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71. 发明申请

US20120101280A1 COMPOUND HAVING SPIRO-BONDED CYCLIC GROUP AND USE THEREOF 失效
标题翻译：具有螺旋结合循环组的化合物及其用途
公开(公告)号：US20120101280A1
公开(公告)日：2012-04-26
申请号：US13378799
申请日：2010-06-15
申请人： Koji Yoshida , Hiroshi Ochiai , Kousuke Tani , Shiro Shibayama , Miki Kasano
发明人： Koji Yoshida , Hiroshi Ochiai , Kousuke Tani , Shiro Shibayama , Miki Kasano
IPC分类号： C07D471/10
CPC分类号： C07D471/10
摘要： The invention relates to a compound represented by formula (I): a salt thereof, an N-oxide thereof, or a solvate thereof (symbols in the formula are as described in the specification).The compound of the present invention exhibits very low risk of side effects and also has persistent and strong antagonistic activity against CXCR4, and is therefore useful as pharmaceuticals, for example, preventive and/or therapeutic agent for inflammatory and immune diseases, infections (for example, HIV infection), diseases associated with HIV infection (for example, acquired immunodeficiency syndrome (AIDS)), cancer, cancer metastasis, psychoneurotic diseases and cardiovascular diseases (for example, retinopathy), metabolic diseases, cancerous diseases, or an agent for regeneration therapy.
摘要翻译：本发明涉及由式（I）表示的化合物：其盐，其N-氧化物或其溶剂化物（式中的符号如说明书中所述）。本发明的化合物显示出非常低的副作用风险，并且对CXCR4具有持久和强烈的拮抗活性，因此可用作药物，例如用于炎症和免疫疾病，感染的预防和/或治疗剂（例如，艾滋病毒感染），与艾滋病毒感染有关的疾病（例如，获得性免疫缺陷综合征（AIDS）），癌症，癌症转移，精神神经病和心血管疾病（例如视网膜病变），代谢疾病，癌性疾病或再生药剂治疗。

72. 发明授权

US08003642B2 Nitrogenated heterocyclic derivative, and pharmaceutical agent comprising the derivative as active ingredient 失效
标题翻译：氮化杂环衍生物和包含该衍生物作为活性成分的药剂
公开(公告)号：US08003642B2
公开(公告)日：2011-08-23
申请号：US12282464
申请日：2007-03-09
申请人： Shinya Kusuda , Toshihiko Nishiyama , Kazuya Hashimura , Junya Ueda , Shiro Shibayama
发明人： Shinya Kusuda , Toshihiko Nishiyama , Kazuya Hashimura , Junya Ueda , Shiro Shibayama
IPC分类号： A61K31/5377 , A61K31/4545 , C07D413/14 , C07D401/14
CPC分类号： C07D401/12 , C07D401/14 , C07D417/14 , C07D419/14
摘要： The compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof specifically binds CCR5, so it is useful for preventing and/or treating CCR5-related diseases, for example, various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, ulcerative colitis, etc.), immunological diseases (autoimmune diseases, rejection in organ transplantation, immunosuppression, psoriasis, multiple sclerosis, etc.), infectious diseases (infection with human immunodeficiency virus, acquired immunodeficiency syndrome, etc.), allergic diseases (atopic dermatitis, urticaria, allergic bronchopulmonary aspergillosis, allergic eosinophilic gastroenteritis, etc.), ischemic reperfusion injury, acute respiratory distress syndrome, shock accompanying bacterial infection diabetes cancer metastasis and so on Wherein all symbols in formula are as defined in the specification.
摘要翻译：由式（I）表示的化合物，其盐，其N-氧化物，其溶剂合物或其前药特异性结合CCR5，因此其可用于预防和/或治疗CCR5相关疾病，例如各种炎性疾病（哮喘，肾炎，肾病，肝炎，关节炎，类风湿性关节炎，鼻炎，结膜炎，溃疡性结肠炎等），免疫疾病（器官移植中的自身免疫性疾病，排斥反应，免疫抑制，牛皮癣，多发性硬化症等），感染性疾病（人体免疫缺陷病毒感染，获得性免疫缺陷综合征等），过敏性疾病（特应性皮炎，荨麻疹，过敏性支气管肺曲霉病，过敏嗜酸性胃肠炎等），缺血再灌注损伤，急性呼吸窘迫综合征，伴随细菌感染糖尿病的休克癌症转移等等，其中公式中的所有符号如说明书中所定义。

