Abstract: Intermediate compounds having the formula wherein the substituents are defined as set forth in the disclosure.

Abstract: This invention provides novel bicyclic compounds of Formula (I): 1

Abstract: Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.

Abstract: The present invention relates to processes for the production of &agr;-aryl-&bgr;-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.

Abstract: A first process for producing an optically active perfluoroalkylcarbinol derivative includes (a) reacting an optically active imine with a compound that is a hemiacetal of a perfluoroalkylaldehyde or a hydrate of a perfluoroalkylaldehyde to obtain a condensate; and (b) hydrolyzing the condensate under an acid condition. A second process for increasing optical purity of an optically active 4,4,4-trifluoro 3-hydroxy-1-aryl-1-butanone derivative includes (a) precipitating a racemic crystal of the derivative, from the derivative; and (b) removing the racemic crystal from the derivative. A third process for increasing optical purity of the butanone derivative includes recrystallizing the derivative. Novel compounds are optically active and inactive 4,4,4-trifluoro-3-hydroxybutanoic aryl ester derivatives.

Abstract: This invention relates to novel substituted succinic acid metallo-&bgr;-lactamase inhibitors which are useful potentiators of &bgr;-lactam antibiotics.

Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.

Abstract: A compound of formula (I): wherein: G represents a group such as: wherein R1 and R2 independently represent a hydrogen atom or an alkyl, cycloalkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl or heteroarylalkyl group, or, R1 and R2 together with the nitrogen atom form a heterocycloalkyl group, R3 represents a hydrogen atom or an alkyl or optionally substituted phenyl group, Ra represents a hydroxy group, a linear or branched (C1-C6)alkoxy group or an amino group, Rb and Rc, which may be identical or different, each represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, a hydroxy group or a trihaloalkyl group, m is an integer of from 0 to 1 inclusive, n and q are integers of from 0 to 6 inclusive, p and r are integers of from 1 to 6 inclusive, its enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base; and medicinal products containing the same which are useful as a TXA2 recept

Abstract: The present application describes modulators of MCP-1 of formula (I): 1

Abstract: Para-alkyl, aryl, cycloheteroalkyl or heteroaryl [carbonyl or sulfonyl] amino substituted phenyl amides active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.

Abstract: New compounds of formula I are described: 1

Abstract: The present invention relates to processes for the preparation of any of the intermediate 1,3-substituted indenes of the formulae (Ia), (Ib) and (Ic) or a mixture thereof: 1

Abstract: An S,S-ethylenediamine-N,N′-disuccinic acid iron alkali salt which contains a lactam compound represented by the following general formula (1): wherein M is an ammonium ion or an alkali metal ion, and an ethylenediaminemonosuccinic acid represented by the following general formula (2): wherein M is an ammonium ion or an alkali metal ion, in an amount of 7 wt % or less, respectively.

Abstract: The present invention provides a process for producing intermediates of antibacterial agents in accordance with the following steps and intermediates in the production thereof.

Abstract: The present invention is directed to certain novel compounds represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein R3, R5, R6, R7, R8, R11, R12, R13, Q, W, X, Y and Z are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of psychiatric disorders including depression and anxiety.

Abstract: The compounds represented by the formula (I), and pharmacologically acceptable salts and solvates thereof are disclosed. The compound is hydrolyzed in organisms into a compound represented by the formula in which W represents a hydrogen atom, and D represents the group —V—(CH2)p—COOR, wherein R represents a hydrogen atom. The compound inhibits the aggregation of platelets via the inhibition of the linkage of the platelet membrane protein GPIIb/IIIa to fibrinogen. wherein A represents CH2 or CO, B represents the group —(CH2)k— or —(CH2)m—CO—, X and Y are different from each other and represent N or CH, W represents an ester moiety which can be removed under the physiological condition, and Z represents the groups (II) or (III): wherein D represents the group —V—(CH2)p—COOR.

Abstract: This disclosure relates to the use of &agr;,&agr;-dibromo-&agr;-chloroacetophenone compounds as intermediates for the preparation of aromatic carbonyl compounds, especially aromatic amides. The compound 2,5-bis(2,2,2-trifluoroethoxy)-&agr;,&agr;-dibromo-&agr;-chloroacetophenone is especially useful as an intermediate for the preparation of flecainide, a known pharmaceutical.

