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: 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: 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: Compounds having the formula: wherein L is a bond or (C1-C4)alkylene, R″ is hydrogen or (C1-C8)alkyl, and R1, R2, R4, R, R′, and the subscript n are as described herein, are provided, which are useful in the treatment and/or prevention of a condition or disorder mediated by a G-protein coupled receptor. Pharmaceutical compositions and methods of using these compounds for the treatment and/or prevention of a condition or disorder mediated by a G-protein coupled receptor, such as eating disorders, obesity, anxiety disorders and mood disorders, are also provided.

Abstract: Imidazonaphthyridine and tetrahydroimidazonaphthyridine compounds induce the biosynthesis of cytokines such as interferon and tumor necrosis factor. The compounds exhibit antiviral and antitumor properties. Methods of preparing the compounds and intermediates useful in the preparation of the compounds are also disclosed.

Abstract: The present invention relates to an anti-tumor agent containing a tubulin polymerization-inhibitory active substance and an anti-inflammatory active substance. The present invention also relates to an anti-tumor pharmaceutical preparation containing one or more tubulin polymerization-inhibitory active substance and/or anti-inflammatory active substance, which can be individually combined with one or more additional tubulin polymerization-inhibitory active substance and/or anti-inflammatory active substance. The present invention also relates to methods and therapeutic regimens for administering the same to a subject in need thereof.

Abstract: A salt of a codrug of at least two drug compounds covalently linked to one another via a labile bond to form a single codrug, and methods of use of the codrug salt for the treatment of various medical conditions. The codrug salt may be administered by itself or in the form of a bioerodible or nonbioerodible substance.

Abstract: The present invention provides compounds 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: 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: 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: 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: The invention provides compounds of formula I: 1

Abstract: The invention provides compounds of formula I: 1

Abstract: There are described tetrahydrocarbazoles of formula (1) or (2). The compounds are suitable as antimicrobial active ingredients.

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: Methods and composition are provided for treating cancer, the methods including the step a administering, either sequentially or simultaneously, (i) a compound of the xanthenone acetic acid group of compounds, and (ii) at least one compound selected from compounds which modulate TNF production and compounds which act on biochemical pathways leading to TNF synthesis. Compositions include a combination of (i) and (ii) above, together with acceptable pharmaceutical carriers and/or vehicles.

Abstract: A compound having the following structure: 1

Abstract: A method of inhibiting retroviral reverse transcriptase or hepadnaviral reverse transcriptase includes the step of administering a pharmaceutically effective amount of a mappicine analog or a pharmaceutically acceptable salt thereof.

Abstract: A composition is disclosed which, depending on the user, may take the form of a health food or a medicine, comprising a combination of the following as its characterising components: (a) L-carnitine inner salt or one of its pharmacologically acceptable salts; (b) acetyl L-carnitine inner salt or one of its pharmacologically acceptable salts; and (c) huperzine A or huperzine B or mixtures thereof or extracts of Huperzia serrata containing them, suitable for the prevention/treatment of learning disorders in children suffering form Attention Deficit/Hyperactive Disorder (ADHD).

Abstract: The invention is directed to a pharmaceutical composition and a corresponding method for inhibiting respiratory depression in a mammalian subject during treatment with opiates. The composition contains in combination, an opiate or opioid analgesic or anesthetic and a D1-dopamine receptor agonist in an amount sufficient to inhibit respiratory depression caused by the opiate or opioid.

Abstract: Imido and amido substituted acylhydroxamic acids which reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propanoylamino)propanoate.

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

Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.

Abstract: Novel polycyclic compounds of the formula [I], wherein R1, R2, R3, R4, R5, R6, R7, ring A, ring B, X, Y and Z are as defined herein and the pharmaceutically acceptable salts thereof. These compounds have antitumor activity and useful for the treatment of cancer.

Abstract: This invention is concerned with novel polycyclic compounds of formula [I], 1

Abstract: The present invention provides methods of reducing angiogenesis in an individual. The methods generally involve administering to the individual an effective amount of a nicotinic acetyl choline receptor antagonist. The methods are useful to treat conditions associated with or resulting from angiogenesis, particularly pathological angiogenesis. The invention further provides methods of treating a condition associated with or resulting from angiogenesis.

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: The invention relates to an animal feed which contains conventional animal feed substances like grain or grain products, maize, protein and aromatic amino acids, vitamins, mineral additives like salts, phosphates, lime, enzymes and the like, or an animal feed additive, whereby to reduce the enzymatic decomposition of the essential aromatic amino acids it contains one or more benzophenanthridine alkaloids or their derivatives or synthetic analogs in an effective amount. Furthermore the invention relates to the use of benzophenanthridine alkaloids, their derivatives or synthetic analogs and a medicament.

Abstract: The present invention provides a series of novel bifunctional molecules based on viologen linked acridine, bisacridine and bisacridinium salts of the general formula 1 (1a, 1b, 1c and 1d) and or pharmaceutically acceptable derivatives thereof, which can be used as phototherapeutic and catalytic photoactivated DNA cleaving agents. These molecules are very stable and exhibit high solubility in buffer at physiological conditions. They undergo strong binding with DNA through intercalation and groove binding interactions and show remarkably high affinity for poly(dA).poly(dT) sequences. Upon photoactivation, they cleave DNA catalytically and selectively at guanine (G) sites in duplex DNA exclusively through cosensitization mechanism with a preference for 5′-G over 3′-G. They induce unusally high specificity of cleavage at G site of the AG two base bulge sequences.

Abstract: The present invention relates to a composition useful for hepatoprotection, said composition comprising polar extract of plant Cryptolepis Buchanani and/or fractions of the said extract, and optionally pharmaceutically acceptable additives and a method of producing said composition and also a method of treating a subject using said composition.

Abstract: Disclosed is an agent for improving learning and/or memory, which is useful for therapy of dementia accompanying disorder of memory due to a cerebrovascular disease, neurodegenerative disease such as Alzheimer's disease, endocrine disease, nutritional or metabolic disorder, infectious disease, drug addiction or the like. The agent for improving learning and/or memory according to the present invention comprises as an effective ingredient an isoquinoline derivative having a specific structure, such as (4aR, 12aR)-2-methyl-4a-(3-hydroxyphenyl)-1,2,3,4,4a,5,12,12a-octahydro-quinoline[2,3-g]isoquinoline or a pharmaceutically acceptable salt thereof.

Abstract: Compounds according to formula I: T1—L—T2   (I), wherein T1 is a taxoid group, preferably of Formula II: wherein R1 is C6H5; R2 is O; L is a linking group; and T2 is a substituent selected from the group consisting of epipodophyllotoxin, amsacrine, ellipticine, anthracycline antibiotic, mitoxantrone, and colchicine groups, and pharmaceutically acceptable salts thereof, are provided herein. The compounds are useful in, among other things, treating tumors or cancer in subjects in need thereof, inducing cellular differentiation, and inhibiting cellular mitosis.

Abstract: A drug for curing or preventing mood disorder or anxiety disorder that has fewer and milder side effects comprising, as an effective component, an isoquinoline derivative or a physiologically acceptable acid addition salt thereof, the representative example of the isoquinoline derivative being (4aS, 12aS)-2-methyl-4a-(3-hydroxyphenyl)-1,2,3,4,4a,5,12,12a-octahydroquinolino [2,3-g]isoquinoline; a method for curing or preventing mood disorder or anxiety disorder using the same; and a use of the isoquinoline derivative or the physiologically acceptable acid addition salt thereof for the manufacture of a medicament for curing or preventing mood disorder and anxiety disorder.

Abstract: Polymeric conjugates of camptothecin derivatives having increased circulating half-lives are disclosed. In preferred aspects, the E ring lactone of the camptothecin derivative is opened and functionalized to allow attachment of a polymer such as PEG in the 17- or 20-position thereof. A representative example of such compounds is Methods of preparing and using the same are also disclosed.

