Abstract: The present invention relates to novel pyrido-thieno-diazepines, their preparation process and the pharmaceutical compositions containing them.

Abstract: A method of determining the ability of a compound to both bind to somatostatin type-5 receptor (“SSTR-5”) and inhibit amylin release. The method includes obtaining a preparation, either a cell preparation or a membrane preparation, which contains SSTR-5; incubating the preparation, the compound, and a SSTR-5 ligand, at least one of the ligand and the compound being detectably labeled; determining the ability of the compound to compete against the ligand for binding to SSTR-5; if and only if the compound is determined to be able to bind to SSTR-5, obtaining pancreatic cells; incubating the compound, the pancreatic cells, and an amylin release stimulator under conditions in which the amylin release stimulator would induce release of amylin from the pancreatic cells; and determining the ability of the compound to inhibit amylin release. Also disclosed is a method of treating hyperamylinemia with a ligand selective for SSTR-5.

Abstract: A seat adjustment mechanism is provided and includes an arm defining a first locking shoulder, a sector plate rotatably supported by the arm and defining a second locking shoulder having a lock recess, a locking member selectively engaging at least one of the first and second locking shoulders, a quadrant rotatably supported by the arm and slidably supporting the locking member for locking the quadrant in one of a first and second position relative to the arm and a cam plate rotatably supported by the quadrant for selectively engaging the locking member for locking the quadrant in one of the first and second positions. In the first position the locking member is biased against the first locking shoulder and in the second position the locking member is biased into the lock recess. A gear assembly is preferably provided and operably supported by the quadrant for actuation of the cam plate.

Abstract: The invention concerns DNA polymerase inhibitors, namely mikanolide and dihydromikanolide and dihydromikanolide-enriched extracts. Said compounds or mixtures can be used for preparing medicines designed to treat proliferative diseases, in particular cancer, viral diseases or parasitic diseases provoked by protozoae (for example malaria) or protists (for example, diseases caused by amoebae).

Abstract: A process for the preparation of a compound of the formula wherein the substituents are defined as set forth in the specification comprising reacting a compound of the formula with a 2-halo-3-quinoline-methanol of the formula to obtain a compound of the formula which is then cyclized to form the compound of Formula I.

Abstract: The invention concerns compounds for treating pathological conditions or diseases wherein one (or several) somatostatin receptors is (are) involved, corresponding to general formula (I) wherein: R1 represents in particular a carbocyclic or heterocyclic aryl radical optionally substituted or a non-aromatic heterocyclic radical optionally substituted; R2 represents H, alkyl or aryl optionally substituted; R3 represents H or —(CH2)p—Z3, Z3 representing in particular alkyl, cycloalkyl, bis-arylalkyl or di-aryalkyl, —Y1—(CH2)p-phenyl-(X1)n, carbocyclic or heterocyclic aryl optionally substituted, a non-aromatic heterocyclic radical optionally substituted, X1, every time it is present, being independently selected in particular among the radicals H, Cl, F, Br, I, CF3, NO2, OH, NH2, CN, N3, —OCF3, alkyl, alkoxy, —S-alkyl, —(CH2)p—NH2, —(CH2)p—NH-alkyl, —(CH2)p—N-alkyl; Y1 represents O, S, NH or is not present; R4 represents —(CH2)p—Z

Abstract: The present invention relates to new heterocyclic derivatives having an inhibitory activity on calpains and/or a trapping activity on reactive oxygen species, of formula in which A, X, Y, R1, R2 and Het represent variable groups. The invention also relates to their preparation methods, the pharmaceutical preparations containing them and their use for therapeutic purposes, in particular as inhibitors of calpains and/or traps of reactive oxygen species, selectively or non-selectively.

Abstract: The invention features somatostatin antagonists having a D-amino acid at the second residue.

Abstract: The invention concerns novel 2-arylimino-2,3-dihydrothiazole derivatives of general formula (I), their preparation methods and their use as medicines, in particular for treating pathological conditions or diseases wherein one (or several) somatostatin receptors is/are involved. Said pathological conditions include in particular acromegaly, pituitary adenoma or endocrine gastroenteropanceatic tumors including the carcinoid syndrome, and gastrointestinal bleeding.

