Patents Represented by Attorney, Agent or Law Firm Kimberly J. Prior
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Patent number: 6835732Abstract: The present invention relates to substituted benzothiazole derivitives and to their pharmaceutically acceptable salts useful for the treatment of diseases related to the adenosine receptor.Type: GrantFiled: December 5, 2002Date of Patent: December 28, 2004Assignee: Hoffman-La Roche Inc.Inventors: Alexander Alanine, Alexander Flohr, Aubry Kern Miller, Roger David Norcross, Claus Riemer
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Patent number: 6831087Abstract: The invention relates to compounds of formulae: Compounds of the invention have a good affinity to the NMDA receptor and are useful for the treatment of diseases related to this receptor.Type: GrantFiled: October 29, 2002Date of Patent: December 14, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Emmanuel Pinard, Rene Wyler
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Patent number: 6818774Abstract: Disclosed are isoquinolino derivatives of the formula wherein Y is >C═O or —CH2—, Z is >C═O or —CH2—, and R1, R2 and m are as defined herein as well as the pharmaceutically acceptable salts thereof. These compounds are MAO-B selective inhibitors useful, inter alia, in the treatment of Alzheimer's disease and/or senile dementia.Type: GrantFiled: April 16, 2003Date of Patent: November 16, 2004Assignee: Hoffman-La Roche Inc.Inventors: Andrea Cesura, Rosa Maria Rodriguez Sarmiento, Michelangelo Scalone, Andrew William Thomas, Rene Wyler
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Patent number: 6806370Abstract: Compounds of the invention are amine oxide prodrugs showing activity on the NK1 receptor.Type: GrantFiled: August 21, 2003Date of Patent: October 19, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Torsten D. Hoffmann, Sonia Maria Poli, Patrick Schnider, Andrew Sleight
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Patent number: 6803381Abstract: The present invention relates to compounds of formula wherein R1 is hydrogen or lower alkyl; R2, R2′ are each independently hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; X is O, S or two hydrogen atoms not forming a bridge; A1/A2 is phenyl; B is a group of formula wherein R3 is lower alkyl, lower alkenyl, lower alkinyl, benzyl, lower alkyl-cycloalkyl, lower alkyl-cyano, lower alkyl-pyridinyl, lower alkyl-lower alkoxy-phenyl, lower alkyl-phenyl, which is optionally substituted by lower alkoxy, or phenyl, which is optionally substituted by lower alkoxy, or lower alkyl-thienyl, cycloalkyl, lower alkyl-trifluoromethyl or lower alkyl-morpholinyl; Y is —O—, —S— or a bond; and Z is —O—; or a pharmaceutically acceptable salt thereof. These compounds are useful for the control or prevention of acute and/or chronic neurological disorders.Type: GrantFiled: May 14, 2003Date of Patent: October 12, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Konrad Bleicher, Vincent Mutel, Eric Vieira, Jürgen Wichmann, Thomas Johannes Woltering
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Patent number: 6787539Abstract: The invention relates to compounds of the formula wherein R1 is lower alkyl, lower alkoxy, pyridinyl, pyrimidinyl, phenyl, —S-lower alkyl, —S(O)2-lower alkyl, —N(R)—(CH2)n—N(R)2, —O—(CH2)n—N(R)2, —N(R)2, or a cyclic tertiary amine of the group which may contain one additional heteroatom, selected from N, O or S, and wherein this group may be connected with the pyrimidine ring via the linker —O(CH2)n—; R2 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R3/R3′ is, independently from each other, hydrogen or lower alkyl; R4 is independently from each other halogen, trifluoromethyl or lower alkoxy; R5 is hydrogen or lower alkyl; R is, independently from each other, hydrogen or lower alkyl; X is —C(O)N(R)— or —N(R)C(O)—; Y is —O—, —S—, —SO2—, - or —N(R)—; n is 1,2,3 or 4; and m is 0,1 or 2; or a pharmaceuticType: GrantFiled: October 15, 2001Date of Patent: September 7, 2004Assignee: Hoffmann-La Roche Inc.Inventor: Heinz Stadler
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Patent number: 6770637Abstract: Substituted 4-phenyl-pyridine compounds with activity as antagonists of Neurokinin 1 receptors, methods of making these compounds and preparing.Type: GrantFiled: August 3, 2001Date of Patent: August 3, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Thierry Godel, Torsten Hoffmann, Patrick Schnider, Heinz Stadler
