Three Or More Ring Hetero Atoms In The Tetracyclo Ring System Patents (Class 544/247)
-
Patent number: 5510344Abstract: Compounds of formula I ##STR1## wherein X is oxygen or sulphur, W is CH or N, m is 0 or 1, and either a) n is 1 and Q is a non-aromatic heterocyclic ring of 3 to 10 ring atoms, containing one to three hetero atoms selected from oxygen, sulphur and nitrogen, which may be substituted and may be fused to another ring, with the proviso a) that if Q is thiazol-2-in-2-yl, it is substituted but not by methylene, and b) Q is not a six membered ring containing only two nitrogen atoms, or b) n is 0 or 1 and Q is ##STR2## where R.sup.1 is alkyl, alkoxy or alkylthio, and R.sup.2 is heteroaryl, non aromatic heterocyclyl, optionally substituted cycloalkyl or optionally substituted alkyl containing at least 5 carbon atoms, phenyl substituted by one or more groups selected from halogen, optionally substituted alkyl, alkoxy, haloalkoxy, aryloxy, alkylthio and alkoxycarbonyl, and when R.sup.1 is alkyl or alkoxy, or, when W is nitrogen, R.sup.2 can also be unsubstituted phenyl, have pesticidal especially fungicidal activity.Type: GrantFiled: May 4, 1994Date of Patent: April 23, 1996Assignee: Schering Agrochemicals LimitedInventors: Geoffrey R. Cliff, Ian C. Richards
-
Patent number: 5482936Abstract: Compounds and pharmaceutically acceptable salts thereof formally derived by bridging the 1- and 2-positions of 1H-imidazo[4,5-c]quinolin-4-amines. Also, methods of using such compounds and pharmaceutical formulations containing such compounds. Said compounds are useful to induce interferon biosynthesis in an animal.Type: GrantFiled: January 12, 1995Date of Patent: January 9, 1996Assignee: Minnesota Mining and Manufacturing CompanyInventor: Kyle J. Lindstrom
-
Patent number: 5441955Abstract: Methods, compounds and compositions are provided form inhibiting the growth of pathogenic mycobacteria in vitro and of treatment of pathogenic mycobacterial infections in vivo using indolo[2,1-b]quinazoline-6,12-dione compounds of the formula (I): ##STR1## wherein A, B, C, D, E, F, G and H are independently selected from carbon and nitrogen, or A and B or C and D can be taken together to be nitrogen or sulfur, and the pharmaceutically acceptable salts thereof. The methods, compounds and compositons are particularly useful for inhibiting the growth of Mycobacterium tuberculosis, and may be used alone, or in combination with other anti-Mycobacterium tuberculosis agents, such as isoniazid, rifampin, pyrazinamide, rifabutin, streptomycin and ciprofloxacin, to provide new agents for the treatment of tuberculosis, including multidrug-resistant tuberculosis (MDRTB).Type: GrantFiled: November 19, 1993Date of Patent: August 15, 1995Assignee: PathoGenesis CorporationInventors: William R. Baker, Lester A. Mitscher
-
Patent number: 5439916Abstract: 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.Type: GrantFiled: August 31, 1990Date of Patent: August 8, 1995Assignee: Schering CorporationInventors: Ashit K. Ganguly, Richard J. Friary, John H. Schwerdt, Marvin I. Siegel, Sidney R. Smith, Edmund J. Sybertz
-
Patent number: 5393755Abstract: Novel polycylic guanine derivatives of the formula: ##STR1## wherein J is oxygen or sulfur, R.sup.1 is hydrogen, alkyl or alkyl substituted with aryl or hydroxy;R.sup.2 is hydrogen, aryl, heteroaryl, cycloalkyl, alkyl or alkyl substituted with aryl, heteroaryl, hydroxy, alkoxy, amino, monoalkyl amino or dialkylamino, or --(CH.sub.2).sub.m TCOR.sup.20 wherein m is an integer from 1 to 6, T is oxygen or --NH-- and R.sup.20 is hydrogen, aryl, heteroaryl, alkyl or alkyl substituted with aryl or heteroaryl;R.sup.3 is hydrogen, halo, trifluoromethyl, alkoxy, alkylthio, alkyl, cycloalkyl, aryl, aminosulfonyl, amino, monoalkylamino, dialkylamino, hydroxyalkylamino, aminoalkylamino, carboxy, alkoxycarbonyl or aminocarbonyl or alkyl substituted with awl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino;R.sup.a, R.sup.b, R.sup.c, and R.sup.d are defined in the specification; and n is zero or one.The compounds of formulas (I) and (I') are useful as antihypertensive, muscle relaxant and bronchodilating agents.Type: GrantFiled: December 14, 1992Date of Patent: February 28, 1995Assignee: Schering CorporationInventors: Bernard R. Neustadt, Neil A. Lindo, Brian A. Mc Kittrick
-
Patent number: 5342942Abstract: Pyrazolo[5,1-b]quinazoline compounds, salts thereof, methods of production, intermediates in their production, pharmaceutical compositions containing said compounds, and methods for treating neurodegenerative disorders, tumors of neuronal origin, inflammation, allergy, and pain, and methods for screening compounds that interact with the neurotrophic receptors using said compositions are disclosed.Type: GrantFiled: March 29, 1993Date of Patent: August 30, 1994Assignee: Warner-Lambert CompanyInventors: Juan C. Jaen, Bradley W. Caprathe
