Abstract: Provided is an acrylic acid ester derivative which, when used as a constituent unit of a polymer which is included in a photoresist composition for a semiconductor, exhibits excellent lithography characteristics such as LWR and the like. Specifically, provided is an acrylic acid ester derivative represented by the following general formula (1). Furthermore, provided are an intermediate of the acrylic acid ester derivative and a process for producing the same; a polymer containing the acrylic acid ester derivative as a constituent unit; and a photoresist composition for a semiconductor containing the polymer. wherein, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, m, x, and y are as defined in the text of Description.

Abstract: Benzoylthiourea or benzoylthiourethane derivatives as cure accelerators in primers for two step adhesive systems are provided.

Abstract: The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.

Abstract: The present invention discloses and claims a series of substituted N-phenyl-pyrrolidinylmethylpyrrolidine amides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted pyrrolidinylmethylpyrrolidine amides and intermediates therefor.

Abstract: The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.

Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.

Abstract: The present invention is directed to the preparation of novel compounds useful in the treatment of hyperlipidemia, arteriosclerosis, hypercholesterolemia, and other related metabolic disorders. More specifically, the present invention is a novel process for the preparation of 1,4-diphenylazetidinone derivatives from ?-substituted amino amides which are protected in the presence of silylating agents and at least one cyclization catalyst whose structural formula is represented by one of the general formula: wherein the various R-groups are defined herein.

Abstract: Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.

Abstract: Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.

Abstract: Rifamycin derivatives having the following structure of general formula I (both hydroquinone and corresponding quinone (C1-C4) forms): or its salts, hydrates or prodrugs thereof; wherein a preferred R1 comprises hydrogen or acetyl and a prefered R2 comprises hydrogen, methyl or other lower alkyls; wherein asterik (*) denotes the carbon bearing the chiral center, wherein absolute configuration is assigned as R or S. Methods of preparation of the aforementioned rifamycin derivatives are also described. The compounds exhibit antimicrobial activities, including activities against drug-resistant microorganisms.

Abstract: A compound of formula (I) wherein A and B are optionally substituted cyclohexenyl or phenyl groups, X is carbonyl or sulfonyl, and Y is 5–7 atoms-linker, is useful as histone deacetylase inhibitors, particularly for inhibiting cell proliferation.

Abstract: Isothiazoloanthrones, isooxazoloanthrones, isoindolanthrones, and derivatives thereof having the general formula: and pharmaceutically acceptable salts thereof, wherein R0 is —CH2—, —SO—, —O—, —SO2—, or —S—; compositions comprising the isothiazoloanthrones, isooxazoloanthrones, isoindolanthrones, and derivatives thereof; and methods for treating or preventing a disorder alleviated by inhibiting Jun N-terminal kinase (JNK) by administering the isothiazoloanthrones, isooxazoloanthrones, isoindolanthrones, and derivatives thereof are described herein.

Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.

Abstract: Chiral chelating agents and chiral catalysts, which are formed from the chiral chelating agents and metal, are described. One chiral chelating agent has a general formula (1) as illustrated below: wherein R represents H, methyl, ethyl, a primary, secondary or tertiary straight, branched or cyclic alkyl group having 3-7 carbon atoms, a heterocyclic or aromatic group, an aromatic group substituted at the 2-, 3- or 4-position, an aromatic-like group, or a naphthyl or naphthyl-derived group, and n is an integer between 0 and 4.

Abstract: The present invention provides novel 3-heterocyclic benzylamides and related derivatives having the general Formula I 1

Abstract: A compound of formula (I) wherein A and B are optionally substituted cyclohexenyl or phenyl groups, X is carbonyl or sulfonyl, and Y is 5-7 atoms-linker, is useful as histone deacetylase inhibitors, particularly for inhibiting cell proliferation.

Abstract: The invention relates to novel, substituted, fused indole and heteroindole derivatives of the general formula I 1

Abstract: Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.

