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
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 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

    • 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
    • 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
    • A61K31/41961,2,4-Triazoles
    • 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pulmonology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (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
EP12176079.7 2012-07-12
EP12176079 2012-07-12
EP13158756.0 2013-03-12
EP13158756 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)

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* Cited by examiner, † Cited by third party
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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
US9440930B2 (en) 2014-07-31 2016-09-13 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
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
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)
BR112018074608B1 (pt) * 2016-05-31 2024-01-23 Chiesi Farmaceutici S.P.A Composto, composição farmacêutica e uso de um composto
WO2017207432A1 (en) * 2016-05-31 2017-12-07 Chiesi Farmaceutici S.P.A. Novel compounds
US11106356B2 (en) 2017-02-27 2021-08-31 Géza Bálint Smart device with a display that enables simultaneous multi-functional handling of the displayed information and/or data
CN118496198A (zh) 2019-07-23 2024-08-16 拜耳公司 作为农药的新的杂芳基-三唑化合物
PH12022550166A1 (en) 2019-07-23 2022-11-14 Bayer Ag 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
DK4041721T3 (da) 2019-10-09 2024-05-27 Bayer Ag Hidtil ukendte heteroaryltriazolforbindelser som pesticider
TW202128664A (zh) 2019-10-09 2021-08-01 德商拜耳廠股份有限公司 作為除害劑之新穎雜芳基三唑化合物
US20230117470A1 (en) * 2019-11-01 2023-04-20 Bristol-Myers Squibb Company Substituted pyrazole compounds as toll receptor inhibitors
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
ES2962498T3 (es) 2020-04-16 2024-03-19 Mereo Biopharma 4 Ltd Métodos que implican el inhibidor de elastasa de neutrófilos alvelestat para el tratamiento de enfermedades respiratorias mediadas por deficiencia de alfa-1 antitripsina
JP2023542789A (ja) * 2020-09-28 2023-10-12 シチュアン ケルン-バイオテック バイオファーマシューティカル カンパニー リミテッド ピラゾール化合物並びにその調製方法及び使用
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
KR20240090272A (ko) 2021-10-20 2024-06-21 메레오 바이오파마 4 리미티드 섬유화 치료에 사용하기 위한 호중구 엘라스테이스 억제제

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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2006038116A2 (en) 2004-10-07 2006-04-13 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
WO2007139952A2 (en) 2006-05-25 2007-12-06 Synta Pharmaceuticals Corp. Method for the preparation of triazole compounds with hsp90 modulating activity
EA017297B1 (ru) * 2007-11-06 2012-11-30 Астразенека Аб Некоторые производные 2-пиразинона и их применение в качестве ингибиторов нейтрофильной эластазы
PE20091953A1 (es) 2008-05-08 2010-01-09 Du Pont Azoles sustituidos como fungicidas
US8410128B2 (en) * 2008-06-20 2013-04-02 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
RU2015104644A (ru) 2016-08-27
AR091737A1 (es) 2015-02-25
WO2014009425A1 (en) 2014-01-16
KR20150031318A (ko) 2015-03-23
EP2872509A1 (en) 2015-05-20
IN2015DN00202A (enExample) 2015-06-12
CN104428300A (zh) 2015-03-18
EP2872509B1 (en) 2016-09-14
US20140018345A1 (en) 2014-01-16
CA2878792A1 (en) 2014-01-16
BR112015000507A2 (pt) 2017-06-27
US9199984B2 (en) 2015-12-01
RU2638537C2 (ru) 2017-12-14
HK1207078A1 (en) 2016-01-22

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