CA3079617A1 - Antagonists of the muscarinic acetylcholine receptor m4 - Google Patents

Antagonists of the muscarinic acetylcholine receptor m4 Download PDF

Info

Publication number
CA3079617A1
CA3079617A1 CA3079617A CA3079617A CA3079617A1 CA 3079617 A1 CA3079617 A1 CA 3079617A1 CA 3079617 A CA3079617 A CA 3079617A CA 3079617 A CA3079617 A CA 3079617A CA 3079617 A1 CA3079617 A1 CA 3079617A1
Authority
CA
Canada
Prior art keywords
hexahydro
cyclopenta
pyridazin
pyrrol
amine
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.)
Pending
Application number
CA3079617A
Other languages
English (en)
French (fr)
Inventor
Craig W. Lindsley
P. Jeffrey Conn
Darren W. Engers
Julie L. Engers
Kayla J. TEMPLE
Aaron M. Bender
Logan A. BAKER
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 CA3079617A1 publication Critical patent/CA3079617A1/en
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/10—Heterocyclic 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 carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • 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
    • C07D417/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Indole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CA3079617A 2017-10-20 2018-10-20 Antagonists of the muscarinic acetylcholine receptor m4 Pending CA3079617A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762574912P 2017-10-20 2017-10-20
US62/574,912 2017-10-20
PCT/US2018/056803 WO2019079783A1 (en) 2017-10-20 2018-10-20 ANTAGONISTS OF THE MUSCARINIC RECEPTOR OF ACETYLCHOLINE M4

Publications (1)

Publication Number Publication Date
CA3079617A1 true CA3079617A1 (en) 2019-04-25

Family

ID=66173904

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3079617A Pending CA3079617A1 (en) 2017-10-20 2018-10-20 Antagonists of the muscarinic acetylcholine receptor m4

Country Status (10)

