JP2008528505A5 - - Google Patents
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- Publication number
- JP2008528505A5 JP2008528505A5 JP2007552311A JP2007552311A JP2008528505A5 JP 2008528505 A5 JP2008528505 A5 JP 2008528505A5 JP 2007552311 A JP2007552311 A JP 2007552311A JP 2007552311 A JP2007552311 A JP 2007552311A JP 2008528505 A5 JP2008528505 A5 JP 2008528505A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- sulfhydryl
- hydroxyl
- amino
- formula
- 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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- 125000000217 alkyl group Chemical group 0.000 claims 45
- 239000003814 drug Substances 0.000 claims 41
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 29
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 29
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 29
- 125000003118 aryl group Chemical group 0.000 claims 18
- 125000000753 cycloalkyl group Chemical group 0.000 claims 17
- 125000003545 alkoxy group Chemical group 0.000 claims 16
- 125000002252 acyl group Chemical group 0.000 claims 15
- 125000004104 aryloxy group Chemical group 0.000 claims 15
- 229910052736 halogen Inorganic materials 0.000 claims 15
- 150000002367 halogens Chemical class 0.000 claims 15
- 125000001072 heteroaryl group Chemical group 0.000 claims 15
- -1 nitro, sulfo Chemical group 0.000 claims 15
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 14
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 14
- 229910052739 hydrogen Inorganic materials 0.000 claims 14
- 239000001257 hydrogen Substances 0.000 claims 14
- 239000000651 prodrug Substances 0.000 claims 14
- 229940002612 prodrugs Drugs 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 14
- 239000011780 sodium chloride Substances 0.000 claims 14
- 230000002401 inhibitory effect Effects 0.000 claims 11
- 201000010099 disease Diseases 0.000 claims 8
- 210000004027 cells Anatomy 0.000 claims 4
- 200000000018 inflammatory disease Diseases 0.000 claims 4
- 230000001404 mediated Effects 0.000 claims 4
- 206010003816 Autoimmune disease Diseases 0.000 claims 3
- 201000009596 autoimmune hypersensitivity disease Diseases 0.000 claims 3
- 210000004698 Lymphocytes Anatomy 0.000 claims 2
- 230000000926 neurological Effects 0.000 claims 2
- 208000006673 Asthma Diseases 0.000 claims 1
- 206010003736 Attention deficit/hyperactivity disease Diseases 0.000 claims 1
- 102000004127 Cytokines Human genes 0.000 claims 1
- 108090000695 Cytokines Proteins 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 206010021425 Immune system disease Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 102000008070 Interferon-gamma Human genes 0.000 claims 1
- 108010074328 Interferon-gamma Proteins 0.000 claims 1
- 102000003816 Interleukin-13 Human genes 0.000 claims 1
- 108090000176 Interleukin-13 Proteins 0.000 claims 1
- 102000004890 Interleukin-8 Human genes 0.000 claims 1
- 108090001007 Interleukin-8 Proteins 0.000 claims 1
- 229940096397 Interleukin-8 Drugs 0.000 claims 1
- XKTZWUACRZHVAN-VADRZIEHSA-N Interleukin-8 Chemical compound C([C@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@@H](NC(C)=O)CCSC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N[C@@H](CCSC)C(=O)N1[C@H](CCC1)C(=O)N1[C@H](CCC1)C(=O)N[C@@H](C)C(=O)N[C@H](CC(O)=O)C(=O)N[C@H](CCC(O)=O)C(=O)N[C@H](CC(O)=O)C(=O)N[C@H](CC=1C=CC(O)=CC=1)C(=O)N[C@H](CO)C(=O)N1[C@H](CCC1)C(N)=O)C1=CC=CC=C1 XKTZWUACRZHVAN-VADRZIEHSA-N 0.000 claims 1
- 208000009856 Lung Disease Diseases 0.000 claims 1
- 210000001616 Monocytes Anatomy 0.000 claims 1
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 claims 1
- 108010001801 Tumor Necrosis Factor-alpha Proteins 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 201000005794 allergic hypersensitivity disease Diseases 0.000 claims 1
- 239000002269 analeptic agent Substances 0.000 claims 1
- 230000020411 cell activation Effects 0.000 claims 1
