SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Wang, Jinxin
Zhang, Guimin
Wang, Ke
Yao, Jingchun
Pan, Lihong
Abrégé
The present invention relates to a cathepsin K inhibitor having the structure as shown in formula (0) and/or formula (II), wherein cyanopyrimidine or a keto group as an electrophilic group is a key group to exert a good inhibitory effect on cathepsin K. Further provided are a preparation method therefor and use thereof. The provided cathepsin K inhibitor has a relatively high inhibitory effect and selectivity, and is expected to be used for treating diseases including thyroid diseases, cardiovascular diseases, bone diseases and gum diseases.
The present invention relates to a cathepsin K inhibitor having the structure as shown in formula (0) and/or formula (II), wherein cyanopyrimidine or a keto group as an electrophilic group is a key group to exert a good inhibitory effect on cathepsin K. Further provided are a preparation method therefor and use thereof. The provided cathepsin K inhibitor has a relatively high inhibitory effect and selectivity, and is expected to be used for treating diseases including thyroid diseases, cardiovascular diseases, bone diseases and gum diseases.
A61K 31/437 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. indolizine, bêta-carboline
A61K 31/505 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime
A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
C07D 401/12 - 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 deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
C07D 409/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
C07D 417/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Guimin
Zhang, Hao
Yao, Jingchun
Yuan, Jiang
Zhao, Guifang
Li, Rui
Li, Guangyan
Zhao, Yun
Liang, Hongbao
Zhang, Zhenjun
Zhu, Xiangxia
Abrégé
Disclosed are a compound
Disclosed are a compound
Disclosed are a compound
of formula I or a pharmaceutically acceptable salt thereof, and use thereof in regulating and controlling an EGFR tyrosine kinase activity or preventing and treating an EGFR-related disease. The EGFR inhibitor of formula I has an inhibitory activity on EGFR D770-N771 ins NPG and NPG/T790M kinases, and an inhibitory effect on an EGFR-Del19/T790M/C797S kinase and cell proliferation of a KC-0122:Ba/F3EGFR-L858R/T790M/C797S three-mutation cell line and a KC-0116:Ba/F3EGFR-Del19/T790M/C797S three-mutation cell line.
The present invention belongs to the field of traditional Chinese medicine, and specifically relates to the use of a traditional Chinese medicine composition in the preparation of a pharmaceutical for preventing or/and treating amyotrophic lateral sclerosis. Specifically, the traditional Chinese medicine composition is prepared from herba schizonepetae, radix saposhnikoviae divaricatae, rhizoma seu radix notopterygii, radix angelicae pubescentis, radix bupleuri, radix peucedani, rhizoma chuanxiong, fructus aurantii, poria cocos, radix platycodi, and radix glycyrrhizae. Pharmacodynamic test results show that the traditional Chinese medicine composition provided by the present invention can prolong survival, maintain weight increase, and increase the limb strength of amyotrophic lateral sclerosis mouse models, has the effects of delaying the progression of muscle atrophy and delaying motor neuron apoptosis, and has a precise therapeutic effect for treating amyotrophic lateral sclerosis.
A61K 36/752 - Citrus, p. ex. citron vert, orange ou citron
A61P 25/00 - Médicaments pour le traitement des troubles du système nerveux
A61P 25/28 - Médicaments pour le traitement des troubles du système nerveux des troubles dégénératifs du système nerveux central, p. ex. agents nootropes, activateurs de la cognition, médicaments pour traiter la maladie d'Alzheimer ou d'autres formes de démence
4.
APPLICATION OF TRADITIONAL CHINESE MEDICINE COMPOSITION IN PREPARATION OF DRUGS FOR TREATING NEURITIS
Shandong New Time Pharmaceutical Co., Ltd. (Chine)
Inventeur(s)
Zhang, Guimin
Sun, Chenglei
Yao, Jingchun
Guan, Yongxia
Ma, Qingwen
Abrégé
A traditional Chinese medicine composition for treating neuritis. The traditional Chinese medicine composition is prepared mainly from Notopterygii Rhizoma et Radix, Angelicae Pubescentis Radix, Poria, Saposhnikoviae Radix, Schizonepetae Herba, Chuanxiong Rhizoma, Platycodonis Radix, Bupleuri Radix, Peucedani Radix, Aurantii Fructus, and Glycyrrhizae Radix et Rhizoma. The traditional Chinese medicine composition can significantly relieve facial paralysis, movement disorders, and other related symptoms of facial neuritis in a rat, remarkably improve expression of VEGFb, VEGFR1, and VEGFR2 proteins in postoperative side facial nerves of the rat, and promote recovery and regeneration of damaged rear axons.
