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31. 发明申请

US20100234374A1 Heterocycle Substituted Ketone Derivatives as Histone Deacetylase (HDAC) Inhibitors 有权
标题翻译：杂环取代酮衍生物作为组蛋白脱乙酰酶（HDAC）抑制剂
公开(公告)号：US20100234374A1
公开(公告)日：2010-09-16
申请号：US12086812
申请日：2006-12-21
申请人： Philip Jones , Jesus Maria Ontoria Ontoria , Rita Scarpelli , Raffaele Ingenito , Carsten Schultz-Fademrecht
发明人： Philip Jones , Jesus Maria Ontoria Ontoria , Rita Scarpelli , Raffaele Ingenito , Carsten Schultz-Fademrecht
IPC分类号： A61K31/4164 , C07D233/64 , A61K31/4172 , C07D401/06 , A61K31/4439 , C07D403/06 , A61K31/496 , C07D401/12 , A61K31/4709 , A61K31/454 , C07D417/12 , A61K31/427 , C07D413/12 , A61K31/5377 , C07D403/12 , A61K31/4196 , A61P35/00 , A61P25/28 , A61P25/00 , A61P25/18 , A61P29/00 , A61P37/02 , A61P9/10 , A61P9/00 , A61P11/06 , A61P3/10
CPC分类号： C07D233/64 , C07D401/12
摘要： The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts and tautomers thereof. Compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. They are also useful for treating neurodegenerative diseases, mental retardation, schizophrenia, inflammatory diseases, restenosis, immune disorders, diabetes, cardiovascular disorders and asthma.
摘要翻译：本发明涉及式（I）的化合物及其药学上可接受的盐和互变异构体。本发明化合物是组蛋白脱乙酰酶（HDAC）的抑制剂，可用于治疗包括癌症在内的细胞增殖性疾病。它们也可用于治疗神经变性疾病，精神发育迟滞，精神分裂症，炎性疾病，再狭窄，免疫疾病，糖尿病，心血管疾病和哮喘。

32. 发明申请

US20090253681A1 HIV Integrase Inhibitors 有权
标题翻译： HIV整合酶抑制剂
公开(公告)号：US20090253681A1
公开(公告)日：2009-10-08
申请号：US11887305
申请日：2006-03-22
申请人： Vincenzo Summa , Paola Pace , Philip Jones , Alessia Petrocchi , Maria del Rosario Rico Ferreira , Giuseppe Cecere
发明人： Vincenzo Summa , Paola Pace , Philip Jones , Alessia Petrocchi , Maria del Rosario Rico Ferreira , Giuseppe Cecere
IPC分类号： A61K31/554 , C07D498/04 , A61K31/553 , A61P31/18
CPC分类号： C07D487/04 , C07D487/14 , C07D513/04 , C07D513/14
摘要： Compounds of Formula I are inhibitors of FHV integrase and inhibitors of FHV replication (I), wherein m, n, X, R1, R2, R3, R4, R5, R6, R7; R8, R9 and R10 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HTV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HTV infection and ADDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译：式I化合物是FHV整合酶的抑制剂和FHV复制抑制剂（I），其中m，n，X，R 1，R 2，R 3，R 4，R 5，R 6，R 7; R8，R9和R10在本文中定义。该化合物可用于预防或治疗HTV感染以及预防，治疗或延迟AIDS发病。该化合物用于抗HTV感染和ADDS作为化合物本身或以药学上可接受的盐的形式。化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

33. 发明申请

US20090156591A1 Thiophene and Thiazole Substituted trifluoroethanone Derivatives as Histone Deacetylase (Hdac) Inhibitors 有权
标题翻译：噻吩和噻唑取代的三氟乙酮衍生物作为组蛋白脱乙酰酶（Hdac）抑制剂
公开(公告)号：US20090156591A1
公开(公告)日：2009-06-18
申请号：US11991576
申请日：2006-09-05
申请人： Federica Ferrigno , Philip Jones , Ester Muraglia , Jesus Maria Ontoria Ontoria , Rita Scarpelli
发明人： Federica Ferrigno , Philip Jones , Ester Muraglia , Jesus Maria Ontoria Ontoria , Rita Scarpelli
IPC分类号： A61K31/47 , C07D409/02 , C07D417/02 , C07D265/30 , A61K31/496 , A61K31/5375 , A61P25/18 , A61P25/28
CPC分类号： C07D409/08 , C07D277/56 , C07D333/34 , C07D333/38 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D487/08 , C07D491/10 , C07D495/04 , C12Q1/34
摘要： The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt or stereoisomer thereof. The compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐或立体异构体。本发明的化合物是组蛋白脱乙酰酶（HDAC）的抑制剂，可用于治疗包括癌症在内的细胞增殖性疾病。此外，本发明的化合物可用于治疗神经变性疾病，精神分裂症和中风等疾病。

