Abstract: This invention provides a buffered solution comprising acadesine, as well as compositions, formulations and kits containing said solution. The solution, compositions, formulation, and kits can be used to prevent morbidity/mortality in a patient or to treat an ischaemic condition, a condition regulated by adenosine, or a condition associated with reduced blood flow to a tissue in a patient.
Type:
Application
Filed:
December 15, 2014
Publication date:
April 9, 2015
Applicant:
MERCK SHARP & DOHME CORP.
Inventors:
Valentyn Antochshuk, Mohammed Shameem, Amadeep Singh Bhupender BHALLA
Abstract: The present invention is directed to pyridine derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved.
Type:
Application
Filed:
May 3, 2013
Publication date:
April 9, 2015
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Ian M. Bell, Mark Fraley, Tesfaye Biftu, Cheng Zhu, Anilkumar Nair
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 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.
Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring) cyclopropyl ring. Also disclosed are methods of treating cancer using the compounds of formula (1).
Type:
Grant
Filed:
October 24, 2011
Date of Patent:
April 7, 2015
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Sobhana Babu Boga, Joseph M. Kelly, Hugh Y. Zhu, Abdul-Basit Alhassan, Xin Yao, Xiaolei Gao, James J-S Wang, Jagdish A. Desai, Subrahmanyam Gudipati, Sie-Mun Lo, Liang Zhu, Alan B. Cooper, Yongqi Deng, Gerald W. Shipps, 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:
Grant
Filed:
October 22, 2012
Date of Patent:
April 7, 2015
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Haifeng Tang, Barbara Pio, Nardos Teumelsan, Alexander Pasternak, Reynalda DeJesus
Abstract: The present invention provides a compound of the Formula I: (Formular I should be inserted here) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2 and R3 are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
Type:
Grant
Filed:
June 22, 2011
Date of Patent:
April 7, 2015
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Yongqi Deng, Liang Zhu, Gerald W. Shipps, Jr., Sie-Mun Lo, Binyuan Sun, Xiaohua Huang, Corey Bienstock, Alan B. Cooper, Xiaolei Gao, Xin Yao, Hugh Y. Zhu, Joseph M. Kelly, Sobhana Babu Boga, Abdul-Basit Alhassan, Jayaram R. Tagat, Umar Faruk Mansoor, Kevin J. Wilson, Brendan M. O'Boyle, Matthew Hersh Daniels, Adam Schell, Phieng Siliphaivanh, Christian Fischer
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:
Grant
Filed:
October 22, 2012
Date of Patent:
April 7, 2015
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Haifeng Tang, Barbara Pio, Harry R. Chobanian
Abstract: The invention relates to a N-piperidin-4-yl derivative having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same and to the use of said N-piperidin-4-yl derivatives for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, or for the treatment of uterine fibroids or other menstrual-related disorders.
Type:
Grant
Filed:
September 14, 2012
Date of Patent:
March 31, 2015
Assignee:
Merck Sharp & Dohme B.V.
Inventors:
Ines Huisman, Marcelis Van Der Stelt, Wouter Wiedenhof, Charles Anthony Graham Baker-Glenn, Wesley Peter Blackaby, Naimisha Trivedi
Abstract: Compounds of formula I: wherein variables A1, A2, B, m, n, J, R4, G1, G2, G3 and Y are as described herein, which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.
Type:
Grant
Filed:
June 2, 2008
Date of Patent:
March 31, 2015
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Ian Bell, Harold Selnick, C. Blair Zartman
Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. 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 metabotropic glutamate receptors are involved, such as schizophrenia.
Type:
Grant
Filed:
August 5, 2011
Date of Patent:
March 31, 2015
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero
Abstract: The instant invention provides compounds of formula I which are JAK3 inhibitors. Specifically, the compounds of formula I are pyrrolo[2,3-d]pyrimidine derivative compounds. The instant invention also provides methods of treating JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer, by administering the pyrrolo[2,3-d]pyrimidine-derivative compounds of formula I.
Type:
Grant
Filed:
November 30, 2012
Date of Patent:
March 31, 2015
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Sean P. Ahearn, Matthew Christopher, Christopher Dinsmore, Joon Jung, Qinglin Pu, Alexey Rivkin, Mark E. Scott, David J. Witter, Hyun Chong Woo, Brandon Cash
Abstract: The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are useful in the treatment of certain disorders, including overactive bladder, urinary incontinence, and urinary urgency.
Type:
Application
Filed:
October 22, 2012
Publication date:
March 26, 2015
Applicant:
MERCK SHARP & DOHME, CORP.
Inventors:
John Y.L. Chung, Kevin Campos, Edward Cleator, Robert F. Dunn, Andrew Gibson, R. Scott Hoerrner, Stephen Keen, Dave Liebermann, Zhuqing Liu, Joseph Lynch, Kevine M. Maloney, Feng Xu, Nobuyoshi Yasuda, Naoki Yoshikawa, Yong-Li Zhong
Abstract: The present invention relates to hepatitis C virus (HCV) NS3 protease inhibitors containing a spirocyclic moeity, uses of such compounds, and synthesis of such compounds.
Type:
Grant
Filed:
August 6, 2013
Date of Patent:
March 24, 2015
Assignees:
Merck Sharp & Dohme Corp., Merck Canada Inc.
Inventors:
Thomas Bara, Sathesh Bhat, Dipshikha Biswas, Linda Brockunier, Duane A. Burnett, Samuel Chackalamannil, Mariappan V. Chelliah, Austin Chen, Martin Clasby, Vince J. Colandrea, Zhuyan Guo, Yongxin Han, Charles Jayne, Hubert Josien, Karen Marcantonio, Shouwu Miao, Santhosh Neelamkavil, Patrick Pinto, Murali Rajagopalan, Unmesh Shah, Francisco Velazquez, Srikanth Venkatraman, Yan Xia
Abstract: The invention provides certain 3-pyridyl carboxamide-containing compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
Type:
Grant
Filed:
October 1, 2012
Date of Patent:
March 24, 2015
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Michael D. Altman, Kaleen Konrad Childers, Anthony Donofrio, John Michael Ellis, Sandra Lee Knowles, Alan B. Northrup
Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt or a solvate thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
Inventors:
Samuel Chackalamannil, Tin-Yau Chan, Mariappan V. Chelliah, Martin C. Clasby, Michael Dwyer, William J. Greenlee, Tomokazu Hirabayashi, Santhosh Neelamkavil, Hidemitsu Nishida, Fumihiko Saitoh, Unmesh Shah, Yan Xia
Abstract: The present invention provides a compound of Formula (1): as described herein or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
Type:
Grant
Filed:
October 23, 2012
Date of Patent:
March 24, 2015
Assignee:
Merck Sharp & Dohme Corp
Inventors:
Latha G. Nair, Stephane L. Bogen, Ronald J. Doll, Yao Ma, Yuan Tian
Abstract: The present invention is directed to heterocycle amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. 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 T-type calcium channels are involved.
Type:
Grant
Filed:
October 25, 2010
Date of Patent:
March 24, 2015
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
James Barrow, Kelly-Ann Schlegel, Yoheng Shu, Zhi-Qiang Yang