HUP0100901A2 - 20S Ptoteaszóma alfa-ketoamidin inhibitor hatású peptidszármazékok, azokat tartalmazó gyógyszerkészítmények és alkalmazásuk - Google Patents

20S Ptoteaszóma alfa-ketoamidin inhibitor hatású peptidszármazékok, azokat tartalmazó gyógyszerkészítmények és alkalmazásuk

Info

Publication number
HUP0100901A2
HUP0100901A2 HU0100901A HUP0100901A HUP0100901A2 HU P0100901 A2 HUP0100901 A2 HU P0100901A2 HU 0100901 A HU0100901 A HU 0100901A HU P0100901 A HUP0100901 A HU P0100901A HU P0100901 A2 HUP0100901 A2 HU P0100901A2
Authority
HU
Hungary
Prior art keywords
substituted
aryl
heteroaryl
amino acids
alkyl
Prior art date
Application number
HU0100901A
Other languages
English (en)
Inventor
Alison Joly
Suresh Kerwar
Robert T. Lum
Steven R. Schow
Lisa Wang
Michael M. Wick
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 HUP0100901A2 publication Critical patent/HUP0100901A2/hu
Publication of HUP0100901A3 publication Critical patent/HUP0100901A3/hu

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0205—Peptides 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207—Peptides 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • 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
    • A61K38/00—Medicinal preparations containing peptides

Abstract

A találmány a (I) általános képletű vegyületekre vonatkozik, aképletben X2 jelentése -Ar vagy -Ar-X3 általános képletű csoport, aholX3 jelentése -C(O)-, -CH2C(O)- vagy -(CH2)n- általános képletűcsoport, ahol n értéke 0 és 2 közötti szám és Ar jelentése fenil-,helyettesített fenil-, indolil-, helyettesített indolil- vagybármilyen más heteroarilcsoport; R1 és R2 jelentése egymástólfüggetlenül az ismert természetes a-aminosavak és nem természetesaminosavak oldallánca, hidrogénatom, alkil-, helyettesített alkil-,aril-, helyettesített aril-, helyettesített aril-, alkoxiaril-,cikloalkilcsoport, heterociklusos, helyettesített heterociklusoscsoport, heteroaril- vagy helyettesített heteroarilcsoport; X1jelentése hidroxil-, monoalkilamino-, dialkilamino-, alkoxi-,arilkoxi- vagy (a) általános képletű csoport, amelynek képletében X4jelentése hidroxil-, arilamino-, monoalkilamino-, dialkilamino-,alkoxi- vagy arilalkoxicsoport; R3 jelentése az ismert természetes a-aminosavak és nem természetes aminosavak oldallánca, hidrogénatom,alkil-, helyettesített alkil-, aril-, helyettesített aril-,helyettesített aril-, alkoxiaril-, cikloalkilcsoport, heterociklusos,helyettesített heterociklusos csoport, heteroaril- vagy helyettesítettheteroarilcsoport. A találmány kiterjed a fenti vegyületek sóira, ésaz ezeket tartalmazó, sejtszaporodással kapcsolatos betegségekkezelésére alkalmas gyógyszerkészítményekre is, továbbá a fentivegyületek alkalmazására. Ó
HU0100901A 1998-01-26 1999-01-19 Peptide derivatives being alpha-ketoamide inhibitors of 20s proteasome, pharmaceutical compositions comprising thereof and their use HUP0100901A3 (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 (en) 1998-01-26 1999-01-19 α-KETOAMIDE INHIBITORS OF 20S PROTEASOME

Publications (2)

Publication Number Publication Date
HUP0100901A2 true HUP0100901A2 (hu) 2001-08-28
HUP0100901A3 HUP0100901A3 (en) 2001-11-28

Family

ID=21759598

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0100901A HUP0100901A3 (en) 1998-01-26 1999-01-19 Peptide derivatives being alpha-ketoamide inhibitors of 20s proteasome, pharmaceutical compositions comprising thereof and their use

Country Status (20)

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

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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
UA71559C2 (en) 2004-12-15
JP3863370B2 (ja) 2006-12-27
WO1999037666A1 (en) 1999-07-29
BR9907256A (pt) 2001-10-09
CA2319150A1 (en) 1999-07-29
PL343269A1 (en) 2001-08-13
US6781000B1 (en) 2004-08-24
GEP20032869B (en) 2003-01-27
HUP0100901A3 (en) 2001-11-28
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 (en) 2000-12-13
AU747835B2 (en) 2002-05-23
IL137475A (en) 2006-10-05
IL137475A0 (en) 2001-07-24
JP2002501080A (ja) 2002-01-15
CA2319150C (en) 2004-08-31

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