JP2014525428A5 - - Google Patents
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- Publication number
- JP2014525428A5 JP2014525428A5 JP2014527685A JP2014527685A JP2014525428A5 JP 2014525428 A5 JP2014525428 A5 JP 2014525428A5 JP 2014527685 A JP2014527685 A JP 2014527685A JP 2014527685 A JP2014527685 A JP 2014527685A JP 2014525428 A5 JP2014525428 A5 JP 2014525428A5
- Authority
- JP
- Japan
- Prior art keywords
- crystalline
- relapradib
- pharmaceutical composition
- disease
- atr
- 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.)
- Granted
Links
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 238000000634 powder X-ray diffraction Methods 0.000 claims 4
- 238000001237 Raman spectrum Methods 0.000 claims 3
- 238000000862 absorption spectrum Methods 0.000 claims 3
- NNBGCSGCRSCFEA-UHFFFAOYSA-N 2-[2-[(2,3-difluorophenyl)methylsulfanyl]-4-oxoquinolin-1-yl]-n-[1-(2-methoxyethyl)piperidin-4-yl]-n-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamide Chemical compound C1CN(CCOC)CCC1N(C(=O)CN1C2=CC=CC=C2C(=O)C=C1SCC=1C(=C(F)C=CC=1)F)CC1=CC=C(C=2C=CC(=CC=2)C(F)(F)F)C=C1 NNBGCSGCRSCFEA-UHFFFAOYSA-N 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- ADEBPBSSDYVVLD-UHFFFAOYSA-N donepezil Chemical compound O=C1C=2C=C(OC)C(OC)=CC=2CC1CC(CC1)CCN1CC1=CC=CC=C1 ADEBPBSSDYVVLD-UHFFFAOYSA-N 0.000 claims 2
- ASUTZQLVASHGKV-JDFRZJQESA-N galanthamine Chemical compound O1C(=C23)C(OC)=CC=C2CN(C)CC[C@]23[C@@H]1C[C@@H](O)C=C2 ASUTZQLVASHGKV-JDFRZJQESA-N 0.000 claims 2
- 230000008018 melting Effects 0.000 claims 2
- 238000002844 melting Methods 0.000 claims 2
- 229950004360 rilapladib Drugs 0.000 claims 2
- 102000004868 N-Methyl-D-Aspartate Receptors Human genes 0.000 claims 1
- 108090001041 N-Methyl-D-Aspartate Receptors Proteins 0.000 claims 1
- 238000001069 Raman spectroscopy Methods 0.000 claims 1
- XSVMFMHYUFZWBK-NSHDSACASA-N Rivastigmine Chemical compound CCN(C)C(=O)OC1=CC=CC([C@H](C)N(C)C)=C1 XSVMFMHYUFZWBK-NSHDSACASA-N 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 239000000544 cholinesterase inhibitor Substances 0.000 claims 1
- 229960003530 donepezil Drugs 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229960003980 galantamine Drugs 0.000 claims 1
- ASUTZQLVASHGKV-UHFFFAOYSA-N galanthamine hydrochloride Natural products O1C(=C23)C(OC)=CC=C2CN(C)CCC23C1CC(O)C=C2 ASUTZQLVASHGKV-UHFFFAOYSA-N 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- BUGYDGFZZOZRHP-UHFFFAOYSA-N memantine Chemical compound C1C(C2)CC3(C)CC1(C)CC2(N)C3 BUGYDGFZZOZRHP-UHFFFAOYSA-N 0.000 claims 1
- 229960004640 memantine Drugs 0.000 claims 1
- 229960004136 rivastigmine Drugs 0.000 claims 1
- 238000001228 spectrum Methods 0.000 claims 1
- 229960001685 tacrine Drugs 0.000 claims 1
- YLJREFDVOIBQDA-UHFFFAOYSA-N tacrine Chemical compound C1=CC=C2C(N)=C(CCCC3)C3=NC2=C1 YLJREFDVOIBQDA-UHFFFAOYSA-N 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161530104P | 2011-09-01 | 2011-09-01 | |
| US61/530,104 | 2011-09-01 | ||
