Targeting conjugates comprising active agents encapsulated in cyclodextrin-containing polymers 机翻标题: 暂无翻译,请尝试点击翻译按钮。

公开号/公开日
WO2009001364 A2 2008-12-31 [WO200901364]WO2009001364 A3 2010-02-18 [WO200901364] / 2008-12-312010-02-18
申请号/申请日
2008WO-IL00884 / 2008-06-29
发明人
GNAIM JALLAL M;ATHAMNA MUHAMMAD;
申请人
CAPSUTECH;
主分类号
IPC分类号
A01N-043/04A61K-031/715
摘要
(WO200901364) A targeting conjugate is provided comprising an active agent, one or more residues of a cyclodextrin (CD)-containing polymer and a biorecognition molecule.  The polymer is preferably a peptide or a polypeptide comprising at least one amino acid residue containing a functional side group to which at least one of the CD residues is linked covalently; the biorecognition molecule is covalently bonded directly or via a spacer to the polymer backbone of the CD-containing polymer; and the active agent is noncovalently encapsulated within the cavity of the cyclodextrin residues and/or entrapped within the polymer matrix of the CD-containing polymer.
机翻摘要
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地址
代理人
代理机构
;
优先权号
2007US-60946775 2007-06-28
主权利要求
(WO200901364) CLA I MS 1 . An active agent-cyclodcxtrin-biorecognition molecule conjugate, wherein: (i) said cyclodextrin (CD) is a CD-containing polymer comprising one or more CD residues, said polymer is selected from a peptide, a polypeptide, an oligonucleotide or a polynucleotide, the peptide or polypeptide comprises at least one amino acid residue containing a functional side group and at least one of the CD residues is linked covalently to said functional side group or to the sugar moiety of a nucleotide residue oi~said oligonucleotide or polynucleotide; (ii) said biorecognition molecule is covalently bonded directly or via a spacer to the polymer backbone of the CD- containing polymer; and (iii) said active agent is noncovalently encapsulated within the cavity of the cyclodextrin residues and/or entrapped within the polymer matrix of the CD-polymer. 2. The conjugate according to claim I , comprising one or more cyclodextrin residues selected from α-, β-, γ-cyclodextrin, a combination thereof, derivatives, analogs or isomers thereof, preferably β-cyclodcxtrin or a β-cyclodextrin derivative, wherein at least one of the cyclodexlrin residues is covalently linked to a functional side group of an amino acid residue of an all-L, all-D or L.D-peplidc or polypeptide, in which the amino acids may be natural amino acids, non-natural amino acids or chemically modified amino acids. containing a functional side group. 3. The conjugate according to claim 2, wherein said at least one amino acids containing a functional side group is lysine, asparlic acid, glutamic acid, cysteine, serine, threonine, tyrosine or histidine. 4. The conjugate according to claim 1. wherein said peptide is an oligopeptide of 2-20. preferably, 2- 10 amino acid residues, more preferably 2 amino acid residues. 5. The conjugate according to claim 4. wherein said peptide of 2 amino acid residues is the dipeplide GIu-GIu. Asp-Asp. Lys-Lys or Cys-Cys. 6. The conjugate according to claim 1 , wherein said polypeptide or protein has 2 1 to 10,000, preferably, 100-500 amino acid residues. 7. The conjugate according to claim 6, wherein the polypeptide is a homopolypeptide of an amino acid having a functional side group such as polylysine. polygluiamic acid, polyaspartic acid, polycystcine, polyscrine. polyihrconinc or polytyrosine. 8. The conjugate according to claim 1. wherein said biorccognition molecule is a peptide, a protein, a lipid, a carbohydrate, an oligonucleotide, a polynucleotide, or an organic molecule which binds to a target site. 9. The conjugate according to claim 8, wherein the biorecognition molecule is a protein selected from the group consisting of antibodies, antigens, hormones, cytokines, enzymes, and receptors. 10. The conjugate according to claim 9, wherein said antibodies include monoclonal and polyclonal antibodies, fragments such as the Fab and Fc fragments. chimeric and humanized antibodies and derivatives thereof 1 1 . The conjugate according to claim 10, wherein said antibody is a chimeric or humanized anticancer monoclonal antibody. 12. The conjugate according to claim 1. wherein said active agent is a compound that has therapeutic, inhibitory, antimetabolic, or preventive activity toward a disease or it is inhibitory or toxic toward any disease causing agent or it is a label or marker. 13. The conjugate according to claim 12. wherein said active agent is selected from prodrugs, anticancer drugs, antineoplastic drugs, anti fungal drugs, antibacterial drugs, antiviral drugs, cardiac drugs, neurological drugs, and drugs of abuse. 14. The conjugate according to claim 12. wherein said active agent is a fluorescent label. 15. The conjugate according to claim 1 , wherein said biorecognition molecule targets to cancer cells and said active agent is an anticancer drug. 16. The conjugate according to claim 15 wherein said biorecognition molecule is an anticancer monoclonal antibody or folic acid and said anticancer drug is doxorubicin or paclitaxel. 1 7. The conjugate according to claim 1 , wherein said biorecognition molecule targets to cancer cells and said active agent is a fluorescent marker. 1 8. The conjugate according to claim 1 7, wherein said biorecognition molecule is an anticancer monoclonal antibody or folic acid and said fluorescent marker is rhodamine B. 19. The conjugate according to claim 1 , wherein the biorecognition molecule is linked to the polymer backbone of the CD-containing polymer via a linking group selected from a polyether or a polyether amine residue. 20. The conjugate according to claim 19, wherein said linking group is polyethylene glycol of MW 10-50,000 (PEG10.50.000X preferably PEGsoo-io.ooo, most preferably PEG3350 . O,O'-bis(2-aminopiOpyl)polypropylene glycol or O.(7-bis(2- aminopropyl) polypropylene glycol-ό/ocλ'-polyethyleπc glycol-ό/ocA-polypropylene glycol.. 21 . A pharmaceutical composition comprising an active agent-cyelodextrin- biorecognition molecule conjugate as defined in claim 1 . 22. A cyclodextrin-biorecognilion molecule compound, wherein: (i) said cyclodextrin (CD) is a CD-containing polymer comprising one or more CD residues, said polymer is selected from a peptide, a polypeptide, an oligonucleotide or a polynucleotide, the peptide or polypeptide comprises at least one amino acid residue containing a functional side group and at least one of the CD residues is linked covalently to said functional side group or to the sugar moiety of a nucleotide residue of said oligonucleotide or polynucleotide; and (ii) said biorecognition molecule is covalently bonded directly or via a spacer to the polymer backbone of the CD- containing polymer.
