Abstract: Phenethylamine derivatives shown by the general formula ##STR1## wherein Ro represents a lower alkyl group; R.sub.1 represents a lower alkyl group or a lower alkoxy group, R.sub.2 represents hydrogen atom or a hydroxyl group; R.sub.3 and R.sub.4 each represents hydrogen atom or a lower alkyl group; R.sub.5 represents hydrogen atom or a lower alkoxy group; X represents oxygen atom or a methylene group; m is an integer of 1-3; and n is an integer of 0-2and the acid addition salts thereof.These compounds exhibit a strong .alpha.-adrenergic blocking action and are useful as an antihypertensive agent.

Abstract: Heterocyclic spiro compounds represented by the following general formula and salts thereof: ##STR1## wherein A represents piperidine or N alkyl piperidine or N alkylene attached to a non adjacent piperidine ring carbon, X is S or O, Y is carbonyl, thiocarbonyl, methylene, R.sup.5 methylene, ##STR2## in which R.sup.1 to R.sub.3, R.sub.6, R.sub.7 are H or alkyl, R.sub.4 is H, alkyl, --COOH, or ester, or ##STR3## R.sub.5 is halo, OH, SH, O alkyl, S alkyl, O acyl or S acyl, and Z.sub.1 and Z.sub.2 are O or S.The above compounds act upon muscarinic acetylcholine receptors, thereby activating the acetylcholine nervous functions in the central nervous system.

Abstract: (Cycloalkylamino)methylenebis(phosphonic acid) represented by the general formula: ##STR1## in which, R, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent a hydrogen atom or a lower alkyl group, and n represents an integer from 3 to 10, a lower alkyl ester thereof or a pharmaceutically acceptable salt thereof; and a bone-resorption inhibitor and an anti-arthritis containing the same.

Abstract: Novel 1,4-dihydropyridine derivatives and salts thereof are provided, which can be represented by the formula ##STR1## wherein, Y represents an oxygen atom or a sulfur atom; A represents an alkylene group, an alkenylene group or an alkynylene group; and R.sup.7 and R.sup.8 can represent individual groups or may be combined together with a nitrogen atom(s) to form a pyrrole ring, a piperidine ring, a morpholine ring or a piperazine ring or azepine ring which may be substituted with a lower alkyl group or an aralkyl group. Pharmaceutical compositions containing the derivatives and their use for imparting calcium antagonistic activity are also provided.

Abstract: A novel heterocyclic bisphosphonic acid derivatives represented by the following general formula (I): ##STR1## in which .circle.Het means one of the following (A) and (B): ##STR2## wherein a dotted line in (A) means that two adjacent atoms are bonded by a single bond or a double bond, ##STR3## wherein R.sup.6 and R.sup.7 may be the same or different, each represents a hydrogen atom, a lower alkyl group, a halogen atom or a hydroxyl group,R.sup.1 represents a hydrogen atom or a hydroxyl group,R.sup.2, R.sup.3, R.sup.4 and R.sup.5 may be the same or different, each represents a hydrogen atom or a lower alkyl group,"n" is 0 or 1,provided that "n" is 1 when the ring .circle.Het means (A), and "R.sup.1 " is a hydroxyl group when the ring .dotthalfcircle.Het means (B), or pharmaceutically acceptable salts thereof and bone resorption inhibitors containing the compound as an active ingredient.

Abstract: A coating material for controlling drug release, useful for long acting formulations--e.g. for once-a-day administration, and to a long acting granular composition comprising a drug (especially one conventionally difficult to prepare in long acting form) coated with the coating material. This composition may be mixed with other granular drug formulations. The drug-release controlling coating material comprising, in a specific ration, one specific water-insoluble and low water-permeability polymers and two materials differing from each other in the pH-dependency of their solubility (pH-dependent polymer-materials).

Abstract: A lyophilized pharmaceutical composition comprised of a neocarzinostatin derivative having the formula (SMA)-(NCS)-(SMA), is made by a method including dissolving the neocarzinostatin derivative and stabilizing agent comprising at least one saccharide selected from the group consisting of monosaccharides, disaccharides and dextran in an aqueous buffer solution having a pH ranging from about 7.5 to about 9.5, the stabilizing agent being present in an amount by weight (titer) which is at least equal to that of the neocarzinostatin derivative, to provide a solution; adjusting the pH of the solution to provide a pH-adjusted solution having a pH of about 8.0.+-.0.5; sterilizing the pH-adjusted solution by filtration to provide a sterilized solution; and lyophilizing the sterilized solution.

Abstract: Heterocyclic spiro compounds represented by the following general formula and salts thereof ##STR1## The above compounds act upon muscarinic acetylcholine receptors, thereby activating the acetylcholine nervous functions in the central nervous system.

