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1. 发明授权

US06635621B1 Cysteine protease inhibitors 失效
标题翻译：半胱氨酸蛋白酶抑制剂
公开(公告)号：US06635621B1
公开(公告)日：2003-10-21
申请号：US10048396
申请日：2002-01-30
申请人： Rajeshwar Singh , Nian Zhou , Andhe V. N. Reddy , George Thomas , Qizhu Ding , Jadwiga Kaleta , Ronald George Micetich , Mark Whittaker
发明人： Rajeshwar Singh , Nian Zhou , Andhe V. N. Reddy , George Thomas , Qizhu Ding , Jadwiga Kaleta , Ronald George Micetich , Mark Whittaker
IPC分类号： C07D29512
CPC分类号： C07D295/125 , A61K38/00 , C07D207/14 , C07D333/38 , C07K5/06043 , C07K5/06078
摘要： This invention relates to derivatives of alpha-amino acid amides, to pharmaceutical compositions containing such compounds, and to their use in medicine as inhibitors of cysteine proteases, particularly the cathepsins. A compound of formula (I) is described or a pharmaceutically acceptable salt, hydrate or solvate thereof. Pharmaceutically acceptable salts of the compounds of this invention include the sodium, potassium, magnesium, calcium, hydrogen chloride, tartaric acid, succinic acid, fumaric acid and p-toluenesulfonic acid salts.
摘要翻译：本发明涉及α-氨基酸酰胺的衍生物，含有这些化合物的药物组合物，以及它们在医学上作为半胱氨酸蛋白酶特别是组织蛋白酶抑制剂的用途。描述式（I）化合物或其药学上可接受的盐，水合物或溶剂合物。本发明化合物的药学上可接受的盐包括钠，钾，镁，钙，氯化氢，酒石酸，琥珀酸，富马酸和对甲苯磺酸盐。

2. 发明授权

US06232305B1 Substituted amino bicyclic-&bgr;-lactam penam and cepham derivatives as cysteine protease inhibitors 失效
标题翻译：取代的氨基双环β-内酰胺penam和cepham衍生物作为半胱氨酸蛋白酶抑制剂
公开(公告)号：US06232305B1
公开(公告)日：2001-05-15
申请号：US09010993
申请日：1998-01-22
申请人： Rajeshwar Singh , Nian Zhou , Deqi Guo , Ronald G. Micetich
发明人： Rajeshwar Singh , Nian Zhou , Deqi Guo , Ronald G. Micetich
IPC分类号： C07D49940
CPC分类号： C07D499/00 , C07D501/00
摘要： The present invention provides substituted amino bicyclic-&bgr;-lactam penam derivatives and substituted amino bicyclic-&bgr;-lactam cepham derivatives and their diastereoisomers of formula I, as well as compositions, methods of making, and methods of using, which exhibit excellent cysteine protease inhibitory activity and which may be used for treatment of different diseases such as cancer (including cancer metastasis), osteoporosis, rheumatoid arthritis. muscular dystrophy, myocardial infarction, pulmonary emphysema, septic shock, cerebral ischemia, decreased memory function, Alzheimer, cataract, malaria, glomerular basement membrane degradation, bacterial infection, inflammatory diseases, parasitic infections and viral infections, wherein R is a peptidyl residue of a single natural &agr;-amino acid selected from a specific group of natural &agr;-amino acids or a peptidyl residue of a single non-natural amino acid selected from a specified group of non-natural amino acids, in which natural or non-natural peptidyl residue the terminal —NH2 group is unsubstituted or substituted once or twice with group R4, wherein R4 is selected from the group consisting of —COOR5, —COR5, —SO2R5, and —COR6, R6 is an amino group which is unsubstituted or substituted at least once with a C1-C6 alkyl group which is unsubstituted or substituted, R1 is selected from the group consisting of hydrogen, hydroxy, carboxy, —COOR6, —OR7, —CONHR7, and C1-C5 alkyl, in which the C1-C6 alkyl is unsubstituted or substituted, R2 and R3 are independently hydrogen or C1-C3 alkyl which is unsubstituted or substituted, n is 0, 1, or 2, and n1 is 0 or 1.
摘要翻译：本发明提供了取代的氨基双环β-内酰胺penam衍生物和取代的氨基双环-β-内酰胺头孢烯衍生物及其非对映异构体I，以及组合物，制备方法和使用方法，其表现出优异的半胱氨酸蛋白酶抑制活性，其可用于治疗诸如癌症（包括癌症转移），骨质疏松症，类风湿性关节炎等不同疾病。肌肉营养不良，心肌梗死，肺气肿，败血性休克，脑缺血，记忆功能下降，阿尔茨海默病，白内障，疟疾，肾小球基底膜降解，细菌感染，炎症性疾病，寄生虫感染和病毒感染，其中R是单一肽的肽基残基选自特定天然α-氨基酸组的天然α-氨基酸或选自特定非天然氨基酸组的单一非天然氨基酸的肽基残基，其中天然或非天然肽基残基末端-NH 2基团是未取代的或被基团R4取代一次或两次，其中R 4选自-COOR 5，-COR 5，-SO 2 R 5和-COR 6，R 6是未被取代或取代至少一次的氨基与未取代或取代的C1-C6烷基，R1选自氢，羟基，羧基，-COOR6，-OR7，-CONHR7和C1-C5烷基，其中 C 1 -C 6烷基是未取代或取代的，R 2和R 3独立地是氢或未被取代或取代的C 1 -C 3烷基，n是0,1或2，且n 1是0或1。

