77 results about "Nitrosourea" patented technology

Disclosed is an anti solid tumor medicine composition, which comprises medicinal adjuvant and DNA restoring enzyme inhibitor and / or Nitrosoureas anti-cancer drugs, wherein the DAN restoring enzyme inhibitor is selected from methoxamine, hydroxylamine and their analogues, which can effectively destroy the DNA restoring function in the tumor cells, and lower the survivability of tumor cell to Semustine anti-cancer drugs and their analogues, the medicinal adjuvant is biological compactable, degradable and absorbing macromolecular polymer, which can slowly release the DNA restoring enzyme inhibitor onto tumor partially during the degradation and absorption process, thus the whole body toxicity reaction is reduced appreciably , and the effective medicinal concentration can be sustained to the tumor partially. By dispensing the composition to the tumor partially, the whole body toxicity reaction of Nitrosoureas anti-cancer drugs and / or DNA restoring enzyme inhibitor can be lowered, selectively increase the tumor local medicinal concentration, and the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation can be improved.

An anticancer in vivo implant applied locally is prepared from the anticancer nitrosourea-type medicine, the anticancer synergist chosen from nitrogen mustard compound, mitotic inhibitor and antimetabolic anticancer medicine, and the biocompatible and biodegradable high-molecular polymer as medicinal additive.

The invention is directed to an improved drug delivery system that includes a micelle, comprising polyethylene glycol and a lipid component, and a pharmaceutical agent dispersed in the lipid component. The delivery system may also include a targeting ligand. The micelle delivery system of the invention is capable of stabilizing, inter alia, poorly soluble pharmaceutical agents and increasing their delivery efficacy. Appropriate pharmaceutical agents useful in the system of the invention include anti-inflammatory agents, agents for photodynamic therapy, anti-tumor agents, anti-neoplastic agents, anti-metastatic agents, and imaging agents, as well as hydrophobized derivatives thereof. Specifically, the pharmaceutical agent can be porphyrin, chlorine-6-trimethyl ester, tamoxifen, paclitaxel, 1,3-bis(2-chloroethyl)-1-nitrosourea, camptothecin, ellipticine, rhodamine, dequalinium, diphenylhexatriene, vitamin K3, diethylene triamine pentaacetic acid, or a functional derivative thereof. The micelles in the system of the invention have low critical micellar concentration and high kinetic stability, which provides great advantages in biodistribution, for example, accumulation at the site of a tumor.

The invention provides an anti-cancer medicine composition, with comprises medicinal adjuvant and DNA restoring enzyme inhibitor containing effective anticancer constituents, wherein the DNA restoring enzyme inhibitor is selected from poly (ADP-ribose) poly enzyme inhibitor and / or DNA-dependent protein kinase inhibitor, which can effectively destroy the DNA restoring function in the tumor cells, and lower the survivability of tumor cell to Nitrosoureas anti-cancer drugs and their analogues, and the medicinal adjuvant mainly comprises biological compactable, degradable and absorbing macromolecular polymers, which can slowly release the DNA restoring enzyme inhibitor onto tumor partially during the degradation and absorption process, thus the whole body toxicity reaction is reduced appreciably , and the effective medicinal concentration can be sustained to the tumor partially. The anti-cancer medicinal composition also contain Nitrosoureas anti-cancer drugs and their analogues, by dispensing the composition to the tumor partially, the whole body toxicity reaction of Nitrosoureas anti-cancer drugs and / or DNA restoring enzyme inhibitor can be lowered, and the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation can be improved.

The present invention relates to an anticancer medicine composition and belongs to the field of medicine technology. The anticancer medicine composition contains topomerase inhibitor and medicinal supplementary material. The topomerase inhibitorcan inhibit intracellular DNA repair function and reduce the tolerance one tumor cell on anticancer nitrosourea medicine; and the medicine supplementary material is mainly degradable biocompatible polymer. During the degrading and absorption process of the supplementary material, the anticancer medicine is released slowly to the tumor part, and this can lower the systemic toxic reaction while maintaining local effective medicine concentration. The anticancer medicine composition contains also anticancer nitrosourea medicine, and is set to the tumor part locally to enhance the treatment effect.

