EA201500816A1 - Замещенные бициклические дигидропиримидиноны и их применение в качестве ингибиторов активности нейтрофильной эластазы - Google Patents

Замещенные бициклические дигидропиримидиноны и их применение в качестве ингибиторов активности нейтрофильной эластазы

Info

Publication number
EA201500816A1
EA201500816A1 EA201500816A EA201500816A EA201500816A1 EA 201500816 A1 EA201500816 A1 EA 201500816A1 EA 201500816 A EA201500816 A EA 201500816A EA 201500816 A EA201500816 A EA 201500816A EA 201500816 A1 EA201500816 A1 EA 201500816A1
Authority
EA
Eurasian Patent Office
Prior art keywords
substituted bicyclic
elastasy
neutrofil
application
activity inhibitors
Prior art date
Application number
EA201500816A
Other languages
English (en)
Other versions
EA030569B1 (ru
Inventor
Кристиан Гнамм
Торстен Ост
Штефан Петерс
Хольгер Хёш
Уве Йёрг Рис
Original Assignee
Бёрингер Ингельхайм Интернациональ Гмбх
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 Бёрингер Ингельхайм Интернациональ Гмбх filed Critical Бёрингер Ингельхайм Интернациональ Гмбх
Publication of EA201500816A1 publication Critical patent/EA201500816A1/ru
Publication of EA030569B1 publication Critical patent/EA030569B1/ru

Links

Classifications

    • 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
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/06Heterocyclic 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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Данное изобретение относится к замещенным бициклическим дигидропиримидинонам формулы 1и к их применению в качестве ингибиторов активности нейтрофильной эластазы, к фармацевтическим композициям, которые их содержат, и способам их использования в качестве средств лечения и/или предотвращения лёгочных, желудочно-кишечных и мочеполовых заболеваний, воспалительных заболеваний кожи и глаз и других аутоиммунных и аллергических расстройств, отторжения аллотрансплантата и онкологических заболеваний.
EA201500816A 2013-02-06 2014-02-05 Замещенные бициклические дигидропиримидиноны и их применение в качестве ингибиторов активности нейтрофильной эластазы EA030569B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP13154256 2013-02-06
PCT/EP2014/052217 WO2014122160A1 (en) 2013-02-06 2014-02-05 Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity

Publications (2)

Publication Number Publication Date
EA201500816A1 true EA201500816A1 (ru) 2016-01-29
EA030569B1 EA030569B1 (ru) 2018-08-31

Family

ID=47681764

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201500816A EA030569B1 (ru) 2013-02-06 2014-02-05 Замещенные бициклические дигидропиримидиноны и их применение в качестве ингибиторов активности нейтрофильной эластазы

Country Status (39)

