Abstract: The present invention relates to a composition useful for the treatment of leishmaniasis said composition comprising pharmaceutically effective amount of methyl-beta-cyclodextrin, optionally along with other anti-leishmanial agent(s) and/or pharmaceutically acceptable additives, and a method thereof, wherein the said method reduces the cholesterol levels of the plasma membrane of the infected host cells by about 50%.

Abstract: The present invention discloses novel phospho-derivatives of branched-chain lipophilic molecules useful for permeabilizing biological barriers and for inhibiting tumor growth. The invention further discloses pharmaceutical compositions comprising said molecules and their uses.

Abstract: Novel synthetic forms of etherified oxidized phospholipids and methods of utilizing same for preventing and treating atherosclerosis and other related disorders, as well as inflammatory disorders, immune mediated diseases, autoimmune diseases and proliferative disorders, are provided. In addition, methods of synthesizing etherified and esterified oxidized phospholipids and of using same for preventing and treating atherosclerosis and other related disorders are also provided.

Abstract: The present invention relates to a process for the preparation of 3-amino-2-hydroxypropylphosphinic acid derivatives of the formula I, which are valuable pharmaceutical active ingredients and can be used, for example, as antidepressants. The process starts from O-ethyl phosphinates of the formula II into which, after silylation with hexamethyldisilazane, the 3-amino-2-hydroxypropyl moiety is introduced by reactions with epichlorohydrin and ammonia.

Abstract: The present invention provides compositions, methods, and kits for improving health in a woman having elevated SHBG levels, or who is receiving oral estrogen supplementation, by non-orally administering an effective amount of an androgenic steroid. Further, the present invention provides compositions, methods, and kits for coadministering an effective amount of an orally administered estrogen and an effective amount of a non-orally administered androgenic steroid for women in need of estrogen supplementation.

Abstract: The subject invention provides a mechanism by which steroidal quinol compounds confer beneficial ophthalmic effects. The subject compounds possess a lipophilic-hydrophilic balance for transcorneal penetration and are readily reduced into parent phenolic A-ring steroid compounds to provide protection or treatment against various ocular symptoms and disorders. The compounds according to the subject invention appear to be highly advantageous as prodrugs to provide protection and/or treatment against ocular disorders. These prodrugs confer lipid solubility optimal for transocorneal penetration and are readily converted to endogenous reducing agents into active phenolic A-ring steroid compounds. To the extent that these prodrugs have reduced feminizing effects and systemic toxicity, they would be expected to be quite advantageous for protecting or treating the eye against ocular disorders such as cataract or glaucoma without undesired (systemic) side effects).

Abstract: Steroidal compounds or their salts having general formula: A—B—C—NO2 are described, wherein: A=R—, wherein R is a steroidal drug radical; B=—TB—X2—TBI—, wherein TB is (CO), TBI is O, S, NH, and X2 is a bivalent bridging group; and C is a bivalent radical.

Abstract: The present invention provides novel dihydropyrancarboxamide compounds of formula (I): and collections of these compounds, and provides methods for the synthesis of these compounds; wherein R1–R6 are as defined herein. Additionally, the present invention provides pharmaceutical compositions and methods for treating disorders such as proliferative diseases, and cancer, to name a few.

Abstract: The compounds of formula I in which R1, R2, R3, R4 and R5 have the meanings as given in the description are PDE4/7 inhibitors.

Abstract: The invention relates to the use of flumazenil to produce a medicament for the treatment of cocaine dependency. The flumazenil can be administered sequentially in small quantities at short intervals until a therapeutically effective quantity for the treatment of cocaine dependency has been administered.

Abstract: This invention relates to methods of inhibiting growth of a cancer cell and methods of treating cancer using a novel farnesylated dibenzodiazepinone.

Abstract: The present invention provides compounds of formula (I) wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents

Abstract: The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction

Abstract: Compounds of Formula I are useful as mediators of protein kinases and have activity as cell proliferation inhibitors: where X, R1–R7 and R9 are as defined herein.

Abstract: The invention relates to compounds of formula (I) processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.

