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![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](/abs-image/US/2015/04/28/US09018216B2/abs.jpg.150x150.jpg)
1.发明授权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 有权（R）-2-（5-（2-（3-乙基脲基）-6-氟-7-（四氢呋喃-2-基）-1H-苯并[d]咪唑-5-基）嘧啶-2 - 基）丙-2-基磷酸二氢盐及其盐公开(公告)号：US09018216B2
公开(公告)日：2015-04-28
申请号：US13945257
申请日：2013-07-18
申请人： Hardwin O'Dowd , Dainius MacIkenas , Bin Song
发明人： Hardwin O'Dowd , Dainius MacIkenas , Bin Song
IPC分类号： A01N43/54 , C07D239/42 , C07D471/04 , C07F9/6558 , C07D405/14 , A61K31/506 , C07D239/26
CPC分类号： C07F9/65586 , A61K31/506 , C07D239/26 , C07D405/14
摘要： The invention relates to solid forms of the Formula (I) wherein X is —PO(OH)2, —PO(OH)O−M+, or —PO(O−)2.2M+, wherein M is a monovalent cation such as Na+, K+, Li+, or NH4+. The invention also provides pharmaceutically acceptable compositions comprising the solid form of the compound and method of using the compositions in the treatment of various disorders.
摘要翻译： 本发明涉及式（I）的固体形式，其中X为-PO（OH）2，-PO（OH）O-M +或-PO（O-）2.2M +，其中M为单价阳离子如Na + ，K +，Li +或NH4 +。 本发明还提供包含固体形式的化合物的药学上可接受的组合物和使用该组合物治疗各种疾病的方法。
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公开(公告)号：US07361743B2
公开(公告)日：2008-04-22
申请号：US11217836
申请日：2005-08-31
IPC分类号： C07H15/16
CPC分类号： C07H15/16
摘要： Novel lincomycin derivatives are disclosed. These lincomycin derivatives exhibit antibacterial activity. The compounds of the subject invention may exhibit potent activities against bacteria, including Gram positive organisms, and may be useful antimicrobial agents. Methods of synthesis and of use of the compounds are also disclosed.
摘要翻译： 公开了新的林可霉素衍生物。 这些林可霉素衍生物具有抗菌活性。 本发明的化合物可以表现出对细菌的有效活性，包括革兰氏阳性生物，并且可以是有用的抗微生物剂。 还公开了化合物的合成和使用方法。
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![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](/abs-image/US/2014/01/30/US20140031318A1/abs.jpg.150x150.jpg)
3.发明申请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 有权（R）-2-（5-（2-（3-乙酰基氧基）-6-氟-7-（四氢呋喃-2-基）-1H-苯并[d]咪唑烷-5-YL）的固体形式吡咯烷-2 -YL）丙-2-炔基二氢磷酸酯及其盐公开(公告)号：US20140031318A1
公开(公告)日：2014-01-30
申请号：US13945257
申请日：2013-07-18
申请人： Hardwin O'DOWD , DAINIUS MACIKENAS , Bin SONG
发明人： Hardwin O'DOWD , DAINIUS MACIKENAS , Bin SONG
IPC分类号： C07F9/6558
CPC分类号： C07F9/65586 , A61K31/506 , C07D239/26 , C07D405/14
摘要： The invention relates to solid forms of the Formula (I) wherein X is —PO(OH)2, —PO(OH)O−M+, or —PO(O−)2.2M+, wherein M is a monovalent cation such as Na+, K+, Li+, or NH4+. The invention also provides pharmaceutically acceptable compositions comprising the solid form of the compound and method of using the compositions in the treatment of various disorders.
