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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
Authority
ES
Spain
Prior art keywords
new forms
compound
multicyclic compound
theta
degrees
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
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
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.)
Cephalon LLC
Original Assignee
Cephalon LLC
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Filing date
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
Anticipated expiration legal-status Critical

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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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Addition Polymer Or Copolymer, Post-Treatments, Or Chemical Modifications (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Steroid Compounds (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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imagen4
imagen5
imagen6
imagen7
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imagen9
imagen10
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imagen16
imagen17
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imagen19
(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
imagen20
imagen21
imagen22
imagen23
imagen24
imagen25
imagen26
imagen27
imagen28
imagen29
imagen30
imagen31
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 (20)

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)
HK (1) HK1171750A1 (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 (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2772328C (en) * 2009-08-26 2017-06-20 Cephalon, Inc. Novel forms of a multicyclic compound
CN107207511A (zh) * 2014-11-26 2017-09-26 赛福伦公司 Parp抑制剂的结晶形式
KR20200014736A (ko) 2017-03-27 2020-02-11 테사로, 인코포레이티드 니라파립 조성물
BR112020006039A2 (pt) 2017-09-26 2020-10-06 Tesaro, Inc. formulações de niraparibe
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
WO2007025009A2 (en) * 2005-08-24 2007-03-01 Inotek Pharmaceuticals Corporation Indenoisoquinolinone analogs and methods of use thereof
AU2007321987B2 (en) 2006-11-20 2014-01-23 Cephalon, Inc. Method of radio-sensitizing tumors using a radio-sensitizing agent
CA2772328C (en) * 2009-08-26 2017-06-20 Cephalon, Inc. Novel forms of a multicyclic compound

Also Published As

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

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