Patents Represented by Attorney Bernard S. Leon
  • Patent number: 4935560
    Abstract: Novel styryl-tetrahydromaphthalene and indane derivatives useful for treating neoplasms and dermatoses.
    Type: Grant
    Filed: January 16, 1990
    Date of Patent: June 19, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Peter Loeliger, Peter Mohr, Ekkehard Weiss
  • Patent number: 4935359
    Abstract: Disclosed is a fermentation process for the conversion of L-sorbose to 2-keto-L-gulonic acid, which is characterized in that a mixed culture of microorganisms is used, which comprises Gluconobacter oxydans and Bacillus megaterium.
    Type: Grant
    Filed: February 3, 1988
    Date of Patent: June 19, 1990
    Assignee: Institute of Microbiology
    Inventors: Guanglin Yin, Zengxin Tao, Zizheng Yan, Wenzhu Ning, Changhui Wang, Shuiding Wang
  • Patent number: 4935509
    Abstract: Cycloalkyl and aromatic vinblastine and vincristine derivatives useful as anti-tumor agents.
    Type: Grant
    Filed: June 8, 1989
    Date of Patent: June 19, 1990
    Assignees: University of Vermont, State Agricultural College
    Inventor: Martin Kuehne
  • Patent number: 4931574
    Abstract: The invention is directed to a process and intermediates for the preparation of benzopyrans such as racemic-6-acetyl-7-[5-(4-acetyl-3-hydroxy-2-propylphenoxy)pentyloxy]-3,4-d ihydro-2H-1-benzopyran-2-carboxylic acid.
    Type: Grant
    Filed: August 23, 1988
    Date of Patent: June 5, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Percy S. Manchand, Robert A. Micheli
  • Patent number: 4931463
    Abstract: Racemic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n are as described herein, enantiomers and diastereomers thereof, and salts of these esters with weak acids, are described. These compounds inhibit pancreas lipase and are useful agents in the treatment of obesity, hyperlipaemia, atherosclerosis and arteriosclerosis.
    Type: Grant
    Filed: December 17, 1987
    Date of Patent: June 5, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Pierre Barbier, Fernand Schneider, Ulrich Widmer
  • Patent number: 4931458
    Abstract: Heterocyclic compounds of the formula ##STR1## wherein X is --CH.dbd.CH--; R.sup.1 is the group Ar--R.sup.2 or --CH.dbd.CH--C(CH.sub.3).dbd.CH--R.sup.21 ; Ar is phenyl, pyridyl, furyl or thienyl; R.sup.2 is --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3, lower-alkylsulphonyl or formyl; R.sup.21 is --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3 or formyl; R.sup.3 is hydrogen or lower-alkyl; and R.sup.4 is hydrogen, hydroxy, amino, lower-alkyl amino, di-(lower alkyl)amino or lower alkyl; with at least one ring of the molecule being heterocyclic, as well as salts of such compounds are useful in rodenticidal compositions containing a bait to eliminate rodents.
    Type: Grant
    Filed: October 5, 1988
    Date of Patent: June 5, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Peter Loeliger, Harald Weiser
  • Patent number: 4929741
    Abstract: Propiolophenone derivatives of the formula ##STR1## wherein R.sup.6 is hydrogen, lower alkyl or a group of the formula ##STR2## as well as corresponding hydroxy compounds of the formula ##STR3## wherein R.sup.6' is hydrogen, lower alkyl, a group of formula (a), (b), (c), (d) or (e) or a group of the formula--C(R.sup.14)(R.sup.15)OR.sup.16' (f'):exhibit mucosa-protective and/or gastric acid secretion-inhibiting properties, such that they can be used for the control or prevention of illnesses of the gastrointestinal tract, especially against gastric ulcers and/or duodenal ulcers.
    Type: Grant
    Filed: March 17, 1988
    Date of Patent: May 29, 1990
    Assignee: Hoffman-La Roche Inc.
