Abstract: The invention provides Zn-chelating compounds that are molecularly engineered to bind to a specific target sequence in a protein of interest. The Zn2+ ion is far less toxic and promiscuous than nickel and therefore provides an attractive alternative to Ni-based labeling systems. Invention Zn-chelating compounds also do not require oxidizable thiols and therefore can be used in non-reducing environments such as the surface of living cells. In addition, the target sequence is genetically encodable and requires incorporation of only a few amino acids, unlike fusions to fluorescent proteins such as GFP.

Abstract: A compound represented by general formula (IA) or a salt thereof useful as a fluorescent probe for zinc: wherein R1 and R2 represent a hydrogen atom or a group represented by formula (A), wherein X1, X2, X3, and X4 represent a hydrogen atom, an alkyl group, a 2-pyridylmethyl group, or a protective group for an amino group, and m and n represent 0 or 1 provided that R1 and R2 do not simultaneously represent hydrogen atoms; R3 and R4 represent a hydrogen atom or a halogen atom; and R5 and R6 represent a hydrogen atom, an alkylcarbonyl group, or an alkylcarbonyloxymethyl group, and R7 represents a hydrogen atom or an alkyl group.

Abstract: The present invention relates to a process for the production of compound (A) comprising reacting compound (B) with compound (C). A further ring closure reaction may be necessary. The invention further relates to certain novel compounds of formula (B).

Abstract: Novel quinones are provided, as well as compositions comprising these novel quinones. Methods of using the novel quinones in treatment of various indications including cancer are also provided.

Abstract: Disclosed are a novel compound represented by the following chemical formula (1), useful for the prophylaxis and treatment of angiogenic diseases, its production, and a novel microorganism producing the same. Aspergillus sp. Y80118 isolated from soil was found to produce 7,8-dihydro-1,7-dihydroxy-3-hydroxymethyl-xanthenone-8-carboxylic acid methylester which inhibits VEGF-induced proliferation of HUVEC, angiogenesis in CAM assay, and tumor growth. The novel compound can be effectively used for the medical treatment of anigiogenic diseases, including cancers, rheumatoid arthritis, and diabetic retinopathy.

Abstract: Therapeutic compounds and compositions for the treatment of infectious diseases are disclosed. The compounds are xanthones and xanthone derivatives, such as 3,5-bis-&egr;-(N,N-diethylamino)amyloxyxanthone. The described compositions include such compounds and a pharmaceutical carrier. These compositions also can include additional materials conventionally used to form therapeutic compositions. 3,5-bis-&egr;-(N,N-diethylamino)amyloxyxanthone has an IC50 for Plasmodium falciparum of about 0.15 &mgr;M, and an IC50 for Leishmania mexicana of <<0.5 &mgr;M. These compositions are additionally useful for forming soluble complexes with heme and porphyrins.

Abstract: Compounds represented by the following general formula (I): wherein R1, R2, R3, R4, R5, and R6 independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, or a C1-6 alkoxyl group, R7 and R8 independently represent a C1-6 alkyl group or an aryl group which may be substituted, R9 and R10 independently represent a hydrogen atom, a C1-6 alkyl group, or a C1-6 alkoxyl group, and R11 represents a hydrogen atom or a C1-6 alkanoyl group, or salts thereof. The aforementioned compounds are substantially non-fluorescent and react with singlet oxygen under a physiological condition to give a fluorescent substance, and therefore they are useful as agents for measurement of singlet oxygen.

Abstract: This invention relates to novel tracers and their synthesis and use in an immunoassay for the detection of controlled drugs such as amphetamine (APM), methamphetamine (MAPM) and their derivatives, in a biological or aqueous sample. In particular, this invention provides methods for synthesizing novel tracers in which a non-controlled substance is both the starting material in tracer synthesis and the binding site on the resulting novel tracer for the antibody, thereby eliminating the necessity of using controlled substances as starting materials. In addition, the novel tracers of the present invention can be used as an analyte analog in an immunoassay, such as a continuous flow displacement immunoassay. It was unexpectedly discovered that the novel tracers of the present invention substantially improve the performance of the continuous flow displacement immunoassay as compared with conventionally designed tracers.

Abstract: Novel fluorescent substrates of human cytochrome P450 enzymes are provided. Also provided are methods for their manufacture and use. These substrates are useful in assessing cytochrome P450 enzyme activity and in selecting compounds which inhibit cytochrome P450 enzyme activity and, in particular, for identifying potential adverse drug interactions which are mediated by inhibition of cytochrome P450 enzyme activity.

Abstract: An anionic fluorescein homologue capable of selectively staining degenerating neurons in brain slices, the method of making the anionic fluorescein homologue, and the method of using the same for detecting neuronal degeneration. Two anionic fluorescein based fluorescent stains are the water soluble tribasic salt of a mixture of the fluorescein isomers 5-carboxyfluorescein and 6-carboxyfluorescein, and the water soluble tetrabasic salt of 5,6 dicarboxyfluorescein.

