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31. 发明专利

AU2017204191B2 Dihydropyrazoles, pharmaceutical compositions thereof and their use for the treatment of fertility disorders 未知
公开(公告)号：AU2017204191B2
公开(公告)日：2019-10-31
申请号：AU2017204191
申请日：2017-06-21
申请人： MERCK PATENT GMBH
发明人： RICHARDSON THOMAS E , FOGLESONG ROBERT JAMES , DESELM LIZBETH CELESTE , GOUTOPOULOS ANDREAS , YU HENRY
IPC分类号： C07D231/12 , A61K31/4152 , A61K31/4155 , A61P15/08 , C07D401/04 , C07D401/06 , C07D403/06 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/04 , C07D409/06 , C07D413/06
摘要： - 238 Novel dihydropyrazole derivatives of formula (1) x N 2 (CY2 ) N X (CYR)' R (1) wherein L, R, RR4, R,R,R, X', X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, 10 inter alia, for the treatment of fertility disorders.

32. 发明专利

NZ706418A Azaquinazoline carboxamide derivatives 未知
公开(公告)号：NZ706418A
公开(公告)日：2019-09-27
申请号：NZ70641813
申请日：2013-11-27
申请人： MERCK PATENT GMBH
发明人： JOHNSON THERESA L , HUCK BAYARD R , LAN RUOXI , POTNICK JUSTIN , DESELM LIZBETH CELESTE , CRONIN MARK W , CHEN XIAOLING , BOIVIN ROCH , GOUTOPOULOS ANDREAS , NEAGU CONSTANTIN
IPC分类号： C07D403/12 , A61K31/519 , A61K31/53 , A61P35/00 , C07D253/08 , C07D401/12 , C07D471/04
摘要： Novel azaquinazoline carboxamide derivatives of formula (I) wherein each W1, W2, W3, W4 is independently N or CH, wherein at least one of W1, W2, W3 or W4 is N and R1, R2, R3 and m are as defined herein, are p70S6K inhibitor, and can be employed, inter alia, for the treatment of hyperproliferative disorders.

33. 发明专利

SG10201900954SA Heterocycles as Modulators of Kinase Activity 未知
公开(公告)号：SG10201900954SA
公开(公告)日：2019-02-27
申请号：SG10201900954S
申请日：2014-03-10
申请人： MERCK PATENT GMBH
发明人： LAN RUOXI , CHEN XIAOLING , XIAO YUFANG , HUCK BAYARD R , GOUTOPOULOS ANDREAS
摘要： Heterocycles as Modulators of Kinase Activity The invention provides novel heterocyclic amines according to Formula (I) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer. (I)

34. 发明专利

CA2770156C PYRIDO[2,3-D]PYRIMIDINONES AND THEIR USE IN THE TREATMENT OF HYPERPROLIFERATIVE DISEASES 未知
公开(公告)号：CA2770156C
公开(公告)日：2019-02-12
申请号：CA2770156
申请日：2010-07-28
申请人： MERCK PATENT GMBH
发明人： CHEN XIAOLING , KARRA SRINIVASA R , HUCK BAYARD R , LAN RUOXI , SUTTON AMANDA E , GOUTOPOULOS ANDREAS , HODOUS BRIAN L , JONES REINALDO C
IPC分类号： C07D471/04 , A61K31/519 , C07D498/14
摘要： The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.

35. 发明专利

ES2649995T3 Benzamidas 未知
公开(公告)号：ES2649995T3
公开(公告)日：2018-01-16
申请号：ES12738368
申请日：2012-07-17
申请人： MERCK PATENT GMBH
发明人： YU HENRY , LI JIEZHEN , RICHARDSON THOMAS E , BHARATHI PANDI , HEASLEY BRIAN H , GOUTOPOULOS ANDREAS
IPC分类号： C07D401/14 , A61K31/496 , A61P15/08 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/10 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14
摘要： Un compuesto de la fórmula (I-A)I**Fórmula** en donde R1 significa -(CY2)n-E-(CY2)n-Het3, -(CY2)n-Cyc-Het3, -(CY2)n-NHCO-Het3, -(CY2)n-C(Y)(OH)-(CY2)n-Het3, -(CY2)n-Het1, -(CY2)n-NHCO-Het1, -(CY2)n-Ar, -(CY2)n-C(Y)(OH)-(CY2)n-Ar, -(CY2)n-Cyc, -(CY2)n-CONH-Cyc, A, -(CYR8)n-OY, -(CY2)n-COOY, -(CYR8)n-CO-(CY2)n-N(R8)2, -(CY2)n-[C(Y)OH]]m-(CYR8)n-NY2, [-(CY2)n-O]m- (CYR8)n-NYCOY, -(CY2)n-NYCOOY, -(CY2)n-NYCON(R8)2, -(CY2)n-NHCO-CH>=CH2 o -(CY2)n-NHCO-NH- (CY2)n>=CH2; R3 significa Het1, Het3, Ar, H, A o Cyc; R5 significa E-Ar, H, A, COOA o Het1; R8, Y significan, de manera independiente entre sí, H o A; X significa CO o -(CY2)m; E significa -(CY2)m-, CO, -COO- o SO2; A significa alquilo no ramificado o ramificado que tiene 1-10 átomos de C, en donde 1-7 átomos de H se pueden reemplazar de manera independiente entre sí por Hal y/o OH; Cyc significa cicloalquilo que tiene 3-7 átomos de C, en donde 1-4 átomos de H se pueden reemplazar de manera independiente entre sí por Hal y/o OH; Ar significa un carbociclo mono o bicíclico insaturado o aromático que tiene 5-10 átomos de C, que se pueden sustituir con al menos un sustituyente seleccionado del grupo de A, Hal, OY, COOY, CONH2, NHCOY, -(CH2)n- NY2, SO2NH2, NO2, CN y Het2; Het1 significa un heterociclo mono o bicíclico insaturado o aromático que tiene 1-9 átomos de C y 1-3 átomos de N, O y/o S, que se pueden mono o disustituir con al menos un sustituyente seleccionado del grupo de Hal, A, Cyc, OY, CONH2, NHCOY, -(CH2)n-NY2, SO2NY2, NHSO2Y, CN y Ar; Het2 significa imidazolilo, pirazilo, tiazilo o tetrazilo, que pueden estar monosustituidos con metilo; Het3 significa un heterociclo monocíclico saturado que tiene 3-6 átomos de C y 1-3 átomos de N, O y/o S, que se pueden mono, di o trisustituir con al menos un sustituyente seleccionado del grupo de >=O, A, Hal, -(CY2)n-Cyc, - (CY2)n-OY, COY, COOY, CONY2, NHCOY, NY2, CN, SO2Y y -(CY2)n-Ar; Hal significa F, CI, Br o I; y m, n significan, de manera independiente entre sí, 0, 1, 2 ó 3; y/o una sal fisiológicamente aceptable de los mismos, siempre que se excluya el compuesto 3-(3-cloro-benzoilamino)-N-[2-(2,4-dicloro-fenil)-etil]-4-(4-etil-piperazin-1-il)- benzamida.

