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71. 发明申请

US20120252797A1 Isoxazole Compounds As Inhibitors Of Heat Shock Proteins 有权
标题翻译：异恶唑化合物作为热休克蛋白的抑制剂
公开(公告)号：US20120252797A1
公开(公告)日：2012-10-04
申请号：US13525409
申请日：2012-06-18
申请人： Martin James Drysdale , Brian William Dymock , Harry Finch , Paul Webb , Edward McDonald , Karen Elizabeth James , Kwai Ming Cheung , Thomas Peter Matthews
发明人： Martin James Drysdale , Brian William Dymock , Harry Finch , Paul Webb , Edward McDonald , Karen Elizabeth James , Kwai Ming Cheung , Thomas Peter Matthews
IPC分类号： A61K31/42 , C07D413/10 , A61K31/5377 , A61K31/422 , A61K31/4439 , A61P35/00 , A61K31/427 , C07D413/14 , A61K31/496 , A61K31/454 , A61K31/541 , C07D261/08 , C07D417/04
CPC分类号： A61K31/541 , A61K31/42 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/5377 , C07D261/08 , C07D261/10 , C07D413/04 , C07D413/10 , C07D417/04 , C07D495/04
摘要： Isoxazoles of formula (A) or (B) wherein R1 is a group of formula (IB) The isoxazoles are inhibitors of HSP90 activity, and useful for the treatment of, for example, cancers.
摘要翻译：式（A）或（B）的异恶唑其中R1是式（IB）的基团异恶唑是HSP90活性的抑制剂，可用于治疗例如癌症。

72. 发明授权

US08078313B2 Methods and systems for sorting unaddressed items 有权
标题翻译：排除未编址项目的方法和系统
公开(公告)号：US08078313B2
公开(公告)日：2011-12-13
申请号：US10952818
申请日：2004-09-30
申请人： Glenn Edward McDonald , Wilson Wong
发明人： Glenn Edward McDonald , Wilson Wong
IPC分类号： G06F7/00
CPC分类号： B07C3/00 , Y10S209/90
摘要： Systems and methods for sorting a plurality of unaddressed items may comprise receiving delivery point address data. Furthermore, systems and methods for sorting a plurality of unaddressed items may comprise sorting the plurality of unaddressed items based on the delivery point address data. The plurality of unaddressed items may be sorted in an order in which they are to be delivered within a delivery zone specified by the delivery point address data.
摘要翻译：用于排序多个未寻址的物品的系统和方法可以包括接收递送点地址数据。此外，用于排序多个未寻址项目的系统和方法可以包括基于递送点地址数据对多个未寻址项目进行排序。多个未解决的项目可以按照它们在由递送点地址数据指定的递送区域内被递送的顺序进行排序。

73. 发明授权

US07728016B2 Substituted 5-membered ring compounds and their use 失效
标题翻译：取代的5元环化合物及其用途
公开(公告)号：US07728016B2
公开(公告)日：2010-06-01
申请号：US10561969
申请日：2004-06-24
申请人： Kwai Ming Cheung , Brian William Dymock , Edward McDonald , Martin James Drysdale
发明人： Kwai Ming Cheung , Brian William Dymock , Edward McDonald , Martin James Drysdale
IPC分类号： A61K31/4192 , C07D249/06
CPC分类号： A61K31/4196 , A61K31/4192 , A61K31/427 , A61K31/433
摘要： Compound of a compound of formula (I) or a salt, N-oxide, hydrate or solvate thereof, in the preparation of a composition for inhibition of HSP90 activity: wherein ring A is an aromatic or non-aromatic carbocyclic or heterocyclic ring having 5 ring atoms, for example 1,2,3-triazolyl or a 1,2,4-triazolyl or a tetrazolyl ring; and R1 R2 R3 are as defined in the specification are inhibitors of HSP90 and therefore of use in the treatment of, for example, cancers, viral disease, inflammatory diseases such as rheumatoid arthritis, asthma, multiple sclerosis, Type I diabetes, lupus, psoriasis and inflammatory bowel disease; cystic fibrosis angiogenesis-related disease such as diabetic retinopathy, haemangiomas, and endometriosis; or for protection of normal cells against chemotherapy-induced toxicity; or diseases where failure to undergo apoptosis is an underlying factor, or protection from hypoxia-ischemic injury due to elevation of Hsp70 in the heart and brain; scrapie/CJD, Huntingdon's and Alzheimer's disease.
摘要翻译：式（I）化合物或其盐，N-氧化物，水合物或溶剂化物的化合物在制备抑制HSP90活性的组合物中的用途：其中环A是具有5个或更多个碳原子的芳族或非芳族碳环或杂环环原子，例如1,2,3-三唑基或1,2,4-三唑基或四唑基环; 和R1 R2 R3如本说明书中所定义的是HSP90的抑制剂，因此用于治疗例如癌症，病毒性疾病，炎性疾病如类风湿性关节炎，哮喘，多发性硬化，I型糖尿病，狼疮，牛皮癣和炎症性肠病; 囊性纤维化血管生成相关疾病如糖尿病性视网膜病变，血管瘤和子宫内膜异位症; 或用于保护正常细胞免受化疗诱导的毒性; 或未能进行细胞凋亡的疾病是潜在的因素，或由于心脏和脑中Hsp70的升高而保护缺氧缺血性损伤; 瘙痒病/ CJD，亨廷顿氏症和阿尔茨海默病。

74. 发明申请

US20100130496A1 PYRIMIDINE DERIVATIVES AS INHIBITORS OF PHOSPHATIDYLINOSITOL-3-KINASE 审中-公开
标题翻译：作为磷脂酰肌醇三激酶的抑制剂的吡嗪衍生物
公开(公告)号：US20100130496A1
公开(公告)日：2010-05-27
申请号：US12594529
申请日：2008-04-14
申请人： Paul John Goldsmith , Timothy Colin Hancox , Neil Anthony Pegg , Stephen Joseph Shuttleworth , Elsa Amandine Dechaux , Stephen Price , Jonathan Martin Large , Edward McDonald
发明人： Paul John Goldsmith , Timothy Colin Hancox , Neil Anthony Pegg , Stephen Joseph Shuttleworth , Elsa Amandine Dechaux , Stephen Price , Jonathan Martin Large , Edward McDonald
IPC分类号： A61K31/5377 , C07D413/14 , A61P35/00 , A61P37/00 , A61P9/00 , A61P29/00 , A61P31/12 , A61P25/00 , A61P5/00 , A61P3/00
CPC分类号： C07D403/04 , C07D401/14 , C07D417/14
摘要： The invention provides a pyrimidine compound of formula (I): wherein R1, R2, and Y have any of the values defined herein; or a pharmaceutically acceptable salt thereof. The compounds are inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
摘要翻译：本发明提供式（I）的嘧啶化合物：其中R1，R2和Y具有本文定义的任何值; 或其药学上可接受的盐。这些化合物是PI3K的抑制剂，因此可用于治疗由与PI3激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍等相关的异常细胞生长，功能或行为引起的疾病和障碍，神经障碍。

75. 发明申请

US20090270427A1 PURINE DERIVATIVES 审中-公开
标题翻译：嘌呤衍生物
公开(公告)号：US20090270427A1
公开(公告)日：2009-10-29
申请号：US12433388
申请日：2009-04-30
申请人： Peter Martin FISHER , Michael JARMAN , Edward MCDONALD , Bernard NUTLEY , Florence RAYNAUD , Stuart WILSON , Paul WORKMAN
发明人： Peter Martin FISHER , Michael JARMAN , Edward MCDONALD , Bernard NUTLEY , Florence RAYNAUD , Stuart WILSON , Paul WORKMAN
IPC分类号： A61K31/52 , C07D473/16 , A61P35/00 , C12N9/99
CPC分类号： C07D473/16
摘要： The present invention relates to compounds of formula 1 or pharmaceutically acceptable salts thereof, wherein one of R1 and R2 is methyl, ethyl or isopropyl, and the other is H; R3 and R4 are each independently H, branched or unbranched C1-C6 alkyl, or aryl, and wherein at least one of R3 and R4 is other than H; R5 is a branched or unbranched C1-C5 alkyl group or a C1-C6 cycloalkyl group, each of which may be optionally substituted with one or more OH groups; R6, R7, R8 and R9 are each independently H, halogen, NO2, OH, OMe, CN, NH2, COOH, CONH2, or SO2NH2. A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula 1, and the use of said compounds in treating proliferative disorders, viral disorders, CNS disorders, diabetes, stroke, alopecia or neurodegenerative disorders.
摘要翻译：本发明涉及式1化合物或其药学上可接受的盐，其中R 1和R 2之一是甲基，乙基或异丙基，另一个是H; R 3和R 4各自独立地为H，支链或非支链的C 1 -C 6烷基或芳基，并且其中R 3和R 4中的至少一个不是H; R5是支链或非支链C 1 -C 5烷基或C 1 -C 6环烷基，其各自可以任选被一个或多个OH基取代; R6，R7，R8和R9各自独立地为H，卤素，NO2，OH，OMe，CN，NH2，COOH，CONH2或SO2NH2。本发明的另一方面涉及包含式1化合物的药物组合物，以及所述化合物在治疗增殖性疾病，病毒性疾病，中枢神经系统疾病，糖尿病，中风，脱发或神经变性疾病中的用途。

