Abstract: The compounds disclosed herein are indolocarbazoles of Formula (I), which are potent CDK4 inhibitors, and are useful in the treatment of cell proliferative disorders, including cancer. Formula (I).

Abstract: An E-isomeric fulleropyrrolidine compound of formula (I): 1

Abstract: The invention relates to the use of novel indole compounds as direct dyes in compositions intended for dyeing keratin materials, and, for example, compositions intended for dyeing human keratin fibers and including the hair, and in cosmetic compositions intended for making up the skin, the nails and the lips, to the dye compositions or make-up compositions comprising them and to the direct dyeing process using them, and processes of manufacturing said novel indole compounds.

Abstract: The present invention relates to a novel glycosidation process to make intermediates useful in the preparation of indolopyrrolocarbazole derivatives which inhibit the growth of tumor cells and are therefore useful in the treatment of cancer in mammals, and the like.

Abstract: The present invention concerns novel sugar derivatives of indolocarbazoles and pharmaceutical formulations thereof which exhibit topoisomerase-I activity and are useful in inhibiting the proliferation of tumor cells.

Abstract: A compound of formula (I): wherein: R1 represents hydrogen, or linear or branched (C1-C6)alkyl optionally substituted by one or more identical or different groups selected from aryl, heteroaryl, cycloalkyl and heterocycloalkyl, represents a saturated ring having from 4 to 7 ring members that may contain, in addition to nitrogen, one or two hetero atoms selected from O, S and —NR3 groups, wherein R3 represents hydrogen or linear or branched (C1-C6)alkyl, n represents an integer such that 1≦n≦6, R2 represents any one of the groups described in the description, their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as inhibitor of trypsin-related serine proteases and thrombin.

Abstract: Charge transport compounds are described that have a multiple number of hydrazone-bridged heterocyclic groups (especially julolidine, carbazole and/or triarylmethane groups) connected by a central bridging group.

Abstract: The present invention concerns novel sugar derivatives of indolocarbazoles and pharmaceutical formulations thereof which exhibit topoisomerase-I activity and are useful in inhibiting the proliferation of tumor cells.

Abstract: The present invention is directed to novel fused pyrrolocarbazoles and isoindolones, including pharmaceutical compositions, diagnostic kits, assay standards or reagents containing the same, and methods of using the same as therapeutics. The invention is also directed to intermediates and processes for making these novel compounds.

Abstract: Cyanine dye bioconjugates useful for diagnostic imaging and therapy are disclosed. The conjugates include several cyanine dyes with a variety of bis- and tetrakis (carboxylic acid) homologes. The compounds may be conjugated to bioactive peptides, carbohydrates, hormones, drugs, or other bioactive agents. The small size of the compounds allows more favorable delivery to tumor cells as compared to larger molecular weight imaging agents. The various dyes are useful over the range of 350 to 1,300 nm, the exact range being dependent upon the particular dye. The use of dimethylsulfoxide helps to maintain the fluorescence of the compounds. The inventive compounds are useful for diagnostic imaging and therapy, in endoscopic applications for the detection of tumors and other abnormalities, for localized therapy, for photoacoustic tumor imaging, detection and therapy, and for sonofluorescence tumor imaging, detection and therapy.

Abstract: The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles.

Abstract: The present invention is directed to novel fused pyrrolocarbazoles and isoindolones, including pharmaceutical compositions, diagnostic kits, assay standards or reagents containing the same, and methods of using the same as therapeutics. The invention is also directed to intermediates and processes for making these novel compounds.

Abstract: The invention relates to the use of novel indole compounds as direct dyes in compositions intended for dyeing keratin materials, and, for example, compositions intended for dyeing human keratin fibers and including the hair, and in cosmetic compositions intended for making up the skin, the nails and the lips, to the dye compositions or make-up compositions comprising them and to the direct dyeing process using them, and processes of manufacturing said novel indole compounds.

Abstract: Compounds according to Formula I 1

Abstract: The present invention concerns novel sugar derivatives of indolocarbazoles and pharmaceutical formulations thereof which exhibit topoisomerase-1 activity and are useful in inhibiting the proliferation of tumor cells.

Abstract: Photoresist monomers which can be used to form photoresist polymers and photoresist compositions using the same which are suitable for photolithography processes employing a deep ultraviolet light source and copolymers thereof. Monomers are represented by following Formula 1: wherein, R1, is —OH or —R—OH; R represents substituted or unsubstituted linear or branched (C1-C10) alkylene, substituted or unsubstituted (C1-C10) alkylene comprising an ether linkage, substituted or unsubstituted (C1-C10) alkylene comprising an ester linkage, or substituted or unsubstituted (C1-C10) alkylene comprising an ketone moiety; and 1 is an integer of 1 or 2.

