-
21.发明授权公开(公告)号：US10344042B2
公开(公告)日：2019-07-09
申请号：US15625909
申请日：2017-06-16
Inventor： Hiroshi Takenaka , Yoichiro Ohta , Yusuke Taguchi , Sayuri Ueda , Yuko Ishino , Tomohiro Yoshikawa , Hideki Nakashima , Kohki Uehara , Mitsunori Kirihata
IPC: C07F5/02 , C07C271/22 , C07C229/36 , C07C251/24
Abstract: The present invention involves preparing compounds represented by the following formula: from a compound of the following formula: In these formulae: R1 represents a Br group, an iodine group, a Cl group, an NO2 group, or an NH2 group; R2 represents a halogen group, an NO2 group, an NH2 group, Sn(R6)3, N═N—NR7R8, OSO2R9, N R10R11, phenyliodonium, a heterocyclic group iodine, boric acid, or a borate ester; R30 represents a protective group PG1; R40 or R50 represent hydrogen, a protective group PG2, or C6H5(C6H5)C═N, in which NR40R50 are together.
-
22.发明授权公开(公告)号：US10005794B2
公开(公告)日：2018-06-26
申请号：US15105401
申请日：2014-12-16
Inventor： Hiroshi Takenaka , Yoichiro Ohta , Yusuke Taguchi , Sayuri Ueda , Yuko Ishino , Tomohiro Yoshikawa , Hideki Nakashima , Kohki Uehara , Mitsunori Kirihata
IPC: C07F5/02 , C07C271/22 , C07C229/36 , C07C251/24
CPC classification number: C07F5/027 , C07C229/36 , C07C251/24 , C07C271/22 , Y02P20/55
Abstract: The present invention involves preparing compounds represented by the formula. (In the formula: R1 represents a Br group, an iodine group, a Cl group, an NO2 group, or an NH2 group; R2 represents a halogen group, an NO2 group, an NH2 group, Sn(R6)3, N═N—NR7R8, OSO2R9, NR10R11, phenyliodonium, a heterocyclic group iodine, boric acid, or a borate ester; R30 represents a protective group PG1; R40 or R50 represent hydrogen, a protective group PG2, or C6H5(C6H5)C═N, wherein NR40R50 are together.)
-
23.发明授权公开(公告)号：US09422341B2
公开(公告)日：2016-08-23
申请号：US14377748
申请日：2013-02-07
Inventor： Mitsunori Kirihata , Kohki Uehara
IPC: C07K11/02 , C07C229/08 , C07C235/12 , C07K14/32 , C07C229/24 , C07D273/00 , C07C237/12 , C07K11/00
CPC classification number: C07K11/02 , C07C229/08 , C07C229/24 , C07C235/12 , C07C237/12 , C07D273/00 , C07K11/00 , C07K14/32
Abstract: The purpose of the present invention is to provide a novel method for producing cereulide and a derivative thereof; an intermediate for cereulide; and a novel cereulide derivative. A novel didepsipeptide, a novel tetradepsipeptide, a novel octadepsipeptide and a novel dodecadepsipeptide are prepared. A linear precursor of cereulide or a derivative thereof, which is composed of any one of the novel depsipeptides, is cyclized by forming an intramolecular amide bond.
Abstract translation: 本发明的目的是提供一种制备大戟素及其衍生物的新方法; 大众中间物 和一种新型的cereulide衍生物。 制备了一种新型的七叶皂苷肽，一种新型的四肽类，一种新的十八肽和一种新的十二十一生物肽。 通过形成分子内酰胺键将由任何一种新的缩肽组成的大脑或其衍生物的线性前体环化。
-
24.发明授权Chiral 4-boronophenylalanine (BPA) derivative and method for producing same, and method for producing 18F-labeled BPA using said derivative 有权手性4-硼苯丙氨酸（BPA）衍生物及其制备方法，以及使用所述衍生物制备18F标记的BPA的方法公开(公告)号：US09409926B2
公开(公告)日：2016-08-09
申请号：US14435678
申请日：2013-10-08
Inventor： Hiroshi Takenaka , Yoichiro Ohta , Yusuke Taguchi , Sayuri Ueda , Yuko Ishino , Hideki Nakashima , Kohki Uehara , Mitsunori Kirihata
IPC: C07F5/02 , C07C229/08 , C07F5/04 , C07C229/36 , C07B59/00 , C07C271/22 , C07C251/24
CPC classification number: C07F5/025 , C07B59/001 , C07C229/08 , C07C229/36 , C07C251/24 , C07C271/22 , C07F5/027 , C07F5/04 , Y02P20/55
Abstract: Provided are: a novel chiral 4-boronophenylalanine (BPA) derivative; a method for producing the derivative; and a method for producing 18F-2-fluoro-4-borono-L-phenylalanine (18F-labeled BPA; 18F-BPA) using the derivative. A compound represented by formula (1) is prepared. In the formula, R represents BR3R4, BX3− or BX3−M+ (wherein X represents a halogen atom, and M+ represents a monovalent monoatomic cation, a polyatomic cation or a complex cation); R1 represents a hydrogen atom or a protecting group PG1; R2 represents a hydrogen atom or a protecting group PG2; R3 and R4 independently represent OH, or R3, R4 and B together form a ring that serves as a protecting group; and Y represents a halogen atom, NO2, NH2, Sn(R6)3, N═N—NR7R8, OSO2R9, NR10R11, a substituted or unsubstituted phenyliodo group or a substituted or unsubstituted heterocyclic iodo group. The compound is reacted with a fluorination reagent to prepare 18F-labeled BPA.
Abstract translation: 提供：新型手性4-硼苯丙氨酸（BPA）衍生物; 一种制备衍生物的方法; 以及使用该衍生物制备18F-2-氟-4-硼羟-L-苯丙氨酸（18F标记的BPA; 18F-BPA）的方法。 制备由式（1）表示的化合物。 在该式中，R表示BR 3 R 4，BX 3 - 或BX 3 -M +（其中X表示卤原子，M +表示一价单原子阳离子，多原子阳离子或络合阳离子）。 R1表示氢原子或保护基PG1; R2表示氢原子或保护基PG2; R3和R4独立地表示OH，或R3，R4和B一起形成用作保护基的环; Y表示卤素原子，NO 2，NH 2，Sn（R 6）3，N = N-NR 7 R 8，OSO 2 R 9，NR 10 R 11，取代或未取代的苯基碘基或取代或未取代的杂环碘基。 使化合物与氟化试剂反应以制备18F标记的BPA。
-
25.发明授权公开(公告)号：US08940863B2
公开(公告)日：2015-01-27
申请号：US13857754
申请日：2013-04-05
Applicant: Koji Kawakami , Stella Pharma Corporation
Inventor： Koji Kawakami , Masayuki Kohno , Tomohisa Horibe , Oumi Nakajima , Mari Haramoto , Liying Yang
IPC: A61K38/00 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , C12P21/06 , C12N1/00 , C12N15/00 , C12N5/00 , C12N5/02 , C12N15/74 , A61P35/00 , C07H21/04 , C07K7/08 , A61K47/48 , C07K14/475 , C07K14/485 , C07K14/54 , C07K7/06 , C07K14/00
CPC classification number: C07K7/08 , A61K47/6425 , C07K14/475 , C07K14/485 , C07K14/54 , C07K2319/33 , C07K2319/55
Abstract: It is an object of the present invention to provide a substance usable as an anticancer agent or DDS, which has intracellular stability, which is capable of evading side effects from functional disorder with respect to normal cells, or which has instantaneous effect. The inventors developed a novel chimeric peptide targeting cancer cells which overexpress EGFR or the like using a binding peptide such as a peptide sequence binding to EGFR, and a lytic peptide sequence, thereby solving such an object. Particularly, by using a chimeric peptide including an EGF receptor-binding peptide or the like and a cytotoxic peptide, this object was solved.
Abstract translation: 本发明的目的是提供一种可以作为抗癌剂或DDS的物质，其具有细胞内稳定性，其能够逃避相对于正常细胞的功能障碍的副作用或具有瞬时作用。 本发明人开发了使用结合肽如结合EGFR的肽序列和裂解肽序列过表达EGFR等的靶向癌细胞的新型嵌合肽，从而解决了这样的问题。 特别地，通过使用包含EGF受体结合肽等的嵌合肽和细胞毒素肽，解决了该目的。
-
Patent Agency Ranking
公开(公告)号：US20240239816A1
公开(公告)日：2024-07-18
申请号：US18563110
申请日：2022-04-20
Applicant: STELLA PHARMA CORPORATION
Inventor： Yusuke MURATA , Hiroshi TAKENAKA , Yoichiro OHTA , Aya SUDANI , Miki ISHIMURA , Kensuke SUZUKI , Hiroyuki KAI
CPC classification number: C07F5/025 , A61K41/0095 , A61K51/0402
Abstract: Provided are new compounds that can have the property of being specifically taken up into cancer cells. In the present invention, novel 4-borono-phenylalanine derivatives, borono-phenylalanine derivatives having a heterocyclic skeleton, borono-phenylalanine derivatives having a fused ring structure, or pharmaceutically acceptable salts thereof are prepared. These compounds have the property of being taken up specifically by LAT1 and thus easily taken up specifically by cancer cells in the evaluation of LAT1 and LAT2 selective uptake, and can be conveniently used for neutron capture therapy and the like. A typical example is a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof.
-
公开(公告)号：US20220354875A1
公开(公告)日：2022-11-10
申请号：US17636246
申请日：2020-09-11
Applicant: STELLA PHARMA CORPORATION
Inventor： Yoshiya IGUCHI , Yoshimitsu KATAKUSE , Hideki NAKASHIMA
Abstract: The present invention relates to a pharmaceutical composition comprising a liquid composition containing p-boronophenylalanine, in which the liquid composition is accommodated in a packaging material and satisfies the following Condition I or Condition II: Condition I: the liquid composition comprises substantially no antioxidant and a concentration of dissolved oxygen in the liquid composition is 3.5 ppm or less; Condition II: the liquid composition comprises an antioxidant and a concentration of dissolved oxygen in the liquid composition is 3.0 ppm or less.
-
28.发明申请PRODUCTION METHOD FOR 2-FLUORO-4-BORONO-L-PHENYLALANINE, AND PRECURSOR OF 2-FLUORO-4-BORONO-L-PHENYLALANINE 有权2-氟-4-溴硼酸-L-苯乙烯胺的制备方法和2-氟-4-溴硼酸 - 苯甲酰胺的前体公开(公告)号：US20160311836A1
公开(公告)日：2016-10-27
申请号：US15105401
申请日：2014-12-16
Inventor： Hiroshi Takenaka , Yoichiro Ohta , Yusuke Taguchi , Sayuri Ueda , Yuko Ishino , Tomohiro Yoshikawa , Hideki Nakashima , Kohki Uehara , Mitsunori Kirihata
IPC: C07F5/02 , C07C229/36
CPC classification number: C07F5/027 , C07C229/36 , C07C251/24 , C07C271/22 , Y02P20/55
Abstract: The present invention involves preparing compounds represented by the formula. (In the formula: R1 represents a Br group, an iodine group, a Cl group, an NO2 group, or an NH2 group; R2 represents a halogen group, an NO2 group, an NH2 group, Sn(R6)3, N═N—NR7R8, OSO2R9, NR10R11, phenyliodonium, a heterocyclic group iodine, boric acid, or a borate ester; R30 represents a protective group PG1; R40 or R50 represent hydrogen, a protective group PG2, or C6H5(C6H5)C═N, wherein NR40R50 are together.)
