BR112015006029A2 - compostos aza bicíclicos como agonistas de receptor m1 muscarínicos - Google Patents

compostos aza bicíclicos como agonistas de receptor m1 muscarínicos

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Publication number
BR112015006029A2
BR112015006029A2 BR112015006029A BR112015006029A BR112015006029A2 BR 112015006029 A2 BR112015006029 A2 BR 112015006029A2 BR 112015006029 A BR112015006029 A BR 112015006029A BR 112015006029 A BR112015006029 A BR 112015006029A BR 112015006029 A2 BR112015006029 A2 BR 112015006029A2
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BR
Brazil
Prior art keywords
muscarinic
compounds
receptor agonists
aza compounds
bicyclic aza
Prior art date
Application number
BR112015006029A
Other languages
English (en)
Other versions
BR112015006029B1 (pt
Inventor
Gerald Tehan Benjamin
Albert Brown Giles
Elaine Cansfield Julie
Pickworth Mark
Stuart Congreve Miles
Original Assignee
Heptares Therapeutics 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.)
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Publication date
Application filed by Heptares Therapeutics Ltd filed Critical Heptares Therapeutics Ltd
Publication of BR112015006029A2 publication Critical patent/BR112015006029A2/pt
Publication of BR112015006029B1 publication Critical patent/BR112015006029B1/pt

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    • 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
    • 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
    • A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • 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
    • A61P25/04—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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • C07D401/08—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 linked by a carbon chain containing alicyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/14—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantane; Cyclic acetals thereof
    • 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

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

Abstract

resumo “compostos aza bicíclicos como agonistas de receptor m1 muscarínicos” a presente invenção refere-se a compostos (fórmula (1)) que são agonistas do receptor m1 muscarínico e que são úteis no tratamento de doenças mediadas pelo receptor m1 muscarínico. trata-se, também, de composições farmacêuticas contendo os compostos e os usos terapêuticos dos compostos. os compostos fornecidos são de fórmula onde r1-r5, x1, x2 e p são conforme definido no presente documento.
BR112015006029-3A 2012-09-18 2013-09-18 Compostos aza bicíclicos como agonistas de receptor m1 muscarínicos, composição farmacêutica compreendendo ditos compostos e uso dos mesmos para tratar um distúrbio cognitivo ou distúrbio psicótico ou para tratar ou reduzir a gravidade de dores agudas, crônicas, neuropáticas ou inflamatórias BR112015006029B1 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261702330P 2012-09-18 2012-09-18
US61/702,330 2012-09-18
US201361823606P 2013-05-15 2013-05-15
US61/823,606 2013-05-15
PCT/GB2013/052442 WO2014045031A1 (en) 2012-09-18 2013-09-18 Bicyclic aza compounds as muscarinic m1 receptor agonists

Publications (2)

Publication Number Publication Date
BR112015006029A2 true BR112015006029A2 (pt) 2017-07-04
BR112015006029B1 BR112015006029B1 (pt) 2022-01-25

Family

ID=49237505

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112015006029-3A BR112015006029B1 (pt) 2012-09-18 2013-09-18 Compostos aza bicíclicos como agonistas de receptor m1 muscarínicos, composição farmacêutica compreendendo ditos compostos e uso dos mesmos para tratar um distúrbio cognitivo ou distúrbio psicótico ou para tratar ou reduzir a gravidade de dores agudas, crônicas, neuropáticas ou inflamatórias

Country Status (12)

