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1. 发明公开

EP3228616A4 PYRIDINE DERIVATIVES 有权转让
公开(公告)号：EP3228616A4
公开(公告)日：2018-04-25
申请号：EP15865019
申请日：2015-12-04
申请人： ASTELLAS PHARMA INC , KOTOBUKI PHARMACEUTICAL CO LTD
发明人： KAWAGUCHI KENICHI , ISHIHATA AKIHIRO , KANAI AKIRA , TSUCHIYA KAZUYUKI , INAGAKI YUSUKE , KAZAMI JUNICHI , MORIKAWA HIROSHI , HIRAMOTO MASASHI , ENJO KENTARO , TAKAMATSU HAJIME
IPC分类号： C07D213/55 , A61K31/435 , A61K31/438 , A61K31/44 , A61K31/4418 , A61K31/4433 , A61K31/444 , A61K31/472 , A61K31/4747 , A61P7/12 , A61P13/00 , A61P43/00 , C07D213/63 , C07D217/16 , C07D221/02 , C07D221/04 , C07D221/20 , C07D401/04 , C07D405/04
CPC分类号： C07D405/04 , A61K31/435 , A61K31/438 , A61K31/44 , A61K31/4418 , A61K31/4433 , A61K31/444 , A61K31/472 , A61K31/4747 , A61P7/12 , C07D213/55 , C07D213/63 , C07D217/16 , C07D217/24 , C07D221/02 , C07D221/04 , C07D221/20 , C07D401/04
摘要： The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically an agent 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-(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.

3. 发明专利

PL3269721T3 BICYKLICZNY ZWIĄZEK PIRYDYNOWY 未知
公开(公告)号：PL3269721T3
公开(公告)日：2021-10-11
申请号：PL15884684
申请日：2015-11-27
申请人： ASTELLAS PHARMA INC , KOTOBUKI PHARMACEUTICAL CO LTD
发明人： KAWAGUCHI KENICHI , ISHIHATA AKIHIRO , KANAI AKIRA , INAGAKI YUSUKE , HIRAMOTO MASASHI , ENJO KENTARO , TAKAMATSU HAJIME
IPC分类号： A61P13/00 , A61K31/4355 , A61K31/4365 , A61P13/02 , C07D491/048 , C07D495/04

4. 发明专利

CA2976746A1 BICYCLIC PYRIDINE COMPOUND 未知
公开(公告)号：CA2976746A1
公开(公告)日：2016-09-15
申请号：CA2976746
申请日：2015-11-27
申请人： ASTELLAS PHARMA INC , KOTOBUKI PHARMACEUTICAL CO LTD
发明人： KAWAGUCHI KENICHI , ISHIHATA AKIHIRO , KANAI AKIRA , INAGAKI YUSUKE , HIRAMOTO MASASHI , ENJO KENTARO , TAKAMATSU HAJIME
IPC分类号： C07D491/048 , A61K31/4355 , A61K31/4365 , A61P13/02 , C07D495/04
摘要： The present invention addresses the problem of providing a pharmaceutical composition, particularly a compound suitable for the treatment of nocturia. Extensive and intensive studies have been made on compounds capable of inhibiting placental leucineaminopeptidase (P-LAP), in the anticipation that an antidiuretic activity associated with the maintenance of or increase in an endogenous AVP concentration can be exerted by inhibiting P-LAP, which is a metabolic enzyme for AVP, in the nighttime and the urination frequency in the nighttime can be decreased through the antidiuretic activity. As a result, it is found that a (2R)-3-amino-2-(bicyclic pyridylmethyl)-2-hydroxypropanoic acid derivative has a good P-LAP inhibition activity, and it is also found that, in an antidiuretic test using a drinking water-fed rat, the compound has a urine production inhibition activity associated with the increase in an endogenous AVP concentration which is resulted from the P-LAP inhibition by the compound. Thus, the present invention provides a compound which is expected to be used as a therapeutic agent for nocturia and of which the mechanism of action against nocturia is through the inhibition of P-LAP.

