CO2017000745A2 - Dihidropirimidinonas bicíclicas sustituidas y su uso como inhibidores de la actividad de elastasa neutrófila - Google Patents

Dihidropirimidinonas bicíclicas sustituidas y su uso como inhibidores de la actividad de elastasa neutrófila

Info

Publication number
CO2017000745A2
CO2017000745A2 CONC2017/0000745A CO2017000745A CO2017000745A2 CO 2017000745 A2 CO2017000745 A2 CO 2017000745A2 CO 2017000745 A CO2017000745 A CO 2017000745A CO 2017000745 A2 CO2017000745 A2 CO 2017000745A2
Authority
CO
Colombia
Prior art keywords
inhibitors
neutrophil elastase
substituted bicyclic
elastase activity
bicyclic dihydropyrimidinones
Prior art date
Application number
CONC2017/0000745A
Other languages
English (en)
Inventor
Stefan Peters
Thorsten Oost
Ralf Anderskewitz
Christian Gnamm
Holger Hoesch
Gerd Morschhaeuser
Uwe Joerg 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 CO2017000745A2 publication Critical patent/CO2017000745A2/es

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    • 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
    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (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)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Neurology (AREA)
  • Transplantation (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Esta invención se refiere a dihidropirimidinonas bicíclicas sustituidas de la Fórmula 1: y su uso como inhibidores de la actividad de elastasa neutrófila, composiciones farmacéuticas que las contienen, y métodos de uso de estas como agentes para el tratamiento de y/o la prevención de enfermedad pulmonar, gastrointestinal y genitourinaria, enfermedades inflamatorias de la piel y los ojos y otros trastornos autoinmunitarios y alérgicos, rechazo a aloinjerto, y enfermedades oncológicas.
CONC2017/0000745A 2014-07-31 2017-01-27 Dihidropirimidinonas bicíclicas sustituidas y su uso como inhibidores de la actividad de elastasa neutrófila CO2017000745A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14179288 2014-07-31
PCT/EP2015/067501 WO2016016365A1 (en) 2014-07-31 2015-07-30 Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity

Publications (1)

Publication Number Publication Date
CO2017000745A2 true CO2017000745A2 (es) 2017-04-10

Family

ID=51257371

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2017/0000745A CO2017000745A2 (es) 2014-07-31 2017-01-27 Dihidropirimidinonas bicíclicas sustituidas y su uso como inhibidores de la actividad de elastasa neutrófila

Country Status (32)

Country Link
US (1) US9475779B2 (es)
EP (2) EP3174861B1 (es)
JP (1) JP6345337B2 (es)
KR (1) KR102420210B1 (es)
CN (2) CN106660988B (es)
AP (1) AP2016009632A0 (es)
AU (1) AU2015295283B2 (es)
CA (1) CA2956745C (es)
CL (1) CL2017000117A1 (es)
CO (1) CO2017000745A2 (es)
CY (1) CY1121933T1 (es)
DK (1) DK3174861T3 (es)
EA (1) EA033263B1 (es)
ES (1) ES2740428T3 (es)
HR (1) HRP20191353T1 (es)
HU (1) HUE045530T2 (es)
IL (1) IL249687B (es)
LT (1) LT3174861T (es)
ME (1) ME03526B (es)
MX (1) MX2017001347A (es)
MY (1) MY182438A (es)
NZ (1) NZ727554A (es)
PE (1) PE20170524A1 (es)
PH (1) PH12017500114A1 (es)
PL (1) PL3174861T3 (es)
PT (1) PT3174861T (es)
RS (1) RS59040B1 (es)
SA (1) SA517380781B1 (es)
SG (1) SG11201700658UA (es)
SI (1) SI3174861T1 (es)
UA (1) UA118130C2 (es)
WO (1) WO2016016365A1 (es)

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EA201790282A1 (ru) 2017-07-31
EP3539952B1 (en) 2022-06-22
EA033263B1 (ru) 2019-09-30
CN107253933B (zh) 2021-10-26
SG11201700658UA (en) 2017-02-27
CA2956745A1 (en) 2016-02-04
CN107253933A (zh) 2017-10-17
MY182438A (en) 2021-01-25
ME03526B (me) 2020-04-20
IL249687A0 (en) 2017-02-28
US9475779B2 (en) 2016-10-25
EP3174861B1 (en) 2019-05-15
BR112017001554A2 (pt) 2017-11-21
AP2016009632A0 (en) 2016-12-31
US20160031829A1 (en) 2016-02-04
LT3174861T (lt) 2019-07-10
SI3174861T1 (sl) 2019-08-30
CL2017000117A1 (es) 2017-09-15
KR20170032465A (ko) 2017-03-22
MX2017001347A (es) 2017-04-27
ES2740428T3 (es) 2020-02-05
HUE045530T2 (hu) 2020-01-28
NZ727554A (en) 2022-09-30
EP3174861A1 (en) 2017-06-07
WO2016016365A1 (en) 2016-02-04
PH12017500114A1 (en) 2017-05-29
PE20170524A1 (es) 2017-05-19
CY1121933T1 (el) 2020-10-14
UA118130C2 (uk) 2018-11-26
RS59040B1 (sr) 2019-08-30
CA2956745C (en) 2023-03-14
DK3174861T3 (da) 2019-08-12
IL249687B (en) 2019-11-28
HRP20191353T1 (hr) 2019-11-01
KR102420210B1 (ko) 2022-07-13
PT3174861T (pt) 2019-09-04
AU2015295283B2 (en) 2019-12-19
JP2017525687A (ja) 2017-09-07
SA517380781B1 (ar) 2020-09-21
CN106660988B (zh) 2019-06-21
EP3539952A1 (en) 2019-09-18
PL3174861T3 (pl) 2019-11-29
JP6345337B2 (ja) 2018-06-20
CN106660988A (zh) 2017-05-10
AU2015295283A1 (en) 2017-01-12

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