2-position Substituent Contains Nitrogen, Other Than As Nitro Or Nitroso Patents (Class 548/238)
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Publication number: 20010044546Abstract: The invention is drawn to novel transition metal catalysts for the practical synthesis of important chiral molecules. The transition metal catalysts comprise chiral ligands based on chiral amine oxazolinyl ligands. The invention includes methods of making the catalysts, and methods of performing reactions using the catalysts.Type: ApplicationFiled: May 4, 2001Publication date: November 22, 2001Applicant: The Penn State Research FoundationInventor: Xumu Zhang
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Patent number: 6306967Abstract: A solid, oxazoline-terminated, urethane-functional polyaddition compound having a melting point ranging from 40-130° C. and a free NCO content of less than 3% by weight, consisting essentially of a reaction product of a) at least one at least difunctional polyisocyanate and b) at least one hydroxy- or amino-functional oxazoline derivative, the ratio of NCO to OH equivalents ranging from 0.8:1.2 to 1.2:0.8.Type: GrantFiled: September 13, 1999Date of Patent: October 23, 2001Assignee: Degussa-Hüls AktiengesellschaftInventors: Emmanouil Spyrou, Andreas Wenning
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Patent number: 6255493Abstract: The invention is drawn to transition metal catalysts for the practical synthesis of important chiral molecules. The transition metal catalysts comprise chiral ligands based on chiral amine oxazolinyl ligands. The invention includes methods of making the catalysts, and methods of performing reactions using the catalysts.Type: GrantFiled: November 12, 1998Date of Patent: July 3, 2001Assignee: The Penn State Research FoundationInventor: Xumu Zhang
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Patent number: 6235901Abstract: A novel compound having the formula: wherein R is an alkyl group containing 1-5 carbon atoms or an aryl, substituted aryl, substituted or unsubstituted heteroaryl, alkyl-aryl, alkylether-aryl or O; R1 and R2 are hydrogen or a methyl group; X is O, NH, NR′ wherein R′ is an alkyl group containing 1-5 carbon atoms, or O—R″ or NR″ wherein O—R″ is O-alkyl-O or O-alkyl, NR″ is O-alkyl-ONH, wherein each instance alkyl contains 1-5 carbon atoms and n is 0 or 1. The compound of this invention is useful as a monomer which can be polymerized and/or copolymerized by catonic polymerization. Polymers and copolymers produced in this invention can be crosslinked and are useful in coatings, inks, overprint varnishes, and surface treatment applications.Type: GrantFiled: May 6, 1999Date of Patent: May 22, 2001Assignee: S. C. Johnson Commercial Markets, Inc.Inventors: Bill M. Culbertson, David L. Trumbo
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Patent number: 6207693Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc. and represented by general formula (I): wherein R1 is aryl optionally substituted with lower alkoxy, etc., R2 is lower alkyl, etc., R3 is hydrogen, etc., A is NH, etc., E is etc., X is —CH═CH—, —CH═N—, or S, and Y is a condensed heterocyclic group, etc., and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.Type: GrantFiled: June 2, 1999Date of Patent: March 27, 2001Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Hitoshi Sawada, Yuki Sawada, Teruo Oku
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Patent number: 6190580Abstract: Photochromic diaryl-2H-naphthopyran structures, which dye photochromically well at room temperature, lighten up quickly when incorporated into ophthalmic lenses, possess longevity, and due to their special structure, have a reduced tendency of the molecules to migrate in plastics.Type: GrantFiled: November 23, 1999Date of Patent: February 20, 2001Assignee: Optische Werke G. RodenstockInventors: Manfred Melzig, Herbert Zinner
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Patent number: 6147220Abstract: This invention provides a process for the preparation of a 5-methylene-1,3-oxazoline from an alkyl ketone by reacting the alkyl ketone with an acetylating agent and an acid catalyst in an appropriate solvent and at an appropriate temperature. The resulting 5-methylene-1,3-oxazoline can be chlorinated and subsequently hydrolyzed to form an .alpha.-chloroketone which is useful as a fungicide.Type: GrantFiled: May 15, 1998Date of Patent: November 14, 2000Assignee: Rohm and Haas CompanyInventors: Renee Caroline Roemmele, Heather Lynnette Rayle
