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1. 发明授权

US07129215B2 Tripeptide and tetrapeptide thioethers 失效
标题翻译：三肽和四肽硫醚
公开(公告)号：US07129215B2
公开(公告)日：2006-10-31
申请号：US11325846
申请日：2006-01-04
申请人： Natalia Aurrecoechea , Andrew B. Kelson , Robert W. Macsata , Louise Robinson , Anthony J. Sanchez , Nicholas M. Santiago , Steven R. Schow , Reyna J. Simon
发明人： Natalia Aurrecoechea , Andrew B. Kelson , Robert W. Macsata , Louise Robinson , Anthony J. Sanchez , Nicholas M. Santiago , Steven R. Schow , Reyna J. Simon
IPC分类号： A61K38/05 , A61K38/06 , C07K5/02
CPC分类号： C07K5/0215 , A61K38/00
摘要： Tripeptide and tetrapeptide thioethers, pharmaceutical compositions containing them, their pharmaceutical use, and their preparation. The compounds are useful in potentiating the cytotoxic effects of chemotherapeutic agents in tumor cells, selectively exerting toxicity in tumor cells, elevating the production of GM progenitors in bone marrow, stimulating the differentiation of bone marrow, mitigating the myelosuppressive effects of chemotherapeutic agents, and modulating hematopoiesis in bone marrow.
摘要翻译：三肽和四肽硫醚，含有它们的药物组合物，它们的药物用途及其制备。该化合物可用于增强化疗药物在肿瘤细胞中的细胞毒性作用，选择性地在肿瘤细胞中发挥毒性，提高骨髓中转基因祖细胞的产生，刺激骨髓分化，减轻化疗药物的骨髓抑制作用，以及调节骨髓造血。

2. 发明授权

US07192918B2 Tripeptide and tetrapeptide sulfones 失效
标题翻译：三肽和四肽砜
公开(公告)号：US07192918B2
公开(公告)日：2007-03-20
申请号：US11326975
申请日：2006-01-05
申请人： Steven R. Schow , Natalia Aurrecoechea
发明人： Steven R. Schow , Natalia Aurrecoechea
IPC分类号： A61K38/06 , A61K38/07
CPC分类号： C07K5/0215 , A61K38/00
摘要： Tripeptide and tetrapeptide sulfones, pharmaceutical compositions containing them, their pharmaceutical use, and their preparation, are disclosed. The compounds are useful in potentiating the cytotoxic effects of chemotherapeutic agents in tumor cells, selectively exerting toxicity in tumor cells, elevating the production of GM progenitors in bone marrow cells, stimulating the differentiation of bone marrow, mitigating the myelosuppressive effects of chemotherapeutic agents, and modulating hematopoiesis in bone marrow.
摘要翻译：公开了三肽和四肽砜，含有它们的药物组合物，它们的药物用途及其制备方法。这些化合物可用于增强化疗药物在肿瘤细胞中的细胞毒性作用，选择性地在肿瘤细胞中发挥毒性，提高骨髓细胞中转基因祖细胞的产生，刺激骨髓分化，减轻化疗药物的骨髓抑制作用，以及调节骨髓造血功能。

3. 发明授权

US08361971B2 Tablet formulation of ezatiostat 失效
标题翻译：片剂制剂
公开(公告)号：US08361971B2
公开(公告)日：2013-01-29
申请号：US13246732
申请日：2011-09-27
申请人： Robert T. Lum , Stephan D. Parent , Chunsheng Qiao , Steven R. Schow
发明人： Robert T. Lum , Stephan D. Parent , Chunsheng Qiao , Steven R. Schow
IPC分类号： A61K38/05 , A61K9/20
CPC分类号： C07K5/0215 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K31/165 , A61K31/216
摘要： Disclosed herein are tablets comprising ezatiostat hydrochloride wherein the ezatiostat hydrochloride comprises from about 75 to about 82 percent by weight of the tablet.
摘要翻译：本文公开了包含盐酸西替伐他汀的片剂，其中盐酸替扎他昔坦包含片剂的约75-约82重量％。

