EA018328B1 - Новые гетероциклические соединения в качестве антагонистов метаботропных глутаматных рецепторов 5-го подтипа (мглу5) - Google Patents

Новые гетероциклические соединения в качестве антагонистов метаботропных глутаматных рецепторов 5-го подтипа (мглу5) Download PDF

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Publication number
EA018328B1
EA018328B1 EA201000283A EA201000283A EA018328B1 EA 018328 B1 EA018328 B1 EA 018328B1 EA 201000283 A EA201000283 A EA 201000283A EA 201000283 A EA201000283 A EA 201000283A EA 018328 B1 EA018328 B1 EA 018328B1
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EA
Eurasian Patent Office
Prior art keywords
pyridyl
piperidine
prop
methyl
ynylidene
Prior art date
Application number
EA201000283A
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English (en)
Russian (ru)
Other versions
EA201000283A1 (ru
Inventor
Амедео Леонарди
Гьянни Мотта
Карло Рива
Елена Поггеси
Давид Грацьяни
Маттео Марко Лонги
Original Assignee
Рекордати Айерленд Лимитед
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Application filed by Рекордати Айерленд Лимитед filed Critical Рекордати Айерленд Лимитед
Publication of EA201000283A1 publication Critical patent/EA201000283A1/ru
Publication of EA018328B1 publication Critical patent/EA018328B1/ru

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    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D405/14—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 three or more hetero rings
    • 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/02—Heterocyclic 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
    • C07D513/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
EA201000283A 2007-08-02 2008-08-01 Новые гетероциклические соединения в качестве антагонистов метаботропных глутаматных рецепторов 5-го подтипа (мглу5) EA018328B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US95367707P 2007-08-02 2007-08-02
US4517508P 2008-04-15 2008-04-15
PCT/EP2008/006351 WO2009015897A1 (en) 2007-08-02 2008-08-01 Novel heterocyclic compounds as mglu5 antagonists

Publications (2)

Publication Number Publication Date
EA201000283A1 EA201000283A1 (ru) 2010-06-30
EA018328B1 true EA018328B1 (ru) 2013-07-30

Family

ID=39885225

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201000283A EA018328B1 (ru) 2007-08-02 2008-08-01 Новые гетероциклические соединения в качестве антагонистов метаботропных глутаматных рецепторов 5-го подтипа (мглу5)

Country Status (22)

Country Link
US (1) US8518916B2 (https=)
EP (1) EP2178858B1 (https=)
JP (1) JP5412430B2 (https=)
KR (1) KR20100052507A (https=)
CN (1) CN101821256A (https=)
AT (1) ATE539075T1 (https=)
AU (1) AU2008282032B2 (https=)
BR (1) BRPI0814182A2 (https=)
CA (1) CA2694359A1 (https=)
CY (1) CY1112500T1 (https=)
DK (1) DK2178858T3 (https=)
EA (1) EA018328B1 (https=)
ES (1) ES2380165T3 (https=)
HR (1) HRP20120225T1 (https=)
IL (1) IL203659A (https=)
NZ (1) NZ582934A (https=)
PL (1) PL2178858T3 (https=)
PT (1) PT2178858E (https=)
RS (1) RS52167B (https=)
SI (1) SI2178858T1 (https=)
WO (1) WO2009015897A1 (https=)
ZA (1) ZA201001467B (https=)

Families Citing this family (9)

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WO2010089119A1 (en) * 2009-02-04 2010-08-12 Recordati Ireland Limited Heterocyclic derivatives as m-glu5 antagonists
US20120028931A1 (en) * 2009-09-14 2012-02-02 Recordati Ireland Limited Heterocyclic m-glu5 antagonists
WO2012085166A1 (en) * 2010-12-22 2012-06-28 Merz Pharma Gmbh & Co. Kgaa Metabotropic glutamate receptor modulators
AR084515A1 (es) * 2010-12-22 2013-05-22 Merz Pharma Gmbh & Co Kgaa Derivados heterociclicos nitrogenados, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades asociadas al sistema nervioso central tales como parkinson y alzheimer, entre otras
CN104011016B (zh) * 2011-12-27 2016-08-17 帝斯曼知识产权资产管理有限公司 维生素a中间体的催化合成
CN102827056B (zh) * 2012-09-03 2014-07-23 华东理工大学 N-芳基取代吡咯烷酮衍生物及其用途
WO2014039049A1 (en) * 2012-09-07 2014-03-13 Empire Technology Development Llc Regioregular copolymers and methods for making same
AU2014211727B2 (en) * 2013-02-04 2018-07-26 Prexton Therapeutics Sa Positive allosteric modulators of mGluR3
CA3066193A1 (en) * 2017-06-29 2019-01-03 Recordati Industria Chimica E Farmaceutica Spa Heterocyclylmethylidene derivatives and their use as modulators of mglur5 receptors