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Guimin
Yao, Jingchun
Sun, Chenghong
Li, Honghua
Abrégé
Disclosed is a traditional Chinese medicinal composition for treating neurogenic pulmonary edema. The traditional Chinese medicinal composition is mainly prepared from Notopterygium root, angelicae pubescentis radix, poria cocos, radix saposhnikoviae, herba schizonepetae, rhizoma chuanxiong, platycodonis radix, radix bupleuri, common hogfennel root, fructus aurantii, and licorice root. The traditional Chinese medicinal composition can improve a lung index and lung wet weight/dry weight of a rat with neurogenic pulmonary edema, and has a therapeutic effect on the neurogenic pulmonary edema.
Shandong New Time Pharmaceutical Co., Ltd. (Chine)
Inventeur(s)
Zhang, Guimin
Yao, Jingchun
Li, Honghua
Sun, Chenghong
Zhao, Tao
Abrégé
A pharmaceutical composition for preventing or treating Alzheimer's disease and use thereof are disclosed and belong to the technical field of medicines. The pharmaceutical composition includes (Z)-3-(N-(3-bromo-4-fluorophenyl)-N′-hydroxyformamido)-4-(2-guanidinoethyl)amino)-1,2, 5-oxadiazole and anhydroicaritin. A pharmacodynamic experiment proves that the pharmaceutical composition achieves a synergistic therapeutic effect on treating Alzheimer's disease.
A61K 31/352 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à six chaînons avec un oxygène comme seul hétéro-atome d'un cycle condensés avec des carbocycles, p. ex. cannabinols, méthanthéline
A61P 25/28 - Médicaments pour le traitement des troubles du système nerveux des troubles dégénératifs du système nerveux central, p. ex. agents nootropes, activateurs de la cognition, médicaments pour traiter la maladie d'Alzheimer ou d'autres formes de démence
7.
BENZOYL PYRROLOPYRIMIDINE DERIVATIVE, AND USE THEREOF AND PREPARATION METHOD THEREFOR
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Guimin
Zhang, Hao
Yuan, Jiang
Yao, Jingchun
Zhao, Guifang
Li, Rui
Li, Guangyan
Abrégé
The present invention relates to the field of medicine, and specifically provides a benzoyl pyrrolopyrimidine derivative as represented by formula VI and a preparation method therefor, and also relates to the use of the compound in the preparation of a drug for preventing and treating BTK-related autoimmune diseases or tumors.
C07D 519/00 - Composés hétérocycliques contenant plusieurs systèmes de plusieurs hétérocycles déterminants condensés entre eux ou condensés avec un système carbocyclique commun non prévus dans les groupes ou
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Guimin
Liu, Zhong
Lan, Tianlong
Li, Guangyan
Ma, Chunyan
Pan, Gaofeng
Li, Zhenfa
Zhang, Qiang
Xu, Yuankai
Liu, Yunna
Abrégé
Provided is a pyrrolo[2,3-c]pyridine compound having a significant inhibitory effect on a bromodomain protein, or a pharmaceutically acceptable salt, a hydrate, a solvate, a prodrug, a stereoisomer or a tautomer thereof. Provided are a method for preparing the compound and intermediate compounds for use in the method. The compound can be used in preparation of a drug for diseases associated with bromodomain functions.
A61K 31/437 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. indolizine, bêta-carboline
A61P 31/18 - Antiviraux pour le traitement des virus ARN du HIV
9.
USE OF TRADITIONAL CHINESE MEDICINE COMPOSITION IN PREPARATION OF DRUG FOR TREATING COUGH VARIANT ASTHMA
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Guimin
Li, Xin
Liu, Dongguang
Abrégé
A traditional Chinese medicinal composition is prepared from Herba schizonepetae, Radix saposhnikoviae, Notopterygium root, Radix angelicae pubescentis, Radix bupleuri, common hogfennel root, Rhizoma chuanxiong, Fructus aurantii, Poria cocos, Radix platycodonis, and liquorice root. The traditional Chinese medicinal composition can reduce the cough frequency of a guinea pig model with cough variant asthma, a percentage of eosinophils in a bronchoalveolar lavage fluid, and a level of serum eosinophil cationic proteins, and has a prevention and treatment effect on the cough variant asthma.
Shandong New Time Pharmaceutical Co., Ltd. (Chine)
Inventeur(s)
Li, Qiang
Jia, Shixiang
Zhao, Lili
Zhang, Guimin
Liu, Zhong
Ma, Xinlu
Yan, Yuan
Li, Zhenyu
Hu, Xingxia
Zhang, Yuhua
Li, Bin
Abrégé
The invention provided herein relates to methods and uses of a bispecific antibody, which specifically binds the surface antigen CD3 of immune cells and the BCMA antigen on the surface of tumor cells and which may bind to human CD3 with high affinity, induce T cell proliferation, and mediate tumor cell killing effects. The bispecific antibody may be used to mediate the T cell-specific killing of target cells in in vitro tests.
