CL2020002967A1 - Formas cristalinas de un inhibidor de tlr7/tlr8 - Google Patents

Formas cristalinas de un inhibidor de tlr7/tlr8

Info

Publication number
CL2020002967A1
CL2020002967A1 CL2020002967A CL2020002967A CL2020002967A1 CL 2020002967 A1 CL2020002967 A1 CL 2020002967A1 CL 2020002967 A CL2020002967 A CL 2020002967A CL 2020002967 A CL2020002967 A CL 2020002967A CL 2020002967 A1 CL2020002967 A1 CL 2020002967A1
Authority
CL
Chile
Prior art keywords
crystalline forms
pyrazolo
pyridin
methyl
tlr7
Prior art date
Application number
CL2020002967A
Other languages
English (en)
Inventor
Nicole Bieri
Andreas Kordikowski
Bin Li
Philipp Lustenberger
Rita Ramos
Vijay Sethuraman
Sisi Zhang
Original Assignee
Novartis Ag
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of CL2020002967A1 publication Critical patent/CL2020002967A1/es

Links

Classifications

    • 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

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)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Steroid Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

Esta solicitud se refiere a diversas formas cristalinas de (S)–N–(4–((5–(1,6–dimetil–1H–pirazolo[3,4–b]piridin–4–il)–3–metil–4,5,6,7–tetrahidro–1H–pirazolo[4,3–c]piridin–1–il)metil)biciclo[2.2.2]octan–1–il)morfolina–3–carboxamida en su forma libre, al igual que a composiciones, método de preparación y métodos de uso de dichas formas. En algunas formas de realización, las formas cristalinas además contienen agua (“hidratos”). Estos materiales son útiles en el tratamiento de diversas enfermedades autoinmunitarias, que incluyen lupus eritematoso sistémico, lupus cutáneo, lupus discoide, enfermedad mixta del tejido conectivo, cirrosis biliar primaria, púrpura trombocitopénica inmunitaria, hidradenitis supurativa, dermatomiositis, polimiositis, síndrome de Sjögren, artritis, artritis reumatoide y psoriasis.
CL2020002967A 2018-05-18 2020-11-16 Formas cristalinas de un inhibidor de tlr7/tlr8 CL2020002967A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN2018087448 2018-05-18

Publications (1)

Publication Number Publication Date
CL2020002967A1 true CL2020002967A1 (es) 2021-04-30

Family

ID=67145832

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2020002967A CL2020002967A1 (es) 2018-05-18 2020-11-16 Formas cristalinas de un inhibidor de tlr7/tlr8

Country Status (13)

Country Link
US (1) US20210206783A1 (es)
EP (1) EP3793998A1 (es)
JP (2) JP7407740B2 (es)
KR (1) KR20210013554A (es)
CN (1) CN112119078A (es)
AR (1) AR117573A1 (es)
AU (1) AU2019268583B2 (es)
BR (1) BR112020022738A2 (es)
CA (1) CA3097312A1 (es)
CL (1) CL2020002967A1 (es)
MX (2) MX2020012259A (es)
TW (1) TWI826446B (es)
WO (1) WO2019220390A1 (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
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
EP3807270B1 (en) 2018-06-12 2023-09-13 F. Hoffmann-La Roche AG Novel heteroaryl heterocyclyl compounds for the treatment of autoimmune disease
WO2020020800A1 (en) 2018-07-23 2020-01-30 F. Hoffmann-La Roche Ag Novel piperazine compounds for the treatment of autoimmune disease
EP3847169A1 (en) 2018-09-04 2021-07-14 F. Hoffmann-La Roche AG Benzothiazole compounds for the treatment of autoimmune diseases
EP3847170B1 (en) 2018-09-06 2022-06-22 F. Hoffmann-La Roche AG Novel cyclic amidine 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
TW202302598A (zh) 2021-04-16 2023-01-16 美商基利科學股份有限公司 噻吩并吡咯化合物
AU2022351495A1 (en) 2021-09-24 2024-02-01 F. Hoffmann-La Roche Ag Pyrazolo[3,4-b]pyridine compounds for the treatment of autoimmune disease
WO2023135505A1 (en) * 2022-01-11 2023-07-20 Novartis Ag Tlr7/8-antagonist for treating sjögren's syndrome or mixed connective tissue disease

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2994895A1 (en) * 2015-08-25 2017-03-02 Beigene, Ltd. Process for preparing parp inhibitor, crystalline forms, and uses thereof
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
MX2020012259A (es) 2021-01-29
EP3793998A1 (en) 2021-03-24
TWI826446B (zh) 2023-12-21
MX2023013584A (es) 2023-11-30
AU2019268583B2 (en) 2022-01-27
AU2019268583A1 (en) 2020-10-29
CN112119078A (zh) 2020-12-22
CA3097312A1 (en) 2019-11-21
JP2021523918A (ja) 2021-09-09
BR112020022738A2 (pt) 2021-02-02
TW202015698A (zh) 2020-05-01
WO2019220390A1 (en) 2019-11-21
JP2024037930A (ja) 2024-03-19
KR20210013554A (ko) 2021-02-04
JP7407740B2 (ja) 2024-01-04
AR117573A1 (es) 2021-08-18
US20210206783A1 (en) 2021-07-08

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