Country Link
US (3) US11299481B2 (enExample)
EP (1) EP3697759B1 (enExample)
JP (1) JP7270989B2 (enExample)
KR (2) KR20250037575A (enExample)
CN (2) CN118063442A (enExample)
AU (2) AU2018351651B2 (enExample)
CA (1) CA3079617A1 (enExample)
ES (1) ES3064093T3 (enExample)
IL (2) IL273924B2 (enExample)
WO (1) WO2019079783A1 (enExample)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102218333B1 (ko) 2016-06-07 2021-02-22 자코바이오 파마슈티칼스 컴퍼니 리미티드 Shp2 억제제로서 유용한 신규한 헤테로환형 유도체
SG11201908820VA (en) 2017-03-23 2019-10-30 Jacobio Pharmaceuticals Co Ltd Novel heterocyclic derivatives useful as shp2 inhibitors
EP3651762B1 (en) 2017-07-12 2024-07-03 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
RU2764243C2 (ru) 2017-09-22 2022-01-14 ДЖУБИЛАНТ ЭПИПЭД ЭлЭлСи Гетероциклические соединения в качестве ингибиторов PAD
CN111225915B (zh) 2017-10-18 2023-03-07 朱比兰特埃皮帕德有限公司 作为pad抑制剂的咪唑并吡啶化合物
JP7270989B2 (ja) 2017-10-20 2023-05-11 ヴァンダービルト ユニバーシティー ムスカリン性アセチルコリン受容体m4のアンタゴニスト
ES2982890T3 (es) 2017-10-31 2024-10-18 Univ Vanderbilt Antagonistas del receptor muscarínico de acetilcolina M4
US11629135B2 (en) 2017-11-06 2023-04-18 Jubilant Prodell Llc Pyrimidine derivatives as inhibitors of PD1/PD-L1 activation
RS65576B1 (sr) 2017-11-24 2024-06-28 Jubilant Episcribe Llc Heterociklična jedinjenja kao inhibitori prmt5
WO2019126731A1 (en) 2017-12-22 2019-06-27 Petra Pharma Corporation Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors
CA3090130A1 (en) 2018-02-02 2019-08-08 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
CN112105610B (zh) 2018-03-13 2024-01-26 朱比连特普罗德尔有限责任公司 作为pd1/pd-l1相互作用/活化的抑制剂的双环化合物
CN112839935A (zh) 2018-09-26 2021-05-25 北京加科思新药研发有限公司 可用作shp2抑制剂的新型杂环衍生物
TW202112767A (zh) 2019-06-17 2021-04-01 美商佩特拉製藥公司 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物
US12319701B2 (en) 2019-10-04 2025-06-03 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor M4
WO2021119254A1 (en) * 2019-12-10 2021-06-17 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
AU2020402978A1 (en) * 2019-12-10 2022-06-23 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor M4
CA3169667A1 (en) * 2020-02-28 2021-09-02 Dominic Reynolds Pyridazine derivatives for modulating nucleic acid splicing
AR121715A1 (es) 2020-04-03 2022-06-29 Biocryst Pharm Inc Pirrolopirimidinaminas como inhibidores del sistema del complemento
CA3180717A1 (en) * 2020-04-24 2021-10-28 Vanderbilt University Condensed substituted hydropyrroles as antagonists of the muscarinic acetylcholine receptor m4
US20230183219A1 (en) * 2020-04-24 2023-06-15 Vanderbilt University Condensed substituted hydropyrroles as antagonists of the muscarinic acetylcholine receptor m4
EP4196473B1 (en) * 2020-08-13 2024-10-02 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
CA3199786A1 (en) * 2020-11-18 2022-05-27 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
CN116669737A (zh) * 2020-12-22 2023-08-29 范德堡大学 毒蕈碱型乙酰胆碱受体m4的拮抗剂
JP2024500880A (ja) * 2020-12-22 2024-01-10 ヴァンダービルト ユニヴァーシティ ムスカリン性アセチルコリン受容体m4のアンタゴニスト
TWI924832B (zh) * 2021-04-01 2026-05-11 日商小野藥品工業股份有限公司 Abhd6拮抗劑
US20240174655A1 (en) * 2021-04-02 2024-05-30 Vanderbilt University Indazole derivatives as antagonists of the muscarinic acetylcholine receptor m4
US20240228468A1 (en) * 2021-04-05 2024-07-11 Vanderbilt University N-(6-((octahydrocyclopenta[c]pyrrol-5-yi)amino)pyridazin-3-yl)phenyl)carboxamide and (6- ((octahydrocyclopenta[c]pyrrol-5-yl)amino)pyridazin-3-yl)benzamide derivatives as machr m4 antagonists for the treatment of neurodegenerative disorders
WO2022261427A1 (en) 2021-06-11 2022-12-15 Vanderbilt University (4-(6-((2-octahydrocyclopenta[c]pyrrol-5-yl)amino)pyridazin-3-yl)phenyl)(imino)(methyl)-lambda6- sulfanone derivatives and similar compounds as muscarinic acetylcholine receptor m4 antagonists for the treatment of neurodegenerative disorders
EP4104816A1 (en) * 2021-06-14 2022-12-21 Nucleus Medical GmbH Non-nanoparticulate applications forms of macrolides
IL310387A (en) * 2021-08-09 2024-03-01 Sironax Ltd Proptosis modulators, their preparation and uses
US20250101041A1 (en) * 2022-01-19 2025-03-27 Vanderbilt University Positive allosteric modulators of the muscarinic acetylcholine receptor m4
JP7852604B2 (ja) * 2022-09-30 2026-04-28 小野薬品工業株式会社 Abhd6アンタゴニストを含有する医薬組成物
WO2026034623A1 (ja) * 2024-08-09 2026-02-12 住友ファーマ株式会社 アミノメチルシクロヘキサン誘導体

