公开(公告)号：US07671211B1

公开(公告)日：2010-03-02

申请号：US09926218

申请日：2000-03-31

Applicant: Arne Holmgren ,  Marjan H. Amiri ,  Hiroyuki Masayasu

Inventor： Arne Holmgren ,  Marjan H. Amiri ,  Hiroyuki Masayasu

IPC: C07D293/00

CPC classification number: C07D293/04 ,  A61K31/166 ,  A61K31/167 ,  C07C391/02 ,  C12N9/0036 ,  C12P9/00

Abstract: A substrate for thioredoxin reductase which comprises a compound represented by the following general formula (I) or (I′): wherein R1 and R2 independently represent a hydrogen atom, a halogen atom, a trifluoromethyl group and the like; R3 represents an aryl group, an aromatic heterocyclic group and the like; R4 represents a hydrogen atom, a hydroxyl group, a —S-α-amino acid group and the like; R5 represents a hydrogen atom or a C1-C6 alkyl group; Y represents oxygen atom or sulfur atom; n represents an integer of from 0 to 5; and the selenium atom may be oxidized, whose example includes 2-phenyl-1,2-benzisoselenazol-3(2H)-one or a ring-opened form thereof. The substrate is reduced by thioredoxin reductase in the presence of NADPH and enhances peroxidase activity of thioredoxin reductase.

Abstract translation: 用于硫氧还蛋白还原酶的底物，其包含由以下通式（I）或（I'）表示的化合物：其中R 1和R 2独立地表示氢原子，卤素原子，三氟甲基等; R3表示芳基，芳香族杂环基等; R4表示氢原子，羟基，-S-α-氨基酸基等; R5表示氢原子或C1-C6烷基; Y表示氧原子或硫原子; n表示0〜5的整数， 并且硒原子可被氧化，其实例包括2-苯基-1,2-苯并异硒唑-3（2H） - 酮或其开环形式。 在NADPH存在下，底物被硫氧还蛋白还原酶还原，提高硫氧还蛋白还原酶的过氧化物酶活性。

公开(公告)号：US5480888A

公开(公告)日：1996-01-02

申请号：US256268

申请日：1994-07-11

Applicant: Kazuhisa Kodama ,  Atsushi Hirayama ,  Hiroyuki Masayasu

Inventor： Kazuhisa Kodama ,  Atsushi Hirayama ,  Hiroyuki Masayasu

IPC: A61K31/165 ,  A61K31/195 ,  A61K31/28 ,  A61K31/36 ,  A61K31/41 ,  A61K31/555 ,  A61K38/06 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  C07C391/02 ,  C07D293/12 ,  C07D317/62 ,  C07D213/40 ,  A61K31/33 ,  A61K31/34

CPC classification number: A61K38/063 ,  A61K31/28 ,  A61K31/36 ,  A61K31/555

Abstract: An inhibitor for restenosis after percutaneous coronary arterioplasty, which comprises, as an active ingredient, a compound of the following formula (1), (1') or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sup.1 and R.sup.2 are independently a hydrogen atom, a halogen atom, a trifluoromethyl group, a nitro group, a C1-C6 alkyl group or a C1-C6 alkoxyl group, and R.sup.1 and R.sup.2 may be linked to form a methylenedioxy group; R.sup.3 is an optionally substituted aryl group, an optionally substituted aromatic heterocyclic group, an optionally substituted 5 to 7-membered cycloalkyl or cycloalkenyl group; R.sup.4 is a hydrogen atom, a hydroxyl group, an -S-glutathione residue, an -S-.alpha.-amino acid residue, or an aralkyl group optionally having substituent(s) in the aryl moiety; R.sup.5 is a hydrogen atom or a C1-C6 alkyl group, and R.sup.4 and R.sup.5 may be linked to form a single bond; Y is an oxygen atom or a sulfur atom; n is an integer of from 0 to 5, and the selenium atom may be oxidized.The inhibitor of the present invention exhibits excellent inhibitory effect against restenosis after PTCA with low toxicity.

Abstract translation: PCT No.PCT / JP93 / 00045 Sec。 371日期：1994年7月11日 102（e）日期1994年7月11日PCT 1993年1月14日PCT公布。 出版物WO93 / 13762 日期：1993年7月22日。经皮冠状动脉成形术后再狭窄的抑制剂，其包含作为活性成分的下式（1），（1'）或其药学上可接受的盐的化合物：其中1 ）其中R1和R2独立地为氢原子，卤素原子，三氟甲基，硝基，C1-C6烷基或C1-C6烷氧基，R1和R2可以是 连接形成亚甲二氧基; R3是任选取代的芳基，任选取代的芳族杂环基，任选取代的5至7元环烷基或环烯基; R4是氢原子，羟基，-S-谷胱甘肽残基，-S-α-氨基酸残基或芳基中任选具有取代基的芳烷基; R5是氢原子或C1-C6烷基，R4和R5可以连接形成单键; Y是氧原子或硫原子; n为0〜5的整数，可以使硒原子氧化。 本发明的抑制剂对低毒性PTCA后的再狭窄具有优异的抑制作用。

公开(公告)号：US5948800A

公开(公告)日：1999-09-07

申请号：US905530

申请日：1997-08-04

Applicant: Ikuro Maruyama ,  Kazuhiro Abeyama ,  Hiroyuki Masayasu

Inventor： Ikuro Maruyama ,  Kazuhiro Abeyama ,  Hiroyuki Masayasu

IPC: A61K31/41

CPC classification number: A61K31/41

Abstract: The present invention is directed to a drug for preventing or remedying Alzheimer's disease. The drug contains as the active ingredient 2-phenyl-1,2-benzisoselenazol-3(2H)-one (referred as compound (A)), whose effect is based on the action of reducing neuron toxicity induced by .beta.-amyloid protein.

Abstract translation: 本发明涉及用于预防或治疗阿尔茨海默氏病的药物。 该药物含有作为活性成分的2-苯基-1,2-苯并异硒唑-3（2H） - 酮（称为化合物（A）），其作用是基于降低β-淀粉样蛋白质诱导的神经元毒性的作用。