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公开(公告)号:US20220281970A1
公开(公告)日:2022-09-08
申请号:US17414211
申请日:2019-12-18
Applicant: Novartis AG
Inventor: Nelson Guerreiro , Ensar Halilovic , Astrid Jullion , Christophe Meille , Hui-Qin Wang , Claire Fabre
IPC: C07K16/28 , A61K31/506 , A61P35/02 , A61K39/395 , A61K45/06
Abstract: The present invention relates to the combination of the HDM2-p53 interaction inhibitor drug (S)-5-(5-Chloro-1-methyl-2-oxo-1,2-dihydro-pyridin-3-yl)-6-(4-chloro-phenyl)-2-(2,4-dimethoxy-pyrimidin-5-yl)-1-isopropyl-5,6-dihydro-1H-pyrrolo[3,4-d]imidazol-4-one [HDM201] and an anti-TIM-3 antibody molecule as TIM-3 inhibitor. The present invention further relates to the use of said combination in the treatment of cancer, in particular hematological tumors. The present invention further relates to dose and dosing regimen related to this combination cancer treatment.
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公开(公告)号:US10220038B2
公开(公告)日:2019-03-05
申请号:US15914479
申请日:2018-03-07
Applicant: Novartis AG
Inventor: Stephane Ferretti , Sebastien Jeay , Ensar Halilovic , Fang Li , Hui-Qin Wang
IPC: A61K31/519 , A61K31/4188 , A61K31/505 , A61K31/496 , A61K31/506
Abstract: The disclosure relates to a pharmaceutical combination of a mdm2/4 inhibitor, namely (S)-1-(4-Chloro-phenyl)-7-isopropoxy-6-methoxy-2-(4-{methyl-[4-(4-methyl-3-oxo-piperazin-1-yl)-trans-cyclohexylmethyl]-amino}-phenyl)-1,4-dihydro-2H-isoquinolin-3-one or (S)-5-(5-Chloro-1-methyl-2-oxo-1,2-dihydro-pyridin-3-yl)-6-(4-chloro-phenyl)-2-(2,4-dimethoxy-pyrimidin-5-yl)-1-isopropyl-5,6-dihydro-1H-pyrrolo[3,4-d]imidazol-4-one, and a cyclin dependent kinase 4/6 (CDK4/6) inhibitor 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide. In addition, the disclosure relates to a pharmaceutical combination product. The disclosure also relates to corresponding pharmaceutical formulations, uses and treatment methods comprising said mdm2/4 inhibitor or a cyclin dependent kinase 4/6 (CDK4/6) inhibitor.
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公开(公告)号:US20180015092A1
公开(公告)日:2018-01-18
申请号:US15683887
申请日:2017-08-23
Applicant: Novartis AG
Inventor: Stephane Ferretti , Sebastien Jeay , Ensar Halilovic , Fang Li , Hui-Qin Wang
IPC: A61K31/519 , A61K31/506 , A61K31/496
CPC classification number: A61K31/519 , A61K31/4188 , A61K31/496 , A61K31/505 , A61K31/506 , A61K2300/00
Abstract: The disclosure relates to a pharmaceutical combination of a mdm2/4 inhibitor, namely (S)-1-(4-Chloro-phenyl)-7-isopropoxy-6-methoxy-2-(4-{methyl-[4-(4-methyl-3-oxo-piperazin-1-yl)-trans-cyclohexylmethyl]-amino}-phenyl)-1,4-dihydro-2H-isoquinolin-3-one or (S)-5-(5-Chloro-1-methyl-2-oxo-1,2-dihydro-pyridin-3-yl)-6-(4-chloro-phenyl)-2-(2,4-dimethoxy-pyrimidin-5-yl)-1-isopropyl-5,6-dihydro-1H-pyrrolo[3,4-d]imidazol-4-one, and a cyclin dependent kinase 4/6 (CDK4/6) inhibitor 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide. In addition, the disclosure relates to a pharmaceutical combination product. The disclosure also relates to corresponding pharmaceutical formulations, uses and treatment methods comprising said mdm2/4 inhibitor or a cyclin dependent kinase 4/6 (CDK4/6) inhibitor.
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公开(公告)号:US20150290204A1
公开(公告)日:2015-10-15
申请号:US14440915
申请日:2013-11-06
Applicant: NOVARTIS AG
Inventor: Qing Sheng , Hui-Qin Wang , Fang Li , Jinsheng Liang , Zhu Alexander Cao , John Monahan , Richard Versace
IPC: A61K31/5377 , A61K31/506
CPC classification number: A61K31/5355 , A61K31/365 , A61K31/395 , A61K31/416 , A61K31/506 , A61K31/519 , A61K31/52 , A61K31/5377 , A61K45/06 , A61K2300/00
Abstract: A pharmaceutical combination comprising (a) a compound of formula (I), or pharmaceutically acceptable salts thereof; and (b) one or more at least one compound targeting, decreasing or inhibiting the intrinsic ATPase activity of Hsp90 and/or degrading, targeting, decreasing or inhibiting the Hsp90 client proteins via the ubiquitin proteosome pathway; the uses of such combination in the treatment or prevention of proliferative diseases; and methods of treating a subject suffering from a proliferative disease; and methods of treating a subject suffering from a proliferative disease comprising administering a therapeutically effective amount of such combination.
Abstract translation: 一种药物组合,其包含(a)式(I)化合物或其药学上可接受的盐; 和(b)一种或多种至少一种靶向,降低或抑制Hsp90的内在ATP酶活性和/或通过泛素蛋白酶途径降解,靶向,降低或抑制Hsp90客体蛋白的化合物; 这种组合在治疗或预防增殖性疾病中的用途; 以及治疗患有增殖性疾病的受试者的方法; 以及治疗患有增殖性疾病的受试者的方法,包括施用治疗有效量的这种组合。
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