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Quinoxaline compounds

A compound and quinoxaline technology, applied in the field of quinoxaline compounds, can solve the problems of no specific disclosed compound, unrecorded compound having PDE9 inhibitory effect, etc.

Inactive Publication Date: 2012-02-01
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 5 to 10, 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 compounds
  • Quinoxaline compounds
  • Quinoxaline compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 3

[0285] Embodiment 3 (6.7), embodiment 4 (19), embodiment 5 (2.3), embodiment 11 (3.1), embodiment 13 (22), embodiment 27 (18), embodiment 35 (12), implement Example 68 (3.5), Example 71 (9.2), Example 76 (2.5), Example 77 (1.0), Example 80 (2.6), Example 91 (20), Example 93 (15), Example 103(11), Example 134(950), Example 220(18), Example 248(5.8), Example 263(0.9), Example 277(16), Example 279(10), Example 281 (1.6), Example 289 (3.9), Example 290 (1.0), Example 291 (2.8), Example 300 (0.8), Example 306 (4.2), Example 309 (4.1), Example 312 ( 20), Example 318 (5.9), Example 320 (1.0), Example 322 (29), Example 324 (1.7), Example 326 (1.2), Example 330 (1.2), Example 333 (2.9 ), Example 338 (28), Example 343 (13), Example 344 (7.7), Example 346 (27), Example 347 (3.3), Example 350 (9.2), Example 352 (12) , Example 356 (1.5), Example 359 (5.4), Example 516 (0.8), Example 517 (0.9), Example 519 (6.8), Example 522 (3.6), Example 528 (0.9).

[0286] In addition, among the compo...

Embodiment

[0308] 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 obvious to those skilled in the art. manufacture.

[0309] In Examples, Production Examples, and Tables described later, the following abbreviations may be used. tert-: tertiary, Pr: Production example number, Ex: Example number, No: Compound number, Structure: Structural formula, Syn: Production method (the number indicates that the example compound is produced by the same producti...

manufacture example 1

[0311] Suspend 700 mg of methyl 3-chloro-2-hydrazinoquinoxaline-6-carboxylate in 3.7 mL of trimethyl orthobutyrate, and heat to reflux for 2 hours. The solid was filtered off after ice cooling and washed with cold ethyl acetate. The obtained solid was washed with hot ethyl acetate to obtain 612 mg of methyl 4-chloro-1-propyl[1,2,4]triazolo[4,3-a]quinoxaline-7-carboxylate.

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PUM

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Abstract

Disclosed are compounds which have PDE9 inhibitory activity and are useful as the active ingredient of therapeutics and / or preventives for urine collection disorder, urination disorder, bladder / urinary tract diseases and so on. As the results of studies on compounds having PDE9 inhibitory activity and being useful as the active ingredient of therapeutics and / or preventives for urine collection disorder, urination disorder, bladder / urinary tract diseases and so on, it is confirmed that an imidazoquinoxaline compound or a triazoloquinoxaline compound has PDE9 inhibitory activity. The aforesaid imidazoquinoxaline compound or triazoloquinoxaline compound has PDE9 inhibitory activity and is usable as preventives and / or therapeutics for urine collection disorder, urination disorder, bladder / urinary tract diseases and so on.

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 tract diseases. Background technique [0002] The important functions of voiding function are urine storage and urination, which are regulated by the coordination of 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 cannot be full...

Claims

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Application Information

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IPC IPC(8): C07D487/04A61K31/4985A61K31/5377A61K31/5383A61K31/541A61K31/55A61K31/551A61P13/02A61P13/04A61P13/08A61P13/10A61P43/00C07D519/00
CPCC07D498/04C07D487/04C07D519/00C07D491/107A61P13/00A61P13/02A61P13/04A61P13/08A61P13/10A61P43/00C07D405/04A61K31/4985
Inventor 贝泽弘行杉田麻梨蓟英范濑尾龙志野村崇穗山本哲山本博文土屋和之久保田秀树上条一纪
Owner ASTELLAS PHARMA INC
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