Abstract: The invention provides derivatives of 5-arylsulfonyl indole and 5-arylsulfonyl indoline compounds which may be in the form of pharmaceutical acceptable salts or compositions that are useful in treating central nervous system diseases such as anxiety and depression. The invention also includes intermediates and processes to make the compounds, isotopically-labeled forms of the compounds and the use of the isotopically labeled forms of the compounds to perform nuclear magnetic resonance imaging and positron emission tomography.

Abstract: An organic electrically conductive compound represented by general formula (1): 1

Abstract: An organic electrically conductive compound represented by general formula (1): 1

Abstract: An E-isomeric fulleropyrrolidine compound of formula (I): 1

Abstract: An E-isomeric fulleropyrrolidine compound of formula (I): 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 the use of novel indole compounds as direct dyes in compositions intended for dyeing keratin materials, and, for example, compositions intended for dyeing human keratin fibers and including the hair, and in cosmetic compositions intended for making up the skin, the nails and the lips, to the dye compositions or make-up compositions comprising them and to the direct dyeing process using them, and processes of manufacturing said novel indole compounds.

Abstract: The present invention concerns novel sugar derivatives of indolocarbazoles and pharmaceutical formulations thereof which exhibit topoisomerase-I activity and are useful in inhibiting the proliferation of tumor cells.

Abstract: The invention relates to novel indole compounds, to their use as direct dyes in compositions intended for dyeing keratin materials and for example compositions intended for dyeing human keratin fibers and including the hair, and in cosmetic compositions intended for making up the skin, the nails and the lips, to the dye compositions or make-up compositions comprising them and to the direct dyeing process using them, and processes of manufacturing said novel indole compounds.

Abstract: The invention relates to methods and products for analyzing polymers. The polymers are analyzed by reconstructing sequence information from population data sets. The data sets include information about polymer dependent impulses arising from the polymers. The invention is also a method for linearly analyzing polymers by assessing the intensity of a signal arising from the polymer. The signal is generated as units and/or units specific markers pass a fixed station. The quantitative intensity of the signal is proportional to the number of units and/or unit specific markers giving rise to the signal.

Abstract: The present invention is directed to novel fused pyrrolocarbazoles and isoindolones, including pharmaceutical compositions, diagnostic kits, assay standards or reagents containing the same, and methods of using the same as therapeutics. The invention is also directed to intermediates and processes for making these novel compounds.

Abstract: The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles.

Abstract: Dibenzazole compounds having the general structure: ##STR1## wherein; R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 are independently H or a substituent which aids in solubility of the compound or which provides a linker arm for linking the compound to another moiety; Y is H or a cleavable moiety; X is a hydrogen, halogen, CF.sub.3, or SO.sub.3 H; V and W are oxygen or sulfur; Z is --C.dbd.C--, --C.tbd.C-- or an aromatic ring moiety; and n is 0, 1, or 2. When n=0 at least one of R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 is a substituent which aids in solubility of the compound or which provides a linker arm for linking the compound to another moiety or X is a halogen, CF.sub.3 or SO.sub.3 H. These compounds are highly fluorescent and can be easily detected using a fluorometer. Derivatives in which the Y group is a substituent other than H contain a fluorescence inhibiting chemical moiety that upon removal restores the fluorescence of the compound.

Abstract: This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.

Abstract: Dibenzorhodamine compounds having the structure ##STR1## are disclosed, including nitogen- and aryl-substituted forms thereof. In addition, intermediates useful for synthesizing such compounds are disclosed, such intermediates having the structure ##STR2## In Formula I, R.sub.1 is H or ##STR3## wherein Y is H, lower alkyl, lower alkene, lower alkyne, aromatic, phenyl, polycyclic aromatic, heterocycle, water-solubilizing group, or linking group, including substituted forms thereof. When R.sub.1 is H, the C-12-bonded nitrogen and the C-12 and C-13 carbons form a first ring structure having from 4 to 7 members, and/or the C-12-bonded nitrogen and the C-11 and C-12 carbons form a second ring structure having from 5 to 7 members. The compounds of Formula I further include aryl- and nitrogen-substituted forms thereof.

Abstract: Fluorescent conjugates suitable for use in flow cytometry and other biological applications. The fluorescent conjugates comprise an antibody having a polymeric dye bound thereto. The polymeric dye is preferably enhanced by a hydrophobic and conformationally restrictive moiety either bound thereto or in close association therewith. The hydrophobic and conformationally restrictive moiety is preferably derived from a cyclodextrin. The polymeric dye comprises a polymeric entity having signal-generating groups, such as aminostyryl pyridinium dye residues attached thereto. The fluorescent conjugates exhibit exceptional stability characteristics and avoid many of the problems of energy transfer, bio-conjugability, and solubility.

