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37 results about "GABA B Agonists" patented technology
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Agonists GABA Baclofen is a GABA analogue which acts as a selective agonist of GABAB receptors, and is used as a muscle relaxant. However, it can aggravate absence seizures, and so is not used in epilepsy. gamma-Hydroxybutyrate (GHB) Phenibut Isovaline 3-Aminopropylphosphinic acid Lesogaberan
Methods and compositions for the treatment of brain reward system disorders by combination therapy
The present invention is directed to a combination treatment of an opioid antagonist e.g., naltrexone and a second compound selected from the group consisting of a GABA B agonist, an NMDA antagonist, a serotonin antagonist, and a cannabinoid antagonist is the key to the successful treatment of a brain reward system disorder. A brain reward system, include but are not limited, to pathological gambling, compulsive alcohol consumption, compulsive over-eating and obesity, compulsive smoking, and drug addiction. The compounds and methods of the present invention effectively reduce the cravings, withdrawal symptoms and negative drug side effects associated with a monotherapy. As such, patient compliance is greatly increased, thereby decreasing relapse of a brain reward system disorder.
Owner:ALKERMES INC
Thieno-pyridine derivatives as allosteric enhancers of the GABAB receptors
InactiveUS20060135552A1Valuable therapeutic propertyBiocideNervous disorderThienopyridine DerivativesMuscular spasticity
The present invention relates to compounds of formula I wherein R1, R2, R3, R4, and R5 are as defined in the specification. Compounds of the invention are active on the GABAB receptor and are useful for treating a variety of CNS disorders, including anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity-and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, psychosis, panic disorder, posttraumatic stress disorders and gastrointestinal disorders.
Owner:F HOFFMANN LA ROCHE & CO AG
Pharmaceutical dosage forms having immediate release and/or controlled release properties that contain a GABAB receptor agonist
The present invention relates generally to pharmaceutical dosage forms having immediate release and controlled release properties that contain a γ-aminobutyric acid (GABAB) receptor agonist, e.g., baclofen, for the treatment of medical conditions, which includes spasms, cramping, and tightness of muscles, associated with ailments such as multiple sclerosis or certain spinal injuries.
Owner:IMPAX LAB INC
Pharmaceutical dosage forms having immediate and controlled release properties that contain a GABAB receptor agonist
The present invention relates generally to pharmaceutical dosage forms having immediate release and controlled release properties that contain a γ-aminobutyric acid (GABAB) receptor agonist, e.g., baclofen, for the treatment of medical conditions, which includes spasms, cramping, and tightness of muscles, associated with ailments such as multiple sclerosis or certain spinal injuries.
Owner:IMPAX LAB INC
First glass photoaffinity labeling difunctional probe molecule and preparation method and application thereof
The invention relates to a first glass photoaffinity labeling difunctional probe molecule, which has combining ability of strong metabotropic (GABAB) receptor appetency and high selectivity, simultaneously can be used for remarking, tracking and analyzing dynamic change procedures of relevant signal albumen caused by activating or antagonism of the GABAB receptor on a living cell level pair film. The first glass photoaffinity labeling difunctional probe molecule is used for recovering novel target spots and studying protein spectrum, and provides direct, accurate and important information for diagnosis of diseases relevant to the GABAB receptor and development of corresponding psychotherapeutic drugs.
Owner:SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI +1
Pharmaceutical dosage forms having controlled release properties that contain a GABAB receptor agonist
The present invention relates generally to pharmaceutical dosage forms having immediate release and controlled release properties that contain a γ-aminobutyric acid (GABAB) receptor agonist, e.g., baclofen, for the treatment of medical conditions, which includes spasms, cramping, and tightness of muscles, associated with ailments such as multiple sclerosis or certain spinal injuries.
Owner:IMPAX LAB INC
Method for improving cognitive function by co-administration of a GABAB receptor antagonist and an acetylcholinesterase inhibitor
InactiveUS20050267077A1Improve cognitive functionBiocideNervous disorderCholinesterase inhibitionCo administration
The present invention provides methods and compositions for improving cognitive function by administering a GABAB receptor antagonist and an acetylcholinesterase inhibitor.
Owner:THE JOHN HOPKINS UNIV SCHOOL OF MEDICINE
Novel Compounds For The Treatment Of GI Disorders 682
InactiveUS20080262064A1Good curative effectBiocideOrganic active ingredientsAgonistFunctional gastrointestinal disorder
The present invention relates to novel imidazole compounds having a positive allosteric GABAB receptor (CUR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS).
Owner:ASTRAZENECA AB
Novel GABAB receptor DNA sequences
DNA encoding a novel human GABAB receptor subunit, HG20, as well as the protein encoded by the DNA, is provided. Also provided is DNA encoding a novel murine GABAB receptor subunit, GABABR1a, as well as the protein encoded by the DNA. Heterodimers of HG20 protein and GABABR1a protein that form a functional GABAB receptor are disclosed. Methods of identifying agonists and antagonists of the GABAB receptor are also provided.
