公开(公告)号：US20210188863A1

公开(公告)日：2021-06-24

申请号：US16755172

申请日：2018-10-08

申请人： David Annunziato CANDITO ,  Thomas, H. GRAHAM ,  John ACTON ,  Ryan Wing-Kun CHAU ,  Joanna L. CHEN ,  J. Michael ELLIS ,  Peter H. FULLER ,  Anmol GULATI ,  Hakan GUNAYDIN ,  Solomon KATTAR ,  Mitchell Henry KEYLOR ,  Blair T. LAPOINTE ,  Ping LIU ,  Weiguo LIU ,  Joey L. METHOT ,  Santhosh F. NEELAMKAVIL ,  Vladimir SIMOV ,  Ling TONG ,  Harold B. WOOD ,  Merck Sharp & Dohme Corp.

发明人： David Annunziato Candito ,  Thomas H. Graham ,  John Acton ,  Ryan Wing-Kun Chau ,  Joanna L. Chen ,  J. Michael Ellis ,  Peter H. Fuller ,  Anmol Gulati ,  Hakan Gunaydin ,  Solomon Kattar ,  Mitchell Henry Keylor ,  Blair T. Lapointe ,  Ping Liu ,  Weiguo Liu ,  Joey L. Methot ,  Santhosh F. Neelamkavil ,  Vladimir Simov ,  Ling Tong ,  Harold B. Wood

IPC分类号： C07D491/10 ,  C07D403/14 ,  C07D487/08 ,  C07D405/14 ,  C07D401/14 ,  C07D413/14 ,  C07D498/10 ,  C07D519/00 ,  C07D498/04 ,  C07D403/04

摘要： The present invention is directed to substituted certain reversed indazolyl-spiro[2.2]pentane-carbonitrile derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X, Y, and Z are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.

公开(公告)号：US11161854B2

公开(公告)日：2021-11-02

申请号：US16755172

申请日：2018-10-08

申请人： Merck Sharp & Dohme Corp. ,  David Annunziato Candito ,  Thomas H. Graham ,  John Acton ,  Ryan Wing-Kun Chau ,  Joanna L. Chen ,  J. Michael Ellis ,  Peter H. Fuller ,  Anmol Gulati ,  Hakan Gunaydin ,  Solomon Kattar ,  Mitchell Henry Keylor ,  Blair T. Lapointe ,  Ping Liu ,  Weiguo Liu ,  Joey L. Methot ,  Santhosh F. Neelamkavil ,  Vladimir Simov ,  Ling Tong ,  Harold B. Wood

发明人： David Annunziato Candito ,  Thomas H. Graham ,  John Acton ,  Ryan Wing-Kun Chau ,  Joanna L. Chen ,  J. Michael Ellis ,  Peter H. Fuller ,  Anmol Gulati ,  Hakan Gunaydin ,  Solomon Kattar ,  Mitchell Henry Keylor ,  Blair T. Lapointe ,  Ping Liu ,  Weiguo Liu ,  Joey L. Methot ,  Santhosh F. Neelamkavil ,  Vladimir Simov ,  Ling Tong ,  Harold B. Wood

IPC分类号： C07D491/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D487/08 ,  C07D498/04 ,  C07D498/10 ,  C07D519/00

摘要： The present invention is directed to substituted certain reversed indazolyl-spiro[2.2]pentane-carbonitrile derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X, Y, and Z are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.

公开(公告)号：US10975084B2

公开(公告)日：2021-04-13

申请号：US16341313

申请日：2017-10-06

申请人： Merck Sharp & Dohme Corp. ,  Umar Faruk Mansoor ,  Christian Fischer ,  Phieng Siliphaivanh ,  Luis Torres ,  Hakan Gunaydin ,  David L. Sloman

发明人： Umar Faruk Mansoor ,  Christian Fischer ,  Phieng Siliphaivanh ,  Luis Torres ,  Hakan Gunaydin ,  David L. Sloman

IPC分类号： C07D487/04

摘要： The present invention provides a compound of Formula (I) (represented as tautomers Ia and Ib) or the pharmaceutically acceptable salts thereof, which are KDM5 inhibitors.

公开(公告)号：US20200048258A1

公开(公告)日：2020-02-13

申请号：US16341313

申请日：2017-10-06

申请人： UMAR Faruk MANSOOR ,  Christian Fischer ,  Phieng Siliphaivanh ,  Luis Torres ,  Hakan Gunaydin ,  David Sloman ,  Merck Sharp & Dohme Corp.

发明人： UMAR FARUK MANSOOR ,  Christian Fischer ,  Phieng Siliphaivanh ,  Luis Torres ,  Hakan Gunaydin ,  David L. Sloman

IPC分类号： C07D487/04

摘要： The present invention provides a compound of Formula (I) (represented as tautomers Ia and Ib) or the pharmaceutically acceptable salts thereof, which are KDM5 inhibitors.

