Abstract: Compounds of formula (I): wherein X is O, CH2, S or NH, or the moiety X—R1 is hydrogen; V is CH or N; R1 is hydrogen, C1-6alkyl, C3-7cycloalkyl, aryl, arylC1-6alkyl, heterocyclyl, heterocyclylC1-6alkyl, heteroaryl, or heteroarylC1-6alkyl any of which except for hydrogen may be optionally substituted; R2 and R3 independently represent optionally substituted C1-6alkyl, or R2 and R3 together with the carbon atom to which they are attached form an optionally substituted C3-7cycloalkyl or C3-7cycloalkenyl ring; or R2 and R3 together with the carbon atom to which they are attached form an optionally substituted 5 to 7-membered heterocyclyl ring containing up to 3 heteroatoms selected from N, O, S.

Abstract: Novel substituted triazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.

Abstract: Disclosed are novel compounds of the formula wherein R1 is benzimidazolone derivative, M1 and M2 are optionally substituted carbon or nitrogen, R2 includes optionally substituted aryl or heteroaryl, and the remaining variables are as defined in the specification, and the remaining variables are as defined in the specification; also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating various diseases or conditions, such as allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of formula I, as well as methods of treating said diseases or conditions using the compounds of formula I in combination with an H1 receptor antagonist.

Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).

Abstract: A compound having the structural formula: where R is H or lower alkyl of 1 through 12 carbon atoms. In general, the compounds of the invention are 132-Oxo-bacteriopyropheophorbide—a carboxylic acid and C1–C12 alkyl esters thereof. A method for the preparation of the carboxylic acid compounds of the invention includes the step of reacting bacteriopyropheophorbide—a alkyl ester with lithium hydroxide tetrahydrofuran and water.

Abstract: The present invention provides compounds of formula (I): which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine.

Abstract: This invention concerns HIV replication inhibitors of formula (I) the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing ?a1=a2?a3=a4—and ?b1=b2?b3=b4represents pheynl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl, substituted C1-6alkyl, C1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH?2?, —NHC(?O)R6, —C(?NH)R6 or a 5-membered hetrocycl; X1 is —NR5—, —NH—NH—, —N?N—, —O—, —C(?O)—, C1-4alkanediyl, —CHOH—, —S—, —S(?O)p—, —X2—C1-4alkanediyl- or —C1-4alkanediyl-X2—; R3 is NHR13, NR13R14; —

Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.

Abstract: Disclosed are novel compounds of the formula wherein R1 is optionally substituted benzimidazolyl or a derivative thereof; R2 is optionally substituted aryl or heteroaryl; M1 and M2 are C(R3) or N; and the remaining variables are as defined in the specification; also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating various diseases or conditions, such as allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of formula I, as well as methods of treating said diseases or conditions using the compounds of formula I in combination with an H1 receptor antagonist.

Abstract: The present invention relates to a method for producing a pyrimidine derivate useful as a neurocyte neurocyte necrosis inhibitor and an intermediate thereof. Disclosed is a method for producing an acid salt of 4-(4-fluorophenyl)-2-methyl-6-(5-piperidinopentyloxy) pyrimidine. The method comprises reacting 4-chloro-6-(4-fluorophenyl)-2-methylpyrimidine with 5-piperidino-1-pentanol, hydrating the thus obtained 4-(4-fluorophenyl)-2-mehtyl-6-(5-piperidinopentylox) pyrimidine and then converting the resultant the hydrate into an acid salt. The hydrate as a describe above; and a method for producing the hydrate is part of this invention. According to the present invention, a highly pure acid salt of 4-(4-fluorophenyl)-2-methyl-6-(5-piperidinopentyloxy) pyrimidine can be readily and efficiently produced without using a column chromatography. Thus, this method is suitable for the production thereof on a industrial scale.

Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharma-ceutically acceptable acid addition salt thereof, wherein —a1?a2—a3?a4— is a bivalent radical wherein one or two of a1 to a4 are nitrogen and the remaining a1 to a4 are —CH?; —Z1—Z2— is a bivalent radical; —A— is a bivalent radical of formula —N(R6)—Alk2— or a 5, 6 or 7-membered saturated heterocycle containing one or two nitrogen atoms; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R5 is a radical of formula (d-1), (d-2), (d-3), (d-4), (d-5) wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y2 is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl

Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory and immune conditions and diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of a chemokine receptor. The subject methods are useful for the treatment of inflammatory and immunoregulatory disorders and diseases, such as multiple sclerosis, rheumatoid arthritis and type I diabetes.

Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritis, vitiligo, general gastrointestinal disorders, gastric ulceration, d

Abstract: The present invention relates to compounds having the general formula or a pharmaceutically acceptable salt thereof, wherein R1 is a saturated or unsaturated 5-, 6- or 7-membered, ring containing 0, 1, 2 or 3 atoms selected from N, O and S, wherein the ring may be fused with a benzo group, and is substituted by 0, 1 or 2 oxo groups, and wherein R1 is additionally substituted; and R2 is a substituted C1-6alkyl. Also included is a method of prophylaxis or treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic ? cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs.

Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative thereof, wherein R1, R2, V1, V2, and V3 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of AKT, PKA, PDK1, p70S6K, or ROCK kinase, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of utilizing those compositions in the treatment of various disorders.

Abstract: Tri-heterocyclic compound of formula (I) wherein each of W, X and Y is carbon or nitrogen; each of U and Z is CR2, NR13, nitrogen, oxygen, sulfur etc.; A ring is carbocyclic ring, heterocyclic ring; R1 is alkyl, alkenyl, alkynyl, NR4R5, OR6 etc.; R3 is carbocyclic ring, heterocyclic ring; and a pharmaceutically acceptable salt thereof, a process for the preparation thereof, a pharmaceutical comprising them as an active ingredient. A compound of formula (I) is useful, in order to possess corticotropin releasing factor receptor antagonistic activity, for the prevention and/or treatment of depression, anxiety, eating disorder, posttraumatic stress disorder, peptic ulcer, irritable bowl syndrome, Alzheimer's disease, drug addiction or alcohol dependence syndrome etc.

Abstract: Disclosed are 2-alkylated-cyclodextrin derivatives and pharmaceutically acceptable salts thereof. The 2-alkylated-cyclodextrin derivatives are suitable for use in the reversal of drug-induced neuromuscular block.

Abstract: The present invention relates to compounds having the general formula or a pharmaceutically acceptable salt thereof, wherein R1 is a saturated or unsaturated 5-, 6- or 7-membered, ring containing 0, 1, 2 or 3 atoms selected from N, O and S, wherein the ring may be fused with a benzo group, and is substituted by 0, 1 or 2 oxo groups, and wherein R1 is additionally substituted; and R2 is a substituted C1-6alkyl. Also included is a method of prophylaxis or treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic ? cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs.

Abstract: The present invention relates to heterodimeric conjugates of neomycin-chloramphenicol, of formula 1, their preparation and their use. Because of their heterodmieric structure, they can recognize both stem and loop of RNA motif and show binding ability to a certain RNA such that they have an enhanced pharmaceutical efficacy and reduced side effect which can be caused by non-specific drugs. For these reasons, they can be effectively used as an antiviral agent, an antibacterial agent or an anticancer drugs.

Abstract: Derivatives of retinamide are potent and selective apoptosis-inducing agents. These compounds exhibit antitumor properties and as such can be used in the treatment of cancer and other hyperproliferative disorders.