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11. 发明专利

AU2012204063A1 Aminopyrimidines as Syk inhibitors 未知
公开(公告)号：AU2012204063A1
公开(公告)日：2012-07-26
申请号：AU2012204063
申请日：2012-07-10
申请人： MERCK SHARP & DOHME , MERCK CANADA INC
发明人： ALTMAN MICHAEL D , ANDRESEN BRIAN M , ARRINGTON KENNETH L , CHILDERS KALEEN KONRAD , DI FRANCESCO MARIA EMILIA , DONOFRIO ANTHONY , ELLIS JOHN MICHAEL , FISCHER CHRISTIAN , GUERIN DAVID JOSEPH , HAIDLE ANDREW M , KATTAR SOLOMON , KNOWLES SANDRA LEE , LI CHAOMIN , LIM JONGWON , MACHACEK MICHELLE R , NORTHRUP ALAN B , O'BOYLE BRENDAN M , OTTE RYAN D , PETROCCHI ALESSIA , REUTERSHAN MICHAEL H , ROMEO ERIC , SIU TONY , TAOKA BRANDON M , TROTTER B WESLEY , ZHOU HUA , BURCH JASON , COTE BERNARD , DUPONT-GAUDET KRISTINA , FOURNIER JEAN-FRANCOIS , GAUTHIER JACQUES YVES , GUAY DANIEL , ROBICHAUD JOEL S , GRIMM JONATHAN , MADDESS MATTHEW L , SCHELL ADAM J , SPENCER KERRIE B , WOO HYUN CHONG , BHAT SATHESH
IPC分类号： C07D417/12 , A61K31/497 , A61P11/00 , A61P11/06 , A61P29/00 , A61P35/00 , C07D417/14
摘要： AMINOPYRIMIDINES AS SYK INHIBITORS Abstract The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis. (6458414_ ):KZA

12. 发明专利

CA2814703A1 HIV INTEGRASE INHIBITORS 未知
公开(公告)号：CA2814703A1
公开(公告)日：2012-05-03
申请号：CA2814703
申请日：2011-10-25
申请人： MERCK SHARP & DOHME , MERCK CANADA INC
发明人： BARBE GUILLAUME , POWELL DAVID A , HUMPHREY GUY ROLAND , KUETHE JEFFREY THOMAS , CHILDERS KARLA GLASER , FARAND JULIE , RADA VANESSA LOUISE , EMBREY MARK W , STEELE THOMAS G , SISKO JOHN T , BENNETT DAVID JONATHAN , RAHEEM IZZAT TIEDJE , SCHREIER JOHN DAVID , HARTINGH TIMOTHY JOHN , SHIPE WILLIAM D , BUNDA JAIME LYNN , NGUYEN NATALIE N M , BLOUIN MARC , GAREAU YVES , COTE BERNARD , TREPANIER VINCENT HECTOR EMILE , LARIVEE ALEXANDRE
IPC分类号： C07D471/14 , A61K31/4375 , A61P31/18
摘要： Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I), wherein R1A, R1B, R1C, R2A, R2B, R3A, R3B, R4, R5 and R6 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