| PCT/EP2012/067027 WO2013030374A1 (en) | 2011-09-01 | 2012-08-31 | Novel crystal form |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014525428A JP2014525428A (ja) | 2014-09-29 |
| JP2014525428A5 true JP2014525428A5 (https=) | 2015-10-29 |
| JP6199291B2 JP6199291B2 (ja) | 2017-09-20 |
Family
ID=46829730
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014527685A Expired - Fee Related JP6199291B2 (ja) | 2011-09-01 | 2012-08-31 | 新規な結晶形態 |
Country Status (34)
| Country | Link |
|---|---|
| US (3) | US9227953B2 (https=) |
| EP (1) | EP2751094B1 (https=) |
| JP (1) | JP6199291B2 (https=) |
| KR (2) | KR20190075172A (https=) |
| CN (1) | CN103906744A (https=) |
| AU (2) | AU2012300841C1 (https=) |
| BR (1) | BR112014004251A2 (https=) |
| CA (1) | CA2847066C (https=) |
| CL (1) | CL2014000489A1 (https=) |
| CO (1) | CO6890102A2 (https=) |
| CR (1) | CR20140098A (https=) |
| CY (1) | CY1120784T1 (https=) |
| DK (1) | DK2751094T3 (https=) |
| DO (1) | DOP2014000042A (https=) |
| EA (1) | EA027972B1 (https=) |
| ES (1) | ES2686563T3 (https=) |
| HR (1) | HRP20181375T1 (https=) |
| HU (1) | HUE041578T2 (https=) |
| IL (1) | IL230977A (https=) |
| LT (1) | LT2751094T (https=) |
| MA (1) | MA35362B1 (https=) |
| MX (1) | MX349243B (https=) |
| MY (1) | MY172885A (https=) |
| PE (1) | PE20141411A1 (https=) |
| PH (1) | PH12014500382A1 (https=) |
| PL (1) | PL2751094T3 (https=) |
| PT (1) | PT2751094T (https=) |
| RS (1) | RS57644B1 (https=) |
| SG (1) | SG2014011886A (https=) |
| SI (1) | SI2751094T1 (https=) |
| SM (1) | SMT201800455T1 (https=) |
| UA (1) | UA114607C2 (https=) |
| WO (1) | WO2013030374A1 (https=) |
| ZA (1) | ZA201401176B (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103906744A (zh) | 2011-09-01 | 2014-07-02 | 葛兰素集团有限公司 | 新晶型 |
| EP2764866A1 (en) | 2013-02-07 | 2014-08-13 | IP Gesellschaft für Management mbH | Inhibitors of nedd8-activating enzyme |
| TW202144329A (zh) * | 2020-03-30 | 2021-12-01 | 大陸商江蘇亞虹醫藥科技股份有限公司 | 硝羥喹啉前藥的晶型、含其的醫藥組成物及其製備方法和應用 |
Family Cites Families (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4826689A (en) | 1984-05-21 | 1989-05-02 | University Of Rochester | Method for making uniformly sized particles from water-insoluble organic compounds |
| FR2634376B1 (fr) | 1988-07-21 | 1992-04-17 | Farmalyoc | Nouvelle forme unitaire, solide et poreuse comprenant des microparticules et/ou des nanoparticules, ainsi que sa preparation |
| IT1227626B (it) | 1988-11-28 | 1991-04-23 | Vectorpharma Int | Farmaci supportati aventi velocita' di dissoluzione aumentata e procedimento per la loro preparazione |
| IT1243390B (it) | 1990-11-22 | 1994-06-10 | Vectorpharma Int | Composizioni farmaceutiche in forma di particelle atte al rilascio controllato di sostanze farmacologicamente attive e procedimento per la loro preparazione. |
| US5552160A (en) | 1991-01-25 | 1996-09-03 | Nanosystems L.L.C. | Surface modified NSAID nanoparticles |
| US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
| WO1993025190A1 (en) | 1992-06-10 | 1993-12-23 | Eastman Kodak Company | Surface modified nsaid nanoparticles |
| NZ248813A (en) | 1992-11-25 | 1995-06-27 | Eastman Kodak Co | Polymeric grinding media used in grinding pharmaceutical substances |
| US5346702A (en) | 1992-12-04 | 1994-09-13 | Sterling Winthrop Inc. | Use of non-ionic cloud point modifiers to minimize nanoparticle aggregation during sterilization |
| US5298262A (en) | 1992-12-04 | 1994-03-29 | Sterling Winthrop Inc. | Use of ionic cloud point modifiers to prevent particle aggregation during sterilization |
| US5302401A (en) | 1992-12-09 | 1994-04-12 | Sterling Winthrop Inc. | Method to reduce particle size growth during lyophilization |
| US5340564A (en) | 1992-12-10 | 1994-08-23 | Sterling Winthrop Inc. | Formulations comprising olin 10-G to prevent particle aggregation and increase stability |
| US5336507A (en) | 1992-12-11 | 1994-08-09 | Sterling Winthrop Inc. | Use of charged phospholipids to reduce nanoparticle aggregation |
| US5429824A (en) | 1992-12-15 | 1995-07-04 | Eastman Kodak Company | Use of tyloxapole as a nanoparticle stabilizer and dispersant |
| US5352459A (en) | 1992-12-16 | 1994-10-04 | Sterling Winthrop Inc. | Use of purified surface modifiers to prevent particle aggregation during sterilization |
| US5587143A (en) | 1994-06-28 | 1996-12-24 | Nanosystems L.L.C. | Butylene oxide-ethylene oxide block copolymer surfactants as stabilizer coatings for nanoparticle compositions |
| US5585108A (en) | 1994-12-30 | 1996-12-17 | Nanosystems L.L.C. | Formulations of oral gastrointestinal therapeutic agents in combination with pharmaceutically acceptable clays |
| US5665331A (en) | 1995-01-10 | 1997-09-09 | Nanosystems L.L.C. | Co-microprecipitation of nanoparticulate pharmaceutical agents with crystal growth modifiers |
| US5560932A (en) | 1995-01-10 | 1996-10-01 | Nano Systems L.L.C. | Microprecipitation of nanoparticulate pharmaceutical agents |
| US5662883A (en) | 1995-01-10 | 1997-09-02 | Nanosystems L.L.C. | Microprecipitation of micro-nanoparticulate pharmaceutical agents |
| US5569448A (en) | 1995-01-24 | 1996-10-29 | Nano Systems L.L.C. | Sulfated nonionic block copolymer surfactants as stabilizer coatings for nanoparticle compositions |
| US5560931A (en) | 1995-02-14 | 1996-10-01 | Nawosystems L.L.C. | Formulations of compounds as nanoparticulate dispersions in digestible oils or fatty acids |
| US5571536A (en) | 1995-02-06 | 1996-11-05 | Nano Systems L.L.C. | Formulations of compounds as nanoparticulate dispersions in digestible oils or fatty acids |
| US5503723A (en) | 1995-02-08 | 1996-04-02 | Eastman Kodak Company | Isolation of ultra small particles |
| US5518738A (en) | 1995-02-09 | 1996-05-21 | Nanosystem L.L.C. | Nanoparticulate nsaid compositions |
| US5534270A (en) | 1995-02-09 | 1996-07-09 | Nanosystems Llc | Method of preparing stable drug nanoparticles |
| US5622938A (en) | 1995-02-09 | 1997-04-22 | Nano Systems L.L.C. | Sugar base surfactant for nanocrystals |
