Patents by Inventor Juergen Wichmann
Juergen Wichmann 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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Publication number: 20160185721Abstract: The present invention relates to compounds of general formula wherein R1 is aryl or heteroaryl, which are optionally substituted by one, two or three substituents, selected from lower alkyl, halogen, lower alkyl substituted by halogen, hydroxyl, lower alkoxy, lower alkoxy substituted by halogen, cyano or nitro; R2 is halogen, lower alkyl or cyano; R3 is hydrogen or lower alkyl; R4 is hydrogen or lower alkyl; R5, R6 are hydrogen, lower alkyl, or may form together with the N-atom to which they are attached a heterocycloalkyl ring; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof.Type: ApplicationFiled: March 10, 2016Publication date: June 30, 2016Applicant: Hoffmann-La Roche Inc.Inventors: Ravi Jagasia, Roland Jakob-Roetne, Jens-Uwe Peters, Juergen Wichmann
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Patent number: 9365550Abstract: The present invention relates to compounds of general formula wherein R1 hydrogen, lower alkyl, halogen or lower alkyl substituted by halogen; R2 is hydrogen or halogen; X1 is N or CH; X2 is N or CH; with the proviso that only one of X1 or X2 is N; X3 is C(R) or N; and R is hydrogen, lower alkyl, halogen, lower alkyl substituted by halogen, lower alkoxy or SO2-lower alkyl; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof.Type: GrantFiled: March 31, 2015Date of Patent: June 14, 2016Assignee: Hoffmann-La Roche Inc.Inventors: Simona M. Ceccarelli, Ravi Jagasia, Roland Jakob-Roetne, Juergen Wichmann
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Publication number: 20160137643Abstract: The present invention relates to compounds of general formula I wherein R1, R2, R3 and R4 are as defined herein which maybe used for the treatment of schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, cognitive impairment, chemotherapy-induced cognitive dysfunction (“chemobrain”), Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, and disturbances due to radiation therapy, chronic stress, optic neuropathy or macular degeneration, or abuse of neuro-active drugs, selected from alcohol, opiates, methamphetamine, phencyclidine and cocaine.Type: ApplicationFiled: January 27, 2016Publication date: May 19, 2016Applicant: Hoffmann-La Roche Inc.Inventors: Simona M. Ceccarelli, Ravi Jagasia, Roland Jakob-Roetne, Jens-Uwe Peters, Juergen Wichmann
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Patent number: 9315502Abstract: The present invention relates to compounds of general formula wherein Ar is phenyl or pyridinyl; X1 is N or CH, X2 is N or CH, with the proviso that only one of X1 or X2 is N and the other is CH; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, cyano or S(O)2-lower alkyl; R2 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen or cyano; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof.Type: GrantFiled: May 27, 2015Date of Patent: April 19, 2016Assignee: Hoffmann-La Roche Inc.Inventors: Simona M. Ceccarelli, Ravi Jagasia, Roland Jakob-Roetne, Juergen Wichmann
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Patent number: 9284321Abstract: The present invention relates to compounds of general formula I or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X, R and n are as defined herein. The compounds may be used for the treatment of schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction, Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of neuro-active drugs, such as alcohol, opiates, methamphetamine, phencyclidine and cocaine.Type: GrantFiled: February 4, 2015Date of Patent: March 15, 2016Assignee: Hoffmann-La Roche Inc.Inventors: Simona M. Ceccarelli, Ravi Jagasia, Roland Jakob-Roetne, Juergen Wichmann
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Publication number: 20160046583Abstract: The present invention relates to the use of compounds of general formula wherein R1 is phenyl or pyridinyl, which are optionally substituted by halogen, cyano or lower alkyl substituted by halogen, or is dihydro-pyran-4-yl; R2 is hydrogen or lower alkyl; R3 is —(CHR)n-phenyl, optionally substituted by lower alkoxy or S(O)2-lower alkyl, or is heterocycloalkyl, optionally substituted by ?O and lower alkyl, or is —(CH2)n-five or six membered heteroaryl, optionally substituted by lower alkyl, or is hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, —NR—S(O)2-lower alkyl, —(CH2)n-cycloalkyl or —(CH2)n—S(O)2-lower alkyl; or R2 and R3 form together with the N-atom to which they are attached a heterocycloalkyl ring, selected from the group consisting of 1,1-dioxo-thiomorpholinyl, morpholinyl, or pyrrolidinyl, optionally substituted by hydroxyl; R is hydrogen or lower alkyl; n is 0, 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixtureType: ApplicationFiled: October 29, 2015Publication date: February 18, 2016Applicant: Hoffmann-La Roche Inc.Inventors: Simona M. Ceccarelli, Ravi Jagasia, Roland Jakob-Roetne, Rainer E. Martin, Juergen Wichmann
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Publication number: 20160016963Abstract: The present invention relates to compounds of general formula I wherein R1 is halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen or cyano; R2 is hydrogen, CF3 or lower alkyl; R3 is hydrogen, lower alkyl, lower alkenyl, lower alkinyl, heterocycloalkyl, lower alkyl substituted by cyano, cyano, benzyl substituted by halogen, 2-oxa-6-aza-spiro[3.3]hept-6-yl or is lower alkoxy substituted by halogen; X is —CH2— or —CH2—CH2—; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof.Type: ApplicationFiled: September 28, 2015Publication date: January 21, 2016Applicant: HOFFMANN-LA ROCHE INC.Inventors: Ravi Jagasia, Roland Jakob-Roetne, Juergen Wichmann
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Publication number: 20150259341Abstract: The present invention relates to compounds of general formula wherein Ar is phenyl or pyridinyl; X1 is N or CH, X2 is N or CH, with the proviso that only one of X1 or X2 is N and the other is CH; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, cyano or S(0)2-lower alkyl; R2 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen or cyano; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof.Type: ApplicationFiled: May 27, 2015Publication date: September 17, 2015Applicant: Hoffmann-La Roche Inc.Inventors: Simona M. Ceccarelli, Ravi Jagasia, Roland Jakob-Roetne, Juergen Wichmann
