[go: up one dir, main page]

AR075090A1 - Derivados de acido 1-amino-2-ciclobutiletilboronico inhibidores de proteosoma,utiles como agentes anticancerigenos, y composiciones farmaceuticas que los comprenden. - Google Patents

Derivados de acido 1-amino-2-ciclobutiletilboronico inhibidores de proteosoma,utiles como agentes anticancerigenos, y composiciones farmaceuticas que los comprenden.

Info

Publication number
AR075090A1
AR075090A1 ARP090103760A ARP090103760A AR075090A1 AR 075090 A1 AR075090 A1 AR 075090A1 AR P090103760 A ARP090103760 A AR P090103760A AR P090103760 A ARP090103760 A AR P090103760A AR 075090 A1 AR075090 A1 AR 075090A1
Authority
AR
Argentina
Prior art keywords
aliphatic
independently
substituted
unsubstituted
con
Prior art date
Application number
ARP090103760A
Other languages
English (en)
Inventor
Paul E Fleming
Jing Li
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
Application filed by Millennium Pharm Inc filed Critical Millennium Pharm Inc
Publication of AR075090A1 publication Critical patent/AR075090A1/es

Links

Classifications

    • 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
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • 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
    • C07F5/04—Esters of boric acids
    • 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
    • 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
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • C07K5/08—Tripeptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Heart & Thoracic Surgery (AREA)

Abstract

Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1): o una sal farmacéuticamente aceptable o un anhídrido de ácido boronico del mismo, donde: A es 0, 1 o 2; P es hidrogeno o una porcion bloqueante del grupo amino: Ra1 es C1-6 alifático, C1-6 fluoroalifático, -(CH2)m-CH2-Rb, (CH2)m-CH2-NHC(=NR4)NH-Y, -(CH2)m-CH2-CON(R4)2, -(CH2)m-CH2-N(R4)CON(R4)2, -(CH2)m-CH(R6)N(R4)2, -(CH2)m-CH(R5)-OR5, o -(CH2)m-CH(R5)-SR5; cada Ra2 es en forma independiente hidrogeno, C1-6 alifático, C1-6 fluoroalifático, (CH2)m-CH2-Rb, -(CH2)m-CH2-NHC(=NR4)NH-Y, -(CH2)m-CH2-CON(R4)2, -(CH2)m-CH2-N(R4)CON(R4)2, -(CH2)m-CH(R6)N(R4)2, -(CH2)m-CH(R5)-OR5, o -(CH2)m-CH(R5)-SR5; cada Y es en forma independiente hidrogeno, -CN, -NO2, o -S(O)2-R10; cada Rb es en forma independiente un sistema de anillos monocíclico o bicíclico sustituido o no sustituido; cada R4 es en forma independiente hidrogeno o un grupo alifático, arilo, heteroarilo, o heterocíclilo sustituido o no sustituido: o dos R4 sobre el mismo átomo de nitrogeno, tomados junto con el átomo de nitrogeno, forman un anillo heterocíclilo de 4 a 8 miembros sustituido o no sustituido que tiene, además del átomo de nitrogeno, entre 0 y 2 heteroátomos del anillo seleccionados en forma independiente entre N, O, y S, cada R5 es en forma independiente hidrogeno o un grupo alifático, arilo, heteroarilo, o heterocíclilo sustituido o no sustituido: cada R6 es en forma independiente un grupo alifático, arilo, o heteroarilo sustituido o no sustituido: cada R10 es en forma independiente C1-6 alifático, C6-10 arilo, o -N(R4)2; m es 0, 1, o 2; Z1 y Z2 son cada uno en forma independiente hidroxi, alcoxi, ariloxi, o aralcoxi: o Z1 y Z2 juntos forman una porcion derivada de un agente de complexion de ácido boronico.
ARP090103760A 2008-09-29 2009-09-12 Derivados de acido 1-amino-2-ciclobutiletilboronico inhibidores de proteosoma,utiles como agentes anticancerigenos, y composiciones farmaceuticas que los comprenden. AR075090A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US19461408P 2008-09-29 2008-09-29

Publications (1)

Publication Number Publication Date
AR075090A1 true AR075090A1 (es) 2011-03-09

Family

ID=41426361

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090103760A AR075090A1 (es) 2008-09-29 2009-09-12 Derivados de acido 1-amino-2-ciclobutiletilboronico inhibidores de proteosoma,utiles como agentes anticancerigenos, y composiciones farmaceuticas que los comprenden.

