专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

41. 发明专利

SG181610A1 2-AMINO-5, 5-DIFLUORO-5, 6-DIHYDRO-4H-OXAZINES AS BACE 1 AND/OR BACE 2 INHIBITORS 未知
公开(公告)号：SG181610A1
公开(公告)日：2012-07-30
申请号：SG2012042560
申请日：2010-12-06
申请人： HOFFMANN LA ROCHE , SIENA BIOTECH SPA
发明人： BANNER DAVID , GUBA WOLFGANG , HILPERT HANS , MAUSER HARALD , MAYWEG ALEXANDER V , NARQUIZIAN ROBERT , PINARD EMMANUEL , POWER EOIN , ROGERS-EVANS MARK , WOLTERING THOMAS , WOSTL WOLFGANG
摘要： The present invention relates to 2-Amino-5,5-difluoro-5,6-dihydro-4H-[1,3]oxazin-4-yl)- phenyl]-amide derivatives of formula (I) having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

42. 发明专利

AU2010311624A1 Positive allosteric modulators (PAM) 未知
公开(公告)号：AU2010311624A1
公开(公告)日：2012-06-07
申请号：AU2010311624
申请日：2010-10-25
申请人： HOFFMANN LA ROCHE
发明人： GREEN LUKE , GUBA WOLFGANG , JAESCHKE GEORG , JOLIDON SYNESE , LINDEMANN LOTHAR , RICCI ANTONIO , RUEHER DANIEL , STADLER HEINZ , VIEIRA ERIC
IPC分类号： C07D213/74 , A61K31/44 , A61K31/4427 , A61K31/505 , A61K31/506 , C07D239/34 , C07D239/42 , C07D401/06 , C07D405/12 , C07D413/06 , C07D493/08
摘要： The present invention relates to phenylethynyl derivatives of formula (I) wherein R is hydrogen, halogen, lower alkyl or lower alkyl substituted by halogen; R is hydrogen, lower alkyl, =O, lower alkoxy, phenyl, hydroxy or lower alkyl substituted by hydroxy; X is N, CF or CH; L is -NR-, -NHC(R)-, -O-, -OC(R)-, -CRR-; R is hydrogen or lower alkyl; R/Rare independently from each other hydrogen or lower alkyl; cyc is cycloalkyl or heterocycloalkyl, or is a non-aromatic bicycle selected from 7-oxa- bicyclo[2.2.1]hept-1-yl or bicyclo[2.2.1]hept-1-yl; n is 1, 2 or 3; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They are useful for the treatment of schizophrenia or cognitive diseases.

43. 发明专利

CA2797622A1 2,5,6,7-TETRAHYDRO-[1,4]OXAZEPIN-3-YLAMINE OR 2,3,6,7-TETRAHYDRO-[1,4]OXAZEPIN-5-YLAMINE COMPOUNDS 未知
公开(公告)号：CA2797622A1
公开(公告)日：2011-11-10
申请号：CA2797622
申请日：2011-05-03
申请人： HOFFMANN LA ROCHE , SIENA BIOTECH SPA
发明人： BANNER DAVID , GUBA WOLFGANG , HILPERT HANS , HUMM ROLAND , MAUSER HARALD , MAYWEG ALEXANDER V , NARQUIZIAN ROBERT , POWER EOIN , ROGERS-EVANS MARK , ROMBACH DIDIER , WOLTERING THOMAS , WOSTL WOLFGANG
IPC分类号： C07D267/10 , A61K31/553 , A61P25/28 , C07D413/12 , C07D417/12
摘要： This invention relates to compounds of the formula (I), wherein A, B and R1 to R7 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BACE2 inhibitors and can be used as 5 medicaments for the therapeutic and/or prophylactic treatment of diseases such as Alzheimer's disease, diabetes, particularly type 2 diabetes, and other metabolic disorders.

44. 发明专利

CA2786216A1 ARYLETHYNYL DERIVATIVES 未知
公开(公告)号：CA2786216A1
公开(公告)日：2011-10-20
申请号：CA2786216
申请日：2011-04-11
申请人： HOFFMANN LA ROCHE
发明人： GREEN LUKE , GUBA WOLFGANG , JAESCHKE GEORG , JOLIDON SYNESE , LINDEMANN LOTHAR , RICCI ANTONIO , RUEHER DANIEL , STADLER HEINZ , VIEIRA ERIC
IPC分类号： C07D401/04 , A61K31/506 , A61P25/18 , C07D401/14 , C07D403/04 , C07D413/04 , C07D413/14 , C07D498/04
摘要： The present invention relates to ethynyl derivatives of formula (I) as allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5). The variables in formula (I) are defined in the specification.

45. 发明专利

BRPI0615449A2 未知
公开(公告)号：BRPI0615449A2
公开(公告)日：2011-05-17
申请号：BRPI0615449
申请日：2006-08-21
申请人： HOFFMANN LA ROCHE
发明人： BINGGELI ALFRED , CHRIST ANDREAS D , GREEN LUKE , GUBA WOLFGANG , MAERKI HANS P , MARTIN RAINER E , MOHR PETER
IPC分类号： C07D413/12 , A61K31/428 , A61K31/437 , A61P3/04 , A61P3/10 , A61P17/06 , A61P19/02 , C07D413/14 , C07D417/12 , C07D417/14 , C07D498/04
摘要： This invention is concerned with compounds of the formula wherein X, A, B, R1, R2 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.

