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1. 发明申请

US20050065093A1 Inhibitors of the ICE/ced-3 family of cysteine proteases 审中-公开
标题翻译： ICE / ced-3家族半胱氨酸蛋白酶抑制剂
公开(公告)号：US20050065093A1
公开(公告)日：2005-03-24
申请号：US10914981
申请日：2004-08-10
申请人： Robert Ternansky , Patricia Gladstone , Kevin Tomaselli , Bin Chao , Steven Linton
发明人： Robert Ternansky , Patricia Gladstone , Kevin Tomaselli , Bin Chao , Steven Linton
IPC分类号： C12N9/99 , A61K31/18 , A61K31/404 , A61K31/445 , A61K31/662 , A61K38/00 , A61K38/55 , A61P7/00 , A61P7/06 , A61P9/10 , A61P11/00 , A61P19/08 , A61P25/00 , A61P29/00 , A61P31/00 , A61P35/00 , A61P37/00 , A61P37/02 , A61P41/00 , A61P43/00 , C07C311/51 , C07D209/42 , C07D211/60 , C07K5/06 , C07K5/065 , C12N5/06 , A61K38/06
CPC分类号： C07C311/51 , A61K38/05 , C07K5/0202
摘要： This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds having the following structure: wherein A, B, R, R1, R1′ p and q are as defined herein. The invention is also directed to pharmaceutical compositions containing one or more of these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.
摘要翻译：本发明涉及具有以下结构的新型恶草二肽ICE / ced-3家族抑制剂化合物：其中A，B，R，R 1，R 1，p和q如本文所定义。本发明还涉及含有这些化合物中的一种或多种的药物组合物，以及这些组合物在治疗患有炎症，自身免疫和神经变性疾病的患者中的用途，用于预防缺血性损伤和用于保护要进行移植手术的器官。

2. 发明申请

US20060084613A1 Inhibitors of the ICE/ced-3 family of cysteine proteases 审中-公开
标题翻译： ICE / ced-3家族半胱氨酸蛋白酶抑制剂
公开(公告)号：US20060084613A1
公开(公告)日：2006-04-20
申请号：US11241857
申请日：2005-09-30
申请人： Robert Ternansky , Patricia Gladstone , Kevin Tomaselli , Bin Chao , Steven Linton
发明人： Robert Ternansky , Patricia Gladstone , Kevin Tomaselli , Bin Chao , Steven Linton
IPC分类号： A61K38/06 , C07K5/06
CPC分类号： C07C311/51 , A61K38/05 , C07K5/0202
摘要： This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds having the following structure: wherein A, B, R, R1, R1′ p and q are as defined herein. The invention is also directed to pharmaceutical compositions containing one or more of these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.
摘要翻译：本发明涉及具有以下结构的新型氧酰二肽ICE / ced-3家族抑制剂化合物：其中A，B，R，R 1，R 1'和P q如本文所定义。本发明还涉及含有这些化合物中的一种或多种的药物组合物，以及这些组合物在治疗患有炎症，自身免疫和神经变性疾病的患者中的用途，用于预防缺血性损伤和用于保护要进行移植手术的器官。

3. 发明申请

US20050020810A1 Peptides which target tumor and endothelial cells, compositions and uses thereof 审中-公开
标题翻译：靶向肿瘤和内皮细胞的肽，组合物和用途
公开(公告)号：US20050020810A1
公开(公告)日：2005-01-27
申请号：US10722843
申请日：2003-11-25
申请人： Robert Ternansky , Amy Allan , Patricia Gladstone , Won Yoon , Graham Parry , Fernando Donate , Andrew Mazar
发明人： Robert Ternansky , Amy Allan , Patricia Gladstone , Won Yoon , Graham Parry , Fernando Donate , Andrew Mazar
IPC分类号： A61K38/00 , A61K38/08 , A61K38/10 , A61K47/48 , C07K7/06 , C07K7/08
CPC分类号： C07K7/06 , A61K38/00 , A61K47/62
摘要： The present invention relates generally to peptide analogs of Ac—PHSCN—NH2 which target tumor and endothelial cells and have anti-tumor, anti-angiogenic and anti-metasastic activity, methods of making these peptides, compositions thereof and methods of using these peptides and pharmaceutical compositions thereof to treat, prevent and detect diseases characterized by tumor growth, metastasis and angiogenesis. The peptide analogs may serve, inter alia, as carriers of radioactivity, PET-active compounds, toxins, fluorescent molecules and PEG molecules.
摘要翻译：本发明一般涉及靶向肿瘤和内皮细胞并具有抗肿瘤，抗血管生成和抗代谢活性的Ac-PHSCN-NH2的肽类似物，制备这些肽的方法，其组合物和使用这些肽的方法和用于治疗，预防和检测以肿瘤生长，转移和血管发生为特征的疾病的药物组合物。肽类似物尤其可以用作放射性载体，PET活性化合物，毒素，荧光分子和PEG分子。

