Abstract: Cytotoxic dimers comprising CBI-based and/or CPI-based sub-units, antibody drug conjugates comprising such dimers, and to methods for using the same to treat cancer and other conditions.

Abstract: The present invention relates to peptides having one or more stable, internally-constrained HBS ?-helices, where the peptide is capable of interacting with Ras and related proteins.

Abstract: A novel Fmoc protected duocarmycin subunit and utilization as a reagent in solid phase protein synthesis methodology. Also provided is a novel method of solid phase peptide synthesis, and in particular a method for the production of novel intermediates and novel monomeric and extended duocarmycin analogues having amino acid substituents.

Abstract: The present invention provides an imide compound represented by the following general formula (1). The imide compound of the present invention, particularly when used as a thickening agent for grease, is excellent in durability at high temperatures. [wherein X represents a tetravalent residue obtained by removing four carboxylic groups from an aromatic tetracarboxylic acid, Y represents a divalent residue obtained by removing two amino groups from an aliphatic diamine or an aromatic diamine, and R represents a residue obtained by removing an amino group from an aliphatic monoamine, an alicyclic monoamine, or an aromatic monoamine.

Abstract: The invention relates generally to activatable antibodies that include a masking moiety (MM), a cleavable moiety (CM), and an antibody (AB) that specifically binds to epidermal growth factor receptor (EGFR), and to methods of making and using these anti-EGFR activatable antibodies in a variety of therapeutic, diagnostic and prophylactic indications.

Abstract: The invention provides compounds of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.

Abstract: Methods for the synthesis of an indole in provided. Methods comprise oxidizing a N-aryl imine in the presence of a palladium-based catalyst, an oxidant, and a solvent.

Abstract: The present invention relates to polymers comprising one or more (repeating) unit(s) of the formula (I), and compounds of formula (III), wherein Y, Y15, Y16 and Y17 are independently of each other a group of formula (A), (B) or (C) and their use as IR absorber, organic semiconductor in organic devices, especially in organic photovoltaics and photodiodes, or in a device containing a diode and/or an organic field effect transistor. The polymers and compounds according to the invention can have excellent solubility in organic solvents and excellent film-forming properties. In addition, high efficiency of energy conversion, excellent field-effect mobility, good on/off current ratios and/or excellent stability can be observed, when the polymers and compounds according to the invention are used in organic field effect transistors, organic photovoltaics and photodiodes.

Abstract: The present invention provides for an organic compound comprising electron deficient unit covalently linked to two or more electron rich units. The present invention also provides for a device comprising the organic compound, such as a light-emitting diode, thin-film transistor, chemical biosensor, non-emissive electrochromic, memory device, photovoltaic cells, or the like.

Abstract: The present invention provides an imide compound represented by the following general formula (1). The imide compound of the present invention, particularly when used as a thickening agent for grease, is excellent in durability at high temperatures. [wherein X represents a tetravalent residue obtained by removing four carboxylic groups from an aromatic tetracarboxylic acid, Y represents a divalent residue obtained by removing two amino groups from an aliphatic diamine or an aromatic diamine, and R represents a residue obtained by removing an amino group from an aliphatic monoamine, an alicyclic monoamine, or an aromatic monoamine.

Abstract: The invention is based on the discovery that a remarkable improvement in the performance of maleimide thermosets can be achieved by incorporating amide-extended maleimides into an adhesive formulation. Amide-extended maleimides described herein can be used to toughen bismaleimide thermosetting materials without sacrificing any thermal stability. Amide-extended maleimides are readily prepared by reacting a bismaleimide with an appropriate amine via the well-known Michael addition reaction. Acylation of the resulting secondary amines provides the amide-extended maleimide. The acylating agent can also be used to introduce polymerizable functional groups into the backbones of these thermoset monomers. Amide-extended acrylate and methacrylate monomers can also be prepared.

