PE20100256A1 - Compuestos de ester boronato y composiciones farmaceuticas de los mismos - Google Patents

Compuestos de ester boronato y composiciones farmaceuticas de los mismos

Info

Publication number
PE20100256A1
PE20100256A1 PE2009000877A PE2009000877A PE20100256A1 PE 20100256 A1 PE20100256 A1 PE 20100256A1 PE 2009000877 A PE2009000877 A PE 2009000877A PE 2009000877 A PE2009000877 A PE 2009000877A PE 20100256 A1 PE20100256 A1 PE 20100256A1
Authority
PE
Peru
Prior art keywords
alkyl
acid
amino
pharmaceutical compositions
compounds
Prior art date
Application number
PE2009000877A
Other languages
English (en)
Inventor
Eric L Elliott
Abu J Ferdous
Michael J Kaufman
Sonja A Komar
Debra L Mazaik
Quentin J Mccubbin
Phoung M Nguyen
Vaithianathan Palaniappan
Raymond D Skwierczynski
Nobel T Truong
Csanad Varga
Peter N Zawaneh
Original Assignee
Millennium Pharm Inc
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41061278&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20100256(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Millennium Pharm Inc filed Critical Millennium Pharm Inc
Publication of PE20100256A1 publication Critical patent/PE20100256A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/04—Esters of boric acids
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/69—Boron compounds
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/183—Amino acids, e.g. glycine, EDTA or aspartame
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/81—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/82—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/83—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of an acyclic saturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
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    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
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    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/05—Cyclic compounds having at least one ring containing boron but no carbon in the ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C—CHEMISTRY; METALLURGY
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    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Immunology (AREA)
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  • Hematology (AREA)
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  • Hospice & Palliative Care (AREA)

Abstract

SE REFIERE A DERIVADOS DE ESTER BORONATO DE FORMULA (I), DONDE A ES 0-2; P ES H, O UN BLOQUEADOR DEL GRUPO AMINO; Ra Y Ra1 SON CADA UNO H, ALQUILO (C1-C6), FLUOROALQUILO (C1-C6), ENTRE OTROS; Ra2 ES H, ALQUILO (C1-C6), -(CH2)m-CH2-NHC(=NR4)NH-Y, ENTRE OTROS; R4 ES H, ALQUILO, ARILO, ENTRE OTROS; Y ES H, -CN O -NO; m ES 0-2; Z1 Y Z2 FORMAN JUNTOS UN RESTO QUE DERIVA DE UN ACIDO ALFAHIDROXI CARBOXILICO, DONDE EL ATOMO UNIDO A BORO ES O. SON COMPUESTOS PREFERIDOS: ACIDO-(R,S)-(CARBOXIMETIL)-2-((R)-1-(2-(2,5-DICLOROBENZAMIDO)ACETAMIDO)-3-METILBUTIL)-6-OXO-1,3,2-DIOXABORINANO-4-CARBOXILICO; ACIDO 2,2´-{2-[(1R)-3-METIL-1-({(2S)-3-FENIL-2-[(PIRAZIN-2-ILCARBONIL)AMINO]PROPANOIL}AMINO)BUTIL]-5-OXO-1,3,2-DIOXABOROLANO-4,4-DIIL}DIACETICO, ENTRE OTROS. DICHOS COMPUESTOS SON INHIBIDORES DE PROTEASOMA Y SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES PROLIFERATIVAS CELULARES
PE2009000877A 2008-06-17 2009-06-17 Compuestos de ester boronato y composiciones farmaceuticas de los mismos PE20100256A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US13224408P 2008-06-17 2008-06-17
US21149909P 2009-03-31 2009-03-31

Publications (1)

Publication Number Publication Date
PE20100256A1 true PE20100256A1 (es) 2010-04-14

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ID=41061278

Family Applications (5)

