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公开(公告)号:US20130267522A1
公开(公告)日:2013-10-10
申请号:US13779501
申请日:2013-02-27
IPC分类号: A61K31/519
CPC分类号: A61K31/519 , A61K47/551 , A61K47/65
摘要: The invention relates to methods and uses for the treatment of a cancer. In particular, the invention relates to the use of a folate-vinca conjugate to treat urinary bladder cancer (e.g., invasive transitional cell carcinoma (InvTCC)).
摘要翻译: 本发明涉及治疗癌症的方法和用途。 特别地,本发明涉及叶酸 - 长春香缀合物治疗膀胱癌(例如侵袭性移行细胞癌(InvTCC))的用途。
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公开(公告)号:US08105568B2
公开(公告)日:2012-01-31
申请号:US12501283
申请日:2009-07-10
申请人: Iontcho R. Vlahov , Christopher P. Leamon , Matthew A. Parker , Stephen J. Howard , Hari Krishna R. Santhapuram , Apparao Satyam , Joseph A. Reddy
发明人: Iontcho R. Vlahov , Christopher P. Leamon , Matthew A. Parker , Stephen J. Howard , Hari Krishna R. Santhapuram , Apparao Satyam , Joseph A. Reddy
CPC分类号: A61K47/48569 , A61K47/48384 , A61K47/484 , A61K47/48715 , A61K47/551 , A61K47/65 , A61K47/6803 , A61K47/6807 , A61K47/6851 , A61K47/6889 , C07K16/30 , C07K2317/55
摘要: The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety includes vitamins, and vitamin receptor binding analogs and derivatives thereof, and the drug includes analogs and derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) includes components such as spacer linkers, releasable linkers, and heteroatom linkers, and combinations thereof. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.
摘要翻译: 本发明描述了维生素受体结合药物递送缀合物及其制备方法。 药物递送缀合物由维生素受体结合部分,二价连接体(L)和药物组成。 维生素受体结合部分包括维生素和维生素受体结合类似物及其衍生物,并且该药物包括其类似物及其衍生物。 维生素受体结合部分与二价连接体共价连接,药物或其类似物或衍生物与二价连接体共价连接,其中二价连接体(L)包括组分如间隔连接子,可释放接头, 和杂原子接头,及其组合。 还描述了使用药物递送缀合物消除致病细胞群的方法和药物组合物。
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公开(公告)号:US06376662B1
公开(公告)日:2002-04-23
申请号:US09142937
申请日:1998-11-17
IPC分类号: C07H704
摘要: A method for synthesizing C-glycosides of ulosonic acids such as Neu5Ac, by which diastereocontrolled synthesis of &agr;-C-glycosides of ulosonic acids is attained is disclosed. In the method of the present invention, an ulosonic acid sulfone or phosphite is reacted with an aldehyde or ketone compound in the presence of a lanthanide metal halide.
摘要翻译: 公开了用于合成诸如Neu5Ac的尿苷酸的C-糖苷的方法,通过该方法获得了关于酸性盐酸的α-C-糖苷的非对映控制合成。 在本发明的方法中,在镧系元素金属卤化物的存在下,将脲二
酸砜或亚磷酸酯与醛或酮化合物反应。-
公开(公告)号:US20120065149A1
公开(公告)日:2012-03-15
申请号:US13199654
申请日:2011-09-07
申请人: Iontcho R. Vlahov , Christopher P. Leamon , Matthew A. Parker , Stephen J. Howard , Hari Krishna Santhapuram , Apparao Satyam , Joseph Anand Reddy
发明人: Iontcho R. Vlahov , Christopher P. Leamon , Matthew A. Parker , Stephen J. Howard , Hari Krishna Santhapuram , Apparao Satyam , Joseph Anand Reddy
IPC分类号: A61K31/519 , C07D519/00 , C07H15/26 , A61K31/7068 , A61P35/00 , C07K5/083 , A61K38/06 , C07K5/103 , A61K38/07 , C07K9/00 , A61K38/14 , C07K7/06 , A61K38/08 , C07F7/10 , A61K31/695 , C07D475/04
CPC分类号: A61K47/55 , A61K47/551 , A61K47/65 , A61K47/6803 , A61K47/6807 , A61K47/6851 , A61K47/6889 , C07K16/30 , C07K2317/55
摘要: The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety includes vitamins, and vitamin receptor binding analogs and derivatives thereof, and the drug includes analogs and derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) includes components such as spacer linkers, releasable linkers, and heteroatom linkers, and combinations thereof. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.
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公开(公告)号:US07872145B2
公开(公告)日:2011-01-18
申请号:US11753785
申请日:2007-05-25
IPC分类号: C07D277/22 , C07D203/26
CPC分类号: C07D491/04 , A61K47/551 , A61K47/65
摘要: The present invention is directed to aziridinyl epothilone compounds as further described herein, and/or pharmaceutically-acceptable salts and/or solvates thereof having the following Formula: wherein K is —O—, —S—, or —NR7—; A is —(CR8R9)—(CH2)m—Z—wherein Z is —(CHR10)—, —C(═O)—, —C(═O)—C(═O)—, —OC(═O)—, —N(R11)C(═O)—, —SO2—, or —N(R11)SO2—; B1 is hydroxyl or cyano and R1 is hydrogen or B1 and R1 are taken together to form a double bond; R2, R3, and R5 are, independently, hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; or R2 and R3 may be taken together with the carbon to which they are attached to form an optionally substituted cycloalkyl; R4 is hydrogen, alkyl, alkenyl, substituted alkyl, substituted alkenyl, aryl, or substituted aryl; R6 is hydrogen, alkyl or substituted alkyl; R7, R8, R9, R10, R11 and R12 are independently hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heterocycloalkyl, substituted heterocycloalkyl, heteroaryl, or substituted heteroaryl; and R13 is aryl, substituted aryl, heteroaryl or substituted heteroaryl.
