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1. 发明专利

AU2002329097B2 Inclusion compound comprising cucurbituril derivatives as host molecule and pharmaceutical composition comprising the same 未知
公开(公告)号：AU2002329097B2
公开(公告)日：2005-09-15
申请号：AU2002329097
申请日：2002-09-18
申请人： POSTECH FOUND
发明人： KIM KIMOON , JEON YOUNG JIN , KIM SOO-YOUNG , KO YOUNG HO
IPC分类号： C07D487/04 , C07F1/12 , C07F5/00 , C07F15/00 , C07F005/00
摘要： The present invention provides an inclusion compound having a cucurbituril derivative of the formula 1 as a host molecule and a metal complex of the formula 2 as a guest molecule. A pharmaceutical composition having an anticancer effect can be obtained by using the inclusion compound according to the present invention. The pharmaceutical composition can prevent effective components from being biologically degraded in vivo and can exhibit continuous drug effect for a long time just by a single dosage by controlling the release time of the platinum complex once it reaches target tumor cells.

2. 发明申请

US20040253177A1 Method for monitoring blood flow and metabolic uptake in tissue with radiolabeled alkanoic acid 有权
标题翻译：用放射性标记的链烷酸监测组织中血流和代谢摄取的方法
公开(公告)号：US20040253177A1
公开(公告)日：2004-12-16
申请号：US10827054
申请日：2004-04-19
发明人： David R. Elmaleh , Alan J. Fischman , Timothy M. Shoup
IPC分类号： A61K051/00 , C07F005/00
CPC分类号： A61K51/0402
摘要： The present invention relates to novel modified fatty acid analogs, where a positron or gamma-emitting label is placed at a position on a fatty acid backbone and an organic substituent is substituted at the 2,3; 3,4; 4,5; 5,6 and other sequence positions of a fatty acid backbone. These novel fatty acid analogs are designed to enter the tissues of interest by the same long chain fatty acid carrier mechanism as natural fatty acids, however, functional substituents in the 2,3; 3,4; 4,5; 5,6 and other sequence positions, block the catabolic pathway, thus trapping these analogs in a virtually unmodified form in the tissues of interest.
摘要翻译：本发明涉及新的改性脂肪酸类似物，其中将正电子或γ发射标记物置于脂肪酸主链上的位置，有机取代基被置换在2,3; 3,4; 4,5; 5,6和脂肪酸骨架的其他序列位置。这些新的脂肪酸类似物被设计成通过与天然脂肪酸相同的长链脂肪酸载体机制进入感兴趣的组织，然而，2,3中的官能取代基; 3,4; 4,5; 5,6和其他序列位置，阻断分解代谢途径，从而在感兴趣的组织中以几乎未修饰的形式捕获这些类似物。

3. 发明申请

US20040166058A1 Ethylenedicysteine (EC)-drug conjugates, compositions and methods for tissue specific disease imaging 审中-公开
标题翻译：亚乙基半胱氨酸（EC） - 药物共轭物，组织特异性疾病成像的组合物和方法
公开(公告)号：US20040166058A1
公开(公告)日：2004-08-26
申请号：US10703405
申请日：2003-11-07
申请人： Board of Regents, The University of Texas System , Cell>Point LLC
发明人： David J. Yang , Dong-Fang Yu , Chang-Sok Oh , Jerry L. Bryant JR.
IPC分类号： A61K051/00 , C07K016/46 , C07F005/00
CPC分类号： C07F13/005 , A61K51/04 , A61K51/0402 , A61K51/0453 , A61K51/0455 , A61K51/0459 , A61K51/0487 , A61K51/0491 , A61K51/08 , A61K51/081 , A61K51/088 , A61K51/1027 , A61K51/1093
摘要： The invention provides, in a general sense, a new labeling strategy employing compounds that are are N2S2 chelates conjugated to a targeting ligand, wherein the targeting ligand is a disease cell cycle targeting compound, a tumor angiogenesis targeting ligand, a tumor apoptosis targeting ligand, a disease receptor targeting ligand, amifostine, angiostatin, monoclonal antibody C225, monoclonal antibody CD31, monoclonal antibody CD40, capecitabine, COX-2, deoxycytidine, fullerene, herceptin, human serum albumin, lactose, leuteinizing hormone, pyridoxal, quinazoline, thalidomide, transferrin, or trimethyl lysine. The present invention also pertains to kits employing the compounds of interest, and methods of assessing the pharmacology of an agent of interest using the present compounds.
摘要翻译：本发明在一般意义上提供了使用与靶向配体缀合的N 2 S 2螯合物的化合物的新标记策略，其中靶向配体是疾病细胞周期靶向化合物，肿瘤血管生成靶向配体，肿瘤凋亡靶向配体，疾病受体靶向配体，氨磷汀，血管抑素，单克隆抗体C225，单克隆抗体CD31，单克隆抗体CD40，卡培他滨，COX-2，脱氧胞苷，富勒烯，赫赛汀，人血清白蛋白，乳糖，促黄体激素，吡哆醛，喹唑啉，沙利度胺，，或三甲基赖氨酸。本发明还涉及使用目的化合物的试剂盒，以及使用本发明化合物评价感兴趣剂的药理学的方法。

