45 results about "GABA B Agonists" patented technology

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.

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.

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.

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.

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.

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.

The present invention provides methods and compositions for improving cognitive function by administering a GABAB receptor antagonist and an acetylcholinesterase inhibitor.

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).

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.

Disclosed is a novel anti-obesity agent. Also disclosed is a therapeutic method using the anti-obesity agent. The anti-obesity agent comprises a GABAB receptor agonist or a pharmacologically acceptable salt thereof as an active ingredient.

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.

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.

The present invention relates to compounds of formula I wherein R1 to R6 are as described herein, which compounds are active at the GABAB receptor and can be used for the preparation of medicaments useful in the treatment of CNS disorders comprising anxiety and depression.

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.

The present invention provides methods of stimulating tissue growth, including islet cell growth, by administering GABA or a GABA agonist to act on GABAB receptors and GABAB-like receptors to activate cell replication.

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.

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.

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.

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.

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.

The present invention relates to novel compounds of Formula (I), wherein P, Q, A, B, m, n, R1, Z, J and L are defined as in Formula (I); which are gamma-(y)-aminobutyric acid type B receptor ("GABAB-R") positive allosteric modulators which are useful for the treatment or prevention of neurological and psychiatric disorders associated with GABA dysfunction and diseases in which the GABAB receptor is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes of preparing such compounds and such compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which GABAB-R is involved.

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.

The invention discloses application of baclofen in preparation of a medicine for treating glioma, and belongs to the technical field of biological medicine. Through systematic in-vitro and in-vivo experiments, it is proved for the first time that baclofen (especially R-configuration) has a remarkable anti-tumor effect on glioma including temozolomide (TMZ) drug resistance. The invention not only provides a brand-new clinical strategy for treating TMZ drug-resistant glioma, but also shows important value in the field of scientific research: baclofen can be used as a valuable tool compound and is used for exploring a new function of a GABAB receptor signal channel in glioma progress and drug resistance; meanwhile, a key tool is provided for constructing a stable TMZ drug-resistant model, the high-throughput drug screening and evaluation efficiency can be remarkably improved, and the TMZ drug-resistant monoclonal antibody can serve as a positive control drug to accelerate the conversion process from basic research of glioma to clinical application and has wide scientific research application prospects and conversion potential.

The present invention relates to the field of pharmaceutical chemistry. In particular, the present invention relates to a γ-aminobutyric acid type-B receptor (Gamma Aminobutyric Acid B Receptor, referred to as a GABABR or GABAB receptor for short) ligand molecule and a medicinal use thereof, wherein the ligand molecule has the structure of formula I. The ligand molecule which the present invention relates to is a GABAB receptor negative allosteric modulator, can non-competitively inhibit GABAB receptor agonist-induced activation of the receptor, and can be used to prepare drugs for the treatment of GABAB receptor hyperexcitability-related diseases, wherein the diseases comprise epilepsy, anxiety, depression or low cognitive ability caused by nerve damage, and so on.

The present invention relates to novel compounds of Formula (I), (I), wherein P, Q, A, B, m, n, R1 and R2 are defined as in Formula (I); which are gamma-aminobutyric acid type B receptor ("GABAB-R") positive allosteric modulators which are useful for the treatment or prevention of neurological and psychiatric disorders associated with GABA dysfunction and diseases in which the GABAB receptor is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes of preparing such compounds and such compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which GABAB-R is involved.

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.

The present invention relates to novel compounds of Formula (I), wherein Z, P, Q, A, B, m, n, R1 and R2 are defined as in Formula (I); which are gamma-(γ)-aminobutyric acid type B receptor ("GABAB-R") positive allosteric modulators which are useful for the treatment or prevention of central and peripheral nervous system disorders associated with GABA dysfunction and diseases in which the GABAB receptor is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes of preparing such compounds and such compositions, and to the use of such compounds for the prevention or treatment of disorders and diseases in which GABAB-R is involved.

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.