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WO2018171698A1 - Dérivés d'un hétéroaryle et d'une pyrimidinone, leur procédé de préparation et leur application - Google Patents

Dérivés d'un hétéroaryle et d'une pyrimidinone, leur procédé de préparation et leur application Download PDF

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Publication number
WO2018171698A1
WO2018171698A1 PCT/CN2018/080117 CN2018080117W WO2018171698A1 WO 2018171698 A1 WO2018171698 A1 WO 2018171698A1 CN 2018080117 W CN2018080117 W CN 2018080117W WO 2018171698 A1 WO2018171698 A1 WO 2018171698A1
Authority
WO
WIPO (PCT)
Prior art keywords
group
heteroaryl
cycloalkyl
aryl
alkyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/CN2018/080117
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English (en)
Chinese (zh)
Inventor
吕贺军
关东亮
白骅
陈明孝
王景录
钱林
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Zhejiang Hisun Pharmaceutical Co Ltd
Original Assignee
Zhejiang Hisun Pharmaceutical Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Zhejiang Hisun Pharmaceutical Co Ltd filed Critical Zhejiang Hisun Pharmaceutical Co Ltd
Priority to CN201880018956.0A priority Critical patent/CN110431143B/zh
Publication of WO2018171698A1 publication Critical patent/WO2018171698A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Definitions

  • R a is selected from a hydrogen atom or an alkyl group
  • R 4 and R 5 are each independently selected from a hydrogen atom, an alkyl group, -OR 11 , -SR 11 , -NR 9 R 10 , -C(O)NR 9 R 10 , -C(O)R 11 , -OC (O) R 11 , -S(O) n NR 9 R 10 , -C(O)OR 11 or -NR 9 C(O)R 10 ;
  • R 6 is selected from the group consisting of halogen, cycloalkyl, heterocyclic, aryl, heteroaryl, -NR 9 R 10 , -C(O)NR 9 R 10 , -C(O)R 11 , -OC(O) R 11 , -S(O) n NR 9 R 10 , -C(O)OR 11 or -NR 9 C(O)R 10 , preferably a heteroaryl group;
  • R 1 and R 6 together with the atom to which they are attached form a 3 to 8 membered saturated or partially unsaturated cycloalkyl group, or form a hetero atom having one or more selected from N, O, S(O) n .
  • cycloalkyl group, heterocyclic group, aryl group or heteroaryl group is optionally further subjected to one or A plurality selected from the group consisting of hydroxyl, halogen, nitro, cyano, alkyl, alkoxy, cycloalkyl, heterocyclyl, aryl, heteroaryl, -NR 9 R 10 , -C(O)NR 9 R 10, -C (O) R 11 , -OC (O) R 11, -S (O) n NR 9 R 10, -C (O) oR 11 or -NR 9 C (O) R 10 substituents Replace
  • n 0, 1, or 2.
  • the invention also provides the use of a compound of formula (I) or a pharmaceutical composition thereof for the manufacture of a medicament for the treatment or prevention of a disease or condition associated with ACC, wherein the disease or condition is preferably a metabolic disease, a cancer, a fungus a parasitic or bacterial infection; wherein the metabolic disease is preferably hepatic steatosis, nonalcoholic fatty liver, obesity, dyslipidemia, hyperlipidemia, type II diabetes or metabolic syndrome, wherein the obesity is preferred Is Prader-Willi syndrome, Bardet-Biedl syndrome or Cohen syndrome or MOMO syndrome, wherein the cancer is preferably liver Cell carcinoma, non-small cell lung cancer, small cell lung cancer, gastric cancer, colorectal cancer, head and neck cancer, melanoma, ovarian cancer or cervical cancer, more preferably hepatocellular carcinoma and non-small cell lung cancer.
  • the disease or condition is preferably a metabolic disease, a cancer, a fungus a parasitic or bacterial infection
  • Examples of monocyclic cycloalkyl groups include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, cyclohexadienyl, cycloheptyl, cycloheptatriene
  • the alkenyl group, the cyclooctyl group and the like are preferably a cyclopropyl group or a cyclohexenyl group.
  • the spirocycloalkyl group is classified into a monospiro, a spiro- or a spirocycloalkyl group, preferably a mono- and bi-spirocycloalkyl group, preferably 4 yuan/5 yuan, 4, depending on the number of common spiro atoms between the rings. Yuan / 6 yuan, 5 yuan / 5 yuan or 5 yuan / 6 yuan.
  • the heterocyclyl ring may be fused to an aryl, heteroaryl or cycloalkyl ring wherein the ring to which the parent structure is attached is a heterocyclic group.
  • the heterocyclic group may be optionally substituted or unsubstituted.
  • Heteroaryl means an aromatic 5 to 6 membered monocyclic or 9 to 10 membered bicyclic ring which may contain from 1 to 4 atoms selected from nitrogen, oxygen and/or sulfur.
  • heteroaryl include, but are not limited to, furyl, pyridyl, 2-oxo-1,2-dihydropyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, thienyl, isoxazolyl , oxazolyl, oxadiazolyl, imidazolyl, pyrrolyl, pyrazolyl, triazolyl, tetrazolyl, thiazolyl, isothiazolyl, 1,2,3-thiadiazolyl, benzo Dioxolyl, benzimidazolyl, fluorenyl, isodecyl, 1,3-dioxo-isoindenyl, quinolyl, ox
  • Amino means -NH 2 .