73. 发明申请

US20100285527A1 Novel Polypeptide, cDNA Encoding the Same, and Use Thereof 审中-公开
标题翻译：新型多肽，编码它的cDNA及其用途
公开(公告)号：US20100285527A1
公开(公告)日：2010-11-11
申请号：US12772617
申请日：2010-05-03
申请人： Daikichi FUKUSHIMA , Shiro Shibayama , Hideaki Tada
发明人： Daikichi FUKUSHIMA , Shiro Shibayama , Hideaki Tada
IPC分类号： C12P21/02 , C07K14/00 , C07H21/04 , C12N15/63 , C12N1/19
CPC分类号： C07K14/705 , A61K38/00 , C07K14/4703
摘要： Novel polypeptides produced by a human adult brain tissue, a cell line derived therefrom, a cell line derived from human bone marrow and a human umbilical cord venous endothelial cell line; a process for producing these polypeptides; cDNAs encoding the polypeptides; fragments hybridizable selectively with the cDNA sequences; replication or expression plasmids having the cDNAs integrated thereinto; host cells transformed by the plasmids; antibodies against the above polypeptides; and medicinal compositions containing the peptides or the antibodies.
摘要翻译：由人成人脑组织产生的新型多肽，源自其的细胞系，源自人骨髓的细胞系和人脐带静脉内皮细胞系; 一种生产这些多肽的方法; 编码多肽的cDNA; 片段可与cDNA序列选择性杂交; 具有整合cDNA的复制或表达质粒; 由质粒转化的宿主细胞; 针对上述多肽的抗体; 以及含有肽或抗体的药物组合物。

74. 发明申请

US20090305950A1 MULTIMER OF EXTRACELLULAR DOMAIN OF CELL SURFACE FUNCTIONAL MOLECULE 有权
标题翻译：细胞表面功能分子的细胞域的多个
公开(公告)号：US20090305950A1
公开(公告)日：2009-12-10
申请号：US12281427
申请日：2007-03-02
申请人： Nagahiro Minato , Yoshimasa Tanaka , Shiro Shibayama
发明人： Nagahiro Minato , Yoshimasa Tanaka , Shiro Shibayama
IPC分类号： A61K38/16 , C07K14/00 , C07H21/00 , C07H21/04 , C12N15/63 , C12N5/10 , C12P21/02
CPC分类号： C07K14/70503 , A61K9/0019 , A61K9/19 , A61K38/00 , A61K47/26 , C07K14/70532 , Y02A50/465 , Y02A50/481
摘要： As a substance which pharmacologically regulates the function of a cell surface functional molecule, a substance which has specificity and an activity or efficacy equal or superior to an antibody and does not require an advanced production technique and facility for application thereof to a pharmaceutical product has been demanded. The invention relates to a multimer of an extracellular domain of a cell surface functional molecule, particularly a tetramer of an extracellular domain of PD-1 or PD-L1. Further, the invention relates to an application of such a tetramer as a preventive and/or therapeutic agent for cancer, cancer metastasis, immunodeficiency, an infectious disease or the like and an application of PD-1 or PD-L1 as a testing or diagnostic agent or a research agent for such a disease.
摘要翻译：作为药理学上调节细胞表面功能分子的功能的物质，具有特异性，活性或功效等同于或优于抗体且不需要先进的生产技术的物质及其应用于药物的设备已经被要求本发明涉及细胞表面功能分子的细胞外结构域的多聚体，特别是PD-1或PD-L1细胞外结构域的四聚体。此外，本发明涉及这样的四聚体作为癌症，癌症转移，免疫缺陷，感染性疾病等的预防和/或治疗剂的应用，以及应用PD-1或PD-L1作为检测或诊断代理人或这种疾病的研究代理人。

75. 发明授权

US07595048B2 Method for treatment of cancer by inhibiting the immunosuppressive signal induced by PD-1 有权
标题翻译：通过抑制PD-1诱导的免疫抑制信号治疗癌症的方法
公开(公告)号：US07595048B2
公开(公告)日：2009-09-29
申请号：US10519925
申请日：2003-07-02
申请人： Tasuku Honjo , Nagahiro Minato , Yoshiko Iwai , Shiro Shibayama
发明人： Tasuku Honjo , Nagahiro Minato , Yoshiko Iwai , Shiro Shibayama
IPC分类号： A61K39/395 , C07K16/28
CPC分类号： C07K16/2818 , A61K9/0019 , A61K31/7088 , A61K38/1774 , A61K38/212 , A61K39/3955 , A61K45/06 , A61K47/02 , A61K47/26 , A61K2039/505 , A61K2039/507 , C07K14/70521 , C07K16/18 , C07K16/2803 , C07K16/2827 , C07K2317/21 , C07K2317/24 , C07K2317/54 , C07K2317/73 , C07K2317/76 , C07K2319/30 , C12Q1/025 , G01N33/5011 , G01N33/574 , G01N2500/00 , Y02A50/39 , Y02A50/394 , Y02A50/463 , Y02A50/466
摘要： Compositions for cancer or infection treatment via immunopotentiation caused by inhibition of the immunosuppressive signal induced by PD-1, PD-L1, or PD-L2 and therapies using them, immunopotentiative substrates included as the active ingredient, screening methods of the substrates for cancer or infection treatment, cell lines used for the screening methods, evaluation methods that select the substrates for cancer treatment, and carcinoma cell transplanted mammals used for the evaluation methods. The compositions of the present invention that inhibit the function of PD-1, PD-L1, or PD-L2 are useful for treatment of cancer or infection.
摘要翻译：通过由PD-1，PD-L1或PD-L2诱导的免疫抑制信号的抑制和使用它们的疗法，包括作为活性成分的免疫增强底物，用于癌症的底物的筛选方法或通过免疫增强感染治疗，用于筛选方法的细胞系，选择用于癌症治疗的底物的评价方法和用于评价方法的癌细胞移植的哺乳动物。抑制PD-1，PD-L1或PD-L2功能的本发明的组合物可用于治疗癌症或感染。

76. 发明申请

US20070054310A1 Novel polypeptide, cDNA encoding the same, and use thereof 审中-公开
标题翻译：新型多肽，编码其的cDNA及其用途
公开(公告)号：US20070054310A1
公开(公告)日：2007-03-08
申请号：US11593037
申请日：2006-11-06
申请人： Daikichi Fukushima , Shiro Shibayama , Hideaki Tada
发明人： Daikichi Fukushima , Shiro Shibayama , Hideaki Tada
IPC分类号： C12Q1/68 , C07H21/04 , C12P21/06 , C07K14/705
CPC分类号： C07K14/705 , A61K38/00 , C07K14/4703
摘要： Novel polypeptides produced by a human adult brain tissue, a cell line derived therefrom, a cell line derived from human bone marrow and a human umbilical cord venous endothelial cell line; a process for producing these polypeptides; cDNAs encoding the polypeptides; fragments hybridizable selectively with the cDNA sequences; replication or expression plasmids having the cDNAs integrated thereinto; host cells transformed by the plasmids; antibodies against the above polypeptides; and medicinal compositions containing the peptides or the antibodies.
摘要翻译：由人成人脑组织产生的新型多肽，源自其的细胞系，源自人骨髓的细胞系和人脐带静脉内皮细胞系; 一种生产这些多肽的方法; 编码多肽的cDNA; 片段可与cDNA序列选择性杂交; 具有整合cDNA的复制或表达质粒; 由质粒转化的宿主细胞; 针对上述多肽的抗体; 以及含有肽或抗体的药物组合物。

77. 发明申请

US20070043079A1 Heterocyclic compound containing nitrogen atom and use thereof 审中-公开
标题翻译：含氮原子的杂环化合物及其用途
公开(公告)号：US20070043079A1
公开(公告)日：2007-02-22
申请号：US10553704
申请日：2004-04-16
申请人： Hiromu Habashita , Minoru Nishizaki , Kazuya Hayashi , Shiro Shibayama
发明人： Hiromu Habashita , Minoru Nishizaki , Kazuya Hayashi , Shiro Shibayama
IPC分类号： A61K31/445 , A61K31/40 , C07D211/26 , C07D207/04
CPC分类号： C07D295/135 , A61K31/341 , A61K31/381 , A61K31/40 , A61K31/44 , A61K31/45 , A61K31/451 , A61K31/4525 , A61K31/453 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/455 , A61K31/4709 , A61K31/495 , A61K31/496 , C07D211/26
摘要： The present invention relates to a medicament comprising the compound of formula (I) wherein all symbols have the same meanings as defined in the specification, a salt thereof or a prodrug thereof. The compound of the present invention is useful for the prevention and/or treatment of immune diseases such as various types of inflammation, autoimmune disease, allergic diseases, etc.; infection concerning inflammation or HIV infections (e.g. asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, ulcerative colitis, etc.), organ transplantation rejection, immunosuppression, psoriasis, multiple sclerosis, optic neuritis, polymyalgia rheumatica syndrome, uveitis, vasculitis, human immunodeficiency virus infection (acquired immunodeficiency syndrome etc.), atopic dermatitis, urticaria, allergic bronchopulmonary aspergillosis, allergic eosinophilic gastroenteritis, osteoarthritis, ischemic reperfusion injury, acute respiratory distress syndrome, shock accompanying bacteria infection, diabetes, cancer metastasis, atherosclerosis, etc.).
摘要翻译：本发明涉及包含式（I）化合物的药物，其中所有符号具有与说明书中定义的相同的含义，其盐或其前药。本发明的化合物可用于预防和/或治疗各种类型的炎症，自身免疫性疾病，过敏性疾病等免疫疾病; 关于炎症或HIV感染的感染（例如哮喘，肾炎，肾病，肝炎，关节炎，类风湿性关节炎，鼻炎，结膜炎，溃疡性结肠炎等），器官移植排斥反应，免疫抑制，牛皮癣，多发性硬化症，视神经炎，多发性肌痛风湿综合征，葡萄膜炎，血管炎，人类免疫缺陷综合症等，特应性皮炎，荨麻疹，过敏性支气管肺曲霉病，过敏嗜酸性胃肠炎，骨关节炎，缺血再灌注损伤，急性呼吸窘迫综合征，伴随细菌感染的休克，糖尿病，癌症转移，动脉粥样硬化等）。

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