Patents by Inventor Thorsten Muser
Thorsten Muser 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: 20230391778Abstract: The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula wherein Ar1 is phenyl or a five or six membered heteroaryl group, containing one, two or three heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+—(O?); R1 is lower alkyl, halogen, cyano or cycloalkyl; Ar2 is a five or six membered heteroaryl group, containing one, two, three or four heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+—(O?), or is benzo[b]thiophenyl; R2 is hydrogen, lower alkyl, halogen, cyano, lower alkyl substituted by hydroxyl, lower alkyl substituted by halogen, lower alkyl substituted by amino, lower alkyl substituted by alkoxy, lower alkyl substituted by amide, or is cycloalkyl; X is CH or N; n is 1 or 2; m is 1 or 2; as well as with a pharmaceutically acceptable salt thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereofType: ApplicationFiled: August 17, 2023Publication date: December 7, 2023Applicant: Hoffmann-La Roche Inc.Inventors: Hans HILPERT, Sabine KOLCZEWSKI, Roland HUMM, Theodor STOLL, Thorsten MUSER, Jean-Marc PLANCHER, Delphine GAUFRETEAU
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Publication number: 20230087946Abstract: The invention comprises radiolabeled MOEM type oligonucleotide of the formula (I), (I) wherein n, X1, X2, the linker (1), the linker (2), Q* and the receptor targeting moiety are as defined (I) the description. The radiolabeled oligonucleotides of the formula (I) can be used for the determination of the biodistribution and pharmacokinetics of the oligonucleotide in the tissue or body fluid.Type: ApplicationFiled: June 19, 2020Publication date: March 23, 2023Applicant: Hoffmann-La Roche Inc.Inventors: Martin Robert EDELMANN, Thorsten MUSER
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Patent number: 11447478Abstract: The present invention provides a compound of formula I having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.Type: GrantFiled: April 8, 2014Date of Patent: September 20, 2022Assignee: HOFFMANN-LA ROCHE INC.Inventors: Hans Hilpert, Roland Humm, Thorsten Muser, Christian Schnider, Roger Wermuth, Thomas Woltering
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Publication number: 20220033395Abstract: The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula wherein Ar1 is phenyl or a five or six membered heteroaryl group, containing one, two or three heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+—(O?); R1 is lower alkyl, halogen, cyano or cycloalkyl; Ar2 is a five or six membered heteroaryl group, containing one, two, three or four heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+—(O?), or is benzo[b]thiophenyl; R2 is hydrogen, lower alkyl, halogen, cyano, lower alkyl substituted by hydroxyl, lower alkyl substituted by halogen, lower alkyl substituted by amino, lower alkyl substituted by alkoxy, lower alkyl substituted by amide, or is cycloalkyl; X is CH or N; n is 1 or 2; m is 1 or 2; as well as with a pharmaceutically acceptable salt thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereofType: ApplicationFiled: April 22, 2021Publication date: February 3, 2022Applicant: Hoffmann-La Roche Inc.Inventors: Hans Hilpert, Sabine Kolczewski, Roland Humm, Theodor Stoll, Thorsten Muser, Jean-Marc Plancher, Delphine Gaufreteau
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Publication number: 20210246133Abstract: The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula wherein Ar1 is phenyl or a five or six membered heteroaryl group, containing one, two or three heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+—(O?); R1 is lower alkyl, halogen, cyano or cycloalkyl; Ar2 is a five or six membered heteroaryl group, containing one, two, three or four heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+—(O?), or is benzo[b]thiophenyl; R2 is hydrogen, lower alkyl, halogen, cyano, lower alkyl substituted by hydroxyl, lower alkyl substituted by halogen, lower alkyl substituted by amino, lower alkyl substituted by alkoxy, lower alkyl substituted by amide, or is cycloalkyl; X is CH or N; n is 1 or 2; m is 1 or 2; as well as with a pharmaceutically acceptable salt thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereofType: ApplicationFiled: October 13, 2020Publication date: August 12, 2021Applicant: Hoffmann-La Roche Inc.Inventors: Hans Hilpert, Sabine Kolczewski, Roland Humm, Theodor Stoll, Thorsten Muser, Jean-Marc Plancher, Delphine Gaufreteau
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Publication number: 20200010466Abstract: The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula wherein Ar1 is phenyl or a five or six membered heteroaryl group, containing one, two or three heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+—(O?); R1 is lower alkyl, halogen, cyano or cycloalkyl; Ar2 is a five or six membered heteroaryl group, containing one, two, three or four heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+—(O?), or is benzo[b]thiophenyl; R2 is hydrogen, lower alkyl, halogen, cyano, lower alkyl substituted by hydroxyl, lower alkyl substituted by halogen, lower alkyl substituted by amino, lower alkyl substituted by alkoxy, lower alkyl substituted by amide, or is cycloalkyl; X is CH or N; n is 1 or 2; m is 1 or 2; as well as with a pharmaceutically acceptable salt thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereofType: ApplicationFiled: July 19, 2019Publication date: January 9, 2020Applicant: Hoffmann-La Roche Inc.Inventors: Hans Hilpert, Sabine Kolczewski, Roland Humm, Theodor Stoll, Thorsten Muser, Jean-Marc Plancher, Delphine Gaufreteau
