AR100794A1 - Derivados de [1,2,4]triazolo[4,3-a]pirimidin-6-carboxílico - Google Patents

Derivados de [1,2,4]triazolo[4,3-a]pirimidin-6-carboxílico

Info

Publication number
AR100794A1
AR100794A1 ARP150101843A ARP150101843A AR100794A1 AR 100794 A1 AR100794 A1 AR 100794A1 AR P150101843 A ARP150101843 A AR P150101843A AR P150101843 A ARP150101843 A AR P150101843A AR 100794 A1 AR100794 A1 AR 100794A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
hydrogen
group
nr3r7
Prior art date
Application number
ARP150101843A
Other languages
English (en)
Inventor
Andrew Heald Robert
Mark Sutton Jonathan
Capaldi Carmelida
Armani Elisabetta
Original Assignee
Chiesi Farm Spa
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 Chiesi Farm Spa filed Critical Chiesi Farm Spa
Publication of AR100794A1 publication Critical patent/AR100794A1/es

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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
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/14—Antitussive agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/008—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Que tienen propiedades inhibitorias de la elastasa de neutrófilos humana, y su uso en terapia. Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1), o una sal farmacéuticamente aceptable del mismo, donde A es CH o N; B es CH o N; D es CH o N; E es CH o N; R¹ es -CN o un grupo -C(O)-VR²; V se selecciona entre el grupo que consiste en -O-, -(CH₂)- y -NH-; R² es hidrógeno o -C₁₋₆ alquilo, opcionalmente sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en halógeno, OR³ y -NR³R⁷; R³ es hidrógeno o C₁₋₆ alquilo opcionalmente sustituido; R⁴ se selecciona entre -CF₃ y -CHF₂; R⁵ es un grupo seleccionado entre los compuestos del grupo de fórmulas (2); j es 0 o un entero en el rango de 1 a 4; y es 0 o un entero en el rango de 1 a 4; L y T son en forma independiente un anillo heterocicloalquilo de entre 4 y 8 miembros que tiene un grupo -X- en cualquiera de las posiciones libres; X se selecciona entre -O-, -S-, -S(O₂)- y -NR⁶; W se selecciona entre el grupo que consiste en -N(R³)-, -O-, -C(O)-, -OC(O)N(R³)-, -N(R³)C(O)N(R³)-, -C(O)N(R³)-, -NR³C(O)-, -SO₂-, -SO₂N(R³)-, -NR³S(O₂)-, -S-, -C(O)O-, -OC(O)-, C₁₋₆ alquileno opcionalmente sustituido, C₃₋₆ cicloalquileno opcionalmente sustituido y C₄₋₇ heterocicloalquileno opcionalmente sustituido; G es hidrógeno o se selecciona entre el grupo que consiste en halógeno, -CN, -N(R³)(R⁷), -OR³, -OC(O)OR³, -OC(O)NR³R⁷, -N(R³)C(N)N(R³)(R⁷), -N(R³)C(O)N(R³)(R⁷), -C(O)N(R³)(R⁷), -N(R³)C(O)R⁷, -S(O₂)R³, -S(O₂)N(R³)(R⁷), -N(R³)S(O₂)(R⁷), -SR³, -C(O)OR³, -OC(O)R³, C₁₋₆ alquilo opcionalmente sustituido, C₃₋₆ cicloalquilo opcionalmente sustituido y C₄₋₇ heterocicloalquilo opcionalmente monosustituido o bisustituido; Rᵃ es hidrógeno o se selecciona entre el grupo que consiste en -OH, -NH₂ y C₁₋₆ alquilo opcionalmente sustituido; R⁶ es hidrógeno o se selecciona entre el grupo que consiste en -S(O₂)R⁷, -CO₂R⁷, -CONR³R⁷, -SO₂NR³R⁷ y C₁₋₆ alquilo opcionalmente sustituido; R⁷ es hidrógeno o es C₁₋₆ alquilo opcionalmente sustituido; donde, salvo que se especifique lo contrario, opcionalmente sustituido significa opcionalmente sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en C₁₋₆ alquilo, C₁₋₆ alcoxi, C₁₋₆ hidroxialquilo, -OH, -NH₂, halógeno, -CF₃ y -OCF₃; -NR³R⁷ y sales farmacéuticamente aceptables del mismo, con las siguientes condiciones: cuando y es un entero en el rango de 1 a 4, W es -O- y j es 0, entonces G no es hidrógeno o C₁₋₆ alquilo opcionalmente sustituido con uno o más C₁₋₆ alcoxi; cuando y es un entero en el rango de 1 a 4, W es -N(R³)-, R³ es hidrógeno o C₁₋₆ alquilo y j es 0, entonces G no es hidrógeno o C₁₋₆ alquilo; cuando y es 0, W es -C(O)N(R³)-, R³ es hidrógeno o C₁₋₆ alquilo y j es 0, entonces G no es H o C₁₋₆ alquilo opcionalmente sustituido con -NR³R⁷, donde R³ y R⁷ son en forma independiente H o C₁₋₆ alquilo; cuando y es 0, W es -S(O₂)- y j es 0, entonces G no es C₁₋₆ alquilo opcionalmente sustituido con -OH; cuando y es 0, W es -S(O₂)N(R³)-, R³ es H y j es 0, entonces G no es hidrógeno; cuando y es 0, W es -S(O₂)N(R³)-, R³ es H o C₁₋₄ alquilo y j es 0 entonces G no es hidrógeno o C₁₋₆ alquilo.
ARP150101843A 2014-06-12 2015-06-10 Derivados de [1,2,4]triazolo[4,3-a]pirimidin-6-carboxílico AR100794A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP14172176 2014-06-12

