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1. 发明专利

CA2663161C QUINAZOLINONE AND ISOQUINOLINONE ACETAMIDE DERIVATIVES 未知
公开(公告)号：CA2663161C
公开(公告)日：2014-10-28
申请号：CA2663161
申请日：2007-09-10
申请人： ORGANON NV , PHARMACOPEIA L L C
发明人： LETOURNEAU JEFFREY , JOKIEL PATRICK , NAPIER SUSAN ELIZABETH , HO KOC-KAN , OHLMEYER MICHAEL , MCARTHUR DUNCAN ROBERT , JEREMIAH FIONA , RATCLIFFE PAUL DAVID , SCHULZ JURGEN
IPC分类号： C07D403/04 , A61K31/517 , A61K31/551 , A61P25/22 , A61P25/24 , C07D471/08
摘要： The present invention relates to a quinazolinone or isoquinolinone derivative of formula I, wherein R1 is C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-3alkyl, C2-6alkenyl, C2-6alkynyl, said C1-6alkyl, C3-6cycloalkyl and C3-6cycloalkylC1-3alkyl being optionally substituted with hydroxy, C1-6alkyloxy, cyano or one or more halogens; R2 is C6-10aryl optionally substituted with one to three substituents selected from halogen, hydroxy, cyano, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy and C3-6cycloalkyloxy, said C1-6alkyl, C3-6 cycloalkyl, C1-6 alkyloxy and C3-6Cycloalkyloxy being optionally substituted with one or more halogens; or R2 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, C1-6alkyloxy and halogen; or R2 is C4-7cycloalkyl; R3 is an optional substituent selected from C1-6alkyl, C1-6alkyloxy and halogen, said C1-6alkyl and C1-6alkyloxy being optionally substituted with one or more halogens; R4 is a group located at the 6- or 7- position of the quinazolinone or isoquinolinone ring having the formula Il, wherein R5 together with one of R6 forms a 4-8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroatomic moiety selected from O, S and NR9, said heterocyclic ring being optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo or R5 together with one of R7 and R8 forms a 6-8 membered heterocyclic ring optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo; Each R6 is independently H, halogen or C1-4alkyl optionally substituted with halogen or SO2CH3 or one of R6 together with R5 forms a 4-8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroatomic moiety selected from O, S and NR9, said heterocyclic ring being optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo; R7 and R8 are independently H, C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylc1-3alkyl, cyanoC1-3alkyl, C6-10aryl, C6-10arylC1-3alkyl, C1-3alkyloxyC1-3alkyl or C1-6acyl said C1-6alkyl, C3-6cycloalkyl and C3-6cycloalkylC1-3alkyl being optionally substituted with hydroxy, 1 or more halogens or diC1-2alkylamino; or R7 and R8 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 NR10, said heterocyclic ring being optionally substituted with one or two substituents selected from C1-6alkyl, halogen, hydroxy,

2. 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,

3. 发明专利

CA2666940A1 PURINES AS PKC-THETA INHIBITORS 未知
公开(公告)号：CA2666940A1
公开(公告)日：2008-05-02
申请号：CA2666940
申请日：2007-10-19
申请人： ORGANON NV , PHARMACOPEIA L L C
发明人： WIJKMANS JACOBUS CORNELIS HENRICUS MARIA , KINGSBURY CELIA , TEERHUIS NEELTJE MIRANDA , OHLMEYER MICHAEL , DILLER DAVID , HO KOC-KAN , CHAN JUI HSIANG , ROUGHTON ANDREW , LOMMERSE JOHANNES PETRUS MARIA , NEAGU IRINA
IPC分类号： C07D473/32 , A61K31/52 , A61P35/00
摘要： A chemical genus of purines, which are useful as PKC.theta. inhibitors, i s disclosed. The genus is represented by the formula (I); A representative e xample is: (II)

4. 发明专利

CA2663161A1 QUINAZOLINONE AND ISOQUINOLINONE ACETAMIDE DERIVATIVES 未知
公开(公告)号：CA2663161A1
公开(公告)日：2008-03-20
申请号：CA2663161
申请日：2007-09-10
申请人： ORGANON NV , PHARMACOPEIA L L C
发明人： LETOURNEAU JEFFREY , JOKIEL PATRICK , FIONA JEREMIAH , HO KOC-KAN , JURGEN SCHULZ , NAPIER SUSAN ELIZABETH , MCARTHUR DUNCAN ROBERT , OHLMEYER MICHAEL , RATCLIFFE PAUL DAVID
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 deriva tive of formula I, wherein R1 is C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylC1 -3alkyl, C2-6alkenyl, C2-6alkynyl, said C1-6alkyl, C3-6cycloalkyl and C3-6cy cloalkylC1-3alkyl being optionally substituted with hydroxy, C1-6alkyloxy, c yano or one or more halogens; R2 is C6-10aryl optionally substituted with on e to three substituents selected from halogen, hydroxy, cyano, C1-6alkyl, C3 -6cycloalkyl, C1-6alkyloxy and C3-6cycloalkyloxy, said C1-6alkyl, C3-6 cyclo alkyl, C1-6 alkyloxy and C3-6Cycloalkyloxy being optionally substituted with one or more halogens; or R2 is a 5-10 membered heteroaryl ring system compr ising a heteroatom selected from N, O and S and optionally substituted with a substituent selected from methyl, C1-6alkyloxy and halogen; or R2 is C4-7c ycloalkyl; R3 is an optional substituent selected from C1-6alkyl, C1-6alkylo xy and halogen, said C1-6alkyl and C1-6alkyloxy being optionally substituted with one or more halogens; R4 is a group located at the 6- or 7- position o f the quinazolinone or isoquinolinone ring having the formula Il, wherein R5 together with one of R6 forms a 4-8 membered saturated or unsaturated heter ocyclic ring optionally comprising a further heteroatomic moiety selected fr om O, S and NR9, said heterocyclic ring being optionally substituted with on e or two substituents selected from methyl, halogen, hydroxy and oxo or R5 t ogether with one of R7 and R8 forms a 6-8 membered heterocyclic ring optiona lly substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo; Each R6 is independently H, halogen or C1-4alkyl optionally substituted with halogen or SO2CH3 or one of R6 together with R5 forms a 4- 8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroatomic moiety selected from O, S and NR9, said heterocyclic ring being optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo; R7 and R8 are independently H, C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylc1-3alkyl, cyanoC1-3alkyl, C6-10aryl, C6-10ar ylC1-3alkyl, C1-3alkyloxyC1-3alkyl or C1-6acyl said C1-6alkyl, C3-6cycloalky l and C3-6cycloalkylC1-3alkyl being optionally substituted with hydroxy, 1 o r more halogens or diC1-2alkylamino; or R7 and R8 together with the nitrogen to which they are bonded form a 4-8 membered saturated or unsaturated heter ocyclic ring optionally comprising a further heteroatomic moiety selected fr om O, S and NR10, said heterocyclic ring being optionally substituted with o ne or two substituents selected from C1-6alkyl, halogen, hydroxy,

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.

6. 发明专利

CA2663193A1 2-(1-OXO-1H-ISOQUINOLIN-2-YL) ACETAMIDE DERIVATIVES 未知
公开(公告)号：CA2663193A1
公开(公告)日：2008-03-20
申请号：CA2663193
申请日：2007-09-10
申请人： PHARMACOPEIA L L C , ORGANON NV
发明人： RIVIELLO CHRISTOPHER MARK , NAPIER SUSAN ELIZABETH , OHLMEYER MICHAEL , NEAGU IRINA , CHAN JUI HSIANG , MORPHY JOHN RICHARD , HO KOC-KAN , JOKIEL PATRICK , LETOURNEAU JEFFREY
IPC分类号： C07D217/24 , A61K31/472
摘要： The present invention relates to a 2-(1-oxo-IH-isoquinolin-2-yl)acetamide derivative of formula (I).

7. 发明专利

AU2006255009B2 Azinone and diazinone V3 inhibitors for depression and stress disorders 未知
公开(公告)号：AU2006255009B2
公开(公告)日：2011-10-27
申请号：AU2006255009
申请日：2006-06-07
申请人： PHARMACOPEIA L L C
发明人： KOC-KAN HO , JOHN LETOURNEAU JEFFREY , PATRICK JOKIEL , MARK RIVIELLO CHRISTOPHER , OHLMEYER MICHAEL J
IPC分类号： C07D213/82 , A61K31/4412 , A61K31/50 , A61K31/505 , A61P25/24 , C07D239/30 , C07D239/36 , 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).

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