5. 发明专利

CA2712948A1 PHENYLACETAMIDE DERIVATIVE 未知
公开(公告)号：CA2712948A1
公开(公告)日：2009-07-23
申请号：CA2712948
申请日：2009-01-16
申请人： ASTELLAS PHARMA INC
发明人： HAYAKAWA MASAHIKO , KIDO YOSHIYUKI , NIGAWARA TAKAHIRO , OKUMURA MITSUAKI , KANAI AKIRA , MAKI KEISUKE , AMINO NOBUAKI
IPC分类号： C07D213/80 , A61K31/415 , A61K31/4155 , A61K31/426 , A61K31/427 , A61K31/437 , A61K31/44 , A61K31/497 , A61P3/10 , A61P43/00 , C07D231/40 , C07D241/20 , C07D277/20 , C07D277/46 , C07D405/12 , C07D417/12 , C07D513/04
摘要： Disclosed is a compound which is useful as a GK-activator. Intensive studies are made on phenyl acetamide derivatives. As a result, it is confirmed that a phenyl acetamide derivative having a sulfonyl group and a cycloalkyl group on a phenyl group therein and a heteroaryl group on a nitrogen atom in an amide therein has a good GK-activating activity. The compound is useful as a therapeutic agent for diabetes, particularly type-2 diabetes, since the compound has a good GK-activating activity.

6. 发明公开

EP3269721A4 BICYCLIC PYRIDINE COMPOUND 有权
公开(公告)号：EP3269721A4
公开(公告)日：2018-08-01
申请号：EP15884684
申请日：2015-11-27
申请人： ASTELLAS PHARMA INC , KOTOBUKI PHARMACEUTICAL CO LTD
发明人： KAWAGUCHI KENICHI , ISHIHATA AKIHIRO , KANAI AKIRA , INAGAKI YUSUKE , HIRAMOTO MASASHI , ENJO KENTARO , TAKAMATSU HAJIME
IPC分类号： C07D491/048 , A61K31/4355 , A61K31/4365 , A61P13/02 , C07D495/04
CPC分类号： C07D491/048 , A61K31/4355 , A61K31/4365 , C07D495/04
摘要： 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.

7. 发明公开

EP3150581A4 PYRIDINE DERIVATIVE 有权
公开(公告)号：EP3150581A4
公开(公告)日：2018-01-17
申请号：EP15799163
申请日：2015-05-28
申请人： ASTELLAS PHARMA INC , KOTOBUKI PHARMACEUTICAL CO LTD
发明人： KAWAGUCHI KENICHI , ISHIHATA AKIHIRO , INAGAKI YUSUKE , TSUCHIYA KAZUYUKI , HANADATE TADAATSU , KANAI AKIRA , KAIZAWA HIROYUKI , KAZAMI JUNICHI , MORIKAWA HIROSHI , HIRAMOTO MASASHI , ENJO KENTARO , TAKAMATSU HAJIME
IPC分类号： C07D213/68 , A61K31/4355 , A61K31/436 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4725 , A61K31/497 , A61K31/506 , A61K31/5377 , A61P13/00 , A61P43/00 , C07D213/70 , C07D213/74 , C07D401/04 , C07D401/06 , C07D401/12 , C07D407/06
CPC分类号： C07D495/04 , A61K31/4355 , A61K31/436 , A61K31/437 , A61K31/439 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4725 , A61K31/497 , A61K31/506 , A61K31/5377 , C07D213/68 , C07D213/70 , C07D213/74 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/06 , C07D405/12 , C07D407/06 , C07D407/12 , C07D409/12 , C07D471/04 , C07D491/048 , C07D491/056 , C07D491/08
摘要： 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.

