4600-86-6Relevant academic research and scientific papers
PYRAZOLO[3,4-b]PYRIDINE AND PYRROLO[2,3-b]PYRIDINE INHIBITORS OF BRUTON'S TYROSINE KINASE
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, (2018/07/31)
Disclosed are pyrazolo[3,4-b]pyridine and pyrrolo[2,3-b]pyridine inhibitors of Bruton's tyrosine kinase (Btk). Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are described, alone or in combin
SUBSTITUTED BICYCLIC CARBOXAMIDE AND UREA DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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, (2012/05/31)
The invention relates to substituted bicyclic carboxamide and urea derivatives, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.
Preparation, physical properties and n-type FET characteristics of substituted diindenopyrazinediones and bis(dicyanomethylene) derivatives
Nishida, Jun-Ichi,Deno, Hironori,Ichimura, Satoru,Nakagawa, Tomohiro,Yamashita, Yoshiro
, p. 4483 - 4490 (2012/07/28)
A series of halogen and alkyl substituted diindenopyrazinediones and bis(dicyanomethylene) derivatives have been synthesized as new n-type organic semiconductors based on nitrogen-containing heterocycles. Halogen groups were introduced to improve the electron injection. Their crystal structures and solid physical properties are discussed. Alkyl groups were introduced to increase the solubility in organic solvents. Furthermore, hexanoyl groups were introduced by oxidation of alkyl groups to increase the solubility and electron affinity. Dicyanomethylene groups were also introduced to further enhance the electron-accepting properties. Drop-cast as well as vapour deposited thin films showed n-type FET properties.
SEROTONIN RECEPTOR MODULATORS
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Page/Page column 125, (2010/07/10)
The biphenyic compounds of formula (I) are serotonin modulators useful in the treatment of serotonin-mediated diseases.
INHIBITORS OF BURTON'S TYROSINE KINASE
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Page/Page column 73, (2010/02/16)
This application discloses 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-V: wherein, variables Q, R, Y1, Y2, Y2′, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.
Inhibitors of Bruton's Tyrosine Kinase
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Page/Page column 99-101, (2010/09/07)
This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-Phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-III: wherein, variables Q, R, X, X′, Y1, Y2, Y2′, Y3, Y4, Y5, m, and n are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-III and at least one carrier, diluent or excipient.
NOVEL PYRIDINONES AND PYRIDAZINONES
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Page/Page column 77-78, (2009/10/09)
This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one deriva-tives according to generic Formulae I-III : wherein, variables R, X, Y1, Y2, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat in-flammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-III and at least one carrier, diluent or excipient.
Identification of (R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H- indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management
Gomtsyan, Arthur,Bayburt, Erol K.,Schmidt, Robert G.,Surowy, Carol S.,Honore, Prisca,Marsh, Kennan C.,Hannick, Steven M.,McDonald, Heath A.,Wetter, Jill M.,Sullivan, James P.,Jarvis, Michael F.,Faltynek, Connie R.,Lee, Chih-Hung
, p. 392 - 395 (2008/09/17)
Vanilloid receptor TRPV1 is a cation channel that can be activated by a wide range of noxious stimuli, including capsaicin, acid, and heat. Blockade of TRPV1 activation by selective antagonists is under investigation by several pharmaceutical companies in an effort to identify novel agents for pain management. Here we report that replacement of substituted benzyl groups by an indan rigid moiety in a previously described N-indazole-N′-benzyl urea series led to a number of TRPV1 antagonists with significantly increased in vitro potency and enhanced drug-like properties. Extensive evaluation of pharmacological, pharmacokinetic, and toxicological properties of synthesized analogs resulted in identification of (R)-7 (ABT-102). Both the analgesic activity and drug-like properties of (R)-7 support its advancement into clinical pain trials.
Development of a large scale asymmetric synthesis of vanilloid receptor (TRPV1) antagonist ABT-102
Lukin, Kirill,Hsu, Margaret C.,Chambournier, Gilles,Kotecki, Brian,Venkatramani,Leanna
, p. 578 - 584 (2012/12/31)
A highly efficient asymmetric synthesis of TRPV1 antagonist ABT-102 was developed and successfully demonstrated on a multi-kilogram scale. This process incorporates a new asymmetric synthesis of (R)-tert-butylaminoindan, which is based on a chiral auxiliary induced diastereoselective reduction of its iminoindan precursor.
Prodrugs of compounds that inhibit TRPV1 receptor
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Page/Page column 28, (2010/11/27)
Compounds of formula (I) wherein A, R1, R2, and R3 are defined in the specification, and which are useful as therapeutic compounds particularly for treating disorders or conditions associated with inflammation, pain, bladd
