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1. 发明申请

WO2020070651A1 BORON CONTAINING PDE4 INHIBITORS 审中-公开
公开(公告)号：WO2020070651A1
公开(公告)日：2020-04-09
申请号：PCT/IB2019/058355
申请日：2019-10-01
申请人： PFIZER INC.
发明人： STROHBACH, Joseph Walter , BLAKEMORE, David Clive , JONES, Peter , LIMBURG, David Christopher , ODERINDE, Martins Sunday , TORELLA, Rubben Federico , YEOH, Thean Yeow , AKAMA, Tsutomu , JACOBS, Robert Toms , PERRY, Matthew Alexander , PLATTNER, Jacob John , ZHOU, Yasheen
IPC分类号： C07F5/02 , A61P29/00 , A61K31/69
摘要： The present invention relates to boron containing compounds of Formula (I) X-Y-Z Formula (I) that inhibit phosphodiesterase 4 (PDE4). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating diseases, conditions, or disorders ameliorated by inhibition of PDE4.

2. 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。

3. 发明申请

WO2016120850A1 SULFONAMIDE-SUBSITUTED INDOLE MODULATORS OF RORC2 AND METHODS OF USE THEREOF 审中-公开
标题翻译： RORC2的磺酰胺 - 取代吲哚调节剂及其使用方法
公开(公告)号：WO2016120850A1
公开(公告)日：2016-08-04
申请号：PCT/IB2016/050477
申请日：2016-01-29
申请人： PFIZER INC.
发明人： SCHNUTE, Mark Edward , FLICK, Andrew Christopher , JONES, Peter , KAILA, Neelu , MENTE, Scot Richard , TRZUPEK, John David , VAZQUEZ, Michael L. , XING, Li , ZHANG, Liying , WENNERSTAL, Goran Mattias , ZAMARATSKI, Edouard
IPC分类号： C07D401/04 , A61K31/4439 , A61P17/06 , C07D401/14 , C07D405/14 , C07D413/14
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14
摘要： The present invention provides sulfonamide-substituted indoles and Methods of Use Thereof-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating RORy activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such indoles and pharmaceutical compositions thereof.
摘要翻译：本发明提供磺酰胺取代的吲哚及其使用方法其中取代的吡咯并吡啶类，其药物组合物，调节受试者中RORγ活性和/或减少IL-17的量的方法，以及方法用这种吲哚及其药物组合物治疗各种医学病症。

4. 发明申请

WO2016046755A1 METHYL-AND TRIFLUOROMETHYL-SUBSTITUTED PYRROLOPYRIDINE MODULATORS OF RORC2 AND METHODS OF USE THEREOF 审中-公开
标题翻译： RORC2的甲基和三氟甲基取代的吡咯啉调节剂及其使用方法
公开(公告)号：WO2016046755A1
公开(公告)日：2016-03-31
申请号：PCT/IB2015/057314
申请日：2015-09-22
申请人： PFIZER INC.
发明人： FLICK, Andrew Christopher , JONES, Peter , KAILA, Neelu , MENTE, Scot Richard , SCHNUTE, Mark Edward , TRZUPEK, John David , VAZQUEZ, Michael L. , XING, Li , ZHANG, Liying , WENNERSTÅL, Göran Mattias , ZAMARATSKI, Edouard
IPC分类号： C07D401/14 , A61K31/454 , A61P29/02 , A61P37/08
CPC分类号： C07D471/04 , C07D401/14
摘要： The present invention provides methyl-and trifluoromethyl-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating RORγ activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such pyrrolopyridines and pharmaceutical compositions thereof.
摘要翻译：本发明提供甲基和三氟甲基取代的吡咯并吡啶类，其药物组合物，调节受试者的RORγ活性和/或减少IL-17的量的方法，以及使用这种吡咯并吡啶治疗各种医学病症的方法及其药物组合物。

