Patent classifications
C07C271/06
SMALL MOLECULE ANTAGONISTS OF PF4
The present application provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein Y, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are described herein. The methods of using these compounds to inhibit tetramerization of PF4 and to treat the associated diseases and conditions, such as heparin-induced thrombocytopenia and thrombosis (HITT) and vaccine-induced immune thrombotic thrombocytopenia (VITT), methods of making these compounds, and pharmaceutical compositions containing these compounds are also disclosed.
##STR00001##
PI3K-ALPHA INHIBITORS AND METHODS OF USE THEREOF
- Yue PAN ,
- Alessandro BOEZIO ,
- Cary Griffin Fridrich ,
- Elaine B. Krueger ,
- Demetri T. MOUSTAKAS ,
- Kevin David RAYNOR ,
- Kelley C. SHORTSLEEVES ,
- Thomas H. McLean ,
- Michael Paul DENINNO ,
- Christopher Thomson ,
- Alexandre LARIVEE ,
- Andrew J. BURNIE ,
- Bren-Jordan ATIENZA ,
- Christian Perreault ,
- Gaetan MAERTENS ,
- Tarek MOHAMED ,
- Thomas Lepitre ,
- Erich W. Baum ,
- Hakan GUNAYDIN
The present disclosure relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of PI3K enzymes with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with PI3K signaling with the compounds and compositions of the disclosure.
PI3K-ALPHA INHIBITORS AND METHODS OF USE THEREOF
- Yue PAN ,
- Alessandro BOEZIO ,
- Cary Griffin Fridrich ,
- Elaine B. Krueger ,
- Demetri T. MOUSTAKAS ,
- Kevin David RAYNOR ,
- Kelley C. SHORTSLEEVES ,
- Thomas H. McLean ,
- Michael Paul DENINNO ,
- Christopher Thomson ,
- Alexandre LARIVEE ,
- Andrew J. BURNIE ,
- Bren-Jordan ATIENZA ,
- Christian Perreault ,
- Gaetan MAERTENS ,
- Tarek MOHAMED ,
- Thomas Lepitre ,
- Erich W. Baum ,
- Hakan GUNAYDIN
The present disclosure relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of PI3K enzymes with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with PI3K signaling with the compounds and compositions of the disclosure.
Analogs of pterostilbene amino acid bearing carbonates for treating a non-alcoholic fatty liver disease and nonalcoholic steatohepatitis
A series of novel analogs of water soluble pterostilbene amino acid bearing carbonates were synthesized, which show activities in treating a non-alcoholic fatty liver disease and a nonalcoholic steatohepatitis (NASH).
Analogs of pterostilbene amino acid bearing carbonates for treating a non-alcoholic fatty liver disease and nonalcoholic steatohepatitis
A series of novel analogs of water soluble pterostilbene amino acid bearing carbonates were synthesized, which show activities in treating a non-alcoholic fatty liver disease and a nonalcoholic steatohepatitis (NASH).
PI3K-ALPHA INHIBITORS AND METHODS OF USE THEREOF
- Yue PAN ,
- Alessandro BOEZIO ,
- Cary Griffin Fridrich ,
- Elaine B. Krueger ,
- Demetri T. MOUSTAKAS ,
- Kevin David RAYNOR ,
- Kelley C. SHORTSLEEVES ,
- Thomas H. McLean ,
- Michael Paul DENINNO ,
- Christopher Thomson ,
- Alexandre LARIVEE ,
- Andrew J. BURNIE ,
- Bren-Jordan ATIENZA ,
- Christian Perreault ,
- Gaetan MAERTENS ,
- Tarek MOHAMED ,
- Thomas Lepitre ,
- Erich W. Baum ,
- Hakan GUNAYDIN
The present disclosure relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of PI3K enzymes with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with PI3K signaling with the compounds and compositions of the disclosure.
PI3K-ALPHA INHIBITORS AND METHODS OF USE THEREOF
- Yue PAN ,
- Alessandro BOEZIO ,
- Cary Griffin Fridrich ,
- Elaine B. Krueger ,
- Demetri T. MOUSTAKAS ,
- Kevin David RAYNOR ,
- Kelley C. SHORTSLEEVES ,
- Thomas H. McLean ,
- Michael Paul DENINNO ,
- Christopher Thomson ,
- Alexandre LARIVEE ,
- Andrew J. BURNIE ,
- Bren-Jordan ATIENZA ,
- Christian Perreault ,
- Gaetan MAERTENS ,
- Tarek MOHAMED ,
- Thomas Lepitre ,
- Erich W. Baum ,
- Hakan GUNAYDIN
The present disclosure relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of PI3K enzymes with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with PI3K signaling with the compounds and compositions of the disclosure.
PROCESS FOR THE PREPARATION OF FURAZANOBENZIMIDAZOLES AND CRYSTALLINE FORMS THEREOF
The present invention provides processes for preparing a compound of formula I and pharmaceutically acceptable salts thereof,
##STR00001## comprising deprotecting a compound of formula II
##STR00002## wherein each R.sup.3 independently represents a tertiary alkyl group, preferably wherein each R.sup.3 is tertiary butyl. The invention also provides intermediates useful for preparing compounds of formula I and processes for preparing these intermediates. Additionally the invention provides polymorphic forms of the dichloride salt of the compound of formula I and their use in the treatment of proliferative disorders.
PROCESS FOR THE PREPARATION OF FURAZANOBENZIMIDAZOLES AND CRYSTALLINE FORMS THEREOF
The present invention provides processes for preparing a compound of formula I and pharmaceutically acceptable salts thereof,
##STR00001## comprising deprotecting a compound of formula II
##STR00002## wherein each R.sup.3 independently represents a tertiary alkyl group, preferably wherein each R.sup.3 is tertiary butyl. The invention also provides intermediates useful for preparing compounds of formula I and processes for preparing these intermediates. Additionally the invention provides polymorphic forms of the dichloride salt of the compound of formula I and their use in the treatment of proliferative disorders.