Abstract: The present application relates to new taxane analogs, pharmaceutical compositions comprising such analogs and methods of treating cancer comprising such compositions. The compounds according to the present application have the general formula: wherein R1 and R2 are each selected from H, alkyl, alkenyl or aryl; R3 is hydroxyl or OP1; R4 is OH or R7COO; R7 is alkyl, alkenyl or aryl, R8 and R9 are each independently selected from H, alkyl or alkenyl. The compounds of the present application may particularly be 9,10-?,?-OH taxane analogs that are formed by a process starting with a standard taxane as the starting compound.

Abstract: The present application relates to new taxane analogs, pharmaceutical compositions comprising such analogs and methods of treating cancer comprising such compositions. The compounds according to the present application have the general formula: wherein R1 and R2 are each selected from H, alkyl, alkenyl or aryl; R3 is hydroxyl or OP1; R4 is OH or R7COO; R7 is alkyl, alkenyl or aryl, R8 and R9 are each independently selected from H, alkyl or alkenyl. The compounds of the present application may particularly be 9,10-?,?-OH taxane analogs that are formed by a process starting with a standard taxane as the starting compound.

Abstract: The present invention provides fluorogenic probes and corresponding fluorescent compounds, methods of using the probes, compounds and kits that include the probes.

Abstract: The invention relates to chiral compounds of formula I wherein X1,X2,X1,X2,x1,x2,y1,y2,B,C,U1,U2,V1,V2,W1 and W2 have the meaning given in claim 1, to liquid crystal mixtures comprising at least one chiral compound of formula I, to chiral linear or crosslinked liquid crystal polymers obtainable by polymerizing a polymerizade mixture comprising at least one chiral compound of formula I, to the use of chiral compound of formula I and mixtures and polymers obtained thereof in liquid crystal display, active and passive optical elements, adhesives, synthetic resins with anisotropic mechanical properties, cosmetic and pharmaceutical compositions, diagnostics, liquid crystal pigments, for decorative and security applications, nonlinear optics, optical information storage or as chiral dopants, and to a liquid crystal display comprising a mixture comprising at least one chiral compound of formula I.

Abstract: A triterpene derivative useful for the treatment of hepatic disorders is disclosed. This compound comprises as an active ingredient a triterpene derivative represented by the following formula (I) or a salt thereof: wherein R1 represents a hydroxyl group, arylmethyloxy, lower alkoxy, or lower alkanoyloxy, R2 represents lower alkyl, lower alkenyl, —CH2OR5, formyl, —COOR6, or —CH2N(R7)R8, or R1 and R2 may combine with each other to form —O—C(R9)R10—O—CH2—, R3 and R4, which may be the same or different, represent a hydrogen atom, a hydroxyl group, lower alkyl, lower alkenyl, aryl, hydroxymethyl, —N(R11)R12, formyl, —COOR6, or —OR13, or R3 and R4 may combine with each other to form oxo, hydroxyimino, or alkylidene and X represents O, CH2, or NH.

Abstract: The invention relates to a method for the synthesis of galanthamifle, the derivatives and analogues thereof of formula (1) where R1=a hydrogen atom.

Abstract: Compounds of the general formula (I) are described: wherein each of R1, R2, R3, R4, R5 and R6 independently represents a substituent selected from the group consisting of hydrogen, methyl, ethyl, n-propyl, and isopropyl; an wherein x represents either 0 or 1. The compounds are useful as fragrances and as added components in fragrance blends. Methods of improving the harmony, emanation, naturalness an staying power of other fragrance ingredients by the addition of such compounds are also described.

Abstract: Benzodioxino-naphtho[1,2-b]pyran compounds having particularly advantageous photochromic properties, such as, high sensitivity/coloration, two distinct absorption bands in the 430-500 nm range and 520-620 nm range of the visible spectrum may be generally described as a naphthopyran having a central nucleus of the formula: wherein F is a 1,4-benzodioxine ring with its 2,3 positions fused to the i, j, or k faces; and R1 and R2 are the atoms or groups providing photochromic properties to the naphthopyran.

