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1. 发明授权

EP2328876B1 ISOTOPICALLY ENRICHED PYRIMIDIN-5-YL ACETIC ACID DERIVATIVES AS CRTH2 ANTAGONISTS 有权
标题翻译：富集了同位素嘧啶-5-YLESSIGSÄUREDERIVATE作为CRTH2拮抗剂
公开(公告)号：EP2328876B1
公开(公告)日：2012-11-21
申请号：EP09789242.6
申请日：2009-09-01
申请人： Actimis Pharmaceuticals, Inc.,
发明人： LY, Tai, Wei
IPC分类号： C07D239/48 , C07D487/04 , A61K31/505 , A61K31/519 , A61P11/06
CPC分类号： C07D239/48

2. 发明公开

EP1849469A1 ARYLSULFONAMIDE DERIVATIVES FOR USE AS CCR3 ANTAGONISTS IN THE TREATMENT OF INFLAMMATORY AND IMMUNOLOGICAL DISORDERS 有权
标题翻译：在炎症和免疫疾病的治疗中用作拮抗剂CCR3芳基磺酰胺衍生物
公开(公告)号：EP1849469A1
公开(公告)日：2007-10-31
申请号：EP07013793.0
申请日：2002-09-04
申请人： Actimis Pharmaceuticals, Inc.,
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 , A61K31/496 , A61P11/06 , A61P37/00 , A61P29/00 , C07D295/22 , C07D471/04 , C07D211/58 , C07D243/06 , C07D211/28 , C07C311/18 , C07D211/96 , C07D307/14 , C07D207/14 , C07D213/71
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：本发明涉及磺酰胺衍生物的所有其作为药物制剂的活性成分是有用的。本发明的磺胺衍生物具有CCR3（CC型趋化因子受体）拮抗活性，并且可以被用于疾病与CCR3活性用于治疗哮喘，特应性皮炎，过敏性鼻炎和其它炎性相关联，尤其是预防和治疗 /免疫性疾病。

3. 发明公开

EP1688496A3 Regulation of human P2Y1-like G protein-coupled receptor 审中-公开
标题翻译：红细胞生成素P2Y1-ähnlichenG-protein gekoppelten Rezeptors
公开(公告)号：EP1688496A3
公开(公告)日：2006-08-16
申请号：EP06000083.3
申请日：2001-08-10
申请人： Actimis Pharmaceuticals, Inc.,
发明人： Ramakrishnan, Shyam
IPC分类号： C12N15/12 , C12N15/63 , C12N1/19 , C12N15/11 , C12N15/62 , C07K14/705 , C07K16/28 , C12Q1/68 , G01N33/68 , A61K31/7088 , A61K38/17 , A61K39/395 , A61K48/00
CPC分类号： G01N33/74 , C07K14/705 , C07K14/723 , G01N2333/726 , G01N2500/00
摘要： Use of a screening method, said method for the identification of compounds useful in the treatment of chronic obstructive pulmonary or airway disease ("COPD")comprising the step of contacting a test compound with a polypeptide.
摘要翻译：使用筛选方法，所述用于鉴定可用于治疗慢性阻塞性肺或气道疾病（“COPD”）的化合物的方法包括使测试化合物与多肽接触的步骤。

4. 发明授权

EP2205570B1 2-S-BENZYL SUBSTITUTED PYRIMIDINES AS CRTH2 ANTAGONISTS 有权
标题翻译： 2-S-苄基取代的嘧啶作为CRTH2拮抗剂的
公开(公告)号：EP2205570B1
公开(公告)日：2013-09-11
申请号：EP08834170.6
申请日：2008-09-24
申请人： Actimis Pharmaceuticals, Inc.,
发明人： LY, Tai, Wei , POTTER, Garrett, T. , TRAN, Marie, Chantal S. -Y
IPC分类号： C07D239/47 , A61K31/505 , A61P11/06
CPC分类号： C07D239/47

