Abstract: A method of identifying, for a patient having pain of a joint, susceptibility to developing progressive osteoarthritis or loss of joint space, by determining in such patient the presence or absence of bone marrow edema about or of the joint. A determination of the presence of bone marrow edema about or of the joint identifies the patient as susceptible to developing progressive osteoarthritis or loss of joint space.

Abstract: 5-Arylidene-4-oxo-2-thioxo-3-thiazolidinecarboxylic acids of formula I in which the symbols R1, R2, A, A1 and A2 have the significance given in the description as medicaments for the treatment of cancer diseases.

Abstract: Compounds of formula I in which R1 represents a substituted or unsubstituted phenoxy, phenylthio, phenylsulfinyl, phenylsulfonyl, phenylamino or phenylmethyl residue, and R2 represents an optionally substituted aryl or heteroaryl residue, with metallo-proteinase inhibitor activity.

Abstract: A process for the production of a naturally folded eukaryotic polypeptide containing two or several cysteines linked by disulfide bridges by a) culturing prokaryotic cells in which the said prokaryotic cells contain an expression vector which codes for the said polypeptide which contains a prokaryotic signal sequence at the N-terminus, b) secreting the polypeptide into the periplasm or the medium, c) cleaving the signal sequence and isolating the polypeptide from the periplasm or the medium, which is characterized in that a nucleic acid coding for a molecular chaperone is additionally expressed in the said prokaryotic cell and the chaperone is secreted into the periplasm, is suitable for the recombinant production of polypeptides in prokaryotes in a high yield.

Abstract: A compound of the formula wherein R is hydrogen or hydroxy, each R1 is ethyl, propyl, butyl, isopropyl or t-butyl, X is ═CH2, or when R is hydroxy, X is hydrogen or ═CH2, and A is —C≡C—, or —CH2—CH2—. These compounds are useful for the treatment of hyperproliferative disorders, skin diseases, and sebaceous gland diseases.

Abstract: The present invention relates to a pyrrolidine compound and pharmaceutically acceptable esters and/or salts thereof. The compounds are useful as inhibitors of metalloproteases, e.g. zinc proteases, particularly zinc hydrolases, and which are effective in treating disease states are associated with vasoconstriction of increasing occurrences.

Abstract: A hypodermic needleless injection system for injecting a liquid medication, which system comprises: a medication unit configured and dimensioned to store a volume of liquid to be injected, the medication unit having a first region and a second region that are in liquid communication with each other, the first region being deformable and the second region having at least one orifice, a hydrostatic chamber containing a hydrostatic pressure transfer medium, the hydrostatic chamber being so configured and dimensioned that the medication unit is located at least partially within the hydrostatic chamber and so that a pressure exerted on the transfer medium would cause the first region of the medication unit to deform so as to reduce the volume available for the liquid medication within the medication unit, and a first piston having a first end and a second end opposite to the first end, the first end having a surface which forms a closure of the hydrostatic chamber, and is adapted for applying a pressure on the tra

Abstract: The invention relates to a process for the preparation of vinyl pyrimidines of the formula I wherein R1 is hydrogen or a carboxylic ester group, and R2 is hydrogen or a group of the formula (a) wherein Ra is hydrogen, a protecting group or a group easily hydrolyzable under physiological conditions, by reacting a compound of the formula II wherein R21 is hydrogen or a group (a) wherein hydroxy groups are optionally protected, R3 is bromo, chloro or iodo, and R1 is as above, with a vinyl borane compound in the presence of a Pd complex and a base, and optionally, further reacting a product of formula I wherein R2 is hydrogen with a compound of the formula IV wherein Rb is a hydroxy protecting group and Z is a leaving group, in the presence of a Lewis acid catalyst.

Abstract: Compounds of the formula wherein R1 is hydrogen or an alkyl group; R2 is hydrogen or an alkyl group; or R1, R2 and C20 together are cyclopropyl; R3 is alkyl, hydroxy-alkyl or fluoroalkyl; and R4 is alkyl, hydroxy-alkyl or fluoroalkyl which are useful in the treatment of breast cancer, prostate cancer, myeloid leukemia benign prostate growth, baldness and osteoporosis.