Country Status (25)

Country Link
US (3) US8664200B2 (es)
EP (1) EP2346882B1 (es)
JP (3) JP5736314B2 (es)
KR (1) KR101739470B1 (es)
CN (2) CN103554143B (es)
AR (1) AR075090A1 (es)
AU (1) AU2009297113B2 (es)
BR (1) BRPI0919447B8 (es)
CA (1) CA2739375C (es)
CL (1) CL2011000653A1 (es)
CO (1) CO6362015A2 (es)
CR (2) CR20160475A (es)
DO (1) DOP2011000086A (es)
EA (1) EA030539B1 (es)
EC (1) ECSP11011011A (es)
IL (1) IL211983A0 (es)
MA (1) MA32729B1 (es)
MX (1) MX2011003317A (es)
MY (1) MY166653A (es)
NZ (2) NZ606001A (es)
SG (1) SG194388A1 (es)
TW (2) TWI598352B (es)
UA (1) UA105503C2 (es)
WO (1) WO2010036357A1 (es)
ZA (1) ZA201203615B (es)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2628620T3 (es) 2005-11-09 2017-08-03 Onyx Therapeutics, Inc. Compuesto para inhibición de enzimas
CA2657213C (en) 2006-06-19 2017-01-03 Proteolix, Inc. Peptide epoxyketones for proteasome inhibition
KR20100088664A (ko) 2007-10-04 2010-08-10 오닉스 세라퓨틱스, 인크. 결정형 펩티드 에폭시 케톤 프로테아제 저해제 및 아미노산 케토-에폭시드의 합성
EA030685B1 (ru) 2008-06-17 2018-09-28 Милленниум Фармасьютикалз, Инк. Способ получения соединения боронатного эфира
US20110236428A1 (en) 2008-10-21 2011-09-29 Onyx Therapeutics, Inc. Combination therapy with peptide epoxyketones
AR075899A1 (es) 2009-03-20 2011-05-04 Onyx Therapeutics Inc Tripeptidos epoxicetonas cristalinos inhibidores de proteasa
WO2011060179A1 (en) 2009-11-13 2011-05-19 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.
US8513218B2 (en) 2010-03-31 2013-08-20 Millennium Pharmaceuticals, Inc. Derivatives of 1-amino-2-cyclopropylethylboronic acid
WO2013071142A1 (en) 2011-11-11 2013-05-16 Millennium Pharmaceuticals, Inc. Biomarkers of response to proteasome inhibitors
JP6286358B2 (ja) 2011-11-11 2018-02-28 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． プロテアソーム阻害剤に応答するバイオマーカー
JP6129203B2 (ja) * 2011-12-22 2017-05-17 アレス トレーディング ソシエテ アノニム α−アミノボロン酸誘導体、選択性免疫プロテアソーム阻害剤
EP2810066B1 (en) 2012-01-24 2019-07-31 Millennium Pharmaceuticals, Inc. Methods of treatment of cancer
WO2014011695A2 (en) 2012-07-09 2014-01-16 Onyx Therapeutics, Inc. Prodrugs of peptide epoxy ketone protease inhibitors
US9464098B2 (en) * 2012-12-03 2016-10-11 Hoffmann-La Roche Inc. Substituted triazole boronic acid compounds
MX2016003979A (es) 2013-10-03 2016-06-15 Millennium Pharm Inc Metodo para profilaxis o tratamiento de lupus eritematoso sistemico y/o nefritis lupica.
USRE49816E1 (en) 2014-01-10 2024-01-30 Cornell University Dipeptides as inhibitors of human immunoproteasomes
UY36132A (es) 2014-05-20 2015-11-30 Millennium Pharm Inc Métodos para terapia de cáncer
EP3177292B1 (en) 2014-08-07 2020-11-25 Mayo Foundation for Medical Education and Research Compounds and methods for treating cancer
CN114796207A (zh) 2014-08-18 2022-07-29 康奈尔大学 作为人免疫蛋白酶体的抑制剂的二肽模拟物
US10669289B2 (en) * 2014-10-01 2020-06-02 Merck Patent Gmbh Boronic acid derivatives
SG11201702623TA (en) * 2014-10-01 2017-04-27 Merck Patent Gmbh Boronic acid derivatives
CN107074885B (zh) * 2014-10-01 2020-11-27 默克专利股份公司 硼酸衍生物
RU2017115193A (ru) * 2014-10-01 2018-11-06 Мерк Патент Гмбх Производные бороновой кислоты
KR102764027B1 (ko) 2015-10-15 2025-02-07 코넬 유니버시티 프로테아좀 억제제 및 이의 용도
DK3472149T3 (da) 2016-06-21 2023-11-27 Orion Ophthalmology LLC Heterocykliske prolinamidderivater
JP7164521B2 (ja) 2016-06-21 2022-11-01 オリオン・オフサルモロジー・エルエルシー 炭素環式プロリンアミド誘導体
WO2018160717A1 (en) 2017-02-28 2018-09-07 Mayo Foundation For Medical Education And Research Compounds and methods for treating cancer
EP3694605A4 (en) 2017-10-11 2021-10-27 Cornell University PEPTIDOMIMETIC PROTEASOME INHIBITORS
US11243207B2 (en) 2018-03-29 2022-02-08 Mayo Foundation For Medical Education And Research Assessing and treating cancer
PL3952995T3 (pl) 2019-04-12 2024-03-11 Riboscience Llc Pochodne bicyklicznych heteroaryli jako inhibitory ekto- pirofosfatazy/fosfodiesterazy nukleotydowej 1

