Abstract: This invention relates to novel naphthopyrans having an oxygen-containing heterocyclic group F annelated on the i, j, or k side of the naphthopyran ring, having certain substituents at the 2, 5, and 6 positions of the naphthopyran ring. These naphthopyrans may have the formula (I) presented below: These compounds (I) have interesting photochromic properties. Also related to this invention are host materials that contain such naphthopyran compounds, and articles such as ophthalmic lenses or other plastic transparencies that incorporate the naphthopyran compounds.

Abstract: This invention relates to novel naphthopyrans having an oxygen-containing heterocyclic group F annelated on the i, j, or k side of the naphthopyran ring, having certain substituents at the 2, 5, and 6 positions of the naphthopyran ring. These naphthopyrans may have the formula (I) presented below: These compounds (I) have interesting photochromic properties. Also related to this invention are host materials that contain such naphthopyran compounds, and articles such as ophthalmic lenses or other plastic transparencies that incorporate the naphthopyran compounds.

Abstract: The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.

Abstract: Psorospermin and analogs thereof are made using an enantiomerically selective process

Abstract: Biologically active xanthone derivatives, as well as compositions prepared from such derivatives, possessing anti-cancer activity, anti-inflammatory activity, anti-obesity activity, and/or hair growth promotion activity, and a method for producing such derivatives and compositions. The derivatives are obtained by utilizing a heating, extracting and condensing system that efficiently recovers the derivatives from a raw material.

Abstract: The present invention relates to a synthesis of an 8-membered carbocyclic compound having diexomethylene groups, more particularly to a synthesis of an 8-membered carbocyclic compound having diexomethylene groups, a novel compound having the structure represented by the following Chemical Formula 1, from trimethylsilanylmethyl-allenol derivative by the intramolecular Prins cyclization using Lewis acid. The 8-membered carbocyclic compound is a useful intermediate for synthesis of other multicarbocyclic compounds. In Chemical Formula 1, R1 is a phenyl group, and R2 and R3 is a hydrogen atom, or R1, R2 and R3 may be connected with neighboring substituents to form a 5 to 10-membered aliphatic or aromatic ring.

Abstract: This invention relates to novel naphthopyrans having an oxygen-containing heterocyclic group F annelated on the i, j, or k side of the naphthopyran ring, having certain substituents at the 2, 5, and 6 positions of the naphthopyran ring.

Abstract: The present invention relates to a process for the synthesis of oxandrolone from mestanolone. The process comprises the steps of: (a) oxidizing mestanolone to form 17&bgr;-hydroxy-17&agr;-methyl-5&agr;-androst-1-en-3-one; (b) hydroxylating the 17&bgr;-hydroxy-17&agr;-methyl-5&agr;-androst-1-en-3-one to form 1&agr;, 2&agr;, 17&bgr;-trihydroxy-17&agr;-methylandrostan-3-one; (c) cleaving the 1&agr;, 2&agr;, 17&bgr;-trihydroxy-17&agr;-methylandrostan-3-one to form 17&bgr;-hydroxy-17&agr;-methyl-1-oxo-1,2,-seco-A-nor-5&agr;-androstan-2-oic acid; and (d) reducing the 17&bgr;-hydroxy-17&agr;-methyl-1-oxo-1,2,-seco-A-nor-5&agr;-androstan-2-oic acid to form oxandrolone.

Abstract: Psorospermin and analogs thereof are made using an enantiomerically selective process

Abstract: An androgenic steroid compound of the formula: 1

Abstract: The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.

Abstract: The present invention relates to novel compounds of the naphthopyran type with a fused heterocycle in the 5,6-position. These compounds have formula (I) or (II) given below: These compounds (I) or (II) have valuable photochromic properties. The invention further relates to their preparation, to their applications as photochromic substances, and to the (co)polymer compositions and matrices containing them.

Abstract: The disclosure concerns novel use of diterpene compound as a therapeutic agent of inlfammation, immune disease or cancer. More particularly, the present invention relates to novel use of diterpene compound that include kamebanin, kamebacetal A, kamebakaurin, and exisanin A, which would be effective for the treatnent inflammation, immune disease or cancer by inhibiting the production of nitric oxide, prostaglandin, and TNF-a, through the suppression of NF-k B activity.

Abstract: The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them, their use in the treatment and/or prevention of disorders mediated by one or more estrogen receptors and processes for their preparation. The compounds of the invention are useful in the treatment and/or prevention of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.

