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1. 发明申请

WO2004035092A3 USE OF AN AGENT MODULATING COFILIN EXPRESION OR ACTIVITY FOR THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
标题翻译：使用调节CFF表达或活性的药物治疗炎性疾病
公开(公告)号：WO2004035092A3
公开(公告)日：2004-06-10
申请号：PCT/GB0304450
申请日：2003-10-15
申请人： OXFORD GLYCOSCIENCES UK LTD , BAYER HEALTHCARE AG , BACON KEVIN B , HERATH HERATH MUDIYANSELAGE AT , LIU NINGSHU , ROHLFF CHRISTIAN
发明人： BACON KEVIN B , HERATH HERATH MUDIYANSELAGE AT , LIU NINGSHU , ROHLFF CHRISTIAN
IPC分类号： A61P11/00 , A61P11/06 , C07K14/47 , G01N33/68 , C07K149/47 , A61K31/00 , C07C14/38
CPC分类号： C07K14/4702 , G01N33/6893 , G01N2500/00 , G01N2800/122 , G01N2800/52
摘要： Methods for the treatment of inflammatory diseases including respiratory diseases, such as asthma and asthma related conditions, comprising regulation of the polypeptide cofilin, agents which modulate the expression or activity of the polypeptide, methods for the identification of such agents and the use of cofilin in the diagnosis of inflammatory diseases including respiratory diseases such as asthma and asthma related conditions.
摘要翻译：治疗炎性疾病的方法包括呼吸疾病，如哮喘和哮喘相关病症，包括调节多肽cofilin，调节多肽表达或活性的药物，鉴定这些药物的方法以及cofilin在炎性疾病的诊断包括呼吸系统疾病如哮喘和哮喘相关病症。

2. 发明申请

WO2003105884A1 USE OF SHP-1 FOR THE THERAPY OF ASTHMA 审中-公开
标题翻译：使用SHP-1治疗哮喘
公开(公告)号：WO2003105884A1
公开(公告)日：2003-12-24
申请号：PCT/GB2003/002611
申请日：2003-06-18
申请人： OXFORD GLYCOSCIENCES (UK) LTD , BAYER AG , HERATH, Herath, Mudiyanselage, Athula, Chandrasiri , BACON, Kevin, B. , LIU, Ningshu , REINEMER, Peter , ROHLFF, Christian
发明人： BACON, Kevin, B. , LIU, Ningshu , REINEMER, Peter , ROHLFF, Christian
IPC分类号： A61K38/17
CPC分类号： A61K38/465 , C07K16/40 , C12Y301/03048 , G01N33/6893 , G01N2500/00 , G01N2800/122 , G01N2800/52
摘要： The present invention relates to methods for the treatment of asthma and asthma related conditions comprising regulation of the polypeptide SHP-1, agents which modulate the expression or activity of the polypeptide, methods for the identification of such agents and the use of SHP-1 in the diagnosis of asthma and asthma related conditions.
摘要翻译：本发明涉及治疗哮喘和哮喘相关病症的方法，包括调节多肽SHP-1，调节多肽的表达或活性的药剂，用于鉴定这些药物的方法和使用SHP-1 哮喘和哮喘相关病症的诊断。

3. 发明申请

WO2005073234A3 IMIDAZO[1,2-C]PYRIMIDINYLACETIC ACID DERIVATIVES 审中-公开
标题翻译：咪唑并[1,2-C]嘧啶基乙酸衍生物
公开(公告)号：WO2005073234A3
公开(公告)日：2005-10-06
申请号：PCT/EP2005000475
申请日：2005-01-19
申请人： BAYER HEALTHCARE AG , LY TAI-WEI , YOSHINO TAKASHI , TAKEKAWA YUKI , SHINTANI TAKUYA , SUGIMOTO HIROMI , BACON KEVIN B , URBAHNS KLAUS
发明人： LY TAI-WEI , YOSHINO TAKASHI , TAKEKAWA YUKI , SHINTANI TAKUYA , SUGIMOTO HIROMI , BACON KEVIN B , URBAHNS KLAUS
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to an imidazo[1,2-c]pyrimidinylacetic acid derivative and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The imidazo[1,2-c]pyrimidinylacetic acid derivative of the present invention has excellent CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity and can be used for the prophylaxis and treatment of diseases associated with CRTH2 activity, in particular for the treatment of allergic diseases, such as asthma, allergic rhinitis, atopic dermatitis, and allergic conjunctivitis; eosinophil-related diseases, such as Churg-Strauss syndrome and sinusitis; basophil-related diseases, such as basophilic leukemia, chronic urticaria and basophilic leukocytosis in human and other mammals; and inflammatory diseases characterized by T lymphocytes and profuse leukocyte infiltrates such as psoriasis, eczema, inflammatory bowel disease, ulcerative colitis, Crohn's disease, COPD (chronic obstructive pulmonary disorder) and arthritis.
摘要翻译：本发明涉及可用作药物制剂活性成分的咪唑并[1,2-c]嘧啶基乙酸衍生物及其盐。本发明的咪唑并[1,2-c]嘧啶基乙酸衍生物具有优良的CRTH2（在Th2细胞上表达的G蛋白偶联化学引诱物受体）拮抗活性，可用于预防和治疗与CRTH2活性有关的疾病特别是用于治疗过敏性疾病，如哮喘，过敏性鼻炎，特应性皮炎和过敏性结膜炎; 嗜酸性粒细胞相关疾病，如Churg-Strauss综合征和鼻窦炎; 嗜碱性粒细胞相关疾病，如嗜碱性白血病，人类和其他哺乳动物中的慢性荨麻疹和嗜碱性白细胞增多症; 和以T淋巴细胞和大量白细胞浸润为特征的炎性疾病，例如牛皮癣，湿疹，炎性肠病，溃疡性结肠炎，克罗恩病，COPD（慢性阻塞性肺病）和关节炎。

4. 发明申请

WO2004035092A2 REGULATION OF COFILIN 审中-公开
标题翻译：用于治疗炎症性疾病的代理调控COFILIN表达或活性的用途
公开(公告)号：WO2004035092A2
公开(公告)日：2004-04-29
申请号：PCT/GB2003/004450
申请日：2003-10-15
申请人： OXFORD GLYCOSCIENCES (UK) LTD , BAYER HEALTHCARE AG , BACON, Kevin, B. , HERATH, Herath, Mudiyanselage, Athula, Chandrasiri , LIU, Ningshu , ROHLFF, Christian
发明人： BACON, Kevin, B. , HERATH, Herath, Mudiyanselage, Athula, Chandrasiri , LIU, Ningshu , ROHLFF, Christian
IPC分类号： A61K49/00
CPC分类号： C07K14/4702 , G01N33/6893 , G01N2500/00 , G01N2800/122 , G01N2800/52
摘要： Methods for the treatment of inflammatory diseases including respiratory diseases, such as asthma and asthma related conditions, comprising regulation of the polypeptide cofilin, agents which modulate the expression or activity of the polypeptide, methods for the identification of such agents and the use of cofilin in the diagnosis of inflammatory diseases including respiratory diseases such as asthma and asthma related conditions.
摘要翻译：用于治疗包括呼吸系统疾病如哮喘和哮喘相关病症在内的炎性疾病的方法，包括调节多肽胞蛋白，调节多肽的表达或活性的试剂，用于鉴定这些药物的方法和使用cofilin 诊断炎性疾病包括呼吸系统疾病如哮喘和哮喘相关的病症。

5. 发明申请

WO2005019182A1 PYRAZOLYLMETHYLBENZAMIDE DERIVATIVES AS P2XT-RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为P2XT-受体拮抗剂的吡唑并苯并噻吩衍生物
公开(公告)号：WO2005019182A1
公开(公告)日：2005-03-03
申请号：PCT/EP2004/009172
申请日：2004-08-16
申请人： BAYER HEALTHCARE AG , CONCEPCION, Arnel , INOUE, Tadashi , MOCHIZUKI, Yuki , MURAMATSU, Aiko , GANTNER, Florian , NAKASHIMA, Kosuke , URBAHNS, Klaus , BACON, Kevin, B.
发明人： CONCEPCION, Arnel , INOUE, Tadashi , MOCHIZUKI, Yuki , MURAMATSU, Aiko , GANTNER, Florian , NAKASHIMA, Kosuke , URBAHNS, Klaus , BACON, Kevin, B.
IPC分类号： C07D231/12
CPC分类号： C07D231/12 , C07D403/06 , C07D405/12
摘要： The present invention relates to novel pyrazolylmethylbenzamide derivatives of formula (I), processes for preparing them and pharmaceutical preparations containing them. The pyrazolylmethylbenzamide derivatives of the present invention exhibit enhanced potency for P2X7 receptor antagonism and can be used for the prophylaxis and treatment of diseases associated with P2X7 receptor activity. More specifically, the pyrazolylmethylbenzamide derivatives of the. present invention are useful for treatment and prophylaxis of diseases as follows: rheumatoid arthritis, osteoarthritis, psoriasis, allergic dermatitis, asthma, chronic obstructive pulmonary disease (COPD), hyperresponsiveness of the airway, septic shock, glomerulonephritis, irritable bowel disease, Crohn's disease, ulcerative: colitis, atherosclerosis, growth and metastases of malignant cells, myoblastic leukaemia, diabetes, Alzheimer's disease, meningitis, osteoporosis, burn injury, ischaemic heart disease, stroke and varicose veins.
摘要翻译：本发明涉及式（I）的新型吡唑基甲基苯甲酰胺衍生物，其制备方法和含有它们的药物制剂。本发明的吡唑基甲基苯甲酰胺衍生物对P2X7受体拮抗作用表现出增强的效力，可用于预防和治疗与P2X7受体活性相关的疾病。更具体地，吡唑基甲基苯甲酰胺衍生物。本发明可用于治疗和预防疾病如下：类风湿性关节炎，骨关节炎，牛皮癣，过敏性皮炎，哮喘，慢性阻塞性肺病（COPD），气道高反应性，败血性休克，肾小球性肾炎，肠易激综合征，克罗恩病，溃疡性结肠炎，动脉粥样硬化，恶性细胞的生长和转移，成肌细胞性白血病，糖尿病，阿尔茨海默氏病，脑膜炎，骨质疏松症，烧伤，缺血性心脏病，中风和静脉曲张。

6. 发明申请

WO2005073234A2 IMIDAZO[1,2-C]PYRIMIDINYLACETIC ACID DERIVATIVES 审中-公开
标题翻译：咪唑并[1,2-C]吡啶-2-基酸衍生物
公开(公告)号：WO2005073234A2
公开(公告)日：2005-08-11
申请号：PCT/EP2005/000475
申请日：2005-01-19
申请人： BAYER HEALTHCARE AG , LY, Tai-wei , YOSHINO, Takashi , TAKEKAWA, Yuki , SHINTANI, Takuya , SUGIMOTO, Hiromi , BACON, Kevin B. , URBAHNS, Klaus
发明人： LY, Tai-wei , YOSHINO, Takashi , TAKEKAWA, Yuki , SHINTANI, Takuya , SUGIMOTO, Hiromi , BACON, Kevin B. , URBAHNS, Klaus
IPC分类号： C07D487/00
CPC分类号： C07D487/04
摘要： The present invention relates to an imidazo[1,2-c]pyrimidinylacetic acid derivative and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The imidazo[1,2-c]pyrimidinylacetic acid derivative of the present invention has excellent CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity and can be used for the prophylaxis and treatment of diseases associated with CRTH2 activity, in particular for the treatment of allergic diseases, such as asthma, allergic rhinitis, atopic dermatitis, and allergic conjunctivitis; eosinophil-related diseases, such as Churg-Strauss syndrome and sinusitis; basophil-related diseases, such as basophilic leukemia, chronic urticaria and basophilic leukocytosis in human and other mammals; and inflammatory diseases characterized by T lymphocytes and profuse leukocyte infiltrates such as psoriasis, eczema, inflammatory bowel disease, ulcerative colitis, Crohn's disease, COPD (chronic obstructive pulmonary disorder) and arthritis.
摘要翻译：本发明涉及可用作药物制剂活性成分的咪唑并[1,2-c]嘧啶基乙酸衍生物及其盐。本发明的咪唑并[1,2-c]嘧啶基乙酸衍生物具有优异的CRTH2（G蛋白偶联的化学引诱物受体，在Th2细胞上表达）拮抗活性，可用于预防和治疗与CRTH2活性相关的疾病特别是用于治疗过敏性疾病如哮喘，过敏性鼻炎，特应性皮炎和过敏性结膜炎; 嗜酸性粒细胞相关疾病，如中华综合征和鼻窦炎; 嗜碱性粒细胞相关疾病，如嗜碱性白血病，慢性荨麻疹和人类和其他哺乳动物的嗜碱性白细胞增多症; 以T淋巴细胞为特征的炎性疾病和白血球浸润如银屑病，湿疹，炎性肠病，溃疡性结肠炎，克罗恩病，COPD（慢性阻塞性肺病）和关节炎等。

7. 发明申请

WO2004058764A1 4-PHENYL-PYRIMIDO [4,5-B] INDOLE DERIVATIVES 审中-公开
标题翻译： 4-苯基 - 吡啶并[4,5-B]吲哚衍生物
公开(公告)号：WO2004058764A1
公开(公告)日：2004-07-15
申请号：PCT/EP2003/014194
申请日：2003-12-13
申请人： BAYER HEALTHCARE AG , SATO, Hiroki , INOUE, Tadashi , LY, Tai-Wei , MURAMATSU, Aiko , SHIMAZAKI, Makoto , URBAHNS, Klaus , GANTNER, Florian , OKIGAMI, Hiromi , BACON, Kevin, B. , KOMURA, Hiroshi , YOSHIDA, Nagahiro , TSUNO, Naoki
发明人： SATO, Hiroki , INOUE, Tadashi , LY, Tai-Wei , MURAMATSU, Aiko , SHIMAZAKI, Makoto , URBAHNS, Klaus , GANTNER, Florian , OKIGAMI, Hiromi , BACON, Kevin, B. , KOMURA, Hiroshi , YOSHIDA, Nagahiro , TSUNO, Naoki
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to 4-phenyl-pyrimido[4,5-b]indoles which are useful as an active ingredient of pharmaceutical preparations. The 4-phenyl-pyrimido[4,5-b]indoles of the present invention have MKK7 and MKK4 inhibitory activity, and can be used for the prophylaxis and treatment of diseases associated with MKK7 and MKK4 activity.Such diseases include, inflammatory and immunoregulatory disorders and diseases such as asthma, atopic dermatitis, rhinitis, allergic rhinitis, allergic diseases, COPD, septic shock, arthritis, joint diseases and myocardial injuries, as well as autoimmune pathologies such as rheumatoid arthritis, Grave's disease, and atherosclerosis as well as cancer.The compounds of the present invention are also useful for treatment of ischemia, myocardial injury, pulmonary hypertension, renal failure, Huntington's chorea and cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and focal ischemia.
摘要翻译：本发明涉及可用作药物制剂活性成分的4-苯基 - 嘧啶并[4,5-b]吲哚。本发明的4-苯基 - 嘧啶并[4,5-b]吲哚具有MKK7和MKK4抑制活性，可用于预防和治疗与MKK7和MKK4活性相关的疾病。这些疾病包括炎症和免疫调节疾病和疾病如哮喘，特应性皮炎，鼻炎，过敏性鼻炎，过敏性疾病，COPD，败血性休克，关节炎，关节疾病和心肌损伤，以及自身免疫病态如类风湿性关节炎，格雷夫氏病和动脉粥样硬化以及癌症本发明的化合物还可用于治疗缺血，心肌损伤，肺动脉高压，肾衰竭，亨廷顿舞蹈病和心脏肥大，以及神经变性疾病如帕金森病，阿尔茨海默病和局灶性缺血。

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