Abstract: The present invention relates generally to the compound: N-((4aS,6aR,6bS,8aR,12aS,14aR,14bS)-11-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,12a,14,14a,14b-octadecahydropicen-4a-yl)-2,2-difluoropropanamide, polymorphic forms thereof, methods for preparation and use thereof, pharmaceutical compositions thereof, and kits and articles of manufacture thereof.

Abstract: The present invention relates generally to the compound: N-((4aS,6aR,6bS,8aR,12aS,14aR,14bS)-11-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,12a,14,14a,14b-octadecahydropicen-4a-yl)-2,2-difluoropropanamide, polymorphic forms thereof, methods for preparation and use thereof, pharmaceutical compositions thereof, and kits and articles of manufacture thereof.

Abstract: Methods of halogenating a carbon containing compound having an sp3 C—H bond are provided. Methods of fluorinating a carbon containing compound comprising halogenation with Cl or Br followed by nucleophilic substitution with F are provided. Methods of direct oxidative C—H fluorination of a carbon containing compound having an sp3 C—H bond are provided. The halogenated products of the methods are provided.

Abstract: A compound having the structure wherein Y is selected from the group consisting of —C(O)OR2, —C(O)NHR8, —C(CH2)1-2OR3, OH, and or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.

Abstract: Disclosed is a method for monitoring early treatment response of a cancer treatment comprising measuring by magnetic resonance spectroscopy (MRS), for example, proton MRS, the amount of Choline present in the endomembranes of the cancerous tissue before and after treatment; the treatment comprises administration of a cytotoxic therapy, whereby a decrease in the amount of Choline after treatment is indicative of a positive response. The decrease in the amount of Choline represents the decrease in the internal cell membrane as a result of down regulation of the organelles and their secretory granules and their transport vesicles. Disclosed also is a method for determining effectiveness of a cytotoxic treatment of cancer. In addition, a method for monitoring protein translation related to the cytotoxic treatment of cancer is disclosed.

Abstract: The invention at hand describes functionalized diols of diamondoids, in which one of the two hydroxy groups is masked by a protective group, as well as methods for producing these functionalized diols. The protective group is a group —CHR1R2, wherein R1 and R2 stand for alkyl groups and the protective group comprises at least one halogen atom. The monoethers of the diamondoid diols according to the present invention are produced by reacting the diamondoid diol with a halogenated alcohol CHOHR1R2 in the presence of a catalyst acid. The monoetherified diols allow for the targeted production of derivatives of diamondoids, for example, of the corresponding aminoalcohols and aminocarboxylic acids. For that purpose, the diamondoid monoether is reacted in a first step with a halogen nitrile in a Ritter reaction to the corresponding monoether amide.

Abstract: Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.

Abstract: The invention relates to a process for preparing certain adamantanamines, of formula wherein R, R? are each methyl and X is halogen, to intermediates used in the process, and to processes for preparing such intermediates.

Abstract: A process for preparing 5,6-diethyl-2,3-dihydro-1H-inden-2-amine and acid addition salts thereof from 2-aminoindan. The process comprises protecting the amino group of 2-aminoindan, acetylating the ring in the protected compound, reducing the acetyl group to ethyl to form a monoethyl derivative, acetylating the monoethyl derivative, reducing the acetyl group to form a diethyl derivative, deprotecting the latter by hydrolysis and recovering the product in free or salt form. The process does not use deleterious Grignard reagents or nitrites such as isoamyl nitrite, and provides high regioselectivity and high yield of 5,6-diethyl-2,3-dihydro-1H-inden-2-amine. In addition, the process uses acetyl halide as both a reactant and a solvent.

Abstract: The invention relates to a novel process for the preparation of an aminoalcohol of the formula 1

Abstract: A novel process for the preparation of (1S, 4R)- or (1R, 4S)-4-(2-amino-6-chloro-9H-purin-9-yl)-2 -cyclopentene-1-methanol of the formula is described.

