公开(公告)号：US20160229847A1

公开(公告)日：2016-08-11

申请号：US15022313

申请日：2014-09-22

Applicant: PFIZER INC.

Inventor： Martin Youngjin Pettersson ,  Christopher William am Ende ,  Michael Eric Green ,  Douglas Scott Johnson ,  Gregory Wayne Kauffman ,  Christopher William O'Donnell ,  Nandini Chaturbhai Patel ,  Antonia Friederike Stepan ,  Cory Michael Stiff ,  Chakrapani Subramanyam ,  Tuan Phong Tran ,  Patrick Robert Verhoest

IPC: C07D471/04 ,  C07D498/04

CPC classification number: C07D471/04 ,  C07D498/04

Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula II as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract translation: 公开了化合物的化合物和药学上可接受的盐，其中所述化合物具有如说明书中定义的式II的结构。 还公开了相应的药物组合物，治疗方法，合成方法和中间体。

公开(公告)号：US20170073343A1

公开(公告)日：2017-03-16

申请号：US15262112

申请日：2016-09-12

Applicant: Pfizer Inc.

Inventor： Paul Galatsis ,  Jaclyn Louise Henderson ,  Bethany Lyn Kormos ,  Ravi G. Kurumbail ,  Matthew Richard Reese ,  Antonia Friederike Stepan ,  Patrick Robert Verhoest ,  Travis T. Wager ,  Martin Youngjin Pettersson ,  Michelle Renee Garnsey

IPC: C07D471/04 ,  C07D471/14 ,  C07D519/00

CPC classification number: A61K31/435 ,  A61K31/4745 ,  C07D215/38 ,  C07D215/42 ,  C07D471/04 ,  C07D471/14 ,  C07D519/00

Abstract: The present invention provides novel imidazo[4,5-c]quinoline and imidazo[4,5-c][1,5]naphthyridine derivatives of Formula (I), and the pharmaceutically acceptable salts thereof wherein R1, R1a, R1b, R2, R4, R5, R6, X and Z 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.

Abstract translation: 其中R1，R1a，R1b，R2，R4，R5，R6，X和Z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，例如包括帕金森病或阿尔茨海默氏病，癌症，克罗恩病或麻风病的神经变性疾病。

公开(公告)号：US20140005183A1

公开(公告)日：2014-01-02

申请号：US13928696

申请日：2013-06-27

Applicant: Pfizer Inc.

Inventor： Paul Galatsis ,  Matthew Merrill Hayward ,  Bethany Lyn Kormos ,  Travis T. Wager ,  Lei Zhang ,  Antonia Friederike Stepan ,  Jaclyn Louise Henderson ,  Ravi G. Kurumbail ,  Patrick Robert Verhoest

IPC: C07D487/04 ,  C07D519/00

CPC classification number: A61K31/5377 ,  C07D487/04 ,  C07D519/00

Abstract: The present invention provides novel 4,5-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives of Formula I, and the pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4 and R5 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.

Abstract translation: 本发明提供了式I的新的4,5-二取代的-7H-吡咯并[2,3-d]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。

公开(公告)号：US20170096428A1

公开(公告)日：2017-04-06

申请号：US15382778

申请日：2016-12-19

Applicant: Pfizer Inc.

Inventor： Martin Youngjin Pettersson ,  Christopher William am Ende ,  Douglas Scott Johnson ,  Gregory Wayne Kauffman ,  Antonia Friederike Stepan ,  Patrick Robert Verhoest

IPC: C07D471/04

CPC classification number: C07D471/04 ,  A61K31/4985

Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I wherein X, R1, R2a, R2b, R4a, R4b, R5a, R5b, R6, R7, R10, R11, and y are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：US20150366874A1

公开(公告)日：2015-12-24

申请号：US14840528

申请日：2015-08-31

Applicant: Pfizer Inc.

