Abstract: The invention pertains to a near-infrared fluorescent dye that is cell permeable and can be attached to selected proteins in living cells. The dye has the general formula or its corresponding spirolactone wherein Y is chosen from the group consisting of Si, Ge and Sn; R0 is —COO? or COOH; R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15 and R16 are substituents, including hydrogen, independently from each other. The dye (i) absorbs and emits light at wavelengths above 600 nm; (ii) possesses high photostability; (iii) has high extinction coefficients and high quantum yields; (iv) can be derivatized with different molecules; and (v) is membrane-permeable and shows minimal background binding to biomolecules and biomolecular structures.

Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein each of the variables listed above are as defined and described herein, compositions thereof, and methods of using the same.

Abstract: As described herein, the present invention provides compounds useful for treating or lessening the severity of a neurodegenerative disorder. The present invention also provides methods of treating or lessening the severity of such disorders wherein said method comprises administering to a patient a compound of the present invention, or composition thereof. Said method is useful for treating or lessening the severity of, for example, Alzheimer's disease.

Abstract: In accordance with the present invention, novel multifunctional compounds have been developed which have orthogonal reactive groups thereon, thereby facilitating preparation of compounds having multiple functional properties (e.g., a targeting moiety and a biologically active moiety). Such constructs are useful for a variety of applications, e.g., for the delivery of biologically compatible materials, and release thereof in active form. Therefore, in accordance with the present invention, there are provided multifunctional linkers of defined structure, as well as various derivatives thereof bearing one or more biologically active components thereon. Also provided in accordance with the present invention are methods for the preparation of such constructs, as well as various uses thereof.

Abstract: Organic materials which possess outstanding stability to oxidative, thermal or light-induced degradation comprise as stabilizers at least one compound of the formula (I) wherein the general symbols are as defined in claim 1. The compounds of formula I are especially useful as stabilizers for protecting polymers and lubricants against oxidative, thermal or light-induced degradation and as scavengers for oxidized developer in color photographic material.

Abstract: The present invention relates to free cholesterol analogs bearing a boron dipyrromethene difluoro (BODIPY) fluorophore in the side chain and methods of preparation. The compounds of the present invention can be used in fluorescence spectroscopy and fluorescence microscopy to visualize the exchange, distribution, and trafficking of free cholesterol between living cells and to monitor the movement of free cholesterol between ordered and disordered lipid domains in membranes.

Abstract: The present invention is directed toward a method for determination of marinobufagenin concentration in a body specimen through conjugation of marinobufagenin to a suitable protein, thereby creating a conjugate which will trigger an antibody response in a host. The conjugated marinobufagenin is immunogenic. The antibodies so produced may be employed in an ELISA test to ascertain the concentration of marinobufagenin in a body specimen. A number of unique compounds are created in the process and are disclosed. An ELISA assay may be employed.

Abstract: There are provided a novel process for producing [{(5Z,7E)-(1S,3R,20S)-1,3-dihydroxy-9,10-secopregna-5,7,10(19),16-tetraen-20-yl}oxy]-N-(2,2,3,3,3-pentafluoropropyl)acetamide, which process is characterized by irradiating a compound represented by the formula: with UV to ring-open the compound, and then isomerizing the resulting compound; an intermediate useful for carrying out the process; and a process for producing the intermediate.

Abstract: Polyfluorene polymers and copolymers having substantial amounts (10-100%) of fluorenes coupled at the 2 and 5 positions of fluorene are useful as active layers in OLED devices where triplet energies >2.10 eV are required.

Abstract: The present invention relates to free cholesterol analogs bearing a boron dipyrromethene difluoro (BODIPY) fluorophore in the side chain and methods of preparation. The compounds of the present invention can be used in fluorescence spectroscopy and fluorescence microscopy to visualize the exchange, distribution, and trafficking of free cholesterol between living cells and to monitor the movement of free cholesterol between ordered and disordered lipid domains in membranes.

Abstract: This invention relates to a process for the production of 7&agr;-methyl steroids of general formula I, 1

Abstract: The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, thiazolidinedione analogs that have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds that have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester-containing thiazolidinedione analogs are also taught.

Abstract: The present invention involves intermediates, including a 7&agr;-substituted steroid (II), 1

Abstract: The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.

