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    Fused phenol derivatives
    1.
    发明授权
    Fused phenol derivatives 失效
    稠油酚衍生物

    公开(公告)号：US5750544A

    公开(公告)日：1998-05-12

    申请号：US635318

    申请日：1996-04-19

    申请人： Shuichi Ohuchida ,  Fumio Nambu ,  Masaaki Toda

    发明人： Shuichi Ohuchida ,  Fumio Nambu ,  Masaaki Toda

    IPC分类号： C07D311/58 ,  C07D405/06 ,  C07D521/00 ,  A61K31/44

    CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56 ,  C07D311/58 ,  C07D405/06

    摘要： Fused phenol derivatives of the formula (I): ##STR1## (wherein R.sup.1 and R.sup.2 each, independently, is H, halogen, trifluoromethyl, cyano, (substituted) alkyl, alkoxy, cycloalkyl, COOH, COOR.sup.6 (in which R.sup.6 is C1-6 alkyl), alkenyl or R.sup.1 and R.sup.2, taken together, is --CH.dbd.CH--CH.dbd.CH--, when R.sup.1 and R.sup.2 are ortho to each other; A is alkylene, alkenylene, oxyalkylene or ##STR2## (in which m is 1-6); B is a monocyclic hetero ring containing a nitrogen atom; G is --OR.sup.3A or --NR.sup.3B R.sup.3C (in which R.sup.3A, R.sup.3B and R.sup.3C each, independently, is H, alkyl, acyl, or alkoxyalkyl); R.sup.4 and R.sup.5 each, independently, is H, alkyl, or R.sup.4, R.sup.5 together with the carbon atom to which they are attached represent C4-7 cycloalkyl; and n is 1-3; non-toxic salts thereof, non-toxic acid addition salts thereof, and hydrates thereof. The compounds of the formula (I) have inhibitory activities on TXA.sub.2 synthetase and on 5-lipoxygenase and/or a scavenging activity on active oxygen species, and are useful for the prevention and/or the treatment of thrombosis, arteriosclerosis, ischemic heart diseases or brain diseases, bronchial asthma, renal inflammation, rheumatism, arthritis, gout, psoriasis, ulcerative colitis, trichophytosis, cardiac infarction, allergic diseases, etc.

    摘要翻译： （I）的稠合酚衍生物：其中R 1和R 2各自独立地是H，卤素，三氟甲基，氰基，（取代的）烷基，烷氧基，环烷基，COOH，COOR 6（其中R 6 当R1和R2彼此邻位时，A是亚烷基，亚烯基，氧化烯或（IMAGE）（在C 1 -C 6烷基中），链烯基或R 1和R 2一起是-CH = CH-CH = CH- 其中m是1-6）; B是含有氮原子的单环杂环; G是-OR3A或-NR3BR3C（其中R3A，R3B和R3C各自独立地是H，烷基，酰基或烷氧基烷基）; R4 且R 5各自独立地为H，烷基或R 4，R 5与它们所连接的碳原子一起代表C4-7环烷基; n为1-3;其无毒盐，无毒酸加成盐 式（I）化合物对TXA2合成酶和5-脂氧合酶和/或对活性氧物质的清除活性具有抑制活性，可用于预防和/或治疗o 血栓形成，动脉硬化，缺血性心脏病或脑疾病，支气管哮喘，肾脏炎症，风湿病，关节炎，痛风，牛皮癣，溃疡性结肠炎，毛发症，心肌梗塞，过敏性疾病等。

    Fused phenol derivatives
    2.
    发明授权
    Fused phenol derivatives 失效
    稠油酚衍生物

    公开(公告)号：US5534536A

    公开(公告)日：1996-07-09

    申请号：US294015

    申请日：1994-08-23

    申请人： Shuichi Ohuchida ,  Fumio Nambu ,  Masaaki Toda

    发明人： Shuichi Ohuchida ,  Fumio Nambu ,  Masaaki Toda

    IPC分类号： C07D311/58 ,  C07D405/06 ,  C07D521/00 ,  A61K31/415

    CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56 ,  C07D311/58 ,  C07D405/06

