The Nitrogen Is Part Of A Substituent Which Contains Additional Nonionically Bonded Nitrogen Patents (Class 546/106)
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Patent number: 5312820Abstract: Carbamoyl and oxycarbonyl derivatives of biphenylmethylamines of structure I are angiotensin-II antagonists with balanced AT.sub.1 and AT.sub.2 activity useful in the treatment of hypertension and related disorders and ocular hypertension. ##STR1## where X is --O-- or --N(R.sup.7)--.Type: GrantFiled: July 17, 1992Date of Patent: May 17, 1994Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Linda L. Chang, William J. Greenlee, Steven M. Hutchins, Ralph A. Rivero
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Patent number: 5294715Abstract: Hypoxia selective cytotoxins of the general formula ##STR1## wherein n is from 1 to 5, and NO.sub.2 is in at least one of the 2, 4 or 5-positions of the imidazole. Such compounds have utility as radiosensitizers and chemosensitizers.Type: GrantFiled: February 1, 1991Date of Patent: March 15, 1994Assignee: University of PittsburghInventors: Maria Papadopoulou-Rosenzweig, William D. Bloomer, William D. Bloomer
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Patent number: 5204348Abstract: Novel heterocyclic compounds, which are represented by the following general formula, useful as anticancer drug potentiaters having a potentiating effect on the incorporation of anticancer drugs into cancer cells, the compounds each synthesized by, for example, reacting a epoxy compound obtained by reacting a heterocyclic compound with an epihalogenohydrin, with an amine derivative.Type: GrantFiled: December 3, 1991Date of Patent: April 20, 1993Assignee: Mitsui Toatsu Chemicals Inc.Inventors: Nobuyuki Fukazawa, Makoto Odate, Tsuneji Suzuki, Kengo Otsuka, Takashi Tsuruo, Wakao Sato
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Patent number: 5120745Abstract: This invention relates to 1-dimethylcarbamoyl-3-substituted-5-substituted-1H-1,2,4-triazoles of the formula ##STR1## wherein the substituents are as defined herein, compositions containing those compounds and methods of use.Type: GrantFiled: September 27, 1990Date of Patent: June 9, 1992Assignee: Shell Internationale Research Maatschappij B.V.Inventors: Richard M. Jacobson, Luong T. Nguyen, Muthuvelu Thirugnanam
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Patent number: 5100904Abstract: A novel prolinal derivatives of the general formula: ##STR1## [wherein A represents alkylene or alkenylene group of from 1 to 8 carbon atom(s) or a saturated hydrocarbon ring of from 3 to 7 carbon atoms,R represents hydrogen atom, phenyl group, benzyl group, alkyl group of from 1 to 8 carbon atom(s) or cycloalkyl group of from 3 to 7 carbon atoms,B represents alkylene group of from 1 to 8 atom(s) unsubstituted or substituted by phenyl group or benzyl group, or a single bond,D represents carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three of halogen atom, alkyl or alkoxy group of from 1 to 4 carbon atom(s), nitro group or trifluoromethyl group.]possess inhibitory activity on prolyl endopeptidase, and therefore are useful for treating and/or preventing agent as a amnesia.Type: GrantFiled: June 5, 1990Date of Patent: March 31, 1992Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaaki Toda, Shuichi Ohuchida, Hiroyuki Ohno
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Patent number: 5089615Abstract: There are described compounds of the formula ##STR1## where X is hydrogen, loweralkyl, loweralkoxy or halogen;R when present is hydrogen, loweralkyl or aryloweralkyl;R.sub.1 is hydrogen, loweralkyl or arylloweralkyl; andR.sub.2 when present is hydrogen or loweralkyl;which compounds are useful for alleviating various memory dysfunctions characterized by a decreased cholinergic function such Alzheimer's disease.Type: GrantFiled: January 11, 1991Date of Patent: February 18, 1992Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Lawrence L. Martin, Joseph F. Payack, Helen H. Ong
