Abstract: A compound of the formula II wherein one of R1 and R2 is halo and the other is H or halo; R3 is C1-C4 straight or branched chain, optionally fluorinated, alkyl; R4 is H; or R3 together with R4 and the adjoining backbone carbon defines: a spiro-C5-C7 cycloalkyl, optionally substituted with 1 to 3 substituents selected from halo, hydroxyl, C1-C4 alkyl or C1-C4 haloalkyl; or optionally bridged with a methylene group; or a C4-C6 saturated heterocycle having a hetero atom selected from O, NRa, S, S(?O)2; where Ra is H, C1-C4 alkyl or CH3C(?O); R5 is independently selected from H or methyl; E is —C(?O)—, —S(?O)m—, —NR5S(?O)m—, —NR5C(?O)—, —OC(?O)—, R6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or heterocycle; m is independently 0,1 or 2; are inhibitors of cathepsin K and useful in the treatment or prophylaxis of osteoporosis.

Abstract: The present invention relates to a method of treating cancer using PARP inhibitors as radio-sensitization agents of tumors. Specifically the present invention relates to a method of radio-sensitization of tumors using a compound of Formula (I) or a pharmaceutically acceptable salt form thereof. The present invention also relates to a pharmaceutical compositions of PARP inhibitors for radiosensitizing tumors.

Abstract: Disclosed are fungicidal mixtures, compositions and methods for controlling plant diseases relating to combinations comprising (a) N-[2-(1,3-dimethyl-butyl)-3-thienyl]-1-methyl-3-(tri-fluoromethyl)-1H-pyrazole-4 carboxamide (including all stereoisomers) or an agriculturally suitable salt thereof; and (b) at least one compound selected from the group consisting of compounds of Formula III or Formula IV which act at the bcl complex of the fungal mitochondrial respiratory electron transfer site; (INSERT FORMULA III HERE) (INSERT FORMULA IV HERE) wherein W, A, B, D and R5? are disclosed in this specification, and agriculturally suitable salts thereof; and optionally (c) at least one compound selected from the group of compounds acting at the demethylase enzyme of the sterol biosynthesis pathway and agriculturally suitable salts thereof.

Abstract: The present invention is directed to pharmaceutical methods for the treatment of CD30 positive diseases, such as Hodgkin's disease, by administration of a combination of at least one sheddase inhibitor and at least one anti-CD30 immunotherapeutic.

Abstract: The present invention relates to novel tetracyclic arylalkyl indoles, their derivatives, their analogues, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, novel intermediates described herein and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel tetracyclic arylalkyl of the general formula (I), their derivatives, their analogues, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, novel intermediates described herein and pharmaceutically acceptable compositions containing them. This invention also relates to process/es for preparing such compound/s of general formula (I), composition/s containing effective amount/s of such a compound and the use of such a compound/composition in therapy.

Abstract: The present invention relates to 1,3-dioxoisoindole derivatives of Formula (1) or pharmaceutically acceptable salts thereof, a preparation method thereof and use thereof as a T-type calcium channel antagonist, based on the fact that 1,3-dioxoisoindole derivatives of Formula (1) show selective antagonistic activity against T-type calcium channel, thus being effective in treating brain diseases, cardiac diseases and neurogenic pains: wherein R1 is a phenyl or a benzyl group, optionally substituted with a moiety selected from the group consisting of a halogen atom, a C1-C6 alkoxy, a C1-C6 alkyl, and a cyano group; R2 is a heterocyclic group selected from the group consisting of piperidinyl, pyrrolidinyl, morpholinyl, and piperazinyl groups, wherein the heterocyclic group is optionally substituted with a C1-C6 alkyl group; and n is 1 or 2.

Abstract: Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions comprising the compounds are also described as well as methods of preparing the compounds.

Abstract: The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system

Abstract: Pyrrolo[3,4-c]pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 and R5 are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.

