92 results about "Chronic granulocytic leukemia" patented technology

The invention relates to an anhydrogalactitol injection preparation and a preparation method thereof. The preparation is characterized by being made from anhydrogalactitol, a water soluble filler, a pH regulator, water for injection and an osmoregulator, wherein, the anhydrogalactitol is 0.001-50% by weight, and the other is pharmaceutic adjuvants or water. The anhydrogalactitol injection preparation has good stability and high bioavailability, thus solving the injection requirements of treating clinical acute granulocytic leukemia and chronic granulocytic leukemia.

The invention relates to phenylbutyryl curcumin derivate and application thereof in anti-tumor drug preparation, in particular to 4-(di(2-chloroethyl) amino) phenylbutyryl curcumin, 4,4'-(di(2-chloroethyl)amino) diphenylbutyryl curcumin, pharmaceutically acceptable salts and a preparation method thereof, and applications of 4-(di(2-chloroethyl) amino) phenylbutyryl curcumin, and 4,4'-(di(2-chloroethyl)amino) di phenylbutyryl curcumin in anti-tumor drug preparation. The phenylbutyryl curcumin derivate can be used for (but not limited to) preparing drugs for treating leukemia, skin cancer, gastric cancer, colon cancer, liver cancer, breast cancer or prostatic cancer. The derivate has obvious inhibition on a plurality of animal tumor cell transplanting modules, especially for the human chronic granulocytic leukemia model constructed by NOD-SCID mice inoculated with the human chronic granulocytic leukemia K562 cell stain, the life prolonging rate is obviously enhanced, and the serious toxicity to mice does not exist.

The invention relates to a traditional Chinese medicine preparation for treating chronic granulocytic leukemia, comprising the following raw materials according to parts by weight: 28 to 32 parts of indigo naturalis, 14 to 16 parts of realgar, 14 to 16 parts of mastic, 0.28 to 0.32 part of musk and 14 to 16 parts of myrrh. The traditional Chinese medicine preparation has the characteristics of good curative effect, low toxicity and low price.

The invention discloses a Bcr/Abl tyrosine kinase inhibitor capable of treating chronic granulocytic leukemia and a preparation method thereof. The Bcr/Abl tyrosine kinase inhibitor capable of treating chronic granulocytic leukemia obtained by a large number of experimental screenings not only can effectively inhibit Bcr/Abl tyrosine kinase, and still has a good inhibitory effect to mutated Bcr/Abl tyrosine kinase, so that the Bcr/Abl tyrosine kinase inhibitor is a novel Bcr/Abl tyrosine kinase inhibitor for effectively treating chronic granulocytic leukemia.

The invention discloses an antitumor combination drug and an application thereof in preparation of an anti-cancer drug. The antitumor combination drug is prepared from 10-40 parts by weight of a first preparation and 0.1-10 parts by weight of a second preparation. The invention further discloses an application of chlorogenic acid in preparation of a toxic and side effect inhibitor for the anti-cancer drug, and the anti-cancer drug is a BCR-ABL small-molecule inhibitor. With the adoption of the technical scheme, targeting ability of the BCR-ABL small-molecule inhibitor for chronic granulocytic leukemia can be improved, toxic and side effects of the BCR-ABL small-molecule inhibitor are reduced, and drug resistance of the BCR-ABL small-molecule inhibitor is reversed.

The present invention relates to a lobaplatin crystal and a preparation method and drug application thereof, the lobaplatin crystal form is B, the melting point Tm. p. . is 230 +/-5 DEG C, diffraction peaks exist at the 2 theta angle values of 8.25, 9.77, 11.70, 13.13, 15.28, 16.48, 17.22, 17. 74, 19.01, 19.56, 22.28, 23.72, 24.04, 24.30, 25.62, 26.20, 28.57, 30.22 and 30.61 in an X-ray powder diffraction PXRD spectrum, wherein the 2 theta angle value error is in the range of 0.2. The crystal form B is obtained by solvent evaporation of lobaplatin trihydrate, or volatilization at room temperature after addition of a solvent in lobaplatin dihydrate or solvent-out crystallization, and drying. Compared with lobaplatin and the lobaplatin trihydrate in the prior art, the lobaplatin crystal in the crystal form B has better stability and solubility, is more suitable for the preparation of various forms of pharmaceutical preparations and storage and use, and can be better used to treat cancers such as breast cancer, small cell lung cancer or chronic granulocytic leukemia.

