Abstract: There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine.

Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: 1

Abstract: This invention provides a progesterone receptor antagonist of formula 1 having the structure 1

Abstract: This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.

Abstract: The present invention relates to quinolonecarboxylic acid derivatives having more excellent and broad antibacterial activities than the existing quinolone-series antibiotic. More specifically, it pertains to novel quinolonecarboxyllic acid derivative represented by following formula 1, which have a derivative of 7-[8-(alkoxyimino)-2,6-diazaspiro[3.

Abstract: The present invention discloses compounds of formula (I), or a pharmaceutically acceptable salt thereof; wherein n is 1 or 2 or 3, A is —O—, —S—, —CH—, —O—CH2—, or —CH2—O—; B is —O—, —S—, —CH2—, —0—CH2—, or —CH2—O—; and C is N, or —CR1—; D is N, or —CR2—; E is N, or —CR3—; and F is N, or —CR4—; wherein R1, R2, R3 and R4 each independently are selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl and a monocyclic 5 to 6 membered heteroaryl group. The compounds of the invention are useful for the treatment of disorders or diseases responsive to the activity of nicotinic ACh receptor modulators.

Abstract: The present invention relates to photochromic 2H-naphtho[1,2-b]pyrans as well as their use in synthetic resins of all types, especially for ophthalmic purposes. In particular, the present invention relates to photochromic naphthopyran compounds, for which a further ring system is bonded to the f side of the naphthopyran. The inventive photochromic dyes generally have the general formula (I) wherein n, R1, R2, R3, X, B and B′ are defined as in claim 1. The inventive compounds are distinguished by good darkening and decolorizing properties and a very good service life.

Abstract: Compounds or compositions containing compounds of the formula A-(X1—NO2)to or salts thereof, for the preparation of antithrombotic medications wherein “to” is the integer 1 or 2X1 is an alkylene connecting bridge and “A” is the residue of timolol or analapril.

Abstract: Compounds having platelet anti-aggregating activity and antihypertension activity having reduced branchial side effects.

Abstract: The present application describes inhibitors of factor Xa of formula I: or pharmaceutically acceptable salt forms thereof, wherein W, W1, W2, and W3 may be N or C and J, Ja, and Jb combine to form a substituted carbocycle or heterocycle.

Abstract: The present invention relates to compounds of the formula ##STR1## wherein X is --O-- or --CH.sub.2 --;Y is --C(O)--, --(CH.sub.2).sub.n -- or --N(CH.sub.3)--;n is 1 or 2 orX and Y taken together are --CH.dbd.CH--Z is --NH--, --CH.sub.2 --, --O-- or .dbd.CH--;A.sup.1 is a group ##STR2## B is --(CH.sub.2).sub.m --; m is 0, 1 or 2;R.sup.1 and R.sup.2 are each independently hydrogen or lower alkyl;R.sup.3 is hydrogen or halogen;R.sup.4 is hydrogen or hydroxy andthe dotted line is (--CH.sub.2 --CH.sub.2 --).sub.n, and n' is 0 or 1 and to pharmaceutically acceptable acid addition salts thereof.The compounds of the present invention are antagonists of the OFQ receptor.

Abstract: The present invention relates to compounds of formula (I), ##STR1## wherein R.sup.1 represents halogen, hydroxy, C.sub.1-6 alkyl group optionally substituted by one or three fluorine atoms, C.sub.1-6 alkoxy group optionally substituted by one to three fluorine atoms, or C.sub.1-6 alkylthio optionally substituted by one to three fluorine atoms; R.sup.2 represents hydrogen, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or when R.sup.2 is adjacent to R.sup.1, they may be joined together such that there is formed a 5- or 6-membered saturated or unsaturated ring containing one or two oxygen atoms; R.sup.3 represents an optionally substituted 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms, selected from nitrogen, oxygen and sulphur; m is 0-3 and n is 0-3, with the proviso that the sum total of m+n is 2 or 3; p is zero or 1; q is 1 or 2; and when m is 1 and n is 1 or 2, the broken line represents an optional double bond; R.sup.4, R.sup.5, R.sup.6, R.sup.9 and R.sup.

