Abstract: The present invention provides compounds useful for increasing cellular ATP binding cassette transporter ABCA1 production in mammals, and to methods of using such compounds in the treatment of coronary artery diseases, dyslipidiemias and metabolic syndrome. The invention also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.

Abstract: The invention provides novel classes of Isoquinoline Derivatives. Pharmaceutical compositions and methods of making and using the compounds, are also described.

Abstract: The present invention provides compounds useful for increasing cellular ATP binding cassette transporter ABCA1 production in mammals, and to methods of using such compounds in the treatment of coronary artery diseases, dyslipidiemias and metabolic syndrome. The invention also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.

Abstract: Compounds of the formula I, in which s, k, I, W, R1, R2, R3, and U have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.

Abstract: The present invention provides compounds useful for increasing cellular ATP binding cassette transporter ABCA1 production in mammals, and to methods of using such compounds in the treatment of coronary artery diseases, dyslipidiemias and metabolic syndrome. The invention also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.

Abstract: Compositions and methods for treating cancer and other hyperproliferatice disease conditions with topoisomerase inhibitors and their prodrugs are disclosed.

Abstract: The present invention provides fluorogenic probes and corresponding fluorescent compounds, methods of using the probes, compounds and kits that include the probes.

Abstract: The invention provides novel isomers of dihydrotetrabenazine, individual enantiomers and mixtures thereof wherein the dihydrotetrabenazine is a 3,11 b-cis-dihydrotetrabenazine. Also provided are methods for the preparation of the novel isomers, pharmaceutical compositions containing them and their use in treating hyperkinetic movement disorders such as Huntington's disease, hemiballismus, senile chorea, tic, tardive dyskinesia and Tourette's syndrome.

Abstract: This invention provides 6H-[1]benzopyrano[4,3-b]quinoline compounds having the formula I: The invention further provides compositions including the compounds, methods for the use of the compounds, and methods of preparation of the compounds.

Abstract: Various calcium channel blockers and pharmaceutical compositions containing these compounds are disclosed. Calcium channel blockers are compounds capable of inhibiting calcium ion channels. Methods for preparing calcium channel blockers and their use as calcium channel antagonists are also disclosed.

Abstract: The instant invention provides for compounds which comprise substituted triazoloquinazolinones that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.

Abstract: A process for preparing cyclopentadiene derivatives comprising the steps of: a) coupling a five membered heterocycle ring with a five or six membered heterocycle ring; b) reacting the obtained compound with a carbonilating system: c) reducing the obtained compound.

Abstract: Mono-ester and asymmetrically substituted diesters of dihydrexidine, dinapsoline and A-86929 and substituted derivatives thereof are described. The novel ester/diester derivatives exhibit improved pharmacokinetic characteristics relative to their unesterified parent compounds and can be formulated into pharmaceutical compositions useful for the treatment of a wide variety of dopamine related disorders.

Abstract: Substituted 5,6,6a,11b-tetrahydro-7-oxa-5-aza-benzo[c]fluorene-6-carboxylic acid compounds, and processes for the production thereof, pharmaceutical compositions containing these compounds and the use thereof in treatment methods and for the production of pharmaceutical preparations for specific indications, in particular for the treatment of pain.

Abstract: The present invention describes novel dyes, including coumarins, rhodamines, and rhodols that incorporate additional fused aromatic rings. The dyes of the invention absorb at a longer wavelength than structurally similar dyes that do not possess the fused aromatic rings. Many of the dyes of the invention are useful fluorescent dyes. The invention includes chemically reactive dyes, dye-conjugates, and the use of such dyes in staining samples and detecting ligands or other analytes.

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: 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: 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: This invention relates to non-steroidal tricyclic compounds that are modulators of androgen receptors and to methods for making and using such compounds.

