Abstract: Erythromycins, particularly with C-13 substituents R1 (e.g. C3-C6 cycloalkyl or cycloalkenyl groups) are prepared by fermenting suitable organisms in the presence of R1CO2H. A preferred organism is Saccharopolyspora erythraea preferably containing an integrated plasmid capable of directing synthesis of desired compounds.

Abstract: The invention provides a simple and selective method for the deacylation of 4-acylated statins during the preparation of statins from a fermentation broth, more specifically a reduction of impurities from the process, by increasing the pH of the fermentation broth.

Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.

Abstract: Biotransformation products of a fermentation with Streptomyces sp., (Merck Culture Collection MA7165) ATCC No. 55946 are potent antifungal agents. These products may be useful in the treatment of diseases caused by fungal pathogens such as Candida sp. and Cryptococcus neoformans.

Abstract: A subject of the invention is the compounds of formula (I): ##STR1## in which OR.sub.1, OR.sub.2 and OR.sub.3 represent hydroxyl radicals blocked in the form of easily cleavable radicals.The compounds of formula (I) can be used to prepare antibiotic products.

Abstract: There are disclosed novel antifungal macrolides of the formula ##STR1## compositions containing said compounds, methods of using said compounds and a method for synthesizing the compounds.

Abstract: The invention concerns 14-methyl-hexadecen-11-olide, 14-methyl-hexadecen-12-olide and 14-methyl-hexadecanolide and the use of these compounds as fragrance materials with musk odour. The invention also concerns 14-methyl-12-hydroxy-hexasecanolide, which is an intermediate in a novel process to prepare these compounds.

Abstract: A prodrug of the general formula FTLi-(PRT)m, where m is an integer from 1 to 5; FTLi is a ras inhibitor such as a farnesyltransferase inhibitor compound, such as Ia, Ib, Ic; and PRT represents m protecting groups or a precursor thereof, such as compound XVI, which are capable of being cleaved from the ras inhibitor by the action of a enzyme.

Abstract: The present invention relates to a process for producing lactones starting from cyclic ketones which comprises an oxidation reaction which is performed in the presence of an optionally substituted cycloaliphatic peracid or of an optionally substituted aliphatic peracid that is immiscible with water. The process allows to obtain high selectivity, does not entail the use of dangerous reagents, and allows excellent economic advantages.

Abstract: Compound of the Formula 1 ##STR1## wherein: R.sup.1 and R.sup.2 are independently selected from the group comprising hydrogen, C.sub.1 to C.sub.6alkyl, C.sub.1 to C.sub.6 haloalkyl, phenyl, and substituted phenyl;X is selected from the group comprising sulfur, sulphone, disulfide;Y is selected from oxygen, carbon, N--H, N-alkyl, N-aryl, or sulfur; andZ is any linking functionality.The compounds represent a new class of ring opening monomers.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydroxy, 2-hydroxyethoxy, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkanoyloxy, halogen, amino, azido, a keto, p-nitrobenzenesulfonyl or a pyranyloxy group of the formula ##STR2## wherein X is a group of the formula ##STR3## wherein R.sub.3 is hydroxy, C.sub.1 -C.sub.4 alkanoyloxy or organic sulfonyloxy, andR.sub.4 is hydroxy or carbamoyloxy,R.sub.2 is hydrogen, hydroperoxy, hydroxy or methoxy,Y is a group of the formula ##STR4## wherein R.sub.5 is hydroxy or C.sub.1 -C.sub.4 alkanoyloxy, andR.sub.6 and R.sub.7 each independently of the other is hydrogen or methyl, are suitable for the preparation of a medicament for the prophylaxis and treatment of diseases that respond to the inhibition of the osteoclast proton pump.

Abstract: The present invention comprises peptidomimetic compounds which comprise a suitably substituted aminoalkylbenzamide moiety. The instant compounds inhibit the farnesyl protein transferase enzyme and the farnesylation of certain proteins. Furthermore, the instant farnesyl protein transferase inhibitors differ from those previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.