Owner:BOARD OF RGT THE UNIV OF TEXAS SYST +3
Anti-obesity agent and use thereof
InactiveCN101500610AOrganic active ingredientsMetabolism disorderBULK ACTIVE INGREDIENTActive ingredient
Owner:NAGOYA UNIVERSITY
Pharmaceutical dosage forms having controlled release properties that contain a GABAB receptor agonist
The present invention relates generally to pharmaceutical dosage forms having controlled release properties that contain a γ-aminobutyric acid (GABAB) receptor agonist, e.g., baclofen, for the treatment of medical conditions, which includes spasms, cramping, and tightness of muscles, associated with ailments such as multiple sclerosis or certain spinal injuries.
Owner:IMPAX LAB INC
Aminomethylpyrimidines as allosteric enhancers of the GABAB receptors
InactiveUS20050197337A1Valuable therapeutic propertyBiocideNervous disorderMuscular spasticityPosttraumatic stress disorders
The present invention relates to compounds of formula whereinX is —S— or —NH—; R3 / R4 together with the N-atom to which they are attached form a non aromatic 5, 6 or 7 membered ring, which optionally contains in addition to the N-atom one additional heteroatom selected from the group consisting of O, S and N, and wherein the ring is optionally substituted by hydroxy, lower alkyl, lower alkoxy, —NR2, —CONR2, —CO-lower alkyl or benzyl; or R3 / R4 form together with the N-atom to which they are attached a heterocyclic ring system, containing two or three rings and which optionally contains one or two additional heteroatoms selected from the group consisting of N and O and which has no more than 20 carbon atoms; andR, R1, R2, and R5 are as defined herein and to pharmaceutically suitable acid addition salts thereof. It has been found that the compounds of the invention are active on the GABAB receptor and therefore are useful for the treatment of anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, psychosis, panic disorder, posttraumatic stress disorders and gastro-intestinal disorders.
Owner:F HOFFMANN LA ROCHE & CO AG
Compositions and methods for treating or preventing gastrointestinal disorders and gerd-related respiratory disorders
InactiveUS20140105851A1Effective treatmentDigestive systemSynthetic polymeric active ingredientsDiseaseHistamine h
Disclosed herein are novel compositions and methods for treating or preventing GI tract disorders and / or GERD-related respiratory disorders as well as protecting stratified squamous epithelium against injury by a noxious substance. The methods generally include administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition comprising at least one bile acid sequestrant, alone or in combination with at least one proton pump inhibitor, and optionally one or more agent chosen from antacids, histamine H2-receptor antagonists, γ-aminobutyricacid-b (GABA-B) agonists, prodrugs of GABA-B agonists, and protease inhibitors.
Owner:IRONWOOD PHARMA
Gastro-retentive sustained-release oral dosage form of a bile acid sequestrant
InactiveCN105338958APrevent backflowAvoid damageOrganic active ingredientsPeptide/protein ingredientsDiseaseHistamine h2 receptor antagonist
Disclosed herein are novel compositions and methods for controlling the release of bile acid sequestrant to the stomach in order to treat or prevent upper GI tract disorders or disorders of the throat. The methods generally include administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition comprising at least one bile acid sequestrant dispersed in a polymeric matrix. The bile acid sequestrant composition may be administered alone or in combination with at least one proton pump inhibitor, and optionally one or more agents chosen from antacids, histamine H2-receptor antagonists, gamma-aminobutyric acid-beta (GABA-B) agonists, prodrugs of GABA-B agonists, acid pump antagonists, protease inhibitors and GC-C agonists.
Owner:IRONWOOD PHARMA
Chemical composite preparation and use thereof
InactiveCN101422610APlay a role in detoxificationPlay a role in rehabilitationNervous disorderPeptide/protein ingredientsCurative effectNK1 receptor antagonist
The invention relates to a chemical composite preparation and an application thereof, which belong to the technical field of addition medical applications and are characterized in that the chemical composite preparation consists of a GABAB receptor agonist material, an M receptor antagonist material and an auxiliary material (any one of starch, pre-gelatinized starch and dextrin), and the weight proportions of the effective constituents of the materials are as follows: 1 to 40 percent of the GABAB receptor agonist material, 1 to 15 percent of the M receptor antagonist material and 45 to 98 percent of the auxiliary material, and the materials are prepared into tablets according to the conventional method. The chemical composite preparation can be other preparations prepared by the conventional method after changing the auxiliary material. The chemical composite preparation is used for curing opioid type drug dependent patients in the aspects of drug discarding, rehabilitation and drug retaking resistance, and the healing effect is better than that of singly used M receptor antagonist or GABAB receptor agonist, and the invention has significant drug retaking resistant effect.
