CN101077875B - 硼酸酯和硼酸化合物,其合成和应用 - Google Patents

硼酸酯和硼酸化合物,其合成和应用 Download PDF

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Publication number
CN101077875B
CN101077875B CN2007100887250A CN200710088725A CN101077875B CN 101077875 B CN101077875 B CN 101077875B CN 2007100887250 A CN2007100887250 A CN 2007100887250A CN 200710088725 A CN200710088725 A CN 200710088725A CN 101077875 B CN101077875 B CN 101077875B
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aryl
alkyl
compound
group
cycloalkyl
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CN101077875A (zh
Inventor
J·亚当斯
马裕庭
R·斯坦恩
M·巴瓦斯基
L·格里尼尔
L·普拉蒙顿
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Millennium Pharmaceuticals Inc
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Millennium Pharmaceuticals Inc
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    • 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
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
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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
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    • A61P19/00—Drugs for skeletal disorders
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    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
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    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/26—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one amino group bound to the carbon skeleton, e.g. lysine
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • 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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    • C07—ORGANIC CHEMISTRY
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    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
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    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
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    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
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    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043—Leu-amino acid
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    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
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    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
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    • C07K5/08—Tripeptides
    • C07K5/0827—Tripeptides 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
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  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
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  • Transplantation (AREA)
  • AIDS & HIV (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pyridine Compounds (AREA)
CN2007100887250A 1994-10-28 1995-10-27 硼酸酯和硼酸化合物,其合成和应用 Expired - Lifetime CN101077875B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US33052594A 1994-10-28 1994-10-28
US80/330,525 1994-10-28
US08/442,581 1995-05-16
US08/442,581 US6083903A (en) 1994-10-28 1995-05-16 Boronic ester and acid compounds, synthesis and uses

Related Parent Applications (1)

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CNB951965905A Division CN1305475C (zh) 1994-10-28 1995-10-27 硼酸酯和硼酸化合物,其合成和应用

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CN101077875A CN101077875A (zh) 2007-11-28
CN101077875B true CN101077875B (zh) 2011-01-26

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CN2007100887250A Expired - Lifetime CN101077875B (zh) 1994-10-28 1995-10-27 硼酸酯和硼酸化合物,其合成和应用
CNB951965905A Expired - Lifetime CN1305475C (zh) 1994-10-28 1995-10-27 硼酸酯和硼酸化合物,其合成和应用

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US (16) US6083903A (enExample)
EP (4) EP1627880B1 (enExample)
JP (1) JP3717934B2 (enExample)
KR (1) KR100398944B1 (enExample)
CN (2) CN101077875B (enExample)
AT (3) ATE241631T1 (enExample)
AU (1) AU710564B2 (enExample)
CA (2) CA2203936C (enExample)
CH (1) CH0788360H1 (enExample)
CY (1) CY2484B1 (enExample)
DE (5) DE69534727T2 (enExample)
DK (3) DK1312609T3 (enExample)
ES (3) ES2254803T3 (enExample)
FI (2) FI114801B (enExample)
FR (1) FR04C0014I2 (enExample)
IL (5) IL115790A (enExample)
LU (1) LU91083I2 (enExample)
MX (1) MX9703063A (enExample)
NL (1) NL300151I2 (enExample)
NO (2) NO310558B1 (enExample)
NZ (2) NZ337211A (enExample)
PT (3) PT1627880E (enExample)
TW (1) TW318850B (enExample)
WO (1) WO1996013266A1 (enExample)

Families Citing this family (307)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6083903A (en) * 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
US6838477B2 (en) * 1995-04-12 2005-01-04 President And Fellows Of Harvard College Lactacystin analogs
FR2758329B1 (fr) * 1997-01-16 1999-02-12 Synthelabo Derives d'imidazole-4-butane boronique, leur preparation et leur utilisation en therapeutique
AU741802B2 (en) 1997-02-15 2001-12-13 Millennium Pharmaceuticals, Inc. Treatment of infarcts through inhibition of NF-kappaB
US6221888B1 (en) * 1997-05-29 2001-04-24 Merck & Co., Inc. Sulfonamides as cell adhesion inhibitors
AU9580098A (en) * 1997-09-25 1999-04-12 Millennium Pharmaceuticals, Inc. Proteasome inhibitors, ubiquitin pathway inhibitors or agents that interfere with the activation of nf-(k)b via the ubiquitin proteasome pathway to treat inflammatory and autoimmune diseases
IL135068A (en) * 1997-09-29 2004-03-28 Point Therapeutics Inc Stimulation of hematopoietic cells in vitro
US6831057B2 (en) * 1997-10-28 2004-12-14 The University Of North Carolina At Chapel Hill Use of NF-κB inhibition in combination therapy for cancer
CA2219867A1 (en) * 1997-10-31 1999-04-30 Jiangping Wu The use of proteasome inhibitors for treating cancer, inflammation, autoimmune disease, graft rejection and septic shock
DE19802450A1 (de) * 1998-01-23 1999-07-29 Hoechst Marion Roussel De Gmbh Ustilipide, Verfahren zu deren Herstellung sowie deren Verwendung
US6075150A (en) * 1998-01-26 2000-06-13 Cv Therapeutics, Inc. α-ketoamide inhibitors of 20S proteasome
US6617171B2 (en) 1998-02-27 2003-09-09 The General Hospital Corporation Methods for diagnosing and treating autoimmune disease
FR2779653B1 (fr) 1998-06-11 2002-12-20 Inst Nat Sante Rech Med Utilisation de composes modulateurs du proteasome en therapie
US6902721B1 (en) * 1998-07-10 2005-06-07 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone growth
US6838436B1 (en) * 1998-07-10 2005-01-04 Osteoscreen Inc. Inhibitors of proteasomal activity for stimulating bone growth
US6462019B1 (en) 1998-07-10 2002-10-08 Osteoscreen, Inc. Inhibitors of proteasomal activity and production for stimulating bone growth
US6979697B1 (en) * 1998-08-21 2005-12-27 Point Therapeutics, Inc. Regulation of substrate activity
EP0982317A1 (en) * 1998-08-26 2000-03-01 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Bivalent inhibitors of the proteasome
CA2347275C (en) * 1998-10-20 2010-03-09 Millennium Pharmaceuticals, Inc. Method for monitoring proteasome inhibitor drug action
US6492333B1 (en) 1999-04-09 2002-12-10 Osteoscreen, Inc. Treatment of myeloma bone disease with proteasomal and NF-κB activity inhibitors
US6890904B1 (en) * 1999-05-25 2005-05-10 Point Therapeutics, Inc. Anti-tumor agents
US6649593B1 (en) * 1999-10-13 2003-11-18 Tularik Inc. Modulators of SREBP processing
US20040039129A1 (en) * 2000-08-16 2004-02-26 Hall Dennis G. Non-pressurized methods for the preparation of conjugrated solid supports for boronic acids
US6919382B2 (en) 2000-08-31 2005-07-19 The Governors Of The University Of Alberta Preparation and uses of conjugated solid supports for boronic acids
JP2004510826A (ja) * 2000-10-12 2004-04-08 ヴィローミクス　ゲゼルシャフト　ミット　ベシュレンクテル　ハフツング ウイルス感染の治療剤
EP2251344B2 (en) * 2001-01-25 2024-04-24 THE UNITED STATES OF AMERICA, represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES Formulation of boronic acid compounds
ES2278049T3 (es) 2001-05-21 2007-08-01 Alcon, Inc. Uso de inhibidores de proteasoma para tratar trastornos de ojo seco.
