KR102863028B1 - 아데노신 A2a 수용체 길항제로서의 화합물 및 이를 포함하는 약학적 조성물 - Google Patents

아데노신 A2a 수용체 길항제로서의 화합물 및 이를 포함하는 약학적 조성물

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Publication number
KR102863028B1
KR102863028B1 KR1020220049770A KR20220049770A KR102863028B1 KR 102863028 B1 KR102863028 B1 KR 102863028B1 KR 1020220049770 A KR1020220049770 A KR 1020220049770A KR 20220049770 A KR20220049770 A KR 20220049770A KR 102863028 B1 KR102863028 B1 KR 102863028B1
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compound
mmol
tert
synthesis
solution
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KR20220146348A (ko
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이창식
이재원
이재영
박예송
곽달용
김현진
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주식회사 종근당
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    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • 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)
KR1020220049770A 2021-04-23 2022-04-21 아데노신 A2a 수용체 길항제로서의 화합물 및 이를 포함하는 약학적 조성물 Active KR102863028B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR1020210053352 2021-04-23
KR20210053352 2021-04-23

Publications (2)

Publication Number Publication Date
KR20220146348A KR20220146348A (ko) 2022-11-01
KR102863028B1 true KR102863028B1 (ko) 2025-09-22

Family

ID=83722733

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KR1020220049770A Active KR102863028B1 (ko) 2021-04-23 2022-04-21 아데노신 A2a 수용체 길항제로서의 화합물 및 이를 포함하는 약학적 조성물

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 (2)

* 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
WO2004092173A2 (en) 2003-04-09 2004-10-28 Biogen Idec Ma Inc. A2a adenosine receptor antagonists

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0459702A1 (en) * 1990-05-29 1991-12-04 Zeneca Limited Azole Derivatives
CA2148502A1 (en) * 1993-09-06 1995-03-16 Fumio Suzuki Antidepressants
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
CA2459304A1 (en) * 2001-09-13 2003-03-20 Schering Corporation Combination of an adenosine a2a receptor antagonist and an antidepressant or anxiolytic
IL161573A0 (en) * 2001-11-30 2004-09-27 Schering Corp [1,2,4]-TRIAZOLE BICYCLIC ADENOSINE A2a RECEPTOR ANTAGONISTS
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
EP3810610A1 (en) * 2018-05-18 2021-04-28 Incyte Corporation Fused pyrimidine derivatives as a2a / a2b inhibitors
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
AU2019383948A1 (en) * 2018-11-20 2021-05-20 Merck Sharp & Dohme Llc Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use
CN112028891B (zh) * 2019-07-30 2022-07-05 厦门宝太生物科技股份有限公司 腺苷受体拮抗剂

Patent Citations (2)

* 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
WO2004092173A2 (en) 2003-04-09 2004-10-28 Biogen Idec Ma Inc. A2a adenosine receptor antagonists

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
JOURNAL OF CHEMICAL INFORMATION AND MODELING, 2009, 49, 2820-2836.
JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48, No. 6, 2009-2018.
JOURNAL OF MEDICINAL CHEMISTRY, 2011, 54, 877-889

Also Published As

Publication number Publication date
JP2024515739A (ja) 2024-04-10
JP7646873B2 (ja) 2025-03-17
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
CN117120443A (zh) 2023-11-24
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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