MX2022011708A - Derivados de benzodiazepinas como moduladores alostericos positivos (pam) de acido gamma-aminobutirico (gaba) a gamma1. - Google Patents

Derivados de benzodiazepinas como moduladores alostericos positivos (pam) de acido gamma-aminobutirico (gaba) a gamma1.

Info

Publication number
MX2022011708A
MX2022011708A MX2022011708A MX2022011708A MX2022011708A MX 2022011708 A MX2022011708 A MX 2022011708A MX 2022011708 A MX2022011708 A MX 2022011708A MX 2022011708 A MX2022011708 A MX 2022011708A MX 2022011708 A MX2022011708 A MX 2022011708A
Authority
MX
Mexico
Prior art keywords
gamma1
pams
gaba
benzodiazepine derivatives
compounds
Prior art date
Application number
MX2022011708A
Other languages
English (en)
Inventor
Luca Gobbi
Andreas Koblet
Maria-Clemencia Hernandez
Valerie Runtz-Schmitt
Giuseppe Cecere
Frédéric Knoflach
Eoin Cornelius O`Connor
Morales Andres Miguel Olivares
Michael Reutlinger
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 MX2022011708A publication Critical patent/MX2022011708A/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) (ver Fórmula) (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.
MX2022011708A 2020-03-31 2021-03-29 Derivados de benzodiazepinas como moduladores alostericos positivos (pam) de acido gamma-aminobutirico (gaba) a gamma1. MX2022011708A (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
MX2022011708A true MX2022011708A (es) 2022-10-07

Family

ID=70110167

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2022011708A MX2022011708A (es) 2020-03-31 2021-03-29 Derivados de benzodiazepinas como moduladores alostericos positivos (pam) de acido gamma-aminobutirico (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
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
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
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
EP3160969B1 (en) 2014-06-26 2023-09-13 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
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
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
PE20230440A1 (es) 2023-03-08
CO2022013856A2 (es) 2022-10-11
WO2021198124A1 (en) 2021-10-07
AU2021246833A1 (en) 2022-07-21
ZA202207383B (en) 2023-04-26
BR112022018828A2 (pt) 2022-11-22
IL294350A (en) 2022-08-01
CA3167543A1 (en) 2021-10-07
US20210309664A1 (en) 2021-10-07
CL2022002661A1 (es) 2023-03-31
CR20220478A (es) 2022-10-27
CN115380034A (zh) 2022-11-22
EP4126869A1 (en) 2023-02-08
US11739095B2 (en) 2023-08-29
KR20220161307A (ko) 2022-12-06
TW202200585A (zh) 2022-01-01
US20240002393A1 (en) 2024-01-04
AR121676A1 (es) 2022-06-29
JP2023521572A (ja) 2023-05-25

Similar Documents

Publication Publication Date Title
MX2022011708A (es) Derivados de benzodiazepinas como moduladores alostericos positivos (pam) de acido gamma-aminobutirico (gaba) a gamma1.
PH12021551167A1 (en) New heterocyclic compounds
PH12021500013A1 (en) New heterocyclic compounds as monoacylgylcerol lipase inhibitors
CR20200416A (es) Nuevos compuestos heterocíclicos
PH12019500664A1 (en) New isoxazolyl ether derivatives as gaba a alpha5 pam
MX2021014350A (es) Compuestos de 1-oxo-isoindolin-5-carboxamida sustituida, composiciones de los mismos y metodos de tratamiento con los mismos.
MX2022002711A (es) Nuevos inhibidores heterociclicos de monoacilglicerol lipasa (magl).
SI1732933T1 (sl) Spojine za zdravljenje dislipidemije
MX2020009234A (es) Compuestos de heteroarilo como inhibidores de cinasas asociadas con receptores de interleucina-1 (irak) tipo ii y usos de los mismos.
MX2022003023A (es) Compuestos heterociclicos.
TW200613289A (en) Prodrugs of hiv protease inhibitors
MX2022002831A (es) Compuestos heterociclicos.
PH12020552207A1 (en) Pyrazole derivatives as malt1 inhibitors
MX2022000243A (es) Nuevos compuestos heterociclicos.
MX2023002224A (es) Compuestos heterociclicos.
MX2021001565A (es) Inhibidores tipo indol y azaindol de enzimas peptidil arginina deiminasas (pad).
CR20230496A (es) Compuestos heterocíclicos
PH12020552206A1 (en) Pyrazole derivatives as malt1 inhibitors
MY138466A (en) Aminoalkoxyndoles as 5-ht6-receptor ligands for the treatment of cns-disorders
CR20230382A (es) Derivados de tetrahidroazepina bicíclicos para el tratamiento del cáncer
CR20200610A (es) Nuevos derivados de isoxazolit éter como pan de gaba a alfa 5
DK1599460T3 (da) Oxathiincarboxamider
WO2021249908A3 (en) Amino-pyrimidine amides
MX2022010675A (es) Composiciones que comprenden profarmacos de metilfenidato, procesos de elaboracion y uso de los mismos.
MX2023004115A (es) Compuestos del inhibidor de la autotaxina.