Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R2 to R4, L, Q and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.

Abstract: This invention relates to methods for controlling parasitic infestations of animals and their environments, and, more particularly, to methods using isoxazolines to control parasites in or on animals or in their environments, as well as treat parasitoses of animals. The isoxazolines include 4-(isoxazolinyl)-benzamides (specifically, substituted 4-(5-(halomethyl)-5-phenylisoxazolin-3-yl)-benzamides) and 4-(isoxazolinyl)-benzothioamides (specifically, substituted 4-(5-(halomethyl)-5-phenyl-isoxazolin-3-yl)-benzothioamides). This invention also relates to compositions comprising the isoxazolines for use in such methods, the use of the isoxazolines to make medicaments for use in such methods, and kits comprising the isoxazolines for carrying out such methods. This invention further relates to the use of the isoxazolines as medicaments, particularly medicaments that can be used in the above-referenced method.

Abstract: To find a therapeutic agent and/or a preventive agent for diabetes mellitus or the like having excellent activity and safety. A compound represented by the following general formula (I), or a pharmacologically acceptable salt thereof. In the formula, X represents ?C(R5)- or ?N—; Y represents —O— or —NH—; L represents a bond or a substitutable C1-C3 alkylene group; M represents a substitutable C3-C10 cycloalkyl group, a substitutable C6-C10 aryl group, or a substitutable heterocyclic group; R1 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C6 haloalkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C1-C6 aliphatic acyl group, a C1-C6 alkoxy C1-C6 alkyl group, or a C6-C10 aryl group; and R2, R3, R4, and R5 may be the same or different and each represent a hydrogen atom, a halogen atom, a C1-C3 alkyl group, a C1-C3 haloalkyl group, a C1-C3 alkoxy group, or a nitro group.

Abstract: The present invention relates to compounds of formula wherein Ar, Het, R1 and n are as defined herein and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. Compounds of formula I are orexin receptor antagonists and are useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder and sleep disorders associated with neurological diseases.

Abstract: It is intended to provide novel amine compounds which are efficacious against diseases such as infection with HIV virus, rheumatism and cancer metastasis. Namely, amine compounds represented by the following general formula (1): In a typical case, A1 and A2 represent each an optionally substituted monocyclic or polycyclic aromatic heterocycle; W represents cyclic C3-10 alkylene, an optionally substituted monocyclic or polycyclic aromatic heterocycle, a monocyclic or polycyclic aromatic ring or a partly saturated polycyclic aromatic ring; X represents O, CH2, C(?O) or NR11; and D is a group represented by the following general formula (4) or (6). In the formula (6), Q represents a single bond, S, O or NR12; and Y is a group represented by the following general formula (7). —(CR18R19)m3— Or —(CR20R21)m4-z-(CR22R23)m5??(7) z represents an optionally substituted monocyclic or polycyclic aromatic ring. In the formula (6), B represents NR25R26.

Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula (I), and G, X1, X2, R1, R2, R3, R4, R4?, R5, Ra, Rb, and Rc are as described herein.

Abstract: The invention relates to a compound of formula (I): or a tautomer thereof or a pharmaceutically acceptable salt thereof, wherein R1 to R11, W, X, Y, Z, and n are as defined herein. The invention also relates to methods of using the compounds of formula (I) and compositions thereof to treat various diseases and disorders in a patient. The invention also relates to processes for preparing the compounds of formula (I) and intermediates useful in these processes.

Abstract: The invention provides a homocysteine synthase inhibitor useful for the prophylaxis or treatment of diseases involving homocysteine synthase. The homocysteine synthase inhibitor is a compound of the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof.

Abstract: The present invention relates to modulation of the ?7 nicotinic acetylcholine receptor (nAChR) by a compound of List A or a salt thereof, which may be represented, but is not limited to the compound N-[(2-Trifluoromethyl-1H-indol-5-yl)methyl]-5-(trifluoromethyl)-2-pyrimidinecarboxamide.

