Abstract: The present invention relates to inhibition of viruses, e.g., HIV using pyrrolidones and compounds related to pyrrolidones. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions that inhibit HIV in a cell; as well as to methods of prophylaxis, and therapy related to HIV infection and related disease states such as AIDS.

Abstract: The invention relates to a process for the preparation of heterocycles, characterised in that the following components: i) a propargyl derivative of the general structural formula I  a wherein Het is an optionally substituted hetero atom and A is a substituted or unsubstituted aromatic entity, a substituted or unsubstituted aromatic heterocycle, a substituted or unsubstituted vinyl arene and/or a derivative thereof, an olefin, an alkyne, an acceptor group or a nitrile; (ii) a compound of the general structural formula II, B—X  II,  wherein B is an electron-deficient substituted or unsubstituted aromatic entity with or without an acceptor group, an electron-deficient substituted or unsubstituted heteroaromatic entity with or without an acceptor group, an electron-deficient olefin and/or alkyne, a metal complex, and X is a leaving group; (iii) a nucleophile of the general structural formula III, Y—Cn—Z  III,  wherein Y and/or Z, each

Abstract: The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.

Abstract: The present invention provides a compound of formula I: 1

Abstract: The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by Progesterone Receptor. Also provided are methods of making such compounds and pharmaceutical compositions.

Abstract: Compounds of the formula (I) below, or pharmacologically acceptable salts, esters or other derivatives thereof: 1

Abstract: This invention provides compounds and methods for treating melanocortin receptor associated disorders, such as weight loss disorders including cachexia resulting from cancer and other chronic illnesses.

Abstract: Substituted 2-pyridine cyclohexane-1,4-diamine compounds, a method for their production, pharmaceutical compositions containing them, and the use of such substituted 2-pyridine cyclohexane-1,4-diamine compounds for treating pain and various other medical conditions.

Abstract: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which may be useful for the treatment of cytokine mediated diseases such as arthritis.

Abstract: The present invention provides compounds of formula (I), pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.

Abstract: Unsymmetrical cyanine dyes that incorporate an aza-benzazolium ring moiety are described, including cyanine dyes substituted by a cationic side chain, monomeric and dimeric cyanine dyes, chemically reactive cyanine dyes, and conjugates of cyanine dyes. The subject dyes are virtually non-fluorescent when diluted in aqueous solution, but exhibit bright fluorescence when associated with nucleic acid polymers such as DNA or RNA, or when associated with detergent-complexed proteins. A variety of applications are described for detection and quantitation of nucleic acids and detergent-complexed proteins in a variety of samples, including solutions, electrophoretic gels, cells, and microorganisms.

Abstract: The present invention relates to 2-substituted 4-heteroaryl-pyrimidines, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders such as cancer, leukaemia, psoriasis and the like.

Abstract: The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.

Abstract: The invention provides compounds of formula (I) wherein R1 to R5 are as defined in the description, and their preparation. The compounds of formula (I) are useful as pharmaceuticals.

Abstract: The present invention relates to pyridyl substituted heterocycles and hydro isomers thereof and pharmaceutical compositions thereof that inhibit replication and/or proliferation of HCV virus. The present invention also relates to the use of the pyridyl heterocycles and hydro isomers thereof and/or pharmaceutical compositions comprising the compounds to treat or prevent HCV infections.

Abstract: Compounds of the general formula are described: wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R3 is halogen, trifluoromethyl, lower alkoxy or lower alkyl; R4/R4′are each independently hydrogen or lower alkyl; R5 is lower alkyl, lower alkoxy, amino, hydroxy, hydroxy-lower alkyl, —(CH2)n-piperazinyl, optionally substituted by lower alkyl, —(CH2)n-morpholinyl, —(CH2)n+1-imidazolyl, —O—(CH2)n+1-morpholinyl, —O—(CH2)n+1-piperidinyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, —NH—(CH2)n+1N(R4″)2, —(CH2)n—NH—(CH2)n+1N(R4″)2, —(CH2)n+1N(R4″)2, or —O—(CH2)n+1N(R4″)2, wherein R4″ is hydrogen or lower alkyl; R6 is hydrogen; R2 and R6 or R1 and R6 may together be —CH═CH—CH═CH—, wherein R2 and R6 or R1 and R6, respectively, together with the two carbon rin

Abstract: The invention provides a compound of formula I wherein X, R1, R2 and Het are as defined in the description, and a process for preparing them. The compounds of formula I are useful as pharmaceuticals.

Abstract: Isoxazolone compounds having the generic structure: 1

Abstract: An N-aminoimidazole or N-aminoimidazolethione derivative, a pharmaceutically acceptable salt, a tautomer, an isomer, an ester or glycosylation product thereof, said derivative being represented by general formula (I): wherein m=zero or 1, n=zero or 1, R1 is selected from hydrogen, methyl or ethyl, R2 is selected from hydrogen, SH or —SR0 wherein R0 is methyl, benzyl or glucose residue; Q is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring, wherein the substitution is understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ethyl or isopropyl; L is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring wherein the substitution is understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ethyl or isoprop

Abstract: The present invention provides novel aryl hydroxyethyl amides and related derivatives having the general Formula I 1

Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

Abstract: Bombesin receptor antagonists are provided which are useful for the diagnosis, prevention, or treatment of male sexual dysfunction in humans and animals, female sexual dysfunction in humans and animals, anxiety and panic disorders, social phobia, depression, psychoses, sleeping disorders, memory impairment, pulmonary hypertension, lung repair and lung development disorders, cancer including prostate cancer and pancreatic cancer, hepatic porphyria, gastrointestinal secretory disturbances, gastrointestinal disorders including colitis, Crohn's disease and inflammatory bowel disease, emesis, anorexia, pain, seasonal affective disorders, feeding disorders, or pruritus.