Application Number Title Priority Date Filing Date
PE2014000151A PE20141078A1 (es) 2008-06-17 2009-06-17 Compuestos de ester boronato y composiciones farmaceuticas de los mismos
PE2014000152A PE20141076A1 (es) 2008-06-17 2009-06-17 Compuestos de ester boronato y composiciones farmaceuticas de los mismos
PE2014000153A PE20141065A1 (es) 2008-06-17 2009-06-17 Compuestos de ester boronato y composiciones farmaceuticas de los mismos
PE2009000877A PE20100256A1 (es) 2008-06-17 2009-06-17 Compuestos de ester boronato y composiciones farmaceuticas de los mismos
PE2014000150A PE20141064A1 (es) 2008-06-17 2009-06-17 Compuestos de ester boronato y composciones farmaceuticas de los mismos

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PE2014000151A PE20141078A1 (es) 2008-06-17 2009-06-17 Compuestos de ester boronato y composiciones farmaceuticas de los mismos
PE2014000152A PE20141076A1 (es) 2008-06-17 2009-06-17 Compuestos de ester boronato y composiciones farmaceuticas de los mismos
PE2014000153A PE20141065A1 (es) 2008-06-17 2009-06-17 Compuestos de ester boronato y composiciones farmaceuticas de los mismos

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PE2014000150A PE20141064A1 (es) 2008-06-17 2009-06-17 Compuestos de ester boronato y composciones farmaceuticas de los mismos

