EA200870391A1 - Тетрагидропирролопиримидиндионы и их применение в качестве ингибиторов эластазы нейтрофилов человека - Google Patents

Тетрагидропирролопиримидиндионы и их применение в качестве ингибиторов эластазы нейтрофилов человека

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Publication number
EA200870391A1
EA200870391A1 EA200870391A EA200870391A EA200870391A1 EA 200870391 A1 EA200870391 A1 EA 200870391A1 EA 200870391 A EA200870391 A EA 200870391A EA 200870391 A EA200870391 A EA 200870391A EA 200870391 A1 EA200870391 A1 EA 200870391A1
Authority
EA
Eurasian Patent Office
Prior art keywords
inhibitors
tetrahydropyrropropyrimidindiones
elastasis
application
human
Prior art date
Application number
EA200870391A
Other languages
English (en)
Other versions
EA018061B1 (ru
Inventor
Николас Чарльз Рэй
Гарри Финч
Кристина Эдвардс
Элизабет О`Коннор
Original Assignee
Арджента Дискавери Лимитед
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
Priority claimed from GB0608844A external-priority patent/GB0608844D0/en
Priority claimed from GB0612544A external-priority patent/GB0612544D0/en
Application filed by Арджента Дискавери Лимитед filed Critical Арджента Дискавери Лимитед
Publication of EA200870391A1 publication Critical patent/EA200870391A1/ru
Publication of EA018061B1 publication Critical patent/EA018061B1/ru

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    • 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
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • 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
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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

Landscapes

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

Abstract

Соединения формулы (I) и их мультимеры являются ингибиторами активности человеческой нейтрофильной эластазы и обладают пользой при лечении, например, ХОБЛ, где все заместители являются такими, как определено в п. 1 формулы изобретения.
EA200870391A 2006-05-04 2007-05-03 Тетрагидропирролопиримидиндионы и их применение в качестве ингибиторов эластазы нейтрофилов человека EA018061B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0608844A GB0608844D0 (en) 2006-05-04 2006-05-04 Enzyme inhibitors
GB0612544A GB0612544D0 (en) 2006-06-23 2006-06-23 Enzyme inhibitors
PCT/GB2007/001638 WO2007129060A1 (en) 2006-05-04 2007-05-03 Tetrahydropyrrolopyrimidinediones and their use as human neutrophil elastase inhibitors

Publications (2)

Publication Number Publication Date
EA200870391A1 true EA200870391A1 (ru) 2009-06-30
EA018061B1 EA018061B1 (ru) 2013-05-30

Family

ID=38226415

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200870391A EA018061B1 (ru) 2006-05-04 2007-05-03 Тетрагидропирролопиримидиндионы и их применение в качестве ингибиторов эластазы нейтрофилов человека

Country Status (21)

Country Link
US (1) US8957082B2 (ru)
EP (1) EP2024367B1 (ru)
JP (1) JP4999920B2 (ru)
AT (1) ATE480543T1 (ru)
AU (1) AU2007246889B2 (ru)
BR (1) BRPI0711169A2 (ru)
CA (1) CA2657956C (ru)
CY (1) CY1111437T1 (ru)
DE (1) DE602007009095D1 (ru)
DK (1) DK2024367T3 (ru)
EA (1) EA018061B1 (ru)
HK (1) HK1130794A1 (ru)
IL (1) IL194843A (ru)
MX (1) MX2008013996A (ru)
NO (1) NO20084502L (ru)
NZ (1) NZ572250A (ru)
PL (1) PL2024367T3 (ru)
PT (1) PT2024367E (ru)
SI (1) SI2024367T1 (ru)
WO (1) WO2007129060A1 (ru)
ZA (1) ZA200809250B (ru)

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RU2622643C2 (ru) * 2011-09-14 2017-06-19 КЬЕЗИ ФАРМАЧЕУТИЧИ С.п.А. Производные тетрагидротриазолопиримидина в качестве ингибиторов нейтрофильной эластазы человека

