36 results about "Vasopressin receptor" patented technology

The disclosed invention is a composition agonists and / or antagonists of V.sub.2, V.sub.1a or both receptors, in a host, including animals, and especially humans, using a small molecule or its pharmaceutically acceptable salt or prodrug.

Compounds according to general formulae (1 and 2), wherein G<1 >is an azepine derivative and G<2 >is a group according to general formulae (9-11) are new. Compounds according to the invention are vasopressin V2 receptor agonists. Pharmaceutical compositions of the compounds are useful as antidiuretic agents.

Compounds according to general formula (1), and pharmaceutically acceptable salts thereof, wherein V is a covalent bond or NH, X is selected from CH2, O and N-alkyl, Z is either S or -CH=CH-, R<1 >and R<2 >are independently selected from H, F, Cl, Br and alkyl, R<3 >is selected from OH, O-alkyl and NR<4>R<5>, R<4 >and R<5 >are each independently H or alkyl, or together are -(CH2)q-, p is 0, 1, 2, 3 or 4, and q is 4 or 5, are new. They are agonists at the asopressin V2 receptor and are useful as antidiuretics and pro-coagulants.

The invention provides methods, nucleic acids, compositions and kits for predicting a subject's response to treatment with one or more vasopressin receptor agonists to identify subjects having a greater benefit from treatment with vasopressin receptor agonist(s). The method generally comprises determining a vasopressin pathway associated gene polymorphism genotype(s) of a subject for one or more polymorphisms in the these genes, comparing the determined genotype with known genotypes for the polymorphism that correspond with an improved response genotype to identify potential subjects having an inflammatory condition who are more likely to benefit from treatment with a vasopressin receptor agonist and subsequent to treatment recover from the inflammatory condition. The invention also provides for methods of treating such subjects with vasopressin receptor agonists based on the subject's genotype.

The present invention provides a method for regulating blood pressure in a hemodialysis subject using a vasopressin receptor agonist, so as to facilitate removal of excessive extracellular fluid in the subject.

The present invention relates to triazole derivatives of formula (I) notably for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such triazole derivatives. Said triazoles are useful in the treatment and / or prevention of preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. In particular, the present invention is related to triazole derivatives displaying a substantial modulatory, in particular antagonistic activity, of the oxytocin and / or vasopressin receptor. More preferably, said compounds are useful in the treatment and / or prevention of disease states mediated by oxytocin and / or vasopressin. The present invention is furthermore related to novel triazole derivatives as well as to methods of their preparation.

Compounds, and compositions, methods, and uses thereof, are described herein for treating neurodegenerative diseases and disorders. In particular, vasopressin receptor modulators, and compositions, methods and uses thereof, are described herein for treating neuropsychiatric aspects of neurodegenerative diseases such as Huntington's Disease, Parkinson's Disease, and Alzheimer's Disease.

The present invention relates to sulfanilide derivatives of formula (I), in which R1 and R2 are optionally substituted aryl and heteroaryl groups and the other variables are as defined in the claims, for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such sulfanilide derivatives. Said derivatives are useful in the treatment and / or prevention of preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. In particular, the present invention is related to sulfanilide derivatives displaying a substantial modulatory, in particular antagonistic activity, of the oxytocin and / or vasopressin receptor. More preferably, said compounds are useful in the treatment and / or prevention of disease states mediated by oxytocin and / or vasopressin, including preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. The present invention is furthermore related to novel sulfanilide derivatives as well as to methods of their preparation.

The invention relates to a benzazepines compounds serving as vasopressin receptor antagonism, in particular to a benzazepines compound shown in formula (I) or pharmaceutically acceptable salt thereof and a preparation method thereof, and a medicinal composition containing a compound containing curative dose of the compound or the pharmaceutically acceptable salt thereof, and application in preparing medicament for treating diseases related to the vasopressin thereof.

The present invention relates to a vasopressin receptor 1B (V1B) antagonist for use in the treatment of depressive symptoms and / or anxiety symptoms in patients showing an elevated arginine vasopressin (AVP) level and / or an elevated copeptin level. The present invention further relates to a method for predicting the treatment response to a V1B antagonist in patients with depressive symptoms and / or anxiety symptoms.

The invention is directed to nonpeptide substituted benzodiazepines of Formula I, wherein A, X, n, R1, R2, R3, R4, R5, a and b are as described in the specification, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as those involving increased vascular resistance and cardiac insufficiency. Pharmaceutical compositions comprising a compound of Formula I and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, cerebral edema and ischemia, stroke, thrombosis, or water retention are also disclosed.

The present invention provides peptides for use in a medicament which is administered nasally, wherein the peptide is an agonist of neuropeptide S receptor (NPSR), of the receptor TGR23 and / or of vasopressin receptor-related receptor 1 (VRR1) or for use in the treatment of a patient by causing, promoting or increasing relieve or healing of phobic anxiety, avoidance anxiety, dissociative anxiety such as flashbacks, depersonalization, derealization, intrusions, vegetative symptoms related to anxiety symptoms, especially in panic attacks, in posttraumatic stress disorder, in generalised anxiety disorder and in anxiety accompanying depressive, or psychotic episodes, arousal, awakening, alertness, activity, spontaneous movement, an anxiolytic effect or a combination thereof in the patient, wherein the peptide is administered nasally or for use in the prophylaxis and / or treatment of an anxiety or sleep disorder, especially in any type of hypersomnia like idiopathic hypersomnia, wherein the peptide is administered nasally. Further provided are pharmaceutical compositions for nasal administration comprising at least one of said peptides, uses of said peptide or said pharmaceutical composition. The invention also provides a method for identifying target neurons of a peptide in an animal, wherein the peptide is administered nasally.

The use of opportunely modified specific ligands of the receptor for urotensin II (UTR) or antibodies (commercially available) raised against the same receptor as tools for the definition of both the differentiation and the prognosis of human prostate adenocarcinoma is described, moreover, the use of opportunely radiolabeled ligands for UTR in the definition of the extension of disease is also described.

The present invention provides a method for regulating blood pressure in a hemodialysis subject using a vasopressin receptor agonist, so as to facilitate removal of excessive extracellular fluid in the subject.

The present invention relates to a vasopressin receptor 1B (V1B) antagonist for use in the treatment of depressive symptoms and / or anxiety symptoms in patients showing an elevated arginine vasopressin (AVP) level and / or an elevated copeptin level. The present invention further relates to a method for predicting the treatment response to a V1B antagonist in patients with depressive symptoms and / or anxiety symptoms.

Provided is a therapeutic or prophylactic agent for mood disorders, anxiety, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorders, hypertension, digestive diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune related diseases, depilation, and so on. More specifically, provided is a fused azole derivative represented by general formula (I), which has arginine vasopressin 1b receptor antagonism, or a pharmaceutically acceptable salt thereof.

The invention is directed to nonpeptide substituted spiroheterobenzazepine of Formula I, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as those involving increased vascular resistance and cardiac insufficiency, including congestive heart failure, hyponatremia, and hypertension. Pharmaceutical compositions comprising a compound of Formula I and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, hyponatremia, renal vasospasm, renal insufficiency, renal failure, diabetic nephropathy, cerebral edema, cerebral ischemia, stroke, thrombosis, or water retention are also disclosed.

The invention belongs to the technical field of medicaments with a function of diuresis, and discloses benzazepine compound with a general formula I structure, pharmaceutically acceptable salts, an R definition and R claims. The invention further discloses a preparation method for the compound, a medicament composition which takes the compound or the pharmaceutically acceptable salts as active effective components and functions of preventing or treating illnesses related to an arginine vasopressin receptor V1a, an arginine vasopressin receptor V1b, an arginine vasopressin receptor V2, a sympathetic nervous system or a system of rennin-angiotensin-aldosterone.

In alternative embodiments, provided are methods for: modifying circadian rhythmicity or timing in a mammal, treating psychiatric conditions or symptoms due to alterations in a human circadian regulatory system, treating sleep problems in a mammal, or inducing sleep or activity suppression, or causing an arousal or wakening reaction, comprising administration to a mammal or human a compound or composition capable of modifying a prokineticin 2 (PK2) expression or activity, and / or a PKR2 (PK2 receptor), a vasopressin receptor (VR), and / or a melatonin receptor (MR) expression or activity.

Combination of antagonists of the vasopressin receptor and calciomimetics and composition comprising it, and its use for the prevention and / or treatment of polycystic kidney.

The use of opportunely modified specific ligands of the receptor for urotensin II (UTR) or antibodies (commercially available) raised against the same receptor as tools for the definition of both the differentiation and the prognosis of human prostate adenocarcinoma is described, moreover, the use of opportunely radiolabeled ligands for UTR in the definition of the extension of disease is also described.

The invention relates to a label-free arginine vasopressin receptor cell model construction and ligand screening method, in particular to a method for building the models of a subtype (V1a receptor) of an arginine vasopressin receptor on different cell lines and for carrying ligand screening by using a label-free cell dynamic mass reset technology. The V1a receptor model disclosed by the invention is constructed on an HEK293 cell line for endogenous expression of the V1a receptor and a transfected CHO-V1a cell line. The method has the characteristics of being close to an in-vivo real environment, free of labels, capable of monitoring in real time, high in flux and simple to operate, and ligands with V1a receptor activity, including agonists and antagonists, can be screened.

The present invention relates to triazole derivatives of formula (I) notably for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such triazole derivatives. Said triazoles are useful in the treatment and / or prevention of preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. In particular, the present invention is related to triazole derivatives displaying a substantial modulatory, in particular antagonistic activity, of the oxytocin and / or vasopressin receptor. More preferably, said compounds are useful in the treatment and / or prevention of disease states mediated by oxytocin and / or vasopressin. The present invention is furthermore related to novel triazole derivatives as well as to methods of their preparation.

A medicament for suppressing development of tolerance to analgesic effect induced by administration of a narcotic analgesic such as morphine, which comprises an antagonist of the vasopressin receptor 1b as an active ingredient.

The invention relates to a benzazepines compounds serving as vasopressin receptor antagonism, in particular to a benzazepines compound shown in formula (I) or pharmaceutically acceptable salt thereof and a preparation method thereof, and a medicinal composition containing a compound containing curative dose of the compound or the pharmaceutically acceptable salt thereof, and application in preparing medicament for treating diseases related to the vasopressin thereof.