Patents Represented by Attorney Bernard S. Leon
  • Patent number: 4804502
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or hydroxy and R.sub.2 is hydrogen or fluorine are described. The compounds of formula I are useful as agents in the treatment of disease states characterized by metabolic calcium deficiencies. Examplary of such disease states are osteoporosis and renal osteodystrophy.
    Type: Grant
    Filed: January 20, 1988
    Date of Patent: February 14, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Enrico G. Baggiolini, John J. Partridge, Shian-Jan Shiuey, Gary A. Truitt, Milan R. Uskokovic
  • Patent number: 4801704
    Abstract: There are presented compounds of the formula ##STR1## wherein R.sub.2, R.sub.3, R.sub.4 and m are as described herein.
    Type: Grant
    Filed: May 16, 1988
    Date of Patent: January 31, 1989
    Assignee: Hoffman-La Roche Inc.
    Inventors: Dennis D. Keith, Chung-Chen Wei, Manfred Weigele
  • Patent number: 4801584
    Abstract: The invention is concerned with tricyclic compounds of the formula ##STR1## wherein R.sup.1 is a hydrogen atom or a carboxy-protecting radical; R.sup.2 is a hydrogen atom or a lower alkyl radical which may be substituted with a halogen atom; R.sup.3 and R.sup.4 independently are a hydrogen atom or a lower alkyl radical which may be substituted with a hydroxy radical or a substituted or unsubstituted amino radical; X is a halogen atom; and R.sup.5 and R.sup.6 are independently a hydrogen atom or a lower alkyl radical which may be substituted with a hydroxy radical, a lower alkoxy radical or a substituted or unsubstituted amino radical; or R.sup.5 and R.sup.6, taken together with the adjacent nitrogen atom, may form a 5 to 7 membered heterocyclic ring which may be substituted with one or more substituents at the carbon atom(s), and the heterocyclic ring may further contain --NR.sup.7 --, --O--, --S--, --SO--, --SO.sub.2 -- or --NR.sup.7 --CO--, and also R.sup.
    Type: Grant
    Filed: September 8, 1987
    Date of Patent: January 31, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kazuteru Yokose, Nobuo Shimma, Miyako Kamata, Masahiro Aoki, Tatsuo Ohtsuka
  • Patent number: 4800206
    Abstract: Pyridine-ethanolamines of the formula ##STR1## wherein n, X, Y, R.sup.1, R.sup.2 and R.sup.3 have the significances given in the description, their corresponding enantiomers, diastereomers, and racemates as well as the pysiologically compatible salts thereof are describe. The compounds of formula I have catabolic activity and can be used for the treatment of obesity and of diabetes mellitus or of conditions which are associated with an increased protein breakdown, or as feed additives for fattening animals. The compounds of formula I can be prepared by alkylating the primary or secondary amines corresponding to the secondary or tertiary amines of formula I.
    Type: Grant
    Filed: June 3, 1987
    Date of Patent: January 24, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Marcel Muller
  • Patent number: 4792557
    Abstract: 2,4-Diamino-5-benzylpyrimidines of the formula ##STR1## wherein R.sup.1, R.sup.2, A, Z and n are as hereinafter set forth, are described. The 2,4-diamino-5-benzylpyrimidines of the invention have useful antibacterial activity. More particularly, they inhibit bacterial dihydrofolate reductase and potentiate the antibacterial activity of sulfonamides.
    Type: Grant
    Filed: January 14, 1987
    Date of Patent: December 20, 1988
    Assignee: Hoffman-La Roche Inc.
    Inventors: Ivan Kompis, G/e/ rald Rey-Bellet, Guido Zanetti
  • Patent number: 4789453
    Abstract: A combined sensor for sensing partial O.sub.2 pressure and partial CO.sub.2 pressure and comprising measuring electrodes, a reference electrode, a diaphragm covering the electrodes and an electrolyte layer between the electrodes and the diaphragm wherein the reference electrode has disposed around it a screening of gold which is at the same potential as the reference electrode and the electrolyte contains a defined concentration of a soluble silver compound or of a silver complex.
