Abstract: A diaminotrifluoromethylpyridine derivative of the formula (I) or its salt: ##STR1## wherein X is --CW.sup.1 R.sup.1, --COCOR.sup.2, --CW.sup.1 NHCOR.sup.2, --C(.dbd.W.sup.1 (W.sup.2 W.sup.3 or --CW.sup.1 N(R.sup.4)R.sup.5, and Y is alkyl, --CW.sup.3 R.sup.6, --COCOR.sup.7, --NHCOR.sup.7, --C(.dbd.W.sup.3)W.sup.4 R.sup.8, --(NH).sub.m SO.sub.2 R.sup.9, --(NH).sub.m SO.sub.2 OR.sup.10 or --(NH).sub.m SO.sub.2 N R.sup.11)R.sup.12, wherein each of R.sup.1, R.sup.6 and R.sup.9, which are independent from one another, is a chain hydrocarbon group which may be substituted, a monocyclic hydrocarbon group which may be substituted, a polycyclic hydrocarbon group which may be substituted, a monocyclic heterocycle group which may be substituted or a polycyclic heterocycle group which may be substituted, each of R.sup.2 and R.sup.7, which are independent from each other, is alkyl which may be substituted, alkoxy which may be substituted, phenyl which may be substituted or phenoxy which may be substituted, each of R.sup.

Abstract: This invention relates to compounds which are derivatives of cyclopentane which are useful as antihypertensive agents, to pharmaceutical compositions including such compounds, and to their use in treating hypertension.

Abstract: This invention relates to a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxygen, sulfur, --CH.dbd.CH--or --CH.dbd.N--; wherein R.sub.1 is alkyl, alkenyl or alkynyl of about 1 to 20 carbon atoms; wherein R is --CO.sub.2 R.sup.2, tetrazole, methylsulfonamide or benzenesulfonamide, wherein R.sup.2 is hydrogen, alkyl of 1 to 6 carbon atoms or a pharmaceutically acceptable cation and R.sup.3 is hydroxyl or halogen, having utility as LTB.sub.4 synthesis inhibitors.

Abstract: The present invention relates to the derivatives of the formula ##STR1## in the (S) configuration, to their addition salts and to their use in therapy, especially as drugs with analgesic properties.

Abstract: Thiourea derivatives represented by the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents a lower alkyl group, or R.sub.1 or R.sub.2 taken together represent a group having the formula --(CH.sub.2).sub.m --in which m is 4 or 5, R.sub.3 represents a lower alkyl group or a cycloalkyl group or a group having the formula--(CH.sub.2).sub.l --R.sub.4 in which R.sub.4 is a phenyl, naphthyl, pyridyl, furyl or thienyl group optionally having 1-3 substituents selected from the group consisting of lower alkyl, lower alkoxy, phenoxy, lower alkylthio, hydroxy, halogen, nitro, cyano and trifluoromethyl, and l represents an integer of 0 to 2 and n represents an integer of 1 to 5 or a physiologically acceptable salt thereof.The compounds of the invention are useful as a therapeutic agent for peptic ulcers which is also effective on prevention of the recurrence after discontinuation of the administration due to the antimicrobial activity against Helicobacter pyroli.

Abstract: A butenoic or propenoic acid derivative having the following formula in which G is an aryl or a heterocyclic ring, R11 and R12 are hydroben or an alkyl, X is sulfur or oxygen, R2 and R3 are hydrogen, an substituent such as an alkyl and J is pyridyl or phenyl having substituents and a heterocyclic ring may be formed between R2, R3 and J is provided here and is useful in the pharmacological field.

Abstract: The invention relates to novel pyridine derivatives of formula (I), ##STR1## wherein Q stand for a nitro or cyano group; andX.sup.1 and X.sup.2, independently from each other, represent hydrogen or halogen or a trifluoromethyl, a lower alkyl or alkoxy or nitro group bound to any of the carbon atoms of the phenyl ring.The invention further relates to pharmaceutical compositions containing these compounds and a process for their preparation.The compounds of formula (I) possess gastric acid secretion inhibiting, tissue-protecting, analgetic and mild antiinflammatory effects and are useful for therapeutical purposes.

