KR20210013554A - Tlr7/tlr8 억제제의 결정질 형태 - Google Patents

Tlr7/tlr8 억제제의 결정질 형태 Download PDF

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Publication number
KR20210013554A
KR20210013554A KR1020207032942A KR20207032942A KR20210013554A KR 20210013554 A KR20210013554 A KR 20210013554A KR 1020207032942 A KR1020207032942 A KR 1020207032942A KR 20207032942 A KR20207032942 A KR 20207032942A KR 20210013554 A KR20210013554 A KR 20210013554A
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South Korea
Prior art keywords
crystalline form
methyl
pyrazolo
pyridin
crystalline
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Korean (ko)
Inventor
니콜 비에리
안드레아스 코르디코브스키
빈 리
필립 루스텐베르거
리타 라모스
비제이 세투라만
시시 장
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노파르티스 아게
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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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)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
KR1020207032942A 2018-05-18 2019-05-16 Tlr7/tlr8 억제제의 결정질 형태 Ceased KR20210013554A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2018087448 2018-05-18
CNPCT/CN2018/087448 2018-05-18
PCT/IB2019/054066 WO2019220390A1 (en) 2018-05-18 2019-05-16 Crystalline forms of a tlr7/tlr8 inhibitor

Publications (1)

Publication Number Publication Date
KR20210013554A true KR20210013554A (ko) 2021-02-04

Family

ID=67145832

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020207032942A Ceased KR20210013554A (ko) 2018-05-18 2019-05-16 Tlr7/tlr8 억제제의 결정질 형태

Country Status (13)

Country Link
US (2) US12084460B2 (https=)
EP (1) EP3793998A1 (https=)
JP (2) JP7407740B2 (https=)
KR (1) KR20210013554A (https=)
CN (1) CN112119078A (https=)
AR (1) AR117573A1 (https=)
AU (1) AU2019268583B2 (https=)
BR (1) BR112020022738A2 (https=)
CA (1) CA3097312A1 (https=)
CL (1) CL2020002967A1 (https=)
MX (2) MX2020012259A (https=)
TW (2) TW202417000A (https=)
WO (1) WO2019220390A1 (https=)

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Publication number Priority date Publication date Assignee Title
JP7328977B2 (ja) 2018-02-12 2023-08-17 エフ． ホフマン－ラ ロシュ アーゲー ウイルス感染の処置および予防のための新規のスルホン化合物および誘導体
EP3802539B1 (en) 2018-06-05 2023-09-20 F. Hoffmann-La Roche AG Tetrahydro-1h-pyrazino[2,1-a]isoindolylquinoline compounds for the treatment of autoimmune disease
EP3807270B1 (en) 2018-06-12 2023-09-13 F. Hoffmann-La Roche AG Novel heteroaryl heterocyclyl compounds for the treatment of autoimmune disease
CN112584903B (zh) 2018-07-23 2025-12-23 豪夫迈·罗氏有限公司 用于自身免疫性疾病治疗的哌嗪化合物
EP3847169A1 (en) 2018-09-04 2021-07-14 F. Hoffmann-La Roche AG Benzothiazole compounds for the treatment of autoimmune diseases
EP3847173B1 (en) 2018-09-06 2023-04-12 F. Hoffmann-La Roche AG Novel pyrazolopyridine compounds for the treatment of autoimmune disease
US11548884B2 (en) 2018-09-06 2023-01-10 Hoffmann-La Roche Inc. Cyclic amidine compounds for the treatment of autoimmune disease
WO2021084022A1 (en) 2019-10-31 2021-05-06 F. Hoffmann-La Roche Ag Hydropyrazino[1,2-d][1,4]diazepine compounds for the treatment of autoimmune disease
CN114728976B (zh) 2019-11-19 2024-08-16 豪夫迈·罗氏有限公司 用于治疗自身免疫性疾病的氢-1H-吡咯并[1,2-a]吡嗪化合物
WO2021099406A1 (en) 2019-11-20 2021-05-27 F. Hoffmann-La Roche Ag Spiro(isobenzofuranazetidine) compounds for the treatment of autoimmune disease
US20240317735A1 (en) 2020-07-14 2024-09-26 Hoffmann-La Roche Inc. Hydroisoquinoline or hydronaphthyridine compounds for the treatment of autoimmune disease
CR20230478A (es) 2021-04-16 2023-11-30 Gilead Sciences Inc Compuestos de tienopirrol.
KR20240056747A (ko) 2021-09-10 2024-04-30 길리애드 사이언시즈, 인코포레이티드 티에노피롤 화합물
PE20250401A1 (es) 2021-09-24 2025-02-11 Hoffmann La Roche Compuestos de pirazolo[3,4-b]piridina para el tratamiento de enfermedades auto/inmunitarias
AU2023207313A1 (en) * 2022-01-11 2024-06-13 Novartis Ag Tlr7/8-antagonist for treating sjögren's syndrome or mixed connective tissue disease

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2222545A1 (en) 1995-06-07 1996-12-19 Sugen, Inc. Quinazolines and pharmaceutical compositions
AU2006279548A1 (en) 2005-08-16 2007-02-22 Amgen, Inc. Phosphodiesterase 10 inhibitors
TWI674262B (zh) 2011-01-10 2019-10-11 美商英菲尼提製藥股份有限公司 製備異喹啉酮之方法及異喹啉酮之固體形式
DK2812331T3 (en) 2012-02-08 2019-04-08 Janssen Sciences Ireland Unlimited Co PIPERIDINOPYRIMIDINE DERIVATIVES FOR TREATING VIRUS INFECTIONS
EA029281B1 (ru) 2013-07-30 2018-03-30 Джилид Коннектикут, Инк. Полиморф ингибиторов syk
EP3341375B1 (en) 2015-08-25 2022-04-13 BeiGene, Ltd. Process for preparing parp inhibitor, crystalline forms, and uses thereof
GB2566245B (en) * 2016-06-30 2020-09-30 Kimberly Clark Co Method of manufacturing a foam and fiber composite
HRP20220144T1 (hr) * 2016-09-09 2022-04-15 Novartis Ag Spojevi i pripravci kao inhibitori endosomskih toll-u sličnih receptora

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Publication number Publication date
AR117573A1 (es) 2021-08-18
CL2020002967A1 (es) 2021-04-30
AU2019268583A1 (en) 2020-10-29
BR112020022738A2 (pt) 2021-02-02
US20240391938A1 (en) 2024-11-28
US12084460B2 (en) 2024-09-10
TW202015698A (zh) 2020-05-01
JP2024037930A (ja) 2024-03-19
MX2023013584A (es) 2023-11-30
US20210206783A1 (en) 2021-07-08
CN112119078A (zh) 2020-12-22
TW202417000A (zh) 2024-05-01
CA3097312A1 (en) 2019-11-21
JP7407740B2 (ja) 2024-01-04
TWI826446B (zh) 2023-12-21
EP3793998A1 (en) 2021-03-24
MX2020012259A (es) 2021-01-29
JP2021523918A (ja) 2021-09-09
AU2019268583B2 (en) 2022-01-27
WO2019220390A1 (en) 2019-11-21

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