- The preparation method of the megestrol (by machine translation)
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Megestrol preparation method, in order to 6 - keto - 17 a - acetoxy progesterone as raw material, the raw material in the organic solvent, in the original carboxylic acid triethyl ester existence under, with the glycol alkyd catalytic reaction double-[...]; then double [...] in the organic solvent, deprotecting reagent Grignard reaction, after the reaction in under the action of the strong acid, standard hydrolysis, at the same time deprotected, dehydration, by a two-step reaction to synthesize a megestrol crude; crude to decolorize with active carbon crystallization to, be a megestrol product, HPLC content 99.0 - 99.5%, melting point 213 - 220 °C, the weight of the two-step synthesis of the total yield of 80 - 85%. The invention relative to the traditional method, short synthetic route, the process operation is simple, production economy and environmental protection, the total synthesis than the traditional method to improve the yield of 30% or more, the production cost is reduced 30 - 35%; used in the process of recovering the solvent can be recycled, not only economic, environmental protection, and is favorable for industrial production. (by machine translation)
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Paragraph 0009; 0012; 0014; 0016
(2018/01/13)
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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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- Process for the preparation of 6-methyl-Δ4,6 -3-keto steroids
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A process for preparing 6-methyl-Δ4,6 -3-keto steroids of the formula STR1 comprises reacting a corresponding Δ4 -3-keto steroid with methoxymethyl acetate (CH3 --O--CH2 --OAc) in an inert solvent at temperatures above room temperature in the presence of an alkali metal acetate.
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- Water-soluble steroid compounds
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Beta-cyclodextrin forms a water-soluble complex or inclusion compound with steroid compounds having a molecular structure smaller than the interior cavity in the doughnut-shaped molecular structure of beta-cyclodextrin. The resulting inclusion compounds can be used for a variety of applications including aqueous topical ophthalmic preparations and topical dermatological ointments.
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- An One-step Synthesis of 17-Acetoxy-6-methyl-4,6-pregnadiene-3,20-dione (Megestrol Acetate) from 17-Acetoxy-4-pregnene-3,20-dione
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Starting from 17-Acetoxy-4-pregnene-3,20-dione (3), an one-step synthesis of megestrol acetate (5) is described.
- Annen, Klaus,Hofmeister, Helmut,Laurent, Henry,Wiechert, Rudolf
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p. 712 - 713
(2007/10/02)
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- Preparation of tritium labelled compounds. V. A group of steroids by catalytic reduction of unsaturated precursors with tritium gas
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A group of Δ4 3 keto steroids was prepared by catalytic reduction of suitable conjugated diene 3 keto precursors with tritium gas. Thus, 11α hydroxy 4 pregnene 3,20 dione 7 3H (I), 20α hydroxy 4 pregnen 3 one 7 3H (II), 6α methyl 4 pregnene 3,11,20 trione 7 3H (III), 17α hydroxy 6α methyl 4 pregnene 3,20 dione 7 3H, acetate (IV), and 17α hydroxy 6 methyl 3H3 16 methylenepregna 4,6 diene 3,20 dione, acetate (V) were prepared from 11α hydroxypregna 4,6 diene 3,20 dione (VI), 20α hydroxypregna 4,6 dien 3 one (VII), 6 methylpregna 4,6 diene 3,11,20 trione (VIII), 17α hydroxy 6 methylpregna 4,6 diene 3,20 dione, acetate (IX), and 17α hydroxy 6 dibromomethylene 16 methylene 4 pregnene 3,20 dione, acetate (X), respectively. In addition, 3α hydroxy 5β pregnane 11,20 dione 3H, cyclic 20 (trimethylene acetal) (XI) was prepared from I via 11α hydroxy 5β pregnane 3,20 dione 7 3H (XII), 5β pregnane 3,11,20 trione 7 3H (XIII) and 3α hydroxy 5β pregnane 11,20 dione 7 3H (XIV).
- Thomas,Ikeda,Campbell,Harpootlian
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