13. 发明专利

CA2782889C AMINOPYRIMIDINES AS SYK INHIBITORS 未知
公开(公告)号：CA2782889C
公开(公告)日：2014-08-05
申请号：CA2782889
申请日：2010-12-15
申请人： MERCK CANADA INC , MERCK SHARP & DOHME
发明人： ALTMAN MICHAEL D , ANDRESEN BRIAN M , ARRINGTON KENNETH L , CHILDERS KALEEN KONRAD , DI FRANCESCO MARIA EMILIA , DONOFRIO ANTHONY , ELLIS JOHN MICHAEL , FISCHER CHRISTIAN , GUERIN DAVID JOSEPH , HAIDLE ANDREW M , KATTAR SOLOMON , KNOWLES SANDRA LEE , LI CHAOMIN , LIM JONGWON , MACHACEK MICHELLE R , NORTHRUP ALAN B , O'BOYLE BRENDAN M , OTTE RYAN D , PETROCCHI ALESSIA , REUTERSHAN MICHAEL H , ROMEO ERIC , SIU TONY , TAOKA BRANDON M , TROTTER B WESLEY , ZHOU HUA , GRIMM JONATHAN , MADDESS MATTHEW L , SCHELL ADAM J , SPENCER KERRIE B , WOO HYUN CHONG , ROBICHAUD JOEL S , BURCH JASON , COTE BERNARD , DUPONT-GAUDET KRISTINA , FOURNIER JEAN-FRANCOIS , GAUTHIER JACQUES YVES , GUAY DANIEL , BHAT SATHESH
IPC分类号： C07D417/12 , A61K31/497 , A61P11/00 , A61P11/06 , A61P29/00 , A61P35/00 , C07D417/14
摘要： The present invention provides novel pyrimidine amines of formula (Ib) which are potent inhibitors of spleen tyrosine kinase, and may be useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis. (see formula Ib)

14. 发明专利

TN2012000288A1 AMINOPYRIMIDINES AS SYK INHIBITORS 未知
公开(公告)号：TN2012000288A1
公开(公告)日：2013-12-12
申请号：TN2012000288
申请日：2012-06-05
申请人： MERCK SHARP & DOHME , MERCK CANADA INC
发明人： ALTMAN MICHAEL D , ANDRESSEN BRIAN M , ARRINGTON KENNETH L , CHILDERS KALEEN KONRAD , DI FRANCESCO MARIA EMILIA , DONOFRIO ANTHONY , ELLIS JOHN MICHAEL , FISCHER CHRISTIAN , GUERIN DAVID JOSEPH , HAIDLE ANDREW M , KATTAR SOLOMON , KNOWLES SANDRA LEE , LI CHAOMIN , LIM JONGWON , MACHACEK MICHELLE R , NORTHRUP ALAN B , O'BOYLE BRENDAN M , OTTE RYAN D , PETROCCHI ALESSIA , REUTERSHAN MICHAEL H , ROMEO ERIC , SIU TONY , TAOKA BRANDON M , TROTTER B WESLEY , ZHOU HUA , BURCH JASON , COTE BERNARD , DUPONT GAUDET KRISTINA , FORNIER JEAN-FRANCOIS , GAUTHIER JACQUES YVES , GUAY DANIEL , ROBICHAUD JOEL S
IPC分类号： A61K31/497 , A61P11/00 , A61P11/06 , A61P29/00 , A61P35/00 , C07D417/12 , C07D417/14
摘要： The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.

15. 发明专利

AU2010331927B2 Aminopyrimidines as Syk inhibitors 未知
公开(公告)号：AU2010331927B2
公开(公告)日：2013-10-10
申请号：AU2010331927
申请日：2010-12-15
申请人： MERCK CANADA INC , MERCK SHARP & DOHME
发明人： ALTMAN MICHAEL D , ANDRESEN BRIAN M , ARRINGTON KENNETH L , CHILDERS KALEEN KONRAD , DI FRANCESCO MARIA EMILIA , DONOFRIO ANTHONY , ELLIS JOHN MICHAEL , FISCHER CHRISTIAN , GUERIN DAVID JOSEPH , HAIDLE ANDREW M , KATTAR SOLOMON , KNOWLES SANDRA LEE , LI CHAOMIN , LIM JONGWON , MACHACEK MICHELLE R , NORTHRUP ALAN B , O'BOYLE BRENDAN M , OTTE RYAN D , PETROCCHI ALESSIA , REUTERSHAN MICHAEL H , ROMEO ERIC , SIU TONY , TAOKA BRANDON M , TROTTER B WESLEY , ZHOU HUA , BURCH JASON , COTE BERNARD , DUPONT-GAUDET KRISTINA , FOURNIER JEAN-FRANCOIS , GAUTHIER JACQUES YVES , GUAY DANIEL , ROBICHAUD JOEL S , GRIMM JONATHAN , MADDESS MATTHEW L , SCHELL ADAM J , SPENCER KERRIE B , WOO HYUN CHONG , BHAT SATHESH
IPC分类号： C07D417/12 , A61K31/497 , A61P11/00 , A61P11/06 , A61P29/00 , A61P35/00 , C07D417/14
摘要： The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.