Abstract: Compounds of formula (I) ##STR1## and the salts of these compounds, are efficacious PDE (phosphodiesterase) inhibitors.

Abstract: The invention provides compounds of formula ##STR1## as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases.Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.

Abstract: Disclosed are spiro-substituted azacycles of formula I are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma. In particular compounds of formula I are shown to be neurokinin antagonists.

Abstract: A process for synthesizing N-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine derivatives of the following formula (I): ##STR1## in which the definition of R has the same meaning as given in the description by using a sulfite derivative to activate the C-terminus of the three dimensional structure of an amino acid of N-[1-(S)-ethoxycarbonyl-3- phenylpropyl]-L-alanine, which can effectively couple with another amino acid to form a dipeptide of formula (I). The compound of fomula (I) is an inhibitor of ACE.

Abstract: Novel piperidine derivatives of formula (I), processes for their preparation, pharmaceutical compositions containing them and their use as medicaments for the treatment of CNS disorders are disclosed.

Abstract: Novel amide derivatives of formula (I), processes for their preparation, pharmaceutical compositions containing them and their use as medicaments are disclosed.

Abstract: There is disclosed a process for the preparation of compounds having ACE inhibitory action of the formula ##STR1## wherein R has the meanings as in claim 1, wherein the stereospecific amino acid N-?1-(S)-ethoxycarbonyl-3-phenylpropyl!-L-alanine is carboxylically activated with a thionyl chloride derivative wherein at least one chlorine atom is replaced by the residue of a heterocyclic ambident compound such as imidazole, benzimidazole, 2-methylimidazole or triazole, especially chlorothionylimidazole or thionyldiimidazole, in the presence of an organic solvent to the intermediate novel compound A or to the intermediate novel compound B and the obtained intermediate compound is reacted with an amino acid, preferably in the monosilylated form, most preferably in the disilylated form. Disclosed are also novel compounds useful as starting materials or intermediates in the present process.

Abstract: Present invention provides ionic spiropyran compounds having a C10-C22 alkyl group or groups at the 1'- and/or 8-positions of 3',3'-dimethyl-6-nitrospiro?2H-1-benzopyran-2',2'-indoline! and a composite material made by conjugating the said ionic spiropyrans with clay mineral, the said composite material being capable of forming a transparent thin film which is photo-interconvertible between the said spiropyrans and the corresponding merocyanines.

Abstract: The present invention relates to spiro?3H-indole-3(2H),3'-pyrrolidine! derivatives of general formula I ##STR1## as defined in the description. The invention also relates to a process for their preparation and to their therapeutic use, in particular for the treatment of complaints associated with melatonin disorders, and to the pharmaceutical and cosmetic compositions comprising them.

Abstract: To produce defined isomer mixtures of compounds with spirocyclic beta-aminocarboxyl and/or beta-aminocarbonyl systems the invention supposes that they be dissolved in solvents which have good dissolving power for these compounds, whose relative permittivity is sufficient to stabilize the amphoteric intermediates occuring in isomerization, which as proton donors constitute hydrogen bridges, whose basicity is less than that of the compounds for isomerization and whose boiling point is so high that an adequate reaction speed can be attained by raising temperature. Further, the invention proposes that the isomerization be prevented, influenced, or terminated by altering at least one of these factors and or by altering the temperature.

Abstract: Spirocycles of general structural formula: ##STR1## are Class III antiarrhythmic agents.

Abstract: The invention relates to new 1H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A, B, X, Y and G have the meanings given in the description, to a plurality of processes for their preparation, and to their use as pesticides.

