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1. 发明公开

EP3199628A4 CYTOTOXICITY-INDUCING THERAPEUTIC AGENT 审中-公开
公开(公告)号：EP3199628A4
公开(公告)日：2018-06-06
申请号：EP15844692
申请日：2015-09-25
申请人： CHUGAI PHARMACEUTICAL CO LTD
发明人： NEZU JUNICHI , NARITA ATSUSHI , ISHIGURO TAKAHIRO , SAKURAI MIKA , SHIRAIWA HIROTAKE , HIRONIWA NAOKA , IGAWA TOMOYUKI , KAWAI YUMIKO
IPC分类号： C07K16/30 , A61K39/395 , C07K16/28
CPC分类号： C07K16/468 , A61K39/395 , A61K2039/505 , C07K16/28 , C07K16/2809 , C07K16/30 , C07K16/303 , C07K16/46 , C07K2317/24 , C07K2317/31 , C07K2317/34 , C07K2317/524 , C07K2317/526 , C07K2317/565 , C07K2317/567 , C07K2317/71 , C07K2317/73 , C07K2317/92 , C07K2317/94 , C12N5/10 , C12N15/09
摘要： Novel multispecific antigen-binding molecules maintaining excellent cellular cytotoxicity and high stability, which comprise a domain that contains an antibody variable region having glypican 3-binding activity and a domain that contains an antibody variable region having T-cell receptor complex-binding activity, were discovered. Since the molecules of the present invention show a strong cytotoxicity against cells and tissues expressing glypican 3, it is possible to produce novel pharmaceutical compositions for treating or preventing various cancers.

2. 发明公开

EP3153195A4 SYRINGE CAP, NEEDLE-MOUNTED SYRINGE, AND PREFILLED SYRINGE FORMULATION 有权
公开(公告)号：EP3153195A4
公开(公告)日：2018-02-28
申请号：EP15803488
申请日：2015-06-04
申请人： TAISEI KAKO CO , CHUGAI PHARMACEUTICAL CO LTD
发明人： SHIOZAKI RIEKO , YAMANAKA YUJI , HORITA TAIJI , MATSUMOTO IPPEI , TANIGUCHI KENSUKE
IPC分类号： A61M5/32
CPC分类号： A61M5/3202 , A61M5/3213
摘要： Provided is a syringe cap including a projection extending in the circumferential direction of a cap body, wherein the projection includes an apex located radially outward of the cap body from the outer circumferential surface of the cap body, a first inclined surface having a starting end located at the apex and having a terminal end located at a position on the side closer to the proximal end of the cap body than the starting end is, and a second inclined surface having a starting end located at the apex and on the outer circumferential surface of the cap body having a terminal end located at a position on the side closer to the distal end of the cap body than the starting end is, on the outer circumferential surface of the cap body, and the shortest distance from the starting end to the terminal end of the first inclined surface is smaller than the shortest distance from the starting end to the terminal end of the second inclined surface.

3. 发明公开

EP3178817A4 AMORPHOUS FORM OF TETRACYCLIC COMPOUND 有权
公开(公告)号：EP3178817A4
公开(公告)日：2018-01-03
申请号：EP15830197
申请日：2015-08-07
申请人： CHUGAI PHARMACEUTICAL CO LTD
发明人： SHIRAKI KOJI , NAKAYAMA TADANOBU , OTA TOMOAKI
IPC分类号： C07D401/04 , A61K31/5377 , A61P35/00 , A61P35/04
CPC分类号： C07D401/10 , A61K9/10 , A61K31/5377 , A61K47/32 , A61K47/38 , C07D401/04
摘要： An amorphous form of 9-ethyl-6,6-dimethyl-8-(4-morpholin-4-yl-piperidin-1-yl)-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile and a solid dispersion containing the amorphous form can be used extremely advantageously as drugs for oral administration.

4. 发明公开

EP3135287A4 PREPARATION CONTAINING TETRACYCLIC COMPOUND AT HIGH DOSE 审中-实审
公开(公告)号：EP3135287A4
公开(公告)日：2018-01-03
申请号：EP15783124
申请日：2015-04-24
申请人： CHUGAI PHARMACEUTICAL CO LTD
发明人： TOMIMATSU TAKASHI , OKAZAKI KENSUKE , OGAWA YUMI , YAMAMURA TAKAHIRO
IPC分类号： A61K31/5377 , A61K9/16 , A61K9/48 , A61K47/04 , A61K47/20 , A61K47/36 , A61K47/38 , A61P25/24 , A61P25/28 , A61P35/00 , A61P35/04 , A61P43/00 , C07D401/04
CPC分类号： A61K31/5377 , A61K9/16 , A61K9/1617 , A61K9/1652 , A61K9/48 , A61K47/20 , A61K47/36 , A61K47/38 , C07D401/04
摘要： An improved solubility of a pharmaceutical composition or formulation containing a large amount of 9-ethyl-6,6-dimethyl-8-(4-morpholin-4-yl-piperidin-1-yl)-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile or a salt thereof can be achieved by forming granules of the compound or salt thereof and allowing the granules to be present together with a disintegrating agent.

5. 发明授权

EP2552955B1 ANTIBODIES WITH MODIFIED AFFINITY TO FCRN THAT PROMOTE ANTIGEN CLEARANCE 有权
标题翻译： ANTIKÖRPERMITVERÄNDERTERAFFINITÄTZU FCRN ZUR GESTEIGERTEN ANTIGEN-BESEITIGUNG
公开(公告)号：EP2552955B1
公开(公告)日：2017-05-03
申请号：EP11714860
申请日：2011-03-30
申请人： CHUGAI PHARMACEUTICAL CO LTD
发明人： IGAWA TOMOYUKI , ISHII SHINYA , MAEDA ATSUHIKO , NAKAI TAKASHI
IPC分类号： C07K16/00
CPC分类号： C07K16/18 , A61K2039/505 , A61K2039/545 , C07K14/70535 , C07K16/248 , C07K16/28 , C07K16/2866 , C07K16/4241 , C07K2317/24 , C07K2317/31 , C07K2317/52 , C07K2317/71 , C07K2317/72 , C07K2317/76 , C07K2317/77 , C07K2317/92 , C07K2317/94 , C07K2319/30
摘要： An objective of the present invention is to provide methods for facilitating antigen-binding molecule-mediated antigen uptake into cells, methods for facilitating the reduction of antigen concentration in plasma, methods for increasing the number of antigens to which a single antigen-binding molecule can bind, methods for improving pharmacokinetics of antigen-binding molecules, antigen-binding molecules improved for facilitated antigen uptake into cells, antigen-binding molecules capable of facilitating the reduction of antigen concentration in plasma, antigen-binding molecules capable of repeatedly binding to antigens, antigen-binding molecules with improved pharmacokinetics, pharmaceutical compositions comprising such an antigen-binding molecule, and methods for producing those described above. The present inventors discovered that antigen uptake into cells is facilitated by an antibody having human FcRn-binding activity at the plasma pH and a lower antigen-binding activity at the early endosomal pH than at the plasma pH; such antibodies can increase the number of antigens to which a single antibody molecule can bind; the reduction of antigen in plasma can be facilitated by administering such an antibody; and antibody pharmacokinetics can be improved by using such antibodies.
摘要翻译：本发明的一个目的是提供促进抗原结合分子介导的抗原摄入细胞的方法，促进血浆中抗原浓度降低的方法，增加单一抗原结合分子可以将抗原数量增加的方法改善抗原结合分子的药代动力学的方法，为促进抗原摄取进入细胞而改善的抗原结合分子，能够促进血浆中抗原浓度降低的抗原结合分子，能够重复结合抗原的抗原结合分子，具有改善的药代动力学的抗原结合分子，包含这种抗原结合分子的药物组合物，以及用于生产上述那些的方法。本发明人发现，在血浆pH下具有人FcRn结合活性的抗体和早期内体pH下的抗原结合活性低于血浆pH的抗体促进了抗原向细胞的摄取; 这样的抗体可以增加单个抗体分子可以结合的抗原的数量; 通过施用这种抗体可以促进血浆中抗原的减少; 并且通过使用这样的抗体可以改善抗体药代动力学。

6. 发明公开

EP2889376A4 MOUSE Fc RII-SPECIFIC Fc ANTIBODY 审中-公开
标题翻译： MAUS-FC-RII-SPEZIFISCHER FC-ANTIKÖRPER
公开(公告)号：EP2889376A4
公开(公告)日：2016-11-02
申请号：EP13830975
申请日：2013-08-23
申请人： CHUGAI PHARMACEUTICAL CO LTD
发明人： IGAWA TOMOYUKI , MURATA ERIKO , MIMOTO FUTA
IPC分类号： C12N15/09 , A61K39/395 , A61P37/00 , A61P37/06 , C07K16/28 , G01N33/15 , G01N33/50
CPC分类号： C07K16/283 , A61K39/395 , A61K49/0004 , A61K49/0008 , C07K16/28 , C07K16/2866 , C07K2317/52 , C07K2317/72 , C07K2317/92 , C12N15/09 , G01N33/564 , G01N33/6857 , G01N2800/52
摘要： The present inventors have successfully found a large number of Fc variants with remarkably increased binding activity against and/or binding selectivity for mouse Fc³RII by introducing amino acid alteration(s) to the Fc region.
摘要翻译：本发明人已经成功地发现了通过向Fc区引入氨基酸改变，大量Fc变体与小鼠Fc 3 RII具有显着增加的结合活性和/或结合选择性。

7. 发明公开

EP2975030A4 DIHYDROPYRIDAZINE-3,5-DIONE DERIVATIVE 有权
标题翻译：二氢-3,5-二酮衍生金融工具
公开(公告)号：EP2975030A4
公开(公告)日：2016-08-03
申请号：EP14765619
申请日：2014-03-13
申请人： CHUGAI PHARMACEUTICAL CO LTD
发明人： OHTAKE YOSHIHITO , OKAMOTO NAOKI , ONO YOSHIYUKI , KASHIWAGI HIROTAKA , KIMBARA ATSUSHI , HARADA TAKEO , HORI NOBUYUKI , MURATA YOSHIHISA , TACHIBANA KAZUTAKA , TANAKA SHOTA , NOMURA KENICHI , IDE MITSUAKI , MIZUGUCHI EISAKU , ICHIDA YASUHIRO , OHTOMO SHUICHI , HORIBA NAOSHI
IPC分类号： C07D237/04 , A61K31/50 , A61K31/501 , A61K31/5025 , A61K31/504 , A61K31/506 , A61K31/5377 , A61P3/12 , A61P13/12 , A61P43/00 , C07D401/12 , C07D401/14 , C07D403/12 , C07D471/04 , C07D487/04 , C07D487/18
CPC分类号： C07D487/18 , C07D237/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D471/04 , C07D487/04
摘要： The present invention provides a dihydropyridazine-3,5-dione derivative or a salt thereof, or a solvate of the compound or the salt, a pharmaceutical drug, a pharmaceutical composition, a sodium-dependent phosphate transporter inhibitor, and a preventive and/or therapeutic agent for hyperphosphatemia, secondary hyperparathyroidism, and chronic renal failure, comprising the compound as an active ingredient, and a method for prevention and/or treatment.

8. 发明公开

EP2889377A4 FCYRIIB-SPECIFIC FC REGION VARIANT 有权
标题翻译： FCYRIIB-SPEZIFISCHE FC-REGIONSVARIANTE
公开(公告)号：EP2889377A4
公开(公告)日：2016-08-03
申请号：EP13831250
申请日：2013-08-23
申请人： CHUGAI PHARMACEUTICAL CO LTD
发明人： KATADA HITOSHI , KADONO SHOJIRO , MIMOTO FUTA , IGAWA TOMOYUKI
IPC分类号： A61K39/00 , C07K16/00 , C07K16/28 , C07K16/30
CPC分类号： C07K16/00 , A61K9/0019 , A61K2039/505 , C07K16/28 , C07K16/2866 , C07K16/303 , C07K2317/52 , C07K2317/524 , C07K2317/53 , C07K2317/71 , C07K2317/72 , C07K2317/92 , C07K2317/94 , C07K2319/30
摘要： An objective of the present invention is to provide an Fc region variant with enhanced Fc³RIIb-binding activity, and/or enhanced binding selectivity to Fc³RIIb compared to Fc³RIIa (type R), as compared to those of a polypeptide containing an Fc region to which an amino acid alteration(s) has not been introduced; a polypeptide which includes the Fc region variant; a pharmaceutical composition containing the polypeptide; preventing therapeutic or preventive agent for immunological inflammatory diseases that includes the pharmaceutical composition; a production method thereof; and a method of enhancing Fc³RIIb-binding activity and also enhancing binding selectivity to Fc³RIIb compared to Fc³RIIa (type R). It was found that a polypeptide containing an antibody Fc region variant that contains an amino acid sequence in which an amino-acid alteration at position 238 (EU numbering) is combined with other specific amino-acid alterations enhances Fc³RIIb-binding activity, and/or enhances binding selectivity to Fc³RIIb compared to Fc³RIIa (type R).
摘要翻译：本发明的目的是提供与FcαRIIa（R型）相比具有增强的Fc3RIIb结合活性和/或增强的对Fc3RIIb的结合选择性的Fc区变体，与含有Fc区的多肽相比，氨基酸改变尚未引入; 包括Fc区变体的多肽; 含有多肽的药物组合物; 预防包括该药物组合物的免疫性炎性疾病的治疗或预防剂; 其制造方法; 以及增强Fc3RIIb结合活性的方法，并且与FcγRIIa（R型）相比，增强与Fc3RIIb的结合选择性。发现含有含有氨基酸序列的抗体Fc区变体的多肽，其中238位氨基酸改变（EU编号）与其他特异性氨基酸改变组合增强Fc3RIIb结合活性，和/或与FcγRIIa（R型）相比，增强与Fc3RIIb的结合选择性。

9. 发明公开

EP2842939A4 BENZAMIDE DERIVATIVE 有权
标题翻译： BENZAMIDDERIVAT
公开(公告)号：EP2842939A4
公开(公告)日：2015-11-11
申请号：EP13782636
申请日：2013-04-24
申请人： CHUGAI PHARMACEUTICAL CO LTD
发明人： MURATA TAKESHI , NIIZUMA SATOSHI , HARA SOUSUKE , KAWADA HATSUO , HADA KIHITO , SHIMADA HIDEAKI , TANAKA HIROSHI , NAKANISHI YOSHITO
IPC分类号： C07C317/32 , A61K31/166 , A61K31/40 , A61K31/445 , A61K31/495 , A61K31/496 , A61P19/04 , A61P29/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07C211/56 , C07C317/34 , C07C323/42 , C07C323/46 , C07D205/04 , C07D207/09 , C07D207/12 , C07D207/14 , C07D211/26
CPC分类号： C07C321/28 , C07C317/14 , C07C317/34 , C07C317/40 , C07C323/42 , C07C323/48 , C07C2601/02 , C07D205/04 , C07D207/09 , C07D207/12 , C07D207/14 , C07D211/26 , C07D211/56 , C07D211/68 , C07D213/62 , C07D213/82 , C07D241/04 , C07D263/34 , C07D295/14 , C07D295/16 , C07D309/14 , C07D401/12 , C07D403/04 , C07D487/08
摘要： The present invention relates to benzamide derivatives represented by formula (I) or pharmaceutically acceptable salts thereof.

10. 发明公开

EP2700652A4 DIAGNOSIS AND TREATMENT OF CANCER USING ANTI-ITM2A ANTIBODY 有权
标题翻译：诊断和治疗的癌症使用抗ITM2A抗体
公开(公告)号：EP2700652A4
公开(公告)日：2015-07-15
申请号：EP12774392
申请日：2012-04-18
申请人： UNIV TOKYO , CHUGAI PHARMACEUTICAL CO LTD
发明人： ABURATANI HIROYUKI , ISHIKAWA SHUMPEI , KAWAI SHIGETO
IPC分类号： C07K16/28 , A61K39/395 , A61P35/00 , A61P35/02 , C07K16/30 , C07K16/46 , C12N15/09 , C12P21/08 , G01N33/53 , G01N33/574 , G01N33/577
CPC分类号： C07K16/3061 , C07K16/28 , C07K2317/56 , C07K2317/565 , C07K2317/73 , C07K2317/732 , G01N33/57407 , G01N33/57426 , G01N2800/52
摘要： Disclosed is a monoclonal antibody binding to an ITM2A protein. This antibody is useful in the diagnosis, prevention, and treatment of cancer such as Ewing's sarcoma, T cell leukemia, T cell lymphoma, acute myeloid leukemia, B cell tumor, and multiple myeloma. The present invention also provides a pharmaceutical composition, a cell growth inhibitor, and an anticancer agent containing the antibody as an active ingredient, and a method for treating cancer, a method for predicting the efficacy of cancer treatment, and a method for determining the presence of cancer in a test subject using the antibody.

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