Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/48)
  • Patent number: 10253042
    Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, wherein the variables R1, R2, R3, R4 and X are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: August 16, 2017
    Date of Patent: April 9, 2019
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Lei Zhang, Brian Thomas O'Neill
  • Patent number: 10047081
    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: March 16, 2016
    Date of Patent: August 14, 2018
    Assignee: Hoffman-La Roche Inc.
    Inventors: Bjoern Bartels, Cosimo Dolente, Wolfgang Guba, Wolfgang Haap, Ulrike Obst Sander, Jens-Uwe Peters, Thomas Woltering
  • Patent number: 10028962
    Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variable R1 is as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: June 21, 2017
    Date of Patent: July 24, 2018
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Elizabeth Mary Beck, Christopher Ryan Butler, Lei Zhang, Brian Thomas O'Neill, Gabriela Barreiro, Erik Alphie LaChapelle, Bruce Nelsen Rogers
  • Patent number: 9920072
    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: October 30, 2015
    Date of Patent: March 20, 2018
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Bjoern Bartels, Cosimo Dolente, Wolfgang Guba, Wolfgang Haap, Ulrike Obst Sander, Jens-Uwe Peters, Mark Rogers-Evans, Didier Rombach, Thomas Woltering
  • Patent number: 9771379
    Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, wherein the variables R1, R2, R3, R4 and X are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: September 22, 2016
    Date of Patent: September 26, 2017
    Assignee: PFIZER INC.
    Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Lei Zhang, Brian Thomas O'Neill
  • Patent number: 9744173
    Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variable R1 is as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: February 8, 2017
    Date of Patent: August 29, 2017
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Elizabeth Mary Beck, Christopher Ryan Butler, Lei Zhang, Brian Thomas O'Neill, Gabriela Barreiro, Erik Alphie LaChapelle, Bruce Nelsen Rogers
  • Patent number: 9605007
    Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variable R1 is as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: July 20, 2016
    Date of Patent: March 28, 2017
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Elizabeth Mary Beck, Christopher Ryan Butler, Lei Zhang, Brian Thomas O'Neill, Gabriela Barreiro, Erik Alphie LaChapelle, Bruce Nelsen Rogers
  • Patent number: 9550795
    Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: December 4, 2014
    Date of Patent: January 24, 2017
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Christopher John Helal, Brian Thomas O'Neill
  • Patent number: 9540397
    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: October 7, 2015
    Date of Patent: January 10, 2017
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bjoern Bartels, Philipp Cueni, Cosimo Dolente, Wolfgang Guba, Wolfgang Haap, Andreas Kuglstatter, Ulrike Obst Sander, Jens-Uwe Peters, Mark Rogers-Evans, Walter Vifian, Thomas Woltering
  • Patent number: 9522923
    Abstract: The present invention provides a compound of Formula II: or a pharmaceutically acceptable salt thereof, that are inhibitors of BACE.