| US5591456A (en) | 1995-02-10 | 1997-01-07 | Nanosystems L.L.C. | Milled naproxen with hydroxypropyl cellulose as a dispersion stabilizer |
| US5573783A (en) | 1995-02-13 | 1996-11-12 | Nano Systems L.L.C. | Redispersible nanoparticulate film matrices with protective overcoats |
| US5510118A (en) | 1995-02-14 | 1996-04-23 | Nanosystems Llc | Process for preparing therapeutic compositions containing nanoparticles |
| US5580579A (en) | 1995-02-15 | 1996-12-03 | Nano Systems L.L.C. | Site-specific adhesion within the GI tract using nanoparticles stabilized by high molecular weight, linear poly (ethylene oxide) polymers |
| US5718919A (en) | 1995-02-24 | 1998-02-17 | Nanosystems L.L.C. | Nanoparticles containing the R(-)enantiomer of ibuprofen |
| US5747001A (en) | 1995-02-24 | 1998-05-05 | Nanosystems, L.L.C. | Aerosols containing beclomethazone nanoparticle dispersions |
| US5565188A (en) | 1995-02-24 | 1996-10-15 | Nanosystems L.L.C. | Polyalkylene block copolymers as surface modifiers for nanoparticles |
| CH690264A5 (fr) | 1995-06-30 | 2000-06-30 | Symphar Sa | Dérivés aminophosphonates substitués, leur procédé de préparation et leur utilisation pour la préparation de compositions pharmaceutiques. |
| GB9626536D0 (en) | 1996-12-20 | 1997-02-05 | Symphar Sa | Novel compounds |
| GB9626615D0 (en) | 1996-12-20 | 1997-02-05 | Symphar Sa | Novel compounds |
| GB9626616D0 (en) | 1996-12-20 | 1997-02-05 | Symphar Sa | Novel compounds |
| WO1998035666A1 (en) | 1997-02-13 | 1998-08-20 | Nanosystems Llc | Formulations of nanoparticle naproxen tablets |
| GB0024808D0 (en) * | 2000-10-10 | 2000-11-22 | Smithkline Beecham Plc | Novel compounds |
| EP1735457A4 (en) | 2004-04-16 | 2007-08-29 | Glaxo Group Ltd | METHODS FOR DETECTING Lp-PLA2 ACTIVITY AND INHIBITION OF Lp-PLA2 ACTIVITY |
| AU2008251467B2 (en) | 2007-05-11 | 2014-07-31 | The Trustees Of The University Of Pennsylvania | Methods of treatment of skin ulcers |
| WO2008140450A1 (en) * | 2007-05-11 | 2008-11-20 | Thomas Jefferson University | Methods of treatment and prevention of metabolic bone diseases and disorders |
| CN101986785A (zh) * | 2007-05-11 | 2011-03-16 | 托马斯杰弗逊大学 | 治疗和预防神经退行性疾病和紊乱的方法 |
| US20080279846A1 (en) | 2007-05-11 | 2008-11-13 | Thomas Jefferson University | Methods of treatment and prevention of neurodegenerative diseases and disorders |
| US8962633B2 (en) | 2007-05-11 | 2015-02-24 | Thomas Jefferson University | Methods of treatment and prevention of metabolic bone diseases and disorders |
| US8871928B2 (en) | 2010-09-20 | 2014-10-28 | Glaxo Group Limited | Tricyclic compounds, preparation methods, and their uses |
| JP2013544854A (ja) | 2010-12-06 | 2013-12-19 | グラクソ グループ リミテッド | 化合物 |
| PE20140421A1 (es) | 2010-12-06 | 2014-04-26 | Glaxo Group Ltd | COMPUESTOS DERIVADOS DE PIRIMIDINONA COMO INHIBIDORES DE Lp-PLA2 |
| EP2651403B1 (en) | 2010-12-17 | 2020-12-02 | Glaxo Group Limited | Use of lp-pla2 inhibitors in the treatment and prevention of eye diseases |
