288086-98-6Relevant academic research and scientific papers
COMPOUNDS TARGETING RNA-BINDING PROTEINS OR RNA-MODIFYING PROTEINS
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Page/Page column 72, (2021/09/11)
The invention relates to a compound represented by Formula (I): or a pharmaceutically acceptable salt thereof, compositions comprising the same and methods of preparing and using the same. The variables are described herein.
Synthesis of novel phase transfer catalysts derived from proline-mandelic acid/tartaric acid: their evaluation in enantioselective epoxidation and Darzen condensation
Mahajan, Deepak P,Godbole, Himanshu M,Singh, Girij P,Shenoy, Gautham G
, (2019/02/27)
Abstract : Herein, we have described the synthesis of novel chiral cyclic phase transfer catalysts (PTCs). These catalysts are synthesized from proline, mandelic acid and tartaric acid by using simple synthetic methods with competitive yields. These chira
Development of Dual Chitinase Inhibitors as Potential New Treatment for Respiratory System Diseases
Mazur, Marzena,Dymek, Barbara,Koralewski, Robert,Sklepkiewicz, Piotr,Olejniczak, Sylwia,Mazurkiewicz, Marcin,Piotrowicz, Micha?,Salamon, Magdalena,J?drzejczak, Karol,Zagozdzon, Agnieszka,Czestkowski, Wojciech,Matyszewski, Krzysztof,Borek, Bart?omiej,Bartoszewicz, Agnieszka,Pluta, Elzbieta,Rymaszewska, Aleksandra,Mozga, Witold,Stefaniak, Filip,Dobrzański, Pawe?,Dzwonek, Karolina,Golab, Jakub,Golebiowski, Adam,Olczak, Jacek
, p. 7126 - 7145 (2019/08/30)
Acidic mammalian chitinase (AMCase) and chitotriosidase-1 (CHIT1) are two enzymatically active proteins produced by mammals capable of cleaving the glycosidic bond in chitin. Based on the clinical findings and animal model studies, involvement of chitinases has been suggested in several respiratory system diseases including asthma, COPD, and idiopathic pulmonary fibrosis. Exploration of structure-activity relationships within the series of 1-(3-amino-1H-1,2,4-triazol-5-yl)-piperidin-4-amines, which was earlier identified as a scaffold of potent AMCase inhibitors, led us to discover highly active dual (i.e., AMCase and CHIT1) inhibitors with very good pharmacokinetic properties. Among them, compound 30 was shown to reduce the total number of cells in bronchoalveolar lavage fluid of mice challenged with house dust mite extract after oral administration (50 mg/kg, qd). In addition, affinity toward the hERG potassium channel of compound 30 was significantly reduced when compared to the earlier reported chitinase inhibitors.
PROCESS FOR THE PREPARATION OF CHIRAL PYROLLIDINE-2-YL- METHANOL DERIVATIVES
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Page/Page column 17-18, (2018/09/26)
The invention relates to a novel process for the preparation of a chiral pyrollidine-2-yl-methanol derivative or a salt thereof of the formula (I), wherein R1 is aryl or heteroaryl and both aryl or heteroaryl are optionally substituted by C1-4-alkyl, halo-C1-4-alkyl, C1-4-alkoxy or halogen. The synthesis proceeds through an intermediate Weinreb amide, which is reacted with a Grignard reagent and hydrogenated. The chiral pyrollidine-2-yl-methanol derivatives of the formula (I) are versatile building blocks in the synthesis of pharmacologically active compounds, such as for the stereospecific synthesis of oligonucleotides carrying chiral phosphonate moieties.
SUBSTITUTED AMINO TRIAZOLES USEFUL AS HUMAN CHITINASE INHIBITORS
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, (2017/03/21)
Disclosed are amino triazole compounds substituted with a piperidinyl ring that is itself substituted with a heterocyclic ring. These compounds are inhibitors of acidic mammalian chitinase and chitotriosidase. Also disclosed are methods of using the compounds to treat asthma reactions caused by allergens, as well as acute and chronic inflammatory diseases, autoimmune diseases, dental diseases, neurologic diseases, metabolic diseases, liver diseases, polycystic ovary syndrome, endometriosis, and cancer.
MUSCARINIC AGONISTS
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Page/Page column 48; 49, (2017/02/28)
This invention relates to compounds that are agonists of the muscarinic M4 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1a or a salt thereof, wherein n, p, Q, R1, R2, R3, R9 and R4 are as defined herein.
SERINE/THREONINE KINASE INHIBITORS
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Paragraph 00309, (2013/09/12)
Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
QUINAZOLINE COMPOUNDS AS SERINE/THREONINE KINASE INHIBITORS
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Paragraph 00198, (2013/03/26)
Compounds having the formula (I) wherein R1, R2, R3 and Ar as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
SERINE/THREONINE KINASE INHIBITORS
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Page/Page column 138, (2012/09/21)
Compounds having the formula I wherein Z, Z1 Z2 Z3, R3a, R3b and Rb and as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperprolife
MODULATORS OF G PROTEIN-COUPLED RECEPTOR 88
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Page/Page column 66, (2011/04/26)
The present disclosure is generally directed to compounds which can modulate G-protein coupled receptor 88, compositions comprising such compounds, and methods for modulating G-protein coupled receptor 88.
