The Hetero Ring Contains Plural Nitrogens Patents (Class 540/470)
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Patent number: 5627353Abstract: Spheres with a tetrahedral, octahedral and icosohedral geometry containing active compounds, wherein the spheres embrace the same volume as the fullerenes of the same symmetry, and are described by the formulas C.sub.360 N.sub.240 O.sub.24 U.sub.12, C.sub.1080 H.sub.300 N.sub.120 O.sub.24 U.sub.12, C.sub.144 N.sub.96 Cu.sub.14 and C.sub.432 H.sub.132 N.sub.48, their synthesis, the method of liberating the active compounds by irradiating the spheres to destroy the spheres such to release the active compounds, as well as possible uses for spheres filled with active compounds.Type: GrantFiled: December 14, 1993Date of Patent: May 6, 1997Assignee: Udo SchlagweinInventor: Franz D. Oeste
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Patent number: 5624948Abstract: 1-(2-benzimidazolyl)-1,5-diazacyclooctane compounds represented by the formula: ##STR1## wherein X represents a hydrogen atom or a halogen atom; Y represents a covalent bond, a straight- or branched-chain alkylene group having 1 to 6 carbon atoms, or a straight- or branched-chain alkenylene group having 2 to 6 carbon atoms; R represents a hydrogen atom, or a straight- or branched-chain alkyl group having 1 to 6 carbon atoms; and pharmaceutically acceptable salts thereof. The compounds represented above are novel potent and long-lasting histamine HI-receptor antagonist with less-topical irritation, and can be topically administered by inhalation for the treatment of bronchial asthma.Type: GrantFiled: November 14, 1995Date of Patent: April 29, 1997Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hidetoshi Isawa, Nobuko Yanagi, Yasuo Takehana, Den-ichi Momose, Masaaki Satoh, Yoshinori Nonaka
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Patent number: 5610308Abstract: A process is provided for preparing intermediates of the structure ##STR1## wherein Rpg is preferably .dbd.CHC.sub.6 H.sub.5 ; and P.G. is a protecting group CBZ or BOC, wherein a protected guanylpyrazole is reacted with an azacycloalkyl, azacycloalkenyl or azaheteroalkyl derivative (such as a piperidine derivative) in the presence of a DBU catalyst. The resulting intermediate may be used as a starting material for preparing thrombin inhibitors.Type: GrantFiled: May 18, 1995Date of Patent: March 11, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Sharon D. Real, David R. Kronenthal
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Patent number: 5608061Abstract: An improved process for preparing 1,4,8,11-tetraazacyclotetradecane comprising the tetratosylation of an acyclic tetraamine to obtain a tetratoluenesulfonamide compound in a first step, the cyclization of said sulfonamide compound to obtain tetratosyl cyclam in a second step, and the detosylation of tetratosyl cyclam in a third step followed by basification to obtain the desired 1,4,8,11-tetraazacyclotetradecane.Type: GrantFiled: August 2, 1995Date of Patent: March 4, 1997Assignee: Johnson Matthey PLCInventors: Lech Ciszewski, John Amedio, Prasad Kapa, Andrew Kucerovy, George T. Lee
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Patent number: 5606053Abstract: An improved process for preparing 1,1'-[1,4-phenylenebis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane comprising the selective functionalization of an acyclic tetraamine to obtain an acyclic ditosyl intermediate and an acyclic tritosyl intermediate in a first step, the independent dimerization/tosylation of the ditosyl intermediate and dimerization of the tritosyl intermediate to obtain a 1,4-phenylenebis-methylene bridged hexatosyl acyclic precursor in a second step, the cyclization of said precursor to obtain a hexatosyl cyclam dimer in a third step, and the detosylation of said cyclam dimer in a fourth step followed by basification to obtain the desired 1,1'-[1,4-phenylenebis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane.Type: GrantFiled: May 2, 1995Date of Patent: February 25, 1997Assignee: Johnson Matthey PLCInventors: Mahavir Prashad, Prasad Kapa
