Patents by Inventor John W. Clader
John W. Clader has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
-
Patent number: 9278965Abstract: This invention provides for certain bridged and fused compounds of the formula G-L-A??I or a pharmaceutically acceptable salt, ester of solvate thereof wherein: A is and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.Type: GrantFiled: October 2, 2013Date of Patent: March 8, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Hubert B. Josien, John W. Clader, William J. Greenlee, Michael J. Mayer, Jason L. Davis, Shuangyi Wan
-
Patent number: 8759337Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).Type: GrantFiled: December 18, 2009Date of Patent: June 24, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Theodros Asberom, Xianhai Huang, Zhaoning Zhu, John W. Clader, Dmitri A. Pissarnitski, Hubert B. Josien, Hongmei Li
-
Patent number: 8664411Abstract: Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)—O—C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)—O—C(O)-heteroaryl and a basic tertiary amine.Type: GrantFiled: July 1, 2008Date of Patent: March 4, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Wen-Lian Wu, Thomas A. Bara, Duane A. Burnett, John W. Clader, Martin S. Domalski, Yan Jin, Hubert B. Josien, Hongmei Li, Xian Liang, Dmitri A. Pissarnitski, Thavalakulamgara K. Sasikumar, Jesse K. Wong, Ruo Xu, Zhiqiang Zhao, Paul McNamara
-
Publication number: 20140038970Abstract: This invention provides for certain bridged and fused compounds of the formula G-L-A??I or a pharmaceutically acceptable salt, ester of solvate thereof wherein: A is and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.Type: ApplicationFiled: October 2, 2013Publication date: February 6, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: HUBERT B. JOSIEN, John W. Clader, William J. Greenlee, Michael J. Mayer, Jason L. Davis, Shuangyi Wan
-
Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors
Patent number: 8569521Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.Type: GrantFiled: October 6, 2011Date of Patent: October 29, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Theodros Asberom, Thomas A. Bara, Chad E. Bennett, Duane A. Burnett, Mary Anne Caplen, John W. Clader, David J. Cole, Martin S. Domalski, Hubert B. Josien, Chad E. Knutson, Hongmei Li, Mark D. McBriar, Dmitri A. Pissarnitski, Li Qiang, Murali Rajagopalan, Thavalakulamgara K. Sasikumar, Jing Su, Haiqun Tang, Wen-Lian Wu, Ruo Xu, Zhiqiang Zhao -
Patent number: 8426403Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: GrantFiled: May 28, 2008Date of Patent: April 23, 2013Inventors: Zhaoning Zhu, William J. Greenlee, Xianhai Huang, Brian A. McKittrick, John W. Clader, Mark D. McBriar, Anandan Palani
-
BENZENESULFONYL-CHROMANE, THIOCHROMANE, TETRAHYDRONAPHTHALENE AND RELATED GAMMA SECRETASE INHIBITORS
Publication number: 20120264736Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.Type: ApplicationFiled: October 6, 2011Publication date: October 18, 2012Applicant: Schering CorporationInventors: Theodros Asberom, Thomas A. Bara, Chad E. Bennett, Duane A. Burnett, Mary Ann Caplen, John W. Clader, David J. Cole, Martin S. Domalski, Hubert B. Josien, Chad E. Knutson, Hongmei Li, Mark D. McBriar, Dmitri A. Pissarnitski, Li Qiang, Murali Rajagopalan, Thavalakulamgara K. Sasikumar, Jing Su, Haiqun Tang, Wen-Lian Wu, Ruo Xu, Zhiqiang Zhao -
Publication number: 20120135980Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).Type: ApplicationFiled: December 18, 2009Publication date: May 31, 2012Inventors: Theodros Asberom, Zhaoning Zhu, John W. Clader, Zhong-Yue Sun, Mihirbaran Mandal, Gioconda Gallo, Xiaoxiang Liu
-
Patent number: 8114879Abstract: The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v.Type: GrantFiled: March 26, 2008Date of Patent: February 14, 2012Assignee: Schering CorporationInventors: Bahige M. Baroudy, John W. Clader, Hubert B. Josien, Stuart W. McCombie, Brian A. McKittrick, Michael W. Miller, Bernard R. Neustadt, Anandan Palani, Elizabeth M. Smith, Ruo Steensma, Jayaram R. Tagat, Susan F. Vice, Mark A. Laughlin, Eric Gilbert, Marc A. Labroli
-
Publication number: 20110312995Abstract: This invention provides for certain bridged and fused heterocyclic compounds of the formula (I) or a pharmaceutically acceptable salt, ester solvate or prodrug thereof wherein: L is: (II) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.Type: ApplicationFiled: January 21, 2010Publication date: December 22, 2011Applicant: Schering CorporationInventors: Hubert B. Josien, John W. Clader, William J. Greenlee, Michael John Mayer, Robert Jason Herr, Jason L. Davis, Kai Deng, Ming Min Hsia, Shuangyi Wan
-
Publication number: 20110312967Abstract: This invention provides for certain bridged and fused compounds of the formula G-L-A I or a pharmaceutically acceptable salt, ester of solvate thereof wherein: A is: (I) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.Type: ApplicationFiled: January 21, 2010Publication date: December 22, 2011Applicant: Schering CorporationInventors: Hubert B. Josien, John W. Clader, William J. Greenlee, Michael John Mayer, Jason L. Davis, Shuangyi Wan
