CN104245699B - Nedd8‑活化酶抑制剂和低甲基化剂的投与 - Google Patents

Nedd8‑活化酶抑制剂和低甲基化剂的投与 Download PDF

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Publication number
CN104245699B
CN104245699B CN201280062112.9A CN201280062112A CN104245699B CN 104245699 B CN104245699 B CN 104245699B CN 201280062112 A CN201280062112 A CN 201280062112A CN 104245699 B CN104245699 B CN 104245699B
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acceptable salt
pharmaceutically acceptable
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azacitidine
administration
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CN104245699A (zh
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彼得·G·史密斯
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Takeda Pharmaceutical Co Ltd
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Millennium Pharmaceuticals Inc
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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
    • 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
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201280062112.9A 2011-11-03 2012-11-02 Nedd8‑活化酶抑制剂和低甲基化剂的投与 Active CN104245699B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161555049P 2011-11-03 2011-11-03
US61/555,049 2011-11-03
PCT/US2012/063382 WO2013067396A2 (en) 2011-11-03 2012-11-02 Administration of nedd8-activating enzyme inhibitor and hypomethylating agent

Publications (2)

Publication Number Publication Date
CN104245699A CN104245699A (zh) 2014-12-24
CN104245699B true CN104245699B (zh) 2017-06-27

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CN201280062112.9A Active CN104245699B (zh) 2011-11-03 2012-11-02 Nedd8‑活化酶抑制剂和低甲基化剂的投与

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Country Link
US (2) US8980850B2 (enExample)
EP (1) EP2773360B1 (enExample)
JP (2) JP6231988B2 (enExample)
KR (1) KR101987861B1 (enExample)
CN (1) CN104245699B (enExample)
AU (1) AU2012321106C1 (enExample)
BR (1) BR112014010699B1 (enExample)
CA (1) CA2854461C (enExample)
EA (1) EA028380B1 (enExample)
ES (1) ES2668272T3 (enExample)
GE (1) GEP20196940B (enExample)
HK (1) HK1201733A1 (enExample)
IL (1) IL232353B (enExample)
MA (1) MA35662B1 (enExample)
MX (1) MX357835B (enExample)
MY (1) MY176125A (enExample)
PH (1) PH12014501001B1 (enExample)
PL (1) PL2773360T3 (enExample)
SG (1) SG11201401895WA (enExample)
TN (1) TN2014000194A1 (enExample)
TR (1) TR201807342T4 (enExample)
UA (1) UA114414C2 (enExample)
WO (1) WO2013067396A2 (enExample)

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RU2562245C2 (ru) 2009-05-14 2015-09-10 Милленниум Фармасьютикалз, Инк. ГИДРОХЛОРИД (1S,2S,4R)-4-{ 4-[(1S)-2,3-ДИГИДРО-1Н-ИНДЕН-1-ИЛАМИНО]-7Н-ПИРРОЛО [2,3-d]ПИРИМИДИН-7-ИЛ} -2-ГИДРОКСИЦИКЛОПЕНТИЛ)МЕТИЛ СУЛЬФАМАТА
HK1199252A1 (en) * 2011-08-24 2015-06-26 Millennium Pharmaceuticals, Inc. Inhibitors of nedd8-activating enzyme
EP2764866A1 (en) * 2013-02-07 2014-08-13 IP Gesellschaft für Management mbH Inhibitors of nedd8-activating enzyme
WO2014186388A2 (en) 2013-05-14 2014-11-20 Millennium Pharmaceutcals, Inc. Administration of nedd8-activating enzyme inhibitor and chemotherapeutic agents
WO2015011235A1 (en) * 2013-07-26 2015-01-29 Boehringer Ingelheim International Gmbh Volasertib in combination with azacitidine for the treatment of acute myeloid leukemia and myelodysplastic syndrome ii
SG11201608303QA (en) 2014-04-04 2016-11-29 Del Mar Pharmaceuticals Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer
CN103948590A (zh) * 2014-05-22 2014-07-30 中国药科大学 Nedd8激活酶抑制剂及其医药用途
EP3362070B1 (en) * 2015-10-15 2021-01-27 Celgene Corporation Combination of a mutant isocitrate dehydrogenase 2 inhibitor with azacitidine and its use for treating acute myelogenous leukemia
WO2018218119A1 (en) * 2017-05-25 2018-11-29 The Board Of Trustees Of The Leland Stanford Junior University Combination of low dose il-2 and an inhibitor of treg il-2r desensitization to treat autoimmune and allergic inflammatory diseases
JP2020534331A (ja) * 2017-09-21 2020-11-26 ミレニアム ファーマシューティカルズ, インコーポレイテッドMillennium Pharmaceuticals, Inc. ((1s,2s,4r)−4−{4−[(1s)−2,3−ジヒドロ−1h−インデン−1−イルアミノ]−7h−ピロロ[2,3−d]ピリミジン−7−イル}−2−ヒドロキシシクロペンチル)メチルスルファメートの共結晶形態、その製剤及び使用
US20220017908A1 (en) * 2018-11-20 2022-01-20 Fulcrum Therapeutics, Inc. Compositions and methods for increasing fetal hemoglobin and treating sickle cell disease
EP3938050A1 (en) 2019-03-15 2022-01-19 Fulcrum Therapeutics, Inc. Macrocyclic azolopyridine derivatives as eed and prc2 modulators
WO2023025668A1 (en) 2021-08-25 2023-03-02 Asociación Centro De Investigación Cooperativa En Biociencias-Cic Biogune Methods for the generation of stem cell memory t cells for adoptive t cell therapy
WO2023242235A1 (en) * 2022-06-14 2023-12-21 Scandion Oncology A/S Abcg2 inhibitor and nae inhibitor for the treatment of cancer
CN115007323B (zh) * 2022-06-17 2024-01-23 中南大学 一种抑制矿物中黄铁矿浮选的方法
EP4554608A1 (en) * 2022-07-11 2025-05-21 Westlake University Use of a fbxo42 specific inhibitor in treating notch signaling-dependent disease

