RS54857B1 - Konjugati disorazola i njihovih derivata sa molekulima koji se vezuju za ćeliju, novi derivati disorazola, postupci za proizvodnju i njihova upotreba - Google Patents

Konjugati disorazola i njihovih derivata sa molekulima koji se vezuju za ćeliju, novi derivati disorazola, postupci za proizvodnju i njihova upotreba

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Publication number
RS54857B1
RS54857B1 RS20160412A RSP20160412A RS54857B1 RS 54857 B1 RS54857 B1 RS 54857B1 RS 20160412 A RS20160412 A RS 20160412A RS P20160412 A RSP20160412 A RS P20160412A RS 54857 B1 RS54857 B1 RS 54857B1
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Serbia
Prior art keywords
alkyl
group
independently selected
heterocyclyl
heteroaryl
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RS20160412A
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English (en)
Inventor
Eckhard Günther
Olaf Schaefer
Michael Teifel
Klaus Paulini
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Aeterna Zentaris Gmbh
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Publication date
Application filed by Aeterna Zentaris Gmbh filed Critical Aeterna Zentaris Gmbh
Publication of RS54857B1 publication Critical patent/RS54857B1/sr

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    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12PFERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P17/00Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms
    • C12P17/18Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms containing at least two hetero rings condensed among themselves or condensed with a common carbocyclic ring system, e.g. rifamycin
    • C12P17/188Heterocyclic compound containing in the condensed system at least one hetero ring having nitrogen atoms and oxygen atoms as the only ring heteroatoms
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575Hormones
    • C07K14/655Somatostatins
    • C07K14/6555Somatostatins at least 1 amino acid in D-form
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/23Luteinising hormone-releasing hormone [LHRH]; Related peptides

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Zoology (AREA)
  • Medicinal Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Endocrinology (AREA)
  • Engineering & Computer Science (AREA)
  • Wood Science & Technology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biophysics (AREA)
  • Toxicology (AREA)
  • General Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)

Abstract

Jedinjenje formule (I) ili (IV)C1 -B1 -A-B2-C2 (I),C1 - B1 -A (IV),gde za (I) i (IV) :A je disorazolni ostatak prema formuli (III)gde:Rio, Rjo, Rkp, Rmp, R28, R30, R31, R32, R33, R34, R35, R36, R38, R40, R41, R42, R43, R44 su vodonik;RIp, Rnp zajedno obrazuju dvostruku vezu ili su nezavisno izabrani iz grupe koju "vodonik, alkoksil";R27, R29 zajedno obrazuju dvostruku vezu ili eposkid (oksiran);R37, R39 zajedno obrazuju dvostruku vezu ili epoksid (oksiran);R25, R26 su nezavisno jedan od drugog izabrani iz grupe koju čine: "alkil" koji je opciono supstituisan kao alkil grupa sa 1, 2 ili 3 supstituenta nezavisno izabrana jedan od drugog iz grupe koju čine "alkil, cikloalkil, cikloalkil-alkil, aril, heteroaril, aril-alkil, heteroaril-alkil, heterociklil, heterociklil-alkil, alkilsulfonil, arilsulfonil, aril-alkilsulfonil, -F, -Cl, -Br, -I, -N3, -NO2, =O, =S, =S(O)2, hidroksil, acetil, karboksil, karboksilestar, amid, karbonat, karbamat, ostaci alfa-amino kiselina, ostaci beta-amino kiselina, alkoksil, amino, hidroksilamino, mono-alkiiamino, di-alkiiamino, hidrazinil, cijano, cijano-alkii, sulfhidril, disulfidilatkil i/ili alkil-sulfidil";B1 i/ili B2 su nezavisno jedan od drugog izabrani iz grupe koju čine "vezujuća grupa ostatkadikarbonske kiseline, sukcinii, glutaril";C1 i/ili C2 su nezavisno jedan od drugog izabrani iz grupe koju čine "LHRH, [D-Lys6] LHRH, somatostatin, somatostatin analozi, humani albumin iz seruma (HSA)";o je 1 ili 2; p je 1 ili 2;gde izraz "alkil" uključuje aciklične zasićene, delimično nezasićene ili zasićene ugljovodonike koje imaju C1-C12 ugljenikove atome, koji mogu biti ravnolančani ili razgranati i mogu sadržati jednu ili više dvostrukih veza i/ili jednu ili više trostrukih veza; ' gde se izraz "alkoksil" odnosi na radikale u kojima "alkil", "cikloalkil", "cikloalkil-alkil", "aril", "arilalkil", "heteroaril", "heteroaril-alkil", "heterociklil" i/ili "heterociklil-alkil" grupa je vezana preko atoma kiseonika (-O-grupa).Prijava sadrži još 16 patentnih zahteva.
RS20160412A 2006-09-06 2007-09-06 Konjugati disorazola i njihovih derivata sa molekulima koji se vezuju za ćeliju, novi derivati disorazola, postupci za proizvodnju i njihova upotreba RS54857B1 (sr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US84235706P 2006-09-06 2006-09-06
EP06018750A EP1900742A1 (en) 2006-09-07 2006-09-07 Conjugates of disorazoles and their derivatives with cell-binding molecules, novel disorazole derivatives, processes of manufacturing and uses thereof
PCT/EP2007/059310 WO2008028934A1 (en) 2006-09-06 2007-09-06 Conjugates of disorazoles and their derivatives with cell-binding molecules, novel disorazole derivatives, processes of manufacturing and uses thereof
EP07803270.3A EP2066679B1 (en) 2006-09-06 2007-09-06 Conjugates of disorazoles and their derivatives with cell-binding molecules, novel disorazole derivatives, processes of manufacturing and uses thereof

