Patents Represented by Attorney, Agent or Law Firm Richard J. Mazza
  • Patent number: 5574018
    Abstract: Therapeutically useful proteins are conjugated to vitamin B.sub.12 by covalent binding at the primary hydroxyl site of the ribose moiety. The resulting conjugates are biologically active and can be formulated into pharmaceutical compositions suitable for delivery by various routes of administration, preferably oral. Uptake in the gut following oral delivery is further enhanced by the co-administration of purified intrinsic factor.
    Type: Grant
    Filed: July 29, 1994
    Date of Patent: November 12, 1996
    Assignee: Amgen Inc.
    Inventors: Alan D. Habberfield, Olaf B. Kinstler, Colin G. Pitt
  • Patent number: 5538861
    Abstract: A protein which is a stimulator of and presumed ligand for the axl receptor has been identified and sequenced. The protein, termed gas6, bears homology to human protein S and is a growth factor for tissues which express axl.
    Type: Grant
    Filed: July 29, 1994
    Date of Patent: July 23, 1996
    Assignees: Amgen Inc., Claudio Schneider
    Inventors: Claudio Schneider, Brian C. Varnum, Giancarlo Avanzi, Claudio Brancolini, Guidalberto Manfioletti
  • Patent number: 5466447
    Abstract: The present invention provides a therapeutic method of treating a human subject for psoriasis which comprises administering to the subject an effective psoriatic dermatosis-inhibiting amount of IL-2 and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: April 21, 1994
    Date of Patent: November 14, 1995
    Assignee: Amgen Inc.
    Inventors: Robert I. Abels, Karen Reilly
  • Patent number: 5350690
    Abstract: This disclosure relates to a sucrose inducible expression system. The sucrose inducible expression system comprises a novel plasmid vector having a sacY gene of the sacS locus which binds to a transcription terminator to relieve transcription termination when introduced into a B. subtilis host microorganism.
    Type: Grant
    Filed: April 28, 1992
    Date of Patent: September 27, 1994
    Assignee: Amgen Inc.
    Inventor: Mark M. Zukowski
  • Patent number: 5284656
    Abstract: Granulocyte-colony stimulating factor (G-CSF) can be delivered systemically in therapeutically or prophylactically effective amounts by pulmonary administration using a variety of pulmonary delivery devices, including nebulizers, metered dose inhalers and powder inhalers. Aerosol administration in accordance with this invention results in significant elevation of the neutrophil levels that compares favorably with delivery by subcutaneous injection. G-CSF can be administered in this manner to medically treat neutropenia, as well as to combat or prevent infections.
    Type: Grant
    Filed: September 29, 1992
    Date of Patent: February 8, 1994
    Assignee: Amgen Inc.
    Inventors: Robert M. Platz, Mark A. Winters, Colin G. Pitt
  • Patent number: 5104651
    Abstract: A stable pharmaceutically acceptable formulation containing a pharmaceutically acceptable amount of a protein is disclosed. Also disclosed are associated means and methods for preparing such formulations.
    Type: Grant
    Filed: December 16, 1988
    Date of Patent: April 14, 1992
    Assignee: Amgen Inc.
    Inventors: Thomas C. Boone, William C. Kenney
  • Patent number: 4885309
    Abstract: The compound 6-acetyl-7-[5-(4-acetyl-3-hydroxy-2-propylphenoxy)pentyloxy]-3,4-dihydro-2 4-1-benzopyran-2-carboxylic acid, as well as its enantiomers, salts and lower alkyl esters, are useful in topically administrable dosage forms for the treatment of leukotriene-mediated dermal inflammations, such as psoriasis. These compounds can be formulated into creams, ointments, lotions, gels and other types of compositions suitable for applying on the skin.
    Type: Grant
    Filed: August 1, 1986
    Date of Patent: December 5, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Ann F. Welton
  • Patent number: 4876349
    Abstract: The compounds of the formula ##STR1## wherein X and Y are independently --CH.sub.2 -- or >C(CH.sub.3).sub.2 ; Z is --CHR.sup.8 --, >Co, >CR.sup.8 OR.sup.7 , --CHR.sup.8 --CHR.sup.8 --, --CHOR.sup.7 --CH.sub.2 --, --CO--CHOR.sup.7 or --CHOR.sup.7 --CHOR.sup.7 --R.sup.1 is a 5- or 6-membered, monocyclic heterocyclic group which optionally can be C-substituted by halogen, lower-alkyl, lower-alkoxy, acyloxy, nitro, hydroxy, amino, lower-alkylamino or di-lower-alkylamino and/or which can be substituted on a ring --NH-- group by lower-alkyl; R.sup.2 and R.sup.3 are independently hydrogen, lower-alkyl, trifluoromethyl or halogen and one of R.sup.2 and R.sup.3 always is trifluoromethyl or lower-alkyl; R.sup.4 and R.sup.5 are independently hydrogen, alkyl, alkoxy or halogen; R.sup.6 is hydrogen, lower-alkyl or --OR.sup.7 ; R.sup.7 is hydrogen, lower-alkyl or acyl; R.sup.8 is hydrogen or lower-alkyl; and R.sup.7 and R.sup.8 can be the same or different from one another.