Abstract: Compound (1), isolated from a marine dinoflagellate, is a novel macrolide which has potent in vitro cytotoxicity against human colon carcinoma cell line HCT116 (IC.sub.50 =1.6 nM) and a multiple drug resistant subline. In addition, this compound has good in vivo antitumor activity against a P388 mouse leukemia (150% T/C).

Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Abstract: Fluorine-containing, chiral liquid crystal compounds comprise (a) an aliphatic fluorocarbon terminal portion containing at least two catenary ether oxygen atoms; (b) a chiral, aliphatic hydrocarbon terminal portion; and (c) a central core connecting the terminal portions. The compounds have smectic mesophases or latent smectic mesophases and are useful, for example, in liquid crystal display devices.

Abstract: A novel organic compound, designated botcinolide, has been isolated which possesses significant phytotoxic activity and which may be used as a biodegradable contact herbicide. The compound is a hydroxylated nonalactone that is esterified with 4-hydroxy-2-octenoic acid, and has the following structure: ##STR1## Botcinolide is produced by culture of a novel strain of the fungus Botrytis cinerea, designated UK 185, and may be subsequently recovered from the culture medium and purified.

Abstract: 16-membered macrolide compounds wherein both of hydroxyl groups at the 3"- and 4"-positions form ether bonds together with two alkyl groups which are either the same or different from each other is useful as an antibacterial agent. The macrolide compounds represented by formula (I) are prepared by chemically modifying midecamycin A.sub.3 to obtain a synthesis intermediate of the formula (II), which is further chemically modified.

Abstract: A new-type of macrocyclic lactone denominated "dictyostatin 1" bearing a membered ring system is isolated from a Republic of Maldives marine sponge in the genus Spongia sp. and found to strongly inhibit the growth of an important selection of U.S. National Cancer Institute human cancer cell system and the murine P388 lymphocytic leukemia (PS ED.sub.50 3.8.times.10.sup.-4 mg/ml).

Abstract: A novel microorganism, Coniothyrium fuckelii ATCC 74227, and a process of using the microorganism for the production of lovastatin comprising fermenting Coniothyrium fuckelii ATCC 74227 or a lovastatin-producing mutant thereof in a nutrient medium containing assimilable sources of carbon, nitrogen, and inorganic salts under aerobic fermentation conditions.

Abstract: New cholesterol lowering compounds are formed from the photochemical treatment of zaragozic acid A.

Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Abstract: The invention relates to new derivatives of macrocyclic lactones, a process for their preparation, a pyrolysis process using these new derivatives and the use of the pyrolysis products for the preparation of saturated macrocyclic lactones.

Abstract: Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents and as inhibitors of squalene synthase.

Abstract: The use is described of macrolactones, such as cladospolides and patulolides, as medicaments for the treatment of allergic-inflammatory diseases.

Abstract: The present invention provides for the first time an expeditious method to separate polyene macrolide antibiotics into their major components, through a general preparatory procedure employing high pressure liquid chromatography. The procedure allows for the first time a useable preparatory method for separating the polyene macrolide complexes derived from fermentation and cultivation of various organisms, into their major components. Substantially pure dermostatic A and dermostatic B can now be achieved as well as substantially pure mycoticin A and mycoticin B.

Abstract: Novel lactone and lactam compounds which are useful to lower blood cholesterol levels in a patient, said compounds containing an arylcarboxamide or arylthiocarboxamide moiety.

Abstract: The present invention provides a method for treating patients suffering from the acquired immunedeficiency syndrome (AIDS). The method comprises administering dermostatin, dermostatin A, dermostatin B or derivatives thereof, such as pharmaceutically acceptable esters, salts or complexes. The administration of the dermostatin or dermostatin A or dermostatin B should be done as soon as possible after the detection of the presence of the HIV virus which is believed to be responsible for the onset of AIDS. These polyene macrolide antibiotics have been found to be effective in improving the viability of lumphocyte cells infected with the HIV virus and in preventing the replication of the virus. The present invention also provides for the first time substantially pure dermostatin A and dermostatin B and an HPLC method for separation of dermostatin complex into those components in substantial purity.

