Abstract: The disclosed subject matter provides certain N-substituted hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or development of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.

Abstract: The present invention relates to processes for the preparation of (2-Amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol hydrochloride (Fingolimod) and pharmaceutically acceptable salts thereof, and intermediates formed in such processes.

Abstract: Disclosed herein are compounds, compositions, methods of treatment and synthetic methods for making compounds related to Ceramides and the use of Ceramides.

Abstract: A hetero-dimeric or hetero-oligomeric receptor, comprising at least one thyrotropin releasing hormone receptor subunit associated with at least one orexin receptor subunit.

Abstract: A novel amine compound represented by the following formula (I), which is superior in immunosuppressive action, rejection suppressive action and the like, and shows reduced side effects such as bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or hydrates thereof, or solvate, as well as a pharmaceutical composition containing this compound and a pharmaceutically acceptable carrier. wherein R is a hydrogen atom or P(?O)(OH)2, X is an oxygen atom or a sulfur atom, Y is CH2CH2 or CH?CH, R1 is cyano or alkyl having a carbon number of 1 to 4 and substituted by a halogen atom(s), R2 is alkyl having a carbon number of 1 to 4 and optionally substituted by a hydroxyl group(s) or a halogen atom(s), R3 and R4 may be the same or different and each is a hydrogen atom or alkyl having a carbon number of 1 to 4, and n is 5-8.

Abstract: Urea-containing, substituted 4-phenyl-[1,3]-dioxanes, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, obesity or a sleep/wake disorder mediated by orexin-2 are described.

Abstract: The invention relates to liquid-crystalline compounds of the formula I in which R1, A1, A2, Z1, Z2, a, b, L1, L2 and L3 are as defined in claim 1, and to liquid-crystalline media comprising at least compound of the formula I and to electro-optical displays containing a liquid-crystalline medium of this type.

Abstract: A liquid-crystalline medium based on a mixture of polar compounds of positive dielectric anisotropy, which comprises one or more compounds of the formula I where R1, A1, A2, Z1, Z2, L1, L2 and n are as defined herein, is suitable for use in, for example, MLC, TN and STN displays.

Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2; Rx is H, alkyl, aryl or halogen; A is (1) a bond; (2) —O—; or (3) B is: and wherein L2, L1, R1, R2, R3, R3′, R3a, R3b, R4, R4′, R5, X,  are as defined herein.

Abstract: Novel acid-sensitive compounds comprising a cyclic ortho-ester that is acid-sensitive, and their salts, and comprising at least one hydrophilic substituent. These compounds are useful, for example, for forming conjugates (liposomes, complexes, nanoparticles and the like) with biologically active substances and releasing them into cellular tissues or compartments whose pH is acidic, or as nonionic surfactant for stabilizing particles encapsulating a biologically active substance and then destabilizing them in acid medium, or alternatively as a vector covalently linked to a therapeutic molecule so as to release said therapeutic molecule into the cellular tissues or compartments whose pH is acidic.

Abstract: There can be provided a liquid crystalline compound expressed by the general formula (1): 1

Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) in which A, B, G, X, Y, Z and n are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.

Abstract: A process for the preparation of 2-(2-fluoro-4-biphenyl)propianic acid enantiomers comprising a II order resolution of ketals of formula ##STR1## wherein R.sub.1 ad R.sub.2 have the meanings reported in the description; the asterisk shows the chiral carbon atom and the asymmetric carbon atoms marked by .alpha. and .beta. have both R or S configuration is described.

Abstract: A process for the preparation of 5-amino-1,3-dioxanes of formula (I), comprising the catalytic hydrogenation of the new oximes of formula (II) is described.

Abstract: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure ##STR1## including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2;R.sup.x is H, alkyl, aryl or halogen;A is(1) a bond;(2) --O--; or(3) ##STR2## B is: ##STR3## and wherein L.sup.2, L.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.3', R.sup.3a, R.sup.3b, R.sup.4, R.sup.4', R.sup.5, X, ##STR4## are as defined herein.

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention.

Abstract: Described herein is a process for the preparation of 5-amino-1,3-dioxanes of formula (I), wherein R and R.sub.1 have the meanings reported in the description, comprising the catalytic hydrogenation of the new oximes of formula (II).