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Patent number: 5602168Abstract: Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently selected from halogen, hydroxy, lower alkyl, or lower alkoxy;Ar represents optionally substituted aryl or heteroarylZ represents carbon or nitrogen provided thatwhere Z is carbon, R.sub.11 represents hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy, or phenyl optionally substituted with one or two groups selected from hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy; andwhere Z is nitrogen, R.sub.11 represents an electron pair;R.sub.5 is hydrogen or lower alkyl;L and m represent integers;n is 0, or an integer;R.sub.12 and R.sub.Type: GrantFiled: June 5, 1995Date of Patent: February 11, 1997Assignee: Neurogen CorporationInventors: Xiao-shu He, Brian de Costa, Jan W. F. Wasley
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Patent number: 5578542Abstract: An acyclic alkane soluble anionic polymerization initiator includes a mixture of from about 90 to about 10 parts by weight of a lithio amine having the general formula A.sub.1 Li and from about 10 to about 90 parts by weight of at least one other lithio amine having the general formula A.sub.2 Li. A.sub.1 and A.sub.2 are selected from the dialkyl, alkyl, cycloalkyl and dicycloalkyl amine radicals and cyclic amine radicals. There is also provided a method of forming a mixture of anionic polymerization initiators, a functionalized polymer and a method of forming a functionalized polymer.Type: GrantFiled: March 30, 1994Date of Patent: November 26, 1996Assignee: Bridgestone CorporationInventors: David F. Lawson, James E. Hall, Yoichi Ozawa
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Patent number: 5571897Abstract: Lanthanide chelates which contain three heterocyclic rings covalently coupled to each other (either one 2,6-pyridylene and two five-membered unsaturated heterocyclic ring moieties or two 2,6-pyridylene and one five-membered unsaturated heterocyclic ring moiety) and two chelating groups so seated that they together chelate the same lanthanide ion even in aqueous solutions. These lanthanide chelates can optionally contain a reactive group for coupling to biologically active molecules. The new chelates are suitable for classical lanthanide chelate applications and are also useful as probes in time-resolved fluorescence microscopy, cytometry, multilabelling techniques and in process controls in industry.Type: GrantFiled: July 26, 1994Date of Patent: November 5, 1996Assignee: Wallac OyInventors: Harri Takalo, Veli-Matti Mukkala
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Patent number: 5554749Abstract: The present invention provides new and structurally diverse compositions comprising compounds of the general formula: ##STR1## Wherein U is --(CH.sub.2).sub.n X or --(CH.sub.2).sub.n NR.sub.1 (CH.sub.2)X; R.sub.1 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 hydroxyalkyl or C.sub.1 -C.sub.8 alkoxyalkyl; V is --(CH.sub.2).sub.n X, --(CH.sub.2).sub.n NR.sub.1 (CH.sub.2)X, hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 hydroxyalkyl or C.sub.1 -C.sub.8 alkoxyalkyl; V and R.sub.1 may jointly be --(CH.sub.2).sub.m -- to form a heterocyclic ring; X is --CO.sub.2 H, --PO.sub.3 H.sub.2, --SO.sub.3 H or --CONHOH; a, b, c, d, n and m may be the same or different and are from one to about ten, preferably from one to about three.Methods for imaging using compositions of the invention are also provided.Type: GrantFiled: January 14, 1994Date of Patent: September 10, 1996Assignee: Mallinckrodt Medical, Inc.Inventors: Rebacca A. Wallace, Dennis A. Moore
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Patent number: 5530122Abstract: A process for the isolation of sp.sup.3 reduced nonaromatic macrocyclic texaphyrin precursors, aromatic texaphyrin compounds and texaphyrin-metal complexes from aqueous salt solutions.Type: GrantFiled: August 23, 1994Date of Patent: June 25, 1996Assignee: Pharmacyclics, Inc.Inventors: William C. Dow, Joan F. Carvalho, Miguel Rosingana
