Abstract: Compounds and methods useful for the synthesis of (+)-discodermolide, a naturally occurring microtubule stabilizing agent useful as an anti-cancer agent.

Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of the dimeric mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.

Abstract: A method of synthesizing aromatic ketone compositions of formula I comprising the step of introducing a double bond into the 5 membered ring of the 4,5-dihydro-1,3-azoles moiety of formula II is disclosed. A method of synthesizing aromatic ketone compositions of formula I comprising the step of ring synthesis of the tetrahydro-1,3-azoles of formula XI is also disclosed.

Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: wherein R1, R2, R3 and R4 are as defined herein.

Abstract: A polymer-carrying optically active binaphthyl type oxazoline compound having axial asymmetry, represented by the following general formula (1) (wherein R1 and R2 may be the same or different from each other and each represents a hydrogen atom, an alkyl group having from 1 to 6 carbon atoms or the like; R3 is a hydrogen atom or —R5—X—R6; R4 is a hydrogen atom or the like; R5 is a straight- or branched-chain aliphatic hydrocarbon chain which may have a directly or indirectly bonded substituent; X is CH2, CO2, O, CONR7 or NR7; R6 is a directly or indirectly bonded polymer; and R7 is a hydrogen atom or the like), and to a transition metal complex which uses the compound as the ligand.

Abstract: The invention relates to vitamin D derivatives of general formula I, process for their production, intermediate products of the process as well as the use for the production of pharmaceutical agents.

Abstract: The invention relates to novel ligands of the phosphanylbenzothiophenyl-dihydroisoxazoline, phosphanyl-dihydrooxazolyl-indole and phosphanyl-dihydrooxazolyl-benzofuran type, especially compounds of formula I and mixtures of such compounds, wherein X is oxygen, sulfur, selenium or NQ, wherein Q is unsubstituted or substituted aryl, or alkyl or substituted alkyl; n is 0, 1, 2, 3 or 4; A1 and A2 are each an organic radical capable of bonding to phosphorus, especially unsubstituted or substituted alkyl, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl, unsubstituted or substituted cycloalkyl, or —N(D)2 wherein D2 is alkyl or substituted alkyl; or A1 and A2 together with the bonding phosphorus atom form a ring, which may be unsubstituted or substituted; Y, Y?, Y? and Y?? are each independently of the other hydrogen or alkyl, substituted alkyl, unsubstituted or substituted aryl, or unsubstituted or substituted heterocyclyl, at least one of the radicals Y, Y?, Y? or Y?? being one of

Abstract: Disclosed is a method of preparing a composition comprising a compound represented Structural Formula (I): The method comprises the step of reacting an aldehyde compound R10CHO with an isonitrile compound represented by Structural Formula (II):

Abstract: There is a significant demand for organic nitriles, based on their versatility in reactions. Compounds prepared from nitriles have properties including superoxide inhibition, ferrielectric liquid crystal dopant, antipicornaviral agents, anti-inflammatory agents, anti-asthma agents, and fibringoen antagonists. The present invention discloses a facile synthesis for 2,4-dihydroxybenzonitrile, and ethers and diethers thereof, from 2,4-dihydroxybenzoic acid. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, 2,4-dihydroxybenzonitrile is condensed with (S)-2-methylcysteine.

Abstract: Composition, article of manufacture for and method of treating malaria in a human having an infestation of Plasmodium protozoans are described. The method comprises administering a therapeutically-effective amount of a compound of formula (I) or (IV), i.e. sufficient quantity to reduce the population of Plasmodium. The composition of the invention is a compound of formula (I) or (IV) with a pharmaceutical excipient. The article of manufacture is the composition in combination with labeling for treating malaria. The substituents are detailed in the specification.

Abstract: The present invention provides antibacterial agents of formula I described herein and intermediates for their preparation.

Abstract: The invention is directed to physiologically active compounds of general formula (I): wherein: R1 represents aryl, heteroaryl or a group R3—L2—Ar1—L3—; R2 represents hydrogen or lower alkyl; R3 represents aryl or heteroaryl; and Ar1 represents an optionally substituted saturated, partially saturated or fully unsaturated 8 to 10 membered bicyclic ring system containing at least one heteroatom selected from O, S or N; Y is carboxy or an acid bioisostere; and their corresponding N-oxides or prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their corresponding N-oxides or prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (&agr;4&bgr;1).

