公开(公告)号：US08975286B2

公开(公告)日：2015-03-10

申请号：US13391315

申请日：2010-08-16

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

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

IPC分类号： 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分类号： 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

摘要： 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.

摘要翻译： 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：US20120149677A1

公开(公告)日：2012-06-14

申请号：US13391315

申请日：2010-08-16

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

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

IPC分类号： 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分类号： 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

摘要： 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.

摘要翻译： 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：US08785481B2

公开(公告)日：2014-07-22

申请号：US13247009

申请日：2011-09-28

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

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

IPC分类号： A61K31/4245 ,  C07D249/04

CPC分类号： C07D249/18 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04

摘要： 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.

摘要翻译： 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：US20120135977A1

公开(公告)日：2012-05-31

申请号：US13247009

申请日：2011-09-28

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

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

IPC分类号： 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分类号： C07D249/18 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04

摘要： 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：US09139576B2

公开(公告)日：2015-09-22

申请号：US14115123

申请日：2012-04-30

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

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

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

CPC分类号： C07D413/12 ,  C07D249/18 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D413/10

摘要： 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.

摘要翻译： 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：US20140066443A1

公开(公告)日：2014-03-06

申请号：US14115123

申请日：2012-04-30

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

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

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

CPC分类号： C07D413/12 ,  C07D249/18 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D413/10

摘要： 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.

摘要翻译： 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

申请人： Scott D. Kuduk ,  Jason W. Skudlarek

发明人： Scott D. Kuduk ,  Jason W. Skudlarek

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

CPC分类号： C07D401/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： 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.

摘要翻译： 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：US20230066268A1

公开(公告)日：2023-03-02

申请号：US17784718

申请日：2020-12-15

申请人： Andrew John COOKE ,  Christopher D. COX ,  Scott D. EDMONDSON ,  Charles Lee JAYNE ,  Anilkumar NAIR ,  Jeffrey W. SCHUBERT ,  Jason W. SKUDLAREK ,  David M. TELLERS ,  De-Yi YANG ,  Merck Sharp & Dohme LLC

发明人： Andrew John Cooke ,  Christopher D. Cox ,  Scott D. Edmondson ,  Charles Lee Jayne ,  Anilkumar G. Nair ,  Jeffrey W. Schubert ,  Jason W. Skudlarek ,  David M. Tellers ,  De-Yi Yang

IPC分类号： A61K31/416 ,  A61K31/4245 ,  A61K31/427 ,  C07D231/56 ,  A61P31/22

摘要： The present invention relates to novel Indazole Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, X, Y, Z, R1 R5 and R6 are as defined herein. The present invention also relates to compositions comprising at least one Indazole Derivative, and methods of using the Indazole Derivatives for treating or preventing a herpesvirus infection in a patient.

公开(公告)号：US09586950B2

公开(公告)日：2017-03-07

申请号：US14436380

申请日：2013-10-14

申请人： MERCK SHARP & DOHME CORP. ,  Scott D. Kuduk ,  Jason W. Skudlarek

发明人： Scott D. Kuduk ,  Jason W. Skudlarek

IPC分类号： C07D401/14 ,  A61K31/4545 ,  C07D413/14 ,  C07D401/12

CPC分类号： C07D413/14 ,  C07D401/12 ,  C07D401/14

摘要： 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.

摘要翻译： 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：US08557992B2

公开(公告)日：2013-10-15

申请号：US13703983

申请日：2011-06-10

申请人： Scott D. Kuduk ,  Jason W. Skudlarek

发明人： Scott D. Kuduk ,  Jason W. Skudlarek

IPC分类号： A61K31/44 ,  C07D221/22

CPC分类号： A61K31/4745 ,  C07D471/04

摘要： The present invention is directed to heterocyclic fused phenanthrolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

摘要翻译： 本发明涉及式（I）的杂环稠合菲咯啉酮化合物，其为M1受体阳性变构调节剂，可用于治疗涉及M1受体的疾病，例如阿尔茨海默病，精神分裂症，疼痛或睡眠障碍 。 本发明还涉及包含该化合物的药物组合物，以及该化合物和组合物在治疗由M1受体介导的疾病中的用途。