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1. 发明申请

WO9915183A9 PROTEASOME INHIBITORS, UBIQUITIN PATHWAY INHIBITORS OR AGENTS THAT INTERFERE WITH THE ACTIVATION OF NF- kappa B VIA THE UBIQUITIN PROTEASOME PATHWAY TO TREAT INFLAMMATORY AND AUTOIMMUNE DISEASES 审中-公开
标题翻译：抗生素抑制剂，UBIQUITIN途径抑制剂或干扰NF-κB通过UBIQUITIN抗生素途径治疗炎症和自身免疫性疾病的药物
公开(公告)号：WO9915183A9
公开(公告)日：1999-07-29
申请号：PCT/US9820065
申请日：1998-09-25
申请人： PROSCRIPT INC , ELLIOT PETER , ADAMS JULIAN , PLAMONDON LOUIS
发明人： ELLIOT PETER , ADAMS JULIAN , PLAMONDON LOUIS
IPC分类号： A61K45/00 , A61K31/16 , A61K31/407 , A61K31/573 , A61K45/06 , A61P11/06 , A61K31/69 , A61K31/40
CPC分类号： A61K31/16
摘要： This invention is directed to the treatment of inflammatory and autoimmune diseases by administering proteasome inhibitors, ubiquitin pathway inhibitors, agents that interfere with the activation of NF- kappa B via the ubiquitin proteasome pathway, or mixtures thereof. The invention is further directed to the treatment of inflammatory and autoimmune diseases by administering an effective combination of a glucocorticoid and a proteasome inhibitor, ubiquitin pathway inhibitor, agent that interferes with the activation of NF- kappa B via the ubiquitin proteasome pathway, or mixture thereof. Pharmaceutical compositions comprising a combination of a glucocorticoid and a proteasome inhibitor, ubiquitin pathway inhibitor, agent that interferes with the activation of NF- kappa B via the ubiquitin proteasome pathway, or mixture thereof are also contemplated within the scope of the invention.
摘要翻译：本发明涉及通过施用蛋白酶体抑制剂，泛素途径抑制剂，通过泛素蛋白酶体途径干扰NF-κB活化的试剂或其混合物来治疗炎性和自身免疫性疾病。本发明进一步涉及通过施用糖皮质激素和蛋白酶体抑制剂，泛素途径抑制剂，通过泛素蛋白酶体途径干扰NF-κB活化的试剂或其混合物的有效组合来治疗炎性和自身免疫性疾病。包含糖皮质激素和蛋白酶体抑制剂，泛素途径抑制剂，通过泛素蛋白酶体途径干扰NF-κB活化的药剂或其混合物的组合物的药物组合物也包括在本发明的范围内。

2. 发明申请

WO1998025949A1 SUBSTITUTED 5-AMINO-1,3,4-THIADIAZOLE-2-THIONES 审中-公开
标题翻译：取代的5-氨基-1,3,4-噻二唑-2-基
公开(公告)号：WO1998025949A1
公开(公告)日：1998-06-18
申请号：PCT/US1997022534
申请日：1997-12-09
申请人： PROSCRIPT, INC. , OLEKSYSZYN, Jozef , JACOBSON, Alan, R.
发明人： PROSCRIPT, INC.
IPC分类号： C07K05/08
CPC分类号： C07K5/06139 , A61K31/433 , A61K31/4725 , A61K31/58 , A61K38/00 , C07K5/06078 , C07K5/06165
摘要： The use of N5-substituted 5-amino-1,3,4-thiadiazole-2-thiols as metalloproteinases to inhibit matrix metalloproteinase enzymes and cartilage degradation is disclosed. Methods of treating diseases caused by over-activity of matrix metalloproteinases, such as osteoarthritis and rheumatoid arthritis, are also disclosed.
摘要翻译：公开了使用N5-取代的5-氨基-1,3,4-噻二唑-2-硫醇作为金属蛋白酶抑制基质金属蛋白酶和软骨降解。还公开了治疗由基质金属蛋白酶如骨关节炎和类风湿性关节炎过度活动引起的疾病的方法。

