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341 results about "Gefitinib" patented technology

Gefitinib is used to treat lung cancer.

Pyrimidoheterocyclic compound, medicinal composition and application thereof

The invention discloses a pyrimidoheterocyclic compound represented as the formula (I), or a pharmaceutically acceptable salt or a stereisomer thereof, or a prodrug molecule thereof. The pyrimidoheterocyclic compound can effectively inhibit growth of various tumor cells and has an inhibiting effect on EGFR protease. The pyrimidoheterocyclic compound can be used for preparing an anti-tumor drug, and can overcome drug resistance caused by medicines in the prior art, such as gefitinib, erlotinib and the like, has a selectivity on wild non-small cell lung cancer and is excellent in pharmacokinetic property.
Owner:GUANGZHOU INST OF BIOMEDICINE & HEALTH CHINESE ACAD OF SCI

3-(2-pyrimidine amino) phenyl acrylic amide compound and application thereof

The present invention discloses a 3-(2-pyrimidine amino) phenyl acrylic amide compound in the structure of formula (I) or a pharmaceutically acceptable salt or a stereisomer or a prodrug molecule. The 3-(2-pyrimidine amino) phenyl acrylic amide compound or the pharmaceutically acceptable salt can effectively inhibit the growth of various tumor cells, and inhibit EGFR (epidermal growth factor receptor), HER (human epidermal receptor2) family other protease, can be used in the preparation of antitumor drugs, and can overcome the drug resistance induced by gefitinib, erlotinib and the like.
Owner:PHARMA SHANGHAI

Methods and Compositions for Detecting a Drug Resistant Egfr Mutant

Polymerase chain reaction primers and methods directed to detecting the EGFR mutant C→T at the position corresponding to base 2369 of EGFR cDNA. The invention provides a PCR primer that hybridizes under suitable PCR conditions to a polynucleotide sequence 5′ in each respective strand to a mutation of an EGFR gene that encodes a substitution of threonine by methionine at position 790 of the EGFR polypeptide. The invention also provides a PCR primer hybridizes to a sequence that includes a mutant T at the position corresponding to base 2369 of EGFR cDNA but not to a second EGFR polynucleotide containing a wild type C. The invention provides several methods and kits for detecting a mutant epidermal growth factor receptor (EGFR) gene in a sample comprising probing the sample with a means for selectively detecting a nucleotide sequence comprising a mutant T at the position corresponding to base 2369 of EGFR cDNA, and identifying that the base at said position is T. These methods and kits are also useful to predict resistance to the therapeutic effects of gefitinib or erlotinib in a subject suffering from or suspected of having a cancer.
Owner:MEMORIAL SLOAN KETTERING CANCER CENT

Compounds for immunopotentiation

Methods of stimulating an immune response and treating patients responsive thereto with 3,4-di(1H-indol-3-yl)-1H-pyrrole-2,5-diones, staurosporine analogs, derivatized pyridazines, chromen-4-ones, indolinones, quinazolines, nucleoside analogs, and other small molecules are disclosed. In a preferred embodiment benzopyrimidine derivatives such as ZD-6474, MLN-518, lapatinib, gefitinib or erlotinib are used.
Owner:NOVARTIS VACCINES & DIAGNOSTICS INC

Pentadeuteropyridine compounds, and preparation method, pharmaceutical compositions and uses thereof

The invention relates to pentadeuteropyridine compounds represented by the following formula (I) and pharmaceutically acceptable salts, stereoisomers, prodrugs and solvates thereof, and a preparation method, pharmaceutical compositions and uses thereof. The compounds can generate an inhibitory effect on variation forms of epidermal growth factor receptor (EGFR) protein kinase, thereby effectively inhibiting the growth of a variety of tumor cells; the compounds can be used for preparation of antitumor drugs, are used for treatment or prevention of a plenty of different cancers, and moreover, can overcome the drug resistance induced by conventional drugs gefitinib, erlotinib and other first-generation EGFR inhibitors. More specifically, the compounds can be used for preparation of drugs for treatment or prevention of diseases, obstacles, disorders or illness conditions mediated by certain variation-form epidermal growth factor receptors (such as L858R activated mutants, Exon19 deletion activated mutants, and T790M resistance mutants).
Owner:INVENTISBIO CO LTD +1

