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1. 发明公开

US20230322675A1 COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH LPA RECEPTOR ACTIVITY 审中-公开
公开(公告)号：US20230322675A1
公开(公告)日：2023-10-12
申请号：US18322492
申请日：2023-05-23
申请人： Lhotse Bio, Inc.
发明人： Wei Huang , Hui Lei , Zhongmiao Xu , Haizhen Zhang , Qiong Zhang
IPC分类号： C07D211/66 , C07C229/18 , C07C229/28 , C07D309/14 , C07D317/54 , C07D317/58 , C07C61/39 , C07D407/12
CPC分类号： C07D211/66 , C07C229/18 , C07C229/28 , C07D309/14 , C07D317/54 , C07D317/58 , C07C61/39 , C07D407/12 , C07C2602/08 , C07C2601/02 , C07C2601/04 , C07C2601/08
摘要： The present disclosure provides LPA antagonists, as well as pharmaceutical compositions comprising the compounds disclosed herein. Also provided are methods for treating LPA-associated diseases, disorders, and conditions.

2. 发明授权

US09846168B2 Fluorescent metal ion indicators with large stokes shifts 有权
公开(公告)号：US09846168B2
公开(公告)日：2017-12-19
申请号：US15152346
申请日：2016-05-11
申请人： LIFE TECHNOLOGIES CORPORATION
发明人： Kyle Gee , Vladimir Martin
IPC分类号： G01N21/76 , G01N33/84 , C07C229/18 , C07D221/14 , C07D265/38 , C07D311/82 , C09B5/60 , C09B5/62 , C09B11/06 , C09K11/06 , C07D209/14 , C07D311/90 , G01N33/20 , C07C311/44 , C07K14/195 , C07K14/435 , C09B11/08 , C09B19/00 , C09B57/08 , C07D413/04
CPC分类号： G01N33/84 , C07C229/18 , C07C311/44 , C07D209/14 , C07D221/14 , C07D265/38 , C07D311/82 , C07D311/90 , C07D413/04 , C07K14/195 , C07K14/43595 , C09B5/60 , C09B5/62 , C09B11/06 , C09B11/08 , C09B19/00 , C09B19/005 , C09B57/08 , C09K11/06 , C09K2211/1014 , G01N33/20 , G01N2458/00
摘要： The present invention provides fluorogenic compounds for the detection of target metal ions wherein the compounds exhibit a Stokes shift greater than 50 nm and the detectable signal is modulated by photoinduced electron transfer (PET). The present compounds consist of three functional elements, the ion sensing moiety (chelating moiety), the reporter moiety (fluorophore or fluorescent protein) and spacer or linker between the sensing and reporter moieties of the present compound that allows for PET upon binding of a metal ion and excitation by an appropriate wavelength.

4. 发明申请

US20160305964A1 Fluorescent Metal Ion Indicators with Large Stokes Shifts 有权
标题翻译：荧光金属离子指示器，具有大的斯托克斯位移
公开(公告)号：US20160305964A1
公开(公告)日：2016-10-20
申请号：US15152346
申请日：2016-05-11
申请人： LIFE TECHNOLOGIES CORPORATION
发明人： Kyle GEE , Vladimir MARTIN
IPC分类号： G01N33/84 , C07C311/44 , C09B11/08 , G01N33/20 , C09B19/00 , C07K14/435 , C07K14/195 , C07C229/18 , C09B57/08
CPC分类号： G01N33/84 , C07C229/18 , C07C311/44 , C07D209/14 , C07D221/14 , C07D265/38 , C07D311/82 , C07D311/90 , C07D413/04 , C07K14/195 , C07K14/43595 , C09B5/60 , C09B5/62 , C09B11/06 , C09B11/08 , C09B19/00 , C09B19/005 , C09B57/08 , C09K11/06 , C09K2211/1014 , G01N33/20 , G01N2458/00
摘要： The present invention provides fluorogenic compounds for the detection of target metal ions wherein the compounds exhibit a Stokes shift greater than 50 nm and the detectable signal is modulated by photoinduced electron transfer (PET). The present compounds consist of three functional elements, the ion sensing moiety (chelating moiety), the reporter moiety (fluorophore or fluorescent protein) and spacer or linker between the sensing and reporter moieties of the present compound that allows for PET upon binding of a metal ion and excitation by an appropriate wavelength.
摘要翻译：本发明提供用于检测靶金属离子的荧光化合物，其中化合物表现出大于50nm的斯托克斯位移，并且可检测信号通过光诱导电子转移（PET）调节。本发明化合物由三种功能元件组成，即离子感测部分（螯合部分），报道部分（荧光团或荧光蛋白）以及本发明化合物的感测和报道部分之间的间隔物或接头，其允许在结合金属时的PET 通过适当的波长离子和激发。

