CN113301896A - Ep4抑制剂和其合成 - Google Patents

Ep4抑制剂和其合成 Download PDF

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Publication number
CN113301896A
CN113301896A CN201980056154.3A CN201980056154A CN113301896A CN 113301896 A CN113301896 A CN 113301896A CN 201980056154 A CN201980056154 A CN 201980056154A CN 113301896 A CN113301896 A CN 113301896A
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CN
China
Prior art keywords
compound
pharmaceutically acceptable
acceptable salt
composition
cancer
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.)
Pending
Application number
CN201980056154.3A
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English (en)
Chinese (zh)
Inventor
M·曼弗雷迪
J·埃切迪
A·C·卡斯特罗
奥村祥征
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.)
Ascat Ltd
Ares Medical Ltd
Original Assignee
Ascat Ltd
Ares Medical 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 Ascat Ltd, Ares Medical Ltd filed Critical Ascat Ltd
Publication of CN113301896A publication Critical patent/CN113301896A/zh
Pending legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/64—Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/50—Compounds containing any of the groups, X being a hetero atom, Y being any atom
    • C07C311/52—Y being a hetero atom
    • C07C311/54—Y being a hetero atom either X or Y, but not both, being nitrogen atoms, e.g. N-sulfonylurea
    • C07C311/63—N-sulfonylisoureas
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201980056154.3A 2018-07-11 2019-07-11 Ep4抑制剂和其合成 Pending CN113301896A (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201862696440P 2018-07-11 2018-07-11
US62/696,440 2018-07-11
US201862737250P 2018-09-27 2018-09-27
US62/737,250 2018-09-27
US201962834525P 2019-04-16 2019-04-16
US62/834,525 2019-04-16
PCT/US2019/041351 WO2020014445A1 (en) 2018-07-11 2019-07-11 Ep4 inhibitors and synthesis thereof

Publications (1)

Publication Number Publication Date
CN113301896A true CN113301896A (zh) 2021-08-24

Family

ID=69141735

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980056154.3A Pending CN113301896A (zh) 2018-07-11 2019-07-11 Ep4抑制剂和其合成

Country Status (7)

Country Link
US (2) US20210300921A1 (https=)
EP (1) EP3820469A4 (https=)
JP (1) JP2021530487A (https=)
CN (1) CN113301896A (https=)
CA (1) CA3107023A1 (https=)
IL (1) IL280051B2 (https=)
WO (1) WO2020014445A1 (https=)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10973834B2 (en) 2018-04-16 2021-04-13 Arrys Therapeutics, Inc. EP4 inhibitors and use thereof
US20210315909A1 (en) 2018-07-11 2021-10-14 Arrys Therapeutics, Inc. Polymorphic compounds and uses thereof
US11254675B2 (en) * 2019-08-12 2022-02-22 Cadila Healthcare Limited Process for preparation of grapiprant
CN110386941A (zh) * 2019-08-15 2019-10-29 上海邦耀生物科技有限公司 Ep4受体拮抗剂和pd-1抑制剂联合用于癌症的治疗
CN115697317A (zh) * 2020-04-08 2023-02-03 株式会社AskAt Ep4受体拮抗剂用于治疗肝癌、黑色素瘤、淋巴瘤和白血病的应用
TWI877433B (zh) * 2020-11-30 2025-03-21 大陸商杭州阿諾生物醫藥科技有限公司 用於治療ｐｉｋ３ｃａ突變癌症的組合療法
CN117377471A (zh) * 2021-05-28 2024-01-09 凯复(苏州)生物医药有限公司 治疗肿瘤的联合疗法
US20240343725A1 (en) * 2021-08-01 2024-10-17 Zenfold Sustainable Technologies Private Limited A process for the preparation of grapiprant and its intermediates
CN117466888A (zh) * 2023-10-30 2024-01-30 西北农林科技大学 一种1h-咪唑并[4,5-c]吡啶化合物的制备方法

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002032422A2 (en) * 2000-10-19 2002-04-25 Pfizer Pharmaceuticals Inc. Ep4 receptor inhibitors to treat rheumatoid arthritis
CN101137656A (zh) * 2005-03-11 2008-03-05 辉瑞大药厂 咪唑衍生物的晶型
US20090036495A1 (en) * 2004-04-20 2009-02-05 Pfizer, Inc. Combinations Comprising Alpha-2-Delta Ligands and Ep4 Receptor Antagonists
CN105596320A (zh) * 2009-04-22 2016-05-25 拉夸里亚创药株式会社 癌症治疗用选择性ep4受体拮抗物质
WO2018084230A1 (en) * 2016-11-04 2018-05-11 Askat Inc. Use of ep4 receptor antagonists for the treatment of nash-associated liver cancer

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1867551B (zh) * 2003-09-03 2013-09-11 拉夸里亚创药株式会社 作为前列腺素e2拮抗剂的苯基或吡啶基酰胺化合物
UA115576C2 (uk) * 2012-12-06 2017-11-27 Байєр Фарма Акцієнгезелльшафт Похідні бензимідазолу як антагоністи ер4
NZ733234A (en) * 2014-03-06 2018-08-31 Aratana Therapeutics Inc Crystalline forms of grapiprant

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002032422A2 (en) * 2000-10-19 2002-04-25 Pfizer Pharmaceuticals Inc. Ep4 receptor inhibitors to treat rheumatoid arthritis
US20090036495A1 (en) * 2004-04-20 2009-02-05 Pfizer, Inc. Combinations Comprising Alpha-2-Delta Ligands and Ep4 Receptor Antagonists
CN101137656A (zh) * 2005-03-11 2008-03-05 辉瑞大药厂 咪唑衍生物的晶型
CN105596320A (zh) * 2009-04-22 2016-05-25 拉夸里亚创药株式会社 癌症治疗用选择性ep4受体拮抗物质
WO2018084230A1 (en) * 2016-11-04 2018-05-11 Askat Inc. Use of ep4 receptor antagonists for the treatment of nash-associated liver cancer

Also Published As

Publication number Publication date
US20240254120A1 (en) 2024-08-01
JP2021530487A (ja) 2021-11-11
IL280051A (en) 2021-03-01
CA3107023A1 (en) 2020-01-16
US20210300921A1 (en) 2021-09-30
IL280051B1 (en) 2023-11-01
EP3820469A4 (en) 2022-04-13
EP3820469A1 (en) 2021-05-19
WO2020014445A1 (en) 2020-01-16
IL280051B2 (en) 2024-03-01

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Application publication date: 20210824