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Patent number: 6140352Abstract: Disclosed herein are selective beta 3 adrenergic agonists represented by the following structural formula: ##STR1## The variables in the structural formula shown above are defined in the specification. Also disclosed are methods of using these compounds for agonizing the beta 3 adrenergic receptor in patients in need of such treatment, for example, patients in need of treatment for obesity or Type II diabetes.Type: GrantFiled: May 4, 1998Date of Patent: October 31, 2000Assignee: Eli Lilly and CompanyInventors: Thomas A. Crowell, Deborah A. Evrard, Charles D. Jones, Brian S. Muehl, Christopher J. Rito, Anthony J. Shuker, Andrew J. Thorpe, Kenneth J. Thrasher
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Patent number: 6054457Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.Type: GrantFiled: December 9, 1997Date of Patent: April 25, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Hitoshi Sawada, Kentaro Sato, Hirokazu Tanaka
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Patent number: 6051589Abstract: The invention relates to novel diphenyloxazoline derivatives of the formula (I) ##STR1## in which a) A represents tri- to pentasubstituted phenyl andB represents substituted phenyl orb) A represents mono- or disubstituted phenyl andB represents at least trisubstituted phenyl, but where at least one substituent is not fluorine, chlorine, bromine, C.sub.1 -C.sub.6 -alkyl or -alkoxy,to a number of processes for their preparation and to their use as pest control agents.Type: GrantFiled: July 9, 1996Date of Patent: April 18, 2000Assignee: Bayer AktiengesellschaftInventors: Johannes Kanellakopulos, Gerd Kleefeld, Udo Kraatz, Ulrike Wachendorff-Neumann, Christoph Erdelen, Andreas Turberg, Norbert Mencke
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Patent number: 6046227Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta..sub.3 receptor agonists useful in the treatment of Type II diabetes and obesity.Type: GrantFiled: December 4, 1998Date of Patent: April 4, 2000Assignee: Eli Lilly and CompanyInventors: Thomas Alan Crowell, Charles David Jones, Anthony John Shuker
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Patent number: 6036890Abstract: Photochromic diaryl-2H-naphthopyran structures, which dye photochromically well at room temperature, lighten up quickly when incorporated into ophthalmic lenses, possess longevity, and due to their spacial structures, have a reduced tendency of the molecules to migrate in plastics.Type: GrantFiled: July 31, 1998Date of Patent: March 14, 2000Assignee: Optische Werke G. RodenstockInventors: Manfred Melzig, Herbert Zinner
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Patent number: 6028089Abstract: The invention relates to new phenylthio-oxazoline derivatives of the formula (I) ##STR1## in which A represents optionally substituted phenyl;B represents optionally substituted phenyl;D represents hydrogen or alkyl; andn represents 0, 1 or 2;to a plurality of processes for their preparation, and to their use as pesticides.Type: GrantFiled: February 25, 1998Date of Patent: February 22, 2000Assignee: Bayer AktiengesellschaftInventors: Wolfgang Kramer, Ulrike Wachendorff-Neumann, Christoph Erdelen, Andreas Turberg, Norbert Mencke
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Patent number: 6005103Abstract: The present invention relates to novel tri- and tetrasubstituted pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The pyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized pyrones and of related structures.Type: GrantFiled: October 12, 1994Date of Patent: December 21, 1999Assignee: Warner-Lambert CompanyInventors: John Michael Domagala, Elizabeth Lunney, Kimberly Suzanne Para, Josyula Venkata Nagendra Vara Prasad, Bradley Dean Tait
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Patent number: 5990140Abstract: The invention relates to novel substituted oxazolines of the formula (I) ##STR1## in which A, B, D, E and G have the meaning given in the description,to a number of processes for their preparation and to their use as agents for combating pests.Type: GrantFiled: July 10, 1996Date of Patent: November 23, 1999Assignee: Bayer AktiengesellschaftInventors: Wolfgang Kramer, Reiner Fischer, Graham Holmwood, Hermann Hagemann, Ulrike Wachendorff-Neumann, Christoph Erdelen, Andreas Turberg, Norbert Mencke
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Patent number: 5977149Abstract: Cyclic amides of Formula (I) which are useful as fungicides wherein: A is O; S; N; NR.sup.5 ;or CR.sup.14--, G is C or N; W is O or S; X is OR.sup.1, S(O).sub.m R.sup.1 or halogen; R.sup.1, R.sup.2, and R.sup.5 are independently, in part, C.sub.1 -C.sub.6 alkyl; Y is, in part, --O--; --S(O).sub.n --,--CHR.sup.6 O--; or --CHR.sup.6 O--N.dbd.C(R.sup.7)--; Z is, in part, optionally substituted cycloalkyl, phenyl, pyridinyl, pyrimidinyl, or naphthyl; and R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.14, m, and n are defined in the disclosure, are disclosed.Type: GrantFiled: January 14, 1998Date of Patent: November 2, 1999Assignee: E. I. du Pont de Nemours and CompanyInventors: Richard James Brown, King-Mo Sun, Deborah Ann Frasier
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Patent number: 5859035Abstract: The present invention is directed to compounds which inhibit famesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting famesyl-protein transferase and the famesyl of the oncogene protein Ras.Type: GrantFiled: March 27, 1997Date of Patent: January 12, 1999Assignee: Merck & Co., Inc.Inventors: Neville J. Anthony, Robert P. Gomez, Steven D. Young
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Patent number: 5840912Abstract: The invention relates to new substituted pyrazol derivatives of general formula (I) in which: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have the meanings given in the description, agents with herbicidal action containing at least one compound of formula (I), and their use as herbicides.Type: GrantFiled: April 22, 1997Date of Patent: November 24, 1998Assignee: Hoechst Schering AgrEvo GmbHInventors: Jens Geisler, Helga Franke, Uwe Hartfiel, Michael Ganzer, Jurgen Bohner, Richard Rees
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Patent number: 5814648Abstract: Described herein are N-hydroxyurea compounds having the ability to inhibit the 5-lipoxygenase enzyme and having formula (I) and the pharmaceutically acceptable salts thereof. The variables are described herein. These compounds are useful in the treatment or alleviation of inflammatory diseases, allergy and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.Type: GrantFiled: November 5, 1997Date of Patent: September 29, 1998Assignee: Pfizer Inc.Inventors: Akemi Ando, Rodney William Stevens
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Patent number: 5770598Abstract: The present invention relates to heterocyclic compounds which have been found to have anti-tumour activity. More specifically, the invention concerns Pyrrolo ?3,2-b! carbazoles, 1H-Benzofuro ?3,2-.function.! indoles and 1H-?1! Benzothieno ?2,3-.function.! indoles, methods for their preparation, pharmaceutical formulations containing them and their use as anti-tumour agents.Type: GrantFiled: April 10, 1997Date of Patent: June 23, 1998Assignee: University College Cardiff Consultants LimitedInventors: David D. Miller, Paul Barraclough, Sadie Vile, Ann L. Walker, Patrick V. R. Shannon, Laddawan Chunchatprasert, Pierre P. M. Debont, Alan T. Hudson
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Patent number: 5750532Abstract: The disclosed invention is compounds represented by the formula ##STR1## and pharmacetically acceptable acid salts thereof, wherein each Z is independently tetiary butyl, phenyl, naphthyl or adamantyl; substituted phenyl, wherein the substituents are one or more of halogen, lower alkoxy, phenoxy, nitrile, nitro, phenylsulfonyl, loweralkyl-sulfonyl, oxazol-2-yl, lower alkanoyl, benzoyl, lower alkoxycarbonyl, lower alkyl, lower alkylthio, phenyl, phenylaminothiocarbonyl, or lower alkylaminothiocarbonyl, hydroxyiminoloweralkyl hydroxyloweralkyl or carbonyl; or 4 or 6 membered unsubstituted or substituted heterocyclic ring containing at least one nitrogen with the remaining member of the ring being at least one carbon, and optionally sulfur or oxygen,X and Y are each independently a bond, ##STR2## each Q is independently a divalent substituted or unsubstituted, straight or branched chain lower alkanediyl, lower alkanediyl-cycloalkanediyl-lower alkanediyl, lower alkenediyl, lower alkynediyl, phenylene, dihydrofuraType: GrantFiled: May 30, 1995Date of Patent: May 12, 1998Assignee: Schering CorporationInventors: Viyyoor M. Girijavallabhan, Ashit K. Ganguly, Patrick A. Pinto, Richard W. Versace
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Patent number: 5747540Abstract: Compounds such as ##STR1## or pharmaceutically acceptable salts thereof, are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: October 21, 1996Date of Patent: May 5, 1998Assignee: Merck & Co., Inc.Inventors: Craig A. Coburn, Randall W. Hungate, Richard C. A. Isaacs, Joseph P. Vacca, Mary Beth Young
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Patent number: 5696154Abstract: Provided are brefeldin A derivatives of the formula: ##STR1## wherein one of R.sub.1 and R.sub.2 is H and the other of R.sub.1 and R.sub.2 is a substituent group having 1 to 12 carbon atoms containing a basic nitrogen atom or a quaternary ammonium group, or a salt thereof. These derivatives exhibit good antitumor activity, and are administrable to human patients without the problems associated with brefeldin A.Type: GrantFiled: June 29, 1994Date of Patent: December 9, 1997Assignees: The United States of America as represented by the Department of Health and Human Services, Starks Associates, Inc.Inventors: Louis Malspeis, B. Rao Vishnuvajjala, Jeffrey G. Supko, Charles Theodore Kane, Jr.
