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 T45674 Target Info
Target Name Sigma intracellular receptor 2 (TMEM97)
Synonyms Transmembrane protein 97; Sigma2 receptor; Sigma-2 receptor; Meningioma-associated protein 30; MAC30
Target Type Clinical trial Target
Gene Name TMEM97
Biochemical Class TMEM97/sigma-2 receptor
UniProt ID
SGMR2_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2015116923
Title Isoindoline Compositions and Methods for Treating Neurodegenerative Disease.
Abstract Isoindoline sigma-2 receptor antagonist compounds, pharmaceutical compositions comprising such compounds, and methods for inhibiting Abeta- associated synapse loss or synaptic dysfunction in neuronal cells, modulating an Abeta-associated membrane trafficking change in neuronal cells, and treating cognitive decline associated with Abeta pathology are provided.
Applicant(s) Cognition Therapeutics, Inc
Representative Drug(s) D0F8XU Drug Info Ki = 0.44 nM Click to Show More [1]
2 D0EK3Z Drug Info Ki = 0.53 nM [1]
3 D06FNA Drug Info Ki = 1.8 nM [1]
4 D0S3ON Drug Info Ki = 2.6 nM [1]
5 D02NPB Drug Info Ki = 8.1 nM [1]
Patent ID WO2017190109
Title Sigma Receptor Binders.
Abstract Provided herein, inter alia, are compounds and methods of treating diseases including cancer, neurological disease, alcohol withdrawal, depression and anxiety, and neuropathic pain.
Applicant(s) Board of Regents, the University of Texas System
Representative Drug(s) D0R1QI Drug Info N.A. [1]
Patent ID WO2017190107
Title Sigma Receptor Binders.
Abstract Provided herein, inter alia, are compounds and methods of treating diseases including cancer, neurological disease, alcohol withdrawal, depression and anxiety, traumatic brain injury, and neuropathic pain.
Applicant(s) Board of Regents, the University of Texas System
Representative Drug(s) D0K7CD Drug Info Ki = 13 nM Click to Show More [1]
2 D0OZ1P Drug Info Ki = 26 nM [1]
3 D0CK6M Drug Info N.A. [1]
4 D0HY9M Drug Info N.A. [1]
5 D0LN2J Drug Info N.A. [1]
Patent ID WO2017070229
Title Piperazinyl Norbenzomorphan Compounds and Methods for Using The Same.
Abstract Disclosed herein, inter alia, are piperazinyl norbenzom orphan compounds and uses thereof, including, for example, methods for treating a CNS disease, treating traumatic brain injury, improving cognition, or diagnosing and treating cancer.
Applicant(s) Board of Regents, the University of Texas System
Representative Drug(s) D0LV1G Drug Info Ki = 27 nM Click to Show More [1]
2 D04BSD Drug Info N.A. [1]
Patent ID WO2015193255
Title Compounds, Pharmaceutical Composition and Their Use In Treating Neurodegenerative Diseases.
Abstract The present invention is directed to novel compounds of Formula (I), pharmaceutically acceptable salts or solvates thereof, and their use.
Applicant(s) Center Hospitalier Regional et Universitaire De Lille (Chru)
Representative Drug(s) D05YFF Drug Info Ki = 20 nM Click to Show More [1]
2 D0H2SE Drug Info Ki = 48 nM [1]
3 D03MKY Drug Info Ki = 59 nM [1]
4 D0RS2J Drug Info N.A. [1]
Patent ID WO2015134545
Title Highly Selective Sigma Receptor Ligands and Radioligands As Probes In Nociceptive Processing and The Pathphysiological Study of Memory Deficits and Conitive Disorders.
Abstract A method for localizing and quantifying SIR role in nociceptive processing; for providing a guide to providing an analgesic therapy; of using an SIR selective ligand as a biomarker for pathphysiological study of memory deficits and cognitive disorders; or of detecting increased SIR density at the site of nerve injury arising from neuropathic pain comprising using as a probe at least one SRI selective compound or radioligand of the general formula III', or IV' :.
