CA2581025C - 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 Download PDF

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Publication number
CA2581025C
CA2581025C CA2581025A CA2581025A CA2581025C CA 2581025 C CA2581025 C CA 2581025C CA 2581025 A CA2581025 A CA 2581025A CA 2581025 A CA2581025 A CA 2581025A CA 2581025 C CA2581025 C CA 2581025C
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cancer
carcinoma
salt
treatment
pharmaceutical composition
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Expired - Lifetime
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CA2581025A
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English (en)
French (fr)
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CA2581025A1 (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
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Cancer Research Technology Ltd
Pfizer Corp SRL
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Cancer Research Technology Ltd
Pfizer Corp SRL
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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)
CA2581025A 2004-09-22 2005-09-12 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 Expired - Lifetime CA2581025C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US61245904P 2004-09-22 2004-09-22
US60/612,459 2004-09-22
US67929605P 2005-05-09 2005-05-09
US60/679,296 2005-05-09
PCT/IB2005/002941 WO2006033007A2 (en) 2004-09-22 2005-09-12 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

Publications (2)

Publication Number Publication Date
CA2581025A1 CA2581025A1 (en) 2006-03-30
CA2581025C true CA2581025C (en) 2011-06-07

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CA2581025A Expired - Lifetime CA2581025C (en) 2004-09-22 2005-09-12 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
TWI721947B (zh) 2014-06-11 2021-03-21 美商基利法瑪席特有限責任公司 抗病毒化合物的固態形式
RS67356B1 (sr) 2014-08-22 2025-11-28 Pharma& Schweiz Gmbh Tablete rukapariba visoke doze
JP6457696B2 (ja) 2015-07-23 2019-01-23 アンスティテュ・キュリＩｎｓｔｉｔｕｔ Ｃｕｒｉｅ 癌を処置するためのＤｂａｉｔ分子とＰＡＲＰインヒビターとの組合せの使用
GB201519573D0 (en) 2015-11-05 2015-12-23 King S College London Combination
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
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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
TWI365188B (en) 2012-06-01
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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