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BR Ref legal event code: The reaction was concentrated in vacuo and purified on reverse phase HPLC acetonitrile: Kinases either directly or indirectly participate in the signal transduction pathways of a variety of cellular activities including proliferation, adhesion, migration, differentiation and invasion. Example 9t 2-Aminoethylmethyl 2-thienyl pyrido[2,3-J]pyrimidin-7 8H -one: After 48 h, the reaction was cooled to room temperature and concentrated in vacuo.

Fused bicyclic radical includes bridged ring systems. Lactose magnesium stearate 5 Capsule Formulation The following ingredients are mixed intimately and loaded into a hard-shell gelatin capsule. The Compound of Claim 19 where R 6 is heteroaryl optionally substituted with 1, 2, or 3 R 9 groups.

Then the reaction mixture was heated to reflux and reacted for 4 h.

Full text of “Current bibliography for aquatic sciences and fisheries”

The reaction was allowed to stir for 2. Even more specifically, the cancer is ovarian cancer, cervical cancer, breast cancer, colon cancer, rectal cancer, or glioblastomas. More specifically, R 1 is hydrogen, alkyl, alkyl substituted with one or two hydroxy, alkyl substituted with alkoxy, cycloalkyl, fomrulario, or heterocycloalkylalkyl.

Alternatively, the compound of the invention is bound to the support and the protein is added. After evaporation of solvent, the residue was triturated with acetone. Learn more about our Department at http: The organic layer was dried over Formuoario 2 SO 4filtered and concentrated. The Compound of Claim 4 where R 1 is optionally substituted alkyl.


The amount of a compound of the invention which constitutes a “therapeutically effective amount” will vary depending on the compound, the disease state and its severity, the age of the patient to be treated, and the like. Tetrahedron Letters44, ; and references cited therein. Submit abstracts by October 1, using the form at http: A pharmaceutical composition which comprises a compound of Claim 1 or a pharmaceutically acceptable salt or solvate thereof and a pharmaceutically acceptable carrier, excipient, or diluent.

In particular, the invention relates to inhibitors of phosphatidylinositol 3-kinase PBK signaling pathways, and methods of their use.

Summary of the Related Art [] The connection between abnormal protein phosphorylation and the cause or consequence of diseases has been known for over 20 years. Eur J Cancer41,endometrial cancer Oda et al.

September 23, Inquiries should be directed to Dr. The compounds may also exist as geometric isomers. Then the reaction mixture is heated to reflux and reacted for approximately 15 h.

Of particular interest are screening assays for candidate agents that have a low toxicity for human cells. The second component is then added, and the presence or absence of the labeled component is followed, formularrio indicate binding. The terms “candidate bioactive agent” or “drug candidate” or grammatical equivalents as used herein describe any molecule, e. LCMS indicated no presence of starting material.

After completion of reaction, phosphorous oxychloride was removed on a rotary evaporator.


The protected derivatives of compounds of Formula I can be prepared by methods well known in the art. Yet even more specifically, R satt is phenyl, 2-phenyl-phenyl, 3 -phenyl-phenyl, 4-phenyl- phenyl, 2-fluorophenyl, 3 -fluorophenyl, 4-fluorophenyl, 2,3-difluorophenyl, 2,4- difluorophenyl, 2,5-difluorophenyl, 2,6-difluorophenyl, 3,4-difluorophenyl, 3,5-difluorophenyl, 2-chlorophenyl, 3-chlorophenyl, 4-chlorophenyl, 2,3 -dichlorophenyl, 2,4-dichlorophenyl, 2,5-dichlorophenyl, 2,6-dichlorophenyl, 3,4-dichlorophenyl, 3,5-dichlorophenyl, 3-chlorofluoro-phenyl, 2-methoxyphenyl, 3 -methoxyphenyl, formularuo, 2,3 -dimethoxyphenyl, 2,4-dimethoxyphenyl, 2,5 -dimethoxyphenyl, 2,6-dimethoxyphenyl, 3,4-dimethoxyphenyl, 3, 5 -dimethoxyphenyl, 4-phenyloxyphenyl, 2-trifluoromethylphenyl, 3 -trifluoromethylphenyl, or 4-trifluoromethylphenyl.


The crude material was purified using preparative HPLC.

US USB2 en Specifically, R 1 is hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalkyl, or optionally substituted heterocycloalkylalkyl.

These schemes are formu,ario illustrative of some methods by which the compounds of this invention can be synthesized, and various modifications to these schemes can be made and will be suggested to one skilled in the art having referred to this disclosure. OK Open in a new tab For this browsing session please remember my choice and don’t ask again. Formklario layer was dried over Na 2 SO 4 formularuo, filtered, and reduced to dryness yielding 2-aminobromo isopropylmethylpyrido[2,3-d]pyrimidin-7 8H -one as a light yellow powder 2.

The filtrate was concentrated in vacuo and purified on SiO 2 3: Specifically, R 6 is pyrazolyl, pyrazolyl, pyrazol- 5-yl, imidazolyl, imidazolyl, imidazolyl, thienyl, thienyl, thiazolyl, thiazolyl, thiazolyl, oxazolyl, oxazolyl, oxazolyl, isoxazolyl, formularko, isoxazolyl, l,2,3-oxadiazolyl, l,2,3-oxadiazolyl, l,3,4-oxadiazolyl, 1,2,4- oxadiazolyl, l,2,4-oxadiazolyl, furanyl, furanyl, pyrrolyl, pyrrolyl, triazol- 4-yl, triazolyl, or tetrazolyl; each of which is optionally substituted with one R 9 where R 9when present, is methyl, benzyl, cyano, phenyl, or iV-fert-butoxycarbonyl.