Patents Represented by Attorney Catherine R. Roseman
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Patent number: 5538725Abstract: Polypeptides which bind to mammalian .alpha.6-integrin and inhibit metastasis.Type: GrantFiled: August 12, 1994Date of Patent: July 23, 1996Assignee: Hoffman-La Roche Inc.Inventor: Beat A. Imhof
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Patent number: 5508430Abstract: Novel alcohols of the formula ##STR1## wherein R.sup.a is azido or phthalimido, R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.7 and R.sup.8 together are a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, --N(alkoxycarbonyl)--, --N(acyl)-- or --S-- or which carries a fused cycloalkane, aromatic or heteroaromatic ring, and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR2## in which R.sup.10 and R.sup.11 each is alkyl, are described along with a process for their manufacture. These alcohols are useful as intermediates, for example in the manufacture of amino acid derivatives having antiviral activity.Type: GrantFiled: May 12, 1995Date of Patent: April 16, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Kevin E. B. Parkes, Sally Redshaw, Gareth J. Thomas
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Patent number: 5488115Abstract: Novel alcohols of the formula ##STR1## wherein R.sup.a is azido or phthalimido, R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.7 and R.sup.8 together are a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, --N(alkoxycarbonyl)--, --N(acyl)-- or --S-- or which carries a fused cycloalkane, aromatic or heteroaromatic ring, and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR2## in which R.sup.10 and R.sup.11 each is alkyl, are described along with a process for their manufacture. These alcohols are useful as intermediates, for example in the manufacture of amino acid derivatives having antiviral activity.Type: GrantFiled: May 12, 1995Date of Patent: January 30, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Kevin E. B. Parkes, Sally Redshaw, Gareth J. Thomas
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Patent number: 5451678Abstract: Novel alcohols of the formula ##STR1## wherein R.sup.a is azido or phthalimido, R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.7 and R.sup.8 together are a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, --N(alkoxycarbonyl)-, --N(acyl)- or --S-- or which carries a fused cycloalkane, aromatic or heteroaromatic ring, and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR2## in which R.sup.10 and R.sup.11 each is alkyl, are described along with a process for their manufacture. These alcohols are useful as intermediates, for example in the manufacture of amino acid derivatives having antiviral activity.Type: GrantFiled: September 29, 1993Date of Patent: September 19, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Kevin E. B. Parkes, Sally Redshaw, Gareth J. Thomas
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Patent number: 5449785Abstract: Compounds of the formula ##STR1## which have antifungal activity.Type: GrantFiled: July 10, 1992Date of Patent: September 12, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Yuhko Aoki, Hiromichi Kotaki, Kazunao Masubuchi, Toru Okuda, Nobuo Shimma, Takuo Tsukuda, Isao Umeda
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Patent number: 5418147Abstract: The present invention involves the protein glycosyl-phosphatidyl-specific phospholipase D (GPI-PLD) in a substantially pure form, an isolated nucleotide sequence encoding GPI-PLD, vectors containing the isolated nucleotide sequence encoding GPI-PLD, and cells transformed by a vector containing the isolated nucleotide sequence encoding GPI-PLD, also nucleotide sequences, vectors and cells comprising hybrid genes with GPI-PLD, and methods for producing secreted proteins.Type: GrantFiled: March 31, 1992Date of Patent: May 23, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Kuo-Sen Huang, Jarema P. Kochan, Shirley H. Li, Yu-Ching E. Pan, Bernard J. Scallon, Thomas C. H. Tsang
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Patent number: 5405866Abstract: Compounds of the formula. ##STR1## wherein R is a residue of the formula ##STR2## and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X, Y and Z are as described, with the exception of rac-N-(3,4-dimethoxyphenethyl)-2-(3,4-dimethoxyphenyl)-.beta.,N-dimethyl-m -dithiane-2-propanamine, as well as their acid addition salts, in particular for use in eliminating cytostatic resistance in tumor treatment and chloroquine resistance in malaria.Type: GrantFiled: January 24, 1994Date of Patent: April 11, 1995Assignee: Hoffmann-La Roche Inc.Inventors: James F. Eliason, Henri Ramuz, Franz A. Kaufman-Schmid, deceased
