JP4823063B2 - Hivウイルス侵入阻害剤 - Google Patents
Hivウイルス侵入阻害剤 Download PDFInfo
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- JP4823063B2 JP4823063B2 JP2006525834A JP2006525834A JP4823063B2 JP 4823063 B2 JP4823063 B2 JP 4823063B2 JP 2006525834 A JP2006525834 A JP 2006525834A JP 2006525834 A JP2006525834 A JP 2006525834A JP 4823063 B2 JP4823063 B2 JP 4823063B2
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- ZCVNOMAJTIYNMF-MVTLZHEVSA-N C/C=C\C1=C(CO/C(/C)=C/C=C(\C)/N)NCCC1 Chemical compound C/C=C\C1=C(CO/C(/C)=C/C=C(\C)/N)NCCC1 ZCVNOMAJTIYNMF-MVTLZHEVSA-N 0.000 description 1
- WFQDTOYDVUWQMS-UHFFFAOYSA-N [O-][N+](c(cc1)ccc1F)=O Chemical compound [O-][N+](c(cc1)ccc1F)=O WFQDTOYDVUWQMS-UHFFFAOYSA-N 0.000 description 1
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- C07C233/24—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
- C07C233/29—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
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- C07C233/73—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
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- C07C235/18—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides
- C07C235/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
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- C07C235/56—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
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- C07C311/29—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
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- C07D215/08—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms with acylated ring nitrogen atom
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- C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
- C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
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- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Description
Aは、キノリニル、イソキノリニル、R1で置換されているフェニル、または−Y−X−R2で置換されている1,2,3,4−テトラヒドロキノリニルを表し、
Xは、直接結合、−(CH2)t−、−(CH2)t−NH−、−(CH2)t−NH−(CH2)p−、−(CH2)t−O−または−(CH2)t−O−(CH2)p−を表し、そしてXが直接結合以外の時にはXはCH2基を通してYと連結しており、そしてXの定義の範囲内の各CH2基は場合により−C(=O)−OHまたは−C(=O)−O−C1−4アルキルで置換されていてもよく、そして
Yは、−S(=O)2−または−C(=O)−を表し、
各tは、独立して、1、2または3から選択される整数であり、
各pは、独立して、1、2または3から選択される整数であり、
nは、独立して、0、1または2から選択される整数であり、
R1は、−NR3−Y−X−R2、−C1−4アルカンジイル−NR3−Y−X−R2、−NR3−Y−X−C(=O)−C1−6アルキル、または−C1−4アルカンジイル−NR3−Y−X−C(=O)−C1−6アルキルを表し、
R2は、C1−4アルキル、場合によりC1−4アルキルで置換されていてもよいピロリジニル、場合によりC1−4アルキルで置換されていてもよいフラニル、場合によりC1−4アルキルで置換されていてもよいピペラジニル、場合によりC1−4アルキルで置換されていてもよいピペリジニル、場合によりC1−4アルキルで置換されていてもよいチエニル、ベンゾ−1,3−ジオキソラニル、または場合によりC1−6アルキル、C1−6アルキルオキシ、ヒドロキシ、カルボキシル、C1−6アルキルオキシカルボニル、シアノ、ニトロ、ハロゲン、トリフルオロメチル、アミノ、モノ−もしくはジ(C1−6アルキル)アミノ、C1−6アルキルカルボニルアミノ、C1−6アルキルカルボニル、モノ−もしくはジ(C1−6アルキル)アミノカルボニルおよびアミノカルボニルから成る群から選択される1個以上の置換基で置換されていてもよいフェニルを表し、
