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公开(公告)号：US20090306014A1
公开(公告)日：2009-12-10
申请号：US12158174
申请日：2006-12-27
申请人： Carlo Ballatore , Angelo J. Castellino , Amos B. Smith, III , Joel Desharnais , Chengzao Sun , Simon E. Aspland
发明人： Carlo Ballatore , Angelo J. Castellino , Amos B. Smith, III , Joel Desharnais , Chengzao Sun , Simon E. Aspland
IPC分类号： A61K31/695 , C07F7/10 , A61P35/00
CPC分类号： C07D305/14 , C07D405/12 , C07D407/12 , C07D493/10
摘要： Provided herein are C-10 taxane carbamates and pharmaceutically acceptable derivatives thereof. In certain embodiments, provided herein are compounds, compositions and methods for treating cancer and taupathy.
摘要翻译： 本文提供C-10紫杉烷氨基甲酸酯及其药学上可接受的衍生物。 在某些实施方案中，本文提供了用于治疗癌症和甲状腺炎的化合物，组合物和方法。
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公开(公告)号：US08138361B2
公开(公告)日：2012-03-20
申请号：US12158174
申请日：2006-12-27
申请人： Carlo Ballatore , Angelo J Castellino , Amos B Smith, III , Joel Desharnais , Chengzao Sun , Simon E Aspland
发明人： Carlo Ballatore , Angelo J Castellino , Amos B Smith, III , Joel Desharnais , Chengzao Sun , Simon E Aspland
IPC分类号： C07D305/14 , A61K31/35
CPC分类号： C07D305/14 , C07D405/12 , C07D407/12 , C07D493/10
摘要： Provided herein are C-10 taxane carbamates and pharmaceutically acceptable derivatives thereof. In certain embodiments, provided herein are compounds, compositions and methods for treating cancer and taupathy.
摘要翻译： 本文提供C-10紫杉烷氨基甲酸酯及其药学上可接受的衍生物。 在某些实施方案中，本文提供了用于治疗癌症和甲状腺炎的化合物，组合物和方法。
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公开(公告)号：US20050187147A1
公开(公告)日：2005-08-25
申请号：US10948707
申请日：2004-09-22
申请人： Michael Newman , Angelo Castellino , Joel Desharnais , Zijian Guo , Qing Li , Carlo Ballatore , Chengzao Sun
发明人： Michael Newman , Angelo Castellino , Joel Desharnais , Zijian Guo , Qing Li , Carlo Ballatore , Chengzao Sun
IPC分类号： A61K31/337 , A61K31/475 , A61K31/704 , A61K38/00 , A61K47/48 , A61K49/04 , A61P29/00 , A61P35/00 , C07K7/06 , C07K7/08 , A61K38/14 , A61K38/08
CPC分类号： C07K7/08 , A61K31/337 , A61K31/475 , A61K31/704 , A61K38/00 , A61K47/54 , A61K47/64 , A61K47/65 , C07K7/06
摘要： In one embodiment, provided herein are compositions and methods for increasing drug efficiency. In certain embodiments, the compositions contain conjugates having the formula: D-L-S wherein D is a drug moiety; L, which may or may not be present, is a non-releasing linker moiety; and S is a substrate for a protein or lipid kinase that is overexpressed, overactive or exhibits undesired activity in a target system.
摘要翻译： 在一个实施方案中，本文提供了用于提高药物效率的组合物和方法。 在某些实施方案中，组合物包含具有下式的共轭物：<？in-line-formula description =“In-line Formulas”end =“lead”？> DLS <？in-line-formula description =“In-line Formulas” end =“tail”？>其中D是药物部分; 可能存在或不存在的L是非释放连接体部分; 并且S是蛋白质或脂质激酶的底物，其在靶系统中过表达，过度活化或表现出不期望的活性。
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公开(公告)号：US20060234909A1
公开(公告)日：2006-10-19
申请号：US11376695
申请日：2006-03-14
申请人： Michael Newman , Angelo Castellino , Joel Desharnais , Zijian Guo , Qing Li , Carlo Ballatore , Chengzao Sun
发明人： Michael Newman , Angelo Castellino , Joel Desharnais , Zijian Guo , Qing Li , Carlo Ballatore , Chengzao Sun
CPC分类号： C07K7/08 , A61K31/337 , A61K31/475 , A61K31/704 , A61K38/00 , A61K47/54 , A61K47/64 , A61K47/65 , C07K7/06
摘要： In one embodiment, provided herein are compositions and methods for increasing drug efficiency. In certain embodiments, the compositions contain conjugates having the formula: D-L-S wherein D is a drug moiety; L, which may or may not be present, is a non-releasing linker moiety; and S is a substrate for a protein or lipid kinase that is overexpressed, overactive or exhibits undesired activity in a target system.
