37 results about "GABA B Agonists" patented technology

The present invention provides novel compounds of formula I wherein W1, W2, W3, W4, W5, B, X1, X2, X3, X4, X5, E and L are as defined herein; invention compounds are gamma amino butyrique acid receptor-subtype B (“GABAB”) positive allosteric modulators (enhancers), which are useful to provide methods of treating or preventing diseases or disorders, including 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, panic disorder, posttraumatic stress disorders, urge urinary incontinence, gastroesophageal reflux disease, transient lower oesophageal sphincter relaxations, functional gastrointestinal disorders and irritable bowel syndrome.

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 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 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 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.

The present invention relates to compounds of formula Iwherein R1, R2 and R3 are as defined in the specification, which are active at the GABAB receptor and which can be used for the treatment of CNS disorders.