JP2005521641A5 - - Google Patents
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- JP2005521641A5 JP2005521641A5 JP2003545618A JP2003545618A JP2005521641A5 JP 2005521641 A5 JP2005521641 A5 JP 2005521641A5 JP 2003545618 A JP2003545618 A JP 2003545618A JP 2003545618 A JP2003545618 A JP 2003545618A JP 2005521641 A5 JP2005521641 A5 JP 2005521641A5
- Authority
- JP
- Japan
- Prior art keywords
- amino
- alkyl
- sulfonyl
- oxopyrrolidin
- chloro
- Prior art date
- 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.)
- Pending
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- 125000000217 alkyl group Chemical group 0.000 claims 73
- 150000001875 compounds Chemical class 0.000 claims 19
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 8
- -1 substituent halogen Chemical class 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 125000001731 2-cyanoethyl group Chemical group [H]C([H])(*)C([H])([H])C#N 0.000 claims 5
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 125000002947 alkylene group Chemical group 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 125000005638 hydrazono group Chemical group 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 125000004434 sulfur atom Chemical group 0.000 claims 3
- RIQHMAOZARRSCE-YWZLYKJASA-N (2s)-2-[(3s)-3-[(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-(2-hydroxyethyl)-n-propan-2-ylpropanamide Chemical compound O=C1N([C@@H](C)C(=O)N(CCO)C(C)C)CC[C@@H]1NS(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 RIQHMAOZARRSCE-YWZLYKJASA-N 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 2
- 125000000979 2-amino-2-oxoethyl group Chemical group [H]C([*])([H])C(=O)N([H])[H] 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000004450 alkenylene group Chemical group 0.000 claims 2
- 125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims 2
- 125000001325 propanoyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
- LKIBMMIENRYXML-YWZLYKJASA-N (2s)-2-[(3s)-3-[(2-amino-2-oxoethyl)-(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n,n-diethylpropanamide Chemical compound O=C1N([C@@H](C)C(=O)N(CC)CC)CC[C@@H]1N(CC(N)=O)S(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 LKIBMMIENRYXML-YWZLYKJASA-N 0.000 claims 1
- NQWFNUIHYCDECX-UGSOOPFHSA-N (2s)-2-[(3s)-3-[(2-amino-2-oxoethyl)-(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n,n-dimethylpropanamide Chemical compound O=C1N([C@@H](C)C(=O)N(C)C)CC[C@@H]1N(CC(N)=O)S(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 NQWFNUIHYCDECX-UGSOOPFHSA-N 0.000 claims 1
- WSORCIFBCUNUEY-JTSKRJEESA-N (2s)-2-[(3s)-3-[(2-amino-2-oxoethyl)-(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n,n-dipropylpropanamide Chemical compound O=C1N([C@@H](C)C(=O)N(CCC)CCC)CC[C@@H]1N(CC(N)=O)S(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 WSORCIFBCUNUEY-JTSKRJEESA-N 0.000 claims 1
