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

Info

Publication number
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
Authority
CN
China
Prior art keywords
methyl
alkyl
optionally substituted
group
compound
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.)
Active
Application number
CN201580034130.XA
Other languages
English (en)
Chinese (zh)
Other versions
CN106536508A (zh
Inventor
山田昌美
铃木新吉
杉本贵裕
中村实
坂本博辉
鎌田信
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.)
Takeda Pharmaceutical Co Ltd
Original Assignee
Takeda Chemical Industries Ltd
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=53276227&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN106536508(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Takeda Chemical Industries Ltd filed Critical Takeda Chemical Industries Ltd
Publication of CN106536508A publication Critical patent/CN106536508A/zh
Application granted granted Critical
Publication of CN106536508B publication Critical patent/CN106536508B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/325Carbamic acids; Thiocarbamic acids; Anhydrides or salts thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035Isoindoles, e.g. phthalimide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4406Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44Iso-indoles; Hydrogenated iso-indoles
    • C07D209/46Iso-indoles; Hydrogenated iso-indoles with an oxygen atom in position 1
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/10Heterocyclic 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 aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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 two hetero rings
    • C07D405/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
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)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2014089585 2014-04-23
JP2014-089585 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

Publications (2)

Publication Number Publication Date
CN106536508A CN106536508A (zh) 2017-03-22
CN106536508B true CN106536508B (zh) 2019-08-09

Family

ID=53276227

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201580034130.XA Active CN106536508B (zh) 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

Country Status (36)

