Abstract: The invention as disclosed herein is a method and composition for the treatment of HIV in humans and other host animals, that includes the administration of an effective HIV treatment amount of a phenylindole as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier. The compounds of this invention either possess antiviral (i.e., anti-HIV) activity, or are metabolized to a compound that exhibits such activity.

Abstract: The present invention is concerned with the acylation of indoles, specifically the preparation of 3-acylated indoles which may be further treated to provide indoles having an alternative substituent at the 3-position.

Abstract: This invention relates to inhibitors of glycogen synthase kinase-3&bgr;, methods of treating diseases characterized by an excess of Th2 cytokines, and to 3-indolyl-4-phenyl-1H-pyrrole-2,5-dione derivatives of Formula (I): 1

Abstract: A compound selected from those of formula (I): wherein: R1 and R2 each independently represent hydrogen or, alkyl, T1 and T2 each independently represent alkylene, G represents a heterocyclic group selected of formula (&agr;):  wherein: W1 to W5 and X1 to X4 are so defined in the description. Medicinal products containing the same are useful as serotonin-reuptake inhibitors.

Abstract: This invention is directed to isoindolyl and isoquinolinyl aroyl pyrrole compounds pharmaceutically useful as agents or modulators for the treatment of central nervous system disorders and methods for the treatment of central nervous system disorders.

Abstract: The invention is directed to physiologically active compounds of general formula (I):

Abstract: Described are compounds having formula I or II: 1

Abstract: The invention provides 2, 3-, 4- or 5-substituted-N1-(arylsulfonyl)indole and (heteroaryl)indole compounds of the general formula (I): 1

Abstract: This invention provides tissue selective estrogens of formula I having the structure 1

Abstract: There are provided novel compounds of formula (I) 1

Abstract: The invention relates to new hydroxyindoles of the Formula, 1

Abstract: A compound of the formula 1

Abstract: The invention relates to new hydroxyindoles of the Formula, 1

Abstract: Heterocyclically substituted benzamides of the formula I are described, where R1, R2, R3, R4, R5, X, m and n have the meanings given in the description. The novel compounds are useful for controlling diseases.

Abstract: The invention relates to nets hydroxyindoles of the Formula, 1

Abstract: We have discovered a method of modifying the tumor cell microenvironment to reduce or prevent the establishment, growth or metastasis of malignant cells comprising administering to a patient having malignant cells a pharmaceutically effective amount of a PAR-1 inhibitor and optionally a PAR-2 inhibitor to prevent or reduce activation of normal cells within the tumor microenvironment. This method also has the effect in some patients of modulating the immune system to facilitate a more efficient immune response to malignant cells and maybe coupled with cytokine therapy and T-cell therapy to enhance the patient's immune response to the malignant cells.

Abstract: A process and a kit are provided for detecting differences in two or more samples of protein, including proteins bearing post-translational modifications and peptides. Proteins are prepared, for example, from each of a different group of cell samples or body fluid samples to be compared. Each protein extract is labeled with a different one of a luminescent dye from a matched set of dyes. The matched dyes have generally the same ionic and pH characteristics but emit light at different wavelengths to exhibit a different color upon luminescence detection. The labeled protein extracts are mixed together and separated together by electrophoresis or a chromatographic method. The separation is observed to detect proteins unique to one sample or present in a greater ratio in one sample than in the other. Those unique or excess proteins will fluoresce the color of one of the dyes used. Proteins common to each sample migrate together and fluoresce the same.

Abstract: A compound of formula (I): 1

Abstract: Isoindolin-1-one-substituted propionamide glucokinase activators which increase insulin secretion in the treatment of type II diabetes.

Abstract: A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide from a chiral alpha amino aldehyde.

Abstract: The present invention is directed to compounds useful in the treatment of migraine which have the general formula (II).

Abstract: A method for producing an amide derivative of the formula [XV] 1

Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.

Abstract: The invention relates to a compound having formula (I) wherein A is an optionally unsaturated 5- or 6-membered ring, which may comprise a heteroatom selected from N, O and S and which may be substituted with oxo or (1-6C)alkyl; R1, R2 and R3 are independently H, (1-6C)alkyl, (1-6C)alkoxy, (1-6C)alkoxy-(1-6C)alkyl, carbo(1-6C)alkoxy or halogen; X is O or S; and n is 1 or 2; or a pharmaceutically acceptable salt thereof, with the exception of 3-(naphth-1-yl-oxy)-pyrrolidin and 3-(5,6,7,8-tetrahydro-napth-1-yl-oxy)-pyrrolidin. The compounds of the invention have antidepressant activity and can be used in treating or preventing serotonin-related diseases.

