JP4825194B2 - 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 - Google Patents
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 Download PDFInfo
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- JP4825194B2 JP4825194B2 JP2007500099A JP2007500099A JP4825194B2 JP 4825194 B2 JP4825194 B2 JP 4825194B2 JP 2007500099 A JP2007500099 A JP 2007500099A JP 2007500099 A JP2007500099 A JP 2007500099A JP 4825194 B2 JP4825194 B2 JP 4825194B2
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- alkyl
- substituted
- alkoxycarbonyl
- trifluoromethyl
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- 0 *=*(CC1)CC*1C(CN)=O Chemical compound *=*(CC1)CC*1C(CN)=O 0.000 description 6
- PKETXFGBAVBKCU-UHFFFAOYSA-N CC(C(C(C(c(cc1)ccc1C#N)N1)=C(C)N(c2cccc(C(F)(F)F)c2)C1=O)=O)OCc1ccccc1 Chemical compound CC(C(C(C(c(cc1)ccc1C#N)N1)=C(C)N(c2cccc(C(F)(F)F)c2)C1=O)=O)OCc1ccccc1 PKETXFGBAVBKCU-UHFFFAOYSA-N 0.000 description 1
- ZRZMTGMVUGGILU-GAGCMDECSA-N CC(C([C@@H](c(cc1)ccc1C#N)N1)=C(C)N(c2cc(C(F)(F)F)ccc2)C1=O)O Chemical compound CC(C([C@@H](c(cc1)ccc1C#N)N1)=C(C)N(c2cc(C(F)(F)F)ccc2)C1=O)O ZRZMTGMVUGGILU-GAGCMDECSA-N 0.000 description 1
- BMFTVFVJBPREFP-UHFFFAOYSA-N CC(C)(C)OC(CN(C(c(cc1)ccc1C#N)C(C(C(CC1)CCN1C(OC(C)(C)C)=O)=O)=C(C)N1c2cc(C(F)(F)F)ccc2)C1=O)=O Chemical compound CC(C)(C)OC(CN(C(c(cc1)ccc1C#N)C(C(C(CC1)CCN1C(OC(C)(C)C)=O)=O)=C(C)N1c2cc(C(F)(F)F)ccc2)C1=O)=O BMFTVFVJBPREFP-UHFFFAOYSA-N 0.000 description 1
- OSNKRUWWESYONG-UHFFFAOYSA-N CC(C)(C)OC(c1cc(CN(C(c(cc2)ccc2C#N)C(C(C2CCCCC2)=O)=C(C)N2c3cc(C(F)(F)F)ccc3)C2=O)ccc1)=O Chemical compound CC(C)(C)OC(c1cc(CN(C(c(cc2)ccc2C#N)C(C(C2CCCCC2)=O)=C(C)N2c3cc(C(F)(F)F)ccc3)C2=O)ccc1)=O OSNKRUWWESYONG-UHFFFAOYSA-N 0.000 description 1
- GKZMTDSZKWLTTA-UHFFFAOYSA-N CC(N(c1cc(C(F)(F)F)ccc1)C(N(Cc1nc(C(O)=O)c[o]1)C1c(cc2)ccc2C#N)=O)=C1C(C1CCCCC1)=O Chemical compound CC(N(c1cc(C(F)(F)F)ccc1)C(N(Cc1nc(C(O)=O)c[o]1)C1c(cc2)ccc2C#N)=O)=C1C(C1CCCCC1)=O GKZMTDSZKWLTTA-UHFFFAOYSA-N 0.000 description 1
- IAIVBCDXTIKSCE-UHFFFAOYSA-N CC(N(c1cc(C(F)(F)F)ccc1)C(NC1c(cc2)ccc2C#N)=O)=C1C(c(cc1)ccc1Br)=O Chemical compound CC(N(c1cc(C(F)(F)F)ccc1)C(NC1c(cc2)ccc2C#N)=O)=C1C(c(cc1)ccc1Br)=O IAIVBCDXTIKSCE-UHFFFAOYSA-N 0.000 description 1
- HOXAQIYGZSVUFX-UHFFFAOYSA-N CC(N(c1cc(C(F)(F)F)ccc1)C(NC1c(cc2)ccc2C#N)=O)=C1C(c(cc1)ccc1[N+]([O-])=O)=O Chemical compound CC(N(c1cc(C(F)(F)F)ccc1)C(NC1c(cc2)ccc2C#N)=O)=C1C(c(cc1)ccc1[N+]([O-])=O)=O HOXAQIYGZSVUFX-UHFFFAOYSA-N 0.000 description 1
- BBHISLJAQMKEOP-QGZVFWFLSA-N CC(N(c1cc(C(F)(F)F)ccc1)C(N[C@@H]1c(cc2)ccc2C#N)=O)=C1C(O)=O Chemical compound CC(N(c1cc(C(F)(F)F)ccc1)C(N[C@@H]1c(cc2)ccc2C#N)=O)=C1C(O)=O BBHISLJAQMKEOP-QGZVFWFLSA-N 0.000 description 1