The present invention relates to an anticancer medicine composition and belongs to the field of medicine technology. The anticancer medicine composition contains tetrazine medicine and medicinal supplementary material. The tetrazine medicinecan inhibit intracellular DNA repair function and reduce the tolerance one tumor cell on anticancer nitrosourea medicine; and the medicine supplementary material is mainly degradable biocompatible polymer. During the degrading and absorption process of the supplementary material, the anticancer medicine is released slowly to the tumor part, and this can lower the systemic toxic reaction while maintaining local effective medicine concentration. The anticancer medicine composition contains also anticancer nitrosourea medicine, and is set to the tumor part locally to enhance the treatment effect.

The invention relates to novel chloroethyl nitrosourea with anticancer activity and a synthesizing method thereof. The chloroethyl nitrosourea is a compound with a structure of the general formula (I), wherein n is an integer of 2 to 6. The chloroethyl nitrosourea can be used for treating gliomatosis cerebri, colon cancer and leukemia; compared with the existing nitrosourea-type anticancer medicine, the drug resistance is lower, the chemical therapy effect is better, the preparation method is simple in operation, the reaction yield is high, the toxicity is small, the cost is low, the method is suitable for the industrialized production, the development prospect is wide, and the application value is good.

The invention concerns a pharmaceutical composition comprising at least one stimulator of the immune cell functions and at least one substance inhibiting the cell proliferation and / or inducing cell death. In a preferred embodiment the stimulator of the function of the immune system and / or the immune cells are antagonists of TGF-beta selected from the group of oligonucleotides hybridizing with an area of the messenger RNA and or DNA encoding TGF-beta and the at least one substance inhibiting cell proliferation and / or inducing cell death is selected from the group of temozolomide, nitrosoureas, Vinca alkaloids, antagonists of the purine and pyrimidines bases, cytoststatic active antibiotics, caphthotecine derivatives, anti estrogens, anti-androgens and analogs of gonadotropin releasing hormon.

The invention relates to novel beta-chloroethylnitrosourea compounds, and a synthesis method and application thereof. The structure of the beta-chloroethylnitrosourea compounds is disclosed as general formula (II). The in-vitro antitumor screening test on the compounds disclosed as general formula II proves that the compounds disclosed as general formula I have obvious inhibiting action on human cerebral nerve glioma cells SF763, SF767, SF126 and SF188, human colon cancer cell HT29, mouse leukaemia cell L1210 and many other tumor cell lines and have higher tumor inhibiting activity than the existing CENU and CENU / O6-benzylguanine combined medicine.

The invention provides a wheat anther differentiation culture medium formula. The culture medium formula proportionally comprises KNO3, C8H7O2K, (NH4)2SO4, KH2PO4, CaCl2, MgSO4, Na2-EDTA, FeSO4.7H2O, MnSO4.4H2O, ZnSO4.7H2O, H3BO3, KI, CuSO4.5H2O, Na2Mo4.2H2O, CoCl2.6H2O, glycine, folic acid, methyl-nitrosourea, alanine, lysine, vitamin B1, vitamin B6, 3-picolinic acid, sucrose, gelling agent, NAA, KT, prohexadione calcium, sorbitol, protein hydrolysate, colchicine and biotin. The culture medium has the advantages of efficiently improving the differentiation rate of the wheat anther callus seedlings and reducing the ablation rate, and the wheat anther culture efficiency can be obviously improved.

The present invention relates to the combination of PM01183 with several anticancer drugs, in particular other anticancer drugs selected from antitumor platinum coordination complexes, antimetabolites, mitotic inhibitors, anticancer antibiotics, topoisomerase I and / or II inhibitors, proteasome inhibitors, histone deacetylase inhibitors, nitrogen mustard alkylating agents, nitrosourea alkylating agents, nonclassical alkylating agents, estrogen antagonists, androgen antagonists, mTOR inhibitors, tyrosine kinase inhibitors, and other agents selected from aplidine, ET-743, PM02734 and PM00104, and the use of these combinations in the treatment of cancer.

An anticancer in vivo implant applied locally is prepared from the anticancer nitrosourea-type medicine, the anticancer synergist chosen from Pt compound, anticancer taxol, medicine and vegetative alkaloid, and the biocompatible and biodegradable high-molecular polymer as medicinal additive.

The invention provides a free microspore induced culture medium for brassica campestris. A formula of the culture medium contains KNO3, MgSO4.7H2O, KH2PO4, Ca(NO3)2.4H2O, Na2-EDTA, FeSO4.7H2O, MnSO4.4H2O, AgNO3, H3BO3, ZnSO4.7H2O, KI, Na2MoO4.2H2O, CuSO4 .5H2O, CoCl2.6H2O, chlorinated 2-hydroxyethyl trimethylamine, L-glutamine, vitamin B1, vitamin B6, nicotinic acid, folic acid, biotin, inositol, glycine, L-glutathione, methyl nitrosourea, sucrose, phytagel, 6-BA, NAA, polyethylene glycol, protein hydrolysate, active carbon and phytosulfokine PSK-alpha. The culture medium can be used for greatly improving the induction efficiency of free microspore embryogenic calli of brassica campestris, and has an important application value.

The invention discloses a solid tumor resisting medicine composition with arctigenin and nitrosourea alkylating agent anti-tumor medicines as active components. The weight ratio of arctigenin to nitrosourea alkylating agent anti-tumor medicines is 1:0.001-1000, and preferably 1:0.01-600. The anti-tumor medicine composition provided by the invention is advantaged in clear components, wide anti-tumor spectrum, substantial treatment effect against various tumors, low price, low side-effects, and good clinical application prospect.

The invention provides a sustained-release injection containing nitrosourea drug (galamustine), which contains sustained-release microspheres and solvents. The sustained-release microspheres each comprise an anticancer-active component selected from nitrosourea drugs (such as nimustine and carmustine) and / or topoisomerase inhibitors, and a sustained-release agent. The solvents are common solvents or special solvents containing suspending agent. The viscosity of the suspending agent ranges from 100cp to 3000cp (at a temperature ranging from 20 DEG C to 30 DEG C). The suspending agent is selected from sodium carboxymethylcellulose and the like. The sustained-release agent is selected from p(LAEG-EOP) or p(DAPG-EOP) or other polyphosphate ester copolymers, or copolymer or blend of polyphosphate ester and PLA, polifeprosan, PLGA or poly(erucidic acid dipolymer-sebacic acid). The topoisomerase inhibitor is selected from camptothecin, hydroxycamptothecine, topotecan, lartotecan, irinotecan, etoposide or teniposide. The anticancer composition is also available in the dosage form of sustained-release implant, can retain the effective drug concentration for more than 60 days after intratumoral or local injection or implantation, can obviously reduce the systemic reaction to the drug, and can selectively enhance the curative effect of non-operative treatments such as radiotherapy and chemotherapy.

The invention belongs to the field of chemistry, and particularly relates to a method for synthesizing nitrosoureas antineoplastic drugs through a stannic chloride-sodium nitrite system, and the method is used for solving the technical problems of low yield and complicated after-treatment of a conventional synthetic method. The technical scheme adopted by the invention is as follows: the method for synthesizing the nitrosoureas antineoplastic drugs through the stannic chloride-sodium nitrite system comprises the following steps: a, adding stannic chloride, precursors of nitrosoureas antineoplastic drugs and nitrous acid to chloralkane, and stirring; b, filtering to remove insoluble substances, and washing the filtrate by using a saturated weak alkaline solution, and then drying; and c, removing chloralkane from the dried filtrate, and recrystallizing the obtained solid, so as to obtain the nitrosoureas antineoplastic drugs. The invention provides a novel high-yield method for synthesizing nitrosoureas antineoplastic drugs.

Disclosed is an anti solid tumor medicine composition, which comprises anticancer active constituent and medicinal adjuvant, the anticancer active constituent includes guanopterin, guanopterin derivative, guanopterin analogues or their derivatives which can effectively destroy the DNA restoring function in the tumor cells, thus lower the survivability of tumor cells to Semustine anti-cancer drugs, and the medicinal adjuvant mainly employs biological compactable, degradable and absorbing, which can slowly release the anti-cancer medicament onto tumor partially during the degradation and absorption process, thus the whole body toxicity reaction is reduced appreciably , and the effective medicinal concentration can be sustained to the tumor partially. The composition also contain Nitrosoureas anti-cancer drugs, by dispensing the composition to the tumor partially, the whole body toxicity reaction of Nitrosoureas anti-cancer drugs and / or guanopterin and their derivatives can be lowered, selectively increase the tumor local medicinal concentration, and the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation can be improved.