Publications (1)

Publication Number Publication Date
RS54857B1 true RS54857B1 (sr) 2016-10-31

Family

ID=37670733

Family Applications (1)

Application Number Title Priority Date Filing Date
RS20160412A RS54857B1 (sr) 2006-09-06 2007-09-06 Konjugati disorazola i njihovih derivata sa molekulima koji se vezuju za ćeliju, novi derivati disorazola, postupci za proizvodnju i njihova upotreba

Country Status (16)

Country Link
US (3) US7741277B2 (sr)
EP (2) EP1900742A1 (sr)
KR (1) KR101532966B1 (sr)
AR (1) AR062685A1 (sr)
AU (1) AU2007293650B2 (sr)
CA (1) CA2662308C (sr)
DK (1) DK2066679T3 (sr)
ES (1) ES2572183T3 (sr)
HU (1) HUE028061T2 (sr)
MX (2) MX2009002483A (sr)
NZ (1) NZ575032A (sr)
PL (1) PL2066679T3 (sr)
RS (1) RS54857B1 (sr)
SI (1) SI2066679T1 (sr)
TW (1) TWI346116B (sr)
WO (1) WO2008028934A1 (sr)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1900742A1 (en) 2006-09-07 2008-03-19 AEterna Zentaris GmbH Conjugates of disorazoles and their derivatives with cell-binding molecules, novel disorazole derivatives, processes of manufacturing and uses thereof
WO2010033207A1 (en) 2008-09-19 2010-03-25 Nektar Therapeutics Polymer conjugates of therapeutic peptides
WO2010033224A1 (en) * 2008-09-19 2010-03-25 Nektar Therapeutics Polymer conjugates of kiss1 peptides
CN102325545A (zh) * 2009-02-20 2012-01-18 益普生制药股份有限公司 具有神经肽y受体结合化合物的细胞毒性缀合物
US20120004182A1 (en) * 2010-07-02 2012-01-05 Carsten Gruendker Pharmaceutical compositions and methods for induction and enhancement of apoptosis in tumor cells
CN104246497B (zh) * 2012-03-18 2017-10-13 国立大学法人九州大学 疾病样品分析装置、分析系统及分析方法
KR101974583B1 (ko) 2012-08-29 2019-05-02 삼성전자주식회사 링커 폴리펩티드 및 이를 이용한 표적 물질 분석 방법
US11465997B2 (en) 2017-06-22 2022-10-11 William Marsh Rice University Synthesis of disorazoles and analogs thereof as potent anticancer agents

