[go: up one dir, main page]

AR127157A1 - NUEVOS DERIVADOS DE BENZODIAZEPINA COMO MODULADORES ALOSTÉRICOS POSITIVOS DE GABAA g1 - Google Patents

NUEVOS DERIVADOS DE BENZODIAZEPINA COMO MODULADORES ALOSTÉRICOS POSITIVOS DE GABAA g1

Info

Publication number
AR127157A1
AR127157A1 ARP220102592A ARP220102592A AR127157A1 AR 127157 A1 AR127157 A1 AR 127157A1 AR P220102592 A ARP220102592 A AR P220102592A AR P220102592 A ARP220102592 A AR P220102592A AR 127157 A1 AR127157 A1 AR 127157A1
Authority
AR
Argentina
Prior art keywords
alkyl
hydrogen
alkoxy
halo
hydroxy
Prior art date
Application number
ARP220102592A
Other languages
English (en)
Inventor
Bjoern Bartels
Giuseppe Cecere
Guido Galley
Luca Gobbi
Maria Hernandez
- Koblet Andreas Clemencia
Morales Andrs Miguel Olivares
Anglique Patiny-Adam
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 AR127157A1 publication Critical patent/AR127157A1/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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Landscapes

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

Abstract

Reivindicación 1: Un compuesto de fórmula (1) o una sal farmacéuticamente aceptable de este, en donde: W es C-R⁶ o N; X es C-R⁷ o N; R¹ se selecciona de hidrógeno, alquil C₁-C₆, hidroxi-alquil C₁-C₆, halo-alquil C₁-C₆, alcoxi C₁-C₆, alcoxi C₁-C₆-alquil C₁-C₆, ciano, NR⁸R⁹C(O)-, sulfamoílo, alquil C₁-C₆-NH-C(O)-NH-, cicloalquil C₃-C₁₀-NH-C(O)-NH-, alquil C₁-C₆-SO₂-, alquil C₁-C₆-NH-SO₂-, alquil C₁-C₆-C(O)-NH-alquil C₁-C₆-, y un grupo de fórmula (2); R² se selecciona de hidrógeno y alquil C₁-C₆; R³ se selecciona de fluoro y cloro; R⁴ se selecciona de cloro y bromo; R⁵ se selecciona de halógeno, alquil C₁-C₆ y halo-alquil C₁-C₆; R⁶ se selecciona de hidrógeno, alquil C₁-C₆ e hidroxi-alquil C₁-C₆; o R⁶ y R¹, tomados junto con los átomos de carbono a los que están unidos, forman un cicloalquil C₃-C₁₀; R⁷ se selecciona de hidrógeno, fluoro y cloro; R⁸ se selecciona de hidrógeno, alquil C₁-C₆, deuterio-alquil C₁-C₆, halo-alquil C₁-C₆, hidroxi-alquil C₁-C₆, ciano-alquil C₁-C₆, alcoxi C₁-C₆-alquilC₁-C₆, y (alquil C₁-C₆)₂N-; R⁹ se selecciona de hidrógeno, alquil C₁-C₆ y deuterio-alquil C₁-C₆; R¹⁰ se selecciona de hidrógeno, hidroxi, oxo, ciano, halógeno, alquil C₁-C₆, halo-alquil C₁-C₆, alcoxi C₁-C₆, deuterio-alcoxi C₁-C₆, y halo-alcoxi C₁-C₆; R¹¹ se selecciona de hidrógeno y oxo; A se selecciona de un heterocicloalquilo de 3 - 14 miembros y cicloalquil C₃-C₁₀; y L se selecciona de un enlace covalente, carbonilo, O, C(O)NH, NHC(O) y NHC(O)NH.
ARP220102592A 2021-09-29 2022-09-27 NUEVOS DERIVADOS DE BENZODIAZEPINA COMO MODULADORES ALOSTÉRICOS POSITIVOS DE GABAA g1 AR127157A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP21199653 2021-09-29

Publications (1)

