Abstract: Invention provides a cheaper and practical protocol for the construction of a wide variety of 1-Amino-2-naphthalene-carboxylic acid derivatives and their structural analogues that proceeds with high yields in a single step via intramolecular cascade cyano ene reaction.

Abstract: Invention provides a cheaper and practical protocol for the construction of a wide variety of 1-Amino-2-naphthalene-carboxylic acid derivatives and their structural analogues that proceeds with high yields in a single step via intramolecular cascade cyano ene reaction.

Abstract: A photoresist composition containing a polymer having a structural unit including an acid-labile group, and a compound represented by the formula (1). In the formula (1), R1 represents a hydrogen atom or a monovalent acid-labile group. R2 represents an alicyclic hydrocarbon group having 3 to 20 carbon atoms and a valency of (m+1). m is an integer of 2 to 5. R3 and R4 each independently represent a hydrogen atom, a fluorine atom, a monovalent hydrocarbon group having 1 to 20 carbon atoms or a monovalent fluorinated hydrocarbon group having 1 to 20 carbon atoms. n is an integer of 0 to 5. At least two of a plurality of R1 s optionally taken together represent a ring structure, together with a plurality of oxygen atoms bonding to R1 and the carbon atom(s) constituting R2 and bonding to these oxygen atoms. M+ represents a monovalent radiation-degradable onium cation.

Abstract: The present invention relates to naphthoquinone derivatives isolated from solid callus cultures from two species of the palaeotropical plant families Dioncophyllaceae and Ancistrocladaceae. It further relates to methods of their production as well as to their use as antiinfective and antitumoral pharmaceuticals.

Abstract: The present disclosure relates to a method for more easily and economically producing a selenophene-fused aromatic compound derivative containing various substituents and the selenophene-fused aromatic compound produced according to the method, and the selenophene-fused aromatic compound can be used for various purposes such as an intermediate of an anti-bacterial or anticancer substance, an indicator of which color is changed depending on a solvent, or a fluorescent substance.

Abstract: The present invention relates to a pharmaceutical composition comprising specific compounds which may be obtained from Leontopodium alpinum Cass. (Edelweiss). A preferred compound is leoligin (=(2S,3R,4R)-4-(3,4-dimethoxybenzyl) -2-(3,4-dimethoxyphenyl)tetrahydrofuran-3-yl]methyl(2Z)-2-methylbut-2-enoat]). Corresponding means and methods in respect of medical uses of the compounds are described. The present invention also provides a medical device comprising, containing or having been contacted with the compound. The compounds provided herein may particularly be used in the treatment of hyperplastic diseases, in particular intimal hyperplasia, e.g. stenosis, restenosis, atherosclerosis and the like. Also envisaged herein is the use of these compounds in the treatment of proliferative diseases, such as leukemia, prostate cancer and lung cancer.

Abstract: The field of the invention relates to stable dosage forms comprising spiro or dispiro 1,2,4-trioxolane antimalarials, or their pharmaceutically acceptable salts, prodrugs and analogues, and processes for their preparation. The water content of the dosage form is not more than 6.5% w/w.

Abstract: The invention relates to a fluorescent dye of general formula I or II wherein R1, R2, R3 and R4 are independently hydrogen or a branched or unbranched, saturated or unsaturated, aliphatic or aromatic, functionally substituted, or unsubstituted hydrocarbon radical, wherein at least one of the R1 or R2 radicals and one of the R3 or R4 radicals is not hydrogen and the R1 and R3 radicals and/or R2 and R4 radicals in formula I can be bridged to each other, and X and Y independently represent a substituted or unsubstituted C1 or C2 hydrocarbon radical wherein any one carbon unit can be replaced by an N or S heteroatom. The dye is remarkable for its high fluorescence intensity and large Stokes shift in combination with a long fluorescence lifetime.

Abstract: A photoacid generator has the formula (I): wherein R1, R2, R3, L1, L2, L3 X, Z+, a, b, c, d, p, q, and r, are defined herein. A photoresist comprises the photoacid generator, and a coated article comprises the photoresist. The photoresist can be used to form an electronic device.

Abstract: The present disclosure is generally directed to compounds that can inhibit DAGL? and/or ? activity, compositions comprising such compounds, and methods for inhibiting DAGL? and/or ? activity.

Abstract: The invention refers to the use of specific cyclolignans, wherein the carbon atoms in positions 9 and 9? have cis configuration, for inhibition of the insulin-like growth factor-1 receptor. Said compounds can be used for treatment of IGF-1R dependent diseases, such as cancer, psoriasis, artherosclerosis and acromegaly. A preferred compound is picropodophyllin.