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Patent number: 5403581Abstract: The invention provides an immunogenic polypeptide having the amino acid sequence ##STR1## which polypeptides are capable of inducing an immune response against Eimeria parasites, and the DNA encoding such polypeptides, as well as recombinant vectors and recombinant viruses containing the said DNA and transformed microorganisms containing such vectors and viruses and coccidiosis vaccines comprising such polypeptides.Type: GrantFiled: July 12, 1991Date of Patent: April 4, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Mary-Helen Binger, Luis Pasamontes
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Patent number: 5395750Abstract: Methods of producing a protein capable of binding to a predetermined antigen, screening libraries containing such proteins, and proteins and synthetic genes containing randomized sequences are disclosed.Type: GrantFiled: February 28, 1992Date of Patent: March 7, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Patrick J. Dillon, Craig A. Rosen
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Patent number: 5382657Abstract: Substituted PEG-interferon conjugates of formulae IA and IB where PEG is linked by means of activated linking reagents of formulae IIA, IIB, or IIB-1 to an amino group in the interferon, and activated linking reagents of formulae IIA, IIB, or IIB-1. The conjugates are not readily susceptible to in vivo hydrolytic cleavage, have enhanced in vivo half life, and reduce the immunogenicity of the interferon while maintaining biological activity.Type: GrantFiled: August 26, 1992Date of Patent: January 17, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Robert Karasiewicz, Carlo Nalin, Perry Rosen
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Patent number: 5372746Abstract: Compounds of the general formula ##STR1## wherein ring A represents 1,4-phenylene, pyridine-2,5-diyl, pyrimidine-2,5-diyl, trans-1,4-cyclohexylene or trans-1,3-dioxane-2,5-diyl;Z signifies a single covalent bond, --CH.sub.2 CH.sub.2 --, --OCH.sub.2 --, --CH.sub.2 O--, --(CH.sub.2).sub.4 --, --O(CH.sub.2).sub.3 --, --(CH.sub.2).sub.3 O-- or, where ring A represents a saturated ring, also the trans form of --CH.dbd.CH(CH.sub.2).sub.2 -- or --CH.dbd.CHCH.sub.2 O--;X signifies fluorine, chlorine, cyano, --CF.sub.3, --OCF.sub.3 or --OCHF.sub.2 ;Y.sup.1, Y.sup.2 each independently signify fluorine or hydrogen; andR signifies alkyl, alkoxy, alkenyl or alkenyloxy with 1 or, respectively, 2 to 12 carbon atoms in which one CH.sub.2 group or two non-adjacent CH.sub.Type: GrantFiled: November 17, 1992Date of Patent: December 13, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Richard Buchecker, Martin Schadt
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Patent number: 5302727Abstract: Compounds of the formula ##STR1## wherein R is a residue of the formula ##STR2## and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X, Y and Z are as described, with the exception of rac-N-(3,4-dimethoxyphenethyl)-2-(3,4-dimethoxyphenyl)-.beta.,N-dimethyl-m -dithiane-2-propanamine, as well as their acid addition salts, in particular for use in eliminating cytostatic resistance in tumor treatment and chloroquine resistance in malaria.Type: GrantFiled: July 15, 1992Date of Patent: April 12, 1994Assignee: Hoffmann-La Roche Inc.Inventors: James F. Eliason, Henri Ramuz, Franz A. Kaufmann-Schmid, deceased
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Patent number: 5252604Abstract: Compositions of retinoic acids and tocopherols which may be applied topically without producing retinoic acid-induced skin irritation.Type: GrantFiled: July 10, 1992Date of Patent: October 12, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Christa F. Nagy, Timothy W. Quick, Stanley S. Shapiro
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Patent number: 5227507Abstract: A process for the manufacture of compounds of the general formula ##STR1## wherein R.sup.1 signifies hydroxy or an etherified hydroxy group, and of zeaxanthin by converting a compound of the general formula ##STR2## wherein R.sup.1 has the above significance, in an inert organic solvent into the acetylenide and reacting this with methyl vinyl ketone, reducing the alcoholate obtained or the alcohol (obtained after hydrolysis of the alcoholate) of the general formula ##STR3## wherein R.sup.1 has the above significance, in an inert organic solvent with an aluminum hydride of the general formulaR.sub.x MAlH.sub.4-x IIIwherein M signifies alkali metal, R represents C.sub.1 -C.sub.10 -alkoxy or a group of the formula C.sub.n H.sub.2n+1 --O--C.sub.m H.sub.2m --O--, m and n each individually denote whole numbers of 1 to 7 and x stands for 0, 1, 2 or 3,and subsequently hydrolyzing to give the compound of formula IV and, if desired, converting the compound of formula IV obtained into zeaxanthin.Type: GrantFiled: March 23, 1990Date of Patent: July 13, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Teodor Lukac, Milan Soukup
