CN120247875A - 杂芳基氨基嘧啶酰胺自噬抑制剂及其使用方法 - Google Patents

杂芳基氨基嘧啶酰胺自噬抑制剂及其使用方法 Download PDF

Info

Publication number
CN120247875A
CN120247875A CN202510277561.4A CN202510277561A CN120247875A CN 120247875 A CN120247875 A CN 120247875A CN 202510277561 A CN202510277561 A CN 202510277561A CN 120247875 A CN120247875 A CN 120247875A
Authority
CN
China
Prior art keywords
amino
methyl
propyl
pyrazol
pyrimidin
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN202510277561.4A
Other languages
English (en)
Chinese (zh)
Inventor
D·L·弗林
Y·M·安
T·卡德维尔
L·沃盖蒂
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.)
Deciphera Pharmaceuticals LLC
Original Assignee
Deciphera Pharmaceuticals LLC
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Deciphera Pharmaceuticals LLC filed Critical Deciphera Pharmaceuticals LLC
Publication of CN120247875A publication Critical patent/CN120247875A/zh
Pending legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38Nitrogen atoms
    • 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • 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
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN202510277561.4A 2019-05-10 2020-05-08 杂芳基氨基嘧啶酰胺自噬抑制剂及其使用方法 Pending CN120247875A (zh)

Applications Claiming Priority (10)

Application Number Priority Date Filing Date Title
US201962846264P 2019-05-10 2019-05-10
US201962846260P 2019-05-10 2019-05-10
US62/846,260 2019-05-10
US62/846,264 2019-05-10
US201962911736P 2019-10-07 2019-10-07
US201962911733P 2019-10-07 2019-10-07
US62/911,736 2019-10-07
US62/911,733 2019-10-07
CN202080049743.1A CN114072397B (zh) 2019-05-10 2020-05-08 杂芳基氨基嘧啶酰胺自噬抑制剂及其使用方法
PCT/US2020/032090 WO2020231808A1 (en) 2019-05-10 2020-05-08 Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN202080049743.1A Division CN114072397B (zh) 2019-05-10 2020-05-08 杂芳基氨基嘧啶酰胺自噬抑制剂及其使用方法

Publications (1)

Publication Number Publication Date
CN120247875A true CN120247875A (zh) 2025-07-04

Family

ID=70847594

Family Applications (2)

Application Number Title Priority Date Filing Date
CN202510277561.4A Pending CN120247875A (zh) 2019-05-10 2020-05-08 杂芳基氨基嘧啶酰胺自噬抑制剂及其使用方法
CN202080049743.1A Active CN114072397B (zh) 2019-05-10 2020-05-08 杂芳基氨基嘧啶酰胺自噬抑制剂及其使用方法

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN202080049743.1A Active CN114072397B (zh) 2019-05-10 2020-05-08 杂芳基氨基嘧啶酰胺自噬抑制剂及其使用方法

Country Status (28)

Country Link
US (2) US11518758B2 (https=)
EP (2) EP3966206B1 (https=)
JP (2) JP7678763B2 (https=)
KR (1) KR20220019696A (https=)
CN (2) CN120247875A (https=)
AU (1) AU2020274011B2 (https=)
BR (1) BR112021022576A2 (https=)
CA (1) CA3139120A1 (https=)
CL (1) CL2021002953A1 (https=)
CO (1) CO2021016765A2 (https=)
DK (1) DK3966206T3 (https=)
ES (1) ES2962852T3 (https=)
FI (1) FI3966206T3 (https=)
HR (1) HRP20231310T1 (https=)
HU (1) HUE064465T2 (https=)
IL (2) IL287795B2 (https=)
LT (1) LT3966206T (https=)
MX (1) MX2021013662A (https=)
PE (1) PE20220592A1 (https=)
PH (1) PH12021552856A1 (https=)
PL (1) PL3966206T3 (https=)
PT (1) PT3966206T (https=)
RS (1) RS64755B1 (https=)
SG (1) SG11202112171XA (https=)
SI (1) SI3966206T1 (https=)
SM (1) SMT202300364T1 (https=)
TW (2) TWI888380B (https=)
WO (1) WO2020231808A1 (https=)

