AU2015213900B2 - Bicyclic aza compounds as muscarinic M1 receptor and/or M4 receptor agonists - Google Patents

Bicyclic aza compounds as muscarinic M1 receptor and/or M4 receptor agonists Download PDF

Info

Publication number
AU2015213900B2
AU2015213900B2 AU2015213900A AU2015213900A AU2015213900B2 AU 2015213900 B2 AU2015213900 B2 AU 2015213900B2 AU 2015213900 A AU2015213900 A AU 2015213900A AU 2015213900 A AU2015213900 A AU 2015213900A AU 2015213900 B2 AU2015213900 B2 AU 2015213900B2
Authority
AU
Australia
Prior art keywords
mmol
carboxylate
hydrocarbon group
compound according
tert
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
AU2015213900A
Other languages
English (en)
Other versions
AU2015213900A1 (en
Inventor
Giles Albert Brown
Julie Elaine Cansfield
Miles Stuart Congreve
Michael Alistair O'brien
Mark PICKWORTH
Mark David RACKHAM
Benjamin Gerald TEHAN
Barry John TEOBOLD
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.)
Nxera Pharma UK Ltd
Original Assignee
Nxera Pharma UK 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=52465550&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AU2015213900(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from GBGB1402013.5A external-priority patent/GB201402013D0/en
Priority claimed from GBGB1416622.7A external-priority patent/GB201416622D0/en
Application filed by Nxera Pharma UK Ltd filed Critical Nxera Pharma UK Ltd
Publication of AU2015213900A1 publication Critical patent/AU2015213900A1/en
Application granted granted Critical
Publication of AU2015213900B2 publication Critical patent/AU2015213900B2/en
Priority to AU2019201579A priority Critical patent/AU2019201579B2/en
Priority to AU2020277225A priority patent/AU2020277225A1/en
Assigned to NXERA PHARMA UK LIMITED reassignment NXERA PHARMA UK LIMITED Request to Amend Deed and Register Assignors: HEPTARES THERAPEUTICS LIMITED
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/28—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
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/14—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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Addiction (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Indole Compounds (AREA)
AU2015213900A 2014-02-06 2015-02-06 Bicyclic aza compounds as muscarinic M1 receptor and/or M4 receptor agonists Active AU2015213900B2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2019201579A AU2019201579B2 (en) 2014-02-06 2019-03-07 Bicyclic aza compounds as muscarinic M1 receptor and/or M4 receptor agonists
AU2020277225A AU2020277225A1 (en) 2014-02-06 2020-11-26 Bicyclic aza compounds as muscarinic M1 receptor and/or M4 receptor agonists

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GBGB1402013.5A GB201402013D0 (en) 2014-02-06 2014-02-06 Pharmaceutical compounds
GB1402013.5 2014-02-06
GB1416622.7 2014-09-19
GBGB1416622.7A GB201416622D0 (en) 2014-09-19 2014-09-19 Pharmaceutical compounds
PCT/GB2015/050331 WO2015118342A1 (en) 2014-02-06 2015-02-06 Bicyclic aza compounds as muscarinic m1 receptor agonists.

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2019201579A Division AU2019201579B2 (en) 2014-02-06 2019-03-07 Bicyclic aza compounds as muscarinic M1 receptor and/or M4 receptor agonists

Publications (2)

Publication Number Publication Date
AU2015213900A1 AU2015213900A1 (en) 2016-08-11
AU2015213900B2 true AU2015213900B2 (en) 2018-12-13

Family

ID=52465550

Family Applications (3)

Application Number Title Priority Date Filing Date
AU2015213900A Active AU2015213900B2 (en) 2014-02-06 2015-02-06 Bicyclic aza compounds as muscarinic M1 receptor and/or M4 receptor agonists
AU2019201579A Active AU2019201579B2 (en) 2014-02-06 2019-03-07 Bicyclic aza compounds as muscarinic M1 receptor and/or M4 receptor agonists
AU2020277225A Abandoned AU2020277225A1 (en) 2014-02-06 2020-11-26 Bicyclic aza compounds as muscarinic M1 receptor and/or M4 receptor agonists

Family Applications After (2)

Application Number Title Priority Date Filing Date
AU2019201579A Active AU2019201579B2 (en) 2014-02-06 2019-03-07 Bicyclic aza compounds as muscarinic M1 receptor and/or M4 receptor agonists
AU2020277225A Abandoned AU2020277225A1 (en) 2014-02-06 2020-11-26 Bicyclic aza compounds as muscarinic M1 receptor and/or M4 receptor agonists

