Ring Nitrogen Is Shared By Two Of The Cyclos Patents (Class 544/252)
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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
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Patent number: 5055479Abstract: Compounds of formula (I): ##STR1## and pharmaceutically acceptable salts thereof are valuable in the treatment of cachexia.Type: GrantFiled: June 14, 1989Date of Patent: October 8, 1991Assignee: Sankyo Company, LimitedInventors: Yo Takiguchi, Jun Ohsumi, Yasuo Shimoji, Kazuhiko Sasagawa
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Patent number: 4994571Abstract: This invention relates to a process for producing a compound of the formula (I) as shown below. ##STR1## wherein Q is a condensed heterocyclic group having a nitrogen atom in the bridgehead position which may optionally be substituted, R.sub.1 and R.sub.2 each are an alkyl group, an alkoxy group or halogen and Z is CH or N, or a salt thereof.The compound (I) or a salt thereof is novel and of value as agricultural chemicals.According to the process of this invention the compound (I) or a salt thereof can be produced in good yield and high purity.Type: GrantFiled: August 26, 1988Date of Patent: February 19, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideki Miki, Yasuo Ishida
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Patent number: 4994462Abstract: This invention relates to certain N,N'-bis(nipecotyl)piperazines and their use as platelet aggregation inhibtory agents.Type: GrantFiled: October 5, 1988Date of Patent: February 19, 1991Assignee: Research CorporationInventors: Andrew Lasslo, Ronald P. Quintana, Marion Dugdale, Randy W. Johnson
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Patent number: 4880923Abstract: There are disclosed macrocyclic and polycyclic polyamine lubricating oil additives formed by cyclodehydration of reaction products of hydrocarbon substituted succinic anhydrides or carboxylic acids with poly 3-amino propyl compounds or by acylation of macrocyclic polyamines and polycyclic polyamines with hydrocarbon substituted succinic anhydride or carboxylic acids. These compounds are useful as dispersants and dispersants-V.I. improvers in both gasoline and diesel engine lubricating oil compositions and are also useful fuel additives.Type: GrantFiled: September 2, 1986Date of Patent: November 14, 1989Assignee: Exxon Research & Engineering CompanyInventors: Stanley J. Brois, Antonio Gutierrez
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Patent number: 4847378Abstract: Chromogenic polycyclic azamethines of formula ##STR1## wherein T.sub.1 and T.sub.2 are each independently of the other lower alkyl, cycloalkyl, benzyl, or, when taken together, are alkylene,Q is --CH or, preferably, N,W is alkylene, alkenylene, 1,2-cycloalkylene or 1,2-arylene,R is hydrogen, lower alkyl, aryl or aralkyl, andY is alkyl or alkenyl, each unsubstituted or substituted by halogen, hydroxyl, cyano or lower alkoxy, or is aralkyl, and the ring A is unsubstituted or substituted by halogen, cyano, hydroxy, lower alkyl, lower alkoxy, lower alkylcarbonyl, lower alkylcarbonyloxy, lower alkylamino, di-lower alkylamino or lower alkylcarbonylamino, and the ring B is unsubstituted or substituted by halogen, cyano, C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 alkoxy, C.sub.2 -C.sub.12 alkoxyalkoxy or aralkoxy or a glycol ether group.Type: GrantFiled: May 2, 1988Date of Patent: July 11, 1989Assignee: Ciba-Geigy CorporationInventor: Rudolf Zink
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Patent number: 4845214Abstract: Isoindoline pigments are conditioned by means of a heat treatment of the pigment in a mixture of water and benzenemonocarboxylic and/or benzenedicarboxylic acids.Well crystallized, very weatherfast pigmentary forms which give colorations possessing improved purity of shade are obtained.Type: GrantFiled: July 7, 1986Date of Patent: July 4, 1989Assignee: BASF AktiengesellschaftInventors: Wolfgang Lotsch, Reinhard Kemper
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Patent number: 4838925Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.Type: GrantFiled: September 25, 1987Date of Patent: June 13, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Chi-Ping Tseng
