公开(公告)号：WO2009045311A1

公开(公告)日：2009-04-09

申请号：PCT/US2008/011100

申请日：2008-09-25

Applicant: MERCK & CO., INC. ,  SCYNEXIS, INC. ,  BALKOVEC, James, M. ,  SILIPHAIVANH, Phieng ,  BOUFFARD, Frances, Aileen ,  PEEL, Michael, R. ,  FAN, Weiming ,  MAMAI, Ahmed ,  DIMICK GRAY, Sarah, M.

Inventor： BALKOVEC, James, M. ,  SILIPHAIVANH, Phieng ,  BOUFFARD, Frances, Aileen ,  PEEL, Michael, R. ,  FAN, Weiming ,  MAMAI, Ahmed ,  DIMICK GRAY, Sarah, M.

IPC: A61K31/497

CPC classification number: C07J71/0005

Abstract: Novel derivatives of enfumafungin are disclosed herein, along with their, pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (l,3)-β-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.

Abstract translation: 本文公开了enfumafungin的新型衍生物及其药学上可接受的盐，水合物和前药。 还公开了包含这种化合物的组合物，制备这些化合物的方法和使用这种化合物作为抗真菌剂和/或（1,3）-β-D-葡聚糖合酶抑制剂的方法。 所公开的化合物，其药学上可接受的盐，水合物和前药，以及包含这些化合物，盐，水合物和前药的组合物可用于治疗和/或预防真菌感染和相关疾病和病症。

公开(公告)号：WO2007008942A3

公开(公告)日：2007-04-12

申请号：PCT/US2006026976

申请日：2006-07-11

Applicant: AERIE PHARMACEUTICALS INC ,  DELONG MITCHELL A ,  SZNAIDMAN MARCOS L ,  OAKLEY ROBERT H ,  ECKHARDT ALLEN E ,  HUDSON CHRISTINE ,  YINGLING JEFFREY D ,  PEEL MICHAEL ,  RICHARDSON THOMAS E ,  MURRAY CLAIRE LOUISE ,  RAO BYAPPANAHALLY N NARASINGA ,  HEASLEY BRIAN H ,  PATEL PARESMA R

Inventor： DELONG MITCHELL A ,  SZNAIDMAN MARCOS L ,  OAKLEY ROBERT H ,  ECKHARDT ALLEN E ,  HUDSON CHRISTINE ,  YINGLING JEFFREY D ,  PEEL MICHAEL ,  RICHARDSON THOMAS E ,  MURRAY CLAIRE LOUISE ,  RAO BYAPPANAHALLY N NARASINGA ,  HEASLEY BRIAN H ,  PATEL PARESMA R

IPC: C07D213/61 ,  A61K31/341 ,  A61K31/381 ,  A61K31/4164 ,  A61K31/44 ,  A61K31/47 ,  A61K31/513 ,  A61P27/02 ,  C07C251/86 ,  C07D213/36 ,  C07D215/42 ,  C07D233/88 ,  C07D239/54 ,  C07D307/52 ,  C07D333/36

CPC classification number: C07D401/12 ,  C07D213/53 ,  C07D213/61 ,  C07D213/75 ,  C07D215/12 ,  C07D215/42 ,  C07D233/64 ,  C07D239/52 ,  C07D239/54 ,  C07D307/14 ,  C07D307/52 ,  C07D333/22 ,  C07D401/14