5. 发明申请

WO2015015378A2 RORC2 INHIBITORS AND METHODS OF USE THEREOF 审中-公开
标题翻译： RORC2抑制剂及其使用方法
公开(公告)号：WO2015015378A2
公开(公告)日：2015-02-05
申请号：PCT/IB2014/063383
申请日：2014-07-24
申请人： PFIZER INC.
发明人： BLINN, James, Robert , FLICK, Andrew, Christopher , WENNERSTÅL, Göran, Mattias , JONES, Peter , KAILA, Neelu , KIEFER, James, Richard, Jr. , KURUMBAIL, Ravi, G. , MENTE, Scot, Richard , MEYERS, Marvin, Jay , SCHNUTE, Mark, Edward , THORARENSEN, Atli , XING, Li , ZAMARATSKI, Edouard , ZAPF, Christoph, Wolfgang
CPC分类号： C07D401/14 , A61K31/454 , A61K31/497 , A61K31/506 , A61K31/519 , A61K31/5355 , C07D401/04 , C07D403/04 , C07D405/14 , C07D407/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , Y02A50/406 , A61K2300/00
摘要： The present invention provides compounds, pharmaceutical compositions, methods of inhibiting RORγ activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such compounds and pharmaceutical compositions.
摘要翻译：本发明提供化合物，药物组合物，抑制受试者的RORγ活性和/或减少IL-17的量的方法，以及使用这些化合物和药物组合物治疗各种医学病症的方法。

6. 发明申请

WO2016120850A9 SULFONAMIDE-SUBSITUTED INDOLE MODULATORS OF RORC2 AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2016120850A9
公开(公告)日：2016-08-04
申请号：PCT/IB2016/050477
申请日：2016-01-29
申请人： PFIZER INC.
发明人： SCHNUTE, Mark Edward , FLICK, Andrew Christopher , JONES, Peter , KAILA, Neelu , MENTE, Scot Richard , TRZUPEK, John David , VAZQUEZ, Michael L. , XING, Li , ZHANG, Liying , WENNERSTAL, Goran Mattias , ZAMARATSKI, Edouard
IPC分类号： C07D401/04 , A61K31/4439 , A61P17/06 , C07D401/14 , C07D405/14 , C07D413/14
摘要： The present invention provides sulfonamide-substituted indoles and Methods of Use Thereof-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating RORy activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such indoles and pharmaceutical compositions thereof.

7. 发明申请

WO2016120849A9 METHOXY-SUBSTITUTED PYRROLOPYRIDINE MODULATORS OF RORC2 AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2016120849A9
公开(公告)日：2016-08-04
申请号：PCT/IB2016/050473
申请日：2016-01-29
申请人： PFIZER INC.
发明人： SCHNUTE, Mark Edward , FLICK, Andrew Christopher , JONES, Peter , KAILA, Neelu , MENTE, Scot Richard , TRZUPEK, John David , VAZQUEZ, Michael L. , XING, Li , ZHANG, Liying , WENNERSTAL, Goran Mattias , ZAMARATSKI, Edouard
IPC分类号： C07D471/04 , A61K31/435 , A61P29/02 , A61P37/08
摘要： The present invention provides methoxy-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating RORγ activity and/or reducing the amount of IL- 17 in a subject, and methods of treating various medical disorders using such pyrrolopyridines and pharmaceutical compositions thereof.

