JP6262246B2 - ベンダムスチン誘導体およびこれを使用する方法 - Google Patents

ベンダムスチン誘導体およびこれを使用する方法 Download PDF

Info

Publication number
JP6262246B2
JP6262246B2 JP2015541995A JP2015541995A JP6262246B2 JP 6262246 B2 JP6262246 B2 JP 6262246B2 JP 2015541995 A JP2015541995 A JP 2015541995A JP 2015541995 A JP2015541995 A JP 2015541995A JP 6262246 B2 JP6262246 B2 JP 6262246B2
Authority
JP
Japan
Prior art keywords
bendamustine
mmol
ester
solid
alkyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
JP2015541995A
Other languages
English (en)
Japanese (ja)
Other versions
JP2015536996A5 (cg-RX-API-DMAC10.html
JP2015536996A (ja
Inventor
バカレ、ロジャー、ピー．
ブラウン、ピーター、ディー．
チェン、ジアン
ドレーガー、アンソニー、エス．
レーベル、レイチェル、ワイ．
マッキーン、ロバート、イー．
パテル、ピユシュ、アール．
ローメリー、レネイ、シー．
Original Assignee
イグニタ、インク．
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by イグニタ、インク． filed Critical イグニタ、インク．
Publication of JP2015536996A publication Critical patent/JP2015536996A/ja
Publication of JP2015536996A5 publication Critical patent/JP2015536996A5/ja
Application granted granted Critical
Publication of JP6262246B2 publication Critical patent/JP6262246B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/42—Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/16—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Inorganic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2015541995A 2012-11-12 2013-11-12 ベンダムスチン誘導体およびこれを使用する方法 Expired - Fee Related JP6262246B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261725213P 2012-11-12 2012-11-12
US61/725,213 2012-11-12
US201361776951P 2013-03-12 2013-03-12
US61/776,951 2013-03-12
PCT/US2013/069550 WO2014075035A1 (en) 2012-11-12 2013-11-12 Bendamustine derivatives and methods of using same

Publications (3)

Publication Number Publication Date
JP2015536996A JP2015536996A (ja) 2015-12-24
JP2015536996A5 JP2015536996A5 (cg-RX-API-DMAC10.html) 2016-12-28
JP6262246B2 true JP6262246B2 (ja) 2018-01-17

Family

ID=49667594

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2015541995A Expired - Fee Related JP6262246B2 (ja) 2012-11-12 2013-11-12 ベンダムスチン誘導体およびこれを使用する方法

Country Status (17)

Country Link
US (7) US9452988B2 (cg-RX-API-DMAC10.html)
EP (1) EP2917183A1 (cg-RX-API-DMAC10.html)
JP (1) JP6262246B2 (cg-RX-API-DMAC10.html)
KR (1) KR20150086308A (cg-RX-API-DMAC10.html)
AR (1) AR093457A1 (cg-RX-API-DMAC10.html)
AU (1) AU2013342015B2 (cg-RX-API-DMAC10.html)
BR (1) BR112015010501A2 (cg-RX-API-DMAC10.html)
CA (1) CA2890462A1 (cg-RX-API-DMAC10.html)
CL (1) CL2015001246A1 (cg-RX-API-DMAC10.html)
EA (1) EA029706B1 (cg-RX-API-DMAC10.html)
HK (2) HK1215701A1 (cg-RX-API-DMAC10.html)
IL (1) IL238662A (cg-RX-API-DMAC10.html)
MX (1) MX2015005805A (cg-RX-API-DMAC10.html)
PH (1) PH12015501024A1 (cg-RX-API-DMAC10.html)
SG (1) SG11201503560TA (cg-RX-API-DMAC10.html)
TW (1) TWI598341B (cg-RX-API-DMAC10.html)
WO (1) WO2014075035A1 (cg-RX-API-DMAC10.html)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR122019024201B1 (pt) 2010-05-20 2021-08-03 Array Biopharma Inc Composto macrocíclico como inibidores de trk quinase, seu uso, e composição farmacêutica
EP2917183A1 (en) * 2012-11-12 2015-09-16 Ignyta, Inc. Bendamustine derivatives and methods of using same
CA2904143A1 (en) 2013-03-12 2014-10-09 Cephalon, Inc. Nanoparticulate and macroparticulate formulations
CA2992586A1 (en) 2015-07-16 2017-01-19 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
EP3484519A1 (en) * 2016-07-13 2019-05-22 Cephalon, Inc. Pharmaceutical prodrugs and methods of their preparation and use
TWI752098B (zh) 2016-10-10 2022-01-11 美商亞雷生物製藥股份有限公司 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
JP6888101B2 (ja) 2017-01-18 2021-06-16 アレイ バイオファーマ インコーポレイテッド ＲＥＴキナーゼ阻害剤としての置換ピラゾロ［１，５−ａ］ピラジン化合物
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
TWI876442B (zh) 2017-10-10 2025-03-11 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
EP3740491A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
EP3740486A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
CN111630054B (zh) 2018-01-18 2023-05-09 奥瑞生物药品公司 作为RET激酶抑制剂的取代的吡唑并[3,4-d]嘧啶化合物
CA3108065C (en) 2018-07-31 2025-10-07 Loxo Oncology, Inc. SPRAY-DRIED DISPERSIONS, FORMULATIONS AND POLYMORPHIES OF (S)-5-AMINO-3-(4-((5-FLUORO-2-METHOXYBENZAMIDO)METHYL)PHENYL)(1,1,1-TRIFLUOROPROPANE-2-YL)-1H-PYRAZOLE-4-CARBOXAMIDE
ES2922314T3 (es) 2018-09-10 2022-09-13 Array Biopharma Inc Compuestos heterocíclicos condensados como inhibidores de cinasa RET

