Patent classifications
C07D498/02
Fused tricyclic benzimidazoles derivatives as modulators of TNF activity
- Rikki Peter Alexander ,
- Mark Daniel Calmiano ,
- Sabine Defays ,
- Veronique Durieu ,
- Michael Deligny ,
- Jag Paul Heer ,
- Victoria Elizabeth Jackson ,
- Jean Keyaerts ,
- Boris Kroeplien ,
- Malcolm Mac Coss ,
- Yogesh Anil Sabnis ,
- Matthew Duncan Selby ,
- Dominique Louis Leon Swinnen ,
- Nathalie Van Houtvin ,
- Zhaoning Zhu ,
- Uwe Heinelt ,
- Volkmar Wehner
A series of tricyclic benzimidazole derivatives, in particular dihydro-1H-imidazo [1,2-a]benzimidazole, dihydro-1H-pyrrolo [1,2-a]benzimidazole, dihydro-1H-pyrazino[1,2-a]benzimidazole, dihydro-1H-[1,4]oxazino[4,3-a]benzimidazole and dihydrothiazolo[3,4-a]benzimidazolem, and analogs thereof, 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.
Methods of Treating or Preventing Autoimmune Diseases with 2,4-Pyrimidinediamine Compounds
The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lupus erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.
Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.
Small molecule inhibitors of polynucleotide kinase/phosphatase, poly(ADP-ribose) polymerase and uses thereof
The present invention generally relates to use of compounds and compositions as a chemosensitizers and/or radiosensitizers and/or inhibitors of PNKP phosphatase activity. The present invention provides pharmaceutical combinations and/or a pharmaceutically acceptable salt thereof, kits containing such compounds and/composition and methods of using such compounds and/or compositions.
ANTIBACTERIAL COMPOUNDS
The invention relates to antibacterial and anti-mycobacterial drug compounds of formula I. It also relates to pharmaceutical formulations of antibacterial drug compounds. It also relates to uses of the derivatives in treating bacterial infections, and methods of treating bacterial infections. The invention is also directed to antibacterial drug compounds capable of treating bacterial infections that are currently hard to treat with existing drug compounds, e.g., those caused by resistant bacterial or mycobacterial strains.
ANTIBACTERIAL COMPOUNDS
The invention relates to antibacterial and anti-mycobacterial drug compounds of formula I. It also relates to pharmaceutical formulations of antibacterial drug compounds. It also relates to uses of the derivatives in treating bacterial infections, and methods of treating bacterial infections. The invention is also directed to antibacterial drug compounds capable of treating bacterial infections that are currently hard to treat with existing drug compounds, e.g., those caused by resistant bacterial or mycobacterial strains.
Enantiomers of the 1′,6′-isomer of neplanocin A
Enantiomers of 1,6-isoneplanocin, including derivatives of the enantiomers of 1,6-isoneplanocin, are disclosed along with novel synthetic methods. In particular, a substituted cyclopentane epoxide is synthesized into the enantiomers of 1,6-isoneplanocin. Enantiomers of carbocyclic nucleoside analogs of 3-deazaneplanocin to provide D- and L-like 1,6-iso-3-deazaneplanocin are also disclosed. The small molecule chemotherapeutic compounds beneficially provide DNA and RNA antiviral activity, demonstrating activity towards, for example, human cytomegalovirus, measles, Ebola, norovirus, dengue, vaccinia and HBV. Compounds exhibiting reduced S-adenosylhomocysteine hydrolase inhibitory effects are disclosed and provide improved toxicity profiles in comparison to neplanocin. The invention provides improved prophylactic and/or therapeutic antiviral efficacy.
Substituted pyrazolylpyrazole derivative and use of same as herbicide
Provided is a compound capable of effectively control worst weeds of higher leaf stages that present practical problems. A specific pyrazolylpyrazole derivative of formula (I) is disclosed that is able to solve the above-mentioned problems. ##STR00001##
Heterocyclic derivatives as modulators of kinase activity
The invention provides novel imidazol-piperidinyl derivatives of the formula (I) ##STR00001##
in which R.sup.1, R.sup.2, W, X.sup.1, X.sup.2, X.sup.3, X.sup.4 and n have the meanings indicated in formula I, and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
BCL-2 INHIBITORS
The disclosure includes compounds of Formulae (1) wherein Q.sub.1, Q.sub.2, Q.sub.3, Q.sub.4, Q.sub.5, Q.sub.6, Q.sub.7, Q.sub.8, Q.sub.x, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.9, R.sub.10, R.sub.11, R.sub.x, a, b, c, g, j, k, m, n, u, v, L, Z.sub.1, Z.sub.2, Z.sub.4, and Z.sub.5 are defined herein. Also disclosed is a method for treating a neoplastic disease and autoimmune disease with these compounds.
##STR00001##