- 239000000221 dopamine uptake inhibitor Substances 0.000 claims 1
- 230000028993 immune response Effects 0.000 claims 1
- 230000002757 inflammatory Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 229960003130 interferon gamma Drugs 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 230000000770 pro-inflamatory Effects 0.000 claims 1
- 230000035755 proliferation Effects 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 0 *OC(C(C1NCCCC1)C1=CC=*=CC=C1)=O Chemical compound *OC(C(C1NCCCC1)C1=CC=*=CC=C1)=O 0.000 description 1
Claims (27)
- 前記T細胞媒介型の疾患又は病状が、自己免疫性の疾患又は病状である、請求項3記載の治療剤。
- 前記自己免疫性の疾患又は病状が多発性硬化症である、請求項4記載の治療剤。
- 前記自己免疫性の疾患又は病状が全身性エリテマトーデスである、請求項4記載の治療剤。
- 前記T細胞媒介型の疾患又は病状がT細胞媒介肺疾患である、請求項3記載の治療剤。
- 前記炎症性の疾患又は病状が、喘息である、請求項15記載の治療剤。
- 前記炎症性の疾患又は病状が、炎症性の神経疾患又は神経病状である、請求項15記載の治療剤。
- 第1の疾患又は病状が、中枢神経系興奮剤又はドーパミン取り込み阻害因子で治療可能な神経性の疾患又は病状であり、かつ第2の疾患又は病状が、免疫性又は炎症性の疾患若しくは病状である、併存性の疾患又は病状を治療するための治療剤であって、前記治療剤は、式I:
R1は、それぞれ独立して、アリール、ヘテロアリール、アルキル、シクロアルキル、アルコキシ、アリールオキシ、アシル、カルボキシル、ヒドロキシル、ハロゲン、アミノ、ニトロ、スルホ、又はスルフヒドリルであり、ここで各アルキルは、ヒドロキシル、アミノ、又はスルフヒドリルで選択的に置換されており;かつ
R2は、水素又は低級アルキルである)
で示される化合物、又はその塩若しくはプロドラッグの有効量を含む、治療剤。 - 前記併存性の疾患が、アレルギー及び注意欠陥/多動性障害である、請求項20記載の治療剤。
- R1が、それぞれ独立して、アリール、ヘテロアリール、アルキル、シクロアルキル、アルコキシ、ヒドロキシル、ハロゲン、アミノ、ニトロ、スルホ又はスルフヒドリルである、請求項1乃至21のいずれか一項に記載の治療剤。
- R1が、それぞれ独立して、アリール、アルキル、シクロアルキル、アルコキシ、アリールオキシ又はアシルである、請求項1乃至21のいずれか一項に記載の治療剤。
- R1が、それぞれ独立して、アリール、アルキル又はシクロアルキルである、請求項1乃至21のいずれか一項に記載の治療剤。
- R1が、それぞれ独立してアリールである、1乃至21のいずれか一項に記載の治療剤。
- n=1である、請求項1乃至21のいずれか一項に記載の治療剤。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US64577805P | 2005-01-20 | 2005-01-20 | |
US60/645,778 | 2005-01-20 | ||
PCT/US2006/002181 WO2006078984A2 (en) | 2005-01-20 | 2006-01-20 | Uses of methylphenidate derivatives |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2013048099A Division JP5681226B2 (ja) | 2005-01-20 | 2013-03-11 | メチルフェニデート誘導体を含む治療剤 |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2008528505A JP2008528505A (ja) | 2008-07-31 |
JP2008528505A5 true JP2008528505A5 (ja) | 2009-03-05 |
JP5274844B2 JP5274844B2 (ja) | 2013-08-28 |
Family
ID=36692960
Family Applications (3)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2007552311A Expired - Fee Related JP5274844B2 (ja) | 2005-01-20 | 2006-01-20 | メチルフェニデート誘導体を含む治療剤 |
JP2013048099A Expired - Fee Related JP5681226B2 (ja) | 2005-01-20 | 2013-03-11 | メチルフェニデート誘導体を含む治療剤 |
JP2014207423A Withdrawn JP2015003931A (ja) | 2005-01-20 | 2014-10-08 | メチルフェニデート誘導体を含む治療剤 |
Family Applications After (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2013048099A Expired - Fee Related JP5681226B2 (ja) | 2005-01-20 | 2013-03-11 | メチルフェニデート誘導体を含む治療剤 |
JP2014207423A Withdrawn JP2015003931A (ja) | 2005-01-20 | 2014-10-08 | メチルフェニデート誘導体を含む治療剤 |
Country Status (10)
Country | Link |
---|---|
US (1) | US20060183773A1 (ja) |
EP (1) | EP1845780B1 (ja) |
JP (3) | JP5274844B2 (ja) |
CN (1) | CN101123965B (ja) |
AT (1) | ATE517623T1 (ja) |
ES (1) | ES2372004T3 (ja) |
HR (1) | HRP20110779T1 (ja) |
PL (1) | PL1845780T3 (ja) |
SI (1) | SI1845780T1 (ja) |
WO (1) | WO2006078984A2 (ja) |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU2006206410B2 (en) | 2005-01-20 | 2012-08-30 | Ampio Pharmaceuticals, Inc. | Methylphenidate derivatives and uses of them |
WO2009146320A1 (en) | 2008-05-27 | 2009-12-03 | Dmi Life Sciences, Inc. | Therapeutic methods and compounds |
CN102134208B (zh) * | 2010-01-27 | 2014-05-14 | 爱斯特(成都)医药技术有限公司 | [r,r]-哌甲酯中间体及其类似物以及它们的合成与应用 |
US10085414B2 (en) * | 2011-05-19 | 2018-10-02 | Gilrose Pharmaceuticals, Llc | Pre-frontal cortex processing disorder speech, gait and limb impairments treatment |
SG10201408115SA (en) * | 2014-12-05 | 2016-07-28 | Chakra Biotech Pte Ltd | Use of tetrahydropyridines in the treatment of sodium channel related disease and disorders |
SG11201702514PA (en) * | 2015-01-09 | 2017-07-28 | Mitsubishi Electric Corp | Outdoor unit and air-conditioning apparatus |
