Stereoselective estarase from aspergillus oryzae

An esterase isolated from Aspergillus oryzae is capable of stereoselective hydrolysis of chiral esters and also has arylesterase activity (EC 3.1.1.2) and feruloyl esterase activity (EC 3.1.1.73). The esterase has only a limited homology to known amino acid sequences.

N-ADAMANTYL BENZAMIDES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE

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.

N-ADAMANTYL BENZAMIDES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE

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.

Stereoselective esterase from Aspergillus oryzae

An esterase isolated from Aspergillus oryzae is capable of stereoselective hydrolysis of chiral esters and also has arylesterase activity (EC 3.1.1.2) and feruloyl esterase activity (EC 3.1.1.73). The esterase has only a limited homology to known amino acid sequences.

Novel process

The present invention relates to a novel processes for preparing pharmaceutically active fused 1,2,4-thiadiazine derivatives of general formula (I) as defined in the description and intermediates therefore.

N-adamantyl benzamides as inhibitors of 11--hydroxysteroid dehydrogenase

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 11-hydroxysteroid dehydrogenase type 1 (11HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.

Adamantyl Benzamide Derivatives

Embodiments of the present invention provide adamantyl benzamide derivtives and pharmaceutical compositions comprising adamantyl benzamide derivatives. Methods of use of such compounds and compositions to modulate the activity of 11-hydroxysteroid dehydrogenase type 1 (11HSD1) in a subject are also provided.

Use of compounds for decreasing activity of hormone-sensitive

Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.

11BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ACTIVE COMPOUNDS

A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11β-hydroxy-steroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.

Use of compounds for decreasing activity of hormone-sensitive lipase

Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.

Pharmaceutical use of substituted amides

The use of substituted amides for modulating the activity of 11-hydroxysteroid dehydro-genase type 1 (11HSD1) and the use of these compounds as pharmaceutical composi-tions, are described. Also a novel class of substituted amides, their use in therapy, phar-maceutical compositions comprising the compounds, as well as their use in the manufac-ture 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 of a range of medical disorders where a decreased intracellular concentration of active gluco-corticoid is desirable.

N-ADAMANTYL BENZAMIDES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE

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.

Pharmaceutical use of boronic acids and esters thereof

Use of compounds to inhibit hormone-sensitive lipase, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, method of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of a range of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.

Crystalline R-guanidines, arginine or (L)-arginine (2S)-2-ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate

The present invention relates to crystalline R-guanidines of (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate, its preparations and its use as therapeutic agents. More specifically the present invention relates to crystalline Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate, preferably (L)-Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate, its preparation and its use as therapeutic agent.

PHENOXY ACETIC ACIDS AS PPAR DELTA ACTIVATORS

The present invention describes phenoxy-acetic acids and pharmaceutical compositions containing the same and methods of using the same. The phenoxy-acetic acids are activators of PPAR- and should be useful for treating conditions mediated by the same.

Pyridinyl carbamates

Novel substituted pyridinyl carbamates, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to hormone sensitive lipase. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which modulation of the activity of hormone sensitive lipase is beneficial.

11-Beta-Hydroxysteroid Dehydrogenase Type 1 Active Compounds

A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11β-hydroxy-steroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.

PROCESS FOR PREPARING 7H-PYRROLO[2,3-d]PYRIMIDINE DERIVATIVES AND SYNTHETIC INTERMEDIATES THEREOF

The present invention provides processes for preparing 7H-pyrrolo[2,3-d]pyrimidine derivatives, which are useful as a Janus kinase (JAK) inhibitor, intermediates thereof, and processes for preparing the intermediates. The present invention provides processes for preparing 3-[(3S, 4R)-3-methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile using salts of (3S,4R)-1-benzyl-3-methyl-1,6-diazaspiro[3.4]octane with organic acids. 3. The process of claim 2 , further comprising the step of adding an organic acid to the compound of formula [10] to give a salt of the compound of formula [10] with the organic acid.4. The process of claim 2 , wherein the salt with an organic acid is a disuccinate claim 2 , an oxalate or a hemi-oxalate.5. The process of claim 2 , wherein the salt with an organic acid is a hemi-oxalate.7. The process of claim 6 , wherein the reduction is carried out in the presence of an acid and lithium aluminum hydride.13. The process of claim 12 , wherein the base is lithium hexamethyldisilazide.1924.-. (canceled)27. The salt of claim 26 , wherein the salt with an organic acid is a disuccinate claim 26 , an oxalate or a hemi-oxalate.28. The salt of claim 26 , wherein the salt with an organic acid is a hemi-oxalate.3235.-. (canceled)4043.-. (canceled) The present invention relates to process for preparing 7H-pyrrolo[2,3-d]pyrimidine derivatives which are useful as a Janus kinase (JAK) inhibitor, synthetic intermediates thereof, and process for preparing the intermediates.JAK is a member of a cytoplasmic protein tyrosine kinase family, and for example, includes JAK1, JAK2, JAK3, and TYK2.Patent Literature 1 discloses Compound A (Compound [17]: 3-[(3S,4R)-3-methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile) which is useful as a JAK inhibitor.The present invention provides processes for preparing 7H-pyrrolo[2,3-d]pyrimidine derivatives which are useful as a JAK inhibitor, synthetic ...