    Type: Grant
    Filed: February 17, 2016
    Date of Patent: December 20, 2016
    Assignee: Eli Lilly and Company
    Inventors: Simon James Richards, Erik James Hembre, Jose Eduardo Lopez, Leonard Larry Winneroski, Jr., Timothy Andrew Woods, Jennifer Anne McMahon
  • Patent number: 9428523
    Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variable R1 is as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: February 9, 2016
    Date of Patent: August 30, 2016
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Elizabeth Mary Beck, Christopher Ryan Butler, Lei Zhang, Brian Thomas O'Neill, Gabriela Barreiro, Erik Alphie LaChapelle, Bruce Nelsen Rogers
  • Patent number: 9403846
    Abstract: The present invention provides compounds of formula I, wherein the variables R1, R2, R5 and b are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: December 4, 2013
    Date of Patent: August 2, 2016
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Brian Thomas O'Neill, Christopher Ryan Butler, Erik Alphie LaChapelle
  • Patent number: 9365589
    Abstract: In its many embodiments, the present invention provides certain C2-ring-substituted iminothiazine compounds, including compounds Formula (I): (structurally represented) or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and, wherein R1, R2, R3, R4, X, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
    Type: Grant
    Filed: December 16, 2013
    Date of Patent: June 14, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, David Earl Kaelin, Jr., Jack D. Scott, Wen-Lian Wu, Duane A. Burnett
  • Patent number: 9328124
    Abstract: The present invention provides compounds of Formula I useful as BACE inhibitors in the treatment of e.g. Alzheimer's disease: wherein A is selected from the group consisting of; of; R1 is H or F; R2 is H, —OCH3, C1-C3 alkyl; R3 is H, —CH3, or —OCH3; and R4 is H or F; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 17, 2013
    Date of Patent: May 3, 2016
    Assignee: Eli Lilly and Company
    Inventors: Fionna Mitchell Martin, Dustin James Mergott, William Martin Owton
  • Patent number: 9315520
    Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variable R1 is as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: April 9, 2015
    Date of Patent: April 19, 2016
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Elizabeth Mary Beck, Christopher Ryan Butler, Lei Zhang, Brian Thomas O'Neill, Gabriela Barreiro, Erik Alphie LaChapelle, Bruce Nelsen Rogers
  • Patent number: 9260455
    Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, wherein the variables R1 and R2 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: September 9, 2013
    Date of Patent: February 16, 2016
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Elizabeth Mary Beck, Christopher Ryan Butler, Jennifer Elizabeth Davoren
  • Patent number: 9233981
    Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, wherein the variables R1 and R2 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: February 2, 2014
    Date of Patent: January 12, 2016
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Brian Thomas O'Neill, Christopher Ryan Butler, Elizabeth Mary Beck
  • Patent number: 9175013
    Abstract: The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; R is monofluoromethyl or difluoromethyl; and pharmaceutically acceptable salts thereof; which compound has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.
    Type: Grant
    Filed: January 19, 2012
    Date of Patent: November 3, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Mamoru Takaishi, Tasuku Ishida
  • Patent number: 9169271
    Abstract: The present invention provides a compound of Formula III: wherein A is: and Z, R1, R2, R3, and R4 are as defined herein, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 2, 2015
    Date of Patent: October 27, 2015
    Assignee: Eli Lilly and Company
    Inventors: Steven James Green, Erik James Hembre, Dustin James Mergott, Yuan Shi, Brian Morgan Watson, Leonard Larry Winneroski, Jr.
  • Patent number: 9045498
    Abstract: The present invention provides compounds of Formula I, and the tautomers thereof, and the pharmaceutically acceptable salts of the compounds and tautomers, wherein the compounds have the structure wherein the variables R1, R2, R3, R4 and x are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: July 8, 2014
    Date of Patent: June 2, 2015
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Elizabeth Mary Beck, Christopher Ryan Butler, Jennifer Elizabeth Davoren, Brian Thomas O'Neill
  • Publication number: 20150148334
    Abstract: This invention provides compounds of formula I-A or I-B: wherein HY, G1, G2, R2, R12, W1, W2, n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: June 27, 2014
    Publication date: May 28, 2015
    Inventors: Brian S. Freeze, Masaaki Hirose, Hong Myung Lee, Todd B. Sells, Zhan Shi, Leo R. Takaoka, Stepan Vyskocil, Tianlin Xu
  • Publication number: 20150141412
    Abstract: The invention refers to a process for preparing sterile active pharmaceutical ingredients (APIs) useful in the preparation of sterile product for ophthalmic use. The process comprises the gamma-ray sterilization treatment of the APIs powder in a protective atmosphere.