Country Link
US (16) US9315458B2 (OSRAM)
EP (1) EP3134386B1 (OSRAM)
JP (1) JP6517239B2 (OSRAM)
KR (1) KR102349237B1 (OSRAM)
CN (1) CN106536508B (OSRAM)
AR (1) AR100154A1 (OSRAM)
AU (1) AU2015250610B2 (OSRAM)
BR (1) BR112016024472B1 (OSRAM)
CA (1) CA2946519C (OSRAM)
CL (1) CL2016002661A1 (OSRAM)
CR (1) CR20160544A (OSRAM)
CY (1) CY1123569T1 (OSRAM)
DK (1) DK3134386T3 (OSRAM)
DO (1) DOP2016000286A (OSRAM)
EA (1) EA030373B1 (OSRAM)
EC (1) ECSP16090152A (OSRAM)
ES (1) ES2811088T3 (OSRAM)
HR (1) HRP20201171T1 (OSRAM)
HU (1) HUE050543T2 (OSRAM)
IL (1) IL248393B (OSRAM)
LT (1) LT3134386T (OSRAM)
MX (1) MX373274B (OSRAM)
MY (1) MY195742A (OSRAM)
NZ (1) NZ725921A (OSRAM)
PE (1) PE20161400A1 (OSRAM)
PH (1) PH12016502095B1 (OSRAM)
PL (1) PL3134386T3 (OSRAM)
PT (1) PT3134386T (OSRAM)
RS (1) RS60524B1 (OSRAM)
SG (1) SG11201608785PA (OSRAM)
SI (1) SI3134386T1 (OSRAM)
TN (1) TN2016000455A1 (OSRAM)
TW (1) TWI664165B (OSRAM)
UA (1) UA122391C2 (OSRAM)
UY (1) UY36091A (OSRAM)
WO (1) WO2015163485A1 (OSRAM)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2909778T3 (es) 2013-03-15 2022-05-10 Incyte Holdings Corp Heterociclos tricíclicos como inhibidores de proteína BET para su uso en el tratamiento de una enfermedad proliferativa en combinación con un inhibidor de Janus quinasas
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
WO2015163485A1 (en) 2014-04-23 2015-10-29 Takeda Pharmaceutical Company Limited Isoindoline-1-one derivatives as cholinergic muscarinic m1 receptor positive alloesteric modulator activity for the treatment of alzheimers disease
SG10201809353TA (en) 2014-04-23 2018-11-29 Incyte Corp 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS
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
JP6571077B2 (ja) 2014-06-13 2019-09-04 武田薬品工業株式会社 含窒素複素環化合物
WO2016044130A1 (en) 2014-09-15 2016-03-24 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
KR20180019234A (ko) 2015-06-26 2018-02-23 다케다 야쿠힌 고교 가부시키가이샤 콜린성 무스카린 m1 수용체의 조절제로서의 2,3-디히드로-4h-1,3-벤족사진-4-온 유도체
US10548899B2 (en) 2015-10-20 2020-02-04 Takeda Pharmaceutical Company Limited Quinazolinone and benzotriazinone compounds with cholinergic muscarinin M1 receptor positive allosteric modulator activity
AR106520A1 (es) 2015-10-29 2018-01-24 Incyte Corp Forma sólida amorfa de un inhibidor de proteína bet
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
TWI830533B (zh) 2016-06-20 2024-01-21 美商英塞特公司 Bet抑制劑之結晶固體形式
WO2018005249A1 (en) * 2016-06-28 2018-01-04 Merck Sharp & Dohme Corp. Benzoisoquinolinone m1 receptor positive allosteric modulators
CA3054773A1 (en) 2017-02-28 2018-09-07 Takeda Pharmaceutical Company Limited Method for producing heterocyclic compound
EP3612527B1 (en) 2017-04-18 2022-07-20 Takeda Pharmaceutical Company Limited Heterocyclic compounds useful as modulators of acetylcholine receptors
US12298319B2 (en) 2017-05-19 2025-05-13 Takeda Pharmaceutical Company Limited Method for measuring alpha value of muscarinic M1 receptor positive allosteric modulators
US10945771B2 (en) 2017-06-09 2021-03-16 Merck Sharp & Dohme Corp. Azabicyclo[4.1.0]heptane allosteric modulators of the M4 muscarinic acetylcholine receptor
EP3643718B1 (en) 2017-06-20 2023-07-26 Takeda Pharmaceutical Company Limited Heterocyclic compound and its use as positive allosteric modulator of the cholinergic muscarinic m1 receptor.
HUE063823T2 (hu) 2017-06-20 2024-02-28 Heterociklusos vegyület és annak alkalmazása a kolinerg muszkarin M1 receptor pozitív alloszterikus modulátoraként
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
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
WO2019000238A1 (en) * 2017-06-27 2019-01-03 Merck Sharp & Dohme Corp. 5- (PYRIDIN-3-YL) OXAZOLE ALLOSTERIC MODULATORS OF 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
JP7034284B2 (ja) * 2017-11-23 2022-03-11 スヴェン・ライフ・サイエンシーズ・リミテッド ムスカリン性m1受容体ポジティブアロステリックモジュレーターとしての置換アザ環
AU2019351469B2 (en) 2018-09-28 2024-10-03 Takeda Pharmaceutical Company Limited Heterocyclic compound
EP3858823A4 (en) 2018-09-28 2022-07-06 Takeda Pharmaceutical Company Limited Condensed-cyclic compound
