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1. 发明申请

WO1994026723A2 PREPARATION OF N-CYANODITHIOIMINO-CARBONATES AND 3-MERCAPTO-5-AMINO-1H-1,2,4-TRIAZOLE 审中-公开
标题翻译： N-氰基亚氨基二碳酸酯和3-巯基-5-氨基-1H-1,2,4-三唑的制备
公开(公告)号：WO1994026723A2
公开(公告)日：1994-11-24
申请号：PCT/US1994005157
申请日：1994-05-10
申请人： GENENTECH, INC. , BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , MARSTERS, James, C., Jr. , BROWN, Michael, S. , CROWLEY, Craig, W. , GOLDSTEIN, Joseph, L. , JAMES, Guy, L. , McDOWELL, Robert, S. , OARE, David , RAWSON, Thomas, E. , REYNOLDS, Mark , SOMERS, Todd, G.
发明人： GENENTECH, INC. , BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
IPC分类号： C07D243/14
CPC分类号： C07D223/16 , A61K38/00 , C07D243/10 , C07D243/24 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/06 , C07D409/14 , C07D487/04 , C07D513/04 , C07K5/0207 , C07K5/0606 , C07K5/06139 , C07K5/06191 , C07K5/081 , C07K5/0821 , C07K5/0827 , C07K5/1013 , C07K5/1024 , C07K5/1027
摘要： Benzodiazepine derivatives are disclosed that act as potent inhibitors of ras farnesyl:protein transferase. Pharmaceutical compositions containing these benzodiazepines are provided for treatment of diseases for which inhibition of the ras farnesyl:protein transferase is indicated.
摘要翻译：公开了苯并二氮杂衍生物，其作为法西尼酯：蛋白转移酶的有效抑制剂。提供含有这些苯二氮卓类药物的药物组合物，用于治疗对法拉第法：蛋白转移酶的抑制作用的疾病的治疗。

2. 发明申请

WO1994004561A1 METHODS AND COMPOSITIONS FOR THE IDENTIFICATION, CHARACTERIZATION, AND INHIBITION OF FARNESYLTRANSFERASE 审中-公开
标题翻译：鉴定，鉴定和抑制番茄红素的方法和组合物
公开(公告)号：WO1994004561A1
公开(公告)日：1994-03-03
申请号：PCT/US1993008062
申请日：1993-08-24
申请人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , GENENTECH, INC. , BROWN, Michael, S. , GOLDSTEIN, Joseph, L. , REISS, Yuval , MARSTERS, James, C., Jr.
发明人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , GENENTECH, INC.
IPC分类号： C07K05/10
CPC分类号： C12N9/1085 , A61K38/00 , C07K1/1077 , C07K5/1013 , C07K5/1016 , C07K5/1019 , C07K5/1024 , C07K7/02 , C07K7/06 , C07K14/82
摘要： Disclosed are methods and compositions for the identification, characterization and inhibition of mammalian farnesyl protein transferases, enzymes involved in the farnesylation of various cellular proteins, including cancer related (ras) proteins such as p21ras. The nucleotide and amino acid sequences of the (alpha) and (beta) subunits of both rat and human farnesyl transferase are disclosed, as are methods and compositions for the preparation of farnesyl transferase by recombinant means, following the molecular cloning and co-expression of its two subunits, for assay and purification of the enzyme, as well as procedures for using the purified enzyme in screening protocols for the identification of possible anticancer agents which inhibit the enzyme and thereby prevent expression of proteins such as p21ras. Also disclosed is a family of compounds which act either as false substrates for the enzyme or as pure inhibitors and can therefore be employed for inhibition of the enzyme. The most potent inhibitors are ones in which phenylalanine occurs at the third position of a tetrapeptide whose amino terminus is cysteine. Improved inhibitors with defined structures and characteristics are also disclosed.
摘要翻译：公开了用于鉴定，表征和抑制哺乳动物法尼基蛋白转移酶的方法和组合物，涉及各种细胞蛋白的法呢基化的酶，包括癌相关（ras）蛋白如p21ras。公开了大鼠和人类法呢基转移酶的（α）和（β）亚基的核苷酸和氨基酸序列，以及通过重组方法制备法呢基转移酶的方法和组合物，分子克隆和共表达其两个亚基用于酶的测定和纯化，以及在筛选方案中使用纯化酶鉴定可能的抗癌剂的程序，所述抗癌剂抑制酶，从而阻止诸如p21ras的蛋白质的表达。还公开了一种化合物家族，其作用为酶的假基质或作为纯抑制剂，因此可用于抑制酶。最有效的抑制剂是其氨基末端是半胱氨酸的四肽的第三位发生苯丙氨酸的抑制剂。还公开了具有限定结构和特征的改进的抑制剂。

