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1. 发明申请

WO2003037898A1 PYRIMIDO [4,5-B] INDOLE DERIVATIVES 审中-公开
标题翻译：吡咯烷[4,5-B]吲哚衍生物
公开(公告)号：WO2003037898A1
公开(公告)日：2003-05-08
申请号：PCT/EP2002/012057
申请日：2002-10-29
申请人： BAYER AKTIENGESELLSCHAFT , LOWINGER, Timothy , SHIMAZAKI, Makoto , SATO, Hiroki , TANAKA, Kazuho , TSUNO, Naoki , MARX, Karsten , YAMAMOTO, Masaru , URBAHNS, Klaus , GANTNER, Florian , OKIGAMI, Hiromi , NAKASHIMA, Kosuke , TAKESHITA, Keisuke , BACON, Kevin , KOMURA, Hiroshi , YOSHIDA, Nagahiro
发明人： LOWINGER, Timothy , SHIMAZAKI, Makoto , SATO, Hiroki , TANAKA, Kazuho , TSUNO, Naoki , MARX, Karsten , YAMAMOTO, Masaru , URBAHNS, Klaus , GANTNER, Florian , OKIGAMI, Hiromi , NAKASHIMA, Kosuke , TAKESHITA, Keisuke , BACON, Kevin , KOMURA, Hiroshi , YOSHIDA, Nagahiro
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to pyrimido[4,5-b]indoles which are useful as an active ingredient of pharmaceutical preparations. The 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. 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嘧啶并[4,5-b]吲哚。本发明的嘧啶并[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。这些疾病包括炎性和免疫调节性疾病以及诸如哮喘，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等疾病，以及自身免疫性病变如类风湿性关节炎，格雷夫氏病，和动脉粥样硬化。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，亨廷顿氏舞蹈病和心脏肥大，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。

2. 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。

3. 发明申请

WO2005054239A1 2-AMINOPYRIMIDINE DERIVATIVES 审中-公开
标题翻译： 2-氨基嘧啶衍生物
公开(公告)号：WO2005054239A1
公开(公告)日：2005-06-16
申请号：PCT/EP2004/013322
申请日：2004-11-24
申请人： BAYER HEALTHCARE AG , SATO, Hiroki , TANAKA, Kazuho , SHIMAZAKI, Makoto , URBAHNS, Klaus , SAKAI, Katsuya , GANTNER, Florian , BACON, Kevin
发明人： SATO, Hiroki , TANAKA, Kazuho , SHIMAZAKI, Makoto , URBAHNS, Klaus , SAKAI, Katsuya , GANTNER, Florian , BACON, Kevin
IPC分类号： C07D471/04
CPC分类号： C07D403/04 , C07D409/14 , C07D471/04 , C07D487/04
摘要： The present invention relates to novel 2-aminopyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The 2-aminopyrimidine derivatives of the present invention exhibit enhanced potency for histamine H4 receptor antagonism and can be used for the prophylaxis and treatment of diseases associated with histamine H4 receptor activity. More specifically, the 2-aminopyrimidine derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: asthma, rhinitis, allergic diseases, chronic obstructed pulmonary disease (COPD), atherosclerosis, rheumatoid arthritis, thromboembolic diseases or disorders and urological diseases or disorders.
摘要翻译：本发明涉及新的2-氨基嘧啶衍生物，其制备方法和含有它们的药物制剂。本发明的2-氨基嘧啶衍生物对组胺H 4受体拮抗作用表现出增强的效力，可用于预防和治疗与组胺H 4受体活性相关的疾病。更具体地，本发明的2-氨基嘧啶衍生物可用于治疗和预防以下疾病：哮喘，鼻炎，过敏性疾病，慢性阻塞性肺病（COPD），动脉粥样硬化，类风湿性关节炎，血栓栓塞性疾病或病症和泌尿系统疾病或障碍。

4. 发明申请

WO2005014556A1 2-AMINOPYRIMIDINE DERIVATIVES 审中-公开
标题翻译： 2-氨基嘧啶衍生物
公开(公告)号：WO2005014556A1
公开(公告)日：2005-02-17
申请号：PCT/EP2004/008225
申请日：2004-07-23
申请人： BAYER HEALTHCARE AG , SATO, Hiroki , FUKUSHIMA, Keiko , SHIMAZAKI, Makoto , URBAHNS, Klaus , SAKAI, Katsuya , GANTER, Florian , BACON, Kevin
发明人： SATO, Hiroki , FUKUSHIMA, Keiko , SHIMAZAKI, Makoto , URBAHNS, Klaus , SAKAI, Katsuya , GANTER, Florian , BACON, Kevin
IPC分类号： C07D239/04
CPC分类号： C07D239/48 , C07D403/04
摘要： The present invention relates to novel 2-aminopyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The 2-aminopyrimidine derivatives of the present invention exhibit enhanced potency for histamine H4 receptor antagonism and can be used for the prophylaxis and treatment of diseases associated with histamine H4 receptor activity. More specifically, the 2-aminopyrimidine derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: asthma, rhinitis, allergic diseases, chronic obstructed pulmonary disease (CORD), atherosclerosis and rheumatoid arthritis.
摘要翻译：本发明涉及新的2-氨基嘧啶衍生物，其制备方法和含有它们的药物制剂。本发明的2-氨基嘧啶衍生物对组胺H 4受体拮抗作用表现出增强的效力，可用于预防和治疗与组胺H 4受体活性相关的疾病。更具体地，本发明的2-氨基嘧啶衍生物可用于治疗和预防以下疾病：哮喘，鼻炎，过敏性疾病，慢性阻塞性肺疾病（CORD），动脉粥样硬化和类风湿性关节炎。

5. 发明申请

WO2003106402A1 2-NAPHTAMIDE DERIVATIVES 审中-公开
公开(公告)号：WO2003106402A1
公开(公告)日：2003-12-24
申请号：PCT/EP2003/005705
申请日：2003-05-30
申请人： BAYER AKTIENGESELLSCHAFT , SHIMAZAKI, Makoto , SAKURAI, Osamu , MURATA, Toshiki , URBAHNS, Klaus , YAMAMOTO, Noriyuki , YOSHIKAWA, Satoru , UMEDA, Masaomi , TAJIMI, Masaomi , MASUDA, Tsutomu , SHINTANI, Takuya , SHIMIZU, Haruka
发明人： SHIMAZAKI, Makoto , SAKURAI, Osamu , MURATA, Toshiki , URBAHNS, Klaus , YAMAMOTO, Noriyuki , YOSHIKAWA, Satoru , UMEDA, Masaomi , TAJIMI, Masaomi , MASUDA, Tsutomu , SHINTANI, Takuya , SHIMIZU, Haruka
IPC分类号： C07C235/34
CPC分类号： C07C235/66
摘要： The present invention relates to 2-naphthamides, which are useful as an active ingredient of pharmaceutical preparations. The 2-naphthamides of the present invention have IP receptor antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with IP receptor activity. Such diseases include urological diseases or disorder as follows: bladder outlet obstruction, overactive bladder, urinary incontinence, detrusor hyper-reflexia, detrusor instability, reduced bladder capacity, frequency of micturition, urge incontinence, stress incontinence, bladder hyperreactivity, benign prostatic hypertrophy (BPH), prostatitis, urinary frequency, nocturia, urinary urgency, pelvic hypersensitivity, urethritis, pelvic pain syndrome, prostatodynia, cystitis, or idiophatic bladder hypersensitivity. The compounds of the present invention are also useful for treatment of pain including, but not limited to inflammatory pain, neuropathic pain, acute pain, chronic pain, dental pain, premenstrual pain, visceral pain, headaches, and the like; hypotension; hemophilia and hemorrhage; and inflammation, since the disease is also alleviated by treatment with an IP receptor antagonist.
摘要翻译：本发明涉及可用作药物制剂活性成分的2-萘甲酰胺。本发明的2-萘甲酰胺具有IP受体拮抗活性，可用于预防和治疗与IP受体活性相关的疾病。这些疾病包括尿路疾病或病症如下：膀胱出口阻塞，膀胱过度活动，尿失禁，逼尿肌反射反射，逼尿肌不稳定，膀胱容量减少，排尿频率，急迫性尿失禁，压力性尿失禁，膀胱高反应性，良性前列腺肥大），前列腺炎，尿频，夜尿症，尿急，盆腔超敏反应，尿道炎，盆腔疼痛综合征，前列腺痛，膀胱炎或自发性膀胱过敏。本发明的化合物还可用于治疗疼痛，包括但不限于炎性疼痛，神经性疼痛，急性疼痛，慢性疼痛，牙痛，经前痛，内脏痛，头痛等; 低血压; 血友病和出血; 和炎症，因为该疾病也通过用IP受体拮抗剂治疗而缓解。

6. 发明申请

WO2003106403A1 CARBOXAMIDES DERIVATIVES 审中-公开
标题翻译：碳氧化物衍生物
公开(公告)号：WO2003106403A1
公开(公告)日：2003-12-24
申请号：PCT/EP2003/006168
申请日：2003-06-12
申请人： BAYER HEALTHCARE AG , SHIMAZAKI, Makoto , SAKURAI, Osamu , HIRAI, Kanako , URBAHNS, Klaus , YAMAMOTO, Noriyuki , YOSHIKAWA, Satoru , UMEDA, Masaomi , TAJIMI, Masaomi
发明人： SHIMAZAKI, Makoto , SAKURAI, Osamu , HIRAI, Kanako , URBAHNS, Klaus , YAMAMOTO, Noriyuki , YOSHIKAWA, Satoru , UMEDA, Masaomi , TAJIMI, Masaomi
IPC分类号： C07C235/34
CPC分类号： C07C235/34
摘要： The present invention relates to carboxamides which are useful as an active ingredient of pharmaceutical preparations. The carboxamides of the present invention have IP receptor antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with IP receptor antagonistic activity.Such diseases include urological diseases or disorder as follows: bladder outlet obstruction, overactive bladder, urinary incontinence, detrusor hyper-reflexia, detrusor instability, reduced bladder capacity, frequency of micturition, urge incontinence, stress incontinence, bladder hyperreactivity, benighn prostatic hypertrophy (BPH), prostatitis, urinary frequency, nocturia, urinary urgency, pelvic hypersensitivity, urethritis, pelvic pain syndrome, prostatodynia, cystitis, or idiophatic bladder hypersensitivity.The compounds of the present invention are also useful for treatment of pain including, but not limited to inflammatory pain, neuropathic pain, acute pain, chronic pain, dental pain, premenstrual pain, visceral pain, headaches, and the like; hypotension;hemophilia and hemorrhage; and inflammation, since the diseases are alleviated by treatment with an IP receptor antagonist.
摘要翻译：本发明涉及可用作药物制剂活性成分的羧酰胺。本发明的甲酰胺具有IP受体拮抗活性，可用于预防和治疗与IP受体拮抗作用相关的疾病。这些疾病包括泌尿系统疾病或病症如下：膀胱出口阻塞，膀胱过度活动症，尿失禁，逼尿肌反射反射，逼尿肌不稳定，膀胱容量减少，排尿频率，急迫性尿失禁，压力性尿失禁，膀胱反应过度，前列腺肥大（BPH），前列腺炎，尿频，夜尿症，尿急，盆腔超敏反应，尿道炎，盆腔疼痛综合征，前列腺痛，膀胱炎或自发性膀胱过敏症。本发明的化合物还可用于治疗疼痛，包括但不限于炎症性疼痛，神经性疼痛，急性疼痛，慢性疼痛，牙痛，经前痛，内脏痛，头痛等; 低血压;血友病和出血; 和炎症，因为通过用IP受体拮抗剂治疗来减轻疾病。

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