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61. 发明授权

US06204293B1 Inhibitors of protein isoprenyl transferases 失效
标题翻译：蛋白质异戊二烯转移酶抑制剂
公开(公告)号：US06204293B1
公开(公告)日：2001-03-20
申请号：US09073807
申请日：1998-05-07
申请人： Said M. Sebti , Andrew D. Hamilton , David J. Augeri , Kenneth J. Barr , Stephen A. Fakhoury , David A. Janowick , Douglas M. Kalvin , Stephen J. O'Connor , Saul H. Rosenberg , Wang Shen , Rolf E. Swenson , Bryan K. Sorensen , Gerard M. Sullivan , Andrew S. Tasker , James T. Wasicak , Lissa T. J. Nelson , Kenneth J. Henry , Le Wang , Gang Liu , Indrani W. Gunawardana
发明人： Said M. Sebti , Andrew D. Hamilton , David J. Augeri , Kenneth J. Barr , Stephen A. Fakhoury , David A. Janowick , Douglas M. Kalvin , Stephen J. O'Connor , Saul H. Rosenberg , Wang Shen , Rolf E. Swenson , Bryan K. Sorensen , Gerard M. Sullivan , Andrew S. Tasker , James T. Wasicak , Lissa T. J. Nelson , Kenneth J. Henry , Le Wang , Gang Liu , Indrani W. Gunawardana
IPC分类号： C07C26302
CPC分类号： C07C237/36 , C07B2200/07 , C07C239/20 , C07C271/22 , C07C317/50 , C07C323/59 , C07C323/60 , C07C327/42 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2602/08 , C07C2603/18 , C07C2603/24 , C07C2603/74 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/10 , C07D207/12 , C07D207/26 , C07D207/267 , C07D209/48 , C07D211/14 , C07D211/42 , C07D211/52 , C07D211/58 , C07D213/30 , C07D213/32 , C07D213/34 , C07D213/36 , C07D213/38 , C07D213/56 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/82 , C07D213/89 , C07D231/12 , C07D233/56 , C07D233/64 , C07D233/90 , C07D235/06 , C07D237/14 , C07D239/26 , C07D239/42 , C07D241/04 , C07D241/12 , C07D241/18 , C07D249/08 , C07D253/06 , C07D257/04 , C07D261/02 , C07D263/22 , C07D263/32 , C07D265/30 , C07D277/30 , C07D277/36 , C07D277/48 , C07D277/50 , C07D277/587 , C07D279/12 , C07D295/084 , C07D295/13 , C07D295/155 , C07D295/185 , C07D307/54 , C07D307/81 , C07D317/30 , C07D317/60 , C07D333/18 , C07D333/20 , C07D333/24 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D417/12 , C07D487/08 , C07F9/5333
摘要： Compounds having the formula or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L2—, and (i) heterocyclic-L2—; R2 is selected from (b) —C(O)NH—CH(R14)—C(O)OR15, (d) —C(O)NH—CH(R14)—C(O)NHSO2R16, (e) —C(O)NH—CH(R14)-tetrazolyl, (f) —C(O)NH-heterocyclic, and (g) —C(O)NH—CH(R14)—C(O)NR17R18; R3 is heterocyclic, aryl, substituted or unsubstituted cycloalkyl; R4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) —L4—N(R5)—L5—, (b) —L4—O—L5—, (c) —L4—S(O)n—L5— (d) —L4—L6—C(W)—N(R5)—L5—, (e) —L4—L6—S(O)m—N(R5)—L5 —, (f) —L4—N(R5)—C(W)—L7—L5 —, (g) —L4—N(R5)—S(O)p—L7—L5—, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, and (j) optionally substituted alkynylene are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.
摘要翻译：具有式的化合物或其药学上可接受的盐，其中R 1是（a）氢，（b）低级烷基，（c）烯基，（d）烷氧基，（e）硫代烷氧基，（f）卤素，（g）卤代烷基，（h）芳基-L2-和（i）杂环-L2-; R2选自（b）-C（O）NH-CH（R14）-C（O）OR15，（d）-C（O）NH-CH（R14）-C（O）NHSO2R16，（e） C（O）NH-CH（R 14） - 四唑基，（f）-C（O）NH-杂环基和（g）-C（O）NH-CH（R 14）-C（O）NR 17 R 18; R3是杂环，芳基，取代或未取代的环烷基; R4是氢，低级烷基，卤代烷基，卤素，芳基，芳基烷基，杂环或（杂环）烷基; （a）-L4-N（R5）-L5-，（b）-L4-O-L5-，（c）-L4-S（O）n-L5-（d） - L4-L6-C（W）-N（R5）-L5-，（e）-L4-L6-S（O）mN（R5）-L5 - ，（f）-L4-N（R5）-C W）-L7-L5 - ，（g）-L4-N（R5）-S（O）p-L7-L5-，（h）任选取代的亚烷基，（i）任选取代的亚烯基，和（j）亚炔基是蛋白质异戊二烯转移酶的抑制剂。还公开了蛋白质异戊二烯转移酶抑制组合物和抑制蛋白质异戊二烯转移酶的方法。

