JP2004505084A5 - - Google Patents

Info

Publication number

JP2004505084A5

JP2004505084A5 JP2002515897A JP2002515897A JP2004505084A5 JP 2004505084 A5 JP2004505084 A5 JP 2004505084A5 JP 2002515897 A JP2002515897 A JP 2002515897A JP 2002515897 A JP2002515897 A JP 2002515897A JP 2004505084 A5 JP2004505084 A5 JP 2004505084A5

Authority

JP

Japan

Prior art keywords

alkyl

aryl

heteroaryl

alkoxy

cycloalkyl

Prior art date

2001-07-23

Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Granted

Links

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• 125000004178 (C1-C4) alkyl group Chemical group 0.000 description 16
• 150000001875 compounds Chemical class 0.000 description 16
• 125000002887 hydroxy group Chemical group [H]O* 0.000 description 14
• 229910052739 hydrogen Inorganic materials 0.000 description 13
• 239000001257 hydrogen Substances 0.000 description 13
• 125000001072 heteroaryl group Chemical group 0.000 description 11
• 125000006708 (C5-C14) heteroaryl group Chemical group 0.000 description 10
• 125000000217 alkyl group Chemical group 0.000 description 10
• 125000003118 aryl group Chemical group 0.000 description 10
• WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 description 9
• ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 9
• PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 description 9
• GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 description 9
• 229910052794 bromium Inorganic materials 0.000 description 9
• 229910052801 chlorine Inorganic materials 0.000 description 9
• 239000000460 chlorine Substances 0.000 description 9
• 125000000753 cycloalkyl group Chemical group 0.000 description 9
• 229910052731 fluorine Inorganic materials 0.000 description 9
• 239000011737 fluorine Substances 0.000 description 9
• -1 nitro, carboxyl Chemical group 0.000 description 9
• 150000003839 salts Chemical class 0.000 description 9
• 125000000229 (C1-C4)alkoxy group Chemical group 0.000 description 7
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 7
• 125000004191 (C1-C6) alkoxy group Chemical group 0.000 description 6
• 239000000203 mixture Substances 0.000 description 6
• 125000004435 hydrogen atom Chemical group [H]* 0.000 description 5
• 125000000008 (C1-C10) alkyl group Chemical group 0.000 description 4
• 125000004169 (C1-C6) alkyl group Chemical group 0.000 description 4
• 125000004093 cyano group Chemical group *C#N 0.000 description 4
• 125000006702 (C1-C18) alkyl group Chemical group 0.000 description 3
• 125000006273 (C1-C3) alkyl group Chemical group 0.000 description 3
• 125000004209 (C1-C8) alkyl group Chemical group 0.000 description 3
• IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 3
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 3
• 239000000651 prodrug Substances 0.000 description 3
• 229940002612 prodrug Drugs 0.000 description 3
• 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 description 2
• 125000004890 (C1-C6) alkylamino group Chemical group 0.000 description 2
• 125000004750 (C1-C6) alkylaminosulfonyl group Chemical group 0.000 description 2
• 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 description 2
• 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 description 2
• 125000004845 (C1-C6) alkylsulfonylamino group Chemical group 0.000 description 2
• 125000006244 carboxylic acid protecting group Chemical group 0.000 description 2
• 229920001577 copolymer Chemical group 0.000 description 2
• 229910052736 halogen Inorganic materials 0.000 description 2
• 150000002367 halogens Chemical group 0.000 description 2
• 239000003112 inhibitor Substances 0.000 description 2
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 2
• 229910052757 nitrogen Inorganic materials 0.000 description 2
• 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 description 1
• 206010003210 Arteriosclerosis Diseases 0.000 description 1
• 208000006386 Bone Resorption Diseases 0.000 description 1
• 208000024172 Cardiovascular disease Diseases 0.000 description 1
• 102100022337 Integrin alpha-V Human genes 0.000 description 1
• 206010027476 Metastases Diseases 0.000 description 1
• 208000001132 Osteoporosis Diseases 0.000 description 1
• 201000004681 Psoriasis Diseases 0.000 description 1
• 208000017442 Retinal disease Diseases 0.000 description 1
• 206010038923 Retinopathy Diseases 0.000 description 1
• 108010048673 Vitronectin Receptors Proteins 0.000 description 1
• 125000003545 alkoxy group Chemical group 0.000 description 1
• 150000001413 amino acids Chemical class 0.000 description 1
• 125000003277 amino group Chemical group 0.000 description 1
• 229940121363 anti-inflammatory agent Drugs 0.000 description 1
• 239000002260 anti-inflammatory agent Substances 0.000 description 1
• 208000011775 arteriosclerosis disease Diseases 0.000 description 1
• 125000004429 atom Chemical group 0.000 description 1
• 230000024279 bone resorption Effects 0.000 description 1
• 125000004432 carbon atom Chemical group C* 0.000 description 1
• 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 1
• 125000004122 cyclic group Chemical group 0.000 description 1
• 125000000000 cycloalkoxy group Chemical group 0.000 description 1
• 239000003937 drug carrier Substances 0.000 description 1
• 125000005842 heteroatom Chemical group 0.000 description 1
• 150000002431 hydrogen Chemical group 0.000 description 1
• 208000017169 kidney disease Diseases 0.000 description 1
• 238000004519 manufacturing process Methods 0.000 description 1
• 230000009401 metastasis Effects 0.000 description 1
• 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 1
• QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 1
• 125000004043 oxo group Chemical group O=* 0.000 description 1
• 229910052760 oxygen Inorganic materials 0.000 description 1
• 239000008194 pharmaceutical composition Substances 0.000 description 1
• 125000006239 protecting group Chemical group 0.000 description 1
• 239000002464 receptor antagonist Substances 0.000 description 1
• 229940044551 receptor antagonist Drugs 0.000 description 1
• 208000037803 restenosis Diseases 0.000 description 1
• 206010039073 rheumatoid arthritis Diseases 0.000 description 1
• 229910052717 sulfur Inorganic materials 0.000 description 1
• LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 description 1
• 230000004614 tumor growth Effects 0.000 description 1