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1. 发明申请

WO2008124582A1 RENIN INHIBITORS 审中-公开
标题翻译：雷宁抑制剂
公开(公告)号：WO2008124582A1
公开(公告)日：2008-10-16
申请号：PCT/US2008/059399
申请日：2008-04-04
申请人： SMITHKLINE BEECHAM CORPORATION , VITAE PHARMACEUTICALS, INC. , BALDWIN, John, J. , CACATIAN, Salvacion , CLAREMON, David , DILLARD, Lawrence, W. , FLAHERTY, Patrick, T. , GHAVIMI-ALAGHA, Bahman , GHIRLANDA, Damiano , HOU, Xiaoping , ISHCHENKO, Alexey, V. , KALLANDER, Lara, S. , KNAPP-REED, Beth, A. , LAWHORN, Brian , LU, Qing , MCGEEHAN, Gerard , SEMUS, Simon , SIMPSON, Robert, D. , SINGH, Suresh, B. , TERRELL, Lamont, R. , TICE, Colin , TRAN, Tritin , XU, Zhenrong , YUAN, Jing , ZHANG, Jing , ZHAO, Wei
发明人： BALDWIN, John, J. , CACATIAN, Salvacion , CLAREMON, David , DILLARD, Lawrence, W. , FLAHERTY, Patrick, T. , GHAVIMI-ALAGHA, Bahman , GHIRLANDA, Damiano , HOU, Xiaoping , ISHCHENKO, Alexey, V. , KALLANDER, Lara, S. , KNAPP-REED, Beth, A. , LAWHORN, Brian , LU, Qing , MCGEEHAN, Gerard , SEMUS, Simon , SIMPSON, Robert, D. , SINGH, Suresh, B. , TERRELL, Lamont, R. , TICE, Colin , TRAN, Tritin , XU, Zhenrong , YUAN, Jing , ZHANG, Jing , ZHAO, Wei
IPC分类号： A01N43/50 , A61K31/415
CPC分类号： C07D401/06 , C07D211/22 , C07D265/30
摘要： Described are compounds which bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof.
摘要翻译：描述了结合天冬氨酸蛋白酶抑制其活性的化合物。它们可用于治疗或改善与天冬氨酸蛋白酶活性相关的疾病。还描述了本文所述化合物在有需要的受试者中改善或治疗天冬氨酸蛋白酶相关病症的方法。

2. 发明申请

WO2009096996A1 RENIN INHIBITORS 审中-公开
标题翻译：雷宁抑制剂
公开(公告)号：WO2009096996A1
公开(公告)日：2009-08-06
申请号：PCT/US2008/067650
申请日：2008-06-20
申请人： SMITHKLINE BEECHAM CORPORATION , VITAE PHARMACEUTICALS, INC. , BALDWIN, John J. , CACATIAN, Salvacion , CLAREMON, David , DILLARD, Lawrence, W. , FLAHERTY, Patrick, T. , GHAVIMI-ALAGHA, Bahman , ISHCHENKO, Alexey, V. , GHIRLANDA, Damiano , KALLANDER, Lara, S. , LAWHORN, Brian , LU, Qing , MCGEEHAN, Gerard , KNAPP-REED, Beth, A. , SEMUS, Simon , SIMPSON, Robert, D. , SINGH, Suresh, B. , TERRELL, Lamont, R. , TICE, Colin , TRAN, Tritin , Xu, Zhenrong , YUAN, Jing , ZHAO, Wei , ZHAO, Yongdong Y.
发明人： BALDWIN, John J. , CACATIAN, Salvacion , CLAREMON, David , DILLARD, Lawrence, W. , FLAHERTY, Patrick, T. , GHAVIMI-ALAGHA, Bahman , ISHCHENKO, Alexey, V. , GHIRLANDA, Damiano , KALLANDER, Lara, S. , LAWHORN, Brian , LU, Qing , MCGEEHAN, Gerard , KNAPP-REED, Beth, A. , SEMUS, Simon , SIMPSON, Robert, D. , SINGH, Suresh, B. , TERRELL, Lamont, R. , TICE, Colin , TRAN, Tritin , Xu, Zhenrong , YUAN, Jing , ZHAO, Wei , ZHAO, Yongdong Y.
IPC分类号： C09K11/06
CPC分类号： C07D211/22 , C07D265/30
摘要： Disclosed are compounds having the formula (I): wherein the R 1 , R 2 , R 3 , X, Y, A, L, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.
摘要翻译：公开了具有式（I）的化合物：其中R1，R2，R3，X，Y，A，L和G如本文所定义。这些化合物与天冬氨酸蛋白酶结合以抑制其活性，并且可用于治疗或改善与天冬氨酸蛋白酶活性相关的疾病。还公开了使用式I化合物在有需要的受试者中改善或治疗天冬氨酸蛋白酶相关病症的方法。