Compounds and uses thereof for decreasing activity of hormone-sensitive lipase

Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.

N-adamantyl benzamides as inhibitors of 11--hydroxysteroid dehydrogenase

Novel substituted amide 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 11-hydroxysteroid dehydrogenase type 1 (11HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.

PHARMACEUTICAL USE OF SUBSTITUTED AMIDES

The use of substituted amides for modulating the activity of 11-hydroxysteroid dehydro-genase type 1 (11HSD1) and the use of these compounds as pharmaceutical composi-tions, are described. Also a novel class of substituted amides, their use in therapy, phar-maceutical compositions comprising the compounds, as well as their use in the manufac-ture 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 of a range of medical disorders where a decreased intracellular concentration of active gluco-corticoid is desirable.

PHARMACEUTICAL USE OF SUBSTITUTED AMIDES

The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) 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 11βHSD1 and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.

11-beta-hydroxysteroid dehydrogenase type 1 active compounds

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, of the general formula I. 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 11HSDI and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.

Substituted piperidine carbamates

Novel substituted piperidine carbamates, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to hormone sensitive lipase. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which modulation of the activity of hormone sensitive lipase is beneficial.

N-adamantyl benzamides as inhibitors of 11-beta-hydroxysteroid dehydrogenase

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.

Peptides derived from NCAM (FGLs)

The present invention relates to novel compounds comprising at most 13 contiguous amino acid residues derived from the fibronectin type 3,11 module of neural cell adhesion molecule (NCAM), or a variant or fragment thereof, capable of interacting with an FGFR and thereby the compounds are capable of inducing differentiation, modulating proliferation, stimulate regeneration, neuronal plasticity or survival of cells. Further, the present invention relates to the use of the compounds for production of a medicament for treatment of conditions and diseases, in which NCAM or FGFR play a prominent role.

N-ADAMANTYL BENZAMIDES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE

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. 2. The method of claim 1 , wherein the compound is 4-{2-[3-(5-Hydroxy-adamantan-2-ylcarbamoyl)-phenoxy]-ethyl}-piperidine-1-carboxylic acid isopropylamide or a pharmaceutically acceptable salt thereof.3. The method of claim 1 , wherein the compound is 3-(6-Chloro-pyridin-3-ylmethoxy)-N-(5-hydroxy-adamantan-2-yl)-benzamide or a pharmaceutically acceptable salt thereof.4. The method of claim 1 , wherein the compound is N-(5-Hydroxy-adamantan-2-yl)-3-(tetrahydro-pyran-4-ylmethoxy)-benzamide or a pharmaceutically acceptable salt thereof.5. The method of claim 1 , wherein the compound is N-(5-Hydroxy-adamantan-2-yl)-3-[2-(2-oxo-pyrrolidin-1-yl)-ethoxy]-benzamide or a pharmaceutically acceptable salt thereof.6. The method of claim 1 , wherein the compound is 3-(5-Chloro-pyridin-2-yloxy)-N-(5-hydroxy-adamantan-2-yl)-benzamide or a pharmaceutically acceptable salt thereof.7. The method of claim 1 , wherein the compound is 3-(6-Bromo-pyridin-3-yloxy)-N-(5-hydroxy-adamantan-2-yl)-benzamide or a pharmaceutically acceptable salt thereof.8. The method of claim 1 , wherein the compound is N-(5-Hydroxy-adamantan-2-yl)-3-phenethyloxy-benzamide or a pharmaceutically acceptable salt thereof.9. The method of claim 1 , wherein the compound is N-(5-Hydroxy-adamantan-2-yl)-3-[2-(tetrahydro-pyran-4-yl)-ethoxy]-benzamide or a pharmaceutically acceptable salt thereof.10. The method of claim 1 , wherein the compound is 3-Benzyloxy-N-(5-hydroxy-adamantan-2-yl)-benzamide or a pharmaceutically acceptable ...

PHARMACEUTICAL USE OF SUBSTITUTED AMIDES

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.

Pharmaceutical use of boronic acids and esters thereof

Use of compounds to inhibit hormone-sensitive lipase, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, method of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of a range of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.

Polymorphic form of a calcimimetic compound

The present invention relates to the crystalline, polymorphic Form C of the calcimimetic compound {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid, to methods of preparation thereof, to methods of characterization thereof by single crystal X-Ray crystallography (XRC), X-Ray Powder diffractometry, attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, Solid State NMR spectroscopy and Differential Scanning Calorimetry (DSC), and to its use. The invention also relates to the preparation of Form C by crystallization from a saturated solution of {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid in the presence of crystallization seeds of Form C, or alternatively by conversion of an amorphous starting material into the different crystalline polymorphic Form X by crystallization of {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid, followed by a solid solution transformation thereof into the desired polymorphic Form C.

11-hydroxysteroid dehydrogenase type 1 active compounds

A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11-hydroxy-steroid dehydrogenase type 1 (11HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.

Pharmaceutical use of substituted amides

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.

Substituted piperazine carbamates

Novel substituted piperazine carbamates, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to hormone sensitive lipase. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which modulation of the activity of hormone sensitive lipase is beneficial.

PHARMACEUTICAL USE OF SUBSTITUTED AMIDES

The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) 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 11βHSD1 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 COMPOUNDS

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 11-hydroxysteroid dehydrogenase type 1 (11HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.

Compounds and uses thereof for decreasing activity of hormone-sensitive lipase

Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.

11BETA-HSD1 ACTIVE COMPOUNDS

A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11-hydroxysteroid dehydrogenase type 1 (11HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.

4-PIPERIDYLBENZAMIDES AS 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS

A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11β-hydroxy-steroid dehydrogenase type 1 (11 βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g the metabolic syndrome.

Process for the preparation of substituted 3-phenyl-propanoic acid esters and substituted 3-phenyl-propanoic acids

The present invention relates to a process comprising hydrolysis or trans esterification of one of the two enantiomeric forms of a racemic or enantiomerically enriched ester of formula I or IV by a higher rate than the other by an enzyme to give an ester and a acid (III) or two different esters (V) and (VI) with different R groups both with increased enantiomeric purity and a esterification process of a racemic or enantiomerically enriched acid (VII) by an enzyme to give an ester and an acid both with increased enantiomeric purity.

Substituted p-phenyl carbamates

Novel substituted p-phenyl carbamates, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to hormone sensitive lipase. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which modulation of the activity of hormone sensitive lipase is beneficial.

Substitued piperazine carbamates

Novel piperazines, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to hormone sensitive lipase. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which modulation of lipolysis, such as decreased lipolysis is beneficial.

11BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ACTIVE COMPOUNDS

The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, of the general formula I. 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 11βHSDI and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.

PROCESS FOR PREPARING 7H-PYRROLO[2,3-d]PYRIMIDINE DERIVATIVES AND SYNTHETIC INTERMEDIATES THEREOF

The present invention provides processes for preparing 7H-pyrrolo[2,3-d]pyrimidine derivatives, which are useful as a Janus kinase (JAK) inhibitor, intermediates thereof, and processes for preparing the intermediates. The present invention provides processes for preparing 3-[(3S,4R)-3-methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile using salts of (3S,4R)-1-benzyl-3-methyl-1,6-diazaspiro[3.4]octane with organic acids.

Novel polymorphic forms of an antidiabetic agent: process for their preparation and a pharmaceutical composition containing them

This invention relates to novel polymorphic/pseudopolymorphic forms of arginine salt of 3-[4-[2-(phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid, having the formula I shown below. The invention also relates to a pharmaceutical composition comprising the novel polymorphic form or their mixture and a pharmaceutically acceptable carrier. The polymorphic forms of the present invention are more active, as antidiabetic and hypolipidemic agent, than the novel 3-[4-[2-(phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid.

Phenoxy acetic acids as PPAR delta activators

The present invention describes phenoxy-acetic acids and pharmaceutical compositions containing the same and methods of using the same. The phenoxy-acetic acids are activators of PPAR- and should be useful for treating conditions mediated by the same.

N-adamantyl benzamides as inhibitors of 11--hydroxysteroid dehydrogenase

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 11-hydroxysteroid dehydrogenase type 1 (11HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.

Process for the preparation of substituted 3-phenyl-propanoic acid esters and substituted 3-phenyl-propanoic acids

The present invention relates to a process comprising hydrolysis or trans esterification of one of the two enantiomeric forms of a racemic or enantiomerically enriched ester of formula I or IV by a higher rate than the other by an enzyme to give an ester and a acid (III) or two different esters (V) and (VI) with different R groups both with increased enantiomeric purity and a esterification process of a racemic or enantiomerically enriched acid (VII) by an enzyme to give an ester and an acid both with increased enantiomeric purity.

Crystalline R-guanidines, arginine or (L)-arginine (2S)-2-ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate

The present invention relates to crystalline R-guanidines of (2S)-2-Ethoxy-3{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate, its preparations and its use as therapeutic agents. More specifically the present invention relates to crystalline Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate, preferably (L)-Arginine (2S)-2-Ethoxy-3-{4-[2-(10H-phenoxazin-10-yl)ethoxy]phenyl}propanoate, its preparation and its use as therapeutic agent.