Citations (3)

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CN101516850A (zh) * 2006-08-08 2009-08-26 米伦纽姆医药公司 适用作e1活化酶抑制剂的杂芳基化合物
US20100292177A1 (en) * 2009-03-23 2010-11-18 Armstrong Robert C Methods of treatment using combination therapy
CN102088969A (zh) * 2008-06-09 2011-06-08 西克拉塞尔有限公司 沙帕他滨或cndac与dna甲基转移酶抑制剂如地西他滨和普鲁卡因的组合

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US6887855B2 (en) 2003-03-17 2005-05-03 Pharmion Corporation Forms of 5-azacytidine
US6943249B2 (en) 2003-03-17 2005-09-13 Ash Stevens, Inc. Methods for isolating crystalline Form I of 5-azacytidine
US20060063735A1 (en) 2004-09-17 2006-03-23 Supergen, Inc. Salts of 5-azacytidine
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WO2006084281A1 (en) 2005-02-04 2006-08-10 Millennium Pharmaceuticals, Inc. Inhibitors of e1 activating enzymes
JP5231251B2 (ja) 2006-02-02 2013-07-10 ミレニアム ファーマシューティカルズ, インコーポレイテッド E1活性化酵素の阻害剤
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SI2695609T1 (sl) 2008-05-15 2020-03-31 Celgene Corporation Oral formulacije anologov citidina in postopki za njihovo uporabo
RU2562245C2 (ru) 2009-05-14 2015-09-10 Милленниум Фармасьютикалз, Инк. ГИДРОХЛОРИД (1S,2S,4R)-4-{ 4-[(1S)-2,3-ДИГИДРО-1Н-ИНДЕН-1-ИЛАМИНО]-7Н-ПИРРОЛО [2,3-d]ПИРИМИДИН-7-ИЛ} -2-ГИДРОКСИЦИКЛОПЕНТИЛ)МЕТИЛ СУЛЬФАМАТА
EP2670396A1 (en) 2011-01-31 2013-12-11 Celgene Corporation Pharmaceutical compositions of cytidine analogs and methods of use thereof
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CN101516850A (zh) * 2006-08-08 2009-08-26 米伦纽姆医药公司 适用作e1活化酶抑制剂的杂芳基化合物
CN102088969A (zh) * 2008-06-09 2011-06-08 西克拉塞尔有限公司 沙帕他滨或cndac与dna甲基转移酶抑制剂如地西他滨和普鲁卡因的组合
US20100292177A1 (en) * 2009-03-23 2010-11-18 Armstrong Robert C Methods of treatment using combination therapy

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"Substrate-Assisted Inhibition of Ubiquitin-like Protein-Activating Enzymes: The NEDD8 E1 Inhibitor MLN4924 Forms a NEDD8-AMP Mimetic In Situ";James E. Brownell et al.;《Molecular Cell》;20100115;第37卷;第102-111页 *
"Targeting protein neddylation: a novel therapeutic strategy for the treatment of cancer";Meng Wang et al.;《Expert Opin. Ther. Targets》;20110331;第15卷(第3期);第253-264页 *

Also Published As

Publication number Publication date
CN104245699A (zh) 2014-12-24
JP6231988B2 (ja) 2017-11-15
PL2773360T3 (pl) 2018-09-28
AU2012321106C1 (en) 2016-11-24
KR20140097229A (ko) 2014-08-06
BR112014010699B1 (pt) 2020-12-15
ES2668272T3 (es) 2018-05-17
TR201807342T4 (tr) 2018-06-21
IL232353A0 (en) 2014-06-30
MY176125A (en) 2020-07-24
MA35662B1 (fr) 2014-11-01
WO2013067396A2 (en) 2013-05-10
US20130116208A1 (en) 2013-05-09
AU2012321106B2 (en) 2016-08-04
UA114414C2 (uk) 2017-06-12
EA028380B1 (ru) 2017-11-30
IL232353B (en) 2018-11-29
EA201400539A1 (ru) 2014-12-30
EP2773360B1 (en) 2018-02-28
PH12014501001A1 (en) 2014-06-09
CA2854461A1 (en) 2013-05-10
TN2014000194A1 (en) 2015-09-30
JP2015505816A (ja) 2015-02-26
MX2014005323A (es) 2014-06-05
AU2012321106A1 (en) 2013-05-23
EP2773360A4 (en) 2015-09-23
US8980850B2 (en) 2015-03-17
GEP20196940B (en) 2019-01-10
SG11201401895WA (en) 2014-05-29
PH12014501001B1 (en) 2018-05-04
CA2854461C (en) 2021-01-19
MX357835B (es) 2018-07-26
HK1201733A1 (en) 2015-09-11
EP2773360A2 (en) 2014-09-10
BR112014010699A2 (pt) 2017-04-25
US20150366886A1 (en) 2015-12-24
NZ624881A (en) 2016-10-28
KR101987861B1 (ko) 2019-06-11
JP2018009035A (ja) 2018-01-18
WO2013067396A3 (en) 2014-10-16

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Effective date of registration: 20211025

Address after: Osaka, Japan

Patentee after: TAKEDA PHARMACEUTICAL Co.,Ltd.

Address before: Massachusetts, USA

Patentee before: MILLENNIUM PHARMACEUTICALS, Inc.