WO2014035829A1 - Analogues de 3-aminothiéno[2,3-c]pyridine-2-carboxamide substitués utilisés comme modulateurs allostériques positifs - Google Patents

Analogues de 3-aminothiéno[2,3-c]pyridine-2-carboxamide substitués utilisés comme modulateurs allostériques positifs Download PDF

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Publication number
WO2014035829A1
WO2014035829A1 PCT/US2013/056441 US2013056441W WO2014035829A1 WO 2014035829 A1 WO2014035829 A1 WO 2014035829A1 US 2013056441 W US2013056441 W US 2013056441W WO 2014035829 A1 WO2014035829 A1 WO 2014035829A1
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alkyl
independently selected
polyhaloalkyl
hydrogen
monohaloalkyl
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PCT/US2013/056441
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English (en)
Inventor
Craig W. Lindsley
P. Jeffrey Conn
Michael R. Wood
Michael S. Poslusney
Thomas M. Bridges
John S. DANIELS
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Vanderbilt University
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Selon un aspect, l'invention concerne des analogues de 3-aminothiéno[2,3-c]pyridine-2-carboxamide substitués, leurs dérivés et des composés associés, qui sont utiles comme modulateurs allostériques positifs du récepteur muscarinique de l'acétylcholine M4 (mAChR M4); des procédés de synthèse pour fabriquer les composés; des compositions pharmaceutiques les comportant; des méthodes de traitement de troubles neurologiques et psychiatriques associés avec le dysfonctionnement des récepteurs muscariniques de l'acétylcholine à l'aide des composés et des compositions. Cet abrégé est destiné comme outil de criblage à des fins de recherche dans la technique particulière et n'est pas destiné à être limitatif de la présente invention.
PCT/US2013/056441 2012-08-31 2013-08-23 Analogues de 3-aminothiéno[2,3-c]pyridine-2-carboxamide substitués utilisés comme modulateurs allostériques positifs WO2014035829A1 (fr)

Applications Claiming Priority (2)

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US201261696017P 2012-08-31 2012-08-31
US61/696,017 2012-08-31

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WO2014035829A1 true WO2014035829A1 (fr) 2014-03-06

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Cited By (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9493481B2 (en) 2012-02-23 2016-11-15 Vanderbilt University Substituted 5-aminothieno[2,3—C]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4
US9637498B2 (en) 2013-08-23 2017-05-02 Vanderbilt University Substituted thieno[2,3-C]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4
WO2018002760A1 (fr) 2016-07-01 2018-01-04 Pfizer Inc. Dérivés de 5,7-dihydro-pyrrolo-pyridine pour le traitement de maladies neurologiques et neurodégénératives
WO2018035444A1 (fr) * 2016-08-18 2018-02-22 Vanderbilt University Modulateurs allostériques positifs du récepteur muscarinique de l'acétylcholine m4
WO2018211530A1 (fr) 2017-05-19 2018-11-22 Council Of Scientific & Industrial Research Méthanopyrido [2, 1-a] isoindolones substituées utilisées en tant que modulateurs de machr pour traiter diverses conditions pathophysiologiques associées et leur procédé de préparation
WO2018234953A1 (fr) 2017-06-22 2018-12-27 Pfizer Inc. Dérivés de dihydro-pyrrolo-pyridine
US10189857B2 (en) 2016-09-13 2019-01-29 Vanderbilt University Positive allosteric modulators of the muscarinic acetylcholine receptor M4
US10329289B2 (en) 2015-12-23 2019-06-25 Merck Sharp & Dohme Corp. 6,7-dihydro-5H-pyrrolo[3,4-B]pyridin-5-one allosteric modulators of the M4 muscarinic acetylcholine receptor
US10342782B2 (en) 2016-07-27 2019-07-09 Vanderbilt University Positive allosteric modulators of the muscarinic acetylcholine receptor M4
US10512638B2 (en) 2015-12-23 2019-12-24 Merck Sharp & Dohme Corp. 3-(1H-pyrazol-4-yl)pyridine allosteric modulators of the M4 muscarinic acetylcholine receptor
US10836775B2 (en) 2016-12-22 2020-11-17 Merck Sharp & Dohme Corp. 6,6-fused heteroaryl piperidine ether allosteric modulators of the M4 muscarinic acetylcholine receptor
EP3665175A4 (fr) * 2017-08-08 2020-12-09 Vanderbilt University Antagonistes du récepteur muscarinique de l'acétylcholine m4
US11319298B2 (en) 2016-12-22 2022-05-03 Merck Sharp & Dohme Corp. Heteroaryl piperidine ether allosteric modulators of the M4 muscarinic acetylcholine receptor
WO2023114224A1 (fr) 2021-12-13 2023-06-22 Sage Therapeutics, Inc. Combinaison de modulateurs positifs du récepteur muscarinique et de modulateurs allostériques positifs de nmda

