ZA200602664B - Tubulin inhibitors - Google Patents
Tubulin inhibitors Download PDFInfo
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- ZA200602664B ZA200602664B ZA200602664A ZA200602664A ZA200602664B ZA 200602664 B ZA200602664 B ZA 200602664B ZA 200602664 A ZA200602664 A ZA 200602664A ZA 200602664 A ZA200602664 A ZA 200602664A ZA 200602664 B ZA200602664 B ZA 200602664B
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- South Africa
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- alkyl
- independently
- hetaryl
- aryl
- 4alkyl
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- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
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- C—CHEMISTRY; METALLURGY
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- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
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- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D241/20—Nitrogen atoms
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
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Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU2002953255A0 (en) * | 2002-12-11 | 2003-01-02 | Cytopia Research Pty Ltd | Protein kinase inhibitors |
MXPA06005686A (es) | 2003-11-20 | 2006-08-17 | Janssen Pharmaceutica Nv | 2-quinolinonas y 2-quinoxalinonas 7-fenilaquilo sustituidas como inhibidores de la poli(adp-ribosa)polimerasa. |
EP1687277B1 (en) | 2003-11-20 | 2018-04-04 | Janssen Pharmaceutica NV | 6-alkenyl and 6-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(adp-ribose) polymerase inhibitors |
ES2528302T3 (es) * | 2003-12-03 | 2015-02-06 | Ym Biosciences Australia Pty Ltd | Heterociclos con 6 anillos de nitrógeno fenilsustituidos como inhibidores de la polimerización de microtúbulos |
CN1980913B (zh) | 2004-06-30 | 2011-12-14 | 詹森药业有限公司 | 作为parp抑制剂的喹唑啉二酮衍生物 |
US7803795B2 (en) | 2004-06-30 | 2010-09-28 | Janssen Pharmaceutica N.V. | Phthalazine derivatives as parp inhibitors |
UA86237C2 (uk) | 2004-06-30 | 2009-04-10 | Янссен Фармацевтика Н.В. | Похідні заміщеного 2-алкілхіназолінону як інгібітори parp |
US20090196912A1 (en) * | 2004-07-30 | 2009-08-06 | Gpc Botech Ag | Pyridinylamines |
EP1904478B1 (en) * | 2005-06-15 | 2013-07-24 | YM BioSciences Australia Pty Ltd | Acid addition salts of n-ethyl-n'-[2-methoxy-4-(5-methyl-4-{[(1s)-1-pyridin-3-ylbutyl]amino}pyrimidin- 2-yl)phenyl]urea and uses thereof |
US8318723B2 (en) * | 2006-08-16 | 2012-11-27 | Boehringer Ingelheim International Gmbh | Pyrazine compounds, their use and methods of preparation |
DE102006049618A1 (de) * | 2006-10-20 | 2008-05-08 | Tschesche, Harald, Prof. Dr. | Triazine und Ihre Verwendung als Metalloproteinase-Inhibitoren |
LT2848610T (lt) * | 2006-11-15 | 2017-11-10 | Ym Biosciences Australia Pty Ltd | Kinazės aktyvumo inhibitoriai |
AU2013273769B2 (en) * | 2006-11-15 | 2016-05-12 | Ym Biosciences Australia Pty Ltd | Inhibitors of Kinase Activity |
EP2134691B1 (en) | 2007-03-08 | 2012-01-25 | Janssen Pharmaceutica, N.V. | Quinolinone derivatives as parp and tank inhibitors |
US8404713B2 (en) | 2007-10-26 | 2013-03-26 | Janssen Pharmaceutica Nv | Quinolinone derivatives as PARP inhibitors |
WO2009096198A1 (ja) * | 2008-02-01 | 2009-08-06 | Pharma Ip Limited Liability Intermediary Corporations | 新規ビアリール誘導体 |
CN101981013B (zh) | 2008-03-27 | 2013-05-29 | 詹森药业有限公司 | 作为parp和微管蛋白聚合抑制剂的四氢菲啶酮和四氢环戊二烯并喹啉酮 |
AU2009228945B2 (en) | 2008-03-27 | 2013-05-02 | Janssen Pharmaceutica Nv | Quinazolinone derivatives as tubulin polymerization inhibitors |