US7112588B2 (en) * 2001-05-21 2006-09-26 Alcon, Inc. Use of proteasome inhibitors to treat dry eye disorders
WO2002096933A1 (en) * 2001-05-30 2002-12-05 Novartis Ag 2-{[n-(2-amino-3-(heteroaryl or aryl)propionyl)-aminoacyl]-amino}-alkylboronic acid derivatives
JPWO2003033506A1 (ja) * 2001-10-12 2005-02-03 杏林製薬株式会社 アミノボラ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
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
WO2003077928A1 (en) * 2002-03-12 2003-09-25 Ariad Pharmaceuticals, Inc. Peptide analogues and uses thereof
AU2003218735B2 (en) * 2002-03-13 2009-03-12 Janssen Pharmaceutica N.V. Piperazinyl-, piperidinyl- and morpholinyl-derivatives as novel inhibitors of histone deacetylase
OA12790A (en) * 2002-03-13 2006-07-10 Janssen Pharmaceutica Nv New inhibitors of histone deacetylase.
CN1305850C (zh) 2002-03-13 2007-03-21 詹森药业有限公司 作为组蛋白脱乙酰酶新颖抑制剂的磺酰基氨基衍生物
PL205531B1 (pl) 2002-03-13 2010-04-30 Janssen Pharmaceutica Nv Pochodna karbonyloaminowa, jej zastosowanie i sposób wytwarzania oraz kompozycja farmaceutyczna
US20050203029A1 (en) * 2002-04-05 2005-09-15 Ulrich Schubert Agents for treating <I>flaviviridae</I>infections
WO2003106384A2 (en) * 2002-06-01 2003-12-24 Johns Hopkins University Novel boronic chalcone derivatives and uses thereof
JP2006506442A (ja) * 2002-07-09 2006-02-23 ポイント セラピューティクス， インコーポレイテッド ボロプロリン化合物併用療法
DE60311825T2 (de) * 2002-08-14 2007-12-06 Janssen Pharmaceutica N.V. Verwendung von nf-kappa b hemmern zur behandlung von brustdrüsenentzündung
US7371729B2 (en) * 2002-09-09 2008-05-13 Trigen Limited Boronic acid salts useful in parenteral formulations
DE60305113T2 (de) * 2002-09-09 2006-12-07 Trigen Ltd. Borsäuresalze und deren Verwendung in der Bereitstellung von Medikamente für die Thrombosebehandlung
US20050119226A1 (en) * 2003-09-09 2005-06-02 Trigen Limited Methods for synthesizing organoboronic compounds and products thereof
US20050176651A1 (en) * 2002-09-09 2005-08-11 Trigen Limited Peptide boronic acids useful in making salts thereof
US20060084592A1 (en) * 2002-09-09 2006-04-20 Trigen Limited Peptide boronic acid inhibitors
US20050282757A1 (en) * 2002-09-09 2005-12-22 Trigen Limited Peptide boronic acid compounds useful in anticoagulation
CA2497977A1 (en) * 2002-09-20 2004-04-01 Alcon, Inc. Use of cytokine synthesis inhibitors for the treatment of dry eye disorders
MXPA05005923A (es) 2002-12-06 2005-09-21 Millennium Pharm Inc Metodos para la identificacion, valoracion y tratamiento de pacientes con terapia para la inhibicion de la proteasoma.
CN100341880C (zh) * 2003-02-13 2007-10-10 上海仁虎制药股份有限公司 新型硼酸或硼酸酯类化合物、制备方法及在药学上的应用
WO2005007211A2 (en) * 2003-07-03 2005-01-27 Medtronic Vascular Inc. Medical devices with proteasome inhibitors for the treatment of restenosis
US7576206B2 (en) * 2003-08-14 2009-08-18 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US7223745B2 (en) * 2003-08-14 2007-05-29 Cephalon, Inc. Proteasome inhibitors and methods of using the same
EP1682179A4 (en) * 2003-11-05 2008-09-03 Palingen Inc IMPROVED B-CELL CYTOTOXICITY OF CDIM BINDING ANTIBODY
US20060052390A1 (en) * 2003-12-24 2006-03-09 Scios, Inc. Treatment of multiple myeloma by p38 MAP kinase and proteasome inhibition
KR101292707B1 (ko) * 2004-02-23 2013-08-02 트러스티즈 오브 터프츠 칼리지 디펩티딜펩티다아제 ⅳ의 억제제
GB0405272D0 (en) * 2004-03-09 2004-04-21 Trigen Ltd Compounds
US7371875B2 (en) * 2004-03-12 2008-05-13 Miikana Therapeutics, Inc. Cytotoxic agents and methods of use
AU2016202747B2 (en) * 2004-03-30 2017-11-23 Millennium Pharmaceuticals, Inc. Synthesis of boronic ester and acid compounds
PL4008721T3 (pl) * 2004-03-30 2024-05-13 Millennium Pharmaceuticals, Inc. Synteza związków estrów i kwasów boronowych
US8198270B2 (en) 2004-04-15 2012-06-12 Onyx Therapeutics, Inc. Compounds for proteasome enzyme inhibition
CA2562411A1 (en) 2004-04-15 2005-11-10 Proteolix, Inc. Compounds for enzyme inhibition
SG185963A1 (en) 2004-05-10 2012-12-28 Onyx Therapeutics Inc Compounds for enzyme inhibition
EP1765313A2 (en) 2004-06-24 2007-03-28 Novartis Vaccines and Diagnostics, Inc. Compounds for immunopotentiation
AU2005267093B2 (en) 2004-07-23 2009-10-01 Nuada Llc Peptidase inhibitors
WO2006010750A1 (en) 2004-07-28 2006-02-02 Janssen Pharmaceutica N.V. Substituted indolyl alkyl amino derivatives as novel inhibitors of histone deacetylase
EP1805208A2 (en) 2004-10-20 2007-07-11 Proteolix, Inc. Labeled compounds for proteasome inhibition
JP2008519030A (ja) 2004-11-05 2008-06-05 パリンゲン インコーポレーテッド 抗体で誘導される細胞膜損傷
TW200618820A (en) * 2004-11-05 2006-06-16 Alza Corp Liposome formulations of boronic acid compounds
US8017395B2 (en) 2004-12-17 2011-09-13 Lifescan, Inc. Seeding cells on porous supports
US20070098685A1 (en) * 2005-01-19 2007-05-03 Brand Stephen J Methods and kits to treat chronic inflammatory immune diseases by administering a proteasome inhibitor and an interleukin 2 receptor agonist
KR101346886B1 (ko) 2005-01-21 2014-01-02 아스텍스 테라퓨틱스 리미티드 제약 화합물
CA2595749A1 (en) * 2005-01-27 2006-08-03 Research Development Foundation Combination therapy with triterpenoid compounds and proteasome inhibitors
US7468383B2 (en) * 2005-02-11 2008-12-23 Cephalon, Inc. Proteasome inhibitors and methods of using the same
KR101426220B1 (ko) * 2005-02-16 2014-08-05 아나코르 파마슈티칼스 인코포레이티드 보론함유 소분자
EP1863513A2 (en) * 2005-03-11 2007-12-12 The University of North Carolina at Chapel Hill Potent and specific immunoproteasome inhibitors
EP1874297A4 (en) * 2005-04-29 2009-04-22 Kosan Biosciences Inc METHOD OF TREATING MULTIPLE MYELOMES USING 17AGENE OR 17-AG OR A PRODRUG OR ALL IN COMBINATION WITH A PROTEASOMIC INHIBITOR
US8138198B2 (en) 2005-05-18 2012-03-20 Angibaud Patrick Rene Substituted aminopropenyl piperidine or morpholine derivatives as novel inhibitors of histone deacetylase
AU2006202209B2 (en) * 2005-05-27 2011-04-14 Lifescan, Inc. Amniotic fluid derived cells
CA2613889A1 (en) * 2005-06-08 2006-12-14 Centocor, Inc. A cellular therapy for ocular degeneration
