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: 20170233437
    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: October 27, 2016
    Publication date: August 17, 2017
    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
  • Publication number: 20170101409
    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: December 22, 2016
    Publication date: April 13, 2017
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Hans Hilpert, Sabine Kolczewski, Roland Humm, Theodor Stoll, Thorsten Muser, Jean-Marc Plancher, Delphine Gaufreteau
  • Patent number: 9616053
    Abstract: The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula (I) wherein Ar, X, X1, R1, R2, R3, m, n and the dotted line are as defined herein which compounds are useful for treating certain central nervous system disorders as described herein.
    Type: Grant
    Filed: December 16, 2015
    Date of Patent: April 11, 2017
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniela Brunner, Hans Hilpert, Sabine Kolczewski, Anja Limberg, Jessica Malberg, Eric Prinssen, Claus Riemer, Bavani G. Shankar, Theodor Stoll
  • Publication number: 20170057960
    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: November 16, 2016
    Publication date: March 2, 2017
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Hans Hilpert, Sabine Kolczewski, Anja Limberg, Theodor Stoll
  • Publication number: 20160095844
    Abstract: The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula wherein Ar is a 6-membered heteroaryl group, containing one or two N-atoms, which are the groups, pyridinyl, pyrimidinyl, pyridazinyl, or a 5-membered heteroaryl group containing from 1 to 3 heteroatoms, selected from N, S or O, which groups are imidazolyl, 1,2,4-oxadiazolyl, 1,3,4-oxadazolyl, isoxazolyl, oxazolyl, 1,3,4-thiadiazolyl or pyrazolyl; R1 is hydrogen, lower alkyl, halogen, amino, dimethylamino, cyano, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, CH(OH)CF3, (CH2)o-lower alkoxy, cycloalkyl optionally substituted by CF3, or heterocycloalkyl optionally substituted by lower alkyl; R2 is hydrogen, lower alkyl, (CH2)o-cycloalkyl, (CH2)o—O-cycloalkyl, (CH2)o-lower alkoxy, CH2)o-lower alkoxy substituted by halogen, (CH2)o-heterocycloalkyl optionally substituted by lower alkyl, (CH2)o—S(O)2-cycloalkyl, lower alkyl substituted by one or two hydroxy, lower alkyl substituted by one or two lo
    Type: Application
    Filed: December 16, 2015
    Publication date: April 7, 2016
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Daniela Brunner, Hans Hilpert, Sabine Kolczewski, Anja Limberg, Jessica Malberg, Eric Prinssen, Claus Riemer, Bavani G. Shankar, Theodor Stoll
  • Patent number: 9273042
    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: May 21, 2013
    Date of Patent: March 1, 2016
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Hans Hilpert, Thomas Woltering
  • Publication number: 20160052920
    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: Application
    Filed: April 8, 2014
    Publication date: February 25, 2016
    Applicants: HOFFMANN-LA ROCHE INC., SIENA BIOTECH S.p.A.
    Inventors: Hans Hilpert, Roland Humm, Thorsten Muser, Christian Schnider, Roger Wermuth, Thomas Woltering
  • Patent number: 9242943
    Abstract: The present invention relates to 1,4 Oxazines of formula I having BACE1 and/or BACE2 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 and type 2 diabetes.
    Type: Grant
    Filed: January 12, 2012
    Date of Patent: January 26, 2016
    Assignees: SIENA BIOTECH S.P.A., HOFFMANN-LA ROCHE INC.
    Inventors: Matteo Andreini, Emanuele Gabellieri, Wolfgang Guba, Hans Hilpert, Alexander V. Mayweg, Robert Narquizian, Eoin Power, Massimiliano Travagli, Thomas Woltering, Wolfgang Wostl, Harald Mauser
  • Publication number: 20150376172
    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: Application
    Filed: January 15, 2014
    Publication date: December 31, 2015
    Inventors: Wolfgang Guba, Hans Hilpert, Andreas Kuglstatter, Anja Limberg, Ulrike Obst Sander, Emmanuel Pinard, Wolfgang Wostl, Thomas Woltering
  • Publication number: 20150322054
    Abstract: The present invention provides 4-(3-Amino-phenyl)-5,6-dihydro-4H-[1,3]oxazin-2-ylamines of formula I having BACE1 and/or BACE2 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 and type 2 diabetes.
