{N-(C1-4alkil)-imidazol-2-il}, -NHC(=O)RV, -NRVC(=O)RV, -C(=O)RV, -C(=O)OH, -C(=O)ORV, -C(=O)NH2, -C(=O)NHRV, -C(=O)NRV2, -C(=O)-pirolidino, -C(=O)-piperidino, -C(=O)-morfolino, -C(=O)-piperizino, -C(=O)-{N-(C1-4alkil)-piperizino}-, -NHC(=O)NH2, -NHC(=O)NHRV, -NHC(=O)NRV2, -NHC(=O)-pirolidino, -NHC(=O)-piperidino, -NHC(=O)-morfolino, -NHC(=O)-piperizino, -NHC(=O)-{N-(C1-4alkil)-piperizino}-, -S(=O)2RV, -S(=O)2NH2, -S(=O)2NHRV, -S(=O)2NRV2, i =O; pri čemu je svaki -LV- zasićeni alifatski C1-4alkilen; gdje je svaki -RV neovisno zasićeni alifatski C1-6alkil, fenil, -CH2-fenil, C5-6heteroaril, ili -CH2-C5-6heteroaril; dok je svaki fenil po želji supstituiran s jednom ili više skupina odabranih od sljedećih: -F, -Cl, -Br, -I, -RVV, -CF3, -OH, -ORVV, ili -OCF3; pri čemu je svaki C5-6heteroaril po želji supstituiran s jednom ili više skupina odabranih od sljedećih: -F, -Cl, -Br, -I, -RVV, -CF3, -OH, -ORVV, ili -OCF3; dok je svaki -RVV zasićeni alifatski C1-4alkil; i dodatno, dvije susjedne skupine -RX3 mogu zajedno tvoriti: -OCH2O-, -OCH2CH2O-, -CH2OCH2-, ili -OCH2CH2-; te dodatno, dvije susjedne skupine -RX3 zajedno s atomima prstena, na koje su priključeni, mogu tvoriti C5-7karbociklički prsten ili C5-7heterociklički prsten.
2. Spoj prema zahtjevu 1, naznačen time, da -R1 je -R1A, gdje -R1A je -iPr.
3. Spoj prema zahtjevu 1 ili 2, naznačen time, da -R3 je -H, i -R6 je -H.
4. Spoj prema bilo kojem od zahtjeva 1 do 3, naznačen time, da -R7 je -R7A, i -R7A je -tBu.
5. Spoj prema bilo kojem od zahtjeva 1 do 3, naznačen time, da -R7 je -R7B; -R7B je -L7B1-R7BB; -L7B1- je -CH2-; -R7BB je -R7BB1; i -R7BB1 je fenil.
6. Spoj prema bilo kojem od zahtjeva 1 do 5, naznačen time, da -R9 je -H; -R10 je -R10A; i -R10A je fenil, te je po želji supstituiran s jednim ili više supstituenata -RX3.
7. Spoj prema bilo kojem od zahtjeva 1 do 5, naznačen time, da -R9 je -H; -R10 je -R10B; i -R10B je piridil, te je po želji supstituiran s jednim ili više supstituenata -RX3.
8. Spoj prema bilo kojem od zahtjeva 1 do 5, naznačen time, da -R9 je -H; -R10 je -R10B; a -R10B je neovisno indazolil, benzimidazolil, benzotiazolil, kinolinil, ili izokinolinil, te je po želji supstituiran s jednim ili više supstituenata -RX3.
9. Spoj prema bilo kojem od zahtjeva 1 do 5, naznačen time, da -R9 je -H; -R10 je -R10D; i -R10D je neovisno sljedeće: [image] [image]
10. Spoj prema bilo kojem od zahtjeva 1 do 5, naznačen time, da skupina -N(R9)-C(=O)-R10 je sljedeća skupina: [image]
11. Spoj prema bilo kojem od zahtjeva 1 do 10, naznačen time, da: -R11 je -R11A; -R11A je -LZ-RZ4; -LZ- je -CH2- ili -CH(Me)-; i -RZ4 je neovisno odabrana od sljedećih: [image] i -R12 je -H.
12. Spoj prema bilo kojem od zahtjeva 1 do 10, naznačen time, da: -R11 je -R11B; -RJ1 je neovisno -H, -Me, -Et, -nPr, ili -iPr; -RJ2 je -H; -NRJ3RJ4 je neovisno odabrana od sljedećih: [image] [image] [image] 1,2,3,4-tetrahidro-izokinolin-2-il, i 2,3-dihidro-1H-indol-1-il; i -R12 je -H.
13. Spoj prema bilo kojem od zahtjeva 1 do 12, naznačen time, da je svaki -RX1, ako je prisutan, neovisno odabran od sljedećih: -F, -Cl, -Br, -I, -OH, -ORS, -NH2, -NHRS, -NRS2, pirolidino, piperidino, morfolino, piperizino, N-(C1-4alkil)-piperizino, -NHC(=O)RS, -NRSC(=O)RS, -C(=O)NH2, -C(=O)NHRS, -C(=O)NRS2, -C(=O)-pirolidino, -C(=O)-piperidino, -C(=O)-morfolino, -C(=O)-piperizino, i -C(=O)-{N-(C1-4alkil)-piperizino}-; te je svaki -RX2, ako je prisutan, neovisno odabran od sljedećih: -RT, -OH, -ORT, -C(=O)RT, -NH2, -NHRT, -NRT2, pirolidino, piperidino, morfolino, piperizino, N-(C1-4alkil)-piperizino, -NHC(=O)RT, i -NRTC(=O)RT.
