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61. 发明专利

ES2568603T3 Pirano[3,2-d][1,3]tiazol como inhibidores de glicosidasas 未知
公开(公告)号：ES2568603T3
公开(公告)日：2016-05-03
申请号：ES12753341
申请日：2012-08-22
申请人： MERCK PATENT GMBH
发明人： DONNELLY MARIANNE , QIU HUI , YU HENRY , LIU-BUJALSKI LESLEY , GOUTOPOULOS ANDREAS
IPC分类号： C07D513/04 , A61K31/429
摘要： Compuesto de fórmula (I)**Fórmula** en la que R1 indica Y, COA, COOA, COO-(CH2)n-Ar, COO-(CH2)n-Cyc; R2, R3 indican independientemente entre sí Y o SO2Y; R4 indica Cl, Br, I, COOY, SO2Y, CN, CAr3, (CH2)m-Ar,**Fórmula** o ; R5 indica (CH2)n-Ar, (CH2)n-Cyc, (CH2)n-Het, (CH2)n-O-Ar, (CH2)n-CY(OH)-Ar, (CH2)n-CO-Ar o (CH2)n-NYAr; X indica CH2, CO o CH(OH); Y indica H o A; A indica alquilo no ramificado o ramificado que tiene 1-10 átomos de C, en el que 1-7 átomos de H pueden reemplazarse independientemente entre sí por Hal y/o en el que un grupo CH2 puede reemplazarse con un grupo -CH>=CH-; Cyc indica cicloalquilo que tiene 3-7 átomos de C, en el que 1-4 átomos de H pueden reemplazarse independientemente entre sí por Hal y/o que pueden sustituirse por Ar; Ar indica un carbociclo mono o bicíclico insaturado o aromático que tiene 3-12 átomos de C, que pueden sustituirse con al menos un sustituyente seleccionado del grupo de Hal, A, (CY2)n-OY, (CY2)n-NYY, COOY, CONYY, NHCOY, SO2Y, CN y fenoxilo; Het indica un heterociclo mono, bi o tricíclico insaturado o aromático que tiene 1-12 átomos de C y 1-4 átomos de N, que pueden sustituirse con al menos un sustituyente seleccionado del grupo de Hal, A, (CY2)n-OY, (CY2)n-NYY, COOY, CONYY, NHCOY, SO2Y, SO2Ar, CN y tiofenilo; Hal indica F, Cl, Br o I; m indica 1, 2 ó 3; y n indica 0, 1, 2, 3, 4, 5 ó 6; y/o sal fisiológicamente aceptable del mismo.

62. 发明专利

CA2960401A1 HETEROARYL COMPOUNDS AS BTK INHIBITORS AND USES THEREOF 未知
公开(公告)号：CA2960401A1
公开(公告)日：2016-04-14
申请号：CA2960401
申请日：2015-10-06
申请人： MERCK PATENT GMBH
发明人： GAILLARD PASCALE , SEENISAMY JEYAPRAKASHNARAYANAN , LIU-BUJALSKI LESLEY , POTNICK JUSTIN , CALDWELL RICHARD D , QIU HUI , NEAGU CONSTANTIN , JONES REINALDO , WON ANNIE CHO , GOUTOPOULOS ANDREAS , SHERER BRIAN A , JOHNSON THERESA L , GARDBERG ANNA
IPC分类号： C07D471/04 , A61K31/395 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/4725 , A61K31/553 , A61P29/00 , A61P37/06 , C07D519/00
摘要： The present invention relates to imidazopyridine compounds of formula I, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.

63. 发明专利

CA2926207A1 HETEROARYL COMPOUNDS AS BTK INHIBITORS AND USES THEREOF 未知
公开(公告)号：CA2926207A1
公开(公告)日：2015-04-30
申请号：CA2926207
申请日：2014-10-21
申请人： MERCK PATENT GMBH
发明人： QIU HUI , CALDWELL RICHARD D , NEAGU CONSTANTIN , MOCHALKIN IGOR , LIU-BUJALSKI LESLEY , JONES REINALDO , TATE DEVON , JOHNSON THERESA L , GARDBERG ANNA
IPC分类号： C07D213/81 , A61K31/4439 , A61K31/506 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D407/04 , C07D409/04 , C07D413/04 , C07D413/06 , C07D487/04
摘要： The present invention relates to pyridine, pyrimidine, pyrazine, and pyridazine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.

64. 发明专利

CA2918242A1 PYRIDINES, PYRIMIDINES, AND PYRAZINES, AS BTK INHIBITORS AND USES THEREOF 未知
公开(公告)号：CA2918242A1
公开(公告)日：2015-02-05
申请号：CA2918242
申请日：2014-07-30
申请人： MERCK PATENT GMBH
发明人： LIU-BUJALSKI LESLEY , NGUYEN NGAN , QIU HUI , JONES REINALDO , MOCHALKIN IGOR , CALDWELL RICHARD D
IPC分类号： C07D487/04 , A61K31/519 , A61P29/00
摘要： The present invention relates to pyridine, pyrimidine, and pyrazene compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.