Abstract: A naphthopyran compound of general formula (I) ##STR1## wherein R.sub.1 represents a group of the formula --NR.sub.2 R.sub.3 wherein each of R.sub.2 and R.sub.3, which may be the same or different, independently represents an alkyl group, or a carbocyclic or heterocyclic group, or R.sub.2 and R.sub.3 taken together with the nitrogen atom to which they are attached represent a heterocyclic ring having one or more hetero atoms and which may optionally carry at least one substituent selected from alkyl, aryl, or heteroaryl groups; each of R.sub.4 and R.sub.5, which may be the same or different, independently represents an alkyl, alkenyl, carbocyclic or heterocyclic group, or R.sub.4 and R.sub.5 taken together with the carbon atom to which they are attached form a carboxylcyclic ring or a heterocyclic ring; and R.sub.6 represents a hydrogen atom or a substituent selected from alkyl, alkoxy, aryl, aryloxy, heteroaryl, halogen, a group of formula R.sub.

Abstract: Photochromic products belonging to the group of chromenes having general formula (I): ##STR1##

Abstract: The present invention relates to a spiropyran compound represented by the formula (1); an optically active spiropyran compound wherein an asymmetric center is introduced on a spirocarbon; and optical functional materials using these compounds, ##STR1## wherein R.sup.1 is alkyl group having 1 to 20 carbon atoms, aralkyl group, hydroxyethyl group, methacryloxymethyl group or methacryloxyethyl group; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and are each hydrogen atom, alkyl group having 1 to 6 carbon atoms, aryl group, aralkyl group, alkoxy group having 1 to 5 carbon atoms, hydroxymethyl group, carboxyl group, halogen atom, amino group, cyano group, trichloromethyl group, trifluoromethyl group or nitro group; R.sup.6 and R.sup.7 are the same or different and are each hydrogen atom, alkyl group having 1 to 6 carbon atoms, aryl group, aralkyl group, halogen atom, cyano group or nitro group; R.sup.

Abstract: The present invention provides a novel photochromic material which is capable of forming two kinds of aggregates, each having a sharp absorption peak at a different wavelength. The photochromic material comprises a spiropyran compound represented by the following general formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently alkyl groups each containing 1 to 30 carbon atoms, and R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are independently selected from the group consisting of hydrogen, an amino group, an alkoxy group with 1 to 5 carbon atoms, and an alkylamino group with 1 to 5 carbon atoms with the proviso that at least one of R.sup.3, R.sup.4, R.sup.5, and R.sup.6 is an amino group, an alkoxy group or an alkylamino group.

Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R.sub.1, R.sub.2, R.sub.3, A and m are as defined in the description.Medicinal product which is useful for treating depression and anxiety.

Abstract: The object of the invention is to provide a novel compound exhibiting stable photochromism.The invention is directed to a transition metal-spirobenzothiopyran complex of the general formula ##STR1## wherein R.sup.1 for example be C.sub.1-20 alkyl; R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 independently may mean hydrogen; Y means O or S; M may for example be Cr, and a process for producing the complex.

Abstract: Novel peptoids of .alpha.-substituted Trp derivatives useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further the compounds are antianxiety agents and antiulcer agents. They are agents useful for preventing the response to withdrawal from chronic treatment or use of nicotine, diazepam, alcohol, cocaine, caffeine, or opioids. The compounds are also useful in the treatment and/or prevention of panic attacks. Also disclosed are pharmaceutical compositions and methods of treatment using the peptoids as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds to prepare diagnostic compositions.

Abstract: The present invention provides a spiropyran compound represented by the formula ##STR1## wherein R.sup.1 is alkyl having 1 to 20 carbon atoms or aralkyl, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and are each a hydrogen atom, alkyl having 1 to 6 carbon atoms, aryl or aralkyl, alkoxyl having 1 to 5 carbon atoms, halogen atom, cyano, trichloromethyl, trifluoromethyl or nitro, R.sup.6 and R.sup.7 are the same or different and are each a hydrogen atom, alkyl having 1 to 6 carbon atoms, aryl or aralkyl, halogen atom, cyano or nitro, X is an oxygen atom or sulfur atom, Y is Se or (CH.sub.3).sub.2 C<, Z is ##STR2## and X is a sulfur atom when Y is (CH.sub.3).sub.2 C<. The spiropyran compound of the present invention itself is usable as a material such as recording material, photosensitive material, optical filter or decorative material.

