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1. 发明申请

US20050014802A1 Triheterocyclic compounds, compositions, and methods for treating cancer or viral diseases 有权
公开(公告)号：US20050014802A1
公开(公告)日：2005-01-20
申请号：US10857458
申请日：2004-05-28
申请人： Giorgio Attardo , Kenza Dairi , Jean-Francois Lavallee , Elise Rioux , Sasmita Tripathy , Terrence Doyle , Xavier Billot
发明人： Giorgio Attardo , Kenza Dairi , Jean-Francois Lavallee , Elise Rioux , Sasmita Tripathy , Terrence Doyle , Xavier Billot
IPC分类号： C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D491/04 , C07F9/6558 , A61K31/433 , A61K31/4196 , A61K31/4245 , C07D417/14
CPC分类号： C07D403/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D491/04 , C07F9/65583
摘要： The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Triheterocyclic Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus.

2. 发明申请

US20050032802A1 Diterpenoid compounds, compositions thereof and their use as anti-cancer or anti-fungal agents 失效
公开(公告)号：US20050032802A1
公开(公告)日：2005-02-10
申请号：US10865262
申请日：2004-06-10
申请人： Jean-Francois Lavallee , Terrence Doyle , Elise Rioux , Laurent Belec , Daniel Rabouin , Xavier Billot
发明人： Jean-Francois Lavallee , Terrence Doyle , Elise Rioux , Laurent Belec , Daniel Rabouin , Xavier Billot
IPC分类号： A61K31/085 , A61K31/121 , A61K31/495 , A61K31/502 , A61K31/517 , A61P35/00 , C07C43/162 , C07C43/164 , C07C45/29 , C07C49/115 , C07C49/225 , C07C49/755 , C07C69/00 , C07C323/59 , C07F9/117 , C07D237/36 , A61K31/498
CPC分类号： C07C45/292 , C07C49/755 , C07C69/757 , C07C323/59 , C07C2603/26 , C07F9/117
摘要： The present invention relates to Diterpenoid Compounds, compositions comprising an effective amount of a Diterpenoid Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering an effective amount of a Diterpenoid Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, or for inducing apoptosis in a cancer or neoplastic cell. The compounds, compositions, and methods of the invention are further useful for treating or preventing a fungal infection. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a fungus.

3. 发明申请

US20060089332A1 Phosphate-bearing prodrugs of sulfonyl hydrazines as hypoxia-selective antineoplastic agents 有权
标题翻译：含磺酸肼的含磷前体作为缺氧选择性抗肿瘤药
公开(公告)号：US20060089332A1
公开(公告)日：2006-04-27
申请号：US11232252
申请日：2005-09-21
申请人： Xu Lin , Ivan King , Michael Belcourt , Terrence Doyle
发明人： Xu Lin , Ivan King , Michael Belcourt , Terrence Doyle
IPC分类号： A61K31/675 , C07F9/58 , C07F9/28
CPC分类号： C07F9/12 , C07F9/6518
摘要： Novel phosphate-bearing prodrugs of sulfonyl hydrazines have the formulas I, II, III and IV. Pharmaceutical compositions and uses thereof in the treatment of cancer are claimed. The aforementioned prodrugs include enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates and metabolites from all stages. The aforementioned prodrugs are preferentially activated in hypoxic tumors and can be given either alone, or in combination with other anticancer agents or with phototheraphy or radiotherapy. Where R=C1-10 alkyl, or C1-10 haloalkyl (preferably containing no more than 5 halogen groups, preferably 2-chloroethyl); R′ and R″ are independently C1-10 alkyl, or C5-20 aryl or heteroaryl (preferably methyl); R1 is H, C1-10 alkyl, C1-10 alkoxyl, C5-20 aryl or heteroaryl or C5-20 aroxyl or heteroaroxyl (preferably methyl and ethyl); X is O, NH, or NR (preferably O); Y is (CH2)n, O(CH2)n, NH(CH2)n, NR(CH2)n, OCOO(CH2)n, NHCOO(CH2)n; n is 1, 2, 3, 4 or 5 (preferably n=2 and 3); or Y=aryl or heteroaryl (preferably para-phenyl); A=CH, or N (preferably CH); and B=CH═CH, O, S, NH, or NR (preferably CH═CH); or pharmaceutically acceptable salts, solvates, polymorphs or metabolites, thereof.
摘要翻译：磺酰肼的新型含磷酸酯前药具有式I，II，III和IV。要求保护药物组合物及其在治疗癌症中的用途。前述药物包括对映异构体，立体异构体和互变异构体，以及来自所有阶段的药学上可接受的盐或溶剂合物和代谢物。上述前药优先在缺氧性肿瘤中活化，并且可以单独给予，也可以与其它抗癌剂或光疗法或放疗相结合。其中R = C 1-10烷基或C 1-10 1-10卤代烷基（优选含有不超过5个卤素基团，优选2-氯乙基）; R'和R“独立地为C 1-10烷基或C 5-20-20芳基或杂芳基（优选甲基）; R 1是H，C 1-10烷基，C 1-10烷氧基，C 5-20-20芳基或杂芳基或C 5-20芳基或杂芳基（优选甲基和乙基）; X是O，NH或NR（优选O）; Y（CH 2）n，O（CH 2）n，NH（CH 2） NR（CH 2）n，OCOO（CH 2）2，N（CH 2）n， nCO 2，NHCOO（CH 2 CH 2）n N; n为1,2,3,4或5（优选n = 2和3）; 或Y =芳基或杂芳基（优选对苯基）; A = CH或N（优选CH）; 和B = CH-CH，O，S，NH或NR（优选CH-CH）; 或其药学上可接受的盐，溶剂合物，多晶型物或代谢物。