-
Patent number: 5288870Abstract: The present invention relates to a process for the preparation of specifically labelled TTX of high specific activity. In the present process, TTX is oxidized by use of the Pfitzer-Moffat method or Fenton's reagent and the aldehyde obtained is hydrated. The hydrated aldehyde is reduced with alkali metal o alkaline earth metal borotritide. The radioactive TTX so obtained, quite surprisingly, has a specific activity many times greater than previously prepared radioactive TTX.Type: GrantFiled: November 18, 1991Date of Patent: February 22, 1994Assignee: Research Foundation of the State University of New YorkInventors: Chien-yuan Kao, Biqi Wu
-
Patent number: 5260298Abstract: Imidazotriazoloquinazoline compounds having the general formula ##STR1## wherein A together with the .alpha.-marked carbon atom and the .beta.-marked nitrogen atom is one of the groups ##STR2## cyano or CO.sub.2 R.sup.5, wherein R.sup.5 is H, alkyl, cycloalkyl, trifluoromethyl or alkoxymethyl; and R.sup.2, R.sup.3 and R.sup.4 independently are H, hydroxy, halogen, CN, alkyl, alkenyl, alkynyl, trifluoromethyl, alkoxy, dialkylaminoalkoxy, aralkoxy, aryloxy which may be substituted, acyclic amino group, or NR.sup.6 R.sup.7, wherein R.sup.6 and R.sup.7 independently are H or alkyl.The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, antipsychotics, antiemetics, or in improving the cognitive function of the brain of mammals, or as benzodiazepine antagonsists.Type: GrantFiled: February 20, 1992Date of Patent: November 9, 1993Assignee: Novo Nordisk A/SInventor: Holger C. Hansen
-
Patent number: 5239074Abstract: The present invention relates to a novel method of preparing diastereoisomers derived from tetrahydrofolic acid. By reacting (i) (6RS)-folinic acid or one of its salts, or (ii) 5,10-methenyl-5,6,7,8-tetrahydrofolic acid, with HCOOH at pH 2.0-2.6, a precipitate is obtained which consists of a mixture of two diastereoisomers of orthoamide structure and of the formulae ##STR1## in which R is the p-benzoyl-(L)-glutamic acid residue, in a molar ratio IV/III of about 7/3, compound III being of so-called natural configuration and compound IV being of so-called unnatural configuration. The pure compound IV is isolated from said precipitate and the pure compound III is isolated from the corresponding filtrate. The diastereoisomers of the reduced folates and their salts of natural and unnatural configuration are prepared from compounds III and respectively IV.Type: GrantFiled: November 6, 1991Date of Patent: August 24, 1993Assignee: Sapec S.A.Inventors: Fabrizio Marazza, Attilio Melera, Rene Viterbo
-
Patent number: 5214047Abstract: A tetracyclic quinazoline derivative of the formula I: ##STR1## wherein A is C.sub.2-3 -alkylene or C.sub.2-3 -alkylene which is substituted by one or two C.sub.1-4 -alkyl radicals or A is cyclohexylene; X is phenyl, naphthyl or phenyl or naphthyl which is substituted by halogen, nitro, amino, C.sub.1-4 -alkylamino, sulfonylamino, C.sub.1-4 -acylamino, hydroxyl, C.sub.1-4 -alkoxy, --O--(CH.sub.2).sub.2-4 --NR.sup.1 R.sup.2, C.sub.1-4 -alkyl or C.sub.1-4 -alkylsulfonyl, wherein R.sup.1 and R.sup.2 are each hydrogen or C.sub.1-4 -alkyl; or X is thienyl or thienyl which is substituted by chlorine, fluorine, methyl, ethyl, methoxy, ethoxy, nitro or hydroxyl; and R is hydrogen, halogen, nitro, amino, C.sub.1-4 -alkylamino, sulfonylamino, C.sub.1-4 -acylamino, hydroxyl, C.sub.1-4 -alkoxy, --O--(CH.sub.2).sub.2-4 --NR.sup.3 R.sup.4, C.sub.1-4 -alkyl or C.sub.1-4 -alkylsulfonyl, wherein R.sup.3 and R.sup.4 are each hydrogen or C.sub.1-4 -alkyl, and the pharmaceutically acceptable salts thereof.Type: GrantFiled: September 12, 1988Date of Patent: May 25, 1993Assignee: BASF AktiengesellschaftInventors: Bernd Ostersehlt, Rainer Schlecker, Beatrice Rendenbach, Gerda von Philipsborn, Albrecht Franke, deceased
-
Patent number: 5164496Abstract: Compounds of the formula ##STR1## in which R.sup.1, R.sup.2, X.sup.1, X.sup.2, Y.sup.1 and Y.sup.2 have the following meaningsR.sup.1 and R.sup.2 designate optionally substituted aryl, or an optionally substituted heterocyclic radical which contain 1 or 2 five-, six- or seven-membered rings at least one of which contains 1, 2 or 3 hetero atoms from the series comprising O, N and S which has a C.dbd.C in conjugation with the C.dbd.C bond in the five-membered ring of III,X.sup.1, X.sup.2, Y.sup.1 and Y.sup.2 designate O, S, NR.sup.5, or X.sup.1 and Y.sup.1 or X.sup.2 and Y.sup.2 in each case form parts of a fused-on heterocyclic five-membered or six-membered ring,processes for their preparation and their use as dyestuffs and pigments.Type: GrantFiled: July 26, 1991Date of Patent: November 17, 1992Assignee: Bayer AktiengesellschaftInventor: Hans Hochstetter
