Phosphorus Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/21)
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Patent number: 5750680Abstract: N-vinyllactam derivatives protected at the 3-position are provided and represented by the following formula (I). These are polymerized into homo- and copolymers for use in microlithography of semiconductor manufacture. The polymers are used as a photoresist material suitable for a deep UV process so that pictures of high sensitivity and high resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in pattern formation can be accomplished through the use of the photoresist of the invention.Type: GrantFiled: September 12, 1996Date of Patent: May 12, 1998Assignees: Hyundai Electronics Industries Co., Ltd., Korea Advanced Institute of Science & TechnologyInventors: Jin Baek Kim, Min Ho Jung, Kyeong Ho Chang
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Patent number: 5731300Abstract: Novel substituted benzimidazoles of the formula ##STR1## in which Q, R, X and Z have the meanings given in the description,a process for the preparation of the novel substances and their use for combating pests.Type: GrantFiled: October 30, 1996Date of Patent: March 24, 1998Assignee: Bayer AktiengesellschaftInventors: Lutz Assmann, Albrecht Marhold, Heinz-Wilhelm Dehne, Stefan Dutzmann, Christoph Erdelen, Klaus Stenzel
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Patent number: 5726185Abstract: Acetic acid derivatives of the formula ##STR1## wherein L, M, T and Q have the significance given in the description, can be used for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion, and are manufactured by cleaving protecting groups in the corresponding protected compounds or by converting the cyano group into the amidino group in corresponding nitriles.Type: GrantFiled: December 1, 1994Date of Patent: March 10, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Paul Hadvary, Marianne Hurzeler Muller, Marcel Muller, Beat Steiner, Thomas Weller
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Patent number: 5719135Abstract: The present invention relates to compound of formula (I) ##STR1## wherein A is benzene, naphthalene, 5,6,7,8,-tetrahydronaphthalene, quinoline, isoquinoline, indole or 7-azaindole;R.sub.1 is --H, --CN, --SO.sub.3 R.sub.4 --, --SO.sub.2 NHR.sub.5, ##STR2## --COOR.sub.6, --CONHCH.sub.2 (CHOH).sub.n CH.sub.2 OH, ##STR3## --NR.sub.7 R.sub.8, --N(CH.sub.2 CH.sub.2 OH).sub.2, --NHCH.sub.2 (CHOH).sub.n CH.sub.2 OH, --NHCONH.sub.2, --NH--C(NH.sub.2).dbd.NH, --NHCO(CHOH).sub.n CH.sub.2 OH, ##STR4## --NHSO.sub.2 R.sub.9, --OR.sub.10, --OCH.sub.2 (CHOH).sub.n CH.sub.2 OH, --OOC(CHOH).sub.n CH.sub.2 OH, --OPO(OH).sub.2, --CH.sub.2 NH.sub.2, --C(NH.sub.2).dbd.NH, --CH.sub.2 NHC(NH.sub.2).dbd.NH, ##STR5## --CH.sub.2 OH, --CH.sub.2 OOC(CHOH).sub.n CH.sub.2 OH, --CH.sub.2 OPO(OH).sub.2 or --PO(OH).sub.2 ;R.sub.2 is C.sub.1 -C.sub.6 alkyl, halogen, or hydroxy;R.sub.3 is --H or C.sub.1 -C.sub.6 alkyl;R.sub.4 is --H, C.sub.1 -C.sub.6 alkyl or --CH.sub.2 (CHOH).sub.n CH.sub.2 OH;R.sub.5 is --H, C.sub.1 -C.sub.6 alkyl, --CH.sub.Type: GrantFiled: July 9, 1996Date of Patent: February 17, 1998Assignee: Pharmacia S.p.A.Inventors: Franco Buzzetti, Gabriella Maria Brasca, Antonio Longo, Dario Ballinari
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Patent number: 5716958Abstract: A compound represented by the formula (1): ##STR1## wherein, m is an integer of 1 to 3;n is an integer 0 or 1;A represents CH or N atom, and forms together with the N atom bonded to the carbonyl group a piperidine ring or a piperazine ring;R.sub.1 independently represents a straight or branched chain alkyl group having 1 to 4 carbon atoms; a cycloalkyl group having 3 to 8 carbon atoms; a phenyl group, unsubstituted or substituted with a halogen atom or with an alkoxy group having 1 to 4 carbon atoms; or a pyridyl group; or two R.sub.1, together with the group >CH-- to which they bind, form a dibenzo cycloheptenyl group or a fluorenyl group;R.sub.Type: GrantFiled: August 9, 1995Date of Patent: February 10, 1998Assignee: Tobishi Pharmaceutical Co., Ltd.Inventors: Masashi Ogawa, Tadashi Morita, Kiyoshi Matsuda, Norihiro Iibuchi, Shinpei Kidokoro
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Patent number: 5698541Abstract: The invention concerns compounds of the general formula I ##STR1## in which R denotes a lower alkyl which can be substituted if desired by hydroxy, alkoxy, amino, dialkylamino, alkylmercapto, alkylsulfinyl, alkanesulfonyl, cycloalkyl, aryl or a heterocyclic ring, or it denotes lower alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocyclic ring andR.sub.1 and R.sub.2 can be, independently of one another, hydrogen, lower alkyl, cycloalkyl, aryl or arylmethyl,their optically active salts as well as their pharmacologically acceptable salts, processes for their production as well as pharmaceutical agents which contain these compounds for treating diseases of calcium metabolism. Moreover the invention concerns compounds of formula II as intermediate products for the production of compounds of formula I.Type: GrantFiled: September 25, 1996Date of Patent: December 16, 1997Assignee: Boehringer Mannheim GmbHInventors: Gerd Zimmermann, Angelika Esswein, Christos Tsaklakidis, Frieder Bauss
