公开(公告)号：US20090062382A1

公开(公告)日：2009-03-05

申请号：US12197438

申请日：2008-08-25

Applicant: Yasumi UCHIDA ,  Yasuto Uchida ,  Haruko Uchida

Inventor： Yasumi UCHIDA ,  Yasuto Uchida ,  Haruko Uchida

IPC: A61K31/343 ,  A61P15/10

CPC classification number: A61K9/0014 ,  A61K9/0034 ,  A61K9/145 ,  A61K9/146 ,  A61K31/5575 ,  A61K38/40 ,  A61K47/06 ,  A61K47/10 ,  A61K47/36 ,  A61K47/38 ,  A61K47/42

Abstract: The present invention provides a preventive or a remedy for penile erectile dysfunction, which promotes blood-flow in a penile sponge body over long time and thus induces erection while showing high safety without any adverse effect on a body as a whole, when externally administered to a penis.Use of a drug of the present invention enables to prevent or treat male penile erectile dysfunction and, at the same time, overcome a problem of female insertion impediment caused by increased resistance due to vaginal secretion disorder. Namely, a sexual life of patients (including aged persons) having coital dysfunction can be normalized and thus QOL can be improved.

Abstract translation: 本发明提供了阴茎勃起功能障碍的预防或补救措施，其可以长时间促进阴茎海绵体中的血液流动，从而诱导勃起，同时显示高安全性，而对整个身体没有任何不利影响，当外部给予 阴茎 使用本发明的药物能够预防或治疗男性阴茎勃起功能障碍，同时克服由阴道分泌障碍引起的阻力增加引起的女性插入障碍的问题。 也就是说，具有社会功能障碍的患者（包括老年人）的性生活可以被归一化，因此可以改善生活质量。

公开(公告)号：US20060189695A1

公开(公告)日：2006-08-24

申请号：US10561814

申请日：2003-06-25

Applicant: Yasumi Uchida ,  Yasuto Uchida ,  Haruko Uchida

Inventor： Yasumi Uchida ,  Yasuto Uchida ,  Haruko Uchida

IPC: A61K31/557

CPC classification number: A61K9/0014 ,  A61K9/0034 ,  A61K9/145 ,  A61K9/146 ,  A61K31/5575 ,  A61K38/40 ,  A61K47/06 ,  A61K47/10 ,  A61K47/36 ,  A61K47/38 ,  A61K47/42

Abstract: The present invention provides a preventive or a remedy for penile erectile dysfunction, which promotes blood-flow in a penile sponge body over long time and thus induces erection while showing high safety without any adverse effect on a body as a whole, when externally administered to a penis. Use of a drug of the present invention enables to prevent or treat male penile erectile dysfunction and, at the same time, overcome a problem of female insertion impediment caused by increased resistance due to vaginal secretion disorder. Namely, a sexual life of patients (including aged persons) having coital dysfunction can be normalized and thus QOL can be improved.

Abstract translation: 本发明提供了阴茎勃起功能障碍的预防或补救措施，其可以长时间促进阴茎海绵体中的血液流动，从而诱导勃起，同时显示高安全性，而对整个身体没有任何不利影响，当外部给予 阴茎 使用本发明的药物能够预防或治疗男性阴茎勃起功能障碍，同时克服由阴道分泌障碍引起的阻力增加引起的女性插入障碍的问题。 也就是说，具有社会功能障碍的患者（包括老年人）的性生活可以被归一化，因此可以改善生活质量。

公开(公告)号：US4737506A

公开(公告)日：1988-04-12

申请号：US851134

申请日：1986-04-07

Applicant: Noboru Shimizu ,  Hiroyuki Ishiwata ,  Tomio Ohta ,  Hiroshi Ishihama ,  Yasumi Uchida

Inventor： Noboru Shimizu ,  Hiroyuki Ishiwata ,  Tomio Ohta ,  Hiroshi Ishihama ,  Yasumi Uchida

IPC: C07D401/12 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/455 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D211/90 ,  C07D401/14

