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 T60857 Target Info
Target Name Dihydrodiol dehydrogenase type I (AKR1C3)
Synonyms Trans-1,2-dihydrobenzene-1,2-diol dehydrogenase; Testosterone 17-beta-dehydrogenase 5; Prostaglandin F synthase; PGFS; KIAA0119; Indanol dehydrogenase; HSD17B5; HA1753; Dihydrodiol dehydrogenase 3; DDH1; DD3; DD-3; Chlordecone reductase homolog HAKRb; Aldo-keto reductase family 1 member C3; 3-alpha-hydroxysteroid dehydrogenase type 2; 3-alpha-HSD type II, brain; 3-alpha-HSD type 2; 17-beta-hydroxysteroid dehydrogenase type 5; 17-beta-HSD 5
Target Type Successful Target
Gene Name AKR1C3
Biochemical Class Short-chain dehydrogenases reductase
UniProt ID
AK1C3_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2015065919
Title Treatment of Metastatic Prostate Cancer.
Abstract The present invention provides new compositions and methods for treating prostate cancer, e.g., drug-resistant prostate cancer, such as anti-androgen drug (e.g., enzalutamide) resistant and/or castration resistant prostate cancer (CRPC). These new compositions include, but are not limited to, pharmaceutical compositions that include an AR-V7 inhibitor, such as niclosamide. Alternatively, these new compositions can include, but are not limited to, pharmaceutical compositions that include an AKR1C3 inhibitor, such as indomethacin. These new methods include, but are not limited to, methods of administering an AR-V7 inhibitor, such as niclosamide, and/or an AKR1C3 inhibitor, such as indomethacin, to treat patients having prostate cancer. The present invention also provides methods of inhibiting androgen receptor variant expression, e.g. AR-V7, and methods of killing cells expressing AR-V7. The present invention further provides methods of inhibiting AKR1C3 expression or activity, and methods of killing cells that express AKR1C3.
Applicant(s) The Regents of the University of California
Representative Drug(s) D0E2TY Drug Info IC50 = 90 nM Click to Show More [1]
2 D0F0PK Drug Info IC50 = 90 nM [1]
3 D0GY2Z Drug Info IC50 = 90 nM [1]
Patent ID WO2013059245
Title Indomethacin Analogs for The Treatment of Castrate-Resistant Prostate Cancer.
Abstract Provided are compositions for inhibiting a biological activity of an aldoketo reductase family 1, member C3 (AKR1 C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1 C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects.
Applicant(s) Vanderbilt University the Trustes of the University of Pennsylvania
Representative Drug(s) D0E2TY Drug Info IC50 = 90 nM Click to Show More [1]
2 D0F0PK Drug Info IC50 = 90 nM [1]
3 D0GY2Z Drug Info IC50 = 90 nM [1]
Patent ID WO2010087319
Title Method for Screening Substance Useful As Therapeutic Agent for Prostate Cancer.
Abstract Disclosed is a method for screening a compound that is useful as a therapeutic agent for diseases associated with 17HSD type-5 and/or a therapeutic agent for cancer associated with 17HSD type-5, suc.
Applicant(s) Astellas Pharma Inc
Representative Drug(s) D02JPV Drug Info IC50 = 40 to 50 nM Click to Show More [1]
2 D0S6TL Drug Info IC50 = 40 to 50 nM [1]
Patent ID WO2009014150
Title Benzimidazole Derivative.
Applicant(s) Astellas Pharma Inc
Representative Drug(s) D02JPV Drug Info IC50 = 40 to 50 nM Click to Show More [1]
2 D0S6TL Drug Info IC50 = 40 to 50 nM [1]
Patent ID WO2017070448
Title 2-Beta-Naphthyl-Acetic Acid Analogs As Akr1C3 Inhibitors and Methods of Using Same.
Abstract The invention includes 2-gama-naphthyl-acetic acid derivatives, which are selective AKR1C3 inhibitors. In certain embodiments, the compounds of the invention are R-naproxen analogs. The invention further includes methods of treating cancer, such as prostate cancer and/or castration-resistant prostate cancer, using at least one compound of the invention.
Applicant(s) The Trustes of the University of Pennsylvania
Representative Drug(s) D0G8VB Drug Info IC50 = 110 nM [1]
Patent ID WO2016037956
Title 3-Nitrogen or Sulphur Substituted Oestra-1,3,5(10),16-Tetraene Akr1C3 Inhibitors.
