343788-67-0Relevant academic research and scientific papers
OXYMETHYLENE ARYL COMPOUNDS FOR TREATING INFLAMMATORY GASTROINTESTINAL DISEASES OR GASTROINTESTINAL CONDITIONS
-
, (2018/03/28)
Use of oxymethylene aryl GPRl 19 agonists, and optionally DPP IV inhibitors and optionally metformin, for the treatment of inflammatory gastrointestinal diseases or gastrointestinal conditions involving malabsorption of nutrients and/or fluids are provide
INDUCTION OF GATA2 BY HDAC1 AND HDAC2 INHIBITORS
-
, (2016/05/02)
Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with Gata2 deficiency, particularly diseases or disorders that involve any type of HDAC1 and/or HDAC2 expression. Such diseases include acute myeloid leukemia (AML); familial myelodysplastic syndrome (MDS); leukemia; sickle-cell anemia; beta-thalassemia; monocytopenia and mycobacterial infections; dendritic cell, nonocyte, B, and natural killer lymphoid deficiency; Emberger syndrome; asymptomatic neurocognitive impairment; mild neurocognitive disorder; and HIV- associated dementia.
PIPERIDINE DERIVATIVES AS HDAC1/2 INHIBITORS
-
, (2016/06/28)
Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDACl and/or HDAC2 activity.
PYRIMIDINE HYDROXY AMIDE COMPOUNDS AS HISTONE DEACETYLASE INHIBITORS
-
, (2015/04/21)
Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1, HDAC2, and/or HDAC6. Also provided herein are methods for inhibiting migration of a neuroblastoma cell, inducing maturation of a neuroblastoma cell, and altering cell cycle progression of a neuroblastoma cell comprising administering to the cell a therapeutically effective amount of a HDAC1, HDAC2, and/or HDAC6 selective inhibitor or a pharmaceutically acceptable salt thereof.
SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF
-
Page/Page column 26, (2012/07/13)
This invention provides compounds of formula (I): wherein R1, R2, X, p, q, m, n, and Ring C have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
2′ Biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR
Budzik, Brian,Garzya, Vincenzo,Shi, Dongchuan,Foley, James J.,Rivero, Ralph A.,Langmead, Christopher J.,Watson, Jeannette,Wu, Zining,Forbes, Ian T.,Jin, Jian
scheme or table, p. 3540 - 3544 (2010/08/22)
Biaryl amides were discovered as novel and subtype selective M1 muscarinic acetylcholine receptor agonists. The identification, synthesis, and initial structure-activity relationships that led to compounds 3j and 4c, possessing good M1 agonist potency and intrinsic activity, and subtype selectivity for M1 over M2-5, are described.
Development of a scalable synthesis of dipeptidyl peptidase-4 inhibitor ABT-279
McDermott, Todd S.,Bhagavatula, Lakshmi,Borchardt, Thomas B.,Engstrom, Kenneth M.,Gandarilla, Jorge,Kotecki, Brian J.,Kruger, Albert W.,Rozema, Michael J.,Sheikh, Ahmad Y.,Wagaw, Seble H.,Wittenberger, Steven J.
experimental part, p. 1145 - 1155 (2010/04/22)
A convergent, scalable synthesis of dipeptidyl peptidase-4 inhibitor, ABT-279, has been developed and demonstrated on multikilogram scale. The cis-2,5-disubstituted pyrrolidine is generated by cyclization of a Boc-amine onto an alkynyl ketone followed by stereospecific reduction of the resulting acyliminium intermediate. The amine coupling partner was prepared by a novel Hofmann rearrangement promoted by 1,3-dibromo-5,5-dimethylhydantoin. The final product was isolated as the L-malic acid salt. The scaleup campaign consisted of 15 steps and delivered 42 kg of ABT-279 in 14% overall yield. A second-generation synthesis that addresses some of the issues encountered during scale-up was developed and demonstrated on kilogram scale.
UREIDE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES
-
Page/Page column 90, (2009/01/24)
This invention relates to a pharmaceutical comprising, as an active ingredient, a ureide derivative represented by formula: or a pharmaceutically acceptable salt thereof. The ureide derivative or a pharmaceutically acceptable salt thereof according to the present invention is useful for relieving pain and treating or preventing neuropathic pain.
HETEROCYCLIC RECEPTOR AGONISTS FOR THE TREATMENT OF DIABETES AND METABOLIC DISORDERS
-
Page/Page column 97, (2008/12/07)
Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control. The compounds of the invention are orally active.
SYNTHESIS OF (2S,5R)-5-ETHYNYL-1-{N-(4-METHYL-1-(4-CARBOXY-PYRIDIN-2-YL)PIPERIDIN-4-YL)GLYCYL}PYRROLIDINE-2-CARBONITRILE
-
Page/Page column 40, (2008/06/13)
A process for making (2S,5R)-5-ethynyl-1-{N-(4-methyl-1-(4-carboxy-pyridin-2-yl)piperidin-4-yl)glycyl}pyrrolidine-2-carbonitrile and salts thereof, and intermediates used in the process are disclosed.
