Patent classifications
C07D239/47
NOVEL PROCESSES FOR PREPARING A DIAMINOPYRIMIDINE DERIVATIVE OR ACID ADDITION SALT THEREOF
The present invention provides a novel process for preparing a diaminopyrimidine derivative or acid addition salt thereof having an activity as a 5-HT.sub.4 receptor agonist. And also, the present invention provides novel crystalline forms of a hydrochloride of the diaminopyrimidine derivative and processes for preparing the same.
Cyclopropanecarboxamido-substituted aromatic compounds as anti-tumor agents
The present disclosure relates to novel cyclopropanecarboxamido-substituted aromatic compounds that inhibit protein kinases and their use in anti-tumor area. In particular, the disclosure relates to novel tyrosine-kinase inhibitors and Raf-kinase inhibitors as anti-tumor agents, their preparation, pharmaceutical composition, and their use in the treatment of cancer.
Cyclopropanecarboxamido-substituted aromatic compounds as anti-tumor agents
The present disclosure relates to novel cyclopropanecarboxamido-substituted aromatic compounds that inhibit protein kinases and their use in anti-tumor area. In particular, the disclosure relates to novel tyrosine-kinase inhibitors and Raf-kinase inhibitors as anti-tumor agents, their preparation, pharmaceutical composition, and their use in the treatment of cancer.
N-(substituted)-5-fluoro-4-imino-3-methyl-2-oxo-3,4-dihydropyrimidine-1(2H)-carboxamide derivatives
This present disclosure is related to the field of to N-(substituted)-5-fluoro-4-imino-3-methyl-2-oxo-3,4-di-hydropyrimidme-1(2H)-carboxamide compounds and their derivatives and to the use of these compounds as fungicides. This application claims the benefit of U.S. Provisional Patent Application Ser. No. 61/746,837 filed Dec. 28, 2012, which is expressly incorporated by reference herein. Background and Summary of the Invention Fungicides are compounds, of natural or synthetic origin, which act to protect and/or cure plants against damage caused by agriculturally relevant fungi. Generally, no single fungicide is useful in all situations. Consequently, research is ongoing to produce fungicides that may have better performance, are easier to use, and cost less.
N-(substituted)-5-fluoro-4-imino-3-methyl-2-oxo-3,4-dihydropyrimidine-1(2H)-carboxamide derivatives
This present disclosure is related to the field of to N-(substituted)-5-fluoro-4-imino-3-methyl-2-oxo-3,4-di-hydropyrimidme-1(2H)-carboxamide compounds and their derivatives and to the use of these compounds as fungicides. This application claims the benefit of U.S. Provisional Patent Application Ser. No. 61/746,837 filed Dec. 28, 2012, which is expressly incorporated by reference herein. Background and Summary of the Invention Fungicides are compounds, of natural or synthetic origin, which act to protect and/or cure plants against damage caused by agriculturally relevant fungi. Generally, no single fungicide is useful in all situations. Consequently, research is ongoing to produce fungicides that may have better performance, are easier to use, and cost less.
5-fluoro-4-imino-3-(alkyl/substituted alkyl)-1-(arylsulfonyl)-3,4-dihydropyrimidin-2(1H)-one and processes for their preparation
Provided herein are 5-fluoro-4-imino-3-(alkyl/substituted alkyl)-1-(arylsulfonyl)3,4-dihydropyrimidin-2(1H)-one and processes for their preparation which may include the use of an alkali alkoxide and an alkylating agent ##STR00001##
5-fluoro-4-imino-3-(alkyl/substituted alkyl)-1-(arylsulfonyl)-3,4-dihydropyrimidin-2(1H)-one and processes for their preparation
Provided herein are 5-fluoro-4-imino-3-(alkyl/substituted alkyl)-1-(arylsulfonyl)3,4-dihydropyrimidin-2(1H)-one and processes for their preparation which may include the use of an alkali alkoxide and an alkylating agent ##STR00001##
INHIBITORS OF LRRK2 KINASE
Compounds having activity as inhibitors of LRRK2 kinase are provided. The compounds have Structure (I):
##STR00001##
or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A, B, R.sup.1a, R.sup.1b, R.sup.2, and L are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of LRRK2 kinase are also provided.
INHIBITORS OF LRRK2 KINASE
Compounds having activity as inhibitors of LRRK2 kinase are provided. The compounds have Structure (I):
##STR00001##
or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A, B, R.sup.1a, R.sup.1b, R.sup.2, and L are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of LRRK2 kinase are also provided.
(TRIFLUOROMETHYL)PYRIMIDINE-2-AMINE COMPOUNDS
The present invention provides a compound of Formula I:
##STR00001## wherein R.sup.1 is hydrogen or methyl; and R.sup.2 is:
##STR00002##
or a pharmaceutically acceptable salt thereof, useful for treating pain, including chronic pain, chronic lower back pain, diabetic peripheral neuropathic pain, and osteoarthritis pain.