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Patent number: 6762320Abstract: This invention relates to N-acylamino aryl derivatives of the formula where R1, R21, R22, R23, R24, R3, R4, R5 R6, R7, R8, R, and n are as defined herein and where X is —CHRO, —OCHR—, —CH2S—, —SCH2—, —CH2CH2—, —CH═CH— or —C≡C—. The compounds of the invention are selective monoamine oxidase B inhibitors, and they are therefore useful in the treatment of diseases mediated by monoamine oxidase B, for example, for the treatment of Alzheimer's disease or senile dementia.Type: GrantFiled: May 27, 2003Date of Patent: July 13, 2004Assignee: Hoffman-La Roche Inc.Inventors: Synese Jolidon, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
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Patent number: 6747026Abstract: Compounds of the invention are amine oxide prodrugs showing activity on the NK1 receptor.Type: GrantFiled: January 7, 2003Date of Patent: June 8, 2004Assignee: Hoffman-La Roche Inc.Inventors: Torsten Hoffmann, Sonia Maria Poli, Patrick Schnider, Andrew Sleight
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Patent number: 6743789Abstract: The present invention is a compound of formula The compound and derivatives or pharmaceutically acceptable salts thereof of the invention have a good affinity and selectivity to the GABA A &agr;5 receptor and are useful for the treatment of diseases related to this receptor.Type: GrantFiled: November 8, 2001Date of Patent: June 1, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Raffaello Masciadri, Andrew William Thomas, Juergen Wichmann
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Patent number: 6740760Abstract: New compounds have the formula: wherein R, R1, X and Y have the meanings described herein. Methods are set forth for synthesizing these compounds and using these compounds to treat diseases associated with amyloidosis, such as Alzheimer's disease, maturity onset diabetes mellitus, familial amyloid polyneuropathy, scrapie, and Kreuzfeld-Jacob disease.Type: GrantFiled: July 1, 2002Date of Patent: May 25, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Cornelia Hertel, Torsten Hoffmann, Roland Jakob-Roetne, Roger David Norcross
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Patent number: 6730670Abstract: A compound of the formula Compounds of formula I have a good affinity to the A2A receptor and are useful for the treatment of diseases mediated by this receptor.Type: GrantFiled: December 10, 2002Date of Patent: May 4, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Alexander Flohr
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Patent number: 6727247Abstract: A compound of formula I and a method of treatment of diseases, related to modulation of the adenosine A2 receptor system comprising administering a compound of formula to a person in need of such treatment.Type: GrantFiled: December 3, 2002Date of Patent: April 27, 2004Assignee: Hoffman-La Roche Inc.Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
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Patent number: 6719996Abstract: A pharmaceutical composition for oral administration of an active compound having a bioavailability of 20% or less. The composition comprises, based on its total weight, from 0.01% to about 15% (w/w) of said active compound molecularly dissolved in the composition, from 30 to 80% (w/w) of an edible lipid matrix and from 1 to 20% (w/w) of an edible emulsifier, the ratio between the dose weight of the active compound and its solubility in the composition being equal to or greater than 0.6 ml. The high percentage of fat (30-80%) enables a considerable increase the amount of the drug that is molecularly dispersed in the dosage form, thus allowing a significant reduction in the number of unit doses that must be taken daily-by patients.Type: GrantFiled: December 10, 2001Date of Patent: April 13, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Martin Kuentz, Dieter Roethlisberger
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Patent number: 6706707Abstract: This invention relates to a compound and the use of the compound of the formula wherein R1, R2, R3, R4 and R5 are as defined in the description, A signifies —CH═CH— or —C≡C—; and B signifies wherein R6 to R26, X and Y are as defined in the specification or a pharmaceutically acceptable salt thereof, for use in pharmaceutical compositions for the treatment or prevention of mGluR5 receptor mediated disorders.Type: GrantFiled: November 28, 2001Date of Patent: March 16, 2004Assignee: Hoffman-La Roche Inc.Inventors: Vincent Mutel, Jens-Uwe Peters, Juergen Wichmann
