Abstract: The present invention relates to biaryl-benzylamine compounds, to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.

Abstract: The present invention provides cyclic nitro compounds, pharmaceutical compositions of cyclic nitro compounds and methods of using cyclic nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.

Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.

Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.

Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-Beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, or salts thereof, wherein A, W, X and Z are defined herein.

Abstract: The present invention relates to novel organic compounds comprising a naphthyridine which may be mediators of a selective subset of kinases belonging to the AGC kinase family, such as for example PKC, PKD, PKN-1/2, CDK-9, MRCK-beat, PASK, PRKX, ROCK-I/II or mediators of other kinases, the selectivity of which would be depending on the structural variation thereof.

Abstract: The invention provides a novel class of cyclic oximes of Formula I: wherein A, X, Y, Z, W, R1, R2, R3 and n are as described in the summary of the invention; useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.

Abstract: Compounds of the formula (I), and pharmaceutically acceptable salts thereof, are found to be antagonists of SNS sodium channels.

Abstract: An oral pharmaceutical formulation comprising iota-carrageenan, one or more neutral gelling polymers and a basic pharmaceutically active ingredient; which formulation inhibits the release of the basic pharmaceutically active ingredient from the formulation at acidic pH; a process for the manufacture of said formulation; and the use of said formulation in medicine.

Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

Abstract: A compound having immunosuppressive activity with low toxicity or a pharmacological salt thereof.

Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.

Abstract: The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein the groups R1-R5, R10 and X1-X7 are as defined in the specification.

Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF-? or combinations thereof.

Abstract: There is provided a compound of formula (I) wherein Ra, R1, R2, Y and R3 have meanings given in the description and pharmaceutically-acceptable derivatives (including prodrugs) thereof, which compounds and derivatives are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is required (e.g., thrombosis) or as anticoagulants.

Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, aggrecanase, ADMP, LpxC, ADAMs, TACE, TNF-? or combinations thereof.

Abstract: The present invention provides compounds of formula (I) in which n, y, X1, X2, A, B, R1, R2, R3, R4 and R5 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: Disclosed is a 1-glycidyl-3,3-dinitroazetidine(GDNAZ) of Formula I wherein dinitroazetidine group which is a high energy group having unit structure of explosive moiety is incorporated to a monomer, and the method thereof. By using the GDNAZ of the present invention in the synthesis of energetic binder for high-performance insensitive explosive, an energetic binder with enhanced thermal and storing stability and explosive power can be provided.

Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.

Abstract: The present invention provides novel substituted amino-azetidines that are useful as cannabinoid receptor antagonists/inverse agonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, dyslipidemias, cardiovascular disorders, hepatic disorders, and a combination thereof.

Abstract: Novel compounds inhibiting the integrin ?2?1/GPIa-IIa receptor are disclosed. Also disclosed are pharmaceutical compositions containing the compounds, as well as methods of their therapeutic use. The compounds disclosed are useful, inter alia, as inhibitors of integrin ?2?1/GPIa-IIa-mediated activity.

Abstract: Compounds of formula (I) and their use in therapy, particularly for the treatment of a disorder mediated by CB1 receptors, such as obesity, wherein: R1 is aryl or heteroaryl; R2 is alkyl, aryl or heteroaryl; R3 is alkyl, aryl, heteroaryl, NR9R10, OR15, or NR16C(O)R17; Y is C?O, C?S, SO2, or (CR7R8)p; m=1 or 2; n=1 or 2; and p=1, 2, 3 or 4, R7 to R17 being as defined in the specification; wherein if —Y—R3 is C(O)NH(alkyl) then: R1 and/or R2 is selected from heteroaryl; and/or m and/or n is 2; and/or R11 and/or R12 is lower alkyl, or a pharmaceutically acceptable salt or prodrug thereof.

Abstract: The present invention provides cyclic nitro compound, pharmaceutical compositions of cyclic nitro compounds and methods of using cyclic nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.

Abstract: Compounds of the formula provide pharmacological agents which are potent agonists of Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.

Abstract: The present invention provides cyclic nitro compounds, pharmaceutical compositions of cyclic nitro compounds and methods of using cyclic nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.

Abstract: It is intended to provide compounds having EDG-5 antagonism. Because of having EDG-5 antagonism, compounds of the formula (I): wherein each symbol is as defined in the description; salts thereof, N-oxides thereof, solvates thereof or prodrugs thereof are useful as preventive and/or therapeutic agent for EDG-5 mediated diseases, for example, diseases caused by blood vessel contraction (e.g. cerebrovascular spasms disease, cardiovascular spasms diseases, coronary artery spasms disease, hypertension, pulmonary hypertension, renal diseases, myocardial infarction, angina pectoris, arrhythmia, portal hypertension, varicosity and the like), arteriosclerosis, pulmonary fibrosis, hepatic fibrosis, renal fibrosis, respiratory diseases (e.g. bronchial asthma, chronic obstructive pulmonary diseases and the like), nephropathy, diabetes, hyperlipemia and the like.

Abstract: The present invention relates to amides that have activity as SIP receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.

