AU2016211246B2 - Crystalline forms of C21H22CI2N4O2 - Google Patents

Crystalline forms of C21H22CI2N4O2 Download PDF

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Publication number
AU2016211246B2
AU2016211246B2 AU2016211246A AU2016211246A AU2016211246B2 AU 2016211246 B2 AU2016211246 B2 AU 2016211246B2 AU 2016211246 A AU2016211246 A AU 2016211246A AU 2016211246 A AU2016211246 A AU 2016211246A AU 2016211246 B2 AU2016211246 B2 AU 2016211246B2
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AU
Australia
Prior art keywords
crystalline
present
compound
isopropylaminopyridin
pyrrole
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.)
Active
Application number
AU2016211246A
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English (en)
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AU2016211246A1 (en
Inventor
Rossitza Gueorguieva Alargova
Alexander Aronov
Stephan X.M. BOERRIGTER
Gary Decrescenzo
Irina Nikolaevna Kadiyala
Ali Keshavarz-Shokri
Benjamin Littler
Alexander N. SCANGAS
Kathy Stavropoulos
Petinka I. Vlahova
Dean WELSCH
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Vertex Pharmaceuticals Inc
Biomed Valley Discoveries Inc
Original Assignee
Vertex Pharmaceuticals Inc
Biomed Valley Discoveries Inc
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 Vertex Pharmaceuticals Inc, Biomed Valley Discoveries Inc filed Critical Vertex Pharmaceuticals Inc
Publication of AU2016211246A1 publication Critical patent/AU2016211246A1/en
Application granted granted Critical
Publication of AU2016211246B2 publication Critical patent/AU2016211246B2/en
Priority to AU2020257041A priority Critical patent/AU2020257041C1/en
Priority to AU2022228084A priority patent/AU2022228084B2/en
Priority to AU2023254937A priority patent/AU2023254937B2/en
Priority to AU2025263912A priority patent/AU2025263912A1/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • 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
    • C07B2200/07—Optical isomers
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Developing Agents For Electrophotography (AREA)
  • Crystals, And After-Treatments Of Crystals (AREA)
  • Removal Of Specific Substances (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
AU2016211246A 2015-01-30 2016-01-29 Crystalline forms of C21H22CI2N4O2 Active AU2016211246B2 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
AU2020257041A AU2020257041C1 (en) 2015-01-30 2020-10-20 Crystalline forms of C21H22CI2N4O2
AU2022228084A AU2022228084B2 (en) 2015-01-30 2022-09-05 CRYSTALLINE FORMS OF C21H22Cl2N4O2
AU2023254937A AU2023254937B2 (en) 2015-01-30 2023-10-25 Crystalline forms of C21H22CI2N4O2
AU2025263912A AU2025263912A1 (en) 2015-01-30 2025-11-10 Crystalline forms of C21H22CI2N4O2

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562110449P 2015-01-30 2015-01-30
US62/110,449 2015-01-30
PCT/US2016/015829 WO2016123574A1 (en) 2015-01-30 2016-01-29 Crystalline forms of c21h22ci2n4o2

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2020257041A Division AU2020257041C1 (en) 2015-01-30 2020-10-20 Crystalline forms of C21H22CI2N4O2

Publications (2)

Publication Number Publication Date
AU2016211246A1 AU2016211246A1 (en) 2017-08-10
AU2016211246B2 true AU2016211246B2 (en) 2020-08-27

Family

ID=56544441

Family Applications (5)

Application Number Title Priority Date Filing Date
AU2016211246A Active AU2016211246B2 (en) 2015-01-30 2016-01-29 Crystalline forms of C21H22CI2N4O2
AU2020257041A Active AU2020257041C1 (en) 2015-01-30 2020-10-20 Crystalline forms of C21H22CI2N4O2
AU2022228084A Active AU2022228084B2 (en) 2015-01-30 2022-09-05 CRYSTALLINE FORMS OF C21H22Cl2N4O2
AU2023254937A Active AU2023254937B2 (en) 2015-01-30 2023-10-25 Crystalline forms of C21H22CI2N4O2
AU2025263912A Pending AU2025263912A1 (en) 2015-01-30 2025-11-10 Crystalline forms of C21H22CI2N4O2