    Type: Grant
    Filed: January 25, 1988
    Date of Patent: December 6, 1988
    Assignee: Kontron Holding A.G.
    Inventors: Patrick Eberhard, Wolfgang Mindt, Jean-Pierre Palma
  • Patent number: 4788206
    Abstract: Compounds of the formula ##STR1## Y is O ir S, *A is paraphenylene or *----(CH.sub.2)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, aryl, R.sub.3, R.sub.4 and R.sub.8, independently, are hydrogen, lower alkyl, aryl, R.sub.5 and R.sub.6, independently, are hydrogen or lower alkyl, R.sub.7 is hydrogen, lower alkyl, cycloalkyl, Het-lower alkyl or aryl, Het is a monocyclic 5- or 6-membered hetero aromatic or a bicyclic heteroaromatic radical containing one or two hetero atoms selected from nitrogen, oxygen and sulfur, which radical may be substituted by lower alkyl, halogen or aryl, and the asterisk denotes the point of attachment,and when R.sub.6 and R.sub.7 are different, their enantiomers and racemic mixtures thereof, when R.sub.1 and R.sub.
    Type: Grant
    Filed: July 10, 1987
    Date of Patent: November 29, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Robert W. Guthrie, Richard W. Kierstead, Jefferson W. Tilley
  • Patent number: 4788214
    Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; R.sup.2 is hydrogen or halogen; R.sup.3, R.sup.4 and R.sup.5 are hydrogen, acyl or lower alkyl; R.sup.6 and R.sup.7, independently, are hydrogen or lower alkyl; X is alkylene.sub.3-7 ; and n is an integer of zero to four; provided that only one of R.sup.3, R.sup.4 or R.sup.5 can be acyl;enatiomers thereof, and, when R.sup.7 is hydrogen, salts thereof with pharmaceutically acceptable bases.The compounds of formulas I and II are useful as agents for the treatment of allergic conditions.
    Type: Grant
    Filed: September 15, 1986
    Date of Patent: November 29, 1988
    Assignee: Hoffman-La Roche Inc.
    Inventors: Noal Cohen, Giuseppe F. Weber
  • Patent number: 4786646
    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 from 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: July 10, 1987
    Date of Patent: November 22, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Robert W. Guthrie, Richard W. Kierstead, Jefferson W. Tilley
  • Patent number: 4785093
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, alkanoyl or aroyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or aryl; R.sup.4 and R.sup.5 each are hydrogen or R.sup.4 and R.sup.5 taken together are oxo; and Y is --CH.sub.2 --, --CH.sub.2 CH.sub.2 --or--N(R.sup.6)--in which R.sup.6 is hydrogen, alkyl or aralkyl, as well as pharmaceutically acceptable salts thereof with bases when R.sup.2 is hydrogen and pharmaceutically acceptable salts thereof with acids when Y is --N(R.sup.6)--, which have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations, are described.The compounds of formula I contain at least one asymmetric carbon atom. Therefore, the invention comprises not only the optically uniform forms of these compounds, but also the various diastereoisomeric racemates and mixtures of different diastereoisomeric racemates.
    Type: Grant
    Filed: May 11, 1987
    Date of Patent: November 15, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Cedric H. Hassall, Geoffrey Lawton, Sally Redshaw
  • Patent number: 4785017
    Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; R.sup.2 is hydrogen or halogen; R.sup.3, R.sup.4 and R.sup.5 are hydrogen, acyl or lower alkyl; R.sup.6 and R.sup.7, independently, are hydrogen or lower alkyl; X is alkylene.sub.3-7 ; and n is an integer of zero to four; provided that only one of R.sup.3, R.sup.4 or R.sup.5 can be acyl;enantiomers thereof, and, when R.sup.7 is hydrogen, salts thereof with pharmaceutically acceptable bases.The compounds of formulas I and II are useful as agents for the treatment of allergic conditions.
