WO2002026774A3 - Melanocortin receptor ligands - Google Patents

Melanocortin receptor ligands Download PDF

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Publication number
WO2002026774A3
WO2002026774A3 PCT/US2001/030051 US0130051W WO0226774A3 WO 2002026774 A3 WO2002026774 A3 WO 2002026774A3 US 0130051 W US0130051 W US 0130051W WO 0226774 A3 WO0226774 A3 WO 0226774A3
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WO
WIPO (PCT)
Prior art keywords
ligands
receptor ligands
melanocortin receptor
formula
disclosed
Prior art date
Application number
PCT/US2001/030051
Other languages
French (fr)
Other versions
WO2002026774A2 (en
Inventor
Frank Hallock Ebetino
Adam W Mazur
Jeffrey Charles Hayes
Feng Wang
Mark Gregory Solinsky
Anny-Odile Colson
Qishen Lin
Original Assignee
Procter & Gamble
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
Priority to JP2002531157A priority Critical patent/JP2004509974A/en
Priority to EP01977175A priority patent/EP1409540A2/en
Priority to NZ524190A priority patent/NZ524190A/en
Priority to PL36200301A priority patent/PL362003A1/en
Application filed by Procter & Gamble filed Critical Procter & Gamble
Priority to HU0303085A priority patent/HUP0303085A2/en
Priority to AU9631301A priority patent/AU9631301A/en
Priority to KR10-2003-7004415A priority patent/KR100519204B1/en
Priority to MXPA03002691A priority patent/MXPA03002691A/en
Priority to AU2001296313A priority patent/AU2001296313B2/en
Priority to IL15443701A priority patent/IL154437A0/en
Priority to BR0114257-7A priority patent/BR0114257A/en
Priority to CA002420045A priority patent/CA2420045A1/en
Publication of WO2002026774A2 publication Critical patent/WO2002026774A2/en
Priority to NO20031287A priority patent/NO20031287D0/en
Publication of WO2002026774A3 publication Critical patent/WO2002026774A3/en

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    • 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
    • C07K5/10Tetrapeptides
    • C07K5/1027Tetrapeptides 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/04Drugs for disorders of the respiratory system for throat disorders
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P3/06Antihyperlipidemics
    • 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
    • A61P35/00Antineoplastic 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
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • 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
    • C07K5/0207Peptides 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)4-C(=0), e.g. 'isosters', replacing two amino acids
    • 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
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
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    • C07ORGANIC CHEMISTRY
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    • C07K5/06095Arg-amino acid
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    • C07K5/0827Tripeptides containing heteroatoms different from O, S, or N
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    • C07ORGANIC CHEMISTRY
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    • 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
    • C07K5/10Tetrapeptides
    • C07K5/1002Tetrapeptides with the first amino acid being neutral
    • C07K5/1005Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/1008Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
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    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides
    • C07K5/1002Tetrapeptides with the first amino acid being neutral
    • C07K5/1016Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
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    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides
    • C07K5/1024Tetrapeptides with the first amino acid being heterocyclic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
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  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
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Abstract

Disclosed are MC-4 and/or MC-3 receptor ligands, the ligands having a structure according to Formula (I): wherein R?2, R4, R4', R5, R6, R6', R7, R8, R8', R9, R9', R10, Ar, Z1, Z2, Z3¿, X, B, D, p, q, r and s are as described in the specification and claims, and optical isomers, diastereomers or enantiomers thereof; pharmaceutically-acceptable salts, hydrates, and biohydrolyzable esters, amides or imides thereof. Also disclosed are pharmaceutical compositions comprising the ligands of Formula (I), as well as methods of treating diseases mediate by the MC-4/MC-3 receptors, as described in the Detailed Descriptions section of the specification.
PCT/US2001/030051 2000-09-27 2001-09-26 Melanocortin receptor ligands WO2002026774A2 (en)

Priority Applications (13)