Abstract: The present invention relates to the use of cilansetron for the treatment of non-obstipative male IBS patients.

Abstract: The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.

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: The invention is directed to a pharmaceutical composition and a corresponding method for inducing analgesia or anesthesia in a mammalian subject, while simultaneously inhibiting respiratory depression in the subject. The composition contains in combination, an opiate or opioid analgesic or anesthetic and a D1-dopamine receptor agonist in an amount sufficient to inhibit respiratory depression caused by the opiate or opioid.

Abstract: The invention discloses quaternary ante-iso acids useful as additives in personal care products. Various quaternary derivatives of ante-sio acids are described, and examples of their use in personal care composition are presented.

Abstract: Novel polycyclic compounds of the formula [I], 1

Abstract: Compounds having Formula I 1

Abstract: The invention relates to compound of formula (I): wherein: represents a single or double bond, R0 represents hydrogen or hydroxy or alkoxy, R1 and R2, which are identical or different, each represents hydrogen or halogen or alkyl, alkoxy, hydroxy, polyhaloalkyl, nitro or optionally substituted amino or  wherein m represents an integer such that 1≦m≦4, or form together with the carbon atoms carrying them an aromatic or non-aromatic, mono- or bi-cyclic group having from 5 to 12 ring members and optionally containing 1 or 2 hetero atoms selected from O, S and N, R3 represents hydrogen or aryl, heteroaryl, cycloalkyl, optionally substituted alkyl or a group of formula COR7 wherein R7 represents aryl, optionally substituted alkyl, optionally substituted amino or OR10 wherein R10 represents aryl or optionally substituted alkyl, X represents oxygen or sulphur or —CH2— or —CH2—CH2—, Ar represents aryl, heteroaryl or arylalkyl, its op

Abstract: The invention relates to the identification of cdk inhibitors as inhibitors of gene expression, replication and reactivation in pathogenic agents.

Abstract: Non-steroidal compounds that are high affinity, high selectivity modulators for androgen receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring androgen receptor agonist, partial agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the androgen receptor modulator compounds.

Abstract: The present invention provides a series of novel bifunctional molecules based on viologen linked acridine, bisacridine and bisacridinium salts of the general formula 1 (1a, 1b, 1c and 1d) and or pharmaceutically acceptable derivatives thereof, which can be used as phototherapeutic and catalytic photoactivated DNA cleaving agents. These molecules are very stable and exhibit high solubility in buffer at physiological conditions. They undergo strong binding with DNA through intercalation and groove binding interactions and show remarkably high affinity for poly(dA).poly(dT) sequences. Upon photoactivation, they cleave DNA catalytically and selectively at guanine (G) sites in duplex DNA exclusively through cosensitization mechanism with a preference for 5′-G over 3′-G. They induce unusally high specificity of cleavage at G site of the AG two base bulge sequences.

Abstract: A method for the preparation of a compound of general Formula: or pharmaceutically acceptable derivatives and salts, racemates, isomers and/or tautomers thereof comprising cyclizing an azomethine ylide of general Formula: wherein, A is a cyclic or non-cyclic group; Z is a carbon or a heteroatom; n is selected from 0, 1, 2, or 3; W, X and Y may be the same of different and each are selected from hydrogen; optionally substituted alkyl, alkenyl, alkynyl, amino, alkoxy, alkinoxy, alkynoxy, aryl, alkylthio, heterocyclyl; carboxy, carboxy ester, carboxamido, acyl, acyloxy, mercapto, halogen, nitro, sulfate, phosphate, cyano and optionally protected hydroxy; or W and X, together with the nitrogen and carbon atoms to which they are attached, form a saturated or unsaturated nitrogen containing heterocyclic group which may be optionally substituted or optionally fused to a saturated or unsaturated carbocyclic group, aryl group or heterocyclic group is provided.