Abstract: The Invention relates to novel ketones of formulae (I) and (II) wherein R1, R2, R3 and R4 are, for example, C1-C8alkyl, R5 is, for example, hydrogen, A is CI, Br, -0-R7, —NR8R9 or —S—R16, A? is —O—, —NH— or —NR8—, X and Y are each independently of the other —O—R10 or —N(R11)(R12), n is an integer from 1 to 10, R6 is, for example, an n-valent radical of linear or branched C2-C20alkyl the carbon chain of which may be interrupted by cyclohexanediyl, phenylene, —CH(OH)—, —C(C2H5)(CH2—CH2—OH)—, —C(CH3)(CH2—CH2—OH)—, —C(CH2—CH2—OH)2—, —N(CH3)—, —N(C2H5)—, —N(CH2—CH2—OH)—, —CO—O—, —O—CO—, —P(CH2—CH2—OH)—, —P(O)(CH2—CH2—OH)—, -0-P(O—CH2—CH2—OH)—O—, -0-P(O)(0-CH2—CH2—OH)—O—, —O-cyclohexanediyl-C(CH3)2-Cyclohexanediyl-O—, —O-phenylene-C(CH3)2-phenylene-O—, —O-phenylene-CH2-phenylene-O—, —Si(CH3)2—, -0-Si(CH3)2—O—, —O—Si(CH3)(0-CH3)—O—, —Si(CH3)(R17)—O—Si(CH3)(R18)—, 5-(2-hydroxyethyl)-[1,3,5]triazinane-2,4,6-trione-1,3-diyl and/or by from one to nine oxygen atoms.

Abstract: The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.

Abstract: Compounds represented by the following structural formulas can be used as photoacid generators: Such compounds are useful, for example, in fabricating arrays of polymers.

Abstract: A pyridazine compound represented by the formula (1): has an excellent plant disease controlling activity.

Abstract: Process for the preparation of enantiomerically enriched compounds of formula Ar—C(R1)—C(R2)-Z wherein Ar represents an optionally substituted (hetero)aryl group R1 and R2, each independently, represent H, an alkyl, (hetero)aryl, dialkylamino, amido, thioether, alkoxy or aryloxy group with the proviso that not both R1 and R2 represent H, or R1 and R2 form together with the C-atoms to which they are bound a (hetero)alkyl or (hetero)alkenyl ring and Z represents an electron withdrawing group, in which process a boronic acid derivate of formula Ar—B(OR3)OR4 or its anhydride, wherein R3 and R4, each independently, represent H or an alkyl group, is reacted with an olefinic unsaturated compound of formula R2—C?C—(R1)Z in the presence of a transition metal catalyst comprising a transition metal chosen from Cu and group VIII and an enantiomerically enriched ligand L, having formula (I) where Cn together with the two O-atoms and the P-atom forms a substituted or nonsubstituted ring with 2-6 C-atoms, R5 and R6 each ind

Abstract: These are described biphenylene compounds of formula (I) wherein R1 is a C1-C18alkyl, C2-C18alkenyl, C6-C10aryl or C6-C10aryl or C6-C10heteroaryl radical each unsubstituted or mono- or poly-substituted by hydroxy, halogen, C1-C18alkyl, C1-C18alkoxy, amino, C1-C5monoalkyamino or by di-C1-C5alkylamino; C5-C7cycloalkyl or C5-C7cycloalkenyl each unsubstituted or substituted by C1-C5alkyl; —OR?; or NR?R?; R2 is a C1-C18alkyl, C2-C18alkenyl, C6-C10aryl or C6-C10heteroaryl radical each unsubstituted or mono- poly-substituted by hydroxy, hadroxy, C1-C18alkoxy, amino, C1-C5monoalkylamino or by di-C1-C5alkylamino; —OR?; —NR?R?; or R1 and R2 together form a 5- to 7- membered monocyclic carbocyclic or heterocyclic ring; R3 is hydrogen; C1-C6alkyl or C1-C6alkoxy; R? and R? are each independently of the other hydrogen; unsubstituted or mono- or poly-hydroxy-, halo-, C1-C18alkyl-, C1-C18alkoxy-, amino- or quaternary ammonium groupsubstituted C1-C18alkyl, C5-C7cycloalkyl or phenyl; and n is 0 or 1; wherein, when R2 is OR? or

Abstract: The present invention relates to chalcone and chalcone derivatives and analogs which are useful as angiogenesis inhibitors. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good activity as angiogenesis inhibitors. The present invention also relates to the use of chalcone and its analogs as antitumor/anticancer agents and to treat a number of conditions or disease states in which angiogenesis is a factor, including angiongenic skin diseases such as psoriasis, acne, rosacea, warts, eczema, hemangiomas, lymphangiogenesis, among numerous others, as well as chronic inflammatory disease such as arthritis.

Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Pagets disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

Abstract: Analogs of combretastatin have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin polymerization. Such compounds are excellent clinical candidates for the treatment of cancer in humans. In addition, certain of these ligands, as pro-drugs, may well prove to be tumor selective vascular targeting chemotherapeutic agents or to have vascular targeting activity resulting in the selective prevention and/or destruction of nonmalignant proliferating vasculature.

Abstract: The present invention has its object to provide a specific compound derived from a naturally occurring substance, and a composition for the prevention and/or treatment of metabolic syndrome and insulin resistance syndrome which comprises that as an active ingredient, easily and efficiently. The present invention relates to a composition for the prevention and/or treatment of metabolic syndrome and a composition for the prevention and/or treatment of insulin resistance syndrome, each of which comprises, as an active ingredient, at least one compound selected from among the compound represented by the formula (1), compounds represented by the formula (4) and compounds represented by the formula (5), or a salt or ester thereof.

Abstract: In this patent we describe the purification of prenylated benzophenones from the fruit rinds of Garcinia species and its evaluation as an inhibitor for Histone acetyltransferases p300 and PCAF. We have found that prenylated benzophenones are potent HAT inhibitors of p300 (IC50-1 ?M) and pCAF (IC50-15 ?M). The inhibitors significantly repress the p300 HAT dependent transcriptional activation from in vitro assembled chromatin template but had no effect on transcription from DNA. These results suggest that the compounds could be specific to HATs. Thus these compounds should be useful as biological switching molecule for evaluating the role of p300 and PCAF in cellular functions and may be useful as new chemical entities for the development of anticancer drugs.

Abstract: The present invention relates to compounds capable of acting as androgen receptor antagonists, pharmaceutical formulations containing the same, and methods of use thereof. Such uses include, but are not limited to, use as antitumor agents, particularly for the treatment of cancers such as colon, skin and prostate cancer and to induce androgen receptor antagonist activity in a subject afflicted with an androgen-related affliction. Examples of androgen-related afflictions include, but are not limited to, baldness, hirsutism, behavioral disorders, acne, and uninhibited spermatogenesis wherein inhibition of spermatogenesis is so desired.

Abstract: The present invention relates to compounds capable of acting as androgen receptor antagonists, pharmaceutical formulations containing the same, and methods of use thereof. Such uses include, but are not limited to, use as antitumor agents, particularly for the treatment of cancers such as colon, skin and prostate cancer and to induce androgen receptor antagonist activity in a subject afflicted with an androgen-related affliction. Examples of androgen-related afflictions include, but are not limited to, baldness, hirsutism, behavioral disorders, acne, and uninhibited spermatogenesis wherein inhibition of spermatogenesis is so desired.

Abstract: This invention relates to the compositions and processes for preparing 2,3,3?,4?-tetramethylbenzophenone and asymmetrical dianhydrides such as 2,3,3?,4? benzophenone dianhydride (a-BTDA), and 3,4?-(hexafluoroisopropylidene)diphthalic anhydride (a-6FDA). a-BTDA is prepared by Suzuki coupling with catalysts from a mixed anhydride of 3,4-dimethylbenzoic acid and 2,3-dimethylbenzoic acid with a respective 2,3-dimethylphenylboronic acid and 3,4-dimethyl phenylboronic acid to form 2,3,3?,4?-tetramethylbenzophenone which is oxidized to 2,3,3?,4?-benzophenonetetracarboxylic acid followed by cyclodehydration to obtain a-BTDA. The a-6FDA was prepared by nucleophilic trifluoromethylation of 2,3,3?,4?-tetramethylbenzophenone with trifluoromethyltrimethylsilane to form 3,4?-(trifluoromethylmethanol) bis(o-xylene) which is converted to 3,4?-(hexafluoroisopropylidene-bis(o-xylene). The 3,4?-(hexafluoroisopropylidene)-bis(o-xylene) is oxidized to the corresponding tetraacid followed by cyclodehydration to yield a-6FDA.