    Inventors: Albert Fischli, Eva-Maria Gutknecht, Daniel Obrecht
  • Patent number: 4929609
    Abstract: Compounds of the formula ##STR1## wherein R" is hydrogen or hydroxy, epimers at the 24-position of compounds of formula I, diastereomeric mixtures of compounds of formula I which are epimeric at the 24-position, and mixtures thereof, which are useful as agents for the treatment of psoriasis, and osteoporosis, are described.
    Type: Grant
    Filed: November 14, 1988
    Date of Patent: May 29, 1990
    Assignees: Hoffmann-La Roche Inc., The United States of America as represented by the Department of Agriculture
    Inventors: Andrew D. Batcho, Ronald L. Horst, Milan R. Uskokovic, Joseph L. Napoli
  • Patent number: 4929610
    Abstract: Novel combination preparations containing 1.alpha.,25-dihydroxy vitamin D.sub.3 or 1.alpha.-hydroxy vitamin D.sub.3 and 1.alpha.,24,25(or 1.alpha.,25,26)-trihydroxy vitamin D.sub.3 are described. These preparations are useful in the treatment of various disorders which are characterized by disturbances of the calcium and phosphate metabolism such as osteoporosis and can also be used in animal nutrition.
    Type: Grant
    Filed: July 21, 1989
    Date of Patent: May 29, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Werner Meier, Walter A. Rambeck, Harald Weiser, Hermann Zucker
  • Patent number: 4927826
    Abstract: The invention relates to compounds of the formula ##STR1## Y is O or S, *A is paraphenylene or *--(CH.sub.2).sub.n --(X).sub.m --(CH.sub.2).sub.r --, X is O, S or --CH.dbd.CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R.sub.1 and R.sub.2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl. Het or aryl, *E is ##STR2## or --(CH.sub.2).sub.k -- wherein k is an integer fro 0 to 4. R.sub.3, R.sub.4 and R.sub.8 are independently hydrogen or lower alkyl, R.sub.5 and R.sub.6, independently are hydrogen or lower alkyl, R.sub.
    Type: Grant
    Filed: August 30, 1988
    Date of Patent: May 22, 1990
    Assignee: Hoffman-La Roche Inc.
    Inventors: Robert W. Guthrie, Richard W. Kierstead, Jefferson W. Tilley
  • Patent number: 4927838
    Abstract: The invention relates to compounds of the formula ##STR1## wherein Y and Y' are hydrogen or taken together are O or S, *A is paraphenylene or *----(CH.sub.2).sub.n --(X).sub.s --(CH.sub.2).sub.r ----, X is O, S or --CH.dbd.CH--, n or r, independently, are integers from 0 to 3, m is an integer from 0 to 1, s is an integer from 0 to 1, provided that when s is 1, n+m must be at least 2, t is an integer from 0 to 10, R.sub.1 and R.sub.2, independently, are lower alkyl, lower alkenyl or aryl, or one of R.sub.1 or R.sub.2 is hydrogen and the other is ##STR2## wherein W is ##STR3## --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --, O, S, or ##STR4## and X.sub.1 is lower alkyl, phenyl unsubstituted or mono-, di- or trisubstituted by lower alkoxy, lower alkyl or halogen, and X.sub.2, X.sub.3 and X.sub.4, independently, are hydrogen, lower alkyl, lower alkoxy or halogen, R.sub.3 is hydrogen, lower alkyl or aryl, R.sub.4 is hydrogen, lower alkyl, aryl, aryl-lower alkyl or acyl, R.sub.5 is hydrogen or lower alkyl,R.sub.
    Type: Grant
    Filed: July 5, 1988
    Date of Patent: May 22, 1990
    Assignee: Hoffman-La Roche Inc.
    Inventors: Robert W. Guthrie, Richard W. Kierstead, John G. Mullin, Jefferson W. Tilley
  • Patent number: 4927958
    Abstract: Styryl ketones of the formula ##STR1## wherein R.sup.8 and R.sup.9 are independently hydrogen or lower alkyl or together represent an additional carbon-carbon bond andR.sup.10 is a group of the formula ##STR2## as well as corresponding compounds of the formula ##STR3## wherein R.sup.10' is a group of formula (a), (b), (d) or (e) or a group of the formula--C(R.sup.18)(R.sup.19)OR.sup.20' ; (f')have mucosa-protective and/or gastric acid secretion-inhibiting properties, such that they can be used for the control or prevention of illnesses of the gastrointestinal tract, especially against gastric ulcers or duodenal ulcers.
    Type: Grant
    Filed: March 17, 1988
    Date of Patent: May 22, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Albert Fischli, Eva-Maria Gutknecht, Daniel Obrecht
  • Patent number: 4925278
    Abstract: Compounds of the formula ##STR1## wherein m represents is the number 0 or 1; A is a single covalent bond, --CH.sub.2 --CH.sub.2 --, --OCH.sub.2 --, --COO-- or --OOC--; rings B, C and D are 1,4-phenylene optionally substituted with cyano, halogen or lower alkyl; Y.sup.1 and Y.sup.2 are hydrogen or one of them also is cyano; and R.sup.1 and R.sup.2 each represents C.sub.1 -C.sub.18 -alkyl or C.sub.2 -C.sub.18 alkenyl, either of which is optionally halogen-substituted, in which one CH.sub.2 group or two non-adjacent CH.sub.2 groups is/are optionally replaced by oxygen; with the provisos that at least one of R.sup.1 and R.sup.2 has a chiral carbon atom or a C-C double bond or both when A is --COO-- and at least one of R.sup.1 and R.sup.2 has a C-C double bond when A is a single covalent bond, their preparation, liquid crystalline mixtures containing these compounds and their use for electro-optical purposes are described.
    Type: Grant
    Filed: December 13, 1988
    Date of Patent: May 15, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Buchecker, Hans-Jurgen Fromm, Stephen Kelly, Martin Schadt
  • Patent number: 4925589
    Abstract: Polymers having a monomeric unit of the formula ##STR1## wherein R.sup.1 represents hydrogen, methyl, ethyl, fluorine, chlorine, bromine, cyano or phenyl; X.sup.1 denotes oxygen, sulfur, --NH-- or --N(CH.sub.3)--; R.sup.2 is alkylene with 3-15 carbon atoms in which optionally a non-terminal methylene group is replaced by oxygen or sulfur; X.sup.2 denotes a single covalent bond, oxygen or sulfur; rings A and B each independently represent 1,4-phenylene which is unsubstituted or substituted with halogen, methyl, methoxy and/or cyano and in which optionally one CH group or two CH groups is/are replaced by nitrogen; ring C represents 1,4-phenylene which is unsubstituted or substituted with halogen, methyl, methoxy and/or cyano and in which optionally one CH group or two CH groups is/are replaced by nitrogen or represents trans-1,4-cyclohexylene; n stands for the number 0 and Z.sup.1 stands for --CONH-- or --NHCO--; or n stands for the number 1, one of the groups Z.sup.1 and Z.sup.
    Type: Grant
    Filed: November 28, 1988
    Date of Patent: May 15, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Reinhard Lorenz
  • Patent number: 4920119
    Abstract: Compounds of the formula ##STR1## wherein A represents a grouping of the formula ##STR2## in which R.sup.1 and R.sup.2 each individually represent hydrogen, halogen, trifluoromethyl, nitro, amino, cyano, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.3 -C.sub.6 -alkenyloxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 14 C.sub.6 -alkanoylamino, aryloxy, aryl-(C.sub.1 -C.sub.6 -alkyl), aryl-(C.sub.1 -C.sub.6 -alkoxy), aryl-(C.sub.1 -C.sub.6 -alkoxy)carbonylamino or a group of the formula --O--CH.sub.2 --R.sup.3 or R.sup.1 and R.sup.2 on adjacent carbon atoms together represent a group of the formula --CH.dbd.CH--CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --O-- and R.sup.3 represents hydroxy-(C.sub.1 -C.sub.4 -alkyl) or vicinal dihydroxy-(C.sub.2 -C.sub.5 -alkyl), and pharmaceutically acceptable acid addition salts of those compounds of formula I in which R.sup.1 and/or R.sup.
