ES2572652T3 - Nuevas formas de un compuesto multicíclico - Google Patents

Nuevas formas de un compuesto multicíclico Download PDF

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Publication number
ES2572652T3
ES2572652T3 ES10750210.6T ES10750210T ES2572652T3 ES 2572652 T3 ES2572652 T3 ES 2572652T3 ES 10750210 T ES10750210 T ES 10750210T ES 2572652 T3 ES2572652 T3 ES 2572652T3
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ES
Spain
Prior art keywords
new forms
compound
multicyclic compound
theta
degrees
Prior art date
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Active
Application number
ES10750210.6T
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English (en)
Inventor
Stephen Bierlmaier
Michael Christie
Laurent Courvoisier
R. Scott Field
R. Curtis Haltiwanger
Linli He
Martin J. Jacobs
Michael Kress
Robert E. Mckean
Dale R. Mowrey
Joseph Petraitis
Mehran Yazdanian
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Cephalon LLC
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Cephalon LLC
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Publication date
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Application filed by Cephalon LLC filed Critical Cephalon LLC
Application granted granted Critical
Publication of ES2572652T3 publication Critical patent/ES2572652T3/es
Active legal-status Critical Current
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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Steroid Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
  • Addition Polymer Or Copolymer, Post-Treatments, Or Chemical Modifications (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Forma cristalina del Compuesto I que tiene la Fórmula**Fórmula** en donde la forma cristalina es: (A) a. la Forma A0 se caracteriza por un patrón de difracción de rayos X de polvo que comprende uno o más de los siguientes picos: 4.32, 6.07, 8.55, 12.07 y 15.37 ± 0.2 grados 2-theta; o (B) a. la Forma HC0 se caracteriza por un patrón de difracción de rayos X de polvo que comprende uno o más de los siguientes picos: 8.36, 8.71, 16.69, 17.39 y 24.59 ± 0.2 grados 2-theta; o b. la Forma HD0 se caracteriza por un patrón de difracción de rayos X de polvo que comprende uno o más de los siguientes picos: 7.60, 8.99 y 15.16 ± 0.2 grados 2-theta; o una mezcla de estos.

Description

imagen1
imagen2
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(Continúa)
Disolvente
Formas obtenidas por XRPD
Diisopropil éter
A0, HA0, HC0, HD0
Dimetilsulfóxido
HC0, HD0
Etanol
S40
Acetato de etilo
A0, HC0, HD0
Formiato de etilo
HA0
Etilenglicol
S60
Heptano
A0, HC0, HD0
Isobutanol
S120, HD0
Acetato de isopropilo
A0, HC0, HD0
Metanol
S20
Metoxibenceno
HD0
Acetato de metilo
A0, HA0, HC0, HD0
Metil isobutil cetona
A0, HC0, HD0
Metil terc-butil éter
A0, HA0, HC0, HD0
N,N-dimetilacetamida
S100
N,N-dimetilformamida
S50
Acetato de N-butilo
A0, HC0, HD0
Propanonitrilo
A0, HA0, HC0, HD0
Carbonato de propileno
A0, HC0, HD0
Piridina
S70
Terc-butanol
A0, HC0, HD0
Tetrahidrofurano
A0, HC0, HD0
Tetrahidropirano
HC0, HD0
Tolueno
A0, HC0, HD0
Trietilamina
HC0, HD0
Agua
A0, HA0, HC0, HD0
Xileno
A0, HA0, BC0, HD0

Tabla 16: Datos de la caracterización de las formas aisladas del Compuesto I
5
10
15
20
25
30
35
40
El tamizaje de polimorfos del Compuesto I rindió catorce formas y una nueva forma (Forma B0) obtenidas solo al 45 calentar los hidratos por encima de 120 °C. Un resumen de los resultados de las formas aisladas se muestra en la Tabla 16más abajo.
EstabilidadEstabilidad física
50 TGA química (HPLC DVS % del XRPD
(XRPD después
(pérdida de después de 4 aumento en después del PurezaForma XRPD DSC de 4 semanas a peso 25 °C semanas a 40 masa a 90 análisis de (%)
40 °C/75 % de
a 150 °C) °C/75 % de HR (%% de HR DVS
HR)
de Área) 55
Endoterma Sin cambios Sin cambios
A0 Cristalina de fusión a 0.07 % 99.0 0.1 99.2
significativos significativos239.7 °C
Endoterma 60 B0 Cristalina defusióna -----
199.8 °C
21
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imagen21
imagen22
imagen23
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imagen28
imagen29
imagen30
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imagen32
imagen33
imagen34

