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![DISUBSTITUTED [4-(5-AMINOMETHYL-PHENYL)-PIPERIDIN-1-YL]- 1H-INDOL-3-YL]-METHANONES](/abs-image/US/2012/06/07/US20120142735A1/abs.jpg.150x150.jpg)
1.发明申请DISUBSTITUTED [4-(5-AMINOMETHYL-PHENYL)-PIPERIDIN-1-YL]- 1H-INDOL-3-YL]-METHANONES 审中-公开分离的[4-（5-氨基苯基） - 哌啶-1-基] -1H-吲哚-3-基] - 乙二醇公开(公告)号：US20120142735A1
公开(公告)日：2012-06-07
申请号：US13396111
申请日：2012-02-14
申请人： Yong- Mi CHOI-SLEDESKI , Charles J. GARDNER , Guyan LIANG , Gregory B. POLI , Patrick Wai-Kwok SHUM , Grzegory T. STOKLOSA , Zhicheng ZHAO
发明人： Yong- Mi CHOI-SLEDESKI , Charles J. GARDNER , Guyan LIANG , Gregory B. POLI , Patrick Wai-Kwok SHUM , Grzegory T. STOKLOSA , Zhicheng ZHAO
IPC分类号： A61K31/454 , A61P25/00 , A61P29/00 , A61P27/02 , A61P1/00 , A61P11/06 , A61P37/08 , A61P11/00 , A61P1/16 , A61P17/02 , A61P17/00 , A61P9/10 , A61P3/10 , A61P35/00 , A61P1/04 , A61P31/12 , A61P19/02 , A61P17/06 , C07D401/06
CPC分类号： C07D401/06 , A61K31/454 , A61K45/06 , A61K2300/00
摘要： The present invention extends to a compound of formula I: or a pharmaceutically acceptable salt of said compound, or a pharmaceutical composition comprising the compound of formula I and a pharmaceutically acceptable carrier. The invention is also directed to the use of a compound of formula I as an inhibitor of tryptase and for treating a patient suffering from, or subject to, a physiological condition in need of amelioration by an inhibitor of tryptase. The invention further includes methods for the preparation of a compound of formula I.
摘要翻译： 本发明延伸到式I化合物：或所述化合物的药学上可接受的盐，或包含式I化合物和药学上可接受的载体的药物组合物。 本发明还涉及式I化合物作为类胰蛋白酶抑制剂的用途，并且用于治疗患有需要由类胰蛋白酶抑制剂改善的生理条件或受其影响的患者。 本发明还包括制备式I化合物的方法。
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2.发明申请2,6-SUBSTITUTED-4-MONOSUBSTITUTED AMINO-PYRIMIDINE AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS 审中-公开作为前列腺素D2受体拮抗剂的2,6-取代的4-单核苷酸氨基嘧啶公开(公告)号：US20090036469A1
公开(公告)日：2009-02-05
申请号：US12246918
申请日：2008-10-07
申请人： David STEFANY , Keith John HARRIS , Timothy Alan GILLESPY , Charles J. GARDNER , Joacy C. AGUIAR
发明人： David STEFANY , Keith John HARRIS , Timothy Alan GILLESPY , Charles J. GARDNER , Joacy C. AGUIAR
IPC分类号： C07D239/47 , A61K31/506 , A61K31/505 , C07D401/04 , C07D409/04 , A61K31/495 , A61P37/08 , A61P17/00 , A61P11/00
CPC分类号： C07D403/04 , C07D239/47 , C07D409/04
摘要： The present invention is directed to a compound of formula (I), wherein R1 and R2 are as defined herein, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds of the invention in admixture with a pharmaceutically acceptable carrier, and a method of treating a patient suffering from a PGD2-mediated disorder by administering to said patient a pharmaceutically effective amount of a compound of the invention.
