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1. 发明申请

WO2004062609A3 PYRIMIDINE DERIVATIVES AS IL-8 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡嗪衍生物作为IL-8受体拮抗剂
公开(公告)号：WO2004062609A3
公开(公告)日：2004-11-25
申请号：PCT/US2004000584
申请日：2004-01-09
申请人： PHARMACOPEIA INC , ERICKSON SHAWN DAVID , BALDWIN JOHN J , DOLLE RONALD E III , INGLESE JAMES , OHLMEYER MICHAEL H J , HO KOC-KAN , BOHNSTEDT ADOLPH C , KULTGEN STEVEN G , WEBB MARIA L , AULD DOUGLAS S , ROUGHTON ANDREW LAIRD , CONTI PAOLO GIOVANNI MARTINO C , LEYSEN DIRK , VAN DER LOUW JAAP , AKZO NOBEL NV
发明人： ERICKSON SHAWN DAVID , BALDWIN JOHN J , DOLLE RONALD E III , INGLESE JAMES , OHLMEYER MICHAEL H J , HO KOC-KAN , BOHNSTEDT ADOLPH C , KULTGEN STEVEN G , WEBB MARIA L , AULD DOUGLAS S , ROUGHTON ANDREW LAIRD , CONTI PAOLO GIOVANNI MARTINO C , LEYSEN DIRK , VAN DER LOUW JAAP
IPC分类号： A61P35/00 , C07D239/42 , C07D239/46 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/12 , C07D521/00 , A61K31/505 , A61K31/506 , C07D239/47 , C07D405/14
CPC分类号： C07D239/42 , C07D231/12 , C07D233/56 , C07D239/47 , C07D249/08 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/12
摘要： Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed. The compounds are of the formula (I). In these compounds, Q is preferably unsubstituted and substituted heterocyclyl; U is usually hydrogen or fluorine; and V is preferably hydrogen, halogen, alkyl, -O-alkyl or -S-alkyl. A representative example is formula (X).
摘要翻译：公开了含有嘧啶核的化合物及其用于治疗与不适当的白细胞介素-8受体活性有关的疾病和病症的用途。该化合物具有式（I）。在这些化合物中，Q优选为未取代的和取代的杂环基; U通常是氢或氟; 且V优选为氢，卤素，烷基，-O-烷基或-S-烷基。一个代表性的例子是公式（X）。

2. 发明申请

WO2011041655A1 QUINAZOLIN-4-AMINE DERIVATIVES; AND METHODS OF USE 审中-公开
标题翻译：喹唑啉-4-胺衍生物; 和使用方法
公开(公告)号：WO2011041655A1
公开(公告)日：2011-04-07
申请号：PCT/US2010/051090
申请日：2010-10-01
申请人： THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , THOMAS, Craig, J. , MOTT, Bryan, T. , TANEGA, Cordelle , SHEN, Min , AULD, Douglas, S. , ROSENTHAL, Andrew, S. , MALONEY, David, J.
发明人： THOMAS, Craig, J. , MOTT, Bryan, T. , TANEGA, Cordelle , SHEN, Min , AULD, Douglas, S. , ROSENTHAL, Andrew, S. , MALONEY, David, J.
IPC分类号： C07D401/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D419/12 , C07D419/14 , A61K31/517
CPC分类号： C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Disclosed herein are novel quinazolin-4-amine derivatives that are inhibitors of Clk1, Clk2, Clk3, Clk4, or Dyrk1A. Also disclosed are quinazolin-4-amine derivatives as potent and selective inhibitors of Clk1, Clk4, and Dyrk1A. These agents provide useful tools for the study of Clk1, Clk4 and Dyrk1A and their respective roles in pre-mRNA splicing. Methods of treating Clk1, Clk2, Clk4, or Dyrk1A kinase mediated disorders with certain quinazolin-4-amine derivatives are also disclosed.
摘要翻译：本文公开的是作为Clk1，Clk2，Clk3，Clk4或Dyrk1A的抑制剂的新的喹唑啉-4-胺衍生物。还公开了喹唑啉-4-胺衍生物作为Clk1，Clk4和Dyrk1A的有效和选择性抑制剂。这些试剂为研究Clk1，Clk4和Dyrk1A及其各自在mRNA前剪接中的作用提供了有用的工具。还公开了用某些喹唑啉-4-胺衍生物治疗Clk1，Clk2，Clk4或Dyrk1A激酶介导的病症的方法。

