Abstract: Thiophene derivatives of formula (I) ##STR1## wherein X and Y are the same or different O, S or N--R.sup.3,Z is a C.sub.1 -C.sub.6 -alkylene residue that may be substituted by R.sup.1 and R.sup.2,R.sup.1, R.sup.2 are the same or different hydrogen, or --(CH.sub.2).sub.n --OR.sup.4, --CH.dbd.CH.sub.2 or ##STR2## n is 1 to 10, R.sup.3 is aryl, C.sub.1-18 -alkyl or H,R.sup.4 is SO.sub.3.sup.- (H.sup.+,Na.sup.+,K.sup.+,Li.sup.+) or --(CH.sub.2 --CH.sub.2 --O).sub.m --R.sup.5,m is 1 to 10 andR.sup.5 is alkyl with 1 to 6 C atoms,wherein compounds in which X and Y are both O and R.sup.1 and R.sup.2 are both hydrogen atoms are excluded, are suitable for the preparation of polythiophenes which can be used as organic electrical conductors.

Abstract: Bile acid derivatives, processes for their preparation and use as pharmaceuticals Bile acid derivatives of the formula IW--X--Gin which G is a bile acid radical, W is an active compound moiety of a medicament and X is a bonding member between a bile acid radical and active compound moiety, are outstandingly suitable for introducing active compounds into the enterohepatic circulation. The compounds I are absorbed and pass into the bloodstream. It is possible in this way, using the natural reabsorption of the bile acids, to achieve improved absorption of non-absorbable or poorly absorbable pharmaceuticals.W may be, for example, a peptide, an antibiotic, an antiviral substance, an anticancer agent, a hepatoprotective agent, an antihyperlipidemic, a diuretic, a hypotensive, a renin inhibitor, a substance for the treatment of cirrhosis of the liver or a substance for the treatment of diabetes.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is H or an optionally substituted hydrocarbon or acyl group; ring A is an optionally further substituted benzene ring; n is an integer of 1 to 10; R.sup.2, R.sup.3 and R.sup.4 are H or an optionally substituted hydrocarbon group; R.sup.3 and R.sup.4 may form an optionally substituted heterocyclic group, taken together with the adjacent nitrogen atom; k is an integer of 0 to 3; and m is an integer of 1 to 8; provided that when k=0 and m=2, n is an integer of not less than 2 or a pharmaceutically acceptable salt thereof, exhibiting excellent cholinesterase inhibitory activity and monoamine reuptake inhibitory activity, thus being useful as therapeutic/prophylactic medicaments of senile dementia.

Abstract: Compounds of formula (I), and salts and prodrugs thereof: ##STR1## wherein X represents O or S;Y represents (CH.sub.2).sub.m, where m is 0 or 1;Z represents (CH.sub.2).sub.n, where n is 0 or 1;R.sup.1 represents optionally substituted phenyl;R.sup.2 is phenyl, naphthyl, indazolyl, thienyl, furyl, pyridyl, thiazolyl, tetrazolyl, quinolyl, benzhydryl or benzyl;R.sup.3 is H, COR.sup.a, CO.sub.2 R.sup.a C(COOR).sub.2, C(CONR.sup.a R.sup.b).sub.2, COCONR.sup.a R.sup.b, COCO.sub.2 R.sup.a, C.sub.1-6 alkyl optionally substituted by a group selected from (CO.sub.2 R.sup.a, CONR.sup.a R.sup.b, hydroxy, cyano, COR.sup.a, NR.sup.a R.sup.b, C(NOH)NR.sup.a R.sup.b, CONHphenyl(C.sub.1-4 alkyl), COCO.sub.2 R.sup.a, C(.dbd.NR.sup.a)NR.sup.b NR.sup.c CO.sub.2 R.sup.d, CONHNR.sup.a R.sup.b, C(S)NR.sup.a R.sup.b, CONR.sup.a C.sub.1-6 alkylR.sup.12, CONR.sup.13 C.sub.2-6 alkynyl, CONR.sup.13 C.sub.2-6 alkenyl, COCONR.sup.a R.sup.b, CONR.sup.a C(NR.sup.b)NR.sup.c R.sup.d, CONR.sup.13 SO.sub.2 R.sup.a, SO.sub.2 R.sup.13 COR.sup.

Abstract: The present invention provides substituted dibenzoxazepine and dibenzthiazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, and for prostaglandin-E.sub.2 mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal, and a method for treating prostaglandin-E.sub.2 mediated diseases in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.

Abstract: Disclosed are a process and intermediates of the formulae ##STR1## wherein R is --CH.sub.2 OH or --OH and R.sup.3 is H or C.sub.1 -C.sub.6 alkyl; useful for preparing benzazepines of the formula ##STR2## having activity as selective D1 antangonists.

Abstract: The invention features novel derivatives of K-252a, as well as novel bis-N-substituted derivatives of staurosporine. Also, a method for treating diseased neuronal cells involving the administration of either the novel staurosporine derivatives or specified functional derivatives of K-252a.