Compounds, their preparation and use

Novel compounds of the general formula (I), in which the variables are as defined in claim 1, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR subtype, namely, type 1 diabetes, type 2 diabetes, dyslipidaemia, syndrome X (including the metabolic syndrome, i.e. impaired glucose tolerance, insulin resistance, hyper-triglyceridaemia and/or obesity), cardiovascular diseases (including atherosclerosis) and hypercholesterolaemia.

NEW POLYMORPHIC FORM OF A CALCIMIMETIC COMPOUND

The present invention relates to the crystalline, polymorphic Form C of the calcimimetic compound {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid, to methods of preparation thereof, to methods of characterization thereof by single crystal X-Ray crystallography (XRC), X-Ray Powder diffractometry, attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, Solid State NMR spectroscopy and Differential Scanning Calorimetry (DSC), and to its use. The invention also relates to the preparation of Form C by crystallization from a saturated solution of {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid in the presence of crystallization seeds of Form C, or alternatively by conversion of an amorphous starting material into the different crystalline polymorphic Form X by crystallization of {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid, followed by a solid solution transformation thereof into the desired polymorphic Form C. 1. A crystalline form of {4-[(1R ,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid.2. The crystalline form according to which belongs to the tetragonal space group P422 having unit-cell parameters a=10.2289(16) Å claim 1 , b=10.2289(16) Å and c=41.492(13) Å.3. The crystalline form according to which has an X-ray powder diffraction pattern that exhibits characteristic peaks expressed in 2θ at approximately 8.8 claim 1 , 9.5 claim 1 , 12.3 claim 1 , 16.0 claim 1 , 18.3 claim 1 , 19.1 and/or 20.2 (±0.1 degrees) (underlined primary) claim 1 , respectively.4. The crystalline form according to which has an X-ray powder diffraction pattern substantially as appears from Graph 2a.5. The crystalline form according to which has a differential scanning calorimetry curve comprising an event with an onset at about 240° C. (±2° C.).6. The crystalline form according to which has Solid State NMR spectrum substantially as ...

Phenoxy acetic acids as PPAR delta activators

The present invention describes phenoxy-acetic acids and pharmaceutical compositions containing the same and methods of using the same. The phenoxy-acetic acids are activators of PPAR- and should be useful for treating conditions mediated by the same.

Phenoxy acetic acids as PPAR delta activators

The present invention describes phenoxy-acetic acids and pharmaceutical compositions containing the same and methods of using the same. The phenoxy-acetic acids are activators of PPAR-delta and should be useful for treating conditions mediated by the same.

Adamantyl benzamide derivatives

Embodiments of the present invention provide adamantyl benzamide derivatives and pharmaceutical compositions comprising adamantyl benzamide derivatives. Methods of use of such compounds and compositions to modulate the activity of 11-hydroxysteroid dehydrogenase type 1 (11HSD1) in a subject are also provided.

ADAMANTANE DERIVATIVES FOR THE TREATMENT OF THE METABOLIC SYNDROME

Novel substituted adamantane 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 11-hydroxysteroid dehydrogenase type 1 (11HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.

11-Beta-Hydroxysteroid Dehydrogenase Type 1 Active Compounds

The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, of the general formula I. 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 11βHSDI and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.

Process for the preparation of substituted 3-phenyl-propanoic acid esters and substituted 3-phenyl-propanoic acids

The present invention relates to a process comprising hydrolysis or trans esterification of one of the two enantiomeric forms of a racemic or enantiomerically enriched ester of formula I or IV by a higher rate than the other by an enzyme to give an ester and a acid (III) or two different esters (V) and (VI) with different R groups both with increased enantiomeric purity and a esterification process of a racemic or enantiomerically enriched acid (VII) by an enzyme to give an ester and an acid both with increased enantiomeric purity.

PHENOXY ACETIC ACIDS AS PPAR DELTA ACTIVATORS

The present invention describes phenoxy-acetic acids and pharmaceutical compositions containing the same and methods of using the same. The phenoxy-acetic acids are activators of PPAR- and should be useful for treating conditions mediated by the same.

11-hydroxysteroid dehydrogenase type 1 active compounds

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, of the general formula I. 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 11HSDI and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.

N-ADAMANTYL BENZAMIDES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE

Novel substituted amide 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.

