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1. 发明申请

WO2017117535A1 NUCLEAR TRANSPORT MODULATORS AND USES THEREOF 审中-公开
标题翻译：核输运调节器及其用途
公开(公告)号：WO2017117535A1
公开(公告)日：2017-07-06
申请号：PCT/US2016/069508
申请日：2016-12-30
申请人： KARYOPHARM THERAPEUTICS INC.
发明人： BALOGLU, Erkan
IPC分类号： C07D403/12 , C07D401/08 , C07D401/12 , C07D403/06 , C07D403/08 , C07D239/26 , C07D409/06 , C07D413/06 , C07D241/12 , A61K31/4965 , A61P35/00
CPC分类号： C07D241/12 , C07D239/26 , C07D401/08 , C07D401/12 , C07D403/06 , C07D403/08 , C07D403/12 , C07D409/06 , C07D413/06
摘要： The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula (I) or their pharmaceutically acceptable salts, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐，包含式（I）化合物或其药学上可接受的盐的药物组合物，以及使用所述化合物，盐和组合物用于治疗与CRM1活性有关的各种疾病。

2. 发明申请

WO2017031204A1 CYCLOPROPYLDERIVATIVES AND THEIR USE AS KINASE INHIBITORS 审中-公开
标题翻译：环丙基胆碱衍生物及其作为激酶抑制剂的用途
公开(公告)号：WO2017031204A1
公开(公告)日：2017-02-23
申请号：PCT/US2016/047337
申请日：2016-08-17
申请人： KARYOPHARM THERAPEUTICS INC.
发明人： BALOGLU, Erkan , SHACHAM, Sharon , SENAPEDIS, William
IPC分类号： C07D405/14 , C07D413/14 , C07D405/12 , A61K31/443 , A61K31/4439 , A61P35/00 , A61P29/00 , A61P37/00
CPC分类号： C07D405/14 , C07D405/12 , C07D413/14
摘要： The invention generally relates to cyclic compounds and, more particularly, to a compound represented by Structural Formula I: or a pharmaceutically acceptable salt thereof and pharmaceutical comopositions comprising the multicyclic compounds. The invention also relates to a method for treating a disease or disorder selected from cancer (e.g., lymphoma, such as mantle cell lymphoma), a neurodegenerative disease, an inflammatory diseases or an immune system disease (e.g., a T-Cell mediated autoimmune disesase) in a subject in need thereof. The method comprises administering to a subject in need thereof a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof, or a composition comprising a compound of the invention, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明一般涉及环状化合物，更具体地说，涉及由结构式I表示的化合物或其药学上可接受的盐和包含多环化合物的药物组合物。本发明还涉及一种治疗选自癌症（例如淋巴瘤，例如套细胞淋巴瘤），神经变性疾病，炎性疾病或免疫系统疾病（例如，T细胞介导的自身免疫性疾病）在有需要的受试者中。该方法包括向有需要的受试者施用治疗有效量的本发明化合物或其药学上可接受的盐，或包含本发明化合物或其药学上可接受的盐的组合物。

3. 发明申请

WO2014085607A1 SUBSTITUTED 2,3-DIHYDROBENZOFURANYL COMPOUNDS AND USES THEREOF 审中-公开
标题翻译：取代的2,3-二氢苯并呋喃化合物及其用途
公开(公告)号：WO2014085607A1
公开(公告)日：2014-06-05
申请号：PCT/US2013/072264
申请日：2013-11-27
申请人： KARYOPHARM THERAPEUTICS INC.
发明人： BALOGLU, Erkan , SHECHTER, Sharon , SHACHAM, Sharon , MCCAULEY, Dilara , SENAPEDIS, William , GOLAN, Gali , KALID, Ori
IPC分类号： C07D405/14 , C07D405/12 , C07D409/14 , A61K31/4427 , A61P35/00
CPC分类号： C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D495/04
摘要： The invention generally relates to substituted 2,3-dihydrobenzofuranyl compounds, and more particularly to a compound represented by Structural Formula (I), or a pharmaceutically acceptable salt thereof, wherein 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 of cancer (e.g., mantle cell lymphoma), and other diseases and disorders.
摘要翻译：本发明一般涉及取代的2,3-二氢苯并呋喃基化合物，特别是涉及由结构式（I）表示的化合物或其药学上可接受的盐，其中变量如本文所定义和描述。本发明还包括结构式（I）的化合物或其药学上可接受的盐或组合物的合成和用途，例如用于治疗癌症（例如，套细胞淋巴瘤）和其它疾病和病症。