76. 发明申请

US20090264472A1 METHODS AND COMPOSITIONS FOR TREATING POST-OPERATIVE PAIN COMPRISING A LOCAL ANESTHETIC 有权
标题翻译：用于治疗包括局部麻醉的手术后疼痛的方法和组合
公开(公告)号：US20090264472A1
公开(公告)日：2009-10-22
申请号：US12420177
申请日：2009-04-08
申请人： Amira Wohabrebbi , William F. McKay , Vanja Margareta King , Danielle L. Biggs , Katara Shaw , Christopher M. Hobot , Phillip Edward McDonald
发明人： Amira Wohabrebbi , William F. McKay , Vanja Margareta King , Danielle L. Biggs , Katara Shaw , Christopher M. Hobot , Phillip Edward McDonald
IPC分类号： A61K31/445
CPC分类号： A61K31/445 , A61K9/0024 , A61K9/146 , A61K9/1647 , A61K9/7007 , A61K31/4458
摘要： The present invention is directed to an implantable drug depot useful for reducing, preventing or treating post-operative pain in a patient in need of such treatment, the implantable drug depot comprising a polymer and a therapeutically effective amount of a local anesthetic or pharmaceutically acceptable salt thereof, wherein the drug depot is implantable at a site beneath the skin to reduce, prevent or treat post-operative pain, and the drug depot is capable of releasing (i) a bolus dose of the local anesthetic or pharmaceutically acceptable salt thereof at a site beneath the skin and (ii) a sustained release dose of an effective amount of the local anesthetic or pharmaceutically acceptable salt thereof over a period of at least 4 days.
摘要翻译：本发明涉及可用于减少，预防或治疗需要这种治疗的患者的手术后疼痛的可植入药物储存库，所述可植入药物储库包含聚合物和治疗有效量的局部麻醉剂或药学上可接受的盐其中所述药物储存库可植入皮肤下面的部位以减少，预防或治疗手术后疼痛，并且所述药物储库能够释放（i）所述局部麻醉剂或其药学上可接受的盐的推注剂量（ii）持续释放剂量的有效量的局部麻醉剂或其药学上可接受的盐在至少4天的时间内。

