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1. 发明申请

WO2009016048A1 2-AZETIDINEMETHANEAMINES AND 2-PYRROLIDINEMETHANEAMINES AS TAAR-LIGANDS 审中-公开
标题翻译： 2-氨基乙酰胺和2-吡咯烷基磺酰胺作为TAAR-LIGANDS
公开(公告)号：WO2009016048A1
公开(公告)日：2009-02-05
申请号：PCT/EP2008/059429
申请日：2008-07-18
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , GOERGLER, Annick , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
发明人： GALLEY, Guido , GOERGLER, Annick , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
IPC分类号： C07D205/04 , C07D207/09 , A61K31/397 , A61K31/40 , A61P25/00
CPC分类号： C07D205/04 , C07D207/09
摘要： The present invention relates to compounds of formula (I) wherein R 1 is hydrogen, lower alkyl or benzyl which may be optionally substituted by halogen or lower alkoxy; R 2 is hydrogen, halogen or OR, wherein R is lower alkyl, aryl or lower alkyl substituted by halogen; R 3 is hydrogen or fluorine; Ar is phenyl; n is 0 or 1; o is 0, 1 or 2; and to their pharmaceutically active salts. It has been found that the compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
摘要翻译：本发明涉及式（I）化合物，其中R 1是氢，可以被卤素或低级烷氧基任意取代的低级烷基或苄基; R2是氢，卤素或OR，其中R是被卤素取代的低级烷基，芳基或低级烷基; R3是氢或氟; Ar是苯基; n为0或1; o为0,1或2; 和其药物活性盐。已经发现，式I化合物对微量胺相关受体（TAAR）具有良好的亲和力，特别是对于TAAR1。这些化合物可用于治疗抑郁症，焦虑障碍，双相情感障碍，注意力缺陷多动障碍（ADHD），应激相关疾病，精神病性精神障碍如精神分裂症，神经系统疾病如帕金森病，神经变性疾病如阿尔茨海默病，癫痫，偏头痛，高血压，药物滥用和代谢障碍如进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡紊乱和失调，睡眠和昼夜节律紊乱以及心血管疾病。