Abstract: Novel naphthopyrans having an oxygen-containing heterocyclic group F annelated on the f, i, j, or k side of the naphthopyran ring. These naphthopyrans may have the formula (I) presented below: These compounds (I) have interesting photochromic properties. Various organic host materials that contain such compounds are described. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations are enabled.

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: This invention provides estrogen receptor modulators of formula I, having the structure wherein X, Y1, Y2, Y3, Y4, Z1, Z2, Z3, and Z4 are as defined in the specification, or a pharmaceutically acceptable salt thereof.

Abstract: Psorospermin is a cytotoxic dihydroflranoxanthone that has found to exhibit significant activity against various tumor cell lines. Unfortunately, psorospermin is no longer readily available from its natural plant source. The present invention is directed to a method for preparing psorospermin and psorospermin analogs. Methods are also disclosed for utilizing psorospermin analogs to inhibit cellular proliferation.

Abstract: This invention provides estrogen receptor modulators of formula 1, having the structure 1

Abstract: Compounds, compositions and methods are provided that are useful in the treatment and/or prevention of a condition or disorder mediated by a G-protein coupled receptor. In particular, the compounds of the invention are useful in the treatment and/or prevention of eating disorders, obesity, anxiety disorders and mood disorders.

Abstract: The present invention relates to novel compounds of the naphthopyran type which have an annelated carbocycle in position 5,6.

Abstract: This invention provides estrogen receptor modulators of formula 1, having the structure 1

Abstract: The present invention relates to novel compounds of the naphthopyran type which have a perfluoroalkyl group (X) in position 5. These compounds are of formula (I) given below: These compounds (I) possess interesting photochromic properties. The invention also relates to their preparation, their applications as photochromes as well as the compositions and matrices containing them.

Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxypyrone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.

Abstract: The invention provides a urokinase production inhibitor or angiogenesis inhibitor comprising as an active component an ozonide derivative represented by the formula (1), and method of prevention or therapy using the inhibitor wherein A is an oxygen atom or N—R (wherein R is phenyl or phenyl having as a substituent lower alkyl having 1 to 6 carbon atoms, lower alkoxyl having 1 to 6 carbon atoms or a halogen atom); B is an oxo group or —R4; and (1) when A is an oxygen atom, R1 is a hydrogen atom, etc., R2 is phenyl, etc., R3 is a hydrogen atom, etc., B is an oxo group or —R4, R4 is a hydrogen atom, etc., R5 is a hydrogen atom, etc.; (2) when A is N—R, R1 is a hydrogen atom, etc., R2 is a hydrogen atom, etc., R3 is a hydrogen atom, etc., B is —R4, R4 is a hydrogen atom, etc., R5 is a hydrogen atom, etc.

Abstract: The present invention relates to photochromic 2H-naphtho[1,2-b]pyrans as well as their use in synthetic resins of all types, especially for ophthalmic purposes. In particular, the present invention relates to photochromic naphthopyran compounds, for which a further ring system is bonded to the f side of the naphthopyran. The inventive photochromic dyes generally have the general formula (I) wherein n, R1, R2, R3, X, B and B′ are defined as in claim 1. The inventive compounds are distinguished by good darkening and decolorizing properties and a very good service life.

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: Novel tricyclic compounds of formula I as defined in the specification, a process for their preparation and their use for the preparation of optically active or racemic colchicine and thiocolchicine derivatives.

Abstract: Disclosed are novel cannabinoids which are selective for the CB2 receptor. The novel cannabinoids comprise a substituted or unsubstituted tricyclic cannabinoid core and a substituted or unsubstituted C5-C8 carbocyclic ring, five to eight-membered heterocyclic ring or a seven to ten membered bicyclic ring system fused to the monhydroxylated phenyl ring of the cannabinoid core. Also disclosed are methods of suppressing the immune system in a subject by administering to the subject a (e.g. immunosuppressive amount) effective amount of a novel cannabinoid described above.