JP7199656B2 (ja) * | 2018-12-07 | 2023-01-06 | 日本たばこ産業株式会社 | 注意欠如・多動症又は注意欠如・多動性障害の評価方法及び評価を補助するための方法、並びに注意欠如・多動症又は注意欠如・多動性障害を評価するためのデータ取得方法 |
Family Cites Families (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2507631A (en) * | 1944-01-19 | 1950-05-16 | Ciba Pharm Prod Inc | Pyridine and piperidine compounds and process of making same |
US2957880A (en) * | 1953-12-23 | 1960-10-25 | Ciba Pharm Prod Inc | Process for the conversion of stereoisomers |
US5407926A (en) * | 1987-12-29 | 1995-04-18 | Alcon Laboratories, Inc. | Ophthalmic composition |
NZ283658A (en) * | 1994-04-04 | 1999-09-29 | William R Freeman | Compositions and treatment of increased intraocular pressure with phosphonyl-alkyloxy-pyrimidines/purines (nucleosides) |
US5658955A (en) * | 1994-11-01 | 1997-08-19 | Hitzig; Pietr | Combined use of dopamine and serotonin agonists in the treatment of immune disorders |
MXPA98000395A (es) * | 1995-07-14 | 2005-04-29 | Medeva Europ Ltd | Composicion que comprende d-treo-metilfenidato y otra droga. |
US5922736A (en) * | 1995-12-04 | 1999-07-13 | Celegene Corporation | Chronic, bolus administration of D-threo methylphenidate |
US5908850A (en) * | 1995-12-04 | 1999-06-01 | Celgene Corporation | Method of treating attention deficit disorders with d-threo methylphenidate |
US6486177B2 (en) * | 1995-12-04 | 2002-11-26 | Celgene Corporation | Methods for treatment of cognitive and menopausal disorders with D-threo methylphenidate |
US5859249A (en) * | 1997-02-19 | 1999-01-12 | Takasago International Corporation | 2-phenyl-2-(2'-piperidinylidene)acetate derivative, process for manufacturing the same, and process for manufacturing optically active 2-phenyl-2-(2'-piperidinyl)acetate derivative by asymmetrically hydrogenating the same |
US6210705B1 (en) * | 1997-12-15 | 2001-04-03 | Noven Pharmaceuticals, Nc. | Compositions and methods for treatment of attention deficit disorder and attention deficit/hyperactivity disorder with methylphenidate |
US6395752B1 (en) * | 1999-03-04 | 2002-05-28 | Pharmaquest Limited | Method of treating depression using 1-threo-methylphenidate |
US6127385A (en) * | 1999-03-04 | 2000-10-03 | Pharmaquest Limited | Method of treating depression using l-threo-methylphenidate |
US6025502A (en) * | 1999-03-19 | 2000-02-15 | The Trustees Of The University Of Pennsylvania | Enantopselective synthesis of methyl phenidate |
DE19927080A1 (de) * | 1999-06-15 | 2000-12-21 | Zahnradfabrik Friedrichshafen | Zahnradlagerung in Getrieben |
US20020132793A1 (en) * | 2000-08-28 | 2002-09-19 | Mel Epstein | Use of methylphenidate compounds to enhance memory |
US20050101582A1 (en) * | 2003-11-12 | 2005-05-12 | Allergan, Inc. | Compositions and methods for treating a posterior segment of an eye |
US20050192290A1 (en) * | 2004-01-13 | 2005-09-01 | Isaac Melamed | Treatment of behavioral disorders |
AU2006206410B2 (en) * | 2005-01-20 | 2012-08-30 | Ampio Pharmaceuticals, Inc. | Methylphenidate derivatives and uses of them |
-
2006
- 2006-01-20 JP JP2007552311A patent/JP5274844B2/ja not_active Expired - Fee Related
- 2006-01-20 WO PCT/US2006/002181 patent/WO2006078984A2/en active Application Filing
- 2006-01-20 ES ES06719144T patent/ES2372004T3/es active Active
- 2006-01-20 SI SI200631125T patent/SI1845780T1/sl unknown
- 2006-01-20 US US11/336,436 patent/US20060183773A1/en not_active Abandoned
- 2006-01-20 EP EP06719144A patent/EP1845780B1/en active Active
- 2006-01-20 PL PL06719144T patent/PL1845780T3/pl unknown
- 2006-01-20 AT AT06719144T patent/ATE517623T1/de not_active IP Right Cessation
- 2006-01-20 CN CN2006800055421A patent/CN101123965B/zh not_active Expired - Fee Related
-
2011
- 2011-10-26 HR HR20110779T patent/HRP20110779T1/hr unknown
-
2013
- 2013-03-11 JP JP2013048099A patent/JP5681226B2/ja not_active Expired - Fee Related
-
2014
- 2014-10-08 JP JP2014207423A patent/JP2015003931A/ja not_active Withdrawn