46 results about "Enediyne" patented technology

Enediyne compounds having a structure according to formula (I), where R0, R2, R3, R4, R5, R6, and R7 are defined herein, can be used in chemotherapeutic drugs, especially in conjugates, for the treatment of diseases such as cancer.

A pharmaceutical compositions comprises a compound of formula (I): or a pharmaceutically acceptable salt thereof: wherein R1═R2 ═H; or R1 and R2 together form a moiety represented by the formula R3 represents a substituted or unsubstituted alkyl having 4-30 carbon atoms, or a substituted or unsubstituted aryl group having 3-30 carbon atoms; and R4 represents a substituted or unsubstituted aryl group having 3-30 carbon atoms; with the proviso that R3 is not butyl, pentyl, tetrahydropyranyloxymethyl, tetrahydropyranyloxypropyl or phenyl when R1═R2═H and R4 is o-cyanophenyl,; and with the proviso that R3 is not butyl when R1═R2═H and R4 is phenyl. The pharmaceutical composition may be used to treat a subject afflicted with a tumor / cancer by inhibiting topoisomerase I activities or blocking the S phase or G2 / M phase of the tumor / cancer cells.

This invention provides aryl-substituted acyclic enediyne compounds of formula (I):or a pharmaceutically acceptable salt or solvate thereof,whereinR1=R2=H; or R1 and R2 together form a moiety represented by the formulaR3 represents a substituted or unsubstituted alkyl having 4-30 carbon atoms, or a substituted or unsubstituted aryl group having 3-30 carbon atoms; andR4 represents a substituted or unsubstituted aryl group having 3-30 carbon atoms;with the proviso that R3 is not butyl, pentyl, tetrahydropyranyloxymethyl, tetrahydropyranyloxypropyl or phenyl when R1=R2=H and R4 is o-cyanophenyl,; and with the proviso that R3 is not butyl when R1=R2=H and R4 is phenyl.The compounds of formula (I) are found to have inhibitory activities against topoisomerase I or act as a S phase or G2 / M phase blocker.

Enediyne compounds having a structure according to formula (I), where R0, R2, R3, R4, R5, R6, and R7 are defined herein, can be used in chemotherapeutic drugs, especially in conjugates, for the treatment of diseases such as cancer.

Disclosed are a novel aromatic enediyne derivative, an organic semiconductor thin film using the same, and an electronic device. Example embodiments pertain to an aromatic enediyne derivative which enables the formation of a chemically and electrically stable and reliable semiconductor thin film using a solution process, e.g., spin coating and / or spin casting, at about room temperature when applied to devices, an organic semiconductor thin film using the same, and an electronic device including the organic semiconductor thin film. A thin film having a relatively large area may be formed through a solution process, therefore simplifying the manufacturing process and decreasing the manufacturing cost. Moreover, it is possible to provide an organic semiconductor that may be effectively applied to various fields including organic thin film transistors, electroluminescent devices, solar cells, and memory.

The invention relates to fusion protein ER (Fv-LDP) and reinforced fusion protein ER (Fv-LDP-AE) thereof. The fusion protein consists of anti-EGFR single chain antibody scFv, lidamycin apoprotein LDP and carboxyl terminal hexahistine; the overall length of gene is 1089 bp, and 363 amino acids are coded; the reinforced fusion protein comprises fusion protein ER (scFv-LDP) (molecular weight about 38 kDa) and activated enediyne chromophore AE (molecular weight 843 Da); in vivo test and in vitro test demonstrate that the fusion protein and the reinforced fusion protein thereof have strong killing effects on EGFR over-expression tumor cell, have significant efficacies on animal in vivo test, and can be developed into targeting drug of miniaturized antibody with high clinical efficiency.

Disclosed are aromatic enediyne derivatives, methods of manufacturing organic semiconductor thin films from such aromatic enediyne derivatives, and methods of fabricating electronic devices incorporating such organic semiconductor thin films. Aromatic enediyne derivatives according to example embodiments provide improved chemical and / or electrical stability which may improve the reliability of the resulting semiconductor devices. Aromatic enediyne derivatives according to example embodiments may also be suitable for deposition on various substrates via solution-based processes, for example, spin coating, at temperatures at or near room temperature to form a coating film that is then heated to form an organic semiconductor thin film. The availability of this reduced temperature processing allows the use of the aromatic enediynes derivatives on large substrate surfaces and / or on substrates not suitable for higher temperature processing. Accordingly, the organic semiconductor thin films according to example embodiments may be incorporated in thin film transistors, electroluminescent devices, solar cells, and memory devices.

