专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US07029695B2 Therapeutic compositions containing glutathione analogs 失效
公开(公告)号：US07029695B2
公开(公告)日：2006-04-18
申请号：US09903442
申请日：2001-07-10
申请人： Thomas Redelmeier , Lawrence M. Kauvar , Robert T. Lum , Matthew H. Lyttle , Robert W. Macsata , Steven R. Schow , Hugo O. Villar , Michael R. Kozlowski
发明人： Thomas Redelmeier , Lawrence M. Kauvar , Robert T. Lum , Matthew H. Lyttle , Robert W. Macsata , Steven R. Schow , Hugo O. Villar , Michael R. Kozlowski
IPC分类号： A61K9/127 , A61K38/06 , C07K5/08
CPC分类号： A61K9/1075 , A61K9/127 , A61K38/063
摘要： Pharmaceutical compositions and methods of using them. Lipid formulations of a glutathione analog and methods of manufacturing them. Their use to stimulate hematopoiesis, protect hematopoietic cells from damage caused by radiation or chemotherapy, or potentiate the stimulatory action of one or a combination of cytokines on colony formation by hematopoietic progenitor cells, protect a subject from a destructive effect of a chemotherapeutic agent or irradiation, or to potentiate the effect of a chemotherapeutic agent.

2. 发明授权

US5908919A Urethane mediated, GST specific molecular release systems 失效
标题翻译：氨基甲酸酯介导的GST特异性分子释放系统
公开(公告)号：US5908919A
公开(公告)日：1999-06-01
申请号：US476119
申请日：1995-06-07
申请人： Lawrence M. Kauvar , Matthew H. Lyttle , Apparao Satyam
发明人： Lawrence M. Kauvar , Matthew H. Lyttle , Apparao Satyam
IPC分类号： A61K38/00 , A61K38/04 , A61P35/00 , C07K5/02 , C07K5/023 , C07K5/037 , C07K5/08 , A61K38/06
CPC分类号： C07K5/0215 , A61K38/00
摘要： Compounds of the formula ##STR1## or of the formula ##STR2## or the amides, esters or salts thereof, wherein: S.sup.x is S.dbd.O, O.dbd.S.dbd.O, S.dbd.NH, HN.dbd.S.dbd.O, Se.dbd.O, O.dbd.Se.dbd.O, Se.dbd.NH, HN.dbd.Se.dbd.O, S.sup.+ R.sup.3 wherein R.sup.3 is alkyl (1-6C) or O--C.dbd.O or HN--C.dbd.O;each R of R.sup.1, and R.sup.2 is independently H or a noninterfering substituent;wherein (conj) represents a conjugated system capable of transmitting electrons;n is 0 or 1;YCO is selected from the group consisting of .gamma.-Glu, .gamma.-Glu-Gly, Glu, Glu-Gly, .beta.Asp, .beta.-Asp-Gly, Asp and Asp-Gly;AA.sub.C is an amino acid linked through a peptide bond to the remainder of said compound of Formula 1; andN(Z) represents a reduced nitrogen-containing leaving group and L represents an electron-withdrawing leaving group,are useful as prodrugs and to generate active components released by the activity of glutathione S-transferase.
摘要翻译：式或式的化合物或其酰胺，酯或盐，其中：Sx为S = O，O = S = O，S = NH，HN = S = O，Se = O，O = Se = O ，Se = NH，HN = Se = O，S + R3，其中R3是烷基（1-6C）或OC = O或HN-C = O; R 1的每个R和R 2独立地为H或非干扰取代基; 其中（conj）表示能够传输电子的共轭系统; n为0或1; YCO选自γ-Glu，γ-Glu-Gly，Glu，Glu-Gly，β-Asp，β-Asp-Gly，Asp和Asp-Gly; AAC是通过肽键与所述式1化合物的剩余部分连接的氨基酸; 并且N（Z）表示还原的含氮离去基团，L表示吸电子离去基团，可用作前药并产生通过谷胱甘肽S-转移酶活性释放的活性成分。

3. 发明授权

US5763570A Glutathione analogs and paralog panels comprising glutathione mimics 失效
标题翻译：谷胱甘肽类似物和包含谷胱甘肽模拟物的旁系同源片段
公开(公告)号：US5763570A
公开(公告)日：1998-06-09
申请号：US473397
申请日：1995-06-07
申请人： Lawrence M. Kauvar , Matthew H. Lyttle
发明人： Lawrence M. Kauvar , Matthew H. Lyttle
IPC分类号： A61K38/00 , A61K38/06 , C07K5/02 , C07K5/037 , C07K7/06 , C07K7/08 , C07K7/56 , C07K16/00 , C07K16/30 , C07K16/44 , C12N9/10 , G01N30/00 , G01N30/02 , G01N33/53 , G01N33/573 , G01N33/574 , G01N33/68 , C07K5/08
CPC分类号： C12N9/1088 , A61K38/06 , C07K16/00 , C07K16/30 , C07K16/44 , C07K5/0215 , C07K7/06 , C07K7/08 , C07K7/56 , G01N33/53 , G01N33/573 , G01N33/57496 , G01N33/68 , G01N33/6878 , G01N2030/027 , G01N2333/91177 , G01N30/00 , G01N30/02 , G01N30/48 , Y10S435/814
摘要： Compounds of the formula ##STR1## or the alkyl (1-6C), alkenyl (1-6C), or arylalkyl (7-12C) amides or salts including the cycloamido forms thereof; wherein n is 1 or 2; wherein when n is 1, X is a mono- or disubstituted or unsubstituted hydrocarbyl (1-20C) moiety optionally containing 1 or 2 nonadjacent heteroatoms (O, S or N), and wherein said substitution is selected from the group consisting of halo, OR, and SR, wherein R is H or lower alkyl (1-4C); when n is 2, one X is as above defined and the other X is lower alkyl (1-4C); Y is selected from the group consisting of ##STR2## wherein m is 1 or 2; and AA.sub.C is an amino acid coupled through a peptide bond to the remainder of the compound of formula 1, are useful as affinity ligands, elution reagents, solution inhibitors, diagnostic reagents and therapeutics. These compounds and analogous tripeptide glutathione analogs can be used as members of panels to obtain specific characteristic profiles for various glutathione-S-transferases.
摘要翻译：式（1）的化合物或烷基（1-6C），烯基（1-6C）或芳烷基（7-12C）酰胺或包括其环酰胺基的盐; 其中n为1或2; 其中当n为1时，X为任选含有1或2个不相邻杂原子（O，S或N）的单取代或未取代的烃基（1-20C）部分，并且其中所述取代选自卤素， OR和SR，其中R是H或低级烷基（1-4C）; 当n为2时，一个X如上定义，另一个X为低级烷基（1-4C）; Y选自，其中m为1或2; 并且AAC是通过肽键与式1化合物的其余部分偶联的氨基酸，可用作亲和配体，洗脱试剂，溶液抑制剂，诊断试剂和治疗剂。这些化合物和类似的三肽谷胱甘肽类似物可用作面板的成员以获得各种谷胱甘肽-S-转移酶的特定特征。