8. 发明申请

WO2015173683A1 PYRAZOLOPYRIDINES AND PYRAZOLOPYRIMIDINES 审中-公开
标题翻译：吡唑并吡啶和吡唑并吡啶
公开(公告)号：WO2015173683A1
公开(公告)日：2015-11-19
申请号：PCT/IB2015/053174
申请日：2015-04-30
申请人： PFIZER INC.
发明人： COE, Jotham Wadsworth , DEHNHARDT, Christoph Martin , JONES, Peter , SABNIS, Yogesh Anil , STROHBACH, Joseph Walter , WAKENHUT, Florian Michel , WHITLOCK, Gavin Alistair
IPC分类号： C07D471/04 , C07D487/04 , A61K31/4162 , A61P35/00
CPC分类号： A61K31/519 , A61K31/437 , A61K31/4725 , C07D471/04 , C07D487/04
摘要： A compound having the structure: A 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 and A' are independently C or N, where C may be unsubstituted or substituted by halo or C 1 -C 6 alkyl; R and R 0 are independently selected from the group consisting of H, C 1 -C 6 alkyl, hydroxy(C 1 -C 6 alkyl), phenyl(C 1 -C 6 alkyl), and -(CH 2 ) n -W, where W is C 3 -C 8 cycloalkyl, phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocyclic containing 1 -3 N, S and/or 0 atoms, -SO 2 -R', -NHSO 2 -R', -NR"SO 2 -R' and SR', where R' and R" are independently C 1 -C 6 alkyl or C 3 -C 8 cycloalkyl, etc.; wherein each of said alkyl, cycloalkyl, heterocyclic, phenyl, naphthyl or heteroaryl may be unsubstituted or substituted by phenyl, heteroaryl, etc.; or, R and R 0 and the N atom to which they are bonded together form a monocyclic or bicyclic heterocyclic ring which may be unsubstituted or substituted by (a) halo, hydroxy, heteroaryl, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, etc., or (b) -(CH 2 ) n -W, where W is C 3 -C 8 cycloalkyl, phenyl, etc.; R 1 is H, halo or cyano; R 2 and R 2' are independently H, C 1 -C 6 alkyl, cyano, C 1 -C 6 alkoxy, C 1 -C 6 alkylthio, or C 3 -C 8 cycloalkyl where alkyl, alkoxy, or cycloalkyl is optionally substituted by one or more fluorine atoms; X is a bond, -CO-, -CONH-, -S0 2 -, -SONH-, or -(CH 2 ) m -; R 3 is H, C 1 -C 4 alkyl, phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocyclic containing 1 -3 N atoms, a 5-membered heteroaryl or heterocyclic, etc., or (c) 2 O or S atoms and 0-2 N atoms; wherein each of said phenyl, naphthyl, heteroaryl or heterocyclic is optionally substituted by alkyl, 1 substituent -Y-R 4 and/or 1 -4 substituents each independently selected from R 5 ; with the proviso that when X is -CO- or -SO 2 -, R 3 is not H; Y is a bond, -(CH 2 ) m - or -O-; R 4 is (a) H, C 1 -C 6 alkyl, C 3 -C 8 cycloalkl, halo, oxo, -OR 6 , -NR 7 R 8 , -SR 6, -SOR 9 , -SO 2 R 9 , -COR 6 , -OCOR 6 , -COOR 6 , -NR 6 COR 6 , -CONR 7 R 8 , etc.; (b) phenyl or naphthyl, said phenyl and naphthyl being optionally substituted with 1 -5 substituents selected from C 1 -C 6 alkyl, C 3 -C 8 cycloalkyl, halo, cyano, -OR 6 , -NR 7 R 8, etc.; or (c) a 3 to 8-membered saturated or partially unsaturated monocyclic heteroaryl, etc.; R 6 is H, C 1 -C 6 alkyl or C 3 -C 8 cycloalkyl, etc.; R 7 and R 8 are each independently H, C 1 -C 6 alkyl or C 3 -C 8 cycloalkyl or are taken together with the nitrogen atom to which they are attached to form a 4-, 5- or 6-membered saturated heterocyclic ring containing 1 -2 nitrogen atoms or 1 nitrogen and 1 oxygen atom, said C 1 -C 6 alkyl is optionally substituted by C 3 -C 8 cycloalkyl, ha lo, etc., and said heterocyclic ring being optionally substituted by one or more C 1 -C 6 alkyl or C 3 -C 8 cycloalkyli groups; R 9 is C 1 -C 6 alkyl or C 3 -C 8 cycloalkyl; and, m and n are independently 0, 1, 2 or 3. The invention also relates to pharmaceutically acceptable salts of these compounds and to pharmaceutically acceptable solvates thereof; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly asthma and COPD.
摘要翻译：具有以下结构的化合物：具有结构（I）的化合物或其药学上可接受的盐，或所述化合物或其药学上可接受的盐的药学上可接受的溶剂合物，其中A和A'独立地为C或N，其中C可以是未取代的或被卤素或C 1 -C 6烷基取代; R和R 0独立地选自H，C 1 -C 6烷基，羟基（C 1 -C 6烷基），苯基（C 1 -C 6烷基）和 - （CH 2）n W，其中W是C 3 -C 8环烷基，苯基，萘基，含有1-3个S，和/或0个原子的5或6元杂芳基或杂环，-SO 2 -R'，-NHSO 2 -R'，-NR“SO 2 -R'和SR'，其中R '和R“独立地为C 1 -C 6烷基或C 3 -C 8环烷基等; 其中所述烷基，环烷基，杂环，苯基，萘基或杂芳基中的每一个可以是未取代的或被苯基，杂芳基等取代; 或者，R和R 0以及它们所连接的N原子一起形成单环或双环杂环，其可以是未取代的或被（a）卤素，羟基，杂芳基，C 1 -C 6烷基，C 1 -C 6烷氧基等取代。，或（b） - （CH 2）n W，其中W是C 3 -C 8环烷基，苯基等; R1是H，卤素或氰基; R 2和R 2'独立地为H，C 1 -C 6烷基，氰基，C 1 -C 6烷氧基，C 1 -C 6烷硫基或C 3 -C 8环烷基，其中烷基，烷氧基或环烷基任选被一个或多个氟原子取代; X是键，-CO - ， - CONH - ， - SO 2 - ， - SOH-或 - （CH 2）m - ; R3是H，C1-C4烷基，苯基，萘基，含有1-3个N原子的5元或6元杂芳基或杂环，5元杂芳基或杂环等，或（c）2 O或S原子和 0-2个N原子; 其中所述苯基，萘基，杂芳基或杂环中的每一个任选被烷基，1个取代基-Y-R 4和/或1-4个独立地选自R 5的取代基取代; 条件是当X是-CO - 或-SO 2 - 时，R 3不是H; Y是键， - （CH 2）m - 或-O-; R4是（a）H，C1-C6烷基，C3-C8环烷基，卤素，氧代，-OR6，-NR7R8，-SR6，-SOR9，-SO2R9，-COR6，-OCOR6，-COOR6，-NR6COR6，-CONR7R8 等等（b）苯基或萘基，所述苯基和萘基任选被1-5个选自C 1 -C 6烷基，C 3 -C 8环烷基，卤素，氰基，-OR 6，-NR 7 R 8等的取代基取代; 或（c）3至8元饱和或部分不饱和单环杂芳基等; R6是H，C1-C6烷基或C3-C8环烷基等; R 7和R 8各自独立地为H，C 1 -C 6烷基或C 3 -C 8环烷基，或与它们所连接的氮原子一起形成含有1-2个氮的4-，5-或6-元饱和杂环原子或1个氮原子和1个氧原子，所述C 1 -C 6烷基任选被C 3 -C 8环烷基，卤素等取代，所述杂环任选被一个或多个C 1 -C 6烷基或C 3 -C 8环烷基基团取代 ; R9为C1-C6烷基或C3-C8环烷基; m和n独立地为0,1,2或3.本发明还涉及这些化合物及其药学上可接受的溶剂合物的药学上可接受的盐; 含有这些化合物的组合物; 以及这些化合物在治疗各种疾病，特别是哮喘和COPD中的用途。

