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91.发明授权Amide substituted indazoles as poly(ADP-ribose)polymerase(PARP) inhibitors 有权酰胺取代的吲唑作为聚（ADP-核糖）聚合酶（PARP）抑制剂公开(公告)号：US08071623B2
公开(公告)日：2011-12-06
申请号：US12006993
申请日：2008-01-08
Applicant: Philip Jones , Jesus Maria Ontoria Ontoria , Rita Scarpelli , Carsten Schultz-Fademrecht
IPC: A61K31/445 , C07D231/56
CPC classification number: C07D401/10 , A61K31/4439
Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts, stereoisomers or tautomers thereof which are inhibitors of poly (ADP-ribose) polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes, neurodegenerative diseases, retroviral infection, retinal damage or skin senescence and UV-induced skin damage, and as chemo- and/or radiosensitizers for cancer treatment.
Abstract translation: 本发明涉及式I化合物及其药学上可接受的盐，立体异构体或互变异构体，其是聚（ADP-核糖）聚合酶（PARP）的抑制剂，因此可用于治疗癌症，炎性疾病，再灌注损伤，缺血性疾病 ，中风，肾衰竭，心血管疾病，心血管疾病以外的血管疾病，糖尿病，神经变性疾病，逆转录病毒感染，视网膜损伤或皮肤衰老以及UV诱导的皮肤损伤，以及用作癌症治疗的化学和/或放射增敏剂。
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公开(公告)号：US20110183989A1
公开(公告)日：2011-07-28
申请号：US13060718
申请日：2009-08-28
Applicant: Danila Branca , Federica Ferrigno , Jose Ignacio Martin Hernando , Philip Jones , Olaf Kinzel , Savina Malancona , Ester Muraglia , Maria Cecilia Palumbi , Giovanna Pescatore , Rita Scarpelli
Inventor： Danila Branca , Federica Ferrigno , Jose Ignacio Martin Hernando , Philip Jones , Olaf Kinzel , Savina Malancona , Ester Muraglia , Maria Cecilia Palumbi , Giovanna Pescatore , Rita Scarpelli
IPC: A61K31/4985 , C07D487/04 , A61P35/00
CPC classification number: C07D487/04
Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of the Sonic Hedgehog pathway, in particular Smoantagonists. Thus the compounds of this invention are useful for the treatment of diseases associated with abnormal hedgehog pathway activation, including cancer, for example basal cell carcinoma, medulloblastoma, prostate, pancreatic, breast, colon, bone and small cell lung cancers, and cancers of the upper GI tract.
Abstract translation: 本发明涉及式I化合物及其药学上可接受的盐或互变异构体，其是Sonic Hedgehog途径的抑制剂，特别是Smoantagonists。 因此，本发明的化合物可用于治疗与异常hedgehog途径活化相关的疾病，包括癌症，例如基底细胞癌，成神经管细胞瘤，前列腺，胰腺癌，乳腺癌，结肠癌，骨细胞和小细胞肺癌，以及癌症 上胃肠道
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93.发明申请TRICYCLIC DERIVATIVES AS INHIBITORS OF POLY(ADP-RIBOSE) POLYMERASE (PARP) 失效作为聚（ADP-RIBOSE）聚合酶（PARP）的抑制剂的三聚衍生物公开(公告)号：US20110053911A1
公开(公告)日：2011-03-03
申请号：US12922270
申请日：2009-03-13
Applicant: Raffaele Ingenito , Philip Jones , Laura Llauger Bufi , Jesus Maria Ontoria Ontoria , Rita Scarpelli
Inventor： Raffaele Ingenito , Philip Jones , Laura Llauger Bufi , Jesus Maria Ontoria Ontoria , Rita Scarpelli
IPC: A61K31/55 , C07D471/16 , C07D487/06 , A61K31/4375 , A61K31/551 , A61K31/438 , A61P35/00 , A61P9/10 , A61P29/00 , A61P3/10 , A61P9/00 , A61P27/02 , A61P17/00
CPC classification number: C07D471/06 , C07D471/16
Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment.