摘要翻译： 本发明涉及式（I）的固体形式，其中X为-PO（OH）2，-PO（OH）O-M +或-PO（O-）2.2M +，其中M为单价阳离子如Na + ，K +，Li +或NH4 +。 本发明还提供包含固体形式的化合物的药学上可接受的组合物和使用该组合物治疗各种疾病的方法。
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公开(公告)号：US08466288B2
公开(公告)日：2013-06-18
申请号：US13349868
申请日：2012-01-13
申请人： Alex Aronov , Jon H. Come , Robert J. Davies , Albert Charles Pierce , Philip N. Collier , Ronald Lee Grey, Jr. , Hardwin O'Dowd , James A. Henderson , Elaine B. Krueger , Arnaud Le Tiran , Yusheng Liao , David Messersmith , Jian Wang , Suganthini S. Nanthakumar , Jingrong Cao , Upul Keerthi Bandarage , Anne-Laure Grillot
发明人： Alex Aronov , Jon H. Come , Robert J. Davies , Albert Charles Pierce , Philip N. Collier , Ronald Lee Grey, Jr. , Hardwin O'Dowd , James A. Henderson , Elaine B. Krueger , Arnaud Le Tiran , Yusheng Liao , David Messersmith , Jian Wang , Suganthini S. Nanthakumar , Jingrong Cao , Upul Keerthi Bandarage , Anne-Laure Grillot
IPC分类号： C07D471/02 , C07D213/04 , C07D401/00 , C07D401/02 , C12N9/99 , A61K31/437
CPC分类号： C07D409/14 , C07D401/04 , C07D401/14 , C07D405/14 , C07D417/14 , C07D471/04 , C07D471/20 , C07D491/20
摘要： The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3Kγ. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
摘要翻译： 本发明涉及可用作PI3K抑制剂，特别是PI3Kgamma的化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。
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公开(公告)号：US07199106B2
公开(公告)日：2007-04-03
申请号：US10871618
申请日：2004-06-17
CPC分类号： C07D405/12
摘要： Novel lincomycin derivatives are disclosed. These lincomycin derivatives exhibit antibacterial activity. The compounds of the subject invention may exhibit potent activities against bacteria, including gram positive organisms, and may be useful antimicrobial agents. Methods of synthesis and of use of the compounds are also disclosed.
摘要翻译： 公开了新的林可霉素衍生物。 这些林可霉素衍生物具有抗菌活性。 本发明的化合物可以表现出对细菌的有效活性，包括革兰氏阳性生物，并且可以是有用的抗微生物剂。 还公开了化合物的合成和使用方法。
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公开(公告)号：US20140045791A1
公开(公告)日：2014-02-13
申请号：US13942342
申请日：2013-07-15
申请人： Christopher Phillip Locher , Youssef Laafiret Bennani , Ann-Laure Grillot , Hardwin O'Dowd , Emanuele Perola , Arnaud Le Tiran
发明人： Christopher Phillip Locher , Youssef Laafiret Bennani , Ann-Laure Grillot , Hardwin O'Dowd , Emanuele Perola , Arnaud Le Tiran
IPC分类号： A61K31/506 , A61K31/47 , A61K31/498 , A61K31/496 , A61K31/4709 , A61K31/5377 , A61K31/675 , A61K31/4965
CPC分类号： A61K31/675 , A61K31/132 , A61K31/34 , A61K31/4164 , A61K31/4168 , A61K31/421 , A61K31/454 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/4965 , A61K31/498 , A61K31/506 , A61K31/5377 , A61K45/06 , A61K2300/00
摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein X and R are as defined herein. The compounds of formula (I) are useful as gyrase and/or topoisomerase IV inhibitors for treating bacterial infections. The compounds of formula (I) either possess a broad range of anti-bacterial activity and advantageous toxicological properties or are prodrugs of compounds having said activity.
摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，其中X和R如本文所定义。 式（I）的化合物可用作用于治疗细菌感染的旋转酶和/或拓扑异构酶IV抑制剂。 式（I）化合物具有广泛的抗菌活性和有利的毒理特性，或具有所述活性的化合物的前药。
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公开(公告)号：US20130090326A1
公开(公告)日：2013-04-11
申请号：US13501834
申请日：2010-10-15
申请人： Erin M. Duffy , Ashoke Bhattacharjee , Hardwin O'Dowd , Marco DeVivo , Yanming Du , Sandra Sinishtaj , Yuanqing Tang , Brian T. Wimberly
发明人： Erin M. Duffy , Ashoke Bhattacharjee , Hardwin O'Dowd , Marco DeVivo , Yanming Du , Sandra Sinishtaj , Yuanqing Tang , Brian T. Wimberly
IPC分类号： C07D471/10 , C07D403/04 , C07D251/16 , C07D413/14 , C07D239/22 , C07D403/12
CPC分类号： C07D239/47 , A61K31/505 , A61K31/506 , A61L31/16 , A61L2300/404 , C07D239/10 , C07D239/22 , C07D239/36 , C07D251/16 , C07D251/42 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/10 , C07D487/04 , C07D491/048 , C07D519/00
摘要： The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals.
