JP2008513436A5 - - Google Patents
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- Publication number
- JP2008513436A5 JP2008513436A5 JP2007531869A JP2007531869A JP2008513436A5 JP 2008513436 A5 JP2008513436 A5 JP 2008513436A5 JP 2007531869 A JP2007531869 A JP 2007531869A JP 2007531869 A JP2007531869 A JP 2007531869A JP 2008513436 A5 JP2008513436 A5 JP 2008513436A5
- Authority
- JP
- Japan
- Prior art keywords
- azepino
- indol
- methylamino
- tetrahydro
- fluoro
- 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.)
- Pending
Links
- NBIIXXVUZAFLBC-UHFFFAOYSA-K [O-]P([O-])([O-])=O Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 7
- 239000010452 phosphate Substances 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 238000000634 powder X-ray diffraction Methods 0.000 claims 6
- AGPZUEDYVLUKMF-UHFFFAOYSA-N 1,3,4,5-Tetrahydro-6H-azepino[5,4,3-cd]indol-6-one Chemical compound O=C1NCCC2=CNC3=CC=CC1=C23 AGPZUEDYVLUKMF-UHFFFAOYSA-N 0.000 claims 5
- 239000007787 solid Substances 0.000 claims 2
- SRQIXYAZHSQGIT-UHFFFAOYSA-N C1=CC(CNC)=CC=C1C(N1)=C2CCNC(=O)C3=C2C1=CC=C3 Chemical compound C1=CC(CNC)=CC=C1C(N1)=C2CCNC(=O)C3=C2C1=CC=C3 SRQIXYAZHSQGIT-UHFFFAOYSA-N 0.000 claims 1
- 102000012338 Poly(ADP-ribose) Polymerases Human genes 0.000 claims 1
- 108010061844 Poly(ADP-ribose) Polymerases Proteins 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000000051 modifying Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
Claims (8)
- 回折角(2θ)10.9、19.3、22.9及び25.0でピークを含むＸ線粉末回折パターンを有する、形態Ｉの多形体である、8−フルオロ−2−｛4−[(メチルアミノ)メチル]フェニル｝1,3,4,5−テトラヒドロ−6H−アゼピノ[5,4,3−cd]インドール−6−オンの結晶質リン酸塩。
- 回折角(2θ)11.2、14.0、20.1及び23.1でピークを含むＸ線粉末回折パターンを有する、形態IIの多形体である、8−フルオロ−2−｛4−[(メチルアミノ)メチル]フェニル｝1,3,4,5−テトラヒドロ−6H−アゼピノ[5,4,3−cd]インドール−6−オンの結晶質リン酸塩。
- 回折角(2θ)10.7、11.0、19.4及び25.1でピークを含むＸ線粉末回折パターンを有する、形態IIIの多形体である、8−フルオロ−2−｛4−[(メチルアミノ)メチル]フェニル｝1,3,4,5−テトラヒドロ−6H−アゼピノ[5,4,3−cd]インドール−6−オンの結晶質リン酸塩。
- 回折角(2θ)10.8、14.8、21.6及び25.8でピークを含むＸ線粉末回折パターンを有する、形態Ｖの多形体である、8−フルオロ−2−｛4−[(メチルアミノ)メチル]フェニル｝1,3,4,5−テトラヒドロ−6H−アゼピノ[5,4,3−cd]インドール−6−オンの結晶質リン酸塩。
- 回折角(2θ)14.8、20.0、22.3及び23.5でピークを含むＸ線粉末回折パターンを有する、形態VIの多形体である、8−フルオロ−2−｛4−[(メチルアミノ)メチル]フェニル｝1,3,4,5−テトラヒドロ−6H−アゼピノ[5,4,3−cd]インドール−6−オンの結晶質リン酸塩。
- 結晶質形態の特徴である鋭いピークを全く有することなく４〜４０°の範囲の回折角(2θ)で広いピークを示すＸ線粉末回折パターンを有する、非晶質形態である、8−フルオロ−2−｛4−[(メチルアミノ)メチル]フェニル｝1,3,4,5−テトラヒドロ−6H−アゼピノ[5,4,3−cd]インドール−6−オンのリン酸塩。
- 固体形態が以下の形態：請求項１〜６のいずれか１項記載の多形体形態Ｉ、II、III、Ｖ、VI又は非晶質形態の少なくとも２つを含む、8−フルオロ−2−｛4−[(メチルアミノ)メチル]フェニル｝−1,3,4,5−テトラヒドロ−6H−アゼピノ[5,4,3−cd]インドール−6−オンのリン酸塩の固体形態。
- ポリ(ADP−リボース)ポリメラーゼ活性のモジュレーターとしての作用を有する、請求項１〜７のいずれか１項記載の塩を含む医薬組成物。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US61245904P | 2004-09-22 | 2004-09-22 | |
| US67929605P | 2005-05-09 | 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 |
|---|---|
| JP2008513436A JP2008513436A (ja) | 2008-05-01 |
| JP2008513436A5 true JP2008513436A5 (ja) | 2008-10-23 |
Family
ID=35526956