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6214969B1 (en) 1988-10-21 2001-04-10 The Administrators Of The Tulane Educational Fund Luteinizing hormone releasing hormone analogs with cytotoxic moiety
US5866679A (en) 1994-06-28 1999-02-02 Merck & Co., Inc. Peptides
US5843903A (en) 1995-11-27 1998-12-01 The Administrators Of The Tulane Educational Fund Targeted cytotoxic anthracycline analogs
JP2001501601A (ja) 1996-09-12 2001-02-06 メルク エンド カンパニー インコーポレーテッド 前立腺ガンの治療において有用な共役体
DE19728737C1 (de) 1997-07-04 1999-02-11 Johannes Christian Groeninghen Verfahren zur Erkennung und Bestimmung von GnRH-Rezeptoren und die Verwendung von GnRH-Agonisten und GnRH-Antagonisten zur Behandlung eines Tumors ausgehend vom Hirn und/oder Nervensystem und/oder den Hirnhäuten
WO1999002175A1 (en) 1997-07-10 1999-01-21 Merck & Co., Inc. Conjugates useful in the treatment of prostate cancer
EP1536789A1 (de) 2002-08-24 2005-06-08 Zentaris GmbH Arzneimittel enthaltend disorale und ihre derivate und deren anwendung zur behandlung gutartiger und bösartiger tumorerkrankngen
AU2003298864A1 (en) 2002-12-06 2004-06-30 Kosan Biosciences, Inc. Disorazole polyketide synthase encoding polynucleotides
US7517903B2 (en) * 2004-05-19 2009-04-14 Medarex, Inc. Cytotoxic compounds and conjugates
US20060199252A1 (en) 2005-01-13 2006-09-07 Herbert Irschik Genes encoding the synthetic pathway for the production of disorazole
WO2006075013A1 (en) 2005-01-13 2006-07-20 Helmholtz-Zentrum für Infektionsforschung GmbH Genes encoding the synthetic pathway for the production of disorazole
WO2006135371A1 (en) * 2005-06-09 2006-12-21 Kosan Biosciences Incorporated Conjugates with reduced adverse systemic effects
EP1743897A1 (en) * 2005-07-15 2007-01-17 Gesellschaft für Biotechnologische Forschung mbH Biologically active compounds obtainable from Sorangium cellulosum
EP1900742A1 (en) 2006-09-07 2008-03-19 AEterna Zentaris GmbH Conjugates of disorazoles and their derivatives with cell-binding molecules, novel disorazole derivatives, processes of manufacturing and uses thereof

Also Published As

Publication number Publication date
EP2066679A1 (en) 2009-06-10
CA2662308A1 (en) 2008-03-13
ES2572183T3 (es) 2016-05-30
TW200823228A (en) 2008-06-01
US20080090758A1 (en) 2008-04-17
MX2009002483A (es) 2009-03-23
RU2009112546A (ru) 2010-10-20
CA2662308C (en) 2014-10-28
WO2008028934A1 (en) 2008-03-13
US20100323963A1 (en) 2010-12-23
PL2066679T3 (pl) 2016-09-30
US20100317580A1 (en) 2010-12-16
HUE028061T2 (en) 2016-11-28
US8470776B2 (en) 2013-06-25
SI2066679T1 (sl) 2016-06-30
EP2066679B1 (en) 2016-03-09
AU2007293650B2 (en) 2012-06-14
NZ575032A (en) 2011-02-25
EP1900742A1 (en) 2008-03-19
WO2008028934A8 (en) 2008-05-02
MX337358B (es) 2016-02-29
DK2066679T3 (en) 2016-06-27
US7741277B2 (en) 2010-06-22
KR20090064436A (ko) 2009-06-18
KR101532966B1 (ko) 2015-07-02
AU2007293650A1 (en) 2008-03-13
TWI346116B (en) 2011-08-01
AR062685A1 (es) 2008-11-26

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