14. Spoj prema bilo kojem od zahtjeva 1 do 13, naznačen time, da je svaki -RX3, ako je prisutan, neovisno odabran od sljedećih: -F, -Cl, -Br, -I, -RV, -CN, -OH, -ORV, -NH2, -NHRV, -NRV2, pirolidino, piperidino, morfolino, piperizino, N-(C1-4alkil)-piperizino, -LV-NH2, -LV-NHRV, -LV-NRV2, -LV-pirolidino, -LV-piperidino, -LV-morfolino, -LV-piperizino, -LV-{N-(C1-4alkil)-piperizino}-, -C(=O)OH, -C(=O)ORV, -C(=O)NH2, -C(=O)NHRV, -C(=O)NRV2, -NHC(=O)NH2, -S(=O)2NH2, -S(=O)2NHRV, -S(=O)2NRV2, i =O.
15. Spoj prema bilo kojem od zahtjeva 1 do 13, naznačen time, da je svaki -RX3, ako je prisutan, neovisno odabran od sljedećih: -F, -Cl, -Br, -I, -RV, -OH, -ORV, -NH2, -NHRV, -NRV2, pirolidino, piperidino, morfolino, piperizino, N-(C1-4alkil)-piperizino.
16. Spoj prema zahtjevu 1, naznačen time, da je odabran od sljedećih spojeva i njihovih farmaceutski prihvatljivih soli, hidrata i solvata: PVA-001 do PVA-005, PVA-008 do PVA-013, PVA-015 do PVA-017, PVA-019 do PVA-086, PVA-089, PVA-092 do PVA-099, PVA-102 do PVA-122, PVA-124 do PVA-138, PVA-141-PVA-144, i PVA-146-PVA-216.
17. Sastav, naznačen time, da obuhvaća spoj prema bilo kojem od zahtjeva 1 do 16, te farmaceutski prihvatljiv nosač, razrjeđivač ili pomoćno sredstvo.
18. Postupak priprave sastava, naznačen time, da obuhvaća sastavljanje miješanjem spoja prema bilo kojem od zahtjeva 1 do 16 i farmaceutski prihvatljivog nosača, razrjeđivača ili pomoćnog sredstva.
19. Spoj prema bilo kojem od zahtjeva 1 do 16, naznačen time, da se upotrebljava u postupku liječenja ljudskog ili životinjskog tijela pomoću terapije.
20. Spoj prema bilo kojem od zahtjeva 1 do 16, naznačen time, da se upotrebljava u postupku liječenja sljedećih stanja: astma, primjerice atopijska astma; alergijska astma; atopijska bronhijalna IgE-posredovana astma; bronhijalna astma; ekstrinzična astma; astma izazvana alergenom; alergijska astma pogoršana putem respiratorne virusne infekcije; infekcijska astma; infekcijska astma uzrokovana bakterijskom infekcijom; infekcijska astma uzrokovana gljivičnom infekcijom; infekcijska astma uzrokovana protozoalnom infekcijom; ili infekcijska astma uzrokovana virusnom infekcijom; bronhijalna hiper-reaktivnost povezana s astmom; ili prekomjerni bronhijalni odgovor povezan s astmom; preoblikovanje dišnih puteva povezano s alergijskom bolesti grla, primjerice preoblikovanje dišnih puteva povezano s astmom; astma koja se pojavljuje zajedno s kroničnom opstrukcijskom plućnom bolesti, primjerice astma koja se pojavljuje s emfizemom; ili astma koja se pojavljuje s kroničnim bronhitisom; rinitis, primjerice alergijski rinitis; perenijalni rinitis; uporni rinitis; ili IgE-posredovani rinitis; alergijski konjunktivitis, primjerice IgE-posredovani konjunktivitis; atopijski dermatitis; alergijsko stanje koje iniciraju grinje; alergijsko stanje koje iniciraju alergeni peptidaze grinja skupine 1; ili pseća atopija.
21. Spoj prema zahtjevu 20, naznačen time, da liječenje nadalje obuhvaća liječenje s jednim ili više dodatnih terapeutskih sredstava u liječenju respiratornih bolesti, koja su odabrana od već korištenih sredstava ili od sredstava koja se tek namjeravaju koristiti.