Abstract: A compound comprising or a pharmaceutically acceptable salt thereof, or a prodrug thereof is disclosed herein. Y, A, and B are as described herein. Methods, compositions, and medicaments related to these compounds are also disclosed.

Abstract: This invention relates to compounds and methods for the inhibition of HDAC enzymatic activity. More particularly, the invention provides for compounds of formula (I), (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein L, M, n, R, W, X and Y are as defined in the specification.

Abstract: The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).

Abstract: The present invention is directed to 1,3,4-oxadiazalones, compounds of formula I and their pharmaceutically acceptable salts stereoisomers, tautomers, or solvates thereof. Novel compounds include those of formula I, in which radicals are as defined herein. The compounds of this invention are modulators of PPARdelta and therefore useful as pharmaceutical agents, especially for the treatment of demyelinating diseases and disorders of fatty acid metabolism and glucose utilization.

Abstract: Epothilone derivatives of Formula (I) and their use as a pharmaceutical.

Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein Q and Z are as defined in the disclosure comprising distilling water from a mixture comprising a compound of Formula 2, a compound of Formula 3, a base comprising at least one compound selected from the group consisting of alkaline earth metal hydroxides of Formula 4 wherein M is Ca, Sr or Ba, alkali metal carbonates of Formula 4a wherein M1 is Li, Na or K, 1,5-diazabicyclo[4.3.0]non-5-ene and 1,8-diazabicyclo[5.4.0]undec-7-ene, and an aprotic solvent capable of forming a low-boiling azeotrope with water.

Abstract: The invention concerns a compound of the formula (I) wherein Ring A is heterocyclyl; m is 0-4 and each R1 is a group such as hydroxy, halo, trifluoromethyl and cyano; R2 is halo and n is 0-2; and each R4 is a group such as hydroxy, halo, trifluoromethyl and cyano; p is 0-4; and R3 is amino or hydroxy; or pharmaceutically-acceptable salts or in-vivo-hydrolysable ester or amide thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical condions mediated by histone deacetylase.

Abstract: The present invention relates to processes for making epothilone compounds and analogs thereof, such as epi-epothilone A or epi-epothilone B, and aziridinyl-epothilone analogs.

Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.

Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.

Abstract: The present invention relates to the purification of (2S,3S,5S)-5-amino-2-N,N-dibenzylamino-3-hydroxy-1,6-diphenylhexane (III) by making its crystalline acid addition salt, which can be used as such to produce Lopinavir/Ritonavir with high purity and yield.

Abstract: The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, wherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.

Abstract: The present invention provides novel compounds with histamine-H3 receptor antagonist or inverse agonist activity. In particular, the invention provides a compound of Formula I, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and intermediates and methods for making these compounds. The invention provides methods of using compounds and pharmaceutical compositions to treat obesity, cognitive deficiences, narcolepsy, and other histamine H3 receptor-related diseases.

Abstract: The present invention relates to epothilones C, D, E, and F, their preparation and their use for the production of therapeutic compositions and compositions for plant protection.

Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, are suitable for use as herbicides.

Abstract: The invention relates to the substituted 1,2-ethylenediamines of general formula (I), wherein the groups R1 to R13, A, B, L and i are defined as in the description and the claims. The invention also relates to the use thereof in the treatment of Alzheimer's disease (AD) and similar diseases.

Abstract: The invention relates to aryl-substituted polycyclic amines of formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof; where the symbols and radicals are explained in the description, as well as to pharmaceutical compositions containing them and to methods of treatment using them.

Abstract: The present invention relates to compounds of general formula (I) as tublin polymerisation inhibitors and methods for preparing such compounds.

Abstract: The present invention relates generally to novel therapeutic compounds and more particularly to novel compounds, their use as GPR40 agonists, processes for their manufacture, and intermediates useful in their preparation.

