Patent classifications
C07D215/18
Modulators of potassium ion and TRPV1 channels and uses thereof
Novel compounds usable in modulating an activity or function of a voltage-dependent potassium channel and/or of TRPV1 are provided. The compounds are represented by Formula I as described and defined in the specification.
METAL OXIDE CATALYZED RADIOFLUORINATION
Inter alia, the first titania-catalyzed [.sup.18F]-radiofluorination in highly aqueous medium is provided. In embodiments, the method utilizes titanium dioxide, 1:1 acetonitrile-thexyl alcohol solvent mixture and tetrabutylammonium bicarbonate as a base. Radiolabeling may be directly performed with aqueous [.sup.18F]fluoride without the need for drying/azeotroping step, which reduces radiosynthesis time while keeping high fluoride conversion. The general applicability of the synthetic strategy to the synthesis of the wide range of PET probes from tosylated precursors is demonstrated.
SUBSTITUTED QUINOLINYLCYCLOHEXYLPROPANAMIDE COMPOUNDS AND IMPROVED METHODS FOR THEIR PREPARATION
- Albert J. DELMONTE ,
- Benjamin M. COHEN ,
- Kenneth Joseph FRAUNHOFFER ,
- Sergei KOLOTUCHIN ,
- Francisco GONZALEZ-BOBES ,
- Gregory Louis BEUTNER ,
- Adam Joseph FREITAG ,
- Michael Scott BULTMAN ,
- Yu Fan ,
- Prantik MAITY ,
- Ian Scott YOUNG ,
- Hilary Plake Beck ,
- Maksim Osipov ,
- Jay Patrick Powers ,
- Maureen Kay Reilly ,
- Hunter Paul Shunatona ,
- James Ross Walker ,
- Mikhail Zibinsky
The disclosure is directed to improved methods for preparing substituted quinolinylcyclohexylpropanamide compounds.
SUBSTITUTED QUINOLINYLCYCLOHEXYLPROPANAMIDE COMPOUNDS AND IMPROVED METHODS FOR THEIR PREPARATION
- Albert J. DELMONTE ,
- Benjamin M. COHEN ,
- Kenneth Joseph FRAUNHOFFER ,
- Sergei KOLOTUCHIN ,
- Francisco GONZALEZ-BOBES ,
- Gregory Louis BEUTNER ,
- Adam Joseph FREITAG ,
- Michael Scott BULTMAN ,
- Yu Fan ,
- Prantik MAITY ,
- Ian Scott YOUNG ,
- Hilary Plake Beck ,
- Maksim Osipov ,
- Jay Patrick Powers ,
- Maureen Kay Reilly ,
- Hunter Paul Shunatona ,
- James Ross Walker ,
- Mikhail Zibinsky
The disclosure is directed to improved methods for preparing substituted quinolinylcyclohexylpropanamide compounds.
Substituted quinolinylcyclohexylpropanamide compounds and improved methods for their preparation
- Albert J. DELMONTE ,
- Benjamin M. COHEN ,
- Kenneth Joseph FRAUNHOFFER ,
- Sergei KOLOTUCHIN ,
- Francisco GONZALEZ-BOBES ,
- Gregory Louis BEUTNER ,
- Adam Joseph FREITAG ,
- Michael Scott BULTMAN ,
- Yu Fan ,
- Prantik MAITY ,
- Ian Scott YOUNG ,
- Hilary Plake Beck ,
- Maksim Osipov ,
- Jay Patrick Powers ,
- Maureen Kay Reilly ,
- Hunter Paul Shunatona ,
- James Ross Walker ,
- Mikhail Zibinsky
The disclosure is directed to improved methods for preparing substituted quinolinylcyclohexylpropanamide compounds.
Substituted quinolinylcyclohexylpropanamide compounds and improved methods for their preparation
- Albert J. DELMONTE ,
- Benjamin M. COHEN ,
- Kenneth Joseph FRAUNHOFFER ,
- Sergei KOLOTUCHIN ,
- Francisco GONZALEZ-BOBES ,
- Gregory Louis BEUTNER ,
- Adam Joseph FREITAG ,
- Michael Scott BULTMAN ,
- Yu Fan ,
- Prantik MAITY ,
- Ian Scott YOUNG ,
- Hilary Plake Beck ,
- Maksim Osipov ,
- Jay Patrick Powers ,
- Maureen Kay Reilly ,
- Hunter Paul Shunatona ,
- James Ross Walker ,
- Mikhail Zibinsky
The disclosure is directed to improved methods for preparing substituted quinolinylcyclohexylpropanamide compounds.
Amorphous and crystalline forms of IDO inhibitors
The present disclosure relates to amorphous and crystalline forms of (R)-N-(4-chlorophenyl)-2-((1S,4S)-4-(6-fluoro-quinolin-4-yl) cyclohexyl)propanamide and its salts and hydrates, processes for their production, pharmaceutical compositions comprising them, and methods of treatment using them.
Amorphous and crystalline forms of IDO inhibitors
The present disclosure relates to amorphous and crystalline forms of (R)-N-(4-chlorophenyl)-2-((1S,4S)-4-(6-fluoro-quinolin-4-yl) cyclohexyl)propanamide and its salts and hydrates, processes for their production, pharmaceutical compositions comprising them, and methods of treatment using them.
Polymorphs of 4-[3-chloro-4-(n′-cyclopropyl ureido)phenoxy] -7-methoxyquinoline-6-carboxamide, its salts and process for the preparation thereof
The present invention relates to novel polymorphs of 4-[3-chloro-4-(N′-cyclopropyl ureido) phenoxy]-7-methoxyquinoline-6-carboxamide methanesulfonate represented by following structural formula-1a and process for preparation thereof. ##STR00001## Further, the present invention relates to an improved process for the preparation of 4-[3-chloro-4-(N′-cyclopropylureido) phenoxy]-7-methoxyquinoline-6-carboxamide compound of formula-1 or its salts and its intermediates thereof.
Histone deacetylase inhibitors and compositions and methods of use thereof
Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use. ##STR00001##