公开(公告)号：WO2010125082A1

公开(公告)日：2010-11-04

申请号：PCT/EP2010/055666

申请日：2010-04-28

Applicant: GLAXO GROUP LIMITED ,  HAMBLIN, Julie, Nicole ,  JONES, Paul, Spencer ,  KEELING, Suzanne, Elaine ,  LE, Joelle ,  MITCHELL, Charlotte, Jane ,  PARR, Nigel, James

Inventor： HAMBLIN, Julie, Nicole ,  JONES, Paul, Spencer ,  KEELING, Suzanne, Elaine ,  LE, Joelle ,  MITCHELL, Charlotte, Jane ,  PARR, Nigel, James

IPC: C07D413/14 ,  A61K31/422 ,  A61K31/4439 ,  A61P35/00 ,  A61P37/00 ,  A61P11/00 ,  A61P31/12

CPC classification number: A61K31/5377 ,  A61K31/496 ,  A61K31/497 ,  A61K31/535 ,  A61K45/06 ,  C07B2200/13 ,  C07D413/14 ,  Y02A50/409

Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.

Abstract translation: 本发明涉及某些新化合物。 具体地，本发明涉及式（I）的化合物及其盐。 本发明的化合物是激酶活性抑制剂，特别是PI3-激酶活性。

公开(公告)号：WO2011098451A1

公开(公告)日：2011-08-18

申请号：PCT/EP2011/051828

申请日：2011-02-08

Applicant: GLAXOSMITHKLINE LLC ,  BAZIN-LEE, Helene ,  COE, Diane, Mary ,  JOHNSON, David, A. ,  MITCHELL, Charlotte, Jane

Inventor： BAZIN-LEE, Helene ,  COE, Diane, Mary ,  JOHNSON, David, A. ,  MITCHELL, Charlotte, Jane

IPC: C07D473/16 ,  C07D473/18 ,  A61K31/522 ,  A61P35/00 ,  A61P29/00 ,  A61P11/06 ,  A61P31/00

CPC classification number: C07D473/18 ,  C07D473/16

Abstract: Compounds of formula (I), wherein; R 1 represents hydrogen or C 1-3 alkyl; n is an integer having a value of 1 to 5; X represents O or NH; Y represents C or N; or a pharmaceutically acceptable salt thereof, have been shown to be inducers of human interferon and may possess an improved profile with respect to known inducers of human interferon, for example enhanced potency. The compounds of the invention may therefore be useful in the treatment of various disorders, in particular the treatment of infectious diseases, cancer, allergic diseases and other inflammatory conditions, and their use as vaccine adjuvants.

Abstract translation: 式（I）化合物，其中： R1代表氢或C1-3烷基; n为1〜5的整数， X表示O或NH; Y表示C或N; 已经显示其是人类干扰素的诱导剂，并且相对于人干扰素的已知诱导剂可能具有改进的特征，例如增强的效力。 因此，本发明的化合物可用于治疗各种疾病，特别是治疗感染性疾病，癌症，过敏性疾病和其它炎性病症，以及它们作为疫苗佐剂的用途。

公开(公告)号：WO2010018131A1

公开(公告)日：2010-02-18

申请号：PCT/EP2009/060263

申请日：2009-08-07

Applicant: SMITHKLINE BEECHAM CORPORATION ,  BAZIN-LEE, Helene ,  BIGGADIKE, Keith ,  COE, Diane, Mary ,  LEWELL, Xiao, Qing ,  MITCHELL, Charlotte, Jane ,  TRIVEDI, Naimisha

Inventor： BAZIN-LEE, Helene ,  BIGGADIKE, Keith ,  COE, Diane, Mary ,  LEWELL, Xiao, Qing ,  MITCHELL, Charlotte, Jane ,  TRIVEDI, Naimisha

IPC: C07D473/16 ,  C07D473/18 ,  A61K31/522 ,  A61P37/00 ,  A61P35/00

CPC classification number: C07D473/16 ,  C07D473/18

Abstract: Compounds of Formula (I): wherein R 1 is C 1-6 alkylamino, C 1-6 alkoxy, or C 3-7 cycloalkyloxy; m is an integer having a value of 2 to 6; R 2 is hydrogen, C 1-6 alkyl, or C 3-7 cycloalkylC 0-6 alkyl; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.

