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31. 发明申请

US20080045598A1 Novel sulfonanilide analogs as selective aromatase modulators (SAMs) 失效
标题翻译：新型磺酰苯胺类似物作为选择性芳香酶调节剂（SAM）
公开(公告)号：US20080045598A1
公开(公告)日：2008-02-21
申请号：US11702276
申请日：2007-02-05
申请人： Robert Brueggemeier , Bin Su , Edgar Diaz-Cruz , Serena Landini
发明人： Robert Brueggemeier , Bin Su , Edgar Diaz-Cruz , Serena Landini
IPC分类号： A61K31/18 , A61K31/135 , A61P35/00 , C07C211/00 , C07C303/00
CPC分类号： C07C233/75 , C07C233/25 , C07C233/60 , C07C255/57 , C07C311/08 , C07C311/21 , C07C2601/08 , C07C2601/14
摘要： Compounds and methods suppressing aromatase activity expression in cancer cells. Provided are compounds are those of formula I: wherein R1 may be alkyl, cycloalkyl, haloalkyl, aryl, substituted aryl, haloaryl, alkoxy, alkylaryl, and arylalkyl; R2 is H, alkyl, aryl, alkylaryl, arylalkyl, and cycloalkyl; R3, with the base nitrogen, forms an amide or sulfonamide; R4 is selected from nitro, amine, amide, and benzamide; or a pharmaceutically acceptable salts thereof Also provided are small molecule selective aromatase inhibitors having a molecular weight of less 500 g/mol. In some embodiments, the small molecule selective aromatase inhibitors described herein have a molecular weight of less than 450 g/mol. Also provided are methods for suppressing aromatase activity expression in cancer cells comprising the step of administering a pharmaceutically effective amount of a small molecule aromatase inhibitor to a subject in need of such treatment. In one embodiment, the cancer cells are breast cancer cells.
摘要翻译：抑制癌细胞中芳香酶活性表达的化合物和方法。提供的化合物是式I的化合物：其中R 1可以是烷基，环烷基，卤代烷基，芳基，取代的芳基，卤代芳基，烷氧基，烷基芳基和芳基烷基; R 2是H，烷基，芳基，烷基芳基，芳基烷基和环烷基; R 3与碱式氮形成酰胺或磺酰胺; R 4选自硝基，胺，酰胺和苯甲酰胺; 或其药学上可接受的盐。还提供分子量小于500g / mol的小分子选择性芳香酶抑制剂。在一些实施方案中，本文所述的小分子选择性芳香酶抑制剂具有小于450g / mol的分子量。还提供了抑制癌细胞中芳香酶活性表达的方法，包括向需要这种治疗的受试者施用药学有效量的小分子芳香酶抑制剂的步骤。在一个实施方案中，癌细胞是乳腺癌细胞。

32. 发明授权

US07230031B2 Thyroid hormone receptor ligand, medicinal compositions containing the same and use thereof 失效
标题翻译：甲状腺激素受体配体，含有其的药物组合物及其用途
公开(公告)号：US07230031B2
公开(公告)日：2007-06-12
申请号：US10502737
申请日：2003-01-28
申请人： Hiroaki Shiohara , Tetsuya Nakamura , Norihiko Kikuchi , Tomonaga Ozawa , Makio Kitazawa
发明人： Hiroaki Shiohara , Tetsuya Nakamura , Norihiko Kikuchi , Tomonaga Ozawa , Makio Kitazawa
IPC分类号： A61K31/19 , C07C303/00
CPC分类号： C07D213/75 , A61K31/19 , A61K31/22 , A61K31/223 , A61K31/225 , A61K31/27 , A61K31/341 , A61K31/351 , A61K31/40 , A61K31/426 , A61K31/44 , A61K31/4406 , A61K31/50 , A61K31/5375 , A61K31/54 , C07C59/72 , C07C233/25 , C07C233/56 , C07C235/66 , C07C309/65 , C07C311/29 , C07C317/22 , C07C323/41 , C07C323/67 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D209/08 , C07D213/76 , C07D237/14 , C07D249/12 , C07D253/075 , C07D257/04 , C07D257/06 , C07D271/07 , C07D277/34 , C07D295/13 , C07D295/192 , C07D295/26 , C07D307/12 , C07D309/06 , C07D403/12 , C07D413/12 , C07D417/12
摘要： The present invention provides a compound represented by general formula (I): or pharmaceutically acceptable salts thereof, wherein W is O, S(O)m, CH2 and the like; R1 is halogen, lower alkyl, halo-lower alkyl, CN and the like; R3 is hydrogen and the like; R4 is hydrogen, halogen, alkyl, halo-lower alkyl, substituted alkyl, aryl, aralkyl, alkoxy, substituted alkoxy, alkanoyl, aroyl, —CONR7(R8), —S(O)mR9, —SO2NR7(R8) and the like; R5 is hydrogen, halogen, alkyl, substituted alkyl and the like; A is —N(R6)CO—A1—COR10 and the like; pharmaceutical compositions containing them and their uses, which have a high affinity to human thyroid hormone receptors, in particular human thyroid hormone receptor β.
摘要翻译：本发明提供由通式（I）表示的化合物或其药学上可接受的盐，其中W为O，S（O）m，CH 2等 ; R 1是卤素，低级烷基，卤代低级烷基，CN等; R 3是氢等; R 4是氢，卤素，烷基，卤代低级烷基，取代的烷基，芳基，芳烷基，烷氧基，取代的烷氧基，烷酰基，芳酰基，-CONR 7 S（O）m R 9，-SO 2 NR 7，S（O）（R 8 S 8）等; R 5是氢，卤素，烷基，取代的烷基等; A是-N（R 6）CO-A 1 -COR 10等; 含有它们的药物组合物及其用途，其对人甲状腺激素受体，特别是甲状腺激素受体β具有高亲和力。

