Target and Its Patented Drug(s)

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Target General Information
Patent(s) and the Corresponding Patented Drug(s)
References
Target General Information  Top
Target ID T69685 Target Info
Target Name Glycine transporter GlyT-1 (SLC6A9)
Synonyms Solute carrier family 6 member 9; Sodium- and chloride-dependent glycine transporter 1; Glycine type-1 transporter; Glycine transporter type 1; GlyT1; GlyT-1
Target Type Clinical trial Target
Gene Name SLC6A9
Biochemical Class Neurotransmitter:sodium symporter
UniProt ID
SC6A9_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2011161006
Title Amido-Tropane Derivatives.
Abstract The present invention relates to a compound of general formula (I) wherein R1, R2 and R3 are independently from each other hydrogen, lower alkyl, lower alkoxy, cycloalkyl, lower alkyl substituted by halogen or S-lower alkyl; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. It has been found that the compounds of general formula (I) are good inhibitors of the glycine transporter 1 (GlyT-1), and that they have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors. The compounds may be used in the treatment of neurological and neuropsychiatric disorders.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D08GXR Drug Info IC50 = 6 nM Click to Show More [1]
2 D02TZT Drug Info IC50 = 25 nM [1]
Patent ID WO2011153359
Title Glycine Transporter-1 Inhibitors, Methods of Making Them, and Uses Thereof.
Abstract The compounds of the present invention are represented by the following formula (I): wherein the substituents R1, R2, R3, R4, (R5)m, R6, A, X, and Y are as defined herein. The compounds are useful in methods of treating a disorder which is created by or is dependent upon inhibiting GlyT-1.
Applicant(s) Albany Molecular Research, Inc
Representative Drug(s) D0EF0P Drug Info IC50 = 0.67 nM Click to Show More [1]
2 D0W7FS Drug Info IC50 = 29 nM [1]
3 D0T2QP Drug Info N.A. [1]
Patent ID WO2013187503
Title Glycine Transporter Inhibitor.
Abstract The present invention provides a novel compound represented by formula (I) or a pharmaceutically acceptable salt thereof, which is useful for prophylaxis or treatment of diseases such as schizophrenia, Alzheimer's disease, cognitive impairment, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, a specific phobia, acute stress disorder and the like), depression, drug dependence, convulsion, tremor, pain, Parkinson's disease, attention deficit hyperactivity disorder, bipolar disorder, eating disorder and sleep disorder, on the basis of an inhibitory activity on glycine uptake.
Applicant(s) Taisho Pharma Co Ltd
Representative Drug(s) D0B5NJ Drug Info N.A. Click to Show More [1]
2 D0XS1I Drug Info N.A. [1]
Patent ID WO2016038160
Title 4,5-Dihydropyrazole Derivatives, Pharmaceutical Compositions Containing Them, and Their Use In Therapy.
Abstract The present invention relates to 4,5-dihydropyrazole derivatives of the formula (I) and physiologically tolerated salts thereof which are GlyTl inhibitors. The invention further relates to pharmaceutical compositions comprising such 4,5-dihydropyrazole derivatives, and the use of such 4,5-dihydropyrazole derivatives for therapeutic purposes.
Applicant(s) Abbvie Deutschland
Representative Drug(s) D07GSH Drug Info Kiapp <= 1000 nM [1]
Patent ID WO2015055770
Title Aminochromane, Aminothiochromane and Amino-1,2,3,4-Tetrahydroquinoline Derivatives, Pharmaceutical Compositions Containing Them, and Their Use In Therapy.
Abstract The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4- tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothio-chromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.
Applicant(s) Abbvie Deutschland
Representative Drug(s) D0FG2H Drug Info Kiapp <= 10 nM [1]
Patent ID WO2014199960
Title Glycine Transporter Inhibitor.
Abstract The present invention provides a novel compound represented by formula (IA) or a pharmaceutically acceptable salt thereof, which is useful for prophylaxis or treatment of diseases such as schizophrenia, Alzheimer's disease, cognitive impairment, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, a specific phobia, acute stress disorder and the like), depression, drug dependence, convulsion, tremor, pain, Parkinson's disease, attention deficit hyperactivity disorder, bipolar disorder, eating disorder and sleep disorder, on the basis of an inhibitory activity on glycine uptake.
Applicant(s) Taisho Pharmaceutical Co., Ltd
Representative Drug(s) D0EV6V Drug Info IC50 = 34 nM [1]
Patent ID WO2012152915
Title Benzazepine Derivatives, Pharmaceutical Compositions Containing Them, and Their Use In Therapy.
Abstract The present invention relates to benzazepine derivatives of the formula (I) or a physiologically tolerated salt thereof. The present invention also relates to pharmaceutical compositions comprising such benzazepine derivatives, and the use of such benzazepine derivatives for therapeutic purposes.