Abstract: The present invention relates to compounds capable of acting as androgen receptor antagonists, pharmaceutical formulations containing the same, and methods of use thereof. Such uses include, but are not limited to, use as antitumor agents, particularly for the treatment of cancers such as colon, skin and prostate cancer and to induce androgen receptor antagonist activity in a subject afflicted with an androgen-related affliction. Examples of androgen-related afflictions include, but are not limited to, baldness, hirsutism, behavioral disorders, acne, and uninhibited spermatogenesis wherein inhibition of spermatogenesis is so desired.

Abstract: The present invention relates to improved methods for achieving the synthesis of 1,7-diaryl-1,6-heptadiene-3,5-diones, and in particular curcumin and its analogues. The invention provides a process for synthesizing such compounds in substantial yield and purity using environmentally benign processes and materials. The invention also relates to the use of such synthesized products in the treatment of Alzheimer's Disease and other diseases.

Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget's disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, age-related mild cognitive impairment, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, irritable bowel syndrome, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.

Abstract: It has been discovered certain 1,3-bis-(substituted-phenyl)-2-propen-1-ones, including compounds of formula (I) inhibit the expression of VCAM-1, and thus can be used to treat a patient with a disorder mediated by VCAM-1. Examples of inflammatory disorders that are mediated by VCAM-1 include, but are not limited to arthritis, asthma, dermatitis, cystic fibrosis, post transplantation late and chronic solid organ rejection, multiple sclerosis, systemic lupus erythematosis, inflammatory bowel diseases, autoimmune diabetes, diabetic retinopathy, rhinitis, ischemia-reperfusion injury, post-angioplasty restenosis, chronic obstructive pulmonary disease (COPD), glomerulonephritis, Graves disease, gastrointestinal allergies, conjunctivitis, atherosclerosis, coronary artery disease, angina and small artery disease.

Abstract: The invention relates to 1,2-substituted 2,3-dihydro-1H-5,9-dioxacyclohepta[f]inden-7-ones and 7-substituted benzo[b][1,4]dioxepin-3-ones and to the use of these compounds in fragrance compositions.

Abstract: The present invention provides a fragrance precursor of formula I: that is capable of forming a fragrant ketone of formula II: and a fragrant lactone of formula III:

Abstract: The present invention relates to chalcone and chalcone derivatives and analogs which are useful as angiogenesis inhibitors. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good activity as angiogenesis inhibitors. The present invention also relates to the use of chalcone and its analogs as antitumor/anticancer agents and to treat a number of conditions or disease states in which angiogenesis is a factor, including angiongenic skin diseases such as psoriasis, acne, rosacea, warts, eczema, hemangiomas, lymphangiogenesis, among numerous others, as well as chronic inflammatory disease such as arthritis.

Abstract: The invention provides methods for treating beta-Amyloid protein-induced disease, pharmaceutical compositions and compounds useful for the same, and the use of these compounds for the manufacture of a medicament for treating the same. More particularly, the invention relates to the use of natural product compounds isolated from turmeric, gingko biloba, and ginger, and synthetic chemical analogues thereof, for the treatment of a beta-Amyloid protein-induced disease.

Abstract: The present invention is directed to a convenient method of synthesizing radiolabeled ?-trifluoromethyl ketones by a fluorination reaction. The present invention also relates to imaging agents and markers for identifying cell proliferation, or viral infection. The markers and imaging agents including the radiolabeled ?-trifluoromethyl ketones that are prepared by the present method.

Abstract: A process for the purification of 1,3-diketones comprising reacting a 1,3-diketone with an earth metal or alkaline earth metal complexing agent in an organic solvent, isolating, washing and decomposing the resulting complex, and isolating the purified 1,3-diketone.

Abstract: The present invention relates to compounds capable of acting as androgen receptor antagonists, pharmaceutical formulations containing the same, and methods of use thereof. Such uses include, but are not limited to, use as antitumor agents, particularly for the treatment of cancers such as colon, skin and prostate cancer and to induce androgen receptor antagonist activity in a subject afflicted with an androgen-related affliction. Examples of androgen-related afflictions include, but are not limited to, baldness, hirsutism, behavioral disorders, acne, and uninhibited spermatogenesis wherein inhibition of spermatogenesis is so desired.