Abstract: Compounds of formula I wherein R1, R2, and R3 independently of one another are hydrogen; C1-C20alkyl which is unsubstituted or substituted by OH, C1-C4alkoxy, C1-C4alkylthio, phenylthio, F, Cl, Br, I, CN, (C1-8alkyl)O—(CO)—, (C1-C4alkyl)—(CO)O— or/and di(C1-C4alkyl)amino; or R1, R2, and R3 independently of one another are C3-C6alkenyl; phenyl which is unsubstituted or substituted by OH, C1-C4alkoxy, C1-C4alkylthio, phenylthio, F, Cl, Br, I, CN, (C1-C8alkyl)O(CO)—, (C1-C4alkyl)—(CO)O— or/— and di(C1-C4alkyl)amino; or R1 and R2 together are C2-C9alkylene, o-xylylene, 2-butenylene, C3-C9oxaalkylene or C3-C9azaalkylene; R4, R5, R6, and R7 independently of one another are sec-C3-C20alkyl, tert-C4-C20alkyl or phenyl wherein these radicals are unsubstituted or substituted by OH, C1-C4alkoxy, C1-C4alkylthio, phenylthio, F, Cl, Br, I, CN, (C1-C8alkyl)O(CO)—, (C1-C4alkyl)—(CO)O— or/and di(C1-C4alkyl)amino; or R4 and R5, and/or R6 and R7

Abstract: A reagent having the general formula of General Formula I: 1

Abstract: The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.

Abstract: This invention relates to novel inhibitors of androgen synthesis that are useful in the treatment of prostate cancer and benign prostatic hypertrophy. The present invention also provides methods of synthesizing these novel compounds, pharmaceutical compositions containing these novel compounds, and methods of treating prostate cancer and benign prostatic hypertrophy using the androgen synthesis inhibitors of the present invention.

Abstract: The invention relates to the field of polymer- and other matrix-supported sapphyrins. Disclosed are silica gel, glass, resin and other polymer- and matrix-supported sapphyrins and sapphyrin-containing chromatographic and electrophoretic supports.

Abstract: The present invention discloses novel steroid nitrite ester derivatives, and to their use treating inflammatory diseases.

Abstract: The novel intermediates of the formula ##STR1## wherein L, K and M are as defined in the specification which are useful intermediates for the preparation of .DELTA..sup.4,9(11),16 -pregnatriene-3-ones.

Abstract: Compounds of the formula I ##STR1## are inhibitors of 5.alpha.-reductase, and are useful for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, prostatic carcinoma, prostatitis and benign prostatic hyperplasia.

Abstract: The invention relates to linker-modified bile acid derivatives of the formula I: ##STR1## wherein the radicals X.sup.1, X.sup.2, X.sup.3 and Y and n are as defined in the claims, and to a process for their preparation. The compounds according to the invention are therapeutically active and are thus suitable as drugs, especially as hypolipldemics. The invention further relates to the use of the bile acid derivatives according to the invention as drugs.

Abstract: A process for the preparation of a compound of the formula ##STR1## wherein R.sub.1 is acyl of 1 to 8 carbon atoms, by reducing an intermediary to form an alcohol, oxidizing the alcohol to form an aidehyde, which is subjected to the action of an acyloxylation agent.

Abstract: A method of treatment of androgen-related diseases such as prostate cancer in susceptible male animals, including humans, comprises administering novel antiandrogens and/or novel sex steroid biosynthesis inhibitors as part of a combination therapy. Sex steroid biosynthesis inhibitors, especially those capable of inhibiting conversion of dehydroepiandrosterone (DHEA) or 4-androstenedione (.DELTA..sup.4 -dione) to natural sex steroida (and testosterone into dihydrotestosterone) in peripheral tissues, are used in combination with antiandrogens usually after blockade of testicular hormonal secretions. Antiestrogens can also be part of the combination therapy. Pharmaceutical compositions and two, three, four and five component kits are useful for such combination treatment.

Abstract: Naphthalocyanine-chelate complexes of formula I ##STR1## are described which contain as central atom M aluminum, gallium, indium, fin, ruthenium or preferably germanium and in which the remaining symbols are as defined in claim 1. The complexes can be used inter alia in the photodynamic chemotherapy of tumors.

