Novartis Ag

Yale University

Tejaskumar Pankajbhai Pathak

James Neef

Amir Masoud Sadaghiani

Xilin Zhou

Zaixing Li

Chui Lu

Danuta Lubicka

Hye-Yeon Park

Sung David C Kim

Scott J Miller

Thomas Charles Caya

The present disclosure provides for a compound according to formula (I)

Methyl (R)-2-(fluoromethyl)-5-oxo-4-phenyl-4,5,6,7-tetrahydro-1H-cyclopenta[B]pyridine-3-carboxylate and methyl 2-(fluoromethyl)-5-oxo-4-phenyl-1,4,5,7-tetrahydrofuro[3,4-b]pyrodine-3-carboxylate as Ca1.2 activators

The present disclosure provides for a compound according to formula (I) or a pharmaceutically acceptable salt thereof as Ca1.22 activators for the treatment of schizophrenia, bipolar disorder, major depressive disorder, substance use disorder, ADHD, Phelan-McDermid Syndrome, autism spectrum disorder, multiple sclerosis, frontotemporal dementia, Alzheimer's disease, Brugada Syndrome, Short QT syndrome, or early repolarization syndrome.

Methyl (r)-2-(fluoromethyl)-5-oxo-4-phenyl-4,5,6,7-tetrahydro-1H-cyclopenta[b]pyridine-3-carboxylate and methyl (r)-2-(fluoromethyl)-5-oxo-4-phenyl-1,4,5,7-tetrahydrofuro[3,4-b]pyridine-3-carboxylate as CAV1.2 activators

The present disclosure provides for a compound according to formula (I) or a pharmaceutically acceptable salt thereof as Cav1.2 activators for the treatment of schizophrenia, bipolar disorder, major depressive disorder, substance use disorder, ADHD, Phelan-McDermid Syndrome, autism spectrum disorder, multiple sclerosis, frontotemporal dementia, Alzheimer's disease, Brugada Syndrome, Short QT syndrome, and early repolarization syndrome.

Methyl 2-methyl-5-oxo-1,4,5,7-tetradhydrofuro[3,4-b]pyridine-3-carboxylate compounds as Ca1.2 activators

Site-selective functionalized glycopeptide antibiotics, methods of making and using are described herein. The compounds exhibit improved activity against methicillin-susceptible(MSSA), methicillin-resistant(MRSA), vancomycin-sensitive(VSE), vancomycin-resistant enterococci (VRE), or combinations thereof. The compounds can be administered as the neutral free acid or free base or can be administered as a pharmaceutically acceptable acid-addition or base-addition salt. The compounds can be formulated with one or more pharmaceutically acceptable excipients to prepare pharmaceutical compositions. The compounds can be administered by a variety of routes of administration including enteral, parenteral, topical, or transmucosal.

Site-selective functionalization of glycopeptide antibiotics

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Boston, MA, United States of America

Tejaskumar Pankajbhai Pathak