C07K 16/30 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des récepteurs, des antigènes de surface cellulaire ou des déterminants de surface cellulaire provenant de cellules de tumeurs
A61K 39/395 - AnticorpsImmunoglobulinesImmunsérum, p. ex. sérum antilymphocitaire
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
C07K 16/28 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des récepteurs, des antigènes de surface cellulaire ou des déterminants de surface cellulaire
C07K 16/32 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des produits de traduction des oncogènes
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Wang, Jinxin
Zhang, Guimin
Wang, Ke
Yao, Jingchun
Pan, Lihong
Abrégé
The present invention relates to a cathepsin K inhibitor having a structure as shown in formula (0) and/or formula (II), wherein cyanopyrimidine or a ketone serving as an electrophilic group is a key group to exert a good inhibition effect on cathepsin K. Further provided are a method for preparing the cathepsin K inhibitor and the use thereof. The provided cathepsin K inhibitor has a relatively high inhibition effect and selectivity, and is expected to be used for treating diseases including thyroid diseases, cardiovascular diseases, bone diseases and gingival diseases.
C07D 247/02 - Composés hétérocycliques contenant des cycles comportant deux atomes d'azote comme uniques hétéro-atomes du cycle couverts par plus d'un des groupes principaux comportant les atomes d'azote en positions 1, 3
C07D 309/16 - Composés hétérocycliques contenant des cycles à six chaînons comportant un atome d'oxygène comme unique hétéro-atome du cycle, non condensés avec d'autres cycles comportant une liaison double entre chaînons cycliques ou entre chaînon cyclique et chaînon non cyclique
A61K 31/437 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. indolizine, bêta-carboline
A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
A61K 31/341 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à cinq chaînons avec un oxygène comme seul hétéro-atome d'un cycle, p. ex. isosorbide non condensés avec un autre cycle, p. ex. ranitidine, furosémide, bufétolol, muscarine
A61P 19/10 - Médicaments pour le traitement des troubles du squelette des maladies osseuses, p. ex. rachitisme, maladie de Paget de l'ostéoporose
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Guimin
Sun, Chenglei
Yao, Jingchun
Guan, Yongxia
Ma, Qingwen
Abrégé
A traditional Chinese medicine composition for treating neuritis. The traditional Chinese medicine composition is prepared mainly from Notopterygii Rhizoma et Radix, Angelicae Pubescentis Radix, Poria, Saposhnikoviae Radix, Schizonepetae Herba, Chuanxiong Rhizoma, Platycodonis Radix, Bupleuri Radix, Peucedani Radix, Aurantii Fructus, and Glycyrrhizae Radix et Rhizoma. The traditional Chinese medicine composition can significantly relieve facial paralysis, movement disorders, and other related symptoms of facial neuritis in a rat, remarkably improve expression of VEGFb, VEGFR1, and VEGFR2 proteins in postoperative side facial nerves of the rat, and promote recovery and regeneration of damaged rear axons.
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Guimin
Zhao, Wenxue
Yue, Ling
Min, Shujun
Yao, Jingchun
Abrégé
A use of a Jingfang preparation in preparation of a drug for preventing or treating hepatitis C virus (HCV). The Jingfang preparation is made from Root And Rhizome of Incised Notoptergium, Doubleteeth Pubescent Angelica Root, Indian Bread, Root of Divaricate Saposhnikovia, All-Grass of Fineleaf Schizonepeta, Szechuan Lovage Root, Platycodon Root, Root of Chinese Thorowax, Root of Grand Hogfennel, Fruit of Seville Orange, and Root of Ural Licorice, and can inhibit the activity of HCV and the expression of HCV-RNA in cells and decrease a level of DHCV-DNA in the serum of ducks infected with HCV in vivo.
A61P 1/16 - Médicaments pour le traitement des troubles du tractus alimentaire ou de l'appareil digestif des troubles de la vésicule biliaire ou du foie, p. ex. protecteurs hépatiques, cholagogues, cholélitholytiques
14.
PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING ALZHEIMER'S DISEASE
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Yao, Jingchun
Li, Honghua
Sun, Chenghong
Zhang, Guimin
Zhao, Tao
Abrégé
A pharmaceutical composition for preventing or treating Alzheimer?s disease and use thereof are disclosed and belong to the technical field of medicines. The pharmaceutical composition includes (Z)-3-(N-(3-bromo-4-fluorophenyl)-N?-hydroxyformamido)-4-(2-guanidinoethyl)amino)-1,2,5-oxadiazole and anhydroicaritin. A pharmacodynamic experiment proves that the pharmaceutical composition achieves a synergistic therapeutic effect on treating Alzheimer?s disease.