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Patent number: 5504098Abstract: Disclosed are a benzothiazolesulfonamide derivative represented by the formula (I) or a pharmaceutically acceptable acid addition salt thereof ##STR1## wherein A represents a lower alkylene group which is unsubstituted or substituted; R.sup.1 represents a hydrogen atom or a lower alkyl group; each of R.sup.2 and R.sup.3 independently represents a hydrogen atom or a lower alkyl group, or R.sup.2 and R.sup.3 are bonded together to form a lower alkylene group which is unsubstituted or substituted; and R.sup.4 represents a hydrogen atom, a lower alkyl group, an amidino group, or a phenyl-substituted lower alkyl group, wherein the lower alkyl group is substituted or unsubstituted, and the phenyl group is unsubstituted or substituted with a lower alkyl group, a lower alkoxy group, a halogen atom or a methylenedioxy group;a method for preparing the same; and a pharmaceutical composition comprising the same.Type: GrantFiled: February 9, 1995Date of Patent: April 2, 1996Assignee: Asahi Kasei Kogyo Kabushiki KaishaInventors: Akiro Kajihara, Masahiko Tsuchiya
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Patent number: 5484772Abstract: This invention relates to L-arginine aldehyde derivatives, pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents.Type: GrantFiled: October 5, 1994Date of Patent: January 16, 1996Assignee: Eli Lilly and CompanyInventors: Daniel J. Sall, Robert T. Shuman, Gerald F. Smith, Michael R. Wiley
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Patent number: 5457184Abstract: The invention relates to macrocyclic rare earth complexes which consist of at least one rare earth salt complexed by a macrocyclic compound of formula (I): ##STR1## in which: the bivalent radicals A, B, C and D, which are identical or different, are hydrocarbon chains optionally containing one or more heteroatoms, at least one of said radicals containing at least one molecular unit or essentially consisting of a molecular unit possessing a triplet energy greater than the energy of the emission level of the complexed rare earth ion, at least one of said radicals consisting of a substituted or unsubstituted nitrogen-containing heterocyclic system in which at least one of the nitrogen atoms carries an oxy group, and it being possible for one of the radicals C or D not to exist; andX.sub.1 and X.sub.2, which are identical or different, are hydrogen or a hydrocarbon chain (CH.sub.2).sub.Type: GrantFiled: February 25, 1994Date of Patent: October 10, 1995Assignee: Cis Bio InternationalInventors: Jean-Marie Lehn, Christine O. Roth, Gerard Mathis
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Patent number: 5457098Abstract: There are disclosed preparation and compounds of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or lower alkyl or taken together are a --CH.sub.2 -- group to form a cyclopropane ring.X is ##STR2## wherein R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are hydrogen or alkyl,p and q are independently either 0 or 1;R.sup.3 is alkyl, alkenyl, cycloalkyl, alkoxy, thiopyridyl, adamantyl, --NR.sup.9 R.sup.10 or --Ar--NR.sup.9 R.sup.10 whereinR.sup.9 and R.sup.10 are hydrogen or alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, adamantyl, aryl, benzyl, diphenylmethyl, norbornyl, or taken together with the nitrogen to form 4 to 8 atom heterocyclic group, ##STR3## optionally substituted with alkyl groups; Ar is aromaticR.sup.4 is hydrogen or methyl;Z is --O--, --NH--, --N(lower alkyl), --S--, --SO--, --SO.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, CO, CO.sub.2, O.sub.2 C, --N.dbd.N--, --CH.dbd.N--, or --N.dbd.CH--,and n and m are 0, 1 or 2.Type: GrantFiled: January 28, 1994Date of Patent: October 10, 1995Assignee: Glaxo Inc.Inventors: Stephen V. Frye, David Middlemiss, Francis G. Fang
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Patent number: 5453220Abstract: Calixarene-based, noncentrosymmetric transition metal complexes that exhibit large second order nonlinear optical and related electro-optical properties are provided, as are materials and devices comprising the same.Type: GrantFiled: January 29, 1993Date of Patent: September 26, 1995Assignee: The Trustees of the University of PennsylvaniaInventors: Timothy M. Swager, Bing Xu
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Patent number: 5438133Abstract: Cyclodextrin catenanes capable of forming inclusion complexes and a method of preparing them are disclosed. The catenanes comprise one or two per-2,6- di-O-alkyl-.beta.-cyclodextrin macrocycles wherein each per-2,6-di-O-alkyl-.beta.-cyclodextrin macrocycle is interpenetrated by another macrocycle. Such modified cyclodextrins may be used for the electrochemical and optical sensing of small organic molecules, especially small aromatic molecules.Type: GrantFiled: January 27, 1994Date of Patent: August 1, 1995Assignee: Eastman Kodak CompanyInventors: Christopher P. Moore, Trevor J. Wear, James F. Stoddart, Dominique Armspach
