Patents by Inventor Andrew William Thomas
Andrew William Thomas has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 8293730Abstract: The present invention is concerned with a method of treating Alzheimer's disease by administering a therapeutically effective amount of a substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine of formula I wherein R1, R2, and R3 are as defined herein, and their pharmaceutically acceptable acid addition salts. The invention also provides novel compounds of formula I-A and pharmaceutical compositions containing them.Type: GrantFiled: November 16, 2009Date of Patent: October 23, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Henner Knust, Heinz Stadler, Andrew William Thomas
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Publication number: 20100075954Abstract: The present invention is concerned with a method of treating Alzheimer's disease by administering a therapeutically effective amount of a substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine of formula I wherein R1, R2, and R3 are as defined herein, and their pharmaceutically acceptable acid addition salts. The invention also provides novel compounds of formula I-A and pharmaceutical compositions containing them.Type: ApplicationFiled: November 16, 2009Publication date: March 25, 2010Inventors: Henner Knust, Heinz Stadler, Andrew William Thomas
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Patent number: 7671048Abstract: The present invention is concerned with a method of treating a disease selected from the group consisting of cognitive disorders, anxiety, Alzheimer's disease, and schizophrenia comprising administering a therapeutically effective amount of a substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of the following formula wherein R1 is halogen, lower alkyl, lower alkynyl, cycloalkyl, lower alkoxy, OCF3, —NHR, —NHC(O)R or —NHSO2R; R2 is hydrogen, methyl or aryl which is unsubstituted or substituted by one or two substituents selected from the group consisting of halogen and lower alkoxy; R3 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl, lower alkoxy, —O(CH2)n+1—O-lower alkyl, —(CH2)n-aryl which is optionally substituted by lower alkyl or halogen, heteroaryl, —NHR, —N(R)2, wherein each R can be the same or different, —NHCH2C?CH, or pyrrolidin-1-one; R is hydrogen, lower alkyl, lower alkyl substituted by halogen, heteroaryl, —(CH2)nO-lower alkyl, —NH-lower alkyl, cycloalkyl orType: GrantFiled: October 7, 2005Date of Patent: March 2, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Henner Knust, Heinz Stadler, Andrew William Thomas
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Patent number: 7576217Abstract: The present invention relates to compounds of formula I wherein R1 to R6 are as described herein, which compounds are active at the GABAB receptor and can be used for the preparation of medicaments useful in the treatment of CNS disorders comprising anxiety and depression.Type: GrantFiled: October 27, 2005Date of Patent: August 18, 2009Assignee: Hoffman-La Roche Inc.Inventors: Parichehr Malherbe, Raffaello Masciadri, Roger David Norcross, Hasane Ratni, Andrew William Thomas
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Patent number: 7538132Abstract: The present invention is concerned with aryl-isoxazole-4-carbonyl-pyrrole-2-carboxylic acid amide derivatives of formula wherein R1, R2, R3, R4, and R5, and m are as defined herein and with their pharmaceutically acceptable acid addition salts. This class of compounds have high affinity and selectivity for GABA A ?5 receptor binding sites and therefore may be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.Type: GrantFiled: September 13, 2006Date of Patent: May 26, 2009Assignee: Hoffman-La Roche Inc.Inventors: Bernd Buettelmann, Bo Han, Henner Knust, Matthias Heinrich Nettekoven, Andrew William Thomas
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Patent number: 7514426Abstract: The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of formula I wherein R1 is hydrogen, halogen, lower alkyl, lower alkynyl, cycloalkyl, heterocycloalkyl, benzyl, cyano, lower alkoxy, OCF3, —NHR, —NHC(O)R or —NHSO2R; R2 is lower alkyl substituted by halogen; R3 is hydrogen, methyl or aryl; R is lower alkyl, cycloalkyl or aryl; and pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: October 17, 2005Date of Patent: April 7, 2009Assignee: Hoffman-La Roche Inc.Inventors: Henner Knust, Andrew William Thomas