3. 发明申请

WO2007117482A2 RENIN INHIBITORS 审中-公开
标题翻译：肾素抑制剂
公开(公告)号：WO2007117482A2
公开(公告)日：2007-10-18
申请号：PCT/US2007/008339
申请日：2007-04-05
申请人： VITAE PHARMACEUTICALS, INC. , SMITHKLINE BEECHAM CORPORATION , BALDWIN, John, J. , CLAREMON, David, A. , TICE, Colin, M. , CACATIAN, Salvacion , DILLARD, Lawrence, W. , ISHCHENKO, Alexey, V. , YUAN, Jing , XU, Zhenrong , MCGEEHAN, Gerard , ZHAO, Wei , SIMPSON, Robert, D. , SINGH, Suresh, B. , FLAHERTY, Patrick, T. , KALLANDER, Lara, S. , LEACH, Colin, A. , LAWHORN, Brian , LU, Qing , TERRELL, Lamont, R. , GHAVINI-ALAGHA, Bahman , ZHANG, Jing , GHIRLANDA, Damiano , HOU, Xiaoping , SEMUS, Simon
发明人： BALDWIN, John, J. , CLAREMON, David, A. , TICE, Colin, M. , CACATIAN, Salvacion , DILLARD, Lawrence, W. , ISHCHENKO, Alexey, V. , YUAN, Jing , XU, Zhenrong , MCGEEHAN, Gerard , ZHAO, Wei , SIMPSON, Robert, D. , SINGH, Suresh, B. , FLAHERTY, Patrick, T. , KALLANDER, Lara, S. , LEACH, Colin, A. , LAWHORN, Brian , LU, Qing , TERRELL, Lamont, R. , GHAVINI-ALAGHA, Bahman , ZHANG, Jing , GHIRLANDA, Damiano , HOU, Xiaoping , SEMUS, Simon
IPC分类号： C07D211/22 , C07D265/30 , C07D401/06 , A61K31/44 , A61K31/5375 , A61P9/12
CPC分类号： C07D211/22 , C07D265/30 , C07D401/06
摘要： Disclosed are compounds according to Formula (I): wherein the variables are defined herein. Such compounds are can bind aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described herein are methods of antagonizing aspartic protease inhibitors in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a compound according to Formula (I).
摘要翻译：公开了根据式（I）的化合物：其中变量如本文所定义。这些化合物可以结合天冬氨酸蛋白酶以抑制它们的活性。它们可用于治疗或改善与天冬氨酸蛋白酶活性相关的疾病。本文还描述了在有需要的受试者中拮抗天冬氨酸蛋白酶抑制剂的方法，其包括向受试者施用治疗有效量的根据式（I）的化合物。

