公开(公告)号：US20100168159A1

公开(公告)日：2010-07-01

申请号：US12696327

申请日：2010-01-29

Applicant: Hironori Harada ,  Kazuyuki Hattori ,  Kazuya Fujita ,  Masataka Morita ,  Sunao Imada ,  Yoshito Abe ,  Hiromichi Itani ,  Tatsuaki Morokata ,  Hideo Tsutsumi

Inventor： Hironori Harada ,  Kazuyuki Hattori ,  Kazuya Fujita ,  Masataka Morita ,  Sunao Imada ,  Yoshito Abe ,  Hiromichi Itani ,  Tatsuaki Morokata ,  Hideo Tsutsumi

IPC: A61K31/4439 ,  A61K31/4709 ,  C07D471/04 ,  C07D413/14 ,  A61P35/02 ,  A61P37/06 ,  A61P29/00 ,  A61P9/10 ,  A61P35/00

CPC classification number: C07D413/04 ,  C07D417/04 ,  C07D471/04

Abstract: [Problems]To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 agonist activity.[Means for solving]Since the compound of the invention has an S1P1 agonist activity, it is useful as an active ingredient for a treating or preventing agent for a disease caused by unfavorable lymphocytic infiltration, for example, an autoimmune disease such as graft rejection in the transplantation of an organ, bone marrow, or a tissue, a graft-versus-host disease, rheumatic arthritis, multiple sclerosis, systemic lupus erythematosus, a nephrotic syndrome, encephalomeningitis, myasthenia gravis, pancreatitis, hepatitis, nephritis, diabetes, pulmonary disorder, asthma, atopic dermatitis, inflammatory bowel disease, atherosclerosis, ischemia-reperfusion injury, or an inflammatory disease, and further, a disease caused by the abnormal growth or accumulation of cells such as cancer and leukemia.

Abstract translation: [问题]提供一种有用的化合物作为活性成分，用于预防和/或治疗移植器官，骨髓或组织，自身免疫疾病等中的排斥反应，其具有优异的S1P1激动剂 活动。 [解决方法]由于本发明的化合物具有S1P1激动剂活性，因此可用作由不利的淋巴细胞浸润引起的疾病的治疗或预防剂的活性成分，例如自身免疫性疾病如移植排斥反应 器官移植，骨髓或组织，移植物抗宿主病，风湿性关节炎，多发性硬化，系统性红斑狼疮，肾病综合征，脑炎，重症肌无力，胰腺炎，肝炎，肾炎，糖尿病，肺功能障碍 哮喘，特应性皮炎，炎症性肠病，动脉粥样硬化，局部缺血再灌注损伤，炎症性疾病等疾病，以及癌症，白血病等细胞异常生长或积累引起的疾病。

公开(公告)号：US20060004003A1

公开(公告)日：2006-01-05

申请号：US11171320

申请日：2005-07-01

Applicant: Yoshito Abe ,  Kazuhiko Ohne ,  Kentaro Sato ,  Makoto Inoue ,  Mitsuaki Okumura

Inventor： Yoshito Abe ,  Kazuhiko Ohne ,  Kentaro Sato ,  Makoto Inoue ,  Mitsuaki Okumura

IPC: A61K31/5377 ,  A61K31/4745 ,  C07D471/02

CPC classification number: C07D471/04

Abstract: The invention relates to compound of the formula (I) or its salt, in which R1, R2, R3 and R4 are as defined in the description, their use of as medicament, the process for their preparation and use for the treatment of PDE-IV or TNF-α mediated diseases.

Abstract translation: 本发明涉及式（I）化合物或其盐，其中R 1，R 2，R 3和R 0 > 4 如说明书中所定义，它们作为药物的用途，其制备方法和用于治疗PDE-IV或TNF-α介导的疾病。

公开(公告)号：US06194396B1

公开(公告)日：2001-02-27

申请号：US09425207

申请日：1999-10-22

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: A61K314184

CPC classification number: C07D209/48 ,  C07D235/06 ,  C07D235/08 ,  C07D235/12 ,  C07D235/16 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D263/56 ,  C07D277/64 ,  C07D307/79 ,  C07D307/80 ,  C07D307/84 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07F7/1804

Abstract: This invention relates to a heterocyclic compound of the formula wherein a group of the formula: is a group of the formula X is O, S or N-R5, R1 is lower alkyl, etc., R5 is hydrogen, lower alkyl, etc., R2 is hydrogen, halogen, lower alkyl, etc., R3 is halogen, lower alkyl, etc., R4 is amino optionally having suitable substituent(s), and A is lower alkylene, and a salt thereof, to processes for preparation thereof, and to a pharmaceutical composition comprising the same for the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.

