Abstract: Disclosed are an Hsp90 inhibitor and a preparation method and use thereof. The Hsp90 inhibitor is 2-(4-(3-acetylcarnitineacyloxy)cyclohexylamino)-4-(1-(3,6,6-trimethyl-4-oxy-4,5,6,7-tetrahydroindazole))benzamide. The Hsp90 inhibitor has good water solubility and high bioavailability, and can effectively inhibit the proliferation of cancer cells, such as leukemia, cervical cancer, breast cancer, human laryngeal epithelial carcinoma, or malignant melanoma cells. It can also effectively inhibit the activity of herpes simplex virus. The maximal non-toxic concentration of the Hsp90 inhibitor on normal cells is a high, and the Hsp90 inhibitor only has specific inhibition effect on cancer cells.
Abstract: Disclosed are an anti-bFGF humanized double-stranded antibody with stable disulfide bond, the preparation method and the applications thereof. The amino acid sequence of the anti-bFGF humanized ds-Diabody is shown in SEQ ID NO.1. The nucleotide sequence of gene encoding the anti-bFGF humanized ds-Diabody is shown in SEQ ID NO.2. By site-directed mutation, two cysteine residues are introduced into VL and VH domain of anti-bFGF Diabody, thus introducing the disulfide bond and form ds-Diabody. It is shown by experiments that the obtained ds-Diabody has the following advantages: enhanced stability; better affinity when binding to the specific antigen bFGF; moderate relative molecular weight, good tumor targeting, more powerful in tumor tissue penetration, and higher blood clearance rate, showing a broad application prospects in the clinic diagnosis and tumor therapy.
Type:
Grant
Filed:
August 20, 2012
Date of Patent:
March 1, 2016
Assignee:
Jinan University
Inventors:
Ning Deng, Haowu Jiang, Zhongkui Kang, Hong Wang, Qifang Song
Abstract: Disclosed are an anti-bFGF humanized double-stranded antibody with stable disulfide bond, the preparation method and the applications thereof. The amino acid sequence of the anti-bFGF humanized ds-Diabody is shown in SEQ ID NO. 1. The nucleotide sequence of gene encoding the anti-bFGF humanized ds-Diabody is shown in SEQ ID NO. 2. By site-directed mutation, two cysteine residues are introduced into each single-stranded antibody, thus introducing the disulfide bond and form ds-Diabody. It is shown by experiments that the obtained ds-Diabody has the following advantages: enhanced stability; better affinity when binding to the specific antigen bFGF; moderate relative molecular weight, good tumor targeting, more powerful in tumor tissue penetration, and higher blood clearance rate, showing a broad application prospects in the clinic diagnosis and tumor therapy.
Type:
Application
Filed:
August 20, 2012
Publication date:
November 27, 2014
Applicant:
JINAN UNIVERSITY
Inventors:
Ning Deng, Haowu Jiang, Zhongkui Kang, Hong Wang, Qifang Song
Abstract: The present invention provides pyrazine derivatives of formula I and pharmaceutically acceptable salts thereof, wherein the designation of R1, R2, R3 and R4 is provided herein. The invention also provides syntheses for preparation of such compounds. The invention further provides methods of use of these compounds and pharmaceutical compositions containing them for treatment and/or prevention of diseases and for manufacture of medicaments. These compounds and pharmaceutical compositions have antioxidative and thrombolytic effects, and thus can be used for the treatment and/or prevention of cerebral stroke caused by ischemia, and used for manufacture of medicaments for the treatment and/or prevention of nervous system diseases caused by excessive amount of radicals and/or thrombosis, infectious diseases, metabolic system diseases, cardiovascular and cerebrovascular diseases, and age-related degenerative diseases.
Abstract: The present invention provides novel nitrones, their preparation and use. The novel compounds have the following formula: I The compounds of the present invention have strong antioxidative activity, and are thrombolytic. These compounds can be used to treat and/or prevent diseases caused by overproduction of free radicals and/or formation of thrombus.
Type:
Grant
Filed:
April 16, 2009
Date of Patent:
March 26, 2013
Assignee:
Jinan University
Inventors:
Yuqiang Wang, Jie Jiang, Pei Yu, Yewei Sun, Linda Wang, Zaijun Zhang
Abstract: The present invention provides pyrazine derivatives of formula I and pharmaceutically acceptable salts thereof, wherein the designation of R1, R2, R3 and R4 is provided herein. The invention also provides syntheses for preparation of such compounds. The invention further provides methods of use of these compounds and pharmaceutical compositions containing them for treatment and/or prevention of diseases and for manufacture of medicaments. These compounds and pharmaceutical compositions have antioxidative and thrombolytic effects, and thus can be used for the treatment and/or prevention of cerebral stroke caused by ischemia, and used for manufacture of medicaments for the treatment and/or prevention of nervous system diseases caused by excessive amount of radicals and/or thrombosis, infectious diseases, metabolic system diseases, cardiovascular and cerebrovascular diseases, and age-related degenerative diseases.