Abstract: Hydrazide compounds with GPCR desensitization inhibitory activity are provided that may be used to influence, inhibit or reduce the action of a G-protein receptor kinase. Pharmaceutical compositions including therapeutically effective amounts of the hydrazide compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions controlled or influenced by GPCRs are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer osteoporosis and glaucoma are also provided. (Formula (I)). A is selected from a heteroaryl group (i): wherein X 1 , X 2 , X 3 and X 4 are, independently, CH, O, S or N-R 6 , with the proviso that at least one of X 2 or X 3 is O, S or N-R 6 ; and a heteroaryl group (ii): wherein X 5 and X 9 are CH or C-halogen, X 6 and X 8 are CH, and X 7 is N, and wherein the six-membered heteroaryl group may be further fused with an unsubstituted six-member aryl group; R 1 , R 2 , R 3 , R 4 , and R 5 are, independently, hydrogen; halogen; C 1 -C 4 alkyl; amino; nitro; cyano; heteroaryl; carboxy, carbonylamino; aminosulfonyl; sulfonylamino; aminoacyl; thioalkyl; sulfonyl; acyl; heterocycle; -OR; -O-C 1 -C 4 alkyl-heterocycle; -C(O)NH-C 1 -C 4 alkyl-heterocycle; -C(O)NH-heteroaryl; -C(O)NH-aryl; or carboxylamino; wherein R is C 1 -C 4 alkyl; aryl, heteroaryl, C 1 -C 4 alkyl aryl or C 1 -C 4 alkyl heteroaryl; R 6 is H or C 1 -C 4 alkyl; R 7 is hydrogen, C 1 -C 4 alkyl or C 1 -C 4 alkoxy; and X is N-R 6 .

Abstract translation: 提供具有GPCR脱敏抑制活性的酰肼化合物，其可用于影响，抑制或降低G蛋白受体激酶的作用。 还提供包含治疗有效量的酰肼化合物和药学上可接受的载体的药物组合物。 还提供了使用化合物和/或组合物影响受GPCR控制或影响的疾病状态或病症的各种方法。 还提供了使用化合物和/或组合物影响疾病状态或病症如癌症骨质疏松症和青光眼的各种方法。 （式（I））。 A选自杂芳基（i）：其中X 1，X 2，X 3和X 4 >独立地是CH，O，S或NR 6，条件是X 2或X 3中的至少一个是O ，S或NR 6; 和杂芳基（ii）：其中X 5和X 9是CH或C-卤素，X 6和X 8 H是CH，X 7是N，并且其中六元杂芳基可以进一步与未取代的六元芳基稠合; R 1，R 2，R 3，R 4和R 5， 独立地是氢; 卤素; C 1 -C 4烷基; 氨基; 硝基; 氰基; 杂; 羧基，羰基氨基; 氨基磺酰基; 磺酰; 氨; 硫代; 磺酰基; 酰基; 杂环; -要么; -O-C _{1 -C 4 烷基 - 杂环; -C（O）NH-C 1 -C 4 烷基 - 杂环; -C（O）NH杂芳基; -C（O）NH-芳基; 或羧基氨基; 其中R是C 1 -C 4烷基; 芳基，杂芳基，C 1 -C 4烷基芳基或C 1 -C 4烷基杂芳基; R 6是H或C 1 -C 4烷基; R 7是氢，C 1 -C 4烷基或C 1 -C 4烷基或C 1 -C 4 - 烷氧基; X为N-R 6。}

公开(公告)号：WO03051886A8

公开(公告)日：2004-08-19

申请号：PCT/US0239672

申请日：2002-12-11

Applicant: SMITHKLINE BEECHAM CORP ,  HARRIS PHILIP ANTHONY ,  JUNG DAVID KENDALL ,  PEEL MICHAEL ROBERT ,  RENO MICHAEL JOHN ,  RHEAULT TARA RENAE ,  BADIANG JENNIFER G ,  STEVENS KIRK LAWRENCE ,  VEAL JAMES MARVIN ,  DICKERSON SCOTT HOWARD ,  TAVARES FRANCIS XAVIER

Inventor： HARRIS PHILIP ANTHONY ,  JUNG DAVID KENDALL ,  PEEL MICHAEL ROBERT ,  RENO MICHAEL JOHN ,  RHEAULT TARA RENAE ,  BADIANG JENNIFER G ,  STEVENS KIRK LAWRENCE ,  VEAL JAMES MARVIN ,  DICKERSON SCOTT HOWARD ,  TAVARES FRANCIS XAVIER

IPC: A61K31/506 ,  A61K31/5377 ,  A61K45/00 ,  A61P35/00 ,  A61P43/00 ,  C07D487/04 ,  A61K31/5025

CPC classification number: C07D487/04

Abstract: Fused pyradazine derivatives, which are useful as CDK inhibitors are described herein. The described invention also includes methods of making such fused pyradazines derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.

