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1. 发明授权

US07875612B2 Folate mimetics and folate-receptor binding conjugates thereof 有权
标题翻译：叶酸模拟物和叶酸受体结合结合物
公开(公告)号：US07875612B2
公开(公告)日：2011-01-25
申请号：US10475876
申请日：2002-04-24
申请人： Mark A. Green , Chun-Yen Ke , Christopher P. Leamon
发明人： Mark A. Green , Chun-Yen Ke , Christopher P. Leamon
IPC分类号： A01N43/64 , A01N43/58 , A01N43/60 , A01N43/90 , A61K31/53 , A61K31/50 , A61K31/495 , A61K31/519 , C07D253/08 , C07D487/00 , C07D475/00
CPC分类号： C07D475/04 , A61K31/519 , A61K51/0497
摘要： A cell population expressing folate receptors is selectively targeted with a non-peptide folic acid analogue. The non-peptide folic acid analogue is conjugated to a diagnostic or therapeutic agent to enable selective delivery of the agent to the targeted cell population.
摘要翻译：表达叶酸受体的细胞群体选择性地用非肽叶酸类似物靶向。非肽叶酸类似物与诊断或治疗剂缀合以使得药剂能够选择性递送至靶细胞群体。

2. 发明申请

US20110028714A1 FOLATE MIMETICS AND FOLATE-RECEPTOR BINDING CONJUGATES THEREOF 有权
标题翻译： FOLATE与其结合的物质和功能受体结合
公开(公告)号：US20110028714A1
公开(公告)日：2011-02-03
申请号：US12775824
申请日：2010-05-07
申请人： Mark A. Green , Chun-Yen Ko , Christopher P. Leamon
发明人： Mark A. Green , Chun-Yen Ko , Christopher P. Leamon
IPC分类号： C07D475/04
CPC分类号： C07D475/04 , A61K31/519 , A61K51/0497
摘要： A cell population expressing folate receptors is selectively targeted with a folate mimetic. The folate mimetic is conjugated to a diagnostic or therapeutic agent to enable selective delivery of the agent to the targeted cell population.
摘要翻译：表达叶酸受体的细胞群体选择性地用叶酸盐模拟物靶向。叶酸酯模拟物与诊断或治疗剂缀合以使得药剂能够选择性递送至靶细胞群体。

3. 发明授权

US07128893B2 Vitamin-targeted imaging agents 有权
标题翻译：维生素靶向成像剂
公开(公告)号：US07128893B2
公开(公告)日：2006-10-31
申请号：US10430519
申请日：2003-05-06
申请人： Christopher P. Leamon , Matthew A. Parker
发明人： Christopher P. Leamon , Matthew A. Parker
IPC分类号： A61K49/00
CPC分类号： A61K51/08 , A61K47/54 , A61K47/551 , A61K51/025 , A61K51/0402 , A61K51/0459 , A61K51/0497 , A61K51/088
摘要： The invention relates to compounds and methods for targeting radionuclide-based imaging agents to cells having receptors for a vitamin, or vitamin receptor binding derivative or analog thereof, by using such a vitamin as the targeting ligand for the imaging agent. The invention provides a compound of the formula for use in such methods. In the compound, V is a vitamin that is a substrate for receptor-mediated transmembrane transport in vivo, or a vitamin receptor binding derivative or analog thereof, L is a divalent linker, R is a side chain of an amino acid, M is a cation of a radionuclide, n is 1 or 0, K is 1 or 0, and the compound can be in a pharmaceutically acceptable carrier therefor. The vitamin-based compounds can be used to target radionuclides to cells, such as a variety of tumor cell types, for use in diagnostic imaging of the targeted cells.
摘要翻译：本发明涉及通过使用这样的维生素作为成像剂的靶向配体，将基于放射性核素的成像剂靶向具有维生素或维生素受体结合衍生物或其类似物的受体的细胞的化合物和方法。本发明提供了用于这些方法的式的化合物。在化合物中，V是作为体内受体介导的跨膜转运的底物的维生素或维生素受体结合衍生物或其类似物，L是二价连接基，R是氨基酸的侧链，M是放射性核素的阳离子，n为1或0，K为1或0，并且该化合物可以在其药学上可接受的载体中。基于维生素的化合物可用于将放射性核素靶向细胞，例如各种肿瘤细胞类型，用于靶向细胞的诊断成像。

4. 发明授权

US08105568B2 Vitamin receptor binding drug delivery conjugates 有权
标题翻译：维生素受体结合药物递送缀合物
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
IPC分类号： A61K51/00 , A61M36/14
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。