    Type: Grant
    Filed: May 29, 1984
    Date of Patent: November 15, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Noal Cohen, Giuseppe F. Weber
  • Patent number: 4783280
    Abstract: There is described a liquid crystalline mixture for electro-optical devices which are operated according to the two-frequency matrix addressing procedure. The mixture consists of three components A, B and C, each of which contains one or more compounds. Component A has a viscosity of at most about 40 cp, a clearing point of at least about 40.degree. C. and a dielectric anisotropy between about -2 and about +1. Component B has a dielectric anisotropy below about -2 both above and below the cross-over frequency of the total mixture and component C has a dielectric anisotropy above about +10, a clearing point of at least about 100.degree. C. and there is a cross-over frequency in the total mixture of at most about 15 kHz at 20.degree. C. Novel compounds for such mixtures and their manufacture and use are also described. The novel mixtures make possible especially high multiplex rates and short response times.
    Type: Grant
    Filed: May 20, 1987
    Date of Patent: November 8, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Martin Petrzilka, Martin Schadt, Alois Villiger
  • Patent number: 4782176
    Abstract: Phenoxycarboxylic acids of the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 R.sub.5, Z and n are as hereinafter set forth, are as described. The compounds of formula I are antagonists of slow reacting substance of anaphylaxis (SRS-A), which renders them useful as agents for the treatment of allergic conditions.
    Type: Grant
    Filed: May 23, 1983
    Date of Patent: November 1, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Matthew Carson, Ronald A. LeMahieu, William C. Nason
  • Patent number: 4782149
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently represent hydrogen, C.sub.1 -C.sub.10 -alkyl, adamantyl-(C.sub.1 -C.sub.4 -alkyl) or (C.sub.2 -C.sub.6 -alkanoyloxy)-(C.sub.1 -C.sub.4 -alkyl), and pharmaceutically acceptable salts thereof possess antihypertensive activity and can be used as theraputic or prophylactic agents in pharmaceutical preparations. Intermediates for the production of such compounds are also provided.
    Type: Grant
    Filed: March 17, 1988
    Date of Patent: November 1, 1988
    Assignee: Hoffman-La Roche Inc.
    Inventors: Geoffrey Lawton, Sally Redshaw
  • Patent number: 4775756
    Abstract: The invention relates to substituted phenylbarbituric acids of the formula ##STR1## wherein R.sup.1 and R.sup.3, independently, are lower-alkoxy or lower-alkylthio; R.sup.2 is lower-alkoxy, hydroxy or amino; and R.sup.4 is hydrogen; or R.sup.1 and R.sup.2 are lower-alkoxy, R.sup.3 is hydrogen and R.sup.4 is lower-alkyl,which are prepared from correspondingly substituted benzene derivatives and alloxan. The compounds of formula I can be converted into substituted benzaldehydes which in turn are known intermediates in the preparation of pharmaceutically valuable benzylpyrimidines.
    Type: Grant
    Filed: October 10, 1986
    Date of Patent: October 4, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Dieter Kagi
  • Patent number: 4775671
    Abstract: There is presented compounds of the formula ##STR1## wherein A together with the two carbon atoms denoted by .alpha. and .beta. signifies one of the groups ##STR2## and the dotted line signifies the double bond present in cases (1), (2) and (4) and wherein R.sup.1 signifies a 5- or 6-membered aromatic heterocyclic group or the group --C(R.sup.6).dbd.NOR.sup.7 (B), R.sup.2 signifies hydrogen and R.sup.3 signifies hydrogen or lower alkyl or R.sup.2 and R.sup.3 together signify dimethylene, trimethylene or propenylene, R.sup.4 and R.sup.5 each signify hydrogen, halogen, trifluoromethyl, cyano, nitro, amino or lower alkyl, R.sup.6 signifies hydrogen or lower alkyl and R.sup.7 signifies lower alkyl, the compound of formula I having the (S) or (R,S) configuration with reference to the carbon atom denoted by .gamma. when R.sup.2 and R.sup.
