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1.发明公开INSULIN RECEPTOR ACTIVATORS FOR THE TREATMENT OF METABOLIC DISORDERS IN HUMANS RESULTING FROM TREATMENT OF HIV INFECTION WITH HIV PROTEASE INHIBITORS 审中-公开胰岛素受体激活剂治疗代谢性疾病的HIV感染了HIV蛋白酶抑制剂的治疗引起的
公开(公告)号：EP1355698A2
公开(公告)日：2003-10-29
申请号：EP01980019.2
申请日：2001-10-10
申请人： TELIK, INC.
IPC分类号： A61P3/10 , A61P5/50 , A61K31/655 , A61K31/195 , A61K31/185
CPC分类号： A61K31/19 , A61K31/17 , A61K31/18 , A61K31/185 , A61K31/195 , A61K31/655
摘要： The present invention comprises the use of insulin receptor activating compounds, optionally in conjunction with insulin, for the treatment of HIV protease inhibitor-induced metabolic disorders. Any insulin receptor activating compounds is suitable for the practice of the invention. In addition, preferred compounds are disclosed. Methods of treating a person suffering from HIV protease inhibitor-induced metabolic disorders such as lipodystrophy, hypertriglyceridemia, insulin resistance, hyperglycemia, diabetes and ketoacidosis are also provided.
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公开(公告)号：EP1289936A1
公开(公告)日：2003-03-12
申请号：EP01941753.4
申请日：2001-06-01
申请人： TELIK, INC.
IPC分类号： C07C237/42 , C07C237/40 , C07C233/81 , C07C235/56 , C07C309/61 , A61K31/196 , A61K31/24 , C07C231/02
CPC分类号： C07C233/81 , C07C233/88 , C07C235/56 , C07C235/64 , C07C235/84 , C07C237/40 , C07C237/42 , C07C309/51 , C07C309/61 , C07D317/60
摘要： The present invention relates to chemical compounds, pharmaceutical compositions comprising said compounds, methods of treatment administering these compounds to mammalian hosts, and processes for their preparation. Specifically, the invention relates to a means to enhance insulin-dependent glucose uptake. More specifically, the invention concerns compounds and pharmaceutical compositions that activate the insulin receptor kinase, which leads to increased sensitivity to insulin and an increase in glucose uptake, as well as processes for the preparation of the compounds. The invention also specifically concerns methods for treating humans with hyperglycemia, especially for the treatment of Type II diabetes.
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3.发明授权BIS-(N,N'-BIS-(2-HALOETHYL)AMINO) PHOSPHORAMIDATES AS ANTITUMOR AGENTS 有权双（N，N'-双（2-卤代乙基）氨基）磷酸酯作为抗肿瘤剂
公开(公告)号：EP1278759B1
公开(公告)日：2005-12-21
申请号：EP01935025.5
申请日：2001-05-02
申请人： TELIK, INC.
发明人： HERR, Jason, R. , LUM, Robert, T. , SCHOW, Steven, R. , MENG, Fanying , KOZLOWSKI, Michael, R. , ZHICHKIN, Pavel
IPC分类号： C07F9/24 , A61K31/664 , A61P35/04
CPC分类号： C07F9/2458 , C07F9/2408
摘要： The present invention relates to chemical compounds, methods of treatment, pharmaceutical compositions, and processes for their preparation. The compounds possess anti-tumor activities or are capable of being modified to have anti-tumor activities, and therefore, this invention particularly relates to the use of the compounds in methods for the treatment of tumors and especially for the treatment of cancer, as well as to the processes for their preparation.
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公开(公告)号：EP1289936B1
公开(公告)日：2004-10-20
申请号：EP01941753.4
申请日：2001-06-01
申请人： TELIK, INC.
IPC分类号： C07C237/42 , C07C237/40 , C07C233/81 , C07C235/56 , C07C309/61 , A61K31/196 , A61K31/24 , C07C231/02
CPC分类号： C07C233/81 , C07C233/88 , C07C235/56 , C07C235/64 , C07C235/84 , C07C237/40 , C07C237/42 , C07C309/51 , C07C309/61 , C07D317/60
摘要： The present invention relates to chemical compounds, pharmaceutical compositions comprising said compounds, methods of treatment administering these compounds to mammalian hosts, and processes for their preparation. Specifically, the invention relates to a means to enhance insulin-dependent glucose uptake. More specifically, the invention concerns compounds and pharmaceutical compositions that activate the insulin receptor kinase, which leads to increased sensitivity to insulin and an increase in glucose uptake, as well as processes for the preparation of the compounds. The invention also specifically concerns methods for treating humans with hyperglycemia, especially for the treatment of Type II diabetes.
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5.发明公开BIS-(N,N'-BIS-(2-HALOETHYL)AMINO) PHOSPHORAMIDATES AS ANTITUMOR AGENTS 有权双（N，N'-双（2-卤代乙基）氨基）磷酸酯作为抗肿瘤剂
公开(公告)号：EP1278759A1
公开(公告)日：2003-01-29
申请号：EP01935025.5
申请日：2001-05-02
申请人： TELIK, INC.
发明人： HERR, Jason, R. , LUM, Robert, T. , SCHOW, Steven, R. , MENG, Fanying , KOZLOWSKI, Michael, R. , ZHICHKIN, Pavel
IPC分类号： C07F9/24 , A61K31/664 , A61P35/04
CPC分类号： C07F9/2458 , C07F9/2408
摘要： The present invention relates to chemical compounds, methods of treatment, pharmaceutical compositions, and processes for their preparation. The compounds possess anti-tumor activities or are capable of being modified to have anti-tumor activities, and therefore, this invention particularly relates to the use of the compounds in methods for the treatment of tumors and especially for the treatment of cancer, as well as to the processes for their preparation.
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6.发明公开
公开(公告)号：EP1200396A1
公开(公告)日：2002-05-02
申请号：EP00952351.5
申请日：2000-07-28
申请人： TELIK, INC.
发明人： SPEVAK, Wayne, R. , SONGYUAN, Shi , PRASAD, V., V., S., V., Manchem , KOZLOWSKI, Michael, R. , SCHOW, Steven, R. , LUM, Robert, T. , ROBINSON, Louise , PARK, Jeong, Weong
IPC分类号： C07C309/51 , C07C309/59 , C07D213/81 , C07D213/82 , C07D307/85 , C07C311/21 , C07C311/29 , C07C311/13 , C07C237/42 , A61K31/16 , A61K31/18 , A61K31/33
CPC分类号： C07D241/44 , C07C237/42 , C07C309/51 , C07C309/59 , C07C311/13 , C07C311/21 , C07C311/29 , C07D213/81 , C07D213/82 , C07D215/48 , C07D307/68 , C07D307/85
摘要： Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds are provided. Compounds of formula (1) where: R?1 and R2¿ are, independently, hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, R3 is a substituent on the B ring; and is -SO¿2OR?6, -C(O)OR6, -SO2NR62-C(O)NR62 or tetrazolyl; the linker -WY- between the naphthyl and phenyl intersects the A ring of the naphthyl and is, independently, -C(O)NR?7-, -NR7¿C(O)-, -C(O)O-, -OC(O)-, -CH=CH-, -NR7CH2-, -CH2NR?7-, -NR7C(O)NR7- -NR7¿C(O)O-, -OC(O)NR?7-, -NR7SO¿2O-, -OSO2NR7-, -OC(O)O-, -SO¿2?NR?7-, -NR7SO¿2-, -OSO2-, or -SO2O-; each R?6 and R7¿ is, independently, hydrogen or lower alkyl; optionally in the form of single stereoisomers or mixtures of stereoisomers, or the pharmaceutically acceptable salts thereof; are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.
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公开(公告)号：EP1143992A2
公开(公告)日：2001-10-17
申请号：EP00908420.3
申请日：2000-01-27
申请人： TELIK, INC.
发明人： REDELMEIER, Thomas , KAUVAR, Lawrence, M. , LUM, Robert, T. , LYTTLE, Matthew, H. , MACSATA, Robert, W. , SCHOW, Steven, R. , VILLAR, Hugo, O. , KOZLOWSKI, Michael, R.
CPC分类号： A61K9/127 , A61K9/1075 , 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.
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公开(公告)号：EP1181271B1
公开(公告)日：2005-01-19
申请号：EP00936360.7
申请日：2000-05-25
申请人： TELIK, INC.
发明人： SPEVAK, Wayne , LUM, Robert, T. , SHI, Songyuan , MANCHEM, Prasad , KOZLOWSKI, Michael, R. , SCHOW, Steven, R.
IPC分类号： C07C311/47 , C07C309/51 , C07D257/04 , C07D213/76 , C07D233/32 , C07D335/18 , C07C335/32 , C07D211/96 , A61K31/18 , A61K31/395
CPC分类号： C07D257/04 , C07C309/51 , C07C311/47 , C07C335/16 , C07C335/18 , C07C335/32 , C07D211/96 , C07D213/76 , C07D233/36 , C07D239/42 , C07D241/20 , C07F9/4021
摘要： Compounds of formula (I), wherein R?1 and R2¿ are substituents on the A rings and are, independently, -SO¿2NR?72, -C(O)NR72, -NR7SO2R?7, -NR7C(O)R7, -SO¿2OR7, -C(O)OR7, -OSO¿2R?7, or -OC(O)R?7, R3 and R4¿ are, independently, hydrogen or lower alkyl, or R?3 and R4¿ together are -(CH¿2?)2-, -(CH2)3-, or -(CH2)4-, or R?3 or R4¿ may be an electron pair, R?5 and R6¿ are, independently, hydrogen, alkyl, substituted alkyl, cyano, halo, nitro, -SR8, -C(O)R8, -SO2OR8, -OSO¿2?R?8, -SO¿2NR82, -NR8SO2R8, -OC(O)R8, -C(O)OR8, -C(O)NR82, -NR?8C(O)R8, -OR8¿, or -NR82, each R?7 and R8¿ is, independently, hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, aryl(lower)alkyl, substituted aryl(lower)alkyl, heteroaryl(lower)alkyl, substituted heteroaryl(lower)alkyl, heterocyclyl, substituted heterocyclyl, heteroaryl, or substituted heteroaryl, each Y is, independently, a non-interfering substituent which is not linked to the naphthalene ring via an azo or amide linkage, each x is independently, 0, 1 or 2, and the linker connects a carbon designated as c to a carbon designated as d, or a pharmaceutically acceptable salt thereof, as a single stereoisomer or mixture of stereoisomers, are useful for treating conditions associated with hyperglycemia, especially Type II diabetes, with dinaphthylureas. These compounds are useful in stimulating the kinase activity of the insulin receptor, activating the insulin receptor, and stimulating the uptake of glucose. Pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.
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公开(公告)号：EP1143992B1
公开(公告)日：2005-01-12
申请号：EP00908420.3
申请日：2000-01-27
申请人： TELIK, INC.
发明人： REDELMEIER, Thomas , KAUVAR, Lawrence, M. , LUM, Robert, T. , LYTTLE, Matthew, H. , MACSATA, Robert, W. , SCHOW, Steven, R. , VILLAR, Hugo, O. , KOZLOWSKI, Michael, R.
CPC分类号： A61K9/127 , A61K9/1075 , 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.
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公开(公告)号：EP1181271A2
公开(公告)日：2002-02-27
申请号：EP00936360.7
申请日：2000-05-25
申请人： Telik, Inc.
发明人： SPEVAK, Wayne , LUM, Robert, T. , SHI, Songyuan , MANCHEM, Prasad , KOZLOWSKI, Michael, R. , SCHOW, Steven, R.
IPC分类号： C07C311/47 , C07C309/51 , C07D257/04 , C07D213/76 , C07D233/32 , C07D335/18 , C07C335/32 , C07D211/96 , A61K31/18 , A61K31/395
CPC分类号： C07D257/04 , C07C309/51 , C07C311/47 , C07C335/16 , C07C335/18 , C07C335/32 , C07D211/96 , C07D213/76 , C07D233/36 , C07D239/42 , C07D241/20 , C07F9/4021
摘要： Compounds of formula (I), wherein R?1 and R2¿ are substituents on the A rings and are, independently, -SO¿2NR?72, -C(O)NR72, -NR7SO2R?7, -NR7C(O)R7, -SO¿2OR7, -C(O)OR7, -OSO¿2R?7, or -OC(O)R?7, R3 and R4¿ are, independently, hydrogen or lower alkyl, or R?3 and R4¿ together are -(CH¿2?)2-, -(CH2)3-, or -(CH2)4-, or R?3 or R4¿ may be an electron pair, R?5 and R6¿ are, independently, hydrogen, alkyl, substituted alkyl, cyano, halo, nitro, -SR8, -C(O)R8, -SO2OR8, -OSO¿2?R?8, -SO¿2NR82, -NR8SO2R8, -OC(O)R8, -C(O)OR8, -C(O)NR82, -NR?8C(O)R8, -OR8¿, or -NR82, each R?7 and R8¿ is, independently, hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, aryl(lower)alkyl, substituted aryl(lower)alkyl, heteroaryl(lower)alkyl, substituted heteroaryl(lower)alkyl, heterocyclyl, substituted heterocyclyl, heteroaryl, or substituted heteroaryl, each Y is, independently, a non-interfering substituent which is not linked to the naphthalene ring via an azo or amide linkage, each x is independently, 0, 1 or 2, and the linker connects a carbon designated as c to a carbon designated as d, or a pharmaceutically acceptable salt thereof, as a single stereoisomer or mixture of stereoisomers, are useful for treating conditions associated with hyperglycemia, especially Type II diabetes, with dinaphthylureas. These compounds are useful in stimulating the kinase activity of the insulin receptor, activating the insulin receptor, and stimulating the uptake of glucose. Pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.
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