Abstract: The present invention relates to novel colchicine derivatives having antiproliferative, antineoplastic, antiinflammatory and muscle relaxant activities; said derivatives include novel colchine nitrogen amides for use either as such or after derivatization of the hydroxyl at C.sub.3 of the aromatic ring and at C.sub.10 of the tropolone ring. These novel compounds have a cytotoxicity on human tumoral cell lines comparable with colchicine but, in comparison with the latter, they are much more active on cells resistant to the usual antiblastics. The compounds can be included in pharmaceutical formulations useful for the intravenous, oral and topical administrations.

Abstract: A compound of formula (I): ##STR1## and its pharmaceutically acceptable salt, wherein R is hydrogen or hydroxy; Ar is unsubstituted or substituted phenyl; X is unsubstituted or substituted phenyl or heterocyclic, mono-, di- or trihalomethyl, cyano, or the like; and X.sup.2 is phenyl, naphthyl, furyl, thienyl, pyridyl, thiazolyl, benzofuryl or benzothienyl, each of which may either be unsubstituted or substituted. These compounds have agonist activity toward opioid kappa receptors and are thus useful as analgesic, anti-inflammatory, diuretic and neuroprotective agents.

Abstract: Certain N-acyl 2-aryl cyclopropylmethylamine derivatives are useful as melatonergic agents.

Abstract: Novel substituted fluorene compunds of Formula I are active as melatonergic agents: ##STR1## wherein: X=H, halogen, OH or OZ;Z=C.sub.1-6 alkyl; --(CH.sub.2).sub.m --CF.sub.3 (m=0-2); CD.sub.3 ; or ##STR2## n=1 or 2; and R=C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl, halogen substituted C.sub.1-6 alkyl, or C.sub.1-6 alkoxy substituted C.sub.1-6 alkyl.

Abstract: A process for producing an ethenyl amide compound, which comprises reacting a Schiff base compound having a carbon atom adjacent to a carbon atom constituting an imino group and at least one hydrogen atom on the carbon atom with an acylhalide at a reduced pressure while removing by-produced hydrogen halide by distillation to produce an ethenyl amide compound having an amide bond in the molecule and a double bond between carbons at .alpha.-position and .beta.-position with respect to the nitrogen atom of the amide bond.

Abstract: The present invention provides novel intermediates which are useful for the preparation of excitatory amino acid receptor antagonists. Further provided is a process to enatioselectively prepare hydroisoquinoline compounds with central nervous system activity.

Abstract: Provided is a method of producing a highly pure amide compound in a high yield, wherein a silazane compound and/or a silane compound having at least one silicone-nitrogen bond are added to a reaction mixture obtained by reacting an acylfluoride group-containing compound with an amino compound, wherein the amide compound is present together with hydrogen fluroide and/or the amine hydrofluoride, thereby removing the hydrogen fluoride and/or the amine hydrofluoride from the reaction mixture.

Abstract: A novel hexa-cyclic compound, a derivative of camptothecin, of the general formula: ##STR1## The compound is prepared from an aminoketone compound and a pyranoindolizine compound by the condensation-ring closing reaction. It is abundantly water-soluble, and has an excellent antitumour activity and a high degree of safety, and can be applied as an antitumour medicine for curing tumors of various kinds.

Abstract: The present invention relates to a novel enantiospecific process for preparing (S)-1- 2(S)-(1,3-dihydro-1,3-dioxo-isoindo-2-yl)-1-oxo-3-phenylpropyl!-1,2 ,3,4-tetrahydro-2-pyridine-carboxylic acid methyl ester which is a useful intermediate in the preparation of 4S- 4.alpha., 7.alpha.(R*), 12b.beta.!!-7- (1-oxo-2(S)-thio-3-phenylpropyl)amino!-1,2,3,4,6,7,8,12b-oc tahydro-6-oxo-pyrido 2,1-a! 2!benzazepine-4-carboxylic acid and 4S- 4.alpha., 7.alpha.(R*), 12b.beta.!!-7- (1-oxo-2(S)-acetylthio-3-phenylpropyl)amino!-1,2,3,4,6,7,8, 12b-octahydro-6-oxo-pyrido 2,1-a! 2!benzazepine-4-carboxylic acid and pharmaceutically acceptable salts thereof which is useful as an inhibitor of enkephalinase and angiotensin converting enzyme and to novel intermediates thereof.