22. Uporaba spoja prema bilo kojem od zahtjeva 1 do 16, naznačena time, da služi u proizvodnji lijeka za liječenje sljedećih stanja: astma, primjerice atopijska astma; alergijska astma; atopijska bronhijalna IgE-posredovana astma; bronhijalna astma; ekstrinzična astma; astma izazvana alergenom; alergijska astma pogoršana putem respiratorne virusne infekcije; infekcijska astma; infekcijska astma uzrokovana bakterijskom infekcijom; infekcijska astma uzrokovana gljivičnom infekcijom; infekcijska astma uzrokovana protozoalnom infekcijom; ili infekcijska astma uzrokovana virusnom infekcijom; bronhijalna hiper-reaktivnost povezana s astmom; ili prekomjerni bronhijalni odgovor povezan s astmom; preoblikovanje dišnih puteva povezano s alergijskom bolesti grla, primjerice preoblikovanje dišnih puteva povezano s astmom; astma koja se pojavljuje zajedno s kroničnom opstrukcijskom plućnom bolesti, primjerice astma koja se pojavljuje s emfizemom; ili astma koja se pojavljuje s kroničnim bronhitisom; rinitis, primjerice alergijski rinitis; perenijalni rinitis; uporni rinitis; ili IgE-posredovani rinitis; alergijski konjunktivitis, primjerice IgE-posredovani konjunktivitis; atopijski dermatitis; alergijsko stanje koje iniciraju grinje; alergijsko stanje koje iniciraju alergeni peptidaze grinja skupine 1; ili pseća atopija.
23. Uporaba prema zahtjevu 22, naznačena time, da liječenje nadalje obuhvaća liječenje s jednim ili više dodatnih terapeutskih sredstava u liječenju respiratornih bolesti, koja su odabrana od već korištenih sredstava ili od sredstava koja se tek namjeravaju koristiti.
24. Postupak inhibiranja alergena peptidaze grinja skupine 1, naznačen time, da obuhvaća, in vitro, dovođenje u doticaj navedenog alergena peptidaze grinja skupine 1 s učinkovitom količinom spoja prema bilo kojem od zahtjeva 1 do 16.
25. Postupak inhibiranja alergena peptidaze grinja skupine 1 u stanici, naznačen time, da obuhvaća, in vitro, dovođenje u doticaj stanice s učinkovitom količinom spoja prema bilo kojem od zahtjeva 1 do 16.
26. Spoj prema bilo kojem od zahtjeva 1 do 16, naznačen time, da se upotrebljava kao akaricid.
27. Sastav koji obuhvaća spoj prema bilo kojem od zahtjeva 1 do 16, naznačen time, da se upotrebljava kao akaricid.
28. Akaricidni sastav, naznačen time, da obuhvaća spoj prema bilo kojem od zahtjeva 1 do 16.
29. Uporaba spoja prema bilo kojem od zahtjeva 1 do 16, naznačena time, da služi kao akaricid.
30. Postupak uništavanja grinja, naznačen time, da obuhvaća izlaganje navedenih grinja učinkovitoj količini spoja prema bilo kojem od zahtjeva 1 do 16.
31. Postupak suzbijanja populacije grinja, naznačen time, da obuhvaća izlaganje grinja učinkovitoj količini spoja prema bilo kojem od zahtjeva 1 do 16.
HRP20150844TT 2010-01-22 2015-08-07 Spojevi piruvamida kao inhibitori alergena peptidaze od kuä†nih grinja skupine 1 HRP20150844T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1001070.0A GB201001070D0 (en) 2010-01-22 2010-01-22 Theraputic compounds and their use
PCT/GB2011/000079 WO2011089396A2 (en) 2010-01-22 2011-01-21 Pyruvamide compounds as inhibitors of dust mite group 1 peptidase allergen and their use.
EP20110701854 EP2526116B1 (en) 2010-01-22 2011-01-21 Pyruvamide compounds as inhibitors of dust mite group 1 peptidase allergen