    摘要： Fused phenol compounds of the formula (I): ##STR1## (wherein R.sup.1 and R.sup.2 each, independently, is H, halogen, trifluoromethyl, cyano, (substituted) alkyl, alkoxy, cycloalkyl, COOH, COOR.sup.6 (in which R.sup.6 is C1-6 alkyl), alkenyl or R.sup.1 and R.sup.2, taken together, is --CH.dbd.CH--CH.dbd.CH--, when R.sup.1 and R.sup.2 are ortho to each other; A is alkylene, alkenylene, oxyalkylene or ##STR2## (in which m is 1-6); B is a monocyclic hetero ring containing a nitrogen atom; G is --OR.sup.3A or --NR.sup.3B R.sup.3C (in which R.sup.3A, R.sup.3B and R.sup.3C each, independently, is H, alkyl, acyl, or alkoxyalkyl); R.sup.4 and R.sup.5 each, independently, is H, alkyl, or R.sup.4, R.sup.5 together with the carbon atom to which they are attached represent C4-7 cycloalkyl; and n is 1-3; non-toxic salts thereof, non-toxic acid addition salts thereof, and hydrates thereof.The compounds of the formula (I) have inhibitory activities on TXA.sub.2 synthetase and on 5-lipoxygenase and/or a scavenging activity on active oxygen species, and are useful for the prevention and/or the treatment of thrombosis, arteriosclerosis, ischemic heart diseases or brain diseases, bronchial asthma, renal inflammation, rheumatism, arthritis, gout, psoriasis, ulcerative colitis, trichophytosis, cardiac infarction, allergic diseases, etc.

    摘要翻译： 式（I）的稠合酚化合物：其中R 1和R 2各自独立地是H，卤素，三氟甲基，氰基，（取代的）烷基，烷氧基，环烷基，COOH，COOR 6（其中R 6 当R1和R2彼此邻位时，A是亚烷基，亚烯基，氧化烯或（IMAGE）（在C 1 -C 6烷基中），链烯基或R 1和R 2一起是-CH = CH-CH = CH- 其中m是1-6）; B是含有氮原子的单环杂环; G是-OR3A或-NR3BR3C（其中R3A，R3B和R3C各自独立地是H，烷基，酰基或烷氧基烷基）; R4 且R 5各自独立地为H，烷基或R 4，R 5与它们所连接的碳原子一起代表C4-7环烷基; n为1-3;其无毒盐，无毒酸加成盐 式（I）化合物对TXA2合成酶和5-脂氧合酶和/或对活性氧物质的清除活性具有抑制活性，可用于预防和/或治疗 血栓形成，动脉硬化，缺血性心脏病或脑疾病，支气管哮喘，肾脏炎症，风湿病，关节炎，痛风，牛皮癣，溃疡性结肠炎，毛发症，心肌梗塞，过敏性疾病等。

    Indole derivatives
    3.
    发明授权
    Indole derivatives 失效
    吲哚衍生物

    公开(公告)号：US07291644B2

    公开(公告)日：2007-11-06

    申请号：US11412879

    申请日：2006-04-28

    申请人： Kazuhiko Torisu ,  Maki Iwahashi ,  Kaoru Kobayashi ,  Fumio Nambu

    发明人： Kazuhiko Torisu ,  Maki Iwahashi ,  Kaoru Kobayashi ,  Fumio Nambu

    IPC分类号： A61K31/335 ,  C07D265/36 ,  C07D405/00 ,  C07D209/02 ,  C07D209/04

    CPC分类号： C07D405/12 ,  A61K31/405 ,  A61K31/422 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/538 ,  C07D209/22 ,  C07D401/12 ,  C07D413/12

    摘要： Compounds represented by formula (I) wherein all symbols represent the same meanings as described in specification and salts thereof. Since the compound represented by the formula (I) binds and antagonizes to DP receptor, it is useful for the prevention or treatment against the disease such as allergic disorder, diseases accompanied with itching, secondary diseases generated by behaviors caused by itching, inflammation, chronic obstructive pulmonary disease, ischemic reperfusion disorder, pleuritis complicated by rheumatoid arthritis, cerebrovascular disease, and ulcerative colitis.

