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1. 发明申请

WO2011140232A3 DESAZADESFERROTHIOCIN AND DESAZADESFERROTHIOCIN POLYETHER ANALOGUES AS METAL CHELATION AGENTS 审中-公开
标题翻译：作为金属螯合剂的DESAZADESFERROTHIOCIN和DESAZADESFERROTHIOCIN聚醚类似物
公开(公告)号：WO2011140232A3
公开(公告)日：2012-02-23
申请号：PCT/US2011035211
申请日：2011-05-04
申请人： FERROKIN BIOSCIENCES INC , MALECHA JAMES W
发明人： MALECHA JAMES W
IPC分类号： C07D263/16 , A61K31/4164 , A61K31/421 , A61P3/10 , A61P31/12 , C07D231/14 , C07D233/22 , C07D263/14
CPC分类号： C07D263/16 , C07D231/14 , C07D233/28 , C07D277/12 , C07D277/56
摘要： Disclosed herein are new compounds of desazadesferrothiocin polyether (DADFT- PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.
摘要翻译：本文公开了新型的脱氮硫代酯聚醚（DADFT-PE）类似物的化合物，以及包含它们的药物组合物及其作为用于治疗疾病的金属螯合剂的应用。还提供了人或动物受试者中铁和其他金属的螯合方法用于治疗金属过载和毒性。

2. 发明申请

WO2008011557A3 HETEROARYL INHIBITORS OF RHO KINASE 审中-公开
标题翻译：杂合子抑制剂RHO激酶
公开(公告)号：WO2008011557A3
公开(公告)日：2008-07-31
申请号：PCT/US2007073967
申请日：2007-07-20
申请人： BORCHARDT ALLEN J , KAHRAMAN MEHMET , COOK TRAVIS G , DAVIS ROBERT L , GARDINER ELISABETH M M , MALECHA JAMES W , NOBLE STEWART A , PRINS THOMAS J , SERTIC MICHAEL , SIEGEL DANA L
发明人： BORCHARDT ALLEN J , KAHRAMAN MEHMET , COOK TRAVIS G , DAVIS ROBERT L , GARDINER ELISABETH M M , MALECHA JAMES W , NOBLE STEWART A , PRINS THOMAS J , SERTIC MICHAEL , SIEGEL DANA L
IPC分类号： C07D401/04 , A61K31/4375 , A61K31/4439 , A61P27/00 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
CPC分类号： A61K31/395 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds and methods which may be useful as inhibitors of Rho kinase for the treatment or prevention of disease.
摘要翻译：本发明涉及可用作Rho激酶抑制剂用于治疗或预防疾病的化合物和方法。

3. 发明申请

WO2008045663A2 ARYL-SUBSTITUTED HETEROCYCLIC INHIBITORS OF PDE4 审中-公开
标题翻译： ARYL取代的PDE4的杂环化合物抑制剂
公开(公告)号：WO2008045663A2
公开(公告)日：2008-04-17
申请号：PCT/US2007/078980
申请日：2007-09-20
申请人： KALYPSYS, INC. , GOVEK, Steven, P. , OSHIRO, Guy , NOBLE, Stewart, A. , MALECHA, James, W. , SHIAU, Andrew, K.
发明人： GOVEK, Steven, P. , OSHIRO, Guy , NOBLE, Stewart, A. , MALECHA, James, W. , SHIAU, Andrew, K.
IPC分类号： A61K31/415 , A61K31/4155 , A61K31/4709 , A61P29/00 , A61P27/02 , A61P27/06
CPC分类号： A61K31/415 , A61K31/4155 , A61K31/4709
摘要： Disclosed herein are potent and selective aryl-substituted heterocyclic compounds, useful as inhibitors of phosphodiesterase 4 (PDE4), compositions comprising the same, and their application as pharmaceuticals for the treatment of disease. Methods of inhibition of PDE4 activity are also provided, as well as methods for the treatment of inflammatory diseases and other diseases in which PDE4 or one of its isoforms may play a role.
摘要翻译：本文公开了有效和选择性的芳基取代的杂环化合物，其可用作磷酸二酯酶4（PDE4）的抑制剂，包含其的组合物及其作为用于治疗疾病的药物的应用。还提供了抑制PDE4活性的方法，以及治疗炎性疾病和其中PDE4或其一种同工型可能发挥作用的其它疾病的方法。