A kind of gefitinib dispersible tablet and its preparation method and application

The invention discloses a gefitinib dispersible tablet, a preparation method and an application thereof. The gefitinib dispersible tablet of the invention comprises the following components by weight: 10-65% of gefitinib, 1-30% of fillers, 10-50% of disintegrants, 1-60% of acidifiers, 0.1-20% of adhesives, and 0.1-30% of lubricants and glidants. According to the invention, gefitinib is wrapped bythe acidifier or gefitinib and the acidifier are wrapped with each other so as to reach the embedding effect. Compared with commercially available common tablets, the gefitinib dispersible tablet of the invention does not contain surfactants, has good dissolvability, dispersibility and disintegrability, and can be disintegrated completely within one minute. The gefitinib dispersible tablet prepared by the method of the invention has a high dissolution rate, good bioavailability, rapid distribution in vivo, and stable quality, and the preparation method is simple and practical, and is applicable to industrial production.
Owner:GUANGDONG PHARMA UNIV

4- fragrant amido quinazoline derivatives and method of manufacturing the same and application in pharmacy thereof

The invention relates to a 4-aromatic aminoquinazoline compounds with general formula of (I) or a receivable salt pharmaceutically and the application in preparing the drugs for treating the tumour. Wherein, R1, R2 are hydrogen, halogen, nitryl, amino, alkyl of C1-6, alkylamino of C1-6 or alkoxy of C1-6, or the group replaced by the alkylamino on the terminal of the alkyl of C1-6, alkylamino and alkoxy; X is N,O or S; Ar is aromatic ring or heteroaromatic groups replaced by the ester of C5 to C8. The invention can inhibit the increase of the tumour cell obviously and has obvious inhibited effect on the tyrosine kinase of the cell, and has activity equal to that of the positive drugs Gefitinib and Erlotinib and even exceeds the positive control.
Owner:SOUTHEAST UNIV

Preparing method for gefitinib

InactiveCN101148439AHigh yieldReduce manufacturing costOrganic chemistryMorpholine3-chloro-4-fluoroaniline
The process of preparing gefitinib, 4-(3-chloro-4-fluorophenylamido)-7-methoxyl-6-[3-(4- morpholinyl) propoxy] quinazoline, includes following steps: 1. reaction of 3-hydroxy-4-methoxy methyl benzoate as material and 4-(3-chloropropyl) morpholine to obtain 4- methoxyl-3-[3-(4- morpholinyl) propoxy] methyl benzoate; 2. nitration to obtain 2-nitro-4- methoxyl-5-[3-(4- morpholinyl) propoxy] methyl benzoate; 3. reduction to obtain 2-amino-4- methoxyl-5-[3-(4- morpholinyl) propoxy] methyl benzoate; 4. closing cycle to create 7- methoxyl-6-[3-(4- morpholinyl) propoxy] quinazoline-4(3H)-one; 5. chlorinating to obtain 4-chloro-7- methoxyl -6-[3-(4-morpholinyl) propoxy] quinazoline; and 6. reaction to 3-chloro-4-fluoroaniline to obtain gefitinib.
Owner:SOUTHEAST UNIV

Pyrimidoheterocyclic compound and its pharmaceutical composition and application

The invention discloses a pyrimidoheterocyclic compound represented as the formula (I), or a pharmaceutically acceptable salt or a stereisomer thereof, or a prodrug molecule thereof. The pyrimidoheterocyclic compound can effectively inhibit growth of various tumor cells and has an inhibiting effect on EGFR protease. The pyrimidoheterocyclic compound can be used for preparing an anti-tumor drug, and can overcome drug resistance caused by medicines in the prior art, such as gefitinib, erlotinib and the like, has a selectivity on wild non-small cell lung cancer and is excellent in pharmacokinetic property.
Owner:GUANGZHOU INST OF BIOMEDICINE & HEALTH CHINESE ACAD OF SCI

Pyrimido diazepine compound as well as pharmaceutical composition and application thereof

