公开(公告)号：US07060721B1

公开(公告)日：2006-06-13

申请号：US09869135

申请日：1999-12-20

Applicant: Noriko Oku, legal representative ,  Chikako Oku, legal representative ,  Tomohito Oku, legal representative ,  Hiroshi Kayakiri ,  Yoshito Abe ,  Hitoshi Hamashima ,  Hitoshi Sawada ,  Naoki Ishibashi ,  Hiroyuki Setoi ,  Noritsugu Yamasaki ,  Takafumi Imoto ,  Takahiro Hiramura

Inventor： Teruo Oku, deceased

IPC: A61K31/4174 ,  C07D233/68

CPC classification number: C07D233/64 ,  C07D233/90 ,  C07D233/94 ,  C07D405/10 ,  C07D409/10 ,  C07D409/12

Abstract: Imidazole compounds represented by general formula (I): wherein each symbol is as defined in the specification, and salts thereof, and a pharmaceutical composition containing same are provided. These compounds are useful in treating the diseases curable based on a hypoglycemic action, and the diseases curable based on a cGMP-PDE inhibitory action, a smooth muscle relaxing action, a bronchodilating action, a vasodilating action, a smooth muscle cell inhibitory action and an allergy inhibitory action.

Abstract translation: 由通式（I）表示的咪唑化合物：其中每个符号如说明书中所定义，及其盐，以及含有其的药物组合物。 这些化合物可用于治疗基于降血糖作用可治疗的疾病，以及基于cGMP-PDE抑制作用，平滑肌松弛作用，支气管扩张作用，血管扩张作用，平滑肌细胞抑制作用和 过敏抑制作用。

公开(公告)号：US06573274B1

公开(公告)日：2003-06-03

申请号：US09856172

申请日：2001-09-12

Applicant: Teruo Oku ,  Hiroshi Kayakiri ,  Yoshito Abe ,  Hitoshi Hamashima ,  Hitoshi Sawada ,  Naoki Ishibashi ,  Hiroyuki Setoi ,  Noritsugu Yamasaki ,  Takafumi Imoto ,  Takahiro Hiramura

Inventor： Teruo Oku ,  Hiroshi Kayakiri ,  Yoshito Abe ,  Hitoshi Hamashima ,  Hitoshi Sawada ,  Naoki Ishibashi ,  Hiroyuki Setoi ,  Noritsugu Yamasaki ,  Takafumi Imoto ,  Takahiro Hiramura

IPC: A61K31437

CPC classification number: C07D471/04

Abstract: The present invention relates to a sulfonamide compound of the formula (I): wherein each symbol is as defined in the specification, a salt thereof, and a pharmaceutical composition containing same. This compound can be an effective agent for the prophylaxis and treatment of the diseases curable based on a hypoglycemic action, and the diseases curable based on a cGMP-PDE inhibitory action, a smooth muscle relaxing action, a bronchodilating action, a vasodilating action, a smooth muscle cell inhibitory action and an allergy suppressing action.

Abstract translation: 本发明涉及式（I）的磺酰胺化合物：其中每个符号如说明书中所定义，其盐和含有其的药物组合物。 该化合物可以是用于预防和治疗基于降血糖作用的可治疗疾病的有效试剂，以及基于cGMP-PDE抑制作用，平滑肌松弛作用，支气管扩张作用，血管舒张作用， 平滑肌细胞抑制作用和过敏抑制作用。

公开(公告)号：US5210092A

公开(公告)日：1993-05-11

申请号：US748954

申请日：1991-08-23

Applicant: Teruo Oku ,  Hiroyuki Setoi ,  Hiroshi Kayakiri ,  Shigeki Satoh ,  Takayuki Inoue ,  Yuki Saitoh ,  Akio Kuroda ,  Hirokazu Tanaka

Inventor： Teruo Oku ,  Hiroyuki Setoi ,  Hiroshi Kayakiri ,  Shigeki Satoh ,  Takayuki Inoue ,  Yuki Saitoh ,  Akio Kuroda ,  Hirokazu Tanaka

IPC: A61K31/415 ,  A61K31/435 ,  A61K31/52 ,  A61P9/00 ,  A61P9/12 ,  A61P43/00 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/00 ,  C07D487/04 ,  C07D495/04

CPC classification number: C07D403/14 ,  C07D471/04 ,  C07D495/04 ,  Y02P20/55

Abstract: The invention concerns compounds of the formula ##STR1## represents a condensed or uncondensed imidazolyl ring and the rest of the variables are defined in the specification. They are angiotensin II antagonists useful for treating hypertension, etc.

公开(公告)号：US5514701A

公开(公告)日：1996-05-07

申请号：US95350

申请日：1993-07-23

Applicant: Hiroyuki Setoi ,  Akihiko Sawada ,  Hirokazu Tanaka ,  Masashi Hashimoto

Inventor： Hiroyuki Setoi ,  Akihiko Sawada ,  Hirokazu Tanaka ,  Masashi Hashimoto

IPC: C07D207/14 ,  C07D207/32 ,  C07D207/335 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D521/00 ,  A61K31/40

CPC classification number: C07D207/335 ,  C07D207/14 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  Y10S514/826

Abstract: This invention relates to pyrrolidine derivatives and pharmaceutically acceptable salts, their pharmaceutical compositions, and methods of use as thromboxane A.sub.2 antagonists and/or thromboxane A.sub.2 synthetase inhibitors in the treatment of thrombotic diseases, asthma or nephritis, e.g. of the formula: ##STR1## wherein R.sup.1 is thienyl(lower)alkyl, furyl(lower)alkyl or pyrrolyl(lower)alkyl.

Abstract translation: 本发明涉及吡咯烷衍生物及其药学上可接受的盐，其药物组合物，以及作为血栓素A2拮抗剂和/或血栓素A2合成酶抑制剂用于治疗血栓性疾病，哮喘或肾炎的方法。 （低级）烷基或吡咯基（低级）烷基。

公开(公告)号：US4929639A

公开(公告)日：1990-05-29

申请号：US208665

申请日：1988-06-20

Applicant: Hiroyuki Setoi ,  Akio Kuroda ,  Hirokazu Tanaka ,  Hideo Hirai ,  Hiroshi Marusawa ,  Masashi Hashimoto

Inventor： Hiroyuki Setoi ,  Akio Kuroda ,  Hirokazu Tanaka ,  Hideo Hirai ,  Hiroshi Marusawa ,  Masashi Hashimoto

IPC: A61K31/357 ,  A61P7/02 ,  C07D309/06 ,  C07D319/06 ,  C07D405/12 ,  C07D409/12

CPC classification number: C07D405/12 ,  C07D309/06 ,  C07D319/06 ,  C07D409/12

Abstract: The invention relates to treatment of diseases caused by thromboxane A.sub.2 comprising administering a compound ##STR1## wherein R.sup.1 is hydrogen or lower alkyl,R.sup.2 is carboxy(lower)alkyl or protected carboxy(lower)alkyl andR.sup.3 is --CH.dbd.N--R.sup.4 in which R.sup.4 is arylureido or arylthioureido andX is --O--,or a pharmaceutically acceptable salt thereof.

公开(公告)号：US4479942A

公开(公告)日：1984-10-30

申请号：US403117

申请日：1982-07-29

Applicant: Michio Yamashita ,  Tadaaki Komori ,  Junji Hosoda ,  Yoshio Kawai ,  Itsuo Uchida ,  Masanobu Kohsaka ,  Hiroshi Imanaka ,  Kazuo Sakane ,  Hiroyuki Setoi ,  Tsutomu Teraji

Inventor： Michio Yamashita ,  Tadaaki Komori ,  Junji Hosoda ,  Yoshio Kawai ,  Itsuo Uchida ,  Masanobu Kohsaka ,  Hiroshi Imanaka ,  Kazuo Sakane ,  Hiroyuki Setoi ,  Tsutomu Teraji

IPC: A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7076 ,  A61P31/04 ,  C07H19/16 ,  C12P19/40 ,  C07H17/00 ,  C07H19/06

CPC classification number: C12R1/645 ,  C07H19/16 ,  C12P19/40 ,  Y02P20/55

Abstract: This invention relates to tetrahydrofuran-carboxylic acid derivatives, of antimicrobial activity, of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group,R.sup.2 is amino or acylamino andR.sup.3 is carboxy or a protected carboxy groupor a pharmaceutically acceptable salt thereof.

Abstract translation: 本发明涉及抗微生物活性的四氢呋喃 - 羧酸衍生物，其具有下式：其中R1是氨基或被保护的氨基，R2是氨基或酰基氨基，R3是羧基或被保护的羧基或药学上可接受的盐 其中。

公开(公告)号：US06495542B1

公开(公告)日：2002-12-17

申请号：US09600857

申请日：2000-10-16

Applicant: Hiroyuki Setoi ,  Takehiko Ohkawa ,  Yuki Sawada ,  Kazuhiko Osoda ,  Teruo Oku

Inventor： Hiroyuki Setoi ,  Takehiko Ohkawa ,  Yuki Sawada ,  Kazuhiko Osoda ,  Teruo Oku

IPC: A61K3155

CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

Abstract: A compound of formula (I): wherein A is an optionally substituted heterocyclic group, R is a lower alkoxy; Z is C═O or CH2; and B is benzazapinyl, which may be optionally substituted, or a salt thereof, that possesses vasopressin antagonistic activity and is useful as a vasopressin antagonist.

Abstract translation: 式（I）的化合物：其中A是任选取代的杂环基，R是低级烷氧基; Z是C = O或CH 2; 并且B是具有加压素拮抗活性并且可用作加压素拮抗剂的苯并氮杂基，其可以是任选被取代的，或其盐。

公开(公告)号：US5521170A

公开(公告)日：1996-05-28

申请号：US220695

申请日：1994-03-31

Applicant: Hiroyuki Setoi ,  Takehiko Ohkawa ,  Tatsuya Zenkoh ,  Keiji Hemmi ,  Hirokazu Tanaka

Inventor： Hiroyuki Setoi ,  Takehiko Ohkawa ,  Tatsuya Zenkoh ,  Keiji Hemmi ,  Hirokazu Tanaka

IPC: A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/47 ,  A61K31/495 ,  A61K31/55 ,  A61K31/551 ,  A61P1/16 ,  A61P3/08 ,  A61P9/00 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P43/00 ,  C07D209/08 ,  C07D209/34 ,  C07D215/08 ,  C07D223/16 ,  C07D223/20 ,  C07D241/40 ,  C07D241/44 ,  C07D243/04 ,  C07D243/12 ,  C07D243/14 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D405/06 ,  C07D471/04 ,  C07D241/36 ,  C07D245/06

CPC classification number: C07D223/16 ,  C07D209/08 ,  C07D215/08 ,  C07D223/20 ,  C07D241/44 ,  C07D243/04 ,  C07D243/12 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D471/04

Abstract: Compounds having the structure below ##STR1## and pharmaceutically acceptable salts thereof exhibit vasopressin antagonistic activity, vasodilating activity, hypotensive activity, activity for inhibiting saccharide release in the liver, activity for inhibiting growth of mesagium cells, water diuretic activity, platelet agglutination inhibitory activity, oxytocin antagonistic activity and the like, and are useful in treating or preventing hypertension, heart failure, renal insufficiency, edema, ascites, vasopressin parasecretion syndrome, hepatocirrhosis, hyponatremia, hypokalemia, diabetic or circulation disorder, oxytocin related diseases and the like.

Abstract translation: 具有以下结构的化合物及其药学上可接受的盐显示出加压素拮抗活性，血管舒张活性，降血压活性，抑制肝中糖释放的活性，抑制中期细胞生长的活性，水利尿活性，血小板凝集抑制活性， 催产素拮抗活性等，可用于治疗或预防高血压，心力衰竭，肾功能不全，水肿，腹水，血管加压素副作用综合征，肝硬化，低钠血症，低钾血症，糖尿病或循环障碍，催产素相关疾病等。

公开(公告)号：US5130323A

公开(公告)日：1992-07-14

申请号：US421399

申请日：1989-10-13

Applicant: Hiroyuki Setoi ,  Akihiko Sawada ,  Hirokazu Tanaka ,  Masashi Hashimoto

Inventor： Hiroyuki Setoi ,  Akihiko Sawada ,  Hirokazu Tanaka ,  Masashi Hashimoto

IPC: A61K31/40 ,  A61K31/4025 ,  A61K31/415 ,  A61K31/425 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/47 ,  A61K31/495 ,  A61P1/04 ,  A61P9/00 ,  A61P9/10 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D207/14 ,  C07D207/32 ,  C07D207/335 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D521/00

CPC classification number: C07D207/335 ,  C07D207/14 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06

Abstract: The invention relates to pyrrolidine derivatives having thromboxane A.sub.2 antagonism and TXA.sub.2 synthetase-inhibitory activity, of the formula ##STR1## wherein R.sup.1 is pyridyl(lower)alkyl, R.sup.2 is an acyl group selected from the group consisting of lower alkanoyl, lower alkoxycarbonyl, lower alkylsulfonyl, phenylsulfonyl, benzoyl, phenyl(lower)alkanoyl, cyclo(lower)alkyl(lower)alkanoyl, phenyl(lower)alkoxycarbonyl and phenylcarbamoyl, each of which may have 1 to 3 substituent(s) selected from the group consisting of halogen, lower alkyl, lower alkoxy, nitro and mono(or di or tri)halo(lower)alkyl, andR.sup.3 is carboxy(lower)alkyl, protected carboxy(lower)alkyl, carboxyphenyl or protected carboxyphenyl,or a pharmaceutically acceptable salt thereof.

公开(公告)号：US06316482B1

公开(公告)日：2001-11-13

申请号：US09614132

申请日：2000-07-11

Applicant: Hiroyuki Setoi ,  Takehiko Ohkawa ,  Tatsuya Zenkoh ,  Hitoshi Sawada ,  Yuki Sawada ,  Teruo Oku

Inventor： Hiroyuki Setoi ,  Takehiko Ohkawa ,  Tatsuya Zenkoh ,  Hitoshi Sawada ,  Yuki Sawada ,  Teruo Oku

IPC: A61K31415

CPC classification number: C07D209/48 ,  C07C237/44 ,  C07D209/08 ,  C07D209/12 ,  C07D209/14 ,  C07D209/42 ,  C07D215/48 ,  C07D231/12 ,  C07D231/56 ,  C07D233/56 ,  C07D235/06 ,  C07D235/08 ,  C07D235/10 ,  C07D235/12 ,  C07D235/14 ,  C07D235/16 ,  C07D235/24 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D235/32 ,  C07D239/88 ,  C07D239/96 ,  C07D241/42 ,  C07D249/08 ,  C07D249/18 ,  C07D263/10 ,  C07D263/56 ,  C07D265/32 ,  C07D295/135 ,  C07D295/185 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D413/12 ,  C07D471/04 ,  C07D473/00 ,  C07D487/04 ,  C07F7/1804

Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc. and represented by general formula (I): wherein R1 is aryl optionally substituted with lower alkoxy, etc., R2 is lower alkyl, etc., R3 is hydrogen, etc., A is NH, etc., E is etc., X is —CH═CH—, —CH═N—, or S, and Y is a condensed heterocyclic group, etc., and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.

Abstract translation: 本发明涉及具有加压素拮抗活性的新型苯甲酰胺衍生物等，并由通式（I）表示：其中R 1为任选被低级烷氧基取代的芳基，R 2为低级烷基等，R 3为氢等。 ，A是NH等，E isetc。，X是-CH = CH-，-CH = N-或S，Y是稠合杂环基等，及其药学上可接受的盐，其制备方法 以及含有该组合物的药物组合物。