Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
Type:
Application
Filed:
October 6, 2014
Publication date:
April 9, 2015
Inventors:
Shawn Stachel, Daniel V. Paone, Jing Li, Kausik Nanda
Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using such CFTR modulators.
Type:
Grant
Filed:
December 9, 2013
Date of Patent:
April 7, 2015
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Hayley Binch, Dennis Hurley, Lev T. D. Fanning, Peter D. J. Grootenhuis, Martyn Botfield, Fredrick Van Goor
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
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
Abstract: The present invention provides arylpiperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression.
Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, L1, L2, X, Y, Q and Z have defined meanings.
Type:
Application
Filed:
November 13, 2014
Publication date:
March 12, 2015
Inventors:
Laurence Anne Mevellec, Edmond J.K. Ludo, Josephus Carolus Mertens, Jacobus A.J. Van Dun, Maria V.F. Somers, Walter B.L. Wouters
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.
Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
Type:
Application
Filed:
November 11, 2014
Publication date:
March 5, 2015
Inventors:
Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fred Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
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
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
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
Abstract: The present invention relates to a novel fused pyrimidine derivative having an inhibitory activity for tyrosine kinases, and a pharmaceutical composition for preventing or treating cancers, tumors, inflammatory diseases, autoimmune diseases, or immunologically mediated diseases comprising same as an active ingredient.
Type:
Application
Filed:
October 23, 2014
Publication date:
February 12, 2015
Applicant:
HANMI SCIENCE CO., LTD
Inventors:
Mi Young CHA, Seok Jong KANG, Mi Ra KIM, Ju Yeon LEE, Ji Young JEON, Myoung Gi JO, Eun Joo KWAK, Kwang Ok LEE, Tae Hee HA, Kwee Hyun SUH, Maeng Sup KIM
Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.
Type:
Application
Filed:
July 29, 2014
Publication date:
February 5, 2015
Inventors:
Richard T. LEWIS, Jennifer R. ALLEN, James BROWN, Angel GUZMAN-PEREZ, Zihao HUA, Ted JUDD, Qingyian LIU, Philip R. OLIVIERI, Karina ROMERO, Laurie SCHENKEL, John STELLWAGEN, Ryan WHITE
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.
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.
Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, and R6 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (?) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
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
Abstract: The present invention relates to fused pyrroledicarboxamides of the formula (I), in which R1 to R9, X, m and n are as defined in the claims. The compounds of the formula (I) are inhibitors of the acid-sensitive potassium channel TASK-1 and suitable for the treatment of TASK-1 channel-mediated diseases such as arrhythmias, in particular atrial arrhythmias like atrial fibrillation or atrial flutter, and respiratory disorders, in particular sleep-related respiratory disorders like sleep apnea, for example.
Type:
Application
Filed:
February 1, 2013
Publication date:
January 15, 2015
Applicant:
SANOFI
Inventors:
Laurent Bialy, Katrin Lorenz, Klaus Wirth, Klaus Steinmeyer, Gerhard Hessler
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
Abstract: The invention provides novel substituted azaheterocyclic compounds compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases.
Type:
Application
Filed:
January 10, 2013
Publication date:
January 1, 2015
Applicants:
CANCER RESEARCH TECHNOLOGY LIMITED, MERCK PATENT GMBH
Inventors:
Kai Schiemann, Frank Stieber, Christina Esdar
Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
Type:
Application
Filed:
February 28, 2014
Publication date:
January 1, 2015
Inventors:
Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
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.
Abstract: Disclosed are compounds, compositions and methods for treating Type II diabetes. Such compounds are represented by Formula (I) as follows: wherein R1, R2, L, and Q are defined herein.
Type:
Application
Filed:
June 9, 2014
Publication date:
December 11, 2014
Applicant:
JANSSEN PHARMACEUTICA, NV
Inventors:
Mark R. Player, Sanath K. Meegalla, Carl R. Illig, Jinsheng Chen, Kenneth J. Wilson, Yu-Kai Lee, Daniel J. Parks, Hui Huang, Sharmila Patel, Tianbao Lu
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
Abstract: The present disclosure relates to 2,4-pyrimidinediamines substituted with tricyclic carbamates and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, such as JAK2 or JAK3, is therapeutically useful.
Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as or pharmaceutically acceptable salts, or tautomerism isomers, or enantiomers, or diastereomers thereof. The invention also contains compositions including the compounds and methods of using the compounds.
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.
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
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
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
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
Abstract: Benzothiazinethione derivatives of formula (I), their preparative methods and uses are provided. Benzothiazinethione derivatives of the invention have significant effect of inhibiting Mycobacterium tuberculosis.
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.
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
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
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.
Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using such CFTR modulators.
Type:
Application
Filed:
December 9, 2013
Publication date:
August 21, 2014
Applicant:
Vertex Pharmaceuticals Incorporated
Inventors:
Hayley Binch, Dennis Hurley, Lev T.D. Fanning, Peter D.J. Grootenhuis, Martyn Botfield, Fredrick Van Goor
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:
February 12, 2014
Publication date:
August 14, 2014
Applicant:
Pfizer Inc.
Inventors:
Michael Aaron Brodney, Christopher Ryan Butler, Elizabeth Mary Beck, Jennifer Elizabeth Davoren, Erik Alphie LaChapelle, Brian Thomas O'Neill
Abstract: The present invention relates to a hard capsule composite formulation comprising a capsule having a hemispherical closure at each end and an interior space; and one or more tablets encapsulated in the capsule, wherein the tablet or the tablets as a whole have a shape conforming to the internal space of the capsule. The hard capsule composite formulation can efficiently charge pharmaceutical compositions inside the limited interior space of the capsule, and hence, it allows packing a high-dose of pharmaceutical composition in a relatively small-sized capsule, which increases productivity and patient compliance. Also, the composite formulation exhibits good dissolution rate because pharmaceutically active ingredients contained in the capsule are separated from one another, and thus, the ingredients are less affected by the dissolution rate of one another, allowing good storage stability which can optimize the therapeutic effects.
Type:
Application
Filed:
October 15, 2012
Publication date:
August 14, 2014
Applicant:
HANMI PHARM CO., LTD.
Inventors:
Kyeong Soo Kim, Ki Young Jang, Seung Jae Park, Yong Il Kim, Jae Hyun Park, Jong Soo Woo
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:
March 17, 2014
Publication date:
August 7, 2014
Applicant:
Basilea Pharmaceutica AG
Inventors:
Berangere Gaucher, Franck Hubert Danel, Patrick Roussel
Abstract: The present invention provides compounds of Formula Ia and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
Type:
Application
Filed:
August 16, 2012
Publication date:
July 24, 2014
Inventors:
Alexander Pasternak, Timothy Blizzard, Harry Chobanian, Reynalda de Jesus, Fa-Xiang Ding, Shuzhi Dong, Candido Gude, Dooseop Kim, Haifeng Tang, Shawn Walsh, Barbara Pio, Jinlong Jiang
Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Type:
Application
Filed:
January 12, 2013
Publication date:
July 24, 2014
Applicant:
Vanderbilt University
Inventors:
Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
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:
December 4, 2013
Date of Patent:
July 8, 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.
Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds of Formula I wherein X is CR3, and A is and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
Type:
Application
Filed:
February 28, 2014
Publication date:
June 26, 2014
Applicant:
OTSUKA PHARMACEUTICAL CO., LTD.
Inventors:
Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA