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1. 发明申请

WO2016057762A1 SUBSTITUTED PYRIMIDINES AS INHIBITORS OF HIF PROLYL HYDROXYLASE 审中-公开
公开(公告)号：WO2016057762A1
公开(公告)日：2016-04-14
申请号：PCT/US2015/054643
申请日：2015-10-08
申请人： MERCK SHARP & DOHME CORP , UJJAINWALLA, Fez , TAN, John Qiang , DANG, Qun , SINZ, Christopher J. , CRESPO, Alejandro , WANG, Ming , CHEN, Yili , CAI, Jiaqiang , WU, Fan , DU, Xiaoxing
发明人： UJJAINWALLA, Fez , TAN, John Qiang , DANG, Qun , SINZ, Christopher J. , CRESPO, Alejandro , WANG, Ming , CHEN, Yili , CAI, Jiaqiang , WU, Fan , DU, Xiaoxing
IPC分类号： C07D239/26
CPC分类号： C07D239/36 , C07D239/34 , C07D401/12 , C07D403/12 , C07D405/12
摘要： The present invention concerns compounds of Formula I that inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.

2. 发明申请

WO2016054806A1 SUBSTITTUED PYRIDINE INHIBITORS OF HIF PROLYL HYDROXYLASE 审中-公开
标题翻译： HIF促性腺素的替代吡啶抑制剂
公开(公告)号：WO2016054806A1
公开(公告)日：2016-04-14
申请号：PCT/CN2014/088320
申请日：2014-10-10
申请人： MERCK SHARP & DOHME CORP. , UJJAINWALLA, Fez , TAN, John Qiang , DANG, Qun , SINZ, Christopher J. , WANG, Ming , CHEN, Yili , CAI, Jiaqiang , DU, Xiaoxing
发明人： UJJAINWALLA, Fez , TAN, John Qiang , DANG, Qun , SINZ, Christopher J. , WANG, Ming , CHEN, Yili , CAI, Jiaqiang , DU, Xiaoxing
IPC分类号： C07D213/81 , A61K31/505 , A61K31/506 , A61K31/66 , A61P7/00
CPC分类号： C07D213/82 , A61P7/08 , C07D401/04
摘要： The present invention concerns compounds of formula I that inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
摘要翻译：本发明涉及抑制HIF脯氨酰羟化酶的式I化合物，其用于增强促红细胞生成素的内源性产生的用途，以及用于治疗与减少红细胞生成素的内源性产生如贫血和类似病症相关的病症，以及包含这种化合物和药用载体。

3. 发明申请

WO2012097744A1 MINERALOCORTICOID RECEPTOR ANTAGONISTS 审中-公开
标题翻译：矿物胆碱受体拮抗剂
公开(公告)号：WO2012097744A1
公开(公告)日：2012-07-26
申请号：PCT/CN2012/070597
申请日：2012-01-19
申请人： MERCK SHARP & DOHME CORP. , CRESPO, Alejandro , LAN, Ping , MAL, Rudrajit , OGAWA, Anthony , SHEN, Hong , SINCLAIR, Peter J. , SUN, Zhongxiang , BUNTE, Ellen K. Vande , WU, Zhicai , LIU, Kun , DEVITA, Robert J. , SHEN, Dong-Ming , SHU, Min , TAN, John Qiang , QI, Changhe , WANG, Yuguang , BERESIS, Richard
发明人： CRESPO, Alejandro , LAN, Ping , MAL, Rudrajit , OGAWA, Anthony , SHEN, Hong , SINCLAIR, Peter J. , SUN, Zhongxiang , BUNTE, Ellen K. Vande , WU, Zhicai , LIU, Kun , DEVITA, Robert J. , SHEN, Dong-Ming , SHU, Min , TAN, John Qiang , QI, Changhe , WANG, Yuguang , BERESIS, Richard
IPC分类号： C07D209/08 , C07D209/10 , C07D231/56 , A61K31/404 , A61K31/416 , A61P3/00 , A61P9/04 , A61P9/06 , A61P9/12 , A61P13/12
CPC分类号： C07D413/06 , A61K31/404 , A61K31/4045 , A61K31/405 , A61K31/416 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K45/06 , C07D209/08 , C07D209/10 , C07D231/56 , C07D403/04 , C07D403/06 , C07D405/06
摘要： Disclosed are the compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof, which are useful for treating aldosterone-mediated diseases. The processes for preparing compounds of the Formula (I), the use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and the pharmaceutical compositions which comprise compounds of the formula (I) are disclosed too.
摘要翻译：公开了式（I）化合物及其药学上可接受的盐，其可用于治疗醛固酮介导的疾病。还公开了制备式（I）化合物，用于治疗和预防上述疾病和用于制备用于此目的的药物的方法和包含式（I）化合物的药物组合物。