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007531869A Pending JP2008513436A (ja) | 2004-09-22 | 2005-09-12 | ８−フルオロ−２−｛４−［（メチルアミノ）メチル］フェニル｝−１，３，４，５−テトラヒドロ−６ｈ−アゼピノ［５，４，３−ｃｄ］インドール−６−オンのリン酸塩の多形性及び非晶質形態 |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US7268126B2 (ja) |
| EP (1) | EP1799685B1 (ja) |
| JP (1) | JP2008513436A (ja) |
| KR (1) | KR100853601B1 (ja) |
| AR (1) | AR051296A1 (ja) |
| AT (1) | ATE551345T1 (ja) |
| AU (1) | AU2005286191B2 (ja) |
| BR (1) | BRPI0516766A (ja) |
| CA (1) | CA2581025C (ja) |
| ES (1) | ES2382950T3 (ja) |
| HK (1) | HK1116483A1 (ja) |
| IL (1) | IL181463A (ja) |
| MX (1) | MX2007002461A (ja) |
| NO (1) | NO337938B1 (ja) |
| NZ (1) | NZ554659A (ja) |
| RU (1) | RU2355691C2 (ja) |
| TW (1) | TWI365188B (ja) |
| WO (1) | WO2006033007A2 (ja) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA05010563A (es) * | 2003-03-31 | 2005-11-23 | Pfizer | Sales de los inhibidores triciclicos de las poli(adp-ribosa) polimerasas. |
| US8425929B2 (en) * | 2004-04-30 | 2013-04-23 | Allergan, Inc. | Sustained release intraocular implants and methods for preventing retinal dysfunction |
| KR20080035630A (ko) * | 2005-07-18 | 2008-04-23 | 바이파 사이언스 인코포레이티드 | 암의 치료 |
| US20100279327A1 (en) * | 2006-06-12 | 2010-11-04 | Bipar Sciences, Inc. | Method of treating diseases with parp inhibitors |
| US8143447B2 (en) * | 2006-09-05 | 2012-03-27 | Bipar Sciences, Inc. | Treatment of cancer |
| EP2061479A4 (en) * | 2006-09-05 | 2010-08-04 | Bipar Sciences Inc | FETTIC ACID SYNTHESIS INHIBITED BY PARP HEMMER AND TREATMENT PROCEDURES THEREWITH |
| WO2008114114A2 (en) * | 2007-03-16 | 2008-09-25 | Pfizer Products Inc. | Poly(adp-ribose) polymerases inhibitor for treating ophthalmic condition |
| KR20100102609A (ko) * | 2007-11-12 | 2010-09-24 | 바이파 사이언스 인코포레이티드 | Ｐａｒｐ 억제제를 단독으로 사용하거나 항종양제와 병용하여 유방암을 치료하는 방법 |
| JP2011503071A (ja) * | 2007-11-12 | 2011-01-27 | バイパー サイエンシズ，インコーポレイティド | Ｐａｒｐ阻害剤単独又は抗腫瘍剤との組み合わせによる子宮がん及び卵巣がんの治療 |
| WO2009073869A1 (en) * | 2007-12-07 | 2009-06-11 | Bipar Sciences, Inc. | Treatment of cancer with combinations of topoisomerase inhibitors and parp inhibitors |
| AU2009212401A1 (en) * | 2008-02-04 | 2009-08-13 | Bipar Sciences, Inc. | Methods of diagnosing and treating PARP-mediated diseases |
| MX361709B (es) | 2009-11-09 | 2018-12-07 | Allergan Inc | Composiciones y metodos para estimular el crecimiento del cabello. |
| US8754072B2 (en) * | 2010-02-12 | 2014-06-17 | 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 |
| US20130116284A1 (en) | 2010-05-10 | 2013-05-09 | Radikal Therapeutics Inc. | Lipoic acid and nitroxide derivatives and uses thereof |
| JP6511401B2 (ja) | 2013-02-15 | 2019-05-15 | アラーガン、インコーポレイテッドＡｌｌｅｒｇａｎ，Ｉｎｃｏｒｐｏｒａｔｅｄ | 持続型薬物送達インプラント |
| 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 |
| CN106794185A (zh) | 2014-08-22 | 2017-05-31 | 克洛维斯肿瘤有限公司 | Rucaparib的高剂量强度片剂 |
| EP3325623B3 (en) | 2015-07-23 | 2021-01-20 | 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 |
| KR20190110579A (ko) | 2017-01-24 | 2019-09-30 | 아시아 케미컬 인더스트리스 리미티드 | 루카파립 및 루카파립 염의 고체상 형태 |