R3は、水素、C1−6アルキルまたはC3−7シクロアルキルを表す]
で表される本発明の化合物、これらのN−オキサイド形態、立体化学異性体、ラセミ混合物、塩、プロドラッグ、エステルおよび代謝産物は、HIVに感染した人の治療およびそのような人の予防で用いるに有用である。
塩形態の調製は便利に適切な酸、例えば無機酸、例えばハロゲン化水素酸、例えば塩酸または臭化水素酸など、硫酸、硝酸、燐酸など、または有機酸、例えば酢酸、プロピオン酸、ヒドロキシ酢酸、乳酸、ピルビン酸、しゅう酸、マロン酸、こはく酸、マレイン酸、フマル酸、リンゴ酸、酒石酸、クエン酸、メタンスルホン酸、エタンスルホン酸、ベンゼンスルホン酸、p−トルエンスルホン酸、シクラミン酸、サリチル酸、p−アミノサリチル酸、パモ酸などを用いて実施可能である。
せることで実施可能である。
入または局所などで実施可能であり、好適な投与は個々の症例、例えば治療すべき疾患の個々の過程などに依存する。経口投与が好適である。
ースまたは澱粉、特にコーンスターチなどである。その場合の調製は乾燥した顆粒または湿った顆粒の両方として実施可能である。適切な油状賦形剤または溶媒は植物油または動物油、例えばヒマワリ油または肝油などである。水溶液またはアルコール溶液用の適切な溶媒は水、エタノール、糖溶液またはこれらの混合物である。また、ポリエチレングリコールおよびポリプロピレングリコールも他の投与形態用のさらなる助剤として用いるに有用である。
れている調合は抗菌・カビ活性材料を用いた調合であるが、それらも同様に本発明の化合物を調合する時に興味が持たれる。そこに記述されている調合物は特に経口投与に適し、抗菌・カビ剤を活性材料として含有し、シクロデキストリンまたはこれの誘導体を可溶化剤として充分な量で含有し、酸水溶液媒体を多量の液状担体として含有しかつ当該組成物の調製を非常に簡潔にするアルコール系共溶媒を含有する。また、前記調合物に薬学的に受け入れられる甘味剤および/または風味剤を添加することで味をより良くすることも可能である。
切な賦形剤にはいろいろな重合体、低分子量のオリゴマー、天然産物および界面活性剤が含まれる。好適な表面修飾剤には非イオン性およびアニオン性界面活性剤が含まれる。
スキームAに従う化合物1の製造[酢酸{4−[4−(4−メトキシ−ベンゼンスルホニルアミノ)−フェノキシ]−フェニルカルバモイル}−メチルエステル]
20gのアミノフェノールを400mlのN,N−ジメチルホルムアミド(DMF)に入れることで生じさせた室温の混合物に炭酸カリウムを30g(1.2当量)加えた。この混合物を撹拌しながらこれにパラ−フルオロニトロベンゼンを25.8g加えた。この反応混合物を室温で12時間撹拌した。その後、出発材料が消費された時点で、その混合物を水(250ml)の中に注ぎ込んだ。その溶液に塩酸溶液をpH=7になるまで添加することで酸性にした。DMFを蒸発させた後、酢酸エチルを用いて生成物を抽出した。その有機層を分離し、MgSO4で乾燥させた後、蒸発させることで中間体Aを30g(71%)得た。
式Bで表される化合物の製造
1gの中間体Aを25mlのテトラヒドロフラン(THF)に入れることで生じさせた室温の混合物に水を15mlおよび炭酸カリウムを1.18g(2当量)加えた。この混合物を撹拌しながらこれにパラ−メトキシスルホニルクロライドを988mg(1.1当量)加えた。この反応混合物を室温で4時間撹拌した。水(25ml)を加えた後、酢酸エチルを用いて生成物を抽出した。その有機層を分離し、MgSO4で乾燥させた後、蒸発させることで中間体Bを1.44g(83%)得た。
中間体Cの製造
中間体Bが1.24gの混合物をメタノールに溶解させた後、炭素に担持されているパラジウムを触媒量で加えた。この混合物を水素下室温で撹拌した。4時間後に混合物を濾過した後、溶媒を除去した。中間体Cを700mg(61%)単離した。
化合物1の製造
500mgの中間体Cを10mlのTHFに入れることで生じさせた室温の混合物に水を10mlおよび炭酸カリウムを429mg加えた。この混合物を撹拌しながらこれにアセトキシアセチルクロライドを203mg(1.1当量)加えた。この反応混合物を室温で4時間撹拌した。水(50ml)を加えた後、酢酸エチル(3x20ml)を用いて生成物を抽出した。その有機層を分離し、MgSO4で乾燥させた後、蒸発させることで化
合物1を377mg(80%)得た。
スキームBに従う化合物23の製造[フラン−2−カルボン酸{4−[1−(フラン−2−カルボニル)−1,2,3,4−テトラヒドロ−キノリン−8−イルオキシ]−フェニル}−アミド]
1gの8−ヒドロキシ−キノレインを20mlのDMFに入れることで生じさせた室温の混合物に炭酸カリウムを2.85g(1.1当量)加えた。この混合物を撹拌しながらこれにパラ−フルオロニトロベンゼンを1g加えた。この反応混合物を140℃で3時間撹拌した。その後、出発材料が消費された時点で、その混合物を水(25ml)の中に注ぎ込んだ。その溶液に塩酸溶液をpH=7になるまで添加することで酸性にした。DMFを除去した後、酢酸エチルを用いて生成物を抽出した。その有機層を分離し、MgSO4で乾燥させた後、蒸発させることで中間体Aを1.5g(81%)得た。
化合物Bの製造
中間体Aが1.5gの混合物をメタノールに溶解させた後、炭素に担持されているパラジウムを触媒量で加えた。この混合物を水素下室温で撹拌した。4時間後に混合物を濾過した後、溶媒を除去した。中間体Bを1.4g(86%)単離した。
化合物23の製造
200mgの中間体Bを10mlのTHFに入れることで生じさせた室温の混合物に水を10mlおよび炭酸カリウムを260mg加えた。この混合物を撹拌しながらこれに2−フランカルボニルクロライドを2.2当量加えた。この反応混合物を室温で12時間撹拌した。水(20ml)を加えた後、酢酸エチル(3x20ml)を用いて生成物を抽出した。その有機層を分離し、MgSO4で乾燥させた後、蒸発させることで化合物23を得た。
