Abstract: The present invention is directed to benzo-fused heterocyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.

Abstract: The present disclosure relates to the preparation of ketal compounds from polyols and oxocarboxylates, and uses thereof.

Abstract: Ketal compounds of the structure I and a method of preparation of the compound from polyols and oxocarboxylates, as well as uses thereof.

Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.

Abstract: The invention provides a method of identifying an inhibitor of LtaS comprising: (a) providing bacteria which comprise a mutation in the mbl gene or homologue thereof; (b) culturing the bacteria of (a) in the presence of a test substance under conditions of low magnesium; (c) monitoring the growth of the bacteria; wherein growth or more rapid growth of the bacteria compared to growth in the absence of the test substance is indicative that the test substance is an inhibitor of LtaS.

Abstract: The present invention relates to a HIV-1 inhibiting pharmaceutical composition containing, as an active ingredient, 6,6?-bieckol which is a phloroglucinol polymer compound separated from Ecklonia cava. The Ecklonia cava-derived 6,6?-bieckol according to the present invention inhibits HIV-1 induced cell fusion, the cell lysis effect, and the cytopathogenic effect including virus p24 antibody production, exhibits RT enzyme inhibition activity and HIV-1 infection inhibition activity, and shows no cytotoxicity at the concentration that almost perfectly inhibits HIC-1 replication.

Abstract: A process of making entecavir comprising converting a compound of formula (M5) to entecavir, wherein the two PGs on the formula (M5) are taken together to form an optionally substituted six- or seven-member cyclic ring.

Abstract: Novel 3?-deoxy-3?-acylaminospectinomycin compounds are described. Also described are methods of using the 3?-deoxy-3-acylaminospectinomycin compounds and other spectinomycin analogs in treating tuberculosis and in treating microbial infections.

Abstract: The present disclosure relates to the preparation of ketal compounds from polyols and oxocarboxylates, and uses thereof.

Abstract: The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide derivatives, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds, and to intermediate precursors to such compounds.

Abstract: The present invention is directed to novel compounds of the formula (I) wherein X, R1, R2, R3, R4, R5 and R6 are as described in the specification, processes for the preparation of and pharmaceutical compositions comprising said derivatives. The compounds of the present invention are useful for the treatment of epilepsy. The invention is further directed to a process for the preparation of compounds of formula (XX), wherein X, R3, R4, R5 and R6 are as described in the specification.

Abstract: Compounds of the formula useful for the treatment of diseases such as depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder (including trichotillomania), social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa, bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.

Abstract: Compounds of the formula 1

Abstract: This invention relates generally to phosphate esters of bis-amino acid sulfonamides containing substituted benzyl amines of formula I: or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as HIV protease inhibitors, pharmaceutical compositions comprising the same, and methods of using the same for treating viral infection.

Abstract: The invention relates to compounds of formula (I): and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.

Abstract: The invention relates to compounds of the formula I in which the radicals R1, R2, R3 and A have the meaning mentioned in the description. The invention further relates to a process for the preparation of the compounds of the formula I by means of solid-phase synthesis, and use thereof as pharmaceuticals.

Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxypyrone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.

Abstract: Dikegulac, its salts and related derivatives are prepared by reacting 2-Keto-L-gulonic acid with 2,2 dimethoxypropane at an elevated temperature in the presence of a catalytic amount of a strong acid. This produces a reaction intermediate which is then reacted with a base to complete hydrolysis and produce an acid salt of dikegulac. Simple concentration and phase separation techniques are used to provide a more efficient, environmentally friendly and cost effective process.

Abstract: A process for the manufacture of polyene aldehydes comprises reacting a polyene O,O-ethylene acetal with a 1-alkoxy-1,3-diene in the presence of a Lewis acid or Bronsted acid, hydrolyzing the resulting condensation product and cleaving off alcohol under basic or acidic conditions from the polyene derivative produced at this stage. The novel polyene O,O-ethylene acetals as well as the likewise novel condensation products in this process form further aspects of the invention. The final products are primarily carotenoids which find corresponding use, e.g. as colorants and pigments for foodstuffs, animal products etc.

