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WO2001062765A3 - Small molecule modulators of g protein-coupled receptor six - Google Patents

Small molecule modulators of g protein-coupled receptor six Download PDF

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Publication number
WO2001062765A3
WO2001062765A3 PCT/US2000/004945 US0004945W WO0162765A3 WO 2001062765 A3 WO2001062765 A3 WO 2001062765A3 US 0004945 W US0004945 W US 0004945W WO 0162765 A3 WO0162765 A3 WO 0162765A3
Authority
WO
WIPO (PCT)
Prior art keywords
protein
small molecule
coupled receptor
molecule modulators
compounds
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/US2000/004945
Other languages
French (fr)
Other versions
WO2001062765A2 (en
Inventor
Nigel R A Beeley
Dominic P Behan
Derek T Chalmers
Frederique Menzaghi
Sonja Strah-Pleynet
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Arena Pharmaceuticals Inc
Original Assignee
Arena Pharmaceuticals Inc
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 Arena Pharmaceuticals Inc filed Critical Arena Pharmaceuticals Inc
Priority to IL14493400A priority Critical patent/IL144934A0/en
Priority to CA002368447A priority patent/CA2368447A1/en
Priority to AU64535/01A priority patent/AU6453501A/en
Priority to MXPA01008618A priority patent/MXPA01008618A/en
Priority to JP2001562547A priority patent/JP2004515449A/en
Priority to EP00993678A priority patent/EP1200427A2/en
Priority to KR1020017010819A priority patent/KR20020015307A/en
Anticipated expiration legal-status Critical
Publication of WO2001062765A2 publication Critical patent/WO2001062765A2/en
Publication of WO2001062765A3 publication Critical patent/WO2001062765A3/en
Ceased legal-status Critical Current

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/30Oxygen or sulfur atoms
    • C07D233/42Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/705Assays involving receptors, cell surface antigens or cell surface determinants
    • G01N2333/72Assays involving receptors, cell surface antigens or cell surface determinants for hormones
    • G01N2333/726G protein coupled receptor, e.g. TSHR-thyrotropin-receptor, LH/hCG receptor, FSH

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Disclosed herein are small molecule modulators of the G protein-coupled receptor six, represented structurally as follows: formula(I) or formula (II), methods of making such compounds, and methods of using such compounds.
PCT/US2000/004945 1999-02-26 2000-02-25 Small molecule modulators of g protein-coupled receptor six Ceased WO2001062765A2 (en)

Priority Applications (7)

Application Number Priority Date Filing Date Title
IL14493400A IL144934A0 (en) 1999-02-26 2000-02-25 Small molecule modulators of g protein-coupled receptor six
CA002368447A CA2368447A1 (en) 1999-02-26 2000-02-25 Small molecule modulators of g protein-coupled receptor six
AU64535/01A AU6453501A (en) 1999-02-26 2000-02-25 Small molecule modulators of G protein-coupled receptor six
MXPA01008618A MXPA01008618A (en) 1999-02-26 2000-02-25 Small molecule modulators of g protein-coupled receptor six.
JP2001562547A JP2004515449A (en) 1999-02-26 2000-02-25 Small molecule modulator of 6G protein-coupled receptor
EP00993678A EP1200427A2 (en) 1999-02-26 2000-02-25 Small molecule modulators of g protein-coupled receptor six (gpr6)
KR1020017010819A KR20020015307A (en) 1999-02-26 2000-02-25 Small Molecule Modulators of G Protein-Coupled Receptor Six

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US12185199P 1999-02-26 1999-02-26
US60/121,851 1999-02-26
US17385099P 1999-12-30 1999-12-30
US60/173,850 1999-12-30
US17442800P 2000-01-04 2000-01-04
US60/174,428 2000-01-04

Publications (2)

Publication Number Publication Date
WO2001062765A2 WO2001062765A2 (en) 2001-08-30
WO2001062765A3 true WO2001062765A3 (en) 2002-03-07

Family

ID=27382687

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2000/004945 Ceased WO2001062765A2 (en) 1999-02-26 2000-02-25 Small molecule modulators of g protein-coupled receptor six