- XERLAFZWYABQAT-LJQANCHMSA-N CC(N(c1cc(C(F)(F)F)ccc1)C(N[C@@H]1c(cc2)ccc2C#N)=O)=C1C(OCCO)=O Chemical compound CC(N(c1cc(C(F)(F)F)ccc1)C(N[C@@H]1c(cc2)ccc2C#N)=O)=C1C(OCCO)=O XERLAFZWYABQAT-LJQANCHMSA-N 0.000 description 1
- VDDANIYSDIBFJS-UHFFFAOYSA-N CC(N(c1cccc(C(F)(F)F)c1)C(N(CC(NS(c(cc1)ccc1C#N)(=O)=O)=O)C1c(cc2)ccc2C#N)=O)=C1C(C1CC1)=O Chemical compound CC(N(c1cccc(C(F)(F)F)c1)C(N(CC(NS(c(cc1)ccc1C#N)(=O)=O)=O)C1c(cc2)ccc2C#N)=O)=C1C(C1CC1)=O VDDANIYSDIBFJS-UHFFFAOYSA-N 0.000 description 1
- OTPMOUAVZRNQRG-UHFFFAOYSA-N CC(N(c1cccc(C(F)(F)F)c1)C(NC1c(cc2)ccc2C#N)=O)=C1C(C(CCCC1)N1C(OCc1ccccc1)=O)=O Chemical compound CC(N(c1cccc(C(F)(F)F)c1)C(NC1c(cc2)ccc2C#N)=O)=C1C(C(CCCC1)N1C(OCc1ccccc1)=O)=O OTPMOUAVZRNQRG-UHFFFAOYSA-N 0.000 description 1
- AAOCHJQJPVPDCQ-LJQANCHMSA-N CC(N1c2cc(C(F)(F)F)ccc2)=C(CC(C(O)=O)C(O)=O)[C@@H](c(cc2)ccc2C#N)NC1=O Chemical compound CC(N1c2cc(C(F)(F)F)ccc2)=C(CC(C(O)=O)C(O)=O)[C@@H](c(cc2)ccc2C#N)NC1=O AAOCHJQJPVPDCQ-LJQANCHMSA-N 0.000 description 1
- ULGIVTLZXRBMOX-HXUWFJFHSA-N CC(N1c2cc(C(F)(F)F)ccc2)=C(CCC(O)=O)[C@@H](c(cc2)ccc2C#N)NC1=O Chemical compound CC(N1c2cc(C(F)(F)F)ccc2)=C(CCC(O)=O)[C@@H](c(cc2)ccc2C#N)NC1=O ULGIVTLZXRBMOX-HXUWFJFHSA-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
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/20—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D239/22—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
-
- 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
- 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
- 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
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
-
- 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
- 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
-
- 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
- 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
- C07D413/06—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 only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04004314.3 | 2004-02-26 | ||
| EP04004314 | 2004-02-26 | ||
| PCT/EP2005/001486 WO2005082864A1 (en) | 2004-02-26 | 2005-02-15 | 1,4-diaryl-dihydropyrimidin-2-ones and their use as human neutrophil elastase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2007524696A JP2007524696A (ja) | 2007-08-30 |
| JP2007524696A5 JP2007524696A5 (https=) | 2008-04-03 |
| JP4825194B2 true JP4825194B2 (ja) | 2011-11-30 |
Family
ID=34895952
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007500099A Expired - Fee Related JP4825194B2 (ja) | 2004-02-26 | 2005-02-15 | 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 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8101615B2 (https=) |
