Abstract: A 4-desoxy-4-epipodophyllotoxin derivative of the following formula ##STR1## wherein R and R.sub.1 are as defined in the specification or a pharmaceutically acceptable salt thereof as well as an antitumor composition comprising such derivative or salt as an active ingredient.

Abstract: A 4-desoxy-4-epipodophyllotoxin derivative of the following formula ##STR1## wherein R and R.sub.1 are as defined in the specification or a pharmaceutically acceptable salt thereof as well as an antitumor composition comprising such derivative or salt as an active ingredient.

Abstract: Conjugate of general formula 1:[A--O--W-Z].sub.a -T 1wherein the moity A--O--is the residue of drug of formula A--O--H in which --O--H is a primary or secondary hydroxyl group; a is an integer of from 1 to 30; W is a group of general formula 2: ##STR1## wherein b is an integer of from 1 to 4, B represents a C.sub.1 -C.sub.3 alkylene group and R.sub.1 and R.sub.2 each independently represent hydrogen, halogen, alkyl, phenyl or substituted phenyl; Z is a spacer group and T is a carrier moiety.

Abstract: A method of preparing a 4'-0-demethy-4.beta.-NHR podophyllotoxin, where R is an aryl or dialkyl amino alkyl group, is disclosed. The method includes reacting H.sub.2 NR under basic conditions with a mixture of .alpha. and .beta. epimers of 4'-0-demethyl-4-bromo-podophyllotoxin, to form an epimeric mixture of the 4'-0-demethyl-4-NHR-podophyllotoxin compounds, removing acidic impurities which bind to silica gel in a dichloromethane solvent, and crystallizing 4'-0-demethyl-4.beta.-NHR-podophyllotoxin from its .alpha. epimer.

Abstract: Compounds which are analogs of etoposide and which exhibit anti-tumor activity are disclosed. These compounds having the following structure: ##STR1## wherein R is selected from ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently selected from H, CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, i--C.sub.3 H.sub.7, C.sub.4 H.sub.9, CF.sub.3, OCH.sub.3, OC.sub.2 H.sub.5 , OC.sub.3 H.sub.7, OC.sub.4 H.sub.9, O--i--C.sub.3 H.sub.7, O--i--C.sub.4 H.sub.9, --OCH.sub.2 O--, --OCH.sub.2 CH.sub.2 O--, CH.sub.2 OH, C.sub.2 H.sub.4 OH, CH.sub.2 Cl C.sub.2 H.sub.4 Cl, CH.sub.2 F, C.sub.2 H.sub.4 F, CH.sub.2 OCH.sub.3, COCH.sub.3, COC.sub.2 H.sub.5, CO.sub.2 CH.sub.3, CO.sub.2 C.sub.2 H.sub.5, NO.sub.2, NH.sub.2, NH.sub.2.HCl, NH.sub.2.HAc, NH.sub.2.1/2H.sub.2 SO.sub.4 , NH.sub.2.1/3H.sub.3 PO.sub.4, N(CH.sub.3).sub.2, N(C.sub.2 H.sub.5).sub.2, OH, CN, N.sub.3, SO.sub.2 H, SO.sub.2 NH.sub.2 , SO.sub.

Abstract: A process for preparing crystalline, anhydrous podophyllotoxin from a podophyllotoxin product comprises dissolving the product in a non-aromatic and non-halogenated solvent which has a boiling point at atmospheric pressure not exceeding 130.degree. C., and which contains at the most about 1% v/v of water, cooling the solution to precipitate crystals of podophyllotoxin, isolating the crystals and drying them at a temperature which during the drying procedure is increased but is always such that it is below the temperature at which the crystals sinter or melt, the drying being continued until the melting point is in a range of 183.degree.-184.degree. C. and the residual amount of solvent is at the most 500 ppm. When the starting material contains complexed or adsorbed organic solvent, an initial azeotropic evaporation treatment is performed to remove this solvent. The yield of pure podophyllotoxin is greatly increased by adding water to the crystallization mixture.

Abstract: Novel podophyllotoxin compounds and their use in treating tumors are disclosed.

Abstract: Novel phenanthrene derivatives represented by the general formula (1), ##STR1## wherein the group of the formula ##STR2## is a group of the formula ##STR3## (wherein R.sup.1 is a hydrogen atom or a lower alkyl group), a group of the formula ##STR4## (wherein R.sup.2 is a hydrogen atom or a lower alkanoyl group) or a group of the formula ##STR5## (wherein R.sup.2 is the same as defined above), and salts thereof, and other compounds derived therefrom and salts thereof; processes for preparing the same; and interleukin-1 (IL-1) inhibitors containing the abovementioned novel phenanthrene derivatives as to the active ingredient(s).

