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51. 发明授权

US08080573B2 Heterocycle substituted amide and sulfur amide derivatives as histone deacetylase (hdac) inhibitors 有权
标题翻译：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：US08080573B2
公开(公告)日：2011-12-20
申请号：US12084269
申请日：2006-10-26
申请人： Philip Jones , Jesus Maria Ontoria Ontoria
发明人： Philip Jones , Jesus Maria Ontoria Ontoria
IPC分类号： A61K31/4164 , C07D233/54
CPC分类号： C07D403/12 , C07D233/64 , C07D409/14
摘要： 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.
摘要翻译：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。

52. 发明授权

US08071623B2 Amide substituted indazoles as poly(ADP-ribose)polymerase(PARP) inhibitors 有权
标题翻译：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
申请人： Philip Jones , Jesus Maria Ontoria Ontoria , Rita Scarpelli , Carsten Schultz-Fademrecht
发明人： Philip Jones , Jesus Maria Ontoria Ontoria , Rita Scarpelli , Carsten Schultz-Fademrecht
IPC分类号： A61K31/445 , C07D231/56
CPC分类号： C07D401/10 , A61K31/4439
摘要： 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.
摘要翻译：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。

53. 发明申请

US20110183989A1 SATURATED BICYCLIC HETEROCYCLIC DERIVATIVES AS SMO ANTAGONISTS 有权
标题翻译：饱和双环杂环衍生物作为SMO拮抗剂
公开(公告)号：US20110183989A1
公开(公告)日：2011-07-28
申请号：US13060718
申请日：2009-08-28
申请人： Danila Branca , Federica Ferrigno , Jose Ignacio Martin Hernando , Philip Jones , Olaf Kinzel , Savina Malancona , Ester Muraglia , Maria Cecilia Palumbi , Giovanna Pescatore , Rita Scarpelli
发明人： Danila Branca , Federica Ferrigno , Jose Ignacio Martin Hernando , Philip Jones , Olaf Kinzel , Savina Malancona , Ester Muraglia , Maria Cecilia Palumbi , Giovanna Pescatore , Rita Scarpelli
IPC分类号： A61K31/4985 , C07D487/04 , A61P35/00
CPC分类号： C07D487/04
摘要： 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.
摘要翻译：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

54. 发明申请

US20110053911A1 TRICYCLIC DERIVATIVES AS INHIBITORS OF POLY(ADP-RIBOSE) POLYMERASE (PARP) 失效
标题翻译：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
申请人： Raffaele Ingenito , Philip Jones , Laura Llauger Bufi , Jesus Maria Ontoria Ontoria , Rita Scarpelli
发明人： Raffaele Ingenito , Philip Jones , Laura Llauger Bufi , Jesus Maria Ontoria Ontoria , Rita Scarpelli
IPC分类号： 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分类号： C07D471/06 , C07D471/16
摘要： 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.
摘要翻译：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。

55. 发明授权

US07799825B2 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：US07799825B2
公开(公告)日：2010-09-21
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： A61K31/381 , C07D333/04
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。

56. 发明申请

US20100081792A1 Ligand 审中-公开
标题翻译：配体
公开(公告)号：US20100081792A1
公开(公告)日：2010-04-01
申请号：US11981821
申请日：2007-10-31
申请人： 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
发明人： 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分类号： C07K16/00
CPC分类号： 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
摘要： 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.
摘要翻译：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。

57. 发明申请

US20090156619A1 Heterocycle Substituted Amide and Sulfur Amide Derivatives as Histone Deacetylase (HDAC) Inhibitors 有权
标题翻译：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
申请人： Philip Jones , Jesus Maria Ontoria Ontoria
发明人： Philip Jones , Jesus Maria Ontoria Ontoria
IPC分类号： A61K31/517 , A61K31/4172 , A61K31/4178 , C07D403/12 , C07D233/64 , A61P25/18 , A61P7/12 , A61P11/06 , A61K31/4439
CPC分类号： C07D403/12 , C07D233/64 , C07D409/14
摘要： 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.
摘要翻译：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。

58. 发明申请

US20090148434A1 Antibody Compositions and Methods 审中-公开
标题翻译：抗体组合物和方法
公开(公告)号：US20090148434A1
公开(公告)日：2009-06-11
申请号：US12186281
申请日：2008-08-05
申请人： Ian Tomlinson , Amrik Basran , Philip Jones
发明人： Ian Tomlinson , Amrik Basran , Philip Jones
IPC分类号： A61K39/395 , C07K16/18
CPC分类号： 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
摘要： 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.
摘要翻译：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。

59. 发明申请

US20080167345A1 Amide substituted indazoles as poly(ADP-ribose)polymerase(PARP) inhibitors 有权
标题翻译：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
申请人： Philip Jones , Jesus Maria Ontoria Ontoria , Rita Scarpelli , Carsten Schultz-Fademrecht
发明人： Philip Jones , Jesus Maria Ontoria Ontoria , Rita Scarpelli , Carsten Schultz-Fademrecht
IPC分类号： C07D401/10 , A61K31/4525 , A61P13/12 , A61P9/00 , A61P3/00 , A61P25/00 , A61P27/00 , A61P35/00 , A61P37/00
CPC分类号： C07D401/10 , A61K31/4439
摘要： 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.
摘要翻译：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。

60. 发明申请

US20070117847A1 N-(3-(4-Substituted-1-piperiding1)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists 审中-公开
标题翻译： N-（3-（4-取代-1-哌啶-1-基）-1-苯基丙基）取代磺酰胺作为NK-3受体拮抗剂
公开(公告)号：US20070117847A1
公开(公告)日：2007-05-24
申请号：US11635942
申请日：2006-12-08
申请人： Mark Chambers , Philip Jones , Helen Szekeres
发明人： Mark Chambers , Philip Jones , Helen Szekeres
IPC分类号： A61K31/454 , C07D409/14
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。

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