公开(公告)号：US20210169894A1

公开(公告)日：2021-06-10

申请号：US17032692

申请日：2020-09-25

Applicant: Genzyme Corporation

Inventor： John L. Kane, JR. ,  Gloria Matthews ,  Markus Metz ,  Michael Kothe ,  Jinyu Liu ,  Andrew Scholte

IPC: A61K31/551 ,  C07F9/6506 ,  A61K31/501 ,  C07D401/14 ,  C07D405/14 ,  A61K31/444 ,  C07D487/10 ,  C07D401/12 ,  A61K31/506 ,  C07D413/14 ,  A61K31/4545 ,  C07D519/00 ,  A61K31/5377 ,  C07D401/04 ,  C07D413/04 ,  A61K31/4439 ,  C07D471/08 ,  C07D403/14 ,  C07D471/10 ,  C07F9/50 ,  C07D417/14 ,  A61K31/4184 ,  C07F9/6558 ,  C07D487/04 ,  A61K31/496 ,  A61K31/4725 ,  C07D487/08 ,  C07F9/6561 ,  A61K31/437 ,  C07D403/04 ,  C07D471/04

Abstract: Tropomyosin-related kinase inhibitors (Trk inhibitors) are small molecule compounds useful in the treatment of disease. Trk inhibitors can be used as pharmaceutical agents and in pharmaceutical compositions. Trk inhibitors are useful in the treatment of inflammatory diseases, autoimmune disease, defects of bone metabolism and/or cancer, and are particularly useful in the treatment of osteoarthritis (OA), pain, and pain associated with OA. Trk inhibitors are also useful for inhibiting tropomyosin-related kinase A (TrkA), tropomyosin-related kinase B (TrkB), tropomyosin-related kinase C (TrkC), and/or c-FMS (the cellular receptor for colony stimulating factor-1 (CSF-1)).

公开(公告)号：US12060349B2

公开(公告)日：2024-08-13

申请号：US17230385

申请日：2021-04-14

Applicant: Genzyme Corporation

Inventor： Elyse Bourque ,  Mario A. Cabrera-Salazar ,  Cassandra Celatka ,  Seng H. Cheng ,  Bradford Hirth ,  Andrew Good ,  Katherine Jancsics ,  John Marshall ,  Markus Metz ,  Ronald K. Scheule ,  Renato Skerlj ,  Yibin Xiang ,  Zhong Zhao ,  John Leonard ,  Thomas Natoli ,  Elina Makino ,  Herve Husson ,  Oxana Beskrovnaya

IPC: C07D453/02 ,  A61K31/439 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  C07D471/08

CPC classification number: C07D453/02 ,  A61K31/439 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  C07D471/08

Abstract: The invention relates to inhibitors of glucosylceramide synthase (GCS) of the Formula I: represented by the following structural formula




or a pharmaceutically acceptable salt thereof, wherein the variables are as defined herein, useful for the treatment of metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, cystic disease and for the treatment of cancer.

公开(公告)号：US20240217991A1

公开(公告)日：2024-07-04

申请号：US18404409

申请日：2024-01-04

Applicant: GENZYME CORPORATION

Inventor： John L. Kane, JR. ,  Claude Barberis ,  Mark Czekaj ,  Paul Erdman ,  Barret Giese ,  Michael Kothe ,  Tieu-Binh Le ,  Jinyu Liu ,  Liang Ma ,  Markus Metz ,  Vinod Patel ,  Andrew Scholte ,  Patrick Shum ,  Linli Wei

IPC: C07D519/00 ,  A61P37/06 ,  C07D405/06 ,  C07D471/04 ,  C07D487/04

CPC classification number: C07D519/00 ,  A61P37/06 ,  C07D405/06 ,  C07D471/04 ,  C07D487/04

Abstract: Compounds of the formulas




which are useful as colony stimulating factor-1 receptor inhibitors (“CSF-1R inhibitors”).

公开(公告)号：US11274108B2

公开(公告)日：2022-03-15

申请号：US15745223

申请日：2016-07-19

Applicant: Genzyme Corporation

Inventor： John L. Kane, Jr. ,  Claude Barberis ,  Mark Czekaj ,  Paul Erdman ,  Barret Giese ,  Michael Kothe ,  Tieu-Binh Le ,  Jinyu Liu ,  Liang Ma ,  Markus Metz ,  Vinod Patel ,  Andrew Scholte ,  Patrick Wai-Kwok Shum ,  Linli Wei

IPC: C07D519/00 ,  C07D471/04 ,  C07D405/06 ,  C07D487/04 ,  A61P37/06

Abstract: Compounds of the formulas which are useful as colony stimulating factor-1 receptor inhibitors (“CSF-1R inhibitors”).

公开(公告)号：US10166239B2

公开(公告)日：2019-01-01

申请号：US15436195

申请日：2017-02-17

Applicant: Genzyme Corporation

Inventor： John L. Kane, Jr. ,  Gloria Matthews ,  Markus Metz ,  Michael Kothe ,  Jinyu Liu ,  Andrew Scholte

IPC: A61K31/4184 ,  A61K31/437 ,  C07D471/04 ,  C07D413/04 ,  C07D401/04 ,  C07D403/04 ,  A61K31/551 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D487/04 ,  C07D487/10 ,  C07F9/6506 ,  C07D413/14 ,  C07D417/14 ,  C07D487/08 ,  C07F9/6558 ,  C07F9/6561 ,  C07D471/08 ,  C07D471/10 ,  C07D519/00 ,  C07F9/50 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377

Abstract: Tropomyosin-related kinase inhibitors (Trk inhibitors) are small molecule compounds useful in the treatment of disease. Trk inhibitors can be used as pharmaceutical agents and in pharmaceutical compositions. Trk inhibitors are useful in the treatment of inflammatory diseases, autoimmune disease, defects of bone metabolism and/or cancer, and are particularly useful in the treatment of osteoarthritis (OA), pain, and pain associated with OA. Trk inhibitors are also useful for inhibiting tropomyosin-related kinase A (TrkA), tropomyosin-related kinase B (TrkB), tropomyosin-related kinase C (TrkC), and/or c-FMS (the cellular receptor for colony stimulating factor-1 (CSF-1)).

公开(公告)号：US09067914B1

公开(公告)日：2015-06-30

申请号：US14564773

申请日：2014-12-09

Applicant: Genzyme Corporation

Inventor： John L. Kane, Jr. ,  Gloria Matthews ,  Markus Metz ,  Michael Kothe ,  Jinyu Liu ,  Andrew Scholte

IPC: C07D403/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D487/04 ,  C07D487/10 ,  C07F9/6506 ,  C07D401/12

CPC classification number: A61K31/551 ,  A61K31/4184 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D519/00 ,  C07F9/5022 ,  C07F9/6506 ,  C07F9/65583 ,  C07F9/6561

Abstract: Tropomyosin-related kinase inhibitors (Trk inhibitors) are small molecule compounds useful in the treatment of disease. Trk inhibitors can be used as pharmaceutical agents and in pharmaceutical compositions. Trk inhibitors are useful in the treatment of inflammatory diseases, autoimmune disease, defects of bone metabolism and/or cancer, and are particularly useful in the treatment of osteoarthritis (OA), pain, and pain associated with OA. Trk inhibitors are also useful for inhibiting tropomyosin-related kinase A (TrkA), tropomyosin-related kinase B (TrkB), tropomyosin-related kinase C (TrkC), and/or c-FMS (the cellular receptor for colony stimulating factor-1 (CSF-1)).

Abstract translation: 原肌球蛋白相关激酶抑制剂（Trk抑制剂）是用于治疗疾病的小分子化合物。 Trk抑制剂可用作药剂和药物组合物。 Trk抑制剂可用于治疗炎性疾病，自身免疫性疾病，骨代谢缺陷和/或癌症，并且特别可用于治疗骨关节炎（OA），疼痛和与OA相关的疼痛。 Trk抑制剂也可用于抑制原肌球蛋白相关激酶A（TrkA），原肌球蛋白相关激酶B（TrkB），原肌球蛋白相关激酶C（TrkC）和/或c-FMS（集落刺激因子-1的细胞受体 （CSF-1））。

公开(公告)号：US20230080874A1

公开(公告)日：2023-03-16

申请号：US17883350

申请日：2022-08-08

Applicant: Genzyme Corporation

Inventor： John L. Kane, JR. ,  Gloria Matthews ,  Markus Metz ,  Michael Kothe ,  Jinyu Liu ,  Andrew Scholte

