Patents Represented by Attorney Jon S. Saxe
  • Patent number: 4587256
    Abstract: The invention relates to with novel thiazolidine derivatives of the formula ##STR1## wherein X is methylene, oxygen or sulfur; R.sup.1 is halogen; R.sup.2 is hydrogen, nitro, cyano, OR.sup.3 or NHR.sup.3 ; or R.sup.1 and R.sup.2 both simultaneously are hydrogen or nitro; R.sup.3 is hydrogen, alkyl, acyl, --CO--OR.sup.4 or --CO--NHR.sup.4 ; and R.sup.4 is alkyl, unsubstituted or substituted aryl or aralkyl,and their salts with physiologically compatible cations. The compounds of formula I are useful in the treatment of metabolic disorders.
    Type: Grant
    Filed: June 11, 1984
    Date of Patent: May 6, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Heinz Hasler, Fernand Schneider
  • Patent number: 4585796
    Abstract: The tertiary amines of the formula ##STR1## wherein n represents a whole number of 1 to 5;X.sup.1 represents phenyl or phenyl mono-, di- or tri-substituted by R.sup.1, R.sup.2 and R.sup.3 ;X.sup.2 represents hydrogen, lower-alkyl, phenyl or phenyl mono-, di- or tri-substituted by R.sup.1, R.sup.2 and R.sup.3 ;Y represents hydrogen, lower-alkyl, hydroxymethyl, carboxy or lower-alkoxycarbonyl;Z represents a group of the formula ##STR2## R.sup.1, R.sup.2 and R.sup.3 represent hydrogen, halogen, hydroxy, benzyloxy, lower-alkyl, lower-alkoxy, hydroxymethyl, amino, acylamino, lower-alkoxybenzylamino, nitro, carbamoyl, trifluoromethyl or lower-alkylsulphonylmethyl;R.sup.4, R.sup.5 and R.sup.51 represent hydrogen, lower-alkyl, lower-alkoxy, lower alkanoyl, carboxy, cyano, hydroxy, hydroxy-lower-alkyl, acyloxy or a group --C(R.sup.6).dbd.C(R.sup.7)COOR.sup.8, --SO.sub.2 R.sup.9, --C(O)R.sup.9 or --CH.sub.2 R.sup.10, with the proviso that R.sup.4 does not represent hydrogen when R.sup.
    Type: Grant
    Filed: August 1, 1983
    Date of Patent: April 29, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Marcel Muller
  • Patent number: 4585885
    Abstract: A silyl-enol ether of the formula ##STR1## wherein n stands for the number and X stands for a group ##STR2## or n stands for the number 1 and X stands for the 6,11-dimethylhexadeca-2,4,6,8,10,12,14-heptaene-2,15-diyl group, the symbols R.sup.1 have the same or different significances and denote alkyl groups, and the symbol R.sup.2 represents a trialkylsiloxy group --OSi(R.sup.1).sub.3 or an ether group,is oxidized with percarboxylic acid and, if desired, the resulting .alpha.-siloxy ketone is hydrolyzed to an .alpha.-hydroxy ketone. This process is especially suitable for the manufacture of astaxanthin.
    Type: Grant
    Filed: August 19, 1983
    Date of Patent: April 29, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kurt Bernhard, Robert K. Muller, Robert Spruijtenburg
  • Patent number: 4584191
    Abstract: Biotin esters, namely biotin C.sub.2-4 -alkyl esters, are prepared by esterifying biotin with a C.sub.2-4 -alkanol. These esters have the capability of being absorbed by the human skin better than biotin and are converted into biotin during or after absorption. Since biotin itself promotes the fat and cholesterol synthesis of the skin, the novel biotin esters of this invention are useful as active ingredients for cosmetic hair-care and skin-care compositions.
    Type: Grant
    Filed: December 2, 1982
    Date of Patent: April 22, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans U. Hostettler, Bruno Poncioni
  • Patent number: 4584295
    Abstract: Heterocyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and X are as defined hereinafter, process for their preparation, as well as pesticidal compositions containing these compounds as the active ingredient and methods for using the pesticidal compositions for the control of pests are described.
