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1. 发明申请

WO0033888A9 PRODRUG COMPOUNDS AND PROCESS FOR PREPARATION THEREOF 审中-公开
标题翻译： PRODRUG化合物及其制备方法
公开(公告)号：WO0033888A9
公开(公告)日：2001-05-10
申请号：PCT/US9930393
申请日：1999-12-10
申请人： COULTER PHARM INC , LOBL THOMAS J , DUBOIS VINCENT , FERNANDEZ ANNE MARIE , GANGWAR SANJEEV , LEWIS EVAN , NIEDER MATTHEW H , TROUET ANDRE , VISKI PETER , YARRANTON GEOFFREY T
发明人： LOBL THOMAS J , DUBOIS VINCENT , FERNANDEZ ANNE-MARIE , GANGWAR SANJEEV , LEWIS EVAN , NIEDER MATTHEW H , TROUET ANDRE , VISKI PETER , YARRANTON GEOFFREY T
IPC分类号： A61K31/138 , A61K31/165 , A61K31/198 , A61K31/337 , A61K31/407 , A61K31/437 , A61K31/4745 , A61K31/513 , A61K31/519 , A61K31/52 , A61K31/5517 , A61K31/555 , A61K31/7004 , A61K31/7028 , A61K31/7048 , A61K31/7064 , A61K31/7068 , A61K33/24 , A61K47/42 , A61K47/48 , A61P29/00 , A61P35/00 , C07K5/10 , C07K7/00
CPC分类号： A61K47/65
摘要： The prodrug of the invention is a modified form of a therapeutic agent and comprises a therapeutic agent, an oligopeptide, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by the enzyme trouase. Also disclosed are processes for making the prodrug compounds.
摘要翻译：本发明的前药是治疗剂的修饰形式，并且包含治疗剂，寡肽，稳定基团和任选的连接基团。前药可被酶木瓜酶切割。还公开了制备前药化合物的方法。

2. 发明申请

WO0033888A3 PRODRUG COMPOUNDS AND PROCESS FOR PREPARATION THEREOF 审中-公开
标题翻译： PRODRUG化合物及其制备方法
公开(公告)号：WO0033888A3
公开(公告)日：2001-11-08
申请号：PCT/US9930393
申请日：1999-12-10
申请人： COULTER PHARM INC , LOBL THOMAS J , DUBOIS VINCENT , FERNANDEZ ANNE MARIE , GANGWAR SANJEEV , LEWIS EVAN , NIEDER MATTHEW H , TROUET ANDRE , VISKI PETER , YARRANTON GEOFFREY T
发明人： LOBL THOMAS J , DUBOIS VINCENT , FERNANDEZ ANNE-MARIE , GANGWAR SANJEEV , LEWIS EVAN , NIEDER MATTHEW H , TROUET ANDRE , VISKI PETER , YARRANTON GEOFFREY T
IPC分类号： A61K31/138 , A61K31/165 , A61K31/198 , A61K31/337 , A61K31/407 , A61K31/437 , A61K31/4745 , A61K31/513 , A61K31/519 , A61K31/52 , A61K31/5517 , A61K31/555 , A61K31/7004 , A61K31/7028 , A61K31/7048 , A61K31/7064 , A61K31/7068 , A61K33/24 , A61K47/42 , A61K47/48 , A61P29/00 , A61P35/00 , C07K5/10 , C07K7/00
CPC分类号： A61K47/65
摘要： The compound of the invention is a prodrug form of a therapeutic agent linked directly or indirectly to an oligopeptide, which in turn, is linked to a stabilizing group. More generally, the present invention may be described as a new prodrug compound of a therapeutic agent, especially prodrugs comprising an antitumor therapeutic agent, displaying improved therapeutic properties relative to the products of the prior art, especially improved therapeutic properties in the treatment of cancerous tumors and/or in the treatment of inflammatory reactions such as rheumatic diseases. Improved therapeutic properties include decreased toxicity and increased efficacy. Particularly desired are prodrugs which display a high specificity of action, a reduced toxicity, an improved stability in the serum and blood, and which do not move into target cells until activated by a target cell associated enzyme. Prodrug compounds of a marker enabling tumors to be characterized (diagnosis, progression of the tumor, assay of the factors secreted by tumor cells, etc.) are also contemplated. The present invention also relates to the pharmaceutical composition comprising the compound according to the invention and optionally a pharmaceutically acceptable adjuvant or vehicle. Further, a method of decreasing toxicity by modifying a therapeutic agent to create a prodrug is disclosed. Several processes for creating a prodrug of the invention are described. Compounds of the invention include the prodrugs, Suc-ssAla-Leu-Ala-Leu-Dox, Suc-ssAla-Leu-Ala-Leu-Dnr, and Glutaryl-ssAla-Leu-Ala-Leu-Dox. Additionally intermediate compounds, important to the process of preparation of the prodrugs of the invention are claimed.
摘要翻译：本发明的化合物是与寡肽直接或间接连接的治疗剂的前药形式，其又与稳定基团连接。更一般地，本发明可以描述为治疗剂的新的前药化合物，特别是包含抗肿瘤治疗剂的前药，相对于现有技术的产品显示出改善的治疗性质，特别是治疗癌性肿瘤的改善的治疗性质和/或治疗诸如风湿性疾病的炎性反应。改进的治疗性质包括毒性降低和功效增加。特别期望的是显示出高度的作用特异性，毒性降低，血清和血液中改善的稳定性，并且不会移动到靶细胞中直到被靶细胞相关的酶活化的前药。还考虑了能够表征肿瘤（诊断，肿瘤进展，肿瘤细胞分泌的因子的测定等）的标记物的前药化合物。本发明还涉及包含根据本发明的化合物和任选的药学上可接受的佐剂或赋形剂的药物组合物。此外，公开了通过修饰治疗剂以产生前药来降低毒性的方法。描述了用于制备本发明的前药的几种方法。本发明的化合物包括前体药物Suc-ssAla-Leu-Ala-Leu-Dox，Suc-ssAla-Leu-Ala-Leu-Dnr和Glutaryl-ssAla-Leu-Ala-Leu-Dox。要求保护本发明前药制备方法重要的中间体化合物。