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Patent number: 10457667Abstract: The present invention is concerned with indolin-2-one derivatives of general formula wherein A is phenyl or a six membered heteroaryl group, containing one or two N atoms, selected from or the oxygen atom may form together with two neighboring carbon atoms from the group A an additional fused ring, selected from R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen or oxetanyl; R2 is hydrogen, lower alkyl lower alkoxy, halogen or cycloalkyl; --- the dotted line is nothing or may be —CH2—; as well as with a pharmaceutically acceptable salt thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.Type: GrantFiled: May 4, 2018Date of Patent: October 29, 2019Assignee: Hoffmann-La Roche Inc.Inventors: Delphine Gaufreteau, Hans Hilpert, Roland Humm, Sabine Kolczewski, Thorsten Muser, Jean-Marc Plancher, Theodor Stoll
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Patent number: 10377746Abstract: The present invention is concerned with indolin-2-one derivatives of general formula wherein A is phenyl or a six membered heteroaryl group, containing one or two N atoms, selected from R1 is S(O)2lower alkyl, S(O)2NR4R5, S(O)2cycloalkyl, S-lower alkyl or S(O)2-azetidin-1-yl; R4 and R5 are independently from each other hydrogen, lower alkyl or (CH2)2OCH3; or the group A-R1 may form together with two neighboring carbon atoms from the group A an additional fused ring, selected from R2 is hydrogen or cycloalkyl; R3 is methyl or halogen; n is 1 or 2; X is N, N+O? or CH; --- the dotted line may be nothing or —CH2—; as well as with a pharmaceutically acceptable salt thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.Type: GrantFiled: May 4, 2018Date of Patent: August 13, 2019Assignee: Hoffmann-La Roche Inc.Inventors: Delphine Gaufreteau, Hans Hilpert, Roland Humm, Sabine Kolczewski, Thorsten Muser, Jean-Marc Plancher, Theodor Stoll
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Publication number: 20180251451Abstract: The present invention is concerned with indolin-2-one derivatives of general formula wherein A is phenyl or a six membered heteroaryl group, containing one or two N atoms, selected from or the oxygen atom may form together with two neighboring carbon atoms from the group A an additional fused ring, selected from R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen or oxetanyl; R2 is hydrogen, lower alkyl lower alkoxy, halogen or cycloalkyl; --- the dotted line is nothing or may be —CH2—; as well as with a pharmaceutically acceptable salt thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.Type: ApplicationFiled: May 4, 2018Publication date: September 6, 2018Applicant: Hoffmann-La Roche Inc.Inventors: Delphine Gaufreteau, Hans Hilpert, Roland Humm, Sabine Kolczewski, Thorsten Muser, Jean-Marc Plancher, Theodor Stoll
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Publication number: 20180251455Abstract: The present invention is concerned with indolin-2-one derivatives of general formula wherein A is phenyl or a six membered heteroaryl group, containing one or two N atoms, selected from R1 is S(O)2lower alkyl, S(O)2NR4R5, S(O)2cycloalkyl, S-lower alkyl or S(O)2-azetidin-1-yl; R4 and R5 are independently from each other hydrogen, lower alkyl or (CH2)2OCH3; or the group A-R1 may form together with two neighboring carbon atoms from the group A an additional fused ring, selected from R2 is hydrogen or cycloalkyl; R3 is methyl or halogen; n is 1 or 2; X is N, N+O? or CH; --- the dotted line may be nothing or —CH2—; as well as with a pharmaceutically acceptable salt thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.Type: ApplicationFiled: May 4, 2018Publication date: September 6, 2018Applicant: Hoffmann-La Roche Inc.Inventors: Delphine Gaufreteau, Hans Hilpert, Roland Humm, Sabine Kolczewski, Thorsten Muser, Jean-Marc Plancher, Theodor Stoll
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Pyrimidone derivatives and their use in the treatment, amelioration or prevention of a viral disease
Patent number: 9988390Abstract: The present invention relates to compounds having the general formula (Ia) or (Ib), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease, in particular influenza.Type: GrantFiled: October 28, 2016Date of Patent: June 5, 2018Inventors: Hans Hilpert, Lukas Kreis, Christian Lerner, Roland Humm, Thorsten Muser, Bernd Kuhn -
Pyrimidone derivatives and their use in the treatment, amelioration or prevention of a viral disease
Publication number: 20170267680Abstract: The present invention relates to compounds having the general formula (Ia) or (Ib), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease, in particular influenza.Type: ApplicationFiled: October 28, 2016Publication date: September 21, 2017Inventors: Hans HILPERT, Lukas KREIS, Christian LERNER, Roland HUMM, Thorsten MUSER, Bernd KUHN -
Publication number: 20170101409Abstract: The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula wherein Ar1 is phenyl or a five or six membered heteroaryl group, containing one, two or three heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+—(O?); R1 is lower alkyl, halogen, cyano or cycloalkyl; Ar2 is a five or six membered heteroaryl group, containing one, two, three or four heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+—(O?), or is benzo[b]thiophenyl; R2 is hydrogen, lower alkyl, halogen, cyano, lower alkyl substituted by hydroxyl, lower alkyl substituted by halogen, lower alkyl substituted by amino, lower alkyl substituted by alkoxy, lower alkyl substituted by amide, or is cycloalkyl; X is CH or N; n is 1 or 2; m is 1 or 2; as well as with a pharmaceutically acceptable salt thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereofType: ApplicationFiled: December 22, 2016Publication date: April 13, 2017Applicant: Hoffmann-La Roche Inc.Inventors: Hans Hilpert, Sabine Kolczewski, Roland Humm, Theodor Stoll, Thorsten Muser, Jean-Marc Plancher, Delphine Gaufreteau
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Publication number: 20160052920Abstract: The present invention provides a compound of formula I having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.Type: ApplicationFiled: April 8, 2014Publication date: February 25, 2016Applicants: HOFFMANN-LA ROCHE INC., SIENA BIOTECH S.p.A.Inventors: Hans Hilpert, Roland Humm, Thorsten Muser, Christian Schnider, Roger Wermuth, Thomas Woltering