    Type: Grant
    Filed: December 27, 1983
    Date of Patent: April 22, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Christoph Luthy
  • Patent number: 4584132
    Abstract: A novel family of .beta.-lactam antibacterials, synthetic methods and intermediates useful in the production of such antibacterials, and the use of such compounds as antibacterials are disclosed. The novel compounds have the formula ##STR1## wherein, Z.sup.1 is a group --OR.sup.1, --NR.sup.3 R.sup.4, or --SR.sup.5 ;Z.sup.2 is a group --OR.sup.2, --NR.sup.3 R.sup.4, or --SR.sup.6 ;R.sup.1 and R.sup.2 may be either the same or different and each is H, lower alkyl, aralkyl, aryl or heteroaryl;R.sup.3 and R.sup.4 may be either the same or different and each is H, lower alkyl, aralkyl, aryl or heteroaryl;R.sup.5 and R.sup.6 may be either the same of different and each is H, lower alkyl, aralkyl, aryl or heteroaryl;R.sup.7 is H, lower alkyl, or lower alkoxycarbonyl; and,R.sup.8 is acyl;as well as pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: August 9, 1983
    Date of Patent: April 22, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Harry A. Albrecht, Frederick M. Konzelmann, Dennis D. Keith
  • Patent number: 4583826
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 signifies trans-4-alkylcyclohexyl, 4'-alkyl-4-biphenylyl, p-(trans-4-alkylcyclohexyl)phenyl, 2-(trans-4-alkylcyclohexyl)ethyl or p-[2-(trans-4-alkylcyclohexyl)ethyl]phenyl and R.sup.2 signifies trans-4-alkylcyclohexyl; or R.sup.1 signifies trans-4-alkylcyclohexyl and R.sup.2 signifies p-(trans-4-alkylcyclohexyl)phenyl, p-[2-(trans-4-alkylcyclohexyl)ethyl]phenyl or 4'-(trans-4-alkylcyclohexyl)-4-biphenylyl; or R.sup.1 signifies p-alkylphenyl and R.sup.2 signifies p-[2-(trans-4-alkylcyclohexyl)ethyl]phenyl, and the alkyl groups in the substituents R.sup.1 and R.sup.2 are straight-chain groups containing 1 to 7 carbon atoms, liquid crystalline mixtures which contain these compounds and their use for electro-optical purposes are described.The novel compounds of formula I are especially valuable as components in liquid crystal mixtures and themselves have liquid crystalline properties.
    Type: Grant
    Filed: October 1, 1982
    Date of Patent: April 22, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Martin Petrzilka, Martin Schadt
  • Patent number: 4582800
    Abstract: Improved vectors and methods for regulating the expression in bacteria of a eucaryotic anti-viral protein, such as mature human immune interferon, the gene for which has been cloned onto a bacterial plasmid, is disclosed. The improved vectors incorporate and method utilizes transcriptional regulatory elements derived from bacteriophage lambda and ribosome binding sites either derived from bacteriophage lambda and/or synthesized chemically.
    Type: Grant
    Filed: July 12, 1982
    Date of Patent: April 15, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Robert M. Crowl
  • Patent number: 4582919
    Abstract: There is described a novel process for producing hydroquinone derivatives of the formula ##STR1## wherein R is an ether protecting group, and their conversion into d-.alpha.-tocopherol, starting from compounds of the formula ##STR2## wherein R is an ether protecting group and R.sup.1 is hydrogen or an ether protecting group.
    Type: Grant
    Filed: June 11, 1984
    Date of Patent: April 15, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Barner, Josef Hubscher
  • Patent number: 4582853
    Abstract: The present invention relates to a novel polyether ionophore antibiotic of the formula ##STR1## and its pharmaceutically acceptable salts. The compound of formula I and its salts exhibit activity as an antibacterial agent and as an anticoccidial agent.
    Type: Grant
    Filed: January 22, 1985
    Date of Patent: April 15, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Chao-Min Liu, John Westley
  • Patent number: 4582641
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 -R.sup.4 is hydrogen or chlorine, R.sup.5 is --COOMe or --SO.sub.3 Me, Me is an alkali metal cation and X is oxygen, sulfur or selenium,photosensitizers for the conversion of tachysterol into previtamin D are described. The tachysterol content in mixtures of previtamin D and tachysterol can be greatly reduced by UV-irradiation in the presence of such photosensitizers.
