CN114846015B - 用作t细胞激活剂的经取代的杂芳基化合物 - Google Patents

用作t细胞激活剂的经取代的杂芳基化合物 Download PDF

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CN114846015B
CN114846015B CN202080089546.2A CN202080089546A CN114846015B CN 114846015 B CN114846015 B CN 114846015B CN 202080089546 A CN202080089546 A CN 202080089546A CN 114846015 B CN114846015 B CN 114846015B
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cys
gly
ala
thr
methyl
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CN114846015A (zh
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U·维拉帕蒂
C·P·达恩
R.E.奥尔森
P·R·贾拉甘
J·S·瓦瑞尔
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Bristol Myers Squibb Co
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • 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
    • A61K31/5025Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/127Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Dispersion Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
CN202080089546.2A 2019-12-23 2020-12-22 用作t细胞激活剂的经取代的杂芳基化合物 Active CN114846015B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IN201911053558 2019-12-23
IN201911053558 2019-12-23
PCT/US2020/066510 WO2021133752A1 (en) 2019-12-23 2020-12-22 Substituted heteroaryl compounds useful as t cell activators

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CN114846015A CN114846015A (zh) 2022-08-02
CN114846015B true CN114846015B (zh) 2024-07-30

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US (1) US20230086933A1 (https=)
EP (1) EP4081524B1 (https=)
JP (1) JP7677976B2 (https=)
KR (1) KR20220119458A (https=)
CN (1) CN114846015B (https=)
AU (1) AU2020412472A1 (https=)
BR (1) BR112022012204A2 (https=)
CA (1) CA3163003A1 (https=)
ES (1) ES3013568T3 (https=)
IL (1) IL294273A (https=)
MX (1) MX2022007372A (https=)
WO (1) WO2021133752A1 (https=)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL294085A (en) * 2019-12-19 2022-08-01 Bristol Myers Squibb Co Combinations of dgk inhibitors and checkpoint antagonists
IL294032A (en) 2019-12-24 2022-08-01 Carna Biosciences Inc Compounds that regulate diacylglycerol kinase
MX2023014762A (es) 2021-06-23 2024-01-15 Gilead Sciences Inc Compuestos moduladores de diacilglicerol quinasa.
JP7651018B2 (ja) 2021-06-23 2025-03-25 ギリアード サイエンシーズ, インコーポレイテッド ジアシルグリセロールキナーゼ調節化合物
JP7686091B2 (ja) 2021-06-23 2025-05-30 ギリアード サイエンシーズ, インコーポレイテッド ジアシルグリセロールキナーゼ調節化合物
AU2022299051B2 (en) 2021-06-23 2025-03-13 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
WO2023011456A1 (en) * 2021-08-03 2023-02-09 Beigene, Ltd. Pyrazolopyridinone compounds
WO2023122772A1 (en) * 2021-12-22 2023-06-29 Gossamer Bio Services, Inc. Oxime derivatives useful as t cell activators
WO2023122777A1 (en) * 2021-12-22 2023-06-29 Gossamer Bio Services, Inc. Oxime derivatives useful as t cell activators
CN118451073A (zh) * 2021-12-29 2024-08-06 百济神州有限公司 杂环化合物
WO2023150186A1 (en) * 2022-02-01 2023-08-10 Arvinas Operations, Inc. Dgk targeting compounds and uses thereof
WO2023165525A1 (en) * 2022-03-01 2023-09-07 Insilico Medicine Ip Limited Diacylglycerol kinase (dgk) alpha inhibitors and uses thereof
EP4486741A4 (en) * 2022-03-01 2026-04-08 Insilico Medicine Ip Ltd Diacylglycerol Kinase (DGK) Alpha Inhibitors and Their Uses
CN118974049A (zh) * 2022-03-31 2024-11-15 益方生物科技(上海)股份有限公司 激酶抑制剂,其制备方法和用途
US20250215014A1 (en) * 2022-03-31 2025-07-03 InventisBio Co., Ltd. Kinase inhibitors, preparation methods and uses thereof
US12600723B2 (en) 2022-07-18 2026-04-14 Incyte Corporation Tetracyclic compounds as DGK inhibitors
US12600722B2 (en) 2022-07-18 2026-04-14 Incyte Corporation Tetracyclic compounds as DGK inhibitors
CN119677740A (zh) * 2022-08-09 2025-03-21 百时美施贵宝公司 用作t细胞活化剂的叔胺取代的双环化合物
EP4658650A1 (en) * 2023-02-02 2025-12-10 Beone Medicines I GmbH Heterocyclic compounds
EP4658655A1 (en) * 2023-02-02 2025-12-10 Beone Medicines I GmbH Condensed heterocyclic compounds as inhibitor of diacylglycerol kinases
JP2026505790A (ja) * 2023-02-02 2026-02-18 ビーワン メディシンズ ワン ゲーエムベーハー ジアシルグリセロールキナーゼの阻害剤としての縮合ヘテロ環式化合物
EP4661869A1 (en) 2023-02-06 2025-12-17 Bayer Aktiengesellschaft Combinations of dgk (diacylglycerol kinase) inhibitors and immune checkpoint inhibitors and modulators
WO2025030002A2 (en) * 2023-08-02 2025-02-06 Arvinas Operations, Inc. Dgk targeting compounds and uses thereof
WO2025051110A1 (en) * 2023-09-04 2025-03-13 Insilico Medicine Ip Limited Combinations treatments of diacylglycerol kinase (dgk) alpha inhibitors and other therapies