Abstract The invention relates to AKR1C3 inhibitors of formula (I) and to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of bleeding disorders and endometriosis.
Applicant(s) Bayer Pharma Aktiengesellschaft
Representative Drug(s) D0PI1W Drug Info IC50 = 1 nM [1]
Patent ID WO2014128108
Title Estra-1,3,5(10),16-Tetraene-3-Carboxamides for Inhibition of 17.Beta.-Hydroxysteroid Dehydrogenase (Akr1 C3).
Abstract The invention relates to AKR1C3 inhibitors of the formula (I) and to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of menstrual complaints and endometriosis.
Applicant(s) Bayer Pharma Aktiengesellschaft
Representative Drug(s) D0PI1W Drug Info IC50 = 1 nM [1]
Patent ID WO2014039820
Title Aldo-Keto Reductase Subfamily 1C3 (Akr1C3) Inhibitors.
Abstract The present invention relates to a novel class of AKR1C3 inhibitors, to compositions containing them, to methods for their preparation, and to methods of use thereof. The AKR1C3 inhibitors may be useful in the treatment of, for example, prostate cancer, benign prostate hyperplasia (BPH), lung cancer, acne, seborrhea, hirsuitism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, uterine cancer, uterine fibroids, endometriosis, myeloma and leiomyoma.
Applicant(s) Gtx, Inc
Representative Drug(s) D0Y7XJ Drug Info IC50 = 770 nM [1]
Patent ID WO2014009274
Title 3-Substituted Estra-1,3,5(10),16-Tetraene Derivatives, Methods for The Production Thereof, Pharmaceutical Preparations Containing Same, and Use Thereof for The Production of Medicaments.
Abstract The invention relates to AKR1C3 inhibitors and methods for the production thereof, the use thereof for treating and/or preventing diseases, and the use thereof for producing medicaments for treating and/or preventing diseases, in particular menstrual pain and endometriosis.
Applicant(s) Bayer Pharma Aktiengesellschaft
Representative Drug(s) D0PI1W Drug Info IC50 = 1 nM [1]
Patent ID WO2013142390
Title Aldo-Keto Reductase Subfamily 1C3 (Akr1C3) Inhibitors.
Abstract The present invention relates to a novel class of AKR1C3 inhibitors, to compositions containing them, to methods for their preparation, and to methods of use thereof. The AKR1C3 inhibitors may be useful in the treatment of, for example, prostate cancer, benign prostate hyperplasia (BPH), lung cancer, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, uterine cancer, uterine fibroids, endometriosis, myeloma and leiomyoma.
Applicant(s) Gtx, Inc
Representative Drug(s) D0Y7XJ Drug Info IC50 = 770 nM [1]
Patent ID WO2013045407
Title Estra-1,3,5(10),16-Tetraene-3-Carboxamide Derivatives, Process for Preparation Thereof, Pharmaceutical Preparations Comprising Them, and Use Thereof for Production of Medicaments.
Abstract The invention relates to AKR1C3 inhibitors and to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of bleeding problems and endometriosis.
Applicant(s) Bayer Intellectual Property Gmbh
Representative Drug(s) D0PI1W Drug Info IC50 = 1 nM [1]
Patent ID WO2012122208
Title Hydrocracking Catalysts Containing Stabilized Aggregates of Small Crystallites of Zeolite Y and Associated Hydrocarbon Conversion Processes.
Abstract This invention relates to hydrocracking catalysts utilizing stabilized aggregates of small primary crystallites of zeolite Y that are clustered into larger secondary particles. At least 80% of the secondary particles may comprise at least 5 primary crystal lites. The size of the primary crystallites may be at most about 0.5 micron, or at most about 0.3 micron, and the size of the secondary particles may be at least about 0.8 micron, or at least about 1.0 im. The silica to alumina ratio of the resulting stabilized aggregated Y zeolite may be 4: 1 or more. This invention also relates to the use of such catalysts in hydrocracking processes for the conversion of heavy oils into lighter fuel products. The invention is particularly suited for the selective production of diesel range products from gas oil range feedstock materials under hydrocracking conditions.
Applicant(s) Exxonmobil Research and Engineering Company
Representative Drug(s) D05GKS Drug Info IC50 = 60 nM [1]
Patent ID WO2007100066
Title 17 Beta Hsd Type 5 Inhibitor.
