- Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M4 positive allosteric modulator (PAM) chemotype
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This Letter details our efforts to discover structurally unique M4 PAMs containing 5,6-heteroaryl ring systems. In an attempt to improve the DMPK profiles of the 2,3-dimethyl-2H-indazole-5-carboxamide and 1-methyl-1H-benzo[d][1,2,3]triazole-6-carboxamide cores, we investigated a plethora of core replacements. This exercise identified a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide core that provided improved M4 PAM activity and CNS penetration.
- Temple, Kayla J.,Engers, Julie L.,Long, Madeline F.,Watson, Katherine J.,Chang, Sichen,Luscombe, Vincent B.,Jenkins, Matthew T.,Rodriguez, Alice L.,Niswender, Colleen M.,Bridges, Thomas M.,Conn, P. Jeffrey,Engers, Darren W.,Lindsley, Craig W.
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- Catalytic Aerobic Photo-oxidation of a Methyl Group on a Heterocycle to Produce an Aldehyde via Homolytic C-I Bond Cleavage caused by Irradiation with Visible Light
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A new catalytic method was developed for photo-oxidizing the methyl group on aromatic heterocycles such as benzothiazole, benzoxazole, and quinoline to produce the corresponding aldehyde. This is the first report of the metal-free catalytic synthesis of benzothiazole-2-carboxaldehydes using molecular oxygen as the terminal oxidant.
- Nagasawa,Tachikawa,Yamaguchi,Tada,Miura,Itoh
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supporting information
p. 178 - 182
(2016/02/14)
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- PYRAZOLOPYRIDINE PYRAZOLOPYRIMIDINE AND RELATED COMPOUNDS
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In one aspect this invention relates generally to compounds of Formula: and sub-formulas thereof, or a tautomer of each thereof, a pharmaceutically acceptable salt of each thereof, or a pharmaceutically acceptable solvate of each of the foregoing, where X1, L1, L3, and R3 are described herein.
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Paragraph 1240; 1241
(2015/11/25)
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- INFRARED DYE FOR SILVER HALIDE-BASED PHOTOGRAPHIC ELEMENTS
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A non-infrared sensitized low silver photographic element with a non-light sensitive layer, preferably an antihalation layer, containing a diphenylaminocyclopentene heptacyanine benzothiazolium infrared dye where the benzothiazolium groups have electron-withdrawing substituents on the phenyl ring and solubilzed alkyl groups on the nitrogen. The infrared dye can be present as a liquid-crystalline dispersion. This class of infrared dyes form J-aggregrated species in a liquid-crystalline or a solid particle dispersion with high IR density and low visible absorbance.
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Page/Page column 16
(2009/09/28)
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- INFRARED DYE FOR SILVER HALIDE-BASED PHOTOGRAPHIC ELEMENTS
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A non-infrared sensitized low silver photographic element with a non-light sensitive layer, preferably an antihalation layer, containing a diphenylaminocyclopentene heptacyanine benzothiazolium infrared dye where the benzothiazolium groups have electron-withdrawing substituents on the phenyl ring and solubilzed alkyl groups on the nitrogen. The infrared dye can be present as a liquid-crystalline dispersion. This class of infrared dyes form J-aggregated species in a liquid-crystalline or a solid particle dispersion with high IR density and low visible absorbance.
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- NOVEL BENSOPHENONE DERIVATIVES OR SALTS THEREOF
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A benzophenone derivative represented by the following formula: whereinR1 represents, for example, an optionally substituted heterocyclic group, or a substituted phenyl group; Z represents, for example, an alkylene group; R2 represents, for example, a carboxyl group optionally protected with alkyl;R3 represents, for example, an optionally protected hydroxyl group; R4 represents, for example, an optionally substituted cycloalkyloxy group; and R5 represents, for example, a hydrogen atom, ???or a salt thereof has anti-arthritic activity, inhibits bone destruction caused by arthritis, and provides high safety and excellent pharmacokinetics and thus is useful as therapeutic agent for arthritis. These compounds have inhibitory effect on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression of AP-1 is involved.
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- Synthesis of a new spiropyran based on [60]fullerene unit
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A new compound 2: spiropyran with [60]fullerene unit was synthesized and characterized by FT-IR, MALDI-TOF MS, NMR, and UV-Vis spectra.
- Xu, Ju-Hua,Li, Yu-Liang,Zhu, Dao-Ben
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p. 1647 - 1652
(2007/10/03)
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