Abstract: There is disclosed an advantageous mixed acid anhydride production method of formula (1): R1C(O)OY(O)n(R2)p  (1) wherein R1, R2 and Y denote the same as defined below, n and p denote an integer of 1 or 2, which is characterized by adding a carboxylic acid of formula (2); R1COOH  (2) wherein R1 denotes a hydrogen atom, an optionally substituted alkyl group or the like, an organic base to a solution of a carboxylic acid activating agent of formula (3); (R2)pY(O)nX  (3) wherein R2 denotes an optionally substituted aliphatic hydrocarbyl group or the like, Y denotes a carbon atom, a phosphorus atom, or a sulfur atom, and X denotes a chlorine atom or the like.

Abstract: A polymer-carrying optically active binaphthyl type oxazoline compound having axial asymmetry, represented by the following general formula (1) 1

Abstract: The present invention relates to a benzoxazole compound represented by the following formula (1): wherein R1 to R4 each represents hydrogen atom, C1-6 alkyl group, C1-4 alkoxy group, C1-4 haloalkyl group, C1-4 haloalkoxy group, halogen atom, nitro group, cyano group, etc.; R5 represents C1-4 haloalkyl group, C1-4 haloalkoxy group, halogen atom, nitro group, cyano group, etc.; R6 represents hydrogen atom, halogen atom, cyano group, nitro group, etc.; R7 represents hydrogen atom, C1-6 alkyl group, C1-4 haloalkyl group, etc.; and X represents O, S, SO or SO2, a process for producing the same and a herbicide containing the same as an effective ingredient.

Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 4-pyrone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.

Abstract: The present invention relates to novel 1-phenylbenzimidazole derivatives having particular alkoxycarbonyl substituents in the 5-position of the benz ring and having particular cyclic substituents in the meta-position of the phenyl ring, as well as to pharmaceutical compositions containing these compounds and to methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of GABAA receptor complex, and in particular for inducing and maintaining anaesthesia, sedation, and muscle relaxation, as well as for combating febrile convulsions in children. The compounds of the invention may also be used by veterinarians.

Abstract: Imidazol-4-ylmethanols and their uses for preventing and treating primary tumors, metastasis and recurrence of tumors, various symptoms accompanying tumors, prostatic hypertrophy, virilism, hirsutism, male pattern alopecia, precocious puberty, endometriosis, uterine myoma, mastopathy and polycystic ovary syndrome are disclosed.

Abstract: Compounds of the formula (I), are described in which X is halogen, cyano, nitro, (C1-C4)-alkyl, (C1-C4)-alkoxy, (C1-C4)-alkylthio or (C1-C4)-alkylsulfinyl; R1 is halogen, (C1-C4)-haloalkyl, (C1-C4)-alkyl, (C1-C4)-alkoxy, (C1-C4)-haloalkoxy or cyano; m is 0 to 3; n is 1 to 5; Z is oxygen, sulfur, CH2 or NR2; R2 is CN, (C1-C4)-alkoxy-(C1-C4)-alkyl, CHO, (C1-C6)-alkylcarbonyl, (C1-C6)-alkoxycarbonyl or (CW)NR3R4; R3, R4 are H or (C1-C6)-alkyl; W is O or S; G is mono- to tetrasubstituted isoxazoline which is attached in the 3-, 4- or 5-position to the adjacent phenyl ring. The compounds are suitable for use as pesticides.

Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates useful for preparing said epothilones.

Abstract: The invention relates to vitamin D derivatives of formula (I), processes for the production thereof and uses thereof: wherein Y1, Y2, R1-R6, Q and Z are as defined herein.

Abstract: The invention relates to 3-(4,5-dihydroisoxazole-5-yl)benzoylcyclohexenones of the general formula (I), wherein the variables have the following meanings: R1, R2 represents hydrogen, nitro, halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, alkylsulfinyl, haloalkylsulfinyl, alkysulfonyl or C1-C6 haloalkylsulfonyl; R3 represents hydrogen, halogen or alkyl; R4 represents hydrogen or alkyl; R5, R6 represents hydrogen, halogen, cyano, nitro, alkyl, alkoxy, alkylthio, dialkylamino, phenyl, benzyl or carbonyl, wherein the 7 last residues can be substituted; R11 represents optionally substituted cyclohexenone that is linked in the 2 position and that carries a hydroxy residue or derivatives thereof in the 1 position.