5. 发明授权

US07910594B2 Vitamin-mitomycin conjugates 失效
标题翻译：维生素丝裂霉素缀合物
公开(公告)号：US07910594B2
公开(公告)日：2011-03-22
申请号：US10513372
申请日：2003-05-13
申请人： Iontcho Radoslavov Vlahov , Christopher P. Leamon
发明人： Iontcho Radoslavov Vlahov , Christopher P. Leamon
IPC分类号： A61K31/40 , A61K51/00 , A61P35/00 , A61M36/14 , C07D487/14
CPC分类号： C07D475/04 , A61K47/551
摘要： This invention relates to vitamin-mitomycin conjugates, to a method of using the conjugates to selectively eliminate a population of pathogenic cells in a host animal harboring the pathogenic cells, and to a method of preparation of the conjugates. The conjugate is of the general formula B-L-X wherein the group B is a vitamin, or an analog or a derivative thereof, that binds to a surface accessible vitamin receptor that is uniquely expressed, overexpressed, or preferentially expressed by a population of pathogenic cells, wherein the group L comprises a cleavable linker, and wherein the group X comprises a mitomycin compound, or an analog or a derivative thereof. An additional therapeutic agent, such as a chemotherapeutic agent, can be administered in combination with the conjugate.
摘要翻译：本发明涉及维生素丝裂霉素缀合物，涉及一种使用该缀合物选择性地消除携带致病细胞的宿主动物中的病原细胞群的方法，以及该缀合物的制备方法。缀合物是通式BLX，其中B组是维生素或其类似物或衍生物，其结合表达可获得的维生素受体，所述维生素受体是唯一表达，过表达或优先由病原细胞群体表达的，其中组L包含可切割的接头，并且其中组X包含丝裂霉素化合物或其类似物或衍生物。可以与缀合物组合施用另外的治疗剂，例如化学治疗剂。

6. 发明申请

US20100004276A1 VITAMIN RECEPTOR BINDING DRUG DELIVERY CONJUGATES 有权
标题翻译：维生素B受体结合药物联合用药
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。

7. 发明授权

US07601332B2 Vitamin receptor binding drug delivery conjugates 有权
标题翻译：维生素受体结合药物递送缀合物
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
IPC分类号： A61K51/00 , A61M36/14
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。

8. 发明授权

US08313728B2 Vitamin-targeted imaging agents 有权
标题翻译：维生素靶向成像剂
公开(公告)号：US08313728B2
公开(公告)日：2012-11-20
申请号：US12558163
申请日：2009-09-11
申请人： Christopher P. Leamon , Matthew A. Parker
发明人： Christopher P. Leamon , Matthew A. Parker
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： A61K51/08 , A61K47/54 , A61K47/551 , A61K51/025 , A61K51/0402 , A61K51/0459 , A61K51/0497 , A61K51/088
摘要： The invention relates to compounds and methods for targeting radionuclide-based imaging agents to cells having receptors for a vitamin, or vitamin receptor binding derivative or analog thereof, by using such a vitamin as the targeting ligand for the imaging agent. The invention provides a compound of the formula for use in such methods. In the compound, V is a vitamin that is a substrate for receptor-mediated transmembrane transport in vivo, or a vitamin receptor binding derivative or analog thereof, L is a divalent linker, R is a side chain of an amino acid of the formula H2NCHRCOOH, M is a cation of a radionuclide, n is 1 or 0, K is 1 or 0, and the compound can be in a pharmaceutically acceptable carrier therefor. The vitamin-based compounds can be used to target radionuclides to cells, such as a variety of tumor cell types, for use in diagnostic imaging of the targeted cells.
摘要翻译：本发明涉及通过使用这样的维生素作为成像剂的靶向配体，将基于放射性核素的成像剂靶向具有维生素或维生素受体结合衍生物或其类似物的受体的细胞的化合物和方法。本发明提供了用于这些方法的式的化合物。在化合物中，V是作为体内受体介导的跨膜转运的底物的维生素或维生素受体结合衍生物或其类似物，L是二价连接基，R是式H2NCHRCOOH的氨基酸的侧链 M是放射性核素的阳离子，n为1或0，K为1或0，该化合物可以是药学上可接受的载体。基于维生素的化合物可用于将放射性核素靶向细胞，例如各种肿瘤细胞类型，用于靶向细胞的诊断成像。

9. 发明申请

US20120065149A1 Vitamin receptor binding drug delivery conjugates 审中-公开
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.

10. 发明授权

US07872145B2 Aziridinyl-epothilone compounds 有权
标题翻译：氮丙啶基 - 埃坡霉素化合物
公开(公告)号：US07872145B2
公开(公告)日：2011-01-18
申请号：US11753785
申请日：2007-05-25
申请人： Gregory D. Vite , Francis Y. Lee , Christopher P. Leamon , Iontcho R. Vlahov
发明人： Gregory D. Vite , Francis Y. Lee , Christopher P. Leamon , Iontcho R. Vlahov
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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