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1. 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）。

2. 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。

3. 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。

4. 发明申请

WO2004071445A2 2-(AMINOMETHYL)ARYLAMIDE ANALGESICS 审中-公开
标题翻译： 2-（氨基甲基）丙酰胺解毒剂
公开(公告)号：WO2004071445A2
公开(公告)日：2004-08-26
申请号：PCT/US2004/004017
申请日：2004-02-11
申请人： PHARMACOPEIA DRUG DISCOVERY, INC. , HO, Koc-Kan , BALDWIN, John, J. , BOHNSTEDT, Adolph, C. , KULTGEN, Steven, G. , MCDONALD, Edward , GUO, Tao , MORPHY, John, Richard , RANKOVIC, Zoran , HORLICK, Robert , APPELL, Kenneth, C.
发明人： HO, Koc-Kan , BALDWIN, John, J. , BOHNSTEDT, Adolph, C. , KULTGEN, Steven, G. , MCDONALD, Edward , GUO, Tao , MORPHY, John, Richard , RANKOVIC, Zoran , HORLICK, Robert , APPELL, Kenneth, C.
IPC分类号： A61K
CPC分类号： C07C237/30 , C07C237/32 , C07C311/08 , C07C311/37 , C07C323/42 , C07C2602/10 , C07C2602/12 , C07D207/08 , C07D209/14 , C07D209/16 , C07D209/44 , C07D211/22 , C07D213/81 , C07D217/04 , C07D223/16 , C07D295/155 , C07D401/06 , C07D401/12 , C07D471/04
摘要： A chemical genus of 2-(aminomethyl)arylamides, which are useful as analgesics, is disclosed. The genus is represented by the Formula I: a representative example is:
摘要翻译：公开了可用作镇痛剂的2-（氨基甲基）芳基酰胺的化学属。该属由公式I表示：一个代表性的例子是：

5. 发明申请

WO2010091009A1 ISOXAZOLE-3-CARBOXAMIDE DERIVATIVES 审中-公开
标题翻译： ISOXAZOLE-3-CARBOXAMIDE衍生物
公开(公告)号：WO2010091009A1
公开(公告)日：2010-08-12
申请号：PCT/US2010/022869
申请日：2010-02-02
申请人： N.V. ORGANON , PHARMACOPEIA, LLC , PALIN, Ronald , RATCLIFFE, Paul, David , KULTGEN, Steven, G. , HO, Koc-Kan , ROUGHTON, Andrew, Laird , OHLMEYER, Michael
发明人： PALIN, Ronald , RATCLIFFE, Paul, David , KULTGEN, Steven, G. , HO, Koc-Kan , ROUGHTON, Andrew, Laird , OHLMEYER, Michael
IPC分类号： C07D261/18 , C07D413/06 , C07D413/12 , A61P25/00 , A61K31/42 , A61K31/422 , A61K31/45 , A61K31/4468 , A61K31/4453 , A61K31/4439 , A61K31/5377
CPC分类号： C07D261/18 , C07D413/06 , C07D413/12
摘要： The present invention relates to isoxazole-3-carboxamide derivative having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-3-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders.
摘要翻译：本发明涉及具有通式I的异恶唑-3-甲酰胺衍生物或其药学上可接受的盐，其涉及包含该异构体的药物组合物，以及所述异恶唑-3-甲酰胺衍生物用于治疗TRPV1介导的急性和慢性疼痛障碍，急性和慢性神经性疼痛，急性和慢性炎性疼痛，呼吸系统疾病和下尿路疾病。

