Abstract: Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor expression, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.

Abstract: The present invention relates to fungicidal compositions and their use for controlling oomycete pathogen induced disease or diseases in one or more plants.

Abstract: The invention features methods, compositions, and kits for selective inhibition of pain-and itch sensing neurons (nociceptors and pruriceptors) by drug molecules of small molecule weight, while minimizing effects on non-pain-sensing neurons or other types of cells.

Abstract: This invention relates to novel benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.

Abstract: The present invention provides a method of treating fibromyalgia syndrome (FMS), chronic fatigue syndrome (CFS), and pain in an animal subject. The method generally involves administering a therapeutically effective amount of a dual serotonin norepinephrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof, wherein said dual serotonin norepinephrine reuptake inhibitor compound is characterized by a non-tricyclic structure and an equal or greater inhibition of norepinephrine reuptake than serotonin reuptake. In particular, the use of milnacipran to treat FMS, CFS, and pain is disclosed.

Abstract: A compound having selective modulating activity at the alpha 2B and/or alpha 2C adrenergic receptor subtypes is represented by the general Formula 1: wherein n=1-4; X is C or N; R1-R6 can be the same or different and are independently selected from the group consisting of H, C1-6 alkyl, OCH3, OH, F, Cl, Br, CH2OH, CH2N(R7)2, C(O)R8, CH2CN, CF3; wherein R7 is H or C1-6 alkyl; and R8 is C1-6 alkyl or aryl. The compounds of Formula 1 can be incorporated in pharmaceutical compositions and used in methods of treatment of alpha 2 receptor mediated diseases and conditions.

Abstract: The invention provides immunostimulatory compositions comprising a small molecule immuno-poteniator (SMIP) compound and methods of administration thereof. Also provided are methods of administering a SMIP compound in an effective amount to enhance the immune response of a subject to an antigen. Further provided are novel compositions and methods of administering SMIP compounds alone or in combination with another agent for the treatment of cancer, infectious diseases and/or allergies/asthma.

Abstract: The present invention provides a method of treating fibromyalgia syndrome (FMS), chronic fatigue syndrome (CFS), and pain in an animal subject. The method generally involves administering a therapeutically effective amount of a dual serotonin norepinephrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof, wherein said dual serotonin norepinephrine reuptake inhibitor compound is characterized by a non-tricyclic structure and an equal or greater inhibition of norepinephrine reuptake than serotonin reuptake. In particular, the use of milnacipran to treat FMS, CFS, and pain is disclosed.

Abstract: A water dispersible granule formulation prepared by pulverized a part of active ingredients into fine particles under wet milling and pulverized another part of the active ingredients into coarse particles under dry milling, then kneading the both active ingredients for the granulation, and a process for producing the water dispersible granule formulation are disclosed. The water dispersible granule formulation according to the present invention is applicable for production of a water dispersible granule formulation comprising an active ingredient which is easily decomposed owing to environmental conditions and allows to provide the water dispersible granule formulation provided with enhanced initial and residual biological activities.

Abstract: The present invention provides compounds of the following structure; A-Q-B—C-D that are useful for treating conditions or disorders associated with DGAT1 activity in animals, particularly humans.

Abstract: The present invention is directed to 1,3,4-oxadiazalones, compounds of formula I and their pharmaceutically acceptable salts stereoisomers, tautomers, or solvates thereof. Novel compounds include those of formula I, in which radicals are as defined herein. The compounds of this invention are modulators of PPARdelta and therefore useful as pharmaceutical agents, especially for the treatment of demyelinating diseases and disorders of fatty acid metabolism and glucose utilization.

Abstract: Disclosed is an emulsifiable concentrate composition characterized by containing not less than 0.5% by weight but not more than 25% by weight of a hydrophobic agrochemically active compound, not less than 5% by weight but not more than 15% by weight of a surfactant, not less than 2% by weight but not more than 60% by weight of an aromatic hydrocarbon solvent, not less than 2% by weight but not more than 60% by weight of an ether compound represented by the following formula (1): R1—O-A1-O-A2-(O-A3)n—O—R2 (wherein R1 and R2 respectively represent a C1-C3 alkyl group; A1, A2 and A3 respectively represent an ethylene group or a propylene group; and n represents 0, 1 or 2), and not less than 12% by weight but not more than 90% by weight of 1,3-dimethyl-2-imidazolidinone. The emulsifiable concentrate composition is also characterized in that the weight ratio of 1,3-dimethyl-2-imidazolidinone to the ether compound (1,3-dimethyl-2-imidazolidinone:ether compound) is within the range from 1:0.03 to 1:2.

Abstract: The present invention relates to a compound of formula I, wherein R1 is selected from the group consisting of hydrogen and lower alkyl; each R2 is independently selected from the group consisting of hydrogen and lower alkyl; each R3 is independently selected from the group consisting of hydrogen, lower alkyl, lower alkoxy, phenyloxy, benzyloxy, halogen and lower alkyl substituted by halogen; R4 is selected from the group consisting of hydrogen and lower alkyl; X is selected from the group consisting of —CH2—, —CH— and —O—; Y is selected from the group consisting of —CH2—, —CH2CH2—, —CH— and a bond; with the proviso that, when X is —O—, Y is —CH2—; Z is selected from the group consisting of —CH2— and —CH—; m is 1 or 2; and n is 1 or 2. The invention relates also to a pharmaceutically-acceptable acid-addition salt of such a compound, methods for making the compound, and a composition comprising such a compound.