Abstract: Compounds of Formula 1, Formula 2 or Formula 3 where X is O, S, or (CR.sub.1 R.sub.1).sub.n where n is 0, 1 or 2; Y is a bivalent radical having Formula 4 or Formula 5 where o is an integer from 1 to 4 ##STR1## or Y is a bivalent aryl or 5 or 6 membered heteroaryl radical having 1 to 3 heteroatoms selected from N, S and O, said aryl or heteroaryl groups being unsubstituted, or substituted with 1 to 3 C.sub.1-6 alkyl or with 1 to 3 C.sub.1-6 fluoroalkyl groups; and the remaining symbols have the meaning described in the specification, have RXR selective retinoid agonist-like activity.

Abstract: 3-Substituted-.beta.-lapachone analogs and their use either alone or to augment chemotherapy or radiotherapy to induce programmed neoplastic cell death without exhibiting toxicity to surrounding normal cells are disclosed. In particular, 3-allyl-.beta.-lapachones, 3-alkyl-.beta.-lapachones and 3-halo-.beta.-lapachones were found to be Topoisomerase (Topo I) inhibitors. When these analogs are used alone there is a reversible single-strand break in the DNA of neoplastic cells causing apoptosis and cell death in some cells. However, when these analogs are combined with chemotherapy or X-irradiation, an irreversible Topo I-mediated break is achieved. A new and more efficient chemical synthesis of the compounds is also disclosed.

Abstract: The invention relates to novel compounds of formula (I) wherein R is a hydrogen atom or a C.sub.1 -C.sub.5 alkyl group and R.sup.2 is selected from the group consisting of: (a) a straight-chained or branched C.sub.5 -C.sub.12 alkyl radical; (b) a group --O--R.sup.4, wherein R.sup.4 is a straight-chained or branched C.sub.2 -C.sub.9 alkyl radical which may be substituted at the terminal carbon atom by a phenyl group; (c) a group --(CH.sub.2).sub.n --O--alkyl, wherein n is an integer of from 1 to 7 and the alkyl group contains from 1 to 5 carbon atoms, having the (3S,4S) configuration, essentially free of the (3R,4R) enantiomer. The invention also relates to process for the preparation of compounds of formula (I) as defined above. The invention further relates to pharmaceutical compositions which possess analgesic, anti-inflammatory, anti-emetic, anti-glaucoma, leukocytes antiadhesion or PAF activity, containing as active ingredient compounds of formula (I) as defined above.

Abstract: Non-psychoactive derivatives of .DELTA..sup.6 -THC-7-oic acid are described which have analgesic and anti-inflammatory properties.

Abstract: Compounds of the formula I ##STR1## in which X is O, S, SO, SO.sub.2 or NR.sub.13, R.sub.13 is, for example, methyl, and R.sub.1 to R.sub.12, independently of one another, are, for example, H, C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 Alkoxy, halogen or --CN. The compounds are photosensitive and photochromic and are suitable as photosensitizers and simultaneously as color indicators, and as photoswitchable color filters.

Abstract: The present invention is directed to novel THC derivatives which are synthesized for the covalent attachment to antigens (proteins or polypeptides) for the preparation of antibodies or receptors to the THC metabolites. The resulting novel antigens may be used for the production of antibodies or receptors using standard methods. Once generated, the antibodies or receptors and the novel derivatives which are covalently attached to proteins, polypeptides or labels may be used in the immunoassay process.

Abstract: Aryloxypropanolaminotetralins with beta-antagonist activity of the formula ##STR1## wherein R is hydrogen, hydroxy or methoxy and Ar is an optionally substituted aromatic or heteroaromatic group, in optically active or inactive form as well as their acid addition salts are described.A process for their preparation and pharmaceutical compositions containing the compounds of formula (i) or their pharmaceutically acceptable acid addition salts, are also described.

Abstract: The compound of the formula ##STR1## and its tautomer are obtained from cultures of Eupenicillium sp. The compound has antifungal activity.

Abstract: Disclosed are rigid fluorinated monomers 9-phenyl-9-perfluoroalkylxanthene ##STR1## . The monomers have utility in the preparation of advanced high-performance polymers, particularly polyimides.

Abstract: Described are a series of novel photochromic benzopyran and naphthopyran compounds substituted with (1) a cyclopropyl group and (2) a phenyl, substituted phenyl, or 5-member aromatic heterocyclic group at the 2-position of the benzopyran or naphthopyran ring. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic or plano lenses that incorporate the novel pyran compounds or combinations of the novel pyran compounds with other complementary photochromic compounds are described.

