Patent classifications
C07D279/06
IDO inhibitors
Presently provided are methods for (a) modulating an activity of indoleamine 2,3-dioxygenase comprising contacting an indoleamine 2,3-dioxygenase with a modulation effective amount of a compound as described in one of the aspects described herein; (b) treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression in a subject in need thereof, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (c) treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (d) enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent and a compound as described in one of the aspects described herein; (e) treating tumor-specific immunosuppression associated with cancer comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; and (f) treating immunosuppression associated with an infectious disease, e.g., HIV-I infection, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount a compound as described in one of the aspects described herein.
IDO inhibitors
Presently provided are methods for (a) modulating an activity of indoleamine 2,3-dioxygenase comprising contacting an indoleamine 2,3-dioxygenase with a modulation effective amount of a compound as described in one of the aspects described herein; (b) treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression in a subject in need thereof, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (c) treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (d) enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent and a compound as described in one of the aspects described herein; (e) treating tumor-specific immunosuppression associated with cancer comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; and (f) treating immunosuppression associated with an infectious disease, e.g., HIV-I infection, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount a compound as described in one of the aspects described herein.
N-ACYL AMINO ACID COMPOUNDS AND METHODS OF USE
The invention relates to compounds of formula (I):
##STR00001##
or a salt thereof, wherein R.sup.1, A, L, and R.sup.2 and n are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are v1 integrin inhibitors that are useful for treating tissue specific fibrosis.
N-ACYL AMINO ACID COMPOUNDS AND METHODS OF USE
The invention relates to compounds of formula (I):
##STR00001##
or a salt thereof, wherein R.sup.1, A, L, and R.sup.2 and n are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are v1 integrin inhibitors that are useful for treating tissue specific fibrosis.
Targeted nitroxide agents
Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.
Targeted nitroxide agents
Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.
Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
The following compound is provided as an agent for treating a disease induced by production, secretion and/or deposition of amyloid protein, for example, a compound represented by the formula (I): ##STR00001## wherein ring A in an optionally substituted carbocyclic group or an optionally substituted heterocyclic group, R.sup.1 is optionally substituted lower alkyl or the like, R.sup.2a and R.sup.2b are each independently hydrogen, optionally substituted lower alkyl or the like, R.sup.3a and R.sup.3c are each independently hydrogen, halogen, hydroxy, optionally substituted lower alkyl or the like,
or a pharmaceutical acceptable salt thereof, or a solvate thereof.
Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
The following compound is provided as an agent for treating a disease induced by production, secretion and/or deposition of amyloid protein, for example, a compound represented by the formula (I): ##STR00001## wherein ring A in an optionally substituted carbocyclic group or an optionally substituted heterocyclic group, R.sup.1 is optionally substituted lower alkyl or the like, R.sup.2a and R.sup.2b are each independently hydrogen, optionally substituted lower alkyl or the like, R.sup.3a and R.sup.3c are each independently hydrogen, halogen, hydroxy, optionally substituted lower alkyl or the like,
or a pharmaceutical acceptable salt thereof, or a solvate thereof.
N-arylamidine-substituted trifluoroethyl sulfide derivatives as acaricides and insecticides
The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) ##STR00001## in which X.sup.1, X.sup.2, X.sup.3, X.sup.4, R.sup.1, R.sup.2, R.sup.3, n have the meanings given in the descriptionto their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation.
N-arylamidine-substituted trifluoroethyl sulfide derivatives as acaricides and insecticides
The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) ##STR00001## in which X.sup.1, X.sup.2, X.sup.3, X.sup.4, R.sup.1, R.sup.2, R.sup.3, n have the meanings given in the descriptionto their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation.