Nagano-shi, Japan
Nagano-shi, Japan

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Patent
Astellas Pharma Inc. and Kotobuki Pharmaceutical Co. | Date: 2017-04-05

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.


Patent
Astellas Pharma Inc. and Kotobuki Pharmaceutical Co. | Date: 2016-09-27

As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen-containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.


Patent
Astellas Pharma Inc. and Kotobuki Pharmaceutical Co. | Date: 2016-04-20

Provided is the compound 6-ethyl-3-({3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)-5-(tetrahydro-2H-pyran-4-ylamino)pyrazine-2-carboxamide or a salt thereof for use in a method for preventing and/or treating acute myelocytic leukemia or atypical chronic myelocytic leukemia.


A compound represented by following general formula (I) :---- represents a single bond or a double bond; L represents -NH- or the like; X^(1) represents N or C, provided that in the case where X^(1) is N, X^(2) represents C-R and in the case where X^(1) is C, X^(2) represents N-R^(1) or the like; Ys may be either the same or different and represent CH_(2) or the like; A represents a non-natural sugar residue represented by following general formula:---- represents a single bond or a double bond; X represents O or the like; R^(3) to R^(8) may be either the same or different and represent hydroxy group or the like; and B represents a group represented by following general formula:---- represents a single bond or a double bond; Z^(1) to Z^(16) may be either the same or different and represent CH or the like; R^(10) and R^(11) may be either the same or different and represent a lower alkoxy group having 1 to 5 carbon atoms or the like; and R^(15) represents a hydrogen atom or the like, a pharmaceutically acceptable salt thereof, a prodrug thereof, a hydrate thereof or solvate thereof. Because of having an excellent CNT2 inhibitory activity and showing a high in vivo stability and stable physicochemical properties, the aforesaid compound is useful as a remedy for hyperuricemia.


Patent
Astellas Pharma Inc. and Kotobuki Pharmaceutical Co. | Date: 2012-03-14

Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein. As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EMLA-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.


Patent
Astellas Pharma Inc. and Kotobuki Pharmaceutical Co. | Date: 2014-08-29

Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein. As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.


Patent
Astellas Pharma Inc. and Kotobuki Pharmaceutical Co. | Date: 2015-01-07

Provided is a compound useful as a prophylactic and/or therapeutic agent for bladder cancer. As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen-containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.


Patent
Kotobuki Pharmaceutical Co. and Astellas Pharma Inc. | Date: 2013-02-26

Provided is a compound useful as a prophylactic and/or therapeutic agent for bladder cancer. As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen-containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.


Patent
Astellas Pharma Inc. and Kotobuki Pharmaceutical Co. | Date: 2010-10-06

The present invention provides a pharmaceutical composition useful as a therapeutic agent for fatty liver disease. A pharmaceutical composition, which comprises (1S)-1,5-anhydro-1-[5-(azulen-2-ylmethyl)-2-hydroxyphenyl]-D-glucitol or a pharmaceutically acceptable salt thereof, (1S)-1,5-anhydro-1-[3-(1-benzothiophen-2-ylmethyl)-4-fluorophenyl]-D-glucitol or a pharmaceutically acceptable salt thereof, or alternatively, (1S)-1,5-anhydro-1-[4-chloro-3-(4-ethoxybenzyl)phenyl]-D-glucitol or a pharmaceutically acceptable salt thereof, more specifically such a pharmaceutical composition for treating fatty liver disease, such as nonalcoholic fatty liver disease in one embodiment, or nonalcoholic simple fatty liver and/or nonalcoholic steatohepatitis in another embodiment.


Patent
Astellas Pharma Inc. and Kotobuki Pharmaceutical Co. | Date: 2012-08-29

The present invention provides a solid pharmaceutical composition comprising a cocrystal of (1S)-1,5-anhydro-1-[3-(1-benzothien-2-ylmethyl)-4-fluorophenyl]-D-glucitol and L-proline, in combination with crystalline cellulose, and also provides a method for producing the composition.

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