CN117120443A - 作为腺苷A2a受体拮抗剂的化合物及包含其的药物组合物 - Google Patents

作为腺苷A2a受体拮抗剂的化合物及包含其的药物组合物 Download PDF

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Publication number
CN117120443A
CN117120443A CN202280022844.9A CN202280022844A CN117120443A CN 117120443 A CN117120443 A CN 117120443A CN 202280022844 A CN202280022844 A CN 202280022844A CN 117120443 A CN117120443 A CN 117120443A
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CN
China
Prior art keywords
compound
mmol
synthesis
tert
alkyl
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CN202280022844.9A
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English (en)
Chinese (zh)
Inventor
李昌植
李载元
李在英
朴艺松
郭达容
金炫进
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Chong Kun Dang Corp
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Chong Kun Dang Corp
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Publication of CN117120443A publication Critical patent/CN117120443A/zh
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—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
    • A61K31/33—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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN202280022844.9A 2021-04-23 2022-04-21 作为腺苷A2a受体拮抗剂的化合物及包含其的药物组合物 Pending CN117120443A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
KR10-2021-0053352 2021-04-23
KR20210053352 2021-04-23
PCT/IB2022/053721 WO2022224180A1 (en) 2021-04-23 2022-04-21 Compound as adenosine a2a receptor antagonist and pharmaceutical composition comprising same

Publications (1)

Publication Number Publication Date
CN117120443A true CN117120443A (zh) 2023-11-24

Family

ID=83722733

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202280022844.9A Pending CN117120443A (zh) 2021-04-23 2022-04-21 作为腺苷A2a受体拮抗剂的化合物及包含其的药物组合物

Country Status (11)

Country Link
US (1) US20240217978A1 (https=)
EP (1) EP4326724A4 (https=)
JP (1) JP7646873B2 (https=)
KR (1) KR102863028B1 (https=)
CN (1) CN117120443A (https=)
AU (1) AU2022262777C1 (https=)
BR (1) BR112023021918A2 (https=)
CA (1) CA3207935A1 (https=)
MX (1) MX2023012338A (https=)
TW (1) TWI838736B (https=)
WO (1) WO2022224180A1 (https=)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2023296161A1 (en) * 2022-06-13 2025-01-02 Alivexis, Inc. Azacycloalkyl carbonyl cyclic amine compound

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1056879A (zh) * 1990-05-29 1991-12-11 帝国化学工业公司 吡咯衍生物及其制备方法
WO1995007282A1 (en) * 1993-09-06 1995-03-16 Kyowa Hakko Kogyo Co., Ltd. Depression remedy
US20030139395A1 (en) * 2001-09-13 2003-07-24 Schering Corporation Combination of an adenosine A2a receptor antagonist and an antidepressant or anxiolytic
CN1688581A (zh) * 2001-11-30 2005-10-26 先灵公司 [1,2,4]－三唑二环腺苷A2ａ受体拮抗剂
US20190375752A1 (en) * 2018-05-18 2019-12-12 Incyte Corporation Fused pyrimidine derivatives as a2a / a2b inhibitors
WO2020106558A1 (en) * 2018-11-20 2020-05-28 Merck Sharp & Dohme Corp. Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use
CN112028891A (zh) * 2019-07-30 2020-12-04 杭州阿诺生物医药科技有限公司 腺苷受体拮抗剂

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5356894A (en) 1990-05-29 1994-10-18 Rodney Peter W Morpholinyl substituted [1,2,4]-triazolo[1,5-a]triazine as antagonist
US6232297B1 (en) * 1999-02-01 2001-05-15 University Of Virginia Patent Foundation Methods and compositions for treating inflammatory response
US6664252B2 (en) * 1999-12-02 2003-12-16 Osi Pharmaceuticals, Inc. 4-aminopyrrolo[2,3-d]pyrimidine compounds specific to adenosine A2a receptor and uses thereof
JPWO2003068776A1 (ja) * 2002-02-15 2005-06-02 協和醗酵工業株式会社 ［１，２，４］トリアゾロ［１，５−ｃ］ピリミジン誘導体
WO2004092173A2 (en) 2003-04-09 2004-10-28 Biogen Idec Ma Inc. A2a adenosine receptor antagonists
JP7197206B2 (ja) * 2018-06-26 2022-12-27 チョーチヤン ビムグリーン ファーマシューティカルズ、リミテッド Ａ２ａ受容体拮抗薬として用いられるトリアゾロトリアジン誘導体

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1056879A (zh) * 1990-05-29 1991-12-11 帝国化学工业公司 吡咯衍生物及其制备方法
WO1995007282A1 (en) * 1993-09-06 1995-03-16 Kyowa Hakko Kogyo Co., Ltd. Depression remedy
US20030139395A1 (en) * 2001-09-13 2003-07-24 Schering Corporation Combination of an adenosine A2a receptor antagonist and an antidepressant or anxiolytic
CN1688581A (zh) * 2001-11-30 2005-10-26 先灵公司 [1,2,4]－三唑二环腺苷A2ａ受体拮抗剂
US20190375752A1 (en) * 2018-05-18 2019-12-12 Incyte Corporation Fused pyrimidine derivatives as a2a / a2b inhibitors
WO2020106558A1 (en) * 2018-11-20 2020-05-28 Merck Sharp & Dohme Corp. Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use
CN112028891A (zh) * 2019-07-30 2020-12-04 杭州阿诺生物医药科技有限公司 腺苷受体拮抗剂

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
屠美玲等: "A_(2A)腺苷受体拮抗剂中间体与抗结剂合成方法研究", 《浙江大学学报(理学版)》, vol. 43, no. 04, 31 July 2016 (2016-07-31), pages 420 - 425 *
蔡海英等: "腺苷受体激动剂和拮抗剂的研究概况", 《国外医学.药学分册》, no. 06, 18 October 2006 (2006-10-18), pages 335 - 338 *

Also Published As

Publication number Publication date
JP2024515739A (ja) 2024-04-10
JP7646873B2 (ja) 2025-03-17
KR102863028B1 (ko) 2025-09-22
AU2022262777C1 (en) 2025-02-13
WO2022224180A1 (en) 2022-10-27
TW202302593A (zh) 2023-01-16
BR112023021918A2 (pt) 2023-12-19
AU2022262777A1 (en) 2023-09-21
MX2023012338A (es) 2023-10-30
US20240217978A1 (en) 2024-07-04
TWI838736B (zh) 2024-04-11
AU2022262777B2 (en) 2024-11-07
EP4326724A4 (en) 2025-03-26
CA3207935A1 (en) 2022-10-27
EP4326724A1 (en) 2024-02-28
KR20220146348A (ko) 2022-11-01

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