PE20151084A1 - Derivados de pirimidinona inhibidoras de la elastasa de neutrofilos humanos (hne) - Google Patents

Derivados de pirimidinona inhibidoras de la elastasa de neutrofilos humanos (hne)

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Publication number
PE20151084A1
PE20151084A1 PE2015000931A PE2015000931A PE20151084A1 PE 20151084 A1 PE20151084 A1 PE 20151084A1 PE 2015000931 A PE2015000931 A PE 2015000931A PE 2015000931 A PE2015000931 A PE 2015000931A PE 20151084 A1 PE20151084 A1 PE 20151084A1
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Peru
Prior art keywords
hne
alkyl
inhibiting human
pyrimidinone derivatives
derivatives inhibiting
Prior art date
Application number
PE2015000931A
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English (en)
Inventor
Lilian Alcaraz
Robert Andrew Heald
Jonathan Mark Sutton
Elisabetta Armani
Carmelida Capaldi
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Chiesi Farma Spa
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=50030225&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20151084(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Chiesi Farma Spa filed Critical Chiesi Farma Spa
Publication of PE20151084A1 publication Critical patent/PE20151084A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • 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
    • 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
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/02Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/02Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/07Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing oxygen atoms bound to the carbon skeleton
    • C07C309/08Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing oxygen atoms bound to the carbon skeleton containing hydroxy groups bound to the carbon skeleton
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/02Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/20Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic unsaturated carbon skeleton
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    • 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
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C47/00Compounds having —CHO groups
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D453/00Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Otolaryngology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Se refiere a derivados de 3-oxo-7-metil-8-(3-trifluorometil-fenil)-[1, 2, 4]triazolo[4, 3-a]pirimidina de formula (I), donde A, B y D son independientemente CH o N; R1 es H, (C1-C6)alquilo, fenil(C1-C6)alquilo, -CH2(CH2)OH, -CH2CONH2, -CH2SO2NH2, entre otros; R2 es -CONH2, C2-C6-alquenilo opcionalmente sustituido con OH o NH2, entre otros; y R3 es CN o -C(O)-XR4, donde X es -O-, -CH2- o -NH-; y R4 es H, (C1-C6)alquilo, entre otros. Los compuestos de la invencion son inhibidores de la elastasa de neutrofilos humanos (HNE), por lo cual son utiles en el tratamiento de enfermedades mediadas por la accion de la HNE, tales como enfermedad pulmonar obstructiva cronica (EPOC), fibrosis quistica, bronquiectasias, entre otros
PE2015000931A 2012-12-18 2013-12-16 Derivados de pirimidinona inhibidoras de la elastasa de neutrofilos humanos (hne) PE20151084A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12197767 2012-12-18
EP13158757 2013-03-12

Publications (1)

Publication Number Publication Date
PE20151084A1 true PE20151084A1 (es) 2015-08-07

Family

ID=50030225

Family Applications (1)

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PE2015000931A PE20151084A1 (es) 2012-12-18 2013-12-16 Derivados de pirimidinona inhibidoras de la elastasa de neutrofilos humanos (hne)

Country Status (33)

