PE20221454A1 - Derivados de 2-azaespiro[3.4]octano como agonistas de m4 - Google Patents

Derivados de 2-azaespiro[3.4]octano como agonistas de m4

Info

Publication number
PE20221454A1
PE20221454A1 PE2022000586A PE2022000586A PE20221454A1 PE 20221454 A1 PE20221454 A1 PE 20221454A1 PE 2022000586 A PE2022000586 A PE 2022000586A PE 2022000586 A PE2022000586 A PE 2022000586A PE 20221454 A1 PE20221454 A1 PE 20221454A1
Authority
PE
Peru
Prior art keywords
halogen
agonists
octane
azaspyro
azaspiro
Prior art date
Application number
PE2022000586A
Other languages
English (en)
Inventor
Amy Calhoun
Xin Chen
Kevin Matthew Gardinier
Edward Charles Hall
Keith Jendza
Nancy Labbe-Giguere
James Neef
Daniel Steven Palacios
Ming Qian
Michael David Shultz
Christopher G Thomson
Kate Yaping Wang
Fan Yang
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of PE20221454A1 publication Critical patent/PE20221454A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • 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
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P25/18Antipsychotics, 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
    • A61P25/24Antidepressants
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence

Landscapes

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

Abstract

Referido a un compuesto derivado de 2-azaespiro[3.4]octano de formula (I), o una sal farmaceutica aceptable del mismo, en donde R1 es halogeno o H; R2 es halogeno o H; R3 es alquilo C1-3 opcionalmente sustituido; R5 es halogeno o H; R7 es heteroarilo de 5 miembros. Un compuesto seleccionado es (S)-7-(4-(5-fluor-2-(oxetan-3-iloxi)fenil)piperidin-1-il)-2-(1,3,4-oxadiazol-2-il)-5-oxa-2-azaspiro[3.4]octano. Dichos compuestos actuan como agonistas del receptor M4. Tambien refiere a una composicion farmaceuticas que los comprende y su uso para el tratamiento de afecciones, enfermedades y trastornos relacionados con el receptor M4, tales como psicosis, disfuncion cognitiva y trastornos por uso de sustancias.
PE2022000586A 2019-10-09 2020-10-07 Derivados de 2-azaespiro[3.4]octano como agonistas de m4 PE20221454A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962912986P 2019-10-09 2019-10-09
PCT/IB2020/059431 WO2021070091A1 (en) 2019-10-09 2020-10-07 5-oxa-2-azaspiro[3.4]octane derivatives as m4 agonists

Publications (1)

Publication Number Publication Date
PE20221454A1 true PE20221454A1 (es) 2022-09-21

Family

ID=72944206

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2022000586A PE20221454A1 (es) 2019-10-09 2020-10-07 Derivados de 2-azaespiro[3.4]octano como agonistas de m4

Country Status (20)

Country Link
US (3) US11485742B2 (es)
EP (1) EP4041737A1 (es)
JP (1) JP7349567B2 (es)
KR (1) KR20220079608A (es)
CN (1) CN114555606A (es)
AR (1) AR120169A1 (es)
AU (1) AU2020364186B2 (es)
CA (1) CA3155589A1 (es)
CL (1) CL2022000892A1 (es)
CO (1) CO2022004391A2 (es)
CR (1) CR20220153A (es)
EC (1) ECSP22027784A (es)
IL (1) IL291600A (es)
JO (1) JOP20220084A1 (es)
MX (1) MX2022004215A (es)
PE (1) PE20221454A1 (es)
TW (1) TW202128703A (es)
UY (1) UY38907A (es)
WO (1) WO2021070091A1 (es)
ZA (1) ZA202202913B (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR120170A1 (es) * 2019-10-09 2022-02-02 Novartis Ag Derivados de 2-azaspiro[3,4]octano como agonistas de m4
WO2024059249A1 (en) * 2022-09-16 2024-03-21 Cerevel Therapeutics, Llc M4 activators/modulators and uses thereof

Family Cites Families (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1597255A1 (en) 2002-11-13 2005-11-23 Rigel Pharmaceuticals, Inc. Rhodanine derivatives and pharmaceutical compositions containing them
US7479496B2 (en) 2004-02-19 2009-01-20 Bristol-Myers Squibb Company Substituted spiro azabicyclics as modulators of chemokine receptor activity
WO2006006490A1 (ja) 2004-07-08 2006-01-19 Ono Pharmaceutical Co., Ltd. スピロ化合物
WO2006058294A2 (en) * 2004-11-29 2006-06-01 Vertex Pharmaceuticals Incorporated Modulators of muscarinic receptors
WO2008024497A2 (en) 2006-08-25 2008-02-28 Vitae Pharmaceuticals, Inc. INHIBITORS OF 11β -HYDROXYSTEROID DEHYDROGENASE TYPE 1
US20090291134A1 (en) * 2006-11-21 2009-11-26 Jina Pharmaceuticals, Inc. Endoxifen methods and compositions in the treatment of psychiatric and neurodegenerative diseases
WO2010049146A1 (en) 2008-10-29 2010-05-06 Grünenthal GmbH Substituted spiroamines
RU2506266C2 (ru) * 2009-01-26 2014-02-10 Израэл Инститьют Фо Байолоджикал Рисерч Бициклические гетероциклические спиросоединения
WO2012062752A1 (en) 2010-11-08 2012-05-18 Janssen Pharmaceuticals, Inc. RADIOLABELLED mGLuR2 PET LIGANDS
EP2675812B1 (en) 2011-02-18 2017-08-30 Vertex Pharmaceuticals Incorporated Chroman - spirocyclic piperidine amides as modulators of ion channels
WO2013013308A1 (en) 2011-07-27 2013-01-31 Beta Pharma Canada Inc. Spirocyclic molecules as protein kinase inhibitors
WO2014039489A1 (en) 2012-09-07 2014-03-13 Zoetis Llc Spirocyclic derivatives as antiparasitic agents
WO2014045031A1 (en) 2012-09-18 2014-03-27 Heptares Therapeutics Limited Bicyclic aza compounds as muscarinic m1 receptor agonists
JP6479029B2 (ja) * 2014-02-06 2019-03-06 ヘプタレス セラピューティクス リミテッドHeptares Therapeutics Limited ムスカリンm1受容体アゴニストとしての二環式アザ化合物
MA40858A (fr) 2014-10-31 2021-03-31 Indivior Uk Ltd Composés antagonistes des récepteurs d3 à la dopamine
GB201504675D0 (en) 2015-03-19 2015-05-06 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201513740D0 (en) * 2015-08-03 2015-09-16 Heptares Therapeutics Ltd Muscarinic agonist
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
GB2540998A (en) 2015-08-04 2017-02-08 Phagenesis Ltd Catheter
GB201519352D0 (en) 2015-11-02 2015-12-16 Heptares Therapeutics Ltd Pharmaceutical compounds
ES2831084T3 (es) * 2016-06-10 2021-06-07 Vitae Pharmaceuticals Inc Inhibidores de la interacción menina-MLL
GB201617454D0 (en) 2016-10-14 2016-11-30 Heptares Therapeutics Limited Pharmaceutical compounds
CN108456208B (zh) 2017-02-22 2021-04-16 广州市恒诺康医药科技有限公司 氮杂螺环类化合物及其制备方法和应用
WO2018175746A1 (en) 2017-03-24 2018-09-27 Kura Oncology, Inc. Methods for treating hematological malignancies and ewing's sarcoma
US11524954B2 (en) 2018-03-23 2022-12-13 Pfizer Inc. Piperazine azaspiro derivatives
GB201810245D0 (en) 2018-06-22 2018-08-08 Heptares Therapeutics Ltd Pharmaceutical compounds

