CN104428300B - 酶的抑制 - Google Patents

酶的抑制 Download PDF

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Publication number
CN104428300B
CN104428300B CN201380036973.4A CN201380036973A CN104428300B CN 104428300 B CN104428300 B CN 104428300B CN 201380036973 A CN201380036973 A CN 201380036973A CN 104428300 B CN104428300 B CN 104428300B
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CN
China
Prior art keywords
phenyl
methyl
trifluoromethyl
base
pyridine
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CN201380036973.4A
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English (en)
Chinese (zh)
Other versions
CN104428300A (zh
Inventor
C·卡帕蒂
R·A·希尔德
N·C·瑞
J·M·萨顿
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Chiesi Farmaceutici SpA
Original Assignee
Chiesi Farmaceutici SpA
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Filing date
Publication date
Application filed by Chiesi Farmaceutici SpA filed Critical Chiesi Farmaceutici SpA
Publication of CN104428300A publication Critical patent/CN104428300A/zh
Application granted granted Critical
Publication of CN104428300B publication Critical patent/CN104428300B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—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
    • A61K31/41—Heterocyclic 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
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201380036973.4A 2012-07-12 2013-07-10 酶的抑制 Expired - Fee Related CN104428300B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP12176079 2012-07-12
EP12176079.7 2012-07-12
EP13158756 2013-03-12
EP13158756.0 2013-03-12
PCT/EP2013/064603 WO2014009425A1 (en) 2012-07-12 2013-07-10 Inhibition of enzymes

Publications (2)

Publication Number Publication Date
CN104428300A CN104428300A (zh) 2015-03-18
CN104428300B true CN104428300B (zh) 2016-11-09

Family

ID=48953361

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201380036973.4A Expired - Fee Related CN104428300B (zh) 2012-07-12 2013-07-10 酶的抑制

Country Status (10)

Country Link
US (1) US9199984B2 (enExample)
EP (1) EP2872509B1 (enExample)
KR (1) KR20150031318A (enExample)
CN (1) CN104428300B (enExample)
AR (1) AR091737A1 (enExample)
BR (1) BR112015000507A2 (enExample)
CA (1) CA2878792A1 (enExample)
IN (1) IN2015DN00202A (enExample)
RU (1) RU2638537C2 (enExample)
WO (1) WO2014009425A1 (enExample)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
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RU2016123379A (ru) 2013-12-16 2017-12-19 КЬЕЗИ ФАРМАЧЕУТИЧИ С.п.А. Тетрагидротриазолопиримидиновые соединения в качестве ингибиторов нейтрофильной эластазы человека
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
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
US9409870B2 (en) * 2014-12-15 2016-08-09 Chiesi Farmaceutici S.P.A. Compounds
EP3464269B1 (en) * 2016-05-31 2020-04-01 Chiesi Farmaceutici S.p.A. Heterocyclic compounds for use in the treatment of a hne related disease
US10172830B2 (en) 2016-05-31 2019-01-08 Chiesi Farmaceutici S.P.A. Pyrazolone compounds having human neutrophil elastase inhibitory properties
JP6990663B2 (ja) 2016-05-31 2022-01-13 シエッシ ファーマスーティシ エス．ピー．エー． ヒト好中球エラスターゼ阻害剤としてのイミダゾロン化合物
CN120578329A (zh) 2017-02-27 2025-09-02 格扎·巴林特 具有能实现所显示信息和/或数据的同时多功能操作的显示器的智能设备
JP7691973B2 (ja) 2019-07-23 2025-06-12 バイエル・アクチエンゲゼルシヤフト 殺有害生物剤としての新規なヘテロアリール－トリアゾール化合物
CA3148216A1 (en) 2019-07-23 2021-01-28 Bayer Aktiengesellschaft Novel heteroaryl-triazole compounds as pesticides
AU2020349353A1 (en) 2019-09-17 2022-04-14 Duke University Alvelestat for use in the treatment of graft rejection, bronchiolitis obliterans syndrome and graft versus host disease
CN117567338A (zh) 2019-10-09 2024-02-20 拜耳公司 作为农药的新的杂芳基三唑化合物
PH12022550862A1 (en) 2019-10-09 2023-04-24 Bayer Ag Novel heteroaryl-triazole compounds as pesticides
JP7652772B2 (ja) * 2019-11-01 2025-03-27 ブリストル－マイヤーズ スクイブ カンパニー 置換ピラゾール化合物
TW202134226A (zh) 2019-11-18 2021-09-16 德商拜耳廠股份有限公司 作為殺蟲劑之新穎雜芳基-三唑化合物
HUE064089T2 (hu) 2020-04-16 2024-02-28 Mereo Biopharma 4 Ltd Alvelesztat neutrofil elasztáz inhibitort alkalmazó módszerek alfa-1-antitripszin hiány által közvetített légzõszervi megbetegedés kezelésére
US12668593B2 (en) * 2020-09-28 2026-06-30 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Pyrazole compound and preparation method therefor and use thereof
CN113480486B (zh) * 2021-07-30 2022-05-24 赣南师范大学 一种3-胺基-1,2,4-三唑类衍生物及其制备方法和应用
AU2022373971A1 (en) 2021-10-20 2024-04-04 Mereo Biopharma 4 Limited Neutrophil elastase inhibitors for use in the treatment of fibrosis