摘要翻译： 本发明涉及式（I）化合物，其中R 1和R 2如本文所定义，药物组合物包含药学上有效量的一种或多种本发明化合物与药学上可接受的载体的混合物，以及方法 通过向所述患者施用药学有效量的本发明化合物来治疗患有PGD2介导的病症的患者。
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3.发明授权2,6-substituted-4-monosubstitutedamino-pyrimidine as prostaglandin D2 receptor antagonists 有权2,6-取代-4-单取代氨基嘧啶作为前列腺素D2受体拮抗剂公开(公告)号：US08193183B2
公开(公告)日：2012-06-05
申请号：US11735751
申请日：2007-04-16
申请人： Sungtaek Lim , Keith John Harris , David Stefany , Charles J. Gardner , Bin Cao , Ray Boffey , Timothy A. Gillespy , Joacy C. Aguiar , Hazel J. Dyke , Elsa A. Dechaux
发明人： Sungtaek Lim , Keith John Harris , David Stefany , Charles J. Gardner , Bin Cao , Ray Boffey , Timothy A. Gillespy , Joacy C. Aguiar , Hazel J. Dyke , Elsa A. Dechaux
IPC分类号： C07D239/47 , C07D413/12 , A61K31/505 , A61K31/5355 , A61P37/00 , A61P37/08 , A61P17/00
CPC分类号： C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14
摘要： The present invention is directed to a compound of Formula (I) wherein Cy1, Cy2, L1, L2, and R1 are as defined herein, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds according to Formula (I) in admixture with a pharmaceutically acceptable carrier, and a method of treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like by administering to said patient a pharmaceutically effective amount of a compound according to Formula (I).
摘要翻译： 本发明涉及式（I）的化合物，其中Cy1，Cy2，L1，L2和R1如本文所定义，药物组合物包含药学上有效量的一种或多种式（I）化合物的混合物 与药学上可接受的载体和治疗患有PGD2介导的病症的患者的方法，包括但不限于过敏性疾病（例如过敏性鼻炎，过敏性结膜炎，特应性皮炎，支气管哮喘和食物过敏），系统性肥大细胞增多症 ，伴有系统性肥大细胞活化，过敏性休克，支气管收缩，支气管炎，荨麻疹，湿疹，伴有瘙痒的疾病（例如特应性皮炎和荨麻疹），疾病（例如白内障，视网膜脱离，炎症，感染和睡眠障碍） 由于伴随瘙痒的行为（如刮伤和跳动），炎症，慢性阻塞性肺疾病 脑缺血再灌注损伤，脑血管意外，慢性类风湿性关节炎，胸膜炎，溃疡性结肠炎等，通过向所述患者施用药学有效量的根据式（I）的化合物。
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公开(公告)号：US5051405A
公开(公告)日：1991-09-24
申请号：US419305
申请日：1989-10-10
CPC分类号： C07K5/1024 , A61K38/00
摘要： Disclosed are novel peptides and pseudopeptides and pharmaceutical compositions thereof containing certain amino acids and pharmaceutical compositions thereof that inhibit platelet aggregation and thrombus formation in mammalian blood.
摘要翻译： 公开了含有抑制哺乳动物血液中的血小板聚集和血栓形成的某些氨基酸及其药物组合物的新型肽和假肽及其药物组合物。
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公开(公告)号：US07943616B2
公开(公告)日：2011-05-17
申请号：US10995103
申请日：2004-11-23
申请人： Paul J. Cox , Tahir N. Majid , Justine Yeun Quai Lai , Andrew D. Morley , Shelley Amendola , Stephanie D. Deprets , Christopher Edlin , Charles J. Gardner , Dorothea Kominos , Brian L. Pedgrift , Frank Halley , Timothy A. Gillespy , Michael Edwards , Francois F. Clerc , Conception Nemecek , Olivier Houille , Dominique Damour , Herve Bouchard , Daniel N. A. Bezard , Chantal Carrez
发明人： Paul J. Cox , Tahir N. Majid , Justine Yeun Quai Lai , Andrew D. Morley , Shelley Amendola , Stephanie D. Deprets , Christopher Edlin , Charles J. Gardner , Dorothea Kominos , Brian L. Pedgrift , Frank Halley , Timothy A. Gillespy , Michael Edwards , Francois F. Clerc , Conception Nemecek , Olivier Houille , Dominique Damour , Herve Bouchard , Daniel N. A. Bezard , Chantal Carrez
IPC分类号： C07D487/04 , A61K31/5025 , A61P29/00 , A61P35/00 , A61P19/02
CPC分类号： C07D519/00 , C07D471/04 , C07D487/04
摘要： The invention is directed to physiologically active compounds of general formula (I):— and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.
