Boron Or Silicon Containing Patents (Class 544/229)
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Patent number: 5238938Abstract: The novel indole derivatives and salts thereof represented by the general formula (1) ##STR1## possess, for example, an inhibitory effect against superoxide (O.sub.2.sup.-) released from the macrophage cells of guinea pig by stimulation and an anti-albuminuria activity against Masugi nephritis, and are useful in various clinical fields as an agent for preventing and treating diseases and cases associated with the above superoxide radical, for example, autoimmune diseases (e.g. rheumatism), arteriosclerosis, ischemic disease, ischemic encephalopathia, hepatic insufficiency and renal insufficiency, and also as an agent for preventing and treating nephritis.Type: GrantFiled: March 26, 1992Date of Patent: August 24, 1993Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hitoshi Tone, Seiji Sato, Hideaki Sato, Katsumi Tamura, Shigeharu Tamada, Kazumi Kondo, Tomoyuki Kawaguchi, Yoshimasa Nakano, Yasuyuki Kita, Shuji Akai, Hiromichi Fujioka, Yasumitsu Tamura, Katsuhide Matoba, Youichi Taniguchi, Shinji Nishitani, Satoshi Hayakawa, Toshinori Kaneyasu, Yoshihiko Ito, Masahiro Murakami
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Patent number: 5235053Abstract: 4-Hydroxypyrrolo[2,3-d]pyrimidines are regiospecifically halogenated at the C-5 position by silylation in the presence of an inert organic solvent and iodination, bromination or chlorination.Type: GrantFiled: June 22, 1992Date of Patent: August 10, 1993Assignee: Eli Lilly and CompanyInventors: Charles J. Barnett, Michael E. Kobierski
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Patent number: 5229514Abstract: Compounds of formula III ##STR1## wherein R.sub.1 is hydrogen; X is oxygen or sulfur; A is C.sub.1 -C.sub.2 alkylene and Q is --COOR.sub.16, where R.sub.16 is C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkylthio-C.sub.1 -C.sub.4 alkyl are intermediates to compounds which have good pre- and post-emergence selective herbicidal and growth-regulating properties.Type: GrantFiled: May 12, 1992Date of Patent: July 20, 1993Assignee: Ciba-Geigy CorporationInventors: Georg Pissiotas, Hans Moser, Hans-Georg Brunner
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Patent number: 5221761Abstract: A melt transesterification process for the production of polycarbonates, wherein at least one bis(aryl)carbonate is reacted with at least one dihydric phenol in the melted state, in the presence of a transesterification catalyst comprising at least one heterocyclic borate salt of the formula:M.sup.+ B(R).sub.n (A).sup.-.sub.4-n (I)where M.sup.+ is an alkali metal, tetra-alkylammonium, tetra-arylammonium, tetra-alkylphosphonium and tetra-arylphosphonium ion; R is H, alkyl, aryl or aralkyl; n is an integer from 0-3; and A is an aromatic or aliphatic heterocyclic ring.Type: GrantFiled: April 29, 1992Date of Patent: June 22, 1993Assignees: Instituto Guido Donegani, Enichem America, Inc.Inventors: Kwan-Yue A. Jen, Terence Moran
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Patent number: 5216155Abstract: Silicon and aluminum complexes having the following formula I, II or III: ##STR1## wherein x is 0 or 1, T is H or ##STR2## each R is independently selected from the group consisting of H, OH, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.2-6 alkene, C.sub.6-12 aryl, C.sub.1-6 hydroxyalkyl, C.sub.1-6 thioalkyl, C.sub.2-12 alkoxyalkyl, C.sub.3-20 heteroaromatic, and combinations thereof, wherein R may further contain one or more atoms of a non-carbon element such as Si, Ge, Sn, P, and the like; Y is a cation, and Z is a multivalent cation, are prepared by reacting silica or alumina with a diol, in the presence of a base, while removing water formed during the reaction. Methods for producing such complexes starting with silica or alumina, and methods for converting such complexes into other silicon or aluminum-containing compounds, are disclosed.Type: GrantFiled: November 12, 1991Date of Patent: June 1, 1993Assignee: Washington Research FoundationInventors: Richard M. Laine, Kay A. Youngdahl
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Patent number: 5204466Abstract: The present invention relates to a method of preparing BCH-189 and various analogs of BCH-189 from inexpensive precursors with the option of introducing functionality as needed. This synthetic route allows the stereoselective preparation of the biologically active isomer of these compounds, .beta.-BCH-189 and related compounds. Furthermore, the steochemistry at the nucleoside 4' position can be controlled to produce enantiomerically-enriched .beta.-BCH-189 and its analogs.Type: GrantFiled: February 1, 1990Date of Patent: April 20, 1993Assignee: Emory UniversityInventors: Dennis C. Liotta, Woo-Baeg Choi
