JP2012508249A5 - - Google Patents
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- Publication number
- JP2012508249A5 JP2012508249A5 JP2011535698A JP2011535698A JP2012508249A5 JP 2012508249 A5 JP2012508249 A5 JP 2012508249A5 JP 2011535698 A JP2011535698 A JP 2011535698A JP 2011535698 A JP2011535698 A JP 2011535698A JP 2012508249 A5 JP2012508249 A5 JP 2012508249A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- hydrogen atom
- compound
- amino
- nitrophenyl
- 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
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- 150000001875 compounds Chemical class 0.000 claims 15
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 13
- 102000006772 Acid Ceramidase Human genes 0.000 claims 8
- 108020005296 Acid Ceramidase Proteins 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 7
- YPFDHNVEDLHUCE-UHFFFAOYSA-N 1,3-propanediol Substances OCCCO YPFDHNVEDLHUCE-UHFFFAOYSA-N 0.000 claims 6
- 229920000166 polytrimethylene carbonate Polymers 0.000 claims 6
- 238000000034 method Methods 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 230000002401 inhibitory effect Effects 0.000 claims 4
- 239000000651 prodrug Substances 0.000 claims 3
- 229940002612 prodrug Drugs 0.000 claims 3
- ZDRVLAOYDGQLFI-UHFFFAOYSA-N 4-[[4-(4-chlorophenyl)-1,3-thiazol-2-yl]amino]phenol;hydrochloride Chemical compound Cl.C1=CC(O)=CC=C1NC1=NC(C=2C=CC(Cl)=CC=2)=CS1 ZDRVLAOYDGQLFI-UHFFFAOYSA-N 0.000 claims 2
- 102000004201 Ceramidases Human genes 0.000 claims 2
- 108090000751 Ceramidases Proteins 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 150000002148 esters Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 238000000338 in vitro Methods 0.000 claims 2
- 238000001727 in vivo Methods 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 108010035597 sphingosine kinase Proteins 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 125000004434 sulfur atom Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 230000001687 destabilization Effects 0.000 claims 1
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Substances C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 230000002132 lysosomal effect Effects 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 230000017854 proteolysis Effects 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11185208P | 2008-11-06 | 2008-11-06 | |
| US61/111,852 | 2008-11-06 | ||
| PCT/US2009/063586 WO2010054223A1 (en) | 2008-11-06 | 2009-11-06 | Lysosomotropic inhibitors of acid ceramidase |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012508249A JP2012508249A (ja) | 2012-04-05 |
| JP2012508249A5 true JP2012508249A5 (enExample) | 2012-12-20 |
| JP5721631B2 JP5721631B2 (ja) | 2015-05-20 |
Family
ID=42153265
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011535698A Active JP5721631B2 (ja) | 2008-11-06 | 2009-11-06 | 酸性セラミダーゼのリソソーム親和性阻害剤 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US8697379B2 (enExample) |
| EP (1) | EP2348839B1 (enExample) |
| JP (1) | JP5721631B2 (enExample) |
| CN (1) | CN102368905B (enExample) |
| AU (1) | AU2009313400A1 (enExample) |
| BR (1) | BRPI0921278A2 (enExample) |
| CA (1) | CA2742866C (enExample) |
| RU (1) | RU2011117722A (enExample) |
| WO (1) | WO2010054223A1 (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006050264A1 (en) | 2004-10-29 | 2006-05-11 | Musc Foundation For Research Development | Cationic ceramides, and analogs thereof, and their use for preventing or treating cancer |
| WO2006050265A2 (en) * | 2004-10-29 | 2006-05-11 | Musc Foundation For Research Development | Ceramides and apoptosis-signaling ligand |
| CN102368905B (zh) | 2008-11-06 | 2015-04-01 | 南卡罗来纳医科大学研究发展基金会 | 酸性神经酰胺酶的向溶酶体抑制剂 |
| WO2010078247A1 (en) * | 2008-12-30 | 2010-07-08 | Musc Foundation For Research Development | Sphingo-guanidines and their use as inhibitors of sphingosine kinase |
| ES2791760T3 (es) | 2011-09-07 | 2020-11-05 | Sinai School Medicine | Ceramidasa y diferenciación celular |