A61K 9/22 - Pilules, pastilles ou comprimés du type à libération prolongée ou discontinue
A61K 9/24 - Pilules, pastilles ou comprimés du type à libération prolongée ou discontinue en doses unitaires constituées de couches ou feuilletées
A61K 9/28 - DragéesPilules ou comprimés avec revêtements
A61K 9/48 - Préparations en capsules, p. ex. de gélatine, de chocolat
A61K 31/352 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à six chaînons avec un oxygène comme seul hétéro-atome d'un cycle condensés avec des carbocycles, p. ex. cannabinols, méthanthéline
A61P 25/28 - Médicaments pour le traitement des troubles du système nerveux des troubles dégénératifs du système nerveux central, p. ex. agents nootropes, activateurs de la cognition, médicaments pour traiter la maladie d'Alzheimer ou d'autres formes de démence
15.
USE OF TRADITIONAL CHINESE MEDICINE COMPOSITION IN PREPARATION OF DRUGS FOR TREATING NEUROGENIC PULMONARY EDEMA
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Guimin
Yao, Jingchun
Sun, Chenghong
Li, Honghua
Abrégé
A traditional Chinese medicine composition for treating neurogenic pulmonary edema. The traditional Chinese medicine composition is mainly prepared from Rhizoma seu Radix Notopterygii, Radix Angelicae Pubescentis, Poria, Radix Saposhnikoviae, Herba Schizonepetae, Rhizoma Chuanxiong, Radix Platycodi, Radix Bupleuri, Radix Peucedani, Fructus Aurantii, and Radix Glycyrrhizae. The traditional Chinese medicine composition can improve the lung index and lung wet weight/dry weight of rats with neurogenic pulmonary edema, and has a therapeutic effect on neurogenic pulmonary edema.
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Guimin
Yao, Jingchun
Li, Honghua
Sun, Chenghong
Zhao, Tao
Abrégé
A pharmaceutical composition for preventing or treating Alzheimer's disease and the use thereof, which belong to the technical field of medicine. The pharmaceutical composition contains (Z)-3-(N-(3-bromo-4-fluorophenyl)-N'-hydroxy carboxamido)-4-(2-guanidinoethyl)amino)-1,2,5-oxadiazole and anhydroicaritin. Pharmacodynamic experiments have proven that the pharmaceutical composition achieves a synergistic therapeutic effect on Alzheimer's disease.
A61K 31/352 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à six chaînons avec un oxygène comme seul hétéro-atome d'un cycle condensés avec des carbocycles, p. ex. cannabinols, méthanthéline
A61P 25/28 - Médicaments pour le traitement des troubles du système nerveux des troubles dégénératifs du système nerveux central, p. ex. agents nootropes, activateurs de la cognition, médicaments pour traiter la maladie d'Alzheimer ou d'autres formes de démence
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Guimin
Zhang, Hao
Yao, Jingchun
Yuan, Jiang
Zhao, Guifang
Li, Rui
Li, Guangyan
Zhao, Yun
Liang, Hongbao
Zhang, Zhenjun
Zhu, Xiangxia
Abrégé
A compound of formula I or a pharmaceutically acceptable salt thereof, and use thereof in a preparation for modulation of EGFR tyrosine kinase activity or prevention and treatment EGFR related diseases. An EGFR inhibitors of formula I has inhibitory activity against EGFR D770-N771 ins NPG and NPG/T790M kinases, and inhibitory effects on cell proliferation of EGFR-Del19/T790M/C797S kinases, KC-0122:Ba/F3EGFR-L858R/T790M/C797S trimutated cell lines, and KC-0116:Ba/F3EGFR-Del19/T790M/C797S trimutated cell lines.
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Guimin
Li, Xin
Liu, Donggaung
Abrégé
A traditional Chinese medicine composition, prepared from Herba Schizonepetae, Root of Divaricate Saposhnikovia, Radix Et Rhizoma Notopterygii, Radix Angelicae Pubescentis, Root of Chinese Thorowax, Root of Grand Hogfennel, Rhizoma Chuanxiong, Fruit of Seville Orange, Poria, Platycodon Root, and Root of Ural Licorice. The traditional Chinese medicine composition can reduce the number of coughs of a guinea pig model of cough variant asthma, reduce an eosinophil percentage in bronchoalveolar lavage fluid, reduce a serum eosinophil cationic protein level, and has a prevention and treatment effect on cough variant asthma.
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Guimin
Li, Tao
Guo, Jinjuan
Abrégé
A traditional Chinese medicine composition with a uric acid reducing effect. The traditional Chinese medicine composition is mainly prepared from Notopterygii rhizoma et radix, Angelicae pubescentis radix, Poria, Saposhnikoviae radix, Schizonepetae herba, Chuanxiong rhizoma, Platycodonis radix, Bupleuri radix, Peucedani radix, Aurantii fructus and Glycyrrhizae radix et rhizoma. The traditional Chinese medicine composition can obviously reduce the level of rat blood uric acid caused by the uricase inhibitor potassium oxonate, and can be used for preparing a drug for preventing and treating hyperuricemia or gout.