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BRPI0711169A2 (pt) 2006-05-04 2011-08-23 Argenta Discovery Ltd tetrahidropirrolopiridinadionas e seu uso como inibidores de elastase neutrófilo humano
US8198288B2 (en) 2006-05-04 2012-06-12 Pulmagen Therapeutics (Inflammation) Limited Tetrahydropyrrolopyrimidinediones and their use in therapy
WO2009013444A1 (en) * 2007-07-25 2009-01-29 Argenta Discovery Limited Tetrahydropyrrolopyrimidinediones and their use as human neutrophil elastase inhibitors
TW200808771A (en) 2006-05-08 2008-02-16 Astrazeneca Ab Novel compounds II
TW200808763A (en) 2006-05-08 2008-02-16 Astrazeneca Ab Novel compounds I
US20110003858A1 (en) * 2006-09-04 2011-01-06 Bergstroem Lena Multimeric heterocyclic compounds useful as neutrophil elastase inhibitors
AU2008325288B2 (en) 2007-11-06 2011-12-22 Astrazeneca Ab Some 2-pyrazinone derivatives and their use as inhibitors of neutrophile elastase
WO2009060206A1 (en) * 2007-11-07 2009-05-14 Argenta Discovery Limited 3,4,6,7-tetrahydro-1h-pyrrolo[3,4-d]pyrimidine-2,5-diones and their therapeutic use
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GB0721866D0 (en) * 2007-11-07 2007-12-19 Argenta Discovery Ltd Pharmaceutical compounds having dual activities
PT2234985E (pt) 2007-12-20 2012-05-17 Bayer Pharma AG 4-(4-ciano-2-tioaril)-di-hidropirimidinona e sua utilização
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DE102007061766A1 (de) 2007-12-20 2009-06-25 Bayer Healthcare Ag 4-(4-Cyano-2-thioaryl)-dihydropyrimidinone und ihre Verwendung
DE102008052013A1 (de) 2008-10-17 2010-04-22 Bayer Schering Pharma Aktiengesellschaft 4-(4-Cyano-2-thioaryl)-dihydropyrimidinone und ihre Verwendung
GB0817429D0 (en) * 2008-09-23 2008-10-29 Argenta Discovery Ltd Enzyme inhibitors
DE102009004197A1 (de) 2009-01-09 2010-07-15 Bayer Schering Pharma Aktiengesellschaft Heterocyclisch anellierte Diaryldihydropyrimidin-Derivate und ihre Verwendung
EP2391629B1 (en) * 2009-01-30 2012-10-31 CHIESI FARMACEUTICI S.p.A. Dimeric pyrrolopyrimidinedione and its use in therapy of respiratory diseases
TW201036957A (en) 2009-02-20 2010-10-16 Astrazeneca Ab Novel salt 628
JP2013506649A (ja) 2009-10-02 2013-02-28 アストラゼネカ・アクチエボラーグ 好中球エラスターゼの阻害剤として使用する２−ピリドン化合物
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
DE102010030187A1 (de) 2010-06-16 2011-12-22 Bayer Schering Pharma Aktiengesellschaft 4-Cyan-2-sulfonylphenyl)pyrazolyl-substituierte Pyridinone und Pyrazinone und ihre Verwendung
US20140221335A1 (en) * 2013-02-06 2014-08-07 Boehringer Ingelheim International Gmbh Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
US9115093B2 (en) 2013-03-04 2015-08-25 Boehringer Ingelheim International Gmbh Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
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
USRE47493E1 (en) 2014-02-20 2019-07-09 Boehringer Ingelheim International Gmbh Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
US9487528B2 (en) 2014-06-09 2016-11-08 Chiesi Farmaceutici S.P.A. 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
US9458113B2 (en) * 2014-07-31 2016-10-04 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
US9657015B2 (en) 2014-07-31 2017-05-23 Boehringer Ingelheim International Gmbh Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
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KR20220079527A (ko) 2019-09-17 2022-06-13 메레오 바이오파마 4 리미티드 이식편 거부반응, 폐쇄성 세기관지염 증후군 및 이식편 대 숙주병의 치료에 사용하기 위한 알베레스타트
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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2622643C2 (ru) * 2011-09-14 2017-06-19 КЬЕЗИ ФАРМАЧЕУТИЧИ С.п.А. Производные тетрагидротриазолопиримидина в качестве ингибиторов нейтрофильной эластазы человека

Also Published As

Publication number Publication date
CY1111437T1 (el) 2015-08-05
AU2007246889A1 (en) 2007-11-15
PT2024367E (pt) 2010-12-03
AU2007246889B2 (en) 2011-03-10
ATE480543T1 (de) 2010-09-15
US20120202826A1 (en) 2012-08-09
MX2008013996A (es) 2009-01-14
CA2657956C (en) 2015-01-06
EA018061B1 (ru) 2013-05-30
HK1130794A1 (en) 2010-01-08
JP2009535389A (ja) 2009-10-01
NZ572250A (en) 2011-10-28
WO2007129060A1 (en) 2007-11-15
JP4999920B2 (ja) 2012-08-15
EP2024367B1 (en) 2010-09-08
PL2024367T3 (pl) 2011-05-31
DK2024367T3 (da) 2011-01-03
IL194843A0 (en) 2009-08-03
US8957082B2 (en) 2015-02-17
ZA200809250B (en) 2010-02-24
CA2657956A1 (en) 2007-11-15
SI2024367T1 (sl) 2011-04-29
BRPI0711169A2 (pt) 2011-08-23
EP2024367A1 (en) 2009-02-18
DE602007009095D1 (de) 2010-10-21
IL194843A (en) 2014-04-30
NO20084502L (no) 2008-11-26

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