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Patent number: 5225534Abstract: The invention provides polypeptides which correspond in at least one specific epitope with a plasmodium falciparum merozoite antigen having a molecular weight of about 41,000 Daltons, and a process for their production. The invention further provides immunogenic compositions which contain such a polypeptide and a suitable adjuvant, a DNA sequence which codes for such a polypeptide, replicable microbial vectors which contain such a DNA sequence, microorganisms which contain such a replicable vector and antibodies against a polypeptide of the invention. The invention still further provides processes for the production of the immunogenic compositions, the microorganisms and the antibodies and for the use of the polypeptides and the immunogenic compositions for the immunization of mammals against malaria.Type: GrantFiled: July 29, 1991Date of Patent: July 6, 1993Assignee: Hoffmann-La Roche Inc.Inventor: Ulrich Certa
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Patent number: 5221735Abstract: Inclusion complexes of the polyenes apocarotenal and lycopene in a cyclodextrin as well as their manufacture are described. The inclusion complexes are soluble in water, alcohol or water/alcohol mixtures.Type: GrantFiled: February 14, 1992Date of Patent: June 22, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Bruno Leuenberger, Hansjorg Stoller
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Patent number: 5214162Abstract: The invention is concerned with a process for the manufacture of 5-cyano-4-lower alkyl-oxazoles by dehydrating a 5-carbamoyl-4-lower alkyl-oxazole in the gas phase in the presence of a heterogeneous catalyst based on silicon dioxide and in the presence of an inert solvent. The heterogeneous catalyst used is formed SiO.sub.2 or SiO.sub.2 doped with an oxide of V, Mo, Fe, Co and/or Zn. An N-lower alkyl-pyrrolidone is preferably used as the inert solvent.Type: GrantFiled: December 5, 1991Date of Patent: May 25, 1993Assignee: Hoffman-La Roche Inc.Inventor: Paul Nosberger
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Patent number: 5182205Abstract: The present invention provides nucleotide sequences which are selectively expressed in pre-B cells, probes comprising a polynucleotide hybridizing specifically to such a nucleotide sequence and methods for the production of such probes. These probes may be used for identifying pre-B cells. The invention further provides polypeptides translated from a transcript comprising a nucleotide sequence which is selectively expressed in pre-B cells or parts thereof, antibodies against these polypeptides and methods for the preparation and use of the polypeptides and antibodies raised against them.Type: GrantFiled: May 8, 1991Date of Patent: January 26, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Steven R. Bauer, Akira Kudo, Georg F. Melchers, Nobuo Sakaguchi
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Patent number: 5162577Abstract: A novel process for the lithiation of 1,3-bis(trifluoro-methyl)benzene in a solvent is described, said process comprising carrying out the lithiation with the lithium salt of an amine of the general formulaR.sup.1 R.sup.2 NH Iwherein R.sup.1 and R.sup.2 are secondary or tertiary lower alkyl or secondary or tertiary lower alkyl substituted by a lower alkyl or lower cycloalkyl or lower cycloaklyl substituted by a lower alkyl, or R.sup.1 and R.sup.2 taken together form a C.sub.6-14 -alkylene group in which the two carbon atoms linked with the nitrogen atom are secondary or tertiary and are separated from each other by 2 to 4 carbon atoms.The solution of the lithiated 1,3-bis(trifluoromethyl)-benzene obtained can be reacted with an electrophile which is suitable for the substitution of lethiated benzene derivatives, whereby a compound of the formula ##STR1## wherein R.sup.3 signifies the residue of an electrophile which is suitable for the substitution of lithiated benzene derivatives, is obtained.Type: GrantFiled: February 1, 1991Date of Patent: November 10, 1992Assignee: Hoffmann-La Roche Inc.Inventor: Raffaello Masciadri
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Patent number: 5155255Abstract: A process for the manufacture of certain cycloalkenylalkenes, e.g. vitamin A acetate, comprises dehydrating 1-(5-acetoxy-3-methyl-penta-1,3-dienyl)-2,6,6-trimethyl-cyclo hexanol or 4 aetoxy-1-(5-acetoxy-3-methyl-penta-1,3-dienyl)-2,6,6-trimethyl-cyclohexano l or 1-(9-acetoxy-3,7-dimethyl-4-hydroxy-nona-2,5,7-trienyl)-2,6,6-trimethyl- cyclohexene in the presence of an alkali metal bromide or of manganese bromide or of a hydrate of such a bromide as the catalyst and in an organic solvent.The products are especially suitable as intermediates in carotinoid syntheses.Type: GrantFiled: March 25, 1991Date of Patent: October 13, 1992Assignee: Hoffmann-La Roche Inc.Inventors: Mario Mazzuchelli, Milan Soukup, Paul Spurr, Claude Stritt