JP2011507915A5

JP2011507915A5 -

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Publication number: JP2011507915A5
Authority: JP; Japan
Prior art keywords: oxo; phenyl; ethoxy; carbonyl; pyrazole
Prior art date: 2008-12-12
Legal status : Granted

Application number

JP2010540046A

Other languages

English (en)

Japanese (ja)

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JP2011507915A (ja

JP5504171B2 (ja

Filing date

2008-12-12

Publication date

2012-02-02

2008-12-12 Application filed filed Critical

2008-12-12 Priority claimed from PCT/EP2008/010572 external-priority patent/WO2009080226A2/en

2011-03-10 Publication of JP2011507915A publication Critical patent/JP2011507915A/ja

2012-02-02 Publication of JP2011507915A5 publication Critical patent/JP2011507915A5/ja

2014-05-28 Application granted granted Critical

2014-05-28 Publication of JP5504171B2 publication Critical patent/JP5504171B2/ja

Status Expired - Fee Related legal-status Critical Current

2028-12-12 Anticipated expiration legal-status Critical

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-1 5- {2-[(S) -2- (4,4-difluoro-piperidin-1-carbonyl) -pyrrolidin-1-yl] -2- Oxo-ethoxy} -1-phenyl-1H-pyrazole-3-carbonyl Chemical group 0.000 claims 40
125000000623 heterocyclic group Chemical group 0.000 claims 8
125000004435 hydrogen atom Chemical group [H]* 0.000 claims 7
RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 6
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 4
NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 4
239000002253 acid Substances 0.000 claims 4
125000000217 alkyl group Chemical group 0.000 claims 4
150000001875 compounds Chemical class 0.000 claims 4
125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 3
HFUXCRXQICHWAR-KRWDZBQOSA-N 5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carboxylic acid Chemical compound O=C([C@@H]1CCCN1C(=O)COC1=CC(=NN1C=1C=CC=CC=1)C(=O)O)NC1CCC1 HFUXCRXQICHWAR-KRWDZBQOSA-N 0.000 claims 3
125000002393 azetidinyl group Chemical group 0.000 claims 3
125000000753 cycloalkyl group Chemical group 0.000 claims 3
VILAVOFMIJHSJA-UHFFFAOYSA-N dicarbon monoxide Chemical group [C]=C=O VILAVOFMIJHSJA-UHFFFAOYSA-N 0.000 claims 3
229910052736 halogen Inorganic materials 0.000 claims 3
229910052757 nitrogen Inorganic materials 0.000 claims 3
125000004433 nitrogen atom Chemical group N* 0.000 claims 3
125000004193 piperazinyl group Chemical group 0.000 claims 3
125000003386 piperidinyl group Chemical group 0.000 claims 3
125000000719 pyrrolidinyl group Chemical group 0.000 claims 3
150000003839 salts Chemical class 0.000 claims 3
MMFKCRKIICEICG-SMCANUKXSA-N (4s)-5-(4-benzoylpiperidin-1-yl)-4-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound O=C([C@@H]1CCCN1C(=O)COC1=CC(=NN1C=1C=CC=CC=1)C(=O)N[C@@H](CCC(=O)O)C(=O)N1CCC(CC1)C(=O)C=1C=CC=CC=1)NC1CCC1 MMFKCRKIICEICG-SMCANUKXSA-N 0.000 claims 2
GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims 2
TXCXOAAMMUSZNO-YTMVLYRLSA-N butyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-hydroxypentanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H](CCCO)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 TXCXOAAMMUSZNO-YTMVLYRLSA-N 0.000 claims 2
