42 results about "Glycine transporter" patented technology

This invention provides isolated nucleic acid molecules encoding a mammalian glycine transporter, isolated nucleic acid molecules encoding a human glycine transporter, isolated proteins which are mammalian glycine transporter proteins, isolated proteins which are human glycine transporter proteins, vectors comprising isolated nucleic acid molecules encoding a mammalian or a human glycine transporter, mammalian cells comprising such vectors, antibodies directed to a mammamlian glycine transporter, antibodies directed to a human glycine transporter, nucleic acid probes useful for detecting nucleic acid encoding mammalian glycine transporter, nucleic acid probes useful for detecting nucleic acid encoding human glycine transporter, antisense oligonucleotides complementary to any sequences of a nucleic acid molecule which encodes a mammalian glycine transporter, antisense oligonucleotides complementary to any sequences of a nucleic said molecule which encodes a human glycine transporter, pharmaceutical compounds related to mammalian glycine transporter and nonhuman transporter, pharmaceutical compounds related to human glycine transporter and nonhuman transgenic animals which express DNA encoding a normal or a mutant mammalian or human glycine transorter. This invention also provides methods for determining ligand binding, detecting expression, drug screening, and treatments for alleviating abnormalities associated with mammalian glycine transporter. This invention further provides methods for determining ligand binding, detecting expression, drug screening, and treatments for alleviating abnormalities associated with human glycine transporter.

The invention relates to a triazole derivative with an activity inhibiting glycine transporter and for use as a pharmaceutical drug, and a novel triazole derivative. The inventive triazole derivative has an excellent activity inhibiting glycine transporter and is useful as a therapeutic agent of dementia, schizophrenia, cognitive disorders, or cognitive disorders involved in various diseases such as Alzheimer disease, Parkinson's disease, or Huntington disease or the like, or spasm involved in diseases such as nerve degenerative diseases and cerebrovascular disorders, or the like. Particularly, the pharmaceutical drug is useful for the amelioration of learning disability of dementia and the like.

The present invention is directed to compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.

The present invention is directed to pyridyl, pyridazinyl, pyrimidinyl and pyrazinyl piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.

The present invention relates to a pharmaceutical combination of a glycine transporter inhibitor (GlyT1) and an atypical antipsychotic drug which may be used for the treatment of positive and negative symptoms of schizophrenia.

Disclosed are a combination of active components inducing synergistic effects of multi-targeting and a use thereof. More particularly, disclosed are a functional food composition, a cosmetic composition, a pain-suppressive composition, and a composition for treatment or prevention of pruritus or atopic dermatitis, which comprise as active components, two or more components selected from a group consisting of (a) a 5-hydroxytryptamine subtype 2 (5-HT2) receptor antagonist; (b) a P2X receptor antagonist; and (c) any one of a glycine receptor agonist, a glycine transporter (GlyT) antagonist, a gamma-aminobutyric acid (GABA) receptor agonist, and a GABA transporter 1 (GAT1) antagonist. The multi-targeting composite composition (specifically, natural substances composite composition) has synergistic effects, and thus a treatment using a combination of respective components may achieve increased biological effects, in which mechanisms targeted by respective components are involved. Thus, the multi-targeting composite composition may not only remarkably control pain but may also increase effects of: alleviating symptoms of skin diseases such as itching and atopic dermatitis; preventing or improving depression, refreshment, pore minimization, improving wrinkles, skin regeneration, skin health, recovery of skin condition, skin whitening, preventing or improving athlete's foot, recovery of scalp health and regeneration of scalp, promoting hair growth, preventing gray hair, and improving dental and periodontal diseases, etc.

The present invention is directed to morpholinyl piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.

The present invention is directed to azetidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.

The present invention is directed to cyclopropyl piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neuro-transmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.

Chronic pain is treated in an individual suffering from chronic pain by administering to the individual an amount of a therapeutic containing a glycine receptor agonist such as D-cycloserine or a GlyT-1 glycine transporter antagonist such as sarcosine in an amount effective to treat the chronic pain. The therapeutic may also contain a secondary analgesic such as opiates, NSAIDs or cox-2 inhibitors. The analgesic can be formulated in a pharmaceutical composition in the form of an injectable solution that contains at least two different analgesics, at least one of the analgesics of which is a glycine receptor agonist or a GlyT-1 glycine transporter antagonist. Suitable pharmaceutical compositions contain D-cycloserine and / or sarcosine, optionally in combination with opiates, NSAIDs or cox-2 inhibitors.

The present invention is directed to radiolabeled glycine transporter inhibitors which are useful for the labeling and diagnostic imaging of glycine transporters in mammals.

The invention relates to a triazole derivative with an activity inhibiting glycine transporter and for use as a pharmaceutical drug, and a novel triazole derivative. The inventive triazole derivative has an excellent activity inhibiting glycine transporter and is useful as a therapeutic agent of dementia, schizophrenia, cognitive disorders, or cognitive disorders involved in various diseases such as Alzheimer disease, Parkinson's disease, or Huntington disease or the like, or spasm involved in diseases such as nerve degenerative diseases and cerebrovascular disorders, or the like. Particularly, the pharmaceutical drug is useful for the amelioration of learning disability of dementia and the like.

The present invention is directed to pyridyl, pyridazinyl, pyrimidinyl and pyrazinyl piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.

