- Method for preparing high-purity carmustine
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The invention provides a method for preparing high-purity carmustine. Specifically, the preparation method comprises a step of recrystallizing a crude carmustine product with an organic solvent, wherein the organic solvent is a mixed solvent of an alcohol solvent and water, and the alcohol solvent is preferably at least one selected from the group consisting of methanol, ethanol and isopropanol. The method can be used for preparing high-purity carmustine.
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Paragraph 0062-0063; 0066-0082
(2020/04/17)
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- SAFE AND EFFICIENT PROCESS FOR THE PREPARATION OF CARMUSTINE
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Carmustine may be safely and efficiently produced by reacting 2-chloroethylamine hydrochloride and 1,1′-carbonyldiimidazole to afford 1,3-bis(2-chloroethyl)-1-urea, followed by nitrosation to give the final product.
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Paragraph 0074-0077
(2017/09/25)
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- AN IMPROVED PROCESS FOR THE PREPARATION OF 1,3-BIS(2-CHLOROETHYL)-1-NITROSOUREA
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The present invention relates to an improved process for the preparation of 1,3-bis(2-chloroethyl)-1 -nitrosourea compound of formual-1 which is represented by the following structural formula:
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Page/Page column 10; 11
(2017/09/27)
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- PROCESS FOR PREPARATION OF CARMUSTINE
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The present invention relates to an improved process for preparation of carmustine (I). The present invention also relates to preparation of 1,3-bis(2-chloroethyl)urea (II) an intermediate used in preparation of carmustine.
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Page/Page column 9
(2017/11/10)
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- Concatamers for Immunemodulation
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The invention relates to a polymeric, non-coding nucleic acid molecule for modulation of the activity of the human and animal immune system as well as a method for the manufacture thereof and a vaccine, comprising the polymeric, non-coding nucleic acid molecule, wherein polymeric, non-coding nucleic acid molecules may be understood as non-coding nucleic acid molecules, comprising at least four covalently bound molecules (tetramer) or are assemblies of more non-coding nucleic acid molecules (high molecular polymers) which are covalently bound to each other.
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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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- Tin(IV) chloride-sodium nitrite as a new nitrosating agent for N-nitrosation of amines, amides and ureas under mild and heterogeneous conditions
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We have developed a new method of N-nitrosation of various secondary and tertiary amines, amides and ureas using a mixture of tin(IV) chloride and sodium nitrate. This method leads to a selective, high-yielding and mild heterogeneous N-nitrosation by in situ generation of nitrosyl chloride (NOCl). The reaction can be carried out in several different solvents such as chloroform, dichloromethane, ethers, ethyl acetate and alcohols, at room temperature. Georg Thieme Verlag Stuttgart.
- Celaries, Benoit,Parkanyi, Cyril
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p. 2371 - 2375
(2008/02/03)
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- Method of treating nausea and vomiting with certain substituted-phenylalkylamino (and aminoacid) derivatives and other serotonin depleting agents
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A method for the treatment of emesis in a mammal, which method comprises administering to said mammal an emesis inhibiting amount of a compound which depletes serotonin in the brain of mammals; among which are compounds having the formula: STR1 wherein, R is selected from hydrogen, loweralkyl, trifluoromethyl, carboxyl, or loweralkoxycarbonyl; R1 and R2 are hydrogen or loweralkyl; Z is trifluoromethyl or halogen; the optical isomers and pharmaceutically acceptable salts thereof; two of the preferred compounds of the invention are fenfluramine and norfenfluramine.
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- 1,2,2,2-Tetrachloroethyl Carbamates: Versatile Intermediates for the Synthesis of N-Nitrosoureas
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1,2,2,2-Tetrachloroethyl carbamates 3 were prepared by the reaction of 1,2,2,2-tetrachloroethyl carbonochloridate with amines.Carbamates 3 were then nitrosated and reacted with amines to yield N-nitrosoureas.
- Barcelo, Gerard,Senet, Jean-Pierre,Sennyey, Gerard
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p. 1027 - 1029
(2007/10/02)
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- Process of preparing 1,3-bis(2-chloroethyl)-1-nitrosourea
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A method of producing 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) by nitrosation of 1,3-bis(2-chloroethyl)-urea utilizing as a nitrosating agent dinitrogen trioxide (N2 O3) in molar excess of theoretical wherein the molar excess of N2 O3 ranges from 10-200% and preferably from 10-20%. The nitrosation reaction is conventionally carried out in the cold from 0° C to -20° C and a non-aqueous solvent is utilized. The preferred non-aqueous solvent is of the chlorinated variety; i.e., methylene dichloride. Other preferred solvents include related halogenated compounds such as ethylene dichloride, nitro-compounds such as nitromethane, acetonitrile, and simple ethers such as ethyl ether. Other less preferred but operable compounds include esters such as ethyl acetate, simple ketones such as acetones, and chloroform. Solvents to be avoided are olefins, unsaturated ethers and other unsaturated compounds, amines, malonate esters, acid anhydrides, and solvents which would interact with the reactant N2 O3 and the urea as well as the product nitrosourea.
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