Abstract: The present invention relates to specific adamantyl or adamantyl group derivative containing retinoid compounds induce apoptosis of cancer cells. These adamantyl retinoid derivatives are useful for the treatment of many cancers and solid tumors, especially androgen-independent prostate cancer, skin cancer, pancreatic carcinomas, colon cancer, melanoma, ovarian cancer, liver cancer, small cell lung carcinoma, non-small cell lung carcinoma, cervical carcinoma, brain cancer, bladder cancer, breast cancer, neuroblastoma/glioblastoma, and leukemia. Also, the invention relates to novel adamantyl or adamantyl group derivative compounds which are useful as active agents for the treatment or prevention of keratinization disorders and other dermatological conditions, and other diseases.

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: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxyprone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.

Abstract: The present invention relates to a plant growth regulator comprising as an active ingredient an epoxycyclohexane derivative represented by general formula (1): ##STR1## wherein R.sup.1 is a hydrogen atom, a C.sub.1 -C.sub.6, alkyl group or C.sub.3 -C.sub.6 cycloalkyl group, and R.sup.2 and R.sup.3 are independently C.sub.1 -C.sub.6 alkyl groups or are combined to form a C.sub.2 -C.sub.3 polymethylene group which may be substituted with a C.sub.1 -C.sub.6, alkyl group, as well as to a plant growth regulator comprising the epoxycyclohexane derivative and a brassinosteroid as active ingredients. The epoxycyclohexane derivatives exhibit a potent plant growth regulating action which is equivalent to or higher than that of abscisic acid, and are useful as plant growth regulators such as a plant growth accelerator, a germination growth accelerator, a transpiration and wilting inhibitor, a cold resistance enhancer, an accelerator for growing, thickening or maturing fruits, roots, stems or bulbs, etc..

Abstract: A novel process for preparing a 1,4 benzodioxane derivative shown by the formula (1) which is a useful intermediate of circulatory drugs and drugs for psychoneurosis, characterized in sulfonating a phenoxypropanediol with a sulfonyl halide, eliminating the protective group, and then cyclizing the sulfonated compound by treating with a base followed by, if necessary, further sulfonation. ##STR1## In the above formula, R.sup.1 is H, RSO.sub.2, R is alkyl, phenyl which may be substituted with alkyl, R.sup.2, R.sup.3, R.sup.4 are H, halogen, OH, nitro, cyano, formyl, COOH, alkoxycarbonyloxy, alkyl, alkoxy, haloalkyl, N,N-dialkylamino, alkylcarbonyl, alkoxycarbonyl, phenyl which may be substituted by alkyl, etc.

Abstract: A process is provided for producing dikegulac and its salts and derivatives from 2-keto-L-gulonic acid starting material.

Abstract: 1,2,4-trioxane derivatives of formula: ##STR1## (wherein each of the subscripts m and n is equal to 0 or 1;the symbol Z represents an epoxide oxygen atom at the 5,6 or 6,7 positions, or a pair of electrons forming a double bond at the 5,6 or 6,7 positions;each of the symbols Ar.sup.1 and Ar.sup.2, being the same or different represents an aromatic group which optionally substituted;each of the symbols AR.sup.1 and R.sup.2, being the same or different, represents a linear or branched alkyl group, which is optionally substituted, or R.sup.1 and R.sup.

Abstract: Aqueous pharmaceutical compositions containing up to about 40% spectinomycin, prepared by the reaction of the ketone hydrate of spectinomycin with boric acid to form the boron compound, and with a base such as sodium hydroxide to form the stable salt of the compound.

Abstract: A process for oxidizing silyl enone ethers to alpha, beta-unsaturated enodes having the formulas ##STR1## which comprises reacting the appropriate silyl enone ether with a radical generated by the metal catalyst decomposition of a peroxide composition.