46. 发明专利

BRPI0611138A2 未知
公开(公告)号：BRPI0611138A2
公开(公告)日：2010-08-17
申请号：BRPI0611138
申请日：2006-05-23
申请人： HOFFMANN LA ROCHE
发明人： BINGGELI ALFRED , CHRIST ANDREAS , GREEN LUKE GIDEON GRANVILLE , MAERKI HANS-PETER , MARTIN RAINER EUGEN , MOHR PETER , GUBA WOLFGANG
IPC分类号： C07D401/14 , A61K31/4468 , A61K31/506 , A61K31/5375 , A61P3/10 , C07D211/58 , C07D401/10 , C07D401/12 , C07D407/12 , C07D413/14
摘要： This invention is concerned with compounds of the formula wherein R1 to R5, R5′ and A are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.

47. 发明专利

AR070395A1 DERIVADOS DE 4,5-DIHIDRO-OXAZOL-2-IL- AMINA 未知
公开(公告)号：AR070395A1
公开(公告)日：2010-03-31
申请号：ARP090100540
申请日：2009-02-16
申请人： HOFFMANN LA ROCHE , SIENA BIOTECH SPA
发明人： MARCONI GUIDO , ANDREINI MATTEO , NARQUIZIAN ROBERT , WOSTL WOLFGANG , GABELLERI EMANUELE , GUBA WOLFGANG , WOLTERING THOMAS , EOIN POWER , TRAVAGLI MASSIMILIANO
IPC分类号： C07D263/28 , C07D413/10 , A61K31/422 , A61P25/28
摘要： La presente se refiere a compuestos de la formula (1) en la que R1/R1' con independencia entre sí son hidrogeno, halogeno, alcoxi inferior, alquilo inferior, alquilo inferior sustituido por halogeno, alcoxi inferior sustituido por halogeno, alcoxi inferior sustituido por hidroxi, - O-(CH2)o-O-alquilo inferior, -(CH2)p-O-alquilo inferior, -O-S(O)2-alquilo inferior, -S(O)2-aIquilo inferior o ciano; o R1 y R1' junto con -(CH2)2O-, -O-CH2-O- o -N(R)-(CH2)2-O- pueden formar un anillo de 5 o 6 eslabones junto con los átomos de carbono a los que están unidos; R es hidrogeno o alquilo inferior; R2 es hidrogeno, halogeno, alquilo inferior, ciano, alcoxi inferior, alcoxi inferior sustituido por halogeno, -O-(CH2)p-cicIoalquilo C3-6 o (CH2)o-O-alquilo inferior; R3 con independencia entre sí son hidrogeno, ciano, alcoxi inferior, alquilo inferior, alquilo inferior sustituido por halogeno, alcoxi inferior sustituido por halogeno, -CH2-O-alquilo inferior, -C(O)N-dialquilo inferior o halogeno; R4 es hidrogeno o alquilo inferior; X es un enlace, -NH-C(O)-, -NH- o -O-CH2; Ar es arilo o heteroarilo; y en la que -X-Ar-(R3)m ocupa la posicion 3 o 4 del anillo fenilo; o X-Ar-(R3)m significa benzo[1,3]dioxol; m es el numero 0, 1 o 2; o es el numero 2 o 3; p es el numero 1, 2 o 3; o las sales de adicion de ácido farmacéuticamente activas de los mismos. Se ha encontrado que los compuestos presentes tienen actividad inhibidora de la Asp2 (beta- secretasa, BACE 1 o memapsina-2) y por ello estos compuestos pueden utilizarse para el tratamiento de enfermedades caracterizadas por niveles elevados de amiloide beta o depositos de amiloide beta, en particular la enfermedad de Alzheimer. Procesos de obtencion y composiciones farmacéuticas.

48. 发明专利

DE602006009804D1 未知
公开(公告)号：DE602006009804D1
公开(公告)日：2009-11-26
申请号：DE602006009804
申请日：2006-05-23
申请人： HOFFMANN LA ROCHE
发明人： BINGGELI ALFRED , CHRIST ANDREAS , GREEN LUKE GIDEON GRANVILLE , GUBA WOLFGANG , MAERKI HANS-PETER , MARTIN RAINER EUGEN , MOHR PETER
IPC分类号： C07D401/14 , A61K31/4468 , A61K31/506 , A61K31/5375 , A61P3/10 , C07D211/58 , C07D401/10 , C07D401/12 , C07D407/12 , C07D413/14
摘要： This invention is concerned with compounds of the formula wherein R1 to R5, R5′ and A are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.

49. 发明专利

DE60319837T2 未知
公开(公告)号：DE60319837T2
公开(公告)日：2009-04-30
申请号：DE60319837
申请日：2003-07-18
申请人： HOFFMANN LA ROCHE
发明人： ALANINE ALEXANDER , BLEICHER KONRAD , GUBA WOLFGANG , HAAP WOLFGANG , KUBER DAGMAR , LUEBBERS THOMAS , PLANCHER JEAN-MARC , ROGERS-EVANS MARK , SCHNEIDER GISBERT , ZUEGGE JOCHEN , ROCHE OLIVIER
IPC分类号： C07D317/62 , A61K31/36 , C07D317/46 , C07D317/54 , C07D317/72 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D417/06 , C07D451/06 , C07D491/10
摘要： The present invention relates to compounds of the general formula and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases such as obesity by selective modulation of CB1 receptors.

50. 发明专利

NO20076060L 未知
公开(公告)号：NO20076060L
公开(公告)日：2007-12-28
申请号：NO20076060
申请日：2007-11-26
申请人： HOFFMANN LA ROCHE
发明人： MOHR PETER , BINGGELI ALFRED , MAERKI HANS-PETER , CHRIST ANDREAS , GREEN LUKE GIDEON GRANVILLE , GUBA WOLFGANG , MARTIN REINER EUGEN
IPC分类号： C07D401/12 , A61K31/4523 , A61P3/04 , A61P3/10 , C07D211/58 , C07D401/14
摘要： This invention is concerned with compounds of the formula wherein R1 to R5, R5′ and A are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式