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：US06787565B2

公开(公告)日：2004-09-07

申请号：US10047093

申请日：2002-01-17

Applicant: Hiroshi Kayakiri ,  Yoshito Abe ,  Hitoshi Hamashima ,  Hitoshi Sawada ,  Tsuyoshi Mizutani ,  Teruo Oku ,  Noritsugu Yamasaki ,  Osamu Onomura ,  Masahiro Nishikawa ,  Takahiro Hiramura ,  Takafumi Imoto

Inventor： Hiroshi Kayakiri ,  Yoshito Abe ,  Hitoshi Hamashima ,  Hitoshi Sawada ,  Tsuyoshi Mizutani ,  Teruo Oku ,  Noritsugu Yamasaki ,  Osamu Onomura ,  Masahiro Nishikawa ,  Takahiro Hiramura ,  Takafumi Imoto

IPC: A61K3134

CPC classification number: C07D241/52 ,  C07D215/48 ,  C07D231/56 ,  C07D239/96 ,  C07D249/18 ,  C07D307/79 ,  C07D333/54 ,  C07D333/62 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

Abstract: A sulfonamide compound of the formula (I): R1—SO2NHCO—A—X—R2  (I) wherein R1 is alky, alkenyl, alkynyl and the like; A is an optionally substitutedheteropolycyclic group except benzimidazolyl, indolyl, 4,7-dihydrobenzimidazolyland 2,3-dihydrobenzoxazinyl; X is alkylene, oxa, oxa(lower)alkylene and the like; and R2 is optionally substituted aryl, substituted biphenylyl and the like, a salt thereof and a pharmaceutical composition comprising the same. The sulfonamide compound is effective for the diseases treatable based on their blood sugar level-depressing activity, cGMP-PDE (especially PDE-V)-inhibiting activity, smooth muscle relaxing activity, bronchodilating activity, vasodilating activity, smooth muscle cell suppressing activity, and antiallergic activity.

Abstract translation: 式（I）的磺酰胺化合物：其中R 1是烷基，烯基，炔基等; A是任选取代的杂多环基团，除了苯并咪唑基，吲哚基，4,7-二氢苯并咪唑啉-2,3-二氢苯并恶嗪基; X是亚烷基，氧杂，氧杂（低级）亚烷基等; 和R 2是任选取代的芳基，取代的联苯基等，其盐和包含它们的药物组合物。 磺胺类化合物可以基于其血糖降低活性，cGMP-PDE（特别是PDE-V）抑制活性，平滑肌松弛活性，支气管扩张活性，血管舒张活性，平滑肌细胞抑制活性，以及 抗过敏活性。

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：US6015818A

公开(公告)日：2000-01-18

申请号：US117453

申请日：1998-08-03

Applicant: Teruo Oku ,  Hiroshi Kayakiri ,  Yoshito Abe ,  Yuki Sawada ,  Tsuyoshi Mizutani

Inventor： Teruo Oku ,  Hiroshi Kayakiri ,  Yoshito Abe ,  Yuki Sawada ,  Tsuyoshi Mizutani

IPC: A61K31/4439 ,  A61K31/4709 ,  A61P1/00 ,  A61P1/16 ,  A61P1/18 ,  A61P3/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P13/12 ,  A61P15/00 ,  A61P15/12 ,  A61P27/02 ,  A61P27/06 ,  A61P43/00 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  A61K31/395

CPC classification number: C07D401/14 ,  C07D401/12 ,  C07D409/14

Abstract: This invention relates to a compound of formula (1) wherein R.sup.1 is halogen, etc., R.sup.2 is halogen, etc., R.sup.3 is amino substituted with substituent(s) selected from the group consisting of lower alkyl and acyl, etc., R.sup.4 is heterocyclic (lower)alkyl, R.sup.5 is lower alkyl, and A.sup.1 is lower alkylene, and pharmaceutically acceptable salts thereof, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to methods of using the same therapeutically in the prevention and/or the treatment of hypertension or the like. ##STR1##

Abstract translation: PCT No.PCT / JP97 / 00233 Sec。 371日期1998年8月3日 102（e）1998年8月3日PCT PCT 1997年1月31日PCT公布。 公开号WO97 / 28153 PCT 日期：1997年8月7日本发明涉及式（1）化合物，其中R 1为卤素等，R 2为卤素等，R 3为被选自下列基团的取代基取代的氨基：低级烷基和酰基 等等，R4是杂环（低级）烷基，R5是低级烷基，并且A1是低级亚烷基及其制药方法的药学上可接受的盐，包括它们的药物组合物及其使用方法 治疗性地预防和/或治疗高血压等。

公开(公告)号：US5356897A

公开(公告)日：1994-10-18

申请号：US931093

申请日：1992-08-17

Applicant: Teruo Oku ,  Yoshio Kawai ,  Hiroshi Marusawa ,  Hitoshi Yamazaki ,  Yoshito Abe ,  Hirokazu Tanaka

Inventor： Teruo Oku ,  Yoshio Kawai ,  Hiroshi Marusawa ,  Hitoshi Yamazaki ,  Yoshito Abe ,  Hirokazu Tanaka

IPC: A61K31/415 ,  A61K31/505 ,  A61K31/53 ,  A61P29/00 ,  A61P37/00 ,  A61P43/00 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: This invention relates to heterocyclic derivatives useful for inhibiting the production of Interleukin-1 (IL-1) and tumor necrosis factor (TNF) and the like, which can be represented by the following formula: ##STR1## to a process for their production, to a pharmaceutical composition containing the same and to uses thereof.

Abstract translation: 本发明涉及可用于抑制白细胞介素-1（IL-1）和肿瘤坏死因子（TNF）等的产生的杂环衍生物，其可以由下式表示：（I） 它们的生产，涉及含有该组合物的药物组合物及其用途。

公开(公告)号：US06348474B1

公开(公告)日：2002-02-19

申请号：US09446110

申请日：2000-02-14

Applicant: Hiroshi Kayakiri ,  Yoshito Abe ,  Hitoshi Hamashima ,  Hitoshi Sawada ,  Tsuyoshi Mizutani ,  Teruo Oku ,  Noritsugu Yamasaki ,  Osamu Onomura ,  Masahiro Nishikawa ,  Takahiro Hiramura ,  Takafumi Imoto

Inventor： Hiroshi Kayakiri ,  Yoshito Abe ,  Hitoshi Hamashima ,  Hitoshi Sawada ,  Tsuyoshi Mizutani ,  Teruo Oku ,  Noritsugu Yamasaki ,  Osamu Onomura ,  Masahiro Nishikawa ,  Takahiro Hiramura ,  Takafumi Imoto

IPC: A61K31435

CPC classification number: C07D241/52 ,  C07D215/48 ,  C07D231/56 ,  C07D239/96 ,  C07D249/18 ,  C07D307/79 ,  C07D333/54 ,  C07D333/62 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

Abstract: A sulfonamide compound of the formula (I): R1—SO2NHCO—A—R2  (I) wherein R1 is alkyl, alkenyl, alkynyl and the like; A is an optionally substituted heteropolycyclic group except benzimidazolyl, indolyl, 4,7-dihydrobenzimidazolyl and 2,3-dihydrobenzoxazinyl; X is alkylene, oxa, oxa(lower)alkylene and the like; and R2 is optionally substituted aryl, substituted biphenylyl and the like, a salt thereof and a pharmaceutical composition comprising the same. The sulfonamide compound is effective for the diseases treatable based on their blood sugar level-depressing activity, cGMP-PDE (especially PDE-V)-inhibiting activity, smooth muscle relaxing activity, bronchodilating activity, vasodilating activity, smooth muscle cell suppressing activity, and antiallergic activity.

Abstract translation: 式（I）的磺酰胺化合物：其中R1是烷基，烯基，炔基等; A是任选取代的杂多环基团，除了苯并咪唑基，吲哚基，4,7-二氢苯并咪唑基和2,3-二氢苯并恶嗪基; X是亚烷基，氧杂，氧杂（低级）亚烷基等; 并且R 2是任选取代的芳基，取代的联苯基等，其盐和包含它们的药物组合物。 磺胺类化合物可以基于其血糖降低活性，cGMP-PDE（特别是PDE-V）抑制活性，平滑肌松弛活性，支气管扩张活性，血管舒张活性，平滑肌细胞抑制活性，以及 抗过敏活性。

公开(公告)号：US06242474B1

公开(公告)日：2001-06-05

申请号：US09446619

申请日：2000-03-21

Applicant: Noritsugu Yamasaki ,  Takafumi Imoto ,  Takahiro Hiramura ,  Osamu Onomura ,  Masahiro Nishikawa ,  Hiroshi Kayakiri ,  Yoshito Abe ,  Hitoshi Hamashima ,  Hitoshi Sawada

Inventor： Noritsugu Yamasaki ,  Takafumi Imoto ,  Takahiro Hiramura ,  Osamu Onomura ,  Masahiro Nishikawa ,  Hiroshi Kayakiri ,  Yoshito Abe ,  Hitoshi Hamashima ,  Hitoshi Sawada

IPC: A61K314164

CPC classification number: C07D213/78 ,  C07C311/51 ,  C07D213/81 ,  C07D233/64 ,  C07D233/68 ,  C07D409/06

Abstract: Novel aromatic ring derivatives represented by formula (I) or their pharmaceutical acceptable salts are provided. wherein Nu represents a 5- or 6-membered aromatic ring; ch1 and ch2 each represents a cross-linking group; and A represents an aromatic ring. These compounds have blood sugar-depressing activity or PDE 5 inhibitory activity and are useful as medicines for treating impaired glucose tolerance, diabetes, diabetic complications, syndrome of insulin-resistance, polycystic ovary syndrome, hyperlipidemia, atherosclerosis, cardiovascular disorders, hyperglycemia, hypertension, stenocardia, pulmonary hypertension, congestive heart failure, glomerulopathy, tubulointerstitial disorders, renal failure, angiostenosis, distal angiopathy, cerebral apoplexy, chronic reversible obstructions, autoimmune diseases, allergic rhinitis, urticaria, glaucoma, diseases characterized by enteromotility disorders, impotence, nephritis, cachexia, pancreatitis, restenosis after PTCA, etc.

Abstract translation: 提供由式（I）表示的新颖芳环衍生物或其药学上可接受的盐。其中Nu表示5-或6-元芳环; ch1和ch2各自表示交联基团; 并且A代表芳香环。这些化合物具有抑制血糖的活性或PDE 5抑制活性，可用作治疗糖耐量异常，糖尿病，糖尿病并发症，胰岛素抵抗综合征，多囊卵巢综合症，高脂血症，动脉粥样硬化， 心血管疾病，高血糖症，高血压，心律失常，肺动脉高压，充血性心力衰竭，肾小球病，肾小管间质性疾病，肾衰竭，血管狭窄，远端血管病，脑中风，慢性可逆障碍，自身免疫性疾病，过敏性鼻炎，荨麻疹，青光眼，以肠蠕动为特征的疾病 疾病，阳ence，肾炎，恶病质，胰腺炎，PTCA后再狭窄等。

公开(公告)号：US5994368A

公开(公告)日：1999-11-30

申请号：US809416

申请日：1997-04-25

Applicant: Teruo Oku ,  Hiroshi Kayakiri ,  Shigeki Satoh ,  Yoshito Abe ,  Yuki Sawada ,  Takayuki Inoue ,  Hirokazu Tanaka

Inventor： Teruo Oku ,  Hiroshi Kayakiri ,  Shigeki Satoh ,  Yoshito Abe ,  Yuki Sawada ,  Takayuki Inoue ,  Hirokazu Tanaka

IPC: C07D237/28 ,  A61K31/47 ,  A61K31/495 ,  A61K31/505 ,  A61K31/517 ,  A61K31/535 ,  A61P29/00 ,  A61P37/00 ,  A61P37/02 ,  A61P37/08 ,  A61P43/00 ,  C07D215/26 ,  C07D215/38 ,  C07D215/40 ,  C07D215/42 ,  C07D215/48 ,  C07D237/30 ,  C07D239/74 ,  C07D241/38 ,  C07D241/40 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  A01N43/42 ,  C07D215/16

CPC classification number: C07D401/12 ,  C07D215/26 ,  C07D215/40 ,  C07D215/42 ,  C07D215/48 ,  C07D241/40 ,  C07D401/14 ,  C07D403/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

Abstract: This invention relates to a compound of the formula: ##STR1## wherein Z is a group of the formula: ##STR2## in which X.sup.1 is N or C--R.sup.1,X.sup.2 is N or C--R.sup.9,X.sup.3 is N or C--R.sup.2,R.sup.1 is lower alkyl,R.sup.2 is hydrogen, lower alkyl, etc.,R.sup.9 is hydrogen or lower alkyl,R.sup.3 is halogen, etc.,R.sup.4 is halogen, etc.,R.sup.5 is a group of the formula: ##STR3## A is lower alkylene, and Y is O, etc.,and pharmaceutically acceptable salts thereof, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to methods to using the same therapeutically in the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.

Abstract translation: 本发明涉及下式化合物：其中Z为下式基团：其中X1为N或C-R1，X2为N或C-R9，X3为N或C-R2，R1为低级烷基， R2是氢，低级烷基等，R9是氢或低级烷基，R3是卤素等，R4是卤素等，R5是下式的基团：A是低级亚烷基，Y是O等 及其药学上可接受的盐，其制备方法，涉及包含其的药物组合物，以及在预防和/或治疗缓激肽或其类似物介导的人或动物疾病中的治疗方法 。

公开(公告)号：US5750699A

公开(公告)日：1998-05-12

申请号：US662198

申请日：1996-06-12

Applicant: Teruo Oku ,  Hiroshi Kayakiri ,  Shigeki Satoh ,  Yoshito Abe ,  Yuki Sawada ,  Hirokazu Tanaka

Inventor： Teruo Oku ,  Hiroshi Kayakiri ,  Shigeki Satoh ,  Yoshito Abe ,  Yuki Sawada ,  Hirokazu Tanaka

IPC: C07D471/04 ,  C07D471/02

CPC classification number: C07D471/04

Abstract: The invention relates to bradykinin antagonists of the formula: ##STR1## wherein R.sup.1 is halogen, R.sup.2 and R.sup.3 are each hydrogen, lower alkyl, halo(lower)alkyl or acyl, R.sup.4 is aryl having suitable substituent(s), or a heterocyclic group optionally having suitable substituent(s), Q is O or N--R.sup.11, in which R.sup.11 is hydrogen or acyl, and A is lower alkylene, and pharmaceutically acceptable salts thereof.

Abstract translation: 本发明涉及下式的缓激肽拮抗剂：其中R 1为卤素，R 2和R 3各自为氢，低级烷基，卤代（低级）烷基或酰基，R 4为具有合适取代基的芳基或杂环基 任选具有合适的取代基，Q是O或N-R 11，其中R 11是氢或酰基，A是低级亚烷基，及其药学上可接受的盐。

公开(公告)号：US5708173A

公开(公告)日：1998-01-13

申请号：US660393

申请日：1996-06-07

Applicant: Teruo Oku ,  Hiroshi Kayakiri ,  Shigeki Satoh ,  Yoshito Abe ,  Yuki Sawada ,  Takayuki Inoue ,  Hirokazu Tanaka

Inventor： Teruo Oku ,  Hiroshi Kayakiri ,  Shigeki Satoh ,  Yoshito Abe ,  Yuki Sawada ,  Takayuki Inoue ,  Hirokazu Tanaka

IPC: A61K31/47 ,  A61K31/495 ,  A61K31/498 ,  A61K31/50 ,  A61K31/502 ,  A61K31/505 ,  A61K31/517 ,  A61K31/53 ,  A61P35/00 ,  A61P37/08 ,  A61P43/00 ,  C07D215/24 ,  C07D215/26 ,  C07D215/40 ,  C07D237/10 ,  C07D237/28 ,  C07D239/74 ,  C07D241/42 ,  C07D241/44 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07F7/18 ,  C07D215/20 ,  C07D215/36

CPC classification number: C07D401/12 ,  C07D215/26 ,  C07D237/28 ,  C07D239/74 ,  C07D241/42 ,  C07D401/14 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07F7/1856

Abstract: A compound of the formula: ##STR1## or its salt is prepared by reacting a compound of the formula: ##STR2## with a compound of the formula: ##STR3## Wherein the variables are all defined in claim 1.

Abstract translation: 通过使下式化合物与下式化合物反应制备下式的化合物：其中所有的变量都被定义 在权利要求1中。