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Patent number: 4824846Abstract: Compounds I ##STR1## where A equals CH or N; Ar equals naphthyl, thienyl or phenyl; R.sup.1 equals alkyl, F or Cl; g equals zero, 1 or 2; and Y equals various heterocyclic bases, and the acid-addition salts thereof, are described.Several preparation processes are described.The compounds IIIa ##STR2## where R.sup.1, g and Y are as specified in the case of the formula I, serve as intermediates for the preparation of these compounds. Processes are also specified for the preparation of IIIa.I represent valuable antimycotics.Type: GrantFiled: March 19, 1987Date of Patent: April 25, 1989Assignee: Hoechst AktiengesellschaftInventors: Klaus D. Kampe, Wolfgang Raether, Walter Dittmar, Heinz Hanel
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Patent number: 4784996Abstract: Compounds of formula ##STR1## wherein A represents a lower alkylene chain optionally containing one double or triple bond, RO represents (lower)alkoxy, aryl(lower)alkoxy, hydroxy or protected hydroxy, R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, hydroxyl, lower alkyl, lower alkoxy, halo(lower)alkyl, halogen, amino or mono- or di(lower)alkylamino and R.sup.3 and R.sup.4 each independently represent hydrogen or lower alkyl and their pharmaceutically acceptable acid addition salts are useful as hypoglycaemics or as intermediates for hypoglycaemics.Type: GrantFiled: March 9, 1987Date of Patent: November 15, 1988Assignee: John Wyeth & Brother Ltd.Inventors: Alan C. White, Ian A. Cliffe, Richard S. Todd
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Patent number: 4783455Abstract: Compounds of formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R represents lower alkyl or a mono- or bicyclic aryl or heteroaryl radical, R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, hydroxyl, lower alkyl, lower alkoxy, halo(lower)alkyl, halogen, amino or mono- or di(lower)alkylamino, X represents--CH.sub.2 CR.sup.3 R.sup.4 CH.sub.2 --or --(CH.sub.2).sub.4 --where R.sup.3 and R.sup.4 each independently represent hydrogen or lower alkyl or R.sup.3 and R.sup.4 together with the carbon atom to which they are attached represent a 5, 6 or 7 membered carbocyclic ring and R.sup.5 represents acyl and R.sup.6 represents hydrogen or R.sup.5 and R.sup.6 each independently represent hydrogen or lower alkyl, are useful as hypoglycaemics.Type: GrantFiled: May 22, 1987Date of Patent: November 8, 1988Assignee: John Wyeth and Brother Ltd.Inventor: Ian A. Cliffe
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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
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Patent number: 4678499Abstract: Benzenesulfonamide compounds such as N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl-4 -oxo-1-phenyl-indeno[1,2-C]-pyrazole-5-sulfonamide and N-[(4-methoxy-6-methyl-pyrimidin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl- 4-oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide, agricultural compositions containing them, and their herbicidal utility are disclosed.Type: GrantFiled: January 30, 1986Date of Patent: July 7, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventors: Robert J. Pasteris, Ramaurthi Muthukrishnan
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Patent number: 4673676Abstract: Pyrimidoisoquinoline/compounds of the formula: ##STR1## where R.sup.1 is H, halogen or lower alkyl, R.sup.2 is NH.sub.2, NO.sub.2 or acylamino and R.sup.3 is carboxy or protected carboxy, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof are disclosed in this application. Also disclosed is a method of treating allergies by administering the compounds of this invention.Type: GrantFiled: November 9, 1984Date of Patent: June 16, 1987Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Ikuo Ueda, Youichi Shiokawa, Takashi Manabe
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Patent number: 4661592Abstract: This invention relates to a class of novel 4H-pyrimido[2,1-a]isoquinoline derivatives. The invention further relates to pharmaceutical compositions containing such 4H-pyrimido[2,1-a]isoquinoline-4-one derivatives and to the use of such compounds and compositions as anorectic agents. In particular, the novel 4H-pyrimido[2,1-a]isoquinoline-4-one derivatives are effective anorectic agents when administered orally.Type: GrantFiled: June 27, 1984Date of Patent: April 28, 1987Assignee: G. D. Searle & Co.Inventors: Arthur L. Campbell, Suzanne Evans Radak, Melanie J. Loots
