Abstract: Disclosed are compounds of the formula 1

Abstract: Photochromic pyran compounds and their use in synthetic resin objects of all types, especially for ophthalmic applications, particularly spiro compounds having a fluorene structure derived from naphthopyrans, which are known as spirofluorenopyrans. By introducing respectively only one strongly electron donating or withdrawing group at specific positions in the periphery of the pyran dye, photochromic compounds obtained which in the excited state are distinguished by an expanded color spectrum, while simulataneously offering comparably good bleaching rates and good durability.

Abstract: Compounds represented by the formula: 1

Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure: 1

Abstract: Compounds useful in the inhibition of HIV integrase, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines are described. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. The culture Actinoplanes sp. MA7220 (ATCC 202188) is also disclosed, as well as processes for making compounds of the present invention employing the culture.

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.

Abstract: A photochromic compound having a high color-developing sensitivity, a large fading rate and good durability of photochromic property. A novel chromene compound is, for example, represented by the following formula, and in which, as a basic structure, a condensed ring having a particular divalent group bonded to carbon atoms at the fourth and fifth positions of a fluoreno group is spiro-bonded to the first position of an indene ring, a particular divalent group is bonded to carbon atoms at the fifth and sixth positions of a chromene ring to form a condensed ring, and particular substituents are bonded to a carbon atom at the second position of the chromene ring.

Abstract: Disclosed are naphthopyran-type compounds having a pyrrole group annelated in position 5.6, as well as compositions and particularly (co)polymer matrices containing them. These compounds, compositions, and matrices have photochromic properties. These [pyrrole]naphthopyran compounds have the general formula: Articles containing these photochromic compounds, such as ophthalmic and/or solar glasses, lenses, glazing, devices, and the like, are also disclosed.

Abstract: Dibenzazole compounds having the general structure: ##STR1## wherein; R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 are independently H or a substituent which aids in solubility of the compound or which provides a linker arm for linking the compound to another moiety; Y is H or a cleavable moiety; X is a hydrogen, halogen, CF.sub.3, or SO.sub.3 H; V and W are oxygen or sulfur; Z is --C.dbd.C--, --C.tbd.C-- or an aromatic ring moiety; and n is 0, 1, or 2. When n=0 at least one of R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 is a substituent which aids in solubility of the compound or which provides a linker arm for linking the compound to another moiety or X is a halogen, CF.sub.3 or SO.sub.3 H. These compounds are highly fluorescent and can be easily detected using a fluorometer. Derivatives in which the Y group is a substituent other than H contain a fluorescence inhibiting chemical moiety that upon removal restores the fluorescence of the compound.

Abstract: The present invention describes xanthene dyes, including rhodamines, rhodols and fluoresceins that are substituted one or more times by a sulfonic acid or a salt of a sulfonic acid. The dyes of the invention, including chemically reactive dyes and dye-conjugates are useful as fluorescent probes, particularly in biological samples.

Abstract: A novel fulgimide compound in which the nitrogen atom of the imide ring is substituted by a phenyl group having an electron-attracting group at least at the meta position, which is represented by the following general formula (I): ##STR1## [wherein the group (a) of the following formula is a divalent aromatic hydrocarbon group or unsaturated heterocyclic group, each of which may have a substituent(s); ##STR2## the group (b) of the following formula is a norbornylidene, bicyclo[3.3.1]nonylidene or adamantylidene group, ##STR3## and R.sup.2 is an electron-attracting group] and its use as a photochromic material.The fulgimide compound of the present invention has a higher color density in a color-developed state than conventional photochromic compounds.

Abstract: A thiopyran derivative represented by the following formula (I) or (I'), or the salt thereof. ##STR1## wherein A is S or --CH.dbd.CH--; the dotted line indicates that the bond may be either present or absent; Z and Z' are typically ##STR2## L is an ethylene or trimethylene group; Y is CH or N; n is 2; B is a carbonyl group; m is 0 or 1; D is a phenyl group; and E.sub.1 and E.sub.2 are hydrogen atoms. These compounds exhibit a strong serotonin-2 blocking action and highly safe. Some compounds also exhibit an .alpha..sub.1 -blocking action and therefore are useful as an antihypertensive agent with less side effects. Thus, the thiopyran derivatives are useful as drugs for the treatment of circulatory diseases in general such as hypertension, ischemic heart disease, cerebrovascular disturbance, and peripheral circulatory disturbance.

