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1. 发明申请

WO2015021358A2 COMPOUNDS AND METHODS FOR INHIBITING PHOSPHATE TRANSPORT 审中-公开
标题翻译：抑制磷酸盐运输的化合物和方法
公开(公告)号：WO2015021358A2
公开(公告)日：2015-02-12
申请号：PCT/US2014/050290
申请日：2014-08-08
申请人： CHARMOT, Dominique , LEWIS, Jason G. , JACOBS, Jeffrey W. , LANGSETMO, Ingrid , CARRERAS, Christopher
发明人： CHARMOT, Dominique , LEWIS, Jason G. , JACOBS, Jeffrey W. , LANGSETMO, Ingrid , CARRERAS, Christopher
IPC分类号： A61K38/10
CPC分类号： A61K38/10 , A61K31/00 , A61K31/195 , A61K31/27 , A61K31/352 , A61K31/353 , A61K31/382 , A61K31/4045 , A61K31/421 , A61K31/4418 , A61K31/4439 , A61K31/4525 , A61K31/475 , A61K31/506 , A61K31/7072 , A61K33/26 , A61K38/16 , A61K45/06 , G01N33/5038 , G01N33/5044 , G01N33/84 , A61K2300/00
摘要： Provided are non-NHE3-binding agents having activity as phosphate transport/uptake inhibitors in the gastrointestinal tract, including in the small intestine, methods for their use as therapeutic or prophylactic agents, and related methods of drug discovery.
摘要翻译：提供了在胃肠道中包括小肠中的作为磷酸盐转运/摄取抑制剂的活性的非NHE3结合剂，其用作治疗剂或预防剂的方法以及药物的相关方法发现。

2. 发明申请

WO2012006474A2 COMPOUNDS AND METHODS FOR INHIBITING PHOSPHATE TRANSPORT 审中-公开
标题翻译：用于抑制磷酸盐运输的化合物和方法
公开(公告)号：WO2012006474A2
公开(公告)日：2012-01-12
申请号：PCT/US2011/043262
申请日：2011-07-07
申请人： ARDELYX, INC. , LEWIS, Jason, G. , JACOBS, Jeffrey, W. , REICH, Nicholas , LEADBETTER, Michael, R. , BELL, Noah , CHANG, Han-Ting , CHEN, Tao , NAVRE, Marc , CHARMOT, Dominique , CARRERAS, Christopher , LABONTE, Eric
发明人： LEWIS, Jason, G. , JACOBS, Jeffrey, W. , REICH, Nicholas , LEADBETTER, Michael, R. , BELL, Noah , CHANG, Han-Ting , CHEN, Tao , NAVRE, Marc , CHARMOT, Dominique , CARRERAS, Christopher , LABONTE, Eric
IPC分类号： C07D403/02
CPC分类号： A61K31/5377 , A61K31/497 , A61K31/506 , A61K31/59 , A61K45/06 , C07D239/42 , C07D241/20
摘要： Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
摘要翻译：具有作为磷酸盐转运抑制剂的活性的化合物，更具体地，公开了肠顶膜Na /磷酸盐共转运的抑制剂。该化合物具有以下结构（I）：包括立体异构体，其药学上可接受的盐和前药，其中X，Y和A如本文所定义。还公开了与这种化合物的制备和使用相关的方法以及包含这些化合物的药物组合物。

3. 发明申请

WO2012006475A1 COMPOUNDS AND METHODS FOR INHIBITING PHOSPHATE TRANSPORT 审中-公开
标题翻译：抑制磷酸盐运输的化合物和方法
公开(公告)号：WO2012006475A1
公开(公告)日：2012-01-12
申请号：PCT/US2011/043263
申请日：2011-07-07
申请人： ARDELYX, INC. , LEWIS, Jason, G. , JACOBS, Jeffrey, W. , REICH, Nicholas , LEADBETTER, Michael, R. , BELL, Noah , CHANG, Han-Ting , CHEN, Tao , NAVRE, Marc , CHARMOT, Dominique , CARRERAS, Christopher , LABONTE, Eric , DU, Xunxiang , OSLOB, Johan
发明人： LEWIS, Jason, G. , JACOBS, Jeffrey, W. , REICH, Nicholas , LEADBETTER, Michael, R. , BELL, Noah , CHANG, Han-Ting , CHEN, Tao , NAVRE, Marc , CHARMOT, Dominique , CARRERAS, Christopher , LABONTE, Eric , DU, Xunxiang , OSLOB, Johan
IPC分类号： G01N33/48 , G01N31/00 , G01G23/01 , G06G7/58
CPC分类号： A61K33/24 , A61K31/19 , A61K31/415 , A61K31/4192 , A61K31/4418 , A61K31/4433 , A61K31/4439 , A61K31/4453 , A61K31/454 , A61K31/4545 , A61K31/465 , A61K31/496 , A61K31/505 , A61K31/506 , A61K31/522 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/706 , A61K31/785 , A61K33/10 , A61K45/06 , C07D213/81 , C07D295/155 , C07D401/12 , C07D405/12 , C07D417/12
摘要： Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
摘要翻译：具有作为磷酸盐转运抑制剂的活性的化合物，更具体地，公开了肠顶膜Na /磷酸盐共转运的抑制剂。还公开了与这种化合物的制备和使用相关的方法以及包含这些化合物的药物组合物。