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Patent number: 5200521Abstract: Cyclohexylphenylpyrimidines of the formula (I) ##STR1## in which R.sup.1 is straight-chain or branched, chiral or achiral alkyl or alkenyl having 2 to 16 carbon atoms, in which one or two nonadjacent --CH.sub.2 -- groups may be replaced by --O--, --S--, --CO--, --COO--, --OCO--, --Si(CH.sub.3).sub.2 -- or --C(CH.sub.3).sub.2 --, and in which one or more hydrogen atoms of the alkyl or alkenyl radical may be replaced by fluorine atoms, and in which the terminal CH.sub.3 group of the alkyl may also be replaced by ##STR2## R.sup.2 is straight-chain or branched, chiral or achiral alkyl having 1 to 10 carbon atoms,are particularly suitable components for ferroelectric liquid-crystal mixtures since they result in favorable properties, such as, for example, high contrast, when used in electrooptical switching and display devices.Type: GrantFiled: September 25, 1991Date of Patent: April 6, 1993Assignee: Hoechst AktiengesellschaftInventors: Gerd Illian, Rainer Wingen, Ingrid Muller
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Patent number: 5191079Abstract: Novel quinolinecarboxylic acid derivatives of the formula: ##STR1## wherein Z is ##STR2## in which R.sup.1 is hydrogen atom, a halogen atom, hydroxy or a lower alkyloxy; R.sup.2 is a halogen atom, hydroxy or a lower alkyloxy; R.sup.3 is a lower alkyl; and R.sup.4 is hydroxy or a di(lower alkyl)amino, and a pharmaceutically acceptable salt thereof, which have excellent antibacterial activities and are useful as an antibacterial agent, a pharmaceutical composition containing the same, and process for preparing the same.Type: GrantFiled: June 30, 1992Date of Patent: March 2, 1993Assignee: Kanebo, Ltd.Inventors: Hirosato Kondo, Masahiro Taguchi, Yoshikazu Jinbo, Yoshimasa Inoue, Yasuo Kotera, Fumio Sakamoto
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Patent number: 5188762Abstract: A mesomorphic compound represented by the following formula (I): ##STR1## wherein R.sub.1 denotes a linear or branched alkyl group having 2-16 carbon atoms capable of including one or two non-neighboring methylene groups which can be replaced with ##STR2## and capable of including fluorine substituted for hydrogen; A denotes --A.sub.1 -- or --A.sub.1 --A.sub.2 -- and B denotes --B.sub.1 -- or --B.sub.1 --B.sub.2 -- wherein A.sub.1, A.sub.2, B.sub.1 and B.sub.2 respectively denote ##STR3## wherein Y.sub.1 and Y.sub.2 respectively denote H, F, Cl, Br, --CH.sub.3, --CN or --CF.sub.3 ; Z.sub.1 and Z.sub.2 respectively denote ##STR4## Z.sub.3 denotes ##STR5## R.sub.2, R.sub.3 and R.sub.4 respectively denote a linear or branched alkyl group having 1-16 carbon atoms including a methylene group which can be replaced with ##STR6## with proviso that it is not adjacent to the silicon atom; p and q are respectively 0 or 1 with proviso that p+q is 0 or 1; and n is an integer of 1-12.Type: GrantFiled: May 20, 1991Date of Patent: February 23, 1993Assignee: Canon Kabushiki KaishaInventors: Takashi Iwaki, Takao Takiguchi, Takeshi Togano, Yoko Yamada, Shinichi Nakamura
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Patent number: 5185342Abstract: A fungicidal composition for agricultural use, which comprises a compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen, lower alkyl or cyclo(lower)alkyl; R.sup.3 is lower alkyl or cyclo(lower)alkyl; R.sup.4 and R.sup.5 are each hydrogen, lower alkyl, lower alkoxy, halogen-substituted lower alkyl, lower alkyl-substituted silyl, halogen or nitro; A represents an unsaturated hydrocarbon group, a halogen-substituted unsaturated hydrocarbon group, a phenyl group or a heterocyclic group, among which the phenyl group and the heterocyclic group may be optionally substituted with not more than three substituents; and Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, --NR-- (R being hydrogen or lower alkyl), --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 SO--, --OCH.sub.2 --, --SCH.sub.2 -- or --SOCH.sub.2 --.Type: GrantFiled: May 16, 1990Date of Patent: February 9, 1993Assignee: Shionogi Seiyaku Kabushiki KaishaInventors: Yoshio Hayase, Takahiro Kataoka, Hideyuki Takenaka, Mitsuhiro Ichinari, Michio Masuko, Toshio Takahashi, Norihiko Tanimoto
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Patent number: 5185337Abstract: There is described pyrroloquinoline derivatives of general formula: ##STR1## wherein R' is a C.sub.1 -C.sub.6 alkyl group, R.sup.2 is a group: ##STR2## or group: ##STR3## wherein R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as defined, or salt thereof. These compounds have an antimicrobial activity.Type: GrantFiled: April 25, 1991Date of Patent: February 9, 1993Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Setsuro Fujii, deceased, Kaoruko Takada, legal heir, Hiroshi Ishikawa, Hidetsugu Tsubouchi, Koichiro Jitsukawa
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Patent number: 5183889Abstract: A benzonphthalene compound has the formula ##STR1## wherein R.sub.1 represents ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --O--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy.This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjuctive tissues.Type: GrantFiled: December 9, 1991Date of Patent: February 2, 1993Assignee: Centre International de Recherches Dermatologiques (CIRD)Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