125000002541 furyl group Chemical group 0.000 claims 2
150000002367 halogens Chemical class 0.000 claims 2
125000002883 imidazolyl group Chemical group 0.000 claims 2
125000001041 indolyl group Chemical group 0.000 claims 2
125000000842 isoxazolyl group Chemical group 0.000 claims 2
239000000203 mixture Substances 0.000 claims 2
125000001715 oxadiazolyl group Chemical group 0.000 claims 2
125000002971 oxazolyl group Chemical group 0.000 claims 2
125000003831 tetrazolyl group Chemical group 0.000 claims 2
125000001544 thienyl group Chemical group 0.000 claims 2
XISCQOBIDCUORV-RZUBCFFCSA-N (2r,4r)-1-[2-[5-[[(2s)-4-carboxy-1-(4-ethoxycarbonylpiperazin-1-yl)-1-oxobutan-2-yl]carbamoyl]-2-phenylpyrazol-3-yl]oxyacetyl]-4-hydroxypyrrolidine-2-carboxylic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@H](C[C@@H](O)C2)C(O)=O)=C1 XISCQOBIDCUORV-RZUBCFFCSA-N 0.000 claims 1
ZXKHGNKMAPRUGZ-FPOVZHCZSA-N (2s)-1-[2-[5-[[(2s)-4-carboxy-1-(4-ethoxycarbonylpiperazin-1-yl)-1-oxobutan-2-yl]carbamoyl]-2-phenylpyrazol-3-yl]oxyacetyl]azetidine-2-carboxylic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CC2)C(O)=O)=C1 ZXKHGNKMAPRUGZ-FPOVZHCZSA-N 0.000 claims 1
UTKQDUVLHCPYRU-UNMCSNQZSA-N (2s)-1-[2-[5-[[(2s)-4-carboxy-1-(4-ethoxycarbonylpiperazin-1-yl)-1-oxobutan-2-yl]carbamoyl]-2-phenylpyrazol-3-yl]oxyacetyl]pyrrolidine-2-carboxylic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(O)=O)=C1 UTKQDUVLHCPYRU-UNMCSNQZSA-N 0.000 claims 1
IELBGBJNDBGVDM-FLJXZVEISA-N (2s)-1-[2-[5-[[(2s)-4-carboxy-1-(4-ethoxycarbonylpiperazin-1-yl)-1-oxobutan-2-yl]carbamoyl]-2-phenylpyrazol-3-yl]oxypropanoyl]pyrrolidine-2-carboxylic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OC(C)C(=O)N2[C@@H](CCC2)C(O)=O)=C1 IELBGBJNDBGVDM-FLJXZVEISA-N 0.000 claims 1
XISCQOBIDCUORV-URVUXULASA-N (2s,4r)-1-[2-[5-[[(2s)-4-carboxy-1-(4-ethoxycarbonylpiperazin-1-yl)-1-oxobutan-2-yl]carbamoyl]-2-phenylpyrazol-3-yl]oxyacetyl]-4-hydroxypyrrolidine-2-carboxylic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](C[C@@H](O)C2)C(O)=O)=C1 XISCQOBIDCUORV-URVUXULASA-N 0.000 claims 1
COZKKGNEYIDZNQ-VXKWHMMOSA-N (3s)-3-[[5-[2-[(2s)-2-(2,2-difluoroethylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-4-(4-ethoxycarbonylpiperazin-1-yl)-4-oxobutanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NCC(F)F)=C1 COZKKGNEYIDZNQ-VXKWHMMOSA-N 0.000 claims 1
PNSWWJSTHMVLIX-DQEYMECFSA-N (3s)-3-[[5-[2-[(2s)-2-(cyclopropylmethylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-4-(4-ethoxycarbonylpiperazin-1-yl)-4-oxobutanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NCC2CC2)=C1 PNSWWJSTHMVLIX-DQEYMECFSA-N 0.000 claims 1
ARGXISHBETUOII-FWUCURJTSA-N (3s)-3-[[5-[2-[(2s)-2-carbamoyl-2-cyclopropylpyrrolidin-1-yl]-2-oxoethoxy]-1-(3-fluorophenyl)pyrazole-3-carbonyl]amino]-4-(4-ethoxycarbonylpiperazin-1-yl)-4-oxobutanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CC(O)=O)NC(=O)C1=NN(C=2C=C(F)C=CC=2)C(OCC(=O)N2[C@@](CCC2)(C2CC2)C(N)=O)=C1 ARGXISHBETUOII-FWUCURJTSA-N 0.000 claims 1