Abstract: The present invention relates to cyclic amine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.

Abstract: The present invention relates N-substituted glycine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.

Abstract: An amide compound of the formula (I): wherein R is amino and the like, A is alkylene and the like, X is O, S and the like, M is arylene and the like, R1, R2, R3 and R4 are H, hydroxy and the like, R5 is H, alkyl and the like, m is an integer of 0-6, R6 is an optionally substituted aryl and the like, and R7 is H, an optionally substituted alkyl and the like, a pharmaceutically acceptable acid addition salt thereof and a pharmaceutical containing same as an active ingredient. The amide compounds exhibit superior suppressive effects on cytokines directly or indirectly involved in inflammations, such as IL-8, IL-1, IL-6, TNF-&agr;, GM-CSF and the like, and are useful for the prophylaxis and treatment of rheumatic diseases, arthritis due to gout and the like.

Abstract: This invention is directed to novel (substituted)acyl dipeptidyl ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.

Abstract: The present invention relates to new aminoindane piperidine compounds, the method of using aminoindane compounds as local anesthetics, said compounds having particularly valuable properties as dermal and topical anesthetics in mammals, including man, as well as compositions containing said compounds.

Abstract: The present invention relates to benzofuran derivatives represented by following general formula (I): wherein R1 represents lower alkyl, R2 represents hydrogen or substituted or unsubstituted lower alkyl, R3, R4, R5 and R6 independently represent hydrogen or lower alkyl, X represents CH2 or C═O, and Y represents CH2 or NH, or pharmaceutically acceptable salts thereof.

Abstract: The present invention provides a linker binding carrier for organic synthesis represented by the formula: —Z—W—(SO2X)m wherein  is a carrier, X is a leaving group, Y is a bond or spacer, Z is a bivalent group, when Z is a bivalent electron attractive group, W is an aromatic ring which may be substituted and when Z is a bivalent non-electron attractive group, W is an aromatic ring which is substituted by an electron attractive group and may be further substituted and m is 1 or 2, or a salt thereof, which is useful for synthesizing a novel organic compound.

Abstract: Compounds having Formula 8 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.

Abstract: The present application describes novel substituted aryl hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring A is a 5-8 membered ring containing from 0-1 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.

Abstract: Novel compounds of the general formula: 1

Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3, &agr;v&bgr;5, and/or &agr;v&bgr;6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.

Abstract: A compound selected from the group consisting of a compound of the formula wherein A is selected from the group consisting of and the other substituents are defined in the specification having an inhibitory activity of NO-synthase enzymes producing nitrogen mono-oxide and/or an activity which traps the reactive oxygen species.

Abstract: Processes for the preparation of derivatives of hydroxyphenylsulfanylbenzoic and hydroxyphenylsulfanylarylacetic acids of Formula (I) and pharmaceutical compositions including these compounds are provided: wherein X is H, halogen or NO2 group, n is 0 or 1, and m is 2 to 4 if Z is either 4-acetyl-3 -hydroxy-2-propylphenoxy of Formula (II): or a piperazinyl residue, or m is 1 if Z is quinolin-2-yl or 6-chloroquinoli-2-yl.

Abstract: An S,S-ethylenediamine-N,N′-disuccinic acid iron alkali salt which contains a lactam compound represented by the following general formula (1): wherein M is an ammonium ion or an alkali metal ion, and an ethylenediaminemonosuccinic acid represented by the following general formula (2): wherein M is an ammonium ion or an alkali metal ion, in an amount of 7 wt % or less, respectively.

Abstract: Disclosed are compounds of formula I: 1

Abstract: A process for the production of a Mannich reagent comprises reacting formaldehyde, especially paraformaldehyde, with a secondary amine in the complete or almost complete absence of a solvent. An alternative comprises reacting a diaminomethane produced from a secondary amine, formaldehyde, especially paraformaldehyde, as well as water with one another in about equimolar amounts. The invention is also concerned with a process for the aminomethylation of &dgr;-tocopherol or of tocopherol mixtures containing this and comprises using a Mannich reagent which has been produced in the above manner. After completion of this aminomethylation process excess Mannich reagent can be separated by distillation and can be reacted with water and formaldehyde, especially paraformaldehyde, in order to regenerate further Mannich reagent suitable for use in the aminomethylation, this regeneration representing a further aspect of the invention. Finally, the invention includes certain novel bis(aminomethyl)-&ggr;-tocopherols.