4. 发明申请

WO2012006477A1 COMPOUNDS AND METHODS FOR INHIBITING PHOSPHATE TRANSPORT 审中-公开
标题翻译：抑制磷酸盐运输的化合物和方法
公开(公告)号：WO2012006477A1
公开(公告)日：2012-01-12
申请号：PCT/US2011/043266
申请日：2011-07-07
申请人： ARDELYX, INC. , LEWIS, Jason, G. , JACOBS, Jeffrey, W. , REICH, Nicholas , LEADBETTER, Michael, R. , BELL, Noah , CHANG, Han-Ting , CHEN, Tao , NAVRE, Marc , CHARMOT, Dominique , CARRERAS, Christopher , LABONTE, Eric
发明人： LEWIS, Jason, G. , JACOBS, Jeffrey, W. , REICH, Nicholas , LEADBETTER, Michael, R. , BELL, Noah , CHANG, Han-Ting , CHEN, Tao , NAVRE, Marc , CHARMOT, Dominique , CARRERAS, Christopher , LABONTE, Eric
IPC分类号： A01N43/38 , A61K31/405
CPC分类号： A61K31/5377 , A61K31/454 , A61K31/59 , A61K45/06 , C07D209/12 , C07D209/14
摘要： Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y, R 1 and R 2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
摘要翻译：具有作为磷酸盐转运抑制剂的活性的化合物，更具体地，公开了肠顶膜Na /磷酸盐共转运的抑制剂。所述化合物具有以下结构（I）：包括立体异构体，其药学上可接受的盐和前药，其中X，Y，R 1和R 2如本文所定义。还公开了与这种化合物的制备和使用相关的方法以及包含这些化合物的药物组合物。

5. 发明申请

WO2012054110A3 COMPOUNDS AND METHODS FOR INHIBITING PHOSPHATE TRANSPORT 审中-公开
公开(公告)号：WO2012054110A3
公开(公告)日：2012-04-26
申请号：PCT/US2011/043267
申请日：2011-07-07
申请人： ARDELYX, INC. , LEWIS, Jason, G. , JACOBS, Jeffrey, W. , REICH, Nicholas , LEADBETTER, Michael, R. , BELL, Noah , CHANG, Han-Ting , CHEN, Tao , NAVRE, Marc , CHARMOT, Dominique , CARRERAS, Christopher , LABONTE, Eric
发明人： LEWIS, Jason, G. , JACOBS, Jeffrey, W. , REICH, Nicholas , LEADBETTER, Michael, R. , BELL, Noah , CHANG, Han-Ting , CHEN, Tao , NAVRE, Marc , CHARMOT, Dominique , CARRERAS, Christopher , LABONTE, Eric
IPC分类号： A61K31/165
摘要： Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): (I) including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y, A, R 1 and R 2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

6. 发明申请

WO2012006473A1 COMPOUNDS AND METHODS FOR INHIBITING PHOSPHATE TRANSPORT 审中-公开
标题翻译：抑制磷酸盐运输的化合物和方法
公开(公告)号：WO2012006473A1
公开(公告)日：2012-01-12
申请号：PCT/US2011/043261
申请日：2011-07-07
申请人： ARDELYX, INC. , LEWIS, Jason, G. , JACOBS, Jeffrey, W. , REICH, Nicholas , LEADBETTER, Michael, R. , BELL, Noah , CHANG, Han-Ting , CHEN, Tao , NAVRE, Marc , CHARMOT, Dominique , CARRERAS, Christopher , LABONTE, Eric
发明人： LEWIS, Jason, G. , JACOBS, Jeffrey, W. , REICH, Nicholas , LEADBETTER, Michael, R. , BELL, Noah , CHANG, Han-Ting , CHEN, Tao , NAVRE, Marc , CHARMOT, Dominique , CARRERAS, Christopher , LABONTE, Eric
IPC分类号： A61K31/506 , A61K31/4965 , C07D401/00 , C07D403/00 , C07D211/68 , C07D413/00
CPC分类号： A61K31/5377 , A61K31/415 , A61K31/454 , A61K31/4545 , A61K31/4965 , A61K31/505 , A61K31/59 , A61K45/06 , C07D211/68 , C07D231/40 , C07D233/88 , C07D249/14 , C07D255/02 , C07D277/46 , C07D285/135 , C07D401/12 , A61K2300/00
摘要： Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
摘要翻译：公开了具有作为磷酸盐转运抑制剂的活性的化合物，更具体地说，具有肠顶膜Na /磷酸盐共转运的抑制剂。所述化合物具有以下结构（I）：包括其立体异构体，药学上可接受的盐和前药，其中X，Y和A如本文所定义。还公开了与这些化合物的制备和使用有关的方法，以及包含这些化合物的药物组合物。