    Type: Application
    Filed: May 9, 2012
    Publication date: May 21, 2015
    Applicant: ICROM SpA
    Inventors: Mario Leone, Pierfrancesco Morosini
  • Publication number: 20150133438
    Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Application
    Filed: January 9, 2015
    Publication date: May 14, 2015
    Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Elizabeth Mary Beck, Jennifer Elizabeth Davoren, Brian Thomas O'Neill
  • Publication number: 20150087637
    Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Application
    Filed: December 4, 2014
    Publication date: March 26, 2015
    Applicant: PFIZER INC.
    Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Christopher John Helal, Brian Thomas O'Neill
  • Patent number: 8987254
    Abstract: The present invention provides a compound of Formula I: wherein R is H or F; and A is: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 7, 2014
    Date of Patent: March 24, 2015
    Assignee: Eli Lilly and Company
    Inventors: Steven James Green, Dustin James Mergott, Brian Morgan Watson, Leonard Larry Winneroski, Jr.
  • Publication number: 20150080373
    Abstract: The antibacterial compound of formula I wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; A1, A2, A3, R1 and R4 represent various substituents, G represents aryl or heteroaryl, which is unsubstituted or substituted which compounds show good activity against pathogenic bacteria.
    Type: Application
    Filed: November 25, 2014
    Publication date: March 19, 2015
    Inventors: Berangere Gaucher, Franck Hubert Danel, Patrick Roussel
  • Publication number: 20150072975
    Abstract: The present invention relates to antibacterial compounds of formula I: wherein all variable substituents are defined as described herein, which are useful for the treatment of bacterial infections.
    Type: Application
    Filed: November 18, 2014
    Publication date: March 12, 2015
    Inventors: Berangere Gaucher, JR., Franck Hubert Danel, XiaoHu Tang, Tong Xie, Lin XU
  • Publication number: 20150065493
    Abstract: Process of preparing sterile brinzolamide using ethylene-oxide gas sterilisation, sterile brinzolamide obtainable by said process and pharmaceutical compositions comprising said sterile brinzolamide.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 5, 2015
    Applicant: AZAD Pharmaceutical Ingredients AG
    Inventors: Van Van Khov-Tran, Frank Porstmann, Jan Ondracek, Gregory Grams
  • Patent number: 8962616
    Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: May 3, 2013
    Date of Patent: February 24, 2015
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Elizabeth Mary Beck, Jennifer Elizabeth Davoren, Brian Thomas O'Neill
  • Patent number: 8962618
    Abstract: The invention pertains to the use of fused bicyclo heterocyclic adducts of thiohdroxy pridines or primidines as diacylglycerol O-acyltransferase 1 DGAT-1 inhibitors to treat hyperlipidiemias and various diseases and disorders associated therewith. Other conditions also can be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: February 24, 2015
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: K. Raja Reddy, Jeff Stebbins, Serge H. Boyer, Mark D. Erion, Scott J. Hecker, Nicholas Brian Raffaele, Brett C. Bookser, Venkat Reddy Mali
  • Publication number: 20150051188
    Abstract: The invention relates to antibacterial compounds of formula I wherein R1a represents H or carboxy and R1b represents H, or R1a and R1b represent together either the group *—C(O)—NH—S—# or the group *—C(OH)?N—S—# wherein “*” represents the point of attachment of R1a and “#” represents the point of attachment of R1b; R2 represents H, (C1-C3)alkyl, hydroxy-(C1-C3)alkyl, benzyl or (C3-C5)cycloalkyl; R3 represents H or halogen; U represents N or CR4; wherein R4 is H or (C1-C3)alkoxy; A represents CH, B represents NH and m represents 1 or 2 and n represents 1 or 2; or A represents N, B is absent, m represents 2 and n represents 2; Y represents CH or N; and Q represents O or S; and salts of such compounds.