Abstract: A compound of formula (I): wherein: R1 and R2 together form a benzo ring optionally substituted by halogen or by alkyl, alkoxy, cyano, nitro, hydroxy, amino, alkylamino, dialkylamino or trifluoromethyl, and R3 and R4 represent hydrogen, or R1 and R4 represent hydrogen and R2 and R3 together form a benzo ring optionally substituted by halogen or by alkyl, alkoxy, cyano, nitro, hydroxy, amino, alkylamino, dialkylamino or trifluoromethyl, or R1 and R2 represent hydrogen and R3 and R4 together form a benzo ring optionally substituted by halogen or by alkyl, alkoxy, cyano, nitro, hydroxy, amino, alkylamino, dialkylamino or trifluoromethyl, addition salts thereof with a pharmaceutically acceptable acid or base, and methods of treating conditions susceptible to ?2-AR/5-HT2C antagonists.

Abstract: Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).

Abstract: Novel piperazine and homopiperazine derivatives are agonists of melanocortin receptor(s) and are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of the melanocortin receptors. The compounds of the present invention are therefore useful for treatment or prevention of diseases and disorders such as obesity, diabetes, and sexual dysfunction.

Abstract: The present invention relates to a novel 1,4-disubstituted piperazine derivatives of Formula I, and their pharmaceutically acceptable acid addition salts having excellent uro-selective ?1-adrenoceptor antagonistic activity exceeding those of previously described compounds. The compounds of the present invention hold promise for treating the symptoms of benign prostatic hyperplasia (BPH). The invention also relates to methods for making the novel compounds, pharmaceutical compositions containing the compounds, and method of treating the symptoms of benign prostatic hyperplasia using the compounds.

Abstract: This invention relates to a series of arylsubstituted piperazines, of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the ?-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this and other disease.

Abstract: This invention relates to new piperazine derivatives of general formula I, in which V, W, n, R, R?, i, j, Y and Z have the meaning that is indicated in the description. The compounds according to the invention are distinguished by a diazacycloalkane substituent. They have at their disposal a special action with respect to the action that destabilizes the androgen receptor and can be used, for example, for treating prostrate cancer.

Abstract: The present invention is directed to imidazolyl derivatives of the formula: where the substituents are defined in the specification, or a pharmaceutically acceptable salt thereof. The derivatives bind selectively to the somatostatin subtype receptors and elicit either an agonist or antagonist effect from the somatostatin subtype receptors.

Abstract: The present invention relates to the synthesis of a new class of indeno [1,2-c]pyrazol-4-ones of formula (I): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

Abstract: Compounds of the formula: are disclosed as ligands for neuropeptide Y receptors and as such are useful in the treatment of obesity and disorders of the central nervous system.

Abstract: The invention encompasses novel N-alkyl-hydroxamic acid-isoindolyl compounds, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions for treatment or prevention of various diseases and disorders, for example, diseases associated with PDE4.

Abstract: This invention relates to compounds of formula (I) wherein R2 to R10, —X—Y—, A, —W—, n and p have the values defined in claim 1, their preparation and use as pharmaceuticals.

Abstract: Compounds of formula (I): and medicinal products containing the same which are useful as dual &agr;2/5-HT2c antagonists.

Abstract: Prodrugs of a glycogen phosphorylase inhibiting compounds are provided, said prodrug compounds having the formula I

Abstract: This invention is directed to pharmaceutical compositions useful in treating heart transplant rejection in mammals comprising a pharmaceutically acceptable excipient, a therapeutically effective amount of a non-peptide CCR1 receptor antagonist and a sub-nephrotoxic amount of cyclosporin A.

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: The invention relates to the mesylates of a group of piperazine derivatives and to a process for the preparation of these mesylates in an economic way in the high yield and of high purity. According to the process of the invention the synthesis of the piperazine ring and the mesylate formation are combined in a single reaction step. The invention relates to the mesylate of compounds of the formula (I) wherein X is a bicyclic heterocyclic phenyl group and Y is methyl, ethyl (optionally substituted with fluorine), cycloalkyl (3-7C) methyl, benzyl or m-phenyl benzyl.