5. 发明授权

EP2205569B1 ALKYLTHIO PYRIMIDINES AS CRTH2 ANTAGONISTS 有权
标题翻译： ALKYLTHIOPYRIMIDINE作为CRTH2拮抗剂
公开(公告)号：EP2205569B1
公开(公告)日：2012-02-29
申请号：EP08833849.6
申请日：2008-09-24
申请人： Actimis Pharmaceuticals, Inc.,
发明人： LY, Tai, Wei , RAAUM, Erik, D. , TRAN, Marie, Chantal S.-Y
IPC分类号： C07D239/38 , C07D239/47 , C07D239/58 , A61K31/505 , A61P29/00
CPC分类号： C07D239/38 , C07D239/47 , C07D239/58 , C07D403/12
摘要： Provided herein are alkylthio substituted pyrimidine compounds having CRTH2 (G- protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity, useful for the treatment or prophylaxis of diseases associated with CRTH2 activity, including the treatment of allergic diseases, eosinophil-related diseases and basophil-related diseases.

6. 发明公开

EP1644493A1 REGULATION OF A KINASE, 'REGULATED IN COPD KINASE' (RC KINASE) 有权
标题翻译：调节型激素，“慢性阻塞性激素释放激素”（RC-KINASE）
公开(公告)号：EP1644493A1
公开(公告)日：2006-04-12
申请号：EP04739941.5
申请日：2004-06-16
申请人： Actimis Pharmaceuticals, Inc.,
发明人： WATANABE, Shinichi , ENCINAS, Jeffrey, 464-1-1401 Toroyama-cho , KONDO, Shinichi , BACON, Kevin
IPC分类号： C12N9/02 , A61K38/43
CPC分类号： C12N9/0004
摘要： Reagents which regulate human RC Kinase activity and reagents which bind to human RC Kinase gene products can be used to regulate this protein for therapeutic effects. Such regulation is particularly useful for treating chronic obstructive pulmonary disease, asthma, cancer, and diseases in which cell signaling is defective.

7. 发明公开

EP2328876A1 ISOTOPICALLY ENRICHED PYRIMIDIN-5-YL ACETIC ACID DERIVATIVES AS CRTH2 ANTAGONISTS 有权
标题翻译：富集了同位素嘧啶-5-YLESSIGSÄUREDERIVATE作为CRTH2拮抗剂
公开(公告)号：EP2328876A1
公开(公告)日：2011-06-08
申请号：EP09789242.6
申请日：2009-09-01
申请人： Actimis Pharmaceuticals, Inc.,
发明人： LY, Tai, Wei
IPC分类号： C07D239/48 , C07D487/04 , A61K31/505 , A61K31/519 , A61P11/06
CPC分类号： C07D239/48
摘要： Provided herein are
2 H- and
13 C-enriched compounds of formula (I) or (II); wherein R is as defined herein, and wherein at least one hydrogen atom, in certain embodiments, three or more hydrogen atoms, are deuterium atoms or at least one carbon atom is a carbon- 13 atom. Also provided are pharmaceutical compositions and methods using the
2 H- and
13 C-enriched compounds, useful for treating CRTH2-related diseases or disorders such as, for example, asthma, allergic rhinitis, atopic dermatitis, allergic conjuvatitis, Churg-Strauss syndrome, sinusitis, basophilic leukemia, chronic urticaria or basophilic leukocytosis.

