Abstract: A series of 5-halopyrimidin-2-ylpiperazinylalkyl derivatives having useful anti-ischemic properties for treatment and prevention of dirorders resulting from brain and/or spinal cord anoxia.

Abstract: Novel polycyclic quinoline, naphthyridine and pyrazinopyridine derivatives are disclosed which are useful for treating allergic reactions, inflammation, peptic ulcers, hypertension, and hyperproliferative skin diseases and for suppressing the immune response in mammals. Methods for preparing said compounds are also disclosed.

Abstract: N-hetaryl imidazole derivatives of general Formula I ##STR1##are disclosed in whichHet represents an optionally substituted monocyclic or bicyclic heteroaromate,R.sup.3 represents hydrogen, a straight or branched C.sub.1-6 -alkyl group, or a C.sub.1-6 -alkoxy-alkyl group, andR.sup.4 represents --COOR.sup.5 --CONR.sup.6 R.sup.7 --CN, ##STR2##with R.sup.5 meaning hydrogen, a straight or branched C.sub.1-6 -alkyl group, R.sup.6 and R.sup.7 are the same of different and represent hydrogen or a straight, branched, or cyclic alkyl group with up to 7 carbon atoms or, together with the nitrogen atom, form a saturated five or six ring optionally containing another heteroatom and R.sup.8 means hydrogen or a straight, branched or cyclic alkyl group with up to 7 carbon atoms.

Abstract: 2-Amino and 2-thio-4-substituted-5-(hydroxy or alkoxy)-pyrimidines, which may be 6-substituted, and derivatives thereof are disclosed. The compounds are inhibitors of leukotriene synthesis and are, therefore, useful for the treatment of pulmonary, inflammatory, dermatological, allergic and cardiovascular diseases. The compounds are also cytoprotective and therefore, useful in the treatment of peptic ulcers.

Abstract: This invention provides compositions comprising a physiologically-active agent and a compound represented by the general formula ##STR1## wherein X may represent sulfur, oxygen or 2 hydrogen radicals; Y may represent --CH.sub.2 --, --NH-- or oxygen; n and m are integers of from 1 to 3; p is an integer of from 3 to 17; q is 2, 4, 6 or 8; wherein p.gtoreq.9; and R' is selected from the group consisting of H, a lower alkyl group having from 1 to 4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkanoyl. These compositions are useful in topical or transdermal applications of the physiologically-active agent.

Abstract: A compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is hydrogen; R.sup.2 is (C.sub.1 -C.sub.15) alkyl, (C.sub.3 -C.sub.15)alkenyl, phenyl, substituted phenyl, (C.sub.7 -C.sub.20)-phenylalkyl, or substituted (C.sub.7 -C.sub.20)phenylalkyl wherein the substituents on the substituted phenyl and substituted phenylalkyl are independently one or two of fluoro, chloro, (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3 alkoxy, and trifluoromethyl; or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a pyrrolodinyl, substituted pyrrolidinyl, piperidyl or substituted piperidyl group, wherein the substituents on said substituted pyrrolidinyl and piperidyl groups are independently one of (C.sub.1 -C.sub.6)alkyl, phenyl, and (C.sub.7 -C.sub.9)phenylalkyl; and R.sup.3 is hydrogen, (C.sub.1 -C.sub.6)alkyl, phenyl, substituted phenyl, (C.sub.7 -C.sub.9)phenylalkyl, or substituted (C.sub.7 -C.sub.

Abstract: This invention relates to imidazolidinone compounds of the formula ##STR1## wherein Q is methylene group or a single bond:R is a heterocyclic group selected from the group consisting of pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl and 1,3-thiazolyl which may be unsubstituted or with a substituent selected from the group consisting of lower alkyl, lower alkoxy and halogen atom, wherein R is bonded to Q or, when Q is a single bond, to the imidazolidinone ring, through the carbon atom of R;the ring A is an unsubstituted phenyl or a substituted phenyl having 1 or 2 substituent(s) selected from the group consisting of lower alkyl, lower alkoxy, halogen, lower alkylthio, trihalogeno-lower alkyl and nitro;Y is vinylene group or ethynylene;m is a integer from 1 to 6 andn is 0, 1 or 2,or a pharmacetically acceptable salt thereof.These compounds aer useful as cerebral activators, anti-depressants and nootropic drugs.

Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comnprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## wherein X represents sulfur, oxygen or 2 hydrogen radicals; Y represents --CH.sub.2 --, --NH-- or oxygen; n and m are integers of from 1 to 3; p is an integer of from 3 to 17; wherein p.gtoreq.9; q is 2, 4, 6 or 8; and R' is selected from the group consisting of H, a lower alkyl group having from 1 to 4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkanoyl.