8. 发明专利

ES2869924T3 Compuesto de piridina bicíclica 未知
公开(公告)号：ES2869924T3
公开(公告)日：2021-10-26
申请号：ES15884684
申请日：2015-11-27
申请人： KOTOBUKI PHARMACEUTICAL CO LTD , ASTELLAS PHARMA INC
发明人： KAWAGUCHI KENICHI , ISHIHATA AKIHIRO , KANAI AKIRA , INAGAKI YUSUKE , HIRAMOTO MASASHI , ENJO KENTARO , TAKAMATSU HAJIME
IPC分类号： A61P13/00 , A61K31/4355 , A61K31/4365 , A61P13/02 , C07D491/048 , C07D495/04
摘要： Compuesto representado por la fórmula (I) o sal del mismo: [Fórmula química 11] **(Ver fórmula)** en la que X es O o S; una línea discontinua es un enlace sencillo o un doble enlace; R1 es un alquilo C1-10 que tiene opcionalmente de uno a cuatro sustituyentes seleccionados del grupo G1; cicloalquilo que tiene opcionalmente de uno a cinco sustituyentes seleccionados del grupo G2; o -alquilen C1- 10-cicloalquilo, en el que el cicloalquilo tiene opcionalmente de uno a cinco sustituyentes seleccionados del grupo G2; R2 y R5 son iguales o diferentes entre sí y son H, alquilo C1-10 o cicloalquilo; R3 es -alquilen C1-10-X3-alquilo C1-10; -alquilen C1-10-X3-alquilen C1-10-cicloalquilo, en el que el cicloalquilo tiene opcionalmente de uno a cinco sustituyentes seleccionados del grupo G2; -alquilen C1-10-cicloalquilo, en el que el cicloalquilo tiene opcionalmente de uno a cinco sustituyentes seleccionados del grupo G2; o -alquilen C1- 10-X3-cicloalquilo, en el que el cicloalquilo tiene opcionalmente de uno a cinco sustituyentes seleccionados del grupo G2; X3 es O o S(O)n, en el que n es 0, 1 ó 2; R4 es OH, NH2 o -O-alquilo C1-10 y R6 es H; o R4 y R6 están unidos entre sí para formar, junto con el -C(=O)- C-O- al que están unidos, 2,2-di(alquil C1-10)-4-oxo-1,3-dioxolan-5,5-diílo; el grupo G1 consiste en halógeno, OH, -O-alquilo C1-10, -S-alquilo C1-10 y -O-halogenoalquilo C1-10; y el grupo G2 consiste en alquilo C1-10, halógeno, halogenoalquilo C1-10, OH, -O-alquilo C1-10, -S-alquilo C1-10 y - O-halogenoalquilo C1-10.

9. 发明专利

PH12017501596A1 BICYCLIC PYRIDINE COMPOUND 未知
公开(公告)号：PH12017501596A1
公开(公告)日：2018-02-12
申请号：PH12017501596
申请日：2017-09-05
申请人： KOTOBUKI PHARMACEUTICAL CO LTD , ASTELLAS PHARMA INC
发明人： KAWAGUCHI KENICHI , ISHIHATA AKIHIRO , KANAI AKIRA , INAGAKI YUSUKE , HIRAMOTO MASASHI , ENJO KENTARO , TAKAMATSU HAJIME
IPC分类号： A61K31/4365 , A61K31/4355 , A61P13/02 , C07D491/048 , C07D495/04
摘要： The present invention addresses the problem of providing a pharmaceutical composition, particularly a compound suitable for the treatment of nocturia. Extensive and intensive studies have been made on compounds capable of inhibiting placental leucineaminopeptidase (P-LAP), in the anticipation that an antidiuretic activity associated with the maintenance of or increase in an endogenous AVP concentration can be exerted by inhibiting P-LAP, which is a metabolic enzyme for AVP, in the nighttime and the urination frequency in the nighttime can be decreased through the antidiuretic activity. As a result, it is found that a (2R)-3-amino-2-(bicyclic pyridylmethyl)-2-hydroxypropanoic acid derivative has a good P-LAP inhibition activity, and it is also found that, in an antidiuretic test using a drinking water-fed rat, the compound has a urine production inhibition activity associated with the increase in an endogenous AVP concentration which is resulted from the P-LAP inhibition by the compound. Thus, the present invention provides a compound which is expected to be used as a therapeutic agent for nocturia and of which the mechanism of action against nocturia is through the inhibition of P-LAP.

10. 发明专利

SG11201706745PA BICYCLIC PYRIDINE COMPOUND 未知
公开(公告)号：SG11201706745PA
公开(公告)日：2017-09-28
申请号：SG11201706745P
申请日：2015-11-27
申请人： ASTELLAS PHARMA INC , KOTOBUKI PHARMACEUTICAL CO LTD
发明人： KAWAGUCHI KENICHI , ISHIHATA AKIHIRO , KANAI AKIRA , INAGAKI YUSUKE , HIRAMOTO MASASHI , ENJO KENTARO , TAKAMATSU HAJIME
IPC分类号： C07D491/048 , A61K31/4355 , A61K31/4365 , A61P13/02 , C07D495/04
摘要： 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.

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