JP5047782B2 - フィコトキシン及びその使用 - Google Patents
フィコトキシン及びその使用 Download PDFInfo
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- JP5047782B2 JP5047782B2 JP2007511659A JP2007511659A JP5047782B2 JP 5047782 B2 JP5047782 B2 JP 5047782B2 JP 2007511659 A JP2007511659 A JP 2007511659A JP 2007511659 A JP2007511659 A JP 2007511659A JP 5047782 B2 JP5047782 B2 JP 5047782B2
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- 0 C[*@]([C@@]([C@](C*)N(*)C(*1C[C@](C)(*)C2(*)*)=C)([C@]12N1)N)C1=N* Chemical compound C[*@]([C@@]([C@](C*)N(*)C(*1C[C@](C)(*)C2(*)*)=C)([C@]12N1)N)C1=N* 0.000 description 2
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- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Description
この出願の発明に関連する先行技術文献情報としては、以下のものがある(国際出願日以降国際段階で引用された文献及び他国に国内移行した際に引用された文献を含む)。
R1及びR5はそれぞれ、−H及び−OHから成る群から選択され、R2及びR3はそれぞれ、−H及び−OSO 3 − から成る群から独立して選択され、及びR4は、−H、−OH、−OC(O)NH 2 、−OC(O)NHSO 3 − 、及び−OC(O)CH 3 から成る群から選択されるものであるが、但し、R2及びR3のうちのいずれか1つは−OSO 3 − であるか、若しくはR4は−OC(O)NHSO 3 − でなければならないものである。
毒素の各用量は、ゴニオトキシン(GTX2/GTX3)混合物の活性の10〜400ユニットを含み、図1の図に示された2〜20の筋肉ポイントにおいて局所的に筋肉内へ浸透させた。各注入ポイントには、0.1〜0.2ml(10〜20ユニット)の毒素溶液を注入し、溶液1ミリリットルにつきGTX2/GTX3混合物の活性の100ユニットを含むものである。担体は、0.9%塩化ナトリウム滅菌溶液であり、保存料は無添加である。この用量は、例えば医者に処方されるか又は痛みを最小限にするために患者の要求に応じて、4週間毎に繰り返した。
毒素の各用量は、ゴニオトキシン(GTX2/GTX3)混合物の活性の10〜400ユニットを含み、図2の図に従って2〜20の筋肉ポイントにおいて局所的に筋肉内へ浸透させた。各注入ポイントには、0.1ml(10ユニット)の毒素溶液を注入し、溶液1ミリリットルにつきGTX2/GTX3混合物の活性の100ユニットを含む。担体は、0.9%塩化ナトリウム滅菌溶液であり、保存料は無添加である。この用量は、例えば医者に処方されるか又は患者の要求に応じて、4週間毎に繰り返した。
毒素の各用量は、ゴニオトキシン(GTX2/GTX3)混合物の活性の10〜400ユニットを含み、2〜4投与ポイントを介して眼窩筋へ局所的に筋肉内浸透させた。付加的な局所的投与ポイントは、医者により及び/若しくは各患者の病状の深刻さに従って決定されたように、他の顔面筋肉において使用した。各注入ポイントへは、0.1〜0.4ml(10〜40ユニット活性)の毒素溶液を注入し、溶液1ミリリットルにつきGTX2/GTX3混合物の活性の100ユニットを含む。担体は、0.9%塩化ナトリウム滅菌溶液であり、保存料は無添加である。この投与は、医者に処方されるか又は患者の要求に応じて2〜4週間毎に繰り返した。
エトキシジグリコール 6.500% w/w
ラウレス−7 1.000% w/w
ジアゾリジニル尿素 0.300% w/w
メチルパラベン 0.150% w/w
プロピルパラベン 0.050% w/w
ヒドロキシエチルセルロース 1.500% w/w
毒素GTX2/GTX3 0.01〜0.0001% w/w
水 100% w/wになるまで
エトキシジグリコール:浸透促進剤(有機溶媒)
ラウレス−7:浸透促進剤(界面活性剤)
ジアゾリジニル尿素、メチルパラベン、プロピルパラベン:保存料
ヒドロキシエチルセルロース:増粘剤
ヒドロキシエチルセルロース以外の全成分を水に溶解し、攪拌して透明で均一な溶液にした。ボルテックス混合でヒドロキシエチルセルロースポリマーを分散させ、ボルテックスなしで滑らかで透明のゲル状になるまで攪拌を続けた。
ワセリン 75.000% w/w
セスキオレイン酸ソルビタン 10.000% w/w
白ろう 10.000% w/w
毒素GTX2/GTX3 0.01〜0.0001%w/w
水 100%になるまで
ワセリン:皮膚軟化軟膏基剤
セスキオレイン酸ソルビタン:乳化剤、浸透促進剤
白ろう:増粘剤、安定剤
ワセリン、セスキオレイン酸ソルビタン、及び白ロウを60℃で溶解し、均一になるまで攪拌した。ゆっくりと毒素の水溶液を入れ、軟膏が凝固するまで攪拌を続けた。
2人の患者は、手掌の発汗過多の治療を受けた。患者の症候に合わせ、医者は毒素注射ポイントの数(2〜20)を、基本的に指及び手掌の一般注射図に従って決定した。毒素の各用量は、GTX2/GTX3混合物の10〜400活性単位を含み、2〜10筋肉ポイントにおいて局所的に筋肉内へ浸透させた。各注射ポイントへは、0.1〜0.2ml(10〜20単位)の毒素溶液を注入し、1ミリリットルにつき100活性単位のGTX2/GTX3混合物を含む。この溶液は0.9%塩化ナトリウム滅菌溶液で製造し、保存料は無添加である。
Claims (16)
- 線維筋痛症、半側顔面痙攣、緊張性頭痛から選択される少なくとも1つの病気を治療するための薬物に使用される組成物であって、