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Patent number: 7507728Abstract: The invention relates to halogen substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of formula I wherein R1, R2, R3, R4 and n are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The compounds can be used as a cognitive enhancer or for the treatment of cognitive disorders, anxiety, Alzheimer's disease and schizophrenia.Type: GrantFiled: October 17, 2005Date of Patent: March 24, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Henner Knust, Andrew William Thomas
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Patent number: 7432256Abstract: The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of the formula I wherein R1 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, nitro, cycloalkyl, —O(CH2)mO(CH2)mOH or —C?C—R?; R2 is hydrogen or methyl; R3 is lower alkyl, lower alkyl substituted by halogen, lower alkenyl, lower alkenyl substituted by halogen, lower alkynyl, —(CH2)n-cycloalkyl, —(CR?R?)m—CH3, phenyl that is unsubstituted or substituted by halogen, pyridinyl or thienyl each of which is unsubstituted or substituted by lower alkyl, —(CH2)n—NH-cycloalkyl, lower alkenyl-cycloalkyl, lower alkynyl-(CR?R?)mOH, or lower alkynyl-phenyl wherein the phenyl ring is unsubstituited or substituted by halogen, CF3, lower alkyl or lower alkoxy; R? is hydrogen or lower alkyl; R? is hydrogen, hydroxy or lower alkyl; n is 0, 1 or 2; m is 1, 2 or 3; and o is 1 or 2; and pharmaceutically acceptable acid addition salts thType: GrantFiled: December 8, 2005Date of Patent: October 7, 2008Assignee: Hoffman-La Roche Inc.Inventors: Bernd Buettelmann, Henner Knust, Andrew William Thomas
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Patent number: 7390903Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, R4, and R5 are as defined in the specification. Compounds of the invention are active on the GABAB receptor and are useful for treating a variety of CNS disorders, including anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity-and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, psychosis, panic disorder, posttraumatic stress disorders and gastro-intestinal disorders.Type: GrantFiled: December 13, 2005Date of Patent: June 24, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Parichehr Malherbe, Raffaello Masciadri, Roger David Norcross, Hasane Ratni, Andrew William Thomas
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Patent number: 7351700Abstract: The present invention relates to compounds of formula wherein X is —S— or —NH—; R3/R4 together with the N-atom to which they are attached form a non aromatic 5, 6 or 7 membered ring, which optionally contains in addition to the N-atom one additional heteroatom selected from the group consisting of O, S and N, and wherein the ring is optionally substituted by hydroxy, lower alkyl, lower alkoxy, —NR2, —CONR2, —CO-lower alkyl or benzyl; or R3/R4 form together with the N-atom to which they are attached a heterocyclic ring system, containing two or three rings and which optionally contains one or two additional heteroatoms selected from the group consisting of N and O and which has no more than 20 carbon atoms; and R, R1, R2, and R5 are as defined herein and to pharmaceutically suitable acid addition salts thereof.Type: GrantFiled: February 23, 2005Date of Patent: April 1, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Pari Malherbe, Raffaello Masciadri, Eric Prinssen, Will Spooren, Andrew William Thomas
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Patent number: 7265126Abstract: The present invention relates to compounds of formula wherein A-B, R1, R2, R3, R4, and n are as defined herein; and to pharmaceutically acceptable salts thereof. The compounds of formula I may be used in the treatment of neurological and neuropsychiatric disorders.Type: GrantFiled: January 3, 2005Date of Patent: September 4, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Synese Jolidon, Emmanuel Pinard, Andrew William Thomas
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Patent number: 7253318Abstract: The invention relates to compounds of the formula and their pharmaceutically acceptable salts wherein R1, R2, R3, R4, R5, n, m, and o are as defined in the specification. The compounds are selective monoamine oxidase ? inhibitors and are useful for the treatment and prevention of Alzheimer's disease and senile dementia, as well as other CNS disorders. The invention also relates to processes for preparing such compounds and pharmaceutical compositions containing them.Type: GrantFiled: June 20, 2005Date of Patent: August 7, 2007Assignee: Hoffman-La Roche Inc.Inventors: Synese Jolidon, Rosa Maria Rodriguez-Sarmiento, Andrew William Thomas, Wolfgang Wostl, Rene Wyler