4. 发明申请

WO2014120346A1 FACTOR IXA INHIBITORS 审中-公开
标题翻译：因子IXA抑制剂
公开(公告)号：WO2014120346A1
公开(公告)日：2014-08-07
申请号：PCT/US2013/075233
申请日：2013-12-16
申请人： MERCK SHARP & DOHME CORP. , MOCHIDA PHARMACEUTICAL CO., LTD. , SMITH, Cameron, James , TAN, John, Qiang , ZHANG, Ting , BALKOVEC, James , GREENLEE, William, John , GUO, Liangqin , XU, Jiayi , CHEN, Yi-heng , CHEN, Yili , CHACKALAMANNIL, Samuel , HIRABAYASHI, Tomokazu , NAGASUE, Hiroshi , OGAWA, Kouki
发明人： SMITH, Cameron, James , TAN, John, Qiang , ZHANG, Ting , BALKOVEC, James , GREENLEE, William, John , GUO, Liangqin , XU, Jiayi , CHEN, Yi-heng , CHEN, Yili , CHACKALAMANNIL, Samuel , HIRABAYASHI, Tomokazu , NAGASUE, Hiroshi , OGAWA, Kouki
IPC分类号： A61K31/5377 , C07D413/12
CPC分类号： C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04
摘要： The present invention provides a compound of Formula (I) (structurally represented) wherein R1 is H or C1-6 alkyl, R2 is H or C1-6 alkyl or CH20H, R3 is H or C1-6 alkyl, and R4 is H or C1-6 alkyl, provided that when R1, R2, and R3 are H, R4 is C1-6 alkyl, and when R1, R2, and R4 are H, then R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl or-CH20H, and when R2, R3, and R4 are H, then R1 is C 1-6 alkyl; A is 1 ) a 9-10 membered bicyclic heterocycle having 1-3 heteroatoms independently selected from N, S and 0, which 9-10 membered bicyclic heterocycle is unsubstituted or substituted with R5 and unsubstituted or substituted with R6 and unsubstituted or substituted with NH2, or 2) a 6-9 membered monocyclic or bicyclic carbocyclic ring system unsubstituted or substituted with R5, unsubstituted or substituted with R6, and unsubstituted or substituted with -CH2NH2; and B is 1) a 5- or 6-membered monocyclic heterocycle having 1 or 2 heteroatoms independently selected from N, S or 0, which is unsubstituted or substituted on a carbon or nitrogen atom with R7, unsubstituted or substituted on a carbon or nitrogen atom with R8, and unsubstituted or substituted on a carbon or nitrogen atom with R9, or 2) an 8- or 9-membered fused bicyclic heterocycle having 1, 2 or 3 nitrogen atoms which is unsubstituted or substituted on a carbon or nitrogen atom with R7, and unsubstituted or substituted on a carbon or nitrogen atom with R8; and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses.
摘要翻译：本发明提供式（I）（结构上表示）的化合物，其中R 1是H或C 1-6烷基，R 2是H或C 1-6烷基或CH 2 OH，R 3是H或C 1-6烷基，R 4是H或 C 1 -C 6烷基，条件是当R 1，R 2和R 3为H时，R 4为C 1-6烷基，并且当R 1，R 2和R 4为H时，R 3为C 1-6烷基，并且当R 1，R 3和 R 4是H，R 2是C 1-6烷基或-CH 2 OH，当R 2，R 3和R 4是H时，R 1是C 1-6烷基; A是1）具有1-3个独立地选自N，S和0的杂原子的9-10元双环杂环，其中9-10元双环杂环是未取代的或被R5取代，未被取代或被R6取代，未被取代或被NH 2取代，或2）未被取代或被未取代或被R 6取代的R 5取代的未取代或被-CH 2 NH 2取代的6-9元单环或双环碳环系统; 和B为1）具有1或2个独立地选自N，S或0的杂原子的5或6元单环杂环，其未被取代或在碳或氮原子上被取代或未取代或在碳或氮上取代的R7取代具有R 8的未取代或取代的碳原子或氮原子上的取代基，或2）具有1,2或3个氮原子的8或9元稠合双环杂环，其未被取代或在碳原子或氮原子上被取代， R7，并且在碳或氮原子上未被取代或取代为R8; 和包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓形成的方法。

