TWI568730B - 刻痕(notch)路徑信號抑制劑化合物 - Google Patents

刻痕(notch)路徑信號抑制劑化合物 Download PDF

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Publication number
TWI568730B
TWI568730B TW101125459A TW101125459A TWI568730B TW I568730 B TWI568730 B TW I568730B TW 101125459 A TW101125459 A TW 101125459A TW 101125459 A TW101125459 A TW 101125459A TW I568730 B TWI568730 B TW I568730B
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TW
Taiwan
Prior art keywords
cancer
compound
leukemia
pharmaceutically acceptable
hydrate
Prior art date
Application number
TW101125459A
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English (en)
Chinese (zh)
Other versions
TW201315732A (zh
Inventor
菲利普 亞瑟 希普斯金
葛瑞格里 艾倫 史蒂芬生
Original Assignee
美國禮來大藥廠
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Publication of TW201315732A publication Critical patent/TW201315732A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • A61K38/00—Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
TW101125459A 2011-07-27 2012-07-13 刻痕(notch)路徑信號抑制劑化合物 TWI568730B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161512016P 2011-07-27 2011-07-27
US201161560486P 2011-11-16 2011-11-16

Publications (2)

Publication Number Publication Date
TW201315732A TW201315732A (zh) 2013-04-16
TWI568730B true TWI568730B (zh) 2017-02-01

Family

ID=46598983

Family Applications (1)

Application Number Title Priority Date Filing Date
TW101125459A TWI568730B (zh) 2011-07-27 2012-07-13 刻痕(notch)路徑信號抑制劑化合物

Country Status (36)

Country Link
US (1) US8569286B2 (enExample)
EP (1) EP2736920B1 (enExample)
JP (1) JP6027110B2 (enExample)
KR (1) KR101578309B1 (enExample)
CN (1) CN103732612B (enExample)
AP (1) AP4080A (enExample)
AR (1) AR087107A1 (enExample)
AU (1) AU2012287251B2 (enExample)
BR (1) BR112014001600B1 (enExample)
CA (1) CA2841178C (enExample)
CL (1) CL2014000175A1 (enExample)
CO (1) CO6862159A2 (enExample)
CR (1) CR20140036A (enExample)
CY (1) CY1116645T1 (enExample)
DK (1) DK2736920T3 (enExample)
DO (1) DOP2014000011A (enExample)
EA (1) EA023044B1 (enExample)
EC (1) ECSP14013179A (enExample)
ES (1) ES2544937T3 (enExample)
GT (1) GT201400012A (enExample)
HR (1) HRP20150771T1 (enExample)
HU (1) HUE027534T2 (enExample)
IL (1) IL229988A (enExample)
JO (1) JO3148B1 (enExample)
MA (1) MA35611B1 (enExample)
ME (1) ME02171B (enExample)
MX (1) MX356536B (enExample)
MY (1) MY184303A (enExample)
PE (1) PE20141061A1 (enExample)
PH (1) PH12014500215B1 (enExample)
PL (1) PL2736920T3 (enExample)
PT (1) PT2736920E (enExample)
RS (1) RS54135B1 (enExample)
SI (1) SI2736920T1 (enExample)
TW (1) TWI568730B (enExample)
WO (1) WO2013016081A1 (enExample)

Families Citing this family (20)

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Publication number Priority date Publication date Assignee Title
WO2014110506A2 (en) * 2013-01-14 2014-07-17 The Trustees Of Columbia University In The City Of New York Methods of treating, preventing and diagnosing leukemia and other blood diseases and disorders
AU2014293013A1 (en) 2013-07-26 2016-03-17 Race Oncology Ltd. Combinatorial methods to improve the therapeutic benefit of bisantrene
TWI704151B (zh) 2014-12-22 2020-09-11 美商美國禮來大藥廠 Erk抑制劑
TWI609687B (zh) * 2015-04-14 2018-01-01 美國禮來大藥廠 平滑肌肉瘤之標靶性治療
JO3491B1 (ar) * 2015-07-07 2020-07-05 Audion Therapeutics مركبات مثبطة لإشارات مسار notch
US9815850B2 (en) 2016-02-05 2017-11-14 Denali Therapeutics Inc. Compounds, compositions and methods
CN120661674A (zh) 2016-03-15 2025-09-19 奥莱松基因组股份有限公司 用于治疗实体瘤的lsd1抑制剂的组合
US11564929B2 (en) 2016-04-12 2023-01-31 Eli Lilly And Company Combination therapy with Notch and PI3K/mTOR inhibitors for use in treating cancer
MX380779B (es) * 2016-04-12 2025-03-12 Lilly Co Eli Terapia combinatoria con inhibidores notch y cdk4/6
EP3458091B1 (en) * 2016-05-20 2021-11-17 Eli Lilly and Company Combination therapy with notch and pd-1 or pd-l1 inhibitors
JP2019526632A (ja) * 2016-08-31 2019-09-19 イーライ リリー アンド カンパニー 固形腫瘍の治療のための投薬レジメン
EP3525796A1 (en) 2016-10-12 2019-08-21 Eli Lilly and Company Targeted treatment of mature t-cell lymphoma
LT3552017T (lt) 2016-12-09 2022-05-10 Denali Therapeutics Inc. Junginiai, naudotini kaip ripk1 inhibitoriai
IL268349B2 (en) 2017-02-17 2024-08-01 Hutchinson Fred Cancer Res Combination therapies for treatment of bcma-related cancers and autoimmune disorders
US11066475B2 (en) 2017-11-01 2021-07-20 Juno Therapeutics, Inc. Chimeric antigen receptors specific for B-cell maturation antigen and encoding polynucleotides
AU2018359907A1 (en) * 2017-11-06 2020-05-07 Fred Hutchinson Cancer Center Combination of a cell therapy and a gamma secretase inhibitor
EP3790552A4 (en) * 2018-05-06 2022-06-15 Ayala Pharmaceuticals Inc. COMBINATION COMPOSITIONS WITH BISFLUORAKYL-1,4-BENZODIAZEPINONE COMPOUNDS AND METHODS OF USE THERE
BR112021006092A2 (pt) 2018-10-02 2021-07-20 Frequency Therapeutics, Inc. composições farmacêuticas que compreendem agentes terapêuticos óticos e métodos relacionados
MX2021012258A (es) 2019-04-08 2022-01-04 Frequency Therapeutics Inc Combinacion de chir99021 y acido valproico para tratar la perdida auditiva.
EP4463229A1 (en) 2022-01-12 2024-11-20 Denali Therapeutics Inc. Crystalline forms of (s)-5-benzyl-n-(5-methyl-4-oxo-2, 3,4,5- tetrahydropyrido [3,2-b] [l,4]oxazepin-3-yl)-4h-l,2,4-triazole-3-carboxamide

