cas 102877-78-1, 4-(4-Aminophenoxy)pyridine

Articles about 102877-78-1Total 15 be found

Identification of Diarylurea Inhibitors of the Cardiac-Specific Kinase TNNI3K by Designing Selectivity against VEGFR2, p38α, and B-Raf
A series of diarylurea inhibitors of the cardiac-specific kinase TNNI3K were developed to elucidate the biological function of TNNI3K and evaluate TNNI3K as a therapeutic target for the treatment of cardiovascular diseases. Utilizing a structure-based design, enhancements in kinase selectivity were engineered into the series, capitalizing on the established X-ray crystal structures of TNNI3K, VEGFR2, p38α, and B-Raf. Our efforts culminated in the discovery of an in vivo tool compound 47 (GSK329), which exhibited desirable TNNI3K potency and rat pharmacokinetic properties as well as promising kinase selectivity against VEGFR2 (40-fold), p38α (80-fold), and B-Raf (>200-fold). Compound 47 demonstrated positive cardioprotective outcomes in a mouse model of ischemia/reperfusion cardiac injury, indicating that optimized exemplars from this series, such as 47, are favorable leads for discovering novel medicines for cardiac diseases.
Cheung, Mui,Desai, Tina A.,Fries, Harvey,Gatto, Gregory J.,Graves, Alan P.,Holt, Dennis A.,Kallander, Lara S.,Patterson, Jaclyn R.,Shewchuk, Lisa,Stoy, Patrick,Totoritis, Rachel,Wang, Liping
p. 15651 - 15670
(2021/11/16)

MITOGEN-ACTIVATED PROTEIN KINASE INHIBITORS, METHODS OF MAKING, AND METHODS OF USE THEREOF
Compounds that inhibit mitogen-activated protein kinases (MAPKs) are disclosed. Some inhibitor compounds specifically target a single MAPK such as MAPK13, while others target multiple MAPKs such as MAPK13 and MAPK12. The compounds can be used therapeutica
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(2019/12/25)

ANTI-MUCUS DRUGS AND USES THEREFOR
Disclosed are methods of identifying, generating and synthesizing compounds that inhibit MAPK13 activity. In various embodiments, compounds, salts thereof and prodrugs thereof of the present teachings can be useful for the treatment of diseases and disord
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Paragraph 0176; 0177

(2015/07/15)

COMPOUNDS USEFUL AS ANTIBIOTIC TOLERANCE INHIBITORS
The disclosure provides compounds and pharmaceutical compositions of the compounds useful for treating chronic and acute bacterial infections. Certain of the compounds are compounds and salts of general Formula VIII Certain compounds of this disclosure are MvfR inhibitors. MvfR inhibitors reduce the formation of antibiotic tolerant bacterial strains and are useful for treating Gram-negative bacterial infections and reducing the virulence of Pseudomonas aeruginosa. Methods of treating bacterial infections in a patient, including Pseudomonas aeruginosa infections, are also provided by the disclosure.
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Page/Page column 32

(2014/11/13)

HETEROCYCLIC MODULATORS OF GPR119 FOR TREATMENT OF DISEASE
The present invention relates to compounds and methods which may be useful as inhibitors of GPR119 for the treatment or prevention of metabolic, cardiovascular, and metabolic diseases.
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Page/Page column 210

(2009/10/22)

BENZIMIDAZOLYL DERIVATIVES
The invention relates to the novel compounds of formula (I) wherein R1, R1 , L, E, G, M, Q, U, R2, m, p and q are defined as in claim 1. The novel compounds are tyrosinkinase inhibitors, especially TIE-2 inhibitors, and Ra
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Page/Page column 77

(2008/06/13)

BENZIMIDAZOLE CARBOXAMIDES AS RAF KINASE INHIBITORS
The present invention relates to benzimidazole carboxamides of formula (I), the use of the compounds of formula (I) as inhibitors of as inhibitors of one or more kinases, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient. Accordingly, the compound of Formula (I) or a pharmaceutically acceptable salt thereof is administered for the treatment of diseases mediated by one or more kinase phathways, preferably by the raf kinase pathway, especially cancers.
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Page/Page column 127-128

(2008/06/13)

SEMICARBAZIDE DERIVATIVES AS KINASE INHIBITORS
The present invention relates to semicarbazide derivatives of formula I, the use of the compounds of formula I as inhibitors of one or more kinases, the use of the compounds of formula I for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.
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Page/Page column 197-198

(2008/06/13)

MALONAMIDE DERIVATIVES
The present invention relates to malonamide derivatives of formula (I): A-D-B, the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.
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Page 163

(2010/02/10)

BISARYLUREA DERIVATIVES
The present invention relates to bisarylurea derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.
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Page/Page column 179

(2010/02/13)

Monocyclic heterocycles as kinase inhibitors
The present invention is directed to compounds having the formula and methods for using them for the treatment of cancer.
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Page/Page column 23

(2008/06/13)

OXAMIDE DERIVATIVES USEFUL AS RAF-KINASE INHIBITORS
The present invention relates to oxamide derivatives of Formula (I), the use of the compounds of Formula (I) as inhibitors of raf-kinase, the use of the compounds of Formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.
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Page 166

(2008/06/13)

GLYCINAMIDE DERIVATIVES AS RAF-KINASE INHIBITORS
The present invention relates to glycinamide derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.
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Page/Page column 152

(2008/06/13)

INHIBITION OF RAF KINASE USING QUINOLYL, ISOQUINOLYL OR PYRIDYL UREAS
This invention relates to a group of quinolyl, isoquinolyl and pyridyl ureas, their the use in treating raf mediated diseases, and pharmaceutical compositions which contain these ureas for use in such therapy.
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Page/Page column 17

(2010/11/29)

DIARYL UREA DERIVATIVES USEFUL FOR THE TREATMENT OF PROTEIN KINASE DEPENDENT DISEASES
The invention relates to the use of diaryl urea derivatives in the treatment of protein kinase dependent diseases or for the manufacture of pharmaceutical compositions for use in the treatment of said diseases, methods of use of diaryl urea derivatives in the treatment of said diseases, pharmaceutical preparations comprising diaryl urea derivatives for the treatment of said diseases, diaryl urea derivatives for use in the treatment of said diseases, novel diaryl urea derivatives, pharmaceutical preparations comprising these novel diaryl urea derivatives, processes for the manufacture of the novel diaryl urea derivatives, the use or methods of use of the novel diaryl urea derivatives as mentioned above, and/or these novel diaryl urea derivatives for use in the treatment of the animal or human body.
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Page 55

(2008/06/13)