The invention belongs to the field of biological medicine, and particularly relates to application of berberine in preparing a drug for overcoming the drug resistance of chronic granulocytic leukemia or a drug sensitizer for resisting chronic granulocytic leukemia. Berberine can improve the sensitivity of chronic granulocytic leukemia cells to imatinib and overcome the multi-drug resistance of chronic granulocytic leukemia cells to imatinib. Berberine degrades BCR-ABL protein mainly through a ubiquitination mechanism, and thus the multi-drug resistance of chronic granulocytic leukemia caused by T315I mutation is overcome.

The present invention relates to a Chinese medicine prescription for curing chronic myeloid leukemia and a preparation method thereof, pertaining to the art of Chinese medicine. The internal prescription includes 20 to 40g of radix notoginseng, 10 to 40g of field thistle, 15 to 40g of pilose deer horn, 20 to 45 of lotus powder, 20 to 50g of prepared rehmannia rhizome, 20 to 55g of donkey-hid gelatin, 20 to 60g of dangshen, 20 to 40g of milk veteh, 20 to 40g of carbonized sanguisorba root, 15 to 40g of saffron, 10 to 40g of medlar, 15 to 45g of carbonized buffalo horn, 15 to 50g of Chinese caterpillar fungus, 10 to 40g of carbonized leatherleaf millettia, 10 to 45g of carbonized black plum and 10 to 50g of carbonized hair. The external prescription includes 5 to 15g of carbonized radix notoginseng, 5 to 20g of carbonized setose thistle, 5 to 25 carbonized field thistle, 5 to 15g of carbonized human hair, 5 to 20g of carbonized petiole of windmill palm, 5 to 15g of carbonized rehmannia root and 5 to 25g of common bletilla. The oral powder made by smashing the internal materials is added with honey and made into honey pills or added with water and made into waterdewed pills. The external materials are smashed to obtain the external powder. Patients with chronic myeloid leukemia select honey pill or waterdewed pill and have one pill before three meals a day; the external powder is coated on the affected part by a tampon. Patients with chronic myeloid leukemia use the present invention both for external use and oral administration.

The invention relates to a lobaplatin crystal, a preparing method and a medicine application. The crystal form of the lobaplatin crystal is C, and the melting point Tm.p.. is 228+/-5 DEG C; in a PXRD pattern of the lobaplatin crystal, diffraction peaks exist when the 2theta value is 6.79, 8.07, 12.24, 12.61, 13.50, 16.50, 17.83, 18.32, 18.79, 20.09, 21.64, 22.27, 23.19, 24.73, 27.34, 28.35, 29.12 and 31.92, and the error range of the 2theta value is 0.2. The preparing method for the crystal form C includes the steps that isobutanol or normal propyl alcohol is added into lobaplatin dihydrate, the mixture is stirred in a suspension mode, and the crystal is dissolved out, separated out, dried and then obtained. Compared with existing lobaplatin and lobaplatin trihydrate, better stability and better solubility are achieved, and the lobaplatin crystal can be better suitable for preparing medicine preparations in various forms, can be better stored and used and can be better used for treating cancers such as the breast cancer, the small cell lung cancer and the chronic granulocytic leukemia.

The invention relates to a lobaplatin crystal, a preparation method and a medical application thereof. A crystal form of the crystal is D, its melting point Tm.p..is 218+/-5 DEG C, in a PXRD pattern of the lobaplatin crystal, diffraction peaks exist when the 2theta value is 6.76, 11.07, 12.35, 12.65, 13.88, 15.18, 15.56, 16.68, 17.70, 17.90, 20.08, 21.02, 22.70, 22.92, 25.41, 25.64, 26.41, 26.79, 27.02, 28.15, 31.44, 31.96, 32.96, 34.34, 34.62, 36.93, 40.82 and 43.46, and the error range of the 2theta value is 0.2. The preparing method for the crystal form D includes the steps that 1,2-dichloroethane is added into lobaplatin dihydrate, a mixture is stirred in a suspension mode, and the crystal is dissolved out, separated out, dried and then obtained. Compared with existing lobaplatin and lobaplatin trihydrate, better stability and better solubility are achieved, and the lobaplatin crystal can be better suitable for preparing medicine preparations in various forms, can be better stored and used and can be better used for treating cancers such as the breast cancer, the small cell lung cancer and the chronic granulocytic leukemia.

