JP2013509441A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2013509441A5 JP2013509441A5 JP2012537154A JP2012537154A JP2013509441A5 JP 2013509441 A5 JP2013509441 A5 JP 2013509441A5 JP 2012537154 A JP2012537154 A JP 2012537154A JP 2012537154 A JP2012537154 A JP 2012537154A JP 2013509441 A5 JP2013509441 A5 JP 2013509441A5
- Authority
- JP
- Japan
- Prior art keywords
- day
- administered
- ginarine
- dose
- consecutive days
- 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
- VAZAPHZUAVEOMC-UHFFFAOYSA-N tacedinaline Chemical compound C1=CC(NC(=O)C)=CC=C1C(=O)NC1=CC=CC=C1N VAZAPHZUAVEOMC-UHFFFAOYSA-N 0.000 claims 42
- 239000000203 mixture Substances 0.000 claims 16
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims 9
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims 8
- 150000002148 esters Chemical class 0.000 claims 8
- 239000002207 metabolite Substances 0.000 claims 8
- 229940002612 prodrug Drugs 0.000 claims 8
- 239000000651 prodrug Substances 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 239000011780 sodium chloride Substances 0.000 claims 8
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 8
- FXHOOIRPVKKKFG-UHFFFAOYSA-N N,N-Dimethylacetamide Chemical compound CN(C)C(C)=O FXHOOIRPVKKKFG-UHFFFAOYSA-N 0.000 claims 6
- 239000008389 polyethoxylated castor oil Substances 0.000 claims 5
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 4
- 208000023105 Huntington disease Diseases 0.000 claims 3
- 229920002565 Polyethylene Glycol 400 Polymers 0.000 claims 3
- 150000001875 compounds Chemical class 0.000 claims 3
- 238000007918 intramuscular administration Methods 0.000 claims 3
- 238000007912 intraperitoneal administration Methods 0.000 claims 3
- 238000001990 intravenous administration Methods 0.000 claims 3
- JLFNLZLINWHATN-UHFFFAOYSA-N pentaethylene glycol Chemical compound OCCOCCOCCOCCOCCO JLFNLZLINWHATN-UHFFFAOYSA-N 0.000 claims 3
- 238000007920 subcutaneous administration Methods 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- SECXISVLQFMRJM-UHFFFAOYSA-N N-Methylpyrrolidone Chemical compound CN1CCCC1=O SECXISVLQFMRJM-UHFFFAOYSA-N 0.000 claims 2
- -1 SP3 Proteins 0.000 claims 2
- 238000011374 additional therapy Methods 0.000 claims 2
- 238000009472 formulation Methods 0.000 claims 2
- 238000007914 intraventricular administration Methods 0.000 claims 2
- 238000011282 treatment Methods 0.000 claims 2
- 102100040006 Annexin A1 Human genes 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 102100023147 E3 ubiquitin-protein ligase MARCHF7 Human genes 0.000 claims 1
- 102100026671 F-actin-capping protein subunit alpha-1 Human genes 0.000 claims 1
- 101000959738 Homo sapiens Annexin A1 Proteins 0.000 claims 1
- 101000978673 Homo sapiens E3 ubiquitin-protein ligase MARCHF7 Proteins 0.000 claims 1
- 101000910965 Homo sapiens F-actin-capping protein subunit alpha-1 Proteins 0.000 claims 1
- 101001046870 Homo sapiens Hypoxia-inducible factor 1-alpha Proteins 0.000 claims 1
- 101000584499 Homo sapiens Polycomb protein SUZ12 Proteins 0.000 claims 1
- 101000669917 Homo sapiens Rho-associated protein kinase 1 Proteins 0.000 claims 1
- 101000707567 Homo sapiens Splicing factor 3B subunit 1 Proteins 0.000 claims 1
- 101000657366 Homo sapiens Transcription initiation factor TFIID subunit 7 Proteins 0.000 claims 1
- 102100022875 Hypoxia-inducible factor 1-alpha Human genes 0.000 claims 1
- 102100040406 Lysophosphatidic acid receptor 6 Human genes 0.000 claims 1
- 101710149751 Lysophosphatidic acid receptor 6 Proteins 0.000 claims 1