Also Published As

Publication number Publication date
KR20220079608A (ko) 2022-06-13
UY38907A (es) 2021-05-31
AR120169A1 (es) 2022-02-02
US11485742B2 (en) 2022-11-01
CA3155589A1 (en) 2021-04-15
JP2022551853A (ja) 2022-12-14
ECSP22027784A (es) 2022-05-31
CO2022004391A2 (es) 2022-04-29
US20220411435A1 (en) 2022-12-29
WO2021070091A1 (en) 2021-04-15
US20240140959A1 (en) 2024-05-02
AU2020364186A1 (en) 2022-04-21
EP4041737A1 (en) 2022-08-17
US11820778B2 (en) 2023-11-21
JP7349567B2 (ja) 2023-09-22
ZA202202913B (en) 2023-06-28
IL291600A (en) 2022-05-01
TW202128703A (zh) 2021-08-01
MX2022004215A (es) 2022-05-03
CN114555606A (zh) 2022-05-27
JOP20220084A1 (ar) 2023-01-30
CR20220153A (es) 2022-05-03
CL2022000892A1 (es) 2023-01-20
AU2020364186B2 (en) 2023-11-30
US20210130365A1 (en) 2021-05-06

Similar Documents

Publication Publication Date Title
PE20190329A1 (es) Compuestos moduladores de fxr (nr1h4)
PE20220133A1 (es) Inhibidores del inflamasoma nlrp3
PE20230249A1 (es) Compuestos de heteroarilo biciclicos y usos de estos
PE20230238A1 (es) Inhibidores de kras g12c
PE20220931A1 (es) Inhibidores de shp2 fosfatasa de tipo pirazolo[3,4-b]pirazina
PE20190806A1 (es) Agonistas heterociclicos del receptor de apelina (apj) y usos de los mismos
PE20180227A1 (es) Benzamidas sustituidas con 1,3-tiazol-2-ilo
MY194461A (en) N-[2-(1-benzylpiperidin-4-yl)4-(pyrazin-2-yl)-piperazine-1-carboxamide derivatives and related compounds as muscarinic receptor 4 (m4) antagonists for treating neurological diseases
PE20061150A1 (es) Derivados de n-(n-sulfonilaminoarilmetil)ciclopropanocarboxamida sustituidos como antagonistas del receptor vainilloide tipo 1 (vdr1)
AR075729A1 (es) Derivados de benzofuranilo, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de la obesidad y/o diabetes.
AR056103A1 (es) Compuestos de(piran-piperidinil)benzimidazol, composiciones farmaceuticas que los comprenden, proceso de preparacion y usos en el tratamiento de afecciones mediadas por agonistas del receptor muscarinico m1
AR072952A1 (es) Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso
PE20170682A1 (es) Derivados de pirimidina sustituidos con heterociclilo opcionalmente condensados utiles para el tratamiento de enfermedades inflamatorias, metabolicas, oncologicas y autoinmunitarias
PE20221454A1 (es) Derivados de 2-azaespiro[3.4]octano como agonistas de m4
BR112022005674A2 (pt) Derivado de anel fundido aromático substituído e composição compreendendo o mesmo, e uso do mesmo
PE20161369A1 (es) Inhibidores de monoacilglicerol aciltransferasa 2 (mgat2) de dihidropiridinona sustituidos con tetrazolona
CR20200418A (es) Inhibidores de orginasa y sus mètodos de uso antecedentes
PE20240930A1 (es) Analogos de benzoazepina como agentes inhibidores de la tirosina cinasa de bruton
RU2017117559A (ru) Бензопроизводные с шестичленным кольцом в качестве ингибитора dpp-4 и их применение
AR116880A1 (es) Compuestos de pirimidinodiona bicíclicos sustituidos con tetrahidropirano, forma polimórfica del mismo y el uso de los mismos para el tratamiento del hcm
ZA202104940B (en) Novel substituted sulfonylurea derivatives
PE20190109A1 (es) Nuevos derivados de [1,2,3]triazolo[4,5-d]pirimidina
CL2009001146A1 (es) Compuestos derivados de 5-(5-(2-(3,5-bis(trifluorometil)fenil)-n,2-dimetilpropanoamida)-4-(4-fluoro-2-metilfenil)piridin-2-il)pirrolidin-2-carboxamida, antagonistas de los receptores nk-1; composicion farmaceutica; y uso del compuesto para el tratamiento de la depresion; ansiedad, trastornos del sueño o emesis.
CL2022000893A1 (es) Derivados de 2-azaspiro[3,4]octano como agonistas de m4
AR118641A1 (es) Compuestos, composiciones y métodos