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW568914B (en) * 1996-12-23 2004-01-01 Athena Neurosciences Inc Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
WO2011060051A1 (en) * 2009-11-12 2011-05-19 University Of Massachusetts Methods for treating glioblastoma

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU4710199A (en) * 1998-06-22 2000-01-10 Elan Pharmaceuticals, Inc. Compounds for inhibiting beta-amyloid peptide release and/or its synthesis
AU4707999A (en) 1998-06-22 2000-01-10 Elan Pharmaceuticals, Inc. Compounds for inhibiting beta-amyloid peptide release and/or its synthesis
CN100480248C (zh) 2003-02-04 2009-04-22 弗·哈夫曼-拉罗切有限公司 用作γ-分泌酶抑制剂的丙二酰胺衍生物
BRPI0413533A (pt) 2003-09-09 2006-10-10 Hoffmann La Roche derivados de malonamida que bloqueiam a atividade de gama-secretase
SI1673347T1 (sl) 2003-10-06 2015-10-30 F. Hoffmann - La Roche Ag Substituirani derivati dibenzo-azepina in benzo-diazepina, ki so uporabni kot inhibitorji gama-sekretaze
WO2007110335A1 (en) 2006-03-27 2007-10-04 F. Hoffmann-La Roche Ag Malonamide derivatives as gamma secretase inhibitors
KR101150574B1 (ko) * 2007-02-02 2012-05-30 에프. 호프만-라 로슈 아게 6-옥소-6,7-다이하이드로-5h-다이벤조[b,d]아제핀-7-일 유도체
US20090181944A1 (en) 2008-01-11 2009-07-16 John Frederick Boylan Method for cancer therapy

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW568914B (en) * 1996-12-23 2004-01-01 Athena Neurosciences Inc Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
WO2011060051A1 (en) * 2009-11-12 2011-05-19 University Of Massachusetts Methods for treating glioblastoma

Also Published As

Publication number Publication date
CN103732612A (zh) 2014-04-16
ES2544937T3 (es) 2015-09-07
PE20141061A1 (es) 2014-09-06
BR112014001600B1 (pt) 2022-09-13
HRP20150771T1 (hr) 2015-08-28
DOP2014000011A (es) 2014-07-31
US20130029972A1 (en) 2013-01-31
CA2841178C (en) 2016-12-20
DK2736920T3 (en) 2015-07-20
EP2736920B1 (en) 2015-07-01
ME02171B (me) 2015-10-20
EA201490161A1 (ru) 2014-04-30
PT2736920E (pt) 2015-09-16
US8569286B2 (en) 2013-10-29
HUE027534T2 (en) 2016-11-28
JO3148B1 (ar) 2017-09-20
JP6027110B2 (ja) 2016-11-16
BR112014001600A2 (pt) 2017-02-21
JP2014527042A (ja) 2014-10-09
CR20140036A (es) 2014-03-21
CO6862159A2 (es) 2014-02-10
KR20140026624A (ko) 2014-03-05
PL2736920T3 (pl) 2015-11-30
PH12014500215A1 (en) 2014-03-17
KR101578309B1 (ko) 2015-12-16
EP2736920A1 (en) 2014-06-04
CA2841178A1 (en) 2013-01-31
EA023044B1 (ru) 2016-04-29
AP2014007362A0 (en) 2014-01-31
TW201315732A (zh) 2013-04-16
AR087107A1 (es) 2014-02-12
SI2736920T1 (sl) 2015-08-31
AP4080A (en) 2017-03-29
AU2012287251A1 (en) 2014-01-30
WO2013016081A1 (en) 2013-01-31
PH12014500215B1 (en) 2018-09-07
MY184303A (en) 2021-03-31
NZ618891A (en) 2015-12-24
CL2014000175A1 (es) 2014-08-22
ECSP14013179A (es) 2014-03-31
GT201400012A (es) 2014-07-16
MX356536B (es) 2018-06-01
CN103732612B (zh) 2015-09-23
MA35611B1 (fr) 2014-11-01
IL229988A (en) 2017-07-31
HK1194086A1 (en) 2014-10-10
RS54135B1 (sr) 2015-12-31
CY1116645T1 (el) 2017-03-15
AU2012287251B2 (en) 2015-05-14
MX2014001084A (es) 2014-02-27

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