3. 发明申请

WO9962565A3 PATIENT-SPECIFIC DOSIMETRY 审中-公开
标题翻译：患者特异性剂量
公开(公告)号：WO9962565A3
公开(公告)日：2000-04-06
申请号：PCT/US9912506
申请日：1999-06-04
申请人： COULTER PHARM INC , UNIV MICHIGAN , KROLL STEWART M , SIEGEL JEFFRY A , WAHL RICHARD L , ZASADNY KENNETH R
发明人： KROLL STEWART M , SIEGEL JEFFRY A , WAHL RICHARD L , ZASADNY KENNETH R
IPC分类号： A61K51/00 , A61K51/10 , A61K51/12 , A61N5/10
CPC分类号： A61K51/1069
摘要： A patient-specific optimally effective radiation dose for administration of a radiopharmaceutical to a patient for treatment of a disease may be established by basing the calculation of the appropriate therapeutic dose on factors such as the desired total body dose, the maximum tolerated dose, the typical clearance profile of the radiopharmaceutical, the patient's mass or maximum effective mass, and the patient-specific residence time of the radiopharmaceutical or an analog in the whole body of the patient. The use of the method allows for treatment of a patient with an appropriate dose which is maximally effective against the disease yet minimally toxic. The determination of a patient-specific therapeutic dose may be assisted by the use of a software program set to the particular parameters of the radiopharmaceutical.
摘要翻译：可以通过将适当治疗剂量的计算基于诸如所需总体剂量，最大耐受剂量，典型的剂量等因素的计算来建立用于向患者施用放射性药物以治疗疾病的患者特异性的最佳有效辐射剂量放射性药物的清除曲线，患者的质量或最大有效质量以及放射性药物或类似物在患者全身中的患者特异性停留时间。该方法的使用允许用适当的剂量治疗患者，其对该疾病具有最大的有效性，但是具有最低限度的毒性。可以通过使用针对放射性药物的特定参数的软件程序来辅助确定患者特异性治疗剂量。

4. 发明申请

WO9855154A9 RADIOPROTECTANT FOR PEPTIDES LABELED WITH RADIOISOTOPE 审中-公开
标题翻译：用放射性标记标记的肽的放射治疗仪
公开(公告)号：WO9855154A9
公开(公告)日：1999-04-08
申请号：PCT/US9811428
申请日：1998-06-03
申请人： COULTER PHARM INC , SHOCHAT DAN , CHAN ALBERT S K , BUCKLEY MICHAEL J , COLCHER DAVID
发明人： SHOCHAT DAN , CHAN ALBERT S K , BUCKLEY MICHAEL J , COLCHER DAVID
IPC分类号： A61K51/00 , A61K39/395 , A61K51/08 , A61K51/12 , A61P37/00
CPC分类号： A61K51/12 , A61K51/1027
摘要： A method of ameliorating degradation of radiolabeled peptides, especially radiolabeled proteins such as antibodies, by including povidone, also widely known as polyvinylpyrrolidone or PVP, as a radioprotectant in a composition containing a radiolabeled peptide is described. A radioprotectant composition and a stable peptide-radioisotope composition having povidone are also described. Ascorbic acid or other secondary stabilizers may also be added to the compositions to further enhance radioprotection.
摘要翻译：描述了通过包括聚维酮（也称为聚乙烯吡咯烷酮或PVP）作为包含放射性标记肽的组合物中的放射防护剂来改善放射性标记的肽，特别是放射性标记的蛋白质如抗体的降解的方法。还描述了具有聚维酮的防辐射剂组合物和稳定的肽 - 放射性同位素组合物。还可以将抗坏血酸或其它二级稳定剂加入到组合物中以进一步增强放射防护。

