AR092205A1 - 4-piridonas sustituidas y su uso como inhibidores de la actividad de elastasa de neutrofilos - Google Patents

4-piridonas sustituidas y su uso como inhibidores de la actividad de elastasa de neutrofilos

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Publication number
AR092205A1
AR092205A1 ARP130102982A ARP130102982A AR092205A1 AR 092205 A1 AR092205 A1 AR 092205A1 AR P130102982 A ARP130102982 A AR P130102982A AR P130102982 A ARP130102982 A AR P130102982A AR 092205 A1 AR092205 A1 AR 092205A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
haloalkyl
ring
replaced
Prior art date
Application number
ARP130102982A
Other languages
English (en)
Inventor
Oost Thorsten
Gnamm Christian
Fiegen Dennis
Original Assignee
Boehringer Ingelheim Int
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 Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR092205A1 publication Critical patent/AR092205A1/es

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    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Composiciones farmacéuticas que los contienen y sus métodos de uso como agentes para el tratamiento y/o la prevención de enfermedades pulmonares, gastrointestinales y genitourinarias enfermedades inflamatorias de la piel y los ojos y otros trastornos autoinmunes y alérgicos rechazo de aloinjertos y enfermedades oncológicas. Reivindicación 1: Compuestos caracterizados porque tienen la fórmula (1) en donde A es fenilo o un heteroanillo aromático de cinco o seis miembros, en donde uno, dos o tres elementos están reemplazados por un elemento seleccionado, de modo independiente entre sí, del grupo que consiste en N, (O⁻)-N⁺, O y S; R¹ᵃ es un resto de fórmula (2) ó (3); R¹ᵃ.¹ es alquilo C₁₋₄, cicloalquilo C₃₋₆, haloalquilo C₁₋₄, H₂N-, alquil C₁₋₄-NH-, cicloalquil C₃₋₆-NH-, (alquil C₁₋₄)₂N-, (cicloalquil C₃₋₆)(alquil C₁₋₄)N-, azetidinilo, pirrolidinilo, piperidinilo, morfolinilo, piperazinilo, piperazinil-alquilo C₁₋₄, alquil C₁₋₄-O-NH-, (alquil C₁₋₄-O)(alquil C₁₋₄)N-; R¹ᵃ.² es H, NC-, O₂N-, alquil C₁₋₄-SO₂-, aril-SO₂-, (heteroanillo aromático)-SO₂-, alquil C₁₋₄-O-(O)C-, alquil C₁₋₄-(O)C-, cicloalquil C₃₋₆-(O)C-, H₂N-(O)C-, alquil C₁₋₄-NH-(O)C-, cicloalquil C₃₋₆-NH-(O)C-, (alquil C₁₋₄)₂N-(O)C-, (cicloalquil C₃₋₆)(alquil C₁₋₄)N-(O)C-, azetidinil-(O)C-, pirrolidinil-(O)C-, piperidinil-(O)C-, morfolinil-(O)C-, piperazinil-(O)C-, piperazinil-alquil C₁₋₄-(O)C-, alquilo C₁₋₄, cicloalquilo C₃₋₆, haloalquilo C₁₋₄, arilo, heteroarilo; R¹ᵇ es H, alquilo C₁₋₄, cicloalquilo C₃₋₆, haloalquilo C₁₋₄ o halógeno; o R¹ᵃ y R¹ᵇ son juntos alquileno C₂₋₄ que forman un heteroanillo carbocíclico; R² es alquilo C₁₋₆ o un residuo seleccionado del grupo que consiste en cicloalquilo C₃₋₆, en donde un elemento del anillo está opcionalmente reemplazado por O; fenil-alquilo C₁₋₄, (heteroanillo aromático)-alquilo C₁₋₄ y un heteroanillo aromático de cinco o seis miembros, en donde uno, dos o tres elementos están reemplazados por un elemento seleccionado, de modo independiente entre sí, del grupo que consiste en N, O y S; cada elemento de uno de los anillos está opcionalmente sustituido con uno o dos grupos seleccionados de alquilo C₁₋₄, cicloalquilo C₃₋₆, halógeno, haloalquilo C₁₋₄, alquil C₁₋₄-O-, alquil C₁₋₄-SO₂- o NC-; R³ es H o alquilo C₁₋₄; R⁴ es fenilo, un heteroanillo aromático de cinco o seis miembros que contiene uno, dos o tres átomos seleccionados de N, O y S; cada uno opcionalmente sustituido con uno o dos residuos seleccionados, de modo independiente entre sí, del grupo que consiste en alquilo C₁₋₄, cicloalquilo C₃₋₆, halógeno o haloalquilo C₁₋₄; R⁵ es H, alquilo C₁₋₄, haloalquilo C₁₋₄, cicloalquil C₃₋₆-; R⁶ es H o alquilo C₁₋₄; R⁷ es H o alquilo C₁₋₄; o R⁶ y R⁷ forman juntos un alquileno C₂₋₅, en donde un elemento del anillo formado está opcionalmente reemplazado por O; o una de sus sales farmacéuticamente aceptables.
ARP130102982A 2012-08-23 2013-08-22 4-piridonas sustituidas y su uso como inhibidores de la actividad de elastasa de neutrofilos AR092205A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP12181542 2012-08-23