Abstract: HMG-COA reductase-inhibiting compounds of the formula ##STR1## in which X represents a group of the formula --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,R represents a group of the formula ##STR2## R.sup.1 represents optionally substituted aryl, R.sup.2 represents --CH.sub.2 OR.sup.8 or --X--R, andR.sup.5 represents straight-chain or branched alkyl having up to 10 carbon atoms, orand their pharmaceutically acceptable salts.

Abstract: Compounds of having the general formula (I): ##STR1## and stereoisomers thereof, wherein R.sup.1 is hydrogen, halogen, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, COR or cyano; R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen, halogen or methyl, provided that R.sup.2, R.sup.3 and R.sup.4 are not all hydrogen and provided that when one of them is methyl then at least one of the other two is not hydrogen; ##STR2## wherein R.sup.5 is hydrogen, C.sub.1-4 alkyl (optionally substituted by hydrogen or cyano), optionally substituted benzyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, cyano, COR, C.sub.1-4 thioalkoxy, C.sub.1-4 thiohaloalkoxy or SNR.sup.7 R.sup.8 ; R.sup.7 and R.sup.8 are independently C.sub.1-4 alkyl or CO.sub.2 R; Y is oxygen or sulphur; R.sup.6 is C.sub.1-4 alkoxy, C.sub.1-4 thioalkoxy or --NR.sup.9 R.sup.10 ; and R.sup.9 and R.sup.10 are independently hydrogen, C.sub.1-4 alkyl, aryl or aralkyl or R.sup.9 and R.sup.

Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxphenyl-N'-diarylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis with urea and thiourea compounds.

Abstract: Novel carboxamides and sulfonamides are described having of the formulaR.sup.1 --A--(W).sub.a --X--(CH.sub.2).sub.b --(Y).sub.c --B--Z--COOR (I),in which R.sup.1, A, W, X, Y, B, Z, R, a, b and c are as provided in the description. These compounds are useful in the treatment of thromboses, apoplexy, myocardial infarct, inflammations, arteriosclerosis as well as in the treatment and prevention of tumors. These novel compounds are prepared by eliminating the protective groups in corresponding compounds with protected amidino or guanidino groups.

Abstract: Novel 3-amino-2,4-dialkylpyridine derivatives ##STR1## in which R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.6 alkyl, R.sup.3 is C.sub.1 -C.sub.12 alkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.1 -C.sub.4 alkyl substituted by C.sub.3 -C.sub.6 cycloalkyl, or C.sub.3 -C.sub.6 cycloalkyl substituted by C.sub.1 -C.sub.4 alkyl, R.sup.4 is hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, phenoxy, or phenoxy that is mono- or di-substituted by halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylamino, di-C.sub.1 -C.sub.4 alkylamino, C.sub.1 -C.sub.4 alkylcarbonylamino, C.sub.1 -C.sub.4 alkylcarbonyl, benzoyl, nitro, cyano, C.sub.1 -C.sub.4 alkoxycarbonyl, C.sub.1 -C.sub.4 haloalkyl or by C.sub.1 -C.sub.4 haloalkoxy, and Z is a bridge member --NH--CS--NH--, --N.dbd.C(SR.sup.5)--NH-- or --N.dbd.C.dbd.N-- wherein R.sup.5 is C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.5 alkenyl, can be used as pesticides. Preferably, insects and arachnids can be controlled.

Abstract: There are disclosed novel 1-nitro-2,2-diaminoethylene derivatives of formula I ##STR1## wherein X is chlorine, fluorine, unsubstituted or halogen-substituted C.sub.1 -C.sub.5 alkyl; unsubstituted or halogen-substituted C.sub.1 -C.sub.5 alkoxy, unsubstituted or halogen-substituted C.sub.1 -C.sub.5 alkylthio, unsubstituted or halogen-substituted alkylsulfinyl, unsubstituted or halogen-substituted alkylsulfonyl; or also nitro, cyano, thiocyanato, C.sub.3 -C.sub.5 haloalkenyl, C.sub.3 -C.sub.5 haloalkynyl, hydroxy, C.sub.1 -C.sub.5 alkoxycarbonyl, amino, C.sub.1 -C.sub.4 dialkylamino, C.sub.1 -C.sub.5 alkylcarbonyl, C.sub.1 -C.sub.5 alkylcarbamoyl or C.sub.1 -C.sub.5 alkylcarbonyloxy,n is an integer from 0 to 4,R.sub.1 is hydrogen, C.sub.1 -C.sub.5 alkyl or C.sub.3 -C.sub.7 cycloalkyl,R.sub.2 is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.7 cycloalkyl,R.sub.3 is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.7 cycloalkyl, benzyl or pyridinylmethyl, or R.sub.2 and R.sub.

Abstract: A pharmaceutical product comprising a potassium channel activator antihypertensive agent and a .beta.-blocker antihypertensive agent as a combined preparation for simultaneous, separate or sequential use in therapy of hypertension.

Abstract: Prostaglandin analogues exhibiting activity at thromboxane receptor sites have been prepared.

Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein K is oxygen or sulphur; Z is optionally substituted aryl or optionally substituted heteroaryl; X is O, S(O).sub.n, NR.sup.4, CR.sup.1 R.sup.2, CHR.sup.5, CO, CR.sup.1 (OR.sup.2), C.dbd.CR.sup.1 R.sup.2, CHR.sup.1 CHR.sup.2, CR.sup.1 .dbd.CR.sup.2, CHR.sup.1 CR.sup.2 .dbd.CH, C.dbd.C, OCHR.sup.1, CHR.sup.1 O, OCHR.sup.1 O, S(O).sub.n CHR.sup.1, S(O).sub.n CHR.sup.1 O, CHR.sup.1 S(O).sub.n, CHR.sup.1 OSO.sub.2, NR.sup.4 CHR.sup.1, CHR.sup.1 NR.sup.4, CO.sub.2, O.sub.2 C, SO.sub.2 O, OSO.sub.2, CO.CO, COCHR.sup.1, COCHR.sup.1 O, CHR.sup.1 CO, CHOH.CHR.sup.1, CHR.sup.1.CHOH, ##STR2## CONR.sup.4, OCONR.sup.4, NR.sup.4 CO, CSNR.sup.4, OCS.NR.sup.4, SCO.NR.sup.4, NR.sup.4 CO.sub.2, NR.sup.4 CS, NR.sup.4 CSO, NR.sup.4 COS, NR.sup.4 CONR.sup.4, S(O).sub.n NR.sup.4, NR.sup.4 S(O).sub.n, CS.sub.2, S.sub.2 C, CO.S, SCO, N.dbd.N, N.dbd.CR.sup.1, CR.sup.1 .dbd.N, CHR.sup.1 CHR.sup.2 CH(OH), CHR.sup.1 OCO, CHR.sup.1 SCO, CHR.sup.1 NR.sup.

Abstract: Insecticides of the general formula ##STR1## wherein R.sub.1 is an optionally substituted 5- to 10-member heterocyclic moiety; R.sub.2 is an optionally substituted alkyl, cycloalkyl or alkenyl moiety; X is oxygen, sulfur or --NH--; and R.sub.3 is: (a) an optionally substituted 3-phenoxyphenalkyl, 3-phenoxypyridylalkyl, 3-(pyridyloxy)phenalkyl, 3-phenylaminophenoalkyl, 3-benzylphenalkyl or 3-benzyloxyphenalkyl moiety; (b) a benzylfuranylmethyl moiety; (c) a 3- or 4-substituted benzyl or tetrafluorobenzyl moiety; (d) 4-phenoxy-2-butyn-2-yl; or (e) 2-methyl-3-phenylbenzyl.

