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61. 发明申请

US20070269368A1 HYDROPHILIC LIGHT ABSORBING COMPOSITIONS FOR DETERMINATION OF PHYSIOLOGICAL FUNCTION IN CRITICALLY ILL PATIENTS 失效
标题翻译：用于确定临床病人生理功能的亲水性吸收组合物
公开(公告)号：US20070269368A1
公开(公告)日：2007-11-22
申请号：US11778447
申请日：2007-07-16
申请人： Samuel Achilefu , Raghavan Rajagopalan , Richard Dorshow , Joseph Bugaj , Muthunadar Periasamy
发明人： Samuel Achilefu , Raghavan Rajagopalan , Richard Dorshow , Joseph Bugaj , Muthunadar Periasamy
IPC分类号： A61K49/20 , A61K31/19 , C07D235/04 , C07D277/84 , C07D293/10 , C07D263/60 , A61K31/4184
CPC分类号： C07D209/58 , A61K31/403 , A61K49/0021 , A61K49/0032 , C07D209/08 , C07D209/12 , C07D209/60
摘要： Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.
摘要翻译：公开了在可见光区域吸收和发出荧光的高度亲水的吲哚和苯并吲哚衍生物。这些化合物可用于生理和器官功能监测。特别地，本发明的分子可用于肾脏和心脏疾病的光学诊断以及体内血液体积估计。

62. 发明申请

US20060177457A1 DYE-SULFENATES FOR DUAL PHOTOTHERAPY 失效
公开(公告)号：US20060177457A1
公开(公告)日：2006-08-10
申请号：US11277057
申请日：2006-03-21
申请人： Raghavan Rajagopalan , Samuel Achilefu , Joseph Bugaj , Richard Dorshow
发明人： Raghavan Rajagopalan , Samuel Achilefu , Joseph Bugaj , Richard Dorshow
IPC分类号： A61K39/395 , A61K38/17 , A61K48/00 , A61K31/655 , A61K31/555 , A61K31/426 , A61K31/409 , A61K31/405 , C07K16/46 , C07K14/705
CPC分类号： A61K41/0033 , A61K41/0057 , A61K41/0071 , A61K49/0032 , A61K49/0056 , C09B23/083 , C09B47/065 , C09B47/0678 , C09B47/26
摘要： The present invention discloses dye-sulfenate derivatives and their bioconjugates for dual phototherapy of tumors and other lesions. The compounds of the present invention may contain either a mixture of Type 1 and Type 2 agents or a single entity that integrates both units in the same molecules. The compounds are designed to produce both Type 1 and Type 2 phototherapeutic effect at once using dual wavelength light source that will produce singlet oxygen and free radicals at the lesion of interest.
摘要翻译：本发明公开了用于肿瘤和其他病变双光疗法的染料 - 次硫酸盐衍生物及其生物缀合物。本发明的化合物可以含有1型和2型试剂的混合物，或者可以将相同分子中的两个单元整合的单个实体。这些化合物被设计成同时使用将在感兴趣的病变处产生单线态氧和自由基的双波长光源产生1型和2型光疗效应。