- JJDIFJWXXSMKGZ-UUOWRZLLSA-N (2s)-2-[(3s)-3-[(2-amino-2-oxoethyl)-(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-(2-cyanoethyl)-n-cyclopentylpropanamide Chemical compound O=C([C@@H](N1C([C@@H](N(CC(N)=O)S(=O)(=O)C=2C=C3C=CC(Cl)=CC3=CC=2)CC1)=O)C)N(CCC#N)C1CCCC1 JJDIFJWXXSMKGZ-UUOWRZLLSA-N 0.000 claims 1
- QKGOEVVGKSORGS-AOMKIAJQSA-N (2s)-2-[(3s)-3-[(2-amino-2-oxoethyl)-(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-(2-cyanoethyl)-n-cyclopropylpropanamide Chemical compound O=C([C@@H](N1C([C@@H](N(CC(N)=O)S(=O)(=O)C=2C=C3C=CC(Cl)=CC3=CC=2)CC1)=O)C)N(CCC#N)C1CC1 QKGOEVVGKSORGS-AOMKIAJQSA-N 0.000 claims 1
- ZZKNWBYDRWQASH-JTSKRJEESA-N (2s)-2-[(3s)-3-[(2-amino-2-oxoethyl)-(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-(2-cyanoethyl)-n-propan-2-ylpropanamide Chemical compound O=C1N([C@@H](C)C(=O)N(CCC#N)C(C)C)CC[C@@H]1N(CC(N)=O)S(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 ZZKNWBYDRWQASH-JTSKRJEESA-N 0.000 claims 1
- AQIQXBFMTBVKLX-KKSFZXQISA-N (2s)-2-[(3s)-3-[(2-amino-2-oxoethyl)-(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-(2-hydroxyethyl)-n-propan-2-ylpropanamide Chemical compound O=C1N([C@@H](C)C(=O)N(CCO)C(C)C)CC[C@@H]1N(CC(N)=O)S(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 AQIQXBFMTBVKLX-KKSFZXQISA-N 0.000 claims 1
- AWMYONBMACNGKM-YWZLYKJASA-N (2s)-2-[(3s)-3-[(2-amino-2-oxoethyl)-(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-(2-methoxyethyl)-n-methylpropanamide Chemical compound O=C1N([C@@H](C)C(=O)N(C)CCOC)CC[C@@H]1N(CC(N)=O)S(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 AWMYONBMACNGKM-YWZLYKJASA-N 0.000 claims 1
- PBQNZJUORSGHTL-QXWFTVPKSA-N (2s)-2-[(3s)-3-[(2-amino-2-oxoethyl)-(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-[2-(azepan-1-yl)ethyl]-n-propan-2-ylpropanamide;formic acid Chemical compound OC=O.O=C([C@H](C)N1C([C@@H](N(CC(N)=O)S(=O)(=O)C=2C=C3C=CC(Cl)=CC3=CC=2)CC1)=O)N(C(C)C)CCN1CCCCCC1 PBQNZJUORSGHTL-QXWFTVPKSA-N 0.000 claims 1
- BRRGSGRWNJJGEB-KKSFZXQISA-N (2s)-2-[(3s)-3-[(2-amino-2-oxoethyl)-(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-[2-(carbamoylamino)ethyl]-n-propan-2-ylpropanamide Chemical compound O=C1N([C@@H](C)C(=O)N(CCNC(N)=O)C(C)C)CC[C@@H]1N(CC(N)=O)S(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 BRRGSGRWNJJGEB-KKSFZXQISA-N 0.000 claims 1
- LPYFVQPZXSKJJP-ZLLYMXMVSA-N (2s)-2-[(3s)-3-[(2-amino-2-oxoethyl)-(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-[2-(dimethylamino)ethyl]-n-ethylpropanamide;formic acid Chemical compound OC=O.O=C1N([C@@H](C)C(=O)N(CCN(C)C)CC)CC[C@@H]1N(CC(N)=O)S(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 LPYFVQPZXSKJJP-ZLLYMXMVSA-N 0.000 claims 1
- WLMUXXMFDQETHR-LIRRHRJNSA-N (2s)-2-[(3s)-3-[(2-amino-2-oxoethyl)-(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-ethyl-n-methylpropanamide Chemical compound O=C1N([C@@H](C)C(=O)N(C)CC)CC[C@@H]1N(CC(N)=O)S(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 WLMUXXMFDQETHR-LIRRHRJNSA-N 0.000 claims 1
