Abstract: The present invention relates to chalcone and chalcone derivatives and analogs which are useful as angiogenesis inhibitors. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good activity as angiogenesis inhibitors. The present invention also relates to the use of chalcone and its analogs as antitumor/anticancer agents and to treat a number of conditions or disease states in which angiogenesis is a factor, including angiongenic skin diseases such as psoriasis, acne, rosacea, warts, eczema, hemangiomas, lymphangiogenesis, among numerous others, as well as chronic inflammatory disease such as arthritis.

Abstract: Compounds of formula I, wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atoms; R3 represents a 5- or 6-membered heterocyclic ring, the ring being optionally substituted; R4 represents a 4-, 5-, 6-, or 7-membered heterocyclic ring, the ring being optionally fused to a benzene ring or 5- or 6-membered heterocyclic ring, the ring system as a whole being optionally substituted; L is absent; and pharmaceutically acceptable salts thereof; are useful in therapy, in particular in the treatment of benign prostatic hyperplasia.

Abstract: Compounds of the formula 1

Abstract: Compounds of the formula 1

Abstract: A benzimidazole compound represented by the formula (I): wherein R3 is a carboxyl group, a esterified carboxyl group, an amidated carboxyl group, an amino group, an amido group, or a sulfonyl group, or their pharmaceutically acceptable salts. Because of their blood sugar-depressing effect or PDE5 inhibitory effect, these compounds or salts thereof are useful as medicines for treating impaired glucose tolerance, diabetes, diabetic complications, syndrome of insulin resistance, hyperlipidemia, atherosclerosis, cardiovascular disorders, hyperglycemia, or hypertension; or stenocardia, hypertension, pulmonary hypertension, congestive heart failure, glomerulopathy, tubulointerstitial disorders, renal failure, atherosclerosis, angiostenosis, distal angiopathy, cerebral apoplexy, chronic reversible obstructions, allergic rhinitis, urticaria, glaucoma, diseases characterized by enteromotility disorders, impotence, diabetic complications, nephritis, cancerous cachexia, or restenosis after PTCA.

Abstract: The present invention relates to novel 3-(substituted)-2-indolinones compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related disorders such as cancer.

Abstract: The present invention relates to pharmaceutical compositions containing, as active ingredient, a compound of formula: 1

Abstract: 1

Abstract: The present application describes novel cyclic &bgr;-amino acid derivatives of formula I: 1

Abstract: The present invention relates to compounds of the formula wherein R1 is hydrogen, lower alkyl, lower alkoxy, hydroxy, amino, nitro, cyano, lower alkyl-amino, di-lower alkyl-amino or halogen; R2 is hydrogen, lower alkyl, amino, pyrrolidin-3-ol, pyrrolidin-2-yl-methanol or —NHCH2CHROH; R3 is hydrogen or halogen; R is hydrogen, lower alkyl or —CH2OH; n is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof which are are NMDA(N-methyl-D-aspartate)-receptor subtype selective blockers.

Abstract: The present invention relates a process for producing the quinoline derivative (3) via the nitrile compound (1) obtained by reacting the aldehyde compound represented by formula (2) with diethyl cyanomethylphosphonate and its intermediate (1).

Abstract: The invention relates to 1-aminoethylquinoline derivatives, to pharmaceutical compositions containing them, to therapeutic methods of using them and to processes for preparing them.

Abstract: The present invention provides compounds of the formula where R1-R5 are each, independently, a hydrogen atom or a normal or branched C1-C6-alkyl group; A is a methionyl, phenylalanyl or phenylglycyl residue; n is 0 or 1; R6 is a hydrogen atom; and R7 is a carbocylic group, an aromatic group, a C1-C4-alkyl group, a pyridylalkyl group or a heterocyclic group. In another embodiment, R6 is benzyl or —C(O)OR8, where R8 is a C1-C6-alkyl group, and R7 is a heteroaromatic group, such as a 2-thiazolyl group.