3. 发明授权

US07701092B1 Connector module with embedded power-over-ethernet voltage isolation and method 有权
标题翻译：具有嵌入式以太网电压隔离和方法的连接器模块
公开(公告)号：US07701092B1
公开(公告)日：2010-04-20
申请号：US10741920
申请日：2003-12-19
申请人： Timothy J. Parker , Nian Zhou
发明人： Timothy J. Parker , Nian Zhou
IPC分类号： H02J1/00 , H02B1/24
CPC分类号： H04L12/10 , Y10T307/297
摘要： A connector module includes a jack socket capable of receiving a communication link. The connector module also includes magnetics coupled to the jack socket for supplying power to a peripheral device coupled to the link through the jack socket. The connector module further includes Power-over-Ethernet management logic for controlling the supplying of power to the peripheral device by providing a voltage to the magnetics. In addition, the connector module includes at least one voltage isolator for isolating the voltage used by the Power-over-Ethernet management logic from at least one digitally-referenced voltage.
摘要翻译：连接器模块包括能够接收通信链路的插座。连接器模块还包括耦合到插座插座的磁体，用于通过插座插座向耦合到链路的外围设备供电。连接器模块还包括以太网供电管理逻辑，用于通过向磁体提供电压来控制向外围设备供电。此外，连接器模块包括至少一个电压隔离器，用于将由以太网供电管理逻辑使用的电压与至少一个数字参考电压隔离。

4. 发明申请

US20150017673A1 COMPOSITIONS AND METHODS FOR DRUG-SENSITIZATION OR INHIBITION OF A CANCER CELL 审中-公开
标题翻译：用于药物敏感性或抑制癌症细胞的组合物和方法
公开(公告)号：US20150017673A1
公开(公告)日：2015-01-15
申请号：US14013842
申请日：2013-08-29
申请人： James Sacchettini , Nian Zhou , Dwight Baker , Steven A. Maxwell , Deeann Wallis
发明人： James Sacchettini , Nian Zhou , Dwight Baker , Steven A. Maxwell , Deeann Wallis
IPC分类号： G01N33/84 , G01N33/58 , A61K31/435
CPC分类号： A61K31/395 , A61K31/122 , A61K31/136 , A61K31/337 , A61K31/435 , A61K31/4745 , A61K31/475 , A61K31/5377 , A61K31/573 , A61K31/675 , A61K31/69 , A61K31/704 , A61K31/7068 , A61K33/24 , A61K38/08 , A61K45/06 , C07D498/22 , G01N33/582 , G01N33/84 , G01N2800/52 , A61K2300/00
摘要： The disclosure provides rifamycin and rifamycin derivative compositions, including rifabutin and rifabutin derivative compositions able to cause drug-sensitization in a cancer cell or inhibition of a cancer cell. The disclosure also provides methods of administering such compositions to cancer cells to sensitize them to drugs, such as chemotherapeutics, or directly inhibit them. The disclosure also provides methods of administering such compositions to increase reactive oxygen species (ROS), particularly superoxides, in cancer cells. The disclosure further provides methods of determining whether a cancer will respond to chemotherapeutics and whether to administer rifamycin or a rifamycin derivative based on ROS levels in cancer cells of a patient.
摘要翻译：本公开提供了利福霉素和利福霉素衍生物组合物，其包括能够在癌细胞中引起药物敏化或抑制癌细胞的利福布丁和利福布汀衍生物组合物。本公开还提供了将这种组合物施用于癌细胞以使其对药物（例如化学治疗剂）敏化或直接抑制它们的方法。本公开还提供了施用这样的组合物以增加癌细胞中的活性氧（ROS），特别是超氧化物的方法。本公开进一步提供了确定癌症是否将响应化学治疗剂以及是否施用基于患者的癌细胞中的ROS水平的利福霉素或利福霉素衍生物的方法。