5. 发明授权

US09334281B2 Fluorochromes for organelle tracing and multi-color imaging 有权
标题翻译：荧光色素用于细胞器追踪和多色成像
公开(公告)号：US09334281B2
公开(公告)日：2016-05-10
申请号：US12231988
申请日：2008-09-08
申请人： Wayne Forrest Patton , Praveen Pande , Yuejun Xiang , Zaiguo Li , James J. Donegan , Elazar Rabbani
发明人： Wayne Forrest Patton , Praveen Pande , Yuejun Xiang , Zaiguo Li , James J. Donegan , Elazar Rabbani
IPC分类号： C07C211/61 , C07D487/06 , C07C225/34 , C07C225/36 , C07C229/18 , C07C335/20 , C07D213/74 , C07D295/135 , C07F9/53 , C07F9/6503 , C09B1/00 , C09B1/51 , C09B1/515 , C40B40/04 , G01N33/50
CPC分类号： C07D487/06 , C07C225/34 , C07C225/36 , C07C229/18 , C07C335/20 , C07C2603/24 , C07D213/74 , C07D295/135 , C07F9/5304 , C07F9/65038 , C09B1/005 , C09B1/51 , C09B1/512 , C09B1/5155 , C40B40/04 , G01N33/5005 , G01N33/5011
摘要： Provided are compounds, methods and kits for identifying in cells of interest organelles including nuclei and a wide variety of organelles other than nuclei (non-nuclear organelles), as well as cell regions or cell domains. These compounds and methods can be used with other conventional detection reagents for identifying the location or position or quantity of organelles and even for distinguishing between organelles in cells of interest.
摘要翻译：提供了用于在感兴趣细胞中鉴定细胞器的化合物，方法和试剂盒，包括细胞核和除核以外的多种细胞器（非核细胞器）以及细胞区域或细胞结构域。这些化合物和方法可以与其它常规检测试剂一起使用，用于鉴定细胞器的位置或位置，甚至用于鉴别感兴趣的细胞中的细胞器。

6. 发明授权

US09174924B2 Hydrolysable linkers and cross-linkers for absorbable polymers 有权
公开(公告)号：US09174924B2
公开(公告)日：2015-11-03
申请号：US14724779
申请日：2015-05-28
申请人： Bezwada Biomedical, LLC
发明人： Rao S Bezwada
IPC分类号： C07C69/74 , C07C69/708 , A61L31/10 , A61L17/14 , A61L27/18 , A61L17/00 , A61L24/06 , C08G63/16 , C08G63/91
CPC分类号： C07C265/12 , A47F5/0006 , A61L17/00 , A61L17/105 , A61L17/12 , A61L17/145 , A61L24/06 , A61L27/18 , A61L27/34 , A61L27/52 , A61L27/58 , A61L31/10 , A61L31/145 , A61L31/148 , B65D25/22 , C07C69/34 , C07C69/67 , C07C69/708 , C07C205/37 , C07C205/43 , C07C205/57 , C07C217/84 , C07C219/34 , C07C225/22 , C07C229/18 , C07C229/60 , C07C235/16 , C08G63/16 , C08G63/916 , Y02W90/13 , Y10T24/44291 , Y10T24/51 , Y10T428/139 , Y10T442/10 , C08L67/04
摘要： The present invention relates to the discovery of new class of linear and multiarmed hydrolysable linkers and cross linkers for use in the synthesis of biodegradable polymers such as, polyesters, polyurethanes, polyamides, polyureas and degradable epoxy amine resin. The linear and multiarmed hydrolysable linkers of the present invention include symmetrical and/or unsymmetrical ether carboxylic acids, amines, amide diols, amine polyols and isocyanates.