    Type: Grant
    Filed: June 26, 1985
    Date of Patent: April 15, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans-Jurgen Hansen, Karlheinz Pfoertner
  • Patent number: 4582844
    Abstract: Imidazole derivatives of the formula ##STR1## wherein X is hydrogen or C.sub.1-4 -n-alkyl and Y is thienyl, optionally substituted by methyl or fluorine, or a group of the formula ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 independently are hydrogen, methyl, fluorine, hydroxy or methoxy, or two of R.sup.1, R.sup.2 and R.sup.3 on adjacent carbon atoms taken together are methylenedioxy or ethylenedioxy, or one of R.sup.1, R.sup.2 and R.sup.3 is mono- or di-(C.sub.1-4 -n-alkyl)-amino and the other two are hydrogen, and physiologically compatible or pharmaceutically acceptable acid addition salts thereof, are described. These compounds of formula I inhibit the aggregation of the blood platelets.
    Type: Grant
    Filed: September 10, 1985
    Date of Patent: April 15, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Romano Derungs
  • Patent number: 4582526
    Abstract: Carbamic acid ester compounds of the formula ##STR1## wherein A represents the group (a) or (b) ##STR2## wherein R.sup.1 -R.sup.8, X and Y are as defined hereinafter, processes for their preparation, herbicidal compositions containing these compounds and methods for the use of the compounds and the herbicidal compositions are disclosed.
    Type: Grant
    Filed: December 9, 1983
    Date of Patent: April 15, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Wenger, Rene Zurfluh
  • Patent number: 4581172
    Abstract: Pyrimidone derivatives of the formula ##STR1## wherein n is the integer 1 or 0; A.sup.1 and A.sup.2 are independently methylene or mono-lower alkyl or di-lower alkyl methylene; X is methylene, mono-lower alkyl or di-lower alkyl methylene, nitrogen or lower alkyl nitrogen; R is hydrogen or lower alkyl; and Y and Z taken together are the group .dbd.NR.sup.5, or R and Z taken together form a N--C--bond and Y is a group --N(H)R.sup.5 ; R.sup.1, R.sup.2 and R.sup.3 are hydrogen, lower alkyl or lower alkoxy, or R.sup.1 and R.sup.2 or R.sup.2 and R.sup.3 taken together are methylenedioxy or ethylenedioxy; R.sup.4 is hydrogen or lower-alkyl; R.sup.5 is phenyl or phenyl substituted by one or more of R.sup.6, R.sup.7 and R.sup.8 which, independently, are chlorine, fluorine, bromine, lower-alkyl or lower-alkoxy; and provided that at least one of the methylene groups A.sup.1 and A.sup.2 is mono-lower alkyl or di-lower alkyl methylene, when R.sup.
    Type: Grant
    Filed: April 25, 1984
    Date of Patent: April 8, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ado Kaiser, Frank Kienzle
  • Patent number: 4579973
    Abstract: A novel process for the manufacture of cyclohexene derivatives which are suitable as intermediates for the manufacture of rhodoxanthin or zeaxanthin, as well as a process for the manufacture of rhodoxanthin or of zeaxanthin itself. The invention is also concerned with a novel starting material and novel intermediates in this process.
    Type: Grant
    Filed: February 8, 1985
    Date of Patent: April 1, 1986
    Assignee: Hoffman-La Roche Inc.
    Inventors: Erich Widmer, Reinhard Zell
  • Patent number: 4579855
    Abstract: Mefloquin hydrochloride in the form of modification E as characterized by IR spectrum and X-ray diffraction pattern, as well as a process for the preparation thereof by treating mefloquin hydrochloride, comprising at least partially another modification, that is, mefloquin hydrochloride which is not pure mefloquin hydrochloride in the form of modification E, with methanol and/or ethanol, in the presence of less than 30 volume/percent of water.
