854044-52-3Relevant academic research and scientific papers
PROCESS FOR THE PREPARATION OF HETEROCYCLIC ESTER DERIVATIVES
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Paragraph 0144; 0145; 0146; 0147, (2014/03/21)
The present invention is directed to a process for the preparation of heterocyclic ester derivatives of formula I wherein A1, SEM, and W1 are as defined herein. Such compounds are useful as intermediates in the synthesis of derivatives useful as protein tyrosine kinase inhibitors, more particularly inhibitors of c-fms kinase.
METHOD OF INHIBITING C-KIT KINASE
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Page/Page column 34, (2008/06/13)
A method of reducing or inhibiting kinase activity of C-KIT in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to C-KIT using a compound of the present invention: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.
Cyano-substituted 2-carboxyimidazoles: Synthesis of 4-cyano-1-{[2- (trimethylsilyl)ethoxy]methyl}-1H-imidazole-2-carboxylate potassium salt
Wall, Mark J.,Schubert, Carsten,Illig, Carl R.
experimental part, p. 3377 - 3379 (2009/05/07)
The first example of a monocyano-substituted 2-carboxyimidazole is reported. A synthesis of potassium 4-cyano-1-{[2-(trimethylsilyl)ethoxy]methyl}- 1H-imidazole-2-carboxylate (2) is demonstrated where the carboxylate group is introduced via bromine-magnesium exchange on a SEM-protected cyanoimidazole followed by reaction with ethyl cyanoformate. The synthesis includes the equilibration of a regioisomeric mixture of SEM-protected imidazoles to give a single product. Georg Thieme Verlag Stuttgart.
Structure-based optimization of a potent class of arylamide FMS inhibitors
Meegalla, Sanath K.,Wall, Mark J.,Chen, Jinsheng,Wilson, Kenneth J.,Ballentine, Shelley K.,DesJarlais, Renee L.,Schubert, Carsten,Crysler, Carl S.,Chen, Yanmin,Molloy, Christopher J.,Chaikin, Margery A.,Manthey, Carl L.,Player, Mark R.,Tomczuk, Bruce E.,Illig, Carl R.
scheme or table, p. 3632 - 3637 (2009/04/06)
An anti-inflammatory 1,2,4-phenylenetriamine-containing series of FMS inhibitors with a potential to form reactive metabolites was transformed into a series with equivalent potency by incorporation of carbon-based replacement groups. Structure-based modeling provided the framework to efficiently effect this transformation and restore potencies to previous levels. This optimization removed a risk factor for potential idiosyncratic drug reactions.
INHIBITORS OF C-FMS KINASE
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Page/Page column 35, (2008/06/13)
The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
INHIBITORS OF C-FMS KINASE
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Page/Page column 23, (2008/06/13)
The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, es
INHIBITORS OF C-FMS KINASE
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Page/Page column 25, (2008/06/13)
The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, es
C-FMS KINASE INHIBITORS
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Page/Page column 41-42, (2008/06/13)
The invention is directed to compounds of Formula II: wherein A, R1, R2, R3, R4, X, Y and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.
METHOD OF INHIBITING FLT3 KINASE
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Page/Page column 60; 148-149, (2010/11/27)
A method of reducing or inhibiting kinase activity of FLT3 in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to FLT3 using a compound of the present invention (I), or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.
INHIBITORS OF C-FMS KINASE
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Page/Page column 42-43, (2008/06/13)
The invention is directed to compounds of Formula (I): wherein A, X, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula (I), are also provided.