33. 发明授权

US07217492B2 Onium salt compound and radiation-sensitive resin composition 有权
标题翻译： ium盐化合物和辐射敏感性树脂组合物
公开(公告)号：US07217492B2
公开(公告)日：2007-05-15
申请号：US10743809
申请日：2003-12-24
申请人： Eiji Yoneda , Yong Wang , Yukio Nishimura
发明人： Eiji Yoneda , Yong Wang , Yukio Nishimura
IPC分类号： G03F7/038 , G03F7/039 , C07C303/00 , C07C307/00 , C07C315/00
CPC分类号： C07D317/72 , C07C317/14 , C07C381/12 , C07C2601/14 , C07C2602/42 , C07D319/08 , C07D333/46 , G03F7/0045 , G03F7/0392 , G03F7/0757 , Y10S430/115 , Y10S430/122
摘要： An onium salt compound having a cation moiety of the following formula (1) is disclosed. wherein A represents I or S, m is 1 or 2, n is 0 or 1, x is 1–10, and Ar1 and Ar2 are (substituted) aromatic hydrocarbon group, and P represents —O—SO2R, —O—S(O)R, or —SO2R, wherein R represents a hydrogen atom, a (substituted) alkyl group, or a (substituted) alicyclic hydrocarbon group. The onium salt compound is suitable as a photoacid generator for photoresists of a positive-tone radiation-sensitive resin composition. The positive-tone radiation-sensitive resin composition containing this compound is useful as a chemically-amplified photoresist exhibiting high resolution at high sensitivity, responsive to various radiations, and having outstanding storage stability.
摘要翻译：公开了具有下式（1）的阳离子部分的鎓盐化合物。其中A表示I或S，m为1或2，n为0或1，x为1-10，Ar 1和Ar 2为（取代的）芳族烃基，P为-O-SO 2，（O）R或-SO 2 R，其中R表示氢原子，（取代的）烷基或（取代的）脂环族烃基。鎓盐化合物适合作为正色散辐射敏感性树脂组合物的光致抗蚀剂的光致酸发生剂。含有该化合物的正色散辐射敏感性树脂组合物可用作高灵敏度的高分辨率的化学扩增光致抗蚀剂，对各种辐射有响应，并且具有优异的储存稳定性。

34. 发明申请

US20070106095A1 Vitamin d receptor modulators 失效
标题翻译：维生素d受体调节剂
公开(公告)号：US20070106095A1
公开(公告)日：2007-05-10
申请号：US10579563
申请日：2004-11-16
申请人： Jianliang Lu , Tianwei Ma , Sunil Nagpal , Quanrong Shen , Alan Warshawsky , Jason Ochoada , Ying Yee
发明人： Jianliang Lu , Tianwei Ma , Sunil Nagpal , Quanrong Shen , Alan Warshawsky , Jason Ochoada , Ying Yee
IPC分类号： C07C303/00
CPC分类号： C07D405/12 , C07D307/80 , C07D407/12
摘要： The present invention relates to novel, non-secosteroidal, phenyl-benzofuran compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1α,25 dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.
摘要翻译：本发明涉及具有维生素D受体（VDR）调节活性的新颖非壬基苯基 - 苯并呋喃化合物，其比1α，25二羟基维生素D3低高钙血症。这些化合物可用于治疗骨病和牛皮癣。