公开(公告)号：US20200048259A1

公开(公告)日：2020-02-13

申请号：US16341323

申请日：2017-10-06

申请人： Umar Faruk MANSOOR ,  Christian FISCHER ,  Phieng SILIPHAIVANH ,  Hakan GUNAYDIN ,  Merck Sharp & Dohme Corp.

发明人： UMAR FARUK MANSOOR ,  Christian Fischer ,  Phieng Siliphaivanh ,  Hakan Gunaydin

IPC分类号： C07D487/04

摘要： The present invention provides a compound of Formula (I) (represented as tautomers Ia and Ib): (I) or the pharmaceutically acceptable salts thereof, which are KDM5 inhibitors.

公开(公告)号：US20240174679A1

公开(公告)日：2024-05-30

申请号：US18549223

申请日：2022-03-14

申请人： Kaleen Konrad Childers ,  J. Michael Ellis ,  Peter J. Fuller ,  Hakan Gunaydin ,  Jack D. Scott ,  Haiqun Tang ,  Charles S. Yeung ,  MERCK SHARP & DOHME LLC

发明人： Kaleen Konrad Childers ,  J. Michael Ellis ,  Peter J. Fuller ,  Hakan Gunaydin ,  Jack D. Scott ,  Haiqun Tang ,  Charles S. Yeung

IPC分类号： C07D487/04 ,  A61K31/4155 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5365 ,  A61K31/5377 ,  A61K31/55 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D498/04

CPC分类号： C07D487/04 ,  A61K31/4155 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5365 ,  A61K31/5377 ,  A61K31/55 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D498/04

摘要： The present invention is directed to certain (hetero)aroyl 4-aminopyrazole derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, R1, R2, and R3 are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.

公开(公告)号：US10689369B2

公开(公告)日：2020-06-23

申请号：US16356172

申请日：2019-03-18

申请人： Merck Sharp & Dohme Corp.

发明人： Blair T. Lapointe ,  Peter H. Fuller ,  Hakan Gunaydin ,  Kun Liu ,  Mark E. Scott ,  B. Wesley Trotter ,  Hongjun Zhang

IPC分类号： C07D403/08 ,  C07D401/12 ,  C07D401/06 ,  C07D491/107 ,  C07D491/048 ,  C07D487/10 ,  C07D487/04 ,  C07D405/12 ,  C07D403/14 ,  C07D403/06 ,  C07D231/56 ,  C07D403/12 ,  A61P19/02

摘要： The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.

公开(公告)号：US10584121B2

公开(公告)日：2020-03-10

申请号：US15770257

申请日：2016-10-27

申请人： Merck Sharp & Dohme Corp.

发明人： Hongjun Zhang ,  Kenneth Jay Barr ,  Blair T. Lapointe ,  Hakan Gunaydin ,  Kun Liu ,  B. Wesley Trotter

IPC分类号： C07D471/04 ,  A61K31/4353 ,  A61P37/00 ,  A61P11/06 ,  A61P19/02 ,  A61P29/00

摘要： The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.

公开(公告)号：US20190276438A1

公开(公告)日：2019-09-12

申请号：US16356172

申请日：2019-03-18

申请人： Merck Sharp & Dohme Corp.

发明人： Blair T. Lapointe ,  Peter H. Fuller ,  Hakan Gunaydin ,  Kun Liu ,  Mark E. Scott ,  B. Wesley Trotter ,  Hongjun Zhang

IPC分类号： C07D403/08 ,  A61P19/02 ,  C07D401/12 ,  C07D401/06 ,  C07D491/107 ,  C07D491/048 ,  C07D403/12 ,  C07D487/04 ,  C07D405/12 ,  C07D403/14 ,  C07D403/06 ,  C07D231/56 ,  C07D487/10

摘要： The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.

公开(公告)号：US20180312489A1

公开(公告)日：2018-11-01

申请号：US15770256

申请日：2016-10-27

申请人： Merck Sharp & Dohme Corp.

发明人： Blair T. Lapointe ,  Peter H. Fuller ,  Hakan Gunaydin ,  Kun Liu ,  Mark E. Scott ,  B. Wesley Trotter ,  Hongjun Zhang

IPC分类号： C07D403/08 ,  C07D487/10 ,  C07D403/14 ,  C07D491/107 ,  C07D487/04 ,  C07D405/12 ,  C07D401/12 ,  C07D231/56 ,  A61P19/02

CPC分类号： C07D403/08 ,  A61P19/02 ,  C07D231/56 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D487/04 ,  C07D487/10 ,  C07D491/048 ,  C07D491/107

摘要： The present invention relates to compounds according to Formula (I) and pharmaceutically acceptable salts thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.