| WO2018162439A1 (en) | 2017-03-08 | 2018-09-13 | Onxeo | New predictive biomarker for the sensitivity to a treatment of cancer with a dbait molecule |
| CA3064761A1 (en) * | 2017-05-24 | 2018-11-29 | The Trustees Of The University Of Pennsylvania | Radiolabeled and fluorescent parp inhibitors for imaging and radiotherapy |
| MX2020004545A (es) * | 2017-11-03 | 2020-08-03 | Sandoz Ag | Sal cristralina de un inhibidor triciclico de poli(adp-ribosa)-polimerasa. |
| MX2020007060A (es) | 2018-01-05 | 2020-11-11 | Cybrexa 1 Inc | Compuestos, composiciones y metodos para tratar enfermedades que involucren tejidos con enfermedades acidas o hipoxicas. |
| 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 |
| MX2022000450A (es) | 2019-07-10 | 2022-04-25 | Cybrexa 3 Inc | Conjugados peptídicos de agentes dirigidos a microtúbulos como terapéuticos. |
| EP3997093A1 (en) | 2019-07-10 | 2022-05-18 | Cybrexa 2, Inc. | Peptide conjugates of cytotoxins as therapeutics |
| 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 |
| KR20230002487A (ko) | 2020-04-28 | 2023-01-05 | 리젠 파마슈티컬스 아게 | 폴리(adp-리보스) 폴리머라제(parp) 억제제로서 유용한 신규 화합물 |
| EP4182318A1 (en) | 2020-07-14 | 2023-05-24 | 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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE261963T1 (de) * | 1999-01-11 | 2004-04-15 | Agouron Pharma | Tricyclische inhibitoren von poly(adp-ribose) polymerasen |
| MXPA05010563A (es) * | 2003-03-31 | 2005-11-23 | Pfizer | Sales de los inhibidores triciclicos de las poli(adp-ribosa) polimerasas. |
| DK1660095T3 (da) * | 2003-07-25 | 2010-05-25 | Cancer Rec Tech Ltd | Tricykliske PARP-inhibitorer |
-
2005
- 2005-09-12 EP EP05799991A patent/EP1799685B1/en active Active
- 2005-09-12 BR BRPI0516766-3A patent/BRPI0516766A/pt not_active Application Discontinuation
- 2005-09-12 MX MX2007002461A patent/MX2007002461A/es active IP Right Grant
- 2005-09-12 WO PCT/IB2005/002941 patent/WO2006033007A2/en active Application Filing
- 2005-09-12 CA CA2581025A patent/CA2581025C/en active Active
- 2005-09-12 RU RU2007110026/04A patent/RU2355691C2/ru active
- 2005-09-12 AU AU2005286191A patent/AU2005286191B2/en active Active
- 2005-09-12 NZ NZ554659A patent/NZ554659A/en unknown
- 2005-09-12 JP JP2007531869A patent/JP2008513436A/ja active Pending
- 2005-09-12 ES ES05799991T patent/ES2382950T3/es active Active
- 2005-09-12 KR KR1020077006422A patent/KR100853601B1/ko active IP Right Grant
- 2005-09-12 AT AT05799991T patent/ATE551345T1/de active
- 2005-09-20 AR ARP050103934A patent/AR051296A1/es unknown
- 2005-09-21 US US11/233,835 patent/US7268126B2/en active Active
- 2005-09-21 TW TW094132634A patent/TWI365188B/zh active
-
2007
- 2007-02-16 NO NO20070920A patent/NO337938B1/no unknown
- 2007-02-20 IL IL181463A patent/IL181463A/en active IP Right Grant
-
2008
- 2008-06-20 HK HK08106859.9A patent/HK1116483A1/xx unknown
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