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1. 发明申请

WO2006006933A2 NEW COMPOSITIONS 审中-公开
标题翻译：新组合
公开(公告)号：WO2006006933A2
公开(公告)日：2006-01-19
申请号：PCT/SE2005/001152
申请日：2005-07-14
申请人： GLUCOGENE MEDICAL HFM AB , ELLERVIK, Ulf , FRANSSON, Lars-Åke , BELTING, Mattias, Nils, Henry , MANI, Katrin
发明人： ELLERVIK, Ulf , FRANSSON, Lars-Åke , BELTING, Mattias, Nils, Henry , MANI, Katrin
IPC分类号： A61K31/7028 , A61K45/06 , C07H20060101
CPC分类号： A61K45/06 , A61K31/7028 , A61K2300/00
摘要： The invention relates to the use of compounds for the preparation of a pharmaceutical composition comprising a) at least one compound having the general formula I: wherein R1 groups are same or different and independently selected from N-Y1Y2 or O-Y; Y, Y1 and Y2 are independently selected from H, alkyl, C(O)aryl, CH2aryl, C(O)alkyl, C(O)Oalkyl, C(O)Oalkenyl, where the alkyl and alkenyl groups have 1-100 carbon atoms and the aryl group has 6-100 carbon atoms; the C(O)Oalkyl and C(O)Oalkenyl includes preferentially all acyls from acetyl (2 carbon atoms) to eicosatetranoyl (20 carbon atoms) with or without single or multiple double bonds in all positions, or R2 is or R2 is A is O, S, NH or CH2; B is selected from naphthyl, naphthylalkyl, anthracenyl, antracenylalkyl or biphenyl, substituted with one or more substituents that are independently selected from F, Cl, Br, I, NO2, CF3, COOH, N-Y1Y2 or O-Y; Y, Y1 and Y2 are independently selected from H, alkyl, C(O)aryl, CH2aryl, C(O)alkyl, C(O)Oalkyl, where the alkyl group has 1-100 carbon atoms and the aryl group has 6-100 carbon atoms; and pharmaceutically acceptable salts thereof, in combination with b) non-xylose compounds chosen from at least one polyamine synthesis inhibitor; and at least one nitric oxide donor or stimulator of nitric oxide synthesis or inducer of nitric oxide release from S-nitrosothiols; and optionally also at least at least one anti-tumor agent selected from the group consisting growth factor-receptor interaction inhibitor or heparanase inhibitor and/or cholesterol traffic inhibitors and/or from the group of inducer of epoxygenase and/or inhibitor of topoisomerase and/or cyanide-donor and/or selene-containing compounds; said combinations of compound(s) a) and agents b) being selected such that a synergistic cytotoxisk proliferative effect is accomplished. Some of the compounds with formula (I) are new and the invention also relates to the new compounds as such and compositions comprising them.
摘要翻译：本发明涉及化合物用于制备药物组合物的用途，其包含a）至少一种具有通式I的化合物：其中R1基团相同或不同并且独立地选自N-Y1Y2或O-Y; Y，Y 1和Y 2独立地选自H，烷基，C（O）芳基，CH 2芳基，C（O）烷基，C（O）O烷基，C（O）O链烯基，其中烷基和烯基具有1-100碳原子和芳基具有6-100个碳原子; C（O）O烷基和C（O）O链烯基优先包括在所有位置具有或不具有单个或多个双键的乙酰基（2个碳原子）至二十碳四烯酰基（20个碳原子）的所有酰基，或者R2是或R2是A是 O，S，NH或CH 2; B选自由一个或多个独立地选自F，Cl，Br，I，NO 2，CF 3，COOH，N-Y 1 Y 2或O-Y的取代基取代的萘基，萘基烷基，蒽基，蒽基烷基或联苯基; Y，Y 1和Y 2独立地选自H，烷基，C（O）芳基，CH 2芳基，C（O）烷基，C（O）O烷基，其中烷基具有1-100个碳原子， 100个碳原子; 和b）非木糖化合物的组合，所述非木糖化合物选自至少一种多胺合成抑制剂; 和至少一种一氧化氮供体或一氧化氮合成的刺激剂或一氧化氮从S-亚硝基硫醇中释放的诱导剂; 和任选地至少一种选自生长因子 - 受体相互作用抑制剂或乙酰肝素酶抑制剂和/或胆固醇交通抑制剂和/或来自环氧化酶诱导剂和/或拓扑异构酶抑制剂的组的至少一种抗肿瘤剂和/ 或氰化物供体和/或含烯内酯的化合物; 化合物a）和试剂b）的组合被选择为使得可以实现协同细胞毒素增殖作用。一些具有式（I）的化合物是新的，本发明还涉及新的化合物，以及包含它们的组合物。