| EP (1) | EP1723121B1 (https=) |
| JP (1) | JP4825194B2 (https=) |
| CA (1) | CA2557271C (https=) |
| ES (1) | ES2394177T3 (https=) |
| WO (1) | WO2005082864A1 (https=) |
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE0302486D0 (sv) | 2003-09-18 | 2003-09-18 | Astrazeneca Ab | Novel compounds |
| WO2005080372A1 (en) * | 2004-02-19 | 2005-09-01 | Bayer Healthcare Ag | Dihydropyridinone 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 |
| CA2590851A1 (en) * | 2004-12-16 | 2006-06-22 | Bayer Healthcare Ag | Crystal structure of enzyme and uses thereof |
| GB0502258D0 (en) * | 2005-02-03 | 2005-03-09 | Argenta Discovery Ltd | Compounds and their use |
| GB0516313D0 (en) | 2005-08-08 | 2005-09-14 | Argenta Discovery Ltd | Azole derivatives and their uses |
| JP2009504624A (ja) | 2005-08-08 | 2009-02-05 | アージェンタ ディスカバリー リミテッド | ビシクロ[2.2.1]ヘプタ−7−イルアミン誘導体およびその使用 |
| TW200808771A (en) | 2006-05-08 | 2008-02-16 | Astrazeneca Ab | Novel compounds II |
| TW200808763A (en) | 2006-05-08 | 2008-02-16 | Astrazeneca Ab | Novel compounds I |
| 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 |
| WO2008104752A1 (en) * | 2007-02-26 | 2008-09-04 | Astrazeneca Ab | Dihydropyridones as elastase inhibitors |
| DE102007019691A1 (de) | 2007-04-26 | 2008-10-30 | Bayer Healthcare Ag | Verwendung von acyclisch substituierten Furopyrimidin-Derivaten zur Behandlung der pulmonalen arteriellen Hypertonie |
| DE102007019690A1 (de) | 2007-04-26 | 2008-10-30 | Bayer Healthcare Ag | Verwendung von cyclisch substituierten Furopyrimidin-Derivaten zur Behandlung der pulmonalen arteriellen Hypertonie |
| DE102007027800A1 (de) | 2007-06-16 | 2008-12-18 | Bayer Healthcare Ag | Substituierte bicyclische Heteroaryl-Verbindungen und ihre Verwendung |
| DE102007027799A1 (de) | 2007-06-16 | 2008-12-18 | Bayer Healthcare Ag | Substituierte Furopyrimidine und ihre Verwendung |
| DE102007051762A1 (de) | 2007-10-30 | 2009-05-07 | Bayer Healthcare Ag | Substituierte Pyrrolotriazine und ihre Verwendung |
| EP2217591A4 (en) | 2007-11-06 | 2011-10-26 | Astrazeneca Ab | CERTAIN 2-PYRAZINONE DERIVATIVES AND THEIR USE AS NEUTROPHILES ELASTASE INHIBITORS |
| DE102007054786A1 (de) | 2007-11-16 | 2009-05-20 | Bayer Healthcare Ag | Trisubstituierte Furopyrimidine und ihre Verwendung |
| 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 |
| 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 |
| DE102008052013A1 (de) | 2008-10-17 | 2010-04-22 | Bayer Schering Pharma Aktiengesellschaft | 4-(4-Cyano-2-thioaryl)-dihydropyrimidinone und ihre Verwendung |