Family Applications After (4)

Application Number Title Priority Date Filing Date
AU2020257041A Active AU2020257041C1 (en) 2015-01-30 2020-10-20 Crystalline forms of C21H22CI2N4O2
AU2022228084A Active AU2022228084B2 (en) 2015-01-30 2022-09-05 CRYSTALLINE FORMS OF C21H22Cl2N4O2
AU2023254937A Active AU2023254937B2 (en) 2015-01-30 2023-10-25 Crystalline forms of C21H22CI2N4O2
AU2025263912A Pending AU2025263912A1 (en) 2015-01-30 2025-11-10 Crystalline forms of C21H22CI2N4O2

Country Status (12)

Country Link
US (6) US9676746B2 (enExample)
EP (2) EP3250562B1 (enExample)
JP (5) JP7258460B2 (enExample)
CN (2) CN116854662A (enExample)
AU (5) AU2016211246B2 (enExample)
CA (3) CA3218488A1 (enExample)
ES (1) ES3009552T3 (enExample)
HK (1) HK1244274A1 (enExample)
MX (1) MX382289B (enExample)
NZ (2) NZ734041A (enExample)
SG (2) SG11201705924RA (enExample)
WO (1) WO2016123574A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015095842A2 (en) * 2013-12-20 2015-06-25 Biomed Valley Discoveries, Inc. Methods and compositions for treating non-erk mapk pathway inhibitor-resistant cancers
SG11201705924RA (en) 2015-01-30 2017-08-30 Biomed Valley Discoveries Inc CRYSTALLINE FORMS OF C<sb>21</sb>H<sb>22</sb>CI<sb>2</sb>N<sb>4</sb>O<sb>2</sb>
MX380123B (es) * 2016-01-27 2025-03-11 Jiangsu Hengrui Medicine Co Metodo para preparar una composicion farmaceutica que comprende un derivado de quinolina o una sal del mismo.
US10172862B2 (en) * 2017-01-30 2019-01-08 Oncoceutics, Inc. Imipridones for gliomas
WO2021020841A1 (en) * 2019-07-29 2021-02-04 Standigm Inc. Composition for preventing or treating metabolic liver disease
US20230024584A1 (en) * 2019-11-20 2023-01-26 University Of Kentucky Research Foundation Anti-cancer compositions and methods
CN118765276A (zh) * 2022-03-08 2024-10-11 甘李药业股份有限公司 氘代化合物，及其制备方法和应用
WO2023183905A2 (en) * 2022-03-24 2023-09-28 Biomed Valley Discoveries, Inc. Deuterated analogs of pyrrole inhibitors of erk, synthesis thereof and intermediates thereto

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7354939B2 (en) * 2004-05-14 2008-04-08 Vertex Pharmaceuticals Incorporated Pyrrole inhibitors of ERK protein kinase, synthesis thereof and intermediates thereto

Family Cites Families (13)