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Guimin
Li, Xin
Liu, Dongguang
Abrégé
A traditional Chinese medicinal composition is prepared from herba schizonepetae, radix saposhnikoviae, notopterygium root, radix angelicae pubescentis, radix bupleuri, common hogfennel root, rhizoma chuanxiong, fructus aurantii, poria cocos, radix platycodonis, and liquorice root. The traditional Chinese medicinal composition can reduce the cough frequency of a guinea pig model with cough variant asthma, a percentage of eosinophils in a bronchoalveolar lavage fluid, and a level of serum eosinophil cationic proteins, and has a prevention and treatment effect on the cough variant asthma.
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Hu, Lihong
Abrégé
A pyrrole-substituted indolone derivative or pharmaceutically acceptable salts thereof, and a preparation method therefor and application thereof. The pyrrole-substituted indolone derivative or pharmaceutically acceptable salts thereof is simple to synthesize, easy to prepare, rich in raw materials for synthesis, and has an inhibitory effect on a plurality of tyrosine kinases, especially has higher selective inhibitory activity against KDR (VEGFR2), and FLT3 and its mutants, and can avoid toxic side effects caused by inhibiting KDR.
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
A61P 35/02 - Agents anticancéreux spécifiques pour le traitement de la leucémie
C07D 403/06 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne carbonée ne contenant que des atomes de carbone aliphatiques
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhai, Lihai
Xia, Xianglai
Ma, Chao
Yu, Junhou
Liu, Zhong
Abrégé
Provided are a 1,2-bis(4-pyridyl)ethane-acipimox co-crystal and a preparation method therefor. The 1,2-bis(4-pyridyl)ethane-acipimox co-crystal is formed by combining acipimox and 1,2-bis(4-pyridyl)ethane according to a molar ratio of 2:1, and an X-ray diffraction pattern has characteristic peaks at 2θ angles of 9.88±0.2°, 9.1±0.2°, 13.92±0.2°, 24.56±0.2°, 26.12±0.2°, and 26.86±0.2° using Cu-Kα radiation. The co-crystal product is high in purity, high in stability and simple in preparation process.
C07D 241/24 - Atomes de carbone comportant trois liaisons à des hétéro-atomes avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile
C07D 401/06 - 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 deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Guimin
Du, Liping
Gao, Ximeng
Liu, Zhong
Abrégé
Disclosed are galantamine pamoate sustained-release microparticles for injection and a preparation method therefor. The microparticles comprise galantamine pamoate, a lactide-glycolide copolymer, and a weak alkaline additive. The microparticles are prepared by means of hot-melt extrusion combined with low-temperature pulverization technology. Compared with the prior art, the prepared particles have low burst release, sufficient drug release, low moisture content, simple preparation process, high product yield, high encapsulation rate, and are suitable for industrial production.
A61K 31/55 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol ou de poloxamères
A61P 25/28 - Médicaments pour le traitement des troubles du système nerveux des troubles dégénératifs du système nerveux central, p. ex. agents nootropes, activateurs de la cognition, médicaments pour traiter la maladie d'Alzheimer ou d'autres formes de démence
24.
TABLET OF STEROID CYP17 INHIBITOR SOLID DISPERSION AND PREPARATION METHOD THEREFOR
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Guimin
Hao, Guizhou
Ding, Bing
Chen, Yinghui
Abrégé
The present invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a tablet of a steroid CYP17 inhibitor solid dispersion and a preparation method therefor. The tablet is prepared by heating, melting and extruding abiraterone acetate, an antioxidant and copovidone using a hot melt extruder at 115℃-125℃ to prepare a solid dispersion, crushing the extrudate, then mixing the crushed extrudate with a surfactant and pharmaceutically acceptable supplementary materials and tabletting. The tablet has fast dissolution speed, good stability and process reproducibility and high bioavailability, and is suitable for scale production.