EP1912664A2 (en) * 2005-07-06 2008-04-23 Biodevelops Pharma Entwicklung GmbH Use of a compound for enhancing the expression of membrane proteins on the cell surface
EP1752467A1 (en) 2005-08-10 2007-02-14 4Sc Ag Inhibitors of cancer cell, t-cell and keratinocyte proliferation
US7531517B2 (en) 2005-08-10 2009-05-12 4Sc Ag Inhibitors of cancer cell, T-cell and keratinocyte proliferation
US20070059382A1 (en) * 2005-09-09 2007-03-15 Board Of Regents, Univ. And Comm. College System Of Nevada... Medical treatment of breast cancer with boric acid materials
US7687456B2 (en) 2005-11-09 2010-03-30 Proteolix, Inc. Compounds for enzyme inhibition
US20090221488A1 (en) * 2005-12-08 2009-09-03 Wood Kenneth W Certain Compositions and Methods of Treatment
CN106008583A (zh) 2005-12-30 2016-10-12 安纳考尔医药公司 含硼的小分子
WO2007082882A1 (en) * 2006-01-19 2007-07-26 Janssen Pharmaceutica N.V. Substituted indolyl-alkyl-amino-derivatives as inhibitors of histone deacetylase
CA2631874C (en) * 2006-01-19 2014-11-18 Janssen Pharmaceutica N.V. Pyridine and pyrimidine derivatives as inhibitors of histone deacetylase
JP5225104B2 (ja) * 2006-01-19 2013-07-03 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 新しい、ヒストンデアセチラーゼのインヒビターとしてのアミノフェニル誘導体
US8114876B2 (en) * 2006-01-19 2012-02-14 Janssen Pharmaceutica N.V. Pyridine and pyrimidine derivatives as inhibitors of histone deacetylase
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
PE20070978A1 (es) * 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
CA2933994A1 (en) 2006-02-16 2007-08-23 Anacor Pharmaceuticals, Inc. Boron-containing small molecules as anti-inflammatory agents
AR060358A1 (es) * 2006-04-06 2008-06-11 Novartis Vaccines & Diagnostic Quinazolinas para la inhibicion de pdk 1
US8741643B2 (en) 2006-04-28 2014-06-03 Lifescan, Inc. Differentiation of pluripotent stem cells to definitive endoderm lineage
DE102006026464A1 (de) 2006-06-01 2007-12-06 Virologik Gmbh Innovationszentrum Medizintechnik Und Pharma Pharmazeutische Zusammensetzung zur Behandlung von Virusinfektionen und / oder Tumorerkrankungen durch Inhibition der Proteinfaltung und des Proteinabbaus
WO2007143600A2 (en) * 2006-06-05 2007-12-13 Incyte Corporation Sheddase inhibitors combined with cd30-binding immunotherapeutics for the treatment of cd30 positive diseases
EP2484688B1 (en) 2006-06-19 2016-06-08 Onyx Therapeutics, Inc. Peptide epoxyketones for proteasome inhibition
EP2066327B1 (en) * 2006-09-15 2012-11-14 Janssen Pharmaceutica NV Histone deacetylase inhibitors with combined activity on class-i and class-iib histone deacetylases in combination with proteasome inhibitors
EP2066328A2 (en) * 2006-09-15 2009-06-10 Janssen Pharmaceutica N.V. Combinations of class-i specific histone deacetylase inhibitors with proteasome inhibitors
EP2073807A1 (en) 2006-10-12 2009-07-01 Astex Therapeutics Limited Pharmaceutical combinations
JP5528806B2 (ja) 2006-10-12 2014-06-25 アステックス、セラピューティックス、リミテッド 複合薬剤
AU2007221966A1 (en) * 2006-12-08 2008-06-26 Centenary Institute Of Cancer Medicine And Cell Biology Assay for response to proteasome inhibitors
JO3396B1 (ar) 2007-06-20 2019-10-20 Anacor Pharmaceuticals Inc جزيئات صغيرة تحتوي على البورون
US9080145B2 (en) * 2007-07-01 2015-07-14 Lifescan Corporation Single pluripotent stem cell culture
CA3114827C (en) 2007-07-31 2023-09-05 Lifescan, Inc. Differentiation of human embryonic stem cells to pancreatic endocrine
LT2170396T (lt) 2007-08-03 2017-03-10 Summit (Oxford) Limited Vaistų deriniai, skirti diušeno raumenų distrofijos gydymui
GB0715087D0 (en) 2007-08-03 2007-09-12 Summit Corp Plc Drug combinations for the treatment of duchenne muscular dystrophy
US7442830B1 (en) 2007-08-06 2008-10-28 Millenium Pharmaceuticals, Inc. Proteasome inhibitors
GEP20125599B (en) * 2007-08-06 2012-08-10 Millennium Pharm Inc Proteasome inhibitors
AU2016253697A1 (en) * 2007-08-06 2016-11-24 Millennium Pharmaceuticals, Inc. Proteasome inhibitors
EA034601B1 (ru) * 2007-08-06 2020-02-25 Милленниум Фармасьютикалз, Инк. Способ получения бороновых кислот
MX2010002836A (es) * 2007-09-12 2010-03-31 Reddys Lab Ltd Dr Bortezomib y proceso para la produccion del mismo.
US20090076031A1 (en) * 2007-09-17 2009-03-19 Protia, Llc Deuterium-enriched bortezomib
MX2010003732A (es) 2007-10-04 2010-08-09 Onyx Therapeutics Inc Inhibidores de peptido cetona epoxi de proteasa cristalina y la sintesis de ceto-epoxidos de aminoacido.
US7838673B2 (en) * 2007-10-16 2010-11-23 Millennium Pharmaceuticals, Inc. Proteasome inhibitors
US20090110688A1 (en) * 2007-10-24 2009-04-30 Georg Fertig Combination therapy of type ii anti-cd20 antibody with a proteasome inhibitor
CA2954431C (en) * 2007-11-27 2021-08-24 Lifescan, Inc. Differentiation of human embryonic stem cells to pancreatic cells
CN101220048B (zh) * 2007-12-14 2012-08-15 江苏先声药物研究有限公司 ZnCl2催化下的蒎烷二醇酯的制备方法
AU2008340053A1 (en) 2007-12-20 2009-07-02 Novartis Ag Thiazole derivatives used as PI 3 kinase inhibitors
RU2551772C2 (ru) 2008-02-21 2015-05-27 Сентокор Орто Байотек Инк. Способы, поверхностно-модифицированные носители и композиции для иммобилизации, культивирования и открепления клеток
RU2015109165A (ru) * 2008-03-06 2015-11-10 Анакор Фармасьютикалз, Инк. Борсодержащие малые молекулы в качестве противовоспалительных агентов
WO2009140309A2 (en) * 2008-05-12 2009-11-19 Anacor Pharmaceuticals, Inc. Boron-containing small molecules
BR122014008753A2 (pt) * 2008-06-17 2015-12-29 Millennium Pharm Inc compostos de éster boronato e composições farmacêuticas dos mesmos
AU2009267137A1 (en) 2008-06-30 2010-01-07 Centocor Ortho Biotech Inc. Differentiation of pluripotent stem cells
CN101638414B (zh) * 2008-07-30 2014-01-08 江苏先声药物研究有限公司 肽硼酸及其酯类化合物、制备方法及其用途
US20100028307A1 (en) * 2008-07-31 2010-02-04 O'neil John J Pluripotent stem cell differentiation
WO2010028005A1 (en) 2008-09-04 2010-03-11 Anacor Pharmaceuticals, Inc. Boron-containing small molecules
WO2010027975A1 (en) * 2008-09-04 2010-03-11 Anacor Pharmaceuticals, Inc. Boron-containing small molecules
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.