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Patent number: 5650427Abstract: A compound of Formula I ##STR1## or pharmaceutically acceptable salts of Formula I, where R.sup.1 is H, C.sub.1 -C.sub.3 alkyl, --(CH.sub.2).sub.n CONH.sub.2 where n is 2 to 6, (CH2).sub.n -1-(4,4-dimethylpiperidine-2,6-dione-yl), or cyclopropylmethyl;R.sup.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl or combined with R.sup.1 to form a C.sub.3 -C.sub.8 cycloalkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.8 akynyl, (CH.sub.2).sub.n --X--Ar where X is O, S, or NH, 3,3,3-trifluoropropyl, --(CH.sub.2).sub.m --R.sup.9 where m is 2 or 3 and R.sup.9 is phenyl, 2-thiophenyl or 3-thiophenyl; R.sup.3 is hydrogen, C.sub.1 -C.sub.3 alkyl, 2,2,2-trifluoroethyl, 3,3,3-trifluoropropyl, formyl, CN, halogen, CH.sub.2 OR.sup.2, C(O)C(O)OR.sup.1, C(O)CO NR.sup.1 R.sup.2, --(CH.sub.2).sub.q --NR.sup.1 R.sup.2 where q is 0 to 5, C.dbd.NOR.sup.2, 2(4,5-dihydro)oxazolyl, or COR.sup.10 where R.sup.10 is H, R.sup.1, NR.sup.1 R.sup.2 or CF.sub.3 ; R.sup.4 is hydrogen, C.sub.1 -C.sub.Type: GrantFiled: June 2, 1995Date of Patent: July 22, 1997Assignee: The Upjohn CompanyInventors: Hakan Vilhelm Wikstrom, Per Arvid Emil Carlsson, Bengt Ronny Andersson, Kjell Anders Ivan Svensson, Stig Thomas Elebring, Nils Peter Stjernlof, Arthur Glenn Romero, Susanne R. Haadsma-Svensson, Chiu-Hong Lin, Michael Dalton Ennis
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Patent number: 5612359Abstract: Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols are defined as follows: R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each directly bonded to a ring carbon and are each independently(a) hydrogen;(b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z.sup.1, Z.sup.2 and Z.sup.3 ;(c) halo;(d) hydroxyl;(e) cyano;(f) nitro;(g) --C(O)H or --C(O)R.sup.5 ;(h) --CO.sub.2 H or --CO.sub.2 R.sup.5 ;(i) --Z.sup.4 --NR.sup.6 R.sup.7 ;--Z.sup.4 --N(R.sup.10)--Z.sup.5 --NR.sup.8 R.sup.9 ; or(k) R.sup.3 and R.sup.4 together may also be alkylene or alkenylene, either of which may be substituted with Z.sup.1, Z.sup.2 and z.sup.3, completing a 4- to 8-membered saturated, unsaturated or aromatic ring together with the carbon atoms to which they are attached; and the remaining symbols are as defined in the specification.Type: GrantFiled: June 7, 1995Date of Patent: March 18, 1997Assignee: Bristol-Myers Squibb CompanyInventor: Natesan Murugesan
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Patent number: 5556981Abstract: This invention provides novel heterocyclic derivatives, their pharmaceutical formulations, and their use for antagonizing angiotensin II receptors in mammals.Type: GrantFiled: May 30, 1995Date of Patent: September 17, 1996Assignee: Eli Lilly and CompanyInventors: Donald B. Boyd, Sherryl L. Lifer, Winston S. Marshall, Alan D. Palkowitz, William Pfeifer, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, K. Jeff Thrasher, Venkatraghaven Vasudevan, Celia A. Whitesitt
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Patent number: 5491201Abstract: Novel cyclic imino ether compositions containing one or more mesogenic moieties, when polymerized, result in products having improved properties.Type: GrantFiled: February 16, 1995Date of Patent: February 13, 1996Assignee: The Dow Chemical CompanyInventors: Robert E. Hefner, Jr., Jimmy D. Earls
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Patent number: 5466813Abstract: Imine dyes useful in photographic materials have the formula ##STR1## wherein R.sup.1, E.sup.1, E.sup.2, L.sup.1, L.sup.2, L.sup.3,D and m are defined as in the specification.Solid particle dispersions of dyes of formula (I) that contain at least one base-ionizable functional group such as carboxy, sulfonamido, or sulfamoyl are useful as filter dyes in photographic elements.Type: GrantFiled: July 20, 1993Date of Patent: November 14, 1995Assignee: Eastman Kodak CompanyInventors: Donald R. Diehl, Margaret J. Helber, Hugh Williamson
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Patent number: 5466687Abstract: The invention relates to arylidene-1-azacycloalkanes and arylalkyl-1-azacycloalkanes of the general formula ##STR1## (wherein n, m, p, A, W.sup.1, W.sup.2, X, Y, and R.sup.1 to R.sup.11 are as defined in claim 1) and the isomers, isomer mixtures and salts thereof, which have useful properties, in particular an inhibitory effect on cholesterol biosynthesis.Type: GrantFiled: March 25, 1994Date of Patent: November 14, 1995Assignee: Dr. Karl Thomae GmbHInventors: Roland Maier, Peter Muller, Eberhard Woitun, Rudolf Hurnaus, Michael Mark, Bernhard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
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Patent number: 5414121Abstract: Adducts containing mesogenic or rodlike moieties are prepared by reacting (1) at least one compound containing an average of more than one vicinal epoxide group per molecule with (2) at least one compound containing an average of more than one reactive hydrogen atom per molecule; with the proviso that at least one member of components (1) and (2) contains a mesogenic or rodlike moiety. These compounds are useful as curing agents for epoxy resins.Type: GrantFiled: September 8, 1993Date of Patent: May 9, 1995Assignee: The Dow Chemical CompanyInventors: Robert E. Hefner, Jr., Jimmy D. Earls
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Patent number: 5374654Abstract: The invention relates to carbacyclin derivatives of Formula I ##STR1## wherein the various substituents are defined herein, including, inter alia,if R.sub.2 is a hydrogen atom, their salts with physiologically compatible bases, their cyclodextrin clathrates, and their use as medicinal agents.Type: GrantFiled: April 21, 1993Date of Patent: December 20, 1994Assignee: Schering AktiengesellschaftInventors: Helmut Vorbruggen, Ulrich Klar, Bob Nieuweboer, Claus-Steffen Sturzebecher
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Patent number: 5292756Abstract: A series of non-peptide derivatives of the formula ##STR1## that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.Type: GrantFiled: March 25, 1992Date of Patent: March 8, 1994Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman
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Patent number: 5288748Abstract: A compound of Formula I ##STR1## or pharmaceutically acceptable salts of Formula I, where R.sup.1 is H, C.sub.1 -C.sub.3 alkyl, --(CH.sub.2).sub.n CONH.sub.2 where n is 2 to 6, (CH2).sub.n -1-(4,4-dimethylpiperidine-2,6-dione-yl), or cyclopropylmethyl;R.sup.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl or combined with R.sup.1 to form a C.sub.3 -C.sub.8 cycloalkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.8 akynyl, (CH.sub.2).sub.n --R"--Ar where R" is O, S, or NH, 3,3,3-trifluoropropyl, --(CH.sub.2).sub.m --R.sup.9 where m is 2 or 3 and R.sup.9 is phenyl, 2-thienyl or 3-thienyl; R.sup.3 is hydrogen, C.sub.1 -C.sub.3 alkyl, 2,2,2-trifluoroethyl, 3,3,3-trifluoropropyl, formyl, CN, halogen, CH.sub.2 OR.sup.2, C(O)C(O)OR.sup.1, C(O)CO NR.sup.1 R.sup.2, --(CH.sub.2).sub.q --NR.sup.1 R.sup.2 where q is 0 to 5, C.dbd.NOR.sup.2, 2(4,5-dihydro)oxazolyl, or COR.sup.10 where R.sup.10 is H, R.sup.1, NR.sup.1 R.sup.2 or CF.sub.3 ; R.sup.4 is hydrogen, C.sub.1 -C.sub.3 alkyl, cyclopropylmethyl, CF.Type: GrantFiled: July 1, 1992Date of Patent: February 22, 1994Assignee: The Upjohn CompanyInventors: Hakan V. Wikstrom, Per A. E. Carlsson, Bengt R. Andersson, Kjell A. I. Svensson, Stig T. Elebring, Nils P. Stjernlof, Arthur G. Romero, Susanne R. Haadsma-Svensson, Chiu-Hong Lin, Michael D. Ennis
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Patent number: 5276037Abstract: The invention concerns an aryl derivative of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl, naphthyl or a heterocyclic moiety, and X.sup.1 is oxy, thio, sulphinyl, sulphonyl, difluoromethylene, imino, (1-4C)alkylimino or optionally substituted (1-4C)alkylene, or X.sup.1 is a group of the formula--X.sup.4 --CR.sub.2 -- or --CR.sub.2 --X.sup.4 --whereinX.sup.4 is oxy, thio, sulphinyl, sulphonyl or carbonyl and each R is hydrogen, methyl or ethyl;each of Ar.sup.2 and Ar.sup.3 is optionally substituted phenylene;X.sup.2 is oxy, thio, sulphinyl or sulphonyl;R.sup.1 is (1-4C)alkyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.1 --X.sup.3 --A.sup.2 -- which together with the carbon atom to which A.sup.1 and A.sup.2 are attached define a ring having 5 to 7 ring atoms, wherein each of A.sup.1 and A.sup.2 is (1-3C)alkylene and X.sup.Type: GrantFiled: April 14, 1993Date of Patent: January 4, 1994Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Robert I. Dowell, Philip N. Edwards, Keith Oldham