Publication Number Publication Date
AR127157A1 true AR127157A1 (es) 2023-12-27

Family

ID=78049169

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP220102592A AR127157A1 (es) 2021-09-29 2022-09-27 NUEVOS DERIVADOS DE BENZODIAZEPINA COMO MODULADORES ALOSTÉRICOS POSITIVOS DE GABAA g1

Country Status (7)

Country Link
US (2) US12365687B2 (es)
EP (1) EP4408848B1 (es)
JP (1) JP2024537773A (es)
CN (1) CN118019742A (es)
AR (1) AR127157A1 (es)
TW (1) TW202322802A (es)
WO (1) WO2023052312A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2026021911A1 (en) 2024-07-23 2026-01-29 Basf Se New substituted benzothiazine pyridine compounds for combatting phytopathogenic fungi
WO2026021909A1 (en) 2024-07-23 2026-01-29 Basf Se New substituted benzothiazine pyridine compounds for combatting phytopathogenic fungi
WO2026021912A1 (en) 2024-07-23 2026-01-29 Basf Se New substituted benzothiazine pyridine compounds for combatting phytopathogenic fungi
WO2026021910A1 (en) 2024-07-23 2026-01-29 Basf Se New substituted benzothiazine pyridine compounds for combatting phytopathogenic fungi

Family Cites Families (30)

* 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
CH562246A5 (es) 1971-04-08 1975-05-30 Ciba Geigy Ag
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
BE786530A (fr) 1971-07-23 1973-01-22 Ciba Geigy Procede de preparation de nouveaux derives de diazepine et composes obtenus
CH551993A (de) 1971-07-23 1974-07-31 Ciba Geigy Ag Verfahren zur herstellung von neuen diazepinderivaten.
US3927016A (en) * 1971-08-04 1975-12-16 Upjohn Co 6-Substituted 4H-imidazo (1,2-a) (1,4)-benzodiazepine-1-carboxaldehydes and processes for their production
BE795020A (fr) 1972-02-07 1973-08-06 Ciba Geigy Procede de preparation de nouvelles diazepines
CH567025A5 (en) 1972-02-07 1975-09-30 Ciba Geigy Ag 4h-s-triazolo (1,5-a) (1,4) benzodiazepine-2-carboxylic acid amide(s) - CNS inhibitors, anticonvulsants, tranquillizers, etc.
CH569018A5 (en) 1972-02-07 1975-11-14 Ciba Geigy Ag 4h-s-triazolo (1,5-a) (1,4) benzodiazepine-2-carboxylic acid amide(s) - CNS inhibitors, anticonvulsants, tranquillizers, etc.
CH569739A5 (en) 1972-02-07 1975-11-28 Ciba Geigy Ag 4h-s-triazolo (1,5-a) (1,4) benzodiazepine-2-carboxylic acid amide(s) - CNS inhibitors, anticonvulsants, tranquillizers, etc.
CH574426A5 (en) 1972-03-20 1976-04-15 Ciba Geigy Ag Triazole carboxylates prepn - 1-(2-Benzoyl-phenyl)-1H-1, 2,4-triazole-3-carboxylates prepd. by reacting 2-aminobenzophenone diazo salts with dialkyl acylamino malonates
CH572057A5 (en) 1973-01-19 1976-01-30 Ciba Geigy Ag 6-Phenyl-s-triazolo(1,5-a)(1,4)-benzodiazepine-2-carboxamides - with CNS depressant activity, from corresp. aldehydes
AT328458B (de) 1973-02-06 1976-03-25 Ciba Geigy Ag Verfahren zur herstellung neuer diazepinderivate sowie deren 5-oxide und saureadditionssalze
CH601264A5 (es) 1974-06-14 1978-06-30 Ciba Geigy Ag
DE2533924C3 (de) 1975-07-30 1979-05-03 C.H. Boehringer Sohn, 6507 Ingelheim Verfahren zur Herstellung von 6- Aryl-4H-striazolo [3,4-c] thieno [2,3-e] 1,4-diazepinen
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
DE3724031A1 (de) 1986-07-22 1988-01-28 Boehringer Ingelheim Kg Neue hetrazepine und verfahren zu ihrer herstellung
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
JP6715830B2 (ja) * 2014-06-26 2020-07-01 ザ・ジョンズ・ホプキンス・ユニバーシティ 過敏性腸症候群および末梢神経系の他の病気の治療のための末梢限局性ｇａｂａポジティブアロステリックモジュレーター
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
BR112022018828A2 (pt) 2020-03-31 2022-11-22 Hoffmann La Roche Derivados de benzodiazepina como gaba a gamma1 pams
EP3901155A1 (en) 2020-04-20 2021-10-27 F. Hoffmann-La Roche AG New benzodiazepine derivatives as gaba a gamma1 pam
AR127127A1 (es) 2021-09-24 2023-12-20 Hoffmann La Roche NUEVOS DERIVADOS DE PIRIDODIAZEPINAS COMO PAM DE GABAA g1
CA3232152A1 (en) 2021-10-06 2023-04-13 F. Hoffman-La Roche Ag Benzodiazepine derivatives as positive allosteric modulators of the gaba a gamma1 receptor