4. 发明授权

US08334266B2 Process for and intermediates in the preparation of canfosfamide and its salts 有权
标题翻译：用于制备卡非司酮及其盐的方法和中间体
公开(公告)号：US08334266B2
公开(公告)日：2012-12-18
申请号：US13429065
申请日：2012-03-23
申请人： William A. Boulanger , Steven J. Collier , Stephen A. Eastham , Dennis L. Edie , Ronan Y. Guevel , Pedro E. Hernandez Abad , R. Jason Herr , Hans J. Kjaersgaard , Harold Meckler , Robert E. Polomski , Steven R. Schow , Pavel E. Zhichkin
发明人： William A. Boulanger , Steven J. Collier , Stephen A. Eastham , Dennis L. Edie , Ronan Y. Guevel , Pedro E. Hernandez Abad , R. Jason Herr , Hans J. Kjaersgaard , Harold Meckler , Robert E. Polomski , Steven R. Schow , Pavel E. Zhichkin
IPC分类号： A61K38/07 , C07K38/06
CPC分类号： C07K5/0205 , A61K38/00 , C07F9/2408 , C07F9/2458 , C07K5/0215 , C07K5/0606 , C07K5/06191
摘要： A process for and intermediates in the preparation of canfosfamide and its salts. Some of the intermediates have anticancer activity.
摘要翻译：一种在制备头孢噻吩及其盐的过程和中间体。一些中间体具有抗癌活性。

5. 发明申请

US20120238772A1 PROCESS FOR AND INTERMEDIATES IN THE PREPARATION OF CANFOSFAMIDE AND ITS SALTS 有权
标题翻译：在制备氰氟虫及其盐的过程和中间体
公开(公告)号：US20120238772A1
公开(公告)日：2012-09-20
申请号：US13429065
申请日：2012-03-23
申请人： William A. Boulanger , Steven J. Collier , Stephen A. Eastham , Dennis L. Edie , Ronan Y. Guevel , Pedro E. Hernández Abad , R. Jason Herr , Hans J. Kjaersgaard , Harold Meckler , Robert E. Polomski , Steven R. Schow , Pavel E. Zhichkin
发明人： William A. Boulanger , Steven J. Collier , Stephen A. Eastham , Dennis L. Edie , Ronan Y. Guevel , Pedro E. Hernández Abad , R. Jason Herr , Hans J. Kjaersgaard , Harold Meckler , Robert E. Polomski , Steven R. Schow , Pavel E. Zhichkin
IPC分类号： C07F9/24 , C07C323/59
CPC分类号： C07K5/0205 , A61K38/00 , C07F9/2408 , C07F9/2458 , C07K5/0215 , C07K5/0606 , C07K5/06191
摘要： A process for and intermediates in the preparation of canfosfamide and its salts. Some of the intermediates have anticancer activity.
摘要翻译：一种在制备头孢噻吩及其盐的过程和中间体。一些中间体具有抗癌活性。

6. 发明授权

US06458998B1 Naphthalene ureas as glucose uptake enhancers 失效
标题翻译：萘脲作为葡萄糖摄取增强剂
公开(公告)号：US06458998B1
公开(公告)日：2002-10-01
申请号：US09579279
申请日：2000-05-25
申请人： Wayne R. Spevak , Songyuan Shi , Prasad V. V. S. V. Manchem , Michael R. Kozlowski , Steven R. Schow , Robert T. Lum
发明人： Wayne R. Spevak , Songyuan Shi , Prasad V. V. S. V. Manchem , Michael R. Kozlowski , Steven R. Schow , Robert T. Lum
IPC分类号： C07C27300
CPC分类号： C07D257/04 , C07C309/51 , C07C311/47 , C07C335/16 , C07C335/18 , C07C335/32 , C07D211/96 , C07D213/76 , C07D233/36 , C07D239/42 , C07D241/20 , C07F9/4021
摘要： Compounds of formula I are useful for treating conditions associated with hyperglycemia, especially Type II diabetes. These compounds are useful in stimulating the kinase activity of the insulin receptor, activating the insulin receptor, and stimulating the uptake of glucose. Pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.
摘要翻译：式I化合物可用于治疗与高血糖相关的病症，特别是II型糖尿病。这些化合物可用于刺激胰岛素受体的激酶活性，激活胰岛素受体，并刺激葡萄糖摄取。还公开了包含抗糖尿病化合物的药物组合物。

