Abstract: The invention provides cannabinol derivatives and pharmaceutical preparations thereof.

Abstract: The present invention relates to the preparation of chiral glucocorticoid receptor agents via biaryl atropisomers.

Abstract: Compounds of formula I are useful for treating type II diabetes, obesity, hyperglycemia, inadequate glucose clearance, hyperinsulinemia, hypertriglyceridemia, and high-circulating glucocorticoid levels, preparations of the compounds, compositions containing the compounds, and methods of treatment using the compounds.

Abstract: Disclosed are novel compounds represented by the following structural formula:

Abstract: Xanthone derivatives of the formula I where the index and the variables are as defined below: n is 0, 1 or 2; R1 is alkyl or haloalkyl; R2,R3 are alkoxy, alkenyloxy or alkynyloxy, or R2 and R3 together form an unsubstituted or substituted oxyalkyleneoxy group; R4 is halogen, cyano, hydroxyl, amino, mercapto, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, alkylcarbonyloxy or alkylcarbonylthio; R5 is a group R4, where the groups R5 may be different if n=2; X, Y are oxygen or sulfur; Processes for preparing these compounds, compositions comprising them and their use for controlling phytopathogenic harmful fungi are described.

Abstract: A compound represented by the following general formula (I): 1

Abstract: The present invention relates to the preparation of chiral glucocorticoid receptor agents via biaryl atropisomers.

Abstract: A process for supercritical fluid extraction of delta-9-tetrahydrocannabinol (delta-9-THC), delta-8-THC, cannabinoids or other medicinal value compounds from marijuana and other plants. Preferably, the extraction is carried out with a solvent of liquid carbon dioxide alone, or in combination with a solvent of ethanol, methanol, isopropanol, and other nonpolar/semipolar solvents at a temperature and pressure to maintain the solvents in a supercritical state. The extraction process is preferably carried out for a period of from 0 to 9 hours. The extraction process conditions result in different strengths of extracted marijuana and selective isolation of extracted compounds or mixtures of compounds.

Abstract: In this disclosure, novel caanabinol-based tracers suitable for use in immunoassays that detect cannabinoids in a biological sample are disclosed. These cannabinol-based tracers are particularly useful in a continuous flow displacement immunoassay. The disclosure also describes the processes for synthesizing the novel tracers, and the application of these tracers in fluorescence immunoassays for detecting and quantifying cannabinoids in biological samples.

Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.

Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure: 1

Abstract: A catalyst is for use in a reaction using an oxygen-atom-containing reactant and includes a nitrogen-containing heterocyclic compound of the following formula (1): wherein each of R1 and R2 is, identical to or different from each other, a hydrogen atom, a halogen atom, an alkyl group, a haloalkyl group, an aryl group, a cycloalkyl group, a hydroxyl group, an alkoxy group, a carboxyl group, an alkoxycarbonyl group, or an acyl group, and R1 and R2 may be combined to form a double bond or to form an aromatic or non-aromatic ring with the adjacent two carbon atoms, where one or two of heterocyclic ring containing three nitrogen atoms indicated in the formula may be further formed on the R1 or R2, or on the double bond or aromatic or non-aromatic ring formed by R1 and R2; X is an oxygen atom or a hydroxyl group; and Y is a single bond, a methylene group, or a carbonyl group. This catalyst can introduce an oxygen-atom-containing group into an organic substrate under mild conditions.

Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: Compounds of formula I are useful for treating type II diabetes, obesity, hyperglycemia, inadequate glucose clearance, hyperinsulinemia, hypertriglyceridemia, and high-circulating glucocorticoid levels, preparations of the compounds, compositions containing the compounds, and methods of treatment using the compounds.