Abstract It is intended to provide a novel and excellent method of treating and/or preventing prostate cancer, prostate enlargement, acne, seborrhea, hypertrichosis, calvities, alopecia, sexual precocity, adrenal hypertrophy, multilocular ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and so on based on an effect of selectively inhibiting 17gama HSD type 5. It is found out that an N-sulfonylindole derivative, in which a carbon atom in the indole group is substituted by a carboxy group, a carboxy-substituted lower alkyl group or a carboxy-substituted lower alkenyl group, has a potent activity of selectively inhibiting 17gama HSD type 5 and is usable as a remedy and/or a preventive for diseases, in which 17gama HSD type 5 participates, such as prostate enlargement and prostate cancer without showing any side effect caused by a decrease in testosterone.
Applicant(s) Astellas Pharma Inc
Patent ID WO2010101128
Title Amide Compound.
Applicant(s) Astellas Pharma Inc
Representative Drug(s) D0SM2O Drug Info IC50 = 24 nM [1]
Patent ID WO2010101127
Title Indole Compound.
Applicant(s) Astellas Pharma Inc
Representative Drug(s) D0Q8RC Drug Info IC50 = 3.7 nM [1]
Patent ID WO2012142208
Title Hydrocracking Catalysts Containing Stabilized Aggregates of Small Crystallites of Zeolite Y and Associated Hydrocarbon Conversion Processes.
Representative Drug(s) D0M6LX Drug Info IC50 = 80 nM [1]
United States Patent and Trademark Office (USPTO)
Patent ID US20160303082
Title Indomethacin Analogs for The Treatment of Castrate-Resistant Prostate Cancer.
Representative Drug(s) D0E2TY Drug Info IC50 = 90 nM Click to Show More [1]
2 D0F0PK Drug Info IC50 = 90 nM [1]
3 D0GY2Z Drug Info IC50 = 90 nM [1]
Patent ID US20140107085
Title Bifunctional Akr1C3 Inhibitors/androgen Receptor Modulators and Methods of Use Thereof.
Representative Drug(s) D05GKS Drug Info IC50 = 60 nM Click to Show More [1]
2 D0M6LX Drug Info IC50 = 80 nM [1]
Japan Patent Office (JPO)
Patent ID JP2012102017
Title Indole Compound.
Representative Drug(s) D0Q8RC Drug Info IC50 = 3.7 nM [1]
Patent ID JP201202018
Title Preparation of N-(benzimidazolylcarbonyl)-piperidines As AKR1C3 Inhibitors.
Applicant(s) Preclinical(Astellas)
Representative Drug(s) D0N3XY Drug Info IC50 = 110 nM [1]
Patent ID JP2010222350
Title Piperidine Derivative.
Representative Drug(s) D0Q8RC Drug Info IC50 = 3.7 nM [1]
Patent ID JP2015020966
Title Akr1C3 Inhibitor.
Canadian Intellectual Property Office (CIPO)
Patent ID CA02694216
Title Preparation of N-(benzimidazoles or indole) benzoic acids As AKR1C3 Inhibitor.
Representative Drug(s) D02JPV Drug Info IC50 = 40 to 50 nM Click to Show More [1]
2 D0S6TL Drug Info IC50 = 40 to 50 nM [1]
Patent ID CA2644809
Title Beta. Hsd Type 5 Inhibitor.
Abstract It is intended to provide a novel and excellent method of treating and/or preventing prostate cancer, prostate enlargement, acne, seborrhea, hypertrichosis, calvities, alopecia, sexual precocity, adrenal hypertrophy, multilocular ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and so on based on an effect of selectively inhibiting 17.beta. HSD type 5. It is found out that an N-sulfonylindole derivative, in which a carbon atom in the indole group is substituted by a carboxy group, a carboxy-substituted lower alkyl group or a carboxy-substituted lower alkenyl group, has a potent activity of selectively inhibiting 17.beta. HSD type 5 and is usable as a remedy and/or a preventive for diseases, in which 17.beta. HSD type 5 participates, such as prostate enlargement and prostate cancer without showing any side effect caused by a decrease in testosterone.
Applicant(s) Preclinical(Astellas)
References  Top
REF 1 Aldo-Keto Reductase (AKR) 1C3 inhibitors: a patent review.Expert Opin Ther Pat. 2017 Dec;27(12):1329-1340.

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