Abstract: The invention relates to antibacterial pseudo-primycin complexes of formula (I) ##STR1## to the components and acid addition salts thereof, as well as to the preparation of these compounds and to the pharmaceutical compositions containing said compounds as active ingredient.In the formula (I) R.sup.1 is butyl, pentyl or hexyl, R.sup.2 is hydrogen, hydroxyl or O-arabinose and X is organic or inorganic acid ion.

Abstract: The invention relates to the components of primycin antibiotic complex and the salts thereof and to the process for the separation of the individual components by chromatography. A further object of the invention is a synergistic antimicrobial composition containing the said components and a process for the preparation thereof.

Abstract: The invention relates to antibacterial pseudo-primycin complexes of formula (I) ##STR1## to the components and acid addition salts thereof, as well as to the preparation of these compounds and to the pharmaceutical compositions containing said compounds as active ingredient.In the formula (I) R.sup.1 is butyl, pentyl or hexyl, R.sup.2 is hydrogen, hydroxyl or O-arabinose and X is organic or inorganic acid ion.

Abstract: New 10-membered ring lactones, a process for the preparation thereof, and the use thereof.It is possible with the aid of Penicillium strains to prepare new 10-membered ring lactones having a pharmacological action.

Abstract: New benz[b]pyranes and pyranopyridines of formula I, ##STR1## wherein the significances of substituents V, T, W, R.sub.3 to R.sub.5, R.sub.9, R.sub.10, m, X, Y and Z are given in claim 1 and their N-oxides and their salts and their use in the treatment of raised blood pressure in the treatment of vascular disorders and other disorders in which a reduction in tension of the smooth muscles is therapeutically useful, as well as in the treatment of hair loss and baldness. Further the compounds are useful in the treatment of asthma and obstructive disorders of the respiratory system as well as in the prophylactic treatment of obstructive or inflammatory airways disease, for example asthma, as well as novel pharmaceutical compositions comprising said K.sup.+ channel activators suitable for such use.

Abstract: Scytophycins A, B, C, D and E, an aldehyde and alcohol derivative of scytophycin B and the specified alkanoyl and benzoyl esters of scytophycins A, B, C, D and E and the B derivatives (scytophycin compounds) are novel antineoplastic and antifungal agents. Antifungal compositions containing a scytophycin compound and methods of inhibiting fungi, especially plant pathogenic fungi, using these compositions are included. A method for producing the scytophycin complex, comprising scytophycins A, B, C, D and E, using a new strain of the blue-green alga Scytonema pseudohofmanni, and a biologically purified culture of the alga are also provided.

Abstract: Oxypricin, an antibiotic of the Formula (II) ##STR1## having antibiotic activity is disclosed.

Abstract: Scytophycins A, B, C, D and E, an aldehyde and alcohol derivative of scytophycin B and the specified alkanoyl and benzoyl esters of scytophycins A, B, C, D and E and the B derivatives (scytophycin compounds) are novel antineoplastic and antifungal agents. Antifungal compositions containing a scytophycin compound and methods of inhibiting fungi, especially plant pathogenic fungi, using these compositions are included. A method for producing the scytophycin complex, comprising scytophycins A, B, C, D and E, using a new strain of the blue-green alga Scytonema pseudohofmanni, and a biologically purified culture of the alga are also provided.

Abstract: 6-Substituted-4-hydroxy-tetrahydropyran-2-ones, useful as anti-atherosclerotic agents, are obtainable by the process of the invention. The 6-substituents have a phenyl, naphthyl, tetrahydronaphthyl or indolyl nucleus bound through an ethenyl unit. The invention includes novel intermediates.

Abstract: New tetra-alkyl-2,2,5,5-cyclohexanone-4-ol-1-compounds and their sulphonyl derivatives with the general formula: ##STR1## in which: each of R and R', identical or different, represents an alkyl radical (1-5 carbons) and R" represents a hydrogen atom or a radical SO.sub.2 R"' in which R"' represents an alkyl radical (1-5 carbons) or an aryl radical (6-14 carbons), the process and the intermediates for their preparation, as well as their use in the synthesis of cyclopropane lactones of cis structure.