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Patent number: 5210206Abstract: The present invention relates to a process for the preparation of a compound of the formula: ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, loweralkyl, loweralkoxy-substituted loweralkyl, lower alkenyl, lower alkynyl, cycloalkyl and cycloalkylalkyl; R.sub.2 is selected from the group consisting of hydrogen, loweralkyl, loweralkoxy-substituted loweralkyl, halogen and loweralkoxy; R.sub.3 is selected from hydrogen, loweralkyl, and halogen; R* and R** are independently selected from loweralkyl and P.sub.1 is hydrogen or an nitrogen-protecting group; or an acid addition salt thereof.Type: GrantFiled: January 10, 1992Date of Patent: May 11, 1993Assignee: Abbott LaboratoriesInventors: Howard E. Morton, Biswanath De, Daniel J. Kerkman
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Patent number: 5196544Abstract: This invention concerns polyiminoethers of general formula (I) in which A is an aliphatic, aromatic or araliphatic group containing 4 to 40 carbon atoms and n free valencies at various carbon atoms, x may assume values of 0 to 40, n has a value of 2, 3 or 4, Z is either a direct bond or the group CR.sup.5 R.sup.6, the substituents R.sup.1 to R.sup.6 independently of one another are H, alkyl or aryl containing up 8 carbon atoms, the substituent R.sup.7 is hydrogen, methyl or ethyl and Q is a phenylene group, which may be substituted by one or two methyl groups, or the group --CHR--M--, where R is selected from the group consisting of H, alkyl or alkenyl and M is selected from the group consisting of alkylene, alkenylene, arylene and alkarylene, and the parts R and M of the molecule independently of one another contain 0 to 12 carbon atoms and, in addition, may be substituted by a C.sub.1-3 alkoxy group. These compounds are made from polyisocyanates of formula A(NCO).sub.Type: GrantFiled: January 16, 1992Date of Patent: March 23, 1993Assignee: Henkel Kommanditgesellschaft auf AktienInventors: Brigitte Hase, Horst-Juergen Krause, William Fristad
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Patent number: 5162353Abstract: The invention relates to carbacyclin derivatives with general formula I: ##STR1## in which Y.sub.1 stands for the radical --CH.sub.2 --X--(CH.sub.2).sub.n --R.sub.1 or the radical ##STR2## n, 1 or 3, R.sub.1, the radical ##STR3## the radical ##STR4## R.sub.9 stands for the radical --(CH.sub.2).sub.m --R.sub.6 or the radical --(CH.sub.2).sub.m-o --[Z.sub.1 --(CH.sub.2).sub.m-p ].sub.x --[Z.sub.2 --(CH.sub.2).sub.m-q ].sub.y --R.sub.6,m=2-20,o, p, and q are less than or equal to 19,x, y=0, 1 or 2,Z.sub.1 stands for a cis--CH.dbd.CH group, a trans--CH.dbd.CH group of a --C.dbd.C group, and each of these groups must be separated at least by a methylene group from the C-9 carbon atom of the carbacyclin bicyclic compound,Z.sub.2 stands for oxygen, sulfur, an NH or an N methyl group,R.sub.6 stands for amino, methylamino, hydroxy, carboxy or mercapto,X an oxygen atom or a methylene group,Y.sub.2 hydrogen or fluorine,A a --CH.sub.2 --CH.sub.2, trans--CH.dbd.CH or --C.dbd.Type: GrantFiled: August 21, 1990Date of Patent: November 10, 1992Assignee: Schering AktiengesellschaftInventors: Helmut Vorbrueggen, Bob Nieuweboer, Claus-Steffen Stuerzebecher
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Patent number: 5140034Abstract: A class of 5-membered heterocyclic compounds having at least one heteroatom, substituted on the heterocyclic ring by an imidazolyl moiety, are useful in the treatment of psychotic disorders (e.g. schizophrenia and mania); anxiety; alcohol or drug withdrawal or dependence; pain; gastric stasis; gastric dysfunction (such as occurs with dyspepsia, peptic ulcer, reflux oesophagitis and flatulence); migraine, nausea and vomiting; movement disorders; and presenile and senile dementia.Type: GrantFiled: March 8, 1990Date of Patent: August 18, 1992Assignee: Merck Sharp & Dohme Ltd.Inventors: Raymond Baker, Christopher Swain, John Saunders
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Patent number: 5086184Abstract: N-Aryl benzamides wherein the aryl group is a nitrogen containing heterocycle are useful as selective herbicidal agents. Compositions containing the novel benzamides and a herbicidal method of selective weed control are disclosed.Type: GrantFiled: May 7, 1990Date of Patent: February 4, 1992Assignee: DowElancoInventor: Kenneth W. Burow, Jr.