Family Cites Families (101)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5221675A (en) 1989-12-15 1993-06-22 Abbott Laboratories Aza-spirocyclic compounds that enhance cholinergic neurotransmission
US5726172A (en) 1996-01-16 1998-03-10 Merck & Co., Inc. Tocolytic oxytocin receptor antagonists
KR20010072784A (ko) 1998-08-18 2001-07-31 지. 카파트 무스카린성 작용제 및 길항제
US6809105B2 (en) 2000-04-27 2004-10-26 Abbott Laboratories Diazabicyclic central nervous system active agents
US6995144B2 (en) 2002-03-14 2006-02-07 Eisai Co., Ltd. Nitrogen containing heterocyclic compounds and medicines containing the same
DE60324544D1 (de) 2002-04-26 2008-12-18 Schering Corp Muskarin antagonisten
EP1521747B1 (en) * 2002-07-15 2018-09-05 Symphony Evolution, Inc. Receptor-type kinase modulators and methods of use
US20040044029A1 (en) 2002-08-14 2004-03-04 Dart Michael J. Azabicyclic compounds are central nervous system active agents
AU2002347553A1 (en) 2002-12-23 2004-07-14 Ranbaxy Laboratories Limited Flavaxate derivatives as muscarinic receptor antagonists
EP1618091A1 (en) 2003-04-09 2006-01-25 Ranbaxy Laboratories, Ltd. Substituted azabicyclo hexane derivatives as muscarinic receptor antagonists
EP2210607B1 (en) * 2003-09-26 2011-08-17 Exelixis Inc. N-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide for the treatment of cancer
BRPI0510319A (pt) 2004-04-26 2007-10-16 Pfizer inibidores da enzima integrase de hiv
DE102004039789A1 (de) 2004-08-16 2006-03-02 Sanofi-Aventis Deutschland Gmbh Arylsubstituierte polycyclische Amine, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US20090176856A1 (en) 2004-09-27 2009-07-09 Anita Mehta Muscarinic receptor antagonists
WO2006035280A1 (en) 2004-09-27 2006-04-06 Ranbaxy Laboratories Limited 3,4-dihydroisoquinoline compounds as muscrinic receptor antagonists for the treatment of respiratory, urinary and gastrointestinal diseases
GB0510204D0 (en) 2005-05-19 2005-06-22 Chroma Therapeutics Ltd Enzyme inhibitors
EP1904495A2 (en) 2005-07-11 2008-04-02 Ranbaxy Laboratories Limited Muscarinic receptor antagonists
GB0521508D0 (en) 2005-10-21 2005-11-30 Novartis Ag Organic compounds
EA018128B1 (ru) 2006-01-23 2013-05-30 Амген Инк. Модуляторы аурора киназы, способы их получения и их применение
US7560551B2 (en) 2006-01-23 2009-07-14 Amgen Inc. Aurora kinase modulators and method of use
RU2008137583A (ru) 2006-02-22 2010-03-27 Вертекс Фармасьютикалз Инкорпорейшн (Us) Спиропиперидины в качестве модуляторов мускариновых рецепторов
EP2038289A2 (en) 2006-04-21 2009-03-25 Amgen Inc. Thieno-[2,3-d]pyrimidine and thieno-pyridazine compounds and methods of use
WO2007138431A2 (en) 2006-05-30 2007-12-06 Pfizer Products Inc. Azabicyclic ether histamine-3 antagonists
WO2008065500A2 (en) * 2006-11-30 2008-06-05 Pfizer Products Inc. Heteroaryl amides as type i glycine transport inhibitors
JP2010513458A (ja) 2006-12-19 2010-04-30 ファイザー・プロダクツ・インク H−pgdsの阻害剤としてのニコチンアミド誘導体、およびプロスタグランジンd2の仲介による疾患を治療するためのその使用
CN101230058A (zh) * 2007-01-23 2008-07-30 上海恒瑞医药有限公司 双环氮杂烷类衍生物、其制备方法及其在医药上的用途
MX2010005650A (es) 2007-11-21 2010-06-02 Abbott Lab Derivados de diazabicicloalcano substituidos con biarilo.
US8148408B2 (en) 2008-05-09 2012-04-03 Abbott Laboratories Selective substituted pyridine ligands for neuronal nicotinic receptors
WO2010067102A1 (en) 2008-12-09 2010-06-17 Astrazeneca Ab Diazaspiro [5.5] undecane derivatives and related compounds as muscarinic-receptor antagonists and beta-adrenoreceptor agonists for the treatment of pulmonary disorders
US9034891B2 (en) 2009-01-26 2015-05-19 Israel Institute For Biological Research Bicyclic heterocyclic spiro compounds
FR2945531A1 (fr) 2009-05-12 2010-11-19 Sanofi Aventis Derives de 7-aza-spiro°3,5!nonane-7-carboxylates, leur preparation et leur application en therapeutique
US8735409B2 (en) * 2009-12-21 2014-05-27 Qiang Zhang Quinazoline derivatives
WO2011149995A1 (en) 2010-05-25 2011-12-01 Abbott Laboratories Novel substituted octahydrocyclopenta [c]pyrrol-4-amines as calcium channel blockers
WO2012047703A2 (en) 2010-10-04 2012-04-12 Schering Corporation Cyclopropyl-spiro-piperidines useful as sodium channel blockers
