63 results about "New chemical entity" patented technology

The subject invention provides liposome formulations that are capable of specifically targeting cell types. The subject invention also provides for the encapsulation of new chemical entities (NCE) or other drug candidate molecules (DCM) within liposomes that specifically target a particular cell type. The subject invention, advantageously, solubilizes compounds, with low solubility in aqueous environments, and permits screening of these compounds against intact cells for biological activity in the absence of detergents that can damage cell membranes. Also provided are methods of preparing liposome formulations that target a specific cell type and methods of delivering therapeutic agents to target cells.

The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts,

wherein R¹, R², R³, A, B, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.

This patent describes a novel in vitro cell-based method for biological validation and pharmacological screening of drugs, new chemical entities (NCEs) and biologics, which is predictive of in vivo testing for efficacy and adverse events in patients, as occurs in clinical trials. The same method can be used to create an in vitro cell-based assay to identify the ‘right marketed medication for the right patient’ (personalized medicine), and to identify responders/non-responders in ongoing clinical trials with NCEs. In addition this approach can be used to identify new indications for existing medicines and new indications for NCEs that were unsuccessful in their intended uses.

The present invention provides preparation process of antrodia camphorata polysaccharide and antrodia camphorata triterpene with adsorptive microporous resin and its product, and relates to chromatographic separation technology with adsorptive microporous resin and extraction of effective Chinese medicine component. Antrodia camphorata sporophore or mycelium is extracted with hot water and sectional eluted in microporous resin with water and alcohol to obtain antrodia camphorata polysaccharide and antrodia camphorata triterpene separately. The products of the present invention are used in preparing medicine and antrodia camphorata triterpene has excellent liver cancer cell resisting activity.

In this patent we describe the purification of prenylated benzophenones from the fruit rinds of Garcinia species and its evaluation as an inhibitor for Histone acetyltransferases p300 and PCAF. We have found that prenylated benzophenones are potent HAT inhibitors of p300 (IC₅₀-1 μM) and pCAF (IC₅₀-15 μM). The inhibitors significantly repress the p300 HAT dependent transcriptional activation from in vitro assembled chromatin template but had no effect on transcription from DNA. These results suggest that the compounds could be specific to HATs. Thus these compounds should be useful as biological switching molecule for evaluating the role of p300 and PCAF in cellular functions and may be useful as new chemical entities for the development of anticancer drugs.

Creatine derivatives and compositions containing a [one or more?] bioactive form[s] of creatine. The new chemical entity comprises an acetyl creatine, N-acyl creatines, N,N-diacyl creatines or any N-acetyl creatine species with enhanced solubility and bioavailability. Also provided by this invention are various methods for providing several beneficial effects that comprise administering compositions comprising N-acetyl creatine, N-acyl creatines, N,N-diacyl creatines or any N-acetyl creatine species to a mammalian subject, either chronically or acutely.

New chemical entities which comprise corticosteroids and phosphorylated β-agonists for use in therapy and compositions comprising and processes for preparing the same.

The invention provides a 5-lipoxygenase inhibitor and a preparation method, a medical composite and an application thereof. More specifically, the invention provides a compound shown in general formula (I) or acceptable salt, solvate or hydrate thereof in pharmacy. The invention also relates to a preparation method, medical composite and application of the compound. The biological activity experiment shows that the compound of the invention is effective 5-LOX small molecule inhibitor with novel structure. Therefore the compound is expected to be developed to be new powerful chemical entity forcuring diseases related to leukotriene.

Described herein are pharmaceutical compositions and medicaments, and methods of using such pharmaceutical compositions and medicaments in the treatment of inflammation and cancer.

The invention discloses a sesquiterpene quinone compound separated and purified from abelmoschus sagittifolius, as well as a preparation method and applications thereof, relating to the technical field of medicines. The new sesquiterpene quinone compound with antitumor activity is named as Acylhisbiscone B, with the molecular formula of C17H22O4 and the structural formula shown in the specification. According to the preparation method, the detection on the antitumor activity of the new compound is carried out by adopting an MTT method through combination of column chromatography and preparative liquid chromatography purification methods. In vitro experiment results show that the new sesquiterpene quinone compound has activity on significantly inhibiting the growth of Hela (human cervical carcinoma cells) and HepG-2 (human hepatoma carcinoma cells). The new sesquiterpene quinone compound can provide new chemical entity or lead compound for research of antitumor medicaments, and can also be used as food raw materials for preparation of health food.

The present invention discloses a chrysotoxine bibenzyl derivative shown as a formula I. R1 represents C=O, CH2, NH, S=O or a covalent bond; R2 represents alkyl, phenyl, substituted phenyl, benzene ring substituted C1-3 alkyl, C5-C6 cycloalkyl, and a pentabasic or hexahydric unsaturated heterocyclic group containing one or more O, S and N. The invention also discloses a simple and efficient preparation method of the chrysotoxine bibenzyl derivative, and application of the derivative to the preparation of neuroprotective drugs and drugs for treating Alzheimer disease. The chrysotoxine 4-O-substituted bibenzyl derivative has significant protective effect on A beta-induced neuronal apoptosis, and is a potential novel chemical entity for the treatment of AD.