- LMQOMPYKLNZNPF-KKSFZXQISA-N (2s)-2-[(3s)-3-[(2-amino-2-oxoethyl)-(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-ethyl-n-propan-2-ylpropanamide Chemical compound O=C1N([C@@H](C)C(=O)N(C(C)C)CC)CC[C@@H]1N(CC(N)=O)S(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 LMQOMPYKLNZNPF-KKSFZXQISA-N 0.000 claims 1
- PNZATZXFJZLWFP-AOMKIAJQSA-N (2s)-2-[(3s)-3-[(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-(2-cyanoethyl)-n-cyclobutylpropanamide Chemical compound O=C([C@@H](N1C([C@@H](NS(=O)(=O)C=2C=C3C=CC(Cl)=CC3=CC=2)CC1)=O)C)N(CCC#N)C1CCC1 PNZATZXFJZLWFP-AOMKIAJQSA-N 0.000 claims 1
- OZQSLBZUKQKNMX-XPOCZOTCSA-N (2s)-2-[(3s)-3-[(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-(2-hydroxypropyl)-n-propan-2-ylpropanamide Chemical compound O=C1N([C@@H](C)C(=O)N(C(C)C)CC(O)C)CC[C@@H]1NS(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 OZQSLBZUKQKNMX-XPOCZOTCSA-N 0.000 claims 1
- CINHTYQJBRISDA-KKSFZXQISA-N (2s)-2-[(3s)-3-[(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-(3-hydroxypropyl)-n-propan-2-ylpropanamide Chemical compound O=C1N([C@@H](C)C(=O)N(CCCO)C(C)C)CC[C@@H]1NS(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 CINHTYQJBRISDA-KKSFZXQISA-N 0.000 claims 1
- ZPZHPLVVYWTQQN-YWZLYKJASA-N (2s)-2-[(3s)-3-[(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-(cyanomethyl)-n-propan-2-ylpropanamide Chemical compound O=C1N([C@@H](C)C(=O)N(CC#N)C(C)C)CC[C@@H]1NS(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 ZPZHPLVVYWTQQN-YWZLYKJASA-N 0.000 claims 1
- XVICGUQRBYJWKH-ZOEDVAEJSA-N (2s)-2-[(3s)-3-[(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-[2-(dimethylamino)ethyl]-n-ethylpropanamide;formic acid Chemical compound OC=O.O=C1N([C@@H](C)C(=O)N(CCN(C)C)CC)CC[C@@H]1NS(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 XVICGUQRBYJWKH-ZOEDVAEJSA-N 0.000 claims 1
- HYHOSSUACIGAJZ-JTSKRJEESA-N (2s)-2-[(3s)-3-[(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-[2-(dimethylamino)ethyl]-n-propan-2-ylpropanamide Chemical compound O=C1N([C@@H](C)C(=O)N(CCN(C)C)C(C)C)CC[C@@H]1NS(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 HYHOSSUACIGAJZ-JTSKRJEESA-N 0.000 claims 1
- MTIPCPPIOZUMIV-KKSFZXQISA-N (2s)-2-[(3s)-3-[(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-[2-(methanesulfonamido)ethyl]-n-propan-2-ylpropanamide Chemical compound O=C1N([C@@H](C)C(=O)N(CCNS(C)(=O)=O)C(C)C)CC[C@@H]1NS(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 MTIPCPPIOZUMIV-KKSFZXQISA-N 0.000 claims 1
- HLQIJPDUFSPOBV-YWZLYKJASA-N (2s)-2-[(3s)-3-[(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-ethyl-n-propan-2-ylpropanamide Chemical compound O=C1N([C@@H](C)C(=O)N(C(C)C)CC)CC[C@@H]1NS(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 HLQIJPDUFSPOBV-YWZLYKJASA-N 0.000 claims 1
- LEXGOWJJRLAVCQ-YWZLYKJASA-N (2s)-2-[(3s)-3-[(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-propan-2-yl-n-(2-sulfamoylethyl)propanamide Chemical compound O=C1N([C@@H](C)C(=O)N(CCS(N)(=O)=O)C(C)C)CC[C@@H]1NS(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 LEXGOWJJRLAVCQ-YWZLYKJASA-N 0.000 claims 1
