Abstract: Novel isoquinoline-3-carboxamides of the formula I: ##STR1## in which R.sub.1 is hydrogen or chlorine, R.sup.2 is hydrogen, alkyl, alkoxy, chlorine, trifluoromethyl, hydroxyl, or benzyloxy which is optionally substituted, or fluoroalkoxy of the formula O--[CH.sub.2 ].sub.x --C.sub.f H.sub.(2f+1-g) F.sub.g, where x=0 or 1, f=1-5, and g=1 to (2f+1), R.sup.3 is hydrogen, alkyl, alkoxy, fluorine, chlorine, cyano, trifluoromethyl, hydroxyl, or benzyloxy which is optionally substituted, or fluoroalkoxy of the above formula, R.sup.4 and R.sup.5 are hydrogen, alkyl, fluorine, chlorine, bromine, trifluoromethyl, cyano, alkoxy, or fluoroalkoxy of the above formula, including the physiologically active salts, are strong prolyl-4-hydroxylase inhibitors which do not cause steatosis.

Abstract: A device for establishing a flange connection, having a bearing which can act on a first flange, a counter-bearing which can act on a second flange, and a connecting lever between the two bearings is described. The invention is distinguished by the fact that the connecting lever is a lever with a drawing element. The drawing element and the lever each have a first and second end. The drawing element's first end engages the bearing and its second end jointedly mounts in between the first and second ends of the lever. The counter-bearing has at least one contact location for the first end of the lever and a recess for the drawing element.

Abstract: A particular subject of the invention is the products of formula (I): ##STR1## in which: R.sub.1 and R.sub.2 represent in particular cyano and trifluoromethyl,R.sub.3 represents in particular alkyl, alkenyl or alkynyl, optionally substituted by one or more halogen, cyano or hydroxyl radicals,R.sub.4 and R.sub.5 either represent in particular methyl optionally substituted by fluorine,or form in particular a cyclohexyl radical,X and Y represent in particular oxygen,as well as their salts and isomers.

Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.2 or --NR.sub.3 R.sub.4 where R.sub.2 is hydrogen or loweralkyl, and R.sub.3 and R.sub.4 are independently hydrogen, loweralkyl or cycloalkyl; R is hydrogen, loweralkyl or loweralkylcarbonyl; and R.sub.1 is hydrogen, loweralkyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, furylloweralkyl, thienylloweralkyl, pyridinylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl or oxygen-bridged diarylloweralkyl; stereo, optical and geometrical isomers thereof, and pharmaceutically acceptable acid addition salts thereof which are useful for enhancing memory.

Abstract: This invention relates to polyfluoroalkyl tryptophan tripeptides and to compositions containing them. The compounds are highly selective thrombin inhibitors which provide anticoagulant effects useful in the treatment of thrombin conditions and in preventing the coagulation of stored whole blood and blood products.

Abstract: The present invention is directed to esters of (+)-.alpha.-(2,3-Dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidine methanol, pharmaceutical formulations, methods of making and methods of using these esters. These compounds antagonize the effects of serotonin at the 5HT.sub.2A receptor and are useful in treating various conditions such as, for example, psychoses such as schizophrenia.

Abstract: The invention relates to a crystal modification of the compound of the formula I ##STR1## and the processes for the preparation of and use that crystal modifications 1. The invention is used for treating acute immunological episodes, such as sepsis, allergies, graft-versus-host and host-versus-graft-reactions, autoimmune diseases, in particular rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis, psoriasis, atopic dermatitis, asthma, urticaria, rhinitis, uveitis, type II diabetes, liver fibrosis, cystic fibrosis, colitis, cancers, such as lung cancer, leukemia, ovarian cancer, sarcomas, Kaposi's sarcoma, meningioma, intestinal cancer, lymphatic cancer, brain tumors, breast cancer, pancreatic cancer, prostate cancer, or skin cancer.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: The invention provides an intravaginal drug delivery system having a first intravaginal part comprising at least one active agent in a polymer matrix, said first part being provided in association with a second part comprising a removable polymer membrane arranged to absorb excess active agent. Use of a polymer membrane in this way serves to substantially reduce the initial high burst of active from the intravaginal part following administration. It also reduces the levels of release of active during the first few weeks of use. Also provided is an intravaginal drug delivery device comprising at least one active agent dispersed in a polymer matrix, wherein the concentration of active agent at the outer surface of the device at the time of use is not substantially higher than the concentration of the active agent in the remainder of the device.

Abstract: The present invention provides a pharmaceutical composition in the form of a bilayer tablet comprising,(a) a first discrete zone made with Formulation (A) which comprises, a therapeutically effective decongestant amount of a sympathomimetic drug, or a pharmaceutically acceptable salt thereof, in an amount of about 18% to about 39% by weight of Formulation (A), and a first carrier base material, the first carrier base material comprising a mixture of;(I) carnauba wax in an amount of about 59% to about 81% by weight of Formulation (A); and(ii) a suitable antiadherent in an amount of about 0.25% to about 2.

Abstract: The present invention relates to a method of providing an antihistaminic effect in a hepatically impaired patient in need thereof comprising administering to said patient an effective antihistaminic amount of a compound of the formula ##STR1## wherein R.sub.1 is hydrogen or hydroxy;R.sub.2 is hydrogen;or R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ;n is an integer of from 1 to 5;R.sub.3 is --COOH or --COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched;each of A and B is hydrogen or hydroxy with the proviso that at least one of A or B is hydrogen;or a pharmaceutically acceptable salt and individual isomers thereof.

Abstract: Compounds of the formula I, ##STR1## in which B, E, W, Y, Z, R, R.sup.2, R.sup.2a, R.sup.2b, R.sup.3, g and h have the meanings indicated in the specifications. The compounds of the formula I are valuable pharmaceutical active compounds, which are suitable, for example, for the therapy and prophylaxis of inflammatory disorders, for example of rheumatoid arthritis, or of allergic disorders. The compounds of the formula I are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 belonging to the integrins group. They are generally suitable for the therapy or prophylaxis of illnesses which are caused by an undesired extent of leucocyte adhesion and/or leucocyte migration or are associated therewith, or in which cell-cell or cell-matrix interactions which are based on interactions of VLA-4 receptors with their ligands play a part.

Abstract: A process of converting a hydroxy heteroaromatic compound to an arylamine, comprising the steps of:(1) treating a salt of a hydroxy heteroaromatic compound with an alkylating agent; and(2) treating the reaction mixture with a Smiles solvent system and raising the temperature of the reaction mixture; andA compound made according to the above process.

Abstract: The present invention is directed to esters of (+)-.alpha.-(2,3 Dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol, pharmaceutical formulations, methods of making and methods of using these esters. These compounds antagonize the effects of serotonin at the 5HT.sub.2A receptor and are useful in treating various conditions such as, for example, psychoses such as schizophrenia.

Abstract: The present invention relates to a novel lantibiotic having the formula NH.sub.2 --R-actagardine, where NH.sub.2 --R is the radical of the amino acid alanine, which is formed by the microorganism Actinoplanes liguriae, DSM 11797 or Actinoplanes garbadiensis, DSM 11796 during fermentation, chemical derivatives of the lantibiotic, a process for its preparation and the use of the lantibiotics as pharmaceuticals.

Abstract: An isomerization method wherein a compound of formula ##STR1## wherein X and y together form a 3-oxo radical, or X is a hydrogen atom and Y is either a radical a ##STR2## where R.sub.2 is OH or O-acyl, or an O-alkyl or NH.sub.2 radical; R.sub.1 is a hydrogen atom or a methyl radical; Z is hydrogen or an acyl radical; and R is a hydrogen atom, an NH.sub.2 radical or a (CH.sub.2).sub.n Ar, NH(CH.sub.2).sub.n Ar or N.dbd.CH(CH.sub.2).sub.n Ar radical, in the form of a 10.alpha. isomer or a mixture of 10.alpha. and 10.beta. isomers, is exposed to a basic agent to give the corresponding compound of formula I in which the 10-methyl radical is in the .beta. position.

Abstract: The present invention is directed to the use of (+)-.alpha.-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidine methanol in treating Depressive Disorders and Bipolar Disorders.

Abstract: There are disclosed various compounds of the formula below, ##STR1## where R, R.sub.1, W, X, Y and Z are as defined in the specification; which are useful for alleviating various memory dysfunctions such as Alzheimer's disease, as modulators of neurotransmitter functions such as serotonergic and adrenergic, and as such are useful as antidepressants, anxiolytics, atypical antipsychotics, antienmtics, and for the treatment of personality disorders such as obsessive compulsive disorder.

Abstract: An isolated DNA molecule consisting of SEQ I.D. No: 22 encoding a polypeptide having a protease activity and capable of inducing a apoptosis and the method of producing a polypeptide consisting of the said sequence.