- DRUG DERIVATIVES
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The present invention relates to derivatives of known active pharmaceutical compounds. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more reactions which may be considered to represent a change of oxidation state. We refer to these compounds generally as redox derivatives. The derivatives of the invention may be related to the original parent active pharmaceutical compound by only a single step transformation, or may be related via several synthetic steps including one or more changes of oxidation state. In certain cases, the functional group obtained after two or more transformations may be in the same oxidation state as the parent active compound (and we include these compounds in our definition of redox derivatives). In other cases, the oxidation state of the derivative of the invention may be regarded as being different from that of the parent compound. In many cases, the compounds of the invention have inherent therapeutic activity on their own account. In some cases, this activity relative to the same target or targets of the parent compound is as good as or better than the activity which the parent compound has against the target or targets.
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Paragraph 0501; 0502
(2013/09/12)
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- DRUG DERIVATIVES
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The present invention relates to derivatives of known active pharmaceutical compounds. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more reactions which may be considered to represent a change of oxidation state. We refer to these compounds generally as redox derivatives. The derivatives of the invention may be related to the original parent active pharmaceutical compound by only a single step transformation, or may be related via several synthetic steps including one or more changes of oxidation state. In certain cases, the functional group obtained after two or more transformations may be in the same oxidation state as the parent active compound (and we include these compounds in our definition of redox derivatives). In other cases, the oxidation state of the derivative of the invention may be regarded as being different from that of the parent compound. In many cases, the compounds of the invention have inherent therapeutic activity on their own account. In some cases, this activity relative to the same target or targets of the parent compound is as good as or better than the activity which the parent compound has against the target or targets.
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Page/Page column 128-129
(2012/05/31)
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- A concise access to a new class of selective anti-inflammatory steroid derivatives
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The 17β-thiomethyl-16α,17α-ketal motif of a new class of selective anti-inflammatory androstane derivatives useful in the treatment of asthma is readily constructed by a new radical degradation of the corticosteroid side chain.
- Quiclet-Sire, Beatrice,Zard, Samir Z.
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p. 1173 - 1174
(2007/10/03)
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- Process for the manufacture of steroid carboxylic acids and the esters thereof
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The present invention provides a novel process for the manufacture of 17- and 17a-carboxylic acids of the androstane and D-homo-androstane series respectively, of the following partial formula of the ring D STR1 wherein R represents a hydrogen atom or an unsubstituted or substituted hydrocarbon radical or a free or functionally modified hydroxyl group, and wherein the carboxyl group can be in the α- or β-position, and of the salts and functional acid derivatives thereof, in particular their esters. The new process consists in the oxidative degradation of the side chain of corrsponding 20, 21-ketoaldehydes of the pregnane or D-homopregnane series or of the 17α-pregnane or 17aα-D-homopregnane series with an organic peracid in an inert solvent, preferably at temperatures between -20 and +30° C, and optionally converting free functional groups present into their derivatives or setting free functional groups from substituents which are derivatives of such groups.
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