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51. 发明专利

JP2014181234A Tofacitinib oral sustained release dosage forms 有权
标题翻译： TOFACITINIB口腔持续释放剂量形式
公开(公告)号：JP2014181234A
公开(公告)日：2014-09-29
申请号：JP2014045951
申请日：2014-03-10
申请人： Pfizer Inc , ファイザー・インク
发明人： HERBIG SCOTT MAX , SRIRAM KRISHNASWAMI , JOSEPH KUSHNER IV , MANISHA LAMBA , THOMAS C STOCK
IPC分类号： A61K31/519 , A61K9/22 , A61K31/40 , A61K45/00 , A61K47/10 , A61K47/14 , A61K47/26 , A61K47/32 , A61K47/34 , A61K47/36 , A61K47/38 , A61K47/44 , A61P1/04 , A61P3/10 , A61P5/14 , A61P9/10 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/28 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/06 , A61P37/08 , A61P43/00
CPC分类号： A61K31/519 , A61K9/0004 , A61K9/2018 , A61K9/2054 , A61K9/2086 , A61K9/2866 , A61K9/4891 , A61K31/40 , A61K45/06 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide oral sustained release compositions of tofacitinib for the treatment of inflammatory and auto-immune diseases, especially Rheumatoid Arthritis (RA).SOLUTION: The present invention relates to oral sustained release formulations of tofacitinib and pharmaceutical acceptable salts thereof. The formulations described herein have desirable pharmacokinetic characteristics.
摘要翻译：要解决的问题：提供tofacitinib的口服持续释放组合物用于治疗炎性和自身免疫性疾病，特别是类风湿关节炎（RA）。解决方案：本发明涉及tofacitinib的口服缓释制剂及其药学上可接受的盐。本文描述的制剂具有所需的药代动力学特征。

52. 发明专利

JP2013151511A Treatment of male sexual dysfunction 审中-公开
标题翻译：治疗男性性功能障碍
公开(公告)号：JP2013151511A
公开(公告)日：2013-08-08
申请号：JP2013038357
申请日：2013-02-28
申请人： Pfizer Inc , ファイザー・インク
发明人： NAYLOR ALASDAIR MARK , RUSSELL RACHEL JANE , STREET STEPHEN DEREK ALBERT , TANG KIM-WAH , VAN DER GRAAF PIETER HADEWIJN , WAYMAN CHRISTOPHER PETER
IPC分类号： A01K67/027 , A61K45/00 , A61K31/4545 , A61K31/495 , A61K38/11 , A61K45/06 , A61P15/00 , A61P43/00 , C07D295/22 , C07D295/26 , C07K14/72
CPC分类号： C07D295/26 , A61K31/495 , A61K45/06
摘要： PROBLEM TO BE SOLVED: To provide a compound and a pharmaceutical composition that are useful for the treatment and/or prevention of male sexual dysfunction, in particular ejaculatory disorders, such as premature ejaculation.SOLUTION: A composition contains a selective oxytocin antagonist for use in the treatment and/or prevention of a male ejaculatory disorder, which selective oxytocin antagonist is optionally admixed with a pharmaceutically acceptable carrier, diluent or excipient.
摘要翻译：要解决的问题：提供可用于治疗和/或预防男性性功能障碍，特别是射精性疾病例如早泄的化合物和药物组合物。解决方案：组合物含有选择性催产素拮抗剂，其用于治疗和/或预防男性射精障碍，该选择性催产素拮抗剂任选与药学上可接受的载体，稀释剂或赋形剂混合。

53. 发明专利

JP2013126979A Combination of inotuzumab ozogamicin and torisel for treatment of cancer 审中-公开
标题翻译：阿托单抗OZOGAMICIN和TORISEL联合治疗癌症
公开(公告)号：JP2013126979A
公开(公告)日：2013-06-27
申请号：JP2012273427
申请日：2012-12-14
申请人： Pfizer Inc , ファイザー・インク , Oncology Inst Of Southern Switzerland , オンコロジー・インスティチュート・オブ・サザン・スイッツランド
发明人： BRUEDERLE ANDREAS , MORAN PADRAIG , STATHIS ANASTASIOS
IPC分类号： A61K31/704 , A61K31/436 , A61K31/439 , A61P35/00 , A61P35/02 , A61P43/00
CPC分类号： A61K47/48407 , A61K31/436 , A61K31/704 , A61K39/39558 , A61K47/6809 , C07K16/2803 , C07K16/3061 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide a therapeutic method for the treatment of cancer.SOLUTION: A combination of inotuzumab ozogamicin (CMC-544) and temsirolimus is provided. The enhanced antitumor of the combination therapy is particularly useful for patient population that are recalcitrant to inotuzumab ozogamicin or temsirolimus therapy, relapse after treatment with inotuzumab ozogamicin or temsirolimus, where enhanced antitumor effect reduces toxicities associated with treatment using inotuzumab ozogamicin or temsirolimus.
摘要翻译：待解决的问题：提供治疗癌症的治疗方法。解决方案：提供了奥妥珠单抗奥佐霉素（CMC-544）和替西罗莫司的组合。联合治疗的增强抗肿瘤药物对于不利于阿托珠单抗奥佐霉素或替西罗莫司治疗的患者群体特别有用，其中使用阿托珠单抗奥佐霉素或替西罗莫司治疗后复发，其中增强的抗肿瘤作用降低与使用阿托单抗奥佐霉素或替西罗莫司治疗相关的毒性。版权所有（C）2013，JPO＆INPIT

54. 发明专利

JP2013100281A Method for treating inflammatory disorder using anti-m-csf antibody 审中-公开
标题翻译：使用抗M-CSF抗体治疗炎症性疾病的方法
公开(公告)号：JP2013100281A
公开(公告)日：2013-05-23
申请号：JP2012244623
申请日：2012-11-06
申请人： Pfizer Inc , ファイザー・インク
发明人： BEEBE JEAN ELIZABETH , BEIDLER DAVID , COMER GAIL , DIEHL ANNETTE , DUNUSSI-JOANNOPOULOS KYRIAKI , FOGEL ROBERT , GUAY HEATH M , HEGEN MARTIN , HONCZARENKO MAREK , O'TOOLE MARGOT MARY , REDDY PADMALATHA SUNKARA , SRIDHARAN SUDHAKAR , VON SCHACK DAVID JOHANNES , YOUNG DEBORAH ANN
IPC分类号： A61K39/395 , A61P13/12 , A61P17/00 , A61P37/02 , C07K16/24 , C12N15/09
CPC分类号： C07K16/243 , A61K2039/505 , C07K2317/21 , C07K2317/56 , C07K2317/73 , C07K2317/76 , C07K2317/92 , C07K2317/94
摘要： PROBLEM TO BE SOLVED: To provide a therapeutic M-CSF antibody for inhibiting M-CSF activity.SOLUTION: There are provided uses of antibodies and antigen-binding portions thereof which specifically bind to an M-CSF, preferably human M-CSF, and that function to inhibit an M-CSF. There are also provided human anti-M-CSF antibodies and antigen-binding portions thereof. Moreover, antibodies which are chimeric, bispecific, derivatized, single chain antibodies or portions of fusion proteins are provided. Furthermore, isolated heavy and light chain immunoglobulins derived from human anti-M-CSF antibodies and nucleic acid molecules encoding such immunoglobulins are provided. The invention relates to methods of making human anti-M-CSF antibodies, compositions comprising these antibodies and methods of using the antibodies and compositions for diagnosis and treatment. The invention also relates to gene therapy methods using nucleic acid molecules encoding the heavy and/or light immunoglobulin molecules that comprise the human anti-M-CSF antibodies.
摘要翻译：待解决的问题：提供用于抑制M-CSF活性的治疗性M-CSF抗体。解决方案：提供了特异性结合M-CSF，优选人M-CSF的抗体及其抗原结合部分的用途，并且其功能是抑制M-CSF。还提供人抗M-CSF抗体及其抗原结合部分。此外，提供了嵌合，双特异性，衍生化，单链抗体或融合蛋白部分的抗体。此外，提供衍生自人抗M-CSF抗体的分离的重链和轻链免疫球蛋白和编码这种免疫球蛋白的核酸分子。本发明涉及制备人抗M-CSF抗体的方法，包含这些抗体的组合物和使用抗体和组合物进行诊断和治疗的方法。本发明还涉及使用编码包含人抗M-CSF抗体的重和/或轻免疫球蛋白分子的核酸分子的基因治疗方法。版权所有（C）2013，JPO＆INPIT