The invention provides novel tetradentate enediyne ligands that are themselves thermally stable, yet react at about room temperature or slightly higher upon addition of metal ions or under photothermal conditions. In another aspect of the invention, a method of treating a disorder in a mammal comprising administering a therapeutically effective amount of a compound or composition is provided. In addition, the free ligand can be delivered to the mammal prior to complexation to metals, such that the ligand is exposed to a metal in the body and forms a metal complex in vivo. Furthermore, a metal complex of the invention can be administered to the mammal such that the complex exchanges the first metal center with another endogenous metal in order to form a second metal complex in vivo. The second metal complex is capable of forming a benzenoid diradical under physiological conditions and / or under photothermal conditions.

A chemical composition and method of use of the composition is described. The chemical composition includes an aza-enediyne, aza-enyne allene, or an aza-diallene. These compound are preferably non-hydrolyzable, cationic compounds that bind to nucleic acids. In addition it is believed that these compounds may undergo chemical reactions in the presence of a nucleic acid to generate reactive intermediates that cleave nucleic acids.

The invention relates to fusion protein (Arg)9-LDP and reinforced fusion protein (Arg)9-LDP-AE thereof. The fusion protein consists of cell-penetrating peptide (Arg)9, lidamycin apoprotein LDP and carboxyl terminal hexamerichistidine tail, wherein the full length of gene is 387bp, and 129 amino acids are encoded; the reinforced fusion protein is formed by fusion protein (Arg)9-LDP with molecular weight of about 14.5kDa and activated enediyne chromophore AE with molecular weight of 843Da; in-vivo and in-vitro experiment results prove that the fusion protein and reinforced fusion protein thereof have intense killing effect on glioma cells, and have remarkable curative effect in in-vivo animal experiments, and are expected to be developed into clinic efficient glioma treating medicament.

Emulsions are prepared by heating and polymerizing a mixture containing (i) a non-crosslinked silicone polyether; (ii) optionally, a cosurfactant which can be a monohydroxy alcohol, diol, triol, or glycol ether; (iii) an =Si-H containing polysiloxane; (iv) a mono-alkenyl polyether; (v) an alpha,omega-diene, alpha,omega-diyne, or alpha,omega-ene-yne; (vi) optionally, a silicone oil such as (a) a low molecular weight linear or cyclic volatile methyl siloxane, or (b) a low molecular weight linear or cyclic volatile or non-volatile alkyl or aryl siloxane; (vii) a platinum catalyst; and (viii) water.

Disclosed are aromatic enediyne derivatives, methods of manufacturing organic semiconductor thin films from such aromatic enediyne derivatives, and methods of fabricating electronic devices incorporating such organic semiconductor thin films. Aromatic enediyne derivatives according to example embodiments provide improved chemical and / or electrical stability which may improve the reliability of the resulting semiconductor devices. Aromatic enediyne derivatives according to example embodiments may also be suitable for deposition on various substrates via solution-based processes, for example, spin coating, at temperatures at or near room temperature to form a coating film that is then heated to form an organic semiconductor thin film. The availability of this reduced temperature processing allows the use of the aromatic enediynes derivatives on large substrate surfaces and / or on substrates not suitable for higher temperature processing. Accordingly, the organic semiconductor thin films according to example embodiments may be incorporated in thin film transistors, electroluminescent devices, solar cells, and memory devices.

The invention relates to Micromonospora echinospora var. Sheshanensis C-3509 generating enediyne antitumor antibiotics. Experimental results show that the fermentation liquor of the Micromonospora echinospora var. Sheshanensis C-3509 is tested positive by a spermatogonium method, and is subjected to isolation and purification to obtain high-efficiency antitumor bioactive substances, namely four compositions of Calicheamicins gamma1, gamma1, beta1 and beta1; therefore, the Micromonospora echinospora var. Sheshanensis C-3509 is hopeful to be used for preparing the enediyne antitumor antibiotics.

A fusion gene encoding the fusion protein LhFVII-LDP is formed by linking the gene encoding the light chain of human blood coagulation factor VII and the gene encoding lidamycin prosthetic protein, and its nucleotide sequence is shown in SEQ ID NO. 3. A recombinant plasmid expressing the fusion protein LhFVII-LDP contains a fusion gene encoding the fusion protein LhFVII-LDP. The fusion protein LhFVII-LDP is expressed from the above-mentioned recombinant plasmid, and its amino acid sequence is shown in SEQ ID NO.4 in the sequence listing. The enhanced fusion protein LhFVII-LDP-AE is composed of the fusion protein LhFVII-LDP whose amino acid sequence is shown in SEQ ID NO.4 in the sequence listing and the enediyne chromophore AE. The fusion protein LhFVII-LDP and the strengthened fusion protein LhFVII-LDP-AE can be used in the preparation of medicines for treating tumors.