    Type: Grant
    Filed: October 1, 1984
    Date of Patent: April 1, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Helmut Bomches, Bruno Hardegger
  • Patent number: 4578475
    Abstract: The novel D-homosteroids of the formula ##STR1## wherein R.sup.1 represents a --CN, .dbd.NOH or .dbd.CH--NHOH group; R.sup.2 represents oxo or, where R.sup.1 represents a --CN group, R.sup.2 represents oxo or a --OAc group; or R.sup.1 and R.sup.2 together with carbon atoms 2 and 3 of the steroid skeleton represents a [2,3-d]-fused isoxazole ring, a [3,2-c]-fused pyrazole ring, a [3,2-c]-fused N-acylated pyrazole ring or a [2,3-c]-fused furazan ring; Ac represents an acyl group; R.sup.3 and R.sup.4 represent methyl and R.sup.5 and R.sup.6 together represent an additional bond between carbon atoms 5 and 6 of the steroid skeleton; or R.sup.4 and R.sup.5 together represent --O--, R.sup.3 represents hydrogen or methyl, and R.sup.6 represents hydrogen; R.sup.7 represents hydrogen, lower-alkyl or ethynyl; R.sup.8 represents hydroxy or acyloxy; or R.sup.7 and R.sup.
    Type: Grant
    Filed: January 26, 1984
    Date of Patent: March 25, 1986
    Assignee: Hoffman-La Roche Inc.
    Inventors: Andor Furst, Marcel Muller, Ulrich Kerb, Rudolf Wiechert
  • Patent number: 4578462
    Abstract: The manufacture of optically active bifunctional compounds of the general formula ##STR1## wherein R represents protected hydroxymethyl, protected formyl or alkoxycarbonyl and R.sup.1 represents a group of the formula ##STR2## or --CH.sub.2 --CH.dbd.NR.sup.2 in which R.sup.2 and R.sup.3 represent lower alkyl or cycloalkyl or R.sup.2 and R.sup.3 together with the nitrogen atom represent a heterocyclic ring,by isomerizing compounds of the general formula ##STR3## wherein R, R.sup.2 and R.sup.3 have the above significance and R.sup.3 can additionally signify hydrogen,is described.The compounds of formula I are potential intermediates in the manufacture of, inter alia, natural vitamin E and natural vitamin K.sub.1.
    Type: Grant
    Filed: August 22, 1983
    Date of Patent: March 25, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans-Jurgen Hansen, Rudolf Schmid, Max Schmid
  • Patent number: 4577030
    Abstract: Phenoxy-aminopropanol derivatives of the formula ##STR1## wherein R is lower alkyl, X is oxygen or sulfur, n is the integer zero or 1, Y is methylene, ethylene or propylene or, when n is zero, Y can also be a group of the formula ##STR2## wherein the double-bond is trans and the carbon atom marked with an asterisk is linked to Z, and Z is a 5-membered aromatic heterocyclic ring which contains one or more nitrogen atoms as the sole hetero atom (s), said heterocyclic ring is linked to Y via a nitrogen atom, and may be substituted by halogen, lower alkyl, lower alkoxy, aryl, cyano or carboxamido, or on adjacent carbon atoms by a group of the formula--(CH.sub.2).sub.4 -- (b)or--CH.dbd.CH--CH.dbd.CH--, (c)and pharmaceutically acceptable acid addition salts thereof are described. A process for the preparation of the compound of formula I and pharmaceutical preparations containing them are also described. The aforementioned compounds and salts possess .beta.
    Type: Grant
    Filed: March 14, 1983
    Date of Patent: March 18, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Peter J. Machin
  • Patent number: 4576751
    Abstract: There is presented optically uniform .beta.-lactams of the formulae ##STR1## wherein Z is a readily cleavable acyl group, R.sup.1 is amino or a group convertible into amino, R.sup.2 is hydrogen or a readily cleavable protecting group and R.sup.3 and R.sup.4 each are a lower hydrocarbon group which optionally contains oxygen and which is attached via a carbon atom, whereby these groups can also be joined with one another to form a ring, with the proviso that R.sup.1 is a readily cleavable acylamino when R.sup.2 is hydrogen,and the corresponding optical antipodes, their manufacture and use in the manufacture of antimicrobially-active .beta.-lactams as well as novel intermediates usable in their manufacture.
    Type: Grant
    Filed: August 11, 1982
    Date of Patent: March 18, 1986
    Assignee: Hoffman-La Roche Inc.
    Inventors: Christian N. Hubschwerlen, Gerard Schmid