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: There are disclosed intermediates which can be converted into podophyllotoxin and related compounds, which are known antineoplastic agents. There are also disclosed processes for the preparation of such intermediates, and processes for the conversion of the intermediates into known intermediates which are readily converted into podophyllotoxin and related compounds.

Abstract: Preparation of 4-bromo-4'-demethylepipodophyllotoxin by reacting podophyllotoxin with hydrogen bromide at about -20.degree. C. New antitumor compounds of the formula: ##STR1## wherein R is A--(CH.sub.2).sub.n [A(CH.sub.2).sub.n ].sub.m (CHAH).sub.p --Q or ##STR2## each A, independently, is O, S, SO or SO.sub.2 ; n is an integer from 1 to 6, except when n and p, taken together, are zero, then n is 2 to 6; n is 0, 1, or 2; p is 0, 1, or 2; Q is H, alkyl from 1 to 6 carbon atoms which may be substituted with an NR.sub.1 R.sub.2 group wherein each R.sub.1 and R.sub.2, independently, is selected from the group of H, alkyl containing 1 to 6 carbon atoms which may be substituted with OH, alkanoyl containing 1 to 6 carbon atoms, or R.sub.1 and R.sub.2 are interconnected and together with the N to which they are connected form an N heterocyclic ring of 5 to 6 carbon atoms; R.sub.3 is hydrogen, and R.sub.

Abstract: Podophyllotoxin is recovered from podophyllum resin with improved efficiency by adsorbing impurities out of a solution using a solid adsorbent, preferably alumina. This improvement finds application in an overall process for purifying podophyllotoxin from podophyllum resin in which the podophyllotoxin is first crystallized from the podophyllum resin, the crystals so formed are dissolved and subjected to the solid adsorbent treatment, crystals are then recovered and optionally recrystallized and dried to give the desired product.

Abstract: There are disclosed intermediates which can be converted into podophyllotoxin and related compounds, which are known antineoplastic agents. There are also disclosed processes for the preparation of such intermediates, and processes for the conversion of the intermediates into known intermediates which are readily converted into podophyllotoxin and related compounds.

Abstract: There is provided a novel and efficient stereoselective total synthesis of epipodophyllotoxin and related epipodophyllotoxin compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each are independently hydrogen or (lower)alkoxy, or R.sup.1 and R.sup.2, taken together, is methylenedioxy; R.sup.4 and R.sup.6 each are independently hydrogen or (lower)alkoxy; and R.sup.5 is hydrogen or a phenol-protecting group; or an acid addition salt thereof. The present invention also provides novel intermediates and processes for the preparation of said intermediates, which are then converted into known antineoplastic agents.

Abstract: A novel process for preparing a naphthalene derivative of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are a lower alkoxycarbonyl group or both may combine to form a group of the formula ##STR2## one of R.sup.3 and R.sup.4 is hydrogen atom or a lower alkoxy group and the other is a lower alkoxy group; ring A is a substituted or unsubstituted benzene ring, which is useful as a hypolipidemic agent, and a novel intermediate of the formula: ##STR3## wherein R1, R2, R3, R4 and ring A are the same as defined above.

Abstract: A new pyranoquinone and use thereof as an anticoccidial agent.

Abstract: It has now been discovered that the acid catalyzed Michael reaction products of ascorbic acid and certain selected ketones are useful for their therapeutic activity. More specifically the useful reaction products of the invention are those obtained by reactions of ascorbic acid with .alpha.,.beta. unsaturated alicyclic diketones containing from 5 to 7 carbon atoms.The preferred compounds of the invention may be represented by the formula: ##STR1## wherein n is 1, 2 or 3. The ability of the compounds of this invention to stimulate an immune response has been established by a number of art recognized tests.

Abstract: The present invention is directed to novel taxols useful as a chemotherapeutic agent. Moreover, the present invention is directed to the process of preparing taxols and various intermediates in said process. A key intermediate is this process is 2,5-dihydroxy-2-patchoulenes. Therefore the present invention is also related to said intermediate and the process for its preparation.

