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1. 发明申请

WO2016027195A1 AMINOPYRIMIDINYL COMPOUNDS AS JAK INHIBITORS 审中-公开
标题翻译：氨基酰亚胺化合物作为JAK抑制剂
公开(公告)号：WO2016027195A1
公开(公告)日：2016-02-25
申请号：PCT/IB2015/056021
申请日：2015-08-07
申请人： PFIZER INC.
发明人： FENSOME, Andrew , GOPALSAMY, Ariamala , GERSTENBERGER, Brian S. , EFREMOV, Ivan Viktorovich , WAN, Zhao-Kui , PIERCE, Betsy , TELLIEZ, Jean-Baptiste , TRUJILLO, John I , ZHANG, Liying , XING, Li
IPC分类号： C07D401/14 , C07D405/14 , C07D403/14 , C07D487/08 , C07D519/00 , A61K31/506 , A61P35/00 , A61P37/00
CPC分类号： A61K31/55 , A61K31/506 , A61K45/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D487/08 , C07D519/00
摘要： A compound compound having the structure or a pharmaceutic acceptable salt thereof: Formula (I). Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations with other therapeutic agents.
摘要翻译：具有结构或其药学上可接受的盐的化合物：式（I）。还提供了作为Janus Kinase抑制剂和含有本发明化合物的药物组合物和与其它治疗剂的组合的治疗方法。

2. 发明申请

WO2019175776A1 CYCLOPENTANE-BASED MODULATORS OF STING (STIMULATOR OF INTERFERON GENES) 审中-公开
公开(公告)号：WO2019175776A1
公开(公告)日：2019-09-19
申请号：PCT/IB2019/052009
申请日：2019-03-12
申请人： PFIZER INC.
发明人： WYTHES, Martin James , MCALPINE, Indrawan James , PATMAN, Ryan , RUI, Eugene Yuanjin , FENSOME, Andrew , MADERNA, Andreas , JALAIE, Mehran , GAJIWALA, Ketan S.
IPC分类号： C07H19/213 , A61P35/00
摘要： Compounds of the general formula (I), or a pharmaceutically acceptable salt thereof, processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.

3. 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.

4. 发明申请

WO2022112919A1 (AZA)BENZOTHIAZOLYL SUBSTITUTED PYRAZOLE COMPOUNDS 审中-公开
公开(公告)号：WO2022112919A1
公开(公告)日：2022-06-02
申请号：PCT/IB2021/060806
申请日：2021-11-22
申请人： PFIZER INC.
发明人： CABRAL, Shawn , CANTERBURY, Daniel Paul , DOW, Robert Lee , FENSOME, Andrew , KORCZYNSKA, Magdalena , LAVERGNE, Sophie Yvette , LONDREGAN, Allyn Timothy , MASCITTI, Vincent , PIOTROWSKI, David Walter , SHAVNYA, Andre , TU, Meihua Mike , WANG, Tao , WISNIEWSKA, Hanna Maria
IPC分类号： C07D417/04 , A61P25/00 , A61K31/428
摘要： This application includes a compound of Formula I or a pharmaceutically acceptable salt thereof; wherein the variables R1a, R1b, R2, R3, X, Y and Z are as defined herein, pharmaceutical compositions comprising the compounds of Formula I and methods of treatment comprising administering to a patient in need thereof a compound of Formula I for the treatment of transthyretin amyloidosis and diseases related thereto.

5. 发明申请

WO2021059136A1 POLYHETEROCYCLIC MODULATORS OF STING (STIMULATOR OF INTERFERON GENES) 审中-公开
公开(公告)号：WO2021059136A1
公开(公告)日：2021-04-01
申请号：PCT/IB2020/058854
申请日：2020-09-22
申请人： PFIZER INC.
发明人： FENSOME, Andrew , FISHER, Ethan Lawrence , GAJIWALA, Ketan S. , HUH, Chan Woo , JALAIE, Mehran , MCALPINE, Indrawan James , PATMAN, Ryan , RUI, Eugene Yuanjin , TRAN, Tuan Phong , WYTHES, Martin James , ZHANG, Lei , ZHOU, Dahui
IPC分类号： C07D403/14 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D451/02 , C07D455/02 , C07D471/04 , C07D487/04 , C07D491/107 , C07D498/04 , C07D498/08 , A61K31/4196 , A61P35/00
摘要： Compounds of the general formula (I), or a pharmaceutically acceptable salt thereof, processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.

6. 发明申请

WO2021009676A1 IMIDAZO[4,5-C]PYRIDINE DERIVATIVES AS TOLL-LIKE RECEPTOR AGONISTS 审中-公开
公开(公告)号：WO2021009676A1
公开(公告)日：2021-01-21
申请号：PCT/IB2020/056605
申请日：2020-07-14
申请人： PFIZER INC.
发明人： AHMAD, Omar , FENSOME, Andrew , FISHER, Ethan Lawrence , LACHAPELLE, Erik Alphie , UNWALLA, Rayomand J , XIAO, Jun , ZHANG, Lei
IPC分类号： C07D471/04 , A61P35/00 , A61K31/437
摘要： The present invention relates to imidazo-pyridinyl compounds, or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer, in a subject.

7. 发明申请

WO2021048736A1 TREATMENT OF HIDRADENITIS WITH JAK INHIBITORS 审中-公开
公开(公告)号：WO2021048736A1
公开(公告)日：2021-03-18
申请号：PCT/IB2020/058333
申请日：2020-09-08
申请人： PFIZER INC.
发明人： FENSOME, Andrew , GERSTENBERGER, Brian Stephen , OWEN, Dafydd Rhys
IPC分类号： A61K31/4985 , A61K31/506 , A61K31/519 , A61P17/00
摘要： Methods for treating hidradenitis suppurtiva using compounds and analogues which inhibit certain kinases including Janus Kinase (JAK).

8. 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。

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