IPC: A61K31/551 ,  C07D403/04 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D487/04 ,  C07D487/10 ,  C07F9/6506 ,  C07D413/14 ,  C07D417/14 ,  C07D487/08 ,  C07F9/6558 ,  C07F9/6561 ,  C07D413/04 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D519/00 ,  C07F9/50 ,  A61K31/4184 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377

Abstract: Tropomyosin-related kinase inhibitors (Trk inhibitors) are small molecule compounds useful in the treatment of disease. Trk inhibitors can be used as pharmaceutical agents and in pharmaceutical compositions. Trk inhibitors are useful in the treatment of inflammatory diseases, autoimmune disease, defects of bone metabolism and/or cancer, and are particularly useful in the treatment of osteoarthritis (OA), pain, and pain associated with OA. Trk inhibitors are also useful for inhibiting tropomyosin-related kinase A (TrkA), tropomyosin-related kinase B (TrkB), tropomyosin-related kinase C (TrkC), and/or c-FMS (the cellular receptor for colony stimulating factor-1 (CSF-1)).

公开(公告)号：US11406644B2

公开(公告)日：2022-08-09

申请号：US17032692

申请日：2020-09-25

Applicant: Genzyme Corporation

Inventor： John L. Kane, Jr. ,  Gloria Matthews ,  Markus Metz ,  Michael Kothe ,  Jinyu Liu ,  Andrew Scholte

IPC: A61K31/4184 ,  A61K31/437 ,  A61K31/551 ,  C07F9/6506 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/496 ,  C07D403/04 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D487/04 ,  C07D487/10 ,  C07D413/14 ,  C07D417/14 ,  C07D487/08 ,  C07F9/6558 ,  C07F9/6561 ,  C07D413/04 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D519/00 ,  C07F9/50 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377

Abstract: Tropomyosin-related kinase inhibitors (Trk inhibitors) are small molecule compounds useful in the treatment of disease. Trk inhibitors can be used as pharmaceutical agents and in pharmaceutical compositions. Trk inhibitors are useful in the treatment of inflammatory diseases, autoimmune disease, defects of bone metabolism and/or cancer, and are particularly useful in the treatment of osteoarthritis (OA), pain, and pain associated with OA. Trk inhibitors are also useful for inhibiting tropomyosin-related kinase A (TrkA), tropomyosin-related kinase B (TrkB), tropomyosin-related kinase C (TrkC), and/or c-FMS (the cellular receptor for colony stimulating factor-1 (CSF-1)).

公开(公告)号：US11008316B2

公开(公告)日：2021-05-18

申请号：US15490385

申请日：2017-04-18

Applicant: Genzyme Corporation

Inventor： Elyse Bourque ,  Mario A. Cabrera-Salazar ,  Cassandra Celatka ,  Seng H. Cheng ,  Bradford Hirth ,  Andrew Good ,  Katherine Jancsics ,  John Marshall ,  Markus Metz ,  Ronald K. Scheule ,  Renato Skerlj ,  Yibin Xiang ,  Zhong Zhao ,  John Leonard ,  Thomas Natoli ,  Elina Makino ,  Herve Husson ,  Oxana Beskrovnaya

IPC: C07D453/02 ,  C07D471/08 ,  A61K31/439 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06

Abstract: The invention relates to inhibitors of glucosylceramide synthase (GCS), such as Compound of Formula I, shown below, as defined herein, useful for the treatment of metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, cystic disease and for the treatment of cancer.

公开(公告)号：US20220396588A1

公开(公告)日：2022-12-15

申请号：US17668209

申请日：2022-02-09

Applicant: Genzyme Corporation

Inventor： John L. Kane, JR. ,  Claude Barberis ,  Mark Czekaj ,  Paul Erdman ,  Barret Giese ,  Michael Kothe ,  Tieu-Binh Le ,  Jinyu Liu ,  Liang Ma ,  Markus Metz ,  Vinod Patel ,  Andrew Scholte ,  Patrick Shum ,  Linli Wei

IPC: C07D519/00 ,  C07D405/06 ,  C07D471/04 ,  C07D487/04 ,  A61P37/06

Abstract: Compounds of the formulas which are useful as colony stimulating factor-1 receptor inhibitors (“CSF-1R inhibitors”).