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Patent number: 5180717Abstract: Bivalent ligand compounds synthesized from a tether composition joining two heterocyclic groups comprising furochromones, furobenzoxazinones, and benzobisdifurans. These compounds show pharmacological activity in blocking ACAT enzymes which are major regulators of cholesterol metabolism. The compounds also show activity in lowering plasma triglycerides and elevating HDL cholesterol. They are useful in the prevention or treatment of the constriction or obstruction of arterial vessels, atherosclerosis, hyperlipidemia, hypertriglyceridemia, chylomicronemia, and pancreatitis.Type: GrantFiled: May 7, 1991Date of Patent: January 19, 1993Assignee: The Upjohn CompanyInventors: Ronald B. Gammill, Frank P. Bell
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Patent number: 5180418Abstract: Cycloalkanecarboxylic acid derivatives of formula I ##STR1## wherein W is ##STR2## and A is CO--R.sub.3 or CN; R.sub.1 is hydrogen or fluorine; R.sub.2 is halogen or cyano; R.sub.3 is chlorine, X--R.sub.5, amino, C.sub.1 -C.sub.4 alkylamino, d-C.sub.1 -C.sub.4 alkylamino, C.sub.2 -C.sub.4 haloalkylamino, di-C.sub.2 -C.sub.4 haloalkylamino, C.sub.1 -C.sub.4 hydroxyalkylamino, di-C.sub.1 -C.sub.4 hydroxyalkylamino, C.sub.3 -C.sub.4 alkenylamino, diallylamino, --N-pyrrolidino, --N-piperidino, --N-morpholino, --N-thiomorpholino, --N-piperidazino, the group --O--N.dbd.C--(R.sub.9)R.sub.10 or the group --N--R.sub.6 (OR.sub.6); each of R.sub.4 and R.sub.14, independently of the other, is hydrogen, fluorine, chlorine, bromine, C.sub.1 -C.sub.4 alkyl or trifluoromethyl; R.sub.5 is hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.4 alkyl, halo-C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.10 alkylthio-C.sub.1 -C.sub.4 alkyl, di-C.sub.1 -C.sub.4 alkylamino-C.sub.1 -C.sub.4 alkyl, cyano-C.sub.1 -C.sub.Type: GrantFiled: July 19, 1991Date of Patent: January 19, 1993Assignee: Ciba-Geigy CorporationInventors: Georg Pissiotas, Hans Moser, Hans-Georg Brunner, Eginhard Steiner
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Patent number: 5166198Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sub.1 is hydroxy or amino;R.sub.2 is hydrogen or amino;R.sub.3 is hydrogen, hydroxymethyl or acyloxymethyl;R.sub.4 is hydrogen or (when R.sub.3 =H and Z is a bond or CH.sub.2) hydroxy, acyloxy, hydroxymethyl or acyloxymethyl;Z is a bond, or a group CHR.sub.8 wherein R.sub.8 is hydrogen, or (when R.sub.3 =R.sub.4 =H), R.sub.8 is hydroxy, acyloxy, hydroxymethyl or acyloxymethyl;R.sub.5 is a group of formula: ##STR2## wherein R.sub.6 and R.sub.7 are independently selected from hydrogen,C.sub.1-6 alkyl and optionally substituted phenyl.Type: GrantFiled: March 28, 1990Date of Patent: November 24, 1992Assignee: Beecham p.l.c.Inventors: Michael R. Harnden, David M. Duckworth, Halina T. Serafinowska
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Patent number: 5157117Abstract: The invention relates to novel compounds of the formula: ##STR1## useful as an intermediate in the preparation of quinoline carboxylic acid medicaments.Type: GrantFiled: July 1, 1991Date of Patent: October 20, 1992Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Naomi Takagi, Hironobu Fubasami, Hiroshi Matsukubo
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Patent number: 5151520Abstract: A cationic dye-borate anion compound represented by the formula: ##STR1## where D+ is a cationic dye moiety selected from the group consisting of cationic cyanine, carbocyanine, hemicyanine, rhodamine, and azamethine dyes; R.sup.1 is alkyl; and R.sup.2, R.sup.3, and R.sup.4 are aryl. Such cationic dye-borate anion compounds are useful photoinitiators of free radical addition reactions.Type: GrantFiled: January 30, 1990Date of Patent: September 29, 1992Assignee: The Mead CorporationInventors: Peter Gottschalk, Douglas C. Neckers, Gary B. Schuster
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Patent number: 5145856Abstract: Compounds having the formula (I): ##STR1## in which any two of K, L and M are nitrogen and the other is CE; X and Y are independently hydrogen, halogen, C.sub.1-4 alkyl, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, C.sub.2-4 alkynyloxy, phenyl, benzyloxy, cyano, isocyano, isothiocyanato, nitro, NR.sup.1 R.sup.2, NR.sup.1 OR.sup.2, N.sub.3, NHCOR.sup.1, NR.sup.1 CO.sub.2 R.sup.2, NHCONR.sup.1 R.sup.2, N.dbd.CHNR.sup.1 R.sup.2, NHSO.sub.2 R.sup.1, OR.sup.1, OCOR.sup.1, OSO.sub.2 R.sup.1, SR.sup.1, SOR.sup.1, SO.sub.2 R.sup.1, SO.sub.2 OR.sup.1, SO.sub.2 NR.sup.1 R.sup.2, COR.sup.1, CR.sup.1 .dbd.NOR.sup.2, CHR.sup.1 CO.sub.2 R.sup.2, CO.sub.2 R.sup.1, CONR.sup.1 R.sup.2, CSNR.sup.1 R.sup.2, CH.sub.3 O.sub.2 C.C:CH.OCH.sub.Type: GrantFiled: December 27, 1991Date of Patent: September 8, 1992Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Ian T. Streeting, Rex Cheetham