Abstract: A compound represented by the formula (I) [A represents a 5- to 7-membered hydrocarbon ring group; L represents —NR3—CO—, —CO—NR3— and the like (R3 represents a hydrogen atom, a lower alkyl group, a lower acyl group and the like); M represents an alkylene linking group (a carbon atom constituting the carbon chain may be replaced with a nitrogen atom, an oxygen atom and the like); X represents —S—, —O—, —NR4—, —NR5—CO— and the like (R4 and R5 represent a hydrogen atom, a lower alkyl group and the like) or a single bond; Y represents an alkyl group, an aryl group, an amino group, an aromatic heterocyclic group and the like; R1 represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group or a lower acyl group; and R21, R22 and R23 represent a hydrogen atom, a hydroxyl group, a lower alkyl group and the like] or a salt thereof.

Abstract: Certain thienopyrrolyl and furanopyrrolyl compounds are disclosed as useful to treat or prevent disorders and conditions mediated by the histamine H4 receptor, including allergic rhinitis.

Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 and R5 are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1&bgr; secretion.

Abstract: A compound of formula I 1

Abstract: Novel piperazine and homopiperazine derivatives are agonists of melanocortin receptor(s) and are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of the melanocortin receptors. The compounds of the present invention are therefore useful for treatment or prevention of diseases and disorders such as obesity, diabetes, and sexual dysfunction.

Abstract: This invention relates to novel, pharmaceutically active compounds of formula (I) wherein a, b and R1 through R6 are as defined in the specification These compounds exhibit central dopaminergic activity and are useful in the treatment of CNS disorders.

Abstract: A method for delivering a melanocortin-4 receptor agonist to a mammalian subject, includes administering the melanocortin-4 receptor agonist to a tissue inside the nasal cavity or sinuses of the mammalian subject. In some instances, the melanocortin-4 receptor agonist includes a guanidine functional group.

Abstract: The invention relates to new &agr;-arylethylpiperazine derivatives, which are useful as neurokinin receptor antagonists (NK1antagonists). It also relates to processes for the preparation of said &agr;-arylethylpiperazine derivatives, to their use for the prevention and/or treatment of a condition associated with pathogical levels of substance P in a patient and to pharmaceutical compositions containing them.

Abstract: Compounds of formula I, 1

Abstract: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytoxic drugs in a targeted fashion.

Abstract: Compound of formula (I): 1

Abstract: The present invention relates to an indole derivative having the formula 1

Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract: This invention is directed to acyl piperazine derivatives, for example, of the following formula (Ia): wherein R1a, R2, R3, R4, R5, and R6 are described herein. These derivatives are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the derivatives, and methods of using the derivatives to treat inflammatory disorders in humans.

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

Abstract: The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I 1

Abstract: Compounds of formula I: 1

Abstract: Disclosed are compounds of the formula 1

Abstract: Disclosed are 1-Azatricyclic-4-benzylpiperazine compounds which are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.

Abstract: Tricyclic sulfonamide compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, collagenase-3, and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurysm, heart failure, left ventricular dilation, restenosis, periodontal disease, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.

Abstract: The present invention relates to a novel 1,4-disubstituted piperazine derivatives of Formula I, 1

Abstract: The compounds of the formulas described herein, wherein X, R0, R1, R2, n and m have the meanings given in the specification, are useful as active ingredients in pharmaceutical compositions. The invention relates to the use of said compounds as a medicament and for the manufacture of a medicament for the treatment of erectile dysfunction.

Abstract: Isoindolin-1-one-substituted propionamide glucokinase activators which increase insulin secretion in the treatment of type II diabetes.

Abstract: Optically active tetrahydrobenzindole type compounds having affinity for a 5-HT receptor, useful for prevention and treatment of mental diseases. A species compound is (S)-2a-4-(4-(2-methoxyphenyl)piperazinyl)butyl)-2a,3,4,5,-tetrahydro 1 H-benz[cd]indol-2-one.