N-ADAMANTYL BENZAMIDES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE

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. 2. The method of claim 1 , wherein the compound is 4-{2-[3-(5-Hydroxy-adamantan-2-ylcarbamoyl)-phenoxy]-ethyl}-piperidine-1-carboxylic acid isopropylamide or a pharmaceutically acceptable salt thereof.3. The method of claim 1 , wherein the compound is 3-(6-Chloro-pyridin-3-ylmethoxy)-N-(5-hydroxy-adamantan-2-yl)-benzamide or a pharmaceutically acceptable salt thereof.4. The method of claim 1 , wherein the compound is N-(5-Hydroxy-adamantan-2-yl)-3-(tetrahydro-pyran-4-ylmethoxy)-benzamide or a pharmaceutically acceptable salt thereof.5. The method of claim 1 , wherein the compound is N-(5-Hydroxy-adamantan-2-yl)-3-[2-(2-oxo-pyrrolidin-1-yl)-ethoxy]-benzamide or a pharmaceutically acceptable salt thereof.6. The method of claim 1 , wherein the compound is 3-(5-Chloro-pyridin-2-yloxy)-N-(5-hydroxy-adamantan-2-yl)-benzamide or a pharmaceutically acceptable salt thereof.7. The method of claim 1 , wherein the compound is 3-(6-Bromo-pyridin-3-yloxy)-N-(5-hydroxy-adamantan-2-yl)-benzamide or a pharmaceutically acceptable salt thereof.8. The method of claim 1 , wherein the compound is N-(5-Hydroxy-adamantan-2-yl)-3-phenethyloxy-benzamide or a pharmaceutically acceptable salt thereof.9. The method of claim 1 , wherein the compound is N-(5-Hydroxy-adamantan-2-yl)-3-[2-(tetrahydro-pyran-4-yl)-ethoxy]-benzamide or a pharmaceutically acceptable salt thereof.10. The method of claim 1 , wherein the compound is 3-Benzyloxy-N-(5-hydroxy-adamantan-2-yl)-benzamide or a pharmaceutically acceptable ...

Substituted p-phenyl carbamates

Novel substituted p-phenyl carbamates, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to hormone sensitive lipase. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which modulation of the activity of hormone sensitive lipase is beneficial.

Phenoxy Acetic Acids as PPAR Delta Activators

The present invention describes phenoxy-acetic acids and pharmaceutical compositions containing the same and methods of using the same. The phenoxy-acetic acids are activators of PPAR-δ and should be useful for treating conditions mediated by the same.

POLYMORPHIC FORM OF A CALCIMIMETIC COMPOUND

The present invention relates to the crystalline, polymorphic Form X of the calcimimetic compound {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid, to methods of preparation thereof, to methods of characterization thereof by single crystal X-Ray crystallography (XRC), X-Ray Powder diffractometry, attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, Solid State NMR spectroscopy and Differential Scanning Calorimetry (DSC), and to its use. The invention also relates to the preparation of Form X by crystallization from a saturated solution of {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid in a C-Calkyl alcohol, or alternatively by precipitation from a neutralized saponification reaction mixture following the alkaline hydrolysis of a C-Calkyl ester of {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid. 1. A crystalline form of {4-[(1R ,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid.2. The crystalline form according to which belongs to the orthorhombic space group P222having unit-cell parameters a=8.7299(17) Å claim 1 , b=14.822(3) Å and c=16.353(3) Å.3. The crystalline form according to which has an X-ray powder diffraction pattern that exhibits characteristic peaks expressed in 2θ at approximately 8.0 claim 1 , 11.3 claim 1 , 11.4 claim 1 , 15.0 claim 1 , 18.2 and/or 21.5 (±0.05 degrees) (underlined primary) claim 1 , respectively.4. The crystalline form according to which has an X-ray powder diffraction pattern substantially as appears from Graph 2b.5. The crystalline form according to which has a differential scanning calorimetry curve comprising an event with an onset at about 255° C. (±2° C.).6. The crystalline form according to which has a differential scanning calorimetry curve substantially as appears from Graph 4b.7. The crystalline form according to which has Solid State NMR spectrum substantially as ...

Enhancement of enzyme reactions

This invention relates to activation of enzymes. More specifically, the invention relates to peroxidase enhancing agents. The invention also relates to methods of oxidizing a substrate with a source of hydrogen peroxide in the presence of a peroxidase enzyme and a peroxidase enhancing agent. More specifically, the invention relates to a method of bleaching of dye in solutions, to a method of inhibiting the transfer of a textile dye from a dyed fabric to another fabric when said fabrics are washed together in a wash liquor, to a method of bleaching of lignin-containing material, in particular bleaching of pulp for paper production, to a method of treatment of waste water from pulp manufacturing, and to a method of enzymatic polymerization and/or modification of lignin or lignin containing material.

Para-subtituted phenyl carbamates as inhibitors of hormone sensitive lipase

Novel para-substituted phenyl carbamates, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to hormone sensitive lipase. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which modulation of the activity of hormone sensitive lipase is beneficial.

Pharmaceutical use of substituted amides

N-ADAMANTIL BENZAMIDS AS 11-BETAHYDROXYESTEROID DEHYDROGENASE INHIBITORS

Adamantane derivatives for the treatment of the metabolic syndrome

Novel substituted adamantane based inhibitors of structure (I), 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 11-hydroxysteroid dehydro-genase type (1) (11HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.

