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

Info

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)
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

Links

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
    • C07D487/06—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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (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)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Surgery (AREA)
  • Psychiatry (AREA)
  • Hematology (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 (18)

Country Link
US (1) US7268126B2 (zh)
EP (1) EP1799685B1 (zh)
JP (1) JP2008513436A (zh)
KR (1) KR100853601B1 (zh)
AR (1) AR051296A1 (zh)
AT (1) ATE551345T1 (zh)
AU (1) AU2005286191B2 (zh)
BR (1) BRPI0516766A (zh)
CA (1) CA2581025C (zh)
ES (1) ES2382950T3 (zh)
HK (1) HK1116483A1 (zh)
IL (1) IL181463A (zh)
MX (1) MX2007002461A (zh)
NO (1) NO337938B1 (zh)
NZ (1) NZ554659A (zh)
RU (1) RU2355691C2 (zh)
TW (1) TWI365188B (zh)
WO (1) WO2006033007A2 (zh)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004087713A1 (en) * 2003-03-31 2004-10-14 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
JP5177429B2 (ja) * 2005-07-18 2013-04-03 バイパー サイエンシズ，インコーポレイティド 癌の治療
US20100279327A1 (en) * 2006-06-12 2010-11-04 Bipar Sciences, Inc. Method of treating diseases with parp inhibitors
CA2662337A1 (en) * 2006-09-05 2008-03-13 Bipar Sciences, Inc. Inhibition of fatty acid synthesis by parp inhibitors and methods of treatment thereof
EP2059498A4 (en) * 2006-09-05 2011-01-12 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
CN101917982B (zh) * 2007-11-12 2013-03-20 彼帕科学公司 使用4-碘-3-硝基苯甲酰胺与抗肿瘤剂组合治疗乳腺癌
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
JP2011506343A (ja) * 2007-12-07 2011-03-03 バイパー サイエンシズ，インコーポレイティド トポイソメラーゼ阻害剤とｐａｒｐ阻害剤との組み合わせによるがんの治療
RU2010136966A (ru) * 2008-02-04 2012-03-20 Байпар Сайенсиз, Инк. (Us) Способы диагностики и лечения заболеваний, опосредованных parp
WO2011057129A2 (en) 2009-11-09 2011-05-12 Allergan, Inc. Compositions and methods for stimulating hair growth
PL3150610T3 (pl) 2010-02-12 2020-02-28 Pfizer Inc. Sole i polimorfy 8-fluoro-2-{4-[(metyloamino}metylo]fenylo}-1,3,4,5-tetrahydro-6Hazepino[5,4,3-cd]indol-6-onu
CA2798697A1 (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
RU2705156C2 (ru) 2014-08-22 2019-11-05 Кловис Онколоджи, Инк. Таблетки, содержащие большую дозу рукапариба
WO2017013237A1 (en) 2015-07-23 2017-01-26 Institut Curie Use of a combination of dbait molecule and parp inhibitors to treat cancer
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
WO2018218025A1 (en) * 2017-05-24 2018-11-29 The Trustees Of The University Of Pennsylvania Radiolabeled and fluorescent parp inhibitors for imaging and radiotherapy
EP3704124A1 (en) * 2017-11-03 2020-09-09 Sandoz AG Crystalline salt of a tricyclic poly(adp-ribose) polymerase inhibitor
EP3735297A1 (en) 2018-01-05 2020-11-11 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
AU2019235337A1 (en) 2018-03-13 2020-08-27 Centre National De La Recherche Scientifique A Dbait molecule against acquired resistance in the treatment of cancer
PE20220563A1 (es) 2019-07-10 2022-04-13 Cybrexa 2 Inc Conjugados peptidicos de citotoxinas como terapeuticos
JP2022541747A (ja) 2019-07-10 2022-09-27 サイブレクサ ３，インコーポレイテッド 治療薬としての微小管標的化剤のペプチドコンジュゲート
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
WO2021156140A1 (en) 2020-02-03 2021-08-12 Sandoz Ag Polymorph of rucaparib mesylate
BR112022021521A2 (pt) 2020-04-28 2023-01-24 Rhizen Pharmaceuticals Ag Compostos inovadores úteis como inibidores de poli(adp-ribose)polimerase (parp)
WO2022015557A1 (en) 2020-07-14 2022-01-20 Assia Chemical Industries Ltd Solid state forms of rucaparib salts
WO2022090938A1 (en) 2020-10-31 2022-05-05 Rhizen Pharmaceuticals Ag Phthalazinone derivatives useful as parp inhibitors
MX2023011793A (es) 2021-04-08 2023-10-12 Rhizen Pharmaceuticals Ag Inhibidores de poli(adenosin difosfato-ribosa) polimerasa.
WO2023137060A1 (en) 2022-01-11 2023-07-20 Assia Chemical Industries Ltd. Solid state forms of rucaparib tosylate