Inventor： Paul Galatsis ,  Matthew Merrill Hayward ,  Bethany Lyn Kormos ,  Travis T. Wager ,  Lei Zhang ,  Antonia Friederike Stepan ,  Jaclyn Louise Henderson ,  Ravi G. Kurumbail ,  Patrick Robert Verhoest

IPC: A61K31/5377

CPC classification number: A61K31/5377 ,  C07D487/04 ,  C07D519/00

Abstract: The present invention provides novel 4,5-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives of Formula I, and the pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4 and R5 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.

Abstract translation: 本发明提供了式I的新的4,5-二取代的-7H-吡咯并[2,3-d]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。

公开(公告)号：US09193726B2

公开(公告)日：2015-11-24

申请号：US14543020

申请日：2014-11-17

Applicant: Pfizer Inc.

Inventor： Martin Youngjin Pettersson ,  Douglas Scott Johnson ,  Chakrapani Subramanyam ,  Christopher John O'Donnell ,  Christopher William am Ende ,  Michael Eric Green ,  Nandini Chaturbhai Patel ,  Cory Michael Stiff ,  Tuan Phong Tran ,  Gregory Wayne Kauffman ,  Antonia Friederike Stepan ,  Patrick Robert Verhoest

IPC: C07D241/36 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract translation: 公开了化合物的化合物和药学上可接受的盐，其中化合物具有说明书中定义的式I的结构。 还公开了相应的药物组合物，治疗方法，合成方法和中间体。

公开(公告)号：US08916564B2

公开(公告)日：2014-12-23

申请号：US14031163

申请日：2013-09-19

Applicant: Pfizer Inc.

Inventor： Martin Youngjin Pettersson ,  Douglas Scott Johnson ,  Chakrapani Subramanyam ,  Christopher John O'Donnell ,  Christopher William am Ende ,  Michael Eric Green ,  Nandini Chaturbhai Patel ,  Cory Michael Stiff ,  Tuan Phong Tran ,  Gregory Wayne Kauffman ,  Antonia Friederike Stepan ,  Patrick Robert Verhoest

IPC: A61K31/4985 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract translation: 公开了化合物的化合物和药学上可接受的盐，其中化合物具有说明书中定义的式I的结构。 还公开了相应的药物组合物，治疗方法，合成方法和中间体。

公开(公告)号：US20140088111A1

公开(公告)日：2014-03-27

申请号：US14031163

申请日：2013-09-19

Applicant: Pfizer Inc.

Inventor： Martin Youngjin Pettersson ,  Douglas Scott Johnson ,  Chakrapani Subramanyam ,  Christopher John O'Donnell ,  Christopher William am Ende ,  Michael Eric Green ,  Nandini Chaturbhai Patel ,  Cory Michael Stiff ,  Tuan Phong Tran ,  Gregory Wayne Kauffman ,  Antonia Friederike Stepan ,  Patrick Robert Verhoest

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract translation: 公开了化合物的化合物和药学上可接受的盐，其中化合物具有说明书中定义的式I的结构。 还公开了相应的药物组合物，治疗方法，合成方法和中间体。

公开(公告)号：US09765073B2

公开(公告)日：2017-09-19

申请号：US15382778

申请日：2016-12-19

Applicant: Pfizer Inc.

Inventor： Martin Youngjin Pettersson ,  Christopher William am Ende ,  Douglas Scott Johnson ,  Gregory Wayne Kauffman ,  Antonia Friederike Stepan ,  Patrick Robert Verhoest

IPC: C07D471/04 ,  A61K31/4985

CPC classification number: C07D471/04 ,  A61K31/4985

Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I wherein X, R1, R2a, R2b, R4a, R4b, R5a, R5b, R6, R7, R10, R11, and y are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：US09751877B2

公开(公告)日：2017-09-05

申请号：US14877118

申请日：2015-10-07

Applicant: Pfizer Inc.

Inventor： Martin Youngjin Pettersson ,  Douglas Scott Johnson ,  Chakrapani Subramanyam ,  Christopher John O'Donnell ,  Christopher William am Ende ,  Michael Eric Green ,  Nandini Chaturbhai Patel ,  Cory Michael Stiff ,  Tuan Phong Tran ,  Gregory Wayne Kauffman ,  Antonia Friederike Stepan ,  Patrick Robert Verhoest

IPC: A61K31/4985 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.