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Patent number: 7235581Abstract: The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of illness, e.g. which are mediated by monoamine oxidase B inhibitors, in particular Alzheimer's disease or senile dementia.Type: GrantFiled: September 18, 2003Date of Patent: June 26, 2007Assignee: Hoffman-La Roche Inc.Inventors: Synese Jolidon, Rosa Maria Rodriguez-Sarmiento, Andrew William Thomas, Wolfgang Wostl, Rene Wyler
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Patent number: 7173133Abstract: The present invention relates to compounds of formula wherein A-B is —CH2—CH2—, —CH2—O— or —O—CH2—; X is hydrogen or hydroxy; R1 is aryl, optionally substituted by one or two substituents selected from the group consisting of halogen, lower alkyl, cyano, CF3, —OCF3, lower alkoxy, —SO2-lower alkyl and heteroaryl; R2 is aryl, optionally substituted by one or two substituents selected from the group consisting of halogen, lower alkyl, CF3, and lower alkoxy; R3 is hydrogen or lower alkyl; n is 0, 1 or 2; or a pharmaceutically active salt thereof. The compounds of the invention may be used in the treatment of neurological and neuropsychiatric disorders.Type: GrantFiled: January 3, 2005Date of Patent: February 6, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Simona Maria Ceccarelli, Synese Jolidon, Emmanuel Pinard, Andrew William Thomas
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Patent number: 7173023Abstract: The present invention relates to novel benzazepine derivatives of the following formula: wherein R1, R2, R3, R4 and R5, X, X?, Y and Y? are as defined in the description and claims, processes for their preparation, pharmaceutical compositions containing said derivatives and their use for the preparation of medicaments useful for the prevention and treatment of diseases in which selective inhibition of monoamine oxidase B activity plays a role or is implicated.Type: GrantFiled: October 18, 2004Date of Patent: February 6, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Synese Jolidon, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Wolfgang Wostl, Rene Wyler
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Patent number: 7151111Abstract: The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of a disease which is mediated by a monoamine oxidase B inhibitor, in particular Alzheimer's disease and senile dementia.Type: GrantFiled: September 18, 2003Date of Patent: December 19, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Hans Iding, Synese Jolidon, Daniela Krummenacher, Rosa Maria Rodriguez-Sarmiento, Andrew William Thomas, Beat Wirz, Wolfgang Wostl, Rene Wyler
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Patent number: 7122562Abstract: The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of illness, in particular which is mediated by monoamine oxidase B inhibitors, in particular Alzheimer's disease or senile dementia.Type: GrantFiled: January 5, 2006Date of Patent: October 17, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Hans Iding, Synese Jolidon, Daniela Krummenacher, Rosa Maria Rodriguez-Sarmiento, Andrew William Thomas, Beat Wirz, Wolfgang Wostl, Rene Wyler
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Patent number: 7087612Abstract: This invention relates to 3H-quinazolin-4-one derivatives as defined in the specification and claims, to a process for their preparation, to pharmaceutical compositions comprising them and to their use as selective monoamine oxidase B inhibitors.Type: GrantFiled: December 13, 2003Date of Patent: August 8, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
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Patent number: 7053245Abstract: 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 5, 2004Date of Patent: May 30, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Synese Jolidon, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
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Patent number: 7037935Abstract: The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of illness, in particular which is mediated by monoamine oxidase B inhibitors, in particular Alzheimer's disease or senile dementia.Type: GrantFiled: September 18, 2003Date of Patent: May 2, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Hans Iding, Synese Jolidon, Daniela Krummenacher, Rosa Maria Rodriguez-Sarmiento, Andrew William Thomas, Beat Wirz, Wolfgang Wostl, Rene Wyler