-transparent.png){kind=logo}
Sulfonamidolactam inhibitors of coagulation factor Xa. 2008
Joanne M Smallheer, and
Shuaige Wang, and
Mia L Laws, and
Suanne Nakajima, and
Zilun Hu, and
Wei Han, and
Irina Jacobson, and
Joseph M Luettgen, and
Karen A Rossi, and
Alan R Rendina, and
Robert M Knabb, and
Ruth R Wexler, and
Patrick Y S Lam, and
Mimi L Quan
Bristol-Myers Squibb Company, Cardiovascular Diseases Chemistry, PO Box 5400, Princeton, NJ 08543-5400, USA. joanne.smallheer@bms.com
As part of an effort to identify novel backups for previously reported pyrazole-based coagulation Factor Xa inhibitors, the pyrazole 5-carboxamide moiety was replaced by 3-(sulfonylamino)-2-piperidone. This led to the identification of a structurally diverse chemotype that was further optimized to incorporate neutral or weakly basic aryl and heteroaryl P1 groups while maintaining good potency versus Factor Xa. Substitution at the sulfonamide nitrogen provided further improvements in potency and as did introduction of alternate P4 moieties.
Related Publications
Joanne M Smallheer, and
Shuaige Wang, and
Mia L Laws, and
Suanne Nakajima, and
Zilun Hu, and
Wei Han, and
Irina Jacobson, and
Joseph M Luettgen, and
Karen A Rossi, and
Alan R Rendina, and
Robert M Knabb, and
Ruth R Wexler, and
Patrick Y S Lam, and
Mimi L Quan
May 1999,
Expert opinion on investigational drugs,
Joanne M Smallheer, and
Shuaige Wang, and
Mia L Laws, and
Suanne Nakajima, and
Zilun Hu, and
Wei Han, and
Irina Jacobson, and
Joseph M Luettgen, and
Karen A Rossi, and
Alan R Rendina, and
Robert M Knabb, and
Ruth R Wexler, and
Patrick Y S Lam, and
Mimi L Quan
August 2007,
Bioorganic & medicinal chemistry letters,
Joanne M Smallheer, and
Shuaige Wang, and
Mia L Laws, and
Suanne Nakajima, and
Zilun Hu, and
Wei Han, and
Irina Jacobson, and
Joseph M Luettgen, and
Karen A Rossi, and
Alan R Rendina, and
Robert M Knabb, and
Ruth R Wexler, and
Patrick Y S Lam, and
Mimi L Quan
April 2010,
Thrombosis and haemostasis,
Joanne M Smallheer, and
Shuaige Wang, and
Mia L Laws, and
Suanne Nakajima, and
Zilun Hu, and
Wei Han, and
Irina Jacobson, and
Joseph M Luettgen, and
Karen A Rossi, and
Alan R Rendina, and
Robert M Knabb, and
Ruth R Wexler, and
Patrick Y S Lam, and
Mimi L Quan
June 2001,
Current topics in medicinal chemistry,
Joanne M Smallheer, and
Shuaige Wang, and
Mia L Laws, and
Suanne Nakajima, and
Zilun Hu, and
Wei Han, and
Irina Jacobson, and
Joseph M Luettgen, and
Karen A Rossi, and
Alan R Rendina, and
Robert M Knabb, and
Ruth R Wexler, and
Patrick Y S Lam, and
Mimi L Quan
December 2004,
Bioorganic & medicinal chemistry letters,
Joanne M Smallheer, and
Shuaige Wang, and
Mia L Laws, and
Suanne Nakajima, and
Zilun Hu, and
Wei Han, and
Irina Jacobson, and
Joseph M Luettgen, and
Karen A Rossi, and
Alan R Rendina, and
Robert M Knabb, and
Ruth R Wexler, and
Patrick Y S Lam, and
Mimi L Quan
January 2004,
Methods in molecular medicine,
Joanne M Smallheer, and
Shuaige Wang, and
Mia L Laws, and
Suanne Nakajima, and
Zilun Hu, and
Wei Han, and
Irina Jacobson, and
Joseph M Luettgen, and
Karen A Rossi, and
Alan R Rendina, and
Robert M Knabb, and
Ruth R Wexler, and
Patrick Y S Lam, and
Mimi L Quan
May 2024,
Journal of thrombosis and haemostasis : JTH,
Joanne M Smallheer, and
Shuaige Wang, and
Mia L Laws, and
Suanne Nakajima, and
Zilun Hu, and
Wei Han, and
Irina Jacobson, and
Joseph M Luettgen, and
Karen A Rossi, and
Alan R Rendina, and
Robert M Knabb, and
Ruth R Wexler, and
Patrick Y S Lam, and
Mimi L Quan
July 2004,
Bioorganic & medicinal chemistry letters,
Joanne M Smallheer, and
Shuaige Wang, and
Mia L Laws, and
Suanne Nakajima, and
Zilun Hu, and
Wei Han, and
Irina Jacobson, and
Joseph M Luettgen, and
Karen A Rossi, and
Alan R Rendina, and
Robert M Knabb, and
Ruth R Wexler, and
Patrick Y S Lam, and
Mimi L Quan
February 2011,
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences,
Joanne M Smallheer, and
Shuaige Wang, and
Mia L Laws, and
Suanne Nakajima, and
Zilun Hu, and
Wei Han, and
Irina Jacobson, and
Joseph M Luettgen, and
Karen A Rossi, and
Alan R Rendina, and
Robert M Knabb, and
Ruth R Wexler, and
Patrick Y S Lam, and
Mimi L Quan
September 2019,
Expert opinion on drug discovery,
