BR112018002279B1 - Compostos agonistas muscarinícos, composição farmacêutica e usos terapêuticos dos mesmos - Google Patents

Compostos agonistas muscarinícos, composição farmacêutica e usos terapêuticos dos mesmos Download PDF

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Publication number
BR112018002279B1
BR112018002279B1 BR112018002279-9A BR112018002279A BR112018002279B1 BR 112018002279 B1 BR112018002279 B1 BR 112018002279B1 BR 112018002279 A BR112018002279 A BR 112018002279A BR 112018002279 B1 BR112018002279 B1 BR 112018002279B1
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BR
Brazil
Prior art keywords
ethyl
carboxylate
amino
piperidin
octane
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BR112018002279-9A
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English (en)
Portuguese (pt)
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BR112018002279A2 (enExample
Inventor
Giles Albert Brown
Miles Stuart Congreve
Mark Pickworth
Benjamin Gerald Tehan
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Heptares Therapeutics Limited
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Publication of BR112018002279A2 publication Critical patent/BR112018002279A2/pt
Publication of BR112018002279B1 publication Critical patent/BR112018002279B1/pt

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    • 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
    • C07D401/04Heterocyclic 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
    • 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
    • C07D401/08Heterocyclic 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
    • 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
    • A61K31/451Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
    • 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
    • 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
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • 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
    • A61P25/28Drugs 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
    • 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
    • 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
    • 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
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
BR112018002279-9A 2015-08-03 2016-08-03 Compostos agonistas muscarinícos, composição farmacêutica e usos terapêuticos dos mesmos BR112018002279B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1513742.5A GB201513742D0 (en) 2015-08-03 2015-08-03 Muscarinic agonists
GB1513742.5 2015-08-03
PCT/GB2016/052386 WO2017021730A1 (en) 2015-08-03 2016-08-03 Muscarinic agonists

Publications (2)

Publication Number Publication Date
BR112018002279A2 BR112018002279A2 (enExample) 2018-10-02
BR112018002279B1 true BR112018002279B1 (pt) 2024-01-30

Family

ID=54063148

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112018002279-9A BR112018002279B1 (pt) 2015-08-03 2016-08-03 Compostos agonistas muscarinícos, composição farmacêutica e usos terapêuticos dos mesmos

Country Status (23)

Country Link
US (4) US9758506B2 (enExample)
EP (2) EP3822262B1 (enExample)
JP (1) JP6876675B2 (enExample)
KR (1) KR102664558B1 (enExample)
CN (1) CN107949558B (enExample)
AR (1) AR105593A1 (enExample)
AU (1) AU2016302048B2 (enExample)
BR (1) BR112018002279B1 (enExample)
CA (1) CA2993484C (enExample)
CL (1) CL2018000292A1 (enExample)
CO (1) CO2018002060A2 (enExample)
DK (1) DK3331869T3 (enExample)
ES (2) ES2980578T3 (enExample)
GB (1) GB201513742D0 (enExample)
IL (1) IL257064A (enExample)
MX (1) MX379530B (enExample)
MY (1) MY195244A (enExample)
PH (1) PH12018500259A1 (enExample)
RU (1) RU2737158C2 (enExample)
TW (1) TWI723037B (enExample)
UA (1) UA123315C2 (enExample)
WO (1) WO2017021730A1 (enExample)
ZA (1) ZA201800715B (enExample)

Families Citing this family (27)

* 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
GB201404922D0 (en) 2014-03-19 2014-04-30 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
SG10201911831RA (en) 2015-08-03 2020-02-27 Bristol Myers Squibb Co Heterocyclic compounds useful as modulators of tnf alpha
CN108026050B (zh) 2015-08-03 2021-04-30 格兰马克药品股份有限公司 作为RORγ调节剂的新型化合物
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
US10329289B2 (en) 2015-12-23 2019-06-25 Merck Sharp & Dohme Corp. 6,7-dihydro-5H-pyrrolo[3,4-B]pyridin-5-one allosteric modulators of the M4 muscarinic acetylcholine receptor
GB201617454D0 (en) 2016-10-14 2016-11-30 Heptares Therapeutics Limited Pharmaceutical compounds
WO2018112843A1 (en) 2016-12-22 2018-06-28 Merck Sharp & Dohme Corp. Heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor
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
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
EP3661939B1 (en) * 2017-08-01 2021-07-21 Boehringer Ingelheim International GmbH Intermediate compounds and methods
CA3079188A1 (en) * 2017-10-17 2019-04-25 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
WO2019183636A1 (en) * 2018-03-23 2019-09-26 Pfizer Inc. Piperazine azaspiro derivaves
GB201810245D0 (en) * 2018-06-22 2018-08-08 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201810239D0 (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
CR20220153A (es) 2019-10-09 2022-05-03 Novartis Ag Derivados de 2–azaespiro [3.4] octano como agonistas de m4
WO2023114224A1 (en) 2021-12-13 2023-06-22 Sage Therapeutics, Inc. Combination of muscarinic receptor positive modulators and nmda positive allosteric modulators