3. 发明申请

WO2010042867A3 ACTIVATORS OF HUMAN PYRUVATE KINASE 审中-公开
公开(公告)号：WO2010042867A3
公开(公告)日：2010-04-15
申请号：PCT/US2009/060237
申请日：2009-10-09
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , THOMAS, Craig J. , AULD, Douglas S. , INGLESE, James , SKOUMBOURDIS, Amanda P. , JIANG, Jian-Kang , BOXER, Matthew
发明人： THOMAS, Craig J. , AULD, Douglas S. , INGLESE, James , SKOUMBOURDIS, Amanda P. , JIANG, Jian-Kang , BOXER, Matthew
IPC分类号： C07D209/08 , C07D211/54 , C07D215/36 , C07D265/36 , C07D277/64 , C07D295/26 , C07D311/70 , C07D317/62 , C07D319/18 , C07D321/10 , C07D401/12 , C07D403/12 , C07D495/14 , A61K31/18 , A61P35/00
摘要： Disclosed are pyruvate kinase M2 activators, which are bis sulfonamide piperazinyl and piperidinyl compounds of Formula (I), 2,4-disubstituted 4 H - thieno[3,2- c ]pyrrole-2-(substituted benzyl)pyridazin-3(2 H )-ones of Formula (II) and 6-(3,4-dimethylphenylaminosulfonyl)-3,4-dihydro-1 H -quinolin-2-one of formula (III), wherein L, R 1 , R 2 , R 11 to R 16 , R 21 and R 22 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia.

4. 发明申请

WO2013043192A1 GALACTOKINASE INHIBITORS FOR THE TREATMENT AND PREVENTION OF ASSOCIATED DISEASES AND DISORDERS 审中-公开
标题翻译：用于治疗和预防相关疾病和疾病的GALACTOKINASE抑制剂
公开(公告)号：WO2013043192A1
公开(公告)日：2013-03-28
申请号：PCT/US2011/053021
申请日：2011-09-23
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , UNIVERSITY OF UTAH RESEARCH FOUNDATION , BOXER, Matthew B. , WALSH, Martin J. , LIU, Li , TANEGA, Cordelle D. , SHEN, Min , LAI, Kent , TANG, Manshu , AULD, Douglas S.
发明人： BOXER, Matthew B. , WALSH, Martin J. , LIU, Li , TANEGA, Cordelle D. , SHEN, Min , LAI, Kent , TANG, Manshu , AULD, Douglas S.
IPC分类号： C07D403/12 , C07D413/12 , C07D413/14 , C07D493/10 , C07D495/10 , A61K31/506 , A61K31/517 , A61P35/00 , A61P3/00
CPC分类号： A61K31/517 , A61K31/506 , A61K31/527 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/14 , C07D491/107 , C07D493/10 , C07D495/10
摘要： Disclosed are inhibitors of human galactokinase of formula (1) that are useful in treating or preventing a galactokinase mediated disease or disorder, e.g., galactosemia. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one inhibitor of the invention, and a method of treating or preventing such disease or disorder in a mammal. Formula (I)
摘要翻译：公开了可用于治疗或预防半乳糖激酶介导的疾病或病症例如半乳糖血症的式（1）的人类半乳糖激酶的抑制剂。还公开了包含药学上可接受的载体和本发明的至少一种抑制剂的组合物，以及治疗或预防哺乳动物中的这种疾病或病症的方法。式（I）