2. 发明申请

WO2008046757A1 AMINOMETHYL-4-IMIDAZOLES 审中-公开
标题翻译：氨基甲基-4-咪唑类
公开(公告)号：WO2008046757A1
公开(公告)日：2008-04-24
申请号：PCT/EP2007/060666
申请日：2007-10-09
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , GOERGLER, Annick , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
发明人： GALLEY, Guido , GOERGLER, Annick , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
IPC分类号： C07D233/64 , A61K31/4178 , A61P25/00
CPC分类号： C07D233/64
摘要： The present invention relates to compounds of formula (I) wherein R 1 is hydrogen, lower alkyl, -(CR 2 ) n -OH, -(CH2) n -aryl or -(CH 2 ) n -heteroaryl, which are optionally substituted by halogen, lower alkoxy or lower alkyl substituted by halogen, or is -(CR 2 ) n - cycloalkyl, optionally substituted by hydroxy, -(CH 2 ) n -heterocyclyl, -(CH 2 ) n -NH-S(O) 2 CH 3 , or is -(CR 2 ) n O-lower alkyl or lower alkyl substituted by halogen; R is hydrogen or lower alkyl, and when two R-groups are present, they may or may not be the same; R 2 is 2,2-dioxo-2,3-dihydro-1 H -benzo[c]thiophenyl, 6,7-dihydro-5 H -cyclopentapyrimidin-2-yl, 2,2-difluoro-benzo[1,3]dioxol-5-yl, 2,2,3,3-tetrafluoro-2,3-dihydro-benzo[1,4]dioxin-6-yl, or is aryl or heteroaryl, optionally substituted by one or more substituents, selected from the group consisting of halogen, lower alkyl, cycloalkyl, -(CH 2 ) n -hydroxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, -S(O) 2 -lower alkyl, -(CH 2 ) n -S(O) 2 -NH-lower alkyl, -(CH 2 ) n -O-lower alkyl, nitro, amino, cyano, -NHC(O)-lower alkyl, -C(O)NH-lower alkyl, or O-tetrahydro-naphthalenyl, or are substituted by -(CH 2 ) n -aryl, optionally substituted by halogen, or by -CH=CH-aryl, optionally substituted by halogen, or by -(CH 2 ) n -O-aryl, optionally substituted by halogen, lower alkoxy or lower alkyl substituted by halogen, or by -O-(CH 2 ) n -aryl, optionally substituted by halogen, or by -(CH 2 ) n -heteroaryl, or by -(CH 2 ) n -O-heteroaryl or by -(CH 2 ) n -heterocyclyl, optionally substituted by =O, or by -(CH 2 ) n -O-heterocyclyl, optionally substituted by lower alkyl, or by -S-aryl, -CH(OH)-aryl, -C(CH 3 ) 2 -aryl, -NR-aryl, or by 2-oxo-2H-pyridin-1-yl; R 3 is hydrogen or lower alkyl; R 4 is hydrogen or lower alkyl; n is 0, 1, 2, 3 or 4 and to their pharmaceutically active salts for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
摘要翻译：本发明涉及式（I）化合物，其中R 1是氢，低级烷基， - （CR 2）n -OH， - （CH 2）n - 芳基或 - （CH 2）n - 杂芳基，其任选被卤素，低级烷氧基或低级烷基被卤素取代，或是 - （CR 2）n - 环烷基，任选被羟基取代， - （CH 2）n - （CH 2）n - 杂环基， - （CH 2）n -NH-S（O）2 CH 3 >或者是 - （CR 2）n - 低级烷基或被卤素取代的低级烷基; R是氢或低级烷基，当存在两个R基时，它们可以相同也可以不相同; R 2是2,2-二氧代-2,3-二氢-1H-苯并[c]噻吩基，6,7-二氢-5H-环戊基嘧啶-2-基，2,2-二氟 - 苯并[1,3]二氧杂环戊烯-5-基，2,2,3,3-四氟-2,3-二氢 - 苯并[1,4]二恶英-6-基，或者是芳基或杂芳基，任选被一个或更多取代基，选自卤素，低级烷基，环烷基， - （CH 2）n - 羟基，被卤素取代的低级烷基，被卤素，-S（O）2 - 低级烷基， - （CH 2）n - （O）2 - （CH 2）n - 低级烷基，硝基，氨基，氰基，-NHC（O） - 低级烷基， - （CH 2） C（O）NH-低级烷基或O-四氢 - 萘基，或被 - （CH 2 CH 2）n - 芳基取代，任选被卤素取代，或被 -CH = CH-芳基，任选被卤素取代，或被 - （CH 2 CH 2）n -O-取代的，被卤素，低级烷氧基或低级烷基取代的通过卤素或-O-（CH 2 CH 2）n

3. 发明申请

WO2008046756A1 AMINOMETHYL-2-IMIDAZOLES WITH AFFINITY WITH THE TRACE AMINE ASSOCIATED RECEPTORS 审中-公开
标题翻译：与维生素A相关受体有亲和力的氨基甲基-2-咪唑烷
公开(公告)号：WO2008046756A1
公开(公告)日：2008-04-24
申请号：PCT/EP2007/060664
申请日：2007-10-09
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , GOERGLER, Annick , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
发明人： GALLEY, Guido , GOERGLER, Annick , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
IPC分类号： C07D233/64 , C07D401/12 , C07D403/12 , C07D409/12 , A61K31/417 , A61P25/00
CPC分类号： C07D233/64 , C07D401/12 , C07D403/12 , C07D409/12
摘要： The present invention relates to compounds of Formula (I) and to their pharmaceutically active salts. It has been found that the compounds of formula (I) have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm and cardiovascular disorders.
摘要翻译：本发明涉及式（I）的化合物及其药学活性盐。已经发现式（I）化合物对微量胺相关受体（TAAR）具有良好的亲和力，特别是对于TAAR1。这些化合物可用于治疗抑郁症，焦虑障碍，双相情感障碍，注意力缺陷多动障碍（ADHD），应激相关疾病，精神病性精神障碍如精神分裂症，神经系统疾病如帕金森病，神经变性疾病如阿尔茨海默病，癫痫，偏头痛，高血压，药物滥用和代谢紊乱，如进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡失调和失眠，睡眠障碍和昼夜节律和心血管疾病。