- DBTKJOYXTHPISW-NUNBJPPLSA-N (2s)-2-[(3s)-3-[[(e)-2-(4-chlorophenyl)ethenyl]sulfonylamino]-2-oxopyrrolidin-1-yl]-n-ethyl-n-propan-2-ylpropanamide Chemical compound O=C1N([C@@H](C)C(=O)N(C(C)C)CC)CC[C@@H]1NS(=O)(=O)\C=C\C1=CC=C(Cl)C=C1 DBTKJOYXTHPISW-NUNBJPPLSA-N 0.000 claims 1
- MRDYIFQDTQYNKT-SBUREZEXSA-N (2s)-n-(2-acetamidoethyl)-2-[(3s)-3-[(2-amino-2-oxoethyl)-(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-propan-2-ylpropanamide Chemical compound O=C1N([C@@H](C)C(=O)N(CCNC(C)=O)C(C)C)CC[C@@H]1N(CC(N)=O)S(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 MRDYIFQDTQYNKT-SBUREZEXSA-N 0.000 claims 1
- FRVORBIJEZUXOS-AOMKIAJQSA-N (2s)-n-(2-acetamidoethyl)-2-[(3s)-3-[(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-propan-2-ylpropanamide Chemical compound O=C1N([C@@H](C)C(=O)N(CCNC(C)=O)C(C)C)CC[C@@H]1NS(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 FRVORBIJEZUXOS-AOMKIAJQSA-N 0.000 claims 1
- URNLGUWXLQOSPP-LIRRHRJNSA-N (2s)-n-(2-amino-2-oxoethyl)-2-[(3s)-3-[(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-propan-2-ylpropanamide Chemical compound O=C1N([C@@H](C)C(=O)N(CC(N)=O)C(C)C)CC[C@@H]1NS(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 URNLGUWXLQOSPP-LIRRHRJNSA-N 0.000 claims 1
- ABLGPKPAIZKHJR-ZOEDVAEJSA-N (2s)-n-(2-aminoethyl)-2-[(3s)-3-[(2-amino-2-oxoethyl)-(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-propan-2-ylpropanamide;hydrochloride Chemical compound Cl.O=C1N([C@@H](C)C(=O)N(CCN)C(C)C)CC[C@@H]1N(CC(N)=O)S(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 ABLGPKPAIZKHJR-ZOEDVAEJSA-N 0.000 claims 1
- FBHQNSBRZXDZSA-YWZLYKJASA-N (2s)-n-(2-aminoethyl)-2-[(3s)-3-[(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-propan-2-ylpropanamide Chemical compound O=C1N([C@@H](C)C(=O)N(CCN)C(C)C)CC[C@@H]1NS(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 FBHQNSBRZXDZSA-YWZLYKJASA-N 0.000 claims 1
- NODFNDAAXRPXLM-ZOEDVAEJSA-N (2s)-n-(3-aminopropyl)-2-[(3s)-3-[(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-propan-2-ylpropanamide;hydrochloride Chemical compound Cl.O=C1N([C@@H](C)C(=O)N(CCCN)C(C)C)CC[C@@H]1NS(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 NODFNDAAXRPXLM-ZOEDVAEJSA-N 0.000 claims 1
- ZRVKEOJDQJYCNG-SCFGKSIXSA-N (2s)-n-[2-(azepan-1-yl)ethyl]-2-[(3s)-3-[(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-propan-2-ylpropanamide;formic acid Chemical compound OC=O.O=C([C@H](C)N1C([C@@H](NS(=O)(=O)C=2C=C3C=CC(Cl)=CC3=CC=2)CC1)=O)N(C(C)C)CCN1CCCCCC1 ZRVKEOJDQJYCNG-SCFGKSIXSA-N 0.000 claims 1
- LPFRYZFMDLZOOO-KKSFZXQISA-N (2s)-n-[3-(carbamoylamino)propyl]-2-[(3s)-3-[(6-chloronaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]-n-propan-2-ylpropanamide Chemical compound O=C1N([C@@H](C)C(=O)N(CCCNC(N)=O)C(C)C)CC[C@@H]1NS(=O)(=O)C1=CC=C(C=C(Cl)C=C2)C2=C1 LPFRYZFMDLZOOO-KKSFZXQISA-N 0.000 claims 1
- XHAFIUUYXQFJEW-UHFFFAOYSA-N 1-chloroethenylbenzene Chemical compound ClC(=C)C1=CC=CC=C1 XHAFIUUYXQFJEW-UHFFFAOYSA-N 0.000 claims 1