5. 发明申请

WO2004069829A1 (2S)-2-((PYRIMIDIN-4-YL)AMINO)-4-METHYLPENTANOIC ACID AMINOETHYLAMID DERIVATIVES AS IL-8 RECEPTOR MODULATORS FOR THE TREATMENT OF ATHEROSCLEROSIS AND RHEUMATOID ARTHRITIS 审中-公开
标题翻译：（2S）-2 - （（吡咯烷-4-基）氨基）-4-甲基戊酸氨基氨基甲酸酯衍生物作为治疗角质层坏死和炎症性角膜炎的IL-8受体调节剂
公开(公告)号：WO2004069829A1
公开(公告)日：2004-08-19
申请号：PCT/US2004/000437
申请日：2004-01-09
申请人： PHARMACOPEIA DRUG DISCOVERY, INC. , CONTI, Paolo, Giovanni, Martino , LEYSEN, Dirk , LOUNNAS, Valere, X., H. , OHLMEYER, Michael, H., J. , BOHNSTEDT, Adolph, C. , HO, Koc-Kan , KULTGEN, Steven, G. , ROUGHTON, Andrew, Laird , AULD, Douglas, S.
发明人： CONTI, Paolo, Giovanni, Martino , LEYSEN, Dirk , LOUNNAS, Valere, X., H. , OHLMEYER, Michael, H., J. , BOHNSTEDT, Adolph, C. , HO, Koc-Kan , KULTGEN, Steven, G. , ROUGHTON, Andrew, Laird , AULD, Douglas, S.
IPC分类号： C07D403/04
CPC分类号： C07D405/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/12 , C07D417/14 , C07D491/04
摘要： The invention relates to compounds of the formula: (I); wherein R1 is a basic moiety having the structure -NH(CH 2 ) 2 NR5R6, (Formula II) or (Formula II); wherein R5, R6 and R7 are independently selected from H, (1-6C)alkyl, (2-6C)alkenyl; (3-8C)cycloalkyl, and (1-6C)alkyl substituted with furanyl, (1-6C)alkoxy, (3-8C)cycloalkyl, trifluoromethyl or amido; or R5 and R6 together with N to which they are attached are a (4-8) membered heterocycle, which heterocycle may be substituted with (1-6C)alkoxy, trifluoromethyl or amido and which heterocycle may be fused with another (5-6) membered heterocycle; n is 1, 2 or 3; and the ring structure A represents a (4-6) membered heterocycle; R2 is (1-6C)alkyl, optionally substituted with (1-6C)alkoxy; R3 is aryl, heterocyclyl, -X-(CH 2 ) m aryl or -X-(CH 2 ) m -heterocyclyl, wherein X is O, S or NR8, R8 being H or (1-6C)alkyl, and m is 0, 1, 2 or 3; and R4 is H, (1-8C)akyl, (1-8C)alkoxy or (2-8C)alkenyl, the alkyl moiety of each optionally being substituted with hydroxy, halogen, cyano, nitro, oxo, amino, alkylamino, dialkylamino, amido, alkylamido, carboxy, (1-8C)alkoxy, (1-8C)alkylthio, perfluoro (1-4C)alkyl, (3-8C)cycloalky, aryl, aryloxy, heterocyclyl or-0-heterocyclyl; or a pharmaceutically acceptable salt thereof. The compounds of the invention are Il-8 receptor modulators, in particular inhibitors thereof, and can be used for treating or preventing Il-8 receptor mediated disorders, such as atherosclerosis, inflammation, rheumatoid arthritis and related disorders.
摘要翻译：本发明涉及下式的化合物：（I）; 其中R1是具有结构-NH（CH 2）2 NR 5 R 6，（式II）或（式II）的碱性部分; 其中R5，R6和R7独立地选自H，（1-6C）烷基，（2-6C）烯基; （3-8C）环烷基和被呋喃基，（1-6C）烷氧基，（3-8C）环烷基，三氟甲基或酰氨基取代的（1-6C）烷基; 或R 5和R 6与它们所连接的N一起为（4-8）元杂环，该杂环可以被（1-6C）烷氧基，三氟甲基或酰氨基取代，并且该杂环可以与另一个（5-6 ）元杂环 n为1,2或3; 环结构A表示（4-6）元杂环; R2是（1-6C）烷基，任选地被（1-6C）烷氧基取代; R3是芳基，杂环基，-X-（CH2）马来酰基或-X-（CH2）m-杂环基，其中X是O，S或NR8，R8是H或（1-6C）烷基，m是0,1 ，2或3; 并且R 4是H，（1-8C）烷基，（1-8C）烷氧基或（2-8C）烯基，其烷基部分任选被羟基，卤素，氰基，硝基，氧代，氨基，烷基氨基，二烷基氨基，（1-8C）烷氧基，（1-8C）烷硫基，全氟（1-4C）烷基，（3-8C）环烷基，芳基，芳氧基，杂环基或-O-杂环基; 或其药学上可接受的盐。本发明的化合物是II-8受体调节剂，特别是其抑制剂，并且可用于治疗或预防II-8受体介导的病症，例如动脉粥样硬化，炎症，类风湿性关节炎和相关疾病。