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Patent number: 5686466Abstract: A novel compound of the formula: ##STR1## wherein Ar represents an optionally substituted tricyclic condensed benzene ring group which includes at least one heterocyclic ring as a component ring; n represents an integer from 2 to 10; R.sup.1 represents H or an optionally substituted hydrocarbon group, which may be different from one another in the repetition of n; and Y represents an optionally substituted 4-piperidinyl, 1-piperazinyl or 4-benzyl-1-piperidinyl group, or a salt thereof, inhibiting excellent cholinesterase inhibitory activity and monoamine reuptake inhibitory activity, thus being useful as therapeutic and/or prophylactic medicaments of senile dementia.Type: GrantFiled: March 20, 1996Date of Patent: November 11, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Giichi Goto, Yuji Ishihara, Keisuke Hirai
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Patent number: 5686613Abstract: Novel pyridine phosphonate ligands are disclosed that when combined with polyvalent metals results in useful catalyst compositions for the conversion of hydrogen sulfide to solid sulfur. Catalysts containing these novel ligands exhibit resistance to metal precipitation and demonstrate little or no oxidative chemical degradation when employed to convert hydrogen sulfide to elemental sulfur.Type: GrantFiled: January 16, 1996Date of Patent: November 11, 1997Assignee: Wheelabrator Clean Air Systems Inc.Inventors: Derek McManus, Arthur E. Martell, Dian Chen
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Patent number: 5672592Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme inhibitors which are proposed as novel agents for the treatment of prostate cancer. NAALADase is enzyme which is a membrane-bound metalloprotease which hydrolyzes the dipeptide, N-acetyl-L-aspartate-L-glutamate (NAAG) to yield glutamate and N-acetylaspartate. The compounds of the present invention include phosphinic acid derivatives that inhibit NAALADase enzyme activity and which have been found useful for inhibiting the growth of prostate cancer cells.Type: GrantFiled: June 17, 1996Date of Patent: September 30, 1997Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Barbara S. Slusher
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Patent number: 5654429Abstract: A process for the preparation of a 3-amino-2-chloro-4-alkylpyridine of the formula: ##STR1## wherein R1 is a linear, branched or cyclic hydrocarbon of from one to eight carbon atoms, optionally substituted with one or more electron stabilizing groups,an intermediate in the preparation of certain 5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepine compounds useful in the prevention and treatment of HIV infection.Type: GrantFiled: June 7, 1995Date of Patent: August 5, 1997Inventor: Laurence John Nummy
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Patent number: 5627169Abstract: Novel phosphinic and phosphonic acid derivatives of pyridine, pyrrole and azepine with utility as antagonists of the GABA.sub.rho receptor are disclosed. These compounds have utility as modulators of the excitability of the central nervous system as mediated by their ability to specifically act on closed-channel binding sites of GABA.sub.rho receptors.Type: GrantFiled: July 20, 1994Date of Patent: May 6, 1997Assignee: The Regents of The University of CaliforniaInventors: Ricardo Miledi, Larry E. Overman, Yoshinori Murata, Richard M. Woodward
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Patent number: 5580863Abstract: This invention relates to a compound represented by the formula: ##STR1## wherein B represents a hydrogen atom or a lower alkyl group; ring A represents a benzene ring which may have one or more substituents; .multidot..multidot..multidot..multidot..multidot. represents a single or double bond; Q.sub.1 represents the group represented by the formula, ##STR2## or a hydrocarbon residue substituted with the group represented by the formula, ##STR3## wherein X represents a bond or a spacer having a chain length of 1 to 4 atoms as the linear moiety which may have one or more side chains; R.sup.1 and R.sup.2, whether identical or not, independently represent a hydrogen atom or a lower alkyl, or may bind together to form a ring; Q.sub.2 represents a hydrogen atom, a hydrocarbon residue which may be substituted or a heterocyclic ring residue which may be substituted; or a salt thereof.Type: GrantFiled: May 13, 1994Date of Patent: December 3, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Shigehisa Taketomi, Tsuneo Oda
