Heavy Metal Or Aluminum Containing Patents (Class 540/465)
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Patent number: 5280117Abstract: A process is described for the preparation of a manganese complex catalyst having the formula: ##STR1## wherein Mn is manganese in the +4 oxidation state; R is a C.sub.1 -C.sub.20 radical selected from the group consisting of alkyl, cycloalkyl, aryl, benzyl and radical combinations thereof;at least two R radicals may also be connected to one another so as to form a bridging unit between two oxygens that coordinate with the manganese;L is a ligand selected from a C.sub.3 -C.sub.60 radical having at least 3 nitrogen atoms coordinating with the manganese; andY is an oxidatively-stable counterion;the process includes the steps of:(i) reacting in an nonaqueous alcoholic medium a manganese (II) salt with the ligand L to form a manganese coordinated substance, a counterion salt M.sub.z Y.sub.Type: GrantFiled: September 9, 1992Date of Patent: January 18, 1994Assignee: Lever Brothers Company, a Division of Conopco, Inc.Inventors: Judith L. Kerschner, Vikki Chin Quee-Smith
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Patent number: 5277895Abstract: Tetraazacyclododecane compounds of general formula I ##STR1## in which E and Q are defined herein and their salts with inorganic and/or organic bases, amino acids or amino acid amides are valuable pharmaceutical agents.Type: GrantFiled: November 8, 1991Date of Patent: January 11, 1994Assignee: Schering AktiengesellschaftInventors: Johannes Platzek, Heinz Gries, Hanns-Joachim Weinmann, Wolf-Rudiger Press, Hubert Vogler
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Patent number: 5274147Abstract: A process for preparing a dinuclear manganese complex of formula (A) ##STR1## wherein: Mn represents manganese in the III or IV oxidation state, each X is independently a co-ordinating or bridging species selected from H.sub.2 O, O.sub.2.sup.-, O.sup.2-, OH.sup.-, SH.sup.-, S.sup.2-,>S=O, Cl.sup.-, N.sub.3.sup.-, SCN.sup.-, N.sup.3-, RCOO.sup.-, NH.sub.2.sup.- and NR.sub.Type: GrantFiled: July 6, 1992Date of Patent: December 28, 1993Assignee: Lever Brothers Company, Division of Conopco, Inc.Inventors: Judith Kerschner, Jean H. Koek, Ronald P. Potman, Lodewijk Van der Wolf
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Patent number: 5271927Abstract: The conjugation of antibodies to a macrocyclic conjugate compound wherein the conjugate compound has the structure (I), wherein R.sup.1 is --(CH.sub.2).sub.p --R.sup.6 --CH.sub.2).sub.q -- where p and q are the same or different and are 0, 1 or 2, and --R.sup.6 -- is --((CH.sub.2).sub.n --, where n is 0 or 1, --NH--, --O--, --S-- or (II), R.sup.1 optionally being alkyl substituted, provided that neither p nor q is 0 unless R.sup.6 is --CH.sub.2 --; R.sup.2 are --CH.sub.2 CH.sub.2 -- or --CH.sub.2 CH.sub.2 CH.sub.2 --, optionally alkyl, alkoxyalkyl or hydroxyalkyl substituted; R.sup.3 are the same or different and are --H, alkyl, hydroxyalkyl, alkoxyalkyl, carboxyalkyl, carboxyalkyl ester, phosphate, sulphonate or phosphonate; R.sup.4 is one of the compounds of formula (III) optionally alkyl substituted, wherein R.sup.7 is --H, alkyl, hydroxyalkyl, or alkoxyalkyl provided that when R.sup.4 is (III d), R.sup.3 is not carboxyalkyl, R.sup.5 is a linker, and Ab is an antibody.Type: GrantFiled: March 18, 1993Date of Patent: December 21, 1993Assignee: Celltech LimitedInventors: David Parker, Thomas A. Millican
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Patent number: 5262526Abstract: A fluorescent compound, which is readily capable of forming a stable complex with a rare-earth metal ion having fluorescence with satisfactory intensity even in an aqueous system and long fluorescence lifetime when formed a complex with the rare-earth metal ion, a complex of the fluorescent compound and the rare-earth metal ion, and a labelled reagent made therefrom, together with a specific binding assay using said labelling agent.A fluorescent compound expressed by the following formula A, typically exemplified by 2,15-diaza[3,3](2,9)-1,10-phenanthrolinophane-N.sup.2,N.sup.15 -diacetic acid.Type: GrantFiled: December 20, 1991Date of Patent: November 16, 1993Assignees: Dojindo Laboratories, Mochida Pharmaceutical Co., Ltd.Inventors: Kazumi Sasamoto, Daikichi Horiguchi, Masahiro Nobuhara, Hiroshi Mochizuki