34. 发明申请

US20090076101A1 Thiophene and Thiazole Substituted Trifluoroethanone Derivatives as Histone Deacetylase (HDAC) Inhibitors 有权
标题翻译：噻吩和噻唑取代三氟乙酮衍生物作为组蛋白脱乙酰酶（HDAC）抑制剂
公开(公告)号：US20090076101A1
公开(公告)日：2009-03-19
申请号：US12223943
申请日：2007-02-14
申请人： Federica Ferrigno , Philip Jones , Ester Muraglia , Jesus Maria Ontoria Ontoria , Rita Scarpelli , Carsten Schultz-Fademrecht
发明人： Federica Ferrigno , Philip Jones , Ester Muraglia , Jesus Maria Ontoria Ontoria , Rita Scarpelli , Carsten Schultz-Fademrecht
IPC分类号： A61K31/426 , C07D333/28 , A61K31/381 , A61P11/00 , A61P3/00 , A61P25/00 , A61P29/00 , C07D277/20
CPC分类号： C07D333/22 , C07D409/04 , C07D413/04 , C07D417/04
摘要： The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts and tautomers thereof. Compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. They are also useful for treating neurodegenerative diseases, mental retardation, 10 schizophrenia, inflammatory diseases, restenosis, immune disorders, diabetes, cardiovascular disorders and asthma.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐和互变异构体。本发明化合物是组蛋白脱乙酰酶（HDAC）的抑制剂，可用于治疗包括癌症在内的细胞增殖性疾病。它们也可用于治疗神经变性疾病，精神发育迟滞，10精神分裂症，炎性疾病，再狭窄，免疫疾病，糖尿病，心血管疾病和哮喘。

35. 发明申请

US20090054448A1 Amino Acid Derivatives as Histone Deacetylase (HDAC) Inhibitors 审中-公开
标题翻译：氨基酸衍生物作为组蛋白脱乙酰酶（HDAC）抑制剂
公开(公告)号：US20090054448A1
公开(公告)日：2009-02-26
申请号：US11991579
申请日：2006-09-05
申请人： Philip Jones
发明人： Philip Jones
IPC分类号： A61K31/16 , C07D209/18 , C07D263/58 , C07D213/75 , C07D277/28 , C07D333/22 , C07D233/26 , C07D401/02 , C07D417/02 , A61K31/495 , A61K31/4709 , A61K31/47 , A61K31/427 , A61K31/426 , A61K31/381 , A61K31/423 , A61P25/18 , A61P25/28 , A61P9/10 , A61K31/27
CPC分类号： C07D263/58 , C07C323/60 , C07C2601/08 , C07D207/06 , C07D209/18 , C07D211/58 , C07D211/62 , C07D213/75 , C07D213/82 , C07D215/12 , C07D231/14 , C07D233/90 , C07D241/44 , C07D257/04 , C07D277/28 , C07D295/13 , C07D295/15 , C07D307/52 , C07D333/28 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts or stereoisomers thereof. The compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐或立体异构体。本发明化合物是组蛋白脱乙酰酶（HDAC）的抑制剂，可用于治疗包括癌症在内的细胞增殖性疾病。此外，本发明的化合物可用于治疗神经变性疾病，精神分裂症和中风等疾病。