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2642649A1 (en) * 2006-02-22 2007-09-07 Vertex Pharmaceuticals Incorporated Modulators of muscarinic receptors
UY31672A1 (es) 2008-02-28 2009-09-30 "agonistas de receptores muscarínicos composiciones farmacéuticas métodos de tratamiento de los mismos, y procedimientos para su preparación"
WO2011112825A2 (en) * 2010-03-10 2011-09-15 Vanderbilt University Heterocyclyl-azabicyclo[3.2.1]octane analogs as selective m1 agonists and methods of making and using same
ES2619829T3 (es) * 2011-11-18 2017-06-27 Heptares Therapeutics Limited Agonistas del receptor muscarínico M1
EP2897948B1 (en) * 2012-09-18 2016-08-31 Heptares Therapeutics Limited Bicyclic aza compounds as muscarinic m1 receptor agonists
EP4413985A3 (en) * 2014-02-06 2024-10-23 Nxera Pharma UK Limited Pharmaceutical compounds
GB201513742D0 (en) 2015-08-03 2015-09-16 Heptares Therapeutics Ltd Muscarinic agonists
AR105556A1 (es) 2015-08-03 2017-10-18 Hoffmann La Roche Derivados de etinilo
CN108026050B (zh) 2015-08-03 2021-04-30 格兰马克药品股份有限公司 作为RORγ调节剂的新型化合物
SG10201911831RA (en) 2015-08-03 2020-02-27 Bristol Myers Squibb Co Heterocyclic compounds useful as modulators of tnf alpha

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Publication number Publication date
WO2017021730A1 (en) 2017-02-09
CN107949558A (zh) 2018-04-20
ES2850298T3 (es) 2021-08-26
KR102664558B1 (ko) 2024-05-09
MX379530B (es) 2025-03-11
RU2018105020A (ru) 2019-09-06
RU2737158C2 (ru) 2020-11-25
DK3331869T3 (da) 2021-02-15
BR112018002279A2 (enExample) 2018-10-02
US20180155315A1 (en) 2018-06-07
AU2016302048B2 (en) 2020-09-10
CL2018000292A1 (es) 2018-06-29
HK1250160A1 (en) 2018-11-30
CN107949558B (zh) 2022-03-15
KR20180039657A (ko) 2018-04-18
ZA201800715B (en) 2018-12-19
AU2016302048A1 (en) 2018-02-22
US10351545B2 (en) 2019-07-16
US10167272B2 (en) 2019-01-01
IL257064A (en) 2018-03-29
TWI723037B (zh) 2021-04-01
EP3822262A1 (en) 2021-05-19
JP2018522032A (ja) 2018-08-09
CO2018002060A2 (es) 2018-06-20
US9758506B2 (en) 2017-09-12
CA2993484A1 (en) 2017-02-09
GB201513742D0 (en) 2015-09-16
AR105593A1 (es) 2017-10-18
US20190270718A1 (en) 2019-09-05
EP3822262C0 (en) 2024-03-27
EP3331869B1 (en) 2020-12-23
JP6876675B2 (ja) 2021-05-26
PH12018500259A1 (en) 2018-08-13
MY195244A (en) 2023-01-11
EP3822262B1 (en) 2024-03-27
US20170037025A1 (en) 2017-02-09
CA2993484C (en) 2023-10-24
EP3331869A1 (en) 2018-06-13
MX2018001564A (es) 2018-09-06
UA123315C2 (uk) 2021-03-17
ES2980578T3 (es) 2024-10-02
RU2018105020A3 (enExample) 2019-09-06
US20180022726A1 (en) 2018-01-25
TW201716391A (zh) 2017-05-16
US11091456B2 (en) 2021-08-17

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B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 03/08/2016, OBSERVADAS AS CONDICOES LEGAIS

B25G Requested change of headquarter approved

Owner name: HEPTARES THERAPEUTICS LIMITED (GB)

B25D Requested change of name of applicant approved

Owner name: NXERA PHARMA UK LIMITED (GB)