Abstract: Disclosed herein are compounds of Formula (I) that include a sulfonate ester, ester or ether group. Compounds of Formula (I) can be included in pharmaceutical compositions, and can be used to treating and/or ameliorating a disease or condition, such as cancer, a microbial disease and/or inflammation.

Abstract: The present invention relates to methods and compositions for treating and evaluating metastatic conditions.

Abstract: Disclosed are methods of treating cancer comprising administering to the animal, a therapeutically effective amount of a heterocyclic compound of Formula VI. The animal is a mammal, preferably a human or a rodent.

Abstract: Disclosed are methods of modulating biosynthesis of Salinosporamide A and its analogs, which are useful in treating cancer, inflammatory conditions, and/or infectious disease. The methods involve, for example, genetic manipulation, selection of reagents in the fermentation feedstock, and selection of fermentation conditions.

Abstract: The invention is the discovery of an actinomycete genus, given the name Salinospora gen. nov., that displays an obligate requirement of seawater (Na+) for growth and unique 16S rRNA signature nucleotides. The invention is also the use of the genus for the production and discovery of active biomolecules such as pharmaceutical agents, agrichemicals, immunomodifiers, enzymes and enzyme inhibitors.

Abstract: Disclosed are methods of treating cancer, inflammatory conditions, and/or infectious disease in an animal comprising: administering to the animal, a therapeutically effective amount of a heterocyclic compound. The animal is a mammal, preferably a human or a rodent.

Abstract: A microcapsule can be produced readily by (a) pulverizing a solid pesticidal compound in terpineol, dihydroterpineol, terpinel acetate, dihydroterpinel acetate or a mixture thereof to form a suspension, (b) mixing the resulting suspension and water to prepare a liquid droplet, and (c) forming a coating film of a resin around the liquid droplet. The microcapsule obtained by such a method contains most of the solid pesticidal compound within the microcapsule.

Abstract: Disclosed are methods of treating Waldenstrom's Macroglobulinemia comprising administering to the animal, a therapeutically effective amount of a heterocyclic compound of Formula I.

Abstract: The present application demonstrates that Salinosporamide A can be used to sensitize cancer cells to cancer therapy. Furthermore, the present application demonstrates that Salinosporamide A acts as a therapeutic agent to kill or inhibit cancer cells after sensitization of the cells by an antibody or other chemosensitizing reagents. The cancer cells can be either therapy-sensitive or therapy resistant. The present application further demonstrates that Salinosporamide A induces the expression of Raf kinase inhibitor protein (RKIP) and PTEN, tumor suppressor proteins, and inhibits the expression of YY1, a transcriptional regulator protein overexpressed in cancer cells and also inhibits the growth factor pleiotrophin (PTN).

Abstract: Compounds of Formulae I-VI and derivatives thereof having anti-cancer, anti-inflammatory, and anti-microbial properties and to compositions that include one or more of compounds and their derivatives or analogs having anti-cancer, anti-inflammatory and anti-microbial properties are disclosed. Pharmaceutical compositions comprising such compounds and methods of treating cancer, inflammatory conditions, and microbial infections with the disclosed compounds or the disclosed pharmaceutical compositions are also disclosed.

Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease and diseases involving matrix or cartilate degradation.

Abstract: The present invention relates to indolinone derivatives substituted in the 6 position of general formula wherein R1 to R6 and X are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof, which have valuable pharmacological properties, in particular an inhibiting effect on various receptor tyrosine kinases and on the proliferation of endothelial cells and various tumour cells, pharmaceutical compositions containing these compounds, their use and processes for preparing them.

Abstract: Methods for purifying a compound of formula I are provided, wherein A, B X, Q, and R1 are defined herein. The methods include mixing the compound of formula I and a solvent; adding a base to the solvent; and precipitating purified compound of formula I.

Abstract: The invention is the discovery of an actinomycete genus, given the name Salinospora gen. nov., that displays an obligate requirement of seawater (Na+) for growth and unique 16S rRNA signature nucleotides. The invention is also the use of the genus for the production and discovery of active biomolecules such as pharmaceutical agents, agrichemicals, immunomodifiers, enzymes and enzyme inhibitors.

