AU2016217496B2 - Crystalline forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide - Google Patents

Crystalline forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide Download PDF

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AU2016217496B2
AU2016217496B2 AU2016217496A AU2016217496A AU2016217496B2 AU 2016217496 B2 AU2016217496 B2 AU 2016217496B2 AU 2016217496 A AU2016217496 A AU 2016217496A AU 2016217496 A AU2016217496 A AU 2016217496A AU 2016217496 B2 AU2016217496 B2 AU 2016217496B2
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solvate
crystalline form
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crystalline
accordance
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AU2016217496A1 (en
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Ann Marie Diederich
Philip Anthony Harris
Robert Herrmann
John Kenna
Lara Kathryn LEISTER
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GlaxoSmithKline Intellectual Property Development Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C223/00Compounds containing amino and —CHO groups bound to the same carbon skeleton
    • C07C223/04Compounds containing amino and —CHO groups bound to the same carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/101,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D267/00Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02Seven-membered rings
    • C07D267/08Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/12Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D267/14Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2016217496A 2015-02-13 2016-02-12 Crystalline forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide Ceased AU2016217496B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562115674P 2015-02-13 2015-02-13
US62/115,674 2015-02-13
PCT/IB2016/050755 WO2016128936A1 (en) 2015-02-13 2016-02-12 Crystalline forms of (s)-5-benzyl-n-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4h-1,2,4-triazole-3-carboxamide

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AU2016217496A1 AU2016217496A1 (en) 2017-08-17
AU2016217496B2 true AU2016217496B2 (en) 2019-03-07

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AU2016217496A Ceased AU2016217496B2 (en) 2015-02-13 2016-02-12 Crystalline forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide

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Country Link
US (1) US10287280B2 (enExample)
EP (1) EP3256467A1 (enExample)
JP (1) JP2018505199A (enExample)
KR (1) KR20170117472A (enExample)
CN (1) CN107207485A (enExample)
AU (1) AU2016217496B2 (enExample)
BR (1) BR112017017411A2 (enExample)
CA (1) CA2976172A1 (enExample)
IL (1) IL253731A0 (enExample)
RU (1) RU2017131862A (enExample)
WO (1) WO2016128936A1 (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6754772B2 (ja) 2015-10-23 2020-09-16 武田薬品工業株式会社 複素環化合物
EA201891620A1 (ru) 2016-02-05 2019-02-28 Денали Терапьютикс Инк. Ингибиторы взаимодействующей с рецептором протеинкиназы 1
PL3552017T3 (pl) 2016-12-09 2022-08-08 Denali Therapeutics Inc. Związki użyteczne jako inhibitory RIPK1
WO2019123219A1 (en) * 2017-12-20 2019-06-27 Glaxosmithkline Intellectual Property Development Limited Crystalline salt form of (s)-5-benzyl-n-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4h-1,2,4-triazole-3-carboxamide
WO2019213445A1 (en) 2018-05-03 2019-11-07 Rigel Pharmaceuticals, Inc. Rip1 inhibitory compounds and methods for making and using the same
EA202092580A1 (ru) 2018-05-03 2021-04-07 Ригел Фармасьютикалз, Инк. Соединения, ингибирующие rip1, а также способы их получения и применения
BR112021023040A2 (pt) * 2019-05-17 2021-12-28 Glaxosmithkline Ip Dev Ltd Composição de matriz compreendendo (s)-5-benzil-n-(5- metil-4-oxo-2,3,4,5-tetrahidrobenzo[b][1,4]oxazepin-3-il)-4h-1,2,4- triazol-3-carboxamida
MX2022002718A (es) 2019-09-06 2022-08-10 Rigel Pharmaceuticals Inc Compuestos inhibidores de rip1 y metodos para preparar y usar los mismos.
CN114728958B (zh) 2019-09-06 2025-05-02 里格尔药品股份有限公司 Rip1抑制性化合物和制备与使用其的方法
KR20250095767A (ko) 2019-11-07 2025-06-26 리겔 파마슈티칼스, 인크. 헤테로시클릭 rip1 억제 화합물
AR121717A1 (es) 2020-04-02 2022-06-29 Rigel Pharmaceuticals Inc Inhibidores de rip1k
TWI824259B (zh) 2020-07-01 2023-12-01 美商雷傑製藥公司 Rip1k抑制劑
AR125587A1 (es) 2021-03-11 2023-08-02 Rigel Pharmaceuticals Inc Inhibidores heterocíclicos de la quinasa de rip1
MX2024008648A (es) 2022-01-12 2024-09-23 Denali Therapeutics Inc Formas cristalinas de (s)-5-bencil-n-(5-metil-4-oxo-2,3,4,5-tetrah idropirido [3,2- b][1,4]oxacepin-3-il)-4h-1,2,4-triazol-3-carboxam ida.

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014125444A1 (en) * 2013-02-15 2014-08-21 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014125444A1 (en) * 2013-02-15 2014-08-21 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors

Non-Patent Citations (2)

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Title
BYRN S ET AL, "PHARMACEUTICAL SOLIDS: A STRATEGIC APPROACH TO REGULATORY CONSIDERATIONS", PHARMACEUTICAL RESEARCH, SPRINGER NEW YORK LLC, US, (1995-07-01), vol. 12, no. 7, doi:10.1023/A:1016241927429, ISSN 0724-8741, pages 945 - 954 *
CAIRA, "Crystalline Polymorphism of Organic Compounds", TOPICS IN CURRENT CHEMISTRY, SPRINGER, BERLIN, DE, (1998-01-01), vol. 198, ISSN 0340-1022, pages 163 - 208 *

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Publication number Publication date
US10287280B2 (en) 2019-05-14
AU2016217496A1 (en) 2017-08-17
RU2017131862A (ru) 2019-03-13
CN107207485A (zh) 2017-09-26
WO2016128936A1 (en) 2016-08-18
JP2018505199A (ja) 2018-02-22
RU2017131862A3 (enExample) 2019-06-06
KR20170117472A (ko) 2017-10-23
EP3256467A1 (en) 2017-12-20
US20180022737A1 (en) 2018-01-25
CA2976172A1 (en) 2016-08-18
BR112017017411A2 (pt) 2018-04-03
IL253731A0 (en) 2017-09-28

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