Abstract: Disclosed are a process and intermediates of the formula ##STR1## wherein R is --CH.sub.3 or --C(O)--OR.sup.1, and R.sup.1 is C.sub.1 -C.sub.6 alkyl or --CH.sub.2 C.sub.6 H.sub.5 ; or the formula ##STR2## wherein: R.sup.2 is H or OH, R is --C(O)OR.sup.1 and R.sup.1 is C.sub.1 -C.sub.6 alkyl or --CH.sub.2 C.sub.6 H.sub.5, or where R.sup.2 is H, R can also be CH.sub.3 ; for preparing benzazepine intermediates of the formula ##STR3## The benzazepine intermediates are useful for preparing benzazepines having activity as selective D1 receptor antagonists.

Abstract: Amide tetrazoles of the formula ##STR1## wherein aryl includes phenyl and naphthyl, unsubstituted or substituted, X is .dbd.O, .dbd.N--R.sub.5, or --NR.sub.3 R.sub.4, where R.sub.2, R.sub.4, and R.sub.5 include alkyl and alkoxy and R.sub.3 includes alkyl, are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia or atherosclerosis.

Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.

Abstract: The present invention is concerned with novel imidazo[1,2-a](pyrrolo, thieno or furano)[3,2-d]azepines of formula ##STR1## the pharmaceutically acceptable addition salts and stereochemically isomefic forms thereof, wherein each of the dotted lines independently represents an optional bond;R.sup.1 represents hydrogen, C.sub.1-4 alkyl, halo, ethenyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, hydroxy C.sub.1-4 alkyl, formyl, hydroxycarbonyl or hydroxycarbonyl C.sub.1-4 alkyl;R.sup.2 represents hydrogen, C.sub.1-4 alkyl, ethenyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, hydroxy C.sub.1-4 alkyl, formyl or hydroxycarbonyl;R.sup.3 represents hydrogen, C.sub.1-4 alkyl, hydroxy C.sub.1-4 alkyl, phenyl or halo;L represents hydrogen; C.sub.1-6 alkyl; C.sub.1-6 alkyl substituted with one substituent selected from the group consisting of hydroxy, halo, C.sub.1-4 alkyloxy, hydroxycarbonyl, C.sub.

Abstract: 1. A compound of the formula: ##STR1## wherein the symbol of a solid line with a broken line means a single bond or a double bond,R and R' are independently selected from the group consisting of hydrogen atom, halogen atom, lower alkyl, nitro, unsubstituted amino and substituted amino,A and B are independently selected from the group consisting of hydrogen atom, lower alkyl optionally substituted with a lower cycloalkyl, aryl optionally substituted with one or more halogen atoms and the group: -Y-R.sup.2wherein Y is lower alkylene and R.sup.2 is the group: ##STR2## wherein m is integer of 1 to 3, n is 0 or 1, Z is >N-, >CH-- or >C=, R.sup.3 is diaryl (lower) alkyl optionally substituted with one or more halogen atoms or is condensed heterocyclic group optionally substituted with oxo, with the proviso that(a) at least one of A and B is the group -Y-R.sup.2 and(b) when A is hydrogen atom and B is the group -Y-R.sup.2, then Z is >CH-- or >C= if R.sup.

Abstract: The present invention relates to 24R-scymnol, including its preparation in substantially pure form and to its use in the treatment of liver dysfunction.

Abstract: This invention relates to the antibiotics LL-14E605.beta. and O-methyl-LL-14E605.beta. derived from the microorganism Sebekia benihana which are useful as antibacterial agents.

Abstract: The present invention provides substituted dibenzoxazepine and dibenzthiazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.

Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.

Abstract: Compounds of the formula ##STR1## in which Y represents hydrogen, fluorine, chlorine, methyl or methoxy, R.sub.1 represents phenyl substituted by fluorine, methyl, methoxy, trifluoromethyl or phenyl, or R.sub.1 represents 2-thienyl, R.sub.2 represents methyl, and R.sub.3 represents (C.sub.1 -C.sub.4)-alkyl, or phenyl-(C.sub.1 -C.sub.2)-alkyl optionally substituted on the ring by 2 to 3 methoxy groups, or 2-(2-pyridyl)ethyl, or R.sub.2 and R.sub.3 form, with the adjacent nitrogen, 4-phenyl(1-piperidyl), 4-phenylmethyl(1-piperidyl), 1,2,3,4-tetrahydro-2-isoquinolyl, 6-methoxy-1,2,3,4-tetrahydro-2-isoquinolyl, 5,8-dimethoxy-1,2,3,4-tetrahydro-2-isoquinolyl, 6,7-dimethoxy 1,2,3,4-tetrahydro-2-isoquinolyl, 2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl, or 7,8-dimethoxy-2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl, and X represents carbonyl or sulphonyl, and their salts are useful as neuroprotective and antiiischaemic agents.

Abstract: A triazolo-1,4-di-azepine compound of the below given formula and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to allergic diseases. ##STR1## in which R1 and R2 are hydrogen or an alkyl, R3 is hydrogen or a halogen, R4 is hydrogen or an alkyl, X is --OOO--, --NHCO--, --CO-- or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.

Abstract: The invention relates to enantiomerically pure 2-oxa-5,8-diazabicyclo[4.3.0]nonanes and processes for their preparation.

Abstract: A method for visibly reducing a skin wrinkle by topically applying to the wrinkle lactic acid or a topically effective salt thereof.