Abstract: Novel photochromic spiropyran compounds having an absorption sensitivity in a longer wavelength region than known photochromic compounds are provided. The novel spiropyran compounds have a spiropyran skeleton having a methoxy group at the 6 position, a nitro group at the 8 position, a bromine atom at the 5' and 7' positions, and an alkyl group at the 1' position.

Abstract: Substituted 4,5-dihydrothieno[2,3-b]thiophene-2-sulfonamides and 6,6-dioxides thereof are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.

Abstract: The present invention provides a photochromic material possessing absorption sensitivity in a longer wavelength region when compared with conventional photochromic materials.

Abstract: Antibacterial 5-alkylquinolonecarboxylic acids of the formula ##STR1## in which R.sup.3 is C.sub.1 -C.sub.4 -alkyl,R.sup.1 is optionally substituted alkyl or cycloalkyl, alkenyl, alkoxy, amino or alkylamino or optionally substituted phenyl,R.sup.2 is hydrogen or optionally substituted alkyl,R.sup.4 is a nitrogen-containing heterocyclic radical, andA is hydrogen, halogen, methyl, cyano or nitro, or forms a bridge with R.sup.1.and hydrates and salts thereof.

Abstract: Novel antibacterial compounds are disclosed having the formula ##STR1## as well as pharmaceutically acceptable salts, esters, amide and prodrugs thereof,wherein R.sup.1 is selected from the group consisting of (a) lower alkyl, (b) halo(lower alkyl), (c) lower alkyl(alkynyl), (d) lower cycloalkyl, (e) lower alkylamino, (f) nitrogen-containing aromatic heterocycle, (g) bicyclic alkyl and (h) phenyl;R.sup.2 is selected from the group consisting of hydrogen, lower alkyl, a pharmaceutically acceptable cation, and a prodrug ester group;R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen, halogen, amino, and lower alkyl;R.sup.5 is either a nitrogen-containing heterocycle or a nitrogen-containing spiro-bicyclic-heterocycle; andA is N or C--R.sup.6, wherein R.sup.6 is selected from the group consisting of hydrogen, halogen, lower alkyl, and lower alkoxy, or R.sup.1 and R.sup.

Abstract: Compounds of the formula ##STR1## in which R.sup.1 /R.sup.2 are alkyl, cycloalkyl, aralkyl or alkylene,R.sup.3 is alkyl, cycloalkyl or aralkyl,Z is alkylene,X is O orare highly suitable as color formers in recording materials based on acid developers. They give yellow or orange hues which have excellent sublimation and light fastness.

Abstract: Compound of the general formula (I), which is useful as an agricultural and horticultural fungicide, an agricultural and horticultural fungicidal composition containing said compound, use of said composition for controlling plant disease, and process for the production of said compound: ##STR1## wherein ##STR2## shows a case in which R.sup.3 and R.sup.4 together form a cyclic substituent, and R.sup.1 and R.sup.4 are substituents disclosed in the specification.

Abstract: The invention relates to novel sulfobetaine-substituted .alpha.-sulfonylcarboxylic acids of the general formula I and to processes for the preparation thereof. As organic intermediates, the compounds according to formula I represent a reactive synthesis component having the character of a sulfobetaine and can be used for further syntheses. In the case of a long-chain alkyl radical R.sub.1, polyfunctional surfactants are obtained. According to the invention, molar quantities of diallylammonium chloride are reacted with chloroacetic acid and twice the molar quantity of sodium hydrogen sulfite in the presence of a catalytic quantity of a peroxodisulfate, and the reaction solution obtained is converted, after addition of a catalytic quantity of iodide, by heating into sulfobetaine-substituted .alpha.-sulfonylacetic acids according to the general formula I.