4. 发明申请

WO2008124575A8 RENIN INHIBITORS 审中-公开
公开(公告)号：WO2008124575A8
公开(公告)日：2008-10-16
申请号：PCT/US2008/059384
申请日：2008-04-04
申请人： VITAE PHARMACEUTICALS, INC. , BALDWIN, John, J. , CACATIAN, Salvacion , CLAREMON, David , DILLARD, Lawrence, W. , FLAHERTY, Patrick, T. , GHAVIMI-ALAGHA, Bahman , GHIRLANDA, Damiano , ISHCHENKO, Alexey, V. , KALLANDER, Lara, S. , LAWHORN, Brian , LEACH, Colin, A. , LU, Qing , MCGEEHAN, Gerald , PATTERSON, Jaclyn, R. , SIMPSON, Robert, D. , SINGH, Suresh, B. , STOY, Patrick , TERRELL, Lamont, R. , TICE, Colin , XU, Zhenrong , YUAN, Jing , YUAN, Catherine, C., K. , ZHANG, Jing , ZHAO, Wei
发明人： BALDWIN, John, J. , CACATIAN, Salvacion , CLAREMON, David , DILLARD, Lawrence, W. , FLAHERTY, Patrick, T. , GHAVIMI-ALAGHA, Bahman , GHIRLANDA, Damiano , ISHCHENKO, Alexey, V. , KALLANDER, Lara, S. , LAWHORN, Brian , LEACH, Colin, A. , LU, Qing , MCGEEHAN, Gerald , PATTERSON, Jaclyn, R. , SIMPSON, Robert, D. , SINGH, Suresh, B. , STOY, Patrick , TERRELL, Lamont, R. , TICE, Colin , XU, Zhenrong , YUAN, Jing , YUAN, Catherine, C., K. , ZHANG, Jing , ZHAO, Wei
IPC分类号： A01N35/00 , A61K31/10 , A61K31/12
摘要： Disclosed are compounds of Formula (I) wherein the R, R 1 , R 2 , R 3 , X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.

5. 发明申请

WO2005121122A1 IMIDAZOL-2-ONE COMPOUNDS USEFUL IN THE TREATMENT OF VARIOUS DISORDERS 审中-公开
标题翻译： IMIDAZOL-2-ONE化合物可用于治疗各种各样的疾病
公开(公告)号：WO2005121122A1
公开(公告)日：2005-12-22
申请号：PCT/EP2005/006183
申请日：2005-06-07
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , GHIRLANDA, Damiano
发明人： ALVARO, Giuseppe , GHIRLANDA, Damiano
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： A compound of formula (I) wherein: R represents a group selected from: i) ii) iii) or iv) in which R 6 is halogen, cyano, C 1-4 alkyl or trifluoromethyl and p is 2 or 3 or R 6 is halogen, cyano, C 1-4 alkyl, C 1-4 alkoxy, trifluoromethoxy or trifluoromethyl and p is 0 or 1; R 1 represents hydrogen, halogen, cyano, C 2-4 alkenyl, C 1-4 alkyl optionally substituted by halogen, cyano or C 1-4 alkoxy; R 2 represents hydrogen or (CH 2 )qR 7 ; R 3 and R 4 each independently are hydrogen or C 1-4 alkyl; R5 represents : phenyl substituted by 1 to 3 groups independently selected from trifluoromethyl, C 1-4 alkyl, cyano, C 1-4 alkoxy, trifluoromethoxy, halogen, S(O)rC1-4 alkyl or a phenyl substituted by a 5 or 6 membered heteroaryl group optionally substituted by 1 to 3 groups independently selected from trifluoromethyl, C 1-4 alkyl, cyano, C 1-4 alkoxy, trifluoromethoxy, halogen or S(O)rC 1-4 alkyl; naphthyl substituted by 1 to 3 groups independently selected from trifluoromethyl, C 1-4 alkyl, cyano, C 1-4 alkoxy, trifluoromethoxy, halogen or S(O)rC 1-4 alkyl; a 9 to 10 membered fused bicyclic heterocyclic group substituted by 1 to 3 groups independently selected from trifluoromethyl, C 1-4 alkyl, cyano, C 1-4 alkoxy, trifluoromethoxy, halogen or S(O)rC 1-4 alkyl or R 5 is a 5 or 6 membered heteroaryl group substituted by 1 to 3 groups independently selected from trifluoromethyl, C 1-4 alkyl, cyano, C 1-4 alkoxy, trifluoromethoxy, halogen or S(O)rC 1-4 alkyl; R 7 is hydrogen, C 3-7 cycloalkyl, C 1-4 alkoxy, amine, C 1-4 alkylamine, (C 1-4 alkyl) 2 amine, OC(O)NR 8 R 9 or C(O)NR 8 R 9 ; R 8 and R 9 each independently represent hydrogen, C 1-4 alkyl or C 3-7 cycloalkyl; A-B is a bivalent radical of formula (v) -CH=C(R 11 )- (vi) -C (R 10 )=CH- or (vii) -C(R 12 )(R 10 )-C(R 11 )(R 13 )- wherein R 10 , R 11 , R 12 and R 13 each independently are hydrogen or C 1-4 alkyl; n is 1 or 2; q is an integer from 1 to 4; r is 1 or 2; or pharmaceutically acceptable salts and solvates thereof, process for their preparation and their use in the treatment of conditions mediated by tachykinins and/or by selective inhibition of serotonin reuptake transporter protein.
摘要翻译：式（I）化合物，其中：R表示选自以下的基团：i）ii）iii）或iv）其中R 6为卤素，氰基，C 1-4烷基或三氟甲基，p为2或3或R6为卤素，氰基，C 1-4烷基，C 1-4烷氧基，三氟甲氧基或三氟甲基，p为0或1; R 1表示氢，卤素，氰基，C 2-4烯基，任选被卤素，氰基或C 1-4烷氧基取代的C 1-4烷基; R2代表氢或（CH2）qR7; R 3和R 4各自独立地为氢或C 1-4烷基; R5代表：被1至3个独立地选自三氟甲基，C 1-4烷基，氰基，C 1-4烷氧基，三氟甲氧基，卤素，S（O）r C 1-4烷基或被5或6元杂芳基取代的苯基取代的苯基。任选被1至3个独立地选自三氟甲基，C 1-4烷基，氰基，C 1-4烷氧基，三氟甲氧基，卤素或S（O）r C 1-4烷基的基团取代的基团; 被1-3个独立地选自三氟甲基，C 1-4烷基，氰基，C 1-4烷氧基，三氟甲氧基，卤素或S（O）r C 1-4烷基取代的萘基; 被1至3个独立地选自三氟甲基，C 1-4烷基，氰基，C 1-4烷氧基，三氟甲氧基，卤素或S（O）r C 1-4烷基或R 5的基团取代的9至10元稠合双环杂环基是5或被1-3个独立地选自三氟甲基，C 1-4烷基，氰基，C 1-4烷氧基，三氟甲氧基，卤素或S（O）r C 1-4烷基取代的6元杂芳基; R 7是氢，C 3-7环烷基，C 1-4烷氧基，胺，C 1-4烷基胺，（C 1-4烷基）2胺，OC（O）NR 8 R 9或C（O）NR 8 R 9; R8和R9各自独立地表示氢，C1-4烷基或C3-7环烷基; AB是式（v）-CH = C（R 11） - （vi）-C（R 10）= CH-或（i）-C（R 12）（R 10）-C（R 11）（R 13）其中R 10，R 11，R 12和R 13各自独立地为氢或C 1-4烷基; n为1或2; q是1至4的整数; r为1或2; 或其药学上可接受的盐和溶剂化物，其制备方法及其用于治疗由速激肽介导的病症和/或通过选择性抑制5-羟色胺再摄取转运蛋白。