    Type: Application
    Filed: November 7, 2012
    Publication date: February 19, 2015
    Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
  • Patent number: 8946211
    Abstract: A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: February 3, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Yuichi Suzuki, Takafumi Motoki, Toshihiko Kaneko, Mamoru Takaishi, Tasuku Ishida, Yoichi Kita, Kunitoshi Takeda, Noboru Yamamoto, Afzal Khan, Paschalis Dimopoulos
  • Patent number: 8946210
    Abstract: A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: February 3, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Yuichi Suzuki, Takafumi Motoki, Toshihiko Kaneko, Mamoru Takaishi, Tasuku Ishida, Yoichi Kita, Kunitoshi Takeda, Noboru Yamamoto, Afzal Khan, Paschalis Dimopoulos
  • Patent number: 8940734
    Abstract: The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; A is CH or N; Y is methyl, ethyl, monofluoromethyl, difluoromethyl, trifluoromethyl, difluoroethyl, methoxy, ethoxy, methoxymethyl or —C?N; and pharmaceutically acceptable salts thereof; which compound has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.
    Type: Grant
    Filed: October 18, 2013
    Date of Patent: January 27, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Adrian Hall, Christopher Neil Farthing, Jose Luis Castro Pineiro
  • Patent number: 8933221
    Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: August 28, 2012
    Date of Patent: January 13, 2015
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Christopher John Helal, Brian Thomas O'Neill
  • Patent number: 8933441
    Abstract: An organic electronic device may include an organic semiconductor compound represented by the following Chemical Formula 1 or Chemical Formula 2. Each substituent of the above Chemical Formulas 1 and 2 may be the same as described in the detailed description.
    Type: Grant
    Filed: January 8, 2013
    Date of Patent: January 13, 2015
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Jong Won Chung, Bang Lin Lee, Jeong Il Park, Yong Wan Jin
  • Publication number: 20140371212
    Abstract: The present invention provides a compound of Formula III: wherein A is: and Z, R1, R2, R3, and R4 are as defined herein, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: June 11, 2014
    Publication date: December 18, 2014
    Inventors: Steven James GREEN, Erik James HEMBRE, Dustin James MERGOTT, Yuan SHI, Brian Morgan WATSON, Leonard Larry WINNEROSKI, JR.
  • Publication number: 20140364426
    Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variables R1 and R2 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Application
    Filed: August 21, 2014
    Publication date: December 11, 2014
    Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Elizabeth Mary Beck, Jennifer Elizabeth Davoren, Erik Alphie LaChapelle, Brian Thomas O'Neill
  • Publication number: 20140350245
    Abstract: The present invention provides a compound of Formula I: wherein R is H or F; and A is: or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: August 7, 2014
    Publication date: November 27, 2014
    Inventors: Steven James GREEN, Dustin James MERGOTT, Brian Morgan WATSON, Leonard Larry WINNEROSKI, JR.
  • Patent number: 8889856
    Abstract: The present invention provides compounds of Formula I: wherein A is selected from the group consisting of; R1 is H or F; R2 is H, —CH2OH, C1-C3 alkyl, R3 is H, F, or CN; R4 is H, F; or CN; and R5 is H, —CH3, or —OCH3; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 22, 2014
    Date of Patent: November 18, 2014
    Assignee: Eli Lilly and Company
    Inventors: James Peter Beck, Steven James Green, Jose Eduardo Lopez, Brian Michael Mathes, Dustin James Mergott, Warren Jaye Porter, Zoran Rankovic, Yuan Shi, Brian Morgan Watson, Leonard Larry Winneroski, Jr.
  • Publication number: 20140336177
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.