Abstract: A process for preparing photochromic spiropyran compounds having a halogen atom or atoms and a hydrophobic alkyl group wherein a starting photochromic spiropyran compound having the hydrophobic alkyl group is reacted directly with a halogenating agent in a solvent. This reaction efficiently proceeds with the product being obtained in high yield.

Abstract: Crosslinking reagents for amino group-containing compounds are provided, which crosslinkers can be cleaved under mildly acidic conditions. The crosslinkers can be used to crosslink biologically active substances to be delivered to the cells, wherein the crosslinker will be cleaved in the mildly acidic conditions within the cell.

Abstract: Squaraine dyes and compositions of matter containing such dyes are disclosed. The squaraine dyes have an absorption maximum greater than 600 nanometers and are particularly useful in conjunction with a helium/neon (He/Ne) laser. Some of the squaraine dyes are hydrophilic and are therefore water soluble or water compatible and others of the squaraine dyes are lipophilic.

Abstract: Disclosed are new 1,3-dioxenones having the formulae ##STR1## in an optically pure state, a process for preparing same and the use thereof.

Abstract: Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing action against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.

Abstract: Cyanatoaryl-substituted 1,6-diaza[4.4]spirodilactam having a cyanatoaryl-containing substituent on each spiro ring nitrogen atom self-cure upon application of heat to produce cured, crosslinked thermoset resins of high glass transition temperature.

Abstract: Compounds of the formulae: ##STR1## are useful as anti-hypertensives.

Abstract: A thermal imaging method is provided which comprises heating imagewise a di- or triarylmethane compound possessing within its di- or triarylmethane structure an aryl group substituted in the ortho position to the meso carbon atom with a moiety ring-closed on the meso carbon atom directly through a nitrogen atom, which nitrogen atom is also bound to a group with a masked acyl substituent that undergoes fragmentation upon heating to liberate the acyl group for effecting intramolecular acylation of said nitrogen atom to form a new group in the ortho position whereby the di- or triarylmethane compound is rendered colored in an imagewise pattern corresponding to said imagewise heating.

Abstract: The present invention provides a compound of formula I or a salt or prodrug thereof: ##STR1## wherein the dotted line represents an optional chemical bond in one of the two possible positions;A represents a group of formula II: ##STR2## in which R.sup.1 represents hydrogen, hydroxy, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkoxy, benzyloxy, hydroxy (C.sub.1-6)alkyl, halogen, amino, cyano, nitro, --CONR.sup.6 R.sup.7 or --SO.sub.2 NR.sup.6 R.sup.7, in which R.sup.6 and R.sup.7 independently represent hydrogen, halogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl;R.sup.2 represents hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or C.sub.1-6 alkylcarbonyl;V represents nitrogen, --CH or --C--; andW represents oxygen, sulphur or --NR.sup.8, in which R.sup.8 represents hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.

Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof, ##STR1## in which, R.sub.1 is hydrogen, lower alkyl or CH.sub.2 OR.sub.6 ;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is hydrogen or lower alkyl;each of W and Z, which are different, represents --CR.sub.4 R.sub.5 -- or --(CR.sub.x R.sub.y).sub.n --, in which,R.sub.4 is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkylthio or C.sub.1-3 alkoxy;R.sub.5 is C.sub.1-3 alkyl, C.sub.1-3 alkylthio or C.sub.1-3 alkoxy; or together R.sub.4 and R.sub.5 form a 3 to 6 membered carbocyclic ring, or a heterocyclic ring containing one or two ring oxygen, nitrogen or sulphur atoms;or R.sub.4 and R.sub.5 together form an oxo or methylene group;each of R.sub.x and R.sub.y is hydrogen or C.sub.1-3 alkyl; n is zero or 1;R.sub.6 is hydrogen, lower alkyl, lower alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heteroarylcarbonyl, optionally substituted aminocarbonyl, lower alkoxycarbonyl and aryloxycarbonyl;R.sub.