WO2010045503A1 (en) * 2008-10-15 2010-04-22 Anacor Pharmaceuticals, Inc. Boron-containing small molecules as anti-protozoal agents
PE20120059A1 (es) * 2008-10-21 2012-02-27 Onyx Therapeutics Inc Combinaciones farmaceuticas con epoxicetonas peptidicas
MX2011004565A (es) 2008-10-31 2011-07-28 Centocor Ortho Biotech Inc Diferenciacion de celulas madre embrionarias humanas al linaje endocrino pancreatico.
MX2011004563A (es) 2008-10-31 2011-06-01 Centocor Ortho Biotech Inc Diferenciacion de celulas madre embrionarias humanas al linaje endocrino pancreatico.
EP3260534A1 (en) 2008-11-20 2017-12-27 Janssen Biotech, Inc. Pluripotent stem cell culture on micro-carriers
BRPI0921996A2 (pt) * 2008-11-20 2015-08-18 Centocor Ortho Biotech Inc Métodos e composições para cultura e ligação de células em substratos planos.
CN101747354B (zh) * 2008-12-04 2014-08-13 江苏先声药物研究有限公司 一类β氨基酸组成的二肽硼酸及其酯类化合物、制备方法及其用途
CA2744231A1 (en) * 2008-12-17 2010-07-15 Anacor Pharmaceuticals, Inc. Polymorphs of (s)-3-aminomethyl-7-(3-hydroxy-propoxy)-3h-benzo[c][1,2] oxaborol-1-ol
KR20110114562A (ko) 2009-01-09 2011-10-19 썬 파마 어드밴스트 리서치 컴패니 리미티드 보르테조밉 함유 약학적 조성물
WO2010096574A1 (en) 2009-02-20 2010-08-26 Lisanti Michael P A method of diagnosis or prognosis of a neoplasm comprising determining the level of expression of a protein in stromal cells adjacent to the neoplasm
CA2753285A1 (en) 2009-03-12 2010-09-16 Genentech, Inc. Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents for the treatment of hematopoietic malignancies
WO2010106135A1 (en) 2009-03-20 2010-09-23 Sigma-Tau Industrie Farmaceutiche Riunite S.P.A. Combined use for the treatment of ovarian carcinoma
TWI504598B (zh) 2009-03-20 2015-10-21 Onyx Therapeutics Inc 結晶性三肽環氧酮蛋白酶抑制劑
SI2411535T1 (sl) * 2009-03-24 2015-08-31 Janssen Pharmaceutica N.V. Biooznačevalci za ovrednotenje odziva periferne nevropatije na zdravljenje z inhibitorjem proteazoma
WO2010114768A1 (en) * 2009-03-30 2010-10-07 Cerulean Pharma Inc. Polymer-epothilone conjugates, particles, compositions, and related methods of use
WO2010114770A1 (en) * 2009-03-30 2010-10-07 Cerulean Pharma Inc. Polymer-agent conjugates, particles, compositions, and related methods of use
EP2413901A4 (en) * 2009-03-30 2015-05-06 Cerulean Pharma Inc POLYMER CONCRETE CONJUGATES, PARTICLES, COMPOSITIONS AND CORRESPONDING USES
MX2011012538A (es) * 2009-05-27 2012-02-08 Cephalon Inc Terapia de combinacion para el tratamiento del mieloma multiple.
US8785674B2 (en) 2009-06-19 2014-07-22 Lek Pharmaceuticals D.D. Process for hydrogenation of halogenoalkenes without dehalogenation
EP2270019A1 (en) 2009-06-19 2011-01-05 LEK Pharmaceuticals d.d. New synthetic route for the preparation of alpha-amino boronic esters
CN101928329B (zh) * 2009-06-19 2013-07-17 北京大学 三肽硼酸(酯)类化合物、其制备方法和应用
EP2280016A1 (en) 2009-07-27 2011-02-02 LEK Pharmaceuticals d.d. New synthetic route for the preparation of alpha-amino boronic esters via substituted alk-1-ynes
US8293753B2 (en) 2009-07-02 2012-10-23 Novartis Ag Substituted 2-carboxamide cycloamino ureas
DE102009027754A1 (de) 2009-07-15 2011-05-05 Schubert, Ulrich, Dr. Verfahren zur Hemmung der Reifung von dendritischen Zellen
KR101785626B1 (ko) * 2009-07-20 2017-10-16 얀센 바이오테크 인코포레이티드 인간 배아 줄기 세포의 분화
KR101786735B1 (ko) 2009-07-20 2017-10-18 얀센 바이오테크 인코포레이티드 인간 배아 줄기 세포의 분화
EP2456862A4 (en) 2009-07-20 2013-02-27 Janssen Biotech Inc DIFFERENTIATION OF HUMAN EMBRYONIC STEM CELLS
JP2013500974A (ja) * 2009-07-28 2013-01-10 アナコール ファーマシューティカルズ，インコーポレイテッド 三置換ホウ素含有分子
AP4039A (en) 2009-08-14 2017-02-28 Daitao Chen Boron-containing small molecules as antiprotozoal agents
WO2011022502A1 (en) 2009-08-18 2011-02-24 Georgetown University Boronic acid compositions and methods related to cancer
MX2012002031A (es) * 2009-08-19 2012-07-04 Anacor Pharmaceuticals Inc Moleculas pequeñas que contienen boro como agentes antiprotozoarios.
EP2475659B1 (en) 2009-09-08 2015-10-28 F.Hoffmann-La Roche Ag 4-substituted pyridin-3-yl-carboxamide compounds and methods of use
WO2011037731A1 (en) * 2009-09-25 2011-03-31 Anacor Pharmaceuticals, Inc. Boron containing small molecules
EP2305285A1 (en) 2009-09-29 2011-04-06 Julius-Maximilians-Universität Würzburg Means and methods for treating ischemic conditions
DK2519231T3 (en) * 2009-10-01 2017-06-26 Janssen Pharmaceutica Nv Proteasome inhibitors for the treatment of cancer
WO2011049971A1 (en) 2009-10-20 2011-04-28 Anacor Pharmaceuticals, Inc. Boron-containing small molecules as antiprotozoal agents
WO2011060196A1 (en) * 2009-11-11 2011-05-19 Anacor Pharmaceuticals, Inc. Boron-containing small molecules
US8853147B2 (en) 2009-11-13 2014-10-07 Onyx Therapeutics, Inc. Use of peptide epoxyketones for metastasis suppression
CN102725300B (zh) 2009-12-22 2015-03-11 赛福伦公司 蛋白酶体抑制剂及其制备、纯化、和应用的方法
BR112012017761A2 (pt) 2009-12-23 2015-09-15 Centocor Ortho Biotech Inc diferenciação das células-tronco embrionárias humanas
PH12012501254A1 (en) 2009-12-23 2012-11-05 Janssen Biotech Inc Differentiation of human embryonic stem cells
WO2011090940A1 (en) 2010-01-19 2011-07-28 Cerulean Pharma Inc. Cyclodextrin-based polymers for therapeutic delivery
WO2011094450A1 (en) 2010-01-27 2011-08-04 Anacor Pharmaceuticals, Inc Boron-containing small molecules
US9359398B2 (en) 2010-03-01 2016-06-07 Onyx Therapeutics, Inc. Compounds for immunoproteasome inhibition
US9969981B2 (en) * 2010-03-01 2018-05-15 Janssen Biotech, Inc. Methods for purifying cells derived from pluripotent stem cells
US8263578B2 (en) 2010-03-18 2012-09-11 Innopharma, Inc. Stable bortezomib formulations
RU2529800C2 (ru) * 2010-03-18 2014-09-27 ИННОФАРМА, Инк. Стабильные составы бортезомиба
AP2012006482A0 (en) 2010-03-19 2012-10-31 Anacor Pharmacueticals Inc Boron-containing small molecules as anti-protozoalagent
CA2793959C (en) 2010-03-25 2019-06-04 Oregon Health & Science University Cmv glycoproteins and recombinant vectors
AU2013204868B2 (en) * 2010-03-31 2016-10-13 Millennium Pharmaceuticals, Inc. Derivatives of 1-amino-2-cyclopropylethylboronic acid
CN106008570A (zh) * 2010-03-31 2016-10-12 米伦纽姆医药公司 1-氨基-2-环丙基乙硼酸衍生物
WO2011136905A2 (en) 2010-04-07 2011-11-03 Onyx Therapeutics, Inc. Crystalline peptide epoxyketone immunoproteasome inhibitor
CN101812026B (zh) * 2010-04-12 2013-08-28 亚邦医药股份有限公司 一种硼替佐米的合成方法
CN102946879B (zh) 2010-04-19 2015-04-22 尼基制药公司 一种蛋白酶体抑制剂和镓络合物在制备治疗增殖性疾病的药物中的应用
US8809282B2 (en) 2010-05-06 2014-08-19 Duke University Method of reducing titers of antibodies specific for a therapeutic agent
RU2663339C1 (ru) 2010-05-12 2018-08-03 Янссен Байотек, Инк. Дифференцирование эмбриональных стволовых клеток человека
WO2011146638A1 (en) 2010-05-18 2011-11-24 Cerulean Pharma Inc. Compositions and methods for treatment of autoimmune and other diseases
AR082418A1 (es) 2010-08-02 2012-12-05 Novartis Ag Formas cristalinas de 1-(4-metil-5-[2-(2,2,2-trifluoro-1,1-dimetil-etil)-piridin-4-il]-tiazol-2-il)-amida de 2-amida del acido (s)-pirrolidin-1,2-dicarboxilico
JP6133776B2 (ja) 2010-08-31 2017-05-24 ヤンセン バイオテツク，インコーポレーテツド 多能性幹細胞の分化
KR101836850B1 (ko) 2010-08-31 2018-03-09 얀센 바이오테크 인코포레이티드 인간 배아 줄기 세포의 분화
CA2809300A1 (en) 2010-08-31 2012-03-08 Janssen Biotech, Inc. Differentiation of human embryonic stem cells
US9126997B1 (en) 2010-09-07 2015-09-08 Northwestern University Synergistic effect of glucocorticoid receptor agonists in combination with proteosome inhibitors for treating leukemia and myeloma
MX338209B (es) 2010-09-07 2016-04-07 Anacor Pharmaceuticals Inc Derivados de benzoxaborol para tratar infecciones bacterianas.
US8962572B2 (en) 2010-10-05 2015-02-24 Fresenius Kabi Usa, Llc Bortezomib formulations
WO2012048745A1 (en) 2010-10-14 2012-04-19 Synthon Bv Process for making bortezomib and intermediates for the process
TW201309700A (zh) 2011-01-31 2013-03-01 Novartis Ag 新穎雜環衍生物
TW201309303A (zh) * 2011-03-03 2013-03-01 Cephalon Inc 用於治療狼瘡的蛋白酶體抑制劑
WO2012135528A2 (en) 2011-03-29 2012-10-04 Texas Tech University System Galectin-3c combination therapy for human cancer
CN103502319B (zh) 2011-03-31 2015-11-25 那野伽利阿株式会社 包含含有硼酸化合物的嵌段共聚物的医药组合物
PT2691530T (pt) 2011-06-10 2018-05-10 Univ Oregon Health & Science Glicoproteínas e vectores recombinantes cmv
MX2013015308A (es) * 2011-06-22 2014-05-20 Cephalon Inc Inhibidores de proteasoma y procesos para su preparacion, purificacion y uso.
US8481655B2 (en) 2011-07-27 2013-07-09 Wacker Chemical Corporation Copper complexes of amino-functional organosilicon compounds and their use
SI2742356T1 (sl) 2011-08-11 2016-06-30 Janssen Pharmaceutica N.V. Prediktorji pri zdravljenju raka
WO2013021032A1 (en) 2011-08-11 2013-02-14 Janssen Pharmaceutica Nv Histone deacetylase inhibitors in combination with proteasome inhibitors and dexamethasone
JP6367712B2 (ja) 2011-08-19 2018-08-01 グラクソ グループ リミテッドＧｌａｘｏ Ｇｒｏｕｐ Ｌｉｍｉｔｅｄ Ｃ型肝炎ウイルス感染の治療のためのベンゾフラン化合物
HUE060305T2 (hu) 2011-08-30 2023-02-28 Tufts College FAP-aktivált proteaszóma inhibitorok a szolid tumorok kezelésére
EP2568289A3 (en) 2011-09-12 2013-04-03 International AIDS Vaccine Initiative Immunoselection of recombinant vesicular stomatitis virus expressing hiv-1 proteins by broadly neutralizing antibodies
EP2586461A1 (en) 2011-10-27 2013-05-01 Christopher L. Parks Viral particles derived from an enveloped virus
CA2853822A1 (en) 2011-10-28 2013-05-02 Millennium Pharmaceuticals, Inc. Biomarkers of response to nae inhibitors
WO2013061305A1 (en) 2011-10-28 2013-05-02 Novartis Ag Novel purine derivatives and their use in the treatment of disease
US20150184246A1 (en) 2011-11-11 2015-07-02 Millennium Pharmaceuticals, Inc. Biomarkers of response to proteasome inhibitors
JP6397765B2 (ja) 2011-11-11 2018-09-26 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． プロテアソーム阻害剤に応答するバイオマーカー
ES2603632T3 (es) 2011-11-17 2017-02-28 The University Of Tokyo Copolímero en bloque que tiene un grupo ácido fenilborónico introducido en el mismo, y usos del mismo
AU2012355698B2 (en) 2011-12-22 2018-11-29 Janssen Biotech, Inc. Differentiation of human embryonic stem cells into single hormonal insulin positive cells
US9732101B2 (en) 2012-01-18 2017-08-15 Wisconsin Alumni Research Foundation Bioreversible boronates for delivery of molecules into cells
US9234048B2 (en) 2012-01-18 2016-01-12 Wisconsin Alumni Research Foundation Boronate-mediated delivery of molecules into cells
CA2862492A1 (en) 2012-01-24 2013-08-01 Millennium Pharmaceuticals, Inc. Methods of treatment of cancer
US10085987B2 (en) 2012-01-27 2018-10-02 Thomas Jefferson University MCT protein inhibitor-related prognostic and therapeutic methods
MX363819B (es) 2012-02-08 2019-04-03 Igm Biosciences Inc Uniones a cdim y sus usos.
AU2013227219A1 (en) 2012-03-02 2014-10-23 Dr. Reddy's Laboratories Limited Pharmaceutical compositions comprising boronic acid compounds
RU2018128383A (ru) 2012-03-07 2019-03-14 Янссен Байотек, Инк. Среда определенного состава для размножения и обновления плюрипотентных стволовых клеток
CA2784240C (en) 2012-03-27 2014-07-08 Innopharma, Inc. Stable bortezomib formulations
EP2849756A1 (en) 2012-05-16 2015-03-25 Novartis AG Dosage regimen for a pi-3 kinase inhibitor
RU2018108850A (ru) 2012-06-08 2019-02-26 Янссен Байотек, Инк. Дифференцировка эмбриональных стволовых клеток человека в панкреатические эндокринные клетки
ES2631608T3 (es) 2012-06-27 2017-09-01 International Aids Vaccine Initiative Variante de la glicoproteína Env del VIH-1
US9309283B2 (en) 2012-07-09 2016-04-12 Onyx Therapeutics, Inc. Prodrugs of peptide epoxy ketone protease inhibitors
JP2013006855A (ja) * 2012-09-03 2013-01-10 Millennium Pharmaceuticals Inc プロテアソーム阻害剤
BR112015005343A2 (pt) * 2012-09-11 2017-07-04 Cipla Ltd processo para a preparação de bortezomib, composto, bortezomib ou seu anidrido, e, processo para a preparação de um composto
CA2886783A1 (en) 2012-10-01 2014-04-10 Millennium Pharmaceuticals, Inc. Biomarkers and methods to predict response to inhibitors and uses thereof
WO2014072985A1 (en) 2012-11-06 2014-05-15 Natco Pharma Limited Novel boronic acid derivatives as anti cancer agents
JP2015536342A (ja) 2012-11-16 2015-12-21 シルパ・メディケア・リミテッドＳｈｉｌｐａ Ｍｅｄｉｃａｒｅ Ｌｉｍｉｔｅｄ 結晶ボルテゾミブの方法
WO2014097306A1 (en) 2012-12-21 2014-06-26 Natco Pharma Limited Stable and pure polymorphic form of bortezomib
EP4039798A1 (en) 2012-12-31 2022-08-10 Janssen Biotech, Inc. Suspension and clustering of human pluripotent cells
US10370644B2 (en) 2012-12-31 2019-08-06 Janssen Biotech, Inc. Method for making human pluripotent suspension cultures and cells derived therefrom
SG10201707811XA (en) 2012-12-31 2017-11-29 Janssen Biotech Inc Differentiation of human embryonic stem cells into pancreatic endocrine cells using hb9 regulators
MX2015008577A (es) 2012-12-31 2015-09-07 Janssen Biotech Inc Cultivo de celulas madre embrionarias humanas en la interfase aire-liquido para la diferenciacion en celulas endocrinas pancreaticas.
KR102194745B1 (ko) 2013-03-13 2020-12-24 포르마 세라퓨틱스 인크. Ｆａｓｎ 억제용 신규 화합물 및 조성물
EP2986619A1 (en) 2013-04-16 2016-02-24 Cipla Limited Process for the preparation of bortezomib mannitol ester
EP2986290A4 (en) 2013-04-19 2017-01-04 Thomas Jefferson University Caveolin-1 related methods for treating glioblastoma with temozolomide
US9603775B2 (en) 2013-04-24 2017-03-28 Corning Incorporated Delamination resistant pharmaceutical glass containers containing active pharmaceutical ingredients
WO2015003146A1 (en) 2013-07-03 2015-01-08 Georgetown University Boronic acid derivatives of resveratrol for activating deacetylase enzymes
US20150065381A1 (en) 2013-09-05 2015-03-05 International Aids Vaccine Initiative Methods of identifying novel hiv-1 immunogens
KR20160058886A (ko) 2013-10-03 2016-05-25 밀레니엄 파머슈티컬스 인코퍼레이티드 전신 홍반성 낭창 및/또는 낭창성 신염의 예방 또는 치료 방법
EP2873423B1 (en) 2013-10-07 2017-05-31 International Aids Vaccine Initiative Soluble hiv-1 envelope glycoprotein trimers
CN104586776B (zh) * 2013-10-30 2017-05-17 扬子江药业集团上海海尼药业有限公司 以硼替佐米为活性成分的制剂及其制备方法
WO2015076359A1 (ja) * 2013-11-21 2015-05-28 国立大学法人北海道大学 プロテアソーム阻害性化合物
US10191033B2 (en) 2013-12-05 2019-01-29 The Broad Institute, Inc. Biomarkers for detecting pre-cachexia or cachexia and methods of treatment thereof
CA2930359C (en) 2013-12-06 2022-03-01 Novartis Ag Dosage regimen for an alpha-isoform selective phosphatidylinositol 3-kinase inhibitor
EP3102585B1 (en) 2014-02-03 2021-05-19 Ohio State Innovation Foundation Boronic acid esters and pharmaceutical formulations thereof
EP2910557A1 (en) * 2014-02-20 2015-08-26 Ikerchem, S.L. Enantiopure tetrasubstituted pyrrolidines as scaffolds for proteasome inhibitors and medicinal applications thereof
JP6566936B2 (ja) 2014-05-08 2019-08-28 国立大学法人 東京大学 医薬組成物
KR102162138B1 (ko) 2014-05-16 2020-10-06 얀센 바이오테크 인코포레이티드 췌장 내분비 세포에서 mafa 발현을 향상시키기 위한 소분자의 용도
CN106659761A (zh) 2014-05-20 2017-05-10 千年药物公司 初级癌症疗法后使用的含硼蛋白酶体抑制剂
EP3808349B1 (en) 2014-08-07 2022-10-05 Mayo Foundation for Medical Education and Research Compounds and methods for treating cancer
CA2963198A1 (en) * 2014-10-01 2016-04-07 Merck Patent Gmbh Boronic acid derivatives
WO2016110870A1 (en) 2015-01-07 2016-07-14 Emcure Pharmaceuticals Limited Pharmaceutical composition of bortezomid
MA41505A (fr) 2015-02-11 2017-12-19 Millennium Pharm Inc Nouvelle forme cristalline d'un inhibiteur de protéasome
US20180243217A1 (en) 2015-03-17 2018-08-30 Leon-Nanodrugs Gmbh Nanoparticles comprising a stabilized boronic acid compound
US10174292B2 (en) 2015-03-20 2019-01-08 International Aids Vaccine Initiative Soluble HIV-1 envelope glycoprotein trimers
US9931394B2 (en) 2015-03-23 2018-04-03 International Aids Vaccine Initiative Soluble HIV-1 envelope glycoprotein trimers
WO2016184793A1 (en) 2015-05-15 2016-11-24 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for treating a patient with vegfr inhibitor-resistant metastatic renal cell carcinoma
US10144761B2 (en) 2015-06-19 2018-12-04 Hanlin Scientific Inc. Chiral specific boron-containing compounds and their use in treating cancer or amyloidosis
EP3120836A1 (de) 2015-07-22 2017-01-25 Stada Arzneimittel Ag Gebrauchsfertige bortezomib-lösung
EP3120837A1 (de) 2015-07-22 2017-01-25 Stada Arzneimittel Ag Verfahren zur herstellung einer bortezomibester-lösung
CN106478700B (zh) * 2015-08-26 2020-12-29 杭州雷索药业有限公司 硼基取代的苯胺类蛋白激酶抑制剂
CN106588965A (zh) * 2015-10-15 2017-04-26 北京大学 脲拟肽硼酸化合物及其药物组合物、制备方法和用途