6. 发明申请

WO2011137089A1 ACTIVATORS OF HUMAN PYRUVATE KINASE 审中-公开
标题翻译：人类激素激酶的激活剂
公开(公告)号：WO2011137089A1
公开(公告)日：2011-11-03
申请号：PCT/US2011/033852
申请日：2011-04-26
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , BOXER, Matthew, B. , SHEN, Min , AULD, Douglas, S. , THOMAS, Craig, J. , WALSH, Martin, J.
发明人： BOXER, Matthew, B. , SHEN, Min , AULD, Douglas, S. , THOMAS, Craig, J. , WALSH, Martin, J.
IPC分类号： C07D209/30 , C07D215/36 , C07D223/16 , C07D265/36 , A61K31/404 , A61K31/4704 , A61K31/538 , A61K31/55 , A61P35/00
CPC分类号： C07D215/227 , C07D209/12 , C07D209/30 , C07D209/34 , C07D215/36 , C07D223/16 , C07D235/26 , C07D265/36
摘要： Disclosed are pyruvate kinase M2 activators which are compounds of Formula (I), including those of Formula (II), wherein A 1 , A 2 , L, R, R 1 to R 3 , X 1 to X 3 , k, n, and m are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer. A 1 -NR-L-A 2 (I)
摘要翻译：公开了作为式（I）化合物的丙酮酸激酶M2活化剂，包括式（II）的化合物，其中A1，A2，L，R，R1至R3，X1至X3，k，n和m如本文所定义，其可用于治疗可通过激活PKM2（例如癌症）治疗的许多疾病。 A1 -NR-L-A2（I）

7. 发明申请

WO2010042867A2 ACTIVATORS OF HUMAN PYRUVATE KINASE 审中-公开
标题翻译：人类激素激酶的激活剂
公开(公告)号：WO2010042867A2
公开(公告)日：2010-04-15
申请号：PCT/US2009060237
申请日：2009-10-09
申请人： US HEALTH , THOMAS CRAIG J , AULD DOUGLAS S , INGLESE JAMES , SKOUMBOURDIS AMANDA P , JIANG JIAN-KANG , BOXER MATTHEW
发明人： THOMAS CRAIG J , AULD DOUGLAS S , INGLESE JAMES , SKOUMBOURDIS AMANDA P , JIANG JIAN-KANG , BOXER MATTHEW
IPC分类号： C07D209/08 , A61K31/18 , A61P35/00 , C07D211/54 , C07D215/36 , C07D265/36 , C07D277/64 , C07D295/26 , C07D311/70 , C07D317/62 , C07D319/18 , C07D321/10 , C07D401/12 , C07D403/12 , C07D495/14
CPC分类号： A61K31/496 , A61K31/445 , A61K31/495 , A61K31/5025 , C07D295/26 , C07D319/18 , C07D495/14
摘要： Disclosed are pyruvate kinase M2 activators, which are, bis sulfonamide piperazinyl compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and R1 to R16 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia, Formulas (I); (II).
摘要翻译：公开了丙酮酸激酶M2活化剂，其为式（I）的双磺酰胺哌嗪基化合物和2,4-二取代的4H-噻吩并[3,2-b]吡咯-2-（取代的苄基）哒嗪-3（2H）式（II）的化合物，其中L和R 1至R 16如本文所定义，其可用于治疗可通过PKM2的活化治疗的许多疾病，例如癌症和贫血，式（I）; （II）。

