UA71559C2 - a-KETOAMIDES BEING 20S PROTEASOME INHIBITORS - Google Patents

a-KETOAMIDES BEING 20S PROTEASOME INHIBITORS Download PDF

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Publication number
UA71559C2
UA71559C2 UA2000074508A UA2000074508A UA71559C2 UA 71559 C2 UA71559 C2 UA 71559C2 UA 2000074508 A UA2000074508 A UA 2000074508A UA 2000074508 A UA2000074508 A UA 2000074508A UA 71559 C2 UA71559 C2 UA 71559C2
Authority
UA
Ukraine
Prior art keywords
substituted
phenyl
alkyl
group
chi
Prior art date
Application number
UA2000074508A
Other languages
English (en)
Ukrainian (uk)
Original Assignee
Cv Therapeutics 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 Cv Therapeutics Inc filed Critical Cv Therapeutics Inc
Publication of UA71559C2 publication Critical patent/UA71559C2/uk

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0205Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)3-C(=0)-, e.g. statine or derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043Leu-amino acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
UA2000074508A 1998-01-26 1999-01-19 a-KETOAMIDES BEING 20S PROTEASOME INHIBITORS UA71559C2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US09/013,365 US6075150A (en) 1998-01-26 1998-01-26 α-ketoamide inhibitors of 20S proteasome
PCT/US1999/001097 WO1999037666A1 (fr) 1998-01-26 1999-01-19 INHIBITEURS α-CETOAMIDE DE 20S PROTEASOME

Publications (1)

Publication Number Publication Date
UA71559C2 true UA71559C2 (en) 2004-12-15

Family

ID=21759598

Family Applications (1)

Application Number Title Priority Date Filing Date
UA2000074508A UA71559C2 (en) 1998-01-26 1999-01-19 a-KETOAMIDES BEING 20S PROTEASOME INHIBITORS

Country Status (20)

Country Link
US (2) US6075150A (fr)
EP (1) EP1058689A1 (fr)
JP (1) JP3863370B2 (fr)
KR (1) KR100417888B1 (fr)
CN (1) CN1289340A (fr)
AR (1) AR012781A1 (fr)
AU (1) AU747835B2 (fr)
BR (1) BR9907256A (fr)
CA (1) CA2319150C (fr)
GE (1) GEP20032869B (fr)
HU (1) HUP0100901A3 (fr)
IL (2) IL137475A0 (fr)
NO (1) NO327049B1 (fr)
NZ (1) NZ505892A (fr)
PL (1) PL202504B1 (fr)
RU (1) RU2192429C2 (fr)
TW (1) TW593339B (fr)
UA (1) UA71559C2 (fr)
WO (1) WO1999037666A1 (fr)
ZA (1) ZA99161B (fr)