Abstract: Aryl-substituted naphthyridines and pyridopyrazines are disclosed which are useful in treating allergic reactions, inflammation, peptic ulcers and/or hyperproliferative skin disease. Pharmaceutical compositions and methods of treatment employing such compounds are also disclosed.

Abstract: Quaternary 8-(alkyldithio)-1-(2-pyrimidyl)-quinolinium salts, inhibitors of the H.sup.30 /K.sup.+ ATPase enzyme, are useful in the treatment of ulcers.

Abstract: The present invention relates to novel pyrimidine derivatives of the general formula ##STR1## wherein R.sup.1 represents a pyrazolyl, imidazolyl, or triazolyl group, R.sup.2 represents hydrogen atom or lower alkyl group, R.sup.3 represents a halo, amino, lower alkoxy, pyrazolyl, imidazolyl, triazolyl, piperidinyl, or aryloxy group, one of X or Y represents N and the other of X or Y represents CH, and the salts thereof.These derivatives may be used in the treatment of peptic ulcer disease.

Abstract: Certain 8 to 12 membered cycloalka-[b]-pyrazolo[3,4,-d]-pyridin-3- one compounds which are useful as benzodiazepine receptor modulators are disclosed.

Abstract: A series of diazinylpiperidine compounds of Formula I ##STR1## wherein X is an ethylene chain or a 1,2-benzo ring; Y is carbonyl or methylene; R.sup.1 is hydrogen or lower alkyl; and Z is an R.sup.2, R.sup.3 -disubstituted diazinyl ring selected from pyridazine, pyrimidine, and pyrazine ring systems. Pharmacologic and neuroanatomical testing demonstrates that compounds of the series act to enhance cerebral function in mammals, particularly when there is a deficit in normal cerebral functioning. Specific pharmacologic test results indicate that compounds of Formula I possess cognition and memory enhancing activity.

Abstract: A sustained absorption theophylline-containing pellet for oral administration comprises a core of theophylline or a pharmacological equivalent thereof and an organic acid embedded in a polymeric material in a multi-layer arrangement and an outer membrane which permits release of the theophylline at a controlled rate in an aqueous medium. The pellet has a dissolution rate in vitro in an aqueous medium, which when measured in a basket assembly according to U.S. Pharmacopoeia XX at 37.degree. C. and 75 r.p.m., is not more than 15% of the total theophylline after 2 hours of measurement in a buffer solution at pH 7.5. Not more than 35% of the total theophylline is released after a total of 7 hours of measurement and not more than 65% of the total theophylline is released after a total of 13 hours.

Abstract: The compound of the formula ##STR1## wherein X is a cyclic group which may optionally be substituted; Y is a carboxyl group which may optionally be esterified or amidated; Z is --CH.dbd.CH--CH.dbd.CH--, --S--(CH.sub.2).sub.l --S-- (l is an integer of 1 to 3), --N.dbd.CH--CH.dbd.N-- or --(CH.sub.2).sub.m -- (m is an integer of 3 to 5); ring A may optionally be substituted with halogen, nitro, amino, alkanoylamino, alkoxycarbonyl, carboxyl or carbamoyl; and n is an integer of 1 to 3, and salts thereof. The compounds display a strong antianxiety effect to mammalian animals and are useful for the prevention or treatment of a disease such as psychoromatic disease and anxiety neurosis.

Abstract: Pyridyloxy derivatives represented by the general formula: ##STR1## wherein the substituted group Z is either one of the following groups: ##STR2## were prepared. These derivatives exert antagonism against Histamine H2-receptors and hence are efficacious for the treatments of digestive ulcers.

Abstract: 1-Phenyl-3-benzazepine compounds are useful in treating gastrointestinal motility disorders. A particular compound of this invention is 8-hydroxy-3-methyl-1-phenyl-7-phenylthio-2,3,4,5-tetrahydro-1H-3-benzazepi ne.

Abstract: Buspirone and its pharmaceutically acceptable salts are useful in the clinical improvement of short term memory.

Abstract: A series of novel 2-substituted 4-amino-6,7-dimethoxyquinoline derivatives have been prepared, including their pharmaceutically acceptable acid addition salts. These particular compounds are useful in therapy as highly potent antihypertensive agents. Preferred member compounds include 4-amino-2-[4-(2-furoyl)piperazin-1-yl]-6,7-dimethoxyquinoline, 4-amino-2-[4-(1,4-benzodioxan-2-carbonyl)piperazin-1-yl]-6,7-dimethoxyquin oline and 4-amino-6,7-dimethoxy-2-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinol-2-yl)qu inoline, respectively. Methods for preparing these compounds from known starting materials are provided.