The present invention relates to a series of substituted bicyclic[3.1.0]amines of the Formula I: wherein A, B, D, Q, V, W, X, Y, Z, R2, R3, R4, R5, R14, R15, R30. o, p, s,t and q are as defined in the specification, their pharmaceutically acceptable salts, pharmaceutical compositions thereof, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.

Disclosed are a combination of active components inducing synergistic effects of multi-targeting and a use thereof. More particularly, disclosed are a functional food composition, a cosmetic composition, a pain-suppressive composition, and a composition for treatment or prevention of pruritus or atopic dermatitis, which comprise as active components, two or more components selected from a group consisting of (a) a 5-hydroxytryptamine subtype 2 (5-HT2) receptor antagonist; (b) a P2X receptor antagonist; and (c) any one of a glycine receptor agonist, a glycine transporter (GlyT) antagonist, a gamma-aminobutyric acid (GABA) receptor agonist, and a GABA transporter 1 (GAT1) antagonist.

The present invention relates to a method of treating schizophrenia prodrome in human subjects using a NMDA glycine site agonist, a glycine transporter-1 inhibitor or mixtures thereof, optionally in combination with a pharmaceutically acceptable additive, carrier or excipient.

The invention discloses 2-substituted-oxy-5-methylsulfonyl aryl piperazine acidamide analogue and a preparation method and application thereof, and particularly, relates to 2-substituted-oxy-5-methylsulfonyl aryl piperazine acidamide analogue with a formula (I) compound and a preparation method and application thereof, wherein substitutions in the formula (I) compound are defined as in the description. This serial compound can inhibit the activity of glycine transport protein-1 (GlyT1), is useful in treating related diseases in central nerve and psychological fields, for example, schizophrenia (including positive symptoms, negative symptoms and cognitive symptoms), senile dementia, Parkinson's disease and other related psychological diseases, is widely applicable to the drugs for preventing and treating central nerve and psychological diseases, and is expected to be developed into new-generation GlyT1 inhibitors.

The present invention is directed to cyclopropyl piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neuro-transmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.

The present invention relates to a series of substituted bicyclic[3.1.0]amines of the Formula I:wherein A, B, D, Q, V, W, X, Y, Z, R2, R3, R4, R5, R14, R15, R30. o, p, s,t and q are as defined in the specification, their pharmaceutically acceptable salts, pharmaceutical compositions thereof, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.

The invention relates to a triazole derivative with an activity inhibiting glycine transporter and for use as a pharmaceutical drug, and a novel triazole derivative. The inventive triazole derivative has an excellent activity inhibiting glycine transporter and is useful as a therapeutic agent of dementia, schizophrenia, cognitive disorders, or cognitive disorders involved in various diseases such as Alzheimer disease, Parkinson's disease, or Huntington disease or the like, or spasm involved in diseases such as nerve degenerative diseases and cerebrovascular disorders, or the like. Particularly, the pharmaceutical drug is useful for the amelioration of learning disability of dementia and the like.

The present invention provides trichloroethyl-sulfonylurea-containing compounds that inhibit glycing transporters, pharmaceutical compositions comprising such compounds, methods for using such compounds for inhibiting glycine transporters and methods for using such compounds for the treatment of disease states in which glycine is involved.

Chronic pain is treated in an individual suffering from chronic pain by administering to the individual an amount of a therapeutic containing a glycine receptor agonist such as D-cycloserine or a GlyT-1 glycine transporter antagonist such as sarcosine in an amount effective to treat the chronic pain. The therapeutic may also contain a secondary analgesic such as opiates, NSAIDs or cox-2 inhibitors. The analgesic can be formulated in a pharmaceutical composition in the form of an injectable solution that contains at least two different analgesics, at least one of the analgesics of which is a glycine receptor agonist or a GlyT-1 glycine transporter antagonist. Suitable pharmaceutical compositions contain D-cycloserine and / or sarcosine, optionally in combination with opiates, NSAIDs or cox-2 inhibitors.

The present invention relates to a method of treating schizophrenia prodrome in human subjects using a NMDA glycine site agonist, a glycine transporter-1 inhibitor or mixtures thereof, optionally in combination with a pharmaceutically acceptable additive, carrier or excipient.

Substituted phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones which are glycine transporter-1 (GlyT1) inhibitors. These are useful for the treatment of schizophrenia, Alzheimer's Disease and other neurological and psychiatric disorders.

Substituted phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones which are glycine transporter-1 (GlyT1) inhibitors. These are useful for the treatment of schizophrenia, Alzheimer's Disease and other neurological and psychiatric disorders.

The present invention relates to compounds useful as inhibitors of type 1 glycine transporter (GlyT1) activity; synthetic methods for preparing said compounds; pharmaceutical compositions comprising said compounds; and the use of said compounds and compositions for the treatment of patients with type 1 A method for disorders related to glycine transporter (GlyT1) activity.

The invention discloses a new compound with inhibiting the activity to glycine transporters, which is shown in a formula (I). The compound can be used for treating mental disorders associated with NMDA glycine receptors. The invention also discloses a preparation method of the compound shown in the formula (I), a pharmaceutical composition taking the compound as an active ingredient, and the application of the compound in preparation of drugs for treating mental disorders reacting with NMDA glycine receptors.

The present invention is directed to radiolabeled glycine transporter inhibitors which are useful for the labeling and diagnostic imaging of glycine transporters in mammals.

The present invention is directed to azetidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.