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011039528A1 (en) * 2009-10-02 2011-04-07 Astrazeneca Ab 2-pyridone compounds used as inhibitors of neutrophil elastase
CN102131805A (zh) * 2008-06-20 2011-07-20 百时美施贵宝公司 用作激酶抑制剂的咪唑并吡啶和咪唑并吡嗪化合物
US20120004203A1 (en) * 2009-01-09 2012-01-05 Bayer Schering Pharma Aktiengesellschaft Triazolo and tetrazolo pyrimidine derivatives as hne inhibitors for treating copd

Family Cites Families (12)

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US4259504A (en) 1979-08-27 1981-03-31 American Cyanamid Company Substituted 1H-1,2,4-triazoles
US4451471A (en) 1981-03-18 1984-05-29 Ciba-Geigy Corporation Certain 2,4,5-tri-substituted thiazoles, pharmaceutical compositions containing same and methods of using same
US4576958A (en) 1984-01-23 1986-03-18 E. I. Du Pont De Nemours And Company Antihypertensive 4,5-diaryl-1H-imidazole-2-methanol derivatives
AU650953B2 (en) 1991-03-21 1994-07-07 Novartis Ag Inhaler
ES2184633B1 (es) 2001-08-07 2004-08-01 J. URIACH & CIA, S.A. Procedimiento para la preparacion de derivados de 4-(imidazol-1-il) bencenosulfonamida.
US6693116B2 (en) * 2001-10-08 2004-02-17 Hoffmann-La Roche Inc. Adenosine receptor ligands
EP1799680A2 (en) 2004-10-07 2007-06-27 Warner-Lambert Company LLC Triazolopyridine derivatives as antibacterial agents
US7902374B2 (en) 2005-05-06 2011-03-08 Universal Display Corporation Stability OLED materials and devices
TW200806637A (en) 2006-05-25 2008-02-01 Synta Pharmaceuticals Corp Synthesis of triazole compounds that modulate HSP90 activity
WO2009061271A1 (en) * 2007-11-06 2009-05-14 Astrazeneca Ab Some 2-pyrazinone derivatives and their use as inhibitors of neutrophile elastase
PE20091953A1 (es) 2008-05-08 2010-01-09 Du Pont Azoles sustituidos como fungicidas
WO2009155389A1 (en) * 2008-06-20 2009-12-23 Bristol-Myers Squibb Company Triazolopyridine compounds useful as kinase inhibitors

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102131805A (zh) * 2008-06-20 2011-07-20 百时美施贵宝公司 用作激酶抑制剂的咪唑并吡啶和咪唑并吡嗪化合物
US20120004203A1 (en) * 2009-01-09 2012-01-05 Bayer Schering Pharma Aktiengesellschaft Triazolo and tetrazolo pyrimidine derivatives as hne inhibitors for treating copd
WO2011039528A1 (en) * 2009-10-02 2011-04-07 Astrazeneca Ab 2-pyridone compounds used as inhibitors of neutrophil elastase

Also Published As

Publication number Publication date
RU2638537C2 (ru) 2017-12-14
US9199984B2 (en) 2015-12-01
HK1207078A1 (en) 2016-01-22
EP2872509B1 (en) 2016-09-14
US20140018345A1 (en) 2014-01-16
RU2015104644A (ru) 2016-08-27
WO2014009425A1 (en) 2014-01-16
KR20150031318A (ko) 2015-03-23
BR112015000507A2 (pt) 2017-06-27
EP2872509A1 (en) 2015-05-20
CN104428300A (zh) 2015-03-18
IN2015DN00202A (enExample) 2015-06-12
AR091737A1 (es) 2015-02-25
CA2878792A1 (en) 2014-01-16

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