Patents Examined by Peter Davis
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Patent number: 5167695Abstract: Quinoline derivatives fused to a five-membered heterocyclic ring and of the formula ##STR1## where R.sup.1 is hydrogen, halogen, carboxyl or substituted or unsubstituted alkyl,Y is nitrogen or C--R.sup.2, whereR.sup.2 is hydrogen, halogen, hydroxyl, alkoxy, alkylthio, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted benzyl, phenethyl, phenyl or naphthyl, or a substituted or unsubstituted 5- or 6-membered heterocyclic ring with one or two heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen,X is oxygen or N--R.sup.3, R.sup.3 being hydrogen, substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl or subsituted or unsubstituted benzyl,processes for their manufacture and their use for combating unwanted plant growth.Type: GrantFiled: May 24, 1990Date of Patent: December 1, 1992Assignee: BASF AktiengesellschaftInventors: Gunter Brill, Helmut Hagen, Karl-Otto Westphalen, Bruno Wuerzer
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Patent number: 5103002Abstract: Ceramide derivatives of the following general formula ##STR1## are described, wherein the individual radicals have the following meanings:X=--NH or --CH.sub.2,R.sub.1 =H or C.sub.1-11 -alkyl,R.sub.2 =C.sub.2-9 -alkenyl, wherein the double bond is in .alpha. position to the OR.sub.3 groupR.sub.3 =H, C.sub.1-6 -alkyl or C.sub.1-6 -acyl andR.sub.4 =OH, C.sub.1-6 -alkoxy or morpholino.These ceramide derivatives represent inhibitors of the biosynthesis of sphingolipids.Type: GrantFiled: May 17, 1990Date of Patent: April 7, 1992Inventor: Felix Wieland
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Patent number: 5084474Abstract: The present invention provides ketones of the general formula (I): ##STR1## and physiologically acceptable salts and solvates thereof, wherein R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom or a C.sub.1-6 alkyl group; Im represents an imidazolyl group of formula: ##STR2## wherein one of the groups represented by R.sup.3, R.sup.4 and R.sup.5 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; andA is a group of the formula (a), (b), (c), (d), (e), (f) or (g) as set forth hereinafter,and when A is the group (g), the group --COCR.sup.1 R.sup.2 CH.sub.2 Im is attached at the 2- or 4- position of the indole moiety.The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.Type: GrantFiled: February 4, 1991Date of Patent: January 28, 1992Assignee: Glaxo Group LimitedInventors: Alexander W. Oxford, David J. Cavalla, Peter C. North
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Patent number: 5076832Abstract: Compounds having the formula ##STR1## wherein R and R.sup.1 are hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy and Ar is a substituted phenyl group as herbicide.Type: GrantFiled: July 20, 1990Date of Patent: December 31, 1991Assignee: ICI Americas Inc.Inventor: Siok H. H. Wee
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Patent number: 5071999Abstract: 2,7-Diazabicyclo[3.3.0]octanes, suitable for 7-position substituents or antibacterially active quinolone carboxylic acids, of the formula ##STR1## in which R.sup.1, R.sup.3, R.sup.4, R.sup.5, R.sup.7 and R.sup.8 may be identical or different and in each case denote H, C.sub.1 -C.sub.5 -alkyl (optionally substituted by halogen, hydroxyl or C.sub.1 -C.sub.3 -alkoxy), C.sub.1 -C.sub.3 -alkoxycarbonyl or C.sub.6 -C.sub.12 -aryl,R.sup.4 additionally denotes halogen,R.sup.2 and R.sup.6 may be identical or different, denote H, C.sub.1 -C.sub.6 -alkyl, benzyl, C.sub.6 -C.sub.12 -aryl, C.sub.1 -C.sub.3 -alkanoyl, benzoyl or C.sub.1 -C.sub.5 -alkoxycarbonyl, orR.sup.2 and R.sup.3 together denote a bridge of the structure (CH.sub.2).sub.n, n=2-4, CH.sub.2 --CHOH--CH.sub.2, CH.sub.2 --S--CH.sub.2 or C(CH.sub.3).sub.2 --S--CH.sub.2,excluding 2,7-diazabicyclo[3.3.0]octane.Also their preparation by the reaction ##STR2## Intermediates II are also new.Type: GrantFiled: April 10, 1990Date of Patent: December 10, 1991Assignee: Bayer AktiengesellschaftInventors: Thomas Schenke, Uwe Petersen
