Patent classifications
C07D498/06
Biologically active macrolides, compositions, and uses thereof
The present invention provides a compound of the formula (I) or (II), wherein R.sup.1 is H, alkyl, alkenyl or aryl, R.sup.2 is H, alkyl or aryl, R.sup.3 is H, a alkyl, alkenyl or aryl, R.sup.4 and R.sup.4-R.sup.8 are independently R.sup.10, C(O)R.sup.10 or SO.sub.2R.sup.10, wherein R.sup.10 is H, alkyl, alkenyl or aryl, and R.sup.9 is R.sup.9a, C(O)R.sup.9a or SO.sub.2R.sup.9a, wherein R.sup.9a is H, alkyl, alkenyl or aryl. R.sup.9a can be unsubstituted or substituted with one or more oxo(═O), OR.sup.9b, OC(O)R.sup.9b, OSO.sub.2R.sup.9b, NHR.sup.9b, NHC(O)R.sup.9b and NHSO.sub.2R.sup.9b groups. R.sup.9b is H, alkyl, alkenyl, or aryl. R.sup.9b can be unsubstituted or substituted with one or more groups such as oxo(═O), OR.sup.9c, CO.sub.2R.sup.9c, CO.sub.2R.sup.9c and OC(O)R.sup.9c. R.sup.9c is H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent. The present invention further provides a method of treating a condition treatable by the inhibition of vacuolar-type (H+)-ATPase and a method of treating cancer. ##STR00001##
Granzyme B directed imaging and therapy
Provided herein are heterocyclic compounds useful for imaging Granzyme B. Methods of imaging Granzyme B, combination therapies, and kits comprising the Granzyme B imaging agents are also provided.
Granzyme B directed imaging and therapy
Provided herein are heterocyclic compounds useful for imaging Granzyme B. Methods of imaging Granzyme B, combination therapies, and kits comprising the Granzyme B imaging agents are also provided.
Macrocycles as factor XIa inhibitors
The present invention provides compounds of Formula (I): ##STR00001##
or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
Macrocycles as factor XIa inhibitors
The present invention provides compounds of Formula (I): ##STR00001##
or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
Compositions of protein receptor tyrosine kinase inhibitors
The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.
Compositions of protein receptor tyrosine kinase inhibitors
The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.
INHIBITORS OF HIF PROLYL HYDROXYLASE
The present invention concerns compounds of formula I or pharmaceutically acceptable salts thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
##STR00001##
INHIBITORS OF HIF PROLYL HYDROXYLASE
The present invention concerns compounds of formula I or pharmaceutically acceptable salts thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
##STR00001##
LIGHT EMITTING DEVICE AND POLYCYCLIC COMPOUND FOR THE SAME
A light emitting device of an embodiment includes a first electrode, a second electrode disposed on the first electrode, and at least one functional layer disposed between the first electrode and the second electrode. The at least one functional layer includes a polycyclic compound represented by Formula 1, thereby showing high emission efficiency properties and improved life characteristics.
##STR00001##