公开(公告)号：US20100004276A1

公开(公告)日：2010-01-07

申请号：US12501283

申请日：2009-07-10

Applicant: Iontcho R. Vlahov ,  Christopher P. Leamon ,  Matthew A. Parker ,  Stephen J. Howard ,  Hari Krishna Santhapuram ,  Apparao Satyam ,  Joseph Anand Reddy

Inventor： Iontcho R. Vlahov ,  Christopher P. Leamon ,  Matthew A. Parker ,  Stephen J. Howard ,  Hari Krishna Santhapuram ,  Apparao Satyam ,  Joseph Anand Reddy

IPC: A61K47/48 ,  A61K31/4745 ,  A61P35/00

CPC classification number: A61K47/48569 ,  A61K47/48384 ,  A61K47/484 ,  A61K47/48715 ,  A61K47/551 ,  A61K47/65 ,  A61K47/6803 ,  A61K47/6807 ,  A61K47/6851 ,  A61K47/6889 ,  C07K16/30 ,  C07K2317/55

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07601332B2

公开(公告)日：2009-10-13

申请号：US10765336

申请日：2004-01-27

Applicant: Iontcho R. Vlahov ,  Christopher P. Leamon ,  Matthew A. Parker ,  Stephen J. Howard ,  Hari Krishna Santhapuram ,  Apparao Satyam ,  Joseph Anand Reddy

Inventor： Iontcho R. Vlahov ,  Christopher P. Leamon ,  Matthew A. Parker ,  Stephen J. Howard ,  Hari Krishna Santhapuram ,  Apparao Satyam ,  Joseph Anand Reddy

IPC: A61K51/00 ,  A61M36/14

CPC classification number: A61K47/48569 ,  A61K47/48384 ,  A61K47/484 ,  A61K47/48715 ,  A61K47/551 ,  A61K47/65 ,  A61K47/6803 ,  A61K47/6807 ,  A61K47/6851 ,  A61K47/6889 ,  C07K16/30 ,  C07K2317/55

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20050002942A1

公开(公告)日：2005-01-06

申请号：US10765336

申请日：2004-01-27

Applicant: Iontcho Vlahov ,  Christopher Leamon ,  Matthew Parker ,  Stephen Howard ,  Hari Santhapuram ,  Apparao Satyam ,  Joseph Reddy

Inventor： Iontcho Vlahov ,  Christopher Leamon ,  Matthew Parker ,  Stephen Howard ,  Hari Santhapuram ,  Apparao Satyam ,  Joseph Reddy

IPC: A61K20060101 ,  A61K39/395 ,  A61K51/00 ,  A61K51/08 ,  A61M36/14 ,  C07K16/46

CPC classification number: A61K47/48569 ,  A61K47/48384 ,  A61K47/484 ,  A61K47/48715 ,  A61K47/551 ,  A61K47/65 ,  A61K47/6803 ,  A61K47/6807 ,  A61K47/6851 ,  A61K47/6889 ,  C07K16/30 ,  C07K2317/55

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US5545621A

公开(公告)日：1996-08-13

申请号：US130736

申请日：1993-10-01

Applicant: Lawrence M. Kauvar ,  Matthew H. Lyttle ,  Apparao Satyam

Inventor： Lawrence M. Kauvar ,  Matthew H. Lyttle ,  Apparao Satyam

IPC: A61K38/00 ,  A61K38/06 ,  C07K5/02 ,  C07K5/037 ,  G01N30/02 ,  G01N33/573 ,  G01N33/574 ,  C07K5/023

CPC classification number: A61K38/06 ,  C07K5/0215 ,  G01N33/573 ,  G01N33/57496 ,  G01N2333/91177 ,  G01N30/02

Abstract: Compounds of the formula: ##STR1## or the amides, esters or salts thereof, wherein: L is an electron withdrawing leaving group;S.sup.x is S=O, O=S=O, S=NH, HN=S=O, Se=O, O=Se=O, Se=NH, HN=Se=O, S+R.sup.4 wherein R.sup.4 is alkyl (1-6 C), or O--C=O or HN--C=O;each R of R.sup.1, R.sup.2 and R.sup.3 is independently H or a noninterfering substituent;n is 0, 1 or 2;Y is selected from the group consisting of ##STR2## wherein m is 1 or 2; and AA.sub.C is an amino acid linked through a peptide bond to the remainder of said compound of formula 1, are dislosed.These compounds are useful prodrugs for selective treatment of target tissues which contain compatible glutathione S-transferase (GST) isoenzymes.

Abstract translation: 下式的化合物：其中：L是吸电子离去基团; S x为S = O，O = S = O，S = NH，HN = S = O，Se = O，O = Se = O，Se = NH，HN = Se = O，S + 1-6C），或OC = O或HN-C = O; R 1，R 2和R 3的每个R独立地为H或非干扰取代基; n为0,1或2; Y选自 ，其中m为1或2; 并且AAC是通过肽键与所述式1的化合物的其余部分连接的氨基酸被断开。 这些化合物是用于选择性治疗含有相容的谷胱甘肽S-转移酶（GST）同工酶的靶组织的有用的前药。