Three Or More Amino Nitrogens Patents (Class 514/674)
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Patent number: 5889061Abstract: Compounds of Formula I:E-NH-D-NH-B-A-B-NH-D-NH-E (I)wherein A is C.sub.2 -C.sub.6 alkene, C.sub.3 -C.sub.6 cycloalkyl, cycloalkenyl, or cycloaryl; B is independently a single bond, C.sub.1 -C.sub.6 alkyl alkenyl; D is independently C.sub.1 -C.sub.6 alkyl or alkenyl, or C.sub.3 -C.sub.6 cycloalkyl, cycloalkenyl, or cycloaryl; and E is independently H, C.sub.1 -C.sub.6 alkyl or alkenyl; and pharmaceutically-suitable salts thereof; a synthetic method therefor, pharmaceutical dosage forms containing one of more of these compounds, and use of these compounds in the treatment of neoplastic cell growth, are disclosed.Type: GrantFiled: October 15, 1997Date of Patent: March 30, 1999Assignee: Wisconsin Alumni Research FoundationInventors: Benjamin J. Frydman, Laurence J. Marton, Vendohar K. Reddy, Aldonia L. Valasinas, Donald T. Witiak
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Patent number: 5886051Abstract: Methods and pharmaceutical compositions in unit dosage form for treating neurodegeneration in a human or non-human animal afflicted therewith wherein the active agent is a therapeutically effective amount of a polyamine having the formula: ##STR1## or a salt thereof with a pharmaceutically acceptable acid wherein: R.sub.1 and R.sub.6 may be the same or different and are hydrogen, alkyl, hydrocarbyl aryl, hydrocarbyl aryl alkyl, cycloalkyl, or any of the foregoing wherein the alkyl chain is interrupted by at least one etheric oxygen atom;N.sup.1, N.sup.2, N.sup.3 and N.sup.4 are nitrogen atoms capable of protonation at physiological pH's;a and b may be the same or different and are integers from 1 to 4;A, B and C may be the same or different and are bridging groups of variable length.Type: GrantFiled: November 8, 1995Date of Patent: March 23, 1999Assignees: University Of Florida Research Foundation, Inc., SunPharm CorporationInventors: Raymond J. Bergeron, Jr., Stefan Borg
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Patent number: 5886050Abstract: Polyamines having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are alkyl, aralkyl or aryl having up to 10 carbon atoms; anda and b may be the same or different and are integers from 1 to 8; ora salt thereof with a pharmaceutically acceptable acid. Anti-neoplastic, anti-diarrheal, anti-peristaltic, gastro-intestinal anti-spasmodic, anti-viral, anti-retroviral, anti-psoriasis and insecticidal compositions comprising biologically effective amounts of the above-described amines and biologically acceptable carriers therefor are also disclosed, as well as methods of treatment, administration or application of biologically effective amounts of the polyamines of the invention. Also disclosed are methods for preparing the polyamines of the invention.Type: GrantFiled: September 18, 1996Date of Patent: March 23, 1999Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.
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Patent number: 5880161Abstract: Therapeutic polyamines useful as a cancer chemotherapeutic agents, including molecules having a formula R.sub.1 --NH--(CH.sub.2).sub.x --NH-- (CH.sub.2).sub.x --NH-- (CH.sub.2).sub.y --NH--(CH.sub.2).sub.z --NH--R, wherein R.sub.1 and R.sub.2 are hydrocarbon chains having 1 to 5 carbons and w, x, y and z are integer of 1 to 10, are disclosed. One such molecule is N.sup.1, N.sup.19 -bis(ethylamino)-5,10,15-triazanonadecane, which is longer than spermine. This preferred compound may be used alone or in combination with other therapeutic agents, such as 1,3-bis(2-chloroethyl)-1-nitrosourea or cis-Pt.Type: GrantFiled: July 29, 1996Date of Patent: March 9, 1999Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Hirak Subhra Basu, Burt Feuerstein, Keijiro Samejima, Laurence Marton
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Patent number: 5866613Abstract: A polyamine and pharmaceutical composition containing an effective amount of the polyamine useful for administration to a human or non-human animal afflicted with neoplastic cells, the polyamine having the formula:R.sub.1 --NH--(CH.sub.2).sub.3 --NH--(CH.sub.2).sub.3 --NH--(CH.sub.2).sub.3 --NH--R.sub.2wherein R.sub.1 and R.sub.2 are both ethyl; or a salt thereof with a pharmaceutically acceptable acid, as well as a method of treatment comprising administering to such animals an effective amount of a polyamine of the above formula wherein R.sub.1 and R.sub.2 are each lower alkyl of 1-4 carbon atoms.Type: GrantFiled: June 7, 1995Date of Patent: February 2, 1999Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron
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Patent number: 5827894Abstract: An anti-viral, anti-psoriasis or anti-retroviral therapy based on the administration of a compound having one of the formulae: ##STR1## wherein: R.sub.1 and R.sub.6 may be the same or different and are alkyl having from 1 to 12 carbon atoms or hydrocarbyl aralkyl having up to 12 carbon atoms;R.sub.2 -R.sub.5 may be the same or different and are H, R.sub.1 or R.sub.6 ;m is an integer from 3 to 6, inclusive;n is an integer from 3 to 6, inclusive; or(III) a salt thereof with a pharmaceutically acceptable acid.Type: GrantFiled: September 18, 1996Date of Patent: October 27, 1998Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron
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Patent number: 5776352Abstract: The invention relates to a process for the treatment of water and of surfaces in contact with the said water in order to prevent the attachment and/or to, remove and/or to control macroorganisms, in particular molluscs, on the said surfaces in contact with the water, in which process at least one biocidal and/or biostatic active product is employed which is injected into the water and/or applied to the said surfaces, according to which process the active product(s) used comprise(s) at least one polyamine of formula I:R.sub.1 --NH?(CH.sub.2).sub.3 --NH!.sub.n --(CH.sub.2).sub.3 NH.sub.2(I)in which formula R.sub.1 is a C.sub.8 -C.sub.22 alkyl or alkenyl radical and/or at least one monoamine of formula II:R.sub.2 NH.sub.2 (II)in which formula R.sub.2 is a C.sub.8 -C.sub.22 alkyl or alkenyl radical, and n is an integer between 0 and 3 (inclusive).The invention also relates to a composition to be injected into the water and to a paint for covering the surfaces in contact with the water.Type: GrantFiled: April 1, 1996Date of Patent: July 7, 1998Inventor: Antoine Vanlaer
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Patent number: 5760091Abstract: A preventive agent against adhesion of a marine organism comprising: at least one amine compound represented by the following formula (I): ##STR1## , wherein R is a C.sub.8-22 saturated or unsaturated aliphatic hydrocarbon group, R.sup.1 is hydrogen atom, aminopropyl, a C.sub.1-22 saturated aliphatic hydrocarbon or C.sub.2-22 unsaturated aliphatic hydrocarbon group, R.sup.2 is aminopropyl, a C.sub.1-8 saturated aliphatic hydrocarbon or C.sub.2-8 unsaturated aliphatic hydrocarbon group, provided that R.sup.1 is hydrogen atom or aminopropyl group when R.sup.2 is represents aminopropyl group, or a salt thereof; and at least one N-alkyl polyamine compound represented by the following formula (II):R--?NH(CH.sub.2).sub.3 !.sub.n --NH.sub.2 (II), wherein R is a C.sub.8-22 saturated or unsaturated aliphatic hydrocarbon group and n is an integer from 2 to 4, or a salt thereof in an amount of 0.1 to 9 parts by weight to one part by weight of the compound (I).Type: GrantFiled: March 20, 1996Date of Patent: June 2, 1998Assignee: Katayama Chemical, Inc.Inventors: Yoshiharu Wakao, Toru Yasunaga
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Patent number: 5760092Abstract: Disclosed are allocolchinones, which are anti-mitotic agents. Allocolchinones bind to tubulin reversibly and are more effective at inhibiting microtubule formation than colchicine. 7-Acetamido-allocolchinone inhibits the growth of a number of tumor cell lines at concentrations about 100 times lower than colchicine. Also disclosed is a method of treating an individual with cancer by administering a composition which comprises a therapeutically effective amount of an allocolchinone which inhibits microtubule assembly. Administering a therapeutically effective amount of a composition which comprises an allocolchinone which inhibits microtubule assembly can also be used for treating inflammatory diseases, multiple sclerosis, primary biliary cirrhosis, Alzheimer's Disease and Behcet's Disease.Type: GrantFiled: March 11, 1996Date of Patent: June 2, 1998Assignee: Brandeis UniversityInventors: Serge M. Timasheff, Marina J. Gorbunoff, Bernardo Perez-Ramirez
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Patent number: 5719193Abstract: This invention relates to a method of potentiating cell-mediated immunity which comprises administering to a patient a cell-mediated immunity potentiating amount of a compound of the formula:RHN--Z--NH--(CH.sub.2).sub.m --NH--Z--NHRor a pharmaceutically acceptable salt thereof, wherein m is an integer 3 to 12, Z is a saturated C.sub.2 -C.sub.6 alkylene moiety of straight or branched chain configuration, each R group is independently H, a C.sub.1 -C.sub.6 saturated or unsaturated hydrocarbyl, or --(CH.sub.2).sub.x --(Ar)--X wherein X is H, C.sub.1 -C.sub.6 alkoxy, halogen, C.sub.1 -C.sub.4 alkyl, or --S(O).sub.x R.sub.1, x is an integer 0, 1 or 2, and R.sub.1 is C.sub.1 -C.sub.6 alkyl.Type: GrantFiled: April 14, 1995Date of Patent: February 17, 1998Assignee: Merrell Pharmaceuticals, Inc.Inventors: Terry L. Bowlin, Nellikunja J. Prakash