Abstract: Compounds having the formula: 1

Abstract: Substituted propanolamine derivatives and pharmaceutically tolerated salts and physiologically functional derivatives thereof are described. Also described are compounds of formula (I), in which the radicals have the meanings given in the specification and claims, and physiologically tolerated salts and physiologically functional derivatives thereof, and processes for their preparation, are described. The compounds are suitable, for example, as hypolipidemic agents.

Abstract: There are described compounds of formula I*, wherein R1 is lower alkoxycarbonyl, R2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl, R3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C4-C8cycloalkyl, R4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, suffinyl (—SO—) and sulfonyl (—SO2—) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl, R5, independently of R2, has one of the meanings mentioned for R2, and R6, independently of R1, is lower alkoxycarbonyl, or salts thereof, provided that at least one salt-forming group is present. The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS.

Abstract: Disclosed are aryl and heteroaryl substitated pyridino compounds. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.

Abstract: The invention concerns new guanidine derivatives of formula (I), methods of preparing them and their use in drugs containing such compounds.

Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.

Abstract: 7-Aza-bicyclo[2.2.1]-heptane and -heptene derivatives are disclosed that can be administered to a mammal, including a human, to treat disorders associated with a decrease or increase in cholinergic activity.

Abstract: Compounds of formula I are useful antidepressant agents demonstrating potent inhibition of 5-HT reuptake. Z is selected from among various phenyl and hetaryl moieties while Y is benzyl or indolyl.

Abstract: The cycloalkano-pyridines are prepared by reacting corresponding cycloalkano-pyridine-aldehydes with suitable organometallic compounds or Wittig or Grignard reagents or reacting compounds of the cycloalkano-pyridine alcohols type with suitable bromine compounds, and optionally varying the functional groups accordingly. The cycloalkanopyridines are suitable as active compounds in medicaments, in particular in medicaments for the treatment of hypertipoproteinaemia and arteriosclerosis.

Abstract: This invention relates to a method of making N-benzyl indoles, and to intermediates for use in the method, and to certain substantially optically pure N-benzyl indoles obtained by the method.

Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

Abstract: Piperidine derivatives, their manufacture and use as medicaments, are disclosed. The invention is concerned with the piperidine derivatives of general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, Q, X, Z, m and n are as described herein.

Abstract: Aminoalkyl and acylaminoalkyl ethers which are distinguished by high affinity for the bradykinin B.sub.2 receptor and improved solubility in water are described. These aminoalkyl and acylaminoalkyl ethers can be represented by the formula (I) ##STR1## in which R.sup.1,R.sup.2,R.sup.3 are alkyl, aryl, alkylaryl, halogen, hydrogen, cycloalkyl, CHO, CO--O-alkyl, COOH; R.sup.4, R.sup.5 are hydrogen, halogen, alkoxy, nitro, cyano, S-alkyl; n is a number from 1 to 8; R.sup.6 is hydrogen, alkyl, alkylalkenyl, alkylaryl; R.sup.7 is hydrogen and a substituted or unsubstituted acyl radical. A process for preparing the compounds of the formula (I) is likewise described.

Abstract: Organometallic iron complexes containing one or more basic structural components characterizing a molecule with antimalarial properties such as quinine, chloroquinine or mepacrine, as well as one or more iron atoms are described. The complexes of the invention are more particularly characterized in that they contain one or more ferrocene groups.

Abstract: This invention provides compounds of formula (1) ##STR1## wherein the substituents are described in the specification. The compounds of formula (1) are plant fungicides.

Abstract: The present invention is directed to a piperidine derivative represented by the following formula (1) or a salt thereof: ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 individually represent hydrogen atoms, etc., Y represents ##STR2## B represents a single bond, an alkylene group, --S--CH.sub.2 --, or --CH.dbd.CH--, E represents a single bond or a trimethylene group, Z represents an oxygen atom, etc., and n represents a number between 2 and 5 inclusive; and to a medicine containing the compound. The medicine according to the present invention is endowed with excellent anti-histaminic activity and antileukotriene activity, and exhibits reduced side effects such as drowsiness.