The present invention concerns antibody-conjugate having general structure (2):AB-[(L6)-{Z-(L1)n-(L2)o-(L3)p-(L4)q-D}xx]yy   (2)wherein AB is an antibody capable of targeting Trop-2-expressing tumours and D is selected from the group consisting of taxanes, anthracyclines, camptothecins, epothilones, mytomycins, combretastatins, vinca alkaloids, maytansinoids, enediynes such as calicheamicins, duocarmycins, tubulysins, amatoxins, bleomycins, dolastatins and auristatins, pyrrolobenzodiazepine dimers, indolinobenzodiazepine dimers, radioisotopes, therapeutic proteins and peptides (or fragments thereof), kinase inhibitors, MEK inhibitors, KSP inhibitors, and analogues or prodrugs thereof. These antibody-conjugates exhibit an improved therapeutic index. The invention further concerns a process for preparing the antibody-conjugate according to the invention, a method for targeting Trop-2-expressing cells, medical uses of the antibody-conjugates according to the invention.

The invention relates to a novel acetylene compound applied to an anti-cancer drug as well as a preparation method and application thereof. The invention provides an acetylene compound of which the structural formula is as shown in the specification, wherein R represents a functional group; R=R, CR1R2R3, (CR1R2)nX or NR1R2; R, R1, R2 and R3 are hydrogen, halogen, C1-C24 alkyl chains, an aromatic group and a heterocyclic group; n is 1-6; X is amino, an ether group, an amidogent, sulfydryl, phosphino, halogen or an ester group; the aromatic group is phenyl, naphthyl, pyrenyl, anthryl, alkyl or halogen; the heterocyclic group is pyrrole, thiophene, pyridine, piperazine, pyran, furfuran, imidazole, parazole or morpholine. The experiment proves that the acetylene can lead obvious chain interruption of DNA and apoptosis of tumor cells. The acetylene compound proves that the synthetic acetylene has high biological activity.

The invention relates to a novel synergetic medical compound being capable of suppressing growth of tumors, which consists of an enediyne drug and an alkylated chemotherapeutic drug, i.e. lidamycin and temodar; relevant researches prove that the medical compound can synergetically resist the multiplication of the tumor cells, induce apoptosis and suppress angiogenesis; in vivo test has an obvious curative effect on nude mice transplanted tumor of the human neuroglioma U87 cells. The medical compound has an enhanced function of suppressing the growth of tumors and angiogenesis in tumor tissues, thus displaying a synergetic tumor suppressing effect and having good application prospect.

The invention provides two eneyne glucoside ester compounds of 3S,8S-dihtdroxydec-9-en-4,6-yne 1-O-(6'-O-caffeyl)-beta-D-glucopyranoside,1 and 3S,8S-dihtdroxydec-9-en-4,6-yne 1-O-(2'-O-caffeyl)-beta-D-glucopyranoside,2 shown in the structural formula I, a drug composition composed of therapeutically effective amount of the compound 1 or / and the compound 2 and a pharmaceutical carrier or an excipient, a preparation method of the compound 1 or / and the compound 2 and the drug composition thereof, and application of the compound 1 or / and the compound 2 and the drug composition for preparing drugs for treating human diseases particularly the viral hepatitis type B.

The invention relates to the technical field of identification of traditional Chinese medicinal materials, in particular to an identification method of Campanumoea javanica and Codonopsis pilosula, which comprises an HPLC identification step of establishing an HPLC characteristic chromatogram of an HPLC sample and an HPLC reference substance, and enabling the HPLC reference substance to comprises 9-(2-tetrahydropyran)-8E-ene-4, 6-diyne-3-nonanol. According to the scheme, the technical problem that the Campanumoea javanica and the Codonopsis pilosula cannot be effectively and accurately identified in the prior art is solved. The establishment of an exclusive identification method for Campanumoea javanica participating in the same-family plant Codonopsis pilosula medicinal material has important significance for ensuring the safety and effectiveness of related clinical medication.

Disclosed are aromatic enediyne derivatives, methods of manufacturing organic semiconductor thin films from such aromatic enediyne derivatives, and methods of fabricating electronic devices incorporating such organic semiconductor thin films. Aromatic enediyne derivatives according to example embodiments provide improved chemical and / or electrical stability which may improve the reliability of the resulting semiconductor devices. Aromatic enediyne derivatives according to example embodiments may also be suitable for deposition on various substrates via solution-based processes, for example, spin coating, at temperatures at or near room temperature to form a coating film that is then heated to form an organic semiconductor thin film. The availability of this reduced temperature processing allows the use of the aromatic enediynes derivatives on large substrate surfaces and / or on substrates not suitable for higher temperature processing. Accordingly, the organic semiconductor thin films according to example embodiments may be incorporated in thin film transistors, electroluminescent devices, solar cells, and memory devices.

Five protein families cooperate to form the warhead structure that characterizes enediyne compounds, both chromoprotein enediynes and non-chromoprotein enediynes. The protein families include a polyketide synthase and thioesterase protein which form a polyketide synthase catalytic complex involved in warhead formation in enediynes. Genes encoding a member of each of the five protein families are found in all enediyne biosynthetic loci. The genes and proteins may be used in genetic engineering applications to design new enediyne compounds and in methods to identify new enediyne biosynthetic loci.

Enediyne compounds of the formula: (1) characterized in that the structure thereof is very simple and the production process is easy, and that the molecular length thereof is shorter than those of compounds having been proposed. Consequently, electrode assemblies comprising any of these enediyne compounds are highly promising in the application to nanomolecular wiring (nanomolecular wire) whose production has been difficult.

The invention relates to the use of 1,5-enediyne compounds of formula (I) as curing agents in polymeric systems. In particular the invention relates to a curable composition comprising a curing agent of formula (I) and a polymer suitable to be cross-linked and to the cured article obtained therefrom.

The invention relates to a method for determining the activity of an enzyme or enediyne capable of altering the structure of a “substrate” nucleic acid from a first to a second state wherein the activity of the enzyme or enedyine is monitored using a chemiluminescent label that is either attached to the “substrate” nucleic acid or an oligonucleotide which is complementary thereto or the enzyme or enediyne product thereof.

The invention relates to fusion protein (Arg)9-LDP and reinforced fusion protein (Arg)9-LDP-AE thereof. The fusion protein consists of cell-penetrating peptide (Arg)9, lidamycin apoprotein LDP and carboxyl terminal hexamerichistidine tail, wherein the full length of gene is 387bp, and 129 amino acids are encoded; the reinforced fusion protein is formed by fusion protein (Arg)9-LDP with molecular weight of about 14.5kDa and activated enediyne chromophore AE with molecular weight of 843Da; in-vivo and in-vitro experiment results prove that the fusion protein and reinforced fusion protein thereof have intense killing effect on glioma cells, and have remarkable curative effect in in-vivo animal experiments, and are expected to be developed into clinic efficient glioma treating medicament.

The invention provides a compound 8S-Deca-9-en-4,6-diyne-1,8-diol, 1 shown in structural formula (I) as well as a compound 1 containing 8S-Deca-9-en-4,6-diyne-1,8-diol as an active ingredient and pharmaceutical composition containing a pharmaceutically acceptable carrier or excipient. The invention further provides preparation methods of the compound and the pharmaceutical composition containing the compound and applications of the compound and the pharmaceutical composition in preparation of drugs for treating human diseases, especially in preparation of drugs for resisting viral hepatitis B.

Enediyne compounds of the formula: (1) characterized in that the structure thereof is very simple and the production process is easy, and that the molecular length thereof is shorter than those of compounds having been proposed. Consequently, electrode assemblies comprising any of these enediyne compounds are highly promising in the application to nanomolecular wiring (nanomolecular wire) whose production has been difficult.

A chemical composition and method of use of the composition is described. The chemical composition includes an aza-enediynes, aza-enyne allenes, or an aza-diallenes. These compound are preferably non-hydrolyzable, cationic compounds that bind to nucleic acids. In addition it is believed that these compounds may undergo chemical reactions in the presence of a nucleic acid to generate reactive intermediates that cleave nucleic acids.

The invention provides novel tetradentate enediyne ligands that are themselves thermally stable, yet react at about room temperature or slightly higher upon addition of metal ions or under photothermal conditions. In another aspect of the invention, a method of treating a disorder in a mammal comprising administering a therapeutically effective amount of a compound or composition is provided. In addition, the free ligand can be delivered to the mammal prior to complexation to metals, such that the ligand is exposed to a metal in the body and forms a metal complex in vivo. Furthermore, a metal complex of the invention can be administered to the mammal such that the complex exchanges the first metal center with another endogenous metal in order to form a second metal complex in vivo. The second metal complex is capable of forming a benzenoid diradical under physiological conditions and / or under photothermal conditions.