Abstract: The invention relates to a pharmaceutical composition as a therapeutic agent for ischemic disease comprising a compound of the formula ##STR1## wherein R.sup.1 is carbamoyl substituted with morpholino (lower) alkyl, thiomorpholino(lower)alkyl or lower alkylamino(lower)alkyl; or ureido substituted with lower alkylamino(lower)alkyl; andR.sup.2 is phenyl substituted with nitro, andR.sup.4 is lower alkyl; orR.sup.2 is lower alkyl, andR.sup.4 is phenyl substituted with nitro;with proviso that R.sup.1 is carbamoyl substituted with thiomorpholino(lower)alkyl or lower alkylamino(lower)alkyl; or ureido substituted with lower alkylamino(lower)alkyl when R.sup.4 is lower alkyl; or its salt, as an active ingredient, in association with a pharmaceutically acceptable, substantially nontoxic carrier or excipient.

Abstract: Compounds presented by the general formula: ##STR1## wherein Y is oxygen, R.sup.2 is H, alkyl, alkoxy, alkoxymethyl, --COOR.sup.3, --CH.sub.2 COOR.sup.3, --CH.dbd.CH--COOR.sup.3, halogen, --CF.sub.3, --COR.sup.4, --OCOR.sup.4, --CH.sub.2 OCOR.sup.4, --SO.sub.2 R.sup.4, --OSO.sub.2 R.sup.4, --CONR.sup.5 R.sup.6, --OCONR.sup.5 R.sup.6, --SO.sub.2 NR.sup.5 R.sup.6, --COHN-- SO.sub.2 NR.sup.5 R.sup.6, --NHSO.sub.2 R.sup.7, --NO.sub.2, --OH, --CH.sub.2 OH, guanidino, benzyloxy, guanidinophenylthiomethyl, morpholinosulfonylphenoxymethyl, pyridyloxymethyl, or (1,1-dioxothiazol-3-yl)carbonyl, or when Y is sulfur, R.sup.2 is H, alkyl, alkoxy, halogen, --COOR.sup.3, --CH.sub.2 COOR.sup.3, --NO.sub.2, or --SO.sub.2 NR.sup.5 R.sup.6, and n represents an integer of one to five, and when n represents more than two, each or R.sup.

Abstract: Novel fungicidal pyridyl cyclopropane carboxamidines having the general structural formula ##STR1## and tautomers thereof whereinR is selected from the group consisting of hydrogen, pyridyl, substituted pyridyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.6 alkyl, acyl, carbamoyl, sulfonyl and cyano;R.sub.1 is selected from the group consisting of halogen, C.sub.1 -C.sub.3 alkoxy and C.sub.1 -C.sub.3 alkenyloxy;R.sub.2 is selected from the group consisting of hydrogen and C.sub.1 -C.sub.3 alkyl;R.sub.3 is selected from the group consisting of hydrogen, alkyl, aryl or arylalkyl;and fungicidally acceptable organic and inorganic salts thereof.

Abstract: N-(2,6-Disubstitutedphenyl)-N'-3- and 4-pyridinyl ureas and pharmaceutically acceptable acid addition salts having anticonvulsant activity are described as well as a process for their manufacture, formulations containing the compounds and a method of treating epilepsy using the compounds in unit dosage form.

Abstract: Certain trans-6,6'-[[(substituted)pyridin-3,5-diyl]-dialkane- and dialkene-diyl]bis [tetrahydro-4-hydroxypyran]-2-ones and the corresponding ring-opened acids derived therefrom are potent inhibitors of the enzyme 3-hydroxy-3-methyl-glutaryl-coenzyme A reductase (HMG-CoA reductase) and are useful as hypocholesterolemic and hypolipidemic agents.

Abstract: There are described compounds of the formula ##STR1## where R is hydrogen, loweralkyl, arylloweralkyl or loweralkylcarbonyl;X is O or NR.sub.1, R.sub.1 being hydrogen, loweralkyl or loweralkylcarbonyl; andY is hydrogen, loweralkyl, loweralkoxy, halogen or trifluoromethyl;which compounds are useful as topical antiinflammatory agents for the treatment of skin disorders.