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US (17) US20090325903A1 (es)
EP (6) EP2318419B1 (es)
JP (9) JP5566380B2 (es)
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Families Citing this family (82)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL1948678T3 (pl) 2005-11-09 2013-09-30 Onyx Therapeutics Inc Związki do hamowania enzymów
DK2041158T3 (da) 2006-06-19 2013-06-24 Onyx Therapeutics Inc Peptid-epoxidketoner til proteasom inhibering
KR20150131405A (ko) 2007-10-04 2015-11-24 오닉스 세라퓨틱스, 인크. 결정형 펩티드 에폭시 케톤 프로테아제 저해제 및 아미노산 케토-에폭시드의 합성
KR101690571B1 (ko) * 2008-06-17 2016-12-28 밀레니엄 파머슈티컬스 인코퍼레이티드 보로네이트 에스테르 화합물 및 이의 제약학적 조성물
KR101023994B1 (ko) 2008-08-28 2011-03-28 한국생산기술연구원 디지털 밴드용 커넥터, 리셉터클 및 커넥터 조립체
AR075090A1 (es) 2008-09-29 2011-03-09 Millennium Pharm Inc Derivados de acido 1-amino-2-ciclobutiletilboronico inhibidores de proteosoma,utiles como agentes anticancerigenos, y composiciones farmaceuticas que los comprenden.
EP2349313A4 (en) 2008-10-21 2012-08-29 Onyx Therapeutics Inc COMBINATION THERAPY WITH EPOXYCLETON PEPTIDES
AR075899A1 (es) 2009-03-20 2011-05-04 Onyx Therapeutics Inc Tripeptidos epoxicetonas cristalinos inhibidores de proteasa
US8853147B2 (en) 2009-11-13 2014-10-07 Onyx Therapeutics, Inc. Use of peptide epoxyketones for metastasis suppression
MX2012010017A (es) 2010-03-01 2012-10-01 Onyx Therapeutics Inc Compuestos de para la inhibicion de inmunoproteasomas.
CN102892291A (zh) 2010-03-31 2013-01-23 米伦纽姆医药公司 1-氨基-2-环丙基乙硼酸衍生物
CA2813003A1 (en) 2010-10-05 2012-04-12 Fresenius Kabi Usa, Llc Bortezomib formulations stabilised with boric acid
CN102784114B (zh) * 2011-05-14 2016-03-02 山东新时代药业有限公司 一种硼替佐米冻干粉针及其制备方法
CA2833775A1 (en) 2011-06-22 2012-12-27 Cephalon, Inc. Proteasome inhibitors and processes for their preparation, purification and use
EP2567959B1 (en) 2011-09-12 2014-04-16 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
EP2776043B1 (en) * 2011-11-11 2018-02-21 Millennium Pharmaceuticals, Inc. Biomarkers of response to proteasome inhibitors
WO2013071163A2 (en) 2011-11-11 2013-05-16 Millennium Pharamaceuticals, Inc. Biomarkers of response to proteasome inhibitors
US9732101B2 (en) 2012-01-18 2017-08-15 Wisconsin Alumni Research Foundation Bioreversible boronates for delivery of molecules into cells
WO2013110005A1 (en) 2012-01-18 2013-07-25 Wisconsin Alumni Research Foundation Boronate-mediated delivery of molecules into cells
CN104271583B (zh) 2012-01-24 2017-10-24 米伦纽姆医药公司 治疗鼻咽癌的方法
CA2862492A1 (en) 2012-01-24 2013-08-01 Millennium Pharmaceuticals, Inc. Methods of treatment of cancer
AU2013227219A1 (en) * 2012-03-02 2014-10-23 Dr. Reddy's Laboratories Limited Pharmaceutical compositions comprising boronic acid compounds
CA2784240C (en) 2012-03-27 2014-07-08 Innopharma, Inc. Stable bortezomib formulations
US20140105921A1 (en) 2012-07-09 2014-04-17 Onyx Therapeutics, Inc. Prodrugs of Peptide Epoxy Ketone Protease Inhibitors
ITMI20121394A1 (it) 2012-08-06 2014-02-07 Chemi Spa Esteri di bortezomib e loro formulazioni
US20170035917A1 (en) * 2013-06-10 2017-02-09 Millennium Pharmaceuticals, Inc. Methods of treatment of cancer
WO2015025000A1 (en) * 2013-08-23 2015-02-26 Synthon B.V. Pharmaceutical compositions comprising bortezomib
CN105705149A (zh) * 2013-10-03 2016-06-22 米伦纽姆医药公司 用于预防或治疗系统性红斑狼疮和/或狼疮性肾炎的方法
CN111116622A (zh) * 2014-02-03 2020-05-08 俄亥俄州创新基金会 硼酸酯和其药物制剂
JP2015200016A (ja) * 2014-03-31 2015-11-12 富士フイルム株式会社 水分解用光電極、水分解装置
KR102481856B1 (ko) * 2014-05-20 2022-12-26 밀레니엄 파머슈티컬스 인코퍼레이티드 일차 암 치료법 후 사용하기 위한 붕소-함유 프로테아좀 저해제
WO2016022955A1 (en) 2014-08-07 2016-02-11 Mayo Foundation For Medical Education And Research Compounds and methods for treating cancer
EP3212196A4 (en) 2014-10-29 2018-07-11 Wisconsin Alumni Research Foundation Boronic acid inhibitors of hiv protease
EP3031811A1 (en) 2014-12-09 2016-06-15 Teva Pharmaceuticals Ltd. Malic acid esters of bortezomib
MA41505A (fr) * 2015-02-11 2017-12-19 Millennium Pharm Inc Nouvelle forme cristalline d'un inhibiteur de protéasome
MA41555A (fr) * 2015-02-17 2017-12-26 Millennium Pharm Inc Polythérapie pour le traitement du cancer
CZ2015233A3 (cs) 2015-04-03 2016-10-12 Zentiva, K.S. Způsob přípravy Ixazomib citrátu
CZ2015253A3 (cs) 2015-04-15 2016-10-26 Zentiva, K.S. Nové formy Ixazomib citrátu
EP3310360B1 (en) * 2015-06-19 2024-03-27 Beijing Artivila BioPharma Co. Ltd. Chiral specific boron-containing compounds and their use in treating cancer or amyloidosis
WO2016205790A2 (en) * 2015-06-19 2016-12-22 Hanlin Scientific, Inc. Chiral specific boron-containing compounds and their use in treating cancer or amyloidosis
EP3120837A1 (de) 2015-07-22 2017-01-25 Stada Arzneimittel Ag Verfahren zur herstellung einer bortezomibester-lösung
EP3120836A1 (de) 2015-07-22 2017-01-25 Stada Arzneimittel Ag Gebrauchsfertige bortezomib-lösung
US20180282351A1 (en) * 2015-09-16 2018-10-04 Mylan Laboratories Ltd Amorphous Ixazomib Citrate
CN106608883A (zh) * 2015-10-21 2017-05-03 北京大学 蛋白酶体抑制剂mln9708的合成方法
WO2017079572A1 (en) 2015-11-04 2017-05-11 Millennium Pharmaceuticals, Inc. Methods for the identification, evaluation and treatment of patients having multiple myeloma
CN106986884A (zh) * 2016-01-20 2017-07-28 成都贝斯凯瑞生物科技有限公司 一种高效的高纯度含硼化合物制备方法
CN105622658B (zh) * 2016-03-18 2018-06-19 中国药科大学 非肽类蛋白酶体抑制剂、其药物组合物、制备方法和应用
WO2017163190A1 (en) * 2016-03-23 2017-09-28 Dr. Reddy’S Laboratories Limited Amorphous ixazomib citrate and solid dispersion thereof
CN107224569A (zh) * 2016-03-26 2017-10-03 复旦大学 一种硼替佐米水溶性药用组合物及其制备方法和用途
CZ2016204A3 (cs) 2016-04-08 2017-11-01 Zentiva, K.S. Formulace Ixazomib citrátu formy 3
ES2836050T3 (es) 2016-06-21 2021-06-23 Teva Pharmaceuticals Int Gmbh Formas en estado sólido de citrato de ixazomib
US10995103B2 (en) 2016-07-25 2021-05-04 Shenzhen Targetrx, Inc. Substituted boric acid compound, pharmaceutical composition comprising same, and application thereof
EP3493793A4 (en) * 2016-08-04 2020-04-01 Millennium Pharmaceuticals, Inc. COMBINATION OF PROTEASOM INHIBITORS AND ANTI-CD30 ANTIBODIES