Abstract: A method for the treatment of gastrointestinal disorders in a patient which comprises administering to the patient a gastric anti-secretory effective amount of a 2-amino-5-hydroxy-4-methylpyrimidine or a substituted amino derivative thereof, optionally in admixture with an additional gastric anti-secretory agent.

Abstract: Microbicidally active novel 1-heteroaryl-4-aryl-pyrazolin-5-ones of the formula ##STR1## in which R represents hydrogen or alkyl,R.sup.1 represents halogen, hydroxyl, optionally substituted alkyl, optionally substituted alkoxy, optionally substituted phenoxy, a radical --S(O).sub.p -- alkyl which is optionally substituted in the alkyl part, nitro, optionally substituted amino or a fused-on carbocyclic or heterocyclic radical,p represents an integer 0, 1 or 2,R.sup.2 represents halogen or optionally substituted alkyl, or represents alkoxy, alkylmercapto, nitro, cyano, carboxamide or a fused-on carbocyclic radical,m represents an integer from 0 to 5,n represents an integer from 0 to 4, it being possible for the substituents to be identical or different when m and/or n represent a number greater than 1, andX, Y and Z are identical or different and represent a nitrogen atom or the radical .dbd.CH or ##STR2## wherein R.sup.

Abstract: Compounds of the formula formula IA or IB ##STR1## wherein A represents an optionally substituted saturated divalent grouping which together with the two carbon atoms to which it is attached represents a fused 5-, 6- or 7-membered carbocyclic or heterocyclic ring selected from optionally substituted fused cyclopenteno, cyclohexeno, cyclohepteno, dihydrothieno, dihydrothiopyrano, tetrahydrothiepino, dihydrofuro, dihydropyrano, tetrahydrooxepino, dihydropyrrolo, tetrahydropyrido and tetrahydroazepino; R.sub.1 represents lower alkyl, phenyl, or phenyl mono- or disubstituted by lower alkyl, lower alkoxy, halogen or trifluoromethyl; or R.sub.1 represents an aromatic heterocyclic radical selected from e.g. optionally substituted pyridyl, quinolyl, isoquinolyl, pyrimidyl and thiazolyl; R.sub.2, R.sub.3, R.sub.3 ' are hydrogen or lower alkyl; and pharmaceutically acceptable salts; are useful as benzodiazepine receptor modulators for the treatment of nervous system disorders.

Abstract: Compounds of the formula formula IA or IB ##STR1## wherein A represents an optionally substituted saturated divalent grouping which together with the two carbon atoms to which it is attached represents a fused 5-, 6- or 7-membered carbocyclic or heterocyclic ring selected from optionally substituted fused cyclopenteno, cyclohexeno, cyclohepteno, dihydrothieno, dihydrothiopyrano, tetrahydrothiepino, dihydrofuro, dihydropyrano, tetrahydrooxepino, dihydropyrrolo, tetrahydropyrido and tetrahydroazepino; R.sub.1 represents lower alkyl, phenyl, or phenyl mono- or disubstituted by lower alkyl, lower alkoxy, halogen or trifluoromethyl; or R.sub.1 represents an aromatic heterocyclic radical selected from e.g. optionally substituted pyridyl, quinolyl, isoquinolyl, pyrimidyl and thiazolyl; R.sub.2, R.sub.3, R.sub.3 ' are hydrogen or lower alkyl; and pharmaceutically acceptable salts; are useful as benzodiazepine receptor modulators for the treatment of nervous system disorders.

Abstract: Novel N-(bicyclic heterocyclyl)-4-piperidinamines having antihistaminic and serotonin-antagonistic properties which are useful in the treatment of allergic diseases.

Abstract: Novel 2-amino-5-hydroxy-4-methylpyrimidines and substituted amino derivatives thereof useful as inhibitors of leukotriene synthesis for the treatment of pulmonary, inflammatory and cardiovascular diseases, cancer and psoriasis. In addition these compounds are cytoprotective and therefore useful in the treatment of peptic ulcers. A process for the preparation of such active compounds by ring rearrangement of 2-amino-5-acetyloxazole, pharmaceutical compositions containing the novel active compounds and compositions containing these compounds in combination with other anti-inflammatory agents or gastric anti-secretory agents.

Abstract: Pyrazolo[4,3-c]quinolin-3-ones of the formula ##STR1## e.g. wherein R.sub.1 is an aromatic heterocyclic radical selected from quinolyl, isoquinolyl, pyrimidyl and thiazolyl, or such said heterocyclic radical mono- or di-substituted by lower alkyl, lower alkoxy or halogen; R.sub.2 and R.sub.3, each independently, represents hydrogen or lower alkyl; R.sub.4 and R.sub.5, each independently, represents hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; and pharmaceutically acceptable salts thereof, are benzodiazepine receptor modulators.