Phenoxy acetic acids as ppar delta activators

The present invention describes phenoxy-acetic acids and pharmaceutical compositions containing the same and methods of using the same. The phenoxy-acetic acids are activators of PPAR-δ and should be useful for treating conditions mediated by the same.

Process for oxidizing a substrate with a peroxidase enzyme or a compound acting as peroxidase in the presence of a source of hydrogen peroxide additive detergent and detergent composition

Pharmaceutical use of substituted amides

The use of substituted amides for modulating the activity of 11.beta.-hydroxysteroid dehydrogenase type 1 (11.beta.HSD1) 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.beta.HSD1 and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.

Pharmaceutical use of substituted amides

Method for producing 7h-pyrrolo[2,3-d]pyrimidine derivative and synthetic intermediate of same

PROCESS FOR PREPARING 7H-PYRROLO[2,3-d]PYRIMIDINE DERIVATIVES AND SYNTHETIC INTERMEDIATES THEREOF

The present invention provides processes for preparing 5 7H-pyrrolo[2,3-d]pyrimidine derivatives, which are useful as a Janus kinase (JAK) inhibitor, intermediates thereof, and processes for preparing the intermediates. The present invention provides processes for preparing 3-[(3S,4R)-3 methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6 10 diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile using salts of (3S,4R)-1-benzyl-3-methyl-1,6-diazaspiro[3.4]octane with organic acids.

Novel compounds

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 11.beta. -hydroxysteroid dehydrogenase type 1 (11.beta.HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.

Adamantyl benzamide compounds

Embodiments of the present invention provide adamantyl benzamide derivtives and pharmaceutical compositions comprising adamantyl benzamide derivatives. Methods of use of such compounds and compositions to modulate the activity of 11.beta.-hydroxysteroid dehydrogenase type 1(11.beta.HSD1) in a subject are also provided.

Novel compounds, their preparation and use

Novel compounds of the general formula (I), in which the variables are as defined in claim 1, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPARδ subtype, namely, type 1 diabetes, type 2 diabetes, dyslipidaemia, syndrome X (including the metabolic syndrome, i.e. impaired glucose tolerance, insulin resistance, hyper-triglyceridaemia and/or obesity), cardiovascular diseases (including atherosclerosis) and hypercholesterolaemia.

Method for producing 7h-pyrrolo[2,3-d]pyrimidine derivative and synthetic intermediate of same.

La presente invención proporciona procesos para preparar derivados de 7Hpirrolo[ 2,3-d]pirimidina, que son útiles como un inhibidor de Janus quinasa (JAK), intermedios de los mismos, y procesos para preparar los intermedios; la presente invención proporciona procesos para preparar 3-[(3S,4R)-3-metil-6-(7H-pirrol o[2,3-d]pirimidin-4-il)-1,6-diazaespiro[3.4]octan-1-il]-3- oxopropanonitrilo usando sales de (3S,4R)-1-bencil-3-metil-1,6-dia zaespiro[3.4]octano con ácidos orgánicos.

Crystalline r- guanidines, arginine or (l) -arginine (2s) -2- ethoxy -3-{4- [2-(10h -phenoxazin -10-yl)ethoxy]phenyl}propanoate

The present invention relates to crystalline R- guanidines of (2S) -2- Ethoxy-3- {4-[2- (10H -phenoxazin -10-yl) ethoxy]phenyl} propanoate, its preparations and its use as therapeutic agents. More specifically the present invention relates to crystalline Arginine (2S) -2- Ethoxy-3- {4-[2- (10H -phenoxazin -10-yl) ethoxy] phenyl} propanoate, preferably (L)- Arginine (2S) -2- Ethoxy-3- {4-[2- (10H -phenoxazin -10-yl) ethoxy] phenyl} propanoate, its preparation and its use as therapeutic agent.

Adamantyl benzamide compounds.

La presente invención se refiere a modalidades que proporcionan derivados de adamantilo benzamida y a composiciones farmacéuticas que comprenden los derivados de adamantilo benzamida. También se proporcionan métodos de uso de tales compuestos y composiciones para modular la actividad de la deshidrogenasa 11ß-hidroxiesteroide del tipo 1 (11ßHSD1) en un paciente.

11beta-HSD1 active compounds

Pharmaceutical use of substituted amides

The use of substituted amides for modulating the activity of 11&bgr;-hydroxysteroid dehydro-genase type 1 (11&bgr;HSD1) and the use of these compounds as pharmaceutical composi-tions, are described. Also a novel class of substituted amides, their use in therapy, phar-maceutical compositions comprising the compounds, as well as their use in the manufac-ture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11&bgr;HSD1 and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active gluco-corticoid is desirable.

