CN103261205A - 动点马达蛋白cenp-e小分子抑制剂syntelin及其应用 - Google Patents

动点马达蛋白cenp-e小分子抑制剂syntelin及其应用 Download PDF

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CN103261205A
CN103261205A CN2011800483798A CN201180048379A CN103261205A CN 103261205 A CN103261205 A CN 103261205A CN 2011800483798 A CN2011800483798 A CN 2011800483798A CN 201180048379 A CN201180048379 A CN 201180048379A CN 103261205 A CN103261205 A CN 103261205A
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CN103261205B (zh
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姚雪彪
丁霞
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    • 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
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

本发明公开了一种动点马达蛋白CENP-E小分子抑制剂Syntelin及其应用。本发明提供的与CENP-E马达驱动域结合的有机小分子化合物,它与CENP-E结合后可抑制CENP-E马达在微管上的行走,但不影响其与微管的相互作用,当该化合物加入细胞培养基中能够进入细胞抑制CENP-E的功能,导致部分染色体排列错误并长时间维系纺锤体检验点的活性。

Description

PCT国内申请,说明书已公开。

Claims (1)

  1. PCT国内申请,权利要求书已公开。
CN201180048379.8A 2010-11-12 2011-11-11 动点马达蛋白cenp-e小分子抑制剂syntelin及其应用 Active CN103261205B (zh)

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CN201180048379.8A CN103261205B (zh) 2010-11-12 2011-11-11 动点马达蛋白cenp-e小分子抑制剂syntelin及其应用

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CN201010544018.X 2010-11-12
CN201010544018 2010-11-12
CN201010544018X 2010-11-12
PCT/CN2011/001897 WO2012062044A1 (zh) 2010-11-12 2011-11-11 动点马达蛋白cenp-e小分子抑制剂syntelin及其应用
CN201180048379.8A CN103261205B (zh) 2010-11-12 2011-11-11 动点马达蛋白cenp-e小分子抑制剂syntelin及其应用

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CN201110356727.XA Active CN102532159B (zh) 2010-11-12 2011-11-11 动点马达蛋白CENP-E小分子抑制剂Syntelin
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CN201110356727.XA Active CN102532159B (zh) 2010-11-12 2011-11-11 动点马达蛋白CENP-E小分子抑制剂Syntelin

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AU2011281015B2 (en) 2010-07-23 2015-09-24 President And Fellows Of Harvard College Tricyclic proteasome activity enhancing compounds
CA2861464C (en) 2012-01-25 2018-03-06 Proteostasis Therapeutics, Inc. Proteasome activity modulating tricyclic compounds

Citations (4)

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CN1192142A (zh) * 1995-08-03 1998-09-02 普罗克特和甘保尔公司 1h-1,2,4-三唑衍生物用于抑制癌症生长的用途
WO2001007436A2 (en) * 1999-07-28 2001-02-01 Aventis Pharmaceuticals Inc. Substituted oxoazaheterocyclyl compounds
CN1291892A (zh) * 1998-01-27 2001-04-18 阿温蒂斯药物制品公司 取代的氧代氮杂杂环基因子Xa抑制剂
CN101100472A (zh) * 2001-04-30 2008-01-09 美国拜尔公司 4-氨基-5,6-取代的噻吩并[2,3-d]嘧啶化合物及其应用

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Publication number Priority date Publication date Assignee Title
US6710017B2 (en) * 2000-02-07 2004-03-23 Avecia, Inc. Compositions and methods for controlling algae in recirculating water systems
US7462614B2 (en) * 2003-04-01 2008-12-09 Smithkline Beecham Corporation Imidazotriazine compounds
CN100391451C (zh) * 2005-04-08 2008-06-04 中山大学 斑蝥素衍生物在制备抗肿瘤药物中的应用
JP2011507910A (ja) * 2007-12-21 2011-03-10 ユニバーシティー オブ ロチェスター 真核生物の寿命を変更するための方法

Patent Citations (4)

* Cited by examiner, † Cited by third party
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CN1192142A (zh) * 1995-08-03 1998-09-02 普罗克特和甘保尔公司 1h-1,2,4-三唑衍生物用于抑制癌症生长的用途
CN1291892A (zh) * 1998-01-27 2001-04-18 阿温蒂斯药物制品公司 取代的氧代氮杂杂环基因子Xa抑制剂
WO2001007436A2 (en) * 1999-07-28 2001-02-01 Aventis Pharmaceuticals Inc. Substituted oxoazaheterocyclyl compounds
CN101100472A (zh) * 2001-04-30 2008-01-09 美国拜尔公司 4-氨基-5,6-取代的噻吩并[2,3-d]嘧啶化合物及其应用

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
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CHAMANLAL J. SHISHOO,等: "Design, synthesis and antihistaminic(H1) activity of some condensed 3-aminopyrimidin-4(3H)-ones", 《EUR. J. MED. CHEM.》 *

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Publication number Publication date
WO2012062044A1 (zh) 2012-05-18
CN102552274B (zh) 2013-10-23
CN103261205B (zh) 2015-08-19
CN102552274A (zh) 2012-07-11
CN102532159A (zh) 2012-07-04
CN102532159B (zh) 2015-02-11

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