7. 发明授权

US06337338B1 Heteroaryl-aryl ureas as IGF-1 receptor antagonists 有权
标题翻译：杂芳基芳基脲作为IGF-1受体拮抗剂
公开(公告)号：US06337338B1
公开(公告)日：2002-01-08
申请号：US09464360
申请日：1999-12-15
申请人： Michael R. Kozlowski , Robert T. Lum , Steven R. Schow , Hugo O. Villar , Micheal M. Wick
发明人： Michael R. Kozlowski , Robert T. Lum , Steven R. Schow , Hugo O. Villar , Micheal M. Wick
IPC分类号： A61K3147
CPC分类号： A61K31/4706 , A61K31/425 , A61K31/47 , A61K2300/00
摘要： Methods for treating diseases associated with the activity of the insulin growth factor-1 receptor (IGF-1R), such as cancer, are provided. Methods for inhibiting cell growth and proliferation, especially of tumor cells, and promoting apoptosis are also provided. Each of these methods employs the use of a heteroaryl-aryl urea compound as an antagonist for IGF-1R.
摘要翻译：提供了治疗与胰岛素生长因子-1受体（IGF-1R）的活性相关的疾病如癌症的方法。还提供了抑制细胞生长和增殖，特别是肿瘤细胞增殖和促进细胞凋亡的方法。这些方法中的每一种都使用杂芳基 - 芳基脲化合物作为IGF-1R的拮抗剂。

8. 发明申请

US20080159980A1 Combination cancer therapy with a GST-activated anticancer compound and another anticancer therapy 审中-公开
标题翻译：组合癌症治疗与GST活化的抗癌化合物和另一种抗癌疗法
公开(公告)号：US20080159980A1
公开(公告)日：2008-07-03
申请号：US11872659
申请日：2007-10-15
申请人： Hua Xu , Gail L. Brown , Steven R. Schow , James G. Keck
发明人： Hua Xu , Gail L. Brown , Steven R. Schow , James G. Keck
IPC分类号： A61K31/664 , A61K38/20 , A61K38/21 , A61K39/395 , A61K31/704 , A61P35/00
CPC分类号： A61K45/06 , A61K31/282 , A61K31/337 , A61K31/475 , A61K31/5377 , A61K31/70 , A61K38/05 , A61K2300/00
摘要： A method of combination cancer therapy in a mammal, especially a human, by administering a therapeutically effective amount of a GST-activated anticancer compound and a therapeutically effective amount of another anticancer therapy, that is, an anticancer therapy that is not a treatment with a GST- activated anticancer compound (including chemotherapy; molecular targeted therapy; biologic therapy; and radiotherapy, used as monotherapy or in combination). Pharmaceutical compositions, products, and kits for the method. The use of a GST-activated anticancer compound in the manufacture of a medicament for the method. A method of potentiating an anticancer therapy in a mammal, especially a human, comprising administering a therapeutically effective amount of a GST-activated anticancer compound to the mammal being treated with the anticancer therapy. The use of a GST-activated anticancer compound in the manufacture of a medicament for the method. The GST-activated anticancer compound is preferably a compound of U.S. Pat. No. 5,556,942, and more preferably TLK286, especially as the hydrochloride salt.
摘要翻译：通过施用治疗有效量的GST活化的抗癌化合物和治疗有效量的另一种抗癌疗法，即哺乳动物，特别是人的组合癌症治疗的方法，即不是治疗的抗癌疗法 GST活化的抗癌化合物（包括化学疗法;分子靶向治疗;生物治疗和放疗，用作单一疗法或组合）。用于该方法的药物组合物，产品和试剂盒。使用GST活化的抗癌化合物在制备该方法的药物中的用途。一种增强哺乳动物，特别是人类抗癌疗法的方法，包括向用抗癌疗法治疗的哺乳动物施用治疗有效量的GST活化抗癌化合物。使用GST活化的抗癌化合物在制备该方法的药物中的用途。 GST活化的抗癌化合物优选为美国专利No. 更优选TLK 286，特别是作为盐酸盐。

