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1. 发明申请

WO2011073845A1 N-LINKED HYDROXAMIC ACID DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译： N-连接的羟基酸衍生物作为抗菌剂有用
公开(公告)号：WO2011073845A1
公开(公告)日：2011-06-23
申请号：PCT/IB2010/055596
申请日：2010-12-06
申请人： PFIZER INC. , BROWN, Matthew Frank , CHE, Ye , MARFAT, Anthony , MELNICK, Michael Joseph , MONTGOMERY, Justin Ian , REILLY, Usa
发明人： BROWN, Matthew Frank , CHE, Ye , MARFAT, Anthony , MELNICK, Michael Joseph , MONTGOMERY, Justin Ian , REILLY, Usa
IPC分类号： A61K31/4412 , A61K31/4418 , A61K31/4427 , A61K31/4439 , A61K31/506 , C07D213/64 , C07D401/04 , C07D401/08 , C07D401/10 , C07D401/12 , C07D407/04 , C07D407/10 , C07D409/04 , C07D413/10 , C07D413/12
CPC分类号： A61K31/4412 , A61K31/4439 , C07D211/86 , C07D213/64 , C07D401/04 , C07D401/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/10 , C07D409/04 , C07D413/10 , C07D413/12 , C07D417/04 , C07D417/10 , C07D417/12 , Y02A50/473
摘要： The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections. Formula (I).
摘要翻译：本发明涉及一类新的异羟肟酸衍生物，它们用作LpxC抑制剂，更具体地说是它们用于治疗细菌感染的用途。式（I）。

2. 发明申请

WO2011045703A2 C-LINKED HYDROXAMIC ACID DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译： C链接的羟基酸衍生物作为抗菌剂有用
公开(公告)号：WO2011045703A2
公开(公告)日：2011-04-21
申请号：PCT/IB2010/054463
申请日：2010-10-04
申请人： PFIZER INC. , BROWN, Matthew Frank , MARFAT, Anthony , MELNICK, Michael Joseph , REILLY, Usa
发明人： BROWN, Matthew Frank , MARFAT, Anthony , MELNICK, Michael Joseph , REILLY, Usa
IPC分类号： C07C317/44
CPC分类号： C07C317/50 , C07C317/44 , C07C317/46 , C07C317/48 , C07C323/65 , C07C2601/02 , C07C2601/08 , C07C2601/16 , C07C2601/18 , C07D213/30 , C07D213/56 , C07D215/06 , C07D231/12 , C07D231/56 , C07D233/36 , C07D239/26 , C07D261/08 , C07D263/08 , C07D263/20 , C07D295/03 , C07D335/02 , C07F9/09 , C07F9/12
摘要： The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
摘要翻译：本发明涉及一类新的异羟肟酸衍生物，它们用作LpxC抑制剂，更具体地说是其用于治疗细菌感染的用途。

3. 发明申请

WO2010032147A2 HYDROXAMIC ACID DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译：用作抗菌剂的羟氨酸衍生物
公开(公告)号：WO2010032147A2
公开(公告)日：2010-03-25
申请号：PCT/IB2009/053809
申请日：2009-09-01
申请人： PFIZER INC. , BROWN, Matthew Frank , DONOVAN, Charles Francis , ELLSWORTH, Edmund Lee , HOYER, Denton Wade , JOHNSON, Timothy Allen , LALL, Manjinder Singh , LIMBERAKIS, Chris , MURPHY, Sean Timothy , SHERRY, Debra Ann , TAYLOR, Clarke Bentley , WARMUS, Joseph Scott
发明人： BROWN, Matthew Frank , DONOVAN, Charles Francis , ELLSWORTH, Edmund Lee , HOYER, Denton Wade , JOHNSON, Timothy Allen , LALL, Manjinder Singh , LIMBERAKIS, Chris , MURPHY, Sean Timothy , SHERRY, Debra Ann , TAYLOR, Clarke Bentley , WARMUS, Joseph Scott
IPC分类号： C07C239/14
CPC分类号： C07C259/06 , C07C2601/04 , C07D207/267 , C07D213/30 , C07D213/38 , C07D213/55 , C07D231/12 , C07D233/64 , C07D237/04 , C07D239/26 , C07D249/04 , C07D249/08 , C07D257/04 , C07D261/08 , C07D261/10 , C07D263/32 , C07D271/06 , C07D277/24 , C07D277/28 , C07D277/30 , C07D285/06 , C07D307/14 , C07D307/42 , C07D307/54 , C07D309/10 , C07D413/04 , C07D413/12 , C07D471/04 , C07F9/653
摘要： The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II); and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B. L 1 -L 4 A, B, R 1 -R 4 and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中：G为式（II）的基团; 及其药学上可接受的盐，前药，水合物或溶剂合物，其中A，B，L，L，L，L，R，R 1， > -R 4和m如本文所定义。本发明还涉及包含式（I）化合物及其在治疗细菌感染中的用途的药物组合物。