Applicant(s) The University of Mississippi
Representative Drug(s) D0DZ5H Drug Info Ki = 0.39 nM Click to Show More [1]
2 D0M5LL Drug Info Ki = 0.55 nM [1]
3 D0LP3P Drug Info Ki = 6 nM [1]
4 D0DW1D Drug Info Ki = 360 nM [1]
5 D02ZGY Drug Info N.A. [1]
Patent ID WO2013029057
Title Compositions and Methods for Treating Neurodegenerative Disease.
Abstract This invention relates to novel diarylamino compounds that bind to the sigma-2 receptor, to pharmaceutical compositions comprising such compounds, and to methods for inhibiting or restoring synapse loss in neuronal cells, modulating a membrane trafficking change in neuronal cells, and treating cognitive decline and neurodegenerative diseases and disorders therewith.
Applicant(s) Cognition Therapeutics, Inc
Representative Drug(s) D0SG9W Drug Info Ki = 60 nM Click to Show More [1]
2 D0N5JQ Drug Info N.A. [1]
Patent ID WO2016178852
Title 211-Astatine Containing Radiotherapeutics for The Treatment of Cancer.
Abstract Described herein is an alpha-emitting radionuclide, 211At, which has been incorporated into a selective sigma-2 ligand moiety to provide cytotoxic capabilities to a chemical compound. As described herein, a compound of formula (I), wherein R1-R4, m, and n are defined herein, was prepared and utilized in in vitro and in vivo tumor targeting of alpha-emitting sigma-2 ligand in a breast cancer model. In one embodiment, the compound is 5-(211At)-N-(4-(6,7-dimethoxy-3,4- dihydroisoquinolin-2(lH)-yl)butyl)-2,3-dimethoxybenzamide.
Applicant(s) The Trustes of the University of Pennsylvania
Representative Drug(s) D05MST Drug Info N.A. Click to Show More [1]
2 D0A1DV Drug Info N.A. [1]
Patent ID WO2015153814
Title Sigma-2 Receptor Ligand Drug Conjugates As Antitumor Compounds, Methods of Synthesis and Uses Thereof.
Abstract Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described. At least one described molecular species exhibits an IC50 value below 5 against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo, and led to 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.
Applicant(s) Washington University
Representative Drug(s) D01IVR Drug Info N.A. Click to Show More [2]
2 D04WKL Drug Info N.A. [2]
3 D06HRI Drug Info N.A. [2]
4 D0AT9E Drug Info N.A. [2]
5 D0BI1O Drug Info N.A. [2]
Patent ID WO200230422
Title Use of Defined Substances That Bind To The Sigma Receptor for Combating Sarcoma and Carcinoma.
Applicant(s) Merk Patent Gmbh
Representative Drug(s) D0J9SL Drug Info N.A. Click to Show More [2]
2 D0T5SO Drug Info N.A. [2]
Patent ID WO199620928
Title Piperidine-Based Sigma Receptor Ligands.
Applicant(s) Australian Nuclear Science & Technology Organisation
Patent ID WO2010097641
Title Sigma Receptors Ligands with Anti-Apoptotic and/or Pro-Apoptotic Properties, Over Cellular Mechanisms, Exhibiting Prototypical Cytoprotective and Also Anticancer Activity.
Abstract The present invention involves new and original sigma receptors Iigands : (Mono-or dialkylaminoalkyl)- gama-butyrolactones, their analogues aminotetrahydroturanes, the (1-adamantyl) benzene alkylamines, the N,N Dialkyl alpha-[(adamantyl-1)benzyloxy-2] alkylamines and the 3-cyclopentyl adamantyl-amines or alkylamines or-alkyl phenylamines, their enantiomers or diastereoisomers, their pharmaceutically acceptable salts and Quinacrine Me-thylene blue, Astemizole and their relative analogues with pro-apoptotic and/or anti-apoptotic properties over cellular biochemical mechanisms, with prototypical anti-cancer, antimetastatic and antiviral activities associated with antagonism of the neuropatic pain and, at very low doses, with cytoprotectve and cytoregenerative activity against the cytodegenerative diseases.
