KR102760889B1 - 2-(3급-부틸아미노)-4-((1ｒ,3ｒ,4ｒ)-3-하이드록시-4-메틸사이클로헥실아미노)-피리미딘-5-카복스아미드의 고체형, 이의 조성물 및 이의 사용방법 - Google Patents

2-(3급-부틸아미노)-4-((1ｒ,3ｒ,4ｒ)-3-하이드록시-4-메틸사이클로헥실아미노)-피리미딘-5-카복스아미드의 고체형, 이의 조성물 및 이의 사용방법 Download PDF

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KR102760889B1
KR102760889B1 KR1020227013115A KR20227013115A KR102760889B1 KR 102760889 B1 KR102760889 B1 KR 102760889B1 KR 1020227013115 A KR1020227013115 A KR 1020227013115A KR 20227013115 A KR20227013115 A KR 20227013115A KR 102760889 B1 KR102760889 B1 KR 102760889B1
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compound
formula
chemical formula
solvent
chiral
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KR20220051440A (ko
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안토니오 크리스티앙 페르티
혼-와 만
잘리 머슬히디노글루
진 쉬
켈빈 힌-영 용
마리아 조르주 보샹
모히트 아툴 코타르
난페이 추
나단 앤드류 뵈르젠
이이잉 리
로버트 힐그라프
마크 에이 나지
다오종 추
리안펭 황
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시그날 파마소티칼 엘엘씨
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Dermatology (AREA)
  • Transplantation (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Cosmetics (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020227013115A 2014-01-30 2015-01-29 2-(3급-부틸아미노)-4-((1ｒ,3ｒ,4ｒ)-3-하이드록시-4-메틸사이클로헥실아미노)-피리미딘-5-카복스아미드의 고체형, 이의 조성물 및 이의 사용방법 Active KR102760889B1 (ko)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201461933636P 2014-01-30 2014-01-30
US61/933,636 2014-01-30
US201462025161P 2014-07-16 2014-07-16
US62/025,161 2014-07-16
KR1020167023497A KR102505677B1 (ko) 2014-01-30 2015-01-29 2-(3급-부틸아미노)-4-((1ｒ,3ｒ,4ｒ)-3-하이드록시-4-메틸사이클로헥실아미노)-피리미딘-5-카복스아미드의 고체형, 이의 조성물 및 이의 사용방법
PCT/US2015/013412 WO2015116755A2 (en) 2014-01-30 2015-01-29 Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use

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KR1020167023497A Division KR102505677B1 (ko) 2014-01-30 2015-01-29 2-(3급-부틸아미노)-4-((1ｒ,3ｒ,4ｒ)-3-하이드록시-4-메틸사이클로헥실아미노)-피리미딘-5-카복스아미드의 고체형, 이의 조성물 및 이의 사용방법

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KR20220051440A KR20220051440A (ko) 2022-04-26
KR102760889B1 true KR102760889B1 (ko) 2025-02-03

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KR1020227013115A Active KR102760889B1 (ko) 2014-01-30 2015-01-29 2-(3급-부틸아미노)-4-((1ｒ,3ｒ,4ｒ)-3-하이드록시-4-메틸사이클로헥실아미노)-피리미딘-5-카복스아미드의 고체형, 이의 조성물 및 이의 사용방법
KR1020167023497A Active KR102505677B1 (ko) 2014-01-30 2015-01-29 2-(3급-부틸아미노)-4-((1ｒ,3ｒ,4ｒ)-3-하이드록시-4-메틸사이클로헥실아미노)-피리미딘-5-카복스아미드의 고체형, 이의 조성물 및 이의 사용방법

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KR1020167023497A Active KR102505677B1 (ko) 2014-01-30 2015-01-29 2-(3급-부틸아미노)-4-((1ｒ,3ｒ,4ｒ)-3-하이드록시-4-메틸사이클로헥실아미노)-피리미딘-5-카복스아미드의 고체형, 이의 조성물 및 이의 사용방법

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US (7) US9365524B2 (enExample)
EP (2) EP3099302B1 (enExample)
JP (3) JP2017504632A (enExample)
KR (2) KR102760889B1 (enExample)
CN (3) CN106163523A (enExample)
AU (2) AU2015211036B2 (enExample)
BR (2) BR122020003206B1 (enExample)
CA (1) CA2938187C (enExample)
CL (1) CL2016001927A1 (enExample)
CR (1) CR20160346A (enExample)
CY (1) CY1123267T1 (enExample)
DK (1) DK3099302T3 (enExample)
EA (2) EA031671B1 (enExample)
ES (1) ES2811834T3 (enExample)
HR (1) HRP20201244T1 (enExample)
HU (1) HUE051266T2 (enExample)
IL (2) IL246931B (enExample)
LT (1) LT3099302T (enExample)
MX (3) MX373804B (enExample)
MY (1) MY180020A (enExample)
NZ (3) NZ715903A (enExample)
PE (1) PE20161437A1 (enExample)
PH (1) PH12016501472B1 (enExample)
PL (1) PL3099302T3 (enExample)
PT (1) PT3099302T (enExample)
RS (1) RS60715B1 (enExample)
SA (1) SA516371578B1 (enExample)
SG (1) SG11201606054SA (enExample)
SI (1) SI3099302T1 (enExample)
SM (1) SMT202000430T1 (enExample)
TW (1) TWI631108B (enExample)
WO (1) WO2015116755A2 (enExample)

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