85160-82-3

Upstream product

• 7623-09-8 2-chloropropionyl chloride 
• 121-88-0 5-Nitro-2-aminophenol 
• 5445-17-0 Methyl 2-bromopropionate 
• 598-21-0 2-Bromoacetyl bromide 
• 535-11-5 Ethyl 2-bromopropionate 

Downstream Products

• 941291-25-4 (+/-)-3,4-dihydro-2-methyl-7-nitro-2H-1,4-benzoxazine 
• 105807-79-2 7-amino-2-methyl-2H-benzo[b][1,4]oxazin-3(4H)-one 

Relevant academic research and scientific papers

Pyrimidomorpholine derivative, and preparation method and application thereof

The invention specifically relates to a small molecule compound capable of resisting medullary thyroid carcinoma, acute leukemia and inflammations, and a preparation method and application thereof, belonging to the field of chemical pharmaceuticals. The objective of the invention is to overcome the technical problems of poor selectivity, easy incurrence of drug resistance and toxic and side effectof conventional commercially-available clinical medicines for medullary thyroid carcinoma. The invention provides a pyrimidomorpholine derivative to overcome the above technical problem. The pyrimidomorpholine derivative is mainly characterized in that the position 6 of pyrimidine is substituted, and the structure of the pyrimidomorpholine is as shown in a formula I which is described in the specification. The compound provided by the invention has the advantages of high activity in resisting medullary thyroid carcinoma, low toxic and side effect and capacity of overcoming clinical drug resistance, and has great value in development of medicines for treating medullary thyroid carcinoma.

Benzomorpholone derivative as well as preparation method and application of benzomorpholone derivative

The invention belongs to the field of chemical medicines and particularly relates to a benzomorpholone derivative as well as a preparation method and application of the benzomorpholone derivative. The invention provides a benzomorpholone derivative with a structure as shown in the formula I and also provides a preparation method and application of the benzomorpholone derivative. The benzomorpholone derivative provided by the invention is novel in structure, has a good effect on selectively inhibiting BET targets, produces cytotoxicity for various tumor cells to different extents and is a novel BET small-molecule inhibitor. The compound disclosed by the invention has the potential to develop antitumor drugs.

Synthesis and biological evaluation of N-(3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-7-yl)benzenesulfonamide derivatives as new BET bromodomain inhibitors for anti-hematologic malignancies activities

The bromodomain and extra-terminal proteins (BETs), in particular BRD4, has been reported to play important roles in cancer, inflammation, obesity, cardiovascular disease, and neurological disorders. In this paper, a series of benzomorpholinone derivatives were synthesized and biologically evaluated as BETs inhibitors. Detailed structure–activity relationship studies led to the discovery of several new potent compounds, of which 15h and 15i displayed IC 50 values of 2.8 and 4.5 μ M against BRD4 (D1), respectively, and showed good anti-proliferation activities against four hematologic malignancies cell lines at low-micromolar concentrations, including MV4-11, OCI-LY10, Pfeifer, and Su-DHL-6 cells. This chemotype could be further optimized with respect to its potency and drug-like properties in the future.

HETEROCYCLIC COMPOUND

The present invention provides a heterocyclic compound having an RORγt inhibitory action. The present invention relates to a compound represented by the formula (I): wherein Ar is a the partial structure (1) to the partial structure (5), Q is a bivalent group selected from the group consisting of (Ia)-(If), and B is a ring optinally having substituent(s), or a salt thereof.

INHIBITORS OF THE INTERACTION BETWEEN MDM2 AND P53

The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds: wherein n, s, t, R1, R2, R3, R4, Rs

Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones

Recent interest in orally available androgens has fueled the search for new androgens for use in hormone replacement therapy and as anabolic agents. In pursuit of this, we have discovered a series of novel androgen receptor modulators derived from 7H-[1,4]oxazino[3,2-g]quinolin-7-ones. These compounds were synthesized and evaluated in competitive binding assays and an androgen receptor transcriptional activation assay. A number of compounds from the series demonstrated single-digit nanomolar agonist activity in vitro. In addition, lead compound (R)-16e was orally active in established rodent models that measure androgenic and anabolic properties of these agents. In this assay, (R)-16e demonstrated full efficacy in muscle and only partially stimulated the prostate at 100 mg/kg. These data suggest that these compounds may be utilized as selective androgen receptor modulators or SARMs. This series represents a novel class of compounds for use in androgen replacement therapy.

Microwave-assisted one-pot regioselective synthesis of 2-alkyl-3,4-dihydro- 3-oxo-2H-1,4-benzoxazines

A protocol for regioselective one-pot synthesis of 2-alkyl-3,4-dihydro-3- oxo-2H-1,4-benzoxazines under controlled microwave heating has been developed. Starting from commercially available 2-aminophenols, a base-mediated regioselective O-alkylation took

Androgen receptor modulator compounds and methods

Compounds, pharmaceutical compositions, and methods for modulating processes mediated by steroid receptors. In particular, preparation and methods of use of non-steroidal compounds and compositions that are agonists, partial agonists, and antagonists for the androgen receptor (AR) are described. Further, described are the methods of making and use of critical intermediates including a stereoselective synthetic route to intermediates for the AR modulators.