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61. 发明专利

NO20031190L 未知
公开(公告)号：NO20031190L
公开(公告)日：2003-05-13
申请号：NO20031190
申请日：2003-03-14
申请人： VERTEX PHARMA
发明人： DAVIES ROBERT , BEBBINGTON DAVID , BINCH HALEY , KNEGTEL RONALD , GOLEC JULIAN M C , PATEL SANJAY , CHARRIER JEAN-DAMIEN , KAY DAVID
IPC分类号： C07D403/12 , A61K31/415 , A61K31/437 , A61K31/4709 , A61K31/4725 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/53 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/00 , A61P1/16 , A61P3/08 , A61P3/10 , A61P3/14 , A61P5/00 , A61P9/00 , A61P9/10 , A61P11/06 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P25/18 , A61P25/28 , A61P29/00 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D239/26 , C07D239/36 , C07D239/70 , C07D239/88 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D475/10 , C07D487/04 , C07D491/04 , C07D491/044 , C07D491/048 , C07D491/052 , C07D491/107 , C07D491/113 , C07D491/20 , C07D493/04 , C07D495/04 , C07D498/04 , C07D513/04 , C07D521/00 , A61K31/4155
摘要： This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from -R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; R1, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3 and Aurora, for treating diseases such as diabetes, cancer, and Alzheimer's disease.

62. 发明专利

NO20031189L 未知
公开(公告)号：NO20031189L
公开(公告)日：2003-05-13
申请号：NO20031189
申请日：2003-03-14
申请人： VERTEX PHARMA
发明人： BEBBINGTON DAVID , BINCH HALEY , KNEGTEL RONALD , GOLEC JULIAN M C , PATEL SANJAY , CHARRIER JEAN-DAMIEN , KAY DAVID , DAVIES ROBERT , LI PAN , WANNAMAKER MARION W , FORSTER CORNELIA , PIERCE ALBERT
IPC分类号： C07D403/12 , A61K31/415 , A61K31/437 , A61K31/4709 , A61K31/4725 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/53 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/00 , A61P1/16 , A61P3/08 , A61P3/10 , A61P3/14 , A61P5/00 , A61P9/00 , A61P9/10 , A61P11/06 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P25/18 , A61P25/28 , A61P29/00 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D239/26 , C07D239/36 , C07D239/70 , C07D239/88 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D475/10 , C07D487/04 , C07D491/04 , C07D491/044 , C07D491/048 , C07D491/052 , C07D491/107 , C07D491/113 , C07D491/20 , C07D493/04 , C07D495/04 , C07D498/04 , C07D513/04 , C07D521/00 , A61K31/4155
摘要： This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from -R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; R1, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3 and Aurora, for treating diseases such as diabetes, cancer, and Alzheimer's disease.

63. 发明专利

NO20031188L 未知
公开(公告)号：NO20031188L
公开(公告)日：2003-05-13
申请号：NO20031188
申请日：2003-03-14
申请人： VERTEX PHARMA
发明人： BEBBINGTON DAVID , KNEGTEL RONALD , GOLEC JULIAN M C , LI PAN , DAVIES ROBERT , CHARRIER JEAN-DAMIEN
IPC分类号： C07D403/12 , A61K31/415 , A61K31/437 , A61K31/4709 , A61K31/4725 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/53 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/00 , A61P1/16 , A61P3/08 , A61P3/10 , A61P3/14 , A61P5/00 , A61P9/00 , A61P9/10 , A61P11/06 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P25/18 , A61P25/28 , A61P29/00 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D239/26 , C07D239/36 , C07D239/70 , C07D239/88 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D475/10 , C07D487/04 , C07D491/04 , C07D491/044 , C07D491/048 , C07D491/052 , C07D491/107 , C07D491/113 , C07D491/20 , C07D493/04 , C07D495/04 , C07D498/04 , C07D513/04 , C07D521/00
摘要： This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from -R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; R1, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3 and Aurora, for treating diseases such as diabetes, cancer, and Alzheimer's disease.

64. 发明专利

CA2450769A1 5-(2-AMINOPYRIMIDIN-4-YL) BENZISOXAZOLES AS PROTEIN KINASE INHIBITORS 未知
公开(公告)号：CA2450769A1
公开(公告)日：2002-12-27
申请号：CA2450769
申请日：2002-06-14
申请人： VERTEX PHARMA
发明人： MOON YOUNG CHOON , CHOQUETTE DEB , DAVIES ROBERT , GREEN JEREMY , PIERCE ALBERT , LEDEBOER MARK
IPC分类号： A61K31/506 , A61K31/5377 , A61K31/551 , A61K31/635 , A61L27/00 , A61P1/16 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/06 , A61P19/02 , A61P25/00 , A61P25/02 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/28 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D413/04 , C07D413/14 , C07D401/14 , C07D409/14 , A61K31/505
摘要： Described herein are benzisoxazole compounds of formula I or a pharmaceutically acceptable derivative or prodrug thereof, wherein A-B is N- O or O-N; Ar is an optionally substituted C5-10 aryl group; R1 is hydrogen or an optionally substituted group selected from C1-I0 aliphatic, C5-10 aryl, C6-1 2 aralkyl, C3-10 heterocyclyl, or C4-12 heterocyclylalkyl; and T, n, R2 and R3 are as described in the specification. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK-3 and JAK mammalian protein kinases. The invention also provides pharmaceutically acceptable composition s comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various -, protein kinase mediated disorders.

65. 发明专利

AU3404702A Pyrazole compounds useful as protein kinase inhibitors 未知
公开(公告)号：AU3404702A
公开(公告)日：2002-07-01
申请号：AU3404702
申请日：2001-12-19
申请人： VERTEX PHARMA
发明人： BEBBINGTON DAVID , CHARRIER JEAN-DAMIEN , DAVIES ROBERT , EVERITT SIMON , KAY DAVID , KNEGTEL RONALD , PATEL SANJAY
IPC分类号： C12N9/99 , A61K20060101 , A61K31/435 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/513 , A61K31/517 , A61K31/519 , A61K31/53 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/00 , A61P20060101 , A61P1/00 , A61P3/08 , A61P3/10 , A61P3/14 , A61P5/00 , A61P5/18 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P11/06 , A61P13/12 , A61P15/00 , A61P17/06 , A61P17/14 , A61P19/02 , A61P19/08 , A61P19/10 , A61P21/00 , A61P21/02 , A61P21/04 , A61P25/00 , A61P25/02 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/28 , A61P29/00 , A61P31/12 , A61P31/18 , A61P31/20 , A61P31/22 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D20060101 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D487/04 , C07D491/04 , C07D493/04 , C07D495/04 , C07D498/04 , C07D513/04 , C07D521/00
摘要： This invention describes novel pyrazole compounds of formula (I), wherein R 1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; R x , R y , R 2 , and R 2' are as described in the specification, and processes for preparing these compounds. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

66. 发明专利

PE20020451A1 COMPUESTOS DE PIRAZOL UTILES COMO INHIBIDORES DE CINASA PROTEINA 未知
公开(公告)号：PE20020451A1
公开(公告)日：2002-06-06
申请号：PE2001000931
申请日：2001-09-14
申请人： VERTEX PHARMA
发明人： DAVIES ROBERT , BEBBINGTON DAVID , KNEGTEL RONALD , WANNAMAKER MARION , LI PAN , FORSTER CORNELIA J , LAUFFER DAVID , PIERCE ALBERT , KAY DAVID
IPC分类号： C07D403/12 , A61K31/415 , A61K31/4155 , A61K31/437 , A61K31/4427 , A61K31/4709 , A61K31/4725 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/53 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/00 , A61P1/16 , A61P3/08 , A61P3/10 , A61P3/14 , A61P5/00 , A61P9/00 , A61P9/10 , A61P11/06 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P25/18 , A61P25/28 , A61P29/00 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D239/26 , C07D239/36 , C07D239/70 , C07D239/88 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D475/10 , C07D487/04 , C07D491/04 , C07D491/044 , C07D491/048 , C07D491/052 , C07D491/107 , C07D491/113 , C07D491/20 , C07D493/04 , C07D495/04 , C07D498/04 , C07D513/04 , C07D521/00
摘要： SE REFIERE A COMPUESTOS DE PIRAZOL DE FORMULA I DONDE EL ANILO C ES FENILO, PIRIDINILO, PIRIMIDINILO, PIRIDAZINILO, PIRAZINILO, 1,2,4-TRIAZINILO SUSTITUIDO EN LA POSICION ORTO POR HALO, CN, NO2, T-V-R6, FENILO, HETEROARILO, HETEROCICLO, UN GRUPO ALIFATICO C1-C6; EN LA POSICION DIFERENTE DE ORTO ES SUSTITUIDO POR R5; R1 Y R2 SON R, R-W-R6, ANILLO DE 5-8 MIEMBROS SUSTITUIDO CON HALO, OXO, CN, NO2R7, VR6; Rx Y Ry SON T-R3, ANILLO FUSIONADO SUSTITUIDO CON T-R3, OXO, R4; T ES ENLACE, ALQUILIDENO, C1-C4; R3 ES R, HALO, OR, COR, N(R4)2, CON(R7)2, ENTRE OTROS; R ES H, ARILO C6-C10, HETEROARILO C5-C10, HETEROCICLO 5-10 MIEMBROS; R4 ES R7, CON(R7)2, SO2R7; R7 ES H, GRUPO ALIFATICO, DOS R7 FORMAN HETEROARILO, HETEROCICLO; R5 ES R, HALO, OR, NR4COR, COCOR, ENTRE OTROS; V ES O, S, SO, SO2, NR6SO2, SO2NR6, CONR6, ENTRE OTROS; R6 ES H, GRUPO ALIFATICO C1-C4, DOS R6 FORMAN HETEROARILO, HETEROCICLO; W ES C(R6)2O, C(R6)2S, CO2, CONR6. TAMBIEN SE REFIERE A COMPUESTOS DE FORMULA A, B, ENTRE OTROS; R10 ES F, Br, HALOALQUILO C1-C6, NITRO, 1-PIRROLO; R1 ES Cl, F, CF3, CN, NO2; LOS COMPUESTOS SON INHIBIDORES DE LA ACTIVIDAD DE CINASAS GLICOGENO SINTASA GSK-3; SERINA TREONINA AURORA-2, AUMENTAN LA SINTESIS DE GLICOGENO, DISMINUYEN NIVEL SANGUINEO DE GLUCOSA, INHIBEN LA PRODUCCION DE PROTEINA TAU HIPERFOSFORILADA, INHIBEN LA FOSFORILACION DE ß-CATEINA Y PUEDEN SER UTILES PARA EL TRATAMIENTO DE DIABETES, ALZHEIMER, ESQUIZOFRENIA, CANCER

67. 发明专利

AP2002002406A0 Prodrug of an ice inhibitor. 未知
公开(公告)号：AP2002002406A0
公开(公告)日：2002-03-31
申请号：AP2002002406
申请日：2001-05-18
申请人： VERTEX PHARMA
发明人： WANNAMAKER MARION WOODS , DAVIES ROBERT
IPC分类号： A61K38/00 , A61P1/02 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/04 , A61P3/10 , A61P5/14 , A61P7/04 , A61P7/06 , A61P9/04 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/06 , A61P17/14 , A61P19/00 , A61P19/02 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/02 , A61P37/06 , A61P43/00 , C07D477/02 , C07D477/20 , C07K5/02 , C07K5/06
摘要： This invention described an ice inhibitor prodrug (i)having good bioavaialability. Compound of formula (i)is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ trnasplant rejection, osteoarthritis, asthama, psoriasis, alzheimer's disese, mycardial infarction, congestive heart failure, huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.

68. 发明专利

CA2422379A1 PYRAZOLE COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS 未知
公开(公告)号：CA2422379A1
公开(公告)日：2002-03-21
申请号：CA2422379
申请日：2001-09-14
申请人： VERTEX PHARMA
发明人： KNEGTEL RONALD , WANNAMAKER MARION , FORESTER CORNELIA , LI PAN , BEBBINGTON DAVID , KAY DAVID , DAVIES ROBERT , PIERCE ALBERT
IPC分类号： C07D403/12 , A61K31/415 , A61K31/437 , A61K31/4709 , A61K31/4725 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/53 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/00 , A61P1/16 , A61P3/08 , A61P3/10 , A61P3/14 , A61P5/00 , A61P9/00 , A61P9/10 , A61P11/06 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P25/18 , A61P25/28 , A61P29/00 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D239/26 , C07D239/36 , C07D239/70 , C07D239/88 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D475/10 , C07D487/04 , C07D491/04 , C07D491/044 , C07D491/048 , C07D491/052 , C07D491/107 , C07D491/113 , C07D491/20 , C07D493/04 , C07D495/04 , C07D498/04 , C07D513/04 , C07D521/00 , A61K31/4155
摘要： This invention describes novel pyrazole compounds of formula II:wherein Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, o r 1, 2, 4-triazinyl ring, and R2, R2, Rx, and Ry are as described in the specification. Ring C has an ortho substituent and is optionally substituted in the non-ortho positions. R2 and R2 are optionally taken together with the ir intervening atoms to form a fused ring system, such as an indazole ring; and Rx and Ry are optionally taken together with their intervening atoms to form a fused ring system, such as a quinazoline ring. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3, for treating diseases such as diabetes and Alzheimer's disease.

69. 发明专利

AU6477001A Prodrug of an ice inhibitor 未知
公开(公告)号：AU6477001A
公开(公告)日：2001-12-03
申请号：AU6477001
申请日：2001-05-18
申请人： VERTEX PHARMA
发明人： WANNAMAKER MARION , DAVIES ROBERT
IPC分类号： A61K38/00 , A61P1/02 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/04 , A61P3/10 , A61P5/14 , A61P7/04 , A61P7/06 , A61P9/04 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/06 , A61P17/14 , A61P19/00 , A61P19/02 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/02 , A61P37/06 , A61P43/00 , C07D477/02 , C07D477/20 , C07K5/02 , C07K5/06
摘要： This invention described an ICE inhibitor prodrug (I) having good bioavailability. Compound of formula (I) is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.

70. 发明专利

ES2655391T3 Inhibidores isoindolinona de fosfatidilinositol 3-quinasa 未知
公开(公告)号：ES2655391T3
公开(公告)日：2018-02-19
申请号：ES10805555
申请日：2010-12-21
申请人： VERTEX PHARMA
发明人： ARONOV ALEX , COME JON , DAVIES ROBERT , PIERCE ALBERT , WANG JIAN , NANTHAKUMAR SUGANTHINI , CAO JINGRONG , BANDARAGE UPUL , KRUEGER ELAINE , TIRAN AMAUD , LIAO YUSHENG , MESSERSMITH DAVID , COLLIER PHILIP , GREY RONALD , ODOWD HARDWIN , HENDERSON JAMES , GRILLOT ANNE LAURE
IPC分类号： C07D401/04 , A61K31/352 , A61K31/424 , A61K31/429 , A61P9/00 , A61P29/00 , A61P37/00 , C07D401/14 , C07D405/14 , C07D417/14 , C07D471/04 , C07D471/20 , C07D491/20
摘要： Compuesto que presenta la fórmula: **(Ver fórmula)** o una sal farmacéuticamente aceptable del mismo, en la que: X1 es N, X2 es N, CH o C-CH3, R1 es un pirazol-4-ilo sustituido opcionalmente con 1 o 2 apariciones de R1a, R1a es cloro, flúor, alifático C1-8, -(CH2)0-2cicloalifático C3-6, -(CH2)0-2-heterocíclico de 5 a 6 elementos que presenta hasta dos heteroátomos seleccionados de entre nitrógeno, oxígeno o azufre, -CN, -C(O)-alifático C1-4, -C(O)NH(alifático C1-4), -C(O)N(alifático C1-4)2, -C(O)O-alifático C1-4, -S(O)2NH(alifático C1-4), - S(O)2N(alifático C1-4)2 o -S(O)2-alifático C 1-4, en los que hasta 3 átomos de carbono no contiguos de dicho alifático o cicloalifático de R1a pueden sustituirse por -O-, -S- o -N(R1b)- y en los que cada uno de dicho alifático, cicloalifático o heterocíclico de R1a se sustituye opcional e independientemente con hasta 4 apariciones de JR, cada JR es independientemente flúor, oxo, -(CH2)0-2CN, -(CH2)0-2CF3 -C(O)R1b, -C(O)N(R1b)2, -C(O)O(R1b), -N(R1b)2, -N(R1b)C(O)R1b, -(CH2)0-2OR1b, fenilo o un heteroarilo de 5 a 6 elementos, heterociclo de 4 a 6 elementos o heteroarilo o heterociclilo bicíclico fusionado de 9 a 11 elementos, presentando cada uno de dichos anillos heteroarilo o heterociclilo que presentan hasta 3 átomos seleccionados de entre nitrógeno, oxígeno o azufre, en el que cada uno de dichos grupos cicloalifático, fenilo, heteroarilo o heterociclilo se sustituyen opcionalmente con hasta 2 R1c, cada R1b se selecciona, independientemente de entre hidrógeno, alifático C1-8, -(CH2)0-1cicloalifático C3-6, -(CH2)0-1heterocíclico C4-6 que presenta hasta dos heteroátomos seleccionados de entre N o O, o dos R1b junto con el átomo al que se encuentran unidos forman un anillo heterocíclico de 5 a 6 elementos, en el que cada grupo alifático, cicloalifático o heterocíclico se sustituye opcionalmente con hasta tres átomos de F o hasta dos grupos -OH, -alquilo C1-2 o -O-alquilo C1-2, cada R1c es, independientemente, flúor, cloro, alifático C1-4, -(CH2)0-2OH, -CN, -C(O)-alifático C1-4 o -C(O)O-alifático C1-4, R2 es hidrógeno, F, Cl, CF3, alifático C1-2, cicloalifático C3-4, -N(CH3)2, -N(CH2)3,-OCF3, -OCHF2 o -O-alifático C1-2, R3 es hidrógeno, alifático C1-6, cicloalifático C3-6, heterocíclico C4-7 que presenta 1 o 2 átomos seleccionados de entre N o O, -(CH2)0-1CF3, -OH, -O-alifático C1-6, -O-cicloalifático C3-6, -O-heterociclilo C3-6 que presenta un átomo de oxígeno, -O(CH2)2O-alifático C1-2 o -O-alquilo C1-2-C(O)O-alifático C1-3 o bencilo, y R4 es hidrógeno o alquilo C1-6, en el que por lo menos uno de entre R3 y R4 no es hidrógeno, o R3 y R4 junto con el carbono al que se encuentran unidos forman un anillo cicloalifático de 3 a 6 elementos, un anillo heterocíclico de 3 a 6 elementos que presenta hasta dos átomos seleccionados de entre N o O, o un alquenilo C2, en el que cada uno de entre dichos grupos alifático, cicloalifático o heterociclilo de R3, R4 o R3 y R4 juntos se sustituyen opcionalmente con hasta tres átomos de F, o hasta dos grupos alquilos C1-2,-C(O)-alquilo C1-4, -C(O)O-alquilo C1-4, -OH o -O-alquilo C1-2, A es N o CRA, B es N o CRB, o A>=B es un átomo de azufre, C es N o CRC, D es N o CRD, E es N o CRE, en el que no más de dos de entre A, B, C, D o E son N, ...

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