The invention discloses a 5,8-dioxo-pyrimido[4,5-e][1,4]diazepine compound of a structural formula (1) or a pharmaceutically acceptable salt or stereoisomer or prodrug molecule thereof. The 5,8-dioxo-pyrimido[4,5-e][1,4]diazepine compound has the effects of effectively inhibiting the growth of various tumor cells and the generation of the EGFR (epidermal growth factor receptor), can be used for preparing anticancer medicaments and can overcome the resistance of the existing medicaments including the gefitinib, the erlotinib and the like.
Owner:GUANGZHOU INST OF BIOMEDICINE & HEALTH CHINESE ACAD OF SCI

Gefitinib Sensitivity-Related Gene Expression and Products and Methods Related Thereto

InactiveUS20070270505A1BiocideOrganic active ingredientsEgfr pathwayPolynucleotide
Disclosed is the identification, provision and use of a panel of biomarkers that predict sensitivity or resistance to gefitinib and other EGFR inhibitors, and products and processes related thereto. Specifically, a method is described for selecting a cancer patient who is predicted to benefit from therapeutic administration of an EGFR inhibitor, an agonist thereof, or a drug having substantially similar biological activity as EGFR inhibitor. Also described is a method to identify molecules that interact with the EGFR pathway to allow or enhance responsiveness to EGFR inhibitors, as well as a plurality of polynucleotides or antibodies for the detection of the expression of genes that are indicative of sensitivity or resistance to EGFR inhibitors, an agonist thereof, or a drug having substantially similar biological activity as EGFR inhibitors. A method to identify a compound with the potential to enhance the efficacy of EGFR inhibitors is also described.
Owner:UNIV OF COLORADO THE REGENTS OF

Inhalation-type pharmaceutical composition for the treatment of lung cancer and preparation method thereof

The present invention provides an inhalation-type pharmaceutical composition for lung cancer and preparation method thereof, comprising a first gas and an atomized medicine. The first gas comprises hydrogen. The gas volume concentration of hydrogen in the inhalation-type pharmaceutical composition is between 2 to 96%. The atomized medicine is selected from a group comprising cisplatin, docetaxel, etoposide, gefitinib, erlotinib, and any combination thereof. The inhalation-type pharmaceutical composition of the present invention can remove harmful radicals in the body of the patient through the use of hydrogen while also increases the absorption effect of the medicine for the patient by using an atomized medicine. At the same time, because the use of the small amount of the vaporized pharmaceutical liquid can indirectly reduce the side effects on the user.
Owner:LIN HSIN YUNG

Gefitinib medicinal composition and tablet containing gefitinib medicinal composition

The invention belongs to the field of medicinal preparations, and provides a gefitinib medicinal composition and a tablet thereof. The gefitinib medicinal composition contains polyacrylic resin substances. By adopting the provided composition and tablet, the precipitating speed of gefitinib from a solution can be well controlled, and the bioavailability of gefitinib is improved.
Owner:JIANGSU AOSAIKANG PHARMA CO LTD

New preparation method for crystal form Gefitinib Form 1

The invention provides a new preparation method for a crystal form Gefitinib Form 1, which comprises the following steps: dissolving Gefitinib into one type or multiple types of solvents of ethanol, isopropanol and butyl alcohol; cooling; and crystallizing to prepare the crystal form Gefitinib Form 1.
Owner:HAINAN SIMCERE PHARMA CO LTD

Medicinal composition for treating non-small cell lung cancer and application thereof

The invention discloses a medicinal composition for treating non-small cell lung cancer. The medicinal composition comprises a target medicament, a chemotherapeutic medicament and a traditional Chinese medicament, wherein the target medicament is one or more of bortezomib, imatinib, gefitinib and sunitinib; the chemotherapeutic medicament is one or more of 5-fluorouracil, carboplatin, epirubicin, adriamycin and fludarabine; and the traditional Chinese medicament is one or more of salvia miltiorrhiza, astragalus membranaceus, sappanwood, Chinese pulsatilla root and portulaca oleracea. The medicinal composition has a remarkable synergetic treatment effect when being used for treating the non-small cell lung cancer, and can be used for remarkably strengthening the cancer-inhibition effect compared with treatment of a single medicament, so that the medicament dosage can be reduced, and the toxic and side effects of chemotherapeutic medicaments can be reduced.
Owner:NORTHWEST A & F UNIV