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5681964A (en) * 1990-10-23 1997-10-28 University Of Kentucky Research Foundation Permeable, non-irritating prodrugs of nonsteroidal and steroidal agents
US5834025A (en) 1995-09-29 1998-11-10 Nanosystems L.L.C. Reduction of intravenously administered nanoparticulate-formulation-induced adverse physiological reactions
US7089218B1 (en) 2004-01-06 2006-08-08 Neuric Technologies, Llc Method for inclusion of psychological temperament in an electronic emulation of the human brain
US8853260B2 (en) 1997-06-27 2014-10-07 Abraxis Bioscience, Llc Formulations of pharmacological agents, methods for the preparation thereof and methods for the use thereof
CA2428018A1 (en) * 2000-12-01 2002-06-06 Enzon, Inc. Tetrapartate prodrugs
WO2003086369A2 (en) * 2002-04-05 2003-10-23 Valorisation-Recherche, Societe En Commandite Stealthy polymeric biodegradable nanospheres and uses thereof
DK1585548T3 (en) 2002-12-09 2018-09-03 Abraxis Bioscience Llc COMPOSITIONS AND PROCEDURES FOR THE DELIVERY OF PHARMACOLOGICAL AGENTS
US8436190B2 (en) 2005-01-14 2013-05-07 Cephalon, Inc. Bendamustine pharmaceutical compositions
CN103169729A (zh) 2005-02-18 2013-06-26 阿布拉科斯生物科学有限公司 治疗剂的组合和给予方式以及联合治疗
DE102005062440B4 (de) * 2005-12-27 2011-02-24 Lts Lohmann Therapie-Systeme Ag Proteinbasiertes Trägersystem zur Resistenzüberwindung von Tumorzellen
CN101878024B (zh) 2007-11-28 2014-04-09 塞拉特药物股份有限公司 改良的紫杉烷递送系统
AR072777A1 (es) 2008-03-26 2010-09-22 Cephalon Inc Formas solidas de clorhidrato de bendamustina
CN104224703A (zh) * 2008-09-25 2014-12-24 赛福伦公司 苯达莫司汀的液体配制品
US9149441B2 (en) * 2008-09-29 2015-10-06 The Corporation Of Mercer University Nanospheres encapsulating bioactive material and method for formulation of nanospheres
MX2011003751A (es) * 2008-10-08 2011-04-27 Cephalon Inc Procesos para preparar bendamustina.
NZ592970A (en) * 2008-12-03 2013-05-31 Astellas Deutschland Gmbh Oral dosage forms of bendamustine
AU2011260615B2 (en) 2010-06-02 2016-11-17 Pharma& Schweiz Gmbh Oral dosage forms of bendamustine
TWI455722B (zh) 2010-06-04 2014-10-11 Pfizer Vaccines Llc 用於預防或治療菸鹼成癮之共軛體
CN101966158A (zh) 2010-09-28 2011-02-09 上海丽思化工科技有限公司 一种注射用盐酸苯达莫司汀冻干粉针剂及其制备方法
US20130217888A1 (en) 2010-11-01 2013-08-22 Shailpa Medicare Limited Process for preparing bendamus tine hydrochloride monohydrate
DE102010055499A1 (de) * 2010-12-22 2011-06-16 W.C. Heraeus Gmbh Prozess zur Herstellung von Bendamustinalkylester, Bendarmustin sowie Derivaten davon
HUE048876T2 (hu) 2011-05-09 2020-08-28 Mayo Found Medical Education & Res Rákos megbetegedések kezelése
US9308276B2 (en) 2011-05-17 2016-04-12 University Of South Alabama Combination therapy for treatment of cancer
ES2613838T3 (es) 2011-09-26 2017-05-26 Fresenius Kabi Oncology Ltd Un procedimiento mejorado para la preparación de hidrocloruro de bendamustina
PT2656843E (pt) 2012-04-26 2015-04-14 Helmut Schickaneder Ésteres de bendamustina e compostos relacionados e a sua utilização médica
UA117809C2 (uk) 2012-06-19 2018-10-10 Хельмут Шикканедер Похідні бендамустину, споріднені сполуки та їхнє медичне застосування для лікування раку
US9314532B2 (en) 2012-08-10 2016-04-19 University Of North Texas Health Science Center Drug delivery vehicle
EP2917183A1 (en) * 2012-11-12 2015-09-16 Ignyta, Inc. Bendamustine derivatives and methods of using same