Abstract: The present invention pertains, at least in part, to novel 7-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

Abstract: This invention comprises compositions containing dihydroartemisinin and dihydroartemisitene dimers with activity as anticancer agents and anti-protozal, including anti-malarial and anti-leishmanial properties. This invention also describes methods of preparation of these compositions and methods of use of such compositions for the treatment of cancer, and protozoal infections, including malaria, or leishmaniasis. The compounds of this invention represent a potential new class of anti-tumor agents, one that has shown promising activity against solid tumors, and with a pattern of selectivity that suggests a possible new mechanism of action.

Abstract: The present invention relates to an epoxy resin composition a cure article thereof, a novel epoxy resin used therein, a polyhydric phenol compound suited for used as an intermediate thereof, and a process for preparing the same. One of the objects to be achieved by the present invention is to exert the heat resistance, the moisture resistance, the dielectric performances and the flame-resistant effect required of electric or electronic materials such as semiconductor encapsulating materials and varnishes for circuit boards in the epoxy resin composition.

Abstract: The present invention pertains, at least in part, to novel substituted 4-dedimethylamino tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

Abstract: Compounds of the Formula I: 1

Abstract: The present invention provides a novel dioxin analogue for use in the search for organisms capable of degrading dioxin.

Abstract: The present invention of compounds of formula (I) 1

Abstract: Certain multi-substituted dibenzylidene sorbitol acetals having electron withdrawing groups as constituents and electron donating groups on the other such that the compounds are asymmetric in structure and are dipolar in nature are provided. Polymer compositions comprising such compounds, are also contemplated which may be utilized within, as merely examples, food or cosmetic containers and packaging. These inventive asymmetric dipolar dibenzylidene sorbitol acetals are also useful as gelling agents for water and organic solvents, particularly those used in the preparation of antiperspirant gel sticks.

Abstract: Novel naphthopyrans having an oxygen-containing heterocyclic group F annelated on the f, i, j, or k side of the naphthopyran ring.

Abstract: This invention provides estrogen receptor modulators of formula 1, 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: Couplers for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein R is selected from the group consisting of C1 to C2 alkyl and hydroxyethyl; R1 is selected from the group consisting of a hydrogen, hydroxy, nitro, halogen, C1 to C5 alkyl or haloalkyl, C1 to C5 alkoxy or cycloalkoxy, C1 to C5 hydroxyalkyl and C1 to C5 hydroxyalkoxy; Ar is an aromatic group, preferably an aromatic group selected from the group consisting of a furyl, thienyl, pyridyl, phenyl, 2,3-dihydro-benzo[1,4]dioxin-5 or -6-yl or benzo[1,3]dioxol-4 or -5-yl group; and y=1 to 3.

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 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: The present invention is directed to tetrahydronaphthalene derivatives of &agr;-conindendrin, &bgr;-conindendrin, sikkimotoxin, and podophyllotoxin having at least one methyleneoxy bridge wherein the oxygen atom extends to the benzhydrylic carbon atom.

Abstract: Novel tetracyclic aromatic ketones are natural product compounds useful in the inhibition of HIV integrase, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. Further, the novel fungal cultures MF6388 (ATCC 74478), Sterile Fungus, and MF6591 (ATCC 74477), Ascochyta sp. are also disclosed. Further, the cultures Sterile Fungus MF6388 (ATCC 74478) and Ascochyta sp. MF6591 (ATCC 74477) are also disclosed, as well as processes for making compounds of the present invention employing the cultures.

Abstract: The compounds of Formula I are useful as immunosuppressive agents.

Abstract: An industrial method for preparation of a 1,4-benzodioxane derivative (1), which comprises reacting a diol compound (2) with a carbonating agent to prepare a carbonate compound (3) and after removal of the protective group, cyclizing it by heating or by treating with a base or a fluoride salt.

Abstract: The present invention relates to a class of 1,4-dihydrodioxin masked quinone compounds which are useful as DNA or RNA cleaving reagents. These compounds may additionally include moieties which target the compounds to specific base sequences on the DNA or RNA molecule to permit site-specific cleavage. The process for using these compounds in a UV or short wavelength visible light-activated reaction for cleaving DNA, as well as pharmaceutical compositions containing these compounds, are also disclosed.

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: A compound of formula (I): ##STR1## in which R.sup.1, R.sup.2, X and Y are as defined in the description, the isomers thereof and the addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same are useful in the treatment of certain cancers.

Abstract: The present invention provides methods for making a novel class of 1-deoxy paclitaxel derivatives. These derivatives include 1-deoxy paclitaxel. The derivatives of the present invention are potent cytotoxic agents.

Abstract: This invention relates to the compounds represented by general formula (I) and the processes for their preparation, wherein R is selected from C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.6 cycloalkyl, phenyl unsubstituted or substituted by a halogen atom or nitro group, biphenyl unsubstituted by a halogen atom or nitro group, naphthyl unsubstituted or substituted by a halogen atom or nitro group. The compounds of this invention are used to prepare agents for prevention and treatment of AIDS and drugs against malaria and toxoplasmosis.

Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.

Abstract: Disclosed herein are new anthracyclines which are derived from conjugation with glutathione, for example from conjugation of adriamycin, daunomycin and menogaril with glutathione: compounds 7 I, 7 II, 8 I, 8 II, 9 I and 9II, are obtained by reduction of the anthracycline followed by reaction of the reduced product with glutathione in aqueous (H.sub.2 O or D.sub.2 O) or organic solvent. The invention also provides salts of these glutathione derivatives, particularly salts formed from anthracycline glutathione anions with anthracycline cations. These anthracycline derivatives are useful as antibiotics, as antitumor agents, and in the treatment of AIDS. These derivatives are particularly useful in the treatment of cancer when multiple drug resistance is present.

Abstract: A production stimulator of nerve growth factor contains a new cyathane derivative of the form ##STR1## where R is either CHO or CH.sub.2 OH.

Abstract: Novel podophyllotoxin compounds and their use in treating tumors are disclosed. The analogs have the general formula: ##STR1## wherein NH--R is a selected aryl amine, dialkylaminoalkyleneamino, or dialkylaminoanilino group.

Abstract: Compounds represented by the general formula (I): ##STR1## (where R.sub.1 is an admantyl group; R.sub.2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or an aralkyl group; R.sub.3 is a 1,4-benzodioxane ring that may optionally have 1-4 substituents selected from among a lower alkyl group, a lower alkoxy group, a halogen atom, an amino group, a hydroxyl group and a lower alkylcarbonyl group; n is an integer of 1-4) or a salt thereof. These compounds have both antianxiety and antidepressant actions and yet they cause less side effects. Therefore, they can be used as excellent drugs that are highly effective in the prevention and treatment of various diseases such as neurosis. psychosomatic diseases, autonomic imbalance and depression.

Abstract: New cyathane derivatives shown by Formula (1) or (2) given below have the effect of stimulating production of nerve growth factors and antimicrobial effects: ##STR1## where R is either CHO or CH.sub.2 OH.

Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.

Abstract: Herein disclosed are an antibacterial substance: BE-24566B represented by the following structural formula (I): ##STR1## or a pharmaceutically acceptable salt thereof; and an antibacterial agent comprising, as an essential component, the foregoing antibacterial substance: BE-24566B or a pharmaceutically acceptable salt thereof. The antibacterial substance BE-24566B or pharmaceutically acceptable salts thereof can be prepared according to a method comprising the steps of inoculating an antibacterial substance: BE-24566B-producing microorganism or a variant thereof into a culture medium to cultivate the microorganism or variant, in particular the strain FERM BP-3994 or a variant thereof, and isolating the intracellularly and/or extracellularly produced antibacterial substance.