Abstract: The present invention relates to a delivery system for ophthalmic drugs, and more particularly, to a non aqueous oil delivery system. Low concentrations of ophthalmic drugs suspended in an oil vehicle delivery system are as therapeutically effective in man and animals as the corresponding higher concentrations of ophthalmic drugs that are commercially used in aqueous solutions. Eye drops that utilize this nonaqueous oil delivery system, when used in man, are comfortable to use and produce little ocular irritation, have a longer shelf-life, low systemic toxic potential, and only short term blurring of vision. Using this nonaqueous oil delivery system, a single drop of ophthalmic drug with a concentration that is 10 times less than the same drug used in commercially available aqueous eye drops is as effective as the commercially available aqueous ophthalmic eye drops that require many applications to be effective.

Abstract: There is provided a compound of formula I and the pharmaceutically acceptable salts and esters thereof wherein X1, X2, R1, R2, R3, R4, R5 and R6 are herein described. The compounds exhibit activity as anticancer agents.

Abstract: The present invention provides in vitro assays, e.g., FtsZ GTPase assays, and/or in vivo assays and methods of use thereof to identify particular compounds and combinations of compounds that affect microbial cell division. The invention further provides such compounds and compound combinations, including combinations that result in inhibition of cell survival or growth when present together at concentrations below their individual MICs. Certain of the compound combinations display synergism. Certain of the combinations include a compound that inhibits FtsZ GTPase activity and a compound that inhibits cell growth by a mechanism other than inhibition of FtsZ GTPase activity. The present invention further provides pharmaceutical compositions that have anti-microbial activity and methods of treating microbial infections.

Abstract: This application describes quinone derivatives which target the redox site of Ape1/Ref1. Also included in the invention are pharmaceutical formulations containing the derivatives and therapeutic uses of the derivatives.

Abstract: Compounds of formula I: (wherein variables A, m, n, J, Re, Rf, R4, Ea, Eb, Ec, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Abstract: The present invention relates to compounds of formula I wherein R1 is selected from the group consisting of hydrogen and lower alkyl; each R2 is independently selected from the group consisting of hydrogen and lower alkyl; each R3 is independently selected from the group consisting of hydrogen, lower alkyl, lower alkoxy, phenyloxy, benzyloxy, halogen and lower alkyl substituted by halogen; X is selected from the group consisting of —CH2—, —CH— and —O—; Y is selected from the group consisting of —CH2—, —CH— and a bond with the proviso that, when X is —O—, Y may not be a bond; Z is selected from the group consisting of —CH2— and —CH—; m is 0, 1 or 2; and n is 0, 1 or 2; and to pharmaceutically-acceptable acid addition salts of such compounds.

Abstract: Compounds that are useful in treating or preventing viral infections, such as influenza, are described herein. Further described are compositions made from these compounds and methods for using the compounds and their compositions in treating or preventing viral infections.

Abstract: Provided are compositions comprising beta-alanylhistidine peptides and beta-alanines, and methods for administering these peptides and amino acids. In one aspect, the compositions and methods cause an increase in the blood plasma concentrations of beta-alanine and/or creatine.

Abstract: The present invention provides a method of treating fibromyalgia syndrome (FMS), chronic fatigue syndrome (CFS), and pain in an animal subject. The method generally involves administering a therapeutically effective amount of a dual serotonin norepinephrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof, wherein said dual serotonin norepinephrine reuptake inhibitor compound is characterized by a non-tricyclic structure and an equal or greater inhibition of norepinephrine reuptake than serotonin reuptake. In particular, the use of milnacipran to treat FMS, CFS, and pain is disclosed.

Abstract: The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein R1 is independently hydrogen; alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl or substituted arylalkyl; R2 is independently —NR3R4, R3 is independently alkyl, cycloalkyl, alkoxy, alkylamine, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl, R4 is independently alkyl, cycloalkyl, alkoxy, alkylamine, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R5 is independently H, COR6, CO2R6, SOR6, SO3R6, alkyl, cycloalkyl, alkoxy, —NH2, alkylamine, —NR7COR6, halogen, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R6 is independently H, alkyl, cycloalkyl, —NH2, alkylamine, aryl or heteroaryl; R7 is independently H, alkyl, cycloalkyl, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, aryl, or heteroaryl; p is 0, or 1;

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: Biocompatible, bioerodible sustained release implants and microspheres for intracameral or anterior vitreal placement include an anti-hypertensive agent and a biodegradable polymer effective to treat an ocular hypertensive condition (such as glaucoma) by relapsing therapeutic amount of the anti-hypertensive agent over a period of time between 10 days and 1 year.