65. 发明专利

EA020731B1 АМИНОАЗАГЕТЕРОЦИКЛИЧЕСКИЕ КАРБОКСАМИДЫ 未知
公开(公告)号：EA020731B1
公开(公告)日：2015-01-30
申请号：EA201101182
申请日：2010-02-04
申请人： MERCK PATENT GMBH
发明人： SUTTON AMANDA E , RICHARDSON THOMAS E , HUCK BAYARD R , KARRA SRINIVASA R , CHEN XIAOLING , XIAO YUFANG , GOUTOPOULOS ANDREAS , LAN RUOXI , PERREY DAVID , VANDEVEER HAROLD GEORGE , LIU-BUJALSKI LESLEY , STIEBER FRANK , HODOUS BRIAN L , QIU HUI , JONES REINALDO C , HEASLEY BRIAN
IPC分类号： C07D239/94 , A61K31/517 , A61P35/00 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04
摘要： Изобретениеобеспечиваетновыезамещенныеаминоазагетероциклическиекарбоксамидныесоединенияв соответствиис формулой (II)ихприготовлениеи применениедлялечениягиперпролиферативныхзаболеваний, такихкакзлокачественноеновообразование.

66. 发明专利

SG2014009617A PYRANO [3, 2 - D] [1, 3] THIAZOLE AS GLYCOSIDASE INHIBITORS 未知
公开(公告)号：SG2014009617A
公开(公告)日：2014-05-29
申请号：SG2014009617
申请日：2012-08-22
申请人： MERCK PATENT GMBH
发明人： DONNELLY MARIANNE , QIU HUI , YU HENRY , LIU-BUJALSKI LESLEY , GOUTOPOULOS ANDREAS
IPC分类号： C07D513/04 , A61K31/429

67. 发明专利

ZA201106624B NOVEL AMINO AZAHETEROCYCLIC CARBOXAMIDES 未知
公开(公告)号：ZA201106624B
公开(公告)日：2012-05-30
申请号：ZA201106624
申请日：2011-09-09
申请人： MERCK PATENT GMBH
发明人： SUTTON AMANDA E , HUCK BAYARD R , CHEN XIAOLING , GOUTOPOULOS ANDREAS , PERREY DAVID , LIU-BUJASKI LESLEY , HODOUS BRIAN , JONES REINALDO C , RICHARDSON THOMAS E , KARRA SRINIVASA R , XIAO YUFANG , LAN RUOXI , VANDEVEER HAROLD GEORGE , STIEBER FRANK , QIU HUI , HEASLEY BRIAN
IPC分类号： A61K20060101 , A61P20060101 , C07D20060101

68. 发明专利

MX2011008395A NUEVAS AMINO CARBOXAMIDAS AZAHETEROCICLICAS. 未知
公开(公告)号：MX2011008395A
公开(公告)日：2011-09-01
申请号：MX2011008395
申请日：2010-02-04
申请人： MERCK PATENT GMBH
发明人： HODOUS BRIAN L , STIEBER FRANK , LAN RUOXI , XIAO YUFANG , KARRA SRINIVASA R , HUCK BAYARD R , SUTTON AMANDA E , GOUTOPOULOS ANDREAS , LIU-BUJALSKI LESLEY , RICHARDSON THOMAS E , CHEN XIAOLING , PERREY DAVID , VANDEVEER HAROLD GEORGE , QIU HUI , JONES REINALDO C , HEASLEY BRIAN
IPC分类号： C07D239/94 , A61K31/517 , A61P35/00 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04
摘要： Nuevos compuestos de amino carboxamida azaheterocíclica sustituida de acuerdo con la fórmula (I), su fabricación y su uso para el tratamiento de enfermedades hiperproliferativas como el cáncer.

69. 发明专利

CA2926207C HETEROARYL COMPOUNDS AS BTK INHIBITORS AND USES THEREOF 未知
公开(公告)号：CA2926207C
公开(公告)日：2022-06-21
申请号：CA2926207
申请日：2014-10-21
申请人： MERCK PATENT GMBH
发明人： QIU HUI , CALDWELL RICHARD D , NEAGU CONSTANTIN , MOCHALKIN IGOR , LIU-BUJALSKI LESLEY , JONES REINALDO , TATE DEVON , JOHNSON THERESA L , GARDBERG ANNA
IPC分类号： C07D213/81 , A61K31/4439 , A61K31/506 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D407/04 , C07D409/04 , C07D413/04 , C07D413/06 , C07D487/04
摘要： The present invention relates to pyridine, pyrimidine, pyrazine, and pyridazine compounds, and phaimaceutically acceptable compositions thereof, useful as BTK inhibitors. In particular, these BTK inhibitors are compounds of formula I, in which Ring A is a 6-membered heteroaryl ring having 1 or 2 nitrogens, selected from pyridine, pyrazine, pyridazine, and pyrimidine. Representative of the inhibitors of the present application is compound 63 shown below.

70. 发明专利

CA2918242C PYRIDINES, PYRIMIDINES, AND PYRAZINES, AS BTK INHIBITORS AND USES THEREOF 未知
公开(公告)号：CA2918242C
公开(公告)日：2022-06-21
申请号：CA2918242
申请日：2014-07-30
申请人： MERCK PATENT GMBH
发明人： LIU-BUJALSKI LESLEY , NGUYEN NGAN , QIU HUI , JONES REINALDO , MOCHALKIN IGOR , CALDWELL RICHARD D
IPC分类号： C07D487/04 , A61K31/519 , A61P29/00
摘要： The present invention relates to pyridine, pyrimidine, and pyrazene compounds of Formula The present application further relates to pharmaceutically acceptable compositions comprising compounds of Fommla I. The compounds of Fonnula I, and the pharmaceutical compositions thereof, are useful as BTK inhibitors.

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