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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: 5066664Abstract: Compounds of the formula ##STR1## where X is O or S; R.sub.1 is lower alkyl having 1 to 6 carbons; R.sub.2 is H, lower alkyl having 1 to 6 carbons; or OR.sub.2.sup.* where R.sub.2.sup.* is lower alkyl having 1 to 6 carbons; Y is O, S or NH; and R.sub.3 is H, lower alkyl having 1 to six carbons, or C(O)R.sub.3.sup.* where R.sub.3.sup.* is lower alkyl having 1 to 5 carbons, with the proviso that the YR.sub.3 group is not disposed in the ortho position on the benzene nucleus relative to the 2-amino group of the oxazoline or thiazoline heterocycle, are active in maintaining or reducing intraocular pressure in the mammalian eye, and are active as vasoconstrictors and capable of reducing or controlling intraocular bleeding of the mammalian eye.Type: GrantFiled: February 28, 1990Date of Patent: November 19, 1991Assignee: Allergan, Inc.Inventor: Charles Gluchowski
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Patent number: 5039677Abstract: (1H-azol-1-ylmethyl)substituted benzotriazole derivatives, compositions containing the same, and methods of treating estrogen dependent disorders.Type: GrantFiled: June 13, 1990Date of Patent: August 13, 1991Assignee: Janssen Pharmaceutica N.V.Inventors: Alfons H. M. Raeymaekers, Eddy J. E. Freyne, Josephus L. H. Van Gelder, Marc G. Venet
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Patent number: 5026866Abstract: The present invention relates to a new method of synthesis of 2,2'-bis.DELTA..sup.2 -oxazoline, which consists of three steps:in the first step,N,N'-bis-(2-hydroxyethyl)-oxamide (I) is reacted with hydrogen chloride and a nitrile of formula RCN in which R.dbd.H, alkyl, aryl, arylalkyl, alkylaryl, in order to yield the correspondingN,N'-bis-(2-iminoacyloxyethyl)oxamide.2HCl (II).In the second step, the compound (II) is pyrolyzed in order to yieldN,N'-bis-(2-chloroethyl)oxamide (III) which in the third step generates, by means of the treatment with a base, the desired product 2,2'-bis-.DELTA..sup.2 -oxazoline.Type: GrantFiled: December 21, 1989Date of Patent: June 25, 1991Assignee: Enichem Anic S.p.A.Inventors: Giuseppe Messina, Loreno Lorenzoni, Giovanna Chessa
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Patent number: 4981974Abstract: What is described herein are polymerizable pyrrolidonyl 4,5-unsubstituted oxazoline monomers, homopolymers thereof, and copolymers with other monomers. A preferred polymerizable monomer compound is 2-(1-methyl-2-pyrrolidon-4-yl)-2- oxazoline. The polymers herein have excellent hydrotropic properties thus increasing the water solubility of organic compounds previously considered as water insoluble, and exhibit complexation with water soluble consolutes.Type: GrantFiled: March 19, 1990Date of Patent: January 1, 1991Assignee: GAF Chemicals CorporationInventors: Gary . Dandreaux, Robert B. Login, John J. Merianos, Paul Garelick, Krystyna Plochocka, Max Negrin, Jenn S. Shih
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Patent number: 4971987Abstract: The invention also relates to carbacyclin derivatives of general formula I' ##STR1## wherein R.sub.9 is an alkyl group of 1-10 carbon atoms or the group --C.dbd.C--(CH.sub.2).sub.m --R.sub.6 whereinm is 1 to 16 andR.sub.6 is hydroxy on amino.Type: GrantFiled: March 7, 1988Date of Patent: November 20, 1990Assignee: Schering AktiengesellschaftInventors: Helmut Vorbrueggen, Bob Nieuweboer, Claus-Steffen Stuerzebecher, Ulrich Klar
