CR20220478A - Derivados de benzodiazepinas como pam de gaba a gamma 1 - Google Patents

Derivados de benzodiazepinas como pam de gaba a gamma 1

Info

Publication number
CR20220478A
CR20220478A CR20220478A CR20220478A CR20220478A CR 20220478 A CR20220478 A CR 20220478A CR 20220478 A CR20220478 A CR 20220478A CR 20220478 A CR20220478 A CR 20220478A CR 20220478 A CR20220478 A CR 20220478A
Authority
CR
Costa Rica
Prior art keywords
sup
gamma1
pams
gaba
benzodiazepine derivatives
Prior art date
Application number
CR20220478A
Other languages
English (en)
Inventor
Eoin Cornelius O`Connor
Luca Gobbi
Giuseppe Cecere
Frédéric Knoflach
Michael Reutlinger
Morales Andres Miguel Olivares
Andrea Koblet
Nicolas Zorn
Maria-Clemencia Hernandez
Cusulin Jaclyn Ivy Wamsteeker
Valerie Runtz-Schmitt
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of CR20220478A publication Critical patent/CR20220478A/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/55171,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system

Landscapes

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

Abstract

La invención proporciona compuestos novedosos que tienen la fórmula general (I) en donde R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5 </sup>y X son como se describe en la presente, en donde las composiciones incluyen los compuestos y métodos de uso de los compuestos.
CR20220478A 2020-03-31 2021-03-29 Derivados de benzodiazepinas como pam de gaba a gamma 1 CR20220478A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP20167239 2020-03-31
PCT/EP2021/058063 WO2021198124A1 (en) 2020-03-31 2021-03-29 Benzodiazepine derivatives as gaba a gamma1 pams

Publications (1)

Publication Number Publication Date
CR20220478A true CR20220478A (es) 2022-10-27

Family

ID=70110167

Family Applications (1)

Application Number Title Priority Date Filing Date
CR20220478A CR20220478A (es) 2020-03-31 2021-03-29 Derivados de benzodiazepinas como pam de gaba a gamma 1

Country Status (19)

Country Link
US (2) US11739095B2 (es)
EP (1) EP4126869B1 (es)
JP (1) JP2023521572A (es)
KR (1) KR20220161307A (es)
CN (1) CN115380034A (es)
AR (1) AR121676A1 (es)
AU (1) AU2021246833A1 (es)
BR (1) BR112022018828A2 (es)
CA (1) CA3167543A1 (es)
CL (1) CL2022002661A1 (es)
CO (1) CO2022013856A2 (es)
CR (1) CR20220478A (es)
IL (1) IL294350A (es)
MX (1) MX2022011708A (es)
PE (1) PE20230440A1 (es)
PT (1) PT4126869T (es)
TW (1) TW202200585A (es)
WO (1) WO2021198124A1 (es)
ZA (1) ZA202207383B (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115380034A (zh) * 2020-03-31 2022-11-22 豪夫迈·罗氏有限公司 作为GABA Aγ1 PAM的苯并二氮杂䓬衍生物
WO2023213757A1 (en) 2022-05-03 2023-11-09 F. Hoffmann-La Roche Ag Pet tracers for visualizing gabaa gamma1 receptors
WO2024023268A1 (en) 2022-07-29 2024-02-01 F. Hoffmann-La Roche Ag Characterisation of neurological dysfunction

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3987052A (en) * 1969-03-17 1976-10-19 The Upjohn Company 6-Phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines
US3734922A (en) * 1971-05-11 1973-05-22 Upjohn Co Certain 4h-s-triazolo(4,3-a)(1,4)benzodiazepines
US3681343A (en) * 1971-05-11 1972-08-01 Upjohn Co 6-phenyl-s-triazolo{8 4,3-a{9 {8 1,4{9 {0 benzodiazepines
US4201712A (en) 1975-07-16 1980-05-06 Boehringer Ingelheim Gmbh Process for preparation of 6-aryl-4H-s-triazolo-[3,4-c]-thieno-[2,3-e]-1,4-diazepines
DE3435973A1 (de) * 1984-10-01 1986-04-10 Boehringer Ingelheim KG, 6507 Ingelheim Diazepine enthaltende pharmazeutische zusammensetzungen mit paf-antagonistischer wirkung
PH30676A (en) 1986-07-22 1997-09-16 Boehringer Ingelhein Kg Hetrazepine compounds which have useful pharmaceutical utility
DE4101146A1 (de) 1991-01-16 1992-07-23 Boehringer Ingelheim Kg Neue in 6-position substituierte diazepine, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
DE60319812T2 (de) 2002-03-28 2009-04-23 Wisys Technology Foundation, Inc., Madison Angstlösende wirkstoffe mit verminderten beruhigenden und ataktischen nebenwirkungen
US9006233B2 (en) * 2011-04-28 2015-04-14 Uwm Research Foundation, Inc. Gabaergic receptor subtype selective ligands and their uses
EP4299126A3 (en) 2014-06-26 2024-04-03 The Johns Hopkins University Peripherally restricted gaba positive allosteric modulators for the treatment of irritable bowel syndrome and other ailments of the peripheral nervous system
WO2018035246A1 (en) * 2016-08-16 2018-02-22 Uwm Research Foundation, Inc. Gaba(a) receptor modulators and methods to control airway hyperresponsiveness and inflammation in asthma
US12077512B2 (en) 2019-03-25 2024-09-03 President And Fellows Of Harvard College Compositions and methods for reducing tactile dysfunction, anxiety, and social impairment
CN115380034A (zh) * 2020-03-31 2022-11-22 豪夫迈·罗氏有限公司 作为GABA Aγ1 PAM的苯并二氮杂䓬衍生物

Also Published As

Publication number Publication date
EP4126869B1 (en) 2024-06-05
CO2022013856A2 (es) 2022-10-11
WO2021198124A1 (en) 2021-10-07
TW202200585A (zh) 2022-01-01
EP4126869A1 (en) 2023-02-08
CL2022002661A1 (es) 2023-03-31
PT4126869T (pt) 2024-07-29
CN115380034A (zh) 2022-11-22
JP2023521572A (ja) 2023-05-25
US20240002393A1 (en) 2024-01-04
AR121676A1 (es) 2022-06-29
BR112022018828A2 (pt) 2022-11-22
MX2022011708A (es) 2022-10-07
US20210309664A1 (en) 2021-10-07
ZA202207383B (en) 2023-04-26
IL294350A (en) 2022-08-01
CA3167543A1 (en) 2021-10-07
US11739095B2 (en) 2023-08-29
AU2021246833A1 (en) 2022-07-21
PE20230440A1 (es) 2023-03-08
KR20220161307A (ko) 2022-12-06

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