77. 发明申请

US20090156601A1 PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的吡嗪衍生物
公开(公告)号：US20090156601A1
公开(公告)日：2009-06-18
申请号：US12089874
申请日：2006-10-10
申请人： Edward McDonald , Jonathan M. Large , Adrian J. Folkes , Stephen J. Shuttleworth , Nan Chi Wan
发明人： Edward McDonald , Jonathan M. Large , Adrian J. Folkes , Stephen J. Shuttleworth , Nan Chi Wan
IPC分类号： A61K31/5377 , C07D413/14 , A61P29/00
CPC分类号： C07D239/48 , C07D401/12 , C07D401/14 , C07D405/12
摘要： The invention provides compounds which are pyrimidines of formula (I): wherein —XR3 is bonded at ring position 2 and —YR4 is bonded at ring position 5 or 6; R1 and R2 form, together with the N atom to which they are attached, a morphorine ring which is unsubstituted or substituted; X is a direct bond; R3 is selected from (i) a group of the following formula (1): wherein B is a phenyl ring which is unsubstituted or substituted and Z is selected from —OR, CH2OR and —NRS(O) mR, wherein each R is independently selected from H, C1-C6 alkyl, C3-C10 cycloalkyl and a 5- to 12-membered aryl or heteroaryl group, the group being unsubstituted or substituted, and m is 2; and (ii) an indazole group which is unsubstituted or substituted; and Y is selected from —O—(CH2)n—, —NH—(CH2)n, —NHC(O)—(CH2)n— and —C(O)NH—(CH2)n— wherein n is 0 or an integer of 1 to 3, and R4 is selected from an unsaturated 5- to 12-membered carbocyclic or heterocyclic group which is unsubstituted or substituted and a group —NR5R6 wherein R5 and R6, which are the same or different, are each independently selected from H, C1-C6 alkyl which is unsubstituted or substituted, C3-C10 cycloalkyl which is unsubstituted or substituted, —C(O)R, —C(O)N(R)2 and —S(O)mR wherein R and m are as defined above, or R5 and R6 together form, with the nitrogen atom to which they are attached, a saturated 5-, 6- or 7-membered N-containing heterocyclic group which is unsubstituted or substituted; and the pharmaceutically acceptable salts thereof. These compounds are inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
摘要翻译：本发明提供了式（I）的嘧啶的化合物：其中-XR3在环位置2键合，-YR4键合在环位置5或6; R1和R2与它们所连接的N原子一起形成未取代或取代的吗啉环; X是直接的债券; R3选自（i）下式（1）的基团：其中B是未取代或取代的苯基环，Z选自-OR，CH 2 OR和-NRS（O）m R，其中每个R独立地为选自H，C 1 -C 6烷基，C 3 -C 10环烷基和5至12元芳基或杂芳基，该基团是未取代或取代的，m为2; 和（ii）未取代或取代的吲唑基; 并且Y选自-O-（CH 2）n - ， - NH - （CH 2）n，-NHC（O） - （CH 2）n - 和-C（O）NH-（CH 2）或1〜3的整数，R 4选自未取代或取代的不饱和5〜12元碳环或杂环基和-NR 5 R 6基，其中R 5和R 6相同或不同，各自独立地为未取代或未取代的C 1 -C 6环烷基，-C（O）R 1 -C（O）N（R）2和-S（O）m R，其中R 和m如上所定义，或者R 5和R 6与它们所连接的氮原子一起形成未取代或取代的饱和的5-，6-或7-元含氮杂环基; 及其药学上可接受的盐。这些化合物是PI3K的抑制剂，因此可用于治疗与PI3激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍等相关的异常细胞生长，功能或行为引起的疾病和障碍，神经障碍。

78. 发明申请

US20090081273A1 Medical Devices and Methods Including Polymers Having Biologically Active Agents Therein 有权
标题翻译：包括其中具有生物活性剂的聚合物的医疗设备和方法
公开(公告)号：US20090081273A1
公开(公告)日：2009-03-26
申请号：US12234011
申请日：2008-09-19
申请人： Phillip Edward McDonald , Christopher M. Hobot
发明人： Phillip Edward McDonald , Christopher M. Hobot
IPC分类号： A61F2/04 , A61K38/18
CPC分类号： A61K38/1875 , A61L27/34 , A61L27/54 , A61L2300/252 , A61L2300/45 , A61L2300/602
摘要： Medical devices and methods including polymers having biologically active agents therein are disclosed. The medical devices can be useful as implantable devices such as orthopedic implants.
摘要翻译：公开了包括其中具有生物活性剂的聚合物的医疗装置和方法。医疗设备可用作诸如矫形植入物之类的可植入装置。

79. 发明授权

US07179819B2 VLA-4 inhibitor compounds 失效
标题翻译： VLA-4抑制剂化合物
公开(公告)号：US07179819B2
公开(公告)日：2007-02-20
申请号：US10787905
申请日：2004-02-26
申请人： John J. Baldwin , Edward McDonald , Kevin Joseph Moriarty , Christopher Ronald Sarko , Nobuo Machinaga , Atsushi Nakayama , Jun Chiba , Iimura Shin , Yoshiyuki Yoneda
发明人： John J. Baldwin , Edward McDonald , Kevin Joseph Moriarty , Christopher Ronald Sarko , Nobuo Machinaga , Atsushi Nakayama , Jun Chiba , Iimura Shin , Yoshiyuki Yoneda
IPC分类号： C07D277/04 , A61K31/425 , C07D207/12
CPC分类号： C07D207/08 , C07C275/42 , C07C2601/02 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/22 , C07D207/24 , C07D209/12 , C07D211/26 , C07D211/34 , C07D211/38 , C07D213/55 , C07D217/02 , C07D277/04 , C07D277/28 , C07D277/48 , C07D295/13 , C07D295/185 , C07D307/33 , C07D311/20 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/02 , C07D413/06 , C07D491/04
摘要： Compounds that selectively inhibit the binding of ligands to α4β1 integrin (VLA-4) and methods for their preparation are disclosed. In one embodiment, compounds of the invention are represented by Formula I: As selective inhibitors of VLA-4 mediated cell adhesion, compounds of the present invention are useful in the treatment of conditions associated with such adhesion, including, but not limited to, such conditions as inflammatory and autoimmune responses, diabetes, asthma, psoriasis, inflammatory bowel disease, transplantation rejection, and tumor metastasis. Also disclosed are methods of inhibiting VLA-4 mediated cell adhesion and methods of treating conditions associated with LA-4 mediated cell adhesion.
摘要翻译：公开了选择性抑制配体与α4β1整联蛋白（VLA-4）的结合的化合物及其制备方法。在一个实施方案中，本发明的化合物由式I表示：作为VLA-4介导的细胞粘附的选择性抑制剂，本发明的化合物可用于治疗与这种粘附相关的病症，包括但不限于此作为炎症和自身免疫反应的病症，糖尿病，哮喘，牛皮癣，炎性肠病，移植排斥反应和肿瘤转移。还公开了抑制VLA-4介导的细胞粘附的方法以及治疗与LA-4介导的细胞粘附相关的病症的方法。

80. 发明授权

US06462196B1 Preparation of a camptothecin derivative by intramolecular cyclization 失效
标题翻译：通过分子内环化制备喜树碱衍生物
公开(公告)号：US06462196B1
公开(公告)日：2002-10-08
申请号：US09552214
申请日：2000-04-19
申请人： Francis Gerard Fang , Edward McDonald Huie , Shiping Xie , Daniel L. Comins
发明人： Francis Gerard Fang , Edward McDonald Huie , Shiping Xie , Daniel L. Comins
IPC分类号： C07D41304
CPC分类号： C07D213/64 , C07D213/69 , C07D491/04
摘要： The present invention relates to a method for the preparation for camptothecin and camptothecin-like compounds and to novel intermediates used in this preparation. In particular, the invention provides a process for the preparation of the camptothecin derivative of formula (I′) known by the chemical name “7-(4-methylpiperazino-methylene)-10,11-ethylenedioxy-20(R,S)-camptothecin”, which comprises cyclising the compound of formula (II′), wherein X is halogen, particularly chloro, bromo, or iodo; and when the compound of formula (I′) is obtained as a mixture of enantiomers optionally resolving the mixture to obtain the desired enantiomer; and/or if desired, converting the resulting compound of formula (I′) or a salt thereof into a physiologically acceptable salt or solvate thereof.
摘要翻译：本发明涉及一种制备喜树碱和喜树碱样化合物的方法以及本制剂中使用的新型中间体。特别地，本发明提供制备式（I'）的喜树碱衍生物的方法，该化合物名称为“7-（4-甲基哌嗪基 - 亚甲基）-10,11-亚乙基二氧基-20（R，S） - 喜树碱“，其包括使式（II'）化合物环化，其中X是卤素，特别是氯，溴或碘; 并且当以对映异构体的混合物获得式（I'）化合物时，任选地拆分混合物以获得所需的对映异构体; 和/或如果需要，将所得的式（I'）化合物或其盐转化为其生理学上可接受的盐或溶剂化物。

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