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Patent number: 5256779Abstract: A process is described for the preparation of a compound having the formula: ##STR1## wherein Mn is manganese in a III or IV oxidation state; X is independently selected from a coordinating or bridging species selected from the group consisting of:H.sub.2 O, O.sub.2.sup.2-, O.sub.2-, OH.sup.-, HO.sub.2.sup.-, SH.sup.-, S.sup.2-, SO, Cl.sup.-, N.sub.3.sup.-, SCN.sup.-, N.sup.3-, HCOO.sup.-, NH.sub.2.sup.- and NH.sub.3 ;L is an organic ligand that is at least a nine-membered ring wherein at least two nitrogen atoms form part of the ring and coordinate with the Mn;z is an integer ranging from -4 to +4;Y is a monovalent or multivalent counterion leading to charge neutrality selected from the group consisting of halides, sulphates, sulphonates, nitrates, boron and phosphorus salt counterions; andq is an integer from 1 to 4;the process comprising the steps of:(i) reacting in an aqueous medium a manganese (II) salt with the ligand L to form a manganese coordinated substance, a counterion salt M.sub.z Y.sub.Type: GrantFiled: June 18, 1992Date of Patent: October 26, 1993Assignee: Lever Brothers Company, Division of Conopco, Inc.Inventors: Judith L. Kerschner, Lisa DelPizzo
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Patent number: 5252720Type: GrantFiled: January 21, 1992Date of Patent: October 12, 1993Assignee: Board of Regents, The University of Texas SystemInventors: Jonathan L. Sessler, Gregory W. Hemmi, Tarak D. Mody
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Patent number: 5252733Abstract: Volatile .beta.-diketonate alkaline earth metal complexes useful in chemical vapor deposition (CVD) operations are formed using a cyclic ligand, such as a macrocyclic crown ether, to increase the degree of coordination and shielding around the individual metal ions in the diketonate structure. The resultant monomeric complexes readily volatize to give a chemically stable vapor.Type: GrantFiled: June 5, 1990Date of Patent: October 12, 1993Assignee: Air Products and Chemicals, Inc.Inventors: John A. T. Norman, Guido P. Pez
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Patent number: 5247075Abstract: Tri-aza macrocycles of formula (I), wherein m and n, which may be the same or different, is each zero or an integer 1, 2, or 3; p is zero or an integer 1 or 2; q is zero or an integer from 1 to 6 inclusive; R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, is each a hydrogen atom or an alkyl, alkoxyalkyl, --CO.sub.2 H, ---SO.sub.3 H, PO.sub.3 H.sub.2 or aryl group; L is a covalent bond or linker group; Z is a hydrogen atom or a reactive functional group, with the proviso that when L is a covalent bond Z is a reactive functional group; and metal complexes and/or salts thereof are described together with processes for their preparation and compositions containing them. The compounds are useful for imaging and in the treatment of abnormal cell disorders, such as in the treatment of tumours, and are particularly suitable for coupling to other molecules such as proteins for use in diagnosis and therapy.Type: GrantFiled: October 22, 1991Date of Patent: September 21, 1993Assignee: Celltech LimitedInventors: David Parker, Thomas A. Millican
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Patent number: 5247077Type: GrantFiled: March 31, 1992Date of Patent: September 21, 1993Assignee: Celltech LimitedInventors: David Parker, Michael A. W. Eaton
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Patent number: 5236695Abstract: Polyphosphonate ligands containing three or more phosphonate groups, combined with paramagnetic metal cations and administered in the form of pharmacologically acceptable salts, are useful as MRI contrast enhancement agents, which tend to localize in bone tissue without being conjugated to bone-specific biomolecules. Triazacyclononanes and tetraazacyclododecanes, with dihydroxyphosphorylmethyl or dihydroxyphosphorylethyl groups, optionally substituted at the methyl or ethyl bridges with alkyl, aryl, hydroxyl or amino groups, are particularly preferred.Type: GrantFiled: September 11, 1991Date of Patent: August 17, 1993Assignee: Concat, Ltd.Inventors: Harry S. Winchell, Joseph Y. Klein, Elliot D. Simhon, Rosa L. Cyjon, Ofer Klein, Haim Zaklad
