JP6484327B2 - 置換二環式ジヒドロピリミジノン及び好中球エラスターゼ活性の阻害薬としてのそれらの使用 - Google Patents
置換二環式ジヒドロピリミジノン及び好中球エラスターゼ活性の阻害薬としてのそれらの使用 Download PDFInfo
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- JP6484327B2 JP6484327B2 JP2017505234A JP2017505234A JP6484327B2 JP 6484327 B2 JP6484327 B2 JP 6484327B2 JP 2017505234 A JP2017505234 A JP 2017505234A JP 2017505234 A JP2017505234 A JP 2017505234A JP 6484327 B2 JP6484327 B2 JP 6484327B2
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- 0 CC(C*)CC*CCc1cc(*)ccc1[C@](C(C(CCC1)=O)=C1N1c2cccc(C(F)(F)F)c2)N(C)C1=O Chemical compound CC(C*)CC*CCc1cc(*)ccc1[C@](C(C(CCC1)=O)=C1N1c2cccc(C(F)(F)F)c2)N(C)C1=O 0.000 description 1
- JCUDBPCHKXCCCV-UHFFFAOYSA-N CS(c1cc(C#N)ccc1C(C(C(CCC1)=O)=C1N1c2cc(C(F)(F)F)ccc2)NC1=O)(=O)=O Chemical compound CS(c1cc(C#N)ccc1C(C(C(CCC1)=O)=C1N1c2cc(C(F)(F)F)ccc2)NC1=O)(=O)=O JCUDBPCHKXCCCV-UHFFFAOYSA-N 0.000 description 1
Classifications
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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
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
- C07D239/80—Oxygen atoms
- C07D239/82—Oxygen atoms with an aryl radical attached in position 4
-
- 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
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- 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
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- 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
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- 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
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- 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
- A61P11/08—Bronchodilators
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- 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
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- 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
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- 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]
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- 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
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- 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
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- 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
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- 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
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- 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
- A61P37/08—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
- A61P9/12—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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pulmonology (AREA)
- Obesity (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Child & Adolescent Psychology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Endocrinology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Gastroenterology & Hepatology (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14179261 | 2014-07-31 | ||
| EP14179261.4 | 2014-07-31 | ||
| PCT/EP2015/067506 WO2016016368A1 (en) | 2014-07-31 | 2015-07-30 | Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017522350A JP2017522350A (ja) | 2017-08-10 |
| JP2017522350A5 JP2017522350A5 (enExample) | 2018-07-26 |
| JP6484327B2 true JP6484327B2 (ja) | 2019-03-13 |
Family
ID=51257368
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017505234A Active JP6484327B2 (ja) | 2014-07-31 | 2015-07-30 | 置換二環式ジヒドロピリミジノン及び好中球エラスターゼ活性の阻害薬としてのそれらの使用 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US9440930B2 (enExample) |
| EP (1) | EP3174862B1 (enExample) |
| JP (1) | JP6484327B2 (enExample) |
| WO (1) | WO2016016368A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| USRE47493E1 (en) | 2014-02-20 | 2019-07-09 | Boehringer Ingelheim International Gmbh | Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
| US9856232B1 (en) | 2017-06-20 | 2018-01-02 | King Saud University | Dihydropyrimidinone derivatives |
| US10047071B1 (en) | 2018-01-15 | 2018-08-14 | King Saud University | Dihydropyrimidinone derivatives |
| US10111873B1 (en) | 2018-01-17 | 2018-10-30 | King Saud University | Dihydropyrimidinone derivatives |
| 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 |
| SI4106757T1 (sl) | 2020-04-16 | 2023-11-30 | Mereo Biopharma 4 Limited | Postopki, ki vključujejo zaviralec nevtrofilne elastaze alvelestat, za zdravljenje bolezni dihal, ki jo sproži pomanjkanje antitripsina alfa-1 |
| 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 (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4486817B2 (ja) | 2001-12-20 | 2010-06-23 | 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−ジヒドロ−1,4−ジフェニルピリジン誘導体 |
| GB0219896D0 (en) | 2002-08-27 | 2002-10-02 | Bayer Ag | Dihydropyridine derivatives |
| JP4619122B2 (ja) | 2002-08-27 | 2011-01-26 | 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 | Hneインヒビターとしてのジヒドロピリジノン誘導体 |
| MXPA05002644A (es) | 2002-09-10 | 2005-09-20 | Bayer Healthcare Ag | Derivados de pirimidinona como agentes terapeuticos contra procesos de remodelacion, isquemicos e inflamatorios agudos y cronicos. |
| WO2004024701A1 (en) | 2002-09-10 | 2004-03-25 | Bayer Healthcare Ag | Heterocyclic derivatives |
| GB2392910A (en) | 2002-09-10 | 2004-03-17 | Bayer Ag | 2-Oxopyrimidine derivatives and their use as human leukocyte elastase inhibitors |
| ES2394177T3 (es) | 2004-02-26 | 2013-01-23 | Bayer Intellectual Property Gmbh | 1,4-diaril-dihidropirimidin-2-onas y su uso como inhibidores de elastasa de neutrófilos humanos |
| WO2005082863A2 (en) | 2004-02-26 | 2005-09-09 | Bayer Healthcare Ag | 1,4 diaryl-dihydropyrimidin-2 ones and their use as a human neutrophil elastase inhibitors |
| GB0502258D0 (en) | 2005-02-03 | 2005-03-09 | Argenta Discovery Ltd | Compounds and their use |
| GB0512940D0 (en) | 2005-06-24 | 2005-08-03 | Argenta Discovery Ltd | Compounds and their use |
| US8198288B2 (en) | 2006-05-04 | 2012-06-12 | Pulmagen Therapeutics (Inflammation) Limited | Tetrahydropyrrolopyrimidinediones and their use in therapy |
| DE602007009095D1 (de) * | 2006-05-04 | 2010-10-21 | Pulmagen Therapeutics Inflamma | Tetrahydropyrrolopyrimidindione und ihre verwendung als inhibitoren der humanen neutrophilen elastase |
| WO2009013444A1 (en) | 2007-07-25 | 2009-01-29 | Argenta Discovery Limited | Tetrahydropyrrolopyrimidinediones and their use as human neutrophil elastase inhibitors |
| 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 |
| 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 |
| DE102007061766A1 (de) | 2007-12-20 | 2009-06-25 | Bayer Healthcare Ag | 4-(4-Cyano-2-thioaryl)-dihydropyrimidinone und ihre Verwendung |
| DE102008022521A1 (de) | 2008-05-07 | 2009-11-12 | Bayer Schering Pharma Aktiengesellschaft | 1,4-Diaryl-pyrimidopyridazin-2,5-dione und ihre Verwendung |
| SG186679A1 (en) | 2007-12-20 | 2013-01-30 | Bayer Schering Pharma Ag | 4-(4-cyano-2-thioaryl)dihydropyrimidinones and use thereof |
| DE102009004197A1 (de) | 2009-01-09 | 2010-07-15 | Bayer Schering Pharma Aktiengesellschaft | Heterocyclisch anellierte Diaryldihydropyrimidin-Derivate und ihre Verwendung |
| DE102009016553A1 (de) | 2009-04-06 | 2010-10-07 | Bayer Schering Pharma Aktiengesellschaft | Sulfonamid- und Sulfoximin-substituierte Diaryldihydropyrimidinone und ihre Verwendung |
| GB201004178D0 (en) | 2010-03-12 | 2010-04-28 | Pulmagen Therapeutics Inflamma | Enzyme inhibitors |
| GB201004179D0 (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 |
| US9040516B2 (en) | 2011-08-01 | 2015-05-26 | Sumitomo Dainippon Pharma Co., Ltd. | Uracil derivative and use thereof for medical purposes |
| TWI568735B (zh) | 2011-09-14 | 2017-02-01 | 吉斯藥品公司 | 新穎化合物 |
| WO2014009425A1 (en) | 2012-07-12 | 2014-01-16 | Chiesi Farmaceutici S.P.A. | Inhibition of enzymes |
| US20140057920A1 (en) | 2012-08-23 | 2014-02-27 | Boehringer Ingelheim International Gmbh | Substituted 4-pyridones and their use as inhibitors of neutrophil elastase activity |
| US9102624B2 (en) | 2012-08-23 | 2015-08-11 | Boehringer Ingelheim International Gmbh | Substituted 4-pyridones and their use as inhibitors of neutrophil elastase activity |
| US20140057926A1 (en) | 2012-08-23 | 2014-02-27 | Boehringer Ingelheim International Gmbh | Substituted 4-pyridones and their use as inhibitors of neutrophil elastase activity |
| US10590601B2 (en) | 2012-08-31 | 2020-03-17 | Hewlett-Packard Development Company, L.P. | Printable medium |
| US20140221335A1 (en) | 2013-02-06 | 2014-08-07 | Boehringer Ingelheim International Gmbh | Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
| US9198215B2 (en) * | 2013-03-01 | 2015-11-24 | Qualcomm Incorporated | Peer connectivity using reciprocal wireless connections |
| US9115093B2 (en) * | 2013-03-04 | 2015-08-25 | Boehringer Ingelheim International Gmbh | Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
-
2015
- 2015-07-27 US US14/809,311 patent/US9440930B2/en active Active
- 2015-07-30 EP EP15744232.8A patent/EP3174862B1/en active Active
- 2015-07-30 JP JP2017505234A patent/JP6484327B2/ja active Active
- 2015-07-30 WO PCT/EP2015/067506 patent/WO2016016368A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| EP3174862A1 (en) | 2017-06-07 |
| WO2016016368A1 (en) | 2016-02-04 |
| JP2017522350A (ja) | 2017-08-10 |
| US20160031831A1 (en) | 2016-02-04 |
| EP3174862B1 (en) | 2019-10-23 |
| US9440930B2 (en) | 2016-09-13 |
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