5. 发明申请

US20070072835A1 Method of preparing and use of prodrugs of betulinic acid derivatives 审中-公开
标题翻译：制备和使用桦木酸衍生物前药的方法
公开(公告)号：US20070072835A1
公开(公告)日：2007-03-29
申请号：US11477177
申请日：2006-06-28
申请人： John Pezzuto , Jerome Kosmeder , Ze-Qi Xu , Nian Zhou , Miriam Goldsmith
发明人： John Pezzuto , Jerome Kosmeder , Ze-Qi Xu , Nian Zhou , Miriam Goldsmith
IPC分类号： A61K31/56
CPC分类号： C07J1/00 , A61K31/56 , C07J63/008
摘要： A composition and method of preventing or inhibiting tumor growth and, more particularly, of treating a malignant tumor, using prodrugs of plant-derived compounds and derivatives is disclosed. In the method, a composition containing betulinic acid or a betulinic acid derivative is administered in a prodrug form to release betulinic acid or a betulinic acid derivative in vivo at the tumor site.
摘要翻译：公开了使用植物衍生化合物和衍生物的前药来预防或抑制肿瘤生长，更具体地治疗恶性肿瘤的组合物和方法。在该方法中，含有桦木酸或桦木酸衍生物的组合物以前药形式给药以在肿瘤部位体内释放桦木酸或桦木酸衍生物。

6. 发明申请

US20060079520A1 Sulfonamide peri-substituted bicyclics for occlusive artery disease 失效
公开(公告)号：US20060079520A1
公开(公告)日：2006-04-13
申请号：US11169161
申请日：2005-06-27
申请人： Jasbir Singh , Mark Gurney , Georgeta Hategan , Peng Yu , David Zembower , Nian Zhou
发明人： Jasbir Singh , Mark Gurney , Georgeta Hategan , Peng Yu , David Zembower , Nian Zhou
IPC分类号： A61K31/538 , A61K31/4704 , A61K31/43 , A61K31/4188 , A61K31/4162 , C07D498/04 , C07D487/04
CPC分类号： C07D263/58 , C07D209/12 , C07D209/30 , C07D209/34 , C07D401/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D471/04 , C07D487/04 , C07D513/04
摘要： Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. The compounds are of the general formula A representative example is:

7. 发明授权

US07714017B2 Carboxylic acid peri-substituted bicyclics for occlusive artery disease 有权
标题翻译：用于闭塞性动脉疾病的羧酸邻位取代双环体
公开(公告)号：US07714017B2
公开(公告)日：2010-05-11
申请号：US11247431
申请日：2005-10-11
申请人： Jasbir Singh , Mark Gurney , Georgeta Hategan , Peng Yu , David Zembower , Nian Zhou , Alexandre Mikhaylovich Polozov , Wayne Edward Zeller
发明人： Jasbir Singh , Mark Gurney , Georgeta Hategan , Peng Yu , David Zembower , Nian Zhou , Alexandre Mikhaylovich Polozov , Wayne Edward Zeller
IPC分类号： A61K31/403 , A61K31/404 , A61K31/405 , C07D209/02 , C07D209/04 , A61K31/19 , A61K31/192 , C07C61/12
CPC分类号： C07D263/58 , C07D209/08 , C07D209/12 , C07D209/34 , C07D235/06 , C07D487/04 , C07D513/04
摘要： Peri-substituted, fused bicyclic ring carboxylic acids useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. The compounds are of the general formula A representative example is:
摘要翻译：公开了用于治疗或预防前列腺素介导的疾病或病症的环取代的稠合双环羧酸。化合物具有通式A的代表性实例是：