The invention relates to a preparation method of a drug for treating chronic granulocytic leukemia, belonging to the field of medical chemistry, and specifically relates to a preparation method of 3-[2-(imidazo[1,2-b] pyridazine-3-yl) acetenyl]-4-methyl-N-{4-[4-methyl piperazine-1-yl] methyl}-3- trifluoromethyl phenyl} benzoyl amide (ponatinib). The method comprises the following steps: adding a phosphine ligand and cesium carbonate at the same time by taking Pd(PPh3)2Cl2 as a catalyst; adding strong base DBU or adding CuI as a cocatalyst to carry out sonagashira reaction, wherein the phosphine ligand is selected from tricyclohexyl phosphine (PCy3), tri-tert-butyl phosphine (PtBu3) or tri(funan-2-yl) phosphine (P(2-furyl)3). The method disclosed by the invention is complete in reaction, does not have or has extremely few diyne byproduct of alkyne coupling, and is easy to separate and purity.

The present invention relates to a lobaplatin crystal and a preparation method and drug application thereof, the lobaplatin crystal form is F, the melting point Tm. p. . is 229 +/-5 DEG C, diffraction peaks exist at the 2 theta angle values of 8.21, 11.60, 12.99, 15.24, 16.44, 17.11, 17.55, 18.42, 19.01, 19.20, 19.42, 21.81, 22.17, 22.42, 23.33, 23.85, 24.18, 24.40, 24.77, 25.46, 25.98, 26.13, 27.89, 28.42, 29.03, 30.32, 31.17, 31.94, 33.30, 36.20, 37.62 and 39.66 in an X-ray powder diffraction PXRD spectrum, wherein the 2 theta angle value error is in the range of 0.2. The crystal form F is obtained by adding methanol or ethanol into lobaplatin dihydrate, stirring at room temperature until the solid is dissolved, filtering insoluble matters out, adding dropwise slowly an organic solvent, after precipitation of a crystal, separating the crystal, and drying. Compared with lobaplatin and lobaplatin trihydrate in the prior art, the lobaplatin crystal in the crystal form F has better stability and solubility, is more suitable for the preparation of various forms of pharmaceutical preparations and storage and use, and can be better used to treat cancers such as breast cancer, small cell lung cancer or chronic granulocytic leukemia.

The invention discloses a neo-clerodane diterpenoid compound and a preparation method and medical application thereof, and provides the structure of the compound, a pharmaceutical composition containing the compound and a preparation method and application of the pharmaceutical composition. The compound is reported for the first time, is a neo-clerodane diterpenoid compound with a novel structure and can be extracted, separated and purified from dried mature fruit of cardamom. In-vitro test results prove that the compound can directly inhibit propagation of K562 cells, and the inhibition capability of the compound is improved with increase of concentration and prolongation of action time. Meanwhile, the compound can induce apoptosis of K562 cells, and the apoptosis promotion effect is improved with increase of concentration and time. The compound (I) may provide a potential means for treatment of chronic granulocytic leukemia and can be used for developing medicines for treating chronic granulocytic leukemia.

The invention discloses a metal organic complex having antineoplastic activity. A chemical reaction of the complex is [Pr(C7H3NO4)3].C4H10N2, the molecular weight is 1677.01, is characterized by comprising a zero-dimensional structure and a trigonal system, a space group is P-3, the unit cell parameter is a=14.953(2), b=14.953(2), c=10.099(2), alpha=beta=90 DEG, gamma=120 DEG, V=1955.5(5), Z=1; wherein the metal organic complex is prepared by taking Pr(NO3)3.6H2O, 2,6-dipicolinic acid, and anhydrous piperazine as raw materials through a hydrothermal method. The process is simple, cost is low, the obtained complex has good inhibition effect on chronic granulocytic leukemia cell strain K562 and esophageal cancer cell line OE-19, and is hopeful for preparing the corresponding antitumor drug.

The invention relates to a fluorescent quantitative PCR (Polymerase Chain Reaction) diagnosis kit for detecting mRNA of an M BCR fusion gene, belonging to the field of biotechnology. The kit comprises a detection primer, a fluorescent probe, a cDNA first-chain synthesis reagent, a fluorescent quantitative PCR mixed liquor, negative control and positive control, wherein the detection primer and the fluorescent probe comprise an M BCR gene primer, a reference gene ABL primer and a Taqman fluorescent probe. The kit can effectively detect the M BCR fusion gene forms, such as e14a3, e13a3, e14a2 and e13a2. The M BCR fusion gene is a gene mark of malignant clone of pluripotential hemopoietic stem cells, is a typical molecular marker of chronic granulocytic leukemia and is related to inhibition of the apoptosis of the leukemic cell. The fluorescent quantitative PCR technology with higher sensitivity and specificity is used for detecting the mRNA level of the M BCR gene, and the specificity and the sensitivity of the detection result both are improved remarkably. The kit provided by the invention provides a brand-new rapid, simple and convenient gene diagnosis technology for making a therapeutic regimen for the patients with chronic granulocytic leukemia, and predicting prognosis.

