55 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).

Trisubstituted heteroaromatic compounds having the structure are provided, wherein X is C or N; A and B are each independently CH or N, with the proviso that A and B cannot both be CH; R1 is Ar-L-; R2 is hydrogen or alkyl; or R1 and R2 can be joined together to form a 4- to 7-membered cycloheteroalkyl ring; R3 to R8, Ar and L are as defined herein. A method for using these compounds to treat diseases associated with abnormal bone or mineral homeostasis is also provided.

The present invention relates to methods for treating or preventing podocyte-related diseases and disorders using compounds that modulate the calcium sensing receptor or pharmaceutical compositions comprising thereof.

A compound represented by the following formula (1), a pharmaceutically acceptable salt thereof or an optically active form thereof: wherein each symbol is as defined in the specification. A compound having a calcium-sensing receptor antagonistic action, a pharmaceutical composition comprising the compound, particularly a calcium receptor antagonist and a therapeutic drug for osteoporosis are provided.

[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 formulawhereinm is 0, 1, 2, 3 or 4;each X is independently selected from the group consisting of hydrogen, halo, cyano, nitro, OCF3, hydroxy, amino, carboxyl, alkyl, alkenyl, alkynyl, cycloalkyl, cycloheteroalkyl, haloalkyl, alkoxy, alkoxycarbonylalkyl, hydroxycarbonylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkylalkyl, R1O, R1R2N, R1OCO, R1CO, R1R2NCO, R1R2NCONR2a, R1OCONR2a, R1CONR2a, R1S, R1SO, R1SO2, R1R2NSO2, R1R2NSO2NR2a, and R1SO2NR2a;R1 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloheteroalkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl;R2 and R2a are the same or different and are independently selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloheteroalkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl;n is 1, 2, or 3;W is O or H,R3;R3 is hydrogen or hydroxyl;Ar is a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaryl group;Q is hydrogen, F, or hydroxyl.In addition, a method for using these compounds to treat diseases associated with abnormal or mineral homeostasis is also provided.

A compound represented by the following formula (1), a pharmaceutically acceptable salt thereof or an optically active form thereof:wherein each symbol is as defined in the specification. A compound having a calcium-sensing receptor antagonistic action, a pharmaceutical composition comprising the compound, particularly a calcium receptor antagonist and a therapeutic drug for osteoporosis are provided.

The present invention relates to modulators of the calcium sensing receptor having the formula IwhereinAr1, X, J, R1, R2, R3, R7, R8 and Q are as defined herein.

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 methods of raising crustaceans, comprising maintaining crustaceans in low salinity water having a Calcium-sensing Receptor (CaSR) modulator(s), and adding feed that contains an agent that contributes to modulation of a crustacean CaSR to the water.

The invention discloses a skin external-use patch containing a calcium-sensing receptor stimulant. For the patch disclosed by the invention, a medicinal storage layer, a backing layer and a protection layer are adopted as the necessary ingredients of the patch, and meanwhile, other pharmaceutically acceptable excipients also can be added. The patch is administrated through the skin, so that the first-pass effect of the liver and the stimulation to the gastrointestinal tract are avoided, the untoward effects of the medicines are effectively reduced, the medication to patients is safe, meanwhile, compared with the tablets for oral administration, the patch provided by the invention has the permanent efficacies, and the bioavailability is obviously improved.

The present invention relates to methods of maintaining, and methods of restoring, a desired calcium homeostasis in a non-human terrestrial animal by administering an effective amount of one or more Calcium-Sensing Receptor modulators (CaSRs) to the animal. The invention further provides methods of reducing foot lesions in chickens. The invention also relates to food compositions useful in the methods of the invention.

The present invention relates to modulators of the calcium sensing receptor having the formula IwhereinAr1, X, n, R1, R2, R3 and Q are as defined herein.

The present invention provides calcium sensing receptor modulators (CaSR). In particular, the compounds described herein are useful for treating, managing, and / or lessening the severity of diseases, disorders, syndromes and / or conditions associated with the modulation of calcium sensing receptors (CaSR). The invention also provides herein the pharmaceutical compositions thereof, and methods for treating, managing, and / or lessening the severity of diseases, disorders, syndromes and / or conditions associated with the modulation of CaSR. The invention also relates to process for the preparation of the compounds of the invention.

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).