Abstract: Disclosed is the synthesis of benzodipyrrolidone and their polymers and small molecules for electronic and optoelectronic applications. Also disclosed are devices that incorporate such polymers and small molecules.

Abstract: The invention is directed to maleimide thermosets incorporating imide-extended mono-, bis-, or polymaleimide compounds. These imide-extended maleimide compounds are prepared by the condensation of appropriate anhydrides with appropriate diamines to give amine terminated compounds. These compounds are then condensed with excess maleic anhydride to yield imide-extended maleimide compounds.

Abstract: The invention relates to novel polymers containg repeating units based on benzodifuran, benzodipyrrole or benzodithiophene, monomers and methods for their preparation, their use as semiconductors in organic electronic (OE) devices, especially in organic photovoltaic (OPV) devices, and to OE and OPV devices comprising these polymers.

Abstract: The present invention provides a blue or green phosphorescent organic electroluminescent device which has high luminous efficiency. An organic electroluminescent device includes a light-emitting layer containing a pyrroloindole compound represented by general formula (1) below. In general formula (1), X represents a substituted or unsubstituted arylene group, Ar1 and Ar2 each represent a substituted or unsubstituted aryl group, and R1 to R8 each represent a hydrogen atom or an alkyl group having 1 to 2 carbon atoms.

Abstract: A condensed-cyclic compound represented by Formula 1, and an organic light-emitting device including the condensed-cyclic compound. wherein R1 and R2, Ar1 through Ar4, L1 and L2, X1 and X2, and a and b are defined as in the specification.

Abstract: Polymers for photoresists and monomers for incorporation into those polymers are disclosed. The polymers comprise a photoacid generator (PAG) component and at least a second component that is photolytically stable and acid-stable. The polymers may also contain a third, acid-labile component. The photoacid generator is based on N-sulfoxyimides and related moieties that contain photolabile oxygen-heteroatom and oxygen-aromatic carbon bonds.

Abstract: Organic charge-transfer (CT) co-crystals in a mixed stack system are disclosed, wherein a donor molecule (D) and an acceptor molecule (A) occupy alternating positions (DADADA) along the CT axis. A platform is provided which amplifies the molecular recognition of donors and acceptors and produces co-crystals at ambient conditions, wherein the platform comprises (i) a molecular design of the first constituent (?-complement), (ii) a molecular design of the second compound (?-complement), and (iii) a solvent system that promotes co-crystallization.

Abstract: Dispersants for pigments as well as dispersions containing them, and compositions such as inks and coatings containing them are described. The dispersants are the reaction product of at least one dianhydride with at least two different reactants, each of which can be an amine, alcohol, or thiol, and at least one of which is polymeric.

Abstract: n-type organic semiconductors have a pyromellitic diimide structure and electronic or electro-optic devices include pyromellitic diimide compounds as organic semiconductors. Specific semiconductors include pyromellitic diimide compounds have sidechains comprising fluorine substituted aliphatic or aromatic moieties linked to the pyromellitic diimide structure by an alkylene or heteroalkylene linking group. An electronic or electro-optic device includes a first electrode, a second electrode space apart from the first electrode, and an organic semiconductor layer arranged between the first and second electrodes. The organic semiconductor layer comprises a pyromellitic diimide compound.

Abstract: Provided is a heterocyclic compound represented by Formula I: wherein Ar1 is a linking group and a C6-C16 arylene or heteroarylene group; Ar2 and Ar3 are each independently a C6-C20 aryl group, a C4-C20 heteroaryl group or a C6-C20 fused polycyclic group; Ar4 is a C6-C20 aryl group, a C6-C20 aryloxy group, a C4-C20 heteroaryl group or a C6-C20 fused polycyclic group; and Ar1 and Ar3, or Ar2 and Ar3 may be connected to each other to form a ring. The heterocyclic compound has high electrical stability and excellent charge transporting capability, and thus can be efficiently used as a material for forming at least one of a hole injecting layer, a hole transporting layer and an emitting layer suitable for fluorescent and phosphorescent devices realizing all colors including red, green, blue and white.

