CN116528864A - 杂芳基甲酰胺化合物 - Google Patents

杂芳基甲酰胺化合物 Download PDF

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Publication number
CN116528864A
CN116528864A CN202180080083.8A CN202180080083A CN116528864A CN 116528864 A CN116528864 A CN 116528864A CN 202180080083 A CN202180080083 A CN 202180080083A CN 116528864 A CN116528864 A CN 116528864A
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China
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methyl
compound
phenyl
alkyl
salt
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Pending
Application number
CN202180080083.8A
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English (en)
Chinese (zh)
Inventor
渡边英之
上久保隆
神川晃雄
鹫尾卓哉
关阳平
奥山圭一郎
池田收
富山泰
岩井辰宪
中村章彦
宫坂晃三
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.)
Kotobuki Seiyaku Co Ltd
Astellas Pharma Inc
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Kotobuki Seiyaku Co Ltd
Astellas Pharma Inc
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Publication of CN116528864A publication Critical patent/CN116528864A/zh
Pending legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems

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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)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
CN202180080083.8A 2020-11-30 2021-11-29 杂芳基甲酰胺化合物 Pending CN116528864A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2020197899 2020-11-30
JP2020-197899 2020-11-30
PCT/JP2021/043540 WO2022114164A1 (ja) 2020-11-30 2021-11-29 ヘテロアリールカルボキシアミド化合物

Publications (1)

Publication Number Publication Date
CN116528864A true CN116528864A (zh) 2023-08-01

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CN202180080083.8A Pending CN116528864A (zh) 2020-11-30 2021-11-29 杂芳基甲酰胺化合物

Country Status (20)

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US (2) US20240043403A1 (https=)
EP (1) EP4253373A4 (https=)
JP (1) JP7397452B2 (https=)
KR (1) KR20230116838A (https=)
CN (1) CN116528864A (https=)
AR (1) AR124172A1 (https=)
AU (1) AU2021389180A1 (https=)
CA (1) CA3203285A1 (https=)
CL (1) CL2023001534A1 (https=)
CO (1) CO2023008271A2 (https=)
CR (1) CR20230415A (https=)
DO (1) DOP2023000107A (https=)
EC (1) ECSP23048974A (https=)
IL (1) IL303209A (https=)
JO (1) JOP20230118A1 (https=)
MX (1) MX2023006318A (https=)
PE (1) PE20231986A1 (https=)
TW (1) TWI911340B (https=)
WO (1) WO2022114164A1 (https=)
ZA (1) ZA202305845B (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025067360A1 (zh) * 2023-09-27 2025-04-03 海思科医药集团股份有限公司 一种DGKzeta拮抗剂及其在医药上的应用
WO2025082460A1 (zh) * 2023-10-20 2025-04-24 上海先祥医药科技有限公司 二酰基甘油激酶抑制剂化合物及其应用

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202525813A (zh) 2019-12-19 2025-07-01 比利時商健生藥品公司 經取代之直鏈螺環接衍生物
AR120896A1 (es) 2019-12-25 2022-03-30 Astellas Pharma Inc COMPUESTO DE PIRIDAZINIL-TIAZOLCARBOXAMIDA COMO INHIBIDORES DE DGKz
CR20230415A (es) * 2020-11-30 2023-09-08 Kotobuki Pharmaceutical Co Ltd Compuesto de heteroarilcarboxamida
US20250312341A1 (en) 2022-06-20 2025-10-09 Astellas Pharma Inc. Methods for treating patients with locally advanced and/or metastatic solid tumors using a dgk zeta inhibitor
US12600722B2 (en) 2022-07-18 2026-04-14 Incyte Corporation Tetracyclic compounds as DGK inhibitors
US12600723B2 (en) 2022-07-18 2026-04-14 Incyte Corporation Tetracyclic compounds as DGK inhibitors
US20240217989A1 (en) * 2022-11-18 2024-07-04 Incyte Corporation Heteroaryl Fluoroalkenes As DGK Inhibitors
TW202428575A (zh) * 2023-01-12 2024-07-16 美商英塞特公司 作為dgk抑制劑之雜芳基氟代烯烴
EP4661869A1 (en) 2023-02-06 2025-12-17 Bayer Aktiengesellschaft Combinations of dgk (diacylglycerol kinase) inhibitors and immune checkpoint inhibitors and modulators
CN120826398A (zh) * 2023-03-30 2025-10-21 微境生物医药科技(上海)有限公司 作为DGKζ抑制剂的化合物
CN120826393A (zh) * 2023-04-06 2025-10-21 微境生物医药科技(上海)有限公司 作为DGKζ抑制剂的噻唑类化合物

