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1. 发明申请

WO2010146488A1 BICYCLIC AND TRICYCLIC COMPOUNDS AS KAT II INHIBITORS 审中-公开
标题翻译：双相和三聚体化合物作为KAT II抑制剂
公开(公告)号：WO2010146488A1
公开(公告)日：2010-12-23
申请号：PCT/IB2010/052349
申请日：2010-05-26
申请人： PFIZER INC. , CLAFFEY, Michelle Marie , DOUNAY, Amy Beth , GAN, Xinmin , HAYWARD, Matthew Merrill , RONG, Suobao , TUTTLE, Jamison Bryce , VERHOEST, Patrick Robert
发明人： CLAFFEY, Michelle Marie , DOUNAY, Amy Beth , GAN, Xinmin , HAYWARD, Matthew Merrill , RONG, Suobao , TUTTLE, Jamison Bryce , VERHOEST, Patrick Robert
IPC分类号： C07D215/60 , C07D401/04 , C07D401/12 , C07D405/04 , C07D471/04 , C07D491/04 , A61K31/4375 , A61K31/4704 , A61P25/00
CPC分类号： C07D215/60 , C07D401/04 , C07D401/12 , C07D405/04 , C07D471/04 , C07D491/04
摘要： Compounds of Formula X: wherein A, X, Y, Z, R 5 , R 6a , and R 6b are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other neurodegenerative and/or neurological disorders in mammals, including humans.
摘要翻译：式X的化合物：其中A，X，Y，Z，R 5，R 6a和R 6b如本文所定义，及其药学上可接受的盐被描述为可用于治疗与精神分裂症和其它神经变性和/或其它神经变性相关的认知缺陷包括人在内的哺乳动物的神经障碍。

2. 发明申请

WO2016020786A1 IMIDAZOPYRIDAZINE COMPOUNDS 审中-公开
标题翻译：咪唑吡嗪化合物
公开(公告)号：WO2016020786A1
公开(公告)日：2016-02-11
申请号：PCT/IB2015/055597
申请日：2015-07-23
申请人： PFIZER INC.
发明人： CHAPPIE, Thomas Allen , HAYWARD, Matthew Merrill , HELAL, Christopher John , LACHAPELLE, Erik Alphie , PATEL, Nandini Chaturbhai , SCIABOLA, Simone , VERHOEST, Patrick Robert , YOUNG, Joseph Michael
IPC分类号： C07D487/04 , A61K31/5025 , A61P9/00 , A61P11/00 , A61P25/00 , A61P27/02
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention is directed to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents R 1 , R 3 , R 6 , R 7 , and b are as defined herein. The invention is also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, and methods of preparing the compounds.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐，其中取代基R 1，R 3，R 6，R 7和b如本文所定义。本发明还涉及包含该化合物的药物组合物，使用该化合物的治疗方法，以及制备该化合物的方法。

3. 发明申请

WO2015083028A1 PYRROLO[2,3-D]PYRIMIDINYL, PYRROLO[2,3-B]PYRAZINYL AND PYRROLO[2,3-D]PYRIDINYL ACRYLAMIDES 审中-公开
标题翻译：吡咯并[2,3-D]吡啶基，吡咯并[2,3-b]吡嗪并吡咯并[2,3-D]吡啶-2-基丙烯酰胺
公开(公告)号：WO2015083028A1
公开(公告)日：2015-06-11
申请号：PCT/IB2014/066202
申请日：2014-11-20
申请人： PFIZER INC.
发明人： BROWN, Matthew Frank , CASIMIRO-GARCIA, Agustin , CHE, Ye , COE, Jotham Wadsworth , FLANAGAN, Mark Edward , GILBERT, Adam Matthew , HAYWARD, Matthew Merrill , LANGILLE, Jonathan David , MONTGOMERY, Justin Ian , TELLIEZ, Jean-Baptiste , THORARENSEN, Atli , UNWALLA, Rayomand Jal
IPC分类号： C07D471/04 , C07D487/04 , A61K31/4375 , A61P35/00
CPC分类号： C07D471/04 , C07D471/08 , C07D487/04 , C07D487/10 , C07D498/04
摘要： The present invention provides pharmaceutically active pyrrolo[2,3- d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylamides 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]嘧啶基和吡咯并[2,3-d]吡啶基丙烯酰胺及其类似物。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。

4. 发明申请

WO2014001973A1 NOVEL 4-(SUBSTITUTED-AMINO)-7H-PYRROLO[2,3-d]PYRIMIDINES AS LRRK2 INHIBITORS 审中-公开
标题翻译：新的4-（取代的氨基）-7H-吡咯并[2,3-d]嘧啶作为LRRK2抑制剂
公开(公告)号：WO2014001973A1
公开(公告)日：2014-01-03
申请号：PCT/IB2013/055039
申请日：2013-06-19
申请人： PFIZER INC.
发明人： GALATSIS, Paul , HAYWARD, Matthew Merrill , HENDERSON, Jaclyn , KORMOS, Bethany Lyn , KURUMBAIL, Ravi G , STEPAN, Antonia Friederike , VERHOEST, Patrick Robert , WAGER, Travis T. , ZHANG, Lei
IPC分类号： C07D487/04 , C07D519/00
CPC分类号： A61K31/5377 , C07D487/04 , C07D519/00
摘要： The present invention provides novel 4,5- disubstituted-7H-pyrrolo [2,3- c/]pyrimidine derivatives of Formula I, and the pharmaceutically acceptable salts thereof wherein R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.
摘要翻译：本发明提供式I的新的4,5-二取代-7H-吡咯并[2,3-c]嘧啶衍生物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4和R 5如本说明书中所定义。本发明还涉及包含式I化合物的药物组合物，以及该化合物在治疗与LRRK2相关的疾病中的应用，例如包括帕金森病或阿尔茨海默病，神经变性疾病或克罗恩病或麻风病的神经变性疾病。

