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31. 发明申请

US20060183760A1 New purine derivatives 有权
标题翻译：新嘌呤衍生物
公开(公告)号：US20060183760A1
公开(公告)日：2006-08-17
申请号：US11238533
申请日：2005-09-28
申请人： Peter Fischer , Michael Jarman , Edward McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
发明人： Peter Fischer , Michael Jarman , Edward McDonald , Bernard Nutley , Florence Raynaud , Stuart Wilson , Paul Workman
IPC分类号： A61K31/52 , C07D473/12
CPC分类号： C07D473/16
摘要： The present invention relates to compounds of formula I 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 un branched 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I化合物或其药学上可接受的盐，其中R 1和R 2中的一个为甲基，乙基或异丙基，另一个为H; R 3和R 4各自独立地为H，支链或非支链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; R 5是支链或非支链C 1 -C 5烷基或C 1 -C 3亚烷基其中每一个可以任选地被一个或多个OH基团取代; R 6，R 7，R 8和R 9各自独立地为H，卤素，NO 3， 2，OH，OMe，CN，NH 2，COOH，CONH 2或SO 2 NH 2， / SUB>。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。

32. 发明申请

US20050239770A1 N-heterocyclic inhibitors of TNF-alpha expression 有权
标题翻译： TNF-α表达的N-杂环抑制剂
公开(公告)号：US20050239770A1
公开(公告)日：2005-10-27
申请号：US11143430
申请日：2005-06-02
申请人： Kevin Moriarty , Yvonne Shimshock , Gulzar Ahmed , Junjun Wu , James Wen , Wei Li , Shawn Erickson , Jeffrey Letourneau , Edward McDonald , Katerina Leftheris , Stephen Wrobleski , Zahid Hussain , Ian Henderson , Axel Metzger , John Baldwin , Alaric Dyckman
发明人： Kevin Moriarty , Yvonne Shimshock , Gulzar Ahmed , Junjun Wu , James Wen , Wei Li , Shawn Erickson , Jeffrey Letourneau , Edward McDonald , Katerina Leftheris , Stephen Wrobleski , Zahid Hussain , Ian Henderson , Axel Metzger , John Baldwin , Alaric Dyckman
IPC分类号： A61K31/40 , A61K31/551 , C07D251/52 , C07D251/54 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D521/00
CPC分类号： C07D251/52 , C07D231/12 , C07D233/56 , C07D249/08 , C07D251/48 , C07D251/54 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula I: Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-α expression utilizing compounds of the present invention are also disclosed.
摘要翻译：公开了通过抑制p38激酶阻断细胞因子产生的N-杂环化合物。在一个实施方案中，本发明的化合物由式I表示：还公开了使用本发明化合物的生产方法，药物组合物和治疗与不适当的p38激酶活性或TNF-α表达相关的病症的方法。

33. 发明授权

US06756378B2 VLA-4 inhibitor compounds 失效
标题翻译： VLA-4抑制剂化合物
公开(公告)号：US06756378B2
公开(公告)日：2004-06-29
申请号：US10034585
申请日：2001-12-28
申请人： John J. Baldwin , Edward McDonald , Kevin Joseph Moriarty , Christopher Ronald Sarko , Nobuo Machinaga , Atsushi Nakayama , Jun Chiba , Shin Iimura , Yoshiyuki Yoneda
发明人： John J. Baldwin , Edward McDonald , Kevin Joseph Moriarty , Christopher Ronald Sarko , Nobuo Machinaga , Atsushi Nakayama , Jun Chiba , Shin Iimura , Yoshiyuki Yoneda
IPC分类号： C07D20712
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 &agr;4&bgr;1 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 pharmaceutical compositions, methods of inhibiting VLA-4 mediated cell adhesion and methods of treating conditions associated with LA-4 mediated cell adhesion, which involve compounds of Formula I.
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。还公开了药物组合物，抑制VLA-4介导的细胞粘附的方法和治疗与LA-4介导的细胞粘附相关的病症的方法，涉及式I化合物。