4. 发明授权

US5556942A Glutathione S-transferase-activated compounds 失效
标题翻译：谷胱甘肽S-转移酶活化化合物
公开(公告)号：US5556942A
公开(公告)日：1996-09-17
申请号：US309005
申请日：1994-09-19
申请人： Lawrence M. Kauvar , Matthew H. Lyttle , Apparao Satyam
发明人： Lawrence M. Kauvar , Matthew H. Lyttle , Apparao Satyam
IPC分类号： A61K38/00 , A61K38/06 , A61P31/12 , A61P35/00 , A61P43/00 , C07K5/02 , C07K5/037 , C12N9/10 , G01N30/02 , G01N33/573 , G01N33/574 , C07K5/083
CPC分类号： A61K38/06 , C07K5/0215 , C12N9/1088 , G01N33/573 , G01N33/57496 , G01N2333/91177 , G01N30/02
摘要： 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.dbd.O, O.dbd.S.dbd.O, S.dbd.NH, HN.dbd.S.dbd.O, Se.dbd.O, O.dbd.Se.dbd.O, Se.dbd.NH, HN.dbd.Se.dbd.O, S.sup.+ R.sup.4 wherein R.sup.4 is alkyl (1-6C), or O--C.dbd.O or HN--C.dbd.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 disclosed.These compounds are useful prodrugs for selective treatment of target tissues which contain compatible glutathione S-transferase (GST) isoenzymes, and simultaneously elevate the levels of GM progenitor cells in bone marrow.
摘要翻译：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选自和，其中m为1或2; 并且AAC是通过肽键与所述式1化合物的其余部分连接的氨基酸。这些化合物是用于选择性处理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，并且同时提高骨髓中GM祖细胞的水平。

5. 发明授权

US5955432A Metabolic effects of certain glutathione analogs 失效
标题翻译：某些谷胱甘肽类似物的代谢作用
公开(公告)号：US5955432A
公开(公告)日：1999-09-21
申请号：US675095
申请日：1996-07-03
申请人： Lawrence M. Kauvar , Amy S. Morgan , Matthew H. Lyttle , Richard F. Borch
发明人： Lawrence M. Kauvar , Amy S. Morgan , Matthew H. Lyttle , Richard F. Borch
IPC分类号： A61K38/06 , C07K5/037 , G01N30/02 , C07K5/08
CPC分类号： A61K38/06 , G01N30/02
摘要： Compounds of the formula ##STR1## and the esters, amides, amide/esters and salts thereof, wherein YCO is .gamma.-glu or .beta.-asp;G* is phenylglycine or glycine;Z is CH.sub.2, O or S; andX is a hydrocarbon radical selected from C.sub.6 -C.sub.8 alkyl or selected aromatic groupsare useful in modulating hematopoiesis in bone marrow, mitigating the bone-marrow-destructive effects of a chemotherapeutic agent, and in potentiating the toxicity of chemotherapeutic agents.
摘要翻译：式的化合物及其酯，酰胺，酰胺/酯和盐，其中YCO是γ-Glu或β-asp; G *是苯基甘氨酸或甘氨酸; Z是CH 2，O或S; X是选自C 6 -C 8烷基或所选芳族基团的烃基可用于调节骨髓造血，减轻化疗剂的骨髓破坏作用，以及增强化学治疗剂的毒性。