Country Status (30)

Country Link
US (6) US9670183B2 (enExample)
EP (4) EP3102568B1 (enExample)
JP (7) JP6479029B2 (enExample)
KR (1) KR102352388B1 (enExample)
CN (2) CN106458986B (enExample)
AU (3) AU2015213900B2 (enExample)
BR (1) BR112016017979B1 (enExample)
CA (1) CA2938169C (enExample)
CL (1) CL2016001983A1 (enExample)
CY (1) CY1120834T1 (enExample)
DK (3) DK4413985T3 (enExample)
ES (3) ES3073836T3 (enExample)
FI (2) FI4413985T3 (enExample)
HR (2) HRP20241145T1 (enExample)
HU (1) HUE068301T2 (enExample)
IL (1) IL247117B (enExample)
LT (3) LT4413985T (enExample)
MX (2) MX371529B (enExample)
NZ (1) NZ723103A (enExample)
PH (1) PH12016501570B1 (enExample)
PL (2) PL3102568T3 (enExample)
PT (3) PT3102568T (enExample)
RS (3) RS68268B1 (enExample)
RU (1) RU2685230C2 (enExample)
SA (1) SA516371614B1 (enExample)
SG (1) SG11201606269WA (enExample)
SI (2) SI3406609T1 (enExample)
SM (1) SMT202400446T1 (enExample)
UA (1) UA122121C2 (enExample)
WO (1) WO2015118342A1 (enExample)

