CN106536508B - 用于治疗阿尔茨海默病的具有胆碱能毒蕈碱m1受体正变构调节剂活性的化合物 - Google Patents

用于治疗阿尔茨海默病的具有胆碱能毒蕈碱m1受体正变构调节剂活性的化合物 Download PDF

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CN106536508B
CN106536508B CN201580034130.XA CN201580034130A CN106536508B CN 106536508 B CN106536508 B CN 106536508B CN 201580034130 A CN201580034130 A CN 201580034130A CN 106536508 B CN106536508 B CN 106536508B
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CN106536508A (zh
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山田昌美
铃木新吉
杉本贵裕
中村实
坂本博辉
鎌田信
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Takeda Pharmaceutical Co Ltd
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CN201580034130.XA 2014-04-23 2015-04-22 用于治疗阿尔茨海默病的具有胆碱能毒蕈碱m1受体正变构调节剂活性的化合物 Active CN106536508B (zh)

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JP2014-089585 2014-04-23
JP2014089585 2014-04-23
PCT/JP2015/062912 WO2015163485A1 (en) 2014-04-23 2015-04-22 Isoindoline-1-one derivatives as cholinergic muscarinic m1 receptor positive alloesteric modulator activity for the treatment of alzheimers disease

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CN106536508B true CN106536508B (zh) 2019-08-09

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Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11201506924YA (en) 2013-03-15 2015-09-29 Incyte Corp Tricyclic heterocycles as bet protein inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
UA119870C2 (uk) 2014-04-23 2019-08-27 Інсайт Корпорейшн 1H-ПІРОЛО[2,3-c]ПІРИДИН-7(6H)-ОНИ ТА ПІРАЗОЛО[3,4-c]ПІРИДИН-7(6H)-ОНИ ЯК ІНГІБІТОРИ БІЛКІВ BET
CN106536508B (zh) 2014-04-23 2019-08-09 武田药品工业株式会社 用于治疗阿尔茨海默病的具有胆碱能毒蕈碱m1受体正变构调节剂活性的化合物
JP6531093B2 (ja) 2014-05-16 2019-06-12 武田薬品工業株式会社 含窒素複素環化合物
WO2015190564A1 (ja) 2014-06-13 2015-12-17 武田薬品工業株式会社 含窒素複素環化合物
US9527864B2 (en) 2014-09-15 2016-12-27 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
CR20170568A (es) 2015-06-26 2018-04-20 Takeda Pharmaceuticals Co Compuesto heterocíclico
JP6787913B2 (ja) 2015-10-20 2020-11-18 武田薬品工業株式会社 複素環化合物
TW201722966A (zh) 2015-10-29 2017-07-01 英塞特公司 Bet蛋白質抑制劑之非晶固體形式
WO2017107089A1 (en) 2015-12-23 2017-06-29 Merck Sharp & Dohme Corp. 3- (1h-pyrazol-4-yl) pyridineallosteric modulators of the m4 muscarinic acetylcholine receptor
EP3428150B1 (en) 2016-03-11 2023-07-12 Takeda Pharmaceutical Company Limited Aromatic ring compound having a cholinergic muscarine m1 receptor positive allosteric modulator activity
IL263824B2 (en) 2016-06-20 2023-10-01 Incyte Corp Crystals in solid form in the presence of an inhibitor
WO2018005249A1 (en) * 2016-06-28 2018-01-04 Merck Sharp & Dohme Corp. Benzoisoquinolinone m1 receptor positive allosteric modulators
US10710989B2 (en) 2017-02-28 2020-07-14 Takeda Pharmaceutical Company Limited Method for producing heterocyclic compound
JP7145875B2 (ja) 2017-04-18 2022-10-03 武田薬品工業株式会社 アセチルコリン受容体のモジュレーターとして有用な複素環化合物
EP3627152A4 (en) * 2017-05-19 2021-02-24 Takeda Pharmaceutical Company Limited Screening method
WO2018226545A1 (en) 2017-06-09 2018-12-13 Merck Sharp & Dohme Corp. Azabicyclo[4.1.0]heptane allosteric modulators of the m4 muscarinic acetylcholine receptor
JP7123042B2 (ja) 2017-06-20 2022-08-22 武田薬品工業株式会社 複素環化合物
HRP20231236T1 (hr) 2017-06-20 2024-02-16 Takeda Pharmaceutical Company Limited Heterociklički spoj i njegova uporaba kao pozitivnog alosteričnog modulatora kolinergičkog muskarinskog m1 receptora
WO2019000236A1 (en) 2017-06-27 2019-01-03 Merck Sharp & Dohme Corp. ALLOSTERIC MODULATORS OF 3- (1H-PYRAZOL-4-YL) PYRIDINE FROM THE M4 ACETYLCHOLINE MUSCARINIC RECEPTOR
WO2019000238A1 (en) * 2017-06-27 2019-01-03 Merck Sharp & Dohme Corp. 5- (PYRIDIN-3-YL) OXAZOLE ALLOSTERIC MODULATORS OF M4 ACETYLCHOLINE MUSCARINIC RECEPTOR
WO2019000237A1 (en) 2017-06-27 2019-01-03 Merck Sharp & Dohme Corp. ALLOSTERIC MODULATORS OF 3- (1H-PYRAZOL-4-YL) PYRIDINE FROM THE M4 ACETYLCHOLINE MUSCARINIC RECEPTOR
JP2020158392A (ja) * 2017-07-25 2020-10-01 Agc株式会社 フルオロフェノール誘導体の製造方法及び新規なフルオロ化合物
BR112020010138A2 (pt) * 2017-11-23 2020-11-10 Suven Life Sciences Limited azaciclos substituídos como moduladores alostéricos positivos do receptor muscarínico m1
WO2020067457A1 (ja) 2018-09-28 2020-04-02 武田薬品工業株式会社 縮合環化合物
BR112021005759A2 (pt) 2018-09-28 2021-07-06 Takeda Pharmaceuticals Co composto, medicamento, métodos de modulação alostérica positiva e para a profilaxia ou o tratamento de constipação, e, uso do composto ou de um sal do mesmo
US11970483B2 (en) 2018-09-28 2024-04-30 Takeda Pharmaceutical Company Limited Heterocyclic compound
WO2020139372A1 (en) * 2018-12-28 2020-07-02 Shui Yin Lo Method for detection treatment and prevention of neurological development disorders
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
IL300172A (en) * 2020-07-29 2023-03-01 Vivozon Inc A dual regulator for MGLUR5 and 5-HT2A receptors and its use
EP4447953A1 (en) 2021-12-13 2024-10-23 Sage Therapeutics, Inc. Combination of muscarinic receptor positive modulators and nmda positive allosteric modulators
WO2025231255A1 (en) * 2024-05-01 2025-11-06 Vanderbilt University Positive allosteric modulators of the muscarinic acetylcholine receptor m1

