AR101364A1 - DERIVATIVE OF AZOLCARBOXYL ACID - Google Patents

DERIVATIVE OF AZOLCARBOXYL ACID

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Publication number
AR101364A1
AR101364A1 ARP150102423A ARP150102423A AR101364A1 AR 101364 A1 AR101364 A1 AR 101364A1 AR P150102423 A ARP150102423 A AR P150102423A AR P150102423 A ARP150102423 A AR P150102423A AR 101364 A1 AR101364 A1 AR 101364A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
group optionally
groups
diseases
halogen atoms
Prior art date
Application number
ARP150102423A
Other languages
Spanish (es)
Original Assignee
Teijin Pharma 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 Teijin Pharma Ltd filed Critical Teijin Pharma Ltd
Publication of AR101364A1 publication Critical patent/AR101364A1/en

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Classifications

    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/433—Thidiazoles
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Abstract

La presente provee un compuesto representado por la fórmula (1) o una sal del mismo farmacéuticamente aceptable, que tiene una excelente actividad inhibidora de la xantina oxidasa y es útil como un agente terapéutico o como un agente preventivo para enfermedades asociadas con xantina oxidasa tales como gota, hiperuricemia, síndrome de lisis tumoral, cálculos urinarios, hipertensión, dislipidemia, diabetes, enfermedades cardiovasculares tales como arteriosclerosis o insuficiencia cardíaca, enfermedades renales tales como nefropatía diabética, enfermedades respiratorias tales como las enfermedades pulmonares obstructivas crónicas, enfermedades intestinales inflamatorias o enfermedades autoinmunes y un medicamento o una composición farmacéutica que comprende el compuesto o la sal como un ingrediente activo. Reivindicación 1: Un compuesto representado por la fórmula (1) o una sal del mismo farmacéuticamente aceptable [donde, R⁰ representa un resto de fórmula (2) ó (3); R¹ representa un grupo arilo opcionalmente sustituido con uno o una pluralidad de grupos alquilo C₁₋₆, grupos alcoxi C₁₋₆ o átomos de halógeno, OR, NRR los cuales pueden formar un anillo o SR, donde R y R cada uno representa independientemente un átomo de hidrógeno, un grupo alquilo C₁₋₈ opcionalmente sustituido con uno o una pluralidad de grupos alcoxi C₁₋₈, átomos de halógeno o grupos hidroxilo, un grupo arilo opcionalmente sustituido con uno o una pluralidad de grupos alquilo C₁₋₆, grupos alcoxi C₁₋₆, átomos de halógeno o grupos ciano o un grupo heteroarilo opcionalmente sustituido con uno o una pluralidad de grupos alquilo C₁₋₆, grupos alcoxi C₁₋₆ o átomos de halógeno; R² representa un átomo de hidrógeno, un grupo amino, o un grupo alquilo C₁₋₈ opcionalmente sustituido con uno o una pluralidad de átomos de halógeno; X¹ representa CR³ o un átomo de nitrógeno, donde R³ representa un átomo de hidrógeno o un átomo de halógeno; y el anillo A representa un heteroareno monocíclico de 5 ó 6 miembros opcionalmente sustituido con de 1 a 4 grupos seleccionados del grupo que consiste en un grupo alquilo C₁₋₆ opcionalmente sustituido con uno o una pluralidad de grupos alcoxi C₁₋₃ o un átomo de halógeno, un grupo alcoxi C₁₋₆ opcionalmente sustituido con uno o una pluralidad de átomos de halógeno y un átomo de halógeno].The present provides a compound represented by the formula (1) or a pharmaceutically acceptable salt thereof, which has excellent xanthine oxidase inhibitory activity and is useful as a therapeutic agent or as a preventive agent for diseases associated with xanthine oxidase such as gout, hyperuricemia, tumor lysis syndrome, urinary calculi, hypertension, dyslipidemia, diabetes, cardiovascular diseases such as arteriosclerosis or heart failure, kidney diseases such as diabetic nephropathy, respiratory diseases such as chronic obstructive pulmonary diseases, inflammatory bowel diseases or autoimmune diseases and a medicament or pharmaceutical composition comprising the compound or salt as an active ingredient. Claim 1: A compound represented by the formula (1) or a pharmaceutically acceptable salt thereof [wherein, R⁰ represents a moiety of formula (2) or (3); R¹ represents an aryl group optionally substituted with one or a plurality of C₁₋₆ alkyl groups, C₁₋₆ alkoxy groups or halogen atoms, OR, NRR which can form a ring or SR, where R and R each independently represents a hydrogen atom, a C₁₋₈ alkyl group optionally substituted with one or a plurality of C₁₋₈ alkoxy groups, halogen atoms or hydroxyl groups, an aryl group optionally substituted with one or a plurality of C₁₋₆ alkyl groups, alkoxy groups C₁₋₆, halogen atoms or cyano groups or a heteroaryl group optionally substituted with one or a plurality of C₁₋₆ alkyl groups, C₁₋₆ alkoxy groups or halogen atoms; R² represents a hydrogen atom, an amino group, or a C₁₋₈ alkyl group optionally substituted with one or a plurality of halogen atoms; X¹ represents CR³ or a nitrogen atom, where R³ represents a hydrogen atom or a halogen atom; and ring A represents a 5- or 6-membered monocyclic heteroarene optionally substituted with 1 to 4 groups selected from the group consisting of a C₁₋₆ alkyl group optionally substituted with one or a plurality of C₁₋₃ alkoxy groups or an atom of halogen, a C₁₋₆ alkoxy group optionally substituted with one or a plurality of halogen atoms and a halogen atom].

ARP150102423A 2014-07-30 2015-07-29 DERIVATIVE OF AZOLCARBOXYL ACID AR101364A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP2014155026A JP2017165653A (en) 2014-07-30 2014-07-30 Azole carboxylic acid derivative

Publications (1)

Publication Number Publication Date
AR101364A1 true AR101364A1 (en) 2016-12-14

Family

ID=55217597

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP150102423A AR101364A1 (en) 2014-07-30 2015-07-29 DERIVATIVE OF AZOLCARBOXYL ACID

Country Status (4)

Country Link
JP (1) JP2017165653A (en)
AR (1) AR101364A1 (en)
TW (1) TW201619141A (en)
WO (1) WO2016017699A1 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11344539B2 (en) 2016-02-19 2022-05-31 National University Corporation Tottori University Therapeutic or prophylactic drug for dementia
CN113024534B (en) * 2019-12-24 2023-03-21 武汉光谷亚太医药研究院有限公司 2-pyridylthiazole derivatives and use thereof

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992009279A1 (en) * 1990-11-30 1992-06-11 Teijin Limited 2-arylthiazole derivative and pharmaceutical composition containing the same
MX2009010491A (en) * 2007-04-11 2009-11-09 Kissei Pharmaceutical 5-membered heterocyclic derivative and use thereof for medical purposes.
EP2536699A2 (en) * 2010-02-19 2012-12-26 Cadila Healthcare Limited Substantially pure salts of febuxostat and processes for preparation thereof

Also Published As

Publication number Publication date
JP2017165653A (en) 2017-09-21
TW201619141A (en) 2016-06-01
WO2016017699A1 (en) 2016-02-04

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