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Patent number: 5144032Abstract: An improved curing agent for use in coatings, laminates, moldings, castings and adhesives comprising the use of an amine-boron adduct component along with anhydride and epoxy component mixtures. Also provided is an improved process for the preparation of tertiary amine borane curing agents.Type: GrantFiled: April 19, 1991Date of Patent: September 1, 1992Assignee: E. I. Du Pont de Nemours and CompanyInventor: Anthony J. Arduengo
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Patent number: 5144035Abstract: This invention provides pyridylthiazolidine carboxamide derivative shown by general formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein A.sup.1 is a single bond, carbonyl group or lower alkylene group which may include a carbonyl group and R.sup.1 is a heterocyclic ring which may be substituted with a lower alkyl group and further provides N-substituted piperazine derivatives useful as intermediates for preparing said compounds (I).Type: GrantFiled: April 10, 1990Date of Patent: September 1, 1992Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Toshiyasu Mase, Hiromu Hara, Toshimitsu Yamada
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Patent number: 5143915Abstract: A compound of the formula ##STR1## (symbols defined in the specification), its 3,4-dihydropyrimidine tautomer form and pharmaceutically acceptable salts thereof have calcium entry blocking activity. A process of preparation, pharmaceutical composition and method of using the compound to reduce blood pressure are also provided.Type: GrantFiled: July 25, 1990Date of Patent: September 1, 1992Assignee: E. R. Squibb & Sons, Inc.Inventors: George C. Rovnyak, Spencer D. Kimball
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Patent number: 5137879Abstract: Compounds of the formula ##STR1## R.sup.1 is H, C.sub.1 -C.sub.4 alkyl, or phenyl optionally substituted with halo, (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, halo (C.sub.1 -C.sub.4) alkyl, or halo (C.sub.1 -C.sub.4) alkoxy;R.sup.2 is H, (C.sub.1 -C.sub.4) alkyl, nitro, halo; orR.sup.1 and R.sup.2 combine to form --(CH.sub.2).sub.4 --;R.sup.3 is H, (C.sub.1 -C.sub.4) alkyl, halo (C.sub.1 -C.sub.4 alkyl, phenyl, or substituted phenyl;Y is a bivalent hydrocarbon radical two to six carbon atoms long, optionally substituted with (C.sub.1 -C.sub.4) alkyl, (C.sub.2 -C.sub.4) alkenyl or -alkynyl, branched (C.sub.3 -C.sub.7) alkyl, (C.sub.3 -C.sub.7) cycloalkyl or cycloalkenyl, halo, halo (C.sub.1 -C.sub.4) alkyl, halo (C.sub.1 -C.sub.4) alkoxy, hydroxy, or (C.sub.1 -C.sub.4) acyl; andZ is an optionally substituted cycloalkyl, cycloalkenyl, phenyl, naphtyl, or pyridyl group;are useful as fungicides and as intermediates in making other pesticides.Type: GrantFiled: March 30, 1990Date of Patent: August 11, 1992Assignee: DowElancoInventors: Ronnie G. Edie, Eriks V. Krumkalns, Ronald E. Hackler
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Patent number: 5137891Abstract: The present invention provides a compound of the formula: ##STR1## process for their production, pharmaceutical compositions containing them and their pharmaceutical uses, and intermediates useful for their production and processes for the production of such intermediates.Type: GrantFiled: June 14, 1991Date of Patent: August 11, 1992Assignee: Nissan Chemical Industries Ltd.Inventors: Yoshihiro Fujikawa, Mikio Suzuki, Hiroshi Iwasaki, Mitsuaki Sakashita, Masaki Kitahara
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Patent number: 5135562Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is halogen;X is oxygen; or sulfur;Y is oxygen; or sulfur;A is a straight-chain or branched C.sub.1 -C.sub.4 alkylene chain;Q is hydroxy; halogen; cyano; unsubstituted or cyano- or halo-substituted C.sub.2 -C.sub.6 alkenyl; C.sub.2 -C.sub.4 alkynyl; --CR.sub.2 .dbd.CH--COOR.sub.3 ; --CH[N(R.sub.2).sub.2 ]COOR.sub.2 ; --NR.sub.4 (R.sub.5); --CO--NR.sub.6 R.sub.7 ; --COON.dbd.CR.sub.8 (R.sub.8); --C(R.sub.2)(OR.sub.9).sub.2 ; --Si(R.sub.10).sub.3 ; --COOCH.sub.2 Si(CH.sub.3).sub.2 --C.sub.1 -C.sub.6 alkyl; ##STR2## --CON(R.sub.12)SO.sub.2 --C.sub.1 -C.sub.6 alkyl; --CON(R.sub.12)SO.sub.2 --C.sub.1 -C.sub.4 haloalkyl; C.sub.1 -C.sub.6 alkylcarbonyl; C.sub.2 -C.sub.6 alkoxyalkylcarbonyl; benzoyl; benzylcarbonyl; --COOR.sub.16 ; --CO--N(R.sub.2)CH.sub.2 --CH.sub.2 --CH(O--C.sub.1 -C.sub.6 alkyl).sub.2 ; --COO(CH.sub.2).sub.j N(R.sub.2).sub.2 ; --S(O).sub.k --R.sub.14 ; --S(O).sub.k --A'--COOR.sub.Type: GrantFiled: March 19, 1991Date of Patent: August 4, 1992Assignee: Ciba-Geigy CorporationInventors: Georg Pissiotas, Hans Moser, Hans-Georg Brunner
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Patent number: 5122609Abstract: Novel cyclic N,N,N' and N,N,N',N'-substituted organyloxysilyl-functional silanes are prepared by reacting an aminopropyl silane with carbon disulfide and heating the dithiocarbamate.Type: GrantFiled: January 10, 1991Date of Patent: June 16, 1992Assignee: Degussa AktiengesellschaftInventors: Ulrich Deschler, Peter Kleinschmit