7. 发明授权

US08946224B2 Substituted [1,2,4]triazolo[4,3-A]pyrazines for medicaments and pharmaceutical compositions 有权
标题翻译：用于药物和药物组合物的取代的[1,2,4]三唑并[4,3-A]吡嗪
公开(公告)号：US08946224B2
公开(公告)日：2015-02-03
申请号：US13883713
申请日：2011-11-11
申请人： Mark Craighead , Ronald Palin , Neil Murray , Derek Lindsay
发明人： Mark Craighead , Ronald Palin , Neil Murray , Derek Lindsay
IPC分类号： A61K31/4985 , C07D487/04 , C07D498/06 , C07D413/12 , C07C63/64 , C07D213/60 , C07C217/58 , C07D403/06 , C07C69/12 , C07C235/16 , C07D257/04 , C07D313/04 , C07D407/06 , C07C43/205 , C07C215/46 , C07C255/25 , C07D205/08 , C07D281/06 , C07D417/06 , C07D413/04 , C07D401/04 , C07C63/66 , C07D499/88 , C07D401/12 , C07D519/00 , C07D209/18 , C07D307/00 , C07D501/00 , C07C233/22 , C07D473/00 , C07H19/052 , C07C251/40 , C07D403/12 , C07D513/06 , C07C251/54 , C07C257/14 , C07C251/48 , C07C57/00 , C07C233/36 , C07H19/173 , C07D411/10 , C07C229/18 , C07D295/02 , C07H19/06 , C07C235/28 , C07D233/54 , C07J5/00 , C07D471/04 , C07D241/04 , C07D235/16 , C07D277/40 , C07D417/12 , C07D309/32 , C07C237/20 , C07C251/58 , C07D401/14 , C07D491/04
CPC分类号： C07D487/04 , C07C43/205 , C07C57/00 , C07C63/64 , C07C63/66 , C07C69/12 , C07C215/46 , C07C217/58 , C07C229/18 , C07C233/22 , C07C233/36 , C07C235/16 , C07C235/28 , C07C237/20 , C07C251/40 , C07C251/48 , C07C251/54 , C07C251/58 , C07C255/25 , C07C257/14 , C07C2601/16 , C07C2602/10 , C07C2603/74 , C07D205/08 , C07D209/18 , C07D213/60 , C07D233/54 , C07D235/16 , C07D241/04 , C07D257/04 , C07D277/40 , C07D281/06 , C07D295/02 , C07D307/00 , C07D309/32 , C07D313/04 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D407/06 , C07D411/10 , C07D413/04 , C07D413/12 , C07D417/06 , C07D417/12 , C07D471/04 , C07D473/00 , C07D491/04 , C07D498/06 , C07D499/88 , C07D501/00 , C07D513/06 , C07D519/00 , C07H19/052 , C07H19/06 , C07H19/173 , C07J5/00 , C07J71/0031
摘要： The present invention relates to derivatives of known active pharmaceutical compounds. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more reactions which may be considered to represent a change of oxidation state. We refer to these compounds generally as redox derivatives. The derivatives of the invention may be related to the original parent active pharmaceutical compound by only a single step transformation, or may be related via several synthetic steps including one or more changes of oxidation state. Exemplary derivatives have the formula
摘要翻译：本发明涉及已知的活性药物化合物的衍生物。由于活性化合物的氧化还原衍生物，这些衍生物与母体活性化合物不同。这意味着活性化合物中的一个或多个官能团已经在一个或多个反应中被转化为另一个基团，这可被认为代表氧化态的变化。我们通常将这些化合物称为氧化还原衍生物。本发明的衍生物可以仅通过单步转化与原始的母体活性药物化合物相关，或者可以通过包括氧化态的一个或多个变化的几个合成步骤相关。示例性衍生物具有式