6. 发明申请

WO2018198035A1 SINGLE-PIECE FLOATING TRAY FOR HYDROPONIC CULTIVATION 审中-公开
公开(公告)号：WO2018198035A1
公开(公告)日：2018-11-01
申请号：PCT/IB2018/052857
申请日：2018-04-24
申请人： GHIRLANDA, Damiano , GHIRLANDA, Martino
发明人： GHIRLANDA, Damiano , GHIRLANDA, Martino
IPC分类号： A01G9/02 , A01G31/02
摘要： The present invention relates to a single-piece tray for hydroponic cultivation, composed of a plastic material shaped so as to define inside the tray a plurality of identical cultivation cells. Each cultivation cell has: a housing defining a raised plane and configured to house a bulb or seedling to be cultivated, with a hole having dimensions such as to support the bulb or seedling to be cultivated without letting it fall through, while allowing its roots to protrude below the tray; a buoyant portion, defining a lowered plane intended to sink below a waterline, and delimited by side walls, each buoyant portion defining: - a bottomside with a first height, intended to remain below the waterline, - a waterline zone with a second height, which remains above the waterline when the bulb or seedling to be cultivated is placed in the cultivation cell and is intended to sink completely below the waterline when the bulb or seedling to be cultivated has become a mature plant, - a topside with a third height, which remains above the waterline when the bulb or seedling to be cultivated has become a mature plant; the sum of the first, second and third heights corresponding to the height of the side walls which connect the raised plane to the lowered plane and wherein said side walls form a channel which communicates directly with the space outside that subtended by said tray.

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