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003011858A1 (de) * 2001-07-30 2003-02-13 Bayer Healthcare Ag Substituierte isoindole und ihre verwendung
CN101039907A (zh) * 2004-08-13 2007-09-19 阿斯利康(瑞典)有限公司 异吲哚酮化合物及其作为代谢性谷氨酸受体增效剂的用途
WO2012003147A1 (en) * 2010-07-01 2012-01-05 Merck Sharp & Dohme Corp. Isoindolone m1 receptor positive allosteric modulators
CN102762548A (zh) * 2009-12-22 2012-10-31 沃泰克斯药物股份有限公司 磷脂酰肌醇3-激酶的异吲哚啉酮抑制剂

Family Cites Families (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS4416647Y1 (OSRAM) 1965-05-26 1969-07-18
JPS60172704A (ja) 1984-02-14 1985-09-06 Mitsuwa Seiki Co Ltd 流体アクチユエ−タの制御方法
JP2699511B2 (ja) 1988-01-29 1998-01-19 武田薬品工業株式会社 置換アミン類
US5538983A (en) 1990-05-16 1996-07-23 The Rockefeller University Method of treating amyloidosis by modulation of calcium
JPH06220044A (ja) * 1991-12-25 1994-08-09 Mitsubishi Kasei Corp ベンズアミド誘導体
TW219935B (OSRAM) 1991-12-25 1994-02-01 Mitsubishi Chemicals Co Ltd
GB9409150D0 (en) 1994-05-09 1994-06-29 Black James Foundation Cck and gastrin receptor ligands
US5744476A (en) 1994-06-27 1998-04-28 Interneuron Pharmaceuticals, Inc. Dopamine D1 agonists for the treatment of dementia
JP2992677B2 (ja) 1995-06-05 1999-12-20 武田薬品工業株式会社 骨形成促進医薬組成物
AU5716898A (en) 1997-01-08 1998-08-03 Warner-Lambert Company Acetylcholinesterase inhibitors in combination with muscarinic agonists for the treatment of alzheimer's disease
US7084126B1 (en) 2000-05-01 2006-08-01 Healthpartners Research Foundation Methods and compositions for enhancing cellular function through protection of tissue components
WO2002003684A2 (en) 2000-06-30 2002-01-10 Eli Lilly And Company Combination for treating psychoses, comprising an antipsychotic and a muscarinic agonist
AU2002245692A1 (en) 2001-03-15 2002-10-03 David Pharmaceuticals Methods for restoring cognitive function following systemic stress
WO2002081446A1 (en) 2001-04-06 2002-10-17 Daewoong Co., Ltd. 3-cyclopentyloxy-4-methoxyphenyl-isoindolinone derivatives and the use thereof
WO2002081447A1 (en) 2001-04-06 2002-10-17 Daewoong Pharmaceutical Co., Ltd. 3-cyclopentyloxy-4-methoxyphenyl-isothiazolinone derivatives and the use thereof
US20040023951A1 (en) 2001-06-18 2004-02-05 Bymaster Franklin Porter Combination therapy for treatment of psychoses
US20040044023A1 (en) 2002-08-30 2004-03-04 Marc Cantillon Compositions and methods for treating or preventing memory impairment
WO2004073639A2 (en) 2003-02-19 2004-09-02 Merck & Co. Inc. Treatment of psychosis with a muscarinic m1 receptor ectopic activator
CA2520125A1 (en) 2003-03-28 2004-10-14 Acadia Pharmaceuticals Inc. Muscarinic m1 receptor agonists for pain management
US20040266659A1 (en) 2003-06-27 2004-12-30 Stephen LaBerge Substances that enhance recall and lucidity during dreaming
EP1885708A2 (en) 2005-04-15 2008-02-13 Board of Trustees of Michigan State University Gpcr modulators
US7868008B2 (en) 2005-08-12 2011-01-11 Astrazeneca Ab Substituted isoindolones and their use as metabotropic glutamate receptor potentiators
US7807706B2 (en) 2005-08-12 2010-10-05 Astrazeneca Ab Metabotropic glutamate-receptor-potentiating isoindolones
US20110319386A1 (en) 2005-08-26 2011-12-29 Braincells Inc. Neurogenesis by muscarinic receptor modulation
US7678363B2 (en) 2005-08-26 2010-03-16 Braincells Inc Methods of treating psychiatric conditions comprising administration of muscarinic agents in combination with SSRIs
WO2007044937A2 (en) 2005-10-13 2007-04-19 President And Fellows Of Harvard College Compositions and methods to modulate memory
GB0607946D0 (en) 2006-04-21 2006-05-31 Minster Res The Ltd Mono and combination therapy
GB0607952D0 (en) 2006-04-21 2006-05-31 Minster Res Ltd Novel treatment
