EP2162136A4 - Benzamide mglur5 positive allosteric modulators and methods of making and using same - Google Patents

Benzamide mglur5 positive allosteric modulators and methods of making and using same

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Publication number
EP2162136A4
EP2162136A4 EP08770045A EP08770045A EP2162136A4 EP 2162136 A4 EP2162136 A4 EP 2162136A4 EP 08770045 A EP08770045 A EP 08770045A EP 08770045 A EP08770045 A EP 08770045A EP 2162136 A4 EP2162136 A4 EP 2162136A4
Authority
EP
European Patent Office
Prior art keywords
benzamide
making
methods
same
positive allosteric
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.)
Withdrawn
Application number
EP08770045A
Other languages
German (de)
French (fr)
Other versions
EP2162136A1 (en
Inventor
P Jeffrey Conn
Craig W Lindsley
Charles David Weaver
Alice L Rodriguez
Colleen M Niswender
Carrie K Jones
Richard Williams
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.)
Vanderbilt University
Original Assignee
Vanderbilt University
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 Vanderbilt University filed Critical Vanderbilt University
Publication of EP2162136A1 publication Critical patent/EP2162136A1/en
Publication of EP2162136A4 publication Critical patent/EP2162136A4/en
Withdrawn legal-status Critical Current

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D211/60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • A61K31/166Amides, 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
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Families Citing this family (71)

