CN110678466B - 作为hpk1抑制剂的二氮杂萘类 - Google Patents

作为hpk1抑制剂的二氮杂萘类 Download PDF

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Publication number
CN110678466B
CN110678466B CN201880034930.5A CN201880034930A CN110678466B CN 110678466 B CN110678466 B CN 110678466B CN 201880034930 A CN201880034930 A CN 201880034930A CN 110678466 B CN110678466 B CN 110678466B
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alkyl
optionally substituted
compound
amino
mmol
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CN110678466A (zh
Inventor
B·陈
B·丹尼尔斯
J·德罗布尼克
L·加扎德
T·赫夫伦
M·赫斯特斯
梁军
S·马尔霍特拉
R·门登卡
N·拉贾帕克萨
M·肖
C·斯蒂瓦拉
J·泰利斯
王炜如
魏斌清
周爱和
M·W·卡特赖特
E·甘西亚
G·琼斯
M·兰奇伯里
A·马丁
E·西沃德
D·法沃
K·C·方
胡永韩
A·古德
胡百华
陆爱军
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further 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
    • A61K31/495—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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61K31/535—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
    • A61K31/535—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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • 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
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • 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
    • 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
    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D497/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D497/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D497/04—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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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201880034930.5A 2017-03-30 2018-03-30 作为hpk1抑制剂的二氮杂萘类 Active CN110678466B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN2017078792 2017-03-30
CNPCT/CN2017/078792 2017-03-30
CNPCT/CN2018/076909 2018-02-15
CN2018076909 2018-02-15
PCT/US2018/025562 WO2018183956A1 (en) 2017-03-30 2018-03-30 Naphthyridines as inhibitors of hpk1

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CN110678466A CN110678466A (zh) 2020-01-10
CN110678466B true CN110678466B (zh) 2023-01-31

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US (2) US10407424B2 (enExample)
EP (1) EP3601284B1 (enExample)
JP (1) JP7154221B2 (enExample)
KR (1) KR20190136028A (enExample)
CN (1) CN110678466B (enExample)
AU (1) AU2018244935A1 (enExample)
BR (1) BR112019018093A2 (enExample)
CA (1) CA3052492A1 (enExample)
IL (1) IL268262A (enExample)
MX (1) MX2019011511A (enExample)
TW (1) TW201904964A (enExample)
WO (1) WO2018183956A1 (enExample)

Families Citing this family (83)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2018244935A1 (en) * 2017-03-30 2019-08-15 F. Hoffmann-La Roche Ag Naphthyridines as inhibitors of HPK1
JP6836693B2 (ja) * 2017-09-28 2021-03-03 シーストーン・ファーマスーティカルズ・（スージョウ）・カンパニー・リミテッドＣｓｔｏｎｅ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ （Ｓｕｚｈｏｕ） Ｃｏ．， Ｌｔｄ． Ａ２ａ受容体アンタゴニストとしての縮合環誘導体
EP3707138B1 (en) 2017-11-06 2022-07-13 Bristol-Myers Squibb Company Isofuranone compounds useful as hpk1 inhibitors
CR20200347A (es) 2018-02-13 2020-09-23 Gilead Sciences Inc Inhibidores pd-1/pd-l1
EP3765459A1 (en) 2018-03-13 2021-01-20 Shire Human Genetic Therapies, Inc. Substituted imidazopyridines as inhibitors of plasma kallikrein and uses thereof
TWI712412B (zh) 2018-04-19 2020-12-11 美商基利科學股份有限公司 Pd‐1/pd‐l1抑制劑
SG11202012425QA (en) 2018-07-13 2021-01-28 Gilead Sciences Inc Pd-1/pd-l1 inhibitors
TW202012405A (zh) * 2018-07-24 2020-04-01 瑞士商赫孚孟拉羅股份公司 萘啶化合物及其用途
EP3856724A1 (en) * 2018-09-30 2021-08-04 F. Hoffmann-La Roche AG Cinnoline compounds and for the treatment of hpk1-dependent disorders such as cancer
US11203591B2 (en) 2018-10-31 2021-12-21 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds
WO2020092528A1 (en) 2018-10-31 2020-05-07 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity
WO2020120257A1 (en) 2018-12-11 2020-06-18 Bayer Aktiengesellschaft Substituted pyrrolopyridine-derivatives
US12492194B2 (en) 2019-03-26 2025-12-09 Janssen Pharmaceutica Nv HPK1 inhibitors
US12486264B2 (en) 2019-03-26 2025-12-02 Janssen Pharmaceutica Nv Bicyclic HPK1 inhibitors
EP3972695A1 (en) 2019-05-23 2022-03-30 Gilead Sciences, Inc. Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors
WO2020263830A1 (en) 2019-06-25 2020-12-30 Gilead Sciences, Inc. Flt3l-fc fusion proteins and methods of use
TWI848141B (zh) 2019-07-04 2024-07-11 英屬開曼群島商百濟神州有限公司 及其用途
TW202116753A (zh) * 2019-07-11 2021-05-01 大陸商南京征祥醫藥有限公司 以噌啉作為hpk1的抑制劑
US12459958B2 (en) 2019-07-17 2025-11-04 Beone Medicines I Gmbh Tricyclic compounds as HPK1 inhibitor and the use thereof
CN110483402B (zh) * 2019-08-12 2021-07-23 上海毕得医药科技股份有限公司 一种3-溴-5-苯基-1h-吡唑的合成方法
WO2021032148A1 (en) * 2019-08-21 2021-02-25 Beigene, Ltd. Aminopyrazine compounds as hpk1 inhibitor and the use thereof
MX2022002877A (es) * 2019-09-13 2022-08-08 Nimbus Saturn Inc Antagonistas de cinasa progenitora hematopoyetica 1 (hpk1) y sus usos.
DK4031547T3 (da) 2019-09-18 2024-09-09 Takeda Pharmaceuticals Co Plasmakallikreininhibitorer og anvendelser deraf
EP4031245A1 (en) 2019-09-18 2022-07-27 Takeda Pharmaceutical Company Limited Heteroaryl plasma kallikrein inhibitors
ES2973832T3 (es) 2019-10-18 2024-06-24 Forty Seven Inc Terapias combinadas para el tratamiento de síndromes mielodisplásicos y leucemia mieloide aguda
JP2022552748A (ja) 2019-10-31 2022-12-19 フォーティ セブン， インコーポレイテッド 抗ｃｄ４７及び抗ｃｄ２０による血液癌の治療
TWI778443B (zh) 2019-11-12 2022-09-21 美商基利科學股份有限公司 Mcl1抑制劑
IL294032A (en) 2019-12-24 2022-08-01 Carna Biosciences Inc Compounds that regulate diacylglycerol kinase
TW202140473A (zh) * 2020-01-15 2021-11-01 美商纜圖藥品公司 Map4k1抑制劑
TWI890283B (zh) 2020-02-14 2025-07-11 美商基利科學股份有限公司 結合ccr8之抗體及融合蛋白及其用途
CN113336747A (zh) * 2020-03-03 2021-09-03 轶诺(浙江)药业有限公司 新型hpk1抑制剂及其制备方法和应用
IL297327B2 (en) 2020-05-01 2026-01-01 Gilead Sciences Inc 4,2-dioxopyrimidine compounds CD73 inhibitors
WO2021249913A1 (en) 2020-06-09 2021-12-16 Bayer Aktiengesellschaft 2'-(quinolin-3-yl)-5',6'-dihydrospiro[azetidine-3,4'-pyrrolo[1,2-b]pyrazole]-1-carboxylate derivatives and related compounds as map4k1 (hpk1) inhibitors for the treatment of cancer
CN111965367A (zh) * 2020-07-23 2020-11-20 北京大学第三医院（北京大学第三临床医学院） Hip-55在作为gpcr偏向药物靶点中的应用
WO2022064459A1 (en) * 2020-09-28 2022-03-31 1ST Biotherapeutics, Inc. Indazoles as hematopoietic progenitor kinase 1 (hpk1) inhibitors and methods of using same
US20240174683A1 (en) 2021-02-05 2024-05-30 Bayer Aktiengesellschaft Map4k1 inhibitors
CN114907374B (zh) * 2021-02-07 2026-03-10 苏州信诺维医药科技股份有限公司 杂环化合物、其制备方法、药物组合物及应用
CN114907375B (zh) * 2021-02-07 2026-03-31 苏州信诺维医药科技股份有限公司 杂环化合物、其制备方法、药物组合物及应用
EP4291235A4 (en) 2021-02-12 2025-01-08 Nimbus Saturn, Inc. HPK1 ANTAGONISTS AND USES THEREOF
