944902-31-2Relevant academic research and scientific papers
PHARMACEUTICAL COMPOSITIONS AND COMBINATIONS COMPRISING INHIBITORS OF THE ANDROGEN RECEPTOR AND USES THEREOF
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Paragraph 0329-0330, (2022/04/03)
The present disclosure generally relates to pharmaceutical compositions and combinations comprising N-(4-((4-(2-(3-chloro-4-(2-chloroethoxy)-5-cyanophenyl)propan-2-yl)phenoxy) methyl)pyrimidin-2-yl)methanesulfonamideN-(4-((4-(2-(3-chloro-4-(2-chloroethoxy)-5-cyanophenyl) propan-2-yl) phenoxy) methyl)pyrimidin-2-yl)methanesulfonamide or a pharmaceutically acceptable salt, solvate, stereoisomer, or prodrug thereof, and a second therapeutically active agent, such as an anti androgen. In particular, the present disclosure relates to pharmaceutical compositions and combinations useful for treatment of various cancers, for example breast cancer and prostate cancer.
Discovery of IACS-9439, a Potent, Exquisitely Selective, and Orally Bioavailable Inhibitor of CSF1R
Czako, Barbara,Marszalek, Joseph. R.,Burke, Jason P.,Mandal, Pijus,Leonard, Paul G.,Cross, Jason B.,Mseeh, Faika,Jiang, Yongying,Chang, Edward Q.,Suzuki, Erika,Kovacs, Jeffrey J.,Feng, Ningping,Gera, Sonal,Harris, Angela L.,Liu, Zhen,Mullinax, Robert A.,Pang, Jihai,Parker, Connor A.,Spencer, Nakia D.,Yu, Simon S.,Wu, Qi,Tremblay, Martin R.,Mikule, Keith,Wilcoxen, Keith,Heffernan, Timothy P.,Draetta, Giulio F.,Jones, Philip
, p. 9888 - 9911 (2020/10/19)
Tumor-associated macrophages (TAMs) have a significant presence in the tumor stroma across multiple human malignancies and are believed to be beneficial to tumor growth. Targeting CSF1R has been proposed as a potential therapy to reduce TAMs, especially the protumor, immune-suppressive M2 TAMs. Additionally, the high expression of CSF1R on tumor cells has been associated with poor survival in certain cancers, suggesting tumor dependency and therefore a potential therapeutic target. The CSF1-CSF1R signaling pathway modulates the production, differentiation, and function of TAMs; however, the discovery of selective CSF1R inhibitors devoid of type III kinase activity has proven to be challenging. We discovered a potent, highly selective, and orally bioavailable CSF1R inhibitor, IACS-9439 (1). Treatment with 1 led to a dose-dependent reduction in macrophages, promoted macrophage polarization toward the M1 phenotype, and led to tumor growth inhibition in MC38 and PANC02 syngeneic tumor models.
ANDROGEN RECEPTOR MODULATORS AND METHODS FOR THEIR USE
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Paragraph 1085; 1086, (2020/05/06)
The present invention relates to compounds of formula (I)-(VI) and/or (A)-(H-I), or any subgenera thereof, or a pharmaceutically acceptable salt, tautomer or stereoisomer. The compounds of the present disclosure are useful in modulating androgen receptor activity and for treating cancer including prostate cancer.
SMALL MOLECULE INHIBITORS OF COLONY STIMULATING FACTOR-1 RECEPTOR (CSF-1R) AND USES THEREOF
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Page/Page column 171, (2018/07/29)
Compounds of formula (I), which are useful as CSF-1R inhibitors, are provided. Also provided are pharmaceutical compositions and kits comprising said compounds, as well as methods and uses pertaining to said compounds.
GLUCOSYLCERAMIDE SYNTHASE INHIBITORS
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Page/Page column 224; 225, (2014/04/03)
The invention relates to inhibitors of glucosylceramide synthase (GCS) useful for the treatment of metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, cystic disease and for the treatment of cancer.
HETEROCYCLES CAPABLE OF MODULATING T-CELL RESPONSES, AND METHODS OF USING SAME
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Paragraph 00154; 00155, (2014/01/07)
The present disclosure is directed in part to heterocycles, and their use in treating medical disorders, such as immune inflammatory disorders such as Crohn's disease, ulcerative colitis, rheumatic disorders, psoriasis, and allergies. The compounds are co
Novel HIV reverse transcriptase inhibitors
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Page/Page column 41-42, (2008/06/13)
The invention is related to compounds of Formula (I), (II), or (III): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
PHARMACOLOGICALLY ACTIVE GUANIDINE COMPOUNDS
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, (2008/06/13)
The compounds are substituted thioalkyl-, aminoalkyl-and oxyalkyl-guanidines which are inhibitors of histamine activity.
PHARMACOLOGICALLY ACTIVE THIOUREA AND UREA COMPOUNDS
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, (2008/06/13)
The compounds are substituted thioalkyl-, aminoalkyl-and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity.
