Quinoxaline compound

A compound, quinoxaline technology, applied in the directions of organic chemistry, drug combination, urinary system diseases, etc., can solve the problems such as no specific disclosed compound, unrecorded compound with PDE9 inhibitory effect, etc.

Active Publication Date: 2013-05-08
ASTELLAS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In addition, in Patent Documents 7 to 12, compounds represented by the following formulas (C) to (H) are disclosed, but the compounds of the present invention are not specifically disclosed, and it is not described that these compounds have PDE9 inhibitory activity

Method used

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  • Quinoxaline compound
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  • Quinoxaline compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1(3.5)、 Embodiment 2(51)、 Embodiment 3(22)、 Embodiment 4(a)(62)、 Embodiment 4(b)(11)、 Embodiment 5(62)、 Embodiment 6(64)、 Embodiment 7(2.1)、 Embodiment 8(2.8)、 Embodiment 9(1.3)、 Embodiment 10(4.5)、 Embodiment 11(31)、 Embodiment 12(3.6)、 Embodiment 13

[0609]Example 1 (3.5), Example 2 (51), Example 3 (22), Example 4 (a) (62), Example 4 (b) (11), Example 5 (62), Example 6 (64), Example 7 (2.1), Example 8 (2.8), Example 9 (1.3), Example 10 (4.5), Example 11 (31), Example 12 (3.6), Example 13 (14), embodiment 14 (14), embodiment 15 (2.8), embodiment 16 (3.3), embodiment 17 (8.5), embodiment 18 (5.4), embodiment 21 (22), embodiment 22 ( 56), Example 23 (4.9), Example 24 (17), Example 25 (a) (62), Example 25 (b) (14), Example 26 (a) (152), Example 26 (b)(45), Example 27(84), Example 27(a)(137), Example 27(b)(26), Example 28(52), Example 28(a)(139) , embodiment 28 (b) (47), embodiment 29 (15), embodiment 29 (a) (13), embodiment 29 (b) (2.2), embodiment 30 (11), embodiment 30 (a )(38), Example 30(b)(5.8), Example 31(1.4), Example 32(2.6), Example 33(0.81), Example 34(7.5), Example 35(19), Example 36(53), Example 37(53), Example 38(28), Example 39(a)(52), Example 39(b)(14), Example 40(a)(77) , embodiment 40 (b) (16), embodiment ...

Embodiment

[0633] Hereinafter, the production method of the compound of formula (I) is demonstrated in more detail based on an Example. In addition, the present invention is not limited to the compounds described in the following Examples. In addition, the production methods of the raw material compounds are described in the production examples, respectively. In addition, the production method of the compound of formula (I) is not limited to the production method of the specific examples shown below, and the compound of formula (I) can also be produced by a combination of these production methods or methods that are obvious to those skilled in the art .

[0634] In addition, regarding the salt-forming reaction obvious to those skilled in the art, additions or omissions may be added or omitted in the production methods of the specific examples shown below.

[0635] The following abbreviations are sometimes used in Examples, Production Examples, and Tables described below. tert-: tertia...

manufacture example 1

[0637] To 4-chloro-8-methyl-1-(tetrahydro-2H-pyran-4-yl)[1,2,4]triazolo[4,3-a]quinoxaline-7-carboxylic acid 12 mL of 6M hydrochloric acid was added to 649 mg of the ester, and heated to reflux for 20 hours. After ice-cooling, the precipitated solid was filtered and washed with water and ether. The obtained solid was dried under reduced pressure, thereby obtaining 8-methyl-4-oxo-1-(tetrahydro-2H-pyran-4-yl)-4,5-dihydro[1,2, 4] Triazolo[4,3-a]quinoxaline-7-carboxylic acid 307mg.

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PUM

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Abstract

[Problem] To provide a compound that has the effect of inhibiting PDE9 and is useful as an active ingredient in a therapeutic and/or prophylactic agent for urine collection disorders, urination disorders, diseases of the bladder and urinary system, and the like. [Solution] Investigating compounds that have the effect of inhibiting PDE9 and are useful as active ingredients in a therapeutic and/or prophylactic agent for urine collection disorders, urination disorders, diseases of the bladder and urinary system, and the like, the inventors of the present invention verified that an imidazoquinoxaline compound or a triazolo-quinoxaline compound has the effect of inhibiting PDE9, thereby completing the present invention. This imidazoquinoxaline compound or triazolo-quinoxaline compound has the effect of inhibiting PDE9 and can be used a therapeutic and/or prophylactic agent for urine collection disorders, urination disorders, diseases of the bladder and urinary system, and the like.

Description

technical field [0001] The present invention relates to a quinoxaline compound useful as an active ingredient of a pharmaceutical composition, particularly a pharmaceutical composition for treating urinary storage disorders, voiding disorders, and bladder-urinary diseases. Background technique [0002] The important functions of voiding function are urine storage and urination, and these functions are regulated by the synergy between the bladder and urethra. That is, bladder smooth muscle relaxes and urethral sphincter contracts during urine storage, thereby maintaining a state of high urethral resistance and maintaining continence. On the other hand, bladder smooth muscle contracts during urination, while urethral smooth muscle relaxes, and contraction of the external urethral sphincter is also inhibited. Urinary dysfunction includes urinary storage disorders such as overactive bladder in which urine cannot be retained during storage, and voiding disorder in which urine ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D519/00A61K31/4985A61P13/02A61P43/00C07D487/04
CPCC07D519/00C07D487/04A61P13/02A61P13/10A61P43/00A61K31/4985
Inventor 贝泽弘行杉田麻梨山本博文上条一纪土屋和之濑尾龙志山本哲
Owner ASTELLAS PHARMA INC
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