Patents by Inventor Hans Hilpert
Hans Hilpert 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: 20220411468Abstract: The present invention provides compounds of formula (I) wherein X1 to X8 and R1 to R8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.Type: ApplicationFiled: July 15, 2021Publication date: December 29, 2022Applicant: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Julien Beignet, Konrad Bleicher, Bernhard Fasching, Hans Hilpert, Taishan Hu, Dwight MacDonald, Stephen Jackson, Sabine Kolczewski, Carsten Kroll, Adrian Schaeublin, Hong Shen, Theodor Stoll, Helmut Thomas, Amal Wahhab, Claudia Zampaloni
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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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Patent number: 11098080Abstract: The present invention provides compounds of formula (I) wherein X1 to X8 and R1 to R8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.Type: GrantFiled: June 12, 2018Date of Patent: August 24, 2021Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Julien Beignet, Konrad Bleicher, Bernhard Fasching, Hans Hilpert, Taishan Hu, Dwight MacDonald, Stephen Jackson, Sabine Kolczewski, Carsten Kroll, Adrian Schaeublin, Hong Shen, Theodor Stoll, Helmut Thomas, Amal Wahhab, Claudia Zampaloni
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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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Patent number: 11066443Abstract: The present invention relates to compounds of formula (I) wherein X1 to X8 and R1 to R8 are as described herein, as well as pharmaceutically acceptable salts thereof for the use in the treatment or prevention of infections and resulting diseases caused by Pseudomonas aeruginosa.Type: GrantFiled: April 9, 2018Date of Patent: July 20, 2021Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Kurt Amrein, Konrad Bleicher, Bernhard Fasching, Hans Hilpert, Sabine Kolczewski, Carsten Kroll, Adrian Schaeublin, Claudia Zampaloni
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Publication number: 20200040031Abstract: The present invention relates to compounds of formula (I) wherein X1 to X8 and R1 to R8 are as described herein, as well as pharmaceutically acceptable salts thereof for the use in the treatment or prevention of infections and resulting diseases caused by Pseudomonas aeruginosa.Type: ApplicationFiled: April 9, 2018Publication date: February 6, 2020Inventors: Alexander Alanine, Kurt Amrein, Konrad Bleicher, Bernhard Fasching, Hans Hilpert, Sabine Kolczewski, Carsten Kroll, Adrian Schaeublin, Claudia Zampaloni
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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: 10385050Abstract: The present invention is concerned with indolin-2-one and 1,3-dihydro-pyrrolo[3,2-c]pyridin-2-one derivatives of general formula I wherein Ar1, A2, R1, R2, R3, X and n are as described herein and pharmaceutically acceptable salts thereof for treatment of central nervous system disordersType: GrantFiled: August 9, 2018Date of Patent: August 20, 2019Assignee: Hoffmann-La Roche Inc.Inventors: Hans Hilpert, Sabine Kolczewski, Anja Limberg, 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: 20190016719Abstract: The present invention is concerned with indolin-2-one and 1,3-dihydro-pyrrolo[3,2-c]pyridin-2-one derivatives of general formula I wherein Ar1, A2, R1, R2, R3, X and n are as described herein and pharmaceutically acceptable salts thereof for treatment of central nervous system disordersType: ApplicationFiled: August 9, 2018Publication date: January 17, 2019Applicant: Hoffmann-La Roche Inc.Inventors: Hans Hilpert, Sabine Kolczewski, Anja Limberg, Theodor Stoll
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Publication number: 20180362578Abstract: The present invention provides compounds of formula (I) wherein X1 to X8 and R1 to R8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.Type: ApplicationFiled: June 12, 2018Publication date: December 20, 2018Applicant: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Julien Beignet, Konrad Bleicher, Bernhard Fasching, Hans Hilpert, Taishan Hu, Dwight MacDonald, Stephen Jackson, Sabine Kolczewski, Carsten Kroll, Adrian Schaeublin, Hong Shen, Theodor Stoll, Helmut Thomas, Amal Wahhab, Claudia Zampaloni
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Patent number: 10112938Abstract: The present invention is concerned with indolin-2-one and 1,3-dihydro-pyrrolo[3,2-c]pyridin-2-one derivatives of general formula I wherein Ar1, A2, R1, R2, R3, X and n are as described herein and pharmaceutically acceptable salts thereof for treatment of central nervous system disordersType: GrantFiled: November 16, 2016Date of Patent: October 30, 2018Assignee: Hoffman-La Roche Inc.Inventors: Hans Hilpert, Sabine Kolczewski, Anja Limberg, 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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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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Patent number: 10030047Abstract: The present invention provides compounds of formula (I) wherein X1 to X8 and R1 to R8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.Type: GrantFiled: October 27, 2016Date of Patent: July 24, 2018Assignee: HOFFMANN-LA ROCHE INC.Inventors: Alexander Alanine, Julien Beignet, Konrad Bleicher, Bernhard Fasching, Hans Hilpert, Taishan Hu, Dwight MacDonald, Stephen Jackson, Sabine Kolczewski, Carsten Kroll, Adrian Schaeublin, Hong Shen, Theodor Stoll, Helmut Thomas, Amal Wahhab, Claudia Zampaloni
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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: 20170233437Abstract: The present invention provides compounds of formula (I) wherein X1 to X8 and R1 to R8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.Type: ApplicationFiled: October 27, 2016Publication date: August 17, 2017Applicant: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Julien Beignet, Konrad Bleicher, Bernhard Fasching, Hans Hilpert, Taishan Hu, Dwight MacDonald, Stephen Jackson, Sabine Kolczewski, Carsten Kroll, Adrian Schaeublin, Hong Shen, Theodor Stoll, Helmut Thomas, Amal Wahhab, Claudia Zampaloni