4. 发明申请

US20040102311A1 Bridged metallocene catalyst component, method of making, polyolefin catalyst having C1, C2, or Cs symmetry, methods of making, methods of polymerizing, olefins and products made thereof 审中-公开
标题翻译：桥接金属茂催化剂组分，制备方法，具有C1，C2或Cs对称性的聚烯烃催化剂，制备方法，聚合方法，烯烃和由其制成的产物
公开(公告)号：US20040102311A1
公开(公告)日：2004-05-27
申请号：US10301884
申请日：2002-11-21
发明人： Abbas Razavi , Margarito Lopez , Didier Baekelmans
IPC分类号： B01J031/00 , C07F005/00 , C07F017/02
CPC分类号： B01J31/1815 , B01J23/74 , B01J31/1845 , B01J31/2204 , B01J2531/0258 , B01J2531/84 , B01J2531/842 , C07F15/025 , C07F15/065 , C07F17/00 , C08F10/00 , C08F4/80 , C08F4/7042
摘要： Bridged metallocene catalyst component in which a bridge spans two cyclopentadienyl groups, which Cp groups are attached to same or different heteroatoms of the bridge, which heteroatoms are also bonded to the metal. A catalyst systems is made by contacting the bridged component with a cocatalyst. Polymerization of olefins in catalyzed by the system.
摘要翻译：桥接茂金属催化剂组分，其中桥跨过两个环戊二烯基，其Cp基团连接到桥的相同或不同的杂原子，该杂原子也与金属键合。通过使桥连组分与助催化剂接触来制备催化剂体系。由系统催化的烯烃聚合。

5. 发明申请

US20040086460A1 Novel bifunctional chelating compounds containing hydroxamic acid residues 失效
标题翻译：含有异羟肟酸残基的新型双功能螯合化合物
公开(公告)号：US20040086460A1
公开(公告)日：2004-05-06
申请号：US10634335
申请日：2003-08-04
发明人： Jean-Marc DuFour
IPC分类号： A61K049/00 , C07F005/00 , C07C331/20 , C07C259/06
CPC分类号： C07C259/06 , C07F7/1804
摘要： New types of hydroxamic acid-based bifunctional chelators are provided. These chelators are designed to chelate metal ions that can be detected either by their paramagnetic or radioactive properties. Conjugation with peptides or protein can be achieved by the presence of a linker moiety in the molecular structure of these chelators.
摘要翻译：提供了新型异羟肟酸双功能螯合剂。这些螯合剂设计用于螯合可以通过其顺磁性或放射性检测的金属离子。可以通过在这些螯合剂的分子结构中存在连接体部分来实现与肽或蛋白质的缀合。

