公开(公告)号：US20210188863A1

公开(公告)日：2021-06-24

申请号：US16755172

申请日：2018-10-08

Applicant: 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.

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

Abstract: 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：US10508108B2

公开(公告)日：2019-12-17

申请号：US15532552

申请日：2015-12-01

Applicant: Merck Sharp & Dohme Corp.

Inventor： Christian Fischer ,  Stephane L. Bogen ,  Matthew L. Childers ,  Francesc Xavier Fradera Llinas ,  J. Michael Ellis ,  Sara Esposite ,  Dawn M. Hoffman ,  Chunhui Huang ,  Solomon D. Kattar ,  Alexander J. Kim ,  John W. Lampe ,  Michelle R. Machacek ,  Daniel R. McMasters ,  Dann L. Parker, Jr. ,  Michael H. Reutershan ,  Nunzio Sciammetta ,  Pengcheng P. Shao ,  David L. Sloman ,  Wanying Sun ,  Feroze Ujjainwalla ,  Zhicai Wu ,  Yang Yu ,  Craig R. Gibeau

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

Abstract: The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes (I); wherein A is —C(R1)═ or —N═; and X is selected from the group consisting of: (II-i), and (II-ii). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

公开(公告)号：US20210188818A1

公开(公告)日：2021-06-24

申请号：US16755177

申请日：2018-10-08

Applicant: Merck Sharp & Dohme Corp.

Inventor： John Acton ,  David Annunziato Candito ,  J. Michael Ellis ,  Peter H. Fuller ,  Hakan Gunaydin ,  Blair T. Lapointe ,  Weiguo Liu ,  Joey L. Methot ,  Santhosh F. Neelamkavil ,  Barbara Pio ,  Vladimir Simov ,  Harold B. Wood

IPC: C07D403/14 ,  C07D401/14 ,  C07D498/10 ,  C07D498/04 ,  C07D413/14 ,  C07D519/00 ,  C07D405/14

Abstract: The present invention is directed to substituted certain reversed indazole compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1A, R1B, X, Y, RZ and R2 are as defined herein, which are potent inhibitors of LRRK2 kinase and 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：US11174248B2

公开(公告)日：2021-11-16

申请号：US16755177

申请日：2018-10-08

Applicant: Merck Sharp & Dohme Corp.

Inventor： John Acton ,  David Annunziato Candito ,  J. Michael Ellis ,  Peter H. Fuller ,  Hakan Gunaydin ,  Blair T. Lapointe ,  Weiguo Liu ,  Joey L. Methot ,  Santhosh F. Neelamkavil ,  Barbara Pio ,  Vladimir Simov ,  Harold B. Wood

IPC: A61K31/506 ,  C07D403/14 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D498/04 ,  C07D498/10 ,  C07D519/00

Abstract: The present invention is directed to substituted certain reversed indazole compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1A, R1B, X, Y, RZ and R2 are as defined herein, which are potent inhibitors of LRRK2 kinase and 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

Applicant: 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

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

Abstract: 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.