Patent classifications
C07D513/00
Compounds for treatment of pain
The aspects of the disclosed embodiments are directed to novel compounds, specifically, quaternary ammonium derivatives of tertiary amine containing opioid drug compounds such as hydrocodone, hydromorphone and oxycodone, formulations containing said. compounds or pharmaceutically acceptable salts thereof, which are capable of providing controlled release of the opioid drug upon administration to a patient in order to treat pain.
Glutaminase inhibitors and method of use
Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.
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.
Crystal forms of (R)-N-methylnaltrexone bromide and uses thereof
The present invention provides a new forms of (R)-N-methylnaltrexone, and compositions thereof, useful as a peripheral mu opioid receptor antagonist.
Rhodamine derivatives dyes and uses thereof
This invention is directed to photoluminescent compounds based on rhodamine dyes with red-shifted absorption and emission maxima and uses thereof for photoluminescence based devices.
Fluorescent monomers and tagged treatment polymers containing same for use in industrial water systems
The invention is directed towards methods and compositions for making and using fluorescent monomers which are synthesized by reacting a substituted or non-substituted benzoxanthene anhydride with an amine and with a moiety containing a polymerizable group. Such monomers are useful for the preparation of tagged treatment polymers. Such tagged treatment polymers are useful as scale inhibitors in industrial water systems.
Selective glycosidase inhibitors and uses thereof
The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
Derivatives of camptothecin, a method of producing them and their use
The subject of the present invention are water-soluble derivatives of camptothecin, their synthesis and use. These compounds exhibit preferable biological properties for use in anti-neoplasm therapy.
Indole and indoline derivatives and methods of use thereof
The present application relates to indole and indoline derivatives of formula (I), (II), (III), (IV), (V), or (VI) ##STR00001##
wherein a, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, U, V, W, X, Y, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
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##