Abstract: Compounds of formula (I) and their use in therapy, particularly for the treatment of a disorder mediated by CB1 receptors such as obesity: Formula (I) wherein: R1 and R2 are independently selected from aryl; and R3 is hydrogen or alkyl; or a pharmaceutically acceptable salt or prodrug thereof, wherein at least one of R1 and R2 has a non-hydrogen substituent in the ortho-position(s) thereof relative to the point of attachment to the [—CH—O—] group.

Abstract: The invention relates to substituted azacycloalka?e compounds useful in treating conditions of the Central Nervous System (CNS); a pharmaceutical composition comprising same; a method of treating such conditions and of treating conditions in which inhibition of beta-secretase is indicated.

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

Abstract: The present invention relates to compounds that are useful as protease inhibitors, particularly as serine protease inhibitors, and more particularly as hepatitis C NS3 protease inhibitors. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HCV NS3 protease activity and consequently, may be advantageously used as therapeutic agents against the hepatitis C virus and other viruses that are dependent upon a serine protease for proliferation. This invention also relates to methods for inhibiting the activity of proteases, including hepatitis C virus NS3 protease and other serine proteases, using the compounds of this invention and related compounds.

Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1? converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-? inducing factor-(IGIF), or interferon-?-(“IFN-?”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting caspase activity and decreasing IGIF production and IFN-? production and methods for treating interleukin-1, apoptosis-, and interferon-?-mediated diseases using the compounds and compositions of this invention.

Abstract: The present invention is directed to a compound of formula (I): wherein Ar1, Ar2, Ar3, R1 and T are as defined herein, its preparation, pharmaceutical composition and uses as orexin 2 receptor antagonist.

Abstract: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.

Abstract: The present invention is directed to novel, potent, and selective agents, which are agonists or antagonists of the one or more of the individual receptors of the S1P receptor family. The compounds of the invention are useful as therapeutics for treating medical conditions associated with agonism or antagonism of the individual receptors of the S1P receptor family.

Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the treatment of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.

Abstract: The present invention encompasses compounds of Formula 1: as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.

Abstract: A process for preparing a protected amidine group of formula (I): wherein R6 represents, for example, C1-10 alkyl (optionally substituted), aryl, C1-3 alkylaryl or C1-3 alkyloxyaryl; which comprises reacting a nitrile containing compound with an oxyamine of formula (II): R6ONH2 wherein R6 is as defined above for (I); in the presence of a thio-keto activating agent of formula (III): HS—Ry, —C(O)-Z wherein Z is -(1-4C)alkyl, —OH, —O-(1-4C)alkyl, —SH, —S(1-4C)alkyl, —NH2, —NH(1-4C)alkyl or —N[(1-4C)alkyl]2; Ry is (1-2C)alkyl (optionally substituted); or Z and Ry are linked so as to form a 5- or 6-membered ring of formula (IV): wherein X is —CH2—, —O—, —NH— or —N(1-4C)alkyl; p is 1 or 2; m is 1 or 2 and Rz is independently selected from H, (1-4C)alkyl, halo and amino.

Abstract: Compounds of Formula (I) wherein: R1 is methyl; R2 is selected from —C (O) NR4R5, SO2NR4R5, S (O) pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from for example hydrogen, optionally substituted (1-4C) alkyl and HET-2; R5 is hydrogen or (1-4C) alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro drug or solvate thereof, are described.

Abstract: There are provided crystalline forms of the compounds Ph(3-Cl)(5-OCHF2)—(R)CH(OH)C(O)-Aze-Pab(OMe) and Ph(3-Cl)(5-OCHF2)—(R)CH(OH)C(O)-Aze-Pab(OH), pharmaceutical compositions containing them, processes for obtaining them and their use in medical treatment.

Abstract: The invention relates to EP2 antagonist azetidines of formula (I) wherein Ar, R1, X, and Z are as defined herein, to their use in medicine, particularly in the treatment of endometriosis and/or uterine fibroids, to intermediates useful in their synthesis, and to compositions containing them.

Abstract: The invention provides compounds of the formula: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a, Z and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.

Abstract: In some aspects, the present invention provides a method of preparing a compound of the formula (I) comprising reacting a mesylate compound of the formula (II) by direct aminolysis with a reagent comprising ammonia. The reaction is preferably carried out in a solvent, such as an alcohol, and is preferably carried out in a sealed vessel such as a Parr reactor or the like.

Abstract: The invention relates to a novel method for the synthesis of N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-(3,5-difluorophenyl)methylsulfonamide.

Abstract: Disclosed are urea compounds of formula I, stereoisomer, or pharmaceutical acceptable salts thereof, and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetic-related diseases.

Abstract: The present invention relates to compounds capable of inhibiting binding of the Smac protein to Inhibitors of apoptosis (IAPs). Such compounds are preferably capable of inhibiting IAP and thus may promote apoptosis or sensitize cells for apoptosis. The compounds may be used in the treatment of proliferative diseases, such as cancer.

Abstract: The present invention relates to a compound represented by the following formula: (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, or a combination thereof, wherein Ro, R1, R1?, R2, R2?, R3 and n are defined herein. The present invention further relates to a method of treating a patient from endometreosis or uterine fibroids.

Abstract: The present invention provides compounds of the formula: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.

Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.