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71. 发明申请

WO2007089335A2 MULTICYCLIC AMINO ACID DERIVATIVES AND METHODS OF THEIR USE 审中-公开
标题翻译：多环氨基酸衍生物及其使用方法
公开(公告)号：WO2007089335A2
公开(公告)日：2007-08-09
申请号：PCT/US2006/047579
申请日：2006-12-12
申请人： LEXICON GENETICS INCORPORATED , DEVASAGAYARAJ, Arokiasamy , JIN, Haihong , LIU, Qingyun , MARINELLI, Brent , SAMALA, Lakshama , SHI, Zhi-Cai , TUNOORI, Ashok , WANG, Ying , WU, Wenxue , ZHANG, Chengmin , ZHANG, Haiming
发明人： DEVASAGAYARAJ, Arokiasamy , JIN, Haihong , LIU, Qingyun , MARINELLI, Brent , SAMALA, Lakshama , SHI, Zhi-Cai , TUNOORI, Ashok , WANG, Ying , WU, Wenxue , ZHANG, Chengmin , ZHANG, Haiming
CPC分类号： C07D251/18 , C07B2200/07 , C07C229/36 , C07C229/42 , C07C229/44 , C07C275/42 , C07C311/29 , C07C2601/08 , C07D213/74 , C07D239/34 , C07D239/42 , C07D239/47 , C07D239/48 , C07D241/20 , C07D241/24 , C07D249/06 , C07D251/16 , C07D251/22 , C07D251/52 , C07D401/04 , C07D403/04 , C07D403/12 , C07D409/04 , C07D409/12 , C07D413/12
摘要： Compounds of formulae I and II are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and manage serotonin-mediated diseases and disorders.
摘要翻译：公开了式I和II化合物，以及包含它们的组合物及其用于治疗，预防和控制血清素介导的疾病和病症的方法。

72. 发明申请

WO2005120515A2 NOVEL SULFONAMIDES AS INHIBITORS OF HISTONE DEACETYLASE FOR THE TREATMENT OF DISEASE 审中-公开
标题翻译：作为治疗疾病的组胺脱乙酰酶的抑制剂的新型磺酰胺
公开(公告)号：WO2005120515A2
公开(公告)日：2005-12-22
申请号：PCT/US2005/020770
申请日：2005-06-09
申请人： KALYPSYS, INC. , MALECHA, James , NOBLE, Stewart , HASSIG, Christian , WASH, Paul , WILEY, Brandon , LAWRENCE, Charles , HOFFMAN, Timothy
发明人： MALECHA, James , NOBLE, Stewart , HASSIG, Christian , WASH, Paul , WILEY, Brandon , LAWRENCE, Charles , HOFFMAN, Timothy
IPC分类号： A61K31/55
CPC分类号： C07D213/70 , C07C327/30 , C07C329/06 , C07D209/08 , C07D213/76 , C07D231/18 , C07D239/40 , C07D239/42 , C07D251/22 , C07D261/10 , C07D263/50 , C07D271/07 , C07D307/64 , C07D333/34 , C07D333/36 , C07D409/12 , C07D413/12 , C07D417/12 , C07F9/1653
摘要： Disclosed herein are carbonyl compounds of having the structural formula (I) or a pharmaceutically acceptable salt, amide, ester, or prodrug thereof, Methods and compositions are disclosed for treating disease states including, but not limited to cancers, autoimmune diseases, tissue damage, central nervous system disorders, neurodegenerative disorders, fibrosis, bone disorders, polyglutamine-repeat disorders, anemias, thalassemias, inflammatory conditions, cardiovascular conditions, and disorders in which angiogenesis play a role in pathogenesis, using the compounds of the invention. In addition, methods of modulating the activity of histone deacetylase (HDAC) are also disclosed.
摘要翻译：本文公开了具有结构式（I）的羰基化合物或其药学上可接受的盐，酰胺，酯或前药。公开了用于治疗疾病状态的方法和组合物，包括但不限于癌症，自身免疫疾病，组织损伤，使用本发明的化合物，中枢神经系统疾病，神经退行性疾病，纤维化，骨病，聚谷氨酰胺重复病症，贫血，地贫，炎性病症，心血管疾病和血管发生在发病机理中发挥作用的病症。此外，还公开了调节组蛋白脱乙酰酶（HDAC）的活性的方法。

