951626-95-2Relevant academic research and scientific papers
SUBSTITUTED N-(METHYL-D3)PYRIDAZINE-3-CARBOXAMIDE OR N-(METHYL-D3)-NICOTINAMIDE COMPOUNDS AS IL-12, IL-23 AND/OR IFNALPHA MODULATORS
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Page/Page column 96; 98, (2021/11/06)
There are disclosed compounds of the following formula I or a stereoisomer or pharmaceutically-acceptable salt thereof, wherein all substituents are as defined herein, which are useful in the modulation of IL-12, IL-23 and/or IFN?, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of the invention may be useful for treating inflammatory and autoimmune diseases or disorders.
MACROCYCLIC COMPOUNDS
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Paragraph 0457-0458, (2020/09/27)
Disclosed are macrocyclic compounds of formula (I) comprising a 2-carboxy indole ring. Such compounds, and their pharmaceutically acceptable salts, are useful as Mcl-1 (myeloid cell leukemia-1) inhibitors. The compounds may be used in treating a disease o
FUSED HETEROCYCLIC DERIVATIVES
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Page/Page column 197, (2020/12/11)
The application describes fused heterocycle derivative compounds, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases associated with HBV infection.
Identification and synthesis of novel inhibitors of mycobacterium ATP synthase
Surase, Yogesh B.,Samby, Kirandeep,Amale, Sagar R.,Sood, Ruchi,Purnapatre, Kedar P.,Pareek, Pawan K.,Das, Biswajit,Nanda, Kamna,Kumar, Subodh,Verma, Ashwani K.
supporting information, p. 3454 - 3459 (2017/07/07)
A non-diaryl quinoline scaffold 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one was identified by screening of diverse set of compounds against M. smegmatis ATP synthase. Herein, we disclose our efforts to develop the structure activity relationship against Mycob
SPIROCYCLOHEPTANES AS INHIBITORS OF ROCK
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Page/Page column 239, (2016/02/05)
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia
Conde-Ceide, Susana,Alcázar, Jesús,Alonso De Diego, Sergio A.,López, Silvia,Martín-Martín, María Luz,Martínez-Viturro, Carlos M.,Pena, Miguel-Angel,Tong, Han Min,Lavreysen, Hilde,MacKie, Claire,Bridges, Thomas M.,Daniels, J. Scott,Niswender, Colleen M.,Jones, Carrie K.,MacDonald, Gregor J.,Steckler, Thomas,Conn, P. Jeffrey,Stauffer, Shaun R.,Lindsley, Craig W.,Bartolomé-Nebreda, José Manuel
, p. 429 - 434 (2016/01/09)
As part of our efforts to identify a suitable back-up compound to our recently disclosed mGlu5 positive allosteric modulator (PAM) clinical candidate VU0490551/JNJ-46778212, this letter details the investigation and challenges of a novel series of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives. From these efforts, compound 4k emerged as a potent and selective mGlu5 PAM displaying overall attractive in vitro (pharmacological and ADMET) and PK profiles combined with in vivo efficacy in preclinical models of schizophrenia. However, further advancement of the compound was precluded due to severely limiting CNS-related side-effects confirming the previously reported association between excessive mGlu5 activation and target-related toxicities.
NEGATIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR 3
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Paragraph 0480, (2015/12/30)
Described are negative allosteric modulators of metabotropic glutamate receptor 3 (mGlu3), pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating depression, cognitive disorders, schizophrenia, Alzheimer's disease, or cancer in a subject.
SUBSTITUTED BICYCLIC ARALKYL PYRAZOLE LACTAM ANALOGS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS
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Paragraph 00591, (2014/01/09)
In one aspect, the invention relates to substituted bicyclic aralkyl pyrazole lactam analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
BICYCLIC PYRAZOLE COMPOUNDS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS
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Page/Page column 140, (2012/06/30)
In one aspect, the invention relates to bicyclic pyrazole compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the
BICYCLIC TRIAZOLE AND PYRAZOLE LACTAMS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS
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Page/Page column 266, (2012/06/30)
In one aspect, the invention relates to bicyclic triazole and pyrazole lactams, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for