GB0607949D0 (en) 2006-04-21 2006-05-31 Minster Res The Ltd Mono and combination therapy
TW200806625A (en) 2006-05-26 2008-02-01 Astrazeneca Ab Therapeutic compounds
US8143284B2 (en) 2006-10-05 2012-03-27 Abbott Laboratories Poly(ADP-ribose)polymerase inhibitors
WO2008113072A2 (en) 2007-03-15 2008-09-18 Board Of Regents, The University Of Texas System Gpcr enhanced neuroprotection to treat brain injury
NO2200610T3 (OSRAM) 2007-09-21 2018-06-09
US20090082342A1 (en) 2007-09-21 2009-03-26 Acadia Pharmaceuticals, Inc. N-substituted piperidine derivatives as serotonin receptor agents
WO2009039635A1 (en) * 2007-09-24 2009-04-02 Painceptor Pharma Corporation Methods of modulating neurotrophin-mediated activity
WO2009042907A1 (en) * 2007-09-27 2009-04-02 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Isoindoline compounds for the treatment of spinal muscular atrophy and other uses
WO2010042603A1 (en) 2008-10-08 2010-04-15 Cingulate Neuro Therapeutics, Llc Amyloid and depression
US8486946B2 (en) 2009-02-23 2013-07-16 Merck Sharp & Dohme Corp. Pyrazolo [4,3-c] cinnolin-3-one M1 receptor positive allosteric modulators
JP2012519704A (ja) 2009-03-05 2012-08-30 ミスリィディオン,インク. 認知増強用化合物及び組成物、製造法、並びに治療法
EP2454236B1 (en) 2009-07-14 2019-09-04 Nerviano Medical Sciences S.r.l. 3-oxo-2,3-dihydro-1h-isoindole-4-carboxamides as parp inhibitors
US10265311B2 (en) 2009-07-22 2019-04-23 PureTech Health LLC Methods and compositions for treatment of disorders ameliorated by muscarinic receptor activation
DK3061821T3 (da) 2009-07-22 2019-08-26 PureTech Health LLC Sammensætninger til behandling af forstyrrelser lindret af muskarinreceptoraktivering
US8314120B2 (en) * 2010-03-30 2012-11-20 Abbott Gmbh & Co. Kg Small molecule potentiators of metabotropic glutamate receptors
WO2012149524A1 (en) 2011-04-29 2012-11-01 The University Of Toledo Muscarinic agonists as enhancers of working memory and cognitive flexibility
WO2012158475A1 (en) 2011-05-17 2012-11-22 Merck Sharp & Dohme Corp. N-linked lactam m1 receptor positive allosteric modulators
WO2012170599A1 (en) 2011-06-10 2012-12-13 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
DK2770997T3 (en) * 2011-10-28 2016-12-19 Univ Vanderbilt SUBSTITUTED 2- (4-HETEROCYCLYLBENSYL) isoindolin-1-ON-ANALOGS AS POSITIVE allosteric modulators OF THE muscarinic acetylcholine receptor M1
WO2013129622A1 (ja) 2012-03-02 2013-09-06 武田薬品工業株式会社 複素環化合物およびその用途
US20130289019A1 (en) 2012-04-26 2013-10-31 Amazing Grace, Inc. Methods of treating behaviorial and/or mental disorders
JP6211530B2 (ja) 2012-11-19 2017-10-11 武田薬品工業株式会社 含窒素複素環化合物
TW201512197A (zh) 2013-08-30 2015-04-01 Hoffmann La Roche 吡咯并吡啶或吡唑并吡啶衍生物
MX2016001942A (es) 2013-09-27 2016-06-02 Hoffmann La Roche Derivados de indol e indazol.
GB201317363D0 (en) 2013-10-01 2013-11-13 Eisai Ltd Novel compounds
CN106536508B (zh) * 2014-04-23 2019-08-09 武田药品工业株式会社 用于治疗阿尔茨海默病的具有胆碱能毒蕈碱m1受体正变构调节剂活性的化合物
US20180250270A1 (en) 2015-09-11 2018-09-06 Chase Pharmaceuticals Corporation Muscarinic combination and its use for combating hypocholinergic disorders of the central nervous system
EP3562477A4 (en) 2016-12-29 2020-11-18 Synnerva Ltd. PROCEDURES AND COMPOSITIONS FOR POTENTIATING CNS DRUGS AND REDUCING THEIR SIDE EFFECTS

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003011858A1 (de) * 2001-07-30 2003-02-13 Bayer Healthcare Ag Substituierte isoindole und ihre verwendung
CN101039907A (zh) * 2004-08-13 2007-09-19 阿斯利康(瑞典)有限公司 异吲哚酮化合物及其作为代谢性谷氨酸受体增效剂的用途
CN102762548A (zh) * 2009-12-22 2012-10-31 沃泰克斯药物股份有限公司 磷脂酰肌醇3-激酶的异吲哚啉酮抑制剂
WO2012003147A1 (en) * 2010-07-01 2012-01-05 Merck Sharp & Dohme Corp. Isoindolone m1 receptor positive allosteric modulators

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