3. 发明申请

WO1997035014A1 A KINASE CAPABLE OF SITE-SPECIFIC PHOSPHORYLATION OF I'kappa'B'alpha' 审中-公开
标题翻译：一种可以进行I kappa Bα的位点特异性磷酸化的激酶
公开(公告)号：WO1997035014A1
公开(公告)日：1997-09-25
申请号：PCT/US1997004195
申请日：1997-03-19
申请人： PROSCRIPT, INC.
发明人： PROSCRIPT, INC. , CHEN, Zhijian, J.
IPC分类号： C12N15/54
CPC分类号： C12N9/1205 , A01K2217/05 , A01K2217/075 , A61K38/00 , A61K48/00 , Y10S435/81
摘要： The present invention relates, in general, to a kinase which in its activated state is capable of site-specific phosphorylation of I kappa B alpha , I kappa B alpha kinase. In particular, the present invention relates to the purified kinase, purified polypeptide subunits of the kinase, nucleic acid molecules coding for the purified polypeptide subunits; recombinant nucleic acid molecules; cells containing the recombinant nucleic acid molecules; antibodies having binding affinity specifically to the kinase or its polypeptide subunits; hybridomas containing the antibodies; nucleic acid probes for the detection of the nucleic acid encoding the kinase; a method of detecting nucleic acids encoding the kinase or polypeptides of the kinase in a sample; and kits containing nucleic acid probes or antibodies. This invention further relates to bioassays using the nucleic acid sequence, protein or antibodies of this invention to diagnose, assess, or prognose a mammal afflicted with an undesired activation of NF- kappa B. This invention also relates to ligands, agonists, and antagonists of the kinase, and diagnostic and therapeutic uses thereof. This invention also relates to bioassays using the kinase or polypeptides of the kinase of this invention to identify ligands, agonists, and antagonists. More specifically, this invention relates to selective inhibitors of the kinase and to structure-based design of ligands, agonists, and antagonists of the kinase. This invention further relates to gene therapy using the nucleic acids of the invention.
摘要翻译：本发明一般涉及在其活化状态下能够进行IκBα，IκBα激酶的位点特异性磷酸化的激酶。特别地，本发明涉及激酶的纯化的激酶，纯化的多肽亚基，编码纯化的多肽亚基的核酸分子; 重组核酸分子; 含有重组核酸分子的细胞; 具有与激酶或其多肽亚基特异性结合亲和力的抗体; 含有抗体的杂交瘤; 用于检测编码激酶的核酸的核酸探针; 检测样品中激酶或激酶多肽的核酸的检测方法; 和含有核酸探针或抗体的试剂盒。本发明进一步涉及使用本发明的核酸序列，蛋白质或抗体来诊断，评估或预测患有NF-κB不希望的活化的哺乳动物的生物测定。本发明还涉及配体，激动剂和拮抗剂激酶及其诊断和治疗用途。本发明还涉及使用本发明激酶的激酶或多肽鉴定配体，激动剂和拮抗剂的生物测定。更具体地，本发明涉及激酶的选择性抑制剂和激酶的配体，激动剂和拮抗剂的基于结构的设计。本发明还涉及使用本发明的核酸的基因治疗。

4. 发明申请

WO1996013266A1 BORONIC ESTER AND ACID COMPOUNDS, SYNTHESIS AND USES 审中-公开
标题翻译： BORONIC ESTER和酸化合物，合成和用途
公开(公告)号：WO1996013266A1
公开(公告)日：1996-05-09
申请号：PCT/US1995014117
申请日：1995-10-27
申请人： PROSCRIPT, INC.
发明人： PROSCRIPT, INC. , ADAMS, Julian , MA, Yu-Ting , STEIN, Ross , BAEVSKY, Matthew , GRENIER, Louis , PLAMONDON, Louis
IPC分类号： A61K31/535
CPC分类号： C07K5/0808 , A61K38/00 , C07F5/025 , C07F5/04 , C07K5/06 , C07K5/06043 , C07K5/06139 , C07K5/06191 , C07K5/0827
摘要： Disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.
摘要翻译：本文公开了一种用于降低动物中蛋白质降解速率的方法，包括使动物细胞与某些硼酸酯和酸化合物接触。本文还公开了新的硼酸酯和酸化合物，它们的合成和用途。

5. 发明专利

BR9710408A 未知
公开(公告)号：BR9710408A
公开(公告)日：1999-08-17
申请号：BR9710408
申请日：1997-03-19
申请人： PROSCRIPT INC
发明人： CHEN ZHIJIAN J
IPC分类号： C12N15/02 , A01K67/027 , A61K31/00 , A61K38/00 , A61K45/00 , A61K48/00 , A61P17/00 , A61P17/06 , A61P29/00 , A61P31/00 , A61P35/00 , A61P43/00 , C07K16/40 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N9/12 , C12N15/09 , C12N15/54 , C12P21/08 , C12Q1/48 , C12Q1/68 , G01N33/15 , G01N33/566 , A61K38/45 , C12N5/12
摘要： The present invention relates, in general, to a kinase which in its activated state is capable of site-specific phosphorylation of IkappaBalpha, IkappaBalpha kinase. In particular, the present invention relates to the purified kinase, antibodies having binding affinity specifically to the kinase, and hybridomas containing the antibodies. This invention further relates to bioassays using protein or antibodies of this invention to diagnose, assess, or prognose a mammal afflicted with an undesired activation of NF-kappaB. This invention also relates to ligands, agonists, and antagonists of the kinase, and diagnostic and therapeutic uses thereof. This invention also relates to bioassays using the kinase to identify ligands, agonists, and antagonists. More specifically, this invention relates to selective inhibitors of the kinase.

