Abstract: Quinuclidine derivatives represented by general following general formula (I), salts, N-oxides or quaternary ammonium salts thereof, and medicinal compositions containing the same. The compound has an antagonistic effect on muscarinic M3 receptors and is useful as a preventive or remedy for urologic diseases, respiratory diseases or digestive diseases.

Abstract: Quinuclidine derivatives represented by general following general formula (I), salts, N-oxides or quaternary ammonium salts thereof, and medicinal compositions containing the same. ##STR1## The compound has an antagonistic effect on muscarinic M.sub.3 receptors and is useful as a preventive or remedy for urologic diseases, respiratory diseases or digestive diseases.

Abstract: An azole derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof, having both of a leukotriene antagonistic effect and a thromboxane A2 antagonistic effect and being useful in preventing or treating allergic diseases, ischemic heart diseases or ischemic brain diseases, and a medicinal composition containing the same as the active ingredient, wherein R.sup.1 and R.sup.2 may be the same or different and represent each hydrogen, cycloalkyl, etc., or R.sup.1 and R.sup.2 together with (a) may form a fused ring (b) or (c) which may be substituted by optionally substituted lower alkyl, amino, etc.; R.sup.3, R.sup.6, R.sup.7, R.sup.8 may be the same or different and represent each hydrogen, amino, etc.; R.sup.4 represents cyano, tetrazolyl, --COOR.sup.9, etc.; R.sup.5 represents hydrogen or lower alkyl; D represents optionally substituted lower alkylene; X and Z may be the same or different and represent each oxygen or sulfur; Y represents --N.dbd. or --CH.dbd.

Abstract: 1,8-Naphthyridine derivatives represented by the following general formula (I), salts thereof, hydrates thereof and solvates thereof. ##STR1## They have an activity to inhibit type IV phosphodiesterase and are useful as agents for the prevention and treatment of respiratory diseases, inflammatory diseases accompanying organ transplantation, systemic or local arthropathy, proliferative diseases, micturition-related diseases and diseases in which tumor necrosis factor (TNF) and other cytokine (IL-1, IL-6 or the like) are concerned.

Abstract: A triazolylated tertiary amine compound represented by general formula (I) or a salt thereof, having an aromatase inhibitory activity and being useful for preventing and treating breast cancer, mastopathy, endometriosis, prostatomergaly, etc., wherein A represents a single bond, lower alkylene or carbonyl; B represents lower alkyl, aryl, a 5- or 6-membered heterocyclic group, or a bicyclic fused heterocyclic group; D represents aryl, a 5- or 6-membered heterocyclic group, or a bicyclic fused heterocyclic group; and E represents 4H-1,2,4-triazolyl, 1H-1,2,4-triazolyl or 1H-1,2,3-triazolyl.

Abstract: A process is provided for producing diastereoisomer A or a pharmaceutically acceptable acid addition salt of 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-(1-benzylpyrrolidin-3-yl) ester 5-methyl ester which comprises subjecting a mixture of diastereoisomers A and B of 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-(1-benzylpyrrolidin-3-yl) ester 5-methyl ester to column chromatography using silica gel as a carrier and a mixture of ethyl acetate and acetic acid as an eluant, and then separating the acetate of diastereoisomer A from the eluate, or treating the acetate with a base, or further treating the resulting diastereoisomer A with a pharmaceutically acceptable acid.

Abstract: A substituted tertiary amino compound represented by general formula (I) or a pharmaceutically acceptable salt thereof. They have an aromatase inhibiting activity and are useful as a prophylactic and/or therapeutic agent for breast cancer, mastopathy, endometriosis, prostatic-hypertrophy, and so forth.

Abstract: Crystal D or E of 1-hydroxy-2-(imidazo[1,2-a]pyridin-3-yl)ethane -1,1-bis(phosphonic acid) monohydrate having specified lattice spacing and relative intensity in the powder X-ray diffraction spectrum obtained by using Cu-K.alpha. radiation and a dehydration peak temperature of 135.degree. to 149.degree. C. or 160.degree. to 170.degree. C. according to TG-DSC thermogravimetric analysis; and to a solid pharmaceutical preparation containing the same. The crystals are useful for producing a stable solid pharmaceutical preparation of the above compound which has an excellent drug efficacy for diseases wherein increased bone resorption participates, such as osteoporosis.

Abstract: A dextro-rotatory optical isomer of diastereoisomer A of (.+-.)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-(1-benzylpyrrolidin-3-yl)ester 5-methyl ester is provided having the formula ##STR1## and wherein the melting point of the hydrochloride of the dextro-rotatory optical isomer is 223.degree. to 230.degree. C. (decomp.), or a pharmaceutically acceptable acid addition salt thereof.

Abstract: The diastereoisomer A of a dihydropyridine-3,5-dicarboxylic acid ester derivative is provided as well as its pharmaceutically acceptable acid addition salts. The invention further discloses a process for producing the compounds and their use as medicaments in imparting vasodilating 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: 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: Substituted aminomethylenebis(phosphonic acid) derivatives represented by the general formula: ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may be the same or different, each represents a hydrogen atom or a lower alkyl group; "m" is zero or represents an integer from 1 to 4; and a ring "A" represents a cycloalkenyl group having 5 to 8 carbon atoms, a bicycloheptyl group, a bicycloheptenyl group or a saturated heterocyclic group having 4 to 7 carbon atoms and containing an oxygen atom, a sulfur atom, a sulfinyl group (--SO--) or a sulfonyl group (--SO.sub.2 --), or pharmaceutically acceptable salts thereof.

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 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: (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: Substituted aminomethylenebis(phosphonic acid) derivatives represented by the general formula: ##STR1## in which R.sup.1, R.sup.2 R.sup.3 and R.sup.4 may be the same or different, each represents a hydrogen atom or a lower alkyl group; "m" is zero or represents an integer from 1 to 4; and a ring "A" represents a cycloalkenyl group having 5 to 8 carbon atoms, a bicycloheptyl group, a bicycloheptenyl group or a saturated heterocyclic group having 4 to 7 carbon atoms and containing an oxygen atom, a sulfur atom, a sulfinyl group (--SO--) or a sulfonyl group (--SO.sub.2 --),or pharmaceutically acceptable salts thereof.

Abstract: A dihydropyridine compound of the following general formula (I) or a salt thereof: ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, each represents a C.sub.1 to C.sub.10 alkyl group, a lower alkyl group which is interrupted by oxygen atom(s), or a lower alkyl group substituted by C.sub.3 to C.sub.6 alicyclic group(s); R.sup.3 and R.sup.4, which are the same or different, each represents a lower alkyl group; R.sup.5 and R.sup.6, which are the same or different, each represents a hydrogen atom, a nitro group, a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a lower alkylsulfonyl group, or a lower alkylsulfinyl group; R.sup.7 and R.sup.8, which are the same or different, each represents a hydrogen atom, a halogen atom, a cyano group, a lower alkoxy group, or a lower alkanoylamino group, or R.sup.7 may combine with R.sup.8 to form a naphthyl group together with the adjacent phenyl group; A represents a single bond, a vinylene group (--CH.dbd.