Abstract: Tetralone derivatives of the formula ##STR1## where R.sup.1 is halo, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, (aryl)alkenyl, (aryl)alkynyl, alkoxy, O-alkenyl, O-aryl, O-alkyl(heterocyclo), COO-alkyl,alkanoyl, CO-amino, CO-substituted amino, alkyl-CO-amino, alkyl-CO-substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-alkyl(heterocyclo), N(alkyl)CO-alkyl, N(alkyl)CO-aryl, N(alkyl)CO-heterocyclo, N(alkyl)CO-alkyl(heterocyclo);R.sup.2 is hydrogen, alkyl, halo, aryl, alkoxy, amino, substituted amino;R.sup.3 is oxo, hydroxy, alkoxy, O--COalkyl, --O--COaryl, --O--COheterocyclo, NOH, NO-alkyl, N-amino, N-substituted amino, N-NHCONHalkyl, N-NHSO.sub.2 alkyl, N-NHSO.sub.2 aryl, amino, substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-heterocyclo, spiroheterocyclo;R.sup.4 is hydrogen, alkyl, alkyl(COalkyl), alkyl(COOalkyl); orR.sup.3 and R.sup.4 taken together with the atoms to which they are attached form a five- to seven-membered ring which can contain up to three heteroatoms selected from oxygen, nitrogen and sulfur;R.sup.

Abstract: A thiopyran derivative represented by the following formula (I) or (I'), or the salt thereof. ##STR1## wherein A is S or --CH.dbd.CH--; the dotted line indicates that the bond may be either present or absent; Z and Z' are typically ##STR2## L is an ethylene or trimethylene group; Y is CH or N; n is 2; B is a carbonyl group; m is 0 or 1; D is a phenyl group; and E.sub.1 and E.sub.2 are hydrogen atoms. These compounds exhibit a strong serotonin-2 blocking action and highly safe. Some compounds also exhibit an .alpha..sub.1 -blocking action and therefore are useful as an antihypertensive agent with less side effects. Thus, the thiopyran derivatives are useful as drugs for the treatment of circulatory diseases in general such as hypertension, ischemic heart disease, cerebrovascular disturbance, and peripheral circulatory disturbance.

Abstract: Diphenyl-cyclopropene derivatives, their nontoxic, pharmaceutically acceptable acid addition salts and compositions are kapa opiods useful in the treatment of pain, inflammation, Parkinsonism, dystonia, cerebral ischemia, diuresis, asthma, psoriasis, irritable bowel syndrome and stroke.

Abstract: Compounds of formula I: ##STR1## wherein R.sub.1 and R.sub.2 have any of the values defined in the specification, and their pharmaceutically acceptable salts, are PKC activators and are useful for treating diseases, such as, for example, cancer. Also disclosed are pharmaceutical compositions comprising compounds of formula I, processes for preparing compounds of formula I, and intermediates useful for preparing compounds of formula I.

Abstract: Use of spiro compounds of the formula (I) ##STR1## where K.sup.1 and K.sup.2 are, independently of one another, conjugated systems, in electroluminescence devices.Preferred compounds of the formula (I) are 9,9'-spirobifluorene derivatives of the formula (II) ##STR2## where the benzo groups can be substituted independently of one another. Compounds of the formula (I) have a good solubility in customary organic solvents, improved film-forming properties and a significantly reduced tendency to crystallize. The production of electroluminescence devices is thereby made easier and their service life is increased.

Abstract: We have found that indoles of structural formula (III): ##STR1## can be cost-effectively synthesized in high yield by the palladium-catalyzed coupling/ring closure of a 2-halo- or 2-trifluoromethylsulfonyl-aniline and a cyclic ketone derivative. The process of the present invention is particularly useful to form indoles containing acid-labile substituents such as triazole, acetyl, ketal, cyano, and carbamate, or indoles having a good leaving group in the benzyl position. The advantages of the present process are that it does not require the use of triphenyl phosphine or tetrabutyl ammonium chloride or lithium chloride.

Abstract: N-Substituted cyclic imides are obtained by reacting a cyclic acid anhydride with an amine in the presence of a solvent and an acid catalyst at 80.degree. to 200.degree. C. and with removal of the water formed, it being particularly advantageous to carry out this reaction in the presence of a stabilizer and an inert, dipolar aprotic cosolvent, optionally to add an inert organic solvent of low or zero polarity to the reaction mixture present after the reaction, to add a non-aqueous base in an amount of 0.5 to 50% by weight, based on the cyclic anhydride of the formula (II) used, and to separate off the precipitate formed to give a filtrate containing the N-substituted cyclic imide.