34. 发明授权

US5011359A Silo rotary unloader monitor 失效
标题翻译：筒仓旋转卸载机监视器
公开(公告)号：US5011359A
公开(公告)日：1991-04-30
申请号：US503950
申请日：1990-04-04
申请人： Edward McDonald
发明人： Edward McDonald
IPC分类号： B65G65/38
CPC分类号： B65G65/38
摘要： A silo rotary unloader monitor provides an indication of a rotational speed of the rotary collector ring of a material unloading device suspended within the top portion of a vertical silo. A limit switch has an actuating sensor biased into engagement with a sinusoidal cylindrical surface formed on a wheel mounted for rotation with the rotary collector ring. An electric circuit connected to the limit switch causes a remotely mounted electric signalling lamp or buzzer to flash or sound at a rate proportional to the rotary speed of the collector ring.
摘要翻译：筒仓旋转卸载器监视器提供悬挂在垂直仓的顶部内的卸料装置的旋转集合环的转速的指示。限位开关具有致动传感器，该致动传感器被偏置成与安装成与旋转集电环旋转的轮上形成的正弦圆柱形表面接合。连接到限位开关的电路导致远程安装的电信号灯或蜂鸣器以与收集环的旋转速度成比例的速率闪烁或发出声音。

35. 发明授权

US4760143A Cyclopropane derivatives 失效
公开(公告)号：US4760143A
公开(公告)日：1988-07-26
申请号：US928461
申请日：1986-11-10
申请人： Edward McDonald , Roger Salmon
发明人： Edward McDonald , Roger Salmon
IPC分类号： A01N53/00 , C07D239/26 , C07D239/30 , C07D401/12 , C07D239/02
CPC分类号： C07D239/26 , A01N53/00 , C07D239/30 , C07D401/12
摘要： Cyclopropane acids and derivatives thereof useful as intermediates, insecticidally active esters of these acids, compositions comprising these esters and methods of using the same. The compounds involved have the formula: ##STR1## wherein R.sup.2 represents an .alpha.-branched alkyl group containing from 3 to 6 carbon atoms, and R represents either (a) hydroxy, halo or alkoxy of up to six carbon atoms, or (b) the group --OR.sup.1 where R.sup.1 is the residue of an alcohol of formula R.sup.1 OH which forms an insecticidal ester with chrysanthemic acid, permethrin acid or cyhalothrin acid.

36. 发明申请

US20100256143A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：US20100256143A1
公开(公告)日：2010-10-07
申请号：US12594543
申请日：2008-04-14
申请人： Stewart James Baker , Paul John Goldsmith , Timothy Colin Hancox , Neil Anthony Pegg , Stephen Joseph Shuttleworth , Elsa Amandine Dechaux , Sussie Lerche Krintel , Stephen Price , Jonathan Martin Large , Edward McDonald
发明人： Stewart James Baker , Paul John Goldsmith , Timothy Colin Hancox , Neil Anthony Pegg , Stephen Joseph Shuttleworth , Elsa Amandine Dechaux , Sussie Lerche Krintel , Stephen Price , Jonathan Martin Large , Edward McDonald
IPC分类号： A61K31/5377 , C07D413/14 , A61P35/00 , A61P31/12 , A61P37/00 , A61P29/00 , A61P25/00 , A61P9/00 , A61P3/00
CPC分类号： C07D487/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14
摘要： The invention provides a pyrimidine compound of formula (I): wherein R1 and R2 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和R2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。

37. 发明授权

US07696204B2 Pharmaceutical compounds 失效
标题翻译：药物化合物
公开(公告)号：US07696204B2
公开(公告)日：2010-04-13
申请号：US12089677
申请日：2006-10-11
申请人： Edward McDonald , Jonathan M Large , Stephen J Shuttleworth
发明人： Edward McDonald , Jonathan M Large , Stephen J Shuttleworth
IPC分类号： C07D239/48 , A61K31/505
CPC分类号： C07D239/48 , C07D401/12 , C07D401/14 , C07D405/12
摘要： Pyrimidines of formula (I): wherein R1 to R4, X and Y are defined in the specification are inhibitors of P13K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behavior associated with P13 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
摘要翻译：式（I）的嘧啶：其中R1至R4，X和Y在本说明书中定义为P13K的抑制剂，因此可用于治疗与P13激酶例如癌症相关的异常细胞生长，功能或行为引起的疾病和病症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍和神经障碍。