スキームCに従う化合物9の製造[N,N’−(オキシジ−4,1−フェニレン)−ビス(2−フランカルボキサミド)]
1gの3−シアノフェノールを20mlのDMFに入れることで生じさせた室温の混合物に炭酸カリウムを1.27g(1.1当量)加えた。この混合物を撹拌しながらこれにパラ−フルオロニトロベンゼンを1g加えた。この反応混合物を140℃で3時間撹拌した。その後、出発材料が消費された時点で、その混合物を水(25ml)の中に注ぎ込んだ。その溶液に塩酸溶液をpH=7になるまで添加することで酸性にした。DMFを除去した後、酢酸エチルを用いて生成物を抽出した。その有機層を分離し、MgSO4で乾燥させた後、蒸発させることで中間体Aを1.6g(80%)得た。
中間体Bの製造
中間体Aが1.6gの混合物をメタノールに溶解させた後、炭素に担持されているパラジウムを触媒量で加えた。この混合物を水素下室温で撹拌した。4時間後に混合物を濾過した後、溶媒を除去した。中間体Bを1.2g(85%)単離した。
化合物9の製造
300mgの中間体Bを10mlのTHFに入れることで生じさせた室温の混合物に水を10mlおよび炭酸カリウムを2.2当量加えた。この混合物を撹拌しながらこれに2−フランカルボニルクロライドを2.2当量加えた。この反応混合物を室温で12時間撹拌した。水(20ml)を加えた後、酢酸エチル(3x20ml)を用いて生成物を抽出した。その有機層を分離し、MgSO4で乾燥させた後、蒸発させることで化合物9を得た。
本化合物に試験をMT4−LTR−EGFP細胞を用いた抗ウイルス複製検定およびERA検定で受けさせた。MT4−CMV−EGFP細胞を用いて毒性を測定した。
Claims (6)
- 請求項1に記載のリストから選択される化合物を含んで成る医薬組成物。
- HIVに感染した温血動物の治療および温血動物のHIVでの感染の予防に有用な薬剤の製造における請求項1記載のリストから選択される化合物の使用。
- 前記温血動物がエイズ、エイズ関連症候群(ARC)、進行性全身性リンパ節腫脹(PGL)、HIV介在認知症およびHIV介在多発性硬化症に罹患している請求項3記載の使用。
- 前記治療がHIVと哺乳類細胞の間の結合および融合のいろいろな段階を妨害することでHIVが哺乳類細胞の中に入り込むのを阻止することを伴う請求項3または4記載の使用。
- 薬学的に無害な通常の賦形剤および助剤に加えて請求項1に記載のリストから選択される化合物の中の少なくとも1種を有効成分として有効量で含有する医薬製剤。
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EP03103362 | 2003-09-11 | ||
US50247603P | 2003-09-12 | 2003-09-12 | |
US60/502,476 | 2003-09-12 | ||
PCT/EP2004/052139 WO2005023242A1 (en) | 2003-09-11 | 2004-09-10 | Entry inhibitors of the hiv virus |
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TWI401254B (zh) | 2005-05-09 | 2013-07-11 | Hydra Biosciences Inc | 用於調節trpv3功能之化合物 |
US8916550B2 (en) | 2005-05-09 | 2014-12-23 | Hydra Biosciences, Inc. | Compounds for modulating TRPV3 function |
US7998980B2 (en) | 2006-09-15 | 2011-08-16 | Hydra Biosciences, Inc. | Compounds for modulating TRPV3 function |
CL2008001631A1 (es) * | 2007-06-06 | 2009-01-02 | Smithkline Beecham Corp | Compuestos derivados de heterociclos sustituidos, con la presencia de un grupo fenoxi, inhibidores de transcriptasa inversa; composicion farmaceutica; y uso en el tratamiento de infecciones virales por vih. |
US9066951B2 (en) * | 2008-05-29 | 2015-06-30 | Wisconsin Alumni Research Foundation | Drugs to treat HPV infection |
CN102656141B (zh) * | 2009-10-13 | 2016-04-06 | 利亘制药公司 | 模拟造血生长因子的小分子化合物及其用途 |
EP2721006A1 (en) | 2011-06-20 | 2014-04-23 | E. I. Du Pont de Nemours and Company | Heterocyclic compounds for treating helminth infections |
US9248139B2 (en) * | 2011-12-21 | 2016-02-02 | Bristol-Myers Squibb Company | Co-processing method and formulations for HIV attachment inhibitor prodrug compound and excipients |
WO2021154966A1 (en) | 2020-01-29 | 2021-08-05 | Kamari Pharma Ltd. | Compounds and compositions for use in treating skin disorders |
