THIAZOLE DERIVATIVES

• US 20100280023A1
• Filed: 06/23/2006
• Published: 11/04/2010
• Est. Priority Date: 06/23/2005
• Status: Abandoned Application

• Current Assignee: Kyowa Hakko Kirin Company Limited (Kirin Holdings Company Limited)
• Original Assignee: Kyowa Hakko Kogyo Company Limited (Kirin Holdings Company Limited)
• Inventors: Yamada, Koji, Nakajima, Takao, Sugawara, Masamori, Nakasato, Yoshisuke, Uesaka, Noriaki
• Application Number:
  US11/917,972
• Publication Number:
  US 20100280023A1
• Time in Patent Office: Days
• US Class Current: 514/230.5
• CPC Class Codes: A61P 21/00 Drugs for disorders of the muscular or neuromuscular system
• CPC Class Codes: A61P 21/04 for myasthenia gravis
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/02 for peripheral neuropathies
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/06 Antimigraine agents
• CPC Class Codes: A61P 25/08 Antiepileptics; Anticonvulsants
• CPC Class Codes: A61P 25/14 for treating abnormal movements, e.g. chorea, dyskinesia
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives
• CPC Class Codes: A61P 25/22 Anxiolytics
• CPC Class Codes: A61P 25/24 Antidepressants
• CPC Class Codes: A61P 25/28 for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• CPC Class Codes: A61P 25/30 for treating abuse or dependence
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 31/18 for HIV
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 9/08 Vasodilators for multiple indications
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• CPC Class Codes: C07D 417/04 : directly linked by a ring-member-to-ring-member bond
• CPC Class Codes: C07D 417/14 : containing three or more hetero rings
• CPC Class Codes: C07D 491/08 : Bridged systems
• CPC Class Codes: C07D 493/08 : Bridged systems
• CPC Class Codes: C07D 493/10 : Spiro-condensed systems

Abstract

It is intended to provide an adenosine A_2A receptor antagonist containing as an active ingredient a thiazole derivative represented by the general formula (I) [in the formula, R¹ represents a substituted or unsubstituted five-membered aromatic heterocyclic group containing at least one oxygen atom, R² represents a substituted or unsubstituted heterocyclic group, —COR⁶ (in the formula, R⁶ represents a substituted or unsubstituted heterocyclic group, a substituted or unsubstituted aromatic heterocyclic group or the like) or the like, R³ represents the general formula (II), —NHCOR (in the formula, R⁷ represents —NR⁸R⁹ or the like) or the like], or a pharmacologically acceptable salt thereof, etc. (I) (II)

Claims

1. A method for antagonizing adenosine A_2A receptor comprising the step of administering an effective amount of a thiazole derivative represented by the general formula (I):

2. The method for antagonizing adenosine A_2A receptor according to claim 1, wherein R¹ is substituted or unsubstituted furyl.

3. (canceled)

4. A thiazole derivative represented by the general formula (IA):

5. The thiazole derivative or the pharmaceutically acceptable salt thereof according to claim 4, wherein R^1A is substituted or unsubstituted furyl.

6. The thiazole derivative or the pharmaceutically acceptable salt thereof according to claim 4 or 5, wherein R^6A is a substituted or unsubstituted alicyclic heterocyclic group, or a substituted or unsubstituted aromatic heterocyclic group, and —

CO—

in —

COR^6A binds to a carbon atom of R^6A.

7. The thiazole derivative or the

pharmaceutically acceptable salt thereof according to claim 4, wherein R^6A is a substituted or unsubstituted alicyclic heterocyclic group.

8. The thiazole derivative or the pharmaceutically acceptable salt thereof according to claim 4, wherein R^6A is substituted or unsubstituted tetrahydropyranyl, substituted or unsubstituted pyridyl or substituted or unsubstituted dioxepanyl.

9. The thiazole derivative or the

pharmaceutically acceptable salt thereof according to claim 4, wherein R^3A is —

CONHR¹¹ (wherein R¹¹ has the same meaning as defined above).

10. The thiazole derivative or the

pharmaceutically acceptable salt thereof according to claim 4, wherein R^3A is the formula (II):

11. The thiazole derivative or the pharmaceutically acceptable salt thereof according to claim 10, wherein R¹² and R¹³ are combined with the two carbon atoms adjacent thereto, respectively, to form a substituted or unsubstituted carbon ring, or a substituted or unsubstituted heterocyclic ring.

12. The thiazole derivative or the

pharmaceutically acceptable salt thereof according to claim 4, wherein R^3A is —

NHCOR⁷.

13. A pharmaceutical composition comprising, as an active ingredient, the thiazole derivative or the pharmaceutically acceptable salt thereof described in claim 4.

18. A method for antagonizing adenosine A_2A receptor comprising the step of administering an effective amount of the thiazole derivative or the pharmaceutically acceptable salt thereof described in claim 6.

19. A method for preventing and/or treating a disease associated with adenosine A_2A receptor comprising the step of administering an effective amount of the thiazole derivative or the pharmaceutically acceptable salt thereof described in claim 6.

14-16. -16. (canceled)

17. A method for preventing and/or treating a disease associated with adenosine A_2A receptor comprising the step of administering an effective amount of a thiazole derivative represented by the general formula (I):

24. The method for preventing and/or treating a disease associated with adenosine A_2A receptor according to claim 17, wherein R¹ is substituted or unsubstituted furyl.

20-23. -23. (canceled)