35. 发明授权

US07135487B2 Sulphonamide derivatives 失效
标题翻译：磺酰胺衍生物
公开(公告)号：US07135487B2
公开(公告)日：2006-11-14
申请号：US10447619
申请日：2003-05-29
申请人： Macklin B Arnold , Stephen R Baker , Thomas J Bleisch , Buddy E Cantrell , Ana M Escribano , Ken Matsumoto , Tracey E McKennon , Paul L Ornstein , Richard L Simon , Edward C. R. Smith , Hamideh Zarrinmayeh , Dennis M Zimmerman
发明人： Macklin B Arnold , Stephen R Baker , Thomas J Bleisch , Buddy E Cantrell , Ana M Escribano , Ken Matsumoto , Tracey E McKennon , Paul L Ornstein , Richard L Simon , Edward C. R. Smith , Hamideh Zarrinmayeh , Dennis M Zimmerman
IPC分类号： A61K31/44 , C07D213/06 , C07D333/12 , C07C255/03 , C07C303/00
CPC分类号： A61K31/18 , A61K31/381 , A61K31/41 , A61K31/42 , A61K31/4245 , A61K31/4418 , A61K31/451 , A61K31/455 , C07C307/08 , C07C311/03 , C07C311/04 , C07C311/05 , C07C311/06 , C07C311/09 , C07C311/14 , C07C311/16 , C07C311/24 , C07C311/29 , C07C311/39 , C07C311/53 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/42 , C07D207/277 , C07D211/18 , C07D211/28 , C07D213/42 , C07D213/81 , C07D213/82 , C07D239/26 , C07D257/04 , C07D261/08 , C07D261/10 , C07D261/18 , C07D271/06 , C07D277/24 , C07D277/28 , C07D277/56 , C07D277/66 , C07D279/02 , C07D307/12 , C07D307/52 , C07D307/68 , C07D307/71 , C07D333/16 , C07D333/20 , C07D333/22 , C07D333/28 , C07D333/34 , C07D333/38 , C07D333/58 , C07D333/68 , C07D409/04
摘要： The present invention relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.
摘要翻译：本发明涉及新型磺酰胺衍生物，其制备方法和含有它们的药物组合物。

36. 发明授权

US07078551B2 Blocked mercaptosilane coupling agents for filled rubbers 有权
标题翻译：用于填充橡胶的封闭的巯基硅烷偶联剂
公开(公告)号：US07078551B2
公开(公告)日：2006-07-18
申请号：US10835726
申请日：2004-04-30
申请人： Richard W. Cruse , Robert J. Pickwell , Eric Raymond Pohl , Keith J. Weller
发明人： Richard W. Cruse , Robert J. Pickwell , Eric Raymond Pohl , Keith J. Weller
IPC分类号： C07C303/00 , C07C331/00 , B60C1/00
CPC分类号： C07F9/4075 , C07F7/1804 , C07F9/1651 , C08J3/203 , C08J2321/00 , C08K3/013 , C08K3/36 , C08K5/0025 , C08K5/5406 , C08K5/548 , C08L9/00 , C08L9/06 , C08L21/00 , C08L2666/08
摘要： A blocked mercaptosilane of the structure: G-C(═O)—S—CH2CH2CH2SiX3 is disclosed wherein each X is an independently selected RO— group or R— group wherein each R is independently selected from the group consisting of hydrogen, alkyl that may or may not contain unsaturation, alkenyl groups, aryl groups, and aralkyl groups, such moieties other than hydrogen having from 1 to 18 carbon atoms, at least one X is RO—, and G is a monovalent alkyl group.
摘要翻译：具有以下结构的封端巯基硅烷：GC（-O）-S-CH 2 CH 2 CH 2 SiX 3 ，其中每个X是独立选择的RO-基团或R-基团，其中每个R独立地选自氢，可以含有或可以不含有不饱和键的烷基，烯基，芳基和芳烷基，例如具有1至18个碳原子的氢以外的部分，至少一个X为RO-，G为一价烷基。

37. 发明授权

US07049455B2 Process for producing shogaols and intermediates for the synthesis thereof 失效
标题翻译：制备shogaols及其合成中间体的方法
公开(公告)号：US07049455B2
公开(公告)日：2006-05-23
申请号：US10514130
申请日：2003-04-25
申请人： Hisatoyo Kato , Shuhei Yamaguchi
发明人： Hisatoyo Kato , Shuhei Yamaguchi
IPC分类号： C07C303/00
CPC分类号： C07C317/18 , A61K31/121 , C07C45/512 , C07C45/65 , C07C49/248 , C07C49/255 , Y02P20/55
摘要： In accordance with the invention, an industrial process for producing shogaols useful in the fields of for example foods, flavor, pharmaceutical products, qui-pharmaceutical products and cosmetics can be provided. The invention relates to novel intermediates represented by the following general formula and a process for producing shogaols from the intermediates. In accordance with the invention, shogaols can readily be produced, of which mass production has been difficult because shogaols have been produced only by the extraction process from a natural ginger.Intermediates; (in the formula (1), R1 represents hydrogen atom or methyl group; R2 represents optionally branched alkyl group with one to 18 carbon atoms; R3 and R4 each independently represents hydrogen atom, a lower alkyl group or a protective group of the phenolic hydroxyl group; A represents an alkylene group with one to 4 carbon atoms; and X represents benzenesulfonyl group or toluenesulfonyl group.)
摘要翻译：根据本发明，可以提供用于生产例如食品，风味剂，药品，药品和化妆品领域的商品的工业方法。本发明涉及由以下通式表示的新型中间体和由中间体生产皂醇的方法。根据本发明，可以容易地生产shogaols，其大批量生产是困难的，因为shogaols仅通过从天然姜的提取过程产生。中间体（式（1）中，R 1表示氢原子或甲基; R 2表示任选具有1至18个碳原子的支链烷基; R 3 R 4和R 4各自独立地表示氢原子，低级烷基或酚羟基的保护基; A表示碳原子数1〜4的亚烷基，X表示苯磺酰基基或甲苯磺酰基。）

38. 发明授权

US06852755B1 Nitrogen mustard compounds and prodrugs therefor 有权
标题翻译：氮芥化合物及其前药
公开(公告)号：US06852755B1
公开(公告)日：2005-02-08
申请号：US09937714
申请日：2000-03-29
申请人： Caroline J. Springer , Lawrence C. Davies
发明人： Caroline J. Springer , Lawrence C. Davies
IPC分类号： A61K48/00 , A61K31/606 , A61K31/609 , A61K38/46 , A61K47/48 , A61P35/00 , A61P43/00 , C07C229/60 , C07C237/36 , A61K31/235 , A61K31/255 , C07C229/14 , C07C303/00 , C07C313/00
CPC分类号： B82Y5/00 , A61K47/6899 , A61K47/6957 , C07C229/60 , C07C237/36
摘要： This invention pertains to nitrogen mustard compounds (Formula (II)) and prodrugs therefor (Formula (I)), methods for their preparation, pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in therapy and treatment, for example, of cancer, wherein: R1 and R2 are independently —Cl, —Br, —I, —OSO2CH3, or —OSO2Ph; R1a, R2a, R1b, and R2b are independently —H, a C1-4alkyl group, or a C1-4haloalkyl group; R3 is —F, —Cl, —Br, —I, —OCHF2, —C≡CH, —OCF3, —CH3, —CF3, —SF5, —SCF3, or —CF2CF3; R4 is —H or as defined for R3−, R5 is —H or —F; R7 is —H, —C(CH3)3, or —CH2—CH—CH2; Z is —CH2—T—W; T is —CH2—, —O—, —S—, —(S═O)—, or —(SO2)—; W is one of: (1) —COOH; (2)—(C═O)OR8; (3) —(C═O)NR9R9; (4) —SO2NHR10−, (5) SO2OR11; (6)—PO3R11R11; (7) a tetrazol-5-yl group; (8) —CONH—SO2R12; and, (9)-M-Het.
摘要翻译：本发明涉及氮芥化合物（式（II））及其前药（式（I）），其制备方法，包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，在治疗和治疗中，例如癌症，其中：R 1和R 2独立地是-Cl，-Br，-I，-OSO 2 CH 3或-OSO 2 Ph; R 1a，R 2a，R 1b和R 2b独立地是-H，C 1-4烷基或C 1-4卤代烷基; R 3是-F，-Cl，-Br，-I，-OCHF 2，-C = CH，-OCF 3，-CH 3，-CF 3，-SF 5，-SCF 3或-CF 2 CF 3; R 4是-H或如对R 3-3所定义，R 5是-H或-F; R 7是-H，-C（CH 3）3或-CH 2 -CH-CH 2; Z是-CH 2 -T-W; T是-CH 2 - ， - O - ， - S - ， - （S = O） - 或 - （SO 2） - ; W是以下之一：（1）-COOH; （2） - （C = O）OR 8; （3） - （C = O）NR 9 R 9; （4）-SO 2 NHR 10，（5）SO 2 OR 11; （6）-PO 3 R 11 R 11; （7）四唑-5-基; （8）-CONH-SO 2 R 12; 和（9）-M-Het。

39. 发明申请

US20040220381A1 Catalyst and method for the production of polytetrahydrofuran 有权
标题翻译：用于生产聚四氢呋喃的催化剂和方法
公开(公告)号：US20040220381A1
公开(公告)日：2004-11-04
申请号：US10481564
申请日：2003-12-22
发明人： Stephan Schlitter , Christoph Sigwart , Walter Dorflinger , Michael Hesse , Rolf-Hartmuth Fischer
IPC分类号： C07C303/00
CPC分类号： B01J21/16 , B01J35/10 , B01J35/1061 , B01J35/1066 , C08G65/20 , C08G65/2657
摘要： Polytetrahydrofuran, polytetrahydrofuran copolymers, diesters or monoesters of these polymers are prepared by polymerization of tetrahydrofuran in the presence of at least one telogen and/or comonomer, which is in the form of shaped catalyst bodies or catalyst particles having a volume of the individual shape of the body or particle of at least 0.05 mm3, preferably at least 0.2 mm3, in particular 1 mm3, and has at least one of the features a) and b): a) a pore radius distribution having at least one maximum in the pore radius range from 100 to 5000 null, b) a pore volume of catalyst pores having radii of 200-3000 null of greater than 0.05 cm3/g and/or a pore volume of pores having radii of 200-5000 null of greater than 0.075 cm3/g and/or a pore volume of pores having radii of >200 null of greater than 0.1 cm3/g.
摘要翻译：这些聚合物的聚四氢呋喃，聚四氢呋喃共聚物，二酯或单酯通过四氢呋喃在至少一种具有各种形状的成型催化剂体或催化剂颗粒的形式的存在下，至少0.05mm 3，优选至少0.2mm 3，特别是1mm 3的主体或颗粒，并且具有特征a）和b）中的至少一个：a）孔半径分布在孔径半径范围内具有至少一个最大值为100至5000，b）具有大于0.05cm 3 / g的半径的200-3000埃的催化剂孔的孔体积和/或具有具有大于0.075cm 3 / g的200-5000埃的半径和/或具有大于0.1cm 3 / g的半径大于等于200埃的孔的孔体积。

40. 发明授权

US6093744A N-acyl sulfamic acid esters useful as hypocholesterolemic agents 失效
标题翻译：可用作降胆固醇药的N-酰基氨基磺酸酯
公开(公告)号：US6093744A
公开(公告)日：2000-07-25
申请号：US117748
申请日：1998-08-10
申请人： Helen Tsenwhei Lee , Joseph Armand Picard , William Howard Roark , Bruce David Roth , Drago Robert Sliskovic
发明人： Helen Tsenwhei Lee , Joseph Armand Picard , William Howard Roark , Bruce David Roth , Drago Robert Sliskovic
IPC分类号： C07C307/02 , C07C311/08 , C07C311/16 , C07C311/44 , C07C331/08 , C07C335/16 , C07D209/20 , C07D333/34 , A01N41/06 , A01K31/18 , C07C303/00 , C07C307/00
CPC分类号： C07C311/08 , C07C307/02 , C07C311/16 , C07C311/44 , C07C331/08 , C07C335/16 , C07D209/20 , C07D333/34
摘要： The instant invention is new compounds of Formula I ##STR1## their use as cerebrovascular agents in diseases such as stroke, peripheral vascular disease, restenosis, and as agents for regulating plasma cholesterol concentrations, for treating hypercholesterolemia and atherosclerosis, and for lowering the serum or plasma level of Lp(a). A pharmaceutical composition is also claimed.
摘要翻译： PCT No.PCT / US97 / 06725 Sec。 371日期：1998年8月10日 102（e）日期1998年8月10日PCT 1997年4月21日PCT PCT。 WO97 / 44314 PCT公开号日期1997年11月27日本发明是式I化合物的新化合物，其用作中风，外周血管疾病，再狭窄等疾病，作为调节血浆胆固醇浓度的药剂，用于治疗高胆固醇血症和动脉粥样硬化的脑血管药，血清或血浆中的Lp（a）水平。还要求药物组合物。

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