CSXHCTNCEPEFKP-LUTIACGYSA-N (3s)-4-(4-ethoxycarbonylpiperazin-1-yl)-2-methyl-4-oxo-3-[[5-[2-oxo-2-(2-oxopyrrolidin-1-yl)ethoxy]-1-phenylpyrazole-3-carbonyl]amino]butanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](C(C)C(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2C(CCC2)=O)=C1 CSXHCTNCEPEFKP-LUTIACGYSA-N 0.000 claims 1
JJQBDHQOTDWTHW-GOTSBHOMSA-N (3s)-4-(4-ethoxycarbonylpiperazin-1-yl)-3-[[5-[2-[(2s)-2-(2-fluoroethylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-4-oxobutanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NCCF)=C1 JJQBDHQOTDWTHW-GOTSBHOMSA-N 0.000 claims 1
QSDQTUDROSJPPN-VXKWHMMOSA-N (3s)-4-(4-ethoxycarbonylpiperazin-1-yl)-4-oxo-3-[[5-[2-oxo-2-[(2s)-2-(2,2,2-trifluoroethylcarbamoyl)pyrrolidin-1-yl]ethoxy]-1-phenylpyrazole-3-carbonyl]amino]butanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NCC(F)(F)F)=C1 QSDQTUDROSJPPN-VXKWHMMOSA-N 0.000 claims 1
FNWMCWMNAGUTNE-PWMMPXSUSA-N (4s)-4-[[5-[(2r)-1-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-1-oxopropan-2-yl]oxy-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(O[C@H](C)C(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 FNWMCWMNAGUTNE-PWMMPXSUSA-N 0.000 claims 1
QXVPESFLVQKFNB-DSBYRVASSA-N (4s)-4-[[5-[(2r)-1-[(2s)-2-(cyclopropylcarbamoyl)pyrrolidin-1-yl]-1-oxopropan-2-yl]oxy-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(O[C@H](C)C(=O)N2[C@@H](CCC2)C(=O)NC2CC2)=C1 QXVPESFLVQKFNB-DSBYRVASSA-N 0.000 claims 1
FNWMCWMNAGUTNE-LNBJVWSJSA-N (4s)-4-[[5-[(2s)-1-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-1-oxopropan-2-yl]oxy-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(O[C@@H](C)C(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 FNWMCWMNAGUTNE-LNBJVWSJSA-N 0.000 claims 1
QXVPESFLVQKFNB-CVJWPJSTSA-N (4s)-4-[[5-[(2s)-1-[(2s)-2-(cyclopropylcarbamoyl)pyrrolidin-1-yl]-1-oxopropan-2-yl]oxy-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(O[C@@H](C)C(=O)N2[C@@H](CCC2)C(=O)NC2CC2)=C1 QXVPESFLVQKFNB-CVJWPJSTSA-N 0.000 claims 1
JHHNVUQQSXAHSU-AZGAKELHSA-N (4s)-4-[[5-[1-[(2r)-2-(cyclopropylcarbamoyl)pyrrolidin-1-yl]-2-methyl-1-oxopropan-2-yl]oxy-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OC(C)(C)C(=O)N2[C@H](CCC2)C(=O)NC2CC2)=C1 JHHNVUQQSXAHSU-AZGAKELHSA-N 0.000 claims 1
KAIMHFXKOBXCSG-WAXYSGSMSA-N (4s)-4-[[5-[1-[(2s)-2-(cyclopropylcarbamoyl)azetidin-1-yl]-1-oxopropan-2-yl]oxy-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OC(C)C(=O)N2[C@@H](CC2)C(=O)NC2CC2)=C1 KAIMHFXKOBXCSG-WAXYSGSMSA-N 0.000 claims 1
QXVPESFLVQKFNB-KLZDYHPHSA-N (4s)-4-[[5-[1-[(2s)-2-(cyclopropylcarbamoyl)pyrrolidin-1-yl]-1-oxopropan-2-yl]oxy-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OC(C)C(=O)N2[C@@H](CCC2)C(=O)NC2CC2)=C1 QXVPESFLVQKFNB-KLZDYHPHSA-N 0.000 claims 1
JHHNVUQQSXAHSU-AHWVRZQESA-N (4s)-4-[[5-[1-[(2s)-2-(cyclopropylcarbamoyl)pyrrolidin-1-yl]-2-methyl-1-oxopropan-2-yl]oxy-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OC(C)(C)C(=O)N2[C@@H](CCC2)C(=O)NC2CC2)=C1 JHHNVUQQSXAHSU-AHWVRZQESA-N 0.000 claims 1
IQMDQKQFNHYJAZ-XIAJTGEISA-N (4s)-4-[[5-[1-[(2s)-2-(dimethylcarbamoyl)pyrrolidin-1-yl]-1-oxopropan-2-yl]oxy-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OC(C)C(=O)N2[C@@H](CCC2)C(=O)N(C)C)=C1 IQMDQKQFNHYJAZ-XIAJTGEISA-N 0.000 claims 1