    Type: Grant
    Filed: November 24, 1987
    Date of Patent: April 24, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael R. Attwood, Peter H. Crackett, Geoffrey Lawton
  • Patent number: 4916145
    Abstract: The invention relates to compounds of the formula ##STR1## wherein *B is ##STR2## Y is O or S, *A is *--(CH.sub.2).sub.n --(X).sub.m --(CH.sub.2).sub.r --, n or r, independently, are integers from 0 to 3, m is an integer from 0 to 1, provided that when m is 1, then n must be at least 1, X is O or S, R.sub.1 and R.sub.4, independently, are hydrogen, lower alkyl, hydroxy or lower alkoxy, provided that when *B is other than ##STR3## at least one of R.sub.1 and R.sub.4, and one of R.sub.6 and R.sub.7 must be hydrogen, R.sub.2 and R.sub.3 are independently hydrogen, lower alkyl, cycloalkyl, halogen, nitro, lower alkoxy, lower alkenyl, lower alkynyl or aryl, R.sub.5 and R.sub.6, independently are hydrogen or lower alkyl, R.sub.
    Type: Grant
    Filed: July 10, 1987
    Date of Patent: April 10, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jefferson W. Tilley, Robert W. Guthrie, John W. Clader, Ronald A. LeMahieu
  • Patent number: 4916069
    Abstract: The present invention relates to novel coenyme independent L-sorbose dehydrogenase and a process for producing the same. The enzyme provided by the present invention catalyzes the oxidation of L-sorbose to L-sorbosone, the precursor of 2-keto-L-gulonic acid which is an important intermediate in the production of vitamin C.Due to the release duties in foreign countries, the original deposits with respect to the following strains have been transferred to the deposit under the Budapest Treaty at Agency of Industrial Science and Technology, Fermentation Research Institute, Japan on Jan. 29, 1987. And the following accession numbers have been allotted to each strain.______________________________________ strain Old No. New No. ______________________________________ Gluconobacter oxydans FERM-P No. 8422, Accession No. UV-10 FERM BP-1267 Gluconobacter oxydans E-1 FERM-P No. 8353, Accession No. FERM BP-1265 Gluconobacter oxydans H-2 FERM-P No. 8354, Accession No. FERM BP-1266 Gluconobacter oxydans L-8 FERM-P No.
    Type: Grant
    Filed: May 29, 1987
    Date of Patent: April 10, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Akiko Fujiwara, Tatsuo Hoshino, Teruhide Sugisawa
  • Patent number: 4913851
    Abstract: An asymmetric synthesis for Vitamin E in an optically active pure form for 4-(2,5-diloweralkanoyloxy)-3,4,6-trimethylphenyl-butan-2-one and intermediates therein.
    Type: Grant
    Filed: May 15, 1989
    Date of Patent: April 3, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ka-kong Chan, Gabriel G. Saucy
  • Patent number: 4914217
    Abstract: An asymmetric synthesis for Vitamin E in an optically active pure form for 4-(2,5-diloweralkanoyloxy)-3,4,6-trimethylphenyl-butan-2-one and intermediates therein.
    Type: Grant
    Filed: May 15, 1989
    Date of Patent: April 3, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ka-kong Chan, Gabriel G. Saucy
  • Patent number: 4914095
    Abstract: A compound of the formula ##STR1## is useful to treat psychotic disorders in humans, especially schizophrenia, and to prevent exacerbations thereof. The compound can be used as a single therapeutic agent or in combination with neuroleptics such as haloperidol.
    Type: Grant
    Filed: January 13, 1989
    Date of Patent: April 3, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Walter Merz