TWI815820B - ２－（５－（４－（２－嗎啉乙氧基）苯基）吡啶－２－基）－ｎ－芐乙醯胺之固態形式 - Google Patents

２－（５－（４－（２－嗎啉乙氧基）苯基）吡啶－２－基）－ｎ－芐乙醯胺之固態形式 Download PDF

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Publication number
TWI815820B
TWI815820B TW107131540A TW107131540A TWI815820B TW I815820 B TWI815820 B TW I815820B TW 107131540 A TW107131540 A TW 107131540A TW 107131540 A TW107131540 A TW 107131540A TW I815820 B TWI815820 B TW I815820B
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Prior art keywords
compound
polymorph
cancer
xrpd
solvent
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TW107131540A
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English (en)
Chinese (zh)
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TW201920160A (zh
Inventor
麥可 史莫林斯基
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美商Ａｔｎｘ特殊目的實體公司
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/56—Amides
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Physics & Mathematics (AREA)
  • Condensed Matter Physics & Semiconductors (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW107131540A 2017-09-07 2018-09-07 ２－（５－（４－（２－嗎啉乙氧基）苯基）吡啶－２－基）－ｎ－芐乙醯胺之固態形式 TWI815820B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762555390P 2017-09-07 2017-09-07
US62/555,390 2017-09-07

Publications (2)

Publication Number Publication Date
TW201920160A TW201920160A (zh) 2019-06-01
TWI815820B true TWI815820B (zh) 2023-09-21

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TW107131540A TWI815820B (zh) 2017-09-07 2018-09-07 ２－（５－（４－（２－嗎啉乙氧基）苯基）吡啶－２－基）－ｎ－芐乙醯胺之固態形式

Country Status (22)

Country Link
US (4) US10669236B2 (https=)
EP (2) EP4674486A3 (https=)
JP (3) JP7843116B2 (https=)
KR (2) KR102691700B1 (https=)
CN (2) CN118439992A (https=)
AU (2) AU2018330163B2 (https=)
BR (1) BR112020004419A2 (https=)
CA (1) CA3074831A1 (https=)
DK (1) DK3679016T3 (https=)
ES (1) ES3056703T3 (https=)
FI (1) FI3679016T3 (https=)
HR (1) HRP20260002T1 (https=)
IL (2) IL326637A (https=)
LT (1) LT3679016T (https=)
MX (2) MX2020002622A (https=)
PL (1) PL3679016T3 (https=)
PT (1) PT3679016T (https=)
RS (1) RS67706B1 (https=)
SG (1) SG11202001868RA (https=)
SM (1) SMT202500467T1 (https=)
TW (1) TWI815820B (https=)
WO (1) WO2019051147A1 (https=)

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* Cited by examiner, † Cited by third party
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US7968574B2 (en) * 2004-12-28 2011-06-28 Kinex Pharmaceuticals, Llc Biaryl compositions and methods for modulating a kinase cascade
EP4186890A1 (en) 2021-11-29 2023-05-31 Moehs Ibérica, S.L. Preparation of n-benzyl-2-(5-bromo-pyridin-2-yl)-acetamide for the synthesis of tirbanibulin
CN115010655A (zh) * 2022-07-21 2022-09-06 重庆迈德凯医药有限公司 一种替尼布林的纯化方法
WO2026022219A1 (en) 2024-07-24 2026-01-29 Almirall, S.A. Injectable formulations comprising tirbanibulin

Citations (1)

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Publication number Priority date Publication date Assignee Title
CN106810490A (zh) * 2017-02-06 2017-06-09 重庆泰润制药有限公司 一种二芳基化合物的晶型及其制备方法和应用