Abstract: There is disclosed a process for producing an optically active hemiester of formula (1): wherein R1, R2 and R5 represent the same meanings as described below, which comprises reacting a cyclic acid anhydride of formula (2): wherein R1 and R2 are different and independently represent a hydrogen atom, a halogen atom, an alkyl group optionally substituted with an alkoxy group or a halogen atom, and the like, with a hydroxy compound of formula (3): R3OH  (3) wherein R3 represents an alkyl group optionally substituted with an alkoxy group, a phenoxy group, a dialkylamino group or a halogen atom and the like, in the presence of an asymmetric catalyst.

Abstract: The invention relates to vitamin D derivatives of formula (I), processes for the production thereof and uses thereof: wherein Y1, Y2, R1—R6, Q and Z are as defined herein.

Abstract: The invention includes pharmaceutically active compounds and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for treating or prophylaxis of undesired thrombosis.

Abstract: Disclosed is a method of preparing a composition comprising a compound represented Structural Formula (I): 1

Abstract: The invention concerns new vitamin D derivatives of general formula (I) a process for their production, their use for production of medicaments, and intermediate products used in the process.

Abstract: Described herein is a method for preparing an ester by (a) admixing a compound having the formula I: with a base to form an intermediate, and (b) admixing the intermediate produced in step (a) with a compound composed of an alcohol, an alkoxide, or a combination thereof, wherein steps (a) and (b) are performed in situ.

Abstract: Arylisoxazoline derivatives, processes for their preparation and their use as pesticides

Abstract: Provided herein are novel substituted thiazoles and oxazoles of the Formula (I): 1

Abstract: The invention relates to inhibitors of matrix metalloproteases, more specifically a 3-aryl-succinamido-hydroxamic acid of formula (I) and its salt, ester and derivative thereof, along with methods of producing a compound of formula (I) and pharmaceutical compositions thereof.

Abstract: Oxazoline compounds having a 2,6-disubstituted-phenyl group in the 2-position, an aryl or heteroaryl group in the 4-position and an alkyl group in the 5-position are effective in controlling aphids, insects and mites.

Abstract: Methods for the preparation of chemical intermediates in the synthesis of HIV-protease inhibitors related to and including nelfinavir mesylate are disclosed. The method of this invention comprises converting tetrohydran derivatives into oxazolines to provide key reaction intermediates for the preparation of nelfinavir. Also disclosed is a method for the preparation of a chiral amino alcohol from an epoxy-tetrahydrofuran.

Abstract: A method for the preparation of 5-cyanophthalide comprising treatment of a compound of formula IV 1

Abstract: This invention is to develop novel transition metal catalysts for the practical synthesis of important chiral molecules. The invention emphasizes asymmetric catalysis based on chiral amine oxazolinyl ligands and related ligands. Specially, a direct asymmetric hydrogenation system based on Ru-Ambox catalyst was discovered.

Abstract: A 4-(2-amino-1-hydroxyethyl)oxazoline derivative of the formula [XIII] and a method for producing the same, in which R4 is an optionally substituted alkyl, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted aralkyl or an optionally substituted heteroarylalkyl, and R6 and R7 are the same or different and each is a hydrogen atom, an optionally substituted alkyl, an optionally substituted aryl, an optionally substituted heteroaryl or an optionally substituted aralkyl, or R6 and R7 combinedly form, together with the adjacent nitrogen atom, a hetero ring, the hetero ring being optionally substituted by halogen atom, alkyl, alkenyl, alkoxy, amino, alkoxycarbonyl, carboxamide or alkyl-substituted carbamoyl, an enantiomer thereof or a salt thereof.

Abstract: Methods for the preparation of chemical intermediates in the synthesis of HIV-protease inhibitors related to and including nelfinavir mesylate are disclosed. The method of this invention comprises converting tetrohydran derivatives into oxazolines to provide key reaction intermediates for the preparation of nelfinavir. Also disclosed is a method for the preparation of a chiral amino alcohol from an epoxy-tetrahydrofuran.

