[go: up one dir, main page]

AR012781A1 - Alfa-cetoamida inhibidores de 20s proteosoma. - Google Patents

Alfa-cetoamida inhibidores de 20s proteosoma.

Info

Publication number
AR012781A1
AR012781A1 ARP990100205A ARP990100205A AR012781A1 AR 012781 A1 AR012781 A1 AR 012781A1 AR P990100205 A ARP990100205 A AR P990100205A AR P990100205 A ARP990100205 A AR P990100205A AR 012781 A1 AR012781 A1 AR 012781A1
Authority
AR
Argentina
Prior art keywords
substituted
aryl
linear
heteroaryl
carbon
Prior art date
Application number
ARP990100205A
Other languages
English (en)
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 AR012781A1 publication Critical patent/AR012781A1/es

Links

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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Indole Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

Alfa-cetoamida inhibidores de 20S proteasoma que comprende un compuesto que tiene la formula (I), en la cual X2 es Ar o Ar-X3, donde X3 es -C=O o-CH2CO- o (CH2)n donde n = 0-2 y donde Ar es fenilo, fenilo sustituido, indol, indoles sustituidosy cualquier otro heteroarilo. Cada uno de R1 y R2 esseleccionado individualmente entre las cadenas laterales de los alfa-aminoácidos naturales y aminoácidos no naturales conocidos, hidrogeno,alquilo lineal o ramificado de 1-10 carbonos , alquilosustituido lineal o ramificado de 1-10 carbonos, arilo y arilo sustituido, arilo lineal oramificado de 1-10 carbonos, alcoxiarilo, cicloalquilo de 3-8 carbones, heterociclo, heterociclo sustituido, heteroarilo y heteroarilo su stituido. X1esseleccionado entre -OH, monoalquilamino, dialquilamino, alcoxido, arilcoxido y formula (II), donde X4 es hidroxido, arilamino,monoalquilamino, dialquilamino, alcoxido o arilalcoxido; R3 es seleccionado entre las cadenas laterales de los alfa-aminoácidos naturales y aminoácidos nonaturales conocidos, hidrogeno, sustituyentes alquilo lineal y ramificado de 1-10 carbonos, alquilo sustituido lineal o ramificado de 1-10 carbonos, arilo,arilo sustituido, arilo lineal o ramificado de 1-10carbonos, alcoxiarilo, cicloalquilo de 3-8 carbones, heterociclo, heterociclo sustituido, heteroarilo y heteroarilo sustituido, el uso de la misma para la manufactura de un medicamento y composicion farmacéutica que l a comprende.
ARP990100205A 1998-01-26 1999-01-20 Alfa-cetoamida inhibidores de 20s proteosoma. AR012781A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US09/013,365 US6075150A (en) 1998-01-26 1998-01-26 α-ketoamide inhibitors of 20S proteasome

Publications (1)

Publication Number Publication Date
AR012781A1 true AR012781A1 (es) 2000-11-08

Family

ID=21759598

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP990100205A AR012781A1 (es) 1998-01-26 1999-01-20 Alfa-cetoamida inhibidores de 20s proteosoma.

Country Status (20)