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Patent number: 5681837Abstract: A mosquito insecticidal composition for controlling the growth of mosquitos wherein the active agent is a polyamine having one of the formulae: ##STR1## wherein: R.sub.1 and R.sub.6 may be the same or different and are alkyl having from 1 to 12 carbon atoms or hydrocarbyl aralkyl having up to 12 carbon atoms;R.sub.2 -R.sub.5 may be the same or different and are H, R.sub.1 or R.sub.6 ;R.sub.7 is H, alkyl having from 1 to 12 carbon atoms, hydrocarbyl aryl or hydrocarbyl aralkyl, each having up to 12 carbon atoms;m is an integer from 3 to 6, inclusive;n is an integer from 3 to 6, inclusive; or(IV) a salt thereof with an acid and a carrier therefor.Type: GrantFiled: September 18, 1996Date of Patent: October 28, 1997Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron
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Patent number: 5679682Abstract: A method of controlling the growth of mosquitos comprising administering to the mosquitos a mosquito insecticidal effective amount of a compound having one of the formulae: ##STR1##R.sub.1 --N.sup.1 H--(CH.sub.2).sub.3 --N.sup.2 H--(CH.sub.2).sub.3 --N.sup.3 H--(CH.sub.2).sub.4 --N.sup.4 H--(CH.sub.2).sub.3 --N.sup.5 H--(CH.sub.2).sub.3 --N.sup.6 H--R.sub.6 (II);or ##STR2## wherein: R.sub.1 and R.sub.6 may be the same or different and are alkyl having from 1 to 12 carbon atoms or hydrocarbyl aralkyl having up to 12 carbon atoms;R.sub.2 -R.sub.5 may be the same or different and are H, R.sub.1 or R.sub.6 ;R.sub.7 is H, alkyl having from 1 to 12 carbon atoms, hydrocarbyl aryl or hydrocarbyl aralkyl, each having up to 12 carbon atoms;m is an integer from 3 to 6, inclusive;n is an integer from 3 to 6, inclusive; or (IV) a salt thereof with an acid and a carrier therefor.Type: GrantFiled: September 18, 1996Date of Patent: October 21, 1997Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron
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Patent number: 5677351Abstract: Polyamines having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are alkyl, aralkyl or aryl having up to 10 carbon atoms; anda and b may be the same or different and are integers from 1 to 8; or a salt thereof with a pharmaceutically acceptable acid. Anti-neoplastic, anti-diarrheal, anti-peristaltic, gastrointestinal anti-spasmodic, anti-viral, anti-retroviral, anti-psoriasis and insecticidal compositions comprising biologically effective amounts of the above-described amines and biologically acceptable carriers therefor are also disclosed, as well as methods of treatment, administration or application of biologically effective amounts of the polyamines of the invention. Also disclosed are methods for preparing the polyamines of the invention.Type: GrantFiled: June 7, 1995Date of Patent: October 14, 1997Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.
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Patent number: 5677352Abstract: Anti-diarrheal, anti-secretory, nitric oxide agonist, nitric oxide synthase activating or gastrointestinal anti-spasmodic compounds of the formula: ##STR1## wherein: R.sub.1 and R.sub.6 may be the same or different and are H, alkyl or aralkyl having from 1 to 12 carbon atoms;R.sub.2 -R.sub.5 may be the same or different and are H, R.sub.1 or R.sub.6 ;R.sub.7 is H, alkyl, aryl or aralkyl having from 1 to 12 carbon atoms;m is an integer from 3 to 6, inclusive; andn is an integer from 3 to 6, inclusive; or(IV) a salt thereof with a pharmaceutically acceptable acid; and a pharmaceutically acceptable carrier therefor. Methods of treatment utilizing the composition are also disclosed.Type: GrantFiled: June 7, 1995Date of Patent: October 14, 1997Assignee: University of Florida Research Foundation, Inc.Inventors: Raymond J. Bergeron, Jr., Charles A. Sninsky
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Patent number: 5656671Abstract: Polyamines having the formula: ##STR1## wherein R.sup.1 and R.sub.2 are alkyl, aralkyl or aryl having up to 10 carbon atoms; anda and b may be the same or different and are integers from 1 to 8; ora salt thereof with a pharmaceutically acceptable acid. Anti-neoplastic, anti-diarrheal, anti-peristaltic, gastrointestinal anti-spasmodic, anti-viral, anti-retroviral, anti-psoriasis and insecticidal compositions comprising biologically effective amounts of the above-described amines and biologically acceptable carriers therefor are also disclosed, as well as methods of treatment, administration or application of biologically effective amounts of the polyamines of the invention. Also disclosed are methods for preparing the polyamines of the invention.Type: GrantFiled: June 7, 1995Date of Patent: August 12, 1997Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.