Abstract: The invention provides compounds of general formula (I), in which m, n, Z1, Z2, R1, R2, R3, R4 and R5 are as defined in the specification; processes for their preparation; pharmaceutical compositions containing them; and their use in therapy

Abstract: Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(?O) or the formula: —C(?O)NH(OH); R1 represents hydrogen, C1–C6 alkyl or C1–C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(?O), a hydroxy, C1–C6 alkoxy, C1–C6 alkenyloxy, amino, C1–C6 alkylamino, or di-(C1–C6 alkyl)amino group; R2 represents a substituted or unsubstituted C1–C6 alkyl, cycloalkyl(C1–C6 alkyl)- or aryl(C1–C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.

Abstract: The present invention relates to compounds of formula (I): in which X represents N or CH; R1 represents a hydrogen or halogen atom or a CF3 group; R2 and R3 independently represent a hydrogen atom or a methyl group; n is 0 or 1; A represents an optionally substituted nitrogenous heterocycle; and to their N-oxides and to their salts or solvates, to the pharmaceutical compositions and the medicaments comprising them, and to a process for their preparation.

Abstract: Novel substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.

Abstract: Novel ?1-pyrrolines of the Formula (I) in which R1, R2, R3 and Het have the meanings given in the description, a plurality of processes for preparing these compounds and their use for controlling pests, and also novel intermediates and processes for their preparation.

Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.

Abstract: The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders.

Abstract: The present invention provides compositions and their use in the treatment of inflammatory diseases caused by T-cell proliferation such as sepsis, inflammatory bowel diseases, autoimmune encephalomyelitis, or lupus. The compositions comprise disubstituted ureas of Formulas I, II, III or IV: R1—NH—CO—NH-Q-R2Formula I: Et-NH—CO—NH-Q-R2:??Formula (II) Et-NH—CO—NH—(CH2)3—NR6R7:??Formula (III) Me2N—(CH2)3—NH—CO—NH-Q-R2.

Abstract: Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.

Abstract: A class of substituted spiro-hydantoin compounds (II) having the formula: its pharmaceutically acceptable salts, enantiomers, solvates, or prodrugs thereof, wherein R16 is a substituted pyridinyl group, as defined herein, is provided. Pharmaceutical compositions and methods of treating anti-inflammatory and/or immune diseases with the pyridyl-substituted spiro-hydantoin compounds are also objectives of this invention.

Abstract: 17-methylene-4-azasteroid compounds of formula I: wherein R20 denotes fluoro, chloro or bromo R20a denotes hydrogen, R10 and R4 each denote a hydrogen atom or a methyl group, and R1 and R2 each denote a hydrogen atom or together denote an additional bond, are useful for treating diseases or conditions caused by excessive androgen levels, such as acne, prostate diseases, alopecia and hirsutism, as well as gynecological conditions. Methods of synthesizing the new 17-methylene-4-azasteroid compounds are described.

Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation.

Abstract: Piperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.

Abstract: A compound of the formula (I) or a pharmaceutically acceptable salt thereof: [wherein X1 and X2 each is independently lower alkylene; X3 is ?CH2, ?CHF or ?CF2; R1 is substituent, R2 and R3 each is independently H or lower alkyl; n is 0, 1, 2, 3 or 4.] having the activity inhibiting DPP-IV activity. They are therefore useful in the treatment of conditions mediated by DPP-IV, such as NIDDM.

Abstract: Substituted aryloxyalkylamines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.

Abstract: Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, and pyridine N-oxide; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1–C6alkyl, NO2, CF3, C1–C6alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety or functional gastrointestinal disorders.

Abstract: The invention provides Aryl substituted imidazoles, pyrazoles, pyridizines and related compounds of the Formula where the variables are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of the invention act bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptos. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory and immune system disorders.

Abstract: The present invention relates to acylated arylcycloalkylamines, to pharmaceutical compositions comprising such compounds, to methods for the stimulation of the expression of endothelial NO synthase, and methods of treatment comprising administering such compounds.

Abstract: The present invention is directed to compounds and methods suitable for the treatment of HIV infection.

Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to inhibitors of ZAP70. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereo Formula (I): wherein N-HeT is for example triazolyl; Q is for example phenyl or pyridyl, substituted with: T is for example selected from (TAa1 to TAa12) such as (TAa1) and (TAa5): R4h, R5h, R6h are for example selected from hydrogen, (1–4C)alkyl, (1–4C)alkoxy-carbonyl, (1–4C)alkanoyl and carbamoyl; processes for making them, compositions containing them and their use as antibacterial agents are described.