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

Families Citing this family (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050227925A1 (en) * 2004-04-08 2005-10-13 Robbert Benner Compositions capable of reducing elevated blood urea concentration
US6844315B2 (en) 1998-05-20 2005-01-18 Erasmus Universiteit Rotterdam Immunoregulator
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
US20040202645A1 (en) * 2003-04-08 2004-10-14 Khan Nisar Ahmed Administration of gene-regulatory peptides
US8680059B2 (en) * 1998-05-20 2014-03-25 Biotempt B.V. Oligopeptide acetate and formulations thereof
US6902721B1 (en) * 1998-07-10 2005-06-07 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone growth
EP1300418A1 (en) * 2001-10-04 2003-04-09 Erasmus Universiteit Rotterdam Gene regulation by oligopeptides
US7358330B2 (en) * 2001-03-29 2008-04-15 Biotempt B.V. Immunoregulatory compositions
EP1395548A1 (en) 2001-02-26 2004-03-10 4Sc Ag Derivatives of diphenylurea, diphenyloxalic acid diamide and diphenylsulfuric acid diamide and their use as medicaments
US20080242837A1 (en) * 2001-12-21 2008-10-02 Khan Nisar A Peptide compositions
US20040013661A1 (en) * 2001-12-21 2004-01-22 Gert Wensvoort Stratification
US7560433B2 (en) 2001-12-21 2009-07-14 Biotempt B.V. Treatment of multiple sclerosis (MS)
US20080318871A1 (en) * 2001-12-21 2008-12-25 Khan Nisar A Treatment of neurological disorders
US20030220260A1 (en) * 2001-12-21 2003-11-27 Khan Nisar Ahmed Peptide compositions
US7501391B2 (en) * 2001-12-21 2009-03-10 Biotempt B.V. Treatment of transplant survival
US20030220261A1 (en) * 2001-12-21 2003-11-27 Khan Nisar Ahmed Treatment of iatrogenic disease
US20030220257A1 (en) * 2001-12-21 2003-11-27 Robbert Benner Treatment of trauma
US7786084B2 (en) * 2001-12-21 2010-08-31 Biotempt B.V. Treatment of burns
WO2003062192A1 (en) 2002-01-17 2003-07-31 Smithkline Beecham Corporation Cycloalkyl ketoamides derivatives useful as cathepsin k inhibitors
RU2004133044A (ru) 2002-04-11 2006-01-27 Вертекс Фармасьютикалз Инкорпорейтед (Us) Ингибиторы сериновых протеаз, в частности, протеазы ns3-ns4a hcv
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
UY28500A1 (es) 2003-09-05 2005-04-29 Vertex Pharma Inhibidores de proteasas de serina, en particular proteasa ns3-ns4a del vhc.
US20090227505A1 (en) * 2004-01-07 2009-09-10 Biotempt B.V. Methods and uses for protein breakdown products
EP2030981B1 (en) * 2004-05-10 2014-07-09 Onyx Therapeutics, Inc. Compounds for proteasome enzyme inhibition
EP1637529A1 (en) 2004-09-20 2006-03-22 4Sc Ag Novel piperidin-4-yl-thiazole-carboxamide analogues as inhibitors of T-cell proliferation and uses thereof
US7468383B2 (en) * 2005-02-11 2008-12-23 Cephalon, Inc. Proteasome inhibitors and methods of using the same
WO2006124494A1 (en) * 2005-05-13 2006-11-23 Virginia Tech Intellectual Properties, Inc. TRANSITION-STATE INHIBITORS OF PIN1, α-KETOAMIDE-CONTAINING PEPTIDOMIMETICS, AND SYNTHESES THEREOF
CA2614084A1 (en) * 2005-07-05 2007-01-11 Biotempt B.V. Treatment of tumors
JP5230416B2 (ja) 2005-07-29 2013-07-10 テイボテク・フアーマシユーチカルズ C型肝炎ウイルスの大員環状阻害剤
AR055361A1 (es) 2005-07-29 2007-08-22 Medivir Ab Inhibidores macrociclicos del virus de la hepatitis c
PL1948678T3 (pl) * 2005-11-09 2013-09-30 Onyx Therapeutics Inc Związki do hamowania enzymów
US8594771B2 (en) * 2005-12-28 2013-11-26 General Electric Company Devices and methods for self-administered ECG examinations
EP1864692A1 (en) * 2006-06-07 2007-12-12 Biotempt B.V. Use of peptides for the control of radiation injury
CA2657213C (en) 2006-06-19 2017-01-03 Proteolix, Inc. Peptide epoxyketones for proteasome inhibition
PL2120991T3 (pl) * 2007-02-12 2014-07-31 Biotempt Bv Leczenie urazów krwotocznych krótkimi oligopeptydami
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.
EP3536693A1 (en) 2008-06-17 2019-09-11 Millennium Pharmaceuticals, Inc. Boronate ester compounds and pharmaceutical compositions thereof
EP2349313A4 (en) 2008-10-21 2012-08-29 Onyx Therapeutics Inc COMBINATION THERAPY WITH EPOXYCLETON PEPTIDES
EP2399129B1 (en) 2009-02-20 2015-11-25 Michael P. Lisanti 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
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
EP2498793B1 (en) 2009-11-13 2019-07-10 Onyx Therapeutics, Inc. Oprozomib for use in metastasis suppression
CA2785300A1 (en) 2009-12-22 2011-07-21 Cephalon, Inc. Proteasome inhibitors and processes for their preparation, purification and use
US9359398B2 (en) 2010-03-01 2016-06-07 Onyx Therapeutics, Inc. Compounds for immunoproteasome inhibition
AU2011245630B2 (en) 2010-04-07 2014-07-03 Onyx Therapeutics, Inc. Crystalline peptide epoxyketone immunoproteasome inhibitor
EP2742356B1 (en) 2011-08-11 2016-04-27 Janssen Pharmaceutica N.V. Predictors for cancer treatment
US9827246B2 (en) 2011-10-28 2017-11-28 Millennium Pharmaceuticals, Inc. Biomarkers of response to NAE inhibitors
US20150184246A1 (en) 2011-11-11 2015-07-02 Millennium Pharmaceuticals, Inc. Biomarkers of response to proteasome inhibitors
EP2810066B1 (en) 2012-01-24 2019-07-31 Millennium Pharmaceuticals, Inc. Methods of treatment of cancer
WO2013112881A1 (en) 2012-01-27 2013-08-01 Thomas Jefferson University Mct protein inhibitor-related prognostic and therapeutic methods
WO2014011695A2 (en) 2012-07-09 2014-01-16 Onyx Therapeutics, Inc. Prodrugs of peptide epoxy ketone protease inhibitors
JP6486826B2 (ja) 2012-10-01 2019-03-20 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. 阻害剤に対する応答を予測するためのバイオマーカーおよび方法、ならびにそれらの使用
CA2892368A1 (en) * 2012-10-11 2014-04-17 F. Hoffmann-La Roche Ag Ketoamide immunoproteasome inhibitors
WO2014172627A1 (en) 2013-04-19 2014-10-23 Thomas Jefferson University Caveolin-1 related methods for treating glioblastoma with temozolomide
WO2015179443A1 (en) 2014-05-20 2015-11-26 Millennium Pharmaceuticals. Inc. Boron-containing proteasome inhibitors for use after primary cancer therapy
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 (ja) 2017-08-28 2019-03-07 静岡県公立大学法人 コリバクチンおよびコリバクチン産生菌の検出方法および検出プローブ

