A method of using a DNA alkylating agent prodrug compound-containing single drug or using the single drug and other drugs in combination for treatment of p53 gene mutation or defect negative cancer and tumor patients, and a pharmaceutical use. In particular, the DNA alkylating agent prodrug compound is selected from a hypoxia-activated DNA alkylating agent prodrug compound, an AKR1C3-activated DNA alkylating agent prodrug compound, and a β-D-Glucosidase- or β-galactosidase-activated DNA alkylating agent prodrug compound.
A61K 31/4535 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un hétérocycle avec le soufre comme hétéro-atome du cycle, p. ex. pizotifène
A61K 31/675 - Composés du phosphore ayant l'azote comme hétéro-atome d'un cycle, p. ex. phosphate de pyridoxal
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/396 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à trois chaînons, p. ex. aziridine
The present application relates to a new method for synthesizing isophosphoramide nitrogen mustard (X-IPM) that is suitable for industrialized production, involves fewer types of solvents, and leads to stable products with high yield. This method is charazterized mainly by the batchwise addition of M (e.g., M is R3N with R being ethyl; i.e., M is triethylamine) and the specific post-reaction treatment, which make it possible for the reaction to fully proceed, lead to products with less impurities, high yield and relatively stable properties, and can lead to stable crystallized substances with specific crystal structures. The present application also relates to stable crystal forms of the isophosphoramide nitrogen mustard (X-IPM) prepared by the aforementioned method, and use of the same as reactants for the synthesis of aziridine structure-containing compounds.
C07F 9/655 - Composés hétérocycliques, p. ex. contenant du phosphore comme hétéro-atome du cycle comportant des atomes d'oxygène, avec ou sans atomes de soufre, de sélénium ou de tellure, comme uniques hétéro-atomes du cycle
C07F 9/6553 - Composés hétérocycliques, p. ex. contenant du phosphore comme hétéro-atome du cycle comportant des atomes de soufre, avec ou sans atomes de sélénium ou de tellure, comme uniques hétéro-atomes du cycle
C07F 9/6558 - Composés hétérocycliques, p. ex. contenant du phosphore comme hétéro-atome du cycle contenant au moins deux hétérocycles différents ou différemment substitués ni condensés entre eux ni condensés avec un carbocycle commun ou un système carbocyclique commun
A solid dispersion containing dimethyl sulfone and the use thereof. The solid dispersion contains a dispersant, i.e., dimethyl sulfone and at least one drug, and is preferably substantially composed of the dispersant dimethyl sulfone and at least one drug. The solid dispersion is prepared by means of the following four methods: method I: uniformly dispersing dimethyl sulfone and a drug in a molten clear state so as to obtain a dispersion system in a molten state, and cooling the dispersion system in a molten state so as to obtain a solid dispersion; method II: uniformly dispersing dimethyl sulfone in a molten clear state, a third solvent mixture and a drug so as to obtain a dispersion system in a molten state, cooling the dispersion system in a molten state, and removing the third solvent so as to obtain a solid dispersion; method III: extruding or grinding dimethyl sulfone and a drug, and then stirring, melting, mixing, and cooling same, so as to obtain a solid dispersion; and method IV: preparing a molten mixture of dimethyl sulfone and a high-molecular polymer, adding a drug when the melting mixture is in a molten state, and uniformly dispersing same, so as to obtain a solid dispersion. The solid dispersion can be used for preparing pharmaceutical preparations.
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 9/14 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p. ex. poudres
A61K 31/00 - Préparations médicinales contenant des ingrédients actifs organiques
A61K 47/00 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p. ex. les supports ou les additifs inertesAgents de ciblage ou de modification chimiquement liés à l’ingrédient actif
A61P 9/00 - Médicaments pour le traitement des troubles du système cardiovasculaire
A61P 19/02 - Médicaments pour le traitement des troubles du squelette des troubles articulaires, p. ex. arthrites, arthroses
4.
PREPARATION PROCESS OF INTERMEDIATE, SYNTHESIS PROCESS OF AMINO IMIDAZOLE CARBOXYLATE ESTER AND HPLC PURITY MEASURE METHOD
This invention relates to a process for preparing an intermediate of aminoimidazole carboxylate, a process for synthesizing aminoimidazole carboxylate and an HPLC method for determining purity. The process of preparing the intermediate of aminoimidazole carboxylate comprises subjecting a compound of formula I-2 and a formate as the reactants to a first-step reaction in a benzene solvent and at a temperature of −5° C.−5° C., with the addition of a solution of sodium alkoxide in such a way that the temperature of the reaction solution is not higher than 5° C., to obtain the intermediate of aminoimidazole carboxylate or a mixture comprising a compound of formula I-3, i.e., the intermediate of aminoimidazole carboxylate. By using a sodium alkoxide reagent, as a comparatively safe alternative to NaH and potassium tert-butoxide which are prone to cause fire hazards or explosions and are not suitable for use in large-scale production, the process of the present application can ensure smooth progression of the reaction to the product and effectively improve the overall safety of the reaction without noticeably impairing the reaction efficiency.
C07D 233/90 - Atomes de carbone comportant trois liaisons à des hétéro-atomes avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile
C07C 227/16 - Préparation de composés contenant des groupes amino et carboxyle liés au même squelette carboné à partir de composés contenant déjà des groupes amino et carboxyle ou leurs dérivés par des réactions n'impliquant pas les groupes amino ou carboxyle
5.
Preparation Process of 1-N-Methyl-2-Nitro-5-Hydroxymethyl Imidazole
The present invention provides a preparation process of 1-N-methyl-2-nitro-5-hydroxymethylimidazole comprising using N,N′-carbonyldiimidazole and 1-N-methyl-2-aminoimidazole-5-carboxylic acid to react at 45˜65° C. for a period of time, and then cooling to 15˜25° C. for a period of time until the reaction is complete, and then reacting with a reducing agent to finally obtain 1-N-methyl-2-nitro-5-hydroxymethylimidazole. The present invention uses the relatively safe N,N′-carbonyldiimidazole to replace the highly toxic, strong irritating, strong corrosive, and environmentally demanding isobutyl chloroformate. It has the following advantages: CDI is a solid, non-irritating and non-corrosive, favorable for storage, transportation and environmental protection, low requirements on equipment, and less physical harm to operators; the reaction operation is simple and the post-treatment is simple. The reaction temperature is higher than that of using isobutyl chloroformate, so as to speed up the reaction, save the reaction time and energy consumption. The yield is high, the side reaction is less, and the product is easy to purify: after the reaction is complete, extracting, drying, and concentrating under reduced pressure until it is drained to obtain a high purity product.