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Patent number: 5217706Abstract: Novel magnetic resonance imaging agents comprise complexes of paramagnetic ions with hydrazide derivatives of polyaminocarboxylic acid chelating agents. These novel imaging agents are characterized by excellent NMR image-contrasting properties and by high solubilities in physiological solutions.A novel method of performing an NMR diagnostic procedure involves administering to a warm-blooded animal an effective amount of a complex as described above and then exposing the warm-blooded animal to an NMR imaging procedure, thereby imaging at least a portion of the body of the warm-blooded animal.Type: GrantFiled: June 3, 1992Date of Patent: June 8, 1993Assignee: Mallinckrodt Medical, Inc.Inventors: Raghavan Rajagopalan, Rebecca A. Wallace, Muthunadar P. Periasamy
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Patent number: 5198208Abstract: There are provided chelating agents particularly useful for the preparations of diagnostic and therapeutic agents for magnetic resonance imaging, scintigraphy, ultrasound imaging, radiotherapy and heavy metal detoxification, said agents being compounds of formula X--CHR.sub.1 --NZ--(CHR.sub.1).sub.n --A--(CHR.sub.1).sub.m --NZ--CHR.sub.1 --X wherein (each of the groups Z is a group --CHR.sub.1 X or the groups Z together are a group --(CHR.sub.1).sub.q --A'--(CHR.sub.1).sub.r --, where A' is an oxygen or sulphur atom or a group --N--Y; A is a group --N--Y or A--(CHR.sub.1).sub.m -- represents a carbon-nitrogen bond or, when the groups Z together are a group --(CHR.sub.1).sub.q --A'--(CHR.sub.1).sub.r --, A may also represent an oxygen or sulphur atom; each Y, which may be the same or different, is a group --(CHR.sub.1).sub.p --N(CHR.sub.1 X).sub.2 or a group --CHR.sub.1 X; each X, which may be the same or different, is a carboxyl group or a derivative thereof or a group R.sub.1 ; each R.sub.Type: GrantFiled: March 16, 1990Date of Patent: March 30, 1993Assignee: Nycomed Imaging ASInventors: Arne Berg, Torsten Almen, Jo Klaveness, Pal Rongved, Terje Thomassen
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Patent number: 5188816Abstract: The present invention relates to a method of using a polyazamacrocyclic compound or a salt thereof to measure intracellular metal ions formula ##STR1## where x is 2, 3 or a combination of p 2(s) and q 3(s) where p +q=y;y is 3 or 4;R is (CH.sub.2).sub.z P(=O)R.sup.1 R.sup.2;R.sup.1 is R.sup.3 or OR.sup.3 where R.sup.3 is alkyl, cycloalkyl or aryl;R.sup.2 is H, alkyl or ##STR2## where R.sup.4 is alkyl, cycloalkyl or aryl; and z is 1 to 3.Type: GrantFiled: November 26, 1991Date of Patent: February 23, 1993Assignee: Board of Regents, The University of Texas SystemInventors: A. Dean Sherry, Istvan Lazar, Erno Brucher, Ravichandran Ramasamy
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Patent number: 5180821Abstract: Cyclic tetrabenzimidazole, a yellowish, visually non-fluorescent substance, and its chelates, tautomers, ionization and oxidation forms, having utility as chelating agents, catalysts and electrooptic components.Type: GrantFiled: March 9, 1992Date of Patent: January 19, 1993Assignee: Moleculon Research CompanyInventors: Arthur S. Obermayer, James B. Hendrickson, Sajjat Hussoin