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2619829T3 (es) 2011-11-18 2017-06-27 Heptares Therapeutics Limited Agonistas del receptor muscarínico M1
DK2968297T3 (en) 2013-03-15 2019-01-07 Verseon Inc MULTI-SUBSTITUTED AROMATIC COMPOUNDS AS SERINE PROTEASE INHIBITORS
RU2685230C2 (ru) 2014-02-06 2019-04-17 Хептарес Терапьютикс Лимитед Бициклические азотсодержащие соединения как агонисты М1 мускариновых рецепторов
GB201404922D0 (en) * 2014-03-19 2014-04-30 Heptares Therapeutics Ltd Pharmaceutical compounds
JP2017528486A (ja) 2014-09-17 2017-09-28 ヴァーセオン コーポレイション セリンプロテアーゼ阻害剤としてのピラゾリル置換ピリドン化合物
ES2931460T3 (es) * 2015-02-27 2022-12-29 Verseon Int Corporation Compuestos de pirazol sustituido como inhibidores de serina proteasa
GB201504675D0 (en) 2015-03-19 2015-05-06 Heptares Therapeutics Ltd Pharmaceutical compounds
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
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
EP3394061B1 (en) 2015-12-23 2020-03-11 Merck Sharp & Dohme Corp. 6,7-dihydro-5h-pyrrolo[3,4-b]pyridin-5-one allosteric modulators of the m4 muscarinic acetylcholine receptor
PL3478679T3 (pl) * 2016-07-01 2021-10-25 Pfizer Inc. Pochodne 5,7-dihydro-pirolopirydyny do leczenia chorób neurologicznych i neurodegeneracyjnych
GB201617454D0 (en) * 2016-10-14 2016-11-30 Heptares Therapeutics Limited Pharmaceutical compounds
WO2018112842A1 (en) 2016-12-22 2018-06-28 Merck Sharp & Dohme Corp. 6,6-fused heteroaryl piperidine ether allosteric modulators of m4 muscarinic acetylcholine receptor
WO2018112843A1 (en) 2016-12-22 2018-06-28 Merck Sharp & Dohme Corp. Heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor
GB201709652D0 (en) * 2017-06-16 2017-08-02 Heptares Therapeutics Ltd Pharmaceutical compounds
EP3643703A4 (en) 2017-06-21 2020-12-23 Daiichi Sankyo Co., Ltd. EP300 / CREBBP INHIBITOR
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
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
EP3651762B1 (en) 2017-07-12 2024-07-03 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
CN110944999A (zh) * 2017-08-01 2020-03-31 勃林格殷格翰国际有限公司 中间体化合物和方法
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
US10501483B2 (en) 2017-10-24 2019-12-10 Allergan, Inc. Enamines and diastereo-selective reduction of enamines
EP3732163A4 (en) * 2017-12-20 2021-07-14 Vanderbilt University MUSCARIN M4 ACETYLCHOLIN RECEPTOR ANTAGONISTS
EP3768669B1 (en) * 2018-03-23 2023-01-25 Pfizer Inc. Piperazine azaspiro derivaves
GB201810239D0 (en) 2018-06-22 2018-08-08 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201810245D0 (en) * 2018-06-22 2018-08-08 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201819960D0 (en) 2018-12-07 2019-01-23 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201819961D0 (en) 2018-12-07 2019-01-23 Heptares Therapeutics Ltd Pharmaceutical compounds
GB202020191D0 (en) 2020-12-18 2021-02-03 Heptares Therapeutics Ltd Pharmaceutical compounds
UY38906A (es) * 2019-10-09 2021-05-31 Novartis Ag Compuestos 2- derivados de azaspiro[3,4]octano como agonistas de m4 y composiciones de los mismos
PH12022550860A1 (en) * 2019-10-09 2023-06-14 Novartis Ag 5-oxa-2-azaspiro[3.4]octane derivatives as m4 agonists
US12486250B2 (en) 2019-12-06 2025-12-02 Neurocrine Biosciences, Inc. Muscarinic receptor 4 antagonists and methods of use
TWI889751B (zh) * 2020-02-05 2025-07-11 美商紐羅克里生物科學有限公司 蕈毒受體4拮抗劑及使用方法
US11912705B2 (en) * 2020-08-20 2024-02-27 The Corporation Of Mercer University Cathinone derivatives, pharmaceutical formulations, and methods
US20250064833A1 (en) 2021-12-13 2025-02-27 Sage Therapeutics, Inc. Combination of muscarinic receptor positive modulators and nmda positive allosteric modulators
CR20250069A (es) 2022-08-04 2025-05-26 Nxera Pharma Uk Ltd Formas cristalinas y sales de un agonista del receptor muscarínico
KR20250086639A (ko) * 2022-09-16 2025-06-13 세레벨 쎄라퓨틱스, 엘엘씨 M4 활성제/조절제 및 이의 용도
AU2024208125A1 (en) * 2023-01-12 2025-07-10 Cerevel Therapeutics, Llc Spiro derivatives as m4 activators/modulators and uses thereof
JP2026503599A (ja) 2023-01-24 2026-01-29 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 重水素化化合物
CN116496195A (zh) * 2023-05-10 2023-07-28 南京优氟医药科技有限公司 一种(r)-4,4-二氟代吡咯烷-2-羧酸的制备方法
KR20260046441A (ko) 2023-08-03 2026-04-07 뉴로크린 바이오사이언시즈 인코퍼레이티드 합성 방법
WO2026050225A1 (en) 2024-08-27 2026-03-05 Neurocrine Biosciences, Inc. Method of treating a neurological or psychiatric disease or disorder
WO2026050236A1 (en) 2024-08-27 2026-03-05 Neurocrine Biosciences, Inc. Muscarinic receptor agonist in combination with a vesicular monoamine transporter 2 inhibitor, for use in the treatment of a neurological or psychiatric disorder
TW202615016A (zh) 2024-08-27 2026-04-16 美商紐羅克里生物科學有限公司 醫藥調配物
TW202615015A (zh) 2024-08-27 2026-04-16 美商紐羅克里生物科學有限公司 特定毒蕈鹼受體激動劑之投與方法
WO2026050238A1 (en) 2024-08-27 2026-03-05 Neurocrine Biosciences, Inc. Muscarinic receptor agonist for use in the treatment of a neurological or psychiatric disorder
TW202619719A (zh) 2024-08-27 2026-05-16 美商紐羅克里生物科學有限公司 治療方法
TW202619712A (zh) * 2024-09-09 2026-05-16 大陸商翼思生物醫藥(蘇州)有限公司 5-ht2a受體激動劑及m4活化劑之組合及其用途

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070054911A1 (en) * 2005-03-28 2007-03-08 Ioana Drutu Muscarinic modulators
WO2007100670A1 (en) * 2006-02-22 2007-09-07 Vertex Pharmaceuticals Incorporated Spiro condensed piperidnes as modulators of muscarinic receptors
CN101874020A (zh) * 2007-09-11 2010-10-27 阿斯利康(瑞典)有限公司 作为毒蕈碱受体激动剂的哌啶衍生物
WO2013072705A1 (en) * 2011-11-18 2013-05-23 Heptares Therapeutics Limited Muscarinic m1 receptor agonists
WO2014045031A1 (en) * 2012-09-18 2014-03-27 Heptares Therapeutics Limited Bicyclic aza compounds as muscarinic m1 receptor agonists

