[go: up one dir, main page]

MA38327B1 - Dihydropyrimidinones bicycliques substituées et leur utilisation à titre d'inhibiteurs de l'activité élastase neutrophile - Google Patents

Dihydropyrimidinones bicycliques substituées et leur utilisation à titre d'inhibiteurs de l'activité élastase neutrophile

Info

Publication number
MA38327B1
MA38327B1 MA38327A MA38327A MA38327B1 MA 38327 B1 MA38327 B1 MA 38327B1 MA 38327 A MA38327 A MA 38327A MA 38327 A MA38327 A MA 38327A MA 38327 B1 MA38327 B1 MA 38327B1
Authority
MA
Morocco
Prior art keywords
inhibitors
neutrophil elastase
elastase activity
bicyclic substituted
dihydropyrimidinones
Prior art date
Application number
MA38327A
Other languages
English (en)
Other versions
MA38327A2 (fr
MA38327A3 (fr
Inventor
Stefan Peters
Christian Gnamm
Thorsten Oost
Holger Hoesch
Uwe Jörg Ries
Original Assignee
Boehringer Ingelheim Int
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 Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of MA38327A2 publication Critical patent/MA38327A2/fr
Publication of MA38327A3 publication Critical patent/MA38327A3/fr
Publication of MA38327B1 publication Critical patent/MA38327B1/fr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54—Heterocyclic 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
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/06—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/06—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/06—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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
    • 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
    • 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

Landscapes

  • 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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (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

Cette invention concerne des dihydropyrimidinones bicycliques substituées de formule (i) et leur utilisation à titre d'inhibiteurs de l'activité élastase neutrophile, des compositions les contenant, et des méthodes pour les utiliser à titre d'agents pour traiter et/ou prévenir les maladies pulmonaires, gastro-intestinales et génito-urinaires, les maladies inflammatoires de la peau et de l'œil et autres troubles auto-immuns et allergiques, le rejet d'allogreffe, et les maladies oncologiques.
MA38327A 2013-02-06 2014-02-05 Dihydropyrimidinones bicycliques substituées et leur utilisation à titre d'inhibiteurs de l'activité élastase neutrophile MA38327B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP13154256 2013-02-06
PCT/EP2014/052217 WO2014122160A1 (fr) 2013-02-06 2014-02-05 Dihydropyrimidinones bicycliques substituées et leur utilisation à titre d'inhibiteurs de l'activité élastase neutrophile

Publications (3)

Publication Number Publication Date
MA38327A2 MA38327A2 (fr) 2016-12-30
MA38327A3 MA38327A3 (fr) 2019-01-31
MA38327B1 true MA38327B1 (fr) 2019-03-29

Family

ID=47681764

Family Applications (1)

Application Number Title Priority Date Filing Date
MA38327A MA38327B1 (fr) 2013-02-06 2014-02-05 Dihydropyrimidinones bicycliques substituées et leur utilisation à titre d'inhibiteurs de l'activité élastase neutrophile

Country Status (39)

Country Link
US (4) US20140221335A1 (fr)
EP (1) EP2953943B1 (fr)
JP (1) JP6130519B2 (fr)
KR (1) KR102221201B1 (fr)
CN (4) CN106008369B (fr)
AP (1) AP2015008535A0 (fr)
AR (2) AR095164A1 (fr)
AU (1) AU2014214031B2 (fr)
BR (1) BR112015017929B1 (fr)
CA (1) CA2900308C (fr)
CL (1) CL2015002030A1 (fr)
CY (1) CY1119063T1 (fr)
DK (1) DK2953943T3 (fr)
EA (1) EA030569B1 (fr)
EC (1) ECSP15036282A (fr)
ES (1) ES2629023T3 (fr)
GE (1) GEP201706741B (fr)
HR (1) HRP20171040T1 (fr)
HU (1) HUE14705723T2 (fr)
IL (1) IL239472B (fr)
LT (1) LT2953943T (fr)
MA (1) MA38327B1 (fr)
ME (1) ME02697B (fr)
MX (1) MX361166B (fr)
MY (1) MY172167A (fr)
NZ (1) NZ709041A (fr)
PE (1) PE20151429A1 (fr)
PH (1) PH12015501697B1 (fr)
PL (1) PL2953943T3 (fr)
PT (1) PT2953943T (fr)
RS (1) RS56063B1 (fr)
SG (1) SG11201505959QA (fr)
SI (1) SI2953943T1 (fr)
TN (1) TN2015000328A1 (fr)
TW (2) TWI634109B (fr)
UA (1) UA117007C2 (fr)
UY (1) UY35311A (fr)
WO (1) WO2014122160A1 (fr)
ZA (1) ZA201504257B (fr)