- 125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 claims 1
- CPYLFALFYKCLRI-UHFFFAOYSA-N 2-chloro-1-benzothiophene Chemical compound C1=CC=C2SC(Cl)=CC2=C1 CPYLFALFYKCLRI-UHFFFAOYSA-N 0.000 claims 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 1
- 229940123583 Factor Xa inhibitor Drugs 0.000 claims 1
- BDAGIHXWWSANSR-UHFFFAOYSA-M Formate Chemical compound [O-]C=O BDAGIHXWWSANSR-UHFFFAOYSA-M 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 230000001668 ameliorated effect Effects 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000003205 fragrance Substances 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- UORSJOLJOHEDFS-UHFFFAOYSA-N n-(2-piperidin-1-ylethyl)propanamide Chemical compound CCC(=O)NCCN1CCCCC1 UORSJOLJOHEDFS-UHFFFAOYSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- ISTGQSQWSKCNFJ-UHFFFAOYSA-N tert-butyl n-ethylcarbamate Chemical compound CCNC(=O)OC(C)(C)C ISTGQSQWSKCNFJ-UHFFFAOYSA-N 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0127568.4A GB0127568D0 (en) | 2001-11-16 | 2001-11-16 | Chemical compounds |
| PCT/GB2002/005134 WO2003043981A1 (en) | 2001-11-16 | 2002-11-13 | 2-(3-sulfonylamino-2-oxopyrrolidin-1-yl)propanamides as factor xa inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005521641A JP2005521641A (ja) | 2005-07-21 |
| JP2005521641A5 true JP2005521641A5 (OSRAM) | 2006-01-05 |
Family
ID=9925931
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003545618A Pending JP2005521641A (ja) | 2001-11-16 | 2002-11-13 | 第ｘａ因子阻害剤としての２−（３−スルホニルアミノ−２−オキソピロリジン−１−イル）プロパンアミド |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US7179835B2 (OSRAM) |
| EP (1) | EP1444201B1 (OSRAM) |
| JP (1) | JP2005521641A (OSRAM) |
| AT (1) | ATE372982T1 (OSRAM) |
| AU (1) | AU2002339158A1 (OSRAM) |
| DE (1) | DE60222459T2 (OSRAM) |
| ES (1) | ES2292820T3 (OSRAM) |
| GB (1) | GB0127568D0 (OSRAM) |
| WO (1) | WO2003043981A1 (OSRAM) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0228533D0 (en) * | 2002-12-06 | 2003-01-15 | Glaxo Group Ltd | Crystalline form |
| GB0228552D0 (en) * | 2002-12-06 | 2003-01-15 | Glaxo Group Ltd | Chemical compounds |
| GB0314299D0 (en) | 2003-06-19 | 2003-07-23 | Glaxo Group Ltd | Chemical compounds |
| JP2006527732A (ja) * | 2003-06-19 | 2006-12-07 | グラクソ グループ リミテッド | Ｘａ因子の阻害剤としての３−スルホニルアミノ−ピロリジン−２−オン誘導体 |
| GB0314373D0 (en) * | 2003-06-19 | 2003-07-23 | Glaxo Group Ltd | Chemical compounds |
| GB0314370D0 (en) * | 2003-06-19 | 2003-07-23 | Glaxo Group Ltd | Chemical compounds |
| JP6050238B2 (ja) | 2011-10-19 | 2016-12-21 | 興和株式会社 | 新規なスピロインドリン化合物、及びそれを含有する医薬 |
| HRP20190245T1 (hr) * | 2013-04-26 | 2019-04-05 | Sanofi | Tartratna sol [(s)-2-[metil-3-(2-okso-pirolidin-1-il)-benzensulfonilamino]-3-(4-metil piperazin-1 -il)-3-okso-propril]amida 5-kloro-tiofen-2-karboksilne kiseline |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL92011A0 (en) | 1988-10-19 | 1990-07-12 | Abbott Lab | Heterocyclic peptide renin inhibitors |