Abstract: A process for the preparation of Iopamidol and 5-amino-2,2-dialkyl-1,3-dioxanes of formula ##STR1## wherein R and R.sub.1 are the same or different and represent a straight or branched C.sub.1 and C.sub.2 alkyl group or together with the carbon atom to which they are bonded, form a C.sub.5 -C.sub.6 cycloaliphatic ring; comprising the transformation of a 2,2-dialkyl-1,3-dioxane-5-carboxylic acid ester of formula ##STR2## wherein R.sub.2 represents a straight or branched C.sub.1 -C.sub.2 alkyl group, a phenyl optionally substituted by nitro groups or a benzyl; by treatment with ammonia into the corresponding amides and the subsequent rearrangement of the latter into the compounds of formula I, by treatment with a hypohalogenite. The resultant ketals may be used as is, or be converted to 2-amino-1,3-propanediol, and reacted with 5-amino-2,4,6-triiodo-isophthalic acid dichloride or, alternatively,L-5-(2-acetoxy-propionylamino)-2,4,6-triido-isophthalic acid dichloride, to produce Iopamidol.

Abstract: Provided by the present invention is a process for the biocatalytic synthesis of optically pure sphingosines from achiral starting material. The stereoisomers of sphingosine are prepared from chiral arene diols using stereospecific reaction techniques to obtain the desired sphingosine or derivative thereof.

Abstract: The invention relates to .DELTA..sup.8 - and .DELTA..sup.9 -prostaglandin derivatives of formula I, ##STR1## in which means the radicals or , R.sup.1 means ##STR2## COOR.sup.4 or CONHR.sup.5, R.sup.2 and R.sup.3 respectively mean a hydrogen atom or a hydroxy group, and the OH group can be respectively in alpha- or beta- position,means a CH.sub.2 group, an O or S atom,W means hydrogen, --OR.sup.6, halogen, --CN--, --NO.sub.2, trifluoromethyl or COOR.sup.6, and if R.sup.4 means hydrogen, their salts with physiologically compatible bases, the alpha-, beta- or gamma- cyclodextrin clathrates, as well as the compounds of formula I encapsulated with liposomes, process for their production and their pharmaceutical use.

Abstract: The present invention provides compounds having the formula ##STR1## wherein R.sub.1 is alkyl, alkenyl and alkynyl having from 2 to about 20 carbon atoms; R.sub.2, R.sub.3 and R.sub.6 are independently H, phenyl or alkyl having from 1 to about 20 carbon atoms; and R.sub.4 and R.sub.5 are independently H, R.sub.6 imino, or amidino, and pharmaceutically acceptable salts thereof which are useful for inhibiting protein kinase C and treating conditions related to, or affected by inhibition of protein kinase C, particularly cancer tumors, inflammatory disease, reperfusion injury, and cardiac dysfunctions related to reperfusion injury.

Abstract: The present invention provides a process for the preparation of N-cyanoimidocarbonates of the general formula: ##STR1## in which R.sup.1 and R.sup.2 are the same and are alkyl radicals containing up to 4 carbon atoms or R.sup.1 and R.sup.2 are joined together to give an ethylene or propylene chain which is optionally substituted by an alkyl radical containing up to 3 carbon atoms, wherein an imidocarbonate obtained in aqueous alkaline solution from the appropriate alcohol and cyanogen chloride is added with an acid to an aqueous solution of cyanamide in such a manner that the reaction mixture has a pH value of from 3 to 8.

Abstract: A ferroelectric liquid crystalline mixture containing at least one optically active compound of the general formula ##STR1## wherein X.sup.1 denotes a single covalent bond, --COO--, --OOC--, --CH.sub.2 CH.sub.2 --, --OCH.sub.2 -- or --CH.sub.2 O--; one of rings A.sup.1, A.sup.2 and A.sup.3 represents trans-m-dioxan-2,5-diyl and the other two of rings A.sup.1, A.sup.2 and A.sup.3 each independently represent unsubstituted 1,4-phenylene or 1,4-phenylene substituted with cyano, halogen or lower alkyl; R.sup.1 and R.sup.2 each independently signify an optionally halogen-substituted alkyl group with up to 18 carbon atoms in which optionally 1 CH.sub.2 group or 2 non-adjacent CH.sub.2 groups is/are replaced by --O--, --CO--, --COO-- and/or --OOC--,as well as novel compounds falling under formula I and ferroelectric electrode-optical indicating devices including same.

