- Preparation method of selinexor and intermediate thereof
-
The invention relates to a preparation method of selinexor and an intermediate thereof, which has the advantages of short synthetic route, mild reaction conditions, no foul gas generation in the reaction process, high safety, wide acceptable range of vari
- -
-
Paragraph 0167-0170
(2021/04/21)
-
- PROCESS FOR PREPARING XPO1 INHIBITORS AND INTERMEDIATES FOR USE IN THE PREPARATION OF XP01 INHIBITORS
-
The present invention provides an improved process for preparation of the (Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)acrylic acid (referred to as compound of the structural formula (III)), which is a useful key intermediate for the sy
- -
-
Paragraph 0068; 0090-0091; 0093-0094
(2020/11/12)
-
- Acryloyl group-containing nuclear transport modulator and uses thereof
-
The invention relates to a novel acryloyl-containing compound as well as a preparation method and application thereof. Specifically, the invention relates to an acryloyl-containing compound as shown in a formula (1) and a preparation method thereof, and a
- -
-
-
- NOVEL CRYSTALLINE FORMS OF SELINEXOR AND PROCESS FOR THEIR PREPARATION
-
The present disclosure relates to solid state forms of Selinexor, processes for preparation thereof and pharmaceutical compositions thereof.
- -
-
-
- SOLID FORMS OF SELINEXOR AND PROCESS FOR THEIR PREPARATION
-
Aspects of the present application relate to solid forms of Selinexor, processes for their preparation and pharmaceutical compositions thereof. Specific aspects relate to crystalline and amorphous forms of Selinexor.
- -
-
Page/Page column 60
(2017/08/01)
-
- NUCLEAR TRANSPORT MODULATORS AND USES THEREOF
-
The present invention relates to compounds of Structural Formulas (I), (II) and (III): or their pharmaceutically acceptable salts; pharmaceutical compositions comprising the compounds of Structural Formulas (I), (II) and (III); and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRMl activity. The values for the variables in Structural Formulas (I), (II) and (III) are as described and defined herein.
- -
-
-
- Selinexor
-
Advances in the understanding of the pathophysiology, molecular biology and genetics of solid tumors and hematological malignancies have culminated in the development of novel targeted therapeutic agents leading to improved prognosis and quality of life for cancer patients. Despite these advances, prognosis remains poor for many cancer patients, and there is an unmet need for new therapeutic options. Exportin-1 (XPO1) is a nuclear export receptor that is responsible for exporting proteins, including tumor suppressor proteins, out of the nucleus. Nuclear export of tumor suppressor proteins is an important mechanism by which cancer cells avoid apoptosis and cell death. Overexpression of XPO1 imparts poor prognosis, indicating that XPO1 inhibition can be a potential therapeutic target. Recently, selective inhibitors of nuclear export (SINE) drugs have been developed. Selinexor (KPT-330) is an oral SINE with a favorable toxicity profile and demonstrated to have preclinical and clinical activity against a broad range of solid tumors and hematological malignancies.
- Riaz,Burke,Mahipal
-
p. 685 - 692
(2015/02/02)
-
- HYDRAZIDE CONTAINING NUCLEAR TRANSPORT MODULATORS AND USES THEREOF
-
The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula (I): or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
- -
-
-
- NUCLEAR TRANSPORT MODULATORS AND USES THEREOF
-
The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula I, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.
- -
-
-