Abstract: &bgr;-diketone fluorescent tags are disclosed, particularly those enabling the use of excitation energy in the near visible or visible spectrum. In some cases, these tags allow the use of cost-effective excitation devices such as LED's. The compounds form fluorescent chelates (complexes) with lanthanide (III) rare earth metal ions (such as Eu3+). The fluorescent complex may be included in a latex microparticle, such as a styrene latex particle. Ideally, the complex has an absorption maximum &lgr; equal to or greater than 360 nm, and the compound is characterized by a pKa<9.0. Kits and methods for detecting target molecules (e.g. immunoassays) are also disclosed. Such methods and kits typically use a ligand for binding to the target molecule and a labeling agent attached to the ligand. The fluorescent complexes described above are at least part of the labeling agent.

Abstract: A process for the purification of 1,3-diketones comprising reacting a 1,3-diketone with an earth metal or alkaline earth metal complexing agent in an organic solvent, isolating, washing and decomposing the resulting complex, and isolating the purified 1,3-diketone.

Abstract: A method for prevention or treating myocarditis, dilated cardiomyopathy and heart failure comprising administering to a patient in need of such treatment a NF-&kgr;B inhibitor in a therapeutically effective amount, wherein said NF-&kgr;B inhibitor is a benzoquinone derivative represented by the following formula (I): wherein R1, R2 and R3 are each independently a hydrogen atom, an alkyl group having 1 to 5 carbons or an alkoxy group having 1 to 5 carbons; R4 is a hydrogen atom, a hydroxymethyl group, an alkyl group, or a carboxyl group which is optionally esterified or amidated; Z is and n is an integer from 0 to 6, or its hydroquinone form, or a pharmaceutically acceptable salt thereof, is provided.

Abstract: Novel chromene compounds having various substituents to exhibit a high color-developing sensitivity and a high density even when dispersed in a high-molecular matrix, and exhibiting a large fading rate, less color when deteriorated, and excellent light resistance in the photochromic properties; photochromic materials containing the chromene compounds; and use thereof.

Abstract: This invention relates to novel polyhydroxy curcumins of the formula (I), wherein R and R1 may be same or different and are selected from H, OH and OCH3. This invention also includes a process for synthesising the above polyhydroxy curcumins by reacting substituted aromatic alhehydes with a diketone in the presence of boron oxide, alkyl borate and a primary or secondary amine catalyst. If desired, the resulting compounds can be deprotected by known means. These compounds are used as anti-oxidants.

Abstract: The present invention relates to compounds capable of acting as androgen receptor antagonists, pharmaceutical formulations containing the same, and methods of use thereof. Such uses include, but are not limited to, use as antitumor agents, particularly for the treatment of cancers such as colon, skin and prostate cancer and to induce androgen receptor antagonist activity in a subject afflicted with an androgen-related affliction. Examples of androgen-related afflictions include, but are not limited to, baldness, hirsutism, behavioral disorders, acne, and uninhibited spermatogenesis wherein inhibition of spermatogenesis is so desired.

Abstract: A &ohgr;-cycloalkyl-prostaglandin E2 derivatives of the formula (I) 1

Abstract: Compounds that inhibit 5-alpha-reductase are provided. The compounds are used to treat prostate cancer, breast cancer, obesity, skin disorders and baldness.

Abstract: Benzylidene cyclohexanone, cyclopentanone and acteone derivatives and therapeutic methods of using same are disclosed. The compounds are non-toxic and exhibit potent anti-inflammatory, antibacterial and antioxidation activity. Also, certain compounds of the invention inhibit glutathione S-transferase (“GST”), but do not irritate the gastrointestinal tract. Pharmaceutical compositions containing the compounds of the invention and pharmaceutically acceptable carriers are also disclosed.

Abstract: The present invention relates to polyalkylene oxide porogens having hyper-branches and low dielectric-constant insulators using them. More particularly, the present invention relates to polyalkylene oxide porogens having hyper-branches expressed by the following formula (1), where the polyalkylene oxide porogen has a center molecular (D) having branches (W), and low dielectric-constant insulators having nanopores prepared by coating a mixture of the porogen and a high heat-resistant resin such as polysilsesquioxane and thermal treating the coated substrate at a temperature effective to degrade the porogen.