Abstract: The present invention provides compounds of formula I and II: ##STR1## wherein X is --O--, --S--, or --NR.sup.5 --;Y is --O--, --S--, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, or --NR.sup.5 --;B is --CH.sup.2 -- or --CO--;R.sup.1, R.sup.2, and R.sup.3 are each independently --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), --OSO.sub.2 CF.sub.3, Cl, or F;n is 1 or 2;W is CH.sub.2 or C.dbd.O;R.sup.4 is 1-piperidinyl, 2-oxo-1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;R.sup.5 is C.sub.1 -C.sub.3 alkyl, --COC.sub.6 H.sub.5, --CO(C.sub.1 -C.sub.6 alkyl), --C(O)OC.sub.6 H.sub.5, --C(O)O(C.sub.1 -C.sub.6 alkyl), --SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --SO.sub.2 C.sub.6 H.sub.5, or --SO.sub.2 CF.sub.3 ;or a pharmaceutically acceptable salt or solvate thereof.

Abstract: A photochromic article that includes a host material and a photochromic amount of a benzopyran compound, the benzopyran compound represented by one of the formulas: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.10 are selected from hydrogen, a stable organic radical, a heterocyclic group, halogen, a nitrogen-substituted group, and a nitrogen-substituted ring compound.

Abstract: The invention concerns novel bi-aromatic dibenzofuran derivatives of formula (I),and their use in pharmaceutical compositions for human or veterinary medicine (skin, rheumatic respiratory, cardiovascular, and ophthalmologic disorders), or in cosmetic compositions as well. The X, Ar, R.sub.1 and R.sub.2 in formula (I) are defined in the specification.

Abstract: A class of benzopyran, derivatives is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I' ##STR1## wherein X, A.sup.1, A.sup.2, A.sup.3, A.sup.4, R, R", R.sup.1 and R.sup.2 are as described in the specification.

Abstract: The compounds of the present invention are those of structural formula (I) ##STR1## wherein X is oxygen or sulfur. Pharmaceutical compositions and methods of use of the compounds in the treatment of hyperandrogenic conditions are disclosed. In addition, the combination of the compounds with other active agents such as finasteride, minoxidil and retinoic acid or a derivative thereof is disclosed.

Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxyprone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.

Abstract: Novel polycyclic ethyl alkylamides of formula I are active as melatonergic agents. ##STR1## wherein Z=CH (when a double bond is present) or (CH.sub.2).sub.n, wherein n is 1-4;X=O, CH.sub.2, or CH (when a double bond is present);R=C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, or C.sub.1-3 haloalkyl, C.sub.2-6 alkenyl, C.sub.2-4 alkoxyalkyl, C.sub.1-4 trifluoromethylalkyl, C.sub.1-6 aminoalkyl; andY=H, C.sub.1-6 alkoxy or halogen.

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: Benzopyran compounds represented by the formulas: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.10 are selected from hydrogen, a stable organic radical, a heterocyclic group, halogen, a nitrogen-substituted group, and a nitrogen-substituted ring compound.

Abstract: Described are novel 7-methylidene-5-oxo-furo fused naphthopyran compounds having certain substituents at the 2 position of the pyran ring. Also described are polymeric organic host materials that contain or that are coated with such compounds.

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: Described are novel pentahydrophenanthro?9,10-b!pyrans and tetrahydrocyclopenta?c!-naphtho?1,2-b!pyrans. Also described are polymeric organic host materials that contain or that are coated with such compounds.

Abstract: The invention discloses novel triterpene derivatives of azadirachtin of the formulae 2 to 11 of the drawings and a process for isolating new triterpene derivatives of azadirachtin from the various parts of the neem plant (Azadirachta indica A-Juss), which process comprises grinding the parts of the neem plant to get a powder, extracting the powder with a binary immiscible solvent consisting of one polar and another non-polar solvent in a ratio of 1:2 to obtain an extract, filtering the extract to get a filtrate having two layers, one layer containing lipids and the other layer containing the new triterpene derivatives of azadirachtin and water soluble constituents including sugars, separating the layers by known methods, concentrating the layer containing the new triterpenes of the formulae 2-11 including derivatives of azadirachtin and water soluble salts, treating the resultant concentrate with a polar solvent and if necessary, warm the concentrate having the solvent, and filtering/decanting the resultant s

Abstract: Novel pharmaceutically/cosmetically-active dibenzofuran compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (II) to (VI): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: Described are novel reversible photochromic naphthopyran compounds, examples of which are 3H-naphtho?2,1-b!pyrans having an acyl or aroyl oxy-bearing substituent at the number 6 carbon atom and certain substituents at the 3-position of the pyran ring. Certain substituents may also be present at the number 5, 7, 8, 9 or 10 carbon atom of the naphthopyran. These compounds may be represented by the following graphic formula: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds. Optically clear articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline)type compounds, are also described.