62. 发明授权

US5391755A Synthesis of 19-NOR vitamin D compounds 失效
标题翻译： 19-NOR维生素D化合物的合成
公开(公告)号：US5391755A
公开(公告)日：1995-02-21
申请号：US180702
申请日：1994-01-13
申请人： Hector F. DeLuca , Heinrich K. Schnoes , Kato L. Perlman , Rolf E. Swenson
发明人： Hector F. DeLuca , Heinrich K. Schnoes , Kato L. Perlman , Rolf E. Swenson
IPC分类号： A61K31/59 , A61P35/00 , C07C35/14 , C07C35/17 , C07C43/115 , C07C49/497 , C07C67/343 , C07C69/732 , C07C69/734 , C07C69/74 , C07C317/18 , C07C401/00 , C07D307/20 , C07D309/12 , C07F7/08 , C07F7/18 , C07F9/40 , C07F9/53 , C07C69/75
CPC分类号： C07F7/1856 , C07C401/00 , C07F9/532 , Y02P20/55
摘要： A convergent synthesis of 19-nor-vitamin D compounds, specifically 19-nor-1.alpha.,25-dihydroxyvitamin D.sub.3, is disclosed. The synthesis can also readily be utilized for preparing other 1.alpha.-hydroxylated 19-nor-vitamin D compounds. The key step in the synthesis is a suitable application of Lythgoe's procedure i.e. a Horner-Wittig reaction of the lithium anion of a phosphine oxide with a Windaus Grundmann ketone to give, after any necessary deprotection, the desired 19-nor-vitamin D compound.
摘要翻译：公开了19-维生素D化合物，特别是19-nor-1α，25-二羟基维生素D3的会聚合成。合成还可以容易地用于制备其它1α-羟基化的19-维生素D化合物。合成中的关键步骤是Lythgoe方法的合适应用，即氧化膦锂的阴离子与Windaus Grundmann酮的Horner-Wittig反应，在任何必需的脱保护后，得到所需的19-维生素D化合物。