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Patent number: 5428155Abstract: The pH controlled selectivity of the sulfomethylation reaction is used to prepare a series of di-, tri-, tetra- and hexaazacyclomacrocycles with specified patterns of pendent side-chain chelating groups. The prepared mono and diacetic acid derivatives, together with monomethylenephosphonate and monomethylenephosphinate derivatives of [12]aneN4, [12]aneN3 and [9]aneN3, make these types of ligands easily available by a synthetic pathway that avoids the use of protective groups. The invention thus comprises a variety of compounds, methods and uses characterized by relatively high synthetic yields of polyazamacrocyclic ligands exhibiting a wide and predictable choice of metal ion binding constants water and lipid solubilities by reason of their substituent pendent groups.Type: GrantFiled: May 27, 1994Date of Patent: June 27, 1995Assignee: Board of Regents, The University of Texas SystemInventors: A. Dean Sherry, Jeroen van Westrenen
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Patent number: 5389630Abstract: Diamine compounds of formula (I) or an addition salt thereof are provided: ##STR1## These compounds have an excellent cerebral protective action, are very safe, and exhibit a strong action when orally administered, and therefore, medicines containing such compounds are effective for treating disorders caused by cerebral hemorrhage, cerebral infarction, subarachnoid hemorrhage, transient ischemic attack, cerebrovascular disorders and the like, or preventing progress of such disorders.Type: GrantFiled: January 22, 1993Date of Patent: February 14, 1995Assignee: Kowa Co., Ltd.Inventors: Seiichi Sato, Kiyoshi Kawamura, Yoshio Takahashi, Koichiro Watanabe, Sadahiro Shimizu, Tomio Ohta
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Patent number: 5378839Abstract: There are provided 1-(substituted)thioalkylpyrrole compounds of formula I ##STR1## the use thereof for the control of insect, acarid and mollusk pests and methods and compositions for the protection of crops from the ravages of said pests.Type: GrantFiled: January 26, 1994Date of Patent: January 3, 1995Assignee: American Cyanamid CompanyInventors: David G. Kuhn, Venkataraman Kameswaran
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Patent number: 5364868Abstract: Amino-substituted benzoylguanidines, process for their preparation, their use as a medicament and medicament containing themBenzoylguanidines of the formula I ##STR1## are described in which R(1) or R(2) is an amino group --NR(3)R(4), where R(3) and R(4) are H or (cyclo)alkyl or R(3) is phenyl-(CH.sub.2).sub.p -- where p=0, 1, 2, 3 or 4, or phenyl, or R(3) and R(4) can also together be a methylene chain, and in which the other substituent R(1) or R(2) in each case is H, F, Cl, alkyl, alkoxy, CF.sub.3, C.sub.m F.sub.2m+1 --CH.sub.2 --, benzyl or phenoxy, and their pharmaceutically tolerable salts.The compounds according to the invention have very good antiarrhythmic properties, as occur, for example, in the case of oxygen deficiency symptoms.Type: GrantFiled: February 11, 1993Date of Patent: November 15, 1994Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Dieter Mania, Hans-Jochen Lang, Wolfgang Scholz, Wolfgang Linz, Udo Albus
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Patent number: 5354507Abstract: Compounds of general formula ##STR1## wherein: R is a linear or branched C.sub.1 -C.sub.20 alkyl radical, m is either 0 or 1; n has a value of from 1 to 10, are corrosion inhibitors, suitable for inhibiting the general corrosion and the stress brittlening caused by hydrogen sulfide (SSC), in an acidic environment, in the presence, or absence of carbon dioxide, of medium-and high-strength manganese steels and low-alloy steels, commonly used in petrochemical facilities and in bore drilling, transport and processing systems for natural gas or petroleum.Type: GrantFiled: January 21, 1993Date of Patent: October 11, 1994Assignee: Eniricerche S.p.AInventors: Viviana De Malde, Luigi Rivola, Arnaldo Roggero, Alberto Gandini