CN108472289A (zh) 2015-11-02 2018-08-31 诺华股份有限公司 磷脂酰肌醇3-激酶抑制剂的给药方案
WO2017106196A1 (en) 2015-12-14 2017-06-22 The Broad Institute, Inc. Compositions and methods for treating cardiac dysfunction
CN107151255A (zh) * 2016-03-06 2017-09-12 复旦大学 硼酸类化合物及其制备方法和用途
CN107151254A (zh) * 2016-03-06 2017-09-12 复旦大学 一种作为20s蛋白酶体抑制剂的硼酸类化合物及其制备方法
MA45479A (fr) 2016-04-14 2019-02-20 Janssen Biotech Inc Différenciation de cellules souches pluripotentes en cellules de l'endoderme de l'intestin moyen
US11447506B2 (en) 2016-05-09 2022-09-20 Anacor Pharmaceuticals, Inc. Crystal forms of crisaborole in free form and preparation method and use thereof
CN106008572B (zh) * 2016-05-23 2018-08-17 成都千禧莱医药科技有限公司 一类二肽硼酸化合物及制备方法和用途
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
MX392422B (es) 2016-06-21 2025-03-24 Orion Ophthalmology LLC Derivados de prolinamida heterociclica
JP6681284B2 (ja) * 2016-06-23 2020-04-15 信越化学工業株式会社 糖アルコール化合物の金属低減方法
JP6223508B2 (ja) * 2016-06-27 2017-11-01 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
WO2018038687A1 (en) 2016-08-22 2018-03-01 Mustafa Nevzat Ilaç Sanayii A.Ş. Pharmaceutical formulations comprising a bortezomib-cyclodextrin complex
WO2018060833A1 (en) 2016-09-27 2018-04-05 Novartis Ag Dosage regimen for alpha-isoform selective phosphatidylinositol 3-kinase inhibitor alpelisib
CA3040820A1 (en) 2016-10-20 2018-04-26 Pfizer Inc. Therapeutic particles with peptide boronic acid or boronate ester compounds and methods of making and using same
US11584733B2 (en) 2017-01-09 2023-02-21 Shuttle Pharmaceuticals, Inc. Selective histone deacetylase inhibitors for the treatment of human disease
US11034667B2 (en) 2017-01-09 2021-06-15 Shuttle Pharmaceuticals, Inc. Selective histone deacetylase inhibitors for the treatment of human disease
US11667654B2 (en) 2017-02-17 2023-06-06 Fresenius Kabi Oncology Ltd. Process for the preparation of boronic acid esters
ES3036483T3 (en) 2017-02-28 2025-09-19 Mayo Found Medical Education & Res Combinations for use in the treatment of cancer
EP3672586A1 (en) 2017-08-23 2020-07-01 Kezar Life Sciences Immunoproteasome inhibitors and immunosuppressive agent in the treatment of autoimmune disorders
WO2019053611A1 (en) 2017-09-14 2019-03-21 Glaxosmithkline Intellectual Property Development Limited POLY THERAPY FOR THE TREATMENT OF CANCER
JP2018024694A (ja) * 2017-10-03 2018-02-15 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
EA202090900A1 (ru) 2017-11-16 2020-10-02 Принсипиа Биофарма Инк. Ингибиторы иммунопротеасом
LT3710457T (lt) * 2017-11-16 2022-11-10 Principia Biopharma Inc. Imunoproteasomos inhibitoriai
US10537585B2 (en) 2017-12-18 2020-01-21 Dexcel Pharma Technologies Ltd. Compositions comprising dexamethasone
CN112004537A (zh) 2018-01-09 2020-11-27 穿梭药业公司 用于治疗人疾病的选择性组蛋白去乙酰化酶抑制剂
JP2021512165A (ja) 2018-01-29 2021-05-13 コグノス・セラピューティクス・インコーポレイテッド ボルテゾミブの腫瘍内送達
TW202003553A (zh) 2018-03-15 2020-01-16 美商艾伯維有限公司 用於治療癌症之abbv-621與抗癌劑之組合
US11243207B2 (en) 2018-03-29 2022-02-08 Mayo Foundation For Medical Education And Research Assessing and treating cancer
EP3873214A4 (en) 2018-10-29 2022-07-13 Forma Therapeutics, Inc. Solid forms of (4-(2-fluoro-4-(1-methyl-1 h-benzo[d]imidazol-5-yl)benzoyl) piperazin-1-yl)(1-hydroxycyclopropyl)methanone
CN109824756B (zh) * 2019-03-19 2022-03-22 山东大学 含有4-(苯磺酰基)哌嗪-2-酮的苯丙氨酸衍生物及其制备方法与应用
JP2020079299A (ja) * 2020-02-18 2020-05-28 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
CN114437119B (zh) * 2020-10-30 2024-08-09 苏州开拓药业股份有限公司 一种c-Myc蛋白抑制剂及其制备方法和用途
JP2023553011A (ja) * 2020-12-02 2023-12-20 ホフマン・テクノロジーズ・エルエルシー 非ヒト哺乳動物においてがんを調節するための組成物および方法
KR102825542B1 (ko) * 2020-12-10 2025-06-26 주식회사 엘지화학 보론산 화합물
US11964993B2 (en) 2021-07-03 2024-04-23 Shilpa Pharma Lifesciences Limited Crystalline bortezomib process
US20230062279A1 (en) 2021-08-12 2023-03-02 Extrovis Ag Pharmaceutical compositions of bortezomib
CN113957441B (zh) * 2021-10-29 2024-01-02 光华科学技术研究院(广东)有限公司 蚀刻液及其制备方法和应用
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
WO2024097905A1 (en) 2022-11-02 2024-05-10 Celgene Corporation Methods of treatment with t cell therapy and immunomodulatory agent maintenance therapy

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4499082A (en) * 1983-12-05 1985-02-12 E. I. Du Pont De Nemours And Company α-Aminoboronic acid peptides
US5106948A (en) * 1988-05-27 1992-04-21 Mao Foundation For Medical Education And Research Cytotoxic boronic acid peptide analogs
US5169841A (en) * 1987-11-05 1992-12-08 Hoechst Aktiengesellschaft Renin inhibitors

Family Cites Families (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4261868A (en) * 1979-08-08 1981-04-14 Lever Brothers Company Stabilized enzymatic liquid detergent composition containing a polyalkanolamine and a boron compound
US4369183A (en) * 1979-09-06 1983-01-18 Merck & Co., Inc. 2-Pyridyl-1,2-benzisothiazolinone-1,1-dioxides and their use as selective protease inhibitors
US4510130A (en) 1983-05-20 1985-04-09 Genetic Diagnostics Corporation Promoting animal and plant growth with leupeptin
US4537773A (en) 1983-12-05 1985-08-27 E. I. Du Pont De Nemours And Company α-Aminoboronic acid derivatives
US4537707A (en) * 1984-05-14 1985-08-27 The Procter & Gamble Company Liquid detergents containing boric acid and formate to stabilize enzymes
US4842769A (en) * 1985-07-26 1989-06-27 Colgate-Palmolive Co. Stabilized fabric softening built detergent composition containing enzymes
US4759032A (en) 1987-06-03 1988-07-19 Monsanto Company Electrode seal assembly
US5250720A (en) * 1987-06-05 1993-10-05 The Dupont Merck Pharmaceutical Company Intermediates for preparing 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
