TWI365188B - Polymorphic and amorphous forms of the phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}}-1,3,4,5-tetrahydro-6h-azepino[5,4,3-cd]indol-6-one - Google Patents

Polymorphic and amorphous forms of the phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}}-1,3,4,5-tetrahydro-6h-azepino[5,4,3-cd]indol-6-one

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Publication number
TWI365188B
TWI365188B TW094132634A TW94132634A TWI365188B TW I365188 B TWI365188 B TW I365188B TW 094132634 A TW094132634 A TW 094132634A TW 94132634 A TW94132634 A TW 94132634A TW I365188 B TWI365188 B TW I365188B
Authority
TW
Taiwan
Prior art keywords
azepino
indol
polymorphic
methylamino
tetrahydro
Prior art date
Application number
TW094132634A
Other languages
English (en)
Chinese (zh)
Other versions
TW200613305A (en
Inventor
Jia Liu
Naresh Nayyar
Ming Guo
Zhen-Ping Wu
Bennett Chaplin Borer
Aparna Nadig Srirangam
Mark Bryan Mitchell
Yi Li
Jan-Jon Chu
Original Assignee
Pfizer
Cancer Rec Tech Ltd
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 Pfizer, Cancer Rec Tech Ltd filed Critical Pfizer
Publication of TW200613305A publication Critical patent/TW200613305A/zh
Application granted granted Critical
Publication of TWI365188B publication Critical patent/TWI365188B/zh

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    • 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
    • C07D487/06—Peri-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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P41/00—Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW094132634A 2004-09-22 2005-09-21 Polymorphic and amorphous forms of the phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}}-1,3,4,5-tetrahydro-6h-azepino[5,4,3-cd]indol-6-one TWI365188B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US61245904P 2004-09-22 2004-09-22
US67929605P 2005-05-09 2005-05-09

Publications (2)

Publication Number Publication Date
TW200613305A TW200613305A (en) 2006-05-01
TWI365188B true TWI365188B (en) 2012-06-01

Family

ID=35526956

Family Applications (1)

Application Number Title Priority Date Filing Date
TW094132634A TWI365188B (en) 2004-09-22 2005-09-21 Polymorphic and amorphous forms of the phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}}-1,3,4,5-tetrahydro-6h-azepino[5,4,3-cd]indol-6-one

Country Status (17)

Country Link
US (1) US7268126B2 (enExample)
EP (1) EP1799685B1 (enExample)
JP (1) JP2008513436A (enExample)
KR (1) KR100853601B1 (enExample)
AR (1) AR051296A1 (enExample)
AT (1) ATE551345T1 (enExample)
AU (1) AU2005286191B2 (enExample)
BR (1) BRPI0516766A (enExample)
CA (1) CA2581025C (enExample)
ES (1) ES2382950T3 (enExample)
IL (1) IL181463A (enExample)
MX (1) MX2007002461A (enExample)
NO (1) NO337938B1 (enExample)
NZ (1) NZ554659A (enExample)
RU (1) RU2355691C2 (enExample)
TW (1) TWI365188B (enExample)
WO (1) WO2006033007A2 (enExample)

