CN112119078A - Tlr7/tlr8抑制剂的晶型 - Google Patents

Tlr7/tlr8抑制剂的晶型 Download PDF

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Publication number
CN112119078A
CN112119078A CN201980032642.0A CN201980032642A CN112119078A CN 112119078 A CN112119078 A CN 112119078A CN 201980032642 A CN201980032642 A CN 201980032642A CN 112119078 A CN112119078 A CN 112119078A
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China
Prior art keywords
degrees
crystalline form
methyl
pyridin
pyrazolo
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Pending
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CN201980032642.0A
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English (en)
Chinese (zh)
Inventor
N·比厄里
A·柯迪考斯基
李斌
P·卢斯滕贝格尔
R·拉莫斯
V·塞图拉曼
张思思
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Novartis AG
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Novartis AG
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Publication of CN112119078A publication Critical patent/CN112119078A/zh
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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)
CN201980032642.0A 2018-05-18 2019-05-16 Tlr7/tlr8抑制剂的晶型 Pending CN112119078A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CNPCT/CN2018/087448 2018-05-18
CN2018087448 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
CN112119078A true CN112119078A (zh) 2020-12-22

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980032642.0A Pending CN112119078A (zh) 2018-05-18 2019-05-16 Tlr7/tlr8抑制剂的晶型

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

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WO2019155042A1 (en) 2018-02-12 2019-08-15 F. Hoffmann-La Roche Ag Novel sulfone compounds and derivatives for the treatment and prophylaxis of virus infection
US12157746B2 (en) 2018-06-05 2024-12-03 Hoffmann-La Roche Inc. 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
US11952363B2 (en) 2018-07-23 2024-04-09 Hoffmann-La Roche Inc. Piperazine compounds for the treatment of autoimmune disease
CN112638908A (zh) 2018-09-04 2021-04-09 豪夫迈·罗氏有限公司 用于治疗自身免疫性疾病的苯并噻唑类化合物
WO2020048596A1 (en) 2018-09-06 2020-03-12 F. Hoffmann-La Roche Ag Novel pyrazolopyridine compounds for the treatment of autoimmune disease
EP3847170B1 (en) 2018-09-06 2022-06-22 F. Hoffmann-La Roche AG Novel cyclic amidine compounds for the treatment of autoimmune disease
CN114599652B (zh) 2019-10-31 2024-07-12 豪夫迈·罗氏有限公司 用于治疗自身免疫性疾病的氢吡嗪并[1,2-d][1,4]二氮杂䓬化合物
EP4061816A1 (en) 2019-11-19 2022-09-28 F. Hoffmann-La Roche AG Hydro-1h-pyrrolo[1,2-a]pyrazine compounds for the treatment of autoimmune disease
EP4061821B1 (en) 2019-11-20 2025-08-06 F. Hoffmann-La Roche AG Spiro(isobenzofuranazetidine) compounds for the treatment of autoimmune disease
JP2023533807A (ja) 2020-07-14 2023-08-04 エフ． ホフマン－ラ ロシュ アーゲー 自己免疫疾患の処置のためのヒドロイソキノリン又はヒドロナフチリジン化合物
US11661431B2 (en) 2021-04-16 2023-05-30 Gilead Sciences, Inc. Thienopyrrole compounds
TW202440078A (zh) 2021-09-10 2024-10-16 美商基利科學股份有限公司 噻吩并吡咯化合物
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

Citations (1)

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Publication number Priority date Publication date Assignee Title
WO2018047081A1 (en) * 2016-09-09 2018-03-15 Novartis Ag Compounds and compositions as inhibitors of endosomal toll-like receptors

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JPH11507052A (ja) 1995-06-07 1999-06-22 スージェン・インコーポレーテッド キナゾリンおよび医薬組成物
EP1940819A1 (en) 2005-08-16 2008-07-09 Memory Pharmaceuticals Corporation Phosphodiesterase 10 inhibitors
EP3238722B1 (en) 2011-01-10 2019-03-13 Infinity Pharmaceuticals, Inc. Solid forms of isoquinolinones
EA039373B1 (ru) 2012-02-08 2022-01-19 Янссен Сайенсиз Айрлэнд Юси Производные пиперидино-пиримидина для лечения вирусных инфекций
EA029281B1 (ru) 2013-07-30 2018-03-30 Джилид Коннектикут, Инк. Полиморф ингибиторов syk
AU2016312011B2 (en) * 2015-08-25 2021-02-04 Beigene, Ltd. Process for preparing Parp inhibitor, crystalline forms, and uses thereof
BR112018074911B1 (pt) * 2016-06-30 2023-01-17 Kimberly-Clark Worldwide, Inc. Processo para fabricar um compósito de espuma e fibra, compósito de espuma e fibra, e, artigo absorvente

Patent Citations (1)

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Publication number Priority date Publication date Assignee Title
WO2018047081A1 (en) * 2016-09-09 2018-03-15 Novartis Ag Compounds and compositions as inhibitors of endosomal toll-like receptors

Non-Patent Citations (1)

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EP3793998A1 (en) 2021-03-24
CL2020002967A1 (es) 2021-04-30
MX2020012259A (es) 2021-01-29
MX2023013584A (es) 2023-11-30
JP7407740B2 (ja) 2024-01-04
TWI826446B (zh) 2023-12-21
CA3097312A1 (en) 2019-11-21
KR20210013554A (ko) 2021-02-04
WO2019220390A1 (en) 2019-11-21
AU2019268583A1 (en) 2020-10-29
JP2024037930A (ja) 2024-03-19
US20210206783A1 (en) 2021-07-08
US20240391938A1 (en) 2024-11-28
TW202015698A (zh) 2020-05-01
TW202417000A (zh) 2024-05-01
US12084460B2 (en) 2024-09-10
AU2019268583B2 (en) 2022-01-27
AR117573A1 (es) 2021-08-18
BR112020022738A2 (pt) 2021-02-02
JP2021523918A (ja) 2021-09-09

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