Patent classifications
C07C307/06
N-substituted benzamides and methods of use thereof
The invention provides novel compounds having the general formula (I) and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X.sup.2, L, subscript m, X.sup.1, ring D, R.sup.1, and R.sup.N have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions. ##STR00001##
N-substituted benzamides and methods of use thereof
The invention provides novel compounds having the general formula (I) and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X.sup.2, L, subscript m, X.sup.1, ring D, R.sup.1, and R.sup.N have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions. ##STR00001##
PROCESS FOR THE SYNTHESIS OF AN INDOLEAMINE 2,3-DIOXYGENASE INHIBITOR
The present application is directed to processes and intermediates for making 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N-hydroxy-1,2,5-oxadiazole-3-carboximidamide, which is an inhibitor of indoleamine 2,3-dioxygenase, useful in the treatment of cancer and other disorders.
PROCESS FOR THE SYNTHESIS OF AN INDOLEAMINE 2,3-DIOXYGENASE INHIBITOR
The present application is directed to processes and intermediates for making 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N-hydroxy-1,2,5-oxadiazole-3-carboximidamide, which is an inhibitor of indoleamine 2,3-dioxygenase, useful in the treatment of cancer and other disorders.
METHOD FOR MAKING N-(FLUOROSULFONYL) DIMETHYLAMINE
Dimethylamine (Me.sub.2NH) is reacted with sulfuryl fluoride (SO.sub.2F.sub.2) to form at least a first phase comprising N-(fluoro sulfonyl) dimethylamine (FSO.sub.2NMe.sub.2), tetramethylsulfamide (SO.sub.2(NMe.sub.2).sub.2), or a combination thereof. A second phase, which may include dimethylamine hydrofluoride (Me.sub.2NH.sub.2F), may be also formed and separated from the first phase. FSO.sub.2NMe.sub.2 or SO.sub.2(NMe.sub.2).sub.2 is then isolated from the first phase. For example, the first phase may be a liquid phase, and FSO.sub.2NMe.sub.2 and SO.sub.2(NMe.sub.2).sub.2 are separated by distillation, optionally under reduced pressure.
METHOD FOR MAKING N-(FLUOROSULFONYL) DIMETHYLAMINE
Dimethylamine (Me.sub.2NH) is reacted with sulfuryl fluoride (SO.sub.2F.sub.2) to form at least a first phase comprising N-(fluoro sulfonyl) dimethylamine (FSO.sub.2NMe.sub.2), tetramethylsulfamide (SO.sub.2(NMe.sub.2).sub.2), or a combination thereof. A second phase, which may include dimethylamine hydrofluoride (Me.sub.2NH.sub.2F), may be also formed and separated from the first phase. FSO.sub.2NMe.sub.2 or SO.sub.2(NMe.sub.2).sub.2 is then isolated from the first phase. For example, the first phase may be a liquid phase, and FSO.sub.2NMe.sub.2 and SO.sub.2(NMe.sub.2).sub.2 are separated by distillation, optionally under reduced pressure.
HERBICIDAL MALONAMIDES
The present invention relates to malonamide compounds of the formula (I) where the variables are as defined in the claims and the description, and to compositions comprising these compounds. The invention also relates to the use of said malonamide compounds or the corresponding compositions for controlling unwanted vegetation, and to methods of applying the malonamide compounds or the corresponding compositions.
##STR00001##
HERBICIDAL MALONAMIDES
The present invention relates to malonamide compounds of the formula (I) where the variables are as defined in the claims and the description, and to compositions comprising these compounds. The invention also relates to the use of said malonamide compounds or the corresponding compositions for controlling unwanted vegetation, and to methods of applying the malonamide compounds or the corresponding compositions.
##STR00001##
INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
- John A. Bender ,
- Robert G. Gentles ,
- Annapurna PENDRI ,
- Alan Xiangdong Wang ,
- Nicholas A. MEANWELL ,
- Brett R. Beno ,
- Robert A. Fridell ,
- Makonen Belema ,
- Van N. Nguyen ,
- Zhong Yang ,
- Gan Wang ,
- Selvakumar Kumaravel ,
- Srinivasan Thangathirupathy ,
- Rajesh Onkardas Bora ,
- Shilpa Maheshwarappa Holehatti ,
- Mallikarjuna Rao Mettu ,
- Manoranjan Panda
Compounds of Formula I, including pharmaceutically acceptable salts thereof, and compositions and methods for treating human immunodeficiency virus (HIV) infection are set forth:
##STR00001##
INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
- John A. Bender ,
- Robert G. Gentles ,
- Annapurna PENDRI ,
- Alan Xiangdong Wang ,
- Nicholas A. MEANWELL ,
- Brett R. Beno ,
- Robert A. Fridell ,
- Makonen Belema ,
- Van N. Nguyen ,
- Zhong Yang ,
- Gan Wang ,
- Selvakumar Kumaravel ,
- Srinivasan Thangathirupathy ,
- Rajesh Onkardas Bora ,
- Shilpa Maheshwarappa Holehatti ,
- Mallikarjuna Rao Mettu ,
- Manoranjan Panda
Compounds of Formula I, including pharmaceutically acceptable salts thereof, and compositions and methods for treating human immunodeficiency virus (HIV) infection are set forth:
##STR00001##