2. 发明申请

WO2005108411A3 SUBSTITUTED PIXYL PROTECTING GROUPS FOR OLIGONUCLEOTIDE SYNTHESIS 审中-公开
标题翻译：用于寡核苷酸合成的取代的PIXYL保护组
公开(公告)号：WO2005108411A3
公开(公告)日：2006-01-19
申请号：PCT/US2005015240
申请日：2005-05-03
申请人： ISIS PHARMACEUTICALS INC , GRIFFEY RICHARD H , ROSS BRUCE S , QUANLAI SONG
发明人： GRIFFEY RICHARD H , ROSS BRUCE S , QUANLAI SONG
IPC分类号： C07H20060101 , C07H19/06 , C07H21/00 , C07H19/16
CPC分类号： C07H19/06 , C07H21/00 , Y02P20/55
摘要： The present invention is directed to amidites useful in the synthesis of oligonucleotides comprising at least one RN moiety, and to methods of using such amidites in the synthesis of such oligonucleotides. The inventive amidites possess surprising coupling efficiency as compared to prior art amidites, while providing convenient intermediates in the synthesis of oligonucleotides possessing at least one free 2'-OH moiety.
摘要翻译：本发明涉及可用于合成包含至少一个RN部分的寡核苷酸的脒基，以及在合成这些寡核苷酸时使用这种脒基的方法。与现有技术的脒基相比，本发明的脒基具有惊人的偶联效率，同时在合成具有至少一个游离2'-OH部分的寡核苷酸的合成中提供方便的中间体。

3. 发明申请

WO2005056570A9 PRODUCTION OF AMINO SUGARS 审中-公开
标题翻译：生产氨基糖
公开(公告)号：WO2005056570A9
公开(公告)日：2005-12-22
申请号：PCT/US2004041006
申请日：2004-12-08
申请人： CARGILL INC , MCFARLAN SARA C , SCHROEDER WILLIAM A , FOSDICK LAWRENCE E , BOHLMANN JOHN A
发明人： MCFARLAN SARA C , SCHROEDER WILLIAM A , FOSDICK LAWRENCE E , BOHLMANN JOHN A
IPC分类号： C07H20060101 , C12N1/18 , C12P19/28 , C07H
CPC分类号： C12P19/28 , C12N1/18
摘要： The present invention provides a method for producing an amino sugar selected from the group consisting of N-acetylglucosamine, glucosamine, or a combination thereof. The method comprises culturing a yeast in a culture medium and recovering N-acetylglucosamine, glucosamine, or a combination thereof, wherein the yeast comprises an exogenous nucleic acid sequence encoding glucosamine-6-phosphate synthase operably linked to a promoter. The invention also provides a genetically modified yeast that produces an amino sugar selected from the group consisting of N-acetylglucosamine, glucosamine, or a combination thereof.
摘要翻译：本发明提供了选自N-乙酰葡糖胺，葡糖胺或其组合的氨基糖的制备方法。该方法包括在培养基中培养酵母并回收N-乙酰氨基葡萄糖，葡糖胺或其组合，其中酵母包含可操作地连接于启动子的编码葡糖胺-6-磷酸合成酶的外源核酸序列。本发明还提供一种经遗传修饰的酵母，其产生选自N-乙酰葡糖胺，葡糖胺或其组合的氨基糖。