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN118416236A (zh) 2018-01-31 2024-08-02 德西费拉制药有限责任公司 治疗胃肠道间质瘤的组合疗法
IL276398B2 (en) 2018-01-31 2026-03-01 Deciphera Pharmaceuticals Llc Combination therapy for mastocytosis
WO2019217307A1 (en) 2018-05-07 2019-11-14 Mirati Therapeutics, Inc. Kras g12c inhibitors
EP3849535A4 (en) 2018-09-10 2022-06-29 Mirati Therapeutics, Inc. Combination therapies
EP3849537B1 (en) 2018-09-10 2024-10-23 Mirati Therapeutics, Inc. Combination therapies
EA202190749A1 (ru) 2018-09-10 2021-07-09 Мирати Терапьютикс, Инк. Способы комбинированной терапии
JP2022500385A (ja) 2018-09-10 2022-01-04 ミラティ セラピューティクス, インコーポレイテッド 組み合わせ療法
MX2021002804A (es) 2018-12-05 2021-07-15 Mirati Therapeutics Inc Terapias de combinacion.
BR112021012812A2 (pt) 2018-12-28 2021-12-07 Deciphera Pharmaceuticals Llc Csf1r inhibitors para uso e tratamento de câncer
EP3908283A4 (en) 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
WO2020185812A1 (en) 2019-03-11 2020-09-17 Teva Pharmaceuticals International Gmbh Solid state forms of ripretinib
PE20220597A1 (es) 2019-05-10 2022-04-22 Deciphera Pharmaceuticals Llc Inhibidores de la autofagia de fenilaminopirimidina amida y metodos de uso de estos
US11518758B2 (en) * 2019-05-10 2022-12-06 Deciphera Pharmaceuticals, Llc Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof
PE20221083A1 (es) 2019-06-17 2022-07-05 Deciphera Pharmaceuticals Llc Inhibidores de la autofagia de la amida aminopirimidina y sus metodos de uso
EP4013412B1 (en) 2019-08-12 2026-01-28 Deciphera Pharmaceuticals, LLC Ripretinib for treating gastrointestinal stromal tumors
TWI878335B (zh) 2019-08-12 2025-04-01 美商迪賽孚爾製藥有限公司 治療胃腸道基質瘤方法
MX2022002465A (es) 2019-08-29 2022-05-19 Mirati Therapeutics Inc Inhibidores de kras g12d.
WO2021061749A1 (en) 2019-09-24 2021-04-01 Mirati Therapeutics, Inc. Combination therapies
IL326597A (en) 2019-10-07 2026-04-01 Contineum Therapeutics Inc Muscarinic M1 acetylcholine receptor antagonists
US11752149B2 (en) 2019-12-02 2023-09-12 Pipeline Therapeutics, Inc. Muscarinic acetylcholine M1 receptor antagonists
PH12022551513A1 (en) 2019-12-20 2023-04-24 Mirati Therapeutics Inc Sos1 inhibitors
EP4084779B1 (en) 2019-12-30 2024-10-09 Deciphera Pharmaceuticals, LLC Compositions of 1-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3-phenylurea
MX2022008103A (es) 2019-12-30 2022-09-19 Deciphera Pharmaceuticals Llc Formulaciones de inhibidores de la cinasa amorfa y metodos de estas.
KR20220153582A (ko) 2020-02-14 2022-11-18 솔크 인스티튜트 포 바이올로지칼 스터디즈 마크로시클릭 ulk1/2 억제제
EP4210833A4 (en) 2020-09-11 2024-09-11 Mirati Therapeutics, Inc. CRYSTALLINE FORMS OF A KRAS G12C INHIBITOR
IL302807A (en) 2020-11-18 2023-07-01 Deciphera Pharmaceuticals Llc Gcn2 and perk kinase inhibitors and methods of use thereof
JP2023553492A (ja) 2020-12-15 2023-12-21 ミラティ セラピューティクス, インコーポレイテッド アザキナゾリン汎KRas阻害剤
EP4262803A4 (en) 2020-12-16 2025-03-12 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors
CN113527294A (zh) * 2021-08-25 2021-10-22 都创(上海)医药开发有限公司 Mrtx849化合物的晶型及其制备方法和用途
CN118834147A (zh) 2021-09-22 2024-10-25 杭州天玑济世生物科技有限公司 一类具有萘胺结构的小分子化合物及其应用
PE20250609A1 (es) 2021-12-03 2025-02-26 Deciphera Pharmaceuticals Llc Inhibidores de gcn2 y perk quinasa y metodos de uso de los mismos
CA3240263A1 (en) 2021-12-09 2023-06-15 Daniel L. Flynn Raf kinase inhibitors and methods of use thereof
US11779572B1 (en) 2022-09-02 2023-10-10 Deciphera Pharmaceuticals, Llc Methods of treating gastrointestinal stromal tumors
WO2024140401A1 (zh) * 2022-12-30 2024-07-04 捷思英达控股有限公司 作为激酶抑制剂的杂环化合物以及包括其的组合物
JP2026505741A (ja) 2023-01-19 2026-02-18 ハンジョウ イノゲート ファーマ カンパニー リミテッド キナーゼ阻害剤としての縮合三環式化合物
TW202509027A (zh) * 2023-05-04 2025-03-01 美商艾瑞斯卡公司 噻吩ulk1/2抑制劑及其用途
WO2025045203A1 (zh) * 2023-09-01 2025-03-06 葆元生物医药科技(杭州)有限公司 杂环化合物及其中间体和应用
US20250206720A1 (en) 2023-12-08 2025-06-26 Deciphera Pharmaceuticals, Llc Solid forms of an ulk inhibitor
WO2025122952A1 (en) 2023-12-08 2025-06-12 Deciphera Pharmaceuticals, Llc Formulations of vimseltinib
WO2025166161A1 (en) * 2024-02-02 2025-08-07 Deciphera Pharmaceuticals, Llc Ulk inhibitors and methods of use thereof
WO2025166180A1 (en) * 2024-02-02 2025-08-07 Deciphera Pharmaceuticals, Llc Ulk inhibitors and methods of use thereof
WO2025194599A1 (en) * 2024-03-18 2025-09-25 Galixir Technologies (Beijing) Limited Heterocycle ulk1/2 inhibitors and methods of use thereof
WO2025231106A1 (en) 2024-05-01 2025-11-06 Deciphera Pharmaceuticals, Llc Csf-1r inhibitors and methods of use thereof
CN118724900B (zh) * 2024-09-04 2025-01-28 浙江大学智能创新药物研究院 4-氨基-7-氮杂吲哚类化合物、其制备方法及应用