Abstract: Certain substituted semicarbazones, including all geometric and stereoisomers thereof, agricultural compositions containing them and their use as arthropodicides.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, alkanamido or sulfonamido, or R.sup.1 and R.sup.2 together are methylenedioxy, ethylenedioxy, or propylenedioxy; R.sup.3 is hydrogen or alkyl; n is one of the integers 2,3 or 4; X is --C(.dbd.O)-- or --(CH.sub.2).sub.m --, in which m is the integer 0 or 1; Y is methylene, ethylene or ethenylene, or a pharmaceutically acceptable salt thereof, are antipsychotic agents.

Abstract: Process for alkylating protected spectinomycin enone derivatives in the gamma position in order to produce intermediates useful in the synthesis of 6'alkylspectinomycins. The intermediate have the formula ##STR1## which comprises reacting a compound having the formula ##STR2## with a strong base and an alkenyl halide, wherein R.sub.1 is selected from the group consisting of alkoxycarbonyl, halogenated alkoxycarbonyl, aralkoxycarbonyl, and arylsulfone; R.sub.2 is selected from the group consisting of hydrogen, trimethylsilyl (TMS), tetrahydropyran (THP), and triethylsilyl (TES); A is selected from the group consisting of oxygen and sulfur; M is selected from the group consisting of lithium and potassium; and n is an integer from 1 to 3.

Abstract: A clerodane-type diterpene derivative, which has antibacterial and antitumor activities, as well as chemically equivalent tautomers thereof and a process for producing said derivative using a microorganism belonging to the genus Streptomyces.

Abstract: The compounds: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, alkanamido, or sulfonamido, or R.sup.1 and R.sup.2 together form methylenedioxy, ethylenedioxy, or propylenedioxy; R.sup.3 is hydrogen or alkyl; n is one of the integers 2, 3 or 4; R.sup.4 and R.sup.5 are, independently, hydrogen, alkyl, cycloalkyl, alkanoyl, aroyl, alkylsulfonyl or arylsulfonyl, or R.sup.4 and R.sup.5 together form a 3-7 membered polymethylene ring; or a pharmaceutically acceptable salt thereof, are antipsychotic, antidepressant and anxiolytic agents useful in the treatment of multi-CNS disease states.

Abstract: This invention relates to novel reactive amino or hydrazino peroxides (hereinafter generally referred to as "AHP's") and derivatives all having a Structure A:(P--R11--X--(--NH--).sub.x --R22--).sub.y --Q].sub.z Ain which the definitions of P, R11, R22, X, Q and x, y and z are given in the Summary of The Invention section, for example, 4,4-di-(t-butylperoxy)pentanohydrazide (I-1), and the use of these novel compounds in curing unsaturated polyester resins, in initiating polymerization of ethylenically unsaturated monomers, for modifying rheology, for crosslinking and curing olefin polymers and elastomers, for producing novel graft and block copolymers, and for producing novel polymers with covalently bound performance additive functions.

Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are inhibitors of leukotriene biosynthesis. These compounds inhibit the mammalian 5-lipoxygenase enzyme, thus preventing the metabolism of arachidonic acid to the leukotrienes. These compounds are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.

Abstract: A method of performing an oxidation reaction in which an alkali hypohalite is used as an oxidizing agent which comprises: carrying out the oxidation reaction in an aqueous medium with concurrently distilling off a solvent used in the reaction as the reaction proceeds under a reduced pressure.The method is in particular useful for the oxidation of diacetone-L-sorbose to diacetone-2-keto-L-gulonic acid in water. The reaction temperature is so accurately controlled that the same optimum yield of diacetone-2-keto-L-gulonic acid is obtained by the use of a reduced amount of sodium hypochlorite as compared with the conventional manner of reaction under atmospheric pressure.

Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are inhibitors of leukotriene biosynthesis. These compounds inhibit the mammalian 5-lipoxygenase enzyme, thus preventing the metabolism of arachidonic acid to the leukotrienes. These compounds are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.

Abstract: Disclosed are 6'-thiomethylsubstituted spectinomycins (XII) which are useful in the same way as other spectinomycin pharmaceutical agents.6'-Thiomethylsubstituted (XIV) and protected spectinomycin (XIII) intermediates useful in the production of 6'-thiomethylsubstituted spectinomycins (XII) and 6'-alkenylspectinomycins (IX) are also disclosed.