Abstract: According to the present invention, there is provided a non-linear optical device comprising a non-linear optical medium comprising an organic compound, which remarkably improves the non-linear optical properties. The non-linear optical device according to the present invention is suited for the second and third harmonic generations, photomixing optical parametric oscillations, optical switches and optical bistable devices.

Abstract: This disclosure related to a method and reagents for determining tetrahydrocannabinoids (THC) and THC metabolites in a biological fluid such as urine. In particular, this disclosure relates to a fluorescence polarization immunoassay procedure for determining the presence of THC and to a novel class of tracer compounds employed as reagents in such procedures. The procedure described also provides for novel wash reagent for a THC fluorescence polarization assay.

Abstract: The invention relates to novel (3S,4S)-7-hydroxy-.DELTA..sup.6 -tetrahydrocannabinol homologes and derivatives, essentially free of the (3R,4R) form and to pharmaceutical compositions which have a potent analgetic, antiemetic and antiglaucoma effect, which compositions contain an effective dosage of a compound of this type. The novel pharmaceutical compositions are practically devoid of the undesired side effects of the (3R,4R) type compounds, such as cannabimimetic psychotropic effects. The pharmaceutical compositions are of special utility in cases of acute and of chronic pain. The invention also relates to a process for the production of the above defined novel compounds.

Abstract: 2,6-di-O-methyl-beta-cyclodextrin complexes of compounds of the formula (1a) ##STR1## wherein R.sup.2' stands for C.sub.1 to C.sub.12 alkyl or a group of the formula ##STR2## in which R.sup.11 is C.sub.1 to C.sub.4 alkyl;R.sup.12 is hydrogen or C.sub.1 to C.sub.4 alkyl;n is 0 or 1;p is 1 to 4;r is 1 to 4; andR.sup.3' and R.sup.4' are each C.sub.1 to C.sub.4 alkyl, or pharmaceutically salts thereof are disclosed, having analgesic activity.

Abstract: The invention provides various medical compositions for use in treating or preventing certain of the side effects of diabetes or galactosemia. The active ingredients are selected from a series of novel aldose reductase inhibitory spiro-linked pyrrolidine-2,5-diones of the general formula: ##STR1## or a pharmaceutically acceptable salt, or a non-toxic, biodegradable precursor thereof. Processes for the production of these compounds are also provided. A particular compound suitable for use as an active ingredient is spiro[pyrrolidine-3,9'-xanthene]-2,5-dione.

Abstract: Compounds corresponding to the general formula: ##STR1## in which X and Y identical or different, represent a hydrogen or a halogen atom, a lower alkyl, a lower alkoxy or a trifluormethyl group,A represents a methylene group, a direct bond or an imino--NR.sub.3 -- group in which R.sub.3 is a hydrogen atom or a lower alkyl or lower alkanoyl groupR.sub.1 and R.sub.2 identical or different, each represents a hydrogen atom or a lower alkyl group, or together with the nitrogen atom to which they are attached they form a pyrrolidino, piperidino or methyl-4 piperazine group, andn represents an integer from 1 to 3, in their racemic or optical isomeric forms, as well as their salts of addition with a therapeutically compatible mineral or organic acid.These compounds are useful as antidepressants.

Abstract: The present invention relates to new 6-substituted 6H-dibenzo [b,d]pyran derivatives, to a process for their preparation and pharmaceutical and veterinary compositions containing them.

Abstract: The present invention comprises novel compounds of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein: G is hydroxymethylene or carbonyl;R.sub.a and R.sub.b are each methyl or hydrogen;R.sub.1 is hydrogen or alkanoyl having one to five carbon atoms;R.sub.2 is hydrogen, bromo, chloro or fluoro;R.sub.3 is hydrogen, bromo, chloro, fluoro, alkyl having one to six carbon atoms, (CH.sub.2).sub.p COOR.sub.4 wherein p is an integer from 0-6 and R.sub.4 is hydrogen, methyl or ethyl, or (CH.sub.2).sub.q OH wherein q is an integer from 1-6; with the proviso that when R.sub.3 is hydrogen or alkyl, R.sub.2 is bromo, chloro or fluoro;Z is (--alk.sub.1).sub.m --X--(alk.sub.2).sub.n --wherein each of (alk.sub.1) and (alk.sub.2) has from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 9;m and n are each zero or 1;X is oxygen or methylene; andW is methyl, pyridyl, piperidyl or ##STR2## wherein W.sub.

Abstract: Reaction of an O-methyl or O-ethyl resorcinol with a cyclohexene carbinol derivative in the presence of a catalyst affords a 6a,10a-trans-1-methoxy or 1-ethoxy-6,6-dimethyl-6,6a,7,8,10,10a-hexahydro-9H-dibenzo[b,d]pyran-9-one derivative.