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EP1611137A1 (en) * 2003-03-31 2006-01-04 Pfizer Inc. Salts of tricyclic inhibitors of poly(adp-ribose) polymerases
US8425929B2 (en) * 2004-04-30 2013-04-23 Allergan, Inc. Sustained release intraocular implants and methods for preventing retinal dysfunction
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US20100279327A1 (en) * 2006-06-12 2010-11-04 Bipar Sciences, Inc. Method of treating diseases with parp inhibitors
AU2007292306A1 (en) * 2006-09-05 2008-03-13 Bipar Sciences, Inc. Inhibition of fatty acid synthesis by PARP inhibitors and methods of treatment thereof
AU2007292387A1 (en) * 2006-09-05 2008-03-13 Bipar Sciences, Inc. Treatment of cancer
WO2008114114A2 (en) * 2007-03-16 2008-09-25 Pfizer Products Inc. Poly(adp-ribose) polymerases inhibitor for treating ophthalmic condition
NZ586123A (en) * 2007-11-12 2012-12-21 Bipar Sciences Inc Treatment of ovarian cancer with 4-iodo-3-nitrobenzamide in combination with topoisomerase inhibitors
KR20100102609A (ko) * 2007-11-12 2010-09-24 바이파 사이언스 인코포레이티드 Ｐａｒｐ 억제제를 단독으로 사용하거나 항종양제와 병용하여 유방암을 치료하는 방법
CA2708157A1 (en) * 2007-12-07 2009-06-11 Bipar Sciences, Inc. Treatment of cancer with combinations of topoisomerase inhibitors and parp inhibitors
KR20100112192A (ko) * 2008-02-04 2010-10-18 바이파 사이언스 인코포레이티드 Ｐａｒｐ－매개된 질병을 진단 및 치료하는 방법
KR20170095402A (ko) 2009-11-09 2017-08-22 알러간, 인코포레이티드 모발 성장을 촉진하기 위한 조성물 및 방법
CA3024216C (en) 2010-02-12 2021-03-30 Pfizer Inc. Salts and polymorphs of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6h-azepino[5,4,3-cd]indol-6-one
WO2011141909A2 (en) 2010-05-10 2011-11-17 Radikal Therapeutics Inc. Lipoic acid and nitroxide derivatives and uses thereof
AU2014216112B2 (en) 2013-02-15 2019-02-21 Allergan, Inc. Sustained drug delivery implant
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US10875870B2 (en) 2017-01-24 2020-12-29 Assia Chemical Industries Ltd. Solid state forms of rucaparib and of rucaparib salts
WO2018162439A1 (en) 2017-03-08 2018-09-13 Onxeo New predictive biomarker for the sensitivity to a treatment of cancer with a dbait molecule
CN110997068B (zh) 2017-05-24 2022-12-06 宾夕法尼亚大学董事会 用于成像和放射疗法的经放射标记的荧光parp抑制剂
MX2020004545A (es) * 2017-11-03 2020-08-03 Sandoz Ag Sal cristralina de un inhibidor triciclico de poli(adp-ribosa)-polimerasa.
US10933069B2 (en) 2018-01-05 2021-03-02 Cybrexa 1, Inc. Compounds, compositions, and methods for treatment of diseases involving acidic or hypoxic diseased tissues
US10442813B2 (en) 2018-01-30 2019-10-15 RK Pharma Solutions LLC Polymorphs of rucaparib camsylate and methods of making same
WO2019175132A1 (en) 2018-03-13 2019-09-19 Onxeo A dbait molecule against acquired resistance in the treatment of cancer
PH12022550037A1 (en) 2019-07-10 2023-04-12 Cybrexa 3 Inc Peptide conjugates of microtubule-targeting agents as therapeutics
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WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
EP4100125A1 (en) 2020-02-03 2022-12-14 Sandoz AG Polymorph of rucaparib mesylate
ES3014370T3 (en) 2020-04-28 2025-04-22 Rhizen Pharmaceuticals Ag Novel compounds useful as poly(adp-ribose) polymerase (parp) inhibitors
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ATE454893T1 (de) * 2003-07-25 2010-01-15 Cancer Rec Tech Ltd Tricyclische parp-hemmer

Also Published As

Publication number Publication date
NZ554659A (en) 2010-08-27
ES2382950T3 (es) 2012-06-14
EP1799685A2 (en) 2007-06-27
EP1799685B1 (en) 2012-03-28
WO2006033007A3 (en) 2006-11-02
KR100853601B1 (ko) 2008-08-22
AR051296A1 (es) 2007-01-03
US20060100198A1 (en) 2006-05-11
CA2581025C (en) 2011-06-07
AU2005286191A1 (en) 2006-03-30
MX2007002461A (es) 2008-03-13
TW200613305A (en) 2006-05-01
ATE551345T1 (de) 2012-04-15
RU2007110026A (ru) 2008-10-27
CA2581025A1 (en) 2006-03-30
US7268126B2 (en) 2007-09-11
HK1116483A1 (en) 2008-12-24
AU2005286191B2 (en) 2011-11-17
JP2008513436A (ja) 2008-05-01
IL181463A (en) 2012-02-29
IL181463A0 (en) 2007-07-04
RU2355691C2 (ru) 2009-05-20
BRPI0516766A (pt) 2008-09-16
WO2006033007A2 (en) 2006-03-30
NO20070920L (no) 2007-03-15
NO337938B1 (no) 2016-07-11
KR20070089121A (ko) 2007-08-30

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