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
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
US9458113B2 (en) 2014-07-31 2016-10-04 Boehringer Ingelheim International Gmbh Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
WO2017046355A1 (fr) * 2015-09-18 2017-03-23 Boehringer Ingelheim International Gmbh Procédé stéréosélectif
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
JP7672641B2 (ja) 2019-09-17 2025-05-08 メレオ バイオファーマ ４ リミテッド 移植片拒絶反応、閉塞性細気管支炎症候群、及び移植片対宿主病の治療に使用するためのアルベレスタット
MX2022012942A (es) 2020-04-16 2023-01-11 Mereo Biopharma 4 Ltd Metodos que involucran el inhibidor de la elastasa de neutrofilo alvelestat para el tratamiento de enfermedades respiratorias mediadas por deficiencia de alfa-1 antitripsina.
GB202009069D0 (en) * 2020-06-15 2020-07-29 Z Factor Ltd Process
GB202009074D0 (en) * 2020-06-15 2020-07-29 Z Factor Ltd Compound
IL312002A (en) 2021-10-20 2024-06-01 Mereo Biopharma 4 Ltd Neutrophil elastase inhibitors for use in the treatment of fibrosis

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
EP1458682B1 (fr) 2001-12-20 2006-08-30 Bayer HealthCare AG Derives de 1,4-dihydro-1,4-diphenylpyridine
AU2003263574A1 (en) 2002-05-31 2003-12-19 Patel, Hetalkumar, Virendrabhai A process for the preparation of phenylcarbamates
GB0219896D0 (en) 2002-08-27 2002-10-02 Bayer Ag Dihydropyridine derivatives
US7230017B2 (en) 2002-08-27 2007-06-12 Bayer Healthcare Ag Dihydropyridinone derivatives
EP1539710B1 (fr) 2002-09-10 2010-10-27 Bayer Schering Pharma Aktiengesellschaft Derives heterocycliques
BR0314186A (pt) 2002-09-10 2005-08-09 Bayer Healthcare Ag Derivados de pirimidinona como agentes terapêuticos contra processos inflamatórios, isquêmicos e remodeladores, agudos e crÈnicos
GB2392910A (en) 2002-09-10 2004-03-17 Bayer Ag 2-Oxopyrimidine derivatives and their use as human leukocyte elastase inhibitors
JP4825194B2 (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
ES2428503T3 (es) 2004-02-26 2013-11-08 Bayer Intellectual Property Gmbh 1,4-Diaril-dihidropirimidin-2-onas y su uso como inhibidores de elastasa de neutrófilos humanos
EP1568696A1 (fr) 2004-02-26 2005-08-31 4Sc Ag Composés comme inhibiteurs de prolifération de cellules et d'infections virales
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
BRPI0617513A2 (pt) 2005-10-20 2011-07-26 Sumitomo Chemical Co compostos de benzoilurÉia, processo para a produÇço e uso dos mesmos e mÉtodo para controlar pestes
WO2009013444A1 (fr) 2007-07-25 2009-01-29 Argenta Discovery Limited Tétrahydropyrrolopyrimidinediones et leur utilisation comme inhibiteurs de l'élastase des neutrophiles humains
GB0608844D0 (en) * 2006-05-04 2006-06-14 Argenta Discovery Ltd Enzyme inhibitors
US8198288B2 (en) 2006-05-04 2012-06-12 Pulmagen Therapeutics (Inflammation) Limited Tetrahydropyrrolopyrimidinediones and their use in therapy
PL2024367T3 (pl) * 2006-05-04 2011-05-31 Chiesi Farm Spa Tetrahydropirolopirymidynodiony i ich zastosowanie jako inhibitory ludzkiej elastazy neutrofilowej
GB0610765D0 (en) 2006-05-31 2006-07-12 Proskelia Sas Imidazolidine derivatives, uses therefor, preparation thereof and compositions comprising such
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
US20100010024A1 (en) 2006-07-01 2010-01-14 Bayer Healthcare Ag Use of1,4-diaryl-dihydropyrimidine-2-on derivatives for treating pulmonary arterial hypertension
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 (fr) 2007-09-19 2009-03-26 Argenta Discovery Limited Dimères de 5-[(4-cyanophényl)sulfinyl]-6-méthyl-2-oxo-1-[3-(trifluorométhyl)phényl]-1,2-dihydropyridine-3-carboxamide en tant qu'inhibiteurs de l'élastase des neutrophiles humains pour traiter des maladies respiratoires
