JP2017522350A5 - - Google Patents
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- JP2017522350A5 JP2017522350A5 JP2017505234A JP2017505234A JP2017522350A5 JP 2017522350 A5 JP2017522350 A5 JP 2017522350A5 JP 2017505234 A JP2017505234 A JP 2017505234A JP 2017505234 A JP2017505234 A JP 2017505234A JP 2017522350 A5 JP2017522350 A5 JP 2017522350A5
- Authority
- JP
- Japan
- Prior art keywords
- formula
- compound
- pharmaceutical composition
- group
- treatment
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims 12
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 6
- 201000003883 Cystic fibrosis Diseases 0.000 claims 5
- 239000003112 inhibitor Substances 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 208000002815 pulmonary hypertension Diseases 0.000 claims 3
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 2
- 206010019708 Hepatic steatosis Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 206010069351 acute lung injury Diseases 0.000 claims 2
- 201000009267 bronchiectasis Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000024908 graft versus host disease Diseases 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- XGWFJBFNAQHLEF-UHFFFAOYSA-N 9-anthroic acid Chemical compound C1=CC=C2C(C(=O)O)=C(C=CC=C3)C3=CC2=C1 XGWFJBFNAQHLEF-UHFFFAOYSA-N 0.000 claims 1
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 1
- 102000003902 Cathepsin C Human genes 0.000 claims 1
- 108090000267 Cathepsin C Proteins 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010014561 Emphysema Diseases 0.000 claims 1
- 208000027004 Eosinophilic disease Diseases 0.000 claims 1
- 208000004930 Fatty Liver Diseases 0.000 claims 1
- 208000017189 Gastrointestinal inflammatory disease Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 229940122236 Histamine receptor antagonist Drugs 0.000 claims 1
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 claims 1
- 102000009389 Prostaglandin D receptors Human genes 0.000 claims 1
- 108050000258 Prostaglandin D receptors Proteins 0.000 claims 1
- 102000002255 Secretory Proteinase Inhibitory Proteins Human genes 0.000 claims 1
- 108010000303 Secretory Proteinase Inhibitory Proteins Proteins 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- 206010047115 Vasculitis Diseases 0.000 claims 1
- 208000002223 abdominal aortic aneurysm Diseases 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 239000000808 adrenergic beta-agonist Substances 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 208000006682 alpha 1-Antitrypsin Deficiency Diseases 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 208000007474 aortic aneurysm Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 230000003454 betamimetic effect Effects 0.000 claims 1
- 210000000621 bronchi Anatomy 0.000 claims 1
- 239000000812 cholinergic antagonist Substances 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 239000003246 corticosteroid Substances 0.000 claims 1
- 229960001334 corticosteroids Drugs 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 229940121647 egfr inhibitor Drugs 0.000 claims 1
- 208000010706 fatty liver disease Diseases 0.000 claims 1
- 230000003176 fibrotic effect Effects 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 1
- 239000003591 leukocyte elastase inhibitor Substances 0.000 claims 1
- YEESKJGWJFYOOK-IJHYULJSSA-N leukotriene D4 Chemical compound CCCCC\C=C/C\C=C/C=C/C=C/[C@H]([C@@H](O)CCCC(O)=O)SC[C@H](N)C(=O)NCC(O)=O YEESKJGWJFYOOK-IJHYULJSSA-N 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 244000000010 microbial pathogen Species 0.000 claims 1
- 230000003448 neutrophilic effect Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 230000002685 pulmonary effect Effects 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 230000009529 traumatic brain injury Effects 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 0 *C(C(C(CCC1)=O)=C1N1*)N(*)C1=O Chemical compound *C(C(C(CCC1)=O)=C1N1*)N(*)C1=O 0.000 description 1
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 true JP2017522350A5 (enExample) | 2018-07-26 |
| JP6484327B2 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 |
| WO2021053058A1 (en) | 2019-09-17 | 2021-03-25 | Mereo Biopharma 4 Limited | Alvelestat for use in the treatment of graft rejection, bronchiolitis obliterans syndrome and graft versus host disease |
| DK4106757T3 (da) | 2020-04-16 | 2023-10-23 | Mereo Biopharma 4 Ltd | Fremgangsmåder der involverer neutrofil elastase-inhibitor alvelestat til behandling af luftvejssygdom medieret af alpha-1-antitrypsin-mangel |
| AU2022373971A1 (en) | 2021-10-20 | 2024-04-04 | Mereo Biopharma 4 Limited | Neutrophil elastase inhibitors for use in the treatment of fibrosis |
Family Cites Families (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2470813A1 (en) | 2001-12-20 | 2003-07-03 | Bayer Healthcare Ag | 1,4-dihydro-1,4-diphenylpyridine derivatives |
| 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 |
| PL375647A1 (en) | 2002-09-10 | 2005-12-12 | Bayer Healthcare Ag | 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 |
| GB2392910A (en) * | 2002-09-10 | 2004-03-17 | Bayer Ag | 2-Oxopyrimidine derivatives and their use as human leukocyte elastase inhibitors |
| 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 |
| 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 |
| 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 |
| JP4999920B2 (ja) | 2006-05-04 | 2012-08-15 | プルマジェン セラピューティクス （インフラメーション） リミテッド | テトラヒドロピロロピリミジンジオン類およびヒト好中球エラスターゼ阻害薬としてのそれらの使用 |
| US8198288B2 (en) | 2006-05-04 | 2012-06-12 | Pulmagen Therapeutics (Inflammation) Limited | Tetrahydropyrrolopyrimidinediones and their use in therapy |
| 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 |
| 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 |
| 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 |
| GB0721866D0 (en) | 2007-11-07 | 2007-12-19 | Argenta Discovery Ltd | Pharmaceutical compounds having dual activities |
| MX2010006033A (es) | 2007-12-20 | 2010-07-16 | Bayer Schering Pharma Ag | 4-(4-ciano-2-tioaril)dihidropirimidinonas y su uso. |
| 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 |
| 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 |
| KR20140060513A (ko) | 2011-09-14 | 2014-05-20 | 키에시 파르마슈티시 엣스. 피. 에이. | 인체 호중구 엘라스타제 억제제인 테트라히드로트리아졸로피리미딘 유도체 |
| 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 |
| US20140057926A1 (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 |
| EP2890567B1 (en) | 2012-08-31 | 2016-12-07 | 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 WO PCT/EP2015/067506 patent/WO2016016368A1/en not_active Ceased
- 2015-07-30 JP JP2017505234A patent/JP6484327B2/ja active Active
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