Abstract: A compound which is selected from those of formula (I): ##STR1## in which A, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined in the description, its optical isomers, and its addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful for treating a disorder of the melatoninergic system.

Abstract: The invention concerns nitric acid esters of cyclohexanol of formula I ##STR1## in which A signifies a valency bond or a C.sub.1 -C.sub.6 -alkylene chain and B the group --NR.sup.1 --CO--Z, --NR.sup.1 --SO.sub.2 --Z or --CO--NR.sup.2 --Z, whereby R.sup.1 signifies hydrogen or a C.sub.1 -C.sub.6 -alkyl alkyl group R.sup.2 hydrogen, a hydroxyl, hydroxy-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.2 -C.sub.6 -alkynyl group and Z signifies hydrogen a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.2 -C.sub.6 -alkynyl group which may optionally be substituted for the case that B is an --NR.sup.1 --CO--Z group, Z can also signify a C.sub.1 -C.sub.6 -alkoxy group.

Abstract: Intermediate compounds (formula [III]and [IV]) useful as starting materials for the synthesis of amino acid derivatives which have renin inhibitory activity and which are useful as remedies for hypertension are prepared stereoselectively in high yield, without requiring complicated process steps. In this method, by reaction of .alpha.-amino aldehyde derivative [I] and compound [II] in the presence of BF.sub.3.OEt.sub.2, as shown in the following reaction formula, .alpha.-amino-.beta.-hydroxy-.delta.-ketone derivative [III] is prepared, and furthermore, by reducing it as required, compound [IV] is obtained: ##STR1## (where R.sup.1 is a protective group on the amino group, R.sup.2 is a lower alkyl group which may be branched, and R.sup.4 is a cyclohexyl group or phenyl group).

Abstract: A haloacetamide compound of the following formula (I) ##STR1## wherein R.sub.1 represents a substituted or unsubstituted C.sub.6 -C.sub.14 aryl group or a substituted or unsubstituted C.sub.3 -C.sub.8 heteroaryl group having one or two hetero atoms selected from the group consisting of O, S and N,R.sub.2 and R.sub.3, independently from each other, represent a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a C.sub.1 -C.sub.6 alkoxy group, or R.sub.2 and R.sub.3, taken together, represent a C.sub.2 -C.sub.16 alkylene group,R.sub.4 represents a substituted or unsubstituted C.sub.1 -C.sub.12 alkyl group, a substituted or unsubstituted C.sub.6 -C.sub.14 aryl group, a C.sub.2 -C.sub.12 alkenyl grup or a C.sub.2 -C.sub.12 alkynyl group, andY represents a halogen atom selected from the group consisting of Cl, Br and I;and its use as herbicide.

Abstract: The invention relates to the novel cyclohexanediones of formula I ##STR1## in which R is hydrogen or C.sub.1 -C.sub.6 -alkyl,A is R.sub.2, OR.sub.3 or NR.sub.3 R.sub.4,R.sub.2 is C.sub.1 -C.sub.6 -alkyl that is unsubstituted or is mono-substituted by C.sub.1 -C.sub.4 -alkoxy or mono- or poly-substituted by halogen, or is C.sub.3 -C.sub.6 -cycloalkyl,R.sub.3 is C.sub.1 -C.sub.6 -alkyl or C.sub.3 -C.sub.6 -cycloalkyl, or is phenyl or benzyl each of which is unsubstituted or is mono-, di- or tri-substituted by R.sub.5,R.sub.4 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.3 -C.sub.6 -cycloalkyl,R.sub.3 and R.sub.4 are, in addition, together with the nitrogen atom to which they are bonded, a pyrrolidine, morpholine or piperidine radical,B is one of the radicals ##STR2## m is 0, 1, 2 or 3, R.sub.5 is halogen, nitro, cyano, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkylsulphinyl or C.sub.1 -C.sub.