| CN103906744A (zh) * | 2011-09-01 | 2014-07-02 | 葛兰素集团有限公司 | 新晶型 |
| EP2764866A1 (en) | 2013-02-07 | 2014-08-13 | IP Gesellschaft für Management mbH | Inhibitors of nedd8-activating enzyme |
-
2012
- 2012-08-31 CN CN201280051671.XA patent/CN103906744A/zh active Pending
- 2012-08-31 JP JP2014527685A patent/JP6199291B2/ja not_active Expired - Fee Related
- 2012-08-31 MY MYPI2014700470A patent/MY172885A/en unknown
- 2012-08-31 PT PT12756693T patent/PT2751094T/pt unknown
- 2012-08-31 PE PE2014000274A patent/PE20141411A1/es not_active Application Discontinuation
- 2012-08-31 EA EA201490536A patent/EA027972B1/ru not_active IP Right Cessation
- 2012-08-31 ES ES12756693.3T patent/ES2686563T3/es active Active
- 2012-08-31 WO PCT/EP2012/067027 patent/WO2013030374A1/en not_active Ceased
- 2012-08-31 UA UAA201403151A patent/UA114607C2/uk unknown
- 2012-08-31 SI SI201231371T patent/SI2751094T1/sl unknown
- 2012-08-31 DK DK12756693.3T patent/DK2751094T3/en active
- 2012-08-31 PH PH1/2014/500382A patent/PH12014500382A1/en unknown
- 2012-08-31 EP EP12756693.3A patent/EP2751094B1/en active Active
- 2012-08-31 CA CA2847066A patent/CA2847066C/en not_active Expired - Fee Related
- 2012-08-31 SG SG2014011886A patent/SG2014011886A/en unknown
- 2012-08-31 RS RS20181064A patent/RS57644B1/sr unknown
- 2012-08-31 BR BR112014004251A patent/BR112014004251A2/pt not_active Application Discontinuation
- 2012-08-31 HU HUE12756693A patent/HUE041578T2/hu unknown
- 2012-08-31 KR KR1020197017797A patent/KR20190075172A/ko not_active Ceased
- 2012-08-31 AU AU2012300841A patent/AU2012300841C1/en not_active Ceased
- 2012-08-31 LT LTEP12756693.3T patent/LT2751094T/lt unknown
- 2012-08-31 MX MX2014002454A patent/MX349243B/es active IP Right Grant
- 2012-08-31 US US14/241,913 patent/US9227953B2/en not_active Expired - Fee Related
- 2012-08-31 SM SM20180455T patent/SMT201800455T1/it unknown
- 2012-08-31 KR KR1020147005011A patent/KR20140056297A/ko not_active Ceased
- 2012-08-31 HR HRP20181375TT patent/HRP20181375T1/hr unknown
- 2012-08-31 PL PL12756693T patent/PL2751094T3/pl unknown
-
2014
- 2014-02-13 IL IL230977A patent/IL230977A/en active IP Right Grant
- 2014-02-17 ZA ZA2014/01176A patent/ZA201401176B/en unknown
- 2014-02-27 CR CR20140098A patent/CR20140098A/es unknown
- 2014-02-27 CL CL2014000489A patent/CL2014000489A1/es unknown
- 2014-02-28 DO DO2014000042A patent/DOP2014000042A/es unknown
- 2014-02-28 CO CO14043369A patent/CO6890102A2/es not_active Application Discontinuation
- 2014-02-28 MA MA36784A patent/MA35362B1/fr unknown
-
2015
- 2015-11-25 US US14/951,997 patent/US9682074B2/en not_active Expired - Fee Related
-
2016
- 2016-01-28 AU AU2016200492A patent/AU2016200492B2/en not_active Ceased
- 2016-09-01 US US15/254,160 patent/US9694004B2/en not_active Expired - Fee Related
-
2018
- 2018-09-04 CY CY181100922T patent/CY1120784T1/el unknown
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