4. 发明申请

WO2014128591A1 PYRROLO [2, 3 -D]PYRIMIDINE DERIVATIVES AS INHIBITORS OF JANUS- RELATED KINASES (JAK) 审中-公开
标题翻译：作为JANUS相关动物（JAK）的抑制剂的吡咯并[2,3-D]吡啶衍生物
公开(公告)号：WO2014128591A1
公开(公告)日：2014-08-28
申请号：PCT/IB2014/058889
申请日：2014-02-11
申请人： PFIZER INC.
发明人： BROWN, Matthew Frank , FENWICK, Ashley Edward , FLANAGAN, Mark Edward , GONZALES, Andrea , JOHNSON, Timothy Allan , KAILA, Neelu , MITTON-FRY, Mark J. , STROHBACH, Joseph Walter , TENBRINK, Ruth E. , TRZUPEK, John David , UNWALLA, Rayomand Jal , VAZQUEZ, Michael L.
IPC分类号： C07D487/04 , A61K31/519 , C07D519/00 , A61P37/00
CPC分类号： A61K31/519 , A61K31/5386 , C07D207/18 , C07D487/04 , C07D519/00
摘要： Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them.
摘要翻译：本文描述的是吡咯并[2,3-d]嘧啶衍生物，它们用作Janus Kinase（JAK）抑制剂，以及含有它们的药物组合物。

5. 发明申请

WO2019175828A1 FLUORO-PYRIDINONE PHOSPHATES AND BORONATES USEFUL AS ANTIBACTERIAL AGENTS 审中-公开
公开(公告)号：WO2019175828A1
公开(公告)日：2019-09-19
申请号：PCT/IB2019/052082
申请日：2019-03-14
申请人： PFIZER INC.
发明人： REILLY, Usa , MELNICK, Michael Joseph , BROWN, Matthew Frank , PLUMMER, Mark Stephen , MONTGOMERY, Justin Ian , CHE, Ye , PRICE, Loren Michael , JOHNSON, Timothy Allan , EWIN, Richard Andrew , UCCELLO, Daniel , BRAISH, Tamim Fehme
IPC分类号： C07F9/58 , A61K31/45 , A61K33/22 , C07F5/02 , A61P31/04
摘要： The present invention is directed to a new fluoro-pyridinone hydroxamic acid phosphates and boronates of Formulae (I), (II) and (III) wherein Q is selected from the group consisting of –P(O)(OH) 2 , –P(O)(OH)(O-M + ), –P(O)(O-M+) 2 and –P(O)(O-) 2 M 2+ ; M + at each occurrence is a pharmaceutically acceptable monovalent cation; and M 2+ is a pharmaceutically acceptable divalent cation and their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.