Family Cites Families (105)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19824922A1 (de) 1998-06-04 1999-12-09 Boehringer Ingelheim Pharma Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel
US6262088B1 (en) 1998-11-19 2001-07-17 Berlex Laboratories, Inc. Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants
GB9910807D0 (en) 1999-05-10 1999-07-07 Prometic Biosciences Limited Novel detoxification agents and their use
US6906067B2 (en) 1999-12-28 2005-06-14 Bristol-Myers Squibb Company N-heterocyclic inhibitors of TNF-α expression
AU783981C (en) 2000-05-08 2007-05-03 Janssen Pharmaceutica N.V. HIV replication inhibitors
PE20030008A1 (es) 2001-06-19 2003-01-22 Bristol Myers Squibb Co Inhibidores duales de pde 7 y pde 4
CA2450934A1 (en) 2001-06-19 2002-12-27 Marco Dodier Pyrimidine inhibitors of phosphodiesterase (pde) 7
AU2002316421B2 (en) 2001-06-26 2008-05-15 Bristol-Myers Squibb Company N-heterocyclic inhibitors of TNF-ALPHA expression
WO2003030909A1 (en) 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
WO2003032994A2 (de) 2001-10-17 2003-04-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg 5-substituierte 4-amino-2-phenylamino-pyrimidinderivate und ihre verwendung als beta-amyloid modulatoren
ATE407678T1 (de) 2001-10-17 2008-09-15 Boehringer Ingelheim Pharma Pyrimidinderivate, arzneimittel enthaltend diese verbindungen, deren verwendung und verfahren zu ihrer herstellung
JP4072615B2 (ja) 2002-03-05 2008-04-09 独立行政法人産業技術総合研究所 配位子を有する複素環化合物及びその製造方法、及びこの複素環化合物を用いる金属元素の固定化膜
JP2006508997A (ja) 2002-11-28 2006-03-16 シエーリング アクチエンゲゼルシャフト Chk−、Pdk−およびAkt−阻害性ピリミジン、それらの製造および薬剤としての使用
US7279576B2 (en) 2002-12-31 2007-10-09 Deciphera Pharmaceuticals, Llc Anti-cancer medicaments
US7144911B2 (en) 2002-12-31 2006-12-05 Deciphera Pharmaceuticals Llc Anti-inflammatory medicaments
US7202257B2 (en) 2003-12-24 2007-04-10 Deciphera Pharmaceuticals, Llc Anti-inflammatory medicaments
CL2004000306A1 (es) 2003-02-20 2005-04-08 Tibotec Pharm Ltd Compuestos derivados de pirimidina sustituidas con indano; proceso para su preparacion; composicion farmaceutica que lo comprende; combinacion farmaceutica; y su uso para el tratamiento o profilaxis de una enfermedad infecciosa.
EP1781659B1 (en) 2003-07-16 2008-11-05 Janssen Pharmaceutica N.V. Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors
WO2005012294A1 (en) 2003-07-30 2005-02-10 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
ATE506953T1 (de) 2003-08-07 2011-05-15 Rigel Pharmaceuticals Inc 2,4-pyrimidindiamin-verbindungen und verwendungen als antiproliferative mittel
US7754714B2 (en) 2004-05-18 2010-07-13 Rigel Pharmaceuticals, Inc. Cycloalkyl substituted pyrimidinediamine compounds and their uses
PL1756084T3 (pl) 2004-06-04 2009-06-30 Arena Pharm Inc Podstawione pochodne arylowe i heteroarylowe jako modulatory metabolizmu oraz profilaktyka i leczenie zaburzeń z metabolizmem związanych
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
CA2592118C (en) 2004-12-23 2015-11-17 Deciphera Pharmaceuticals, Llc Urea derivatives as enzyme modulators
BRPI0519794A2 (pt) 2005-01-07 2009-03-17 Hoffmann La Roche derivados de [4-(heteroaril)piperazin-1-il]-(fenil 2,5-substituìdo)metanona como inibidores de transportador de glicina 1 (glyt-1) para o tratamento de distúrbios neurológicos e neuropsiquiátricos
WO2006128129A2 (en) 2005-05-26 2006-11-30 Synta Pharmaceuticals Corp. Method for treating cancer
US20070032493A1 (en) 2005-05-26 2007-02-08 Synta Pharmaceuticals Corp. Method for treating B cell regulated autoimmune disorders
US8193206B2 (en) 2005-06-14 2012-06-05 Taigen Biotechnology Co., Ltd. Pyrimidine compounds
CN101484433A (zh) 2006-02-15 2009-07-15 艾博特公司 新的乙酰辅酶a羧化酶(acc)抑制剂及其在糖尿病、肥胖症和代谢综合征中的应用
MX2008014618A (es) 2006-05-15 2008-11-28 Irm Llc Composiciones y metodos para inhibidores de cinasas del receptor fgf.
RU2008152195A (ru) 2006-06-15 2010-07-20 БЕРИНГЕР ИНГЕЛЬХАЙМ ИНТЕРНАЦИОНАЛЬ ГмбХ (DE) 2-анилино-4-(гетероциклил)аминопиримидины, как ингибиторы протеинкиназы с-альфа
US7897762B2 (en) 2006-09-14 2011-03-01 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of proliferative diseases
US8188113B2 (en) 2006-09-14 2012-05-29 Deciphera Pharmaceuticals, Inc. Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
US7790756B2 (en) 2006-10-11 2010-09-07 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases
CA2673965A1 (en) 2006-12-28 2008-07-10 Taisho Pharmaceutical Co., Ltd. Pyrazolopyrimidine compound
WO2008131276A1 (en) 2007-04-20 2008-10-30 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases
AU2008317057B8 (en) 2007-10-22 2014-02-13 Merck Sharp & Dohme Corp. Bicyclic Heterocycle Derivatives and their use as modulators of the activity of GPR119
US20100056524A1 (en) 2008-04-02 2010-03-04 Mciver Edward Giles Compound
PE20100087A1 (es) 2008-06-25 2010-02-08 Irm Llc Compuestos y composiciones como inhibidores de cinasa
US20110098221A1 (en) 2008-06-26 2011-04-28 Hong Lin INHIBITORS OF Akt ACTIVITY
NZ603525A (en) 2008-06-27 2015-02-27 Celgene Avilomics Res Inc Pyrimidine based compound and uses thereof
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
JP5444365B2 (ja) 2008-10-29 2014-03-19 デシフェラ ファーマシューティカルズ,エルエルシー 抗癌活性および抗増殖活性を示すシクロプロパンアミドおよび類似物質
WO2010111406A2 (en) 2009-03-24 2010-09-30 Myriad Pharmaceuticals, Inc. Compounds and therapeutic uses thereof
US8410126B2 (en) 2009-05-29 2013-04-02 Boehringer Ingelheim International Gmbh Pyrimidine inhibitors of PKTK2
TW201100441A (en) 2009-06-01 2011-01-01 Osi Pharm Inc Amino pyrimidine anticancer compounds
PH12012500097A1 (en) 2009-07-21 2011-01-27 Shanghai Inst Organic Chem Potent small molecule inhibitors of autophagy, and methods of use thereof
KR101445012B1 (ko) 2009-12-17 2014-09-26 머크 샤프 앤드 돔 코포레이션 Syk 억제제로서의 아미노피리미딘
JP2013516422A (ja) 2009-12-30 2013-05-13 アビラ セラピューティクス, インコーポレイテッド タンパク質のリガンド−指向性共有的修飾
SG185073A1 (en) 2010-04-29 2012-12-28 Deciphera Pharmaceuticals Llc Cyclopropyl dicarboxamides and analogs exhibiting anti-cancer and anti-proliferative activites
CA2800998A1 (en) 2010-04-29 2011-11-10 Deciphera Pharmaceuticals, Llc Pyridone amides and analogs exhibiting anti-cancer and anti-proliferative activities
ES2577829T3 (es) 2010-06-04 2016-07-19 F. Hoffmann-La Roche Ag Derivados de aminopirimidina como moduladores de la LRRK2
