211 results about "Hydroxysteroid Dehydrogenases" patented technology

The invention relates to a composition for topical application or oral administration, containing an effective quantity of at least one inhibitor of the enzyme 3beta-hydroxysteroid dehydrogenase. This composition is designed in particular for the treatment of certain effects of chronological ageing and photo-ageing of the skin.

Combination therapy comprising the administration of an 11β-hydroxysteroid dehydrogenase type 1 inhibitor and an antihypertensive agent useful for treating, preventing and reducing the risk of developing insulin resistance, dyslipidemia, obesity, hypertension and other related diseases and disorders.

The invention relates to the use of non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment and prophylaxis of hormone-dependent, particularly estrogen-dependent, diseases. The invention further relates to suitable inhibitors and to a method for the production thereof.

This invention relates to novel compounds of the Formula Il Ik, Im³, Im⁴, Im^6-12, In³, In⁴, In^6-12, lo³, lo⁴, lo^6-12, Ip², Ip^4-7, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.

The invention relates to novel compounds of the Formula Ik, Im¹, Im², Im⁵, In¹, In², In⁵, Io₁, Io², Io⁵, Ip¹, Ip³, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.

This invention relates to novel compounds of the Formula (I), (I*), (I**), I, Ia, Ib, Ic, Id, Ie, If, Ig, Il^1-3, Im^1-3, In^1-3, or Io^1-2, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.

This invention relates to novel compounds of the Formula I, Ik, Iq^1-21, Ir^1-21, Is^1-21, It^1-7, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.

This invention relates to novel compounds of the Formula I, II, III, IHa, NIb, IV, IVa, IVb, IVc, IVd, IVe, V, Va, Vb1 V1, V1a, VIb, VII, Vi1a, VIIb, VIII, V111a, VIIIb, IX, IXa, X, and Xa, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.

This invention relates to novel compounds of the Formula (I), (I*), (Ia), (Ib), (Ic), (Id), (Ie), (If), (If*), (Ig), (Ih), (Ij), (Ik), (ll1-3), (Im1-3), (In1-3), (lo1-2), (Ip1-9), (Iq1-9), (Ir1-9) and (Is1-3) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.

The use of substituted amides for modulating the activity of 11-hydroxysteroid dehydrogenase type 1 (11HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.

The use of substituted amides of structure (I) for modulating the activity of 11 β-hydroxysteroid dehydrogenase type 1 (11 βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11 βHSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.

Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.

A compound having Formula I

R₁-Z-R₂  Formula I

wherein R₁ is an optionally substituted phenyl ring; R₂ is or comprises an optionally substituted-aromatic ring; and Z is -X-Y-L- or -Y-X-L- wherein either X is selected from —S(═O)(═O)— and —C(═O)—, and Y is —NR₃—; or X is selected from —S(═O)(═O)— and —S—, and Y is —C(R₄)(R₅)—; L is an optional linker; and R₃, R₄ and R₅ are each independently selected from H and hydrocarbyl; and wherein when R₂ comprises the following structural moiety

wherein Q is an atom selected from the group consisting of S, O, N and C; the compound is selected from compounds of the formulae R₁C(═O)—NR₃-L-R₂; R₁—S(═O)(═O)—C(R₄)(R₅)-L-R₂; R₁—S—C(R₄)(R₅)-L-R₂; R₁—NR₃—S(═O)(═O)-L-R₂; R₁—NR₃—C(═O)-L-R₂; R₁—C(R₄)(R₅)—S(═O)(═O)-L-R₂; and R₁—C(R₄)(R₅)—S-L-R₂.

This invention relates to substituted 1,3-oxazin-2-one compounds of the Formula (I), (II), (IIA), (IIB), (IIC), (II D), (IIE), (III), (III A), (III B), (IV), (IV A), (IV B), (IV C), (IV D), (V), (V A), (V B), (VI), (VI A), (VI B), (VII), (VII A), (VII B), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.

The invention relates to hydroxysteroid dehydrogenase and particularly relates to a clostridium sardiniense 7alpha-hydroxysteroid dehydrogenase mutant T145S. The amino acid sequence of the clostridium sardiniense 7alpha-hydroxysteroid dehydrogenase mutant T145S is shown by SEQ ID No:2 and obtained by changing the 145th-site amino acid of the 7alpha-hydroxysteroid dehydrogenase with an amino acid sequence of SEQ ID No:1 from Thr into Ser. The mutant is 4.85 times of a wild type in the catalysis efficiency against the substrates TCDCA and NADP<+> and has a huge application potential in a biotransformation process of CDCA/TCDCA for obtaining UDCA/TUDCA.

The invention relates to a method for preparing an ursodesoxycholic acid by using a biological enzyme catalysis technology and 7beta-hydroxysteroid dehydrogenase for preparation of the ursodesoxycholic acid. The method comprises the following steps: adopting a 3alpha-hydroxyl -7-oxo-5beta-cholanic acid as a substrate and catalyzing the 3alpha-hydroxyl -7-oxo-5beta-cholanic acid by using the 7beta-hydroxysteroid dehydrogenase to prepare the ursodesoxycholic acid in the presence of an NADP, glucose, glucose dehydrogenase and a buffer solution, wherein the 7beta-hydroxysteroid dehydrogenase is from Turneriella parva. The method is simple in operation, short in reaction time, the reaction conditions are mild and easy to control, the conversion rate of the substrate can reach 99.8% and the content of the obtained product is greater than 98.5%.

Compounds having Formula I, including pharmaceutically acceptable salts, hydrates and solvates thereof:

are selective inhibitors of the 11β-HSD1 enzyme. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dylsipidernia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM.

The invention relates to novel 7β-hydroxysteroid dehydrogenase mutants, to the sequences which encode these enzyme mutants, to processes for the preparation of the enzyme mutants and to their use in enzymatic reactions of cholic acid compounds, in particular in the preparation of ursodeoxycholic acid (UDCS). The invention also relates to novel processes for the synthesis of UDCS using the enzyme mutants; and to the preparation of UDCS using recombinant, multiply-modified microorganisms.