6. 发明申请

WO2009016241A1 5-PHENYL-ISOXAZOLE-3-CARBOXAMIDE DERIVATIVES AS TRPV1 MODULATORS 审中-公开
标题翻译：作为TRPV1调节剂的5-苯基 - 异恶唑-3-羧酰胺衍生物
公开(公告)号：WO2009016241A1
公开(公告)日：2009-02-05
申请号：PCT/EP2008/060090
申请日：2008-07-31
申请人： N.V. ORGANON , ROUGHTON, Andrew, Laird , HO, Koc-Kan , OHLMEYER, Michael , NEAGU, Irina , KULTGEN, Steven, G. , ANSARI, Nasrin , RONG, Yajing , RATCLIFFE, Paul, David , PALIN, Ronald
发明人： ROUGHTON, Andrew, Laird , HO, Koc-Kan , OHLMEYER, Michael , NEAGU, Irina , KULTGEN, Steven, G. , ANSARI, Nasrin , RONG, Yajing , RATCLIFFE, Paul, David , PALIN, Ronald
IPC分类号： C07D261/14 , A61K31/4155 , A61P25/00 , A61P29/00
CPC分类号： C07D413/12 , C07D261/18
摘要： The present invention relates to isoxazole-3-carboxamide derivative having the general Formula (I), or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-3-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders.
摘要翻译：本发明涉及具有通式（I）的异恶唑-3-甲酰胺衍生物或其药学上可接受的盐，涉及含有该异构体的异恶唑-3-甲酰胺衍生物用于治疗的药物组合物的TRPV1介导的疾病，例如急性和慢性疼痛障碍，急性和慢性神经性疼痛，急性和慢性炎性疼痛，呼吸系统疾病和下尿路疾病。

7. 发明申请

WO2002070493A1 BISARYL DERIVATIVES HAVING FSH RECEPTOR MODULATORY ACTIVITY 审中-公开
标题翻译：具有FSH受体调节剂活性的双联衍生物
公开(公告)号：WO2002070493A1
公开(公告)日：2002-09-12
申请号：PCT/US2002/003777
申请日：2002-01-18
申请人： PHARMACOPEIA, INC. , GUO, Tao , HO, Koc-Kan , MCDONALD, Edward , DOLLE, Roland, Ellwood , SAIONZ, Kurt, W. , KULTGEN, Steven, G. , LIU, Ruiyan , DONG, Guizhen , GENG, Peng , ADANG, Anton, Egbert, Peter , VAN STRATEN, Nicole, Corine, Renee
发明人： GUO, Tao , HO, Koc-Kan , MCDONALD, Edward , DOLLE, Roland, Ellwood , SAIONZ, Kurt, W. , KULTGEN, Steven, G. , LIU, Ruiyan , DONG, Guizhen , GENG, Peng , ADANG, Anton, Egbert, Peter , VAN STRATEN, Nicole, Corine, Renee
IPC分类号： C07D241/08
CPC分类号： C07D207/273 , A61K38/00 , C07C237/22 , C07C271/22 , C07C275/14 , C07C2601/02 , C07D223/10 , C07D233/76 , C07D241/08 , C07D243/08 , C07K5/06078 , C07K5/06191
摘要： The invention relates to a bisaryl derivative of the formula I, wherein (R, R) is selected from (H, H), O, (H, CH 3 ), (H, OH) and (H, CN); Ar is substituted phenyl; and A is a group of following formula II, III, IV or V: The compounds of the invention have FSH receptor modulatory activity and can be used for the control of fertility, for contraception or for treatment of hormone-dependent disorders.
摘要翻译：本发明涉及式I的二芳基衍生物，其中（R，R）选自（H，H），O，（H，CH 3），（H，OH）和（H，CN）; Ar是取代的苯基; 并且A是以下式II，III，IV或V的组：本发明的化合物具有FSH受体调节活性，并且可用于控制生育力，避孕或用于治疗激素依赖性疾病。

8. 发明申请

WO2013013188A1 HETEROCYCLIC PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：杂环蛋白激酶抑制剂
公开(公告)号：WO2013013188A1
公开(公告)日：2013-01-24
申请号：PCT/US2012/047685
申请日：2012-07-20
申请人： TOLERO PHARMACEUTICALS, INC. , XU, Yong , BRENNING, Benjamin, Gary , KULTGEN, Steven, G. , LIU, Xiaohui , SAUNDERS, Michael , HO, Koc-Kan
发明人： XU, Yong , BRENNING, Benjamin, Gary , KULTGEN, Steven, G. , LIU, Xiaohui , SAUNDERS, Michael , HO, Koc-Kan
IPC分类号： A61K31/497
CPC分类号： C07D487/04 , C07D471/04
摘要： The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R 1 , R 2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.
摘要翻译：本发明提供具有以下结构（I），（II）或（III）之一的蛋白激酶：或其立体异构体，前药，互变异构体或其药学上可接受的盐，其中R，R 1，R 2和X如本文所定义。还公开了用于治疗癌症，自身免疫性，炎性和其它Pim激酶相关病症的组合物和方法。

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