CN109195965B - Wdr5蛋白质-蛋白质结合的抑制剂 - Google Patents

Wdr5蛋白质-蛋白质结合的抑制剂 Download PDF

Info

Publication number
CN109195965B
CN109195965B CN201780024229.0A CN201780024229A CN109195965B CN 109195965 B CN109195965 B CN 109195965B CN 201780024229 A CN201780024229 A CN 201780024229A CN 109195965 B CN109195965 B CN 109195965B
Authority
CN
China
Prior art keywords
fluoro
phenyl
pyridine
carboxamide
oxo
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.)
Active
Application number
CN201780024229.0A
Other languages
English (en)
Chinese (zh)
Other versions
CN109195965A (zh
Inventor
R·阿瓦尔
C·A·泽佩达-维拉兹奎兹
G·波达
M·艾萨克
D·尤林
B·威尔逊
B·约瑟夫
Y·刘
P·苏布拉马尼安
A·马迈
M·普拉克施
J·K·斯蒂尔
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.)
Propelon Therapeutics
Original Assignee
Propelon Therapeutics
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 Propelon Therapeutics filed Critical Propelon Therapeutics
Publication of CN109195965A publication Critical patent/CN109195965A/zh
Application granted granted Critical
Publication of CN109195965B publication Critical patent/CN109195965B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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
    • A61K31/505—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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/10—Heterocyclic 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 carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/10—Heterocyclic 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 carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/10—Heterocyclic 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 linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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 two hetero rings
    • C07D417/12—Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic 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
    • C07D451/02—Heterocyclic 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
    • 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
    • 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
    • C07D487/02—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
    • C07D487/08—Bridged 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
    • C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyrrole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
CN201780024229.0A 2016-03-01 2017-03-01 Wdr5蛋白质-蛋白质结合的抑制剂 Active CN109195965B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662301673P 2016-03-01 2016-03-01
US62/301,673 2016-03-01
PCT/CA2017/050269 WO2017147700A1 (en) 2016-03-01 2017-03-01 Inhibitors of wdr5 protein-protein binding

Publications (2)

Publication Number Publication Date
CN109195965A CN109195965A (zh) 2019-01-11
CN109195965B true CN109195965B (zh) 2022-07-26

Family

ID=59743306

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201780024229.0A Active CN109195965B (zh) 2016-03-01 2017-03-01 Wdr5蛋白质-蛋白质结合的抑制剂

Country Status (17)