WO2012033195A1 (ja) 2010-09-10 2012-03-15 京都薬品工業株式会社 複素環化合物
NO2638031T3 (https=) 2010-11-10 2018-03-10
US20130324532A1 (en) 2011-02-17 2013-12-05 Cancer Therapeutics Crc Pty Limited Fak inhibitors
EP2736901A1 (en) * 2011-07-28 2014-06-04 Cellzome Limited Heterocyclyl pyrimidine analogues as jak inhibitors
JP2015507606A (ja) 2011-11-22 2015-03-12 デシフェラ ファーマシューティカルズ,エルエルシー 抗癌および抗増殖作用を示すピリドンアミドおよび類似体
MX348920B (es) 2011-11-29 2017-07-04 Genentech Inc Derivados de 2-(fenil o pirid-3-il)aminopirimidina como moduladores de proteina cinasa 2 de repeticion rica en leucina (lrrk2) para el tratamiento de la enfermedad de parkinson.
US9145402B2 (en) 2011-11-29 2015-09-29 Genentech, Inc. Aminopyrimidine derivatives as LRRK2 modulators
EP2785381B1 (en) 2011-11-30 2016-05-18 F.Hoffmann-La Roche Ag Fluorine-18 and carbon-11 labeled radioligands for positron emission tomography (pet) imaging for lrrk2
CN103159736B (zh) 2011-12-10 2015-05-13 通化济达医药有限公司 取代的吡唑激酶抑制剂
AR090151A1 (es) 2012-03-07 2014-10-22 Lilly Co Eli Compuestos inhibidores de raf
WO2013134298A1 (en) 2012-03-07 2013-09-12 Deciphera Pharmaceuticals, Llc Raf inhibitor compounds
GB201204384D0 (en) 2012-03-13 2012-04-25 Univ Dundee Anti-flammatory agents
US8461179B1 (en) 2012-06-07 2013-06-11 Deciphera Pharmaceuticals, Llc Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
WO2014031928A2 (en) 2012-08-24 2014-02-27 Philip Jones Heterocyclic modulators of hif activity for treatment of disease
WO2014078378A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014086102A1 (zh) 2012-12-06 2014-06-12 山东亨利医药科技有限责任公司 作为酪氨酸激酶抑制剂的吲哚满酮衍生物
WO2014145029A2 (en) 2013-03-15 2014-09-18 Deciphera Pharmaceuticals, Llc N-acyl-n'-(pyridin-2-yl) ureas and analogs exhibiting anti-cancer and anti-proliferative activities
WO2014145015A2 (en) 2013-03-15 2014-09-18 Deciphera Pharmaceuticals, Llc Imidazolidinones and analogs exhibiting anti-cancer and anti-proliferative activities
DK2968286T3 (en) 2013-03-15 2018-01-02 Deciphera Pharmaceuticals Llc 2-AMINOPYRIMIDIN-6-ONES AND ANALOGS THAT HAVE ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES
US9012635B2 (en) 2013-03-15 2015-04-21 Deciphera Pharmaceuticals, Llc Pyridone amides and analogs exhibiting anti-cancer and anti-proliferative activities
WO2014145023A1 (en) 2013-03-15 2014-09-18 Deciphera Pharmaceuticals, Llc 1,2,4-triazol-5-ones and analogs exhibiting anti-cancer and anti-proliferative activities
JP6364472B2 (ja) 2013-03-15 2018-07-25 デシフェラ ファーマシューティカルズ,エルエルシー 抗がんおよび抗増殖活性を示すn−アシル−n’−(ピリジン−2−イル)尿素および類似体
CN103242341B (zh) 2013-04-19 2015-12-09 中国科学院广州生物医药与健康研究院 噻吩并2,4取代嘧啶类化合物及其药物组合物与应用
US9783504B2 (en) 2013-07-09 2017-10-10 Dana-Farber Cancer Institute, Inc. Kinase inhibitors for the treatment of disease
KR101879422B1 (ko) 2013-09-18 2018-07-17 베이징 한미 파마슈티컬 컴퍼니 리미티드 Btk 및/또는 jak3 키나제의 활성을 억제하는 화합물
WO2015039613A1 (zh) 2013-09-18 2015-03-26 北京韩美药品有限公司 抑制btk和/或jak3激酶活性的化合物
PH12016500676B1 (en) 2013-10-18 2022-07-20 Eisai R&D Man Co Ltd Pyrimidine fgfr4 inhibitors
BR112016008632A8 (pt) 2013-10-21 2020-03-17 Merck Patent Gmbh compostos de heteroarila como inibidores de btk, seus usos, e composição farmacêutica
