Patent classifications
A61K31/5355
Small molecule inhibitors of lactate dehydrogenase and methods of use thereof
- David J. Maloney ,
- Alex Gregory Waterson ,
- Ganesh Rai Bantukallu ,
- Kyle Ryan Brimacombe ,
- Plamen Christov ,
- Chi V. Dang ,
- Victor Darley-Usmar ,
- Xin Hu ,
- Ajit Jadhav ,
- Somnath Jana ,
- Kwangho Kim ,
- Jennifer L. Kouznetsova ,
- William J. Moore ,
- Bryan T. Mott ,
- Leonard M. Neckers ,
- Anton Simeonov ,
- Gary Allen Sulikowski ,
- Daniel Jason Urban ,
- Shyh Ming Yang
Provided is a compound of formula (I), ##STR00001##
in which Ar.sup.1, R.sup.1, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.
Small molecule inhibitors of lactate dehydrogenase and methods of use thereof
- David J. Maloney ,
- Alex Gregory Waterson ,
- Ganesh Rai Bantukallu ,
- Kyle Ryan Brimacombe ,
- Plamen Christov ,
- Chi V. Dang ,
- Victor Darley-Usmar ,
- Xin Hu ,
- Ajit Jadhav ,
- Somnath Jana ,
- Kwangho Kim ,
- Jennifer L. Kouznetsova ,
- William J. Moore ,
- Bryan T. Mott ,
- Leonard M. Neckers ,
- Anton Simeonov ,
- Gary Allen Sulikowski ,
- Daniel Jason Urban ,
- Shyh Ming Yang
Provided is a compound of formula (I), ##STR00001##
in which Ar.sup.1, R.sup.1, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.
COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
Disclosed are compounds of Formula I(b):
##STR00001##
or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Ring A, Ring HD, J, each T, R.sup.3, R.sup.4, R.sup.5, each R.sup.7, and m are as described in any of the embodiments described in this disclosure; compositions thereof; and uses thereof.
COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
Disclosed are compounds of Formula I(b):
##STR00001##
or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Ring A, Ring HD, J, each T, R.sup.3, R.sup.4, R.sup.5, each R.sup.7, and m are as described in any of the embodiments described in this disclosure; compositions thereof; and uses thereof.
TREATMENT OF LUPUS NEPHRITIS USING LAQUINIMOD
This invention provides a method of treating a subject afflicted with active lupus nephritis comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to treat the subject. This invention also provides laquinimod or pharmaceutically acceptable salt thereof for use in treating a subject afflicted with active lupus nephritis. This invention further provides a pharmaceutical composition comprising an amount of laquinimod or pharmaceutically acceptable salt thereof for use in treating a subject afflicted with active lupus nephritis.
TREATMENT OF LUPUS NEPHRITIS USING LAQUINIMOD
This invention provides a method of treating a subject afflicted with active lupus nephritis comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to treat the subject. This invention also provides laquinimod or pharmaceutically acceptable salt thereof for use in treating a subject afflicted with active lupus nephritis. This invention further provides a pharmaceutical composition comprising an amount of laquinimod or pharmaceutically acceptable salt thereof for use in treating a subject afflicted with active lupus nephritis.
LOW-DOSE BRIMONIDINE COMBINATIONS AND USES THEREOF
The present invention is directed to compositions containing low-dose brimonidine and either a second glaucoma drug, an anti-histamine or non-steroidal anti-inflammatory drug. The present invention is further directed to methods of treating glaucoma or allergies or reducing inflammation by administering compositions of the present invention.
LOW-DOSE BRIMONIDINE COMBINATIONS AND USES THEREOF
The present invention is directed to compositions containing low-dose brimonidine and either a second glaucoma drug, an anti-histamine or non-steroidal anti-inflammatory drug. The present invention is further directed to methods of treating glaucoma or allergies or reducing inflammation by administering compositions of the present invention.
NOVEL COMPOUNDS AS MODULATORS OF PROTEIN KINASES
The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
NOVEL COMPOUNDS AS MODULATORS OF PROTEIN KINASES
The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.