Abstract: The present invention comprises phenyl-[1,2,4]-oxadiazol-5-one derivatives of the general formula I: wherein the R1-R10 and B, U, V, W, X, Y and Z substituents are defined herein. The claimed invention also comprises the compounds isomers and their physiologically acceptable salts as well as processes for their preparation. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

Abstract: The present invention relates to novel thiazole-substituted indolin-2-ones as inhibitors of CSCPK and related kinases; to methods of inhibiting cancer stem cells by using a kinase inhibitor; to pharmaceutical compositions containing such compounds; and to methods of using such compounds in the treatment of a protein kinase related disorder in a mammal; and to processes of making such compounds and intermediates thereof.

Abstract: The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating of Alzheimer's disease.

Abstract: The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.

Abstract: The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating of Alzheimer's disease.

Abstract: There is provided a composition comprising a compound represented by general formula (I), wherein Rl represents a 5-iodothiophen-2-yl group or the like, and R2 represents a 4-dimethylaminophenyl group or the like. This composition is useful for diagnosis of an amyloid-related disease such as Alzheimer's disease because the compound has high binding specificity to amyloid ? protein, high permeability through the blood-brain barrier, and a property of being rapidly eliminated from sites other than senile plaques in the brain.

Abstract: Novel compounds of formula 1 or a pharmaceutically acceptable salt thereof inhibit cytochrome P450 monooxygenase.

Abstract: Pyrandione, thiopyrandione and cyclohexanetrione compounds of formula (I), which are suitable for use as herbicides.

Abstract: Epothilone derivatives of Formula (I) and their use as a pharmaceutical.

Abstract: A method of providing a range of flavors to an orally-receivable or ingestible product, the method including adding at least one compound, including salts thereof, of the formula: wherein R1 may be H, OH, O(CH2)2OH, OCH2OCH3 or R2 may be selected from a range of 5- and 6-membered heterocyclic rings, and wherein R3 may be H or OH. The compounds give rise to a wide range of flavors, and some are useful as sweetness enhancers, this allowing sweetener content to be reduced while maintaining sweetness. Also disclosed are orally-receivable or ingestible products including the compounds.

Abstract: The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.

Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.

Abstract: The present invention relates to a compound represented by formula (I): wherein ring A, ring B and ring D each independently represents a cyclic group which may have a substituent(s); W is a spacer having 1 to 8 atom(s) in its main chain; X is a spacer having 1 to 2 atom(s) in its main chain; Y is a binding bond or a spacer having 1 to 8 atom(s) in its main chain; and Z is an acidic group, or a salt thereof, a solvate thereof or a prodrug thereof. The compound represented by formula (I) has a PPAR ? agonistic action and is useful as a preventive and/or treating agent for diseases where sugar and lipid metabolisms are abnormal (diabetes, hyperlipemia, arteriosclerosis, cardiovascular diseases, obesity and metabolic syndrome or the like), hypertension, circulatory diseases and skin inflammation diseases.

Abstract: The invention provides methods and intermediates that are useful for preparing a compound of formula I: and salts thereof.

Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein R1 is CHX2, CX3, CX2CHX2 or CX2CX3; each X is independently Cl or F; Z is optionally substituted phenyl; and Q is phenyl or 1-naphthalenyl, each optionally substituted as defined in the disclosure; comprising contacting a compound of Formula 2 with hydroxylamine in the presence of a base. The present invention also relates to novel compounds of Formula 2, useful as starting materials for the aforedescribed method.

Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein G, B, Y, and A are as described. Methods, compositions, and medicaments related thereto are also disclosed.

Abstract: The invention relates to azoloarine derivatives of formula I wherein R, A, B, D, Y, X, M and W are as defined herein, and their physiologically tolerated salts.

Abstract: The disclosure provides compounds and compositions, and methods of using these compounds and compositions, for the targeted delivery of chemotherapeutic agents.

Abstract: The present invention relates to epothilone derivatives, having the following formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.

Abstract: The present invention relates to epothilone derivatives, having the following formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.

Abstract: The present invention relates to epothilone derivatives, having the following formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.

Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.