4. 发明申请

WO2007137098A3 SULFONYL-SUBSTITUTED BICYCLIC COMPOUNDS AS MODULATORS OF PPAR 审中-公开
公开(公告)号：WO2007137098A3
公开(公告)日：2007-11-29
申请号：PCT/US2007/069083
申请日：2007-05-16
申请人： KALYPSYS, INC. , MALECHA, James, W. , NOBLE, Stewart, A. , DURON, Sergio, G. , LINDSTROM, Andrew, K. , SHIAU, Andrew, K. , GOVEK, Steven, P.
发明人： MALECHA, James, W. , NOBLE, Stewart, A. , DURON, Sergio, G. , LINDSTROM, Andrew, K. , SHIAU, Andrew, K. , GOVEK, Steven, P.
IPC分类号： C07D295/22 , A61K31/495 , A61P3/04 , A61P3/06
摘要： The present invention relates to compounds of structural Formula XIII and methods useful as inhibitors of PPAR, particularly PPARdelta, and for the treatment or prevention of PPAR-mediated diseases, including metabolic diseases.

5. 发明申请

WO2007137098A2 SULFONYL-SUBSTITUTED BICYCLIC COMPOUNDS AS MODULATORS OF PPAR 审中-公开
标题翻译：作为PPAR的调节剂的磺基取代的双环化合物
公开(公告)号：WO2007137098A2
公开(公告)日：2007-11-29
申请号：PCT/US2007069083
申请日：2007-05-16
申请人： KALYPSYS INC , MALECHA JAMES W , NOBLE STEWART A , DURON SERGIO G , LINDSTROM ANDREW K , SHIAU ANDREW K , GOVEK STEVEN P
发明人： MALECHA JAMES W , NOBLE STEWART A , DURON SERGIO G , LINDSTROM ANDREW K , SHIAU ANDREW K , GOVEK STEVEN P
IPC分类号： C07D295/22 , A61K31/495 , A61P3/04 , A61P3/06
CPC分类号： C07D295/26
摘要： The present invention relates to compounds and methods useful as inhibitors of PPAR, particularly PPARd, and for the treatment or prevention of PPAR-mediated diseases, including metabolic diseases.
摘要翻译：本发明涉及可用作PPAR抑制剂，特别是PPARd的化合物和方法，以及用于治疗或预防包括代谢性疾病在内的PPAR介导的疾病。

6. 发明申请

WO2008045664A2 HETEROCYCLIC INHIBITORS OF PDE4 审中-公开
标题翻译： PDE4的杂环抑制剂
公开(公告)号：WO2008045664A2
公开(公告)日：2008-04-17
申请号：PCT/US2007/078984
申请日：2007-09-20
申请人： KALYPSYS, INC. , GOVEK, Steven, P. , OSHIRO, Guy , NOBLE, Stewart, A. , MALECHA, James, W. , SHIAU, Andrew, K.
发明人： GOVEK, Steven, P. , OSHIRO, Guy , NOBLE, Stewart, A. , MALECHA, James, W. , SHIAU, Andrew, K.
IPC分类号： A61K31/166 , A61K31/4162 , A61K31/4192 , A61K31/4365 , A61K31/443 , A61K31/4741 , A61K31/498 , A61K31/4985 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/53 , A61K31/538 , A61K31/4015 , A61K31/428
CPC分类号： A61K31/519 , A61K31/166 , A61K31/4015 , A61K31/4162 , A61K31/4192 , A61K31/428 , A61K31/4365 , A61K31/443 , A61K31/4741 , A61K31/498 , A61K31/4985 , A61K31/505 , A61K31/506 , A61K31/53 , A61K31/538
摘要： The present invention is directed to potent and selective heterocyclic compounds, useful as inhibitors of phosphodiesterase 4 (PDE4), compositions comprising the same, and their application as pharmaceuticals for the treatment of disease. Methods of inhibition of PDE4 activity are also provided, as well as methods for the treatment of inflammatory diseases and other diseases in which PDE4 or one of its isoforms may play a role.
摘要翻译：本发明涉及有效和选择性的杂环化合物，其可用作磷酸二酯酶4（PDE4）的抑制剂，包含其的组合物及其作为用于治疗疾病的药物的应用。还提供了抑制PDE4活性的方法，以及治疗炎性疾病和其中PDE4或其一种同工型可能发挥作用的其它疾病的方法。