Abstract: Novel phosphine oxazoline ligands of formula (I) wherein m is 1, 2, 3 or 4; n, p, q, r are independently zero or 1 provided that at least one of n, p, q and r is 1; X is O, S, Se, CH2, NH; Y is N, P, As, S; R is H; a straight, branched or cyclo alkyl optionally substituted by one or more groups independently selected from alkyl, aryl, halo, alkoxy, amine, phosphine, ether; aryl optionally substituted by one or more groups independently selected from alkyl, aryl, halo, alkoxy, amine, phosphine, ether; ferrocenyl; a thioalkyl group; a thioaryl group; or R is part of a polymeric structure, for example polyacrylic acid; R1 to R13 are independently selected from H; a straight, branched or cyclo alkyl optionally substituted by one or more groups independently selected from alkyl, aryl, halo, alkoxy, amine, phosphine, ether; aryl optionally substituted by one or more groups independently selected from alkyl, aryl, halo, alkoxy, amine, phosphine, ether; a process for the preparation thereof,

Abstract: Enantiomers of formula 1

Abstract: Disclosed are compounds of the formula: which are useful for inhibiting neuraminidases from disease-causing microorganisms, especially, influenza neuraminidase. Also disclosed are compositions and methods for preventing and treating diseases caused by microorganisms having a neuraminidase, processes for preparing the compounds and synthetic intermediates used in these processes.

Abstract: The present invention relates to novel oxazoline derivatives of the formula (I) in which the radicals A, B, Q and R are each as defined in the description to processes for their preparation and to their use for controlling animal pests.

Abstract: An antioxidant which comprises a primary aliphatic hydroxyl group linked to an organic backbone such that upon oxidation a hydroperoxyl moiety capable of boosting the efficacy of free radical scavengers and hydroperoxide decomposer type antioxidants is generated in situ. The antioxidant is preferably a high hydroxyl polyol ester having a hydroxyl number ranging from about 30 to about 180 which ester is the reaction product of polyol and an acid which is at least fifty percent branched carboxylic acid, wherein the unconverted hydroxyl group is reacted with a facile leaving group, thereby producing free —CH2OH groups upon hydrolysis or oxidation.

Abstract: An optically active bisoxazoline compound of the formula [I]: wherein R1 represents alkyl group, cycloalkyl group, aralkyl group, phenyl group which may be substituted or alkoxy group and two geminal alkyl groups may be joined together to form a cyclic structure; R2 represents alkyl group, cycloalkyl group, aralkyl group, phenyl group which may be substituted; R3 represents hydrogen atom, (C2-C4)alkyl group or cycloalkyl group; and the asterisk * represents an asymmetric carbon atom

Abstract: This invention relates to certain novel imidazoline compounds and analogues thereof, to their use for the treatment of diabetes, diabetic complications, metabolic disorders, or related diseases where impaired glucose disposal is present, to pharmaceutical compositions comprising them, and to processes for their preparation.

Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.

Abstract: The invention concerns new vitamin D derivatives of general formula (I) a process for their production, their use for production of medicaments, and intermediate products used in the process.

Abstract: The present invention relates to therapeutically active compounds of formula I a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in the prevention or treatment of estrogen related diseases or syndromes.

Abstract: A novel compound having the formula: 1

Abstract: The present invention relates to new intermediates for the semisynthesis of taxanes and their preparation processes. It relates to derivatives of oxazolidines or oxazolidinones, as well as to new derivatives of baccatine III. The general process for the synthesis of taxanes according to the invention enables to obtain a product such as PACLITAXEL in only five steps from products available in the market, compared to nine steps in general, for processes of the prior art.

Abstract: A method for producing an amide derivative of the formula [XV] wherein each-symbol is as defined in the specification, and an enantiomer thereof, a novel intermediate useful for producing said compound and a production method thereof. The production method of the present invention is extremely easy and simple as compared to the conventional methods, and enables effective production of compound [XV] at high yields, which includes compound [XVI] having an HIV protease inhibitory action. In addition, the novel intermediates of the present invention are extremely useful as intermediates for producing not only the aforementioned compound [XVI] but also compounds useful as X-ray contrast media.