公开(公告)号：US20170305916A1

公开(公告)日：2017-10-26

申请号：US15529764

申请日：2015-11-20

Applicant: SCOTT D. KUDUK ,  THOMAS S. REGER ,  JASON W. SKUDLAREK

Inventor： SCOTT D. KUDUK ,  THOMAS S. REGER ,  JASON W. SKUDLAREK

IPC: C07D487/04 ,  C07D401/04 ,  C07D401/14 ,  C07D409/14

CPC classification number: C07D487/04 ,  C07D401/04 ,  C07D401/14 ,  C07D409/14

Abstract: The present invention is directed to methyl diazepane 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 compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.

公开(公告)号：US09139576B2

公开(公告)日：2015-09-22

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

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：US20130102619A1

公开(公告)日：2013-04-25

申请号：US13653454

申请日：2012-10-17

Applicant: Scott D. Kuduk ,  Jason W. Skudlarek

Inventor： Scott D. Kuduk ,  Jason W. Skudlarek

IPC: A61K31/4545 ,  C07D417/14 ,  A61P3/04 ,  A61K31/506 ,  A61P25/20 ,  C07D401/14 ,  C07D409/14

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

Abstract: The present invention is directed to 2-pyridyloxy-4-nitrile compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyl-oxy-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-4-腈化合物。 本发明还涉及本文所述的2-吡啶基 - 氧-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：US20160368898A1

公开(公告)日：2016-12-22

申请号：US15103079

申请日：2014-12-04

Applicant: SCOTT D. KUDUK ,  JASON W. SKUDLAREK

Inventor： SCOTT D. KUDUK ,  JASON W. SKUDLAREK

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

CPC classification number: C07D401/14 ,  A61K31/444 ,  A61K31/454 ,  A61K31/506 ,  C07D401/12 ,  C07D409/14 ,  C07D413/14

Abstract: The present invention is directed to 2-pyridyloxy-4-methyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-methyl 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拮抗剂的2-吡啶氧基-4-甲基化合物。 本发明还涉及本文所述的2-吡啶氧基-4-甲基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：US20160318900A1

公开(公告)日：2016-11-03

申请号：US15105815

申请日：2014-12-18

Applicant: SCOTT D. KUDUK ,  JASON W. SKUDLAREK

Inventor： SCOTT D. KUDUK ,  JASON W. SKUDLAREK

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

CPC classification number: C07D401/14 ,  C07D409/14 ,  C07D413/14

Abstract: The present invention is directed to 2-amino-3-ester pyridyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-amino-3-ester pyridyl 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-氨基-3-酯吡啶基化合物。 本发明还涉及本文所述的2-氨基-3-酯吡啶基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：US08785481B2

公开(公告)日：2014-07-22

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: A61K31/4245 ,  C07D249/04

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.

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。

公开(公告)号：US20150322039A1

公开(公告)日：2015-11-12

申请号：US14647766

申请日：2013-11-22

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

Inventor： SCOTT D. KUDUK ,  JASON W. SKUDLAREK

IPC: C07D401/14 ,  C07D409/14

CPC classification number: C07D401/14 ,  C07D409/14

Abstract: The present invention is directed to 2-pyridylamino-4-nitrile-piperidinyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridylamino-4-nitrile-piperidinyl 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-吡啶基氨基-4-腈 - 哌啶基化合物。 本发明还涉及本文所述的2-吡啶基氨基-4-腈 - 哌啶基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：US08975286B2

公开(公告)日：2015-03-10

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

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。

公开(公告)号：US08940898B2

公开(公告)日：2015-01-27

申请号：US14354454

申请日：2012-10-19

Applicant: Scott D. Kuduk ,  Jason W. Skudlarek

Inventor： Scott D. Kuduk ,  Jason W. Skudlarek

IPC: C07D211/68 ,  A61K31/47 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D417/06 ,  C07D417/14

CPC classification number: C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D417/06 ,  C07D417/14

Abstract: The present invention is directed to piperidinyl alkyne compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the piperidinyl alkyne 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素受体拮抗剂的哌啶基炔化合物。 本发明还涉及本文所述的哌啶基炔化合物在治疗或预防涉及食欲素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：US08772276B2

公开(公告)日：2014-07-08

申请号：US14115109

申请日：2012-04-30

Applicant: Scott D. Kuduk ,  Jason W. Skudlarek

Inventor： Scott D. Kuduk ,  Jason W. Skudlarek

IPC: A61K31/397 ,  A61K31/00 ,  A61K31/519 ,  A61K31/44 ,  A61K31/41 ,  C07D401/00 ,  C07D257/00 ,  C07D403/00 ,  C07D249/08

CPC classification number: C07D249/18 ,  C07D401/06 ,  C07D403/06

Abstract: The present invention is directed to alkyne 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受体的增效剂的炔类苯并三唑衍生物，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。