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| Number | Title | Issue Date |
| 5620978 | 8-aza, 6-aza and 6,8-diaza-1,4-dihydroquinoxaline-2,3-diones and the use thereof as antagonists for the glycine/NMDA receptor Disclosed is a method of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma or hypoglycemia. The method comprises administering to an animal a compound of the formula: ##STR1## or a pharmaceutically acceptable salt ther... | 04/15/1997 |
| 5599812 | Tricyclic pyrrolopyrazine 5-HT3 -active compounds The present invention relates to a compound selected from these of formula (I): ##STR1## in which A and R1 are as defined in the description, and medicinal product containing the same which is useful for treating a disorder linked to ... | 02/04/1997 |
| 5580870 | Quinazoline derivatives The invention concerns quinazoline derivatives of the formula I ##STR1## wherein m is 1, 2 or 3 and each R1 includes hydroxy, amino, ureido, hydroxyamino, trifluoromethoxy, (1-4C)alkyl, (1-4C)alkoxy and (1-3C)alkylenedioxy; and Q is a 9- o... | 12/03/1996 |
| 5561133 | Thymidylate synthase inhibiting quinazolinones Quinazolines of the formula ##STR1## wherein R1 is typically methyl, hydrogen or amino; R2 is typically methyl or propargyl; Ar is typically phenylene or 2'-fluorophenylene; R3 is the residue of a dipeptide substitute... | 10/01/1996 |
| 5556860 | Quinazolinone derivatives possessing calcium uptake inhibiting activity This invention is to provide quinazolinone derivatives, and their acid salts and quaternary ammonium salts, having an effect of preventing or treating diseases caused by calcium ion overload in cells, such as ischemic heart disease, ischemic cerebral dise... | 09/17/1996 |
| 5556841 | Thiazine or thiomorpholine derivatives This invention relates to the compounds of the formula [I] which are useful for the treatment of cataracts, and the synthetic intermediates of the formula [II], ##STR1## wherein R1 is hydroxy which can be protected by a hydroxy protective ... | 09/17/1996 |
| 5552409 | Dihydropyridazinones, pyridazinones and related compounds as fungicides This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula ##STR1## wherein A, Q, D and R1 are as defined within, compositions containing these compounds and methods of controlling agric... | 09/03/1996 |
| 5550240 | Piperazinyl-bis(alkylamino)pyrimidine derivatives and process for preparing same An intermediate compound is disclosed that is useful in the preparation of a lipid-peroxidation inhibiting substance and that is selected from the group consisting of: 2,4-bis[1-adamantylamino]-6-(1-piperazinyl)pyrimidine; and 4,6-bis(1-adamantylamino)-2-(1-pi... | 08/27/1996 |
| 5550239 | Process for large-scale production of indolyl alkyl pyrimidinyl piperazine compounds An improved, novel convergent process suitable for large scale preparation of the antimigraine agent 4-(5-methoxy-4-pyrimidinyl)-1-[3-[5-[[(methylamino)sulfonyl]methyl]-1H-ind ol-3-yl]propyl]piperazine (BMS 180048) and close analogs. The improved proc... | 08/27/1996 |
| 5547953 | Substituted 1-oxo-1,2-dihydroisoquinolinoylguanidines and 1,1-dioxo-2H-1,2-benzothiazinoylguanidines, a process for their preparation, their use as medicaments or diagnostic agents, and medicaments containing them Substituted 1-oxo-1,2-dihydroisoquinolinoylguanidines and 1,1-dioxo-2H-1,2-benzothiazinoylguanidines, a process for their preparation, their use as medicament or diagnostic agent, and also a medicament containing them. Acylguanidines I ##STR1## ... | 08/20/1996 |
| 5545738 | Alfuzosin hydrochloride dihydrate Alfuzosin hydrochloride is stabilized as alfuzosin hydrochloride dihydrate, which is useful for the production of antihypertensive agents or dysuria curing agents.... | 08/13/1996 |
| 5543517 | Substituted bicyclic phosphoramides and derivatives thereof This invention relates to substituted bicyclic phosphoramides and derivatives thereof, useful as retroviral protease inhibitors and as standards and reagents in determining the ability of a potential pharmaceutical to inhibit viral replication or HIV prot... | 08/06/1996 |
| 5543516 | Process for preparation of benzoxazine compounds in solventless systems A method for preparing a desired benzoxazine compound comprises preparing a substantially homogeneous reaction mixture that includes a phenolic compound; a primary amine; and an aldehyde, but no solvent other than for the solvency which the reactants may ... | 08/06/1996 |
