Abstract: An intermediate, useful in the conversion of FK-506 to FK-525 and analogous 23-membered ring macrolides, of the structure: ##STR1##

Abstract: A process for the preparation of isophorone nitrile utilizing solutions of lithium hydroxide or lithium cyanide, solid LiOH or solid LiOH.cndot.H.sub.2 O as a catalyst. The reaction is carried out under precisely controlled temperature conditions and cyanide feed rate profiles to maintain a reasonably constant concentration of non-reacted cyanide, thereby minimizing the formation of undesirable diisophorone, its nitrile derivative(s) and HCN polymers. A polyacidic acid can be used to acidify the batch, followed by filtration to remove the precipitated lithium salt of the acid, and vacuum distillation to remove liberated HCN and excess isophorone. The resulting isophorone nitrile is obtained in high yield and with low impurity content.

Abstract: Provided are the dialkyl amines: ##STR1## wherein Q is ##STR2## R is --CH.sub.3 or Q and a has a value of 1 to 3.

Abstract: Catechol derivatives which produce nerve growth factor in particular tissues of the brain are disclosed. These derivatives provide preventive and therapeutic effects for regressive disorders of the central nervous system including senile dementia of the Alzheimer type.

Abstract: Benzobisthiazole polymers with thiophene moieties having repeating units of the formula:--Bt--(--Tp--).sub.n --wherein Bt is ##STR1## Tp is ##STR2## and n has a value of 1 to 3.

Abstract: This invention relates to novel fluorinated bis-imides of the formula ##STR1## where X is H or F. The compounds are useful as additives to enhance the properties of high performance polymers such as polyimides.

Abstract: Non-peptidyl compounds characterized generally as imidazolyl/imidazolylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is imidazolyl or imidazolylmethyl; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 and R.sub.7 are taken together to form a partially saturated or fully saturated heterocyclic ring containing five to eight ring members with one or two ring members being oxygen atoms and the remaining ring members being carbon atoms, and which heterocyclic ring may be optionally substituted with lower alkyl; or a pharmaceutically-acceptable salt thereof.

Abstract: A process for producing a nitrile, which comprises subjecting an alkane and ammonia in the gaseous state to catalytic oxidation in the presence of an oxide of the formula:Mo.sub.a V.sub.b Te.sub.c Nb.sub.d X.sub.x O.sub.n ( 1)wherein X is at least one element selected from the group consisting of Mg, Ca, Sr, Ba, Al, Ga, Tl, In, Ti, Zr, Hf, Ta, Cr, Mn, W, Fe, Ru, Co, Rh, Ni, Pd, Pt, Zn, Sn, Pb, As, Sb, Bi, La and Ce,when a=1,b=0.01 to 1.0,c=0.01 to 1.0,d=0 to 1.0, andx=0.0005 to 1.0,and n is a number such that the total valency of the metal elements is satisfied.

Abstract: Compounds of the general formula I ##STR1## wherein R.sup.1 represents a halophenyl, dihalophenyl, nitrophenyl, cyanophenyl or trifluoromethylphenyl group;X represents a single bond, --CH.sub.2 --, --OCH.sub.2 --, SCH.sub.2, --S(O)--CH.sub.2 --, --S(O).sub.2 --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --R.sup.2 represents hydrogen or C.sub.1-3 alkyl;R.sup.3 represents a phenyl group substituted in the meta-position by a radical containing an organic base, an organic acid or a quaternary ammonium salt and optionally further substituted.R.sup.4 and R.sup.5 which may be the same or different each represents a C.sub.3-5 alkenyl, C.sub.3-5 alkynyl, C.sub.1-6 alkyl, or C.sub.4-7 cycloalkylalkyl group, or together with the intervening nitrogen atom represents a 4-7 membered heterocyclic ring, and the pharmaceutically acceptable salts thereof are useful for the treatment of hypertension and/or inflammation in the warm-blooded animals.

Abstract: The present invention provides a carbamoyl-2-pyrrolidinone compound which has the following formula (2) and is useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and cerebral metabolism activators or anoxic brain damage protectives ##STR1## wherein R.sup.1 is a hydrogen atom, hydroxyl or lower alkyl substituted or unsubstituted with hydroxyl, and R.sup.3 is phenyl, tetrahydronaphthyl, pyridyl or thiazolyl having or not having lower alkoxyl, lower alkylamino, a halogen atom or halogenomethyl as a substituent.Further, the present invention provides novel carbamoyl-2-pyrrolidinone compounds represented by the formula ##STR2## wherein R.sup.1 is a hydrogen atom, hydroxyl or lower alkyl substituted or unsubstituted with hydroxyl, and R.sup.2 is phenyl, tetrahydronaphthyl, pyridyl or thiazolyl having or not having methoxy or lower alkylamino as a substituent, provided that when R.sup.1 is a hydrogen atom or unsubstituted lower alkyl, R.sup.2 is not unsubstituted phenyl.

Abstract: A process for preparing perfluoro-oxyaziridines of formula: ##STR1## where R.sub.x is F, a C.sub.1 -C.sub.10 perfluoroalkyl group or a --NR.sup.f.sub.2 group in which R.sup.f is a C.sub.1 -C.sub.10 perfluoroalkyl group, R.sub.y is F or a C.sub.1 -C.sub.10 perfluoroalkyl group and R.sub.z is a C.sub.1 -C.sub.10 perfluoroalkyl group. The process consists in reacting the corresponding perfluoroimine with an aromatic peroxyacid having a benzenic nucleus, in an aprotic solvent, at a temperature ranging from -50.degree. to +100.degree. C.

