Patents Represented by Attorney, Agent or Law Firm Ross J. Oehler
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Patent number: 6433172Abstract: This invention is directed to methods for stereospecifically preparing [(1-optionally substituted aryl)- or (1-optionally substituted heteroaryl)]-2-substituted ethyl-2-amines, having chirality at the 2-position, and to intermediates to the substituted ethyl-2-amines.Type: GrantFiled: October 25, 1999Date of Patent: August 13, 2002Assignee: Aventis Pharmaceuticals Inc.Inventors: Luc Grondard, Jean-Paul Casimir, Patrick Leon, Michael K. O'Brien, Matthew R. Powers, Daniel Robin
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Patent number: 6309668Abstract: This invention relates to an abuse resistant tablet containing two or more layers having one or more drugs and one or more gelling agents and its preparation. The drug(s) and gelling agent(s) are in separate layers of the tablet. The multilayer tablet is particularly suitable for the administration of drugs prone to abuse by unauthorized parenteral administration such as analgesics, hypnotics, and anxiolytics.Type: GrantFiled: July 30, 1996Date of Patent: October 30, 2001Assignee: Aventis Pharma LimitedInventors: Richard James Bastin, Bruce Hamilton Lithgow
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Patent number: 6133409Abstract: This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and .alpha.,.beta.-unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.Type: GrantFiled: June 24, 1998Date of Patent: October 17, 2000Assignee: Aventis Pharmaceuticals Products Inc.Inventors: Joseph M. Salvino, George C. Morton, Helen J. Mason, Richard F. Labaudiniere
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Patent number: 6127550Abstract: This invention is directed to methods for stereospecifically preparing [(1-optionally substituted aryl)- or (1-optionally substituted heteroaryl)]-2-substituted ethyl-2-amines, having chirality at the 2-position, and to intermediates to the substituted ethyl-2-amines.Type: GrantFiled: March 11, 1999Date of Patent: October 3, 2000Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Luc Grondard, Jean-Paul Casimir, Patrick Leon, Michael K. O'Brien, Matthew R. Powers, Daniel Robin
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Patent number: 6120805Abstract: Biocompatible microspheres containing one or more active principals, a biodegradable and biocompatible polymer and a surface-active agent which is also biodegradable and biocompatible, contain less than 10 ppm of heavy metals. These microspheres are prepared by providing a solution of the polymer and of the active principal in a water-immiscible solvent which is more volatile than water and mixing with an aqueous solution of the surface-active agent, followed by evaporation of the solvent.Type: GrantFiled: May 31, 1995Date of Patent: September 19, 2000Assignee: Rhone-Poulenc Rorer SAInventors: Gilles Spenlehauer, Michel Veillard, Thierry Verrechia
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Patent number: 6109261Abstract: There is provided a device for the administration of an inhalation medicament, including a body defining a through-going air pathway having a longitudinal axis, an air inlet, an air outlet forming a mouthpiece, means for dispensing medicament into the pathway and air flow regulating means, characterized in that the air flow regulating means includes a movable obstructing means adapted to reduce the cross-sectional area of the pathway at a location between the air inlet and the means for dispensing medicament, and biassing means, whereby the obstructing means is biassed into a first resting position in which the cross-sectional area of the pathway is minimum and is adapted to move against the bias of the biassing means to a second position in which the cross-section area of the pathway is maximum in response to a pressure fall at the mouthpiece caused by inhalation and is adapted to move farther to a third position in which the cross-sectional area of the pathway is less than maximum in response to a greater pType: GrantFiled: January 14, 1998Date of Patent: August 29, 2000Assignee: Fisons plcInventors: Alastair Robert Clarke, Clive Sleath, Michael Trevor Shepherd
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Patent number: 6103705Abstract: The invention is also directed to pharmaceutical composition comprising a compound having anti-Xa activity, a platelet aggregation antagonist compound and a pharmaceutically acceptable carrier. The invention is also directed to a method of treating or preventing a thrombogenic condition associated with a thrombosis related ischemic disorder in a patient comprising administering to said patient pharmaceutically effective amounts of a compound having anti-Xa activity and a platelet aggregation antagonist compound. In addition, this invention is directed to the use of pharmaceutically effective amounts of a compound having anti-Xa activity and a platelet aggregation antagonist compound in the preparation of a medicament for treating or preventing a physiological condition associated with thrombosis related ischemic disorder.Type: GrantFiled: November 16, 1998Date of Patent: August 15, 2000Assignee: Aventis Pharmaceuticals Products Inc.Inventors: Andre Uzan, Alain H. Curaudeau, Robert J. Leadley, Christopher T. Dunwiddie, Mark H. Perrone