Abstract: A process for the preparation of tertiary N,N-dimethylamines by the reaction of primary amines, formaldehyde, and hydrogen under pressure and at elevated temperature in the presence of a nickel-containing hydrogenation catalyst in the liquid phase. The hydrogenation catalyst is suspended in a solvent, the nickel concentration is 0.1 to 10% by weight, based on the primary amine. The starting materials are separate from each other, brought to 80.degree. to 150.degree. C. and 1 to 15 MPa and fed into the catalyst suspension simultaneously with stirring and reacted in one step to form the tertiary N,N-dimethylamines.

Abstract: Ether-substituted isonitriles, Tc99m complexes thereof, and processes for myocardial tissue radioimaging using the Tc99m complexes.

Abstract: Optically active compounds of the formula I ##STR1## in which R.sup.1 is C.sub.1 -C.sub.4 -alkyl, phenyl or benzyl, R.sup.2 is a radical of the formula II or IIa ##STR2## in which R.sup.3 is H or --CH.sub.3, or R.sup.1 and R.sup.2 together form a radical of the formula ##STR3## in which R.sup.2 has the meaning given above; and * represents predominantly R or predominantly S configuration.The compounds can be polymerized to give homopolymers or copolymers. The compounds and the polymers can be complexed with iridium(I) salts in the presence of a diene. The complexes are suitable as enantioselective catalysts.

Abstract: A process of forming 2-amino-1,3-propanediol by reducing the compound, 5-nitro-1,3-dioxane and subsequently hydrolyzing the reduced compound.

Abstract: Unpurified 2-bromo-2-nitro-1,3-propanediol is used as the starting material for a process for the preparation of 5-bromo-5-nitro-1,3-dioxane from 2-nitro-1,3-propanediol without the use of an organic solvent on an industrial scale. This is carried out in such a way that in a first stage a mixture of bromine and aqueous hydrogen bromide solution is cooled and an aqueous solution of an alkali metal or an alkaline-earth metal salt of 2-nitro-1,3-propanediol is added at such a rate that, with cooling, the maximum reaction temperature does not exceed 30.degree. C., and then in a second reaction stage paraformaldehyde and sulfuric acid are added, left to react above room temperature, and the organic phase separated.

Abstract: The new esters derived from a chiral compound containing two OH groups and at least one mesogenic carboxylic acid which have the general formula (I) ##STR1## in which X.sup.1 =O--H or O--CO--(C.sub.1 to C.sub.12)alkyl and X.sup.2 =O--MC or X.sup.1 and X.sup.2 denote O-MC independently of each other, where MC is the molecular radical of a mesogenic monocarboxylic acid after splitting off an OH group.The esters or esters substituted in the aromatic part of the phenolic part preferably find application as an admixture intwistable liquid crystal phases in which they produce a temperature compensation and a high degree of twisting.

Abstract: Sulfur-containing bis-amino carbamate compounds exhibit outstanding acaricidal, nematocidal and insecticidal activity.

Abstract: Compounds of the formula IR.sup.1 --A.sup.1 --Z.sup.1 --A.sup.2 --R.sup.2 IwhereinR.sup.1 and R.sup.2 are each H, an alkyl, alkoxy, alkanoyl, alkanoyloxy or alkoxycarbonyl group with in each case 1-10 C atoms, F, Cl, Br, CN or R.sup.3 --A.sup.3 --Z.sup.2 --,A.sup.1 is --A--, --A.sup.4 --A--or --A--A.sup.4 --,A is a 1,3-dioxane-2,5-diyl or a 1,3-dithiane-2,5-diyl group,A.sup.2, A.sup.3 are each a 1,4-cyclohexylene, 1,3-dioxane-2,5-diyl,and A.sup.4 1,3-dithiane-2,5-diyl, piperidine-1,4-diyl or 1,4-bicyclo(2,2,2)octylene group, or a 1,4-phenylene, pyrimidine-2,5-diyl or pyridazine-3,6-diyl group which is unsubstituted or substituted by one or two F and/or Cl atoms and/or CH.sub.3 groups and/or CN groups,Z.sup.1 and Z.sup.2 are each --CO--O--, --O--CO--, --CH.sub.2 CH.sub.2 --, --OCH.sub.2 --, --CH.sub.2 O or a single bond andR.sup.3 is H, an alkyl, alkoxy, alkanoyl, alkanoyloxy or alkoxycarbonyl group with in each case 1-10 C atoms, F, Cl, Br or CN, with the proviso that(a) at least one group A.sup.2, A.sup.