63. 发明申请

US20060100282A1 Novel diaminopropane-based metal chelators as antiviral agents 审中-公开
标题翻译：新型二氨基丙烷基金属螯合剂作为抗病毒剂
公开(公告)号：US20060100282A1
公开(公告)日：2006-05-11
申请号：US11259773
申请日：2005-10-27
申请人： Raghavan Rajagopalan , John Babu
发明人： Raghavan Rajagopalan , John Babu
IPC分类号： A61K31/195 , C07C229/34
CPC分类号： C07D215/26
摘要： This invention relates to novel diaminopropane-based divalent metal ion chelating ligands of Formula I, wherein A is selected from the group consisting of —(CH2)a—, —(CH2)bO(CH2)c—, —(CH2O)d—, and —(CH2)eN(R4)(CH2)f—; a and c vary from 0 to 10; b, e, and f vary from 2 to 10, and d varies from 1 to 10. X and Y are independently —CR5R6, or —CH(R7)CH(R8). R1 to R8 are various substituents selected to optimize the physicochemical and biological properties such as enzyme binding, tissue penetration, lipophilicity, toxicity, bioavailability, and pharmacokinetics of compounds of Formula 13. R1 to R8 may include, but are not limited to hydrogen, alkyl, acyl, hydroxyl, hydroxyalkyl, substituted or unsubstituted aryl, amino, aminoalkyl, alkoxyl, aryloxyl, carboxyl, halogen, alkoxycarbonyl, cyano, and other suitable electron donating or electron withdrawing groups. Ar may unsubstituted phenyl group or may be substituted with suitable electron donating or electron withdrawing groups. The compounds of the present invention are useful for inhibiting the activity of viral enzymes responsible for the proliferation of human immunodeficiency virus (HIV).
摘要翻译：本发明涉及式I的新型二氨基丙烷基二价金属离子螯合配体，其中A选自 - （CH 2）n - ， - （ CH 2（CH 2）2 - （CH 2）2 - ， - （CH 2） - （CH 2）2 N（R 4）（CH 3） > 2 a和c从0到10不等; b，e和f在2至10之间变化，d从1变化到10.X和Y独立地为-CR 6，或-CH（R CH（R 8）8。 R 1至R 8是各种取代基，其被选择用于优化式（I）化合物的物理化学和生物学性质，例如酶结合，组织穿透，亲油性，毒性，生物利用度和药代动力学 R 1至R 8可以包括但不限于氢，烷基，酰基，羟基，羟基烷基，取代或未取代的芳基，氨基，氨基烷基，烷氧基，芳氧基，羧基，卤素，烷氧基羰基，氰基和其它合适的给电子或吸电子基团。 Ar可以是未取代的苯基或可以被合适的给电子或吸电子基取代。本发明的化合物可用于抑制负责人免疫缺陷病毒（HIV）增殖的病毒酶的活性。

64. 发明授权

US5753205A Radiolabelled peptide compounds 失效
公开(公告)号：US5753205A
公开(公告)日：1998-05-19
申请号：US372547
申请日：1995-01-13
申请人： Leon R. Lyle , Raghavan Rajagopalan , Karen Deutsch
发明人： Leon R. Lyle , Raghavan Rajagopalan , Karen Deutsch
IPC分类号： A61K51/04 , A61K51/08 , C07B59/00 , C07D213/40 , C07D213/64 , C07D213/68 , C07F13/00 , C07K14/655 , C07K14/815 , A61K51/00 , A61M36/14
CPC分类号： C07K14/815 , A61K51/0478 , A61K51/083 , A61K51/088 , C07B59/004 , C07D213/40 , C07D213/64 , C07D213/68 , C07F13/005 , C07K14/6555 , A61K2121/00 , A61K2123/00
摘要： A diagnostic composition suitable for administration to a warm-blooded animal comprising somatostatin or a molecule capable of interacting with the somatostatin receptor labeled with a radionuclide by means of a chelate ligand capable of administration to an animal to produce reliable visual imaging of tumors or therapeutic effects on tumors.