Citations (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS49128933A (ja) * | 1973-04-11 | 1974-12-10 | ||
JPS5176232A (ja) * | 1974-11-25 | 1976-07-01 | Inst Francais Du Petrole | Hokozokujesuteruujiamidonoseizoho |
JPH036527A (ja) * | 1989-06-02 | 1991-01-14 | Matsushita Electric Ind Co Ltd | 液晶表示素子 |
US5070096A (en) * | 1986-09-24 | 1991-12-03 | Bayer Aktiengesellschaft | Quinolinoxy phenylsulphonamides |
JPH06181264A (ja) * | 1992-12-14 | 1994-06-28 | Hitachi Ltd | 配線構造体及びその製造方法 |
JPH07164756A (ja) * | 1993-12-15 | 1995-06-27 | Nippon Paper Ind Co Ltd | 感熱記録体 |
JPH11277906A (ja) * | 1998-03-27 | 1999-10-12 | Ricoh Co Ltd | 感熱記録材料 |
WO2000013058A1 (fr) * | 1998-08-26 | 2000-03-09 | Nissan Chemical Industries, Ltd. | Agent de traitement pour couche d'alignement du cristal liquide et dispositif a cristaux liquide l'utilisant, et procede d'alignement du cristal liquide |
JP2001515470A (ja) * | 1997-02-21 | 2001-09-18 | バイエル・アクチエンゲゼルシヤフト | アリールスルホンアミド及びそれらの類似体並びに神経変性疾患の治療におけるそれらの使用 |
JP2001519808A (ja) * | 1997-04-10 | 2001-10-23 | ファルマシア・アンド・アップジョン・カンパニー | ポリ芳香族抗菌組成物 |
JP2001329053A (ja) * | 2000-05-24 | 2001-11-27 | Jsr Corp | ポリアリーレン系共重合体およびプロトン伝導膜 |
JP2002502850A (ja) * | 1998-02-06 | 2002-01-29 | マックス−プランク−ゲゼルシャフト・ツア・フェルデルング・デア・ヴィッセンシャフテン・エー・ファオ | トリプターゼ阻害物質 |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
PH30929A (en) | 1992-09-03 | 1997-12-23 | Janssen Pharmaceutica Nv | Beads having a core coated with an antifungal and a polymer. |
SK283569B6 (sk) | 1993-10-01 | 2003-09-11 | Astra Aktiebolag | Spôsob spracovania jemne deleného práškového liečiva, zariadenie na vykonávanie tohto spôsobu a aglomeráty vyrobené týmto spôsobom |
EP0904060B1 (en) | 1996-05-20 | 2003-12-10 | Janssen Pharmaceutica N.V. | Antifungal compositions with improved bioavailability |
ATE241969T1 (de) | 1997-03-26 | 2003-06-15 | Janssen Pharmaceutica Nv | Tabletten mit einem kern, der mit einem pilzbekämpfungsmittel und einem polymeren beschichtet ist |
IL163959A0 (en) * | 2002-03-11 | 2005-12-18 | Tibotec Pharm Ltd | Small molecule entry inhibitors |
-
2004
- 2004-09-10 JP JP2006525834A patent/JP4823063B2/ja not_active Expired - Fee Related
- 2004-09-10 TW TW093127475A patent/TW200518742A/zh unknown
- 2004-09-10 EA EA200600560A patent/EA010911B1/ru not_active IP Right Cessation
- 2004-09-10 NZ NZ544980A patent/NZ544980A/en unknown
- 2004-09-10 MX MXPA06002780A patent/MXPA06002780A/es active IP Right Grant
- 2004-09-10 WO PCT/EP2004/052139 patent/WO2005023242A1/en active Application Filing
- 2004-09-10 AT AT04766768T patent/ATE532509T1/de active
- 2004-09-10 BR BRPI0414199-7A patent/BRPI0414199A/pt not_active IP Right Cessation
