CN103702994B - 旋转酶和拓扑异构酶抑制剂的磷酸酯 - Google Patents
旋转酶和拓扑异构酶抑制剂的磷酸酯 Download PDFInfo
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- CN103702994B CN103702994B CN201280036458.1A CN201280036458A CN103702994B CN 103702994 B CN103702994 B CN 103702994B CN 201280036458 A CN201280036458 A CN 201280036458A CN 103702994 B CN103702994 B CN 103702994B
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Classifications
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- A—HUMAN NECESSITIES
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
- A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
- A61K31/685—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
- A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
- A61K31/688—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols both hydroxy compounds having nitrogen atoms, e.g. sphingomyelins
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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Abstract
Description
选择的化合物 | Ki(nM) |
化合物23 | 9 |
化合物X | <9 |
化合物Y | 13 |
化合物Z | <9 |
选择的化合物 | Ki(nM) |
化合物23 | 9 |
化合物X | 45 |
化合物Y | 24 |
化合物Z | 80 |
Claims (20)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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US201161499144P | 2011-06-20 | 2011-06-20 | |
US61/499,144 | 2011-06-20 | ||
PCT/US2012/043266 WO2012177707A1 (en) | 2011-06-20 | 2012-06-20 | Phosphate esters of gyrase and topoisomerase inhibitors |
Publications (2)
Publication Number | Publication Date |
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CN103702994A CN103702994A (zh) | 2014-04-02 |
CN103702994B true CN103702994B (zh) | 2016-03-23 |
Family
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CN201280036458.1A Active CN103702994B (zh) | 2011-06-20 | 2012-06-20 | 旋转酶和拓扑异构酶抑制剂的磷酸酯 |
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US (1) | US9125922B2 (zh) |
EP (1) | EP2721026B1 (zh) |
JP (1) | JP5977344B2 (zh) |
KR (1) | KR101941420B1 (zh) |
CN (1) | CN103702994B (zh) |
ES (1) | ES2576298T3 (zh) |
HK (1) | HK1194365A1 (zh) |
TW (1) | TWI554515B (zh) |
WO (1) | WO2012177707A1 (zh) |
Families Citing this family (17)
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RU2625305C2 (ru) | 2011-01-14 | 2017-07-13 | Сперо Тринем, Инк. | Твердые формы ингибитора гиразы (r)-1-этил-3-[6-фтор-5[2-(1-гидрокси-1-метил-этил) пиримидин-5-ил]-7-(тетрагидрофуран-2-ил)-1н-бензимидазол-2-ил] мочевины |
AU2012205415B2 (en) | 2011-01-14 | 2017-02-02 | Spero Therapeutics, Inc. | Pyrimidine gyrase and topoisomerase IV inhibitors |
KR101897950B1 (ko) * | 2011-01-14 | 2018-09-12 | 스페로 트리넴, 인코포레이티드 | 자이라제 억제제 (r)1에틸3[5[2{1하이드록시1메틸에틸}피리미딘5일]7(테트라하이드로푸란2일}1h벤즈이미다졸2일]우레아의 고체 형태 |
WO2012097274A1 (en) | 2011-01-14 | 2012-07-19 | Vertex Pharmaceuticals Incorporation | Process of making gyrase and topoisomerase iv inhibitors |
TWI554515B (zh) | 2011-06-20 | 2016-10-21 | 維泰克斯製藥公司 | 旋轉酶(gyrase)及拓樸異構酶抑制劑之磷酸酯 |
US9572809B2 (en) | 2012-07-18 | 2017-02-21 | Spero Trinem, Inc. | Combination therapy to treat Mycobacterium diseases |
US9018216B2 (en) | 2012-07-18 | 2015-04-28 | Vertex Pharmaceuticals Incorporated | Solid forms of (R)-2-(5-(2-(3-ethylureido)-6-fluoro-7-(tetrahydrofuran-2-yl)-1H-benzo[d]imidazol-5-yl)pyrimidin-2-yl)propan-2-yl dihydrogen phosphate and salts thereof |
CA2938459A1 (en) | 2014-02-03 | 2015-08-06 | Spero Gyrase, Inc. | Antibacterial compounds |
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BR112018069931A2 (pt) | 2016-04-01 | 2019-02-05 | Sanofi Sa | derivados de imidazol pentacíclicos fundidos como moduladores de atividade do tnf |
JP6968090B2 (ja) | 2016-04-01 | 2021-11-17 | ユーシービー バイオファルマ エスアールエル | Tnf活性のモジュレーターとしての縮合五環式イミダゾール誘導体 |
JP6968089B2 (ja) | 2016-04-01 | 2021-11-17 | ユーシービー バイオファルマ エスアールエル | Tnf活性のモジュレーターとしての縮合六環式イミダゾール誘導体 |
CN110461842A (zh) | 2017-03-15 | 2019-11-15 | Ucb生物制药私人有限公司 | 作为tnf活性调节剂的稠合五环咪唑衍生物 |
CN109725101B (zh) * | 2017-10-31 | 2021-11-19 | 正大天晴药业集团股份有限公司 | 盐酸特拉万星原料中有关物质的检测方法 |
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RU2625305C2 (ru) | 2011-01-14 | 2017-07-13 | Сперо Тринем, Инк. | Твердые формы ингибитора гиразы (r)-1-этил-3-[6-фтор-5[2-(1-гидрокси-1-метил-этил) пиримидин-5-ил]-7-(тетрагидрофуран-2-ил)-1н-бензимидазол-2-ил] мочевины |
WO2012097274A1 (en) | 2011-01-14 | 2012-07-19 | Vertex Pharmaceuticals Incorporation | Process of making gyrase and topoisomerase iv inhibitors |
AU2012205415B2 (en) | 2011-01-14 | 2017-02-02 | Spero Therapeutics, Inc. | Pyrimidine gyrase and topoisomerase IV inhibitors |
TWI554515B (zh) | 2011-06-20 | 2016-10-21 | 維泰克斯製藥公司 | 旋轉酶(gyrase)及拓樸異構酶抑制劑之磷酸酯 |
US9604976B2 (en) | 2012-03-22 | 2017-03-28 | Spero Gyrase, Inc. | Antibacterial compounds |
US9018216B2 (en) * | 2012-07-18 | 2015-04-28 | Vertex Pharmaceuticals Incorporated | Solid forms of (R)-2-(5-(2-(3-ethylureido)-6-fluoro-7-(tetrahydrofuran-2-yl)-1H-benzo[d]imidazol-5-yl)pyrimidin-2-yl)propan-2-yl dihydrogen phosphate and salts thereof |
US9572809B2 (en) * | 2012-07-18 | 2017-02-21 | Spero Trinem, Inc. | Combination therapy to treat Mycobacterium diseases |
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WO2006022773A1 (en) * | 2004-07-29 | 2006-03-02 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
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CN103702994A (zh) | 2014-04-02 |
WO2012177707A1 (en) | 2012-12-27 |
ES2576298T3 (es) | 2016-07-06 |
US9125922B2 (en) | 2015-09-08 |
TW201313732A (zh) | 2013-04-01 |
EP2721026B1 (en) | 2016-03-02 |
US20130157979A1 (en) | 2013-06-20 |
KR101941420B1 (ko) | 2019-01-23 |
HK1194365A1 (zh) | 2014-10-17 |
JP2014520152A (ja) | 2014-08-21 |
KR20140041768A (ko) | 2014-04-04 |
JP5977344B2 (ja) | 2016-08-24 |
TWI554515B (zh) | 2016-10-21 |
EP2721026A1 (en) | 2014-04-23 |
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