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA01007001A (es) * 1999-01-11 2002-07-30 Agouron Pharma Inhibidores triciclicos de poli (adp-ribosa) polimerasas.
WO2004087713A1 (en) * 2003-03-31 2004-10-14 Pfizer Inc. Salts of tricyclic inhibitors of poly(adp-ribose) polymerases
BRPI0412899B1 (pt) * 2003-07-25 2021-10-05 Cancer Research Technology Limited Uso de um composto ou um sal farmaceuticamente aceitável do mesmo para a manufatura de um medicamento citotóxico para o tratamento de câncer de ovário, câncer de mama, câncer de próstata ou câncer pancreático

Also Published As

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

Similar Documents

Publication Publication Date Title
TWI365188B (en) 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
HRP20180578T1 (hr) Pirolo[2,3-b]piridin-4-il-amini i pirolo[2m3-b]pirimidin-4-il-amini kao inhibitori janus kinaze
IL178899A0 (en) [3.2.0] heterocyclic compounds and methods of using the same
IL176737A0 (en) Pyrazolo[1,5-a] pyrimidin-7-yl-amine derivatives for use in the treatment of protein kinase dependent diseases
IL183110A0 (en) Certain imidazo[1,2-a]pyrazin-8-ylamines, method of making, and method of use thereof
IS8192A (is) Pýrróló[3,4-c] pýrasól afleiður virkar sem kínasahindrar
ZA200802998B (en) Use of pyrazolo [1,5-a] pyrimidine derivatives for inhibiting protein kinases methods for inhibiting protein kinases
NO20053955D0 (no) Pyrazolo [1,5-A] pyrimidinderivater
EP1796467A4 (en) INHIBITORS IMIDAZO {4,5-B} PYRAZINONE PROTEIN KINASES
HK1099302A1 (en) Pyrazolo and imidazo-pyrimidine derivatives
NO20054331D0 (no) Substituerte-8-perfluoralkyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-on-derivater
ZA200703623B (en) Formulations of [1,4]diazepino[6,7,1-ij]quinoline derivatives
HRP20130533T1 (en) Amorphous solid dispersions of 7-chloro-n,n, 5-trimethyl-4-oxo-3-phenyl-3, 5,-dihydro-4h-pyridazino[4,5-b]indole-1-acetamide
IL169153A0 (en) Formulation and methods for the treatment of thrombocythemia
HK1083844A1 (en) N-[3-(3-substituted-pyrazolo[1,5-a] pyrimidin-7-yl) phenyl]-sulfonamides, and compositions, and methods related thereto
IL182755A0 (en) Metabolites of certain [1,4]diazepino
IL172629A0 (en) Process for the preparation of nonpeptide substituted spirobenzoazepine derivatives
HK1102395A1 (en) Indene derivatives and process for the preparation thereof
IL179670A0 (en) Heterocyclic compounds and processes for the preparation thereof
ZA200701404B (en) 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
EP1756036A4 (en) INDENED DERIVATIVES AND PROCESS FOR THEIR PREPARATION
EP1646284A4 (en) AZOL DERIVATIVES AND METHOD FOR THEIR PREPARATION
IL187441A0 (en) Derivatives of 6,7-dihydro-5h-imidazo[1,2-a] imidazole-3-sulfonic acid
AU2003231555A1 (en) Adjuster with caster
ZA200609778B (en) [3.2.0.] Heterocyclic compounds and methods of using the same