Citations (5)

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WO1997005139A1 (fr) * 1995-07-28 1997-02-13 Abbott Laboratories Furopyridine, thienopyridine, pyrrolopyridine et composes connexes a base de pyrimidine, de pyridazine et de triazine utiles pour gerer la transmission synaptique par voie chimique
US20090105244A1 (en) * 2004-10-25 2009-04-23 Eli Lilly And Company Thienopyridines as allosteric potentiators of the m4 muscarinic receptor
WO2011063415A2 (fr) * 2009-11-23 2011-05-26 Afraxis, Inc. Méthodes de traitement de trouble cognitif léger
WO2012007593A1 (fr) * 2010-07-16 2012-01-19 Vib Vzw Domaines de liaison à des protéines stabilisant les états conformationnels fonctionnels de gpcr et utilisations de ceux-ci
US8247409B2 (en) * 2006-04-21 2012-08-21 Amgen Inc. Thieno-[2,3-d]pyrimidine and thieno-pyridazine compounds and methods of use

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997005139A1 (fr) * 1995-07-28 1997-02-13 Abbott Laboratories Furopyridine, thienopyridine, pyrrolopyridine et composes connexes a base de pyrimidine, de pyridazine et de triazine utiles pour gerer la transmission synaptique par voie chimique
US20090105244A1 (en) * 2004-10-25 2009-04-23 Eli Lilly And Company Thienopyridines as allosteric potentiators of the m4 muscarinic receptor
US8247409B2 (en) * 2006-04-21 2012-08-21 Amgen Inc. Thieno-[2,3-d]pyrimidine and thieno-pyridazine compounds and methods of use
WO2011063415A2 (fr) * 2009-11-23 2011-05-26 Afraxis, Inc. Méthodes de traitement de trouble cognitif léger
WO2012007593A1 (fr) * 2010-07-16 2012-01-19 Vib Vzw Domaines de liaison à des protéines stabilisant les états conformationnels fonctionnels de gpcr et utilisations de ceux-ci

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
LE, UM.: "Optimization and Characterization of Muscarinic Acetylcholine Receptor M4 Positive Allosteric Modulators.", MS DISSERTATION, December 2011 (2011-12-01), pages 1 - 102, Retrieved from the Internet <URL:http://etd.library.vanderbilt.edu/available/etd-12112011-145832/unrestricted/le.pdf> [retrieved on 20131230] *

