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65 results about "Hemopressin" patented technology

Hemopressin (Hp) is an alpha hemoglobin fragment with the sequence PVNFKFLSH, originally identified in extracts of rat brain using an enzyme capture technique. It binds cannabinoid receptors, acting as an inverse agonist at CB₁ receptors. Longer forms of hemopressin containing 2-3 additional amino acids on the N-terminus have been identified in extracts of mouse brain. These longer hemopressin peptides, named RVD-Hpα and VD-Hpα, bind to CB1 receptors and were originally reported to be agonists. In addition to the Hp peptides from alpha hemoglobin, a related peptide from beta hemoglobin has been found in mouse brain extracts; this peptide, named VD-Hpβ, is also an agonist at CB1 cannabinoid receptors. Hemopressin is not an endogenous peptide but rather an extraction artefact [Bauer M, Chicca A, Tamborrini M, Eisen D, Lerner R, Lutz B, Poetz O, Pluschke G, Gertsch J. Identification and quantification of a new family of peptide endocannabinoids (Pepcans) showing negative allosteric modulation at CB1 receptors. J Biol Chem. 2012 Oct 26;287(44):36944-67. doi: 10.1074/jbc.M112.382481. Epub 2012 Sep 5.]. The only endogenous peptide found endogenously at physiological conditions is RVD-hemopressin (pepcan-12), which has more recently been shown to be a negative allosteric modulator of CB1 receptors and positive allosteric modulator of CB2 receptors [Bauer M, Chicca A, Tamborrini M, Eisen D, Lerner R, Lutz B, Poetz O, Pluschke G, Gertsch J. Identification and quantification of a new family of peptide endocannabinoids (Pepcans) showing negative allosteric modulation at CB1 receptors. J Biol Chem. 2012 Oct 26;287(44):36944-67. doi: 10.1074/jbc.M112.382481. Epub 2012 Sep 5.] [Petrucci V, Chicca A, Glasmacher S, Paloczi J, Cao Z, Pacher P, Gertsch J. Pepcan-12 (RVD-hemopressin) is a CB2 receptor positive allosteric modulator constitutively secreted by adrenals and in liver upon tissue damage. Sci Rep. 2017 Aug 25;7(1):9560. doi: 10.1038/s41598-017-09808-8.]. RVD-hemopressin (pepcan-12) is generated from a pro-peptide called pepcan-23 and these peptides are exclusively found in noradrenergic neurons in the brain and in the adrenal medulla [Hofer SC, Ralvenius WT, Gachet MS, Fritschy JM, Zeilhofer HU, Gertsch J. Localization and production of peptide endocannabinoids in the rodent CNS and adrenal medulla. Neuropharmacology. 2015 Nov;98:78-89. doi: 10.1016/j.neuropharm.2015.03.021. Epub 2015 Mar 31.]

Fused azepine derivatives and their use as antidiuretic agents

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.
Owner:VANTIA

Bicyclic vasopressin agonists

InactiveUS6664249B1BiocideOrganic chemistryAgonistAntidiuretic
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.
Owner:VANTIA

Heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes

The present invention provides heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula Iwherein R1, R2 and R3 are as described herein.The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
Owner:F HOFFMANN LA ROCHE & CO AG

Tricyclic benzodiazepines as vasopressin receptor antagonists

The invention is directed to tricyclic benzodiazepines useful as vasopressin receptor antagonists for treating conditions involving increased vascular resistance and cardiac insufficiency. Pharmaceutical compositions comprising tricyclic benzodiazepines of the present invention 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.
Owner:ORTHO MCNEIL PHARM INC

3-pyrrole carboxylic acid derivatives, and preparing method and application thereof

InactiveCN103420890AHas receptor antagonistic effectReceptor antagonismOrganic active ingredientsNervous disorderArginineAcid derivative
The invention relates to 3-pyrrole carboxylic acid derivatives, and a preparing method and an application thereof, and particularly relates to the 3-pyrrole carboxylic acid derivatives having a structure represented by formula I and pharmaceutically acceptable salts thereof and the preparing method of the derivatives, pharmaceutical compositions with the 3-pyrrole carboxylic acid derivatives having the structure represented by the formula I and the pharmaceutically acceptable salts of the 3-pyrrole carboxylic acid derivatives as active ingredients, and applications of the pharmaceutical compositions in prevention or treatment of diseases related with an arginine vasopressin V1a receptor, an arginine vasopressin V1b receptor, an arginine vasopressin V2 receptor, a sympathetic nervous system or a renin-angiotensin-aldosterone system.
Owner:TIANJIN INSTITUTE OF PHARMA RESEARCH

Nonpeptide substituted spirobenzoazepines as vasopressin antagonists

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.
Owner:ORTHO MCNEIL PHARM INC

Method for preparing terlipressin

The invention relates to a method for preparing terlipressin, and belongs to the technical field of polypeptide synthesis. The method comprises the steps that terlipressin peptide resin is synthesized through a fragment condensation method, 3-12 fragments are synthesized through a solid phase method, 1-2 fragments are connected to 3-12 solid phase amino-acid resin, full-peptide resin is obtained, and the terlipressin is obtained after cracking and cyclizing. Due to the fact that Boc-Gly-Cly-OH is adopted as a raw material, lack of glycine impurities is reduced, the operation step of removing glycine protection groups at an N terminal is omitted, product purity is improved, and the total cost is obviously reduced.
Owner:ANHUI UNIVERSITY OF TECHNOLOGY AND SCIENCE

Pharmaceutically active sulfanilide derivatives

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.
Owner:MERCK SERONO SA

Benzazepines compounds serving as vasopressin receptor antagonism

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.
Owner:SHANGHAI HANSOH BIOMEDICAL

Treatment of male sexual dysfunction

InactiveUS20050026810A1BiocideOrganic chemistryEjaculation disorderAVP - Arginine vasopressin
The present invention relates the use of antagonists of vasopressin V1a receptors for the treatment of male sexual dysfunction, in particular ejaculatory disorders, such as premature ejaculation or rapid ejaculation. The present invention also relates to a method of treatment of male sexual dysfunction, in particular ejaculatory disorders, such as premature ejaculation or rapid ejaculation. The present invention also relates to assays to screen for compounds useful in the treatment of male sexual dysfunction, in particular ejaculatory disorders, such as premature ejaculation or rapid ejaculation, by screening for compounds which are V1a receptor antagonists.
Owner:PFIZER INC

Treatment of congestive heart failure

Combinations of diuretics and vasopressin antagonists are useful to slow and reverse the symptoms and process of congestive heart failure, to increase the excretion of water in the urine, and to decrease the excretion of sodium and potassium ions in urine. Preferred vasopressin antagonists have the formulawherein R and R5 are hydrogen or lower alkyl;R1, R2, and R3 are hydrogen, halo, alkyl, alkoxy, and amino; andR4 is hydrogen or phenyl, and a pharmaceutically acceptable salt thereof.
Owner:CUMBERLAND PHARM INC

Fused azole derivative

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.
Owner:TAISHO PHARMACEUTICAL CO LTD

Compound with function of diuresis, preparation method and functions thereof

InactiveCN102690259AImprove solubilitySolve problems such as poor absorptionNervous disorderOrganic chemistryDiuresisSympathetic nervous system
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.
Owner:TIANJIN INSTITUTE OF PHARMA RESEARCH

Triazolobenzazepines as vasopressin v1a receptor antagonists

The present invention relates to 5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine derivatives of general formula (I) and / or salts thereof and / or geometric isomers thereof and / or stereoisomers thereof and / or enantiomers thereof and / or racemates thereof and / or diastereomers thereof and / or biologically active metabolites thereof and / or prodrugs thereof and / or solvates thereof and / or hydrates thereof and / or polymorphs thereof which are centrally and / or peripherally acting V1a receptor modulators, particularly V1a receptor antagonists. Additional subject of the present invention is the process for the preparation of the compounds and the intermediates of the preparation process as well. The invention also relates to the pharmaceutical compositions containing the compounds or together with one or more other active substances, as well as to the use in the treatment and / or prophylaxis of a disease or condition associated with V1a receptor function.
Owner:RICHTER GEDEON NYRT

Preparation method of terlipressin impurity Q

The invention relates to the technical field of polypeptide synthesis, in particular to a preparation method of a terlipressin impurity Q. The preparation method comprises the following steps: firstly synthesizing a polypeptide fragment I and a polypeptide fragment II which are good in stability, then carrying out disulfide bond exchange on SH of a fourth Cys residue at the C end of the polypeptide fragment I and SNpys or SPyr of the fourth Cys residue at the C end of the polypeptide fragment II through condensation reaction to form a first pair of disulfide bonds, and carrying out iodine oxidation reaction to form a second pair of disulfide bonds while removing an Acm protecting group of the Cys. Experiments show that the terlipressin impurity Q obtained by the preparation method is high in purity and few in impurity, and the purity of a crude product can reach 75% or above.
Owner:HYBIO PHARMA

Peptides having octopus octopressin activity and use thereof

ActiveUS11459355B2Promotes brooding behaviors of motherIncrease sociabilityPeptide/protein ingredientsPeptidesAnimal scienceAmino acid
The present invention relates to an Octopus minor-specific octopressin peptide comprising the amino acid sequence of SEQ ID NO: 3, and the peptide, by promoting the brooding behaviors of mother Octopus minor to protect her eggs, may increase the hatched larva rate when applied to partial cultivation of octopuses, and thus may be used for the growth of octopus resources.
Owner:NAT MARINE BIODIVERSITY INST OF KOREA

Process for preparing benzazepine compounds or salts thereof

This invention provides a process for preparing benzazepine compounds of the formula (1): wherein X1 is a halogen atom, R1 and R2 are a lower alkyl group, or salts thereof as well as intermediate benzoic acid compounds in high yield and high purity on industrial scale, which are useful as an intermediate for preparing a pharmaceutically active 2,3,4,5-tetrahydro-1H-1-benzazepine compound having vasopressin antagonistic activity.
Owner:OTSUKA PHARM CO LTD
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