4. 发明申请

US20050232924A1 Antibodies and/or conjugates thereof which bind to the amino terminal fragment of urokinase, compositions and uses thereof 审中-公开
标题翻译：结合尿激酶的氨基末端片段的抗体和/或缀合物，其组合物和用途
公开(公告)号：US20050232924A1
公开(公告)日：2005-10-20
申请号：US10993007
申请日：2004-11-18
申请人： Andrew Mazar , Robert Ternansky , Graham Parry , Patricia Gladstone , Susan Gawlak
发明人： Andrew Mazar , Robert Ternansky , Graham Parry , Patricia Gladstone , Susan Gawlak
IPC分类号： A61K39/395 , A61K47/48 , A61K49/00 , A61K51/10 , C07K16/40
CPC分类号： C07K16/40 , A61K47/6871 , A61K49/0002 , A61K51/1075 , A61K2039/505 , C07K2317/77
摘要： Antibodies and/or conjugates thereof which bind to the amino terminal fragment of urokinase, compositions and uses thereof are provided. The antibodies and antibody conjugates, which may include a therapeutic agent or a diagnostic agent, may be used to treat, prevent or detect diseases such as for example cancer.
摘要翻译：提供了结合尿激酶氨基末端片段的抗体和/或缀合物，其组合物和用途。可以使用可以包括治疗剂或诊断剂的抗体和抗体缀合物来治疗，预防或检测诸如癌症的疾病。

5. 发明申请

US20060160805A1 Thiotungstate analogues and uses thereof 有权
标题翻译：噻肟类似物及其用途
公开(公告)号：US20060160805A1
公开(公告)日：2006-07-20
申请号：US10857321
申请日：2004-05-27
申请人： Robert Ternansky , Patricia Gladstone , Amy Allan , Melissa Price , Andrew Mazar
发明人： Robert Ternansky , Patricia Gladstone , Amy Allan , Melissa Price , Andrew Mazar
IPC分类号： A61K31/537 , A61K31/44 , A61K31/4164 , A61K31/425 , A61K31/40 , A61K31/407 , A61K31/14
CPC分类号： C01G41/006 , C07C211/62 , C07C211/63 , C07C211/64 , C07C215/40 , C07C217/08 , C07C219/06 , C07C229/60 , C07C317/28 , C07C2601/02 , C07C2601/14 , C07D207/323 , C07D213/20 , C07D213/53 , C07D233/56 , C07D233/58 , C07D275/02 , C07D295/037 , C07D295/088
摘要： The current invention provides novel thiotungstate derivatives, methods of making novel thiotungstate derivatives, pharmaceutical compositions of novel thiotungstate derivatives, methods of using novel thiotungstate derivatives to treat diseases associated with aberrant vascularization, copper metabolism disorders and obesity and methods of using pharmaceutical compositions of thiotungstate derivatives to treat diseases associated with aberrant vascularization, copper metabolism disorders, neurodegenerative disorders, obesity or NF-κB dysregulation.
摘要翻译：本发明提供了新的硫代钨酸衍生物，制备新型硫代钨酸衍生物的方法，新型硫代钨酸衍生物的药物组合物，使用新型硫代钨酸衍生物治疗与异常血管形成相关的疾病，铜代谢紊乱和肥胖症的方法，以及使用噻唑类衍生物药物组合物的方法治疗与异常血管化相关的疾病，铜代谢障碍，神经退行性疾病，肥胖或NF-κB调节异常。

6. 发明申请

US20050020504A1 C-terminal modified oxamyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases 有权
标题翻译： C末端修饰的oxamyl二肽作为ICE / ced-3家族半胱氨酸蛋白酶的抑制剂
公开(公告)号：US20050020504A1
公开(公告)日：2005-01-27
申请号：US10926800
申请日：2004-08-25
申请人： Donald Karanewsky , Robert Ternansky , Steven Linton , Thang Dinh
发明人： Donald Karanewsky , Robert Ternansky , Steven Linton , Thang Dinh
IPC分类号： C07D307/33 , A61K31/341 , A61K38/00 , A61K38/05 , A61P1/04 , A61P1/16 , A61P3/10 , A61P5/14 , A61P7/00 , A61P7/04 , A61P7/06 , A61P9/10 , A61P11/00 , A61P13/12 , A61P17/02 , A61P17/12 , A61P19/02 , A61P21/04 , A61P25/00 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/12 , A61P31/14 , A61P31/16 , A61P31/20 , A61P37/00 , A61P37/02 , A61P43/00 , C07C237/12 , C07C237/22 , C07C317/50 , C07D295/135 , C07D295/185 , C07F9/32 , C07K5/023 , C07K5/06
CPC分类号： C07D295/185 , C07B2200/07 , C07C237/22 , C07C317/50 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2603/74 , C07D295/135 , C07F9/3264
摘要： This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.
摘要翻译：本发明涉及新型牛磺酰二肽ICE / ced-3家族抑制剂化合物。本发明还涉及含有这些化合物的药物组合物，以及这些组合物在治疗患有炎症，自身免疫和神经变性疾病的患者中的用途，用于预防缺血性损伤以及用于保护进行移植手术。

7. 发明申请

US20060148891A1 Formulations of thiomolybdate or thiotungstate compounds and uses thereof 审中-公开
标题翻译：硫钼酸盐或硫代钨酸盐化合物的制剂及其用途
公开(公告)号：US20060148891A1
公开(公告)日：2006-07-06
申请号：US11256540
申请日：2005-10-21
申请人： Robert Ternansky , Brian Sullivan , Andrew Chen
发明人： Robert Ternansky , Brian Sullivan , Andrew Chen
IPC分类号： A61K31/28
CPC分类号： A61K33/24 , A61K31/24 , A61K31/54
摘要： Formulations of thiomolybdate or thiotungstate derivatives, methods of making formulations of thiomolybdate or thiotungstate derivatives, solid dosage forms of thiomolybdate or thiotungstate analogues, methods of making solid dosage forms of thiomolybdate or thiotungstate analogues and methods of using solid dosage forms of thiomolybdate or thiotungstate derivatives to treat or prevent diseases associated with aberrant vascularization or aberrant angiogenesis, copper metabolism disorders neurodegenerative disorders and obesity are disclosed herein.
摘要翻译：硫钼酸盐或硫钨酸盐衍生物的制剂，制备硫钼酸盐或硫代钨酸盐衍生物的制剂的方法，硫钼酸盐或硫代钨酸盐类似物的固体剂型，硫代钼酸盐或硫代钨酸盐类似物的固体剂型的制备方法和使用硫代钼酸盐或硫代钨酸盐衍生物的固体剂型的方法治疗或预防与异常血管形成或异常血管发生相关的疾病，铜代谢障碍神经变性障碍和肥胖症在本文中公开。

8. 发明申请

US20100216875A1 METHODS OF TREATING ALZHEIMER'S DISEASE 审中-公开
标题翻译：治疗阿尔茨海默病的方法
公开(公告)号：US20100216875A1
公开(公告)日：2010-08-26
申请号：US12520375
申请日：2007-12-17
申请人： Gregory Hook , Vivian Hook , Robert Ternansky
发明人： Gregory Hook , Vivian Hook , Robert Ternansky
IPC分类号： A61K31/336 , A61P25/28
CPC分类号： A61K38/55 , A61K31/00 , A61K31/075
摘要： The invention is directed to a method of treating Alzheimer's disease. The method comprises administering a cysteine protease inhibitor to a patient and thereby affecting the disease. In a preferred method, the cysteine protease inhibitor is a cathepsin B inhibitor. A preferred method causes a reversal in the progression of the Alzheimer's disease, especially an improvement in cognitive deficit. A preferred method also causes a reduction in Aβ. The method includes using a reversible or irreversible cysteine protease inhibitor or a combination thereof.
摘要翻译：本发明涉及一种治疗阿尔茨海默病的方法。该方法包括向患者施用半胱氨酸蛋白酶抑制剂，从而影响该疾病。在优选的方法中，半胱氨酸蛋白酶抑制剂是组织蛋白酶B抑制剂。优选的方法导致阿尔茨海默病进展逆转，特别是认知缺陷的改善。优选的方法也导致A＆bgr的降低。该方法包括使用可逆或不可逆的半胱氨酸蛋白酶抑制剂或其组合。

9. 发明申请

US20080227806A1 Novel Drugs for Dementia 审中-公开
标题翻译：新药痴呆症
公开(公告)号：US20080227806A1
公开(公告)日：2008-09-18
申请号：US12088202
申请日：2006-09-28
申请人： Robert Ternansky
发明人： Robert Ternansky
IPC分类号： A61K31/44 , C07D405/12 , A61K31/4375 , A61P25/28 , A61K31/40 , C07D471/04
CPC分类号： C07D405/12 , C07D471/04 , C07K5/0205 , C07K5/06034
摘要： The invention is directed to compounds that are prodrugs containing a chemical delivery system (CDS) moiety and a cysteine protease inhibitor moiety. The CDS moiety targets the prodrug to the brain or central nervous system. The cysteine protease inhibitor inhibits cysteine proteases upon release from the prodrug. Cysteine protease inhibitors are effective for treating dementia, Alzheimer's disease and vascular dementia. Targeting the brain or central nervous system offers significant advantages in treating these conditions and diseases. A preferred CDS prodrug is a dihydrotrigoneline CDS moiety coupled to an epoxysuccinyl peptide cysteine protease inhibitor moiety.
摘要翻译：本发明涉及化合物，其是含有化学递送系统（CDS）部分和半胱氨酸蛋白酶抑制剂部分的前药。 CDS部分将前药靶向脑或中枢神经系统。半胱氨酸蛋白酶抑制剂在从前药释放后抑制半胱氨酸蛋白酶。半胱氨酸蛋白酶抑制剂对于治疗痴呆，阿尔茨海默病和血管性痴呆是有效的。针对大脑或中枢神经系统，在治疗这些疾病和疾病方面提供了显着的优势。优选的CDS前药是与环氧琥珀酰肽半胱氨酸蛋白酶抑制剂部分偶联的二氢三配体CDS部分。

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