- 101710130510 PEST proteolytic signal-containing nuclear protein Proteins 0.000 claims 1
- 102100024312 PEST proteolytic signal-containing nuclear protein Human genes 0.000 claims 1
- 102100030702 Polycomb protein SUZ12 Human genes 0.000 claims 1
- 102100039313 Rho-associated protein kinase 1 Human genes 0.000 claims 1
- 102100031711 Splicing factor 3B subunit 1 Human genes 0.000 claims 1
- 102100034748 Transcription initiation factor TFIID subunit 7 Human genes 0.000 claims 1
- 230000003542 behavioural effect Effects 0.000 claims 1
- 230000008033 biological extinction Effects 0.000 claims 1
- 239000000090 biomarker Substances 0.000 claims 1
- 238000009225 cognitive behavioral therapy Methods 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 230000003920 cognitive function Effects 0.000 claims 1
- 238000009226 cognitive therapy Methods 0.000 claims 1
- 230000007547 defect Effects 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 150000003840 hydrochlorides Chemical class 0.000 claims 1
- 238000000185 intracerebroventricular administration Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- ODLHGICHYURWBS-FOSILIAISA-N molport-023-220-444 Chemical compound CC(O)COC[C@@H]([C@@H]([C@H]([C@@H]1O)O)O[C@@H]2O[C@H]([C@H](O[C@@H]3O[C@@H](COCC(C)O)[C@@H]([C@H]([C@@H]3O)O)O[C@@H]3O[C@@H](COCC(C)O)[C@@H]([C@H]([C@@H]3O)O)O[C@@H]3O[C@@H](COCC(C)O)[C@@H]([C@H]([C@@H]3O)O)O[C@@H]3O[C@@H](COCC(C)O)[C@@H]([C@H]([C@@H]3O)O)O3)[C@@H](O)[C@@H]2O)COCC(O)C)O[C@H]1O[C@@H]1[C@@H](O)[C@H](O)[C@H]3O[C@H]1COCC(C)O ODLHGICHYURWBS-FOSILIAISA-N 0.000 claims 1
- 238000002610 neuroimaging Methods 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 238000001671 psychotherapy Methods 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25692709P | 2009-10-30 | 2009-10-30 | |
| US61/256,927 | 2009-10-30 | ||
| US26546809P | 2009-12-01 | 2009-12-01 | |
| US61/265,468 | 2009-12-01 | ||
| PCT/US2010/054872 WO2011053876A1 (en) | 2009-10-30 | 2010-10-29 | The use of ci-994 and dinaline for the treatment of memory/cognition and anxiety disorders |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013509441A JP2013509441A (ja) | 2013-03-14 |
| JP2013509441A5 true JP2013509441A5 (https=) | 2013-12-19 |
Family
ID=43922604
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012537154A Pending JP2013509441A (ja) | 2009-10-30 | 2010-10-29 | 記憶／認知および不安障害の処置のためのｃｉ−９９４およびジナリンの使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US8563615B2 (https=) |
| EP (1) | EP2493298A4 (https=) |
| JP (1) | JP2013509441A (https=) |
| CN (1) | CN102834002A (https=) |
| AU (1) | AU2010313255B2 (https=) |
| CA (1) | CA2779497A1 (https=) |
| IN (1) | IN2012DN03807A (https=) |
| NZ (1) | NZ599757A (https=) |
| WO (1) | WO2011053876A1 (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20110009475A1 (en) * | 2007-07-13 | 2011-01-13 | Massachusetts Institute Of Technology | Methods for treating stress induced emotional disorders |
| WO2009154697A2 (en) | 2008-05-28 | 2009-12-23 | Massachusetts Institute Of Technology | Disc-1 pathway activators in the control of neurogenesis |
| WO2011053876A1 (en) | 2009-10-30 | 2011-05-05 | Massachusetts Institute Of Technology | The use of ci-994 and dinaline for the treatment of memory/cognition and anxiety disorders |
| WO2012003413A1 (en) * | 2010-06-30 | 2012-01-05 | The Broad Institute, Inc. | Novel solid forms of tacedinaline |
| EP2701699B1 (en) | 2011-04-28 | 2019-10-16 | The Broad Institute, Inc. | Inhibitors of histone deacetylase |