Application Number Priority Date Filing Date Title
AU9631301A AU9631301A (en) 2000-09-27 2001-09-26 Melanocortin receptor ligands
NZ524190A NZ524190A (en) 2000-09-27 2001-09-26 Melanocortin receptor ligands
PL36200301A PL362003A1 (en) 2000-09-27 2001-09-26 Melanocortin receptor ligands
MXPA03002691A MXPA03002691A (en) 2000-09-27 2001-09-26 Melanocortin receptor ligands.
HU0303085A HUP0303085A2 (en) 2000-09-27 2001-09-26 Melanocortin receptor ligands and pharmaceutical compositions containing them
EP01977175A EP1409540A2 (en) 2000-09-27 2001-09-26 Melanocortin receptor ligands
KR10-2003-7004415A KR100519204B1 (en) 2000-09-27 2001-09-26 Melanocortin receptor ligands
JP2002531157A JP2004509974A (en) 2000-09-27 2001-09-26 Melanocortin receptor ligand
AU2001296313A AU2001296313B2 (en) 2000-09-27 2001-09-26 Melanocortin receptor ligands
IL15443701A IL154437A0 (en) 2000-09-27 2001-09-26 Melanocortin receptor ligands
BR0114257-7A BR0114257A (en) 2000-09-27 2001-09-26 Melanocortin Receptor Ligands
CA002420045A CA2420045A1 (en) 2000-09-27 2001-09-26 Melanocortin receptor ligands
NO20031287A NO20031287D0 (en) 2000-09-27 2003-03-20 Melanokortinreseptorligander

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US23585800P 2000-09-27 2000-09-27
US60/235,858 2000-09-27

Publications (2)

Publication Number Publication Date
WO2002026774A2 WO2002026774A2 (en) 2002-04-04
WO2002026774A3 true WO2002026774A3 (en) 2003-03-27

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ID=22887187

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PCT/US2001/030051 WO2002026774A2 (en) 2000-09-27 2001-09-26 Melanocortin receptor ligands

Country Status (19)

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EP (1) EP1409540A2 (en)
JP (1) JP2004509974A (en)
KR (1) KR100519204B1 (en)
CN (1) CN1571796A (en)
AR (1) AR030806A1 (en)
AU (2) AU9631301A (en)
BR (1) BR0114257A (en)
CA (1) CA2420045A1 (en)
CZ (1) CZ2003788A3 (en)
HU (1) HUP0303085A2 (en)
IL (1) IL154437A0 (en)
MX (1) MXPA03002691A (en)
NO (1) NO20031287D0 (en)
NZ (1) NZ524190A (en)
PE (1) PE20020447A1 (en)
PL (1) PL362003A1 (en)
RU (1) RU2246501C2 (en)
WO (1) WO2002026774A2 (en)
ZA (1) ZA200301561B (en)

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US9174950B2 (en) 2009-07-06 2015-11-03 Aerpio Therapeutics, Inc. Compounds, compositions, and methods for preventing metastasis of cancer cells
US9284285B2 (en) 2006-06-27 2016-03-15 Aerpio Therapeutics, Inc. Human protein tyrosine phosphatase inhibitors and methods of use

