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1. 发明申请

WO2008033757A3 2-(1-OXO-1H-ISOQUINOLIN-2-YL) ACETAMIDE DERIVATIVES 审中-公开
标题翻译： 2-（1-氧代-1H-异喹啉-2-基）乙酰胺衍生物
公开(公告)号：WO2008033757A3
公开(公告)日：2008-12-11
申请号：PCT/US2007077999
申请日：2007-09-10
申请人： ORGANON NV , LETOURNEAU JEFFREY , CHAN JUI HSIANG , JOKIEL PATRICK , OHLMEYER MICHAEL , NEAGU IRINA , RIVIELLO CHRISTOPHER MARK , MORPHY JOHN RICHARD , NAPIER SUSAN ELIZABETH , HO KOC-KAN
发明人： LETOURNEAU JEFFREY , CHAN JUI HSIANG , JOKIEL PATRICK , OHLMEYER MICHAEL , NEAGU IRINA , RIVIELLO CHRISTOPHER MARK , MORPHY JOHN RICHARD , NAPIER SUSAN ELIZABETH , HO KOC-KAN
IPC分类号： C07D217/24 , A61K31/472
CPC分类号： C07D217/24 , C07D401/12
摘要： The present invention relates to a 2-(1-oxo-IH-isoquinolin-2-yl)acetamide derivative of formula (I).
摘要翻译：本发明涉及式（I）的2-（1-氧代-1H-异喹啉-2-基）乙酰胺衍生物。

2. 发明申请

WO2008051826A3 PURINES AS PKC-THETA INHIBITORS 审中-公开
标题翻译：匹配PKC-THETA抑制剂
公开(公告)号：WO2008051826A3
公开(公告)日：2008-10-02
申请号：PCT/US2007081899
申请日：2007-10-19
申请人： ORGANON NV , PHARMACOPEIA INC , NEAGU IRINA , ROUGHTON ANDREW , HO KOC-KAN , DILLER DAVID , CHAN JUI HSIANG , KINGSBURY CELIA , OHLMEYER MICHAEL , WIJKMANS JACOBUS CORNELIS HENRICUS MARIA , TEERHUIS NEELTJE MIRANDA , LOMMERSE JOHANNES PETRUS MARIA
发明人： NEAGU IRINA , ROUGHTON ANDREW , HO KOC-KAN , DILLER DAVID , CHAN JUI HSIANG , KINGSBURY CELIA , OHLMEYER MICHAEL , WIJKMANS JACOBUS CORNELIS HENRICUS MARIA , TEERHUIS NEELTJE MIRANDA , LOMMERSE JOHANNES PETRUS MARIA
IPC分类号： C07D473/32 , A61K31/52 , A61P35/00
CPC分类号： C07D473/32
摘要： A chemical genus of purines, which are useful as PKC? inhibitors, is disclosed. The genus is represented by the formula (I); A representative example is: (II)
摘要翻译：一种化学属嘌呤，可用作PKC？公开了抑制剂。该属由式（I）表示; 一个具有代表性的例子是：（二）

3. 发明申请

WO2006133242A3 AZINONE AND DIAZINONE V3 INHIBITORS FOR DEPRESSION AND STRESS DISORDERS 审中-公开
标题翻译： AZINONE和DIAZINONE V3抑制剂抑制和应激障碍
公开(公告)号：WO2006133242A3
公开(公告)日：2007-02-15
申请号：PCT/US2006022025
申请日：2006-06-07
申请人： PHARMACOPEIA DRUG DISCOVERY , LETOURNEAU JEFFREY JOHN , HO KOC-KAN , OHLMEYER MICHAEL J , JOKIEL PATRICK , RIVIELLO CHRISTOPHER MARK
发明人： LETOURNEAU JEFFREY JOHN , HO KOC-KAN , OHLMEYER MICHAEL J , JOKIEL PATRICK , RIVIELLO CHRISTOPHER MARK
IPC分类号： A61K31/4412 , A61K31/50 , A61K31/505 , A61P25/24 , C07D213/82 , C07D239/30 , C07D239/36 , C07D295/088 , C07D403/04 , C07D403/12 , C07D413/04
CPC分类号： C07D213/82 , C07D239/26 , C07D239/36 , C07D241/24 , C07D295/088 , C07D403/04 , C07D403/12 , C07D413/04
摘要： Substituted pyridines, pyrimidines, pyrazines, pyridinones, pyrimidinones, pyrazinones and phenylacetamides useful in treating depression, stress and other disorders are disclosed. The compounds are of the formulae: (I).
摘要翻译：公开了用于治疗抑郁症，压力和其它疾病的取代的吡啶，嘧啶，吡嗪，吡啶酮，嘧啶酮，吡嗪酮和苯乙酰胺。化合物具有下式：（I）。

4. 发明申请

WO2008033764A2 QUINAZOLINONE AND ISOQUINOLINONE ACETAMIDE DERIVATIVES 审中-公开
标题翻译：喹唑啉酮和异喹啉酮酰胺衍生物
公开(公告)号：WO2008033764A2
公开(公告)日：2008-03-20
申请号：PCT/US2007078022
申请日：2007-09-10
申请人： ORGANON NV , LETOURNEAU JEFFREY , JOKIEL PATRICK , NAPIER ELIZABETH , HO KOC-KAN , OHLMEYER MICHAEL , MCARTHUR DUNCAN ROBERT , FIONA JEREMIAH , RATCLIFFE PAUL DAVID , SCHULZ JUERGEN
发明人： LETOURNEAU JEFFREY , JOKIEL PATRICK , NAPIER ELIZABETH , HO KOC-KAN , OHLMEYER MICHAEL , MCARTHUR DUNCAN ROBERT , FIONA JEREMIAH , RATCLIFFE PAUL DAVID , JURGEN SCHULZ
IPC分类号： A61K31/517 , A61K31/5377 , A61K31/551 , A61P25/00 , C07D401/02 , C07D403/02 , C07D413/14
CPC分类号： C07D403/04 , C07D217/24 , C07D239/91 , C07D401/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D471/08 , C07D487/04
摘要： The present invention relates to a quinazolinone or isoquinolinone derivative of formula I, wherein R 1 is C 1-6 alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkylC 1-3 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, said C 1-6 alkyl, C 3-6 cycloalkyl and C 3-6 cycloalkylC 1-3 alkyl being optionally substituted with hydroxy, C 1-6 alkyloxy, cyano or one or more halogens; R 2 is C 6-10 aryl optionally substituted with one to three substituents selected from halogen, hydroxy, cyano, C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 alkyloxy and C 3-6 cycloalkyloxy, said C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 alkyloxy and C 3-6 Cycloalkyloxy being optionally substituted with one or more halogens; or R 2 is a 5-10 membered heteroaryl ring system comprising a heteroatom selected from N, O and S and optionally substituted with a substituent selected from methyl, C 1-6 alkyloxy and halogen; or R 2 is C 4-7 cycloalkyl; R 3 is an optional substituent selected from C 1-6 alkyl, C 1-6 alkyloxy and halogen, said C 1-6 alkyl and C 1-6 alkyloxy being optionally substituted with one or more halogens; R 4 is a group located at the 6- or 7- position of the quinazolinone or isoquinolinone ring having the formula Il, wherein R 5 together with one of R 6 forms a 4-8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroatomic moiety selected from O, S and NR 9 , said heterocyclic ring being optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo or R 5 together with one of R 7 and R 8 forms a 6-8 membered heterocyclic ring optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo; Each R 6 is independently H, halogen or C 1-4 alkyl optionally substituted with halogen or SO 2 CH 3 or one of R 6 together with R 5 forms a 4-8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroatomic moiety selected from O, S and NR 9 , said heterocyclic ring being optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo; R 7 and R 8 are independently H, C 1-6 alkyl, C 3-6 cycloalkyl, C 3-6 cycloalkylc 1-3 alkyl, cyanoC 1-3 alkyl, C 6-10 aryl, C 6-10 arylC 1-3 alkyl, C 1-3 alkyloxyC 1-3 alkyl or C 1-6 acyl said C 1-6 alkyl, C 3-6 cycloalkyl and C 3-6 cycloalkylC 1-3 alkyl being optionally substituted with hydroxy, 1 or more halogens or diC 1-2 alkylamino; or R 7 and R 8 together with the nitrogen to which they are bonded form a 4-8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroatomic moiety selected from O, S and NR 10 , said heterocyclic ring being optionally substituted with one or two substituents selected from C 1-6 alkyl, halogen, hydroxy,
摘要翻译：本发明涉及式I的喹唑啉酮或异喹啉酮衍生物，其中R 1是C 1-6烷基，C 3-6环烷基，C 3-6环烷基C 1-3烷基，C 2-6链烯基，C 2-6亚炔基所述C 1-6烷基，C 3-6环烷基和C 3-6环烷基C 1-3烷基，烷基任选被羟基，C 1-6烷氧基，氰基或一个或多个卤素取代; R 2是任选被一至三个选自卤素，羟基，氰基，C 1-6烷基的取代基取代的C 6-10芳基， C 3-6环烷基，C 1-6烷氧基和C 3-6环烷氧基，所述C 1-6 - 亚烷基烷基，C 3-6环烷基，C 1-6烷氧基和C 3-6环烷氧基任选被一个或多个卤素取代; 或R 2是包含选自N，O和S的杂原子并任选被选自甲基，C 1-6烷基的取代基取代的5-10元杂芳基环系统。烷氧基和卤素; 或R 2是C 4-7环烷基; R 3是选自C 1-6烷基，C 1-6烷氧基和卤素的任意取代基，所述C 1〜 C 1-6烷基和任选被一个或多个卤素取代的C 1-6烷氧基; R 4是位于具有式II的喹唑啉酮或异喹啉酮环的6-或7-位的基团，其中R 5与R“ 6〜6元饱和或不饱和杂环任选地包含选自O，S和NR 9的另外的杂原子部分，所述杂环任选被一个或两个选自下列的取代基取代：从甲基，卤素，羟基和氧代或R 5与R 7和R 8和R 8之一一起形成6-8元杂环，任选地被一个或两个选自甲基，卤素，羟基和氧代的取代基取代; 每个R 6独立地是H，卤素或任选被卤素或SO 2 CH 3取代的C 1-4烷基 >或R 6中的一个与R 5一起形成4-8元饱和或不饱和杂环，任选地包含另外的选自O，S和NRO的杂原子部分所述杂环任选被一个或两个选自甲基，卤素，羟基和氧代的取代基取代; R 7和R 8独立地为H，C 1-6烷基，C 3-6环烷基，C 3-6个环烷基C 1-3烷基，氰基C 1-3烷基，C 6-10芳基，C C 6-10芳基C 1-3烷基，C 1-3烷氧基C 1-3烷基或C _{1-6个酰基，所述C 1-6烷基，C 3-6环烷基和C 3-6环烷基C SUB 任选被羟基，一个或多个卤素或二-C 1-2烷基氨基取代的烷基，或R 7和R 8与它们所键合的氮一起形成4-8元饱和或不饱和杂环，任选地包含另外的选自O， S和NR 10，所述杂环任选被一个或两个选自C 1-6烷基，卤素，羟基，}

5. 发明申请

WO2010008777A3 FUSED AZABICYCLIC PYRIDINES 审中-公开
标题翻译：熔化的亚硫酸吡啶
公开(公告)号：WO2010008777A3
公开(公告)日：2010-03-25
申请号：PCT/US2009048062
申请日：2009-06-19
申请人： LIGAND PHARM INC , LETOURNEAU JEFFREY JOHN , FLOYD DAVID M , HO KOC-KAN , OLSON JOHN T , RIVIELLO CHRISTOPHER MARK
发明人： LETOURNEAU JEFFREY JOHN , FLOYD DAVID M , HO KOC-KAN , OLSON JOHN T , RIVIELLO CHRISTOPHER MARK
IPC分类号： C07D471/04 , A61K31/437 , A61K31/4375 , A61K31/5365 , A61P25/28 , A61P27/02 , A61P29/00 , C07D498/04
CPC分类号： C07D471/04 , C07D495/04 , C07D519/00
摘要： Azabicyclic pyridine derivatives and pharmaceutically acceptable salts thereof are disclosed herein These compounds are useful as EP2 antagonists. Uses of these compounds and pharmaceutical compositions thereof are also disclosed.
摘要翻译：氮杂双环吡啶衍生物及其药学上可接受的盐在本文中公开。这些化合物可用作EP2拮抗剂。还公开了这些化合物及其药物组合物的用途。

6. 发明申请

WO2004071445A3 2-(AMINOMETHYL)ARYLAMIDE ANALGESICS 审中-公开
标题翻译： 2-（氨基甲酰基）亚胺酰胺
公开(公告)号：WO2004071445A3
公开(公告)日：2004-09-16
申请号：PCT/US2004004017
申请日：2004-02-11
申请人： PHARMACOPEIA DRUG DISCOVERY , 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： C07D207/08 , C07D209/14 , C07D209/16 , C07D209/44 , C07D211/22 , C07D213/81 , C07D217/04 , C07D223/16 , C07D295/155 , C07D401/06 , C07D401/12 , C07D471/04 , C07C237/30 , A61K31/166 , A61K31/4035 , A61K31/404 , A61K31/435 , A61K31/55 , C07C237/32 , C07D217/16
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：公开了可用作止痛剂的2-（氨基甲基）芳基酰胺的化学属。该属由式I表示：代表性的例子是：