CN108440583B (zh) * 2017-01-23 2020-12-04 成都奥璟生物科技有限公司 一种新的硼酸衍生物及其药物组合物
WO2018160717A1 (en) 2017-02-28 2018-09-07 Mayo Foundation For Medical Education And Research Compounds and methods for treating cancer
WO2018158697A1 (en) 2017-03-03 2018-09-07 Fresenius Kabi Oncology Limited A process for the preparation of ixazomib citrate
WO2018173071A1 (en) * 2017-03-20 2018-09-27 Msn Laboratories Private Limited, R&D Center Novel crystalline forms of ixazomib citrate and its process for preparation thereof
CN106916177B (zh) * 2017-03-23 2019-04-23 南京陵瑞医药科技有限公司 一种氘代的二肽硼酸或其酯类化合物及其合成方法与用途
CN108794516A (zh) * 2017-04-26 2018-11-13 上海时莱生物技术有限公司 硼酸和硼酸酯类化合物及其制备方法和用途
CN108794520B (zh) * 2017-05-02 2020-07-24 北京大学 包括埃沙佐米在内的硼酸柠檬酸酯类化合物的合成方法
WO2019020099A1 (zh) * 2017-07-28 2019-01-31 成都地奥九泓制药厂 一种硼酸酯化合物、其合成方法及其用途
EP3672977B1 (en) 2017-08-24 2022-06-22 Merck Patent GmbH Boronic acid derivatives
WO2019038406A1 (en) 2017-08-25 2019-02-28 Synthon B.V. PROCESS FOR THE PREPARATION OF IXAZOMIB OR ITS INTERMEDIATES
WO2019043544A1 (en) * 2017-09-02 2019-03-07 Sun Pharmaceutical Industries Limited PROCESS FOR THE PREPARATION OF IXAZOMIB CITRATE
CN111108125A (zh) 2017-09-14 2020-05-05 葛兰素史密斯克莱知识产权发展有限公司 用于癌症的组合治疗
CN113603713A (zh) * 2017-12-05 2021-11-05 深圳市塔吉瑞生物医药有限公司 一种取代的硼酸酯化合物的制备方法及其晶型
US10537585B2 (en) 2017-12-18 2020-01-21 Dexcel Pharma Technologies Ltd. Compositions comprising dexamethasone
US10118937B1 (en) 2018-01-03 2018-11-06 Scinopharm Taiwan, Ltd. Process for preparing ixazomib citrate and intermediates therefor
CN110041353A (zh) * 2018-01-16 2019-07-23 成都译山生物科技有限公司 一种新的硼酸水杨酸酯类衍生物及其药物组合物
IL276813B2 (en) 2018-03-05 2024-09-01 Arcus Biosciences Inc History of 4-substituted 5-amino-octahydrocyclopenta[c]pyrrole-5-carboxylic acid, their pharmaceutical combinations and their use for the treatment of diseases
US11243207B2 (en) 2018-03-29 2022-02-08 Mayo Foundation For Medical Education And Research Assessing and treating cancer
CN110540547A (zh) * 2018-05-28 2019-12-06 秦艳茹 一种肽硼酸酯类化合物的合成与用途
BR112021001359A2 (pt) 2018-07-26 2021-04-20 Merck Patent Gmbh derivados de ácido borônico
CN112513052B (zh) * 2018-08-02 2022-12-16 正大天晴药业集团股份有限公司 氮杂环丁烷衍生物的硼酸酯
CN110903310B (zh) * 2018-09-14 2022-11-22 成都奥璟生物科技有限公司 一种硼酸酯类药物及其用途
CN110357787A (zh) * 2019-08-02 2019-10-22 苏州艾和医药科技有限公司 依沙佐米合成工艺研究
WO2023220641A2 (en) 2022-05-11 2023-11-16 Juno Therapeutics, Inc. Methods and uses related to t cell therapy and production of same
WO2023220655A1 (en) 2022-05-11 2023-11-16 Celgene Corporation Methods to overcome drug resistance by re-sensitizing cancer cells to treatment with a prior therapy via treatment with a t cell therapy
WO2023232830A1 (en) 2022-06-02 2023-12-07 Merck Patent Gmbh Boronic acid adducts
WO2024006337A1 (en) 2022-06-30 2024-01-04 Principia Biopharma Inc. Cyclic boronic esters and their uses
WO2024097905A1 (en) 2022-11-02 2024-05-10 Celgene Corporation Methods of treatment with t cell therapy and immunomodulatory agent maintenance therapy
CN117964650B (zh) * 2024-03-28 2024-06-07 成都硕德药业有限公司 一种枸橼酸伊沙佐米的制备方法