3. 发明申请

WO1991016340A1 METHODS AND COMPOSITIONS FOR THE IDENTIFICATION, CHARACTERIZATION AND INHIBITION OF FARNESYL PROTEIN TRANSFERASE 审中-公开
标题翻译：鉴定，表征和抑制农杆菌蛋白转移的方法和组合物
公开(公告)号：WO1991016340A1
公开(公告)日：1991-10-31
申请号：PCT/US1991002650
申请日：1991-04-18
申请人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , BROWN, Michael, S. , GOLDSTEIN, Joseph, L. , REISS, Yuval
发明人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
IPC分类号： C07K07/06
CPC分类号： C07K7/06 , A61K38/00 , C07K1/1077 , C07K5/1013 , C07K5/1016 , C07K5/1019 , C07K5/1024 , C07K7/02 , C07K14/82 , C12N9/1085 , Y10S435/815
摘要： Disclosed are methods and compositions for the identification, characterization and inhibition of farnesyl protein transferases, enzymes involved in the farnesylation of various cellular proteins, including cancer related ras proteins such as p21ras. One farnesyl protein transferase which is disclosed herein exhibits a molecular weight of between about 70,000 and about 100,000 upon gel exclusion chromatography. The enzyme appears to comprise one or two subunits of approximately 50 kDa each. Methods are disclosed for assay and purification of the enzyme, as well as procedures for using the purified enzyme in screening protocols for the identification of possible anticancer agents which inhibit the enzyme and thereby prevent expression of proteins such as p21ras. Also disclosed is a family of compounds which act either as false substrates for the enzyme or as pure inhibitors and can therefore be employed for inhibition of the enzyme. The most potent inhibitors are ones in which phenylalanine occurs at the third position of a tetrapeptide whose amino terminus is cysteine.

4. 发明申请

WO1998017797A1 ANTI-ErbB2 ANTIBODIES 审中-公开
标题翻译：抗ErbB2抗体
公开(公告)号：WO1998017797A1
公开(公告)日：1998-04-30
申请号：PCT/US1997018385
申请日：1997-10-09
申请人： GENENTECH, INC. , BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
发明人： GENENTECH, INC. , BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , FENDLY, Brian, M. , PHILLIPS, Gail, Dianne , SCHEUERMANN, Richard, H. , UHR, Jonathan, W.
IPC分类号： C12N15/13
CPC分类号： C07K16/32 , A61K2039/505 , C07K2317/73 , C07K2317/92
摘要： Anti-ErbB2 antibodies are described which bind to an epitope in Domain 1 of ErbB2 and induce cell death via apoptosis. Various uses for these antibodies are also described.
摘要翻译：描述了抗ErbB2抗体，其结合ErbB2的结构域1中的表位并通过凋亡诱导细胞死亡。还描述了这些抗体的各种用途。

5. 发明公开

EP0569552A1 IMPROVED INTRAMEDULLARY CATHETER 失效
标题翻译：改进的导管髓内。
公开(公告)号：EP0569552A1
公开(公告)日：1993-11-18
申请号：EP92907523.0
申请日：1992-01-30
申请人： BOARD OF REGENTS THE UNIVERSITY OF TEXAS SYSTEM
发明人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , MILLER, Larry, J. , ZAMORANO-GAMEZ, Ruben
IPC分类号： A61M25 , A61M39 , A61B10
CPC分类号： A61M39/0208 , A61B2010/0258 , A61M2039/0223 , A61M2210/02
摘要： Procédé et dispositif pour l'apport ou le retrait d'un fluide à ou du système vasculaire de la moelle osseuse, dans lesquels un conduit tubulaire est inséré dans l'os et du fluide est apporté ou retiré à ou d'un réservoir par l'intermédiaire d'un moyen d'étanchéité entourant une tête fixée à une extrémité du conduit en communication avec la moelle osseuse à l'extrémité opposée du conduit. L'accès à la moelle osseuse est réalisé par l'implantation d'un cathéter intramédullaire perfectionné à l'intérieur d'un os et par la création d'un passage réutilisable via un conduit placé entre la moelle osseuse et la surface extérieure de l'os ou de la peau.