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JPS5995249A (ja) * 1982-11-24 1984-06-01 Ono Pharmaceut Co Ltd ロイコトリエンｂ４類似化合物、その製造方法及びそれらを有効成分として含有する治療剤
EP0537993A1 (en) * 1991-10-17 1993-04-21 Eli Lilly And Company Nicotinic activity of a series of arecolones and isoarecolones
WO2001002386A1 (en) * 1999-07-01 2001-01-11 Mediolanum Farmaceutici S.P.A. SELECTIVE M2 MUSCARINIC RECEPTOR ANTAGONISTS HAVING 5H-DIBENZ[b,f]AZEPINE STRUCTURE
US6265434B1 (en) * 1999-04-06 2001-07-24 Merck & Co., Inc. Pyrrolidine modulators of chemokine receptor activity
WO2003093236A1 (en) * 2002-05-02 2003-11-13 Euro-Celtique, S.A. 1-(pyrid-2-yl)-piperazine compounds as metabotropic glutamate receptor inhibitor
WO2004020435A1 (en) * 2002-08-16 2004-03-11 Janssen Pharmaceutica N.V. Piperidinyl compounds that selectively bind integrins
US20040077671A1 (en) * 1999-04-01 2004-04-22 Chu-Moyer Margaret Y. Sorbitol dehydrogenase inhibitors
WO2004069158A2 (en) * 2003-01-27 2004-08-19 Merck & Co., Inc. Substituted pyrazoles, compositions containing such compounds and methods of use
US20040186292A1 (en) * 2002-05-28 2004-09-23 Tao Wang Indole, azaindole and related heterocyclic 4-alkenyl piperidine amides
US20050065156A1 (en) * 2003-09-17 2005-03-24 Li James J. Compounds useful as motilin agonists and method
WO2005090347A1 (fr) * 2004-02-26 2005-09-29 Sanofi-Aventis Derives d’aryl- et d’heteroaryl-piperidinecarboxylates, leur preparation et leur application comme inhibiteurs de l'enzyme faah
WO2006089700A1 (en) * 2005-02-22 2006-08-31 Novartis Ag Pyrrolidine and piperidine acetylene derivatives for use as mglur5 antagonists
US20060264415A1 (en) * 2005-04-01 2006-11-23 Methylgene Inc. Inhibitors of histone deacetylase
WO2007006530A1 (en) * 2005-07-12 2007-01-18 Novartis Ag Use of mglur5 (esp. afq056) in gi (esp. gerd)
WO2007070173A2 (en) * 2005-10-31 2007-06-21 Merck & Co., Inc. Cetp inhibitors
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US2867620A (en) * 1956-08-30 1959-01-06 Lakeside Lab Inc N-alkylpiperidyl alkynylamines
JPS5995249A (ja) * 1982-11-24 1984-06-01 Ono Pharmaceut Co Ltd ロイコトリエンｂ４類似化合物、その製造方法及びそれらを有効成分として含有する治療剤
EP0537993A1 (en) * 1991-10-17 1993-04-21 Eli Lilly And Company Nicotinic activity of a series of arecolones and isoarecolones
US20040077671A1 (en) * 1999-04-01 2004-04-22 Chu-Moyer Margaret Y. Sorbitol dehydrogenase inhibitors
US6265434B1 (en) * 1999-04-06 2001-07-24 Merck & Co., Inc. Pyrrolidine modulators of chemokine receptor activity
WO2001002386A1 (en) * 1999-07-01 2001-01-11 Mediolanum Farmaceutici S.P.A. SELECTIVE M2 MUSCARINIC RECEPTOR ANTAGONISTS HAVING 5H-DIBENZ[b,f]AZEPINE STRUCTURE
WO2003093236A1 (en) * 2002-05-02 2003-11-13 Euro-Celtique, S.A. 1-(pyrid-2-yl)-piperazine compounds as metabotropic glutamate receptor inhibitor
US20040186292A1 (en) * 2002-05-28 2004-09-23 Tao Wang Indole, azaindole and related heterocyclic 4-alkenyl piperidine amides
WO2004020435A1 (en) * 2002-08-16 2004-03-11 Janssen Pharmaceutica N.V. Piperidinyl compounds that selectively bind integrins
WO2004069158A2 (en) * 2003-01-27 2004-08-19 Merck & Co., Inc. Substituted pyrazoles, compositions containing such compounds and methods of use
US20050065156A1 (en) * 2003-09-17 2005-03-24 Li James J. Compounds useful as motilin agonists and method
WO2005090347A1 (fr) * 2004-02-26 2005-09-29 Sanofi-Aventis Derives d’aryl- et d’heteroaryl-piperidinecarboxylates, leur preparation et leur application comme inhibiteurs de l'enzyme faah
WO2006089700A1 (en) * 2005-02-22 2006-08-31 Novartis Ag Pyrrolidine and piperidine acetylene derivatives for use as mglur5 antagonists
US20060264415A1 (en) * 2005-04-01 2006-11-23 Methylgene Inc. Inhibitors of histone deacetylase
WO2007006530A1 (en) * 2005-07-12 2007-01-18 Novartis Ag Use of mglur5 (esp. afq056) in gi (esp. gerd)
WO2007070173A2 (en) * 2005-10-31 2007-06-21 Merck & Co., Inc. Cetp inhibitors
WO2007118137A1 (en) * 2006-04-07 2007-10-18 Methylgene Inc. Benzamide derivatives as inhibitors of histone deacetylase