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US7176279B2 (en) 2000-06-28 2007-02-13 Palatin Technologies, Inc. Cyclic peptide compositions and methods for treatment of sexual dysfunction
US7507568B2 (en) 2002-09-25 2009-03-24 The Proctor & Gamble Company Three dimensional coordinates of HPTPbeta
US7226755B1 (en) 2002-09-25 2007-06-05 The Procter & Gamble Company HPTPbeta as a target in treatment of angiogenesis mediated disorders
ATE550041T1 (en) 2004-01-21 2012-04-15 Novo Nordisk Healthcare Ag TRANSGLUTAMINASE-MEDIATED CONJUGATION OF PEPTIDES
RU2309144C2 (en) * 2005-03-25 2007-10-27 Общество С Ограниченной Ответственностью "Фарминтерпрайсез" Phenyl-containing n-acylamine derivatives, method for production thereof, pharmaceutical composition and uses thereof as anti-inflammatory and analgesic agents
US8247530B2 (en) 2005-11-08 2012-08-21 Palatin Technologies, Inc. N-alkylated cyclic peptide melanocortin agonists
MX2008012991A (en) 2006-04-07 2008-10-17 Procter & Gamble Antibodies that bind human protein tyrosine phosphatase beta (hptpbeta) and uses thereof.
RU2303597C1 (en) * 2006-05-12 2007-07-27 Иващенко Андрей Александрович Pharmaceutical composition, method for its preparing and using
US7795444B2 (en) 2006-06-27 2010-09-14 Warner Chilcott Company Human protein tyrosine phosphatase inhibitors and methods of use
US8846685B2 (en) 2006-06-27 2014-09-30 Aerpio Therapeutics Inc. Human protein tyrosine phosphatase inhibitors and methods of use
US7589212B2 (en) 2006-06-27 2009-09-15 Procter & Gamble Company Human protein tyrosine phosphatase inhibitors and methods of use
WO2008107362A2 (en) * 2007-03-07 2008-09-12 Novo Nordisk Health Care Ag Stabiliser and inhibitors of factor vii
MX2010013436A (en) 2008-06-09 2011-06-21 Palatin Technologies Inc Melanocortin receptor-specific peptides for treatment of sexual dysfunction.
US9096555B2 (en) 2009-01-12 2015-08-04 Aerpio Therapeutics, Inc. Methods for treating vascular leak syndrome
MX2011013117A (en) 2009-06-08 2012-05-23 Palatin Technologies Inc Melanocortin receptor-specific peptides.
WO2010144341A2 (en) 2009-06-08 2010-12-16 Palatin Technologies, Inc. Lactam-bridged melanocortin receptor-specific peptides
UY32690A (en) 2009-06-08 2011-01-31 Astrazeneca Ab SPECIFIC PEPTIDES FOR MELANOCORTIN RECEPTORS
US8883832B2 (en) 2009-07-06 2014-11-11 Aerpio Therapeutics Inc. Compounds, compositions, and methods for preventing metastasis of cancer cells
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EP2504351A4 (en) 2009-11-23 2013-10-30 Palatin Technologies Inc Melanocortin-1 receptor-specific linear peptides
CN102725305B (en) 2009-11-23 2016-08-24 帕拉丁科技公司 Melanocortin-1 receptor-specific cyclic peptide
US10347423B2 (en) 2014-05-12 2019-07-09 Capacitor Sciences Incorporated Solid multilayer structure as semiproduct for meta-capacitor
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US10340082B2 (en) 2015-05-12 2019-07-02 Capacitor Sciences Incorporated Capacitor and method of production thereof
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US9932358B2 (en) * 2015-05-21 2018-04-03 Capacitor Science Incorporated Energy storage molecular material, crystal dielectric layer and capacitor
US9941051B2 (en) 2015-06-26 2018-04-10 Capactor Sciences Incorporated Coiled capacitor
US10026553B2 (en) 2015-10-21 2018-07-17 Capacitor Sciences Incorporated Organic compound, crystal dielectric layer and capacitor
US10305295B2 (en) 2016-02-12 2019-05-28 Capacitor Sciences Incorporated Energy storage cell, capacitive energy storage module, and capacitive energy storage system
US10153087B2 (en) 2016-04-04 2018-12-11 Capacitor Sciences Incorporated Electro-polarizable compound and capacitor
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US10395841B2 (en) 2016-12-02 2019-08-27 Capacitor Sciences Incorporated Multilayered electrode and film energy storage device
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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9284285B2 (en) 2006-06-27 2016-03-15 Aerpio Therapeutics, Inc. Human protein tyrosine phosphatase inhibitors and methods of use
US9174950B2 (en) 2009-07-06 2015-11-03 Aerpio Therapeutics, Inc. Compounds, compositions, and methods for preventing metastasis of cancer cells

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PL362003A1 (en) 2004-10-18
NO20031287L (en) 2003-03-20
IL154437A0 (en) 2003-09-17
AU2001296313B2 (en) 2005-06-02
AU9631301A (en) 2002-04-08
HUP0303085A2 (en) 2003-12-29
ZA200301561B (en) 2004-03-10
BR0114257A (en) 2003-07-01
RU2246501C2 (en) 2005-02-20
NZ524190A (en) 2004-09-24
NO20031287D0 (en) 2003-03-20
CA2420045A1 (en) 2002-04-04
PE20020447A1 (en) 2002-07-02
CZ2003788A3 (en) 2003-08-13
CN1571796A (en) 2005-01-26
KR100519204B1 (en) 2005-10-06
MXPA03002691A (en) 2003-06-06
KR20030061814A (en) 2003-07-22
WO2002026774A2 (en) 2002-04-04
AR030806A1 (en) 2003-09-03
JP2004509974A (en) 2004-04-02
EP1409540A2 (en) 2004-04-21

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