Applicant(s) Vamvakides, Alexandre
Representative Drug(s) D0EO9Z Drug Info N.A. [2]
Patent ID WO2008087458
Title New Sigma-Receptor Ligands with Anti-Apoptotic and/or Pro-Apoptotic Properties Over Cellular Biochemical Mechanisms, with Neuroprotective, Anti-Cancer, Anti-Metastatic and Anti-(Chronic) Inflammatory Action.
Abstract The present invention involves new and original sigma receptors ligands : (Mono-or di-alkylaminoalkyl)- gama-butyrolactones, their analogues aminotetrahydrofuranes, the (1-adamantyl) phenyl(s) alkylamines, the N,N Dialkyl alpha-[(adamantyl-l)benzyloxy-2] alkylamines and the 3-cyclopentyl adamantyl-amines or alkylamines or-alkyl phenylamines, their enantiomers or diastereoisomers and their pharmaceutically acceptable salts, with pro-apoptotic and/or anti-apoptotic properties over cellular biochemical mechanisms, with anti-cancer, anti-metastatic, anti-(chronic) inflammatory, neuro-protective, anticonvulsive, antidepressive and nooanaleptic or sedative action.
Applicant(s) Vamvakides, Alexandre
Representative Drug(s) D0EO9Z Drug Info N.A. [2]
Patent ID WO9730983
Title Tetrahydro-N,N-Dimeti-Iyl-2,2-Diphenyl-3-Feranemetiianamine, Its Enantiomers, and Their Pharmaceutically Acceptable Acid Addition Salts.
Representative Drug(s) D0EO9Z Drug Info N.A. [2]
United States Patent and Trademark Office (USPTO)
Patent ID US20120190710
Title Bicyclo-Heptan-2-Amines.
Representative Drug(s) D0FU2M Drug Info Ki = 5.5 nM Click to Show More [2]
2 D04OPJ Drug Info Ki = 9.6 nM [2]
3 D0PF9X Drug Info Ki = 16 nM [2]
Patent ID US7893266
Title Detection of Cancer Cells In Vitro Using S2R Ligands As Radiotracers.
Applicant(s) Washington University
Representative Drug(s) D03DNE Drug Info N.A. Click to Show More [2]
2 D04PDM Drug Info N.A. [2]
3 D0E9CV Drug Info N.A. [2]
4 D0M4BI Drug Info N.A. [2]
Patent ID US8168650
Title Therapeutic Uses of Bicylic Ligands of Sigma2 Receptor.
Representative Drug(s) D0FH5K Drug Info N.A. Click to Show More [2]
2 D0N6JH Drug Info N.A. [2]
Patent ID US7612085
Title Sigma 2 Receptor Ligands and Therapeutic Uses Therefor.
Representative Drug(s) D0FH5K Drug Info N.A. Click to Show More [2]
2 D0N6JH Drug Info N.A. [2]
Patent ID US20100048614
Title Therapeutic Uses of Bicyclic Ligands of Sigma-2 Receptor.
Representative Drug(s) D0FH5K Drug Info N.A. Click to Show More [2]
2 D0N6JH Drug Info N.A. [2]
Patent ID US2008161343
Title Sigma 2 Receptor Ligands and Therapeutic Uses Therefor.
Representative Drug(s) D0FH5K Drug Info N.A. Click to Show More [2]
2 D0N6JH Drug Info N.A. [2]
Patent ID US20050107398
Title Sigma-2 Receptor Radiotracers for Imaging The Proliferative Status of Solid Tumors.
Representative Drug(s) D0E3OT Drug Info N.A. [1]
References  Top
REF 1 The sigma-2 (-2) receptor: a review of recent patent applications: 2013-2018.Expert Opin Ther Pat. 2018 Sep;28(9):655-663.
REF 2 Are sigma modulators an effective opportunity for cancer treatment A patent overview (1996-2016).Expert Opin Ther Pat. 2017 May;27(5):565-578.

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