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Patent number: 5179120Abstract: A porphycene having the structure ##STR1## wherein each R.sup.1 is, independently, (a) --(CH.sub.2).sub.n --X, where n=1-4, X is OR.sup.2 and R.sup.2 is C.sub.1-6 alkyl, aralkyl or aryl; CN; OH; OSO.sub.2 R.sup.2 ; NH.sub.2 ; NHR.sup.2 ; NR.sub.2.sup.2 ; SH; SR.sup.2 ; S(O).sub.1-2 R.sup.2 ; COOH; CO.sub.2 R.sup.2 ; C(O)NH.sub.2 ; C(O)NHR.sup.2 ; C(O)NR.sub.2.sup.2 ; halogen; or CHO;(b) --(CH.sub.2).sub.m CH.dbd.CH.sub.2 where m is 0-2; or(c) --(CH.sub.2).sub.n --O--G where G is a mono- or oligosaccharide;(d) --(CH.sub.2).sub.2n --X, where X is an amino acid, oligopeptide covalently bonded by an ether-, ester- or amine-bond or --Y--(CH.sub.2).sub.n -porphycene.sup.2 (porphycene.sup.2 being a compound of the same structure and Y is a direct bond; --O--; or --CH.dbd.CH.sub.2); or(e) where one, two or three of the substituents R.sup.1 are C.sub.1-6 alkyl or aryl and the remaining substituents are as above under (a)-(d), and salts and metal complexes thereof.Type: GrantFiled: June 28, 1991Date of Patent: January 12, 1993Assignee: Cytopharm, Inc.Inventors: Emanuel Vogel, Clemens Richert, Thomas Benninghaus, Martin Muller, Alexander D. Cross
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Patent number: 5162509Abstract: The present invention involves a novel tripyrrole dimethine-derived "expanded porphyrin" (texaphyrin), the synthesis of such compounds, their analogs or derivatives and their uses. These expanded porphyrin-like macrocycles are efficient chelators of divalent and trivalent metal ions. Metal complexes of these compounds are active as photosensitizers for the generation of singlet oxygen and thus potentially for inactivation or destruction of human immunodeficiency virus (HIV-1), mononuclear or other cells infected with such virus and tumor cells as well. A variety of texaphyrin derivatives have been produced and many more are readily obtainable. Various metal (e.g., transition, main group, and lanthanide) complexes with the texaphyrin and texaphyrin derivatives of the present invention have unusual water solubility and stability which render them particularly useful. These metallotexaphyrin complexes have optical properties making them unique as compared to existing porphyrin-like or other macrocycles.Type: GrantFiled: June 18, 1990Date of Patent: November 10, 1992Assignee: Board of Regents, The University of Texas SystemInventors: Jonathan L. Sessler, Gregory W. Hemmi, Toshiaki Murai
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Patent number: 5162508Abstract: The invention relates to rare earth cryptates consisting of at least one rare earth salt complexed by a macropolycyclic compound corresponding to one of formulae I or II below, in which:the ring ##STR1## is the N.sub.2 O.sub.4 macrocycle, the N.sub.2 O.sub.3 macrocycle or a bis-bipyridine macrocycle;Y is a spacer arm or group which consists of a divalent organic radical selected from linear or branched C.sub.1 to C.sub.20 alkylene groups optionally containing one or more double bonds and/or optionally being interrupted by one or more heteroatoms such as oxygen, nitrogen, sulfur or phosphorus, or from C.sub.5 to C.sub.8 cycloalkylene groups or C.sub.6 to C.sub.Type: GrantFiled: July 26, 1991Date of Patent: November 10, 1992Assignee: Compagnie Oris IndustrieInventors: Jean-Marie Lehn, Mathis Gerard, Beatrice Alpha, Robert Deschenaux, Etienne Jolu
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Patent number: 5159065Abstract: The present invention involves, in addition to many unique substituted sapphyrins, a novel method for synthesizing sapphyrins with good efficiency and high yield. An improved 9-step synthesis of substituted sapphyrins, e.g., the two C.sub.2 symmetric sapphyrins, compounds 2 and 4 of FIG. 1C, is described herein. This synthesis involves as an important step the condensation between a tripyrrane diacid and a diformyl bipyrrole. The key tripyrrane component is prepared in three high-yield steps from readily available pyrrolic precursors and the bipyrrole portion is prepared in four steps from ethyl 3-methyl-4-methylpyrrole-2-carboxylate in roughly 33% yield overall.Type: GrantFiled: December 21, 1989Date of Patent: October 27, 1992Assignee: Board of Regents, The University of Texas SystemInventors: Jonathan L. Sessler, Michael J. Cyr
