- LPXH TARGETING COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF MAKING AND USING THE SAME
-
LpxH targeting compounds, compositions thereof, as well as methods for for making and using the same are disclosed herein. The LpxH target compounds typically have a structure pursuant to Formula (I) and/or a salt thereof, wherein Rb is selecte
- -
-
-
- Synthesis and evaluation of sulfonyl piperazine LpxH inhibitors
-
The UDP-2,3-diacylglucosamine pyrophosphate hydrolase LpxH is essential in lipid A biosynthesis and has emerged as a promising target for the development of novel antibiotics against multidrug-resistant Gram-negative pathogens. Recently, we reported the c
- Ennis, Amanda F.,Fenton, benjamin A.,Hong, Jiyong,Kwak, Seung-Hwa,Lim, Won Young,Webster, caroline G.,Zhou, Pei,cho, Jae,cochrane, c. Skyler
-
-
- INHIBITORS OF DIHYDROCERAMIDE DESATURASE FOR TREATING DISEASE
-
Disclosed herein are dihydroceramide desaturase 1 (Des1) inhibitor compounds and compositions, which are useful in the treatment of diseases, such as metabolic disorders, where inhibition of Des1 is expected to be therapeutic to a patient. Methods of inhibition of Des1 activity in a human or animal subject are also provided.
- -
-
-
- PYRROLE mTORC INHIBITORS AND USES THEREOF
-
The present invention provides compounds, compositions thereof, and methods of using the same.
- -
-
-
- PYRROLE mTORC INHIBITORS AND USES THEREOF
-
The present invention provides compounds, compositions thereof, and methods of using the same.
- -
-
-
- TREATMENT OF AMYOTROPHIC LATERAL SCLEROSIS
-
The present invention relates to the identification of compounds and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the provided compounds.
- -
-
Page/Page column 119-120
(2010/07/10)
-
- ACYLATED PIPERIDIHES AS GLYCINE TRANSPORTER INHIBITORS
-
The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R1, n, X, Y and Z are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
- -
-
Page/Page column 68
(2010/11/23)
-
- Parallel synthesis of N-arylpiperazines using polymer-assisted reactions
-
A series of N-arylpiperazines were prepared in a parallel fashion using palladium-catalyzed cross-coupling, or nucleophilic aromatic displacement chemistries, and polymer-assisted sequestration and purification techniques as key steps.
- Duncton, Matthew A. J.,Roffey, Jonathan R. A.,Hamlyn, Richard J.,Adams, David R.
-
p. 2549 - 2552
(2007/10/03)
-
- Synthesis and antitumor activity of novel pyrimidinyl pyrazole derivatives. II. Optimization of the phenylpiperazine moiety of 1-[5-methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-3-phenylpiperazinyl-1-trans-propenes.
-
A series of novel 3-substituted-1-[5-methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-1-trans-propenes in order to improve the in vitro and in vivo activity of our prototype 3-[4-(3-chlorophenyl)-1-piperazinyl]-1-[5-methyl-1-(2-pyrimidinyl)-4-pyrazolyl]-1-trans-propene (2) were synthesized and evaluated by assays of growth inhibition against several tumor cell lines in vitro and antitumor activity against some tumor models when dosed both intraperitoneally and orally in vivo. Compounds 7a and 7e, the 3,5-difluorophenyl and 3,5-dichlorophenyl analogues of 2, respectively, showed significantly more potent cytotoxicity than 2 in vitro and potent antitumor activities without causing decrease of body temperature related to side effects.
- Naito, Hiroyuki,Ohsuki, Satoru,Sugimori, Masamichi,Atsumi, Ryo,Minami, Megumi,Nakamura, Yoshihide,Ishii, Mineko,Hirotani, Kenji,Kumazawa, Eiji,Ejima, Akio
-
p. 453 - 462
(2007/10/03)
-