4. 发明申请

WO2013019561A1 NUCLEAR TRANSPORT MODULATORS AND USES THEREOF 审中-公开
标题翻译：核输运调节器及其用途
公开(公告)号：WO2013019561A1
公开(公告)日：2013-02-07
申请号：PCT/US2012048368
申请日：2012-07-26
申请人： KARYOPHARM THERAPEUTICS INC , SANDANAYAKA VINCENT P , SHACHAM SHARON , KAUFFMAN MICHAEL , SHECHTER SHARON , MCCAULEY DILARA , LANDESMAN YOSEF , SENAPEDIS WILLIAM , SAINT-MARTIN JEAN-RICHARD
发明人： SANDANAYAKA VINCENT P , SHACHAM SHARON , KAUFFMAN MICHAEL , SHECHTER SHARON , MCCAULEY DILARA , LANDESMAN YOSEF , SENAPEDIS WILLIAM , SAINT-MARTIN JEAN-RICHARD
IPC分类号： C07D213/50 , A61K31/407 , A61K31/4196 , A61K31/421 , A61K31/4439 , A61K31/454 , A61K31/497 , A61K31/506 , C07D401/08 , C07D401/12 , C07D401/14 , C07D403/08 , C07D403/12 , C07D413/12 , C07D487/10
CPC分类号： C07D487/10 , C07D213/50 , C07D401/06 , C07D401/08 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/12
摘要： The invention generally relates to nuclear transport modulators, e.g CRM1inhibitors, and more particularly to a compound represented by formula (I): or a pharmaceutically acceptable salt thereof, wherein 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.
摘要翻译：本发明总体上涉及核转运调节剂，例如CRM1抑制剂，并且更具体地涉及由式（I）表示的化合物：或其药学上可接受的盐，其中变量如本文所定义和描述。本发明还包括结构式（I）的化合物或其药学上可接受的盐或组合物的合成和用途，例如用于治疗，调节和/或预防与CRM1活性相关的生理病症。

5. 发明申请

WO2011109799A8 NUCLEAR TRANSPORT MODULATIORS AND USES THEREOF 审中-公开
标题翻译：核运输调节剂及其用途
公开(公告)号：WO2011109799A8
公开(公告)日：2011-12-22
申请号：PCT/US2011027328
申请日：2011-03-05
申请人： KARYOPHARM THERAPEUTICS INC , SHACHAM SHARON , KAUFFMAN MICHAEL , SANDANYAKA VINCENT P , SHECHTER SHARON
发明人： SHACHAM SHARON , KAUFFMAN MICHAEL , SANDANYAKA VINCENT P , SHECHTER SHARON
IPC分类号： A01N57/00
CPC分类号： C07D409/04 , A61K31/4196 , A61K31/433 , A61K31/4439 , A61K31/444 , A61K31/496 , A61K31/505 , C07D207/337 , C07D231/12 , C07D233/64 , C07D249/08 , C07D257/04 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D417/04 , C07D417/12
摘要： The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).
摘要翻译：本发明一般涉及核转运调节剂领域，例如CRM1抑制剂，更具体地涉及新的取代杂环唑化合物，这些化合物及其药物组合物的合成和用途，例如在治疗，调节和/或预防与CRM1活动相关的生理条件，例如治疗癌症和其它肿瘤性疾病，炎性疾病，异常组织生长障碍和纤维化，包括心肌病，肺纤维化，肝纤维化，肾小球性肾炎和其他肾脏疾病，以及用于治疗病毒感染（急性和慢性）。