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US4599331A (en) 1984-12-24 1986-07-08 Syntex (U.S.A.) Inc. Etianic acids as antiangiogenics
EP0245357B1 (en) 1985-10-23 1991-08-07 The Upjohn Company Angiostatic steroids
US4771042A (en) 1985-11-25 1988-09-13 The Upjohn Company Inhibition of angiogenesis involving the coadministration of steroids with heparin or heparin fragments
EP0477195A1 (en) 1989-06-16 1992-04-01 The Upjohn Company Suramin type compounds and angiostatic steroids to inhibit angiogenesis
AU678961B2 (en) 1991-11-22 1997-06-19 Alcon Laboratories, Inc. Angiostatic steroids
JP4783532B2 (ja) * 2000-02-05 2011-09-28 バーテックス ファーマシューティカルズ インコーポレイテッド Ｅｒｋのインヒビターとして有用なピラゾール組成物
US7927613B2 (en) 2002-02-15 2011-04-19 University Of South Florida Pharmaceutical co-crystal compositions
EP1506189A1 (en) * 2002-04-26 2005-02-16 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as inhibitors of erk2 and uses thereof
US7582623B2 (en) 2004-05-20 2009-09-01 The Regents Of The University Of California Photoactive metal nitrosyls for blood pressure regulation and cancer therapy
CN103951583B (zh) 2006-12-06 2016-01-06 科内图斯医药公司 一种抑制剂的结晶形式
JP6362601B2 (ja) * 2012-09-18 2018-07-25 オースペックス・ファーマシューティカルズ・インコーポレイテッドＡｕｓｐｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． 小胞モノアミン輸送体２の重水素化ベンゾキノリン阻害剤の製剤薬物動態
US9227969B2 (en) * 2013-08-14 2016-01-05 Novartis Ag Compounds and compositions as inhibitors of MEK
SG11201705924RA (en) 2015-01-30 2017-08-30 Biomed Valley Discoveries Inc CRYSTALLINE FORMS OF C<sb>21</sb>H<sb>22</sb>CI<sb>2</sb>N<sb>4</sb>O<sb>2</sb>

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7354939B2 (en) * 2004-05-14 2008-04-08 Vertex Pharmaceuticals Incorporated Pyrrole inhibitors of ERK protein kinase, synthesis thereof and intermediates thereto

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
"Certificate of Analysis: Ulixertinib (Hydrochloride)", CHEMIETEK, (2014), URL: http://www.chemietek.com/ ProductFiles/Coa/Ulixertinib,%20(HCl%20salt),%20Lot%2001,%20Certificate%20of% 20Analysis.pdf, (2016-03-19) *

Also Published As

Publication number Publication date
CA2975048A1 (en) 2016-08-04
EP4477222A2 (en) 2024-12-18
AU2020257041A1 (en) 2020-11-12
JP7258460B2 (ja) 2023-04-17
US9676746B2 (en) 2017-06-13
AU2023254937B2 (en) 2025-08-14
JP2023096080A (ja) 2023-07-06
ES3009552T3 (en) 2025-03-27
AU2023254937A1 (en) 2023-11-16
NZ783866A (en) 2025-03-28
US11390600B2 (en) 2022-07-19
US20220324832A1 (en) 2022-10-13
EP3250562A1 (en) 2017-12-06
NZ772411A (en) 2022-05-27
US12187698B2 (en) 2025-01-07
JP2022033866A (ja) 2022-03-02
US20170320851A1 (en) 2017-11-09
NZ783808A (en) 2025-03-28
US20190127348A1 (en) 2019-05-02
AU2022228084B2 (en) 2023-11-16
SG11201705924RA (en) 2017-08-30
AU2025263912A1 (en) 2025-12-04
SG10202101979TA (en) 2021-04-29
AU2020257041B2 (en) 2022-06-23
EP4477222A3 (en) 2025-02-26
CN107406413A (zh) 2017-11-28
US10738027B2 (en) 2020-08-11
MX382289B (es) 2025-03-13
CA3218488A1 (en) 2016-08-04
NZ734041A (en) 2022-02-25
US10183927B2 (en) 2019-01-22
HK1244274A1 (zh) 2018-08-03
CA3308777A1 (en) 2026-05-13
US20160221987A1 (en) 2016-08-04
EP3250562B1 (en) 2024-11-27
JP2020100674A (ja) 2020-07-02
CA2975048C (en) 2024-01-02
CN116854662A (zh) 2023-10-10
WO2016123574A1 (en) 2016-08-04
US20200339531A1 (en) 2020-10-29
AU2016211246A1 (en) 2017-08-10
JP2025089464A (ja) 2025-06-12
AU2020257041C1 (en) 2022-10-27
US20250084059A1 (en) 2025-03-13
EP3250562A4 (en) 2018-07-11
MX2017009696A (es) 2017-10-23
AU2022228084A1 (en) 2022-09-29
JP2018503649A (ja) 2018-02-08

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