The invention discloses a solid tumor resisting medicine composition with arctigenin and nitrosourea alkylating agent anti-tumor medicines as active components. The weight ratio of arctigenin to nitrosourea alkylating agent anti-tumor medicines is 1:0.001-1000, and preferably 1:0.01-600. The anti-tumor medicine composition provided by the invention is advantaged in clear components, wide anti-tumor spectrum, substantial treatment effect against various tumors, low price, low side-effects, and good clinical application prospect.

The invention provides an improved synthesis technology of istradefylline. According to the technology, istradefylline is prepared from 1,3-diethyl-6-amino-5-nitrosouracil (SM-III) as a starting material through four steps.

The invention discloses a bicyclo[4.1.0]heptane nitrosourea derivative for a biological orthogonal reaction, and a preparation method and an application thereof. The structural formula of the bicyclo[4.1.0]heptane nitrosourea derivative is represented by formula I; and in the formula I, R represents an alkyl group with the carbon atom number of 1-15, an aryl group with the carbon atom number of 6-15 or H, X represents O or N, and n is a natural number between 1 and 10. A pH-initiated IEDDA reaction of trans-cycloheptene and tetrazine is provided for the first time, and can be used as a biological orthogonal reaction. A bicyclonitrosourea derivative (BNU)-bicyclo[4.1.0]heptane nitrosourea derivative is introduced as a precursor for storing and releasing trans-cycloheptene, so that the highactivity of the trans-cycloheptene is utilized, and the instability of the trans-cycloheptene is avoided as much as possible. The pH-initiated biological orthogonal reaction can be applied to in-vitroprotein labeling, living cell imaging and tissue pre-labeling imaging, and can also be applied to living animal tumor pre-labeling imaging. The novel biological orthogonal reaction has a wide application prospect.

Disclosed is a slow release injection agent of anticancer composition containing nitrosourea drugs and synergistic agent, which comprises slow release microspheres and dissolvent, wherein the slow release microspheres comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being conventional dissolvent or specific dissolvent containing suspension adjuvant. The viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose, the nitrosourea drugs are selected from Carmustine, Nimustine or Fotemustine, the synergistic agent can be selected from tetrazine drugs such as Mitozolomide or temozolomide and / or anticancer antibiotics such as Adriamycin, Aclarubicin, Epirubicin, mitomycin or pidorubicin, the slow release auxiliary materials are selected from polyphosphate ester copolymers such as p(LAEG-EOP), p(DAPG-EOP), copolymer or blend of polyphosphate ester with polylactic acid, Polifeprosan, sebacylic acid and PLGA. The anticancer composition can also be prepared into slow release implanting agent, for injection or placement in or around tumor with a period of effective concentration maintenance over 60 days, as well as the treatment effect of appreciably lowering general reaction of the drugs, and improving the treatment effect of the non-operative treatment methods such as chemotherapy.

The present invention relates to the combination of PM01183 with several anticancer drugs, in particular other anticancer drugs selected from antitumor platinum coordination complexes, antimetabolites, mitotic inhibitors, anticancer antibiotics, topoisomerase I and / or II inhibitors, proteasome inhibitors, histone deacetylase inhibitors, nitrogen mustard alkylating agents, nitrosourea alkylating agents, nonclassical alkylating agents, estrogen antagonists, androgen antagonists, mTOR inhibitors, tyrosine kinase inhibitors, and other agents selected from aplidine, ET-743, PM02734 and PM00104, and the use of these combinations in the treatment of cancer.