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Patent number: 5654287Abstract: The present invention relates to a method of treating a patient suffering from a neoplastic disease state comprising administering to said patient an effective antineoplastic amount of N,N'-bis[3-(ethylamino)propyl]-1,7-heptanediamine in conjunctive therapy with an effective antineoplastic amount of a cytotoxic agent selected from the group consisting of an antineoplastic vinca alkaloid, an antineoplastic antibiotic, an antineoplastic antimetabolite and an antineoplastic platinum coordination complex, wherein a synergistic antineoplastic effect results.Type: GrantFiled: June 2, 1995Date of Patent: August 5, 1997Assignee: Merrell Phamaceuticals Inc.Inventors: Nellikunja J. Prakash, Terry L. Bowlin
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Patent number: 5646124Abstract: The present invention relates to a method of treating a patient suffering from a neoplastic disease state comprising administering to said patient an effective antineoplastic amount of N,N'-bis[3-(ethylamino)propyl]-1,7-heptanediamine in conjunctive therapy with an effective antineoplastic amount of a cytotoxic agent selected from the group consisting of an antineoplastic vinca alkaloid, an antineoplastic antibiotic, an antineoplastic antimetabolite and an antineoplastic platinum coordination complex, wherein a synergistic antineoplastic effect results.Type: GrantFiled: June 2, 1995Date of Patent: July 8, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Nellikunja J. Prakash, Terry L. Bowlin
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Patent number: 5635218Abstract: The present invention relates to a method of treating a patient suffering from a neoplastic disease state comprising administering to said patient an effective antineoplastic amount of N,N'-bis[3-(ethylamino)propyl]-1,7-heptanediamine in conjunctive therapy with an effective antineoplastic amount of a cytotoxic agent selected from the group consisting of an antineoplastic vinca alkaloid, an antineoplastic antibiotic, an antineoplastic antimetabolite and an antineoplastic platinum coordination complex, wherein a synergistic antineoplastic effect results.Type: GrantFiled: June 2, 1995Date of Patent: June 3, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Nellikunja J. Prakash, Terry L. Bowlin
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Patent number: 5627215Abstract: The invention relates to compounds of formula (I), R.sub.1 and R.sub.2, each independently of the other, are selected from lower alkyl that is unsubstituted or substituted by one or more fluorine atoms which are not linked to the carbon atom of R.sub.1 or R.sub.2 bonding the nitrogen; from lower alkenyl wherein the double bond does not originate from the carbon atom that is bonded to a nitrogen bonding R.sub.1 or R.sub.2 ; from lower alkynyl wherein the triple bond does not originate from the carbon atom that is bonded to a nitrogen bonding R.sub.1 or R.sub.2 ; from cycloalkyl; and from cycloalkyl-lower alkyl; with the proviso that not more than one of the two radicals R.sub.1 and R.sub.2 is methyl; or salts thereof. The mentioned compounds are pharmacologically active against disorders that are responsive to a recuction in intracellular polyamines, such as tumours or protozoal diseases.Type: GrantFiled: August 18, 1995Date of Patent: May 6, 1997Assignee: Ciba-Geigy CorporationInventors: Jorg Frei, Jaroslav Stanek
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Patent number: 5622995Abstract: A method is provided for controlling the proliferation of molluscs in target habitat by applying to the habitat a compound or mixture of compounds which are amines, ethoxylated amines, quaternary amines, ethoxylated quaternary amines and cyclic amines.Type: GrantFiled: August 15, 1994Date of Patent: April 22, 1997Assignee: Electric Power Research Institute, Inc.Inventors: Billy D. Fellers, Arthur J. Freedman, Thomas M. Laronge
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Patent number: 5614509Abstract: The use of NMDA receptor antagonists or their physiologically compatible salts for preventing the development of tolerance during the long-term treatment with benzodiazepine-receptor-binding active ingredients as well as the combination of new pharmaceutical agents with benzodiazepine-receptor-binding active ingredients is described.Type: GrantFiled: March 2, 1995Date of Patent: March 25, 1997Assignee: Schering AktiengesellschaftInventors: Lechoslaw Turski, Karin G. Steppuhn, Herbert Schneider, David N. Stephens