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Patent number: 4999358Abstract: There are described compounds of the formula, ##STR1## where X is hydrogen, loweralkyl, loweralkoxy or halogen;R when present is hydrogen, loweralkyl or arylloweralkyl;R.sub.1 is hydrogen, loweralkyl or arylloweralkyl; andR.sub.2 when present is hydrogen or loweralkyl;which compounds are useful for alleviating various memory dysfunctions characterized by a decreased cholinergic function such Alzheimer's disease.Type: GrantFiled: June 26, 1989Date of Patent: March 12, 1991Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Lawrence L. Martin, Joseph F. Payack, Helen H. Ong
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Patent number: 4985430Abstract: There are disclosed a 9-acylamino-tetrahydroacridine derivative represented by the following formula (I): ##STR1## wherein R ##STR2## are as defined in the specification, its optical antipode or pharmaceutically acceptable acid addition salt thereof and a memory enhancing agent containing the same as an active ingredient.Type: GrantFiled: December 2, 1988Date of Patent: January 15, 1991Assignee: Mitsubishi Kasei CorporationInventors: Shuji Morita, Ken-Ichi Saito, Kunihiro Ninomiya, Akihiro Tobe, Issei Nitta, Mamoru Sugano
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Patent number: 4952589Abstract: This invention relates to aminoalkylphenoxyalkyl substituted heterocycles. These compounds antagonize the action of histamine on histamine H.sub.2 -receptors in the brain. A compound of the invention is 2-[3-[3-(piperidinomethyl)phenoxy]propylamino]benzthiazole.Type: GrantFiled: June 3, 1987Date of Patent: August 28, 1990Assignee: Smith Kline & French Laboratories LimitedInventors: Thomas H. Brown, Robert C. Mitchell, Ian R. Smith, Rodney C. Young
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Patent number: 4916135Abstract: There are described compounds of the formula ##STR1## where --R is ##STR2## --R.sub.3 and R.sub.3 being independently --H, loweralkyl, --CHO, --CH.dbd.CH.sub.2, --CH.dbd.CH--loweralkyl, --CH.dbd.CHCO.sub.2 C.sub.2 H.sub.5, --CH.sub.2 N(C.sub.2 H.sub.5).sub.2 or ##STR3## --R.sub.1 when existent is --H, loweralkyl, --CH.sub.2 C.tbd.CH, ##STR4## R.sub.5 being methyl or phenyl optionally mono-substituted with loweralkyl or loweralkoxy;--R.sub.2 when existent is loweralkyl or --CH.sub.2 C.tbd.CH;--X is --H, loweralkyl, loweralkoxy, halogen or trifluoromethyl; and the two --Y groups when existent are both --H, or combine to constitute --(CH.sub.2).sub.4 --;which compounds are useful as analgesic agents, and for treating various memory dysfunctions characterized by decreased cholinergic function such as Alzheimer's disease.Type: GrantFiled: May 8, 1989Date of Patent: April 10, 1990Assignee: Hoechst Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Joseph T. Klein, Larry Davis, Gordon E. Olsen
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Patent number: 4851536Abstract: There are disclosed compounds of the formula ##STR1## wherein X is O, S, SO, SO.sub.2 or CR.sup.1 R.sup.2 ;R.sup.1 and R.sup.2 are each independently hydrogen, lower alkyl, carboxyl, lower alkoxy carbonyl, lower cycloalkyl, phenyl, naphthyl, pyridyl, quinolinyl, pyrazinyl, pyridinyl, pyridazinyl, pyrimidinyl, quinoxalinyl, quinazolinyl or any of the foregoing aryl or hetaryl substituents substituted with halo, lower alkyl, lower alkyl carbonyl, benzoyl, COOR.sup.3, OR.sup.3, N(R.sup.3).sub.2, CON(R.sup.3).sub.2, SO.sub.3 R.sup.3, SO.sub.2 N(R.sup.3).sub.2, phenylsulfonyl, lower alkyl sulfonyl, cyano, nitro or trifluoromethyl;R.sup.3 is hydrogen, lower alkyl or phenyl;R.sup.4 is halo, morpholino, 4-methylpiperazino, R.sup.5 NNHR.sup.6,R.sup.5 NCH.sub.2 CH.sub.2 OCH.sub.3, or ##STR2## R.sup.5 is hydrogen or lower alkyl; R.sup.6 is hydrogen, lower alkyl, lower alkanoyl, lower cycloalkyl or phenyl; andR.sup.7 and R.sup.Type: GrantFiled: April 20, 1988Date of Patent: July 25, 1989Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Steven C. Gilman
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Patent number: 4839364Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1, 2 or 3; X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, NHCOR.sub.2 where R.sub.2 is loweralkyl, or NR.sub.3 R.sub.4 where R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R is hydrogen or loweralkyl; R.sub.1 is hydrogen, loweralkyl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, furylloweralkyl, thienylloweralkyl, oxygen-bridged arylloweralkyl, oxygen-bridged diarylloweralkyl, oxygen-bridged furylloweralkyl or oxygen-bridged thienylloweralkyl; Y is C.dbd.O or CR.sub.5 OH where R.sub.5 is hydrogen or loweralkyl; Z is CH.sub.2 or C.dbd.CR.sub.6 R.sub.7 where R.sub.6 and R.sub.7 are independently hydrogen or loweralkyl; or Y and Z taken together is CR.sub.5 .dbd.Ch where CR.sub.Type: GrantFiled: January 28, 1987Date of Patent: June 13, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Gregory M. Shutske, Frank A. Pierrat
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Patent number: 4834769Abstract: Dye compositions containing (a) at least one blue sulpho group-containing triphendioxazine dye and (b) at least one blue sulpho group-containing anthraquinone dye and preferably (c) lignine sulphonic acid or a salt of it and optionally (d) a non-ionic blending agent are outstandingly suitable for the level and fast dyeing of leather substrates.Type: GrantFiled: December 8, 1987Date of Patent: May 30, 1989Assignee: Sandoz Ltd.Inventors: Michel Dien, Herbert Holliger
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Patent number: 4824472Abstract: Novel herbicidal 1-cyclyl or polycyclyl substituted 1H-imidazole-5-carboxylic acid derivatives, compositions containing these compounds as active ingredients, and a method for controlling weeds, preferably selectively in crops of useful plants. Processes for making these novel compounds.Type: GrantFiled: December 23, 1987Date of Patent: April 25, 1989Assignee: Janssen Pharmaceutica N.V.Inventors: Guy R. E. Van Lommen, Victor Sipido, Wim G. Verschueren, William R. Lutz
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Patent number: 4813998Abstract: Novel herbicidal 1-heterocyclyl-1H-imidazole-5-carboxylic acid derivatives, compositions containing these compounds as active ingredients, and a method for controlling weeds, preferably selectively in crops of useful plants. Further the invention also relates to a process for making these novel compounds.Type: GrantFiled: August 24, 1987Date of Patent: March 21, 1989Assignee: Janssen Pharmaceutica N.V.Inventors: Guy R. E. Van Lommen, William R. Lutz, Jozef F. E. Van Gestel
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Patent number: 4711889Abstract: The invention relates to acridanone derivatives of the formula ##STR1## wherein the dotted line is an optional bond, R.sup.1 is hydrogen, halogen or nitro,R.sup.2 is hydrogen or lower alkyl,one of R.sup.3 and R.sup.4 is hydrogen or lower alkyl and the other together with R is an additional bond,A is lower alkylene,R.sup.5 is a 5-membered nitrogen-containing, optionally lower alkyl-substituted aromatic heterocycle, amino or the group ##STR2## the symbol is a 5- or 6-membered, optionally lower alkyl-substituted saturated heterocycle which can contain as a ring member oxygen or sulfur or the group >NH or >N(B).sub.n --A.sup.1 --R.sup.6, B is the group --CO--, --COO-- or --SO.sub.2 --, n is the number 0 or 1, A.sup.1 is lower alkylene, R.sup.6 is hydrogen, amino, lower alkylamino or di(lower alkyl)amino and R.sup.7 is hydrogen or lower alkyl, and pharmaceutically acceptable acid addition salts thereof, their preparation and pharmaceutical compositions based thereon.Type: GrantFiled: July 18, 1986Date of Patent: December 8, 1987Assignee: Hoffman-La Roche Inc.Inventors: Urs Brombacher, Helmut Link, Marc Montavon
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Patent number: 4704397Abstract: Pharmaceutical salts of 4'-(9-acridinylamino)--methanesulfon-m-anisidide, methods for their preparation and use of said salts in the form of pharmaceutical compositions as antineoplastic agents.Type: GrantFiled: September 16, 1981Date of Patent: November 3, 1987Assignee: Warner-Lambert CompanyInventors: James R. Fisher, Charles P. Kulier
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Patent number: 4695573Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1, 2 or 3; X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, NHCOR.sub.2 where R.sub.2 is loweralkyl, or NR.sub.3 R.sub.4 where R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R is hydrogen or loweralkyl; R.sub.1 is hydrogen, loweralkyl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, furylloweralkyl, thienylloweralkyl, oxygen-bridged arylloweralkyl, oxygen-bridged diarylloweralkyl, oxygen-bridged furylloweralkyl or oxygen-bridged thienylloweralkyl; Y is C.dbd.O or CR.sub.5 OH where R.sub.5 is hydrogen or loweralkyl; Z is CH.sub.2 or C.dbd.CR.sub.6 R.sub.7 where R.sub.6 and R.sub.7 are independently hydrogen or loweralkyl; or Y and Z taken together is CR.sub.5 .dbd.CH where CR.sub.Type: GrantFiled: October 1, 1985Date of Patent: September 22, 1987Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Frank A. Pierrat
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Patent number: 4663458Abstract: This invention relates to novel compositions of the antitumor agent [4'-9-(acridinylamino) methanesulfon-m-anisidide] (m-AMSA). The m-AMSA lactate salts in combination with Tween-80 provide a highly stable, ready to use aqueous product.Type: GrantFiled: December 9, 1985Date of Patent: May 5, 1987Assignee: Bristol-Myers CompanyInventor: Murray A. Kaplan
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Patent number: 4603125Abstract: Compounds represented by the general formula (I): ##STR1## in which R.sub.1 represents ##STR2## A and B each represent H or a lower alkane optionally substituted with amino and/or hydroxyl functions, except that A and B are not both H; R.sub.3 represents H, OCH.sub.3, CH.sub.3, halogen, NH.sub.2, NO.sub.2, NHCH.sub.3, N.sub.3 (CH.sub.3).sub.2, N.sub.3, NHCOCH.sub.3, NHCOOCH.sub.3, N(CH.sub.3)COOCH.sub.3, CONH.sub.2 or CONHCH.sub.3 ; R.sub.4 represents H, alkyl, O-alkyl, CONH.sub.2, CONHCH.sub.3 or CONHCH.sub.2 CONHCH.sub.3, except that R.sub.3 and R.sub.4 taken together can represent --C.dbd.CH--CH.dbd.N--; R.sub.5 represents H, alkyl, O-alkyl, CONH.sub.2, CONHCH.sub.3 or CONH.sub.2 CH.sub.2 CONHCH.sub.3 ; R.sub.6 represents lower alkyl; R.sub.7 represents CH.sub.3 or C.sub.6 H.sub.5 (phenyl); R.sub.8 represents lower alkyl or C.sub.6 H.sub.5 (phenyl); R.sub.9 represents H, NHCOCH.sub.3, NH.sub.2 or N.dbd.CHN(CH.sub.3).sub.2 ; and R.sub.10 represents H or NH.sub.Type: GrantFiled: November 14, 1983Date of Patent: July 29, 1986Assignee: Development Finance Corporation of New ZealandInventors: Graham J. Atwell, Bruce C. Baguley, William A. Denny, Gordon W. Rewcastle
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Patent number: 4590277Abstract: 4-Carboxamidoacridine compounds represented by the general formula (I), ##STR1## where R.sub.1 represents H, CH.sub.3 or NHR.sub.3, where R.sub.3 is H, COCH.sub.3, SO.sub.2 CH.sub.3, COPh, SO.sub.2 Ph or lower alkyl optionally substituted with hydroxyl and/or amino functions;R.sub.2 represents H or up to two of the groups CH.sub.3, OCH.sub.3, halogen, CF.sub.3, NO.sub.2, NH.sub.2, NHCOCH.sub.3, and NHCOOCH.sub.3 placed at positions 1-3 or 5-8;Y represents C(NH)NH.sub.2, NHC(NH)NH.sub.2, or NR.sub.4 R.sub.5, where each of R.sub.4 and R.sub.5 is H or lower alkyl optionally substituted with hydroxyl and/or amino functions; andx is from 2 to 6,and the acid addition salts thereof, possess antibacterial and antitumor properties.Type: GrantFiled: June 21, 1983Date of Patent: May 20, 1986Assignee: Development Finance Corporation of New ZealandInventors: Graham J. Atwell, Bruce C. Baguley, William A. Denny, Gordon W. Rewcastle
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Patent number: 4575509Abstract: This invention concerns novel water-soluble salts and compositions of the antitumor agent 4'-(9-acridinylamino) methanesulfon-m-anisidide (m-AMSA). More particularly, there are provided (1) the mono- and dipyroglutamate salts of m-AMSA and (2) compositions of m-AMSA with pyroglutamic acid. The novel salts and compositions provided enable m-AMSA to be administered as an aqueous solution without the necessity of using dimethylacetamide as a pharmaceutical vehicle.Type: GrantFiled: July 18, 1984Date of Patent: March 11, 1986Assignee: Bristol-Myers CompanyInventors: Jivn-Ren Chen, Edward C. Shinal
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Patent number: 4575553Abstract: The compounds are of the class of 9-anilinoacridines, useful as antitumor agents and are analogs of m-AMSA. These compounds have the formula ##STR1## in which R.sup.1 is Br, Cl or CH.sub.3, and R.sup.2 is CH.sub.2 NHCH.sub.3, CH.sub.2 N(CHO)CH.sub.3 or CH.sub.2 NHCHO. Intermediate 3-substituted-9(10H)acridone-5-carboxylic acids are prepared by converting diphenylaminedicarboxylic acids via acyl chloride to dipiperidides, purifying the dipiperidides, treating said dipiperidides with phosphorous oxychloride in an inert organic solvent at a temperature in the range of about 70.degree. C. to 110.degree. C. to yield 9-acridine, subjecting said 9-acridine to mild acid hydroylsis to yield 9-acridone and thereafter hydroylzing said 9-acridones to the acid product.Type: GrantFiled: June 18, 1984Date of Patent: March 11, 1986Assignee: Bristol-Myers CompanyInventors: Gerry Kavadias, Terrance W. Doyle, Elizabeth Janik, Richard A. Partyka
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Patent number: 4544659Abstract: Acridanone derivatives of the formula ##STR1## wherein the dotted line is an optional bond, R.sup.1 is hydrogen, halogen or nitro, R.sup.2 is hydrogen or lower alkyl, one of the substituents R.sup.3 and R.sup.4 is hydrogen or lower alkyl and the other together with R is an additional bond and R.sup.5 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl or lower alkyl substituted by halogen or lower alkoxy,and pharmaceutically acceptable acid addition salts thereof, processes for their preparation and pharmaceutical compositions based thereon, are described. The compounds of formula I are useful as schistosomicidal agents.Type: GrantFiled: November 15, 1983Date of Patent: October 1, 1985Assignee: Hoffman-La Roche Inc.Inventors: Urs Brombacher, Marc Montavon, Hermann Bretschneider, Joachim Schantl, Wolfgang Turk
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Patent number: 4472582Abstract: 3,5-Disubstituted-4'-(9-acridinylamino)-methane-sulfon-m-anisidide compounds represented by the general formula ##STR1## in which R.sup.2 and R.sup.3 represent, respectively, --CH.sub.3 and --CONHCH.sub.3, --CH.sub.3 and --CONHCH.sub.2 CONH.sub.2, --Cl and --CONHCH.sub.2 CONH.sub.2, --CONHCH.sub.3 and --CH.sub.3 ; and acid addition salts thereof have unexpectedly high antitumor activity in leukemic animals and low or no direct mutagenicity.Type: GrantFiled: June 7, 1982Date of Patent: September 18, 1984Assignee: Development Finance Corporation of New ZealandInventors: Bruce F. Cain, deceased, Graham J. Atwell, Bruce C. Baguley, William A. Denny
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Patent number: 4399283Abstract: Pharmaceutical salts of 4'-(9-acridinylamino)-methanesulfon-m-anisidide, methods for their preparation and use of said salts in the form of pharmaceutical compositions as antineoplastic agents.Type: GrantFiled: September 16, 1981Date of Patent: August 16, 1983Assignee: Warner Lambert CompanyInventors: James R. Fisher, Charles P. Kulier
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Patent number: 4366318Abstract: The compound 4'-(9-[4-[N-methyl-carboxamido]-5-methyl]acridinylamino)methanesulphon-m-a nisidide and acid addition salts thereof have antitumor properties.Type: GrantFiled: April 27, 1981Date of Patent: December 28, 1982Assignee: Development Finance Corporation of New ZealandInventors: Bruce F. Cain, deceased, Graham J. Atwell
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Patent number: 4335244Abstract: This invention concerns three particular crystalline monolactate salts of the antitumor agent 4'-(9-acridinylamino)methanesulfon-m-anisidide. The salts are characterized in having unexpectedly high water-solubility.Type: GrantFiled: May 23, 1980Date of Patent: June 15, 1982Assignee: Bristol-Myers CompanyInventors: Murray A. Kaplan, Alphonse P. Granatek
