Abstract: According to one embodiment the invention concerns a process for a degradation of an epothilone C or a epothilone D, wherein an epothilone C or epothilone D is subjected to an olefin metathesis in the presence of ethylene and subsequently an optional ester hydrolysis.

Abstract: The present invention provides novel compounds and use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: Wherein X and Y are independently chosen from O, N, S and (CH2)n, where n is 0, 1, 2, 3, 4, or 5, or a combination of these and may contain carbon-carbon multiple bonds and branched chains as well as alicyclic and heterocyclic groups; Q is H or OH; R1 and R2 can be either the same or different and are chosen from hydrogen or the residue of an aromatic group as listed in Scheme 1 and the pharmacologically active salts thereof

Abstract: A process for the manufacture of 2,3,5-trimethylhydroquinone diacylate comprising reacting ketoisophorone with an acylating agent in the presence of a NH- or CH-acidic catalyst, particularly certain bis(perfluorinated hydrocarbyl sulphonyl) imides and metal salts thereof and, respectively, certain tris(perfluoroalkanesulphonyl or pentafluorobenzenesulphonyl) methanes and metal salts thereof. The acylating agent is particularly an acid anhydride, an acyl halide or an enol ester. The so-obtained 2,3,5-trimethylhydroquinone diacylate can be converted into (all-rac)-?-tocopherol by transesterification to yield 2,3,5-trimethylhydroquinone and reaction of the latter with isophytol. (all-rac)-?-Tocopherol itself is the most active member of the vitamin E group.

Abstract: A manufacturing process for the preparation of ?,?-branched alkane carboxylic acids, by reacting a mono-olefin or a precursor thereof, with carbon monoxide in the presence of a strong acid catalyst characterized in that the starting olefin is a dimmer C8 or trimer C12 derived from n-butene, which predominantly comprise 2-butene, that the acid catalyst is composed of BF3/H3PO4 in a molar ratio of BF3:H3PO4 in the range of from 0.5:1.0 to 5.0:1.0, or of CF3SO 3H, that the weight ratio of the catalyst relative to the mono-olefin is in the range of from 1:1 to 10:1, that the reaction is carried out at a temperature in the range of from 60 to 140° C., and with an initial water content in the catalyst system in the range of from 8 to 25 wt %; and vinyl esters and glycidyl esters derived from said carboxylic acids.

Abstract: A new crystalline polymorph of ritonavir and methods for its use and preparation are disclosed.

Abstract: A Vpr function regulating composition useful in the treatment of subjects infected with HIV or having AIDS, wherein the composition comprises an aminostilbazole derivative represented by the following formula [1] or a salt thereof as an active ingredient: A-B-D-E[1] wherein A represents heteroaryl or an oxide thereof, B represents ethenylene, D represents phenylene, and E represents the formula: —N(R)—SO2-G wherein G represents phenyl, R represents hydrogen, alkyl, or —COR0 (R0 represents alkyl, alkoxy, aryloxy, 5- to 6-membered heteroaryl, heteroarylmethyl, aminoalkylene, or cyclic amino alkylene)or the like.

Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein R1, R2, R2a, R3, R3a, and R4, and X as defined in the specification, or a pharmaceutically acceptable salt thereof.

Abstract: Tert-alkylphenoxy-substituted polycyclic compounds of the general formula I where P is a conjugated polycyclic radical which is stable to bases and nucleophiles, optionally bears aryl substituents and contains no group from the group consisting of —CO—NH—CO—, —COOH and —CO—O—CO—; R is C1–C8-alkyl, whose carbon chain may be interrupted by one or more groups selected from the group consisting of —O—, —S—, —NR1—, —CO— and/or —SO2— and which may be monosubstituted or polysubstituted by C1–C6-alkoxy or by a 5- to 7-membered heterocyclic radical which is attached via a nitrogen atom and may contain further heteroatoms and be aromatic; C5–C8-cycloalkyl whose carbon chain may be interrupted by one or more groups selected from the group consisting of —O—, —S—, —NR1—, —CO— and/or —SO2— and which may be monosubstituted or polysubstituted by C1–C6-alkyl; R1 is hydrogen or C1–C6-alkyl; Hal is chlorine and/or bromine; m is from 0 to 15; n is from 1 to 16, subject to the proviso that the sum m+n is ?16, are prepared a

Abstract: A method for making epothilones and epothilone analogs is described, as are novel compounds made by the method. One embodiment of the method was used to synthesize epothilone B by a convergent approach that entailed Wittig coupling of an ylide derived from phosphonium bromide with an aldehyde. The former was prepared from propargyl alcohol by a nine-step pathway which installed both trisubstituted double bonds with clean Z configuration. Macrolactonization of a resulting seco acid provided the following intermediate diene epothilone analog.

