AU2021276912B2 - Crystalline form of LNP023 - Google Patents

Crystalline form of LNP023 Download PDF

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Publication number
AU2021276912B2
AU2021276912B2 AU2021276912A AU2021276912A AU2021276912B2 AU 2021276912 B2 AU2021276912 B2 AU 2021276912B2 AU 2021276912 A AU2021276912 A AU 2021276912A AU 2021276912 A AU2021276912 A AU 2021276912A AU 2021276912 B2 AU2021276912 B2 AU 2021276912B2
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AU
Australia
Prior art keywords
lnp023
hydrochloride
hydrate form
crystalline hydrate
disease
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Active
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AU2021276912A
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English (en)
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AU2021276912A1 (en
Inventor
Zichen JIA
Philipp Lustenberger
Marie Meyer
Massimo MORATTO
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Novartis AG
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Novartis AG
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Publication date
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Publication of AU2021276912A1 publication Critical patent/AU2021276912A1/en
Application granted granted Critical
Publication of AU2021276912B2 publication Critical patent/AU2021276912B2/en
Priority to AU2024201640A priority Critical patent/AU2024201640B2/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Crystals, And After-Treatments Of Crystals (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
AU2021276912A 2020-05-18 2021-05-17 Crystalline form of LNP023 Active AU2021276912B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2024201640A AU2024201640B2 (en) 2020-05-18 2024-03-13 Crystalline form of LNP023

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US202063026637P 2020-05-18 2020-05-18
US63/026,637 2020-05-18
US202063052699P 2020-07-16 2020-07-16
US63/052,699 2020-07-16
PCT/IB2021/054225 WO2021234544A1 (en) 2020-05-18 2021-05-17 Crystalline form of lnp023

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2024201640A Division AU2024201640B2 (en) 2020-05-18 2024-03-13 Crystalline form of LNP023

Publications (2)

Publication Number Publication Date
AU2021276912A1 AU2021276912A1 (en) 2022-11-24
AU2021276912B2 true AU2021276912B2 (en) 2023-12-14

Family

ID=76076387

Family Applications (2)

Application Number Title Priority Date Filing Date
AU2021276912A Active AU2021276912B2 (en) 2020-05-18 2021-05-17 Crystalline form of LNP023
AU2024201640A Active AU2024201640B2 (en) 2020-05-18 2024-03-13 Crystalline form of LNP023

Family Applications After (1)

Application Number Title Priority Date Filing Date
AU2024201640A Active AU2024201640B2 (en) 2020-05-18 2024-03-13 Crystalline form of LNP023

Country Status (10)

Country Link
US (3) US11603363B2 (https=)
EP (1) EP4153580A1 (https=)
JP (3) JP7592743B2 (https=)
KR (2) KR20230009478A (https=)
CN (4) CN120168469A (https=)
AU (2) AU2021276912B2 (https=)
CA (1) CA3180829A1 (https=)
IL (1) IL297975A (https=)
TW (2) TW202504893A (https=)
WO (1) WO2021234544A1 (https=)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI3675854T1 (sl) 2017-08-31 2025-05-30 Novartis Ag Derivati piperidinil-indola za uporabo v zdravljenju glomerulopatije c3
TW202504893A (zh) * 2020-05-18 2025-02-01 瑞士商諾華公司 Lnp023之結晶形式
US11951101B2 (en) 2020-07-16 2024-04-09 Novartis Ag Methods of using factor B inhibitors
WO2022143940A1 (zh) * 2020-12-30 2022-07-07 南京明德新药研发有限公司 一系列哌啶取代的苯酸类化合物及其应用
EP4333845A1 (en) * 2021-05-07 2024-03-13 Novartis AG Iptacopan for the treatment of atypical hemolytic uremic syndrome
WO2022264101A1 (en) 2021-06-18 2022-12-22 Novartis Ag Method of treating an autoimmune hematological disorder
CA3248808A1 (en) 2022-03-04 2023-09-07 Novartis Ag USE OF IPTACOPAN FOR THE TREATMENT OF LUPUS NEPHROPATHY
JP7849520B2 (ja) * 2022-06-30 2026-04-21 江▲蘇▼恒瑞医▲薬▼股▲フン▼有限公司 含窒素架橋複素環誘導体の薬学的に許容される塩、結晶形及びその調製方法
EP4669321A1 (en) 2023-02-23 2025-12-31 Novartis AG METHODS OF USING FACTOR B INHIBITORS
CN121712505A (zh) 2023-08-25 2026-03-20 诺华股份有限公司 使用因子b抑制剂的方法
WO2025148628A1 (zh) * 2024-01-10 2025-07-17 河北以岭医药研究院有限公司 哌啶基吲哚衍生物及其制备方法和应用
WO2025172910A1 (en) 2024-02-16 2025-08-21 Novartis Ag Factor b inhibitors for treatment of anca-associated vasculitis
WO2026003809A1 (en) * 2024-06-29 2026-01-02 Assia Chemical Industries Ltd. Solid state forms of iptacopan hydrochloride

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015009616A1 (en) * 2013-07-15 2015-01-22 Novartis Ag Piperidinyl indole derivatives and their use as complement factor b inhibitors

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0301259D0 (en) 2003-01-20 2003-02-19 Novartis Ag Organic compounds
KR20130086534A (ko) 2010-06-01 2013-08-02 플러스 케미칼스, 에스.에이. 익사베필론의 고체 형태
MX2018007392A (es) 2015-12-23 2018-08-15 Greenovation Biotech Gmbh Polipeptidos para inhibir la activacion del complemento.
SI3675854T1 (sl) 2017-08-31 2025-05-30 Novartis Ag Derivati piperidinil-indola za uporabo v zdravljenju glomerulopatije c3
TW202504893A (zh) * 2020-05-18 2025-02-01 瑞士商諾華公司 Lnp023之結晶形式

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015009616A1 (en) * 2013-07-15 2015-01-22 Novartis Ag Piperidinyl indole derivatives and their use as complement factor b inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
MAINOLFI NELLO ET AL: "Discovery of 4-((2 S ,4 S )-4-Ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), ..", JOURNAL OF MEDICINAL CHEMISTRY, vol. 63, no. 11, 19 February 2020, pages 5697 - 5722 *

Also Published As

Publication number Publication date
JP2024150466A (ja) 2024-10-23
JP2026048795A (ja) 2026-03-17
JP7592743B2 (ja) 2024-12-02
CN120168469A (zh) 2025-06-20
WO2021234544A1 (en) 2021-11-25
AU2024201640B2 (en) 2025-10-09
KR20250048392A (ko) 2025-04-08
IL297975A (en) 2023-01-01
KR20230009478A (ko) 2023-01-17
CN120208923A (zh) 2025-06-27
TW202204335A (zh) 2022-02-01
TWI858258B (zh) 2024-10-11
US20230265067A1 (en) 2023-08-24
US11603363B2 (en) 2023-03-14
JP7789850B2 (ja) 2025-12-22
AU2021276912A1 (en) 2022-11-24
TW202504893A (zh) 2025-02-01
EP4153580A1 (en) 2023-03-29
CA3180829A1 (en) 2021-11-25
AU2024201640A1 (en) 2024-04-04
CN115667240B (zh) 2025-04-22
CN120172955A (zh) 2025-06-20
JP2023518552A (ja) 2023-05-02
CN115667240A (zh) 2023-01-31
US20250270186A1 (en) 2025-08-28
US12384758B2 (en) 2025-08-12
US20210371394A1 (en) 2021-12-02

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