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Publication number Priority date Publication date Assignee Title
AU2007334436A1 (en) 2006-12-15 2008-06-26 Abbott Laboratories Novel oxadiazole compounds
US8853392B2 (en) 2007-06-03 2014-10-07 Vanderbilt University Benzamide mGluR5 positive allosteric modulators and methods of making and using same
US8034806B2 (en) 2007-11-02 2011-10-11 Vanderbilt University Bicyclic mGluR5 positive allosteric modulators and methods of making and using same
GB0811643D0 (en) 2008-06-25 2008-07-30 Cancer Rec Tech Ltd New therapeutic agents
TW201028421A (en) * 2009-01-15 2010-08-01 Abbott Lab Novel benzenesulfonamides as calcium channel blockers
US8389536B2 (en) 2009-10-27 2013-03-05 Hoffmann-La Roche Inc. Positive allosteric modulators (PAM)
US8586581B2 (en) 2009-12-17 2013-11-19 Hoffmann-La Roche Inc Ethynyl compounds useful for treatment of CNS disorders
EP2513117B1 (en) 2009-12-18 2013-08-28 Janssen Pharmaceutica, N.V. Bicyclic thiazoles as allosteric modulators of mglur5 receptors
US8772301B2 (en) 2009-12-18 2014-07-08 Sunovion Pharmaceuticals, Inc. Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof
CA2782947A1 (en) 2009-12-18 2011-06-23 Janssen Pharmaceutica Nv Bicyclic thiazoles as allosteric modulators of mglur5 receptors
SI2516434T1 (en) 2009-12-23 2015-10-30 Takeda Pharmaceutical Company Limited Fused heteroaromatic pyrrolidinones as syk inhibitors
US8420661B2 (en) 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
AU2011258389A1 (en) 2010-05-24 2012-12-06 Vanderbilt University Substituted-6-methylnicotinamides as mGluR5 positive allosteric modulators
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
US8772300B2 (en) 2011-04-19 2014-07-08 Hoffmann-La Roche Inc. Phenyl or pyridinyl-ethynyl derivatives
EP2702050B1 (en) 2011-04-26 2016-05-18 F.Hoffmann-La Roche Ag Pyrazolidin-3-one derivatives
HUE025031T2 (en) 2011-04-26 2016-02-29 Hoffmann La Roche Ethynyl derivatives as positive allosteric modulators of the mglur5
US9056873B2 (en) 2011-06-22 2015-06-16 Takeda Pharmaceutical Company Limited Substituted 6-aza-isoindolin-1-one derivatives
US20130123254A1 (en) 2011-09-30 2013-05-16 Barbara Biemans Pharmaceutically acceptable mglur5 positive allosteric modulators and their methods of identification
UA110862C2 (en) * 2011-10-07 2016-02-25 Ф. Хоффманн-Ля Рош Аг Ethinyl derivatives as allosteric modulators of metabotropic glutamate receptor 5 mglur
UA110995C2 (en) 2011-10-07 2016-03-10 Ф. Хоффманн-Ля Рош Аг ETHINYL DERIVATIVES AS MODULATORS OF THE METABOTROPIC GLUTAMATE RECEPTOR
TWI622578B (en) * 2011-12-21 2018-05-01 諾維拉治療公司 Hepatitis b antiviral agents
ME03300B (en) 2012-06-13 2019-07-20 Incyte Holdings Corp Substituted tricyclic compounds as fgfr inhibitors
SI2875000T1 (en) 2012-07-17 2017-01-31 F.Hoffmann-La Roche Ag Arylethynyl derivatives
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
UA113223C2 (en) * 2012-08-13 2016-12-26 ARYLETINYLPYRIMIDINE
EA025482B1 (en) 2012-09-27 2016-12-30 Ф. Хоффманн-Ля Рош Аг Arylethynyl derivatives
SG11201501375YA (en) * 2012-10-18 2015-03-30 Hoffmann La Roche Ethynyl derivatives as modulators of mglur5 receptor activity
KR101684816B1 (en) * 2012-10-18 2016-12-20 에프. 호프만-라 로슈 아게 Ethynyl derivatives as modulators of mglur5 receptor activity
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
DK2986610T5 (en) 2013-04-19 2018-12-10 Incyte Holdings Corp BICYCLIC HETEROCYCLES AS FGFR INHIBITORS
DK3049409T3 (en) * 2013-09-25 2017-07-10 Hoffmann La Roche ethynyl derivatives
TWI649310B (en) * 2014-01-10 2019-02-01 赫孚孟拉羅股份公司 Acetylene derivative
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
EA038045B1 (en) 2015-02-20 2021-06-28 Инсайт Корпорейшн Bicyclic heterocycles as fgfr inhibitors
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MA41551A (en) 2015-02-20 2017-12-26 Incyte Corp BICYCLIC HETEROCYCLES USED AS FGFR4 INHIBITORS
TWI713497B (en) 2015-02-26 2020-12-21 南韓商愛思開生物製藥股份有限公司 Imidazopyrimidine and imidazotriazine derivative, and pharmaceutical composition comprising the same
CN106146391A (en) * 2015-04-15 2016-11-23 中国科学院上海药物研究所 Substituted benzamide compound of 5-fragrance alkynyl and preparation method thereof, pharmaceutical composition and purposes
CN107849006B (en) 2015-06-03 2020-11-13 豪夫迈·罗氏有限公司 Ethynyl derivatives
EP3319968A1 (en) 2015-07-06 2018-05-16 Rodin Therapeutics, Inc. Heterobicyclic n-aminophenyl-amides as inhibitors of histone deacetylase
PL3319959T3 (en) 2015-07-06 2022-02-14 Alkermes, Inc. Hetero-halo inhibitors of histone deacetylase
CN107580598B (en) 2015-07-15 2020-11-13 豪夫迈·罗氏有限公司 Ethynyl derivatives as metabotropic glutamate receptor modulators
GB201517217D0 (en) 2015-09-29 2015-11-11 Astex Therapeutics Ltd And Cancer Res Technology Ltd Pharmaceutical compounds
GB201517216D0 (en) 2015-09-29 2015-11-11 Cancer Res Technology Ltd And Astex Therapeutics Ltd Pharmaceutical compounds
PE20190382A1 (en) 2016-07-18 2019-03-08 Hoffmann La Roche ETHINYL DERIVATIVES
WO2018132533A1 (en) 2017-01-11 2018-07-19 Rodin Therapeutics, Inc. Bicyclic inhibitors of histone deacetylase
GB201704966D0 (en) 2017-03-28 2017-05-10 Astex Therapeutics Ltd Pharmaceutical compounds
GB201704965D0 (en) 2017-03-28 2017-05-10 Astex Therapeutics Ltd Pharmaceutical compounds
AR111960A1 (en) 2017-05-26 2019-09-04 Incyte Corp CRYSTALLINE FORMS OF A FGFR INHIBITOR AND PROCESSES FOR ITS PREPARATION
SI3664802T1 (en) 2017-08-07 2022-10-28 Alkermes, Inc. Bicyclic inhibitors of histone deacetylase
US11466004B2 (en) 2018-05-04 2022-10-11 Incyte Corporation Solid forms of an FGFR inhibitor and processes for preparing the same
EA202092649A1 (en) 2018-05-04 2021-06-21 Инсайт Корпорейшн FGFR INHIBITOR SALTS
DE102019200805A1 (en) * 2019-01-23 2020-07-23 Henkel Ag & Co. Kgaa New fluorescent materials based on phthalimides
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
IL291901A (en) 2019-10-14 2022-06-01 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
KR20220131900A (en) 2019-12-04 2022-09-29 인사이트 코포레이션 Derivatives of FGFR inhibitors
WO2021113479A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US11691971B2 (en) 2020-06-19 2023-07-04 Incyte Corporation Naphthyridinone compounds as JAK2 V617F inhibitors
US11753413B2 (en) 2020-06-19 2023-09-12 Incyte Corporation Substituted pyrrolo[2,1-f][1,2,4]triazine compounds as JAK2 V617F inhibitors
WO2022006456A1 (en) 2020-07-02 2022-01-06 Incyte Corporation Tricyclic pyridone compounds as jak2 v617f inhibitors
MX2023000056A (en) 2020-07-02 2023-04-12 Incyte Corp Tricyclic urea compounds as jak2 v617f inhibitors.
KR20220014854A (en) * 2020-07-29 2022-02-07 주식회사 비보존 Dual Modulator of mGluR5 and 5-HT2A Receptor, and Use Thereof
JP2023539463A (en) 2020-08-17 2023-09-14 アリゴス セラピューティクス インコーポレイテッド Methods and compositions for targeting PD-L1
US11661422B2 (en) 2020-08-27 2023-05-30 Incyte Corporation Tricyclic urea compounds as JAK2 V617F inhibitors
WO2022140231A1 (en) 2020-12-21 2022-06-30 Incyte Corporation Deazaguaine compounds as jak2 v617f inhibitors
TW202302589A (en) 2021-02-25 2023-01-16 美商英塞特公司 Spirocyclic lactams as jak2 v617f inhibitors
AR126102A1 (en) 2021-06-09 2023-09-13 Incyte Corp TRICYCLIC HETEROCYCLES AS FGFR INHIBITORS
KR20230116709A (en) * 2022-01-27 2023-08-04 주식회사 비보존 Pharmaceutical composition for prevention or treatment of mental disorder

Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003009807A2 (en) * 2001-07-23 2003-02-06 Galileo Laboratories, Inc. Cytoprotective compounds, pharmaceutical and cosmetic formulations, and methods
US6656957B1 (en) * 1997-07-11 2003-12-02 Novartis Ag Pyridine derivatives
WO2004009549A2 (en) * 2002-07-18 2004-01-29 Actelion Pharmaceuticals Ltd Piperidines useful for the treatment of central nervous system disorders
WO2005040144A1 (en) * 2003-10-15 2005-05-06 Glaxo Group Limited Novel compounds
WO2005044797A1 (en) * 2003-11-06 2005-05-19 Addex Pharmaceuticals Sa Allosteric modulators of metabotropic glutamate receptors
WO2005046683A1 (en) * 2003-10-07 2005-05-26 Renovis, Inc. Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
WO2006089700A1 (en) * 2005-02-22 2006-08-31 Novartis Ag Pyrrolidine and piperidine acetylene derivatives for use as mglur5 antagonists
WO2006093832A2 (en) * 2005-02-28 2006-09-08 Renovis, Inc. Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
US20060235069A1 (en) * 2003-03-26 2006-10-19 Duggan Mark E Benzamide modulators of metabotropic glutamate receptors
EP1748048A1 (en) * 2004-05-10 2007-01-31 Banyu Pharmaceutical Co., Ltd. Imidazopyridine compound