    摘要翻译： 由式（I）表示的化合物，其中所有符号表示与说明书及其盐中所述相同的含义。 由于式（I）表示的化合物与DP受体结合并拮抗，因此可用于预防或治疗诸如过敏性疾病，伴有瘙痒的疾病，由瘙痒引起的行为引起的继发性疾病，炎症，慢性 阻塞性肺病，局部缺血再灌注障碍，类风湿关节炎并发的胸膜炎，脑血管疾病和溃疡性结肠炎。

    Carboxylic acid compounds and medicinal compositions containing the same as the active ingredient
    4.
    发明授权
    Carboxylic acid compounds and medicinal compositions containing the same as the active ingredient 有权
    羧酸化合物和含有与活性成分相同的药物组合物

    公开(公告)号：US08138335B2

    公开(公告)日：2012-03-20

    申请号：US12551860

    申请日：2009-09-01

    申请人： Atsushi Naganawa ,  Maki Iwahashi ,  Atsushi Kinoshita ,  Atsushi Shimabukuro ,  Seiji Ogawa ,  Koji Yano ,  Kaoru Kobayashi ,  Yutaka Okada ,  Yoko Kishida ,  Shouji Kawauchi ,  Kohki Tsukamoto ,  Yoko Matsunaga ,  Fumio Nambu

    发明人： Atsushi Naganawa ,  Maki Iwahashi ,  Atsushi Kinoshita ,  Atsushi Shimabukuro ,  Seiji Ogawa ,  Koji Yano ,  Kaoru Kobayashi ,  Yutaka Okada ,  Yoko Kishida ,  Shouji Kawauchi ,  Kohki Tsukamoto ,  Yoko Matsunaga ,  Fumio Nambu

    IPC分类号： C07D265/36 ,  A61K31/535

    CPC分类号： C07D307/80 ,  A61K31/343 ,  A61K31/538 ,  C07D265/36 ,  C07D317/48

    摘要： A compound represented by formula (I) wherein the symbols in the formula are the same meanings as those in specification, salts thereof, solvates thereof, or prodrugs thereof binds to DP receptor and shows antagonistic activity for DP receptor. Thus, it is useful for prevention and/or treatment of diseases such as allergic disease (e.g., allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, urticaria, eczema, diseases accompanied by itch (e.g., atopic dermatitis and urticaria), diseases (e.g., cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (e.g., scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis, etc. Since it specifically binds to DP receptor and binds weakly to other prostaglandins receptors, they can be pharmaceuticals having little side effect.

    摘要翻译： 由式（I）表示的化合物，其中式中的符号与说明书中的符号相同，其盐，溶剂合物或其前药与DP受体结合并显示DP受体的拮抗活性。 因此，它可用于预防和/或治疗过敏性疾病（例如过敏性鼻炎，过敏性结膜炎，特应性皮炎，支气管哮喘和食物过敏），系统性肥大细胞增多症，伴有全身性肥大细胞活化的病症，过敏性休克， 支气管收缩，荨麻疹，湿疹，伴有瘙痒的疾病（例如特应性皮炎和荨麻疹），伴随瘙痒的行为的结果产生的疾病（例如白内障，视网膜脱离，炎症，感染和睡眠障碍）（例如， 搔抓和殴打），炎症，慢性阻塞性肺疾病，缺血再灌注损伤，脑血管意外，慢性类风湿关节炎，胸膜炎，溃疡性结肠炎等。由于其特异性结合DP受体并且弱结合到其他前列腺素受体，它们可以是具有 小副作用。

    Carboxylic acid compounds and a pharmaceutical agent comprising the compound as the active ingredient
    5.
    发明授权
    Carboxylic acid compounds and a pharmaceutical agent comprising the compound as the active ingredient 有权
    羧酸化合物和包含该化合物作为活性成分的药剂