7. 发明申请

WO2008011560A2 BENZOTHIOPHENE INHIBITORS OF RHO KINASE 审中-公开
标题翻译：苯并噻吩对RHO激酶的抑制剂
公开(公告)号：WO2008011560A2
公开(公告)日：2008-01-24
申请号：PCT/US2007/073971
申请日：2007-07-20
申请人： KAHRAMAN, Mehmet , BORCHARDT, Allen, J. , COOK, Travis, G. , DAVIS, Robert, L. , GARDINER, Elisabeth, M.m. , MALECHA, James, W. , NOBLE, Stewart, A. , PRINS, Thomas, J.
发明人： KAHRAMAN, Mehmet , BORCHARDT, Allen, J. , COOK, Travis, G. , DAVIS, Robert, L. , GARDINER, Elisabeth, M.m. , MALECHA, James, W. , NOBLE, Stewart, A. , PRINS, Thomas, J.
CPC分类号： A61K31/395 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds and methods which may be useful as inhibitors of Rho kinase for the treatment or prevention of disease.
摘要翻译：本发明涉及可用作Rho激酶抑制剂用于治疗或预防疾病的化合物和方法。

8. 发明申请

WO2008011557A2 HETEROARYL INHIBITORS OF RHO KINASE 审中-公开
标题翻译： RHO激酶的HETEROARYL抑制剂
公开(公告)号：WO2008011557A2
公开(公告)日：2008-01-24
申请号：PCT/US2007/073967
申请日：2007-07-20
申请人： BORCHARDT, Allen, J. , KAHRAMAN, Mehmet , COOK, Travis, G. , DAVIS, Robert, L. , GARDINER, Elisabeth, M., M. , MALECHA, James, W. , NOBLE, Stewart, A. , PRINS, Thomas, J. , SERTIC, Michael , SIEGEL, Dana, L.
发明人： BORCHARDT, Allen, J. , KAHRAMAN, Mehmet , COOK, Travis, G. , DAVIS, Robert, L. , GARDINER, Elisabeth, M., M. , MALECHA, James, W. , NOBLE, Stewart, A. , PRINS, Thomas, J. , SERTIC, Michael , SIEGEL, Dana, L.
CPC分类号： A61K31/395 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds and methods which may be useful as inhibitors of Rho kinase for the treatment or prevention of disease.
摘要翻译：本发明涉及可用作Rho激酶抑制剂用于治疗或预防疾病的化合物和方法。

9. 发明申请

WO2004110418A2 CARBONYL COMPOUNDS AS INHIBITORS OF HISTONE DEACETYLASE FOR THE TREATMENT OF DISEASE 审中-公开
标题翻译：作为用于治疗疾病的组胺脱乙酰酶的抑制剂的碳化合物
公开(公告)号：WO2004110418A2
公开(公告)日：2004-12-23
申请号：PCT/US2004/018502
申请日：2004-06-10
申请人： KALYPSYS, INC. , WASH, Paul, L. , WILEY, Brandon, M. , HASSIG, Christian , MALECHA, James, W. , NOBLE, Stewart, A.
发明人： WASH, Paul, L. , WILEY, Brandon, M. , HASSIG, Christian , MALECHA, James, W. , NOBLE, Stewart, A.
IPC分类号： A61K31/00
CPC分类号： C07C323/49 , C07C323/67 , C07C327/30 , C07D277/16 , C07D277/36 , C07D295/112 , C07D319/18 , C07D417/12
摘要： Disclosed herein are carbonyl compounds of Formula (I), (II) or (III), and others as described herein. Also disclosed are methods of treating disease, such as cancer, neurological disorders, including polyglutamine-repeat disorders, anemias, thalassemias, inflammatory conditions, autoimmune diseases and cardiovascular conditions, using the compounds of the invention. In addition, methods of modulating the activity of histone deacetylase (HDAC) are also disclosed.
摘要翻译：本文公开的是式（I），（II）或（III）的羰基化合物和本文所述的其它物质。还公开了使用本发明的化合物治疗诸如癌症的疾病，包括多聚谷氨酰胺重复病症，贫血，地贫，炎性病症，自身免疫性疾病和心血管疾病的疾病的方法。此外，还公开了调节组蛋白脱乙酰酶（HDAC）的活性的方法。