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US20040202645A1 (en) * 2003-04-08 2004-10-14 Khan Nisar Ahmed Administration of gene-regulatory peptides
US6844315B2 (en) 1998-05-20 2005-01-18 Erasmus Universiteit Rotterdam Immunoregulator
US8680059B2 (en) * 1998-05-20 2014-03-25 Biotempt B.V. Oligopeptide acetate and formulations thereof
US20030220258A1 (en) * 2001-12-21 2003-11-27 Robbert Benner Treatment of ischemic events
US6921751B1 (en) * 1998-05-20 2005-07-26 Erasmus Universiteit Rotterdam Immunoregulator
US6902721B1 (en) * 1998-07-10 2005-06-07 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone growth
US7358330B2 (en) 2001-03-29 2008-04-15 Biotempt B.V. Immunoregulatory compositions
EP1300418A1 (fr) * 2001-10-04 2003-04-09 Erasmus Universiteit Rotterdam Régulation génétique par des oligopeptides
US6949567B2 (en) 2001-02-26 2005-09-27 4Sc Ag Compounds for the treatment of protozoal diseases
US7786084B2 (en) * 2001-12-21 2010-08-31 Biotempt B.V. Treatment of burns
US7560433B2 (en) 2001-12-21 2009-07-14 Biotempt B.V. Treatment of multiple sclerosis (MS)
US7501391B2 (en) * 2001-12-21 2009-03-10 Biotempt B.V. Treatment of transplant survival
US20080242837A1 (en) * 2001-12-21 2008-10-02 Khan Nisar A Peptide compositions
US20040013661A1 (en) * 2001-12-21 2004-01-22 Gert Wensvoort Stratification
US20030220260A1 (en) * 2001-12-21 2003-11-27 Khan Nisar Ahmed Peptide compositions
US20030220257A1 (en) * 2001-12-21 2003-11-27 Robbert Benner Treatment of trauma
US20080318871A1 (en) * 2001-12-21 2008-12-25 Khan Nisar A Treatment of neurological disorders
US20030220261A1 (en) * 2001-12-21 2003-11-27 Khan Nisar Ahmed Treatment of iatrogenic disease
EP1465862A1 (fr) 2002-01-17 2004-10-13 SmithKline Beecham Corporation Derives de cetoamides a substitution cycloalkyle, utiles comme inhibiteurs de cathepsine k
NZ561851A (en) 2002-04-11 2009-05-31 Vertex Pharma Inhibitors of serine proteases, particularly hepatitis C virus NS3 - NS4 protease
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
TW201127828A (en) 2003-09-05 2011-08-16 Vertex Pharma Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
US20090227505A1 (en) * 2004-01-07 2009-09-10 Biotempt B.V. Methods and uses for protein breakdown products
EP1637529A1 (fr) * 2004-09-20 2006-03-22 4Sc Ag Nouveaux analogues de piperidin-4-yl-thiazole-carboxamide en tant qu'inhibiteurs de proliferation de lymphocytes T er leurs utilisations
US7468383B2 (en) * 2005-02-11 2008-12-23 Cephalon, Inc. Proteasome inhibitors and methods of using the same
WO2006124494A1 (fr) * 2005-05-13 2006-11-23 Virginia Tech Intellectual Properties, Inc. Inhibiteurs d'etat de transition de pin1, constitues par des composes peptidomimetiques contenant un $g(a)-cetoamide, et synthese de ceux-ci
JP4846799B2 (ja) * 2005-07-05 2011-12-28 バイオテンプト ベー.フェー. 腫瘍の治療
TW200745061A (en) 2005-07-29 2007-12-16 Tibotec Pharm Ltd Macrocylic inhibitors of hepatitis C virus
MX2008001402A (es) 2005-07-29 2008-04-04 Tibotec Pharm Ltd Inhibidores macrociclicos del virus de la hepatitis c.
CN105237621A (zh) 2005-11-09 2016-01-13 欧尼斯治疗公司 用于酶抑制的化合物
US8594771B2 (en) * 2005-12-28 2013-11-26 General Electric Company Devices and methods for self-administered ECG examinations
EP1864692A1 (fr) * 2006-06-07 2007-12-12 Biotempt B.V. Utilisation de peptides pour la protection contre les radiolésions
EP2041158B1 (fr) 2006-06-19 2013-04-17 Onyx Therapeutics, Inc. Peptide epoxycetones destinees a l'inhibition de proteasome
SG178780A1 (en) * 2007-02-12 2012-03-29 Biotempt Bv Treatment of trauma-hemorrhage with short oligopeptides
US8859021B2 (en) * 2007-05-14 2014-10-14 Sytheon Skin appearance through gene manipulation
US7442830B1 (en) 2007-08-06 2008-10-28 Millenium Pharmaceuticals, Inc. Proteasome inhibitors
CL2008002966A1 (es) 2007-10-04 2010-06-25 Onyx Therapeutics Inc Compuesto tetrapeptido ceto-epoxido cristalino; sal citrato cristalina del compuesto; metodos de preparacion; compuesto intermediario cristalino; metodo de preparacion; y uso para tratar cancer, enfermedad autoinmune, afeccion relacionada con trasplante, enfermedad neurodegenerativa, afeccion asociada con fibrosis, entre otros.
MX349769B (es) 2008-06-17 2017-08-11 Millennium Pharm Inc Compuestos de éster boronato y composiciones farmacéuticas de los mismos.
EA035100B1 (ru) 2008-10-21 2020-04-28 Оникс Терапьютикс, Инк. Комбинированная терапия с применением пептид эпоксикетонов
EP3021120A1 (fr) 2009-02-20 2016-05-18 Michael P. Lisanti Procédé de diagnostic ou de pronostic d'un néoplasme comprenant la détermination du niveau d'expression d'une protéine dans des cellules stromales adjacentes au néoplasme
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
WO2011060179A1 (fr) 2009-11-13 2011-05-19 Onyx Therapeutics, Inc Utilisation de peptides epoxycetones pour la suppression de la metastase
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
US9359398B2 (en) 2010-03-01 2016-06-07 Onyx Therapeutics, Inc. Compounds for immunoproteasome inhibition
BR112012025264A2 (pt) 2010-04-07 2019-09-24 Onyx Therapeutics Inc inibidor de imunoproteassoma de e´poxicetona peptídica cristalina.
JP6002222B2 (ja) 2011-08-11 2016-10-05 ヤンセン ファーマシューティカ エヌ.ベー. がん治療用予測因子
EP2771489B1 (fr) 2011-10-28 2018-07-04 Millennium Pharmaceuticals, Inc. Biomarqueurs de réponse à des inhibiteurs de nae
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
EP2810066B1 (fr) 2012-01-24 2019-07-31 Millennium Pharmaceuticals, Inc. Méthodes de traitement du cancer
GB2523211B (en) 2012-01-27 2020-03-18 Univ Jefferson MCT protein inhibitor-related prognostic and therapeutic methods
UY34897A (es) 2012-07-09 2014-01-31 Onyx Therapeutics Inc Profarmacos de inhibidores peptidicos de expoxi cetona proteasa
CA2886783A1 (fr) 2012-10-01 2014-04-10 Millennium Pharmaceuticals, Inc. Biomarqueurs et procedes pour predire la reponse vis-a-vis d'inhibiteurs et leurs utilisations
EP2906581A1 (fr) * 2012-10-11 2015-08-19 F. Hoffmann-La Roche AG Inhibiteurs de cétoamide immunoprotéasome
US10022372B2 (en) 2013-04-19 2018-07-17 Thomas Jefferson University Caveolin-1 related methods for treating glioblastoma with temozolomide
JP2017524652A (ja) 2014-05-20 2017-08-31 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. 一次癌療法後に使用するためのホウ素含有プロテアソーム阻害剤
JP6859559B2 (ja) * 2017-03-16 2021-04-14 二村 芳弘 抗アレルギー作用を呈するフェニルペプチド誘導体
WO2019044736A1 (fr) * 2017-08-28 2019-03-07 静岡県公立大学法人 Procédé de détection et sonde de détection pour la colibactine et des bactéries produisant de la colibactine

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JPH04211648A (ja) * 1990-07-27 1992-08-03 Nippon Kayaku Co Ltd ケト酸アミド誘導体
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US5834487A (en) * 1996-09-24 1998-11-10 Cv Therapeutics Inhibition of 26S and 20S proteasome by indanones

Also Published As

Publication number Publication date
US6075150A (en) 2000-06-13
KR100417888B1 (ko) 2004-02-11
NZ505892A (en) 2002-10-25
CN1289340A (zh) 2001-03-28
PL202504B1 (pl) 2009-06-30
NO20003807D0 (no) 2000-07-25
AU2326799A (en) 1999-08-09
ZA99161B (en) 1999-07-28
NO327049B1 (no) 2009-04-14
JP3863370B2 (ja) 2006-12-27
WO1999037666A1 (fr) 1999-07-29
BR9907256A (pt) 2001-10-09
CA2319150A1 (fr) 1999-07-29
PL343269A1 (en) 2001-08-13
US6781000B1 (en) 2004-08-24
GEP20032869B (en) 2003-01-27
HUP0100901A3 (en) 2001-11-28
HUP0100901A2 (hu) 2001-08-28
TW593339B (en) 2004-06-21
KR20010034381A (ko) 2001-04-25
NO20003807L (no) 2000-09-25
AR012781A1 (es) 2000-11-08
RU2192429C2 (ru) 2002-11-10
EP1058689A1 (fr) 2000-12-13
AU747835B2 (en) 2002-05-23
IL137475A (en) 2006-10-05
IL137475A0 (en) 2001-07-24
JP2002501080A (ja) 2002-01-15
CA2319150C (fr) 2004-08-31

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