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020006016A1 (en) * 2018-06-27 2020-01-02 Bristol-Myers Squibb Company Naphthyridinone compounds useful as t cell activators
WO2020006018A1 (en) * 2018-06-27 2020-01-02 Bristol-Myers Squibb Company Substituted naphthyridinone compounds useful as t cell activators
WO2020071550A1 (ja) * 2018-10-04 2020-04-09 京都薬品工業株式会社 Cdk8阻害剤およびその用途

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2544939B2 (ja) * 1987-09-01 1996-10-16 大塚製薬株式会社 ベンゾヘテロ環誘導体
TWI380996B (zh) 2004-09-17 2013-01-01 Hoffmann La Roche 抗ox40l抗體
PT2343320T (pt) 2005-03-25 2018-01-23 Gitr Inc Anticorpos anti-gitr e as suas utilizações
PL1879573T3 (pl) 2005-05-10 2013-05-31 Incyte Holdings Corp Modulatory 2,3-dioksygenazy indoloaminy i sposoby ich zastosowania
PT1907424E (pt) 2005-07-01 2015-10-09 Squibb & Sons Llc Anticorpos monoclonais humanos para o ligando 1 de morte programada (pd-l1)
US8450351B2 (en) 2005-12-20 2013-05-28 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
CL2007002650A1 (es) 2006-09-19 2008-02-08 Incyte Corp Compuestos derivados de heterociclo n-hidroxiamino; composicion farmaceutica, util para tratar cancer, infecciones virales y desordenes neurodegenerativos entre otras.
WO2008036642A2 (en) 2006-09-19 2008-03-27 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
EP1987839A1 (en) 2007-04-30 2008-11-05 I.N.S.E.R.M. Institut National de la Sante et de la Recherche Medicale Cytotoxic anti-LAG-3 monoclonal antibody and its use in the treatment or prevention of organ transplant rejection and autoimmune disease
US8591886B2 (en) 2007-07-12 2013-11-26 Gitr, Inc. Combination therapies employing GITR binding molecules
EP2044949A1 (en) 2007-10-05 2009-04-08 Immutep Use of recombinant lag-3 or the derivatives thereof for eliciting monocyte immune response
US10047066B2 (en) 2007-11-30 2018-08-14 Newlink Genetics Corporation IDO inhibitors
WO2009156652A1 (fr) 2008-05-29 2009-12-30 Saint-Gobain Centre De Recherches Et D'etudes Europeen Structure en nid d'abeille a base de titanate d'aluminium
AR072999A1 (es) 2008-08-11 2010-10-06 Medarex Inc Anticuerpos humanos que se unen al gen 3 de activacion linfocitaria (lag-3) y los usos de estos
EP3255060A1 (en) 2008-12-09 2017-12-13 F. Hoffmann-La Roche AG Anti-pd-l1 antibodies and their use to enhance t-cell function
KR101790802B1 (ko) 2009-09-03 2017-10-27 머크 샤프 앤드 돔 코포레이션 항-gitr 항체
EP2493862B1 (en) 2009-10-28 2016-10-05 Newlink Genetics Corporation Imidazole derivatives as ido inhibitors
ES2722300T3 (es) 2009-12-10 2019-08-09 Hoffmann La Roche Anticuerpos que se unen preferentemente al dominio extracelular 4 de CSF1R y su uso