| ITMI20120921A1 (it) * | 2012-05-28 | 2013-11-29 | Fond Istituto Italiano Di Tec Nologia 45 | Inibitori della ceramidasi acida e loro usi come medicamenti |
| ITMI20120923A1 (it) | 2012-05-28 | 2013-11-29 | Fond Istituto Italiano Di Tec Nologia 45 | Inibitori della ceramidasi acida e loro usi come medicamenti |
| HUE051020T2 (hu) * | 2012-06-01 | 2021-01-28 | Icahn School Med Mount Sinai | A ceramid szintjei a fertõzések kezelésében és megelõzésében |
| JP6832158B2 (ja) | 2013-03-14 | 2021-02-24 | アイカーン スクール オブ メディシン アット マウント サイナイ | 治療用酸性セラミダーゼ組成物ならびにそれを作製および使用する方法 |
| WO2015119393A1 (ko) * | 2014-02-04 | 2015-08-13 | (주)네오팜 | 발모촉진용 또는 탈모방지용 조성물 |
| KR20150091983A (ko) * | 2014-02-04 | 2015-08-12 | (주)네오팜 | 발모촉진용 또는 탈모방지용 조성물 |
| WO2015173168A1 (en) | 2014-05-12 | 2015-11-19 | Fondazione Istituto Italiano Di Tecnologia | Benzoxazolone derivatives as acid ceramidase inhibitors, and their use as medicaments |
| WO2015173169A1 (en) | 2014-05-12 | 2015-11-19 | Fondazione Istituto Italiano Di Tecnologia | Substituted benzoxazolone derivatives as acid ceramidase inhibitors, and their use as medicaments |
| WO2018200931A1 (en) * | 2017-04-28 | 2018-11-01 | University Of Virginia Patent Foundation | Compositions and methods for treating cancer |
| CN110598636B (zh) * | 2019-09-09 | 2023-01-17 | 哈尔滨工业大学 | 一种基于特征迁移的舰船目标识别方法 |
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| US2515465A (en) | 1946-03-22 | 1950-07-18 | Merck & Co Inc | Preparation of 2-alkyl-4-isopropylidene-5(4)-oxazolones |
| GB630712A (en) | 1946-03-22 | 1949-10-19 | Merck & Co Inc | Process of preparing intermediates useful in the preparation of penicill amine |
| GB844431A (en) * | 1957-12-07 | 1960-08-10 | Boehringer & Soehne Gmbh | Injectable aqueous solutions of chloramphenicol |
| US3466292A (en) | 1966-05-13 | 1969-09-09 | Upjohn Co | Diazatricyclododecanediones and diazatricyclododecadiendiones |
| GB1307539A (en) * | 1970-06-25 | 1973-02-21 | Smith Kline French Lab | Thiourea derivatives |
| US4016287A (en) | 1972-07-17 | 1977-04-05 | Boehringer Ingelheim Gmbh | Dermatological compositions containing an acylamino-carboxylic acid or an alkyl ester thereof |
| DE2408813A1 (de) | 1974-02-23 | 1975-09-04 | Agfa Gevaert Ag | N-carbamoyloxypyridiniumsalze und verfahren zur herstellung derselben |
| US4481203A (en) | 1977-04-05 | 1984-11-06 | Taiho Pharmaceutical Company, Limited | Composition containing 1-(n-hexylcarbamoyl)-5-fluorouracil and uracil |
| DE2817494A1 (de) | 1977-05-03 | 1978-11-09 | Continental Pharma | Aminoalkohol-derivat |
| US4151198A (en) | 1978-06-02 | 1979-04-24 | American Cyanamid Company | Resolution of N-acyl-DL (+)-phenylalanines |
| US4283541A (en) | 1980-05-27 | 1981-08-11 | Usv Pharmaceutical Corporation | Pyridylacyl-hydroxamates |
| US4544670A (en) | 1982-08-24 | 1985-10-01 | William H. Rorer, Inc. | Method of treating coccidiosis with acyl guanidines |
| US4897355A (en) | 1985-01-07 | 1990-01-30 | Syntex (U.S.A.) Inc. | N[ω,(ω-1)-dialkyloxy]- and N-[ω,(ω-1)-dialkenyloxy]-alk-1-yl-N,N,N-tetrasubstituted ammonium lipids and uses therefor |
| US4937232A (en) | 1986-09-15 | 1990-06-26 | Duke University | Inhibition of protein kinase C by long-chain bases |
| EP0310545A3 (de) | 1987-09-02 | 1989-07-26 | Ciba-Geigy Ag | Cyanoguanidine als Härter für Epoxidharze |
| US5262568A (en) | 1990-03-02 | 1993-11-16 | State Of Oregon | Tri- and tetra-substituted guanidines and their use as excitatory amino acid antagonists |
| US5679350A (en) | 1992-05-28 | 1997-10-21 | The University Of Toledo | Method of delivery of a medicament to a cancer cell using a pathway of plasminogen activator material |
| US5369030A (en) | 1992-09-11 | 1994-11-29 | Duke University | Method of inducing cellular differentiations and altering cell phenotype using ceramide analogs |
| WO1995006037A1 (en) * | 1993-08-27 | 1995-03-02 | Vrije Universiteit | New imidazole derivatives having agonistic or antagonistic activity on the histamine h3 receptor |