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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
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Patent number: 4590197Abstract: 9,10-substituted-2-mesitylimino-3-alkyl-3,4,6,7-tetrahydro-2H-pyrimido-(6,1 -a)isoquinoline-4-ones and salts thereof having hypotensive and vasodilating properties.Type: GrantFiled: May 7, 1984Date of Patent: May 20, 1986Assignee: Hoechst AktiengesellschaftInventors: Bansi Lal, Alihussein N. Dohadwalla, Vijay A. Aroskar, Nandkumar K. Dadkar, Horst Dornauer, Julius Mascarenhas, Noel J. deSouza
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Patent number: 4588526Abstract: The invention relates to new azepino[1,2-a]pyrimidine derivatives--of the general formula ##STR1## wherein p=1, 2 and acid addition salts thereof which can be prepared by(a) reacting a compound of the formula ##STR2## with a compound of the general formula ##STR3## wherein p is as defined above and R.sup.7 is alkoxycarbonyl containing 2 to 5 carbon atoms or carboxamido or(b) reacting a compound of the general formula ##STR4## wherein R.sup.8 is alkyl containing 1 to 4 carbon atoms with a compound of the general formula ##STR5## wherein R.sup.7 is as defined above and if desired converting a compound of the general formula I to acid addition salt thereof or setting it free from the salt thereof.The new compounds show bronchodilatory activity.Type: GrantFiled: November 10, 1983Date of Patent: May 13, 1986Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara RtInventors: Istvan Hermecz, Lelle Vasvari nee Debreczy, Agnes Horvath, Jozsef Kokosi, Sandor Virag, Tibor Breining
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Patent number: 4581172Abstract: Pyrimidone derivatives of the formula ##STR1## wherein n is the integer 1 or 0; A.sup.1 and A.sup.2 are independently methylene or mono-lower alkyl or di-lower alkyl methylene; X is methylene, mono-lower alkyl or di-lower alkyl methylene, nitrogen or lower alkyl nitrogen; R is hydrogen or lower alkyl; and Y and Z taken together are the group .dbd.NR.sup.5, or R and Z taken together form a N--C--bond and Y is a group --N(H)R.sup.5 ; R.sup.1, R.sup.2 and R.sup.3 are hydrogen, lower alkyl or lower alkoxy, or R.sup.1 and R.sup.2 or R.sup.2 and R.sup.3 taken together are methylenedioxy or ethylenedioxy; R.sup.4 is hydrogen or lower-alkyl; R.sup.5 is phenyl or phenyl substituted by one or more of R.sup.6, R.sup.7 and R.sup.8 which, independently, are chlorine, fluorine, bromine, lower-alkyl or lower-alkoxy; and provided that at least one of the methylene groups A.sup.1 and A.sup.2 is mono-lower alkyl or di-lower alkyl methylene, when R.sup.Type: GrantFiled: April 25, 1984Date of Patent: April 8, 1986Assignee: Hoffmann-La Roche Inc.Inventors: Ado Kaiser, Frank Kienzle
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Patent number: 4579847Abstract: Amino derivatives of benzylidene-Pyrrolo[2,1-b] Quinazolines are provided, together with pharmaceutical compositions containing them. The compounds and the compositions have pharmaceutical utility and are particularly useful as anti allergy agents.Type: GrantFiled: December 14, 1984Date of Patent: April 1, 1986Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Gianfederico Doria, Carlo Passarotti, Maria L. Corno
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Patent number: 4551460Abstract: Pyrido[2,1-b]quinazoline derivatives of the formulas ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as hereinafter set forth, are described. The compounds of formulas I and II are useful as agents for the treatment of allergic conditions as well as for the treatment of vascular disorders involving thrombosis.Type: GrantFiled: March 2, 1983Date of Patent: November 5, 1985Assignee: Hoffmann-La Roche Inc.Inventor: Jefferson W. Tilley