Publications (1)

Publication Number Publication Date
HRP20150844T1 true HRP20150844T1 (hr) 2015-11-06

Family

ID=42045942

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20150844TT HRP20150844T1 (hr) 2010-01-22 2015-08-07 Spojevi piruvamida kao inhibitori alergena peptidaze od kuä†nih grinja skupine 1

Country Status (28)

Country Link
US (2) US8541363B2 (hr)
EP (1) EP2526116B1 (hr)
JP (1) JP5859980B2 (hr)
KR (1) KR101798676B1 (hr)
CN (1) CN102822192B (hr)
AU (1) AU2011208510B2 (hr)
BR (1) BR112012017476B8 (hr)
CA (1) CA2786690C (hr)
CY (1) CY1116824T1 (hr)
DK (1) DK2526116T3 (hr)
ES (1) ES2544732T3 (hr)
GB (1) GB201001070D0 (hr)
HK (1) HK1173735A1 (hr)
HR (1) HRP20150844T1 (hr)
HU (1) HUE025340T2 (hr)
IL (1) IL220665A (hr)
ME (1) ME02218B (hr)
MX (1) MX2012007711A (hr)
NZ (1) NZ601155A (hr)
PL (1) PL2526116T3 (hr)
PT (1) PT2526116E (hr)
RS (1) RS54148B1 (hr)
RU (1) RU2586215C2 (hr)
SG (1) SG182535A1 (hr)
SI (1) SI2526116T1 (hr)
SM (1) SMT201500215B (hr)
WO (1) WO2011089396A2 (hr)
ZA (1) ZA201204764B (hr)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201001070D0 (en) 2010-01-22 2010-03-10 St George's Hospital Medical School Theraputic compounds and their use
KR20150065885A (ko) * 2012-10-11 2015-06-15 에프. 호프만-라 로슈 아게 케토아마이드 이뮤노프로테아좀 억제제
CN103724334A (zh) * 2013-10-02 2014-04-16 张惠琳 新的抗变态反应的苯并环庚并噻吩类化合物
WO2015106242A2 (en) * 2014-01-13 2015-07-16 The General Hospital Corporation Bisamide compounds as allosteric effectors for reducing the oxygen-binding affinity of hemoglobin
EP3626707A1 (en) 2014-01-13 2020-03-25 The General Hospital Corporation Heteroaryl disulfide compounds as allosteric effectors for increasing the oxygen-binding affinity of hemoglobin
GB201908511D0 (en) 2019-06-13 2019-07-31 Adorx Therapeutics Ltd Hydroxamate compounds
WO2022133069A1 (en) * 2020-12-17 2022-06-23 Disc Medicine, Inc. Peptidomimetic matriptase 2 inhibitors and uses thereof
WO2023165334A1 (zh) * 2022-03-01 2023-09-07 成都威斯克生物医药有限公司 酮酰胺类衍生物及其制药用途
WO2024028417A1 (en) 2022-08-03 2024-02-08 Institut National de la Santé et de la Recherche Médicale New composition for the treatment and/or prevention of vitiligo