A61K 31/58 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes contenant des hétérocycles, p. ex. danazol, stanozolol, pancuronium ou digitogénine
A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. carbomères
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Guimin
Li, Weiqun
Wang, Haixiang
Abrégé
The present invention relates to the field of herbal medicine preparations, and disclosed thereby are a microcapsule preparation for eliminating food stagnation and relieving coughs in children and a preparation method therefor, the microcapsule preparation is made of extract fine powder for eliminating food stagnation and relieving coughs in children, a capsule material, an anti-sticking agent and a plasticizer. The preparation method for the microcapsule preparation for eliminating food stagnation and relieving coughs in children comprises the preparation of the extract fine powder for eliminating food stagnation and relieving cough of children and the preparation of micro capsules. The microcapsules for eliminating food stagnation and relieving coughs in children according to the present invention are spherical or spheroid, have low hygroscopicity, have good fluidity, and do not easily clump together. The obtained microcapsule preparation has obvious slow-release effects, has high bioavailability, is not affected by gastrointestinal rhythm, and may have the best effect with regards to treating a cough. At the same time, by means of the encapsulation of the capsule material, the undesirable smell inherent in the preparation for eliminating food stagnation and relieving coughs in children may be masked, thereby improving the taste and the compliance of sick children to using the medication.
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Yu, Chengbin
Wang, Xiujuan
Abrégé
A method for synthesizing an argatroban hydrate. A compound I argatroban monohydrate is obtained by using a compound II as a starting material and an organosilane compound as a reducing agent under the catalytic reduction of an organic amine salt and a nonmetallic boron compound. The method has mild reaction conditions, simple and convenient operation process, and low production cost; the prepared argatroban monohydrate has high purity and yield; and the ratio of the 21(R) and 21(S) isomers is in the range of 64 to 65 : 36 to 35, meeting the pharmaceutical standard.
C07K 5/068 - Dipeptides la chaîne latérale du premier amino-acide contenant plus de groupes amino que de groupes carboxyle, ou leurs dérivés, p. ex. Lys, Arg
C07D 401/12 - 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 deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhai, Lihai
Lu, Yuansheng
Ma, Chao
Xie, Yinjie
Liu, Yunna
Abrégé
Provided is a tegafur-1,2-bis(4-pyridyl)ethylene cocrystal. The present invention relates to the technical field of crystal form drug molecules. According to the tegafur cocrystal, Cu-Kα radiation is used, and an X-ray diffraction pattern represented in 2θ has characteristic peaks at 6.26+/−0.2°, 9.30+/−0.2°, 11.89+/−0.2°, 12.60+/−0.2°, 14.79+/−0.2°, 20.28+/−0.2°, 23.98+/−0.2° and 26.43+/−0.2°; the crystallographic measurement parameter is: a triclinic system with a chiral space group of P-1; and cell parameters are: a=5.1391(4) Å, b=9.7392(7) Å, c=13.9658(10) Å, α=96.008(6)°, β=92.368(7)°, γ=103.481(7)°, and unit cell volume V=674.44(9) Å 3. Also provided are a related preparation method and a use. The tegafur-1,2-bis(4-pyridyl)ethylene cocrystal is good in stability and has a high solubility and dissolution rate.
C07D 405/04 - Composés hétérocycliques contenant à la fois un ou plusieurs hétérocycles comportant des atomes d'oxygène comme uniques hétéro-atomes du cycle et un ou plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
C07C 235/46 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des atomes d'oxygène ayant des atomes de carbone de groupes carboxamide liés à des atomes de carbone de cycles aromatiques à six chaînons et des atomes d'oxygène, liés par des liaisons simples, liés au même squelette carboné avec des atomes de carbone de groupes carboxamide et des atomes d'oxygène, liés par des liaisons simples, liés à des atomes de carbone du même cycle aromatique à six chaînons non condensé ayant les atomes d'azote des groupes carboxamide liés à des atomes d'hydrogène ou à des atomes de carbone acycliques
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Guimin
Chen, Xiaowei
Li, Ze
Abrégé
Disclosed are an orlistat capsule and a preparation method therefor, pertaining to the technical field of pharmaceutical preparations. Orlistat forms with hydroxypropyl cellulose, leucine, and propylene carbonate into a complex, so as to reduce the particle size of the raw materials and improve the hydrophilicity, fluidity, and stability of the drug, thereby improving the stability of orlistat during preparation and storage. The preparation process is simple, and the prepared orlistat capsule dissolves quickly and has good stability.
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Guimin
Bai, Wenqin
Zheng, Yi
Abrégé
Provided is a 5-deoxy-D-ribose derivative (III), when the derivative (III) is used for preparing capecitabine, the stereoselectivity is good and the yield is high. Further provided is a preparation method of the derivative, wherein the preparation method comprises: step a: performing oxymethylation of 1-hydroxyl group of 5-deoxy-D-ribose; step b: protecting 2-, 3-hydroxyl groups with Fmoc-; and finally protecting the 1-group with acetylation. The method is simple and convenient to operate, does not need special equipment, and is suitable for industrial production.
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
C07H 13/12 - Composés contenant des radicaux saccharide estérifiés soit par l'acide carbonique ou ses dérivés, soit par des acides organiques, p. ex. acides phosphoniques par des acides comportant le groupe —X—C (=X)—X—, ou leurs halogénures, dans lesquels chaque X signifie de l'azote, de l'oxygène, du soufre, du sélénium ou du tellure, p. ex. acide carbonique, acide carbamique
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Guimin
Ma, Qingwen
Cheng, Guoliang
Abrégé
Disclosed is the use of a traditional Chinese medicine composition in the preparation of a drug for treating hyperlipidemia, wherein the traditional Chinese medicine composition is mainly prepared from the following components: Crataegi fructus, Alismatis rhizome, Artemisiae scopariae herba, Rhei radix et rhizoma, Cassiae semen, Cirsii herba, Atractylodis rhizome, Atractylodis macrocephalae rhizome, Polyporus, Bupleuri radix and Glycyrrhizae radix et rhizoma; and the composition further can comprise Ligustri lucidi fructus, Ecliptae herba, Lycii fructus, Trichosanthis fructus and Citri reticulatae pericarpium.
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Guimin
Wang, Zhaoqin
Abrégé
A tirofiban hydrochloride injection and a preparation method therefor, the injection comprising tirofiban hydrochloride, sodium alginate, a pH adjuster and water. The preparation method is as follows: first preparing a citric acid-sodium citrate buffer solution by dissolving citric acid and sodium citrate in 10-50% water, and then dissolving tirofiban hydrochloride and sodium alginate in water, mixing the two solutions, adjusting pH, filtering, aliquoting, sterilizing, inspecting by using light, and packaging.
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Guimin
Chen, Chengfu
Zhu, Jianbo
Abrégé
The present invention relates to the pharmaceutical synthesis field, and provides a method for synthesizing 5-isosorbide mononitrate by means of a micro-channel reactor. In the present invention, a nitrating reagent and isosorbide liquid are pumped into the micro-channel reactor respectively for mixing reaction; after the reaction is completed, a product flows out from an outlet of the micro-channel reactor, and is subjected to post-treatment, separation, and purification to obtain the target product 5-isosorbide mononitrate. According to the method provided in the present invention, reaction time is short, and compared with a conventional technology, the method is safe, and the yield of the 5-isosorbide mononitrate is greatly improved.
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Sun, Jianhe
Wang, Zhaoqin
Abrégé
The present invention relates to the field of medical preparations, and relates in particular to a ketorolac tromethamine tablet. In the present invention, ketorolac tromethamine is prepared into a solid dispersion which is then prepared into a tablet. The present invention greatly improves the dissolution rate of ketorolac tromethamine, while also effectively improving the stability thereof. Thus, ketorolac tromethamine is effectively prevented from generating impurities caused by factors such as light and heat, and the safety of the clinical medication is improved.
A61K 9/28 - DragéesPilules ou comprimés avec revêtements
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
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. carbomères
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Guimin
Zhu, Anguo
Liu, Dong
Abrégé
The present invention provides a method for synthesizing potassium oxonate. The method comprises the following steps: adding 2-carbamoylamino-2-oxoacetic acid, urea, and a catalyst to a solvent at room temperature, raising temperature to perform a cyclization reaction, performing detection until the reaction is finished, lowering temperature, adjusting the pH value of the reaction solution, forming a potassium salt, stirring and growing the crystal, then performing suction filtration, sequentially washing the filter cake with purified water and cold anhydrous alcohols, and then drying in vacuum, so as to obtain potassium oxonate. Compared with the prior art, in the whole process, the raw materials are simple and easily obtainable, the operations are easy, the reaction conditions are mild, the quality is stable, the yield is high, and the environment is not contaminated, the whole process being suitable for industrial production.
C07D 251/20 - Composés hétérocycliques contenant des cycles triazine-1, 3, 5 non condensés avec d'autres cycles comportant trois liaisons doubles entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques avec des atomes d'hydrogène ou de carbone liés directement à au moins un atome de carbone du cycle à un seul atome de carbone du cycle aucun atome d'azote n'étant lié directement à un atome de carbone du cycle
35.
Pegylated analogue protein or canine urate oxidase, preparation method and use thereof
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhang, Chun
Fan, Kai
Ma, Xuefeng
Yang, Li
Hu, Chunlan
Luo, Hua
Mei, Xiang
Abrégé
Provided are a PEGylated analogue protein of canine urate oxidase, preparation method and use thereof. The analogue protein of canine urate oxidase is a canine urate oxidase, or a chimeric protein comprising part of the amino acid sequence of a canine urate oxidase and part of the amino acid sequence of a human urate oxidase, or a mutant protein thereof. The PEGylated analogue protein of canine urate oxidase and pharmaceutical compositions thereof according to the present invention can be used for the prevention and/or treatment of hyperuricemia and chronic gout.