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Patent number: 5120843Abstract: The aromatic amines (I), alkyl amines (II), bicyclic amines (III). ##STR1## cycloalkyl amines (IV), aromatic bicyclic amines (V), hydroquinone amines (VI), quinone amines (VII), amino-ethers (VIII) and bicyclic amino ethers (IX) are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc. Also disclosed is a method of treatment using the 3,4-dihydrobenzopyrans (XI).Type: GrantFiled: October 23, 1989Date of Patent: June 9, 1992Assignee: UpjohnInventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer
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Patent number: 5120845Abstract: The present invention relates to novel positive inotropic and lusitropic 3,5-dihydroimidazo[2,1-b]quinazolin-2(1H)-one derivatives having positive inotropic and lusitropic properties which are useful in the treatment of warm-blooded animals suffering from Congestive Heart Failure. Pharmaceutical compositions containing said compounds as an active ingredient. Methods of preparing said compounds and pharmaceutical compositions.Type: GrantFiled: July 24, 1991Date of Patent: June 9, 1992Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers
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Patent number: 5120741Abstract: Compounds of the formula ##STR1## in which R.sub.1 is hydrogen, halogen, methyl, methoxy or trifluoromethyl; n is 1 or 2; R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.3 alkyl which is substituted by halogen, cyano or methoxy, or is C.sub.2 -C.sub.5 alkenyl, C.sub.2 -C.sub.5 alkynyl, benzyl, COR.sub.5, CON(R.sub.5)R.sub.6, CSN(R.sub.5)R.sub.6, CO(OR.sub.6), CO(SR.sub.6), CS(SR.sub.5), SO.sub.2 R.sub.7, PO(OR.sub.6).sub.2 or Si(R.sub.6).sub.3 ; R.sub.3 and R.sub.4 independently of one another are hydrogen, C.sub.1 -C.sub.5 alkyl, CH.sub.2 OR.sub.6, cyclopropyl, methylcyclopropyl, C.sub.2 -C.sub.5 alkenyl, C.sub.2 -C.sub.5 alkynyl or C.sub.1 -C.sub.2 haloalkyl; R.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.3 alkyl which is substituted by 1 to 3 halogens, C.sub.1 -C.sub.3 alkyl which is substituted or OR.sub.6 or SR.sub.6, or is C.sub.2 -C.sub.5 alkenyl, C.sub.2 -C.sub.5 alkenyl which is substituted by 1 to 3 halogens, C.sub.2 -C.sub.5 alkynyl, C.sub.3 -C.sub.Type: GrantFiled: February 1, 1991Date of Patent: June 9, 1992Assignee: Ciba-Geigy CorporationInventor: Helmut Zondler
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Patent number: 5118339Abstract: A pyrimidine or triazine derivative and its salt, said pyrimidine or triazine derivative having the formula: ##STR1## wherein R represents a group of the formula OR.sub.3 {wherein R.sup.3 represents a hydrogen atom, an alkyl gorup, etc.}, a group of the formula SR.sup.6 {wherein R.sup.6 represents a hydrogen atom, an alkyl group, etc.}, a group of the formula ##STR2## {wherein R.sup.7 and R.sup.8 represent a hydrogen atom, an alkyl group, etc.}, or an imidazolyl group:R.sup.1 represents a hydrogen atom, an alkyl group, etc.;R.sup.2 represents a hydroxyl group, an alkyl group, etc.;A and B represent an alkyl group, etc.;Y represents an oxygen atom, etc.; andZ represents a methine group or a nitrogen atom.Type: GrantFiled: December 20, 1990Date of Patent: June 2, 1992Assignees: Kumiai Chemical Co., Ihara Chemical Industry Co., Ltd.Inventors: Masatoshi Tamaru, Norihiro Kawamura, Masahiro Sato, Fumiaki Takabe, Shigehiko Tachikawa, Ryo Yoshida
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Patent number: 5116404Abstract: The present invention provides novel uracil derivatives and pesticides which contain the novel uracil derivatives as an active ingredient, and exhibit preventing and controlling effects against harmful living things, especially agricultural insect pests, sanitary insect pests, stored product insect pests, house insect pests and veterinary insect pests at a very low drug-concentration.Type: GrantFiled: January 8, 1991Date of Patent: May 26, 1992Assignee: Nissan Chemical Industries Ltd.Inventors: Shigeru Ishii, Kazunari Nakayama, Kazuo Yagi, Jun Satow, Kenzou Fukuda, Kaoru Itoh, Toshiyuki Umehara, Masaki Kudo, Yoichi Inoue, Tsutomu Nawamaki, Shigeomi Watanabe
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Patent number: 5116980Abstract: The present invention pertains to boron containing thiouracil derivatives, their method of preparations, and their use in the therapy of malignant melanoma using boron neutron capture therapy.Type: GrantFiled: February 25, 1991Date of Patent: May 26, 1992Assignee: The United States of America as represented by the United States Department of EnergyInventor: Detlef Gabel