Abstract: The present invention relates to novel bisbenzophenones and the use thereof as an ultraviolet light absorber. The presently claimed compounds are particularly useful, either alone or in combination with other additives, including other ultraviolet light absorbers, antioxidants and stabilizers, in stabilizing polymers and other materials from degradation by environmental forces such as actinic radiation (ultraviolet light), oxidation, moisture, atmospheric pollutants and combinations thereof.

Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula 1

Abstract: Compositions and methods are provided for prevention and treatment of cancer. The compositions comprise pure hydroxylated chalcone compounds of licorice root (Glycyrrhiza glabra) including 1-propanone-1-(2,4-dihydroxyphenyl)-3-hydroxy-3-(4′-hydroxyphenyl).

Abstract: Inhibitors of the cytosolic phospholipase A2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases. The inhibitors of the present invention have the general formula where X, Z, R1, R2, R3, R4, Ra and Rb are as defined in the specification.

Abstract: The polymerizable compound of this invention is represented by general formula (I): where R is H, R′, R′O, R′COO, or R′OCO, R′ is a linear or branched alkyl group or alkenyl group having 1 to about 15 carbon atoms, A1 and A2 are independently a cyclohexane ring or a benzene ring which may include a substituent represented by formula (II) below; X is H or CH3; and Y1, Y2, Y3, and Y4 are independently H, F, Cl, CH3, CH3O, CF3, or CF3O wherein at least two of Y1, Y2, Y3, and Y4 are H and, if both A1 and A2 are cyclohexane rings, at least one of Y1, Y2, Y3, and Y4 is not H: where Y5, Y6, Y7, and Y8 are independently H, F, Cl, CH3, CH3O, CF3, or CF3O, at least two of Y5, Y6, Y7, and Y8 are H.

Abstract: This invention provides an improved process for cis-1-{2-[4-(6-methoxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenoxy]ethyl}pyrrolidine which is an intermediate for the preparation of (−)cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol which is useful for the treatment of osteoporosis.

Abstract: 2-Benzyloxyalkyl halophenones of the formula (3): wherein X1 and X2 are each independently H, Cl or F, provided that at least one of X1 and X2 is Cl or F; one of R3 and R4 is H and the other is optionally substituted benzyloxy; and R5 is an unsubstituted alkyl, preferably a C1-6 alkyl group. The compounds are useful as intermediates for preparing 2-hydroxyalkyl halophenones.

Abstract: Process for the oxidation of substrates containing methyl, methylene or methine groups by cooxidation with an aldehyde as cosubstrate in the presence of a catalyst system consisting of an imide compound and a metal cocatalyst.

Abstract: There is provided a process for the prepartion of 2,2-dimethyl-5-(4-chlorobenzyl)cyclopentanone 1

Abstract: Novel dephenylethylene compounds that are administered orally to decrease circulating concentrations of glucose are provided. The effect on insulin resistant rats is also shown. The effects on lipid and leptin concentrations are also shown. The compounds are orally effective anti-diabetic agents that may normalize glucose and lipid metabolism in subjects with diabetes.

Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula 1

Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula (T)xA—B—D—E—G wherein A is an aryl or heteroaryl rings; B is an aryl or heteroaryl ring or a bond; each T is a substituent group; x is 0, 1, or 2; the group D represents the group E represents a two or three carbon chain bearing one to three substituent groups which are independent or are involved in ring formation, possible structures being shown in the text and claims; and the group G represents and with the proviso that when G is each of the substituents on E is an independent substituent; and include pharmaceutically acceptable salts thereof.

Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula 1

Abstract: The invention discloses ketones of formula I: wherein, Y is an optionally substituted alkyl, cycloalkyl, or cycloalkylalkyl, wherein each alkyl group is straight or branched and each alkyl and cycloalkyl group is saturated or unsaturated; R1 is hydrogen or a C1-6 alkyl group that is substituted, saturated or unsaturated, straight or branched; A is a chromophoric substituted aromatic ring or ring system; n is an integer; and with the proviso that formula I is not 2-ethoxy-1-phenyl-ethanone. These compositions are useful for the delivery of organoleptic compounds, especially of flavors, fragrances, masking agents and antimicrobial compounds.

Abstract: A series of aryl piperazine compounds of the formula: or the pharmaceutically acceptable salts thereof, are effective pharmaceuticals for the treatment of conditions related to or affected by the serotonin 1A receptor; the compounds are particularly effective antagonists at that receptor, and are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal.