Patents by Inventor Thomas J. Greshock
Thomas J. Greshock 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).
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Publication number: 20180071412Abstract: The present invention is directed to pyrrolopyridine compounds of formula (I) or their pharmaceutically acceptable salts, which may be suitable for imaging tau aggregates, b-sheet aggregates, beta-amyloid aggregates or alpha-synuclein aggregates, and hence are useful in binding and imaging tau aggregates in Alzheimer's patients. More specifically, this invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study tau deposits in brain in vivo to allow diagnosis of Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology. The invention further relates to a method of measuring clinical efficacy of therapeutic agents for Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology.Type: ApplicationFiled: October 4, 2017Publication date: March 15, 2018Applicant: Merck Sharp & Dohme Corp.Inventors: Abbas M. Walji, Eric Hostetler, Thomas J. Greshock, Jing Li, Keith P. Moore, Idriss Bennacef, James Mulhearn, Harold Selnick, Yaode Wang, Kun Yang, Jianmin Fu
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Publication number: 20180030007Abstract: The present disclosure relates to compounds of formula I that are useful as modulators of ?7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammationType: ApplicationFiled: October 9, 2017Publication date: February 1, 2018Applicant: Merck Sharp & Dohme Corp.Inventors: Brendan M. Crowley, Brian T. Campbell, Joseph L. Duffy, Thomas J. Greshock, Deodial G. Guiadeen, Andrew John Harvey, Belinda C. Huff, Kenneth J. Leavitt, Vanessa L. Rada, John M. Sanders, William D. Shipe, Linda M. Suen, Ian M. Bell
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Patent number: 9840481Abstract: The present disclosure relates to compounds of formula I that are useful as modulators of ?7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammationType: GrantFiled: March 20, 2017Date of Patent: December 12, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Brendan M. Crowley, Brian T. Campbell, Joseph L. Duffy, Thomas J. Greshock, Deodial G. Guiadeen, Andrew John Harvey, Belinda C. Huff, Kenneth J. Leavitt, Vanessa L. Rada, John M. Sanders, William D. Shipe, Linda M. Suen, Ian M. Bell
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Patent number: 9834526Abstract: The present invention is directed to 2,5,6-substituted morpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: December 17, 2014Date of Patent: December 5, 2017Assignees: MERCK SHARP & DOHME CORP., MERCK CANADA INC.Inventors: John A. McCauley, Christian Beaulieu, David Jonathan Bennett, Christopher J. Bungard, Sheldon Crane, Thomas J. Greshock, Katharine M. Holloway, Daniel McKay, Carmela Molinaro, Oscar Miguel Moradei, Satyanarayana Tummanapalli, Vouy Linh Truong, Peter D. Williams
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Patent number: 9808542Abstract: The present invention is directed to pyrrolopyridine compounds of formula (I) or their pharmaceutically acceptable salts, which may be suitable for imaging tau aggregates, b-sheet aggregates, beta-amyloid aggregates or alpha-synuclein aggregates, and hence are useful in binding and imaging tau aggregates in Alzheimer's patients. More specifically, this invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study tau deposits in brain in vivo to allow diagnosis of Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology. The invention further relates to a method of measuring clinical efficacy of therapeutic agents for Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology.Type: GrantFiled: June 9, 2015Date of Patent: November 7, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Abbas W. Walji, Eric Hostetler, Thomas J. Greshock, Jing Li, Keith P. Moore, Idriss Bennacef, James Mulhearn, Harold Selnick, Yaode Wang, Kun Yang, Jianmin Fu