以下の化学式Iで示される三環式3,4−プロピノペルヒドロプリンを少なくとも1つと、薬学的に許容可能な担体とを含む組成物であり、前記化学式(I)は、
R1及びR5はそれぞれ、−H及び−OHから選択されるものであり、
R2及びR3はそれぞれ、−H及び−OSO3 −から選択されるものであり、
R4は−H、−OH、−OC(O)NH2、−OC(O)NHSO3 −、及び−OC(O)CH3から選択されるものであり、
ただし、R2及びR3のいずれか1つは−OSO3 −であるか、若しくはR4は−OC(O)NHSO3 −である
組成物。 - 請求項1の組成物において、前記化学式Iの化合物の少なくとも1つは、GTX−1、GTX−2、GTX−3、GTX−4、及びGTX−5から選択されるものである、組成物。
- 請求項1の組成物において、この組成物は、GTX−2及びGTX−3を含むものである、組成物。
- 請求項1〜3のいずれか1つの組成物において、前記薬物は、筋肉注射によって投与されるものである、組成物。
- 請求項1〜3のいずれか1つの組成物において、前記薬物は、局所投与に適用されるものである、組成物。
- 請求項1〜3のいずれか1つの組成物において、前記病気は、線維筋痛症である、組成物。
- 請求項1〜3のいずれか1つの組成物において、前記病気は、半側顔面痙攣である、組成物。
- 請求項1〜3のいずれか1つの組成物において、前記病気は、緊張性頭痛である、組成物。
- しわを軽減する或いは除去する組成物を製造するための、以下の化学式Iで示される三環式3,4−プロピノペルヒドロプリンの少なくとも1つの使用であって、
前記組成物は、薬学的に許容可能な担体と共にその処置を必要とする患者に投与されるものであり、前記化学式Iは、
R1及びR5はそれぞれ、−H及び−OHから選択されるものであり、
R2及びR3はそれぞれ、−H及び−OSO3 −から選択されるものであり、
R4は−H、−OH、−OC(O)NH2、−OC(O)NHSO3 −、及び−OC(O)CH3から選択されるものであり、
ただし、R2及びR3のいずれか1つは−OSO3 −であるか、若しくはR4は−OC(O)NHSO3 −であり、
前記しわは、ボツリヌス菌毒素A耐性のしわである、
使用。 - 請求項9の使用において、前記組成物は、筋肉内に注入されるものである、使用。
- 請求項9の使用において、前記化学式Iの少なくとも1つの化合物は、GTX−1、GTX−2、GTX−3、GTX−4、及びGTX−5から選択されるものである、使用。
- 請求項11の使用において、前記組成物は、GTX−2及びGTX−3を含むものである、使用。
- 請求項10の使用において、前記組成物は、複数の注入ポイントで注入されるものである、使用。
- 請求項13の使用において、前記複数の注入ポイントの位置は、処置される特定の状態に対する予定処置プランに基づいて、少なくとも一部は決定されているものである、使用。
- 請求項9の使用において、前記組成物は、経皮的に適用されるものである、使用。
- 請求項1の組成物において、前記半側顔面痙攣は、ボツリヌス菌毒素A耐性の半側顔面痙攣である、組成物。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US56938304P | 2004-05-07 | 2004-05-07 | |
US56938004P | 2004-05-07 | 2004-05-07 | |
US60/569,383 | 2004-05-07 | ||
US60/569,380 | 2004-05-07 | ||
PCT/US2005/015946 WO2005110417A1 (en) | 2004-05-07 | 2005-05-06 | Phycotoxins and uses thereof |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2007536264A JP2007536264A (ja) | 2007-12-13 |
JP2007536264A5 JP2007536264A5 (ja) | 2008-06-26 |
JP5047782B2 true JP5047782B2 (ja) | 2012-10-10 |
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ID=35393960
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2007511659A Expired - Fee Related JP5047782B2 (ja) | 2004-05-07 | 2005-05-06 | フィコトキシン及びその使用 |
JP2007511671A Pending JP2007536269A (ja) | 2004-05-07 | 2005-05-06 | ゴニオトキシンを用いた創傷の治療方法 |
Family Applications After (1)
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JP2007511671A Pending JP2007536269A (ja) | 2004-05-07 | 2005-05-06 | ゴニオトキシンを用いた創傷の治療方法 |
Country Status (10)
Country | Link |
---|---|
US (3) | US20080021051A1 (ja) |
EP (2) | EP1802250A4 (ja) |
JP (2) | JP5047782B2 (ja) |
CN (1) | CN1997373B (ja) |
AU (2) | AU2005244105B2 (ja) |
BR (2) | BRPI0510761A (ja) |
CA (3) | CA2606530C (ja) |
ES (1) | ES2646087T3 (ja) |
MX (2) | MXPA06012961A (ja) |
WO (2) | WO2005110417A1 (ja) |