Drug composition containing gefitinib

The invention relates to a drug composition containing gefitinib, in particular to a tablet comprising the gefitinib. The tablet containing the gefitinib is made of the gefitinib with the particle size distribution as follows: D(0.1) is equal to 2-6mm, D(0.5) is equal to 11-20mm, and D(0.9) is equal to 35-50mm. According to the drug composition, active ingredients can be released continuously and stably, and the drug composition has a good treatment effect on the local advanced lung cancer or metastatic non-small cell lung cancer subjected to the chemotherapy in the past.
Owner:江苏万高药业股份有限公司

Targeted anti-cancer molecule gefitinib phthalocyanine conjugate, and preparation and application thereof

The invention discloses a targeted anti-cancer molecule gefitinib phthalocyanine conjugate, and a preparation method and application thereof. The molecular formula of the gefitinib phthalocyanine conjugate is C56+2nH42+4nO5+nClFN12Zn (n=2-8). Gefitinib with an alkoxyl long chain is introduced into the periphery of a metal phthalocyanine large ring, so the amphipathicity and the biocompatibility can be improved, and the targeting property of a photosensitizer is enhanced. The gefitinib phthalocyanine conjugate is difficult to aggregate, so the cellular uptake ratio is increased and the activity of the photosensitizer in photodynamic therapy is also enhanced. The compound has single structure, is not provided with an isomer, and is easy to purify. A synthesis method is simple, little in side reaction, high in yield, easily available in raw materials, low in cost and favorable for industrialized production.
Owner:FUZHOU UNIV

Method of treatment of philadelphia chromosome positive leukaemia

InactiveUS20120244116A1Organic active ingredientsPeptide/protein ingredientsBcr-Abl tyrosine-kinase inhibitorLestaurtinib
The invention provides a method for the treatment of Ph+ leukemia in a patient comprising administering to the patient (i) a BCR-ABL tyrosine kinase inhibitor, and (ii) an agent which selectively binds to a cell surface receptor expressed on Ph+ leukemic stem cells. The invention further provides for the use of (i) and (ii) in, or in the manufacture of a medicament for, the treatment of Ph+ leukemia in a patient; and a composition for the treatment of Ph+ leukemia in a patient comprising (i) and (ii); and kits comprising (i) and (ii). In some embodiments, the tyrosine kinase inhibitor is or is not imatinib; or is selected from the group consisting of dasatinib, nilotinib, bosutinib, axitinib, cediranib, crizotinib, damnacanthal, gefitinib, lapatinib, lestaurtinib, neratinib, semaxanib, sunitinib, toceranib, tyrphostins, vandetanib, vatalanib, INNO-406, AP24534, XL228, PHA-739358, MK-0457, SGX393 and DC2036; or is selected from the group consisting of dasatinib and nilotinib. In some embodiments, the agent binds to a receptor involved in signalling by at least one of IL-3, G-CSF and GM-CSF. In some embodiments, the agent is a mutein selected from the group consisting of IL-3 muteins, G-CSF muteins and GM-CSF muteins. In some embodiments, the mutein is an IL-3 mutein. In some embodiments, the agent is a soluble receptor which is capable of binding to IL-3.
Owner:CSL LTD

Eutectic complex composed of resveratrol and protein kinase inhibitor, and composition comprising eutectic complex

The invention provides a eutectic complex composed of resveratrol and a protein kinase inhibitor, and a composition comprising the eutectic complex. The eutectic complex is characterized in that the protein kinase inhibitor is selected from one of imatinib, gefitinib, erlotinib, sunitinib, sorafenib, dasatinib, lapatinib, nilotinib, pazopanib, afatinib, crizotinib, axitinib, regorafenib, ibrutinib, lenvatinib, palbociclib, osimertinib and alectinib or pharmaceutically acceptable salt thereof. The eutectic complex provided by the invention can produce synergistic effects of inhibiting histamine release.
Owner:黄泳华

Pyrimidine or pyridine compounds, preparation method therefor and pharmaceutical uses thereof

