INGENOL-3-ACYLATES III AND INGENOL-3-CARBAMATES

• Main Authors: LIANG XIFU, PER VEDSOE, THOMAS VIFIAN, THOMAS HOEGBERG, KRISTOFFER MAANSSON, GUNNAR GRUE-SOERENSEN
• Format: Patent
• Language: English; Japanese
• Published: 03.03.2016
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; SPECIFIC USE OF COSMETICS OR SIMILAR TOILETPREPARATIONS

PROBLEM TO BE SOLVED: To provide a medicine for prevention, treatment or amelioration of a disease or condition responsive to stimulation of neutrophil oxidative burst, stimulation of keratinocyte IL-8 release, and induction of necrosis.SOLUTION: The invention relates to a compound of formula I for use alone or in combination with at least one pharmaceutically active compound in therapy, {ingenol 3-(N-alkyl-N phenylcarbamate)}derivative}, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, where R is X; X is -NR11R12; R11 and R12 independently represent H, alkyl, alkynyl, alkenyl, cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, alkylaryl or the like)].SELECTED DRAWING: None 【課題】好中球の酸化バーストの刺激、ケラチノサイトＩＬ−８放出の刺激或いはネクローシスの誘導に応答性の疾患又は状態を予防、処置若しくは改善する医薬の提供。【解決手段】単独使用又は１以上の治療上薬学的に活性な化合物と組合せて使用する式Ｉで表される化合物｛インゲノール３−（Ｎ−アルキル−Ｎフェニルカルバメート）｝誘導体｝又はその薬学的に許容される塩、水和物もしくは溶媒和物。［ＲはＸ；Ｘは−ＮＲ１１Ｒ１２；Ｒ１１及びＲ１２は各々独立にＨ、アルキル、アルキニル、アルケニル、シクロアルキル、アリール、ヘテロアリール、シクロアルキルルアルキル、アルキルアリール等）］【選択図】なし