GB0721866D0 (en) 2007-11-07 2007-12-19 Argenta Discovery Ltd Pharmaceutical compounds having dual activities
WO2009060158A1 (fr) 2007-11-07 2009-05-14 Argenta Discovery Limited Dérivés de 4-(4-cyanophényl)-1-(3-trifluorométhylphényl)-3,4,6,7-tétrahydro-1h-pyrrolo[3,4-d]pyrimidine-2,5-dione et leur utilisation en tant qu'inhibiteurs de l'élastase des neutrophiles humains
WO2009060206A1 (fr) 2007-11-07 2009-05-14 Argenta Discovery Limited 3,4,6,7-tétrahydro-1h-pyrrolo[3,4-d]pyrimidine-2,5-diones et leur utilisation thérapeutique
CN101903356B (zh) 2007-12-20 2013-05-22 拜耳知识产权有限责任公司 4-(4-氰基-2-硫代芳基)二氢嘧啶酮和它们的使用
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
ES2409262T3 (es) 2008-06-02 2013-06-26 Janssen Pharmaceutica, N.V. Antagonistas de TRPA1 de 3,4-dihidropirimidina
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
US8865704B2 (en) 2009-10-07 2014-10-21 Siena Biotech S.P.A. Wnt pathway antagonists
BR112012016879A2 (pt) 2010-01-08 2015-09-01 Catabasis Pharmaceuticals Inc Derivados de fumarato de acido graxo e seus usos
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
EP2740728A4 (fr) 2011-08-01 2015-04-01 Sumitomo Dainippon Pharma Co Ltd Dérivé d'uracile et utilisation de celui-ci pour des applications médicales
CA2848557A1 (fr) 2011-09-14 2013-03-21 Chiesi Farmaceutici S.P.A. Derives de tetrahydrotriazolopyrimidine en tant qu'inhibiteurs de la neutrophile elastase humaine
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
CN106045921A (zh) 2016-10-26
CN106008369B (zh) 2019-06-21
CN106008369A (zh) 2016-10-12
MY172167A (en) 2019-11-15
DK2953943T3 (en) 2017-07-03
CN104995186B (zh) 2017-06-20
MA38327A2 (fr) 2016-12-30
IL239472A0 (en) 2015-07-30
EA030569B1 (ru) 2018-08-31
NZ709041A (en) 2020-01-31
UY35311A (es) 2014-08-29
KR20150114575A (ko) 2015-10-12
KR102221201B1 (ko) 2021-03-03
HUE14705723T2 (hu) 2018-02-28
US20160060230A1 (en) 2016-03-03
US20140221335A1 (en) 2014-08-07
CN104995186A (zh) 2015-10-21
ME02697B (fr) 2017-10-20
CN106045920B (zh) 2018-10-19
ZA201504257B (en) 2017-11-29
AU2014214031A1 (en) 2015-07-02
LT2953943T (lt) 2017-06-12
JP6130519B2 (ja) 2017-05-17
BR112015017929A8 (pt) 2019-11-05
CL2015002030A1 (es) 2015-12-11
US20160340319A1 (en) 2016-11-24
US9670166B2 (en) 2017-06-06
CN106045921B (zh) 2018-09-25
PL2953943T3 (pl) 2017-10-31
SI2953943T1 (sl) 2017-07-31
PH12015501697B1 (en) 2018-12-14
EA201500816A1 (ru) 2016-01-29
PE20151429A1 (es) 2015-10-14
CN106045920A (zh) 2016-10-26
MX2015009512A (es) 2015-10-30
RS56063B1 (sr) 2017-10-31
PT2953943T (pt) 2017-07-18
US9290459B1 (en) 2016-03-22
MX361166B (es) 2018-11-29
EP2953943B1 (fr) 2017-04-12
ECSP15036282A (es) 2016-01-29
BR112015017929A2 (pt) 2017-07-11
AU2014214031B2 (en) 2018-06-28
TWI634109B (zh) 2018-09-01
EP2953943A1 (fr) 2015-12-16
US20160060231A1 (en) 2016-03-03
AR128259A2 (es) 2024-04-10
TW201444804A (zh) 2014-12-01
SG11201505959QA (en) 2015-08-28
AP2015008535A0 (en) 2015-06-30
GEP201706741B (en) 2017-09-25
PH12015501697A1 (en) 2015-10-12
ES2629023T3 (es) 2017-08-07
TN2015000328A1 (en) 2017-01-03
WO2014122160A1 (fr) 2014-08-14
CA2900308A1 (fr) 2014-08-14
BR112015017929B1 (pt) 2023-01-24
UA117007C2 (uk) 2018-06-11
AR095164A1 (es) 2015-09-30
JP2016511240A (ja) 2016-04-14
CY1119063T1 (el) 2018-01-10
MA38327A3 (fr) 2019-01-31
TW201831455A (zh) 2018-09-01
HRP20171040T1 (hr) 2017-10-06
HK1211573A1 (en) 2016-05-27
CA2900308C (fr) 2021-01-12
TWI663156B (zh) 2019-06-21
IL239472B (en) 2018-06-28

Similar Documents

Publication Publication Date Title
MA38327A2 (fr) Dihydropyrimidinones bicycliques substituées et leur utilisation à titre d'inhibiteurs de l'activité élastase neutrophile
EA201792047A1 (ru) Новые соединения
MA34591B1 (fr) Dérivés de benzimidazole utilisés comme inhibiteurs de pi3 kinase
MX2015005015A (es) Inhibidores heteroarilo de pde4.
EA201591689A1 (ru) НОВЫЕ N-АЦИЛ-(3-ЗАМЕЩЕННЫЕ)-(8-ЗАМЕЩЕННЫЕ)-5,6-ДИГИДРО[1,2,4]ТРИАЗОЛО[4,3-a]ПИРАЗИНЫ КАК СЕЛЕКТИВНЫЕ АНТАГОНИСТЫ РЕЦЕПТОРА NK-3, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И МЕТОДЫ ИСПОЛЬЗОВАНИЯ ПРИ РАССТРОЙСТВАХ,ОПОСРЕДОВАННЫХ РЕЦЕПТОРОМ NK-3
GEP20166554B (en) Nitrogenated heterocyclic compound
EA201890827A1 (ru) Конденсированные производные пиразола в качестве ингибиторов киназы
MA44948A1 (fr) Inhibiteurs de bace 1
PH12015501586A1 (en) 2,3-dihydroimidazol[1,2-c]pyrimidin-5(1h)-one based lipoprotein-associated phospholipase a2 (lp-pla2) inhibitors
CY1121933T1 (el) Υποκατεστημενες δικυκλικες διυδροπυριμιδινονες και χρηση αυτων ως αναστολεις δραστικοτητας ελαστασης ουδετεροφιλου
MX356163B (es) Anilinas sustituidas como antagonistas de ccr(4).
EP2563794A4 (fr) Inhibiteurs de l'activité protéine tyrosine kinase et leurs applications au traitement de troubles ophtalmiques
MA39533B1 (fr) Composés, composition pharmaceutique et leur utilisation dans le traitement de maladies neurodégénératives
EA201890826A1 (ru) Конденсированные производные пиридина в качестве ингибиторов киназы
EA201790795A1 (ru) СОЕДИНЕНИЯ 4Н-ПИРИДО[1,2-a]ПИРИМИДИН-4-ОНА
MA45537B1 (fr) 1h-pyrazolo [4,3-b]pyridines en tant qu'inhibiteurs de pde1
MA44969B1 (fr) 5,6,7,8-tétrahydro[1,2,4]triazolo[4,3- a]pyridin-3(2h)-ones et 2,5,6,7-tétrahydro-3h-pyrrolo[2,1 -c][1,2,4]triazol-3-ones substituées et leur utilisation
MA39260A1 (fr) (benzyl-cyano-méthyl)-amides substitués de l'acide 2-aza-bicyclo[2.2.1]heptane-3-carboxylique utilisés comme inhibiteurs de la cathépsine c
HK1228398A1 (en) Protein kinase inhibitors
MA40553B1 (fr) Derives de pyrimidine eventuellement condensee utiles dans le traitement de maladies inflammatoires, metaboliques, oncologiques et auto-immunes
GEP201606554B (en) Nitrogenated heterocyclic compound
MA38473B1 (fr) (benzyl-cyano-méthyl)-amides substitués de l'acide 2-aza-bicyclo[2.2.1]heptane-3-carboxylique utilisés comme inhibiteurs de la cathépsine c
HK1228397A1 (en) Protein kinase inhibitors