- AMIDE-SUBSTITUTED HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF CONDITIONS RELATED TO THE MODULATION OF IL-12, IL-23 AND/OR IFN-ALPHA
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Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-2
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Page/Page column 192
(2020/05/29)
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- Heterocyclic compounds as TYK2 inhibitors and methods of synthesis and use
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The invention provides a heterocyclic compound serving as a TYK2 inhibitor and a synthesis and use method, and particularly provides a compound shown as a formula (I), a preparation method of the compound and application of the compound serving as the TYK2 inhibitor. The compounds of the present invention exhibit excellent inhibitory activity against TYK2.
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Paragraph 0180-0181; 0184-0186
(2020/11/23)
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- ALKYL-AMIDE-SUBSTITUTED PYRIDYL COMPOUNDS USEFUL AS MODULATORS OF IL-12, IL-23 AND/OR IFNα RESPONSES
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Compounds having the following formula I: or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα by acting on Tyk-2 to cause signal transduction inhibition.
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Page/Page column 87
(2017/09/02)
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- BICYCLO-SUBSTITUTED PYRAZOLON AZO DERIVATIVES PHARMACEUTCIAL SALTS, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF
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The present invention relates to bicyclo-substituted pyrazolon azo derivatives pharmaceutical acceptable salts of formula (I), methods for their preparation, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor. The definition of substituents in formula (I) are the same as the description.
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- NOVEL COMPOUND WITH ANTIBACTERIAL ACTIVITY
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A compound represented by the general formula (I) or a salt thereof having a potent antibacterial activity against bacteria that have acquired resistance to quinolones, and a medicament for prophylactic and/or therapeutic treatment of an infectious disease containing the compound or a salt thereof as an active ingredient, as well as a medicament for prophylactic and/or therapeutic treatment of an infectious disease containing a combination of the compound or a salt thereof, and a quinolone.
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Paragraph 0129-0130
(2016/04/26)
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- ALKYL-AMIDE-SUBSTITUTED PYRIDYL COMPOUNDS USEFUL AS MODULATORS OF IL-12, IL-23 AND/OR IFNALPHA RESPONSES
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Compounds having the following formula (I): or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα by acting on Tyk-2 to cause signal transduction inhibition.
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Paragraph 00184
(2015/05/26)
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- AMIDE-SUBSTITUTED HETEROCYCLIC COMPOUNDS USEFUL AS MODULATORS OF IL-12, IL-23 AND/OR IFN ALPHα RESPONSES
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Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNa, by acting on Tyk-2 to cause signal transduction inhibition.
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Paragraph 00172
(2014/05/24)
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- INDOLINONE ANALOGUES
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The present invention encompasses compounds of general formula (I) wherein the groups R1 to R4, A1 and A2 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
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Paragraph 0254; 0255; 0256
(2014/10/16)
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- INDOLINONE ANALOGUES AS BRD4 INHIBITORS
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The present invention encompasses compounds of general formula (I) wherein the groups R1 to R4, A1 and A2 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
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Page/Page column 55
(2014/10/15)
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- PYRIMIDINE DERIVATIVES FOR USE AS SPHINGOSINE 1-PHOSPHATE 1 (S1P1) RECEPTOR AGONISTS
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Disclosed are pyrimidine derivatives for use as a sphingosine 1-phosphate 1 (S1P1) receptor agonists, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions or diseases mediated by S1P1 receptors, particularly multiple sclerosis.
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Paragraph 0202; 0203
(2013/03/26)
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- SALTS OF BICYCLO-SUBSTITUTED PYRAZOLON AZO DERIVATIVES, PREPARATION METHOD AND USE THEREOF
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The present invention relates to pharmaceutically acceptable salts of bicycle-substituted pyrazolon azo derivatives represented by general formula (I), methods for their preparation, pharmaceutical compositions comprising the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics, and their use as agonists of thrombopoietin receptor. The definitions of substituents in general formula (I) are the same as the description.
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- PYRIMIDINE DERIVATIVES FOR USE AS SPHINGOSINE 1-PHOSPHATE 1 (S1P1) RECEPTOR AGONISTS
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Disclosed are pyrimidine derivatives for use as sphingosine 1- phosphate 1 (S1P1) receptor agonists, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions or diseases mediated by S1P1 receptors, particularly multiple sclerosis.
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Page/Page column 35
(2011/10/10)
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- DIKETOPIPERAZINE DERIVATIVES AS P2X7 MODULATORS
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The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein: A represents an aryl, heteroaryl or heterocyclyl group; and any ring or ring system of said aryl or heteroaryl is optionally substituted with 1 to 3 substituents, which may be the same or different, selected from the group consisting of halogen, C1-6 alkyl, -CF3, - OCF3, cyano, C1-6 alkoxy, -NR10R11, -X-aryl, -X-heteroaryl and -X-heterocyclyl; R1, R2, R3, R4 and R5 independently represent hydrogen, fluorine, chlorine, -CF3, cyano or C1-6 alkyl, such that at least one of R1, R2, R3, R4 and R5 is other than hydrogen; R6, R7, R8, R9, R10 and R11 independently represent hydrogen or C1-6 alkyl; X represents a linker selected from a bond, -(CH2)n- and -O-(CH2)n-; and n represents an integer from 1 to 3. The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor ("P2X7 receptor antagonists").
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Page/Page column 78-79
(2010/11/17)
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- BICYCLO-SUBSTITUTED PYRAZOLON AZO DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF
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The bicyclo-substituted pyrazolon-azo derivatives of formula (I) or pharmaceutical acceptable salts, hydrates or solvates thereof, methods for their preparation, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor are disclosed. The definition of substituents in formula (I) are the same as defined in the description.
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Page/Page column 15
(2010/10/19)
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- SUBSTITUTED PIPERIDINES FOR USE IN THE TREATMENT OF BACTERIAL INFECTIONS
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The present invention relates compounds of Formula (I) or pharmaceutically acceptable salts thereof, which are believed to possess antibacterial activity.
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Page/Page column 50
(2008/12/04)
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- Regulated activation of cell-membrane receptors by metal-chelating agonists
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Invented is a regulated activation of cell-membrane receptors by small molecule agents. Also invented is a method to render a cell-membrane receptor responsive to the activation by small molecule compounds by specific single point mutations in the transmembrane region.
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- Thrombopoietin mimetics
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Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative.
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- Theoretical Calculations of Chemical Interactions. Part 4. Aromatic Nucleophilic Substitutions and SN2 Reactions of 4- and 6-Substituted 2-Nitroanisoles
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The reactions of 4-R- and 6-R-2-nitroanisoles (R=Me, Br) in neat cyclohexylamine and piperidine have been studied.The reactions with cyclohexylamine lead to the respective aromatic nucleophilic substitution products while the reactions with piperidine mainly yield the substituted nitrophenols.It was found that 6-R-2-nitroanisoles react faster than the respective 4-R-2-nitroanisoles.The absence of the expected primary steric effect is thought to be due to the spatial arrangement of the methoxide group, which adopts a conformation perpendicular to the ring plane when it is surrounded by two ortho-substituents.CNDO and INDO calculations for different conformations of the substrates give support to this assumption.
- Nudelman, N. Sbarbati,Palleros, Daniel R.
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p. 805 - 810
(2007/10/02)
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