US9457019B2 (en) 2013-11-07 2016-10-04 Deciphera Pharmaceuticals, Llc Methods for inhibiting tie-2 kinase useful in the treatment of cancer
WO2015123722A1 (en) 2014-02-19 2015-08-27 Bionomics Limited Inhibitors
US20150284341A1 (en) 2014-04-07 2015-10-08 Catylix, Inc. Fluoroalkyl-substituted derivatives of pyridine, pyrimidine, and pyrazine
US10266549B2 (en) * 2014-08-25 2019-04-23 Salk Institute For Biological Studies ULK1 inhibitors and methods using same
EP3056202A1 (en) 2015-02-16 2016-08-17 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Benzopyrrolidone derivatives possessing antiviral and anticancer properties
WO2016135163A1 (en) 2015-02-25 2016-09-01 F. Hoffmann-La Roche Ag Alkynyl alcohols and methods of use
CN108348779A (zh) 2015-08-02 2018-07-31 H·李·莫菲特癌症中心研究有限公司 Ack1/tnk2酪氨酸激酶的抑制剂
WO2017066428A1 (en) 2015-10-13 2017-04-20 H. Lee Moffitt Cancer Center & Research Institute, Inc. Brd4-kinase inhibitors as cancer therapeutics
US11028080B2 (en) 2016-03-11 2021-06-08 Denali Therapeutics Inc. Substituted pyrimidines as LRKK2 inhibitors
CN108239069B (zh) 2016-12-26 2021-01-05 南京药捷安康生物科技有限公司 一种用于成纤维细胞生长因子受体的抑制剂及其用途
AU2018226771B2 (en) 2017-02-28 2023-11-23 Dana-Farber Cancer Institute, Inc. Uses of pyrimidopyrimidinones as SIK inhibitors
MY205552A (en) 2017-05-30 2024-10-25 Deciphera Pharmaceuticals Inc Use of 1-[4-bromo-5-[1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl]-2-fluorophenyl ]-3-phenylurea and analogs for the treatment of cancers associated with genetic abnormalities in platelet derived growth factor receptor alpha
CN109535132B (zh) * 2017-09-21 2021-07-20 北京赛特明强医药科技有限公司 2-取代吡唑氨基-4-取代氨基-5-嘧啶甲酰胺类化合物、组合物及其应用
IL276398B2 (en) 2018-01-31 2026-03-01 Deciphera Pharmaceuticals Llc Combination therapy for mastocytosis
EA202092305A1 (ru) 2018-03-27 2020-12-07 Нейропор Терапиз, Инк. Соединения в качестве модуляторов сигнализации tlr2
KR102803762B1 (ko) 2018-04-10 2025-05-09 뉴로포레 테라피스, 인코포레이티드 Pi3-키나제 및 오토파지 경로의 조절인자로서의 트리-치환된 아릴 및 헤테로아릴 유도체
BR112021012812A2 (pt) 2018-12-28 2021-12-07 Deciphera Pharmaceuticals Llc Csf1r inhibitors para uso e tratamento de câncer
BR112021022237A2 (pt) 2019-05-10 2022-03-29 Janssen Biotech Inc Queladores macrocíclicos e métodos de uso dos mesmos
US11518758B2 (en) 2019-05-10 2022-12-06 Deciphera Pharmaceuticals, Llc Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof
PE20220597A1 (es) 2019-05-10 2022-04-22 Deciphera Pharmaceuticals Llc Inhibidores de la autofagia de fenilaminopirimidina amida y metodos de uso de estos
SG11202110561XA (en) 2019-05-10 2021-10-28 Cersci Therapeutics Inc Manufacturing methods and polymorphs of a thiazoline anti-hyperalgesic agent
PE20221083A1 (es) 2019-06-17 2022-07-05 Deciphera Pharmaceuticals Llc Inhibidores de la autofagia de la amida aminopirimidina y sus metodos de uso
KR20220150270A (ko) 2019-10-07 2022-11-10 칼리오페, 인크. Gpr119 효능제
US12458630B2 (en) 2020-01-14 2025-11-04 The Regents Of The University Of California Combination therapy for cancer
WO2023108110A2 (en) 2021-12-10 2023-06-15 Verastem, Inc. Combination therapy for treating abnormal cell growth