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Patent number: 5574024Abstract: The present invention involves novel methylene phosphonoalkylphosphinic acids, pharmaceutical compositions containing such compounds, and methods for treating or preventing pathological conditions characterized by abnormal calcium and phosphate metabolism by administering such compounds to a human or lower animal.Type: GrantFiled: June 3, 1994Date of Patent: November 12, 1996Inventor: Frank H. Ebetino
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Patent number: 5545647Abstract: 3-Phenylpyrrolidine compounds of the formula ##STR1## effectively inhibit phosphodiesterase (PDE) IV activities and can be used as medicaments for conditions such as asthma.Type: GrantFiled: March 6, 1995Date of Patent: August 13, 1996Assignee: Mitsubishi Chemical CorporationInventors: Toshihiko Tanaka, Akihiro Yamamoto, Akira Amenomori
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Patent number: 5543396Abstract: Peptidyl derivatives of diesters of .alpha.-aminoalkylphosphonic acids, particularly those with proline or related structures, their use in inhibiting serine proteases with chymotrypsin-like, trypsin-like, elastase-like, and dipeptidyl peptidase IV specificity and their roles as anti-inflammatory agents, anticoagulants, and anti-tumor agents.Type: GrantFiled: April 28, 1994Date of Patent: August 6, 1996Assignee: Georgia Tech Research Corp.Inventors: James C. Powers, Bogdan Boduszek, Jozef Oleksyszyn
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Patent number: 5536710Abstract: This invention relates to bisphosphoryl hydrazine compounds and to compositions thereof which are useful as pesticides. The compounds of this invention are effective against soil insects, especially the corn rootworm.Type: GrantFiled: June 6, 1995Date of Patent: July 16, 1996Assignee: Rohm and Haas CompanyInventors: Richard M. Jacobson, Luong T. Nguyen
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Patent number: 5536709Abstract: Compound of formula (I): ##STR1## in which R.sub.1, R.sub.2 and R.sub.3, which are identical or different, represent hydrogen or halogen or alkyl, nitro, cyano or aminosulfonyl, or alternatively, when two of them are located on adjacent carbons, form, with the carbon atoms to which they are attached, (C.sub.3 -C.sub.7) cycloalkyl ring or substituted or unsubstituted benzene ring,R.sub.4 represents hydrogen, linear or branched (C.sub.1 -C.sub.6) alkyl, substituted or unsubstituted phenyl or a group ##STR2## in which R.sub.6 and R.sub.7, which are identical or different, represent hydrogen or substituted or unsubstituted, linear or branched (C.sub.1 -C.sub.6) alkyl,R.sub.5 represents hydrogen, hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy, phenoxy, mercapto, linear or branched (C.sub.1 -C.sub.6) alkylthio, substituted or unsubstituted, linear or branched (C.sub.1 -.sub.6) alkyl, substituted or unsubstituted phenyl or substituted or unsubstituted amino; or a group ##STR3## in which R.sub.6 and R.sub.Type: GrantFiled: August 30, 1994Date of Patent: July 16, 1996Assignee: Adir et CompagnieInventors: Alex Cordi, Patrice Desos, Jean Lepagnol
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Patent number: 5510338Abstract: The present invention pertains to antagonists of excitatory amino acid receptors, their method of preparation as well as compositions pertaining to them, which have the general formula: ##STR1## wherein n is 0, 1, 2, or 3; R1 and R.sub.2 are selected from the group consisting of hydrogen, halogen, halomethyl, nitro, amino, alkoxy, hydroxyl, hydroxymethyl, C.sub.1 to C.sub.6 lower alkyl and C.sub.7 to C.sub.12 higher alkyl, aryl and aralkyl; and the pharmaceutically acceptable salts thereof.Type: GrantFiled: June 14, 1994Date of Patent: April 23, 1996Assignee: Guilford Pharmaceuticals Inc.Inventor: Gregory S. Hamilton
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Patent number: 5508403Abstract: An agent for enhancing the drug effects of an antitumor drug, which comprises a compound of the formula I: ##STR1## or a pharmaceutically acceptable salt of the compound.Type: GrantFiled: June 5, 1995Date of Patent: April 16, 1996Assignee: Nissan Chemical Industries Ltd.Inventors: Shin-ichi Akiyama, Ryozo Sakoda, Kiyotomo Seto, Norimasa Shudo
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Patent number: 5484780Abstract: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their methods of use for antagonizing angiotensin II receptors in mammals.Type: GrantFiled: December 14, 1994Date of Patent: January 16, 1996Assignee: Eli Lilly and CompanyInventors: Donald B. Boyd, Kenneth L. Hauser, Sherryl L. Lifer, Winston S. Marshall, Alan D. Palkowitz, William Pfeifer, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, Kumiko Takeuchi, K. Jeff Thrasher, Celia A. Whitesitt
