公开(公告)号：US20230391758A1

公开(公告)日：2023-12-07

申请号：US18043413

申请日：2021-09-15

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Michael J. Breslin ,  Mark E. Fraley ,  Melissa C. Ford ,  Kristen L.G. Jones, SR. ,  Anthony J. Roecker ,  Kathy M. Schirripa ,  Ling Tong

IPC: C07D405/12 ,  C07D471/04 ,  C07D307/85 ,  C07D405/06 ,  C07D453/02 ,  C07D405/14 ,  C07D413/12

CPC classification number: C07D405/12 ,  C07D471/04 ,  C07D307/85 ,  C07D405/06 ,  C07D453/02 ,  C07D405/14 ,  C07D413/12

Abstract: The present invention relates to Compounds of Formula I: and pharmaccutically acceptable salts or prodrug thereof. The present invention also relates to compositions comprising at least one compound of Formula I, and methods of using the compounds of Formula I for treatment or prophylaxis of lysosomal storage diseases, neurodegenerative disease, cystic disease, cancer, or a diseases or disorders associated with elevated levels of glucosylceramide (GlcCer), glucosylsphingosine (GlcSph) and/or other glucosylceramide-based glycosphingolipids (GSLs).

公开(公告)号：US10272077B2

公开(公告)日：2019-04-30

申请号：US15830131

申请日：2017-12-04

Applicant: Merck Sharp & Dohme Corp.

Inventor： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Anthony Ginetti ,  Helen J. Mitchell ,  Daniel V. Paone ,  Donnette D. Staas ,  Cheng Wang ,  C. Blair Zartman

IPC: C07D471/10 ,  A61K31/4545 ,  A61K31/435 ,  A61K31/438 ,  C07D471/20

Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.

公开(公告)号：US20210008055A1

公开(公告)日：2021-01-14

申请号：US16940943

申请日：2020-07-28

Applicant: Merck Sharp & Dohme Corp.

Inventor： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Anthony Ginnetti ,  Helen J. Mitchell ,  Daniel V. Paone ,  Donnette D. Staas ,  Cheng Wang ,  C. Blair Zartman

IPC: A61K31/4545 ,  A61K31/435 ,  A61K31/438 ,  C07D471/10 ,  C07D471/20

Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.

公开(公告)号：US20180092900A1

公开(公告)日：2018-04-05

申请号：US15830131

申请日：2017-12-04

Applicant: Merck Sharp & Dohme Corp.

Inventor： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Anthony Ginetti ,  Helen J. Mitchell ,  Daniel V. Paone ,  Donnette D. Staas ,  Cheng Wang ,  C. Blair Zartman

IPC: A61K31/4545 ,  C07D471/20 ,  A61K31/435 ,  A61K31/438 ,  C07D471/10

CPC classification number: A61K31/4545 ,  A61K31/435 ,  A61K31/438 ,  C07D471/10 ,  C07D471/20

Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.

公开(公告)号：US09914736B2

公开(公告)日：2018-03-13

申请号：US15128782

申请日：2015-03-23

Applicant: Merck Sharp & Dohme Corp.

Inventor： Helen Mitchell ,  Mark E. Fraley ,  Andrew J. Cooke ,  Craig A. Stump ,  Xu-Fang Zhang ,  Casey C. McComas ,  Kathy Schirripa ,  Melody McWherter ,  Ping Liu ,  Dann Parker ,  Chun Sing Li ,  Qinghua Mao

IPC: A61K31/40 ,  C07D487/04 ,  C07D277/46 ,  C07D231/40 ,  C07D417/12 ,  C07D401/04 ,  C07D417/14 ,  C07D403/14 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04

CPC classification number: C07D487/04 ,  C07D231/40 ,  C07D277/46 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

Abstract: The present invention is directed to substituted five membered heteroaryl benzamide compounds of formula (I) (Formula (I)) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.

公开(公告)号：US09833448B2

公开(公告)日：2017-12-05

申请号：US15293569

申请日：2016-10-14

Applicant: Merck Sharp & Dohme Corp.