| US5916911A (en) | 1995-09-20 | 1999-06-29 | The Regents Of The University Of Michigan | Amino ceramide--like compounds and therapeutic methods of use |
| US5830916A (en) | 1996-05-23 | 1998-11-03 | Duke University | Inhibitor of ceramidase |
| DE19621038A1 (de) | 1996-05-24 | 1997-11-27 | Boehringer Ingelheim Kg | Aminoguanidine, Verfahren zu ihrer Herstellung und Arzneimittel, die diese Verbindungen enthalten |
| US6649362B2 (en) | 1997-09-08 | 2003-11-18 | Medvet Science Pty. Ltd. | Screening method for an agent having an effect on a sphingosine kinase signaling pathway |
| AU765809B2 (en) | 1998-02-12 | 2003-10-02 | Emory University | Sphingolipid derivatives and their methods of use |
| JP2002529068A (ja) | 1998-11-06 | 2002-09-10 | マスク ファウンデーション フォー リサーチ デヴェロップメント | Ｆａｓ−誘導アポトーシスを用いた腫瘍の治療方法 |
| US6756504B2 (en) | 2000-04-19 | 2004-06-29 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Sphingolipids |
| WO2001079152A1 (en) | 2000-04-19 | 2001-10-25 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Sphingolipids |
| US6696081B2 (en) | 2000-06-09 | 2004-02-24 | Duke University | Carbohydrate based lipid compositions and supramolecular structures comprising same |
| CA2421585A1 (en) | 2000-09-11 | 2002-03-21 | Musc Foundation For Research Development | Method and composition for treating tumors by selective induction of apoptosis |
| WO2003005965A2 (en) | 2001-07-11 | 2003-01-23 | Musc Foundation For Research Development | Modulators of ceramidase and methods of use based thereon |
| JP2004210733A (ja) * | 2003-01-07 | 2004-07-29 | Kyowa Hakko Kogyo Co Ltd | アリールスルファマート誘導体 |
| JP2006516603A (ja) * | 2003-01-27 | 2006-07-06 | ファイザー・プロダクツ・インク | イソチアゾール誘導体 |
| JP2006518390A (ja) | 2003-02-19 | 2006-08-10 | エンダシア，インコーポレイテッド | Ａ１アデノシンレセプターアンタゴニスト |
| WO2005051406A1 (ja) * | 2003-11-28 | 2005-06-09 | Takara Bio Inc. | セラミダーゼ阻害剤 |
| PL1725540T3 (pl) | 2004-03-05 | 2013-02-28 | Hoffmann La Roche | Diaminopirymidyny jako antagoniści p2x3 i p2x2/3 |
| JP2005336174A (ja) * | 2004-04-27 | 2005-12-08 | Santen Pharmaceut Co Ltd | 変形性関節症治療剤 |
| WO2006050265A2 (en) | 2004-10-29 | 2006-05-11 | Musc Foundation For Research Development | Ceramides and apoptosis-signaling ligand |
| WO2006050264A1 (en) | 2004-10-29 | 2006-05-11 | Musc Foundation For Research Development | Cationic ceramides, and analogs thereof, and their use for preventing or treating cancer |
| JP2006298807A (ja) * | 2005-04-19 | 2006-11-02 | Lead Chemical Co Ltd | 新規化合物及びその用途 |
| AU2006261327B2 (en) | 2005-06-17 | 2012-07-05 | Apogee Biotechnology Corporation | Sphingosine kinase inhibitors |
| EP2004188B1 (en) * | 2006-03-31 | 2010-09-01 | Janssen Pharmaceutica NV | Benzoimidazol-2-yl pyridines as modulators of the histamine h4 receptor |
| MX2009006467A (es) * | 2006-12-13 | 2009-08-21 | Schering Plough Ltd | Profarmacos solubles en agua de cloranfenicol, tiamfenicol y analogos de los mismos. |
| CN102368905B (zh) | 2008-11-06 | 2015-04-01 | 南卡罗来纳医科大学研究发展基金会 | 酸性神经酰胺酶的向溶酶体抑制剂 |
| WO2010078247A1 (en) | 2008-12-30 | 2010-07-08 | Musc Foundation For Research Development | Sphingo-guanidines and their use as inhibitors of sphingosine kinase |
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2009
- 2009-11-06 CN CN200980154007.6A patent/CN102368905B/zh not_active Expired - Fee Related
- 2009-11-06 JP JP2011535698A patent/JP5721631B2/ja active Active
- 2009-11-06 BR BRPI0921278-7A patent/BRPI0921278A2/pt not_active Application Discontinuation
- 2009-11-06 RU RU2011117722/13A patent/RU2011117722A/ru not_active Application Discontinuation
- 2009-11-06 CA CA2742866A patent/CA2742866C/en not_active Expired - Fee Related
- 2009-11-06 AU AU2009313400A patent/AU2009313400A1/en not_active Abandoned
- 2009-11-06 US US13/127,888 patent/US8697379B2/en not_active Expired - Fee Related
- 2009-11-06 EP EP09825496.4A patent/EP2348839B1/en active Active
- 2009-11-06 WO PCT/US2009/063586 patent/WO2010054223A1/en not_active Ceased