The invention provides an anti-cancer medicine composition, which comprises anticancer active constituent and medicinal adjuvant, the anticancer active constituent employs phosphoinositide-3 and nitrosoureas, wherein the phosphoinositide-3 can effectively suppress the growth of the tumor cells, lower the survivability of tumor cells to Semustine anti-cancer drugs, and the medicinal adjuvant mainly employs biological compactable, degradable and absorbing, which can slowly release the phosphoinositide-3 kinase inhibitor onto tumor partially during the degradation and absorption process, thus the whole body toxicity reaction is reduced appreciably , and the effective medicinal concentration can be sustained to the tumor partially. The anti-cancer medicinal composition also contain Nitrosoureas anti-cancer drugs, when locally dispensed on the tumor, the composition can lower down the whole body toxicity reaction of the anti-cancer medicament, selectively increase the tumor local medicinal concentration, and the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation can be improved.

An anticancer composition carrying melphalan and carmustine is a sustained release injection which consists of sustained release microspheres and a dissolvent, wherein, the sustained release microspheres comprise an anticancer active component and a sustained release adjuvant, and the dissolvent is a common dissolvent or a special dissolvent containing a suspending agent. The suspending agent has the viscosity of 100cp-3000cp (at the temperature of 20-30 DEG C) and is selected from sodium carboxymethyl cellulose and the like; the anticancer active component is a combination of a nitrosourea drug and an alkylating agent selected from the melphalan, ifosfamide, 4H-peroxycyclophosphamide or norcantharidin; the sustained release adjuvant is selected from copolymer of polyphosphate esters such as p(LAEG-EOP), p(DAPG-EOP) and the like, copolymer of the polyphosphate ester and polylactic acid, polifeprosan, dienoic fatty acid and sebacic acid, or copolymer or polyblend of poly(erucic acid dimmer-sebacic acid) or poly(fumaric acid-sebacic acid); the anticancer composition is also made into a sustained release implant, and injected into or placed inside or at the periphery of tumor to keep the effective drug concentration more than 60 days. The anticancer composition can also obviously reduce the general reaction of the drug, and selectively enhance the curative effects of non-operative therapies such as radiotherapy, chemotherapy and the like.

The invention relates the anti-cancer drugs. The drugs comprise medicinal findings and DNA duplicate inhibiting agent. The DNA duplicate inhibiting agent, from polymeric (ADP- ribose) polymerization inhibitor and DNA-dependence protease inhibitor, destructs the DNA refinishing function in tumor cell, and reduces the survivability. The medicinal findings comprises degradable absorbing high molecular polymer, and at the course of degrading and absorbing, the findings can release the DNA duplicate inhibiting agent into the tumor parts, reducing the toxicity reaction and keeping effective drug concentration. The anti-cancer drugs also comprise nitrosourea drugs, which can reduce toxicity reaction and improve therapeutic efficacy.

The invention relates to the field of biotechnology and particularly relates to a composition and its preparation method and application. The composition comprises cruciferous vegetable lyophilized powder, pumpkin lyophilized powder and konjac gum. The pharmaceutical composition for observably preventing and treating gastric cancer and colon cancer can prevent and treat rat ulcerative gastric cancer induced by an acetic acid solution with acetic acid content of 30% and methyl-nitro-nitrosoguanidine (MNNG) and can also prevent and reduce rat colon cancer induced by N-methyl-N-nitrosourea (MNU).

An anticancer in vivo implant applied locally is prepared from the anticancer nitrosourea-type medicine, the anticancer synergist chosen from bichloroethanamine-type alkylating agent, anticancer antibiotic, and hormone-type anticancer medicine, and the biocompatible and biodegradable high-molecular polymer as medicinal additive.

The invention discloses a tumor-targeting drug-resistant O6-thiophenemethyl guanine-indolequinone-chloroethyl nitrosourea combined molecule and a preparation method thereof, and relates to the field of pharmacy. According to the compound, indolequinone serves as a hypoxia activation pharmacophore, and under the tumor hypoxia condition, indolequinone is reduced to generate an imine substance with cytotoxicity; the CENUs pharmacophore is decomposed to generate chloroethyl carbocations, so that DNA interstrand cross-linking is caused; and meanwhile, an AGT inhibitor O6-TMG derivative is released, and an AGT inhibition effect is achieved. Therefore, the compound disclosed by the invention not only can play a dual anti-tumor effect, but also has drug resistance and tumor hypoxia targeting property, and has high-efficiency and low-toxicity anti-cancer activity.