6. 发明申请

WO2001077154A2 METHODS AND COMPOSITIONS FOR STAT-1 CONFERRED RESISTANCE TO IMMUNOTOXICITY 审中-公开
标题翻译： STAT-1对免疫毒素抗性的方法和组合
公开(公告)号：WO2001077154A2
公开(公告)日：2001-10-18
申请号：PCT/US2001011845
申请日：2001-04-10
申请人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , CHEN, Guoxun , NEWGARD, Christopher, B.
发明人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
IPC分类号： C07K14/00
CPC分类号： C07K14/4705 , A61K48/00 , C07K2319/00
摘要： The present invention describes methods and compositions for preventing immunocytotoxicity of transplanted cells. The invention provides cells and expression constructs encoding STAT-1α polypeptides that prevent cytokine-mediated cytotoxicity. Thus, the invention provides treatment methods for preventing the rejection of transplanted cells by a host. In a particular embodiment, the invention provides for treatment of diabetes by transplanting into a subject insulinoma cells that secrete insulin in response to glucose and further express STAT-1α, thereby conferring resistance to inflammatory cytokines involved in the cell-rejection response.
摘要翻译：本发明描述了用于预防移植细胞的免疫细胞毒性的方法和组合物。本发明提供编码能够阻止细胞因子介导的细胞毒性的STAT-1α多肽的细胞和表达构建体。因此，本发明提供了防止宿主移植细胞排斥的治疗方法。在一个具体实施方案中，本发明提供了通过移植到对葡萄糖分泌胰岛素并进一步表达STAT-1α的受试者胰岛素瘤细胞来治疗糖尿病，从而赋予参与细胞排斥反应的炎性细胞因子的抗性。

7. 发明申请

WO1998045433A1 PROTEINS AND COMPOSITIONS FOR MODULATING MITOSIS 审中-公开
标题翻译：调理麻醉剂的蛋白质和组合物
公开(公告)号：WO1998045433A1
公开(公告)日：1998-10-15
申请号：PCT/US1998006727
申请日：1998-04-03
申请人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , CLARK, Gary, M. , ALLRED, D., Craig , HILSENBECK, Susan, G. , CHAMNESS, Gary, C. , OSBORNE, C., Kent
发明人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
IPC分类号： C12N15/12
CPC分类号： C07K14/47 , A61K38/00
摘要： The protein encoded by the human gene HEC ( h ighly e xpressed in c ancer) contains a long series of leucine heptad repeats and appears to be crucial for normal mitosis. HEC localizes to the nuclei of interphase cells and redistributes to centromeres during M phase. Ectopic expression of a mutant HEC containing only the heptad repeats results in the inability of cells to divide more than once. Inactivation of HEC results in disordered sister chromatid alignment and separation, as well as in the formation of nonviable cells with multiple, fragmented micronuclei. HEC interacts through its leucine heptad repeats with several proteins involved in mitosis, including nek2, sb1.8, and two different regulatory subunits of the 26S proteasome, MSS1 and p45. These biochemical properties of HEC suggest its potential roles in modulating proteins important for spindle attachment to kinetochores, sister chromatid movement, and M phase progression.
摘要翻译：由人类基因HEC（高表达胰岛素）表达的蛋白质编码的蛋白质含有长序列的亮氨酸七肽重复序列，似乎是对正常有丝分裂至关重要 HEC定位于相间细胞核，并在M期期间重新分布至着丝粒。仅含有七重复重复的突变体HEC的异位表达导致细胞不能分裂多于一次。 HEC的失活导致无序的姐妹染色单体比对和分离，以及形成具有多个片段微核的不可维持细胞。 HEC通过其亮氨酸七肽重复与涉及有丝分裂的几种蛋白质相互作用，包括nek2，sb1.8和26S蛋白酶体，MSS1和p45的两个不同调节亚基。 HEC的这些生物化学性质表明其在调节重要的心脏附着到动粒细胞，姐妹染色单体运动和M期进展中的蛋白质的潜在作用。