摘要翻译： 本发明涉及通式（I）的生理活性化合物： - 含有这些化合物的组合物; 及其前药，以及这些化合物及其前药的药学上可接受的盐和溶剂合物，以及式（I）范围内的新化合物。 这些化合物和组合物具有有价值的药物特性，特别是抑制激酶的能力。
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公开(公告)号：US06897208B2
公开(公告)日：2005-05-24
申请号：US10279834
申请日：2002-10-24
申请人： Michael L. Edwards , Paul J. Cox , Shelley Amendola , Stephanie D. Deprets , Timothy A. Gillespy , Christopher D. Edlin , Andrew D. Morley , Charles J. Gardner , Brian Pedgrift , Herve Bouchard , Didier Babin , Laurence Gauzy , Alain Le-Brun , Tahir N. Majid , John C. Reader , Lloyd J. Payne , Nawaz M. Khan , Michael Cherry
发明人： Michael L. Edwards , Paul J. Cox , Shelley Amendola , Stephanie D. Deprets , Timothy A. Gillespy , Christopher D. Edlin , Andrew D. Morley , Charles J. Gardner , Brian Pedgrift , Herve Bouchard , Didier Babin , Laurence Gauzy , Alain Le-Brun , Tahir N. Majid , John C. Reader , Lloyd J. Payne , Nawaz M. Khan , Michael Cherry
IPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D521/00 , A61K31/33 , A61K31/415 , C07D231/00 , C07D235/00 , C07D487/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04 , C07D491/04
摘要： The invention is directed to physiologically active compounds of the general formula (Ix) and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.
摘要翻译： 本发明涉及通式（Ix）的生理活性化合物和含有这些化合物及其前药以及这些化合物及其前药的药学上可接受的盐和溶剂合物的组合物，以及式（Ix）范围内的新化合物 Ix），以及它们的制备过程。 这些化合物和组合物具有有价值的药物特性，特别是抑制激酶的能力。
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公开(公告)号：US4952562A
公开(公告)日：1990-08-28
申请号：US415006
申请日：1989-09-29
CPC分类号： C07K5/1019 , C07K5/021 , C07K5/06026 , C07K5/06113 , C07K5/0817 , A61K38/00
摘要： Disclosed are novel peptides and pseudopeptides and pharmaceutical compositions thereof that inhibit platelet aggregation and thrombus formation in mammalian blood.
摘要翻译： 公开了抑制哺乳动物血液中的血小板聚集和血栓形成的新型肽和假肽及其药物组合物。
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公开(公告)号：US06897207B2
公开(公告)日：2005-05-24
申请号：US10177804
申请日：2002-06-21
申请人： Paul J. Cox , Tahir N. Majid , Justine Yeun Quai Lai , Andrew D. Morley , Shelley Amendola , Stephanie D. Deprets , Christopher Edlin , Charles J. Gardner , Dorothea Kominos , Brian L. Pedgrift , Frank Halley , Timothy A. Gillespy , Michael Edwards , Francois F. Clerc , Conception Nemecek , Olivier Houille , Dominique Damour , Herve Bouchard , Daniel N. A. Bezard , Chantal Carrez
发明人： Paul J. Cox , Tahir N. Majid , Justine Yeun Quai Lai , Andrew D. Morley , Shelley Amendola , Stephanie D. Deprets , Christopher Edlin , Charles J. Gardner , Dorothea Kominos , Brian L. Pedgrift , Frank Halley , Timothy A. Gillespy , Michael Edwards , Francois F. Clerc , Conception Nemecek , Olivier Houille , Dominique Damour , Herve Bouchard , Daniel N. A. Bezard , Chantal Carrez
IPC分类号： A61K20060101 , A61K31/437 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/4985 , A61K31/5355 , A61K31/5377 , A61K31/541 , A61P20060101 , A61P9/00 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/08 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P27/14 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07D20060101 , C07D209/00 , C07D221/00 , C07D241/00 , C07D471/04 , C07D487/04 , C07D519/00 , A61K31/33 , A61K31/66 , C07D417/02
CPC分类号： C07D519/00 , C07D471/04 , C07D487/04
摘要： The invention is directed to physiologically active compounds of general formula (I): and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.