Also Published As

Publication number Publication date
US9913827B2 (en) 2018-03-13
KR20150086308A (ko) 2015-07-27
HK1215701A1 (zh) 2016-09-09
CN105051016A (zh) 2015-11-11
BR112015010501A2 (pt) 2017-07-11
TWI598341B (zh) 2017-09-11
EA201590925A1 (ru) 2015-09-30
US9149464B2 (en) 2015-10-06
CA2890462A1 (en) 2014-05-15
EP2917183A1 (en) 2015-09-16
US9630926B2 (en) 2017-04-25
AU2013342015A1 (en) 2015-05-28
US20160289198A1 (en) 2016-10-06
US20150232427A1 (en) 2015-08-20
WO2014075035A1 (en) 2014-05-15
US20160016912A1 (en) 2016-01-21
EA029706B1 (ru) 2018-05-31
JP2015536996A (ja) 2015-12-24
SG11201503560TA (en) 2015-06-29
AU2013342015B2 (en) 2016-11-24
US20180147186A1 (en) 2018-05-31
IL238662A (en) 2017-08-31
PH12015501024A1 (en) 2015-07-27
CL2015001246A1 (es) 2016-01-15
HK1212977A1 (zh) 2016-06-24
IL238662A0 (en) 2015-06-30
US9150517B2 (en) 2015-10-06
TW201439069A (zh) 2014-10-16
US9452988B2 (en) 2016-09-27
US20150274675A1 (en) 2015-10-01
AR093457A1 (es) 2015-06-10
US20150246023A1 (en) 2015-09-03
MX2015005805A (es) 2016-04-15
US20170182008A1 (en) 2017-06-29

Similar Documents

Publication Publication Date Title
JP2015536996A (ja) ベンダムスチン誘導体およびこれを使用する方法
Duhem et al. Self-assembling doxorubicin–tocopherol succinate prodrug as a new drug delivery system: Synthesis, characterization, and in vitro and in vivo anticancer activity
JP6466283B2 (ja) 安定なミセルのためのブロックコポリマー
US20110040113A1 (en) Pure PEG-lipid conjugates
JP2016511222A (ja) ポルフィリン修飾されたテロデンドリマー
AU2006202613A1 (en) Taxane Prodrugs
JP2003525282A (ja) 診断および治療用の新規キノリン配位子および金属錯体
WO2012103328A1 (en) Labeled, non- peptidic multivalent integrin alpha -v - beta - 3 antagonists, compositions containing them and their use
US12527880B2 (en) Cyanine-based telodendrimers and uses for treating cancer
RU2721949C2 (ru) Модифицированные цитотоксины и их терапевтическое применение
CN111344018A (zh) 聚乙二醇化卡非佐米化合物的稳定的组合物
US20130203647A1 (en) Delivery of hydrophilic peptides
WO2011139343A2 (en) Amino acid linked peg-lipid conjugates
Zhang et al. Cholic acid-modified dendritic multimolecular micelles and enhancement of anticancer drug therapeutic efficacy
CN105051016B (zh) 苯达莫司汀衍生物及其使用方法
WO2023222659A1 (en) Trehalose-based surfactants
US20160143914A1 (en) Nanoparticles for Encapsulation and Delivery of Bioactive Compounds and Compositions Thereof
Sun A Sequential Stimulus-Responsive Nanoparticle Platform for Enhanced Tumor Growth Inhibition and Efficient Drug Delivery
Xu et al. A small molecular “albumin hitchhiking” deferoxamine conjugate improved iron clearance efficacy
JP6235460B2 (ja) 可逆的に架橋されたミセルｓｙｓｔｅｍｓ
JP6235460B6 (ja) 可逆的に架橋されたミセルｓｙｓｔｅｍｓ

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20161111

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20161111

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20170817

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20170822

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20171113

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20171128

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20171213

R150 Certificate of patent or registration of utility model

Ref document number: 6262246

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

LAPS Cancellation because of no payment of annual fees