Abstract: New compounds of the general formula: ##STR1## wherein the symbols X stand for carbon atom bonded with two hydrogen atoms /--CH.sub.2 -- group/ and the symbols Z stand for oxygen atom or the symbols X stand for oxygen atom and the symbols Z stand for carbon atom bonded with two hydrogen atoms /--CH.sub.2 -- group/, m is an integer of 1 to 2, R represents an alkyl /H.sub.2n+1 C.sub.n / or an 4-alkylphenyl /H.sub.2n+1 C.sub.n --C.sub.6 H.sub.4 / or an alkylbiphenyl /H.sub.2n+1 C.sub.n --C.sub.6 H.sub.4 --C.sub.6 H.sub.4 / or an alkylcyclohexylphenyl group /H.sub.2n+1 C.sub.n --C.sub.6 H.sub.10 --C.sub.6 H.sub.4 /, the term alkyl group signifies an alkyl chain containing 1 to 15 carbon atoms or it also signifies a branched-chain alkyl group C.sub.2 H.sub.5 --CH/CH.sub.3 /--/CH.sub.2 /.sub.k where k in an integer of 1 to 3, have utility as liquid crystals. A process for manufacture of compounds of the general formula I.

Abstract: Quaternary ammonium salts exhibiting strong antimicrobial activity are disclosed along with the method of using them as antimicrobial agents. The salts having the formulas I or II: ##STR1## wherein R is C.sub.1-20 alkyl, C.sub.5-7 cycloalkyl or an aralkyl group, R.sup.

Abstract: Herbicide antidote compounds having the formula: ##STR1## in which R is haloalkyl wherein halo is chlorine, bromine or iodine and the alkyl group has 1-4 carbon atoms, inclusive;R.sub.1 is selected from the group consisting of hydrogen; lower alkyl having 1-4 carbon atoms, inclusive; alkenyl having 2-4 carbon atoms, inclusive; and phenyl;R.sub.2 is selected from the group consisting of hydrogen and lower alkyl having 1-4 carbon atoms, inclusive;R.sub.3 is selected from the group consisting of hydrogen and lower alkyl having 1-4 carbon atoms, inclusive;R.sub.4 is selected from the group consisting of hydrogen and a nitro group; andeither R.sub.3 is hydrogen or R.sub.4 is hydrogen.

Abstract: New polyhalogenoaromatic compounds of Formula I ##STR1## wherein Y and Z are each independently alkyl, alkoxy or alkanoyl each of 1 to 12 C atoms, --COOR.sup.1, --O--CO--R.sup.1, CN, NO.sub.2, NH.sub.2 or OH;Q is one or two identical or different radicals selected from Ph, Cy, 1,4-bicyclo[2,2,2]octylene or 1,3-dioxane-2,5-diyl;X.sup.1 to X.sup.4 are each independently H, F, Cl or Br;R.sup.1 is alkyl of 1 to 4 C atoms, Ph--R.sup.2 or Cy--R.sup.2 ;R.sup.2 is alkyl or alkoxy each of 1-12 C atoms or CN;Ph is 1,4-phenylene; and Cy is 1,4-cyclohexylene,can be used as components of liquid-crystal dielectrics.

Abstract: Unsymmetrical N-substituted bis-carbamoyl sulfide compounds exhibit exceptional broad spectrum pesticidal activity coupled with extremely low mammalian toxicity and phytotoxicity.

Abstract: A method of increasing the yield of legumes (soybeans) utilizing a compound of the formula ##STR1## where R is chloromethyl or dichloromethyl; R.sup.1 is lower alkyl, vinyl or phenyl; R.sup.2 is hydrogen or lower alkyl and R.sup.3 is hydrogen or lower alkyl.

Abstract: Carbamate-sulfenyl-carba moyl fluoride compounds are valuable insecticidal compositions and are also useful intermediates in the production of bis-carbamate compounds.

Abstract: Novel carbamates derived from substituted cyclic .beta.-keto-alcohols, their preparation, and pharmaceutical formulations which contain these compounds and which may be used as hypnotics in the treatment of sleep disturbance and as sedatives.

Abstract: An improved process is disclosed for sulfenylating carbamates in the presence of a solvent and acid acceptor, in which the reaction between a carbamate and a sulfenyl halide is conducted in the presence of a catalytic amount of a complex of a lower alkylamine and sulfur dioxide. Several methods for preparing and utilizing the complex in the reaction are disclosed and exemplified.