Country Status (6)

Country Link
JP (1) JP2004515449A (en)
KR (1) KR20020015307A (en)
CN (1) CN1364167A (en)
AU (1) AU6453501A (en)
MX (1) MXPA01008618A (en)
WO (1) WO2001062765A2 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003078602A2 (en) * 2002-03-15 2003-09-25 Arena Pharmaceuticals, Inc. Methods of expressing non-endogenous g protein coupled receptors in cells
AU2003274005A1 (en) * 2002-10-24 2004-05-13 Bayer Healthcare Ag Diagnostics and therapeutics for diseases associated with human g-protein coupled receptor 6 (gpr6)
WO2004047776A1 (en) * 2002-11-20 2004-06-10 L'oreal Composition for hair care or eyelashes containing a pyrazol-carboxamide, its use for stimulating hair and eyelash growth and/or for preventing loss thereof
EP1745295B1 (en) 2004-04-20 2010-10-06 Galapagos N.V. Methods, compositions and compound assays for inhibiting amyloid-beta protein production
HRP20131224T1 (en) * 2006-02-15 2014-01-31 Dendreon Corporation Small-molecule modulators of trp-p8 activity
JO3466B1 (en) * 2013-12-20 2020-07-05 Takeda Pharmaceuticals Co Tetrahydropyridopyrazines modulators of gpr6
MY184366A (en) * 2014-02-14 2021-04-01 Takeda Pharmaceuticals Co Pyrazines modulators of gpr6
BR112020019148A2 (en) 2018-03-23 2021-01-26 Carmot Therapeutics, Inc. g protein-coupled receptor modulators
GEAP202416419A (en) 2021-05-13 2024-03-25 Carmot Therapeutics Inc Modulators of g-protein coupled receptors

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999009024A1 (en) * 1997-08-14 1999-02-25 Smithkline Beecham Plc Phenyl urea and phenyl thiourea derivatives as hfgan72 antagonists

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999009024A1 (en) * 1997-08-14 1999-02-25 Smithkline Beecham Plc Phenyl urea and phenyl thiourea derivatives as hfgan72 antagonists

Non-Patent Citations (7)

* Cited by examiner, † Cited by third party
Title
ACTA POL. PHARM., vol. 50, no. 4-5, - 1993, pages 341 - 344 *
CHEMICAL ABSTRACTS, vol. 111, no. 20, 13 November 1989, Columbus, Ohio, US; abstract no. 184593k, GDANIEC, MARIA ET AL.: "Crystal and molecular structure of 3-(4-chloro-benzoylimino)-5,6-dihydro-3H-imidazo(2,1-c)-1,2,4-dithiazole" XP002177674 *
CHEMICAL ABSTRACTS, vol. 121, no. 7, 15 August 1994, Columbus, Ohio, US; abstract no. 83208q, SACZEWSKY, FRANCISZEK: "Synthesis, transformations and tuberculostatic activity of 1-(N-aroylthiocarbamoyl)imidazolidine-2-thiones." XP002177673 *
DATABASE CHEMICAL ABSTRACTS XP002177675 *
DATABASE CHEMICAL ABSTRACTS XP002177676 *
FRACISZEK SACZEWSKI ET AL.: "Synthesis and transformations of 3-benzoylimino-5,6-dihydro-3H-(imidazo(2,1-c)(1,2,4)dithiazole)", SYNTHESIS., vol. 9, - 1986, GEORG THIEME VERLAG. STUTTGART., DE, pages 751 - 753, XP002177672, ISSN: 0039-7881 *
J. CRYSTALLOGR. SPECTROSC. RES., vol. 19, no. 3, - 1989, pages 507 - 512 *

Also Published As

Publication number Publication date
JP2004515449A (en) 2004-05-27
MXPA01008618A (en) 2002-03-20
WO2001062765A2 (en) 2001-08-30
KR20020015307A (en) 2002-02-27
CN1364167A (en) 2002-08-14
AU6453501A (en) 2001-09-03

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