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Patent number: 6096768Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.Type: GrantFiled: April 29, 1999Date of Patent: August 1, 2000Assignee: Rhone-Poulenc Rorer LimitedInventors: Michael John Ashton, David Charles Cook, Garry Fenton, Susan Jacqueline Hills, Ian Michael McFarlane, Andrew David Morley, Malcolm Norman Palfreyman, Andrew James Ratcliffe, Brian William Sharp, Sukanthini Thurairatnam, Bernard Yvon Jack Vacher, Nigel Vicker
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Patent number: 6092522Abstract: An inhaler for inhaling pulverulent medicament from within a capsule comprises a chamber 24 within which the capsule is free to rotate while having its longitudinal axis in the median plane of the chamber and thus generally parallel to the front and rear walls 30 and 31 of the chamber, by virtue of the fact that the spacing between said front and rear walls is less than the axial length of the capsule but just greater than the diameter of the capsule. The device includes pins 21 serving as opening means to pierce the ends of the capsule while it is seated in a recess 25, whereupon the retraction of the pins 21 allows the capsule to be entrained into swirling airflow in the chamber 24 during inhalation of air through air inlets 26 and out through a mouthpiece nozzle 27.Type: GrantFiled: February 29, 1996Date of Patent: July 25, 2000Assignee: Rhone-Poulenc Rorer LimitedInventors: John Richard Calvert, Robert Stanley Cook, Michael Anthony Hobbs, Ann-Marie Leighton, Gordon Thomas Simpkin, Roy Trunley, Anthony Douglas West
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Patent number: 6080767Abstract: The compounds according to the invention are substituted N-[(aminoiminomethyl or aminomethyl)phenyl]propyl amides of formula I herein which exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More especially, they are Factor Xa inhibitors. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, methods for their preparation and their use, which are for treating a patient suffering from, or subject to, conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.Type: GrantFiled: June 27, 1997Date of Patent: June 27, 2000Assignee: Aventis Pharmaceuticals Products Inc.Inventors: Scott I. Klein, Kevin R. Guertin, Alfred P. Spada
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Patent number: 6074580Abstract: Pearls of an active principle exhibiting an indefinite crystallization point, wherein said pearls exhibit a prolonged, immediate or combination release profiles, are made by melting the active principle and a crystallization excipient to create a molten mixture; introducing the mixture into feed receptacles of a prilling tower; passing the mixture through a nozzle which is vibrated to form pearls; and allowing the pearls to fall in the tower countercurrentwise to cold air, where the tower is provided with a fluidized bed proximate the bottom of the tower and the temperature conditions of the said fluidized bed are maintained depending on the release profile desired.Type: GrantFiled: December 3, 1996Date of Patent: June 13, 2000Assignee: Aventis Pharma SAInventors: Jean-claude Le Thiesse, Michel Deleuil
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Patent number: 6048893Abstract: This invention is directed to compounds of formula I ##STR1## wherein R.sup.1 is CN, CH.sub.2 CN, CH.dbd.CHCN, CHO, or CH.dbd.CHCO.sub.2 H;R.sup.2 is aryl lower alkoxy, heteroaryl lower alkoxy, aryl lower alkylthio or heteroaryl lower alkylthio wherein each of the aryl and heteroaryl moieties is optionally substituted;R.sup.3 is halogen;R.sup.4 is optionally substituted aryl or optionally substituted heteroaryl;R.sup.5 is carboxy or an acid isostere;X is oxygen or sulphur; andn is zero or 1; or an N-oxide thereof, prodrug thereof solvate thereof, or pharmaceutically acceptable salt thereof, which compounds have endothelin antagonist activity. The invention is also directed to methods for preparing the compounds of formula I and their pharmaceutical use.Type: GrantFiled: June 11, 1999Date of Patent: April 11, 2000Assignee: Rhone-Poulenc Rorer LimitedInventors: Christopher Smith, Barry Porter, Roger Walsh, Tahir Majid, Clive McCarthy, Neil Harris, Peter Astles, Iain McLay, Andrew Morley, Andrew Bridge, Andrew Van Sickle, Frank Halley, Alan Roach, Martyn Foster
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Patent number: 6013637Abstract: Compositions and methods for the treatment of acne including a peroxide and an antibiotic from the lincomycin family of antibiotics are disclosed.Type: GrantFiled: June 12, 1998Date of Patent: January 11, 2000Assignee: Dermik Laboratories Inc.Inventors: Robert W. Klein, Albert M. Packman
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Patent number: 5908639Abstract: A powder composition for inhalation comprising at least one microfine drug and a carrier, in which at least a portion of the said carrier comprises an antistatic agent.Type: GrantFiled: March 19, 1997Date of Patent: June 1, 1999Assignee: Rhone-Poulenc Rorer LimitedInventors: Gordon Thomas Simpkin, Roy Trunley, Ann-Marie Leighton