US5242904A (en) * 1987-06-05 1993-09-07 The Dupont Merck Pharmaceutical Company Peptide boronic acid inhibitors of trypsin-like proteases
SE8702550D0 (sv) * 1987-06-18 1987-06-18 Anders Grubb Cysteinproteashemmare
KR960012512B1 (ko) 1987-06-19 1996-09-20 캔디스 엘. 볼커 신규한 종류의 저칼로리 단백질 감미제
US4963655A (en) * 1988-05-27 1990-10-16 Mayo Foundation For Medical Education And Research Boron analogs of amino acid/peptide protease inhibitors
DE3827340A1 (de) * 1988-08-12 1990-02-15 Hoechst Ag Verwendung von (alpha)-aminoboronsaeure-derivaten zur prophylaxe und behandlung von viruserkrankungen
ZA897514B (en) * 1988-10-07 1990-06-27 Merrell Dow Pharma Novel peptidase inhibitors
US4997929A (en) * 1989-01-05 1991-03-05 Synergen, Inc. Purified ciliary neurotrophic factor
US4959179A (en) * 1989-01-30 1990-09-25 Lever Brothers Company Stabilized enzymes liquid detergent composition containing lipase and protease
JP2701932B2 (ja) * 1989-04-10 1998-01-21 サントリー株式会社 タンパク質分解酵素阻害剤
US5030378A (en) * 1990-01-02 1991-07-09 The Procter & Gamble Company Liquid detergents containing anionic surfactant, builder and proteolytic enzyme
CA2077665A1 (en) 1990-03-05 1991-09-06 Robert Siman Chymotrypsin-like proteases and their inhibitors
GB9017694D0 (en) * 1990-08-13 1990-09-26 Sandoz Ltd Improvements in or relating to organic chemistry
EP0478050A1 (en) * 1990-09-24 1992-04-01 Unilever N.V. Detergent composition
GB9024129D0 (en) * 1990-11-06 1990-12-19 Thrombosis Research Trust Inhibitors and substrates of thrombin
JP2703408B2 (ja) 1990-12-28 1998-01-26 麒麟麦酒株式会社 １，４‐ベンゾチアゼピン誘導体
AU667463B2 (en) * 1990-12-28 1996-03-28 Cortex Pharmaceuticals, Inc. Use of calpain inhibitors in the inhibition and treatment of neurodegeneration
JPH06504547A (ja) * 1990-12-28 1994-05-26 ジョージア・テック・リサーチ・コーポレーション ペプチドケトアミド、ケト酸およびケトエステル
EP0511456A1 (en) * 1991-04-30 1992-11-04 The Procter & Gamble Company Liquid detergents with aromatic borate ester to inhibit proteolytic enzyme
HUT65823A (en) * 1991-04-30 1994-07-28 Procter & Gamble Liquid detergents with an aryl boronic acid and process for using thereof
SK120893A3 (en) * 1991-04-30 1994-08-10 Procter & Gamble Liquid detergent mixtures with boric-polyol complex for inhibition of proteolytic enzyme
US5554728A (en) * 1991-07-23 1996-09-10 Nexstar Pharmaceuticals, Inc. Lipid conjugates of therapeutic peptides and protease inhibitors
CA2133658A1 (en) * 1992-04-16 1993-10-28 Peter R. Bernstein Heterocyclic derivatives
CA2133657A1 (en) * 1992-04-16 1993-10-28 Peter R. Bernstein Substituted derivatives
ATE149563T1 (de) * 1992-08-14 1997-03-15 Procter & Gamble Alpha-aminoborsäurehaltige flüssige waschmittel
WO1994017816A1 (en) 1993-02-10 1994-08-18 The President And Fellows Of Harvard College Role of atp-ubiquitin-dependent proteolysis in mhc-1 restricted antigen presentation and inhibitors thereof
US5384410A (en) * 1993-03-24 1995-01-24 The Du Pont Merck Pharmaceutical Company Removal of boronic acid protecting groups by transesterification
DE4311835A1 (de) * 1993-04-07 1994-10-13 Boehringer Ingelheim Int Verfahren zur Inhibierung der Transkription von Genen
US5424904A (en) * 1993-10-04 1995-06-13 Taylor, Sr.; Thomas T. Circuit for electrically controlled intermittent motion
IL111176A0 (en) * 1993-10-07 1994-12-29 Du Pont Merck Pharma Dipeptide boronic acid inhibitors of trypsin-like enzymes and pharmaceutical compositions containing them
US5693617A (en) * 1994-03-15 1997-12-02 Proscript, Inc. Inhibitors of the 26s proteolytic complex and the 20s proteasome contained therein
US6660268B1 (en) * 1994-03-18 2003-12-09 The President And Fellows Of Harvard College Proteasome regulation of NF-KB activity
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
US5550262A (en) * 1994-11-14 1996-08-27 Cephalon, Inc. Multicatalytic protease inhibitors
EP2251344B2 (en) * 2001-01-25 2024-04-24 THE UNITED STATES OF AMERICA, represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES Formulation of boronic acid compounds
PL4008721T3 (pl) 2004-03-30 2024-05-13 Millennium Pharmaceuticals, Inc. Synteza związków estrów i kwasów boronowych

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4499082A (en) * 1983-12-05 1985-02-12 E. I. Du Pont De Nemours And Company α-Aminoboronic acid peptides
US5169841A (en) * 1987-11-05 1992-12-08 Hoechst Aktiengesellschaft Renin inhibitors
US5106948A (en) * 1988-05-27 1992-04-21 Mao Foundation For Medical Education And Research Cytotoxic boronic acid peptide analogs

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AU710564C (en) 1996-05-23
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US20040167332A1 (en) 2004-08-26
US20110306560A1 (en) 2011-12-15
US6617317B1 (en) 2003-09-09
NO310558B1 (no) 2001-07-23
NO971929L (no) 1997-06-12
US20030199561A1 (en) 2003-10-23
CA2203936A1 (en) 1996-05-09
US20070282100A1 (en) 2007-12-06
US7119080B2 (en) 2006-10-10
US6747150B2 (en) 2004-06-08
US6066730A (en) 2000-05-23
ATE411324T1 (de) 2008-10-15
DE122004000025I2 (de) 2006-09-07
US5780454A (en) 1998-07-14
PT1312609E (pt) 2006-05-31
JP3717934B2 (ja) 2005-11-16
DE69530936T3 (de) 2010-08-26
ES2199257T7 (es) 2010-03-31
DE69534727T2 (de) 2006-09-14
IL137726A0 (en) 2001-10-31
NZ337211A (en) 2000-12-22
FI971746A0 (fi) 1997-04-23
NZ296717A (en) 1999-11-29
CA2496538A1 (en) 1996-05-09
CA2203936C (en) 2005-04-12
NL300151I2 (nl) 2004-09-01
CN1305475C (zh) 2007-03-21
EP0788360B3 (en) 2009-08-12
EP1627880B1 (en) 2008-10-15
NL300151I1 (nl) 2004-08-02
NO2004004I2 (no) 2007-09-10
IL115790A0 (en) 1996-01-19
DE69530936D1 (de) 2003-07-03
FR04C0014I1 (enExample) 2004-09-17
ATE241631T1 (de) 2003-06-15
NO971929D0 (no) 1997-04-25
US8003791B2 (en) 2011-08-23

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