-
Patent number: 5100895Abstract: New imidazoquinazoline compounds having the general formula ##STR1## wherein A together with the .alpha.-marked carbon atom and the .beta.-marked nitrogen atom is one of the groups ##STR2## wherein R.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently are hydrogen, halogen C.sub.1-6 -alkyl, aryl or aralkylR.sup.1 is ##STR3## cyano or CO.sub.2 R.sup.8, wherein R.sup.8 is hydrogen, C.sub.1-6 -alkyl or C.sub.3-7 -cycloalkyl, trifluoromethyl or C.sub.1-6 -alkoxymethyl,R.sup.2 and R.sup.3 independently are hydrogen, halogen, CN, C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl, C.sub.2-6 -alkynyl, trifluoromethyl, C.sub.1-6 -alkoxy, dialkylaminoalkoxy, aralkoxy, aryloxy which may be substituted with halogen or alkoxy, a cyclic amino group, or NR.sup.9 R.sup.10, wherein R.sup.9 and R.sup.10 independently are hydrogen or C.sub.1-6 -alkyl.Type: GrantFiled: September 5, 1990Date of Patent: March 31, 1992Assignee: Novo Nordisk A/SInventors: Holger C. Hansen, Marit Kristiansen
-
Patent number: 5077403Abstract: A process for the production of a compound of the formula ##STR1## where R.sub.1 and R.sub.2 each are alkyl C.sub.1 -C.sub.16, aryl, aralkyl, alkenyl, alkynyl, cyano, carboxy and esters, carboximido, N-monosubstituted and N,N-disubstituted carboximido with alkyl, aralkyl, and aryl groups; R.sub.3 is tertiary butyldimethyl silyl, R.sub.4 is tertiarybutyldimethylsilyl, trimethylsilyl, X=O or NH comprising condensing a compound of the formula ##STR2## wherein R.sub.3 and R.sub.4 are as defined above with a compound of either the formula: ##STR3## wherein R.sub.1 and R.sub.2 are as defined above and R.sub.5 is C.sub.1 -C.sub.4 ; in the presence of a reaction-inert solvent at a temperature of from 50.degree.to about 150.degree. C. forming an intermediate and oxidizing the intermediate product, to form the desired compound of formula I. The products are antiviral.Type: GrantFiled: August 16, 1990Date of Patent: December 31, 1991Assignee: The Board of Governors for Higher Education, State of Rhode Island and Providence PlantationsInventors: Elie Abushanab, Chandra Vargeese
-
Patent number: 5070086Abstract: Imidazo- and pyrimido-quinoline, naphthyridine and pyridopyrazine compounds, methods of making said compounds and their use as anti-allergy, antiinflammatory and/or agents for the treatment of hyperproliferative skin disease are disclosed.Type: GrantFiled: June 15, 1990Date of Patent: December 3, 1991Assignee: Schering CorporationInventor: Richard Friary
-
Patent number: 5066800Abstract: A novel process and intermediates used therein for linking a cephalosporin compound to a quinolone are disclosed. According to the disclosed process, the 2-carboxylic acid moiety of the cephalosporin compound is treated with an organic base. The resulting salt is then reacted with a quinolone compound which has been activated using a haloformate. The reaction is run in a non-aqueous organic solvent. 4-Dimethylaminopyridine is used to promote the reaction between the cephalosporin salt and the activated quinolone.Type: GrantFiled: April 27, 1990Date of Patent: November 19, 1991Assignee: Hoffmann-La Roche Inc.Inventor: Masami Okabe
-
Patent number: 4968797Abstract: 4,4-diaryldihydroquinazolones of the formula ##STR1## wherein X.sup.1, X.sup.2 and X.sup.3, independently of one another, denote hydrogen, halogen, alkyl, aryl, alkanoylamino, aroylamino, heteryl, NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3, at least one of the radicalsX.sup.1, X.sup.2 or X.sup.3 standing for NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3,R.sup.1 denotes hydrogen, alkyl, cycloalkyl, aralkyl, aryl or the members of a bridge to the o-carbon of ring C,R.sup.2 denotes a radical of an acid,Y.sup.1, Y.sup.2 and Y.sup.3, independently of one another, denote hydrogen, alkyl, cycloalkyl, aralkyl aryl or heteryl or the remaining members of a 5- or 6-membered ring which reaches to one of the o-position benzene C atoms and may contain further hetero atoms orY.sup.1 +Y.sup.Type: GrantFiled: October 30, 1987Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Horst Berneth, Alfred Brack, Karlheinrich Meisel
-