Abstract: Provided is a polymerizable compound represented by the following general formula (ca-1) or (cb-1): wherein the variables in the formulae are defined in the specification.

Abstract: Disclosed is the use of benzotropolone derivatives of formula (1), wherein R1, R2 and R7 independently from each other are hydrogen; C1-C3alkyl; or COR8; R3 is hydrogen; or COOR9 R4 is hydrogen; or C1-C3alkyl; R5 is hydrogen; hydroxy; C1-C3-alkoxy; or -0-(CO)—R10; R6 is hydrogen; C1-C3alkyl; or COR8; or R5 and R6 together may form a five or six membered ring; or R6 and R7 together form a five or six membered ring; and R8, R9, R10 independently of each other are C1-C30alkyl; for protecting body-care and household products from photolytic and oxidative degradation.

Abstract: Provided is a polymerizable compound represented by the following general formula (ca-1) or (cb-1): wherein the variables in the formulae are defined in the specification.

Abstract: The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures: (Formula (I) or (XXXV)).

Abstract: The invention relates to a fluorescent dye of general formula I or II wherein R1, R2, R3 and R4 are independently hydrogen or a branched or unbranched, saturated or unsaturated, aliphatic or aromatic, functionally substituted, or unsubstituted hydrocarbon radical, wherein at least one of the R1 or R2 radicals and one of the R3 or R4 radicals is not hydrogen and the R1 and R3 radicals and/or R2 and R4 radicals in formula I can be bridged to each other, and X and Y independently represent a substituted or unsubstituted C1 or C2 hydrocarbon radical wherein any one carbon unit can be replaced by an N or S heteroatom. The dye is remarkable for its high fluorescence intensity and large Stokes shift in combination with a long fluorescence lifetime.

Abstract: The present invention is directed to novel sulfamide and sulfamate derivatives, pharmaceutical compositions containing them and their use in the treatment of epilepsy and related disorders.

Abstract: The invention relates 1,2,3,6,7,8-hexahydro-s-indacene derivatives and 6,7-dihydro-5H-indeno[5,6-d]-1,3-dioxole derivatives, and to the use thereof as component(s) in liquid-crystalline media. In addition, the present invention relates to liquid-crystal and electro-optical display elements which contain the liquid-crystalline media according to the invention.

Abstract: The present invention relates to naphthoquinone derivatives isolated from solid callus cultures from two species of the palaeotropical plant families Dioncophyllaceae and Ancistrocladaceae. It further relates to methods of their production as well as to their use as antiinfective and antitumoral pharmaceuticals.

Abstract: Disclosed are (N)-methanocarba adenine nucleosides of the formula: as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias. The invention also provides compounds that are agonists of both A1 and A3 adenosine receptors for use in cardioprotection.

Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families, particularly the activity of PPAR?.

Abstract: The invention relates 1,2,3,6,7,8-hexahydro-s-indacene derivatives and 6,7-dihydro-5H-indeno[5,6-d]-1,3-dioxole derivatives, and to the use thereof as component(s) in liquid-crystalline media. In addition, the present invention relates to liquid-crystal and electro-optical display elements which contain the liquid-crystalline media according to the invention.

Abstract: An indene derivative for selectively modulating the activities of peroxisome proliferator activated receptors (PPARs) having the following formula (I): wherein, R1 is C1-6 alkyl, C1-6 alkenyl, or C3-6 cycloalkyl, each of which is unsubstituted or substituted with one or more phenyl groups; R2 is H, CN, CO2Ra, CH2CO2Ra, CONRbRc, or phenyl; R3 is C1-6 alkyl, C3-6 cycloalkyl, naphthyl, phenyl, being each unsubstituted or substituted with one or more substituents selected from the group consisting of halogen, CN, NH2, NO2, ORa, phenyloxy, C1-6 alkyl, and C3-6 cycloalkyl; and R4, R5, R6, and R7 are each independently H, OH, OSO2CH3, O(CH2)mRe, CH2Rf, OCOCH2ORg, OCH2CH2ORg, OCH2CH?CHRg, or pyridine-2-yloxy, or R5 and R6 together form OCH2O.

Abstract: The invention refers to the use of specific cyclolignans, wherein the carbon atoms in positions 9 and 9? have cis configuration, for inhibition of the insulin-like growth factor-1 receptor. Said compounds can be used for treatment of IGF-1R dependent diseases, such as cancer, psoriasis, atherosclerosis and acromegaly. A preferred compound is picropodophyllin.

Abstract: Novel salicylic anilides are chemical uncouplers useful e.g. for the treatment of obesity.

Abstract: The invention refers to the use of specific cyclolignans, wherein the carbon atoms in positions 9 and 9? have cis configuration, for inhibition of the insulin-like growth factor-1 receptor. Said compounds can be used for treatment of IGF-1R dependent diseases, such as cancer, psoriasis, artherosclerosis and acromegaly. A preferred compound is picropodophyllin.

Abstract: The invention refers to the use of specific cyclolignans, wherein the carbon atoms in positions 9 and 9? have cis configuration, for inhibition of the insulin-like growth factor-1 receptor. Said compounds can be used for treatment of IGF-1R dependent diseases, such as cancer, psoriasis, artherosclerosis and acromegaly. A preferred compound is picropodophyllin.

Abstract: A compound of the formula I in which the moieties R1-R13 are independently selected from the following moieties: R1, R5, R6, R8, R11—H, methyl, ethyl, propyl, isopropyl; R3—H, methyl, ethyl, propyl, isopropyl, vinyl; R4—H, methyl, ethyl; R2, R7, R9—H, methyl, ethyl, propyl, isopropyl, n-butyl, isobutyl, t-butyl; R10—H, methyl, ethyl, propyl, isopropyl, t-butyl; R12, R13—H, C1-6 linear or branched alkyl; or R4 and R11 together with the carbon atoms to which they are attached form a 5- or a 6-membered cycloalkyl ring; or R6 and R7 together with the carbon atoms to which they are attached form a cycloalkyl ring having 3, 4, 5 or 6 members. The compounds have strong odours and are useful in fragrances and fragrance applications.

Abstract: A compound of the formula I in which the moieties R1—R13 are independently selected from the following moieties: R1, R5, R6, R8, R11—H, methyl, ethyl, propyl, isopropyl; R3—H, methyl, ethyl, propyl, isopropyl, vinyl; R4—H, methyl, ethyl; R2, R7, R9—H, methyl, ethyl, propyl, isopropyl, n-butyl, isobutyl, t-butyl; R10—H, methyl, ethyl, propyl, isopropyl, t-butyl; R12, R13—H, C1-6 linear or branched alkyl; or R4 and R11 together with the carbon atoms to which they are attached form a 5- or a 6-membered cycloalkyl ring; or R6 and R7 together with the carbon atoms to which they are attached form a cycloalkyl ring having 3, 4, 5 or 6 members. The compounds have strong odours and are useful in fragrances and fragrance applications.

Abstract: The present invention relates to novel antiviral helioxanthin analogs. These compounds may particularly be used alone or in combination with other drugs for the treatment of the following: hepadnaviruses, flaviviruses, herpesviruses and human immunodeficiency virus. In addition, compounds according to the present invention can be used to prevent or reduce the likelihood of the occurrence of tumors secondary to virus infection as well as other infections or disease states that are secondary to the virus infection.

Abstract: The invention refers to the use of specific cyclolignans, wherein the carbon atoms in positions 9 and 9? have cis configuration, for inhibition of the insulin-like growth factor-1 receptor. Said compounds can be used for treatment of IGF-1R dependent diseases, such as cancer, psoriasis, artherosclerosis and acromegaly. A preferred compound is picropodophyllin.

Abstract: Disclosed is a compound represented by Structural Formula (I): Ar is a substituted or unsubstituted aromatic group. Q is a covalent bond, —CH2— or —CH2CH2—; W is a substituted or unsubstituted alkylene or a substituted or unsubstituted heteroalkylene linking group from two to ten atoms in length, preferably from two to seven atoms in length.

Abstract: The present invention is directed to a one-step process for the preparation of fructopyranose sulfamate derivatives of the general formula (I) wherein X, R1, R3, R4, R5 and R6 are as described in the specification.

Abstract: This invention relates to a novel fused tricyclic heterocycle of the formula (Ia, Ib) and its use for the treatment of hyper-proliferative disorders

Abstract: 1-Deoxybaccatin III, 1-deoxytaxol and 1-deoxy taxol analogs and method for the preparation thereof.

Abstract: The present invention relates to novel oxime carbamyl derivatives and pharmaceutical compositions comprising said derivatives which inhibit fatty acid amide hydrolase. These pharmaceutical compositions are useful for the treatment of conditions which can be effected by inhibiting fatty acid amide hydrolase including, but not limited to, neuropathic pain, emesis, anxiety, altering feeding behaviors, movement disorders, glaucoma, brain injury, and cardiovascular disease.

Abstract: The invention refers to the use of specific cyclolignans, wherein the carbon atoms in positions 9 and 9′ have cis configuration, for inhibition of the insulin-like growth factor-1 receptor. Said compounds can be used for treatment of IGF-IR dependent diseases, such as cancer, psoriasis, artherosclerosis and acromegaly. A preferred compound is picropodophyllin.