Abstract: Certain organic compounds derived from urea or thiourea having insecticidal activity and methods of their preparation are disclosed. The compounds according to the invention have been found to interfere with the mechanism of metamorphoses which occurs in insects. Hence, the substances according to the invention are specifically active against insects. Owing to this specificity and because of the absence of phytotoxicity effects, the compounds of this invention are of prime importance.

Abstract: A method for the treatment and/or prophylaxis of disorders associated with pulmonary hypertension and/or disorders associated with right heart failure, in mammals, such as humans, which method comprises administering to the mammal in need of such treatment and/or prophylaxis an effective and/or prophylactic amount of pinacidil; or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof.

Abstract: The growth of livestock is promoted by the new compounds of the formula ##STR1## in which R.sup.1 represents hydrogen, alkyl, halogen, halogenoalkyl, hydroxyl, cyano, alkoxycarbonyl, aminocarbonyl, mono- and dialkylaminocarbonyl, alkoxy, halogenoalkoxy, halogenoalkylthio or NHSO.sub.2 -alkyl,R.sup.2 represents hydrogen, hydroxyl, alkoxy or the --NR.sup.11 R.sup.12 radical,R.sup.3 represents the radicals mentioned in the case of R.sup.1R.sup.4 represents hydroxyl, acyloxy or alkoxy,R.sup.5 represents hydrogen or alkyl,R.sup.6 represents hydrogen or alkyl,R.sup.7 represents hydrogen or alkyl,R.sup.8 represents hydrogen or alkyl,X represents C.sub.1 -C.sub.10 -alkylene or a direct bond,Y represents oxygen or a direct bond,R.sup.9 represents hydrogen, C.sub.1 -C.sub.10 -alkyl which is optionally substituted by hydroxyl, alkoxy, acyloxy or the --NR.sup.13 R.sup.14 radical, or represents the COR.sup.15 radical or the O--Z--R.sup.16 radical,Z represents C.sub.1 -C.sub.10 -alkylene, C.sub.1 -C.sub.

Abstract: Certain organic compounds derived from urea or thio-urea having insectical activity and methods of their preparation are disclosed. The compounds according to the invention have been found to interfere with the mechanism of metamorphoses which occurs in insects. Hence, the substances according to the invention are specifically active against insects. Owing to this specificity and because of the absence of phytotoxicity effects, the compounds of this invention are of prime importance.

Abstract: The invention relates to compounds for treatment of hypertension, and cardiovascular and cerebrovascular diseases, which compounds are of the formula: ##STR1## wherein R.sup.1 is piperazinyl(lower)alkyl, carbamoyl substituted with piperazinyl(lower)alkyl, or piperazinylcarbonyl, in each of which a piperazinyl group may be substituted with lower alkyl, andR.sup.3 is hydrogen or halogen;R.sup.2 is phenyl substituted with nitro, andR.sup.4 is lower alkyl or halo(lower)alkyl; orR.sup.2 is lower alkyl, andR.sup.4 is phenyl substitured with nitro;and a pharmaceutically acceptable salt thereof.

Abstract: Acrylic acid derivatives having the formula (I): ##STR1## and stereoisomers thereof, wherein W is R.sup.1 O.sub.2 C--C.dbd.CH--ZR.sup.2, R.sup.1 and R.sup.2 are alkyl or fluoroalkyl groups, and Z is oxygen or sulphur; A, B, D and E are hydrogen, halogen, hydroxy or optionally substituted alkyl, alkoxy, aralkyl, arylalkoxy, alkenyl, alkynyl, aryl, aryloxy, arylthio, heteroaryloxy, heteroarylthio, acyloxy, amino, arylazo or acylamino, nitro, cyano, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --CR.sup.3 .dbd.NR.sup.4, --N.dbd.CR.sup.3 R.sup.4 or --S(O).sub.n R.sup.3 groups; any two of the groups A, B, D and E, when they are in adjacent positions on the ring, optionally join to form a fused ring, n is 0, 1 or 2; and R.sup.3 and R.sup.4 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl or optionally substituted aryl or aralkyl; and metal complexes thereof. These compounds are useful as fungicides, insecticides, nematicides or plant growth regulators.

Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.

Abstract: A method for the treatment and/or prophylaxis of incontinence in mammals, which method comprises administering to the mammal an effective amount of the compound pinacidil or a pharmaceutically acceptable salt or solvate thereof.

Abstract: The invention relates to new benzoylurea compounds having insecticidal and acaricidal activity, of the general formula ##STR1## wherein R.sub.1 is a hydrogen atom or represents 1 or 2 halogen atoms;Ar is a para-phenylene group or a para-pyridylene group, which groups may be substituted with 1 or 2 substituents selected from the group consisting of chlorine, methyl and trifluoromethyl;B is an oxygen atom or represents a group having the formula ##STR2## wherein R.sub.

Abstract: Certain tetrasubstituted alkyl, aryl, pyridinyl, piperidinyl, and piperazinyl urea compounds stimulate the release of acetylcholine and are thus useful analgesic agents for alleviating pain or as cholinergic agents which are useful for the amelioration of the symptoms of cognitive decline in the elderly.These compounds have the general formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.4 are phenyl or substituted phenyl, and R.sub.3 is pyridinyl.Pharmaceutical compositions including these compounds as well as methods for the preparation of the compounds are also disclosed.

Abstract: This invention relates to a method for antagonizing induced the neuromuscular blocking effects of certain therapeutic agents and pathological disorders in mammals, which comprises administering to said mammal an antagonizing-effective amount of a compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, cycloalkyl, cycloalkyl-lower alkyl or hydroxyalkyl, or, when taken together, form a heterocyclic ring with the nitrogen to which they are attached, with the proviso that both are not hydrogen;R.sub.3 is hydrogen or alkyl; andR.sub.4 is hydrogen, alkyl, alkenyl, alkynyl, halogen or acyl; or a salt thereof with acids.

Abstract: New semicarbazide derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen,R.sup.2 is hydrogen, lower alkyl, ar(lower)alkyl, lower alkenyl or aryl,R.sup.3 is lower alkyl, ar(lower)alkyl, lower alkenyl or aryl, orR.sup.2 and R.sup.3 are taken together to form (C.sub.2 -C.sub.6)alkylidene group optionally substituted with aryl or taken together with the adjacent nitrogen atom to form a saturated or unsaturated, 5- or 6-membered heterocyclic group optionally substituted with aryl; orR.sup.1 and R.sup.2 are taken together with the adjacent nitrogen atoms to form a saturated or unsaturated, 5- or 6-membered heterocyclic group or 1,2-diazaspiroalkane-1,2-diyl group,R.sup.3 is hydrogen, lower alkyl, ar(lower)alkyl, lower alkenyl or aryl;R.sup.4 is aryl which may have substituent(s) selected from lower alkyl, halogen, lower alkoxy, lower alkylamino, halo(lower)alkyl, hydroxy, lower alkanoyl, esterified carboxy and carboxy,R.sup.

Abstract: Highly effective and orally administrable sustained-release preparation of an antihypertensive agent, pinacidil (N"-cyano-N-4-pyridyl-N'-1,2,2-trimethylpropylguanidine) comprising a rapid-release and a slow-release component at a ratio of about 7:3 to about 1:9 by pinacidil weight.

Abstract: The invention relates to guanidine derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention there is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 and R.sup.2, same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-15C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R.sup.1 and R.sup.2 is halogen substituted, or R.sup.2 is hydrogen and R.sup.1 is R.sup.5 --E--W in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O,S or NR.sup.6 in which R.sup.6 is H or 1-6C alkyl, R.sup.5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R.sup.5 and R.sup.