65. 发明授权

US5672333A Delta.sup.1,6 bicyclo �4,4,0! functional dyes for contrast enhancement in optical imaging 失效
标题翻译： Delta1,6双环[4,4,0]功能染料，用于光学成像中的对比度增强
公开(公告)号：US5672333A
公开(公告)日：1997-09-30
申请号：US649850
申请日：1996-05-13
申请人： Raghavan Rajagopalan , Ella Y. Fung
发明人： Raghavan Rajagopalan , Ella Y. Fung
IPC分类号： C07D277/64 , A61K49/00 , G01N33/52 , G01N31/00 , G01N33/48
CPC分类号： A61K49/0021 , A61K49/0032 , G01N33/52
摘要： This invention provides functional dyes of the general formula: ##STR1## wherein R1, R2, and R.sup.5 may be the same or different and are selected from the group consisting of hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxyl, hydroxyl, C.sub.1 -C.sub.10 hydroxyalkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.10 aryl, carboxyl, C.sub.1 -C.sub.10 carboxylalkyl, halogen, nitro, C.sub.1 -C.sub.10 alkoxycarbonyl, mercapto, C.sub.1 -C.sub.10 mercaptoalkyl, C.sub.1 -C.sub.10 alkylthio, sulfonate, and --(CH.sub.2).sub.m --N(R.sup.6)(R.sup.7) wherein R.sup.6 and R.sup.7 are independently hydrogen or C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 acyl, and R.sup.6 and R.sup.7 are capable of forming 5, 6, or 7 membered rings which may optionally be substituted with --O--, --NR.sup.8, or --S--; R.sup.3 and R.sup.4 may be the same or different and are selected from the group consisting of C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 hydroxyalkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.10 aryl, C.sub.1 -C.sub.10 carboxylalkyl, C.sub.1 -C.sub.10 alkyl sulfonate, mercapto alkyl and --(CH.sub.2).sub.m N(R.sup.6)(R.sup.7); W.sup.1 and W.sup.2 may be the same or different and are selected from the group consisting of --S--, --O--, --Se--, --Te--, --NR.sup.8 and C(R.sup.9)(R.sup.10); and m is about 0-10; R.sup.8, R.sup.9, and R.sup.10 are independently hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy, C.sub.1 -C.sub.10 mercaptoalkyl, hydroxyl, C.sub.1 -C.sub.10 hydroxyalkyl, C.sub.1 -C.sub.10 alkoxyalkyl, C.sub.1 -C.sub.10 aryl, C.sub.1 -C.sub.10 carboxylalkyl, C.sub.1 -C.sub.10 alkoxycarbonyl, C.sub.1 -C.sub.10 alkylthio, and --(CH.sub.2).sub.m --N(R.sup.6)(R.sup.7); and A is selected from the group consisting of --(CH.sub.2)--, --O--, --S--, or --NR.sup.8. Also provided are methods of using dyes of the invention comprising administering a diagnostically effective amount of the dye to a patient and visualizing the dye.
摘要翻译：本发明提供以下通式的功能性染料：其中R 1，R 2和R 5可以相同或不同，并且选自氢，C 1 -C 10烷基，C 1 -C 10烷氧基，羟基，C 1 -C 10羟基烷基，C 1 -C 10烷氧基烷基，C 1 -C 10芳基，羧基，C 1 -C 10羧基烷基，卤素，硝基，C 1 -C 10烷氧基羰基，巯基，C 1 -C 10巯基烷基，C 1 -C 10烷硫基，磺酸酯基和 - （CH 2）（R6）（R7）其中R6和R7独立地是氢或C1-C10烷基，C1-C10酰基，R6和R7能够形成5,6或7元环，其可任选地被-O-取代， -NR8或-S-; R3和R4可以相同或不同，并且选自C1-C10烷基，C1-C10羟基烷基，C1-C10烷氧基烷基，C1-C10芳基，C1-C10羧基烷基，C1-C10烷基磺酸酯，巯基烷基和 - （CH 2）m N（R 6）（R 7）; W1和W2可以相同或不同，并且选自-S-，-O-，-Se-，-Te-，-NR8和C（R9）（R10）; m为约0-10; R8，R9和R10独立地是氢，C1-C10烷基，C1-C10烷氧基，C1-C10巯基烷基，羟基，C1-C10羟基烷基，C1-C10烷氧基烷基，C1-C10芳基，C1-C10羧基烷基，C1-C10 烷氧基羰基，C 1 -C 10烷硫基和 - （CH 2）m N（R 6）（R 7）; 并且A选自 - （CH 2） - ， - O - ， - S - 或-NR 8。还提供了使用本发明的染料的方法，包括向患者施用诊断有效量的染料并使染色剂可视化。