Country Link
US (2) US11319299B2 (https=)
EP (1) EP3423451B1 (https=)
JP (3) JP7624690B2 (https=)
KR (1) KR20180120720A (https=)
CN (1) CN109195965B (https=)
AU (1) AU2017226004B2 (https=)
BR (1) BR112018067392A2 (https=)
CA (1) CA3015406A1 (https=)
CL (1) CL2018002505A1 (https=)
CO (1) CO2018010504A2 (https=)
DK (1) DK3423451T3 (https=)
EA (1) EA038109B1 (https=)
EC (1) ECSP18073726A (https=)
IL (1) IL261472B (https=)
MX (1) MX2018010374A (https=)
WO (1) WO2017147700A1 (https=)
ZA (1) ZA201805879B (https=)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3015417A1 (en) 2016-03-01 2017-09-08 Propellon Therapeutics Inc. Inhibitors of wdr5 protein-protein binding
JP7624690B2 (ja) * 2016-03-01 2025-01-31 プロペロン セラピューティクス インコーポレイテッド Ｗｄｒ５タンパク質－タンパク質結合の阻害剤
EP3532464A4 (en) 2016-10-28 2020-07-08 Icahn School of Medicine at Mount Sinai COMPOSITIONS AND METHODS FOR THE TREATMENT OF EZH2 MEDIATION CANCER
JP2020514252A (ja) 2016-12-08 2020-05-21 アイカーン スクール オブ メディスン アット マウント シナイ Ｃｄｋ４／６媒介性がんを治療するための組成物および方法
PL3601233T3 (pl) 2017-03-27 2025-01-07 HYDRO-QUéBEC Sole do zastosowania w kompozycjach elektrolitowych lub jako dodatki do elektrod
MX2020002399A (es) * 2017-09-06 2020-07-22 Propellon Therapeutics Inc Inhibidores del enlace proteína-proteína de wdr5.
US10501466B2 (en) 2017-09-19 2019-12-10 Vanderbilt University WDR5 inhibitors and modulators
EP3736266A4 (en) * 2018-01-04 2021-01-06 Peking University Shenzhen Graduate School COMPOUND SIMULTANEOUSLY INHIBITING THE LSD1 AND HDAC TARGETS AND ITS APPLICATION
CA3092677A1 (en) 2018-03-06 2019-09-12 Icahn School Of Medicine At Mount Sinai Serine threonine kinase (akt) degradation / disruption compounds and methods of use
CN108715585A (zh) * 2018-04-23 2018-10-30 中国药科大学 苯基联三氮唑类mll1-wdr5蛋白-蛋白相互作用抑制剂
US10844044B2 (en) 2018-06-14 2020-11-24 Vanderbilt University WDR5 inhibitors and modulators
CA3104298A1 (en) 2018-06-21 2019-12-26 Icahn School Of Medicine At Mount Sinai Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use
US10807959B2 (en) 2018-08-16 2020-10-20 Vanderbilt University WDR5-MLL1 inhibitors and modulators
CN109734674B (zh) 2019-02-26 2022-08-26 中国药科大学 苯胺类wdr5蛋白-蛋白相互作用抑制剂及其制法和用途
WO2020179859A1 (ja) 2019-03-06 2020-09-10 第一三共株式会社 ピロロピラゾール誘導体
CN118908962A (zh) 2019-05-06 2024-11-08 西奈山伊坎医学院 作为hpk1的降解剂的异双功能化合物
CN111039860B (zh) * 2019-12-02 2022-09-13 河北科技大学 2-羟基-n-(4’-氯联苯-2-基)烟酰胺的合成方法及应用
CN113024538B (zh) * 2019-12-24 2022-09-09 南开大学 吡唑酰胺类化合物及其制备和在防治植物病菌病和杀虫中的应用
US12103924B2 (en) 2020-06-01 2024-10-01 Icahn School Of Medicine At Mount Sinai Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use
CN114539073A (zh) * 2022-02-18 2022-05-27 郑州萃智医药科技有限公司 3-溴-2-氯-4,6-二氟苯胺的合成方法
KR20250009417A (ko) * 2022-03-14 2025-01-17 후야바이오 인터내셔널, 엘엘씨 혈액-뇌 장벽 교차 mll1-wdr5 단백질-단백질 상호작용 저해제 화합물 및 이의 용도
EP4551560A4 (en) * 2022-03-14 2026-04-08 Huyabio Int Llc HALOALKYLPYRIDYLE TRIAZOLE PROTEIN-PROTEIN INTERACTION INHIBITOR MLL1-WDR5
AR129265A1 (es) 2022-05-12 2024-08-07 Syngenta Crop Protection Ag Compuestos de alcoxi-heteroaril-carboxamida o tioamida
WO2024002379A1 (zh) * 2022-07-01 2024-01-04 甘李药业股份有限公司 一种用作wdr5抑制剂的化合物或其可药用盐及其应用
WO2024015478A2 (en) * 2022-07-14 2024-01-18 Huyabio International, Llc Combination therapies of wdr5 inhibitors and pd-1 inhibitors
CN115974965B (zh) * 2022-08-31 2025-09-12 中国科学技术大学 一种靶向wdr5的多肽抑制剂及其用途
WO2026058961A1 (en) 2024-09-13 2026-03-19 Alivexis, Inc. Wdr5 inhibitors, compounds, pharmaceutical compositions, and methods of use thereof
CN119143715B (zh) * 2024-11-12 2025-03-14 天津匠新致成科技有限公司 二芳基团甲基哌嗪类化合物及其制备方法、药物组合物和应用
CN119661474A (zh) * 2024-12-16 2025-03-21 中国药科大学 一类羟肟酸类的双靶点化合物衍生物及其应用

