CN107635972A - 用于生产(4s)‑4‑[4‑氰基‑2‑(甲基磺酰基)苯基]‑3，6‑二甲基‑2‑氧代‑1‑[3‑(三氟甲基)苯基]‑1，2，3，4‑四氢嘧啶‑5‑甲腈的方法 - Google Patents

用于生产(4s)‑4‑[4‑氰基‑2‑(甲基磺酰基)苯基]‑3，6‑二甲基‑2‑氧代‑1‑[3‑(三氟甲基)苯基]‑1，2，3，4‑四氢嘧啶‑5‑甲腈的方法 Download PDF

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Publication number
CN107635972A
CN107635972A CN201680028214.7A CN201680028214A CN107635972A CN 107635972 A CN107635972 A CN 107635972A CN 201680028214 A CN201680028214 A CN 201680028214A CN 107635972 A CN107635972 A CN 107635972A
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China
Prior art keywords
formula
compound
reaction
reaction step
xxix
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Pending
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CN201680028214.7A
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English (en)
Chinese (zh)
Inventor
H.施尔默
P.鲁本鲍尔
B.凯尔
B.奥勒尼克
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Bayer Pharma AG
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Bayer Pharma AG
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Priority to CN201911315571.3A priority Critical patent/CN110981815A/zh
Publication of CN107635972A publication Critical patent/CN107635972A/zh
Pending legal-status Critical Current

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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)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201680028214.7A 2015-03-18 2016-03-15 用于生产(4s)‑4‑[4‑氰基‑2‑(甲基磺酰基)苯基]‑3，6‑二甲基‑2‑氧代‑1‑[3‑(三氟甲基)苯基]‑1，2，3，4‑四氢嘧啶‑5‑甲腈的方法 Pending CN107635972A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201911315571.3A CN110981815A (zh) 2015-03-18 2016-03-15 用于生产化合物的方法

Applications Claiming Priority (3)

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201911315571.3A Division CN110981815A (zh) 2015-03-18 2016-03-15 用于生产化合物的方法

Publications (1)

Publication Number Publication Date
CN107635972A true CN107635972A (zh) 2018-01-26

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CN201680028214.7A Pending CN107635972A (zh) 2015-03-18 2016-03-15 用于生产(4s)‑4‑[4‑氰基‑2‑(甲基磺酰基)苯基]‑3，6‑二甲基‑2‑氧代‑1‑[3‑(三氟甲基)苯基]‑1，2，3，4‑四氢嘧啶‑5‑甲腈的方法
CN201911315571.3A Pending CN110981815A (zh) 2015-03-18 2016-03-15 用于生产化合物的方法

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US (2) US10316001B2 (enExample)
EP (1) EP3271337B1 (enExample)
JP (4) JP7390100B2 (enExample)
KR (1) KR20170129191A (enExample)
CN (2) CN107635972A (enExample)
AU (1) AU2016232270B2 (enExample)
CA (1) CA2980071A1 (enExample)
ES (1) ES2877583T3 (enExample)
WO (1) WO2016146607A1 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112304919A (zh) * 2020-09-18 2021-02-02 厦门大学 一种乌头碱类植物毒素的定性定量检测方法
CN114761015A (zh) * 2019-08-23 2022-07-15 Ph制药有限公司 中性粒细胞弹性蛋白酶抑制剂在肺病中的用途

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107635972A (zh) 2015-03-18 2018-01-26 拜耳制药股份公司 用于生产(4s)‑4‑[4‑氰基‑2‑(甲基磺酰基)苯基]‑3，6‑二甲基‑2‑氧代‑1‑[3‑(三氟甲基)苯基]‑1，2，3，4‑四氢嘧啶‑5‑甲腈的方法
KR20210002573A (ko) * 2018-04-24 2021-01-08 주식회사 피에이치파마 간 질환에 호중구 엘라스타제 저해제의 사용

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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
CN1732159A (zh) * 2002-09-10 2006-02-08 拜耳医药保健股份公司 嘧啶酮衍生物作为治疗药物治疗急性和慢性炎性、缺血性和重建性病变
CN101903356A (zh) * 2007-12-20 2010-12-01 拜耳先灵制药股份公司 4-(4-氰基-2-硫代芳基)二氢嘧啶酮和它们的使用

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CA2498052C (en) 2002-09-10 2011-05-17 Bayer Healthcare Ag Heterocyclic derivatives
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CN107635972A (zh) 2015-03-18 2018-01-26 拜耳制药股份公司 用于生产(4s)‑4‑[4‑氰基‑2‑(甲基磺酰基)苯基]‑3，6‑二甲基‑2‑氧代‑1‑[3‑(三氟甲基)苯基]‑1，2，3，4‑四氢嘧啶‑5‑甲腈的方法

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WO2005082864A1 (en) * 2004-02-26 2005-09-09 Bayer Healthcare Ag 1,4-diaryl-dihydropyrimidin-2-ones and their use as human neutrophil 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
CN101903356A (zh) * 2007-12-20 2010-12-01 拜耳先灵制药股份公司 4-(4-氰基-2-硫代芳基)二氢嘧啶酮和它们的使用

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114761015A (zh) * 2019-08-23 2022-07-15 Ph制药有限公司 中性粒细胞弹性蛋白酶抑制剂在肺病中的用途
CN112304919A (zh) * 2020-09-18 2021-02-02 厦门大学 一种乌头碱类植物毒素的定性定量检测方法

Also Published As

Publication number Publication date
CN110981815A (zh) 2020-04-10
JP7117415B2 (ja) 2022-08-12
CA2980071A1 (en) 2016-09-22
JP2022145951A (ja) 2022-10-04
KR20170129191A (ko) 2017-11-24
EP3271337A1 (de) 2018-01-24
EP3271337B1 (de) 2021-03-03
US20190248750A1 (en) 2019-08-15
JP2021138711A (ja) 2021-09-16
AU2016232270A1 (en) 2017-10-19
JP2018508549A (ja) 2018-03-29
US20180072685A1 (en) 2018-03-15
US10676443B2 (en) 2020-06-09
JP2020172529A (ja) 2020-10-22
JP7390100B2 (ja) 2023-12-01
US10316001B2 (en) 2019-06-11
ES2877583T3 (es) 2021-11-17
WO2016146607A1 (de) 2016-09-22
JP7125450B2 (ja) 2022-08-24
AU2016232270B2 (en) 2020-09-03

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Application publication date: 20180126