63. 发明授权

US5281731A Synthesis of 19-nor vitamin D compounds 失效
标题翻译：合成19-维生素D化合物
公开(公告)号：US5281731A
公开(公告)日：1994-01-25
申请号：US979482
申请日：1992-11-20
申请人： Hector F. DeLuca , Heinrich K. Schnoes , Kato L. Perlman , Rolf E. Swenson
发明人： Hector F. DeLuca , Heinrich K. Schnoes , Kato L. Perlman , Rolf E. Swenson
IPC分类号： A61K31/59 , A61P35/00 , C07C35/14 , C07C35/17 , C07C43/115 , C07C49/497 , C07C67/343 , C07C69/732 , C07C69/734 , C07C69/74 , C07C317/18 , C07C401/00 , C07D307/20 , C07D309/12 , C07F7/08 , C07F7/18 , C07F9/40 , C07F9/53
CPC分类号： C07F7/1856 , C07C401/00 , C07F9/532 , Y02P20/55
摘要： A convergent synthesis of 19-nor-vitamin D compounds, specifically 19-nor-1.alpha.,25-dihydroxyvitamin D.sub.3, is disclosed. The synthesis can also readily be utilized for preparing other 1.alpha.-hydroxylated 19-nor-vitamin D compounds. The key step in the synthesis is a suitable application of Lythgoe's procedure i.e. a Horner-Wittig reaction of the lithium anion of a phosphine oxide with a Windaus Grundmann ketone to give, after any necessary deprotection, the desired 19-nor-vitamin D compound.
摘要翻译：公开了19-维生素D化合物，特别是19-nor-1α，25-二羟基维生素D3的会聚合成。合成还可以容易地用于制备其它1α-羟基化的19-维生素D化合物。合成中的关键步骤是Lythgoe方法的合适应用，即氧化膦锂的阴离子与Windaus Grundmann酮的Horner-Wittig反应，在任何必需的脱保护后，得到所需的19-维生素D化合物。

64. 发明申请

US20150045332A1 Novel Sphingosine 1-Phosphate Receptor Antagonists 有权
标题翻译：新型鞘氨醇1-磷酸受体拮抗剂
公开(公告)号：US20150045332A1
公开(公告)日：2015-02-12
申请号：US14386990
申请日：2013-03-21
申请人： Rolf E. SWENSON
发明人： Rolf E. Swenson
IPC分类号： C07D471/04 , A61K31/437 , A61K45/06 , A61K31/444
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K45/06
摘要： The present invention relates to sphingosine-1-phosphate (S1P) receptors and compounds of the general formula: that are useful in the treatment and prevention of conditions associated with such receptors. More specifically, the present invention relates to the synthesis and use of sphingosine 1-phosphate receptor 2 (S1P2) antagonists that are useful in the treatment of cancer, atherosclerosis, diabetic retinopathy, and other inflammatory diseases. Among these inflammatory diseases that could be treated with these S1P2 antagonist are those characterized by fibrosis including chronic lung disease, chronic kidney and liver disease, chronic heart disease, and skin diseases such as sclerosis/scleroderma. The S1P2 antagonists can also be used in the treatment of glioblastoma multiforme (brain cancer), pediatric neuroblastoma, and other cancers.
摘要翻译：本发明涉及鞘氨醇-1-磷酸（S1P）受体和通式的化合物：其可用于治疗和预防与此类受体相关的病症。更具体地说，本发明涉及可用于治疗癌症，动脉粥样硬化，糖尿病性视网膜病和其它炎性疾病的鞘氨醇1-磷酸受体2（S1P2）拮抗剂的合成和用途。可以用这些S1P2拮抗剂治疗的这些炎性疾病中的那些是以纤维化为特征的，包括慢性肺部疾病，慢性肾脏和肝脏疾病，慢性心脏病和皮肤疾病如硬化症/硬皮病。 S1P2拮抗剂也可用于治疗多形性成胶质细胞瘤（脑癌），儿科神经母细胞瘤等癌症。