摘要翻译： 本发明涉及通式（I）的生理活性化合物：和含有这些化合物的组合物; 及其前药，以及这些化合物及其前药的药学上可接受的盐和溶剂合物，以及式（I）范围内的新化合物。 这些化合物和组合物具有有价值的药物特性，特别是抑制激酶的能力。
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公开(公告)号：US08288425B2
公开(公告)日：2012-10-16
申请号：US11029064
申请日：2005-01-04
申请人： Michael L. Edwards , Paul J. Cox , Shelley Amendola , Stephanie D. Deprets , Timothy A. Gillespy , Christopher D. Edlin , Andrew D. Morley , Charles J. Gardner , Brian Pedgrift , Herve Bouchard , Didier Babin , Laurence Gauzy , Alain Le-Brun , Tahir N. Majid , John C. Reader , Lloyd J. Payne , Nawaz M. Khan , Michael Cherry
发明人： Michael L. Edwards , Paul J. Cox , Shelley Amendola , Stephanie D. Deprets , Timothy A. Gillespy , Christopher D. Edlin , Andrew D. Morley , Charles J. Gardner , Brian Pedgrift , Herve Bouchard , Didier Babin , Laurence Gauzy , Alain Le-Brun , Tahir N. Majid , John C. Reader , Lloyd J. Payne , Nawaz M. Khan , Michael Cherry
IPC分类号： A61K31/4184 , C07D235/18
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04 , C07D491/04
摘要： The invention is directed to physiologically active compounds of the general formula (Ix) and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.
摘要翻译： 本发明涉及通式（Ix）的生理活性化合物和含有这些化合物及其前药以及这些化合物及其前药的药学上可接受的盐和溶剂合物的组合物，以及式（Ix）范围内的新化合物 Ix），以及它们的制备过程。 这些化合物和组合物具有有价值的药物特性，特别是抑制激酶的能力。
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公开(公告)号：US5780590A
公开(公告)日：1998-07-14
申请号：US700950
申请日：1996-08-21
CPC分类号： C07K5/06113 , C07K5/0806 , A61K38/00 , Y02P20/55
摘要： The invention is directed to a non-hygroscopic stable crystalline form of the antithrombotic compound N-�N-�N-(4-piperdin-4-yl)butanoyl)-N-ethylglycyl!-(L)-aspartyl!-(L)-.beta.-cyclohexyl-alanine amide, to processes for preparing said stable crystalline form, to a pharmaceutical composition thereof, and intermediates thereof, and the invention is directed also to processes for preparing a compound of the formula ##STR1## wherein: A, B, Z, E.sup.1, E.sup.2, G, R, m, n, and p are as defined herein.
摘要翻译： 本发明涉及抗血栓形成的化合物N- [N- [N-（4-哌啶-4-基）丁酰基）-N-乙基甘氨酰] - （L） - 天门冬酰基] - （L ） - β-环己基 - 丙氨酸酰胺，制备所述稳定结晶形式的方法，其制备方法及其中间体，本发明还涉及制备下式化合物的方法：其中：A， B，Z，E1，E2，G，R，m，n和p如本文所定义。
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