Publications (1)

Publication Number Publication Date
AR092205A1 true AR092205A1 (es) 2015-04-08

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ID=46963420

Family Applications (1)

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ARP130102982A AR092205A1 (es) 2012-08-23 2013-08-22 4-piridonas sustituidas y su uso como inhibidores de la actividad de elastasa de neutrofilos

Country Status (7)

Country Link
US (2) US20140057926A1 (es)
EP (1) EP2888242B1 (es)
JP (1) JP6319747B2 (es)
AR (1) AR092205A1 (es)
TW (1) TW201422586A (es)
UY (1) UY34989A (es)
WO (1) WO2014029830A1 (es)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9657015B2 (en) 2014-07-31 2017-05-23 Boehringer Ingelheim International Gmbh Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
US9458113B2 (en) 2014-07-31 2016-10-04 Boehringer Ingelheim International Gmbh Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
US9475779B2 (en) 2014-07-31 2016-10-25 Boehringer Ingelheim International Gmbh Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
US9290457B2 (en) 2014-07-31 2016-03-22 Boehringer Ingelheim International Gmbh Substituted dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
US9440930B2 (en) 2014-07-31 2016-09-13 Boehringer Ingelheim International Gmbh Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
UY36547A (es) 2015-02-05 2016-06-01 Bayer Cropscience Ag Derivados heterocíclicos condensados bicíclicos sustituidos por 2-(het)arilo como pesticidas
EP3896066A3 (de) 2015-08-07 2021-12-08 Bayer CropScience Aktiengesellschaft 2-(het)aryl-substituierte kondensierte heterocyclen-derivate als schädlingsbekämpfungsmittel
BR112019023453A2 (pt) 2017-05-18 2020-06-16 Pi Industries Ltd. Compostos de formimidamidina úteis contra microorganismos fitopatogênicos
EP4031138A1 (en) 2019-09-17 2022-07-27 Mereo Biopharma 4 Limited Alvelestat for use in the treatment of graft rejection, bronchiolitis obliterans syndrome and graft versus host disease
AU2021256835A1 (en) 2020-04-16 2022-10-13 Mereo Biopharma 4 Limited Methods involving neutrophil elastase inhibitor alvelestat for treating respiratory disease mediated by alpha-1 antitrypsin deficiency
WO2023067103A1 (en) 2021-10-20 2023-04-27 Mereo Biopharma 4 Limited Neutrophil elastase inhibitors for use in the treatment of fibrosis

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TW200700392A (en) 2005-03-16 2007-01-01 Astrazeneca Ab Novel compounds
JP5114395B2 (ja) 2005-06-30 2013-01-09 プロシディオン・リミテッド Ｇｐｃｒアゴニスト
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TW200808771A (en) 2006-05-08 2008-02-16 Astrazeneca Ab Novel compounds II
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US20110224229A1 (en) 2010-03-10 2011-09-15 Astrazeneca Ab Novel Crystalline Form

Also Published As

Publication number Publication date
UY34989A (es) 2014-02-28
TW201422586A (zh) 2014-06-16
US9346794B1 (en) 2016-05-24
JP2015526453A (ja) 2015-09-10
JP6319747B2 (ja) 2018-05-09
EP2888242A1 (en) 2015-07-01
WO2014029830A1 (en) 2014-02-27
EP2888242B1 (en) 2016-07-13
US20160130265A1 (en) 2016-05-12
US20140057926A1 (en) 2014-02-27

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