JP6599976B2 - 置換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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- JP6599976B2 JP6599976B2 JP2017505221A JP2017505221A JP6599976B2 JP 6599976 B2 JP6599976 B2 JP 6599976B2 JP 2017505221 A JP2017505221 A JP 2017505221A JP 2017505221 A JP2017505221 A JP 2017505221A JP 6599976 B2 JP6599976 B2 JP 6599976B2
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- 0 CC(N1c2cc(C(F)(F)F)ccc2)=C(*)C(c(c(*)c2)ccc2C#N)N(*)C1=O Chemical compound CC(N1c2cc(C(F)(F)F)ccc2)=C(*)C(c(c(*)c2)ccc2C#N)N(*)C1=O 0.000 description 3
- QZPACNHKTGQRAB-UHFFFAOYSA-N CC(C(C(C1C=CC(C#N)=CC1C(NCC#N)=O)N1C)=C(C)N(c2cc(C(F)(F)F)ccc2)C1=O)=O Chemical compound CC(C(C(C1C=CC(C#N)=CC1C(NCC#N)=O)N1C)=C(C)N(c2cc(C(F)(F)F)ccc2)C1=O)=O QZPACNHKTGQRAB-UHFFFAOYSA-N 0.000 description 1
- PYKIYCDBHRCRSN-UHFFFAOYSA-N CC(C(C(c(c(C(NCC#C)=O)c1)ccc1C#N)N1C)=C(C)N(c2cc(C(F)(F)F)ccc2)C1=O)=O Chemical compound CC(C(C(c(c(C(NCC#C)=O)c1)ccc1C#N)N1C)=C(C)N(c2cc(C(F)(F)F)ccc2)C1=O)=O PYKIYCDBHRCRSN-UHFFFAOYSA-N 0.000 description 1
- VYXTZDPUHHIJQD-UHFFFAOYSA-N CC(C(C(c(c(C1=CCNCC1)c1)ccc1C#N)N1C)=C(C)N(c2cc(C(F)(F)F)ccc2)C1=O)=O Chemical compound CC(C(C(c(c(C1=CCNCC1)c1)ccc1C#N)N1C)=C(C)N(c2cc(C(F)(F)F)ccc2)C1=O)=O VYXTZDPUHHIJQD-UHFFFAOYSA-N 0.000 description 1
- ZKGXWSZOCVKDMQ-UHFFFAOYSA-N CC(C)[SiH-](C(C)C)(C(C)C)c1ncc(B2OC(C)(C)C(C)(C)O2)[o]1 Chemical compound CC(C)[SiH-](C(C)C)(C(C)C)c1ncc(B2OC(C)(C)C(C)(C)O2)[o]1 ZKGXWSZOCVKDMQ-UHFFFAOYSA-N 0.000 description 1
- IZDJSGUXNFGDRA-UHFFFAOYSA-N CC(c1cc(C#N)ccc1C(C(C(C)=O)=C(C)N1c2cc(C(F)(F)F)ccc2)N(C)C1=O)NC1(CC1)C#N Chemical compound CC(c1cc(C#N)ccc1C(C(C(C)=O)=C(C)N1c2cc(C(F)(F)F)ccc2)N(C)C1=O)NC1(CC1)C#N IZDJSGUXNFGDRA-UHFFFAOYSA-N 0.000 description 1
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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
- C07D239/02—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
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- 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
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- 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
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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- 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
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- 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
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
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- C07D487/04—Ortho-condensed systems
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- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
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- C07D498/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
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- 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
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
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- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Neurosurgery (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Child & Adolescent Psychology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Transplantation (AREA)
- Urology & Nephrology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14179289.5 | 2014-07-31 | ||
| EP14179289 | 2014-07-31 | ||
| PCT/EP2015/067504 WO2016016366A1 (en) | 2014-07-31 | 2015-07-30 | Substituted dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017522348A JP2017522348A (ja) | 2017-08-10 |
| JP2017522348A5 JP2017522348A5 (cg-RX-API-DMAC7.html) | 2018-09-06 |
| JP6599976B2 true JP6599976B2 (ja) | 2019-10-30 |
Family
ID=51257372