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Patent number: 5480568Abstract: Alkyl aryl sulfones are disclosed which are useful as high temperature and magnetic recording media lubricants. Also disclosed are lubricating mixtures containing the alkyl aryl sulfones, magnetic recording media containing the alkyl aryl sulfones, and a process for lubricating the magnetic recording media with the alkyl aryl sulfones.Type: GrantFiled: July 22, 1994Date of Patent: January 2, 1996Assignee: The Dow Chemical CompanyInventors: Chester E. Pawloski, Bassam S. Nader
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Patent number: 5463059Abstract: A process for preparing compounds of the formula ##STR1## where a, b, c, R.sub.1, R.sub.2, and R.sub.3 are as defined herein including the step of alkylating a phenol of formula ##STR2## with an acetylene of formula ##STR3## where X is chlorine; bromine; --OC(O)--R.sub.5, where R.sub.5 is alkyl, aryl or substituted aryl; or --OCO.sub.2 R.sub.6, where R.sub.6 is alkyl or ##STR4## in the presence of a catalytic amount of a cuprous or cupric salt. The compounds of formula I are intermediates useful in the preparation of pyranyl cyanoguanidine derivatives.Type: GrantFiled: October 1, 1993Date of Patent: October 31, 1995Assignee: E. R. Squibb & Sons, Inc.Inventors: Jollie D. Godfrey, Jr., Richard H. Mueller, Thomas C. Sedergran, Nachimuthu Soundararajan
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Patent number: 5463071Abstract: Compounds of the formula ##STR1## wherein X.sub.1 to X.sub.5 are as defined herein, the tautomers, the stereoisomers including the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases. The compounds are useful for inhibiting undesirable cell aggregation.Type: GrantFiled: November 8, 1993Date of Patent: October 31, 1995Assignee: Dr. Karl Thomae GmbHInventors: Frank Himmelsbach, Guenter Linz, Volkhard Austel, Helmut Pieper, Thomas Mueller, Johannes Weisenberger, Elke Seewaldt-Becker
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Patent number: 5442101Abstract: The invention relates to novel methylenebisphosphonic acid ester amide derivatives of general formula (I), in which formula W.sup.1, W.sup.2, W.sup.3 and W.sup.4 are independently the group OR.sup.1 or the group NR.sup.2 R.sup.3 wherein R.sup.1, R.sup.2 and R.sup.3 independently are hydrogen or straight or branched, optionally unsaturated C.sub.1 -C.sub.22 -alkyl, optionally substituted, optionally unsaturated C.sub.3 -C.sub.10 -cycloalkyl, aryl, aralkyl or silyl SiR.sub.3, or the groups R.sup.2 and R.sup.3 form together with the adjacent nitrogen atom a 3 to 10-membered saturated, partly saturated or aromatic heterocyclic ring, wherein in addition to the nitrogen atom, there may be one or two heteroatoms from the group N, O and S, provided that in formula (I) at least one of the groups W.sup.1, W.sup.2, W.sup.3 and W.sup.4 is hydroxy and at least one of the groups W.sup.1, W.sup.2, W.sup.3 and W.sup.4 is amino group NR.sup.2 R.sup.3, Q.sup.1 and Q.sup.Type: GrantFiled: October 20, 1993Date of Patent: August 15, 1995Assignee: Leiras OyInventors: Hannu Hanhijarvi, Heikki Nupponen, Jouko Vepsalainen, Esko Pohjala
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Patent number: 5436245Abstract: Hypotensive activity is exhibited by new phosphonate substituted amino or imino acids of the formula ##STR1## isomeric mixtures thereof and pharmaceutically acceptable salts thereof, wherein:X is an imino or amino acid of the formula ##STR2##Type: GrantFiled: November 17, 1993Date of Patent: July 25, 1995Assignee: E. R. Squibb & Sons, Inc.Inventor: Donald S. Karanewsky
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Patent number: 5410060Abstract: Arenebisphosphine oxides of the general formula ##STR1## where R.sup.1 to R.sup.4 independently of one another are each hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.5 -C.sub.10 -aryl, C.sub.5 -C.sub.12 -aryloxy or C.sub.7-C.sub.14 -arylalkoxy, R.sup.5 and R.sup.6 independently of one another may each be C.sub.1 -C.sub.6 -alkyl, C.sub.5 -C.sub.10 -cycloalkyl or C.sub.5 -C.sub.12 -aryl, each of which may furthermore contain one or two nitrogen or sulfur atoms in the ring system or carry one or two halogen atoms or C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -alkoxy groups as substituent on the ring system, or C.sub.1 -C.sub.6 -alkoxy, C.sub.3 -C.sub.8 -alkoxyalkoxy, C.sub.5 -C.sub.12 -aryloxy or C.sub.7 -C.sub.14 -arylalkoxy, or R.sup.5 and R.sup.6 together form a bridge of 2 to 10 carbon atoms, in which some of the carbon atoms may furthermore be part of an aromatic ring.Type: GrantFiled: December 2, 1993Date of Patent: April 25, 1995Assignee: BASF AktiengesellschaftInventors: Jochen Schroeder, Wolfgang Siegel, Matthias Lokai
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Patent number: 5393754Abstract: Insecticidal, acaricidal or nematocidal compositions which comprise a series of organophosphorus compounds represented by the following representative structural formulae: ##STR1## show excellent effect for controlling harmful insects, mites and nematodes, do not give off a bad or irritating smell and exhibit very low toxicity to warm-blooded animals.Type: GrantFiled: September 9, 1993Date of Patent: February 28, 1995Assignee: Agro-Kanesho Co., Ltd.Inventors: Katsumi Nanjo, Akinori Kariya, Shinya Henmi, Hideyo Fujii, Syuichi Usui