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Patent number: 4959374Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, ester or amide thereif, wherein: Z represents a residue of a substituted or unsubstituted aryl group,X represents o or NR.sup.o wherein R.sup.0 represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, an alkanoyl group substituted or unsubstituted in the alkyl moiety, or an arylalkyl moiety substituted or unsubstituted in the aryl moiety,n represents an integer 1 or 2,m represents an integer 1 or 2,p represents an integer 2 or 3,andq represents an integer in the range of from 1 to 12; pharmaceutical compositions containing such compounds and the use of such compounds and compositions in medicine.Type: GrantFiled: July 6, 1989Date of Patent: September 25, 1990Assignee: Beecham Group P.L.C.Inventor: John M. Berge
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Patent number: 4933463Abstract: What is described herein are polymerizable pyrrolidonyl 4,5-unsubstituted oxazoline monomers, homopolymers thereof, and copolymers with other monomers. A preferred polymerizable monomer compound is 2-(1-methyl-2-pyrrolidon-4-yl)-2-oxazoline. The polymers herein have excellent hydrotropic properties thus increasing the water solubility of organic compounds previously considered as water insoluble, and exhibit complexation with water soluble cosolutes.Type: GrantFiled: May 8, 1989Date of Patent: June 12, 1990Assignee: GAF Chemicals CorporationInventors: Gary Dandreaux, Robert B. Login, John J. Merianos, Paul Garelick, Krystyna Plochocka, Max Negrin, Jenn S. Shih
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Patent number: 4889865Abstract: Mono, di and tri-esters of 1,8-dihydroxy-10-phenyl-9-anthrone or -9-anthranol have the formula ##STR1## wherein p is 0 or 1,(a) when p=0, t=1 and R.sub.2 represents hydrogen or --COR.sub.3,(b) when p=1, t=0 and R.sub.1 and R.sub.2 each independently represent hydrogen or --COR.sub.3,R.sub.3 represents linear or branched alkyl having 1-17 carbon atoms, cycloalkyl, phenyl or phenyl substituted by lower alkyl, lower alkoxy, halogen, a nitro function, --CF.sub.3 or a hydroxyl function, and mixtures of said esters. These esters are prepared by reacting 1,8-dihydroxy-10-phenyl-9-anthrone with an activated form of an acid. The esters are useful in human or veterinary medicine and in cosmetic compositions.Type: GrantFiled: February 21, 1989Date of Patent: December 26, 1989Assignee: Centre International de Recherches Dermatologiques C.I.R.D.Inventors: Braham Shroot, Gerard Lang, Jean Maignan, Serge Restle, Christopher Hensby, Michel Colin
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Patent number: 4866139Abstract: Poly(C.sub.5 -C.sub.9 lactone) adducts are made by reacting a C.sub.5 -C.sub.9 lactone with a post reacted hydrocarbyl substituted C.sub.4 -C.sub.10 monounsaturated dicarboxylic acid producing material, e.g., a polyisobutenyl succinic anhydride, which, in turn, preferably was made by reacting a polymer of a C.sub.2 to C.sub.10 monoolefin, preferably polyisobutylene, having a number average molecular weight of about 700 to 5,000, with a C.sub.4 to C.sub.10 monounsaturated acid, anhydride or ester, preferably maleic anhydride, such that there are 0.7 to 2.0 dicarboxylic acid producing moieties per molecular of said olefin polymer used in the reaction mixture, and then, post reacting the substituted acid, anhydride or ester with a polyol such as pentaerythritol or THAM. The resulting adducts are useful per se as oil soluble dispersant additives useful in fuel and lubricating compositions including concentrates containing the additives.Type: GrantFiled: October 7, 1986Date of Patent: September 12, 1989Assignee: Exxon Chemical Patents Inc.Inventors: Antonio Gutierrez, Robert D. Lundberg
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Patent number: 4864032Abstract: A process for the preparation of aryl hydrazines and indazoles by reacting organometallic regents with azodicarboxylates.Type: GrantFiled: July 2, 1987Date of Patent: September 5, 1989Assignee: Ortho Pharmaceutical CorporationInventor: James P. Demers