Abstract: The present invention provides a compound represented by formula (I): wherein n is an integer selected from 1 to 20, Q is A is cyano or the like; B is hydrogen, halogen, or the like; X1 and X2 are each independently selected from O and S; E is a C1-4 alkyl group; and R1, R2, R3 and R4 are each independently selected from a hydrogen atom and a C1-C6 alkyl group, and a drug, a pharmaceutical composition containing the compound, and the like.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, q, Ar, R1, R2 and R7 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.

Abstract: A compound having a structure is disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

Abstract: Topically applicable pharmaceutical compositions contain at least one pharmaceutically active agent and an effective antimicrobial amount of a preservative excipient mixture and devoid of such amount of known preservative(s) as would otherwise itself impart an effective antimicrobial action thereto.

Abstract: This invention relates to novel benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.

Abstract: Improved drug compositions and methods useful in the treatment of male erectile dysfunction. An optimized mixture of the drugs phentolamine mesylate, papaverine hydrochloride, and alprostadil in a buffer containing L-arginine and glycine is to be injected into the penile tissue to produce an erection in otherwise impotent men.

Abstract: Compounds of the formula (I) wherein z is SO2 or SO, useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.

Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.

Abstract: Described herein are new bicyclic arylimidazolones having nootropic action (i.e., protecting and stimulating cerebral functions), analgesic action and anti hyperalgesic action; also described is the process for their preparation and pharmaceutical compositions comprising them, useful for the treatment of cognitive deficits, and of various types of pain.

Abstract: Compounds of Formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), method of treatment comprising compounds of Formula (I), and methods of inhibiting the PARP enzyme comprising compound of Formula (I).

Abstract: This invention relates to non-natural desamino amino acid compounds, methods of making, and peptides containing these compounds as their N-terminus moieties. A preferred example is neurotensin (8-13) in which the N terminus is an alpha desamino N,N dimethyl homolysine residue.

Abstract: A modest (2-5 fold) increase in androgen receptor (AR) mRNA is the only expression change consistently associated with developing resistance to antiandrogen therapy. Increased levels of AR confer resistance to anti-androgens by amplifying signal output from low levels of residual ligand and altering the normal response to antagonists. This invention provides cell based assays for use in the examination of new therapeutic modalities and provides for the design of novel antiandrogen compounds.

Abstract: An object of the present invention is to provide a cerebral infarction suppressant which is effective for brain tissue necrosis after long-time ischemia as in actual cerebral infarction and has fewer side effects. The cerebral infarction suppressant of the present invention is characterized in that histidine is contained and the cerebral infarction is attributed to long-time ischemia.

Abstract: The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.

Abstract: Methods of inhibiting the cytokine or biological activity of Macrophage Migration Inhibitory Factor (MIF) comprising contacting MIF with a compound of formula (I) as defined herein, is provided. The invention also relates to methods of treating diseases or conditions where MIF cytokine or biological activity is implicated comprising administration of compounds of formula (I), either alone or as part of a combination therapy. Novel heterocyclic compounds are also provided for.

Abstract: This invention relates to novel 1,5,7-trisubstituted benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex.

Abstract: Indole derivatives that are useful in the treatment of cancer as a chemotherapeutic agent or radiosensitizing agent.

Abstract: Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.

Abstract: The present disclosure relates to salts and compositions of isophosphoramide mustard and isophosphoramide mustard analogs. In one embodiment the salts can be represented by the formula wherein A+ represents an ammonium species selected from the protonated (conjugate acid) or quaternary forms of aliphatic amines and aromatic amines, including basic amino acids, heterocyclic amines, substituted and unsubstituted pyridines, guanidines and amidines; and X and Y independently represent leaving groups. Also disclosed herein are methods for making such compounds and formulating pharmaceutical compositions thereof. Methods for administering the disclosed compounds to subjects, particularly to treat hyperproliferative disorders, also are disclosed.

Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, G1, Q1, Z, R1, R2, R3, R4a, R4b, R5a, and R5b are defined herein, inhibit the cytochrome P450RAI enzyme and are useful for the treatment and/or prevention of various diseases and conditions which respond to treatment by retinoids and by naturally occurring retinoic acid.

Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Abstract: The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.

Abstract: Novel acetophenone compounds of formula (I), compositions containing (I), processes for the preparation of (I), and use of (I) as inhibitors of the glycine transporter, are provided. Definitions of Ar, R5, R6, R7, R8 and n are provided in the specification.

Abstract: Polyimidazoline molecules and methods of making them are provided. A representative polyimidazoline has a structure: wherein: X is trifluoroacetyl or trifluoromethanesulfonyl; R1, R2, and R3 are each independently selected from a hydrogen, C1-C4 alkyl, C3-C7 cyclic alkyl, C1-C4 alkoxy, alcohol, and halogen; and n is 1 to 3.

Abstract: Compounds of formula I, wherein R1, m, R2, R3, p, n, R5 and R9 are as defined as in the specification, salts, solvates or solvated salts thereof, processes for their preparation, intermediates used in the preparation thereof, pharmaceutical formulations containing said compounds and the use of said compounds in therapy.