Abstract: The invention includes compounds of the following formula ##STR1## where A and B either A and B form an additional double bond and D is a hydrogen atom or B and D form an additional double bond and A is a hydrogen atom and the other variables are as defined in the specification. Also disclosed is a process of making the compounds and a process of using the compounds to make compounds of the following formula ##STR2## where the variables are defined in the specification. These compounds are useful as antigestigens.

Abstract: There are provided pregnane derivatives represented by formula ##STR1## wherein A.sup.1 represents a hydrogen atom or a hydroxyl group, A.sup.2 represents a substituent such as a hydroxyl group when A.sup.1 represents a hydrogen atom, or A.sup.2 represents a hydrogen atom when A.sup.1 represents a hydroxyl group, or A.sup.1 and A.sup.2 are combined together to form an oxo group; D.sup.1 represents a substituent such as a hydroxyl group, and D.sup.2 represents a hydrogen atom, or D.sup.1 and D.sup.2 are combined together to form an epoxy group or a single bond; D.sup.3, D.sup.5 and D.sup.7 each represents a hydrogen atom, D.sup.4 represents a hydroxyl group, and D.sup.6 represents a substituent such as a hydroxyl group, or D.sup.3 and D.sup.4 may be combined together to form an epoxy group or a single bond, or D.sup.4 and D.sup.5 may be combined together to form a single bond, or D.sup.5 and D.sup.6 may be combined together to form an epoxy group or a single bond, or D.sup.6 and D.sup.

Abstract: The process of the invention comprises reacting a C-22-halo-23,24-bisnorsteroid or C-22-halo-23,24-bisnor-9,10-secosteroid with a nickel complex of an electron withdrawing alkene of the formula ##STR1## wherein R.sub.1 is hydrogen, hydroxycarbonyl, lower alkoxycarbonyl, lower alkylcarbonyl or unsubstituted or substituted lower alkyl, and R.sub.2 is hydroxyl, lower alkoxy, or unsubstituted or substituted lower alkyl, to yield a C-25 or C-26 precursor of the formula ##STR2## which is appropriately functionalized for conversion into the corresponding steroid or secosteroid by treatment as hereinafter described.

Abstract: 9.alpha.-Hydroxy-19,11.beta.-bridged steroids of general formula I ##STR1## are described. The more detailed meaning of A, B, R.sup.1, R.sup.2, G, Z, R.sup.4 --Y and R.sup.4' --Y' follows from the description. The steroids of general formula I have antigestagen and/or antiglucocorticoidal action and can be used for the production of pharmaceutical agents.

Abstract: Steroid compounds of the following general formulas (I), (II) and (III) are provided: ##STR1## In the above formulas, R.sup.1 and R.sup.2 each is a hydrogen atom or a hydroxyl-protecting group, R is a group of the formula --CH.sub.2 --X (in which X is a substituent such as a hydroxyl group), a carboxyl group or a protected carboxyl group, A.sup.1 is an aryl group, a lower alkyl group or an aralkyl group, and Z.sup.1, Z.sup.2, Z.sup.3 and Z.sup.4 each is a hydrogen atom, a hydroxyl group or a protected hydroxyl group.The above steroid compounds are useful as intermediates for the synthesis of vitamin D.sub.3 derivatives having a hydroxyl group at the 1.alpha.-position.

Abstract: A compound of the formula ##STR1## wherein Hal is chlorine or bromine, R is selected from the group consisting of alkyl of 1 to 6 carbon atoms, aralkyl of 7 to 15 carbon atoms and a silylated group, K is a protective group selected from the group consisting of ##STR2## n is 2 or 3 and the wavy lines mean the groups may have either isomer form or are mixtures thereof which are intermediates for .DELTA..sup.4,9(11),16 -pregnatriene-3-ones.

Abstract: Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids of the formula ##STR1## and their non-toxic, pharmaceutically acceptable acid addition salts possessing a remarkable antiglucocorticoidal activity.

Abstract: An improved curing agent for use in coatings, laminates, moldings, castings and adhesives comprising the use of an amine-boron adduct component along with anhydride and epoxy component mixtures. Also provided is an improved process for the preparation of tertiary amine borane curing agents.

Abstract: Novel silicon-organic compounds containing an oxazolidine group are defined by the general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, X, n and y have the meanings reported in the description. These compounds are capable of co-cross-linking and to act as adhesion promoters on various polar substrates, in compositions based on poly-isocyanates, polyepoxides or polacrylates, in the field of sealants and adhesives.