73. 发明申请

WO2004050613A2 2-SUBSTITUTED-3-PROPENAMIDE DERIVATIVES AND METHODS OF USING THE SAME 审中-公开
标题翻译： 2-取代-3-丙烯酰胺衍生物及其使用方法
公开(公告)号：WO2004050613A2
公开(公告)日：2004-06-17
申请号：PCT/US2003/038233
申请日：2003-12-02
申请人： TRIANGLE PHARMACEUTICALS, INC. , SZNAIDMAN, Marcos , PAINTER, George, R. , ALMOND, Merrick, R. , CLEARY, Darryl, G. , PESYAN, Amir
发明人： SZNAIDMAN, Marcos , PAINTER, George, R. , ALMOND, Merrick, R. , CLEARY, Darryl, G. , PESYAN, Amir
IPC分类号： C07D
CPC分类号： C07D207/325 , C07C235/38 , C07C237/22 , C07D203/18 , C07D205/04 , C07D207/20 , C07D207/24 , C07D207/33 , C07D211/18 , C07D211/58 , C07D211/62 , C07D211/70 , C07D213/26 , C07D213/40 , C07D213/75 , C07D213/82 , C07D231/40 , C07D233/06 , C07D233/64 , C07D239/06 , C07D239/26 , C07D239/42 , C07D239/48 , C07D239/52 , C07D241/20 , C07D251/22 , C07D253/07 , C07D261/14 , C07D263/12 , C07D277/04 , C07D277/22 , C07D277/46 , C07D277/58 , C07D285/135 , C07D295/185 , C07D295/205 , C07D307/10 , C07D307/14 , C07D307/20 , C07D307/38 , C07D307/52 , C07D307/56 , C07D307/79 , C07D309/04 , C07D309/20 , C07D317/46 , C07D317/52 , C07D317/62 , C07D317/64 , C07D319/18 , C07D333/12 , C07D333/20 , C07D333/36 , C07D333/44 , C07D401/12 , C07D405/12 , C07D417/12 , C07D491/10
摘要： This invention provides 2-substituted-propenamide derivatives and their compositions for the treament of hepatitis B virus and/or hepatitis D virus.
摘要翻译：本发明提供2-取代的丙烯酰胺衍生物及其用于治疗乙型肝炎病毒和/或丙型肝炎病毒的组合物。

74. 发明申请

WO2004000820A2 CERTAIN AROMATIC MONOCYCLES AS KINASE MODULATORS 审中-公开
标题翻译：某些芳香单体作为激酶调节剂
公开(公告)号：WO2004000820A2
公开(公告)日：2003-12-31
申请号：PCT/US2003/019961
申请日：2003-06-23
申请人： CELLULAR GENOMICS, INC.
发明人： DARROW, James, W. , DESIMONE, Robert, W. , PIPPIN, Douglas, A. , MITCHELL, Scott, A.
IPC分类号： C07D251/18
CPC分类号： C07D239/26 , C07D241/12 , C07D251/18 , C07D251/22 , C07D251/70
摘要： Compound having Formula (I): wherein (W) is a monocyclic ring having the structure are useful as modulators of kinase activity.
摘要翻译：具有式（I）的化合物：其中（W）是具有该结构的单环，可用作激酶活性的调节剂。