8. 发明授权

EP1633726B1 PYRIMIDINE DERIVATIVES USEFUL FOR THE TREATMENT OF DISEASES MEDIATED BY CRTH2 有权
标题翻译： ZUR BEHANDLUNG VON DURCH CRTH2 VERMITTELTEN KRANKHEITEN GEEIGNETE PYRIMIDINDERIVATE
公开(公告)号：EP1633726B1
公开(公告)日：2011-01-05
申请号：EP04727274.5
申请日：2004-04-14
申请人： Actimis Pharmaceuticals, Inc.,
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 , C07D403/12 , C07D405/12 , C07D401/12 , C07D407/12 , C07D403/04 , C07D403/14 , C07D239/34 , C07D239/48 , A61K31/506 , A61P11/06
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：嘧啶基乙酸衍生物（I）是新的。式（I）的嘧啶基乙酸衍生物，其互变异构体或立体异构形式和盐是新的。 [图像] R 1：-C（O） - （CH 2）n -Y'，-C（O）-CH = CH-Y'，-SO 2 - （CH 2）n -Y' - （CH 2）n -Y'，-CH 2 -CH = CH-Y'或-C（O）-NH-（CH 2）n -Y'; n：0-6; Y'：H，3-8C环烷基（任选被1-6C烷基取代或任选被苯稠合）或（杂）芳基（任选被CN，卤素，硝基，胍基，吡咯基，氨磺酰基，1-6C烷基氨基磺酰基，二（1-6C烷基）氨基磺酰基，苯氧基，苯基，氨基，1-6C烷基氨基，二1-6C烷基氨基，1-6C烷氧基羰基，1-6C烷酰基，1-6C烷酰基氨基，氨基甲酰基，1-6C烷基氨基甲酰基，二 - （1-6C烷基）氨基甲酰基，1-6C烷基磺酰基，1-6C烷基（任选被卤素单取代至三取代），1-6C烷氧基（任选被卤素单取代至三取代），1-6C烷硫基（任选被卤素单取代至三取代）或芳基（由1,3-二氧戊环稠合））; R 2：H或1-6C烷基; R 3：q：1-3; R 3 c：H，OH，羧基或1-6C烷基（任选被OH，羧基或（苯基取代的C 1-6烷基）氨基甲酰基取代）; X a：-O-，-S-或-N（R 3 d） - ; R 3 d：1-6C烷基或-N（R 3 a）（R 3b）; R 3 a，R 3 b：3-8C环烷基或1-6C烷基（任选被羧基取代，3-8C环烷基，氨基甲酰基，1-6C烷基氨基甲酰基，芳基取代的1-6C烷基氨基甲酰基，1-6C烷基氨基甲酰基，二（1-6C烷基）氨基甲酰基，3-8C环烷基氨基甲酰基，3-8C杂环羰基，1-6C烷基氨基，二1-6C烷基氨基或1-6C烷氧基）; 和R 4：H，卤素，C 1-6烷氧基，二（1-6C烷基）氨基或1-6C烷基（任选被卤素单取代至三取代）。活动：抗哮喘; 抗过敏; 抗炎; 皮肤; 眼科; 抑制细胞生长。作用机制：在Th2细胞（CRTH2）拮抗剂上表达的G蛋白偶联的化学引诱物受体。测试[2-（4-苯甲酰氨基 - 苄基）-4-氯-6-（环戊基氨基甲酰甲基 - 甲基 - 氨基） - 嘧啶-5-基] - 乙酸（A）的人CRTH2受体的结合活性。将细胞悬浮液（2×10 5细胞）（100μl），[3 H] - 标记的PGD 2和（A）与96孔U底聚丙烯板混合，并在室温下孵育60分钟以允许捆绑。孵育后，将细胞悬浮液转移到过滤板中，用结合缓冲液洗涤3次。确定非特异性结合。（A）的IC 5 0为= 0.5nM。

9. 发明授权

EP1461038B9 ARYLSULFONAMIDE DERIVATIVES FOR USE AS CCR3 ANTAGONISTS IN THE TREATMENT OF INFLAMMATORY AND IMMUNOLOGICAL DISORDERS 有权
标题翻译： ACRYLSULFONAMIDDERIVATE用作CCR3拮抗剂炎症和免疫疾病的治疗
公开(公告)号：EP1461038B9
公开(公告)日：2009-09-23
申请号：EP02772265.1
申请日：2002-09-04
申请人： Actimis Pharmaceuticals, Inc.,
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 , A61K31/496 , A61P11/06 , A61P37/00 , A61P29/00 , C07D295/22 , C07D471/04 , C07D211/58 , C07D243/06 , C07D211/28 , C07C311/18 , C07D211/96 , C07D307/14 , C07D207/14 , C07D213/71
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.

10. 发明授权

EP1718649B1 IMIDAZO 1,2-C PYRIMIDINYLACETIC ACID DERIVATIVES 有权
标题翻译：咪唑1,2-C吡啶甲基乙酸衍生物
公开(公告)号：EP1718649B1
公开(公告)日：2009-06-10
申请号：EP05706922.1
申请日：2005-01-19
申请人： Actimis Pharmaceuticals, Inc.,
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。

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