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
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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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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • 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
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal 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)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (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

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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)

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US10350216B2 (en) 2013-01-14 2019-07-16 The Trustees Of Columbia University In The City Of New York Methods of treating, preventing and diagnosing leukemia and other blood diseases and disorders
EP3024456A4 (en) 2013-07-26 2017-04-12 Update Pharma Inc. 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
EP3414239A2 (en) 2016-02-05 2018-12-19 Denali Therapeutics Inc. Inhibitors of receptor-interacting protein kinase 1
MY199967A (en) 2016-03-15 2023-11-30 Oryzon Genomics Sa Combinations of lsd1 inhibitors for use in the treatment of solid tumors
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
KR102418765B1 (ko) * 2016-04-12 2022-07-08 일라이 릴리 앤드 캄파니 암 치료를 위한 Notch 및 CDK4/6 억제제의 조합 요법
KR102463617B1 (ko) 2016-05-20 2022-11-03 일라이 릴리 앤드 캄파니 Notch 및 PD-1 또는 PD-L1 억제제를 이용한 조합 요법
CN116473978A (zh) * 2016-08-31 2023-07-25 伊莱利利公司 用于治疗实体瘤的给药方案
EP3525796A1 (en) 2016-10-12 2019-08-21 Eli Lilly and Company Targeted treatment of mature t-cell lymphoma
SI3552017T1 (sl) 2016-12-09 2022-09-30 Denali Therapeutics Inc. Spojine uporabne kot zaviralci RIPK1
KR20190116420A (ko) 2017-02-17 2019-10-14 프레드 헛친슨 켄서 리서치 센터 Bcma 관련 암 및 자가면역 장애의 치료를 위한 조합 요법
TW201932482A (zh) 2017-11-01 2019-08-16 美商奇諾治療有限公司 對b細胞成熟抗原具特異性之嵌合抗原受體及編碼聚核苷酸
CN111886012A (zh) 2017-11-06 2020-11-03 朱诺治疗学股份有限公司 细胞疗法与γ分泌酶抑制剂的组合
BR112020022654A2 (pt) * 2018-05-06 2021-03-09 Ayala Pharmaceuticals Inc. Composições de combinação que compreendem compostos de bisfluoroalquil-1,4-benzodiazepinona e métodos de uso das mesmas
MX2021003773A (es) 2018-10-02 2021-07-16 Frequency Therapeutics Inc Composiciones farmacéuticas y métodos relacionados con los agentes terapéuticos óticos.
CN114340611A (zh) 2019-04-08 2022-04-12 频率医疗公司 用于治疗听力损失的chir99021和丙戊酸的组合
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)

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JP2002518481A (ja) 1998-06-22 2002-06-25 エラン ファーマシューティカルズ,インコーポレイテッド β−アミロイドペプチドの放出および/またはその合成を阻害するための化合物
CA2325389A1 (en) * 1998-06-22 1999-12-29 James E. Audia Compounds for inhibiting beta-amyloid peptide release and/or its synthesis
JP4662914B2 (ja) 2003-02-04 2011-03-30 エフ.ホフマン−ラ ロシュ アーゲー ガンマ−セクレターゼ阻害剤としてのマロンアミド誘導体
NZ545538A (en) 2003-09-09 2008-12-24 Hoffmann La Roche Malonamide derivatives blocking the activity of gama-secretase
US7166587B2 (en) 2003-10-06 2007-01-23 Hoffmann-La Roche Inc. Carbamic acid alkyl ester derivatives
CN101410378B (zh) 2006-03-27 2012-12-05 霍夫曼-拉罗奇有限公司 作为γ分泌酶抑制剂的丙二酰胺衍生物
CN101622232A (zh) * 2007-02-02 2010-01-06 弗·哈夫曼-拉罗切有限公司 6-氧代-6,7-二氢-5h-二苯并[b,d]氮杂䓬-7-基衍生物
RU2010133489A (ru) 2008-01-11 2012-02-20 Ф.Хоффманн-Ля Рош Аг (Ch) Применение ингибиторов гамма-секретазы для лечения рака

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

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