JP2011519926A (ja) * | 2008-05-05 | 2011-07-14 | ウィンスロップ−ユニバーシティー ホスピタル | Cox阻害薬の心血管系リスク因子の改善方法 |
EP2300013B1 (en) | 2008-05-21 | 2017-09-06 | Ariad Pharmaceuticals, Inc. | Phosphorous derivatives as kinase inhibitors |
CA2733533C (en) | 2008-08-25 | 2013-12-17 | Irm Llc | Hedgehog pathway modulators |
WO2010046780A2 (en) * | 2008-10-22 | 2010-04-29 | Institut Pasteur Korea | Anti viral compounds |
JP2012513409A (ja) * | 2008-12-23 | 2012-06-14 | アボット・ラボラトリーズ | 抗ウイルス化合物 |
CN102245604A (zh) | 2008-12-23 | 2011-11-16 | 雅培制药有限公司 | 抗病毒化合物 |
RU2541571C2 (ru) | 2009-04-15 | 2015-02-20 | Эббви Инк. | Противовирусные соединения |
CN102648208B (zh) * | 2009-11-12 | 2016-04-27 | R&D生技药品有限责任公司 | 微管蛋白抑制剂 |
EP2322537A1 (en) | 2009-11-12 | 2011-05-18 | R & D Biopharmaceuticals Gmbh | Tubulin inhibitors |
CN103608026B (zh) * | 2011-06-13 | 2016-08-24 | 伊利诺伊大学受托管理委员会 | 肽组合物和用于治疗肺损伤、哮喘、过敏反应、血管性水肿、全身性血管通透综合征和鼻塞的方法 |
WO2013121387A1 (en) * | 2012-02-17 | 2013-08-22 | University Of Cape Town | Anti -malarial agents |
CN102826985B (zh) * | 2012-09-18 | 2015-08-19 | 厦门大学 | 一种1-(3,4,5-三羟基)苯基-1-烷基酮的制备方法 |
JP2016506417A (ja) * | 2013-01-10 | 2016-03-03 | プルモキネ、インコーポレイテッド | キナーゼ阻害剤の治療指標 |
EP3007689B1 (en) | 2013-01-10 | 2018-03-07 | Pulmokine, Inc. | Non-selective kinase inhibitors |
JP6483714B2 (ja) | 2013-10-11 | 2019-03-13 | ローレンス エス. ジスマン, | 噴霧乾燥製剤 |
WO2016167795A1 (en) * | 2015-04-17 | 2016-10-20 | Southern Research Institute | Treatment of hepatitis b viral |
CN106167482A (zh) * | 2015-05-19 | 2016-11-30 | 重庆大学 | 一种抑制前列腺癌生长的化合物及其应用 |
WO2017181974A1 (zh) * | 2016-04-20 | 2017-10-26 | 苏州苏领生物医药有限公司 | 五元杂环类化合物及其制备方法、药物组合物和用途 |
CN107304203A (zh) * | 2016-04-20 | 2017-10-31 | 苏州苏领生物医药有限公司 | 五元杂环类化合物及其制备方法、药物组合物和用途 |
CN106565685B (zh) * | 2016-10-11 | 2019-03-01 | 深圳海王医药科技研究院有限公司 | 微管蛋白抑制剂 |
WO2018081567A1 (en) | 2016-10-27 | 2018-05-03 | Pulmokine, Inc. | Combination therapy for treating pulmonary hypertension |
EP3720436A4 (en) | 2017-12-06 | 2021-06-02 | Lin Bioscience, Pty Ltd. | TUBULIN INHIBITORS |
JP7184383B2 (ja) * | 2018-02-01 | 2022-12-06 | ザ・ユニバーシティ・オブ・シドニー | 抗癌性化合物 |
CN108658963A (zh) * | 2018-06-20 | 2018-10-16 | 桑文军 | 一种作用于微管蛋白的抗肿瘤药物 |
JP7555512B1 (ja) | 2024-06-18 | 2024-09-24 | 哲夫 村山 | 幌カバー付軽トラック |
Family Cites Families (37)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE82928C (es) | 1893-06-18 | 1895-10-01 | ||
FR352807A (fr) | 1905-03-28 | 1905-08-22 | Julius Schroeder | Perfectionnements apportés aux boites à fumée des chaudières à tubes bouilleurs et aux brosses de nettoyage |
GB253816A (en) | 1925-12-29 | 1926-06-24 | Spencer Bonecourt Ltd | Improvements relating to the cleaning of the fire-tubes of a boiler |
US3354490A (en) | 1964-06-15 | 1967-11-28 | Power Tube Inc | Boiler tube cleaning apparatus |
CH593266A5 (es) | 1973-09-20 | 1977-11-30 | Delalande Sa | |
US4367790A (en) | 1980-12-16 | 1983-01-11 | Draeger Walter A | Multiple tube cleaning apparatus |
JPS61228296A (ja) | 1985-03-30 | 1986-10-11 | Takao Sakamoto | 熱交換器における伝熱管の内面洗浄方法 |
GB9523675D0 (en) * | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
US6147080A (en) | 1996-12-18 | 2000-11-14 | Vertex Pharmaceuticals Incorporated | Inhibitors of p38 |
AT405973B (de) | 1998-06-26 | 2000-01-25 | Hackl Hubert | Reinigungsvorrichtung für wärmetauscherzüge |
DE19853278A1 (de) | 1998-11-19 | 2000-05-25 | Aventis Pharma Gmbh | Substituierte 4-Amino-2-aryl-cyclopenta[d]pyrimidine, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate |
JP2000180093A (ja) | 1998-12-15 | 2000-06-30 | Toshiba Plant Kensetsu Co Ltd | 熱交換器の管内清掃・探傷検査装置、及び管内清掃・探傷検査方法 |
WO2001017995A1 (en) | 1999-09-10 | 2001-03-15 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
IL154267A0 (en) * | 2000-08-08 | 2003-09-17 | Ortho Mcneil Pharm Inc | Neuroprotective 2-pyridinamine compositions and related methods |
CN100506801C (zh) * | 2000-09-06 | 2009-07-01 | 诺华疫苗和诊断公司 | 糖元合成酶激酶3的抑制剂 |
CN100355750C (zh) * | 2000-09-15 | 2007-12-19 | 沃泰克斯药物股份有限公司 | 可用作蛋白激酶抑制剂的吡唑化合物 |
US7129242B2 (en) * | 2000-12-06 | 2006-10-31 | Signal Pharmaceuticals, Llc | Anilinopyrimidine derivatives as JNK pathway inhibitors and compositions and methods related thereto |
WO2002047690A1 (en) * | 2000-12-12 | 2002-06-20 | Cytovia, Inc. | Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators of caspases and inducers of apoptosis and the use thereof |
CA2436487A1 (en) * | 2001-01-30 | 2002-08-08 | Cytopia Pty Ltd. | Methods of inhibiting kinases |
ES2292753T4 (es) * | 2001-03-29 | 2009-02-16 | Vertex Pharmaceuticals Incorporated | Inhibidores de quinasas n-terminales c-jun (jnk) y otras proteina quinasas. |
WO2003026661A1 (fr) * | 2001-09-14 | 2003-04-03 | Yamanouchi Pharmaceutical Co., Ltd. | Accelerateur de secretion de l'insuline et nouveau derive de pyrimidine |
EP1578722A4 (en) * | 2001-10-12 | 2006-09-06 | Irm Llc | KINASEINHIBITOR SCAFFOLD AND METHOD FOR THE PRODUCTION THEREOF |
DE60317198T2 (de) * | 2002-05-23 | 2008-12-04 | Cytopia Research Pty. Ltd., Richmond | Proteinkinaseinhibitoren |
AUPS251502A0 (en) * | 2002-05-23 | 2002-06-13 | Cytopia Pty Ltd | Protein kinase inhibitors |
AU2003232919B2 (en) * | 2002-05-23 | 2009-03-05 | Ym Biosciences Australia Pty Ltd | Protein kinase inhibitors |
WO2004000318A2 (en) * | 2002-06-21 | 2003-12-31 | Cellular Genomics, Inc. | Certain amino-substituted monocycles as kinase modulators |
CA2506772A1 (en) * | 2002-11-01 | 2004-05-21 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of jak and other protein kinases |
WO2004041810A1 (en) * | 2002-11-05 | 2004-05-21 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of jak and other protein kinases |
US20060089371A1 (en) * | 2002-11-11 | 2006-04-27 | Bayer Healthcare Ag | Phenyl or heteroaryl amino alkane derivatives as ip receptor antagonist |
AU2002953255A0 (en) * | 2002-12-11 | 2003-01-02 | Cytopia Research Pty Ltd | Protein kinase inhibitors |
GB2400101A (en) | 2003-03-28 | 2004-10-06 | Biofocus Discovery Ltd | Compounds capable of binding to the active site of protein kinases |
US20050014753A1 (en) * | 2003-04-04 | 2005-01-20 | Irm Llc | Novel compounds and compositions as protein kinase inhibitors |
EP1644365A2 (en) * | 2003-07-02 | 2006-04-12 | Biofocus Discovery Ltd | Pyrazine and pyridine derivatives as rho kinase inhibitors |
CA2533474A1 (en) * | 2003-07-30 | 2005-02-10 | Shudong Wang | 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors |
ES2528302T3 (es) | 2003-12-03 | 2015-02-06 | Ym Biosciences Australia Pty Ltd | Heterociclos con 6 anillos de nitrógeno fenilsustituidos como inhibidores de la polimerización de microtúbulos |
EP1904478B1 (en) | 2005-06-15 | 2013-07-24 | YM BioSciences Australia Pty Ltd | Acid addition salts of n-ethyl-n'-[2-methoxy-4-(5-methyl-4-{[(1s)-1-pyridin-3-ylbutyl]amino}pyrimidin- 2-yl)phenyl]urea and uses thereof |
JP5539734B2 (ja) | 2007-01-31 | 2014-07-02 | ワイエム・バイオサイエンシズ・オーストラリア・ピーティーワイ・リミテッド | チオピリミジンベースの化合物およびその使用 |
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