Owner:袁才蔚
Methods for diagnosing and treating encephalitis or epilepsy
This invention provides methods of diagnosing or determining a cause of an autoimmune encephalitis or an epilepsy in a subject and of diagnosing a tumor in a subject, comprising the step of testing a biological sample of the subject for an anti-body to a GABAB receptor. This invention further provides methods of treating an autoimmune encephalitis or an epilepsy, comprising the steps of detecting an antibody to a GABAB receptor and treating a tumor associated with the disease.
Owner:THE TRUSTEES OF THE UNIV OF PENNSYLVANIA
Chemical compound medicament for curing alcohol dependence
InactiveCN101559054APlay a therapeutic effectLittle side effectsOrganic active ingredientsNervous disorderSide effectTreatment effect
The invention relates to a chemical compound medicament for curing alcohol dependence. The chemical compound medicament is characterized by containing GABAB receptor stimulating agent baclofen bulk medicament, M receptor antagonist paralest bulk medicament and auxiliary material. The material comprises the following effective components by the weight percent: 0.3-15 of baclofen, 0.05-5of paralest and 80-99.65 of auxiliary material. Taballa or medicament in other forms is prepared by regular methods. The chemical compound medicament has remarkable curative effect and little side effect in the aspects of abstinence, rehabilitation and relapse resistance for alcohol reliers.
Owner:袁才蔚
Triazinedione derivatives as GABAB receptor modulators
Owner:ADDEX PHARM SA
Aminomethylpyrimidines as allosteric enhancers of the GABAB receptors
The present invention relates to compounds of formulawhereinX is —S— or —NH—;R3 / R4 together with the N-atom to which they are attached form a non aromatic 5, 6 or 7 membered ring, which optionally contains in addition to the N-atom one additional heteroatom selected from the group consisting of O, S and N, and wherein the ring is optionally substituted by hydroxy, lower alkyl, lower alkoxy, —NR2, —CONR2, —CO-lower alkyl or benzyl; or R3 / R4 form together with the N-atom to which they are attached a heterocyclic ring system, containing two or three rings and which optionally contains one or two additional heteroatoms selected from the group consisting of N and O and which has no more than 20 carbon atoms; andR, R1, R2, and R5 are as defined herein and to pharmaceutically suitable acid addition salts thereof.It has been found that the compounds of the invention are active on the GABAB receptor and therefore are useful for the treatment of anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, psychosis, panic disorder, posttraumatic stress disorders and gastro-intestinal disorders.
Owner:F HOFFMANN LA ROCHE INC
Pharmacologically active alicyclic-substituted pyrazolo[1,5-a]pyrimidine derivatives
![Pharmacologically active alicyclic-substituted pyrazolo[1,5-a]pyrimidine derivatives](https://images-eureka.patsnap.com/patent_img/010e293f-3bfc-43f0-8644-391a35f12f95/US11026946-C00001.png "Pharmacologically active alicyclic-substituted pyrazolo[1,5-a]pyrimidine derivatives")
![Pharmacologically active alicyclic-substituted pyrazolo[1,5-a]pyrimidine derivatives](https://images-eureka.patsnap.com/patent_img/010e293f-3bfc-43f0-8644-391a35f12f95/US11026946-C00002.png "Pharmacologically active alicyclic-substituted pyrazolo[1,5-a]pyrimidine derivatives")
![Pharmacologically active alicyclic-substituted pyrazolo[1,5-a]pyrimidine derivatives](https://images-eureka.patsnap.com/patent_img/010e293f-3bfc-43f0-8644-391a35f12f95/US11026946-C00003.png "Pharmacologically active alicyclic-substituted pyrazolo[1,5-a]pyrimidine derivatives")
Owner:RICHTER GEDEON NYRT
Pharmacologically Active Alicyclic-Substituted Pyrazolo[1,5-a]Pyrimidine Derivatives
ActiveUS20200129515A1Increased in vitro potencyLarge effect sizeOrganic active ingredientsNervous disorderDiseaseAllosteric modulator
The present invention relates to new pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof that serve as GABAB receptor positive allosteric modulators. The invention al so relates to the process for producing such compounds. The invention further relates to pharmaceutical compositions comprising such compounds optionally in combination with two or more different therapeutic agents and the use of such compounds in methods for treating diseases and conditions mediated and modulated by the GABAB receptor positive allosteric mechanism. The invention al so provides a method for manufacture of medicaments useful in the treatment of such disorders.
![Pharmacologically Active Alicyclic-Substituted Pyrazolo[1,5-a]Pyrimidine Derivatives](https://images-eureka.patsnap.com/patent_img/0bfd6c40-4928-40d7-b355-2373a7ecfa1c/US20200129515A1-C00001.png "Pharmacologically Active Alicyclic-Substituted Pyrazolo[1,5-a]Pyrimidine Derivatives")
![Pharmacologically Active Alicyclic-Substituted Pyrazolo[1,5-a]Pyrimidine Derivatives](https://images-eureka.patsnap.com/patent_img/0bfd6c40-4928-40d7-b355-2373a7ecfa1c/US20200129515A1-C00002.png "Pharmacologically Active Alicyclic-Substituted Pyrazolo[1,5-a]Pyrimidine Derivatives")
![Pharmacologically Active Alicyclic-Substituted Pyrazolo[1,5-a]Pyrimidine Derivatives](https://images-eureka.patsnap.com/patent_img/0bfd6c40-4928-40d7-b355-2373a7ecfa1c/US20200129515A1-C00003.png "Pharmacologically Active Alicyclic-Substituted Pyrazolo[1,5-a]Pyrimidine Derivatives")
Owner:RICHTER GEDEON NYRT
A class of gabab receptor negative allosteric modulator and its medical application
InactiveCN104557495BInhibition of activationNervous disorderOrganic chemistryDiseaseBiological activation
Owner:SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI +1
Thieno-pyridine derivatives as allosteric enhancers of the GABAB receptors
InactiveUS7390903B2Organic active ingredientsNervous disorderThienopyridine DerivativesMuscular spasticity
The present invention relates to compounds of formula Iwherein R1, R2, R3, R4, and R5 are as defined in the specification. Compounds of the invention are active on the GABAB receptor and are useful for treating a variety of CNS disorders, including anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity-and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, psychosis, panic disorder, posttraumatic stress disorders and gastro-intestinal disorders.
Owner:F HOFFMANN LA ROCHE & CO AG
2-phenyl-3,3,3-trifluoro-2-hydroxy-propionic acid derivatives
The present invention relates to compounds of formula I:wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification and claims, which compounds are active on the GABAB receptor and are useful in the control or prevention of CNS illnesses, especially of illnesses and disorders comprising anxiety, depression, epilepsy, schizophrenia, and cognitive disorders.
Owner:F HOFFMANN LA ROCHE & CO AG
Use of chemical compound medicament for curing alcohol dependence
InactiveCN101559054BPlay a therapeutic effectLittle side effectsOrganic active ingredientsNervous disorderSide effectAbstinence
The invention relates to a chemical compound medicament for curing alcohol dependence. The chemical compound medicament is characterized by containing GABAB receptor stimulating agent baclofen bulk medicament, M receptor antagonist paralest bulk medicament and auxiliary material. The material comprises the following effective components by the weight percent: 0.3-15 of baclofen, 0.05-5 of paralest and 80-99.65 of auxiliary material. Taballa or medicament in other forms is prepared by regular methods. The chemical compound medicament has remarkable curative effect and little side effect in the aspects of abstinence, rehabilitation and relapse resistance for alcohol reliers.
Owner:袁才蔚
3-methanesulfonylquinolines as GABAB enhancers
Owner:F HOFFMANN LA ROCHE INC
Sulfur-containing bicyclic compounds
The present invention provides a compound useful as a pharmaceutical composition for the prevention and / or treatment of schizophrenia and the like. The inventors of the present invention have conducted studies on pharmaceutical compositions for the prevention and / or treatment of schizophrenia, etc., which have a positive allosteric modulation effect (PAM effect) of GABAB, and confirmed that the sulfur-containing bicyclic compound is a PAM of the GABAB receptor, The present invention has thus been accomplished. The sulfur-containing bicyclic compound of the present invention has the PAM action of GABAB, and can be used as a preventive and / or therapeutic agent for schizophrenia and the like. (In the formula, X is CH, R1 is a lower alkyl group, R2 is a lower alkyl group, R3 is -H, R4 is -H, the A ring is a cyclohexane ring, and RY is a group shown in formula (III), Y is NH etc., RL is lower alkyl.)
Owner:ASTELLAS PHARMA INC
Application of GABAB receptor antagonist in aspect of blocking TREK-1 channel
InactiveCN109125331ARelieve depression-like symptomsWorsening of depression-like symptomsOrganic active ingredientsNervous disorderDiseaseNK1 receptor antagonist
The invention belongs to the technical field of biological medicines, and particularly relates to an application of a GABAB receptor antagonist in an aspect of blocking a TREK-1 channel. It is indicated from research in an embodiment of the application that the GABAB receptor antagonist acts on the TREK-1 channel and has the anti-depression effect, it has important theoretical significance and anapplication value to reveal a pathogenesis of depression and guide clinical compatibility of drugs. So, the GABAB receptor antagonist has good application prospect in aspects of preparing an antidepressant drug and a biliary tract obstruction drug, and preparing drugs for treating TREK-1 channel related diseases.
Owner:THE SECOND HOSPITAL OF DALIAN MEDICAL UNIV
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