JP2012107001A (ja) * 2010-10-22 2012-06-07 Shionogi & Co Ltd インドールアミド化合物を含有する医薬
WO2012154731A1 (en) 2011-05-08 2012-11-15 Vanderbilt University Substituted 1h-pyrrolo[3,2-c]quinolin-4(5h)-one analogs as positive allosteric modulators of the muscarinic acetylcholine receptor m4
US9073947B2 (en) 2011-06-10 2015-07-07 Merck Patent Gmbh Compositions and methods for the production of pyrimidine and pyridine compounds with BTK inhibitory activity
US9586964B2 (en) 2011-10-28 2017-03-07 Vanderbilt University Substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M1
CN103102352B (zh) * 2011-11-15 2015-08-12 山东亨利医药科技有限责任公司 酪氨酸激酶抑制剂吲哚满酮衍生物
JP6075736B2 (ja) 2011-12-21 2017-02-08 ジエンス ヘンルイ メデイシンカンパニー リミテッドJiangsu Hengrui Medicine Co.,Ltd. ピロール−6員ヘテロアリール環誘導体、その合成法およびその医薬用途
US8697888B2 (en) 2012-01-06 2014-04-15 Vanderbilt University Substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs as antagonists of muscarinic acetylcholine M1 receptors
HRP20170411T1 (hr) 2012-03-02 2017-06-16 Genentech, Inc. Amido spirocilični amidni i sulfonamidni derivati
US9056875B2 (en) 2012-08-31 2015-06-16 Vanderbilt University Substituted pyrazolo[3′,4′:4,5]thieno[2,3-C]pyridazin-3-amine analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4
WO2014035829A1 (en) 2012-08-31 2014-03-06 Vanderbilt University Substituted 3-aminothieno[2,3-c]pyridine-2-carboxamide analogs as positive allosteric modulators
EP2897948B1 (en) 2012-09-18 2016-08-31 Heptares Therapeutics Limited Bicyclic aza compounds as muscarinic m1 receptor agonists
JP6457942B2 (ja) 2012-10-05 2019-01-23 ライジェル ファーマシューティカルズ, インコーポレイテッド Gdf−8阻害剤
MX2015005375A (es) 2012-11-07 2015-07-21 Hoffmann La Roche Compuestos de triazolo.
WO2014093230A2 (en) 2012-12-10 2014-06-19 Merck Patent Gmbh Compositions and methods for the production of pyrimidine and pyridine compounds with btk inhibitory activity
TW201444820A (zh) 2013-03-13 2014-12-01 Abbvie Inc 吡啶cdk9激酶抑制劑
RU2693698C2 (ru) 2013-05-27 2019-07-04 Ф. Хоффманн-Ля Рош Аг Новые соединения 3,4-дигидро-2н-изохинолин-1-она и 2,3-дигидроизоиндол-1-она
WO2014191338A1 (en) 2013-05-27 2014-12-04 F. Hoffmann-La Roche Ag New 3,4-dihydro-2h-isoquinoline-1-one and 2,3-dihydro-isoindol-1-one compounds
WO2015027204A1 (en) 2013-08-23 2015-02-26 Vanderbilt University Substituted thieno[2,3-b]pyridine-2-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
WO2015058163A2 (en) 2013-10-18 2015-04-23 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
US10329270B2 (en) 2013-10-21 2019-06-25 Merck Patent Gmbh Heteroaryl compounds as BTK inhibitors and uses thereof
JP6383418B2 (ja) 2013-11-27 2018-08-29 ジェネンテック, インコーポレイテッド 置換ベンズアミド及びその使用方法
WO2015094803A1 (en) 2013-12-16 2015-06-25 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
US10059667B2 (en) * 2014-02-06 2018-08-28 Merck Sharp & Dohme Corp. Antidiabetic compounds
RU2685230C2 (ru) 2014-02-06 2019-04-17 Хептарес Терапьютикс Лимитед Бициклические азотсодержащие соединения как агонисты М1 мускариновых рецепторов
DK3119782T3 (en) 2014-03-17 2018-03-12 Remynd Nv Bio Incubator 2,7-diazaspiro [3.5] NONANFORBINDELSER
PL3536685T3 (pl) 2014-04-04 2022-05-16 Pfizer Inc. Bicykliczne skondensowane związki heteroarylowe lub arylowe i ich zastosowanie jako inhibitory IRAK4
HRP20210935T1 (hr) 2014-05-23 2021-08-06 F. Hoffmann - La Roche Ag Spojevi 5-kloro-2-difluorometoksifenil pirazolopirimidina koji predstavljaju inhibitore jak
JO3579B1 (ar) 2014-09-26 2020-07-05 Luc Therapeutics Inc مُعدِلات تفاغرية سالبة لمستقبل nr2b من المركب n-ألكيل أريل-5-أوكسي أريل-ثامن هيدرو-خماسي الحلقة [c] بيرول
GB201504675D0 (en) 2015-03-19 2015-05-06 Heptares Therapeutics Ltd Pharmaceutical compounds
US10124004B2 (en) 2015-05-29 2018-11-13 Teijin Pharma Limited Pyrido[3,4-d]pyrimidine derivative and pharmaceutically acceptable salt thereof
MD3316969T2 (ro) 2015-07-02 2022-07-31 Janssen Sciences Ireland Unlimited Co Compuși antibacterieni
EP3375781A4 (en) 2015-07-21 2019-01-09 Sichuan Haisco Pharmaceutical Co., Ltd. BENZORING DERIVATIVE WITH B2 RECEPTOR AGONIST AND M3 RECEPTOR ANTAGONIST ACTIVITIES AND USE THEREOF IN MEDICINE
GB201513743D0 (en) 2015-08-03 2015-09-16 Heptares Therapeutics Ltd Muscarinic agonists
GB201513742D0 (en) 2015-08-03 2015-09-16 Heptares Therapeutics Ltd Muscarinic agonists
GB201513740D0 (en) 2015-08-03 2015-09-16 Heptares Therapeutics Ltd Muscarinic agonist
GB201519352D0 (en) 2015-11-02 2015-12-16 Heptares Therapeutics Ltd Pharmaceutical compounds
JP6917989B2 (ja) 2015-11-06 2021-08-11 ニューロクライン バイオサイエンシーズ,インコーポレイテッド 神経学的疾患を処置するためのムスカリン受容体4(m4)アンタゴニストとしての、n−[2−(1−ベンジルピペリジン−4−イル)エチル]−4−(ピラジン−2−イル)−ピペラジン−1−カルボキサミド誘導体および関連化合物
RU2746188C2 (ru) 2015-11-12 2021-04-08 Афаски, Инк. Ингибиторы ионного канала, фармацевтические составы и применение
BR112018016689A2 (pt) 2016-02-16 2019-02-12 Univ Vanderbilt moduladores alostéricos positivos do receptor muscarínico de acetilcolina m1
AR108326A1 (es) 2016-04-27 2018-08-08 Samumed Llc Isoquinolin-3-il carboxamidas y preparación y uso de las mismas
US20170355708A1 (en) 2016-06-09 2017-12-14 Cadent Therapeutics, Inc. Potassium channel modulators
KR102474326B1 (ko) 2016-06-22 2022-12-05 반더빌트유니버시티 무스카린성 아세틸콜린 수용체 m4의 양성 알로스테릭 조절제
PL3507289T3 (pl) 2016-09-02 2021-01-25 Suven Life Sciences Limited Dodatnie allosteryczne modulatory receptora muskarynowego m1
US10968210B2 (en) * 2016-11-17 2021-04-06 Merck Sharp & Dohme Corp. Diamino-alkylamino-linked arylsulfonamide compounds with selective activity in voltage-gated sodium channels
WO2018226150A1 (en) 2017-06-05 2018-12-13 Medivir Aktiebolag Pyrazolopyrimidine as malt-1 inhibitors
EP3651762B1 (en) 2017-07-12 2024-07-03 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
AU2018313802A1 (en) 2017-08-08 2020-02-20 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor M4
WO2019079410A1 (en) 2017-10-17 2019-04-25 Vanderbilt University ANTAGONISTS OF THE MUSCARINIC RECEPTOR OF ACETYLCHOLINE M4
JP7270989B2 (ja) 2017-10-20 2023-05-11 ヴァンダービルト ユニバーシティー ムスカリン性アセチルコリン受容体m4のアンタゴニスト
ES2982890T3 (es) * 2017-10-31 2024-10-18 Univ Vanderbilt Antagonistas del receptor muscarínico de acetilcolina M4
EP3732163A4 (en) 2017-12-20 2021-07-14 Vanderbilt University MUSCARIN M4 ACETYLCHOLIN RECEPTOR ANTAGONISTS
CA3090130A1 (en) 2018-02-02 2019-08-08 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
EP3810615B1 (en) 2018-06-20 2026-01-28 Merck Sharp & Dohme LLC Arginase inhibitors and methods of use
TWI767148B (zh) 2018-10-10 2022-06-11 美商弗瑪治療公司 抑制脂肪酸合成酶(fasn)
US12319701B2 (en) 2019-10-04 2025-06-03 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor M4
AU2020402978A1 (en) * 2019-12-10 2022-06-23 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor M4
WO2021119254A1 (en) 2019-12-10 2021-06-17 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
CA3180717A1 (en) * 2020-04-24 2021-10-28 Vanderbilt University Condensed substituted hydropyrroles as antagonists of the muscarinic acetylcholine receptor m4
US20230183219A1 (en) * 2020-04-24 2023-06-15 Vanderbilt University Condensed substituted hydropyrroles as antagonists of the muscarinic acetylcholine receptor m4
EP4196473B1 (en) 2020-08-13 2024-10-02 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
CA3199786A1 (en) 2020-11-18 2022-05-27 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
JP2024500880A (ja) 2020-12-22 2024-01-10 ヴァンダービルト ユニヴァーシティ ムスカリン性アセチルコリン受容体m4のアンタゴニスト
CN116669737A (zh) 2020-12-22 2023-08-29 范德堡大学 毒蕈碱型乙酰胆碱受体m4的拮抗剂
US20240174655A1 (en) * 2021-04-02 2024-05-30 Vanderbilt University Indazole derivatives as antagonists of the muscarinic acetylcholine receptor m4
US20240228468A1 (en) * 2021-04-05 2024-07-11 Vanderbilt University N-(6-((octahydrocyclopenta[c]pyrrol-5-yi)amino)pyridazin-3-yl)phenyl)carboxamide and (6- ((octahydrocyclopenta[c]pyrrol-5-yl)amino)pyridazin-3-yl)benzamide derivatives as machr m4 antagonists for the treatment of neurodegenerative disorders
WO2022261427A1 (en) 2021-06-11 2022-12-15 Vanderbilt University (4-(6-((2-octahydrocyclopenta[c]pyrrol-5-yl)amino)pyridazin-3-yl)phenyl)(imino)(methyl)-lambda6- sulfanone derivatives and similar compounds as muscarinic acetylcholine receptor m4 antagonists for the treatment of neurodegenerative disorders

