CN100415770C - 2－{[n－(2－氨基－3－(杂芳基或芳基)丙酰基)－氨基酰基]－氨基}－烷基硼酸衍生物 - Google Patents

2－{[n－(2－氨基－3－(杂芳基或芳基)丙酰基)－氨基酰基]－氨基}－烷基硼酸衍生物 Download PDF

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Publication number
CN100415770C
CN100415770C CNB028108132A CN02810813A CN100415770C CN 100415770 C CN100415770 C CN 100415770C CN B028108132 A CNB028108132 A CN B028108132A CN 02810813 A CN02810813 A CN 02810813A CN 100415770 C CN100415770 C CN 100415770C
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CN
China
Prior art keywords
phenyl
amino
methyl
butyl
group
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
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CNB028108132A
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English (en)
Chinese (zh)
Other versions
CN1512999A (zh
Inventor
P·菲雷
V·瓜尼亚诺
P·因巴赫
M·兰
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Novartis AG
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Novartis AG
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Publication date
Priority claimed from GB0113096A external-priority patent/GB0113096D0/en
Priority claimed from GB0129394A external-priority patent/GB0129394D0/en
Application filed by Novartis AG filed Critical Novartis AG
Publication of CN1512999A publication Critical patent/CN1512999A/zh
Application granted granted Critical
Publication of CN100415770C publication Critical patent/CN100415770C/zh
Anticipated expiration legal-status Critical
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    • 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
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Molecular Biology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CNB028108132A 2001-05-30 2002-05-29 2－{[n－(2－氨基－3－(杂芳基或芳基)丙酰基)－氨基酰基]－氨基}－烷基硼酸衍生物 Expired - Fee Related CN100415770C (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB0113096.2 2001-05-30
GB0113096A GB0113096D0 (en) 2001-05-30 2001-05-30 Organic compounds
GB0129394A GB0129394D0 (en) 2001-12-07 2001-12-07 Organic compounds
GB0129394.3 2001-12-07

Publications (2)

Publication Number Publication Date
CN1512999A CN1512999A (zh) 2004-07-14
CN100415770C true CN100415770C (zh) 2008-09-03

Family

ID=26246132

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB028108132A Expired - Fee Related CN100415770C (zh) 2001-05-30 2002-05-29 2－{[n－(2－氨基－3－(杂芳基或芳基)丙酰基)－氨基酰基]－氨基}－烷基硼酸衍生物

Country Status (11)

Country Link
US (2) US6933290B2 (https=)
EP (1) EP1399468B1 (https=)
JP (1) JP4416501B2 (https=)
CN (1) CN100415770C (https=)
AT (1) ATE317850T1 (https=)
BR (1) BR0210112A (https=)
CA (1) CA2446282A1 (https=)
DE (1) DE60209227T2 (https=)
ES (1) ES2258149T3 (https=)
PT (1) PT1399468E (https=)
WO (1) WO2002096933A1 (https=)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002096933A1 (en) * 2001-05-30 2002-12-05 Novartis Ag 2-{[n-(2-amino-3-(heteroaryl or aryl)propionyl)-aminoacyl]-amino}-alkylboronic acid derivatives
AU2003219652A1 (en) * 2002-01-08 2003-07-30 Eisai Co. Ltd. Eponemycin and epoxomicin analogs and uses thereof
WO2004043926A1 (en) * 2002-11-11 2004-05-27 Bayer Healthcare Ag Phenyl or heteroaryl amino alkane derivatives as ip receptor antagonist
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
US7468383B2 (en) 2005-02-11 2008-12-23 Cephalon, Inc. Proteasome inhibitors and methods of using the same
JP5321061B2 (ja) 2005-08-11 2013-10-23 アリアド・ファーマシューティカルズ・インコーポレイテッド 不飽和複素環誘導体
WO2007059106A2 (en) 2005-11-14 2007-05-24 Ariad Gene Therapeutics, Inc. Administration of mntor inhibitor to treat patients with cancer
EA034598B1 (ru) 2005-12-23 2020-02-25 Ариад Фармасьютикалз, Инк. Применение бициклических гетероарильных соединений для лечения рака
PL2178888T3 (pl) 2007-08-06 2012-11-30 Millennium Pharm Inc Inhibitory proteasomów
MX353308B (es) 2008-05-21 2018-01-08 Ariad Pharma Inc Derivados fosforosos como inhibidores de cinasa.
EP2730579A1 (en) 2008-06-17 2014-05-14 Millennium Pharmaceuticals, Inc. Boronate ester compounds and pharmaceutical compositions thereof
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.
CA2743449C (en) 2008-11-12 2016-10-18 Ariad Pharmaceuticals, Inc. Pyrazinopyrazines and derivatives as kinase inhibitors
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
AU2010341530B2 (en) 2009-12-22 2016-03-10 Cephalon, Inc. Proteasome inhibitors and processes for their preparation, purification and use
EP2542238B1 (en) * 2010-03-01 2015-08-12 Onyx Therapeutics, Inc. Compounds for immunoproteasome inhibition
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
WO2013112881A1 (en) 2012-01-27 2013-08-01 Thomas Jefferson University Mct protein inhibitor-related prognostic and therapeutic methods
CN103421032B (zh) * 2012-05-17 2016-01-20 上海创诺制药有限公司 一种硼替佐米中间体及其制备方法和应用
US10022372B2 (en) 2013-04-19 2018-07-17 Thomas Jefferson University Caveolin-1 related methods for treating glioblastoma with temozolomide
MA39964A (fr) 2014-05-20 2015-11-26 Millennium Pharm Inc Inhibiteurs du protéasome contenant du bore destinés à être utilisés après une thérapie contre le cancer primaire
EP3778584A1 (en) 2014-06-19 2021-02-17 ARIAD Pharmaceuticals, Inc. Production process of 2-chloro-4-heteroaryl-pyrimidine derivatives
MA41505A (fr) 2015-02-11 2017-12-19 Millennium Pharm Inc Nouvelle forme cristalline d'un inhibiteur de protéasome
PL3472149T3 (pl) 2016-06-21 2024-02-12 Orion Ophthalmology LLC Heterocykliczne pochodne prolinamidu
US10526315B2 (en) 2016-06-21 2020-01-07 Orion Ophthalmology LLC Carbocyclic prolinamide derivatives