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5852029A (en) 1990-04-10 1998-12-22 Israel Institute For Biological Research Aza spiro compounds acting on the cholinergic system with muscarinic agonist activity
AU2206699A (en) 1997-12-23 1999-07-12 Alcon Laboratories, Inc. Muscarinic agents and use thereof to treat glaucoma, myopia and various other conditions
US7164024B2 (en) * 2001-04-20 2007-01-16 Banyu Pharmaceutical Co., Ltd. Benzimidazolone derivatives
AU2005249494A1 (en) * 2004-05-28 2005-12-15 Vertex Pharmaceuticals Incorporated Modulators of muscarinic receptors
CA2634456A1 (en) 2005-12-22 2007-07-05 Vertex Pharmaceuticals Incorporated Modulators of muscarinic receptors
US8003660B2 (en) 2006-02-22 2011-08-23 Vertex Pharmaceuticals Incorporated Modulators of muscarinic receptors
WO2007106670A2 (en) * 2006-03-03 2007-09-20 Novartis Ag N-formyl hydroxylamine compounds
GB0706188D0 (en) * 2007-03-29 2007-05-09 Glaxo Group Ltd Compounds
AU2009309988A1 (en) 2008-10-29 2010-05-06 Grunenthal Gmbh Substituted spiroamines
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
WO2012020813A1 (ja) * 2010-08-10 2012-02-16 大日本住友製薬株式会社 縮環ピロリジン誘導体
HK1214815A1 (zh) 2013-04-30 2016-08-05 Glaxosmithkline Intellectual Property (No. 2) Limited Zeste增强子同源物2的抑制剂
RU2685230C2 (ru) * 2014-02-06 2019-04-17 Хептарес Терапьютикс Лимитед Бициклические азотсодержащие соединения как агонисты М1 мускариновых рецепторов
CR20160400A (es) 2014-02-06 2016-11-07 Riboscience Llc Derivados de nucleosido sustituidos con 4´-difluorometilo como inhibidores de la replicación de arn de la influenza
PL3102572T3 (pl) 2014-02-06 2019-04-30 Janssen Sciences Ireland Uc Pochodne sulfamoilopirolamidu i ich zastosowanie jako leki do leczenia wirusowego zapalenia wątroby typu B
WO2016042084A1 (en) 2014-09-19 2016-03-24 Bayer Pharma Aktiengesellschaft Benzyl substituted indazoles as bub1 inhibitors
HUE062424T2 (hu) 2014-09-19 2023-11-28 Forma Therapeutics Inc Piridin-2(1H)-on kinolinon származékok mint mutáns izocitrát dehidrogenáz inhibitorok
EA033697B1 (ru) 2014-09-19 2019-11-18 Glaxosmithkline Ip Dev Ltd Активаторы растворимой гуанилатциклазы и их применение

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070054911A1 (en) * 2005-03-28 2007-03-08 Ioana Drutu Muscarinic modulators
WO2007100670A1 (en) * 2006-02-22 2007-09-07 Vertex Pharmaceuticals Incorporated Spiro condensed piperidnes as modulators of muscarinic receptors
CN101874020A (zh) * 2007-09-11 2010-10-27 阿斯利康(瑞典)有限公司 作为毒蕈碱受体激动剂的哌啶衍生物
WO2013072705A1 (en) * 2011-11-18 2013-05-23 Heptares Therapeutics Limited Muscarinic m1 receptor agonists
WO2014045031A1 (en) * 2012-09-18 2014-03-27 Heptares Therapeutics Limited Bicyclic aza compounds as muscarinic m1 receptor agonists
US9266857B2 (en) * 2012-09-18 2016-02-23 Heptares Therapeutics Limited Bicyclic AZA compounds as muscarinic M1 receptor agonists