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Patent number: 5565021Abstract: The invention relates to a process for the treatment of water and of surfaces in contact with the said water in order to prevent the attachment and/or to remove and/or to control macroorganisms, in particular molluscs, on the said surfaces in contact with the water, in which process at least one biocidal and/or biostatic active product is employed which is injected into the water and/or applied to the said surfaces, according to which process the active product(s) used comprise(s) at least one polyamine of formula I:R.sub.1 -NH[(CH.sub.2).sub.3 -NH].sub.n -(CH.sub.2).sub.3 NH.sub.2(I)in which formula R.sub.1 is a C.sub.8 -C.sub.22 alkyl or alkenyl radical and at least one monoamine of formula II:R.sub.2 NH.sub.2 (II)in which formula R.sub.2 is a C.sub.8-C.sub.22 alkyl or alkenyl radical, and n is an integer between 0 and 3 (inclusive).The invention also relates to a composition to be injected into the water and to a paint for covering the surfaces in contact with the water.Type: GrantFiled: December 28, 1994Date of Patent: October 15, 1996Inventor: Antoine Vanlaer
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Patent number: 5561136Abstract: The present invention relates to a method of treating a patient suffering from a neoplastic disease state comprising administering to said patient an effective antineoplastic amount of N,N'-bis[3-(ethylamino)propyl]-1,7-heptanediamine in conjunctive therapy with an effective antineoplastic amount of a cytotoxic agent selected from the group consisting of an antineoplastic vinca alkaloid, an antineoplastic antibiotic, an antineoplastic antimetabolite and an antineoplastic platinum coordination complex, wherein a synergistic antineoplastic effect results.Type: GrantFiled: May 9, 1995Date of Patent: October 1, 1996Assignee: Merrell Pharmaceuticals Inc.Inventors: Nellikunja J. Prakash, Terry L. Bowlin
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Patent number: 5554656Abstract: The invention relates to a disinfectant concentrate which contains amine and alcohol wherein the alcohol component includes at least one glycol ether of limited miscibility with water and the amine component includes at least one secondary and/or tertiary alkyl amine free from hydroxyl groups. It also relates to a disinfectant producabile from the disinfectant concentrate, the use of the disinfectant concentrate and of the disinfectant as bactericide, in particular mycobactericide, fungicide or virucide.Type: GrantFiled: February 25, 1994Date of Patent: September 10, 1996Assignee: Reckitt & Colman Inc.Inventors: Bernd L ower, Heinz Eggensperger, Peter Goroncy-Bermes, Michael Mohr, Andreas Dettmann
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Patent number: 5541230Abstract: Therapeutic polyamines useful as a cancer chemotherapeutic agents, including molecules having a formula R.sub.1 --NH--(CH.sub.2).sub.x --NH --(CH.sub.2).sub.x --NH--(CH.sub.2).sub.y --NH--(CH.sub.2).sub.z --NH--R, wherein R.sub.1 and R.sub.2 are hydrocarbon chains having 1 to 5 carbons and w, x, y and z are integers of 1 to 10, are disclosed. One such molecule is N.sup.1, N.sup.19 -bis(ethylamino)-5,10,15-triazanonadecane, which is longer than spermine. This preferred compound may be used alone or in combination with other therapeutic agents, such as 1,3-bis(2-chloroethyl)-1-nitrosourea or cis-Pt.Type: GrantFiled: November 5, 1993Date of Patent: July 30, 1996Inventors: Hirak S. Basu, Burt Feuerstein, Laurence Marton, Keijiro Samejima
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Patent number: 5498522Abstract: Disclosed is a method that relates to the measurement of determinants related to the in-vivo induction of spermidine/spermine N.sup.1 -acetyltransferase (SSAT), subsequent to polyamine analog treatment (such as with a bis-ethyl spermine analog) of human malignant solid tumor types responsive to the polyamine analog. The method comprises the measurement of one or more SSAT-specific determinants that include SSAT enzyme activity, SSAT enzyme protein, and SSAT m-RNA transcripts. Alternatively, other determinants related to the SSAT induction may be measured. Such determinants include SSAT co-factor acetylCoenzyme A, and SSAT products N.sup.1 -acetylspermidine and N.sup.1 -acetylspermine. Measurements of these determinants may be useful as prognostic indicia and tumor response markers to evaluate the clinical effectiveness of anticancer agents comprising polyamine analogs.Type: GrantFiled: November 16, 1993Date of Patent: March 12, 1996Assignee: Health Research, Inc.Inventor: Carl W. Porter
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Patent number: 5494935Abstract: Several new powerful chelating agents, suitable for the removal of a variety of certain heavy metal ions from the body of a mammal by oral application, have been synthesized and tested. Structurally, these compounds are partially lipophilic polyaminocarboxylic acids (PACA). They were synthesized in non-aqueous media from triethylenetetramine (TT) by monoalkylation of a primary amino group, followed by exhaustive carboxymethylation of the remaining amino groups using ethylbromoacetate and subsequent alkaline hydrolysis of the ester. In contrast to their non-lipophilic counterparts EDTA and DTPA, compositions of the present inventions exhibit appreciable absorption from the intestine and, therefore, can be administered orally. By varying the length of the alkyl chain, the chelons can be directed primarily to selected target organs. In addition, the compounds can be modified to target particular absorbed heavy metals.Type: GrantFiled: April 3, 1995Date of Patent: February 27, 1996Assignee: University of Utah Research FoundationInventors: Scott C. Miller, Friedrich W. Bruenger
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Patent number: 5462970Abstract: Anti-diarrheal, anti-secretory, nitric oxide agonist, nitric oxide synthase activating or gastrointestinal anti-spasmodic compounds of the formula: ##STR1## wherein: R.sub.1 and R.sub.6 may be the same or different and are H, alkyl or aralkyl having from 1 to 12 carbon atoms;R.sub.2 -R.sub.5 may be the same or different and are H, R.sub.1 or R.sub.6 ;R.sub.7 is H, alkyl, aryl or aralkyl having from 1 to 12 carbon atoms;m is an integer from 3 to 6, inclusive; andn is an integer from 3 to 6, inclusive; or(IV) a salt thereof with a pharmaceutically acceptable acid; and a pharmaceutically acceptable carrier therefor. Methods of treatment utilizing the composition are also disclosed.Type: GrantFiled: January 3, 1995Date of Patent: October 31, 1995Assignee: University of Florida Research Foundation, Inc.Inventors: Raymond J. Bergeron, Jr., Charles A. Sninsky
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Patent number: 5455277Abstract: A mosquito insecticidal composition and method for controlling the growth of mosquitos employing a mosquito insecticidally effective amount of a compound having one of the formulae: ##STR1## wherein: R.sub.1 and R.sub.6 may be the same or different and are alkyl having from 1 to 12 carbon atoms or hydrocarbyl aralkyl having up to 12 carbon atoms;R.sub.2 -R.sub.5 may be the same or different and are H, R.sub.1 or R.sub.6 ;R.sub.7 is H, alkyl having from 1 to 12 carbon atoms, hydrocarbyl aryl or hydrocarbyl aralkyl each having up to 12 carbon atoms;m is an integer from 3 to 6, inclusive;n is an integer from 3 to 6, inclusive; or(IV) a salt thereof with an acid and a carrier therefor.Type: GrantFiled: December 8, 1993Date of Patent: October 3, 1995Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron
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Patent number: 5451608Abstract: Derivatives of 2-amino-1,2,3,4-tetrahydronaphthalene and their use in therapeutic field are described.The compounds are particularly useful in the treatment of arterial hypertension, cardiac decompensation and renal failure, in the treatment of peripheral arteriopathies and in cerebrovascular insufficiency.Type: GrantFiled: July 28, 1994Date of Patent: September 19, 1995Assignee: Zambon Group S.p.A.Inventors: Francesco Santangelo, Giorgio Bertolini, Cesare Casagrande, Francesco Marchini, Stefania Montanari, Claudio Semeraro
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Patent number: 5444093Abstract: Wood preservatives contain a copper salt, a polyamine and a fatty amine and are used for preserving wood from fungi and termites.Type: GrantFiled: November 3, 1993Date of Patent: August 22, 1995Assignee: Dr. Wolman GmbHInventors: Reimer Goettsche, Hans-Volker Borck
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Patent number: 5434145Abstract: The present invention relates to certain polyamine thiols which are useful as radioprotective agents.Type: GrantFiled: October 14, 1994Date of Patent: July 18, 1995Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Michael L. Edwards, Ronald D. Snyder
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Patent number: 5432202Abstract: Methods for regulating cation transport across cellular membranes possessing cation channels are provided. The cell membrane possessing a specific ion channel is exposed to a non-aromatic polyamine compound having a lysine- or arginine-based moiety (or a guanidine moiety) coupled to a straight chain polyamine.These polyamines as well as a method for regulating NMDA through a spermidine-like effect on NMDA receptors by exposing a cell membrane to selected polyamines are also provided.Type: GrantFiled: June 9, 1993Date of Patent: July 11, 1995Assignee: New York UniversityInventors: Bruce D. Cherksey, Rodolfo R. Llinas, Mutsuyuki Sugimori
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Patent number: 5403862Abstract: Several new powerful chelating agents, suitable for the removal of a variety of certain heavy metal ions from the body by oral application, have been synthesized and tested. Structurally, these compounds are partially lipophilic polyaminocarboxylic acids (PACA). They were synthesized in non-aqueous media from triethylenetetramine (TT) by monoalkylation of a primary amino group, followed by exhaustive carboxymethylation of the remaining amino groups using ethylbromoacetate and subsequent alkaline hydrolysis of the ester. Gel permeation chromatography of a mixture of the PACA and actinide elements have shown these substances to be strong chelating agents similar to EDTA or DTPA. In contrast to their non-lipophilic counterparts EDTA and DTPA, compositions of the present inventions exhibit appreciable absorption from the intestine and, therefore, can be administered orally. By varying the length of the alkyl chain, the chelons can be directed primarily to selected target organs.Type: GrantFiled: January 17, 1992Date of Patent: April 4, 1995Assignee: University of Utah Research FoundationInventors: Scott C. Miller, Friedrich W. Bruenger
