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：US20240051963A1

公开(公告)日：2024-02-15

申请号：US18256980

申请日：2021-12-09

申请人： Andrew J. Cooke, JR. ,  Jeffrey W. Schubert ,  Jason W. Skudlarek ,  Merck Sharp & Dohme LLC.

发明人： Andrew J. Cooke, JR. ,  Jeffrey W. Schubert ,  Jason W. Skudlarek

IPC分类号： C07D487/04 ,  A61K31/517 ,  A61P31/22

CPC分类号： C07D487/04 ,  A61K31/517 ,  A61P31/22

摘要： The present invention relates to novel Fused [7,5] Bicyclic Pyrazole Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, and R4 are as defined herein. The present invention also relates to compositions comprising at least one Fused [7,5] Bicyclic Pyrazole Derivative, and methods of using the Fused [7,5] Bicyclic Pyrazole Derivatives for treating or preventing a herpesvirus infection in a patient.

公开(公告)号：US20240083910A1

公开(公告)日：2024-03-14

申请号：US18257003

申请日：2021-12-14

申请人： Richard BERGER ,  Christopher Douglas COX ,  Brendan M. CROWLEY ,  Marc LABROLI ,  Michael Aaron PLOTKIN ,  Izzat Tiedje RAHEEM ,  Deyou SHA ,  Anthony SHAW ,  Jason W. SKUDLAREK ,  Ling TONG ,  Merck Sharp & Dohme LLC

发明人： Richard Thaddeus Berger, JR. ,  Christopher Douglas Cox ,  Brendan M. Crowley ,  Marc Labroli ,  Michael Aaron Plotkin ,  Izzat Tiedje Raheem ,  Deyou Sha ,  Anthony W. Shaw ,  Jason W. Skudlarek ,  Ling Tong

IPC分类号： C07D498/04 ,  A61K31/444 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61P31/22 ,  C07D401/14 ,  C07D519/00

CPC分类号： C07D498/04 ,  A61K31/444 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61P31/22 ,  C07D401/14 ,  C07D519/00

摘要： The present invention relates to novel Amido-Substituted Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are as defined herein. The present invention also relates to compositions comprising at least one Amido-Substituted Heterocycle Compounds for treating or preventing a herpesvirus infection in a patient.

公开(公告)号：US20240067657A1

公开(公告)日：2024-02-29

申请号：US18258903

申请日：2021-12-21

申请人： 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

发明人： 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分类号： C07D498/04 ,  A61K31/517 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D519/00

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

摘要： 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：US11919894B2

公开(公告)日：2024-03-05

申请号：US17695125

申请日：2022-03-15

申请人： Merck Sharp & Dohme LLC

发明人： Sachin Mittal ,  Jason W. Skudlarek ,  Izzat T. Raheem

IPC分类号： C07D417/14

CPC分类号： C07D417/14

摘要： The present invention is directed to pro drugs of 2-methyl-N-((5-methyl-1,3,4-thiadiazol-2-yl)methyl)-6-(((1S,2S)-2-(5-methylpyridin-2-yl)cyclopropyl)methoxy)pyrimidin-4-amine which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

公开(公告)号：US20240059693A1

公开(公告)日：2024-02-22

申请号：US18256997

申请日：2021-12-14

申请人： Merck Sharp & Dohme LLC

发明人： Ronald K. Chang ,  Andrew J. Cooke, JR. ,  Christopher Douglas Cox ,  Marc Labroli ,  Izzat Tiedje Raheem ,  Jack D. Scott ,  Jeffrey W. Schubert ,  Jason W. Skudlarek ,  Zheng Tan ,  Ling Tong

IPC分类号： C07D487/04 ,  C07D519/00 ,  C07D403/14 ,  C07D403/06 ,  C07D413/14 ,  A61K31/517 ,  A61P31/22

CPC分类号： C07D487/04 ,  C07D519/00 ,  C07D403/14 ,  C07D403/06 ,  C07D413/14 ,  A61K31/517 ,  A61P31/22

摘要： The present invention relates to novel Fused Bicyclic Pyrazole Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, and R6 are as defined herein. The present invention also relates to compositions comprising at least one Fused Bicyclic Pyrazole Derivative, and methods of using the Fused Bicyclic Pyrazole Derivatives for treating or preventing a herpesvirus infection in a patient.

公开(公告)号：US20230118665A1

公开(公告)日：2023-04-20

申请号：US17820417

申请日：2022-08-17

申请人： Merck Sharp & Dohme LLC

发明人： Andrew Bett ,  Izzat T. Raheem ,  Jason W. Skudlarek ,  Erica L. Strable

IPC分类号： A61K9/51 ,  A61K39/39 ,  A61K39/12 ,  A61P31/20 ,  A61P37/04 ,  C12N7/00 ,  C08G65/333

摘要： The present disclosure provides, among other things, a lipid nanoparticle adjuvant composition. The present disclosure provides pharmaceutical compositions that include a stable lipid nanoparticle adjuvant and human papillomavirus (HPV) virus-like particles (VLPs) of at least one type of human papillomavirus (HPV) selected from the group consisting of HPV types: 6, 11, 16, 18, 26, 31, 33, 35, 39, 45, 51, 52, 53, 55, 56, 58, 59, 66, 68, 73, and 82.

公开(公告)号：US20240158388A1

公开(公告)日：2024-05-16

申请号：US18538309

申请日：2023-12-13

申请人： Merck Sharp & Dohme LLC

发明人： Sachin Mittal ,  Jason W. Skudlarek ,  Izzat T. Raheem

IPC分类号： C07D417/14

CPC分类号： C07D417/14

摘要： The present invention is directed to pro drugs of 2-methyl-N-((5-methyl-1,3,4-thiadiazol-2-yl)methyl)-6-(((1S,2S)-2-(5-methylpyridin-2-yl)cyclopropyl)methoxy)pyrimidin-4-amine which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

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：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。