| US8691875B2 (en) * | 2011-07-01 | 2014-04-08 | Broad Institute, Inc. | Solid forms of tacedinaline |
| WO2013016193A2 (en) | 2011-07-22 | 2013-01-31 | Massachusetts Istitute Of Technology | Activators of class i histone deacetlyases (hdacs) and uses thereof |
| JP6337255B2 (ja) | 2012-07-27 | 2018-06-06 | ザ ブロード インスティテュート, インコーポレーテッドThe Broad Institute, Inc. | ヒストンデアセチラーゼの阻害剤 |
| WO2014046871A1 (en) * | 2012-09-04 | 2014-03-27 | Massachusetts Institute Of Technology | The use of gene expression profiling as a biomarker for assessing the efficacy of hdac inhibitor treatment in neurodegenerative conditions |
| US9914717B2 (en) | 2012-12-20 | 2018-03-13 | The Broad Institute, Inc. | Cycloalkenyl hydroxamic acid derivatives and their use as histone deacetylase inhibitors |
| CA3125731A1 (en) | 2018-01-12 | 2019-07-18 | KDAc Therapeutics, Inc. | Combination of a selective histone deacetylase 3 (hdac3) inhibitor and an immunotherapy agent for the treatment of cancer |
| GB202001023D0 (en) * | 2020-01-24 | 2020-03-11 | Univ Leicester | HDAC Degrader |
| CN112062826A (zh) * | 2020-06-01 | 2020-12-11 | 暨南大学 | 一种与中枢神经衰老相关的乙酰化修饰h2b蛋白标记分子及其应用 |
| WO2023034440A1 (en) * | 2021-09-01 | 2023-03-09 | Case Western Reserve University | Treatment of neurodegenerative diseases with hdac inhibitors |
Family Cites Families (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5525727A (en) | 1982-05-18 | 1996-06-11 | University Of Florida | Brain-specific drug delivery |
| US5994392A (en) | 1988-02-26 | 1999-11-30 | Neuromedica, Inc. | Antipsychotic prodrugs comprising an antipsychotic agent coupled to an unsaturated fatty acid |
| US5177064A (en) | 1990-07-13 | 1993-01-05 | University Of Florida | Targeted drug delivery via phosphonate derivatives |
| US6110697A (en) | 1995-09-20 | 2000-08-29 | Merck & Co., Inc. | Histone deacetylase as target for antiprotozoal agents |
| ATE361316T1 (de) | 1999-09-08 | 2007-05-15 | Sloan Kettering Inst Cancer | Kristallstruktur einer deacetylase und deren inhibitoren |
| US6713454B1 (en) | 1999-09-13 | 2004-03-30 | Nobex Corporation | Prodrugs of etoposide and etoposide analogs |
| KR20020070285A (ko) | 1999-11-23 | 2002-09-05 | 메틸진, 인크. | 히스톤 디아세틸라제의 억제제 |
| JP2001149081A (ja) | 1999-11-29 | 2001-06-05 | Cyclex Co Ltd | 脱アセチル化酵素の活性測定方法、並びにこれら酵素の阻害剤もしくは促進剤のスクリーニング方法 |
| CA2423744C (en) * | 2000-09-29 | 2012-04-03 | Prolifix Limited | Hydroxamic acid compounds comprising a sulfonamide linkage as hdac inhibitors |
| US20060148743A1 (en) | 2001-05-18 | 2006-07-06 | Vasant Jadhav | RNA interference mediated inhibition of histone deacetylase (HDAC) gene expression using short interfering nucleic acid (siNA) |
| EP1532244A4 (en) | 2001-06-14 | 2005-12-14 | Bristol Myers Squibb Co | NEW HISTONIC HUMAN DEACETYLASES |
| EP1429765A2 (en) | 2001-09-14 | 2004-06-23 | Methylgene, Inc. | Inhibitors of histone deacetylase |
| EP1443928B1 (en) * | 2001-10-16 | 2011-07-27 | Sloan-Kettering Institute For Cancer Research | Treatment of neurodegenerative diseases and cancer of the brain |
| EP1456664A1 (en) | 2001-12-07 | 2004-09-15 | Novartis AG | Use of alpha-tubulin acetylation levels as a biomarker for protein deacetylase inhibitors |
| JP2005517007A (ja) | 2002-02-07 | 2005-06-09 | アクシス・ファーマスーティカルズ | ヒストンデアセチラーゼ阻害剤としての新規二環式ヒドロキサメート |
| AU2003214055A1 (en) | 2002-02-08 | 2003-09-02 | Novartis Ag | Method for screening for compounds having hdac inhibitory activity |
| JP2005525345A (ja) * | 2002-02-15 | 2005-08-25 | スローン−ケッタリング・インスティテュート・フォー・キャンサー・リサーチ | Ｔｒｘ媒介性疾患を処置する方法 |