Abstract: Arylsulphonamide-substituted benzimidazole derivatives of formula (I) having tryptase-inhibiting activity. Exemplary are: 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(2-diethylaminoethyl)-benzenesulphonylamino]-benzimidazole; 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(2-diethlylaminoethyl)-benzylsulfonylamino]-benzimidazole; and, 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(3-diethylaminopropyl)-benzenesulphonylamino]-benzimidazole.

Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.

Abstract: The invention concerns compounds of formula (1) wherein: R represents a chain (A) or (B); R1 is methyl or ethyl; R2 is either an optionally substituted aromatic or an optionally substituted heteroaromatic ring; R3 and R4, identical or different, are either an optionally substituted aromatic or an optionally substituted heteroaromatic ring; R′ represents a hydrogen atom or a —CO—alk radical, their optical isomers, their salts, their preparation and medicines containing them.

Abstract: This invention provides compounds of the formula wherein R1, R2, R3, R4, R5, R6, R7, X, n and Y, are as defined in the specification, or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods utilizing the compounds for treating or preventing disease states or syndromes which are caused or associated with an estrogen deficiency or an excess of estrogen utilizing these compounds.

Abstract: The present invention is directed to Mannich base prodrugs of certain 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

Abstract: This invention relates to a series of substitituted amino acids of Formula I 1

Abstract: Novel processes and intermediates useful in the preparation of 11-oxa prostaglandin analogs are disclosed.

Abstract: This invention provides cyclic-bridged dyes, particularly cyclic-bridged cyanine dyes, of the general formula: In this formula, each dotted line represents carbon atoms necessary to form a fused substituted or unsubstituted aromatic ring; n=1-18; m=1-18, selected independently from n. X and Y are selected independently from the group consisting of S, O, N, CH2 and C(CH3)2; at least one of said R1 and R2 comprises a sulfonic acid or sulfonate group attached to the aromatic ring; and R3 and R4 are independently selected from the group consisting of carboxyl, activated carboxyl and methyl, wherein at least one of said R3 and R4 groups is carboxylate or activated carboxylate. Methods of making and using the cyclic-bridged dyes are also provided.

Abstract: This invention provides dye phosphoramidites, particularly phosphoramidites of cyanine and related dyes, of the general formula: In this formula, each dotted line represents carbon atoms necessary to form a fused substituted or unsubstituted aromatic ring; m is an integer from 1 to 18; Y and Z are independently selected from the group consisting of S, O, N, CH2 and C(CH3)2; R1 is an alkyl; (PAM) is a phosphoramidite group; X⊖ is a negative ion; and Q is or wherein n is 1, 2 or 3. Methods of making and using the dye phosphoramidites are also provided.

Abstract: Disclosed are triaryl cationic compounds that exhibit broad spectrum antibiotic and antifungal activity, pharmaceutical compositions containing the compounds, and methods of treating bacterial and fungal infections using the compounds. The compounds were initially isolated by screening a 25,000-member bacterial artificial chromosome (BAC) library of environmental (eDNA) from soil. At least one clone produced a dark brown melanin-like compound that was found to have antibiotic activity. The compounds were isolated and synthesized de novo. From within the positive clone, a single open reading frame that shares extensive sequence similarity with members of the 4-hydroxyphenylpyruvate family of enzymes was found to be necessary and sufficient to confer the production of at least one of the subject compounds on E. coli.

Abstract: A pharmaceutical composition containing a glycogen phosphorylase inhibitor of Formula I or IA as defined herein is administered to a mammal to treat infection.

Abstract: Compounds of formula (I), wherein A and A are independently the same or different group of formula (II) wherein: R′ is H, CH3, C(CH3)2,—ORa, —N(Ra)2, —N(Ra)ORa or -DP; R is H or CH3; Ra is H, C1-C3 alkyl; D is a bond, alkylene, —C(═O)—, —S(O)— or S(O)2—; P is an optionally substituted, mono or bicyclic carbo- or hetereocycle; R″ is H, any of the sidechains found in the natural amino acids, carboxacetamide, or a group (CH2)nDP; M is a bond or —C(═O)N(R′″)-; Q is absent, a bond, —CH(OH)— or CH2—; or R″ together with Q, M and R define an optionally substituted 5 or 6 membered carbo- or heterocyclic ring which is optionally fused with a further 5 or 6 membered carbo- or heterocyclic ring; with the proviso that R is —ORa, -, N(Ra)2, —N(Ra)ORa or -DP, if M is a bond and Q is absent; X is H, OH, OCH3, Y is H, OH, OCH3, but X and Y are not both H; Z′ and Z″ are independently —(