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Patent number: 5113617Abstract: The present invention relates to a method for inducing male sterility in plants which comprises treating seeds of a plant receptive to said treatment by application of an effective amount of a compound of the formula: ##STR1## wherein R and R.sup.1 are hydrogen, alkyl, alkenl, alkynl, allyl, aryl, halogen or boron and may be the same or different;X and X.sup.1 are fluorine, chlorine, bromine or iodine; nitrate, sulfate, sulfonate, phosphate, citrate, or maleate;n and n.sup.1 are the integers 0 or 1, and may be the same or different;m and m.sup.1 are integers from 0 to 4, and may be the same or different;for a period of time and under conditions sufficient to induce male sterility in adult plants which are grown from said treated seeds.Type: GrantFiled: March 27, 1990Date of Patent: May 19, 1992Assignee: Arizona Board of Regents on behalf of University of ArizonaInventor: Robert G. McDaniel
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Patent number: 5103000Abstract: A packing for use in chromatography which comprises a cyclic amino-substituted silane compound having the formula (I): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and are each an alkyl having 1 to 5 carbon atoms, an alkoxy having 1 to 3 carbon atoms, hydroxy or a halogen atom in which at least one of R.sup.1, R.sup.2 and R.sup.3 are an alkoxy group or a halogen atom; R.sup.4 is .omega.-piperidino, .omega.-piperazino or .omega.-morpholino group which is optionally substituted by a straight chain or branched chain lower alkyl group; n is an integer of from 2 to 10, said compound being grafted onto an inorganic carrier having hydroxyl group on its surface, and a method for separating water soluble organic compounds by chromatography using said packing.Type: GrantFiled: September 10, 1990Date of Patent: April 7, 1992Assignee: Daiso Co., Ltd.Inventors: Shuzo Akiyama, Kenichiro Nakashima, Yasumi Shimizu, Yutaka Kamada, Junichi Kadoya
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Patent number: 5100896Abstract: The present invention provides a compound of formula (I) ##STR1## and salts and solvates and pharmaceutically acceptable derivatives thereof, and describes processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of viral diseases, especially those caused by the Herpetoviridae.Type: GrantFiled: July 23, 1990Date of Patent: March 31, 1992Assignee: Glaxo Group LimitedInventors: Alan D. Borthwick, Keith Biggadike, Barrie E. Kirk, Richard Storer, Niall G. Weir, Anthony D. Baxter, Chi L. Mo
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Patent number: 5099052Abstract: Silicon and aluminum complexes having the following formula: ##STR1## wherein x is 0 or 1, T is H or ##STR2## each R is independently selected from the group consisting of H, OH, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.2-6 alkene, C.sub.6-12 aryl, C.sub.1-6 hydroxyalkyl, C.sub.1-6 thioalkyl, C.sub.2-12 alkoxyalkyl, C.sub.3-20 heteroaromatic, and combinations thereof, wherein R may further contain one or more atoms of a non-carbon element such as Si, Ge, Sn, P, and the like; and Y is a cation, are prepared by reacting silica or alumina with a diol, in the presence of a base, while removing water formed during the reaction. Methods for producing such complexes starting with silica or alumina, and methods for converting such complexes into other silicon or aluminum-containing compounds, are disclosed.Type: GrantFiled: April 13, 1990Date of Patent: March 24, 1992Assignee: Washington Research FoundationInventors: Richard M. Laine, Kay A. Youngdahl, Paola Nardi
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Patent number: 5099020Abstract: The present invention provides methods and compositions for assaying biological samples, such as human serum, for barbiturates. In one aspect, analogs of barbiturates derivatized with fluorescein and analogs of barbiturates derivatized with immunogenic polypeptides are provided. The fluorescent analogs are employed as tracers in a competitive homogeneous immunoassay, i.e., a fluorescence polarization immunoassay, for detecting barbiturates. The immunogenic analogs are employed to make anti-barbiturate antiserum of the invention for use in the immunoassay method. Intermediates for preparing the fluorescent and immunogenic analogs are also provided. Further provided are test kits, comprising a fluorescent tracer and an antiserum according to the invention, for analyzing biological samples by fluorescence polarization immunoassay for the presence of a barbiturate.Type: GrantFiled: June 27, 1990Date of Patent: March 24, 1992Assignee: Abbott LaboratoriesInventors: Jonathan Grote, Hsiang Hu
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Patent number: 5093336Abstract: Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: July 6, 1989Date of Patent: March 3, 1992Assignee: Hoechat-Roussel Pharmaceuticals, Inc.Inventors: Raymond W. Kosley, Jr., Bettina Spahl