Also Published As

Publication number Publication date
CN106458986B (zh) 2019-01-04
BR112016017979B1 (pt) 2022-08-02
HRP20241145T1 (hr) 2024-11-22
EP3102568B1 (en) 2018-06-27
EP4413985A2 (en) 2024-08-14
US20190337925A1 (en) 2019-11-07
US9926297B2 (en) 2018-03-27
AU2019201579B2 (en) 2020-08-27
JP2023073504A (ja) 2023-05-25
PT3102568T (pt) 2018-10-24
DK3102568T3 (en) 2018-10-08
AU2015213900A1 (en) 2016-08-11
FI3406609T3 (fi) 2024-09-10
RS68268B1 (en) 2026-07-31
EP3102568A1 (en) 2016-12-14
KR102352388B1 (ko) 2022-01-17
US10961225B2 (en) 2021-03-30
HK1231473A1 (en) 2017-12-22
EP3406609B1 (en) 2024-06-26
CL2016001983A1 (es) 2017-06-23
RU2685230C2 (ru) 2019-04-17
HUE068301T2 (hu) 2024-12-28
PT4413985T (pt) 2026-06-17
MX371529B (es) 2020-01-31
SI3406609T1 (sl) 2024-10-30
US20190112294A1 (en) 2019-04-18
US20170015650A1 (en) 2017-01-19
US10385039B2 (en) 2019-08-20
CA2938169A1 (en) 2015-08-13
LT4413985T (lt) 2026-07-10
US10196380B2 (en) 2019-02-05
SMT202400446T1 (it) 2024-11-15
RS57843B1 (sr) 2018-12-31
ES2688548T3 (es) 2018-11-05
EP4714446A3 (en) 2026-06-03
EP3406609A1 (en) 2018-11-28
LT3102568T (lt) 2018-11-12
BR112016017979A2 (enExample) 2017-08-08
SA516371614B1 (ar) 2019-10-30
JP2019077725A (ja) 2019-05-23
WO2015118342A8 (en) 2016-06-30
JP7652829B2 (ja) 2025-03-27
CN109851610A (zh) 2019-06-07
AU2020277225A1 (en) 2020-12-24
US10689368B2 (en) 2020-06-23
UA122121C2 (uk) 2020-09-25
JP7652833B2 (ja) 2025-03-27
JP2017505323A (ja) 2017-02-16
PL3406609T3 (pl) 2024-11-25
CA2938169C (en) 2022-03-15
RS65894B1 (sr) 2024-09-30
DK4413985T3 (da) 2026-07-06
JP6479029B2 (ja) 2019-03-06
WO2015118342A1 (en) 2015-08-13
JP6774513B2 (ja) 2020-10-28
JP7652832B2 (ja) 2025-03-27
JP2023087045A (ja) 2023-06-22
CN109851610B (zh) 2021-09-21
RU2016133684A3 (enExample) 2018-08-31
LT3406609T (lt) 2024-09-25
SI3102568T1 (sl) 2018-11-30
JP2023087046A (ja) 2023-06-22
DK3406609T3 (da) 2024-08-26
ES3073836T3 (en) 2026-07-15
US20170240530A1 (en) 2017-08-24
PH12016501570A1 (en) 2016-10-03
HRP20181499T1 (hr) 2018-11-30
RU2016133684A (ru) 2018-03-14
PL3102568T3 (pl) 2019-01-31
AU2019201579A1 (en) 2019-03-28
MX2020001236A (es) 2022-06-30
CN106458986A (zh) 2017-02-22
KR20160129014A (ko) 2016-11-08
EP4413985A3 (en) 2024-10-23
FI4413985T3 (fi) 2026-07-03
IL247117A0 (en) 2016-09-29
JP2021006571A (ja) 2021-01-21
US9670183B2 (en) 2017-06-06
PT3406609T (pt) 2024-09-17
EP4714446A2 (en) 2026-03-25
US20180179184A1 (en) 2018-06-28
CY1120834T1 (el) 2019-12-11
MX2016010322A (es) 2017-04-27
US20200325118A1 (en) 2020-10-15
IL247117B (en) 2021-03-25
JP2025085736A (ja) 2025-06-05
NZ723103A (en) 2022-09-30
ES2986327T3 (es) 2024-11-11
SG11201606269WA (en) 2016-09-29
MX393637B (es) 2025-03-11
EP4413985B1 (en) 2026-05-06
PH12016501570B1 (en) 2016-10-03

Similar Documents

Publication Publication Date Title
US10961225B2 (en) Bicyclic AZA compounds as muscarinic M1 receptor and/or M4 receptor
CA2994143C (en) Muscarinic agonists
HK40114593A (en) Pharmaceutical compounds
RU2811601C1 (ru) Бициклические азотсодержащие соединения как агонисты М1 мускариновых рецепторов
RU2811601C9 (ru) Бициклические азотсодержащие соединения как агонисты М1 мускариновых рецепторов
HK1231473B (en) Bicyclic aza compounds as muscarinic m1 receptor agonists
HK40007500A (en) Bicyclic aza compounds as muscarinic m1 receptor and/or m4 receptor agonists

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
HB Alteration of name in register

Owner name: NXERA PHARMA UK LIMITED

Free format text: FORMER NAME(S): HEPTARES THERAPEUTICS LIMITED