Correlation of the AKR1C3 enzyme expression level with KRAS mutation, and a medical use. For an AKR1C3 enzyme activated anti-cancer prodrug, KRAS gene mutation can directly serve as a test target before drug administration, that is, a patient with KRAS mutation is the patient having a high AKR1C3 enzyme expression level and AKR1C3 enzyme expression level or AKR1C3 RNA testing is not required. That is to say, a positive KRAS mutation testing result can be used as a screening index to screen the patient having a high AKR1C3 enzyme expression level.
C12Q 1/6886 - Produits d’acides nucléiques utilisés dans l’analyse d’acides nucléiques, p. ex. amorces ou sondes pour les maladies provoquées par des altérations du matériel génétique pour le cancer
A61K 31/675 - Composés du phosphore ayant l'azote comme hétéro-atome d'un cycle, p. ex. phosphate de pyridoxal
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
A61K 31/4709 - Quinoléines non condensées contenant d'autres hétérocycles
A61K 31/337 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à quatre chaînons, p. ex. taxol
A61K 31/496 - Pipérazines non condensées contenant d'autres hétérocycles, p. ex. rifampine, thiothixène ou sparfloxacine
A61K 31/513 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime ayant des groupes oxo liés directement à l'hétérocycle, p. ex. cytosine
A61K 31/704 - Composés ayant des radicaux saccharide liés à des composés non-saccharide par des liaisons glycosidiques liés à un composé carbocyclique, p. ex. phloridzine liés à un système carbocyclique condensé, p. ex. sennosides, thiocolchicosides, escine, daunorubicine, digitoxine
A61K 31/4745 - QuinoléinesIsoquinoléines condensées en ortho ou en péri avec des systèmes hétérocycliques condensées avec des systèmes cycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. phénanthrolines
A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p. ex. leucoglucosane, hespéridine, érythromycine, nystatine
A61K 31/14 - Composés d'ammonium quaternaire, p. ex. édrophonium, choline
A61K 31/4045 - Indole-alkylaminesLeurs amides, p. ex. sérotonine, mélatonine
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
A61K 31/4747 - QuinoléinesIsoquinoléines condensées en spiro
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 31/397 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à quatre chaînons, p. ex. azétidine
A61K 31/438 - 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 le cycle étant condensé en spiro avec des systèmes carbocycliques ou hétérocycliques
The present invention relates to a primer-probe composition, a kit, and a detection method. The primer-probe composition is selected from one group of group (i) to group (ix), and the kit comprises the primer-probe composition. According to the present invention, the detection of AKR1C3 RNA content in an ex vivo sample of a patient can be achieved.
C12Q 1/6886 - Produits d’acides nucléiques utilisés dans l’analyse d’acides nucléiques, p. ex. amorces ou sondes pour les maladies provoquées par des altérations du matériel génétique pour le cancer
An injection preparation and a preparation method therefor, and a compatible medicinal liquid and a preparation method therefor. Upon performing tests, the provided injection preparation and compatible medicinal liquid thereof meet the requirements of long-term clinical trials and commercial production and sales. The injection preparation is a solution containing a compound of the following formula I, wherein the solvent of the solution contains C2-C8 alcohol, and can also contain another cosolvent or solubilizer. The preferred injection preparation is a mixed solution of DMA, ELP and ethanol which contains 10 mg/ml of a compound of formula (I), wherein DMA is a cosolvent, and ELP is a solubilizer. For the ready-to-use injection (compatible medicinal liquid) of the compound of following formula (I), the solvent thereof is water, the solute thereof comprises the compound of formula I, DMA, ELP, ethanol, an isosmotic adjusting agent and a pH regulator, the concentration of compound A in the injection is 0.016-1.10 mg/ml, the pH of the injection is 7.4, and the injection is an isosmotic solution. Further disclosed is a method for preparing the above-mentioned injection preparation and a method for preparing the above-mentioned compatible medicinal liquid of the injection.
A61K 31/396 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à trois chaînons, p. ex. aziridine
C07C 205/38 - Composés contenant des groupes nitro liés à un squelette carboné le squelette carboné étant substitué de plus par des groupes hydroxy éthérifiés ayant des groupes nitro et des groupes hydroxy éthérifiés liés à des atomes de carbone de cycles aromatiques à six chaînons du squelette carboné à des atomes de carbone du même cycle aromatique à six chaînons non condensé ou à des atomes de carbone de cycles aromatiques à six chaînons faisant partie du même système cyclique condensé l'atome d'oxygène d'au moins un des groupes hydroxy éthérifiés étant lié de plus à un atome de carbone d'un cycle aromatique à six chaînons, p. ex. éthers nitrodiphényliques
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
The present invention provides gemcitabine anticancer derivatives of formula (III), which have the potential to be developed into AKR1C3-activated anticancer drugs, and the anticancer pharmaceutical use thereof,.
The present invention provides gemcitabine anticancer derivatives of formula (III), which have the potential to be developed into AKR1C3-activated anticancer drugs, and the anticancer pharmaceutical use thereof,.
C07H 19/073 - Radicaux pyrimidine avec un désoxy-2 ribosyle comme radical saccharide
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
Provided are a TH-302 solution, a freeze-dried formulation, a freeze-dried formulation unit package, an injection, and an injection preparation method. The solution for preparing a freeze-dried formulation having high drug loading capacity contains TH-302, water, tert-butyl alcohol, and mannitol; the water and the tert-butyl alcohol are used as a mixed solvent, the volume percentage of the tert-butyl alcohol relative to the solution is (30±3)% or the mass percentage is (24±2.4)%, or the content of the tert-butyl alcohol in the solution is (235.5±23.55) mg/mL; the content of TH-302 in the solution is (8.16±0.82) mg/g or (8.00±0.80) mg/mL; the mannitol is used as an excipient, the mass percentage of the mannitol in the solution is (7.14±0.71)% or the content of the mannitol in the solution is (70±7) mg/mL; and the pH value of the solution is 4-9. The freeze-dried formulation contains TH-302 and mannitol; the drug loading capacity of TH-302 in the freeze-dried formulation is (8.00±0.80) mg/cm3 or the mass percentage of TH-302 in the freeze-dried formulation is (10.23±1.02)%; and the content of the mannitol in the freeze-dried formulation is (70±7) mg/cm3, or the content of the mannitol in the freeze-dried formulation is the percentage balance of the mass percentage, (10.23±1.02)%, of TH-302.
