TW202417000A - Tlr7/tlr8抑制劑之晶型 - Google Patents

Tlr7/tlr8抑制劑之晶型 Download PDF

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Publication number
TW202417000A
TW202417000A TW112150642A TW112150642A TW202417000A TW 202417000 A TW202417000 A TW 202417000A TW 112150642 A TW112150642 A TW 112150642A TW 112150642 A TW112150642 A TW 112150642A TW 202417000 A TW202417000 A TW 202417000A
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TW
Taiwan
Prior art keywords
methyl
pyridin
pyrazolo
crystalline form
octan
Prior art date
Application number
TW112150642A
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English (en)
Chinese (zh)
Inventor
妮可 畢瑞
安德列亞斯 柯迪考斯基
李斌
菲力浦 路司丹伯格
莉塔 雷莫斯
維傑 賽特拉曼
張思思
Original Assignee
瑞士商諾華公司
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Application filed by 瑞士商諾華公司 filed Critical 瑞士商諾華公司
Publication of TW202417000A publication Critical patent/TW202417000A/zh

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • A61K31/41621,2-Diazoles condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/301,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-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)
TW112150642A 2018-05-18 2019-05-16 Tlr7/tlr8抑制劑之晶型 TW202417000A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2018087448 2018-05-18
WOPCT/CN2018/087448 2018-05-18

Publications (1)

Publication Number Publication Date
TW202417000A true TW202417000A (zh) 2024-05-01

Family

ID=67145832

Family Applications (2)

Application Number Title Priority Date Filing Date
TW112150642A TW202417000A (zh) 2018-05-18 2019-05-16 Tlr7/tlr8抑制劑之晶型
TW108116864A TWI826446B (zh) 2018-05-18 2019-05-16 Tlr7/tlr8抑制劑之晶型

Family Applications After (1)

Application Number Title Priority Date Filing Date
TW108116864A TWI826446B (zh) 2018-05-18 2019-05-16 Tlr7/tlr8抑制劑之晶型

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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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

Also Published As

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
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
KR20210013554A (ko) 2021-02-04

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