Abstract: The present invention relates to a novel polycyclic aromatic organic semiconductor compound having a polycyclic aromatic core, a method for preparing the same, and electronic, optical or electro-optical devices such as an organic semiconductor composition, organic semiconductor thin film, organic field effect transistor and solar cell containing the compound. The novel organic semiconductor compound according to the present invention has high crystallinity and control capability, and facilitates control of doping conditions in the manufacture of organic semiconductor element so that it can be used for diverse applications. The compound can be mass-produced at low cost and has high solubility in organic solvents so that a liquid phase process can be applied to the manufacture of semiconductor elements and the like, thus enabling the mass-production of semiconductor elements and solar cells at low cost.

Abstract: The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as other diagnostic and therapeutic moieties. The invention provides prodrugs and conjugates of the duocarmycin analogues with the linker arms of the invention.

Abstract: The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as other diagnostic and therapeutic moieties. The invention provides prodrugs and conjugates of the duocarmycin analogues with the linker arms of the invention.

Abstract: n-type organic semiconductors have a pyromellitic diimide structure and electronic or electro-optic devices include pyromellitic diimide compounds as organic semiconductors. Specific semiconductors include pyromellitic diimide compounds have sidechains comprising fluorine substituted aliphatic or aromatic moieties linked to the pyromellitic diimide structure by an alkylene or heteroalkylene linking group. An electronic or electro-optic device includes a first electrode, a second electrode space apart from the first electrode, and an organic semiconductor layer arranged between the first and second electrodes. The organic semiconductor layer comprises a pyromellitic diimide compound.

Abstract: Polymers for photoresists and monomers for incorporation into those polymers are disclosed. The polymers comprise a photoacid generator (PAG) component and at least a second component that is photolytically stable and acid-stable. The polymers may also contain a third, acid-labile component. The photoacid generator is based on N-sulfoxyimides and related moieties that contain photolabile oxygen-heteroatom and oxygen-aromatic carbon bonds.

Abstract: A heterocyclic compound represented by Formula 1 below: X is selected from the group consisting of nitrogen, boron, and phosphorous; and Ar1, Ar2, Ar3 and Ar4 are each independently selected from the group consisting of a C6-C30 substituted or unsubstituted aryl group, a C6-C30 substituted or unsubstituted aryloxy group, a C4-C20 substituted or unsubstituted heterocyclic group, and a C6-C20 fused polycyclic group. The heterocyclic compound can be included in emission layers of top emission and bottom emission organic light emitting devices.

Abstract: Disclosed are semiconducting compounds having one or more phthalimide units and/or one or more head-to-head (H-H) substituted biheteroaryl units. Such compounds can be monomeric, oligomeric, or polymeric, and can exhibit desirable electronic properties and possess processing advantages including solution-processability and/or good stability at ambient conditions.

Abstract: The present invention provides a negatively charged minor groove binding compound, oligonucleotide conjugates comprising the same, and methods for using the same. The negatively charged minor groove binding compounds of the present invention comprises an acidic moiety that is capable of being ionized under physiological conditions. In particular, the negatively charged minor groove binding compound of the present invention comprises a binding moiety that binds preferentially into a minor groove of a double, triple or higher stranded DNA, RNA, PNA or hybrids thereof. The binding moiety comprises at least one aryl moiety and an acidic moiety which is covalently attached to a phenyl portion of the aryl moiety or to a heteroatom of a heteroaryl portion of the aryl moiety.

Abstract: Compounds of the general formula (I) or (IA) in which X is H, Y is a leaving group, R1 and optionally also R3 preferably being an aromatic DNA binding subunit are prodrug analogues of duocarmycin. The compounds are expected to be hydroxylated at the carbon atom to which X is joined, by cytochrome P450, in particular by CYP1B1, expressed at high levels in tumors. The prodrug is expected to be activated preferentially in tumor cells, where it will act as a DNA alkylating agent preventing cell division.