8. 发明申请

US20140275205A1 PRODRUGS OF FUMARATES AND THEIR USE IN TREATING VARIOUS DISEASES 有权
标题翻译： FUMARATES的原料及其在治疗各种疾病中的应用
公开(公告)号：US20140275205A1
公开(公告)日：2014-09-18
申请号：US14180687
申请日：2014-02-14
申请人： ALKERMES PHARMA IRELAND LIMITED
发明人： Tarek A. Zeidan , Scott Duncan , Christopher P. Hencken , Thomas Andrew Wynn , Carlos N. Sanrame
IPC分类号： C07D207/12
CPC分类号： C07D491/113 , A61K31/4015 , C07C229/12 , C07C229/18 , C07C317/18 , C07C317/28 , C07D207/12 , C07D207/40 , C07D207/408 , C07D211/92 , C07D295/088
摘要： The present invention provides compounds of formula (I), wherein: R1 is unsubstituted C1-C6 alkyl; La is substituted or unsubstituted C1-C6 alkyl linker, substituted or unsubstituted C3-C10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R2 and R3 are each, independently, H, substituted or unsubstituted C1-C6 alkyl, or substituted or unsubstituted C6-C10 aryl; or alternatively, R2 and R3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S. The invention also provides pharmaceutical compositions and methods for treating neurological diseases, such as multiple sclerosis.
摘要翻译：本发明提供式（I）化合物，其中：R 1为未取代的C 1 -C 6烷基; La是取代或未取代的C 1 -C 6烷基接头，取代或未取代的C 3 -C 10碳环，含有一个或两个5-或6-元环和1-4个选自N，O和S的杂原子的取代或未取代的杂环，包含一个或两个5-或6-元环和1-4个选自N，O和S的杂原子的未取代杂芳基; 且R 2和R 3各自独立地为H，取代或未取代的C 1 -C 6烷基或取代或未取代的C 6 -C 10芳基; 或者可选地，R 2和R 3与它们所连接的氮原子一起形成取代或未取代的杂芳基，其包括一个或两个5-或6-元环和1-4个选自N，O和S的杂原子或取代的或未取代的杂环，其包含一个或两个5-或6-元环和1-4个选自N，O和S的杂原子。本发明还提供用于治疗神经疾病如多发性硬化的药物组合物和方法。

9. 发明申请

US20140163253A1 HYDROLYSABLE LINKERS AND CROSS-LINKERS FOR ABSORBABLE POLYMERS 有权
标题翻译：可水解连接器和可吸收聚合物的交联剂
公开(公告)号：US20140163253A1
公开(公告)日：2014-06-12
申请号：US14180561
申请日：2014-02-14
申请人： Bezwada Biomedical, LLC
发明人： Rao S. Bezwada
IPC分类号： C07C265/12 , C07C217/84 , C07C229/60
CPC分类号： C07C265/12 , A47F5/0006 , A61L17/00 , A61L17/105 , A61L17/12 , A61L17/145 , A61L24/06 , A61L27/18 , A61L27/34 , A61L27/52 , A61L27/58 , A61L31/10 , A61L31/145 , A61L31/148 , B65D25/22 , C07C69/34 , C07C69/67 , C07C69/708 , C07C205/37 , C07C205/43 , C07C205/57 , C07C217/84 , C07C219/34 , C07C225/22 , C07C229/18 , C07C229/60 , C07C235/16 , C08G63/16 , C08G63/916 , Y02W90/13 , Y10T24/44291 , Y10T24/51 , Y10T428/139 , Y10T442/10 , C08L67/04
摘要： The present invention relates to the discovery of new class of linear and multiarmed hydrolysable linkers and cross linkers for use in the synthesis of biodegradable polymers such as, polyesters, polyurethanes, polyamides, polyureas and degradable epoxy amine resin. The linear and multiarmed hydrolysable linkers of the present invention include symmetrical and/or unsymmetrical ether carboxylic acids, amines, amide diols, amine polyols and isocyanates.
摘要翻译：本发明涉及用于合成可生物降解聚合物如聚酯，聚氨酯，聚酰胺，聚脲和可降解环氧胺树脂的新类型的线性和多臂可水解连接体和交联剂的发现。本发明的线性和多臂可水解接头包括对称和/或不对称的醚羧酸，胺，酰胺二醇，胺多元醇和异氰酸酯。

10. 发明申请

US20140081054A1 CLASS OF HDAC INHIBITORS EXPANDS THE RENAL PROGENITOR CELLS POPULATION AND IMPROVES THE RATE OF RECOVERY FROM ACUTE KIDNEY INJURY 审中-公开
标题翻译： HDAC抑制剂类扩展了肾上腺癌细胞群体，提高了急性KIDNEY伤害恢复率
公开(公告)号：US20140081054A1
公开(公告)日：2014-03-20
申请号：US13982512
申请日：2012-02-10
申请人： Billy W. Day , Neil Hukriede
发明人： Billy W. Day , Neil Hukriede
IPC分类号： C07C29/80 , B01D15/18
CPC分类号： C07C29/80 , B01D15/1821 , C07C229/18 , C07C317/44 , C07C323/52 , C07C323/56 , C07C323/60 , C07C323/62
摘要： The invention concerns separation methods and systems including those comprising a continuous chromatographic simulated moving bed integrated with vapor compression distillation to create a high efficiency separations platform applicable to a broad range of separation functions.
摘要翻译：本发明涉及分离方法和系统，包括包括与蒸气压缩蒸馏一体化的连续色谱模拟移动床的分离方法和系统，以产生适用于宽范围分离功能的高效分离平台。

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