A61K 48/00 - Préparations médicinales contenant du matériel génétique qui est introduit dans des cellules du corps vivant pour traiter des maladies génétiquesThérapie génique
C12N 9/96 - Stabilisation d'une enzyme par formation d'un adduct ou d'une compositionFormation de conjugaisons d'enzymes
A61K 47/48 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p.ex. supports, additifs inertes l'ingrédient non actif étant chimiquement lié à l'ingrédient actif, p.ex. conjugués polymère-médicament
C12N 9/06 - Oxydoréductases (1.), p. ex. luciférase agissant sur des composés contenant de l'azote comme donneurs (1.4, 1.5, 1.7)
A61K 38/00 - Préparations médicinales contenant des peptides
36.
Homodimer of insulinotropic peptide analogues and method for preparation thereof and use thereof
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Fan, Kai
Zhao, Zhiquan
Chen, Yong
Zhang, Chun
Wang, Lin
Abrégé
Provided is a homodimer of insulinotropic peptide analogues and method for preparation thereof and use thereof, wherein the insulinotropic peptide analogue comprises GLP-1 and Exendin-4. The homodimer of insulinotropic peptide analogues of the invention is made by conjugating two identical insulinotropic peptide analogue molecules at the C-terminal Cys residues via disulfide bond or PEG molecule. The homodimer of insulinotropic peptide analogues of the invention has superior stability and biological activity in vivo, and prolonged half-life in the circulation, and can be used for the preparation of hypoglycemic drugs.
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Fan, Kai
Zhang, Chun
Ma, Xuefeng
Mei, Xiang
Hu, Chunlan
Abrégé
The present invention provides a humanized recombinant uricase and mutants thereof, wherein the humanized recombinant uricase is a chimeric protein which comprises amino acids of non-human mammal uricase and amino acids of human uricase. The humanized recombinant unease and mutants thereof have reduced immunogenicity in human, and can be used for the treatment of hyperuricemia and gout.
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Hao, Wei-Hua
Lin, Tsung-Hsin
Lu, Ta-Chien
Abrégé
A controlled release carvedilol formulation for less frequent, preferably once daily administration is described. The controlled release formulation comprises a therapeutically effective amount of carvedilol or a pharmaceutically acceptable salt thereof, a matrix forming polymer, a solubility enhancer and a pharmaceutically acceptable carrier. In one embodiment, a controlled release formulation having a therapeutically effective amount of carvedilol is contained in two or more subunits having different release profiles. The controlled release formulation is usable in the treatment and/or prophylaxis of one or more conditions such as cardiovascular disorders.
A61K 31/403 - 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 carbocycles, p. ex. carbazole
39.
Synthetic method for montelukast sodium intermediate
Shandong New Time Pharmaceutical Co., Ltd. (Chine)
Inventeur(s)
Zhao, Zhiquan
Wang, Haixin
Wang, Zengxue
Abrégé
A synthesis method for preparing Montelukast sodium intermediate 2-(2-(3-(2-(7-chloro-2-quinolyl)vinyl)phenyl-3-oxopropyl)phenyl) propanol is provided. In this method, the target compound is prepared by condensing the starting materials 7-chloroquinaldine and 3-cyanobenzaldehyde, and then reacting the resultant product with 2-(2-ortho-(2-haloethyl)-phenylpropyl)tetrahydropyrane ether. The present invention can easily obtain start materials and is applicable for mass production.
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhao, Zhiquan
Abrégé
An anti-tumor pharmaceutical composition or packaged medicinal kit containing burdock aglycone and tyrosine kinase inhibitor. The joint application of burdock aglycone and tyrosine kinase inhibitor used in the present invention exhibits significant coordination effects in inhibiting tumors, especially in leukemia and solid tumors such as non-small-cell lung cancer, and reduces the poisonous side effect and drug tolerance of tyrosine kinase inhibitor.
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Zhao, Zhiquan
Wang, Haixin
Wang, Zengxue
Abrégé
A process for preparing montelukast sodium intermediate 2-(2-(3-(2-(7-chloro-2-quinolyl)ethenyl)phenyl-3-oxopropyl)phenyl) propanol is provided. In the process, the target compound is prepared by condensing the starting materials 7-chloroquinaldine and 3-cyanobenzaldehyde, and then reacting with 2-(2-ortho-(2-haloethyl)-phenylpropyl)tetrahydropyrane ether.
SHANDONG NEW TIME PHARMACEUTICAL CO., LTD. (Chine)
Inventeur(s)
Fan, Kai
Zhao, Zhiquan
Abrégé
A chimeric protein containing neutrophil inhibitory factor and hirugen, the chimeric protein having an amino acid sequence that includes FPRPGSGG (SEQ ID NO:21) Also provided is a pharmaceutical composition comprising the chimeric protein, which can be used for treating or preventing cerebral injury and cerebral edema, or for inhibiting platelet aggregation.
brevets
