Inhibitors of canine janus kinase and their use
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- ANIMOL DISCOVERY INC
- Filing Date
- 2024-05-30
- Publication Date
- 2026-06-16
AI Technical Summary
を得るのに、又はそうでなければ、化合物又は組成物が投与される対象に有害で無益な事象を減少するのに十分な化合物又は組成物の量である。治療有効用量は、投与される1つ以上の所望される又は望ましい(例えば有益な)効果をもたらす用量であり得、そのような投与は、所定の時間にわたって1回以上発生する。初期の高い投与量(すなわち、1回以上の負荷量)は、望ましい血漿中濃度を迅速に達成するために投与され得ることも理解されるべきである。一方、初期投与量は、最適量より少ないことがあり、一日投与量は、具体的な状況に応じて、治療の経過中に徐々に増加させてよい(すなわち用量漸増法)。
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Abstract
Claims
1. Equation I 【Chemistry 1】 (In the formula, R １ is H or C which is optionally substituted. １ ~C ３ It is alkyl, n = 0 or 1, R ２ is H or CH ３ And, R ３ C １ ~C ４ Alkyl, phenyl, 【Chemistry 2】 And, m is either 0 or 1. X is H, F, Cl, OCH ３ or CH ３ and R ４ is H or CH ３ And, R ５ H, C １ ~C ４ Alkyl, C ３ ~C ５ Cycloalkyl, CH ２ CH ２ OCH ３ or 2-pyrimidinyl, or R ４ and R ５ Together with the contained N atoms, they form a 4-, 5-, or 6-membered ring, and the 6-membered ring optionally contains one additional heteroatom selected from N and O, or R ２ and R ３ It, together with the N atoms it contains, C １ ~C ４ Alkyl, C ７ ~C １２ Aralkyl or -C(O)-NR ６ R ７ It forms a 6-membered ring which is optionally substituted, R ６ is H or C １ ~C ４ It is alkyl, R ７ H, C １ ~C ４ Alkyl, phenyl, or R ６ and R ７ It, together with the N atoms it contains, C １ ~C ４ A compound having the structure of (which optionally contains one additional N atom) or a pharmaceutically acceptable salt or solvate thereof.
2. R ２ H is, R ３ but, 【Transformation 3】 The compound according to claim 1.
3. n is 1, R １ The compound according to claim 2, wherein is H.
4. R ３ but, 【Chemistry 4】 The compound according to claim 1.
5. The compound according to claim 4, wherein m is 0.
6. R ４ and R ５ The compound according to claim 5, wherein each of them is H. 【Request Item 7】 【Chemistry 5】 A compound according to claim 6, selected from the group consisting of the following.
8. The compound according to claim 4, wherein m is 1.
9. R ４ and R ５ However, each CH ３ The compound according to claim 8.
10. structure 【Transformation 6】 The compound according to claim 9, having the following characteristics.
11. R １ H is, R ２ H is, R ４ H is, R ５ However, C １ ~C ４ Alkyl, C ３ ~C ５ Cycloalkyl, CH ２ CH ２ OCH ３ The compound according to claim 4, selected from the group consisting of and 2-pyrimidinyl.
12. R １ CH3 is, R ２ H is, R ４ H is, R ５ However, C １ ~C ４ Alkyl, C ３ ~C ５ Cycloalkyl, CH ２ CH ２ OCH ３ The compound according to claim 4, selected from the group consisting of and 2-pyrimidinyl. 【Request Item 13】 【Chemistry 7】 A compound according to claim 11 or 12, selected from the group consisting of the following.
14. R １ However, H or CH ３ And, R ２ H is, R ４ and R ５ However, C １ ~C ４ Alkyl, C ３ ~C ５ Cycloalkyl, CH ２ CH ２ OCH ３ The compound according to claim 4, each independently selected from the group consisting of and 2-pyrimidinyl. 【Request Item 15】 【Chemistry 8】 A compound according to claim 14, selected from the group consisting of the following.
16. R １ However, H or CH ３ And, R ２ H is, R ４ and R ５ The compound according to claim 4, wherein the N atom contained therein combines with the N atom to form a 4-, 5-, or 6-membered ring, and the 6-membered ring optionally contains one additional heteroatom selected from N and O. 【Request Item 17】 【Chemistry 9】 A compound according to claim 16, selected from the group consisting of the following. 【Request Item 18】 【Chemistry 10】 The compound according to claim 1. 【Request Item 19】 【Chemistry 11】 The compound according to claim 1.
20. R ２ and R ３ together with the N atom it contains form a 6-membered ring optionally substituted with C １ -C ４ alkyl, C ７ -C １２ aralkyl or -C(O)-NR ６ R ７ The compound according to claim 1, which forms a 6-membered ring optionally substituted with
21. Formula II 【Chemistry 12】 The compound according to claim 20, having the structure (wherein Z is C or N). 【Request Item 22】 【Chemistry 13】 The compound according to claim 21, having a structure selected from the group consisting of the following.
23. structure 【Chemistry 14】 The compound according to claim 20, having the following characteristics.
24. A method for treating allergic reactions, allergic dermatitis, atopic dermatitis, eczema or itching in mammals, comprising the step of administering a therapeutically effective amount of a compound according to any one of claims 1 to 23 to a mammal in need of treatment.
25. The method according to claim 24, wherein the mammal is a pet.
26. The method according to claim 25, wherein the pet is a dog.
27. The method according to any one of claims 24 to 26, wherein the compound of formula I is administered orally, parenterally, or topically.
28. The method according to any one of claims 24 to 27, wherein the compound of formula I is administered orally once a day.