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 T97537 Target Info
Target Name Leucyl-cysteinyl aminopeptidase (LNPEP)
Synonyms Placental leucine aminopeptidase; P-LAP; Oxytocinase; OTase; Leucyl-cystinyl aminopeptidase; Insulin-responsive aminopeptidase; Insulin-regulated membrane aminopeptidase; IRAP; Cystinyl aminopeptidase
Target Type Patented-recorded Target
Gene Name LNPEP
Biochemical Class Peptidase
UniProt ID
LCAP_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
United States Patent and Trademark Office (USPTO)
Patent ID US10059720
Title Pyridine derivative
Abstract The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP.As a result, the inventors have found that (2R)-3-amino-2-{[4-(substituted pyridine)-2-yl]methyl}-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.
Applicant(s) Astellas Pharma Inc.; KOTOBUKI PHARMACEUTICALS CO., LTD.
Representative Drug(s) D05ZEZ Drug Info IC50 = 3.6 nM Click to Show More [1]
2 D06JLW Drug Info IC50 = 3.7 nM [1]
3 D04AFR Drug Info IC50 = 6.5 nM [1]
Patent ID US10059720
Title Pyridine derivative
Abstract The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP.As a result, the inventors have found that (2R)-3-amino-2-{[4-(substituted pyridine)-2-yl]methyl}-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.
Applicant(s) Astellas Pharma Inc.; KOTOBUKI PHARMACEUTICALS CO., LTD.
Representative Drug(s) D05ZEZ Drug Info IC50 = 3.6 nM Click to Show More [1]
2 D06JLW Drug Info IC50 = 3.7 nM [1]
3 D04AFR Drug Info IC50 = 6.5 nM [1]
Patent ID US10059720
Title Pyridine derivative
Abstract The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP.As a result, the inventors have found that (2R)-3-amino-2-{[4-(substituted pyridine)-2-yl]methyl}-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.
Applicant(s) Astellas Pharma Inc.; KOTOBUKI PHARMACEUTICALS CO., LTD.
Representative Drug(s) D05ZEZ Drug Info IC50 = 3.6 nM Click to Show More [1]
2 D06JLW Drug Info IC50 = 3.7 nM [1]
3 D04AFR Drug Info IC50 = 6.5 nM [1]
Patent ID US10023583
Title Bicyclic pyridine compound
Abstract The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-(bi-cyclic pyridylmethyl)-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.
Applicant(s) Astellas Pharma Inc.; KOTOBUKI PHARMACEUTICAL CO., LTD.
Representative Drug(s) D0V4YX Drug Info IC50 = 4.3 nM Click to Show More [2]
2 D0X2XN Drug Info IC50 = 7 nM [2]
3 D0IC5Y Drug Info IC50 = 16 nM [2]
4 D0HO8O Drug Info IC50 = 89 nM [2]
Patent ID US10023583
Title Bicyclic pyridine compound
Abstract The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-(bi-cyclic pyridylmethyl)-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.
Applicant(s) Astellas Pharma Inc.; KOTOBUKI PHARMACEUTICAL CO., LTD.
Representative Drug(s) D0V4YX Drug Info IC50 = 4.3 nM Click to Show More [2]
2 D0X2XN Drug Info IC50 = 7 nM [2]
3 D0IC5Y Drug Info IC50 = 16 nM [2]
4 D0HO8O Drug Info IC50 = 89 nM [2]
Patent ID US10023583
Title Bicyclic pyridine compound
Abstract The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-(bi-cyclic pyridylmethyl)-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.
Applicant(s) Astellas Pharma Inc.; KOTOBUKI PHARMACEUTICAL CO., LTD.
Representative Drug(s) D0V4YX Drug Info IC50 = 4.3 nM Click to Show More [2]
2 D0X2XN Drug Info IC50 = 7 nM [2]
3 D0IC5Y Drug Info IC50 = 16 nM [2]
4 D0HO8O Drug Info IC50 = 89 nM [2]
Patent ID US10023583
Title Bicyclic pyridine compound
Abstract The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-(bi-cyclic pyridylmethyl)-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.
Applicant(s) Astellas Pharma Inc.; KOTOBUKI PHARMACEUTICAL CO., LTD.
Representative Drug(s) D0V4YX Drug Info IC50 = 4.3 nM Click to Show More [2]
2 D0X2XN Drug Info IC50 = 7 nM [2]
3 D0IC5Y Drug Info IC50 = 16 nM [2]
4 D0HO8O Drug Info IC50 = 89 nM [2]
References  Top
REF 1 Pyridine derivative. US10059720.
REF 2 Bicyclic pyridine compound. US10023583.

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