SHANGHAI ACEBRIGHT PHARMACEUTICALS GROUP CO., LTD. (Chine)
Inventeur(s)
Peng, Huan
Min, Sijia
Zhang, Fengjie
Zhang, Liang
Abrégé
Provided is a new crystal form of (7S,13R)-11fluoro-7,14-dimethyl-6,7,13,14-tetrahydro-1,15-vinyl-bridged pyrazolo[4,3-f][1,4,8,10]-benzoxatriazacyclotridecyne-4(5H)-one (formula I). In another aspect, provided is a method for preparing the foregoing crystal form. In comparison with the existing technology, the crystal form prepared in the present invention has high stability, low hygroscopicity, a simple and convenient preparation method, good solubility, and is suitable for subsequent formulation research and development and industrial production.
SHANGHAI ACEBRIGHT PHARMACEUTICALS GROUP CO., LTD. (Chine)
Inventeur(s)
Peng, Huan
Zhang, Fengjie
Zhang, Liang
Abrégé
The present invention provides a new crystal form of (cis)-N-((S)-1-(6-(4-fluoro-1H-pyrazol-1-yl) pyridin-3-yl) ethyl)-1-methoxy-4-(4-methyl-6-((5-methyl-1H-pyrazol-3-yl) amino) pyrimidin-2-yl) cyclohexane formamide (compound of formula (I)) and a preparation method therefor.
C07D 401/14 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant au moins trois hétérocycles
A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
The present invention relates to a pyrrolotriazine derivative, a preparation method thereof and an application thereof in medicine. Specifically, disclosed is a pyrrolotriazine derivative that has remarkable inhibition activity to tyrosine kinase and is an effective tyrosine kinase inhibitor. The pyrrolotriazine derivative provides a new research direction and path for developing new tyrosine kinase inhibiting medicine that has low drug resistance or can relieve early inhibitor drug resistance, and has a wide application prospect and a high medicinal value.
Provided are acetatic Abiraterone trifluoroacetate, a preparation method and an application of same. The acetatic Abiraterone trifluoroacetate is obtained through a salt-forming reaction between acetatic Abiraterone and trifluoroacetic acid. The acetatic Abiraterone trifluoroacetate undergoes self-purification through recrystallization, and dissociation and recrystallization are performed on the purified acetatic Abiraterone trifluoroacetate, so that obtained acetatic Abiraterone has a high purity, a high yield, and stable quality, and is capable of meeting the requirement for mass production of acetatic Abiraterone.
C07J 43/00 - Stéroïdes normaux ayant un hétérocycle contenant de l'azote non condensé ou condensé en spiro avec le squelette du cyclopenta[a]hydrophénanthrène
5.
ERTAPENEM SODIUM CRYSTAL AND PREPARATION METHOD THEREOF
Disclosed are an Ertapenem sodium crystal and preparation method thereof, the Ertapenem sodium crystal has a powder X-ray diffraction spectrum as shown in Fig. 1. The Ertapenem sodium crystal is of low residual solvent content and high stability.
A61K 31/407 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil condensés avec des systèmes hétérocycliques, p. ex. kétorolac, physostigmine
6.
THIENOPYRIMIDINE AND FUROPYRIMIDINE DERIVATIVES, PREPARATION METHOD THEREOF AND MEDICAL USE THEREOF
Disclosed are thienopyrimidine and furopyrimidine derivatives, the preparation method thereof and the medical use thereof. The derivatives have a structure as shown in formula V. The thienopyrimidine and furopyrimidine derivatives provided in the present invention have dominant EGFR inhibiting activity, and some of these compounds also have dominant inhibiting activity against VEGFR; therefore, same can expect to be developed as tyrosine kinase EGFR and/or VEGFR inhibitors, and to be used for preparing the drugs for preventing or treating the diseases related to epidermal growth factor receptor EGFR and/or vascular endothelial growth factor receptor VEGFR. Provided is a new development direction and approach for developing novel tyrosine kinase inhibitor drugs having low drug resistance or able to relieve drug resistance to the inhibitor in the early stages, thereby having extensive application prospects and medical value.
C07D 491/048 - Systèmes condensés en ortho avec un seul atome d'oxygène comme hétéro-atome du cycle contenant de l'oxygène le cycle contenant de l'oxygène étant à cinq chaînons
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/5377 - 1,4-Oxazines, p. ex. morpholine non condensées et contenant d'autres hétérocycles, p. ex. timolol
Disclosed are a doripenem hydrate crystal and preparation method therefor. The X-ray diffraction spectrogram of the crystal powder is basically as represented in figure 1, and the measured water content is 4.4 to 5.5%. The doripenem hydrate crystal of the present invention has high purity, low residual solvent, good stability, and application safety. Additionally, the preparation method for the doripenem hydrate crystal of the present invention has simple techniques and low preparation cost, and is suitable for industrial production.
A61K 31/407 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil condensés avec des systèmes hétérocycliques, p. ex. kétorolac, physostigmine
Disclosed are a crystal of 17α-acetoxy-11β-(4-N,N-dimethylaminophenyl)-19-norpregna-4,9-dien-3,20- dione, and the preparation process thereof. The crystal substantially has the powder X-ray diffraction pattern shown in Fig. 1. The preparation process of the crystal comprises providing an organic solvent solution of a CDB-2914 raw material, with the solution temperature being 30 - 55°C; reducing the temperature to 20 - 30°C, and adding an anti-solvent; and further reducing the temperature to 0 - 10 °C and crystallizing for 2 - 7 hours.
Disclosed are an amorphous substance of 17α-acetoxy-11β-(4-N,N-dimethylaminophenyl)-19-norpregna-4,9-diene-3,20- dione and a preparation method thereof. The said CDB-2914 amorphous substance generally has a powder X-ray diffraction pattern shown as figure 1. The method for preparing the product comprises: providing a solution of CDB-2914 raw material in an organic solvent, and then crystallizing in the presence of a reverse solvent at certain temperature to obtain CDB-2914 amorphous substance.
Disclosed are processes for preparing pemetrexed disodium and its intermediate,4-(4-carbomethoxyphenyl)butanal. The process for preparing the intermediate comprises the following steps: methyl 4-bromobenzoate is condensed with 3-buten-1-ol; organic solvent is used to extract during the post-treatment; silica gel is added to decolorize; and the organic solvent is evaporated to give 4-(4-carbomethoxyphenyl)butanal. The product obtained by the present process, with a yield of higher than 80 %, and a purity measured by GC of higher than 95 %, may be directly used in the next bromination reaction for synthesizing pemetrexed disodium without purification. The present process is suitable for industrial production for the operation is simple and the reagents used are cheap and easy to be obtained.
C07C 45/46 - Préparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par condensation par réactions de Friedel-Crafts
C07C 47/228 - Composés non saturés comportant des groupes —CHO liés à des atomes de carbone acycliques contenant des cycles aromatiques à six chaînons, p. ex. le phénylacétaldéhyde
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