Abstract: A complex of an azo compound of the formula ##STR1## wherein R and R' are selected from the group consisting of hydrogen, --COCR.sub.4.sup.3, --COCHR.sub.2.sup.4, --CO.sub.2 C.sub.2 H.sub.5, --CH.sub.2 CH.sub.2 R.sup.4, --(CH.sub.2 CH.sub.2 R.sup.4)2, --CH.sub.2 CH.sub.2 OH, --CONHCH.sub.2 CH.sub.2 R.sup.4 and --CH.sub.2 CH.sub.2 OCOHN.sub.2, R.sup.4 is selected from the group consisting of chlorine, ##STR2## --NHCO.sub.2 CH.sub.2 CH.sub.2 OH, --HNCO.sub.2 C.sub.2 H.sub.5, --NHOH, --NHCONHOH and --NHCH.sub.3 ; R.sup.1 and R.sup.2 are individually selected from the group consisting of ##STR3## --NHCH.sub.2 CH.sub.2 Cl, --NHCONHOH, --NHCO.sub.2 C.sub.2 H.sub.5, 6-mercapropurin, 5-fluoruracil and prenissolin, R.sup.3 is selected from the group consisting of hydrogen, --COCHR.sub.2.sup.4, --SO.sub.2 CH.sub.3, --COC.sub.2 H.sub.5, --CH.sub.2 CH.sub.2 R.sub.4 and --CONH.sub.2, R.sup.

Abstract: This invention relates to novel herbicidal cycloalkenyl acetamides. These acetamides are useful in the inhibition of undesired vegetation and exhibit excellent selectivity in crops of cultivated plants, particularly in crops of flooded rice.

Abstract: Novel chloroacetic acid cyclohexylamides of the formula I ##STR1## where R.sup.1, R.sup.2 and R.sup.3 have the meanings given in the description, their preparation and their use as herbicides.

Abstract: Sulfonyl or carbonyl derivatives of inositols are found to be effective phospholipase C inhibitors and thereby potent anti-inflammatory and analgesic agents. These inositol derivatives are prepared by condensation of a protected inositol with a substituted sulfonic or carboxylic acid derivative followed by removal of protecting groups.

Abstract: Antimicrobial compounds of the following formula are disclosed: ##STR1## wherein X is selected from the group consisting of --O--, --CH.sub.2 and ##STR2## m is 0 or 1; R.sub.1 is selected from the group consisting of hydrogen, nitro, amino, lower alkyl, lower alkanamido, lower N,N-dialkylamino, formamido, hydroxy, lower alkoxy, halogen, lower haloalkanamido and pyrryl; n is 1 or 2; and R.sub.2 is selected from the group consisting of hydrogen, methyl, fluoro, chloro and nitro. Acyl chlorides, esters, alkylaminoalkyl ester salts, amides and pharmaceutically acceptable carboxylate salts are also disclosed. Pharmaceutical compositions containing these compounds, methods of using these compound and synthetic intermediates are also disclosed.

Abstract: A process for the preparation of N,N-dimethyl-N'-(2-bromo-4-methyl-phenyl)-triazene of the formula ##STR1## comprising (a) reacting N-acetyl-p-toluidine of the formula ##STR2## with bromine at a temperature between about 0.degree. and 100.degree. C., to give the intermediate product of the formula ##STR3## (b) reacting the intermediate product with hydrochloric acid by either (i) adding a dilute solution of aqueous hydrochloric acid to the intermediate product in its reaction solution and heating the mixture to a temperature between about 50.degree. and 120.degree. C., or(ii) precipitating the intermediate product from its reaction solution by mixing with water and filtering off, and without purification or drying heating the precipitate with dilute aqueous hydrochloric acid to a temperature between about 50.degree. and 120.degree. C.

Abstract: The present invention relates to the use of telluroxides as mild and selective oxidizing agents serving to oxidize certain functions, notably >C.dbd.S groups, in the presence of other relatively easily oxidized functions which remain unaffected; telluroxides of interest as oxidizing agents include, for example, compounds of the formula: ##STR1## wherein R and R.sup.1, which may be the same or different, each represent an optionally substituted aryl or heterocyclic group; or R and R.sup.1 together with the tellurium atom therebetween represent a heterocyclic ring, which may contain one or more further heteroatoms, and which may carry substituents and/or fused aromatic rings.