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Patent number: 5399570Abstract: Aspartic acid derivatives of the formula ##STR1## in which X denotes, for example, ##STR2## and R denotes, for example, cyclohexylamino, have useful pharmacological properties.Type: GrantFiled: March 25, 1993Date of Patent: March 21, 1995Assignee: Cassella AktiengesellschaftInventors: Otmar Klingler, Gerhard Zoller, Melitta Just, Bernd Jablonka
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Patent number: 5393789Abstract: The invention relates to a disinfectant concentrate which includes amine and alcohol and is characterized in that the alcohol component includes at least one aromatic alcohol and the amine component includes at least one tertiary alkyl amine which is free of hydroxyl groups. It is also relates to a disinfectant which is preparable from the disinfectant concentrate, and to the use of the disinfectant concentrate or disinfectant as a bactericide, in particular a Mycobactericide, fungicide or virucide.Type: GrantFiled: January 29, 1993Date of Patent: February 28, 1995Assignee: Eastman Kodak CompanyInventors: Heinz Eggensperger, Lower Bernd, Michael Mohr, Peter Goroncy-Bermes, Wolfgang Beilfuss
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Patent number: 5322856Abstract: A fortified glutaraldehyde compound with and without dual synergistic phenols is provided for disinfection and sanitization. One formula consists of: glutaraldehyde; dual quaternary ammonium chloride (n-alkyl dimethylethylbenzyl ammonium chloride and n-alkyl dimethylbenzyl ammonium chloride); para tertiary amyl phenol; ortho phenyl phenol; citric or acetic acid; sodium citrate; isopropyl or ethyl alcohol; triethanol amine-HCl; and water in the following proportions: 25.00 to 42.00 grams; 25.00 grams; 1.00 gram; 1.00 gram; 0.50 grams; 0.25 grams; 14.00 grams; 1.00 gram; and 32.25 to 15.25 grams. The formula for environmentally protected uses consists of: glutaraldehyde; dual quaternary ammonium chloride (n-alkyl dimethylethylbenzyl ammonium chloride and n-alkyl dimethylbenzyl ammonium chloride); citric or acetic acid; sodium citrate; isopropyl or ethyl alcohol; triethanol amine-HCl; and water in the following proportions: 25.00 to 42.00 grams; 25.00 grams; 0.50 grams; 0.25 grams; 14.00 grams; 1.Type: GrantFiled: April 16, 1993Date of Patent: June 21, 1994Inventor: Howard Martin
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Patent number: 5276047Abstract: The invention relates to a liquid preparation containing 1,2-benzoisothiazoline-3-one (BIT) and amines and optionally containing additional solvents and common additives, and containing as amine one or more amines having the general formula ##STR1## wherein R represents a straight-chained or branched alkyl or alkylene radical having 10 to 14 C atoms; n+m has a value of 4 to 12 and neither n nor m can be zero. The liquid composition, in an amount of at least 0.05 to 0.3% (by weight), can be used in products which contain water or can be diluted with water such as dispersions of synthetic materials, emulsion paints, adhesives, paper-coating materials, textile softening agents, sizing agents, surfactants, detergents, cleaning and polishing agents, spinning baths, coolants or metal working fluids, leather auxiliaries, and silicone and bitumen emulsions, as agent against material destruction caused by microbes.Type: GrantFiled: January 28, 1993Date of Patent: January 4, 1994Assignee: Sterling Winthrop, Inc.Inventors: Heinz Eggensperger, Peter Oltmanns, Karl-Heinz Scheler, Karl-Heinz Diehl
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Patent number: 5276029Abstract: Wood preservatives contain a copper salt, a polyamine and a fatty amine and are used for preserving wood from fungi and termites.Type: GrantFiled: November 1, 1990Date of Patent: January 4, 1994Assignee: Dr. Wolman GmbHInventors: Reimer Goettsche, Hans-Volker Borck
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Patent number: 5187194Abstract: Wood preservatives which contain a mixture of an N-organyldiazeniumdioxy-metal salt and a complex-forming polymeric nitrogen compound are used for preserving wood.Type: GrantFiled: October 16, 1990Date of Patent: February 16, 1993Assignee: Dr. Wolman GmbHInventors: Reimer Goettsche, Wolfgang Reuther
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Patent number: 5186947Abstract: Water-soluble wood preservatives which contain mixtures of a metal compound, a metal-fixing acid and a complexing polymeric nitrogen compound, and methods for protecting wood with such mixtures.Type: GrantFiled: September 19, 1991Date of Patent: February 16, 1993Assignee: Dr. Wolman GmbHInventors: Reimer Goettsche, Wolfgang Reuther