6. 发明授权

US6013462A Glutathione analogs as reagents 失效
标题翻译：谷胱甘肽类似物作为试剂
公开(公告)号：US6013462A
公开(公告)日：2000-01-11
申请号：US792996
申请日：1997-02-03
申请人： Lawrence M. Kauvar , Matthew H. Lyttle
发明人： Lawrence M. Kauvar , Matthew H. Lyttle
IPC分类号： A61K38/00 , A61K38/06 , C07K5/02 , C07K5/037 , C07K7/06 , C07K7/08 , C07K7/56 , C07K16/00 , C07K16/30 , C07K16/44 , C12N9/10 , G01N30/00 , G01N30/02 , G01N33/53 , G01N33/573 , G01N33/574 , G01N33/68 , C07K5/00
CPC分类号： C12N9/1088 , A61K38/06 , C07K16/00 , C07K16/30 , C07K16/44 , C07K5/0215 , C07K7/06 , C07K7/08 , C07K7/56 , G01N33/53 , G01N33/573 , G01N33/57496 , G01N33/68 , G01N33/6878 , G01N2030/027 , G01N2333/91177 , G01N30/00 , G01N30/02 , G01N30/48 , Y10S435/814
摘要： Compounds of the formula ##STR1## or the alkyl (1-6C), alkenyl (1-6C), or arylalkyl (7-12C) amides or salts including the cycloamido forms thereof;whereinn is 1 or 2;whereinwhen n is 1, X is a mono- or disubstituted or unsubstituted hydrocarbyl (1-20C) moiety optionally containing 1 or 2 nonadjacent heteroatoms (O, S or N), and wherein said substitution is selected from the group consisting of halo, OR, and SR, wherein R is H or lower alkyl (1-4C); when n is 2, one X is as above defined and the other X is lower alkyl (1-4C);Y is selected from the group consisting of ##STR2## wherein m is 1 or 2; andAA.sub.C is an amino acid coupled through a peptide bond to the remainder of the compound of formula 1, are useful as affinity ligands, elution reagents, solution inhibitors, diagnostic reagents and therapeutics. These compounds and analogous tripeptide glutathione analogs can be used as members of panels to obtain specific characteristic profiles for various glutathione-S-transferases.
摘要翻译：下式的化合物或（1-6C）烷基，（1-6C）或芳基烷基（7-12C）的酰胺或其盐，包括其环酰胺基形式; 其中n为1或2; 其中当n为1时，X为任选含有1或2个不相邻杂原子（O，S或N）的单取代或未取代的烃基（1-20C）部分，并且其中所述取代选自卤素， OR和SR，其中R是H或低级烷基（1-4C）; 当n为2时，一个X如上定义，另一个X为低级烷基（1-4C）; Y选自其中m为1或2; 并且AAC是通过肽键与式1化合物的其余部分偶联的氨基酸，可用作亲和配体，洗脱试剂，溶液抑制剂，诊断试剂和治疗剂。这些化合物和类似的三肽谷胱甘肽类似物可用作面板的成员以获得各种谷胱甘肽-S-转移酶的特定特征。

7. 发明授权

US5880097A Tethered prodrugs 失效
标题翻译：连接前药
公开(公告)号：US5880097A
公开(公告)日：1999-03-09
申请号：US582966
申请日：1996-01-04
申请人： Matthew H. Lyttle , Lawrence M. Kauvar
发明人： Matthew H. Lyttle , Lawrence M. Kauvar
IPC分类号： A61K38/00 , A61K31/00 , A61P31/00 , A61P35/00 , A61P43/00 , C07K1/10 , C07K5/02 , C07K5/037 , C07K5/08 , C07K5/10 , C07K5/023
CPC分类号： C07K5/0215 , A61K38/00
摘要： Compounds wherein a biologically active molecule is coupled to a glutathione analog through a conjugated system which permits activation of the biologically active molecule while retaining the biologically active molecule tethered to the glutathione analog are useful as tethered prodrugs that slow the rate of clearance of an active biomolecule through the multidrug resistance pump.
摘要翻译：生物活性分子通过共轭系统偶联到谷胱甘肽类似物的化合物，其允许激活生物活性分子同时保留与谷胱甘肽类似物结合的生物活性分子，同时可用作延缓活性生物分子清除速率的系留前药通过多药耐药泵。