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Patent number: 5134238Abstract: Disclosed herein is a class of chiral copper-amine complexes of the formula R(L*) CuLi in which L* is selected from: ##STR1## In this formula, R is a transferable ligand, which can be alkyl, aryl or aralkyl. M is a metal ion such as Li, Na, K, Cs, Rb, Be, Mg and other metal ions from the first two columns of the periodic table. R.sub.1 is straight chain alkyl, R.sub.2 is aryl or substituted aryl and R.sub.3 and R.sub.4 form a heterocyclic ring or a substituted heterocyclic ring with 4 to 8 members including oxygen and sulfur.Such complexes react with .alpha.,.beta.-unsaturated ketones, aldehydes, esters and other carbonyl containing compounds such that R is transferred to the 3 position enantioselectively as shown below. ##STR2## Such complexes react with .alpha.,.beta.-unsaturated ketones in the presence of trialkysilyl halides to give silyl enol ether in which R is substituted in the 3 position as shown below.Type: GrantFiled: July 15, 1991Date of Patent: July 28, 1992Assignee: Brigham Young UniversityInventors: Bryant E. Rossiter, Masakatsu Eguchi
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Patent number: 5132409Abstract: Macrocyclic derivatives of 1,4,7,10-tetraazacyclododecane of general formula (I) hereinbelow, wherein A is a group of formula (II) hereinbelow, in which R is H or alkyl or optionally substituted benzyl or a H(OCH.sub.2 CH.sub.2).sub.1-4-, Me(OCH.sub.2 CH.sub.2).sub.1-4-, or Et(OCH.sub.2 CH.sub.2).sub.1-4- group, X or O--R.sub.1, in which R.sub.1 is H or alkyl, hydroxyalkyl, alkoxyalkyl, alkoxyhydroxyalkyl or a polyoxaalkyl group or X is --NR.sub.2 R.sub.3, in which R.sub.2 and R.sub.3 are H or alkyl, hydroxyalkyl, alkoxyalkyl or alkoxyhydroxyalkyl, and B.sub.1, B.sub.2 and B.sub.3 have the same meanings as A or are H or a group of formula (III) hereinbelow, in which R.sub.4 is H or alkyl, Y is a O--R.sub.5 group, wherein R.sub.5 is H or alkyl, hydroxyalkyl, alkoxyalkyl, alkoxyhydroxyalkyl or a polyoxaalkyl group, or Y is a --NR.sub.6 R.sub.7 group, wherein R.sub.6 and R.sub.Type: GrantFiled: November 27, 1989Date of Patent: July 21, 1992Assignee: Bracco Industria Chimica S.p.A.Inventors: Ernst Felder, Carlo Musu, Luciano Fumagalli, Fulvio Uggeri
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Patent number: 5087696Abstract: A conjugate compound has the structure (I), wherein R.sup.1 is --(CH.sub.2).sub.p --R.sup.6 --(CH.sub.2).sub.q -- where p and q are the same or different and are 0, 1 or 2, and --R.sup.6 -- is --(CH.sub.2).sub.n --, where n is 0 or 1, --NH--, --O--, --S-- or (II), R.sup.1 optionally being alkyl substituted, provided that neither p nor q is 0 unless R.sup.6 is --CH.sub.2 --; R.sup.2 are --CH.sub.2 CH.sub.2 -- or --CH.sub.2 CH.sub.2 CH.sub.2 --, optionally alkyl, alkoxyalkyl or hydroxyalkyl substituted; R.sup.3 are the same or different and are --H, alkyl, hydroxyalkyl, alkoxyalkyl, carboxyalkyl, carboxyalkyl ester, phosphate, sulphonate or phosphonate; R.sup.4 is one of the compounds of formula (III) optionally alkyl substituted, wherein R.sup.7 is --H, alkyl, hydroxyalkyl, or alkoxyalkyl provided that when R.sup.4 is (III d), R.sup.3 is not carboxyalkyl, R.sup.5 is a linker, and Ab is an antibody.Type: GrantFiled: December 14, 1987Date of Patent: February 11, 1992Assignee: Celltech LimitedInventors: David Parker, Thomas A. Millican
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Patent number: 4987227Abstract: A 13 or 14 member macrocyclic compound having the following ring nucleus: ##STR1##This work was supported by grants from the National Institutes of Health (GM-34841) and the National Science Foundation (CHE-8706616).Type: GrantFiled: February 23, 1990Date of Patent: January 22, 1991Assignee: The Research Foundation of State University of New YorkInventors: Cynthia Burrows, Heungsik Yoon, Thomas R. Wagler
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Patent number: 4983376Abstract: Compositions for the enhancement of NMR contrast are disclosed which include a complex of a paramagnetic metal selected from the group consisting of gadolinium, manganese, iron, and chromium, with one of a group of triazamacrocyclic ligands. Methods for using such compositions are also disclosed.Type: GrantFiled: December 28, 1988Date of Patent: January 8, 1991Assignee: Board of Regents, The University of Texas SystemInventor: A. Dean Sherry
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Patent number: 4935498Abstract: The present invention involves a novel tripyrrole dimethine-derived "expanded porphyrin" (texaphyrin), the synthesis of such compounds, their analogs or derivatives and their uses. These expanded porphyrin-like macrocycles are efficient chelators of divalent and trivalent metal ions. Metal complexes of these compounds are active as photosensitizers for the generation of singlet oxygen and thus potentially for inactivation or destruction of human immunodeficiency virus (HIV-1), mononuclear or other cells infected with such virus and tumor cells as well. A variety of texaphyrin derivatives have been produced and many more are readily obtainable. Various metal (e.g., transition, main group, and lanthanide) complexes with the texaphyrin and texaphyrin derivatives of the present invention have unusual water solubility and stability which render them particularly useful. These metallotexaphyrin complexes have optical properties making them unique as compared to existing porphyrin-like or other macrocycles.Type: GrantFiled: March 6, 1989Date of Patent: June 19, 1990Assignee: Board of Regents, The University of Texas SystemInventors: Jonathan L. Sessler, Gregory W. Hemmi, Toshiaki Murai
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Patent number: 4906754Abstract: Preparation of ethylene copolymers from ethylene and polar and/or non-polar comonomers in the presence of selected nickel-containing catalysts.Type: GrantFiled: September 1, 1987Date of Patent: March 6, 1990Assignee: E. I. Du Pont de Nemours and CompanyInventor: Ulrich Klabunde
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Patent number: 4902797Abstract: A compound of the formula (I): ##STR1## (wherein R is C.sub.1 -C.sub.6 alkyl, hydroxy, carboxy, C.sub.1 -C.sub.6 alkoxy, halogen or oxo; m is an integer from 2 to 7; X and Y each is chlorine or nit-rato ligand, or taken together form --OCOCH(R.sup.1)O--, OCOCOO--, ##STR2## R.sup.1 is hydrogen, C.sub.1 -C.sub.5 alkyl, hydroxymethyl, halogmethyl or phenyl; R.sup.2 is hydrogen or C.sub.1 -C.sub.5 alkyl; and n is an integer from 2 to 5), being useful as antitumor agents is provided.Type: GrantFiled: December 18, 1987Date of Patent: February 20, 1990Assignee: Shionogi & Co., Ltd.Inventors: Tetsushi Totani, Katsutoshi Aono, Yasuko Adachi
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Patent number: 4889931Abstract: The process of this invention for preparing Mn(II) chelate comprises forming the Mn(II) chelate by mixing manganese(II) oxide (insoluble) with an aqueous suspension comprising a molar equivalent or molar excess of the insoluble protonated chelating compound at a temperature of from 20.degree. to 50.degree. C. When the reaction is carried out with a protonated chelating agent in the absence of base, a precipitate of the protonated Mn(II) chelate is formed. A low osmolarity Mn(II) chelate solution can be formed from the precipitates by dissolving them in an aqueous solution of base. When the initial chelate forming reaction is carried out in a solution containing a molar equivalent or excess of sodium hydroxide, a low osmolarity solution of the Mn(II) chelate is directly formed with most chelating agents. Preferred chelating compounds for this process include DPDP, DTPA, DCTA, EDTP, DOTA, DOXA, DO3A and EDTA.Type: GrantFiled: September 27, 1988Date of Patent: December 26, 1989Assignee: Salutar, Inc.Inventors: Scott M. Rocklage, William P. Cacheris, Gene Jamieson
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Patent number: 4885363Abstract: Metal-chelating liquids having the formula ##STR1## wherein Y is oxygen or ##STR2## R.sub.Type: GrantFiled: December 23, 1987Date of Patent: December 5, 1989Assignee: E. R. Squibb & Sons, Inc.Inventors: Michael F. Tweedle, Glen T. Gaughan, James T. Hagan
