ES2877583T3 - Procedimiento para producir (4S)-4-[4-ciano-2-(metilsulfonil)fenil]-3,6-dimetil-2-oxo-1-[3-(trifluorometil)fenil]-1,2,3,4-tetrahidropirimidin-5-carbonitrilo - Google Patents
Procedimiento para producir (4S)-4-[4-ciano-2-(metilsulfonil)fenil]-3,6-dimetil-2-oxo-1-[3-(trifluorometil)fenil]-1,2,3,4-tetrahidropirimidin-5-carbonitrilo Download PDFInfo
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- ES2877583T3 ES2877583T3 ES16713747T ES16713747T ES2877583T3 ES 2877583 T3 ES2877583 T3 ES 2877583T3 ES 16713747 T ES16713747 T ES 16713747T ES 16713747 T ES16713747 T ES 16713747T ES 2877583 T3 ES2877583 T3 ES 2877583T3
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- 230000008569 process Effects 0.000 title claims description 44
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- CVSWXEFIEBBKHH-UHFFFAOYSA-N 4-formyl-3-methylsulfonylbenzonitrile Chemical compound CS(=O)(=O)C1=CC(C#N)=CC=C1C=O CVSWXEFIEBBKHH-UHFFFAOYSA-N 0.000 description 13
- RIOQSEWOXXDEQQ-UHFFFAOYSA-N triphenylphosphine Chemical compound C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1 RIOQSEWOXXDEQQ-UHFFFAOYSA-N 0.000 description 13
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Classifications
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- 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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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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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- A—HUMAN NECESSITIES
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- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- 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
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C315/00—Preparation of sulfones; Preparation of sulfoxides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
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| EP15159570 | 2015-03-18 | ||
| PCT/EP2016/055498 WO2016146607A1 (de) | 2015-03-18 | 2016-03-15 | Verfahren zur herstellung von (4s)-4-[4-cyano-2-(methylsulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluormethyl)phenyl]-1,2,3,4-tetrahydro pyrimidin-5-carbonitril |
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| ES2877583T3 true ES2877583T3 (es) | 2021-11-17 |
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| EP3784657A4 (en) * | 2018-04-24 | 2022-02-09 | pH Pharma Co., Ltd. | USE OF NEUTROPHIL ELASTASE INHIBITORS IN LIVER DISEASE |
| EP4017497A4 (en) * | 2019-08-23 | 2024-01-10 | pH Pharma Co., Ltd. | USE OF A NEUTROPHIL ELASTASE INHIBITOR IN LUNG DISEASES |
| CN112304919B (zh) * | 2020-09-18 | 2022-07-05 | 公安部物证鉴定中心 | 一种乌头碱类植物毒素的定性定量检测方法 |
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| US6372936B1 (en) | 1999-06-09 | 2002-04-16 | Eli Lilly And Company | Optical resolution of aminoisobobutyric acid |
| MY125533A (en) | 1999-12-06 | 2006-08-30 | Bristol Myers Squibb Co | Heterocyclic dihydropyrimidine compounds |
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| 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 |
| GB0520743D0 (en) | 2005-10-12 | 2005-11-23 | Argenta Discovery Ltd | Compounds and their use |
| WO2007067575A2 (en) | 2005-12-05 | 2007-06-14 | Wyeth | Process for preparing substituted aryl cycloalkanol derivatives |
| 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 |
| US20100010024A1 (en) | 2006-07-01 | 2010-01-14 | Bayer Healthcare Ag | Use of1,4-diaryl-dihydropyrimidine-2-on derivatives for treating pulmonary arterial hypertension |
| EP2064184A1 (en) | 2006-09-04 | 2009-06-03 | AstraZeneca AB | Multimeric heterocyclic compounds useful as neutrophil elastase inhibitors |
| 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 |
| DE102009016553A1 (de) | 2009-04-06 | 2010-10-07 | Bayer Schering Pharma Aktiengesellschaft | Sulfonamid- und Sulfoximin-substituierte Diaryldihydropyrimidinone und ihre Verwendung |
| CN110981815A (zh) | 2015-03-18 | 2020-04-10 | Ph制药有限公司 | 用于生产化合物的方法 |
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2016
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- 2016-03-15 JP JP2017549057A patent/JP7390100B2/ja active Active
- 2016-03-15 KR KR1020177029441A patent/KR20170129191A/ko not_active Ceased
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- 2016-03-15 WO PCT/EP2016/055498 patent/WO2016146607A1/de not_active Ceased
- 2016-03-15 AU AU2016232270A patent/AU2016232270B2/en not_active Ceased
- 2016-03-15 US US15/559,385 patent/US10316001B2/en active Active
- 2016-03-15 CA CA2980071A patent/CA2980071A1/en active Pending
- 2016-03-15 EP EP16713747.0A patent/EP3271337B1/de active Active
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| Publication number | Publication date |
|---|---|
| JP2021138711A (ja) | 2021-09-16 |
| US20190248750A1 (en) | 2019-08-15 |
| EP3271337B1 (de) | 2021-03-03 |
| CN110981815A (zh) | 2020-04-10 |
| JP7117415B2 (ja) | 2022-08-12 |
| JP2022145951A (ja) | 2022-10-04 |
| CA2980071A1 (en) | 2016-09-22 |
| JP7390100B2 (ja) | 2023-12-01 |
| EP3271337A1 (de) | 2018-01-24 |
| AU2016232270A1 (en) | 2017-10-19 |
| WO2016146607A1 (de) | 2016-09-22 |
| JP2018508549A (ja) | 2018-03-29 |
| KR20170129191A (ko) | 2017-11-24 |
| JP7125450B2 (ja) | 2022-08-24 |
| CN107635972A (zh) | 2018-01-26 |
| US10316001B2 (en) | 2019-06-11 |
| US20180072685A1 (en) | 2018-03-15 |
| US10676443B2 (en) | 2020-06-09 |
| AU2016232270B2 (en) | 2020-09-03 |
| JP2020172529A (ja) | 2020-10-22 |
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