CN Patent

CN101454338A — κ阿片样受体肽的N-氧化物

Assigned to Tvardi Therapeutics Inc · Expires 2009-06-10 · 17y expired

What this patent protects

本发明涉及表现出与μ阿片样受体相比而言对κ阿片样受体(KOR)的高选择性并表现出很少或者没有CYP3A4抑制活性的某些肽，所述肽包括四个D－异构体氨基酸残基的四肽，所述四肽具有作为N－氧化物取代酰胺的C－端，例如H－D－Phe－D－Phe－D－Nle－D－Arg－NH－4－吡啶甲基－N－氧化物。一个优选的化合物是H－D－Phe－D－Phe－D－Nle－D－Arg－NH－4－吡啶甲基－N－氧化物，其对KOR的亲和力至少是其对μ阿片样受体的亲和力的1000倍，并且对CYP3A4具有大于约10微摩尔的IC 50 。

USPTO Abstract

本发明涉及表现出与μ阿片样受体相比而言对κ阿片样受体(KOR)的高选择性并表现出很少或者没有CYP3A4抑制活性的某些肽，所述肽包括四个D－异构体氨基酸残基的四肽，所述四肽具有作为N－氧化物取代酰胺的C－端，例如H－D－Phe－D－Phe－D－Nle－D－Arg－NH－4－吡啶甲基－N－氧化物。一个优选的化合物是H－D－Phe－D－Phe－D－Nle－D－Arg－NH－4－吡啶甲基－N－氧化物，其对KOR的亲和力至少是其对μ阿片样受体的亲和力的1000倍，并且对CYP3A4具有大于约10微摩尔的IC 50 。

Drugs covered by this patent

difelikefalin-acetate (DIFELIKEFALIN ACETATE)

Patent Metadata

Patent number: CN101454338A
Jurisdiction: CN
Classification: —
Expires: 2009-06-10
Drug substance claim: No
Drug product claim: No
Assignee: Tvardi Therapeutics Inc
Source: FDA Orange Book + USPTO grounding via Google Patents

Bibliographic data sourced from FDA Orange Book + USPTO public records. Plain-English summary generated by AI grounded in source text. Patent term extensions (PTR, SPC, pediatric) may shift the effective expiry. Not legal advice.

Track this patent

Get a daily-checked alert when vulnerability score, expiry, classification, or assignee changes. Email, Slack, or Teams delivery. Pro: 50 watches, Free: 3.