Abstract: Vasodilating activity is exhibited by compounds having the formula ##STR1## wherein X can be --S--or --CH.sub.2 --; andR.sub.2 is ##STR2##depending upon the definition of X.

Abstract: Novel epoxyalkoxy-containing [4.4] spirodilactams having ring nitrogen atoms in the 1- and the 6- ring positions and having a substituent on each ring nitrogen atom, at least one of which substituents contains an epoxyalkyl moiety. Such epoxy compounds are produced by reaction of a 1-halo-2,3-epoxyalkane and the corresponding hydroxy-containing spirodilactam followed by treatment with strong base.

Abstract: Piperidine compounds of the formula: ##STR1## or isomers thereof as well as pharmaceutically acceptable salts and/or hydrate forms thereof, and piperidine compounds of the formula: ##STR2## or isomers thereof as well as salt and/or hydrate forms thereof. In the above formulae, A represents a methylene group, an oxygen atom or a sulfur atom; B represents an oxygen atom or a sulfur atom; R.sup.1 and R.sup.2 independently represent a hydrogen atom, a lower alkyl group or an aralkyl group; R.sup.3 represents a hydrogen atom or an amino protecting group; Z represents an amino group or a protected amino group, a hydroxy group, or a reactive atom or group; m represents 1 or 2; and n represents the integer of 0 to 3.Piperidine compounds (I) possess an inhibitory activity against angiotensin-converting enzyme, and exhibit a long lasting hypotensive activity and are useful as antihypertensive agents. Piperidine compounds (II) are useful as intermediates for said piperidine compounds (I).

Abstract: Novel compounds of the formula: ##STR1## [wherein A is an .alpha.-amino acid residue; B is a group represented by the formula: ##STR2## (wherein R.sup.4 is hydrogen, lower alkyl, aralkyl or amino-lower alkyl), whereby the linkage between the symbols A and B designates a peptide bond and the group R.sup.4 in B may be linked with A; R.sup.1 is hydrogen, lower alkyl or aralkyl; R.sup.2 is hydrogen, lower alkyl, aralkyl or acyl; X is alkylene] and salts thereof possess, for example, inhibitory activity on angiotensin converting enzyme, and are useful as an agent for diagnosis, prevention or treatment of hypertension as well as circulatory diseases such as cardiopathy and cerebral apoplexy.

Abstract: A process for preparing optically active naphtho[1,2-b][1,4]thiazepin-4(5H)-ones comprising resolution of rac-.beta.-[(2-amino-1-naphthalenyl)thio]-.alpha.-hydroxy-4-methoxybenzene propanoic acid and converting the optically active acids so obtained into final products is described. The end product naphtho[1,2-b][1,4]thiazepin-4(5H)-ones have activity as calcium channel blockers and accordingly are useful as agents for lowering blood pressure, and as agents for treating ischemia.

Abstract: This invention relates to substituted pyridooxazinone pyridones which are useful as cardiotonic agents for the treatment of congestive heart failure, to methods for increasing cardiac contractility using said compounds, and pharmaceutical compositions including the same.

Abstract: This invention is directed to compounds having the formula: ##STR1## wherein: A represents an aromatic or heterocyclic ring having two of its carbon atoms held mutually with the oxazepine, thiazepine or diazepine moiety selected from the group consisting of benzene, naphthalene, a quinoline, a pyridine in any of its four positions, any of which rings are optionally substituted by one or two Y radicals selected from the group consisting of halo, loweralkyl, loweralkoxy, diloweralkylamino, nitro, amino, lower acylamino, trilfuoromethyl, phenyl or phenyl substituted by one to three Y' groups selected from halo, loweralkyl, loweralkoxy, diloweralkylamino, nitro, amino, loweracylamino or trifluoromethyl,E is selected from oxygen, sulfur or ##STR2## B is selected from the group consisting of loweralkyl, cycloalkyl or phenyl-loweralkyl wherein phenyl is optionally substituted by one or two radicals selected from halo, loweralkyl, loweralkoxy, nitro or trifuoromethyl,N is 1 or 2,R.sup.4 and R.sup.