Provided are a gemcitabine anti-cancer derivative, the anti-cancer pharmaceutical use thereof, and a preparation method therefor. The compound has the potential to be developed into an anti-cancer drug activated by means of AKR1C3.
C07H 19/073 - Radicaux pyrimidine avec un désoxy-2 ribosyle comme radical saccharide
C07H 1/00 - Procédés de préparation des dérivés du sucre
A61K 31/7064 - 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
Provided are a stable AST-3424 API product, a preparation method therefor, and storage thereof. The stable AST-3424 API product provided in the present invention is a solution of AST-3424 in ethanol, and the mass percentage of AST-3424 in the solution is 30%-40%. Also provided is a packaging unit of the product, which comprises a container and a stable AST-3424 API product contained in the container. The container is provided with a container body used for containing the product and a sealing structure used for sealing the container body. The container body and the sealing structure are both made from a medicinal-grade high-density polyethylene material. An oily AST-3424 product obtained after separation and purification is mixed with absolute ethyl alcohol at no more than 30 °C, and then distilled under reduced pressure until the mass percentage of AST-3424 reaches a preset value to obtain the product. The described product should be stored in a dark environment at -20 ± 5 °C.
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 31/396 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à trois chaînons, p. ex. aziridine
Described is a deuterated compound, and preparation method and use thereof The deuterated compound I has a structure as shown in Formula (I), wherein A is H or D, and at least one of eight As is D; M is H or an alkali metal, an alkaline earth metal, or an ammonium radical. The present invention provides use of the deuterated compound I as an internal standard for measuring the content of a metabolite II in a biological sample, wherein the metabolite II has a structure as shown in a Formula (II); wherein A is H; M is H or an alkali metal, an alkaline earth metal, or an ammonium radical. The present invention uses the deuterated compound I as an internal standard to quantitatively analysis the content of metabolite II at lower content in biological samples, which can not only meet the requirements for the lower limit of quantitation, but also meet the requirements for DMPK studies in clinical trials.
Described is a deuterated compound, and preparation method and use thereof The deuterated compound I has a structure as shown in Formula (I), wherein A is H or D, and at least one of eight As is D; M is H or an alkali metal, an alkaline earth metal, or an ammonium radical. The present invention provides use of the deuterated compound I as an internal standard for measuring the content of a metabolite II in a biological sample, wherein the metabolite II has a structure as shown in a Formula (II); wherein A is H; M is H or an alkali metal, an alkaline earth metal, or an ammonium radical. The present invention uses the deuterated compound I as an internal standard to quantitatively analysis the content of metabolite II at lower content in biological samples, which can not only meet the requirements for the lower limit of quantitation, but also meet the requirements for DMPK studies in clinical trials.
B01D 15/16 - Adsorption sélective, p. ex. chromatographie caractérisée par des caractéristiques de structure ou de fonctionnement relatives au conditionnement du fluide vecteur
B01D 15/42 - Adsorption sélective, p. ex. chromatographie caractérisée par le mode de développement, p. ex. par déplacement ou par élution
C07B 59/00 - Introduction d'isotopes d'éléments dans les composés organiques
An AKR1C3 detection method, and a diagnostic kit for detecting AKR1C3 and use thereof. The AKR1C3 detection method includes the following steps: treating a formalin-fixed paraffin-embedded human tissue specimen sequentially using an organic solvent, an alcohol, and water; performing antigen retrieval on the treated formalin-fixed paraffin-embedded human tissue specimen in the presence of an antigen retrieval solution; co-incubating the antigen-retrieved formalin-fixed paraffin-embedded human tissue specimen with a blocking buffer to block a non-specific antigen; mixing the blocked formalin-fixed paraffin-embedded human tissue specimen with a certain concentration of AKR1C3 monoclonal antibody solution for primary antibody incubation, and mixing the primary antibody-incubated formalin-fixed paraffin-embedded human tissue specimen with a certain concentration of a secondary antibody solution for secondary antibody incubation. The AKR1C3 detection method can be applied to the detection of AKR1C3 expression levels in various cancer tumor tissues and is stable in dyeing results, and has good sensitivity, precision and consistency.
Provided in the present invention are a treatment method for treating cancer patients accompanied by pain by using a combination of an AKR1C3 activated anticancer prodrug compound and an analgesic drug, a pharmaceutical use, a drug combination and a pharmaceutical preparation thereof. A reasonable selection scheme is provided for the clinical treatment of cancers, and in particular, the effects of simultaneously treating cancers and relieving pain can be achieved by means of the combination of AST-3424 and a non-steroidal analgesic drug.
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
17.
USE OF HYPOXIA-ACTIVATED COMPOUND IN PREPARATION OF MEDICAMENT FOR TREATING CANCER PATIENT
Provided is use of a hypoxia-activated compound alone or in combination with a PARP inhibitor in the preparation of a medicament for treating a cancer patient. In particular, the patient is detected to have pathogenic gene mutations such as an RAD51D mutation. At the same time, a method for treating cancer, a drug combination, and a pharmaceutical preparation are provided. The method, the drug combination, and the pharmaceutical preparation have a very good tumor inhibition effect on the patient with pathogenic gene mutations such as an RAD51D mutation when administered alone, and have a good tumor inhibition effect even if the patient has resistance to the PARP inhibitor. The drug used in combination with PRAP has a certain synergistic effect compared with the efficacy of the drug alone.
