Abstract: The invention relates to novel calcium-sensing receptor (CaSR) modulating trifluoromethylphenylene cyclopentylene compounds represented in formula (I) and derivatives thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.

Abstract: Calcium-sensing receptor (CaSR) modulating substituted cyclopentylene compounds represented in formula I (wherein X is CH or N) and pharmaceutical compositions thereof are useful for treating diseases.

Abstract: The present invention relates to intermediates useful for the synthesis of calcipotriol or calcipotriol monohydrate, to methods of producing said intermediates, and to methods of stereoselectively reducing said intermediates.

Abstract: A pharmaceutical composition comprises, as a therapeutically active ingredient, a corticosteroid and/or vitamin D derivative incorporated as a solid solution or dispersion in lipid nanoparticles, said lipid nanoparticles being solid at ambient temperature and comprising a first lipid with a melting point above body temperature, the first lipid being a wax selected from the group consisting of esters of C12-24 alcohols and C12-24 fatty acids, glyceryl mono-, di- or triesters of C12-24 fatty acids, C12-24 fatty alcohols, and cholesterol, optionally a second lipid which is an oil at ambient temperature and miscible with the first lipid, and a pharmaceutically acceptable surfactant.

Abstract: A cyclic peptide capable of binding specifically to the ?2 I domain of a collagen binding integrin receptor may be conjugated to a drug containing particle via a linker moiety. The conjugate may be used to target a therapeutic drug to a cell expressing a collagen binding integrin receptor on its surface.

Abstract: The invention relates to compounds of general Formula (I), Wherein R1, R2, R3, R4, R5, m, n are defined herein, and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disesase, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immunosuppression would be desirable for example in organ transplantation.

Abstract: Compounds of general formula I, (formula [I)], their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.

Abstract: Compounds of general formula (I), their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.

Abstract: Compounds of general formula (I) their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.

Abstract: Compounds of general formula (I), their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.

Abstract: The present invention relates to a compound according to formula: (1); wherein X1, X2, X3, X4 and X5 independently of each other represent —CH— or N; or X3, X4 and X5 independently of each other represent —CH— or N, and X1 and X2 independently of each other represent C and form part of an additional 6-membered aromatic ring; R1 represents hydrogen, alkyl, alkenyl, alkynyl, haloalkyl, hydroxyalkyl, or alkylcarbonyl, all of which are optionally substituted; R2 and R3 independently represent hydrogen, —CH2, —C(O)NR—R?, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, haloalkyl, hydroxyalkyl, heterocycloalkenyl, alkylaryl, alkylalkoxycarbonyl, aikylcarbonyloxy, or alkoxyalkyl, all of which are optionally substituted; R11 represents hydrogen, halogen, cyano, amino, alkoxy or alkylamino, X1-X5 represent —CH— or N, including N-oxides, enantiomers and diastereomers; and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention relates further to methods of treating dermal disease.

Abstract: The invention relates to compounds of general formula (I) wherein R1, R2, R3, R4, m and n are defined as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immuno-suppression would be desirable for example in organ transplantation.

Abstract: 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 C1-C6 alkyl alcohol, or alternatively by precipitation from a neutralized saponification reaction mixture following the alkaline hydrolysis of a C1-C6 alkyl ester of {4-[(1R,3S)-3-((R)-1-Naphthalen-1-yl-ethylamino)-cyclopentyl]-phenoxy}-acetic acid.

Abstract: Compounds according to formula I in which formula R1 and R2, which may be the same or different, represent halogen, (C1-C6)hydrocarbyl, optionally substituted with one or two hydroxyl group or one or more fluorine atoms, or, together with the carbon atom to which they are both attached, R1 and R2 form a (C3-C6)carbocyclic ring, or one of R1 and R2 taken together with R3 forms a direct bond, such that a triple bond is constituted, or R1 and R2 represent both hydrogen; R3 when not forming a direct bond with one of R1 and R2 represents hydrogen or (C1-C3)hydrocarbyl; X represents (E)-ethylene, (Z)-ethylene, ethynylene, or a bond; Y and Z independently represent hydrogen or methyl; and prodrugs and stereo isomeric forms thereof are provided together with their use in therapy, and their use in the manufacture of medicaments.

Abstract: 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.

Abstract: Compounds of the general formula (I) wherein each of m and n is independently 0 or 1; R1 and R2, together with the carbon atom to which they are attached, form a heterocyclic ring comprising one or two heteroatoms selected from oxygen, sulfur, —S(O)— and —S(0)2-; R3 is —CHF2, —CF3, —OCHF2, —OCF3, —SCHF2 or —SCF3; X is a bond, —CH2—, or —NH—; A is aryl, cycloalkyl, cycloalkenyl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkenyl, optionally substituted with one or more, same or different substituents selected from R4; and R4 is hydrogen, amino, thioxo, alkyl, haloalkyl, hydroxyalkyl, alkoxy, haloalkoxy, halogen, oxo, thia, or hydroxy; or pharmaceutically acceptable salts, hydrates or solvates thereof, have been found to exhibit PDE4 inhibiting activity, and may therefore be useful in the treatment of inflammatory diseases and disorders.

Abstract: The present invention relates to a topical spray composition comprising a biologically active vitamin D derivative and a corticosteroid, and its use in the treatment of dermal diseases and conditions. The spray comprises especially a propellant selected from the group consisting of dimethyl ether, diethyl ether and methylethyl ether or a mixture thereof and further a pharmaceutically acceptable lipid carrier solubilised or suspended in said propellant.

Abstract: Novel biaryl compounds with phosphodiesterase inhibitory activity of the general formula (I), wherein R1, R2, R3, X, Y, Z1, Z2, Z3, and Z4 have the meanings defined herein, as well as their use as therapeutic agents in the treatment of inflammatory diseases and conditions.

Abstract: Calcipotriol monohydrate nanocrystals prepared by the process disclosed herein may be incorporated in a pharmaceutical composition for use in the prevention or treatment of dermal diseases and conditions.