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017505221A Active JP6599976B2 (ja) | 2014-07-31 | 2015-07-30 | 置換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) | US9290457B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP3174860B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP6599976B2 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2016016366A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI581838B (zh) * | 2016-03-23 | 2017-05-11 | 國立清華大學 | 感測式護具內襯及其防護裝置 |
| US10406751B2 (en) * | 2017-04-14 | 2019-09-10 | Desktop Metal, Inc. | Automated de-powdering with level based nesting |
| EP3692028B1 (en) | 2017-10-06 | 2023-04-26 | Forma Therapeutics, Inc. | Inhibiting ubiquitin specific peptidase 30 |
| CN112513036B (zh) | 2018-05-17 | 2024-05-24 | 福马治疗有限公司 | 用作泛素特异性肽酶30抑制剂的稠合双环化合物 |
| FI3860989T3 (fi) | 2018-10-05 | 2023-05-25 | Forma Therapeutics Inc | Ubikitiinispesifisen proteaasi 30:n (usp30) inhiboiminen |
| CN114650819A (zh) | 2019-09-17 | 2022-06-21 | 美莱奥生物制药第四有限公司 | 用于治疗移植物排斥、闭塞性细支气管炎综合征和移植物抗宿主病的阿维来司他 |
| GB201918416D0 (en) * | 2019-12-13 | 2020-01-29 | Z Factor Ltd | Compounds and their use for the treatment of Alpha1-Antitrypsin deficiency |
| US20230218596A1 (en) | 2020-04-16 | 2023-07-13 | Mereo Biopharma 4 Limited | Methods involving neutrophil elastase inhibitor alvelestat for treating coronavirus infection |
| KR20240090272A (ko) | 2021-10-20 | 2024-06-21 | 메레오 바이오파마 4 리미티드 | 섬유화 치료에 사용하기 위한 호중구 엘라스테이스 억제제 |
Family Cites Families (32)
| 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 |
| US7230017B2 (en) | 2002-08-27 | 2007-06-12 | Bayer Healthcare Ag | Dihydropyridinone derivatives |
| GB0219896D0 (en) | 2002-08-27 | 2002-10-02 | Bayer Ag | Dihydropyridine derivatives |
| BR0314186A (pt) | 2002-09-10 | 2005-08-09 | Bayer Healthcare Ag | Derivados de pirimidinona como agentes terapêuticos contra processos inflamatórios, isquêmicos e remodeladores, agudos e crÈnicos |
| GB2392910A (en) | 2002-09-10 | 2004-03-17 | Bayer Ag | 2-Oxopyrimidine derivatives and their use as human leukocyte elastase inhibitors |
| CA2498052C (en) | 2002-09-10 | 2011-05-17 | Bayer Healthcare Ag | Heterocyclic derivatives |
| CA2557272C (en) | 2004-02-26 | 2012-09-11 | Bayer Healthcare Ag | Heterocyclic derivatives |
| EP1723121B1 (en) | 2004-02-26 | 2012-07-25 | Bayer Pharma Aktiengesellschaft | 1,4-diaryl-dihydropyrimidin-2-ones and their use as 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 |
| WO2009013444A1 (en) | 2007-07-25 | 2009-01-29 | Argenta Discovery Limited | Tetrahydropyrrolopyrimidinediones and their use as human neutrophil elastase inhibitors |
| PT2024367E (pt) | 2006-05-04 | 2010-12-03 | Pulmagen Therapeutics Inflammation Ltd | Tetra-hidropirrolopirimidinadionas e a sua utilização a título de inibidores da elastase de neutrófilos humana |
| 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 |
| GB0721866D0 (en) | 2007-11-07 | 2007-12-19 | Argenta Discovery Ltd | Pharmaceutical compounds having dual activities |
| 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 |
| ATE548355T1 (de) | 2007-12-20 | 2012-03-15 | Bayer Pharma 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 |
| 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 |
| US9040516B2 (en) | 2011-08-01 | 2015-05-26 | Sumitomo Dainippon Pharma Co., Ltd. | Uracil derivative and use thereof for medical purposes |
| WO2013037809A1 (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 |
-
2015
- 2015-07-27 US US14/809,322 patent/US9290457B2/en active Active
- 2015-07-30 WO PCT/EP2015/067504 patent/WO2016016366A1/en not_active Ceased
- 2015-07-30 EP EP15744231.0A patent/EP3174860B1/en active Active
- 2015-07-30 JP JP2017505221A patent/JP6599976B2/ja active Active
Also Published As
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|---|---|
| JP2017522348A (ja) | 2017-08-10 |
| EP3174860A1 (en) | 2017-06-07 |
| EP3174860B1 (en) | 2018-09-19 |
| US9290457B2 (en) | 2016-03-22 |
| WO2016016366A1 (en) | 2016-02-04 |
| US20160031825A1 (en) | 2016-02-04 |
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