A treatment method, comprising using a drug containing AST-3424, AST-3423 or AST-2870 and a salt thereof, an ester thereof, a solvate thereof, or an isotopic isomer thereof in combination with a drug containing cytarabine or daunorubicin and a salt thereof, an ester thereof, a solvate thereof, or an isotopic isomer thereof to treat leukemia and lymphoma patients. Where the concentration of daunorubicin or cytarabine is far lower than the clinical dosage thereof, there is no need to limit patients to those with higher (overexpression, excess) AKR1C3 protein or RNA expression; the combination of AST-3424 and cytarabine or daunorubicin still has a remarkable inhibitory effect on the in-vitro proliferation of leukemia or lymphoma cells, and the combination has a relatively good inhibitory effect on the in-vitro proliferation of cell lines with different levels of AKR1C3 protein or RNA expression. Therefore, the described combination protocol is expected to be developed into a new treatment protocol for treating leukemia and lymphoma without limiting the level of AKR1C3 enzyme expression in patients.
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
A61P 35/02 - Agents anticancéreux spécifiques pour le traitement de la leucémie
19.
METHOD FOR TREATING CANCER PATIENT WITH AKR1C3 ENZYME-ACTIVATED PRODRUG
Provided is treatment of a cancer patient with an AKR1C3 enzyme-activated prodrug, which is characterized in that: a tumor or cancer tissue of the patient is detected to have a gene mutation capable of upregulating or activating NRF2; or the patient is detected to have a gene mutation capable of upregulating or activating NRF2.
A61K 31/675 - Composés du phosphore ayant l'azote comme hétéro-atome d'un cycle, p. ex. phosphate de pyridoxal
A61K 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p. ex. pipérazine
A61K 31/496 - Pipérazines non condensées contenant d'autres hétérocycles, p. ex. rifampine, thiothixène ou sparfloxacine
A61K 31/472 - Isoquinoléines non condensées, p. ex. papavérine
A61K 31/4375 - 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 six chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. quinolizines, naphtyridines, berbérine, vincamine
A61K 31/445 - Pipéridines non condensées, p. ex. pipérocaïne
A61K 31/5377 - 1,4-Oxazines, p. ex. morpholine non condensées et contenant d'autres hétérocycles, p. ex. timolol
A61K 31/255 - Esters, p. ex. nitroglycérine, sélénocyanates d'acides oxygénés du soufre ou de leurs thio-analogues
A61K 31/551 - 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 ayant deux atomes d'azote comme hétéro-atomes d'un cycle, p. ex. clozapine, dilazèpe
A61K 31/136 - Amines, p. ex. amantadine ayant des cycles aromatiques, p. ex. méthadone ayant le groupe amino lié directement au cycle aromatique, p. ex. benzène-amine
A61K 31/4709 - Quinoléines non condensées contenant d'autres hétérocycles
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
A61K 31/337 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à quatre chaînons, p. ex. taxol
A61K 31/4523 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques
A61K 31/7072 - 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 ayant deux groupes oxo liés directement au cycle pyrimidine, p. ex. uridine, acide uridylique, thymidine, zidovudine
A61K 31/704 - Composés ayant des radicaux saccharide liés à des composés non-saccharide par des liaisons glycosidiques liés à un composé carbocyclique, p. ex. phloridzine liés à un système carbocyclique condensé, p. ex. sennosides, thiocolchicosides, escine, daunorubicine, digitoxine
A61K 31/4745 - QuinoléinesIsoquinoléines condensées en ortho ou en péri avec des systèmes hétérocycliques condensées avec des systèmes cycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. phénanthrolines
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 38/08 - Peptides ayant de 5 à 11 amino-acides
A61K 31/14 - Composés d'ammonium quaternaire, p. ex. édrophonium, choline
A61K 31/7048 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'oxygène comme hétéro-atome d'un cycle, p. ex. leucoglucosane, hespéridine, érythromycine, nystatine
Provided is a method for treating cancer by combining an alkylating agent prodrug and a cell cycle inhibitor. The alkylating agent prodrug may be a prodrug of an AKR1C3 enzyme-activated alkylating agent or a prodrug of a hypoxia-activated alkylating agent. The cell cycle inhibitor may be a CDK inhibitor, a WEE inhibitor, a CHK inhibitor, or an ATR inhibitor.
A61K 31/675 - Composés du phosphore ayant l'azote comme hétéro-atome d'un cycle, p. ex. phosphate de pyridoxal
A61K 31/519 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
A61K 31/4535 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un hétérocycle avec le soufre comme hétéro-atome du cycle, p. ex. pizotifène
Described are hypoxia-activated DNA alkylating agents having any one of the following structural formulas, or a pharmaceutically acceptable salt, a prodrug, a solvate or an isotopic variant thereof, as well as an anticancer medical use thereof.
Described are hypoxia-activated DNA alkylating agents having any one of the following structural formulas, or a pharmaceutically acceptable salt, a prodrug, a solvate or an isotopic variant thereof, as well as an anticancer medical use thereof.
The present invention provides a method for treating a cancer by using TH-302 and an analogue thereof alone or in combination with a PARP inhibitor, wherein in particular, TH-302 is used alone for treating a cancer patient sensitive to the PARP inhibitor, and TH-302 is used in combination with the PARP inhibitor for treating a cancer patient.
A method for treating BRCA gene-mutated cancer. In the method, a drug containing hypoxia-activated prodrug compounds of formulas (1), (2) and (3) or AKR1C3 enzyme-activated prodrug compounds of formulas (4), (5), (6), (7), (8), (9), (10), (11) and (12) and salts, esters, solvates and isotopic isomers thereof, is used alone or in combination with other drugs to treat patients with BRCA gene-mutated cancer and tumors.
A61K 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p. ex. pipérazine
A61K 31/4747 - QuinoléinesIsoquinoléines condensées en spiro
A deuterated compound, and a preparation method therefor and the use thereof. The structural formula of the deuterated compound I is as shown in formula (I), wherein A is H or D, at least one of the eight A is D, and M is H or an alkali metal, alkaline earth metal and ammonium radical. Provided is the use of the deuterated compound I as an internal standard in the detection of the content of metabolite II in a biological sample, wherein the structural formula of metabolite II is as shown in formula (II), A is H, and M is H or an alkali metal, alkaline earth metal and ammonium radical. The deuterated compound I can be used as an internal standard for quantitatively analyzing the content of low-content metabolite II in a biological sample, can meet the quantitative detection requirements at a low concentration, and is suitable for DMPK research in clinical trials.
An AKR1C3-activated DNA alkylating agent having any one of the following structural formulas (A, B, C), or a pharmaceutically acceptable salt thereof, or a prodrug thereof, or a solvate thereof, or an isotopic variant thereof, and an anticancer medical application thereof.
A61K 31/396 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à trois chaînons, p. ex. aziridine
A61K 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p. ex. pipérazine
A61K 31/496 - Pipérazines non condensées contenant d'autres hétérocycles, p. ex. rifampine, thiothixène ou sparfloxacine
A61K 31/472 - Isoquinoléines non condensées, p. ex. papavérine
A61K 31/551 - 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 ayant deux atomes d'azote comme hétéro-atomes d'un cycle, p. ex. clozapine, dilazèpe
A61K 31/395 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines
A61K 31/4375 - 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 six chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. quinolizines, naphtyridines, berbérine, vincamine
A61K 31/445 - Pipéridines non condensées, p. ex. pipérocaïne
A61K 9/19 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p. ex. poudres lyophilisées
A61K 31/675 - Composés du phosphore ayant l'azote comme hétéro-atome d'un cycle, p. ex. phosphate de pyridoxal
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
The present invention provides a treatment method for treating a PARP inhibitor-resistant patient with TH-302 alone or in combination, a drug, and a pharmaceutical use thereof.
A compound of formula (I), or pharmaceutically acceptable salts, solvates, isotopic variants, or isomers thereof, and anticancer medical use are provided.
A compound of formula (I), or pharmaceutically acceptable salts, solvates, isotopic variants, or isomers thereof, and anticancer medical use are provided.
Described is a method for associating with the expression level of an AKR1C3 enzyme via the content of prostaglandin, and the use of screening for drug administration. In particular, the content of prostaglandin is measured to associate with the expression level of the AKR1C3 enzyme in a biological sample; and the change in the content and the change rate of the content of prostaglandin before and after administering interfering drugs are measured to associate with the expression level of the AKR1C3 enzyme in the biological sample.
G01N 33/88 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique faisant intervenir des prostaglandines
A61K 31/4709 - Quinoléines non condensées contenant d'autres hétérocycles
A61K 31/675 - Composés du phosphore ayant l'azote comme hétéro-atome d'un cycle, p. ex. phosphate de pyridoxal
C12Q 1/32 - Procédés de mesure ou de test faisant intervenir des enzymes, des acides nucléiques ou des micro-organismesCompositions à cet effetProcédés pour préparer ces compositions faisant intervenir une oxydoréductase une déshydrogénase
An orally administered solid dosage form drug for treating cancers, tumors or cell proliferative disorders contains a compound of the following structural formula I or II.
An orally administered solid dosage form drug for treating cancers, tumors or cell proliferative disorders contains a compound of the following structural formula I or II.
The present invention provides gemcitabine anticancer derivatives of formula (III) and the anticancer pharmaceutical use, which have the potential to be developed into AKR1C3-activated anticancer drugs.
C07H 19/073 - Radicaux pyrimidine avec un désoxy-2 ribosyle comme radical saccharide
C07H 1/00 - Procédés de préparation des dérivés du sucre
A61K 31/7064 - 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
Provided are anti-cancer compounds which act as a non-PGP substrate, same being compounds of formula I-1, or a pharmaceutically acceptable salt, a prodrug or a solvate thereof, and the medical use of these compounds in the treatment of cancers, tumors, conditions caused by cancers or tumors, or cell proliferative diseases. Also provided is a method for treating cancers, tumors, conditions caused by cancers or tumors, or cell proliferative diseases using the anti-cancer compounds which act as non-PGP substrates as described above.
A61K 31/396 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à trois chaînons, p. ex. aziridine
A61K 31/357 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant plusieurs atomes d'oxygène dans le même cycle, p. ex. éthers en couronne, guanadrel
34.
RECOMBINANT ONCOLYTIC VIRUS AND MEDICAL USE THEREOF
Provided is a recombinant oncolytic virus obtained by means of integrating a coding sequence capable of expressing the RNA or DNA of a targeted enzyme in tumor cells into the genome of an oncolytic virus, wherein the recombinant oncolytic virus is combined with an antitumor prodrug activated by the targeted enzyme to improve the antitumor effect of the oncolytic virus. Also provided is a recombinant oncolytic virus, characterized in that the recombinant oncolytic virus is a selective replication-type oncolytic virus, a coding sequence capable of expressing the RNA or DNA of a targeted enzyme in tumor cells is integrated in the genome of the recombinant oncolytic virus, and the targeted enzyme is an enzyme capable of activating an antitumor prodrug. Further provided is a pharmaceutical composition, which comprises the recombinant oncolytic virus and a targeted enzyme-activated antitumor prodrug.
The present invention relates to a primer-probe composition, a kit, and a detection method. The primer-probe composition is selected from one group of group (i) to group (ix), and the kit comprises the primer-probe composition. According to the present invention, the detection of AKR1C3 RNA content in an in vitro sample of a patient can be achieved.
C12Q 1/6886 - Produits d’acides nucléiques utilisés dans l’analyse d’acides nucléiques, p. ex. amorces ou sondes pour les maladies provoquées par des altérations du matériel génétique pour le cancer
A61K 31/675 - Composés du phosphore ayant l'azote comme hétéro-atome d'un cycle, p. ex. phosphate de pyridoxal
G01N 33/68 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique faisant intervenir des protéines, peptides ou amino-acides
36.
PRIMER-PROBE COMPOSITION, KIT, AND DETECTION METHOD
The present invention relates to a primer-probe composition, a kit, and a detection method. The primer-probe composition is selected from one group of group (i) to group (ix), and the kit comprises the primer-probe composition. According to the present invention, the detection of AKR1C3 RNA content in an in vitro sample of a patient can be achieved.