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Patent number: 5091530Abstract: The invention relates to a new process for the preparation of compounds of the general Formula I ##STR1## /wherein R stands for piperazinyl, 4-methyl-piperazinyl or 4-ethyl-piperazinyl group/ and pharmaceutically acceptable salts thereof which comprises reacting a compound of the general Formula II ##STR2## /wherein R.sup.1 and R.sup.2 stand for halogen, for an aliphatic acyloxy group containing 2 to 6 carbon atoms and optionally substituted by halogen, or for an aromatic acyloxy group containing 7 to 11 carbon atoms/ with a piperazine derivative of the general Formula ##STR3## /wherein R.sup.3 stands for hydrogen, methyl or ethyl/ or a salt thereof and subjecting the compound of the general Formula IV ##STR4## thus obtained /wherein R, R.sup.1 and R.sup.2 are as stated above/ to hydrolysis after or without isolation and if desired converting the compound of the general Formula I thus obtained into a salt thereof or setting free the same from its salt.Type: GrantFiled: November 23, 1988Date of Patent: February 25, 1992Assignee: Chinoin Gyogyszer- es Vegyeszeti Termekek Gyara Rt.Inventors: Istvan Hermecz, Geza Kereszturi, Lelle Vasvari, Agnes Horvath, Marie Balogh, Peter Ritli, Judit Sipos, Aniko Pajor, Katalin Marmarosi
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Patent number: 5089618Abstract: Crude adenine, that is contaminated by 9-phenyladenine and/or colored additives, is converted with hexamethyldisilazane in the presence of a catalyst into N,N'-bis(trimethylsilyl) adenine, which is distilled and then reconverted into pure adenine by hydrolysis.Type: GrantFiled: July 31, 1990Date of Patent: February 18, 1992Assignee: Lonza Ltd.Inventor: Wilhelm Quittmann
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Patent number: 5084568Abstract: An improved process for preparing trialkylsilyl ester and acid halide derivatives of carboxylic acids is provided along with novel trialkylsilyl ester intermediates of 2-(2-furyl)-2-methoximinoacetic acid.Type: GrantFiled: December 17, 1990Date of Patent: January 28, 1992Assignee: Eli Lilly and CompanyInventor: Charles A. Bunnell
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Intermediates and processes for preparing 4-substituted 2-5(H)-furanones as anti-inflammatory agents
Patent number: 5082954Abstract: Anti-inflammatory 4-substituted 2-furanones are made from intermediates having the formulas: ##STR1## in which R.sub.1, R.sub.2 and R.sub.3 independently are n-alkyl of 1 to 6 carbons, or branched chain alkyl of 1 to 6 carbons; X is H, OH, NH.sub.2, I or Br; R.sub.4 is H, alkyl of 1-20 carbons, phenyl[C.sub.1 -C.sub.20 alkyl], naphthyl[C.sub.1 -C.sub.20 alkyl], CH.sub.2 OH, CH.sub.2 NH.sub.2, CH.sub.2 CH.sub.2 OH, CH.sub.2 --CHO, CH.sub.2 --COOH or CH.sub.2 --COOR.sub.5, and R.sub.5 is alkyl of 1 to 6 carbons, with the proviso that when X is hydrogen then R.sub.4 is selected from the group consisting of CH.sub.2 OH, CH.sub.2 NH.sub.2, CH.sub.2 CH.sub.2 OH, CH.sub.2 --CHO, or CH.sub.2 --COOR.sub.5 ; ##STR2## in which R.sub.1, R.sub.2 and R.sub.3 independently are n-alkyl of 1 to 6 carbons, or branched chain alkyl or 1 to 6 carbons, and R.sub.5 is alkyl or 1 to 6 carbons; ##STR3## in which R.sub.1, R.sub.2 and R.sub.3 independently are n-alkyl of 1 to 6 carbons, or branched chain alkyl of 1 to 6 carbons, and R.Type: GrantFiled: April 24, 1991Date of Patent: January 21, 1992Assignee: Allergan, Inc.Inventors: Gary C. M. Lee, Michael E. Garst -
Patent number: 5081147Abstract: Compounds of the formula ##STR1## where R.sub.1 is H or alkyl of 1 to 20 carbons, CO--R.sub.1 *, CO--O--R.sub.1 *, CO--NH--R.sub.1 *, or PO(OR.sub.1 *).sub.2, PO(OR.sub.1 *)R.sub.1 * where R.sub.1 * independently is H, alkyl of 1 to 20 carbons, phenyl, or substituted phenyl;R.sub.2 is H or alkyl of 1 to 20 carbons;X is H, R.sub.3, CO--R.sub.3, CO--O--R.sub.3, CO--NH--R.sub.3, CO--N--(R.sub.3).sub.2, PO(OR.sub.3).sub.2, PO(OR.sub.3)R.sub.3, and R.sub.3 independently is H, phenyl, substituted phenyl, alkyl of 1 to 20 carbons or is alkyl of 1 to 20 carbons substituted with a hydroxyl, alkoxy, substituted amino, thioalkoxy or with a COR.sub.3 * group where R.sub.3 * is H, lower alkyl, OH, OR.sub.3 **, NH.sub.2, NHR.sub.3 ** or N(R.sub.3 **).sub.2 group wherein R.sub.3 ** independently is H or lower alkyl, with the proviso that when X is CO--O--R.sub.3 or is CO--NH--R.sub.3 then R.sub.3 is not hydrogen;Y is H, R.sub.4, CO--R.sub.4, CO--O--R.sub.Type: GrantFiled: March 15, 1990Date of Patent: January 14, 1992Assignee: Allergan, Inc.Inventor: Gary C. M. Lee