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9823871D0 (en) * 1998-10-30 1998-12-23 Pharmacia & Upjohn Spa 2-Amino-thiazole derivatives, process for their preparation, and their use as antitumour agents

Patent Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6656957B1 (en) * 1997-07-11 2003-12-02 Novartis Ag Pyridine derivatives
WO2003009807A2 (en) * 2001-07-23 2003-02-06 Galileo Laboratories, Inc. Cytoprotective compounds, pharmaceutical and cosmetic formulations, and methods
WO2004009549A2 (en) * 2002-07-18 2004-01-29 Actelion Pharmaceuticals Ltd Piperidines useful for the treatment of central nervous system disorders
US20060235069A1 (en) * 2003-03-26 2006-10-19 Duggan Mark E Benzamide modulators of metabotropic glutamate receptors
WO2005046683A1 (en) * 2003-10-07 2005-05-26 Renovis, Inc. Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
WO2005040144A1 (en) * 2003-10-15 2005-05-06 Glaxo Group Limited Novel compounds
WO2005044797A1 (en) * 2003-11-06 2005-05-19 Addex Pharmaceuticals Sa Allosteric modulators of metabotropic glutamate receptors
EP1748048A1 (en) * 2004-05-10 2007-01-31 Banyu Pharmaceutical Co., Ltd. Imidazopyridine compound
WO2006089700A1 (en) * 2005-02-22 2006-08-31 Novartis Ag Pyrrolidine and piperidine acetylene derivatives for use as mglur5 antagonists
WO2006093832A2 (en) * 2005-02-28 2006-09-08 Renovis, Inc. Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
A. BÖCKER ET AL: "GPCR Targeted Library Design: Novel Dopamine D3 Receptor Ligands", CHEMMEDCHEM, vol. 2, no. 7, 3 May 2007 (2007-05-03), pages 1000 - 1005, XP055082133, ISSN: 1860-7179, DOI: 10.1002/cmdc.200700067 *
ANDREAS RITZÉN ET AL: "Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, ELSEVIER SCIENCE, GB, vol. 19, no. 12, 15 June 2009 (2009-06-15), pages 3275 - 3278, XP002664735, ISSN: 0960-894X, [retrieved on 20090424], DOI: 10.1016/J.BMCL.2009.04.095 *
DE PAULIS ET AL: "Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation on the metabotropic glutamate-5 receptor in rat cortical astrocytes", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 49, 1 January 2006 (2006-01-01), pages 3332 - 3344, XP008103364, ISSN: 0022-2623, DOI: 10.1021/JM051252J *
RODRIGUEZ ALICE L ET AL: "Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity", MOLECULAR PHARMACOLOGY, AMERICAN SOCIETY FOR PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, US, vol. 78, no. 6, 1 December 2010 (2010-12-01), pages 1105 - 1123, XP008145887, ISSN: 0026-895X, [retrieved on 20101005], DOI: 10.1124/MOL.110.067207 *
SAMS A G ET AL: "Efficacy switching SAR of mGluR5 allosteric modulators: Highly potent positive and negative modulators from one chemotype", BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS 20110601 ELSEVIER LTD GBR LNKD- DOI:10.1016/J.BMCL.2011.03.103, vol. 21, no. 11, 1 June 2011 (2011-06-01), pages 3407 - 3410, XP002674409, ISSN: 0960-894X *
See also references of WO2008151184A1 *

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