Abstract: The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.

Abstract: A cyclopropane derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof has orexin receptor inhibitory action, and thus, is extremely useful as an agent for preventing or treating sleep disorder or dyssomnia caused by orexin, including insomnia as a typical example: wherein A1, A2 and A3 each independently represent an aryl group, a heterocyclyl group or the like, R1, R2 and R3 each independently represent a hydrogen atom, a C1-6 alkyl group or the like, X represents an oxygen atom or the like, and L represents a bond or the like.

Abstract: The present invention relates to substituted imidazopyridazines and substituted benzimidazoles, as well as pharmaceutical compositions comprising the same, which are FGFR3 inhibitors useful in the treatment of cancer and other diseases.

Abstract: A method of treating a condition in a subject in need thereof, comprising administering a calcium/calmodulin dependency kinase kinase (CaMKK) inhibitor in a treatment-effective amount. Conditions which may be treated include obesity (particularly adult obesity), insulin resistance (including high fat diet-induced insulin resistance), hyperglycemia (including hyperglycemia accompanying obesity), diabetes, etc.

Abstract: A method of inhibiting viral respiratory infection in a mammal in need of same, includes administering an effective amount of 2-[2-(5-carbamimidoyl-benzofuran-2-yl)-vinyl]-H-benzoimidazole-5-carboxamidine or the Bis-N-hydroxyamidine prodrug thereof, prior to viral infection, or therapeutically following viral infection, to inhibit that viral infection. The compound selectively inhibits Caspase 2 and/or 8 as to prevent infective viral particle release. It is optionally administered IV, IP, orally or via other conventional administration routes in a dosage range of 1 ng/kg-200 mg/kg of body weight.

Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: The present invention is directed to oral formulations of bendamustine, and its pharmaceutically acceptable salts, methods of use thereof, and methods of treatment comprising them.

Abstract: The invention provides a composition in concentrated form (“the concentrate”) for dilution with water in the preparation of an agricultural composition for application to crops, soil or animals, comprising a carbohydrate-based pH modifying agent and a pH indicator. The agricultural composition comprises an agricultural chemical whose agricultural activity varies with the pH of the water. The proportions of the pH indicator and the pH modifying agent in the concentrate are selected so that when the concentrate is diluted with an appropriate amount of water, the pH indicator indicates visually by colouration of the composition, whether or not the pH of the water is suitable for acceptable agricultural activity of the chemical. The invention also provides a process for preparing the agricultural composition by mixing the concentrate with water, and adding the agricultural chemical to the composition, if it is not already present in the concentrate.

Abstract: The invention relates to compounds of formula (I), wherein R1, R2, R1a, R2a, R3, R4, A, B, X, W and n are as defined in the description, and pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium channel blockers.

Abstract: The present invention discloses a novel TGF-? signaling mechanism implicated in craniofacial malformation as well as methods and compositions for treating craniofacial malformation utilizing knowledge of the mechanism. Methods of the invention generally comprises administering an effective amount of a TGF-? inhibitor to a subject in need of the treatment. Also disclosed are methods for treating craniofacial malformation by administering Tgf-?, Tgf-?RIII, p38 MAPK inhibitor or neutralizing antibodies to a subject. Also disclosed is a diagnostic method for diagnosing patients at risk of developing craniofacial malformation by determining the level of Tgf-?2 and ectopic p38 MAPK activation. Compounds useful for treating craniofacial malformation may also be discovered by using animal models of the present invention.

Abstract: The present invention is related to the composition and methods of manufacture of orally-dissolvable, edible films as a vehicle for the non-invasive administration of active drugs through the mucosal tissues of the oral cavity. The films include a water soluble film-forming polymer such as pullulan. Methods for producing the films are also disclosed.

Abstract: Disclosed are pharmaceutical compositions comprising 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide, or a pharmaceutically acceptable salt thereof. Also disclosed are methods of using such compositions for inhibiting abnormal cell growth or treating hyperproliferative diseases in mammals.

Abstract: Disclosed are pharmaceutical compositions comprising 6-(4-Bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide, or a pharmaceutically acceptable salt thereof. Also disclosed are methods of using such compositions for inhibiting abnormal cell growth or treating hyperproliferative diseases in mammals.

Abstract: Disclosed are methods of treating a hyperproliferative disorder or a disease related to vasculogenesis or angiogenesis in a mammal, comprising administering to said mammal an effective amount of a compound of the formula or a pharmaceutically accepted salt thereof, wherein A, R1, R2, R7, R8, and R9 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals.

Abstract: The present invention is related to novel benzimidazole compounds of Formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.

Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.

Abstract: The present invention is directed to nanostructured (nanoparticulated) Telmisartan compositions, process for the preparation thereof and pharmaceutical compositions containing them. The nanoparticles of Telmisartan according to the invention have an average particle size of less than about 600 nm. Telmisartan is an angiotensin II receptor antagonist (ARB) used in the management of hypertension.

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: This invention generally provides compounds, pharmaceutical compositions, and methods for their use, which include methods that result in increased expression in an Atoh1 gene (e.g., Hath1) in a biological cell. More specifically, the invention relates to the treatment of diseases and/or disorders that would benefit from increased Atoh1 expression, e.g., a hearing impairment or imbalance disorder associated with a loss of auditory hair cells, or a disorder associated with abnormal cellular proliferation.

Abstract: The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.

Abstract: The present invention relates to compounds, compositions, methods and/or kits for determining and/or predicting and/or diagnosing and/or treating restenosis in a patient.

Abstract: Stable liquid formulations of bendamustine, and pharmaceutically acceptable salts thereof, and polar aprotic solvents, are described.

Abstract: This invention relates to novel compounds having the formula (I): and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.

Abstract: The invention concerns tricyclic N-heteroaryl-carboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.

Abstract: The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I: wherein R1, R2, R3, R5, X, A3, B1, s and n are defined herein, for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of contrast-induced nephropathy.

Abstract: Glucose deprivation is an attractive strategy in cancer research and treatment. Cancer cells upregulate glucose uptake and metabolism for maintaining accelerated growth and proliferation rates. Specifically blocking these processes is likely to provide new insights to the role of glucose transport and metabolism in tumorigenesis, as well as in apoptosis. As solid tumors outgrow the surrounding vasculature, they encounter microenvironments with a limited supply of nutrients leading to a glucose deprived environment in some regions of the tumor. Cancer cells living in the glucose deprived environment undergo changes to prevent glucose deprivation-induced apoptosis. Knowing how cancer cells evade apoptosis induction is also likely to yield valuable information and knowledge of how to overcome the resistance to apoptosis induction in cancer cells.

Abstract: This invention relates to novel tetrahydronaphthalene derivatives, and pharmaceutically acceptable salts thereof according to the following formulae, in one embodiment: as described herein. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a selective T-type calcium channel blocker.

Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.

Abstract: Provided are certain chemical entities, pharmaceutical compositions, and methods of treatment of a member of the flaviviradae family of viruses such as hepacivirus (Hepatitis C or HCV).

Abstract: Disclosed are compounds of the Formula and pharmaceutically acceptable salts and prodrugs thereof, wherein A, R1, R2, R7, R8, and R9 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.

Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.

Abstract: The invention concerns pharmaceutical compositions containing a hydrogen sulphate salt of 6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide and solvates, crystalline forms and amorphous forms thereof, to the use of said compositions as a medicament; and to processes for the preparation of said compositions.

Abstract: The present invention relates to a use of a compound having an acid pump antagonistic activity, a pharmaceutically acceptable salt thereof or a pharmaceutical composition thereof for the manufacture of a medicament for prevention or treatment of diseases in which abnormal gastrointestinal motility is involved. In addition, the present invention relates to the method of prevention or treatment including administering to a human or animal. The compound, the pharmaceutically acceptable salt thereof, or pharmaceutical compositions containing them, may be used in combination with one or more second active agent. Further, the present invention relates to pharmaceutical compositions and kits comprising a compound having an acid pump antagonistic activity or a pharmaceutically acceptable salt thereof for the prevention or treatment of said diseases.

Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.

Abstract: A compound depicted by the formula below, or a pharmaceutically acceptable salt or solvate thereof. wherein, R1 represents (1) a C3-6 alkyl group, (2) a C1-6 alkyl group substituted with one or more substituent group(s) selected from those consisting a halogen atom, etc., (3) a C3-10 non-aromatic cyclic hydrocarbon group or a 5- to 6-membered non-aromatic heterocyclic group which respectively is optionally substituted with one or more substituent group(s) selected from those consisting an oxo group, etc., (4) an aromatic cyclic hydrocarbon group substituted with one or more substituent selected from the group consisting halogen atom and C1-4 alkoxy group; X represents NH, O, or S; Y represents CH or N; Z represents N or a C—R2; R2 represents (1) hydrogen atom, (2) a C1-6 alkyl group, a C2-6 alkenyl group or a C2-6 alkynyl group that respectively is optionally substituted with one or more substituent group(s) selected from among those consisting (a) a halogen atom, etc.

Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.

Abstract: A cosmetic composition is provided including a water-insoluble UV-A sunscreen agent having a ?max at 330-380 nm, a water-insoluble UV-B sunscreen agent having a ?max between 280 and 320 nm, and a water-soluble sunscreen agent having a ?max between 280 and 400 nm, the water-soluble sunscreen agent being neutralized with metallic counter ions which in a first portion are sodium and in a second portion are potassium ions present in a respective molar ratio of 0.5:2 to 2:1, and a cosmetically acceptable carrier including from 0.2 to 4% of potassium stearate by weight of the composition.

Abstract: The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.

Abstract: The present invention relates to derivatives of 2-phenyl-benzimidazoles of the formula I, in which X, R, R1 to R3 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired.

Abstract: The present invention relates to new compounds or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.

Abstract: The invention relates to a compound of formula (I) wherein A, R1-R6 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.

Abstract: A pharmaceutical solution, preferably a drinkable pharmaceutical solution of the active substance telmisartan is described, having a pH above 10 and additionally containing one or more sugar alcohols added to improve the flavour and shelf life, wherein the sugar alcohols or the pharmaceutical solution have a maximum content of 1000 ppm of reducing sugars.

Abstract: Methods are provided for treating or prophylactically preventing metabolic disorders in humans without causing, promoting, or aggravating fluid retention, peripheral edema, pulmonary edema, or congestive heart failure, by administration of a therapeutically effective amount of a compound sufficient to partially or fully activate peroxisome proliferator activated receptors (PPARs) and partially or fully inhibit, antagonize or block the activity of angiotensin II type 1 receptors. Metabolic disorders that can be treated or prevented include but are not limited to type 2 diabetes, the metabolic syndrome, prediabetes, and other insulin resistance syndromes.

Abstract: The present invention relates to a method of treatment and/or prophylaxis of a microbial infection, comprising the step of administering an effective amount of a compound of formula (I), in which X and Y are either the same or different and selected from a heteroatom; is a double or single bond depending on the heteroatoms X and Y; R1 to R5 are either the same or different and selected from hydrogen or a non-deleterious substituent; and R6 and R7 are either the same or different and selected from hydrogen and a non-deleterious substituent or one of R6 and R7 are absent when there is a double bond present, pharmaceutically acceptable salts or derivatives, pro-drugs, tautomers and/or isomers thereof. The present invention also relates to a method for protecting a subject from radiation damage, a method of cancer radiotherapy and use as an antimicrobial or radioprotective agent of the compound of formula (I) defined above.

Abstract: Heterocyclic compounds that modulate the hedgehog signaling pathway, pharmaceutical composition thereof and their therapeutic applications.

Abstract: The present invention provides a method for treating a disease or condition in a mammal which comprises the steps of; administering a therapeutically effective amount of a T type calcium channel inhibitor to effectively slow or stop progression of eukaryotic cells through the S, G2 and M phases of the cell cycle to increase the proportion of the eukaryotic cells in the G1 phase, stopping administration of the T type calcium channel inhibitor for a period of time, and administering a dosage selected from the group consisting of a dosage of at least one chemotherapeutic agent, a dosage of radiation, and combinations thereof, to kill the proportion of eukaryotic cells progressing past the G1 phase of the cell cycle after the stopping of the administration of the T type calcium channel inhibitor.

Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.

Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to 3-substituted-8-substituted-3H-imidazo[5,1-d][1,2,3,5]tetrazin-4-one compounds of the following formula, wherein -A and —B are as defined herein (collectively referred to herein as 38TM compounds): The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cell proliferation, and in the treatment of proliferative disorders such as cancer, etc., and methods of preparing such compounds.

Abstract: The invention provides for methods of upregulating endogenous GDNF by inhibiting Shh signaling. The invention further provides a method for increasing the production of cholinergic neurons and dopamine neurons by subventricular zone (SVZ) neurogenesis in a subject. The invention further provides methods for treating a neurodegenerative disorder in a subject.

Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.