公开(公告)号：US20170157134A1

公开(公告)日：2017-06-08

申请号：US15433392

申请日：2017-02-15

Applicant: Novartis AG

Inventor： Qing Sheng ,  Hui-Qin Wang ,  Fang Li ,  Jinsheng Liang ,  Zhu Alexander Cao ,  John Monahan ,  Richard Versace

IPC: A61K31/5355 ,  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.

公开(公告)号：US10689459B2

公开(公告)日：2020-06-23

申请号：US15535405

申请日：2015-12-10

Applicant: THE GENERAL HOSPITAL CORPORATION ,  NOVARTIS AG

Inventor： Qing Sheng ,  Rakesh K. Jain ,  Vasileios Askoxylakis ,  Gino B. Ferraro ,  Dai Fukumura ,  David P. Kodack

IPC: A61K39/395 ,  C07K16/32 ,  A61K31/5377 ,  C07K16/30 ,  A61K45/06 ,  A61P35/04 ,  A61K39/00

Abstract: The present invention relates to a pharmaceutical combination which comprises (a) a phosphatidylinositol 3-kinase inhibitor or pharmaceutically acceptable salt thereof, and (b) a Her3 antagonist, for simultaneous, separate or sequential administration for the treatment of breast cancer brain metastases; a method of treating a subject having a breast cancer brain metastases comprising administration of said combination to a subject in need thereof; use of such combination for the treatment of breast cancer brain metastases; and a commercial package comprising such combination.

公开(公告)号：US09192663B2

公开(公告)日：2015-11-24

申请号：US13693330

申请日：2012-12-04

Applicant: NOVARTIS AG

Inventor： Winfried Elis ,  Seth Ettenberg ,  Andrew Paul Garner ,  Nicole Haubst ,  Xizhong Huang ,  Christian Carsten Silvester Kunz ,  Elizabeth Anne Reisinger Sprague ,  Qing Sheng

IPC: A61K39/395 ,  C07K16/00 ,  C07K16/32 ,  A61K45/06 ,  A61K31/4439 ,  C07K16/28 ,  A61K39/00

CPC classification number: A61K39/39558 ,  A61K31/4439 ,  A61K39/3955 ,  A61K45/06 ,  A61K2039/505 ,  A61K2039/507 ,  C07K16/28 ,  C07K16/2863 ,  C07K16/32 ,  C07K2317/21 ,  C07K2317/55 ,  C07K2317/73 ,  C07K2317/76 ,  C07K2317/92 ,  A61K2300/00

Abstract: This invention relates to antibodies or fragments thereof which interact with HER family of receptors, e.g., HER3 receptor. In particular, it relates to antibodies or fragments thereof that recognize a conformational epitope of HER3 receptor comprising residues from both domains 2 and 4 resulting in inhibition of both ligand-dependent and ligand-independent signal transduction; and allow ligand binding (e.g., neuregulin), while preventing ligand-induced activation of signal transduction. These antibodies or fragments can be used to treat a number of diseases or disorders characterized by increased levels of HER3 expression (e.g., esophageal cancer). These antibodies or fragments can be used to treat a number of diseases or disorders characterized by the antibodys or fragments ability to decrease tissue weight (e.g., prostate or uterine weights) or to induce atrophy of tissue (e.g., atrophy of male breast).

Abstract translation: 本发明涉及与HER受体家族例如HER3受体相互作用的抗体或其片段。 特别地，其涉及识别包含来自结构域2和4的残基的HER3受体的构象表位的抗体或其片段，导致抑制配体依赖性和与配体无关的信号转导; 并允许配体结合（例如神经调节蛋白），同时防止配体诱导的信号转导活化。 这些抗体或片段可用于治疗以增加的HER3表达水平为特征的许多疾病或病症（例如食道癌）。 这些抗体或片段可用于治疗以减少组织重量（例如前列腺或子宫重量）或诱导组织萎缩（例如雄性乳房萎缩）为特征的抗体或片段能力的许多疾病或病症。

公开(公告)号：US10080800B2

公开(公告)日：2018-09-25

申请号：US14852003

申请日：2015-09-11

Applicant: NOVARTIS AG

Inventor： Winfried Elis ,  Seth Ettenberg ,  Andrew Paul Garner ,  Nicole Haubst ,  Xizhong Huang ,  Christian Carsten Silvester Kunz ,  Elizabeth Anne Reisinger Sprague ,  Qing Sheng

IPC: C07K16/00 ,  A61K39/395 ,  C12P21/08 ,  C07K16/32 ,  A61K45/06 ,  A61K31/4439 ,  C07K16/28 ,  A61K39/00

CPC classification number: A61K39/39558 ,  A61K31/4439 ,  A61K39/3955 ,  A61K45/06 ,  A61K2039/505 ,  A61K2039/507 ,  C07K16/28 ,  C07K16/2863 ,  C07K16/32 ,  C07K2317/21 ,  C07K2317/55 ,  C07K2317/73 ,  C07K2317/76 ,  C07K2317/92 ,  A61K2300/00

Abstract: This invention relates to antibodies or fragments thereof which interact with HER family of receptors, e.g., HER3 receptor. In particular, it relates to antibodies or fragments thereof that recognize a conformational epitope of HER3 receptor comprising residues from both domains 2 and 4 resulting in inhibition of both ligand-dependent and ligand-independent signal transduction; and allow ligand binding (e.g., neuregulin), while preventing ligand-induced activation of signal transduction. These antibodies or fragments can be used to treat a number of diseases or disorders characterized by increased levels of HER3 expression (e.g., esophageal cancer). These antibodies or fragments can be used to treat a number of diseases or disorders characterized by the antibodys or fragments ability to decrease tissue weight (e.g., prostate or uterine weights) or to induce atrophy of tissue (e.g., atrophy of male breast).

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。