    Type: Application
    Filed: July 20, 2015
    Publication date: November 12, 2015
    Inventors: Hans Hilpert, Wolfgang Wostl
  • Patent number: 9181232
    Abstract: Provided herein is a compound of formula I: as wells as a pharmaceutical composition, a process of making and a method of using a compound of formula I. The compounds of formula I are BACE1 inhibitors useful for the treatment of, for example, Alzheimer's Disease.
    Type: Grant
    Filed: June 24, 2013
    Date of Patent: November 10, 2015
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventor: Hans Hilpert
  • Patent number: 9115098
    Abstract: The present invention provides 4-(3-Amino-phenyl)-5,6-dihydro-4H-[1,3]oxazin-2-ylamines of formula I having BACE1 and/or BACE2 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 and type 2 diabetes.
    Type: Grant
    Filed: May 2, 2014
    Date of Patent: August 25, 2015
    Assignee: HOFFMAN-LA ROCHE INC.
    Inventors: Hans Hilpert, Wolfgang Wostl
  • Patent number: 9073909
    Abstract: The present invention provides compounds of formula I having BACE1 and/or BACE2 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 and type 2 diabetes. The invention further provides a radio-labelled derivative thereof.
    Type: Grant
    Filed: June 4, 2012
    Date of Patent: July 7, 2015
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Edilio Boroni, Luca Gobbi, Hans Hilpert, Michael Honer, Dieter Murl, Robert Narquizian, Alessandra Polara
  • Patent number: 9067924
    Abstract: The present invention relates to 1,4 Thiazepines/Sulfones of formula I having BACE1 and/or BACE2 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 and type 2 diabetes.
    Type: Grant
    Filed: February 27, 2012
    Date of Patent: June 30, 2015
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Hans Hilpert, Mark Rogers-Evans, Didier Rombach
  • Patent number: 9067926
    Abstract: Provided herein is a compound of formula I: as wells as a pharmaceutical composition, a process of making and a method of using a compound of formula I. The compounds of formula I are BACE1 inhibitors useful for the treatement of, for example, Alzheimer's Disease.
    Type: Grant
    Filed: January 23, 2013
    Date of Patent: June 30, 2015
    Assignees: HOFFMANN-LA ROCHE INC., SIENA BIOTECH S.P.A.
    Inventors: Hans Hilpert, Roland Humm, Thomas Woltering
  • Publication number: 20150141413
    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: Application
    Filed: May 21, 2013
    Publication date: May 21, 2015
    Inventors: Hans Hilpert, Thomas Woltering
  • Publication number: 20150133440
    Abstract: The present invention provides difluoro-cyclopentaoxazinyls and difluoroenzooxazinyls 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: Application
    Filed: June 24, 2013
    Publication date: May 14, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hans Hilpert
  • Publication number: 20150031690
    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: Application
    Filed: January 23, 2013
    Publication date: January 29, 2015
    Applicants: F. Hoffmann-La Roche AG, Siena Biotech S.P.A
    Inventors: Hans Hilpert, Roland Humm, Thomas Woltering
  • Publication number: 20140336208
    Abstract: This invention relates to compounds of the formula wherein R1 to R9 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as diabetes, particularly type 2 diabetes, and other metabolic disorders.
    Type: Application
    Filed: July 9, 2014
    Publication date: November 13, 2014
    Inventors: David Banner, Emanuele Gabellieri, Wolfgang Guba, Hans Hilpert, Benoit Hornsperger, Roland Humm, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Emmanuel Pinard, Mark Rogers-Evans, Thomas Woltering, Wolfgang Wostl
  • Publication number: 20140323469
    Abstract: This invention relates to compounds of the formula wherein and R1 to R3 are as described herein, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BACE2 inhibitors and can be used as pharmaceuticals for the therapeutic and/or prophylactic treatment of diseases such as Alzheimer's disease, diabetes, particularly type 2 diabetes, and other metabolic disorders.
    Type: Application
    Filed: July 14, 2014
    Publication date: October 30, 2014
    Inventors: Hans Hilpert, Robert Narquizian