Abstract: 17.beta.-Cyano-17.alpha.-hydroxy steroids (I) are transformed to 17.alpha.-halo silyl ethers (II) which are intermediates useful in the production of progesterones (V), 17-hydroxyprogesterones (VI), corticoids (VII) and 21-halo corticoids (III) which can readily be transformed to corticoids (VII).

Abstract: A process of producing a silanic or siloxanic compound containing at least one cycloalkyl ring by the hydrogenation of a corresponding compound containing at least one aromatic ring, in the presence of a Raney nickel catalyst having a granulometry comprised essentially between 10 and 150 micrometers and a surface area of at least 80 m.sup.2 /g.

Abstract: The present invention is a process for conversion of .DELTA..sup.16 -steroids (I) ##STR1## to the corresponding .DELTA..sup.17(20) -20-silyl ether (III) ##STR2## by reaction with (1) a preformed copper hydride or a metal hydride reducing agent in the presence of a copper species and (2) a silylating agent. The .DELTA..sup.17(20) -20-silyl ether (III) are useful intermediates in the preparation of steroids useful as pharmaceuticals.

Abstract: A composition including a cationic transition metal coordination complex and a borate anion, wherein said composition is capable of absorbing actinic radiation and producing free radicals which can initiate free radical addition polymerization of a free radical addition polymerizable or crosslinkable monomer is disclosed. The compositions are particularly useful as visible light photoinitiators.

Abstract: C.sub.16 -unsaturated corticoids are readily transformed to the corresponding 16.alpha.-methyl-17.alpha.-hydroxy corticoids by use of a .DELTA..sup.17 (.sup.20)-20-silyl ether.

Abstract: The invention is the compound 17.beta.-cyano-9.alpha., 17.alpha.-dihydroxyandrost-4-en-3-one (I) which is particularly useful as an intermediate in the production of the 17.alpha.-halo silyl ethers (II).

Abstract: Novel 11.beta.-alkynylphenyl-19-nor-steroids of the formula ##STR1## wherein R.sub.1 is alkynyl of 2 to 8 carbon atoms optionally substituted with at least one member of the group consisting of --OH halogen, trialkylsilyl of 1 to 6 alkyl carbon atoms, alkoxy and alkylthio of 1 to 6 carbon atoms and dialkylamino of 1 to 6 alkyl carbon atoms having remarkably antiprogestomimetic and antiglucocorticoidal activity.

Abstract: C.sub.16 -unsaturated corticoids are readily transformed to the corresponding 16.alpha.-methyl-17.alpha.-hydroxy corticoids by use of a .DELTA.17(20)-20-silyl ether.

Abstract: Novel 19-nor steroids and 19-nor-D-homo-steroids of the formula ##STR1## wherein R.sub.1 is an organic radical of 1 to 18 carbon atoms containing at least one atom selected from the group consisting of nitrogen, phosphorous and silicon with the atom immediately adjacent to the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is selected from the group consisting of a pentagonal ring and a hexagonal ring optionally substituted and optionally containing a double bond, B and C together form a double bond or an epoxy group, the C.dbd.A group at position 3 is selected from the group consisting of C.dbd.O, ketal, which may be open or closed ##STR2## are selected from the group consisting of alkyl of 1 to 8 carbon atoms and aralkyl of 7 to 15 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having anti-glucocorticoid activity and a process for their preparation.

Abstract: A process for preparing a 3.beta.,7.beta.-dihydroxy-.DELTA..sup.5 -steroid of the formula ##STR1## wherein Q is ##STR2## and R.sub.1 is hydrogen, trimethylacetyl, tert-butyldimethylsilyl, dimethyl-2-(3-methylbutyl)silyl or tribenzylsilyl, comprises fermenting a 3.beta.-hydroxy-.DELTA..sup.5 -steroid of the formula ##STR3## wherein Q is as defined above, andR.sub.2 is hydrogen or alkanoyl of 2-6 carbon atoms, with a culture of Botryodiplodia malorum to obtain the corresponding 3.beta.,7.beta.-dihydroxy-.DELTA..sup.5 -steroid; and, optionally, reacting the resultant product with trimethylacetic anhydride, tert-butyldimethylsilyl chloride, dimethyl-2-(3-methylbutyl)silyl chloride, or tribenzylsilyl chloride.