- Pyrido[2,3-d]pyrimidin-5-ones: A novel class of antiinflammatory macrophage colony-stimulating factor-1 receptor inhibitors
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A series of pyrido[2,3-d]pyrimidin-5-ones has been synthesized and evaluated as inhibitors of the kinase domain of macrophage colony-stimulating factor-1 receptor (FMS). FMS inhibitors may be useful in treating rheumatoid arthritis and other chronic infla
- Huang, Hui,Hutta, Daniel A.,Rinker, James M.,Hu, Aping,Parsons, William H.,Schubert, Carsten,Desjarlais, Renee L.,Crysler, Carl S.,Chaikin, Margery A.,Donatelli, Robert R.,Chen, Yanmin,Cheng, Deping,Zhou, Zhao,Yurkow, Edward,Manthey, Carl L.,Player, Mark R.
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experimental part
p. 1081 - 1099
(2010/01/07)
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- Pd/C-Mediated synthesis of indoles in water
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We describe the utility of a Pd/C-Cu mediated method in the synthesis of 2,s 5-disubstituted indoles in water via a coupling-cyclization strategy. Further application of this methodology has been demonstrated in the preparation of a target indole derivative via a 7-step process the key step being the Pd/C-mediated coupling reaction.
- Layek, Mohosin,Lakshmi, Udaya,Kalita, Dipak,Barange, Deepak K.,Islam, Aminul,Mukkanti, K.,Pal, Manojit
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experimental part
(2010/04/22)
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- 5-OXO-5,8-DIHYDRO-PYRIDO-PYRIMIDINES AS INHIBITORS OF C-FMS KINASE
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The invention addresses the current need for selective and potent protein tyrosine kinase inhibitors by providing potent inhibitors of c-fms kinase. The invention is directed to the novel compounds of Formula I: or a salt, stereoisomer, tautomer, crystalline, polymorph, amorphous, solvate, hydrate, ester, prodrug or metabolite form thereof, wherein A, Y, Z, R101 and R200 are described in the specification.
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Page/Page column 98
(2008/12/05)
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- 5-Oxo-5,8-dihydro-pyrido-pyrimidines as inhibitors of c-fms kinase
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The invention addresses the current need for selective and potent protein tyrosine kinase inhibitors by providing potent inhibitors of c-fms kinase. The invention is directed to the novel compounds of Formula I: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof, wherein: W, A, Y, Z, R101 and R200 are described in the specification.
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Page/Page column 46
(2010/11/26)
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- INHIBITORS OF C-FMS KINASE
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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.
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Page/Page column 53-54
(2008/06/13)
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- PROCESS FOR PREPARING NARATRIPTAN HYDROCHLORIDE
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A process for preparing naratriptan hydrochloride, N-methyl-3-(1-methyl-4-piperidinyl)-1H-indole-5-ethanesulphonamide hydrochloride having formula (I).
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Page/Page column 16-17
(2010/02/15)
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- Synthesis and evaluation of potent and selective β3 adrenergic receptor agonists containing acylsulfonamide, sulfonylsulfonamide, and sulfonylurea carboxylic acid isosteres
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Starting from phenethanolamine aniline leads 3a and 3b, we have identified a series of functionally potent and selective β3 adrenergic receptor (AR) agonists containing acylsulfonamide, sulfonylsulfonamide, or sulfonylurea groups within the ani
- Uehling, David E.,Donaldson, Kelly H.,Deaton, David N.,Hyman, Clifton E.,Sugg, Elizabeth E.,Barrett, David G.,Hughes, Robert G.,Reitter, Barbara,Adkison, Kim K.,Lancaster, Mary E.,Lee, Frank,Hart, Robert,Paulik, Mark A.,Sherman, Bryan W.,True, Timothy,Cowan, Conrad
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p. 567 - 583
(2007/10/03)
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- Nucleosides. Part LIX. The 2-(4-nitrophenyl)ethylsulfonyl (Npes) group: A new type of protection in nucleoside chemistry
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The 2-(4-nitrophenyl)ethylsulfonyl (npes) group is developed as a new sugar OH-blocking group in the ribonucleoside series. Its cleavage can be performed in a β-eliminating process under aprotic conditions using 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) as the most effective base. Since sulfonates do not show acyl migration, partial protection of 1,2-cis-diol moieties is possible leading to new types of oligonucleotide building blocks. A series of Markiewicz-protected ribonucleosides 1-10 is converted into their 2'-O-[2-(4-nitrophenyl)ethylsulfonyl] derivatives 29-38 in which the 5'-O-Si bond can be cleaved by acid hydrolysis forming 39-45. Subsequent monomethoxytritylation leads to 46-50, and desilylation affords the 5'-O-(monomethoxytrityl)-2'-O-[2-(4-nitrophenyl)ethylsulfonyl]ribonucl eosides 51-55. Acid treatment to remove trityl groups do also not harm the npes group(→ 56-58). Unambiguous syntheses of fully blocked 2'-O-[2-(4-nitrophenyl)ethylsulfonyl]ribonucleosides 96-102 are achieved from the corresponding 3'-O-(tert-butyl)dimethylsilyl derivatives. Furthermore, various base-protected 5'-O-(monomethoxytrityl)- and 5'-O-(dimethoxytrityl)ribonucleosides, i.e. 59-77, are treated directly with 2-(4-nitrophenyl)ethylsulfonyl chloride forming in all cases a mixture of the 2',3'-di-O- and the two possible 2'- and 3'-O-monosulfonates 107-148 which can be separated into the pure components by chromatographic methods. The npes group is more labile towards DBU cleavage than the corresponding base-protecting 2-(4-nitrophenyl)ethyl (npe) and 2-(4-nitrophenyl)ethoxycarbonyl (npeoc) groups allowing selective deblocking which is of great synthetic potential.
- Pfister,Schirmeister,Mohr,Farkas,Stengele,Reiner,Dunkel,Gokhale,Charubala,Pfleiderer
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p. 1705 - 1737
(2007/10/02)
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