OA12542A - Thiazolyl-, oxazolyl-, pyrrolyl-, and imidazolyl-acid amide derivatives useful as inhibitors of PDE4isozymes. - Google Patents

Info

Publication number

OA12542A

OA12542A OA1200300177A OA1200300177A OA12542A OA 12542 A OA12542 A OA 12542A OA 1200300177 A OA1200300177 A OA 1200300177A OA 1200300177 A OA1200300177 A OA 1200300177A OA 12542 A OA12542 A OA 12542A

Authority

OA

OAPI

Prior art keywords

formula

group

alkyl

thiazole

methyl

Prior art date

2001-01-31

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• 239000003112 inhibitor Substances 0.000 title claims abstract description 64
• -1 oxazolyl- Chemical group 0.000 title claims description 213
• 125000000335 thiazolyl group Chemical group 0.000 title claims description 11
• 150000001875 compounds Chemical class 0.000 claims abstract description 287
• 125000001424 substituent group Chemical group 0.000 claims abstract description 136
• 208000006673 asthma Diseases 0.000 claims abstract description 96
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract description 96
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 93
• 238000011282 treatment Methods 0.000 claims abstract description 70
• 201000010099 disease Diseases 0.000 claims abstract description 63
• 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract description 53
• 206010006451 bronchitis Diseases 0.000 claims abstract description 45
• 229910052799 carbon Inorganic materials 0.000 claims abstract description 43
• 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims abstract description 38
• 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims abstract description 37
• 150000001721 carbon Chemical group 0.000 claims abstract description 37
• OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims abstract description 33
• 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract description 33
• 210000003979 eosinophil Anatomy 0.000 claims abstract description 23
• 229910052717 sulfur Inorganic materials 0.000 claims abstract description 22
• 229920006395 saturated elastomer Polymers 0.000 claims abstract description 14
• 206010006458 Bronchitis chronic Diseases 0.000 claims abstract description 12
• 208000007451 chronic bronchitis Diseases 0.000 claims abstract description 11
• 229910052760 oxygen Inorganic materials 0.000 claims abstract description 11
• 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims abstract description 8
• 230000004913 activation Effects 0.000 claims abstract description 8
• 125000003003 spiro group Chemical group 0.000 claims abstract description 6
• 101100296720 Dictyostelium discoideum Pde4 gene Proteins 0.000 claims abstract 3
• 101100082610 Plasmodium falciparum (isolate 3D7) PDEdelta gene Proteins 0.000 claims abstract 3
• 230000036961 partial effect Effects 0.000 claims description 162
• 125000000217 alkyl group Chemical group 0.000 claims description 124
• 239000002587 phosphodiesterase IV inhibitor Substances 0.000 claims description 87
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 86
• 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 claims description 80
• 125000001309 chloro group Chemical group Cl* 0.000 claims description 65
• 108060008682 Tumor Necrosis Factor Proteins 0.000 claims description 64
• 125000004076 pyridyl group Chemical group 0.000 claims description 62
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• 125000004093 cyano group Chemical group *C#N 0.000 claims description 49
• MZOFCQQQCNRIBI-VMXHOPILSA-N (3s)-4-[[(2s)-1-[[(2s)-1-[[(1s)-1-carboxy-2-hydroxyethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-[[2-[[(2s)-2,6-diaminohexanoyl]amino]acetyl]amino]-4-oxobutanoic acid Chemical compound OC[C@@H](C(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@@H](N)CCCCN MZOFCQQQCNRIBI-VMXHOPILSA-N 0.000 claims description 43
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• 125000003545 alkoxy group Chemical group 0.000 claims description 32
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• 125000004432 carbon atom Chemical group C* 0.000 claims description 30
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• 125000000623 heterocyclic group Chemical group 0.000 claims description 25
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• 125000004122 cyclic group Chemical group 0.000 claims description 16
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 15
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• 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims description 14
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• 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims description 13
• 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims description 13
• 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 13
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• 125000003342 alkenyl group Chemical group 0.000 claims description 12
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• 125000000842 isoxazolyl group Chemical group 0.000 claims description 12
• 238000004519 manufacturing process Methods 0.000 claims description 12
• 125000002971 oxazolyl group Chemical group 0.000 claims description 12
• 125000000714 pyrimidinyl group Chemical group 0.000 claims description 12
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• ZFXYFBGIUFBOJW-UHFFFAOYSA-N theophylline Chemical compound O=C1N(C)C(=O)N(C)C2=C1NC=N2 ZFXYFBGIUFBOJW-UHFFFAOYSA-N 0.000 claims description 12
• 206010017533 Fungal infection Diseases 0.000 claims description 11
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• 206010037660 Pyrexia Diseases 0.000 claims description 11
• 125000004603 benzisoxazolyl group Chemical group O1N=C(C2=C1C=CC=C2)* 0.000 claims description 11
• 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims description 11
• 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 claims description 11
• 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 11
• 206010035653 pneumoconiosis Diseases 0.000 claims description 11
• 125000000168 pyrrolyl group Chemical group 0.000 claims description 11
• IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 10
• 240000004808 Saccharomyces cerevisiae Species 0.000 claims description 10
• 125000003118 aryl group Chemical group 0.000 claims description 10
• 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims description 10
• 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 claims description 10
• 230000036303 septic shock Effects 0.000 claims description 10
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• 101000988419 Homo sapiens cAMP-specific 3',5'-cyclic phosphodiesterase 4D Proteins 0.000 claims description 9
• 206010022941 Iridocyclitis Diseases 0.000 claims description 9
• 101100258328 Neurospora crassa (strain ATCC 24698 / 74-OR23-1A / CBS 708.71 / DSM 1257 / FGSC 987) crc-2 gene Proteins 0.000 claims description 9
• 201000011152 Pemphigus Diseases 0.000 claims description 9
• 108010029485 Protein Isoforms Proteins 0.000 claims description 9
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• 125000003016 chromanyl group Chemical group O1C(CCC2=CC=CC=C12)* 0.000 claims description 9
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• OTZRAYGBFWZKMX-JUDRUQEKSA-N leukotriene E4 Chemical compound CCCCCC=CCC=C\C=C\C=C\[C@@H](SC[C@H](N)C(O)=O)[C@@H](O)CCCC(O)=O OTZRAYGBFWZKMX-JUDRUQEKSA-N 0.000 claims description 9
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• 125000003367 polycyclic group Chemical group 0.000 claims description 9
• 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims description 9
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• OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 claims description 9
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• 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 8
• 125000003226 pyrazolyl group Chemical group 0.000 claims description 8
• DDNTWEYNZDVVAJ-UHFFFAOYSA-N 4-(1,3-benzodioxol-5-yloxy)-1,3-thiazole-5-carboxylic acid Chemical compound S1C=NC(OC=2C=C3OCOC3=CC=2)=C1C(=O)O DDNTWEYNZDVVAJ-UHFFFAOYSA-N 0.000 claims description 7
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• 125000003037 imidazol-2-yl group Chemical group [H]N1C([*])=NC([H])=C1[H] 0.000 claims description 7
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