66. 发明授权

US08293214B2 Targeting and therapeutic compounds and gas-filled microvesicles comprising said compounds 有权
标题翻译：靶向和治疗化合物和包含所述化合物的充气微泡
公开(公告)号：US08293214B2
公开(公告)日：2012-10-23
申请号：US12448401
申请日：2007-12-19
申请人： Rolf E. Swenson , Philippe Bussat , Bernard Lamy , Sibylle Pochon , Kondareddiar Ramalingam
发明人： Rolf E. Swenson , Philippe Bussat , Bernard Lamy , Sibylle Pochon , Kondareddiar Ramalingam
IPC分类号： A61B8/00 , A61K38/00
CPC分类号： A61K49/223
摘要： New targeting or therapeutic compounds which can be incorporated into a composition of gas-filled microvesicles. The invention further relates to gas-filled microvesicles for diagnostic and/or therapeutic use comprising said compounds and to their method of use. The new compounds are compounds of formula M-S-T, wherein: M represents a component capable of associating with an envelope of a gas-filled microvesicle; T represents a component comprising a targeting ligand or a therapeutic agent; and S represents a component comprising at least two bissulfone groups.
摘要翻译：可以掺入气体填充微泡组合物中的新靶向或治疗化合物。本发明还涉及用于诊断和/或治疗用途的充气微泡，其包含所述化合物及其使用方法。新化合物是式M-S-T的化合物，其中：M表示能与气体填充的微泡的包膜缔合的成分; T表示包含靶向配体或治疗剂的组分; S表示包含至少两个双砜基团的组分。

67. 发明申请

US20120065365A1 Stable Radiopharmaceutical Compositions and Methods for Their Preparation 审中-公开
标题翻译：稳定的放射性药物组合物及其制备方法
公开(公告)号：US20120065365A1
公开(公告)日：2012-03-15
申请号：US13280485
申请日：2011-10-25
申请人： Jianqing Chen , Karen E. Linder , Edmund R. Marinelli , Edmund Metcalfe , Adrian D. Nunn , Rolf E. Swenson , Michael F. Tweedle
发明人： Jianqing Chen , Karen E. Linder , Edmund R. Marinelli , Edmund Metcalfe , Adrian D. Nunn , Rolf E. Swenson , Michael F. Tweedle
IPC分类号： C07K7/06 , C07K14/655 , C07K7/18 , C07K14/595 , C07K7/23 , C07K14/68 , C07K7/16 , C07K14/62 , C07K14/545
CPC分类号： A61K51/12 , A61K51/088
摘要： Stabilized radiopharmaceutical formulations are disclosed. Methods of making and using stabilized radiopharmaceutical formulations are also disclosed. The invention relates to stabilizers that improve the radiostability of radiotherapeutic and radiodiagnostic compounds and formulations containing them. In particular, it relates to stabilizers useful in the preparation and stabilization of targeted radiodiagnostic and radiotherapeutic compounds, and, in a preferred embodiment, to the preparation and stabilization of radiodiagnostic and radiotherapeutic compounds that are targeted to the Gastrin Releasing Peptide Receptor (GRP-Receptor).
摘要翻译：公开了稳定的放射性药物制剂。还公开了制备和使用稳定的放射性药物制剂的方法。本发明涉及改善放射治疗和放射性诊断化合物和含有它们的制剂的无线电稳定性的稳定剂。特别地，本发明涉及可用于靶向放射性诊断和放射治疗化合物的制备和稳定化的稳定剂，并且在优选的实施方案中涉及靶向胃泌素释放肽受体（GRP-受体）的放射性诊断和放射治疗化合物的制备和稳定）。

69. 发明申请

US20110172524A1 INFUSION SYSTEMS INCLUDING COMPUTER-FACILITATED MAINTENANCE AND/OR OPERATION AND METHODS OF USE 有权
标题翻译：输入系统，包括计算机辅助维护和/或操作及使用方法
公开(公告)号：US20110172524A1
公开(公告)日：2011-07-14
申请号：US12808467
申请日：2009-06-11
申请人： Stephen E. Hidem , Aaron M. Fontaine , Janet L. Gelbach , Patrick M. McDonald , Kathryn M. Hunter , Rolf E. Swenson , Julius P. Zodda
发明人： Stephen E. Hidem , Aaron M. Fontaine , Janet L. Gelbach , Patrick M. McDonald , Kathryn M. Hunter , Rolf E. Swenson , Julius P. Zodda
IPC分类号： A61B6/00
CPC分类号： A61M5/007 , A61B6/037 , A61B6/107 , A61B6/481 , A61B6/507 , A61B50/13 , A61B90/39 , A61B2050/105 , A61B2090/392 , A61K51/00 , A61M5/14 , A61M5/1409 , A61M5/142 , A61M5/1452 , A61M5/158 , A61M5/16854 , A61M5/16881 , A61M5/365 , A61M2005/1403 , A61M2205/18 , A61M2205/276 , A61M2205/3375 , A61M2205/50 , A61M2205/505 , A61M2205/52 , A61M2205/584 , A61M2205/587 , A61M2205/6009 , A61M2205/6054 , A61M2205/6072 , A61M2205/70 , A61M2205/75 , A61M2209/084 , A61N5/1001 , A61N5/1007 , A61N5/1075 , A61N2005/1021 , A61N2005/1022 , A61N2005/1074 , A61N2005/1094 , B62B3/005 , G06F19/00 , G06F19/3468 , G06F21/31 , G21F3/00 , G21F7/00 , G21G1/0005 , G21G1/001 , G21G4/08 , G21G2001/0031
摘要： Methods for setting up, maintaining and operating a radiopharmaceutical infusion system, that includes a radioisotope generator, are facilitated by a computer of the system. The computer includes pre-programmed instructions and a computer interface, for interaction with a user of the system, for example, in order to track contained volumes of eluant and/or eluate, and/or to track time from completion of an elution performed by the system, and/or to calculate one or more system and/or injection parameters for quality control, and/or to perform purges of the system, and/or to facilitate diagnostic imaging.
摘要翻译：用于设置，维护和操作包括放射性同位素发生器的放射性药物输注系统的方法由系统的计算机促进。计算机包括用于与系统的用户相互作用的预编程指令和计算机接口，例如，为了跟踪洗脱液和/或洗脱液的含有体积，和/或跟踪从完成洗脱的时间系统和/或计算用于质量控制的一个或多个系统和/或注入参数，和/或执行系统清除和/或促进诊断成像。

70. 发明授权

US07922998B2 Gastrin releasing peptide compounds 失效
标题翻译：胃泌素释放肽化合物
公开(公告)号：US07922998B2
公开(公告)日：2011-04-12
申请号：US11165721
申请日：2005-06-24
申请人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund Marinelli , Palaniappa Nanjappan , Natarajan Raju , Kondareddiar Ramalingam , Rolf E. Swenson , Michael Tweedle
发明人： Enrico Cappelletti , Luciano Lattuada , Karen E. Linder , Edmund Marinelli , Palaniappa Nanjappan , Natarajan Raju , Kondareddiar Ramalingam , Rolf E. Swenson , Michael Tweedle
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： A61K51/088 , A61K49/0002 , C07C269/04 , C07D257/00 , C07J41/0005 , C07J41/0011 , C07J43/003 , C07K14/57572 , C07C271/22
摘要： New and improved compounds for use in diagnostic imaging or therapy having the formula M-N—O—P-G, wherein M is a metal chelator having the structure: wherein R1-R5 and FG are as defined herein (in the form complexed with a metal radionuclide or not), N—O—P is the linker containing at least one non-alpha amino acid with a cyclic group, at least one substituted bile acid or at least one non-alpha amino acid, and G is the GRP receptor targeting peptide. In the preferred embodiment, M is an Aazta metal chelator or a derivative thereof. Methods for imaging a patient and/or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided.
摘要翻译：用于具有式MN-O-PG的诊断成像或治疗的新的和改进的化合物，其中M是具有以下结构的金属螯合剂：其中R1-R5和FG如本文所定义（以与金属放射性核素复合的形式或不是），N-O-P是含有至少一个具有环状基团，至少一个取代的胆汁酸或至少一个非α氨基酸的非α氨基酸的接头，G是GRP受体靶向肽。在优选的实施方案中，M是Aazta金属螯合剂或其衍生物。还提供了使用本发明的化合物对患者成像和/或向患者提供放射治疗或光疗的方法。还提供了用于从该化合物制备诊断显像剂的方法和试剂盒。还提供了用于制备放射治疗剂的方法和试剂盒。

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