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1206078B (it) * 1987-06-03 1989-04-14 Polifarma Spa Procedimento per la produzione di acido 3-indolpiruvico e suoi derivati loro uso farmaceutico
JPH04211648A (ja) * 1990-07-27 1992-08-03 Nippon Kayaku Co Ltd ケト酸アミド誘導体
US5430022A (en) * 1990-05-14 1995-07-04 Fujisawa Pharmaceutical Co., Ltd. Peptide compound and its preparation
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
US6083903A (en) * 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
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
UA71559C2 (en) 2004-12-15
NO20003807D0 (no) 2000-07-25
KR20010034381A (ko) 2001-04-25
PL343269A1 (en) 2001-08-13
US6075150A (en) 2000-06-13
GEP20032869B (en) 2003-01-27
CA2319150A1 (en) 1999-07-29
AU747835B2 (en) 2002-05-23
IL137475A0 (en) 2001-07-24
CN1289340A (zh) 2001-03-28
NO327049B1 (no) 2009-04-14
US6781000B1 (en) 2004-08-24
WO1999037666A1 (en) 1999-07-29
BR9907256A (pt) 2001-10-09
JP2002501080A (ja) 2002-01-15
ZA99161B (en) 1999-07-28
CA2319150C (en) 2004-08-31
HUP0100901A2 (hu) 2001-08-28
EP1058689A1 (en) 2000-12-13
KR100417888B1 (ko) 2004-02-11
JP3863370B2 (ja) 2006-12-27
AU2326799A (en) 1999-08-09
NO20003807L (no) 2000-09-25
RU2192429C2 (ru) 2002-11-10
TW593339B (en) 2004-06-21
PL202504B1 (pl) 2009-06-30
NZ505892A (en) 2002-10-25
IL137475A (en) 2006-10-05
HUP0100901A3 (en) 2001-11-28

Similar Documents

Publication Publication Date Title
AR012781A1 (es) Alfa-cetoamida inhibidores de 20s proteosoma.
CO5550472A2 (es) Piperazinas heterociclicas sustituidas para el tratamiento de la esquizofrenia
CO4970713A1 (es) Derivados de carboxamidotiazoles, su preparacion, composiciones farmaceuticas que los contienen
AR013094A1 (es) Compuestos de urea n-sustituida,composicion farmaceutica y uso de dichos compuestos para preparar medicamentos
ES2196806T3 (es) Derivados de fenilurea y de feniltiourea.
PE20020266A1 (es) Nuevos peptidos como inhibidores de ns3-serina proteasa del virus de la hepatitis c
ES2184352T3 (es) Derivados de adamantano.
CO5640136A2 (es) Derivados de hexahidropiridoisoquinolinas inhibidores de dpp-iv y composiciones farmaceuticas que los contienen
ES2196772T3 (es) Compuestos amino ciclicos.
CO5060510A1 (es) Isotiazol carboxiamidas y composiciones para la proteccion de las plantas
AR003449A1 (es) Compuestos de 6-dimetilaminometil-ciclohexano sustituidos, procedimiento para su preparacion y su uso
AR020165A1 (es) Derivados de pirimidinas sustituidas, su procedimiento de preparacion, composiciones farmaceuticas que las contienen y el uso de los mismos para la preparacion de medicamentos
CO5700752A2 (es) Derivados de piperazina y piperazin-2-ona especificos al receptor de melano cortina
ES2189462T3 (es) Derivados de acido aminometilcarboxilico.
ES8705469A1 (es) Procedimiento para preparar nuevas somatostatinas
CO5611126A2 (es) Derivados de indolinona utiles como inhibidores de la proteina cinasa
CO5130016A1 (es) Derivados de dihidrobenzodioxina carboxamida y cetona
ES2255190T3 (es) Compuestos indol 2,3-sustituidos como inhibidores de cox-2.
AR008267A1 (es) Pirroles sustituidos.
CO5060426A1 (es) 1-aril-3-imidiopirazoles plaguicidas
AR007969A1 (es) Compuestos derivados de pirroles sustituidos, su utilizacion y composiciones farmaceuticas que contienen tales compuestos
ES2038678T3 (es) Procedimiento para la preparacion de n-(2-alquil-3-mercapto-glutaril)-alfamino-acidos.
UY25211A1 (es) Inhibidores de isoquinolinilguanidina uroquinasa
MXPA04000443A (es) Metodo novedoso para la sintesis de derivados del acido (2s, 3as, 7as)-1-[(s)-alanil]-octahidro-1h-indol-2-carboxilico y la aplicacion en la sintesis de perindopril.
CO5680419A2 (es) Derivados de 1-[(indol-3-il)carbonil] piperazinas

Legal Events

Date Code Title Description
FG Grant, registration