PE20211809A1 - Derivados de espirocromano - Google Patents

Derivados de espirocromano

Info

Publication number
PE20211809A1
PE20211809A1 PE2021000053A PE2021000053A PE20211809A1 PE 20211809 A1 PE20211809 A1 PE 20211809A1 PE 2021000053 A PE2021000053 A PE 2021000053A PE 2021000053 A PE2021000053 A PE 2021000053A PE 20211809 A1 PE20211809 A1 PE 20211809A1
Authority
PE
Peru
Prior art keywords
methyl
alkyl
dihydrospiro
benzopyran
indol
Prior art date
Application number
PE2021000053A
Other languages
English (en)
Inventor
Janos Eles
Molnar Katalin Dudasne
Istvan Ledneczki
Pal Tapolcsanyi
Anita Horvath
Zsolt Nemethy
Gyorgy Istvan Levay
Original Assignee
Richter Gedeon Nyrt
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 Richter Gedeon Nyrt filed Critical Richter Gedeon Nyrt
Publication of PE20211809A1 publication Critical patent/PE20211809A1/es

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    • 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
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • 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
    • A61K31/404Indoles, e.g. pindolol
    • 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
    • A61K31/404Indoles, e.g. pindolol
    • A61K31/4045Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • 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
    • A61K31/407Heterocyclic 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 other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K31/425Thiazoles
    • A61K31/428Thiazoles condensed with carbocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/438The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • 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
    • 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
    • C07D491/12Heterocyclic 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 three hetero rings
    • C07D491/20Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Esta referido a un compuesto de Formula I, en donde: A es un heterociclo de cinco o seis miembros; B es un carbociclo o heterociclo de seis miembros; X, Y, Z son C o N; R1 es H, alquilo, halogeno, haloalquilo; R2 es H, O; R3 es H, alquilo, halogeno, haloalquilo, alcoxi; R4, R5 son H, alquilo; n, m son 1, 2; W es O, S. Entre los compuestos preferidos tenemos los siguientes: 6'-Fluoro-N-[(2-metil-1H-indol-5-il)metil]-4'-oxo-3',4'- dihidroespiro[azetidin-3,2'-[1]benzopiran]-1-carboxamida; 7'-fluoro-N-[(1-metil-1H-indol-5-il)metil]-4'-oxo-3',4'-dihidroespiro[azetidin3,2'-[1]benzopiran]-1-carboxamida; entre otros. Estos compuestos son moduladores de la actividad del receptor nicotinico de acetilcolina a7 y se emplean en el tratamiento de esquizofrenia, deterioro cognitivo como resultado de un accidente cerebrovascular, enfermedad de Alzheimer, enfermedad de Huntington, entre otras.
PE2021000053A 2018-07-13 2019-07-12 Derivados de espirocromano PE20211809A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
HUP1800248A HU231333B1 (hu) 2018-07-13 2018-07-13 Spirokromán származékok
PCT/IB2019/055948 WO2020012422A1 (en) 2018-07-13 2019-07-12 Spirochromane derivatives

Publications (1)

Publication Number Publication Date
PE20211809A1 true PE20211809A1 (es) 2021-09-14

Family

ID=89992725

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2021000053A PE20211809A1 (es) 2018-07-13 2019-07-12 Derivados de espirocromano

Country Status (23)

Country Link
US (1) US20210330650A1 (es)
EP (1) EP3820869B1 (es)
JP (1) JP7487167B2 (es)
KR (1) KR20210033002A (es)
CN (1) CN112823157A (es)
AR (1) AR115782A1 (es)
AU (1) AU2019300514B2 (es)
BR (1) BR112020026996A2 (es)
CA (1) CA3104258A1 (es)
CL (1) CL2021000080A1 (es)
CO (1) CO2021001216A2 (es)
CU (1) CU24680B1 (es)
EA (1) EA202190245A1 (es)
ES (1) ES2964617T3 (es)
GE (1) GEP20237534B (es)
HU (2) HU231333B1 (es)
IL (1) IL279938A (es)
MX (1) MX2021000460A (es)
PE (1) PE20211809A1 (es)
PH (1) PH12020552183A1 (es)
SG (1) SG11202012594RA (es)
TW (1) TWI821321B (es)
WO (1) WO2020012422A1 (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202202495A (zh) 2020-03-26 2022-01-16 匈牙利商羅特格登公司 作為gamma-胺基丁酸A受體次單元alpha 5受體調節劑之㖠啶及吡啶并〔3,4-c〕嗒𠯤衍生物
CN115403579A (zh) * 2021-05-27 2022-11-29 上海拓界生物医药科技有限公司 一种新的螺环衍生物及其用途
HUP2100338A1 (hu) 2021-09-29 2023-04-28 Richter Gedeon Nyrt GABAA ALFA5 receptor modulátor hatású biciklusos aminszármazékok