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US (2) US9365577B2 (es)
EP (1) EP2935274B1 (es)
JP (1) JP6390919B2 (es)
KR (1) KR102197721B1 (es)
CN (1) CN104870449B (es)
AU (1) AU2013363783B2 (es)
BR (1) BR112015014438B1 (es)
CA (1) CA2895352C (es)
CL (1) CL2015001678A1 (es)
CY (1) CY1122368T1 (es)
DK (1) DK2935274T3 (es)
EA (1) EA028507B1 (es)
ES (1) ES2700226T3 (es)
GE (1) GEP20186885B (es)
HK (1) HK1212985A1 (es)
HR (1) HRP20182007T1 (es)
IL (1) IL239447B (es)
LT (1) LT2935274T (es)
MX (1) MX2015007379A (es)
NZ (1) NZ709153A (es)
PE (1) PE20151084A1 (es)
PH (1) PH12015501043B1 (es)
PL (1) PL2935274T3 (es)
PT (1) PT2935274T (es)
RS (1) RS58129B1 (es)
SA (1) SA515360612B1 (es)
SG (2) SG10201703484YA (es)
SI (1) SI2935274T1 (es)
TN (1) TN2015000276A1 (es)
TW (1) TWI675837B (es)
UA (1) UA118021C2 (es)
WO (1) WO2014095700A1 (es)
ZA (1) ZA201504331B (es)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2592078A1 (en) 2011-11-11 2013-05-15 Almirall, S.A. New cyclohexylamine derivatives having beta2 adrenergic agonist and M3 muscarinic antagonist activities
TW201517906A (zh) 2013-07-25 2015-05-16 Almirall Sa 含有maba化合物和皮質類固醇之組合
CA2933725A1 (en) * 2013-12-16 2015-06-25 Chiesi Farmaceutici S.P.A. Tetrahydrotriazolopyrimidine derivatives as human neutrophil elastase inhibitors
US9487528B2 (en) 2014-06-09 2016-11-08 Chiesi Farmaceutici S.P.A. Compounds
WO2015188866A1 (en) * 2014-06-12 2015-12-17 Chiesi Farmaceutici S.P.A. Novel compounds
US9475779B2 (en) 2014-07-31 2016-10-25 Boehringer Ingelheim International Gmbh Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
US9657015B2 (en) 2014-07-31 2017-05-23 Boehringer Ingelheim International Gmbh Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
TW201617343A (zh) 2014-09-26 2016-05-16 阿爾米雷爾有限公司 具有β2腎上腺素促效劑及M3蕈毒拮抗劑活性之新穎雙環衍生物
US9890169B2 (en) 2015-12-14 2018-02-13 Chiesi Farmaceutici S.P.A. Triazolinone compounds as HNE inhibitors
AR108609A1 (es) 2016-05-31 2018-09-05 Chiesi Farm Spa Derivados de imidazolona y pirazolona como inhibidores de la elastasa de neutrófilos humana (hne)
SG10201912143UA (en) 2016-05-31 2020-02-27 Chiesi Farm Spa Imidazolone compounds as human neutrophil elastase inhibitors
EP3464268B1 (en) 2016-05-31 2020-03-11 Chiesi Farmaceutici S.p.A. Novel compounds
CN112969490B (zh) 2018-10-30 2024-07-12 奇斯药制品公司 用于向机械辅助呼吸患者施用药物的设备
EP4034079A1 (en) 2019-09-24 2022-08-03 Chiesi Farmaceutici S.p.A. Novel carrier particles for dry powder formulations for inhalation
KR20240124375A (ko) 2021-12-22 2024-08-16 키에시 파르마슈티시 엣스. 피. 에이. 호중구 엘라스타제 억제제로서 트라이아졸론 유도체 염
AU2022418176A1 (en) 2021-12-22 2024-08-01 Chiesi Farmaceutici S.P.A. Triazolone derivative salt as neutrophil elastase inhibitor

Family Cites Families (7)

* 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
SK132498A3 (en) * 1996-03-28 1999-08-06 Glaxo Group Ltd Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase
GB0608844D0 (en) * 2006-05-04 2006-06-14 Argenta Discovery Ltd Enzyme inhibitors
DE102009004197A1 (de) * 2009-01-09 2010-07-15 Bayer Schering Pharma Aktiengesellschaft Heterocyclisch anellierte Diaryldihydropyrimidin-Derivate und ihre Verwendung
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
WO2013037809A1 (en) * 2011-09-14 2013-03-21 Chiesi Farmaceutici S.P.A. Tetrahydrotriazolopyrimidine derivatives as human neutrophil elastase inhibitors

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PH12015501043A1 (en) 2015-07-27
IL239447A0 (en) 2015-07-30
PT2935274T (pt) 2018-12-05
CN104870449B (zh) 2018-11-06
TWI675837B (zh) 2019-11-01
EP2935274B1 (en) 2018-10-03
CN104870449A (zh) 2015-08-26
PH12015501043B1 (en) 2015-07-27
US9828382B2 (en) 2017-11-28
EA028507B1 (ru) 2017-11-30
TW201437210A (zh) 2014-10-01
BR112015014438A2 (pt) 2017-07-11
PL2935274T3 (pl) 2019-04-30
NZ709153A (en) 2019-01-25
US20140171414A1 (en) 2014-06-19
BR112015014438B1 (pt) 2023-02-14
MX2015007379A (es) 2015-09-23
DK2935274T3 (en) 2018-11-26
SA515360612B1 (ar) 2018-01-04
CA2895352A1 (en) 2014-06-26
SI2935274T1 (sl) 2018-12-31
SG10201703484YA (en) 2017-06-29
US20160251362A1 (en) 2016-09-01
GEP20186885B (en) 2018-08-10
HRP20182007T1 (hr) 2019-01-25
EP2935274A1 (en) 2015-10-28
CY1122368T1 (el) 2020-07-31
ES2700226T3 (es) 2019-02-14
IL239447B (en) 2018-06-28
UA118021C2 (uk) 2018-11-12
SG11201504737RA (en) 2015-07-30
AU2013363783B2 (en) 2018-02-08
LT2935274T (lt) 2018-12-10
AU2013363783A1 (en) 2015-07-02
KR102197721B1 (ko) 2021-01-05
RS58129B1 (sr) 2019-02-28
WO2014095700A1 (en) 2014-06-26
JP6390919B2 (ja) 2018-09-19
CL2015001678A1 (es) 2015-10-23
US9365577B2 (en) 2016-06-14
JP2016507488A (ja) 2016-03-10
TN2015000276A1 (fr) 2016-10-03
EA201590962A1 (ru) 2015-10-30
ZA201504331B (en) 2016-11-30
KR20150095692A (ko) 2015-08-21
CA2895352C (en) 2022-05-17
HK1212985A1 (zh) 2016-06-24

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