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1. 发明申请

WO2004096777A1 PYRIMIDINE DERIVATIVES USEFUL FOR THE TREATMENT OF DISEASES MEDIATED BY CRTH2 审中-公开
标题翻译：用于治疗由CRTH2介导的疾病的吡咯烷衍生物
公开(公告)号：WO2004096777A1
公开(公告)日：2004-11-11
申请号：PCT/EP2004/003910
申请日：2004-04-14
申请人： BAYER HEALTHCARE AG , LY, Tai-wei , KORIYAMA, Yuji , YOSHINO, Takashi , SATO, Hiroki , TANAKA, Kazuho , SUGIMOTO, Hiromi , MANABE, Yoshihisa , BACON, Kevin , URBAHNS, Klaus , SEKI, Masanori , SHINTANI, Takuya
发明人： LY, Tai-wei , KORIYAMA, Yuji , YOSHINO, Takashi , SATO, Hiroki , TANAKA, Kazuho , SUGIMOTO, Hiromi , MANABE, Yoshihisa , BACON, Kevin , URBAHNS, Klaus , SEKI, Masanori , SHINTANI, Takuya
IPC分类号： C07D239/42
CPC分类号： C07D239/42 , C07D239/30 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12
摘要： The present invention relates to a pyrimidine derivative of the formula (I) and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The pyrimidine 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：本发明涉及式（I）的嘧啶衍生物及其盐，其可用作药物制剂的活性成分。本发明的嘧啶衍生物具有优异的CRTH2（G蛋白偶联化学引诱物受体，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。

2. 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。

3. 发明申请

WO2003022277A1 ARYLSULFONAMIDE DERIVATIVES FOR USE AS CCR3 ANTAGONISTS IN THE TREATMENT OF INFLAMMATORY AND IMMUNOLOGICAL DISORDERS 审中-公开
标题翻译：用于治疗炎症和免疫疾病的CCR3拮抗剂的磺酰苯胺衍生物
公开(公告)号：WO2003022277A1
公开(公告)日：2003-03-20
申请号：PCT/EP2002/009873
申请日：2002-09-04
申请人： BAYER AKTIENGESELLSCHAFT , LI, Yingfu , WATANABE, Akihiko , LOWINGER, Timothy, B. , BACON, Kevin , KAWAMURA, Norihiro , SHINTANI, Takuya , KIKUCHI, Tetsuo , MORIWAKI, Toshiya , URBAHNS, Klaus , FUKUSHIMA, Keiko , NUNAMI, Noriko , YOSHINO, Takashi , MURATA, Toshiki , YAMAUCHI, Megumi , YOSHINO, Hiroko
发明人： LI, Yingfu , WATANABE, Akihiko , LOWINGER, Timothy, B. , BACON, Kevin , KAWAMURA, Norihiro , SHINTANI, Takuya , KIKUCHI, Tetsuo , MORIWAKI, Toshiya , URBAHNS, Klaus , FUKUSHIMA, Keiko , NUNAMI, Noriko , YOSHINO, Takashi , MURATA, Toshiki , YAMAUCHI, Megumi , YOSHINO, Hiroko
IPC分类号： A61K31/445
CPC分类号： C07D213/70 , C07C311/29 , C07C323/67 , C07D207/14 , C07D207/48 , C07D209/08 , C07D211/28 , C07D211/58 , C07D211/96 , C07D213/65 , C07D213/71 , C07D213/75 , C07D213/76 , C07D213/80 , C07D241/04 , C07D241/06 , C07D243/08 , C07D257/04 , C07D295/088 , C07D295/13 , C07D295/194 , C07D295/26 , C07D307/14 , C07D333/38 , C07D471/04 , C07D487/04 , C07D487/08
摘要： The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders.
摘要翻译：本发明涉及可用作药物制剂活性成分的磺酰胺衍生物。本发明的磺酰胺衍生物具有CCR3（CC型趋化因子受体）拮抗活性，可用于预防和治疗与CCR3活性有关的疾病，特别是用于治疗哮喘，特应性皮炎，过敏性鼻炎等炎症 /免疫学障碍。

4. 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。

5. 发明申请

WO2004069805A1 BIS(HETERO)ARYL CARBOXAMIDE DERIVATIVES FOR USE AS PGI2 ANTAGONISTS 审中-公开
标题翻译：用作PGI2拮抗剂的BIS（HETERO）ARYL CARBOXAMIDE DERIVATIVES
公开(公告)号：WO2004069805A1
公开(公告)日：2004-08-19
申请号：PCT/EP2004/000711
申请日：2004-01-28
申请人： BAYER HEALTHCARE AG , MURATA, Toshiki , SHINTANI, Takuya , UMEDA, Masaomi , LINO, Takashi , MORIWAKI, Toshiya
发明人： MURATA, Toshiki , SHINTANI, Takuya , UMEDA, Masaomi , LINO, Takashi , MORIWAKI, Toshiya
IPC分类号： C07D231/14
CPC分类号： C07D207/325 , C07D211/14 , C07D213/64 , C07D213/82 , C07D231/12 , C07D231/14 , C07D239/34 , C07D261/18 , C07D333/38
摘要： The present invention relates to aryl or heteroaryl amido alkane derivatives of formula (I) wherein R 6 represents carboxy or tetrazolyl, which are useful as an active ingredient of pharmaceutical preparations. The aryl or heteroaryl amido alkanes of the present invention have PGI2 antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with PGI2 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 also relate to PGI2.
摘要翻译：本发明涉及式（I）的芳基或杂芳基酰氨基烷烃衍生物，其中R 6表示羧基或四唑基，其可用作药物制剂的活性成分。本发明的芳基或杂芳基酰氨基烷烃具有PGI 2拮抗活性，可用于预防和治疗与PGI2活性相关的疾病。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，逼尿肌超反射，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，膀胱过敏反应，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，盆腔疼痛综合症，前列腺痛，膀胱炎或自发性膀胱过敏反应。本发明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，因为这些疾病也与PGI2有关。

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