Abstract: The invention relates to methods for the treatment of central nervous system disorders, neurological disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising an effective amount of certain sigma receptor ligands to a patient in need of such treatment. The invention further relates to novel sigma receptor ligands having high binding to the sigma receptor and pharmaceutical compositions thereof.

Abstract: Described are novel water soluble photochromic naphthopyran and benzopyran compounds having an alkylaminoalkylamino group on the pyran portion or on the pyran portion and the naphtho- or benzo-portion thereof. These compounds may be represented by one of the following graphic formula: ##STR1## wherein B and/or B' is an alkylaminoalkylamino-substituted aryl group and R.sub.1 may also be an alkylaminoalkylamino group. Articles such as ophthalmic lenses or other plastic transparencies and coating compositions such as paints and inks that incorporate the novel water soluble compounds are also described.

Abstract: The cycloalkano-pyridines are prepared by reacting corresponding cycloalkano-pyridine-aldehydes with suitable organometallic compounds or Wittig or Grignard reagents or reacting compounds of the cycloalkano-pyridine alcohols type with suitable bromine compounds, and optionally varying the functional groups accordingly. The, cycloalkanopyridines are suitable as active compounds in medicaments, in particular in medicaments for the treatment of hyperlipoproteinaemia and arteriosclerosis.

Abstract: Carboxamide derivatives of pyrrolidine, piperidine, and hexahydroazepine of formula (I): ##STR1## are disclosed as useful in treating platelet-mediated thrombotic disorders.

Abstract: The present invention provides an amino compound represented by Formula: ##STR1## wherein X is CH.sub.2 NH or CONH, Y is CH.sub.2 NH or CONH with the proviso that X and Y are not CONH at the same time; Z is CH.dbd.C(R.sup.4)R.sup.5, CH.sub.2 CH(R.sup.4)R.sup.5 or an alkoxycarbonyl group, R.sup.1 is a hydrogen atom; a lower alkyl group, a cycloalkyl group, a cycloalkyl-substituted alkyl group, an aralkyl group or an aryl group, each group of which is substituted or unsubstituted, R.sup.2 and R.sup.3 are each independently a lower alkyl group or an aralkyl group, each group of which is substituted or unsubstituted, and R.sup.4 and R.sup.

Abstract: The present invention is directed to compounds that act as analgesics and that have the structure of formula (I): ##STR1## wherein; Z is ##STR2## wherein, n is 1 or 2, and R.sub.0 is C.sub.6-12 aryl or C.sub.7-8 aralkyl; orR.sub.1 is selected from the group consisting of hydrogen; --NH--C.sub.1-6 alkyl; C.sub.1-6 alkyl; C.sub.6-12 aryl; C.sub.7-18 aralkyl; arginyl; and R.sub.30 NHC(.dbd.NH)--, wherein R.sub.30 is hydrogen, C.sub.6-12 aryl, C.sub.7-18 aralkyl, or C.sub.1-6 alkyl;R.sub.2 is hydrogen; C.sub.1-6 alkyl; or OH;R.sub.3 is C.sub.6-12 aryl; C.sub.7-18 aralkyl; --CH.sub.2 --C.sub.6 H.sub.2 R.sub.8 R.sub.9 ;or --CH.sub.2 --OHC.sub.6 HR.sub.8 R.sub.9, wherein each of R.sub.8 and R.sub.9 is independently, or hydrogen;R.sub.4 C.sub.6-12 aryl; C.sub.7-18 aralkyl; C.sub.1-12 alkyl; or a substituted or unsubstituted cyclohexyl;R.sub.5 is C.sub.1-6 alkyl; hydrogen; OH; halogen; SH; NO.sub.2 ; NH.sub.2 ; --NH--C.sub.1-6 alkyl; NH.sub.2 C (.dbd.NH--; NH.sub.2 C (.dbd.NH)--NH--; COOR.sub.31, wherein, R.sub.

