- PARG INHIBITORS AND METHOD OF USE THEREOF
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Provided herein are, inter alia, methods of treating cancer using compounds of the invention.
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Paragraph 0601; 0602; 0603
(2020/02/16)
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- NOVEL TETRAZOLE COMPOUNDS AND THEIR USE IN THE TREATMENT OF TUBERCULOSIS
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The invention relates to a compound of Formula (I) or a pharmaceutically acceptable salt thereof and their use in therapy, for example in the treatment of mycobacterial infections or in the treatment of diseases caused by mycobacterium, such as tuberculosis.
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Page/Page column 35
(2019/03/05)
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- 1-(DIHYDRONAPHTHALENYL)PYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS
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This invention relates to novel 1-(dihydronaphthalenyl)pyridones which are antagonists of the melanin-concentrating hormone receptor 1 (MCHR1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy
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Page/Page column 47
(2013/12/03)
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- FAAH INHIBITORS
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The present disclosure relates to compounds useful as inhibitors of the enzyme Fatty Acid Amide Hydrolase (FAAH). The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the com
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Page/Page column 152-153
(2012/07/13)
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- BIS-PYRIDYLPYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS
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The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1 ), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and diabetes.
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Page/Page column 18
(2010/12/29)
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- BIS-PYRIDYLPYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS
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The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1 ), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and diabetes.
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Page/Page column 18
(2010/12/29)
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- BIS-PYRIDYLPYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS
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The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1 ), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment
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Page/Page column 19
(2010/12/29)
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- BIS-PYRIDYLPYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS
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The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1 ), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment
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Page/Page column 17
(2010/12/29)
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- BIS-PYRIDYLPYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS
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The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and/or diabetes.
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Page/Page column 26
(2009/07/17)
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- Triazolopyridine cannabinoid receptor 1 antagonists
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The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents, and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formula: including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein R1, R2, R3, R4 and R5 are described herein.
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Page/Page column 83
(2008/06/13)
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- Triazolopyrimidine cannabinoid receptor 1 antagonists
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The present application describes compounds according to both Formulas I and II, pharmaceutical compositions comprising at least one compound according to either Formula I or II and optionally one or more additional therapeutic agents, and methods of treatment using the compounds according to Formulas I and II both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formulas: including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein R1, R2, R3, R4 and R5 are described herein.
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Page/Page column 47
(2010/11/25)
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- Practical application of new catalytic methods: A concise synthesis of a potent PDE IV inhibitor
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An efficient synthesis of a potent PDE IV inhibitor 1 is described. The synthesis is highlighted by two practical and efficient catalytic reactions: a highly selective catalytic palladium mediated carbonylation of the pyridine side chain and an efficient
- Albaneze-Walker, Jennifer,Murry, Jerry A.,Soheili, Arash,Ceglia, Scott,Springfield, Shawn A.,Bazaral, Charles,Dormer, Peter G.,Hughes, David L.
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p. 6330 - 6336
(2007/10/03)
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- Selective palladium-catalysed carbonylations of dichloroquinoline and simple dichloropyridines
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Dichloroquinoline and some dichloropyridines undergo selective alkoxycarbonylation in the presence of carbon monoxide, an alcohol and PdCl2(PPh3)2 as a catalyst, affording chloro-monoester and/or diesters in good yields under selected reaction conditions.
- Najiba, Douja,Carpentier, Jean-Francois,Castanet, Yves,Biot, Christophe,Brocard, Jacques,Mortreux, Andre
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p. 3719 - 3722
(2007/10/03)
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- Process for preparing pyridine 2-carboxamides
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It has been found that pyridine-2-carboxamides of the formula STR1 wherein R is amino or a residue convertible into amino, and pharmaceutically usable acid addition salts of that carboxamide in which R is amino can be prepared in a simple manner and in good yield by reacting 2,5-dichloropyridine in the presence of a palladium-phosphine catalyst with an alkyne of the formula wherein R1 is hydrogen, lower-alkyl, trimethylsilyl or the group --(R2)(R3)--COH and R2 and R3 each independently are hydrogen or lower-alkyl or together are cyclopentyl or cyclohexyl, oxidizing the resulting alkyne to give 5-chloropyridine-2-carboxylic acid and reacting this acid or a reactive functional derivative thereof with an amino compound of the formula VI. The compound of formula I in which R is amino is a known compound which is a reversible and highly active MAO-B inhibitor.
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- Catechol 2,3-Dioxygenase-catalyzed Synthesis of Picolinic Acids from Catechols
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Various picolinic acid derivatives were synthesized from ammonia and hydroxymuconic semialdehyde derivatives that were oxidatively prepared from various catechols by the action of Pseudomonas catechol 2,3-dioxygenase (C23O, metapyrocatechase).
- Asano, Yasuhisa,Yamamoto, Yasushi,Yamada, Hideaki
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p. 2054 - 2056
(2007/10/02)
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