- Neoplastic diseases and/or infectious diseases is useful bicyclic [...] derivatives (by machine translation)
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The present invention relates to bicyclic tetrahydrothiazepine of formula (I), wherein R1 to R3, X1, X2 and R18 have the meaning as indicated in the description and claims. The invention further relates to pharmaceutical compositions comprising such compo
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Paragraph 0212; 0213
(2018/05/15)
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- Sulfamide derivative and application thereof
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The invention relates to a sulfamide derivative and a pharmaceutical composition comprising the compound as well as use of the sulfamide derivative and the pharmaceutical composition as a preparation drug, in particular, use of a drug for preparing a BCL-2 family protein antagonist and use of the drug for treating cancers.
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Paragraph 0203; 0204
(2017/08/29)
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- Conformation-based restrictions and scaffold replacements in the design of hepatitis C virus polymerase inhibitors: Discovery of deleobuvir (BI 207127)
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Conformational restrictions of flexible torsion angles were used to guide the identification of new chemotypes of HCV NS5B inhibitors. Sites for rigidification were based on an acquired conformational understanding of compound binding requirements and the roles of substituents in the free and bound states. Chemical bioisosteres of amide bonds were explored to improve cell-based potency. Examples are shown, including the design concept that led to the discovery of the phase III clinical candidate deleobuvir (BI 207127). The structure-based strategies employed have general utility in drug design.
- LaPlante, Steven R.,B?s, Michael,Brochu, Christian,Chabot, Catherine,Coulombe, René,Gillard, James R.,Jakalian, Araz,Poirier, Martin,Rancourt, Jean,Stammers, Timothy,Thavonekham, Bounkham,Beaulieu, Pierre L.,Kukolj, George,Tsantrizos, Youla S.
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supporting information
p. 1845 - 1854
(2014/04/03)
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- TRICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS
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The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as m PGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (m PGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
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Page/Page column 57; 60
(2013/11/05)
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- Tricyclic Compounds As mPGES-1 Inhibitors
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The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
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Page/Page column 31
(2012/05/07)
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- Substituted Fused Imidazole Derivatives, Pharmaceutical Compositions, and Methods of Use Thereof
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Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.
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Page/Page column 116; 123
(2011/09/14)
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- CCR5 ANTAGONISTS AS THERAPEUTIC AGENTS
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The present invention relates to compounds useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acq
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Page/Page column 22
(2009/07/17)
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- CCR5 ANTAGONISTS AS THERAPEUTIC AGENTS
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The present invention relates to compounds useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acq
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Page/Page column 22-23
(2009/06/27)
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- CCR5 ANTAGONISTS AS THERAPEUTIC AGENTS
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The present invention relates to compounds useful in the treatment of CCR5-related diseases and disorders, for example, useful in the inhibition of HIV replication, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).
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Page/Page column 11-12
(2009/06/27)
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- INHIBITORS OF SERINE PALMITOYLTRANSFERASE
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This invention provides compounds of the formula (I) useful in the inhibition or modulation of serine palmitoyl transferase and their use in methods of treatment or amelioration of type 2 diabetes, type 1 diabetes, insulin resistance, the effects of obesity, metabolic syndrome (sometimes referred to as Syndrome X), impaired glucose tolerance, Cushing's disease, cardiovascular disease, prothrombotic conditions, myocardial infarction, hypertension, congestive heart failure, cardiomyopathy, atherosclerosis, dyslipidemia, sepsis, liver damage, retinal degenerative disorders, cachexia, emphysema, hepatitis C infections, HIV infections and inflammatory disorders and useful in methods for raising HDL plasma levels in a mammal. The compounds of this invention can also be used to prevent damage or loss of pancreatic islet beta cells (such as in the case of pancreatic beta cell apoptosis, including those related to insulin-dependent diabetes mellitus).
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Page/Page column 28
(2008/12/07)
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- VIRAL POLYMERASE INHIBITORS
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The present invention relates to compounds represented by formula (I) wherein A, B, D, E, R2, R3, R4, R5, R6, R9, a, b, d and e are as defined herein, their salt or ester and pharmaceutical compositions thereof useful in the treatment of hepatitis C viral (HCV) infection. Said compounds were found to have inhibitory activity against HCV polymerase, especially as inhibitors of HCV NS5B polymerase
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Page/Page column 45
(2010/11/26)
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- FUSED HETEROCYCLIC COMPOUND HAVING ANTI-HCV EFFECT
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Disclosed is a compound represented by the formula (I) below, a pharmaceutically acceptable salt thereof, or a solvate of them. (I) (In the formula, A represents N or CH; Het represents any one of the following groups: (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k) wherein R0 and R respectively represent a hydrogen, an optionally substituted alkyl, an optionally substituted cycloalkyl, an optionally substituted aryl or the like; R1 and R2 respectively represent a hydrogen, an optionally substituted alkyl, an optionally substituted alkenyl, an optionally substituted cycloalkyl, an optionally substituted aryl, an optionally substituted heteroaryl or the like; p is an integer of 0-3; and R3 represents an optionally substituted alkyl or the like.)
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Page/Page column 227-228
(2010/02/15)
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- Method of inhibiting amyloid protein aggregation and imaging amyloid deposits
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The present invention provides a method of treating Alzheimer's disease using a compound of Formula I Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of Formula I and a method of imaging amyloid deposits, as we
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- Descriptive Photochemistry of Polyfluorinated Azide Derivatives of Methyl Benzoate
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The photochemistry of several polyfluorinated azide derivatives of methyl benzoate have been studied in a variety of solvents.We have photolyzed methyl 3-azido-6-fluorobenzoate, methyl 3-azido-4-fluorobenzoate, methyl 4-azido-2-fluorobenzoate, methyl 3-azido-2,4-difluorobenzoate, methyl 3-azido-2,6-difluorobenzoate, methyl 3-azido-2,4,6-trifluorobenzoate, and methyl 4-azido-2,3,5,6-tetrafluorobenzoate in toluene, cyclopentane, tetramethylethylene, diethylamine, dimethyl sulfide, dimethyl disulfide, and methanol in an attempt to capture the photogenerated reactive intermediates.Adducts were not formed in cyclopentane, dimethyl disulfide, and methanol solvents.Adducts were formed, however, but in modest yields, in the other solvents.In general the yield of adducts increases with the number of fluorine substituents present, and ortho and para fluorine substituents relative to the azide group are more effective in enhancing the yield of adducts relative to meta fluorine substitution.
- Soundararajan, N.,Platz, Matthew S.
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p. 2034 - 2044
(2007/10/02)
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