33 results about "Pipequaline" patented technology

The invention relates to a novel preparation method of 1-(4-fluorobenzyl)-3-(4-isobutoxybenzyl)-1-(1-methylpiperidyl-4-yl)urea hemitartrate (pimavanserin tartrate), particularly a pharmaceutical compound for treating Parkinson's disease, of which the structural formula is disclosed as Formula (I). The invention also relates to a novel intermediate of the preparation method.

The present application discloses a therapeutic agent for breast cancer, comprising 5-((2-(4-(1-(2-hydroxyethyl)piperidin-4-yl)benzamide)pyridin-4-yl)oxy)-6-(2-methoxyethoxy)-N-methyl-1H-indole-1-carboxamide or a pharmacologically acceptable salt thereof.

A slowly-releasing compound medicine in the form of tablet for treating and preventing thrombosis and apoplexy is prepared from aspirin, 2-(acetoxy) benzoic acid, slow-releasing dipyridamole, 2,2',2'',2''', [(4,8-dipiperidylpyrimido[5,4-d] pyrimidine-2,6-diyl) dihyponitido]-tetraethanol through granulating, tabletting and coating. Its advantages are high curative effect and equickly taking its effect.

The invention belongs to the field of the pharmaceutical chemistry and pharmacology, and concretely relates to an application of a compound of [(1E,1'E)-(4-Oxo-1-propionylpiperidine-3,5-diylidene)bis(methanylylidene)]bis(2-methoxy-4,1-phenylene)dipropionate (S1) in the preparation of anti-inflammation or/and anti-oxidation drugs. The above piperidone type curcumin analog S1 can dose-dependently inhibit the expression and release of inflammation factors comprising TNF-alpha, IL-6 and the like, and can also obviously improve the survival rate of mice death-induced by LPS. The compound has a good safety and stability, and can be exploited to inflammation or/and oxidation stress related disease treatment drugs.

The invention relates to the field of chemical medicines and concretely relates to a 1-(pyrimidine-4-yl)-3-aminopiperdine derivative and its preparation method and use. The invention provides the 1-(pyrimidine-4-yl)-3-aminopiperdine derivative. The 1-(pyrimidine-4-yl)-3-aminopiperdine derivative has a structure shown in the formula IV. The invention also provides a preparation method and a use of the 1-(pyrimidine-4-yl)-3-aminopiperdine derivative. The 1-(pyrimidine-4-yl)-3-aminopiperdine derivative can selectively inhibit JAK3 and provide a novel choice for treating JAK3-related diseases such as rheumatoid arthritis, asthma, chronic obstructive pulmonary diseases and tumors.

The present invention provides a pipecolic acid 4-hydroxylase protein exemplified by the following (A), (B), and (C), having activity to react with L-pipecolic acid in the presence of 2-oxoglutaric acid and iron(II) ions to produce trans-4-hydroxy-L-pipecolic acid, and a method for producing 4-hydroxy amino acid, which method comprises reacting the pipecolic acid 4-hydroxylase protein, cells containing the protein, a treated product of the cells, and/or a culture liquid obtained by culturing the cells, with α-amino acid to produce 4-hydroxy amino acid:

• (A) a polypeptide comprising the amino acid sequence represented by SEQ ID NO:2, 4, 6, 8, 10, 12, 16, or 18;
• (B) a polypeptide comprising the amino acid sequence represented by SEQ ID NO:2, 4, 6, 8, 10, 12, 16, or 18 except that one or several amino acids are deleted, substituted, and/or added, and having pipecolic acid 4-hydroxylase activity; and
• (C) a polypeptide having an amino acid sequence that is not less than 80% identical to the amino acid sequence represented by SEQ ID NO:2, 4, 6, 8, 10, 12, 16, or 18, and having pipecolic acid 4-hydroxylase activity.

The invention discloses a monocarbonyl curcumin analogue as well as preparation and an application thereof, the curcumin analogue is represented by a formula I, or pharmaceutically acceptable salts of the curcumin analogue comprise hydrochloride and sulfate, aldehydes and ketones are used as raw materials, monocarbonyl curcumin analogues CuA-1-CuA-3 are designed and synthesized, by designing and synthesizing a monocarbonyl curcumin analogue CuA-4 by taking 3, 4-dihydro-2H-pyran, vanillin, 4-pyridinium methylbenzenesulfonate and 1-methyl-4-piperidone as raw materials, and substituting an unstable beta-dicarbonyl structure with a monocarbonyl group to obtain the more stable monocarbonyl curcumin analogue CuA-1-CuA-4. The monocarbonyl curcumin has better pharmacokinetic behavior and higher anti-tumor activity, and the monocarbonyl curcumin is applied to preparation of drugs for resisting inflammation and treating inflammation-related diseases, Alzheimer's disease, Parkinson's disease, depression, lung cancer, liver cancer, breast cancer, colon cancer and cervical cancer.