Also Published As

Publication number Publication date
IL287795B1 (en) 2025-01-01
CA3139120A1 (en) 2020-11-19
MX2021013662A (es) 2022-03-11
TWI888380B (zh) 2025-07-01
AU2024203193A1 (en) 2024-06-06
TW202108574A (zh) 2021-03-01
DK3966206T3 (da) 2023-11-13
WO2020231808A1 (en) 2020-11-19
AU2020274011A1 (en) 2021-11-25
AU2020274011B2 (en) 2024-02-15
RS64755B1 (sr) 2023-11-30
EP4295846A3 (en) 2024-02-28
FI3966206T3 (fi) 2023-10-20
JP2025118762A (ja) 2025-08-13
IL287795B2 (en) 2025-05-01
SI3966206T1 (sl) 2023-12-29
CN114072397A (zh) 2022-02-18
LT3966206T (lt) 2023-11-10
CN114072397B (zh) 2025-03-28
US12479833B2 (en) 2025-11-25
SG11202112171XA (en) 2021-12-30
HRP20231310T1 (hr) 2024-02-02
PL3966206T3 (pl) 2024-01-29
PH12021552856A1 (en) 2022-12-19
IL317676A (en) 2025-02-01
JP7678763B2 (ja) 2025-05-16
JP2022531932A (ja) 2022-07-12
SMT202300364T1 (it) 2023-11-13
ES2962852T3 (es) 2024-03-21
EP3966206B1 (en) 2023-08-09
US20230047915A1 (en) 2023-02-16
US20200354346A1 (en) 2020-11-12
HUE064465T2 (hu) 2024-04-28
CL2021002953A1 (es) 2022-07-15
IL287795A (en) 2022-01-01
CO2021016765A2 (es) 2022-04-08
EP4295846A2 (en) 2023-12-27
EP3966206A1 (en) 2022-03-16
TW202544009A (zh) 2025-11-16
US11518758B2 (en) 2022-12-06
PT3966206T (pt) 2023-11-10
KR20220019696A (ko) 2022-02-17
BR112021022576A2 (pt) 2022-01-25
PE20220592A1 (es) 2022-04-22

Similar Documents

Publication Publication Date Title
CN114072397B (zh) 杂芳基氨基嘧啶酰胺自噬抑制剂及其使用方法
CN114127057B (zh) 苯基氨基嘧啶酰胺自噬抑制剂及其使用方法
JP7626722B2 (ja) アミノピリミジンアミドオートファジー阻害剤およびその使用方法
AU2024203193B2 (en) Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof
US20260042750A1 (en) Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof
HK40102041A (en) Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof
HK40062277B (en) Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof
HK40062277A (en) Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof
HK40102390A (en) Phenylaminopyrimidine amide autophagy inhibitors and methods of use thereof

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination