公开(公告)号：US20120135977A1

公开(公告)日：2012-05-31

申请号：US13247009

申请日：2011-09-28

Applicant: Douglas C. Beshore ,  Vadim Dudkin ,  Robert M. Garbaccio ,  Adam W. Johnson ,  Scott D. Kuduk ,  Jason W. Skudlarek ,  Cheng Wang ,  Mark E. Fraley

Inventor： Douglas C. Beshore ,  Vadim Dudkin ,  Robert M. Garbaccio ,  Adam W. Johnson ,  Scott D. Kuduk ,  Jason W. Skudlarek ,  Cheng Wang ,  Mark E. Fraley

IPC: A61K31/4192 ,  C07D401/12 ,  A61K31/4439 ,  C07D403/12 ,  A61K31/506 ,  A61K31/497 ,  C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  C07D413/12 ,  A61K31/5377 ,  A61K31/454 ,  A61K31/551 ,  A61K31/55 ,  C07D417/12 ,  A61K31/541 ,  A61P25/00 ,  A61P25/18 ,  C07D249/18

CPC classification number: C07D249/18 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04

Abstract: The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. 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 metabotropic glutamate receptors are involved.

公开(公告)号：US20240067657A1

公开(公告)日：2024-02-29

申请号：US18258903

申请日：2021-12-21

Applicant: Kira A. ARMACOST ,  Richard Thaddeus BERGER ,  Andrew J. COOKE ,  Christopher Douglas COX ,  Brendan M. CROWLEY ,  Marc LABROLI ,  Michael Aaron PLOTKIN ,  Izzat Tiedje RAHEEM ,  Anthony W. SHAW ,  Kelly-Ann S. SCHLEGEL ,  Jason W. SKUDLAREK ,  Ling TONG ,  Merck Sharp & Dohme LLC

Inventor： Kira A. Armacost ,  Richard Thaddeus Berger, Jr. ,  Andrew J. Cooke ,  Christopher Douglas Cox ,  Brendan M. Crowley ,  Marc Labroli ,  Michael Aaron Plotkin ,  Izzat Tiedje Raheem ,  Anthony W. Shaw ,  Kelly-Ann S. Schlegel ,  Jason W. Skudlarek ,  Ling Tong

IPC: C07D498/04 ,  A61K31/517 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D519/00

CPC classification number: C07D498/04 ,  A61K31/517 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D519/00

Abstract: The present invention relates to novel Amido-Substituted Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R7, and R8 are as defined herein. The present invention also relates to compositions comprising at least one Amido-Substituted Heterocycle Compound, and methods of using the Amido-Substituted Heterocycle Compounds for treating or preventing a herpesvirus infection in a patient.

公开(公告)号：US20160214960A1

公开(公告)日：2016-07-28

申请号：US14653812

申请日：2013-12-16

Applicant: Scott D. KUDUK ,  Jason W. SKUDLAREK ,  MERCK SHARP & DOHME CORP.

Inventor： SCOTT D. KUDUK ,  JASON W. SKUDLAREK

IPC: C07D401/14

CPC classification number: C07D401/14

Abstract: The present invention is directed to 2-pyridyloxy-4-ester compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-ester compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

Abstract translation: 本发明涉及作为食欲肽受体拮抗剂的2-吡啶氧基-4-酯化合物。 本发明还涉及本文所述的2-吡啶氧基-4-酯化合物在潜在的治疗或预防涉及食欲肽受体的神经和精神疾病和疾病中的用途。 本发明还涉及包含这些化合物的药物组合物。 本发明还涉及这些药物组合物在预防或治疗涉及食欲素受体的疾病中的用途。

公开(公告)号：US20160102073A1

公开(公告)日：2016-04-14

申请号：US14786034

申请日：2014-04-21

Applicant: Scott D. KUDUK ,  Jason W. SKUDLAREK ,  MERCK SHARP & DOHME CORP.

Inventor： SCOTT D. KUDUK ,  JASON W. SKUDLAREK

IPC: C07D401/12 ,  C07D409/14 ,  C07D401/14

CPC classification number: C07D401/12 ,  C07D401/00 ,  C07D401/14 ,  C07D409/14

Abstract: The present invention is directed to 2-hydroxymethyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

Abstract translation: 本发明涉及作为食欲肽受体拮抗剂的2-羟甲基化合物。 本发明还涉及本文所述的化合物在涉及食欲素受体的神经和精神病症和疾病的潜在治疗或预防中的用途。 本发明还涉及包含这些化合物的药物组合物。 本发明还涉及这些药物组合物在预防或治疗涉及食欲素受体的疾病中的用途。

公开(公告)号：US20160016935A1

公开(公告)日：2016-01-21

申请号：US14772272

申请日：2014-03-03

Applicant: Scott D. KUDUK ,  Jason W. SKUDLAREK ,  MERCK SHARP & DOHME CORP.

Inventor： SCOTT D. KUDUK ,  JASON W. SKUDLAREK

IPC: C07D401/14 ,  C07D409/14 ,  C07D413/14 ,  C07D401/12 ,  C07D417/14

CPC classification number: C07D401/14 ,  C07D401/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention is directed to 2-pyridyloxy-4-ether compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-ether compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

Abstract translation: 本发明涉及作为食欲素受体的拮抗剂的2-吡啶氧基-4-醚化合物。 本发明还涉及本文所述的2-吡啶氧基-4-醚化合物在潜在的治疗或预防涉及食欲肽受体的神经和精神疾病和疾病中的用途。 本发明还涉及包含这些化合物的药物组合物。 本发明还涉及这些药物组合物在预防或治疗涉及食欲素受体的疾病中的用途。

公开(公告)号：US20150322040A1

公开(公告)日：2015-11-12

申请号：US14653814

申请日：2013-12-16

Applicant: Scott D. KUDUK ,  Jason W. SKUDLAREK ,  MERCK SHARP & DOHME CORP.

Inventor： Scott D. KUDUK ,  Jason W. SKUDLAREK

IPC: C07D401/14 ,  C07D401/10

CPC classification number: C07D401/14 ,  C07D401/10

Abstract: The present invention is directed to 3-ester-4-substituted compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 3-ester-4-substituted compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

Abstract translation: 本发明涉及作为食欲肽受体的拮抗剂的3-酯-4-取代的化合物。 本发明还涉及本文所述的3-酯-4-取代的化合物在潜在的治疗或预防涉及食欲肽受体的神经和精神疾病和疾病中的用途。 本发明还涉及包含这些化合物的药物组合物。 本发明还涉及这些药物组合物在预防或治疗涉及食欲素受体的疾病中的用途。

公开(公告)号：US20150252033A1

公开(公告)日：2015-09-10

申请号：US14436380

申请日：2013-10-14

Applicant: Scott D. KUDUK ,  Jason W. SKUDLAREK ,  MERCK SHARP & DOHME CORP.

Inventor： Scott D. Kuduk ,  Jason W. Skudlarek

IPC: C07D413/14 ,  C07D401/12 ,  C07D401/14

CPC classification number: C07D413/14 ,  C07D401/12 ,  C07D401/14

Abstract: The present invention is directed to 2-pyridyloxy-3-ester-4-nitrile compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-3-ester-4-nitrile compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

Abstract translation: 本发明涉及作为食欲肽受体拮抗剂的2-吡啶氧基-3-酯-4-腈化合物。 本发明还涉及本文所述的2-吡啶氧基-3-酯-4-腈化合物在治疗或预防涉及食欲肽受体的神经和精神病症和疾病中的用途。 本发明还涉及包含这些化合物的药物组合物。 本发明还涉及这些药物组合物在预防或治疗涉及食欲素受体的疾病中的用途。

公开(公告)号：US20140066443A1

公开(公告)日：2014-03-06

申请号：US14115123

申请日：2012-04-30

Applicant: Douglas C. Beshore ,  Robert M. Garbaccio ,  Scott D. Kuduk ,  Adam W. Johnson ,  Jason W. Skudlarek

Inventor： Douglas C. Beshore ,  Robert M. Garbaccio ,  Scott D. Kuduk ,  Adam W. Johnson ,  Jason W. Skudlarek

IPC: C07D413/12 ,  C07D401/12 ,  C07D249/18 ,  C07D401/14 ,  C07D403/10

CPC classification number: C07D413/12 ,  C07D249/18 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D413/10

Abstract: The present invention is directed to aminomethyl biaryl benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. 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 metabotropic glutamate receptors are involved.

Abstract translation: 本发明涉及作为代谢型谷氨酸受体，特别是mGluR2受体的增效剂的氨基甲基联芳基苯并三唑衍生物，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及涉及代谢型谷氨酸受体的疾病 。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。

公开(公告)号：US20120149677A1

公开(公告)日：2012-06-14

申请号：US13391315

申请日：2010-08-16

Applicant: Vadim Y. Dudkin ,  Mark E. Fraley ,  Cheng Wang ,  Robert M. Garbaccio ,  Douglas C. Beshore ,  Scott K. Kuduk ,  Jason W. Skudlarek

Inventor： Vadim Y. Dudkin ,  Mark E. Fraley ,  Cheng Wang ,  Robert M. Garbaccio ,  Douglas C. Beshore ,  Scott K. Kuduk ,  Jason W. Skudlarek

IPC: A61K31/4439 ,  C07D403/12 ,  C07D495/04 ,  C07D403/14 ,  C07D401/14 ,  C07D417/14 ,  A61K31/497 ,  A61K31/4709 ,  A61K31/506 ,  A61K31/519 ,  A61K31/444 ,  A61K31/541 ,  A61K31/438 ,  A61P25/00 ,  A61P25/18 ,  C07D401/12

CPC classification number: C07D417/14 ,  A61K31/4192 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  C07D249/18 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D495/04 ,  C07D498/04

Abstract: The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. 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 metabotropic glutamate receptors are involved.

Abstract translation: 本发明涉及作为代谢型谷氨酸受体，特别是mGluR2受体的增强剂的醚苯并三唑衍生物，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及涉及代谢型谷氨酸受体的疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。