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Patent number: 5069712Abstract: Imidazolidine derivatives of the formula ##STR1## in which R represents in each case optionally substituted alkyl, cycloalkyl or aryl andX and Y independently of one another represent hydrogen, halogen, cyano, nitro or carboxyl, or represent in each case optionally substituted alkyl, alkoxy, alkoxycarbonyl, alkylthio, alkylsulphinyl or alkylsulphonyl,are useful as herbicides. A process for preparing the imidazolidine derivatives is also disclosed.Type: GrantFiled: April 4, 1991Date of Patent: December 3, 1991Assignee: Bayer AktiengesellschaftInventors: Wilfried Draber, Peter Babczinsky, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
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Patent number: 5070093Abstract: A novel series of tetracyclic amines, methods of preparation, compositions containing the amines, and methods for using them in the treatment and/or prevention of cerebrovascular disorders are disclosed.Type: GrantFiled: March 28, 1991Date of Patent: December 3, 1991Assignee: Warner-Lambert CompanyInventor: Thomas C. Malone
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Patent number: 5068447Abstract: Aromatic carbonyl compounds, in particular arylene ether ketones, are prepared by reacting an appropriate reagent system in the presence of free Lewis acid and a complex between a Lewis acid, for example, aluminum trichloride, and an inorganic salt controlling agent, for example, lithium chloride, and, optionally, a diluent, such as methylene chloride. The process is particularly advantageous for the preparation of substantially or all para-linked arylene ether ketones as the presence of the Lewis acid/Lewis base complex markedly reduces alkylation and ensures the substantial absence of ortho substitution.Type: GrantFiled: July 6, 1990Date of Patent: November 26, 1991Assignee: Raychem CorporationInventors: Heinrich C. Gors, Patrick J. Horner, Viktors Jansons
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Patent number: 5057616Abstract: Podophyllotoxin is recovered from podophyllum resin with improved efficiency by adsorbing impurities out of a solution using a solid adsorbent, preferably alumina. This improvement finds application in an overall process for purifying podophyllotoxin from podophyllum resin in which the podophyllotoxin is first crystallized from the podophyllum resin, the crystals so formed are dissolved and subjected to the solid adsorbent treatment, crystals are then recovered and optionally recrystallized and dried to give the desired product.Type: GrantFiled: September 29, 1989Date of Patent: October 15, 1991Assignee: Oclassen Pharmaceuticals, Inc.Inventors: Rex A. Jennings, Jay F. Stearns
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Patent number: 5057612Abstract: Substituted N-halo derivatives of imidazolidin-4-ones having substituents at the 2 and 5 positions of the imidazolidin-4-one ring are described. More particularly, there are described N-chloro, N-bromo, N,N'-dichloro, N,N'-dibromo, and N,N'-bromochloro derivatives of imidazolidin-4-ones having substituents selected from hydrogen, alkyl, alkoxy, hydroxy, phenyl, substituted phenyl, or spiro-substitution at the 2 and 5 positions on the ring. These N-halo compounds are stable, noncorrosive biocides which are resistant to direct sunlight, and are useful as disinfectants, sanitizers, and algae inhibitors.Type: GrantFiled: January 22, 1990Date of Patent: October 15, 1991Assignee: Auburn Research FoundationInventors: Shelby D. Worley, Techen Tsao, Delbert E. Williams
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Patent number: 5053415Abstract: The invention concerns novel, pharmaceutically useful 1,3-dioxane alkenoic acid derivatives of the formula I containing a pyridyl moiety at position 4 of the dioxane ring and in which the groups at positions 2, 4 and 5 have cis-relative stereochemistry, X is hydrogen, alkoxy or hydroxy, Y is vinylene, n is 1 or 2, A.sup.1 is alkylene, the substituents R.sup.1 and R.sup.2 at position 2 of the dioxane ring have a variety of values defined hereinafter, and R.sup.4 is hydroxy, a physiologically acceptable alcohol residue or alkanesulphonamido, and the pharmaceutically acceptable salts thereof. The invention also includes processes for the manufacture and use of the acid derivatives as well as pharmaceutical compositions for therapeutic use in one or more of a variety of diseases such as ischaemic heart disease, cerebrovascular disease, asthmatic disease and/or inflammatory disease.Type: GrantFiled: October 20, 1989Date of Patent: October 1, 1991Assignee: Imperial Chemical Industries PLCInventors: Andrew G. Brewster, George R. Brown, Alan W. Faull, Reginald Jessup, Michael J. Smithers
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Patent number: 5049579Abstract: The invention relates to distamycin A analogs of the following formula ##STR1## wherein n is 2, 3 or 4; A is an optionally substituted divalent radical chosen from ##STR2## and -Het- wherein Het is a pentatomic or hexatomic heteromonocyclic ring, except pyrrole; and wherein either one of R.sub.1 and R.sub.2 is hydrogen and the other is an acylating moiety or R.sub.1 and R.sub.2 are both hydrogen or both alkyl groups optionally substituted, including the pharmaceutically acceptable salts of the said compounds.The compounds of the invention can be useful antitumor and antiviral agents.Type: GrantFiled: October 31, 1990Date of Patent: September 17, 1991Assignee: Farmitalia Carlo Erba, S.r.l.Inventors: Ettore Lazzari, Federico Arcamone, Sergio Penco, Maria A. Verini, Nicola Mongelli
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Patent number: 5047400Abstract: The invention relates to the compounds of general formula: ##STR1## in which: X denotes either an oxygen atom, or two hydrogen atoms;Y denotes either a hydrogen atom, or a hydroxyl group;or Y denotes an amino group on condition that X denotes two hydrogen atoms;R denotes a hydrogen atom, or a straight- or branched-chain alkyl group having 1 to 6 carbon atoms, optionally substituted with one or more hydroxy, amino, mercapto, methylthio or carboxy groups, or aryl groups such as phenyl, pyridyl or thienyl; ##STR2## denotes a polycyclic nitrogenous structure; their enantiomers, epimers and diastereoisomers, as well as their addition salts with a pharmaceutically acceptable acid or base.Type: GrantFiled: June 16, 1988Date of Patent: September 10, 1991Assignee: Adir et CieInventors: Michel Vincent, Georges Remond, Bernard Portevin, Claude Cudennec
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Patent number: 5045540Abstract: This invention relates to novel amino acid derivatives which antagonize the binding of angiotensin II to its receptors. The compounds are useful in the treatment of hypertension, heart failure, glaucoma, and hyperaldosteronism. Methods of making the compounds, novel intermediates useful in the separation of the compounds, compositions containing the compounds and methods of using them are also covered.Type: GrantFiled: April 12, 1991Date of Patent: September 3, 1991Assignee: Warner-Lambert Co.Inventors: John C. Hodges, Ila Sircar
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Patent number: 5041552Abstract: This invention relates to novel amino acid derivatives which antagonize the binding of angiotensin II to its receptors. The compounds are useful in the treatment of hypertension, heart failure, glaucoma, and hyperaldosteronism. Methods of making the compounds, novel intermediates useful in the separation of the compounds, compositions containing the compounds and methods of using them are also covered.Type: GrantFiled: May 25, 1990Date of Patent: August 20, 1991Assignee: Warner-Lambert CompanyInventors: John C. Hodges, Ila Sircar
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Patent number: 5039808Abstract: The novel compound 5-fluoro-2[[(4-cyclopropylmethoxy-2-pyridinyl)methyl]sulfinyl]-1H-benzimid azole and physiologically acceptable salts thereof as well as intermediates, pharmaceutical compositions containing the compound as active ingredient, and the use of the compound in medicine.Type: GrantFiled: December 20, 1990Date of Patent: August 13, 1991Assignee: Aktiebolaget HassleInventors: Arne E. Brandstrom, Per L. Lindberg, Gunnel E. Sunden