Abstract translation: 本发明涉及制备由式表示的化合物。 （式中，R 1表示Br基，碘基，Cl基，NO 2基或NH 2基; R 2表示卤素基，NO 2基，NH 2基，Sn（R 6）3，N = N-NR7R8，OSO2R9，NR10R11，苯基碘鎓，杂环基碘，硼酸或硼酸酯; R30表示保护基PG1; R40或R50表示氢，保护基PG2或C6H5（C6H5） 其中NR40R50在一起。）
-
29.发明申请METHOD FOR PRODUCING CEREULIDE AND DERIVATIVE THEREOF, INTERMEDIATE FOR PRODUCTION OF CEREULIDE, AND CEREULIDE DERIVATIVE 有权用于生产谷粒和衍生物的方法，用于生产谷粒和谷粒衍生物的中间体公开(公告)号：US20150183831A1
公开(公告)日：2015-07-02
申请号：US14377748
申请日：2013-02-07
Inventor： Mitsunori Kirihata , Kohki Uehara
CPC classification number: C07K11/02 , C07C229/08 , C07C229/24 , C07C235/12 , C07C237/12 , C07D273/00 , C07K11/00 , C07K14/32
Abstract: The purpose of the present invention is to provide a novel method for producing cereulide and a derivative thereof; an intermediate for cereulide; and a novel cereulide derivative. A novel didepsipeptide, a novel tetradepsipeptide, a novel octadepsipeptide and a novel dodecadepsipeptide are prepared. A linear precursor of cereulide or a derivative thereof, which is composed of any one of the novel depsipeptides, is cyclized by forming an intramolecular amide bond.
Abstract translation: 本发明的目的是提供一种制备大戟素及其衍生物的新方法; 大众中间物 和一种新型的cereulide衍生物。 制备了一种新型的七叶皂苷肽，一种新型的四肽类，一种新的十八肽和一种新的十二十一生物肽。 通过形成分子内酰胺键将由任何一种新的缩肽组成的大脑或其衍生物的线性前体环化。
-
公开(公告)号：US20130274201A1
公开(公告)日：2013-10-17
申请号：US13857754
申请日：2013-04-05
Applicant: Stella Pharma Corporation , Koji Kawakami
Inventor： Koji Kawakami , Masayuki Kohno , Tomohisa Horibe , Oumi Nakajima , Mari Haramoto , Liying Yang
IPC: C07K14/00
CPC classification number: C07K7/08 , A61K47/6425 , C07K14/475 , C07K14/485 , C07K14/54 , C07K2319/33 , C07K2319/55
Abstract: It is an object of the present invention to provide a substance usable as an anticancer agent or DDS, which has intracellular stability, which is capable of evading side effects from functional disorder with respect to normal cells, or which has instantaneous effect. The inventors developed a novel chimeric peptide targeting cancer cells which overexpress EGFR or the like using a binding peptide such as a peptide sequence binding to EGFR, and a lytic peptide sequence, thereby solving such an object. Particularly, by using a chimeric peptide including an EGF receptor-binding peptide or the like and a cytotoxic peptide, this object was solved.
Abstract translation: 本发明的目的是提供一种可以作为抗癌剂或DDS的物质，其具有细胞内稳定性，其能够逃避相对于正常细胞的功能障碍的副作用或具有瞬时作用。 本发明人开发了使用结合肽如结合EGFR的肽序列和裂解肽序列过表达EGFR等的靶向癌细胞的新型嵌合肽，从而解决了这样的问题。 特别地，通过使用包含EGF受体结合肽等的嵌合肽和细胞毒素肽，解决了该目的。
-
-
-
-
-
-
-
-
-
Search Results
51
records
(took 0.031 seconds)