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100355751C (zh) * 2000-03-29 2007-12-19 西克拉塞尔有限公司 2－取代的4－杂芳基－嘧啶、其组合物及其用途
CN101679266A (zh) * 2007-03-01 2010-03-24 诺瓦提斯公司 Pim激酶抑制剂及其应用方法
WO2011149874A2 (en) * 2010-05-26 2011-12-01 Schering Corporation N-phenyl imidazole carboxamide inhibitors of 3-phosphoinositide-dependent protein kinase-1
WO2014003124A1 (ja) * 2012-06-28 2014-01-03 富士フイルム株式会社 新規なアミド誘導体またはその塩
CN105175284A (zh) * 2015-07-21 2015-12-23 中国药科大学 酰胺类化合物、制备方法及其医药用途

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH09505050A (ja) 1993-11-12 1997-05-20 ジ・アップジョン・カンパニー ピリミジン−チオアルキルおよびアルキルエーテル化合物
JPH0959236A (ja) 1995-08-23 1997-03-04 Dai Ichi Seiyaku Co Ltd ベンズアミド化合物
US20010051719A1 (en) 1996-12-19 2001-12-13 Smithkline Beecham P.L.C. Novel compounds
US6541669B1 (en) 1998-06-08 2003-04-01 Theravance, Inc. β2-adrenergic receptor agonists
DE19952146A1 (de) 1999-10-29 2001-06-07 Boehringer Ingelheim Pharma Arylalkane, Arylalkene und Aryl-azaalkane, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
JP2002193938A (ja) 2000-12-01 2002-07-10 Bayer Ag ４−アリールピリジン誘導体
WO2002088101A2 (en) 2001-04-27 2002-11-07 Vertex Pharmaceuticals Incorporated Inhibitors of bace
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
KR20050029209A (ko) 2002-07-15 2005-03-24 미리어드 제네틱스, 인크. 화합물, 조성물 및 이의 사용방법
US7312341B2 (en) 2002-09-09 2007-12-25 Cgi Pharmaceuticals, Inc. 6-aryl-imidazo[1,2-a] pyrazin-8-ylamines, method of making, and method of use thereof
GB0412072D0 (en) 2004-05-28 2004-06-30 Syngenta Participations Ag Chemical compounds
JP4688876B2 (ja) 2004-06-10 2011-05-25 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼ阻害剤としての化合物および組成物
RU2368602C2 (ru) 2005-01-26 2009-09-27 Айрм Ллк Соединения и композиции в качестве ингибиторов протеинкиназ
WO2006124731A2 (en) 2005-05-12 2006-11-23 Irm Llc Compounds and compositions as protein kinase inhibitors
DE102005022977A1 (de) 2005-05-19 2006-12-07 Merck Patent Gmbh Phenylchinazolinderivate
US20070254894A1 (en) 2006-01-10 2007-11-01 Kane John L Jr Novel small molecules with selective cytotoxicity against human microvascular endothelial cell proliferation
JP2009525978A (ja) 2006-02-06 2009-07-16 アイアールエム・リミテッド・ライアビリティ・カンパニー プロテインキナーゼ阻害剤としての化合物および組成物
EP2606890A1 (en) 2006-04-05 2013-06-26 Novartis AG Combinations comprising BCR-ABL/C-KIT/PDGF-R TK inhibitors for treating cancer
