- Preparation method of medroxyprogesterone acetate for perimenopausal syndrome
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The invention relates to a preparation method of medroxyprogesterone acetate for perimenopausal syndrome. Compared with the prior art, the preparation method disclosed by the invention has the advantages of few steps, simplicity in operation, short total reaction time, high yield, less raw material consumption, low cost, good product quality and the like. The preparation method of medroxyprogesterone acetate has high economic value and is suitable for industrial application.
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- Preparation method of palace progesterone
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The invention relates to the technical field of preparation of pharmaceutical active pharmaceutical chemicals, in particular to a preparation method of palace progesterone. To the preparation method, 17 α - hydroxyl progesterone is used as a substrate, and nucleophilic addition reaction is carried out in sequence. An epoxidation reaction, an open-loop addition reaction, an elimination reaction, an esterification reaction and a hydrolysis reaction are adopted to obtain the toecliptin progesterone, and a precious metal catalyst and a carcinogenic solvent are not used in the preparation process simultaneously. ≥ 91%.
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- Preparation method of medroxyprogesterone acetate
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The invention provides a preparation method of medroxyprogesterone acetate. The preparation method comprises the following steps: using 6-methylene pregna-4-alkene-3, 20-diketone-17 alpha-acetic esteras a raw material, performing a hydrogenation reaction on the 6-methylene pregna-4-alkene-3, 20-diketone-17 alpha-acetic ester and cyclohexene in an alcohols solvent under the catalytic action of 5%palladium on carbon, and filtering and recovering palladium on carbon from reaction solution after the reaction is complete; performing transposition on the reaction solution with hydrochloric acid, adjusting the pH value of the reaction solution to 6-7, concentrating the reaction solution at normal pressure, as well as cooling, filtering, washing and drying the reaction solution, so as to obtaina medroxyprogesterone acetate crude product; finally, performing recrystallization with a mixed solvent of methanol and dichloromethane, so as to obtain a medroxyprogesterone acetate competitive product. According to the preparation method of the medroxyprogesterone acetate provided by the invention, the process method is simple, the alcohols solvent is adopted for the hydrogenation reaction, andthen the transposition is performed with hydrochloric acid, so that the content of the generated impurity F is low, the yield of a target product is high, the product cost is low, and the output of chemical pollutants is less, so that the preparation method is suitable for industrial production.
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Paragraph 0012; 0028; 0033; 0036-0040
(2018/03/26)
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- THERAPEUTIC FOR HEPATIC CANCER
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A novel pharmaceutical composition for treating or preventing hepatocellular carcinoma and a method of treatment are provided. A pharmaceutical composition for treating or preventing liver cancer is obtained by combining a chemotherapeutic agent with an anti-glypican 3 antibody. Also disclosed is a pharmaceutical composition for treating or preventing liver cancer which comprises as an active ingredient an anti-glypican 3 antibody for use in combination with a chemotherapeutic agent, or which comprises as an active ingredient a chemotherapeutic agent for use in combination with an anti-glypican 3 antibody. Using the chemotherapeutic agent and the anti-glypican 3 antibody in combination yields better therapeutic effects than using the chemotherapeutic agent alone, and mitigates side effects that arise from liver cancer treatment with the chemotherapeutic agent.
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- Anti-Claudin 3 Monoclonal Antibody and Treatment and Diagnosis of Cancer Using the Same
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Monoclonal antibodies that bind specifically to Claudin 3 expressed on cell surface are provided. The antibodies of the present invention are useful for diagnosis of cancers that have enhanced expression of Claudin 3, such as ovarian cancer, prostate cancer, breast cancer, uterine cancer, liver cancer, lung cancer, pancreatic cancer, stomach cancer, bladder cancer, and colon cancer. The present invention provides monoclonal antibodies showing cytotoxic effects against cells of these cancers. Methods for inducing cell injury in Claudin 3-expressing cells and methods for suppressing proliferation of Claudin 3-expressing cells by contacting Claudin 3-expressing cells with a Claudin 3-binding antibody are disclosed. The present application also discloses methods for diagnosis or treatment of cancers.
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- PROCESS FOR PREPARING 17ALPHA-ACETOXY-6-METHYLENEPREGN-4-ENE-3,20-DIONE, MEDROXYPROGESTERONE ACETATE AND MEGESTROL ACETATE
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The present invention relates to a process for preparing 17α-acetoxy-6-methylenepregn-4-ene-3,20-dione (4) as an intermediate, and to processes for preparing medroxyprogesterone acetate (1) (17α-acetoxy-6α-methylpregn-4-ene-3,20-dione) and megestrol acetate (2) (17α-acetoxy-6-methylpregna-4,6-diene-3,20-dione) via this intermediate (4).
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Page/Page column 3
(2009/01/24)
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- Anti-glaucomatous pharmaceutical composition and the process for obtaining them
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The invention relates to the domain of medicinal chemistry. It concerns more particularly that of the preparation of pharmaceutical compositions for ocular use. A subject of the invention is pharmaceutical compositions for ocular use characterized in that they contain at least one selected compound of steroidal structure in combination with or admixed with a pharmaceutically-acceptable, inert carrier or vehicle. The compositions according to the invention are intended to the treatment of glaucoma.
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- Cleavage of acetals promoted by copper (II) sulphate adsorbed on silica gel
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Copper sulphate supported on silica gel promotes the easy removal of cyclic acetals and tetrahydropyranyl ethers to give the respective parent carbonyl and hydroxyl compounds.
- Cabellero,Gros
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p. 395 - 404
(2007/10/02)
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- Method of contraception
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A three-phase method of human female contraception wherein (1) starting on about the ninth to about the twelfth day of the female cycle (first cycle day being first menstruation day) an effective amount of at least one progestagenic substance is administered in daily or shorter intervals for about three to about six days followed at substantially similar intervals by (2) administration for about one to about three days starting from about the fourth to about the seventh day after the first phase of both an effective amount of the progestagenic substance(s), and a peptide possessing LHRF (Luteinizing Hormone Release Factor) activity, followed by (3) administration of an effective amount of the progestagenic substance(s) until the total time of the progestagenic substance administration with and without the LHRF compound is from about seven to about fifteen days. A contraceptive preparation or pack comprising a suitable number of dosage units ranging from about seven to about fifteen corresponding with the total time abovementioned, of which the first three to six dosage units contained as hormonal compound only an effective amount of a progestagenic substance, followed by one to three dosage units containing an effective amount of an orally LHRF active peptide in addition to the noted level of progestagenic substance, with the remaining dosage units again containing only the progestagenic substance at the level noted.
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