- Skipped Fluorination Motifs: Synthesis of Building Blocks and Comparison of Lipophilicity Trends with Vicinal and Isolated Fluorination Motifs
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Given there is an optimal lipophilicity range for orally bioavailable drugs, structural modifications applied in the drug development process are not only focused on optimizing bioactivity but also on fine-tuning lipophilicity. Fluorine introduction can b
- Troup, Robert I.,Jeffries, Benjamin,Saudain, Raphael El-Bekri,Georgiou, Eleni,Fish, Johanna,Scott, James S.,Chiarparin, Elisabetta,Fallan, Charlene,Linclau, Bruno
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p. 1882 - 1900
(2021/02/03)
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- TREATMENT OF RESPIRATORY DISEASES WITH AMINO ACID COMPOUNDS
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The invention relates to methods of therapy using compounds of formula (I) and formula (II): or a salt thereof, wherein R1, R2, R10, R11, R12, R13, R14, R15, R16, q and p are as described herein. Compounds of formula (II) and pharmaceutical compositions thereof are integrin inhibitors that are useful in therapy for a condition, for example, caused by or associated with an infectious agent, shock, pancreatitis, or trauma. The condition can include one or more of pulmonary fibrosis associated with rheumatoid arthritis or progressive familial intrahepatic cholestasis (PFIC).
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Paragraph 0766
(2021/11/13)
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- DOSAGE FORMS AND REGIMENS FOR AMINO ACID COMPOUNDS
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The invention relates to dosage forms for daily administration of compounds of formula (A) and formula (I): or a salt thereof, wherein R1, R2, R10, R11, R12, R13, R14, R15, R16, q and p are as described herein. Compounds of formula (A), formula (I), and pharmaceutical compositions thereof are ανβ6 integrin inhibitors that are useful for treating fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP),
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Paragraph 001163
(2020/10/21)
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- AMINO ACID COMPOUNDS AND METHODS OF USE
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The invention relates to compounds of formula (A) and formula (I): or a salt thereof, wherein R1, R2, R10, R11, R12, R13, R14, R15, R16, q and p are as described herein. Compounds of formula (A), formula (I), and pharmaceutical compositions thereof are αvβ6 integrin inhibitors that are useful for treating fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).
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Paragraph 1447
(2019/09/20)
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- PRODUCTION METHOD OF INTERMEDIATE COMPOUND FOR SYNTHESIZING MEDICAMENT
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The present invention relates to a novel method for preparing a compound of formula (2) as the intermediate, which can be effectively used for preparation of a compound of formula (1) exhibiting good inhibitory activity against dipeptidyl peptidase IV enz
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Paragraph 0101; 0102; 0103
(2013/07/05)
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- PRODUCTION METHOD OF INTERMEDIATE COMPOUND FOR SYNTHESIZING MEDICAMENT
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The present invention relates to a novel method for preparing a compound of formula (2) as the intermediate, which can be effectively used for preparation of a compound of formula (1) exhibiting good inhibitory activity against dipeptidyl peptidase IV enz
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Page/Page column 12
(2012/03/26)
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- Certain fluorine substituted PGI2 compounds
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Prostaglandin and prostacyclin compounds which are fluorine substituted in any one or more of the following positions, 4,4; 7,7; 10,10; and 5.
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