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).

  • Publication number: 20230391778
    Abstract: 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 thereof
    Type: Application
    Filed: August 17, 2023
    Publication date: December 7, 2023
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Hans HILPERT, Sabine KOLCZEWSKI, Roland HUMM, Theodor STOLL, Thorsten MUSER, Jean-Marc PLANCHER, Delphine GAUFRETEAU
  • Publication number: 20220411468
    Abstract: 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: Application
    Filed: July 15, 2021
    Publication date: December 29, 2022
    Applicant: 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
  • Patent number: 11447478
    Abstract: 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: Grant
    Filed: April 8, 2014
    Date of Patent: September 20, 2022
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Hans Hilpert, Roland Humm, Thorsten Muser, Christian Schnider, Roger Wermuth, Thomas Woltering
  • Publication number: 20220033395
    Abstract: 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 thereof
    Type: Application
    Filed: April 22, 2021
    Publication date: February 3, 2022
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Hans Hilpert, Sabine Kolczewski, Roland Humm, Theodor Stoll, Thorsten Muser, Jean-Marc Plancher, Delphine Gaufreteau
  • Patent number: 11098080
    Abstract: 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: Grant
    Filed: June 12, 2018
    Date of Patent: August 24, 2021
    Assignee: 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
  • Publication number: 20210246133
    Abstract: 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 thereof
    Type: Application
    Filed: October 13, 2020
    Publication date: August 12, 2021
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Hans Hilpert, Sabine Kolczewski, Roland Humm, Theodor Stoll, Thorsten Muser, Jean-Marc Plancher, Delphine Gaufreteau
  • Patent number: 11066443
    Abstract: 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: Grant
    Filed: April 9, 2018
    Date of Patent: July 20, 2021
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Alanine, Kurt Amrein, Konrad Bleicher, Bernhard Fasching, Hans Hilpert, Sabine Kolczewski, Carsten Kroll, Adrian Schaeublin, Claudia Zampaloni
  • Publication number: 20200040031
    Abstract: 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: Application
    Filed: April 9, 2018
    Publication date: February 6, 2020
    Inventors: Alexander Alanine, Kurt Amrein, Konrad Bleicher, Bernhard Fasching, Hans Hilpert, Sabine Kolczewski, Carsten Kroll, Adrian Schaeublin, Claudia Zampaloni
  • Publication number: 20200010466
    Abstract: 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 thereof
    Type: Application
    Filed: July 19, 2019
    Publication date: January 9, 2020
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Hans Hilpert, Sabine Kolczewski, Roland Humm, Theodor Stoll, Thorsten Muser, Jean-Marc Plancher, Delphine Gaufreteau
  • Patent number: 10457667
    Abstract: 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: Grant
    Filed: May 4, 2018
    Date of Patent: October 29, 2019
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Delphine Gaufreteau, Hans Hilpert, Roland Humm, Sabine Kolczewski, Thorsten Muser, Jean-Marc Plancher, Theodor Stoll
  • Patent number: 10385050
    Abstract: 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 disorders
    Type: Grant
    Filed: August 9, 2018
    Date of Patent: August 20, 2019
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans Hilpert, Sabine Kolczewski, Anja Limberg, Theodor Stoll
  • Patent number: 10377746
    Abstract: 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: Grant
    Filed: May 4, 2018
    Date of Patent: August 13, 2019
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Delphine Gaufreteau, Hans Hilpert, Roland Humm, Sabine Kolczewski, Thorsten Muser, Jean-Marc Plancher, Theodor Stoll
  • Publication number: 20190016719
    Abstract: 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 disorders
    Type: Application
    Filed: August 9, 2018
    Publication date: January 17, 2019
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Hans Hilpert, Sabine Kolczewski, Anja Limberg, Theodor Stoll
  • Publication number: 20180362578
    Abstract: 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: Application
    Filed: June 12, 2018
    Publication date: December 20, 2018
    Applicant: 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
  • Patent number: 10112938
    Abstract: 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 disorders
    Type: Grant
    Filed: November 16, 2016
    Date of Patent: October 30, 2018
    Assignee: Hoffman-La Roche Inc.
    Inventors: Hans Hilpert, Sabine Kolczewski, Anja Limberg, Theodor Stoll
  • Publication number: 20180251455
    Abstract: 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: Application
    Filed: May 4, 2018
    Publication date: September 6, 2018
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Delphine Gaufreteau, Hans Hilpert, Roland Humm, Sabine Kolczewski, Thorsten Muser, Jean-Marc Plancher, Theodor Stoll
  • Publication number: 20180251451
    Abstract: 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: Application
    Filed: May 4, 2018
    Publication date: September 6, 2018
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Delphine Gaufreteau, Hans Hilpert, Roland Humm, Sabine Kolczewski, Thorsten Muser, Jean-Marc Plancher, Theodor Stoll
  • Patent number: 10030047
    Abstract: 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: Grant
    Filed: October 27, 2016
    Date of Patent: July 24, 2018
    Assignee: 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
  • Patent number: 9988390
    Abstract: 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: Grant
    Filed: October 28, 2016
    Date of Patent: June 5, 2018
    Inventors: Hans Hilpert, Lukas Kreis, Christian Lerner, Roland Humm, Thorsten Muser, Bernd Kuhn
  • Publication number: 20170267680
    Abstract: 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: Application
    Filed: October 28, 2016
    Publication date: September 21, 2017
    Inventors: Hans HILPERT, Lukas KREIS, Christian LERNER, Roland HUMM, Thorsten MUSER, Bernd KUHN