Abstract: Compounds of the formula ##STR1## wherein the serrated lines denote both endo and exo forms; R.sub.1 and R.sub.2 are the same or different and are C.sub.1 to C.sub.6 alkyl, C.sub.5 or C.sub.6 cycloalkyl, C.sub.5 or C.sub.6 cycloalkenyl, phenyl optionally substituted with C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy or halo, or 5 or 6 membered heterocyclic aryl wherein the heteroatom is oxygen, nitrogen or sulfur; R.sub.3 is a C.sub.1 to C.sub.6 alkyl radical; R.sub.4 and X are optionally present, and when present R.sub.4 is a C.sub.1 to C.sub.6 alkyl radical or hydrogen and X is an inorganic or organic anion which forms a pharmaceutically acceptable salt. Methods for preparing these compounds are also disclosed. The compounds of the present invention are useful as anticholinergic agents.

Abstract: The disclosure herein relates to tertiary 2-haloacetamides substituted on the amide nitrogen atom with certain 1-cycloalken-1-yl, alkoxymethyl, alkylthiomethyl or acetamidomethyl radicals. These acetamides are useful as herbicides.

Abstract: Numerous alpha-carboxylic acids are prepared in a liquid medium by the reaction of an organic compound having at least one reactive hydroxyl or thiol group, with a monoketone, and a haloform, in the presence of a phase transfer catalyst and an alkali metal hydroxide. The term "alpha-alkoxycarboxylic acids" includes alpha-phenoxycarboxylic acids, alpha-thioalkoxycarboxylic acids and alpha-thiophenoxycarboxylic acids. Specific substituents on the beta carbon atom of an alpha-alkoxycarboxylic (or "2-alkoxycarboxylic") acid reaction product formed in this novel synthesis, are introduced by appropriate choice of the ketone reactant; alkoxy and phenoxy substituents on the alpha carbon atom of a 2-alkoxycarboxylic acid are introduced by appropriate choice of the organic compound having a hydroxyl or thiol group. De-alkoxylation of the 2-alkoxycarboxylic acid yields alpha-beta monoolefinically unsaturated carboxylic acids which are necessarily alpha substituted, and may also be beta-substituted.

Abstract: The present application discloses a method of correcting an imbalance of immune homeostasis caused by cytostatic treatment or radiotherapy by administering to a patient in need of such treatment an effective amount of a novel substituted mercapto acid amide and pharmaceutical compositions containing such novel substituted mercapto acid amides.

Abstract: The disclosure herein relates to a new process for the preparation of N-(halomethyl)acylamides by reacting the corresponding N-(alkoxymethyl)acylamide with thionyl chloride or thionyl bromide in the presence of a Lewis Acid catalyst.

Abstract: Herbicidal-substituted .alpha.-(trimethylcycloalkenyl)-N-alkylacetamides of the formula ##STR1## wherein R is a linear or branched alkyl or alkoxyalkyl radical with 1-6 carbon atoms or an allyl radical, optionally substituted with C.sub.1 -C.sub.4 alkylene groups, and X is a substituent from the group consisting of hydrogen, methyl, chlorine and bromine, in any combination, the free valences signify hydrogen and two of the methyl groups on the ring are attached to the same carbon atom, are useful pre- and post-emergent herbicides for weed control in crops.

Abstract: The disclosure herein relates to a new process for the preparation of N-(halomethyl) acylamides by reacting the corresponding N-(alkoxymethyl) acetamide with a hydrogen halide.

Abstract: The disclosure herein pertains to the preparation of N-(alkoxymethyl)- and other N-methylene ether-substituted 2-haloacetamides from other N-methylene ether-substituted 2-haloacetamides and the appropriate alcohol by a transetherification process.

Abstract: The present invention relates to novel amido and sulfonamido derivatives of 2-decarboxy-2-amino-methyl-PG-type compounds. These analogs are useful as nasal decongestants, antifertility agents, and as cytoprotection agents.

Abstract: The disclosure herein relates to a novel process for producing tertiary 2-haloacetamides by reacting primary or secondary 2-haloacetamides with an agent capable of generating an anion of the primary or secondary 2-haloacetamide under base conditions and alkylating the anion of the 2-haloamide with an alkylating agent; said anion is generated, for example, by electrolysis or by metals, metal hydrides, fluorides, oxides, hydroxides, carbonates, phosphates, or alkoxides.