7. 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）。

8. 发明申请

WO2007095495A3 BENZODIAZEPINE GCNF MODULATORS FOR STEM CELL MODULATION 审中-公开
标题翻译：用于干细胞调节的苯并嗪GCNF调节剂
公开(公告)号：WO2007095495A3
公开(公告)日：2007-11-22
申请号：PCT/US2007061984
申请日：2007-02-12
申请人： PHARMACOPEIA INC , ROUGHTEN ANDREW , RONG YAJING , QUINTERO JORGE , OHLMEYER MICHAEL , KULTGEN STEVEN , KINGSBURY CELIA , HO KOC-KAN
发明人： ROUGHTEN ANDREW , RONG YAJING , QUINTERO JORGE , OHLMEYER MICHAEL , KULTGEN STEVEN , KINGSBURY CELIA , HO KOC-KAN
IPC分类号： C07D243/14 , A61K31/5513 , A61P15/16 , A61P15/18 , A61P35/00 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06
CPC分类号： C07D243/14 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06
摘要： A genus of benzodiazepines that modulate Germ Cell Nuclear Factor (GCNF) is disclosed. The compounds are useful to regulate stem cell differentiation and as contraceptives. Other embodiments are also disclosed.
摘要翻译：公开了一种调节生殖细胞核因子（GCNF）的苯二氮卓类药物。这些化合物可用于调节干细胞分化和避孕药。还公开了其它实施例。

9. 发明申请

WO2009062059A3 ISOMERIC PURINONES AND 1H-IMIDAZOPYRIDINONES AS PKC-THETA INHIBITORS 审中-公开
标题翻译：作为PKC-THETA抑制剂的异构嘌呤和1H-咪唑吡啶
公开(公告)号：WO2009062059A3
公开(公告)日：2009-11-12
申请号：PCT/US2008082832
申请日：2008-11-07
申请人： PHARMACOPEIA LLC , ROUGHTON ANDREW , RONG YAJING , HO KOC-KAN , OHLMEYER MICHAEL , DILLER DAVID , CHAN RAY JUI-HSIANG , LAI GAIFA
发明人： ROUGHTON ANDREW , RONG YAJING , HO KOC-KAN , OHLMEYER MICHAEL , DILLER DAVID , CHAN RAY JUI-HSIANG , LAI GAIFA
IPC分类号： C07D471/04 , A61K31/4353 , A61K31/52 , A61P19/02 , A61P35/00 , C07D473/28
CPC分类号： C07D471/04 , C07D473/28
摘要： A chemical genus of purinones and 1H-imidazopyridinones, which are useful as PKC? inhibitors, and their methods of use are disclosed. The genus is represented by the Formula (I).
摘要翻译：嘌呤酮和1H-咪唑并吡啶酮的化学属，可用作PKC？抑制剂及其使用方法。该属由式（I）表示。

10. 发明申请

WO2011002814A2 BIARYL OXYACETIC ACID COMPOUNDS 审中-公开
标题翻译：二异氰酸酯化合物
公开(公告)号：WO2011002814A2
公开(公告)日：2011-01-06
申请号：PCT/US2010040482
申请日：2010-06-29
申请人： LIGAND PHARM INC , SMITHKLINE BEECHAM CORP , MCGUINNESS BRIAN F , HO KOC-KAN , BABU SURESH , DONG GUIZHEN , DUO JINGQI , LE THUY X H , SAIONZ KURT W , NEEB MICHAEL J
发明人： MCGUINNESS BRIAN F , HO KOC-KAN , BABU SURESH , DONG GUIZHEN , DUO JINGQI , LE THUY X H , SAIONZ KURT W , NEEB MICHAEL J
IPC分类号： C07C311/17
CPC分类号： C07C311/17 , C07C311/19 , C07C311/38 , C07C317/32
摘要： Some embodiments of the present invention include novel phenoxyacetic acids useful for the prevention and treatment of inflammatory disorders, including those affecting the respiratory system and skin. Some compounds provided include those of the general formula (I), and compounds of general formula (Ia).
摘要翻译：本发明的一些实施方案包括可用于预防和治疗炎症性疾病（包括影响呼吸系统和皮肤的那些）的新型苯氧基乙酸。提供的一些化合物包括通式（I）的化合物和通式（Ia）的化合物。

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