| DE102008007400A1 (de) | 2008-02-04 | 2009-08-06 | Bayer Healthcare Ag | Substituierte Furane und ihre Verwendung |
| WO2009149836A1 (en) * | 2008-06-09 | 2009-12-17 | Bayer Schering Pharma Aktiengesellschaft | Annellated 4- (indazolyl) -1,4-dihydropyridine derivatives and methods of use thereof |
| DE102009004197A1 (de) | 2009-01-09 | 2010-07-15 | Bayer Schering Pharma Aktiengesellschaft | Heterocyclisch anellierte Diaryldihydropyrimidin-Derivate und ihre Verwendung |
| TW201036957A (en) | 2009-02-20 | 2010-10-16 | Astrazeneca Ab | Novel salt 628 |
| DE102009016553A1 (de) | 2009-04-06 | 2010-10-07 | Bayer Schering Pharma Aktiengesellschaft | Sulfonamid- und Sulfoximin-substituierte Diaryldihydropyrimidinone und ihre Verwendung |
| CN102639537B (zh) * | 2009-07-10 | 2015-07-22 | 拜耳知识产权有限责任公司 | 吲唑基取代的二氢异*唑并吡啶及其使用方法 |
| AU2010302420B2 (en) | 2009-10-02 | 2013-07-04 | Astrazeneca Ab | 2-pyridone compounds used as inhibitors of neutrophil elastase |
| GB0918924D0 (en) | 2009-10-28 | 2009-12-16 | Vantia Ltd | Azaindole derivatives |
| GB0918923D0 (en) | 2009-10-28 | 2009-12-16 | Vantia Ltd | Aminothiazole derivatives |
| GB0918922D0 (en) | 2009-10-28 | 2009-12-16 | Vantia Ltd | Aminopyridine derivatives |
| DE102010030187A1 (de) | 2010-06-16 | 2011-12-22 | Bayer Schering Pharma Aktiengesellschaft | 4-Cyan-2-sulfonylphenyl)pyrazolyl-substituierte Pyridinone und Pyrazinone und ihre Verwendung |
| 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 |
| US9924721B2 (en) * | 2013-08-28 | 2018-03-27 | Bayer Cropscience Aktiengesellschaft | Malonic ester derivatives of heteroarylpiperidines and -piperazines as fungicides |
| KR102284938B1 (ko) * | 2013-11-27 | 2021-08-02 | 선샤인 레이크 파르마 컴퍼니 리미티드 | 다이하이드로피리미딘 유도체 및 이의 중간산물의 제조 방법 |
| USRE47493E1 (en) | 2014-02-20 | 2019-07-09 | Boehringer Ingelheim International Gmbh | Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
| US20170022171A1 (en) | 2014-04-03 | 2017-01-26 | Bayer Pharma Aktiengesellschaft | 2,5-disubstituted cyclopentanecarboxylic acids and their use |
| US20170119776A1 (en) | 2014-04-03 | 2017-05-04 | Bayer Pharma Aktiengesellschaft | Chiral 2,5-disubstituted cyclopentanecarboxylic acid derivatives and use thereof |
| CA2944614A1 (en) | 2014-04-03 | 2015-10-08 | Bayer Pharma Aktiengesellschaft | 2,5-disubstituted cyclopentane carboxylic acids for the treatment of respiratoy tract diseases |
| US9290457B2 (en) * | 2014-07-31 | 2016-03-22 | Boehringer Ingelheim International Gmbh | Substituted 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 |
| US9657015B2 (en) | 2014-07-31 | 2017-05-23 | 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 |