Abstract: A method for forming bridged biaryl compounds via the intramolecular oxidative biarylic coupling of precursor compounds containing two aromatic rings linked via a hydrocarbon chain is disclosed along with the ruthenium catalyst for its implementation and new compounds resulting therefrom. The biarylic coupling method is characterized in that the biarylic precursors are cyclized in the presence of the catalyst tetrakis(trifluoroacetate) of ruthenium (IV).

Abstract: The invention relates to compounds consisting of podophyllotoxin and its derivatives of the formula ##STR1## wherein R.sub.1 is H or OH and R.sub.2 is H or CH.sub.3, for treatment of psoriasis, malaria and rheumatoid arthritis and to a method for their preparation. Furthermore, the invention concerns the use of the compounds for treatment of said states of illness, as well as the use of said compounds for the preparation of pharmacological compositions for the treatment of said states of illness.

Abstract: Naphthalene derivative of the formula: ##STR1## wherein R.sup.1 is hydrogen atom or a lower alkoxycarbonyl andR.sup.2 is a lower alkoxycarbonyl, or R.sup.1 and R.sup.2 are combined together to form a group of the formula: ##STR2## each of R.sup.3 and R.sup.4 is a lower alkoxy, or one of R.sup.3 and R.sup.4 is hydrogen atom and the other is a lower alkoxy, andRing A is a substituted or unsubstituted benzene ring, and a pharmaceutically acceptable salt thereof are disclosed. Said naphthalene derivative (I) and its salt have excellent hypolipidemic activity and are useful for treatment or prophylaxis of hyperlipidemia and/or arteriosclerosis.

Abstract: There are disclosed intermediates which can be converted into podophyllotoxin and related compounds, which are known antineoplastic agents. There are also disclosed processes for the preparation of such intermediates, and processes for the conversion of the intermediates into known intermediates which are readily converted into podophyllotoxin and related compounds.

Abstract: There is provided a novel and efficient stereoselective total synthesis of epipodophyllotoxin and related epipodophyllotoxin compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each are independently hydrogen or (lower)alkoxy, or R.sup.1 and R.sup.2, taken together, is methylenedioxy; R.sup.4 and R.sup.6 each are independently hydrogen or (lower)alkoxy; and R.sup.5 is hydrogen or a phenol-protecting group; or an acid addition salt thereof. The present invention also provides novel intermediates and processes for the preparation of said intermediates, which are then converted into known antineoplastic agents.

Abstract: A liquid dosage form suitable for oral administration of etoposide which is sufficiently concentrated to be administered in capsule form and which provides improved absorption of the drug relative to prior oral formulations.

Abstract: There is provided a novel and efficient stereoselective total synthesis of epipodophyllotoxin and related epipodophyllotoxin compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each are independently hydrogen or (lower)alkoxy, or R.sup.1 and R.sup.2, taken together, is methylenedioxy; R.sup.4 and R.sup.6 each are independently hydrogen or (lower)alkoxy; and R.sup.5 is hydrogen or a phenol-protecting group; or an acid addition salt thereof. The present invention also provides novel intermediates and processes for the preparation of said intermediates, which are then converted into known antineoplastic agents.

Abstract: A novel Micromonospora strain is provided which produces Crisamicin, a complex having gram positive antibacterial and antiviral activities. Crisamicin contains as major components compounds Crisamicin A and Crisamicin B, and minor amounts of compounds Crisamicin C, D and E.

Abstract: A copolymer formed from an isoimide oligomer and another compound, such as an aryl sulfone, each of which has reactive functional terminal groups, such as ethylenic or acetylenic groups. The isoimide oligomer is soluble in the other compound, unreactive with the compound below a certain temperature and forms a liquid blend therewith. Upon heating the liquid blend above that certain temperature, the terminal groups on the isoimide oligomer and the other compound react with each other to form a copolymer. The liquid blends may be used to form encapsulants, coatings, films, and resin matrices for composites to provide resins with excellent high temperature properties.

Abstract: Hyperacidified tumors having high .beta.-glucuronidase activity can be treated with glucuronides with aglycones toxic to the tumor cells with great safety toward the rest of the body by first administering an alkalinizing agent in an amount sufficient to maintain the pH level of non-tumor tissues at approximately 7.4 during the glucuronide treatment. This will cause inactivation of .beta.-glucuronidase activity in the rest of the body. Novel glucuronides are disclosed the aglycones of which exert a higher toxic effect in an acid environment or is water-soluble only in an alkaline environment. Such compounds have particular utility with the above process. By substituting radioisotopes into the aglycone, diagnosis and in situ radiation therapy may be accomplished. Bacterial cells having .beta.-glucuronidase activity may also be diagnosed and treated in accordance with the present invention.