8. 发明申请

WO1998028423A2 COMPOSITIONS AND METHODS OF USE FOR OSTEOCLAST INHIBITORY FACTORS 审中-公开
标题翻译： OSTEOCLAST抑制因子的组合物和使用方法
公开(公告)号：WO1998028423A2
公开(公告)日：1998-07-02
申请号：PCT/US1997023666
申请日：1997-12-18
申请人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , ROODMAN, G., David , REDDY, Sakamuri, V. , CHOI, Sun-Jin
发明人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
IPC分类号： C12N15/12
CPC分类号： C12N9/6472 , A61K38/00 , A61K39/00 , C07K14/4703 , C07K2319/02
摘要： It has been found that two proteins produced by human osteoclasts inhibit osteoclast formation in bone marrow cultures and inhibit bone resorption in a fetal long bone assay. One of the proteins is identical to an Ly6 gene family protein and homologous to the Sca2 antigen, Ly6A. The second, protein is OIP-2. The discovery of the osteoclast inhibition property of the OIP proteins suggests the therapeutic potential for patients with disordered osteoclast activity in such conditions as osteoporosis.
摘要翻译：已经发现，人类破骨细胞产生的两种蛋白质在骨髓培养物中抑制破骨细胞形成，并在胎儿长骨测定中抑制骨吸收。其中一种蛋白质与Ly6基因家族蛋白质相同，与Sca2抗原Ly6A同源。第二个蛋白质是OIP-2。 OIP蛋白的破骨细胞抑制性质的发现表明在诸如骨质疏松症的病症中具有无序破骨细胞活性的患者的治疗潜力。

9. 发明申请

WO1998027994A1 PROTEINS AND COMPOSITIONS FOR MODULATING MITOSIS 审中-公开
标题翻译：调理麻醉剂的蛋白质和组合物
公开(公告)号：WO1998027994A1
公开(公告)日：1998-07-02
申请号：PCT/US1997023385
申请日：1997-12-18
申请人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
发明人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , LEE, Wen-Hwa , CHEN, Yumay , RILEY, Daniel, J. , CHEN, Phang-Lang
IPC分类号： A61K38/08
CPC分类号： C07K14/4702
摘要： The protein encoded by the human gene HEC( h ighly e xpressed in c ancer) contains a long series of leucine heptad repeats and appears to be crucial for normal mitosis. HEC localizes to the nuclei of interphase cells and redistributes to centromeres during M phase. Ectopic expression of a mutant HEC containing only the heptad repeats results in the inability of cells to divide more than once. Inactivation of HEC results in disordered sister chromatid alignment and separation, as well as in the formation of non viable cells with multiple, fragmented micronuclei. HEC interacts through its leucine heptad repeats with several proteins involved in mitosis, including nek2, sb1.8, and two different regulatory subunits of the 26S proteasome, MSS1 and p45. These biochemical properties of HEC suggest its potential roles in modulating proteins important for spindle attachment to kinetochores, sister chromatic movement, and M phase progression.
摘要翻译：由人类基因HEC（高表达胰岛素）表达的蛋白质编码的蛋白质含有长序列的亮氨酸七肽重复序列，似乎是对正常有丝分裂至关重要 HEC定位于相间细胞核，并在M期期间重新分布至着丝粒。仅含有七重复重复的突变体HEC的异位表达导致细胞不能分裂多于一次。 HEC的失活导致无序的姐妹染色单体比对和分离，以及形成具有多个片段微核的非活细胞。 HEC通过其亮氨酸七肽重复与涉及有丝分裂的几种蛋白质相互作用，包括nek2，sb1.8和26S蛋白酶体，MSS1和p45的两个不同调节亚基。 HEC的这些生物化学性质表明其在调节重要的心脏附着到动粒细胞，姐妹色彩运动和M期进展中的蛋白质的潜在作用。

10. 发明申请

WO1998021359A1 GLUTATHIONE S-TRANSFERASE (GST) GENES IN CANCER 审中-公开
标题翻译：癌症中的GLUTATHIONE S转移（GST）基因
公开(公告)号：WO1998021359A1
公开(公告)日：1998-05-22
申请号：PCT/US1997020987
申请日：1997-11-12
申请人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , THE UNIVERSITY OF MISSISSIPPI
发明人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , THE UNIVERSITY OF MISSISSIPPI , ALI-OSMAN, Francis , LOPEZ-BERESTEIN, Gabriel , BUOLAMWINI, John, K. , ANTOUN, Gamil , LO, Hui-Wen , KELLER, Charles , AKANDE, Olanike
IPC分类号： C12Q01/00
CPC分类号： C12Q1/48 , G01N33/5011 , G01N33/57484
摘要： Complementary DNA and genomic clones for three variants of GST- pi are disclosed. It is demonstrated that certain of these variants are overexpressed in gliomas, thereby indicating an involvement with that form of cancer. This permits the detection and treatment of certain classes of tumors using new compositions such as GST- pi genes, oligonucleotides, peptides and antibodies.
摘要翻译：公开了三种GST-p变体的互补DNA和基因组克隆。证明某些这些变体在神经胶质瘤中过表达，从而表明参与了该形式的癌症。这允许使用新的组合物如GST-pi基因，寡核苷酸，肽和抗体来检测和治疗某些类型的肿瘤。

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