Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.

Abstract: New polymorphic crystal form of (R)-5-[2-(5,6-diethyl-indan-2-ylamino)-1-hydroxyethyl]-8-hydroxy-1H-quinolin-2-one maleate designated crystal form Qalpha that is useful in the treatment of inflammatory or obstructive airways diseases. A method for preparing crystal form Qalpha is also described.

Abstract: A compound of the having the general formula (I) or general formula (II): wherein Z, A, B, C, R1, R2, Q, W, and n are as described herein.

Abstract: The invention relates to novel chimeric antibiotics of formula I wherein R1 represents OH, OPO3H2 or OCOR5; R2 represents H, OH or OPO3H2; A represents N or CR6; R3 represents H or fluorine; R4 is H, (C1-C3) alkyl, or cycloalkyl; R5 is the residue of a naturally occurring amino acid, of the enantiomer of a naturally occurring amino acid or of dimethylaminoglycine; R6 represents H, alkoxy or halogen; and n is 0 or 1; and to salts (in particular pharmaceutically acceptable salts) of compounds of formula I. These chimeric compounds are useful in the manufacture of medicaments for the treatment of infections (e.g. bacterial infections).

Abstract: The present invention provides prodrugs of selective androgen receptor modulators (SARMs), and their use in treating or reducing the incidence of osteoporosis, a variety of hormone-related conditions, conditions associated with Androgen Decline in Aging Male (ADAM); conditions associated with Androgen Decline in Female (ADIF), and muscular wasting conditions, obesity, dry eye conditions, and prostate cancer. The prodrugs are also useful in oral androgen replacement therapy and male contraception.

Abstract: The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.

Abstract: This invention is directed to novel bicyclic compounds, to the uses of these compounds in various medicinal applications, including treating disorders amenable to treatment by peptidyl deformylase inhibitors such as treatment of bacterial infections, and to pharmaceutical compositions comprising these compounds.

Abstract: The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.

Abstract: The invention relates to compounds of the following formula that may be used to inhibits kinases, as well as compositions of matter and kits comprising these compounds. The present invention also relates to methods for inhibiting kinases, as well as treatment methods using compounds according to the present invention.

Abstract: Compounds of formula (I), or pharmaceutically acceptable salts thereof, are provided, wherein R1-R6 and X are defined herein. Also provided are methods of preparing the compounds of formula (I), pharmaceutical compositions and kits containing a compound of formula (I), as are methods of treating endometriosis, hormone-dependent carcinomas, leiomyoma, fibroids, dysfunctional bleeding, polycystic ovary syndrome, and menopause related symptoms; methods of contraception; methods of providing hormone replacement therapy; methods of stimulating food intake; methods of synchronizing estrus; and methods of treating symptoms of premenstrual syndrome and premenstrual dysphoric disorder by administering to a mammal in need thereof a pharmaceutically effective amount of a compound of formula (I).

Abstract: The present invention relates to Aripiprazole, a useful agent for antipsychotic. The present invention also provides new acid addition salts of Aripiprazole and process for the preparation of polymorphs and solvates of Aripiprazole using Aripiprazole acid salts, their interconversion and the process for preparation of Aripiprazole acid salts.

Abstract: The invention relates particularly to 2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof as a medicament, particularly as anti-cancer agents.

Abstract: A novel process for preparing highly pure cilostazol, effected by reacting 6-hydroxy-3,4-dihydroquinolinone and 5-(4-chlorobutyl)-1-cyclohexyl-1H-tetrazole in the presence of a hydrated inorganic base, is disclosed. Further disclosed is highly pure cilostazol, and particularly highly pure cilostazol that is substantially free of 6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)-butoxy]-1-[4-(1-cyclohexyl-1H-tetrazol-5-yl)-butyl ]-3,4-dihydro-1H-quinolin-2-one.

Abstract: The invention provides compounds of the formula: wherein X, Y, and Z are as defined in the specification. The compounds are effective anti-tumor agents. The invention also provides pharmaceutical compositions comprising a compound of the above formula or a salt thereof, intermediates useful for preparing a compound of the above formula, and therapeutic methods comprising administering a compound of the above formula or a salt thereof to a mammal in need thereof.

Abstract: The present application describes deuterium-enriched tafenoquine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: A process for preparing 8-substituted oxy-5-((R)-2-halo-1-hydroxy-ethyl)-(1H)-quinolin-2-ones or acceptable solvates thereof. The process involves reacting a 5-(?-haloacetyl)-8-substituted oxy-(1H)-quinolin-2-one with a reducing agent in the presence of a chiral agent and a base to form a 8-(substituted oxy)-5-((R)-2-halo-1-hydroxy-ethyl)-(1H)-quinolin-2-one, said chiral agent having a formula I or II wherein M, L, X, R1, R2 and R3 have the meanings as indicated in the specification.

Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein R1, X, Z, R2, X1, Ar, n, R3 and R4 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR8 and accordingly are useful for the treatment of a variety of inflammatory and allergic disorders.

Abstract: The invention provides compounds of the formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein m, p, q, r, A, E, X, Y, R1, R4, R5, R6, R7, R8, R9 and are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula I.

Abstract: Compounds of formula (I), and methods and/or compositions comprising compounds that are effective in modulating inflammatory responses, such as those resulting from AGE and glycated protein accumulation are provided. Methods and/or compositions comprising compounds that are effective in modulating smooth muscle cell proliferation and the diseases or conditions related thereto are also provided.

Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.

Abstract: The present invention relates to compounds of formula 1 wherein the groups n, m, B, X and R1 may have the meanings given in the claims and specification, processes for preparing them and their use as pharmaceutical compositions, particularly as pharmaceutical compositions for the treatment of respiratory complaints.

Abstract: The present invention features quinolones, tetrahydroquinolines, and related compounds that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions.

Abstract: The present invention relates to compounds of formula 1, wherein n, A, R1, R2 and R3 may have the meanings specified in the description and claims, processes for preparing them and their use as pharmaceutical compositions, particularly as pharmaceutical compositions for the treatment of respiratory complaints.

Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.

Abstract: The present invention relates to compounds of formula (I) as defined herein and salts or solvates thereof. Processes for preparing these compounds and pharmaceutical formulations containing them are also disclosed, as well as methods for the prophylaxis of treatment of a clinical condition using such compounds.

Abstract: The present invention provides a process for producing carbostyril derivatives (I) which are known to be useful as medical drug such as antithrombotic agent, cerebral circulation improver, anti-inflammatory agent, antiulcer agent, etc. in a high yield and a high purity. The carbostyril derivatives (I) can be produced by reacting a carbostyril derivative (II) with a tetrazole derivative (III) in the presence of a phase transfer catalyst.

Abstract: The present invention relates to bicyclic compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract: The invention encompasses synthesizing 7-(4-bromobutoxy)-3,4-dihydrocarbostyril by mixing 7-hydroxy-tetrahydroquinolinone, dibromobutane, and at least one base to form a reaction mixture; heating the reaction mixture; cooling the reaction mixture; and isolating the 7-(4-bromobutoxy)-3,4-dihydrocarbostyril from the reaction mixture. The invention also encompasses using phase transfer catalysts during the reaction.

Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.

Abstract: Compound of formula (I): wherein: R1, R2, R3, R4, R6, R8, R9 and R10, which may be the same or different, each represent a group selected from hydrogen, hydroxy, alkoxy, alkyl, arylalkoxy, alkoxycarbonylalkoxy and OR? wherein R? represents an ionised or ionisable group, R5 represents a group selected from alkyl, aryl and heteroaryl, R7 represents a group selected from hydrogen, hydroxy, alkoxy, alkyl and cycloalkyl, or R7 represents a nitrogen-containing or oxygen-containing heterocycle, its optical isomers, hydrates and solvates thereof and addition salts thereof, with a pharmaceutically acceptable acid or base. Medicinal products containing the same which are useful as anti-cancer agents.

Abstract: Compounds of formula (I): and salts, solvates, and physiologically functional derivatives thereof, useful for the prophylaxis or treatment of a clinical condition for which a selective ?2-adrenoreceptor agonist is indicated, for example asthma or chronic obstructive pulmonary disease (COPD).

Abstract: The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.

Abstract: This invention comprises the novel compounds of formula (I) wherein r, t, Y1, Y2, R1, R2, R3, R5, R6and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

Abstract: The present invention relates to compounds having a structure according to Formula I wherein n, m, z, R, R2, R3, R4, R5, R6, A, E, X, Y, a and b are as defined above; or an optical isomer, diastereomer or enantiomer thereof; a pharmaceutically acceptable salt, hydrate, or prodrug thereof.

Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.

Abstract: A quianazoline derivative having the formula (1): or a pharmaceutically acceptable salt thereof, which has a chymase inhibitory activity and suppresses the exacerbation of vascular permeability induced by chymase and useful as a medicament, and a pharmaceutical composition containing the same as an essential ingredient.

