AU2016232270B2 - Method for producing (4S)-4-[4-cyano-2-(methylsulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydro pyrimidine-5-carbonitrile - Google Patents

Method for producing (4S)-4-[4-cyano-2-(methylsulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydro pyrimidine-5-carbonitrile Download PDF

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AU2016232270B2
AU2016232270B2 AU2016232270A AU2016232270A AU2016232270B2 AU 2016232270 B2 AU2016232270 B2 AU 2016232270B2 AU 2016232270 A AU2016232270 A AU 2016232270A AU 2016232270 A AU2016232270 A AU 2016232270A AU 2016232270 B2 AU2016232270 B2 AU 2016232270B2
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formula
compound
reacts
stands
methyl
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AU2016232270A1 (en
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Birgit Keil
Britta Olenik
Philipp Rubenbauer
Heiko Schirmer
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Ph Pharma Co Ltd
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Ph Pharma Co Ltd
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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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P9/12—Antihypertensives
    • 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

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  • 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)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • 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)
AU2016232270A 2015-03-18 2016-03-15 Method for producing (4S)-4-[4-cyano-2-(methylsulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydro pyrimidine-5-carbonitrile Ceased AU2016232270B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP15159570.9 2015-03-18
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

Publications (2)

Publication Number Publication Date
AU2016232270A1 AU2016232270A1 (en) 2017-10-19
AU2016232270B2 true AU2016232270B2 (en) 2020-09-03

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AU2016232270A Ceased AU2016232270B2 (en) 2015-03-18 2016-03-15 Method for producing (4S)-4-[4-cyano-2-(methylsulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydro pyrimidine-5-carbonitrile

Country Status (9)

Country Link
US (2) US10316001B2 (enExample)
EP (1) EP3271337B1 (enExample)
JP (4) JP7390100B2 (enExample)
KR (1) KR20170129191A (enExample)
CN (2) CN110981815A (enExample)
AU (1) AU2016232270B2 (enExample)
CA (1) CA2980071A1 (enExample)
ES (1) ES2877583T3 (enExample)
WO (1) WO2016146607A1 (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2008340733A1 (en) * 2007-12-20 2009-07-02 Ph Pharma Co., Ltd. 4-(4-Cyano-2-thioaryl)dihydropyrimidinones and use thereof

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GB9214053D0 (en) 1992-07-02 1992-08-12 Ici Plc Heterocyclic amides
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
GB0219896D0 (en) 2002-08-27 2002-10-02 Bayer Ag Dihydropyridine derivatives
WO2004024701A1 (en) 2002-09-10 2004-03-25 Bayer Healthcare Ag Heterocyclic 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
GB0220962D0 (en) * 2002-09-10 2002-10-23 Bayer Ag Heterocyclic derivatives
AU2003290735A1 (en) 2002-12-06 2004-06-30 Eli Lilly And Company Inhibitors of monoamine uptake
US7166603B2 (en) 2003-07-23 2007-01-23 Bristol-Myers Squibb Co. Dihydropyrimidone inhibitors of calcium channel function
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
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2008340733A1 (en) * 2007-12-20 2009-07-02 Ph Pharma Co., Ltd. 4-(4-Cyano-2-thioaryl)dihydropyrimidinones and use thereof

Also Published As

Publication number Publication date
JP2021138711A (ja) 2021-09-16
US20190248750A1 (en) 2019-08-15
ES2877583T3 (es) 2021-11-17
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
JP2020172529A (ja) 2020-10-22

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Owner name: PH PHARMA CO. LTD.

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Owner name: PH PHARMA CO., LTD.

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