An acyl ethyl ester polycyclic compound, and a pharmaceutical composition and the use thereof. The acyl ethyl ester polycyclic compound is as represented by formula I, wherein X is S or Se. The compound has the effect of preventing or treating individuals infected by viruses.
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
A method for preparing lanthanum carbonate tetrahydrate and a product thereof. The lanthanum carbonate tetrahydrate is prepared by reacting lanthanum oxide and acetic acid with potassium carbonate or potassium bicarbonate or ammonium bicarbonate to prepare lanthanum carbonate octahydrate, and drying the lanthanum carbonate octahydrate. Compared with the lanthanum carbonate tetrahydrate in the prior art, the prepared lanthanum carbonate tetrahydrate has a characteristic spectral peak on a terahertz spectrum, and has excellent dissociation and dissolution characteristics of lanthanum ions.
A method for preparing lanthanum carbonate tetrahydrate and a product thereof. The lanthanum carbonate tetrahydrate is prepared by reacting lanthanum oxide and acetic acid with potassium carbonate or potassium bicarbonate or ammonium bicarbonate to prepare lanthanum carbonate octadhydrate, and drying the lanthanum carbonate decahydrate. Compared with the lanthanum carbonate tetrahydrate in the prior art, the prepared lanthanum carbonate tetrahydrate has a characteristic spectral peak on a terahertz spectrum, and has excellent dissociation and dissolution characteristics of lanthanum ions.
The present application provides a method for synthesis of Roxadustat. A compound as represented by formula (VIII) is used as a raw material, and is reacted with phenol, a vinyl-containing ether, an acid, hydroxylamine, and then the product is reacted with glycine. In addition, the present application also provides intermediate compounds as represented by formula (IX), formula (XI), formula (XII), formula (IV), and formula (V) for synthesis of Roxadustat. Here, details of the substituents involved in formula (VIII), formula (IX), formula (XI), and formula (XII) are stated in the description.
C07C 69/92 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring with etherified hydroxyl groups
C07C 65/40 - Compounds having carboxyl groups bound to carbon atoms of six-membered aromatic rings and containing any of the groups OH, O-metal, —CHO, keto, ether, groups, groups, or groups containing keto groups containing singly bound oxygen-containing groups
5.
USE OF LANTHANUM ACETATE OR HYDRATES THEREOF FOR TREATING HYPERPHOSPHATEMIA
Disclosed is a use of lanthanum acetate or hydrates thereof for treating hyperphosphatemia. The lanthanum acetate or hydrates thereof of the invention have a high capacity of binding phosphorus ions in multiple tests compared with lanthanum carbonate, and the lanthanum acetate has the performance superior to that of the lanthanum carbonate.
The present invention provides polymorph of 3-(4-amino-1-oxo-1,3-dihydro-2H-isoindole-2-yl)-piperidine-2,6-dione, and also the preparing methods and pharmaceutical compositions thereof.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
7.
Methods for synthesizing 3-(substituted dihydroisoindolinone-2-yl)-2, 6-dioxopiperidine, and intermediates thereof
The present invention discloses methods for synthesizing 3-(substituted dihydroisoindolinone-2-yl)-2,6-dioxopiperidine and intermediates thereof, namely, the synthesis of compounds of the Formula (I), with each substitutional group defined in the patent specification. Owing to the advantages of high productivity, little influence to the environment and material accessibility, the methods of the present invention is suitable for industrial production.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 209/48 - Iso-indolesHydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
C07D 209/46 - Iso-indolesHydrogenated iso-indoles with an oxygen atom in position 1
C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
8.
Pharmaceutical formulations comprising voriconazole and processes for preparation thereof
The present invention provides a pharmaceutical formulation comprising voriconazole or a pharmaceutically acceptable derivative thereof, and an excipient of formula (I), i.e., monomethoxy poly(ethylene glycol)-poly (D,L-lactic acid) block copolymers (mPEG-PDLLA). The pharmaceutical formulation of the present invention has been shown to be stable and safe by experiments.
NAN JING CAVENDISH BIO-ENGINEERING TECHNOLOGY CO., LTD. (China)
Inventor
Yan, Rong
Yang, Hao
Hou, Wen
Xu, Yongxiang
Abstract
Synthesis methods of dasatinib are provided, which comprise the following steps: reacting a compound of formula I with a compound of formula II to obtain a compound of formula III, and then connecting the compound of formula III with 2-chloro-6-methylaniline and 1-(2-hydroxyethyl)piperazine in any order to give dasatinib. Furthermore, purification methods of dasatinib are also provided.
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
10.
POLYMORPHS OF DASATINIB, PREPARATION METHODS AND PHARMACEUTICAL COMPOSITIONS THEREOF
NAN JING CAVENDISH BIO-ENGINEERING TECHNOLOGY CO., LTD. (China)
Inventor
Yan, Rong
Yang, Hao
Xu, Yongxiang
Abstract
Polymorph I of dasatinib monohydrate and polymorph II of dasatinib, their preparation methods and pharmaceutical compositions containing the same are provided. These polymorphs have better physicochemical properties, are more stable, and are more suitable for industrial scale production.
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61P 35/02 - Antineoplastic agents specific for leukemia
NAN JING CAVENDISH BIO-ENGINEERING TECHNOLOGY CO., LTD. (China)
Inventor
Yan, Rong
Yang, Hao
Hou, Wen
Xu, Yongxiang
Abstract
Synthesis process of dasatinib is disclosed, which includes the step of reacting the compound of formula I with that of formula II to obtain the compound of formula III. Also disclosed is the compound of formula III which is used as an intermediate for synthesizing dasatinib. The substituents of R1, R2, R3 or R4 in formulae I, II or III are defined as in the description.
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
12.
POLYMORPH OF 3-(SUBSTITUTEDDIHYDROISOINDOLINONE-2-YL)-2,6-DIOXOPIPERIDINE, AND PHARMACEUTICAL COMPOSITIONS THEREOF
The present invention provides polymorph of 3-(4-amino-1-oxo-1,3- dihydro-2H-isoindole-2-yl)-piperidine-2,6-dione, and also the preparing methods and pharmaceutical compositions thereof.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
The present invention discloses methods for synthesizing 3-(substituted dihydroisoindolinone-2-yl)-2,6-dioxopiperidine and intermediates thereof, namely, the synthesis of compounds of the Formula (I), with each substitutional group defined in the patent specification. Owing to the advantages of high productivity, little influence to the environment and material accessibility, the methods of the present invention is suitable for industrial production.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 209/46 - Iso-indolesHydrogenated iso-indoles with an oxygen atom in position 1
C07D 209/48 - Iso-indolesHydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
14.
PHARMACEUTICAL FORMULATIONS COMPRISING VORICONAZOLE AND PROCESSES FOR PREPARATION THEREOF
A pharmaceutical formulation comprises voriconazole or a pharmaceutically acceptable derivative thereof, and an excipient of formula (I), i.e., monomethoxy poly(ethylene glycol)-poly(D,L-lactic acid) block copolymers (mPEG-PDLLA). The pharmaceutical formulation has been shown to be stable and safe by experiments.
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 9/19 - Particulate form, e.g. powders lyophilised
The present invention provides a novel and highly stereoselective process for preparing gemcitabine, which is suitable for industrial production, wherein, it includes the following reactions. Additionally, the invention discloses the key intermediates. The definition for the groups of G1, G2, G3, G4, and G5 are described in the specification.
patents