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US5187157A (en) 1987-06-05 1993-02-16 Du Pont Merck Pharmaceutical Company 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
US5250720A (en) 1987-06-05 1993-10-05 The Dupont Merck Pharmaceutical Company Intermediates for preparing peptide boronic acid inhibitors of trypsin-like proteases
EP0315574A3 (de) * 1987-11-05 1990-08-22 Hoechst Aktiengesellschaft Renin-Inhibitoren
US5106948A (en) 1988-05-27 1992-04-21 Mao Foundation For Medical Education And Research Cytotoxic boronic acid peptide analogs
US5159060A (en) 1988-05-27 1992-10-27 Mayo 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
EP0583536B1 (en) 1992-08-14 1997-03-05 The Procter & Gamble Company Liquid detergents containing an alpha-amino boronic acid
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
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
US6271199B2 (en) 1997-02-15 2001-08-07 Millennium Pharmaceuticals, Inc. Treatment of infarcts
WO1999015183A1 (en) 1997-09-25 1999-04-01 Proscript Inc. PROTEASOME INHIBITORS, UBIQUITIN PATHWAY INHIBITORS OR AGENTS THAT INTERFERE WITH THE ACTIVATION OF NF-λB VIA THE UBIQUITIN PROTEASOME PATHWAY TO TREAT INFLAMMATORY AND AUTOIMMUNE DISEASES
WO1999030707A1 (en) 1997-12-16 1999-06-24 Cephalon Inc. Multicatalytic protease inhibitors for use as anti-tumor agents
US6169076B1 (en) 1999-03-31 2001-01-02 Glcosyn Pharmaceuticals, Inc. P-Boronophenylalanine complexes with fructose and related carbohydrates and polyols
AU5788800A (en) 1999-07-07 2001-01-22 Du Pont Pharmaceuticals Company Peptide boronic acid inhibitors of hepatitis c virus protease
US6846806B2 (en) * 2000-10-23 2005-01-25 Bristol-Myers Squibb Company Peptide inhibitors of Hepatitis C virus NS3 protein
CA2435124A1 (en) 2001-01-25 2002-08-01 Millennium Pharmaceuticals, Inc. Formulation of boronic acid compounds
US6933290B2 (en) 2001-05-30 2005-08-23 Novartis Ag 2-{N-(2-amino-3-(heteroaryl or aryl)propionyl)-aminoacyl}-amino}-alkylboronic acid derivatives
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
US7524883B2 (en) 2002-01-08 2009-04-28 Eisai R&D Management Co., Ltd. Eponemycin and epoxomicin analogs and uses thereof
WO2003105860A1 (en) 2002-06-14 2003-12-24 Novo Nordisk A/S Pharmaceutical use of boronic acids and esters thereof
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
US7223745B2 (en) 2003-08-14 2007-05-29 Cephalon, Inc. Proteasome inhibitors and methods of using the same
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
GB0405267D0 (en) 2004-03-09 2004-04-21 Trigen Ltd Compounds
RS65253B1 (sr) 2004-03-30 2024-03-29 Millennium Pharm Inc Sinteza jedinjenja estra organoborne kiseline i organoborne kiseline
US7468383B2 (en) 2005-02-11 2008-12-23 Cephalon, Inc. Proteasome inhibitors and methods of using the same
MX2008000318A (es) 2005-07-05 2008-03-11 Tufts College Inhibidores de la proteina alfa de activacion del fibroblasto.
JP2009524681A (ja) 2006-01-27 2009-07-02 フェノミックス コーポレーション Ｃ型肝炎ウイルスセリンプロテアーゼインヒビターおよびそのための使用
WO2009006473A2 (en) 2007-07-05 2009-01-08 Trustees Of Tufts College Pro-soft polypeptide proteasome inhibitors, and methods of use thereof
US7442830B1 (en) 2007-08-06 2008-10-28 Millenium Pharmaceuticals, Inc. Proteasome inhibitors
KR20140042933A (ko) 2007-08-06 2014-04-07 밀레니엄 파머슈티컬스 인코퍼레이티드 프로테아좀 억제제
EA030685B1 (ru) 2008-06-17 2018-09-28 Милленниум Фармасьютикалз, Инк. Способ получения соединения боронатного эфира
US8513218B2 (en) * 2010-03-31 2013-08-20 Millennium Pharmaceuticals, Inc. Derivatives of 1-amino-2-cyclopropylethylboronic acid

Also Published As

Publication number Publication date
CR20110216A (es) 2011-07-14
TWI598352B (zh) 2017-09-11
CO6362015A2 (es) 2012-01-20
US8664200B2 (en) 2014-03-04
IL211983A0 (en) 2011-06-30
EP2346882B1 (en) 2017-09-20
UA105503C2 (uk) 2014-05-26
SG194388A1 (en) 2013-11-29
KR101739470B1 (ko) 2017-05-24
JP5736314B2 (ja) 2015-06-17
US9771381B2 (en) 2017-09-26
ECSP11011011A (es) 2011-07-29
EA201170508A1 (ru) 2011-10-31
US10035811B2 (en) 2018-07-31
US20100081633A1 (en) 2010-04-01
JP2015143264A (ja) 2015-08-06
EA030539B1 (ru) 2018-08-31
CA2739375C (en) 2019-03-12
EP2346882A1 (en) 2011-07-27
TW201024313A (en) 2010-07-01
MX2011003317A (es) 2011-04-26
CN102203103A (zh) 2011-09-28
AU2009297113B2 (en) 2016-11-10
US20170349611A1 (en) 2017-12-07
BRPI0919447B1 (pt) 2021-03-30
BRPI0919447A2 (pt) 2015-12-15
MA32729B1 (fr) 2011-10-02
US20140194387A1 (en) 2014-07-10
JP2017025091A (ja) 2017-02-02
WO2010036357A1 (en) 2010-04-01
TW201641504A (zh) 2016-12-01
AU2009297113A1 (en) 2010-04-01
KR20110082534A (ko) 2011-07-19
NZ592497A (en) 2013-02-22
NZ606001A (en) 2014-08-29
MY166653A (en) 2018-07-18
CA2739375A1 (en) 2010-04-01
CN103554143B (zh) 2018-02-23
ZA201203615B (en) 2015-03-25
DOP2011000086A (es) 2011-04-15
JP2012504122A (ja) 2012-02-16
BRPI0919447B8 (pt) 2021-05-25
CN103554143A (zh) 2014-02-05
CL2011000653A1 (es) 2011-09-30
CR20160475A (es) 2016-12-19