Country Link
US (4) US20140221335A1 (ru)
EP (1) EP2953943B1 (ru)
JP (1) JP6130519B2 (ru)
KR (1) KR102221201B1 (ru)
CN (4) CN106008369B (ru)
AP (1) AP2015008535A0 (ru)
AR (2) AR095164A1 (ru)
AU (1) AU2014214031B2 (ru)
BR (1) BR112015017929B1 (ru)
CA (1) CA2900308C (ru)
CL (1) CL2015002030A1 (ru)
CY (1) CY1119063T1 (ru)
DK (1) DK2953943T3 (ru)
EA (1) EA030569B1 (ru)
EC (1) ECSP15036282A (ru)
ES (1) ES2629023T3 (ru)
GE (1) GEP201706741B (ru)
HK (1) HK1211573A1 (ru)
HR (1) HRP20171040T1 (ru)
HU (1) HUE14705723T2 (ru)
IL (1) IL239472B (ru)
LT (1) LT2953943T (ru)
MA (1) MA38327B1 (ru)
ME (1) ME02697B (ru)
MX (1) MX361166B (ru)
NZ (1) NZ709041A (ru)
PE (1) PE20151429A1 (ru)
PH (1) PH12015501697B1 (ru)
PL (1) PL2953943T3 (ru)
PT (1) PT2953943T (ru)
RS (1) RS56063B1 (ru)
SG (1) SG11201505959QA (ru)
SI (1) SI2953943T1 (ru)
TN (1) TN2015000328A1 (ru)
TW (2) TWI634109B (ru)
UA (1) UA117007C2 (ru)
UY (1) UY35311A (ru)
WO (1) WO2014122160A1 (ru)
ZA (1) ZA201504257B (ru)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20140221335A1 (en) * 2013-02-06 2014-08-07 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
US9440930B2 (en) 2014-07-31 2016-09-13 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
EP3599234B1 (en) 2015-09-18 2021-04-07 Boehringer Ingelheim International GmbH Stereoselective process
KR20200020210A (ko) 2018-08-16 2020-02-26 서울대학교산학협력단 식물 추출물을 함유하는 호중구 엘라스타아제 억제용 조성물
GB201820450D0 (en) * 2018-12-14 2019-01-30 Z Factor Ltd Compound and its use for the treatment of alpha1-antitryspin deficiency
CN109331009A (zh) * 2018-12-24 2019-02-15 王萌萌 一种京尼平眼用制剂
BR112022004861A2 (pt) 2019-09-17 2022-06-07 Univ Duke Alvelestat para uso no tratamento de rejeição de transplante, síndrome de bronquiolite obliterante e doença de transplante versus hospedeiro
IL297211A (en) 2020-04-16 2022-12-01 Mereo Biopharma 4 Ltd Methods involving the neutrophil elastase inhibitor albalstat for the treatment of respiratory disease mediated by alpha-1 antitrypsin deficiency
GB202009074D0 (en) * 2020-06-15 2020-07-29 Z Factor Ltd Compound
GB202009069D0 (en) * 2020-06-15 2020-07-29 Z Factor Ltd Process
TW202325294A (zh) 2021-10-20 2023-07-01 英商梅瑞奧生物製藥4有限公司 用於治療纖維化之嗜中性球彈性蛋白酶抑制劑