| US20050288227A1 (en) | 2002-02-15 | 2005-12-29 | Marks Paul A | Use of thioredoxin measurements for diagnostics and treatments |
| US7456219B2 (en) * | 2002-03-04 | 2008-11-25 | Merck Hdac Research, Llc | Polymorphs of suberoylanilide hydroxamic acid |
| US20040077591A1 (en) * | 2002-03-28 | 2004-04-22 | The Brigham And Women's Hospital, Inc. | Histone deacetylase inhibitors for the treatment of multiple sclerosis, amyotrophic lateral sclerosis and Alzheimer's Disease |
| US20030224473A1 (en) | 2002-05-23 | 2003-12-04 | Mccafferty Dewey G. | Methods for screening for histone deacetylase activity and for identifying histone deacetylase inhibitors |
| JP2006503082A (ja) | 2002-10-17 | 2006-01-26 | メシルジーン、インコーポレイテッド | ヒストンデアセチラーゼの阻害剤 |
| TW200424174A (en) | 2003-02-06 | 2004-11-16 | Hoffmann La Roche | New TP diamide |
| US20050037992A1 (en) * | 2003-07-22 | 2005-02-17 | John Lyons | Composition and method for treating neurological disorders |
| KR101153335B1 (ko) | 2003-09-24 | 2012-07-05 | 메틸진 인코포레이티드 | 히스톤 데아세틸라제의 억제제 |
| US20050227929A1 (en) * | 2003-11-13 | 2005-10-13 | Masferrer Jaime L | Combination therapy comprising a Cox-2 inhibitor and an antineoplastic agent |
| AU2005225471B2 (en) | 2004-03-26 | 2011-05-12 | Methylgene Inc. | Inhibitors of histone deacetylase |
| CA2563617A1 (en) * | 2004-04-20 | 2005-11-03 | Rnd Pharmaceuticals | Pharmaceutical compositions and methods of use of lipophilic, silicon-substituted, cyclooxygenase-2 selective non-steroidal anti-inflammatory drugs and derivatives |
| ES2308065T3 (es) * | 2004-04-30 | 2008-12-01 | Topotarget Germany Ag | Formulacion que comprende un inhibidor de histona desacetilasa, que exhibe una liberacion bifasica. |
| US20060008517A1 (en) * | 2004-07-09 | 2006-01-12 | Lynch Marina A | Treatment of age-related memory impairment |
| US20060018921A1 (en) * | 2004-07-16 | 2006-01-26 | Baylor College Of Medicine | Histone deacetylase inhibitors and cognitive applications |
| CA2587013A1 (en) | 2004-11-08 | 2006-05-18 | Errant Gene Therapeutics, Llc | Histone deacetylase inhibitors |
| US7642253B2 (en) * | 2005-05-11 | 2010-01-05 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| US20070015183A1 (en) | 2005-06-03 | 2007-01-18 | The General Hospital Corporation | Biomarkers for huntington's disease |
| EA200800321A1 (ru) | 2005-07-14 | 2008-06-30 | Такеда Сан Диего, Инк. | Ингибиторы гистондеацетилазы |
| JP2009507081A (ja) | 2005-09-07 | 2009-02-19 | ブレインセルス，インコーポレイティド | ＨＤａｃ阻害による神経発生の調整 |
| WO2007049262A1 (en) * | 2005-10-27 | 2007-05-03 | Berand Limited | Methods and compositions for the promotion of neuronal growth and the treatment of asociality and affective disorders |
| WO2007055942A2 (en) | 2005-11-03 | 2007-05-18 | Merck & Co., Inc. | Substituted nicotinamide compounds |
| WO2007056435A2 (en) * | 2005-11-08 | 2007-05-18 | The General Hospital Corporation | Dynamin mediated diseases and associated methods and products |
| JP2009528354A (ja) | 2006-02-28 | 2009-08-06 | メルク エンド カムパニー インコーポレーテッド | ヒストン脱アセチル化酵素のインヒビター |
| KR101495611B1 (ko) | 2006-04-07 | 2015-02-25 | 메틸진 인코포레이티드 | 히스톤 데아세틸라아제의 억제제 |
| CA2649861A1 (en) | 2006-04-26 | 2007-11-08 | Merck & Co., Inc. | Disubstituted aniline compounds |
| CA2651681A1 (en) | 2006-05-18 | 2007-11-29 | Merck & Co., Inc. | Aryl-fused spirocyclic compounds |
| WO2008008472A2 (en) | 2006-07-13 | 2008-01-17 | President And Fellows Of Harvard College | Methods and compositions for modulating synapse formation |