    Type: Grant
    Filed: November 18, 1987
    Date of Patent: October 4, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Walter Hunkeler, Emilio Kyburz
  • Patent number: 4774253
    Abstract: Oxazole and isoxazole derivatives of the formula ##STR1## wherein A is C.sub.1-6 -alkylene, Het is a 2-R-oxazol-5-yl, 5-R-oxazol-2-yl, 4-R-oxazol-2-yl, 2-R-oxazol-4-yl, 3-R-isoxazol-5-yl or 5-R-isoxazol-3-yl group which is optionally substituted on the heterocyclic ring by a C.sub.1-6 -alkyl group, R is phenyl or thienyl monosubstituted or disubstituted by halogen, trifluoromethyl or C.sub.1-6 -alkylthio, R.sup.1 and R.sup.2 each is a C.sub.1-6 -alkyl group and R.sup.3 is a hydroxy or C.sub.1-6 -alkoxy group or a group of the formula --NR.sup.4 R.sup.5 in which R.sup.4 and R.sup.5 each is a hydrogen atom or a C.sub.1-6 -alkyl group or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached is a 5-membered or 6-membered saturated heteromonocyclic ring which may contain an oxygen or sulphur atom or an additional nitrogen atom, and pharmaceutically acceptable salts of the compounds of formula I in which R.sup.3 is a hydroxy group with bases, have anti-arthritic activity.
    Type: Grant
    Filed: October 10, 1986
    Date of Patent: September 27, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Peter J. Machin, John M. Osbond, Christopher R. Self, Carey E. Smithen, Brian P. Tong
  • Patent number: 4774330
    Abstract: There is presented compounds of the formula ##STR1## wherein X represents the 1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-as-triazin-3-yl group or its corresponding tautomeric form, the 2,5-dihydro-6-hydroxy-2-methyl-5-oxo-as-triazin-3-yl group, and the readily hydrolyzable esters, readily hydrolyzable ethers and salts of the compounds and hydrates of the compounds of formula I or of their esters, ethers and salts. Also provided is a method of their manufacture and intermediates therefor as well as corresponding pharmaceutical preparations.
    Type: Grant
    Filed: April 1, 1987
    Date of Patent: September 27, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Roland Reiner
  • Patent number: 4774249
    Abstract: The pyrimidine derivatives of formula I ##STR1## wherein R.sup.1 is naphthyl, substituted naphthyl or substituted phenyl; R.sup.2 is hydrogen or lower alkoxy; and A is an optionally present ethylene or 1,3-propylene, and wherein the diaminopyridine group has the exo-configuration when A is present, are described. These compounds are useful as antibacterial agents, antimalarial agents and antitumor agents, and can be used in combination with sulfonamides in the control of bacterial infections.
    Type: Grant
    Filed: October 23, 1987
    Date of Patent: September 27, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ivan Kompis, Rita Locher, Hans Maag
  • Patent number: 4772701
    Abstract: Novel compounds of the formula ##STR1## wherein B represents a methylene, ethylene or vinylene group, R.sup.1 represents a hydrogen atom or an alkyl, aralkyl, amino-alkyl, mono-alkylamino-alkyl, dialkylamino-alkyl, acylamino-alkyl, phthalimido-alkyl, alkoxycarbonylamino-alkyl, aryloxycarbonylamino-alkyl, aralkoxycarbonylamino-alkyl, alkylaminocarbonylamino-alkyl, arylaminocarbonylamino-alkyl, aralkylaminocarbonylamino-alkyl, alkylsulphonyl-amino-alkly or arylsulphonylamino-alkyl group, R.sup.2 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl carbonyl group or a group of the formula ##STR2## R.sup.3 represents a carboxyl, alkoxycarbonyl or aralykoxycarbonyl group, R.sup.4 and R.sup.5 each represent a hydrogen atom or R.sup.4 and R.sup.5 together represent an oxo group; R.sup.6 and R.sup.7 each represent a hydrogen atom or an alkyl or aralkyl group or R.sup.6 and R.sup.
    Type: Grant
    Filed: November 28, 1986
    Date of Patent: September 20, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael R. Attwood, Cedric H. Hassall, Robert W. Lambert, Geoffrey Lawton, Sally Redshaw