4. 发明申请

WO2010010014A1 4,5-DIHYDRO-OXAZOL-2-YL DERIVATIVES 审中-公开
标题翻译： 4,5-DIHYDRO-OXAZOL-2-YL衍生物
公开(公告)号：WO2010010014A1
公开(公告)日：2010-01-28
申请号：PCT/EP2009/059026
申请日：2009-07-15
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , GOERGLER, Annick , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger
发明人： GALLEY, Guido , GOERGLER, Annick , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger
IPC分类号： C07D263/28 , C07D413/12 , A61K31/421 , A61K31/422 , A61P25/00 , A61P3/04 , A61P3/06 , A61P3/10
CPC分类号： C07D263/28 , C07D413/12
摘要： The invention relates to compounds of formula (I) wherein R 1 is hydrogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, halogen, cyano, nitro, hydroxy, C(O)O-lower alkyl, S(O) 2 -lower alkyl, C(O)OCH 2 -phenyl, OCH 2 -phenyl, tetrazol-1-yl, phenyl optionally substituted by halogen, or is phenyloxy optionally substituted by halogen, or is benzyl optionally substituted by halogen or is benzyloxy optionally substituted by halogen, wherein the substituents for n> 1 may be the same or different; X is -O-(CH 2 ) 2 -, -O-CHR"-CH 2 -, -O-CH 2 -CHR', -O-CR'' 2 -CH 2 -, -(CH 2 ) 2 -CHR', -CHR'-(CH 2 ) 2 -, -CR" 2 -(CH 2 ) 2 -, -CH 2 -CHR'-CH 2 -, -CH 2 -CR'' 2 -CH 2 -, -CHR"-O-CH 2 -, -CH 2 -O-CH 2 -, -CR'' 2 -O-CH 2 -, -CF 2 (CH 2 ) 2 -, -CR" 2 -CH 2 -, -SiR" 2 -(CH 2 ) 2 -, -S-(CH 2 ) 2 -, -S(O) 2 -(CH 2 ) 2 -, -(CH 2 ) 4 -, -CH 2 -O-(CH 2 ) 2 -, for m being 0, 1, 2 or 3; R' is lower alkyl, lower alkoxy or lower alkyl substituted by halogen; R'' is lower alkyl or lower alkyl substituted by halogen; R 2 is hydrogen or lower alkyl; Y is aryl, cycloalkyl or heteroaryl; n is 1, 2 or 3; or to a pharmaceutically suitable acid addition salt. The compounds disclosed in the present formula (I) may be used for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress- related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
摘要翻译：本发明涉及式（I）化合物，其中R 1是氢，低级烷基，低级烷氧基，被卤素取代的低级烷基，被卤素，卤素，氰基，硝基，羟基，C（O）O-低级烷基取代的低级烷氧基， S（O）2 - 低级烷基，C（O）OCH 2 - 苯基，OCH 2 - 苯基，四唑-1-基，任选被卤素取代的苯基，或任选被卤素取代的苯氧基，或是任选被卤素取代的苄基，任选被卤素取代的苄氧基，其中n> 1的取代基可以相同或不同; X是-O-（CH 2）2 - ， - O-CHR“-CH 2 - ，-O-CH 2 -CHR'，-O-CR''2-CH 2 - ， - （CH 2）2 -CHR' ' - （CH 2）2 - ， - CR“2-（CH 2）2 - ， - CH 2 -CHR'-CH 2 - ， - CH 2 -CR''2-CH 2 - ， - CHR”-O-CH 2 - ， - CH 2 （CH 2）2 - ， - CR“2 -CH 2 - ，-SiR”2-（CH 2）2 - ， - S-（CH 2）2 - 2，-S（O）2 - （CH 2）2 - ， - （CH 2）4 - ， - CH 2 -O-（CH 2）2 - ，其中m为0,1,2或3; R' 低级烷氧基或被卤素取代的低级烷基; R“为被卤素取代的低级烷基或低级烷基; R 2为氢或低级烷基; Y为芳基，环烷基或杂芳基; n为1,2或3; 本发明式（I）中公开的化合物可用于治疗与微量胺相关受体的生物学功能有关的疾病，所述疾病是抑郁症，焦虑障碍，双相情感障碍，注意缺陷多动障碍，压力相关疾病，精神病，精神分裂症，神经系统疾病，帕金森病，神经变性疾病，阿尔茨海默病，癫痫，偏头痛，药物滥用和代谢紊乱，饮食失调，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡紊乱和失调，睡眠和昼夜节律紊乱以及心血管疾病。