Abstract: The present invention relates to novel substituted imidazoles, to the use of these compounds as medicaments, to pharmaceutical compositions comprising the compounds, and to a method of treatment employing these compounds and compositions. The present compounds show a high and selective binding affinity to the histamine H3 receptor indicating a histamine H3 receptor antagonistic or agonistic activity. As a result, the compounds are useful for the treatment of disorders related to the histamine H3 receptor. More particularly, the present compounds possess a histamine H3 receptor agonistic activity and are accordingly useful in the treatment of disorders in which a histamine H3 receptor activation is beneficial.

Abstract: &agr;, &bgr;-Unsaturated sulfones of the following formulae are provided, which are useful as antiproliferative agents, including, for example, anticancer agents:

Abstract: The invention provides compounds of the formula I 1

Abstract: The invention is drawn to transition metal catalysts for the practical synthesis of important chiral molecules. The transition metal catalysts comprise chiral ligands based on chiral amine oxazolinyl ligands. The invention includes methods of making the catalysts, and methods of performing reactions using the catalysts.

Abstract: A method for producing camphorsultam, which includes the following steps 1 to 4: Step 1: reacting camphorsulfonic acid with a halogenation agent to give camphorsulfonyl halide, Step 2: reacting the camphorsulfonyl halide with ammonia to give camphorsulfonamide, Step 3: subjecting the camphorsulfonamide to dehydration and ring closure to give camphorsulfonimine, and Step 4: reducing the camphorsulfonimine with sodium borohydride in an aqueous isopropanol solution. According to this invention, camphorsultam and intermediates thereof can be obtained by an industrial method which is comparatively safe to the environment and human body, economical, and which is simple and easy.

Abstract: Novel intermediates, i.e., N-(2S-(2-propenyl)octanoyl)-(1S)-(−)-2,10-camphorsultam, N-(2S-(2-propynyl)octanoyl)-(1S)-(−)-2,10-camphorsultam and N-(2R-(2-propyl)octanoyl)-(1S)-(−)-2,10-camphorsultam; processes for the preparation of the intermediates; and processes for the preparation of optically active 2S-(2-propenyl)octanoic acid, 2S-(2-propynyl)octanoic acid and 2R-propyloctanoic acid by using the same. Optically active 2R-propyloctanoic acid equivalent or superior to that prepared by the process of the prior art in optical purity can be efficiently prepared in shorter reaction steps.

Abstract: Novel oxazolidinone compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. 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 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 can be achieved.

Abstract: Compounds of formula (I) are useful in treating diseases or conditions prevented by or ameliorated with histamine-3 receptor ligands.

Abstract: The present invention relates to carbapenem antibacterial agents of formula I: or a pharmaceutically acceptable salt thereof, wherein: R2 represents: in formula I, in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a CH2 group. The naphthosultam is further substituted with various substituent groups including at least one cationic group.

Abstract: The present invention provides novel compounds of Formula 1, compositions containing these compounds, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTP&agr;, LAR and HePTP or the like, wherein A, R1, R2, R3, R4, R16 and R17 are as defined in the specification.

Abstract: This invention provides for a method of treating a chemokine mediated disease, wherein the chemokine is one which binds to an IL-8 &agr; or &bgr; receptor and which method comprises administering an effective amount of a compound of Formular (I) or a pharmaceuticlly acceptable salt thereof. In particular the chemokine is IL-8.

Abstract: The present invention is concerned with compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen, hydroxy, C.sub.1-6 alkyl or aryl; R.sup.2 is hydrogen; optionally substituted C.sub.1-12 alkyl; C.sub.3-7 cycloalkyl; C.sub.2-8 alkenyl, optionally substituted pyrrolidinyl or aryl; R.sup.3 is hydrogen, optionally substituted C.sub.1-6 alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; ##STR2## is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.

Abstract: The present invention provides a process for the production of 1,8-naphthosultam comprising reacting 1-naphthylamine-8-sulfonic acid with excess POCl.sub.3 or PCl.sub.3 in the presence, as a proton acceptor, of a mono-, di-, or preferably tri-C.sub.1 -C.sub.4 alkylamine, and in the presence, as a reaction solvent, of mono-, di-, or tri-C.sub.1 -C.sub.4 alkylbenzene.

Abstract: Methods of synthesizing compounds of the Formula V: ##STR1## wherein X.sub.c is a chiral auxiliary, m is from 1 to 4, and R.sub.8 is hydrogen or --OH, are provided.Additionally, methods of synthesizing compounds of the Formula XII: ##STR2## wherein m is from 1-4; B is hydrogen or a blocking group; and R.sub.13 is a leaving group or a compound of formula R.sub.14 --N--R.sub.15 ;wherein R.sub.14 is hydrogen or branched or straight-chain C1-C6 alkyl; and R.sub.15 is hydrogen, C3-C8 cycloalkyl, or branched or straight-chain alkyl;are also provided. Novel compounds useful in the synthesis of cyclopentenes and carbocyclic nucleosides are further provided.

Abstract: The benzisothiazolyl-substituted aminomethylchromans are prepared either by substituting the corresponding unsubstituted aminomethylchromans on the amine nitrogen or reacting the corresponding benzisothiazolylalkylamines with appropriate activated methylchromans or reacting the amine nitrogen of aminomethylchroman first with an appropriately substituted alkine and then hydrogenating. The benzisothiazolyl-substituted aminomethylchromans can be used as active compounds in medicaments, in particular in medicaments for the treatment of disorders of the central nervous system.

Abstract: A process for synthesizing a compound of formula I: is disclosed wherein R represents halo or C.sub.1-6 alkyl, unsubstituted or substituted with OP, wherein P represents a protecting group.

Abstract: The present invention is directed to compounds which inhibit famesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting famesyl-protein transferase and the famesyl of the oncogene protein Ras.

Abstract: The present invention relates to new 2-Phenyl-1-?4-(amino-1-yl-alk-1-ynyl)benzyl!-1H-indol-5-ol compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structure below.

Abstract: Novel 5-alkoxy tryptamine derivatives are provided, corresponding to the general formula: ##STR1## in which R may be alkaline, X may be amino, and Y is various N-heterocyclic or N-branched chain moieties. The compounds show selective binding to 5-HT.sub.1D receptor subtypes, and have potential pharmaceutical utility in manufacture of migraine-treating drugs.

Abstract: Compounds of the formula I ##STR1## where the substituents have the meanings given in the description, and their preparation are described. The novel compounds are suitable for the control of diseases.

Abstract: An enantioselective multi-stage process is described which uses as a starting material an .alpha.,.beta.-unsaturated olefin of formula (1):Ar--CH.dbd.C(R.sup.4)COAux (1)where Ar and R.sup.4, which may be the same or different, is each a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; and Aux is the residue of a chiral (R- or S-) auxiliary.In the process, the olefin is converted to a chiral triarylethane which is of use in medicine.

Abstract: For binding 5-HT.sub.1 receptors and thereby treating central nervous system disorders, novel substituted aminomethyltetralins and their heterocyclic analogues of the formula ##STR1## in which Z--denotes a group of the formula ##STR2## R.sup.1, E and F can be hydrogen or other radicals, or salts thereof.

Abstract: A process for enantioselectively alkylating, at the asterisked carbon atom, a single enantiomer of a glycine derivative having the general formula ZCOCH(R)NY wherein Z is a moiety derived from a chiral sultam, R is hydrogen or C.sub.1 to C.sub.10 alkyl and Y is one or more groups rendering the nitrogen atom unreactive towards alkylating agents comprises:(i) reacting the glycine derivative with an enolising agent to produce the corresponding enolate of the glycine derivative, and(ii) thereafter reacting the enolate of the glycine derivative with an alkylating agent of formula R.sup.1 X to generate a single enantiomer of a product of formula ZCOC(R)(R.sup.1)NY where R.sup.1 is selected from C.sub.1 to C.sub.10 alkyl, C.sub.1 to C.sub.20 aralkyl, C.sub.2 to C.sub.10 alkenyl or substituted derivatives thereof and X is Cl, Br or I. The product of the process can be treated with first acid and then base to generate the enantiomerically pure alpha-amino acid of formula HO.sub.2 CC(R)(R.sup.1)NH.sub.