4. 发明申请

WO2005012318A3 SUBSTITUTED FUSED HETEROCYCLIC C-GLYCOSIDES 审中-公开
标题翻译：取代的FUSED杂环C型糖苷
公开(公告)号：WO2005012318A3
公开(公告)日：2005-12-15
申请号：PCT/US2004024625
申请日：2004-07-30
申请人： JANSSEN PHARMACEUTICA NV , TANABE SEIYAKU CO , RYBCZYNSKI PHILIP , URBANSKI MAUD , ZHANG XIAOYAN
发明人： RYBCZYNSKI PHILIP , URBANSKI MAUD , ZHANG XIAOYAN
IPC分类号： A01N43/04 , A61K31/70 , A61K31/7052 , C07H20060101 , C07H1/00 , C07H5/04 , C07H5/06 , C07H7/06 , C07H17/02
CPC分类号： C07H7/06 , Y10S514/866 , Y10S514/909
摘要： This invention relates to substituted fused heterocyclic C-glycosides, compositions containing them, and methods of using them, for example, for the treatment or prophylaxis of diabetes and Syndrome X.
摘要翻译：本发明涉及取代的稠合杂环C糖苷，含有它们的组合物，以及使用它们的方法，例如用于治疗或预防糖尿病和综合征X.

5. 发明申请

WO2004099227A3 POLYOL FATTY ACID POLYESTERS PROCESS AND POLYURETHANES THEREFROM 审中-公开
标题翻译： POLYOL脂肪酸聚酯工艺和聚氨酯
公开(公告)号：WO2004099227A3
公开(公告)日：2005-11-10
申请号：PCT/US2004013244
申请日：2004-04-29
申请人： UNIV MICHIGAN STATE
发明人： DWAN ISA JEAN-PIERRE L , DRZAL LAWRENCE T , MOHANTY AMAR K , MISRA MANJUSRI
IPC分类号： C07C51/43 , C07H20060101 , C07H1/00 , C08G18/36 , C11C1/00
CPC分类号： C08G18/7664 , C08G18/36 , C08G2101/00
摘要： A solvent-free process for making a polyol fatty acid polyester composition useful for preparation of polyurethanes is described. These compositions are preferably made by reaction of a natural oil (from plant or animal) with a multi-functional hydroxyl compound derived from a natural source, such as sorbitol, in presence of an alkali metal salt or base such as potassium hydroxide as a catalyst which also acts to saponify the reaction mixture. The hydroxyl content of the prepared composition depends on the amount of the multi-functional hydroxyl compound used in the preparation. In another embodiment, the hydroxyl groups of these compositions are reacted with an isocyanate, such as the polymeric diphenylmethane diisocyanate (also known as 4,4'-diphenyl methane diisocyanate, or MDI) to form polyurethanes in a conventional manner.
摘要翻译：描述了制备用于制备聚氨酯的多元醇脂肪酸聚酯组合物的无溶剂方法。这些组合物优选通过天然油（来自植物或动物）与衍生自天然来源的多官能羟基化合物如山梨糖醇在碱金属盐或碱如氢氧化钾作为催化剂的存在下反应来制备其还用于皂化反应混合物。制备的组合物的羟基含量取决于制剂中使用的多官能羟基化合物的量。在另一个实施方案中，这些组合物的羟基与异氰酸酯如聚合二苯基甲烷二异氰酸酯（也称为4,4'-二苯基甲烷二异氰酸酯或MDI）反应，以常规方式形成聚氨酯。