Abstract: A chemical compound of the following formula: ##STR1## wherein R.sup.1 is selected from the group consisting of alkyl, aralkyl, and substituted alkyl groups; R.sup.3 is selected from the group consisting of H, PO.sub.3.sup.-2, P.sub.2 O.sub.6.sup.-3 ; P.sub.3 O.sub.9.sup.-4, and .alpha.-thio phoshates (PSO.sub.2.sup.-2 ; P.sub.2 SO.sub.5.sup.-3 ; P.sub.3 O.sub.8.sup.-4); and .alpha.BH.sub.3.sup.- phosphates (P(BH.sub.3)O.sub.2.sup.-2, P.sub.2 (BH.sub.3)O.sub.5.sup.-3, P.sub.3 (BH.sub.3)O.sub.8.sup.-4); R.sup.4 is selected from the group consisting of H, lower alkyl, acyl, (CH.sub.2).sub.p COO(CH.sub.2).sub.q CH.sub.3 wherein p is an integer from 0 to 4 and q is an integer from 0 to 4, and 5,6; 6,7; or 7,8-butadienyl; R.sup.5 is selected from the group consisting of H lower alkyl, acyl, (CH.sub.2).sub.p COO(CH.sub.2).sub.q CH.sub.

Abstract: An organic electroluminescent (EL) device with a charge transport component of an indolocarbazole compound represented by Formulas (I) or (II) ##STR1## wherein R and R' are independently selected from the group consisting of hydrogen, alkyl, alkoxyl, aryl, and halogen; m and n are numbers from 0 to 4; A.sup.1 and A.sup.2 are arylene; Ar.sup.1, Ar.sup.2, Ar.sup.3, and Ar.sup.4 are aryl; R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen, alkyl, alkoxyl, aryl, and halogen; and p is a number from 1 to 3.

Abstract: The invention relates to a process and intermediates for the preparation of enantiomerically pure cycloalkanoindolecarboxylic acids and azaindolecarboxylic acids and pyrimido?1,2a!indolecarboxylic acids and their activated derivatives, characterized in that the tolyl acetic acid is first esterified with a chiral alcohol, then diastereoselective substitution at .alpha.-carbon atoms is carried out and this product is halogenated in the tolyl group and then reacted with appropriate cycloalkanoindoles, cycloalkanoazaindoles or pyrimido?1,2a!indoles. It is possible by this method to prepare specifically, in high purity, the enantiomerically pure carboxylic acids which are intermediates for valuable medicaments.

Abstract: An organic electroluminescent device member comprised of a charge transport component of an indolocarbazole represented by Formulas (I), (II), (III), (IV), (V), or (VI); or optionally mixtures thereof ##STR1## wherein R and R' are independently selected from the group consisting of a hydrogen atom, halogen atom, alkyl, alkoxyl, and aryl; m and n are numbers of 0 to 4; R.sup.1 and R.sup.2 are independently selected from the group consisting of alkyl, aryl, and vinyl; R.sup.3 and R.sup.4 are independently selected from the group consisting of a hydrogen atom, halogen atom, alkyl, alkoxy, and aryl, and p is a number from 1 to 3.

Abstract: Dibenzorhodamine compounds having the structure ##STR1## are disclosed, including nitogen- and aryl-substituted forms thereof. In addition, two intermediates useful for synthesizing such compounds are disclosed, a first intermediate having the structure ##STR2## including nitrogen- and aryl-substituted forms thereof, and a second intermediate having the structure ##STR3## including nitrogen- and aryl-substituted forms thereof, wherein substituents at positions C-14 to C18 taken separately are selected from the group consisting of hydrogen, chlorine, fluorine, lower alkyl, carboxylic acid, sulfonic acid, --CH.sub.2 OH, alkoxy, phenoxy, linking group, and substituted forms thereof. The invention further includes energy transfer dyes comprising the dibenzorhodamine compounds, nucleosides labeled with the dibenzorhodamine compounds, and nucleic acid analysis methods employing the dibenzorhodamine compounds.

Abstract: Novel sulfur, oxygen and nitrogen-containing heterocyclic monomers are provided which may be used to produce conductive graft copolymers.

Abstract: A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The effect has particular application in a wide variety of treatments including hypoxia, hypothermia, ischemia, stroke, ARDS, COPD, surgical blood loss, acute nonvolemic hemodilutions, wounds, diabetic ulcers, chronic leg ulcers, pressure sores, tissue transplants, and sepsis. The compounds are capable of acting on hemoglobin in whole blood.