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Patent number: 5393748Abstract: Novel pharmacologically active methylenebisphosphonates having formula (I) wherein R.sup.1 -R.sup.4 independently are C.sub.1 -C.sub.10 -alkyl, C.sub.3 -C.sub.10 -cycloalkyl, aryl, aralkyl, silyl SiR.sub.3 or hydrogen, whereby in formula (I) at least one of the groups R.sup.1 -R.sup.4 is hydrogen and at least one of the groups R.sup.1 -R.sup.4 is different from hydrogen, Q.sup.1 is hydrogen, hydroxyl, halogen, amino NH.sub.2, or OR'.sub.1, wherein R'.sub.1 is C.sub.1 -C.sub.4 -alkyl or acyl, Q.sup.2 is the group (.alpha.) wherein Y is a six-membered heterocyclic group, or a carbocyclic aromatic group, X is a bond, O, S or NR'", wherein R'" is hydrogen, lower alkyl, or acyl, n is the integer 0 to 6, and R' and R" are hydrogen or lower alkyl provided that as a ring atom of the ring Y and/or a chain atom of the group X, there is always at least one heteroatom from the group O, N and S, including the steroisomers and the salts of the compounds.Type: GrantFiled: October 20, 1993Date of Patent: February 28, 1995Assignee: Leiras OyInventors: Esko Pohjala, Marjaana Heikkila-Hoikka, Hannu Nikander, Hannu Hanhijarvi
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Patent number: 5368985Abstract: Bisacylphosphine sulfides of formula I ##STR1## wherein R.sub.1 is unsubstituted C.sub.1 -C.sub.18 or C.sub.1 -C.sub.8 alkyl which is substituted by phenyl, --CN, C.sub.1 -C.sub.12 alkoxy or halogen, C.sub.2 -C.sub.18 alkenyl, unsubstituted C.sub.5 -C.sub.8 cycloalkyl or C.sub.5 -C.sub.8 cycloalkyl which is substituted by C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 alkoxy or halogen, unsubstituted C.sub.6 -C.sub.12 aryl or C.sub.6 -C.sub.12 aryl which is substituted by halogen, C.sub.1 -C.sub.12 alkyl or C.sub.1 -C.sub.12 alkoxy, or a 5- or 6-membered aromatic heterocyclic radical which contains oxygen, sulfur and/or nitrogen and is unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, andR.sub.2 and R.sub.3 are each independently of the other unsubstituted C.sub.1 -C.sub.18 alkyl or C.sub.1 -C.sub.8 alkyl which is substituted by phenyl, halogen or C.sub.1 -C.sub.12 alkoxy, C.sub.2 -C.sub.6 alkenyl, unsubstituted C.sub.5 -C.sub.8 cycloalkyl or C.sub.5 -C.sub.Type: GrantFiled: February 28, 1994Date of Patent: November 29, 1994Assignee: Ciba-Geigy CorporationInventors: Werner Rutsch, Gebhard Hug, Manfred Kohler
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Patent number: 5360563Abstract: There are disclosed compounds of formulae I and Ia ##STR1## wherein R.sub.1 and R.sub.2 are each independently of the other C.sub.1 -C.sub.13 alkyl which may be interrupted by oxygen, C.sub.5 -C.sub.6 cycloalkyl or, together with the linking N-atom, are a group of formula ##STR2## R is hydrogen or methyl, R.sub.3 is hydrogen or C.sub.1 -C.sub.13 alkyl, andR.sub.4 and R.sub.5 are each independently of the other hydrogen, C.sub.1 -C.sub.18 alkyl which may be interrupted by oxygen, C.sub.5 -C.sub.6 cycloalkyl or, together with the linking N-atom, are a group of formula ##STR3## withe proviso that R.sub.3, R.sub.4 and R.sub.5 are not simultaneously hydrogen and HNR.sub.1 R.sub.2 are not identical with NR.sub.3 R.sub.4 R.sub.5.The compounds are suitable for use as lubricant additives.Type: GrantFiled: May 27, 1993Date of Patent: November 1, 1994Assignee: Ciba-Geigy CorporationInventors: Horst Zinke, Rolf Schumacher
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Patent number: 5354742Abstract: The invention is directed to a pesticide composition comprising free flowing, essentially spherical, water-dispersible granules wherein said water-dispersible granules are from about 150 to about 850 microns in diameter; wherein said granules contain up to about 8.0% by weight moisture; wherein each individual water-dispersible granule is an aggregation of individual spherical microcapsules which contain at least one water-insoluble pesticide within a polymeric shell wall; and wherein said water-dispersible granule disintegrates upon contact with water to release said individual microcapsules.The invention also relates to dry flowable pesticidal formulations of the above water-dispersible granules, together with formulation adjuvants.The invention is further directed to a process for preparing a water-dispersible granule by spary drying an aqueous suspension comprising discrete microcapsules containing at least one water-insoluble pesticide within a polymeric shell wall suspended in an aqueous liquid.Type: GrantFiled: October 14, 1988Date of Patent: October 11, 1994Assignee: Monsanto CompanyInventors: John M. Deming, John M. Surgant, Sr.