Abstract: Compounds which are 1,5-benzothiazepine derivatives of general formula (I) ##STR1## in which R denotes hydrogen or C.sub.1 -C.sub.4 alkyl and R.sub.1 and R.sub.2 either separately denote C.sub.1 -C.sub.4 alkyl groups or together denote a tetramethylene or pentamethylene group and their acid addition salts are therapeutically active as calcium antagonists.

Abstract: N-Aminoalkyl 1,5-benzothiazepines of the following formula (I): ##STR1## for the treatment of angina or hypertension or the prevention of heart attacks in mammals, in particular their use as coronary vasodilators.

Abstract: Calcium channel blocking activity is exhibited by compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein the stereochemistry at the chiral centers in the 3 and 4-positions of the benzothiazepine nucleus is cis, and whereinR.sub.1 is alkyl, aryl, arylalkyl, alkenyl or alkynyl;R.sub.2 and R.sub.5 are each independently hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen or trifluoromethyl; andR.sub.3 and R.sub.4 are each independently alkyl or cycloalkyl or R.sub.3 and R.sub.4 together with the nitrogen atom to which they are attached are pyrrolidinyl, piperidinyl or morpholinyl.

Abstract: Novel 1,5-benzothiazepine derivative of the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkanoyl and each of R.sup.2 and R.sup.3 is lower alkyl, and a pharmaceutically acceptable acid addition salt thereof are disclosed.Said derivative (I) and a salt thereof are useful as a hypotensive agent and/or a cerebral or coronary vasodilator.

Abstract: Novel condensed seven-membered ring compounds of the formula: ##STR1## [wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen, trifluoromethyl, lower alkyl or lower alkoxy, or both jointly form tri- or tetramethylene; R.sup.3 and R.sup.5 are independently hydrogen, lower alkyl or aralkyl; R.sup.4 is hydrogen or lower alkyl; R.sup.6 is a condensed or non-condensed hetero-alicyclic containing at least one atom of N, O and S as a ring-forming atom which may be substituted; A is an alkylene chain; n is 1 or 2] and salts thereof.These compounds exhibit inhibitory activity on angiotensin converting enzyme and so forth, and are of value as an agent for diagnosis, prevention and treatment of circulatory diseases, such as hypertension, cardiopathy and cerebral apoploxy.

Abstract: A piperazine derivative according to the present invention has the following general formula [I]: ##STR1## wherein R.sup.1 is --OH, --OR.sup.3, --SR.sup.3, --SOR.sup.3 or --SO.sub.2 R.sup.3 wherein R.sup.3 is alkyl group having 1 to 3 carbon atoms;R.sup.2 is --SO.sub.2 NH.sub.2, --SO.sub.2 NHR.sup.4, --SO.sub.2 NR.sup.4 R.sup.5, --COOH, --COOR.sup.4, --CONH.sub.2, --CONHR.sup.4, --CONR.sup.4 R.sup.5, --NHCONH.sub.2, --NHCSNH.sub.2, --NHCONHR.sup.4, --NHCOR.sup.4 or --NHSO.sub.2 R.sup.4 wherein R.sup.4 and R.sup.5 are independently alkyl group having 1 to 3 carbon atoms; orR.sup.1 and R.sup.2 together with carbon atoms to which they are attached form ##STR2## Z is --CO-- or --CH(OH)--; Ar is pyridyl or substituted or unsubstituted phenyl; andn is an integer of 3 to 5.An acid addition salt of the piperazine derivative having the above formula [I] is included in the present invention.

Abstract: Vasodilating activity is exhibited by compounds having the formula ##STR1## n is 2 or 3; X is oxygen or sulfur,R.sub.1 and R.sub.2 are each independently hydrogen alkyl, cycloalkyl, or allyl, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached are pyrrolidinyl, piperidinyl, or morpholinyl;R.sub.3 is alkyl, alkoxy, halogen, trifluoromethyl, or nitro;R.sub.4 is hydrogen, halogen, trifluoromethyl, or nitro; andR.sub.5 and R.sub.6 are each independently alkyl or cycloalkyl or R.sub.5 and R.sub.6 together with the nitrogen atom to which they are attached are pyrrolidinyl, piperidinyl, or morpholinyl.