55. 发明专利

JP2013006862A Immunogenic lhrh composition and method relating thereto 审中-公开
标题翻译：免疫组化LHRH组合物及其相关方法
公开(公告)号：JP2013006862A
公开(公告)日：2013-01-10
申请号：JP2012195610
申请日：2012-09-05
申请人： Pfizer Inc , ファイザー・インク
发明人： MCNAMARA MICHAEL KERIN
IPC分类号： A61K39/00 , A61K47/36 , A61K9/00 , A61K38/00 , A61K38/04 , A61K38/09 , A61K38/24 , A61K39/385 , A61K39/39 , A61K47/40 , A61P13/08 , A61P15/00 , A61P15/08 , A61P15/16 , A61P15/18 , A61P35/00 , A61P43/00
CPC分类号： A61K47/4833 , A61K38/09 , A61K39/0006 , A61K47/646 , A61K2039/55583 , A61K2039/6037
摘要： PROBLEM TO BE SOLVED: To provide a prophylactic and/or therapeutic agent for the modification of fertility and behaviour patterns of animals, the achievement of livestock production gains such as increasing growth, decreasing feed conversion ratios or the control of unwanted organoleptic characteristics or the treatment of disorders of the reproductive organs.SOLUTION: The invention relates generally to an immunogenic LHRH composition and more particularly to an immunogenic LHRH composition comprising a LHRH C-terminal fragment of at least five amino acids.
摘要翻译：待解决的问题：提供用于改变动物的生育力和行为模式的预防和/或治疗剂，实现家畜生产增益，例如增加生长，降低饲料转化率或控制不想要的感官特征或治疗生殖器官疾病。解决方案：本发明一般涉及免疫原性LHRH组合物，更具体地涉及包含至少五个氨基酸的LHRH C-末端片段的免疫原性LHRH组合物。版权所有（C）2013，JPO＆INPIT

56. 发明专利

JP2011141279A Biomarker for igf-1r antagonist therapy 审中-公开
标题翻译： IGF-1R拮抗剂治疗的生物标志物
公开(公告)号：JP2011141279A
公开(公告)日：2011-07-21
申请号：JP2011000377
申请日：2011-01-05
申请人： Pfizer Inc , ファイザー・インク
发明人： GREEN STEPHANIE JANET , GUALBERTO ANTONIO
IPC分类号： G01N33/53 , A61K39/395 , A61K45/00 , A61P35/00 , C07K16/28
CPC分类号： G01N33/74 , G01N2333/4745 , G01N2333/62 , G01N2333/65 , G01N2333/71 , G01N2800/52
摘要： PROBLEM TO BE SOLVED: To provide a method for predicting effect of an IGF-1R antagonist therapy on cancers of patients, a method for monitoring effectiveness of the therapy and a method for curing the cancers of the patients.
SOLUTION: The method is for usage of release IGF-1 and ration of insulin/IGFBP as a biomarker regarding the IGF-1R antagonist therapy for the cancers, and curing the cancers using the IGF-1R for the selected patients based on such a biomarker.
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供用于预测IGF-1R拮抗剂治疗对患者癌症的效果的方法，用于监测治疗效果的方法和治疗患者的癌症的方法。解决方案：该方法是使用释放IGF-1和胰岛素/ IGFBP的比例作为IGF-1R拮抗剂治疗癌症的生物标志物，并且使用基于IGF-1R的IGF-1R对所选择的患者进行治疗这样的生物标志物。版权所有（C）2011，JPO＆INPIT