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Patent number: 5344930Abstract: Compounds of the general formula: ##STR1## are useful as surfactants in the preparation of fluorocarbon emulsions, which can be used as oxygen-carrying blood substitutes, and for many other therapeutic and diagnostic applications. They are further useful in liposomal formulations which are themselves therapeutic agents or provide a vehicle for such agents.Type: GrantFiled: November 8, 1993Date of Patent: September 6, 1994Assignee: Alliance Pharmaceutical Corp.Inventors: Jean G. Riess, Francois Jeanneaux, Marie-Pierre Krafft, Catherine Santaella, Pierre Vierling
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Patent number: 5328623Abstract: There are disclosed compositions comprising: A) an organic material which is susceptible to thermal, oxidative and/or light-induced degradation, and B) at least one compound of formula I and/or II, ##STR1## wherein R.sub.0 is hydrogen, C.sub.1 -C.sub.12 alkyl, C.sub.5 -C.sub.12 cycloalkyl, C.sub.2 -C.sub.12 alkenyl, phenyl-C.sub.1 -C.sub.4 alkyl, --CO--R.sub.5 or --CO--OR.sub.5, R.sub.1 is hydrogen, methyl, ethyl or R.sub.1 together with R.sub.2 are ##STR2## R.sub.2 is hydrogen, methyl, ethyl or R.sub.2 together with R.sub.1 are ##STR3## R.sub.3 is hydrogen, methyl, ethyl or R.sub.3 together with R.sub.4 are ##STR4## R.sub.4 is hydrogen, methyl, ethyl or R.sub.4 together with R.sub.3 are ##STR5## R.sub.5 is C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.12 cycloalkyl, phenyl-C.sub.1 -C.sub.4 alkyl or phenyl, R.sub.6 and R.sub.7 are each independently of the other hydrogen, C.sub.1 -C.sub.12 alkyl, C.sub.5 -C.sub.12 cycloalkyl, phenyl or phenyl-C.sub.1 -C.sub.4 alkyl, R.sub.8 is C.sub.1 -C.sub.Type: GrantFiled: August 10, 1992Date of Patent: July 12, 1994Assignee: Ciba-Geigy CorporationInventor: Peter Nesvadba
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Patent number: 5280123Abstract: Insecticidal, acaricidal or nematocidal compositions which comprise organophosphorus compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each represents a C.sub.1 to C.sub.4 alkyl group;X represents NH or N--R.sup.4 wherein R.sup.4 represents an alkyl; an alkenyl; an alkynyl; a phosphoric acid ester radical; a cyano group; a group of formula (II): ##STR2## (wherein R.sup.5 represents an alkyl or alkylamino group); or a group of the formula: --(R.sup.6).sub.n --CO--R.sup.7 (wherein n is 0 or 1; R.sup.6 represents a methylene or an ethylene group; and R.sup.7 represents an alkyl, an alkoxy, an alkylthio group, an alkylamino group or a hydrogen atom);Z represents N--R.sup.8 (wherein R.sup.8 represents a nitro group, a cyano group, an alkylsulfonyl group, a tosyl group or an alkylcarbonyl group) or a group represented by the formula: C(CN)R.sup.9 (wherein R.sup.9 represents a cyano group or an alkoxycarbonyl group); andA represents an ethylene group which may be substituted with C.sub.1 to C.sub.Type: GrantFiled: July 5, 1991Date of Patent: January 18, 1994Assignee: Agro-Kanesho Co., Ltd.Inventors: Katsumi Nanjo, Akinori Kariya, Shinya Henmi
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Patent number: 5268479Abstract: A process is specified for the preparation of tertiary phosphines of the formulaR'PR.sub.2 or R.sub.2 P--[CH.sub.2 ].sub.3 --PR.sub.2in which R is an aryl, pyridyl or arylsulfonic acid group and R' is an aryl, pyridyl, arylsulfonic acid or n-butyl group, which comprises reacting phosphines of the formulaH.sub.n PR".sub.3-n or H.sub.2 P--[CH.sub.2 ].sub.3 --PH.sub.2in which R" is hydrogen or an n-butyl, aryl or pyridyl group and n is 1 or 2 with a halogen compound of the formulaX-R,in which R has the abovementioned meaning and X is fluorine, chlorine or bromine, in the presence of powdered potassium hydroxide and dimethyl sulfoxide and/or dimethoxyethane at temperatures between 0 and 100.degree. C., at least 1 mol of potassium hydroxide being used per mole of halogen compound.Type: GrantFiled: December 2, 1992Date of Patent: December 7, 1993Assignee: Hoechst AktiengesellschaftInventors: Othmar Stelzer, Klaus-Peter Langhans, Norbert Weferling
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Patent number: 5254543Abstract: Sulphonylbenzyl-substituted pyridones can be prepared by reacting pyridones with sulphonylbenzyl compounds. The sulphonylbenzyl-substituted pyridones can be employed as active compounds in medicaments, in particular for the treatment of arterial hypertension and atherosclerosis.Type: GrantFiled: February 18, 1993Date of Patent: October 19, 1993Assignee: Bayer AktiengesellschaftInventors: Rudolf Hanko, Walter Hubsch, Jurgen Dressel, Peter Fey, Thomas Kramer, Ulrich Muller, Matthias Muller-Gliemann, Martin Beuck, Stanislav Kazda, Claudia Hirth-Dietrich, Andreas Knorr, Johannes-Peter Stasch, Stefan Wohlfeil, Ozkan Yalkinoglu