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Patent number: 5036091Abstract: The derivatives of the formula: ##STR1## wherein: R.sub.1 is H or C.sub.1 -C.sub.4 alkyl;X is either an oxygen atom, in which case R.sub.2 =H or halogen, or a methylene group or a --CH.dbd.CH-- group, in which case R.sub.2 =H;n is 1 or 2 when X is an oxygen atom or a methylene group and 0 or 1 when X is a --CH.dbd.CH-- group;each of R.sub.3 and R.sub.4 is independently H, C.sub.1 -C.sub.4 alkyl, C.sub.4 -C.sub.7 cycloalkyl, phenyl or benzyl;R.sub.5 is H or C.sub.1 -C.sub.4 alkyl;R.sub.6 is C.sub.1 -C.sub.4 alkyl, CHF.sub.2, CF.sub.3, CF.sub.3 CH.sub.2, C.sub.4 -C.sub.7 cycloalkyl, phenyl or benzyl;R.sub.4 and R.sub.6 may further form together a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- chain;R.sub.5 and R.sub.6 may further form together a --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 -- chain; andR.sub.7 is H, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.5 acyl or benzyl,useful as drugs.Type: GrantFiled: October 15, 1990Date of Patent: July 30, 1991Assignee: Delalande S.A.Inventors: Francois X. Jarreau, Vincenzo Rovei, Jean-Jacques Koenig, Alain R. Schoffs
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Patent number: 5036088Abstract: Compounds of the formula ##STR1## where Y is alkyl, aryl or heterocyclic, n is 1-7, R is hydrogen, alkyl, aralkyl or carboxymethyl, R.sub.1 is acetoxy, thiophenoxy, hydrogen, halo, alkyl, alkoxy or trifluoromethyl, R.sub.2 is hydrogen, alkyl or alkanoyl and X is C.dbd.O, CH.sub.2, NH, O or S as antiallergy and antiinflammatory agents.Type: GrantFiled: December 3, 1990Date of Patent: July 30, 1991Assignee: Pfizer Inc.Inventors: Yoshihiko Kitaura, Fumitaka Ito, Rodney W. Stevens, Nobuko Asai
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Patent number: 5036090Abstract: The derivatives of the formula: ##STR1## wherein: R.sub.1 is H or C.sub.1 -C.sub.4 alkyl;X is an oxygen atom, a methylene group or a --CH.dbd.CH-- group;n is 1 or 2 when X is an oxygen atom or a methylene group and is 0 or 1 when X is a --CH.dbd.CH-- group;R.sub.3 is a C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, phenyl, benzyl, CHF.sub.2, CF.sub.3 or CF.sub.3 CF.sub.2 group;each of R.sub.2 and R'.sub.2 independently is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl, C.sub.4 -C.sub.7 cycloalkyl, phenyl or benzyl group;R'.sub.2 and R.sub.3 may further form together a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- chain; andeach of R.sub.4 and R'.sub.4 independently is a C.sub.1 -C.sub.4 alkyl group or R.sub.4 and R'.sub.4 form together either a --(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.3 -- chain, a --(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.3 -- chain substituted by one or two C.sub.1 -C.sub.4 alkyl groups, or a --(CH.sub.2).sub.2 -- chain substituted by one or two --CH.sub.2 --NH.sub.Type: GrantFiled: October 15, 1990Date of Patent: July 30, 1991Assignee: Delalande S.A.Inventors: Francois X. Jarreau, Vincenzo Rovei, Jean-Jacques Koenig, Alain R. Schoffs
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Patent number: 5032602Abstract: For inhibiting HMG-CoA reductase and cholesterol synthesis, the novel 2-pyridones and pyrid-2-thiones of the formula ##STR1## in which A is optionally substituted aryl or heterocyclic,B is optionally substituted alkyl, cycloalkyl or aryl,D and E independently are optionally substituted aryl or heterocyclic, H, nitro, cyano, optionally substituted alkyl, alkenyl or imino, amino, alkoxy or acyl, or forms a ring with B,G is O or S,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--, andR represents a group of the formula ##STR2## and salts thereof.Type: GrantFiled: November 27, 1989Date of Patent: July 16, 1991Assignee: Bayer AktiengesellschaftInventors: Peter Fey, Rolf Angerbauer, Walter Hubsch, Thomas Philipps, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt, Gunter Thomas