Abstract: The present invention relates to pharmaceutically acceptable compounds, including certain substituted indolinyl and derivatives thereof, 1,2,3,4-tetrahydroquinolinyl and derivatives thereof, 1,2,3,4-tetrahydroisoquinolinyl, benz[cd]indolinyl and 5,6-dihydrophenanthridinyl compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.

Abstract: This invention relates to a compound of formula (I) wherein A.sup.1 is lower alkylene, R.sup.1 is substituted quinolyl, etc., R.sup.2 is hydrogen, halogen or lower alkyl, R.sup.3 is halogen or lower alkyl, and R.sup.4 is a group of the formula: -Q-A.sup.2 -R.sup.5, etc., in which R.sup.5 is amino, acylamino, etc., A.sup.2 is lower alkylene or a single bond, and Q is a group of formula (a), and pharmaceutically acceptable salts thereof, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to methods of using the same therapeutically in the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.

Abstract: The present invention is concerned with compounds of formula (I), ##STR1## the stereoisomeric forms thereof and the pharmaceutically acceptable acid or base addition salts thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; R.sup.1 is hydrogen, C.sub.1-12 alkyl, Ar.sup.1, Ar.sup.2 C.sub.1-6 alkyl, quinolinylC.sub.1-6 alkyl, pyridylC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.1-6 alkyloxyC.sub.1-6 alkyl, mono- or di(C.sub.1-6 alkyl)-aminoC.sub.1-6 alkyl, aminoC.sub.1-6 alkyl, or a radical of formula --Alk.sup.1 --C(.dbd.O)--R.sup.9, --Alk.sup.1 --S(O)--R.sup.9 or --Alk.sup.1 --S(O).sub.2 --R.sup.9 ; R.sup.2 and R.sup.3 each independently are hydrogen, hydroxy, halo, cyano, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, hydroxyC.sub.1-6 alkyloxy, C.sub.1-6 alkyloxy-C.sub.1-6 alkyloxy, aminoC.sub.1-6 alkyloxy, mono- or di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkyloxy, Ar.sup.1, Ar.sup.2 C.sub.1-6 alkyl, Ar.sup.2 oxy, Ar.sup.2 C.sub.1-6 alkyloxy, hydroxycarbonyl, C.sub.

Abstract: The present invention relates to hitherto unknown compounds of formula (I) in which R.sub.1 is hydrogen or halogen, preferably fluorine or chlorine, and m is 0, 1 or 2. The present compounds are of value in the human and veterinary practice as leukotriene antagonists.

Abstract: This invention relates to compounds that are antagonists of dopamine D4 receptors, to methods of treating psychosis and schizophrenia using a compound that is an antagonist of dopamine D4 receptors, and to pharmaceutically acceptable compositions that contain a dopamine D4 receptor antagonist.

Abstract: Quinolylmethylen-oxindole derivatives having general formula (I), wherein R is H or --(CH.sub.2).sub.n --COR.sub.7 group in which n is an integer of 1 to 4 and R.sub.7 is hydroxy, amino, C.sub.1 -C.sub.6 alkoxy or --NR.sub.5 R.sub.6 in which one of R.sub.5 and R.sub.6 is hydrogen or C.sub.1 -C.sub.6 alkyl and the other is C.sub.1 -C.sub.6 alkyl or R.sub.5 and R.sub.6 taken together with the N atom to which they are linked form a 5 to 7 membered saturated heteromonocycle or R.sub.7 is a N-terminally linked peptidyl residue containing from 1 to 3 aminoacids in which the terminal carboxyl group may be present as such, as amide, as alkali metal salt or as a C.sub.1 -C.sub.4 alkyl ester, one or two of R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, are selected from: a) --X--(CH.sub.2).sub.m --NH.sub.2, --X--(CH.sub.2).sub.m --NR.sub.5 R.sub.6 or --X--(CH.sub.2).sub.m --NHR.sub.8 group; b) --NH--C(.dbd.NH)--NR.sub.5 R.sub.6, --NH--C(.dbd.NH)--NHR.sub.8, --N.dbd.CH--NH.sub.2, --N.dbd.

