- POLYCYCLIC COMPOUNDS AS INHIBITORS OF BRUTON'S TYROSINE KINASE
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The present disclosure is directed to compounds of Formula (I) as Bruton's kinase inhibitors and their preparation, as well as compositions comprising compounds of Formula (I).
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Page/Page column 103; 123
(2017/07/06)
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- Novel 5-anilinoquinazoline-8-nitro derivatives as inhibitors of VEGFR-2 tyrosine kinase: Synthesis, biological evaluation and molecular docking
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Vascular endothelial growth factor receptor-2 (VEGFR-2) kinase inhibition is a well-established strategy to promptly tackle tumor growth by suppression of angiogenesis. We report herein a series of 5-anilinoquinazoline derivatives substituted by 1,3-disubstituted urea. All the newly synthesized compounds described were evaluated for VEGFR-2 kinase inhibition and antiproliferative activity against various cancer cells. The novel 1-aryl, 3-aryl-disubstituted urea quinazolines were effective VEGFR-2 kinase inhibitors with in vitro IC 50 values in the submicromolar range (compound 6f, IC50 12.0 nM), but showed a weak to moderate inhibitory activity on cancer cells. Molecular interactions of the compounds were studied using molecular docking studies. The Royal Society of Chemistry 2013.
- Xi, Liang,Zhang, Jian-Qiang,Liu, Zhi-Cheng,Zhang, Ji-Hong,Yan, Ju-Fang,Jin, Yi,Lin, Jun
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p. 4367 - 4378
(2013/08/23)
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- CYCLOHEXYLAMINES, PHENYLAMINES AND USES THEREOF
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Compounds having the formula I, their methods of synthesis, and pharmaceutically acceptable salts of certain of them are provided in which the variables have the definitions described herein. Compositions including the compounds having the formula I-A in
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- SOLUBLE EPOXIDE HYDROLASE INHIBITORS
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Disclosed are amide, thioamide, urea and thiourea compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The co
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Page/Page column 25
(2009/04/24)
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- Nucleic-acid triggered release of molecules
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It is an object of the present invention to provide a method for highly selectively releasing a molecule of interest such as an agent at a desired site while suppressing the influence of catabolic enzymes existing in vivo. The present invention provides a
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Page/Page column 14
(2009/10/06)
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- Small organic molecule regulators of cell proliferation
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The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a hedgehog agonist, such as the compounds depicted in FIGS. 32 and 33. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal ptc pathway or agonizing smoothened or hedgehog activity.
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- NICOTINAMIDE DERIVATIVES USEFUL AS PDE4 INHIBITORS
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This invention relates to nicotinamide derivatives of formula (I) and to pharmaceutical compositions containing, and the uses of such derivatives as PDE4 inhibitors wherein R7 is attached to the 3-or 4-position of the phenyl ring and is S(O)pR8, R8 is (C1-C4)alkyl optionally substituted by (C3-C6)cycloalkyl; m is 0 or 1; L is a (C3-C8)carbocyclic non-aromatic ring; and the remaining variables are as defined in the claims.
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Page/Page column 70-71
(2010/02/10)
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- Small organic molecule regulators of cell proliferation
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A compound represented in general formula (X) and (XI):
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- Small organic molecule regulators of cell proliferation
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The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a hedgehog agonist, such as the compounds depicted in FIGS. 32 and 33. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal ptc pathway or agonizing smoothened or hedgehog activity.
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- Nicotinamide derivatives and a tiotropium salt in combination for the treatment of diseases
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The invention relates to a combination of a nicotinamide derivative and tiotropium or a derivative thereof, compositions containing it and the uses of, such a combination. The combination according to the present invention is useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
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- Inhibitors of the GPib - vWF interaction
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The present invention relates to compounds of the formula I, in which R1, R2, A, B, D, E, n, m or o have the meanings indicated below. The compounds of the formula I are valuable pharmacologically active compounds. They are reversible inhibitors of the in
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- Anthranilic acid derivatives as inhibitors of the cGMP-phosphodiesterase
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Compounds of formula (I) STR1where R 1 is hydrogen; R 2 is nitro, cyano or halo(lower)alkyl; R 3 is phenyl substituted with one or more substituents selected from halogen, cyano and lower alkoxy; A is a lower alkylene group; R 4 is a group CR 6 R 7 R 8 wherein R 6 and R 7 form, together with the carbon atom to which they are attached a cycloalkyl group optionally substituted with hydroxy, lower alkoxy or a lower alkanoylamino; and R 8 is hydrogen; its prodrug and a salt thereof.
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- Small organic molecule regulators of cell proliferation
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The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a hedgehog agonist, such as the compounds depicted in FIGS. 32 and 33. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal ptc pathway or agonizing smoothened or hedgehog activity.
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- Phenol compound having antioxidative activity and the process for preparing the same
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Disclosed are a phenol compound represented by the formula (1): STR1 wherein R0 represents H, alkyl or alkyloxy; R1 represents alkyl; R2 represents alkyl or alkyloxy; OR3 represents OH; R4 represents H, lower alkyl or acyl, each of the above substituents may be substituted; W represents O, S or NR7 ; where R7 represents H, alkyl, aryl, OH or alkyloxy, a group of the formula (2): STR2 represents an amino which may be mono- or di-substituted or heterocyclic group containing N atom, or a pharmaceutically acceptable salt thereof, and a process for preparing the same.
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