8. 发明申请

WO2005114198A3 PROTEIN PHOSPHORYLATION ASSAY 审中-公开
标题翻译：蛋白质磷酸化测定
公开(公告)号：WO2005114198A3
公开(公告)日：2006-05-26
申请号：PCT/US2005017711
申请日：2005-05-19
申请人： PHARMACOPEIA INC , AULD DOUGLAS S
发明人： AULD DOUGLAS S
IPC分类号： C12N9/12 , C12Q1/42 , C12Q1/48 , G01N33/573
CPC分类号： C12Q1/42 , C12Q1/485 , G01N2500/00
摘要： The present invention provides methods for assaying the activity of protein kinases or phosphatases that involve reacting the enzymes with substrate, at least a portion of which is fluorescently labeled; allowing phosphorylated substrate to bind to a solid support coated with a phosphate-binding material; and measuring the fluorescence produced by bound, labeled substrate. The invention also provides methods for identifying substances that modulate the activity of protein kinases and phosphatases that comprise reacting the enzymes with a substrate, at least a portion of which is fluorescently labeled, in the presence and absence of test compounds, allowing phosphorylated substrate to bind to a solid support coated with a phosphate-binding material, measuring the fluorescence produced by bound, labeled substrate, and comparing the fluorescence from reactions carried out in the presence and absence of test compounds.
摘要翻译：本发明提供了用于测定蛋白激酶或磷酸酶的活性的方法，其涉及使酶与底物反应，其中至少一部分被荧光标记; 允许磷酸化底物结合涂覆有磷酸盐结合材料的固体支持物; 并测量由结合的标记底物产生的荧光。本发明还提供了用于鉴定调节蛋白激酶和磷酸酶的活性的物质的方法，其包括在存在和不存在测试化合物的情况下使酶与底物反应，其中至少一部分被荧光标记，允许磷酸化底物结合包被磷酸盐结合材料的固体支持物，测量由结合的标记底物产生的荧光，并比较在存在和不存在测试化合物的情况下进行的反应的荧光。

9. 发明申请

WO2004063192A1 IMIDAZOLYL PYRIMIDINE DERIVATIVES USEFUL AS IL-8 RECEPTOR MODULATORS 审中-公开
标题翻译：作为IL-8受体调节剂有用的咪唑啉衍生物衍生物
公开(公告)号：WO2004063192A1
公开(公告)日：2004-07-29
申请号：PCT/US2004/000469
申请日：2004-01-09
申请人： PHARMACOPEIA DRUG DISCOVERY, INC. , VAN DER LOUW, Jaap , OHLMEYER, Michael, H., J. , BOHNSTEDT, Adolph, C. , HO, Koc-Kan , AULD, Douglas, S. , KULTGEN, Steven, G. , ROUGHTON, Andrew, Laird
发明人： VAN DER LOUW, Jaap , OHLMEYER, Michael, H., J. , BOHNSTEDT, Adolph, C. , HO, Koc-Kan , AULD, Douglas, S. , KULTGEN, Steven, G. , ROUGHTON, Andrew, Laird
IPC分类号： C07D405/14
CPC分类号： C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The invention relates to compounds of the formula I, wherein R1, R2, R3 and R4 are each independently selected from H, (1-4C)alkyl, (1-4C)alkoxy, trifluoromethyl, trifluoromethoxy, halogen, amino, sulfonamide, cyano, OH and nitro; R5 is H or (1-6C)alkyl; R6 is H, (1-6C)alkyl or (1-6C)alkoxy; R7 is H or (1-6C)alkyl; R8 is (1-6C)alkyl, optionally substituted with (1-6C)alkoxy; R9 is -(CH 2 ) n R10, wherein n is 1, 2 or 3 and R10 is selected from (1-4C)alkoxy, (1-4C)alkylthio, trifluoromethyl, (3-8C)cycloalkyl, phenyl optionally substituted with (1-4C)alkoxy, -NR11R12 and -O(CH 2 ) 2 NR11R12, wherein one of R11 and R12 is (1-4C)alkoxy, the other being H or (1-4C)alkyl, or R9 is -CH 2 (2-7C)heterocycloalkyl, provided that when at least one heteroatom in the heterocycloalkyl moiety is nitrogen, the distance between this nitrogen and the nitrogen in "NHR9" is at least three carbon atoms, or R9 is -(CH 2 ) 3 (2-7C)heterocycloalkyl or -(CH 2 ) 2 CHR13R14, wherein R13 and R14 together with the carbon atom to which they are attached, are (2-7C)heterocycloalkyl; and X is O, S or NH; or a pharmaceutically acceptable salt thereof. The compounds of the invention are Il-8 receptor modulators, in particular inhibitors thereof, and can be used for treating or preventing Il-8 receptor mediated disorders, such as atherosclerosis, inflammation, rheumatoid arthritis and related disorders.
摘要翻译：本发明涉及式I化合物，其中R 1，R 2，R 3和R 4各自独立地选自H，（1-4C）烷基，（1-4C）烷氧基，三氟甲基，三氟甲氧基，卤素，氨基，磺酰胺，氰基，OH和硝基; R5是H或（1-6C）烷基; R6是H，（1-6C）烷基或（1-6C）烷氧基; R 7为H或（1-6C）烷基; R8是（1-6C）烷基，任选被（1-6C）烷氧基取代; R9为 - （CH2）nR10，其中n为1,2或3，R10选自（1-4C）烷氧基，（1-4C）烷硫基，三氟甲基，（3-8C）环烷基，任选被（1 -4C）烷氧基，-NR11R12和-O（CH2）2NR11R12，其中R11和R12之一为（1-4C）烷氧基，另一个为H或（1-4C）烷基，或R9为-CH2（2-7C ）杂环烷基，条件是当杂环烷基部分中的至少一个杂原子为氮时，“NHR9”中该氮与氮之间的距离为至少三个碳原子，或者R 9为 - （CH 2）3（2-7C）杂环烷基或 - （CH 2）2 CHR 13 R 14，其中R 13和R 14与它们所连接的碳原子一起为（2-7C）杂环烷基; X为O，S或NH; 或其药学上可接受的盐。本发明的化合物是II-8受体调节剂，特别是其抑制剂，并且可用于治疗或预防II-8受体介导的病症，例如动脉粥样硬化，炎症，类风湿性关节炎和相关疾病。