C12Q 1/6886 - Produits d’acides nucléiques utilisés dans l’analyse d’acides nucléiques, p. ex. amorces ou sondes pour les maladies provoquées par des altérations du matériel génétique pour le cancer
G01N 33/68 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique faisant intervenir des protéines, peptides ou amino-acides
A61K 31/675 - Composés du phosphore ayant l'azote comme hétéro-atome d'un cycle, p. ex. phosphate de pyridoxal
Provided are the use of the compound 1-(3-(3-N,N-dimethylaminocarbonyl)phenoxyl-4-mtrophenyl)-1-ethyl-N,N'-bis(ethylene)phosphoramidate, or a pharmaceutically acceptable salt, isotopic variant or solvate thereof in the manufacture of a medicament for treating cancer, and a composition which comprises the above compound and at least one anti-cancer drug.
Described are compounds that act as AKR1C3 inhibitors or pharmaceutically acceptable salts or solvates or isotopically substituted compounds thereof and methods thereof.
C07C 205/38 - Composés contenant des groupes nitro liés à un squelette carboné le squelette carboné étant substitué de plus par des groupes hydroxy éthérifiés ayant des groupes nitro et des groupes hydroxy éthérifiés liés à des atomes de carbone de cycles aromatiques à six chaînons du squelette carboné à des atomes de carbone du même cycle aromatique à six chaînons non condensé ou à des atomes de carbone de cycles aromatiques à six chaînons faisant partie du même système cyclique condensé l'atome d'oxygène d'au moins un des groupes hydroxy éthérifiés étant lié de plus à un atome de carbone d'un cycle aromatique à six chaînons, p. ex. éthers nitrodiphényliques
C07F 9/6584 - Composés hétérocycliques, p. ex. contenant du phosphore comme hétéro-atome du cycle comportant des atomes de phosphore, avec ou sans atomes d'azote, d'oxygène, de soufre, de sélénium ou de tellure, comme hétéro-atomes du cycle comportant des atomes de phosphore et d'azote, avec ou sans atomes d'oxygène ou de soufre, comme hétéro-atomes du cycle comportant un atome de phosphore comme hétéro-atome du cycle
C07C 33/20 - Alcools monohydroxyliques ne contenant que des cycles aromatiques à six chaînons dans la partie cyclique monocycliques
C07F 9/6571 - Composés hétérocycliques, p. ex. contenant du phosphore comme hétéro-atome du cycle comportant des atomes de phosphore, avec ou sans atomes d'azote, d'oxygène, de soufre, de sélénium ou de tellure, comme hétéro-atomes du cycle comportant des atomes de phosphore et d'oxygène comme uniques hétéro-atomes du cycle
C07F 9/6581 - Composés hétérocycliques, p. ex. contenant du phosphore comme hétéro-atome du cycle comportant des atomes de phosphore, avec ou sans atomes d'azote, d'oxygène, de soufre, de sélénium ou de tellure, comme hétéro-atomes du cycle comportant des atomes de phosphore et d'azote, avec ou sans atomes d'oxygène ou de soufre, comme hétéro-atomes du cycle
39.
USE OF TIPRANAVIR IN PREPARING CANCER THERAPY DRUGS FOR KILLING TUMOR STEM CELLS AND TUMOR CELLS
A use of Tipranavir in preparing cancer therapy drugs for killing tumor stem cells and tumor cells. Therapeutic drugs for cancer, the drugs being capable of killing tumor stem cells and tumor cells. The drugs use Tipranavir as a main active ingredient, and contain a pharmaceutically acceptable carrier. Tipranavir can be used for preparing anti-cancer drugs for killing tumor stem cells and tumor cells, and has no obvious toxic side effects.
A61K 31/4433 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un cycle à six chaînons avec l'oxygène comme hétéro-atome du cycle
A61K 31/337 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à quatre chaînons, p. ex. taxol
The present invention provides a fluorine-containing compound shown in Formula II/III and its anti-cancer medical use.
The present invention provides a fluorine-containing compound shown in Formula II/III and its anti-cancer medical use.
C07F 9/6558 - Composés hétérocycliques, p. ex. contenant du phosphore comme hétéro-atome du cycle contenant au moins deux hétérocycles différents ou différemment substitués ni condensés entre eux ni condensés avec un carbocycle commun ou un système carbocyclique commun
The present invention relates to a hypoxia-activated DNA alkylating agent having any one among the following structural formulas, or a prodrug, solvate, isotopic variant, or pharmaceutically acceptable salt thereof, as well as an anticancer medical use thereof.
An AKR1C3 detection method, and a diagnostic kit for detecting AKR1C3 and use thereof. The AKR1C3 detection method comprises the following steps: treating a formalin-fixed paraffin-embedded human tissue specimen sequentially using an organic solvent, an alcohol, and water; performing antigen retrieval on the treated formalin-fixed paraffin-embedded human tissue specimen in the presence of an antigen retrieval solution; co-incubating the antigen-retrieved formalin-fixed paraffin-embedded human tissue specimen with a blocking buffer to block a non-specific antigen; mixing the blocked formalin-fixed paraffin-embedded human tissue specimen with a certain concentration of an AKR1C3 monoclonal antibody solution for primary antibody incubation; and mixing the primary antibody-incubated formalin-fixed paraffin-embedded human tissue specimen with a certain concentration of a secondary antibody solution for secondary antibody incubation. The AKR1C3 detection method can be applied to the detection of AKR1C3 expression levels in various cancer tumor tissues and is stable in dyeing results, and has good sensitivity, precision and consistency.
G01N 33/574 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour le cancer
G01N 33/68 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique faisant intervenir des protéines, peptides ou amino-acides
43.
AKR1C3 DETECTION METHOD, AND DIAGNOSTIC KIT FOR DETECTING AKR1C3 AND USE THEREOF
An AKR1C3 detection method, and a diagnostic kit for detecting AKR1C3 and use thereof. The AKR1C3 detection method comprises the following steps: treating a formalin-fixed paraffin-embedded human tissue specimen sequentially using an organic solvent, an alcohol, and water; performing antigen retrieval on the treated formalin-fixed paraffin-embedded human tissue specimen in the presence of an antigen retrieval solution; co-incubating the antigen-retrieved formalin-fixed paraffin-embedded human tissue specimen with a blocking buffer to block a non-specific antigen; mixing the blocked formalin-fixed paraffin-embedded human tissue specimen with a certain concentration of an AKR1C3 monoclonal antibody solution for primary antibody incubation; and mixing the primary antibody-incubated formalin-fixed paraffin-embedded human tissue specimen with a certain concentration of a secondary antibody solution for secondary antibody incubation. The AKR1C3 detection method can be applied to the detection of AKR1C3 expression levels in various cancer tumor tissues and is stable in dyeing results, and has good sensitivity, precision and consistency.