5. 发明申请

WO2013104591A1 HETEROCYCLIC DERIVATIVES AS TRACE AMINE ASSOCIATED RECEPTORS (TAARS) 审中-公开
标题翻译：作为胺类相关受体（TAARS）的杂环衍生物
公开(公告)号：WO2013104591A1
公开(公告)日：2013-07-18
申请号：PCT/EP2013/050170
申请日：2013-01-08
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , GOERGLER, Annick , NORCROSS, Roger , PFLIEGER, Philippe
发明人： GALLEY, Guido , GOERGLER, Annick , NORCROSS, Roger , PFLIEGER, Philippe
IPC分类号： C07D413/10 , C07D413/14 , C07D471/04 , A61K31/5377 , A61P25/00
CPC分类号： C07D413/10 , C07D413/14 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds of formula (I) wherein R 1 is a one or two membered heteroaryl group, selected from the group consisting of formula (a), (b), (c), (d), (e), (f), (g), (h), (i), (j); R 2 is hydrogen or halogen; or R 1 and R 2 may form together with the carbon atoms to with they are attached the following rings formula (k), (l), (m), (n), (o). R 3 is hydrogen, halogen or lower alkyl; n is 1 or 2; R 4 is phenyl, optionally substituted by one or two substituents, selected from halogen or cyano, or is pyridinyl, optionally substituted by halogen, or is tetrahydropyran, or is -NH-C(O)-phenyl, optionally substituted by halogen; R 5 is hydrogen or halogen; R 6 – R 13 are phenyl, optionally substituted by halogen: R 14 is –NH-C(O)-phenyl, substituted by halogen; R 15 is hydrogen, lower alkyl substituted by halogen or is halogen; R 16 is hydrogen or lower alkoxy; R 17 is pyridinyl, optionally substituted by lower alkoxy or lower alkyl substituted by halogen; or to a pharmaceutically suitable acid addition salt thereof, to all racemic mixtures, to all their corresponding enantiomers and/or optical isomers and to all tautomeric forms of compounds of formula I. The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
摘要翻译：本发明涉及式（I）化合物，其中R 1是选自式（a），（b），（c），（d），（e），（d） f），（g），（h），（i），（j）; R2是氢或卤素; 或者R 1和R 2可以与碳原子一起形成，它们连接下列环（k），（l），（m），（n），（o）。 R3是氢，卤素或低级烷基; n为1或2; R4是任选被一个或两个选自卤素或氰基的取代基取代的苯基，或是任选被卤素取代的吡啶基，或是四氢吡喃，或者是任选被卤素取代的-NH-C（O） - 苯基; R5是氢或卤素; R6-R13是任选被卤素取代的苯基; R 14是被卤素取代的-NH-C（O） - 苯基; R 15是氢，被卤素取代的低级烷基或是卤素; R 16是氢或低级烷氧基; R 17为吡啶基，任选被低级烷氧基或被卤素取代的低级烷基取代; 或其药学上合适的酸加成盐，与所有相应的对映异构体和/或光学异构体以及式I化合物的所有互变异构体形式。式I化合物与微量胺相关联具有良好的亲和力受体（TAAR），特别是TAAR1。这些化合物可用于治疗抑郁症，焦虑障碍，双相情感障碍，注意力缺陷多动障碍（ADHD），应激相关疾病，精神病性精神障碍如精神分裂症，神经系统疾病如帕金森病，神经变性疾病如阿尔茨海默病，癫痫，偏头痛，高血压，药物滥用和代谢障碍如进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡紊乱和失调，睡眠和昼夜节律紊乱以及心血管疾病。

6. 发明申请

WO2020254572A1 EGFR INHIBITORS FOR THE TREATMENT OF CANCER 审中-公开
公开(公告)号：WO2020254572A1
公开(公告)日：2020-12-24
申请号：PCT/EP2020/067093
申请日：2020-06-19
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： DOLENTE, Cosimo , GOERGLER, Annick , HEWINGS, David , JAESCHKE, Georg , KUHN, Bernd , NAGEL, Yvonne, Alice , OBST SANDER, Ulrike , RICCI, Antonio , RUEHER, Daniel , STEINER, Sandra
IPC分类号： C07D487/04 , A61P35/00 , A61K31/496 , A61K31/5377 , A61K31/4709 , A61K31/454 , A61K31/4439
摘要： The application relates to (106) specific heterocyclic compounds comprising a thiazole ring, an indazol ring and a 6,7-dihydro-5H- pyrrolo[l,2-c]imidazole ring system, to pharmaceutical compositions containing them and their medical use. The compounds are described as selective allosteric inhibitors of T790M/L858R, T790M/L858R/ C797S, L858R, L858R/C797S containing EGFR mutants and thus useful for the treatment of cancer, in particular non-small cell lung cancer. (formula)