Abstract: The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as other diagnostic and therapeutic moieties. The invention provides prodrugs and conjugates of the duocarmycin analogues with the linker arms of the invention.

Abstract: The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as other diagnostic and therapeutic moieties. The invention provides prodrugs and conjugates of the duocarmycin analogues with the linker arms of the invention.

Abstract: Provided is a heterocyclic compound represented by Formula I: wherein Ar1 is a linking group and a C6-C16 arylene or heteroarylene group; Ar2 and Ar3 are each independently a C6-C20 aryl group, a C4-C20 heteroaryl group or a C6-C20 fused polycyclic group; Ar4 is a C6-C20 aryl group, a C6-C20 aryloxy group, a C4-C20 heteroaryl group or a C6-C20 fused polycyclic group; and Ar1 and Ar3, or Ar2 and Ar3 may be connected to each other to form a ring. The heterocyclic compound has high electrical stability and excellent charge transporting capability, and thus can be efficiently used as a material for forming at least one of a hole injecting layer, a hole transporting layer and an emitting layer suitable for fluorescent and phosphorescent devices realizing all colors including red, green, blue and white.

Abstract: A heterocyclic compound represented by Formula 1 below: X is selected from the group consisting of nitrogen, boron, and phosphorous; and Ar1, Ar2, Ar3 and Ar4 are each independently selected from the group consisting of a C6-C30 substituted or unsubstituted aryl group, a C6-C30 substituted or unsubstituted aryloxy group, a C4-C20 substituted or unsubstituted heterocyclic group, and a C6-C20 fused polycyclic group. The heterocyclic compound can be included in emission layers of top emission and bottom emission organic light emitting devices.

Abstract: Disclosed are compositions which modulate the interaction with nerve growth factor and precursors thereof with neurotrophic receptors. Also disclosed are methods of using the compositions of the invention, including methods of administration.

Abstract: Tricyclic 5-6-5 heteroaromatic keratin dyeing compounds having two heteroatoms. Compositions for the oxidative dyeing of keratin fibers, comprising a medium suitable for dyeing and one or more tricyclic 5-6-5 heteroaromatic keratin dyeing compounds having two heteroatoms. A method for oxidative dyeing of keratin fibers, comprising applying such compositions in the presence of an oxidizing agent, for a period sufficient to develop the desired coloration.

Abstract: The present invention relates to the compounds of formula I: their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of such compounds in the control or prevention of illnesses such as cancer.

Abstract: Methods for treating a neoplastic disease with an antibody-cytotoxin conjugate molecule, methods of synthesizing an antibody-cytotoxin conjugate molecule are provided. Compounds that are useful as antibody-cytotoxin conjugate molecule or useful in the synthesis of these molecules are also provided.

Abstract: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytotoxic drugs in a targeted fashion.

Abstract: The present invention provides a novel ?-sulfonimide compound having at least one imide group and at least one sulfonyl group and a method for preparing the same.

Abstract: Tricyclic 5-6-5 heteroaromatic keratin dyeing compounds having two heteroatoms. Compositions for the oxidative dyeing of keratin fibers, comprising a medium suitable for dyeing and one or more tricyclic 5-6-5 heteroaromatic keratin dyeing compounds having two heteroatoms. A method for oxidative dyeing of keratin fibers, comprising applying such compositions in the presence of an oxidizing agent, for a period sufficient to develop the desired coloration.

Abstract: Improved synthesis of seco(?)CBI (5-hydroxy-3-amino-1-[S]-(chloromethyl)-1,2-dihydro-3H-benz(e)indole): and improved syntheses therefrom of a wide variety of CC-1065 analogs that comprise a cyclopropabenzidole (CBI) alkylating moiety, and which are collectively DC1 and its derivatives, for the synthesis of cell-targeted therapeutic agents.