Abstract: A compound having the Formula I wherein: R1 is independently selected from the group consisting of a straight chain alkyl group, a branched alkyl group, a cycloalkyl group, an alkoxy group, a monocyclic aromatic group, a polycyclic aromatic group, an alkylaryl group, or an arylalkyl group; R2 and R3 are independently selected from the group consisting of a straight chain alkyl group, a branched alkyl group, a cycloalkyl group, an alkoxy group, a monocyclic aromatic group, a polycyclic aromatic group, a heterocyclic group, an alkylaryl group, an arylalkyl group, an alkoxyaryl group, an arylalkoxy group, a halogen, and hydrogen; R4, R5, R6, R7, R8, R9, R10 and R11 are independently selected from the group consisting of a straight chain alkyl group, a branched alkyl group, a cycloalkyl group, an alkoxy group, a monocyclic aromatic group, a polycyclic aromatic group, an alkylaryl group, an arylalkyl group, an alkoxyaryl group, an arylalkoxy group, an aryloxy group, a halogen, and hydrogen.

Abstract: The present invention relates to compounds for the inhibition of poly(ADP-ribose) polymerase (PARP). In some embodiments, the compounds have the Formula: wherein the constituent variables are as defined herein. The invention further provides methods for the use of the compounds disclosed herein.

Abstract: Compounds having Formula I are useful for partially or fully antagonizing, repressing, agonizing, or modulating the glucocorticoid receptor and treating immune, autoimmune and inflammatory diseases in a mammal. Also disclosed are pharmaceutical compositions comprising compounds of Formula I and methods of inhibiting immune or autoimmune diseases in a mammal.

Abstract: (+)-Narciclasine (2), available in quantity from certain Amaryllidaceae species or by total synthesis, is employed in for a ten step synthetic conversion (3.6% overall yield) to natural (+)-pancratistatin (1a). The key procedures involve the epoxidation of natural (+)-narciclasine (2) to an epoxide (6), reduction of the epoxide (6) to diol (8), formation of cyclic sulfate (12) and its ring opening with cesium benzoate followed by saponification of the benzoate to afford (+)-pancratistatin (1a).

Abstract: Compounds of general structural formula (I), and use of the compounds or salts or solvates thereof as therapeutic agents, are disclosed

Abstract: Substituted 5,6,6a, 11b-tetrahydro-7-oxa-5-aza-benzo[c]fluorene-6-carboxylic acid compounds, and processes for the production thereof, pharmaceutical compositions containing these compounds and the use thereof in treatment methods and for the production of pharmaceutical preparations for specific indications, in particular for the treatment of pain.

Abstract: The invention provides novel classes of substituted Indeno[1,2-c]isoquinoline Compounds. Pharmaceutical compositions and methods of making and using the compounds, are also described.

Abstract: The instant invention provides potent antiandrogen compounds, such as 3&bgr;-acetoxyandrost-1,5-diene-17-ethylene ketal and 3&bgr;-hydroxyandrost-1,5-diene-17-ethylene ketal, and methods for their use in the prevention and treatment of biological conditions mediated by androgen receptors. Thus, for example, compounds of the invention are useful in the prevention and treatment of prostrate cancer. Furthermore, it has been discovered that compounds of the invention are useful in the prevention and treatment of androgen-independent cancers such as androgen-independent prostrate cancer. Finally, inventive compounds may be used to treat antiandrogen induced withdrawal syndrome.

Abstract: The invention relates to Tetracyclic Benzamide Derivatives; compositions comprising a Tetracyclic Benzamide Derivative; and methods for treating or preventing an inflammatory disease, a reperfusion disease, an ischemic condition, renal failure, diabetes, a diabetic complication, a vascular disease, or cancer, comprising administering to a subject in need thereof an effective amount of a Tetracyclic Benzamide Derivative.