75. 发明申请

WO2003037346A1 6-PHENYL-N-PHENYL-(1,3,5) -TRIAZINE-2,4-DIAMINE DERIVATIVES AND RELATED COMPOUNDS WITH LYSOPHPHOSPHATIDIC ACID ACYLTRANSFERASE BETA (LPAAT-BETA) INHIBITORY ACTIVITY FOR USE IN THE TREATMENT OF CANCER 审中-公开
标题翻译： 6-苯基-N-苯基 - （1,3,5） - 哒嗪-2,4-二胺衍生物及相关化合物，其具有用于治疗癌症的磷脂酰胆碱酯酶（LPAAT-BETA）抑制活性
公开(公告)号：WO2003037346A1
公开(公告)日：2003-05-08
申请号：PCT/US2002/035256
申请日：2002-10-30
申请人： CELL THERAPEUTICS, INC. , BHATT, Rama , GONG, Baoqing , HONG, Feng , JENKINS, Scott, A. , KLEIN, J., Peter , KUMAR, Anil, M. , TULINSKY, John
发明人： BHATT, Rama , GONG, Baoqing , HONG, Feng , JENKINS, Scott, A. , KLEIN, J., Peter , KUMAR, Anil, M. , TULINSKY, John
IPC分类号： A61K31/53
CPC分类号： C07D403/12 , C07D251/16 , C07D251/18 , C07D251/22 , C07D405/12
摘要： The invention relates to aryl triazines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase β (LPAAT-β) activity and/or proliferation of cells such as tumor cells, where R 1 -R 5 are hydrogen or non-ydrogen substituents, and Q is a heteroatom or heteroatom attached to one or more methylene groups.
摘要翻译：本发明涉及芳基三嗪及其用途，包括抑制溶血磷脂酰基转移酶β（LPAAT-β）活性和/或细胞如肿瘤细胞的增殖，其中R 1 -R 5是氢或非 - 取代基，Q是与一个或多个亚甲基连接的杂原子或杂原子。

76. 发明申请

WO2002064573A1 NEUE CARBONSÄUREDERIVATE MIT ALKYLSUBSTITUIERTEN TRIAZINEN, IHRE HERSTELLUNG UND VERWENDUNG ALS ENDOTHELIN-REZEPTORANTAGONISTEN 审中-公开
标题翻译： NEW羧酸与烷基取代的三嗪，生产和使用AS内皮素受体拮抗剂衍生物
公开(公告)号：WO2002064573A1
公开(公告)日：2002-08-22
申请号：PCT/EP2001/001608
申请日：2001-02-14
申请人： BASF AKTIENGESELLSCHAFT , AMBERG, Wilhelm , KETTSCHAU, Georg , KLING, Andreas , RASCHACK, Manfred , HERGENRÖDER, Stefan , UNGER, Liliane
发明人： AMBERG, Wilhelm , KETTSCHAU, Georg , KLING, Andreas , RASCHACK, Manfred , HERGENRÖDER, Stefan , UNGER, Liliane
IPC分类号： C07D251/22
CPC分类号： C07D403/12 , C07D251/16 , C07D251/20 , C07D251/22
摘要： Die Erfindung betrifft Carbonsäurederivate der Formel (I), wobei die Substituenten die in der Beschreibung angegebene Bedeutung haben.
摘要翻译：本发明涉及式（I）其中取代基具有本说明书中给出的含义的羧酸衍生物。

77. 发明申请

WO01092236A1 4-ALKYL HALIDE TRIAZINE COMPOUNDS USED AS HERBICIDES 审中-公开
标题翻译： 4- HALOGENALKYLTRIAZINVERBINDUNGEN作为除草剂
公开(公告)号：WO01092236A1
公开(公告)日：2001-12-06
申请号：PCT/EP2001/005955
申请日：2001-05-23
IPC分类号： A01N43/66 , C07D251/22 , C07D405/04
CPC分类号： C07D405/04 , A01N43/66 , C07D251/22
摘要： The invention relates to 4-alkyl halide triazine compounds of the general formula (I): wherein the variables R , R , R , R , A, X, Y, Hal, n and R are defined as per claim 1 and to use of said compounds as herbicides.
摘要翻译：本发明涉及4- Halogenalkyltriazinverbindungen的通式：其中变量R <1>，R <2>，R <3>，R <4>中，A，X，Y，哈尔，n和R具有权利要求1中提到的含义有，以及使用这些化合物作为除草剂的。