Novel peptides derived from ncam (fgls)

The present invention relates to novel compounds comprising at most 13 contiguous amino acid residues derived from the fibronectin type 3,Il module of neural cell adhesion molecule (NCAM), or a variant or fragment thereof, capable of interacting with an FGFR and thereby the compounds are capable of inducing differentiation, modulating proliferation, stimulate regeneration, neuronal plasticity and/or survival of cells. Further, the present invention relates to the use of said compounds for production of a medicament for treatment of conditions and diseases, wherein NCAM and/or FGFR play a prominent role.

Compounds and uses thereof for decreasing activity of hormone-sensitive lipase

PROCESS FOR PREPARING 7H-PYRROLO[2,3-d]PYRIMIDINE DERIVATIVES AND SYNTHETIC INTERMEDIATES THEREOF

The purpose of the present invention is to provide: a method for producing a 7H-pyrrolo[2,3-d]pyrimidine derivative which is useful as a Janus kinase (JAK) inhibitory agent; an intermediate of the same; and a method for producing the intermediate. Provided is a method for producing 3-[(3S,4R)-3-methyl-6-(7H-pyrrolo[2,3-d]pyrimidine-4-yl)-1,6-Diazaspiro[3.4]octane-1-yl]-3-oxopropanenitrile using an organic acid of (3S,4R)-1-benzyl-3-methyl-1,6-Diazaspiro[3.4]octane and a salt thereof.

N-adamantyl benzamides as inhibitors of 11-beta-hydroxysteroid dehydrogenase

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.

Compounds and uses thereof for decreasing activity of hormone-sensitive lipase

Carbamates and related compounds of formula R1 R2NCO-Y or R1 R2NCS-Y wherein R1 and R2 are hydrogen, alkyl, aryl, heteroaryl or may together form a piperidine, piperazine, morpholine or other heterocyclic ring, are inhibitors of hormone sensitive lipase and are useful for the treatment of any disorder where it is desirable to modulate the plasma level of free fatty acids, glycerol, LDL-cholesterol, HDL-cholesterol, insulin and/or glucose; and or modulate intracellular triacylglycerol and cholesterol stores, intracellular level of fatty acids, fatty acid esters such as diacylglycerols, phosphatidic acids, long chain acyl-CoA's as well as citrate or malonyl-CoA; and or increase insulin sensitivity ; and or modulate insulin secretion from pancreatic beta cells. More particularly said disorders are selected from the group consisting of insulin resistance, diabetes type 1, diabetes type 2, metabolic syndrome X, impaired glucose tolerance, hyperclycemia, dislipidemia, obesity, abnormalities of lipoprotein metabolism and any combinations. thereof.

Phenoxy acetic acids as ppar delta activators

The present invention describes phenoxy-acetic acids and pharmaceutical compositions containing the same and methods of using the same. The phenoxy-acetic acids are activators of PPAR-δ and should be useful for treating conditions mediated by the same.

Phenoxy acetic acids as ppar delta activators

The present invention describes phenoxy-acetic acids and pharmaceutical compositions containing the same and methods of using the same. The phenoxy- acetic acids are activators of PPAR-.delta. and should be useful for treatin g conditions mediated by the same.

Process for the preparation of substituted 3-phenyl-propanoic acid esters and substituted 3-phenyl-propanoic acids

The present invention relates to a process comprising hydrolysis or trans-esterification of one of the two enantiomeric forms of a racemic or enantiomerically enriched ester of formula (I) or (IV) by a higher rate than the other by an enzyme to give an ester and an acid (III) or two different esters (V) and (VI) with different R groups both with increased enantiomeric purity and an esterification process of a racemic or enantiomerically enriched acid (VII) by an enzyme to give an ester and an acid both with increased enantiomeric purity.

Pharmaceutical use of substituted amides

New polymorphic form of a calcimimetic compound

The present invention relates to the crystalline, polymorphic Form X of the calcimimetic compound {4-[(1 R , 3 S )-3-(( R )-1 -Naphthalen-1 -yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid, to methods of preparation thereof, to methods of characterization thereof by single crystal X-Ray crystallography (XRC), X-Ray Powder diffractometry, attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, Solid State NMR spectroscopy and Differential Scanning Calorimetry (DSC), and to its use. The invention also relates to the preparation of Form X by crystallization from a saturated solution of {4-[(1 R ,3 S )-3-(( R )-1 -Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid in a C 1 -C 6 alkyl alcohol, or alternatively by precipitation from a neutralized saponification reaction mixture following the alkaline hydrolysis of a C 1 -C 6 alkyl ester of {4-[(1 R ,3 S )-3-(( R )-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid.

11beta-hsd1 active compounds

A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11.beta. -hydroxysteroid dehydrogenase type 1 (11.beta.HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.

NEW COMPOUNDS, THEIR PREPARATION AND USE.