Abstract: The present invention provides compounds of formula I: ##STR1## wherein X is --O-- or --S--,Y is --O--, --S--, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, or --NR.sup.5 --;R.sup.1, R.sup.2, and R.sup.3 are each independently --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), --OSO.sub.2 CF.sub.3, Cl, or F;n is 1 or 2;W is CH.sub.2 or C.dbd.O;R.sup.4 is 1-piperidinyl, 2-oxo-1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;R.sup.5 is C.sub.1 -C.sub.3 alkyl, --COC.sub.6 H.sub.5, --CO(C.sub.1 -C.sub.6 alkyl), --C(O)OC.sub.6 H.sub.5, --C(O)O(C.sub.1 -C.sub.6 alkyl), --SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --SO.sub.2 C.sub.6 H.sub.5, or --SO.sub.2 CF.sub.3 ;or a pharmaceutically acceptable salt or solvate thereof.

Abstract: The present invention provides a method of synthesizing compounds of formula (I): ##STR1## wherein R.sub.1 and R.sub.3 are independently H or (C.sub.1 -C.sub.4)alkyl--O--;R.sub.2 is R.sub.5 C(O)-- where R.sub.5 is (C.sub.1 -C.sub.4)alkyl or H; andR.sub.4 is H, (C.sub.1 -C.sub.4)alkyl or (C.sub.5 -C.sub.7)aryl optionally substituted with (C.sub.1 -C.sub.4)alkyl or halo.

Abstract: Described are novel reversible photochromic diaryl-3H-naphtho?2,1-b!pyran compounds having a substituted or unsubstituted, five or six member heterocyclic ring fused to the g, i, or l side of the naphthopyran. The heterocyclic ring contains an oxygen or nitrogen atom and is attached to the number 5, 6, 7, 8, 9, or 10 carbon atom of the naphtho portion of the naphthopyran. Also described are organic host materials containing such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline)oxazine-type compounds, are also described.

Abstract: The invention discloses novel triterpene derivatives of azadirachtin of the formulae 2 to 11 of the drawings and a process for isolating new triterpene derivatives of azadirachtin from the various parts of the neem plant(Azadirachta indica A-Juss), which process comprises grinding the parts of the neem plant to get a powder, extracting the powder with a binary immiscible solvent consisting of one polar and another non-polar solvent in a ratio of 1:2 to obtain an extract, filtering the extract to get a filtrate having two layers, one layer containing lipids and the other layer containing the new triterpene derivatives of azadirachtin and water soluble constituents including sugars, separating the layers by known methods, concentrating the layer containing the new triterpenes of the formulae 2-11 including derivatives of azadirachtin and water soluble salts, treating the resultant concentrate with a polar solvent and if necessary, warm the concentrate having the solvent, and filtering/decanting the resultant so

Abstract: Provided are drug/ligand compounds of Formula (I): ##STR1## in which D is a drug moiety;n is an integer from 1 to 10;p is an integer from 1 to 6;Y is O or NH.sub.2.sup.+ Cl.sup.- ;z is 0 or 1;q is about 1 to about 10;X is a ligand; and,A is a Michael Addition Adduct.In a preferred embodiment, the ligand is an immunoglobulin, preferably a chimeric antibody or fragment thereof. Also provided are formulations comprising as an active ingredient a compound of Formula (I), intermediates useful for preparing the compounds of Formula (I), processes for preparing the compounds of Formula (I), and methods for using the compounds of the invention.

Abstract: The invention disclosed novel triterpene derivatives of azadirachtin of the formulae 2 to 11 of the drawings and a process for isolating new triterpene derivatives of azadirachtin from the various parts of the neem plant(Azadirachta indica A-Juss), which process comprises grinding the parts of the neem plant to get a powder, extracting the powder with a binary immiscible solvent consisting of one polar and another non-polar solvent in a ratio of 1:2 to obtain an extract, filtering the extract to get a filtrate having two layers, one layer containing lipids and the other layer containing the new triterpene derivatives of azadirachtin and water soluble constituents including sugars, separating the layers by known methods, concentrating the layer containing the new triterpenes of the formulae 2-11 including derviatives of azadirachtin and water soluble salts, treating the resultant concentrate with a polar solvent and if necessary, warm the concentrate having the solvent, and filtering/decanting the resultant so