66. 发明授权

US5656253A Ligands useful in radiographic imaging 失效
标题翻译：配体可用于放射成像
公开(公告)号：US5656253A
公开(公告)日：1997-08-12
申请号：US255148
申请日：1994-06-07
申请人： Raghavan Rajagopalan , Ananthachari Srinivasan , Jean-Luc Vanderheyden
发明人： Raghavan Rajagopalan , Ananthachari Srinivasan , Jean-Luc Vanderheyden
IPC分类号： A61K51/04 , A61K51/08 , C07B59/00 , C07D213/40 , C07D213/64 , C07D213/68 , C07F13/00 , C07K14/655 , C07K14/815 , A61K51/00 , A61K7/32 , C07D211/70 , C07D401/02
CPC分类号： C07K14/815 , A61K51/0478 , A61K51/088 , C07B59/004 , C07D213/40 , C07D213/64 , C07D213/68 , C07F13/005 , C07K14/6555 , A61K2121/00 , A61K2123/00
摘要： The present invention relates particularly to novel pyridine based nitrogen-sulfur ligands that are suitable for complexing with a radionuclide, and are useful as general imaging agents for diagnostic purposes, novel aminothiol ligands that are suitable for complexing with a radionuclide, and are useful as general imaging agents for diagnostic purposes, and amide-thiolate ligands having improved metal chelate formation kinetics. The amide-thiolate ligands include an amine which converts to a vinylogous amide upon complexation, thereby providing rapid complexation and thermodynamic stability. The ligands may be used for post formed labeling of biological substances for use in the fields of diagnosis and therapy.
摘要翻译：本发明特别涉及适用于与放射性核素络合的新型吡啶类氮硫配体，并且可用作诊断目的的一般成像剂，适于与放射性核素络合的新型氨基硫醇配体，并且可用作一般用于诊断目的的成像剂和具有改善的金属螯合物形成动力学的酰胺 - 硫醇酸配体。酰胺 - 硫醇酸酯配体包括在络合时转化为戊烯酰胺的胺，从而提供快速的络合和热力学稳定性。配体可用于生物物质的后期标记用于诊断和治疗领域。

67. 发明授权

US5653958A Imidazole based nitrogen-sulfur ligands useful in radiographic imaging agents 失效
标题翻译：用于放射成像剂的咪唑基氮硫配体
公开(公告)号：US5653958A
公开(公告)日：1997-08-05
申请号：US419319
申请日：1995-04-10
申请人： Raghavan Rajagopalan , Ananthachari Srinivasan
发明人： Raghavan Rajagopalan , Ananthachari Srinivasan
IPC分类号： C07D233/64 , A61K51/00 , A61K51/04 , C07D233/54 , C07D233/91 , C07D405/12 , C07F13/00
CPC分类号： C07F13/005 , A61K51/0478 , C07D233/64 , C07D405/12 , A61K2123/00
摘要： The present invention relates particularly to novel imidazole based nitrogen-sulfur ligands that are suitable for complexing with a radionuclide, and are useful as general imaging agents for diagnostic purposes.
摘要翻译：本发明特别涉及适用于与放射性核素络合的新型咪唑基氮硫配体，并且可用作用于诊断目的的一般成像剂。

68. 发明授权

US5376357A Magnetic resonance imaging agents 失效
标题翻译：磁共振成像剂
公开(公告)号：US5376357A
公开(公告)日：1994-12-27
申请号：US631507
申请日：1990-12-21
申请人： Raghavan Rajagopalan , Muthunadar P. Periasamy
发明人： Raghavan Rajagopalan , Muthunadar P. Periasamy
IPC分类号： A61K49/06 , A61K49/00
CPC分类号： A61K49/06 , Y10T436/24
摘要： Novel magnetic resonance imaging agents comprise complexes of paramagnetic ions with aminoalkylamide derivatives of diethylenetriaminepentaacetic acid ("DTPA") or ethylenediaminetetraacetic acid ("EDTA") or other polyaminocarboxylic or cyclic polyaminocarboxylic chelating agents, These novel imaging agents are characterized by excellent NMR image-contrasting properties and by high solubilities in physiological solutions.A novel method of performing an NMR diagnostic procedure involves administering to a warm-blooded animal an effective amount of a complex as described above and then exposing the warm-blooded animal to an NMR imaging procedure, thereby imaging at least a portion of the body of the warm-blooded animal.
摘要翻译：新型磁共振成像剂包括顺磁性离子与二亚乙基三胺五乙酸（“DTPA”）或乙二胺四乙酸（“EDTA”）或其他聚氨基羧酸或环状聚氨基羧酸螯合剂的氨基烷基酰胺衍生物的复合物。这些新型成像剂的特征在于优异的NMR图像对比性质和生理溶液中的高溶解度。执行NMR诊断程序的新方法包括向温血动物施用有效量的如上所述的复合物，然后将温血动物暴露于NMR成像过程，从而使至少一部分身体成像温血动物。

