Abstract: The invention relates to a process for the manufacture of salts of citalopram in high purity. By the careful selection of solvents and the careful manipulation of the pH value, citalopram salts may be isolated in the absence of 5-chlorocitalopram, 5-bromocitalo-pram, desmethyl-citalopram and 5-carobxyamide citalopram.

Abstract: The present invention relates to synthetic green tea derived polyphenolic compounds, their modes of syntheses, and their use in inhibiting proteasomal activity and in treating cancers. The present invention is also directed to pharmaceutical compositions useful in methods of inhibiting proteasomes and of treating cancers.

Abstract: A process for the preparation of clopidogrel (1) by reaction of the N,N?-bis-4,5,6,7-tetrahydro-[3,2-c]-thienopyridyl methane (12) with (R)-2-chlorophenylacetic acid derivatives of formula (13) in which X and R have the meanings as indicated in the disclosure.

Abstract: Process for manufacturing an oxirane by reaction between an olefin and a peroxide compound in a reactor containing a liquid phase, in the presence of water, one or more organic solvents, a catalyst and one or more compounds for increasing the selectivity of the catalyst toward epoxidation reactions, in which: if the process is performed in batchwise mode, the liquid phase present in the reactor when the reaction starts, if the process is performed continuously, all of the liquid phases that are fed continuously into the reactor has/have a total organic solvent content of at least 0.1 g/kg and of not more than 675 g/kg.

Abstract: The invention relates to a new industrially useable process for preparing tropenol, optionally in the form of the acid addition salts thereof.

Abstract: The object of the present invention is a novel mandelate salt of a substituted tetracyclic tetrahydrofuran derivative according to Formula (I) the N-oxide forms and the stereochemically isomeric forms thereof, wherein R1 and R2 each independently are hydrogen or C1-6alkyl and R3 and R4 each independently are hydrogen or halogen. In the foregoing definitions C1-6alkyl defines straight and branched saturated hydrocarbon radicals having from 1 to 6 carbon atoms such as, for example, methyl, ethyl, propyl, butyl, 1-methylpropyl, 1,1-dimethylethyl, pentyl or hexyl. The novel mandelate salt is not light-sensitive and is far more stable than the prior art salts at room temperature, enhanced temperature and at relative high humidities and in aqueous media.

Abstract: The invention relates to pyran derivatives of formula I and processes and intermediates for their preparation and derivatisation, and the use thereof in liquid-crystalline media.

Abstract: A compound which is a carbamate of formula: wherein R1 represents R2 represents a benzyl, phenethyl, furan-2-ylmethyl, furan-3-ylmethyl, thiophen-2-ylmethyl or thiophen-3-ylmethyl group or a straight or branched alkyl group having 3 to 8 carbon atoms, an alkenyl group having 3 to 8 carbon atoms, or a cycloalkyl group of 3 to 6 carbon atoms; p is 1 or 2 and the substitution in the azoniabicyclic ring may be in the 2, 3 or 4 position including all possible configurations of the asymmetric carbons; or a pharmaceutically acceptable salt thereof.

Abstract: A compound of the general formula (I) or (II) wherein X is O, NR4 or S and R1-R8 are as defined in the specification

Abstract: Compounds of the formula having anti-tumor activity, wherein R1 and R2 are as described herein

Abstract: The present invention relates to novel compounds, pharmaceutical compositions and methods for treating tumors, cancer and hyperproliferative diseases including psoriasis, genital warts and hyperproliferative cell growth diseases, including hyperproliferative keratinocyte diseases such as hyperkeratosis, ichthyosis, keratoderma or lichen planus.

Abstract: Competitive progesterone antagonists, including two novel steroids, viz., 11?,19-[4-(cyanophenyl)-o-phenylene]-17?-hydroxy-17?-(3-hydroxyprop-1(Z)-enyl)-4-androsten-3-one and 11?,19-[4-(3-pyridinyl)-o-phenylene]-17?-hydroxy-17?-(3-hydroxyprop-1(Z)-enyl)-4-androsten-3-one, inhibit formation of endometrial glands at below their ovulation inhibiting dose and the abortive dose, and thus achieve oral contraception in females without adversely affecting the menstrual cycle and without risk of aborting a previous implanted fertilized egg or a fetus.

Abstract: N-(4,5,6,7-tetrahydro-thiazolo-[5,4-c]pyridin-2-yl)-(C6-18)arylsulfonamides, wherein the nitrogen atom of the pyridine is substituted, and wherein the pyridine ring is optionally bridged, useful as a pharmaceutical related to steroid sulfatase

Abstract: The subject invention provides anticoagulant compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R1, R3, n and Ar are as defined herein. The compounds of the subject invention can be used to treat at-risk populations thereby bringing relief of symptoms, improving the quality of life, preventing acute and long-term complications, reducing mortality and treating accompanying disorders. The invention further comprises pharmaceutical compositions comprising the compounds and salts of the invention, as well as methods of using the compounds, salts, and compositions of the invention.

Abstract: Cannabinoid agonists and antagonists are provided for use in the treatment of disorders such as acute and chronic pain, inflammation, loss of appetite, convulsions, multiple sclerosis, nausea and vomiting. The cannabinoid agonists and antagonists contain a sulfonamide moiety incorporated into the cannabinoid side chain, and the side chain itself may be saturated or unsaturated.

Abstract: This invention features the use of the spirolaxine of formula (I) for the treatment of those pathologies responding to the activation of the PPAR? receptor, such as the Type 2 insulin-resistant diabetes. This invention also features a pharmaceutical composition in which the spirolaxine of formula (I) acts as active principle in association with the all-trans retinoic acid of formula (II) for the treatment of those pathologies responding to the activation of the PPAR? receptor, such as the acute malignant haemopathies.

Abstract: Compounds of Formula I are useful for inhibiting serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein and have improved pharmacokinetic properties. These compounds may be used in methods of preventing and/or treating clotting disorders.

Abstract: Novel oxazole and thiazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-? signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.

Abstract: Provided herein are compounds of the formula (I): wherein R1-R8 are as described herein, R4 being phthalazinyl, pyrazinyl, pyridazinyl, or quinoxalinyl. Such compounds are particularly useful in the treatment of a disorder which is created by or is dependent upon decreased availability of serotonin, norepinephrine, or dopamine.

Abstract: The invention relates to difluorobenzo-1,3-dioxoles, to a process for their preparation, and to their use for preparing medicaments and crop protection agents.