| 5541218 | Indolinyl N-hydroxyurea and N-hydroxamic acid derivatives as lipoxygenase inhibitors Certain indoline derivatives of the formula I: ##STR1## wherein the variables Y, A, R1, R4 and n have the definitions set forth in the disclosure, have the ability to inhibit the 5-lipoxygenase enzyme. These compounds are useful... | 07/30/1996 |
| 5538950 | Endothelin antagonists and their preparation A compound of the formula: ##STR1## in which R3 is hydrogen or lower alkyl, R4 is pyridyl (lower) alkyl; and R1, R2, R5 and A are defined in the description; or a pharmaceutically acceptable salt ther... | 07/23/1996 |
| 5538968 | Geneserine derivatives processes as cholinesterase inhibitors Geneserine homologs of formula I ##STR1## in which R is a straight or branched C2 -C20 alkyl group, a C3 -C7 cycloalkyl group, an unsubstituted phenyl or benzyl group, or a phenyl or benzyl group substitute... | 07/23/1996 |
| 5539113 | Pyrrolopyrimidine derivatives, their production A process of making a compound of the formula ##STR1## wherein the ring A is a pyrrole or pyrroline ring, X is an amino group or a hydroxyl group, Y is a hydrogen atom, an amino group or a hydroxyl group, R is a hydrogen atom, a fluorine atom, an alk... | 07/23/1996 |
| 5539114 | Process for the preparation of substituted quinazoline-2,4,-diones A process for the preparation of quinazoline-2,4-diones of the formula (I) ##STR1## in which R1 is aryl and R2, R3, R4, and R5 independently of one another are halogen, alkyl, alkoxy or hydrogen, by ... | 07/23/1996 |
| 5538966 | Carbonic anhydrase inhibitors Compounds of the following formula are disclosed: Compounds of Formula I are the topic of this invention: ##STR1## Wherein G, J and the two atoms of the thiophene ring to which they are attached form a six-membered ring chosen from ##STR2## The ... | 07/23/1996 |
| 5536836 | Process for the preparation of 2-(4-[4-(4-chloro-1-pyrazolyl)butyl]-1-piperazinyl)pyrimidine (Lesopitron) The present invention relates to a process for the preparation of 2-{4-[4-(4-chloro-1-pyrazolyl)buty1]-1-piperazinyl}pyrimidine (Lesopitron) of formula I: ##STR1## characterized in that the reaction between 2-(1-piperazinyl)pyrimidine, 4-chlorop... | 07/16/1996 |
| 5534518 | Insecticidal substituted-2,4-diaminoquinazolines An insecticidal composition comprising, in admixture with an agriculturally acceptable carrier, an insecticidally effective amount of a 2,4-diaminoquinazoline compound of the formula: ##STR1## wherein R1, R2, R6, R | 07/09/1996 |
| 5532236 | [1,2,4]triazolo[4,3-a]quinoxaline compounds The present invention relates to [1,2,4]triazolo[4,3-a quinoxaline derivatives of formula I ##STR1## wherein one of R1 and R2 is a 5- or 6-membered nitrogen-containing heterocyclic ring which is optionally substituted with ... | 07/02/1996 |
| 5532208 | Pyrimidone derivatives and their use There are disclosed novel pyrimidone derivatives of the formula I: ##STR1## wherein X is hydrogen, chlorine, methyl or ethyl, R2 is hydrogen or methyl, and Q is ##STR2## A is fluorine, chlorine or bromine; and R1 is alkyl, ... | 07/02/1996 |
| 5523411 | Synthesis of mitomycin and its analogs The present invention relates to the synthesis of mitomycin and analogs thereof that are useful as anticancer antibiotics. The invention further relates to analogs of mitomycin, which can be prepared according to the methods of synthesis provided. The syn... | 06/04/1996 |
| 5521181 | Bicyclic substituted hexahydrobenz[e]isoindole -1 adrenergic antagonists The present invention relates to a compound of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein W is a bicyclic heterocyclic ring system. The compounds are -1 adrenergic antagonists and are useful in the treatment... | 05/28/1996 |
| 5519016 | Aryl group- or aromatic heterocyclic group-substituted aminoquinolone derivatives and anti-HIV agent Disclosed are an aryl group- or heterocyclic group-substituted aminoquinolone compound represented by the formula (Ia), (Ib) or (Ic): ##STR1## wherein each of the substitutents are defined in the specification, or a salt of the compound, and an AIDS ... | 05/21/1996 |