7. 发明申请

WO2005060693A2 9-DESOXOERYTHROMYCIN COMPOUNDS AS PROKINETIC AGENTS 审中-公开
标题翻译：作为促运动剂的9-去氧肿瘤毒素化合物
公开(公告)号：WO2005060693A2
公开(公告)日：2005-07-07
申请号：PCT/US2004/042767
申请日：2004-12-17
申请人： KOSAN BIOSCIENCES, INC. , LIU, Yaoquan , CARRERAS, Christopher , MYLES, David, C.
发明人： LIU, Yaoquan , CARRERAS, Christopher , MYLES, David, C.
IPC分类号： A61K31/7048 , C07H17/08
CPC分类号： C07H17/08
摘要： 9-Desoxoerythromycin compounds of formula (I); wherein R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein, are useful as prokinetic agents for treating disorders of gastric motility.
摘要翻译：式（I）的9-去氧红霉素化合物; 其中R 1，R 2，R 3，R 4和R 5独立地为氢，如本文所定义，可用作促胃肠动力剂用于治疗胃运动障碍。

8. 发明申请

WO2002064092A2 METHOD FOR EVALUATING THERAPEUTIC EFFICACY 审中-公开
标题翻译：评估治疗效果的方法
公开(公告)号：WO2002064092A2
公开(公告)日：2002-08-22
申请号：PCT/US2002/004462
申请日：2002-02-15
申请人： KOSAN BIOSCIENCES, INC. , CARRERAS, Christopher , DILLON, Susan
发明人： CARRERAS, Christopher , DILLON, Susan
IPC分类号： A61K
CPC分类号： G01N33/5041 , C07H21/04 , C07K14/723 , G01N33/5008 , G01N33/566 , G01N33/74 , G01N2333/72 , G01N2333/726 , G01N2500/00
摘要： The present invention relates to in vitro methods for evaluating compounds that better correlate with therapeutic efficiency than evaluating compounds based on potency alone. In general, the inventive methods comprises: (i) determining a potency value for a compound against its target receptor; (ii) determining a potency value for a compound against its target receptor; and (iii) comparing the potency value wit the desensitization value. If the desired action of a compound is as a receptor agonist, the compound's desensitization value should be larger than the compound's potency value. This ensures that the concentration of a compound required for potency will not also cause the receptor to desensitize at the same time, thus in an essence nullifying the desired effect. The inventive methods are used to evaluate novel motilide compounds as well as ABT-229 and EM-574, two motilide compounds for which clinical trials have been initiated.
摘要翻译：本发明涉及用于评价与治疗效能更好相关的化合物的体外方法，而不仅仅是基于单独的效力来评价化合物。通常，本发明的方法包括：（i）确定化合物对其靶受体的效价值; （ii）确定化合物对其靶受体的效价值; 和（iii）比较具有脱敏值的效价值。如果化合物的所需作用是作为受体激动剂，化合物的脱敏值应大于化合物的效价值。这确保了效力所需的化合物的浓度不会同时导致受体脱敏，因此在本质上无效期望的效果。本发明的方法用于评价新型的动物酰胆碱化合物以及ABT-229和EM-574，这两种化合物已经开始临床试验。

9. 发明申请

WO2006127252A1 MOTILIDE COMPOUNDS 审中-公开
标题翻译：胶体化合物
公开(公告)号：WO2006127252A1
公开(公告)日：2006-11-30
申请号：PCT/US2006/017672
申请日：2006-05-08
申请人： KOSAN BIOSCIENCES INCORPORATED , LIU, Yaoquan , CARRERAS, Christopher , MYLES, David, C. , LI, Yong , SHAW, Simon, James , FU, Hong , CHEN, Yue , ZHENG, Hao , LI, Yandong , BURLINGAME, Mark, A.
发明人： LIU, Yaoquan , CARRERAS, Christopher , MYLES, David, C. , LI, Yong , SHAW, Simon, James , FU, Hong , CHEN, Yue , ZHENG, Hao , LI, Yandong , BURLINGAME, Mark, A.
IPC分类号： A61K31/70 , C07H17/08
CPC分类号： C07H17/08
摘要： Compounds having a structure according to formula (I) where R A , R B , R C , R D , R E , and R F are as defined herein, are useful as prokinetic agents.
摘要翻译：具有式（I）结构的化合物其中R A，R B，R C，R D，D， R E和R F如本文所定义，可用作促动力剂。

10. 发明申请

WO2005018576A3 N-DESMETHYL-N-SUBSTITUTED-11-DEOXYERYTHROMYCIN COMPOUNDS TECHNICAL FIELD OF THE INVENTION 审中-公开
公开(公告)号：WO2005018576A3
公开(公告)日：2005-03-03
申请号：PCT/US2004/027854
申请日：2004-08-25
申请人： KOSAN BIOSCIENCES, INC. , CARRERAS, Christopher , LIU, Yaoquan
发明人： CARRERAS, Christopher , LIU, Yaoquan
IPC分类号： C07H17/08
摘要： Compounds having the structure of formula I: wherein R 1 ,R 2 ,R 3 , R 4 , R 5 , and R 6 are as defined herein, are prokinetic agents and can be used to treat disorders of gastric motility.

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