Country Link
US (4) US9266857B2 (pt)
EP (1) EP2897948B1 (pt)
JP (2) JP6204476B2 (pt)
CN (2) CN107098899B (pt)
AU (2) AU2013319989C1 (pt)
BR (1) BR112015006029B1 (pt)
CA (1) CA2883210C (pt)
DK (1) DK2897948T3 (pt)
ES (1) ES2602039T3 (pt)
HK (1) HK1212328A1 (pt)
SG (1) SG11201501620QA (pt)
WO (1) WO2014045031A1 (pt)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
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CA2856076C (en) 2011-11-18 2020-02-25 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
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
GB201404922D0 (en) 2014-03-19 2014-04-30 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201504675D0 (en) * 2015-03-19 2015-05-06 Heptares Therapeutics Ltd Pharmaceutical compounds
WO2016172496A1 (en) 2015-04-23 2016-10-27 Constellation Pharmaceuticals, Inc. Lsd1 inhibitors and uses thereof
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
GB201513743D0 (en) * 2015-08-03 2015-09-16 Heptares Therapeutics Ltd Muscarinic agonists
CN108495854B (zh) * 2015-09-04 2021-10-15 詹森药业有限公司 用于疼痛的治疗性化合物及其合成
GB201519352D0 (en) 2015-11-02 2015-12-16 Heptares Therapeutics Ltd Pharmaceutical compounds
AU2017275657B2 (en) 2016-06-02 2021-08-19 Novartis Ag Potassium channel modulators
GB201617454D0 (en) 2016-10-14 2016-11-30 Heptares Therapeutics Limited Pharmaceutical compounds
HRP20231369T1 (hr) 2016-10-26 2024-02-16 Constellation Pharmaceuticals, Inc. Inhibitori lsd1 i njihova medicinska upotreba
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EP3625232B1 (en) 2017-05-19 2021-06-23 Council of Scientific and Industrial Research Substituted methanopyrido [2, 1-a]isoindolones as machr modulators for treating various associated pathophysiological conditions and process for preparation thereof
GB201709652D0 (en) 2017-06-16 2017-08-02 Heptares Therapeutics Ltd Pharmaceutical compounds
TW201922758A (zh) 2017-10-24 2019-06-16 美商歐樂根公司 烯胺及烯胺的非鏡像選擇性還原
CA3081324A1 (en) 2017-10-31 2019-05-09 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor m4
US11325896B2 (en) 2017-12-20 2022-05-10 Vanderbilt University Antagonists of the muscarinic acetylcholine receptor M4
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
MA53978A (fr) 2018-10-22 2021-09-01 Cadent Therapeutics Inc Formes cristallines de modulateurs des canaux potassiques
GB201819960D0 (en) 2018-12-07 2019-01-23 Heptares Therapeutics Ltd Pharmaceutical compounds
AR120170A1 (es) * 2019-10-09 2022-02-02 Novartis Ag Derivados de 2-azaspiro[3,4]octano como agonistas de m4
TW202128703A (zh) 2019-10-09 2021-08-01 瑞士商諾華公司 作為m4 促效劑之2-氮雜螺[3.4]辛烷衍生物
IL307525A (en) * 2021-04-13 2023-12-01 Pipeline Therapeutics Inc Crystalline compound of EM 1 muscarinic acetylcholine receptor agonists

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WO2014045031A1 (en) * 2012-09-18 2014-03-27 Heptares Therapeutics Limited Bicyclic aza compounds as muscarinic m1 receptor agonists

Also Published As

Publication number Publication date
BR112015006029B1 (pt) 2022-01-25
JP2018021057A (ja) 2018-02-08
EP2897948A1 (en) 2015-07-29
SG11201501620QA (en) 2015-04-29
CA2883210C (en) 2021-06-15
CN104640851B (zh) 2017-05-31
US9975890B2 (en) 2018-05-22
US9266857B2 (en) 2016-02-23
US10259802B2 (en) 2019-04-16
AU2017204256A1 (en) 2017-07-13
AU2013319989A1 (en) 2015-03-12
AU2017204256B2 (en) 2018-10-18
AU2013319989C1 (en) 2017-08-17
US20180258085A1 (en) 2018-09-13
ES2602039T3 (es) 2017-02-17
WO2014045031A1 (en) 2014-03-27
JP2015528489A (ja) 2015-09-28
HK1212328A1 (en) 2016-06-10
JP6204476B2 (ja) 2017-09-27
US20170247369A1 (en) 2017-08-31
CN107098899B (zh) 2019-09-06
CN104640851A (zh) 2015-05-20
US20150232443A1 (en) 2015-08-20
US20160128996A1 (en) 2016-05-12
EP2897948B1 (en) 2016-08-31
JP6438091B2 (ja) 2018-12-12
CN107098899A (zh) 2017-08-29
US9669013B2 (en) 2017-06-06
AU2013319989B2 (en) 2017-03-30
CA2883210A1 (en) 2014-03-27
DK2897948T3 (en) 2016-12-05

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