7. 发明申请

WO2004069826A1 MALONAMIDE DERIVATIVES AS GAMMA-SECRETASE INHIBITORS 审中-公开
标题翻译：作为GAMMA-分泌酶抑制剂的马来酰胺衍生物
公开(公告)号：WO2004069826A1
公开(公告)日：2004-08-19
申请号：PCT/EP2004/000674
申请日：2004-01-27
申请人： F. HOFFMANN-LA ROCHE AG
发明人： GALLEY, Guido , GOERGLER, Annick , JACOBSEN, Helmut , KITAS, Eric, Argirios , PETERS, Jens-Uwe
IPC分类号： C07D401/06
CPC分类号： C07C237/22 , C07C233/47 , C07C323/41 , C07C2601/14 , C07D209/18 , C07D209/44 , C07D215/227 , C07D217/06 , C07D223/18 , C07D243/12 , C07D243/14 , C07D243/24 , C07D265/30 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/12 , C07D409/12 , C07D471/04 , C07D471/06 , C07D471/08 , C07D487/06
摘要： The invention relates to malonamide derivatives of formula (IA) or (IB) and to pharmaceutically suitable acid addition salts thereof. The compounds are γ-secretase inhibitors and the related compounds may be useful in the treatment of Alzheimer's disease.
摘要翻译：本发明涉及式（IA）或（IB）的丙二酰胺衍生物及其药学上合适的酸加成盐。化合物是γ-分泌酶抑制剂，相关化合物可用于治疗阿尔茨海默氏病。

8. 发明申请

WO2022117487A1 NEW INDAZOLE DERIVATIVES 审中-公开
公开(公告)号：WO2022117487A1
公开(公告)日：2022-06-09
申请号：PCT/EP2021/083301
申请日：2021-11-29
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： DOLENTE, Cosimo , GOERGLER, Annick , HEWINGS, David Stephen , JAESCHKE, Georg , OBST SANDER, Ulrike , RICCI, Antonio
IPC分类号： C07D487/04 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/4995 , A61K31/5377 , A61P35/00 , C07D487/08
摘要： The invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R4 and A are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.

9. 发明申请

WO2020254546A1 NEW EGFR INHIBITORS 审中-公开
公开(公告)号：WO2020254546A1
公开(公告)日：2020-12-24
申请号：PCT/EP2020/067055
申请日：2020-06-19
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： DOLENTE, Cosimo , GOERGLER, Annick , HEWINGS, David Stephen , JAESCHKE, Georg , KUHN, Bernd , NAGEL, Yvonne Alice , NORCROSS, Roger David , OBST-SANDER, Christa Ulrike , RICCI, Antonio , RUEHER, Daniel , STEINER, Sandra
IPC分类号： A61P35/00 , C07D417/14 , A61K31/427
摘要： The invention provides novel compounds as described herein, compositions including the compounds and methods of using the compounds.

10. 发明申请

WO2019043217A1 DIHYDROBENZIMIDAZOLONES 审中-公开
公开(公告)号：WO2019043217A1
公开(公告)日：2019-03-07
申请号：PCT/EP2018/073584
申请日：2018-09-03
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： GOERGLER, Annick , NORCROSS, Roger , DEY, Fabian , KUSZNIR, Eric Andre
IPC分类号： C07D401/14 , A61K31/4709 , A61K31/5517 , C07D401/04 , C07D401/12 , C07D235/26 , C07D403/04 , C07D403/06 , C07D403/14 , C07D417/04 , C07D487/04 , C07D495/14 , C07D519/00
CPC分类号： C07D235/26 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D417/04 , C07D487/04 , C07D495/14 , C07D519/00
摘要： The present invention provides compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. Present compounds are thus useful for the treatment of various cancers.

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