-
Publication number: 20110313008Abstract: This invention provides for certain pentafluorosulpholane-containing compounds of the formula or a pharmaceutically acceptable salt, ester, solvate or prodrug thereof, wherein the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.Type: ApplicationFiled: January 21, 2010Publication date: December 22, 2011Applicant: Schering CorporationInventors: Hubert B. Josien, John W. Clader, Andrew Stamford, William J. Greenlee, Michael John Mayer, Jason L. Davis, Ming Min Hsia, Shuangyi Wan
-
Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors
Patent number: 8067621Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substitutents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.Type: GrantFiled: January 18, 2007Date of Patent: November 29, 2011Assignee: Schering CorporationInventors: Theodros Asberom, Thomas A. Bara, Chad E. Bennett, Duane A. Burnett, Mary Ann Caplen, John W. Clader, David J. Cole, Martin S. Domalski, Hubert B. Josien, Chad E. Knutson, Hongmei Li, Mark D. McBriar, Dmitri A. Pissarnitski, Li Qiang, Murali Rajagopalan, Thavalakulamgara K. Sasikumar, Jing Su, Haiqun Tang, Wen-Lian Wu, Ruo Xu, Zhiqiang Zhao -
Publication number: 20110263529Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: November 5, 2009Publication date: October 27, 2011Inventors: Ruo Xu, John W. Clader
-
Publication number: 20110257156Abstract: In its many embodiments, the present invention provides novel heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: November 5, 2009Publication date: October 20, 2011Inventors: Zhaoning Zhu, William J. Greenlee, David James Cole, Dmitri A. Pissarnitski, Gioconda V. Gallo, Hongmei Li, Hubert B. Josien, Jun Qin, Chad E. Knutson, Mihirbaran Mandal, Monica L. Vicarel, Murali Rajagopalan, Pawan Kumar Dhondi, Ruo Xu, Zhong-Yue Sun, Thomas A. Bara, Xianhai Huang, Xiaohong Zhu, Zhiqiang Zhao, John W. Clader, Anandan Palani, Theodros Asberom, Troy McCracken, Chad E. Bennett
-
Publication number: 20110236400Abstract: Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)—O—C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)—O—C(O)-heteroaryl and a basic tertiary amine.Type: ApplicationFiled: July 1, 2008Publication date: September 29, 2011Inventors: Wen-Lian Wu, Thomas A. Bara, Duane A. Burnett, John W. Clader, Martin S. Domalski, Yan Jin, Hubert B. Josien, Hongmei Li, Xian Liang, Dmitri A. Pissarnitski, Thavalakulamgara K. Sasikumar, Jesse K. Wong, Ruo Xu, Zhiqiang Zhao, Paul E. McNamara
-
Patent number: 7998958Abstract: Disclosed are novel gamma secretase inhibitors of the formula: Also disclosed are methods for inhibiting gamma secretase, for treating one or more neurodegenerative diseases, for inhibiting the deposition of beta amyloid protein, and for treating Alzheimer's disease using the compounds of formula (I).Type: GrantFiled: December 8, 2009Date of Patent: August 16, 2011Assignee: Schering CorporationInventors: Hubert B. Josien, John W. Clader, Thomas A. Bara, Ruo Xu, Hongmei Li, Dmitri A. Pissarnitski, Zhiqiang Zhao
-
Publication number: 20110054013Abstract: Disclosed are novel gamma secretase inhibitors of the formula: wherein at least one (e.g., 1-4, 1-3, 1-2, 2 or 1) H is replaced by deuterium. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease.Type: ApplicationFiled: August 26, 2010Publication date: March 3, 2011Inventor: John W. Clader
-
Publication number: 20100256128Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: May 28, 2008Publication date: October 7, 2010Applicant: Schering CorporationInventors: Zhaoning Zhu, William J. Greenlee, Xianhai Huang, Brian A. McKittrick, John W. Clader, Mark D. McBriar, Anandan Palani
-
Patent number: RE42461Abstract: Hydroxy-substituted azetidinone hypocholesterolemic agents of the formula or a pharmaceutically acceptable salt thereof, wherein: Ar1 and Ar2 are aryl or R4-substituted aryl; Ar3 is aryl or R5-substituted aryl; X, Y and Z are —CH2—, —CH(lower alkyl)— or —C(dilower alkyl)—; R and R2 are —OR6, —O(CO)R6, —O(CO)OR9 or —O(CO)NR6R7; R1 and R3 are H or lower alkyl; q is 0 or 1; r is 0 or 1; m, n and p are 0-4; provided that at least one of q and r is 1, and the sum of m, n, p, q and r is 1-6; and provided that when p is O and r is 1, the sum of m, q and n is 1-5; R4 is selected from lower alkyl, R5, —CF3, —CN, —NO2 and halogen R5 is selected from —OR6, —O(CO)R6, —O(CO)OR9, —O(CH2)1-5OR6, —O(CO)NR6R7, —NR6R7, —NR6(CO)R7, —NR6(CO)OR9, —NR6(CO)NR7R8, —NR6SO2R9, —COOR6, —CONR6R7, —COR6, —SO2NR6R7, S(O)0-2R9, —O(CH2)1-10—COOR6, —O(CH2)1-10CON6R7, —(lower alkylene)COOR6 and —CH?CH—COOR6; R6, R7 and R8 are H, lower alkyl or aryl-substituted Ic R9 is lower alkyl, aryl or aryl-substituted lower alkyl; are disclType: GrantFiled: September 14, 1994Date of Patent: June 14, 2011Assignee: Schering CorporationInventors: Stuart B. Rosenblum, Sundeep Dugar, Duane A. Burnett, John W. Clader, Brian A. McKittrick