17. 发明专利

AU2010331927A1 Aminopyrimidines as Syk inhibitors 未知
公开(公告)号：AU2010331927A1
公开(公告)日：2012-07-12
申请号：AU2010331927
申请日：2010-12-15
申请人： MERCK CANADA INC , MERCK SHARP & DOHME
发明人： ALTMAN MICHAEL D , ANDRESEN BRIAN M , ARRINGTON KENNETH L , CHILDERS KALEEN KONRAD , DI FRANCESCO MARIA EMILIA , DONOFRIO ANTHONY , ELLIS JOHN MICHAEL , FISCHER CHRISTIAN , GUERIN DAVID JOSEPH , HAIDLE ANDREW M , KATTAR SOLOMON , KNOWLES SANDRA LEE , LI CHAOMIN , LIM JONGWON , MACHACEK MICHELLE R , NORTHRUP ALAN B , O'BOYLE BRENDAN M , OTTE RYAN D , PETROCCHI ALESSIA , REUTERSHAN MICHAEL H , ROMEO ERIC , SIU TONY , TAOKA BRANDON M , TROTTER B WESLEY , ZHOU HUA , BURCH JASON , COTE BERNARD , DUPONT-GAUDET KRISTINA , FOURNIER JEAN-FRANCOIS , GAUTHIER JACQUES YVES , GUAY DANIEL , ROBICHAUD JOEL S , GRIMM JONATHAN , MADDESS MATTHEW L , SCHELL ADAM J , SPENCER KERRIE B , WOO HYUN CHONG , BHAT SATHESH
IPC分类号： C07D417/12 , A61K31/497 , A61P11/00 , A61P11/06 , A61P29/00 , A61P35/00 , C07D417/14
摘要： The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.

18. 发明专利

ES2609040T3 Aminopirimidinas como inhibidores de Syk 未知
公开(公告)号：ES2609040T3
公开(公告)日：2017-04-18
申请号：ES10801736
申请日：2010-12-15
申请人： MERCK SHARP & DOHME , MERCK CANADA INC
发明人： ALTMANN MICHAEL D , ANDRESEN BRIAN M , ARRINGTON KENNETH L , CHILDERS KALEEN KONRAD , DI FRANCESCO MARIA EMILIA , DONOFRIO ANTHONY , ELLIS JOHN MICHAEL , FISCHER CHRISTIAN , GUERIN DAVID JOSEPH , HAIDLE ANDREW M , KATTAR SOLOMON , KNOWLES SANDRA LEE , LI CHAOMIN , LIM JONGWON , MACHACEK MICHELLE , NORTHRUP ALAN B , O'BOYLE BRENDAN M , OTTE RYAN D , PETROCCHI ALESSIA , REUTERSHAN MICHAEL H , ROMEO ERIC , SIU TONY , TAOKA BRANDON M , TROTTER B WESLEY , ZHOU HUA , BURCH JASON , COTE BERNARD , DUPONT-GAUDET KRISTINA , FOURNIER JEAN-FRANCOIS , GAUTHIER JACQUES YVES , GUAY DANIEL , ROBICHAUD JOEL S , GRIMM JONATHAN , MADDESS MATTHEW L , SCHELL ADAM J , SPENCER KERRIE B , WOO HYUN CHONG , BHAT SATHESH
IPC分类号： C07D417/12 , A61K31/497 , A61P11/00 , A61P11/06 , A61P29/00 , A61P35/00 , C07D417/14
摘要： Un compuesto de formula (I) o una sal farmaceuticamente aceptable del mismo:**Fórmula** en la que p es de 0 a 4; q es 0, 1 o 2; Cy se selecciona entre cicloalquilo C4-7, oxetanilo, pirrolidinilo, piperidinilo y azepanilo; R1 se selecciona entre H, alquilo C1-4, haloalquilo C1-4, cicloalquilo C3-6 y Oalquilo C1-4; R4 se selecciona entre H, alquilo C1-4 y cicloalquilo C3-4; Ry(a) es aminometilo, OH, OCH3, OCH2CH2OH, F, CN, CO2Ra(a), CONRb(a)Rc(a), NRa(a)Ra(a), NHC(O)alquilo C1-3 (opcionalmente sustituido con OH), NHC(O)NH2, NHSO2NH2, NHSO2alquilo C1-3 o NHSO2haloalquilo C1-3; Rz(a) se selecciona entre (A) alquilo C1-4 opcionalmente sustituido con uno a tres grupos seleccionados independientemente entre OH, NH2, CN, CO2Ra(a) y CONH2, (B) fluoroalquilo C1-3, (C) halogeno, (D) CN, (E) COalquilo C1-4 (opcionalmente sustituido con uno o dos grupos seleccionados independientemente entre ORa(a), CN, CO2Ra(a), CONRa(a)Ra(a) y NRa(a)Ra(a)), (F) CO-fenilo (opcionalmente sustituido con uno o dos grupos seleccionados independientemente entre etinilo, CO2Ra(a), CN, F y OH), (G) CO-cicloalquilo C3-6 (opcionalmente sustituido con OH o CO2Ra(a)), (H) alquil C0-3-CO2Ra(a), (I) -C(O)NRb(a)Rc(a), (J) -ORa(a), (K) -OC(O)Ra(a), (L) -NRb(a)Rc(a), (M) -NHC(O)alquilo C1-4 (opcionalmente sustituido con uno a tres OH o un CONRa(a)Ra(a)), (N) -NHSO2alquilo C1-3, (O) -NHSO2NH2, (P) oxo, (Q) 1,3,4-oxadiazol-2(3H)-ona, (R) 1,2,4-oxadiazol-5(4H)-ona, (S) SO2NH2, (T) SO2alquilo C1-3, (U) SO2haloalquilo C1-3 y (V) SO2Ph; Ra(a) es H o alquilo C1-4; Rb(a) y Rc(a) se seleccionan independientemente entre (A) H, (B) cicloalquilo C3-6 opcionalmente sustituido con OH, (C) heteroarilo seleccionado entre imidazolilo, piridilo e indolilo, (D) tetrahidrofuranilo, (E) bencilo, (F) fenilo opcionalmente sustituido con uno o dos grupos seleccionados independientemente entre (CH2)0-2OH y F, (G1) alquilo C1-4 y (G2) haloalquilo C1-4, en donde (G1) y (G2) estan cada uno opcionalmente sustituido con uno a tres grupos seleccionados independientemente entre (i) OH, (ii) cicloalquilo C3-6 opcionalmente sustituido con uno o dos grupos seleccionados independientemente entre alquilo C1-4, CONH2, CO2H y CH2OH, (iii) CONH2, (iv) SO2NH2, (v) SO2alquilo C1-4, (vi) heterociclilo monociclico de 4 a 7 miembros opcionalmente sustituido con uno o dos grupos seleccionados independientemente entre oxo, (CH2)0-2OH y alquilo C1-4, (vii) un heteroarilo de 5 o 6 miembros opcionalmente sustituido con uno o dos grupos seleccionados independientemente entre carboxi, (CH2)0-2OH y alquilo C1-4, (viii) CN, (ix) Oalquilo C1-4, (x) CO2H, (xi) NRa(a)C(O)alquilo C1-4, (xii) fenilo opcionalmente sustituido con uno o dos grupos seleccionados independientemente entre (CH2)0-2OH, SO2NH2, CF3, F y Cl, (xiii) 1-pirrolidinilo opcionalmente sustituido con oxo, (xiv) 1-imidazolidinilo opcionalmente sustituido con oxo, (xv) 1-piperidinilo opcionalmente sustituido con oxo y (xvi) 4-morfolinilo; o Rb(a) y Rc(a) junto con el atomo de nitrogeno al que estan unidos forman un heterociclo de 6 o 7 miembros que tiene de 0 a 1 heteroatomo adicional seleccionado entre N, O y S, en donde dicho heterociclo esta opcionalmente sustituido con uno o dos grupos seleccionados independientemente entre oxo, CN, (CH2)0-2OH, acetilo, bencilo, SO2alquilo C1-4, CONH2, metoximetilo, carboximetilo, CO2Ra(a) y alquilo C1-4.