Abstract: A process is disclosed for the preparation of a piperazine-substituted aliphatic carboxylate having the formula where m and n are individually an integer of from 1 to 6, R and R′ are the same or different and are hydrogen, C1 to C6 alkyl or aryl or heteroaryl that is unsubstituted or is substituted with at least one substituent that is halo, C1 to C6 alkyl or C1 to C6 alkoxy and R″ is C3 to C12 branched alkyl or an organic or inorganic cation. The process comprises treating a solution comprising a compound of the formula wherein m, R and R′ are as defined above and an aliphatic ester of the formula X—(CH2)n—O—CH2—CO(O)R″ where X is a leaving group and n and R″ are as defined above, with an effective amount of a base for a time and at a temperature sufficient to form a piperazine-substituted aliphatic carboxylate.

Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.

Abstract: Disclosed are compounds of formula I: wherein X is a carbonyl, sulfonyl, methylene, or methylene substituted with optionally substituted phenyl; Z is nitrogen or CH; Ar1 and Ar2 independently represent aryl groups; and Y is hydrogen; or Y and R1 or R2 together represent CH2;CH2CH2; CH2O; CH2S forming a five or six membered ring and such ring may be optionally substituted with loweralkyl or phenyl; or the pharmaceutically acceptable salts thereof, useful in the treatment of neoplastic diseases, and bacterial or fungal infections, and in preventing or decreasing the production of abnormally phosphorylated paired helical filament (PHF) epitopes associated with Alzheimer's Disease and, therefore, useful for treating Alzheimer's Disease.

Abstract: A family of compounds capable of inhibiting the activity of prenyl transferases. The compounds are covered by the four following formulas Each of the R groups is defined in the disclosure.

Abstract: Compounds of the formula ##STR1## which inhibit leukocyte adhesion mediated by interaction of the .alpha..sub.4 .beta..sub.1 integrin (VLA-4) with its counterreceptor VCAM-1, and their use for the treatment of inflammatory and autoimmune diseases.

Abstract: Novel bicyclic aryl/bicyclic heterocyclic ring containing compounds having a combined 5HT.sub.1A, 5HT.sub.1B and 5HT.sub.1D receptor antagonistic activity are provided.

Abstract: Novel substituted [2-(1-piperazinyl)ethoxy]methyl compounds.The present invention related to novel substituted [2-(1-piperazinyl)-ethoxy]methyl compounds of formula ##STR1## in which R.sub.1 represents a --CONH.sub.2, --CN, --COOH, --COOM or --COOR.sub.3 group, M being an alkali metal and R.sub.3 being an alkyl radical having from 1 to 4 carbon atoms; andR.sub.2 represents a hydrogen atom or a group --COR.sub.4 or --R.sub.5, where R.sub.4 is chosen from the groups --OR.sub.6 or --R.sub.7, in whichR.sub.5 represents an allyl or alkylaryl radical,R.sub.6 represents a linear or branched alkyl radical having from 1 to 4 carbon atoms, a haloalkyl, alkylaryl, alkylnitroaryl or alkylhaloaryl radical, andR.sub.

Abstract: The present invention provides compounds having the Formula I ##STR1## The present invention also provides methods of treating atherosclerosis, coronary heart disease, and restenosis using the compounds of Formula I, and pharmaceutical compositions comprising the compounds of Formula I.

Abstract: The present invention provides novel hydroxylamine derivatives represented by the general formula: wherein:X is O, --NH, or a group of formula NR', wherein R and R' are independently selected from alkyl, cycloalkyl, phenylalkyl, phenyl optionally substituted with halo, haloalkyl,alkyl, alkoxy or nitro; and a N-containing heterocyclic ring;R.sup.1 is H or alkanoyl,R.sup.2 is H or hydroxy optionally acylated with alkanoyl, andR.sup.3 is a group of the formula --NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently selected fromH, alkyl, and a group of the formula --CO--NH--R wherein R is as defined above, orwherein R.sup.4 and R.sup.5 when taken together form a 5- to 7-membered heterocyclic ring which may optionally contain one additional hetero atom selected from nitrogen, oxygen and sulfur and which is optionally substituted with alkyl or phenylalkyl.

