4-anilino quinazoline derivatives for the treatment of abnormal cell growth
A kind of abnormal cell growth, alkyl technology, applied in the new bicyclic derivatives, pharmaceutical compositions containing such compounds, substances, the field of treatment of mammals, can solve the problem of no effect, weakened growth, etc.
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[0059] The invention also relates to the preparation of the general formula 1 A method of a compound comprising the steps of preparing the compound by a synthetic method.
[0060] The present invention also relates to a method for treating abnormal cell growth in mammals, including humans, comprising administering to the mammal an effective amount of the above formula for treating abnormal cell growth 1 A compound or a pharmaceutically acceptable salt, solvate, hydrate or prodrug thereof. In one embodiment of the method, said abnormal cell growth is cancer, including, but not limited to, lung cancer, bone cancer, pancreatic cancer, skin cancer, head or neck cancer, skin or intraocular melanoma, uterine cancer, Ovarian cancer, rectal cancer, anal region cancer, stomach cancer, colon cancer, breast cancer, fallopian tube cancer, endometrial cancer, cervical cancer, vaginal cancer, vulvar cancer, Hodgkin's disease, esophagus cancer, small intestine cancer, endocrine system cance...
Embodiment 1
[0139] General approach to biotransformation
[0140] Those skilled in the art can contact the substance to be transformed and other necessary reactants with various living microorganisms or their derived enzymes under conditions suitable for chemical reactions to complete biotransformation. The reaction products are then isolated and the desired substance is purified for elucidation of its chemical structure and physical and biological properties. Enzymes can be present as pure reagents, crude extracts or lysates, intact cells, solutions, suspensions, covalently bound to carrier surfaces, or embedded in permeable matrices (e.g., agarose or alginate particles). Substrates and other necessary reactants (eg, water, air, cofactors) are supplied to chemical specifications.
[0141] Typically, the reaction is carried out in the presence of one or more liquid phases - aqueous and / or organic - to facilitate mass transfer of reactants and products. Reactions may or may not be perfo...
Embodiment 2
[0145] Preparation of E-N-(3-{4-[3-hydroxymethyl-4-(6-methyl-pyridin-3-yloxy)-phenylamino]-quinazolin-6-yl}- by microbial transformation Allyl)-2-methoxy-acetamide.
[0146] Add 50 milliliters (50 mL) of IOWA medium (anhydrous glucose 20 g; yeast extract 5 g; dipotassium hydrogen phosphate 5 g; sodium chloride 5 g; soybean powder 5 g; distilled water 1 L) into 29 250 mL Erlenmeyer flasks with foam stoppers. ; adjusted to pH 7.2 with 1N hydrochloric acid), steam sterilized at 15 psig and 121°C for 20 minutes. Three flasks were aseptically inoculated with 0.5 mL of cryopreserved (-80°C) mycelia of Streptomyces albulus (ATCC 12757). The inoculated flasks were mounted vertically on a rotary shaker (2 inch stroke) and shaken at 210 rpm for 2 days at 29°C (inoculum phase). Then, 5 mL of the inoculum stage culture was aseptically transferred to the remaining 26 flasks (biotransformation stage). The inoculated biotransformation flask was mounted vertically on a rotary shaker (2 inc...
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