Abstract: We have now discovered that unexpectedly compounds of the following formulae I or 11 can be used to selectively stimulate the death of mammalian prostate cells, including both epithelial cell and prostate cancer cells, and thus are useful in treating prostate diseases: wherein R and R1 are each independently selected from the group consisting of hydrogen, hydroxy, thio (SH), halogen, substituted and unsubstituted alkyl, substituted and unsubstituted alkenyl, substituted and unsubstituted aryl, and substituted and unsubstituted alkoxy, and salts thereof, wherein the dotted double bond between the ring carbons to which R and R1 are bonded represent an optional ring double bond. Preferred compounds of formula I include those in which at least one of the substituents R and R1 is hydrogen and/or at least one of said substituents is allyl. Specifically preferred compounds include &bgr;-lapachone (i.e., R and R1 both being hydrogen), allyl-&bgr;-lapachone, particularly 3-allyl-&bgr;-lapachone (i.e.

Abstract: The present invention provides an economical and efficient process for converting delta-9-tetrahydrocannabinol to a variety of ester analogs. Delta-9-tetrahydrocannabinol is esterified by reaction with a carboxylic acid, an acid halide or an acid anhydride in the presence of a 4-aminopyridine either alone or in admixture with an organic amine such as a mono-, di-, or tri-alkyl amine.

Abstract: The present invention relates to novel 4-aminotetrahydrobenzisoxazoles or 4-aminotetrahydrobenziothiazoles having gamma-aminobutanoic acid (GABA)-uptake inhibiting activity and thus useful in the treatment of analgesia, psychosis, convulsions, anxiety, epileptic disorders or muscular and movement disorders, such as spastic disorders or symptoms in Huntington's disease or Parkinson disease.

Abstract: Therapeutic compositions for the treatment of infectious diseases are disclosed. These compositions comprise xanthones and xanthone derivatives, such as 2,3,4,5,6-pentahydroxyxanthone. Also disclosed are methods for the treatment of infectious diseases using such compounds.

Abstract: The present invention has for subjects, novel benzopyran derivatives, substituted in position 2 with an adamantyl group as well as the compositions and (co)polymer matrices containing such derivatives. Said derivatives possess interesting photochromic properties.

Abstract: A composition of matter, comprising a cannabinol compound having the structure ##STR1## wherein, Q is --C(R.sup.1)(Y.sup.1)--(CH.sub.2).sub.n --Z.sup.1 ; R.sup.1 is --H or --CH.sub.3 ;Y.sup.1 is --CH.sub.3 or Y.sup.2 ; Y.sup.2 is --N.sub.3 or --NCS; n is 4 or 6;Z.sup.1 is --H, when Y.sup.1 is Y.sup.2, or is Z.sup.2, when Y.sup.1 is --CH.sub.3 ; andZ.sup.2 is --N.sub.3 or --NCS.This composition has good binding affinity to the cannabinoid receptor and therefore, is useful as a receptor probe.

Abstract: Novel water soluble dyes of the formula I are provided ##STR1## wherein R.sup.1 and R.sup.4 are alkyl of 1 to 4 carbon atoms or hydrogen; or R.sup.1 -R.sup.2 or R.sup.2 -R.sup.4 form part of aliphatic heterocyclic rings; R.sup.2 is hydrogen or joined with R.sup.1 or R.sup.4 as described above; R.sup.3 is --(CH.sub.2).sub.m --SO.sub.3.sup.-, where m is 1 to 6;X is N, CH or ##STR2## where Y is 2 --SO.sub.3.sup.- ; Z is 3, 4, 5 or 6 --SO.sub.3.sup.-. The novel dyes are particularly useful as the active media in water solution dye lasers.

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 present invention provides compounds of formula ##STR1## in which R represents an organic group, or a pharmaceutically acceptable metabolically labile ester or amide thereof, or a pharmaceutically acceptable salt thereof, which are useful as antagonists of one or more of the actions of L-glutamate at metabotropic excitatory amino acid receptors.

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: A method of producing a carboxylic acid glucuronide by reacting a carboxylic acid precursor with a blocked sugar epoxide precursor is disclosed. Also disclosed are: deuterated 11-nor-.DELTA..sup.8 - or .DELTA..sup.9 -THC carboxylic acid glucuronide having a deuterated hydrocarbon chain; 5'-deuterated 11-nor-.DELTA..sup.8 - or .DELTA..sup.9 -THC-carboxylic acid or 5'-deuterated .DELTA..sup.8 - or .DELTA..sup.9 -THC glucuronide. The compositions are useful as GC-MS standards; in methods for preparing antibodies reactive with a THC glucuronide; and, in GC-MS diagnostic methods for THC metabolites.