38. 发明申请

US20090247579A1 2-[3H-THIAZOL-2-YLIDINEMETHYL]PYRIDINES AND RELATED COMPOUNDS AND THEIR USE 审中-公开
标题翻译： 2- [3H-噻唑-2-基]乙基]吡啶及其相关化合物及其用途
公开(公告)号：US20090247579A1
公开(公告)日：2009-10-01
申请号：US12280081
申请日：2007-02-21
申请人： Robert Brown , Jane Plumb , Gladys Wynne Aherne , Edward McDonald , Keith Jones , Stephen Hilton
发明人： Robert Brown , Jane Plumb , Gladys Wynne Aherne , Edward McDonald , Keith Jones , Stephen Hilton
IPC分类号： A61K31/4709 , A61K31/4439 , C07D417/06
CPC分类号： C07D513/04 , C07D417/06
摘要： The present invention pertains to certain 2-[3H-thiazol-2-ylidinemethyl]pyridine compounds and analogs thereof, which, inter alia, inhibit cell proliferation, treat cancer, etc., and more specifically to compounds of the following formula, wherein RA1, RA2, RA3, RA4, RB1, RB2, RNA, RNB, and X− are as defined herein: The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cell proliferation, and in the treatment of proliferative conditions such as cancer, etc.
摘要翻译：本发明涉及某些2- [3H-噻唑-2-基吡啶甲基]吡啶化合物及其类似物，其特别是抑制细胞增殖，治疗癌症等，更具体地涉及下式的化合物，其中RA1 RA2，RA3，RA4，RB1，RB2，RNA，RNB和X-如本文所定义：本发明还涉及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，抑制细胞增殖，以及治疗增殖性疾病如癌症等。

39. 发明申请

US20090042884A1 Pharmaceutical Compounds 失效
标题翻译：药物化合物
公开(公告)号：US20090042884A1
公开(公告)日：2009-02-12
申请号：US12089677
申请日：2006-10-11
申请人： Edward McDonald , Jonathan M. Large , Stephen J. Shuttleworth
发明人： Edward McDonald , Jonathan M. Large , Stephen J. Shuttleworth
IPC分类号： C07D413/04 , A61K31/5377 , C07D413/14 , A61P35/00 , A61P31/12 , A61P9/00 , A61P29/00 , A61P37/00 , A61P3/00
CPC分类号： C07D239/48 , C07D401/12 , C07D401/14 , C07D405/12
摘要： Pyrimidines of formula (I): wherein R1 to R4, X and Y are defined in the specification are inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behavior 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：式（I）的嘧啶：其中R1至R4，X和Y在本说明书中定义为PI3K的抑制剂，因此可用于治疗与PI3激酶例如癌症相关的异常细胞生长，功能或行为引起的疾病和障碍，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍和神经障碍。

40. 发明申请

US20070054909A1 VLA-4 inhibitor compounds 审中-公开
公开(公告)号：US20070054909A1
公开(公告)日：2007-03-08
申请号：US11594432
申请日：2006-11-08
申请人： John Baldwin , Edward McDonald , Kevin Moriarty , Christopher Sarko , Nobuo Machinaga , Atsushi Nakayama , Jun Chiba , Shin Iimura , Yoshiyuki Yoneda
发明人： John Baldwin , Edward McDonald , Kevin Moriarty , Christopher Sarko , Nobuo Machinaga , Atsushi Nakayama , Jun Chiba , Shin Iimura , Yoshiyuki Yoneda
IPC分类号： A61K31/5375 , A61K31/496 , A61K31/4439 , A61K31/426 , A61K31/401 , A61K31/405 , C07D403/02
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.

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