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EP1782811A4 (en) 2004-08-09 2010-09-01 Eisai R&D Man Co Ltd INNOVATIVE ANTIPALUDITIC AGENT CONTAINING A HETEROCYCLIC COMPOUND
EA015034B1 (ru) 2005-09-13 2011-04-29 Янссен Фармацевтика Н.В. 2-анилин-4-арилзамещенные тиазольные производные
CN101490056A (zh) * 2006-05-17 2009-07-22 阿斯利康(瑞典)有限公司 烟碱乙酰胆碱受体的配体101
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CA2713519A1 (en) 2008-02-07 2009-08-13 Abbott Laboratories Amide derivatives as positive allosteric modulators and methods of use thereof
KR101564303B1 (ko) 2008-03-19 2015-11-06 얀센 파마슈티카 엔.브이. 니코틴성 아세틸콜린 수용체 조절제로서의 삼치환된 1,2,4-트리아졸
EP2110377A1 (en) * 2008-04-15 2009-10-21 DAC S.r.l. Spirocyclic derivatives as histone deacetylase inhibitors
ES2392795T3 (es) 2008-04-17 2012-12-13 Proximagen Limited Indoles como moduladores del receptor nicotínico de acetilcolina de subtipo alfa-7
WO2009135944A1 (en) 2008-05-09 2009-11-12 Janssen Pharmaceutica Nv Trisubstituted pyrazoles as acetylcholine receptor modulators
WO2009155017A2 (en) 2008-05-30 2009-12-23 Merck & Co., Inc. Novel substituted azabenzoxazoles
HRP20221090T1 (hr) 2009-12-31 2022-11-25 Hutchison Medipharma Limited Određeni triazolopirazini, njihovi pripravci i postupci njihove upotrebe
JP2013538784A (ja) 2010-10-01 2013-10-17 ラクオリア創薬株式会社 Trpm8拮抗剤としてのスルファモイル安息香酸ヘテロ二環性誘導体
CA2892682A1 (en) * 2013-03-13 2014-09-18 Lupin Limited Pyrrole derivatives as alpha 7 nachr modulators
ES2901197T3 (es) 2016-03-22 2022-03-21 Merck Sharp & Dohme Moduladores alostéricos de los receptores nicotínicos de la acetilcolina
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MX2019006920A (es) * 2016-12-14 2019-11-28 89Bio Ltd Derivados de la espiropiperidina.

Also Published As

Publication number Publication date
HU231333B1 (hu) 2023-01-28
BR112020026996A2 (pt) 2021-04-06
US20210330650A1 (en) 2021-10-28
CN112823157A (zh) 2021-05-18
GEP20237534B (en) 2023-09-11
CU20200108A7 (es) 2021-07-02
ES2964617T3 (es) 2024-04-08
AU2019300514A1 (en) 2021-02-11
MX2021000460A (es) 2021-06-23
HUP1800248A2 (en) 2020-01-28
CO2021001216A2 (es) 2021-02-26
JP7487167B2 (ja) 2024-05-20
PH12020552183A1 (en) 2021-06-21
CL2021000080A1 (es) 2021-10-29
HUE064417T2 (hu) 2024-03-28
SG11202012594RA (en) 2021-02-25
CA3104258A1 (en) 2020-01-16
TW202035399A (zh) 2020-10-01
WO2020012422A1 (en) 2020-01-16
JP2021531260A (ja) 2021-11-18
TWI821321B (zh) 2023-11-11
EP3820869B1 (en) 2023-08-30
CU24680B1 (es) 2023-10-06
AU2019300514B2 (en) 2023-02-02
IL279938A (en) 2021-03-01
KR20210033002A (ko) 2021-03-25
EP3820869A1 (en) 2021-05-19
EA202190245A1 (ru) 2021-04-20
AR115782A1 (es) 2021-02-24

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