131052-40-9

Upstream product

• 17874-76-9 6-(methoxycarbonyl)nicotinic acid 
• 75-65-0 tert-butyl alcohol 
• 24424-99-5 di-tert-butyl dicarbonate 
• 67515-76-8 methyl 5-amino-2-pyridinecarboxylate 
• 24242-20-4 5-amino-pyridine-2-carboxylic acid 
• 100-26-5 Pyridine-2,5-dicarboxylic acid 

Downstream Products

• 323578-38-7 tert-butyl N-[6-(hydroxymethyl)pyridin-3-yl]carbamate 
• 873651-92-4 (5-aminopyridin-2-yl)methanol 

Relevant academic research and scientific papers

INHIBITORS OF CYCLIN-DEPENDENT KINASES

Provided herein are inhibitors of cyclin-dependent kinases (CDKs), pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.

Intermediate of (1S,4S)-2,5-diazabicyclo[2,2,2]octane derivative and preparation method of intermediate

The invention discloses an intermediate of a (1S,4S)-2,5-diazabicyclo[2,2,2]octane derivative and a preparation method of the intermediate. The preparation method comprises the following steps of: taking a compound II as a raw material, firstly performing an amidation reaction to protect amido groups of the compound II and obtain a compound III, and conducting a reduction reaction between the compound III and hydrogen in the presence of a catalyst to obtain a compound IV; carrying out an amidation reaction to protect nitrogen atoms in a piperidine ring to obtain a compound V, then conducting areaction of the compound V with a reducing agent to obtain a compound VI, and then conducting a reaction between the compound VI with a halogenating reagent to obtain a compound VII, wherein the compound VII can also be subjected to a ring-closure reaction in the presence of a base so as to obtain a compound I.

BICYCLIC INHIBITORS OF PAD4

The present invention provides compounds useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.

PROBES FOR IMAGING HUNTINGTIN PROTEIN

Provided are imaging agents comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and methods of their use.

PYRROLO[2,3-D]PYRIMIDINYL, PYRROLO[2,3-B]PYRAZINYL AND PYR-ROLO[2,3-D]PYRIDINYL ACRYLAMIDES

The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylamides and analogues thereof. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.

Metallo-controlled dynamic molecular tweezers: Design, synthesis, and self-assembly by metal-ion coordination

The introduction of controllable dynamic features into synthetic receptors represents a step towards "smart" adaptive nanodevices. We report herein our studies on the construction of dynamic molecular tweezers in which the binding of a substrate is allost

Discovery of inhibitors of aberrant gene transcription from libraries ofdna binding molecules: Inhibition of LEF-1-mediated gene transcription and oncogenic transformation

The screening of a >9000 compound library of synthetic DNA binding molecules for selective binding to the consensus sequence of the transcription factor LEF-1 followed by assessment of the candidate compounds in a series of assays that characterized functional activity (disruption of DNA-LEF-1 binding) at the intended target and site (inhibition of intracellular LEF-1-mediated gene transcription) resulting in a desired phenotypic cellular change (inhibit LEF-1-driven cell transformation) provided two lead compounds: lefmycin-1 and lefmycin-2. The sequence of screens defining the approach assures that activity in the final functional assay may be directly related to the inhibition of gene transcription and DNA binding properties of the identified molecules. Central to the implementation of this generalized approach to the discovery of DNA binding small molecule inhibitors of gene transcription was (1) the use of a technically nondemanding fluorescent intercalator displacement (FID) assay for initial assessment of the DNA binding affinity and selectivity of a library of compounds for any sequence of interest, and (2) the technology usedto prepare a sufficiently large library of DNA binding compounds.

CETP INHIBITORS

Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. I

Quinazoline Antifolate Thymidylate Synthase Inhibitors: Heterocyclic Benzoyl Ring Modifications

The synthesis is described of a series of C2-methyl-N10-alkylquinazoline-based antifolates in which the p-aminobenzoate ring is replaced by the heterocycles thiophene, thiazole, thiadiazole, pyridine, and pyrimidine.These were generally elaborated by the reaction of (bromomethyl)quinazoline 18 or its N3--protected derivative 36 with suitable heterocyclic amines although each heterocyclic system required its own particular synthetic approach.The compounds were tested as inhibitors of partially purified L1210 thymidylate synthase (TS).Theywere also examined for their inhibition of the growth of L1210 cells in culture.The thiophene system 7 and its related thiazole 8 gave analogues that were considerably more potent than the parent benzene series 2 as inhibitors of L1210 cell growth although in general these heterocycles were somewhat poorer inhibitors of the isolated TS enzyme.The enhanced cytotoxicities of the thiophene and thiazole analogues result, at least in part, from their efficient transport into the cells via the reduced folate carrier mechanism and very good substrate activity for folypolyglutamate synthetase.The replacement of the C2-methyl group by C2-(fluoromethyl) and C2-(hydroxymethyl) substituents in the thiophene and thiazole series gave derivatives that were only slightly less potent inhibitors of the TS enzyme but which were considerably less cytotoxic.