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Patent number: 5354761Abstract: Compounds of formula I ##STR1## wherein Y, Z, S, S', m, n and R.sub.1 -R.sub.4 are as defined in the description, have valuable pharmaceutical properties and are effective especially against protozoal infections. They are prepared in a manner known per se.Type: GrantFiled: June 1, 1993Date of Patent: October 11, 1994Assignee: Ciba-Geigy Corp.Inventors: Jaroslav Stanek, Giorgio Caravatti, Hans-Georg Capraro, Jorg Frei
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Patent number: 5346907Abstract: Analogs of CCK-tetrapeptides, which analogs have the formula ##STR1## wherein A, B, D, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are specifically defined, having activity as CCK antagonists, useful in the treatment or prevention of disorders of the gastrointestinal, central nervous, appetite regulating or pain regulating systems.Type: GrantFiled: February 16, 1993Date of Patent: September 13, 1994Assignee: Abbott LaboratoriesInventors: James F. Kerwin, Jr., Mark W. Holladay, Michael J. Bennett
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Patent number: 5342947Abstract: The present invention relates to the synthesis of water soluble, camptothecin derivatives of formula (I), ##STR1## wherein: n represents the integer 1 or 2;R.sup.1 represents independently, hydrogen, lower alkyl, (C.sub.3-7)cycloalkyl, (C.sub.3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy lower alkyl; andR.sup.2 represents hydrogen andthe pharmaceutically acceptable salts thereof.Type: GrantFiled: October 9, 1992Date of Patent: August 30, 1994Assignee: Glaxo Inc.Inventors: Karen Lackey, Daniel D. Sternbach
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Patent number: 5338861Abstract: Substituted lactams of the formula ##STR1## can be prepared from lactam N-carboxylates or lactim O-carboxylates of the formulae ##STR2## by thermal or mixed thermal and catalysed CO.sub.2 elimination at 80.degree.-450.degree. C. Lactams substituted on the N atom by aliphatic groups such as those produced herein are useful as industrial aprotic solvents.Type: GrantFiled: July 24, 1992Date of Patent: August 16, 1994Assignee: Bayer AktiengesellschaftInventors: Artur Botta, Hans-Josef Buysch, Otto Immel, Lothar Puppe
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Patent number: 5332822Abstract: Sulfonamide thrombin inhibitors are provided which have the structure ##STR1## including all stereoisomers thereof, wherein X is S or --CH.sub.2 --; m is 0, 1 or 2 when X is --S-- or m is 0 when X is --CH.sub.2 --; n is 1, 2 or 3; R.sup.1 and R.sup.2 are independently H, lower alkyl, cyclo-alkyl, aryl, heteroaryl or heteroarylalkyl, or R.sup.1 and R.sup.2 can be taken together with the N atom to which they are attached to form a 5- to 8-membered ring which may optionally contain an additional N, O or S atom in the ring; R.sup.3 is heteroaryl; and R.sup.4 is alkyl, cycloalkyl, aryl, heteroaryl, quinolinyl or tetrahydroquinolinyl, and pharmaceutically acceptable salts thereof.Type: GrantFiled: December 24, 1992Date of Patent: July 26, 1994Assignee: Bristol-Myers Squibb CompanyInventor: Raj N. Misra
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Patent number: 5326744Abstract: Glycol aldehyde and lactic acid derivatives and their sulfur analogs of the formula I ##STR1## where R.sup.1 to R.sup.3 have the meanings given in the specification, X is oxygen, sulfur or a single bond, and Y is a C.sub.2 -C.sub.4 -alkylene or C.sub.2 -C.sub.4 -alkenylene chain where in each case a methylene group may be substituted by an oxo group (.dbd.O), environmentally compatible salts of the compounds I, methods of preparing the compounds I, and their use as herbicides.Type: GrantFiled: December 21, 1992Date of Patent: July 5, 1994Assignee: BASF AktiengesellschaftInventors: Joachim Rheinheimer, Ernst Baumann, Uwe J. Vogelbacher, Thomas Saupe, Matthias Bratz, Norbert Meyer, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter, Uwe Kardorff
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Patent number: 5300640Abstract: A novel herbicidal pyrimidine derivative represented by the formula ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y.sup.1, Y.sup.2, Y.sup.3, X and Z are as defined herein.Type: GrantFiled: December 19, 1991Date of Patent: April 5, 1994Assignee: Sumitomo Chemical Company, LimitedInventors: Mitsumori Hiratsuka, Naonori Hirata, Kazuo Saito, Hideyuki Shibata