Inventor： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Anthony Ginnetti ,  Helen J. Mitchell ,  Daniel V. Paone ,  Donnette D. Staas ,  Cheng Wang ,  C. Blair Zartman

IPC: A01N43/42 ,  A61K31/44 ,  A61K31/4545 ,  A61K31/435 ,  A61K31/438 ,  C07D471/10 ,  C07D471/20

CPC classification number: A61K31/4545 ,  A61K31/435 ,  A61K31/438 ,  C07D471/10 ,  C07D471/20

Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.

公开(公告)号：US20190275024A1

公开(公告)日：2019-09-12

申请号：US16396056

申请日：2019-04-26

Applicant: Merck Sharp & Dohme Corp.

Inventor： Ian M. Bell ,  Mark E. Fraley ,  Steven N. Gallicchio ,  Anthony Ginnetti ,  Helen J. Mitchell ,  Daniel V. Paone ,  Donnette D. Staas ,  Cheng Wang ,  C. Blair Zartman

IPC: A61K31/4545 ,  C07D471/20 ,  A61K31/438 ,  A61K31/435 ,  C07D471/10

Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.

公开(公告)号：US20230248715A1

公开(公告)日：2023-08-10

申请号：US18137949

申请日：2023-04-21

Applicant: Merck Sharp & Dohme Corp.

Inventor： Chi-Chung Liu ,  David Michelson ,  Gene Marcantonio ,  Kyle Fliszer ,  Rebecca White ,  Mark E. Fraley ,  Leonardo R. Allain ,  Tiffani Voss ,  John Limanto

IPC: A61K31/4545 ,  A61K9/16 ,  A61P25/06 ,  A61K9/20

CPC classification number: A61K31/4545 ,  A61K9/1652 ,  A61P25/06 ,  A61K9/2054

Abstract: A method of alleviating or mitigating at least one symptom of migraine attack by administering to a patient suffering from a migraine attack a therapeutically effective amount of the compound of Formula I:




or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20190185462A1

公开(公告)日：2019-06-20

申请号：US16309390

申请日：2017-06-19

Applicant: Merck Sharp & Dohme Corp.

Inventor： Abbas Walji ,  Richard Berger ,  Craig A. Stump ,  Kelly Ann S. Schlegel ,  James J. Mulhearn ,  Thomas J. Greshock ,  Deping Wang ,  Mark E. Fraley ,  Kristen G. Jones

IPC: C07D413/10 ,  C07D413/14 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D491/052 ,  C07D498/04 ,  C07D513/04 ,  C07D271/06 ,  C07D471/14 ,  A61P25/28 ,  A61P25/18 ,  A61P29/00 ,  A61P11/06 ,  A61P3/10 ,  A61P35/00 ,  A61P37/02

CPC classification number: C07D413/10 ,  A61K45/06 ,  A61P3/10 ,  A61P9/00 ,  A61P11/06 ,  A61P25/18 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P37/02 ,  C07D271/06 ,  C07D271/113 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D491/048 ,  C07D491/052 ,  C07D498/04 ,  C07D513/04 ,  C07F7/0807

Abstract: The present invention is directed to substituted 5-trifluoromethyl oxadiazole compounds of generic formula (I) or a pharmaceutically acceptable salt thereof. In particular, the invention is directed to a class of aryl and heteroaryl substituted 5-trifluoromethyl oxadiazole compounds of formula I which may be useful as HDAC6 inhibitors for treating cellular proliferative diseases, including cancer, neurodegenerative diseases, such as schizophrenia and stroke, as well as other diseases.

公开(公告)号：US09862716B2

公开(公告)日：2018-01-09

申请号：US15129206

申请日：2015-03-23

Applicant: Merck Sharp & Dohme Corp.

Inventor： Helen Mitchell ,  Mark E. Fraley ,  Andrew J. Cooke ,  Craig A. Stump ,  Yi-Heng Chen ,  Xu-Fang Zhang ,  Casey C. McComas ,  Kathy Schirripa ,  Melody McWherter ,  Swati P. Mercer ,  Keith P. Moore ,  Ping Liu ,  Harold B. Wood ,  Chun Sing Li ,  Qinghua Mao ,  Douglas C. Beshore

IPC: C07D471/04 ,  C07D513/04

CPC classification number: C07D403/12 ,  C07D401/12 ,  C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

Abstract: The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.