公开(公告)号：US09018238B2

公开(公告)日：2015-04-28

申请号：US13201309

申请日：2009-12-28

申请人： Masako Okamoto ,  Kiyoshi Takayama

发明人： Masako Okamoto ,  Kiyoshi Takayama

IPC分类号： A61K31/422 ,  A61K31/433 ,  A61K31/4439 ,  C07D413/06 ,  C07D413/14 ,  C07D417/14 ,  C07D413/04 ,  C07D263/18

CPC分类号： C07D413/04 ,  A61K31/422 ,  A61K31/433 ,  A61K31/4439 ,  C07D263/18 ,  C07D413/06 ,  C07D413/14 ,  C07D417/14

摘要： There is provided an inhibitor that inhibits casein kinase 1δ and casein kinase 1ε, and thus, there is also provided a pharmaceutical agent useful for the treatment and/or prevention of a disease, with the pathological condition of which the mechanism of activation of casein kinase 1δ or casein kinase 1ε is associated. Particularly, the above-described inhibitor is used to provide a pharmaceutical agent useful for the treatment of circadian rhythm disorder (including sleep disorder), central neurodegenerative disease, and cancer.An inhibitor of casein kinase 1δ and casein kinase 1ε, which comprises, as an active ingredient, an oxazolone derivative represented by the following general formula (1), a salt thereof, a solvate thereof, or a hydrate thereof: [wherein, in the formula (1), each of R1 and R2 independently represents any one of a substituted or unsubstituted 6-membered or 5-membered heterocyclic group optionally having a condensed ring, a substituted or unsubstituted aromatic hydrocarbon group optionally having a condensed ring, and a substituted or unsubstituted aromatic hydrocarbon lower alkyl group or aromatic hydrocarbon lower alkenyl group optionally having a condensed ring.]

摘要翻译： 提供了抑制酪蛋白激酶1δ和酪蛋白激酶1的抑制剂，因此，还提供了可用于治疗和/或预防疾病的药剂，其病理状况是酪蛋白的活化机制 激酶1δ或酪蛋白激酶1＆egr; 已关联的。 特别地，上述抑制剂用于提供可用于治疗昼夜节律紊乱（包括睡眠障碍），中枢神经变性疾病和癌症的药剂。 酪蛋白激酶1δ和酪蛋白激酶1抑制剂，其包含作为活性成分的由以下通式（1）表示的恶唑酮衍生物，其盐，其溶剂化物或其水合物：[其中，在 式（1）中，R 1和R 2各自独立地表示任选具有稠环的取代或未取代的6元或5元杂环基，任选具有稠环的取代或未取代的芳香族烃基， 取代或未取代的芳烃低级烷基或任选具有稠环的芳烃低级链烯基。

公开(公告)号：US08124744B2

公开(公告)日：2012-02-28

申请号：US12299229

申请日：2007-05-01

申请人： Masato Kashimura ,  Madoka Kawamura ,  Toshifumi Asaka ,  Kiyoshi Takayama ,  Haruhisa Ogita

发明人： Masato Kashimura ,  Madoka Kawamura ,  Toshifumi Asaka ,  Kiyoshi Takayama ,  Haruhisa Ogita

IPC分类号： C07H17/08

CPC分类号： C07H17/08 ,  A61K31/7048 ,  A61K31/7052 ,  C07H17/00

摘要： Compounds represented by formula (I) and the formula (IV) have an inhibitory activity of MMP-9 production, therefore, are useful as a medicine agent with fewer side effects than conventional MMP enzyme activity inhibitors, as a prophylactic and therapeutic drug for oncogenic angiogenesis, chronic rheumatoid arthritis, vascular intimal thickening after a percutaneous coronary transluminal angioplasty, vascular atherosclerosis, hemorrhagic apoplexy, acute myocardial infarction, chronic heart failure, aneurysm, lung cancer metastasis, adult respiratory distress syndrome, asthma, interstitial pulmonary fibrosis, chronic rhinosinusitis, bronchitis or chronic obstructive pulmonary disease (COPD).

摘要翻译： 由式（I）和式（IV）表示的化合物具有抑制MMP-9产生的活性，因此作为一种具有比常规MMP酶活性抑制剂更少副作用的药剂可用作致癌剂的预防和治疗药物 血管生成，慢性类风湿关节炎，经皮冠状动脉腔内血管成形术后血管内膜增厚，血管动脉粥样硬化，出血性中风，急性心肌梗塞，慢性心力衰竭，动脉瘤，肺癌转移，成人呼吸窘迫综合征，哮喘，间质性肺纤维化，慢性鼻鼻窦炎， 支气管炎或慢性阻塞性肺疾病（COPD）。

公开(公告)号：US20090088395A1

公开(公告)日：2009-04-02

申请号：US11917845

申请日：2006-06-21

申请人： Kiyoshi Takayama

发明人： Kiyoshi Takayama

IPC分类号： A61K31/7028 ,  C07H17/08

CPC分类号： A61K31/7048

摘要： For the purpose of treatment and/or prevention of pulmonary disorders caused by the destruction of pulmonary alveoli resulting from smoking, air pollution, noxious gas, etc., there are provided, among others, a method of administering clarithromycin or a salt thereof to a mammal and a pharmaceutical composition comprising clarithromycin or a salt thereof.

摘要翻译： 为了治疗和/或预防由吸烟，空气污染，有害气体等引起的肺泡破坏引起的肺部疾病的目的，提供了将克拉霉素或其盐施用于 哺乳动物和包含克拉霉素或其盐的药物组合物。

公开(公告)号：US20090076253A1

公开(公告)日：2009-03-19

申请号：US12299229

申请日：2007-05-01

申请人： Masato Kashimura ,  Madoka Kawamura ,  Toshifumi Asaka ,  Kiyoshi Takayama ,  Haruhisa Ogita

发明人： Masato Kashimura ,  Madoka Kawamura ,  Toshifumi Asaka ,  Kiyoshi Takayama ,  Haruhisa Ogita

IPC分类号： C07H17/08

CPC分类号： C07H17/08 ,  A61K31/7048 ,  A61K31/7052 ,  C07H17/00

摘要： Compounds represented by formula (I) and the formula (IV) have an inhibitory activity of MMP-9 production, therefore, are useful as a medicine agent with fewer side effects than conventional MMP enzyme activity inhibitors, as a prophylactic and therapeutic drug for oncogenic angiogenesis, chronic rheumatoid arthritis, vascular intimal thickening after a percutaneous coronary transluminal angioplasty, vascular atherosclerosis, hemorrhagic apoplexy, acute myocardial infarction, chronic heart failure, aneurysm, lung cancer metastasis, adult respiratory distress syndrome, asthma, interstitial pulmonary fibrosis, chronic rhinosinusitis, bronchitis or chronic obstructive pulmonary disease (COPD).

摘要翻译： 由式（I）和式（IV）表示的化合物具有抑制MMP-9产生的活性，因此作为一种具有比常规MMP酶活性抑制剂更少副作用的药剂可用作致癌剂的预防和治疗药物 血管生成，慢性类风湿关节炎，经皮冠状动脉腔内血管成形术后血管内膜增厚，血管动脉粥样硬化，出血性中风，急性心肌梗塞，慢性心力衰竭，动脉瘤，肺癌转移，成人呼吸窘迫综合征，哮喘，间质性肺纤维化，慢性鼻鼻窦炎， 支气管炎或慢性阻塞性肺疾病（COPD）。

公开(公告)号：US20120196282A1

公开(公告)日：2012-08-02

申请号：US13015871

申请日：2011-01-28

申请人： Tomoyuki NAKAMURA ,  Kyoko Takagi ,  Kiyoshi Takayama

发明人： Tomoyuki NAKAMURA ,  Kyoko Takagi ,  Kiyoshi Takayama

IPC分类号： C12Q1/68 ,  G01N33/68 ,  C12N5/071

CPC分类号： G01N33/502 ,  C12Q1/6876 ,  C12Q2600/136 ,  C12Q2600/158 ,  G01N33/74 ,  G01N2333/495

摘要： A method of regenerating an elastic fiber according in the present invention is characterized in that the method comprises bringing an elastic fiber regenerating agent containing LTBP-4 into contact with a cell having the fiber regenerating ability. Preferably, the elastic fiber regenerating agent further contains DANCE and/or LTBP-4 expression potentiating factor. According to the present invention, the elastic fiber regenerating ability is further enhanced than so far.

摘要翻译： 根据本发明的再生弹性纤维的方法的特征在于，该方法包括使含有LTBP-4的弹性纤维再生剂与具有纤维再生能力的电池接触。 优选地，弹性纤维再生剂还含有DANCE和/或LTBP-4表达增强因子。 根据本发明，弹性纤维再生能力比迄今为止进一步提高。

公开(公告)号：US20110294857A1

公开(公告)日：2011-12-01

申请号：US13201309

申请日：2009-12-28

申请人： Masako Okamoto ,  Kiyoshi Takayama

发明人： Masako Okamoto ,  Kiyoshi Takayama

IPC分类号： A61K31/422 ,  A61P35/00 ,  A61P43/00 ,  A61P25/28 ,  A61K31/4439 ,  A61K31/433

CPC分类号： C07D413/04 ,  A61K31/422 ,  A61K31/433 ,  A61K31/4439 ,  C07D263/18 ,  C07D413/06 ,  C07D413/14 ,  C07D417/14

摘要： There is provided an inhibitor that inhibits casein kinase 1δ and casein kinase 1ε, and thus, there is also provided a pharmaceutical agent useful for the treatment and/or prevention of a disease, with the pathological condition of which the mechanism of activation of casein kinase 1δ or casein kinase 1ε is associated. Particularly, the above-described inhibitor is used to provide a pharmaceutical agent useful for the treatment of circadian rhythm disorder (including sleep disorder), central neurodegenerative disease, and cancer.An inhibitor of casein kinase 1δ and casein kinase 1ε, which comprises, as an active ingredient, an oxazolone derivative represented by the following general formula (1), a salt thereof, a solvate thereof, or a hydrate thereof: [wherein, in the formula (1), each of R1 and R2 independently represents any one of a substituted or unsubstituted 6-membered or 5-membered heterocyclic group optionally having a condensed ring, a substituted or unsubstituted aromatic hydrocarbon group optionally having a condensed ring, and a substituted or unsubstituted aromatic hydrocarbon lower alkyl group or aromatic hydrocarbon lower alkenyl group optionally having a condensed ring.]

摘要翻译： 提供了抑制酪蛋白激酶1δ和酪蛋白激酶1的抑制剂，因此，还提供了可用于治疗和/或预防疾病的药剂，其病理状况是酪蛋白的活化机制 激酶1δ或酪蛋白激酶1＆egr; 已关联的。 特别地，上述抑制剂用于提供可用于治疗昼夜节律紊乱（包括睡眠障碍），中枢神经变性疾病和癌症的药剂。 酪蛋白激酶1δ和酪蛋白激酶1抑制剂，其包含作为活性成分的由以下通式（1）表示的恶唑酮衍生物，其盐，其溶剂化物或其水合物：[其中，在 式（1）中，R 1和R 2各自独立地表示任选具有稠环的取代或未取代的6元或5元杂环基，任选具有稠环的取代或未取代的芳香族烃基， 取代或未取代的芳烃低级烷基或任选具有稠环的芳烃低级链烯基。