Applicant(s) Abbvie Deutschland
Representative Drug(s) D0H5VO Drug Info Kiapp <= 100 nM [1]
Patent ID WO2012020130
Title Phenalkylamine Derivatives, Pharmaceutical Compositions Containing Them, and Their Use In Therapy.
Abstract The present invention relates to phenalkylamine derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.
Applicant(s) Abbott
Representative Drug(s) D00JEC Drug Info Kiapp <= 100 nM [1]
Patent ID WO2011161008
Title Quinolizidine and Indolizidine Derivatives.
Abstract The present invention relates to a compound of general formula I-A or I-B wherein X is a bond or a CH2- group; R1, R2 and R3 are independently from each other hydrogen, lower alkoxy, lower alkyl substituted by halogen or S-lower alkyl; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. It has been found that the compounds of general formulas I-A and I-B are good inhibitors of the glycine transporter 1 (GlyT-1), and that they have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors, suitable in the treatment of neurological and neuropsychiatric disorders.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0K6CM Drug Info IC50 = 80 nM [1]
Patent ID WO2011095434
Title Tetrahydro-Pyran Derivatives Against Neurological Illnesses.
Abstract The present invention relates to a compound of general formula (I) wherein X is -O- or -CH2-; X' is -O- or -CH2-; with the proviso that one of X or X' is always -O- and the other is -CH2-. It has been found that the compounds of general formula (I) are good inhibitors of the glycine transporter 1 (GIyT-1) and therefore they may be used for the treatment of schizophrenia, psychoses and other neurological conditions, including pain.
Applicant(s) F. Hoffmann-La Roche Ag
Representative Drug(s) D0Y9FA Drug Info IC50 = 7.6 nM [1]
Patent ID WO2011007899
Title Glycine Transporter Inhibitors.
Abstract The present invention aims to provide novel compounds represented by formula [I] or pharmaceutically acceptable salts thereof: [Formula 1] which are useful for prevention or treatment of diseases such as schizophrenia, Alzheimer's disease, cognitive impairment, dementia, anxiety disorders (e.g., generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, acute stress disorder), depression, drug dependence, convulsion, tremor, pain, or sleep disorders, based on their inhibitory effect against glycine uptake.
Applicant(s) Taisho Pharmaceutical Co., Ltd
Representative Drug(s) D0T1BE Drug Info IC50 = 7.3 nM [1]
Patent ID WO2010092181
Title Heterocyclic Compounds, Pharmaceutical Compositions Containing Them, and Their Use As Inhibitors of The Glycine Transporter 1.
Abstract The present invention relates to heterocyclic compounds of the formula (I) or a physiologically tolerated salt thereof. The present invention also relates to pharmaceutical compositions comprising such heterocyclic compounds, and the use of such heterocyclic compounds for the manufacture of a medicament for inhibiting the glycine transporter GIyT1.
Applicant(s) Abbott
Representative Drug(s) D0X1ZA Drug Info Kiapp <= 1000 nM [1]
Patent ID WO2011023367
Title Carbocyclic Glyt1 Receptor Antagonists.
Representative Drug(s) D0S6BG Drug Info IC50 = 35 nM [1]
Patent ID WO2016073420
Title Substituted Azetidinyl Compounds As Glyt1 Inhibitors.
Abstract The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, X, and Y have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; modulating and treating disorders mediated by GlyTl activity; treating neurological disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma-dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training, including animal skill training; and treating other disorders, including pain and alcohol-dependence.
Applicant(s) Dart Neuroscience (Cayman) Ltd
Representative Drug(s) D03PQS Drug Info N.A. [1]
Patent ID WO2015164520
Title Substituted 2,4,5,6-Tetrahydropyrrolo[3,4-C] Pyrazole and 4,5,6,7-Tetrahydro-2H-Pyrazolo [4,3-C] Pyridine Compounds As Glyt1 Inhibitors.
Abstract The invention provides a chemical entity of Formula (I), wherein R1, R2, R3, R4, R5 and X have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; modulating and treating disorders mediated by GlyT1 activity; treating neurological disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma-dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training, including animal skill training; and treating other disorders, including pain and alcohol-dependence.
Applicant(s) Dart Neuroscience (Cayman) Ltd
Representative Drug(s) D0WT3F Drug Info N.A. [1]
Patent ID WO2013120835
Title Isoindoline Derivatives, Pharmaceutical Compositions Containing Them, and Their Use In Therapy.
Abstract The present invention relates to isoindoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The present invention also relates to pharmaceutical compositions comprising such isoindoline derivatives, and the use of such isoindoline derivatives for therapeutic purposes.