Abstract: The present invention relates to novel methods of preparing a wide variety of spectinomycin analogs and biologically acceptable salts thereof. Further, the invention relates both to novel intermediates and novel products therein. The novel products are spectinomycin analogs which can be used for the same biological purposes as spectinomycin. The processes of the invention provide for novel intermediates that are versatile and highly reactive exocyclic enones.

Abstract: Derivatives of 2,2'-iminobisethanol having useful properties in the treatment and/or the prevention of disorders of the coronary-vascular system.

Abstract: The present invention relates to novel compounds and processes. In particular, the invention relates to novel analogs of the aminocyclitol antibiotic spectinomycin. More particularly, it relates to novel processes for synthesizing analogs of spectinomycin; both known analogs and the novel analogs of the present invention. Additionally, the invention includes novel intermediates.The novel analogs of spectinomycin disclosed herein are useful as antimicrobial agents.

Abstract: The invention concerns a method for the synthesis of 6'-ethyl spectinomycin and analogs thereof, including intermediates utilized in the method. The method comprises converting an enamine by a Grignard addition to various novel dienones not hitherto known. The dienones are then hydrogenated and deblocked to obtain 6'-ethyl spectinomycin and analogs thereof. The 6'-ethyl spectinomycin and analogs thereof prepared by the invention exhibit especially good antibacterial activity.

Abstract: The present invention relates to novel methods of preparing a wide variety of spectinomycin analogs and biologically acceptable salts thereof. Further, the invention relates both to novel intermediates and novel products therein. The novel products are spectinomycin analogs which can be used for the same biological purposes as spectinomycin. The processes of the invention provide for novel intermediates that are versatile and highly reactive exocyclic enones.

Abstract: Process for preparing 6'-alkylspectinomycin and analogs thereof. Also provided are novel intermediates utilized in the process.

Abstract: The present invention concerns the novel, sugar-ring expansion for synthesis of novel analogs of spectinomycin or C-6' analogs of spectinomycin from known aminomethyldihydrospectinomycin and analogs thereof. Additionally, the invention concerns the novel synthesis of novel 7 membered sugar-ring analogs of dihydrospectinomycin and C-6' analogs thereof from novel 7 membered sugar-ring spectinomycin and C-6' analogs thereof by treatment with NaBH.sub.4.

Abstract: New bicyclic compounds, inclusive of salts thereof, of the formula: ##STR1## wherein R.sup.1 and R.sup.2, which may be the same or different, each represent hydrogen, halogen, lower alkyl, hydroxyl, lower alkyloxy or aralkyloxy, or R.sup.1 and R.sup.2 jointly represent lower alkylenedioxy; R.sup.3 and R.sup.4 each represent hydrogen or lower alkyl; R.sup.5 represents hydrogen, lower alkyl or --CH.sub.2 SR.sup.7 (R.sup.7 represents hydrogen or acyl); R.sup.6 represents hydrogen or acyl, or R.sup.6 and R.sup.7 jointly represent a single bond; X represents --CH.sub.2 --, --O-- or >N--R.sup.8 (R.sup.8 represents hydrogen, acyl or lower alkyl); and n represents 2, 3 or 4, have inhibitory activities of angiotensin converting enzyme and bradykinin decomposing enzyme, and are useful as antihypertensive agents.

Abstract: Antibiotic acmimycin of the formula ##STR1## is active against Gram positive and Gram negative bacteria. It is produced by culturing the microorganism Streptomyces sp. AC4559 FERM P-6445, and isolating the above compound from the cultured medium.

Abstract: The present invention relates to novel methods of preparing a wide variety of spectinomycin analogs and biologically acceptable salts thereof. Further, the invention relates both to novel intermediates and novel products therein. The novel products are spectinomycin analogs which can be used for the same biological purposes as spectinomycin. The processes of the invention provide for novel intermediates that are versatile and highly reactive exocyclic enones.

Abstract: The present specification provides novel antimicrobial analogs of spectinomycin and intermediates and processes for their preparation. Particularly described are novel 3'-diazo-secospectinomycin derivatives useful in the preparation of a variety of 3'-substituted spectinomycin analogs.