Abstract: Disclosed herein are compounds of the formula wherein R1 is independently H or alkyl of 1 to 6 carbons; R2 is optional and is defined as lower alkyl of 1 to 6 carbons, F, Cl, Br, I, CF3, fluoro substituted alkyl of 1 to 6 carbons, OH, SH, alkoxy of 1 to 6 carbons, or alkylthio of 1 to 6 carbons; n is an integer of between 0 and 2; o is an integer between 0 and 3; R3 is hydrogen, lower alkyl of 1 to 6 carbons, F, Cl, Br or I; R4 is heteroaryl or (R5)p-heteroaryl where the heteroaryl group is 5-membered or 6-membered and has 1 to 3 heteroatoms selected from the group consisting of O, S, and N; p is an integer having the values of 0–5; R5 is F, Cl, Br, I, NO2, N(R8)2, N(R8)CORO8, N(R8)CON(R8)2, OH, OCOR8, OR8, CN, COOH, COOR8, C1-10 alkyl, fluoro substituted C1-10 alkyl, C2-10 alkenyl having 1 to 3 double bonds, C2-10 alkynyl having 1 to 3 triple bonds, or a (trialkyl)silyl or (trialkyl)silyloxy group where the alkyl groups independently have 1 to 6 carbons; A is (CH2)q where q is 0–5, C3-6 branched alkyl,

Abstract: A morphine component, e.g., a concentrate of poppy straw, is converted into codeine in high yield and high purity and in a highly controlled manner. The conversion process involves the following steps: (a) providing a solution or suspension of a morphine component in an inert solvent or a mixture of solvents; (b) methylating the resultant solution or suspension with a methylating agent in the presence of an alkaline ingredient; and (c) recovering the resultant codeine as the free base or as a salt.

Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH2—OH, —CH2NH2, —NHSO2CH3, and Y is O, S or NOH are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. 8-Carboxamides, thiocarboxamides, hydroxyamidines and formamides are preferred.

Abstract: A substituted 1,2,3,4-tetrahydroquinoline-2-carboxylic acid derivative of formula I 1

Abstract: A process for preparing a morphinan derivative, by providing a dihydrofuranyl bridged tetracycle halide of the formula (19) wherein X is halogen, R is an alkyl group of from 1 to about 10 carbon atoms, and R1 is a protecting group; and converting the pentacycle halide into a morphinan derivative of formula (20) wherein R is as defined above.

Abstract: A novel phenanthridinium derivative represented by general formula (A): wherein R1 is a substituted or unsubstituted lower aliphatic hydrocarbon group; R is an aliphatic hydrocarbon chain having 2 to 6 carbon atoms which may optionally be substituted with a substituent selected from the group consisting of a lower alkyl group, a halogen and a hydroxy group; each of Y and Z independently represents a hydrogen, a hydroxy or a lower alkoxy group; or Y and Z are combined together to form methylenedioxy or a phenyl ring; and, X− is an acid residue or a hydrogen acid residue, exhibits an antitumor activity and has resistance to chemical reduction as well as biological metabolic reactions and is thus advantageous for use as a medicine.

Abstract: The present invention describes a family of fluorescent indicators for metal cations. The indicators are fluorophore conjugates of pyridyl-based metal ion chelators. The indicators are very sensitive detection as quantification reagents for a variety of metals, in a variety of oxidation states, even in the presence of high concentrations of Ca.sup.2+, Na.sup.+, or K.sup.+ or other ions, such as is found in seawater, making them highly useful for assaying physiological samples, biological samples, or environmental samples.

Abstract: A chromogenic receptor comprises a self-assembled chromogenic compound having at least one intrinsic binding site. The chromogenic compound is characterized by the property of producing a reversible color change responsive to binding a target substrate to the receptor. The chromogenic compound has a transition metal ion and at least one ligand bound to the transition metal ion. The ligand is selected from the group consisting of substituted phenanthroline, substituted 2,2'-bipyridine and substituted 2,2':6',2"-terpyridine. The transition metal is selected from the group consisting of Cu(I), Cu(II), Ag(I), Ni(II), Fe(II), Fe(III), Ru(II), Co(III), and Os(II). Self-assembly can be effected in the presence of Cu(I) to form receptors for dicarboxylic acids, carbohydrate, amino acids, steroids and pyrophosphates. The receptors are characterized by the formation of a 2:1 complex of the target substrate with the receptor producing a visible color change from orange to red and a measurable change in its luminescence.

Abstract: A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for treating disturbances of memory such as senile dementia and Alzheimer's disease, since it has an action of directly activating malfunctioned cholinergic neuron.

Abstract: A process for isolating berberine from plants is described. An oral formulation of berberine is described.

Abstract: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.

Abstract: Pentacyclic derivatives having the general formulae (Ia), (Ib) and (Ic) ##STR1## denote: hydrogen, alkyl with 1 to 20 carbon atoms polyoxyhydrocarbyl, phenyl, phenylalkyl with 1 to 3 carbon atoms in the alkyl chain, wherein the alkyl residues or/and phenyl residues can be substituted by one or several hydroxy, halogen, sulfo, carboxy or alkoxycarbonyl groups in which alkoxy can have 1 to 4 carbon atoms;R.sup.7 denotes an alkyl group with 1 to 7 carbon atoms, substituted by at least one halogen, or denotes a carboxyalkyl group or a phenyl group which is substituted by a carboxy or alkoxycarbonyl group located at the o-position relative to the carbon atom bound to the pentacyclic ring system and by at least one halogen, wherein alkoxy can have 1 to 4 carbon atoms, or a carboxymethylene-oxy-alkyloxy group; the residues R.sup.14 and R.sup.

Abstract: The present invention relates to benzo?c!phenanthridinium derivative of the general formula A: ##STR1## wherein M and N individually represent a hydroxyl or lower alkoxy group, or M and N simultaneously represent a hydrogen atom or together form a methylenedioxy group, X.sup.- represents an acid residue or a hydrogen acid residue, and R represents a lower alkyl group, and a process for preparing such derivatives. The compounds exhibit both potent antitumor activity and platelet aggregation inhibition activity, and are expected to be useful for the treatment of tumors. The process has good reproducibility and may be effected under moderate conditions, and therefore the process is practically useful. In addition, hydrogen salts of the present compounds have an enhanced stability, which is an advantage in formulating the same into pharmaceutical preparations.

Abstract: A condensed-indan derivative represented by formula (1) and a pharmaceutically acceptable salt thereof: ##STR1## wherein ring A represents an optionally substituted naphthalene ring, ring B represents an optionally substituted benzene ring or a benzene ring having a lower alkylenedioxy group. Y represents --N.dbd.CR-- or --CR.dbd.N--, R represents a --NR.sub.1 R.sub.2 group, an optionally substituted nitrogen-containing heterocyclic group or a --OR.sub.3 group, wherein R.sub.1 and R.sub.2 are the same or different and each is a hydrogen atom; a phenyl group; an optionally substituted nitrogen-containing heterocyclic group; or a lower alkyl group which may be substituted by at least one selected from the group consisting of an optionally substituted amino group, a lower alkoxy group, a phenyl group, a nitrogen-containing heterocyclic group, an amine oxide group substituted by a lower alkyl group or a hydroxyl group(s); R.sub.3 represents a lower alkyl group optionally substituted by a substituted amino group.

Abstract: The present invention relates to certain substituted 17.beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I), especially those of formula (IG) ##STR1## wherein R.sup.1 and R.sup.2 arei) independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, orii) taken together are a --CH.sub.2 -- group to form a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond;R.sup.3c is hydrogen;R.sup.4c is hydrogen, lower alkyl, lower cycloalkyl, lower alkenyl, alkanoyl of 2-6 carbons, --(CH.sub.2).sub.m CO.sub.2 R.sup.16, --(CH.sub.2).sub.m Ar.sup.a, --(CH.sub.2).sub.n 'CONR.sup.17 R.sup.18, --(CH.sub.2).sub.n 'NR.sup.17 R.sup.18 or --(CH.sub.2).sub.n 'OR.sup.16, wherein R.sup.16 is hydrogen, lower alkyl or lower alkenyl; R.sup.17 and R.sup.18 are independently hydrogen, lower alkyl lower cycloalkyl or lower alkenyl; Ar.sup.

Abstract: A process of providing novel compounds of Formula (I), that are useful as 6-azaandrostenone testosterone 5-alpha-reductase inhibitors, from commercially available compounds of Formula (II) ##STR1## wherein the substituents are as defined in the specification, and the pharmaceutically acceptable salts and solvates thereof.

Abstract: A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for treating disturbances of memory such as senile dementia and Alzheimer's disease, since it has an action of directly activating malfunctioned cholinergic neuron.

Abstract: A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for treating disturbances of memory such as senile dementia and Alzheimer's disease, since it has an action of directly activating malfunctioned cholinergic neuron.

Abstract: The present invention relates to certain substituted 17 .beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 arei) independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, orii) taken together are a --CH.sub.2 -- group to form a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond;X is ##STR2## wherein R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen or lower alkyl,p and q are independently either 0 or 1;R.sup.3 is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, thiopyridyl, adamantyl, --NR.sup.9 R.sup.10 or --Ar--NR.sup.9 R.sup.10whereinR.sup.9 and R.sup.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: There are provided compounds of general formula ##STR1## (wherein R.sup.1 is a hydrogen atom or a methyl group;R.sup.2 is a hydrogen or halogen atom or a methyl group;and one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is a group --NR.sup.5 R.sup.6 [where R.sup.5 is a hydrogen atom and R.sup.6 is a group --COCH.sub.2 NR.sup.7 R.sup.8 (wherein R.sup.7 and R.sup.8, which may be the same or different, each represents a hydrogen atom or a C.sub.3-7 cycloalkyl group of a C.sub.1-4 alkyl group optionally substituted by a hydroxyl or benzoyloxy group, or --NR.sup.7 R.sup.8 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring an oxygen or sulphur atom or a group --NH-- or --N(R)-- where R is a C.sub.1-4 alkyl group optionally substituted by a hydroxyl group) or R.sup.6 is a group --COCH.sub.2 NH(CH.sub.2).sub.n NR.sup.7 R.sup.8 (where n is an integer from 2 to 5 inclusive and R.sup.7, R.sup.8 and --NR.sup.7 R.sup.8 are as defined above) or R.sup.

Abstract: A process is described for the preparation of compounds of formula (1) ##STR1## [where OR is hydroxyl, protected hydroxyl or OP(O)(OCH.sub.2 Ph)(OR.sup.1) (where Ph is phenyl and OR.sup.1 is hydroxyl or protected hydroxyl)] and salts thereof, which comprises reacting a compound of formula (2) ##STR2## with a compound of formula (3) ##STR3## (where OR is as defined above and one of X.sup.1 and X.sup.2 is a leaving group and the other is a hydrogen atom) or a salt thereof, followed, if desired, by removal of the hydroxyl protecting group when present and/or by salt formation.The compounds of formula (1) are either anticancer agents or intermediates useful in the synthesis of anticancer agents.

Abstract: Compounds of formula (I) ##STR1## (wherein R.sup.1 is a hydrogen atom or a methyl group;R.sup.2 is a hydrogen atom or a hydroxyl, C.sub.1-4 alkoxy or C.sub.2-4 alkanoyloxy group;R.sup.3 is a hydrogen atom, or (when R.sup.2 is other than a hydrogen atom) optionally a hydroxyl, C.sub.1-4 alkoxy or C.sub.2-4 alkanoyloxy group, or R.sup.2 and R.sup.3 together are a methylenedioxy group;R.sup.4 is a hydrogen or halogen atom or a methyl group;R.sup.5 and R.sup.6 is each a hydrogen atom or a group --OCOCH.sub.2 NR.sup.7 R.sup.8 [where R.sup.7 and R.sup.8, which may be the same or different, each is a hydrogen atom or a C.sub.3-7 cycloalkyl group or a straight or branched C.sub.1-4 alkyl group optionally substituted by a hydroxyl group, or --NR.sup.7 R.sup.8 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring an oxygen or sulphur atom or a group --NH-- or --N(R) where R is a C.sub.

Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 29 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a C.sub.8-13 fused heterotricyclic ring system containing at least two aromatic rings and no more than 3 heteroatoms (in separate rings), or a C.sub.10-17 fused heterotetracyclic ring system containing at least two aromatic rings and no more than 4 heteroatoms (in separate rings) or a C.sub.

Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.

Abstract: There are provided compounds of the general formula (1) ##STR1## (wherein R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom, a hydroxyl group or a group --OP(O) (OH) (OR.sup.4) [where R.sup.4 represents a hydrogen atom or an alkyl (optionally substituted by a hydroxyl, alkoxy, cyclic ether or cycloalkyl group), alkenyl cycloalkyl, aryl, aralkyl or aroylalkyl group], with the proviso that at least one of R.sup.1 and R.sup.2 represents a group --OP(O) (OH) (OR.sup.4); and R.sup.3 represents a hydrogen or halogen atom or a methyl group), and salts thereof. The novel compounds exhibit interesting anti-cancer activity.

Abstract: Pharmaceutical compositions for combatting cancer comprising a compound of formula (I) ##STR1## (wherein R.sup.1 represents a hydrogen atom or a C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl group;R.sup.2 represents a hydrogen atom or a hydroxyl, C.sub.1-4 alkoxy or C.sub.2-4 alkanoyloxy group;R.sup.3 represents a hydrogen atom, or (when R.sup.2 is other than a hydrogen atom) optionally a hydroxyl, C.sub.1-4 alkoxy or C.sub.2-4 alkanoyloxy group, or R.sup.2 and R.sup.3 together represent a methylenedioxy group;R.sup.4 represents a hydrogen or halogen atom or a C.sub.1-3 alkyl group or a phenyl group optionally substituted by a halogen atom or a hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.1-4 alkanoyloxy group; and the ring A represents a group of formula ##STR2## where R.sup.5 and R.sup.6 each represent a hydrogen atom or a hydroxyl, C.sub.1-4 alkoxy or C.sub.1-4 alkanoyloxy group,R.sup.7 and R.sup.8 each represents a hydrogen atom or a methyl group, and one of X, X.sup.1, X.sup.2 and X.sup.

Abstract: 5,14-Dihydrobenz[5,6]isoindolo[2,1-b]isoquinoline-8,13-dione ##STR1## exhibits anticancer activity. The compound can be prepared by reaction of 2-formyl-3-carboxyl-1,2,3,4-tetrahydroisoquinoline with 1,4-naphthoquinone and is particularly suitably administered parenterally in microcrystalline suspension form.

Abstract: Fused ring compounds of formula (I): ##STR1## (where R.sup.1 -R.sup.4, X.sup.1 and X.sup.2 represent hydrogen or various substituents, n and m are 1-3 and 2-7 respectively, the dotted lines are double or single bonds and Y is one oxygen or two hydrogens) have magnificent anti-arrhythmic activity, diuretic activity and the ability to improve brain function.

Abstract: Novel cyclopropyl pyridine compounds useful as calcium channel blockers, pharmaceutical compositions thereof, and methods of treatment are disclosed.

Abstract: A novel process for the preparation of cyclopropyl pyridine compounds, which are useful as calcium channel blockers, is disclosed.

Abstract: Dyes of the formula ##STR1## where R.sup.1 is hydrogen, C.sub.1 -C.sub.6 -alkyl or C.sub.2 -C.sub.6 -alkenyl, R.sup.2 and R.sup.3 independently of one another are hydrogen, C.sub.1 -C.sub.5 -alkyl or C.sub.2 -C.sub.5 -alkenyl, R.sup.4 is C.sub.1 -C.sub.12 -alkyl or hydroxy-C.sub.2 -C.sub.4 -alkyl, X.sup..crclbar. is one equivalent of an anion, mis from 0 to 5 and n is from 0 to 5, with 1.ltoreq.(m+n).ltoreq.5, and F is an (m+n)-valent radical of a monoazo dye, a disazo dye, a polyazo dye, a quinophthalone, a bis-dioxazine, a compound of the 5,6-arylo-2-pyrone series, a naphtholactam dye, a triphenylmethane dye, a xanthene dye, a phthalocyanine, an indigoid, an anthraquinone dye containing one or more phenyl or naphthyl groups, a more highly fused carbonyl-containing dye, a quinacridone, a perylene-3,4,9,10-tetracarboxylic acid diimide, an anthrapyrimidine, a pyrazoloanthrone, a diaminonaphthoquinone, a naphthazarine or a naphthalene-1,4,5,8-tetracarboxylic acid diimide.

Abstract: 13-Chloro-octahydrobanzo[6,7]cyclohepta[1,2,3-de]pyrido[2,1-a]isoquinolin-5 -ols, substituted on the piperidine ring with lower alkyl or a cycloalkyl are disclosed. The compounds are useful CNS depressants. Methods for their preparation and use also are disclosed.