AU2019268583B2 - Crystalline forms of a TLR7/TLR8 inhibitor - Google Patents

Crystalline forms of a TLR7/TLR8 inhibitor Download PDF

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Publication number
AU2019268583B2
AU2019268583B2 AU2019268583A AU2019268583A AU2019268583B2 AU 2019268583 B2 AU2019268583 B2 AU 2019268583B2 AU 2019268583 A AU2019268583 A AU 2019268583A AU 2019268583 A AU2019268583 A AU 2019268583A AU 2019268583 B2 AU2019268583 B2 AU 2019268583B2
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AU
Australia
Prior art keywords
crystalline form
methyl
pyridin
pyrazolo
crystalline
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
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AU2019268583A
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English (en)
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AU2019268583A1 (en
Inventor
Nicole Bieri
Andreas Kordikowski
Bin Li
Philipp Lustenberger
Rita Ramos
Vijay SETHURAMAN
Sisi ZHANG
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Novartis AG
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Novartis AG
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Publication of AU2019268583B2 publication Critical patent/AU2019268583B2/en
Ceased legal-status Critical Current
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    • 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
    • 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
    • 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

Landscapes

  • 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)
AU2019268583A 2018-05-18 2019-05-16 Crystalline forms of a TLR7/TLR8 inhibitor Ceased AU2019268583B2 (en)

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 (2)

Publication Number Publication Date
AU2019268583A1 AU2019268583A1 (en) 2020-10-29
AU2019268583B2 true AU2019268583B2 (en) 2022-01-27

Family

ID=67145832

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2019268583A Ceased AU2019268583B2 (en) 2018-05-18 2019-05-16 Crystalline forms of a TLR7/TLR8 inhibitor

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

Citations (1)

* Cited by examiner, † Cited by third party
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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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

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

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
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
WO2019220390A1 (en) 2019-11-21
KR20210013554A (ko) 2021-02-04

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