摘要翻译： 本发明一般涉及抗微生物化合物领域及其制备和使用方法。 这些化合物可用于治疗，预防和降低人类和动物中微生物感染的风险。
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公开(公告)号：US20120202784A1
公开(公告)日：2012-08-09
申请号：US13349868
申请日：2012-01-13
申请人： Alex Aronov , Jon H. Come , Robert J. Davies , Albert Charles Pierce , Philip N. Collier , Ronald Lee Grey, JR. , Hardwin O'Dowd , James A. Henderson , Elaine B. Krueger , Arnaud Le Tiran , Yusheng Liao , David Messersmith , Jian Wang , Suganthini S. Nanthakumar , Jingrong Cao , Upul Keerthi Bandarage , Anne-Laure Grillot
发明人： Alex Aronov , Jon H. Come , Robert J. Davies , Albert Charles Pierce , Philip N. Collier , Ronald Lee Grey, JR. , Hardwin O'Dowd , James A. Henderson , Elaine B. Krueger , Arnaud Le Tiran , Yusheng Liao , David Messersmith , Jian Wang , Suganthini S. Nanthakumar , Jingrong Cao , Upul Keerthi Bandarage , Anne-Laure Grillot
IPC分类号： A61K31/437 , A61K31/5377 , C12N9/99 , A61K31/496 , A61K31/551 , C07D471/20 , C07D471/04 , C07D491/20
CPC分类号： C07D409/14 , C07D401/04 , C07D401/14 , C07D405/14 , C07D417/14 , C07D471/04 , C07D471/20 , C07D491/20
摘要： The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3Kγ. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
摘要翻译： 本发明涉及可用作PI3K抑制剂，特别是PI3Kγ的化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。
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公开(公告)号：US20120184512A1
公开(公告)日：2012-07-19
申请号：US13349789
申请日：2012-01-13
申请人： Arnaud Le Tiran , Anne-Laure Grillot , Paul S. Charifson , Yousef Laafiret Bennani , Hardwin O'Dowd , Emanuele Perola
发明人： Arnaud Le Tiran , Anne-Laure Grillot , Paul S. Charifson , Yousef Laafiret Bennani , Hardwin O'Dowd , Emanuele Perola
IPC分类号： A61K31/506 , C07F9/09 , A61P31/04 , A01N43/54 , A01N57/16 , A01P1/00 , C07D405/14 , A61K31/675
CPC分类号： C07D405/14 , C07F9/65586
摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein X and R are as defined herein. The compounds of formula (I) are useful as gyrase and/or topoisomerase IV inhibitors for treating bacterial infections. The compounds of formula (I) either possess a broad range of anti-bacterial activity and advantageous toxicological properties or are prodrugs of compounds having said activity.
摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，其中X和R如本文所定义。 式（I）的化合物可用作用于治疗细菌感染的旋转酶和/或拓扑异构酶IV抑制剂。 式（I）化合物具有广泛的抗菌活性和有利的毒理特性，或具有所述活性的化合物的前药。
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公开(公告)号：US07691843B2
公开(公告)日：2010-04-06
申请号：US10617616
申请日：2003-07-11
申请人： Bore G. Raju , Hardwin O'Dowd , Hongwu Gao , Dinesh V. Patel , Jaoquim Trias
发明人： Bore G. Raju , Hardwin O'Dowd , Hongwu Gao , Dinesh V. Patel , Jaoquim Trias
IPC分类号： A61K31/397 , C07D205/00
CPC分类号： C07D405/06 , C07D205/04 , C07D207/16 , C07D207/22
摘要： Novel N-hydroxyamide derivatives are disclosed. These N-hydroxyamide derivatives inhibit UPD-3-O—(R-3-hydroxymyristoyl)-N-acetylglucosamine deacetylase, an enzyme present in gram negative bacteria and are therefore useful as antimicrobials and antibiotics. Methods of synthesis and of use of the compounds are also disclosed.
摘要翻译： 公开了新的N-羟基酰胺衍生物。 这些N-羟基酰胺衍生物抑制存在于革兰氏阴性细菌中的酶的UPD-3-O-（R-3-羟基肉豆蔻酰）-N-乙酰葡糖胺脱乙酰酶，因此可用作抗微生物剂和抗生素。 还公开了化合物的合成和使用方法。
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