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Patent number: 4335226Abstract: Adsorbents are provided for the affinity-specific separation of macromolecular materials, particularly biopolymers, the adsorbents comprising a polymeric carrier on to which an affine residue for the macromolecular material is covalently bound, either directly or via polymeric spacer. Preferred affine residue is comprised of a specific complex formers which are base-specific and/or structure specific for the macromolecular material. The invention also provides novel complex formers comprising a certain dyestuff residues and processes for their preparation.Type: GrantFiled: February 24, 1978Date of Patent: June 15, 1982Assignee: Boehringer Mannheim GmbHInventors: Werner Muller, Hans Bunemann
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Patent number: 4322424Abstract: The invention concerns a crystalline monogluconate salt of the antitumor agent 4'-(9-acridinylamino)-methanesulfon-m-anisidide and compositions comprising mixtures of such salt with an organic acid selected from gluconic acid, gluconolactone or mixtures thereof. The novel salt and compositions are characterized in having unexpectedly high water-solubility.Type: GrantFiled: October 17, 1980Date of Patent: March 30, 1982Assignee: Bristol-Myers CompanyInventors: Daniel Bouzard, Claude Perol, Jacques Stemer, Abraham Weber, Edmund S. Granatek
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Patent number: 4258191Abstract: A multi-step method of producing the compound methanesulfon-m-anisidide, 4'-(9-acridinylamino)-, acetate (VII), which may be in free base form and designated NSC 249992, also known as AMSA. This compound is produced by an elegant process from a starting material, 4-butyrylamino-3-methoxy-nitrobenzene, which is later transformed to methanesulfon-m-anisidide, 4'-amino- (IV) and is coupled or joined to 9-chloro-acridine, producing the chloride salt which is later converted to the acetate.Type: GrantFiled: March 29, 1979Date of Patent: March 24, 1981Assignee: The United States of America as represented by the Secretary of Health, Education and WelfareInventors: Henryk Dubicki, Jack L. Parsons, Fred W. Starks
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Patent number: 4150231Abstract: 1-Nitro-9-dialkylaminoisoalkylaminoacridines or their salts of the formula: ##STR1## wherein R is lower alkyl, such as methyl, ethyl, R.sup.1 is a hydrogen atom or methyl, R.sup.2 is the same as R.sup.1, with the proviso that R.sup.1 is not equal to R.sup.2 and n = 0 or 2, and their preparation is described. These compounds are useful as anti-neoplastic agents.Type: GrantFiled: March 25, 1977Date of Patent: April 17, 1979Assignee: Politechnika GdanskaInventors: Andrzej Ledochowski, Jerzy Gieldanowski, Czeslaw Radzikowski, Cecylia Kwasniewska-Rokicinska, Barbara Wysocka-Skrzela, Lucyna Sawinska, Mieczyslaw Medon
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Patent number: 4139531Abstract: 1-Nitro-9-alkylaminoalkylaminoacridins and their salts, as well as a method for obtaining these compounds, is described. The 1-nitro-9-alkylaminoalkylaminoacridines have the formula 1, ##STR1## wherein R is methyl, ethyl, propyl, isopropyl, butyl, isobutyl, isopentyl, benzyl or cyclohexyl, whereas n is equal to 2 or 3. The salts are those derived from mineral acids or organic acids. These compounds have anti-neoplastic activity.Type: GrantFiled: February 23, 1977Date of Patent: February 13, 1979Assignee: Politechnika GdanskaInventors: Andrzej Ledochowski, Jerzy Gieldanowski, Czeslaw Radzikowski, Barbara Horowska, Cecylia Kwasniewska-Rokicinska, Barbara Wysocka-Skrzela, Lucyna Sawinska, Mieczyslaw Medon
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Patent number: 4126620Abstract: 2,4,5,6-Tetrahydrocyclopenta[c]pyrrole-4-carboxamide and 4-thiocarboxamide derivatives useful as antisecretory and anti-ulcer agents are prepared by hydrolysis or thiohydrolysis of the corresponding 2,4,5,6-tetrahydrocyclopenta[c]pyrrole-4-carbonitriles or, in the case of the thiocarboxamides, by reaction of the 4-carboxamide with phosphorus pentasulfide.Type: GrantFiled: February 25, 1977Date of Patent: November 21, 1978Assignee: Sterling Drug Inc.Inventors: Malcolm R. Bell, Rudolf Oesterlin