摘要翻译： 在一个实施方案中，本文提供了用于提高药物效率的组合物和方法。 在某些实施方案中，组合物包含具有下式的共轭物：<？in-line-formula description =“In-line Formulas”end =“lead”？> DLS <？in-line-formula description =“In-line Formulas” end =“tail”？>其中D是药物部分; 可能存在或不存在的L是非释放连接体部分; 并且S是蛋白质或脂质激酶的底物，其在靶系统中过表达，过度活化或表现出不期望的活性。
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5.发明申请Small molecule compositions and methods for increasing drug efficiency using compositions thereof 审中-公开小分子组合物和使用其组合物提高药物效率的方法公开(公告)号：US20050148534A1
公开(公告)日：2005-07-07
申请号：US10948364
申请日：2004-09-22
申请人： Angelo Castellino , Carlo Ballatore , Simon Aspland , Joel Desharnais , Michael Newman , Chengzao Sun , Peter Wirsching
发明人： Angelo Castellino , Carlo Ballatore , Simon Aspland , Joel Desharnais , Michael Newman , Chengzao Sun , Peter Wirsching
IPC分类号： A61K31/513 , A61K31/522 , A61K31/7072 , A61K31/7076 , A61K47/48 , A61K48/00
CPC分类号： A61K31/7076 , A61K31/513 , A61K31/522 , A61K31/7072 , A61K47/55
摘要： In certain embodiments, provided herein are compositions and methods for increasing drug efficiency. The conjugates provided are in certain embodiments, for compositions and methods in treatment of variety of diseases and have the formula 1: D-L-S (1) or formula 2: D-L-S′ (2) wherein D is a drug moiety; L, which may or may not be present, is a non-releasing linker moiety; S is a substrate for a kinase, other than a hexokinase, a protein kinase or a lipid kinase; and S′ is a substrate for a phosphotransferase, other than a hexokinase, a protein kinase or a lipid kinase.
摘要翻译： 在某些实施方案中，本文提供了用于提高药物效率的组合物和方法。 在某些实施方案中，提供的缀合物用于治疗各种疾病的组合物和方法，并具有式1：<？in-line-formula description =“In-line Formulas”end =“lead”？> DLS（1） 或“公式2”：<？in-line-formula description =“In-line formula”end =“lead”？> DLS' （2）<？in-line-formula description =“In-line Formulas”end =“tail”？>其中D是药物部分; 可能存在或不存在的L是非释放连接体部分; S是除己糖激酶，蛋白激酶或脂质激酶以外的激酶的底物; 和S'是除己糖激酶，蛋白激酶或脂质激酶之外的磷酸转移酶的底物。
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公开(公告)号：US20130029983A1
公开(公告)日：2013-01-31
申请号：US13497697
申请日：2010-09-22
申请人： Carlo Ballatore , Kurt R. Brunden , Alexander L. Crowe , Donna M. Huryn , Virginia M.Y. Lee , John Q. Trojanowski , Amos B. Smith, III , Ruili Huang , Wenwei Huang , Ronald L. Johnson , Francesco Piscitelli
发明人： Carlo Ballatore , Kurt R. Brunden , Alexander L. Crowe , Donna M. Huryn , Virginia M.Y. Lee , John Q. Trojanowski , Amos B. Smith, III , Ruili Huang , Wenwei Huang , Ronald L. Johnson , Francesco Piscitelli
IPC分类号： A61K31/5025 , C07D495/04 , A61K31/5377 , A61P25/28 , A61P25/16
CPC分类号： C07D495/04 , A61K31/5025 , A61K31/5377
摘要： The present invention is directed to methods of inhibiting a tauopathy in a patient by administration of a compound of formula I: Novel aminothienopyridazine compounds are also described.