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Patent number: 5080708Abstract: Isoxazole(isothiazole)-5-carboxamides of the formula ##STR1## where X is oxygen or sulfur,R.sup.1 is hydrogen, substituted or unsubstituted alkyl, alkoxy, substituted or unsubstituted cycloalkyl, a 5- or 6-membered heterocyclic radical having one or two heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen, and which may be substituted, or substituted or unsubstituted phenyl, orR.sup.2 is formyl, 4,5-dihydrooxazol-2-yl or a radical of the formula COYR.sup.5 or CONR.sup.6 R.sup.7, whereY is oxygen or sulfur,R.sup.5 ishydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, haloalkenyl, substituted or unsubstituted alkynyl,cycloalkyl,cycloalkenyl,substituted or unsubstituted phenyl,a 5- or 6-membered heterocyclic radical having one or two heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen,cycloalkanimino, phthalimido, succinimido, or a radical ##STR2## R.sup.3 and R.sup.Type: GrantFiled: April 13, 1989Date of Patent: January 14, 1992Assignee: BASF AktiengesellschaftInventors: Wolfgang Freund, Thomas Kuekenhoehner, Gerhard Hamprecht, Bruno Wuerzer, Karl-Otto Westphalen, Norbert Meyer, Hans Theobald
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Patent number: 5081261Abstract: Compounds of Formula 1, and of Formula 2, ##STR1## in which R.sub.1 is H or alkyl of 1 to 20 carbons, CO--R.sub.1.sup.* CO--O--R.sub.1.sup.* CO--NH--R.sub.1.sup.* or PO(OR.sub.1.sup.*).sub.2 or PO(OR.sub.1.sup.*)R.sub.1.sup.* where R.sub.1.sup.* independently is H, alkyl of 1 to 20 carbons, phenyl, or substituted phenyl; R.sub.2 is H, alkyl of 1 to 20 carbons, or R.sub.2 and Y jointly represent a heterocycle which incorporates the sulfonamide nitrogen in the ring as a heteroatom; R.sub.3 is H or alkyl of 1 to 20 carbons; X is H, R.sub.4, CO--R.sub.4, CO--O--R.sub.4, CO--NH--R.sub.4, CO--N--(R.sub.4).sub.2, PO(OR.sub.4).sub.2 or PO(OR.sub.4)R.sub.4, and R.sub.4 independently is H, phenyl, substituted phenyl, alkyl of 1 to 20 carbons or is alkyl of 1 to 20 carbons substituted with a hydroxyl, alkoxy, substituted amino, thioalkoxy, with a O--COR.sub.4.sup.* group or with a COR.sub.4.sup.* group where R.sub.4.sup.* is H, lower alkyl, OH, OR.sub.4.sup.**, NH.sub.2, NHR.sub.4.sup.** or N(R.sub.4.sup.**).sub.Type: GrantFiled: March 23, 1990Date of Patent: January 14, 1992Assignee: Allergan, Inc.Inventor: Gary C. M. Lee
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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: 5070092Abstract: DC-88A derivatives represented by the general formula: ##STR1## wherein X represents hydrogen or CO.sub.2 R.sup.1 (in which R.sup.1 represents hydrogen, a straight-chain or branched alkyl having 1 to 4 carbon atoms, allyl, or benzyl); and ##STR2## have an excellent anti-tumor activity and are useful as anti-tumor agents.Type: GrantFiled: June 29, 1990Date of Patent: December 3, 1991Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Yutaka Kanda, Youichi Uosaki, Hiromitsu Saito, Hiroshi Sano, Eiji Kobayashi, Makoto Morimoto, Satoru Nagamura
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Patent number: 5070215Abstract: Novel monomers of the general formula ##STR1## where b is 0 or 1, a is 1, 2, 3 or 4, R.sup.2 is a monovalent alkyl radical and R is an organic radical. The novel monomers may be employed to produce novel copolymers useful as hydrogel, soft non-hydrogel and/or rigid gas permeable contact lens materials.Type: GrantFiled: May 2, 1989Date of Patent: December 3, 1991Assignee: Bausch & Lomb IncorporatedInventors: Ronald E. Bambury, David E. Seelye
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Patent number: 5059605Abstract: Fungicidal compounds having the formula (I): ##STR1## in which any two of K, L and M are nitrogen and the other is CE; X and Y are independently hydrogen, halogen, C.sub.1-4 alkyl, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, C.sub.2-4 alkenyloxy, C.sub.2-4 alkynyloxy, phenyl, benzyloxy, cyano, isocyano, isothiocyanato, nitro, NR.sup.1 R.sup.2, NR.sup.1 OR.sup.2, N.sub.3, NHCOR.sup.1, NR.sup.1 CO.sub.2 R.sup.2, NHCONR.sup.1 R.sup.2, N.dbd.CHNR.sup.1 R.sup.2, NHSO.sub.2 R.sup.1, OR.sup.1, OCOR.sup.1, OSO.sub.2 R.sup.1, SR.sup.1, SOR.sup.1, SO.sub.2 R.sup.1, SO.sub.2 OR.sup.1, SO.sub.2 NR.sup.1 R.sup.2, COR.sup.1, CR.sup.1 .dbd.NOR.sup.2, CHR.sup.1 CO.sub.2 R.sup.2, CO.sub.2 R.sup.2, CO.sub.2 R.sup.1, CONR.sup.1 R.sup.2, CSNR.sup.1 R.sup.2, CH.sub.3 O.sub.2 C.C:CH.OCH.sub.Type: GrantFiled: April 10, 1990Date of Patent: October 22, 1991Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Ian T. Streeting
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Patent number: 5055472Abstract: The present invention provides a compound of the formula: ##STR1## process for their production, pharmaceutical compositions containing them and their pharmaceutical uses, and intermediates useful for their production and processes for the production of such intermediates.Type: GrantFiled: October 25, 1989Date of Patent: October 8, 1991Assignee: Nissan Chemical Industries, Ltd.Inventors: Yoshihiro Fujikawa, Mikio Suzuki, Hiroshi Iwasaki, Mitsuaki Sakashita, Masaki Kitahara
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Patent number: 5053071Abstract: This invention pertains to novel heterocyclic 2,3-dihydrobenzofuran and chromane compounds, including stereoisomers, agriculturally suitable compositions containing them, and their use as broad spectrum herbicides.Type: GrantFiled: May 2, 1990Date of Patent: October 1, 1991Assignee: E. I. Du Pont de Nemours and CompanyInventor: Joseph E. Semple