7. 发明专利

MX9703063A COMPUESTOS DE ESTER Y ACIDO BORONICO, SU SINTESIS Y USOS. 未知
公开(公告)号：MX9703063A
公开(公告)日：1998-07-31
申请号：MX9703063
申请日：1997-04-25
申请人： PROSCRIPT INC
发明人： ADAMS JULIAN , MA YU-TING , STEIN ROSS , BAEVSKY MATTHEW , GRENIER LOUIS , PLAMONDON LOUIS
IPC分类号： C07D295/14 , A61K31/185 , A61K31/40 , A61K31/47 , A61K31/535 , A61K31/5375 , A61K31/69 , A61K38/00 , A61K38/05 , A61K38/55 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/18 , A61P35/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07D207/16 , C07D213/30 , C07D215/12 , C07D215/36 , C07D215/48 , C07D241/12 , C07D295/18 , C07D307/68 , C07D401/12 , C07D471/04 , C07F5/02 , C07F5/04 , C07K20060101 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/078 , C07K5/083 , C07C229/26 , C07C229/02
摘要： En la presente se describe un método para reducir la velocidad de degradacion de proteínas en una animal, que comprende poner en contacto las células y el animal con ciertos compuestos de éster y ácido boronico. También se describen en la presente compuestos de éster y ácido boronico novedosos, sus síntesis y usos.

8. 发明专利

FI971746A0 未知
公开(公告)号：FI971746A0
公开(公告)日：1997-04-23
申请号：FI971746
申请日：1997-04-23
申请人： PROSCRIPT INC
发明人： ADAMS JULIAN , MA YU-TING , STEIN ROSS , BAEVSKY MATTHEW , GRENIER LOUIS , PLAMONDON LOUIS
IPC分类号： C07D295/14 , A61K31/185 , A61K31/40 , A61K31/47 , A61K31/535 , A61K31/5375 , A61K31/69 , A61K38/00 , A61K38/05 , A61K38/55 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/18 , A61P35/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07D207/16 , C07D213/30 , C07D215/12 , C07D215/36 , C07D215/48 , C07D241/12 , C07D295/18 , C07D307/68 , C07D401/12 , C07D471/04 , C07F5/02 , C07F5/04 , C07K20060101 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/078 , C07K5/083 , C07C
摘要： Disclosed herein are novel boronic ester and acid compounds, their synthesis and their uses.

9. 发明专利

CA2203936C BORONIC ESTER AND ACID COMPOUNDS, SYNTHESIS AND USES 未知
公开(公告)号：CA2203936C
公开(公告)日：2005-04-12
申请号：CA2203936
申请日：1995-10-27
申请人： PROSCRIPT INC
发明人： STEIN ROSS , PLAMONDON LOUIS , GRENIER LOUIS , BAEVSKY MATTHEW , ADAMS JULIAN , MA YU-TING
IPC分类号： C07D295/14 , A61K31/185 , A61K31/40 , A61K31/47 , A61K31/535 , A61K31/5375 , A61K31/69 , A61K38/00 , A61K38/05 , A61K38/55 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/18 , A61P35/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07D207/16 , C07D213/30 , C07D215/12 , C07D215/36 , C07D215/48 , C07D241/12 , C07D295/18 , C07D307/68 , C07D401/12 , C07D471/04 , C07F5/02 , C07F5/04 , C07K20060101 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/078 , C07K5/083 , C12N9/99
摘要： Disclosed herein is a method for reducing the rate of degradation of protein s in an animal comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are nov el boronic ester and acid compounds, their synthesis and uses.

10. 发明专利

CA2315240A1 HUMAN PROTEINS RESPONSIBLE FOR NEDD8 ACTIVATION AND CONJUGATION 未知
公开(公告)号：CA2315240A1
公开(公告)日：1999-07-01
申请号：CA2315240
申请日：1998-12-18
申请人： PROSCRIPT INC
发明人： CHAU VINCENT
IPC分类号： G01N33/50 , C07K14/47 , C12N9/00 , C12N15/09 , C12N15/12 , C12P21/02 , C12Q1/68 , C12N15/11
摘要： The invention relates to covalent modification of proteins through their conjugation with other proteins. More particularly, the invention relates to the modulation of such conjugation involving the protein NEDD8. The invention provides compositions and methods for detecting and/or modulating the activation and/or conjugation of NEDD8, as well as compositions and methods for discovering molecules which are useful in detecting and/or modulating the activation and/or conjugation of NEDD8. The present invention arises from the purification and characterization of novel NEDD8 activating and conjugating enzymes.

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