- PHARMACEUTICAL COMPOUNDS FOR THE TREATMENT OF COMPLEMENT FACTOR D MEDICAL DISORDERS
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Compounds, methods of use, and processes for making inhibitors of complement factor D or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade. The inhibitors of factor D described herein reduce the excessive activation of complement.
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Page/Page column 287; 341; 486-487
(2020/03/15)
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- Azacycle diketone compound and preparation method thereof (by machine translation)
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The invention provides a azacyclodiketone compound which is characterized by being a compound represented by the following structure. The compound has inhibitory activity on cap-dependent endonuclease. (by machine translation)
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Paragraph 0597-0600; 0603-0604
(2020/09/12)
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- Potential Antitumor Agents. 61. Structure-Activity Relationships for in Vivo Colon 38 Activity among Disubstituted 9-Oxo-9H-xanthene-4-acetic Acids
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Analogues of 9-oxo-9H-xanthene-4-acetic acid (XAA) bearing small, lipophilic 5-substituents are among the most dose-potent compounds yet reported with the capability of causing hemorrhagic necrosis of implanted colon 38 tumors in mice.To further extend structure-activity relationships among this class of compound, a series of XAA derivatives bearing two small lipophilic groups at various positions have been prepared and evaluated.The 5,6-disubstituted compounds in particular show consistently high levels of both dose potency and activity, suggesting this is the optimal configuration among substituted 9-oxo-9H-xanthene-4-acetic acids.The 5,6-dimethyl and 5-methyl-6-methoxy are the most effective analogues, showing in vivo colon 38 activity comparable to that of FAA at 10-15-fold lower doses and superior activity to FAA at the respective optimal doses, and the former has been selected for detailed evaluation.
- Rewcastle, Gordon W.,Atwell, Graham J.,Zhuang, Li,Baguley, Bruce C.,Denny, William A.
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p. 217 - 222
(2007/10/02)
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- Substituted 1,3,4,9-tetrahydropyrano(3,4-B)indole-1-acetic acids
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Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid nucleus bearing a substituent in position 1 and 4. The nucleus may be optionally substituted at positions 5, 6, 7 and 8. The derivatives are useful anti-inflammatory and analgesic agents and methods for their preparation and use are also disclosed.
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