CPC classification number: C07D211/90

Abstract: This invention relates to a 1,4-dihydropyridine-3,5-dicarboxylate derivative represented by the following general formula (I): ##STR1## wherein R means an imidazolyl or pyridyl group, R.sub.1 denotes a hydrogen or halogen atom or a nitro or trifluoromethyl group, R.sub.2 is a lower alkyl group, X is CH or N, A means a lower alkylene group, ##STR2## B being a lower alkylene or O-lower alkylene group, ##STR3## R.sub.4 being a hydrogen atom or lower alkyl group, or ##STR4## m denotes a number of 1-3, and n stands for 1 or 2. The derivative has vasodilative effects, hyperkinemic effects, platelet aggregation inhibitory effects, thromboxane A.sub.2 formation inhibitory effects and so on, and are hence useful as a pharmaceutical product such as vasodilator, antihypertensive, antithrombotic agent, antiarteriosclerotic agent or the like.

Abstract translation: PCT No.PCT / JP85 / 00449 Sec。 一九八六年四月七日 102（e）日期1986年4月7日PCT提交1985年8月12日PCT公布。 公开号WO86 / 01206 PCT 日本特愿1986年2月27日。本发明涉及由以下通式（I）表示的1,4-二氢吡啶-3,5-二羧酸酯衍生物：其中R表示咪唑基或吡啶基，R1 表示氢或卤素原子或硝基或三氟甲基，R 2为低级烷基，X为CH或N，A表示低级亚烷基，B为低级亚烷基或O-低级亚烷基，IMA图 > R4是氢原子或低级烷基，或者表示1-3个数，n代表1或2.该衍生物具有血管扩张作用，超动力作用，血小板聚集抑制作用，血栓素A2形成抑制 效果等，因此可用作药物产品如血管扩张剂，抗高血压剂，抗血栓形成剂，抗动脉硬化剂等。

公开(公告)号：US4394382A

公开(公告)日：1983-07-19

申请号：US271927

申请日：1981-06-09

Applicant: Masami Shiratsuchi ,  Noboru Shimizu ,  Hiromichi Shigyo ,  Yoshinori Kyotani ,  Hisashi Kunieda ,  Kiyoshi Kawamura ,  Seiichi Sato ,  Toshihiro Akashi ,  Masahiko Nagakura ,  Naotoshi Sawada ,  Yasumi Uchida

Inventor： Masami Shiratsuchi ,  Noboru Shimizu ,  Hiromichi Shigyo ,  Yoshinori Kyotani ,  Hisashi Kunieda ,  Kiyoshi Kawamura ,  Seiichi Sato ,  Toshihiro Akashi ,  Masahiko Nagakura ,  Naotoshi Sawada ,  Yasumi Uchida

IPC: C07D311/04 ,  A61K31/353 ,  A61P9/02 ,  A61P9/04 ,  A61P21/02 ,  C07D311/22 ,  C07D311/58 ,  C07D311/64 ,  C07D311/66 ,  A61K31/35

CPC classification number: C07D311/22 ,  C07D311/58 ,  C07D311/64 ,  C07D311/66 ,  Y10S514/821

Abstract: A benzopyran compound represented by the following ##STR1## wherein A represents a direct bond or the bond --CH.sub.2 --O--,R.sub.1 represents a member selected from the group consisting of a C.sub.3 -C.sub.5 alkyl group, a hydroxy-(C.sub.3 -C.sub.5 alkyl) group, a lower alkylamino-lower alkyl group, a nitrato-(C.sub.3 -C.sub.5 alkyl) group and a phenyl-(C.sub.1 -C.sub.5) alkyl group, provided that the phenyl may be substituted by a lower alkoxy group, R.sub.2 represents a member selected from the group consisting of hydrogen, halogen, OH, NO.sub.2, a carbamoyl group, a lower alkyl group, a lower alkoxy group, a lower alkyleneoxy group and acetyl group,R.sub.3 represents hydrogen or NO.sub.2,B represents a direct bond, a C.sub.1 -C.sub.7 alkylene group, a --O-lower alkylene group or a --CONH-lower alkylene group, andn represents 1 or 2;and an acid addition salt thereof and a pharmaceutical composition comprising aforesaid compound.

Abstract translation: 由下式（I）表示的苯并吡喃化合物，其中A表示直接键或键-CH2-O-，R1表示选自C3-C5烷基，羟基 - （C3 -C 5烷基）基，低级烷基氨基 - 低级烷基，硝基 - （C 3 -C 5烷基）基和苯基 - （C 1 -C 5）烷基，条件是苯基可以被低级烷氧基取代，R 2 表示选自氢，卤素，OH，NO 2，氨基甲酰基，低级烷基，低级烷氧基，低级亚烷基氧基和乙酰基的成员，R 3表示氢或NO 2，B表示直接键 ，C 1 -C 7亚烷基，-O-低级亚烷基或-CONH-低级亚烷基，n表示1或2; 及其酸加成盐和包含上述化合物的药物组合物。

公开(公告)号：US20060122264A1

公开(公告)日：2006-06-08

申请号：US10559708

申请日：2003-06-09

Applicant: Yasumi Uchida ,  Haruko Uchida

Inventor： Yasumi Uchida ,  Haruko Uchida

IPC: A61K31/365

CPC classification number: A61L31/16 ,  A61K31/343 ,  A61K31/39 ,  A61L31/10 ,  A61L2300/442 ,  C07D327/04

Abstract: The present invention provides an inhibitor of the invasion of bone-marrow-derived vascular stem cells or inflammatory cells into blood vessel walls, a blood vessel restenosis inhibitor, and a preventive or therapeutic drug for angiitis or myocardiitis, each containing a phthalein dye compound as an active ingredient; and an instrument for treating blood vessels which is coated with a resin containing a phthalein dye compound or made of such a resin. Use of the drug of the present invention enables effective prevention of restenosis of a blood vessel after, for example, angioplasy. Moreover, it is possible to prevent the progress and disruption of a lesion of angiitis, myocarditis, or arterioscrelosis, for which no efficacious preventive or therapeutic method has been established so far, as well as microvascular ischemic diseases. By performing a medical treatment such as angioplasy using the instrument of the present invention for treating blood vessels, events of vascular restenosis can be effectively prevented.

Abstract translation: 本发明提供了将骨髓来源的血管干细胞或炎症细胞侵入血管壁的抑制剂，血管再狭窄抑制剂和用于血管炎或心肌炎的预防或治疗药物，每种含有酞菁染料化合物作为 活性成分; 以及用于治疗血管的器械，其中涂有含有酞菁染料化合物或由这种树脂制成的树脂。 使用本发明的药物能够有效地防止例如血管淤血后的血管再狭窄。 此外，可以防止迄今为止没有建立有效的预防或治疗方法以及微血管缺血性疾病的血管炎，心肌炎或动脉硬化性病变的进展和破坏。 通过使用本发明的用于治疗血管的器械进行诸如血管性皮炎的治疗，可以有效地防止血管再狭窄的事件。

公开(公告)号：US07025981B2

公开(公告)日：2006-04-11

申请号：US10237012

申请日：2002-09-09

Applicant: Yasumi Uchida ,  Haruko Uchida

Inventor： Yasumi Uchida ,  Haruko Uchida

IPC: A61F2/02

CPC classification number: A61L31/16 ,  A61L31/08 ,  A61L2300/416 ,  A61L2300/442 ,  A61L2300/606

Abstract: The present invention relates to a therapeutic tool for vascular diseases, which is coated with a dye-containing resin that comprises one or more biocompatible dyes selected from the group consisting of sulfonic acid azo dye, phthalein dye, triphenylmethane dye, phenantridium dye, acrydine dye, xanthene dye, phenothiazine dye and cyanine dye; a medical treatment by the use of the therapeutic tool for vascular diseases; and a method of preventing vascular restenosis caused mainly through inhibition of migration of vascular progenitor cells by administering the medical treatment to a subject.Since the present therapeutic tool for vascular diseases is capable of staying in vivo for a long term, a medical treatment such as angioplasty (coronary angioplasty, peripheral angioplasty, cerebral angioplasty, etc.) and blood vessel bypass (coronary bypass, peripheral bypass) by the use of the present tool can effectively inhibit the generation of blood vessel restenosis by inhibiting migration of vascular progenitor cells. Thus, the present tool is extremely useful in clinical situations.

公开(公告)号：US5371086A

公开(公告)日：1994-12-06

申请号：US53869

申请日：1993-04-29

Applicant: Tadahiro Takemoto ,  Masahiro Eda ,  Mitsuyoshi Hihara ,  Takehiro Okada ,  Hiroshi Sakashita ,  Miyuki Eiraku ,  Chikara Fukaya ,  Norifumi Nakamura ,  Masanori Sugiura ,  Sumio Matzno ,  Maki Goda ,  Yasumi Uchida

Inventor： Tadahiro Takemoto ,  Masahiro Eda ,  Mitsuyoshi Hihara ,  Takehiro Okada ,  Hiroshi Sakashita ,  Miyuki Eiraku ,  Chikara Fukaya ,  Norifumi Nakamura ,  Masanori Sugiura ,  Sumio Matzno ,  Maki Goda ,  Yasumi Uchida

IPC: C07D213/75 ,  C07D213/76 ,  C07D213/77 ,  C07D213/81 ,  C07D213/84 ,  C07D213/89 ,  C07D405/12 ,  C07D413/12 ,  A61K31/495 ,  A61K31/54 ,  C07D211/56 ,  C07D401/00

CPC classification number: C07D213/75 ,  C07D213/76 ,  C07D213/77 ,  C07D213/81 ,  C07D213/84 ,  C07D213/89 ,  C07D405/12 ,  C07D413/10

Abstract: An aminopyridine compound represented by the formula: ##STR1## wherein n represents 0 or 1; Z represents .dbd.S, .dbd.NCN or .dbd.CHNO.sub.2 ; R.sub.1 represents --NR.sub.3 R.sub.4, --NHNR.sub.3 R.sub.4, --NHCONHR.sub.3 or --NHSO.sub.2 R.sub.3 ; R.sub.2 represents H, or substituted or unsubstituted alkyl; R.sub.3 and R.sub.4, which may be the same or different, represent H, substituted or unsubstituted alkyl, aryl, substituted or unsubstituted acyl or alkoxycarbonyl group; and R.sub.3 and R.sub.4 may form a heterocyclic ring together with a nitrogen atom to which R.sub.3 and R.sub.4 are bound, through another heteroatom or without it; an optical isomer thereof or art acid salt thereof, which is excellent in pharmacological effect and repressed in side effects as a drug for circulatory diseases.

Abstract translation: 由下式表示的氨基吡啶化合物：其中n表示0或1; Z表示= S，= NCN或= CHNO2; R 1表示-NR 3 R 4，-NHNR 3 R 4，-NHCONHR 3或-NHSO 2 R 3; R 2表示H或取代或未取代的烷基; R 3和R 4可以相同或不同，表示H，取代或未取代的烷基，芳基，取代或未取代的酰基或烷氧基羰基; 并且R 3和R 4可以与R3和R4连接的氮原子一起通过另一个杂原子或不与其形成杂环; 其光学异构体或其酸性盐，其药理作用优异，作为循环系统疾病药物的副作用被抑制。

公开(公告)号：US4578465A

公开(公告)日：1986-03-25

申请号：US604415

申请日：1984-04-30

Applicant: Hiroyuki Nagano ,  Mitiro Takagi ,  Noboru Kubodera ,  Isao Matsunaga ,  Hiroyuki Nabata ,  Yasuhiro Ohba ,  Kazushige Sakai ,  Shun-ichi Hata ,  Yasumi Uchida

Inventor： Hiroyuki Nagano ,  Mitiro Takagi ,  Noboru Kubodera ,  Isao Matsunaga ,  Hiroyuki Nabata ,  Yasuhiro Ohba ,  Kazushige Sakai ,  Shun-ichi Hata ,  Yasumi Uchida

IPC: C07D403/06 ,  A61K31/505 ,  A61K31/517 ,  A61P9/00 ,  A61P9/12 ,  C07D239/96

CPC classification number: C07D239/96

Abstract: Phenylpiperazine derivatives of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a straight- or branched-chain saturated or unsaturated alkyl group having 1 to 8 carbon atoms which may be substituted at any position by a hydroxyl group, a carboxyl group, a lower alkoxycarbonyl group or an oxo group; and R.sub.2 is a hydrogen atom, a halogen atom, a lower alkyl group or a sulfamoyl group, and a process for producing the same are disclosed. The derivatives of the formula have alpha blocking and serotonin antagonizing activities and are useful as a drug.

Abstract translation: 具有下式的苯基哌嗪衍生物：其中R1是氢原子或可以在任何位置被羟基取代的具有1-8个碳原子的直链或支链饱和或不饱和烷基， 羧基，低级烷氧基羰基或氧代基; R 2为氢原子，卤素原子，低级烷基或氨磺酰基及其制造方法。 该衍生物具有α阻断和5-羟色胺拮抗活性，可用作药物。

公开(公告)号：US4727085A

公开(公告)日：1988-02-23

申请号：US706748

申请日：1985-02-28

Applicant: Masami Shiratsuchi ,  Kiyoshi Kawamura ,  Toshihiro Akashi ,  Hiroshi Ishihama ,  Yasumi Uchida

Inventor： Masami Shiratsuchi ,  Kiyoshi Kawamura ,  Toshihiro Akashi ,  Hiroshi Ishihama ,  Yasumi Uchida

IPC: A61K31/35 ,  C07D311/64

CPC classification number: A61K31/35 ,  C07D311/64

Abstract: A novel racemate K-351A composed of an optical isomer (2'S),(3S)K-351 [3,4-dihydro-8-(2'-hydroxy-3'-isopropylamino)propoxy-3-nitroxy-2H-1-benzopyran] and (2'R),(3R)K-351, a novel racemate K-351B composed of an optical isomer (2'R),(3S)K-351 and (2'S),(3R)K351 and an acid addition salt of these two novel racemates; a process for converting the two racemates to each other; and also to a pharmaceutical composition comprising each of the two racemates useful for the treatment of cardiovascular diseases.

Abstract translation: 由旋光异构体（2'S），（3S）K-351 [3,4-二氢-8-（2'-羟基-3'-异丙氨基）丙氧基-3-硝酰氧基-2H-1 （3S）K-351和（2'S），（3R）K351组成的新型外消旋体K-351B，（3R）K-351 和这两种新型外消旋体的酸加成盐; 将两种消旋体相互转化的过程; 并且还涉及包含用于治疗心血管疾病的两种外消旋体中的每一种的药物组合物。

公开(公告)号：US4448989A

公开(公告)日：1984-05-15

申请号：US451322

申请日：1982-12-20

Applicant: Masami Shiratsuchi ,  Hiroshi Ishihama ,  Yasumi Uchida

Inventor： Masami Shiratsuchi ,  Hiroshi Ishihama ,  Yasumi Uchida

IPC: A61K31/165 ,  A61P9/00 ,  C07C67/00 ,  C07C231/00 ,  C07C235/48 ,  C07C235/60 ,  C07D303/22 ,  C07C103/76 ,  C07C103/78

CPC classification number: C07D303/22

Abstract: A compound represented by the following formula ##STR1## wherein R represents a lower alkyl group having 2 to 6 carbon atoms, and n is an integer of from 1 to 5.

Abstract translation: 由下式表示的化合物＆lt; IMAGE＆gt;其中，R表示碳原子数2〜6的低级烷基，n为1〜5的整数。