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3149159A (en) 1962-04-16 1964-09-15 Smith Kline French Lab Substituted 7-aminoalkylbicyclo-[4. 2. 0] octa-1, 3, 5-trienes
EP0100673A2 (en) 1982-08-02 1984-02-15 The Research Foundation Of State University Of New York A method of enhancing neurofiber regrowth
US5066785A (en) * 1988-11-15 1991-11-19 City Of Hope Carboxyl terminal peptide and protein sequencing
WO1990012805A1 (en) 1989-04-15 1990-11-01 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Postostatin and related compound thereof, or their salts
US6235929B1 (en) 1991-12-27 2001-05-22 Georgia Tech Research Corporation Tripeptide α-ketoamides
DE4331135A1 (de) 1993-09-14 1995-03-16 Bayer Ag Neue antiviral wirksame valinhaltige Pseudopeptide
US5580854A (en) 1994-03-04 1996-12-03 Mount Sinai School Of Medicine Of The City University Of New York Substrate-related peptidyl-aldehyde inhibitors of the proteolytic activity of the multicatalytic proteinase complex
AU3935895A (en) 1994-11-24 1996-06-17 Takeda Chemical Industries Ltd. Alpha-ketoamide derivatives as cathepsin l inhibitor
JPH08208462A (ja) * 1994-11-24 1996-08-13 Takeda Chem Ind Ltd カテプシンｌ阻害剤
WO1996030395A2 (en) 1995-03-31 1996-10-03 Takeda Chemical Industries, Ltd. Cysteine protease inhibitor
DE69633623T2 (de) 1995-07-17 2005-12-01 Medivir Uk Ltd. Cystein-Protease-Inhibitoren für die Behandlung von allergischen Krankheiten verursacht duch IgE
EP0873519A4 (en) 1995-12-07 2005-04-27 Scripps Research Inst HIV PROTEASE INHIBITORS
WO1997030075A1 (de) 1996-02-16 1997-08-21 Bayer Aktiengesellschaft Antiviral wirksame oxim- und nitronsubstituierte pseudopeptide
CA2225325A1 (en) 1997-12-19 1999-06-19 The University Of British Columbia Hemiasterlin analogs
NZ528282A (en) 1998-03-19 2005-05-27 Vertex Pharma Interleukin-1 beta converting enzyme inhibitors
US7521068B2 (en) 1998-11-12 2009-04-21 Elan Pharma International Ltd. Dry powder aerosols of nanoparticulate drugs
JP2003526634A (ja) 1999-12-03 2003-09-09 ブリストル−マイヤーズ スクイブ ファーマ カンパニー Ｃ型肝炎ウイルスＮＳ３プロテアーゼのα−ケトアミド阻害剤
JP2002030053A (ja) * 2000-07-13 2002-01-29 Senju Pharmaceut Co Ltd α−ケトアミド誘導体の製造法
MXPA03000626A (es) 2000-07-21 2004-07-30 Schering Corp Nuevos peptidos como inhibidores de ns3-serina proteasa del virus de la hepatitis c.
EP1553964A4 (en) * 2002-09-25 2009-08-12 Georgia Tech Res Inst INHIBITORS OF CETOAMIDES IN CHRONIC NERVOUS DISEASES
JP3858080B2 (ja) 2003-11-12 2006-12-13 株式会社信州Ｔｌｏ アレルゲン分解剤、および抗アレルゲン羽毛
JP2009503027A (ja) 2005-08-03 2009-01-29 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング アルツハイマー病ｉｉの治療のための置換エタン−１，２−ジアミン
WO2007041775A1 (en) 2005-10-10 2007-04-19 The University Of Queensland Cysteine protease inhibitors incorporating azide groups
GB201001070D0 (en) 2010-01-22 2010-03-10 St George's Hospital Medical School Theraputic compounds and their use
GB201011411D0 (en) 2010-07-06 2010-08-18 St Georges Hosp Medical School Therapeutic compounds and their use