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MXPA06012960A (es) * | 2004-05-07 | 2007-06-12 | Phytotox Ltd | Administracion transdermal de ficotoxinas. |
AU2006243644A1 (en) * | 2005-05-05 | 2006-11-09 | Phytotox Limited | Use of phycotoxins in veterinary applications |
US9012477B2 (en) * | 2009-01-06 | 2015-04-21 | Nuvo Research Inc. | Method of treating neuropathic pain |
US20100184685A1 (en) * | 2009-01-19 | 2010-07-22 | Zavala Jr Gerardo | Systems and methods for treating post- operative, acute, and chronic pain using an intra-muscular catheter administrated combination of a local anesthetic and a neurotoxin protein |
CL2009000723A1 (es) * | 2009-03-24 | 2009-06-19 | Proteus Sa | Metodo de purificacion industrial de ficotoxinas biologicamente activas que comprende proporcionar una cantidad adecuada de una fuente de ficotoxinas como por ejemplo el cultivo de un clon de cianobacterias. |
WO2010114973A1 (en) * | 2009-04-01 | 2010-10-07 | Jie Zhang | Methods for treating myofascial, muscle, and/or back pain |
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MX2011011698A (es) * | 2009-05-04 | 2012-02-29 | Zars Pharma Inc | Metodo para tratar dolores asociados con neuroma, entrapamiento nervioso y otras condiciones. |
US9174999B2 (en) * | 2009-05-07 | 2015-11-03 | The Board Of Trustees Of The Leland Stanford Junior University | Methods and compositions for studying, imaging, and treating pain |
CN102834096A (zh) | 2010-01-14 | 2012-12-19 | 卢福研究公司 | 用于疼痛控制的固态成型局部麻醉制剂 |
EP2533785B1 (en) * | 2010-02-10 | 2014-04-23 | Phytotox Limited | Treatment of loss of sense of touch with saxitoxin derivatives |
US20130251783A1 (en) * | 2011-09-14 | 2013-09-26 | Universitat Heidelberg | Liposomes containing permeation enhancers for oral drug delivery |
EP2638908A1 (en) * | 2012-03-16 | 2013-09-18 | Phytotox SpA | Paralytic Shellfish Poison |
EP3129381B1 (en) | 2014-04-09 | 2020-11-04 | Siteone Therapeutics Inc. | 10',11'-modified saxitoxins useful for the treatment of pain |
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JP2007536269A (ja) | 2007-12-13 |
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AU2005244116B8 (en) | 2011-03-31 |
AU2005244105A1 (en) | 2005-11-24 |
CA2606530A1 (en) | 2005-11-24 |
US20070280970A1 (en) | 2007-12-06 |
BRPI0510761A (pt) | 2007-11-20 |
EP1824488A4 (en) | 2008-07-02 |
CA2607589A1 (en) | 2005-11-24 |
AU2005244116C1 (en) | 2011-09-29 |
EP1824488B1 (en) | 2017-08-09 |
WO2005110275A1 (en) | 2005-11-24 |
US8623886B2 (en) | 2014-01-07 |
JP2007536264A (ja) | 2007-12-13 |
CN1997373B (zh) | 2010-12-22 |
MXPA06012962A (es) | 2007-06-12 |
CA2606530C (en) | 2014-01-07 |
AU2005244116A1 (en) | 2005-11-24 |
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