Abstract: A compound of the formula wherein the substituents are defined as in the specification and their pharmaceutically acceptable salts having NOS and ROS activity.

Abstract: A subject of the present invention is new compounds having a lanthanide and having a tridentate ligand, a process for their preparation and their use in particular as polymerization catalysts.

Abstract: The invention features somatostatin antagonists having a D-amino acid at the second residue.

Abstract: The invention relates to novel pharmaceutical compositions comprising 2-isoxazole-8-aminotetralin derivatives. The invention more specifically relates to compositions in the form of a patch comprising a therapeutically efficacious amount of a derivative of 2-isoxazole-8-aminotetraline, especially 1,2,3,4-tetrahydro-8(5-isoxazolyl)N-N-diisopropyl-2-naphtalenamine. The invention also relates to a 2-isoxazole-8-aminotetralin derivative, especially 1,2,3,4-tetrahydro-8-(5-isoxazolyl)-N,N-diisopropyl-2-naphtalenamine, which is used to produce a medicament which can be administered transdermally to treat irritable bowel syndrome.

Abstract: The invention concerns novel lipoic acid derivatives, which have an inhibiting action with respect to NO-synthase enzymes producing nitrogen monoxide NO and/or are agents enabling the regeneration of antioxidants or entities trapping reactive oxygen species (ROS) and intervening in a more general manner in the redox status of thiol groups. The invention also concerns methods for preparing them, pharmaceutical compositions containing them and their use for therapeutic purposes, particularly their use as NO-synthase inhibitors and/or as agents acting more generally in the redox status of thiol groups.

Abstract: The present invention is directed to compounds of the wherein the variables are as defined in the specification. The compounds are useful for inhibiting farnesyl transferase and for the treatment of tumors and restenosis.

Abstract: The present invention is directed to imidazolyl derivatives of formula (II), wherein the variables are defined in the specification, which are useful as prenyl transeferase inhibitors.

Abstract: Phenoxyethylamine derivatives of general formula (I) having high affinity for the 5-HT1A receptor, methods for preparing same, pharmaceutical compositions containing said derivatives, and their use, in particular as gastric acid secretion inhibitors or as antiemetics, are disclosed. In general formula (I), Ar is phenyl substituted by one or more substituents; and R is a C1-10 hydrocarbon radical selected from straight or branched alkyl, alkenyl or alkynyl radicals, saturated or unsaturated mono- or polycyclic cycloalkyl, cycloalkylalkyl or alkylcycloalkyl radicals; a pyridyl or isoquinolyl radical, phenyl optionally substituted by one or more substituents, and salts thereof.

Abstract: A device implantable in the vascular ducts. The device includes an elongated intraluminal element that occupies a section of the vascular lumen so as to increase the speed at the vascular wall at the level of the element without decreasing the blood flow and without exerting any substantial mechanical action on the vascular wall, the element also includes a fixing device in the vascular lumen.

Abstract: Amidine compounds of the formula wherein the substituents are defined as in the application useful as NO-synthase enzyme inhibitors.

Abstract: New intermediates of the formula (II)B described below for the synthesis of amidine derivatives of (−)-6-hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid, such as for example (S)-N-{4-[4-[(3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-1-benzopyran-2-yl)-carbonyl]-1-piperazinyl]phenyl}-2-thiophenecarboximidamide wherein A′ is X is —Z1—CO; &rgr; is a bond or a heterocycle selected from the group consisting of piperidine, piperazine, homopiperazine, 2-methylpiperazine, 2,5-dimethyl-piperazine and 4-aminopiperidine; Y is —Z2— or —NR3—Z2, R3 is hydrogen, alkyl of 1 to 6 carbon atoms or —COR4, R4 is alkyl of 1 to 6 carbon atoms; Z1 and Z2 independently are a single bond or alkylene of 1 to 6 carbon atoms; and R6 is hydrogen or OH.