- Method for simply preparing high-purity olopatadine hydrochloride intermediate (by machine translation)
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The invention provides a simple and convenient method for preparing high-purity [3 - (dimethylamine) propyl] triphenylphosphonium bromide hydrobromide. The obtained (1,3 - bromopropyl) triphenylphosphonium bromide does not need to be separated, and is directly reacted with a dimethylamine aqueous solution in n-heptane so as to obtain [3 - 3 - (dimethylamine) propyl] triphenyl phosphonium bromide hydrobromide crude product which is obtained by hot pulping with anhydrous ethanol to obtain the high-purity [3 - 3 - (dimethylamine) propyl] triphenylphosphonium bromide hydrobromide. (by machine translation)
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Paragraph 0048-0072; 0076-0083
(2020/08/26)
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- HYDROXYLATED TRICYCLIC COMPOUNDS
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The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are diff
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Page/Page column 68
(2012/06/30)
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- Polymorphic forms of olopatadine hydrochloride and methods for producing olopatadine and salts thereof
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The present invention provides a novel polymorphic form of olopatadine hydrochloride ([(Z)-3-(dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid hydrochloride), a selective histamine H1-receptor antagonist that is used for the treatment of ocular symptoms of seasonal allergic conjunctivitis. The present invention also provides novel methods for producing olopatadine on a large scale, and in a manner that is cost effective, provides a low level of impurities and eliminates the need to use the costly and dangerous base, butyllithium, which is used in prior art reactions for making olopatadine. The present invention further provides novel processes for carrying out a large scale production of 3-dimethylaminopropyltriphenylphosphonium bromide and its corresponding hydrobromide salt, which are employed in the production of olopatadine, and pharmaceutically acceptable salts of olopatadine.
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Page/Page column 24
(2008/06/13)
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- DIBENZ[B,E]OXEPIN DERIVATIVE AND PHARMACEUTICAL COMPOSITIONS THEREOF
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Novel dibenz[b,e]oxepin derivatives are employed in the treatment and control of allergic conditions such as allergic asthma and also employed in the treatment of inflammation.
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- 7H-dibenzo(a,c,)cyclohepten-5-one-(7) derivatives
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The invention is concerned with 7H-dibenzo(a,c)-cyclohepten-5-one-(7) derivatives of general formula I STR1 wherein R1 and R2 can be the same or different, a hydrogen atom, an alkyl radical containing 1 to 3 carbon atoms, or, together with the nitrogen atom to which they are attached form a heterocyclic ring containing 3 to 6 carbon atoms, n is 2 or 3 R3 is a hydrogen atom or a halogen atom and X is either a methylene radical or an oxygen atom and the pharmacologically acceptable salts thereof with inorganic and organic acids. The invention is furthermore concerned with analogous processes for the preparation thereof and their application for controlling psychic diseases and gastric and/or intestinal ulcers.
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