Also Published As

Publication number Publication date
EP3697759A4 (en) 2021-05-12
IL273924B1 (en) 2024-03-01
US20240116902A1 (en) 2024-04-11
KR102776114B1 (ko) 2025-03-07
EP3697759B1 (en) 2025-12-31
CN111491920B (zh) 2024-01-30
US11299481B2 (en) 2022-04-12
IL273924B2 (en) 2024-07-01
KR20250037575A (ko) 2025-03-17
US20220213069A1 (en) 2022-07-07
WO2019079783A1 (en) 2019-04-25
JP7270989B2 (ja) 2023-05-11
IL273924A (en) 2020-05-31
AU2023202086A1 (en) 2023-05-04
CN118063442A (zh) 2024-05-24
CN111491920A (zh) 2020-08-04
AU2018351651B2 (en) 2023-01-05
ES3064093T3 (en) 2026-04-22
KR20200074164A (ko) 2020-06-24
US20210188820A1 (en) 2021-06-24
US11820757B2 (en) 2023-11-21
AU2018351651A1 (en) 2020-06-04
IL310346A (en) 2024-03-01
AU2023202086B2 (en) 2025-04-03
JP2021500345A (ja) 2021-01-07
US12577234B2 (en) 2026-03-17
EP3697759A1 (en) 2020-08-26