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Patent number: 6689790Abstract: A compound of formula wherein R1 is —NR′R″, wherein R′ and R″ are independently selected from the group consisting of lower alkyl, —(CH2)n—C(O)NRaRb, —(CH2)n,-heteroaryl, —(CH2)n-aryl, —(CH2)n—CN, —(CH2)n—O-lower alkyl or —(CH2)n-cycloalkyl, or R′ and R″ form together with the N-atom a five or six-membered non-aromatic ring, containing no or one additional heteroatom selected from the group consiting of O and S, and said ring being unsubstituted or substituted by one or two substituents, selected from the group consisting of lower alkyl, —C(O)NRaRb and —(CH2)n—O-lower alkyl, and RaRb are independently from each other hydrogen or lower alkyl; R2 is aryl or heteroaryl, unsubstituted or substituted by lower alkyl or halogen; and n is 0, 1, 2 or 3; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 7, 2002Date of Patent: February 10, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Heinrich Nettekoven, Sebastien Schmitt
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Patent number: 6689755Abstract: The present invention relates to a rapid and readily reproducible process for stabilizing biologically active substances by combining the biologically active substance witha a stabilizingmixture and drying the resulting mixture into a dry, amorphous product by means of convection drying. The invention also relates to the amorphous, microscopically homogeneous products which are obtained by this process, are in the form of powders and have a uniform geometric, in particular spherical, shape. The invention furthermore relates to the use of substance mixtures for stabilizing biologically active material, in particular proteins by means of spray drying.Type: GrantFiled: November 3, 1998Date of Patent: February 10, 2004Assignee: Boehringer Mannheim GmbHInventors: Rolf-Dieter Gabel, Markus Mattern, Gerhard Winter, Alexander Wirl, Heinrich Woog
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Patent number: 6686352Abstract: The present invention is a compound of formula wherein R1 is halogen or lower alkyl; R2 is hydrogen, lower alkyl, cycloalkyl, —(CH2)m-phenyl, wherein the phenyl ring may be substituted by lower alkoxy, or is —(CH2)m-indolyl; R3 is —C(O)O-lower alkyl, —C(O)OH, or a five membered heteroaromatic group, which rings may be substituted by lower alkyl or cycloalkyl; n is 0, 1 or 2; m is 0, 1 or 2; or a pharmaceutically acceptable acid addition salt thereof. Compound I shows high affinity and selectivity for GALA A &agr;5 receptor binding sites.Type: GrantFiled: April 9, 2002Date of Patent: February 3, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Raffaello Masciadri, Andrew William Thomas, Juergen Wichmann
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Patent number: 6683097Abstract: Novel imidazole derivatives are disclosed. These compounds have a good affinity to the NMDA (N-methyl-D-aspartate)-receptor subtype selective blockers, which have a key function in modulating neuronal activity and plasticity which makes them key players in mediating processes underlying development of CNS as well as learning and memory formation. These compounds are useful in the control or treatment of diseases mediated by this receptor.Type: GrantFiled: February 11, 2003Date of Patent: January 27, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Georg Jaeschke, Emmanuel Pinard, Rene Wyler
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Patent number: 6673795Abstract: The present invention is a pyrimidine, triazine or pyrazine derivative of the formula or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, R4, X, Y and Z are as defined in the specification. The invention is a pharmaceutical composition containing an effective amount of the compound of formula 1, its preparation and to a method of treatment, control or prevention of acute and/or chronic neurological disorders by administering a therapeutically effective amount of a compound of formula 1.Type: GrantFiled: May 29, 2002Date of Patent: January 6, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Alfred Binggeli, Hans-Peter Maerki, Thierry Masquelin, Vincent Mutel, Maurice Wilhelm, Wolfgang Wostl