Crystalline diacylhydrazine and the use thereof

• Main Authors: SHULMAN INNA, HORMANN ROBERT E, HILFIKER ROLF, RODEL EVA, DEPAUL SUSAN M
• Format: Patent
• Language: English; Korean
• Published: 23.10.2019
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; AGRICULTURE; ANIMAL HUSBANDRY; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES, AS HERBICIDES; CHEMISTRY; FISHING; FORESTRY; HUMAN NECESSITIES; HUNTING; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTSTHEREOF; TRAPPING

본 발명은 (R)-3,5-디메틸-벤조산 N-(1-3급-부틸-부틸)-N'-(2-에틸-3-메톡시-벤조일)-하이드라지드(화합물 1) 또는 (S)-3,5-디메틸-벤조산 N-(1-3급-부틸-부틸)-N'-(2-에틸-3-메톡시-벤조일)-하이드라지드(화합물 2)의 결정성 다형체 또는 무정형 형태를 제공한다. 또한 본 발명은 화합물 1 또는 화합물 2의 결정성 다형체 및 무정형 형태 및 부형제를 포함하는 조성물, 화합물 1 또는 화합물 2의 결정성 다형체 또는 무정형 형태를 제조하는 방법 및, 세포 또는 대상체에서 유전자 발현을 조절하기 위해 화합물 1 또는 화합물 2의 결정성 다형체 또는 무정형 형태를 사용하는 방법을 제공한다. The present disclosure provides crystalline polymorphic and amorphous forms of (R)-3,5-dimethyl-benzoic acid N-(1-tert-butyl-butyl)-N'-(2-ethyl-3-methoxybenzoyl)-hydrazide (Compound 1) or (S)-3,5-dimethyl-benzoic acid N-(1-tert-butyl-butyl)-N'-(2-ethyl-3-methoxy-benzoyl)-hydrazide (Compound 2). The present disclosure further provides compositions comprising crystalline polymorphic and amorphous forms of Compound 1 or Compound 2 and an excipient, methods of making crystalline polymorphic or amorphous forms of Compound 1 or Compound 2, and methods of using crystalline polymorphic or amorphous forms of Compound 1 or Compound 2 to regulate gene expression in a cell or in a subject.