Fast release solid formulation, preparation and use thereof
The present invention relates to a chemically stable formulation of florfenicol, (and structurally related compounds) in compositions such as soluble blended...
Ester compound and use thereof
An ester compound represented by the formula (1): ##STR00001## wherein R represents a C1-C4 alkyl group or a C3-C4 alkenyl group, and A represents a single...
Levodopa prodrug mesylate, compositions thereof, and uses thereof
(2R)-2-Phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate and crystalline form thereof, methods of making the same, pharmaceutical...
Preparation and diabetic use of Gibberellins
The present invention relates to application of compounds of formula (1) (Gibberellins) and their derivatives for the preparation of a pharmaceutical...
Substituted 4-aryl-chromene as activator of caspases and inducer of
apoptosis and as antivascular agent and the...
The present invention is directed to a substituted 4H-chromene represented by the Formula 1R, substantially free from the corresponding (S)-stereoisomer: ...
Pharmaceutical compositions for the treatment of pain
The present invention relates to treatment of cancer related pain and constipation. Preferably the subject in need is administered a combination of the...
This invention provides new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for...
3-aminopyrrolidone compounds and pharmaceutically acceptable salts thereof that are active as sodium and/or calcium channel modulators and therefore useful in...
1,3-disubstituted 4-methyl-1H-pyrrole-2-carboxamides and their use in
1,3-disubstituted 4-methyl-1H-pyrrole-2-carboxamides corresponding to formula I ##STR00001## methods for their production, pharmaceutical compositions...
IAP binding compounds
IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPs (inhibitor of apoptosis proteins) in cells...
Glucagon receptor antagonist compounds, compositions containing such
compounds and methods of use
Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions...
Injectable formulation of antibiotic and solution for intravenous
A pharmaceutical composition for injection comprising a depsipeptide antibiotic, WAP-8294A.sub.2, as an active ingredient, which is stable and contains...
Tetrahydrocyclopenta[b]indole compounds as androgen receptor modulators
The present invention provides a compound of the formula: Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a...
Cytotoxic compounds and conjugates
The present disclosure provides cytoxic compounds useful as drugs or prodrugs and to drug-cleavable substrate conjugates where the drug and cleavable substrate...
Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
The present invention discloses novel compounds of Formula (I): having 11.beta.-HSD type 1 antagonist activity, as well as methods for preparing such compounds....
This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically...
Substituted pyrrolo-pyrazole derivatives active as kinase inhibitors
Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their...
5(S)-substituted pyrazoline compounds, their preparation and use as
The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use...
Imidazolidine compounds as androgen receptor modulators
Novel compounds are disclosed that have a Formula represented by the following: ##STR00001## wherein X, R.sup.1, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3a...
Imidazolidin-2-one derivatives as selective androgen receptor modulators
The present invention is directed to novel imidazolidin-2-one derivatives having a structure according to Formula I ##STR00001## wherein a, b, R.sup.1,...
Antifungal triazole derivatives
Disclosed herein are antifungal triazole derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical...
Indole amide derivatives as EP4 receptor antagonists
The invention is directed to indole amide derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute...
Modulators of glucocorticoid receptor, AP-1, and/or NF-.kappa.B activity
and use thereof
Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or...
Preparation and use of aryl alkyl acid derivatives for the treatment of
This invention relates to certain aryl alkyl acid compounds, compositions, and methods for treating or preventing obesity and related diseases.
Nitric oxide donors and uses thereof
Disclosed are novel NO-donating compounds, designed such that when NO is released from the compound a residue which is a naturally occurring metabolite is...
Biaryl compositions and methods for modulating a kinase cascade
The invention relates to compounds and methods for modulating one or more components of a kinase cascade. The invention relates to compounds of the formula I: ...
Hydrazide compound and pesticidal use of the same
A hydrazide compound represented by the formula (1): ##STR00001## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, A.sup.1, A.sup.2, J, Q and n are defined in the...
Nitrogen-containing heterocyclic compound and pharmaceutical application
It is intended to provide a compound represented by the formula (I): ##STR00001## wherein all the symbols are as defined in the description; which has a p38...
2,4,6-substituted pyridyl derivative compounds useful as beta-secretase
inhibitors for the treatment of...
The present invention is directed to 2,4,6-substituted pyridyl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the...
Isoindolone compounds and their use as metabotropic glutamate receptor
The present invention is directed to compounds of formula I: ##STR00001## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8,...
Methods for treatment of multiple myeloma using
Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are...
Substituted piperidine derivatives as SST5 modulators
This invention is concerned with compounds of the formula ##STR00001## wherein A, R.sup.1 to R.sup.5 and G are as defined in the description and claims, and...
Compounds for the modulation of PPAR.gamma. activity
Modulators of PPAR.gamma. activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II...
Pyrrolo(2,3-b) pyridine derivatives, the preparation and the
pharmaceutical use thereof in the form of kinase...
Novel compounds of formula (I): ##STR00001## or pharmaceutically acceptable salts thereof, wherein R, R1, R2, R3, R4, R5, and R6 have the meanings given in...
Therapeutic combinations comprising
The present invention relates to SNS-595 and methods of treating cancer using the same.
HIV integrase inhibitors
Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: ##STR00001## wherein bond a, ring A, R.sup.1, R.sup.2 and...
Oxime and hydroxylamine substituted imidazo[4,5-c] ring compounds and
Imidazo[4,5-c] ring compounds, (e.g. imidazo[4,5-c]pyridines, imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydro imidazo[4,5-c]quinolines, ...
Pharmaceutical formulations comprising an immune response modifier
Pharmaceutical formulations comprising an immune response modifier (IRM) chosen from imidazoquinoline amines, imidazotetrahydroquinoline amines, imidazopyridine...
Steroidal compounds as steroid sulphatase inhibitors
There is provided a compound having Formula I ##STR00001## wherein G is a fluorocarbyl group, and wherein R.sup.1 is any one of a sulphamate group, a...
Compounds that modulate PPAR.gamma.-type receptors and
cosmetic/pharmaceutical compositions comprising said...
Novel compounds having the general formula (I) below: ##STR00001## are useful in a wide variety of applications in human or veterinary medicine (in...
Methods of using
Compounds of formula I are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and/or manage diseases and disorders: ...
Amidine derivatives of 2-heteroaryl-quinazolines and quinolines; potent
analgesics and anti-inflammatory agents
The present invention concerns novel amidines derivatives of 2-heteroaryl-quinazoline and quinolines of general formula (I), to a process for their preparation,...
Substituted pyrrolo[2,3-2]pyrimidines as protein kinase inhibitors
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent...
Heteroaryl compounds, compositions thereof, and methods of treatment
Provided herein are Heteroaryl Compounds having the following structure: ##STR00001## wherein R.sup.1, R.sup.3, R.sup.4, L, X, Y, A and B are as defined...
Intermediates in the preparation of entecavir via carbon-silicon oxidation
Processes for preparing entecavir and novel intermediates thereof using carbon-silicon oxidation. ##STR00001##
Disclosed are novel pyrazolo[3,4-d]pyrimidine derivatives that are inhibitors of Raf kinase. These compounds and their pharmaceutically-acceptable salts and...
Tetrahydro-4H-pyrido[1,2-a] pyrimidines useful as HIV integrase inhibitors
Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds of Formula A: ##STR00001## are described as inhibitors of HIV integrase and inhibitors of HIV...
A compound which can be used as a pharmaceutical, particularly a insulin secretion promoter or a agent for preventing/treating disease in which GPR40 is...
Chromenoneindole derivatives of the formula (I), in which R.sup.1, R.sup.2, R.sup.3, R, A and B are as defined in Claim 1, and pharmaceutically usable prodrugs,...
Substituted N-aryl heterocycles, process for their preparation and their
use as medicaments
The invention relates to substituted N-aryl heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof....