Abstract: The use of compounds of formula wherein R2, R3, R4, R5, R6 and R7 have several meanings, for the treatment of disorders mediated by protozoan organisms, novel compounds of the above formula and intermediates for the preparation of such compounds, pharmaceutical compositions comprising such novel compounds, a method of treating disorders mediated by protozoan organisms comprising administering such compounds, optionally together with a second drug substance, to a subject in need thereof and the use of such compounds, whenever comprising a photoaffinity label, for the identification of the molecular target(s) of arylamino alcohol antimalarials.

Abstract: The invention relates to a compound having general formula (I): Wherein m, R1 and R2 are as defined herein. The invention also relates to the use of the compound in therapeutics. More specifically, the compounds of the invention are inhibitors of the FAAH enzyme, and therefore, can be used for the treatment of various disorders associated with FAAH enzyme, which include in a non-limiting manner, pain, eating disorders, neurological and psychiatric pathologies, among other disorders.

Abstract: Provided are compounds, methods and kits for identifying in cells of interest organelles including nuclei and a wide variety of organelles other than nuclei (non-nuclear organelles), as well as cell regions or cell domains. These compounds and methods can be used with other conventional detection reagents for identifying the location or position or quantity of organelles and even for distinguishing between organelles in cells of interest.

Abstract: Compounds of the formula wherein m is 0, 1 or 2; wherein when m is 0, Z is O, when m is 1, Z is N, and when m is 2, Z is C; Y is H, OH, NH2, or an organic moiety of 1-20C, optionally additionally containing 1-8 heteroatoms selected from the group consisting of N, P, O, S and halo; each l1 and l2 is independently 0-5; l3 is 0 or 1; each of R1, R2 and R3 is independently alkyl (1-6C), aryl (6-10C) or arylalkyl (7-16C) optionally containing 1-4 heteroatoms selected from the group consisting of halo, N, P, O, and S or each of R1 and R2 may independently be halo, COOR, CONR2, CF3, CN or NO2, wherein R is H or lower alkyl (1-4C) or alkyl (1-6C); n is 0 or 1; X is a linker; with the proviso that Y is not a tropolone, a coumarin, or an antioxidant containing an aromatic group and with the further proviso that if l3 is 0, and either l1 and l2 is 0 or 1 and if R1 and/or R2 represent F in the para position, Z cannot be C or N; and are useful to treat pain.

Abstract: Provided herein are substituted phenanthrene diketo acid compounds. These compounds comprise the diketo acid moiety on one of carbons C1-C4 and C9 in the phenanthrene ring and at least one further substitutent on the other ring carbons. Also provided are methods of inhibiting an activity of a human immunodeficiency virus (HIV) integrase protein and treating an HIV infection in a subject using the substituted phenanthrene diketo acid compounds.

Abstract: Disclosed herein are carbonyl compounds of Formula I as described herein. Methods and compositions are disclosed for treating disease states including, but not limited to cancers, autoimmune diseases, tissue damage, central nervous system disorders, neurodegenerative disorders, fibrosis, bone disorders, polyglutamine-repeat disorders, anemias, thalassemias, inflammatory conditions, cardiovascular conditions, and disorders in which angiogenesis play a role in pathogenesis, using the compounds of the invention. In addition, methods of modulating the activity of histone deacetylase (HDAC) are also disclosed.

Abstract: The present invention relates to compounds of formula I and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.

Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

Abstract: Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.

Abstract: Dibenzosuberanyl piperazine derivatives represented by the following formula (I): wherein R represents an aliphatic hydrocarbon group, which may contain one or more heteroatom-containing substituent groups and may preferably contain 2 to 30 carbon atoms, and physiologically acceptable salts thereof; and medicinal compositions containing these dibenzosuberanyl piperazine derivatives and/or physiologically acceptable salts thereof. These compounds show effectiveness in allowing resistance-acquired causes of diseases to restore sensitivity to drug, that is, a resistance overcoming effect.

Abstract: This invention provides a process to prepare (2R)-anti-5-{3-[4-(10,11-difluoromethanodibenzosuber-5-yl)piperazin-1-yl]-2-hydroxypropoxy}quinoline.

Abstract: This invention provides a process to prepare (2R)-anti-5-{3-[4-(10,11-difluoromethanodibenzosuber-5-yl)piperazin-1-yl]-2-hydroxypropoxy}quinoline.

Abstract: This invention provides a process to prepare 10,11-(optionally substituted)methanodibenzosuberane derivatives. The invention also provides an intermediate in this process.

Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula 1

Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

Abstract: Novel compounds of Formula are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the above formula to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.

Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and m are as defined in the detailed part of the present description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation, as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.

Abstract: Drug and multidrug resistant modulators of the formula: ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen or halo; A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CHR.sup.4 --CH.sub.2 --, or --CH.sub.2 --CHR.sup.5 --CHR.sup.6 --CH.sub.2 --, where R.sup.4 is --H, --OH, or acyloxy; one of R.sup.5 or R.sup.6 is --H, --OH, or acyloxy, and the other is --H; R.sup.3 is a polyaryl; and pharmaceutically acceptable salts and solvates thereof, are described and claimed. Use of the new compounds in the preparation of pharmaceutical compositions is described and claimed. In addition, methods for treating drug and multidrug resistance in various diseases using a compound, or pharmaceutically acceptable salt or solvate thereof, of this invention are described and claimed. Also, methods of enhancing oral bioavailability of a drug and methods of enhancing bioavailability of a drug to the brain using a compound, or pharmaceutically acceptable salt or solvate thereof, of this invention are described and claimed.

Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd. and C(O);Y is selected from N and CH;R.sub.1 represents C.sub.1-4 alkyl;n is 0, 1 or 2;q is 1 or 2; andZ is C.sub.5-10 alkyl optionally substituted with OH, halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy and optionally incorporating a heteroatom selected from O, N and S;and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which D4 receptor stimulation is implicated, such as schizophrenia, is also described.

Abstract: Drug and multidrug resistant modulators of Formula (C): ##STR1## where Z is selected from the group consisting of --S--, --S(O).sub.w --, and --CH.sub.2 --, where w is 1 or 2; and pharmaceutically acceptable salts or solvates thereof are described and claimed.Use of the new compounds in the preparation of pharmaceutical compositions is described and claimed. In addition, methods for treating drug and multidrug resistance in various diseases using a compound of this invention are described and claimed. Also, methods of enhancing oral bioavailability of a drug and methods of enhancing bioavailability of a drug to the brain using a compound of this invention are described and claimed.

Abstract: 10,11-Methanodibenzosuberane derivatives, i.e., the compounds of Formula I: ##STR1## wherein: A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CHR.sup.a --CH.sub.2 --, or --CH.sub.2 --CHR.sup.a --CHR.sup.b --CH.sub.2 --, where one of R.sup.a or R.sup.b is H, OH, or lower acyloxy, and the other is H;R.sup.1 is H, F, Cl or Br;R.sup.2 is H, F, Cl or Br; andR.sup.3 is heteroaryl or phenyl optionally substuted with F, Cl, Br, CF.sub.3, CN, NO.sub.2 or OCHF.sub.2 ;and the pharmaceutically acceptable salts thereof, are useful chemosensitizing agents, e.g., for cancer chemotherapy, particularly for treating multidrug resistance.

Abstract: Compounds of formulae I and II ##STR1## wherein D is H or --OR wherein R is phenyl and R.sub.1 to R.sub.4 are H or a substituent such as phenylthio, and one of the substituents R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is a group of formula III--E-CR.sub.5 =C(R.sub.6).sub.2 (III)or R is substituted by a group of formula III, wherein E is a direct bond or --X-C(O)-- wherein X is a linking group, and R.sub.5 and R.sub.6 are each independently of the other H, halogen, C.sub.1 -C.sub.12 alkyl or C.sub.6 -C.sub.10 aryl, can be polymerised to homopolymers or copolymers. The monomers and polymers are reversible photochromic systems which can be used as color indicators, as photochemically modifiable color filters, or for the optical storage of information.

Abstract: Certain ethanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R.sup.3 and R.sup.4 may be taken together to form oxo;wherein each of R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, phenalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R.sup.11 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl; wherein each of R.sup.12 and R.sup.

Abstract: The use of products of formula (I) is described, wherein X and Y represent hydrogen, hydroxy or alkoxy; and R.sub.1 and R.sub.2 represent H, alkyl, alkenyl or alkynyl, arylalkyl, acyl or R.sub.1 and R.sub.2 together with nitrogen form a heterocycle for preparing an antitumoral drug.

Abstract: A piperazine derivative represented by the following formula or a salt thereof: ##STR1## which is useful for curing cerebro-vascular disease and post-cerebro-vascular disease.

Abstract: The invention provides an indene compound represented by the following general formula (I): ##STR1## wherein R.sub.1 means a lower alkyl group, R.sub.2 and R.sub.3 denote a lower alkyl group individually or an alkylenedioxy group in combination, and R.sub.4 and R.sub.5 mean individually a substituted or unsubstituted lower alkyl or aryl group or in combination a substituted or unsubstituted piperidino, piperazinyl or homopiperazinyl group together with the adjacent nitrogen atom, with a proviso that not both R.sub.4 and R.sub.5 are a methyl group at the same time.

Abstract: A (7S,9S) isomer or its racemic modification of the aminonaphthacene derivative of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom, a hydroxyl group or a lower alkoxy group, R.sup.2 is a hydrogen atom or a hydroxyl group, R.sup.3 and R.sup.4 are each a lower alkoxy group or, when taken together, represent an ethylenedioxy group or an oxo group, A is an ethylene group optionally bearing at least one lower alkyl and Q is a hydroxyl group, a lower alkoxy group or a dimethylamino group, or an acid addition salt thereof, which is useful as an anti-tumor agent.

Abstract: The present invention relates to new tricyclic compounds of the formula: ##STR1## having valuable CNS and cardiovascular properties.

Abstract: Substituted anthranilamides of the formula ##STR1## in which R.sub.1 is hydrogen or an aliphatic, cycloaliphatic or cycloaliphatic-aliphatic hydrocarbon radical, R.sub.2 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, R.sub.3 is hydrogen or an aliphatic or substituted or unsubstituted araliphatic or heteroaryl-aliphatic hydrocarbon radical and alk and alk' are identical or different lower alkylene radicals which separate the nitrogen atoms by 2 or 3 carbon atoms, and salts thereof, possess analgesic, anti-inflammatory and anti-allergic properties and may be used as active ingredients of analgesic, anti-inflammatory and anti-allergic pharmaceuticals. They are prepared, for example, by reacting an acid of the formula ##STR2## or a reactive functional derivative thereof, with an amine of the formula ##STR3## or a reactive derivative or salt thereof.

Abstract: 10-Substituted 5-cyanomethylene-dibenzo[a,d]-cycloheptenes, their pure cis- and trans-isomers, their N-oxides and their pharmaceutically tolerated addition salts with acids, processes for their preparation, therapeutic agents containing these compounds and their use as drugs, especially as sedatives, hypnotics or tranquilizers.

Abstract: 10-Substituted 5-cyanomethylene-10,11-dihydro-dibenzo[a,d]-cycloheptenes, their pharmaceutically tolerated addition salts with acids, processes for their preparation, and their use as drugs, especially as sedatives, hypnotics or tranquilizers.

Abstract: The present invention relates to novel benzo(b) bicyclo[3.3.1]nones of the general formula I: ##STR1## and a salt or nitrogen oxide thereof, in which R.sub.1 and R.sub.2 stand for hydrogen, alkyl of 1-6 carbon atoms, alkenyl of 1-6 carbon atoms, an optionally substituted aralkyl group or an acyl group orR.sub.1 and R.sub.2 together with the nitrogen atom represent a heterocyclic 5- or 6-membered ringR.sub.3 is a free, etherified or esterified hydroxy,X and Y stand for hydrogen, hydroxy, halogen, alkyl or alkoxy of 1-6 C-atoms, nitro, CF.sub.3 or an acyloxy group, having valuable biological activities, particularly anorectic activity.

Abstract: Compounds are provided having the structure ##STR1## wherein n is 1 or 2, n.sup.1 is 0, 1 or 2 and n.sup.2 is 0, 1, 2 or 3, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may be the same or different and can be hydrogen, lower alkyl, halolower alkyl, acyl, lower alkoxy-carbonyl ##STR2## amido ##STR3## or lower alkoxyalkylene, R can be lower alkoxy, lower alkyl or cycloalkyl, R.sub.8 can be hydrogen, lower alkyl, cycloalkyl, hydroxy, dialkylaminoalkyl or R.sub.9 O(CH.sub.2)q-. X is a single bond or a straight or branched bivalent aliphatic radical and Y is ##STR4## These compounds are useful in the treatment of hypertension.

Abstract: The present invention relates to novel biologically active tricyclic compounds of the general formula: ##STR1## and salts thereof, IN WHICHR.sub.1 and R.sub.2 stand for hydroge, alkyl or alkenyl, an optionally substituted aralkyl group or an acyl group orR.sub.1 + r.sub.2 together with the nitrogen atom represent a heterocyclic 5- or 6-membered ring, andX and Y stand for hydrogen, hydroxy, halogen, alkyl or alkoxy of 1-6 carbon atoms, nitro, trifluoromethyl or an acyloxy group,Which compounds have valuable biological activities, particularly anorectic activity.