The present invention disclosed a class of pyrimidine or pyridine compounds, pharmaceutically acceptable salts, stereoisomers, prodrugs and solvates thereof, preparation method therefor and pharmaceutical compositions and pharmaceutical uses thereof. The compounds can inhibit the variants of EGFR (Epidermis Growth Factor Receptor) proteinases, and therefore can inhibit the growth of a variety of tumor cells effectively. The compounds can be used to prepare antitumor drugs, used for the treatment, combined therapy or prevention of various different cancers. The compounds can overcome the drug resistance induced by the existing first-generation EGFR inhibitors such as gefitinib, erlotinib and so on. Particularly, the compounds can be used to prepare drugs for treating or preventing diseases, disturbances, disorders or conditions mediated by epidermis growth factor receptor variants (such as L858R activated mutants, Exon19 deletion activated mutants and T790M resistant mutants).
Owner:INVENTISBIO CO LTD

New gefitinib crystal form and preparation method thereof

The invention relates to a new crystal form alpha crystal form of gefitinib and a preparation method thereof. The crystal form has the strongest characteristic peak at a position where a 2theta angle is 7.12 on an X ray powder diffraction (XRPD) pattern, and has main characteristic peaks at positions where the 2theta angle are respectively 7.12, 24.349 and 26.435, wherein the relative strength of the main characteristic peaks are greater than 60%. The preparation method comprises: (a) adding gefitinib into a strong polarity solvent, and dissolving; (b) adding a smaller polarity anti-solvent into the solution, separating out crystals; (c) filtering, drying, and obtaining an almost white solid. The alpha crystal form is easy to prepare, good in stability and preparation formability, simple in preparation technology and mild in conditions; and the whole preparation process is carried out in 10 hours or less, so that the production efficiency is improved substantially, and the alpha crystal form is more suitable for industrialization production.
Owner:CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD +1

Quinazoline fluorescent probe as well as preparation method and application thereof

InactiveCN104212440AWith diagnostic functionWith therapeutic functionOrganic active ingredientsOrganic chemistryCancer cellCancers diagnosis
The invention discloses a quinazoline fluorescent probe and a preparation method thereof. The fluorescent probe structure is fluorescein-labeled Gefitinib, and has relatively strong inhibitory activity on EGFR protein kinase and potential cancer treatment effect; according to confocal fluorescence imaging results, the fluorescent probe is uniformly distributed on a cell membrane after being acted with a plurality of cell strains, and can be used for cancer cell imaging. According to tested results of flow cytometry, the intensification factor of the cell fluorescence intensity has positive correlation property with the EGFR content in the cell. By virtue of a flow cytometry technology, the fluorescent probe can be applied to relative quantification detection of a biomarker EGFR in the cell, so that relatively direct information is provided for cancer diagnosis. The fluorescent probe has functions of diagnosing and treating cancers, can be used for directly detecting living cells, is quick to analyze, simple and convenient to operate and low in cost, and has a development and application value.
Owner:无锡艾德美特生物科技有限公司

Methods and compositions for predicting resistance to anticancer treatment

The instant application provides methods and related compositions pertaining to the identification of resistance to anticancer treatment in a patient. In a particular embodiment, the invention provides biomarkers for the identification of resistance to anticancer treatment in a lung cancer patient, wherein a reduced expression of a MEDIATOR and / or SW1 / SNF complex gene in the lung cancer cells of the patient indicates that the lung cancer cells in the patient may be resistant to treatment with a receptor tyrosine kinase inhibitor, such as gefitinib and / or erlotinib. In some embodiments, the invention relates to methods and related compositions for predicting resistance to anticancer treatment by detecting the expression levels of one or more TGF-beta pathway nucleic acids and / or proteins.
Owner:STICHTING HET NEDERLANDS KANKER INSTIUUT ANTONI VAN LEEUWENHOEK ZIEKENHUIS

