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32 results about "Oxytocin Antagonist" patented technology
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Any of the synthetic agents that inhibit or antagonize the biosynthesis or biologic effects of oxytocin by either antagonizing the responsiveness of oxytocin sensitive tissues or competing with its binding sites.
Heptapeptide oxytocin analogues
InactiveUS6143722AImprove stabilityAdequate potencyNervous disorderPeptide/protein ingredientsOxytocinAmide bonds
PCT No. PCT / SE97 / 01968 Sec. 371 Date Aug. 2, 1999 Sec. 102(e) Date Aug. 2, 1999 PCT Filed Nov. 21, 1997 PCT Pub. No. WO98 / 23636 PCT Pub. Date Jun. 4, 1998Heptapeptide analogues or pharmaceutically acceptable salts thereof consist of a hexapeptide moiety S and a C-terminal beta -aminoalcohol residue Z bound to the moiety S by an amide bond, wherein the beta -aminoalcohol Z is -NR-CH(Q)-CH2OH, Q is (CH2)n-NH-A is H or -C(=NH)NH2, and R is CH3 or C2H5, and the moiety S wherein H is a D-aromatic alpha -aminoacid and Y is an aliphatic alpha -aminoacid and have oxytocin antagonist activity. Also disclosed is: a method of their synthesis; pharmaceutical compositions containing these analogues; the synthesis of such compositions; a method of control of uterine contractions.
Owner:FERRING BV
Hydroxy cyclohexenyl phenyl carboxamides tocolytic oxytocin receptor antagonists
The present invention provides substituted 10,11-Dihydro-5H-benzo[e]-pyrrolo[1,2-a][1,4]diazepine and 9,10-Dihydro-4H-3a,5,9-triaza-benzo[f]azulene compounds as well as methods and pharmaceutical compositions utilizing these compounds for the treatment and / or prevention and / or suppression of disorders which may be remedied or alleviated by oxytocin antagonist activity, including prevention and / or suppression of preterm labor, suppression labor at term prior to caesarean deliver, and for the treatment of dysmenorrhea. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals.
Owner:WYETH
Cyclohexenyl phenyl carboxamides tocolytic oxytocin receptor antagonists
The present invention provides tricyclic carboxamide compounds and methods and pharmaceutical compositions for their use in treatment, prevention, or suppression of disorders which may be remedied or alleviated by oxytocin antagonist activity, including prevention and / or suppression of preterm labor, suppression of labor at term prior to caesarean deliver, and for the treatment of dysmenorrhea. 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.
Owner:WYETH LLC
Cyclohexylphenyl carboxamides tocolytic oxytocin receptor antagonists
The present invention provides novel tricyclic benzodiazepine carboxamides compounds and methods and pharmaceutical compositions utilizing them for the treatment and / or prevention and / or suppression of disorders which may be remedied or alleviated by oxytocin antagonist activity, including prevention and / or suppression suppression of preterm labor, suppression of labor at term prior to caesarean delivery, and for the treatment of dysmenorrhea. 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.
Owner:WYETH
Tricyclic diazepines tocolytic oxytocin receptor antagonists
This invention provides novel tricyclic diazepine compounds as well as methods and pharmaceutical compositions utilizing these compounds for the treatment and / or prevention and / or suppression of disorders which may be remedied or alleviated by oxytocin antagonist activity, including treatment of preterm labor, dysmenorrhea, endometritis, and for suppressing labor prior to caesarean delivery. 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.
Owner:WYETH LLC
Pyrrolidine derivatives as oxytocin antagonists
Owner:MERCK SERONO SA
Pyrrolidine derivatives as oxytocin antagonists
The present invention relates to novel pyrrolidine derivative of formula (I), its geometrical isomers, its optically active forms as enantiomers, diastereomers, mixtures of these and its racemate forms, as well as salts thereof, wherein R1 is selected from the group comprising or consisting of H and C1-C6-alkyl, for the prevention and / or treatment of preterm labor, premature birth or dysmenorrhea.
Owner:MERCK SERONO SA
Treatment of male sexual dysfunction
A composition comprising a selective oxytocin antagonist for use in the treatment and / or prevention of a male ejaculatory disorder; which selective oxytocin antagonist is optionally admixed with a pharmaceutically acceptable carrier, diluent or excipient.
Owner:IXCHELSIS
Pyrrolidine derivatives as oxytocin antagonists
The present invention relates to novel pyrrolidine derivatives of Formula (I), its geometrical isomers, its optically active forms as enantiomers, diastercomers, mixtures of these and its racemate forms, as well as salts thereof, wherein: Rlis selected from the group comprising or consisting of H and C1-C6-alkyl; R2 is selected from the group comprising or consisting of hydrogen, C1-C6-alkyl, C1-C6 alkyl aryl, heteroaryl, C1-C6 alkyl heteroaryl, C2-C6-alkenyl, C2-C6-alkenyl aryl, C2-C6 alkenyl heteroaryl, C2-C6-alkynyl, C2-C6-alkynyl aryl, C2C6-alkynyl heteroaryl, C3-C8 cycloalkyl, heterocycloalkyl, C1-C6-alkyl cycloallcyl, C1-C6-alkyl heterocycloalkyl, C1C6 alkyl carboxy, acyl, C1-C6-alkyl acyl, C1-C6-alkyl acyloxy, C1-C6-alkyl alkoxy, alkoxycarbonyl, C1-C6-alkyl alkoxycarbonyl, aminocarbonyl, C1-C6-alkyl aminocarbonyl, C1-C6-alkyl acylarnino, C1-C6-alkyl ureido, amino, C1-C6-alkyl amino, sulfonyloxy, C1-C6 alkyl sulfonyloxy, sulfonyl, C1-C6-alkyl sulfonyl, sulfinyl, C1-C6-alkyl sulfinyl, C1-C6alkyl sulfanyl, C1-C6-alkyl sulfonylamino;
Owner:MERCK SERONO SA
Triazoles as oxytocin antagonists
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.
Owner:MERCK SERONO SA
Peptides as oxytocin agonists
InactiveUS20170081369A1Enhance onset and maintenanceOxytocins/vasopressinsNervous disorderPrader�Willi syndromeRecurrent anxiety
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.
Owner:F HOFFMANN LA ROCHE & CO AG
Diazacycloalkanes as oxytocin agonists
Compounds according to general formula (1), wherein G1 is NR5R6 or a fused polycyclic group are novel. They are selective and potent oxytocin agonists. Pharmaceutical compositions of such compounds are useful in the treatment of, inter alia, erectile dysfunction.
Owner:FERRING BV
Method and system for diagnosing uterine contraction levels using image analysis
Method of analyzing uterine contractions by analyzing uterine images using deformable model networks in support of embryo transfer techniques. The method is also used to diagnose premature uterine contractile activity in mammals. The method can be used to control contractile activity during embryo transfer or premature labor when used in conjunction with oxytocin antagonists.
Owner:FERRING BV
Treatment of male sexual dysfunction
InactiveUS20090175793A1Organic active ingredientsOrganic chemistrySexual functioningPharmaceutical medicine
Owner:IXCHELSIS
Piperazine-2,5-dione derivative, as well as preparation method and application thereof to medicine
The invention relates to a piperazine-2,5-dione derivative, as well as a preparation method and application thereof to medicine, and particularly relates to a piperazine-2,5-dione derivative shown asa general formula (I) in the description, a preparation method, a medicinal composition containing the derivative thereof, and application thereof to treatment or prevention of known diseases or diseases to which oxytocin has a beneficial effect as a therapeutic agent, particularly an oxytocin antagonist. The definition of each group in the general formula (I) is the same as the definition in thedescription. The formula (I) is shown in the description.
Owner:JIANGSU HENGRUI MEDICINE CO LTD +1
Fused ring azetidinyl triazole derivatives, preparation method and application in medicine
ActiveCN108884071BPharmacokinetic absorption is goodHas pharmacokinetic advantagesOrganic active ingredientsOrganic chemistryDiseasePharmaceutical drug
The invention relates to a condensed ring-based azetidinyl triazole derivative, a preparation method thereof and an application in medicine. Specifically, the present invention relates to a new fused ring-based azetidinyl triazole derivative represented by general formula (I), its preparation method and its pharmaceutical composition containing the derivative and its therapeutic agent, especially as an oxytocin antagonist and in the preparation of a medicament for the treatment or prevention of a disease or condition for which inhibition of oxytocin is known or can be shown to have a beneficial effect, wherein each of the general formula (I) replaces The base is the same as defined in the specification.
Owner:JIANGSU HENGRUI MEDICINE CO LTD +1
Pharmaceutical composition of male sexual dysfunction
A composition comprising a selective oxytocin antagonist for treating and / or preventing male ejaculatory disorders; the selective oxytocin antagonist can optionally be mixed with a pharmaceutically acceptable carrier, diluent or excipient.
Owner:埃克切西斯有限公司
Novel 3-c(o)r substituted 10-cyclohexylbenzoyl pyrrolobenzodiazepines; tocolytic oxytocin receptor antagonists
The present invention provides novel tricyclic benzodiazepine carboxamides compounds and methods and pharmaceutical compositions utilizing them for the treatment and / or prevention and / or suppression of disorders which may be remedied or alleviated by oxytocin antagonist activity, including prevention and / or suppression suppression of preterm labor, suppression of labor at term prior to caesarean delivery, and for the treatment of dysmenorrhea. 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 treatmraent of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.
Owner:WYETH LLC
Pyrido cyclohexenyl phenyl carboxamides tocolytic oxytocin receptor antagonists
The present invention provides novel tricyclic pyridyl carboxamides as well as methods and pharmaceutical compositions utilizing them compounds for the treatment and / or prevention and / or suppression of disorders which may be remedied or alleviated by oxytocin antagonist activity, including prevention and / or suppression of preterm labor, suppression of labor at term prior to caesarean delivery, and for the treatment of dysmenorrhea. 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.
Owner:WYETH
New methods for making barusiban and its intermediates
InactiveCN108290929AOxytocins/vasopressinsPeptide/protein ingredientsPropanoic acidOxytocin Antagonist
The present invention relates to new solid phase peptide methods for synthesizing analogues that exhibit oxytocin antagonist activity, specifically Barusiban and its intermediates. Specifically, the present invention relates to a solid phase process for preparing a compound having the formula c[AA1-AA6]-AA7-ol, wherein AA1 is propionic acid, AA2 is preferably D-Trp, AA3 is Ile, AA4 is preferably AlloIle, AA5 is Asn, AA6 is hCy, and AA7 is preferably N-Me-Orn-ol, or a pharmaceutically acceptable salt or solvate thereof.
Owner:FERRING BV
New methods for making barusiban and its intermediates
InactiveUS20180282367A1Oxytocins/vasopressinsPeptide/protein ingredientsPropanoic acidOxytocin Antagonist
The present invention relates to new solid phase peptide methods for synthesizing analogues that exhibit oxytocin antagonist activity, specifically Barusiban and its intermediates. Specifically, the present invention relates to a solid phase process for preparing a compound having the formula c[AA1-AA6]-AA7-ol, wherein AA1 is propionic acid, AA2 is preferably D-Trp, AA3 is Ile, AA4 is preferably AlloIle, AA5 is Asn, AA6 is hCy, and AA7 is preferably N-Me-Orn-ol, or a pharmaceutically acceptable salt or solvate thereof.
Owner:FERRING BV
Oxytocin antagonist dosing regimens for promoting embryo implantation and preventing miscarriage
PendingUS20190247361A1Enhance endometrial receptivityReduce the possibilityPeptide/protein ingredientsMammal material medical ingredientsRegimenMiscarriage
The invention provides compositions and methods for the use of oxytocin antagonists, such as substituted pyrrolidin-3-one oxime derivatives, among other compounds, in the treatment of subjects undergoing embryo transfer therapy. The compositions and methods of the invention can be used to dose subjects with oxytocin antagonists, including (3Z,55)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methyloxime, among others, so as to improve endometrial receptivity and reduce the likelihood of embryo implantation failure and miscarriage following, for example, in vitro fertilization (IVF) and intracytoplasmic sperm injection (ICSI) embryo transfer procedures.
Owner:OBSEVA
Tricyclic diazepines as tocolytic oxytocin receptor antagonists
This invention provides novel tricyclic diazepine compounds as well as methods and pharmaceutical compositions utilizing these compounds for the treatment and / or prevention and / or suppression of disorders which may be remedied or alleviated by oxytocin antagonist activity, including treatment of preterm labor, dysmenorrhea, endometritis, and for suppressing labor prior to caesarean delivery. 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.
Owner:WYETH LLC
Triazoles as oxytocin antagonists
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.
Owner:MERCK SERONO SA
Novel 10-cyclohexenyl-phenyl pyrrolobenzodiazepine-3-carboxamides and derivatives thereof; tocolytic oxytocin receptor antagonists
Owner:WYETH LLC
Method and system for diagnosing uterine contraction levels using image analysis
A method for analyzing uterine contractions to support embryo transfer techniques by analyzing uterine images using a deformable model network. The method is also used to diagnose premature uterine contraction activity in mammals. When used with an oxytocin antagonist, the method can be used to control contractile activity during embryo transfer or preterm birth.
Owner:FERRING BV
Novel hydroxy cyclohexenyl phenyl carboxamides tocolytic oxytocin receptor antagonists
Owner:WYETH LLC
Pyrrolidine derivatives as oxytocin antagonists
The present invention relates to novel pyrrolidine derivatives of Formula (I), its geometrical isomers, its optically active forms as enantiomers, diastercomers, mixtures of these and its racemate forms, as well as salts thereof, wherein: R1is selected from the group comprising or consisting of H and C1-C6-alkyl; R2 is selected from the group comprising or consisting of hydrogen, C1-C6-alkyl, C1-C6 alkyl aryl, heteroaryl, C1-C6 alkyl heteroaryl, C2-C6-alkenyl, C2-C6-alkenyl aryl, C2-C6 alkenyl heteroaryl, C2-C6-alkynyl, C2-C6-alkynyl aryl, C2C6-alkynyl heteroaryl, C3-C8 cycloalkyl, heterocycloalkyl, CI-C6-alkyl cycloallcyl, CI-C6-alkyl heterocycloalkyl, CIC6 alkyl carboxy, acyl, C1-C6-alkyl acyl, C1-C6-alkyl acyloxy, C1-C6-alkyl alkoxy, alkoxycarbonyl, C1-C6-alkyl alkoxycarbonyl, aminocarbonyl, C1-C6-alkyl aminocarbonyl, C1-C6-alkyl acylarnino, C1-C6-alkyl ureido, amino, C1-C6-alkyl amino, sulfonyloxy, C1-C6 alkyl sulfonyloxy, sulfonyl, C1-C6-alkyl sulfonyl, sulfinyl, C1-C6-alkyl sulfinyl, C1-C6alkyl sulfanyl, C1-C6-alkyl sulfonylamino.
Owner:MERCK SERONO SA
Novel pyridine- and cyclohexenyl-comprising pyrrolobenzodiazepi ne-carboxamides and derivatives thereof; tocolytic oxytocin receptor antagonists
The present invention provides novel tricyclic pyridyl carboxamides as well as methods and pharmaceutical compositions utilizing them compounds for the treatment and / or prevention and / or suppression of disorders which may be remedied or alleviated by oxytocin antagonist activity, including prevention and / or suppression of preterm labor, suppression of labor at term prior to caesarean delivery, and for the treatment of dysmenorrhea. 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.
Owner:WYETH LLC
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