The present invention relates to a benzopiperidine derivative, a preparation method thereof and a medical use thereof. In particular, the present invention relates to a benzopiperidine derivative as shown by general formula (I), a preparation method thereof and a pharmaceutical composition containing the derivative, as well as a use thereof as an estrogen receptor modulator in the prevention and/or treatment of estrogen receptor-mediated or dependent diseases or conditions. Preferably, the disease is breast cancer. The substituents in the general formula (I) are the same as those defined in the description.

The present invention relates to pharmaceutical compositions suitable for oral administration comprising 5-(1H-pyrazol-4-yl)-2-(6-((2,2,6,6-tetramethylpiperidin-4-yl)oxy)pyridazin-3-yl)phenol (branaplam) and a pharmaceutically acceptable cyclodextrin.

The invention discloses a pipecolinic acid preparation process based on reverse dropping and belongs to the technical field of medicines. By adopting the pipecolinic acid preparation process based onreverse dropping, S1-S2 and S3-S7 can be implemented simultaneously, so that the lasting time of the whole preparation process can be effectively shortened; meanwhile, by adopting a dropping mode in the preparation process, a conventional mode of dropping from top to bottom is changed into a mode of dropping from bottom to top, small water domes can be formed because of instantaneous impact resulted when a liquid to be dropped is fed into a reaction kettle, and are diffused outwards and upwards, liquid convection of the dropped liquid and a reactant can be enhanced because of the water domes,thus a good mixing effect is achieved, reactions can be accelerated to a certain extent, the preparation efficiency can be improved, and compared with the mode of dropping from top to bottom, the process is capable of effectively avoiding the phenomenon that the content of the reactant is changed to a certain extent as the liquid is splashed because of water impact and is adhered to an inner wall.

The invention relates to the technical field of medicines, in particular to a spiro piperidone derivative defined in the specification, wherein the pharmacological experiments show that the derivative or salt has very strong inhibitory activity on KRAS-PDE delta protein-protein interaction and has relatively strong in-vitro anti-tumor activity. The invention also provides a preparation method of the derivative and the pharmaceutically acceptable salt thereof, and an application of the derivative and the pharmaceutically acceptable salt thereof in preparation of a KRAS-PDE delta inhibitor and an antitumor drug.

The invention provides compounds for use as medicaments, which act by inhibiting CYP17A1 and CYP19A1 enzymes. The compounds have particular application in the treatment of cancer especially prostate cancer and breast cancer. The compounds have the formula: [Chem. 1] wherein: R is independently selected from the group consisting of optionally substituted arylamide; optionally substituted alkylarylamide; optionally substituted aryl carboxamide; optionally substituted cyanopiperidine; optionally substituted oxopiperidine; optionally substituted N-(pyridin-3-yl); optionally substituted pyridin-3-yl; optionally substituted pyrazole-4-carboxamide; optionally substituted pyrimidin-4-ylcarboxamide; optionally substituted pyrimidin-4-ylcarboxamide; optionally substituted 1H-pyrrol-2-ylcarboxamide; optionally substituted morpholin carboxamide; optionally substituted 1H-indazol-3-ylcarboxamide; optionally substituted 5-cyanopiperidin-3-ylcarboxamide; optionally substituted quinolin-7-yl; optionally substituted pyrazin-2-ylcarboxamide; optionally substituted 1H-1,3-benzodiazole-6-carboxamide; and optionally substituted 3-oxo-3,4-dihydro-2H-1,4-benzoxazin-7-ylcarboxamide; Each R1, R2, R3, R4, R5 is independently selected from the group consisting of H; OH; a halogen atom; OCH₃; and NH₂; and X is independently selected from the group consisting of O, H and OH. Some of the compounds are claimed per se and the invention also encompasses pharmaceutically acceptable salts, solvates, hydrates, primary metabolites and prodrugs thereof.

Inhibitors of ubiquitin specific protease 19 (USP19) of Formula (I) are provided, together with pharmaceutical compositions comprising said inhibitors, and methods of use thereof. The compounds can be used in in the treatment of muscular atrophy, obesity, insulin resistance or type II diabetes or in reducing the loss of muscle mass.