    Type: Grant
    Filed: July 10, 1987
    Date of Patent: October 24, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Ekkehard Weiss
  • Patent number: 4876340
    Abstract: Benzazecinediones of the formula ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen or chlorine, R.sup.3 is hydrogen, fluorine, chlorine, bromine or methoxy, R.sup.4 is hydrogen, chlorine or methoxy and R.sup.5 is hydrogen, acetyl, propionyl, benzoyl, chlorobenzoyl, methoxybenzoyl or phenylacetyl, with the proviso that 2 or 3 of the groups R.sup.1 to R.sup.4 are hydrogen, as well as many of the corresponding benzo[f]quinolines from which these benzazecinediones can be prepared by oxidation are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions in mammals. They can be produced according to various processes and can be prepared into pharmaceutical compositions.
    Type: Grant
    Filed: February 11, 1988
    Date of Patent: October 24, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Werner Aschwanden, Rene Imhof, Roland Jakob, Emilio Kyburz
  • Patent number: 4863920
    Abstract: A compound for treating disorders of the central nervous system, which is of the formulawherein A taken together with the two carbon atoms denoted by .alpha. and .beta. is one of the following groups: ##STR1## R.sup.1 is one of the following groups:--CH.dbd.CH--R.sup.6 (d)and--C.tbd.C--R.sup.6, (e)R.sup.2 is hydrogen, R.sup.3 is lower alkyl, or R.sup.2 and R.sup.3 together are dimethylene or trimethylene, R.sup.4 and R.sup.5 are independently hydrogen, halogen, trifluoromethyl or lower alkyl, and R.sup.6 is hydrogen, halogen, aryl or a saturated lower hydrocarbon group which is optionally mono- or di-substituted by hydroxy, lower alkoxy, (C.sub.3 -C.sub.7)-cycloalkyl or oxo, wherein the compound has the (S)- or (R,S)-configuration with reference to the carbon atom denoted by .gamma. when R.sup.2 and R.sup.3 together are dimethylene or trimethylene and, further, the double bond present in group (d) has the E- and/or Z-configuration when R.sup.6 is different from hydrogen.
    Type: Grant
    Filed: March 3, 1988
    Date of Patent: September 5, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Walter Hunkeler, Emilio Kyburz, Marc Meier
  • Patent number: 4830470
    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: May 20, 1987
    Date of Patent: May 16, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Buchecker, Hans-Jurgen Fromm, Stephen Kelly, Martin Schadt
  • Patent number: 4831130
    Abstract: Compounds of the formula ##STR1## wherein A is one of the following: ##STR2## in which R.sub.1, is acyl, R.sub.2 is hydrogen, lower alkyl, lower alkoxycarbonyl or aminocarbonyl, R.sub.3 is hydrogen or lower alkyl and R.sub.4 and R.sub.4 ' are hydrogen, lower alkyl, lower alkoxy, acyl or aralkyl, as well as pharmaceutically acceptable salts of such compounds, are useful as antibacterial agents.
    Type: Grant
    Filed: July 10, 1987
    Date of Patent: May 16, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Harry A. Albrecht, Frederick M. Konzelmann, Dennis D. Keith
  • Patent number: 4820734
    Abstract: The novel phenethylamine derivatives of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each signify hydrogen, halogen, trifluoromethyl, lower alkoxy, lower alkyl, hydroxy or nitro, with the proviso that at least one of R.sup.1 and R.sup.2 is different from hydrogen, R.sup.3 and R.sup.4 each signify lower alkyl, n signifies the number 1, 2, 3 or 4 and B signifies the group --CO-- or --CHOH--, and their pharmaceutically acceptable acid addition salts have interesting analgesic and antidepressant properties. These substances can be manufactured according to various methods which are known per se and can be used as medicaments in the form of pharmaceutical preparation.
    Type: Grant
    Filed: November 4, 1987
    Date of Patent: April 11, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Hans Bruderer
  • Patent number: 4816476
    Abstract: Heterocyclic compounds of the formula ##STR1## wherein X is --CH.dbd.CH--, --O-- or --S--; R.sup.1 is a 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 a group --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 a group --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 alkylamino, di-(lower alkyl)amino or lower-alkyl; at least one ring of the molecule being heterocyclic, salts thereof, processes for their preparation, rodenticidal compositions containing these compounds as the active ingredient and methods of use of the rodenticidal compositions are disclosed.
    Type: Grant
    Filed: December 12, 1986
    Date of Patent: March 28, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Peter Loeliger, Harald Weiser
  • Patent number: 4816582
    Abstract: Antimicrobial 2-oxo-1-azetidinesulphonic acids of the formula ##STR1## in which H.sub.2 N ##STR2## represents an amino-substituted thiazolyl group, R.sup.1 is lower alkyl which is substituted by carbamoyl, lower alkylsuphonyl, azido, piperidine-carbonyl, (hexahydro-1H-azepin-1-yl)carbonyl or lower alkynyl, and R.sup.2 is hydrogen or a lower organic group, typically, carbamoyloxymethyl.
    Type: Grant
    Filed: October 22, 1987
    Date of Patent: March 28, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andre Furlenmeier, Werner Hofheinz, Christian N. Hubschwerlen, Hans P. Isenring
  • 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: 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: 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: 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: 4772718
    Abstract: A process for the manufacture of 5-cyano-4-methyl-oxazole which comprises reacting a 5-(lower alkoxycarbonyl)-4-methyl-oxazole with ammonia in the gaseous phase, in the presence of a zirconium oxide or hafnium oxide catalyst.
    Type: Grant
    Filed: October 24, 1986
    Date of Patent: September 20, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Paul Nosberger