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
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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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Publication of TWI568730B publication Critical patent/TWI568730B/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)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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)
  • 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 (https=)
EP (1) EP2736920B1 (https=)
JP (1) JP6027110B2 (https=)
KR (1) KR101578309B1 (https=)
CN (1) CN103732612B (https=)
AP (1) AP4080A (https=)
AR (1) AR087107A1 (https=)
AU (1) AU2012287251B2 (https=)
BR (1) BR112014001600B1 (https=)
CA (1) CA2841178C (https=)
CL (1) CL2014000175A1 (https=)
CO (1) CO6862159A2 (https=)
CR (1) CR20140036A (https=)
CY (1) CY1116645T1 (https=)
DK (1) DK2736920T3 (https=)
DO (1) DOP2014000011A (https=)
EA (1) EA023044B1 (https=)
EC (1) ECSP14013179A (https=)
ES (1) ES2544937T3 (https=)
GT (1) GT201400012A (https=)
HR (1) HRP20150771T1 (https=)
HU (1) HUE027534T2 (https=)
IL (1) IL229988A (https=)
JO (1) JO3148B1 (https=)
MA (1) MA35611B1 (https=)
ME (1) ME02171B (https=)
MX (1) MX356536B (https=)
MY (1) MY184303A (https=)
PE (1) PE20141061A1 (https=)
PH (1) PH12014500215B1 (https=)
PL (1) PL2736920T3 (https=)
PT (1) PT2736920E (https=)
RS (1) RS54135B1 (https=)
SI (1) SI2736920T1 (https=)
TW (1) TWI568730B (https=)
WO (1) WO2013016081A1 (https=)

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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
CN112472699A (zh) 2013-07-26 2021-03-12 种族肿瘤学公司 改善比生群及衍生物的治疗益处的组合方法
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
IL287136B2 (en) 2016-02-05 2023-09-01 Denali Therapeutics Inc Receptor inhibitors - interacting with protein kinase 1
ES3057783T3 (en) 2016-03-15 2026-03-04 Oryzon Genomics Sa Combinations of lsd1 inhibitors for use in the treatment of neoplastic diseases
EP3442528B1 (en) * 2016-04-12 2021-05-26 Eli Lilly and Company Combination therapy with notch and pi3k/mtor inhibitors for use in treating ovarian cancer
JP6911047B2 (ja) * 2016-04-12 2021-07-28 イーライ リリー アンド カンパニー がんの処置のための、Notch阻害剤およびCDK4/6阻害剤の併用療法
JP7194022B2 (ja) 2016-05-20 2022-12-21 イーライ リリー アンド カンパニー Notch阻害剤とPD-1またはPD-L1阻害剤との併用療法
SG11201901325UA (en) * 2016-08-31 2019-03-28 Lilly Co Eli Dosage regimen for treatment of solid tumors
EP3525796A1 (en) 2016-10-12 2019-08-21 Eli Lilly and Company Targeted treatment of mature t-cell lymphoma
JP7208137B2 (ja) 2016-12-09 2023-01-18 デナリ セラピューティクス インコーポレイテッド 化合物、組成物および方法
MX2019009552A (es) 2017-02-17 2019-10-02 Hutchinson Fred Cancer Res Terapias de combinacion para el tratamiento de canceres relacionados con el antigeno de maduracion de celulas b (bcma) y trastornos autoinmunitarios.
PT3703750T (pt) 2017-11-01 2025-01-17 Memorial Sloan Kettering Cancer Center Recetores de antigénio quimérico específicos para o antigénio de maturação das células b e polinucleótidos codificantes
MX2020004568A (es) * 2017-11-06 2020-10-05 Juno Therapeutics Inc Combinación de una terapia celular y un inhibidor de gamma secretasa.
KR20210005714A (ko) * 2018-05-06 2021-01-14 아얄라 파마큐티컬즈 아이엔씨. 비스플루오로알킬-1,4-벤조디아제피논 화합물을 포함하는 조합 조성물 및 이의 사용 방법
CA3114113A1 (en) 2018-10-02 2020-04-09 Frequency Therapeutics, Inc. Pharmaceutical compositions and methods related to otic therapeutic agents
US20220175776A1 (en) 2019-04-08 2022-06-09 Frequency Therapeutics, Inc. Combination of chir99021 and valproic acid for treating hearing loss
TW202334164A (zh) 2022-01-12 2023-09-01 美商戴納立製藥公司 (S)-5-苄基-N-(5-甲基-4-側氧基-2,3,4,5-四氫吡啶並[3,2-b][1,4]氧氮呯-3-基)-4H-1,2,4-三唑-3-甲醯胺的晶型

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
WO1999067221A1 (en) * 1998-06-22 1999-12-29 Elan Pharmaceuticals, Inc. Compounds for inhibiting beta-amyloid peptide release and/or its synthesis
EP1592684B1 (en) 2003-02-04 2008-07-30 F. Hoffmann-La Roche Ag Malonamide derivatives as gamma-secretase inhibitors
KR100838852B1 (ko) 2003-09-09 2008-06-16 에프. 호프만-라 로슈 아게 감마-세크리테이즈의 활성을 차단하는 말론아미드 유도체
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
ES2398531T3 (es) 2006-03-27 2013-03-20 F. Hoffmann-La Roche Ag Derivados de malonamida como inhibidores de gamma secretasa
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
MA33076B1 (fr) 2008-01-11 2012-03-01 Hoffmann La Roche Utilisation d'un inhibiteur de la gamma-secretase pour le traitement du cancer

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

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