http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-041136-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_a7f82940e47ba7a1188f8e2ffca55e0f http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_90b6a94203592576ea1f73ac2c925ec0 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-52 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-704 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-7072 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 |
| filingDate | 2003-09-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2005-05-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-041136-A1 |
| titleOfInvention | PIRAZOLOPIRIMIDINAS AS INHIBITORS OF CINLIN DEPENDENT KINASES |
| abstract | The present provides pyrazolo [1,5-a] pyrimidine compounds as cyclin dependent kinase inhibitors, methods of preparing said compounds, pharmaceutical compositions containing one or more of said compounds, methods of preparing pharmaceutical formulations comprising one or more more of said compounds, and methods of treatment, prevention, inhibition, or improvement of one or more diseases associated with CDKs, using said compounds or pharmaceutical compositions. Claim 1: A compound represented by structural formula (1), wherein: Q is -S (O2) -, -C (O) -; R is aryl or heteroaryl, wherein said aryl or heteroaryl may be unsubstituted, or optionally, independently substituted with one or more same or different portions, wherein each portion is independently selected from the group consisting of halogen, CN , -OR5, -SR5, -S (O2) R6, -S (O2) NR5R6, -NR5R6, -C (O) NR5R6, CF3, alkyl, aryl and OCF3; R2 is selected from the group comprising CN, NR5R6, -C (O2) R6, -C (O) NR5R6, -OR6, -SR6, -S (O2) R7, -S (O2) NR5R6, -N (R5 ) S (O2) R7, -N (R5) C (O) R7 and -N (R5) C (O) NR5R6; alkynyl, heteroaryl, CF3, heterocyclyl, alkylalkyl, cycloalkyl, alkyl substituted with 1 to 6 same or different R9 groups, are independently selected from the list of R9 set forth below, or is a remainder of the group of formula (2 ); R3 is selected from the group comprising H, halogen, -NR5R6, -C (O) NR5R6, alkyl, alkynyl, cycloalkyl, aryl, arylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl and heteroarylalkyl, or is a moiety of the group of formula (3 ), wherein each of said alkyl, cycloalkyl, aryl, arylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl and heteroarylalkyl for R3 and the heterocyclyl portions whose structures were shown above for R3 may be substituted or optionally, independently substituted with one or more same or different portions, wherein each portion is independently selected from the group consisting of halogen, alkyl, aryl, cycloalkyl, CF3, CN, -OCF3, - (CR4R5) nOR5, -OR5, -NR5R6, - (CR4R5 ) nNR5R6, -C (O2) R5, -C (O) R5, -C (O) NR5R6, -SR6, -S (O2) R6, -S (O2) NR5R6, -N (R5) S (O2) R7, -N (R5) C (O) R7 and -N (R5) C (O) NR5R6; R4 is H, halo or alkyl; R5 is H or alkyl; R6 is independently selected from the group comprising H, alkyl, aryl, arylalkyl, cycloalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl and heteroarylalkyl, wherein each of said alkyl, aryl, arylalkyl, cycloalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl may be unsubstituted or optionally substituted with one or more equal or different portions, wherein each portion is independently selected from the group comprising halogen, alkyl, aryl, cycloalkyl, heterocyclylalkyl, CF3, OCF3, CN, -OR5, - NR5R10, -N (R5) Boc, - (CR4R5) nOR5, -C (O2) R5, -C (O) R5, -C (O) NR5R10, -SO3H, -SR10, -S (O2) R7, - S (O2) NR5R10, -N (R5) S (O2) R7, -N (R5) C (O) R7 and -N (R5) C (O) NR5R10; R10 is selected from the group consisting of H, alkyl, aryl, arylalkyl, cycloalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, and heteroarylalkyl, wherein each of said alkyl, aryl, arylalkyl, cycloalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroaryl, and heteroaryl, they may be unsubstituted or optionally substituted with one or more equal or different portions, wherein each portion is independently selected from the group comprising halogen, alkyl, aryl, cycloalkyl, heterocyclylalkyl, CF3, OCF3, CN, -OR5, -NR4R5 , -N (R5) Boc, - (CR4R5) nOR5, -C (O2) R5, -C (O) NR4R5, -C (O) R5, -SO3H, -SR5, -S (O2) R7, -S (O2) NR4R5, -N (R5) S (O2) R7, -N (R5) C (O) R7 and -N (R5) C (O) NR4R5; or optionally, (i) R5 and R10 in the -NR5R10 portion, or (ii) R5 and R6 in the -NR5R6 portion can be joined to form a cycloalkyl or heterocyclyl portion, wherein each cycloalkyl or heterocyclyl portion is unsubstituted or optionally , independently substituted with one or more R9 groups; R7 is selected from the group consisting of alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl and heteroarylalkyl, wherein each of said alkyl, cycloalkyl, heteroarylalkyl, aryl, heteroaryl and arylalkyl may be unsubstituted or optionally substituted independently with one or more equal or different portions, wherein each portion is independently selected from the group comprising halogen, alkyl, aryl, cycloalkyl, CF3, OCF3, CN, -OR5, -NR5R10, -CH2OR5, -C (O2) R5, -C (O) NR5R10, -C (O) R5, -SR10, -S (O2) R10, -S (O2) NR5R10, -N (R5) S (O2) R10, -N (R5) C (O ) R10 and -N (R5) C (O) NR5R10; R8 is selected from the group consisting of R6, -C (O) NR5R10, -S (O2) NR5R10, -C (O) R7 and -S (O2) R7; R9 is selected from the group consisting of halogen, CN, -NR5R10, -C (O2) R6, -C (O) NR5R10, -OR6, -SR6, -S (O2) R7, -S (O2) NR5R10, -N (R5) S (O2) R7, -N (R5) C (O) R7 and -N (R5) C (O) NR5R10; m is 0 to 4; and n is 1 to 4. Claim 30: The method of claim 29, wherein said cyclin dependent kinase is CDK2. Claim 31: The method of claim 29, wherein said disease is selected from the group comprising: bladder, breast, colon, kidney, liver, lung cancer, small cell lung cancer, esophagus, gallbladder, ovary , pancreas, stomach, cervical, thyroid, prostate and skin, including squamous cell carcinoma; leukemia, acute lymphocytosis type leukemia, acute lymphoblast leukemia, B-cell lymphoma, T-cell lymphoma, Hodgkins lymphoma, non-Hodgkins lymphoma, venous cell lymphoma and Burkett lymphoma; acute and chronic myelogenous leukemia, myelodysplastic syndrome, promyelocytic leukemia; fibrosarcoma, rhabdomyosarcoma; astrocytoma, neublastoma, glioma and schwannomas; melanoma, seminoma, teratocarcinoma, osteosarcoma, xenoderoma pigmentosum, keratoacanthoma, thyroid follicular cancer and Kaposi's sarcoma. |
| priorityDate | 2002-09-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 25.