US11926625B2 (en) 2021-03-05 2024-03-12 Nimbus Saturn, Inc. HPK1 antagonists and uses thereof
CN115073308A (zh) * 2021-03-15 2022-09-20 苏州信礼发医药技术有限公司 1-氨甲基-1-环丙醇的合成方法
JP2024512497A (ja) * 2021-03-17 2024-03-19 武田薬品工業株式会社 血漿カリクレインの阻害剤
WO2022213062A1 (en) 2021-03-29 2022-10-06 Nimbus Saturn, Inc. Hpk1 antagonists and uses thereof
TW202304434A (zh) * 2021-04-08 2023-02-01 大陸商杭州阿諾生物醫藥科技有限公司 一種高活性的ｈｐｋ１激酶抑制劑
TW202302145A (zh) 2021-04-14 2023-01-16 美商基利科學股份有限公司 ＣＤ４７／ＳＩＲＰα結合及ＮＥＤＤ８活化酶Ｅ１調節次單元之共抑制以用於治療癌症
WO2022222951A1 (zh) * 2021-04-22 2022-10-27 浙江海正药业股份有限公司 芳香稠合环类衍生物及其制备方法和用途
WO2022245671A1 (en) 2021-05-18 2022-11-24 Gilead Sciences, Inc. Methods of using flt3l-fc fusion proteins
AU2022299051B2 (en) 2021-06-23 2025-03-13 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
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
MX2023014762A (es) 2021-06-23 2024-01-15 Gilead Sciences Inc Compuestos moduladores de diacilglicerol quinasa.
WO2023288254A1 (en) * 2021-07-14 2023-01-19 Blueprint Medicines Corporation Heterocyclic compounds as map4k1 inhibitors
AU2022375782B2 (en) 2021-10-28 2026-02-26 Gilead Sciences, Inc. Pyridizin-3(2h)-one derivatives
JP7787991B2 (ja) 2021-10-29 2025-12-17 ギリアード サイエンシーズ， インコーポレイテッド Ｃｄ７３化合物
US20230220106A1 (en) 2021-12-08 2023-07-13 Dragonfly Therapeutics, Inc. Antibodies targeting 5t4 and uses thereof
WO2023107956A1 (en) 2021-12-08 2023-06-15 Dragonfly Therapeutics, Inc. Proteins binding nkg2d, cd16 and 5t4
US12122764B2 (en) 2021-12-22 2024-10-22 Gilead Sciences, Inc. IKAROS zinc finger family degraders and uses thereof
KR20240123836A (ko) 2021-12-22 2024-08-14 길리애드 사이언시즈, 인코포레이티드 이카로스 아연 핑거 패밀리 분해제 및 이의 용도
TW202340168A (zh) 2022-01-28 2023-10-16 美商基利科學股份有限公司 Ｐａｒｐ７抑制劑
WO2023178181A1 (en) 2022-03-17 2023-09-21 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
KR20240165995A (ko) 2022-03-24 2024-11-25 길리애드 사이언시즈, 인코포레이티드 Trop-2 발현 암의 치료를 위한 병용요법
TWI876305B (zh) 2022-04-05 2025-03-11 美商基利科學股份有限公司 用於治療結腸直腸癌之組合療法
WO2023193759A1 (en) * 2022-04-07 2023-10-12 Insilico Medicine Ip Limited Hpk1 antagonists and uses thereof
CR20240451A (es) 2022-04-21 2024-12-04 Gilead Sciences Inc Compuestos de modulación de kras g12d
EP4539840A4 (en) * 2022-06-17 2026-04-15 Sundance Biosciences Inc Kinase Modulators and Their Methods of Use
WO2024003773A1 (en) * 2022-07-01 2024-01-04 Pfizer Inc. 2,7-naphthyridine compounds as mastl inhibitors
KR20250028371A (ko) 2022-07-01 2025-02-28 길리애드 사이언시즈, 인코포레이티드 Cd73 화합물
EP4590663A2 (en) * 2022-09-21 2025-07-30 Takeda Pharmaceutical Company Limited Synthesis of cyclopropane carboxylic acids
WO2024064668A1 (en) 2022-09-21 2024-03-28 Gilead Sciences, Inc. FOCAL IONIZING RADIATION AND CD47/SIRPα DISRUPTION ANTICANCER COMBINATION THERAPY
US20260092074A1 (en) * 2022-09-23 2026-04-02 Guangzhou Vinnocent Pharmaceutical Limited Annelated Pyridines as Steroidogenesis Inhibitors, Preparation Method and Use Thereof
AU2023409398A1 (en) 2022-12-22 2025-06-05 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
AU2024252725A1 (en) 2023-04-11 2025-11-06 Gilead Sciences, Inc. Kras modulating compounds
CR20250446A (es) 2023-04-21 2025-12-02 Gilead Sciences Inc Inhibidores de prmt5 y usos de los mismos
WO2024243025A1 (en) * 2023-05-19 2024-11-28 Ikena Oncology, Inc. Naphthyl-substituted pyrido[4,3-d]pyrimidines and related compounds and their use in treating medical conditions
AU2024306338A1 (en) 2023-06-30 2026-01-08 Gilead Sciences, Inc. Kras modulating compounds
KR20260046403A (ko) 2023-07-26 2026-04-07 길리애드 사이언시즈, 인코포레이티드 Parp7 저해제
CN121620513A (zh) 2023-07-26 2026-03-06 吉利德科学公司 Parp7抑制剂
US20250101042A1 (en) 2023-09-08 2025-03-27 Gilead Sciences, Inc. Kras g12d modulating compounds
US20250109147A1 (en) 2023-09-08 2025-04-03 Gilead Sciences, Inc. Kras g12d modulating compounds
US20250154172A1 (en) 2023-11-03 2025-05-15 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
WO2025137640A1 (en) 2023-12-22 2025-06-26 Gilead Sciences, Inc. Azaspiro wrn inhibitors
WO2025245003A1 (en) 2024-05-21 2025-11-27 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
US20260098049A1 (en) 2024-08-12 2026-04-09 Gilead Sciences, Inc. Kras modulating compounds