Abstract: Novel phenylene derivatives shown by the general formula ##STR1## wherein A represents a hydrogen atom, a phenyl group or a phenoxy group, n represents an integer of 3 to 10, R.sub.1 represents a hydrogen atom or a lower alkoxy group, X.sub.1 represents --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CONH--, .circle.B represents ##STR2## (wherein R.sub.2 represents a hydrogen atom, a halogen atom, a nitro group, etc.), ##STR3## (wherein R.sub.3 represents a hydrogen atom, a hydroxyl group or a lower alkoxy group), X.sub.2 represents --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, etc. and D represents a carboxy group, a lower alkoxycarbonyl group or ##STR4## which are useful as drugs, particularly SRS-A (slow reacting substance of anaphylaxis) antagonist, i.e. they are useful as prophylaxis and treatment for various allergic diseases (e.g. bronchial asthma, allergic rhinitis, urticaria) or, ischemic heart diseases, inflammation, etc. induced by SRS-A.

Abstract: A novel heterocyclic bisphosphonic acid derivatives represented by the following general formula (I): ##STR1## in which, .circle.Het means one of following (A) and (B): ##STR2## wherein a dotted line in (A) means that two adjacent atoms are bonded by a single bond or a double bond, ##STR3## wherein R.sup.6 and R.sup.7 may be the same or different, each represents a hydrogen atom, a lower alkyl group, a halogen atom or a hydroxyl group,R.sup.1 represents a hydrogen atom or a hydroxyl group,R.sup.2, R.sup.3, R.sup.4 and R.sup.5 may be the same or different, each represents a hydrogen atom or a lower alkyl group,"n" is 0 or 1,provided that "n" is 1 when the ring .circle.Het means (A), and "R.sup.1 " is a hydroxyl group when the ring .circle.Het means (B),or pharmaceutically acceptable salts thereof and bone resorption inhibitors containing the compound as an active ingredient.

Abstract: Novel phenoxy derivatives are provided such as 6-[p-5-(1-imidazolyl)pentyloxy]phenoxy]-2,2-dimethyl-hexanoic acid, pharmaceutical compositions containing the derivative and their use in treating tumors.

Abstract: A saturated heterocyclic carboxamide derivative of the following general formula (I) and salts thereof which have platelet activating factor (PAF) antagonizing activity.

Abstract: Novel sulfamoyl-substituted phenethylamine derivatives which exhibit .alpha.-adrenergic blocking action and are useful as an antihypertensive agent and an agent for the treatment of congestive heart failure.

Abstract: 4,5,6,7-Tetrahydrobenzimidazole derivatives represented by general formula (I) ##STR1## wherein groups represents the following: R.sup.1, R.sup.2, R.sup.3 : independently represent hydrogen atom, hydroxy group, a halogen atom, a lower alkyl group which may optionally be substituted with a halogen atom, a lower alkoxy group, a lower alkylthio group, an aralkyloxy group, an aryloxy group, a lower alkanoyl group, carboxy group, a lower alkoxycarbonyl group or nitro group;R.sup.4, R.sup.5, R.sup.6 : hydrogen atom or a lower alkyl group;X: oxygen atom or sulfur atom;or salts thereof which are believed to have a 5-HT.sub.3 antagonizing activity.

Abstract: "Novel bisphosphonic acid derivatives, and a bone resorption-inhibitor and an anti-arthritis containing a bisphosphonic acid derivative represented by the formula (I): ##STR1## wherein R.sup.2 represents a hydrogen atom, an alkyl group, etc.,R.sup.2 represents a hydrogen atom or a lower alkanoyl group,R.sup.3, R.sup.4, R.sup.5 and R.sup.6 may be the same or different, each represents a hydrogen atom or lower alkyl group.

Abstract: Novel Vitamin D.sub.3 derivatives of the following formula ##STR1## wherein R represents a hydrogen atom or a lower alkyl group. These compounds have an activity of inducing differentiation of tumor cells, and are useful for anti-tumor agents. On the other hand, the compounds have almost no vitamin D activity.

Abstract: (Cycloalkylamino)methylenebis(phosphonic acid) represented by the general formula: ##STR1## in which, R, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent a hydrogen atom or a lower alkyl group, and n represents an integer from 3 to 10, a lower alkyl ester thereof or a pharmaceutically acceptable salt thereof; and a bone-resorption inhibitor and an anti-arthritis containing the same.

Abstract: Therapeutic agents for ischemic heart diseases are provided and contain as an effective component a glutathione monoalkyl ester. The invention is also directed to the use of such therapeutic agents for the treatment of ischemic heart diseases.

Abstract: A compound of the formula (I) or its salt and a process for producing the compounds; The compounds have the effect to dilate neophrovascular tracts; ##STR1## Wherein ##STR2## represents the formula ##STR3## (wherein R.sup.4 is a hydrogen atom or lower alkylsulfonyl); R.sup.1 is hydrogen, lower alkyl, hydroxyl, halogen, amino, or lower acylamino;R.sup.2 is hydrogen, lower alkyl, hydroxyl, amino, or lower alkylsulfonylamino;R.sup.3 is hydrogen, lower alkyl, or hydroxyl;R is hydrogen or halogen;with the proviso that when R.sup.1 is hydroxyl, there is no case that all of R.sup.2, R.sup.3 and R are hydrogens, and further with the proviso that when R is hydrogen, A excludes ##STR4## or a salt therof.

Abstract: Substituted 1,3-dithietane-2-carboxylic acid derivatives useful as intermediates for the preparation of highly effective penicillin and cephalosporin derivatives and the preparation thereof.