Family Cites Families (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6228861B1 (en) 1995-11-16 2001-05-08 Synaptic Pharmaceutical Corporation Dihydropyrimidines and uses thereof
US6207665B1 (en) 1997-06-12 2001-03-27 Schering Aktiengesellschaft Piperazine derivatives and their use as anti-inflammatory agents
JP2001139556A (ja) * 1999-03-18 2001-05-22 Nippon Soda Co Ltd インデノピリジンおよびインデノピリミジン化合物並びにその製造法
JP2000273087A (ja) 1999-03-24 2000-10-03 Mitsui Chemicals Inc 非対称2−イミダゾリジノン類の製造方法
WO2003053930A1 (en) 2001-12-20 2003-07-03 Bayer Healthcare Ag 1,4-dihydro-1,4-diphenylpyridine derivatives
US7385076B2 (en) 2002-05-31 2008-06-10 Sun Pharmaceutical Industries Limited Process for the preparation of phenylcarbamates
GB0219896D0 (en) 2002-08-27 2002-10-02 Bayer Ag Dihydropyridine derivatives
WO2004020410A2 (en) 2002-08-27 2004-03-11 Bayer Healthcare Ag Dihydropyridinone derivatives as hne inhibitors
GB2392910A (en) 2002-09-10 2004-03-17 Bayer Ag 2-Oxopyrimidine derivatives and their use as human leukocyte elastase inhibitors
EP1539710B1 (en) 2002-09-10 2010-10-27 Bayer Schering Pharma Aktiengesellschaft Heterocyclic derivatives
AU2003282006C1 (en) 2002-09-10 2009-11-26 Bayer Schering Pharma Aktiengesellschaft Pyrimidinone derivatives as therapeutic agents against acute and chronic inflammatory ischaemic and remodelling processes
JP4825195B2 (ja) * 2004-02-26 2011-11-30 バイエル・シェーリング・ファルマ・アクチェンゲゼルシャフト 1,4−ジアリール−ジヒドロピリミジン−2オン化合物およびヒト好中球エラスターゼ阻害剤としてのそれらの使用
WO2005082864A1 (en) 2004-02-26 2005-09-09 Bayer Healthcare Ag 1,4-diaryl-dihydropyrimidin-2-ones and their use as human neutrophil elastase inhibitors
EP1568696A1 (en) 2004-02-26 2005-08-31 4Sc Ag Compounds as inhibitors of cell proliferation and viral infections
GB0502258D0 (en) 2005-02-03 2005-03-09 Argenta Discovery Ltd Compounds and their use
DE102005028845A1 (de) 2005-06-22 2006-12-28 Sanofi-Aventis Deutschland Gmbh Substituierte Heterocyclen, ihre Verwendung als Medikament sowie enthaltende pharmazeutische Zubereitungen
GB0512940D0 (en) 2005-06-24 2005-08-03 Argenta Discovery Ltd Compounds and their use
US20090176786A1 (en) 2005-10-20 2009-07-09 Masato Konobe Benzoylurea Compounds and Use Thereof
WO2009013444A1 (en) 2007-07-25 2009-01-29 Argenta Discovery Limited Tetrahydropyrrolopyrimidinediones and their use as human neutrophil elastase inhibitors
NZ572250A (en) * 2006-05-04 2011-10-28 Pulmagen Therapeutics Inflammation Ltd Tetrahydropyrrolopyrimidinediones and their use as human neutrophil elastase inhibitors
US8198288B2 (en) 2006-05-04 2012-06-12 Pulmagen Therapeutics (Inflammation) Limited Tetrahydropyrrolopyrimidinediones and their use in therapy
GB0608844D0 (en) * 2006-05-04 2006-06-14 Argenta Discovery Ltd Enzyme inhibitors
GB0610765D0 (en) 2006-05-31 2006-07-12 Proskelia Sas Imidazolidine derivatives, uses therefor, preparation thereof and compositions comprising such
US20100010024A1 (en) 2006-07-01 2010-01-14 Bayer Healthcare Ag Use of1,4-diaryl-dihydropyrimidine-2-on derivatives for treating pulmonary arterial hypertension
DE102006031314A1 (de) 2006-07-01 2008-01-03 Bayer Healthcare Aktiengesellschaft Verwendung von 1,4-Diaryl-dihydropyrimidin-2-on-Derivaten zur Behandlung der pulmonalen arteriellen Hyptertonie
JP2008273852A (ja) * 2007-04-26 2008-11-13 Kowa Co 3環性ピリミジノン誘導体及びこれを含有するstat6活性化阻害剤
WO2009037413A1 (en) 2007-09-19 2009-03-26 Argenta Discovery Limited Dimers of 5- [ (4-cyanophenyl) sulfinyl] -6-methyl-2-oxo-1- [3- (trifluoromethyl)phenyl] -1,2-dihydropyridine-3-carboxamide as inhibitors of human neutrophil elastase for treating respiratory diseases
GB0721866D0 (en) 2007-11-07 2007-12-19 Argenta Discovery Ltd Pharmaceutical compounds having dual activities
WO2009060158A1 (en) 2007-11-07 2009-05-14 Argenta Discovery Limited 4- (4-cyanophenyl) -1- (3-trifluoromethylphenyl) -3,4, 6, 7-tetrahydro-1h-pyrrolo [3, 4- d] pyrimidine-2, 5-dione derivatives and their use as human neutrophil elastase inhibitors
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
PL2234985T3 (pl) * 2007-12-20 2012-08-31 Bayer Ip Gmbh 4-(4-cyjano-2-tioarylo)-dihydropirymidynony i ich zastosowanie
DE102008022521A1 (de) 2008-05-07 2009-11-12 Bayer Schering Pharma Aktiengesellschaft 1,4-Diaryl-pyrimidopyridazin-2,5-dione und ihre Verwendung
DE102007061766A1 (de) 2007-12-20 2009-06-25 Bayer Healthcare Ag 4-(4-Cyano-2-thioaryl)-dihydropyrimidinone und ihre Verwendung
JP5559156B2 (ja) * 2008-06-02 2014-07-23 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 3,4−ジヒドロピリミジンtrpa1アンタゴニスト
UY32138A (es) * 2008-09-25 2010-04-30 Boehringer Ingelheim Int Amidas sustituidas del ácido 2-(2,6-dicloro-fenilamino)-6-fluoro-1-metil-1h-bencimidazol-5-carboxílico y sus sales farmacéuticamente aceptables
DE102009004197A1 (de) 2009-01-09 2010-07-15 Bayer Schering Pharma Aktiengesellschaft Heterocyclisch anellierte Diaryldihydropyrimidin-Derivate und ihre Verwendung
US8530487B1 (en) * 2009-01-29 2013-09-10 Hydra Biosciences, Inc. Compounds useful for treating disorders related to TRPA1
DE102009016553A1 (de) 2009-04-06 2010-10-07 Bayer Schering Pharma Aktiengesellschaft Sulfonamid- und Sulfoximin-substituierte Diaryldihydropyrimidinone und ihre Verwendung
EP2485728B1 (en) 2009-10-07 2013-07-10 Siena Biotech S.p.a. Wnt pathway antagonists
NZ601698A (en) 2010-01-08 2015-04-24 Catabasis Pharmaceuticals Inc Fatty acid fumarate derivatives and their uses
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
JP5709999B2 (ja) 2011-08-01 2015-04-30 大日本住友製薬株式会社 ウラシル誘導体およびその医薬用途
CA2848557A1 (en) 2011-09-14 2013-03-21 Chiesi Farmaceutici S.P.A. Tetrahydrotriazolopyrimidine derivatives as human neutrophil elastase inhibitors
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