Abstract: Protected amino acid derivatives of the general formula ##STR1## wherein R.sub.1 represents hydrogen atom, and R.sub.2 represents hydrogen, methyl, isopropyl, 1-methylpropyl, 2-methylpropyl, tert-butoxymethyl, 1-tert-butoxyethyl, 2-methylthioethyl, benzyl, carboxamidomethyl, 2-carboxamidoethyl, tert-butoxycarbonylmethyl, 2-(tert-butoxycarbonyl)ethyl, 4-(tert-butoxycarbamido)butyl, 4-tert-butoxybenzyl, indolyl-3-methyl, S-(triphenylmethyl)thiomethyl, 1-(triphenylmethyl)imidazolyl-4-methyl, 3-(N.sup.G -mesitylenesulfonyl)guanidinopropyl, N-xanthylcarboxamidomethyl, 2-(N-xanthylcarboxamido)ethyl or S-(acetamidomethyl)thiomethyl; or R.sub.1 and R.sub.2 together represent propylene radical. Methods for the preparation of said derivatives are provided, and a process for solid phase peptide synthesis using said derivatives is described.

Abstract: Compounds of formula (I) are provided: ##STR1## wherein: R.sup.1 represents an alkyl group; or a group of formula (II), (III), (IV) or (V): ##STR2## and wherein the groups R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen or various organic groups; and pharmaceutically acceptable salts thereof; as well as methods for the preparation of such compounds and their use in the treatment and prophylaxis of hypercholesteremia and arteriosclerosis.

Abstract: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their use for antagonizing angiotensin II receptors in mammals.

Abstract: Novel antagonists of endothelin are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, metabolic, endocrinological, neurological disorders especially cerebral vasospasm, stroke, and head injury, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease, restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, and diabetes.

Abstract: The invention relates to compounds of the formula ##STR1## having the (3S,4S) configuration and being essentially free of the (3R,4R) enantiomer, in which A--B indicates an optional 1(2) or 6(1) double bond, X is carboxy, carbalkoxy, or carboxamido, linked to the ring directly or through an alkylene linkage, G is halogen, alkyl, or oxy, and Y is alkyl, oxy, or oxyalkylene. The invention further relates to the synthesis of such compounds, and to pharmaceutical compositions and therapeutic methods in which such compounds may be employed.

Abstract: Compounds of formula (I) are provided: ##STR1## wherein: R.sup.1 represents an alkyl group; or a group of formula (II), (III), (IV) or (V): ##STR2## and wherein the groups R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen or various organic groups; and pharmaceutically acceptable salts thereof; as well as methods for the preparation of such compounds and their use in the treatment and prophylaxis of hypercholesteremia and arteriosclerosis.

Abstract: A composition of matter, comprising a cannabinol compound having the structure ##STR1## wherein, Q is --C(R.sup.1) (Y.sup.1)--(CH.sub.2).sub.n ----Z.sup.1 ; R.sup.1 is --H or --CH.sub.3 ; Y.sup.1 is --CH.sub.3 or Y.sup.2 ; Y.sup.2 is --N.sub.3 or --NCS; n is 4 or 6; Z.sup.1 is --H, when Y.sup.1 is Y.sup.2, or is Z.sup.2, when Y.sup.1 is --CH.sub.3 ; and Z.sup.2 is --N.sub.3 or --NCS.This composition has good binding affinity to the cannabinoid receptor and therefore, is useful as a receptor probe.

Abstract: The compounds of the present invention have the following formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently phenyl, pyridyl, thienyl, naphthyl, substituted phenyl wherein the substituent is selected from the group consisting of halogen, methoxy, and dialkylamino wherein alkyl contains 1 to 3 carbon atoms; or R.sup.1 and R.sup.2 are independently substituted furanone of the structure ##STR2## wherein R.sup.5 and R.sup.6 are independently alkyl containing 1 to 3 carbon atoms, cycloalkyl containing 5 to 7 carbon atoms, phenyl or substituted phenyl wherein the substituent is alkyl containing 1 to 5 carbon atoms or halogen; R.sup.7 is hydrogen or halogen; or R.sup.1 and R.sup.2 are joined to form ##STR3## R.sup.3 and R.sup.4 are independently hydrogen, alkyl containing 4 to 20 branched, straight chain, cyclic, saturated or unsaturated carbon atoms; or R.sup.3 and R.sup.4 are joined to form ##STR4## wherein R.sup.