19. 发明专利

AU2014200138B8 Aminopyrimidines as Syk inhibitors 未知
公开(公告)号：AU2014200138B8
公开(公告)日：2015-10-29
申请号：AU2014200138
申请日：2014-01-10
申请人： MERCK CANADA INC , MERCK SHARP & DOHME
发明人： ALTMAN MICHAEL D , ANDRESEN BRIAN M , ARRINGTON KENNETH L , CHILDERS KALEEN KONRAD , FRANCESCO MARIA EMILIA DI , DONOFRIO ANTHONY , ELLIS JOHN MICHAEL , FISCHER CHRISTIAN , GUERIN DAVID JOSEPH , HAIDLE ANDREW M , KATTAR SOLOMON , KNOWLES SANDRA LEE , LI CHAOMIN , LIM JONGWON , MACHACEK MICHELLE R , NORTHRUP ALAN B , O'BOYLE BRENDAN M , OTTE RYAN D , PETROCCHI ALESSIA , REUTERSHAN MICHAEL H , ROMEO ERIC , SIU TONY , TAOKA BRANDON M , TROTTER B WESLEY , ZHOU HUA , BURCH JASON , COTE BERNARD , DUPONT-GAUDET KRISTINA , FOURNIER JEAN-FRANCOIS , GAUTHIER JACQUES YVES , GUAY DANIEL , ROBICHAUD JOEL S , GRIMM JONATHAN , MADDESS MATTHEW L , SCHELL ADAM J , SPENCER KERRIE B , WOO HYUN CHONG , BHAT SATHESH
摘要： AMINOPYRIMIDINES AS SYK INHIBITORS Abstract The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.

20. 发明专利

DOP2012000166A AMINOPIRIMIDINAS COMO INHIBIDORES DE SYK 未知
公开(公告)号：DOP2012000166A
公开(公告)日：2012-09-30
申请号：DO2012000166
申请日：2012-06-15
申请人： MERCK SHARP & DOHME , MERCK CANADA INC
发明人： MACHACEK MICHELLE R , GAUTHIER JACQUES YVES , NORTHRUP ALAN B , PETROCCHI ALESSIA , COTE BERNARD , ALTMAN MICHAEL D , ANDRESEN BRIAN M , ARRINGTON KENNETH L , CHILDERS KALEEN KONRAD , DI FRANCESCO MARIA EMILIA , DONOFRIO ANTHONY , ELLIS JOHN MICHAEL , FISCHER CHRISTIAN , GUERIN DAVID JOSEPH , HAIDLE ANDREW M , KATTAR SOLOMON , KNOWLES SANDRA LEE , LI CHAOMIN , LIM JONGWON , BOYLE BRENDAN M O , OTTE RYAN D , REUTERSHAN MICHAEL H , ROMEO ERIC , SIU TONY , TAOKA BRANDON M , WESLEY TROTTER B , ZHOU HUA , BURCH JASON , DUPONT-GAUDET KRISTINA , FOURNIER JEAN-FRANCOIS , GUAY DANIEL , ROBICHAUD JOEL S
摘要： La presente invención proporciona nuevas pirimidina aminas de fórmula (I) que son potentes inhibidores de la tirosina quinasa del bazo, y son útiles en la fabricación de medicamentos útiles en cl tratamiento y prevcnción de enfermedades mediadas por dicha enzima, tales como asma, COPD y artritis reumatoide.

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