6. 发明申请

US20040067924A1 Actinium-225 complexes and conjugates for targeted radiotherapy 审中-公开
标题翻译：锕-225复合物和共轭物用于靶向放射治疗
公开(公告)号：US20040067924A1
公开(公告)日：2004-04-08
申请号：US10664670
申请日：2003-09-18
发明人： R. Keith Frank , Jaime Simon , Garry E. Kiefer
IPC分类号： C07F005/00 , A61K031/555 , A61K051/00
CPC分类号： A61K51/0497 , A61K51/0482
摘要： 225Ac complexes comprising a functionalized polyazamacrocyclic chelant compound of the formula I hereinbelow: 1 G is independently hydrogen or 2 each Q is independently hydrogen, (CHR5)pCO2R or (CHR5)pPO3R6R7 or 3 Q1 is hydrogen, (CHR5)wCO2R or (CHR5)wPO3R6R7; each R is independently hydrogen, benzyl or C1-C4 alkyl; R6 and R7 are independently H, C1-C6 alkyl or (C1-C2 alkyl)phenyl; each R5 is independently hydrogen; C1-C4 alkyl or (C1-C2 alkyl)phenyl; with the proviso that at least two of the sum of Q and Q1 must be other than hydrogen; A is CH, N, CnullBr, CnullCl, CnullSO3H, CnullOR8, CnullOR9NnullnullR10Xnull, or 4 Z and Z1 independently are CH, N, CnullSO3H, NnullnullR10Xnull, CnullCH2nullOR8 or CnullC(O)nullR11; R8 is H, C1-C5 alkyl, benzyl, or benzyl substituted with at least one R12; R9 is C1-C16 alkylamino; R10 is C1-C16 alkyl, benzyl, or benzyl substituted with at least one R12; R11 is nullOnull(C1-C3 alkyl), OH or NHR13; R12 is H, NO2, NH2, isothiocyanato, semicarbazido, thiosemicarbazido, maleimido, bromoacetamido or carboxyl; R13 is C1-C5 alkyl; X and Y are each independently hydrogen or may be taken with an adjacent X and Y to form an additional carbon-carbon bond; n is 0 or 1; m is an integer from 0 to 10 inclusive; p is 1 or 2; r is 0 or 1; w is 0 or 1; with the proviso that n is only 1 when X and/or Y form an additional carbon-carbon bond, and the sum of r and w is 0 or 1; L is a linker/spacer group covalently bonded to, and replaces one hydrogen atom of one of the carbon atoms to which it is joined, said linker/spacer group being represented by the formula 5 nullwherein: s is an integer of 0 or 1; t is an integer of 0 to 20 inclusive; R1 is H or an electrophilic or nucleophilic moiety which allows for covalent attachment to a biological carrier, or synthetic linker which can be attached to a biological carrier, or precursor thereof; and Cyc represents a cyclic aliphatic moiety, aromatic moiety, aliphatic heterocyclic moiety, or aromatic heterocyclic moiety, each of said moieties optionally substituted with one or more groups which do not interfere with binding to a biological carrier; with the proviso that when R1 is H, the linkage to the biological carrier is through one of Q or Q1; and with the proviso that when R1 is other than H, at least one of Q and Q1 must be (CHR5)pPO3R6R7; and with further proviso that when Q is (CHR5)pCO2R, Q1 is (CHR5)wCO2R, R is H, R5 is H, and R1 is H, then the sum of m, n, p, r, s, t, and w is greater than 1; or pharmaceutically acceptable salts thereof; complexed with 225Ac
摘要翻译：包含下文式I的官能化的多氮杂环丁基螯合剂的Ac络合物：G独立地为氢或每个Q独立地为氢，（CHR 5）p CO 2 R或（CHR 5）p PO 3 R 6 R 7 或Q 1是氢，（CHR 5）w CO 2 R或（CHR 5）w PO 3 R 6 R 7; 每个R独立地是氢，苄基或C 1 -C 4烷基; R 6和R 7独立地为H，C 1 -C 6烷基或（C 1 -C 2烷基）苯基; 每个R 5独立地是氢; C 1 -C 4烷基或（C 1 -C 2烷基）苯基; 条件是Q和Q 1之和中的至少两个必须不是氢; A是CH，N，C-Br，C-Cl，C-SO 3 H，C-OR 8，C-OR 9，N + R 10 X或Z和Z' 独立地是CH，N，C-SO 3 H，N + -R 10， - C-CH 2 - 或8或CC（O）-R 11; R 8是H，C 1 -C 5烷基，苄基或被至少一个R 12取代的苄基; R 9是C 1 -C 16烷基氨基; R 10是被至少一个R 12取代的C 1 -C 16烷基，苄基或苄基; R 11是-O-（C 1 -C 3烷基），OH或NHR 13; R 12是H，NO 2，NH 2

7. 发明申请

US20040067199A1 Aminoderivatives of biotin and their conjugates with macrocyclic chelating agents 有权
标题翻译：生物素的氨基衍生物及其与大环螯合剂的缀合物
公开(公告)号：US20040067199A1
公开(公告)日：2004-04-08
申请号：US10468075
申请日：2003-09-30
发明人： Giovanni Paganelli , Marco Chinol , Mauro Ginanneschi
IPC分类号： A61K049/00 , G01N033/53 , C07F005/00
CPC分类号： A61K51/0497
摘要： Formula (I) compounds are described where the groups are as defined here below, processes for their preparation, and their uses for the preparation of conjugates with radionuclides for use in human and animal therapy and diagnostics, particularly for the diagnosis and therapy of pathological conditions such as tumours. 1
摘要翻译：描述了式（I）化合物，其中基团如下文所定义，其制备方法及其用于制备用于人和动物治疗和诊断的放射性核素的缀合物的用途，特别是用于诊断和治疗病理状况如肿瘤。

8. 发明申请

US20040054151A1 Endohedral metallofullerene derivatives 有权
标题翻译：内含金属富勒烯衍生物
公开(公告)号：US20040054151A1
公开(公告)日：2004-03-18
申请号：US10244747
申请日：2002-09-17
发明人： Harry C. Dorn , Erick B. Iezzi , James Duchamp
IPC分类号： C07F005/00
CPC分类号： C07F5/003
摘要： Trimetallic nitride endohedral metallofullerene derivatives and their preparation are described. The trimetallic nitride endohedral metallofullerene derivatives have the general formula A3-nXnnullCm(R) where n ranges from 0 to 3, A and X may be trivalent metals and may be either rare earth metal or group IIIB metals, m is between about 60 and about 200, and R is preferably an organic group. Derivatives where the R group forms cyclized derivatives with the fullerene cage are also described.
摘要翻译：描述了三金属氮化物内嵌金属富勒烯衍生物及其制备方法。三金属氮化物内嵌金属富勒烯衍生物具有通式A3-nXn @ Cm（R）其中n的范围为0至3，A和X可以是三价金属，并且可以是稀土金属或IIIB族金属，m在约60 约200，R优选为有机基团。还描述了R基团与富勒烯笼形成环化衍生物的衍生物。

9. 发明申请

US20030232017A1 Cascade polymer bound complexing compounds, their complexes and conjugates, processes for their production, and pharmaceutical agents containing them 失效
标题翻译：级联聚合物结合的络合化合物，其络合物和共轭物，其生产方法和含有它们的药剂
公开(公告)号：US20030232017A1
公开(公告)日：2003-12-18
申请号：US10316094
申请日：2002-12-11
发明人： Johannes Platzek , Heribert Schmitt-Willich , Heinz Gries , Gabriele Schuhmann-Giampieri , Hubert Vogler , Hanns-Joachim Weinmann , Hans Bauer
IPC分类号： A61K049/04 , C08G002/00 , C07F005/00
CPC分类号： C08G85/00 , A61K49/0002 , A61K49/04 , A61K49/06 , A61K49/085 , A61K49/124 , A61K51/04 , A61K51/065 , C08G83/003 , Y10S514/836 , Y10T436/24
摘要： Cascade polymers, containing complex-forming ligands, optionally at least five ions of an element of atomic numbers 21-29, 39, 42, 44 or 57-83, as well as, if desired, cations of inorganic and/or organic bases, amino acids or amino acid amides, are valuable complexing compounds and complexes for diagnostics and therapy.
摘要翻译：含有复合物形成配体的级联聚合物，任选地是原子序数21-29,39,42,44或57-83的元素的至少五个离子，以及如果需要的话，无机和/或有机碱的阳离子，氨基酸或氨基酸酰胺，是诊断和治疗的有价值的复合化合物和复合物。

10. 发明申请

US20030215386A1 Stereoisomers of fatty acid analogs for diagnostic imaging 失效
标题翻译：用于诊断成像的脂肪酸类似物的立体异构体
公开(公告)号：US20030215386A1
公开(公告)日：2003-11-20
申请号：US10429416
申请日：2003-05-05
申请人： Biostream
发明人： David R. Elmalch
IPC分类号： A61K051/00 , C07F005/00 , C07F013/00
CPC分类号： A61K51/0497 , A61K51/04 , A61K51/0402 , A61K2123/00
摘要： The present invention provides novel imaging agents for clinical diagnosis of injuries and diseases, in the form of a radionuclide in spatial proximity to a substantially pure stereoisomer of a fatty acid analog. The invention also provides methods for using the novel imaging agents, and kits containing one or more of the novel imaging agents of the invention.
摘要翻译：本发明提供用于临床诊断损伤和疾病的新型成像剂，其形式为空间接近脂肪酸类似物的基本上纯的立体异构体的放射性核素。本发明还提供了使用新型成像剂的方法，以及含有本发明的一种或多种新型成像剂的试剂盒。

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