53 results about "Calcium-sensing receptor" patented technology

[Problem] To provide a compound which may be used in treating diseases in which a calcium sensing receptor (CaSR) is concerned, particularly hyperparathyroidism.

[Means for Resolution] It was found that novel pyrrolidine derivatives which are characterized by the possession of aminomethyl group substituted with arylalkyl group or the like, or salts thereof, have excellent CaSR agonistic regulatory activity and also have excellent selectivity with CYP2D6 inhibitory activity having a possibility of causing drug interaction. Based on the above, these novel pyrrolidine derivatives are useful as therapeutic agents for treating diseases in which CaSR is concerned (hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like).

[Problem] To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism.

[Means for Resolution] It was found that a novel piperidine derivative which is characterized in that one of a 3-position and a 4-position is substituted with an aminomethyl group substituted with an arylalkyl group or the like and the other position is substituted with aryl, heteroaryl or the like, or a salt thereof, has an excellent CaSR agonistic regulatory action, and also has excellent selectivity with a CYP2D6 inhibitory action having a possibility of causing drug interaction. Based on the above, this novel piperidine derivative is useful as a therapeutic agent for diseases in which CaSR participates (hyperparathyroidism, renal osteodystrophy, hypercalcemia, and the like).

Compounds are provided which are antagonists of the calcium sensing receptor, and have the general formula

In addition, a method for using these compounds to treat diseases associated with abnormal or mineral homeostasis is also provided.

The present invention relates to modulators of the calcium sensing receptor having the formula I

A compound 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, methods of treating diseases with said compounds, and the use of said compounds in the manufacture of medicaments.

The invention relates to novel calcium-sensing receptor (CaSR) modulating substituted 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.

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.

The present invention relates to modulators of the calcium sensing receptor having the formula I

wherein

• • Ar¹, X, n, R¹, R², R³ and Q are as defined herein.

The invention relates to a high-throughput screening method for a porcine calcium-sensing receptor (CAR) agonist and belongs to the field of the application of agriculture, animal husbandry and veterinarians. The high-throughput screening method comprises the following steps of: extracting total ribonucleic acid (RNA) from a porcine liver, connecting a pgCAR gene fragment obtained through reverse transcription-polymerase chain reaction (RT-PCR) and an eukaryotic expression plasmid, connecting a (NR1)5-TK promoter whole-gene fragment and a reporter plasmid, cotransfecting mammalian cells by using a recombinant expression plasmid, a recombinant reporter plasmid and an internal reference reporter plasmid so as to form stable cell strains, adding medicines to be screened into the stable cell strains, determining the expression level of a reporter gene, evaluating the bioactivities of the medicines, and selecting the medicine with high bioactivity to obtain the pgCAR agonist. A cell screening model established by the method is easy to operate, has good specificity and sensitivity, and can efficiently, quickly and accurately find agonists of porcine CARs.

Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors of Formula (I).

Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors of Formula (I).