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Patent number: 5247081Abstract: Processes for the preparation of biotinylated polynucleotides and analogues thereof and protected intermediate products for use in such processes are described and claimed. The processes may be conveniently used in the automated synthesis of biotinylated polynucleotide on a DNA synthesizer. The polynucleotides so prepared may be used as labelled probes e.g. as diagnostic tools for clinical and research uses.Type: GrantFiled: August 23, 1988Date of Patent: September 21, 1993Assignee: Imperial Chemical Industries PLCInventor: Michael D. Edge
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Patent number: 5245039Abstract: A process for the optical resolution of racemic 1,4-dihydropyridines, containing isothioureido groups. Salification of racemic isothioureas with optically active acids produces diasteroisomeric mixtures of isothiouronium salts, that, using conventional techniques, are separated in the individual components to give optically pure isothioureides of 1,4-dihydropyridines and salts thereof with conventional acids. Said optically pure 1,4-dihydropyridines can then be subjected to desulphuration and to different transformations to give to other enantiomerically pure and therapeutically useful 1,4-dihydropyridines.Type: GrantFiled: August 14, 1991Date of Patent: September 14, 1993Assignee: Boehringer Mannheim ItaliaInventors: Carmelo A. Gandolfi, Marco Frigerio, Carlo Riva, Andrea Zaliani, Giorgio Long, Roberto D. Domenico
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Patent number: 5212304Abstract: The compounds of the invention include novel linking agents comprising 2-substituted-3-protected-1,3,2-oxazaphosphacycloalkanes and their phosphoramidite precursors. The compounds of the invention further include conjugates of the above linking agents with oligonucleotides and polymer supports. The compounds of the present invention are useful for linking organic moieties, such as fluorescent or chromogenic dyes, to polymer supports and oligonucleotides, particularly single- and double-stranded DNA and RNA fragments.Type: GrantFiled: July 8, 1988Date of Patent: May 18, 1993Assignee: Applied Biosystems, Inc.Inventors: Steven Fung, Sam L. Woo, Lloyd M. Smith
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Patent number: 5189169Abstract: Herbicides having the formula ##STR1## in which X is oxygen or sulfur; and if X is sulfur, R.sub.1 is C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.6 cycloalkyl, allyl, phenyl, tolyl, chlorophenyl, 3,4-dichlorophenyl, or phen-(C.sub.1 -C.sub.2)alkyl; R.sub.2 is C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkoxyalkyl, or allyl; R.sub.3 is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxyalkyl, pyridyl, phenyl or substituted phenyl in which the substituents are halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, nitro and/or cyano; or R.sub.2 and R.sub.3 taken together form an alkylene chain having from 2 to 6 carbon atoms optionally substituted by up to two C.sub.1 -C.sub.4 alkyl groups; if R.sub.3 is alkyl or alkoxyalkyl, then R.sub.4 and R.sub.5 are each C.sub.2 -C.sub.4 alkyl; if R.sub.3 is phenyl, substituted phenyl or pyridyl, then R.sub.4 and R.sub.5 are C.sub.2 -C.sub. 6 alkyl, phenyl or substituted phenyl; or R.sub.3 and R.sub.Type: GrantFiled: November 12, 1991Date of Patent: February 23, 1993Assignee: Imperial Chemical Industries PLCInventor: David B. Kanne
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Patent number: 5130303Abstract: Compounds of the formula (I): ##STR1## in which the nitrogen-containing hetero ring portion is a 1,4-dihydropyridine ring or a pyridine ring, R.sup.1 is only present when the nitrogen-containing hetero ring is a 1,4-dihydropyridine ring, and Z is either a CO.sub.2 R.sup.8 group or a group of the formula (II): ##STR2## in which R.sup.4 and R.sup.5 may be the same or different and together may form one divalent group, are effective agents for enhancing the antitumor effect or antitumor drugs.Type: GrantFiled: July 15, 1991Date of Patent: July 14, 1992Assignee: Nissan Chemical Industries Ltd.Inventors: Shin-ichi Akiyama, Ryozo Sakoda, Kiyotomo Seto, Norimasa Shudo
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Patent number: 5128327Abstract: There are disclosed compounds, containing a pyridine, pyrazine or pyrimidine functionality on the lower ring of Formula I, which are useful as angiotensin II antagonists.Type: GrantFiled: March 25, 1991Date of Patent: July 7, 1992Assignee: Merck & Co., Inc.Inventors: Prasun K. Chakravarty, Malcolm MacCross, Nathan Mantlo, Thomas F. Walsh