Patent number: 4963677Abstract: A compound of the formula ##STR1## and pharmaceutically acceptable salts thereof, in which A is --N.dbd.N--NH--, --X--C(R.sub.2).dbd.N--, --N.dbd.C(R.sub.2)--X--, --X--C(R.sub.2)--CH(R.sub.2).dbd.N-- or --N.dbd.C(R.sub.2)--CH(R.sub.2)--X--, wherein X is sulphur, oxygen or nitrogen and R.sub.2 is provided that where two R.sub.2 -groups are present in the A group one of the R.sub.2 groups is hydrogen, amino, substituted amino, C.sub.1-6 alkyl, substituted acylamino or one of the following groups: ##STR2## wherein R.sub.a is hydrogen, amino, substituted amino, C.sub.1-6 alkoxy, heterocyclic five membered ring or --NHCOR', wherein R' is C.sub.1-6 alkyl, aryl or heterocyclic five membered ring, R.sub.b is hydrogen, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio or hydroxy, R.sub.c is hydrogen, C.sub.1-6 alkyl or oxygen and R.sub.d is C.sub.1-6 alkyl or oxygen, R.sub.e is hydrogen, hydroxy or C.sub.1-6 alkoxy, R.sub.f is C.sub.1-6 alkyl, provided that where two R.sub.2 -groups are present in the A group, one of the R.sub.Type: GrantFiled: November 8, 1988Date of Patent: October 16, 1990Assignee: Orion Corporation Ltd.Inventors: Lawrence Sellin, Reijo J. Backstrom, Kalevi E. Heinola, Erkki J. Honkanen, Tord K. W. Langenskiold, Irma O. Ojala, Aino K. Pippuri, Jarmo J. Pystynen
-
Patent number: 4831013Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is optionally substituted phenyl, pyridyl, thienyl, furyl, pyrrolyl, thiazolyl, or ribofuranosyl; X is oxygen, NR, or sulfur; R is hydrogen, lower alkyl, lower alkenyl, or lower alkynyl; and ring A is (a) an optionally substituted 5-8 membered monocycloalken-1,2-diyl; (b) an optionally substituted carbobicyclic ring of the formula ##STR2## wherein n and m are each independently one or two; or (c) an optionally substituted 5-6 membered heterocycle having one or two heteroatoms, the atoms of which are selected from carbon, oxygen, nitrogen, and sulfur. Also disclosed are tautomers of the above and pharmaceutically acceptable salts; compositions thereof; and methods of using the compounds, tautomer, or salts.Type: GrantFiled: February 27, 1987Date of Patent: May 16, 1989Assignee: Ciba-Geigy CorporationInventor: John E. Francis
-
Patent number: 4826968Abstract: The present invention relates to the novel compound N-[2-(S-Coenzyme A) acetyl] sym-norspermidine which electively inhibits the enzyme spermidine/spermine N.sup.1 acetyl transferase thereby aberrating the polyamine biosynthesis pathway. The present compound alone or in combination with other agents can be employed in pharmaceutically acceptable compositions and in convenient dosage forms for use in the treatment of neoplastic diseases, diseases caused by parasitic protozoans, diseases involving deranged cell growth or other related diseases.Type: GrantFiled: April 26, 1985Date of Patent: May 2, 1989Assignee: Research CorporationInventors: Anthony E. Pegg, Bradley G. Erwin
-
Patent number: 4786729Abstract: Benzimidazolo-quinazolines of the general formula ##STR1## in which Y denotes a radical of the formula ##STR2## Y.sub.1 denotes hydrogen or alkyl, X and X.sub.1, independently of one another, denote hydrogen, alkyl, cycloalkyl, aryl or aralkyl, orX and X.sub.1, together with the nitrogen atom connecting them, denote a 5- or 6-membered ring,X.sub.2 denotes hydrogen, halogen, alkyl, alkoxy or alkoxycarbonyl,X.sub.3 denotes hydrogen, alkyl or aryl,X.sub.4 denotes hydrogen, cyano, halogen, alkyl or alkoxy,Z denotes hydrogen, alkyl, cycloalkyl or aralkyl,D denotes an optionally hydrogenated 5- or 6-membered ring, andm and n, independently of one another, denote 0 or 1,in which a double bond is in the positions labelled with 1 and 2 when m=0 and a single bond is in these positions when m=1, andin which the rings A, B and D are the radicals X, X.sub.1, X.sub.2, X.sub.3, X.sub.Type: GrantFiled: April 3, 1987Date of Patent: November 22, 1988Assignee: Bayer AktiengesellschaftInventors: Holger Heidenreich, Gert Jabs
-
Patent number: 4760065Abstract: Trifluoromethyl substituted tetracyclic compounds including optical isomers thereof having the formula: ##STR1## wherein n is 1 or 2 and p is 0 or 1, are useful as CNS agents with tranquilizing effects.Type: GrantFiled: February 13, 1986Date of Patent: July 26, 1988Inventors: Goetz E. Hardtmann, William J. Houlihan, Rudolf K. A. Giger
-
Patent number: 4754034Abstract: 4,4-diaryldihydroquinazolones of the formula ##STR1## wherein X.sup.1, X.sup.2 and X.sup.3, independently of one another, denote hydrogen, halogen, alkyl, aryl, alkanoylamino, aroylamino, heteryl, NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3, at least one of the radicals X.sup.1, X.sup.2 or X.sup.3 standing for NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3,R.sup.1 denotes hydrogen, alkyl, cycloalkyl, aralkyl, aryl or the members of a bridge to the o-carbon of ring C,R.sup.2 denotes a radical of an acid,Y.sup.1, Y.sup.2 and Y.sup.3, independently of one another, denote hydrogen, alkyl, cycloalkyl, aralkyl aryl or heteryl or the remaining members of a 5- or 6-membered ring which reaches to one of the o-position benzene C atoms and may contain further hetero atoms orY.sup.1 +Y.sup.Type: GrantFiled: October 21, 1985Date of Patent: June 28, 1988Assignee: Bayer AktiengesellschaftInventors: Horst Berneth, Alfred Brack, Karlheinrich Meisel