Abstract translation: 本发明涉及下式的下式的杂环化合物：式X的基团是O，S或N-R 5，R 1是低级烷基等，R 5是氢，低级烷基等，R 2是 氢，卤素，低级烷基等，R 3为卤素，低级烷基等，R 4为任选具有合适取代基的氨基，A为低级亚烷基及其盐，其制备方法为 包含其用于预防和/或治疗缓激肽或其类似物介导的人或动物疾病的药物组合物。

公开(公告)号：US6083961A

公开(公告)日：2000-07-04

申请号：US776518

申请日：1997-02-03

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: C07D209/48 ,  C07D235/06 ,  C07D235/08 ,  C07D235/12 ,  C07D235/16 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D263/56 ,  C07D277/64 ,  C07D307/79 ,  C07D307/80 ,  C07D307/84 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D498/04 ,  C07F7/18 ,  A61K31/415 ,  A61K31/42 ,  A61K31/44 ,  A61K31/34 ,  C07D405/12

CPC classification number: C07D209/48 ,  C07D235/06 ,  C07D235/08 ,  C07D235/12 ,  C07D235/16 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D263/56 ,  C07D277/64 ,  C07D307/79 ,  C07D307/80 ,  C07D307/84 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07F7/1856

Abstract: This invention relates to a heterocyclic compound of the formula: ##STR1## wherein a group of the formula: ##STR2## is a group of the formula: ##STR3## etc., X is O, S or N--R.sup.5,R.sup.1 is lower alkyl, etc.,R.sup.5 is hydrogen, lower alkyl, etc.,R.sup.2 is hydrogen, halogen, lower alkyl, etc.,R.sup.3 is halogen, lower alkyl, etc.,R.sup.4 is amino optionally having suitable substituent(s), andA is lower alkylene,and a salt thereof, to processes for preparation thereof, and to a pharmaceutical composition comprising the same for the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.

Abstract translation: PCT No.PCT / JP95 / 01478 Sec。 371日期1997年2月3日 102（e）日期1997年2月3日PCT提交1995年7月25日PCT公布。 公开号WO96 / 04251 日本特开1996年2月15日本发明涉及下式的杂环化合物：其中式为下式的基团：X为O，S或N-R 5，R 1为低级烷基等。 R 5为氢，低级烷基等，R 2为氢，卤素，低级烷基等，R 3为卤素，低级烷基等，R 4为任选具有适当取代基的氨基，A为低级亚烷基， 及其盐，其制备方法，以及包含其的药物组合物，用于预防和/或治疗人类或动物中缓激肽或其类似物介导的疾病。

公开(公告)号：US5478827A

公开(公告)日：1995-12-26

申请号：US269520

申请日：1994-07-01

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：US07459451B2

公开(公告)日：2008-12-02

申请号：US11171320

申请日：2005-07-01

Applicant: Yoshito Abe ,  Kazuhiko Ohne ,  Kentaro Sato ,  Makoto Inoue ,  Mitsuaki Okumura

Inventor： Yoshito Abe ,  Kazuhiko Ohne ,  Kentaro Sato ,  Makoto Inoue ,  Mitsuaki Okumura

IPC: A61K31/535 ,  A61K31/44 ,  A01N43/42 ,  C07D413/00 ,  C07D471/02 ,  C07D491/02 ,  C07D498/02 ,  C07D513/02 ,  C07D515/02

CPC classification number: C07D471/04

Abstract: The invention relates to compound of the formula (I) or its salt, in which R1, R2, R3 and R4 are as defined in the description, their use of as medicament, the process for their preparation and use for the treatment of PDE-IV or TNF-α mediated diseases.

Abstract translation: 本发明涉及式（I）化合物或其盐，其中R 1，R 2，R 3和R 4如说明书中所定义，它们作为药物的用途，其制备方法和用于治疗PDE- IV或TNF-α介导的疾病。

公开(公告)号：US07317009B2

公开(公告)日：2008-01-08

申请号：US11500293

申请日：2006-08-08

Applicant: Yoshito Abe ,  Makoto Inoue ,  Tsuyoshi Mizutani ,  Kozo Sawada ,  Kazuhiko Ohne ,  Mitsuaki Okumura ,  Yuki Sawada ,  Kenichiro Imamura

Inventor： Yoshito Abe ,  Makoto Inoue ,  Tsuyoshi Mizutani ,  Kozo Sawada ,  Kazuhiko Ohne ,  Mitsuaki Okumura ,  Yuki Sawada ,  Kenichiro Imamura

IPC: C07D487/04 ,  A61K31/5025

CPC classification number: C07D487/04

Abstract: The invention relates to compound of the formula (I) or its salt, in which R1, R2, R3 and R4 are as defined in the description, their use of as medicament, the process for their preparation and use for the treatment of PDE-IV or TNF-α mediated diseases

Abstract translation: 本发明涉及式（I）化合物或其盐，其中R 1，R 2，R 3和R 0 > 4 如说明书中所定义，它们作为药物的用途，其制备方法和用于治疗PDE-IV或TNF-α介导的疾病

公开(公告)号：US20070247530A1

公开(公告)日：2007-10-25

申请号：US11661709

申请日：2005-07-29

Applicant: Yoshihisa Takahasi ,  Hisakazu Kikuchi ,  Shogo Muramatsu ,  Yoshito Abe ,  Naoki Mizutani

Inventor： Yoshihisa Takahasi ,  Hisakazu Kikuchi ,  Shogo Muramatsu ,  Yoshito Abe ,  Naoki Mizutani

IPC: H04N9/73 ,  G06T3/40 ,  H04N9/04

CPC classification number: G06T3/4015 ,  H04N1/648 ,  H04N9/045

Abstract: To achieve more appropriate interpolation of a missing pixel, an image is input to a processing section for interpolation. The interpolation is applied utilizing image data of pixels located around the pixel to be interpolated. Specifically, correlations between the image data of the pixels to be interpolated, and pixel data in a horizontal direction, vertical direction, and diagonal direction, are compared to one another; pixel data having stronger correlation is used for the interpolation. Correlation between the image data of the pixels to be interpolated and which direction is strong is determined, so that different weighting for interpolation is used accordingly.

Abstract translation: 为了实现对缺失像素的更合适的插值，将图像输入到用于插值的处理部分。 使用位于要内插的像素周围的像素的图像数据来应用插值。 具体而言，将要内插的像素的图像数据与水平方向，垂直方向和对角线方向上的像素数据之间的相关性相互比较; 使用具有较强相关性的像素数据进行插值。 确定要插值的像素的图像数据和哪个方向是强的相关性，使得相应地使用用于插值的不同加权。

公开(公告)号：US07153854B2

公开(公告)日：2006-12-26

申请号：US10747079

申请日：2003-12-30

Applicant: Yoshito Abe ,  Makoto Inoue ,  Tsuyoshi Mizutani ,  Kozo Sawada ,  Kazuhiko Ohne ,  Mitsuaki Okumura ,  Yuki Sawada ,  Kenichiro Imamura

Inventor： Yoshito Abe ,  Makoto Inoue ,  Tsuyoshi Mizutani ,  Kozo Sawada ,  Kazuhiko Ohne ,  Mitsuaki Okumura ,  Yuki Sawada ,  Kenichiro Imamura

IPC: C07D487/04 ,  A61K31/5025

CPC classification number: C07D487/04

Abstract: The invention relates to compound of the formula (I) or its salt, in which R1, R2, R3 and R4 are as defined in the description, their use of as medicament, the process for their preparation and use for the treatment of PDE-IV or TNF-α mediated diseases

Abstract translation: 本发明涉及式（I）化合物或其盐，其中R 1，R 2，R 3和R 0 > 4 如说明书中所定义，它们作为药物的用途，其制备方法和用于治疗PDE-IV或TNF-α介导的疾病

公开(公告)号：US06911469B2

公开(公告)日：2005-06-28

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: G06Q50/10 ,  A61K20060101 ,  A61K31/381 ,  A63B69/36 ,  C07D20060101 ,  C07D215/48 ,  C07D231/56 ,  C07D239/96 ,  C07D241/52 ,  C07D249/18 ,  C07D307/79 ,  C07D333/54 ,  C07D333/56 ,  C07D333/62 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07F20060101 ,  A61K31/34

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：<？in-line-formula description =“In-line Formulas”end =“lead”→> R 2 NHCO-AXR 2（I）<？in-line-formula description =“In-line Formulas”end =“tail”？>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。