The invention discloses a dendrobium officinale analogue and pharmaceutically acceptable salt and hydrate thereof, and the analogue has anti-tumor activity, especially significantly inhibits the growth of colon cancer SW480 cells, and is a potential new chemical entity for treating colon cancer. The invention further discloses a simple and efficient preparation method of the dendrobium officinaleanalogue and application of the dendrobium officinale analogue in preparation of anti-cancer, anti-tumor and colorectal cancer treatment pharmaceutical compositions, and the dendrobium officinale analogue has important significance in research and development of anti-cancer or anti-colorectal cancer drugs.

The present invention relates to thioester compounds and the incorporation and use of the new chemical entities as flavor and fragrance chemicals.

Lithium is regarded as the gold standard comparator and benchmark treatment for mania. One of the problems associated with Lithium is its narrow therapeutic window. Recent attempts to find new drugs with similar therapeutic activities have yielded new chemical entities. However, these potential new drugs have yet to match the many bioactivities attributable to lithium's efficacy for the treatment of neuropsychiatric diseases. Consequently, an intense effort for re-engineering lithium therapeutics using cocrystallization is currently underway. The evaluation of pharmacokinetics of previously unexplored lithium salts with organic anions (lithium salicylate and lithium lactate) has found that these lithium salts exhibit profoundly different pharmacokinetics compared to the more common FDA approved salt, lithium carbonate, in rats. Remarkably, lithium salicylate produced elevated blood and brain levels of lithium beyond 48 hours post-dose without the sharp peak that contributes to the toxicity problems of current lithium therapeutics.

The invention discloses application of an SRGN gene and polypeptide thereof in serving as a detection marker for breast cancer molecular typing, in particular to application of the SRGN gene and the polypeptide thereof in serving as a serum marker for detecting a triple-negative breast cancer or in preparation of a detection reagent for the triple-negative breast cancer, and provides a novel breast cancer serum marker, that is, the SRGN gene and the polypeptide thereof. It is proved that expression of the SRGN gene in breast cancer serum is enhanced, and expression of the SRGN gene in serum of a triple-negative breast cancer patient is mainly and significantly increased compared with expression of the SRGN gene in serum of a breast cancer patient with the other molecular types. Accordingly, not only is a new target supplied to breast cancer serology detection, but also new data and a quick serology detection method are supplied to breast cancer molecular typing; a new chemical entity is designed at the gene level and the protein level by taking the gene as the target, breast cancer molecular typing can be quickly, conveniently and effectively performed, and therefore the breast cancer treatment effect is improved.

The present invention is directed towards new chemical entities which primarily inhibit the human T-type calcium channels and differentially modulate other key ion channels to control cell excitability, and abnormal neuronal activity particularly involved in the development and maintenance of persistent or chronic pain, and/or neurological disorders. These novel compounds are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which these ion channels are involved. The invention is also directed towards pharmaceutical formulations comprising these compounds and the uses of these compounds.

The invention provides a flavonoid new chemical entity, which has little moisture absorption and good storage stability, and is applicable to preparation of food or health food or drugs for reduction of capillary fragility, treatment or prevention of chronic venous insufficiency, hemorrhoid, scurvy, venous lower limb ulcer, premenstrual syndrome, diabetics' microangiopathy and secondary upper limb lymphedema, cardiovascular diseases, blood glucose and lipid regulation, antisepsis and inflammation reduction, virus resisting, cancer resisting, immunity adjustment, radiation protection, liver protection, rheumatoid arthritis or arthritis resisting, ulcer resisting, phlegm eliminating, asthma relieving, black spots, freckles, free radical resistance, and oxidation resistance.

A mixed metal complex of a compound of Formula I, or a salt thereof, wherein the mixed metals comprise a Group III-XII transition metal and a Group II metal: (Formula I) (I) wherein X, R¹, R², R³, and R⁴ are as defined herein, is produced in a one step crystallization from a solution of the Group III-XII transition metal, the Group II metal, and a compound of Formula I. Methods for treatment of a pathological condition in a patient, for example, a pathological condition caused by the presence of oxygen-derived free radicals, comprises administering the mixed metal complex to the patient.

The invention discloses a method for detecting the metabolic performance of a new chemical entity in different species of liver microsomes, which comprises the following steps: in a reaction system containing a buffer solution, liver microsomes, a substrate, MgCl2 and NADPH, screening out an optimal reaction condition by taking the metabolic rate of the substrate as a reference to obtain a human liver microsome incubation system. According to the establishment method of the human liver microsome incubation system, rat, mouse, dog and monkey liver microsome incubation systems are sequentially established. The method comprises the following steps: performing in-vitro metabolism test on a new chemical entity in incubation systems of different species of liver microsomes, performing positive group reaction by using a substrate, and setting a negative group without adding NADPH and a blank group without adding liver microsomes; and identifying a metabolism result after testing. According to the method for detecting the metabolic performance of the new chemical entity in different species of liver microsomes, false positive and false negative results can be avoided, the reliability of an identification result is improved, and a reliable basis is provided for promoting research and development of new drugs.