Abstract translation: 式（I）的化合物：其中R 1是C 1-6烷基氨基，C 1-6烷氧基或C 3-7环烷氧基; m为2〜6的整数; R 2是氢，C 1-6烷基或C 3-7环烷基C 1-6烷基; 其盐是人类干扰素的诱导剂。 诱导人类干扰素的化合物可用于治疗各种疾病，例如治疗过敏性疾病和其它炎性病症，例如过敏性鼻炎和哮喘，治疗感染性疾病和癌症，并且也可用作疫苗佐剂。

公开(公告)号：WO2004024728A3

公开(公告)日：2004-10-21

申请号：PCT/EP0311814

申请日：2003-09-12

Applicant: GLAXO GROUP LTD ,  ALLEN DAVID GEORGE ,  COE DIANE MARY ,  COOK CAROLINE MARY ,  DOWLE MICHAEL DENNIS ,  EDLIN CHRISTOPHER DAVID ,  HAMBLIN JULIE NICOLE ,  JOHNSON MARTIN REDPATH ,  JONES PAUL SPENCER ,  KNOWLES RICHARD GRAHAM ,  LINDVALL MIKA KRISTIAN ,  MITCHELL CHARLOTTE JANE ,  REDGRAVE ALISON JUDITH ,  TRIVEDI NAIMISHA ,  WARD PETER

Inventor： ALLEN DAVID GEORGE ,  COE DIANE MARY ,  COOK CAROLINE MARY ,  DOWLE MICHAEL DENNIS ,  EDLIN CHRISTOPHER DAVID ,  HAMBLIN JULIE NICOLE ,  JOHNSON MARTIN REDPATH ,  JONES PAUL SPENCER ,  KNOWLES RICHARD GRAHAM ,  LINDVALL MIKA KRISTIAN ,  MITCHELL CHARLOTTE JANE ,  REDGRAVE ALISON JUDITH ,  TRIVEDI NAIMISHA ,  WARD PETER

IPC: A61K31/437 ,  A61P11/00 ,  A61P29/00 ,  C07D221/00 ,  C07D231/00 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: The invention relates to a compound of formula (I) or a salt thereof: wherein:R1 is C1-4alkyl, C1-3fluoroalkyl, -CH2CH2OH or -CH2CH2CO2C1-2alkyl;R2 is a hydrogen atom (H), methyl or C1fluoroalkyl;R3 is optionally substituted C3-8cycloalkyl or optionally substituted mono-unsaturated-C5-7cycloalkenyl or an optionally substituted heterocyclic group of sub-formula (aa), (bb) or (cc); in which n1 and n2 independently are 1 or 2; and in which Y is O, S, SO2, or NR10; or R3 is a bicyclic group (dd) or (ee): ; and wherein X is NR4R5 or OR5a. The compounds are phosphodiesterase (PDE) inhibitors, in particular PDE4 inhibitors. Also provided is the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment and/or prophylaxis of an inflammatory and/or allergic disease in a mammal such as a human, for example chronic obstructive pulmonary disease (COPD), asthma, or allergic rhinitis.

Abstract translation: 本发明涉及式（I）化合物或其盐：其中：R 1为C 1-4烷基，C 1-3氟烷基，-CH 2 CH 2 OH或-CH 2 CH 2 CO 2 C 1-2烷基; R 2为氢原子（H），甲基或C 1-3氟烷基; （aa），（bb）或（cc）的任选取代的C 3-8环烷基或任选取代的单不饱和-C 5-7环烯基或任选取代的杂环基; 其中n1和n2独立地为1或2; 并且其中Y是O，S，SO 2或NR 10; 或R3是双环基团（dd）或（ee）： 并且其中X是NR 4 R 5或OR 5 a。 这些化合物是磷酸二酯酶（PDE）抑制剂，特别是PDE4抑制剂。 还提供了式（I）化合物或其药学上可接受的盐在制备用于治疗和/或预防哺乳动物例如人的炎症和/或过敏性疾病的药物中的用途， 例如慢性阻塞性肺病（COPD），哮喘或过敏性鼻炎。