Also Published As

Publication number Publication date
KR20150114575A (ko) 2015-10-12
KR102221201B1 (ko) 2021-03-03
TWI634109B (zh) 2018-09-01
MX361166B (es) 2018-11-29
JP6130519B2 (ja) 2017-05-17
MA38327A3 (fr) 2019-01-31
US9290459B1 (en) 2016-03-22
MX2015009512A (es) 2015-10-30
BR112015017929B1 (pt) 2023-01-24
CA2900308C (en) 2021-01-12
ZA201504257B (en) 2017-11-29
IL239472B (en) 2018-06-28
SG11201505959QA (en) 2015-08-28
IL239472A0 (en) 2015-07-30
AR095164A1 (es) 2015-09-30
ES2629023T3 (es) 2017-08-07
HRP20171040T1 (hr) 2017-10-06
CN104995186A (zh) 2015-10-21
BR112015017929A2 (pt) 2017-07-11
CN106045921B (zh) 2018-09-25
RS56063B1 (sr) 2017-10-31
CN106045920A (zh) 2016-10-26
ME02697B (me) 2017-10-20
US20160060230A1 (en) 2016-03-03
AR128259A2 (es) 2024-04-10
PH12015501697A1 (en) 2015-10-12
LT2953943T (lt) 2017-06-12
US20160060231A1 (en) 2016-03-03
HK1211573A1 (en) 2016-05-27
CN106008369A (zh) 2016-10-12
MA38327A2 (fr) 2016-12-30
PE20151429A1 (es) 2015-10-14
AP2015008535A0 (en) 2015-06-30
TW201444804A (zh) 2014-12-01
EA030569B1 (ru) 2018-08-31
CA2900308A1 (en) 2014-08-14
AU2014214031B2 (en) 2018-06-28
PH12015501697B1 (en) 2015-10-12
ECSP15036282A (es) 2016-01-29
SI2953943T1 (sl) 2017-07-31
PL2953943T3 (pl) 2017-10-31
HUE14705723T2 (hu) 2018-02-28
CL2015002030A1 (es) 2015-12-11
CY1119063T1 (el) 2018-01-10
CN106045921A (zh) 2016-10-26
CN106008369B (zh) 2019-06-21
US20160340319A1 (en) 2016-11-24
US9670166B2 (en) 2017-06-06
TW201831455A (zh) 2018-09-01
DK2953943T3 (en) 2017-07-03
EP2953943A1 (en) 2015-12-16
AU2014214031A1 (en) 2015-07-02
UA117007C2 (uk) 2018-06-11
MA38327B1 (fr) 2019-03-29
CN104995186B (zh) 2017-06-20
NZ709041A (en) 2020-01-31
UY35311A (es) 2014-08-29
WO2014122160A1 (en) 2014-08-14
TWI663156B (zh) 2019-06-21
JP2016511240A (ja) 2016-04-14
BR112015017929A8 (pt) 2019-11-05
EP2953943B1 (en) 2017-04-12
PT2953943T (pt) 2017-07-18
TN2015000328A1 (en) 2017-01-03
GEP201706741B (en) 2017-09-25
US20140221335A1 (en) 2014-08-07
CN106045920B (zh) 2018-10-19