法律状态
(WO200901364) LEGAL DETAILS FOR WO2009001364  Actual or expected expiration date=2010-12-28    Legal state=DEAD    Status=LAPSED     Event publication date=2008-06-29  Event code=WO/APP  Event indicator=Pos  Event type=Examination events  Application details  Application country=WO WOIL2008000884  Application date=2008-06-29  Standardized application number=2008WO-IL00884     Event publication date=2008-12-31  Event code=WO/A2  Event type=Examination events  International application published without international search report  Publication country=WO  Publication number=WO2009001364  Publication stage Code=A2  Publication date=2008-12-31  Standardized publication number=WO200901364     Event publication date=2010-02-18  Event code=WO/A3  Event indicator=Pos  Event type=Examination events  Later publication of ISR with revised front page  Publication country=WO  Publication number=WO2009001364  Publication stage Code=A3  Publication date=2010-02-18  Standardized publication number=WO200901364     Event publication date=2010-12-28  Event code=WO/EETL  Event type=Event indicating Not In Force  PCT Application validity period expired. LEGAL DETAILS FOR DESIGNATED STATE CA2692021  Actual or expected expiration date=2013-07-02    Legal state=DEAD    Status=LAPSED   Corresponding cc:  Designated or member state=CA Corresponding appl: CA2692021  Application date in the designated or member state=2008-06-29   Application number in the designated or member state=2008CA-2692021 Corresponding cc:  Designated or member state=CA Corresponding pat: CA2692021  Publication stage code in the designated or member state=A1  Publication date in the designated or member state=2008-12-31   Publication number in the designated or member state=CA2692021    Event publication date=2009-12-24  Event code=WO/WWE  Event indicator=Pos  Event type=Entry into national phase  Wipo information: entry into national phase Corresponding cc:  Designated or member state=CA     Event publication date=2013-08-27  Event code=CA/STCHG  Patent Status changed by the national office Corresponding cc:  Designated or member state=CA  LEGAL DETAILS FOR DESIGNATED STATE DE  Actual or expected expiration date=2009-12-29    Legal state=DEAD    Status=LAPSED   Corresponding cc:  Designated or member state=DE     Event publication date=2009-12-29  Event code=WO/NENP  Event type=Event indicating Not In Force  Non-entry into the national phase in: Corresponding cc:  Designated or member state=DE  LEGAL DETAILS FOR DESIGNATED STATE EP2170054  Actual or expected expiration date=2013-01-03    Legal state=DEAD    Status=LAPSED   Corresponding cc:  Designated or member state=EP Corresponding appl: EP08763640  Application date in the designated or member state=2008-06-29   Application number in the designated or member state=2008EP-0763640 Corresponding cc:  Designated or member state=EP Corresponding pat: EP2170054  Publication stage code in the designated or member state=A2  Publication date in the designated or member state=2010-04-07   Publication number in the designated or member state=EP2170054    Event publication date=2009-02-25  Event code=WO/121  Event type=Designated states  EP: The EPO has been informed by wipo that ep was designated in this application Corresponding cc:  Designated or member state=EP     Event publication date=2013-06-26  Event code=EP/STCHG  Patent Status changed by the national office Corresponding cc:  Designated or member state=EP  LEGAL DETAILS FOR DESIGNATED STATE IL202849  Actual or expected expiration date=2016-08-01    Legal state=DEAD    Status=LAPSED   Corresponding cc:  Designated or member state=IL Corresponding appl: IL20284909  Application date in the designated or member state=2008-06-29   Application number in the designated or member state=2008IL-0202849 Corresponding cc:  Designated or member state=IL Corresponding pat: IL202849  Publication stage code in the designated or member state=A  Publication date in the designated or member state=2011-08-01   Publication number in the designated or member state=IL-202849    Event publication date=2011-08-01  Event code=IL/STCHG  Patent Status changed by the national office Corresponding cc:  Designated or member state=IL  LEGAL DETAILS FOR DESIGNATED STATE US2010226987  Actual or expected expiration date=2012-09-28    Legal state=DEAD    Status=LAPSED   Corresponding cc:  Designated or member state=US Corresponding appl: US66693908  Application date in the designated or member state=2008-06-29   Application number in the designated or member state=2008US-12666939 Corresponding cc:  Designated or member state=US Corresponding pat: US2010226987  Publication stage code in the designated or member state=A1  Publication date in the designated or member state=2010-09-09   Publication number in the designated or member state=US20100226987    Event publication date=2010-05-06  Event code=WO/WWE  Event indicator=Pos  Event type=Entry into national phase  Wipo information: entry into national phase Corresponding cc:  Designated or member state=US     Event publication date=2012-09-28  Event code=US/STCHG  Patent Status changed by the national office Corresponding cc:  Designated or member state=US
专利类型码
A2A3
国别省市代码
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