CN112839928B - 用于制备3-[5-氨基-4-(3-氰基苯甲酰基)-吡唑化合物的合成方法 - Google Patents

用于制备3-[5-氨基-4-(3-氰基苯甲酰基)-吡唑化合物的合成方法 Download PDF

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CN112839928B
CN112839928B CN201980063294.3A CN201980063294A CN112839928B CN 112839928 B CN112839928 B CN 112839928B CN 201980063294 A CN201980063294 A CN 201980063294A CN 112839928 B CN112839928 B CN 112839928B
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compound
reaction mass
reaction
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aprotic solvent
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CN112839928A (zh
Inventor
马克·梅森巴赫
本杰明·马丁
尼克·约翰内斯·朗德
卡门·鲁伊斯
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Mereo Biopharma 1 Ltd
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Mereo Biopharma 1 Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C243/00Compounds containing chains of nitrogen atoms singly-bound to each other, e.g. hydrazines, triazanes
    • C07C243/10Hydrazines
    • C07C243/22Hydrazines having nitrogen atoms of hydrazine groups bound to carbon atoms of six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00Carboxylic acid nitriles
    • C07C255/49Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/56Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and doubly-bound oxygen atoms bound to the carbon skeleton
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/12Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/16Systems containing only non-condensed rings with a six-membered ring the ring being unsaturated

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201980063294.3A 2018-09-26 2019-09-26 用于制备3-[5-氨基-4-(3-氰基苯甲酰基)-吡唑化合物的合成方法 Active CN112839928B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB1815695.0 2018-09-26
GBGB1815695.0A GB201815695D0 (en) 2018-09-26 2018-09-26 Synthetic method
PCT/GB2019/052718 WO2020065323A1 (en) 2018-09-26 2019-09-26 Synthetic method for the preparation of a 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol compound

Publications (2)

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CN112839928A CN112839928A (zh) 2021-05-25
CN112839928B true CN112839928B (zh) 2024-04-30

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CN201980063294.3A Active CN112839928B (zh) 2018-09-26 2019-09-26 用于制备3-[5-氨基-4-(3-氰基苯甲酰基)-吡唑化合物的合成方法

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Country Link
US (1) US11649213B2 (https=)
EP (1) EP3856721B1 (https=)
JP (1) JP7291782B2 (https=)
KR (1) KR102711257B1 (https=)
CN (1) CN112839928B (https=)
AU (1) AU2019350525B2 (https=)
CA (1) CA3112993A1 (https=)
DK (1) DK3856721T3 (https=)
ES (1) ES2943289T3 (https=)
GB (1) GB201815695D0 (https=)
IL (1) IL281636B2 (https=)
WO (1) WO2020065323A1 (https=)

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3658838A (en) * 1968-11-16 1972-04-25 Bayer Ag Process for the preparation of 1 5-disubstituted-4-cyano-pyrazoles
US5922741A (en) * 1996-04-24 1999-07-13 Celltech Therapeutics Ltd. 5-aminopyrazoles useful as tyrosine kinase inhibitors
US6103900A (en) * 1992-12-17 2000-08-15 Pfizer Inc Pyrazoles and pyrazolopyrimidines having CRF antagonistic activity
CN1832928A (zh) * 2003-06-26 2006-09-13 诺瓦提斯公司 以5元杂环为基础的p38激酶抑制剂

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4686221A (en) * 1985-10-01 1987-08-11 Kanebo, Ltd. Quinolinecarboxylic acid compounds and antimicrobial agent containing the same
US6005109A (en) * 1997-10-30 1999-12-21 Pflizer Inc. Pyrazoles and pyrazolopyrimidines having CRF antagonistic activity
FR2732967B1 (fr) 1995-04-11 1997-07-04 Sanofi Sa 1-phenylpyrazole-3-carboxamides substitues, actifs sur la neurotensine, leur preparation, les compositions pharmaceutiques en contenant
HRP20000724A2 (en) * 1998-05-05 2001-06-30 Hoffmann La Roche Pyrazole derivatives as p-38 map kinase inhibitors
WO2005007632A1 (en) 2003-07-18 2005-01-27 Pharmacia Corporation Substituted pyridazinones as inhibitors of p38
US7485657B2 (en) 2004-05-12 2009-02-03 Boehringer Ingelheim Pharmaceuticals, Inc. Anti-cytokine heterocyclic compounds
ATE510836T1 (de) 2006-01-19 2011-06-15 Matrix Lab Ltd Umwandlung eines aromatischen diazoniumsalzes in ein arylhydrazin
AU2008281594A1 (en) 2007-08-02 2009-02-05 Generics [Uk] Limited Novel process
WO2009088025A1 (ja) 2008-01-10 2009-07-16 Hokko Chemical Industry Co., Ltd. フェニルトリアゾリノン類の製造法
JP5602387B2 (ja) 2008-05-02 2014-10-08 キヤノン株式会社 インクジェット用インク、インクジェット記録方法、インクカートリッジ、記録ユニット、及びインクジェット記録装置
CN102964270B (zh) 2012-11-21 2015-01-07 合肥星宇化学有限责任公司 一种亚硫酸钠还原重氮盐合成肼的方法
WO2018059533A1 (zh) 2016-09-29 2018-04-05 南京明德新药研发股份有限公司 p38αMAPK激酶抑制剂及其制备方法和应用

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3658838A (en) * 1968-11-16 1972-04-25 Bayer Ag Process for the preparation of 1 5-disubstituted-4-cyano-pyrazoles
US6103900A (en) * 1992-12-17 2000-08-15 Pfizer Inc Pyrazoles and pyrazolopyrimidines having CRF antagonistic activity
US5922741A (en) * 1996-04-24 1999-07-13 Celltech Therapeutics Ltd. 5-aminopyrazoles useful as tyrosine kinase inhibitors
CN1832928A (zh) * 2003-06-26 2006-09-13 诺瓦提斯公司 以5元杂环为基础的p38激酶抑制剂

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
1-甲基-5-氨基-4-氰基吡唑的合成;陆慧, 洪梅, 陈书明, 肖亚平;江苏化工(第03期);第35-36页 *
Microwave-assisted synthesis of a pyrazolyl ketone library for evaluation as p38 MAPK inhibitors in Werner syndrome cells;Bagley, Mark C et al.;《Future Medicinal Chemistry》;第2卷(第2期);第203-213页 *
Synthesis of 4-cyano- and 5-aminopyrazoles and deamination of 5-aminopyrazoles;Toche, R. B et al.;《Organic Preparations and Procedures International》;第40卷(第6期);第551-556页 *

Also Published As

Publication number Publication date
WO2020065323A1 (en) 2020-04-02
KR102711257B1 (ko) 2024-09-30
US20210395207A1 (en) 2021-12-23
JP2022502400A (ja) 2022-01-11
EP3856721A1 (en) 2021-08-04
DK3856721T3 (da) 2023-04-24
US11649213B2 (en) 2023-05-16
EP3856721B1 (en) 2023-03-29
IL281636B2 (en) 2024-08-01
AU2019350525A1 (en) 2021-04-15
CN112839928A (zh) 2021-05-25
AU2019350525B2 (en) 2024-05-02
IL281636B1 (en) 2024-04-01
JP7291782B2 (ja) 2023-06-15
KR20210069044A (ko) 2021-06-10
IL281636A (en) 2021-05-31
CA3112993A1 (en) 2020-04-02
GB201815695D0 (en) 2018-11-07
ES2943289T3 (es) 2023-06-12

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