Publications (1)

Publication Number Publication Date
AR100794A1 true AR100794A1 (es) 2016-11-02

Family

ID=50933039

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP150101843A AR100794A1 (es) 2014-06-12 2015-06-10 Derivados de [1,2,4]triazolo[4,3-a]pirimidin-6-carboxílico

Country Status (11)

Country Link
US (1) US9487528B2 (es)
EP (1) EP3154980B1 (es)
KR (1) KR20170012258A (es)
CN (1) CN106459065A (es)
AR (1) AR100794A1 (es)
CA (1) CA2951743A1 (es)
MA (1) MA39965A (es)
MX (1) MX2016016381A (es)
RU (1) RU2016148397A (es)
TW (1) TW201625627A (es)
WO (1) WO2015189362A1 (es)

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU650953B2 (en) 1991-03-21 1994-07-07 Novartis Ag Inhaler
GB0605469D0 (en) * 2006-03-17 2006-04-26 Argenta Discovery Ltd Multimers of heterocyclic compounds and their use
CA2657956C (en) 2006-05-04 2015-01-06 Argenta Discovery Limited Tetrahydropyrrolopyrimidinediones and their use as human neutrophil elastase inhibitors
US8198288B2 (en) 2006-05-04 2012-06-12 Pulmagen Therapeutics (Inflammation) Limited Tetrahydropyrrolopyrimidinediones and their use in therapy
GB201004179D0 (en) * 2010-03-12 2010-04-28 Pulmagen Therapeutics Inflamma Enzyme inhibitors
GB201004178D0 (en) 2010-03-12 2010-04-28 Pulmagen Therapeutics Inflamma Enzyme inhibitors
BR112014005669A2 (pt) * 2011-09-14 2017-04-04 Chiesi Farm Spa composto, composição farmacêutica e uso de um composto
CA2878792A1 (en) 2012-07-12 2014-01-16 Chiesi Farmaceutici S.P.A. Inhibition of enzymes
EA028507B1 (ru) 2012-12-18 2017-11-30 КЬЕЗИ ФАРМАЧЕУТИЧИ С.п.А. Соединения
RU2016123379A (ru) 2013-12-16 2017-12-19 КЬЕЗИ ФАРМАЧЕУТИЧИ С.п.А. Тетрагидротриазолопиримидиновые соединения в качестве ингибиторов нейтрофильной эластазы человека

Also Published As

Publication number Publication date
CN106459065A (zh) 2017-02-22
KR20170012258A (ko) 2017-02-02
MA39965A (fr) 2021-04-28
US20150353561A1 (en) 2015-12-10
EP3154980A1 (en) 2017-04-19
EP3154980B1 (en) 2021-08-04
TW201625627A (zh) 2016-07-16
WO2015189362A1 (en) 2015-12-17
CA2951743A1 (en) 2015-12-17
US9487528B2 (en) 2016-11-08
RU2016148397A (ru) 2018-07-18
MX2016016381A (es) 2017-05-01

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