- 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS
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Compounds according to formula I are useful as agonists of Toll-like receptor 7 (TLR7). Such compounds can be used in cancer treatment, especially in combination with an anti-cancer immunotherapy agent, or as a vaccine adjuvant.
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Paragraph 00197
(2021/08/06)
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- TETRAZOLINONE COMPOUND AND USE THEREFOR
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A tetrazolinone compound represented by formula (1): wherein R1 and R2 are the same or different and represent a hydrogen atom, etc.; R3 represents a C1-C6 alkyl group, etc.; R4, R5, and R6 are the same or different and represent a hydrogen atom, etc.; A represents a C6-C10 aryl group optionally having one or more atoms or groups selected from Group P1, etc.; Q represents the following group Q1; and X represents an oxygen atom, has excellent control activity against pests.
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Paragraph 0641; 0642
(2016/07/05)
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- Tetrazolinone compound, and use therefor
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A tetrazolinone compound represented by formula (1) (in the formula, R1 and R2 are the same or different, and represent a hydrogen atom, or the like; R3 represents a C1-C6 alkyl group, or the like; R4, R5 and R6 are the same or different, and represent a hydrogen atom, or the like; A represents a C6-C10 aryl group, or the like, which may have one or more atoms or groups selected from group (P1); Q represents group (Q1), or the like; and X represents an oxygen atom, or the like). The tetrazolinone compound has an excellent pest-control effect.
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Paragraph 1015; 1016; 1017; 1018
(2016/10/08)
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- TRICYCLIC PIPERIDINE COMPOUNDS
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The present invention relates to compounds of the formula (I) wherein R1a, R1b, R2, R3, (R4)n and ring (A) are as described in the description, to their preparation, to pharmaceutically acc
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Page/Page column 86
(2016/11/21)
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- TRICYCLIC PIPERIDINE COMPOUNDS
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The present invention relates to compounds of the formula (I), wherein R, R1a, R1b, R2, R3, and X are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), to methods for the preparation of such compounds of formula (I), and especially to their use as TPH modulators.
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Page/Page column 143-144
(2015/06/08)
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- PYRAN-SPIROCYCLIC PIPERIDINE AMIDES AS MODULATORS OF ION CHANNELS
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The invention relates to pyran spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the composition
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Paragraph 00259; 00260
(2013/07/31)
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- TRIAZOLONE COMPOUNDS AND USES THEREOF
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The invention disclosed herein is directed to compounds of Formula (I) and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula (I), or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to methods of treating prostate, breast, ovarian, liver, kidney, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention disclosed herein is further directed to methods of treating prostate, breast, colon, pancreatic, chronic lymphocytic leukemia, melanoma and other cancers comprising administration of a of a therapeutically effective amount of a selective PPARα antagonist. The compounds and pharmaceutical compositions of the invention are also useful in the treatment of viral infections, such as HCV infections and HIV infections. The invention disclosed herein is also directed to a methods of preventing the onset of and/or recurrence of acute and chronic myeloid leukemia, as well as other cancers, comprising administration of a of a therapeutically effective amount of a selective PPARα antagonist.
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Paragraph 00321
(2013/09/26)
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- CHROMAN - SPIROCYCLIC PIPERIDINE AMIDES AS MODULATORS OF ION CHANNELS
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The invention relates to chroman spirocyclic piperidine amide derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
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Page/Page column 153
(2012/09/10)
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- MORPHOLINE-SPIROCYCLIC PIPERIDINE AMIDES AS MODULATORS OF ION CHANNELS
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The invention relates to morpholine spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
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Page/Page column 138-139
(2012/10/07)
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- PYRROLOPYRAZINE-SPIROCYCLIC PIPERIDINE AMIDES AS MODULATORS OF ION CHANNELS
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The invention relates to pyrrolopyrazine-spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
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Paragraph 0335; 0336; 0337
(2013/03/26)
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- BENZIMIDAZOLE COMPOUNDS
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There is provided a compound of the formula (1) wherein R1 is an optionally substituted C1-10 alkyl; R2 is H, or a C1-6 alkyl which may be substituted with 1 to 3 substituents; R3 is a 5- or 6-membered aromatic group which may be substituted with 1 to 5 substituents, wherein the 5- or 6-membered aromatic group may be fused with a 5- or 6- membered ring which may be substituted with 1 to 3 C1-6 alkyls; R4 is a hydrogen, a halogen, a hydroxy, a cyano, a C1-6 alkyl or a C1-6 alkoxy; Z is -O-, -S-, -SO-, -SO2-, or - NR5- wherein R5 is a hydrogen or a C1-6 alkyl; or a salt thereof or a prodrug thereof, which have CRF receptor antagonist activity and use thereof.
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Page/Page column 90-91; 112
(2008/12/05)
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- Efficient regioselective preparation of monobromo and bromoiodo hydroxy pyridines from dibromoderivatives via bromine-lithium exchange
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Annular dibromination of hydroxypyridines with NBS in acetonitrile followed by bromine-lithium exchange with RLi and subsequent trapping with H2O or I2 afforded monobromo and bromoiodo derivatives in a completely regioselective way. Iodination of bromo hydroxypyridines with NIS is totally regioselective.
- Meana, ángela,Rodríguez, Justo F.,Sanz-Tejedor, M. Ascensión,García-Ruano, José L.
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p. 1678 - 1682
(2007/10/03)
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- Halogenation of pyridinols using bis(sym-collidine)iodine(I) and bis(sym-collidine)bromine(I) hexafluorophosphate
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Iodination and bromination of pyridinols was achieved by action of the title reagents in methylene chloride.
- Rousseau, Gerard,Robin, Sylvie
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p. 2467 - 2470
(2007/10/03)
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