G01N 33/574 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour le cancer
G01N 33/68 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique faisant intervenir des protéines, peptides ou amino-acides
44.
USE OF COMPOUND IN DRUG FOR PREVENTING, TREATING, OR ALLEVIATING PAIN
The present invention provides a use of a compound shown in Formula I/II in a drug for preventing, treating or alleviating pain
The present invention provides a use of a compound shown in Formula I/II in a drug for preventing, treating or alleviating pain
The present invention provides a compound of formula (I), or pharmaceutically acceptable salts or solvates or isotope variants or isomers thereof, and anticancer medical use thereof: (I).
Disclosed are a method for associating with the expression level of an AKR1C3 enzyme via the content of prostaglandin, and the use of screening for drug administration. In particular, the content of prostaglandin is measured to associate with the expression level of the AKR1C3 enzyme in a biological sample; and the change in the content and the change rate of the content of prostaglandin before and after administering interfering drugs are measured to associate with the expression level of the AKR1C3 enzyme in the biological sample. Also disclosed is an assembly for measuring the expression level of the AKR1C3 enzyme. The assembly includes a component, which reacts with the biological sample by means of coming into contact with same and quantitatively or semi-quantitatively associates with the content of prostaglandin in the biological sample according to a reaction signal, and a control component, which is used to compare the reaction signal to obtain the content of prostaglandin in the biological sample, and the expression level of the AKR1C3 enzyme corresponding to the change in the content and the change rate of the content of prostaglandin before and after administering interfering drugs. Further disclosed is a drug delivery device, which contains an assembly for measuring the expression level of the AKR1C3 enzyme; and an assembly for drug administration containing an AKR1C3 enzyme-activated anti-cancer prodrug.
G01N 33/50 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique
47.
METHOD FOR ASSOCIATING WITH EXPRESSION LEVEL OF AKR1C3 ENZYME VIA CONTENT OF PROSTAGLANDIN, AND USE OF SCREENING FOR DRUG ADMINISTRATION
Disclosed are a method for associating with the expression level of an AKR1C3 enzyme via the content of prostaglandin, and the use of screening for drug administration. In particular, the content of prostaglandin is measured to associate with the expression level of the AKR1C3 enzyme in a biological sample; and the change in the content and the change rate of the content of prostaglandin before and after administering interfering drugs are measured to associate with the expression level of the AKR1C3 enzyme in the biological sample. Also disclosed is an assembly for measuring the expression level of the AKR1C3 enzyme. The assembly includes a component, which reacts with the biological sample by means of coming into contact with same and quantitatively or semi-quantitatively associates with the content of prostaglandin in the biological sample according to a reaction signal, and a control component, which is used to compare the reaction signal to obtain the content of prostaglandin in the biological sample, and the expression level of the AKR1C3 enzyme corresponding to the change in the content and the change rate of the content of prostaglandin before and after administering interfering drugs. Further disclosed is a drug delivery device, which contains an assembly for measuring the expression level of the AKR1C3 enzyme; and an assembly for drug administration containing an AKR1C3 enzyme-activated anti-cancer prodrug.
G01N 33/50 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique
An orally administered solid dosage form drug for treating cancers or tumors or cell proliferative disorders, containing a compound represented by the following structural formula I or II.
Provided are anti-cancer compounds which act as a non-PGP substrate, same being compounds of formula I-1, or a pharmaceutically acceptable salt, a prodrug or a solvate thereof, and the medical use of these compounds in the treatment of cancers, tumors, conditions caused by cancers or tumors, or cell proliferative diseases. Also provided is a method for treating cancers, tumors, conditions caused by cancers or tumors, or cell proliferative diseases using the anti-cancer compounds which act as non-PGP substrates as described above.
A packaging bottle (100) and packaging kit (1000) for an injection, and a filling, stoppering and capping device and method. The packaging bottle (100) comprises: a bottle body (10); a rubber stopper assembly (20) for plugging into the bottle mouth (13) of the bottle body (10); and a cap (30) disposed on the rubber stopper assembly (20) to clip and fix the bottle mouth (13) and the rubber stopper assembly (20), the rubber stopper assembly (20) comprising a rubber stopper (21) and a covering layer (22) directly attached to the exposed surface of the rubber stopper (21) facing the bottle mouth (13), there being no adhesive layer between the covering layer (22) and the rubber stopper (21), the covering layer (22) being a polytetrafluoroethylene layer, a polyvinylidene fluoride layer, a tetrafluoroethylene/hexafluoropropylene copolymer layer or a composite layer of at least two; a gap (31) being formed on the top of the cap (30) to expose the rubber stopper (21) for easy puncture. Also provided are a corresponding packaging kit (1000) for AST-3424 injection and method. The requirements for the packaging bottle (100) for AST-3424 injection that is separated from an ethanol/propylene glycol solvent to ensure the stability there is no contamination between the injection and the packaging bottle stopper can be satisfied.