Abstract: Embodiments of the invention relate to C2-substituted indan-1-ones and to their physiologically acceptable salts and physiologically functional derivatives. Compounds of embodiments of the invention include compounds of formula I in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable, for example, for use as anorectics.

Abstract: The invention concerns compounds of formula (I): R—A—R′ wherein: A is as defined in the description; R represents a group (V), (VI), (VII) or (VIII), where E, Q, R1, R2, R3, v and R4 are as defined in the description; R′ represents a —(CH2)t—R5 group wherein t and R5 are as defined in the description

Abstract: Etoposide analogs such as 4′-O-demethyl-4&bgr;-[4″-(methyl-L-tyrosine-N-carbonyl)-anilino]-4-desoxy-podophyllotoxin (12) and 4′-O-demethyl-4&bgr;-[4″-(methyl-L-tryptophan-N-carbonyl)-anilino]-4-desoxypodophyllotoxin (13) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.

Abstract: Disclosed is a practical, organic, blue-emitting EL device having a long life and having high luminous efficiency and good thermal stability. The device comprises organic compound layers, of which at least one is an organic blue-emitting layer, as sandwiched between a pair of electrodes, and is characterized in that the organic blue-emitting layer comprises an organic host compound having a fluorescence quantum efficiency of not smaller than 0.3 in a solid state and a fluorescent substance, and the organic host compound and the fluorescent substance are selected such that the device retains a monomeric blue-emitting ability, and that all the organic compound layers have a glass transition temperature of not lower than 75° C., while the organic compound layers adjacent to the organic blue-emitting layer have a glass transition temperature of not lower than 105° C.

Abstract: The present invention provides illudin analogs of the general formula (I): 1

Abstract: Branched, substantially non-antigenic polymers are disclosed. Conjugates prepared with the polymers and biologically active molecules such as proteins and peptides demonstrate extended circulating life in vivo. Substantially fewer sites on the biologically active material are used as attachment sites. Methods of forming the polymer, conjugating the polymers with biologically active moieties and methods of using the conjugates are also disclosed.

Abstract: The present invention provides a compound represented by the formula: wherein R1 is an amino group which may be substituted; R2 is a hydrogen atom or a lower alkyl group which may be substituted; X is a methyne group which may be substituted or N(O)m (m is 0 or 1); a ring A is a homo- or hetero-cycle which is substituted by a halogen atom, lower alkyl, lower alkoxy or lower alkylenedioxy; and a ring B is a homo- or hetero-cycle which may be substituted; or a salt thereof, which exhibits excellent cell differentiation-inducing action and cell differentiation-inducing factor action-enhancing action, and is useful in the treatment and prevention of various nerve diseases or bone/joint diseases.

Abstract: This invention relates to anti-viral drugs such as Helioxanthin and its analogs. The present compounds may be used alone or in combination with other drugs for the treatment of Hepatitis B virus (HBV), Hepatitis C virus (HCV), Yellow Fever, Dengue Virus, Japanese Encephalitis, West Nile virus and related flaviviruses. In addition, compounds according to the present invention can be used to prevent hepatoma secondary to virus infection as well as other infections or disease states which are secondary to the virus infection.

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: The present invention provides an antifeedant and a contact insecticide using the components contained in Cyperaceae species. In particular, the present invention provides an insect antifeedant and a contact insecticide comprising as an active ingredient at least one compound selected from the group consisting of scabequinone, remirol, cyperaquinone and the derivatives thereof.

Abstract: Disclosed are unique starting materials, reaction sequences and intermediate compounds for the preparation of D-3-phosphorylated phosphoinositides (3-PPI) of unambiguous structure and absolute stereochemistry. The enantiomerically pure D-3-phosphorylated phosphoinositides also provided have many uses, including in the development of diagnostics and therapeutics based on the roles of 3-PPI in intracellular signaling.

Abstract: Acyl guanidines are provided which are sodium/proton exchange (NHE) inhibitors which have the structure ##STR1## wherein n is 1 to 5; X is N or C--R.sup.5 wherein R.sup.5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, aryl or heteroaryl; and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, and where X is N, R.sup.1 is preferably aryl or heteroaryl, and are useful as antianginal and cardioprotective agents. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, and arrhythmia employing the above acyl guanidines.

Abstract: Disclosed are unique starting materials, reaction sequences and intermediate compounds for the preparation of D-3-phosphorylated phosphoinositides (3-PPI) of unambiguous structure and absolute stereochemistry. The enantiomerically pure D-3-phosphorylated phosphoinositides also provided have many uses, including the development of diagnostics and therapeutics based on the roles of 3-PPI in intracellular signaling.