Abstract: One aspect of this invention relates to 2-substituted podophyllotoxin corresponding to the formula: ##STR1## where R.sub.1 is the residue of an electrophile reactant with the precursor enolate, e.g., halogen, i.e., Br, Cl, F and I, lower alkyl (preferably methyl), hydroxyl, --SR.sub.5 where R.sub.5 is lower alkyl, aralkyl or aryl and COOR.sub.6 where R.sub.6 is hydrogen or lower alkyl. Another aspect of this invention relates to 2-substituted etopsides and related compounds corresponding to the formula: ##STR2## where R.sub.1 is as defined above, and where R.sub.2 is: ##STR3## where AcO is acetyl; or ##STR4## where R.sub.3 is hydrogen and R.sub.4 is alkyl, alkenyl, cycloalkyl, 2-furyl, 2-thienyl, aryl, aralkyl, or alkenyl wherein the aromatic ring (preferably phenyl) may be optionally substituted by one or more hydroxyl, alkyl, alkoxy, nitro or halogen; or where each of R.sub.3 and R.sub.4 is alkyl or where each of R.sub.3 and R.sub.

Abstract: Processes for forming a class of relatively low molecular-weight oligomers containing at least one isoimide group and terminal groups capable of undergoing an addition polymerization reaction are provided. These oligomers are characterized by excellent solubility in common solvents and a melting temperature considerably lower than their cure temperature, thus enabling the oligomers to be formed into cured polymers more slowly and at lower temperatures, all without the evolution of deleterious gases. The process for forming these oligomers includes the formation of a polyamic acid and dehydration thereof under specified conditions to effect cyclization of the polyamic acid to form the isoimide-containing oligomer, without the formation of undesired side-reaction products.

Abstract: A class of relatively low molecular-weight oligomers containing at least one isoimide group and terminal groups capable of undergoing an addition polymerization reaction are provided. These oligomers are characterized by excellent solubility in common solvents and a melting temperature considerably lower than their cure temperature, thus enabling the oligomers to be formed into cured polymers more slowly and at lower temperatures, all without the evolution of deleterious gases. The oligomers of the present invention may be formed by reacting an aromatic dianhydride with an aromatic diamine, followed by reaction with a monoanhydride. The resulting product is dehydrated to form the isoimide-containing oligomer.

Abstract: A class of relatively low molecular-weight oligomers containing at least one isoimide group and terminal groups capable of undergoing an addition polymerization reaction are provided. These oligomers are characterized by excellent solubility in common solvents and a melting temperature considerably lower than their cure temperature, thus enabling the oligomers to be formed into cured polymers more slowly and at lower temperatures, all without the evolution of deleterious gases. The oligomers of the present invention may be formed by reacting an aromatic dianhydride with an aromatic diamine, followed by reaction with a functional mono-amine. The resulting product is then dehydrated to form the isoimide-containing oligomer.

Abstract: The invention provides a novel antioxidant obtained from rosemary and suitable for preventing oxidation of various organic materials or, in particular, oleaginous foodstuffs. The antioxidant is prepared by extracting rosemary with a non-polar organic solvent and further extracting the thus extracted material with an aqueous alkaline solution having a pH of at least 10.5 as a weakly acidic fraction soluble in such a strongly alkaline solution. The extraction with the non-polar organic solvent is preferably preceded or followed by steam distillation in order to remove any spicy volatile materials undesirable when the antioxidant is added to foodstuffs or the like. Column chromatographic separation of the above obtained weakly acidic fraction into components gives a novel compound 7.beta.,11,12-trihydroxy-6,10-(epoxymethano)abieta-8,11,13-trien-20-one as the effective ingredient of the antioxidant prepared from rosemary. Characterization of the above novel compound is given.

Abstract: A class of relatively low molecular-weight oligomers containing at least one isoimide group and terminal groups capable of undergoing an addition polymerization reaction. The oligomers of the present invention are characterized by excellent solubility in common solvents and a melting temperature considerably lower than their cure temperature, thus enabling the oligomers to be formed into cured polymers more slowly and at lower temperatures, all without the evolution of deletrious gases.

Abstract: Naturally occurring iridoids provide the starting material for a unique synthesis sequence to produce prostaglandin intermediates. The iridoid lactone is hydrogenated, converted to an acetal, and rings opened to introduce the carbonyl octenyl side chain in six steps. The intermediate can be converted to prostaglandin as previously demonstrated.