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. |
Click to Show More |
[1] |
2
|
D0WE5J
|
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] |
6
|
D0VE8R
|
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) |
D0U6OY |
Drug Info
|
Ki = 4 nM |
Click to Show More |
[1] |
2
|
D0LV1G
|
Drug Info
|
Ki = 27 nM
|
[1] |
3
|
D0VC0P
|
Drug Info
|
Ki = 71 nM
|
[1] |
4
|
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
|
D0W3TS
|
Drug Info
|
Ki = 190 nM
|
[1] |
5
|
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 |
Representative Drug(s) |
D0X9RA |
Drug Info
|
Ki = 140 nM |
[2] |
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] |
4
|
D0Y2NR
|
Drug Info
|
N.A.
|
[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] |
3
|
D0V4KJ
|
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] |
3
|
D0V4KJ
|
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] |
3
|
D0V4KJ
|
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] |
3
|
D0V4KJ
|
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] |