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013063068A1 (en) * 2011-10-27 2013-05-02 Merck Sharp & Dohme Corp. Factor ixa inhibitors
CN104379583A (zh) * 2012-06-15 2015-02-25 广州源生医药科技有限公司 作为wnt信号传导抑制剂的化合物、组合物及其应用
CN105142641A (zh) * 2013-03-12 2015-12-09 广州源生医药科技有限公司 用于治疗癌症的化合物
WO2016205942A1 (en) * 2015-06-25 2016-12-29 University Health Network Hpk1 inhibitors and methods of using same

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
PT1907424E (pt) 2005-07-01 2015-10-09 Squibb & Sons Llc Anticorpos monoclonais humanos para o ligando 1 de morte programada (pd-l1)
US8088793B2 (en) 2007-08-15 2012-01-03 Cytokinetics, Inc. Certain chemical entities, compositions, and methods
JP2012500855A (ja) 2008-08-25 2012-01-12 アンプリミューン、インコーポレーテッド Ｐｄ−１アンタゴニストおよび感染性疾患を処置するための方法
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
WO2011066342A2 (en) 2009-11-24 2011-06-03 Amplimmune, Inc. Simultaneous inhibition of pd-l1/pd-l2
PL2504364T3 (pl) 2009-11-24 2017-12-29 Medimmune Limited Ukierunkowane środki wiążące przeciwko B7-H1
AU2018244935A1 (en) * 2017-03-30 2019-08-15 F. Hoffmann-La Roche Ag Naphthyridines as inhibitors of HPK1

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013063068A1 (en) * 2011-10-27 2013-05-02 Merck Sharp & Dohme Corp. Factor ixa inhibitors
CN104379583A (zh) * 2012-06-15 2015-02-25 广州源生医药科技有限公司 作为wnt信号传导抑制剂的化合物、组合物及其应用
CN105142641A (zh) * 2013-03-12 2015-12-09 广州源生医药科技有限公司 用于治疗癌症的化合物
WO2016205942A1 (en) * 2015-06-25 2016-12-29 University Health Network Hpk1 inhibitors and methods of using same

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