Abstract: The present invention is an organic light emitting device (OLED) comprising an anode, a cathode and a luminescent region provided between the anode and the cathode. The luminescent region comprises an electron injection and transporting zone and at least one of a hole injection and transporting zone and a mixed charge transport layer. One or both of the electron injection and transporting zone and the mixed charge transporting layer comprises an azole compound represented by formula I and/or II. The provision of the novel azole compounds of the invention as electron transport materials within an organic electroluminescent device advantageously reduces power consumption and increases power conversion efficiency within the device and as such, are suitable for a variety of display applications.

Abstract: The invention relates to novel 2,4-dihydro-pyrrolo[3,4-b]quinolin-9-one derivatives of the formula (I) and (IV): wherein all variables are as herein defined, pharmaceutical compositions containing the compounds and their use for the treatment of sexual dysfunction.

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: 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: 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: The invention relates to novel polymorph crystal forms A and B of N-(2,3-dimethyl-5,6,7,8-tetrahydrofuro[2,3-b]quinolin-4-yl)-2-(2-oxopyrrolidin-1-yl)acetamide: 1

Abstract: An agent for inducing HSP, comprising a compound represented by the formula (I): 1

Abstract: A novel class of tetracyclic compounds is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.

Abstract: New derivatives of benzazepine, particularly of benzofuro[3a,3,2,ef][2]benzazepin of the general formula (I) 1

Abstract: A novel class of tetracyclic compounds is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock

Abstract: The invention provides novel classes of Isoquinoline Derivatives. Pharmaceutical compositions and methods of making and using the compounds, are also described.

Abstract: The present invention relates to substituted 1,4-dihydro-4-oxoquinolines having antiviral activity. The substituents are present at positions 1, 2 and at least one of 5-8 positions of the quinoline ring.

Abstract: The present invention relates to an efficient process for the preparation of 5-(substituted)-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-chromeno[3,4-f]quinolines.

Abstract: This invention relates generally to tetracyclic tetrahydroquinoline compounds, and analogues thereof, and pharmaceutically acceptable salt forms thereof, which are selective inhibitors of serine protease enzymes, especially factor VIIa; pharmaceutical compositions containing the same; and methods of using the same as anticoagulant agents for modulation of the coagulation cascade.

Abstract: A method for the preparation of a compound of general Formula: 1

Abstract: Compounds are provided that are amide analogs of SR141716A having unique CB1 receptor selectivity and providing WIN sparing binding characteristics, pharmaceutical compositions containing the compounds and their use in a method of treatment of CB1 receptor related disorders, such as obesity, schizophrenia, memory dysfunction and marijuana abuse.

Abstract: Compounds, compositions and methods are provided that are useful in the treatment and/or prevention of a condition or disorder mediated by a G-protein coupled receptor. In particular, the compounds of the invention are useful in the treatment and/or prevention of eating disorders, obesity, anxiety disorders and mood disorders.

Abstract: Methods of preparing amino-substituted-tetrahydroisoquinoline ring compounds include the steps of providing a support-bound amino-substituted-tetrahydroisoquinoline compound; forming an intermediate by reacting the support-bound amino-substituted-tetrahydroisoquinoline compound with a reagent; and cyclizatively cleaving the support-bound amino-substituted-tetrahydroisoquinoline compound to form the amino-substituted-tetrahydroisoquinoline ring compound.

Abstract: A process for preparing 1H-imidazo[4,5-c]quinolin-4-amines is disclosed. The process involves reacting a 6H-imidazo[4,5-c]tetrazolo[1,5-a]quinoline with triphenylphosphine and hydrolyzing the product thereof.

Abstract: The invention provides a novel class of substituted indeno[1,2-c]isoquinoline derivatives. Pharmaceutical compositions and methods of making and using the compounds, are also described.

Abstract: A substituted 1,2,3,4-tetrahydroquinoline-2-carboxylic acid derivative of formula I 1

Abstract: An aqueous solution of a pyrazoloacridone compound or pharmaceutical salt is stabilized using an acid, placing the solution in a well-closed container, evacuating air in the container, and sealing the container.