Abstract: There is disclosed a method for the treatment of immunoinflammatory conditions, such as allergy, anaphylaxis, asthma, psoriasis, inflammatory bowel disease and inflammation in mammals which comprises administering to a mammal so afflicted an effective amount of a compound having the formula: ##STR1## wherein Z is a group having the formula ##STR2## R.sup.1 and R.sup.2 are each, independently, hydrogen or lower alkyl; R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl of 1-20 carbon atoms, halo, halo lower alkyl, halo lower alkoxy, lower alkoxy, halo lower alkylsulfonyl, nitro or trifluoromethyl, where at least one of R.sup.3 and R.sup.4 is other than hydrogen;R.sup.5 is hydrogen, lower alkyl or halo;A is --CH.sub.2 --, --O-- or --S--;m is 0-10;n is 1-8;X is hydrogen, fluoro, lower alkyl or aralkyl of 7-12 carbon atoms;or a pharmacologically acceptable salt thereof.

Abstract: New pyrrolidone compounds of the formula: ##STR1## in which: R is OR", SR" or N (R.sub.3 R.sub.4)R' is optionally substituted alkyl or aryl, andthe carbon in the 5-position of the pyrrolidone ring, which is substituted by CH.sub.2 R has the R or S configuration.These new compounds and their physiologically tolerable salts may be used therapeutically especially in the treatment of asthenias, ischaemic syndromes and nervous disorders associated with normal or pathological ageing.

Abstract: Novel compounds having an affinity for 5-hydroxytryptamine receptors of the formula ##STR1## in which R.sup.1 stands for H, alkyl, aralkyl or heteroarylalkyl,X stands for H, OCH.sub.3, OH, SCH.sub.3, halogen, CN or CONH.sub.2,Y stands for a straight-chain or branched, saturated or unsaturated alkylene chain having up to 6 carbon atomsandZ stands for a group of the formula ##STR2## --OR.sup.4, --SO.sub.m R.sup.5, --COOR.sup.6 or CONR.sup.7 R.sup.8 or salts thereof.

Abstract: This invention relates to a compound ##STR1## in which R.sub.1 representsa 1,2,3,6-tetrahydro-1-pyridyl radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by a halogen atom or an alkyl, hydroxy or alkoxy radical, (c) a 3-indolyl radical, (d) a 3-indolyl radical substituted on the nitrogen atom by an alkyl or alkylcarbonyl radical and/or in the 5-position by a halogen atom or (e) a 3-(5-hydroxyindolyl) radical.a 1-piperazinyl radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by an alkoxy, alkyl, hydroxy, nitro or amino radical or a halogen atom, (c) a 1,2-benzisothiazol-3-yl radical, (d) a 1,2-benzisoxazol-3-yl radical or (e) a 2-pyridyl radical.

Abstract: Compounds of formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are H, alkyl or aryl, m and n are 0 or 1, and A is a divalent organic radical which, with (CR.sup.1 R.sup.2).sub.m NF--SO.sub.2 (CR.sup.3 R.sup.4).sub.n groups, forms a 5- to 8-membered ring, are admirably suitable fluorinating agents for fluorinating carbon atoms, especially as stereospecific fluorinating agents, when the compounds contain a chiral carbon atom and are in optically active form. The compounds of formula I are prepared by reacting the corresponding silated sulfonamides, wherein the NF group is replaced by an N-SiR.sup.7 R.sup.8 R.sup.9 group and R.sup.7, R.sup.8 R.sup.9 are each independently C.sub.1 -C.sub.12 alkyl, cyclopentyl, cyclohexyl, benzyl or phenyl, with a fluorinating agent.

Abstract: The invention relates primarily to quaternized polycyclic compounds having the formula ##STR1## wherein m is an integer having a value of from 1 to 4; R is alkylene having from 3 to 8 carbon atoms and is optionally substituted with C.sub.1 to C.sub.4 alkyl; R.sub.2 together with the quaternary nitrogen, forms a 5 to 14 membered heterocyclic ring, said ring containing from 1 to 2 hetero atoms selected from the group of nitrogen, sulfur and oxygen; R.sub.1 forms a double bond in the heterocyclic ring of the quaternized nitrogen or is alkyl, alkyleneoxyalkyl, alkylhydroxy, aryl, aralkyl, aralkenyl, alkaryl, alkylamidoalkyl and X.sup.- is a chloride, bromide or iodide anion. The invention also relates to the preparation and use of said quaternized polycyclic compounds.

Abstract: In one aspect, this invention relates to a method of synthesizing certain 3-(4'-OH-carbocyclic aryl)-3-(carbocyclic aryl)-2,3-dihydrobenz[d]isothiazole-1,1-dioxides (and -2,3-dihydronaphtho[1,8-de]-1,2-thiazine-1,1-dioxides) by reacting a 3-(4'-OP-carbocyclic aryl)-3-(carbocyclic aryl)-2,3-dihydrobenz[d]isothiazole-1,1-dioxide (or a 3-(4'-OP-carbocyclic aryl)-3-(carbocyclic aryl)-2,3-dihydronaphtho[1,8-de]-1,2-thiazine-1,1-dioxide) wherein P is a protecting group with a carboxylic acid halide in pyridine to yield the corresponding 2-carbonyl derivative followed by removing the protecting group with weak acid to give the product. Optionally, the acylation step may be carried out by sequentially reacting the starting compound with an alkali metal hydride to give the corresponding 2-alkali metal salt and then reacting with the carboxylic acid halide in a suitable inert organic solvent.

Abstract: Antihistamines of the formula ##STR1## wherein ##STR2## is a 5 or 6 membered ring which is phenyl or heterocyclic; ##STR3## is a six membered ring which is 2,3 or 4 pyridyl or is phenyl or substituted phenyl, with the proviso that is ##STR4## is a nitrogen containing ring, ##STR5## must be phenyl; Z is an alkylene chain having 0 to 2 carbon atoms in the chain, said 2 carbon chain optionally having one double bond, said chain optionally having either a carbonyl oxygen, or a hydroxy group as a substituent; W is ##STR6## wherein p is 1 or 2 and n is 1 or 2, R.sup.1 is C.sub.1 to C.sub.6 alkyl, R.sup.2 is hydrogen or C.sub.1 to C.sub.6 alkyl, and the dotted line represents an optical double bond, R.sup.2 being absent if the double bond is present, and Y is substituted carboxylate or substituted sulfonyl. Said antihistamines have little or no sedative effects.

Abstract: This invention relates to certain 3,3,-di(4'-OP-carbocyclic aryl)-2,3-dihydrobenz[d]isothiazole-1,1-dioxides (and-2,3-dihydronaphtho[1,8-de]-1,2-thiazine-1,1-dioxides) and to the preparation thereof by reacting (a) at least 2 equivalents of (i) a 4'-OP-carbocyclic aryllithium compound wherein P is a protecting group compatible with organometallic reagents or (ii) a 4'-OP-carbocyclic arylMgE compound wherein P is a protecting group compatible with organometallic reagents and E is chloro, bromo or iodo and (b) 1 equivalent of a compound selected from a 3-chlorobenz[d]isothiazole-1,1-dioxide and a 3-chloronaphtho[1,8-de]-1,2-thiazine-1,1-dioxide to give the corresponding 3,3-di(4'-OP-carbocyclic aryl)-2,3-dihydrobenz[d]isothiazole-1,1-dioxide or the corresponding 3,3-di(4'-OP-carbocyclic aryl)-2,3-dihydronaphtho[1,8-de]-1,2-thiazine-1,1-dioxide, which compounds are useful in the synthesis of phenol and 1-naphthol sulfam(na)-phthaleins employed, for example, as photographic optical filter agents and filter agent