Claims (1)

  1. imagen1
ES10750210.6T 2009-08-26 2010-08-25 Nuevas formas de un compuesto multicíclico Active ES2572652T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US237180P 2000-10-03
US23718009P 2009-08-26 2009-08-26
PCT/US2010/046671 WO2011028580A1 (en) 2009-08-26 2010-08-25 Novel forms of a multicyclic compound

Publications (1)

Publication Number Publication Date
ES2572652T3 true ES2572652T3 (es) 2016-06-01

Family

ID=43033463

Family Applications (1)

Application Number Title Priority Date Filing Date
ES10750210.6T Active ES2572652T3 (es) 2009-08-26 2010-08-25 Nuevas formas de un compuesto multicíclico

Country Status (19)

Country Link
US (1) US8633314B2 (es)
EP (1) EP2470540B1 (es)
JP (3) JP2013503173A (es)
KR (1) KR20120092100A (es)
CN (1) CN102482282A (es)
AU (1) AU2010289746B2 (es)
BR (1) BR112012004053A2 (es)
CA (1) CA2772328C (es)
CL (1) CL2012000478A1 (es)
DK (1) DK2470540T3 (es)
EA (1) EA020756B1 (es)
ES (1) ES2572652T3 (es)
IL (1) IL218132B (es)
MX (1) MX2012002456A (es)
MY (1) MY156873A (es)
NZ (1) NZ598883A (es)
SG (1) SG178852A1 (es)
UA (1) UA110604C2 (es)
WO (1) WO2011028580A1 (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2572652T3 (es) * 2009-08-26 2016-06-01 Cephalon, Inc. Nuevas formas de un compuesto multicíclico
RU2017120655A (ru) * 2014-11-26 2018-12-14 Сефалон, Инк. Кристаллические формы ингибиторов parp
KR20230042136A (ko) 2016-06-29 2023-03-27 테사로, 인코포레이티드 난소암의 치료 방법
BR112019020211A2 (pt) 2017-03-27 2020-04-22 Tesaro, Inc. composições de niraparib
KR20250016494A (ko) 2017-09-26 2025-02-03 테사로, 인코포레이티드 니라파립 제제
CN109632555B (zh) * 2018-12-28 2021-07-27 上海新黄河制药有限公司 一种富马酸福莫特罗无定型含量的动态蒸汽吸附分析方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060276497A1 (en) * 2000-05-09 2006-12-07 Cephalon, Inc. Novel multicyclic compounds and the use thereof
US7122679B2 (en) 2000-05-09 2006-10-17 Cephalon, Inc. Multicyclic compounds and the use thereof
CN101316592A (zh) * 2005-08-24 2008-12-03 伊诺泰克制药公司 茚并异喹啉酮类似物及其用法
CN101784268B (zh) * 2006-11-20 2013-06-19 赛福伦公司 使用辐射敏化剂使肿瘤对辐射敏化的方法
ES2572652T3 (es) * 2009-08-26 2016-06-01 Cephalon, Inc. Nuevas formas de un compuesto multicíclico

Also Published As

Publication number Publication date
DK2470540T3 (en) 2016-08-01
EP2470540B1 (en) 2016-04-20
KR20120092100A (ko) 2012-08-20
MY156873A (en) 2016-04-15
CL2012000478A1 (es) 2012-11-05
MX2012002456A (es) 2012-05-08
AU2010289746B2 (en) 2016-07-07
IL218132B (en) 2018-02-28
CN102482282A (zh) 2012-05-30
BR112012004053A2 (pt) 2020-12-08
JP2013503173A (ja) 2013-01-31
EA020756B1 (ru) 2015-01-30
EP2470540A1 (en) 2012-07-04
NZ598883A (en) 2014-09-26
HK1171750A1 (zh) 2013-04-05
IL218132A0 (en) 2012-06-28
CA2772328C (en) 2017-06-20
SG178852A1 (en) 2012-04-27
AU2010289746A1 (en) 2012-04-12
CA2772328A1 (en) 2011-03-10
JP2016014029A (ja) 2016-01-28
WO2011028580A1 (en) 2011-03-10
JP2018035158A (ja) 2018-03-08
US20120214998A1 (en) 2012-08-23
EA201270315A1 (ru) 2012-08-30
UA110604C2 (uk) 2016-01-25
US8633314B2 (en) 2014-01-21

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