36. 发明专利

AU2017235978A1 Compositions and methods for the production of pyrimidine and pyridine compounds with BTK inhibitory activity 未知
公开(公告)号：AU2017235978A1
公开(公告)日：2017-10-19
申请号：AU2017235978
申请日：2017-09-28
申请人： MERCK PATENT GMBH
发明人： HODOUS BRIAN L , LIU-BUJALSKI LESLEY , JONES REINALDO , BANKSTON DONALD , JOHNSON THERESA L , MOCHALKIN IGOR , NGUYEN NGAN , QIU HUI , GOUTOPOULOS ANDREAS , BRUGGER NADIA
IPC分类号： C07D239/47 , A61K31/4418 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/5377 , A61P35/00 , A61P35/02 , C07D213/68 , C07D213/73 , C07D213/74 , C07D239/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D495/04
摘要： I- 11 _UUdVVU Abstract The present invention provides novel pyrimidine and pyridine compounds according to Formula (1), Formula (II), Formula (111), Formula (IV) and Formula (V) their manufacture and use for the treatment of hyperproliferative diseases including, but not 5 limited to, Sjogren's disease. In preferred embodiments, the present invention describes irreversible kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase. 9489308_1 (GHMtters) P95096.AU.1

37. 发明专利

PH12017500408A1 HETEROARYL COMPUNDS AS BTK INHIBITORS AND USES THEREOF 未知
公开(公告)号：PH12017500408A1
公开(公告)日：2017-07-17
申请号：PH12017500408
申请日：2017-03-03
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： A61K31/553 , A61K31/437 , A61P29/00 , A61P37/00 , C07D471/04 , C07D519/00
摘要： The present invention relates to imidazopyridine compounds of formula I, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.

38. 发明专利

AU2012267491B2 Compositions and methods for the production of pyrimidine and pyridine compounds with BTK inhibitory activity 未知
公开(公告)号：AU2012267491B2
公开(公告)日：2017-07-06
申请号：AU2012267491
申请日：2012-06-10
申请人： MERCK PATENT GMBH
发明人： HODOUS BRIAN L , LIU-BUJALSKI LESLEY , JONES REINALDO , BANKSTON DONALD , JOHNSON THERESA L , MOCHALKIN IGOR , NGUYEN NGAN , QIU HUI , GOUTOPOULOS ANDREAS , BRUGGER NADIA
IPC分类号： C07D239/47 , A61K31/4418 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/5377 , A61P35/00 , A61P35/02 , C07D213/68 , C07D213/73 , C07D213/74 , C07D239/48 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D495/04
摘要： The present invention provides novel pyrimidine and pyridine compounds according to Formula (I), Formula (II), Formula (III), Formula (IV) and Formula (V) their manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren's disease and rheumatoid arthritis. In preferred embodiments, the present invention describes irreversible kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase.

39. 发明专利

AU2016215185A1 Macrocyclic compounds as IRAK 1/4 inhibitors and uses thereof 未知
公开(公告)号：AU2016215185A1
公开(公告)日：2017-06-29
申请号：AU2016215185
申请日：2016-02-05
申请人： MERCK PATENT GMBH
发明人： CHEN XIAOLING , YU HENRY , LAN RUOXI , JORAND-LEBRUN CATHERINE , JOHNSON THERESA L , GOUTOPOULOS ANDREAS
IPC分类号： C07D487/18 , A61P35/00
摘要： The present invention relates to compounds of Formula (I) and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors. Wherein: Ring A is a 5-membered heterocylic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a 5- membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; each of which is optionally substituted; Ring B is a 6-membered aryl, or a 6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; each of which is optionally substituted; Ring C is a 5-membered heterocylic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a 5- membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; each of which is optionally substituted.

40. 发明专利

AU2017200985A1 Benzamides 未知
公开(公告)号：AU2017200985A1
公开(公告)日：2017-03-02
申请号：AU2017200985
申请日：2017-02-14
申请人： MERCK PATENT GMBH
发明人： YU HENRY , LI JIEZHEN , RICHARDSON THOMAS E , BHARATHI PANDI , HEASLEY BRIAN H , GOUTOPOULOS ANDREAS
IPC分类号： C07D401/14 , A61K31/496 , A61P15/08 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/10 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14
摘要： - 259 Novel benzamide derivatives of formula (1) R 6R _ R - W2 W 1 5 (1) wherein W 1, W2, R1 to R , R6, X and Y have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.

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