Abstract: Heterocyclic amides of formula (1) wherein: is a single or double bond; A is phenylene or heteroarylene; m is 0, 1 or 2; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy; R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R4 is independently selected from for example hydrogen, halo, nitro, cyano, hydroxy, C1-4alkyl, and C1-4alkanoyl; R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity.

Abstract: Hydroxy-imino derivatives of formula IIb are disclosed, in which R and R1 have the meanings given in the description.

Abstract: Novel compounds represented by the following formula (I) that act as a ligand to sigma receptor/binding cite and a medicament comprising the same as an active ingredient: wherein X represents an alkyl group, an aryl group, a heterocyclic group or the like; Q represents a group represented by —CH2—, —CO—, —O—, —CH(OR7)— or the like wherein R7 represents a hydrogen atom, an alkyl group or the like; n represents an integer of from 0 to 5; R1 and R2 each represent a hydrogen atom, an alkyl group or the like; B represents either of the following groups: wherein R3, R4, R5, and R6 each represent a hydrogen atom, a halogen atom, an alkoxyl group or the like; m represents 1 or 2; and the ring of: represents an aromatic heterocyclic ring.

Abstract: The present invention relates to compounds of formula 1 wherein the groups X, Ra, Rb, R1, R1?, R2, R2?, R2?, R2??, V and n may have the meanings given in the claims and in the specification, and the use thereof as pharmaceutical compositions, particularly for the treatment of inflammatory and obstructive respiratory complaints.

Abstract: This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula I in which R1a, R1b, R2a, R3a, R3b, R4, R5, R6, R7, A, Y, D, E, G, Y and Z are as defined in the specification. The compounds are useful in treating malignant tumours, for example, ovarian, stomach, colon, breast, adeno-, head and neck carcinomas, acute lymphocytic and myelocytic leukemia. In addition, these compounds are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases such as psoriasis and arthritis. Methods of use and preparation of the compounds are also described.

Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.

Abstract: The present invention relates to certain substituted heterocycles of Formula (200), wherein B, H, I, J and K together with the Ar5 form a ring containing at least one amide residue, and W, X, Y and Z together form a 2,4-thiazolidinedione, 2-thioxo-thiazolidine-4-one, 2,4-imidazolidinedione or 2-thioxo-imidazolidine-4-one residue; or a pharmaceutically acceptable salt thereof. The compounds are useful in the treatment of diseases such as type 2 diabetes, and related disorders of lipid and carbohydrate metabolism, including atherosclerosis. The compounds are also useful for treating diseases of uncontrolled proliferation, such as cancers in general, including breast cancer.

Abstract: The present invention is directed to a new class of 6-benzylsulfonamido-quinoline/chromene derivatives, to their use as androgen antagonists, and to formulations containing these androgen antagonists.

Abstract: The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I wherein W is C, CH or N, and the dotted line emanating from W indicates a bond when W is C and no bond when W is N or CH; R1 and R2 are independently selected from hydrogen and halogen, provided at least one of R1 and R2 is a halogen atom; R3 is selected from hydrogen, halogen, C1-6 alkyl, trifluoromethyl, C1-6 alkoxy, aryloxy, aralkoxy, hydroxy, amino, C1-6 alkylamino, di(C1-6 alkyl)amino, nitro and cyano n is 2, 3, 4 or 5; X is CH2, O, S, CO, CS, SO or SO2; and Q is a group of formula wherein Z is a chain of 3 to 4 chain members; wherein the chain members are selected from C, CH, CH2, CO, N and NH, provided that only one of the chain members may be N or NH, and said chain optionally containing one or two double bonds; hvad med acyl?? R4, R5, R6, R7, R8, R9 and R10 are independently selected from hydrogen, halogen, C1-6 alkyl, trifluoromethyl, C1-6 alkoxy, hydroxy, amino, C1-6 alkylamino, di(C1-6

Abstract: The present invention provides substantially pure cilostazol. The present invention also provides cilostazol particles that have reduced particle size.

Abstract: The present invention provides substantially pure cilostazol. The present invention also provides cilostazol particles that have reduced particle size.

Abstract: The present invention provides substantially pure cilostazol. The present invention also provides cilostazol particles that have reduced particle size.

Abstract: The present invention provides a process for producing cilostazol [I] in a high yield and a high purity, by reacting a carbostyril derivative [II] with a tetrazole derivative [III] in the presence of an inorganic basic compound in a solvent of water, wherein water is used in an amount of 3 to 7-fold weight to that of the carbostyril derivative [II] and the inorganic basic compound is used in an amount of 1 to 6 mol per mol of the carbostyril derivative [II].

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.