- Compound for treating ulcerative colitis as well as preparation method and application thereof
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The invention provides a compound for treating ulcerative colitis. The compound has a structure as shown in a formula I. The compound provided by the invention can significantly inhibit abnormal secretion of TNF-alpha, IL-1[beta], IL-6 and other proinflammatory factors in colon tissues when colitis happens, inhibit inflammatory cell infiltration, maintain the integrity of intestinal epithelium and crypt gland, effectively relieve inflammation, and improve the symptoms of colon shortening and intestinal wall thickening, has excellent potential application value in preparation of medicines for treating ulcerative colitis, and provides a new choice for clinic.
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Paragraph 0049; 0051; 0056; 0075-0076
(2021/05/19)
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- COMPOUNDS USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS
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The present invention relates to certain compounds 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, a disease or disorder mediated by lymphocytes, an autoimmune disease or disorder, an inflammatory disease or disorder, an inflammatory skin disease or disorder, cancer, psoriasis, atopic dermatitis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, and acne, microbial infections or diseases and viral infections or diseases.
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- Discovery of APD334: Design of a clinical stage functional antagonist of the sphingosine-1-phosphate-1 receptor
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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
- 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.
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supporting information
p. 1313 - 1317
(2015/01/09)
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- 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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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).
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- 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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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.
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Page/Page column 57
(2010/04/03)
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