957205-39-9Relevant academic research and scientific papers
AROMATIC RING DERIVATIVE AS IMMUNOREGULATION AND PREPARATION METHOD AND APPLICATION OF AROMATIC RING DERIVATIVE
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, (2021/10/15)
Relating to a compound represented by formula (I) and a pharmaceutically acceptable salt of the compound, and an application of the compound as an S1P1 agonist.
An Efficient Scale-Up Process for the Preparation of the APD334 Precursor 4-Chloromethyl-1-cyclopentyl-2-(trifluoromethyl)benzene
Sengupta, Dipanjan,Gharbaoui, Tawfik,Krishnan, Ashwin,Buzard, Daniel J.,Jones, Robert M.,Ma, You-An,Burda, Robert,Garrido Montalban, Antonio,Semple, Graeme
, p. 618 - 623 (2015/06/30)
Synthetic studies of the APD334 precursor 4-chloromethyl-1-cyclopentyl-2-(trifluoromethyl)benzene (6) are described. A two-step scalable process was developed starting from commercially available and inexpensive starting materials. An iron(III) chloride-c
Discovery of APD334: Design of a clinical stage functional antagonist of the sphingosine-1-phosphate-1 receptor
Buzard, Daniel J.,Kim, Sun Hee,Lopez, Luis,Kawasaki, Andrew,Zhu, Xiuwen,Moody, Jeanne,Thoresen, Lars,Calderon, Imelda,Ullman, Brett,Han, Sangdon,Lehmann, Juerg,Gharbaoui, Tawfik,Sengupta, Dipanjan,Calvano, Lorene,Montalban, Antonio Garrido,Ma, You-An,Sage, Carleton,Gao, Yinghong,Semple, Graeme,Edwards, Jeff,Barden, Jeremy,Morgan, Michael,Chen, Weichao,Usmani, Khawja,Chen, Chuan,Sadeque, Abu,Christopher, Ronald J.,Thatte, Jayant,Fu, Lixia,Solomon, Michelle,Mills, David,Whelan, Kevin,Al-Shamma, Hussien,Gatlin, Joel,Le, Minh,Gaidarov, Ibragim,Anthony, Todd,Unett, David J.,Blackburn, Anthony,Rueter, Jaimie,Stirn, Scott,Behan, Dominic P.,Jones, Robert M.
, p. 1313 - 1317 (2015/01/09)
APD334 was discovered as part of our internal effort to identify potent, centrally available, functional antagonists of the S1P1 receptor for use as next generation therapeutics for treating multiple sclerosis (MS) and other autoimmune diseases
PROCESSES FOR THE PREPARATION OF (R)-2-(7-(4-CYCLOPENTYL-3-(TRIFLUOROMETHYL)BENZYLOXY)-1,2,3,4-TETRAHYDROCYCLOPENTA[B]INDOL-3-YL)ACETIC ACID AND SALTS THEREOF
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, (2011/08/21)
The present invention relates to processes and intermediates useful in the preparation of of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (Ia) and salts thereof, an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis).
2H-CHROMENE COMPOUND AND DERIVATIVE THEREOF
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Page/Page column 25; 54; 131, (2011/09/12)
[Object] Provided is a compound which has an excellent S1P1 agonist action, and is useful particularly as an active ingredient for an agent for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease ind
SUBSTITUTED 1,2,3,4- TETRAHYDROCYCLOPENTA[b]INDOL-3-YL) ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS
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Page/Page column 56, (2010/04/03)
The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.
