TW200800234A - Piperazine derivatives useful as CCR5 antagonists - Google Patents

Info

Publication number

TW200800234A

TW200800234A TW095138842A TW95138842A TW200800234A TW 200800234 A TW200800234 A TW 200800234A TW 095138842 A TW095138842 A TW 095138842A TW 95138842 A TW95138842 A TW 95138842A TW 200800234 A TW200800234 A TW 200800234A

Authority

TW

Taiwan

Prior art keywords

etoac

compound

mmol

doc

solution

Prior art date

2005-10-21

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• 101710149870 C-C chemokine receptor type 5 Proteins 0.000 title abstract description 22
• 102100035875 C-C chemokine receptor type 5 Human genes 0.000 title abstract description 22
• 239000005557 antagonist Substances 0.000 title abstract description 14
• 150000004885 piperazines Chemical class 0.000 title 1
• 229940066771 systemic antihistamines piperazine derivative Drugs 0.000 title 1
• 150000001875 compounds Chemical class 0.000 claims abstract description 172
• 150000003839 salts Chemical class 0.000 claims abstract description 64
• 239000007787 solid Substances 0.000 claims abstract description 47
• 238000011282 treatment Methods 0.000 claims abstract description 46
• 239000003795 chemical substances by application Substances 0.000 claims abstract description 13
• 201000010099 disease Diseases 0.000 claims abstract description 13
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 13
• 239000003443 antiviral agent Substances 0.000 claims abstract description 11
• 208000022559 Inflammatory bowel disease Diseases 0.000 claims abstract description 10
• 206010020751 Hypersensitivity Diseases 0.000 claims abstract description 9
• 206010052779 Transplant rejections Diseases 0.000 claims abstract description 9
• 230000007815 allergy Effects 0.000 claims abstract description 9
• 206010003246 arthritis Diseases 0.000 claims abstract description 9
• 210000000056 organ Anatomy 0.000 claims abstract description 9
• 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 9
• 206010039073 rheumatoid arthritis Diseases 0.000 claims abstract description 9
• 201000004681 Psoriasis Diseases 0.000 claims abstract description 8
• 208000006673 asthma Diseases 0.000 claims abstract description 7
• 201000006417 multiple sclerosis Diseases 0.000 claims abstract description 7
• 206010012438 Dermatitis atopic Diseases 0.000 claims abstract description 5
• 201000008937 atopic dermatitis Diseases 0.000 claims abstract description 5
• 238000000034 method Methods 0.000 claims description 79
• 241000282414 Homo sapiens Species 0.000 claims description 19
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• YQXCVAGCMNFUMQ-UHFFFAOYSA-N capravirine Chemical compound C=1C(Cl)=CC(Cl)=CC=1SC1=C(C(C)C)N=C(COC(N)=O)N1CC1=CC=NC=C1 YQXCVAGCMNFUMQ-UHFFFAOYSA-N 0.000 claims description 4
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• BEUUJDAEPJZWHM-COROXYKFSA-N tert-butyl n-[(2s,3s,5r)-3-hydroxy-6-[[(2s)-1-(2-methoxyethylamino)-3-methyl-1-oxobutan-2-yl]amino]-6-oxo-1-phenyl-5-[(2,3,4-trimethoxyphenyl)methyl]hexan-2-yl]carbamate Chemical compound C([C@@H]([C@@H](O)C[C@H](C(=O)N[C@H](C(=O)NCCOC)C(C)C)CC=1C(=C(OC)C(OC)=CC=1)OC)NC(=O)OC(C)(C)C)C1=CC=CC=C1 BEUUJDAEPJZWHM-COROXYKFSA-N 0.000 claims description 4
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• NIDRYBLTWYFCFV-FMTVUPSXSA-N (+)-calanolide A Chemical compound C1=CC(C)(C)OC2=C1C(O[C@H](C)[C@@H](C)[C@@H]1O)=C1C1=C2C(CCC)=CC(=O)O1 NIDRYBLTWYFCFV-FMTVUPSXSA-N 0.000 claims description 3
• GWFOVSGRNGAGDL-FSDSQADBSA-N 2-amino-9-[(1r,2r,3s)-2,3-bis(hydroxymethyl)cyclobutyl]-3h-purin-6-one Chemical compound C1=2NC(N)=NC(=O)C=2N=CN1[C@@H]1C[C@H](CO)[C@H]1CO GWFOVSGRNGAGDL-FSDSQADBSA-N 0.000 claims description 3
• XPOQHMRABVBWPR-UHFFFAOYSA-N Efavirenz Natural products O1C(=O)NC2=CC=C(Cl)C=C2C1(C(F)(F)F)C#CC1CC1 XPOQHMRABVBWPR-UHFFFAOYSA-N 0.000 claims description 3
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