Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/48)
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Patent number: 10253042Abstract: 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: GrantFiled: August 16, 2017Date of Patent: April 9, 2019Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Lei Zhang, Brian Thomas O'Neill
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Patent number: 10047081Abstract: 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: March 16, 2016Date of Patent: August 14, 2018Assignee: Hoffman-La Roche Inc.Inventors: Bjoern Bartels, Cosimo Dolente, Wolfgang Guba, Wolfgang Haap, Ulrike Obst Sander, Jens-Uwe Peters, Thomas Woltering
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Patent number: 10028962Abstract: 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: GrantFiled: June 21, 2017Date of Patent: July 24, 2018Assignee: 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
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Patent number: 9920072Abstract: 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: October 30, 2015Date of Patent: March 20, 2018Assignee: 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
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Patent number: 9771379Abstract: 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: GrantFiled: September 22, 2016Date of Patent: September 26, 2017Assignee: PFIZER INC.Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Lei Zhang, Brian Thomas O'Neill
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Patent number: 9744173Abstract: 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: GrantFiled: February 8, 2017Date of Patent: August 29, 2017Assignee: 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
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Patent number: 9605007Abstract: 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: GrantFiled: July 20, 2016Date of Patent: March 28, 2017Assignee: 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
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Patent number: 9550795Abstract: 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: GrantFiled: December 4, 2014Date of Patent: January 24, 2017Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Christopher John Helal, Brian Thomas O'Neill
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Patent number: 9540397Abstract: 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: October 7, 2015Date of Patent: January 10, 2017Assignee: 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
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Patent number: 9522923Abstract: The present invention provides a compound of Formula II: or a pharmaceutically acceptable salt thereof, that are inhibitors of BACE.Type: GrantFiled: February 17, 2016Date of Patent: December 20, 2016Assignee: Eli Lilly and CompanyInventors: Simon James Richards, Erik James Hembre, Jose Eduardo Lopez, Leonard Larry Winneroski, Jr., Timothy Andrew Woods, Jennifer Anne McMahon
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Patent number: 9428523Abstract: 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: GrantFiled: February 9, 2016Date of Patent: August 30, 2016Assignee: 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
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Patent number: 9403846Abstract: 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: GrantFiled: December 4, 2013Date of Patent: August 2, 2016Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Brian Thomas O'Neill, Christopher Ryan Butler, Erik Alphie LaChapelle
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Patent number: 9365589Abstract: 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: GrantFiled: December 16, 2013Date of Patent: June 14, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Jared N. Cumming, David Earl Kaelin, Jr., Jack D. Scott, Wen-Lian Wu, Duane A. Burnett
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Patent number: 9328124Abstract: 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: GrantFiled: October 17, 2013Date of Patent: May 3, 2016Assignee: Eli Lilly and CompanyInventors: Fionna Mitchell Martin, Dustin James Mergott, William Martin Owton
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Patent number: 9315520Abstract: 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: GrantFiled: April 9, 2015Date of Patent: April 19, 2016Assignee: 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
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Patent number: 9260455Abstract: 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: GrantFiled: September 9, 2013Date of Patent: February 16, 2016Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Elizabeth Mary Beck, Christopher Ryan Butler, Jennifer Elizabeth Davoren
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Patent number: 9233981Abstract: 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: GrantFiled: February 2, 2014Date of Patent: January 12, 2016Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Brian Thomas O'Neill, Christopher Ryan Butler, Elizabeth Mary Beck
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Patent number: 9175013Abstract: 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: GrantFiled: January 19, 2012Date of Patent: November 3, 2015Assignee: Eisai R&D Management Co., Ltd.Inventors: Mamoru Takaishi, Tasuku Ishida
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Patent number: 9169271Abstract: 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: GrantFiled: April 2, 2015Date of Patent: October 27, 2015Assignee: Eli Lilly and CompanyInventors: Steven James Green, Erik James Hembre, Dustin James Mergott, Yuan Shi, Brian Morgan Watson, Leonard Larry Winneroski, Jr.
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Patent number: 9045498Abstract: 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: GrantFiled: July 8, 2014Date of Patent: June 2, 2015Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Elizabeth Mary Beck, Christopher Ryan Butler, Jennifer Elizabeth Davoren, Brian Thomas O'Neill
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Publication number: 20150148334Abstract: 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: ApplicationFiled: June 27, 2014Publication date: May 28, 2015Inventors: Brian S. Freeze, Masaaki Hirose, Hong Myung Lee, Todd B. Sells, Zhan Shi, Leo R. Takaoka, Stepan Vyskocil, Tianlin Xu
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Publication number: 20150141412Abstract: 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: ApplicationFiled: May 9, 2012Publication date: May 21, 2015Applicant: ICROM SpAInventors: Mario Leone, Pierfrancesco Morosini
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Publication number: 20150133438Abstract: 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: ApplicationFiled: January 9, 2015Publication date: May 14, 2015Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Elizabeth Mary Beck, Jennifer Elizabeth Davoren, Brian Thomas O'Neill
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Publication number: 20150087637Abstract: 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: ApplicationFiled: December 4, 2014Publication date: March 26, 2015Applicant: PFIZER INC.Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Christopher John Helal, Brian Thomas O'Neill
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Patent number: 8987254Abstract: 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: GrantFiled: August 7, 2014Date of Patent: March 24, 2015Assignee: Eli Lilly and CompanyInventors: Steven James Green, Dustin James Mergott, Brian Morgan Watson, Leonard Larry Winneroski, Jr.
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Publication number: 20150080373Abstract: 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: ApplicationFiled: November 25, 2014Publication date: March 19, 2015Inventors: Berangere Gaucher, Franck Hubert Danel, Patrick Roussel
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Publication number: 20150072975Abstract: 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: ApplicationFiled: November 18, 2014Publication date: March 12, 2015Inventors: Berangere Gaucher, JR., Franck Hubert Danel, XiaoHu Tang, Tong Xie, Lin XU
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Publication number: 20150065493Abstract: Process of preparing sterile brinzolamide using ethylene-oxide gas sterilisation, sterile brinzolamide obtainable by said process and pharmaceutical compositions comprising said sterile brinzolamide.Type: ApplicationFiled: March 15, 2013Publication date: March 5, 2015Applicant: AZAD Pharmaceutical Ingredients AGInventors: Van Van Khov-Tran, Frank Porstmann, Jan Ondracek, Gregory Grams
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Patent number: 8962618Abstract: 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: GrantFiled: April 27, 2012Date of Patent: February 24, 2015Assignee: 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
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Patent number: 8962616Abstract: 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: GrantFiled: May 3, 2013Date of Patent: February 24, 2015Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Elizabeth Mary Beck, Jennifer Elizabeth Davoren, Brian Thomas O'Neill
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Publication number: 20150051188Abstract: 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: ApplicationFiled: November 7, 2012Publication date: February 19, 2015Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
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Patent number: 8946210Abstract: 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: GrantFiled: December 21, 2011Date of Patent: February 3, 2015Assignee: 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
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Patent number: 8946211Abstract: 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: GrantFiled: March 14, 2013Date of Patent: February 3, 2015Assignee: 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
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Patent number: 8940734Abstract: 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: GrantFiled: October 18, 2013Date of Patent: January 27, 2015Assignee: Eisai R&D Management Co., Ltd.Inventors: Adrian Hall, Christopher Neil Farthing, Jose Luis Castro Pineiro
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Patent number: 8933221Abstract: 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: GrantFiled: August 28, 2012Date of Patent: January 13, 2015Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Christopher John Helal, Brian Thomas O'Neill
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Patent number: 8933441Abstract: 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: GrantFiled: January 8, 2013Date of Patent: January 13, 2015Assignee: Samsung Electronics Co., Ltd.Inventors: Jong Won Chung, Bang Lin Lee, Jeong Il Park, Yong Wan Jin
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Publication number: 20140371212Abstract: 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: ApplicationFiled: June 11, 2014Publication date: December 18, 2014Inventors: Steven James GREEN, Erik James HEMBRE, Dustin James MERGOTT, Yuan SHI, Brian Morgan WATSON, Leonard Larry WINNEROSKI, JR.
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Publication number: 20140364426Abstract: 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: ApplicationFiled: August 21, 2014Publication date: December 11, 2014Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Elizabeth Mary Beck, Jennifer Elizabeth Davoren, Erik Alphie LaChapelle, Brian Thomas O'Neill
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Publication number: 20140350245Abstract: 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: ApplicationFiled: August 7, 2014Publication date: November 27, 2014Inventors: Steven James GREEN, Dustin James MERGOTT, Brian Morgan WATSON, Leonard Larry WINNEROSKI, JR.
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Patent number: 8889856Abstract: 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: GrantFiled: May 22, 2014Date of Patent: November 18, 2014Assignee: Eli Lilly and CompanyInventors: 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.
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Publication number: 20140336177Abstract: 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: ApplicationFiled: December 11, 2012Publication date: November 13, 2014Inventors: Barbara Pio, Alexander Pasternak, Aurash Shahripour, Haifeng Tang, Shawn Walsh
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Publication number: 20140323474Abstract: 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: ApplicationFiled: July 8, 2014Publication date: October 30, 2014Inventors: Michael Aaron Brodney, Elizabeth Mary Beck, Christopher Ryan Butler, Jennifer Elizabeth Davoren, Brian Thomas O'Neill
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Patent number: 8865706Abstract: 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: GrantFiled: February 12, 2014Date of Patent: October 21, 2014Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Elizabeth Mary Beck, Jennifer Elizabeth Davoren, Erik Alphie LaChapelle, Brian Thomas O'Neill
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Publication number: 20140309218Abstract: 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: ApplicationFiled: November 29, 2012Publication date: October 16, 2014Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
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Patent number: 8841293Abstract: 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: GrantFiled: March 4, 2014Date of Patent: September 23, 2014Assignee: Eli Lilly and CompanyInventors: Steven James Green, Dustin James Mergott, Brian Morgan Watson, Leonard Larry Winneroski, Jr.
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Publication number: 20140275044Abstract: 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: ApplicationFiled: March 4, 2014Publication date: September 18, 2014Applicant: Eli Lilly and CompanyInventors: Steven James GREEN, Dustin James MERGOTT, Brian Morgan WATSON, Leonard Larry WINNEROSKI, JR.
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Publication number: 20140256933Abstract: 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: ApplicationFiled: May 22, 2014Publication date: September 11, 2014Applicant: Eli Lilly and CompanyInventors: 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.
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Patent number: 8822455Abstract: 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: GrantFiled: January 5, 2012Date of Patent: September 2, 2014Assignee: Eisai R&D Management Co., Ltd.Inventors: Paschalis Dimopoulos, Adrian Hall, Yoichi Kita, Andrew Madin, Nicola Louise Shuker
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Patent number: 8822456Abstract: 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: GrantFiled: December 10, 2013Date of Patent: September 2, 2014Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Elizabeth Mary Beck, Christopher Ryan Butler, Jennifer Elizabeth Davoren, Brian Thomas O'Neill
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Publication number: 20140243302Abstract: 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: ApplicationFiled: June 26, 2012Publication date: August 28, 2014Applicants: MERCK SHARP & DOHME CORPORATION, KYORIN PHARMACEUTICAL CO., LTD.Inventors: Yasumichi Fukuda, David E. Kaelin, JR., Sheo B. Singh