Also Published As

Publication number Publication date
ME02218B (me) 2016-02-20
WO2011089396A3 (en) 2012-04-26
JP2013518040A (ja) 2013-05-20
US8541363B2 (en) 2013-09-24
AU2011208510A1 (en) 2012-07-19
US20130217617A1 (en) 2013-08-22
RS54148B1 (en) 2015-12-31
IL220665A (en) 2016-05-31
PL2526116T3 (pl) 2015-10-30
SG182535A1 (en) 2012-08-30
JP5859980B2 (ja) 2016-02-16
RU2012127709A (ru) 2014-02-27
ES2544732T3 (es) 2015-09-03
PT2526116E (pt) 2015-09-17
HUE025340T2 (en) 2016-02-29
RU2586215C2 (ru) 2016-06-10
KR101798676B1 (ko) 2017-11-16
CA2786690C (en) 2019-05-07
US8637453B2 (en) 2014-01-28
BR112012017476A2 (pt) 2016-04-19
AU2011208510B2 (en) 2015-11-12
US20120322722A1 (en) 2012-12-20
KR20120120306A (ko) 2012-11-01
SI2526116T1 (sl) 2015-09-30
HK1173735A1 (en) 2013-05-24
DK2526116T3 (en) 2015-08-10
BR112012017476B1 (pt) 2021-03-16
CN102822192B (zh) 2015-09-30
NZ601155A (en) 2013-08-30
CN102822192A (zh) 2012-12-12
EP2526116A2 (en) 2012-11-28
CY1116824T1 (el) 2017-03-15
MX2012007711A (es) 2013-01-29
EP2526116B1 (en) 2015-05-13
SMT201500215B (it) 2015-10-30
GB201001070D0 (en) 2010-03-10
IL220665A0 (en) 2012-08-30
ZA201204764B (en) 2013-09-25
BR112012017476B8 (pt) 2021-05-25
WO2011089396A2 (en) 2011-07-28
CA2786690A1 (en) 2011-07-28

Similar Documents

Publication Publication Date Title
HRP20150844T1 (hr) Spojevi piruvamida kao inhibitori alergena peptidaze od kuä†nih grinja skupine 1
JP2013518040A5 (hr)
IL257880A (en) Inhibitors in the cell-lactamase
AR054127A1 (es) Imidazoquinolinas como inhibidores de quinasa de lipido
JP2008509187A5 (hr)
JP2005509024A5 (hr)
AR041566A1 (es) Derivados de indol utiles para el tratamiento de enfermedades
AR035069A1 (es) Compuestos inhibidores de espiropirimidin-2,4,6-triona metaloproteinasas, composicion farmaceutica, procedimiento de tratamiento
AR073348A1 (es) Inhibidores ciclicos de 11 beta-hidroxiesteroide deshidrogenasa 1
AR067575A1 (es) Agentes citotoxicos que comprenden nuevos derivados de tomaimicina y su uso terapeutico
EA200500846A1 (ru) Замещенные арилтиомочевины и родственные соединения; ингибиторы вирусной репликации
CA2758474A1 (en) Novel p2x7r antagonists and their use
RU2006112428A (ru) Производные 2-пиридона в качестве ингибиторов эластазы нейтрофилов и их применение
JP2009537576A (ja) 新規なベンゾチアジノン誘導体、及び抗菌剤としてのその使用
AR038881A1 (es) Compuestos que modulan la actividad de ppar, composicion farmaceutica que los contiene y un procedimiento para la preparcion de aquellos
KR20140129360A (ko) 글루타메이트에 의한 시냅스 반응을 향상시키기 위한 이치환된 아미드 화합물
AR052938A1 (es) Compuestos de n-sulfonilaminofeniletil-2-fenoxiacetamida sustituidos, composiciones farmaceuticas que los comprenden y su uso en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por el receptor vr1
RU2007122485A (ru) Ингибиторы киназы
JP2010513434A5 (hr)
EP0722942A1 (de) Indolpiperidin-Derivate
RU2012131341A (ru) Индол-пиперидинилбензиламины как ингибиторы бета-триптазы
JP2010527984A5 (hr)
JP2016508145A5 (hr)
JP2008540443A (ja) イオンチャネルのモジュレーターとして有用なピリミジンおよびピラジン
RU2014120421A (ru) Производные гетероарилгидроксамовой кислоты и их применение при лечении, облегчении течения или профилактике вирусных заболеваний