4. 发明申请

US20070030004A1 Magnetic resonance imaging scanner with molded fixed shims 有权
标题翻译：具有模制固定垫片的磁共振成像扫描仪
公开(公告)号：US20070030004A1
公开(公告)日：2007-02-08
申请号：US10558768
申请日：2004-05-19
申请人： William Amor , Dennis Everett , Jerome Alden , Robert Henderson , Terrence Doyle , Ronald Sharpless , Gerardus Mulder , Gerardus Peeren
发明人： William Amor , Dennis Everett , Jerome Alden , Robert Henderson , Terrence Doyle , Ronald Sharpless , Gerardus Mulder , Gerardus Peeren
IPC分类号： G01V3/00
CPC分类号： G01R33/3873
摘要： A magnetic resonance imaging scanner includes a generally cylindrical main magnet assembly (10) that defines a cylinder axis (16). A first set of shims (60) are rigidly positioned inside the magnet assembly (10) at about a first distance (d1) relative to the cylinder axis (16). A second set of shims (62) are rigidly positioned inside the main magnet assembly (10) at about a second distance (d2) relative to the cylinder axis (16). The second distance (d2) is different from the first distance (d1). A generally cylindrical radio frequency coil (26) is arranged inside the main magnet assembly (10) at about a third distance (d3) relative to the cylinder axis (16). A plurality of gradient coils (20) are arranged inside the main magnet assembly (10) at about a fourth distance (d4) relative to the cylinder axis (16).
摘要翻译：磁共振成像扫描仪包括限定气缸轴线（16）的大致圆柱形的主磁体组件（10）。第一组垫片（60）相对于气缸轴线（16）以大约第一距离（d 1）刚性地定位在磁体组件（10）的内部。第二组垫片（62）相对于气缸轴线（16）以大约第二距离（d 2）刚性地定位在主磁体组件（10）的内部。第二距离（d 2）与第一距离（d 1）不同。大致圆柱形的射频线圈（26）相对于气缸轴线（16）以大约第三距离（d 3）布置在主磁体组件（10）的内部。多个梯度线圈（20）相对于气缸轴线（16）以大约第四距离（d 4）布置在主磁体组件（10）的内部。

5. 发明申请

US20050267073A1 Triheterocyclic compounds, compositions, and methods for treating cancer or viral diseases 审中-公开
标题翻译：三联环化合物，组合物和治疗癌症或病毒性疾病的方法
公开(公告)号：US20050267073A1
公开(公告)日：2005-12-01
申请号：US11140367
申请日：2005-05-27
申请人： Kenza Dairi , Jean-Francois Lavallee , Terrence Doyle
发明人： Kenza Dairi , Jean-Francois Lavallee , Terrence Doyle
IPC分类号： A61K31/675 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D491/04 , C07F9/572 , C07F9/6558
CPC分类号： C07D491/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07F9/5728 , C07F9/65583
摘要： The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Triheterocyclic Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus.
摘要翻译：本发明涉及新颖的三杂环化合物，包含三杂环化合物的组合物，以及可用于治疗或预防癌症或肿瘤性疾病的方法，包括给予三环杂环化合物。本发明的化合物，组合物和方法也可用于抑制癌细胞或肿瘤细胞的生长，治疗或预防病毒感染，或抑制病毒的复制和/或感染性。

6. 发明申请

US20050043244A1 Water-soluble SHPs as novel alkylating agents 审中-公开
标题翻译：水溶性SHP作为新型烷基化剂
公开(公告)号：US20050043244A1
公开(公告)日：2005-02-24
申请号：US10950890
申请日：2004-09-27
申请人： Xu Lin , Terrence Doyle , Ivan King
发明人： Xu Lin , Terrence Doyle , Ivan King
IPC分类号： A61K38/04 , A61K38/16 , C07C311/55 , C07F9/12 , A61K31/175 , A61K31/195 , A61K31/277 , A61K38/05 , A61K38/06 , A61K38/08 , A61K38/10
CPC分类号： C07C311/55 , A61K38/04 , A61K38/16 , C07F9/12
摘要： The present invention relates to compounds according to the structure (I): Where R is —CH3 or —CH2CH2Cl; R′ is C1-C7 alkyl or —CH2CH2Cl; R2 or R4 is OP03H2, N02, OCO(Glu-OH), NHCO(Glu-OH), NHR7 and unassigned groups of R2, R3, R4, R5 and R6 are, independently, H, F, Cl, Br, I, OH, OP03H2, OCH3, CF3, OCF3, NO2, CN, SO2CH3, SO2CF3, COCH3, COOCH3, SCH3, SFs, NH2, NHR7, N(CH3)2, OPO3H2, or a C1-C7 alkyl group with the proviso that when any two of unassigned groups of R2, R3, R4, R5 or R6 are other than H, the other two of unassigned groups of R2, R3, R4, R5 or R6 are H. R7 is H or polyglutamyl as described. Phosphoric acid and glutamic acid can be a free acid or pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及根据结构（I）的化合物：其中R是-CH 3或-CH 2 CH 2 Cl; R'是C 1 -C 7烷基或-CH 2 CH 2 Cl; R2或R4是OP03H2，N02，OCO（Glu-OH），NHCO（Glu-OH），NHR7，R2，R3，R4，R5和R6的未分配基团独立地是H，F，Cl，Br， OH，OPO 3 H 2，OCH 3，CF 3，OCF 3，NO 2，CN，SO 2 CH 3，SO 2 CF 3，COCH 3，COOCH 3，SCH 3，SF，NH 2，NHR 7，N（CH 3）2，OPO 3 H 2或C 1 -C 7烷基， R2，R3，R4，R5或R6的任何两个未分配的基团不是H，R2，R3，R4，R5或R6的另外两个未分配的基团是H.R 7是H或所述的聚谷氨酰基。磷酸和谷氨酸可以是游离酸或其药学上可接受的盐。

7. 依法登记的发明

USH1487H Benzoate derivatives of taxol 失效
标题翻译：紫杉醇的苯甲酸衍生物
公开(公告)号：USH1487H
公开(公告)日：1995-09-05
申请号：US128949
申请日：1993-09-29
申请人： Henry Wong , Terrence Doyle
发明人： Henry Wong , Terrence Doyle
IPC分类号： A61K31/335 , A61K31/337 , A61P35/00 , C07D305/14 , C07F9/655 , C07F9/6558 , C07D413/00
CPC分类号： C07D305/14 , C07F9/65512 , C07F9/65586
摘要： This invention relates to a compound of formula I ##STR1## or a pharmaceutically acceptable salt thereof, in which R.sup.2 is a radical of the formula ##STR2## in which R.sup.a and R.sup.b are independently hydrogen or C.sub.1-6 alkyl, said C.sub.1-6 alkyl being optionally substituted with hydroxy, phosphono, phosphonooxy, carboxy or di(C.sub.1-6 alkyl) amino; or NR.sup.a R.sup.b together represents a radical of the formula ##STR3## in which y is one to three, and R.sup.a is as defined above; R.sup.p and R.sup.r are independently same or different C.sub.1-6 alkyl;R.sup.1 is hydrogen or a radical Z of the formula ##STR4## in which Q is --(CH.sub.2).sub.f --, optionally substituted with one to six same or different C.sub.1-6 alkyl or C.sub.3-6 cycloalkyl, or a carbon atom of said --(CH.sub.2).sub.f -- radical may also be a part of C.sub.3-6 cycloalkylidene;R.sup.3 and R.sup.4 are independently hydrogen or C.sub.1-6 alkyl, or R.sup.3 and R.sup.4 taken together with the carbon atom to which they are attached form C.sub.3-6 cycloalkylidene;R.sup.5 is --OC(.dbd.O)R, --OP.dbd.O(OH).sub.2 or --CH.sub.2 OP.dbd.O(OH).sub.2, in which R is C.sub.1-6 alkyl;R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are independently halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or hydrogen, but when R.sup.5 is --OC(.dbd.O)R, one of R.sup.6, R.sup.7, R.sup.8 or R.sup.9 is --OP.dbd.O(OH).sub.2 ;f is 2 to 6;n is O, and m is 1 or 0 when R.sup.5 is --CH.sub.2 OP.dbd.O(OH).sub.2 ;and n is 1 or 0, and m is 1 when R.sup.5 is --OC(.dbd.O)R or --OP.dbd.O(OH).sub.2.Also provided by this invention are pharmaceutical formulations and a method for treating mammalian tumors with a compound of formula I.
摘要翻译：本发明涉及式Ⅰ的化合物其中R 2是下式的基团，其中R a和R b独立地是氢或C 1-6烷基，所述C 1-6烷基任选被取代与羟基，膦酰基，膦酰氧基，羧基或二（C 1-6烷基）氨基; 或NRaRb一起表示如上所定义的式的基团; Rp和Rr独立地相同或不同的C1-6烷基; R1是氢或具有一至六个相同或不同的C 1-6烷基或C 3-6环烷基或所述 - （CH 2）f - 基团的碳原子的式“IMAGE”或“IMAGE”的基团Z也可以是部分C3-6亚环烷基; R 3和R 4独立地为氢或C 1-6烷基，或者R 3和R 4与它们所连接的碳原子一起形成C 3-6亚环烷基; R5是-OC（= O）R，-OP = O（OH）2或-CH2OP = O（OH）2，其中R是C1-6烷基; R6，R7，R8和R9独立地是卤素，C1-6烷基，C1-6烷氧基或氢，但当R5是-OC（= O）R时，R6，R7，R8或R9之一是-OP = O（ OH）2; f为2〜6; 当R 5为-CH 2 OP = O（OH）2时，n为O，m为1或0; 当R 5为-OC（= O）R或-OP = O（OH）2时，n为1或0，m为1。本发明还提供药物制剂和用式I化合物治疗哺乳动物肿瘤的方法。

8. 发明授权

US5272171A Phosphonooxy and carbonate derivatives of taxol 失效
标题翻译：紫杉醇的膦酰氧基和碳酸酯衍生物
公开(公告)号：US5272171A
公开(公告)日：1993-12-21
申请号：US981151
申请日：1992-11-24
申请人： Yasutsugu Ueda , Henry Wong , Vittorio Farina , Amarendra Mikkilineni , Dolatrai M. Vyas , Terrence Doyle
发明人： Yasutsugu Ueda , Henry Wong , Vittorio Farina , Amarendra Mikkilineni , Dolatrai M. Vyas , Terrence Doyle
IPC分类号： A61K31/335 , A61K31/337 , A61K31/665 , A61P35/00 , C07D305/14 , C07D407/12 , C07D409/12 , C07F7/18 , C07F9/655 , C07F9/6558 , H01L21/48
CPC分类号： C07D407/12 , C07D305/14 , C07D409/12 , C07F7/1856 , C07F9/65512 , C07F9/65586 , H01L21/4839
摘要： The present invention is directed to novel taxol derivatives useful as anti-tumor agents. Also provided by this invention is pharmaceutical formulations and methods of treating mammalian tumors with the compounds of this invention.

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