Abstract: Isolation of a new taxane having pharmaceutical activity, 1a 14-beta-hydroxy-10-deacetyl-baccatine III and hemisynthesis of some derivatives useful as antitumor agents and intermediates.

Abstract: A process for synthesizing polyoxa tetracyclics which involves the ozonolysis of a single-ring-structure vinyl silane with resulting direct formation of the desired multiple ring material. The polyoxa tetracyclic compounds have the formula ##STR1## The vinyl silanes have the structure ##STR2## The vinyl silanes are new chemical compounds as are corresponding primary ozonide and dioxetane intermediates. In a preferred embodiment, this invention provides a total synthesis of the antimalarial artemisinin.

Abstract: An asymmetric process for the preparation of enantiomerically pure .beta.-D-(-)-dioxolane-nucleosides. The enantiomerically pure dioxolane nucleosides are active HIV agents, that are significantly more effective than the prior prepared racemic mixtures of the nucleosides. The anti-viral activity of the compounds is surprising in light of the generally accepted theory that moieties in the endo conformation, including these dioxolanes, are not effective antiviral agents. The toxicity of the enantiomerically pure dioxolane nucleosides is lower that that of the racemic mixture of the nucleosides, because the nonnaturally occurring .alpha.-isomer is not included.The product can be used as a research tool to study the inhibition of HIV in vitro or can be administered in a pharmaceutical composition to inhibit the growth of HIV in vivo.

Abstract: Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.

Abstract: The invention concerns novel pharmaceutical compositions for use in the treatment of certain complications of diabetes and galactosemia and which contain a nitromethane derivative (or its non-toxic salt) as active ingredient. The nitromethane derivatives are inhibitors of the enzyme aldose reductase. Many of the inhibitors are novel and are provided, together with processes for their manufacture and use, as further features of the invention.

Abstract: Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.

Abstract: Compounds that are analogs of etoposide and exhibit antitumor activity are disclosed. The compounds of the present invention have the following formula: ##STR1## where: R.sub.1 is .beta.-OCH.sub.2 CH.sub.2 NH.sub.2 .beta.-NHCH(CH.sub.3)CH.sub.2 OH, .beta.-NHCH.sub.2 CH(CH.sub.3)OH, .beta.-Cl, .beta.-Br, .beta.-OH, .alpha.-OH, .beta.-NH, .alpha.-NH.sub.2, .beta.-NHCH.sub.2 CH.sub.2 OH, .alpha.-NHCH.sub.2 CH.sub.2 OH, .beta.-NHCH.sub.2 CH.sub.2 CH.sub.3, .beta.-NHCH.sub.2 CH.sub.2 OCH.sub.3, .beta.-NHCH.sub.2 CH.dbd.CH.sub.2, .beta.-NHCH.sub.2 CH(OH)CH.sub.3, .beta.-NHCH.sub.2 CH.sub.2 CH.sub.2 OH, .beta.-OCH.sub.2 CH.sub.2 OH, ##STR2## R.sub.2 is H, or Br; R.sub.1 is H, or Br;R.sub.4 is H, or Br;R.sub.5 is H, or Br; andR.sub.6 is H, or --CH.sub.3.

Abstract: Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.

Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salt thereof, wherein R.sup.2 is selected from hydroxy and lower alkoxy, R.sup.5 is lower alkyl, and R.sup.11 and R.sup.12 are independently selected from hydrogen, halo, hydroxy, methoxy, and lower alkyl, are selective .alpha..sub.2 adrenergic receptor antagonists useful in the treatment of glaucoma.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: This invention provides the 4-mono-anion of myo-inositol orthoformate, and describes a process for preparing this anion as well as the use of this anion in the preparation of a variety of mono- and poly-phosphate derivatives of myo-inositol.

Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.