Abstract: Non-absorbent articles containing an additive are disclosed. The non-absorbent articles include an effective amount of an inhibitory compound such as cerulenin, triclosan, or hexachloroprene, for example, to substantially inhibit the production of TSST-1 by Gram positive bacteria.

Abstract: Disclosed herein are compositions and methods for treating neoplastic diseases. Included are compositions and methods that are effective against multiple myeloma cells resistant to conventional and bortezomib treatment. Furthermore, combination treatment with two different proteosome inhibitors is shown to be synergistic for treating multiple myeloma.

Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.

Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.

Abstract: Disclosed are methods of treating infectious diseases comprising administering to the animal, a therapeutically effective amount of a heterocyclic compound. The animal is a mammal, preferably a human or a rodent.

Abstract: The present invention relates to a process for the preparation of furopyrroles of general formula (I), comprising (a) heating a compound of the formula (II) under microwave irradiation optionally in the presence of an inert solvent, wherein A1 and A2 are C1-C18alkyl, C2-C18alkenyl, C2-C18alkynyl, C5-C8cycloalkyl, C5-C8cycloalkenyl, aryl or heteroaryl, A3 is hydrogen, C1-C18alkyl, cyanomethyl, Ar3, —CR30R31—(CH2)m—Ar3 or Y—R32, wherein R30 and R31 independently of each other stand for hydrogen or C1-C4alkyl, or phenyl which can be substitute up to three times with C1-C4alkyl, Ar3 stands for aryl, C5-C8 cloalkyl, C5-C8cycloalkenyl or heteroaryl, which can be substituted one to three times with C1-C8alkyl, C1-C8alkoxy, halogen or phenyl, which can be substituted with C1-C8alkyl or C1-C8alkoxy one to three times, and m stands for 0, 1, 2, 3 or 4, R is C1-C18alkyl, in particular C1-C4alkyl, aryl, in particular phenyl, or aralkyl, in particular benzyl, which can be substituted one to three times with C1-C8alkyl, C1

Abstract: The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders.

Abstract: The present invention comprises methods for the treatment of central nervous system diseases and disorders including mood disorders and sleep disorders through the administration of compounds of formula (I) and formula (II) which are useful as inhibitors of human casein kinase I?. Pharmaceutical compositions comprising compounds of formula (I) or formula (II) as well as methods for their preparation are also disclosed and claimed.

Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC kinases.

Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula I

Abstract: Lyophilized formulations comprising Salinosporamide A or analogs thereof are provided. In some aspects, lyophilized formulations comprising Salinosporamide A or analogs thereof and bulking agents are provided. Also provided are methods of lyophilizing Salinosporamide A or analogs thereof. In some aspects, a solvent or co-solvent system is utilized. Also provided are methods of administering Salinosporamide A or analogs thereof to patients.

Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is hydrogen or C1-4alkyl; R2 is C1-4alkyl; R3 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl and SF5; p is 0, 1, 2, 3 or 4; and R4 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy and C1-4alkanoyl; n is 0 or 1; wherein when R4 is chlorine and p is 1, such R4 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and wherein, if n is 0, R3 comprises at least one SF5 group as a substituent; processes for their preparation, intermediates used in these processes, pharmaceutical compositions contai

Abstract: Disclosed are compounds that inhibit proteasomic activity in cells. Also disclosed are pharmaceutical compositions comprising such compounds as well as methods to treat conditions, particularly cell proliferative conditions, such as cancer and inflammatory conditions.

Abstract: Compounds of Formulae I-VI and derivatives thereof having anti-cancer, anti-inflammatory, and anti-microbial properties and to compositions that include one or more of compounds and their derivatives or analogs having anti-cancer, anti-inflammatory and anti-microbial properties are disclosed. Pharmaceutical compositions comprising such compounds and methods of treating cancer, inflammatory conditions, and microbial infections with the disclosed compounds or the disclosed pharmaceutical compositions are also disclosed.

Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) specified agonists or antagonists of nicotinic acetylcholine receptors.

Abstract: An aqueous composition suitable for applying fungicides to plant propagation materials is provided, comprising water and a blend of the following components, by weight: a) 2–10% of a surface-active agent comprising a1) at least one anionic surfactant; b) 0.5–10% of at least one polymer selected from water-dispersible polymers and water-soluble film-forming polymers; c) 4–20% of at least one inorganic solid carrier; and d) 3–20% of at least one antifreeze agent. In one embodiment, the composition comprises a fungicidally effective amount of at least one fungicidally active compound. The inventive composition is storage stable, ready-to-apply (RTA), ecologically and toxicologically favorable and has good fungicidal efficacy.

Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.

Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.

Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.

Abstract: Novel amides and imides are inhibitors of tumor necrosis factor? and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions.

Abstract: An aqueous composition suitable for applying fungicides to plant propagation materials is provided, comprising water and a blend of the following components, by weight: a) 2-10% of a surface-active agent comprising a1) at least one anionic surfactant; b) 0.5-10% of at least one polymer selected from water-dispersible polymers and water-soluble film-forming polymers; c) 4-20% of at least one inorganic solid carrier; and d) 3-20% of at least one antifreeze agent. In one embodiment, the composition comprises a fungicidally effective amount of at least one fungicidally active compound. The inventive composition is storage stable, ready-to-apply (RTA), ecologically and toxicologically favorable and has good fungicidal efficacy.

Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) agonists or antagonists of nicotinic acetylcholine receptors.

Abstract: An environmentally safe pesticidal liquid suspension composition including a mixture of sulfur combined with pyrethrins and/or pyrethroids is provided. The pesticidal composition is effective to control plant diseases, as well as insect and mite pests. The composition can be prepared as concentrated or ready-to-use formulations. Formulations can be applied to plants, both indoors and outdoors, to control plant disease and insect and mite pests and reduce plant damage from such pests. The formulations can be applied to plants with minimal phytotoxicity (plant damage) and do not leave unacceptable levels of visible sulfur residue.

Abstract: The present invention is related to a compound of formula (I), salts and pro-drugs of the compound (I) and methods for treating and/or preventing partial or total ischemia, methods for treating and/or preventing pathologies associated with ischemia or with mitochondrial deficiencies.

Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.

Abstract: The invention relates to the use of the disaccharide derivatives 3′-aminosucrose, sucrose-C6-acid and palatinose-C6′-acid and/or of an amide or alkyl ester thereof for the prevention or treatment of hyperglycemias.

Abstract: The present invention relates to compositions comprising analogues of purine nucleosides containing a ring-expanded (“fat”) heterocyclic ring, in place of purine, and an unmodified or modified sugar residue, pharmaceutically acceptable derivatives of such compositions, as well as methods of use thereof. In particular, these compositions may be utilized in the treatment of certain cancers, bacterial, fungal, parasitic, and viral infections, including, but not limited to, Acquired Immunodeficiency Syndrome (AIDS), hepatitis, Epstein-Barr and cytomegalovirus.

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Abstract: A chondrogenic composition comprising a drug with chondrogenic effect, a biodegradable and/or bioerodable polymer and a water-soluble and/or water-dispersible organic solvent.

Abstract: This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I: 1

Abstract: Compounds of the formula I 1

Abstract: Disclosed are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof. The compounds can inhibit the biosynthesis of triglycerides in the liver and can inhibit the secretion of lipoprotein containing apolipoprotein B from the liver. Therefore, they are useful for the prevention or treatment of hyperlipidemia (particularly hyper-very-low-density-lipoproteinemia) and arteriosclerotic diseases, such as cardiac infarction, or pancreatitis induced by hyperlipidemia.

Abstract: Compounds, isolated from the bacteria Xenorhabdus bovienil, have antineoplastic activity. The invention provides pharmaceutical compositions containing the compounds and the methods for employing them as medicaments, particularly in the treatment of human and animal cancers.

Abstract: The present invention relates to new formulations containing one or more estrogens and 2-Phenyl-1-[4-(amino-1-yl-alk-1-ynyl)-benzyl]-1H-indol-5-ol compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structure below: and related methods of treatment for providing tissue selective estrogenic activity while minimizing undesirable side effects of estrogen treatment or therapy, such as excessive estrogenic uterine stimulation.

Abstract: The present invention relates to ion channel activating agents. More particularly, the present invention relates to a particular class of chemical compounds that has proven useful as openers of SKCa and IKCa channels. In further aspects, the present invention relates to the use of these SK/IK channel activating agents for the manufacture of medicaments and pharmaceutical compositions comprising the SK/IK channel activating agents.