An application of the compound PSI in preparing the medicines for treating the leukemia including M2-type acute medullary leukemia and chronic granulocytic leukemia is disclosed. Its advantages are low dosage and moderate cost.

The invention relates to succinyl hydrazine compounds derivative and medical compound containing them; and the application of it in preparing medicine that resists leukemia. The succinyl hydrazine compounds derivative shows inhibiting action to BCR-Ab1 tyrosine kinase activity through pharmacological test. It is characterized by high effecivity and low toxicity, and can be widly used to prepare medicine that treats chronic granulocytic leukemia (CML) and philadelphia chromosome positive acute lymphoblastic leukemia, especially medicine treating patient that generates drug resistance to Gleevec.

The invention discloses application of Cephaloziellin F in preparation of drugs for treating chronic granulocytic leukemia, and belongs to the field of drugs. According to research, the Cephaloziellin F can directly inhibit proliferation of K562 cells, and inhibiting ability is improved along with increasing of concentration and extension of action time. Moreover, the Cephaloziellin F can induce K562 cell apoptosis, and the apoptosis promoting effect can be improved along with increasing of the concentration and extension of the time. Therefore, the Cephaloziellin F can be further researched and developed into the drugs for treating the chronic granulocytic leukemia.

The invention discloses a leucocythemia bcr/abl fusion gene targeting micromolecule inhibitor. The compound is obtained through the reaction and salt forming of 2 Beta-(4'-methyl-1'- piperazine group)-3 Alpha-hydroxy-5 Alpha- steride -17-ketone and caffeic acid. The compound salt effectively suppresses the synthesis of mRNA of the bcr/abl fusion gene to inhibite the expression of BCR/ABL protein to inhibite the activity of protein-tyrosine kinase consequently to finally suppress the growth of leucocythemia cells. The compound salt is developed and is expected to be a bcr/abl fusion gene targeting therapeutic agent in the true sense. Therefore, the leucocythemia bcr/abl fusion gene targeting micromolecule inhibitor provides a brand new chemical entity for treating the CML and Ph positive (Ph+) chronic granulocytic leukemia and Ph positive (Ph<+>) acute lymphoblastic leukemia.

The invention provides a 2-cyano phenalenone compound and application thereof, which belong to the technical field of medical chemistry. The compound is obtained by carrying out compound modification on the 6-site and the 3-site of 2, 3-dicyanophenalenone (namely, respectively introducing R1 and R2). The 2-cyano phenalenone compound disclosed by the invention can be combined with Hsp70 protein in vitro, in cells and in an animal model, and competitively dissociates an Hsp70/Bim protein dimer, so that the apoptosis of chronic granulocytic leukemia cells is induced, and the effects of inhibiting the growth of the chronic granulocytic leukemia cells and killing the chronic granulocytic leukemia cells are achieved; the compound is an apoptosis inducer with very high activity, and can be used for preparing a potential medicine for treating or preventing chronic granulocytic leukemia.

The invention relates to a compound of a derivative containing salicylic acid harringtonine, wherein the derivative containing salicylic acid harringtonine has the following general formula (I) defined in the specification, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 can be the same or different, and can be hydrogen, carbonyl, hydroxyl or C1-C8 alkyl, alkoxy, acyl alkoxy or C2-C6 alkynyl, alkenyl or C3-C9 cycloalkyl or aralkyl, phenyl, cyano alkyl, nitro alkyl, carboxyl, haloalkyl, monohydroxy or polyhydroxy alkyl, alkylthioalkyl, alkylsulfonylalkyl, acyloxyalkyl, acylalkyl and sulfonic group,and at least one of R1, R2, R3, R4 and R5 is R. According to the present invention, the compound has excellent anticancer pharmacological effects on chronic granulocytic leukemia, acute myeloid leukemia and lupus erythematosus diseases, can meet the requirements of the medical field, and has high treatment effect, and the preparation method is easy, and is suitable for industrial production.