EP2542256B1 (en) 2010-03-04 2019-05-22 MacroGenics, Inc. Antibodies reactive with b7-h3, immunologically active fragments thereof and uses thereof
US9169323B2 (en) 2010-03-05 2015-10-27 Hoffmann-La Roche Inc. Antibodies against human CSF-1R
JP5989547B2 (ja) 2010-03-05 2016-09-07 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト ヒトcsf−1rに対する抗体及びその使用
HRP20190047T1 (hr) 2010-05-04 2019-02-22 Five Prime Therapeutics, Inc. Protutijela koja se vežu na csf1r
MX337040B (es) 2010-09-09 2016-02-09 Pfizer Moleculas de union a 4-1bb.
NO2694640T3 (https=) 2011-04-15 2018-03-17
JP6072771B2 (ja) 2011-04-20 2017-02-01 メディミューン,エルエルシー B7−h1およびpd−1に結合する抗体およびその他の分子
KR101764096B1 (ko) 2011-11-28 2017-08-02 메르크 파텐트 게엠베하 항-pd-l1 항체 및 그의 용도
RU2658603C2 (ru) 2011-12-15 2018-06-21 Ф.Хоффманн-Ля Рош Аг Антитела против человеческого csf-1r и их применения
KR20140127855A (ko) 2012-02-06 2014-11-04 제넨테크, 인크. Csf1r 억제제를 사용하는 조성물 및 방법
AR090263A1 (es) 2012-03-08 2014-10-29 Hoffmann La Roche Terapia combinada de anticuerpos contra el csf-1r humano y las utilizaciones de la misma
RU2670743C9 (ru) 2012-05-11 2018-12-19 Файв Прайм Терапьютикс, Инк. Способы лечения состояний антителами, которые связывают рецептор колониестимулирующего фактора 1 (csf1r)
UY34887A (es) 2012-07-02 2013-12-31 Bristol Myers Squibb Company Una Corporacion Del Estado De Delaware Optimización de anticuerpos que se fijan al gen de activación de linfocitos 3 (lag-3) y sus usos
CN107759690A (zh) 2012-08-31 2018-03-06 戊瑞治疗有限公司 用结合群落刺激因子1受体(csf1r)的抗体治疗病状的方法
EA201591746A1 (ru) * 2013-03-14 2016-08-31 КОНВЕРДЖЕН ЭлЭлСи Способы и композиции для ингибирования бромодомен-содержащих белков

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020006016A1 (en) * 2018-06-27 2020-01-02 Bristol-Myers Squibb Company Naphthyridinone compounds useful as t cell activators
WO2020006018A1 (en) * 2018-06-27 2020-01-02 Bristol-Myers Squibb Company Substituted naphthyridinone compounds useful as t cell activators
WO2020071550A1 (ja) * 2018-10-04 2020-04-09 京都薬品工業株式会社 Cdk8阻害剤およびその用途

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
吴姗姗.《STN》.2023,1-12. *

Also Published As

Publication number Publication date
CN114846015A (zh) 2022-08-02
JP7677976B2 (ja) 2025-05-15
IL294273A (en) 2022-08-01
JP2023508054A (ja) 2023-02-28
US20230086933A1 (en) 2023-03-23
EP4081524B1 (en) 2025-01-29
MX2022007372A (es) 2022-07-12
CA3163003A1 (en) 2021-07-01
KR20220119458A (ko) 2022-08-29
BR112022012204A2 (pt) 2022-09-13
AU2020412472A1 (en) 2022-08-18
WO2021133752A1 (en) 2021-07-01
ES3013568T3 (en) 2025-04-14
EP4081524A1 (en) 2022-11-02

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