Also Published As

Publication number Publication date
TW202322802A (zh) 2023-06-16
CN118019742A (zh) 2024-05-10
US20260008781A1 (en) 2026-01-08
US12365687B2 (en) 2025-07-22
JP2024537773A (ja) 2024-10-16
WO2023052312A1 (en) 2023-04-06
US20230136326A1 (en) 2023-05-04
EP4408848B1 (en) 2025-11-05
EP4408848A1 (en) 2024-08-07

Similar Documents

Publication Publication Date Title
AR127157A1 (es) NUEVOS DERIVADOS DE BENZODIAZEPINA COMO MODULADORES ALOSTÉRICOS POSITIVOS DE GABAA g1
AR119943A1 (es) Compuestos heterocíclicos
AR120855A1 (es) Derivados de pirazolilo útiles como agentes anticancerígenos
AR118374A1 (es) Inhibidores de la proteína tirosina fosfatasa y métodos para usarlos
AR120697A1 (es) Inhibidores de braf como rompedores de la paradoja
AR119971A1 (es) Derivados de piridazin-3(2h)-ona fusionados con azol
AR110498A1 (es) DERIVADOS DE ISOXAZOLIL ÉTER COMO MODULADORES ALOSTÉRICOS POSITIVOS (PAM) DE RECEPTORES DE GABAA a5
AR121676A1 (es) DERIVADOS DE BENZODIAZEPINAS COMO PAM DE GABAA g1
AR119910A1 (es) DERIVADOS DE 4,4a,5,7,8,8a-HEXAHIDROPIRIDO[4,3-b][1,4]OXAZIN-3-ONA COMO INHIBIDORES DE MAGL
AR113888A1 (es) Derivados de indol macrocíclicos sustituidos
AR113886A1 (es) Derivados de indol macrocíclicos
AR116400A1 (es) Compuesto de imidazopiridinona
AR113887A1 (es) Derivados de indol macrocíclicos sustituidos con cloro
AR116905A1 (es) Derivados de ácido pirrolidino-2-carboxílico para tratar el dolor y afecciones relacionadas con el dolor
AR121840A1 (es) Compuestos herbicidas
AR116898A1 (es) DERIVADOS DE ARILSULFONILPIRROLCARBOXAMIDA COMO ACTIVADORES DE CANALES DE POTASIO Kv3
AR130125A1 (es) Método de preparación de glufosinato o derivados del mismo
AR118348A1 (es) 3-(2-bromo-4-alquinil-6-alcoxifenil)-3-pirrolin-2-onas y su uso como herbicidas
AR125365A1 (es) Derivados de 1h-pirazol como ligandos sigma
AR127255A1 (es) NUEVOS DERIVADOS DE BENZODIAZEPINA COMO GABAA g1 PAM
AR123700A1 (es) Preparación de derivados de benzoimidazolona como nuevos inhibidores de la diacilglicerol o-aciltransferasa 2
AR122336A1 (es) Compuestos heterocíclicos como inhibidores de delta-5 desaturasa y métodos de uso
AR125750A1 (es) Compuestos herbicidas
AR126442A1 (es) Inhibidores de map4k1
AR121282A1 (es) Moduladores de nampt