Abstract: This invention relates to a class of novel amino bi- and tri-carbocyclic alkane compounds having bis-aryl substitution which exhibit squalene synthase inhibition properties. The bi- and tri-carbocyclic alkane ring contains an amino group and the ring is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.

Abstract: Novel alkenes leading to light producing 1,2-dioxetanes of the formula ##STR1## wherein ArOX is an aryl ring substituted with an X oxy group and A are passive organic groups which allow the 1,2-dioxetane to produce light when triggered by removing X. X is a chemically labile group which is removed by an activating agent. The 1,2-dioxetane compounds can be triggered to produce light at room temperatures.

Abstract: Dibenzo[b,d]pyrans are prepared by heating a dihydroxybenzoic acid derivative in the presence of a Lewis acid catalyst and an inert non-polar solvent in which the dihydroxybenzoic acid is soluble but in which the Lewis acid catalyst is insoluble or very slightly soluble. A typical embodiment involves the preparation of intermediates useful in the synthesis of dronabinol and related dibenzo[b,d]pyrans.

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

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: A method of producing a deuterated or undeuterated 11-nor-.DELTA..sup.8 -tetrahydrocannabinol (THC) glucuronide or deuterated or undeuterated 11-nor-.DELTA..sup.9 -THC glucuronide by reacting a blocked THC carboxylic acid precursor with a blocked sugar epoxide precursor is disclosed. Also disclosed are: deuterated 11-nor-.DELTA..sup.8 - or .DELTA..sup.9 -THC carboxylic acid glucuronide having a deuterated hydrocarbon chain; 5'-deuterated 11-nor-.DELTA..sup.8 - or .DELTA..sup.9 -THC-carboxylic acid or 5'-deuterated .DELTA..sup.8 - or .DELTA..sup.9 -THC glucuronide. The compositions are useful as GC-MS standards; in methods for preparing antibodies reactive with a THC glucuronide; and, in GC-MS diagnostic methods for THC metabolites.

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: A hydrazone compound represented by the following formula (I): ##STR1## wherein R.sub.1 and R.sub.2 each are an aryl group or collectively with the carbon to which they are attached form a polycyclic group; R.sub.3 represents a hydrogen or halogen atom or an alkyl or phenyl group; and R.sub.4 and R.sub.5 each represent an alkyl, aralkyl or aryl group, with the proviso that at least one of R.sub.4 and R.sub.5 is an aryl group, is useful as a charge-transporting material in an electrophotographic photoreceptor and are produced by condensing the corresponding aldehyde with the corresponding H.sub.2 N--NR.sub.4 R.sub.5 hydrazine.

Abstract: Novel cannabinol derivatives are provided which can be used in improved immunoassays for the detection in blood or urine samples of cannabinol metabolites.

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: Substituted xanthene compounds are described which are capable of functioning as absorbers in high intensity light protective compositions and in materials used to prevent the transmission of high intensity light at selected wavelengths. Also described are high intensity light protective compositions containing an effective amount of a substituted xanthene compound and a polymeric compound and a material which prevents transmission of high intensity light at wavelengths between about 482 to about 556 nanometers. The material of this invention can be used to make protective eyewear, optical filters, shields for protecting a persons body from high intensity light, or shields for protecting components of an optical instrument from high intensity light.

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: Compositions and method for accessing delta-9-tetrahydrocannabinol into the system of the body.

Abstract: Described are a series of novel photochromic benzopyran and naphthopyran compounds in which two cyclopropyl groups are appended 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 noval pyran compounds or combinations of the novel pyran compounds with other complementary photochromic compounds are described.

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: Novel cannabinol derivatives are provided which can be used in improved immunoassays for the detection in blood or urine samples of cannabinol metabolites.