Abstract: By using the fluoran compound represented by the following general formula (I); ##STR1## wherein R.sup.1 is alkyl containing 1 to 4 carbon atoms, R.sup.3 is alkyl containing 1 to 8 carbon atoms, R.sup.4 is hydrogen or alkyl containing 1 to 8 carbon atoms, or R.sup.3 and R.sup.4 may bond with each other to form a ring together with a N atom, R.sup.2 is alkyl containing 1 to 4 carbon atoms, and n denotes 0, 1 or 2, however, the substituents represented by R.sup.2 may be different with each other when n is 2, as a color former for color forming recording materials, recording materials which have excellent properties in whiteness of the background of the material under light and in photostability of color-formed images on the materials as well as in sufficient color forming capability of the material even after having exposed them to light, can be provided.

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: Derivatives of 2,3-dihydro-5-benzofuranol, intermediates thereof, and processes useful for their preparation. These compounds are free radical scavengers and are useful in the treatment of conditions capable of being treated by free radical scavengers, such as stroke, nervous system trauma and reperfusion damage.

Abstract: A process for preparing a 1,1-disubstituted-1H-benzo?e!indole compound represented by formula (III) comprising reacting a 2-naphthol compound represented by formula (I), a carbonyl compound represented by formula (II), and a hydrazine compound in the presence of an acid catalyst, ##STR1## wherein R.sup.1 represents a group capable of substituting a hydrogen atom on the naphthalene ring; m represents 0 or an integer of 1 to 6; R.sup.2 and R.sup.3 each represents an alkyl group, an aryl group or a heterocyclic group; and R.sup.4 represents a hydrogen atom, an alkyl group, an aryl group or a heterocyclic group.

Abstract: The invention relates to compounds of formula (I). ##STR1## or a salt, or metabolically labile ester thereof wherein R.sub.1 represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy, trifluoromethyl, trifluoromethoxy, nitro, cyano, SO.sub.2 R.sub.3 or COR.sub.3 wherein R.sub.3 represents hydroxy, methoxy, or amino; m is zero or an integer 1 or 2;A represents an ethynyl group or an optionally substituted ethenyl group;X represents a bond or a C.sub.1-4 alkylene chain;R.sub.2 represents a bridged cycloalkyl or bridged heterocyclic group; which are antagonists of excitatory amino acids, to processes for their preparation and to their use in medicine.

Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds fused on the naphtho-portion of the naphthopyran ring with an indeno group or certain heterocyclic substituents. Certain substituents are also present at the 2 and 5 positions and sometimes at the 6 position of the naphthopyran ring. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.

Abstract: Described are novel reversible photochromic 3H-naphtho[2,1-b]pyran compounds, of the following graphic formula: ##STR1## wherein R.sub.1 is hydrogen or alkyl, R.sub.2 is hydrogen or preferably a carboalkoxy group and R.sub.3 is hydrogen or preferably an alkyl group, provided that either R.sub.1 or R.sub.2 is hydrogen, and B and B' are the aryl groups phenyl or naphthyl, a heterocyclic aromatic group or together form a spiro adamantylene group. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(oxazine) type compounds, are also described.

Abstract: Aminocyclohexylester compounds, including thioesters, are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the blockade of ion channels and the treatment of arrhythmias.

Abstract: A fulgimide compound which reversibly changes from a colorless state into a colored state upon the action of light including ultraviolet-rays, and a composition containing this compound. The fulgimide compound is represented by the following formula (I), ##STR1## wherein the following formula (a) ##STR2## represents a divalent aromatic hydrocarbon or a divalent unsaturated heterocyclic group which may have a substituent, respectively, R.sup.1 represents a monovalent hydrocarbon group or a monovalent heterocyclic group which may have a substituent, respectively, and the following formula (b), ##STR3## represents a norbornylidene group, bicyclo[3,3,1]nonylidene group or adamantylidene group which may have a substituent, respectively, and R.sup.

Abstract: A compound having the structure: ##STR1## pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.

Abstract: New fungicidal spiroheterocyclic compounds are described, having the general formula I, ##STR1## or an acid-addition salt thereof, in which R.sup.1 or each R.sup.1 independently represents an optionally substituted alkyl, cycloalkyl, cycloalkylalkyl, alkoxy, cycloalkoxy, alkoxyalkyl, aralkyl, aryl or aryloxy group, or R.sup.1 or each R.sup.1, together with the ring to which they are attached, represents an optionally substituted polycyclic hydrocarbyl group,R.sup.2 represents a hydrogen atom or a C.sub.1-4 alkyl group,R.sup.3 represents a hydrogen atom, a hydroxy group or an optionally substituted alkoxy or acyloxy group,R.sup.4 and R.sup.5 each independently represent a hydrogen atom, an optionally substituted alkyl, alkenyl, alkynyl, cycloalkylalkyl, cycloalkyl, bicycloalkyl, tricycloalkyl, alkoxyalkyl, aryl, aralkyl, haloaralkyl, a 4- to 6- membered heterocyclyl, tetrahydrofurfuryl or dioxolanyl group, or R.sup.4 and R.sup.

Abstract: The present invention relates to 1-H-3-phenyl-5-cyloalkylpyrrolidine-2,4-diones of the formula (I) ##STR1## in which A represents optionally substituted cycloalkyl andB represents hydrogen or optionally substituted alkyl,X represents alkyl, halogen or alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy or halogenoalkyl,Z represents alkyl, halogen or alkoxy,n represents a number 0, 1, 2 or 3,G represents hydrogen (a) or the groups ##STR2## These compounds possess herbicidal and pesticidal activity.

Abstract: There are described compounds of the formula ##STR1## where (a) X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicycloalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2 R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2-(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;(d) each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heteroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl, with the proviso that when X is O, m is 1, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.

Abstract: An improved process for the preparation of trans-6- 2-(substituted-pyrrole-1-yl)alkyl!pyran-2-ones by a novel synthesis is described where .alpha.-metalated N,N-disubstituted acetamide is converted in seven operations to the desired products, and specifically, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N, 4-diphenyl-1- 2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl!-1H-pyrrol e-3-carboxamide, as well as other valuable intermediates used in the processes and prodrugs which are bioconverted to hypolipidemic and hypocholesterolemic agents and pharmaceutical compositions of the same.

Abstract: Dialkyl-1-H-3-(2,4-dimethylphenyl)-pyrrolidine-2,4-diones of the formula (I) ##STR1## in which A represents alkyl which is optionally substituted by halogen andB represents C.sub.2 -C.sub.10 -alkyl orA and B together with the carbon atom to which they are bonded represent an unsubstituted cycle,G represents hydrogen (a) or the groups ##STR2## E represents a metal ion equivalent or an ammonium ion, L and M represent oxygen and/or sulphur. These compounds possess herbicidal and pesticidal activity.

Abstract: An improved process for the preparation of trans-6-[2-(substituted-pyrrole-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where .alpha.-metalated N,N-disubstituted acetamide is converted in seven operations to the desired products, and specifically, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahy dro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H pyrrole-3-carboxamide, as well as other valuable intermediates used in the processes and prodrugs which are bioconverted to hypolipidemic and hypocholesterolemic agents and pharmaceutical compositions of the same.

Abstract: Fungicidally active compounds of the formula ##STR1## in which X represents oxygen or sulphur,R represents cycloalkyl, or represents optionally substituted aryl, or represents the radical ##STR2## R.sup.1 and R.sup.2 each independently is hydrogen or an organic radical, or together with the nitrogen atom form a heterocyclic radical,R.sup.3 represents hydrogen, alkyl or optionally substituted aryl, andR.sup.4 represents alkyl or cycloalkyl, or represents optionally substituted aryl,but wherein R.sup.3 and R.sup.4 may not simultaneously represent methyl,and acid addition salts thereof, as well as intermediates therefor.

Abstract: 3,9-disubstituted-spiro[5.5]undecanes and ##STR1## wherein, R, Y, A, B and n are defined in the specification, pharmaceutical compositions containing same for the treatment of cardiovascular disorders, such as heart failure and hypertension, are disclosed.

Abstract: Compounds of formula (I): ##STR1## thereof have valuable anthelmintic, acaricidal and insecticidal activities.

Abstract: A novel class of N-substituted triarylmethane sulfonamides is provided which undergo reversible oxidation into colored form and reversible reduction of the oxidized form into colorless form. The N-substituted triarylmethane sulfonamides can be represented by the formulae: ##STR1## wherein B is a carbocyclic ring or rings; T is a 5- or 6-membered ring; Y is a moiety selected from ##STR2## wherein E, positioned ortho or para to said --OH group, is selected from --OH, --NH.sub.2, --NHR', --NR'R" and --NHSO.sub.

Abstract: Compounds of formula: ##STR1## in which R.sub.1 represents a hydrogen atom or an alkyl, alkoxycarbonyl or an unsubstituted or substituted phenyl radical,R.sub.2 represents a hydrogen atom or an unsubstituted or substituted alkyl radical,R.sub.3 represents an alkyl, phenylalkyl, indanyl, cycloalkylalkyl or an unsubstituted or substituted phenyl radical, orR.sub.2 and R.sub.3 form a heterocycle together with the nitrogen atom to which they are attached, andR.sub.4 represents an unsubstituted or substituted phenyl radical, a naphthyl, indolyl or quinolyl radical or a phenylamino radical in which the phenyl ring is unsubstituted or substituted, their preparation and medicaments containing them.

Abstract: Fungicidally active compounds of the formula ##STR1## in which X represents oxygen or sulphur,R represents cycloalkyl, or represents optionally substituted aryl, or represents the radical ##STR2## R.sup.1 and R.sup.2 each independently is hydrogen or an organic radical, or together with the nitrogen atom form a heterocyclic radical,R.sup.3 represents hydrogen, alkyl or optionally substituted aryl, andR.sup.4 represents alkyl or cycloalkyl, or represents optionally substituted aryl,but wherein and R.sup.3 and R.sup.4 may not simultaneously represent methyl,and acid addition salts thereof, as well as intermediates therefore.

Abstract: A compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, independently, halo, trifluoromethyl, cyano, nitro, alkyl, alkoxy, --CO.sub.2 H, alkylcarbonyl, alkylcarbonyloxy, alkoxycarbonyl, mono- or di-alkylaminocarbonyl, or mono- or di-alkylaminocarbonyloxy;m is 0, 1 or 2 andR.sup.3 is alkyl;n and p are, independently, 0, 1 or 2;X is O, S or CR.sup.4 R.sup.5,where R.sup.4 and R.sup.5 are, independently, H or alkyl or R.sup.4 and R.sup.5 together with the interposed carbon atom form a 3 to 8 membered carbocyclic ring, are anti-cholesterolemic agents.

Abstract: A bisphosphonic acid derivative of the formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein A is ##STR2## each of R.sup.3 and R.sup.4, which may be the same or different, is (i) a hydrogen atom, (ii) a C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a C.sub.1-6 alkyl-carbonyl group, a C.sub.2-6 alkenyl-carbonyl group, a C.sub.2-6 alkynyl-carbonyl group R.sup.5 and R.sup.6, which may be the same or different, is a hydrogen atom, a hydroxyl group, a halogen atom, a cyano group, a carbamoyl group, an aralkyl group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted amino group, a C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group;each of m and n is 0 or a positive integer, provided that (m+n) is from 2 to 5; andR is a hydrogen atom, a C.sub.1-8 alkyl group or a C.sub.7-15 aralkyl group.

Abstract: A class of novel heterocyclic aromatic carbamate compounds is described. A method of derivatizing amine-functional compounds with the novel carbamates is also disclosed. The derivatives can be detected using a fluorescence detector. The present composition and method allow femtomole quantities of amine compounds to be detected and measured.

Abstract: The present invention relates to a compound of the formula: ##STR1## wherein R.sup.1 is 2-methyl-1-propenyl group or isobutyl group; R.sup.2 and R.sup.3 are each hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted acyl group or R.sup.2 and R.sup.3 may form a ring together with the adjacent nitrogen atom; and the bonding mark .about. represents an .alpha.-linkage or .beta.-linkage, or a salt thereof. The compound (I) of the present invention has, among others, angiogenesis inhibiting activity, cell-growth inhibiting activity and immune reaction inhibiting activity, thus being useful as medicines, etc.

Abstract: N-succinimidyl and N-phthalimidyl esters of phenylalkanoic acid derivatives which are useful as inhibitors of HLE or HNE.

Abstract: An improved process for the preparation of trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where 1,6-heptadien-4-ol is converted in eight operations to the desired products, as well as an improved process for the preparation of (2R-trans) and trans-(.+-.)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetra hydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide by a novel synthesis where 4-methyl-3-oxo-N-phenylpentanamide is converted in eight operations to the desired product or alternatively 4-fluoro-.alpha.-[2-methyl-1-oxopropyl]-Y-oxo-N,.beta.-diphenylbenzenebuta neamide is converted in one step to the desired product, and additionally, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahy dro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide from (R)-4-cyano-3-[[(1,1-dimethylethyl)dimethylsilyl]oxy]butanoic acid, as well as other valuable intermediates used in the processes.

Abstract: A new method for the treatment of ischemic conditions and arrhythmia is disclosed. The method uses compounds of the formula ##STR1## wherein A can be --CH.sub.2 --, --O--, --NR.sub.9 --, --S--, --SO--, --SO.sub.2 --; X can be oxygen or sulfur; Y can be --NR.sub.8, --O--, --S--, --CH.sub.2 -- and the R groups are as defined herein. Novel compounds within the definition of formula I are also disclosed.

Abstract: Disclosed in a mitomycin derivative represented by the formula (I): ##STR1## wherein W is a heterocyclic group.

Abstract: The present invention provides a new diastereomer ester compound which is useful as an intermediate in the making of an optically active 3,4-dihydro-3,4-epoxy-2H-1-benzopyran compound.