Abstract: Compounds having the formula ##STR1## in which: R is C.sub.1 -C.sub.8 alkyl; or phenyl optionally substituted by 1 or 2 groups selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, nitro or halo;R.sub.1 is C.sub.1 -C.sub.4 alkyl or phenyl;R.sub.2 is C.sub.1 -C.sub.4 alkyl;R.sub.3 is C.sub.2 -C.sub.4 alkyl or allyl; andX is oxygen, sulfur or NR.sub.4 where R.sub.4 is hydrogen or C.sub.3 -C.sub.4 alkyl;provided that(i) if R.sub.1 is methyl, R is phenyl or substituted phenyl and(ii) if R.sub.3 is isopropyl, X is NR.sub.4, and R.sub.1 is alkyl; and their agriculturally acceptable salts are herbicides.

Abstract: A process for producing N.sup.2 -(1-(S)-carboxy-3-phenylpropyl)-L-lysil-L-proline of formula (VIII); ##STR1## N.sup.2 -(1-substituted-3-phenylpropyl)-L-lysil-L-proline derivative of formula (VII); ##STR2## and N.sup.2 -(1-carbonyl-3-phenylpropyl)-L-lysil-L-proline derivative of formula (XXVI); ##STR3## is disclosed.

Abstract: Sulpinine C, secopenitrem B and 10-oxo-11,33-dihydropenitrem B indole compounds have been isolated from the sclerotia of the fungi Aspergillus sulphureus. Aflatrem B has been isolated from the sclerotia of the fungi Aspergillus flavus, and 14-hydroxypaspalinine and 14-(N,N-dimethylvalyloxy)paspalinine have been isolated from the sclerotia of the fungi Aspergillus nomius. The indole compounds are effective for controlling Coleopteran and Lepidopteran insects.

Abstract: A novel compound is proposed which is effective in curing various complications as with catarat, retinopathy, neurotic disorder, and renal disorder. The thiazolidine-2,4-dione compound represented by the following general formula I combines an action to inhibit aldose reductase and an action to depress blood sugar and manifests an efficacy in the cure of various complications as with catarat, retinopathy, neurotic disorder, and renal disorder. ##STR1## wherein R.sup.1 is a hydrogen atom or a methyl group.

Abstract: Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.

Abstract: The 1,4-diaryl-1-cyclopropyl-4-substituted butane pesticides of the following formula are effective as insecticides and acaricides: ##STR1## in which X and Y are independently hydrogen, halogen, alkyl, alkoxy, cycloalkylalkoxy, alkylcarbonyl, alkoxycarbonyl, haloalkyl, haloalkoxy, alkylthio, haloalkylthio, alkylsulfinyl, alkylsulfonyl, trialkylamino, nitro, or cyano; or X and Y together are --OCH.sub.2 O-- or --OCF.sub.2 O-- bridging the 2-3 or 3-4 positions of the phenyl ring; Ar is 3-phenoxyphenyl, 4-fluoro-3-phenoxyphenyl, 6-phenoxypyridin-2-yl, or 2-methyl(1,1'-biphenyl)-3-yl;R is cyano, methyl, trifluoromethyl, alkenyl, alkynyl, or halogen.

Abstract: This invention relates to compounds of the formula: ##STR1## wherein R is an electron withdrawing group;R.sub.1 is H or COZ;X.sub.1 and X.sub.2 are independently H, lower alkyl, aryl, aryl lower-alkyl or polystyrene or R and X.sub.1 taken together with the carbon atoms to which they are attached form a ring containing from 4 to 15 ring carbon atoms and may contain up to 2 heteroatoms, wherein the heteroatoms are O, S, or N; andZ is an amino acid residue, a peptide residue or a leaving group. The compounds of the present invention are adaptable as blocking or protecting groups for an amine composition useful in peptide synthesis. The present invention is also directed to a method of protecting an amino group of an organic molecule during a reaction which modifies a portion of the molecule other than the protected amino group.

Abstract: The present invention discloses a new .alpha.-keto amide derivative or a salt thereof represented by the formula (1): ##STR1## wherein X represents (1) a peptide residue or amino acid residue in which the functional group may be protected, (2) a hydrogen atom or (3) an amino-protective group, Y represents a peptide residue or amino acid residue in which the functional group may be protected, E represents a substituent on the alkylene (C.sub.n H.sub.2n-1) and is a halogen, lower alkoxy or hydrogen, A represents a carbonyl group or mono- or di-substituted methylene (the substituent being a hydroxy, lower alkoxy, phenylimino or benzylimino), and n represents an integer of 2 to 6.The compound of the present invention is effective in inhibiting prolyl endopeptidase activity and useful as an active ingredient of an enzyme inhibitor.

Abstract: O-acylated derivatives of 1,5-dideoxy-1,5-imino-D-glucitol are disclosed that contain an N-alkyl or N-aroyl radical in which from one to four of the free hydroxyl groups are O-acylated with carboxylic alkanoyl radicals selected from the group consisting of .omega.,.omega.,.omega.-trifluoro alkanoyl having from three to eight carbon atoms, carboxylic cycloalkanoyl groups having from four to eight carbon atoms and carboxylic acyclic alkanoyl groups having from two to ten carbon atoms, wherein the N-aroyl radical is selected from the group consisting of p-decylbenzoyl, 3-(p-chlorophenoxy)propanoyl, 2-(acetyloxy)benzoyl, [1,1'-biphenyl]-4-ylcarbonyl, 2-thiopheneacetyl, trans-3-furanacryloyl 3-methoxyphenylacetyl and 3-(trifluoromethyl)benzoyl, and wherein the N-alkyl contains from one to fourteen carbon atoms, provided that when N-alkyl contains from one to five carbon atoms the O-acylated groups are .omega.,.omega.,.omega.-trifluoro alkanoyl or carboxylic cycloalkanoyl.