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1. 发明申请

WO1993021957A1 COMPLEXING AGENTS AND TARGETING IMMUNOREAGENTS 审中-公开
标题翻译：复合药剂和靶向免疫接种
公开(公告)号：WO1993021957A1
公开(公告)日：1993-11-11
申请号：PCT/US1992003858
申请日：1992-05-07
申请人： STERLING WINTHROP INC.
发明人： STERLING WINTHROP INC. , TONER, John, L. , HILBORN, David, A. , MURRAY, Bruce, J. , HOUSSAIN, Timothy, Z. , SNOW, Robert, A. , SAHA, Ashis, K. , PHILION, Richard , SHEARMAN, Clyde, W. , SHAH, Chandra
IPC分类号： A61K47/48
CPC分类号： C07D213/40 , A61K47/6887 , A61K49/0002 , A61K49/0019 , A61K49/0058 , A61K51/10 , A61K51/1093 , A61K2121/00 , C07D213/36 , C07D213/38 , C07D213/42 , C07D471/04 , C07D471/08
摘要： A targeting radioactive immunoreagent comprises a metal radionuclide ion, a complexing agent, and an immunoreactive group covalently bonded to said complexing agent, the complexing agent having the structure (AI), wherein R represents hydrogen, alkyl, alkoxy, alkylthio, alkylamino, alkylformamido, aryl, aryloxy, heterocyclyl or a protein reactive group; R represents hydrogen, alkyl, alkoxy, alkylthio, alkylamino, alkylformamido, aryl, aryloxy, heterocyclyl or a protein reactive group; R represents hydroxy, carboxy, hydroxyalkyl, thioalkyl, formyl, carbonyliminodiacetic acid, methyleneiminodiacetic acid, methylenethioethyleneiminodiacetic acid, carboxyalkylthioalkyl, hydrazinylidenediacetic acid, or a salt of such acids, or two R groups, taken together, represent the atoms necessary to complete a macrocyclic ring structure containing at least one heteroatom coordinating site and at least one, preferably two alkylene groups forming part of the ring structure; R represents hydrogen, alkyl, alkoxy, alkylthio, alkylamino, alkylformamido, aryl, aryloxy, heterocyclyl or a protein reactive group; R represents hydrogen or a protein reactive group; n is 0 to 4; o is 0 or 1; m is 0 or 1; provided that at least one of n and m is 0 and at least one of R, R , R and R is a protein reactive group. In another aspect, this invention provides novel terpyridines, quaterpyridines, quinqepyridines, sexipyridines and phenanthrolines having the structure (AI). Preferred terpyridines have the structure (AI) above wherein n=1, o=1, m=0, and R is a protein reactive group or a phenyl substituted with a protein reactive group. Optionally, the phenyl may also contain one or more substituents selected from alkyl and alkoxy. Preferred phenanthrolines have the structure (AI) above wherein n=0, o=1, m=1 and at least one R is a protein reactive group. The targeting radioactive immunoreagents are particularly useful in therapeutic and diagnostic imaging compositions and methods.
摘要翻译：靶向放射免疫试剂包含金属放射性核素离子，络合剂和与所述络合剂共价结合的免疫反应性基团，具有结构（AI）的络合剂，其中R表示氢，烷基，烷氧基，烷硫基，烷基氨基，烷基甲酰氨基，芳基，芳氧基，杂环基或蛋白质反应性基团; R 1表示氢，烷基，烷氧基，烷硫基，烷基氨基，烷基酰氨基，芳基，芳氧基，杂环基或蛋白质反应性基团; R 2表示羟基，羧基，羟基烷基，硫代烷基，甲酰基，羰基亚氨基二乙酸，亚甲基亚氨基二乙酸，亚甲基亚乙基亚氨基二乙酸，羧基烷硫基烷基，亚肼基二乙酸或这些酸的盐，或两个R 2基团一起表示原子必须完成包含至少一个杂原子配位部位和形成环结构部分的至少一个，优选两个亚烷基的大环环结构; R 3表示氢，烷基，烷氧基，烷硫基，烷基氨基，烷基酰氨基，芳基，芳氧基，杂环基或蛋白质反应性基团; R 4表示氢或蛋白质反应性基团; n为0〜4; o为0或1; m为0或1; 条件是n和m中的至少一个是0，R 1，R 3和R 4中的至少一个是蛋白质反应性基团。另一方面，本发明提供具有结构（AI）的新颖的三联嘧啶，季铵盐，喹吖啶，异吡啶和菲咯啉。优选的三联吡啶具有上述结构（AI），其中n = 1，o = 1，m = 0，R是蛋白质反应性基团或被蛋白质反应性基团取代的苯基。任选地，苯基还可以含有一个或多个选自烷基和烷氧基的取代基。优选的菲咯啉具有上述结构（AI），其中n = 0，o = 1，m = 1，并且至少一个R 4是蛋白质反应性基团。靶向放射免疫试剂在治疗和诊断成像组合物和方法中特别有用。

2. 发明申请

WO1996002261A1 USE OF MAGNESIUM HYDROXIDE AS A STOOL SOFTENER 审中-公开
标题翻译：使用氢氧化镁作为固体SOFTENER
公开(公告)号：WO1996002261A1
公开(公告)日：1996-02-01
申请号：PCT/US1995009166
申请日：1995-07-19
申请人： STERLING WINTHROP INC. , O'KEEFFE, Kenneth, J. , VANDENBROUCKE, Pol
发明人： STERLING WINTHROP INC.
IPC分类号： A61K33/08
CPC分类号： A61K33/08
摘要： Magnesium hydroxide, when used at subeffective laxative doses is an effective stool softener.
摘要翻译：氢氧化镁在有效的泻药剂量下使用是一种有效的大便软化剂。

3. 发明申请

WO1994022864A1 ACYCLIC NUCLEOSIDE ANALOGS AND OLIGONUCLEOTIDE SEQUENCES CONTAINING THEM 审中-公开
标题翻译： ACYCLIC核苷类似物和含有它们的寡核苷酸序列
公开(公告)号：WO1994022864A1
公开(公告)日：1994-10-13
申请号：PCT/US1994002995
申请日：1994-03-21
申请人： STERLING WINTHROP INC.
发明人： STERLING WINTHROP INC. , COOK, Philip, D. , DELECKI, Daniel, J. , GUINOSSO, Charles
IPC分类号： C07D473/34
CPC分类号： C12N15/113 , C07D473/18 , C07D473/34 , C07F9/65616 , C07H21/00
摘要： Compounds of formula (I) wherein R is hydrogen, or a blocking group that is compatible with oligonucleotide synthesis; R is hydrogen or methyl; R is hydrogen or -P(R )OR ; R is chlorine, 4-nitroimidazole, imidazole, tetrazole, triazole or di(lower-alkyl)amino-; R is methyl, 2-cyanoethyl or 2,2,2-trichloroethyl; n is from 0 to 2; X is oxygen, sulfur, or -NR ; R is hydrogen or lower alkyl; Q is chosen from the group consisting of (a) and (b); R is lower-alkyl; and R is hydrogen, benzoyl, anisoyl, or lower-alkyl carbonyl and its pharmaceutically acceptable addition salts are nucleotide analogs. Modified oligonucleotides containing the nucleoside analogs of formula (I) are stable to nuclease degradation and are useful in inhibiting gene expression, in sequencing, and in mutagenesis.
摘要翻译：其中R 1为氢的式（I）化合物或与寡核苷酸合成相容的封闭基团; R 2是氢或甲基; R 3是氢或-P（R 4）OR 5; R 4是氯，4-硝基咪唑，咪唑，四唑，三唑或二（低级 - 烷基）氨基 - ; R 5是甲基，2-氰基乙基或2,2,2-三氯乙基; n为0〜2; X是氧，硫或-NR 6; R 6是氢或低级烷基; Q选自（a）和（b）组成的组; R 7是低级烷基; R 8是氢，苯甲酰基，茴香酰基或低级烷基羰基，其药学上可接受的加成盐是核苷酸类似物。含有式（I）核苷类似物的修饰寡核苷酸对于核酸酶降解是稳定的，可用于抑制基因表达，测序和诱变。

