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 T20371 Target Info
Target Name Prolylcarboxypeptidase (PRCP)
Synonyms Proline carboxypeptidase; PCP; Lysosomal carboxypeptidase C; Lysosomal Pro-X carboxypeptidase; Angiotensinase C
Target Type Patented-recorded Target
Gene Name PRCP
Biochemical Class Peptidase
UniProt ID
PCP_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2011156246
Title Novel Prolylcarboxypeptidase Inhibitors.
Abstract Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0L6CM Drug Info IC50 = 0.7 nM Click to Show More [1]
2 D0X8ZF Drug Info IC50 = 0.7 to 550 nM [1]
Patent ID WO2011156220
Title Novel Prolylcarboxypeptidase Inhibitors.
Abstract Compounds of structural formulas I-1 and I-2 are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D00YYA Drug Info IC50 = 0.5 to 18 nM Click to Show More [1]
2 D01RBE Drug Info IC50 = 0.5 nM [1]
3 D0L8VH Drug Info IC50 = 0.8 nM [1]
Patent ID WO2011146300
Title Novel Prolylcarboxypeptidase Inhibitors.
Abstract Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0AF0O Drug Info IC50 = 0.16 nM Click to Show More [1]
2 D0QM9Q Drug Info IC50 = 0.16 to 0.54 nM [1]
3 D03WDH Drug Info IC50 = 0.18 nM [1]
Patent ID WO2011143057
Title Novel Prolylcarboxypeptidase Inhibitors.
Abstract Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0S3AL Drug Info IC50 = 0.035 nM Click to Show More [1]
2 D0A0QQ Drug Info IC50 = 0.051 to 80 nM [1]
3 D0K1GJ Drug Info IC50 = 0.051 nM [1]
4 D0S4XV Drug Info IC50 = 0.051 to 80 nM [1]
5 D07RIZ Drug Info IC50 = 0.31 nM [1]
6 D0NT8N Drug Info IC50 = 0.51 nM [1]
Patent ID WO2011137024
Title Novel Spiropiperidine Prolylcarboxypeptidase Inhibitors.
Abstract Compounds of structural formula (I) are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0LZ4A Drug Info IC50 = 0.49 nM Click to Show More [1]
2 D03GPW Drug Info IC50 = 0.66 nM [1]
3 D07KNI Drug Info IC50 = 0.66 nM [1]
4 D05NQZ Drug Info IC50 = 5.2 nM [1]
Patent ID WO2011137012
Title Prolylcarboxypeptidase Inhibitors.
Abstract Compounds of structural formula (I) are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D03ASG Drug Info IC50 = 2.3 nM Click to Show More [1]
2 D0J3TN Drug Info IC50 = 3.3 nM [1]
3 D01GEE Drug Info N.A. [1]
4 D0R3WH Drug Info N.A. [1]
Patent ID WO2012075287
Title Novel Selective Inhibitors of Prolylcarboxypeptidase.
Abstract The present invention relates to compounds of the formulae: Formula (I), (II), (III), (IV), (V), (VI) in which R is C5-C16 alkyl, R1 is Formula (VII), or Formula (VIII) and isosteres and saltes therof. These compounds are serine protease procarboxypeptidase (FRCP) inhibitors and can be used in the field of weight management and in the preparation of medications for the treatment and management of obesity. Further, the present invention relates to new anorexigenic and anti-inflammatory drugs, acting through PRCP-mediated mechanisms.
Applicant(s) The University of Mississippi
Representative Drug(s) D0A6QI Drug Info Ki = 43000 nM [1]
Patent ID WO2005115446
Title Detection and Use of Prolylcarboxypeptidase.
Applicant(s) Yale University/University of California
United States Patent and Trademark Office (USPTO)
Patent ID US9365539
Title Novel Prolylcarboxypeptidase Inhibitors.
Applicant(s) Merck & Co., Inc
Representative Drug(s) D0S3AL Drug Info IC50 = 0.035 nM Click to Show More [1]
2 D0A0QQ Drug Info IC50 = 0.051 to 80 nM [1]
3 D0K1GJ Drug Info IC50 = 0.051 nM [1]
4 D0S4XV Drug Info IC50 = 0.051 to 80 nM [1]
5 D07RIZ Drug Info IC50 = 0.31 nM [1]
6 D0NT8N Drug Info IC50 = 0.51 nM [1]
Patent ID US8785634
Title Novel Spiropiperidine Prolylcarboxypeptidase Inhibitors.
Applicant(s) Merck & Co., Inc
Representative Drug(s) D0LZ4A Drug Info IC50 = 0.49 nM Click to Show More [1]
2 D03GPW Drug Info IC50 = 0.66 nM [1]
3 D07KNI Drug Info IC50 = 0.66 nM [1]
4 D05NQZ Drug Info IC50 = 5.2 nM [1]
Patent ID US8669252
Title Novel Prolylcarboxypeptidase Inhibitors.
Applicant(s) Merck & Co., Inc
Representative Drug(s) D0AF0O Drug Info IC50 = 0.16 nM Click to Show More [1]
2 D0QM9Q Drug Info IC50 = 0.16 to 0.54 nM [1]
3 D03WDH Drug Info IC50 = 0.18 nM [1]
Patent ID US9193762
Title Novel Selective Inhibitors of Prolylcarboxypeptidase.
Applicant(s) University of Mississippi
Representative Drug(s) D0A6QI Drug Info Ki = 43000 nM [1]
European Patent Office (EPO)
Patent ID EP2571855
Title Novel Prolylcarboxypeptidase Inhibitors.
Applicant(s) Merck & Co., Inc
Representative Drug(s) D0AF0O Drug Info IC50 = 0.16 nM Click to Show More [1]
2 D0QM9Q Drug Info IC50 = 0.16 to 0.54 nM [1]
3 D03WDH Drug Info IC50 = 0.18 nM [1]
Patent ID EP2568812
Title Novel Prolylcarboxypeptidase Inhibitors.
Applicant(s) Merck & Co., Inc
Representative Drug(s) D0S3AL Drug Info IC50 = 0.035 nM Click to Show More [1]
2 D0A0QQ Drug Info IC50 = 0.051 to 80 nM [1]
3 D0K1GJ Drug Info IC50 = 0.051 nM [1]
4 D0S4XV Drug Info IC50 = 0.051 to 80 nM [1]
5 D07RIZ Drug Info IC50 = 0.31 nM [1]
6 D0NT8N Drug Info IC50 = 0.51 nM [1]
Patent ID EP2563764
Title Novel Spiropiperidine Prolylcarboxypeptidase Inhibitors.
Applicant(s) Merck & Co., Inc
Representative Drug(s) D0LZ4A Drug Info IC50 = 0.49 nM Click to Show More [1]
2 D03GPW Drug Info IC50 = 0.66 nM [1]
3 D07KNI Drug Info IC50 = 0.66 nM [1]
4 D05NQZ Drug Info IC50 = 5.2 nM [1]
References  Top
REF 1 Prolylcarboxypeptidase (PrCP) inhibitors and the therapeutic uses thereof: a patent review.Expert Opin Ther Pat. 2017 Oct;27(10):1077-1088.

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