78. 发明申请

WO01044208A1 4,6-SUBSTITUTED 2-AMINO-1,3,5-TRIAZINE DERIVATIVES, A METHOD FOR PRODUCING SAME AND THE USE THEREOF AS HERBICIDES AND PLANT GROWTH REGULATORS 审中-公开
标题翻译： 4,6-取代的2-氨基-1,3,5-三嗪衍生物，METHOD FOR THEIR及其作为除草剂和植物生长调节剂
公开(公告)号：WO01044208A1
公开(公告)日：2001-06-21
申请号：PCT/EP2000/011861
申请日：2000-11-28
IPC分类号： A01N43/68 , C07D251/18 , C07D251/22 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D521/00 , A01N43/66 , A01N43/76 , A01N43/78
CPC分类号： C07D231/12 , A01N43/68 , C07D233/56 , C07D249/08 , C07D251/18 , C07D251/22 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12
摘要： The invention relates to compounds of formula (I) and the salts thereof in the optically active form. The respective optically active compound is present as a pure stereo isomer (with R- or S-configuration) with regard to the configuration on the C-atom that is marked with a star (*) in formula (I) or as a mixture of the R- and S-stereo isomers with a surplus on one of the stereo isomers in relation to the total quantity of the R- and S-isomers. In said formula (I), R means optionally substituted aryl, cycloalkyl, heterocyclyl, alkyl, alkenyl or akinyl, R means an optionally substituted, saturated, parially unsaturated or aromatic carbocyclic or heterocyclic radical, R means hydrogen or an optionally substituted alkyl, aryl, cycloalkyl, a radical N(B -D )(B -D ) or NR'-N(B -D )(B -D ), R means a radical B -D , R , A means an optionally substituted alkylene, alkenylene or alkinylene, X, independently from each other, means halogen, hydroxy, amino, nitro, formyl, carboxy, cyano, thiocyanato, aminocarbonyl or optionally substituted alkyl, alkoxy, alkylthio, alkylamino, diakylamino, alkenyl, alkinyl, alkylcarbonyl, alkoxycarbonyl, alkylaminocarbonyl, diakylaminocarbonyl, N-alkanoylamino, N-alkanoyl-N-alkyl-amino, cycloalkyl, cycloalkoxy, cycloalkylamino, phenyl phenoxy, phenylthio, phenylcarbonyl, heterocyclyl, heterocyclyloxy, heterocyclylthio or heterocyclylamino or two adjacent radicals X, together, mean a fused carbocycle or heterocycle and n means 0.1 to 5. The inventive compounds are useful as herbicides and plant growth regulators. The compounds (I) can be produced via intermediate products of formulae (III) and (V).
摘要翻译：式（I）的化合物和盐，旋光体，（I），其中，所述各自的光学活性化合物，其为立体异构体（与在式（I有星号（具有R或S构型对于配置））* ）指定C-原子或R-和S-立体异构体与过量的一种立体异构体的混合物获得存在于R和S异构体的总量，并且R <1>是任选取代的芳基，环烷基，杂环基，烷基，烯基或炔基R 2 <2>是任选取代的，饱和的，部分不饱和或芳族碳环或杂环基团R <3>是氢或任选取代的烷基，芳基，环烷基，基团-N（B <1> -D <1> ）（B <2> -D <2>）或-NR'-N（B <1> -D <1>）（B <2> -D <2>）R <4>为基团-B <3 >ð<3> A是任选被取代的亚烷基，亚烯基或亚炔基，X独立地是卤素，羟基，氨基，硝基，甲酰基，羧基，氰基，氰硫基，AM inocarbonyl或任选取代的烷基，烷氧基，烷硫基，烷基氨基，Diakylamino，烯基，炔基，烷基羰基，烷氧基羰基，烷基氨基羰基，Diakylaminocarbonyl，N-烷酰基氨基，N-烷酰基 - N-烷基氨基，环烷基，环烷氧基，环烷基氨基，苯基，苯氧基，苯硫基，苯基羰基，杂环基，杂环氧基，杂环硫基或杂环基氨基; 或两个相邻基团X一起形成稠合的碳环或杂环N，0.1至5，意思是，适合作为除草剂和植物生长调节剂。化合物（I）可以通过下式的中间体制备，并产生（V）（III）。