4. 发明申请

WO1994020382A1 STOPPER FOR MEDICATION CONTAINER 审中-公开
标题翻译：药物容器的停止
公开(公告)号：WO1994020382A1
公开(公告)日：1994-09-15
申请号：PCT/US1994002275
申请日：1994-03-02
申请人： STERLING WINTHROP INC.
发明人： STERLING WINTHROP INC. , NIEDOSPIAL, John, J. , VACEK, Ronald, R. , DEJESUS, Rafael
IPC分类号： B65D51/00
CPC分类号： B65D51/002
摘要： In accordance with this invention, there is provided a closure arrangement for medication containers comprising an elastomeric stopper (14) comprising a tear-away member (22) which blocks a passageway (50) defining a conical luer taper and a cap (16) comprising means (30, 34) for engaging the tear-away member, whereby the engaged tear-away member can be readily torn away by a user by rotating the cap or by pulling the cap off the container in an axial direction. The closure arrangement reduces the risk of particulate contamination associated with stoppers adapted to be ruptured with a luer nozzle.
摘要翻译：根据本发明，提供了一种用于药物容器的封闭装置，其包括弹性止动器（14），该弹性止动件包括撕开构件（22），其阻挡限定圆锥形鲁尔锥形的通道（50）和帽（16），帽用于接合撕开构件的装置（30,34），由此通过旋转盖子或者沿着轴向将盖子从容器拉出来，用户可以容易地撕开接合的撕开构件。闭合装置减少了适于用鲁尔喷嘴破裂的塞子相关的颗粒污染的风险。

5. 发明申请

WO1992008494A2 TARGETING RADIOACTIVE IMMUNOREAGENTS 审中-公开
标题翻译：瞄准放射性免疫接种
公开(公告)号：WO1992008494A2
公开(公告)日：1992-05-29
申请号：PCT/US1991008253
申请日：1991-11-07
申请人： STERLING WINTHROP INC.
发明人： STERLING WINTHROP INC. , TONER, John, L. , HILBORN, David, A. , MURRAY, Bruce, J. , HOSSAIN, Timothy, Z.
IPC分类号： A61K47/48
CPC分类号： C07D213/53 , A61K47/56 , A61K47/6887 , A61K51/1054 , A61K51/1063 , A61K51/1093 , C07D213/61 , C07D213/77 , C07D471/04
摘要： A targeting radioactive immunoreagent comprises a metal radionuclide ion, a complexing agent, and an immunoreactive group covalently bonded to said complexing agent, the complexing agent having structure (A-I), wherein R represents hydrogen, alkyl, alkoxy, alkylthio, alkylamino, alkylformamido, aryl, aryloxy, heterocyclyl or a protein reactive group; R represents hydrogen, alkyl, alkoxy, alkylthio, alkylamino, alkylformamido, aryl, aryloxy, heterocyclyl or a protein reactive group; R represents hydroxy, carboxy, hydroxyalkyl, carbonyliminodiacetic acid, methyleneiminodiacetic acid, methylenethioethyleneiminodiacetic acid, hydrazinylylidenediacetic acid, or a salt of such acids, or two R groups, taken together, represent the atoms necessary to complete a macrocyclic ring structure containing at least one heteroatom coordinating site and at least one, preferably two alkylene groups forming part of the ring structure; R represents hydrogen, alkyl, alkoxy, alkylthio, alkylamino, alkylformamido, aryl, aryloxy, heterocyclyl or a protein reactive group; R represents hydrogen or a protein reactive group; n is 0 to 4, o is 0 or 1, m is 0 or 1; provided that at least one of n and m is 0 and at least one of R, R , R and R is a protein reactive group. In a composition of matter aspect, this invention provides novel terpyridines and phenanthrolines. Preferred terpyridines have the structure (A-I) above wherein n=1, m=0 and R is a substituted phenyl containing an alkyl or alkoxy substituent and a protein reactive group. Preferred phenanthrolines have the structure (A-I) above wherein n=0, m=1 and at least one R is a protein reactive group. The targeting radioactive immunoreagents are particularly useful in therapeutic and diagnostic imaging compositions and methods.
摘要翻译：靶向放射免疫试剂包含金属放射性核素离子，络合剂和与所述络合剂共价结合的免疫反应性基团，具有结构（AI）的络合剂，其中R表示氢，烷基，烷氧基，烷硫基，烷基氨基，烷基甲酰氨基，芳基，芳氧基，杂环基或蛋白质反应性基团; R 1表示氢，烷基，烷氧基，烷硫基，烷基氨基，烷基酰氨基，芳基，芳氧基，杂环基或蛋白质反应性基团; R 2表示羟基，羧基，羟基烷基，羰基亚氨基二乙酸，亚甲基亚氨基二乙酸，亚甲基亚乙基亚氨基二乙酸，肼基亚乙二基二乙酸或这些酸的盐，或两个R 2基团一起代表完成大环所必需的原子包含至少一个杂原子配位部位和至少一个，优选两个形成环结构部分的亚烷基的结构; R 3表示氢，烷基，烷氧基，烷硫基，烷基氨基，烷基酰氨基，芳基，芳氧基，杂环基或蛋白质反应性基团; R 4表示氢或蛋白质反应性基团; n为0〜4，o为0或1，m为0或1; 条件是n和m中的至少一个是0，R 1，R 3和R 4中的至少一个是蛋白质反应性基团。在物质组成方面，本发明提供了新颖的三联吡啶和菲咯啉。优选的三联吡啶具有上述结构（A-I），其中n = 1，m = 0，R为含有烷基或烷氧基取代基的取代苯基和蛋白质反应性基团。优选的菲咯啉具有上述结构（A-I），其中n = 0，m = 1，并且至少一个R 4是蛋白质反应性基团。靶向放射免疫试剂在治疗和诊断成像组合物和方法中特别有用。

6. 发明申请

WO1994025075A1 POLYMERIC X-RAY CONTRAST COMPOSITIONS CONTAINING IODINATED POLYMERIC BEADS 审中-公开
标题翻译：含有碘化聚合物珠的聚合X射线对比组合物
公开(公告)号：WO1994025075A1
公开(公告)日：1994-11-10
申请号：PCT/US1994003919
申请日：1994-04-12
申请人： STERLING WINTHROP INC.
发明人： STERLING WINTHROP INC. , ILLIG, Carl, R.
IPC分类号： A61K49/04
CPC分类号： A61K49/0461 , A61K49/0442 , B82Y5/00 , Y10S514/941 , Y10S514/942
摘要： Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a polymeric material in combination with a divalent cation capable of forming a coating on the gastrointestinal tract and iodinated polymeric, water-insoluble beads having a particle size of from about 0.01 to about 1000 mu wherein said iodinated polymeric beads comprise a polymer containing repeating units of formula (I) wherein A is a repeating organic unit in the backbone chain of the polymer; and X is an organic moiety containing or iodinated aromatic group and a hydrophilic group, said moiety having an iodine content within the range of from about 40 to about 80 weight percent based on the molecular weight of X, in a pharmaceutically acceptable carrier.
摘要翻译：公开了用于胃肠道口服或逆行检查的X射线造影剂组合物，其包含与能够在胃肠道上形成涂层的二价阳离子结合的聚合物材料和具有约 0.01至约1000μm，其中所述碘化聚合物珠粒包含含有式（I）重复单元的聚合物，其中A是聚合物主链中的重复有机单元; 并且X是含有或碘化芳族基团和亲水基团的有机部分，所述部分在药学上可接受的载体中，基于X的分子量，碘含量在约40至约80重量％的范围内。

7. 发明申请

WO1994013304A3 ANTACID COMPOSITION AND METHOD OF PRODUCTION 审中-公开
公开(公告)号：WO1994013304A3
公开(公告)日：1994-06-23
申请号：PCT/US1993011720
申请日：1993-12-03
申请人： STERLING WINTHROP INC.
发明人： STERLING WINTHROP INC. , LIVERSIDGE, Gary, G. , MCINTIRE, Gregory, L.
IPC分类号： A61K33/06

8. 发明申请

WO1994008624A2 THERAPEUTIC AND DIAGNOSTIC IMAGING COMPOSITIONS AND METHODS 审中-公开
标题翻译：治疗和诊断成像组合物和方法
公开(公告)号：WO1994008624A2
公开(公告)日：1994-04-28
申请号：PCT/US1993009645
申请日：1993-10-07
申请人： STERLING WINTHROP INC.
发明人： STERLING WINTHROP INC. , SNOW, Robert, A. , LADD, David, L. , TONER, John, L.
IPC分类号： A61K47/48
CPC分类号： A61K51/0497 , A61K47/59 , A61K47/595 , A61K47/60 , A61K2123/00
摘要： This invention provides therapeutic and diagnostic imaging compositions and methods featuring a polymer comprising units containing a poly(alkylene oxide) moiety linked to the residue of a chelating agent, said polymer having a cytotoxic agent associated therewith.
摘要翻译：本发明提供治疗和诊断成像组合物和方法，其特征在于包含含有与螯合剂残基连接的聚（环氧烷）部分的单元的聚合物，所述聚合物具有与其相关的细胞毒性剂。

9. 发明申请

WO1992007036A1 SELENOMEROCYANINE PHOTOSENSITIZERS 审中-公开
标题翻译：紫杉醇光敏剂
公开(公告)号：WO1992007036A1
公开(公告)日：1992-04-30
申请号：PCT/US1991007603
申请日：1991-10-16
申请人： STERLING WINTHROP INC.
发明人： STERLING WINTHROP INC. , GUNTHER, Wolfgang, H., H. , SEARLE, Roger
IPC分类号： C09B23/10
CPC分类号： C07D413/06 , A61L2/0011 , C07D417/06 , C09B23/10 , C12N7/00 , C12N2710/16063 , C12N2710/16663 , G03C1/22
摘要： Selenomerocyanines having structural formula (I) wherein X is O, S, Se, Te, C(CH3)2 or NR wherein R is methyl, ethyl, propyl, cyclopropyl, cyclohexyl, phenyl or phenyl substituted by from one to three of methyl, trifluoromethyl, methoxycarbonyl, ethoxycarbonyl, cyano, dimethylamino, methoxy, methylthio, fluoro, chloro, bromo, or iodo; Y is alkylene having from two to nine carbon atoms or alkylene having from two to nine carbon atoms interrupted by O, S, NR', CONH or phenylene wherein R' is methyl, ethyl or phenyl; Z1 and Z2 are independently H or alkyl having from one to ten carbon atoms; m is 0 or 1; n is 1, 2 or 3; M+ is a pharmaceutically or photographically acceptable cation; and Ar is a fused aromatic nucleus having from one to three carbocyclic or carbon-nitrogen heterocyclic rings and a process for preparation thereof, methods of use thereof as photosensitizers for generation of singlet oxygen, virus inactivation and cancer cell inactivation, and photosensitized silver halide photographic emulsions containing them are disclosed.

10. 发明申请

WO1994022892A1 7-DEAZAPURINE MODIFIED OLIGONUCLEOTIDES 审中-公开
公开(公告)号：WO1994022892A1
公开(公告)日：1994-10-13
申请号：PCT/US1994002996
申请日：1994-03-21
申请人： STERLING WINTHROP INC.
发明人： STERLING WINTHROP INC. , COOK, Phillip, D. , DELECKI, Daniel, J.
IPC分类号： C07H21/00
CPC分类号： C07H21/00
摘要： Oligonucleotides, which incorporate 7-deazanucleosides, are useful as antisense sequences to inhibit the function of RNA and DNA.
摘要翻译：含有7-脱氮核苷的寡核苷酸可用作抑制RNA和DNA功能的反义序列。

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