Method for preparing gefitinib and intermediate thereof

The invention relates to a preparation method of an anilinoquinazoIine compound, in particular to a method for preparing gefitinib and an intermediate thereof. The preparation method of the invention not only avoids the use of highly-pollutant halogenating agents to greatly reduce environmental pollution, but is also characterized by the connection with a 3-halogenated propyl side chain at first prior to the synthesis of a quinazoline parent ring and then introduction of a morpholine ring at the last step of the synthesis, thus repeated adjustment for pH value in the purification of a reaction product of every step is avoided, a purification method is simplified and the yield is raised.
Owner:SHAANXI NORMAL UNIV +2

Drug composition for curing tumour diseases

The invention discloses a drug composition for curing tumour diseases, which comprises fixed dose of N-(4-(1-cyanocyclopentyl) phenyl)-2-(4-picolyl) amino-3-pyridinecarboxamide or pharmaceutically acceptable salt of the N-(4-(1-cyanocyclopentyl) phenyl)-2-(4-picolyl) amino-3-pyridinecarboxamide and erlotinib or pharmaceutically acceptable salt of the erlotinib or comprises fixed dose of N-(4-(1-cyanocyclopentyl) phenyl)-2-(4-picolyl) amino-3-pyridinecarboxamide or pharmaceutically acceptable salt of the N-(4-(1-cyanocyclopentyl) phenyl)-2-(4-picolyl) amino-3-pyridinecarboxamide and gefitinib or pharmaceutically acceptable salt of the gefitinib. A method for preparing the drug composition and an application of the drug composition in preparing drugs for curing tumour diseases are further provided.
Owner:JIANGSU HENGRUI MEDICINE CO LTD

Method of treatment of EGFR inhibitor toxicity

The invention provides a method of treating and / or preventing a toxicity associated with epidermal growth factor receptor (EGFR) inhibitor therapy in a subject, the method comprising administering to the subject an effective amount of a steroid sulfatase (STS) inhibitor. The toxicity may be ocular toxicity; or dermatologic toxicity, such as papulopustular rash. The EGFR inhibitor may be selected from the group consisting of: a small molecule; an antibody or derivative or fragment thereof; another agent that targets the extracellular or intracellular domain of the EGFR, such as a tyrosine kinase inhibitor selected from the group consisting of: erlotinib; gefitinib; lapatinib; and any combination thereof. The EGFR inhibitor may also be antibody selected from the group consisting of: cetuximab; panitumumab; and any combination thereof.Preferably the STS inhibitor is selected from the group consisting of: alternative STS substrates; reversible STS inhibitors; and irreversible STS inhibitors; and any combination thereof. A preferred STS inhibitor is the irreversible nonsteroidal STS inhibitor STX64.In some embodiments, the subject receiving EGFRI therapy has a cancer comprising cells that express wildtype k-ras and / or wildtype b-raf. In other embodiments, the cancer may be hormone-dependent. Cancers that may be treated with EGFRI therapy include colorectal cancer and non-small cell lung cancer.
Owner:PETER MACCALLUM CANCER INST

Methods for Inhibiting Cell Proliferation in EGFR-Driven Cancers

The invention features a method for treating patients who have an EGFR-driven cancer, which is, or has become, refractory to a tyrosine kinase inhibitor, such as eriotinib and gefitinib, by administering a compound of formula (I) to the patient. The invention also features treating EGFR-driven cancers having an EGFR mutation identified herein.
Owner:ARIAD PHARMA INC

Crystal forms A, H and I of barrack gefitinib phosphate and preparation methods thereof

The invention provides crystal forms A, H and I of barrack gefitinib phosphate as shown in a formula (I). The formula (I) is as shown in the specification, wherein the XRPD atlas of the crystal form A has diffraction peaks at angles 2theta of 8.38, 8.88, 10.48, 13.00, 15.06, 16.22, 16.82, 17.76, 19.18, 19.70, 21.04, 22.22, 22.68, 24.40, 24.94, 26.48 and 27.40, and the 2theta value error range is + / -0.2. The crystal forms A, H and I of barrack gefitinib phosphate have stability approximate to that of an existing crystal form X of barrack gefitinib phosphate, have solubility higher than that of the crystal form X, are enhanced in bioavailability, and are beneficial to use in pharmaceutical processing and pharmaceutical compositions.
Owner:SHANGHAI SUNTRONG BIOTECH
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