Family Cites Families (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US449082A (en) * 1891-03-24 milbeadt
US2160413A (en) 1935-04-16 1939-05-30 Schering Ag Polyiodo derivatives of acylamino acids and their salts and a method of making the same
NZ203706A (en) 1982-04-22 1986-03-14 Squibb & Sons Inc Occlusive multi-layer wound dressing and hydrocolloidal granules for wound treatment
US4499082A (en) 1983-12-05 1985-02-12 E. I. Du Pont De Nemours And Company α-Aminoboronic acid peptides
JPS6233170A (ja) 1985-08-07 1987-02-13 Tokuyama Soda Co Ltd 環状ポリエ−テル化合物
JPH0813759B2 (ja) 1986-09-01 1996-02-14 富士写真フイルム株式会社 アルコキシベンゼン誘導体の製造方法
JP2512303B2 (ja) 1987-03-20 1996-07-03 呉羽化学工業株式会社 ２−オキサゾリン−４，５−ジオンのフエニルヒドラゾン誘導体
US5250720A (en) 1987-06-05 1993-10-05 The Dupont Merck Pharmaceutical Company Intermediates for preparing peptide boronic acid inhibitors of trypsin-like proteases
US5242904A (en) 1987-06-05 1993-09-07 The Dupont Merck Pharmaceutical Company Peptide boronic acid inhibitors of trypsin-like proteases
US5187157A (en) 1987-06-05 1993-02-16 Du Pont Merck Pharmaceutical Company Peptide boronic acid inhibitors of trypsin-like proteases
EP0315574A3 (de) 1987-11-05 1990-08-22 Hoechst Aktiengesellschaft Renin-Inhibitoren
US5159060A (en) * 1988-05-27 1992-10-27 Mayo Foundation For Medical Education And Research Cytotoxic boronic acid peptide analogs
US5106948A (en) 1988-05-27 1992-04-21 Mao Foundation For Medical Education And Research Cytotoxic boronic acid peptide analogs
DE3827340A1 (de) 1988-08-12 1990-02-15 Hoechst Ag Verwendung von (alpha)-aminoboronsaeure-derivaten zur prophylaxe und behandlung von viruserkrankungen
MX9206628A (es) 1991-11-22 1993-05-01 Boehringer Ingelheim Pharma Ester de prolinaboronato y metodo para su preparacion.
US5442100A (en) * 1992-08-14 1995-08-15 The Procter & Gamble Company β-aminoalkyl and β-N-peptidylaminoalkyl boronic acids
ES2098484T3 (es) * 1992-08-14 1997-05-01 Procter & Gamble Detergentes liquidos que contienen un acido alfa-amino-boronico.
US5935944A (en) * 1993-09-10 1999-08-10 Neutron Technology Corporation Formulation for I.V. administration of the boron delivery drug, boronophenylalanine (BPA)
US5492900A (en) * 1993-09-10 1996-02-20 Neutron Technology Corporation Method for enhancing the solubility of the boron delivery drug, boronophenylalanine (BPA)
US6060462A (en) * 1993-10-20 2000-05-09 Dupont Pharmaceuticals Company Electrophilic peptide analogs as inhibitors of trypsin-like enzymes
FR2712602B1 (fr) 1993-11-18 1996-02-09 Centre Nat Rech Scient Virus recombinants, préparation et utilisation en thérapie génique.
US5574017A (en) * 1994-07-05 1996-11-12 Gutheil; William G. Antibacterial agents
US6083903A (en) * 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
US5614649A (en) 1994-11-14 1997-03-25 Cephalon, Inc. Multicatalytic protease inhibitors
JP3403009B2 (ja) 1996-07-12 2003-05-06 キヤノン株式会社 可動部材の変位と気泡成長を伴う液体吐出方法、該吐出方法に用いられる液体吐出ヘッド、ヘッドカートリッジ及びこれらを用いた液体吐出装置
US5834487A (en) 1996-09-24 1998-11-10 Cv Therapeutics Inhibition of 26S and 20S proteasome by indanones
CA2281224A1 (en) 1997-02-15 1998-08-20 Proscript, Inc. Treatment of infarcts through inhibition of nf-kappab
CA2304622A1 (en) 1997-09-25 1999-04-01 Proscript, Inc. Proteasome inhibitors, ubiquitin pathway inhibitors or agents that interfere with the activation of nf-?b via the ubiquitin proteasome pathway to treat inflammatory and autoimmunediseases
CA2314259A1 (en) 1997-12-16 1999-06-24 Robert Siman Multicatalytic protease inhibitors for use as anti-tumor agents
US6075150A (en) 1998-01-26 2000-06-13 Cv Therapeutics, Inc. α-ketoamide inhibitors of 20S proteasome
AU6229699A (en) 1998-10-26 2000-05-15 Sumitomo Pharmaceuticals Company, Limited Beta-amyloid formation inhibitors
US6169076B1 (en) * 1999-03-31 2001-01-02 Glcosyn Pharmaceuticals, Inc. P-Boronophenylalanine complexes with fructose and related carbohydrates and polyols
US6121149A (en) 1999-04-22 2000-09-19 Advanced Micro Devices, Inc. Optimized trench/via profile for damascene filling
KR100307027B1 (ko) 1999-06-17 2001-11-01 서평원 액정 표시장치 및 이것을 이용한 이동 통신 단말기의 표시장치
AU5920400A (en) 1999-07-07 2001-01-22 Du Pont Pharmaceuticals Company Cell-based assay systems for examining hcv ns3 protease activity
SE0100714D0 (sv) 2000-07-13 2001-02-28 Ap Biotech Ab Reaction vessel and method for distributing fluid in such a vessel
US6846806B2 (en) 2000-10-23 2005-01-25 Bristol-Myers Squibb Company Peptide inhibitors of Hepatitis C virus NS3 protein
JP2002145848A (ja) * 2000-11-10 2002-05-22 Kyorin Pharmaceut Co Ltd アルケニルアミノ酸誘導体及びその製造法
EP1217000A1 (en) * 2000-12-23 2002-06-26 Aventis Pharma Deutschland GmbH Inhibitors of factor Xa and factor VIIa
CA2435146C (en) * 2001-01-25 2011-03-29 The United States Of America, Represented By The Secretary, Department Of Health And Human Services Formulation of boronic acid compounds
ATE317850T1 (de) 2001-05-30 2006-03-15 Novartis Pharma Gmbh 2-((n-(2-amino-3-(heteroaryl- oder - aryl)propionyl)aminoacyl)amino)- alkylboronsäurederivate
DE10131283A1 (de) 2001-06-28 2003-01-09 Philips Corp Intellectual Pty Phased Array Antenne
WO2003033506A1 (fr) 2001-10-12 2003-04-24 Kyorin Pharmaceutical Co., Ltd. Derive d'acide d'aminoborane et medicament inhibiteur de proteasomes le contenant
JPWO2003033507A1 (ja) 2001-10-12 2005-02-03 杏林製薬株式会社 ベンジルマロン酸誘導体およびそれを含有するプロテアソーム阻害薬
AU2003219652A1 (en) 2002-01-08 2003-07-30 Eisai Co. Ltd. Eponemycin and epoxomicin analogs and uses thereof
AU2003223930A1 (en) 2002-06-14 2003-12-31 Novo Nordisk A/S Pharmaceutical use of boronic acids and esters thereof
PT1396270E (pt) 2002-09-09 2006-08-31 Trigen Ltd Processo para a preparacao de compostos uteisncomo intermidiarios.
US20060084592A1 (en) 2002-09-09 2006-04-20 Trigen Limited Peptide boronic acid inhibitors
TW200418791A (en) 2003-01-23 2004-10-01 Bristol Myers Squibb Co Pharmaceutical compositions for inhibiting proteasome
US7135575B2 (en) * 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
US7576206B2 (en) * 2003-08-14 2009-08-18 Cephalon, Inc. Proteasome inhibitors and methods of using the same
CN1867572B (zh) * 2003-08-14 2012-03-28 赛福伦公司 蛋白酶体抑制剂及其使用方法
US7223745B2 (en) 2003-08-14 2007-05-29 Cephalon, Inc. Proteasome inhibitors and methods of using the same
GB0405267D0 (en) 2004-03-09 2004-04-21 Trigen Ltd Compounds
PT2377869E (pt) * 2004-03-30 2014-04-15 Millennium Pharm Inc Síntese de bortezomib