    公开(公告)号：US07351705B2

    公开(公告)日：2008-04-01

    申请号：US10507885

    申请日：2003-03-06

    申请人： Maki Iwahashi ,  Kaoru Kobayashi ,  Fumio Nambu

    发明人： Maki Iwahashi ,  Kaoru Kobayashi ,  Fumio Nambu

    IPC分类号： C07D413/12 ,  C07D265/36 ,  A61K31/538

    CPC分类号： C07D319/20 ,  C07D209/12 ,  C07D265/36 ,  C07D307/80 ,  C07D327/06

    摘要： A carboxylic acid compound represented by formula (I): (meanings of the symbols in the formula are as mentioned in the specification) and a pharmaceutical agent comprising the compound. Since the compound represented by formula (I) binds to a DP receptor and shows antagonistic activity for the DP receptor, it is useful for prevention and/or treatment of diseases such as allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like.

    摘要翻译： 由式（I）表示的羧酸化合物：（式中符号的含义如说明书中所述）和包含该化合物的药剂。 由于式（I）表示的化合物与DP受体结合，对DP受体具有拮抗作用，因此可用于预防和/或治疗过敏性疾病（如过敏性鼻炎，过敏性结膜炎，特应性皮炎， 支气管哮喘和食物过敏），系统性肥大细胞增多症，伴有系统性肥大细胞活化的疾病，过敏性休克，支气管收缩，荨麻疹，湿疹，伴有瘙痒的疾病（如特应性皮炎和荨麻疹），疾病（如白内障，视网膜脱离，炎症 ，感染和睡眠障碍），其由伴随瘙痒的行为（例如搔抓和殴打），炎症，慢性阻塞性肺疾病，缺血再灌注损伤，脑血管意外，慢性类风湿性关节炎，胸膜炎，溃疡性结肠炎和 喜欢。

    Carboxylic acid compounds and medicinal compositions containing the same as the active ingredient
    6.
    发明申请
    Carboxylic acid compounds and medicinal compositions containing the same as the active ingredient 有权
    羧酸化合物和含有与活性成分相同的药物组合物

    公开(公告)号：US20070004716A1

    公开(公告)日：2007-01-04

    申请号：US10572578

    申请日：2004-09-16

    申请人： Atsushi Naganawa ,  Maki Iwahashi ,  Atsushi Kinoshita ,  Atsushi Shimabukuro ,  SeijiKoji Ogawa ,  Koji Yano ,  Kaoru Kobayashi ,  Yutaka Okada ,  Yoko Kishida ,  Shouji Kawauchi ,  Kohki Tsukamoto ,  Yoko Matsunaga ,  Fumio Nambu

    发明人： Atsushi Naganawa ,  Maki Iwahashi ,  Atsushi Kinoshita ,  Atsushi Shimabukuro ,  SeijiKoji Ogawa ,  Koji Yano ,  Kaoru Kobayashi ,  Yutaka Okada ,  Yoko Kishida ,  Shouji Kawauchi ,  Kohki Tsukamoto ,  Yoko Matsunaga ,  Fumio Nambu

    IPC分类号： A61K31/538 ,  C07D265/36

    CPC分类号： C07D307/80 ,  A61K31/343 ,  A61K31/538 ,  C07D265/36 ,  C07D317/48

    摘要： A compound represented by formula (I) wherein the symbols in the formula are the same meanings as those in specification, salts thereof, solvates thereof, or prodrugs thereof binds to DP receptor and shows antagonistic activity for DP receptor. Thus, it is useful for prevention and/or treatment of diseases such as allergic disease (e.g., allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, urticaria, eczema, diseases accompanied by itch (e.g., atopic dermatitis and urticaria), diseases (e.g., cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (e.g., scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis, etc. Since it specifically binds to DP receptor and binds weakly to other prostaglandins receptors, they can be pharmaceuticals having little side effect.

    摘要翻译： 由式（I）表示的化合物，其中式中的符号与说明书中的符号相同，其盐，溶剂合物或其前药与DP受体结合并显示DP受体的拮抗活性。 因此，它可用于预防和/或治疗过敏性疾病（例如过敏性鼻炎，过敏性结膜炎，特应性皮炎，支气管哮喘和食物过敏），系统性肥大细胞增多症，伴有全身性肥大细胞活化的病症，过敏性休克， 支气管收缩，荨麻疹，湿疹，伴有瘙痒的疾病（例如特应性皮炎和荨麻疹），伴随瘙痒的行为的结果产生的疾病（例如白内障，视网膜脱离，炎症，感染和睡眠障碍）（例如， 搔抓和殴打），炎症，慢性阻塞性肺疾病，缺血再灌注损伤，脑血管意外，慢性类风湿关节炎，胸膜炎，溃疡性结肠炎等。由于其特异性结合DP受体并且弱结合到其他前列腺素受体，它们可以是具有 小副作用。

    CARBOXYLIC ACID COMPOUNDS AND MEDICINAL COMPOSITIONS CONTAINING THE SAME AS THE ACTIVE INGREDIENT
    9.
    发明申请
    CARBOXYLIC ACID COMPOUNDS AND MEDICINAL COMPOSITIONS CONTAINING THE SAME AS THE ACTIVE INGREDIENT 有权
    羧酸化合物和含有相同活性成分的药物组合物

    公开(公告)号：US20100029631A1

    公开(公告)日：2010-02-04

    申请号：US12551860

    申请日：2009-09-01

    申请人： Atsushi Naganawa ,  Maki Iwahashi ,  Atsushi Kinoshita ,  Atsushi Shimabukuro ,  Seiji Ogawa ,  Koji Yano ,  Kaoru Kobayashi ,  Yutaka Okada ,  Yoko Kishida ,  Shouji Kawauchi ,  Kohki Tsukamoto ,  Yoko Matsunaga ,  Fumio Nambu

    发明人： Atsushi Naganawa ,  Maki Iwahashi ,  Atsushi Kinoshita ,  Atsushi Shimabukuro ,  Seiji Ogawa ,  Koji Yano ,  Kaoru Kobayashi ,  Yutaka Okada ,  Yoko Kishida ,  Shouji Kawauchi ,  Kohki Tsukamoto ,  Yoko Matsunaga ,  Fumio Nambu

    IPC分类号： A61K31/538 ,  C07D265/36 ,  A61P37/08 ,  A61P11/06

    CPC分类号： C07D307/80 ,  A61K31/343 ,  A61K31/538 ,  C07D265/36 ,  C07D317/48

    摘要： A compound represented by formula (I) wherein the symbols in the formula are the same meanings as those in specification, salts thereof, solvates thereof, or prodrugs thereof binds to DP receptor and shows antagonistic activity for DP receptor. Thus, it is useful for prevention and/or treatment of diseases such as allergic disease (e.g., allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, urticaria, eczema, diseases accompanied by itch (e.g., atopic dermatitis and urticaria), diseases (e.g., cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (e.g., scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis, etc. Since it specifically binds to DP receptor and binds weakly to other prostaglandins receptors, they can be pharmaceuticals having little side effect.

    摘要翻译： 由式（I）表示的化合物，其中式中的符号与说明书中的符号相同，其盐，溶剂合物或其前药与DP受体结合并显示DP受体的拮抗活性。 因此，它可用于预防和/或治疗过敏性疾病（例如过敏性鼻炎，过敏性结膜炎，特应性皮炎，支气管哮喘和食物过敏），系统性肥大细胞增多症，伴有全身性肥大细胞活化的病症，过敏性休克， 支气管收缩，荨麻疹，湿疹，伴有瘙痒的疾病（例如特应性皮炎和荨麻疹），伴随瘙痒的行为的结果产生的疾病（例如白内障，视网膜脱离，炎症，感染和睡眠障碍）（例如， 搔抓和殴打），炎症，慢性阻塞性肺疾病，缺血再灌注损伤，脑血管意外，慢性类风湿关节炎，胸膜炎，溃疡性结肠炎等。由于其特异性结合DP受体并且弱结合到其他前列腺素受体，它们可以是具有 小副作用。