Applicant(s) Abbvie Deutschland
Representative Drug(s) D08UQK Drug Info N.A. [1]
Patent ID WO2013017657
Title Phenyl-3-Aza-Bicyclo[3.1.0]Hex-3-Yl-Methanones and The Use Thereof As Medicament.
Abstract The present inventions relates to substituted phenyl-3-aza-bicyclo[3.1.0]hex-3-yl- methanones of general formula (I) wherein R1, R2, R3, R4, R5 and R6 are as herein described or salts thereof, preferably pharmaceutically acceptable salts thereof. The invention further relates to the manufacture of said compounds, pharmaceutical compositions comprising a compound according to general formula (I), and the use of said compounds for the treatment of various conditions such as conditions concerning positive and negative symptoms of schizophrenia as well as cognitive impairments associated with schizophrenia, Alzheimers Disease and other neurological and psychiatric disorders. The compounds of the invention show glycine transporter-1 (GlyT1) inhibiting properties.
Applicant(s) Boehringer Ingelheim International Gmbh
Representative Drug(s) D0E2VI Drug Info N.A. [1]
Patent ID WO2012081665
Title Substance Capable of Inhibiting Glycine Transporter.
Abstract The present invention relates to a novel compound represented by formula [I] or a pharmaceutically acceptable salt thereof. This compound is useful for the prevention or treatment of diseases such as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, a specific phobia, acute stress disorder, and the like), depression, drug dependence, convulsion, tremor, pain, Parkinson's disease, attention deficit/hyperactivity disorder, bipolar disorder, eating disorder, sleep disorder and the like, of which the action relies on an inhibitory activity on the intake of glycine.
Applicant(s) Taisho Pharma Co Ltd
Representative Drug(s) D0V5KY Drug Info N.A. [1]
Patent ID WO2011023753
Title Benzoxazine Derivatives As Glycine Transport Inhibitors.
Abstract The present invention relates to benzoxazinone derivatives, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in treating disorders mediated by Gly T1, including neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder.
Applicant(s) Glaxo Group Limited
Representative Drug(s) D0MT4C Drug Info N.A. [1]
Patent ID WO2010107115
Title Glycine Transporter Inhibitor.
Abstract Provided is a novel compound or a pharmaceutically acceptable salt thereof, which is useful for preventing or treating diseases attributed to glycine uptake inhibitory activity such as schizophrenia, Alzheimer's disease, cognitive impairment, dementia, anxiety disorders (such as generalized anxiety disorders, panic disorders, obsessive-compulsive disorders, social anxiety disorders, post-traumatic stress disorders, specific phobia, and acute stress disorders), depression, drug dependence, convulsion, tremor, and sleep disorders. The compound is represented by formula [I].
Applicant(s) Taisho Pharmaceutical Co., Ltd
Representative Drug(s) D0GX8J Drug Info N.A. [1]
Patent ID WO2006067423
Title Glycine Transport Inhibitors.
Abstract The present invention relates to compounds of formula (I), or to salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.
Applicant(s) Glaxo Group Limited
Representative Drug(s) D0H2KL Drug Info N.A. [1]
Patent ID WO2015021400
Title Glycine Transporter-1 Inhibitors.
Representative Drug(s) D0XG8H Drug Info N.A. [1]
Patent ID WO2006067414
Title Compounds.
Representative Drug(s) D0I7AJ Drug Info N.A. [1]
United States Patent and Trademark Office (USPTO)
Patent ID US20140275087
Title Pyrrolidine Derivatives, Pharmaceutical Compositions Containing Them, and Their Use In Therapy.
Representative Drug(s) D0H5WE Drug Info Kiapp <= 1 nM [1]
Patent ID US20120295881
Title Tetraline and Indane Derivatives, Pharmaceutical Compositions Containing Them, and Their Use In Therapy.
Representative Drug(s) D01IJO Drug Info Kiapp <= 100 nM [1]
Patent ID US20110009440
Title Glyt1 Transporter Inhibitors and Uses Thereof In Treatment of Neurological and Neuropsychiatric Disorders.
Representative Drug(s) D0M6PI Drug Info N.A. [1]
China National Intellectual Property Administration (CNIPA)
Patent ID CN105712952
Title Glyt-1 Inhibitors.
Representative Drug(s) D06BUG Drug Info N.A. [1]
Patent ID CN105712945
Title Glyt-1 Inhibitors.
Representative Drug(s) D06OSE Drug Info N.A. [1]
Patent ID CN105712928
Title Glyt-1 Inhibitors.
Representative Drug(s) D0W2YK Drug Info N.A. [1]
References  Top
REF 1 Glycine transporter-1 inhibitors: a patent review (2011-2016).Expert Opin Ther Pat. 2018 Mar;28(3):197-210.

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