-
Patent number: 4720496Abstract: Compounds of the formula ##STR1## wherein (a)R.sub.1 is hydrogen, lower alkyl, lower alkoxy or 8-halo;R.sub.2 is hydrogen, lower alkyl, lower alkoxy or a fused benzene ring; andR.sub.3 and R.sub.4, together with each other, are --N.dbd.N--NH--; or(b)R.sub.1 and R.sub.2, together with each other, are --N.dbd.N--NH--;R.sub.3 is hydrogen, lower alkyl, lower alkoxy, 2-halo, 3-halo or 4-halo; andR.sub.4 is hydrogen, lower alkyl, lower alkoxy or a fused benzene ring;and non-toxic, pharmacologically acceptable salts thereof formed with an inorganic or organic base. The compounds as well as their salts are useful as antiallergics.Type: GrantFiled: June 4, 1986Date of Patent: January 19, 1988Assignee: Boehringer Ingelheim KGInventors: Kurt Schromm, Anton Mentrup, Ernst-Otto Renth, Armin Fugner
-
Patent number: 4695633Abstract: Chromogenic 4,4-diaryl-dihydroquinazolones of the formula ##STR1## wherein X.sup.1, X.sup.2 and X.sup.3 independently of one another represent hydrogen, halogen, alkyl, aryl, alkanoylamino, aroylamino, NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3,and whereinat least one of the radicals X.sup.1, X.sup.2 or X.sup.3 represents NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3,R.sup.1 denotes hydrogen, alkyl, cycloalkyl, aralkyl, aryl or the members of a bridge to the o-carbon of ring C,R.sup.2 denotes hydrogen, alkyl, cycloalkyl, aralkyl, aryl, hetaralkyl or hetaryl,Y.sup.1, Y.sup.2 and Y.sup.3 independently of one another denote hydrogen, alkyl, cycloalkyl, aralkyl or aryl or the remaining members of a 5-membered or 6-membered ring which reaches to one of the benzene-C atoms in the o-position and optionally contains further hetero-atoms, orY.sup.1 +Y.sup.Type: GrantFiled: May 17, 1985Date of Patent: September 22, 1987Assignee: Bayer AktiengesellschaftInventors: Horst Berneth, Alfred Brack
-
Patent number: 4598148Abstract: What are disclosed are pyrimido(6,1-a)isoquinolin-4-one compounds useful as hypotensive agents, bronchodilators, and anti-allergenics, intermediates useful in their preparation, and method for making the compounds and intermediates.Type: GrantFiled: September 19, 1984Date of Patent: July 1, 1986Assignee: Hoechst AktiengesellschaftInventors: Bansi Lal, Horst Dornauer, Bani K. Bhattacharya, Alihussein N. Dohadwalla, Noel J. de Souza
-
Patent number: 4584374Abstract: 4-Thioxobenzopyrano[2,3-d]-pyrimidine derivatives of the general formulae Ia or Ib ##STR1## are described. Compounds Ia and Ib are tautomers and are valuable intermediates for the preparation of 5H-[1]-benzopyrano[2,3-d]pyrimidine derivatives having ulcer-protective action without inhibition of secretion.Type: GrantFiled: September 24, 1984Date of Patent: April 22, 1986Assignee: Warner-Lambert CompanyInventors: Gerhard Satzinger, Hubert Barth, Johannes Hartenstein, Manfred Herrmann, Edgar Fritschi, Ilse-Dore Schutt
-
Patent number: 4578380Abstract: The invention relates to 5H-[1]benzopyrano-[2,3-d]pyrimidine derivatives of the general formula I ##STR1## which may be prepared by means of a new chemical process and have a protective effect similar to that of cimetidine, but do not exhibit the undesired side effects of antisecretory agents. The invention is based on a new mucoprotective mode of action which prevents lesions of the mucous membrane epithelium to arise.Type: GrantFiled: September 24, 1984Date of Patent: March 25, 1986Assignee: Warner-Lambert CompanyInventors: Gerhard Satzinger, Hubert Barth, Johannes Hartenstein, Manfred Herrmann, Edgar Fritschi, Ilse-Dore Schutt
-
Patent number: 4543356Abstract: This invention is directed to new quinazoline derivatives of the following formula having use in the treatment of symptoms associated with allergic manifestations. ##STR1## wherein R.sub.a.sup.1 and R.sub.b.sup.1 are C.sub.2 -C.sub.7 alkoxycarbonyl or R.sub.a.sup.1 and R.sub.b.sup.1 is linked together to form a group of the formula: ##STR2## R.sup.2 and R.sup.3 are hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, amino, C.sub.1 -C.sub.6 alkoxy, phenoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylpiperazinyl, C.sub.1 -C.sub.18 alkanoylamino, di(C.sub.1 -C.sub.6)alkanoylamino, C.sub.3 -C.sub.9 alkoxalylamino, C.sub.4 -C.sub.8 cycloalkylcarbonylamino, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.6)alkanoylamino, benzamido, phenyl(C.sub.1 -C.sub.6)alkanoylamino, C.sub.1 -C.sub.6 alkylsulfonylamino or di(C.sub.1 -C.sub.6)alkylamino which may be substituted with hydroxy,A.sup.1 is a group of the formula: ##STR3## in which R.sup.4 is hydrogen C.sub.1 -C.sub.6 alkyl, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.Type: GrantFiled: January 3, 1983Date of Patent: September 24, 1985Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Ikuo Ueda, Masayuki Kato, Masanobu Nagano
-
Patent number: 4539402Abstract: The invention relates to quinazolinone derivatives and of formula (I) as defined herein and processes for the production of said derivatives. Also included in the invention are pharmaceutical compositions containing a compound of said formula (I) as active ingredient and the use of said compounds and compositions as anti-inflammatory agents.Type: GrantFiled: May 9, 1983Date of Patent: September 3, 1985Assignee: Troponwerke GmbH & Co.Inventors: Wolfgang Opitz, Haireddin Jacobi, Bernhard Pelster
-
Patent number: 4503227Abstract: The invention relates to chromogenic dihydroquinazolines of the general formula ##STR1## wherein the ring A is a monocyclic or polycyclic, unsubstituted or substituted heterocyclic radical which may contain further heteroatoms as ring members,each of X.sub.1, X.sub.2 and Y independently of one another is hydrogen, halogen, lower alkyl, lower alkanoylamino, or a group of the formula ##STR2## X.sub.3 is hydrogen, halogen, lower alkyl or lower alkoxy; each of R.sub.1, R.sub.2, R.sub.3, R.sub.4, Z.sub.1 and Z.sub.2 independently of one another is C.sub.1 -C.sub.12 alkyl which is unsubstituted or substituted by halogen, hydroxyl, cyano or lower alkoxy, or is cycloalkyl, phenyl, or phenyl or benzyl each substituted by halogen, nitro, lower alkyl or lower alkoxy, and the radicals R may also be hydrogen; oreach pair of substituents (R.sub.1 and R.sub.2), (R.sub.3 and R.sub.4) and (Z.sub.1 and Z.sub.Type: GrantFiled: April 18, 1983Date of Patent: March 5, 1985Assignee: Ciba-Geigy CorporationInventors: Heinz Balli, Sigmund Gunzenhauser, Ian J. Fletcher, Davor Bedekovic
-
Patent number: 4482556Abstract: What are disclosed are pyrimido (6,1-a)isoquinolin-4-one compounds useful as hypotensive agents, bronchodilators, and anti-allergenics, intermediates useful in their preparation, and methods for making the compounds and intermediates.Type: GrantFiled: March 26, 1980Date of Patent: November 13, 1984Assignee: Hoechst AktiengesellschaftInventors: Bansi Lal, Horst Dornauer, Bani K. Bhattacharya, Alihussein N. Dohadwalla, Noel J. de Souza
-
Patent number: 4471117Abstract: This invention relates to 3,4-dihydro-2H-pyrimido[2,1-b]benzothiazoles displaying monoamine-oxidase inhibiting activity. The compounds are useful as antidepressants and anti-Parkinson agents.Type: GrantFiled: March 10, 1980Date of Patent: September 11, 1984Assignee: Janssen Pharmaceutica N.V.Inventor: Victor Sipido
-
Patent number: 4465833Abstract: A novel ethynylation process is disclosed which provides an expanded series of novel ethylnyl-terminated aromatic compounds having base sensitive substituents and which facilitates the economic preparation of prior art ethynyl-substituted aromatic compounds.Type: GrantFiled: October 15, 1980Date of Patent: August 14, 1984Assignees: Hughes Aircraft Company, Hughes Aircraft CompanyInventors: Kreisler S. Y. Lau, Robert H. Boschan
-
Patent number: 4463007Abstract: 1,2,4-Triazolo[1,5-c]-quinazolinones of the general formula I ##STR1## and their pharmaceutically tolerated salts, processes for their preparation and pharmaceutical formulations which contain these compounds and are useful drugs in the treatment of allergic disorders.Type: GrantFiled: November 15, 1982Date of Patent: July 31, 1984Assignee: BASF AktiengesellschaftInventors: Rainer Schlecker, Ludwig Friedrich, Dieter Lenke
-
Patent number: 4429126Abstract: Quinazoline derivatives of the formulae: ##STR1## wherein A.sup.1 is ##STR2## A.sup.2 is ##STR3## R.sup.1 is hydrogen, carboxy or esterified carboxy, R.sub.a.sup.1 and R.sub.b.sup.1 are esterified carboxy,R.sup.2 and R.sup.3 are hydrogen, alkyl, halogen, nitro, amino, alkoxy, aryloxy, alkylthio, alkylpiperazinyl, acylamino or dialkylamino which may be substituted with hydroxy,R.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, alkenyloxy, dialkylamino or 2,2-dialkoxycarbonylvinylaminoR.sub.a.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, alkenyloxy or dialkylamino,R.sup.5 is alkyl or alkenyl, andR.sup.6 is carboxy or esterified carboxy.Type: GrantFiled: June 4, 1982Date of Patent: January 31, 1984Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Ikuo Ueda, Masayuki Kato, Masanobu Nagano
-
Patent number: 4409224Abstract: Pyrimido[1,6-a]indole derivatives characterized by having a substituted ethyl group at position 5 and optionally being further substituted at various positions on the pyrimido[1,6-a]indole nucleus are disclosed. The foregoing compounds are useful as antihypertensive agents in a mammal. Methods for their preparation also are disclosed.Type: GrantFiled: July 13, 1981Date of Patent: October 11, 1983Assignee: American Home Products Corp.Inventor: Ivo L. Jirkovsky
-
Patent number: 4395549Abstract: Intermediates useful in the preparation of Rutecarpine and Rutecarpine derivatives are disclosed as well as a process for the preparation of said intermediates having the following formula: ##STR1## wherein R, R.sup.1 and R.sup.2 are the same or different and stand for hydrogen, halogen, nitro, carboxy, nitrile, alkoxy containing 1 to 4 carbon atoms, alkoxycarbonyl containing 1 to 4 carbon atoms in the alkoxy group, alkyl containing 1 to 4 carbon atoms, amino or hydroxy or R and R.sup.1 together stand for methylenedioxy, R.sup.2 stands for hydrogen, R.sup.3 represents hydrogen or alkyl containing 1 to 4 carbon atoms, R.sup.Type: GrantFiled: October 2, 1981Date of Patent: July 26, 1983Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.Inventors: Istvan Hermecz, Jozsef Kokosi, Agnes Horvath, Zoltan Meszaros, Gyorgy Szasz, Tibor Breining, Lelle Vasvari nee Debreczy
-
Patent number: 4390540Abstract: Imidazoquinazolines of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are hydrogen, halogen, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy or C.sub.2-5 -alkoxyalkyl; or two of R.sup.1, R.sup.2 and R.sup.3 on adjacent carbon atoms taken together are methylenedioxy or ethylenedioxy; and R.sup.4 and R.sup.5 are hydrogen or C.sub.1-4 -alkyl,and their tautomers, as well as their physiologically compatible acid addition salts, are described.The compounds of formula I inhibit the aggregation of the blood platelets, as well as gastric acid secretion, and have activity on the circulatory system.Type: GrantFiled: August 12, 1981Date of Patent: June 28, 1983Assignee: Hoffmann-La Roche Inc.Inventors: Madhukar S. Chodnekar, Ado Kaiser, Frank Kienzle
-
Patent number: 4387226Abstract: There are prepared compound of the formulae ##STR1## Where R.sup.1 is H, lower alkyl S--, lower alkyl ##STR2## NH.sub.2 or halogen, R.sup.2 is OH, lower alkyl S--, halogen, NH.sub.2 or SHR is OH, SH, lower alkyl S--, or halogen andR.sup.3 is OH, SH, lower alkyl S--, halogen or NH.sub.2.The compounds have antiviral and immunomodulating activity.Type: GrantFiled: August 26, 1981Date of Patent: June 7, 1983Assignees: Newport Pharmaceuticals International, Inc., Sloan-Kettering Institute For Cancer ResearchInventors: John W. Hadden, Lionel N. Simon, Alfredo Giner-Sorolla
-
Patent number: 4377580Abstract: Quinazoline derivatives of the formulae: ##STR1## wherein A.sup.1 is ##STR2## A.sup.2 is ##STR3## R.sup.1 is hydrogen, carboxy or esterified carboxy, R.sub.a.sup.1 and R.sub.b.sup.1 are esterified carboxy,R.sup.2 and R.sup.3 are hydrogen, alkyl, halogen, nitro, amino, alkoxy, aryloxy, alkylthio, alkylpiperazinyl, acylamino or dialkylamino which may be substituted with hydroxy,R.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, alkenyloxy, dialkylamino or 2,2-dialkoxycarbonylvinylaminoR.sub.a.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, alkenyloxy or dialkylamino,R.sup.5 is alkyl or alkenyl, andR.sup.6 is carboxy or esterified carboxy.Type: GrantFiled: November 25, 1980Date of Patent: March 22, 1983Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Ikuo Ueda, Masayuki Kato, Masanobu Nagano
-
Patent number: 4372956Abstract: A 5,10-dihydroimidazo[2,1-b]quinazoline in which at least one ring carbon atom, other than the carbon atom in the 2-position, bears a substituent, or a pharmaceutically acceptable acid addition salt thereof is a useful cardiotonic agent and vasodilator in heart insufficiency and a blood platelet aggregation inhibitor.Type: GrantFiled: November 18, 1980Date of Patent: February 8, 1983Assignee: Sandoz Ltd.Inventor: Hans Ott
-
Patent number: 4367230Abstract: A triazafluoranthene compound of the formula: ##STR1## wherein R.sup.1 is hydrogen, phenyl, cycloalkyl having 3 to 6 carbon atom, (lower alkoxy)carbonyl, lower alkoxy or (lower alkyl)carbonyl, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is hydrogen, phenyl, (lower alkoxy)carbonyl, lower alkoxy, di(lower alkyl)amino, (tetrahydropyran-2-yl)oxy, hydroxy or carboxyl, A is single bond, alkylene having one to 5 carbon atoms or alkenylene having 2 to 5 carbon atoms, and B is single bond or alkylene having one to 5 carbon atoms. Methods of preparing the compound (I) are disclosed. The compound (I) and a pharmaceutically acceptable acid addition salt thereof have a potent anti-anoxic activity.Type: GrantFiled: December 10, 1980Date of Patent: January 4, 1983Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Yasuhiko Sato, Tomishige Mizoguchi, Yukitsuka Kudo, Ryuichi Ishida
-
Patent number: 4358451Abstract: Pyrimido- and imidazo-pyridoindole derivatives, in the form of racemates or optically active isomers, of formula: ##STR1## in which n=0 or 1, R.sub.1 =H, Hal, alkyl or alkoxy or CF.sub.3, R.sub.2 =H, alkyl, cycloalkyl-alkyl, cycloalkyl, N,N-dialkylaminoalkyl or phenyl, R.sub.3 =H or alkyl and R.sub.4 =H, alkyl or benzyl are useful as anti-anoxia or psychotropic agents in therapy. They are prepared by cyclizing a compound of formula: ##STR2## wherein R.sub.5 is alkyl, by heating it in an acidic medium, such as ethanolic hydrogen chloride.Type: GrantFiled: January 15, 1980Date of Patent: November 9, 1982Assignee: SynthelaboInventors: Gabor I. Koletar, Jonathan R. Frost, Regis DuPont, Patrick Lardenois, Claude Morel, Henry Najer
-
Patent number: 4323572Abstract: Tricyclic isoindole derivatives characterized by having a 1,2,3,4,6,10b-hexahydropyrazino[2,1-a]isoindole or 1,3,4,10b-tetrahydropyrimido[6,1-a]isoindol-6(2H)-one nucleus are disclosed. The foregoing compounds are useful antihypertensive agents.Type: GrantFiled: February 6, 1981Date of Patent: April 6, 1982Assignee: American Home Products CorporationInventors: Christopher A. Demerson, Leslie G. Humber, Jean-Marie Ferland
-
Patent number: 4307234Abstract: Pyrimido[1,6-a]indole derivatives characterized by having a substituted ethyl group at position 5 and optionally being further substituted at various positions on the pyrimido[1,6-a]indole nucleus are disclosed. The foregoing compounds are useful as antihypertensive agents in a mammal. Methods for their preparation also are disclosed.Type: GrantFiled: September 11, 1978Date of Patent: December 22, 1981Assignee: American Home Products Corp.Inventor: Ivo L. Jirkovsky
-
Patent number: 4302585Abstract: 3-Hydroxy-3-substituted phenylthiazolo[2,3-b]quinazoline-2-acetic acids, their lactones and related compounds, and their use as immunomodulating agents are disclosed.Type: GrantFiled: December 22, 1980Date of Patent: November 24, 1981Assignee: American Home Products CorporationInventors: Peter H. L. Wei, Stanley C. Bell
-
Patent number: 4288383Abstract: Propenimidates are provided having the formula: ##STR1## wherein X and Y are independently O or S; andR.sup.1 and R.sup.2 are independently C.sub.1 -C.sub.4 alkyl, (CH.sub.2).sub.n OR.sup.3 where R.sup.3 is C.sub.1 -C.sub.4 alkyl and n is 1 or 2, CH.sub.2 CH.sub.2 Cl, or CH.sub.2 CF.sub.3, provided that when R or R.sup.2 is CH.sub.2 CH.sub.2 Cl or CH.sub.2 CF.sub.3, then the respective X or Y is O.Preferred propenimidates have X and Y as O and R.sup.1 and R.sup.2 as methyl or ethyl.The propenimidates are made by preparing a monohydrohalide salt from a dihydrohalide salt of the formula: ##STR2## and then contacting the monohydrohalide salt with cyanamide. The propenimidates upon heating ring close to pyrimidines which are useful in preparing herbicidal compounds.Type: GrantFiled: April 24, 1980Date of Patent: September 8, 1981Assignee: E. I. Du Pont de Nemours and CompanyInventor: Julius J. Fuchs
-
Patent number: 4284773Abstract: A 1,2,3,5-tetrahydroimidazothienopyrimidin-2-one represented by the formula: ##STR1## wherein one of Z.sub.1, Z.sub.2 and Z.sub.3 is a sulfur atom and the remaining two of Z.sub.1, Z.sub.2 and Z.sub.3 represent CH, R.sub.1 and R.sub.2 each represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, a phenyl group, a chlorine atom or, when taken together R.sub.1 and R.sub.2 represent an alkylene chain of 3 to 5 carbon atoms, and R.sub.3 represents a hydrogen atom or an alkyl group having 1 to 5 carbon atoms, and a pharmaceutically acceptable acid addition salt thereof, which exhibit an excellent blood platelet anti-aggregatory activity and are useful as anti-thrombotic agents.Type: GrantFiled: August 13, 1979Date of Patent: August 18, 1981Assignee: Daiichi Seiyaku Co., Ltd.Inventors: Fumiyoshi Ishikawa, Shinichiro Ashida
-
Patent number: 4277476Abstract: Derivatives of fluorenes and fluoranthenes, in the form of racemates or of enantiomers, of the formula (I) ##STR1## in which n is 1 or 2, R.sub.1 is a hydrogen or halogen atom or an alkyl or alkoxy radical, R.sub.2 is a hydrogen atom or an alkyl, cycloalkyl, cycloalkylalkyl, benzyl, halogenobenzyl, alkylbenzyl, alkoxybenzyl, acyl, alkoxycarbonyl or alkylaminocarbonyl radical, R.sub.3 is a hydrogen atom or an alkyl radical, R.sub.4 is a hydrogen atom or an alkyl, acyl or aroyl radical, the alkyl and alkoxy radicals or parts of radicals having from 1 to 4 carbon atoms and pharmaceutically acceptable acid addition salts thereof, are therapeutically valuable as anti-anoxia and psychotropic agents.Type: GrantFiled: July 26, 1979Date of Patent: July 7, 1981Assignee: SynthelaboInventors: Regis DuPont, Patrick Lardenois, Claude Morel, Jonathan Frost, Gabor I. Koletar
-
Patent number: 4269836Abstract: New 4H-pyrazolo[4',3':5,6]pyrido[3,4-e][1,2,4]triazolo[1,5-a]pyrimidin-5(8H)on e and new derivatives thereof have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.Type: GrantFiled: July 13, 1976Date of Patent: May 26, 1981Assignee: E. R. Squibb & Sons, Inc.Inventors: Theodor Denzel, Hans Hoehn