AU2009219106B2 - 3-aminoalkyl-1,4-diazepan-2-one melanocortin-5 receptor antagonists - Google Patents

3-aminoalkyl-1,4-diazepan-2-one melanocortin-5 receptor antagonists Download PDF

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Publication number
AU2009219106B2
AU2009219106B2 AU2009219106A AU2009219106A AU2009219106B2 AU 2009219106 B2 AU2009219106 B2 AU 2009219106B2 AU 2009219106 A AU2009219106 A AU 2009219106A AU 2009219106 A AU2009219106 A AU 2009219106A AU 2009219106 B2 AU2009219106 B2 AU 2009219106B2
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methyl
oxo
diazepan
ethyl
naphthamide
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AU2009219106A
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AU2009219106A1 (en
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Mark Arnold Thomas Blaskovich
Peter Joseph Cassidy
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Marp Therapeutics Pty Ltd
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Marp Therapeutics Pty Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/08—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 not condensed with other rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/494—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity 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
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/008—Preparations for oily skin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/20—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms not being part of nitro or nitroso groups
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
    • C07C2603/18—Fluorenes; Hydrogenated fluorenes

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Virology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Birds (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Psychology (AREA)
  • Transplantation (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Macromolecular Compounds Obtained By Forming Nitrogen-Containing Linkages In General (AREA)
AU2009219106A 2008-02-29 2009-02-27 3-aminoalkyl-1,4-diazepan-2-one melanocortin-5 receptor antagonists Ceased AU2009219106B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US3289408P 2008-02-29 2008-02-29
US61/032,894 2008-02-29
US12/391,720 US8008291B2 (en) 2008-02-29 2009-02-24 3-aminoalkyl-1,4-diazepan-2-one melanocortin-5 receptor antagonists
US12/391,720 2009-02-24
PCT/AU2009/000230 WO2009105823A1 (en) 2008-02-29 2009-02-27 3-aminoalkyl-1,4-diazepan-2-one melanocortin-5 receptor antagonists

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AU2009219106A1 AU2009219106A1 (en) 2009-09-03
AU2009219106B2 true AU2009219106B2 (en) 2013-09-26

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US (1) US8008291B2 (enExample)
EP (1) EP2257534B1 (enExample)
JP (1) JP5503557B2 (enExample)
KR (1) KR101620114B1 (enExample)
CN (1) CN102007105B (enExample)
AU (1) AU2009219106B2 (enExample)
BR (1) BRPI0907903B1 (enExample)
CA (1) CA2716250C (enExample)
DK (1) DK2257534T3 (enExample)
ES (1) ES2445456T3 (enExample)
IL (1) IL207700A (enExample)
MX (1) MX2010009487A (enExample)
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PT (1) PT2257534E (enExample)
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Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2009219107B2 (en) * 2008-02-29 2013-11-21 Marp Therapeutics Pty Ltd Methods of modulating the activity of the MC5 receptor and treatment of conditions related to this receptor
WO2010096853A1 (en) * 2009-02-27 2010-09-02 Mimetica Pty Ltd Methods of modulating the activity of the mc1 receptor and treatment of conditions related to this receptor
CN109956947A (zh) * 2017-12-25 2019-07-02 江苏恒瑞医药股份有限公司 一种cns抑制剂的新晶型、制备方法及用途
CN115381955B (zh) * 2021-05-24 2024-05-17 中国科学技术大学 黑皮质素受体mc5r的用途
KR102703324B1 (ko) * 2022-11-08 2024-09-06 국민대학교산학협력단 아미노벤즈이미다졸 유도체 및 이의 제조방법

Citations (2)

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WO1999048913A1 (en) * 1998-03-24 1999-09-30 The University Of Queensland Peptide turn mimetics
WO2008017852A1 (en) * 2006-08-11 2008-02-14 Palatin Technologies, Inc. Diamine-containing, tetra- substituted piperazine compounds as melanocortin receptor modulators