6. 发明申请

WO2011109799A1 NUCLEAR TRANSPORT MODULATIORS AND USES THEREOF 审中-公开
标题翻译：核运输调节器及其用途
公开(公告)号：WO2011109799A1
公开(公告)日：2011-09-09
申请号：PCT/US2011/027328
申请日：2011-03-05
申请人： KARYOPHARM THERAPEUTICS, INC. , SHECHTER, Sharon , KAUFFMAN, Michael , SANDANYAKA, Vincent, P. , SHACHAM, Sharon
发明人： SHECHTER, Sharon , KAUFFMAN, Michael , SANDANYAKA, Vincent, P. , SHACHAM, Sharon
IPC分类号： A01N57/00
CPC分类号： C07D409/04 , A61K31/4196 , A61K31/433 , A61K31/4439 , A61K31/444 , A61K31/496 , A61K31/505 , C07D207/337 , C07D231/12 , C07D233/64 , C07D249/08 , C07D257/04 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D417/04 , C07D417/12
摘要： The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).
摘要翻译：本发明一般涉及核转运调节剂（例如CRM1抑制剂）领域，更具体地涉及新的取代杂环吡咯化合物，这些化合物及其药物组合物的合成和用途，例如，在治疗，调节和/或预防与CRM1活性相关的生理病症中，例如治疗癌症和其他肿瘤病症，炎性疾病，异常组织生长和纤维化病症，包括心肌病，肺纤维化，肝纤维化，肾小球肾炎和其他肾病，并用于治疗病毒感染（包括急性和慢性）。

7. 发明申请

WO2021252900A1 BIOMARKERS FOR RESPONSE TO EXPORTIN-1 INHIBITORS IN MULTIPLE MYELOMA PATIENTS 审中-公开
公开(公告)号：WO2021252900A1
公开(公告)日：2021-12-16
申请号：PCT/US2021/037017
申请日：2021-06-11
申请人： KARYOPHARM THERAPEUTICS INC.
发明人： WALKER, Christopher , ALVAREZ, Mariano Javier , LANDESMAN, Yosef , CALIFANO, Andrea , SHEN, Yao
IPC分类号： A61K31/497 , A61P35/00
摘要： A computer-implemented method of treating a patient suffering from multiple myeloma, comprising: determining whether the patient is a responder based on an output of a classifier, wherein the input to the classifier is a feature vector comprising protein activity values corresponding to a set of proteins in the subject; and administering to the responder a therapeutically effective amount of the compound represented by structural formula (I) or a pharmaceutically acceptable salt thereof. The values and preferred values of the variables of structural formula (I) are defined herein.

8. 发明申请

WO2017117447A1 MULTICYCLIC COMPOUNDS AND USES THEREOF 审中-公开
标题翻译：多环化合物及其用途
公开(公告)号：WO2017117447A1
公开(公告)日：2017-07-06
申请号：PCT/US2016/069303
申请日：2016-12-29
申请人： KARYOPHARM THERAPEUTICS INC.
发明人： BALOGLU, Erkan
IPC分类号： C07D405/14 , C07D471/04 , A61K31/445 , A61P35/00
CPC分类号： C07D405/14 , C07D471/04
摘要： The present invention relates to multicyclic compounds containing a urea or a guanidine moiety, or pharmaceutically acceptable salts or compositions thereof represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof and pharmaceutical comopositions comprising the multicyclic compounds. The invention also relates to a method for treating a disease or disorder selected from cancer (e.g., lymphoma, such as mantle cell lymphoma), a neurodegenerative disease, an inflammatory diseases or an immune system disease (e.g., a T-Cell mediated autoimmune disesase) in a subject in need thereof. The method comprises administering to a subject in need thereof a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof, or a composition comprising a compound of the invention, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及含有脲或胍部分的多环化合物或其结构式（IA）表示的药学上可接受的盐或组合物或其药学上可接受的盐和包含该多环化合物的药物组合物。本发明还涉及治疗选自癌症（例如淋巴瘤，如套细胞淋巴瘤），神经退行性疾病，炎性疾病或免疫系统疾病（例如T细胞介导的自身免疫疾病酶）在有需要的主体中。该方法包括向有需要的受试者施用治疗有效量的本发明化合物或其药学上可接受的盐，或包含本发明化合物或其药学上可接受的盐的组合物。