    Type: Application
    Filed: December 11, 2012
    Publication date: November 13, 2014
    Inventors: Barbara Pio, Alexander Pasternak, Aurash Shahripour, Haifeng Tang, Shawn Walsh
  • Publication number: 20140323474
    Abstract: The present invention provides compounds of Formula I, and the tautomers thereof, and the pharmaceutically acceptable salts of the compounds and tautomers, wherein the compounds have the structure wherein the variables R1, R2, R3, R4 and x are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Application
    Filed: July 8, 2014
    Publication date: October 30, 2014
    Inventors: Michael Aaron Brodney, Elizabeth Mary Beck, Christopher Ryan Butler, Jennifer Elizabeth Davoren, Brian Thomas O'Neill
  • Patent number: 8865706
    Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variables R1 and R2 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: February 12, 2014
    Date of Patent: October 21, 2014
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Elizabeth Mary Beck, Jennifer Elizabeth Davoren, Erik Alphie LaChapelle, Brian Thomas O'Neill
  • Publication number: 20140309218
    Abstract: The invention relates to antibacterial compounds of formula I wherein G and K are as defined in the description; and salts of such compounds.
    Type: Application
    Filed: November 29, 2012
    Publication date: October 16, 2014
    Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
  • Patent number: 8841293
    Abstract: The present invention provides a compound of Formula I: Formula I wherein R is H or F; and A is: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 4, 2014
    Date of Patent: September 23, 2014
    Assignee: Eli Lilly and Company
    Inventors: Steven James Green, Dustin James Mergott, Brian Morgan Watson, Leonard Larry Winneroski, Jr.
  • Publication number: 20140275044
    Abstract: The present invention provides a compound of Formula I: wherein R is H or F; and A is: or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: March 4, 2014
    Publication date: September 18, 2014
    Applicant: Eli Lilly and Company
    Inventors: Steven James GREEN, Dustin James MERGOTT, Brian Morgan WATSON, Leonard Larry WINNEROSKI, JR.
  • Publication number: 20140256933
    Abstract: The present invention provides compounds of Formula I: wherein A is selected from the group consisting of; R1 is H or F; R2 is H, —CH2OH, C1-C3 alkyl, R3 is H, F, or CN; R4 is H, F; or CN; and R5 is H, —CH3, or —OCH3; or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 22, 2014
    Publication date: September 11, 2014
    Applicant: Eli Lilly and Company
    Inventors: James Peter BECK, Steven James GREEN, Jose Eduardo LOPEZ, Brian Michael MATHES, Dustin James MERGOTT, Warren Jaye PORTER, Zoran RANKOVIC, Yuan SHI, Brian Morgan WATSON, Leonard Larry WINNEROSKI, JR.
  • Patent number: 8822455
    Abstract: The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein R is hydrogen or C1-6alkyl, optionally substituted by one to five halogen atoms; n is 0, 1, 2 or 3; Ar is phenyl or a 5- or 6-membered heteroaromatic group containing 1, 2 or 3 N atoms, which Ar is optionally substituted by one to three substituents selected from hal, hydroxyl, —CN, C1-6alkyl, C2-3alkenyl, C2-3alkynyl, C1-6alkoxy, C3-6cycloalkoxy and pyrazine, where C1-6alkyl and C1-6alkoxy are optionally substituted by one to three halogen atoms; and pharmaceutically acceptable salts thereof; which compound has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.
    Type: Grant
    Filed: January 5, 2012
    Date of Patent: September 2, 2014
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Paschalis Dimopoulos, Adrian Hall, Yoichi Kita, Andrew Madin, Nicola Louise Shuker
  • Patent number: 8822456
    Abstract: The present invention provides compounds of Formula I, and the tautomers thereof, and the pharmaceutically acceptable salts of the compounds and tautomers, wherein the compounds have the structure wherein the variables R1, R2, R3, R4 and x are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: December 10, 2013
    Date of Patent: September 2, 2014
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Elizabeth Mary Beck, Christopher Ryan Butler, Jennifer Elizabeth Davoren, Brian Thomas O'Neill
  • Publication number: 20140243302
    Abstract: Novel bridged bicyclic compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.
    Type: Application
    Filed: June 26, 2012
    Publication date: August 28, 2014
    Applicants: MERCK SHARP & DOHME CORPORATION, KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Yasumichi Fukuda, David E. Kaelin, JR., Sheo B. Singh