5. 发明专利

DE69818272T2 未知
公开(公告)号：DE69818272T2
公开(公告)日：2004-07-01
申请号：DE69818272
申请日：1998-06-03
申请人： COULTER PHARM INC
发明人： SHOCHAT DAN , CHAN ALBERT S , BUCKLEY MICHAEL J , COLCHER DAVID
IPC分类号： A61K51/00 , A61K39/395 , A61K51/08 , A61K51/12 , A61P37/00
摘要： A method of ameliorating degradation radiolabeled peptides, especially radiolabeled proteins such as antibodies, by including povidone, also widely known as polyvinylpyrrolidone or PVP, as a radioprotectant in a composition containing a radiolabeled peptide is described. A radioprotectant composition and a stable peptide-radioisotope composition having povidone are also described. Ascorbic acid or other secondary stabilizers may also be added to the compositions to further enhance radioprotection.

6. 发明专利

DK1003560T3 未知
公开(公告)号：DK1003560T3
公开(公告)日：2003-12-01
申请号：DK98928875
申请日：1998-06-03
申请人： COULTER PHARM INC
发明人： SHOCHAT DAN , CHAN ALBERT S K , BUCKLEY MICHAEL J , COLCHER DAVID
IPC分类号： A61K51/00 , A61K39/395 , A61K51/08 , A61K51/12 , A61P37/00
摘要： A method of ameliorating degradation radiolabeled peptides, especially radiolabeled proteins such as antibodies, by including povidone, also widely known as polyvinylpyrrolidone or PVP, as a radioprotectant in a composition containing a radiolabeled peptide is described. A radioprotectant composition and a stable peptide-radioisotope composition having povidone are also described. Ascorbic acid or other secondary stabilizers may also be added to the compositions to further enhance radioprotection.

8. 发明专利

AU8672701A Prodrugs activated by plasmin and their use in cancer chemotherapy 未知
公开(公告)号：AU8672701A
公开(公告)日：2002-03-04
申请号：AU8672701
申请日：2001-08-23
申请人： COULTER PHARM INC
发明人： TROUET ANDRE , DUBOIS VINCENT , PASSIOUKOV ALEXANDRE
IPC分类号： A61K38/06 , A61K38/07 , A61K38/08 , A61K47/48 , A01N61/00 , A01N37/18 , A61K31/00 , A61K38/00 , A61K51/00 , A61M36/14
摘要： The product of the invention is a modified form of a therapeutic agent and comprises a therapeutic agent, an oligopeptide having a plasmin peptide substrate of 2-4 amino acids and mono- or di-peptide linkage, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by plasmin. Also disclosed are methods of making and using the prodrug compounds.

9. 发明专利

IL140028D0 PATIENT SPECIFIC DOSIMETRY 未知
公开(公告)号：IL140028D0
公开(公告)日：2002-02-10
申请号：IL14002899
申请日：1999-06-04
申请人： COULTER PHARM INC , UNIV MICHIGAN
IPC分类号： A61K51/10 , A61K51/00 , A61K51/12 , A61N5/10 , A61K
摘要： A patient-specific optimally effective radiation dose for administration of a radiopharmaceutical to a patient for treatment of a disease may be established by basing the calculation of the appropriate therapeutic dose on factors such as the desired total body dose, the maximum tolerated dose, the typical clearance profile of the radiopharmaceutical, the patient's mass or maximum effective mass, and the patient-specific residence time of the radiopharmaceutical or an analog in the whole body of the patient. The use of the method allows for treatment of a patient with an appropriate dose which is maximally effective against the disease yet minimally toxic. The determination of a patient-specific therapeutic dose may be assisted by the use of a software program set to the particular parameters of the radiopharmaceutical.

10. 发明专利

NO995906L 未知
公开(公告)号：NO995906L
公开(公告)日：1999-12-03
申请号：NO995906
申请日：1999-12-02
申请人： COULTER PHARM INC
发明人： SHOCHAT DAN , CHAN ALBERT S K , BUCKLEY MICHAEL J , COLCHER DAVID
IPC分类号： A61K39/395 , A61K51/00 , A61K51/08 , A61K51/12 , A61P37/00
摘要： A method of ameliorating degradation radiolabeled peptides, especially radiolabeled proteins such as antibodies, by including povidone, also widely known as polyvinylpyrrolidone or PVP, as a radioprotectant in a composition containing a radiolabeled peptide is described. A radioprotectant composition and a stable peptide-radioisotope composition having povidone are also described. Ascorbic acid or other secondary stabilizers may also be added to the compositions to further enhance radioprotection.

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