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050266510A1 (en) * 2004-01-08 2005-12-01 Gajewski Thomas G T cell anergy is reversed by active Ras and regulated by diacylglycerol kinase
JP2008528520A (ja) * 2005-01-25 2008-07-31 シンタ ファーマシューティカルズ コーポレーション 炎症及び免疫に関連する用途に用いる化合物
CN101426774A (zh) * 2006-04-19 2009-05-06 安斯泰来制药有限公司 唑类甲酰胺衍生物
JP2009524677A (ja) * 2006-01-25 2009-07-02 シンタ ファーマシューティカルズ コーポレーション 炎症および免疫関連使用用のチアゾールおよびチアジアゾール化合物
CN101578275A (zh) * 2006-10-31 2009-11-11 先灵公司 苯胺基哌嗪衍生物及其使用方法
WO2020006018A1 (en) * 2018-06-27 2020-01-02 Bristol-Myers Squibb Company Substituted naphthyridinone compounds useful as t cell activators
CN111372926A (zh) * 2017-09-06 2020-07-03 普罗佩纶治疗公司 Wdr5蛋白质-蛋白质结合的抑制剂

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR120896A1 (es) 2019-12-25 2022-03-30 Astellas Pharma Inc COMPUESTO DE PIRIDAZINIL-TIAZOLCARBOXAMIDA COMO INHIBIDORES DE DGKz
CN115697980B (zh) 2020-04-24 2025-03-21 拜耳公司 作为dgkzeta抑制剂用于免疫活化的取代的氨基噻唑
CR20230415A (es) 2020-11-30 2023-09-08 Kotobuki Pharmaceutical Co Ltd Compuesto de heteroarilcarboxamida

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050266510A1 (en) * 2004-01-08 2005-12-01 Gajewski Thomas G T cell anergy is reversed by active Ras and regulated by diacylglycerol kinase
JP2008528520A (ja) * 2005-01-25 2008-07-31 シンタ ファーマシューティカルズ コーポレーション 炎症及び免疫に関連する用途に用いる化合物
JP2009524677A (ja) * 2006-01-25 2009-07-02 シンタ ファーマシューティカルズ コーポレーション 炎症および免疫関連使用用のチアゾールおよびチアジアゾール化合物
CN101426774A (zh) * 2006-04-19 2009-05-06 安斯泰来制药有限公司 唑类甲酰胺衍生物
CN101578275A (zh) * 2006-10-31 2009-11-11 先灵公司 苯胺基哌嗪衍生物及其使用方法
CN111372926A (zh) * 2017-09-06 2020-07-03 普罗佩纶治疗公司 Wdr5蛋白质-蛋白质结合的抑制剂
WO2020006018A1 (en) * 2018-06-27 2020-01-02 Bristol-Myers Squibb Company Substituted naphthyridinone compounds useful as t cell activators

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
VELNATI, S等: "Identification of a novel DGKα inhibitor for XLP-1 therapy by virtual screening", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, vol. 164, 15 February 2019 (2019-02-15), pages 378 - 390 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025067360A1 (zh) * 2023-09-27 2025-04-03 海思科医药集团股份有限公司 一种DGKzeta拮抗剂及其在医药上的应用
WO2025082460A1 (zh) * 2023-10-20 2025-04-24 上海先祥医药科技有限公司 二酰基甘油激酶抑制剂化合物及其应用

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MX2023006318A (es) 2023-06-14
CA3203285A1 (en) 2022-06-02
DOP2023000107A (es) 2023-07-16
ZA202305845B (en) 2024-09-25
JP7397452B2 (ja) 2023-12-13
AU2021389180A9 (en) 2024-06-13
US12077519B2 (en) 2024-09-03
IL303209A (en) 2023-07-01
WO2022114164A1 (ja) 2022-06-02
KR20230116838A (ko) 2023-08-04
PE20231986A1 (es) 2023-12-12
EP4253373A1 (en) 2023-10-04
AU2021389180A1 (en) 2023-06-29
CL2023001534A1 (es) 2023-11-10
CR20230415A (es) 2023-09-08
EP4253373A4 (en) 2024-11-13
US20240043403A1 (en) 2024-02-08
CO2023008271A2 (es) 2023-07-21
ECSP23048974A (es) 2023-07-31
AR124172A1 (es) 2023-02-22
TW202229256A (zh) 2022-08-01
TWI911340B (zh) 2026-01-11
US20240101532A1 (en) 2024-03-28
JPWO2022114164A1 (https=) 2022-06-02
JOP20230118A1 (ar) 2023-05-30

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