6. 发明申请

WO2017144995A1 PYRAZOLO[1,5-A]PYRAZIN-4-YL DERIVATIVES AS JAK-INHIBITORS 审中-公开
标题翻译：作为JAK抑制剂的吡唑并[1,5-A]吡嗪-4-基衍生物
公开(公告)号：WO2017144995A1
公开(公告)日：2017-08-31
申请号：PCT/IB2017/050748
申请日：2017-02-10
申请人： PFIZER INC.
发明人： BROWN, Matthew Frank , DERMENCI, Alpay , FENSOME, Andrew , GERSTENBERGER, Brian Stephen , HAYWARD, Matthew Merrill , OWEN, Dafydd Rhys , WRIGHT, Stephen Wayne , XING, Li Huang , YANG, Xiaojing
IPC分类号： C07D487/04 , A61K31/4985 , A61P37/02 , A61P29/00 , A61P25/28
CPC分类号： C07D487/04
摘要： A compound compound having the structure (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein A, A' and A" are independently O, C=O, C-R' or N-R", where R' and R" may independently be H, amino, -NR 7 COR 6 , COR 6 , -CONR 7 R 8 , C 1 -C 6 alkyl, or hydroxy(C 1 -C 6 alkyl), and R" may be present or absent, and is present where the rules of valency permit, and where not more than one of A, A' and A" is O or C=0; R 0 and R are independently H, Br, CI, F, or C 1 -C 6 alkyl; R 1 is H, C 1 -C 6 alkyl, or hydroxy(C 1 -C 6 alkyl); R 2 is selected from the group consisting of H, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, hydroxy(C 1 -C 6 alkyl), phenyl(C 1 -C 6 alkyl), formyl, heteroaryl, heterocyclic, -COR 6 , -OCOR 6 , -COOR 6 , -NR 7 COR 6 , -CONR 7 R 8 , and -(CH 2 ) n -W, where W is cyano, hydroxy, C 3 -C 8 cycloalkyl, -SO 2 NR 7 R 8 , and -SO 2 -R 9 , where R 9 is C 1 -C 6 alkyl, C 3 -C 8 cycloalkyl, heteroaryl, or heterocyclic; wherein each of said alkyl, cycloalkyl, heterocyclic, or heteroaryl may be unsubstituted or substituted by halo, cyano, hydroxy, or C 1 -C 6 alkyl; X is C-R 3 or N, where R 3 may be H or C 1 -C 6 alkyl; R 4 and R 5 are independently H, amino, C 1 -C 6 alkyl, or hydroxy(C 1 -C 6 alkyl); R 6 , R 7 and R 8 are each independently H, C 1 -C 6 alkyl, C 1 -C 4 alkoxy(C 1 -C 6 alkyl), or C 3 -C 8 cycloalkyl, said C 1 - C 6 alkyl is optionally substituted by halo, CN or hydroxy; or, R 7 and R 8 together with the atom bonded thereto form a 5- or 6-membered ring, said ring being optionally substituted by halo, hydroxy, CN, or C 1 -C 6 alkyl; and, n is 0, 1, 2 or 3. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations thereof with other therapeutic agents.
摘要翻译：具有结构（I）的化合物或其可药用盐，或所述化合物或其可药用盐的可药用溶剂化物，其中A，A'和A“ 独立地为O，C = O，C-R'或N-R“，其中R'和R” 可以独立地为H，氨基，-NR 7 COR 6，COR 6，-CONR 7 R 9， C 1 -C 6烷基或羟基（C 1 -C 6）烷基或C 1 -C 6烷基，烷基），并且R“ 可以存在或不存在，并且存在于价数规则允许的地方，并且A，A'和A“中不多于一个的地方存在。是O或C = 0; R 0和R独立地为H，Br，Cl，F或C 1 -C 6烷基; R 1是H，C 1 -C 6烷基或羟基（C 1 -C 4）烷基， C 1-6烷基）; R 2选自H，C 1 -C 6烷基，C 1 -C 4烷基，C 1 -C 4烷基， C 1-6烷氧基，羟基（C 1 -C 6烷基），苯基（C 1 -C 6烷基） C 1-6烷基），甲酰基，杂芳基，杂环基，-COR 6，-OCOR 6，-COOR 6，-NR 6 R 6，（COR 6），-CONR 7 R 8和 - （CH 2）其中W为氰基，羟基，C 3 -C 8环烷基，-SO 2 NR 其中R 9，R 8，R 8，R 9，R 9，R 9，R 9，是C 1 -C 6烷基，C 3 -C 8环烷基，杂芳基或杂环基; 其中所述烷基，环烷基，杂环或杂芳基中的每一个可以未被取代或被卤素，氰基，羟基或C 1 -C 6烷基取代; X是C-R 3或N，其中R 3可以是H或C 1 -C 6烷基; R 4和R 5独立地为H，氨基，C 1 -C 6烷基或羟基（C 1 - （C 1 -C 6烷基）; R 6，R 7和R 8各自独立地为H，C 1 -C 6， C 1 -C 4烷氧基（C 1 -C 6烷基）或C（C 1 -C 6）烷基，C 1 -C 4烷氧基（C 1 -C 6烷基）所述C 1 -C 6 - 烷基任选被卤素，CN或羟基取代 ; 或者R 7和R 8与其键合的原子一起形成5-或6-元环，所述环任选被卤素，羟基，CN或 C 1 -C 6烷基; C 1 -C 6烷基; 并且n为0,1,2或3.还提供了作为Janus激酶抑制剂和含有本发明化合物及其与其它治疗剂的组合的药物组合物的治疗方法。

7. 发明申请

WO2019034973A1 PYRAZOLO[1,5-A]PYRAZIN-4-YL AND RELATED DERIVATIVES 审中-公开
公开(公告)号：WO2019034973A1
公开(公告)日：2019-02-21
申请号：PCT/IB2018/056007
申请日：2018-08-09
申请人： PFIZER INC.
发明人： BROWN, Matthew Frank , FENSOME, Andrew , GERSTENBERGER, Brian Stephen , HAYWARD, Matthew Merrill , OWEN, Dafydd Rhys , VAJDOS, Felix , XING, Li Huang
IPC分类号： C07D401/14 , C07D401/04 , C07D471/04 , C07D487/04 , C07D519/00 , A61P29/00 , A61P37/00 , A61K31/4375
摘要： A compound having the structure: (I) or (II) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein variables are defined in the specification. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations thereof with other therapeutic agents.