69. 发明授权

US09226980B2 Azulene and azaazulene systems for imaging, monitoring and therapy 有权
标题翻译：用于成像，监测和治疗的Azulene和azaazulene系统
公开(公告)号：US09226980B2
公开(公告)日：2016-01-05
申请号：US13395493
申请日：2010-09-10
申请人： Raghavan Rajagopalan
发明人： Raghavan Rajagopalan
IPC分类号： A61B10/00 , A61B8/00 , A61B5/00 , A61K49/00 , A61K41/00
CPC分类号： C07K7/06 , A61K38/00 , A61K41/0057 , A61K49/0021 , A61K49/0045 , A61K49/0056 , C07C247/14 , C07D261/02 , C07D261/04
摘要： This invention is directed to non-benzenoid aromatic compounds. Other aspects include methods of using non-benzenoid aromatic compounds for imaging and phototherapeutic uses thereof. Non-benzenoid compounds provided herein generally have one or more substituent groups which allow tailoring of the spectral properties or provide photoreactivity or targeting ability.
摘要翻译：本发明涉及非苯类化合物。其他方面包括使用非苯并芳族化合物进行成像和光疗用途的方法。本文提供的非苯类化合物通常具有一个或多个取代基，其允许调整光谱性质或提供光反应性或靶向能力。

70. 发明授权

US08829020B2 Compounds and compositions for use in phototherapy and in treatment of ocular neovascular disease and cancers 有权
标题翻译：用于光疗和治疗眼新生血管病和癌症的化合物和组合物
公开(公告)号：US08829020B2
公开(公告)日：2014-09-09
申请号：US13383243
申请日：2010-07-16
申请人： Gary L. Cantrell , Raghavan Rajagopalan , David W. Berberich , Amolkumar Karwa , Richard B. Dorshow
发明人： Gary L. Cantrell , Raghavan Rajagopalan , David W. Berberich , Amolkumar Karwa , Richard B. Dorshow
IPC分类号： A61K31/485 , A61K31/472 , A61K9/00 , A61K9/02 , A61K9/10 , A61K9/14 , A61K9/20 , A61K9/48 , A61K41/00 , A61K45/06 , A61K47/26 , A61K47/36 , A61K47/38
CPC分类号： C07D489/02 , A61K9/0075 , A61K9/02 , A61K9/10 , A61K9/145 , A61K9/2009 , A61K9/2022 , A61K9/2027 , A61K9/2054 , A61K9/2059 , A61K9/4858 , A61K9/4866 , A61K31/472 , A61K31/485 , A61K41/0057 , A61K45/06 , A61K47/26 , A61K47/36 , A61K47/38 , C07D221/28 , A61K2300/00
摘要： The invention relates generally to anti-angiogenesis agents and related methods of using to anti-angiogenesis agents for biomedical applications including direct monotherapy and combination therapy for treatment of an angiogenesis related condition. In an embodiment, the invention provides a class of opioid compounds and structurally related opioid derivatives exhibiting anti-VEGF activity for use in therapeutic procedures, including phototherapy. Opioid compounds and structurally related opioid derivatives of the invention may be administered alone or in combination with administration of a phototherapy agent and/or other therapeutic agent.
摘要翻译：本发明一般涉及用于生物医学应用的抗血管发生剂的抗血管发生剂和相关方法，包括用于治疗血管生成相关病症的直接单药治疗和联合治疗。在一个实施方案中，本发明提供一类阿片类化合物和结构上相关的阿片类衍生物，其表现出抗VEGF活性，用于治疗程序，包括光疗法。本发明的阿片样物质和结构相关的阿片样物质衍生物可以单独施用或与施用光疗剂和/或其它治疗剂组合施用。

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