摘要翻译： 本发明涉及通过给药式I化合物来抑制患者的tau蛋白病变的方法：还描述了新的氨基噻吩并哒嗪化合物。
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公开(公告)号：US08530520B2
公开(公告)日：2013-09-10
申请号：US13489745
申请日：2012-06-06
申请人： Onur Atasoylu , Carlo Ballatore , Kurt R. Brunden , Longchuan Huang , Donna M. Huryn , Michael James , Virginia M. Y. Lee , Francesco Piscitelli , Amos B. Smith, III , James Soper , John Q. Trojanowski
发明人： Onur Atasoylu , Carlo Ballatore , Kurt R. Brunden , Longchuan Huang , Donna M. Huryn , Michael James , Virginia M. Y. Lee , Francesco Piscitelli , Amos B. Smith, III , James Soper , John Q. Trojanowski
IPC分类号： A61K31/18
CPC分类号： C07C311/17 , A61K31/18 , C07C2601/02 , C07C2601/04 , C07C2601/10 , C07C2601/14 , C07D257/04
摘要： The present invention is directed to carboxylic acid-containing pharmaceutical compounds where the carboxylic acid moieties have been substituted with cycloalkyl-dione derivatives, as well as tautomers and pharmaceutically acceptable salt forms thereof. These bioisosteric replacements improve the compound's ability to effectively cross the blood brain barrier and result in improved pharmacokinetic, toxicological, and/or safety profiles.
摘要翻译： 本发明涉及羧酸部分已被环烷基二酮衍生物取代的含羧酸的药物化合物，以及其互变异构体及其药学上可接受的盐形式。 这些生物电泳替代物可以改善化合物有效跨越血脑屏障的能力，并改善药代动力学，毒理学和/或安全性。
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公开(公告)号：US20120329877A1
公开(公告)日：2012-12-27
申请号：US13489745
申请日：2012-06-06
申请人： Onur Atasoylu , Carlo Ballatore , Kurt R. Brunden , Longchun Huang , Donna M. Huryn , Michael James , Virginia M.Y. Lee , Francesco Piscitelli , Amos B. Smith, III , James Soper , John Q. Trojanowski
发明人： Onur Atasoylu , Carlo Ballatore , Kurt R. Brunden , Longchun Huang , Donna M. Huryn , Michael James , Virginia M.Y. Lee , Francesco Piscitelli , Amos B. Smith, III , James Soper , John Q. Trojanowski
CPC分类号： C07C311/17 , A61K31/18 , C07C2601/02 , C07C2601/04 , C07C2601/10 , C07C2601/14 , C07D257/04
摘要： The present invention is directed to compounds of formula I: wherein A is n is 0, 1, or 2; m is 0 or 1; R1 is H or C1-6alkyl and R2 is H, C1-6 alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; and X is O or N; as well as tautomers and pharmaceutically acceptable salt forms thereof. Uses of these compounds are also described.
摘要翻译： 本发明涉及式I化合物：其中A是n是0,1或2; m为0或1; R 1是H或C 1-6烷基，R 2是H，C 1-6烷基，取代或未取代的芳基或取代或未取代的杂芳基; X为O或N; 以及互变异构体及其药学上可接受的盐形式。 还描述了这些化合物的用途。
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公开(公告)号：US20060063743A1
公开(公告)日：2006-03-23
申请号：US11256061
申请日：2005-10-21
CPC分类号： C07F9/4084 , A61K47/65 , C07F9/4006
摘要： This invention provides compounds and methods for using them to inhibit the growth of microorganism that expresses Peptide Deformylase, the compounds having the general formula:
摘要翻译： 本发明提供了使用它们抑制表达肽变形酶的微生物生长的化合物和方法，该化合物具有以下通式：
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公开(公告)号：US07001922B2
公开(公告)日：2006-02-21
申请号：US10714255
申请日：2003-11-14
IPC分类号： A61K31/192 , A61K31/195 , C07F9/02 , C07F9/535
CPC分类号： C07F9/4084 , A61K47/65 , C07F9/4006
摘要： The invention provides compounds and methods for using them to inhibit the growth of microorganism that expresses Peptide Deformylase, the compounds having the general formula:
摘要翻译： 本发明提供了使用它们抑制表达肽脱甲酰酶的微生物生长的化合物和方法，该化合物具有以下通式：化学式=“CHEM-US-00001”num =“000
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