Patent classifications
C07D513/18
NLRP3 MODULATORS
Described herein are NLRP3 modulators and methods of utilizing NLRP3 modulators in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.
MACROCYCLIC SPIROCYCLE DERIVATIVES AS MCL-1 INHIBITORS
The present invention relates to pharmaceutical agents of formula (I) useful for therapy and/or prophylaxis in a subject, pharmaceutical composition comprising such compounds, and their use as MCL-1 inhibitors, useful for treating diseases such as cancer.
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MACROCYCLIC SPIROCYCLE DERIVATIVES AS MCL-1 INHIBITORS
The present invention relates to pharmaceutical agents of formula (I) useful for therapy and/or prophylaxis in a subject, pharmaceutical composition comprising such compounds, and their use as MCL-1 inhibitors, useful for treating diseases such as cancer.
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Fused pentacyclic imidazole derivatives
- Teresa De Haro Garcia ,
- Michael Deligny ,
- Jag Paul Heer ,
- Joanna Rachel Quincey ,
- Mengyang Xuan ,
- Zhaoning Zhu ,
- Daniel Christopher Brookings ,
- Mark Daniel Calmiano ,
- Yves Evrard ,
- Martin Clive Hutchings ,
- James Andrew Johnson ,
- Sophie Jadot ,
- Jean Keyaerts ,
- Malcolm MacCoss ,
- Matthew Duncan Selby ,
- Michael Alan Shaw ,
- Dominique Louis Leon Swinnen ,
- Laurent Schio ,
- Yann Foricher ,
- Bruno Filoche-Romme
A series of fused pentacyclic imidazole derivatives, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders. In particular, the present invention is concerned with 6, 7-dihydro-7, 14-methanobenzimidazo[1, 2-b][2,5]benzodiazocin-5(14H)-one derivatives and analogs thereof.
Fused pentacyclic imidazole derivatives
- Teresa De Haro Garcia ,
- Michael Deligny ,
- Jag Paul Heer ,
- Joanna Rachel Quincey ,
- Mengyang Xuan ,
- Zhaoning Zhu ,
- Daniel Christopher Brookings ,
- Mark Daniel Calmiano ,
- Yves Evrard ,
- Martin Clive Hutchings ,
- James Andrew Johnson ,
- Sophie Jadot ,
- Jean Keyaerts ,
- Malcolm MacCoss ,
- Matthew Duncan Selby ,
- Michael Alan Shaw ,
- Dominique Louis Leon Swinnen ,
- Laurent Schio ,
- Yann Foricher ,
- Bruno Filoche-Romme
A series of fused pentacyclic imidazole derivatives, being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders. In particular, the present invention is concerned with 6, 7-dihydro-7, 14-methanobenzimidazo[1, 2-b][2,5]benzodiazocin-5(14H)-one derivatives and analogs thereof.
SYNTHESIS OF STRUCTURAL ANALOGS OF LARGAZOLE AND ASSOCIATED COMPOUNDS
Disclosed are various synthetic methods to prepare structural analogs of largazole and derivatives thereof. One structural analog is an amide isostere of largazole. Another structural analog replaces the thiazole ring of largazole with a pyridine moiety or an oxazole moiety. Also disclosed are various intermediate compounds obtained when preparing structural analogs of
SYNTHESIS OF STRUCTURAL ANALOGS OF LARGAZOLE AND ASSOCIATED COMPOUNDS
Disclosed are various synthetic methods to prepare structural analogs of largazole and derivatives thereof. One structural analog is an amide isostere of largazole. Another structural analog replaces the thiazole ring of largazole with a pyridine moiety or an oxazole moiety. Also disclosed are various intermediate compounds obtained when preparing structural analogs of
Antibiotic compounds
Purified compounds of formula I are described. Compounds include all stereoisomeric forms and all tautomeric forms of the compounds of formula I and pharmaceutically acceptable salts and derivatives. Processes for the production of the antibacterial compounds by fermentation of the microorganism belonging to Streptomyces species (PM0626271/MTCC 5447) and to pharmaceutical compositions containing one or more of the novel compounds as active ingredient and their use in medicines for treatment and prevention of diseases caused by bacterial infections are described.
Antibiotic compounds
Purified compounds of formula I are described. Compounds include all stereoisomeric forms and all tautomeric forms of the compounds of formula I and pharmaceutically acceptable salts and derivatives. Processes for the production of the antibacterial compounds by fermentation of the microorganism belonging to Streptomyces species (PM0626271/MTCC 5447) and to pharmaceutical compositions containing one or more of the novel compounds as active ingredient and their use in medicines for treatment and prevention of diseases caused by bacterial infections are described.
Heterocyclic compounds and their use in preventing or treating bacterial infections
The present invention relates to heterocyclic compounds, their process of preparation, pharmaceutical compositions comprising these compounds and use thereof, optionally in combination with other antibacterial agents and/or beta-lactam compounds, for the prevention or treatment of bacterial infections. The present invention also relates to the use of these compounds as -lactamase inhibitors and/or as antibacterial agents.