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1. WO2020111524 - SALT AND CRYSTALLINE FORM OF PUROPYRIMIDINE COMPOUND AND PHARMACEUTICAL USE THEREOF

Publication Number WO/2020/111524
Publication Date 04.06.2020
International Application No. PCT/KR2019/014164
International Filing Date 25.10.2019
IPC
C07D 498/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
498Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12in which the condensed system contains three hetero rings
A61K 31/519 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61K 31/527 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
527spiro-condensed
A61P 5/24 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5Drugs for disorders of the endocrine system
24of the sex hormones
CPC
A61K 31/519
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61K 31/527
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
527spiro-condensed
A61P 5/24
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5Drugs for disorders of the endocrine system
24of the sex hormones
C07B 2200/13
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200Indexing scheme relating to specific properties of organic compounds
13Crystalline forms, e.g. polymorphs
C07D 498/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
498Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12in which the condensed system contains three hetero rings
Applicants
  • 주식회사 티움바이오 TIUMBIO CO., LTD. [KR]/[KR]
Inventors
  • 이민희 LEE, Minhee
  • 김선미 KIM, Seon-Mi
  • 김훈택 KIM, Hun-Taek
Agents
  • 제일특허법인(유) FIRSTLAW P.C.
Priority Data
10-2018-015199030.11.2018KR
Publication Language Korean (KO)
Filing Language Korean (KO)
Designated States
Title
(EN) SALT AND CRYSTALLINE FORM OF PUROPYRIMIDINE COMPOUND AND PHARMACEUTICAL USE THEREOF
(FR) SEL ET FORME CRISTALLINE D'UN COMPOSÉ DE PUROPYRIMIDINE ET UTILISATION PHARMACEUTIQUE ASSOCIÉE
(KO) 퓨로피리미딘 화합물의 염 및 결정형, 및 이의 약학적 용도
Abstract
(EN)
Salts and crystalline forms of the compound of chemical formula 1, that is, (R)-4-((2-(1-(2-fluoro-6-(trifluoromethyl)benzyl)-2,4-dioxo-1'-((5-(trifluoromethyl)furan-2-yl)methyl)-1H-spiro[puro[3,4-d]pyrimidine-5,4'-piperidine]-3(2H,4H,7H)-yl)-1-phenylethyl)amino)butanoic acid according to the present invention are excellent in terms of general physicochemical properties, e.g., hygroscopicity, related substances, chemical stability, etc. and as such, can be utilized for pharmaceutical uses, such as the preparation of a pharmaceutical composition comprising same as an active ingredient.
(FR)
La présente invention concerne des sels et des formes cristallines du composé de formule chimique 1, c'est-à-dire de l'acide (R)-4-((2-(1-(2-fluoro-6-(trifluorométhyl)benzyl)-2,4-dioxo-1'-((5-(trifluorométhyl)furan-2-yl)méthyl)-1H-spiro[puro[3,4-d]pyrimidine-5,4'-pipéridine]-3(2H,4H,7H)-yl)-1-phényléthyl)amino)butanoïque qui présentent d'excellentes propriétés physico-chimiques générales, par exemple l'hygroscopicité, les substances associées, la stabilité chimique, etc. et en tant que tel, peuvent être utilisés pour des utilisations pharmaceutiques, telles que la préparation d'une composition pharmaceutique le comprenant en tant que principe actif.
(KO)
본 발명에 따른 화학식 1의 화합물, 즉 (R)-4-((2-(1-(2-플루오로-6-(트리플루오로메틸)벤질)-2,4-디옥소-1'-((5-(트리플루오로메틸)퓨란-2-일)메틸)-1H-스피로[퓨로[3,4-d]피리미딘-5,4'-피페리딘]-3(2H,4H,7H)-일)-1-페닐에틸)아미노)부타논산의 염 및 결정형은 물리화학적 제반 특성, 즉 흡습도, 유연물질, 화학적 안정성 등의 면에서 우수하여, 이를 유효 성분으로 포함하는 약학적 조성물의 제조와 같은 약학적 용도에 이용될 수 있다.
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