8. 发明申请

US20090291948A1 SULFONAMIDE PERI-SUBSTITUTED BICYCLICS FOR OCCLUSIVE ARTERY DISEASE 审中-公开
标题翻译：磺胺类药物替代自杀性疾病的双因素
公开(公告)号：US20090291948A1
公开(公告)日：2009-11-26
申请号：US12534390
申请日：2009-08-03
申请人： Jasbir Singh , Mark E. Gurney , Georgeta Hategan , Peng Yu , David Zembower , Nian Zhou
发明人： Jasbir Singh , Mark E. Gurney , Georgeta Hategan , Peng Yu , David Zembower , Nian Zhou
IPC分类号： A61K31/538 , C07D403/02 , A61K31/4162 , G01N33/566 , C07D513/04 , C07D487/02 , A61K31/429 , A61K31/4188 , A61K31/47 , C07D215/02 , C07D215/227 , C07D265/36 , C07D209/04 , A61K31/405 , A61P29/00 , A61P9/10
CPC分类号： C07D263/58 , C07D209/12 , C07D209/30 , C07D209/34 , C07D401/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D471/04 , C07D487/04 , C07D513/04
摘要： Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. The compounds are of the general formula A representative example is:
摘要翻译：公开了用于治疗或预防前列腺素介导的疾病或病症的酰基磺酰胺，邻位取代的稠合双环化合物。化合物具有通式A的代表性实例是：

9. 发明授权

US07598397B2 Sulfonamide peri-substituted bicyclics for occlusive artery disease 失效
标题翻译：用于闭塞性动脉疾病的磺酰胺邻位取代的双环体
公开(公告)号：US07598397B2
公开(公告)日：2009-10-06
申请号：US11169161
申请日：2005-06-27
申请人： Jasbir Singh , Mark E. Gurney , Georgeta Hategan , Peng Yu , David Zembower , Nian Zhou
发明人： Jasbir Singh , Mark E. Gurney , Georgeta Hategan , Peng Yu , David Zembower , Nian Zhou
IPC分类号： C07D411/00
CPC分类号： C07D263/58 , C07D209/12 , C07D209/30 , C07D209/34 , C07D401/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D471/04 , C07D487/04 , C07D513/04
摘要： Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. The compounds are of the general formula A representative example is:
摘要翻译：公开了用于治疗或预防前列腺素介导的疾病或病症的酰基磺酰胺，邻位取代的稠合双环化合物。化合物具有通式A的代表性实例是：

10. 发明申请

US20060142355A1 Carboxylic acid peri-substituted bicyclics for occlusive artery disease 有权
标题翻译：用于闭塞性动脉疾病的羧酸邻位取代双环
公开(公告)号：US20060142355A1
公开(公告)日：2006-06-29
申请号：US11247431
申请日：2005-10-11
申请人： Jasbir Singh , Mark Gurney , Georgeta Hategan , Peng Yu , David Zembower , Nian Zhou , Alexandre Polozov , Wayne Zeller
发明人： Jasbir Singh , Mark Gurney , Georgeta Hategan , Peng Yu , David Zembower , Nian Zhou , Alexandre Polozov , Wayne Zeller
IPC分类号： A61K31/43 , A61K31/4188 , A61K31/4162 , C07D498/02 , C07D487/02
CPC分类号： C07D263/58 , C07D209/08 , C07D209/12 , C07D209/34 , C07D235/06 , C07D487/04 , C07D513/04
摘要： Peri-substituted, fused bicyclic ring carboxylic acids useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. The compounds are of the general formula A representative example is:
摘要翻译：公开了用于治疗或预防前列腺素介导的疾病或病症的环取代的稠合双环羧酸。化合物具有通式A的代表性实例是：

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