Patent classifications
C07D495/18
MACROCYCLIC MCL-1 INHIBITORS AND METHODS OF USE
- Wilfried Braje ,
- George Doherty ,
- Katja Jantos ,
- Cheng Ji ,
- Andrew Judd ,
- Aaron Kunzer ,
- Anthony Mastracchio ,
- Xiaohong Song ,
- Andrew Souers ,
- Gerard Sullivan ,
- Zhi-Fu Tao ,
- Chunqiu Lai ,
- Jesse Teske ,
- Michael Wendt ,
- Patrick Brady ,
- Xilu Wang ,
- Thomas Penning ,
- Yujia Dai ,
- Jane Gong ,
- Roberto Risi ,
- Yiyun Yu ,
- Guidong ZHU
The present disclosure provides for compounds of Formula (I)
##STR00001##
wherein A.sup.2, A.sup.3, A.sup.4, A.sup.6, A.sup.7, A.sup.8, A.sup.15, R.sup.A, R.sup.5, R.sup.9, R.sup.10A, R.sup.10B, R.sup.11, R.sup.12, R.sup.13, R.sup.14, R.sup.16, W, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents for the treatment of diseases and conditions, including cancer. Also provided are pharmaceutical compositions comprising compounds of Formula (I).
Opioid receptor modulators
The present invention provides a compound having the structure wherein A is a ring structure, with or without substitution; X1 is C or N; X2 is N, O, or S; Y1 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y 2 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y3 is H-(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y 4 is H-(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y5 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); a and P are each present or absent and when present each is a bond.
Opioid receptor modulators
The present invention provides a compound having the structure wherein A is a ring structure, with or without substitution; X1 is C or N; X2 is N, O, or S; Y1 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y 2 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y3 is H-(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y 4 is H-(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y5 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); a and P are each present or absent and when present each is a bond.
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.
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.
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.
Diindole compounds useful in treatment of nervous system disorders
The invention provides bridged diindole compounds, related pharmaceutical compositions and methods of use thereof, for the prevention, palliation and/or treatment of nervous system disorders.
Diindole compounds useful in treatment of nervous system disorders
The invention provides bridged diindole compounds, related pharmaceutical compositions and methods of use thereof, for the prevention, palliation and/or treatment of nervous system disorders.
Heterocyclic compounds and their use in preventing or treating bacterial infections
The present invention relates to compounds of formula (I) and their use for treating or preventing a bacterial infection or as an antibacterial agent and/or as a -lactamase inhibitor.