9. 发明授权

US07262182B2 Sulfonylethyl phosphorodiamidates 失效
标题翻译：磺酰基乙基磷酰胺
公开(公告)号：US07262182B2
公开(公告)日：2007-08-28
申请号：US11134218
申请日：2005-05-20
申请人： Louise Robinson , Steven R. Schow , Songyuan Shi
发明人： Louise Robinson , Steven R. Schow , Songyuan Shi
IPC分类号： A61K31/66 , C07F9/02
CPC分类号： C07F9/2458 , C07F9/2408 , C07F9/572 , C07F9/58 , C07F9/59 , C07F9/650952 , C07F9/6533 , C07F9/65515 , C07F9/655345 , C07F9/65616
摘要： Sulfonylethyl and thioethyl phosphorodiamidates, their preparation and intermediates in their preparation, formulations containing them, and their pharmaceutical use. The compounds are useful for treating cancer, alone and in combination with other anticancer therapies.
摘要翻译：磺基乙基和硫代乙基磷酰二胺，它们的制备和中间体在制备中，含有它们的制剂及其药物用途。该化合物可用于单独治疗和与其它抗癌疗法组合治疗癌症。

10. 发明授权

US06790958B2 Purine inhibitors of cyclin dependent kinase 2 & IKBA 失效
标题翻译：细胞周期蛋白依赖性激酶2和IKBA的嘌呤抑制剂
公开(公告)号：US06790958B2
公开(公告)日：2004-09-14
申请号：US09929772
申请日：2001-08-14
申请人： Robert T. Lum , Cheri Lynn Blum , Richard Mackman , Michael M. Wick , Steven R. Schow , Jeffery A. Zablocki , Prabbha Ibrahim
发明人： Robert T. Lum , Cheri Lynn Blum , Richard Mackman , Michael M. Wick , Steven R. Schow , Jeffery A. Zablocki , Prabbha Ibrahim
IPC分类号： C07D47304
CPC分类号： B60R1/00 , C07D473/16 , C07D473/40 , G08G1/163
摘要： Compounds of the following formula are provided: wherein: R1 is —X—R1′; in which R1′ is alkyl, cycloalkyl, aryl, aralkyl, hetaryl, or heterocyclyl, all of which are optionally substituted; X is —NH; R2 is optionally substituted lower alkyl; and R3 is —NR4R5; in which R4 and R5 independently are hydrogen or lower alkyl optionally substituted by hydroxy or amino; or acid addition salts or cationic salts thereof. The compounds inhibit CDK-2 activity and are useful for treating disorders characterized by undesirable cell proliferation.
摘要翻译：提供下式的化合物：其中：R1是-X-R1'; 其中R 1'是烷基，环烷基，芳基，芳烷基，杂芳基或杂环基，其全部是任选取代的; X是-NH; R 2是任选取代的低级烷基; 和R 3是-NR 4 R 5; 其中R4和R5独立地是氢或任选被羟基或氨基取代的低级烷基; 或其酸加成盐或阳离子盐。该化合物抑制CDK-2活性，并且可用于治疗以不期望的细胞增殖为特征的疾病。

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