Un compuesto de fórmula general (I): **(Ver fórmula)**en la que X1 es arilo o heteroarilo, cada uno de los cuales está opcionalmente sustituido con uno o más sustituyentes seleccionados entre - halógeno, hidroxi, ciano, amino o carboxi; o - alquilo C1-6, cicloalquilo C3-6, alquenilo C2-6, alquinilo C2-6, aralquilo, heteroaralquilo, alcoxi C1-6, cicloalcoxi C3-6, ariloxi, aralcoxi, heteroaralcoxi, alquiltio C1-6, ariltio, 10 cicloalquiltio C3-6, alquilcarbonilo C1-6, arilcarbonilo, alquilsulfonilo C1-6, alquilsulfoniloxi C1-6, arilsulfonilo, arilsulfoniloxi, alquilamido C1-6, arilamido, alquilaminocarbonilo C1-6, alquilamino C1-6, dialquilamino C1-6 o cicloalquilamino C3-6, cada uno de los cuales está opcionalmente sustituido con uno o más de halógeno o hidroxi; y X2 es arilo o heteroarilo, cada uno de los cuales está opcionalmente sustituido con uno o más 15 sustituyentes seleccionados entre - halógeno, hidroxi, ciano, amino o carboxi; o - alquilo C1-6, cicloalquilo C3-6, alquenilo C2-6, alquinilo C2-6, aralquilo, heteroaralquilo, alcoxi C1-6, cicloalcoxi C3-6, ariloxi, aralcoxi, heteroaralcoxi, alquiltio C1-6, ariltio, cicloalquiltio C3-6, alquilcarbonilo C1-6, arilcarbonilo, alquilsulfonilo C1-6, alquilsulfoniloxi 20 C1-6, arilsulfonilo, arilsulfoniloxi, alquilamido C1-6, arilamido, alquilaminocarbonilo C1-6, alquilamino C1-6, dialquilamino C1-6 o cicloalquilamino C3-6, cada uno de los cuales está opcionalmente sustituido con uno o más de halógeno o hidroxi; y Ar1 es arileno o heteroarileno; y Ar2 es arileno que está opcionalmente sustituido con uno o más sustituyentes seleccionados 25 entre - halógeno, hidroxi o ciano; o - alquilo C1-6, cicloalquilo C3-6, alquenilo C2-6, alquinilo C2-6, arilo, heteroarilo, aralquilo, heteroaralquilo, alcoxi C1-6, cicloalcoxi C3-6, ariloxi, aralcoxi, heteroaralcoxi, alquiltio C1-6, ariltio o cicloalquiltio C4-6, cada uno de los cuales está opcionalmente sustituido con uno 30 o más halógenos; o - dos de los sustituyentes, cuando ...

Neue verbindungen, ihre herstellung und verwendung

4-piperidylbenzamides as 11-beta-hydroxysteroid dehydrogenase type 1 inhibitors

A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11β-hydroxy-steroid dehydrogenase type 1 (11 βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g the metabolic syndrome.

Novel process

The present invention relates to novel processes for preparing pharmaceutically active fused 1,2,4-thiadiazine derivatives of general formula (I) as defined in the description and intermediates therefore.

Phenoxyessigsäuren als ppar-delta-aktivatoren

PROCESS FOR PREPARING 7H-PYRROLO[2,3-d]PYRIMIDINE DERIVATIVES AND SYNTHETIC INTERMEDIATES THEREOF

The present invention provides processes for preparing 5 7H-pyrrolo[2,3-d]pyrimidine derivatives, which are useful as a Janus kinase (JAK) inhibitor, intermediates thereof, and processes for preparing the intermediates. The present invention provides processes for preparing 3-[(3S,4R)-3 methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6 10 diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile using salts of (3S,4R)-1-benzyl-3-methyl-1,6-diazaspiro[3.4]octane with organic acids.

Beschleunigung von enzymreaktionen

Stereoselective esterase from aspergillus oryzae

Stereoselektive esterase aus aspergillus oryzae

Stereoselektive esterase aus aspergillus oryzae

Stereoselektive esterase aus aspergillus oryzae

Proceso para la preparacion de derivados de 7h-pirrolo[2,3-d]pirim idina y sus intermedios sinteticos.

La presente invención proporciona procesos para preparar derivados de 7H-pirrolo[2,3-d]pirimidina, que son útiles como un inhibidor de Janus quinasa (JAK), intermedios de los mismos, y procesos para preparar los intermedios; la presente invención proporciona procesos para preparar 3-[(3S,4R)-3-metil-6-(7H-pirrol o[2,3-d]pirimidin-4-il)-1,6-diazaespiro[3.4]octan-1-il]-3- oxopropanonitrilo usando sales de (3S,4R)-1-bencil-3-metil-1,6-dia zaespiro[3.4]octano con ácidos orgánicos.