WO2015169884A3 - Compounds and methods for the treatment of itch - Google Patents

Compounds and methods for the treatment of itch Download PDF

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Publication number
WO2015169884A3
WO2015169884A3 PCT/EP2015/060019 EP2015060019W WO2015169884A3 WO 2015169884 A3 WO2015169884 A3 WO 2015169884A3 EP 2015060019 W EP2015060019 W EP 2015060019W WO 2015169884 A3 WO2015169884 A3 WO 2015169884A3
Authority
WO
WIPO (PCT)
Prior art keywords
itch
treatment
etar
endothelin
compounds
Prior art date
Application number
PCT/EP2015/060019
Other languages
French (fr)
Other versions
WO2015169884A2 (en
Inventor
Joerg BUDDENKOTTE
Martin Steinhoff
Original Assignee
Westfaelische Wilhelms-Universitaet Muenster
The Regents Of The University Of California
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 Westfaelische Wilhelms-Universitaet Muenster, The Regents Of The University Of California filed Critical Westfaelische Wilhelms-Universitaet Muenster
Priority to EP15723667.0A priority Critical patent/EP3169365A2/en
Publication of WO2015169884A2 publication Critical patent/WO2015169884A2/en
Publication of WO2015169884A3 publication Critical patent/WO2015169884A3/en

Links

Classifications

    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/43—Enzymes; Proenzymes; Derivatives thereof
    • A61K38/46—Hydrolases (3)
    • A61K38/48—Hydrolases (3) acting on peptide bonds (3.4)
    • A61K38/4886—Metalloendopeptidases (3.4.24), e.g. collagenase
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
    • C12Y304/24—Metalloendopeptidases (3.4.24)
    • C12Y304/24071—Endothelin-converting enzyme 1 (3.4.24.71)

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biochemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Dermatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Chemical & Material Sciences (AREA)
  • General Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

The present application provides a compound for use in the treatment of a subject suffering from itch, wherein said compound is endothelin-converting enzyme (ECE-1), a MEK1 inhibitor, or an ETAR inhibitor. Similarly, these compounds can be used in a topic pharmaceutical composition and for the preparation of a medicament. Also, the present invention provides a method for the screening of a compound useful for the treatment of histamine-independent, endothelin-1 (ET-1)/endothelin A receptor (ETAR) induced itch and a method for diagnosing a subject suffering from a histamine-independent, ET-1/ETAR induced itch.
PCT/EP2015/060019 2014-05-07 2015-05-07 Compounds and methods for the treatment of itch WO2015169884A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP15723667.0A EP3169365A2 (en) 2014-05-07 2015-05-07 Compounds and methods for the treatment of itch

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201461989797P 2014-05-07 2014-05-07
US61/989,797 2014-05-07

Publications (2)

Publication Number Publication Date
WO2015169884A2 WO2015169884A2 (en) 2015-11-12
WO2015169884A3 true WO2015169884A3 (en) 2016-01-28

Family

ID=53191649

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2015/060019 WO2015169884A2 (en) 2014-05-07 2015-05-07 Compounds and methods for the treatment of itch

Country Status (2)

Country Link
EP (1) EP3169365A2 (en)
WO (1) WO2015169884A2 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8906951B1 (en) 2013-06-24 2014-12-09 Tigercat Pharma, Inc. Use of NK-1 receptor antagonists in pruritus
US9198898B2 (en) 2013-06-24 2015-12-01 Tigercat Pharma, Inc. Use of NK-1 receptor antagonists in pruritus
WO2019173215A1 (en) * 2018-03-07 2019-09-12 Timber Pharmaceuticals Llc Compositions and methods for treating cutaneous fibrosis
US20210169848A1 (en) * 2018-07-27 2021-06-10 Vyne Therapeutics Inc. Use of neurokinin-1 antagonists to treat pruritus

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4376110A (en) 1980-08-04 1983-03-08 Hybritech, Incorporated Immunometric assays using monoclonal antibodies

Non-Patent Citations (7)

* Cited by examiner, † Cited by third party
Title
D ROOSTERMAN ET AL: "Molecular regulation of neuropeptide receptors by peptidase endothelin-converting enzyme-1: Impact on inflammation and pruritus", JOURNAL OF INVESTIGATIVE DERMATOLOGY, vol. 130, no. Suppl 1, April 2010 (2010-04-01), pages S98, XP055204471, ISSN: 0022-202X *
D S MCQUEEN ET AL: "Endothelin-1 activates ETA receptors to cause reflex scratching in BALB/c mice", BRITISH JOURNAL OF PHARMACOLOGY, vol. 151, no. 2, 12 March 2007 (2007-03-12), BASINGSTOKE, HANTS; GB, pages 278 - 284, XP055204436, ISSN: 0007-1188, DOI: 10.1038/sj.bjp.0707216 *
DIANA M BAUTISTA ET AL: "Why we scratch an itch: the molecules, cells and circuits of itch", NATURE NEUROSCIENCE, vol. 17, no. 2, 28 January 2014 (2014-01-28), pages 175 - 182, XP055204472, ISSN: 1097-6256, DOI: 10.1038/nn.3619 *
M KIDO ET AL: "Endothelin-converting enzyme-1 modulates endothelin-1-induced pruritus by inhibiting endothelin receptor recycling and prolonging ERK1/2 signaling in murine sensory neurons", JOURNAL OF INVESTIGATIVE DERMATOLOGY, vol. 131, no. Suppl 1, April 2011 (2011-04-01), pages S44, XP055204470, ISSN: 0022-202X *
MAKIKO KIDO-NAKAHARA ET AL: "Neural peptidase endothelin-converting enzyme 1 regulates endothelin 1-induced pruritus", JOURNAL OF CLINICAL INVESTIGATION, vol. 124, no. 6, 8 May 2014 (2014-05-08), pages 2683 - 2695, XP055203387, ISSN: 0021-9738, DOI: 10.1172/JCI67323 *
TEJESH PATEL ET AL: "Therapy of pruritus", EXPERT OPINION ON PHARMACOTHERAPY, vol. 11, no. 10, July 2010 (2010-07-01), pages 1673 - 1682, XP055203603, ISSN: 1465-6566, DOI: 10.1517/14656566.2010.484420 *
TRENTIN PATRICIA GONCALVES ET AL: "Endothelin-1 causes pruritus in mice", EXPERIMENTAL BIOLOGY AND MEDICINE (MAYWOOD), vol. 231, no. 6, June 2006 (2006-06-01), pages 1146 - 1151, XP009185544, ISSN: 1535-3702 *

Also Published As

Publication number Publication date
WO2015169884A2 (en) 2015-11-12
EP3169365A2 (en) 2017-05-24

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