5. 发明申请

WO2018020358A1 CYCLIC PEPTIDES AS C5 A RECEPTOR ANTAGONISTS 审中-公开
标题翻译：环肽作为C5受体拮抗剂
公开(公告)号：WO2018020358A1
公开(公告)日：2018-02-01
申请号：PCT/IB2017/054314
申请日：2017-07-17
申请人： PFIZER INC.
发明人： CHE, Ye , FENG, Yiqing , HAYWARD, Matthew Merrill , HEPWORTH, David , JONES, Peter , KAILA, Neelu , PAPAIOANNOU, Nikolaos
IPC分类号： C07K7/56 , A61K38/12 , A61P37/00 , A61P13/12
摘要： The invention relates to cyclic peptide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to cyclic peptide C5a receptor antagonists of formula (Ia)or formula (Ib), or pharmaceutically acceptable salts thereof,wherein R 1a , R 1b , R 2 , R 3 and R 4 areas defined in the description. C5a receptor antagonists are potentially useful in the treatment of a wide range of 1 disorders,including inflammatory disorders and immune disorders.
摘要翻译：本发明涉及环肽衍生物，涉及它们在医学中的用途，含有它们的组合物，其制备方法和用于该方法的中间体。更特别地，本发明涉及式（Ia）或式（Ib）的环肽C5a受体拮抗剂或其药学上可接受的盐，其中R 1a，R 1b，R 在描述中定义的区域2，区域3和区域4。 C5a受体拮抗剂可能用于治疗广泛的1种疾病，包括炎性疾病和免疫疾病。

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

WO2015092592A1 NOVEL 3,4-DISUBSTITUTED-1H-PYRROLO[2,3-B]PYRIDINES AND 4,5-DISUBSTITUTED-7H-PYRROLO[2,3-C]PYRIDAZINES AS LRRK2 INHIBITORS 审中-公开
标题翻译：新的3,4-取代的1H-吡咯并[2,3-B]吡啶和4,5-取代的-7H-吡咯并[2,3-C]吡咯烷作为LRRK2抑制剂
公开(公告)号：WO2015092592A1
公开(公告)日：2015-06-25
申请号：PCT/IB2014/066563
申请日：2014-12-03
申请人： PFIZER INC.
发明人： GALATSIS, Paul , HAYWARD, Matthew Merrill , KORMOS, Bethany Lyn , WAGER, Travis T. , ZHANG, Lei , HENDERSON, Jaclyn Louise , KURUMBAIL, Ravi G. , VERHOEST, Patrick Robert , STEPAN, Antonia Friederike
IPC分类号： C07D471/04 , C07D487/04 , C07D519/00 , A61K31/4375 , A61P25/28
CPC分类号： C07D471/04 , C07D487/04 , C07D491/08 , C07D498/08 , C07D519/00
摘要： The present invention provides novel 3,4-disubstituted-1 H -pyrrolo[2,3- Jb]pyridine derivatives and 4,5-disubstituted-7 H -pyrrolo[2,3-c]pyridazine derivatives of Formula (I), and the pharmaceutically acceptable salts thereof (I) wherein R 1 , R 2 , R 3 , R 4 and X are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.
摘要翻译：本发明提供式（I）的新型3,4-二取代-1H-吡咯并[2,3-b]吡啶衍生物和4,5-二取代-7H-吡咯并[2,3-c]哒嗪衍生物，和其药学上可接受的盐（I）其中R1，R2，R3，R4和X如说明书中所定义。本发明还涉及包含式（I）化合物的药物组合物，以及该化合物在治疗与LRRK2相关的疾病中的应用，例如包括帕金森氏病或阿尔茨海默病，神经变性疾病或克罗恩病或麻风病的神经变性疾病。

8. 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.

9. 发明申请

WO2017145013A1 6,7-DIHYDRO-5H-PYRAZOLO[5,1-B][1,3]OXAZINE-2-CARBOXAMIDE COMPOUNDS 审中-公开
标题翻译： 6,7-二氢-5H-吡唑并[5,1-B] [1,3]恶嗪-2-羧酰胺化合物
公开(公告)号：WO2017145013A1
公开(公告)日：2017-08-31
申请号：PCT/IB2017/050844
申请日：2017-02-15
申请人： PFIZER INC.
发明人： CHAPPIE, Thomas Allen , PATEL, Nandini Chaturbhai , VERHOEST, Patrick Robert , HELAL, Christopher John , SCIABOLA, Simone , LACHAPELLE, Erik Alphie , WAGER, Travis T. , HAYWARD, Matthew Merrill
IPC分类号： C07D498/04 , C07D519/00 , A61K31/5365 , A61P25/00
CPC分类号： C07D498/04 , C07D519/00
摘要： The present invention is directed to PDE4B inhibitors of Formula I: (I) or a pharmaceutically acceptable salt thereof, wherein the substituents R 1 , R 2 , R 3 , and R 4 are as defined herein. The invention is also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, and methods of preparing the compounds.
摘要翻译：本发明涉及式I的PDE4B抑制剂：（I）或其可药用盐，其中取代基R 1， R 2，R 3和R 4如本文所定义。本发明还涉及包含所述化合物的药物组合物，使用所述化合物的治疗方法以及制备所述化合物的方法。

10. 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。

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