| KR20170129191A (ko) | 2015-03-18 | 2017-11-24 | 바이엘 파마 악티엔게젤샤프트 | (4s)-4-[4-사이아노-2-(메틸설폰일)페닐]-3,6-다이메틸-2-옥소-1-[3-(트라이플루오로메틸)페닐]-1,2,3,4-테트라하이드로 피리미딘-5-카보나이트릴의 생성 방법 |
| TWI810220B (zh) | 2017-11-17 | 2023-08-01 | 德商拜耳廠股份有限公司 | 經取代之巨環吲哚衍生物 |
| US12030879B2 (en) | 2018-03-02 | 2024-07-09 | Inflazome Limited | Sulfonyl acetamides as NLRP3 inhibitors |
| US11834433B2 (en) | 2018-03-02 | 2023-12-05 | Inflazome Limited | Compounds |
| US12168653B2 (en) | 2018-03-02 | 2024-12-17 | Inflazome Limited | Sulfonamide derivates as NLRP3 inhibitors |
| WO2019166632A1 (en) | 2018-03-02 | 2019-09-06 | Inflazome Limited | Novel compounds |
| EP3759078A1 (en) | 2018-03-02 | 2021-01-06 | Inflazome Limited | Novel compounds |
| 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 |
| 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 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2006507355A (ja) * | 2002-09-10 | 2006-03-02 | バイエル・ヘルスケア・アクチェンゲゼルシャフト | 急性および慢性炎症、虚血およびリモデリング過程に対する治療剤としてのピリミジノン誘導体 |
| JP2007509174A (ja) * | 2003-10-24 | 2007-04-12 | ワイス | 5ht2cアゴニストとしてのジヒドロベンゾフラニルアルカンアミン誘導体 |
| JP2007509074A (ja) * | 2003-10-16 | 2007-04-12 | サイトキネティクス・インコーポレーテッド | 化合物、組成物、および方法 |
| JP2007523931A (ja) * | 2004-02-26 | 2007-08-23 | バイエル・ヘルスケア・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 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9214053D0 (en) | 1992-07-02 | 1992-08-12 | Ici Plc | Heterocyclic amides |
| DE60214428T2 (de) * | 2001-12-20 | 2007-09-20 | Bayer Healthcare Ag | 1, 4-dihydro-1, 4-diphenylpyridin-derivate |
| 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 |
| WO2005080372A1 (en) | 2004-02-19 | 2005-09-01 | Bayer Healthcare Ag | Dihydropyridinone derivatives |
-
2005
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Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2006507355A (ja) * | 2002-09-10 | 2006-03-02 | バイエル・ヘルスケア・アクチェンゲゼルシャフト | 急性および慢性炎症、虚血およびリモデリング過程に対する治療剤としてのピリミジノン誘導体 |
| JP2007509074A (ja) * | 2003-10-16 | 2007-04-12 | サイトキネティクス・インコーポレーテッド | 化合物、組成物、および方法 |
| JP2007509174A (ja) * | 2003-10-24 | 2007-04-12 | ワイス | 5ht2cアゴニストとしてのジヒドロベンゾフラニルアルカンアミン誘導体 |
| JP2007523931A (ja) * | 2004-02-26 | 2007-08-23 | バイエル・ヘルスケア・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 |
Also Published As
| Publication number | Publication date |
|---|---|
| US8101615B2 (en) | 2012-01-24 |
| US20080064704A1 (en) | 2008-03-13 |
| CA2557271A1 (en) | 2005-09-09 |
| CA2557271C (en) | 2012-08-21 |
| EP1723121A1 (en) | 2006-11-22 |
| ES2394177T3 (es) | 2013-01-23 |
| EP1723121B1 (en) | 2012-07-25 |
| WO2005082864A1 (en) | 2005-09-09 |
| JP2007524696A (ja) | 2007-08-30 |
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