PE20190176A1 - Compuestos de imidazolona como inhibidores de la elastasa de neutrofilos humana - Google Patents

Compuestos de imidazolona como inhibidores de la elastasa de neutrofilos humana

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Publication number
PE20190176A1
PE20190176A1 PE2018002811A PE2018002811A PE20190176A1 PE 20190176 A1 PE20190176 A1 PE 20190176A1 PE 2018002811 A PE2018002811 A PE 2018002811A PE 2018002811 A PE2018002811 A PE 2018002811A PE 20190176 A1 PE20190176 A1 PE 20190176A1
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PE
Peru
Prior art keywords
alkyl
inhibitors
imidazolone
alkylene
aryl
Prior art date
Application number
PE2018002811A
Other languages
English (en)
Inventor
Jonathan Mark Sutton
Robert Andrew Heald
Andrew Stephen Robert Jennings
Carmelida Capaldi
Elizabetta Armani
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 PE20190176A1 publication Critical patent/PE20190176A1/es

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41781,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/28Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Otolaryngology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Se refiere a un compuesto derivado de imidazolona de formula I o una sal farmaceuticamente aceptable del mismo, donde A se selecciona de pirazolilo, imidazolilo o triazolilo; X es un grupo (a), (b), (c), entre otros; y, w y n son un entero entre 1 y 4; m y t son 0 o un numero entero entre 1 y 4; Z y l son 0 o 1; R2 es -H o (C1-C4)alquilo lineal o ramificado; R3 es -(C1-C4)alquilo lineal o ramificado; R4 es -arilen-(C1-C4)alquilen-NRdRe, entre otros; R5 es aril-(C1-C4)alquilenoxi, (C1-C4)alquil-OC(O)-NH, entre otros; R6 es CF3C(O), aril-(C1-C4)alquileno, entre otros; Ra y Rb son alquilo C1-C4; Rd es H o alquilo C1-C4. Dicho compuesto es util en el tratamiento o prevencion de enfermedades tales como enfermedad pulmonar obstructiva cronica, bronquiectasia, bronquitis, entre otras, en la que esta involucrada la elastasa de neutrofilos humana (HNE)
PE2018002811A 2016-05-31 2017-05-26 Compuestos de imidazolona como inhibidores de la elastasa de neutrofilos humana PE20190176A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP16172196 2016-05-31
PCT/EP2017/062754 WO2017207430A1 (en) 2016-05-31 2017-05-26 Imidazolone compounds as human neutrophil elastase inhibitors

Publications (1)

Publication Number Publication Date
PE20190176A1 true PE20190176A1 (es) 2019-02-01

Family

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PE2018002811A PE20190176A1 (es) 2016-05-31 2017-05-26 Compuestos de imidazolona como inhibidores de la elastasa de neutrofilos humana

Country Status (24)

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US (2) US9802919B1 (es)
EP (1) EP3464273B9 (es)
JP (1) JP6990663B2 (es)
KR (1) KR102404031B1 (es)
CN (1) CN109311850B (es)
AR (1) AR108610A1 (es)
AU (1) AU2017272405C1 (es)
BR (1) BR112018074608B1 (es)
CL (1) CL2018003417A1 (es)
CO (1) CO2018012479A2 (es)
EA (1) EA036456B1 (es)
GE (2) GEAP202014924A (es)
IL (1) IL263089B (es)
MX (1) MX381423B (es)
MY (1) MY195210A (es)
NZ (1) NZ747313A (es)
PE (1) PE20190176A1 (es)
PH (1) PH12018502242A1 (es)
SA (1) SA518400429B1 (es)
SG (2) SG11201809671PA (es)
TW (1) TWI738786B (es)
UA (1) UA123109C2 (es)
WO (1) WO2017207430A1 (es)
ZA (1) ZA201806743B (es)