Abstract: A method of combating slugs and snails comprising applying to a plant or to an area from which it is desired to exclude such slugs and snails a repellent amount of at least one benzoyl urea of the formula ##STR1## in which R, R.sup.1 and R.sup.2 each independently is hydrogen, alkyl, alkoxy or halogen,R.sup.3 and R.sup.4 each independently is hydrogen, alkyl, aralkyl, aryl, alkoxy, aralkoxy, aryloxy, alkylthio, aralkylthio or arylthio,A is an aromatic or heteroaromatic radical, andX and X.sup.1 each independently is oxygen or sulphur.

Abstract: The invention relates to carbonyl derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention where is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 and R.sup.2, same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R.sup.1 and R.sup.2 is halogen substituted, or R.sup.2 is hydrogen and R.sup.1 is R.sup.5 -E-W in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O, S, SO, SO.sub.2 or NR.sup.6 in which R.sup.6 is H or 1-6C alkyl, R.sup.5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R.sup.5 and R.sup.6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring, or R.sup.2 is H and R.sup.

Abstract: N-(2,6-Disubstitutedphenyl)-N'-3- and 4-pyridinyl ureas and pharmaceutically acceptable acid addition salts having anticonvulsant activity are described as well as a process for their manufacture, formulations containing the compounds and a method of treating epilepsy using the compounds in unit dosage form.

Abstract: This invention provides a method of treating asthma in mammals which comprises administering an effective amount of Pinacidil.

Abstract: Substituted 2-amino-4(1H)pyridones are provided which are renal vasodilators and bronchodilators.

Abstract: New pharmaceutical preparation containing pinacidil (N"-cyano-N-4-pyridyl-N'-1,2,2-trimethylpropylguanidine) in slow-release form, providing more uniform absorption rates and resulting blood levels when administered to the individual patients.

Abstract: There are described compounds of formula: ##STR1## in which one of R and R.sup.1 is F or Cl and the other is H, F or Cl;X is a 1,4-phenylene or pyridyl bound in positions 2 and 5, optionally substituted;Y is a phenyl, 2- or 3-pyridyl, optionally substituted.The compounds of formula I are endowed with a high insecticide activity which is mainly directed against insect larvae and eggs.

Abstract: Compounds of the formula ##STR1## in which R.sup.1 is an optionally substituted aryl or heteroaryl radical,R.sup.2 is an alkyl or alkenyl radical which is optionally substituted by alkoxy or cycloalkyl, or an optionally substituted aryl or heteroaryl radical, and X is an optionally aklyl-substituted methylene radical or a direct bond, but if X is a direct bond R.sup.2 is not aryl,or physiologically acceptable acid addition salts thereof, exhibit activity on the circulation system particularly as hypotensive agents.

Abstract: Described herein are compounds of the formula ##STR1## wherein R.sub.1 is alkyl of from 1 to about 5 carbon atoms, alkenyl of from 2 to about 5 carbon atoms, alkynyl of from 3 to about 5 carbon atoms, cycloalkyl of from 3 to about 7 carbon atoms, alkylcarboxymethyl wherein the alkyl portion is from 1 to about 5 carbon atoms, arylcarboxymethyl wherein the aryl portion is from 6 to about 10 carbon atoms, aryl of from 6 to about 10 carbon atoms, or aralkyl wherein the alkyl portion is from 1 to about 5 carbon atoms and the aryl portion is from about 6 to about 10 carbon atoms; R.sub.2 and R.sub.

Abstract: Compounds of the formula ##STR1## where R is a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group, a phenoxy group or a phenyl-C.sub.1 -C.sub.2 -alkoxy group, R.sub.1 is hydrogen or a C.sub.1 -C.sub.4 -alkyl group and R.sub.5 is hydrogen or a C.sub.1 -C.sub.4 -alkyl group and the groups R.sub.2, R.sub.3, and R.sub.4 are the same or different and are hydrogen, halogen atoms, C.sub.1 -C.sub.4 alkyl groups, C.sub.1 -C.sub.4 -alkylcarbonyl group, the aminosulfonyl group, the trifluoromethyl group and their acid addition salts are effective as antiepileptics.

Abstract: The present invention is directed to 1-benzoyl-3-(arylpyridyl)urea compounds useful as insecticides.