Patent classifications
C07D495/08
Polycations and methods of making and using thereof
Disclosed are polycationic polymers. The polycationic polymers can include a plurality of positively charged centers, each of which is formed by condensation of cyclic bis-electrophile (e.g., a 9-thia/aza/selenabicyclo[3.3.1]nonyl electrophile) with a nucleophile. The resulting polycationic polymers can efficiently bind nucleic acids. The polycations can also exhibit properties of cytotoxicity and DNA transfection with interesting structure-activity characteristics.
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.
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 Mac Coss ,
- 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 Mac Coss ,
- 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.
Substituted phenyloxazolidinones for antimicrobial therapy
The present invention relates to novel oxazolidinones (Formula I): or a pharmaceutically acceptable salt having ring A characterized by N-containing monocyclic, bicyclic or spirocyclic substituents, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments. ##STR00001##
Substituted phenyloxazolidinones for antimicrobial therapy
The present invention relates to novel oxazolidinones (Formula I): or a pharmaceutically acceptable salt having ring A characterized by N-containing monocyclic, bicyclic or spirocyclic substituents, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments. ##STR00001##
INDAZOLE DERIVATIVES USEFUL AS INHIBITORS OF DIACYLGLYCERIDE O-ACYLTRANSFERASE 2
The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (DGAT2) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.
##STR00001##
TRICYCLIC SULFONES AS ROR GAMMA MODULATORS
There are described ROR modulators of the formula (I),
##STR00001##
and formula (II)
##STR00002##
or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating ROR activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of ROR activity, for example, autoimmune and/or inflammatory disorders.
TRICYCLIC SULFONES AS ROR GAMMA MODULATORS
There are described ROR modulators of the formula (I),
##STR00001##
and formula (II)
##STR00002##
or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating ROR activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of ROR activity, for example, autoimmune and/or inflammatory disorders.