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HIDENORI SOMEYA ET AL.: "Cobalt-catalyzed sequential cyclization/cross-coupling reactions of 6-halo-1-hexene derivatives with Grignard reagents and their application to the synthesis of 1,3-diols", TETRAHEDRON, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, NL, vol. 63, no. 35, 27 July 2007 (2007-07-27), pages 8609-8618, XP022173637, ISSN: 0040-4020, compounds 18A, 18B *
JEFFREY M. DENER ET AL.: "Dibasic inhibitors of human mast cell tryptase. Part 3: Identification of a series of potent and selective inhibitors containing the benzamidine functionality", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 11, no. 13, 2001, pages 1629-1633, XP002503624, compound 19 *
JOHN H. BIEL AND FRANK DIPIERRO: "Hypotensive agents. I. Acetylenic diamines", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 80, 1958, pages 4609-4614, XP002503626, table I, entries 37-39; table II, entries 34-36 *
NEEL K. ANAND AND ERICK M. CARREIRA: "А simple, mild, catalytic, enantioselective addition of terminal acetylenes to aldehydes", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 123, no. 39, 2001, pages 9687-9688, XP002503625, equation 1, table 1, entry 14 *

Also Published As

Publication number Publication date
DK2178858T3 (da) 2012-03-19
EP2178858A1 (en) 2010-04-28
JP2010535165A (ja) 2010-11-18
CY1112500T1 (el) 2015-12-09
WO2009015897A1 (en) 2009-02-05
NZ582934A (en) 2011-10-28
BRPI0814182A2 (pt) 2015-01-27
EA201000283A1 (ru) 2010-06-30
ES2380165T3 (es) 2012-05-09
RS52167B (sr) 2012-08-31
AU2008282032A1 (en) 2009-02-05
ATE539075T1 (de) 2012-01-15
CA2694359A1 (en) 2009-02-05
HK1141788A1 (en) 2010-11-19
ZA201001467B (en) 2010-11-24
US20090042841A1 (en) 2009-02-12
CN101821256A (zh) 2010-09-01
JP5412430B2 (ja) 2014-02-12
EP2178858B1 (en) 2011-12-28
KR20100052507A (ko) 2010-05-19
US8518916B2 (en) 2013-08-27
HRP20120225T1 (hr) 2012-04-30
SI2178858T1 (sl) 2012-03-30
IL203659A (en) 2013-06-27
AU2008282032B2 (en) 2014-08-07
PT2178858E (pt) 2012-02-24
PL2178858T3 (pl) 2012-07-31

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