| US8088951B2 (en) | 2006-11-30 | 2012-01-03 | Massachusetts Institute Of Technology | Epigenetic mechanisms re-establish access to long-term memory after neuronal loss |
| US8030344B2 (en) | 2007-03-13 | 2011-10-04 | Methylgene Inc. | Inhibitors of histone deacetylase |
| US20110009475A1 (en) * | 2007-07-13 | 2011-01-13 | Massachusetts Institute Of Technology | Methods for treating stress induced emotional disorders |
| WO2009154697A2 (en) * | 2008-05-28 | 2009-12-23 | Massachusetts Institute Of Technology | Disc-1 pathway activators in the control of neurogenesis |
| KR20110033304A (ko) * | 2008-07-23 | 2011-03-30 | 메사추세츠 인스티튜트 오브 테크놀로지 | Ｄｎａ 손상에 대해 보호하고 신경세포 생존을 증가시키는 히스톤 디아세틸라제 1 (ｈｄａｃ1)의 활성화 |
| CA2745073A1 (en) * | 2008-12-03 | 2010-06-10 | Li-Huei Tsai | Inhibition of hdac2 to promote memory |
| WO2010098888A1 (en) * | 2009-02-27 | 2010-09-02 | Massachusetts Institute Of Technology | Uses of chemicals to modulate gsk-3 signaling for treatment of bipolar disorder and other brain disorders |
| WO2011053876A1 (en) * | 2009-10-30 | 2011-05-05 | Massachusetts Institute Of Technology | The use of ci-994 and dinaline for the treatment of memory/cognition and anxiety disorders |
| WO2013016193A2 (en) * | 2011-07-22 | 2013-01-31 | Massachusetts Istitute Of Technology | Activators of class i histone deacetlyases (hdacs) and uses thereof |
-
2010
- 2010-10-29 WO PCT/US2010/054872 patent/WO2011053876A1/en not_active Ceased
- 2010-10-29 CA CA2779497A patent/CA2779497A1/en not_active Abandoned
- 2010-10-29 JP JP2012537154A patent/JP2013509441A/ja active Pending
- 2010-10-29 IN IN3807DEN2012 patent/IN2012DN03807A/en unknown
- 2010-10-29 EP EP10827583.5A patent/EP2493298A4/en not_active Withdrawn
- 2010-10-29 NZ NZ599757A patent/NZ599757A/en not_active IP Right Cessation
- 2010-10-29 CN CN201080060203XA patent/CN102834002A/zh active Pending
- 2010-10-29 AU AU2010313255A patent/AU2010313255B2/en not_active Ceased
- 2010-11-01 US US12/917,402 patent/US8563615B2/en not_active Expired - Fee Related
-
2012
- 2012-08-27 US US13/595,048 patent/US8841346B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2013509441A5 (https=) | ||
| RU2010143864A (ru) | Способы лечения нарушений с применением селективного антагониста nr2b-подтипа nmda рецепторов | |
| JP2016534063A5 (https=) | ||
| EA201270221A1 (ru) | Лечение болезни крона с применением лаквинимода | |
| RU2014136394A (ru) | Морфолиноалкилфумаратные соединения, фармацевтические композиции и способы применения | |
| JP2017526716A5 (https=) | ||
| JP2015502974A5 (https=) | ||
| JP2014528474A5 (https=) | ||
| UA109991C2 (xx) | Карбаматні сполуки, їх отримання і застосування | |
| BR112014008789A2 (pt) | prevenção e tratamento de condições oculares | |
| JP2018519329A5 (https=) | ||
| JP2016509601A5 (https=) | ||
| EA201790406A1 (ru) | Ингибиторы кинуренин-3-монооксигеназы, фармацевтические композиции и способы их применения | |
| EA201490163A1 (ru) | Ингибиторы кинуренин-3-монооксигеназы, фармацевтические композиции и способы их применения | |
| JP2016522254A5 (https=) | ||
| UA107578C2 (uk) | Комбінована терапія при лікуванні діабету | |
| KR20160093000A (ko) | 창자 과투과성을 치료하기 위한 티로신 하이드록실라제 억제제 | |
| JP2019516739A5 (https=) | ||
| RU2018103873A (ru) | Терапевтические соединения и композиции для лечения социальных расстройств и расстройств, связанных с употреблением психоактивных веществ | |
| JP2009511568A5 (https=) | ||
| JP2013541583A5 (https=) | ||
| JP2013500977A5 (https=) | ||
| JP2013517300A5 (https=) | ||
| JP2009501202A5 (https=) | ||
| IN2014DN08582A (https=) |