DK2030981T3 (da) 2004-05-10 2014-10-13 Onyx Therapeutics Inc Forbindelser til proteasom-enzymhæmning
WO2006008660A2 (en) 2004-07-20 2006-01-26 Affinium Pharmaceuticals, Inc. Streptococcus pneumoniae enoyl- (acyl-carrier-protein) reductase (fabk)
TW200618820A (en) 2004-11-05 2006-06-16 Alza Corp Liposome formulations of boronic acid compounds
US7468383B2 (en) 2005-02-11 2008-12-23 Cephalon, Inc. Proteasome inhibitors and methods of using the same
CN101120006A (zh) * 2005-02-11 2008-02-06 赛福伦公司 蛋白酶体抑制剂及其使用方法
AU2006242446A1 (en) 2005-04-29 2006-11-09 Kosan Biosciences Incorporated Method of treating multiple myeloma using 17-AAG or 17-AG or a prodrug of either in combination with a proteasome inhibitor
JP5229897B2 (ja) 2005-07-05 2013-07-03 タフツ ユニバーシティー／トラスティーズ オブ タフツ カレッジ 線維芽細胞活性化タンパクα阻害剤
RU2008127486A (ru) * 2005-12-08 2010-01-20 Милленниум Фармасьютикалз, Инк. (Us) Бициклические соединения с ингибиторной активностью в отношении киназы
WO2007089618A2 (en) 2006-01-27 2007-08-09 Phenomix Corporation Hepatitis c serine protease inhibitors and uses therefor
CN101415691B (zh) 2006-02-03 2011-12-14 大正制药株式会社 三唑衍生物
CL2007002499A1 (es) * 2006-08-30 2008-03-14 Phenomix Corp Sales citrato y tartrato de compuestos derivados de acido pirrolidinilaminoacetilpirrolidinboronico, inhibidores de dpp-iv; metodo de preparacion; forma solida; combinacion farmaceutica, util para el tratamiento de diabetes.
WO2009006473A2 (en) 2007-07-05 2009-01-08 Trustees Of Tufts College Pro-soft polypeptide proteasome inhibitors, and methods of use thereof
KR20150010802A (ko) 2007-08-06 2015-01-28 밀레니엄 파머슈티컬스 인코퍼레이티드 프로테아좀 억제제
US7442830B1 (en) * 2007-08-06 2008-10-28 Millenium Pharmaceuticals, Inc. Proteasome inhibitors
ITMI20072397A1 (it) 2007-12-20 2009-06-21 Gambro Lundia Ab Apparecchiatura medicale per il trattamento extracorporeo
KR101690571B1 (ko) * 2008-06-17 2016-12-28 밀레니엄 파머슈티컬스 인코퍼레이티드 보로네이트 에스테르 화합물 및 이의 제약학적 조성물
AR075090A1 (es) 2008-09-29 2011-03-09 Millennium Pharm Inc Derivados de acido 1-amino-2-ciclobutiletilboronico inhibidores de proteosoma,utiles como agentes anticancerigenos, y composiciones farmaceuticas que los comprenden.
CN102892291A (zh) 2010-03-31 2013-01-23 米伦纽姆医药公司 1-氨基-2-环丙基乙硼酸衍生物
WO2012148336A1 (en) 2011-04-29 2012-11-01 Telefonaktiebolaget L M Ericsson (Publ) Decentralised control of interference reduction in a wireless communication system
JP5724951B2 (ja) 2012-06-11 2015-05-27 日立金属株式会社 ネットワーク管理装置
JP6357023B2 (ja) 2014-06-06 2018-07-11 任天堂株式会社 情報処理プログラム、情報処理装置、情報処理装置の制御方法および情報処理システム

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UA115131C2 (uk) 2017-09-25
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US20190048028A1 (en) 2019-02-14
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US10604538B2 (en) 2020-03-31
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BR122014008754A2 (pt) 2015-11-03
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BRPI0915300A2 (pt) 2015-10-27
JP6110813B2 (ja) 2017-04-05
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PE20141078A1 (es) 2014-09-05
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ES2541467T3 (es) 2015-07-20
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