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AR078521A1 - Compuesto pirazolotiazol - Google Patents

Compuesto pirazolotiazol

Info

Publication number
AR078521A1
AR078521A1 ARP100103603A ARP100103603A AR078521A1 AR 078521 A1 AR078521 A1 AR 078521A1 AR P100103603 A ARP100103603 A AR P100103603A AR P100103603 A ARP100103603 A AR P100103603A AR 078521 A1 AR078521 A1 AR 078521A1
Authority
AR
Argentina
Prior art keywords
group
optionally
alkyl
alkoxy
substituent
Prior art date
Application number
ARP100103603A
Other languages
English (en)
Inventor
Akira Inomata
Kodo Shikata
Taro Terauchi
Yoshinori Takahashi
Minako Hashizume
Kogyoku Shin
Kunitoshi Takeda
Original Assignee
Eisai R&D Man Co Ltd
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 Eisai R&D Man Co Ltd filed Critical Eisai R&D Man Co Ltd
Publication of AR078521A1 publication Critical patent/AR078521A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Reivindicacion 1: Un compuesto representado por la formula (1) o su sal aceptable para uso farmacologico, caracterizado porque X es un átomo de nitrogeno o CH, R1 es -A11-A12; A11 es un enlace simple o un grupo alquileno C1-6; A12 es (a) un átomo de hidrogeno, (b) un grupo alquilo C1-6 que tiene opcionalmente 1 a 3 sustituyentes seleccionados del grupo sustituyente A, o (C) un grupo cicloalquilo C3-6 que tiene opcionalmente 1 a 3 sustituyentes seleccionados del grupo sustituyente A; R2 es -A21-A22; A21 es un enlace simple o un grupo alquileno C1-6; A22 es (a) un átomo de hidrogeno, (b) un grupo alquilo C1-6 que tiene opcionalmente 1 a 3 sustituyentes seleccionados del grupo sustituyente A, o (c) un grupo cicloalquilo C3-6 que tiene opcionalmente 1 a 3 sustituyentes seleccionados del grupo sustituyente A; (d) un grupo heterocíclico no aromático seleccionado de un grupo tetrahidropiranilo, un grupo dihidropiranilo, un grupo tetrahidrofurilo, un grupo dioxanilo, un grupo hexahidrooxepinilo, un grupo oxabiciclo[3.1.0]hexilo, un grupo tetrahidrotienilo, un grupo ditianilo, y un grupo hexahidrotiepinilo, el cual tiene opcionalmente 1 a 3 sustituyentes seleccionados del grupo sustituyente A, o (e) un grupo heteroarilo seleccionado del grupo piridilo, un grupo pirimidinilo, y un grupo tiazolilo; R3 es (a) un grupo alquilo C1-6 que tiene opcionalmente 1 a 3 sustituyentes seleccionados del grupo sustituyente A, (b) un grupo cicloalquilo C3-6, (c) un grupo alcoxi C1-6 que tiene opcionalmente 1 a 3 sustituyentes seleccionados del grupo sustituyente A, (d) un grupo cicloalquilo C3-6-alquilo C1-6, (d) un grupo di-alquil C1-6-amino, (f) un átomo de halogeno, (g) un grupo ciano, (h) un grupo formilo, o (i) un grupo carboxilo; R4 es un átomo de hidrogeno, o un grupo alcoxi C1-6; R5 es un átomo de halogeno, un grupo alquilo C1-6, o un grupo alcoxi C1-6; R6 es un átomo de hidrogeno, un grupo alquilo C1-6, un grupo alcoxi C1-6, un grupo alquiltio C1-6; o un grupo alquilsulfinilo C1-6; y R7 es un grupo alquilo C1-6, un grupo alcoxi C1-6, o un grupo alquiltio C1-6; con la condicion de que R3 sea (a) un grupo alquilo C1-6 opcionalmente sustituido con un grupo hidroxilo, (b) un grupo cicloalquilo C3-6, (c) un grupo alcoxi C2-6 que tiene opcionalmente 1 a 3 sustituyentes seleccionados del grupo sustituyente A, (d) un grupo alcoxi C3-6 alcoxi C1-6, (e) un grupo alcoxi C1-2 alquilo C2-6, (f) un grupo di-alquil C1-6 amino, (g) un átomo de halogeno, (h) un grupo formilo o (i) un grupo carboxilo cuando X es CH, A12 es un grupo alquilo C1-6, o un grupo cicloalquilo C3-6 que tiene opcionalmente un grupo metilo, R2 es un grupo tetrahidrofurilmetilo, un grupo tetrahidropiranilmetilo, o un grupo tetrahidropiranilo, R6 es un átomo de hidrogeno, y R7 es un grupo metoxi; y donde el grupo sustituyente A consiste de un átomo de halogeno, un grupo hidroxilo, un grupo alquilo C1-6 y un grupo alcoxi C1-6.
ARP100103603A 2009-10-08 2010-10-04 Compuesto pirazolotiazol AR078521A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US24981709P 2009-10-08 2009-10-08
JP2009233989 2009-10-08
US35297010P 2010-06-09 2010-06-09
JP2010132008 2010-06-09

Publications (1)

Publication Number Publication Date
AR078521A1 true AR078521A1 (es) 2011-11-16

Family

ID=43855334

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100103603A AR078521A1 (es) 2009-10-08 2010-10-04 Compuesto pirazolotiazol

Country Status (6)

Country Link
US (1) US8530504B2 (es)
EP (1) EP2487178A4 (es)
JP (1) JPWO2011043381A1 (es)
AR (1) AR078521A1 (es)
TW (1) TW201127845A (es)
WO (1) WO2011043381A1 (es)

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MX389004B (es) 2014-01-21 2025-03-20 Neurocrine Biosciences Inc Antagonistas de receptor del factor de liberación de corticotropina (crf1) para el tratamiento de hiperplasia adrenal congénita.
ES2998110T3 (en) * 2017-04-27 2025-02-19 Elanco Animal Health Gmbh New bicyclic pyrazole derivatives
MA54395A (fr) 2018-12-07 2022-03-16 Neurocrine Biosciences Inc Antagoniste du récepteur crf1, formulations pharmaceutiques et formes solides correspondantes pour le traitement de l'hyperplasie surrénalienne congénitale
WO2021062246A1 (en) 2019-09-27 2021-04-01 Neurocrine Biosciences, Inc. Crf receptor antagonists and methods of use
CN113372317B (zh) * 2020-03-09 2023-09-22 南京药石科技股份有限公司 一种四氢-2h-吡喃-3-酮的工业化生产方法

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US20110086882A1 (en) 2011-04-14
US8530504B2 (en) 2013-09-10
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