Abstract: The chemotherapy of malignant tumours is greatly restricted by the generally slight differentiation of the available cytostatic agents between normal and malignant tissue. In order to achieve an improvement of the selectivity in cancer therapy, novel prodrugs have been developed from 6-hydroxy-2,3-dihydro-1H-indolene, 5-hydroxy-1,2-dihydro-3H-pyrrolo[3,2-e]indolene and 5-hydroxy-1,2-dihydro-3H-benzo[e]indolene as well as from 6-hydroxy-1,2,3,4-tetrahydro-benzo[f]-quinolines, that may be used within the framework of the ADEP therapy (antibody directed enzyme prodrug therapy). The new prodrugs are characterised by a high difference in toxicity between the prodrug and underlying drug and by a very high efficacy of the drug. After splitting off of the glycosidic and/or acetal group on the phenolic hydroxy groups of the prodrugs, a spirocyclopropacyclohexadiene is formed which, being a highly toxic group, effects an alkylation of the DNA or RNA.

Abstract: The invention is based on the discovery that a remarkable improvement in the performance of maleimide thermosets can be achieved through the incorporation of imide-extended mono-, bis-, or polymaleimide compounds. These imide-extended maleimide compounds are readily prepared by the condensation of appropriate anhydrides with appropriate diamines to give amine terminated compounds. These compounds are then condensed with excess maleic anhydride to yield imide-extended maleimide compounds.

Abstract: The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as other diagnostic and therapeutic moieties. The invention provides prodrugs and conjugates of the duocarmycin analogues with the linker arms of the invention.

Abstract: Compounds represented by the general formula (I): which two DNA strands can be interstrand-crossliked: A-L-B-X-B-L-A??(I) wherein B represents a chemical structure capable of recognizing the nucleotide sequence of DNA; A represents a chemical structure capable of binding to one of the bases of DNA; L represents a linker by which the chemical structures of A and B can be linked to each other; X represents a spacer by which the A-L-B components can be linked to each other. A method of interstrand-crosslinking DNA by using these compounds; and medicinal compositions containing interstarand-crosslinking agents of DNA.

Abstract: Compounds of formula (III) or (V), wherein is a solid support; L is a linking group or a single bond; T is a combinatorial unit; n is a positive integer, where if n is greater than 1, each T may be different: X is an electrophilic leaving group; Y is selected from NH-Prot, O-Prot, S-Prot, NO2, —NHOH. N3, NHR, NRR, N?NR, N(O)RR, NHSO2R, N?N?PhR, SR or SSR, where Prot represents a protecting group; A and B collectively represent a fused benzene or pyrrole ring (in either orientation), which is optionally substituted by up to respectively 4 or 2 groups independently selected from R, OH, OR, halo, nitro, amino, Me3Sn, CO2H, CO2R, R1 is a nitrogen protecting group, where if Y includes a protecting group, these protecting groups are orthogonal and R2 and R7 are independently selected from H, R, OH, OR, halo, nitro, amino, Me3Sn, and other related compounds and collections of compounds.

Abstract: The invention relates to fluorescent dyes. More particularly, the invention relates to fluorescent cyanine dyes, and especially to water soluble fluorescent cyanine dyes that contain additional sites for attachment to biomolecules. The invention provides a group of novel, water soluble fluorescent cyanine dyes that have distinct fluorescence characteristics that permit their use in any assay or method suited to water soluble fluorescent dyes, and especially to assays requiring a plurality of distinguishable fluorescent markers. The invention further relates to nucleotides, nucleosides, polynucleotides and polypeptides labeled with novel fluorescent cyanine dyes according to the invention, and methods of using them.

Abstract: Indole-2,3-dione-3-oxime derivatives, for instance compounds represented by the formula are capable of antagonizing the effect of excitatory amino acids, such as glutamate. Also disclosed are methods of preparing the compounds, pharmaceutical compositions comprising them, and methods of treatment of disorders or diseases which are responsive to excitatory amino acid receptor antagonists.

Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.