36 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 (GABA_B) 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 (GABA_B) 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 (GABA_B) 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 GABA_B receptor antagonist and an acetylcholinesterase inhibitor.

The present invention relates to novel imidazole compounds having a positive allosteric GABA_B receptor (CUR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABA_B 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 GABA_B receptor subunit, HG20, as well as the protein encoded by the DNA, is provided. Also provided is DNA encoding a novel murine GABA_B receptor subunit, GABA_BR1a, as well as the protein encoded by the DNA. Heterodimers of HG20 protein and GABA_BR1a protein that form a functional GABA_B receptor are disclosed. Methods of identifying agonists and antagonists of the GABA_B 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 (GABA_B) 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; and

R, 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 GABA_B 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 GABA_B 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 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.

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 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 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.)