CA2554188A1

CA2554188A1 - Polyethylene glycol conjugates of heterocycloalkyl carboxamido propanoic acids

Polyethylene glycol conjugates of heterocycloalkyl carboxamido propanoic acids Download PDF

Info

Publication number: CA2554188A1
Authority: CA; Canada
Prior art keywords: group; substituted; poam; alkyl; conjugate
Prior art date: 2004-01-23
Legal status : Abandoned

Application number

CA002554188A

Other languages

English (en)

French (fr)

Inventor

Andrei Konradi

Michael A. Pleiss

Chris M. Semko

Jenifer L. Smith

Chris Vandevert

Current Assignee

Elan Pharmaceuticals LLC

Original Assignee

Individual

Priority date

2004-01-23

Filing date

2005-01-24

Publication date

2005-08-04

2005-01-24 Application filed by Individual filed Critical Individual

2005-08-04 Publication of CA2554188A1 publication Critical patent/CA2554188A1/en

Status Abandoned legal-status Critical Current

Links

-1 heterocycloalkyl carboxamido propanoic acids Chemical class 0.000 title claims description 221
229920001223 polyethylene glycol Polymers 0.000 title description 105
239000002202 Polyethylene glycol Substances 0.000 title description 77
235000019260 propionic acid Nutrition 0.000 title description 2
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 97
201000010099 disease Diseases 0.000 claims abstract description 88
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208000027866 inflammatory disease Diseases 0.000 claims abstract description 8
238000006243 chemical reaction Methods 0.000 claims description 102
125000005647 linker group Chemical group 0.000 claims description 99
239000000203 mixture Substances 0.000 claims description 96
238000000034 method Methods 0.000 claims description 77
125000001072 heteroaryl group Chemical group 0.000 claims description 71
125000000217 alkyl group Chemical group 0.000 claims description 63
125000003118 aryl group Chemical group 0.000 claims description 52
125000000623 heterocyclic group Chemical group 0.000 claims description 48
239000001257 hydrogen Substances 0.000 claims description 46
229910052739 hydrogen Inorganic materials 0.000 claims description 46
125000003107 substituted aryl group Chemical group 0.000 claims description 46
125000000547 substituted alkyl group Chemical group 0.000 claims description 38
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 34
125000001424 substituent group Chemical group 0.000 claims description 30
210000000265 leukocyte Anatomy 0.000 claims description 26
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 26
150000003839 salts Chemical class 0.000 claims description 26
230000027455 binding Effects 0.000 claims description 22
239000008194 pharmaceutical composition Substances 0.000 claims description 22
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 19
125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 18
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 17
108010000134 Vascular Cell Adhesion Molecule-1 Proteins 0.000 claims description 16
102100023543 Vascular cell adhesion protein 1 Human genes 0.000 claims description 16
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125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 2
125000004215 2,4-difluorophenyl group Chemical group [H]C1=C([H])C(*)=C(F)C([H])=C1F 0.000 claims description 2
125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims description 2
125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims description 2
125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims description 2
125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 claims description 2
125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims description 2
125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims description 2
125000003762 3,4-dimethoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C(OC([H])([H])[H])C([H])=C1* 0.000 claims description 2
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125000004195 4-methylpiperazin-1-yl group Chemical group [H]C([H])([H])N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims description 2
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