Abstract: A compound of the formula wherein R is hydrogen or hydroxy, each R2 is independently H or halogen, X is ═CH2, or when R is hydroxy, X is hydrogen or ═CH2, and A is —C≡C—, or —CH2—CH2—, provided that when A is —CH2—CH2—, R2 is H.

Abstract: The present invention is concerned with a process for the manufacture of chiral succinic acid derivatives of formula (I) wherein R1 is (C1-C6) alkyl or benzyl, and the novel intermediates used therein.

Abstract: Novel trienoic retinoid compounds of with apoptotic activity useful for the prevention and treatment of cancer.

Abstract: New compounds of formula I wherein: R and R1 are independently selected from hydrogen, (C1-C6)alkyl, styryl and (C3-C6)cycloalkyl or, taken together with the carbon to which they are linked, form a (C3-C6)cycloalkyl group; A is selected from the following groups: —CH2C≡CCH2—, or —(CH2)q—NH—(CH2)q—, wherein q is an integer from 2 to 3 B is selected from T is selected from —CH2—C≡CH, —C≡CH, —(CH2)p—R3, —CH═CH—R3, —CH2—NHCO—R3, —(CH2)p—O—R3, —CH(NH2)—CH2R3, in which p is 0 or an integer from 1 to 4, R3 is a carbocyclic or heterocyclic ring as medicaments having antitumor and/or antimetastatic activities.

Abstract: Invented are improved multidose aqueous formulations of endo-N-(9-methyl-9-azabicyclo[3.3.1.]non-3-yl)-1-methyl-1H-indazole-3-carboxamide hydrochloride.

Abstract: Disclosed are substituted pyrroles having the formula These compounds and their pharmaceutically acceptable salts are useful in the treatment and/or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing the foregoing compounds.

Abstract: A process for preparing granisetron by cyclising a compound of structure (2).

Abstract: The present invention concerns intermediates useful in and a process for the preparation of a compound of formula 1 or a salt thereof comprisingepoxidation of a compound of formula 2 or a salt thereof wherein A, R1 and R2 are as herein defined. These compounds are useful in the synthesis of renin inhibitors.

Abstract: A compound of formula I wherein R1 is hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, aryloxy or alkylalkoxy, and R2 is aryloxy, or a pharmaceutically acceptable salt of an acidic compound of formula I, or a prodrug thereof. The compounds of formula I and their aforementioned salts and prodrugs can be used in the treatment or control of cancer associated with overexpresison of gelatinase-A and/or gelatinase-B, particularly skin cancer, breast cancer, prostate cancer, colon cancer, lung cancer, and gastric cancer. The compounds of the invention are also useful for other diseases associated with unregulated degradation of extracellular matrix, including rheumatoid arthritis, osteoarthritis, multiple sclerosis, corneal ulceration, periodontal disease and the like.

Abstract: The compounds of the formula wherein R signifies halogen or lower alkyl; n signifies 0-3; R1 signifies lower alkyl; cycloalkyl; benzyl optionally substituted by hydroxy, halogen, lower alkoxy or lower alkyl; benzoyl optionally substituted by amino, lower alkylamino or di-lower alkylamino; acetyl or cycloalkyl-carbonyl; and signifies an aromatic 5-membered residue which is bonded via a N-atom and which contains further 1-3 N atoms in addition to the linking N atom, as well as their pharmaceutically acceptable salts as therapeutically active substances, especially for the control or prevention of acute and/or chronic neurological disorders.

Abstract: This invention relates to new processes for manufacturing 4-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-N-methyl-3H-[1,2,3]triazole-5-carboxamide (compound I) as well as the following new intermediates useful in these synthetic processes. 2-benzenesulfonyl-N-methylacetamide (compound IV), 2-(benzenesulfonyl)-3-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-N-methylacrylamide (compound II) and threo-2-[2-benzenesulfonyl-1-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-[(methylcarbamoyl)ethyl]]-5-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-N-methyl-2H-[1,2,3]triazole-4-carboxamide (compound III).