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US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
US7141593B1 (en) * 1999-06-04 2006-11-28 Abbott Laboratories Pharmaceutical formulations
DK1390377T3 (da) * 2001-05-22 2006-06-19 Pfizer Prod Inc Ny krystalform af azithromycin
US6821502B2 (en) * 2002-06-12 2004-11-23 Chevron U.S.A. Inc. Method of making aluminum-containing zeolite with IFR structure
US7351833B2 (en) * 2004-07-23 2008-04-01 Abbott Laboratories (1S,5S)-3-(5,6-dichloropyridin-3-yl)-3,6-diazabicyclo[3.2.0]heptane benzenesulfonate
US7968574B2 (en) 2004-12-28 2011-06-28 Kinex Pharmaceuticals, Llc Biaryl compositions and methods for modulating a kinase cascade
BRPI0519424B8 (pt) 2004-12-28 2021-05-25 Athenex Inc compostos, composição e uso dos ditos compostos para a preparação de um medicamento para prevenção ou tratamento de um distúrbio de proliferação celular ou infecção microbiana
MY152185A (en) * 2005-06-10 2014-08-29 Novartis Ag Modified release 1-[(3-hydroxy-adamant-1-ylamino)-acetyl]-pyrrolidine-2(s)-carbonitrile formulation
BRPI0605937A2 (pt) * 2005-09-13 2009-05-26 Sicor Inc processo para a sìntese de brometo de rocurÈnio
WO2008002676A2 (en) * 2006-06-29 2008-01-03 Kinex Pharmaceuticals, Llc Biaryl compositions and methods for modulating a kinase cascade
WO2008039421A2 (en) * 2006-09-28 2008-04-03 Merck & Co., Inc. Pharmaceutical compositions of hdac inhibitors and chelatable metal compounds, and metal-hdac inhibitor chelate complexes
US7837978B2 (en) * 2006-10-13 2010-11-23 Chevron U.S.A. Inc. Process for preparing aluminum-containing molecular sieve SSZ-26
PE20081506A1 (es) * 2006-12-12 2008-12-09 Infinity Discovery Inc Formulaciones de ansamicina
US7939529B2 (en) 2007-05-17 2011-05-10 Kinex Pharmaceuticals, Llc Process for the preparation of compositions for modulating a kinase cascade and methods of use thereof
TWI457336B (zh) * 2006-12-28 2014-10-21 Kinex Pharmaceuticals Llc 調節激酶級聯之組成物及方法
US7935697B2 (en) 2006-12-28 2011-05-03 Kinex Pharmaceuticals, Llc Compositions for modulating a kinase cascade and methods of use thereof
JP2010527996A (ja) * 2007-05-22 2010-08-19 ウルティモルフィクス・テクノロジーズ・ベー・フェー テノホビルジソプロキシル−ヘミフマル酸共結晶
WO2015069217A1 (en) * 2013-11-05 2015-05-14 Baylor College Of Medicine Src kinase inhibition as treatment for lympangioleiomyomatosis and tuberous sclerosis
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Patent Citations (1)

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CN106810490A (zh) * 2017-02-06 2017-06-09 重庆泰润制药有限公司 一种二芳基化合物的晶型及其制备方法和应用

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Publication number Publication date
RU2020112539A (ru) 2021-10-08
TW201920160A (zh) 2019-06-01
KR20240119192A (ko) 2024-08-06
EP3679016B1 (en) 2025-11-05
RU2020112539A3 (https=) 2022-04-19
US11230527B2 (en) 2022-01-25
HRP20260002T1 (hr) 2026-02-27
SG11202001868RA (en) 2020-03-30
KR102691700B1 (ko) 2024-08-02
US20250115555A1 (en) 2025-04-10
US20190071402A1 (en) 2019-03-07
AU2023201010A1 (en) 2023-03-23
JP7843116B2 (ja) 2026-04-09
PT3679016T (pt) 2025-12-05
EP4674486A3 (en) 2026-03-25
KR20200081359A (ko) 2020-07-07
US12215083B2 (en) 2025-02-04
CN111278808B (zh) 2024-04-26
BR112020004419A2 (pt) 2020-09-08
AU2018330163B2 (en) 2023-02-02
DK3679016T3 (da) 2025-12-15
CN118439992A (zh) 2024-08-06
EP4674486A2 (en) 2026-01-07
AU2023201010B2 (en) 2024-10-03
WO2019051147A1 (en) 2019-03-14
AU2018330163A1 (en) 2020-03-26
US20200255380A1 (en) 2020-08-13
PL3679016T3 (pl) 2026-03-02
ES3056703T3 (en) 2026-02-24
CN111278808A (zh) 2020-06-12
FI3679016T3 (fi) 2025-12-12
LT3679016T (lt) 2026-02-10
US20220098152A1 (en) 2022-03-31
JP2020533412A (ja) 2020-11-19
MX2023001805A (es) 2023-03-13
JP2025131661A (ja) 2025-09-09
EP3679016A4 (en) 2021-09-29
IL326637A (en) 2026-04-01
US10669236B2 (en) 2020-06-02
IL272992A (en) 2020-04-30
JP2023157909A (ja) 2023-10-26
SMT202500467T1 (it) 2026-03-09
CA3074831A1 (en) 2019-03-14
MX2020002622A (es) 2020-10-01
RS67706B1 (sr) 2026-02-27
EP3679016A1 (en) 2020-07-15

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