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1. 发明申请

US20090012102A1 Imidazo[1,2-C]Pyrimidinylacetic Acid Derivatives 有权
标题翻译：咪唑并[1,2-C]嘧啶基乙酸衍生物
公开(公告)号：US20090012102A1
公开(公告)日：2009-01-08
申请号：US10585429
申请日：2005-01-19
申请人： Tai-wei Ly , Takashi Yoshino , Yuki Takekawa , Takuya Shintani , Hiromi Sugimoto , Kevin Bacon , Klaus Urbahns
发明人： Tai-wei Ly , Takashi Yoshino , Yuki Takekawa , Takuya Shintani , Hiromi Sugimoto , Kevin Bacon , Klaus Urbahns
IPC分类号： A61K31/519 , C07D487/04 , A61P11/06 , A61P37/08 , A61P35/00
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. 发明授权

US07750014B2 Imidazo[1,2-C]pyrimidinylacetic acid derivatives 有权
标题翻译：咪唑并[1,2-C]嘧啶基乙酸衍生物
公开(公告)号：US07750014B2
公开(公告)日：2010-07-06
申请号：US10585429
申请日：2005-01-19
申请人： Tai-Wei Ly , Takashi Yoshino , Yuki Takekawa , Takuya Shintani , Hiromi Sugimoto , Kevin Bacon , Klaus Urbahns
发明人： Tai-Wei Ly , Takashi Yoshino , Yuki Takekawa , Takuya Shintani , Hiromi Sugimoto , Kevin Bacon , Klaus Urbahns
IPC分类号： A01N43/90 , A61K31/519 , 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. 发明授权

US07645607B2 Method for producing optically active N-protected-propargylglycine 有权
标题翻译：光学活性N-保护炔丙基甘氨酸的制备方法
公开(公告)号：US07645607B2
公开(公告)日：2010-01-12
申请号：US11378366
申请日：2006-03-20
申请人： Yuki Takekawa , Isao Kurimoto
发明人： Yuki Takekawa , Isao Kurimoto
IPC分类号： C12P41/00
CPC分类号： C12P41/00 , C12P13/04
摘要： A method for producing (S)—N-protected-propargylglycine of the following formula (2), wherein the method comprises asymmetrically hydrolyzing an N-protected-propargylglycine ester of the following formula (1) by using an asymmetric hydrolysis enzyme or a cultured substance of a microorganism having an ability of producing this enzyme or a treated substance thereof. The hydrolysis enzyme is obtained from a microorganism selected from the group consisting of Thermomyces genus, Aspergillus genus, Rhizopus genus, Penicillium genus, Pseudomonas genus, Humicola genus, Burkholderia genus, Candida genus Bacillus genus and Streptomyces genus.
摘要翻译：一种制备下式（2）的（S）-N-保护炔丙基甘氨酸的方法，其中所述方法包括通过使用不对称水解酶或培养的不同的水解酶不对称地水解下式（1）的N-保护炔丙基甘氨酸酯具有生产该酶的能力的微生物的物质或其处理物质。水解酶由选自Thermomyces属，曲霉属，Rhizopus属，Penicillium属，Pseudomonas属，Humicola属，Burkholderia属，假丝酵母属和Streptomyces属的微生物获得。

4. 发明申请

US20060216806A1 Method for producing optically active N-protected-propargylglycine 有权
标题翻译：光学活性N-保护炔丙基甘氨酸的制备方法
公开(公告)号：US20060216806A1
公开(公告)日：2006-09-28
申请号：US11378366
申请日：2006-03-20
申请人： Yuki Takekawa , Isao Kurimoto
发明人： Yuki Takekawa , Isao Kurimoto
IPC分类号： C12N9/00 , C12P1/04
CPC分类号： C12P41/00 , C12P13/04
摘要： A method for producing (S)-N-protected-propargylglycine of the following formula (2), wherein the method comprises asymmetrically hydrolyzing an N-protected-propargylglycine ester of the following formula (1) by using the following asymmetric hydrolysis enzyme or a cultured substance of a microorganism having an ability of producing this enzyme or a treated substance thereof. [Asymmetric Hydrolysis Enzyme]Hydrolysis enzymes derived from a microorganism selected from the group consisting of Thermomyces genus, Aspergillus genus, Rhizopus genus, Penicillium genus, Pseudomonas genus, Humicola genus, Burkholderia genus, Candida genus and Streptomyces genus.
摘要翻译：一种制备下式（2）的（S）-N-保护的炔丙基甘氨酸的方法，其中该方法包括通过使用以下不对称水解酶或下列通式（1）不对称地水解下式（1）的N-保护炔丙基甘氨酸酯：具有生产该酶的能力的微生物的培养物质或其处理物质。 [非对称水解酶]源自选自Thermomyces属，曲霉属，根霉属，青霉属，假单胞菌属，Humicola属，伯克霍尔德氏菌属，假丝酵母属和链霉菌属的微生物的水解酶。

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