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Publication number: 20150259334Abstract: The present invention relates to compounds of general formula wherein Ar1/Ar2 are phenyl or a 5 or 6-membered heteroaryl; R1/R2 is hydrogen, halogen, lower alkyl, CF3 or lower alkoxy; n,m are 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof, with the exception of the compound 2,1-benzisoxazole, 3-(4-chlorophenyl)-5-(1-phenyl-1H-pyrazol-5 -yl)-.Type: ApplicationFiled: January 22, 2015Publication date: September 17, 2015Applicant: Hoffmann-La Roche Inc.Inventors: Simona M. Ceccarelli, Ravi Jagasia, Roland Jakob-Roetne, Juergen Wichmann
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Publication number: 20150252049Abstract: This invention relates to a new medical use for certain chemical compounds and pharmaceutical compositions containing them. The invention relates to compounds which are mGlu2/3 negative allosteric modulators for use in the treatment of Autistic Spectrum Disorder (ASD), in particular, autism. In another aspect, the invention relates to a pharmaceutical composition for use in the treatment of ASD comprising a compound according to the invention and a pharmaceutically acceptable carrier.Type: ApplicationFiled: April 23, 2015Publication date: September 10, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Silvia Gatti McArthur, Michael Saxe, Juergen Wichmann, Thomas Woltering
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Publication number: 20150252044Abstract: The present invention relates to the use of compounds of general formula wherein R? is hydrogen or lower alkyl; R1 is halogen, lower alkyl, cycloalkyl or cyano; or is phenyl, optionally substituted by one to three substituents, selected from lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, halogen, cyano, hydroxy, C(O)—NH-lower alkyl, CH2—C(O)—NH-lower alkyl, CH2—NH—C(O)-lower alkyl, CH2NH2, S(O)2CH3, S(O)2N(CH3)2, or by heterocycloalkyl groups; or is pyrazol-1, 4 or 5-yl, optionally substituted by lower alkyl; or is thiazol-5-yl, optionally substituted by one or two lower alkyl groups; or is pyridine 2, 3 or 4-yl, optionally substituted by lower alkyl, lower alkoxy, halogen or N(CH3)2; or is 3,6-dihydro-2H-pyran; or is benzo[d][1,3]dioxol-5-yl; or is 2,3-dihydrobenzo[b][1,4]dioxin-6-yl; R2 is hydrogen, lower alkyl or lower alkyl substituted by alkoxy; R3 is hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy,Type: ApplicationFiled: May 20, 2015Publication date: September 10, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Simona M. Ceccarelli, Ravi Jagasia, Roland Jakob-Roetne, Rainer E. Martin, Jens-Uwe Peters, Juergen Wichmann
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Publication number: 20150246922Abstract: The present invention relates to compounds of general formula I or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X, R and n are as defined herein. The compounds may be used for the treatment of schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction, Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of neuro-active drugs, such as alcohol, opiates, methamphetamine, phencyclidine and cocaine.Type: ApplicationFiled: February 4, 2015Publication date: September 3, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Simona M. Ceccarelli, Ravi Jagasia, Roland Jakob-Roetne, Juergen Wichmann
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Publication number: 20150203472Abstract: The present invention relates to compounds of general formula wherein R1 hydrogen, lower alkyl, halogen or lower alkyl substituted by halogen; R2 is hydrogen or halogen; X1 is N or CH; X2 is N or CH; with the proviso that only one of X1 or X2 is N; X3 is C(R) or N; and R is hydrogen, lower alkyl, halogen, lower alkyl substituted by halogen, lower alkoxy or SO2-lower alkyl; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof.Type: ApplicationFiled: March 31, 2015Publication date: July 23, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Simona M. Ceccarelli, Ravi Jagasia, Roland Jakob-Roetne, Juergen Wichmann
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Patent number: 8921397Abstract: The present invention is concerned with novel selective dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein R1, R2, R3, n, and Y are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.Type: GrantFiled: April 27, 2012Date of Patent: December 30, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Patent number: 8877778Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, x, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.Type: GrantFiled: December 7, 2011Date of Patent: November 4, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Patent number: 8722683Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions containing them and their use as pharmaceutical agents.Type: GrantFiled: February 10, 2012Date of Patent: May 13, 2014Assignee: Hoffmann LA-Roche Inc.Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Patent number: 8598357Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: February 27, 2012Date of Patent: December 3, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Patent number: 8586579Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein X, Y, A, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as therapeutics.Type: GrantFiled: June 16, 2011Date of Patent: November 19, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Luca Gobbi, Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Patent number: 8470828Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein X, Y, A, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as therapeutics.Type: GrantFiled: June 29, 2011Date of Patent: June 25, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Luca Gobbi, Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Patent number: 8415380Abstract: The present invention relates to compounds of formula (I) wherein A, B, Q, X, Y, R1, and R2 are as defined herein; pharmaceutical compositions containing them; a process for their manufacture; and methods for treating CNS disorders with the same.Type: GrantFiled: July 8, 2011Date of Patent: April 9, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Silvia Gatti McArthur, Juergen Wichmann, Thomas Woltering