Abstract: A compound having cytotoxic activity of the formula: ##STR1## and a composition comprising such compound in a suitable pharmaceutical carrier.

Abstract: Aerocavin, a novel antibiotic substance having the structure ##STR1## and aerocyanidin, a novel antibiotic substance having the structure ##STR2## can be prepared by cultivation of the microorganism Aerocavin caviae SC 14,030 A.T.C.C. No. 53434.

Abstract: An antibiotic substance designated as AM-2604-A is described, and is obtained by cultivating an antibiotic AM-2604-A substance-producing strain belonging to the genus Streptomyces in a nutrient medium and recovering the desired substance from the culture broth.

Abstract: The subject disclosure discloses a chemical intermediate in antibiotic synthesis of the structure: ##STR1## wherein R.sub.1 is H or OH and the asterisks indicate asymmetric carbon atoms. Compounds of this type may be obtained by fermentation with a strain of B. subtilis under aerobic conditions. Compounds of the above structure are biologically inactive but are converted by phosphorylation of the hydroxyl group to produce compounds of the structure: ##STR2## wherein R.sub.1 is H or OH, which are useful antibacterial substances having a broad spectrum of antibacterial activity.

Abstract: Bafilomycins of the formula ##STR1## in which R.sup.1 is hydrogen or CH.sub.3, andR.sup.2 is hydrogen, or the group ##STR2## are produced by culturing certain streptomyces, e.g. Tu 1922, Tu 2437 and Tu 2599. Those wherein at least one of the OH groups is acylated are new. The compounds are pesticidally active.

Abstract: Novel lactonic derivatives and their use as starting materials for preparing macrocyclic hydroxyketones useful as intermediates in the preparation of fragrant compounds.

Abstract: From the fermentation carried, out with mutants blocked in the synthesis respectively of erythromycin and of oleandomycin, namely Streptomyces erythreus ATCC 31772 and Streptomyces antibioticus ATCC 31771, using as the substrate a derivative of erythronolide A, namely (8S)-8-fluoroerythronolide A, a derivative of erythronolide B, namely (8S)-8-fluoroerythronolide B, or a derivative of 3-O-mycarosyl-erythronolide B, namely 3-O-mycarosyl-(8S)-fluoroerythronolide B, the corresponding (8S)-8-fluoro derivatives of the erythromycins A, B, C and D, as well as 3-O-oleandrosyl-5-desosaminyl-(8S)-8-fluoroerythronolide A and 3-O-oleandrosyl-5-O-desosaminyl-(8S)-8-fluoroerythronolide B, all belonging to the class of the macrolide antibiotics are obtained.

Abstract: Novel lactonic derivatives and their use as starting materials for preparing macrocyclic hydroxyketones useful as intermediates in the preparation of fragrant compounds.

Abstract: A method for the synthesis of derivatives of deoxyzoapatanol is described. The derivatives are effective as post-implantive contragestational agents.

Abstract: Oxacycloalkenones are prepared by reacting a cycloalkenone with a base in the presence of a dioxygen source in a suitable solvent and isolating the desired product. 1-Hydroxy 2-oxa-3-oxo-.DELTA..sup.4 steroids are convenient synthetic precursors to 2-oxa-3-oxo-.DELTA..sup.4 steroids which find use in modern clinical therapy.

Abstract: Tylactone (20-dihydro-20,23-dideoxytylonolide), which has the formula: ##STR1## and specified acyl ester derivatives thereof are useful intermediates in the preparation of macrolide antibiotics.

Abstract: A process is provided whereby the malodorous and undesirable constituents present with macrocyclic fragrance compounds obtained by the thermal depolymerization of polyesters are removed. The process involves contacting the macrocyclic compound maintained in a liquid state with ozone or ozone and an aqueous solution of hydrogen peroxide.