| 5516776 | Enantioselective synthesis of antifolates A process and intermediates for the enantioselective synthesis of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid are disclosed.... | 05/14/1996 |
| 5514688 | Carbocyclic adenosine analogs useful as immunosuppressants This invention relates to carbocyclic adenosine compounds of the formula (1) ##STR1## wherein the hydroxy substituent on the cyclopentanyl ring is in the CIS configuration relative to the bicyclic substituent, Y3, Y7, Y8 | 05/07/1996 |
| 5504412 | Replaceable battery pack of rechargeable batteries The present invention is directed to a releasable battery pack containing rechargeable batteries. In particular, the present invention facilitates the easy collection and proper disposal of useless rechargeable batteries without discarding the electrical ... | 04/02/1996 |
| 5482934 | Pregna-1,4-diene3,20-dione-16-17-acetal-21 esters, process for their preparation, composition, and methods for the treatment of inflammatory conditions The present invention relates to compounds of the formula: ##STR1## in which X1 and X2 correspond to H or F without distinction; R1 represents the following radicals: ##STR2## and R2 represents the rad... | 01/09/1996 |
| 5476851 | Pyrazolo[3,4-g]quinoxaline compounds which inhibit PDGF receptor protein tyrosine kinase This invention relates to pyrazolo[3,4-g]quinoxaline compounds exhibiting protein tyrosine kinase inhibition activity of the formula: ##STR1## where: ------ may be a double bond; R, R2, R3 and R4 are as described in claim ... | 12/19/1995 |
| 5474994 | Bicyclic heterocyclic derivatives having 1 -adrenergic and 5HT1A This invention provides bicyclic heterocyclic derivatives and their pharmaceutically acceptable salts useful for the treatment of hypertension, urethral and lower urinary tract contractions, and other disorders. The compounds are also useful for binding &... | 12/12/1995 |
| 5475001 | Quinazoline derivatives The invention concerns quinazoline derivatives of the formula I ##STR1## wherein R1 includes hydroxy, amino, hydroxyamino, (1-4C)alkoxy, (1-4C)alkylamino and di-[(1-4C)alkyl]amino; R3 is halogeno; n is 1, 2 or 3 and R2 inc... | 12/12/1995 |
| 5473067 | Preparation of carbonic anhydrase inhibitors A process for synthesizing carbonic anhydrase inhibitors is disclosed.... | 12/05/1995 |
| 5473072 | Process for the preparation of high purity buspiron and the hydrochloride thereof Process for the preparation of 8 -[4 -[4-(pyrimidine-2-yl)-piperazine-1-yl]-butyl]-8-aza-spiro[4.5]decane-7,9-d ione (buspiron) of the Formula I ##STR1## and the hydrochlorides thereof having high purity by continuously adding a solution of 8-[4-... | 12/05/1995 |
| 5470853 | 6-substituted-hexahydrobenz [CD] indoles The present invention provides 4-amino-6-substituted-hexahydrobenz[cd]indoles which are useful in treating disease states which can be benefited by an alteration of 5-HT1.sbsb.A receptors.... | 11/28/1995 |
| 5470857 | Carbocyclic nucleoside analogs useful as immunosuppressants This invention relates to a method of effecting immunosuppression in a patient in need thereof comprising administering an effective amount of a compound of the formula (1) ##STR1## wherein the hydroxy substituent on the cyclopentenyl ring is in the ... | 11/28/1995 |
| 5466687 | Arylidene-1-azacycloalkanes and arylalkyl-1-azacyclo-alkanes, their salts, medicaments containing these compounds and their use, and processes for their preparation The invention relates to arylidene-1-azacycloalkanes and arylalkyl-1-azacycloalkanes of the general formula ##STR1## (wherein n, m, p, A, W1, W2, X, Y, and R1 to R11 are as defined in claim 1) and the isome... | 11/14/1995 |
| 5463047 | Intermediates for the manufacture of 4-acyloxy-3-hydroxyethylazetidinones The invention relates to the 3-(1'-hydroxyethyl)-2-azetidinone of formula ##STR1## which can be transformed into 4-acyloxy-3-(1-hydroxyethyl)-2-azetidinone derivatives. The latter can be used as starting materials for the manufacture of a large numbe... | 10/31/1995 |
| 5462913 | Substituted 1-H-3-aryl-pyrrolidine-2,4-dione derivatives The invention relates to new 1-H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A and B together with the carbon atom to which they are bonded represent a substituted cycle, X represents alkyl, halogen or alkoxy, Y repr... | 10/31/1995 |