- 2004-09-10 SG SG200806034-5A patent/SG145742A1/en unknown
- 2004-09-10 CA CA2531766A patent/CA2531766C/en not_active Expired - Fee Related
- 2004-09-10 CN CN2004800257513A patent/CN1849117B/zh not_active Expired - Fee Related
- 2004-09-10 EP EP04766768A patent/EP1667675B1/en active Active
- 2004-09-10 AU AU2004269930A patent/AU2004269930B2/en not_active Ceased
- 2004-09-10 US US10/571,325 patent/US8268885B2/en not_active Expired - Fee Related
- 2004-09-10 UA UAA200600176A patent/UA84020C2/ru unknown
-
2006
- 2006-04-10 ZA ZA200602916A patent/ZA200602916B/en unknown
Patent Citations (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS49128933A (ja) * | 1973-04-11 | 1974-12-10 | ||
JPS5176232A (ja) * | 1974-11-25 | 1976-07-01 | Inst Francais Du Petrole | Hokozokujesuteruujiamidonoseizoho |
US5070096A (en) * | 1986-09-24 | 1991-12-03 | Bayer Aktiengesellschaft | Quinolinoxy phenylsulphonamides |
JPH036527A (ja) * | 1989-06-02 | 1991-01-14 | Matsushita Electric Ind Co Ltd | 液晶表示素子 |
JPH06181264A (ja) * | 1992-12-14 | 1994-06-28 | Hitachi Ltd | 配線構造体及びその製造方法 |
JPH07164756A (ja) * | 1993-12-15 | 1995-06-27 | Nippon Paper Ind Co Ltd | 感熱記録体 |
JP2001515470A (ja) * | 1997-02-21 | 2001-09-18 | バイエル・アクチエンゲゼルシヤフト | アリールスルホンアミド及びそれらの類似体並びに神経変性疾患の治療におけるそれらの使用 |
JP2001519808A (ja) * | 1997-04-10 | 2001-10-23 | ファルマシア・アンド・アップジョン・カンパニー | ポリ芳香族抗菌組成物 |
JP2002502850A (ja) * | 1998-02-06 | 2002-01-29 | マックス−プランク−ゲゼルシャフト・ツア・フェルデルング・デア・ヴィッセンシャフテン・エー・ファオ | トリプターゼ阻害物質 |
JPH11277906A (ja) * | 1998-03-27 | 1999-10-12 | Ricoh Co Ltd | 感熱記録材料 |
WO2000013058A1 (fr) * | 1998-08-26 | 2000-03-09 | Nissan Chemical Industries, Ltd. | Agent de traitement pour couche d'alignement du cristal liquide et dispositif a cristaux liquide l'utilisant, et procede d'alignement du cristal liquide |
JP2001329053A (ja) * | 2000-05-24 | 2001-11-27 | Jsr Corp | ポリアリーレン系共重合体およびプロトン伝導膜 |
Also Published As
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EA200600560A1 (ru) | 2006-08-25 |
CN1849117B (zh) | 2010-05-26 |
ZA200602916B (en) | 2007-10-31 |
CA2531766A1 (en) | 2005-03-17 |
UA84020C2 (ru) | 2008-09-10 |
MXPA06002780A (es) | 2006-06-14 |
US8268885B2 (en) | 2012-09-18 |
AU2004269930A1 (en) | 2005-03-17 |
SG145742A1 (en) | 2008-09-29 |
CA2531766C (en) | 2012-11-27 |
ATE532509T1 (de) | 2011-11-15 |
CN1849117A (zh) | 2006-10-18 |
EP1667675A1 (en) | 2006-06-14 |
US20070066623A1 (en) | 2007-03-22 |
TW200518742A (en) | 2005-06-16 |
EA010911B1 (ru) | 2008-12-30 |
AU2004269930B2 (en) | 2011-08-04 |
WO2005023242A1 (en) | 2005-03-17 |
EP1667675B1 (en) | 2011-11-09 |
NZ544980A (en) | 2009-02-28 |
BRPI0414199A (pt) | 2006-10-31 |
JP2007505086A (ja) | 2007-03-08 |
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