Abstract: Disclosed are compounds of the formula: 1

Abstract: The present invention relates to new 2-Phenyl-1-[(2-Aminoethoxy)-Benzyl]-Indole compounds which are usefuil as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utiig these compounds, which have the general structures below: 1

Abstract: Compound of formula (I): wherein: n represents 2 or 3, R1 represents optionally substituted alkyl, cycloalkyl or optionally substituted phenyl, R2 represents amino, optionally substituted amidino, optionally substituted guanidino or optionally substituted isothioureido, Ar represents aryl or heteroaryl, X1 represents hydroxy or optionally substituted amino, isomers thereof, and also salts thereof with a pharmaceutically acceptable acid or base, and which medicinal products containing the same/are useful as trypsin-related serine protease inhibitors.

Abstract: The invention concerns pharmaceutically useful indoles of formula (I), in which Z, X, T, A, R1, R2, p and q have any of the meanings defined herein, and their pharmaceutically acceptable salts or in vivo hydrolysable esters, as well as pharmaceutical compositions containing them. The novel compounds possess inhibitory activity against monocyte chemoattractant protein-1 (MCP-1). The invention further concerns the use of such indoles in the treatment of a disease or condition mediated by MCP-1.

Abstract: This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof wherein R1 is H or C1-4 alkyl; R2 is C(═L′)R3 or So2R4; Y is a direct bond or C1-4 alkylene; L and L′ are independently oxygen or sulfur; Q is selected from the following: C1-6 alkyl, halo-substituted C1-4 alkyl, optionally substituted C3-7 cycloalkyl, optionally substituted phenyl or naphthyl, optionally substituted 5 or 6-membered monocyclic aromatic group; R3 is —OR6, —NR7R8, N(OR1)R7 or a group of formula: Z is a direct bond, O, S or NR5; R4 is C1-6 alkyl, halo-substituted C1-4 alkyl, optionally substituted phenyl or naphthyl; R5 is C1-4 alkyl or halo-substituted C1-4 alkyl; R6 is C1-4 alkyl C3-7 cycloalkyl, C1-4 alkyl-C3-7 cycloalkyl, halo-substituted C1-4 alkyl, optionally substituted C1-4 alkyl-phenyl or phenyl; R7 and R8 are each selected from the following: H, optionally substituted C1-6 alkyl, optionally substituted C3-7 cyclo

Abstract: The present invention provides novel thio-substitutedamido lactam derivatives of the formula useful in as inhibitors of matrix metallo-proteinases (MMPs).

Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.

Abstract: A compound which is a 6-substituted seco indoline of the formula (I): wherein: X is halogen or OSO2R where R represents H or C1-5 alkyl optionally substituted with from 1 to 4 hydroxyl, acid (COOH) or amino groups which amino may be optionally substituted by one or two C1-5 alkyl groups; Y is N02, N3, NHOH, NHR, NRR, N═NR, N(O)RR, SR or SSR, where R is defined as above, but that in the case where Y is SSR or N═NR, then R can also be another moiety of formula (I); or Y is a group of formula:

Abstract: Compositions comprising a naphtho [1,2-b]pyran of formula (I): wherein R7 and/or R9 is hydrogen or an amino group provided that R7 and R9 are not both hydrogen, and the other substituents are as defined in the specifcation.

Abstract: The present invention relates to new prolylendopeptidase inhibitors of general formula (I).

Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.

Abstract: Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.

Abstract: Disclosed are novel 4-alkenyl- and 4-alkynyl oxindoles having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, a, b, and X are as defined herein. These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer, more particularly, the treatment or control of breast and colon tumors. Also disclosed are pharmaceutical compositions containing the compounds of formula I and II as well as intermediates useful in the preparation of the compounds of formula I and II.

Abstract: Novel disubstituted bicyclic heterocycles, of which the following are exemplary:(a) 1-methyl-2-[(4-amidinophenyl)-oxymethyl]-5-[N-(hydroxycarbonylmethyl)-quin oline-8-sulphonylamino]-benzimidazole,(b) 1-methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(N-(hydroxycarbonylmethyl)-ami nocarbonylmethyl)-quinoline-8-sulphonylamino]-benzimidazole,(c) 1-methyl-2-[N-(4-amidinophenyl)-aminomethyl]-5-[N-(hydroxycarbonylmethyl)- quinoline-8-sulphonylamino]-benzimidazole and(d) 1-methyl-2-[N-(4-amidinophenyl)-aminomethyl]-5-[N-(hydroxycarbonylmethyl)- quinoline-8-sulphonylamino]-indole.These are useful for the treatment of thrombotic disease.