Abstract translation: 本文描述了可用作CDK抑制剂的稠合的哒嗪衍生物。 所述的发明还包括制备这种稠合吡嗪嗪衍生物的方法以及使用它们在治疗过度增殖性疾病中的方法。

公开(公告)号：WO2002078700A1

公开(公告)日：2002-10-10

申请号：PCT/US2002/008524

申请日：2002-03-20

Applicant: SMITHKLINE BEECHAM CORPORATION ,  ALBERTI, Michael, John ,  CHAMBERLAIN, Stanley, D. ,  CHUENG, Mui ,  GUDMUNDSSON, Kristjan ,  HARRIS, Philip, Anthony ,  JOHNS, Brian, A. ,  JUNG, David, Kendall ,  PEEL, Michael, Robert ,  STANFORD, Jennifer, Badiang

Inventor： ALBERTI, Michael, John ,  CHAMBERLAIN, Stanley, D. ,  CHUENG, Mui ,  GUDMUNDSSON, Kristjan ,  HARRIS, Philip, Anthony ,  JOHNS, Brian, A. ,  JUNG, David, Kendall ,  PEEL, Michael, Robert ,  STANFORD, Jennifer, Badiang

IPC: A61K31/4162

CPC classification number: C07D471/04

Abstract: The present invention provides compounds of formula (I): wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.

Abstract translation: 本发明提供式（I）化合物：其中所有变量如本文所定义，含有该化合物的药物组合物，其制备方法及其作为药剂的用途。

公开(公告)号：WO1994011377A2

公开(公告)日：1994-05-26

申请号：PCT/US1993010987

申请日：1993-11-10

Applicant: GLAXO INC. ,  BESTERMAN, Jeffrey, Mark ,  EVANS, Michael, Glenn ,  LACKEY, Karen, Elizabeth ,  LUZZIO, Michael, Joseph ,  PEEL, Michael, Robert ,  STERNBACH, Daniel, David

Inventor： GLAXO INC.

IPC: C07D491/22

CPC classification number: C07D317/66 ,  C07D319/18

Abstract: The present invention relates to water soluble, camptothecin derivatives of formula (I), wherein A represents a moiety of formula (IIA), (IIB) or (IIC), X is selected from the group consisting of alkyl, aryl, (CH2)mOR , (CH2)mSR and (CH2)mNR R wherein m is an integer of 0 to 6, and R and R are hydrogen, lower alkyl, aryl or together with the nitrogen form a 5-7 membered ring; q is an integer of 0 to 2; n represents the integer 1 or 2; p is an integer of 1 to 6; Y and W are selected from the group consisting of alkyl, aryl, alkoxy, aryloxy and amino, Q is oxygen or sulfur; P is phosphorus; J represents the atoms necessary to complete a 5 or 6 membered aromatic ring; and the pharmaceutically acceptable salts thereof; their use as topoisomerase inhibitors, their preparation; and their use in the treatment of cancer.

Abstract translation: 本发明涉及式（I）的水溶性喜树碱衍生物，其中A表示式（IIA），（IIB）或（IIC）的部分，X选自烷基，芳基，（CH 2） mOR 1，（CH2）mSR 1和（CH2）mNR 1 R 2其中m是0-6的整数，R 1和R 2是氢，低级烷基， 芳基或与氮一起形成5-7元环; q为0〜2的整数; n表示整数1或2; p为1〜6的整数。 Y和W选自烷基，芳基，烷氧基，芳氧基和氨基，Q是氧或硫; 磷是磷; J表示完成5或6元芳环所必需的原子; 及其药学上可接受的盐; 它们用作拓扑异构酶抑制剂，它们的制备; 并用于治疗癌症。