Similar Documents

Publication Publication Date Title
EA201500816A1 (ru) Замещенные бициклические дигидропиримидиноны и их применение в качестве ингибиторов активности нейтрофильной эластазы
EA201790273A1 (ru) Флагеллиновые композиции и их применение
EA201792047A1 (ru) Новые соединения
SA518391170B1 (ar) مركبات باي أريل مفيدة لعلاج الأمراض البشرية في علم الأمراض، طب الأعصاب وعلم المناعة
UY35357A (es) Dihidropirimidinonas bicíclicas sustituidas y su uso como inhibidores de la actividad de elastasa n eutrofílica
EA201591616A1 (ru) Трифторметил-замещенные аннелированные пиримидины и их применение
EA201792028A1 (ru) Альфа-цинамидные соединения и композиции как ингибиторы hdac8
EA201892008A1 (ru) Соединения и способы лечения неврологических и сердечно-сосудистых состояний
EA201692049A1 (ru) Гетероарилзамещенные гетероциклилсульфоны
CY1121933T1 (el) Υποκατεστημενες δικυκλικες διυδροπυριμιδινονες και χρηση αυτων ως αναστολεις δραστικοτητας ελαστασης ουδετεροφιλου
UY34989A (es) 4-piridonas sustituidas y su uso como inhibidores de la actividad de elastasa de neutrófilos
EA201690783A1 (ru) Вещества, фармацевтическая композиция и методы применения при лечении воспалительных заболеваний
EA201391440A1 (ru) Производные пиразолопиримидина
EA201600288A1 (ru) Замещенные фенилаланиновые производные
EA201792610A1 (ru) Способ лечения неврологического заболевания
EA201692051A1 (ru) Арилзамещенные гетероциклилсульфоны
EA201992389A1 (ru) Замещенные n-арилэтил-2-аминохинолин-4-карбоксамиды и их применение
MX2017003016A (es) Derivados de piridazinona como inhibidores de las fosfoinositido-3-cinasas.
EA201790020A1 (ru) Соединения, фармацевтические композиции и их применение при лечении нейродегенеративных заболеваний
EA201992386A1 (ru) Замещенные n-арилэтил-2-арилхинолин-4-карбоксамиды и их применение
EA201790795A1 (ru) СОЕДИНЕНИЯ 4Н-ПИРИДО[1,2-a]ПИРИМИДИН-4-ОНА
WO2016083315A8 (en) Use of ox1r antagonists for the treatment of inflammatory bowel diseases
EA201401142A1 (ru) Замещенные 6-аминоникотинамиды, несущие он-содержащую группу, в качестве модуляторов kcnq2/3
EA201992673A1 (ru) ЛЕЧЕНИЕ ВОСПАЛИТЕЛЬНЫХ ЗАБОЛЕВАНИЙ С ПОМОЩЬЮ ИНГИБИТОРОВ АКТИВНОСТИ C5a
DK3423081T3 (da) Sammensætninger til brug i behandlingen af neurologisk sygdom

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ KG TJ TM