8. 发明授权

US5786336A Target-selective protocols based on mimics 失效
标题翻译：基于模拟的目标选择性协议
公开(公告)号：US5786336A
公开(公告)日：1998-07-28
申请号：US305993
申请日：1994-09-19
申请人： Lawrence M. Kauvar , Matthew H. Lyttle , Amy S. Morgan , Richard F. Borch
发明人： Lawrence M. Kauvar , Matthew H. Lyttle , Amy S. Morgan , Richard F. Borch
IPC分类号： A61K38/00 , A61K31/195 , A61K38/06 , A61K38/07 , A61K38/45 , A61K45/08 , A61P7/06 , A61P35/00 , A61P43/00 , C07C323/60 , C07D495/14 , C07K1/06 , C07K1/10 , C07K5/02 , C07K5/023 , C07K5/037 , C07K5/08 , C07K5/093 , C07K5/10 , C07K5/113 , C07K7/06 , C12N9/10 , C12Q1/48 , G01N30/02 , G01N33/566 , G01N33/573 , G01N33/574
CPC分类号： A61K38/06 , C07K5/0215 , C12N9/1088 , G01N33/573 , G01N33/57496 , G01N2333/91177 , G01N30/02
摘要： A method to potentiate the effect of a chemotherapeutic agent in a tumor cell, which method comprises administering to said tumor cell, along with said chemotherapeutic agent, a potentiating amount of a compound of the formula: ##STR1## or an amide, ester or hybrid amide/ester thereof, wherein X is a hydrocarbon radical optionally substituted on any aromatic moiety contained therein; Y--CO is .gamma.-Glu or .beta.-Asp and AA.sub.C is an amino acid, preferably glycine, phenylglycine, .beta.-alanine, alanine or phenylalanine is disclosed. Similar compounds can also be used to selectively exert cytotoxicity versus target cells as compared to nontarget cells and also to elevate the production of GM progenitors in bone marrow of mammalian subjects.
摘要翻译：一种加强化学治疗剂在肿瘤细胞中的作用的方法，该方法包括与所述化学治疗剂一起向所述肿瘤细胞施用增强量的下式化合物或酰胺，酯或杂化酰胺/酯，其中X是任选在其中包含的任何芳族部分上被取代的烃基; Y-CO是γ-Glu或β-Asp，AAC是氨基酸，优选甘氨酸，苯基甘氨酸，β-丙氨酸，丙氨酸或苯丙氨酸。与非靶细胞相比，类似的化合物也可用于选择性地对靶细胞发挥细胞毒作用，并且还提高哺乳动物受试者骨髓中GM祖细胞的产生。

9. 发明授权

US5545621A Glutathione S-transferase-activated compounds 失效
标题翻译：谷胱甘肽S-转移酶活化化合物
公开(公告)号：US5545621A
公开(公告)日：1996-08-13
申请号：US130736
申请日：1993-10-01
申请人： Lawrence M. Kauvar , Matthew H. Lyttle , Apparao Satyam
发明人： Lawrence M. Kauvar , Matthew H. Lyttle , Apparao Satyam
IPC分类号： A61K38/00 , A61K38/06 , C07K5/02 , C07K5/037 , G01N30/02 , G01N33/573 , G01N33/574 , C07K5/023
CPC分类号： A61K38/06 , C07K5/0215 , G01N33/573 , G01N33/57496 , G01N2333/91177 , G01N30/02
摘要： 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.
摘要翻译：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。

10. 发明授权

US5767086A Bone marrow stimulation by certain glutathione analogs 失效
标题翻译：某些谷胱甘肽类似物对骨髓的刺激
公开(公告)号：US5767086A
公开(公告)日：1998-06-16
申请号：US482645
申请日：1995-06-07
申请人： Lawrence M. Kauvar , Matthew H. Lyttle , Amy S. Morgan , Richard F. Borch
发明人： Lawrence M. Kauvar , Matthew H. Lyttle , Amy S. Morgan , Richard F. Borch
IPC分类号： A61K38/00 , A61K38/06 , C07K5/02 , C07K5/037 , G01N30/02 , C07K5/08
CPC分类号： A61K38/06 , C07K5/0215 , G01N30/02
摘要： Compounds of the formula ##STR1## and the esters, amides, amide/esters and salts thereof, wherein YCO is .gamma.-glu or .beta.-asp; G* is phenyl glycine or glycine; Z is CH.sub.2, O or S; and X is a hydrocarbon radical of 1-20 C; are useful in stimulating the differentiation of bone marrow, mitigating the bone-marrow-destructive effects of a chemotherapeutic agent, and in potentiating the toxicity of chemotherapeutic agents.
摘要翻译：式（1）的化合物及其酯，酰胺，酰胺/酯和盐，其中YCO是γ-Glu或β-asp; G *是苯基甘氨酸或甘氨酸; Z是CH 2，O或S; X为1-20 C的烃基; 可用于刺激骨髓分化，减轻化疗药物的骨髓破坏作用，增强化学治疗剂的毒性。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式