Abstract: A carbamate compound is disclosed.

Abstract: In its many embodiments, the present invention provides a novel class of imidazo[1,2-a] pyrazine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

Abstract: The invention relates to a group of novel 2,3 diaryl-pyparazolidine derivatives having formula (1). The symbols used in formula (1) have the meanings given in the specification. The compounds have inhibiting activity on enzymes which degrade the neuropeptide neurotensin and can be used for the treatment of affections and diseases caused by disturbances of the neurotensin mediated transmission.

Abstract: The present invention provides benzamide inhibitors of the P2X7 receptor of the formula: wherein R1–R3 are as defined herein. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, including, without limitation, inflammatory diseases such as osteoarthritis and rheumatoid arthritis; allergies, asthma, COPD, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

Abstract: The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.

Abstract: Disclosed herein are compositions comprising an amide related to a prostaglandin and an amine wherein the amine is selected from the group consisting of epinephrine, dopamine, serotonin, and analogs or prodrugs thereof. Also disclosed are certain chemical compounds, pharmaceutical compositions, and methods of treating glaucoma.

Abstract: This invention relates to the use of compounds of Formula (I) as vascular damaging agents: wherein X is selected from: —O—, —S—, —S(O)—, —S(O2)—, —N(R5)—, —C(O)—, —C(O)N(R5)—, —N(R5)C(O)—, —S(O2)N(R5)—, or —N(R5)S(O2)—; R1 is independently selected from: amino, halo, hydroxy, —OPO3H2, C1-4alkyl, or C1-4alkoxy, wherein the amino group is optionally substituted by an amino acid residue and the hydroxy group is optionally esterified; R2 is selected from: hydrogen or C1-4alkyl; R3 is selected from: hydrogen, halo, hydroxy, hydroxyC1-4alkyl, cyano, cyanoC1-4alkyl, carboxy, carboxyC1-4alkyl, C1-4alkanoyl, C1-4alkanoylC1-4alkyl, carbamoyl, carbamoylC1-4alkyl, C1-4alkoxy, C1-4alkoxycarbonyl, C1-4alkoxycarbonylC1-4alkyl, C1-4alkoxycarbonylamino, amino, N—C1-4alkylamino, NN-diC1-4alkylamino, aminoC1-4alkyl, N—C1-4alkylaminoC1-4alkyl, NN-diC1-4alkylaminoC1-4alkyl, ureido, or C1-4alkylureyleno; R4 is independently selected from: C1-4alkyl, C1-4alkoxy or halo; R5 is selected from: hydrogen or C1-4alkyl; n is 0 or 1; p is

Abstract: Indoles having aryloxyalkanoic acid substituents or arylalkanoic acid substituents are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.

Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Abstract: The present invention provides novel compounds of the general Formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is (CH2)n where n is 0, 1 or 2; R1, R2, R3, R4 and R5 may be the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, alkylsulphonyloxy, cyano, nitro, trihaloalkyl, sulpho or one of the structures given in Scheme 1; or two of R1, R2, R3, R4 and R5 may together form a methylenedioxy or ethylenedioxy moiety; R6, R7, R8 and R9 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, amines (primary, secondary or tertiary) having 0, 1 or 2 carbon atoms, cyano, nitro, trihaloalkyl, amide or sulpho, and z where shown represents the point of attachment of the residue to the phenyl or pyrrole ring; and the pharmacologically active salts thereof.

Abstract: The present invention relates to pyrrolo-naphthyl compounds of the formula and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders.

Abstract: Optically active maleimide derivatives of the formula: (where the various substituents are as defined in the description) are used as separating media for separating optical isomers and geometrical isomers such as by high performance liquid chromatography.

Abstract: The disclosure concerns an injectable composition of paclitaxel, more particularly, an injectable composition of paclitaxel having excellent anticancer effect comprising solubilizer such as polyoxyl hydrogenated castor oil, anhydrous ethanol and stabilizer such as N-acetyl amino acid. The injectable compositions of paclitaxel provide a medical effect higher than that of the known compositions showing not only a lower toxicity but also superior solubility of paclitaxel and stability at room temperature, thus enabling venous injection by having fine particles.

Abstract: N-(imino)amines and their preparation and their use as NO synthase inhibitors and selective or non-selective traps for a reactive oxygen species.