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Patent number: 5288718Abstract: Pharmaceutical composition for decorporating radioactive isotopes from living organisms comprising as active agent a product prepared by reacting 1,4,10,17-tetraoxa-7,16-diazacyclooctadecane with 2-bromomalonic acid disodium salt.Type: GrantFiled: June 21, 1993Date of Patent: February 22, 1994Assignees: Orszagos "Frederic Joliot-Curie" Sugarbiologiai es Sugaregeszsegugyi Kutato Intezet, Agromen Agrarmenedzseri Kft, Magyar Kulkereskedelmi Bank Rt.Inventors: Laszlo Varga, Mihaly Torocsik, Laszlo B. Sztanyik, Erno Brucher, Jozsef Emri, Bela Gyori
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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: 5252567Abstract: This invention concerns compounds of the formula I: ##STR1## wherein R.sup.1 is (1-10C)alkyl, (3-8C)cycloalkyl, (3-8C)cycloalkyl-(1-4C)-alkyl, phenyl or phenyl(1-4C)alkyl, the phenyl moiety of the latter two optionally bearing one or more substituents; R.sup.2 is hydrogen, (1-4C)alkyl, amino or (1-4C)alkylamino; R.sup.6 is (1-4C)alkyl, amino or (1-4C)alkylamino; Q is a group of formula II, in which case R.sup.3 and R.sup.4 are independently hydrogen, (1-4C)alkyl, phenyl or benzyl the phenyl moiety of the latter two optionally bearing one or two substituents; R.sup.5 is hydrogen, (1-4C)alkyl or (2-4C)alkenyl; A and B are independently ethylene or trimethylene; Z is a direct bond between A and B, or an oxy, thio, carbonyl, methylene, ethylenedioxymethylene, ethylidene, or isopropylidene link, or Z is a group of the formula .dbd.N.Type: GrantFiled: December 18, 1990Date of Patent: October 12, 1993Assignee: Imperial Chemical Industries PLCInventors: Stuart D. Mills, Rodney B. Hargreaves, Bernard J. McLoughlin
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Patent number: 5245026Abstract: The present invention provides linear, cyclic and trifurcate tri- and tetramine backbone multidentate chelating agents based on the 8-hydroxyquinoline chelating unit. The chelating agents may optionally be substituted with a substrate reactive moiety and antibody-metal ion conjugates may be produced for in vivo diagnostic and therapeutic methods.Type: GrantFiled: May 21, 1991Date of Patent: September 14, 1993Assignees: Abbott Laboratories, Tobishi Yakuhin Kogyo Kabushiki KaishaInventors: David K. Johnson, Steven J. Kline
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Patent number: 5239070Abstract: There are provided alkyl esters of 5-heterocyclic-pyridine-2,3-dicarboxylic acids useful as intermediates for the preparation of highly effective 5-heterocyclic-2-(2-imidazolin-2-yl)pyridine herbicidal agents and methods for the preparation thereof.Type: GrantFiled: June 11, 1991Date of Patent: August 24, 1993Assignee: American Cyanamid CompanyInventor: John M. Finn
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Patent number: 5196535Abstract: Piperidinyl, pyrrolidinyl, azepinyl and piperazinyl pyridazines of formula ##STR1## wherein one or two carbon atoms of the ##STR2## moiety may be substituted with C.sub.1-4 alkyl, C.sub.1-4 alkyloxy or two carbon atoms of the CH.sub.2 groups of said moiety may be bridged with a C.sub.2-4 alkanediyl radical;X represents CH or N; R.sup.1 represents hydrogen, C.sub.1-4 alkyl, halo, hydroxy, trifluoromethyl, cyano, C.sub.1-4 alkyloxy, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulfinyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkylcarbonyl or aryl; R.sup.2 and R.sup.3 each independently represent hydrogen or C.sub.1-4 alkyl; Alk represents C.sub.1-4 alkanediyl; R.sup.4 and R.sup.5 each independently represent hydrogen, C.sub.1-4 alkyl or halo; andHet represents ##STR3## the addition salts and stereochemically isomeric forms thereof, said compounds having antipicornaviral activity.Type: GrantFiled: November 8, 1991Date of Patent: March 23, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Raymond A. Stokbroekx, Marcel G. M. Luyckx, Gilbert A. J. Grauwels, Cyriel A. M. Van der Eycken
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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: 5135563Abstract: The present invention relates to a pyrimidine derivative having the formula ##STR1## (wherein the variables are defined in the full text of the patent), a method for producing the same, and its use as a herbicide.Type: GrantFiled: July 5, 1991Date of Patent: August 4, 1992Assignee: Sumitomo Chemical Company, LimitedInventors: Mitsunori Hiratsuka, Naonori Hirata, Kazuo Saitoh, Hideyuki Shibata
