AU2011240773C1 - Methods for producing viloxazine salts and novel polymorphs thereof - Google Patents

Methods for producing viloxazine salts and novel polymorphs thereof Download PDF

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Publication number
AU2011240773C1
AU2011240773C1 AU2011240773A AU2011240773A AU2011240773C1 AU 2011240773 C1 AU2011240773 C1 AU 2011240773C1 AU 2011240773 A AU2011240773 A AU 2011240773A AU 2011240773 A AU2011240773 A AU 2011240773A AU 2011240773 C1 AU2011240773 C1 AU 2011240773C1
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Prior art keywords
viloxazine
solvent
base
substituted
vol
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AU2011240773B2 (en
AU2011240773A1 (en
Inventor
Padmanabh P. Bhatt
David Dain
Likan Liang
Reynold Mariaux
Aleksandr Pechenov
Jean-Philippe Taquet
Alexei Tchesnokov
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Supernus Pharmaceuticals Inc
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Supernus Pharmaceuticals Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/04—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
    • C07C215/06—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic
    • C07C215/08—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with only one hydroxy group and one amino group bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/02—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C217/04—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C217/28—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having one amino group and at least two singly-bound oxygen atoms, with at least one being part of an etherified hydroxy group, bound to the carbon skeleton, e.g. ethers of polyhydroxy amines
    • C07C217/30—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having one amino group and at least two singly-bound oxygen atoms, with at least one being part of an etherified hydroxy group, bound to the carbon skeleton, e.g. ethers of polyhydroxy amines having the oxygen atom of at least one of the etherified hydroxy groups further bound to a carbon atom of a six-membered aromatic ring
    • C07C217/32—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having one amino group and at least two singly-bound oxygen atoms, with at least one being part of an etherified hydroxy group, bound to the carbon skeleton, e.g. ethers of polyhydroxy amines having the oxygen atom of at least one of the etherified hydroxy groups further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted
    • C07C217/34—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having one amino group and at least two singly-bound oxygen atoms, with at least one being part of an etherified hydroxy group, bound to the carbon skeleton, e.g. ethers of polyhydroxy amines having the oxygen atom of at least one of the etherified hydroxy groups further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted by halogen atoms, by trihalomethyl, nitro or nitroso groups, or by singly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C07D265/32—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Addiction (AREA)
  • Anesthesiology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Catalysts (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AU2011240773A 2010-04-12 2011-04-12 Methods for producing viloxazine salts and novel polymorphs thereof Active AU2011240773C1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US32315110P 2010-04-12 2010-04-12
US61/323,151 2010-04-12
PCT/US2011/032013 WO2011130194A2 (en) 2010-04-12 2011-04-12 Methods for producing viloxazine salts and novel polymorphs thereof

Publications (3)

Publication Number Publication Date
AU2011240773A1 AU2011240773A1 (en) 2012-11-01
AU2011240773B2 AU2011240773B2 (en) 2015-04-02
AU2011240773C1 true AU2011240773C1 (en) 2015-08-27

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AU2011240773A Active AU2011240773C1 (en) 2010-04-12 2011-04-12 Methods for producing viloxazine salts and novel polymorphs thereof

Country Status (8)

Country Link
US (7) US9403783B2 (https=)
EP (1) EP2558437B1 (https=)
JP (5) JP6196551B2 (https=)
AU (1) AU2011240773C1 (https=)
CA (4) CA3215310A1 (https=)
ES (1) ES2552166T3 (https=)
MX (5) MX347218B (https=)
WO (1) WO2011130194A2 (https=)

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MX347218B (es) * 2010-04-12 2017-04-20 Supernus Pharmaceuticals Inc Metodos para producir sales de viloxazina y polimorfos novedosos de las mismas.
CN110799191B (zh) 2017-06-16 2023-05-26 贝塔制药有限公司 N-(2-(2-(二甲氨基)乙氧基)-4-甲氧基-5-((4-(1-甲基-1h-吲哚-3-基)嘧啶-2-基)氨基)苯基)丙烯酰胺及其盐的药物制剂
CN108760719A (zh) * 2018-08-17 2018-11-06 北京理工大学 一种利用拉曼光谱分析cl-20的晶型纯度的方法
KR20260023103A (ko) 2021-03-18 2026-02-20 슈퍼너스 파마슈티컬스, 인크. 치환된 몰폴린의 유도체 및 이의 용도
KR20250134715A (ko) * 2022-03-18 2025-09-11 슈퍼너스 파마슈티컬스, 인크. 치환된 몰폴린의 유도체의 제조 방법
WO2023248154A1 (en) * 2022-06-22 2023-12-28 Glenmark Life Sciences Limited Process for the preparation of viloxazine hydrochloride
EP4317141A1 (en) 2022-08-04 2024-02-07 Curia Spain S.A.U. Process and intermediates for the preparation of viloxazine and other 2-substituted morpholine derivatives
CN119707868A (zh) * 2023-09-27 2025-03-28 西安远大科创医药科技有限公司 一种盐酸维洛沙嗪产品杂质及其合成方法与应用
CN119707851A (zh) * 2023-09-27 2025-03-28 西安远大科创医药科技有限公司 一种盐酸维洛沙嗪产品杂质及其合成方法与应用
KR20250094621A (ko) * 2023-12-18 2025-06-25 주식회사 아스트로젠 (s)-빌록사진 또는 이의 염의 개선된 제조 방법
WO2025219523A1 (en) 2024-04-19 2025-10-23 Cambrex Profarmaco Milano S.R.L. "intermediates and processes for the preparation of viloxazine"

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Also Published As

Publication number Publication date
MX357613B (es) 2018-07-17
WO2011130194A2 (en) 2011-10-20
CA2795408C (en) 2018-03-13
CA2992219A1 (en) 2011-10-20
JP2016006062A (ja) 2016-01-14
ES2552166T3 (es) 2015-11-26
US20110251198A1 (en) 2011-10-13
WO2011130194A3 (en) 2012-01-05
US20260008759A1 (en) 2026-01-08
US20190300492A1 (en) 2019-10-03
AU2011240773B2 (en) 2015-04-02
US9434703B2 (en) 2016-09-06
EP2558437A2 (en) 2013-02-20
US10005743B2 (en) 2018-06-26
JP6196551B2 (ja) 2017-09-13
MX2012011821A (es) 2012-11-30
US9403783B2 (en) 2016-08-02
US20180265482A1 (en) 2018-09-20
EP2558437B1 (en) 2015-08-05
CA3126096C (en) 2023-11-21
JP2017039754A (ja) 2017-02-23
US20220024885A1 (en) 2022-01-27
MX347218B (es) 2017-04-20
AU2011240773A1 (en) 2012-11-01
MX357614B (es) 2018-07-17
JP2013530129A (ja) 2013-07-25
CA2795408A1 (en) 2011-10-20
US10160733B2 (en) 2018-12-25
MX355697B (es) 2018-04-27
CA3126096A1 (en) 2011-10-20
US20150126735A1 (en) 2015-05-07
US20160304475A1 (en) 2016-10-20
CA3215310A1 (en) 2011-10-20
JP6663413B2 (ja) 2020-03-11
JP2019194191A (ja) 2019-11-07
JP2018076325A (ja) 2018-05-17

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