Abstract: Dihydropyrroloindoles and tetrahydropyridoindoles are prostaglandin receptor antagonists useful for the treatment of prostaglandin-mediated diseases such as allergic rhinitis, nasal congestion and asthma.

Abstract: The present invention relates to prodrugs of pharmacologically active five-membered heterocyclic amidines from which are produced in vivo compounds which are competitive inhibitors of trypsin-like serine proteases, in particular thrombin and kininogenases such as kallikrein, to the preparation thereof and to the use thereof as medicines. The invention also relates to pharmaceutical compositions which comprise the prodrugs of the active compounds as ingredients, and to the use of the compounds as thrombin inhibitors, anticoagulants and as antiinflammatory agents.

Abstract: ?-Amino hydroxamic acid derivative of formula (I), in which R is C2–C7-alkyl, which is mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C3–C5-cycloalkyl or unsubstituted or substituted C3–C4-heteroaryl comprising one or two heteroatoms selected from the group consisting of O, S and N; or C3–C7-alkenyl or C3–C7-alkynyl, which in each case is unsubstituted or mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C3–C5-cycloalkyl or unsubstituted or substituted C3–C6-heteroaryl comprising one or two heteroatoms selected from the group consisting of O, S and N; and the other symbols are as defined in claim 1, are described. These compounds are MMP and in particular MMP2 inhibitors and can be used for treatment of MMP dependent diseases, in particular inflammation conditions, rheumatoid arthritis, osteoarthritis, tumors (tumor growth, metastasis, progression or invasi n) and pulmonary disorders (e.g. emphysema, COPD).

Abstract: A composition and a process for producing the composition are disclosed. The composition comprises an alkoxylated phosphite ester which has the formula of (HO[{CH(R)}mO]n)3P in which each R can be the same or different and can be independently hydrogen or an alkyl group, or combinations of two or more thereof and m is a number from 2 to about 20 and n is a number from 2 to about 20. The process comprises contacting a trialkyl phosphite with an alkylene glycol or polyalkylene glycol to produce a mixture followed by heating the mixture. Also disclosed in a process for using the composition, which comprises contacting a carbonyl compound, in the presence of the composition, with an alcohol.

Abstract: The invention provides a compound of formula (I). This invention relates to heterocyclic compounds. It further relates to methods for their preparation, compositions cotaining them and their use as a medicament, particularly as a medicament for the treatment and prophylaxis of cancer.

Abstract: The present invention provides an improved process for the preparation of a polymorph of eletriptan hemisulphate.

Abstract: The present invention relates to novel compounds, their use for inhibiting serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV) and to methods for their production and their therapeutic utility.

Abstract: Renal-selective compounds are described which, in one embodiment, are prodrugs preferentially converted in the kidney to compounds capable of blocking angiotensin II (AII) receptors. These prodrugs are conjugates formed from two components, namely, a first component provided by an AII antagonist compound and a second component which is capable of being cleaved from the first component when both components are chemically linked within the conjugate. The two components are chemically linked by a bond which is cleaved selectively in the kidney, for example, by an enzyme. The liberated AII antagonist compound is then available to block AII receptors within the kidney.

Abstract: Preventives/remedies for voiding disturbance containing a compound having both of an acetylcholinesterase inhibitory action and an ?1 antagonistic action which exhibits an excellent effect of improving the urinary function of the bladder (i.e., effects of improving urine flow rate and voiding efficiency) without affecting the urinary pressure or the blood pressure.

Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.

Abstract: The present invention relates to a crystal of bicalutamide having a defined form, as well as economical and industrially practical production methods of bicalutamide and a crystal thereof, which are superior in environmental benignity and safety. Accordingly, the present invention provides a production method of bicalutamide represented by the formula (I): which includes at least a step of reacting a compound represented by the formula (3): with an oxidizing agent, a production method of a crystal of bicalutamide, as well as a crystal form of bicalutamide as defined by X-ray diffraction (XRD) or solid 13C NMR measurement.