Abstract: The present invention is concerned with the use of indolocarbazole imides of the general formula (I): ##STR1## for the preparation of pharmaceutical compositions for the treatment and/or prevention of cancer, virus diseases (for example HIV infections), heart and blood vessel diseases (for example high blood pressure, thromboses, heart rhythm disturbances and atheroscleroses), bronchopulmonary diseases, degenerative diseases of the central nervous system (for example Alzheimer's disease), inflammatory diseases (for example rheumatism and arthritis), diseases of the immune system (for example allergies), as well as psoriasis and for use as immune suppressives; as well as new compounds of general formula (I).

Abstract: Fluorescent dyes which are free of aggregation and serum binding are provided. These dyes are suitable for applications such as fluorescence immunoassays, in vivo imaging and in vivo tumor therapy. Fluorescence immunoassays methods are provided which use fluorescent dyes which are free of aggregation and serum binding. Such immunoassay methods are thus, particularly useful for the assay of biological fluids, such as serum, plasma, whole blood and urine. The present invention is directed to compositions comprising an oligonucleotide linked to a detectably labeled marker component comprising a fluorophore moiety which comprises a substantially planar, multidentate macrocyclic ligand coordinated to a central atom capable of coordinating with two axial ligands and two polyoxyhydrocarbyl moieties which are attached as axial ligands to the central atom. The present invention is also directed to nucleic acid hybridization and amplification methods employing such compositions.

Abstract: We have found that indoles of structural formula (III): ##STR1## can be cost-effectively synthesized in high yield by the palladium-catalyzed coupling/ring closure of a 2-halo- or 2-trifluoromethylsulfonyl-aniline and a cyclic ketone derivative. The process of the present invention is particularly useful to form indoles containing acid-labile substituents such as triazole, acetyl, ketal, cyano, and carbamate, or indoles having a good leaving group in the benzyl position. The advantages of the present process are that it does not require the use of triphenyl phosphine or tetrabutyl ammonium chloride or lithium chloride.

Abstract: A chemical compound of the following formula is disclosed: ##STR1## where R is selected from the group consisting of H, trityl, 4-O-monomethoxytrityl, 4,4'-O-dimethoxytrityl, and acyl groups, and whereby R can be used as a protecting group or is an H;R' is a phosphoramidite;R" is selected from the group consisting of H and lower alkyl groups;R'" is selected from the group consisting of H and lower alkyl groups;R.sup.4 is selected from the group consisting of H, lower alkyl, acyl, ##STR2## and (CH.sub.2).sub.p COO(CH.sub.2).sub.q CH.sub.3 wherein p is an integer from 0 to 4 and q is an integer from 0 to 4;R.sup.5 is selected from the group consisting of H, lower alkyl, acyl, ##STR3## and (CH.sub.2).sub.p COO(CH.sub.2).sub.q CH.sub.3 wherein p is an integer from 0 to 4 and q is an integer from 0 to 4;n is an integer from 0 to 10;m is an integer from 0 to 10;r is 1, 2, or 3; andX.sup.- is a negative ion.

Abstract: Disclosed are biologically active, non-indole-containing compounds referred to as fused isoindolones, which are represented by the following general formula: ##STR1## The fused indolones can be obtained by complete chemical synthesis. Methods for making and using the fused isoindolones are disclosed.

Abstract: Disclosed in this patent document are synthetic, biologically active molecules referred to as fused pyrrolo?2,3-c!carbazole-6-ones. These molecules are represented by the following general formulae: ##STR1## Methods for making and using the fused pyrrolo?2,3-c!carbazole-6-ones are also disclosed.

Abstract: Compounds of formula (Ia), (Ib), or (Ic), wherein A represents a group having two fused rings, or a group of formula (Id), R.sup.1.sub.(m) represents up to 6 substituents, K represents --O--, --S--, --CH.sub.2 --, --N(R.sup.2)-- or --N(COR.sup.2)--, in which R.sup.2 is H or C.sub.1 to C.sub.3 alkyl, W is a carbonyl, sulfonyl or sulfinyl group, provided that at least one of W and X contains carbonyl, Y and Z are as given in the description, and their pharmaceutically acceptable salts are ligands at CCK and/or gastrin receptors.

Abstract: The instant invention is a compound of formulaA--X--Y--E.sub.n --R.sup.5in which A is a bis-indolylmaleinimide or indolopyrrolocarbazole useful in the treatment and/or prevention of cancer, viral diseases, thrombosis, heart rhythm disturbances, atherosclerosis, bronchopulmonary diseases, degenerative diseases of the central nervous system, inflammatory diseases, diseases of the immune system, psoriasis, and immune suppression. A pharmaceutical composition and methods of preparing the compounds are also included.

Abstract: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.

Abstract: A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The effect has particular application in radiation oncology applications. The compounds are capable of acting on hemoglobin in whole blood.

Abstract: There is disclosed a novel compound having the formula ##STR1## which exhibits antifungal activity.