CO2022013856A2 - Derivados de benzodiazepinas como pam de gaba a gamma1 - Google Patents

Derivados de benzodiazepinas como pam de gaba a gamma1

Info

Publication number
CO2022013856A2
CO2022013856A2 CONC2022/0013856A CO2022013856A CO2022013856A2 CO 2022013856 A2 CO2022013856 A2 CO 2022013856A2 CO 2022013856 A CO2022013856 A CO 2022013856A CO 2022013856 A2 CO2022013856 A2 CO 2022013856A2
Authority
CO
Colombia
Prior art keywords
gamma1
gaba
pam
benzodiazepine derivatives
compounds
Prior art date
Application number
CONC2022/0013856A
Other languages
English (en)
Inventor
Giuseppe Cecere
Maria-Clemencia Hernandez
Luca Gobbi
Frédéric Knoflach
Andreas Koblet
Eoin Cornelius O`Connor
Morales Andres Miguel Olivares
Michael Reutlinger
Valerie Runtz-Schmitt
Cusulin Jaclyn Ivy Wamsteeker
Nicolas Zorn
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 CO2022013856A2 publication Critical patent/CO2022013856A2/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic 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
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • 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

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 R1, R2, R3, R4, R5 y X son como se describe en la presente, en donde las composiciones incluyen los compuestos y métodos de uso de los compuestos.
CONC2022/0013856A 2020-03-31 2022-09-28 Derivados de benzodiazepinas como pam de gaba a gamma1 CO2022013856A2 (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
CO2022013856A2 true CO2022013856A2 (es) 2022-10-11

Family

ID=70110167

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2022/0013856A CO2022013856A2 (es) 2020-03-31 2022-09-28 Derivados de benzodiazepinas como pam de gaba a gamma1

Country Status (18)

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)
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
WO2021198124A1 (en) * 2020-03-31 2021-10-07 F. Hoffmann-La Roche Ag Benzodiazepine derivatives as gaba a gamma1 pams
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
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
US3734922A (en) * 1971-05-11 1973-05-22 Upjohn Co Certain 4h-s-triazolo(4,3-a)(1,4)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
JP2005525392A (ja) 2002-03-28 2005-08-25 ウィシス テクノロジー ファウンデーション，インコーポレイティド 減少された鎮静及び失調効果を有する抗不安薬剤
US9006233B2 (en) * 2011-04-28 2015-04-14 Uwm Research Foundation, Inc. Gabaergic receptor subtype selective ligands and their uses
US10266534B2 (en) 2014-06-26 2019-04-23 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
CN109790170B (zh) * 2016-08-16 2022-08-02 Uwm研究基金会有限公司 Gaba(a)受体调节剂和控制哮喘中气道高反应性和炎症的方法
WO2020198275A1 (en) 2019-03-25 2020-10-01 President And Fellows Of Harvard College Compositions and methods for reducing tactile dysfunction, anxiety, and social impairment
WO2021198124A1 (en) * 2020-03-31 2021-10-07 F. Hoffmann-La Roche Ag Benzodiazepine derivatives as gaba a gamma1 pams

Also Published As

Publication number Publication date
KR20220161307A (ko) 2022-12-06
US20210309664A1 (en) 2021-10-07
BR112022018828A2 (pt) 2022-11-22
US11739095B2 (en) 2023-08-29
WO2021198124A1 (en) 2021-10-07
TW202200585A (zh) 2022-01-01
JP2023521572A (ja) 2023-05-25
MX2022011708A (es) 2022-10-07
AR121676A1 (es) 2022-06-29
CN115380034A (zh) 2022-11-22
EP4126869B1 (en) 2024-06-05
ZA202207383B (en) 2023-04-26
PE20230440A1 (es) 2023-03-08
CA3167543A1 (en) 2021-10-07
IL294350A (en) 2022-08-01
CR20220478A (es) 2022-10-27
US20240002393A1 (en) 2024-01-04
AU2021246833A1 (en) 2022-07-21
EP4126869A1 (en) 2023-02-08
CL2022002661A1 (es) 2023-03-31

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