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
WO2022025636A1 (ko) * 2020-07-29 2022-02-03 주식회사 비보존 Mglur5 및 5-ht2a 수용체의 이중 조절제 및 이의 용도
WO2023114224A1 (en) 2021-12-13 2023-06-22 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
EP1316203A2 (en) 2000-06-30 2003-06-04 Eli Lilly And Company Combination for treating psychoses, comprising an antipsychotic and a muscarinic agonist
CA2442717A1 (en) 2001-03-15 2002-09-26 Saegis Pharmaceuticals, Inc. Methods for restoring cognitive function following systemic stress
WO2002081447A1 (en) 2001-04-06 2002-10-17 Daewoong Pharmaceutical Co., Ltd. 3-cyclopentyloxy-4-methoxyphenyl-isothiazolinone derivatives and the use thereof
WO2002081446A1 (en) 2001-04-06 2002-10-17 Daewoong Co., Ltd. 3-cyclopentyloxy-4-methoxyphenyl-isoindolinone 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
US20060233843A1 (en) 2003-02-19 2006-10-19 Conn P J Treatment of psychosis with a muscarinic m1 receptor ectopic activator
BRPI0409523A (pt) 2003-03-28 2006-04-18 Acadia Pharm Inc método para o tratamento da dor neuropática, método de identificação de um composto e composição farmacêutica
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
US7807706B2 (en) 2005-08-12 2010-10-05 Astrazeneca Ab Metabotropic glutamate-receptor-potentiating isoindolones
US7868008B2 (en) 2005-08-12 2011-01-11 Astrazeneca Ab Substituted isoindolones and their use as metabotropic glutamate receptor potentiators
US20110319386A1 (en) 2005-08-26 2011-12-29 Braincells Inc. Neurogenesis by muscarinic receptor modulation
EP2275095A3 (en) 2005-08-26 2011-08-17 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
WO2007044937A2 (en) 2005-10-13 2007-04-19 President And Fellows Of Harvard College Compositions and methods to modulate memory
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
GB0607946D0 (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
US20090082342A1 (en) 2007-09-21 2009-03-26 Acadia Pharmaceuticals, Inc. N-substituted piperidine derivatives as serotonin receptor agents
AU2008302079A1 (en) 2007-09-21 2009-03-26 Acadia Pharmaceuticals, Inc. Co-administration of pimavanserin with other agents
US20090082368A1 (en) * 2007-09-24 2009-03-26 Painceptor Pharma Corporation Methods of modulating neurotrophin-mediated activity
US20100267712A1 (en) 2007-09-27 2010-10-21 The United States of America, as represented by the Secretary, Department of Health and 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
AU2010216263A1 (en) 2009-02-23 2011-07-14 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
US8877944B2 (en) 2009-07-14 2014-11-04 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
HUE044653T2 (hu) 2009-07-22 2019-11-28 PureTech Health LLC Készítmények olyan rendellenességek kezelésére, amelyek muszkarin-receptor aktiválással enyhíthetõk
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
EP2709451B1 (en) 2011-05-17 2015-12-30 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
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
EP2821401B1 (en) 2012-03-02 2020-09-09 Takeda Pharmaceutical Company Limited Dihydroquinolinone compounds as modulators of the muscarininc m1 receptor
US20130289019A1 (en) 2012-04-26 2013-10-31 Amazing Grace, Inc. Methods of treating behaviorial and/or mental disorders
EP2921480B1 (en) 2012-11-19 2017-10-11 Takeda Pharmaceutical Company Limited Nitrogen-containing heterocyclic compound
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
CA2918925A1 (en) 2013-09-27 2015-04-02 F. Hoffmann-La Roche Ag Indol and indazol derivatives
GB201317363D0 (en) 2013-10-01 2013-11-13 Eisai Ltd Novel compounds
WO2015163485A1 (en) * 2014-04-23 2015-10-29 Takeda Pharmaceutical Company Limited Isoindoline-1-one derivatives as cholinergic muscarinic m1 receptor positive alloesteric modulator activity for the treatment of alzheimers disease
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
US20200188388A1 (en) 2016-12-29 2020-06-18 Rvx Therapeutics Ltd. Methods 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