6. 发明申请

WO2005021563A3 METHOD AND MATERIALS FOR BISULFITE CONVERSION OF CYTOSINE TO URACIL 审中-公开
标题翻译：细胞色素转化为尿素的方法和材料
公开(公告)号：WO2005021563A3
公开(公告)日：2005-06-09
申请号：PCT/US2004027992
申请日：2004-08-27
申请人： APPLERA CORP , BOYD VICTORIA L , ZON GERALD
发明人： BOYD VICTORIA L , ZON GERALD
IPC分类号： C07H20060101 , C07H21/02 , C07H21/04 , C12Q1/68
CPC分类号： C07H21/02 , C07H21/04 , C12Q1/6886 , C12Q2600/154 , Y10S435/81 , Y10S436/808
摘要： The invention provides methods and materials for conversion of cytosine to uracil. In some embodiments, a nucleic acid, such as gDNA, is reacted with at least one bisulfite salt having the formula X HS03 or Y (HS03 )2; wherein X is ammonium ion, a tetraalkyl ammonium ion, or a group 1 A ion other than sodium; and Y is a group 2A ion or a group 7B ion; under conditions effective to convert at least one cytosine nucleobase to a uracil nucleobase. In some embodiments, X comprises at least one of lithium ion, potassium ion, ammonium ion, tetraalkylammoniurn ion, magnesium ion, manganese ion and calcium ion. In some embodiments, the reacting is performed optionally in the presence of a polyamine catalyst and/or a quaternary amine catalyst. Also provided are kits that can be used to carry out methods of the invention.
摘要翻译：本发明提供了将胞嘧啶转化成尿嘧啶的方法和材料。在一些实施方案中，核酸如gDNA与至少一种具有式X + HSO 3 - 或Y +2（HSO 3 - ）2的亚硫酸氢盐反应; 其中X +是铵离子，四烷基铵离子或除钠以外的1AA族离子; Y +2为2A族离子或7B族离子; 在有效将至少一个胞嘧啶核碱基转化为尿嘧啶核碱基的条件下。在一些实施方案中，X +包括锂离子，钾离子，铵离子，四烷基铵离子，镁离子，锰离子和钙离子中的至少一种。在一些实施方案中，反应任选在多胺催化剂和/或季胺催化剂的存在下进行。还提供了可用于实施本发明方法的试剂盒。

7. 发明申请

WO2004063209A3 METHODS OF PRODUCING C-ARYL GLUCOSIDE SGLT2 INHIBITORS 审中-公开
标题翻译：生产C-ARYL GLUCOSIDE SGLT2抑制剂的方法
公开(公告)号：WO2004063209A3
公开(公告)日：2005-05-12
申请号：PCT/US0341373
申请日：2003-12-23
申请人： SQUIBB BRISTOL MYERS CO , DESHPANDE PRASHANT P , ELLSWORTH BRUCE A , SINGH JANAK , LAI CHIAJEN , CRISPINO GERARD , RANDAZZO MICHAEL E , GOUGOUTAS JACK Z , DENZEL THEODOR W
发明人： DESHPANDE PRASHANT P , ELLSWORTH BRUCE A , SINGH JANAK , LAI CHIAJEN , CRISPINO GERARD , RANDAZZO MICHAEL E , GOUGOUTAS JACK Z , DENZEL THEODOR W
IPC分类号： C07G3/00 , C07H20060101 , C07H1/00 , C07H5/04 , C07H5/06 , C07H7/00 , C08B37/00
CPC分类号： C07H23/00 , C07H5/04 , C07H5/06 , C07H7/00 , C07H15/207
摘要： Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.
摘要翻译：生产用于治疗糖尿病和相关疾病的C-芳基葡萄糖苷SGLT2抑制剂的方法。及其中间体。 C-芳基葡糖苷可以与形成氨基酸复合物的试剂络合。

8. 发明申请

WO2004043978A3 2'-METHOXY SUBSTITUTED OLIGOMERIC COMPOUNDS AND COMPOSITIONS FOR USE IN GENE MODULATIONS 审中-公开
标题翻译：用于基因调控的2'-甲氧基取代的低聚物和组合物
公开(公告)号：WO2004043978A3
公开(公告)日：2005-04-07
申请号：PCT/US0334906
申请日：2003-11-04
申请人： ISIS PHARMACEUTICALS INC , BAKER BRENDA F , ELDRUP ANN B , MANOHARAN MUTHIAH , BHAT BALKRISHEN , GRIFFEY RICHARD , SWAYZE ERIC E , CROOKE STANLEY T
发明人： BAKER BRENDA F , ELDRUP ANN B , MANOHARAN MUTHIAH , BHAT BALKRISHEN , GRIFFEY RICHARD , SWAYZE ERIC E , CROOKE STANLEY T
IPC分类号： A01N43/04 , A61K48/00 , C07H20060101 , C07H21/00 , C07H21/02 , C07H21/04 , C12N20060101 , C12N15/113 , C12P19/34 , C12Q1/68
CPC分类号： C12N15/1135 , C07H21/00 , C07H21/02 , C07H21/04 , C12N15/1137 , C12N2310/11 , C12N2310/14 , C12N2310/315 , C12N2310/321 , C12N2310/322 , C12N2310/341 , C12N2310/345 , C12N2310/346 , C12N2310/53 , C12N2310/3521
摘要： Compositions comprising first and second oligomers are provided wherein at least a portion of the first oligomer is capable of hybridizing with at least a portion of the second oligomer, at least a portion of the first oligomer is complementary to and capable of hybridizing to a selected target nucleic acid, and at least one of the first or second oligomers includes a modified sugar and/or backbone modification. In some embodiments the modification is a 2'-OCH3 substituent group on a sugar moiety. Oligomer/protein compositions are also provided comprising an oligomer complementary to and capable of hybridizing to a selected target nucleic acid and at least one protein comprising at least a portion of an RNA-induced silencing complex (RISC), wherein at least one nucleotide of the oligomer has a modified sugar and/or backbone modification.
摘要翻译：提供包含第一和第二寡聚体的组合物，其中至少一部分第一寡聚体能够与至少一部分第二寡聚物杂交，至少一部分第一寡聚体与所选择的靶互补并且能够与选定的靶核酸，并且第一或第二寡聚体中的至少一种包括修饰的糖和/或骨架修饰。在一些实施方案中，修饰是糖部分上的2'-OCH 3取代基。还提供低聚物/蛋白质组合物，其包含与选定的靶核酸互补并且能够与选定的靶核酸杂交的寡聚体和至少一种包含至少一部分RNA诱导的沉默复合物（RISC）的蛋白质，其中至少一个核苷酸低聚物具有修饰的糖和/或骨架修饰。

9. 发明申请

WO2005007663A2 FLUOROGENIC ENZYME SUBSTRATES AND USES THEREOF 审中-公开
公开(公告)号：WO2005007663A2
公开(公告)日：2005-01-27
申请号：PCT/US2004022776
申请日：2004-07-14
申请人： IRM LLC , HARRIS JENNIFER L , DAMOISEAUX ROBERT , BACKES BRADLEY J , WINSSINGER NICOLAS
发明人： HARRIS JENNIFER L , DAMOISEAUX ROBERT , BACKES BRADLEY J , WINSSINGER NICOLAS
IPC分类号： C07H20060101 , C07H21/00 , C07H21/02 , C07H21/04 , C07K14/47 , C12Q1/68 , C07H
CPC分类号： C07H21/00 , C07H21/02 , C07H21/04
摘要： The present invention provides, inter alia, fluorogenic enzyme substrates, such as fluorogenic polypeptide substrates, libraries of fluorogenic enzyme substrates and methods for assaying for enzymatically active enzymes, such as hydrolases (e.g., proteases), in biological samples.

10. 发明申请

WO0190118A3 HAPLOTYPES OF THE EDN2 GENE 审中-公开
标题翻译： EDN2基因的快乐
公开(公告)号：WO0190118A3
公开(公告)日：2003-10-30
申请号：PCT/US0116433
申请日：2001-05-21
申请人： GENAISSANCE PHARMACEUTICALS , KAZEMI AMIR , KOSHY BEENA , TANGUAY DEBRA A
发明人： KAZEMI AMIR , KOSHY BEENA , TANGUAY DEBRA A
IPC分类号： C07H20060101 , C12Q1/68 , G06F19/18
CPC分类号： C12Q1/6883 , C12Q2600/156 , C12Q2600/172 , G06F19/18
摘要： Novel genetic variants of the Endothelin 2 (EDN2) gene are described. Various genotypes, haplotypes, and haplotype pairs that exist in the general United States population are disclosed for the EDN2 gene. Compositions and methods for haplotyping and/or genotyping the EDN2 gene in an individual are also disclosed. Polynucleotides defined by the sequence the haplotypes disclosed herein are also described.
摘要翻译：描述了内皮素2（EDN2）基因的新型遗传变体。对于EDN2基因，公开了存在于美国一般群体中的各种基因型，单元型和单倍型对。还公开了个体中单倍体和/或基因分型EDN2基因的组合物和方法。还描述了由本文公开的单倍型序列定义的多核苷酸。

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