Abstract: 2-Methyl-4,4a-dihydro-3H-carbazolium salts that are useful as dye precursors and dyes derived from those precursors are disclosed. The salts are described by the formula ##STR1## wherein R.sup.1 represents an alkyl, aryl, sulfoalkyl, carboxyalkyl, sulfatoalkyl, alkoxyalkyl, acyloxyalkyl, dialkylaminoalkylene, cycloaminoalkylene, acyl, or alkenyl group having from 1 to 18 carbon atoms; R.sup.2 represents an alkyl group having up to 18 carbon atoms; R.sup.3 represents hydrogen or an alkyl group having from 1 to 18 carbon atoms; R.sup.4 represents hydrogen or an alkyl group having from 1 to 18 carbon atoms; R.sup.5 represents hydrogen, nitro, carboxyl, sulfo, hydroxy, halogen, phospho, or an alkoxy, thioalkoxy, oxyalkyl, acyl, alkyl, aryl, or amino group having up to 18 carbon atoms; wherein any two groups R.sup.5, or R.sup.4 and a group R.sup.5, or R.sup.1 and R.sup.

Abstract: Described are novel water soluble photochromic naphthopyran and benzopyran compounds having an alkylaminoalkylamino group on the naphtho- or benzo-portions and/or pyran portions thereof. These compounds may be represented by one of the following graphic formulae: ##STR1## wherein R.sub.1 is an alkylaminoalkylamino group. Articles such as ophthalmic lenses or other plastic transparencies and coating compositions such as paints and inks that incorporate the novel water soluble compounds are also described.

Abstract: The invention relates to substituted propanolamine derivatives and their acid addition salts.Propanolamine derivatives of formula I, ##STR1## in which R.sup.1 to R.sup.8 have the meanings indicated in the specification, and their physiologically tolerable salts and processes for their preparation are described. The compounds are suitable, for example, as hypolipidemics.

Abstract: This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human .alpha..sub.2 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the .alpha..sub.2 receptors may be useful. The invention further provides for a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Abstract: Using the fluorescent group-containing carbodiimide compound represented-by the following formula (I) as the label and the like in the nucleic acid detection method, immunoassay, or chemiluminescence assay, labeling can be made efficiently for a short time, a nucleic acid derived from nature can be labelled, and highly sensitive assay is enabled.B--Y.sup.3 --N.dbd.C.dbd.N--Y.sup.2 --W--Y.sup.1 --?A!.sub.n --F(I)wherein F represents a fluorescent group;A represents a moiety selected from the group consisting of --CH.sub.2 --, --NHCO--, --CONH--, --O--, --S--, --NR-- wherein R is an alkyl group, --COO--, --OCO--, --NHSO.sub.2 --, and --SO.sub.2 NH--;n is 0 or 1;W represents a direct bond or a quaternary ammonium group;Y.sup.1, Y.sup.2 and Y.sup.3 each represents an alkylene group which may have a functional group in its main chain; andB represents H or a monovalent organic group which may be the same as or different from that represented by --W--Y.sup.1 --?A!.sub.n --F.

Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

Abstract: Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols are defined as follows: R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each directly bonded to a ring carbon and are each independently(a) hydrogen;(b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z.sup.1, Z.sup.2 and Z.sup.3 ;(c) halo;(d) hydroxyl;(e) cyano;(f) nitro;(g) --C(O)H or --C(O)R.sup.5 ;(h) --CO.sub.2 H or --CO.sub.2 R.sup.5 ;(i) --Z.sup.4 --NR.sup.6 R.sup.7 ;(j) --Z.sup.4 --N(R.sup.10)--Z.sup.5 --NR.sup.8 R.sup.9 ; or(k) R.sup.3 and R.sup.4 together may also be alkylene or alkenylene, either of which may be substituted with Z.sup.1, Z.sup.2 and Z.sup.3, completing a 4- to 8-membered saturated, unsaturated or aromatic ring together with the carbon atoms to which they are attached;and the remaining symbols are as defined in the specification.

Abstract: Compounds of Formula I ##STR1## useful in the treatment of inflammatory disorders.