36. 发明授权

US07482457B2 Substituted quinoline-4-carboxylic hydrazides as NK-2/NK-3 receptor ligands 失效
标题翻译：取代的喹啉-4-羧酸酰肼作为NK-2 / NK-3受体配体
公开(公告)号：US07482457B2
公开(公告)日：2009-01-27
申请号：US10544440
申请日：2004-02-03
申请人： Mark Stuart Chambers , Philip Jones , Angus Murray MacLeod
发明人： Mark Stuart Chambers , Philip Jones , Angus Murray MacLeod
IPC分类号： C07D215/38
CPC分类号： C07D215/52
摘要： The present invention discloses a compound of formula (I): wherein: R1 is an aryl or heteroaryl ring; R2 is hydroxy, C1-6 alkoxy, C1-6 alkyl, amino, NR′R″ or C1-6 alkyl-NR′R″ where R′ and R″ are independently chosen from hydrogen and C1-4 alkyl and where R′ and R″, together with the nitrogen atom to which they are attached, form a saturated nitrogen-containing 3-7 membered heterocycle optionally containing a further nitrogen atom and optionally substituted by NR′R″ as defined above or R2 is C1-6 alkoxy substituted by NR′R″ as defined above; R3 is hydrogen or C1-6 alkyl; R4 is hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, aryl or aryl C1-6 alkyl; R5 is hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, aryl, aryl C1-6 alkyl or C1-6 alkoxycarbonyl; or R4 and R5, together with the nitrogen atom to which they are attached, form a C3-C10 mono- or bicyclic saturated ring; X and Y are independently chosen from hydrogen, hydroxy, nitro, amino, cyano, CF3, halogen and C1-4 alkyl; or a pharmaceutically acceptable salt thereof; as NK-2/NK-3 ligands for treating schizophrenia, COPD, asthma or irritable bowel syndrome.
摘要翻译：本发明公开了式（I）的化合物：其中：R1是芳基或杂芳基环; R 2是羟基，C 1-6烷氧基，C 1-6烷基，氨基，NR'R“或C 1-6烷基-NR'R”，其中R'和R“独立地选自氢和C 1-4烷基，其中R'和R“与它们所连接的氮原子一起形成任选含有另外的氮原子并且任选地被如上所定义的NR'R”取代的饱和含氮3-7元杂环或R2 是由如上定义的NR'R“取代的C 1-6烷氧基; R3是氢或C1-6烷基; R4是氢，C1-8烷基，C2-8烯基，C2-8炔基，C3-8环烷基，芳基或芳基C1-6烷基; R5是氢，C1-8烷基，C2-8烯基，C2-8炔基，C3-8环烷基，芳基，芳基C1-6烷基或C1-6烷氧基羰基; 或R 4和R 5与它们所连接的氮原子一起形成C 3 -C 10单环或双环饱和环; X和Y独立地选自氢，羟基，硝基，氨基，氰基，CF 3，卤素和C 1-4烷基; 或其药学上可接受的盐; 作为用于治疗精神分裂症，COPD，哮喘或肠易激综合征的NK-2 / NK-3配体。

37. 发明授权

US07153868B2 N-(3-(4-substituted-1-piperidinyl)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists 失效
标题翻译： N-（3-（4-取代-1-哌啶基）-1-苯基丙基）取代的磺酰胺作为NK-3受体拮抗剂
公开(公告)号：US07153868B2
公开(公告)日：2006-12-26
申请号：US10417360
申请日：2003-04-16
申请人： Mark Stuart Chambers , Philip Jones , Helen Jane Szekeres
发明人： Mark Stuart Chambers , Philip Jones , Helen Jane Szekeres
IPC分类号： A61K31/445 , C07D401/06
CPC分类号： C07D401/04 , A61K31/454 , A61K31/497 , C07D211/58 , C07D401/14 , C07D409/14
摘要： The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a compound of formula I: wherein, generally, Q is R1 is benzyl, phenyl, thiophene or imidazolyl optionally substituted with C1-4alkyl or halogen, such as methyl, fluorine or bromine; R2 is hydrogen or C1-4alkyl such as methyl; R3 is phenyl; R4 is hydrogen; R5 is hydrogen or C1-6alkylcarbonyl such as methylcarbonyl; X is —SO2— or —C(O)N(R2)SO2— where R2 is preferably hydrogen; Y is a bond, CH2 or Z1 where Z1 is —N(Rf)— in which Rf is C1-6alkylcarbonyl such as ethylcarbonyl; and R6 is phenyl, pyrazolyl, pyridyl, pyrimidinyl or benzimidazolonyl optionally substituted with one or two groups chosen from C1-6alkyl and benzyl, such as methyl, ethyl and benzyl; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供治疗患有诸如精神分裂症的受试者的方法，所述疾病包括施用NK-3拮抗剂，其包括向该受试者施用治疗有效量的式I化合物：其中通常，Q是R 1是苄基，苯基，噻吩或任选被C 1-4烷基或卤素取代的咪唑基，例如甲基，氟或溴; R 2是氢或C 1-4烷基，例如甲基; R 3是苯基; R 4是氢; R 5是氢或C 1-6烷基羰基，例如甲基羰基; X是-SO 2 - 或-C（O）N（R 2）SO 2 - ，其中R 2 O / >优选为氢; Y是键，CH 2或Z 1，其中Z 1是-N（R f）， - 其中R 1是C 1-6烷基羰基，例如乙基羰基; R 6是苯基，吡唑基，吡啶基，嘧啶基或苯并咪唑烷基，任选地被一个或两个选自C 1-6烷基和苄基的基团取代，例如甲基，乙基和苄基; 或其药学上可接受的盐。

38. 发明申请

US20060264474A1 Pyrazole derivatives as gamma-secretase inhibitors useful in the treatment of alzheimer's disease 失效
标题翻译：吡唑衍生物作为可用于治疗阿尔茨海默病的γ-分泌酶抑制剂
公开(公告)号：US20060264474A1
公开(公告)日：2006-11-23
申请号：US10549226
申请日：2004-04-01
申请人： Michela Bettati , Mark Chambers , Peter Hunt , Philip Jones , Angus MacLeod , Helen Szekeres , Martin Teall
发明人： Michela Bettati , Mark Chambers , Peter Hunt , Philip Jones , Angus MacLeod , Helen Szekeres , Martin Teall
IPC分类号： A61K31/4545 , A61K31/4439 , A61K31/4152 , C07D403/04
CPC分类号： C07D231/12 , C07D401/04 , C07D401/06 , C07D409/12
摘要： The compounds of formula (I): inhibit gamma-secretase and hence are of utility in the treatment or prevention of Alzheimer's disease.
摘要翻译：式（I）化合物：抑制γ-分泌酶，因此可用于治疗或预防阿尔茨海默氏病。

39. 发明申请

US20060136266A1 Medicinal product order processing system 审中-公开
标题翻译：药品订单处理系统
公开(公告)号：US20060136266A1
公开(公告)日：2006-06-22
申请号：US11015735
申请日：2004-12-20
申请人： Lionel Tarassenko , Neil Townsend , Philip Jones
发明人： Lionel Tarassenko , Neil Townsend , Philip Jones
IPC分类号： G06F19/00
CPC分类号： G06Q50/24 , G06F19/328 , G06Q10/087 , G16H10/60
摘要： A repeat prescription ordering system for allowing patients requiring resupply of medication or medical products to access a server using a portable communications and data processing device such as a smart phone or personal digital assistant. The server supplies to the patient a list of medication and medical products which they are authorized to order. The patient can select the products required, and the order is logged by the server and allocated to a supplier for completion of the order. The server maintains an estimate of the amount of medication or medical product held by the patient, this being based on the prescribed dosage regimen and information entered by the patient on their usage and, optionally, on checks on their own health. The patient may be alerted when the estimate indicates that their supplies are running low. The estimate is allowed to go below zero, this implying a possible departure from the prescribed medication regimen.
摘要翻译：一种重复的处方订购系统，用于允许需要补充药物或医疗产品的患者使用诸如智能电话或个人数字助理的便携式通信和数据处理设备访问服务器。服务器向患者提供他们有权订购的药物和医疗产品清单。患者可以选择所需的产品，服务器记录订单并分配给供应商以完成订单。服务器维持对患者持有的药物或医疗产品的量的估计，这是基于规定的剂量方案和由患者输入的用于其使用的信息，并且可选地基于对自身健康的检查。当估计表明他们的供应量很低时，可能会提醒病人。估计允许低于零，这意味着可能会偏离规定的药物治疗方案。

40. 发明申请

US20060125248A1 Door locking mechanism 审中-公开
标题翻译：门锁机构
公开(公告)号：US20060125248A1
公开(公告)日：2006-06-15
申请号：US10521039
申请日：2003-07-11
申请人： Peter Heeley , Philip Jones
发明人： Peter Heeley , Philip Jones
IPC分类号： E05B3/00
CPC分类号： E05B13/106 , E05B3/06 , E05B3/065 , E05B15/0053 , Y10T292/57
摘要： The locking mechanism includes a lever handle having a fluted passageway for fitting to an adjacent end of a latch spindle. The passageway allows the handle to turn relatively to the latch spindle in opposite directions through a predetermined angle of movement. At one end of this angle of movement, the handle is in a horizontal rest position and is engageable with the latch spindle for turning the spindle in a direction to withdraw the latch bolt from its latching position, and at the opposite end, the handle is in a lifted locking position and is engageable with the spindle to prohibit turning thereof in the opening direction. At the locking position, a locking member slidably mounted in the handle and controlled by a trigger part, extending behind the lever part of the handle is engageable in one of a pair of retainer holes depending on the handing of the lever handle.
摘要翻译：锁定机构包括杠杆手柄，其具有用于配合到闩锁心轴的相邻端的凹槽通道。通道允许手柄相对于锁定主轴在相反方向上转动一预定的移动角度。在该移动角度的一端，手柄处于水平静止位置，并且可与闩锁主轴接合，用于使主轴转动以将闩锁闩锁从其闩锁位置撤回，并且在相对端处，手柄是处于提升的锁定位置并且可与主轴接合以禁止其在打开方向上的转动。在锁定位置，可滑动地安装在手柄中并由触发器部分控制的锁定构件可以在手柄的杠杆部分的后面延伸，这可以根据杠杆手柄的处理而接合在一对保持孔中的一个中。

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