Cited By (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9868746B2 (en) 2012-02-23 2018-01-16 Vanderbilt University Substituted 5-aminothieno[2,3-C]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4
US9493481B2 (en) 2012-02-23 2016-11-15 Vanderbilt University Substituted 5-aminothieno[2,3—C]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4
US9637498B2 (en) 2013-08-23 2017-05-02 Vanderbilt University Substituted thieno[2,3-C]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4
US10351564B2 (en) 2015-12-23 2019-07-16 Merck Sharop & Dohme, Corp. 6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-5-one allosteric modulators of the M4 muscarinic acetylcholine receptor
US10933056B2 (en) 2015-12-23 2021-03-02 Merck Sharp & Dohme Corp. 3-(1H-pyrazol-4-yl)pyridine allosteric modulators of the M4 muscarinic acetylcholine receptor
US10512638B2 (en) 2015-12-23 2019-12-24 Merck Sharp & Dohme Corp. 3-(1H-pyrazol-4-yl)pyridine allosteric modulators of the M4 muscarinic acetylcholine receptor
US10329289B2 (en) 2015-12-23 2019-06-25 Merck Sharp & Dohme Corp. 6,7-dihydro-5H-pyrrolo[3,4-B]pyridin-5-one allosteric modulators of the M4 muscarinic acetylcholine receptor
WO2018002760A1 (fr) 2016-07-01 2018-01-04 Pfizer Inc. Dérivés de 5,7-dihydro-pyrrolo-pyridine pour le traitement de maladies neurologiques et neurodégénératives
EP3872078A1 (fr) 2016-07-01 2021-09-01 Pfizer Inc. Dérivés de 5,7-dihydro-pyrrolo-pyridine destinés à être utilisés dans le traitement de la dépression, l'angoisse et les troubles paniques
CN109641898A (zh) * 2016-07-01 2019-04-16 辉瑞公司 用于治疗神经和神经退行性疾病的5,7-二氢-吡咯并-吡啶衍生物
US10342782B2 (en) 2016-07-27 2019-07-09 Vanderbilt University Positive allosteric modulators of the muscarinic acetylcholine receptor M4
WO2018035444A1 (fr) * 2016-08-18 2018-02-22 Vanderbilt University Modulateurs allostériques positifs du récepteur muscarinique de l'acétylcholine m4
US10189857B2 (en) 2016-09-13 2019-01-29 Vanderbilt University Positive allosteric modulators of the muscarinic acetylcholine receptor M4
US11319298B2 (en) 2016-12-22 2022-05-03 Merck Sharp & Dohme Corp. Heteroaryl piperidine ether allosteric modulators of the M4 muscarinic acetylcholine receptor
US10836775B2 (en) 2016-12-22 2020-11-17 Merck Sharp & Dohme Corp. 6,6-fused heteroaryl piperidine ether allosteric modulators of the M4 muscarinic acetylcholine receptor
WO2018211530A1 (fr) 2017-05-19 2018-11-22 Council Of Scientific & Industrial Research Méthanopyrido [2, 1-a] isoindolones substituées utilisées en tant que modulateurs de machr pour traiter diverses conditions pathophysiologiques associées et leur procédé de préparation
US11065235B2 (en) 2017-05-19 2021-07-20 Council Of Scientific & Industrial Research Substituted methanopyrido [2, 1-a] isoindolones as mAChR modulators for treating various associated pathophysiological conditions and process for preparation thereof
WO2018234953A1 (fr) 2017-06-22 2018-12-27 Pfizer Inc. Dérivés de dihydro-pyrrolo-pyridine
JP2020524687A (ja) * 2017-06-22 2020-08-20 ファイザー・インク ジヒドロ−ピロロ−ピリジン誘導体
CN110944998A (zh) * 2017-06-22 2020-03-31 辉瑞大药厂 二氢-吡咯并-吡啶衍生物
US11198692B2 (en) 2017-06-22 2021-12-14 Pfizer Inc. Dihydro-pyrrolo-pyridine derivatives
TWI680128B (zh) * 2017-06-22 2019-12-21 美商輝瑞股份有限公司 二氫吡咯並吡啶衍生物
JP7263266B2 (ja) 2017-06-22 2023-04-24 ファイザー・インク ジヒドロ－ピロロ－ピリジン誘導体
IL271290B1 (en) * 2017-06-22 2023-07-01 Pfizer Dihydro-pyrrolo-pyridine derivatives
EP3665175A4 (fr) * 2017-08-08 2020-12-09 Vanderbilt University Antagonistes du récepteur muscarinique de l'acétylcholine m4
US11225484B2 (en) 2017-08-08 2022-01-18 Vanderbilt University Substituted octahydropyrrolo[3,4-b]pyrroles as antagonists of the muscarinic acetylcholine receptor M4
WO2023114224A1 (fr) 2021-12-13 2023-06-22 Sage Therapeutics, Inc. Combinaison de modulateurs positifs du récepteur muscarinique et de modulateurs allostériques positifs de nmda

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