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Patent number: 4548938Abstract: Novel 5H-thiazolo- and 5H-1,3,4-thiadiazolo[3,2-a]pyrimidin-5-one and 3,4-dihydro-2H,6H-pyrimido[2,1-b] [1,3]-thiazin-6-one derivatives, which compounds are useful psychotropic agents.Type: GrantFiled: February 19, 1985Date of Patent: October 22, 1985Assignee: Janssen Pharmaceutica N.V.Inventors: Ludo E. J. Kennis, Josephus C. Mertens
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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
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Patent number: 4521419Abstract: Compounds of the formula (1) ##STR1## wherein n is 1 or 2;R.sub.1 represents a hydrogen or a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a --CN group, a --CONH.sub.2 group or a --COOR.sub.8 group, wherein R.sub.8 represents hydrogen or a C.sub.1 -C.sub.6 alkyl group, unsubstituted or substituted by di(C.sub.1 -C.sub.4) - alkylamino;each of R.sub.2, R.sub.3 and R.sub.4 independently represents a hydrogen or a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group or a C.sub.3 -C.sub.4 alkenyloxy group;A completes a bond, thereby providing a double bond or, when R.sub.1 is --COOR.sub.8 wherein R.sub.8 is as defined above, A may represent also a --CH.sub.2 -- group, thereby providing a cyclopropane ring fused to the pyrido ring;R is (a) furyl, thienyl or pyridyl; or(b) a group of formula ##STR2## wherein each of R.sub.5, R.sub.6 and R.sub.7 represents, independently, a hydrogen or a halogen atom, hydroxy, formyloxy, C.sub.2 -C.sub.8 alkanoyloxy, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.Type: GrantFiled: April 27, 1983Date of Patent: June 4, 1985Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Gianfederico Doria, Carlo Passarotti, Pier P. Lovisolo, Ada Buttinoni
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Patent number: 4508899Abstract: Pigments that can be used to color plastics, paints, and printing inks have the structural formula ##STR1## wherein each R.sup.1, each R.sup.3, and R.sup.7 represent hydrogen, halogen, nitro, or lower alkyl and each R.sup.2, each R.sup.4, each R.sup.5, and R.sup.6 represent hydrogen or halogen.Type: GrantFiled: October 14, 1983Date of Patent: April 2, 1985Assignee: Sun Chemical CorporationInventor: Terence R. Chamberlain
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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
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Patent number: 4472398Abstract: Antiphlogistic and anticoagulant compounds of the formula: ##STR1## wherein m is 0, 1 or 2,n is 0, 1 or 2,R is C.sub.1 to C.sub.6 alkyl,R.sub.1 is hydrogen, or C.sub.1 to C.sub.6 alkyl,R.sub.2 is hydrogen, C.sub.1 to C.sub.6 alkyl, substituted or unsubstituted amino, substituted or unsubstituted hydroxy, carboxy or a group derived from a carboxylic acid orR.sub.1 and R.sub.2 together form a --(CH.dbd.CH).sub.2 --group andR.sub.5 is 0 or imino or substituted imino.Type: GrantFiled: February 23, 1979Date of Patent: September 18, 1984Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.Inventors: Zoltan Meszaros, Jozsef Knoll, Istvan Hermecz, Agnes Horvath, Sandor Virag, Lelle Vasvari, nee Debreczy, Agoston David
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Patent number: 4460771Abstract: New optionally racemic or optically active pyrimido(1,2a) heterocyclic compounds of the formula ##STR1## wherein m is 0, 1 or 2,n is 0, 1 or 2,R is an alkyl group containing one to six carbon atoms,R.sup.1 is hydrogen, alkyl containing one to six carbon atoms,R.sup.2 is hydrogen, alkyl containing one to six carbon atoms, optionally substituted amino, optionally substituted hydroxy, carboxy or a group derived from a carboxylic acid orR.sup.1 and R.sup.2 together form a --(CH.dbd.CH).sub.2 -- group attached to the two adjacent carbon atoms of the ring A and the broken line represents a chemical bond,R.sup.3 is hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocycle, optionally substituted cycloalkyl, optionally substituted acyl or optionally substituted hydroxy,R.sup.Type: GrantFiled: November 17, 1976Date of Patent: July 17, 1984Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara R.T.Inventors: Zoltan Meszaros, Jozsef Knoll, Peter Szentmiklosi, Istvan Hermes, Agnes Horvath, Sandor Virag, Lelle Vasvari nee Debreczy, Agoston David
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Patent number: 4457927Abstract: Pyrido[2,1-b]quinazolinones of the formula ##STR1## wherein X is cyano, hydroxyamidocarbonyl, carbamoyl, 5-tetrazolyl, carboxy, carboxy in the form of a salt thereof with a physiologically compatible base, carboxy esterified with a physiologically acceptable alcohol or carboxy amidated with a physiologically acceptable amine;R.sub.1 is hydrogen or methyl; andR.sub.2 through R.sub.5 are independently each hydrogen, halogen, alkyl of 1-4 carbon atoms, trifluoromethyl, carboxy, thiocyano, methylthio, methylsulfinyl, methylsulfonyl, methylsulfonimidoyl or methylsulfonamido with the proviso that two or three of the groups R.sub.2 through R.sub.5 are hydrogen; or a salt thereof with a physiologically acceptable acid or base;possess valuable pharmacological properties.Type: GrantFiled: December 22, 1982Date of Patent: July 3, 1984Assignee: Schering, AktiengesellschaftInventors: Helmut Biere, Joachim-Friedrich Kapp, Irmgard Bottcher
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Patent number: 4454319Abstract: Pyrimido[6,1-a]isoquinoline-4-one derivatives of the formula: ##STR1## wherein R is C.sub.1 -C.sub.6 lower alkyl or 2-haloethyl (halo=Cl, Br or I) having antihypertensive activity.Type: GrantFiled: June 1, 1982Date of Patent: June 12, 1984Assignee: McNeilab, Inc.Inventors: Bruce E. Maryanoff, Albert J. Molinari
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Patent number: 4444768Abstract: Novel amidines, especially N,N'-bridged carboxylic acid amidines of the general formula ##STR1## in which R.sub.1 represents an aromatic radical, R.sub.2 represents optionally esterified or amidated 1-carboxy-lower alkyl, Ph represents optionally substituted 1,2-phenylene and alk represents an aliphatic hydrocarbon radical separating the imino group from the methine group by from 1 to 3 carbon atoms, and their salts, have, inter alia, anti-inflammatory activity and can be used as active medicament substances in pharmaceutical preparations. They are produced according to methods known per se.Type: GrantFiled: July 1, 1982Date of Patent: April 24, 1984Assignee: Ciba-Geigy CorporationInventors: Ulrich Renner, Knut A. Jaeggi
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Patent number: 4443451Abstract: Novel 5H-thiazolo- and 5H-1,3,4-thiadiazolo[3,2-a]pyrimidin-5-one and 3,4-dihydro-2H,6H-pyrimido[2,1-b] [1,3]-thiazin-6-one derivatives, which compounds are useful psychotropic agents.Type: GrantFiled: April 21, 1982Date of Patent: April 17, 1984Assignee: Janssen Pharmaceutica N.V.Inventors: Ludo E. J. Kennis, Josephus C. Mertens
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Patent number: 4428952Abstract: Substituted Pyrrolo [2,1-b] and Pyrido [2, 1 b] Quinazolines are provided, together with pharmaceutical compositions, containing them. The compounds have pharmaceutical utility, and are particularly useful for the treatment of or prevention of the formation of gastrointestinal ulcers.Type: GrantFiled: June 10, 1982Date of Patent: January 31, 1984Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Gianfederico Doria, Carlo Passarotti, Giuliana Arcari
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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
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Patent number: 4400506Abstract: What are disclosed are compounds of the formula ##STR1## wherein, X is oxygen, sulfur, or halogen, useful as intermediates in the preparation of certain pyrimido(6,1-a)isoquinolin-4-ones having pharmaceutical utilities, and methods for making said intermediates.Type: GrantFiled: October 26, 1981Date of Patent: August 23, 1983Assignee: Hoechst AktiengesellschaftInventors: Bansi Lal, Adolf D'Sa, Horst Dornauer, Noel J. de Souza
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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
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Patent number: 4367173Abstract: Azo compounds of the formula: ##STR1## wherein D is a radical of the formula: ##STR2## where Y.sup.1 is acylamino, hydrogen, chlorine, bromine, nitro, cyano, carboxylic acid or ester, trifluoromethyl, alkoxy, methylsulfonyl, and substituted or substituted carbamyl or sulfamyl, phenylcarbonyl, naphthylcarbonyl, pyridylcarbonyl, oxodiazolyl, quinazolonyl phthalazinonyl, phenylazo, naphthylazo, or pyridylazo,Y.sup.2 is hydrogen, chlorine or bromine,Y.sup.4 is hydrogen or chlorine,and wherein D is free from complex forming hydroxy or carboxy; R is hydrogen, phenyl, naphthyl or pyridyl and X is alkyl or a carboxylic acid alkyl ester, or is phenyl, naphthyl or pyridyl, or acylamino, can be used as pigments for coloring surface coatings, printing inks or plastics.Type: GrantFiled: October 28, 1980Date of Patent: January 4, 1983Assignee: BASF AktiengesellschaftInventor: Hartmut Kanter
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Patent number: 4348396Abstract: Pyrido[2,1-b]quinazolines of the formulas ##STR1## wherein R.sub.1, R.sub.1 ', R.sub.2, R.sub.2 ', R.sub.3, R.sub.3 ', R.sub.4 and R.sub.10 are as hereinafter set forth, and processes for the preparation thereof, are described. The compounds of formulas I and II are useful as agents in the prevention of allergic reactions.Type: GrantFiled: May 2, 1980Date of Patent: September 7, 1982Assignee: Hoffmann-La Roche Inc.Inventors: Richard W. Kierstead, Jefferson W. Tilley
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Patent number: 4332802Abstract: This invention relates to the novel compound 11-oxo-11H-pyrido[2,1-b]quinazoline-2-carboxylic acid of the formula ##STR1## and non-toxic, pharmacologically acceptable salts thereof, as well as to pharmaceutical composition containing these compounds as active ingredients, and methods of using them as antiallergics.Type: GrantFiled: November 5, 1980Date of Patent: June 1, 1982Assignee: Boehringer Ingelheim KGInventors: Kurt Schromm, Anton Mentrup, Ernst-Otto Renth, Armin Fugner
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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
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Patent number: 4310526Abstract: Substituted 6,7-methylen[1,2-a]pyrimidines and pharmaceutical compositions containing them, suitable for use as anti-allergic, anti-ulcer and anti-diabetic agents.Type: GrantFiled: April 10, 1980Date of Patent: January 12, 1982Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Gianfederico Doria, Ciriaco Romeo, Piero Sberze, Marcellino Tibolla, Maria L. Corno
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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
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Patent number: 4294755Abstract: Azo compounds of the general formula ##STR1## where D is the radical of a diazo component of the aminoanthraquinone or aminophthalimide series, or the radical of a tetraazo component H.sub.2 N--D--NH.sub.2 having the formula: ##STR2## where Z is a direct bond, SO.sub.2, NH, CO, SO.sub.2 NH, CONH, NHCONH or NHCOCONH and the rings B are unsubstituted or substituted by Cl, Br, CH.sub.3, NO.sub.2 or OCH.sub.3 ; wherein said radical D is free from complex-forming hydroxyl and carboxyl groups and from ionic groups, n is 1 or 2, R is hydrogen or an aromatic radical, X is hydroxyl, alkyl, a carboxylic acid ester group, unsubstituted or substituted aryl or acylamino, and the ring A may be substituted but is free from SO.sub.3 H groups, are exceptionally suitable for use as pigments, for example for coloring surface coatings, printing inks or plastics.Type: GrantFiled: October 10, 1979Date of Patent: October 13, 1981Assignee: BASF AktiengesellschaftInventor: Hartmut Kanter
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Patent number: 4288438Abstract: Novel nitrogen-containing heterocyclic compounds shown by the formula ##STR1## wherein one of R.sub.1 and R.sub.2 represents a lower alkyl group, a phenyl group, a halophenyl group, or a lower alkoxyphenyl group and the other of them represents a hydrogen atom, a lower alkyl group, or a phenyl lower alkyl group; said R.sub.1 and R.sub.2 may combine with each other to form a trimethylene group or a tetramethylene group; R.sub.3 represents a hydrogen atom, a lower alkyl group, a phenyl group, or a phenyl lower alkyl group; X represents an oxygen atom, a sulfur atom, an imino group, or a group shown by ##STR2## (wherein m represents 1 or 2 and R.sub.4 represents a lower alkyl group, a hydroxy lower alkyl group, a cycloalkyl group or a phenyl lower alkyl group); and Y represents an ethylene group which may be substituted by lower alkyl group, a trimethylene group, a tetramethylene group, a vinylene group which may be substituted by a lower alkyl group, or ##STR3## (wherein R.sub.Type: GrantFiled: August 20, 1979Date of Patent: September 8, 1981Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kazuo Kubo, Noriki Ito, Isao Souzu, Yasuo Isomura, Hiroshige Homma, Masuo Murakami
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Patent number: 4273773Abstract: 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: September 24, 1979Date of Patent: June 16, 1981Assignee: American Home Products CorporationInventors: Christopher A. Demerson, Leslie G. Humber, Jean-Marie Ferland
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Patent number: 4260612Abstract: Antiallergic and antiasthmatic compounds of the formula ##STR1## of which 9-phenylamino-6-methyl-4-oxo-6,7-dihydro-4H-pyrido(1,2-a)pyrimidine-3-carb oxylic acid and optically active antipodes and salts thereof are examples.Type: GrantFiled: December 11, 1978Date of Patent: April 7, 1981Assignee: Chinoin Gyogyszer es Vecyeszeti Termekek Gyara Rt.Inventors: Istvan Hermecz, Zoltan Meszaros, Tibor Breining, Sandor Virag, Lelle Vasvari nee Debreczi, Agnes Horvath, Gabor Nagy, Attila Mandi, Tamas Szuts, Istvan Bitteer, Gyula Sebestyen
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Patent number: 4247699Abstract: The reaction of isatoic anhydrides with malononitrile in a reaction-inert solvent in the presence of a base to produce 2-amino-3-cyano-4-hydroxy-quinolines and 2-amino-.alpha.,.alpha.-dicyanoacetophenones which are then hydrolyzed and decarboxylated under acid or base conditions to produce 2-amino-4-hydroxy-quinolines, useful as intermediates for preparation of 1-oxo-1H-6-alkoxy-pyrimido[1,2-a]quinoline-2-carboxylic acids and esters of value as antiallergy agents.Type: GrantFiled: March 14, 1979Date of Patent: January 27, 1981Assignee: Pfizer Inc.Inventor: Saul B. Kadin
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Patent number: 4220771Abstract: Pharmaceutical intermediates, morphine potentiators and other compounds have the formula ##STR1## wherein R is hydrogen, halogen, C.sub.1-4 alkyl, hydroxy, nitro, amino, carboxy or a carboxylic acid derivate radical, R.sup.1 is hydrogen or a C.sub.1-4 alkyl, R.sup.2 is hydrogen or C.sub.1-4 alkyl, R.sup.3 is hydrogen, R.sup.4 is hydrogen or C.sub.1-4 alkyl, R.sup.5 is hydrogen R.sup.6 is hydrogen or R.sup.3 and R.sup.4 and/or R.sup.5 and R.sup.6 form a chemical bond, X is oxygen or imino, m is 1, 2, 3 or 4, n is 0, 1, 2 or 3, and if n is 1, then the dotted lines can stand for bonds, with the proviso that if m=1 and n=1 and if in the 2,3-, 6,7-, 8,9- and 1,10-positions double bonds are present, and R.sup.1 and R.sup.2 are hydrogen, then R is other than 9-hydroxy or 9-methyl; if m=2 and n=1 and R.sup.2 is hydrogen, then at least one of R and R.sup.1 is other than hydrogen; and if m=2 and n=2 and R.sup.2 is hydrogen and the molecule is a 2,3,4,6,7,8,9,10-octahydro derivative, then at least one of R and R.sup.Type: GrantFiled: August 18, 1978Date of Patent: September 2, 1980Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara RtInventors: Istvan Hermecz, Ferenc Fulop, Zoltan Meszaros, Gabor Bernath, Jozsef Knoll
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Patent number: 4214089Abstract: The use of 3-aryl-thiazolo[3,2-a]benzimidazoles, 3-aryl-imidazo[2,1-b]thiazoles, and related compounds as antineoplastic agents, and/or as enhancers of the immune response is disclosed.Type: GrantFiled: July 18, 1978Date of Patent: July 22, 1980Assignee: American Home Products CorporationInventors: Richard L. Fenichel, Peter H. L. Wei, Francis J. Gregory, Harvey E. Alburn
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Patent number: 4209620Abstract: A novel series of substituted 3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-ones is provided for use as inhibitors of allergic reactions. The compounds exhibit antiallergy activity by both oral and parenteral routes of administration.Type: GrantFiled: October 16, 1978Date of Patent: June 24, 1980Assignee: Bristol-Myers CompanyInventor: Peter F. Juby