A61J 1/05 - Récipients spécialement adaptés à des fins médicales ou pharmaceutiques pour recueillir, stocker ou administrer du sang, du plasma ou des liquides à usage médical
A61J 1/14 - Récipients spécialement adaptés à des fins médicales ou pharmaceutiques DétailsAccessoires à cet effet
B65B 3/00 - Emballage de matériaux plastiques, de semi-liquides, de liquides ou de liquides et solides mélangés, dans des réceptacles ou récipients individuels, p. ex. dans des sacs ou sachets, boîtes, cartons, bidons ou pots
B65B 7/28 - Fermeture de réceptacles ou récipients semi-rigides ou rigides, non déformés par le contenu ou n'en prenant pas la forme, p. ex. boîtes ou cartons en appliquant des fermetures séparées préformées, p. ex. couvercles, capuchons
B65D 39/00 - Fermetures disposées dans les cols, les orifices verseurs ou les ouvertures de décharge, p. ex. bouchons
B65D 51/18 - Aménagements des fermetures avec couvercles extérieurs de protection analogues à des capuchons ou de plusieurs fermetures conjuguées
A stable AST-3424 injection preparation, being a solution containing 0.1-200 mg/ml or 1-200 mg/ml of AST-3424 active ingredients. A solvent in the solution contains a C2-C8 monohydric alcohol. The preparation method comprises the following steps: performing first dissolution preparation on the AST-3424 active ingredients and a partial prescription amount of ethanol; adding a prescription amount of propylene glycol for the second-time dissolution preparation; and then, adding the remaining prescription amount of ethanol for mixing and dissolving to obtain a solution containing 1-200 mg/ml of AST-3424 active ingredients. The solvent of the AST-3424 injection is water, or a glucose solution, ethanol, and a propylene glycol solute consist of the AST-3424 active ingredients, an isotonic regulator, and a pH regulator. The concentration of the AST-3424 active ingredients of the injection is 0.001-1.000 mg/ml, the pH of the injection is 6.8-10.5, and the solution is an isotonic solution.
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 31/396 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à trois chaînons, p. ex. aziridine
The present invention provides an AKR1C3 inhibitor of compounds of the following formulas and pharmaceutically acceptable salts or solvates or isotopically substituted compounds thereof and medical use.
C07C 33/20 - Alcools monohydroxyliques ne contenant que des cycles aromatiques à six chaînons dans la partie cyclique monocycliques
C07C 205/38 - Composés contenant des groupes nitro liés à un squelette carboné le squelette carboné étant substitué de plus par des groupes hydroxy éthérifiés ayant des groupes nitro et des groupes hydroxy éthérifiés liés à des atomes de carbone de cycles aromatiques à six chaînons du squelette carboné à des atomes de carbone du même cycle aromatique à six chaînons non condensé ou à des atomes de carbone de cycles aromatiques à six chaînons faisant partie du même système cyclique condensé l'atome d'oxygène d'au moins un des groupes hydroxy éthérifiés étant lié de plus à un atome de carbone d'un cycle aromatique à six chaînons, p. ex. éthers nitrodiphényliques
The present invention belongs to the field of research and development of anticancer compounds. The technical problem solved by the present invention is to provide the simple isolation of anti-cancer compounds. In order to solve this technical problem, the inventors creatively introduced the fluorine-containing groups such as special trifluoromethyl groups, fluorine-substituted aryl groups, or heteroaryl groups at special positions (such as the position between the nitrobenzene ring and the phosphate amine group) in the structures of the existing compounds. After this modification, it was found that all of the resulting compounds shown in Formula II/III were solids (including solids and waxes). Thus, the present invention provides a fluorine-containing compound shown in Formula II/III and its anti-cancer medical use.
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35 - Publicité; Affaires commerciales
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Produits et services
Analgesics; drugs for medical purposes; chemical reagents
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cultures for medical purposes; reagent paper for medical
purposes; diagnostic biomarker reagents for medical
purposes; dietetic foods adapted for medical purposes;
dietetic beverages adapted for medical purposes. Advertising; online advertising on a computer network;
professional business consultancy; commercial intermediation
services; sales promotion for others; provision of an online
marketplace for buyers and sellers of goods and services;
retail services for pharmaceutical, veterinary and sanitary
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pharmaceutical, veterinary and sanitary preparations and
medical supplies. Teaching; instruction services; arranging and conducting of
colloquiums; arranging and conducting of conferences;
arranging and conducting of congresses; arranging and
conducting of seminars; arranging and conducting of
symposiums; publication of texts, other than publicity
texts; publication of books; online publication of
electronic books and journals. Technological research; research and development of new
products for others; scientific laboratory services;
scientific research; clinical trials. Telemedicine services; preparation of prescriptions by
pharmacists; therapy services; health counselling;
palliative care; medical analysis services for diagnostic
and treatment purposes provided by medical laboratories;
medical screening.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
35 - Publicité; Affaires commerciales
41 - Éducation, divertissements, activités sportives et culturelles
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Analgesics; drug delivery agents in the form of powders that provide controlled release of the active ingredients for a wide variety of pharmaceuticals; drug delivery agents in the form of tablets that provide controlled release of the active ingredients for a wide variety of pharmaceuticals; drug delivery agents in the form of capsules that provide controlled release of the active ingredients for a wide variety of pharmaceuticals; drug delivery agents consisting of compounds that facilitate delivery of a wide range of pharmaceuticals; chemical reagents for medical or veterinary purposes; biological tissue cultures for medical purposes; reagent paper for medical purposes; diagnostic biomarker reagents for medical purposes; dietetic foods adapted for medical purposes; dietetic beverages adapted for medical purposes Advertising; online advertising on a computer network; professional business consultancy; sales promotion for others; provision of an online marketplace for buyers and sellers of goods and services; Retail store services for pharmaceutical, veterinary and sanitary preparations and medical supplies; wholesale distributorship services for pharmaceutical, veterinary and sanitary preparations and medical supplies Education services, namely, training educators in the field of science, technology, engineering and mathematics (STEM) curriculum, teaching methods and providing curricula in connection therewith; education services, namely, training educators to teach through service learning and civic engagement and providing curricula in connection therewith; Educational services, namely, conducting classes, seminars, conferences, workshops, retreats, camps and field trips in the field of pet care, math, tax preparation and distribution of training material in connection therewith; publication of texts, other than publicity texts; publication of books; multimedia publishing of books, magazines, journals, software, games, music, and electronic publications Research and development of advanced learning technologies and teaching methods; research and development of new products for others; scientific laboratory services; scientific research; medical and scientific research, namely, conducting clinical trials for others Telemedicine services; preparation of prescriptions by pharmacists; medical, physical rehabilitation and physical therapy services; chemotherapy services; health counseling; palliative care; medical analysis services for diagnostic and treatment purposes provided by medical laboratories; medical screening
The present disclosure is related to a method and composition for treating leukemia. The method comprises administering subject in need with an effective amount of a compound named OBI-3424 or OBI-3423. It shows particular efficacy in treating acute lymphoblastic leukemia (ALL), including T-ALL and B-ALL.