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Patent number: 4851524Abstract: Thio-bis-(hydrocarbyl substituted diacid materials), such as thio-bis-(polyalkyl lactone acid) and/or their precursors, the adducts of sulfur chloride and unsaturated diacid materials, e.g., 4,8-bis-polyalkyl-4, 8-dichloro-6-thiaundecane-1,2,10,11-tetracarboxylic acid bis-anhydride and especially their dehydrochlorinated analogs, when treated with an amine preferably polyalkylene polyamines such as tetraethylene pentamine, directly or in the presence of a metal template reagent, yield aminated thio-bis-(alkyl lactone acid) and thio-bis-(hydrocarbyl diacid) materials or their metal complexes which can be characterized in part, as macrocyclic and/or macrocyclic-like amide and/or imide structures, are useful as stable additives in lubricating compositions, e.g., as varnish inhibiting dispersants and/or inhibitors for lubricating oils and fuels.Type: GrantFiled: November 27, 1985Date of Patent: July 25, 1989Assignee: Exxon Research and Engineering CompanyInventors: Stanley J. Brois, Antonio Gutierrez
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Patent number: 4734406Abstract: Compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and Y have the indicated meanings, their physiologically tolerated acid addition salts, and a process for the preparation of these compounds, are described. The compounds inhibit thromboxane synthetase and can thus be used as medicaments.Type: GrantFiled: March 11, 1986Date of Patent: March 29, 1988Assignee: Hoechst AktiengesellschaftInventors: Hans-Hermann Lau, Wilhelm Bartmann, Gerhard Beck, Gunther Wess
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Patent number: 4716157Abstract: This disclosure describes platinum complexes of heterocyclic-1,2-diamines which possess the property of inhibiting the growth of tumors in mammals.Type: GrantFiled: March 20, 1986Date of Patent: December 29, 1987Assignee: American Cyanamid CompanyInventors: Panayota Bitha, Ralph G. Child, Joseph J. Hlavka, Yang-I Lin
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Patent number: 4684638Abstract: The invention relates to new aqueous pharmaceutical compositions containing as active ingredient a pharmaceutically acceptable complex of a bis-indole compound with a bi- or multivalent metal ion in a therapeutically effective amount. The invention further relates to complexes formed between a bis-indole compound and a bi- or multivalent metal ion.According to another aspect of the invention there is provided a process for the preparation of a pharmaceutically acceptable metal complex of a bis-indole compound and optionally stable aqueous pharmaceutical compositions containing said metal complex, in which a solution of a bis-indole compound or a pharmaceutically acceptable salt thereof in an aqueous medium is reacted with a non-toxic water soluble salt of a bi- or multivalent metal capable of complexation, at a pH of 3.0 to 6.0, optionally in the presence of or followed by the addition of a conventional pharmaceutical carrier and/or further additive, or, if desired, the obtained complex is isolated.Type: GrantFiled: October 1, 1985Date of Patent: August 4, 1987Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Geza T. Nagy, Gabor Szepesi, Maria Gazdag, Zsofia Papp nee Sziklay, Kalman Burger
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Patent number: 4678667Abstract: A copper chelate conjugate which is stable in human serum. The conjugate includes the copper chelate of a cyclic tetraaza di-, tri-, or tetra-acetic acid, a linker attached at one linker end to a ring carbon of the chelate, and a biomolecule joined at the other end of the linker. The conjugate, or the linker-copper chelate compound used in forming the conjugate, are designed for use in diagnostic and therapeutic applications which involve Cu(II) localization via the systemic route.Type: GrantFiled: July 2, 1985Date of Patent: July 7, 1987Assignee: 501 Regents of the University of CaliforniaInventors: Claude F. Meares, Sally J. DeNardo, William C. Cole, Min K. Mol
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Patent number: 4657903Abstract: This invention relates to novel transition metal complexes of 2-acetyl- and -propionylpyridine thiosemicarbazones, their selenium analogs. These compounds are useful as antimalarial and antileukemic agents. Also disclosed are several synthetic procedures used to prepare the thiosemicarbazones and their selenium analogs.Type: GrantFiled: March 31, 1982Date of Patent: April 14, 1987Assignee: The United States of America as represented by the Secretary of the ArmyInventors: John P. Scovill, Daniel L. Klayman, Charles F. Franchino