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Patent number: 5118805Abstract: Novel compositions of phosphoroustriscaprolactams, including tris(caprolactyl)phosphite which may be produced in accordance with the methods disclosed, finding particular utility as catalysts for esterification and other condensation reactions.Type: GrantFiled: April 22, 1991Date of Patent: June 2, 1992Assignee: Allied-Signal Inc.Inventors: Jeffrey H. Glans, Murali K. Akkapeddi
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Patent number: 5104863Abstract: This invention relates to pyrindine-diphosphonic acid derivatives which are useful in treating or preventing diseases characterized by abnormal calcium and phosphate matabolism, in particular those which are characterized by abnormal bone metabolism. This invention further relates to pharmaceutical compositions which contain the novel compounds of the present invention, and to a method of treating or preventing diseases characterized by abnormal calcium and phosphate metabolism utilizing a compound of the present invention.Type: GrantFiled: July 3, 1990Date of Patent: April 14, 1992Assignees: The Procter & Gamble Company, The Procter & Gamble CompanyInventors: James J. Benedict, Karen Y. Johnson, James J. Benedict, Karen Y. Johnson
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Patent number: 5095020Abstract: The invention relates to a group of new .beta.-carbolines, their bio-isosteric benzofuran and benzothiophene analogues, and to the preparation of these compounds.The new compounds can be represented by the formula ##STR1## wherein R, R.sub.1 and R.sub.2 are hydrogen, or R+R.sub.1 or R.sub.1 +R.sub.2 form a saturated heterocyclic ring having 5 or 6 ring atoms, which comprise 1 or 2 oxygen atoms;R.sub.3 is hydrogen, or hydroxy optionally derivatised with a sugar radical the 4,6-hydroxy groups of which are acetalised with an -ylidene group;R.sub.4 is a group of the formula --C(R.sub.11).sub.2 --X--R.sub.12, wherein the groups R.sub.11 are hydrogen, or both groups R.sub.11 together represent a double-bonded keto oxygen atom, X is oxygen or a group NR.sub.14, wherein R.sub.14 is hydrogen or alkyl having 1-4 C-atoms, and R.sub.12 is hydrogen, alkyl having 1-4 C-atoms, alkanoyl having 1-4 C-atoms, the carbamoyl group or mono- or dialkylcarbamoyl group having 1-4 C-atoms per alkyl group;R.sub.Type: GrantFiled: August 24, 1989Date of Patent: March 10, 1992Assignee: Duphar International Research B.V.Inventors: Antonius Hulkenberg, Ineke Van Wijngaarden
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Patent number: 5075303Abstract: Pyridine derivatives of formula ##STR1## their heteroaromatic N-oxides and their pharmaceutically acceptable acid addition salts are disclosed. In the formula z is 0, 1 and 2 and R, R.sup.1, R.sup.2 and R.sup.2 have specified meanings. The compounds exhibit activity as 5-HT.sub.1A agonists, antagonists or partial agonists and are useful for the treatment of CNS disorders e.g. anxiety, as antihypertensives and in treating anorexia.Type: GrantFiled: April 6, 1990Date of Patent: December 24, 1991Assignee: John Wyeth & Brother LimitedInventors: Ian A. Cliffe, Howard L. Mansell, Richard S. Todd, Alan C. White
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Patent number: 5068340Abstract: Glycerol derivatives having at least one heterocyclic group on the 1 or 2 position are PAF antagonists which may be used to treat asthma, inflammation and shock.Type: GrantFiled: June 16, 1989Date of Patent: November 26, 1991Assignee: Sankyo Company, LimitedInventors: Norio Nakamura, Hiroyuki Koike, Takeshi Oshima
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Patent number: 5061813Abstract: Novel compounds are disclosed having the formula ##STR1## and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are as defined herein. These compounds are useful, for example, as cardiovascular agents and especially as anti-ischemic agents.Type: GrantFiled: April 2, 1990Date of Patent: October 29, 1991Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 5059687Abstract: A process for the condensation of imides and alcohols or amines to ester acyl lactams, ester amide acyl lactams or amide acyl lactams by reacting a polyol or polyamine in the liquid phase with an acyl lactam compound is disclosed.Type: GrantFiled: April 12, 1990Date of Patent: October 22, 1991Assignee: Stamicarbon B.V.Inventors: Christiaan Schroder, Albert A. Van Geenen, Josefina M. A. Schiffer
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Patent number: 5036059Abstract: 1,4-Dihydropyridine-3-carboxylate derivatives are produced having vasodilating and hypotensive action.Type: GrantFiled: April 17, 1985Date of Patent: July 30, 1991Assignee: Nippon Shinyaku Company, LimitedInventors: Kiyoshi Kimura, Iwao Morita