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Patent number: 5125957Abstract: A pyrimidine derivative represented by the formula ##STR1## wherein the variables are defined below in the specification, and their production and herbicidal activities are described.Type: GrantFiled: October 24, 1990Date of Patent: June 30, 1992Assignee: Sumitomo Chemical Company, LimitedInventors: Mitsunori Hiratsuka, Naonori Hirata, Kazuo Saito, Hideyuki Shibata
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Patent number: 5089175Abstract: Hydroxyalkane carboxylic acid derivatives of general formula I ##STR1## in which n means the numbers 7 to 18,R.sub.1 represents a hydrogen atom or an acyl group with a maximum of 16 carbon atoms, andoptionally an alkylene group with 4 to 8 carbon atoms interrupted by an oxygen atom or a nitrogen atom, are useful for the production of pharmaceutical agents for local treatment of diseases of the skin and mucous membranes.Type: GrantFiled: February 16, 1990Date of Patent: February 18, 1992Assignee: Schering AktiengesellschaftInventors: Christopher G. Earnshaw, Gerald Kirsch, Petra Rach, Ruth Thieroff-Ekerdt, Michael Topert
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Patent number: 5089471Abstract: Non-peptidyl compounds characterized generally as .beta.-aminoacyl aminodiol carbamates are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: October 1, 1987Date of Patent: February 18, 1992Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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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: 5073556Abstract: Compounds of formula (I): ##STR1## (in which: R.sup.1 represents fluorinated methoxy; R.sup.2 represents a nitrogen-containing heterocyclic group and R.sup.3 represents hydrogen or amino) and pharmaceutically acceptable salts, esters and amides thereof are valuable antibacterial agents, which may be prepared by reacting a compound similar to that of formula (I) but in which R.sup.2 is replaced by a halogen atom with a compound providing the required group R.sup.2.Type: GrantFiled: February 22, 1991Date of Patent: December 17, 1991Assignees: Sankyo Company Limited, Ube Industries LimitedInventors: Masayuki Iwata, Tomio Kimura, Teruhiko Inoue, Yoshimi Fujihara, Tetsushi Katsube
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Patent number: 5041545Abstract: Hydrazide functionalized 2-hydroxybenzophenone ultraviolet light and heat stabilizers and derivatives are disclosed having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, Z, all substituents thereof, and n are set forth in the Summary of the Invention. Y--N(R.sup.6)--Z is the hydrazide or derivative group and --X--R.sup.5 -- links the hydrazide group to an aromatic nucleus of the optionally substituted benzophenone group. Derivatives are, for example, acyl hydrazides, diacyl hydrazides (including imides), hydrazones and alkyl hydrazides. The compounds are useful as ultraviolet light absorbers and heat stabilizers for plastics.Type: GrantFiled: April 6, 1989Date of Patent: August 20, 1991Assignee: Atochem North America, Inc.Inventor: Terry N. Myers
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Patent number: 5030631Abstract: Novel tricyclic arylsulfonamides useful for treating hypertension and bronchoconstiction, as well as to their pharmaceutical compositions and methods for using the same.Type: GrantFiled: November 27, 1989Date of Patent: July 9, 1991Assignee: Schering CorporationInventor: Barr E. Bauer
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Patent number: 5021567Abstract: The present invention provides linear, cyclic and trifurcate tri- and tetramine backbone multidentate chelating agents based on the 8-hydroxyquinoline chelating unit. The chelating agents may optionally be substituted with a substate reactive moiety and antibody-metal ion conjugates may be produced for in vivo diagnostic and therapeutic methods.Type: GrantFiled: September 24, 1987Date of Patent: June 4, 1991Assignee: Abbott LaboratoriesInventors: David K. Johnson, Steven J. Kline