AU2008266290A1 (en) 2007-06-15 2008-12-24 Irm Llc Protein kinase inhibitors and methods for using thereof
CN101875617B (zh) 2009-03-23 2015-05-20 中国医学科学院药物研究所 烷氧基取代芳环的氨甲酰基类芳酸化合物及其制法和用途
CN102574830A (zh) 2009-05-07 2012-07-11 阿斯利康(瑞典)有限公司 取代的1-氰基乙基杂环基甲酰胺化合物750
EP2558085B1 (en) 2010-04-16 2017-08-30 Athenex, Inc. Compositions and methods for the prevention and treatment of cancer
WO2011156557A2 (en) 2010-06-11 2011-12-15 Thomas James B Compounds active at the neurotensin receptor
CN103189067A (zh) * 2010-06-16 2013-07-03 密执安大学评议会 Wdr5与其结合配偶体的相互作用的抑制及治疗方法
WO2012066065A1 (en) 2010-11-17 2012-05-24 Novartis Ag Phenyl-heteroaryl amine compounds and their uses
WO2014048878A1 (en) 2012-09-26 2014-04-03 Evotec (Uk) Ltd. Phenyl- or pyridyl- pyrrolo[2,3b]pyrazine derivatives useful in the treatment or prevention of proliferative disorders or dysplasia
CN105051005B (zh) 2012-10-12 2017-06-13 武田药品工业株式会社 环丙胺化合物及其用途
EP2951170B1 (en) 2013-02-04 2018-10-24 Janssen Pharmaceutica NV Flap modulators
EP3079682A4 (en) 2013-12-13 2017-08-30 Dana-Farber Cancer Institute, Inc. Methods to treat lymphoplasmacytic lymphoma
US9856223B2 (en) 2013-12-13 2018-01-02 Dana-Farber Cancer Institute, Inc. Methods to treat lymphoplasmacytic lymphoma
CN104926801B (zh) 2014-03-22 2019-06-04 浙江大学 取代氮杂环类衍生物、含其的药物组合物及其在抗肿瘤中的应用
CN105585565B (zh) 2014-10-23 2019-10-01 中国医学科学院药物研究所 含2-苯胺基-4-噻唑基吡啶衍生物及其制法和药物组合物与用途
CN105837575B (zh) 2015-01-13 2019-01-15 四川大学 3-乙炔基吡唑并嘧啶衍生物及其制备方法和用途
CN116375797A (zh) 2016-03-01 2023-07-04 伊玛提克斯生物技术有限公司 用于膀胱癌和其他癌症免疫治疗的肽、肽组合物和细胞类药物
CA3015417A1 (en) 2016-03-01 2017-09-08 Propellon Therapeutics Inc. Inhibitors of wdr5 protein-protein binding
JP7624690B2 (ja) 2016-03-01 2025-01-31 プロペロン セラピューティクス インコーポレイテッド Ｗｄｒ５タンパク質－タンパク質結合の阻害剤
WO2017221092A1 (en) 2016-06-20 2017-12-28 Novartis Ag Triazolopyridine compounds and uses thereof
US10160763B2 (en) 2016-09-13 2018-12-25 Vanderbilt University WDR5 inhibitors and modulators
MX2020002399A (es) 2017-09-06 2020-07-22 Propellon Therapeutics Inc Inhibidores del enlace proteína-proteína de wdr5.
US10501466B2 (en) 2017-09-19 2019-12-10 Vanderbilt University WDR5 inhibitors and modulators
EP3870173A4 (en) 2018-10-24 2022-06-22 Vanderbilt University WDR5 INHIBITORS AND MODULATORS
WO2021026672A1 (en) 2019-08-09 2021-02-18 Novartis Ag Heterocyclic wdr5 inhibitors as anti-cancer compounds