| DE4121947A1 (de) * | 1991-07-03 | 1993-01-07 | Basf Ag | 2-(3-(4-amidino-phenyl))-propionsaeurederivate, ihre herstellung und verwendung |
| US5703208A (en) | 1994-06-17 | 1997-12-30 | Corvas International, Inc. | 3-amino-2-oxo-1-piperidineacetic derivatives as enzyme inhibitors |
| US5932733A (en) | 1994-06-17 | 1999-08-03 | Corvas International, Inc. | 3-amino-2-oxo-1-piperidineacetic derivatives containing an arginine mimic as enzyme inhibitors |
| JPH10503176A (ja) | 1994-06-17 | 1998-03-24 | コーバス インターナショナル， インコーポレイテッド | 酵素インヒビターとしての３−アミノ−２−オキソ−１−ピペリジン酢酸誘導体 |
| US5719296A (en) * | 1995-10-30 | 1998-02-17 | Merck & Co., Inc. | Pseudopeptide lactam inhibitors of peptide binding to MHC class II proteins |
| AU7604196A (en) | 1995-10-30 | 1997-05-22 | Merck & Co., Inc. | Novel inhibitors of peptide binding to mhc class ii proteins |
| WO1998016523A2 (en) * | 1996-10-11 | 1998-04-23 | Cor Therapeutics, Inc. | Selective factor xa inhibitors |
| US6602864B1 (en) | 1996-12-13 | 2003-08-05 | Aventis Pharma Deutschland Gmbh | Sulfonic acid or sulfonylamino N-(heteroaralkyl)-azaheterocyclylamide compounds |
| US6281227B1 (en) | 1996-12-13 | 2001-08-28 | Aventis Pharma Deutschland Gmbh | Sulfonic acid sulfonylamino n-(heteroaralkyl)-azaheterocyclylamide compounds |
| PL333921A1 (en) | 1996-12-13 | 2000-01-31 | Rhone Poulenc Rorer Pharma | N-(heteroalkyl)-azaheterocyclyamides of sulphonic acids or other n-(heteroalkyl)-azaheterocyclylamide compounds |
| US6187797B1 (en) | 1996-12-23 | 2001-02-13 | Dupont Pharmaceuticals Company | Phenyl-isoxazoles as factor XA Inhibitors |
| US6525042B1 (en) | 1997-09-30 | 2003-02-25 | Daiichi Pharmaceutical Co., Ltd. | Sulfonyl derivatives |
| ZA988967B (en) | 1997-10-03 | 2000-04-03 | Du Pont Pharm Co | Lactam metalloprotease inhibitors. |
| JP2002536437A (ja) * | 1999-02-09 | 2002-10-29 | ブリストル−マイヤーズ スクイブ カンパニー | ＦＸａのラクタム抑制剤および方法 |
| EP1206449A1 (en) | 1999-07-26 | 2002-05-22 | Bristol-Myers Squibb Company | Lactam inhibitors of hepatitis c virus ns3 protease |
| HK1050005A1 (zh) * | 1999-09-13 | 2003-06-06 | 三维药物公司 | 氮杂环烷酮丝氨酸蛋白酶抑制剂 |
| AU2001255408A1 (en) * | 2000-04-14 | 2001-10-30 | Corvas International, Inc. | Tetrahydro-azepinone derivatives as thrombin inhibitors |
-
2001
- 2001-11-16 GB GBGB0127568.4A patent/GB0127568D0/en not_active Ceased
-
2002
- 2002-11-13 JP JP2003545618A patent/JP2005521641A/ja active Pending
- 2002-11-13 WO PCT/GB2002/005134 patent/WO2003043981A1/en not_active Ceased
- 2002-11-13 ES ES02777533T patent/ES2292820T3/es not_active Expired - Lifetime
- 2002-11-13 DE DE60222459T patent/DE60222459T2/de not_active Expired - Fee Related
- 2002-11-13 AU AU2002339158A patent/AU2002339158A1/en not_active Abandoned
- 2002-11-13 AT AT02777533T patent/ATE372982T1/de not_active IP Right Cessation
- 2002-11-13 US US10/495,586 patent/US7179835B2/en not_active Expired - Fee Related
- 2002-11-13 EP EP02777533A patent/EP1444201B1/en not_active Expired - Lifetime
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