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Publication number: 20170275260Abstract: The present disclosure relates to compounds of formula I that are useful as modulators of ?7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammationType: ApplicationFiled: March 20, 2017Publication date: September 28, 2017Applicant: MERCK SHARP & DOHME CORP.Inventors: BRENDAN M. CROWLEY, BRIAN T. CAMPBELL, JOSEPH L. DUFFY, THOMAS J. GRESHOCK, DEODIAL G. GUIADEEN, ANDREW JOHN HARVEY, BELINDA C. HUFF, KENNETH J. LEAVITT, VANESSA L. RADA, JOHN M. SANDERS, WILLIAM D. SHIPE, LINDA M. SUEN, IAN M. BELL
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Patent number: 9737545Abstract: The present invention is directed to 5-heteroarylmorpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: December 17, 2014Date of Patent: August 22, 2017Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.Inventors: John A. McCauley, Christian Beaulieu, David Jonathan Bennett, Christopher J. Bungard, Sheldon Crane, Thomas J. Greshock, Katharine M. Holloway, Helen Juteau, Daniel McKay, Carmela Molinaro, Oscar Miguel Moradei, Christian Nadeau, Daniel Simard, Satyanarayana Tummanapalli, Vouy Linh Truong, Karine M. Villeneuve, Peter D. Williams
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Publication number: 20170217986Abstract: The present invention is directed to 2,6-morpholine derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein Z1, Z2, V1, V2, V3, R6, R6A, and X are defined herein. The invention also relates to methods of using the 2,6-morpholine derivatives of the invention for the inhibition of HV protease, the inhibition of HV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: March 2, 2015Publication date: August 3, 2017Applicants: Merck Sharp & Dohme Corp., Merck Canada Inc.Inventors: John A. McCauley, David Jonathan Bennett, Christopher J. Bungard, Thomas J. Greshock, M. Katharine Holloway, Peter D. Williams, Christian Beaulieu, Sheldon Crane, Stephanie Lessard, Daniel Mckay, Carmela Molinaro, Oscar Miguel Moradei, Vijayasaradhi Sivalenka, Vouy Linh Truong, Satyanarayana Tummanapalli
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Patent number: 9718818Abstract: The present invention is directed to azaindazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.Type: GrantFiled: August 18, 2014Date of Patent: August 1, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Duane DeMong, Thomas J. Greshock, Ronald K. Chang, Xing Dai, Hong Liu, John A. McCauley, Wei Li, Kallol Basu, Jack D. Scott, Michael Miller
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Patent number: 9708273Abstract: The present invention is directed to benzoquinazilinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: August 17, 2015Date of Patent: July 18, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Douglas C. Beshore, Christina Ng DiMarco, Thomas J. Greshock
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Publication number: 20170174674Abstract: Disclosed are compounds of Formula A, or a salt thereof: wherein R1, R2, and E are defined herein, which compounds have properties for inhibiting Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain disorders, cough, and itch using the same.Type: ApplicationFiled: December 14, 2016Publication date: June 22, 2017Applicant: Merck Sharp & Dohme Corp.Inventors: Thomas J. Greshock, James Mulhearn, Junying Zheng, Ronald M. Kim, Ting Zhang, Anthony J. Roecker, Walter Won, Philippe Nantermet, Rajan Anand, Gang Zhou, Deping Wang, Liangqin Guo
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Publication number: 20170119912Abstract: The present invention is directed to pyrrolopyridine compounds of formula (I) or their pharmaceutically acceptable salts, which may be suitable for imaging tau aggregates, b-sheet aggregates, beta-amyloid aggregates or alpha-synuclein aggregates, and hence are useful in binding and imaging tau aggregates in Alzheimer's patients. More specifically, this invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study tau deposits in brain in vivo to allow diagnosis of Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology. The invention further relates to a method of measuring clinical efficacy of therapeutic agents for Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology.Type: ApplicationFiled: June 9, 2015Publication date: May 4, 2017Applicant: Merck Sharp & Dohme Corp.Inventors: Abbas W. Walji, Eric Hostetler, Thomas J. Greshock, Jing Li, Keith P. Moore, Idriss Bennacef, James Mulhearn, Harold Selnick, Yaode Wang, Kun Yang, Jianmin Fu