10. 发明申请

WO2003099775A1 SULFONE LIVER X-RECEPTOR MODULATORS 审中-公开
标题翻译： SULFONE肝脏X受体调节剂
公开(公告)号：WO2003099775A1
公开(公告)日：2003-12-04
申请号：PCT/US2003/016381
申请日：2003-05-23
申请人： PHARMACIA CORPORATION , BECKER, Daniel, P. , DECRESCENZO, Gary, A. , MALECHA, James, W. , MIYASHIRO, Julie, M. , VAN CAMP, Jennifer, Ann , COLLINS, Joe, T.
发明人： BECKER, Daniel, P. , DECRESCENZO, Gary, A. , MALECHA, James, W. , MIYASHIRO, Julie, M. , VAN CAMP, Jennifer, Ann , COLLINS, Joe, T.
IPC分类号： C07C317/22
CPC分类号： C07C317/22 , C07C317/24
摘要： The present invention is directed to slective LXR modulators, small molecule compounds corresponding to Formula (I) wherein: R 1 and R 2 are independently hydrogen or optionally substituted alkyl, alkenyl, aryl, acyi, or alkaryl; R 3 is optionally substituted alkyl or aryl; each R 4 is independently hydrogen, alkyl, aryl,.heteroaryl, hydroxy, alkoxy, cyano, nitro, amino, alkenyl, alkynyl, amido, alkylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, haloalkylcarbonyl, alkylthiocarbonyl, arylthlocarbonyl, alkyl optionally substituted with one or more substituent selected from lower alkyl, halogen, hydroxyl, haloalkyl, cyano, nitro, carboxyl, amino, alkoxy and aryl, or aryl optionally substituted with one or more substituent selected from hydrogen, halogen, haloalkyl, hydroxy, lower alkyl, alkoxy, methylene dioxy, ethylenedioxy, cyano, nitro, atkylthio, alkylsulfonyl, sulfonic acid, sulfonamide, carboxyl derivatives, amino, aryl and heteroaryl; and a is 0-4, and is further directed to a process of treating a condition in a mammal that is modulated by LXR using a therapeutically effective dose of a compound of Formula I.
摘要翻译：本发明涉及选择性LXR调节剂，对应于式（I）的小分子化合物，其中：R 1和R 2独立地为氢或任选取代的烷基，烯基，芳基，酰基或烷芳基; R3是任选取代的烷基或芳基; 每个R 4独立地是氢，烷基，芳基，杂芳基，羟基，烷氧基，氰基，硝基，氨基，烯基，炔基，酰氨基，烷基羰基，烷氧基羰基，芳氧基羰基，卤代烷基羰基，烷硫基羰基，芳基羰基羰基，任选地被一个或多个取代基由低级烷基，卤素，羟基，卤代烷基，氰基，硝基，羧基，氨基，烷氧基和芳基或任选被一个或多个选自氢，卤素，卤代烷基，羟基，低级烷基，烷氧基，亚甲基二氧基，亚乙二氧基氰基，硝基，烷硫基，烷基磺酰基，磺酸，磺酰胺，羧基衍生物，氨基，芳基和杂芳基; a为0-4，并且还涉及使用治疗有效剂量的式I化合物治疗由LXR调节的哺乳动物状况的方法。

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