Similar Documents

Publication Publication Date Title
AR075090A1 (es) Derivados de acido 1-amino-2-ciclobutiletilboronico inhibidores de proteosoma,utiles como agentes anticancerigenos, y composiciones farmaceuticas que los comprenden.
AR080863A1 (es) Derivados del acido1-amino-2-ciclopropiletilboronico, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del cancer.
CO6321289A2 (es) Compuestos de ester boronato y composiciones farmaceuticas de los mismos
CY1124117T1 (el) Ετεροκυκλικες αλκυνυλοβενζολικες ενωσεις και ιατρικες συνθεσεις και χρησεις αυτων
MD4490B1 (ro) Noi compuşi de indolizină, procedeu de obţinere a lor şi compoziţii farmaceutice care îi conţin
CY1120342T1 (el) Ανταγωνιστης πολυκυκλικου lpa1 και χρησεις εξ' αυτου
EA201690287A1 (ru) 1,4-дизамещенные аналоги пиридазин хинолина и способы лечения состояний, связанных с smn-дефицитом
EA201170527A1 (ru) Фармацевтические композиции, включающие соединения бороновой кислоты
PE20150399A1 (es) Nuevos derivados de pirrol, su procedimiento de preparacion y las composiciones farmaceuticas que los contienen
PE20170127A1 (es) Indazol-3-carboxamidas 5-sustituidas y preparacion y uso de las mismas
CY1118572T1 (el) Παραγωγο κυκλοαλκανιου
AR068897A1 (es) Inhibidores de proteasoma
AR080865A1 (es) Derivados de espirotetrahidronaftaleno, composiciones farmaceuticas que los contienen, proceso de preparacion y uso de los mismos para tratar enfermedades neurodegenerativas,tal como alzheimer.
PH12016500553B1 (en) Substituted quinolizine derivatives useful as hiv integrase inhibitors
EA201592250A1 (ru) Пиразолопирролидиновые производные и их применение в лечение заболеваний
MA37400A1 (fr) Composés hétérocyclyle en tant qu'inhibiteurs de mek
AR087309A1 (es) Compuesto heterociclico de anillos condensados sustituido, composicion farmaceutica que lo comprende y su uso para la fabricacion de un medicamento para el tratamiento de enfermedades neurogenerativas y aterosclerosis
BRPI0718966B8 (pt) composto, composição farmacêutica, inibidor plk1 e agente antitumoral
EA202090860A1 (ru) Аналоги тиадиазола и способы лечения состояний, связанных с дефицитом smn
WO2011159550A3 (en) Lysophosphatidic acid receptor antagonist and uses thereof
AR123783A2 (es) Dispersión sólida amorfa que comprende un derivado de tetrazol y composición farmacéutica que comprende dicha dispersión
EA201591499A1 (ru) Замещенные бисфенилбутановые производные фосфоновой кислоты в качестве ингибиторов nep (нейтральная эндопептидаза)
MX2015014336A (es) Derivados de glutarimida, uso de los mismos, composicion farmaceutica basada en los mismos y metodos para producir derivados de glutarimida.
PH12015500063B1 (en) Azaindole derivatives which act as pi3k inhibitors
MX391096B (es) Formulación liposomal.

Legal Events

Date Code Title Description
FC Refusal