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100355751C (zh) * 2000-03-29 2007-12-19 西克拉塞尔有限公司 2－取代的4－杂芳基－嘧啶、其组合物及其用途
CN101679266A (zh) * 2007-03-01 2010-03-24 诺瓦提斯公司 Pim激酶抑制剂及其应用方法
WO2011149874A2 (en) * 2010-05-26 2011-12-01 Schering Corporation N-phenyl imidazole carboxamide inhibitors of 3-phosphoinositide-dependent protein kinase-1
WO2014003124A1 (ja) * 2012-06-28 2014-01-03 富士フイルム株式会社 新規なアミド誘導体またはその塩
CN105175284A (zh) * 2015-07-21 2015-12-23 中国药科大学 酰胺类化合物、制备方法及其医药用途

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Pharmacological targeting of the Wdr5-MLL interaction in C/EBPa N-terminal leukemia;Florian Grebien et al.;《Nature chemical biology》;20150713;第11卷;第571-578页 *

Also Published As

Publication number Publication date
JP2024102151A (ja) 2024-07-30
JP2022071046A (ja) 2022-05-13
CA3015406A1 (en) 2017-09-08
KR20180120720A (ko) 2018-11-06
AU2017226004A1 (en) 2018-09-06
US11319299B2 (en) 2022-05-03
WO2017147700A1 (en) 2017-09-08
IL261472A (en) 2018-10-31
ZA201805879B (en) 2021-04-28
US20230219926A1 (en) 2023-07-13
JP2019512482A (ja) 2019-05-16
EA038109B1 (ru) 2021-07-07
BR112018067392A2 (pt) 2019-01-02
MX2018010374A (es) 2019-03-28
US12264147B2 (en) 2025-04-01
ECSP18073726A (es) 2018-11-30
CN109195965A (zh) 2019-01-11
EP3423451B1 (en) 2022-08-17
IL261472B (en) 2022-01-01
CO2018010504A2 (es) 2018-12-14
JP7624690B2 (ja) 2025-01-31
EP3423451A1 (en) 2019-01-09
EA201891974A1 (ru) 2019-04-30
AU2017226004B2 (en) 2021-07-22
CL2018002505A1 (es) 2019-01-04
DK3423451T3 (da) 2022-11-28
US20190112290A1 (en) 2019-04-18
EP3423451A4 (en) 2019-09-04

Similar Documents

Publication Publication Date Title
CN109195965B (zh) Wdr5蛋白质-蛋白质结合的抑制剂
JP7775430B2 (ja) Ｉｒａｋ４阻害剤としての二環式ヘテロシクリル誘導体
WO2023045960A1 (zh) 一种吡啶类衍生物及其用途
CN105492433B (zh) 6-(5-羟基-1h-吡唑-1-基)烟碱酰胺衍生物和其作为phd抑制剂的用途
CN105829308B (zh) 作为磷酸肌醇酯3-激酶抑制剂的异色烯衍生物
CN114585628A (zh) 囊性纤维化跨膜传导调节因子的调节剂
CN113105475B (zh) 布鲁顿氏酪氨酸激酶的抑制剂及其使用方法
CN116670143A (zh) 囊性纤维化跨膜传导调控因子的调节剂
CN108026105B (zh) TGFβ受体拮抗剂
CN106795147B (zh) 作为β-分泌酶抑制剂的环丙基稠合噻嗪-2-胺化合物和使用方法
CN111372926A (zh) Wdr5蛋白质-蛋白质结合的抑制剂
JP2019507179A (ja) Ｗｄｒ５タンパク質−タンパク質結合の阻害剤
CN112689636B (zh) 新型杂原子芳香族酰胺衍生物以及含有其的药剂
CN115836063A (zh) 作为运铁素(ferroportin)抑制剂的环烷基嘧啶
HK40046970B (zh) 新型杂原子芳香族酰胺衍生物以及含有其的药剂
HK40076948B (zh) Kras g12d抑制剂
HK40046970A (en) Novel heteroaromatic amide derivative and medicine containing same
HK1226719B (zh) 作为磷酸肌醇酯3-激酶抑制剂的异色烯衍生物

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
GR01 Patent grant
GR01 Patent grant