79. 发明申请

WO00029392A1 PROCESS FOR PREPARING TRIAZINES USING A COMBINATION OF LEWIS ACIDS AND REACTION PROMOTERS 审中-公开
标题翻译：使用LEWIS酸和反应促进剂的组合制备TRIAZINES的方法
公开(公告)号：WO00029392A1
公开(公告)日：2000-05-25
申请号：PCT/US1999/027253
申请日：1999-11-17
IPC分类号： C07D251/14 , C07B61/00 , C07D251/22 , C07D251/24
CPC分类号： C07D251/24 , C07D251/22
摘要： It has been now surprisingly discovered after extensive research that 2-halo-4,6-bisaryl-1,3,5-triazine can be prepared with unprecedented selectivity, efficiency, mild conditions, and in high yield by the reaction of cyanuric halide with aromatics in the presence of at least one Lewis acid and at least one reaction promoter. This reaction is also unprecedently general as a variety of aromatics can be used to produce a wide selection of 2-halo-4,6-bisaryl-1,3,5-triazines. The novel approach includes the use of the reaction promoters in combination with at least one Lewis acid under certain reaction conditions to promote the formation of 2-halo-4,6-bisaryl-1,3,5-triazine compounds from cyanuric halide. Preferably, the Lewis acids and reaction promoters are combined to form a complex. 2-halo-4,6-bisaryl-1,3,5-triazines are key intermediates for making 2-(2-oxyaryl)-4,6-bisarly-1,3,5-triazine class of UV absorbers.
摘要翻译：现在已经广泛研究出人意料地发现，2-卤代-4,6-二芳基-1,3,5-三嗪可以以前所未有的选择性，效率，温和条件制备，并且通过氰尿酰卤与芳族化合物在至少一种路易斯酸和至少一种反应促进剂的存在下进行。该反应也是前所未有的，因为各种芳族化合物可用于产生广泛选择的2-卤代-4,6-二芳基-1,3,5-三嗪。该新方法包括在某些反应条件下使用反应促进剂与至少一种路易斯酸组合以促进由氰尿酰卤形成2-卤代-4,6-二芳基-1,3,5-三嗪化合物。优选将路易斯酸和反应促进剂组合以形成络合物。 2-卤代-4,6-二芳基-1,3,5-三嗪是制备2-（2-氧芳基）-4,6-双 - 1,3,5-三嗪类UV吸收剂的关键中间体。

80. 发明申请

WO99067225A1 BENZOCYCLE-SUBSTITUTED TRIAZINE AND PYRIMIDINE ULTRAVIOLET LIGHT ABSORBERS 审中-公开
标题翻译：苯并噻唑啉和紫杉醇紫外线吸收剂
公开(公告)号：WO99067225A1
公开(公告)日：1999-12-29
申请号：PCT/US1999/013708
申请日：1999-06-17
IPC分类号： A61K8/49 , A61Q17/04 , C07D239/26 , C07D239/32 , C07D251/20 , C07D251/22 , C07D251/24 , C08K5/3492 , A61K7/42
CPC分类号： A61K8/4966 , A61Q17/04 , C07D239/26 , C07D251/20 , C07D251/22 , C07D251/24 , C08K5/3492
摘要： This invention relates generally to benzocycle-substituted pyrimidines and triazines and the use thereof to protect against degradation by environmental forces, inclusive of ultraviolet light, actinic radiation, oxidation, moisture, atmospheric pollutants and combinations thereof. The new class of benzocycle-substituted pyrimidines and triazines comprises a benzocycle attached to the triazine or pyrimidine ring, and preferably an additional aryl ring containing a hydroxyl group, either free or blocked to form a latent stabilizer, ortho- to the point of attachment to the triazine or pyrimidine ring. These materials may, under the appropriate circumstances, be bonded to formulations comprising coatings, polymers, resins, organic compounds and the like via reaction of the bondable functionality with the materials of the formulation. A method for stabilizing a material by incorporating such benzocycle-substituted pyrimidines and triazines is also disclosed.
摘要翻译：本发明一般涉及苯并环取代的嘧啶和三嗪及其用于防止包括紫外光，光化辐射，氧化，水分，大气污染物及其组合在内的环境力降解的用途。新类型的苯并环取代的嘧啶和三嗪包括与三嗪或嘧啶环连接的苯并环，并且优选含有游离或封闭以形成潜稳定剂的羟基的另外的芳环，三嗪或嘧啶环。这些材料可以在适当的情况下通过可结合的官能团与制剂的材料的反应与包含涂料，聚合物，树脂，有机化合物等的制剂结合。还公开了通过掺入这种苯并环取代的嘧啶和三嗪来稳定材料的方法。

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