57. 发明专利

JP2011064695A Treatment of incontinence 审中-公开
标题翻译：治疗不孕症
公开(公告)号：JP2011064695A
公开(公告)日：2011-03-31
申请号：JP2010249395
申请日：2010-11-08
申请人： Pfizer Inc , ファイザー・インク
发明人： MCMURRAY GORDON , MINER WESLEY DENNIS
IPC分类号： G01N33/50 , A61K31/00 , A61K31/495 , A61K45/00 , A61P7/12 , A61P13/06 , A61P43/00 , G01N33/15
CPC分类号： A61K31/00 , A61K31/495
摘要： PROBLEM TO BE SOLVED: To provide a treatment method of incontinence, an assay for screening useful compounds for treatment of incontinence, and a method for manufacturing a composition for treating urinary incontinence. SOLUTION: A method for screening the useful compounds for treatment of stress urinary incontinence, includes the steps of screening compounds on agonistic activities for 5-HT2C receptors, and selecting a compound having less than 100 nM of EC50. The method is the process also providing a medicine for treating the stress urinary incontinence includes the steps of (a) testing compounds in a ligand binding assay for the 5-HT2C receptors, (b) selecting a compound having less than 100 nM of IC50, and (c) formulating a drug of a compound having the same structure as the compound selected in the step (b) or pharmaceutically acceptable salt thereof together with a pharmaceutically acceptable carrier or an excipient. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供一种失禁治疗方法，用于筛选用于治疗失禁的有用化合物的检测方法以及用于制备治疗尿失禁的组合物的方法。解决方案：筛选用于治疗压力性尿失禁的有用化合物的方法包括以下步骤：筛选化合物对5-HT 2C受体的激动活性，并选择具有小于100nM EC 50的化合物。该方法还提供用于治疗压力性尿失禁的药物，其包括以下步骤：（a）在5-HT 2C受体的配体结合测定中测试化合物，（b）选择具有小于100nM的IC 50的化合物，和（c）配制具有与步骤（b）中选择的化合物相同结构的化合物或其药学上可接受的盐以及药学上可接受的载体或赋形剂的药物。版权所有（C）2011，JPO＆INPIT

58. 发明专利

JP2010280693A Benzimidazole derivative 审中-公开
标题翻译：苯并咪唑衍生物
公开(公告)号：JP2010280693A
公开(公告)日：2010-12-16
申请号：JP2010175465
申请日：2010-08-04
申请人： Pfizer Inc , ファイザー・インク
发明人： JONES CHRISTOPHER SCOTT , LA GRECA SUSAN , LI QIFANG , MUNCHHOF MICHAEL JOHN , REITER LAWRENCE ALAN
IPC分类号： C07D401/04 , A61K31/4184 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/5377 , A61K31/538 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D471/14 , C07D491/056
CPC分类号： C07D401/12 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04
摘要： PROBLEM TO BE SOLVED: To provide novel inhibitors of G protein-coupled receptors, Smoothened (Smo). SOLUTION: Novel benzimidazole derivatives such as N-((2R, 4R)-1-methyl-2-(6-methyl-1H-benzo[d]imidazol-2-yl)piperidin-4-yl)-2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamide, N-((2R, 4R)-2-(1H-benzo[d]imidazol-2-yl)-1-cyclopropylpiperidin-4-yl)-2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamide, and 1-((2R, 4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(6-(trifluoromethyl)pyridin-3-yl)urea are provided. The compounds are useful for treating abnormal cell growth, such as cancer, in mammals. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供G蛋白偶联受体的新的抑制剂Smoothened（Smo）。解决方案：新的苯并咪唑衍生物如N - （（2R，4R）-1-甲基-2-（6-甲基-1H-苯并[d]咪唑-2-基）哌啶-4-基）-2 ，3-二氢苯并[b] [1,4]二恶英-6-甲酰胺，N - （（2R，4R）-2-（1H-苯并[d]咪唑-2-基）-1-环丙基哌啶-4-基）-2,3-二氢苯并[b] [1,4]二氧杂环己烯-6-甲酰胺和1 - （（2R，4R）-2-（1H-苯并[d]咪唑-2-基）-1-甲基哌啶 -4-基）-3-（6-（三氟甲基）吡啶-3-基）脲。该化合物可用于治疗哺乳动物中的异常细胞生长，如癌症。版权所有（C）2011，JPO＆INPIT

59. 发明专利

JP2009297037A Antibody to insulin-like growth factor i receptor 有权
标题翻译：抗胰岛素样生长因子I受体
公开(公告)号：JP2009297037A
公开(公告)日：2009-12-24
申请号：JP2009222178
申请日：2009-09-28
申请人： Amgen Fremont Inc , Pfizer Inc , アムジェンフレモントインク. , ファイザー・インク
发明人： COHEN BRUCE D , BEEBE JEAN , MILLER PENELOPE E , MOYER JAMES D , CORVALAN JOSE R , GALLO MICHAEL
IPC分类号： A01K67/027 , C12N15/09 , A61K39/395 , A61K45/00 , A61K48/00 , A61K49/00 , A61P35/00 , A61P43/00 , C07K14/72 , C07K16/28 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/06 , C12N5/10 , C12N15/13 , C12P21/08 , G01N33/574 , G01N33/577 , G01N33/68
CPC分类号： C07K16/2863 , A01K2217/05 , A61K31/138 , A61K31/513 , A61K31/517 , A61K31/704 , A61K39/39541 , A61K39/39558 , A61K48/00 , A61K2039/505 , C07K14/72 , C07K16/30 , C07K16/40 , C07K2317/14 , C07K2317/21 , C07K2317/56 , C07K2317/565 , C07K2317/73 , C07K2317/75 , C07K2317/76 , C07K2317/92 , G01N33/574 , G01N33/57492 , G01N2333/65 , G01N2333/71 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide an antibody specifically binding to an insulin-like growth factor I receptor (IGF-IR), preferably human IGF-IR, and to provide an antigen-binding portion thereof. SOLUTION: A human anti-IGF-IR antibody includes a chimeric antibody, a bispecific antibody, a derivatized antibody, or a single chain antibody, or a portion of fusion proteins. An isolated heavy and light chain immunoglobulin molecule derived from an anti-IGF-IR antibody, and a nucleic acid molecule encoding the molecule are provided. Preparation of the anti-IGF-IR antibody, a pharmaceutical composition comprising the antibody, and use of the antibody, and the composition thereof for diagnosis and treatment are provided. A gene therapy uses the nucleic acid molecule encoding the heavy and/or light chain immunoglobulin molecule that comprises the human anti-IGF-IR antibody. A non-human transgenic animal expresses the nucleic acid. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供与胰岛素样生长因子I受体（IGF-1R）特异性结合的抗体，优选人IGF-1R，并提供其抗原结合部分。解决方案：人抗IGF-1R抗体包括嵌合抗体，双特异性抗体，衍生化抗体或单链抗体或融合蛋白的一部分。提供衍生自抗IGF-1R抗体的分离的重链和轻链免疫球蛋白分子，以及编码该分子的核酸分子。提供抗IGF-1R抗体的制备，包含该抗体的药物组合物和该抗体的用途及其组合物用于诊断和治疗。基因治疗使用编码包含人抗IGF-1R抗体的重链和/或轻链免疫球蛋白分子的核酸分子。非人转基因动物表达核酸。版权所有（C）2010，JPO＆INPIT

60. 发明专利

JP2008266338A Selective dopamine d3 receptor agonist for treating sexual dysfunction 审中-公开
标题翻译：选择性DOPAMINE D3受体激动剂治疗性功能障碍
公开(公告)号：JP2008266338A
公开(公告)日：2008-11-06
申请号：JP2008121009
申请日：2008-05-07
申请人： Pfizer Inc , ファイザー・インク
发明人： VAN DER GRAAF PIETER HADEWIJN , WAYMAN CHRISTOPHER PETER , BAXTER ANDREW DOUGLAS , COOK ANDREW SIMON , WONG STEPHEN KWOK-FUNG
IPC分类号： A61K45/00 , A01K67/027 , A61K31/00 , A61K31/5375 , A61K45/06 , A61P15/00 , A61P15/08 , A61P15/10 , A61P43/00 , G01N33/15 , G01N33/50
CPC分类号： A61K31/5375 , A61K31/00 , A61K45/06
摘要： PROBLEM TO BE SOLVED: To provide a medicinal composition for treating and/or preventing sexual dysfunction. SOLUTION: The medicinal composition contains a selective dopamine D3 receptor agonist, wherein the dopamine D3 receptor agonist is at least about 15-times more functionally selective for a dopamine D3 receptor as compared with a dopamine D2 receptor when being measured by using the same functional assay. COPYRIGHT: (C)2009,JPO&INPIT

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