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5106948A (en) * 1988-05-27 1992-04-21 Mao Foundation For Medical Education And Research Cytotoxic boronic acid peptide analogs
CN1121077A (zh) * 1994-06-22 1996-04-24 阿迪尔公司 衍生自二羟硼烷的新颖肽化合物，制备它们的方法以及含有这类化合物的药物组合物
US5780454A (en) * 1994-10-28 1998-07-14 Proscript, Inc. Boronic ester and acid compounds

Family Cites Families (10)

* 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
EP0315574A3 (de) 1987-11-05 1990-08-22 Hoechst Aktiengesellschaft Renin-Inhibitoren
GB9017694D0 (en) 1990-08-13 1990-09-26 Sandoz Ltd Improvements in or relating to organic chemistry
US5384410A (en) 1993-03-24 1995-01-24 The Du Pont Merck Pharmaceutical Company Removal of boronic acid protecting groups by transesterification
US5658885A (en) 1993-04-27 1997-08-19 The Dupont Merck Pharmaceutical Company Amidino and guanidino substituted boronic acid inhibitors of trypsin-like enzymes
IL109319A0 (en) 1993-04-27 1994-07-31 Du Pont Merck Pharma Amidino and guanidino substituted boronic acid compounds
US5550262A (en) 1994-11-14 1996-08-27 Cephalon, Inc. Multicatalytic protease inhibitors
US5614649A (en) 1994-11-14 1997-03-25 Cephalon, Inc. Multicatalytic protease inhibitors
CA2314259A1 (en) 1997-12-16 1999-06-24 Robert Siman Multicatalytic protease inhibitors for use as anti-tumor agents
WO2002096933A1 (en) * 2001-05-30 2002-12-05 Novartis Ag 2-{[n-(2-amino-3-(heteroaryl or aryl)propionyl)-aminoacyl]-amino}-alkylboronic acid derivatives

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5106948A (en) * 1988-05-27 1992-04-21 Mao Foundation For Medical Education And Research Cytotoxic boronic acid peptide analogs
CN1121077A (zh) * 1994-06-22 1996-04-24 阿迪尔公司 衍生自二羟硼烷的新颖肽化合物，制备它们的方法以及含有这类化合物的药物组合物
US5780454A (en) * 1994-10-28 1998-07-14 Proscript, Inc. Boronic ester and acid compounds

Also Published As

Publication number Publication date
PT1399468E (pt) 2006-05-31
US20040167337A1 (en) 2004-08-26
JP2005501005A (ja) 2005-01-13
EP1399468A1 (en) 2004-03-24
CN1512999A (zh) 2004-07-14
CA2446282A1 (en) 2002-12-05
US6933290B2 (en) 2005-08-23
DE60209227D1 (de) 2006-04-20
BR0210112A (pt) 2004-06-08
WO2002096933A1 (en) 2002-12-05
ES2258149T3 (es) 2006-08-16
JP4416501B2 (ja) 2010-02-17
EP1399468B1 (en) 2006-02-15
US20050239716A1 (en) 2005-10-27
ATE317850T1 (de) 2006-03-15
DE60209227T2 (de) 2006-08-17

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Granted publication date: 20080903

Termination date: 20110529