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Patent number: 5135942Abstract: A fungicidal composition comprisingA) at least one of 1-(4-chlorophenoxy)-3,3-dimethyl-1-(1,2,4-triazol-1-yl)-batan-2-ol of the formula ##STR1## and 1-(4-phenyl-phenoxy)-3,3-dimethyl-1-(1,2,4-triazol-1-yl(butan-2-ol of the formula ##STR2## and B) at least one guanidated aliphatic polyamine of the formula ##STR3## in which R.sup.1 represents a branched or unbranched, divalent aliphatic hydrocarbon radical having 3 to 14 carbon atoms,R.sup.2 represents a branched or unbranched, divalent aliphatic hydrocarbon radical having 3 to 14 carbon atoms,X.sup.1, X.sup.2 and X.sup.3 independently of one another represent hydrogen or the radical of the formula ##STR4## and n represents integers from 0 to 16, it being possible for the divalent aliphatic hydrocarbon radicals which represent R.sup.2 to be different from one another if n represents numbers larger than 1, or their acid addition salts.Type: GrantFiled: January 10, 1991Date of Patent: August 4, 1992Assignee: Bayer AktiengesellschaftInventors: Stefan Dutzmann, Hans Scheinpflug, Dieter Berg, Wolfgang Kramer
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Patent number: 5126360Abstract: A fungicidal composition comprisingA) 1-(4-chlorophenyl)-4,4-dimethyl-3-(1,2,4-triazol-1-yl-methyl)-pentan-3-ol of the formula ##STR1## and B) at least one guanidated aliphatic polyamine of the formula ##STR2## in which R.sup.1 represents a branched or unbranched, divalent aliphatic hydrocarbon radical having 3 to 14 carbon atoms,R.sup.2 represents a branched or unbranched, divalent aliphatic hydrocarbon radical having 3 to 14 carbon atoms,X.sup.1, X.sup.2 and X.sup.3 independently of one another represent hydrogen or the radical of the formula ##STR3## and n represents integers from 0 to 16, it being possible for the divalent aliphatic hydrocarbon radicals which represents R.sup.2 to be different from one another if n represents numbers larger than 1, or their acid addition salts.Type: GrantFiled: January 10, 1991Date of Patent: June 30, 1992Assignee: Bayer AktiengesellschaftInventors: Stefan Dutzmann, Wilhelm Brandes, Dieter Berg, Graham Holmwood
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Patent number: 5109024Abstract: The present invention relates to certain novel polyamine compounds of the formula: ##STR1## wherein Z is a saturated (C.sub.2 -C.sub.6) alkylene moiety, each R group independently is hydrogen, methyl, ethyl, or n-propyl with the provisos that both R groups cannot be hydrogen and that R is hydrogen or methyl when Z is a branched chain alkylene; or a pharmaceutically acceptable acid addition salt thereof.Type: GrantFiled: February 8, 1991Date of Patent: April 28, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Nellikunja Prakash, David M. Stemerick, Michael L. Edwards, Terry L. Bowlin
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Patent number: 4935449Abstract: The importance of polyamines in biological systems is discussed as well as the implications of polyamines in the treatment of various diseases. Novel N-substituted-2,3-butadienyl tri- and tetra-aminoalkanes are disclosed as well as their use inthe treatment of diseases and the pharmaceutical compositions.Type: GrantFiled: August 4, 1988Date of Patent: June 19, 1990Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Philippe Bey, David M. Stemerick, Michael L. Edwards, Alan J. Bitonti
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Patent number: 4559362Abstract: This invention relates to an immunopotentiator or an immunopotentiating method using spermidine or its pharmacologically acceptable salt as an active ingredient.Type: GrantFiled: November 9, 1983Date of Patent: December 17, 1985Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Tomio Takeuchi, Masaaki Ishizuka
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Patent number: 4507321Abstract: Disclosed herein are compositions containing aliphatic di- and polyamine, or agmatine which are useful to regulate, i.e., stimulate or inhibit, epithelial cell growth. The compositions containing low concentrations of these compounds, by virtue of their epithelial cell growth stimulating activity, are useful in promoting wound healing, treating burns, treating ischemic, debubitus and peptic ulcers, plastic and reconstructive surgery, dermatological disorders, promoting autograft and homograft growth, stimulating organ and tissue regeneration in vitro and in vivo, as a component in defined (serum protein-free) media for cultured cells.Compositions containing these compounds in higher concentrations are useful in the inhibition of cell growth and are useful in the treatment of psoriasis and in retardation of fibrosis after injuries to the spinal cord and nervous system. Also disclosed are various methodologies for utilizing such compositions.Type: GrantFiled: February 17, 1982Date of Patent: March 26, 1985Assignee: The Research Foundation of State University of New YorkInventor: Ilene H. Raisfeld