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CA3141826A1 (en) 2019-05-31 2020-12-03 Ikena Oncology, Inc. Tead inhibitors and uses thereof
CA3142351A1 (en) 2019-05-31 2020-12-03 Ikena Oncology, Inc. Tead inhibitors and uses thereof
JP7672641B2 (ja) 2019-09-17 2025-05-08 メレオ バイオファーマ 4 リミテッド 移植片拒絶反応、閉塞性細気管支炎症候群、及び移植片対宿主病の治療に使用するためのアルベレスタット
IL297211B2 (en) 2020-04-16 2025-12-01 Mereo Biopharma 4 Ltd Methods involving neutrophil elastase inhibitor alvelestat for treating respiratory disease mediated by alpha-1 antitrypsin deficiency
KR20240090272A (ko) 2021-10-20 2024-06-21 메레오 바이오파마 4 리미티드 섬유화 치료에 사용하기 위한 호중구 엘라스테이스 억제제
EP4447960A1 (en) * 2021-12-16 2024-10-23 Orixa Therapeutics LLC Small molecule inhibitors of pr3 and hne and uses thereof

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AU650953B2 (en) 1991-03-21 1994-07-07 Novartis Ag Inhaler
JPWO2003031414A1 (ja) * 2001-10-03 2005-01-20 日本曹達株式会社 新規なヘテロ環化合物および抗炎症薬
GB0605469D0 (en) * 2006-03-17 2006-04-26 Argenta Discovery Ltd Multimers of heterocyclic compounds and their use
TW200808771A (en) * 2006-05-08 2008-02-16 Astrazeneca Ab Novel compounds II
DE102009043260A1 (de) * 2009-09-28 2011-04-28 Merck Patent Gmbh Pyridinyl-imidazolonderivate
AU2010302420B2 (en) * 2009-10-02 2013-07-04 Astrazeneca Ab 2-pyridone compounds used as inhibitors of neutrophil elastase
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
JP2013177318A (ja) * 2010-06-30 2013-09-09 Dainippon Sumitomo Pharma Co Ltd ジヒドロピリミジノン誘導体およびその医薬用途
CA2878792A1 (en) * 2012-07-12 2014-01-16 Chiesi Farmaceutici S.P.A. Inhibition of enzymes
EP2935274B1 (en) 2012-12-18 2018-10-03 Chiesi Farmaceutici S.p.A. 3-oxo-2,3,5,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrimidine derivatives for the treatmetn of respiratory diseases
JP5799117B2 (ja) * 2013-02-05 2015-10-21 大日本住友製薬株式会社 ウラシル誘導体からなる医薬
CN105873933A (zh) 2013-12-16 2016-08-17 奇斯药制品公司 作为人中性白细胞弹性蛋白酶抑制剂的四氢三唑并嘧啶衍生物
US9409870B2 (en) * 2014-12-15 2016-08-09 Chiesi Farmaceutici S.P.A. Compounds

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AU2017272405B2 (en) 2020-09-10
CN109311850B (zh) 2021-11-19
AU2017272405A1 (en) 2018-11-22
SG11201809671PA (en) 2018-12-28
SA518400429B1 (ar) 2021-09-22
GEAP202014924A (en) 2020-03-25
UA123109C2 (uk) 2021-02-17
CN109311850A (zh) 2019-02-05
EP3464273B1 (en) 2020-04-08
WO2017207430A1 (en) 2017-12-07
MX2018014145A (es) 2019-03-11
CA3020435A1 (en) 2017-12-07
KR20190015232A (ko) 2019-02-13
MX381423B (es) 2025-03-12
US10023558B2 (en) 2018-07-17
EA036456B1 (ru) 2020-11-12
AU2017272405C1 (en) 2021-01-14
US20180009787A1 (en) 2018-01-11
JP2019520313A (ja) 2019-07-18
IL263089A (en) 2018-12-31
KR102404031B1 (ko) 2022-06-02
PH12018502242A1 (en) 2019-08-19
JP6990663B2 (ja) 2022-01-13
CO2018012479A2 (es) 2018-12-14
EP3464273B9 (en) 2020-10-21
TW201808934A (zh) 2018-03-16
BR112018074608A2 (pt) 2019-03-19
TWI738786B (zh) 2021-09-11
ZA201806743B (en) 2020-02-26
GEP20207130B (en) 2020-07-10
IL263089B (en) 2021-12-01
BR112018074608B1 (pt) 2024-01-23
US9802919B1 (en) 2017-10-31
MY195210A (en) 2023-01-11
NZ747313A (en) 2020-01-31
EA201892714A1 (ru) 2019-05-31
CL2018003417A1 (es) 2019-01-18
AR108610A1 (es) 2018-09-05
EP3464273A1 (en) 2019-04-10
SG10201912143UA (en) 2020-02-27

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