摘要翻译: 本发明涉及如本文进一步描述的氮杂环丙烷基埃坡霉素化合物和/或其药学上可接受的盐和/或溶剂合物,其具有下式:其中K是-O - , - S-或-NR 7 - ; A是 - (CR 8 R 9) - (CH 2)m-Z-,其中Z是 - (CHR 10) - , - C(= O) - , - C(= O)-C(= O) - , - OC ) - , - N(R 11)C(= O) - , - SO 2 - 或-N(R 11)SO 2 - ; B1是羟基或氰基,R1是氢或B1和R1一起形成双键; R2,R3和R5独立地是氢,烷基,取代的烷基,芳基或取代的芳基; 或者R 2和R 3可以与它们所连接的碳一起形成任选取代的环烷基; R4是氢,烷基,烯基,取代的烷基,取代的烯基,芳基或取代的芳基; R6是氢,烷基或取代的烷基; R7,R8,R9,R10,R11和R12独立地是氢,烷基,取代的烷基,环烷基,取代的环烷基,芳基,取代的芳基,杂环烷基,取代的杂环烷基,杂芳基或取代的杂芳基; 并且R 13是芳基,取代的芳基,杂芳基或取代的杂芳基。
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公开(公告)号:US20100004276A1
公开(公告)日:2010-01-07
申请号:US12501283
申请日:2009-07-10
申请人: Iontcho R. Vlahov , Christopher P. Leamon , Matthew A. Parker , Stephen J. Howard , Hari Krishna Santhapuram , Apparao Satyam , Joseph Anand Reddy
发明人: Iontcho R. Vlahov , Christopher P. Leamon , Matthew A. Parker , Stephen J. Howard , Hari Krishna Santhapuram , Apparao Satyam , Joseph Anand Reddy
IPC分类号: A61K47/48 , A61K31/4745 , A61P35/00
CPC分类号: A61K47/48569 , A61K47/48384 , A61K47/484 , A61K47/48715 , A61K47/551 , A61K47/65 , A61K47/6803 , A61K47/6807 , A61K47/6851 , A61K47/6889 , C07K16/30 , C07K2317/55
摘要: The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety includes vitamins, and vitamin receptor binding analogs and derivatives thereof, and the drug includes analogs and derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) includes components such as spacer linkers, releasable linkers, and heteroatom linkers, and combinations thereof. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.
摘要翻译: 本发明描述了维生素受体结合药物递送缀合物及其制备方法。 药物递送缀合物由维生素受体结合部分,二价连接体(L)和药物组成。 维生素受体结合部分包括维生素和维生素受体结合类似物及其衍生物,并且该药物包括其类似物及其衍生物。 维生素受体结合部分与二价连接体共价连接,药物或其类似物或衍生物与二价连接体共价连接,其中二价连接体(L)包括组分如间隔连接子,可释放接头, 和杂原子接头,及其组合。 还描述了使用药物递送缀合物消除致病细胞群的方法和药物组合物。
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公开(公告)号:US07601332B2
公开(公告)日:2009-10-13
申请号:US10765336
申请日:2004-01-27
申请人: Iontcho R. Vlahov , Christopher P. Leamon , Matthew A. Parker , Stephen J. Howard , Hari Krishna Santhapuram , Apparao Satyam , Joseph Anand Reddy
发明人: Iontcho R. Vlahov , Christopher P. Leamon , Matthew A. Parker , Stephen J. Howard , Hari Krishna Santhapuram , Apparao Satyam , Joseph Anand Reddy
CPC分类号: A61K47/48569 , A61K47/48384 , A61K47/484 , A61K47/48715 , A61K47/551 , A61K47/65 , A61K47/6803 , A61K47/6807 , A61K47/6851 , A61K47/6889 , C07K16/30 , C07K2317/55
摘要: The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety includes vitamins, and vitamin receptor binding analogs and derivatives thereof, and the drug includes analogs and derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) includes components such as spacer linkers, releasable linkers, and heteroatom linkers, and combinations thereof. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.
摘要翻译: 本发明描述了维生素受体结合药物递送缀合物及其制备方法。 药物递送缀合物由维生素受体结合部分,二价连接体(L)和药物组成。 维生素受体结合部分包括维生素和维生素受体结合类似物及其衍生物,并且该药物包括其类似物及其衍生物。 维生素受体结合部分与二价连接体共价连接,药物或其类似物或衍生物与二价连接体共价连接,其中二价连接体(L)包括组分如间隔连接子,可释放接头, 和杂原子接头,及其组合。 还描述了使用药物递送缀合物消除致病细胞群的方法和药物组合物。
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