Imidazopyrazinamine phenyl derivative and use thereof

• US 10,640,512 B2
• Filed: 06/29/2017
• Issued: 05/05/2020
• Est. Priority Date: 06/30/2016
• Status: Active Grant

• Current Assignee: Hangzhou Bangshun Pharmaceutical Company Limited
• Original Assignee: Hangzhou Sanyintai Pharmaceutical Technology Co., Ltd.
• Inventors: Yin, Jianming, Lv, Yubin, Li, Bangliang
• Primary Examiner(s): Bernhardt, Emily A
• Application Number:
  US16/311,979
• Publication Number:
  US 20190211023A1
• Time in Patent Office: 1,041 Days
• CPC Class Codes: A61K 31/4985 Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 19/02 for joint disorders, e.g. arthritis, arthrosis
• CPC Class Codes: A61P 19/04 for non-specific disorders of the connective tissue
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 31/00 Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 35/02 specific for leukemia
• CPC Class Codes: A61P 37/00 Drugs for immunological or allergic disorders
• CPC Class Codes: A61P 37/08 Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14
• CPC Class Codes: C07D 487/04 Ortho-condensed systems

Abstract

Imidazopyrazinamine phenyl derivatives, pharmaceutically acceptable salts and hydrates thereof, or metabolites thereof formed by any form of metabolism, and uses thereof in the preparation of medicaments for preventing and/or treating indications/diseases associated with BTK functions are disclosed. The disclosed imidazopyrazinamine phenyl derivatives are ideal high-efficient BTK inhibitors for treating or preventing diseases such as rheumatoid arthritis, B cell lymphoma, leukemia, multiple myeloma, allergies, asthma, multiple sclerosis, type I diabetes and systemic lupus erythematosus.

Claims

1. An imidazopyrazinamine phenyl derivative having a structure represented by general formula (I), a pharmaceutically acceptable salt or hydrate thereof,

2. The imidazopyrazinamine phenyl derivative according to claim 1, a pharmaceutically acceptable salt or hydrate thereof, wherein R₂ is H, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl or tert-butyl.

3. The imidazopyrazinamine phenyl derivative according to claim 1, a pharmaceutically acceptable salt or hydrate thereof, wherein R₃ is

4. The imidazopyrazinamine phenyl derivative according to claim 1, a pharmaceutically acceptable salt or hydrate thereof, wherein R₅ is H, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl or tert-butyl.

5. The imidazopyrazinamine phenyl derivative according to claim 1, a pharmaceutically acceptable salt or hydrate thereof, wherein the imidazopyrazinamine phenyl derivative is one of the compounds represented by the following structural formulas:

6. A method for treating an indication/disease associated with BTK functions, the method comprising administering the imidazopyrazinamine phenyl derivative having a structure represented by general formula (I) according to claim 1, a pharmaceutically acceptable salt or hydrate thereof, wherein the indication/disease associated with BTK functions is B cell lymphoma.