公开(公告)号：WO2012158960A3

公开(公告)日：2012-11-22

申请号：PCT/US2012/038425

申请日：2012-05-17

Applicant: H. LEE MOFFITT CANCER CENTER & RESEARCH INSTITUTE, INC. ,  INTEZYNE TECHNOLOGIES INC. ,  ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA ,  BOARD OF REGENTS, UNIVERSITY OF TEXAS SYSTEM ,  GILLIES, Robert, J. ,  MORSE, David, L. ,  BARKEY, Natalie, M. ,  SILL, Kevin, N. ,  VAGNER, Josef ,  TAFRESHI, Narges, K. ,  SESSLER, Jonathan, L. ,  PREIHS, Christian

Inventor： GILLIES, Robert, J. ,  MORSE, David, L. ,  BARKEY, Natalie, M. ,  SILL, Kevin, N. ,  VAGNER, Josef ,  TAFRESHI, Narges, K. ,  SESSLER, Jonathan, L. ,  PREIHS, Christian

IPC: C07K7/06 ,  C07K7/08 ,  C07K5/10 ,  A61K38/08 ,  A61K38/10 ,  A61K9/127 ,  G01N33/574 ,  A61P35/00

Abstract: The subject invention pertains to a modified MCIR peptide ligand comprising a peptide that is a melanocortin 1 receptor (MCIR) ligand and a functionality or linker, such as a click functionality, for conjugation to a surface or agent. The modified MCIR peptide ligand can be coupled, e.g. , via a click reaction with a complementary click functionality attached, to a moiety to form an MClR-targeted agent. Drugs, contrast agents, polymers, particles, micelles, surfaces of larger structures, or other moieties can be targeted to the MCIR. The subject invention also pertains to a MCIR peptide ligand-micelle complex comprising a peptide that is a melanocortin 1 receptor ligand connected via a click reaction product to a micelle. The micelle is stable in vivo and can target melanoma tumor cells by association of the peptide ligand with the MCIR or the tumor and selectively provide a detectable and/or therapeutic agent (such as an imageable contrast agent and/or anti-cancer agent) selectively to the tumor cell.

公开(公告)号：WO2003009940A2

公开(公告)日：2003-02-06

申请号：PCT/US2002/023489

申请日：2002-07-24

Applicant: HIGH THROUGHPUT GENOMICS, INC. ,  KRCHNAK, Viktor ,  VAGNER, Josef ,  SELIGMANN, Bruce, A.

Inventor： KRCHNAK, Viktor ,  VAGNER, Josef ,  SELIGMANN, Bruce, A.

IPC: B01L

CPC classification number: B01J19/0046 ,  B01L3/02 ,  B01L3/502

Abstract: A sorting apparatus and method for directed sort combinatorial chemical synthesis is provided. This invention relates to a directed flexible, sorting apparatus and method for combinatorial chemical synthesis using a directed split and recombine process. The process utilizes one algorithm that is universal in directing and sorting a library of any size. This invention further provides a method of sorting solid supports for combinatorial chemical synthesis comprising delivering one or more supports which are organized in a one dimensional linear array in one or more reaction vessels, to an isolation and transfer chamber, transferring one or more support from each of said reaction vessels to one or more subsequent reaction vessels, in a patterned distribution; wherein the patterned distribution of supports in each subsequent transfer is identical and the position of each support in a reaction vessel codes for its previous synthesis history. In another aspect, the invention provides a directed sort apparatus wherein all members of a set at a given point in time are reacted with the same chemical building blocks throughout synthesis.

Abstract translation: 提供了一种用于定向分类组合化学合成的分选设备和方法。 本发明涉及一种使用定向拆分和重组方法进行组合化学合成的定向柔性分选装置和方法。 该过程利用一种通用的方法来指导和排序任何大小的库。 本发明还提供了一种分选用于组合化学合成的固体支持物的方法，包括将一个或多个以一维线性阵列组织在一个或多个反应容器中的支撑物输送到隔离和转移室，从每个 的所述反应容器在一个或多个随后的反应容器中以图案化分布; 其中在每个随后的转移中支持体的图案化分布是相同的，并且反应容器中每个载体的位置编码其先前的合成历史。 另一方面，本发明提供一种定向分类装置，其中在给定时间点的一组的所有成员在整个合成中与相同的化学结构单元反应。

公开(公告)号：WO2013036543A3

公开(公告)日：2013-05-02

申请号：PCT/US2012053813

申请日：2012-09-05

Applicant: H LEE MOFFITT CANCER CT & RES ,  UNIV ARIZONA STATE ,  MORSE DAVID L ,  GILLIES ROBERT J ,  HUYNH AMANDA ,  VAGNER JOSEF

Inventor： MORSE DAVID L ,  GILLIES ROBERT J ,  HUYNH AMANDA ,  VAGNER JOSEF

IPC: A61K49/10 ,  A61K49/06 ,  A61K49/14 ,  A61P35/00

CPC classification number: A61K49/0056 ,  A61K49/0021 ,  C07K7/06 ,  C07K7/08

Abstract: Cellular targets on cancer cells have been identified that can be used with targeted molecular imaging to detect the cancer cells in vivo. Non-invasive methods for detecting cancer cells, such as metastasized cancer cells, are therefore provided. Also provided are compositions and kits for use in the disclosed methods.