9. 发明申请

WO2016025904A1 POLYMORPHS OF SELINEXOR 审中-公开
标题翻译：生物多样性
公开(公告)号：WO2016025904A1
公开(公告)日：2016-02-18
申请号：PCT/US2015/045395
申请日：2015-08-14
申请人： KARYOPHARM THERAPEUTICS INC.
发明人： AUSTAD, Brian Clinton , ROE, David, G.
IPC分类号： C07D403/12 , A61K31/497 , A61P35/00 , A61P25/00 , A61P31/00
CPC分类号： C07D403/12 , A61K31/497
摘要： The present invention relates to crystalline forms of the compound represented by Structural Formula I, and compositions comprising crystalline forms of the compound represented by Structural Formula I described herein. The crystalline forms of the compound of Structural Formula I and compositions comprising the crystalline forms of the compound of Structural Formula I provided herein, in particular, single crystalline Form A, can be incorporated into pharmaceutical compositions, which can be used to treat various disorders associated with CRM1 activity, including cancer. Also described herein are methods for preparing the compound of Structural Formula I and its single crystalline forms.
摘要翻译：本发明涉及由结构式I表示的化合物的结晶形式，以及包含本文所述的结构式I表示的化合物的结晶形式的组合物。结构式I的化合物的结晶形式和包含本文提供的结构式I的化合物，特别是单晶形式A的结晶形式的组合物可以掺入药物组合物中，其可用于治疗相关的各种疾病与CRM1活动，包括癌症。本文还描述了制备结构式I化合物及其单一结晶形式的方法。

10. 发明申请

WO2015003166A1 SUBSTITUTED BENZOFURANYL AND BENZOXAZOLYL COMPOUNDS AND USES THEREOF 审中-公开
标题翻译：取代苯并呋喃和苯并咪唑化合物及其用途
公开(公告)号：WO2015003166A1
公开(公告)日：2015-01-08
申请号：PCT/US2014/045479
申请日：2014-07-03
申请人： KARYOPHARM THERAPEUTICS INC.
发明人： BALOGLU, Erkan , SHACHAM, Sharon , SENAPEDIS, William , MCCAULEY, Dilara , LANDESMAN, Yosef , GOLAN, Gali , KALID, Ori , SHECHTER, Sharon
IPC分类号： C07D405/14 , A61K31/4427 , C07D405/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D307/81 , A61P35/00
CPC分类号： C07D405/14 , C07D307/81 , C07D405/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D491/048 , C07D491/08
摘要： The invention generally relates to substituted benzofuranyl and substituted benzoxazolyl compounds, and more particularly to a compound represented by Structural Formula (A) : or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula (A), or a pharmaceutically acceptable salt or composition thereof, e.g. , in the treatment of cancer ( e.g. , mantle cell lymphoma), and other diseases and disorders.
摘要翻译：本发明一般涉及取代的苯并呋喃基和取代的苯并恶唑基化合物，更具体地说，涉及由结构式（A）表示的化合物或其药学上可接受的盐，其中变量如本文所定义和描述。本发明还包括结构式（A）的化合物或其药学上可接受的盐或组合物的合成和用途，例如用于治疗癌症（例如，外套细胞淋巴瘤）和其它疾病和病症。

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