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Font l'objet de la présente invention des dérivés d'un hétéroaryle et d'une pyrimidinone de formule I, leur procédé de préparation et leur application thérapeutique, particulièrement leur application comme inhibiteurs de l'acétyl coenzyme A carboxylase (ACCase), la définition de chaque substituant de formule I étant semblable à celle contenue dans la description.
PCT/CN2018/080117 2017-03-24 2018-03-23 Dérivés d'un hétéroaryle et d'une pyrimidinone, leur procédé de préparation et leur application Ceased WO2018171698A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201880018956.0A CN110431143B (zh) 2017-03-24 2018-03-23 杂芳基并嘧啶酮类衍生物及其制备方法和用途

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201710182530 2017-03-24
CN201710182530.6 2017-03-24

Publications (1)

Publication Number Publication Date
WO2018171698A1 true WO2018171698A1 (fr) 2018-09-27

Family

ID=63584121

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CN2018/080117 Ceased WO2018171698A1 (fr) 2017-03-24 2018-03-23 Dérivés d'un hétéroaryle et d'une pyrimidinone, leur procédé de préparation et leur application

Country Status (2)

Country Link
CN (1) CN110431143B (fr)
WO (1) WO2018171698A1 (fr)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10759812B2 (en) 2017-01-22 2020-09-01 Sunshine Lake Pharma Co., Ltd. Thienopyrimidine derivative and use thereof in medicine
WO2021000242A1 (fr) * 2019-07-02 2021-01-07 广东东阳光药业有限公司 Dérivés de thiénopyrimidine ayant des configurations stéréo et leur utilisation en médecine
CN112739705A (zh) * 2018-11-20 2021-04-30 中国医药研究开发中心有限公司 螺环类化合物及其医药用途
WO2022138812A1 (fr) 2020-12-24 2022-06-30 モジュラス株式会社 Composé de tétrahydrothiénopyridinesulfonamide

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013071169A1 (fr) * 2011-11-11 2013-05-16 Nimbus Apollo, Inc. Inhibiteurs de l'acc et utilisations associées
WO2014182950A1 (fr) * 2013-05-10 2014-11-13 Nimbus Apollo, Inc. Inhibiteurs de l'acc et utilisations associées
WO2014182945A1 (fr) * 2013-05-10 2014-11-13 Nimbus Apollo, Inc. Inhibiteurs de l'acc et leurs utilisations
WO2014182943A1 (fr) * 2013-05-10 2014-11-13 Nimbus Apollo, Inc. Inhibiteurs de l'acc et utilisations associées
WO2017091600A1 (fr) * 2015-11-25 2017-06-01 Gilead Apollo, Llc Inhibiteurs de l'acc à base de pyrazole et utilisations associées
WO2017091602A1 (fr) * 2015-11-25 2017-06-01 Gilead Apollo, Llc Inhibiteurs de l'acc à base d'esters et utilisations associées
WO2017091617A1 (fr) * 2015-11-25 2017-06-01 Gilead Apollo, Llc Inhibiteurs d'acc à base de triazole et utilisations associées

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013071169A1 (fr) * 2011-11-11 2013-05-16 Nimbus Apollo, Inc. Inhibiteurs de l'acc et utilisations associées
WO2014182950A1 (fr) * 2013-05-10 2014-11-13 Nimbus Apollo, Inc. Inhibiteurs de l'acc et utilisations associées
WO2014182945A1 (fr) * 2013-05-10 2014-11-13 Nimbus Apollo, Inc. Inhibiteurs de l'acc et leurs utilisations
WO2014182943A1 (fr) * 2013-05-10 2014-11-13 Nimbus Apollo, Inc. Inhibiteurs de l'acc et utilisations associées
WO2017091600A1 (fr) * 2015-11-25 2017-06-01 Gilead Apollo, Llc Inhibiteurs de l'acc à base de pyrazole et utilisations associées
WO2017091602A1 (fr) * 2015-11-25 2017-06-01 Gilead Apollo, Llc Inhibiteurs de l'acc à base d'esters et utilisations associées
WO2017091617A1 (fr) * 2015-11-25 2017-06-01 Gilead Apollo, Llc Inhibiteurs d'acc à base de triazole et utilisations associées

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10759812B2 (en) 2017-01-22 2020-09-01 Sunshine Lake Pharma Co., Ltd. Thienopyrimidine derivative and use thereof in medicine
CN112739705A (zh) * 2018-11-20 2021-04-30 中国医药研究开发中心有限公司 螺环类化合物及其医药用途
CN112739705B (zh) * 2018-11-20 2022-08-16 中国医药研究开发中心有限公司 螺环类化合物及其医药用途
WO2021000242A1 (fr) * 2019-07-02 2021-01-07 广东东阳光药业有限公司 Dérivés de thiénopyrimidine ayant des configurations stéréo et leur utilisation en médecine
JP2022540560A (ja) * 2019-07-02 2022-09-16 ▲広▼▲東▼▲東▼▲陽▼光▲薬▼▲業▼有限公司 立体配置を有するチエノピリミジン誘導体及び薬物におけるその応用
JP7374233B2 (ja) 2019-07-02 2023-11-06 ▲広▼▲東▼▲東▼▲陽▼光▲薬▼▲業▼有限公司 立体配置を有するチエノピリミジン誘導体及び薬物におけるその応用
US12428432B2 (en) 2019-07-02 2025-09-30 Sunshine Lake Pharma Co., Ltd. Thienopyrimidine derivatives having stereo configurations and use thereof in medicine
WO2022138812A1 (fr) 2020-12-24 2022-06-30 モジュラス株式会社 Composé de tétrahydrothiénopyridinesulfonamide

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Publication number Publication date
CN110431143A (zh) 2019-11-08
CN110431143B (zh) 2022-08-12

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