8. 发明申请

WO2018002760A1 5,7-DIHYDRO-PYRROLO-PYRIDINE DERIVATIVES FOR TREATING NEUROLOGICAL AND NEURODEGENERATIVE DISEASES 审中-公开
标题翻译： 5,7-二氢吡咯 - 吡啶衍生物用于治疗神经和神经退行性疾病
公开(公告)号：WO2018002760A1
公开(公告)日：2018-01-04
申请号：PCT/IB2017/053565
申请日：2017-06-15
申请人： PFIZER INC.
发明人： ZHANG, Lei , BUTLER, Christopher Ryan , BECK, Elizabeth Mary , BRODNEY, Michael Aaron , BROWN, Matthew Frank , MCALLISTER, Laura Ann , LACHAPELLE, Erik Alphie , GILBERT, Adam Matthew
IPC分类号： C07D471/04 , A61K31/437 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/28
摘要： The present invention provides, in part, compounds of Formula (I): or an N -oxide thereof, or a pharmaceutically acceptable salt of the compound or the N - oxide, wherein: R 1 , R 2 , L, A, and E are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N -oxides, or salts, and their uses for treating M4-mediated (or M4- associated) disorders including, e.g., Alzheimer's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.
摘要翻译：本发明部分地提供式（I）的化合物或其N-氧化物，或该化合物或其可药用盐或其可药用盐， N-氧化物，其中：R 1，R 2，L，A和E如本文所述; 制备过程; 用于制备中间体; 和含有这些化合物，N-氧化物或盐的组合物及其用于治疗M4-介导的（或M4-相关的）疾病的用途，所述疾病包括例如阿尔茨海默病，精神分裂症（例如其认知和负面的症状），疼痛，成瘾和睡眠障碍。

9. 发明申请

WO2016178110A1 PYRROLO[2,3-D]PYRIMIDINYL, PYRROLO[2,3-B]PYRAZINYL, PYRROLO[2,3-B]PYRIDINYL ACRYLAMIDES AND EPOXIDES THEREOF 审中-公开
标题翻译：吡咯并[2,3-D]吡啶并[2,3-b]吡嗪并[2,3-b]吡啶-2-基]丙烯酰胺及其环氧化物
公开(公告)号：WO2016178110A1
公开(公告)日：2016-11-10
申请号：PCT/IB2016/052220
申请日：2016-04-19
申请人： PFIZER INC.
发明人： THORARENSEN, Atli , BROWN, Matthew Frank , CASIMIRO-GARCIA, Agustin , CHE, Ye , FLANAGAN, Mark Edward , GILBERT, Adam Matthew , HAYWARD, Matthew Merrill , TELLIEZ, Jean-Baptiste , UNWALLA, Rayomand Jal , TRUJILLO, John I. , LIANG, Sidney Xi
IPC分类号： C07D487/04 , A61K31/395 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3- b]pyrazinyl,and pyrrolo[2,3-b]pyridinyl acrylamides, epoxides,and analogues thereof. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.
摘要翻译：本发明提供药物活性吡咯并[2,3-d]嘧啶基，吡咯并[2,3-b]吡嗪基和吡咯并[2,3-b]吡啶基丙烯酰胺，环氧化物及其类似物。这些化合物可用于抑制Janus Kinase（JAK）。本发明还涉及包含制备这种化合物的方法的组合物，以及用于治疗和预防由JAK介导的病症的方法。

10. 发明申请

WO2018234953A1 DIHYDRO-PYRROLO-PYRIDINE DERIVATIVES 审中-公开
公开(公告)号：WO2018234953A1
公开(公告)日：2018-12-27
申请号：PCT/IB2018/054390
申请日：2018-06-14
申请人： PFIZER INC.
发明人： BECK, Elizabeth Mary , BRODNEY, Michael Aaron , BROWN, Matthew Frank , BUTLER, Christopher Ryan , GILBERT, Adam Matthew , LACHAPELLE, Erik Alphie , MCALLISTER, Laura Ann , UCCELLO, Daniel Paul , ZHANG, Lei
IPC分类号： C07D471/04 , A61K31/437
摘要： The present invention provides, in part, compounds of Formula I, or an N -oxide thereof, or a pharmaceutically acceptable salt of the compound or the N - oxide, wherein: (R 1 )a, (R 2 )b, (R 3 )c, L, A, and E are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N -oxides, or salts, and their uses for treating M4-mediated (or M4- associated) disorders including, e.g., Alzheimer's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.

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