Abstract: Described herein are compounds of the general formula: ##STR1## a stereoisomer, solvate, or pharmaceutically acceptable salt thereof, wherein:R.sub.1 is H, halo, aryl or aryl substituted with one or two groups independently selected from halo, C.sub.1-4 alkyl, C.sub.1-4 -alkoxy, nitro, trifluoromethyl, trifluoromethoxy or cyano;R.sub.2 is C.sub.4-9 alkyl; phenyl or phenyl substituted with one or two groups selected independently from OH, cyano, halo, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, trifluoromethyl, trifluoromethoxy, nitro or phenyl; naphthyl;phenyl fused to a 5 or 6-membered heterocycle; the coumarin moiety ##STR2## wherein R.sub.3 and R.sub.4 are selected independently from H, C.sub.1-4 alkyl and C.sub.1-4 alkoxy;or 1,2-methylenedioxy phenyl;with the proviso that R.sub.2 is not phenyl or 3,4-dimethoxyphenyl when R.sub.1 is H.Also described is their use as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia and anxiety.

Abstract: A process is described for preparing a compound of the formula or the S-enantiomer thereof,wherein:R is alkyl, aryl, cycloalkyl, aralkyl, or cycloalkylalkyl,R.sup.1 is halogen;R.sup.2 is halogen, alkyl, cycloalkyl, aryl or ##STR1## wherein the process comprises treating the associated racemic alcohol with an acylatingagent ##STR2## (wherein L is a leaving group) and an enzyme or microorganism capable of enantioselective acylation. This process may also be used to isolate the unreacted R- or S-alcohol. The acylated product may be enantioselectively hydrolyzed with a lipase or lipase-supplying microorganism to the S- or R-alcohol. Compounds prepared by this invention are useful antipsychotic agents or useful intermediates therefor.

Abstract: A compound selected from the group consisting of a compound of the formula wherein A is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and --NO.sub.2, E is --O-- or a covalent bond, n is an integer from 1 to 12, R.sub.1 and R.sub.2 are individually alkyl of 1 to 6 carbon atoms or taken together with the nitrogen to which they are attached form an optionally unsaturated 5 to 6-member ring of the formula --NX and X is selected from the group consisting of oxygen, sulfur, methylene and >N--R', R' being hydrogen or an alkyl of 1 to 6 carbon atoms, and their pharmaceutically acceptable acid addition salts useful to inhibit --NO synthase.

Abstract: Di-N-substituted piperazine or 1,4-di-substituted piperidine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein Q, n, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations with acetyl-cholinesterase inhibitors of compounds capable of enhancing acetylcholine release and having the above formula.

Abstract: The present invention relates to novel compounds of the general formula I ##STR1## which can be used for treating medical disorders resulting from a deficiency in growth hormone.

Abstract: Novel piperazine derivatives of formula I:Y--(C.sub.m H.sub.2m --CHR.sup.1).sub.n --CO--(NH--CHR.sup.2 --CO).sub.r -- Zwherein ##STR1## R.sup.1, R.sup.2 and R.sup.7 are each, independently, --C.sub.t H.sub.2t --R.sup.9, benzyl, hydroxybenzyl, imidazolylmethyl or indolylmethyl;R.sup.3 is H or H.sub.2 N--C(.dbd.NH)--;R.sup.4 and R.sup.6 are each, independently, (H,H) or .dbd.O;R.sup.5 is H, H.sub.2 N--C(.dbd.NH)-- or H.sub.2 N--C(.dbd.NH)--NH;R.sup.8 is OH, OA or NHOH;R.sup.9 is H, OH, NH.sub.2, SH, SA, COOH, CONH.sub.2 or NH--C(.dbd.NH)--NH.sub.2 ;A is in each case, independently, alkyl having 1-4 C atoms;m and t are each, independently, 0, 1, 2, 3 or 4;n and r are each, independently, 0 or 1; andp is 0, 1 or 2,inhibit the binding of fibrinogen to the fibrinogen receptor and can be used for the treatment of thrombosis, apoplexy, cardiac infarctus, inflammation, arteriosclerosis and tumors.

Abstract: The invention relates to triphenylalkyl antibacterial compounds of the general formula: ##STR1## pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of a bacterial histidine protein kinase and are thus useful as anti-infective agents against a variety of bacterial organisms, including organisms which are resistant to other known antibiotics.

Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.