Abstract translation: 本发明涉及作为聚（ADP-核糖）聚合酶（PARP）的抑制剂的式（I）化合物及其药学上可接受的盐或互变异构体，因此可用于治疗癌症，炎性疾病，再灌注损伤，缺血状况， 中风，肾衰竭，心血管疾病，心血管疾病以外的血管疾病，糖尿病，神经变性疾病，逆转录病毒感染，视网膜损伤，皮肤衰老和紫外线诱发的皮肤损伤，以及用于癌症治疗的化学或放射增敏剂。
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94.发明申请ANTIBACTERIAL FORMULATION COMPRISING A DIALKYL SULPHOSUCCINATE AND A CARBANILIDE ANTIBACTERIAL AGENT 审中-公开包含硫酸二乙酯和抗氧化剂抗菌剂的抗生素配方公开(公告)号：US20100273876A1
公开(公告)日：2010-10-28
申请号：US12600733
申请日：2008-06-02
Applicant: Scott Seville , Stephen Philip Jones , Daniel James Fitzgerald , Nayan N. Desai , Refika I. Pakunlu
Inventor： Scott Seville , Stephen Philip Jones , Daniel James Fitzgerald , Nayan N. Desai , Refika I. Pakunlu
IPC: A61K31/225 , A01N37/36 , A01P1/00 , A61P31/04 , A61P17/10
CPC classification number: A61K31/194 , A61K31/196 , A61K2300/00
Abstract: Antibacterial formulation containing (a) a dialkyl sulphosuccinate (DAS) or derivative thereof and (b) a carbanilide antibacterial agent such as triclocarban (TCC). The formulation may be for use in the treatment of a bacterial condition, in particular acne, body odour or a condition affecting the oral cavity. It may contain, in addition to the DAS and the carbanilide, (i) a poly-oxyalkylene-based solubilising agent; (ii) an organic solvent; (iii) a thickening agent; and (iv) water.
Abstract translation: 含有（a）二烷基磺基琥珀酸酯（DAS）或其衍生物和（b）碳酰苯胺抗菌剂如三氯卡班（TCC）的抗菌制剂。 该制剂可用于治疗细菌病症，特别是痤疮，体臭或影响口腔的病症。 除了DAS和碳酰苯胺之外，它还可以含有（i）聚氧化烯基增溶剂; （ii）有机溶剂; （iii）增稠剂; 和（iv）水。
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95.发明授权Thiophene and thiazole substituted trifluoroethanone derivatives as histone deacetylase (HDAC) inhibitors 有权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：US07799825B2
公开(公告)日：2010-09-21
申请号：US12223943
申请日：2007-02-14
Applicant: Federica Ferrigno , Philip Jones , Ester Muraglia , Jesus Maria Ontoria Ontoria , Rita Scarpelli , Carsten Schultz-Fademrecht
Inventor： Federica Ferrigno , Philip Jones , Ester Muraglia , Jesus Maria Ontoria Ontoria , Rita Scarpelli , Carsten Schultz-Fademrecht
IPC: A61K31/381 , C07D333/04
CPC classification number: C07D333/22 , C07D409/04 , C07D413/04 , C07D417/04
Abstract: 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.
Abstract translation: 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。
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Patent Agency Ranking
公开(公告)号：US20100081792A1
公开(公告)日：2010-04-01
申请号：US11981821
申请日：2007-10-31
Applicant: Steven Grant , Amrik Basran , Olga Ignatovich , Rudolph Maria T. De Wildt , Philip Jones , Neil Brewis , Ben Woolven , Elena De Angelis , Lucy J. Holt , Greg Winter , Ian Tomlinson , Kevin Moulder
Inventor： Steven Grant , Amrik Basran , Olga Ignatovich , Rudolph Maria T. De Wildt , Philip Jones , Neil Brewis , Ben Woolven , Elena De Angelis , Lucy J. Holt , Greg Winter , Ian Tomlinson , Kevin Moulder
IPC: C07K16/00
CPC classification number: C07K16/468 , A61K47/60 , A61K2039/505 , C07K14/415 , C07K16/18 , C07K16/22 , C07K16/241 , C07K16/2866 , C07K2317/21 , C07K2317/31 , C07K2317/34 , C07K2317/52 , C07K2317/522 , C07K2317/55 , C07K2317/569 , C07K2317/622 , C07K2319/00
Abstract: The invention provides a dual-specific ligand comprising a first and second single variable domain, each having binding specificity for a antigenic target. The invention also provides for a single variable domain monomer ligand that specifically binds to an antigenic target.
Abstract translation: 本发明提供了双特异性配体，其包含第一和第二单可变结构域，每一结构域对抗原靶具有结合特异性。 本发明还提供了与抗原靶特异性结合的单个可变域单体配体。
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97.发明申请Heterocycle Substituted Amide and Sulfur Amide Derivatives as Histone Deacetylase (HDAC) Inhibitors 有权杂环取代的酰胺和硫酰胺衍生物作为组蛋白脱乙酰酶（HDAC）抑制剂公开(公告)号：US20090156619A1
公开(公告)日：2009-06-18
申请号：US12084269
申请日：2006-10-26
Applicant: Philip Jones , Jesus Maria Ontoria Ontoria
Inventor： Philip Jones , Jesus Maria Ontoria Ontoria
IPC: A61K31/517 , A61K31/4172 , A61K31/4178 , C07D403/12 , C07D233/64 , A61P25/18 , A61P7/12 , A61P11/06 , A61K31/4439
CPC classification number: C07D403/12 , C07D233/64 , C07D409/14
Abstract: The present invention related to compounds of formula (I): or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof. Compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative diseases, including cancer. Compounds of the present invention are useful for treating or preventing neurodegenerative diseases, schizophrenia and stroke among other diseases.
Abstract translation: 本发明涉及式（I）化合物：或其药学上可接受的盐，立体异构体或互变异构体。 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。 本发明的化合物可用于治疗或预防神经变性疾病，精神分裂症和中风等疾病。
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公开(公告)号：US20090148434A1
公开(公告)日：2009-06-11
申请号：US12186281
申请日：2008-08-05
Applicant: Ian Tomlinson , Amrik Basran , Philip Jones
Inventor： Ian Tomlinson , Amrik Basran , Philip Jones
IPC: A61K39/395 , C07K16/18
CPC classification number: C07K16/005 , A61K47/60 , A61K2039/505 , C07K16/18 , C07K16/241 , C07K16/2875 , C07K16/2878 , C07K16/40 , C07K16/468 , C07K2317/21 , C07K2317/31 , C07K2317/34 , C07K2317/56 , C07K2317/567 , C07K2317/569 , C07K2317/70 , C07K2317/76 , C07K2317/92 , C07K2317/94 , C07K2319/00
Abstract: Provided are concentrated preparations comprising single immunoglobulin variable domain polypeptides that bind target antigen with high affinity and are soluble at high concentration, without aggregation or precipitation, providing, for example, for increased storage stability and the ability to administer higher therapeutic doses.
Abstract translation: 提供了包含单一免疫球蛋白可变结构域多肽的浓缩制剂，其以高亲和力结合靶抗原并且可以高浓度溶解，无聚集或沉淀，提供例如提高储存稳定性和施用较高治疗剂量的能力。
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99.发明申请Amide substituted indazoles as poly(ADP-ribose)polymerase(PARP) inhibitors 有权酰胺取代的吲唑作为聚（ADP-核糖）聚合酶（PARP）抑制剂公开(公告)号：US20080167345A1
公开(公告)日：2008-07-10
申请号：US12006993
申请日：2008-01-08
Applicant: Philip Jones , Jesus Maria Ontoria Ontoria , Rita Scarpelli , Carsten Schultz-Fademrecht
IPC: C07D401/10 , A61K31/4525 , A61P13/12 , A61P9/00 , A61P3/00 , A61P25/00 , A61P27/00 , A61P35/00 , A61P37/00
CPC classification number: C07D401/10 , A61K31/4439
Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts, stereoisomers or tautomers thereof which are inhibitors of poly (ADP-ribose) polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes, neurodegenerative diseases, retroviral infection, retinal damage or skin senescence and UV-induced skin damage, and as chemo- and/or radiosensitizers for cancer treatment.
Abstract translation: 本发明涉及式I化合物及其药学上可接受的盐，立体异构体或互变异构体，其是聚（ADP-核糖）聚合酶（PARP）的抑制剂，因此可用于治疗癌症，炎性疾病，再灌注损伤，缺血性疾病 ，中风，肾衰竭，心血管疾病，心血管疾病以外的血管疾病，糖尿病，神经变性疾病，逆转录病毒感染，视网膜损伤或皮肤衰老以及UV诱导的皮肤损伤，以及用作癌症治疗的化学和/或放射增敏剂。
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100.发明授权8-fluoroimidazo 1,2-a pyridine derivatives as ligands for GABA receptors 失效8-氟咪唑并[1,2-a]吡啶衍生物作为GABA受体的配体公开(公告)号：US07226926B2
公开(公告)日：2007-06-05
申请号：US10515165
申请日：2003-05-23
Applicant: Wesley Peter Blackaby , Jose Luis Castro Pineiro , Simon Charles Goodacre , David James Hallett , Alexander Charles Humphries , Philip Jones , Kevin John Merchant , Michael Reader
Inventor： Wesley Peter Blackaby , Jose Luis Castro Pineiro , Simon Charles Goodacre , David James Hallett , Alexander Charles Humphries , Philip Jones , Kevin John Merchant , Michael Reader
IPC: A61K31/437 , A61K31/506 , C07D544/294 , C07D546/121
CPC classification number: C07D471/04
Abstract: A class of 8-fluoroimidazo[1,2-α]pyridine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
Abstract translation: 一类由任选取代的五元或六元杂芳环在3-位被取代的8-氟咪唑并[1,2-α]吡啶衍生物，是GABA A A受体的选择性配体 特别是对α2和/或α3和/或α5亚基具有高亲和力，因此有益于治疗和/或预防中枢神经系统的不利条件，包括焦虑，抽搐和认知障碍。
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