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JPH08502883A (ja) 1992-08-21 1996-04-02 ヴァー ファルム アーベー ヒトメラノサイト刺激ホルモンレセプター
US5622860A (en) 1994-02-17 1997-04-22 The Regents Of The University Of Michigan Genes encoding melanocortin receptors
WO1996022304A1 (en) 1995-01-20 1996-07-25 Molecumetics, Ltd. Conformationally constrained reverse-turn library and methods relating thereto
US5929237A (en) 1995-10-27 1999-07-27 Molecumetics Ltd. Reverse-turn mimetics and methods relating thereto
AU7162698A (en) 1997-04-25 1998-11-24 Regents Of The University Of California, The Dipeptide surrogates containing asparagine-derived tetrahydropyrimidinones
AU742747B2 (en) 1998-03-24 2002-01-10 Mimetica Pty Ltd Peptide turn mimetics
CA2349848A1 (en) 1998-11-09 2000-05-18 Merck & Co., Inc. Dna molecules encoding the melanocortin 5 receptor protein from rhesus monkey
EP1289965B1 (en) * 2000-05-25 2005-10-26 F. Hoffmann-La Roche Ag Substituted 1-aminoalkyl-lactams and their use as muscarinic receptor antagonists
CA2462200A1 (en) * 2001-08-10 2003-02-20 Palatin Technologies, Inc. Peptidomimetics of biologically active metallopeptides
US20030110518A1 (en) 2001-09-28 2003-06-12 Houseknecht Karen L. Melanocortin-5 receptor sequences and uses thereof
US6916812B2 (en) * 2001-10-09 2005-07-12 Bristol-Myers Squibb Company Alpha-aminoamide derivatives as melanocortin agonists
SG176310A1 (en) 2001-11-08 2011-12-29 Ortho Mcneil Pharm Inc Novel 1,2,4-thiadiazole derivatives as melanocortin receptor modulators
US7319107B2 (en) 2001-11-08 2008-01-15 Johnson & Johnson Consumer Companies, Inc. 1,2,4-thiadiazolium derivatives as melanocortin receptor modulators
AU2003216274A1 (en) * 2002-02-11 2003-09-04 Neurocrine Biosciences, Inc. Pyrrole derivatives as ligands of melanocortin receptors
BRPI0411673A (pt) * 2003-06-20 2006-08-08 Amgen Inc composto, sal farmaceuticamente aceitável, composição farmacêutica, e, uso de um composto
US7281642B2 (en) * 2004-09-16 2007-10-16 Prime Time Toys, Ltd. Squirting toy
AU2009219107B2 (en) * 2008-02-29 2013-11-21 Marp Therapeutics Pty Ltd Methods of modulating the activity of the MC5 receptor and treatment of conditions related to this receptor

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999048913A1 (en) * 1998-03-24 1999-09-30 The University Of Queensland Peptide turn mimetics
WO2008017852A1 (en) * 2006-08-11 2008-02-14 Palatin Technologies, Inc. Diamine-containing, tetra- substituted piperazine compounds as melanocortin receptor modulators

Also Published As

Publication number Publication date
EP2257534A4 (en) 2011-05-04
WO2009105823A1 (en) 2009-09-03
NZ587363A (en) 2012-06-29
RU2530017C2 (ru) 2014-10-10
EP2257534B1 (en) 2013-11-06
CA2716250C (en) 2016-02-16
IL207700A (en) 2017-01-31
BRPI0907903B1 (pt) 2021-11-09
IL207700A0 (en) 2010-12-30
US8008291B2 (en) 2011-08-30
BRPI0907903A2 (pt) 2020-08-18
US20090221557A1 (en) 2009-09-03
ES2445456T3 (es) 2014-03-03
DK2257534T3 (da) 2014-02-03
JP2011513244A (ja) 2011-04-28
MX2010009487A (es) 2011-03-02
CA2716250A1 (en) 2009-09-03
PT2257534E (pt) 2014-02-17
CN102007105A (zh) 2011-04-06
HK1148730A1 (en) 2011-09-16
KR101620114B1 (ko) 2016-05-12
CN102007105B (zh) 2014-09-03
AU2009219106A1 (en) 2009-09-03
KR20100122102A (ko) 2010-11-19
RU2010137034A (ru) 2012-04-10
JP5503557B2 (ja) 2014-05-28
EP2257534A1 (en) 2010-12-08

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