Abstract: The present invention is directed to compounds useful in the treatment of diseases associated with prenylation of proteins and pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising same, and to methods for inhibiting protein prenylation in an organism using the same.

Abstract: The invention describes novel substituted aryl compounds that are cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent, such as, steroids, nonsterodal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B4 (LTB4) receptor antagonists, leukotriene A4 (LTA4) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H2 antagonists, antineoplastic agents, antiplatelet agents, thrombin inhibitors, thromboxane inhibitors, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pyl

Abstract: The invention provides Aryl substituted imidazoles, pyrazoles, pyridizines and related compounds of the Formula 1

Abstract: The tris(hydroxymethyl)aminomethane (“TRIS”) salt of 3-(pyrimidin-5-yl)-9-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)-nonanoic acid is a potent antagonist of the integrin &agr;v&bgr;3 receptor and is useful for the prevention and/or treatment of osteoporosis and vascular restenosis, as well as conditions associated with excessive angiogenesis, such as macular degeneration, diabetic retinopathy, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth. The invention also relates to a process for the preparation of the novel salt as well as pharmaceutical compositions containing the salt and methods of using the salt.

Abstract: The present invention relates to a compound of formula (I): 1

Abstract: This invention provides compounds of formula 1, having the structure 1

Abstract: The active-matrix display contains a chiral smectic liquid-crystal mixture comprising at least one compound of the formula (I) R1—(A1—M1)a—(A2—M2)b—A3—X—B1—(B2)c—R2  (I). where the symbols are as defined in the description.

Abstract: The present invention provides novel 3-heterocyclic benzylamides and related derivatives having the general Formula I 1

Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides sulfonamides, and compositions and methods utilizing sulfonamides that are useful in the treatment of diseases by blocking potassium channels associated with the onset or recurrence of the indicated conditions. Exemplary diseases treatable with the compounds, compositions and methods of the invention include sickle cell disease and glaucoma.

Abstract: Substituted quinazolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Abstract: The present invention further relates to a method of inhibiting MRP1 in a mammal which comprises administering to a mammal in need thereof an effective amount of a compound of formula (I).

Abstract: The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which R1, R2, R3 and A are each as defined, and to processes for their preparation and to their use as medicaments, in particular as medicaments for the treatment of cardiovascular disorders.

Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.

Abstract: The invention provides 4-imidazol-1-ylmethyl pyrimidine of the formula 1

Abstract: The present invention provides novel heterocyclic amides and related derivatives having the general Formula I 1

Abstract: Disclosed are compounds of the formula: wherein R13 represents an imidazole ring; R14 represents a carbamate, urea, amide or sulfonamide group; R8 represents H when the alkyl chain between the amide group and the R13 imidazole group is substituted, or R8 represents a substituent such as arylalkyl, heteroarylalkyl or cycloalkyl; and the remaining substituents are as defined herein. Also disclosed are compounds wherein R8 is H, and the alkyl chain between the amide group and the R13 imidazole group is unsubstituted. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.

Abstract: The present invention relates to certain 4-heteroaryl-3-heteroarylidenyl-2-indolinones compounds and their physiologically acceptable salts which modulate the activity of protein kinases (“PKs”), in particular CDK2. The compounds of the present invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical composition containing these compounds and methods of preparing these compounds are also described.

Abstract: The present invention provides certain amide, carbamate and urea derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.

Abstract: Compounds of the formula (I): wherein Ring A, R1, R3, R4, p, q, and n are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) effect in a warm-quest-blooded animal, such as man.

Abstract: PDF inhibitors and novel methods for their use are provided.

Abstract: Benzanilides are provided which are voltage-dependent potassium channel openers. Methods of using the benzanilides of the invention are also provided.

Abstract: The present invention provides 2-methoxyimino-2-(pyridinyloxymethyl) phenyl acetamides according to formula (I) as well as their use as fungicidal compounds.

Abstract: Novel biphenyl and biphenyl-like cannabinoid compounds are presented. These compounds, when administered in a therapeutically effective amount to an individual or animal, result in a sufficiently high level of that compound in the individual or animal to cause a physiological response. The physiological response useful to treat a number of physiological conditions.

Abstract: Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.

Abstract: Novel &Dgr;1-pyrrolines of the formula (I) 1

Abstract: The present invention is directed to pharmaceutical compositions containing active compounds, which inhibit the activity of the chemokines, MIP-1&agr; and RANTES. It also is directed to methods of treating inflammatory and immunoregulatory disorders and diseases using these pharmaceutical compositions.

Abstract: Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the modulation of the cannabinoid receptors in animals are described herein.

Abstract: Compounds useful for the treatment of pain in accord with the following structural diagram, 1