9. 发明授权

EP3143021B1 PYRAZOLOPYRIDINES AND PYRAZOLOPYRIMIDINES 有权
公开(公告)号：EP3143021B1
公开(公告)日：2019-06-12
申请号：EP15724365.0
申请日：2015-04-30
申请人： Pfizer Inc.
发明人： COE, Jotham Wadsworth , DEHNHARDT, Christoph Martin , JONES, Peter , SABNIS, Yogesh Anil , STROHBACH, Joseph Walter , WAKENHUT, Florian Michel , WHITLOCK, Gavin Alistair
IPC分类号： A61K31/437 , A61K31/4725 , A61K31/519 , C07D471/04 , C07D487/04

10. 发明公开

EP3250570A1 METHOXY-SUBSTITUTED PYRROLOPYRIDINE MODULATORS OF RORC2 AND METHODS OF USE THEREOF 审中-公开
标题翻译：甲氧基取代的RORC2的吡咯并吡啶调节剂及其使用方法
公开(公告)号：EP3250570A1
公开(公告)日：2017-12-06
申请号：EP16703858.7
申请日：2016-01-29
申请人： Pfizer Inc.
发明人： SCHNUTE, Mark Edward , FLICK, Andrew Christopher , JONES, Peter , KAILA, Neelu , MENTE, Scot Richard , TRZUPEK, John David , VAZQUEZ, Michael L. , XING, Li , ZHANG, Liying , WENNERSTAL, Goran Mattias , ZAMARATSKI, Edouard
IPC分类号： C07D471/04 , A61K31/435 , A61P29/02 , A61P37/08
CPC分类号： C07D471/04
摘要： The present invention provides methoxy-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating RORγ activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such pyrrolopyridines and pharmaceutical compositions thereof.

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