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Patent number: 5017573Abstract: An indazole-3-carboxylic acid derivative represented by the following general formula (I) or its physiologically acceptable acid addition salt or quaternary ammonium salt, ##STR1## wherein Y represents --NH-- or --O--; R.sub.1 and R.sub.2 are identical or different and each represents a hydrogen atom, a lower alkyl group, a substituted lower alkyl group, a cycloalkyl group, a lower alkenyl group, a cycloalkenyl group, a lower alkynyl group, an unsubstituted or substituted aryl-lower alkyl group, a lower alkoxycarbonyl group, an unsubstituted or substituted aralkyloxycarbonyl group or an acyl group, or R.sub.1 and R.sub.2, taken together, form a lower alkylene group; R.sub.3 represents a hydrogen atom, a lower alkyl group, or a phenyl group; R.sub.Type: GrantFiled: July 25, 1989Date of Patent: May 21, 1991Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Tatsuya Kon, Shiro Kato, Toshiya Morie, Tadahiko Karasawa, Naoyuki Yoshida
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Patent number: 5015284Abstract: Compounds of the formula I, their stereoisomers or their salts ##STR1## wherein A denotes >C(R.sup.4).sub.2 or >C.dbd.C(R.sup.5).sub.2 ; R.sup.1 denotes H, an optionally substituted aliphatic or cycloaliphatic radical, forfuryl, tetrahydrofurfuryl or (substituted) phenyl; R.sup.2 denotes H, alkyl, alkenyl, alkynyl or alkoxy; R.sup.3 denotes a radical of the formulae ##STR2## X denotes O, S or NR.sup.12 and Y denotes O or S, possess excellent herbicidal and plant-growth regulating properties.Type: GrantFiled: April 6, 1989Date of Patent: May 14, 1991Assignee: Hoechst AktiengesellschaftInventors: Lothar Willms, Klaus Bauer, Hermann Bieringer, Helmut Burstell
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Patent number: 5013846Abstract: Disclosed is a high yield process for preparing substituted imidazoline fabric conditioning compounds. In this process, a fatty acylating agent, e.g., fatty acid, is reacted with a specific polyamine, and the product of this reaction is reacted with an esterifying agent, both reactions being conducted under specifically-defined conditions. Aqueous dispersions containing these substituted imidazoline compounds possess desirable storage stability, viscosity, and fabric conditioning properties.Type: GrantFiled: December 21, 1988Date of Patent: May 7, 1991Assignee: The Procter & Gamble CompanyInventor: Darlene R. Walley
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Patent number: 4988723Abstract: Benzopyran derivatives of formula (I) wherein the substituents are as defined herein are provided. The compounds possess vasodilating activity and are useful in the treatment of hypertension. Pharmaceutical compositions and methods of treating hypertension are also provided.Type: GrantFiled: May 17, 1989Date of Patent: January 29, 1991Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Youichi Shiokawa, Koichi Takimoto, Kohei Takenaka, Takeshi Kato
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Patent number: 4981853Abstract: The compounds of this invention are heterocyclic amides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein q, r and t are independently an integer of from 1 to 8 provided that q+r+t is equal to or less than 10; Y is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene, and R.sub.3 is a heterocyclic amine represented by the formula: ##STR3## wherein R.sub.4 is selected from the group consisting of hydrogen, lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, carboxyl or carboxyloweralkyl; X is selected from the group consisting of N-R.sub.4, O and CH.sub.2 ; m is 2 or 3; n is 2 or 3 when X is O or N-R.sup.4, and n is 1 to 3 when X is CH.sub.2 ; p is 0 to 2; and the pharmaceutically acceptable salts thereof. The compounds are anti-inflammatory and anti-allergy agents.Type: GrantFiled: November 14, 1989Date of Patent: January 1, 1991Assignee: G. D. Searle & Co.Inventors: Richard A. Mueller, Richard A. Partis
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Patent number: 4977149Abstract: Trans-(.+-.)-2-(substituted)-6-(substituted)-5,5a,6,7,8,9,9a,10-octahydropy rido[2,3-g]quinolines are useful in treating a variety of disorders including Parkinsonism, anxiety, depression, hypertension, glaucoma, sexual dysfunction, and prolactin mediated disorders such as galactorrhea, amenorrhea, prolactinoma and the inhibition of postpartum lactation.Type: GrantFiled: April 25, 1990Date of Patent: December 11, 1990Assignee: Eli Lilly and CompanyInventor: John M. Schaus