Similar Documents

Publication Publication Date Title
AU2023202086B2 (en) Antagonists of the muscarinic acetylcholine receptor M4
EP3651762B1 (en) Antagonists of the muscarinic acetylcholine receptor m4
EP4037677B1 (en) Antagonists of the muscarinic acetylcholine receptor m4
US20230122344A1 (en) Antagonists of the muscarinic acetylcholine receptor m4
EP3732163A1 (en) Antagonists of the muscarinic acetylcholine receptor m4
CA3081324A1 (en) Antagonists of the muscarinic acetylcholine receptor m4
CA3180803A1 (en) Condensed substituted hydropyrroles as antagonists of the muscarinic acetylcholine receptor m4
EP4196473B1 (en) Antagonists of the muscarinic acetylcholine receptor m4
EP3665175A1 (en) Antagonists of the muscarinic acetylcholine receptor m4
EP4247803A1 (en) Antagonists of the muscarinic acetylcholine receptor m4
WO2022261427A1 (en) (4-(6-((2-octahydrocyclopenta[c]pyrrol-5-yl)amino)pyridazin-3-yl)phenyl)(imino)(methyl)-lambda6- sulfanone derivatives and similar compounds as muscarinic acetylcholine receptor m4 antagonists for the treatment of neurodegenerative disorders

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20231020

MFA Maintenance fee for application paid

Free format text: FEE DESCRIPTION TEXT: MF (APPLICATION, 6TH ANNIV.) - STANDARD

Year of fee payment: 6

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20241011

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT DETERMINED COMPLIANT

Effective date: 20241011

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL

Effective date: 20241011

D15 Examination report completed

Free format text: ST27 STATUS EVENT CODE: A-2-2-D10-D15-D126 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: EXAMINER'S REPORT

Effective date: 20241115

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-P100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT RECEIVED - RESPONSE TO EXAMINER'S REQUISITION

Effective date: 20250312

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-2-2-W10-W00-W111 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CORRESPONDENT DETERMINED COMPLIANT

Effective date: 20250313

MFA Maintenance fee for application paid

Free format text: FEE DESCRIPTION TEXT: MF (APPLICATION, 7TH ANNIV.) - STANDARD

Year of fee payment: 7

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20250826

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL

Effective date: 20250826

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-P102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT DETERMINED COMPLIANT

Effective date: 20251006

P13 Application amended

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P13-X000 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: APPLICATION AMENDED

Effective date: 20251006

D00 Search and/or examination requested or commenced

Free format text: ST27 STATUS EVENT CODE: A-2-2-D10-D00-D149 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: EXAMINER'S INTERVIEW

Effective date: 20251127

D00 Search and/or examination requested or commenced

Free format text: ST27 STATUS EVENT CODE: A-2-2-D10-D00-D136 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: INTERVIEW REQUEST AUTHORIZED

Effective date: 20251216

Free format text: ST27 STATUS EVENT CODE: A-2-2-D10-D00-D138 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: INTERVIEW PERFORMED

Effective date: 20251216

Free format text: ST27 STATUS EVENT CODE: A-2-2-D10-D00-D135 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: INTERVIEW REQUEST RECEIVED

Effective date: 20251216

D15 Examination report completed

Free format text: ST27 STATUS EVENT CODE: A-2-2-D10-D15-D126 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: EXAMINER'S REPORT

Effective date: 20251224

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-P100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT RECEIVED - RESPONSE TO EXAMINER'S REQUISITION

Effective date: 20260421

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-2-2-W10-W00-W111 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CORRESPONDENT DETERMINED COMPLIANT

Effective date: 20260604

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-P102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT DETERMINED COMPLIANT

Effective date: 20260609

P13 Application amended

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P13-X000 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: APPLICATION AMENDED

Effective date: 20260609