Also Published As

Publication number Publication date
US20220411413A1 (en) 2022-12-29
NZ725921A (en) 2023-09-29
US9775827B2 (en) 2017-10-03
US20170258764A1 (en) 2017-09-14
US20170100373A1 (en) 2017-04-13
EP3134386B1 (en) 2020-05-20
EP3134386A1 (en) 2017-03-01
UY36091A (es) 2015-11-30
US10865200B2 (en) 2020-12-15
WO2015163485A1 (en) 2015-10-29
JP2017513894A (ja) 2017-06-01
KR102349237B1 (ko) 2022-01-07
BR112016024472A2 (pt) 2017-08-15
DK3134386T3 (da) 2020-08-17
CR20160544A (es) 2017-01-13
LT3134386T (lt) 2020-08-10
KR20160143852A (ko) 2016-12-14
BR112016024472A8 (pt) 2021-06-29
EA030373B1 (ru) 2018-07-31
CL2016002661A1 (es) 2017-03-24
TN2016000455A1 (en) 2018-04-04
US9315458B2 (en) 2016-04-19
PE20161400A1 (es) 2017-01-06
HRP20201171T1 (hr) 2020-11-13
US20180000780A1 (en) 2018-01-04
US20210009572A1 (en) 2021-01-14
IL248393A0 (en) 2016-11-30
US10457670B2 (en) 2019-10-29
US20160152598A1 (en) 2016-06-02
US20180346452A1 (en) 2018-12-06
ES2811088T3 (es) 2021-03-10
TWI664165B (zh) 2019-07-01
MY195742A (en) 2023-02-08
CA2946519A1 (en) 2015-10-29
US20240109874A1 (en) 2024-04-04
PL3134386T3 (pl) 2020-11-16
EA201692132A1 (ru) 2017-04-28
US20170044143A1 (en) 2017-02-16
AR100154A1 (es) 2016-09-14
US9868725B2 (en) 2018-01-16
US9655881B2 (en) 2017-05-23
PH12016502095A1 (en) 2017-01-09
US9499516B2 (en) 2016-11-22
SG11201608785PA (en) 2016-11-29
US20150307451A1 (en) 2015-10-29
RS60524B1 (sr) 2020-08-31
US20190241547A1 (en) 2019-08-08
DOP2016000286A (es) 2017-02-15
CN106536508A (zh) 2017-03-22
UA122391C2 (uk) 2020-11-10
ECSP16090152A (es) 2017-08-31
BR112016024472B1 (pt) 2023-02-14
MX2016013810A (es) 2017-03-09
AU2015250610A1 (en) 2016-12-01
PT3134386T (pt) 2020-08-25
AU2015250610B2 (en) 2019-02-07
CY1123569T1 (el) 2022-03-24
US20160152603A1 (en) 2016-06-02
US9662316B2 (en) 2017-05-30
US9675597B2 (en) 2017-06-13
US9789084B2 (en) 2017-10-17
SI3134386T1 (sl) 2020-10-30
US20170027921A1 (en) 2017-02-02
JP6517239B2 (ja) 2019-05-22
CA2946519C (en) 2022-07-19
US20170266162A1 (en) 2017-09-21
IL248393B (en) 2019-10-31
US9518042B2 (en) 2016-12-13
US20170100384A1 (en) 2017-04-13
US20170216255A1 (en) 2017-08-03
US9789083B2 (en) 2017-10-17
HUE050543T2 (hu) 2020-12-28
PH12016502095B1 (en) 2024-07-03
TW201623233A (zh) 2016-07-01
MX373274B (es) 2020-04-16

Similar Documents

Publication Publication Date Title
CN106536508B (zh) 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
JP7135007B2 (ja) 複素環化合物
US10214508B2 (en) Nitrogen-containing heterocyclic compound
CN107922403A (zh) 作为胆碱能毒蕈碱m1受体的调节剂的2,3‑二氢‑4h‑1,3‑苯并噁嗪‑4‑酮衍生物
JP7114594B2 (ja) 複素環化合物
HK1231880A1 (en) Isoindoline-1-one derivatives as cholinergic muscarinic m1 receptor positive alloesteric modulator activity for the treatment of alzheimers disease
HK1231880B (en) Isoindoline-1-one derivatives as cholinergic muscarinic m1 receptor positive alloesteric modulator activity for the treatment of alzheimers disease

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant