JP6591529B2 - 置換二環式ジヒドロピリミジノンおよ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およ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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- JP6591529B2 JP6591529B2 JP2017505222A JP2017505222A JP6591529B2 JP 6591529 B2 JP6591529 B2 JP 6591529B2 JP 2017505222 A JP2017505222 A JP 2017505222A JP 2017505222 A JP2017505222 A JP 2017505222A JP 6591529 B2 JP6591529 B2 JP 6591529B2
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- JEKPOPAAFQNSID-UHFFFAOYSA-N CN(C(C(C(CC1)=O)=C1N1c2cc(C(F)(F)F)ccc2)c(c(-c2nnc[o]2)c2)ccc2C#N)C1=O Chemical compound CN(C(C(C(CC1)=O)=C1N1c2cc(C(F)(F)F)ccc2)c(c(-c2nnc[o]2)c2)ccc2C#N)C1=O JEKPOPAAFQNSID-UHFFFAOYSA-N 0.000 description 1
- KVWLCPVAPWTWTQ-UHFFFAOYSA-N CN(C(C(C(CC1)=O)=C1N1c2cc(C(F)(F)F)ccc2)c(ccc(C#N)c2)c2-c2ncncc2)C1=O Chemical compound CN(C(C(C(CC1)=O)=C1N1c2cc(C(F)(F)F)ccc2)c(ccc(C#N)c2)c2-c2ncncc2)C1=O KVWLCPVAPWTWTQ-UHFFFAOYSA-N 0.000 description 1
- 0 CN(C(C(C(CC1)=O)=C1N1c2cc(C(F)=*)ncc2)c(c(C(N)=O)c2)ccc2C#N)C1=O Chemical compound CN(C(C(C(CC1)=O)=C1N1c2cc(C(F)=*)ncc2)c(c(C(N)=O)c2)ccc2C#N)C1=O 0.000 description 1
- UZOCMQZNFSCFHL-AREMUKBSSA-N CN([C@@H](C(C(CC1)=O)=C1N1c2cc(C(F)(F)F)ccc2)c(ccc(C#N)c2)c2C(C=C2)=CN(C)C2=O)C1=O Chemical compound CN([C@@H](C(C(CC1)=O)=C1N1c2cc(C(F)(F)F)ccc2)c(ccc(C#N)c2)c2C(C=C2)=CN(C)C2=O)C1=O UZOCMQZNFSCFHL-AREMUKBSSA-N 0.000 description 1
Classifications
-
- 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
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- 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
- 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
- A61P3/08—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
- A61P37/08—Antiallergic agents
-
- 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
- C07D401/10—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 aromatic rings
-
- 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
- C07D403/10—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 aromatic rings
-
- 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
- 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
- C07D413/10—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 carbon chain containing aromatic rings
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Obesity (AREA)
- Rheumatology (AREA)
- Child & Adolescent Psychology (AREA)
- Physical Education & Sports Medicine (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Communicable Diseases (AREA)
- Urology & Nephrology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (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 |
|---|---|---|---|
| EP14179259 | 2014-07-31 | ||
| EP14179259.8 | 2014-07-31 | ||
| PCT/EP2015/067497 WO2016016363A1 (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 |
|---|---|
| JP2017522349A JP2017522349A (ja) | 2017-08-10 |
| JP2017522349A5 JP2017522349A5 (https=) | 2018-09-06 |
| JP6591529B2 true JP6591529B2 (ja) | 2019-10-16 |
Family
ID=51257367
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017505222A Active JP6591529B2 (ja) | 2014-07-31 | 2015-07-30 | 置換二環式ジヒドロピリミジノンおよ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) | US9458113B2 (https=) |
| EP (1) | EP3174863B1 (https=) |
| JP (1) | JP6591529B2 (https=) |
| WO (1) | WO2016016363A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9856232B1 (en) | 2017-06-20 | 2018-01-02 | King Saud University | Dihydropyrimidinone derivatives |
| US10111873B1 (en) | 2018-01-17 | 2018-10-30 | King Saud University | Dihydropyrimidinone derivatives |
| 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 |
| GB201918416D0 (en) | 2019-12-13 | 2020-01-29 | Z Factor Ltd | Compounds and their use for the treatment of Alpha1-Antitrypsin deficiency |
| IL297211B2 (en) | 2020-04-16 | 2025-12-01 | Mereo Biopharma 4 Ltd | Methods involving neutrophil elastase inhibitor alvelestat for treating respiratory disease mediated by alpha-1 antitrypsin deficiency |
| KR20240090272A (ko) | 2021-10-20 | 2024-06-21 | 메레오 바이오파마 4 리미티드 | 섬유화 치료에 사용하기 위한 호중구 엘라스테이스 억제제 |
| WO2026032210A1 (zh) * | 2024-08-05 | 2026-02-12 | 上海壹迪生物技术有限公司 | 一种含嘧啶酮的化合物、其药物组合物及其用途 |
Family Cites Families (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60214428T2 (de) | 2001-12-20 | 2007-09-20 | Bayer Healthcare Ag | 1, 4-dihydro-1, 4-diphenylpyridin-derivate |
| GB0219896D0 (en) | 2002-08-27 | 2002-10-02 | Bayer Ag | Dihydropyridine derivatives |
| ES2293077T3 (es) | 2002-08-27 | 2008-03-16 | Bayer Healthcare Ag | Derivados de dihidropiridinona como inhbidores de hne. |
| GB2392910A (en) | 2002-09-10 | 2004-03-17 | Bayer Ag | 2-Oxopyrimidine derivatives and their use as human leukocyte elastase inhibitors |
| EP1546113B1 (en) | 2002-09-10 | 2013-05-01 | Bayer Intellectual Property GmbH | Pyrimidinone derivatives as therapeutic agents against acute and chronic inflammatory, ischaemic and remodelling processes |
| WO2004024701A1 (en) | 2002-09-10 | 2004-03-25 | Bayer Healthcare Ag | Heterocyclic derivatives |
| 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 |
| 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 |
| 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 |
| WO2009013444A1 (en) | 2007-07-25 | 2009-01-29 | Argenta Discovery Limited | Tetrahydropyrrolopyrimidinediones and their use as human neutrophil elastase inhibitors |
| DE602007009095D1 (de) | 2006-05-04 | 2010-10-21 | Pulmagen Therapeutics Inflamma | Tetrahydropyrrolopyrimidindione und ihre verwendung als inhibitoren der humanen neutrophilen elastase |
| US8198288B2 (en) | 2006-05-04 | 2012-06-12 | Pulmagen Therapeutics (Inflammation) Limited | Tetrahydropyrrolopyrimidinediones and their use in therapy |
| 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 |
| 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 |
| GB0721866D0 (en) | 2007-11-07 | 2007-12-19 | Argenta Discovery Ltd | Pharmaceutical compounds having dual activities |
| 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 |
| 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 |
| 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 |
| 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 |
| CN104024241B (zh) | 2011-08-01 | 2016-01-20 | 大日本住友制药株式会社 | 尿嘧啶衍生物和其用于医学目的的用途 |
| CA2848557A1 (en) | 2011-09-14 | 2013-03-21 | Chiesi Farmaceutici S.P.A. | Tetrahydrotriazolopyrimidine derivatives as human neutrophil elastase inhibitors |
| 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 |
| US20140057920A1 (en) | 2012-08-23 | 2014-02-27 | Boehringer Ingelheim International Gmbh | Substituted 4-pyridones and their use as inhibitors of neutrophil elastase activity |
| 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 |
-
2015
- 2015-07-27 US US14/809,314 patent/US9458113B2/en active Active
- 2015-07-30 JP JP2017505222A patent/JP6591529B2/ja active Active
- 2015-07-30 EP EP15744911.7A patent/EP3174863B1/en active Active
- 2015-07-30 WO PCT/EP2015/067497 patent/WO2016016363A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| WO2016016363A1 (en) | 2016-02-04 |
| US20160031830A1 (en) | 2016-02-04 |
| US9458113B2 (en) | 2016-10-04 |
| JP2017522349A (ja) | 2017-08-10 |
| EP3174863B1 (en) | 2018-12-05 |
| EP3174863A1 (en) | 2017-06-07 |
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