41 results about "Oxytocin receptor" patented technology

This invention provides novel substituted tricyclic pyridyl carboxamides which act as oxytocin receptor competitive antagonists, as well as methods of their manufacture, pharmaceutical compositions and methods of their use in treatment, inhibition, suppression or prevention of preterm labor, dysmenorrhea, endometritis, suppression of labor at term prior to caesarean delivery, and to facilitate antinatal transport to a medical facility. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and may be useful in the prevention and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.

The present invention relates to the use of an oxytocin receptor antagonist in females undergoing embryo transfer as part of an assisted reproductive technology. In particular, methods are provided for increasing ongoing implantation rate, increasing ongoing pregnancy rate, increasing clinical pregnancy rate, and / or increasing live birth rate in a female subject undergoing embryo transfer. Specifically, the antagonists are released in the luteal phase when the endometrium is receptive for embryo implantation and / or when the embryo has reached the blastocyst-stage.

The present invention relates to a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methy19243-yloxime, and / or an active metabolite thereof having antagonist action at the oxytocin receptor and / or vasopressin V1a receptor, to processes for their preparation, pharmaceutical compositions containing them and their use.

The present invention relates to the use of an oxytocin receptor antagonist in females undergoing embryo transfer as part of an assisted reproductive technology. In particular, methods are provided for increasing ongoing implantation rate, increasing ongoing pregnancy rate, increasing clinical pregnancy rate, and / or increasing live birth rate in a female subject undergoing embryo transfer. Specifically, the antagonists are released in the luteal phase when the endometrium is receptive for embryo implantation and / or when the embryo has reached the blastocyst-stage.

The present invention is related to pyrrolidine derivatives of formula (I). Saidcompounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula (I) are useful in the treatment and / or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and / or prevention of disease states mediated by oxytocin, including premature labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation, wherein X is selected from the group consisting of CR6R7, NOR6, NNR6R7; A is selected from the group consisting of —(C═O)—, —(C═O)—O—, —C(═NH)—, —(C═O)—NH—, —(C═S)—NH, —SO22-, —SO2NH—, —CH2-, B is either a group —(C═O)—NR8R9 or represents a heterocyclic residue having the formula (a) wherein Q is NR10, O or S; n is an integer selected of 0, 1 or 2; Y, Z and E form together with the 2 carbons to which they are attached a 5–6 membered aryl or heteroaryl ring.

The present invention is related to pyrrolidine oxadiazole and thiadiazole derivatives for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such pyrrolidine oxadiazole derivatives. Said pyrrolidine derivatives are useful in the treatment and / or prevention of preterm labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and / or prevention of disease states mediated by oxytocin, including preterm labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation. (I) B is a oxadiazole or thiadiazole group

The present invention relates to a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methl9243yloxime, and / or an active metabolite thereof having antagonist action at the oxytocin receptor and / or vasopressin V1a receptor, to processes for their preparation, pharmaceutical compositions containing them and their use.

The present invention is related to the use of pyrrolidine esters of formula (I) for the treatment and / or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to the use of pyrrolidine esters of formula (I) to modulate, notably to antagonize the oxytocin receptor. The present invention is furthermore related to novel pyrrolidine esters. X is selected from the group consisting of CR6R7, NOR6, NNR6R7; R is selected from the group comprising or consisting of C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, saturated or unsaturated 3–8-membered cycloalkyl which may contain 1 to 3 heteroatoms selected of N, O, S, aryl, heteroaryl, C1–C6-alkyl aryl, C1–C6-alkyl heteroaryl. R1 is selected from the group comprising or consisting of C1–C6-alkyl, C2–C6-alkenyl, C2–C6-alkynyl, aryl, heteroaryl, 3–8-membered cycloalkyl, acyl, C1–C6-alkyl aryl, C1–C6-alkyl heteroaryl, said cycloalkyl or aryl or heteroaryl groups may be fused with 1–2 further cycloalkyl or aryl or heteroaryl group

The present invention is related to the use of pyrrolidine esters of formula (I) for the treatment and / or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to the use of pyrrolidine esters of formula (I) to modulate, notably to antagonise the oxytocin receptor. The present invention is furthermore related to novel pyrrolidine esters. X is selected from the group consisting of CR6R7, NOR6, NNR6R7; R is selected from the group comprising or consisting of C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, saturated or unsaturated 3-8-membered cycloalkyl which may contain 1 to 3 heteroatoms selected of N, O, S, aryl, heteroaryl, C1-C6-alkyl aryl, C1-C6-alkyl heteroaryl. R1 is selected from the group comprising or consisting of C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, heteroaryl, 3-8-membered cycloalkyl, acyl, C1-C6-alkyl aryl, C1-C6-alkyl heteroaryl, said cycloalkyl or aryl or heteroaryl groups may be fused with 1-2 further cycloalkyl or aryl or heteroaryl group.

The invention relates to compounds of formulawherein variables are defined herein.It has been found that the present compounds are oxytocin receptor agonists for the treatment of autism, stress, including post traumatic stress disorder, anxiety, including anxiety disorders and depression, schizophrenia, psychiatric disorders and memory loss, alcohol withdrawal, drug addiction and for the treatment of Prader-Willi Syndrom.

The present compounds are oxytocin receptor agonists for the treatment of autism, stress, including post-traumatic stress disorder, anxiety, including anxiety disorders and depression, schizophrenia, psychiatric disorders and memory loss, alcohol withdrawal, drug addiction and for the treatment of Prader-Willi Syndrome.

The present invention relates to a compound which is an agonist of the oxytocin receptor o for use in the treatment of a feeding disorder with early-onset. In a particular embodiment, the agonist of the oxytocin receptor is the oxytocin or an active fragment thereof.

The present compounds compounds are oxytocin receptor agonists for the treatment of autism, stress, including post traumatic stress disorder, anxiety, including anxiety disorders and depression, schizophrenia, psychiatric disorders and memory loss, alcohol withdrawal, drug addiction and for the treatment of Prader-Willi Syndrome.

The present invention relates to a compound which is an agonist of the oxytocin receptor o for use in the treatment of a feeding disorder with early-onset. In a particular embodiment, the agonist of the oxytocin receptor is the oxytocin or an active fragment thereof.

The present invention provides methods for the therapy and prevention of problem drinking in alcohol-dependent and non-dependent subjects and those at risk of developing problem drinking behavior, and compositions of matter comprising oxytocin or an analog or derivative thereof or an agonist or partial agonist of an oxytocin receptor that are useful in preventing or treating problem drinking.

Methods and compositions are provided for treating and preventing preterm labor using liposome encapsulated tocolytic agents, such as indomethacin. In certain aspects, targeted liposomes are provided that allow delivery of tocolytic agents directly to the uterus, such as by targeting to the oxytocin receptor.

The invention relates to the technical field of biology, in particular to application of a gene and a construction method of an animal model. The invention discloses an Oxtr gene which can be used asa target gene for treating breast cancer; oxytocin receptor (OXTR) overexpression provides a transgenic mouse breast cancer induction model, and the model can be used for the study of the pathogenesismechanism of breast cancer and also can be used for drug screening and drug function test.

The present invention is related to pyrrolidine derivatives of formula I. Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula I are useful in the treatment and / or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and / or prevention of disease states mediated by oxytocin, including premature labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation.wherein X is selected from the group consisting of CR6R7, NOR6, NNR6R7;A is selected from the group consisting of —(C═O)—, —(C═O)—O—, —C(═NH)—, —(C═O)—NH—, —(C═S)—NH, —SO2—, —SO2NH—, —CH2—,B is either a group —C═O)—NR8R9 or represents a heterocyclic residue having the formula wherein Q is NR10, O or S; n is an integer selected of 0, 1 or 2;Y, Z and E form together with the 2 carbons to which they are attached a 5-6 membered aryl or heteroaryl ring.

The invention discloses a method for constructing a female AD model by utilizing an oxytocin receptor gene silencing technology and an identification method. Constructing and screening are carried outto obtain an AAV9-Oxtr-RNAi vector, AAV9-Oxtr-RNAi viruses are injected into a rat basal nucleus region by utilizing brain stereotaxis, according to a brain infection pathological state, detection and evaluation are carried out in combination with senile dementia symptoms caused by estrogen decline of clinical women, rats are randomly divided into a sham group, a con-shRNA control group and an OXTR-shRNA group, and the learning and memory abilities of the rats are detected by adopting a behavioral Morris water maze experiment and a bright and dark box experiment; an Elisa kit is used for detecting the change of the level of the rat brain tissue cortical estrogen (Estrogen, E2) and the change of the level of a acetylcholine neurotransmitter (acetylcholine, Ach); and in combination with animmunofluorescence technology, the co-localization and expression conditions of incoming nerve fibers of hippocampus in a brain basal nuclear cholinergic neuron fiber projection region, OTR and ChAT are observed, and a basis can be provided for better exploring and researching the pathogenesis and pathological changes of female Alzheimer disease.

Disclosed are oxytocin compositions having a therapeutically effective amount of oxytocin, an analog or derivative of oxytocin, or an oxytocin receptor agonist for the treatment of neonatal abstinence syndrome (“NAS”) in a subject. Also disclosed are methods for the treatment of NAS by administering a therapeutically effective amount of oxytocin, an analog or derivative of oxytocin, or an oxytocin receptor agonist to a subject.

The invention discloses a construction method of human astrocytes stably expressing OXTR (oxytocin receptors). The construction method comprises the following steps: 1) constructing recombinant lentiviral vectors; 2) transfecting packing cells with the recombinant lentiviral vectors for packaging; 3) transducing the human astrocytes with packaged recombinant lentiviruses to obtain the human astrocytes stably expressing the OXTR. According to the method, the OXTR with red fluorescent protein continuously and stably expressed on the human astrocytes are successfully constructed, and real-time monitoring of OXTR becomes possible. Meanwhile, the lentiviral vectors also carry another green fluorescent protein gene copGFP, which can mark the overall outline of astrocytes, and accordingly, morphological studies of the astrocytes are convenient.

This invention provides novel substituted tricyclic pyridyl carboxamides which act as oxytocin receptor competitive antagonists, as well as methods of their manufacture, pharmaceutical compositions and methods of their use in treatment, inhibition, suppression or prevention of preterm labor, dysmenorrhea, endometritis, suppression of labor at term prior to caesarean delivery, and to facilitate antinatal transport to a medical facility. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and may be useful in the prevention and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.

The embodiment of the invention discloses a primer group for detecting the SNP genotypes of an oxytocin receptor. The primer group consists of a specific primer pair and probes, wherein the specific primer pair is used for amplifying the SNP rs53576 of the oxytocin receptor; an oxytocin receptor gene is located on 3p25 to 3p26 and comprises four exons and three introns, and the rs53576 is locatedon the third intron; the probes include a first probe with a nucleotide sequence as shown in SEQ ID NO: 3 and a second probe with a nucleotide sequence as shown in SEQ ID NO: 4. According to the embodiment of the invention, the primer group for detecting the SNP genotypes of the oxytocin receptor is provided; the primer pair and the probes are designed for amplifying the SNP rs53576 of the oxytocin receptor; the SNP types of the site SNP rs53576 of the oxytocin receptor of a detected person is judged through a fluorescence signal diagram of an amplification product; and if the SNP type of thesite SNP rs53576 is A / A, the detected person is a normal pregnant woman, or if the SNP type of the site SNP rs53576 is A / G or G / G, the detected person is a pregnant woman related to slow birth process.

Provides the oxytocin receptor (OTR) inhibitor compound 5‑(3‑(3‑(6‑fluoronaphthalene‑1‑yl)azetidin‑1‑yl)5‑(methoxymethyl)‑4H Polymorphs of -1,2,4-triazole-4-yl)-2-methoxypyridine and methods for their preparation. Compared with the amorphous form, the polymorphic OTR inhibitor has higher purity and better chemical stability, which is of great significance for the development of drugs suitable for industrial production and with good biological activity.

The invention relates to the technical field of biology, in particular to application of a gene and a construction method of an animal model. The invention discloses an Oxtr gene which can be used asa target gene for treating breast cancer; oxytocin receptor (OXTR) overexpression provides a transgenic mouse breast cancer induction model, and the model can be used for the study of the pathogenesismechanism of breast cancer and also can be used for drug screening and drug function test.

The invention discloses a construction method for human astrocytes stably expressing oxytocin receptors, comprising: 1) constructing a recombinant lentiviral vector; 2) transfecting the recombinant lentiviral vector into packaging cells for packaging; 3) using the packaged Human astrocytes were transduced with recombinant lentivirus to obtain human astrocytes stably expressing oxytocin receptor. The method of the present invention successfully constructs and obtains the oxytocin receptor with red fluorescent protein continuously and stably expressed on human astrocytes, making it possible to monitor OXTR in real time. At the same time, the lentiviral vector also carries another green fluorescent protein gene, copGFP, which can mark the overall outline of astrocytes and facilitate morphological research on astrocytes.

The present compounds compounds are oxytocin receptor agonists for the treatment of autism, stress, including post traumatic stress disorder, anxiety, including anxiety disorders and depression, schizophrenia, psychiatric disorders and memory loss, alcohol withdrawal, drug addiction and for the treatment of Prader-Willi Syndrome.

The invention relates to compounds of formulawherein variables are defined herein.It has been found that the present compounds are oxytocin receptor agonists for the treatment of autism, stress, including post traumatic stress disorder, anxiety, including anxiety disorders and depression, schizophrenia, psychiatric disorders and memory loss, alcohol withdrawal, drug addiction and for the treatment of Prader-Willi Syndrom.