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1. 发明专利

AU2007296634B2 Quinazolinone and isoquinolinone acetamide derivatives 未知
公开(公告)号：AU2007296634B2
公开(公告)日：2012-09-20
申请号：AU2007296634
申请日：2007-09-10
申请人： MERCK SHARP & DOHME , PHARMACOPEIA L L C
发明人： JEREMIAH FIONA , OHLMEYER MICHAEL , NAPIER SUSAN ELIZABETH , JURGEN SCHULZ , JOKIEL PATRICK , RATCLIFFE PAUL DAVID , LETOURNEAU JEFFREY , HO KOC-KAN , MCARTHUR DUNCAN ROBERT
IPC分类号： C07D239/70 , A61K31/472 , A61K31/4725 , A61K31/496 , A61K31/519 , A61K31/5513 , A61P25/24 , C07D217/24 , C07D243/08
摘要： The present invention relates to a quinazolinone or isoquinolinone derivative of formula I, wherein R is Calkyl, Ccycloalkyl, CcycloalkylCalkyl, Calkenyl, Calkynyl, said Calkyl, Ccycloalkyl and CcycloalkylCalkyl being optionally substituted with hydroxy, Calkyloxy, cyano or one or more halogens; R is Caryl optionally substituted with one to three substituents selected from halogen, hydroxy, cyano, Calkyl, Ccycloalkyl, Calkyloxy and Ccycloalkyloxy, said Calkyl, C cycloalkyl, C alkyloxy and CCycloalkyloxy being optionally substituted with one or more halogens; or R 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, Calkyloxy and halogen; or R is Ccycloalkyl; R is an optional substituent selected from Calkyl, Calkyloxy and halogen, said Calkyl and Calkyloxy being optionally substituted with one or more halogens; R is a group located at the 6- or 7- position of the quinazolinone or isoquinolinone ring having the formula Il, wherein R together with one of R forms a 4-8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroatomic moiety selected from O, S and NR, said heterocyclic ring being optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo or R together with one of R and R forms a 6-8 membered heterocyclic ring optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo; Each R is independently H, halogen or Calkyl optionally substituted with halogen or SOCH or one of R together with R forms a 4-8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroatomic moiety selected from O, S and NR, said heterocyclic ring being optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo; R and R are independently H, Calkyl, Ccycloalkyl, Ccycloalkylcalkyl, cyanoCalkyl, Caryl, CarylCalkyl, CalkyloxyCalkyl or Cacyl said Calkyl, Ccycloalkyl and CcycloalkylCalkyl being optionally substituted with hydroxy, 1 or more halogens or diCalkylamino; or R and R 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, said heterocyclic ring being optionally substituted with one or two substituents selected from Calkyl, halogen, hydroxy,

2. 发明专利

AU2009285823B8 1-(4-ureidobenzoyl)piperazine derivatives 未知
公开(公告)号：AU2009285823B8
公开(公告)日：2014-08-21
申请号：AU2009285823
申请日：2009-08-26
申请人： MERCK SHARP & DOHME , PHARMACOPEIA LLC
发明人： COOKE ANDREW JOHN , BENNETT DAVID JONATHAN , EDWARDS ANDREW STANLEY , ROUGHTON ANDREW LAIRD , NEAGU IRINA , CHAN JUI-HSIANG , HO KOC-KAN , ANSARI NASRIN , MORRIS MICHELLE LEE , RONG YAJING , OHLMEYER MICHAEL

3. 发明专利

AU2009235409A1 Pyrrolo[2,3-d]pyrimidin-2-yl-amine derivates as PKC-theta inhibitors 未知
公开(公告)号：AU2009235409A1
公开(公告)日：2009-10-15
申请号：AU2009235409
申请日：2009-04-08
申请人： MERCK SHARP & DOHME , PHARMACOPEIA LLC
发明人： WIJKMANS JACOBUS CORNELIS HENRICUS MARIA , LOMMERSE JOHANNES PETRUS MARIA , DILLER DAVID , NEAGU IRINA , PLATE RALF , ROUGHTON ANDREW LAIRD , HO KOC-KAN , OHLMEYER MICHAEL , CHAN JUI-HSIANG , KINGSBURY CELIA , TEERHUIS NEELTJE MIRANDA
IPC分类号： C07D487/04 , A61K31/519
摘要： The present invention relates to a pyrrolo[2,3-d]pyrimidin-2-yl-amine derivative according to formula (I) wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said pyrrolo[2,3-d]pyrimidine-2-ylamine derivatives and to their use in therapy, for instance in the treatment of PKC&thetas; mediated disorders.

4. 发明专利

AU2009285823B2 1-(4-ureidobenzoyl)piperazine derivatives 未知
公开(公告)号：AU2009285823B2
公开(公告)日：2014-04-17
申请号：AU2009285823
申请日：2009-08-26
申请人： MERCK SHARP & DOHME
发明人： COOKE ANDREW JOHN , BENNETT DAVID JONATHAN , EDWARDS ANDREW STANLEY , ROUGHTON ANDREW LAIRD , NEAGU IRINA , CHAN JUI-HSIANG , HO KOC-KAN , ANSARI NASRIN , MORRIS MICHELLE LEE , RONG YAJING , OHLMEYER MICHAEL
IPC分类号： C07D213/56 , A61K31/496 , A61P9/10 , C07D263/34 , C07D307/68 , C07D333/38
摘要： The present invention relates to 1-(4-ureidobenzoyl)piperazine derivatives having the general Formula I (We bring to your attention that formula I is not provided on this electronic version as it is provided in the abstract of the paper copy) Wherein R

5. 发明专利

AU2006328550B2 Compounds with medicinal effects due to interaction with the glucocorticoid receptor 未知
公开(公告)号：AU2006328550B2
公开(公告)日：2012-04-12
申请号：AU2006328550
申请日：2006-12-18
申请人： MERCK SHARP & DOHME , PHARMACOPEIA L L C
发明人： BROWN ANGUS RICHARD , LITTLEWOOD PETER THOMAS ALBERT , HAMILTON NIALL MORTON , HO KOC-KAN , SHERBORNE BRAD , OHLMEYER MICHAEL , KICZUN MICHAEL JOHN , KULTGEN STEVEN G , MORPHY JOHN RICHARD , KINGSBURY CELIA , GROVE SIMON JAMES ANTHONY
IPC分类号： C07C311/17 , A61K31/18 , A61K31/4439 , C07D401/12
摘要： The invention provides for compounds having the structure according to the formula I wherein: X is a carbon or nitrogen atom; Ar is phenyl or heteroaromatic ring; R is hydrogen, halogen, CN or (1 C-4C)alkyl; R is hydrogen, halogen or optionally fluorinated (1 C-3C)alkoxy; R and R are independently hydrogen, optionally halogenated (1C- 4C)alkyl, optionally halogenated (1 C-4C)alkoxy, optionally halogenated aryl(1C-4C)alkoxy, optionally halogenated (1 C-4C)alkenyl or hydroxylmethyl; R is hydrogen, halogen, optionally halogenated (1 C-4C)alkoxy or optionally halogenated aryl(1 C-4C)alkoxy; R is hydrogen, benzyl, optionally substituted with one or more halogens or (1 C-4C)alkyl, or R is optionally halogenated (1 C-4C)alkyl; each R independently is hydrogen, halogen, optionally halogenated (1 C-4C)alkyl or optionally halogenated (1 C-4C)alkoxy and pharmaceutically suitable acid addition salts thereof for use as glucocorticoid receptor modulators, in particular for treatment of central nervous system disorders.

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