CA2603748A1

CA2603748A1 - C-met modulators and methods of use

C-met modulators and methods of use Download PDF

Info

Publication number: CA2603748A1
Authority: CA; Canada
Prior art keywords: optionally substituted; compound according; substituted lower; ring system; lower alkyl
Prior art date: 2005-04-06
Legal status : Abandoned

Application number

CA002603748A

Other languages

English (en)

French (fr)

Inventor

Timothy Patrick Forsyth

Morrison B. Mac

James William Leahy

John M. Nuss

Wei Xu

Current Assignee

Exelixis Inc

Original Assignee

Individual

Priority date

2005-04-06

Filing date

2006-04-06

Publication date

2006-10-12

2006-04-06 Application filed by Individual filed Critical Individual

2006-10-12 Publication of CA2603748A1 publication Critical patent/CA2603748A1/en

Status Abandoned legal-status Critical Current

Links

238000000034 method Methods 0.000 title claims abstract description 116
150000001875 compounds Chemical class 0.000 claims abstract description 233
239000000203 mixture Substances 0.000 claims abstract description 144
230000000694 effects Effects 0.000 claims abstract description 69
102000001253 Protein Kinase Human genes 0.000 claims abstract description 20
108060006633 protein kinase Proteins 0.000 claims abstract description 20
230000001413 cellular effect Effects 0.000 claims abstract description 9
125000000217 alkyl group Chemical group 0.000 claims description 94
-1 napthyl Chemical group 0.000 claims description 93
125000004122 cyclic group Chemical group 0.000 claims description 87
229920006395 saturated elastomer Polymers 0.000 claims description 79
IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 68
108091000080 Phosphotransferase Proteins 0.000 claims description 64
102000020233 phosphotransferase Human genes 0.000 claims description 64
239000003795 chemical substances by application Substances 0.000 claims description 62
102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 claims description 59
108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 claims description 59
229910052736 halogen Inorganic materials 0.000 claims description 54
150000002367 halogens Chemical class 0.000 claims description 54
125000003107 substituted aryl group Chemical group 0.000 claims description 46
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208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 44
125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 44
OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 43
229910052757 nitrogen Inorganic materials 0.000 claims description 43
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125000004429 atom Chemical group 0.000 claims description 39
201000010099 disease Diseases 0.000 claims description 38
125000005842 heteroatom Chemical group 0.000 claims description 38
125000004093 cyano group Chemical group *C#N 0.000 claims description 37
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125000000623 heterocyclic group Chemical group 0.000 claims description 33
GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims description 30
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125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 28
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238000006467 substitution reaction Methods 0.000 claims description 17
125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 16
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239000008194 pharmaceutical composition Substances 0.000 claims description 11
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230000002159 abnormal effect Effects 0.000 claims description 9
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208000035475 disorder Diseases 0.000 claims description 6
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125000005061 octahydroisoindolyl group Chemical group C1(NCC2CCCCC12)* 0.000 claims description 3
125000001715 oxadiazolyl group Chemical group 0.000 claims description 3
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125000005968 oxazolinyl group Chemical group 0.000 claims description 3
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125000001484 phenothiazinyl group Chemical group C1(=CC=CC=2SC3=CC=CC=C3NC12)* 0.000 claims description 3
125000001644 phenoxazinyl group Chemical group C1(=CC=CC=2OC3=CC=CC=C3NC12)* 0.000 claims description 3
125000003373 pyrazinyl group Chemical group 0.000 claims description 3
125000003072 pyrazolidinyl group Chemical group 0.000 claims description 3
125000003226 pyrazolyl group Chemical group 0.000 claims description 3
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125000000714 pyrimidinyl group Chemical group 0.000 claims description 3
125000000168 pyrrolyl group Chemical group 0.000 claims description 3
125000005493 quinolyl group Chemical group 0.000 claims description 3
125000004853 tetrahydropyridinyl group Chemical group N1(CCCC=C1)* 0.000 claims description 3
125000001113 thiadiazolyl group Chemical group 0.000 claims description 3
125000001984 thiazolidinyl group Chemical group 0.000 claims description 3
125000002769 thiazolinyl group Chemical group 0.000 claims description 3
125000000335 thiazolyl group Chemical group 0.000 claims description 3
125000001544 thienyl group Chemical group 0.000 claims description 3
125000001425 triazolyl group Chemical group 0.000 claims description 3
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239000003937 drug carrier Substances 0.000 claims description 2
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