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Patent number: 5896855Abstract: An inhaler for inhalation of a medicament from a pierced capsule has a swirling or emptying chamber where the capsule is emptied by inhalation action of an operator. A rotary magazine for a multi-unit does inhaler which holds a number of capsules containing a medicament in a number of recesses arranged around the periphery of the magazine. The capsules are held in place by pins or plugs at both ends. Either the capsules are pierced before being loaded into the magazine or they are pierced by the pins when they are loaded into the magazine. In either case a seal may be provided around the ends of the capsules near the holes which are plugged to keep them fresh. When a recess is rotated to a particular position within the magazine then it releases its capsule. Contents of a capsule are drawn out during inhalation when the capsule is in the swirling chamber. A motor can be used to operate the magazine.Type: GrantFiled: June 7, 1995Date of Patent: April 27, 1999Assignee: Rhone-Poulenc Rorer LimitedInventors: Michael A. Hobbs, John R. Calvert, Robert S. Cook, Roy Trunley, Gordon T. Simpkin
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Patent number: 5797391Abstract: An inhaler for powdered medicament in capsules has a swirling chamber which can be opened to allow access of a closed capsule into the swirling chamber for operation of capsule-opening means in the swirling chamber. Access to the swirling chamber is gained by a pivoting cover member (22) which is provided with interlock means associated with the capsule-opening means to ensure that the capsule opening means cannot be operated while the cover member is in its open position to allow access of the user's finger to the region (28) of the swirling chamber (26,28) where the capsule-opening pins (30) could damage the user's finger. A further embodiment of an inhaler has a removable capsule reservoir having a container portion (74) with a closure (76) removable to reveal the interior of said reservoir and closable to define one entire side face of said reservoir, the closure member (76) being hinged to the container portion at thin film hinge (78).Type: GrantFiled: September 28, 1993Date of Patent: August 25, 1998Assignee: Rhone-Poulenc Rorer LimitedInventors: Robert Stanley Cook, Michael Anthony Hobbs, Ann-Marie Leighton, Gordon Thomas Simpkin, Roy Trunley
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Patent number: 5767098Abstract: Compositions for treating acne that contain a peroxide and an antibiotic selected from the lincomycin family are disclosed. In particular, compositions containing benzoyl peroxide and clindamycin are disclosed along with methods of treating acne using these compositions.Type: GrantFiled: March 31, 1997Date of Patent: June 16, 1998Assignee: Dermik Laboratories, Inc.Inventors: Robert W. Klein, Albert M. Packman
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Patent number: 5766635Abstract: Nanoparticles are prepared by dissolving a poly(ethylene oxide) and/or poly(propylene oxide) polylactic copolymer in an organic solvent followed by formation of nanoparticles by mixing the solution containing the polymer with an aqueous solution and by precipitation, without using an additional colloidal protective agent or by microfluidization and solvent evaporation. Nanoparticles prepared by this method are disclosed.Type: GrantFiled: June 5, 1995Date of Patent: June 16, 1998Assignee: Rhone-Poulenc Rorer S.A.Inventors: Gilles Spenleuhauer, Didier Bazile, Michel Veillard, Christian Prud'Homme, Jean-Paul Michalon
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Patent number: 5750734Abstract: A process is described for the preparation of a compound of formula (I) or a stereoisomeric compound thereof, in which the 1,2-position is saturated or is a double bond; X.sup.1 and X.sup.2 are each independently hydrogen or halogen; R.sup.1 is hydrogen or acyl; R.sup.2 is hydroxyl, acyloxy or oxo; and R.sup.3 is alkyl, by reacting a compound of formula (II) with an aldehyde R.sup.3 CHO in either phosphoric acid or about 60% to about 75% w/w sulphuric acid. Compounds of formula (I) are either pharmacologically active steroids or are intermediates in the synthesis of pharmacologically active steroids.Type: GrantFiled: May 23, 1997Date of Patent: May 12, 1998Assignee: Rhone-Poulenc Rorer LimitedInventors: Nigel Christopher Parkinson, Andrew Paul Van Sickle
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Patent number: 5727546Abstract: There is provided a device for the administration of an inhalation medicament, including a body defining a through-going air pathway having a longitudinal axis, an air inlet, an air outlet forming a mouthpiece, means for dispensing medicament into the pathway and air flow regulating means, characterised in that the air flow regulating means includes a movable obstructing means adapted to reduce the cross-sectional area of the pathway at a location between the air inlet and the means for dispensing medicament, and biassing means, whereby the obstructing means is biassed into a first resting position in which the cross-sectional area of the pathway is minimum and is adapted to move against the bias of the biassing means to a second position in which the cross-section area of the pathway is maximum in response to a pressure fall at the moiuthpiece caused by inhalation and is adapted to move further to a third position in which the cross-sectional area of the pathway is less than maximum in response to a greaterType: GrantFiled: July 17, 1996Date of Patent: March 17, 1998Assignee: Fisons plcInventors: Alastair Robert Clarke, Clive Sleath, Michael Trevor Shepherd