Abstract translation: 已经鉴定出癌细胞上的细胞靶标可用于靶向分子成像以检测体内的癌细胞。 因此，提供了用于检测癌细胞的非侵入性方法，例如转移的癌细胞。 还提供了用于所公开的方法中的组合物和试剂盒。

公开(公告)号：WO2013036543A2

公开(公告)日：2013-03-14

申请号：PCT/US2012/053813

申请日：2012-09-05

Applicant: H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC. ,  ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA ,  MORSE, David, L. ,  GILLIES, Robert, J. ,  HUYNH, Amanda ,  VAGNER, Josef

Inventor： MORSE, David, L. ,  GILLIES, Robert, J. ,  HUYNH, Amanda ,  VAGNER, Josef

IPC: A61K49/10

CPC classification number: A61K49/0056 ,  A61K49/0021 ,  C07K7/06 ,  C07K7/08

Abstract: Cellular targets on cancer cells have been identified that can be used with targeted molecular imaging to detect the cancer cells in vivo . Non-invasive methods for detecting cancer cells, such as metastasized cancer cells, are therefore provided. Also provided are compositions and kits for use in the disclosed methods.

Abstract translation: 已经鉴定了癌细胞上的细胞靶标，其可用于靶向分子成像以检测体内癌细胞。 因此提供了用于检测癌细胞的非侵入性方法，例如转移的癌细胞。 还提供了用于所公开方法的组合物和试剂盒。

公开(公告)号：WO2003009940A3

公开(公告)日：2003-02-06

申请号：PCT/US2002/023489

申请日：2002-07-24

Applicant: HIGH THROUGHPUT GENOMICS, INC. ,  KRCHNAK, Viktor ,  VAGNER, Josef ,  SELIGMANN, Bruce, A.

Inventor： KRCHNAK, Viktor ,  VAGNER, Josef ,  SELIGMANN, Bruce, A.

IPC: G01N31/00

Abstract: A sorting apparatus and method for directed sort combinatorial chemical synthesis is provided. This invention relates to a directed flexible, sorting apparatus and method for combinatorial chemical synthesis using a directed split and recombine process. The process utilizes one algorithm that is universal in directing and sorting a library of any size. This invention further provides a method of sorting solid supports for combinatorial chemical synthesis comprising delivering one or more supports which are organized in a one dimensional linear array in one or more reaction vessels, to an isolation and transfer chamber, transferring one or more support from each of said reaction vessels to one or more subsequent reaction vessels, in a patterned distribution; wherein the patterned distribution of supports in each subsequent transfer is identical and the position of each support in a reaction vessel codes for its previous synthesis history. In another aspect, the invention provides a directed sort apparatus wherein all members of a set at a given point in time are reacted with the same chemical building blocks throughout synthesis.

公开(公告)号：WO2012158960A2

公开(公告)日：2012-11-22

申请号：PCT/US2012038425

申请日：2012-05-17

Applicant: H LEE MOFFITT CANCER CT & RES ,  INTEZYNE TECHNOLOGIES INC ,  UNIV ARIZONA STATE ,  UNIV TEXAS ,  GILLIES ROBERT J ,  MORSE DAVID L ,  BARKEY NATALIE M ,  SILL KEVIN N ,  VAGNER JOSEF ,  TAFRESHI NARGES K ,  SESSLER JONATHAN L ,  PREIHS CHRISTIAN

Inventor： GILLIES ROBERT J ,  MORSE DAVID L ,  BARKEY NATALIE M ,  SILL KEVIN N ,  VAGNER JOSEF ,  TAFRESHI NARGES K ,  SESSLER JONATHAN L ,  PREIHS CHRISTIAN

CPC classification number: C07K5/1024 ,  A61K38/34 ,  A61K47/48246 ,  A61K47/488 ,  A61K47/64 ,  A61K47/6907 ,  A61K49/0056 ,  A61K49/101 ,  A61K49/1809 ,  C07K7/08 ,  C07K14/68 ,  C07K14/723

Abstract: The subject invention pertains to a modified MCIR peptide ligand comprising a peptide that is a melanocortin 1 receptor (MCIR) ligand and a functionality or linker, such as a click functionality, for conjugation to a surface or agent. The modified MCIR peptide ligand can be coupled, e.g., via a click reaction with a complementary click functionality attached, to a moiety to form an MClR-targeted agent. Drugs, contrast agents, polymers, particles, micelles, surfaces of larger structures, or other moieties can be targeted to the MCIR. The subject invention also pertains to a MCIR peptide ligand-micelle complex comprising a peptide that is a melanocortin 1 receptor ligand connected via a click reaction product to a micelle. The micelle is stable in vivo and can target melanoma tumor cells by association of the peptide ligand with the MCIR or the tumor and selectively provide a detectable and/or therapeutic agent (such as an imageable contrast agent and/or anti-cancer agent) selectively to the tumor cell.

Abstract translation: 本发明涉及包含黑色素皮质素1受体（MCIR）配体的肽和功能性或接头，例如用于与表面或试剂缀合的点击功能的修饰的MCIR肽配体。 修饰的MCIR肽配体可以例如通过与附加的互补点击功能的点击反应偶联到部分上以形成MClR靶向试剂。 药物，造影剂，聚合物，颗粒，胶束，较大结构的表面或其它部分可以靶向MCIR。 本发明还涉及包含通过点胶反应产物与胶束连接的黑皮质素1受体配体的肽的MCIR肽配体 - 胶束复合物。 胶束在体内是稳定的并且可以通过肽配体与MCIR或肿瘤的缔合来靶向黑素瘤肿瘤细胞，并选择性地提供可检测和/或治疗剂（例如可成像的造影剂和/或抗癌剂） 到肿瘤细胞。