5. 发明申请

WO2014099695A1 FACTOR IXA INHIBITORS 审中-公开
标题翻译：因子IXA抑制剂
公开(公告)号：WO2014099695A1
公开(公告)日：2014-06-26
申请号：PCT/US2013/075232
申请日：2013-12-16
申请人： MERCK SHARP & DOHME CORP. , MOCHIDA PHARMACEUTICAL CO., LTD. , SMITH, Cameron, James , TAN, John, Qiang , ZHANG, Ting , BALKOVEC, James , GREENLEE, William, John , GUO, Liangqin , CHEN, Yi-Heng , CHEN, Yili , CHACKALAMANNIL, Samuel , HIRABAYASHI, Tomokazu , KATSUNO, Mika
发明人： SMITH, Cameron, James , TAN, John, Qiang , ZHANG, Ting , BALKOVEC, James , GREENLEE, William, John , GUO, Liangqin , CHEN, Yi-Heng , CHEN, Yili , CHACKALAMANNIL, Samuel , HIRABAYASHI, Tomokazu , KATSUNO, Mika
IPC分类号： A61K31/5377 , C07D413/12
CPC分类号： C07D413/14 , C07D413/12 , C07D513/04
摘要： The present invention provides a compound of Formula (I) (structurally represented) wherein R1, R2, R3 and R4 are independently H or C1-6 alkyl, provided that when R1, R2, and R3 are H, R4 is C1-6 alkyl, and when R1, R2, and R4 are H, R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl, and when R2, R3, and R4 are H, R1 is C1-6 alkyl; and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes.
摘要翻译：本发明提供式（I）化合物（结构表示），其中R 1，R 2，R 3和R 4独立地为H或C 1-6烷基，条件是当R 1，R 2和R 3为H时，R 4为C 1-6烷基当R 1，R 2和R 4为H时，R 3为C 1-6烷基，当R 1，R 3和R 4为H时，R 2为C 1-6烷基，当R 2，R 3和R 4为H时，R 1为 C 1-6烷基; 以及包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓形成，栓塞，高凝状态或纤维化改变的方法。

6. 发明申请

WO2016054805A1 SUBSTITUTED PYRIMIDINES AS INHIBITORS OF HIF PROLYL HYDROXYLASE 审中-公开
公开(公告)号：WO2016054805A1
公开(公告)日：2016-04-14
申请号：PCT/CN2014/088319
申请日：2014-10-10
申请人： MERCK SHARP & DOHME CORP. , UJJAINWALLA, Fez , TAN, John Qiang , DANG, Qun , SINZ, Christopher J. , WANG, Ming , CHEN, Yili , CAI, Jiaqiang
发明人： UJJAINWALLA, Fez , TAN, John Qiang , DANG, Qun , SINZ, Christopher J. , WANG, Ming , CHEN, Yili , CAI, Jiaqiang
IPC分类号： C07D239/36 , C07D411/06 , A61K31/505 , A61K31/506 , A61P7/00
CPC分类号： C07D239/36 , A61P7/06 , C07D413/06
摘要： The present invention concerns compounds of Formula I that inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.

7. 发明申请

WO2016054804A1 SUBSTITUTED PYRIMIDINES AS INHIBITORS OF HIF PROLYL HYDROXYLASE 审中-公开
标题翻译：作为HIF PROLYL羟基酶抑制剂的替代吡咯烷
公开(公告)号：WO2016054804A1
公开(公告)日：2016-04-14
申请号：PCT/CN2014/088318
申请日：2014-10-10
申请人： MERCK SHARP & DOHME CORP. , UJJAINWALLA, Fez , TAN, John Qiang , DANG, Qun , SINZ, Christopher J. , CRESPO, Alejandro , WANG, Ming , CHEN, Yili , CAI, Jiaqiang , WU, Fan , DU, Xiaoxing
发明人： UJJAINWALLA, Fez , TAN, John Qiang , DANG, Qun , SINZ, Christopher J. , CRESPO, Alejandro , WANG, Ming , CHEN, Yili , CAI, Jiaqiang , WU, Fan , DU, Xiaoxing
IPC分类号： C07D239/36 , C07D401/04 , C07D403/04 , C07D417/04 , A61K31/505 , A61K31/506 , A61K31/66 , A61P7/00
CPC分类号： C07D239/36 , C07D239/34 , C07D401/12 , C07D403/12 , C07D405/12
摘要： The present invention concerns compounds of Formula I that inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
摘要翻译：本发明涉及抑制HIF脯氨酰羟化酶的式I化合物，其用于促进促红细胞生成素的内源性产生的用途，以及用于治疗与减少红细胞生成素的内源产生如贫血和类似病症相关的病症，以及包含这种化合物和药用载体。

8. 发明申请

WO2014014794A2 MINERALOCORTICOID RECEPTOR ANTAGONISTS 审中-公开
标题翻译：矿物胆碱受体拮抗剂
公开(公告)号：WO2014014794A2
公开(公告)日：2014-01-23
申请号：PCT/US2013/050427
申请日：2013-07-15
申请人： MERCK SHARP & DOHME CORP. , CERNAK, Timothy, A. , DYKSTRA, Kevin, D. , SHEN, Dong-Ming , LIU, Kun , STAMFORD, Andrew , TAN, John Qiang
发明人： CERNAK, Timothy, A. , DYKSTRA, Kevin, D. , SHEN, Dong-Ming , LIU, Kun , STAMFORD, Andrew , TAN, John Qiang
IPC分类号： A61K31/416
CPC分类号： A61K31/416 , A61K45/06 , C07D231/56 , A61K2300/00
摘要： The present invention is directed to compounds of the Formula I: as well as pharmaceutically acceptable salts thereof, that may be useful for treating aldosterone-mediated diseases. The invention furthermore relates to specific diastereomers and enantiomers of the compounds, to processes for preparing compounds of the Formula I, to their potential use for the therapy and prophylaxis of the above-mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula I.
摘要翻译：本发明涉及可用于治疗醛固酮介导的疾病的式I化合物及其药学上可接受的盐。本发明还涉及该化合物的具体非对映异构体和对映异构体，制备式I化合物的方法，以及其用于治疗和预防上述疾病和用于制备用于此目的的药物的潜在用途，以及药物组合物其包含式I的化合物。

9. 发明申请

WO2016057753A1 SUBSTITUTED PYRIMIDINES AS INHIBITORS OF HIF PROLYL HYDROXYLASE 审中-公开
标题翻译：作为HIF-PRLYL羟化酶抑制剂的取代的嘧啶
公开(公告)号：WO2016057753A1
公开(公告)日：2016-04-14
申请号：PCT/US2015/054626
申请日：2015-10-08
申请人： MERCK SHARP & DOHME CORP , UJJAINWALLA, Fez , TAN, John Qiang , DANG, Qun , SINZ, Christopher J. , WANG, Ming , CHEN, Yili , CAI, Jiaqiang
发明人： UJJAINWALLA, Fez , TAN, John Qiang , DANG, Qun , SINZ, Christopher J. , WANG, Ming , CHEN, Yili , CAI, Jiaqiang
IPC分类号： C07D471/20 , C07D401/14 , C07D471/04
CPC分类号： C07D239/36 , A61P7/06 , C07D413/06
摘要： The present invention concerns compounds of Formula I that inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
摘要翻译：本发明涉及抑制HIF脯氨酰羟化酶的式I化合物，它们用于增强促红细胞生成素的内源产生的用途，以及用于治疗与促红细胞生成素的内源性产生减少有关的疾病如贫血等疾病，以及包含这种化合物和药物载体的药物组合物。

10. 发明申请

WO2016057743A1 SUBSTITUTED PYRIDINE INHIBITORS OF HIF PROLYL HYDROXYLASE 审中-公开
标题翻译：取代的吡啶类抑制剂HIF PROLYL HYDROXYLASE
公开(公告)号：WO2016057743A1
公开(公告)日：2016-04-14
申请号：PCT/US2015/054605
申请日：2015-10-08
申请人： MERCK SHARP & DOHME CORP , UJJAINWALLA, Fez , TAN, John Qiang , DANG, Qun , SINZ, Christopher J. , WANG, Ming , CAI, Jiaqiang , DU, Xiaoxing , CHEN, Yili
发明人： UJJAINWALLA, Fez , TAN, John Qiang , DANG, Qun , SINZ, Christopher J. , WANG, Ming , CAI, Jiaqiang , DU, Xiaoxing , CHEN, Yili
IPC分类号： C07D471/20 , C07D401/14 , C07D471/04
CPC分类号： C07D213/82 , A61P7/08 , C07D401/04
摘要： The present invention concerns compounds of formula I that inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
摘要翻译：本发明涉及抑制HIF脯氨酰羟化酶的式I化合物，其用于增强促红细胞生成素的内源性产生的用途，以及用于治疗与减少红细胞生成素的内源性产生如贫血和类似病症相关的病症，以及包含这种化合物和药用载体。

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