10. 发明申请

WO2004062609A2 PYRIMIDINE DERIVATIVES AS IL-8 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：嘧啶衍生物作为IL-8受体拮抗剂
公开(公告)号：WO2004062609A2
公开(公告)日：2004-07-29
申请号：PCT/US2004/000584
申请日：2004-01-09
申请人： PHARMACOPEIA, INC. , AKZO NOBEL N.V. , ERICKSON, Shawn, David , BALDWIN, John, J. , DOLLE, Ronald, E., III , INGLESE, James , OHLMEYER, Michael H.J. , HO, Koc-Kan , BOHNSTEDT, Adolph, C. , KULTGEN, Steven, G. , WEBB, Maria, L. , AULD, Douglas, S. , ROUGHTON, Andrew, Laird , CONTI, Paolo, Giovanni, Martino, Conti , LEYSEN, Dirk , VAN DER LOUW, Jaap
发明人： ERICKSON, Shawn, David , BALDWIN, John, J. , DOLLE, Ronald, E., III , INGLESE, James , OHLMEYER, Michael H.J. , HO, Koc-Kan , BOHNSTEDT, Adolph, C. , KULTGEN, Steven, G. , WEBB, Maria, L. , AULD, Douglas, S. , ROUGHTON, Andrew, Laird , CONTI, Paolo, Giovanni, Martino, Conti , LEYSEN, Dirk , VAN DER LOUW, Jaap
IPC分类号： A61K
CPC分类号： C07D239/42 , C07D231/12 , C07D233/56 , C07D239/47 , C07D249/08 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/12
摘要： Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed. The compounds are of the formula (I). In these compounds, Q is preferably unsubstituted and substituted heterocyclyl; U is usually hydrogen or fluorine; and V is preferably hydrogen, halogen, alkyl, -O-alkyl or -S-alkyl. A representative example is formula (X).
摘要翻译：公开了含有嘧啶核的化合物及其用于治疗与不适当的白细胞介素-8受体活性有关的疾病和病症的用途。该化合物是式（I）的化合物。在这些化合物中，Q优选是未取代的和取代的杂环基; U通常是氢或氟; 并且V优选为氢，卤素，烷基，-O-烷基或-S-烷基。一个代表性的例子是公式（X）。

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