97628-92-7Relevant academic research and scientific papers
COMPOUNDS, COMPOSITIONS AND METHODS
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, (2019/02/25)
The present disclosure relates generally to eukaryotic initiation factor 2B modulators, or a pharmaceutically acceptable salt, stereoisomer, mixture of stereoisomers or prodrug thereof, and methods of making and using thereof.
NOVEL COMPOUNDS
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Page/Page column 24, (2019/03/05)
The invention relates to compounds of Formula (I) and their use in therapy, for example in the treatment of mycobacterial infections or in the treatment of diseases caused by mycobacterium, such as tuberculosis
Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series
Watterson, Scott H.,Guo, Junqing,Spergel, Steve H.,Langevine, Charles M.,Moquin, Robert V.,Shen, Ding Ren,Yarde, Melissa,Cvijic, Mary Ellen,Banas, Dana,Liu, Richard,Suchard, Suzanne J.,Gillooly, Kathleen,Taylor, Tracy,Rex-Rabe, Sandra,Shuster, David J.,McIntyre, Kim W.,Cornelius, Georgia,D'Arienzo, Celia,Marino, Anthony,Balimane, Praveen,Warrack, Bethanne,Salter-Cid, Luisa,McKinnon, Murray,Barrish, Joel C.,Carter, Percy H.,Pitts, William J.,Xie, Jenny,Dyckman, Alaric J.
, p. 2820 - 2840 (2016/04/10)
Sphingosine 1-phosphate (S1P) is the endogenous ligand for the sphingosine 1-phosphate receptors (S1P1-5) and evokes a variety of cellular responses through their stimulation. The interaction of S1P with the S1P receptors plays a fundamental physiological role in a number of processes including vascular development and stabilization, lymphocyte migration, and proliferation. Agonism of S1P1, in particular, has been shown to play a significant role in lymphocyte trafficking from the thymus and secondary lymphoid organs, resulting in immunosuppression. This article will detail the discovery and SAR of a potent and selective series of isoxazole based full agonists of S1P1. Isoxazole 6d demonstrated impressive efficacy when administered orally in a rat model of arthritis and in a mouse experimental autoimmune encephalomyelitis (EAE) model of multiple sclerosis.
1,3-SUBSTITUTED AZETIDINE PDE10 INHIBITORS
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Paragraph 0075; 0076, (2016/09/12)
The present invention is directed to substituted azetidine compounds 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.
SECONDARY ALCOHOL SUBSITUTED TRIAZOLES AS PDE10 INHIBITORS
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Page/Page column 30; 31, (2014/06/11)
The present invention is directed to secondary alcohol substituted triazole compounds 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.
1,3-SUBSTITUTED AZETIDINE PDE10 INHIBITORS
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Paragraph 38; 39, (2013/04/24)
The present invention is directed to substituted azetidinecompounds 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.
SUBSTITUTED 3-PHENYL-1,2,4-OXADIAZOLE COMPOUNDS
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Page/Page column 44-45, (2012/02/05)
Disclosed are compounds of Formula (I): (I) or stereoisomers, salts, or prodrugs thereof, wherein: (i) R1 and R2 are independently C1-C4 alkyl, or (ii) R1 and R2 together with the carbon atom to which they are a
SPHINGOSINE-1-PHOSPHATE RECEPTOR AGONISTS
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Page/Page column 125-126, (2011/02/24)
Disclosed are compounds of Formula (I), or a stereoisomer or a pharmaceutically acceptable salt thereof, wherein: A is formula (II) Q is a substituted 5-membered monocyclic heteroaryl group; W is CH2, O, or NH; and R1, R2, R3, R4, R5, R6, m, n, t, and x are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
TRICYCLIC HETEROCYCLIC COMPOUNDS
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Page/Page column 86-87, (2011/06/16)
Disclosed are compounds of Formula (I) or stereoisomers or salts thereof, wherein: X1, X2, X3, W, Q1, Q2, and G2 are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
8-METHYL-1-PHENYL-IMIDAZOL[1,5-A]PYRAZINE COMPOUNDS
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Page/Page column 69, (2011/09/14)
The present invention provides 8-methyl-1 -phenyl-imidazo[1,5-a]pyrazine derivatives according to formula I or pharmaceutically acceptable salts thereof. The compounds of the current invention show inhibitory activity against Lck and can be used for the treatment of Lck-mediated diseases or Lck-mediated conditions such as inflammatory disorders.