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Publication number: 20160311786Abstract: The present invention is directed to 2,5,6-substituted morpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: December 17, 2014Publication date: October 27, 2016Applicants: MERCK SHARP & DOHME CORP., MERCK CANADA INC.Inventors: John A. McCauley, Christian Beaulieu, David Jonathan Bennett, Christopher J. Bungard, Sheldon Crane, Thomas J. Greshock, Katharine M. Holloway, Daniel McKay, Carmela Molinaro, Oscar Miguel Moradei, Satyanarayana Tummanapalli, Vouy Linh Truong, Peter D. Williams
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Publication number: 20160296527Abstract: The present invention is directed to 5-heteroarylmorpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: December 17, 2014Publication date: October 13, 2016Applicants: MERCK SHARP & DOHME CORP., MERCK CANADA INC.Inventors: John A. McCauley, Christian Beaulieu, David Jonathan Bennett, Christopher J. Bungard, Sheldon Crane, Thomas J. Greshock, Katharine M. Holloway, Helen Juteau, Daniel McKay, Carmela Molinaro, Oscar Miguel Moradei, Christian Nadeau, Daniel Simard, Satyanarayana Tummanapalli, Vouy Linh Truong, Karine M. Villeneuve, Peter D. Williams
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Publication number: 20160229813Abstract: The present invention is directed to benzoquinazilinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: August 17, 2015Publication date: August 11, 2016Applicant: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Douglas C. Beshore, Christina Ng Di Marco, Thomas J. Greshock
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Publication number: 20160200722Abstract: The present invention is directed to azaindazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.Type: ApplicationFiled: August 18, 2014Publication date: July 14, 2016Applicant: Merck Sharp & Dohme Corp.Inventors: Duane DeMong, Thomas J. Greshock, Ronald K. Chang, Xing Dai, Hong Liu, John A. McCauley, Wei Li, Kallol Basu, Jack D. Scott, Michael Miller
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Patent number: 9315475Abstract: The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: September 9, 2013Date of Patent: April 19, 2016Assignees: MERCK SHARP & DOHME CORP., MERCK CANADA INC.Inventors: Christian Beaulieu, David J. Bennett, Christopher J. Bungard, Ronald K. Chang, Sheldon Crane, Thomas J. Greshock, Li Hao, Kate Holloway, Jesse J. Manikowski, John A. McCauley, Daniel McKay, Carmela Molinaro, Oscar Miguel Moradei, Philippe G. Nantermet, Christian Nadeau, Satyanarayana Tummanapalli, William Shipe, Sanjay Kumar Singh, Vouy Linh Truong, Sivalenka Vijayasaradhi, Peter D. Williams, Catherine M. Wiscount
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Patent number: 9284312Abstract: The present invention is directed to N-methyl tetrahydroquinoline compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: May 11, 2012Date of Patent: March 15, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Christina Ng DiMarco, Thomas J. Greshock
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Patent number: 9260418Abstract: The present invention is directed to pyranyl aryl methyl benzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: August 27, 2014Date of Patent: February 16, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Ronald K. Chang, Thomas J. Greshock
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Patent number: 9233977Abstract: Disclosed are compounds of Formula (I): and the pharmaceutically acceptable salts thereof, wherein “A” is S—; —SO—, —SO2—, —O— or NRac—, wherein Rac is H, or C1-20 alkyl and R1 through R5 are defined herein. Also disclosed are pharmaceutical formulations comprising a compound of Formula I and methods of treating, managing, or ameliorating diseases amenable to treatment, management, or amelioration by inhibition of LRRK2 kinase activity, for example, Parkinson's disease.Type: GrantFiled: October 25, 2011Date of Patent: January 12, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: John A. McCauley, Hemaka A. Rajapakse, Thomas J. Greshock, John Sanders, Boyoung Kim, Vanessa L. Rada, Jonathan T. Kern, Heather H. Stevenson, Mark T. Bilodeau