FFOJTXJCVNWXPA-AIICXWBISA-N (4s)-4-[[5-[1-[(3s,4s)-3,4-dihydroxypyrrolidin-1-yl]-1-oxopropan-2-yl]oxy-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OC(C)C(=O)N2C[C@H](O)[C@@H](O)C2)=C1 FFOJTXJCVNWXPA-AIICXWBISA-N 0.000 claims 1
OLDURABUMGYLTL-PMVMPFDFSA-N (4s)-4-[[5-[1-[(3s,4s)-3,4-dihydroxypyrrolidin-1-yl]-2-methyl-1-oxopropan-2-yl]oxy-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OC(C)(C)C(=O)N2C[C@H](O)[C@@H](O)C2)=C1 OLDURABUMGYLTL-PMVMPFDFSA-N 0.000 claims 1
GFGPMJHUJKJWJD-YANBTOMASA-N (4s)-4-[[5-[2-(3-acetamidopyrrolidin-1-yl)-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2CC(CC2)NC(C)=O)=C1 GFGPMJHUJKJWJD-YANBTOMASA-N 0.000 claims 1
CJDCZRKJXPKEGW-QHCPKHFHSA-N (4s)-4-[[5-[2-(4-acetylpiperazin-1-yl)-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2CCN(CC2)C(C)=O)=C1 CJDCZRKJXPKEGW-QHCPKHFHSA-N 0.000 claims 1
OXZQYIXOZLLFBE-GMAHTHKFSA-N (4s)-4-[[5-[2-[(2s)-2-(2,2-difluoroethylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NCC(F)F)=C1 OXZQYIXOZLLFBE-GMAHTHKFSA-N 0.000 claims 1
HBWOJLBXQOEPSI-XCZPVHLTSA-N (4s)-4-[[5-[2-[(2s)-2-(2-fluoroethylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxo-5-(4-phenoxycarbonylpiperazin-1-yl)pentanoic acid Chemical compound N([C@@H](CCC(=O)O)C(=O)N1CCN(CC1)C(=O)OC=1C=CC=CC=1)C(=O)C(=NN1C=2C=CC=CC=2)C=C1OCC(=O)N1CCC[C@H]1C(=O)NCCF HBWOJLBXQOEPSI-XCZPVHLTSA-N 0.000 claims 1
WDMWBFNHUZYJDA-YTMVLYRLSA-N (4s)-4-[[5-[2-[(2s)-2-(2-fluoroethylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxo-5-(4-phenylmethoxycarbonylpiperazin-1-yl)pentanoic acid Chemical compound N([C@@H](CCC(=O)O)C(=O)N1CCN(CC1)C(=O)OCC=1C=CC=CC=1)C(=O)C(=NN1C=2C=CC=CC=2)C=C1OCC(=O)N1CCC[C@H]1C(=O)NCCF WDMWBFNHUZYJDA-YTMVLYRLSA-N 0.000 claims 1
NIPSIFFFUFYJBI-ZCYQVOJMSA-N (4s)-4-[[5-[2-[(2s)-2-(azetidine-1-carbonyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)N2CCC2)=C1 NIPSIFFFUFYJBI-ZCYQVOJMSA-N 0.000 claims 1
DAZHFSIQGHISMS-AHWVRZQESA-N (4s)-4-[[5-[2-[(2s)-2-(butylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound CCCCNC(=O)[C@@H]1CCCN1C(=O)COC1=CC(C(=O)N[C@@H](CCC(O)=O)C(=O)N2CCN(CC2)C(=O)OCC)=NN1C1=CC=CC=C1 DAZHFSIQGHISMS-AHWVRZQESA-N 0.000 claims 1
YDNDPOSUHSPSFR-ZCYQVOJMSA-N (4s)-4-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)-4,4-difluoropyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CC(F)(F)C2)C(=O)NC2CCC2)=C1 YDNDPOSUHSPSFR-ZCYQVOJMSA-N 0.000 claims 1
FLTCGCFPWANXBR-ZCYQVOJMSA-N (4s)-4-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)azetidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CC2)C(=O)NC2CCC2)=C1 FLTCGCFPWANXBR-ZCYQVOJMSA-N 0.000 claims 1
XPCCZVLFMZWVJM-AHWVRZQESA-N (4s)-4-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-(3-fluorophenyl)pyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=C(F)C=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 XPCCZVLFMZWVJM-AHWVRZQESA-N 0.000 claims 1
ZYGVAQWZGGWPEP-XCZPVHLTSA-N (4s)-4-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-cyclobutyloxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound O=C([C@@H]1CCCN1C(=O)COC1=CC(=NN1C=1C=CC=CC=1)C(=O)N[C@@H](CCC(=O)O)C(=O)N1CCN(CC1)C(=O)OC1CCC1)NC1CCC1 ZYGVAQWZGGWPEP-XCZPVHLTSA-N 0.000 claims 1
JUFWUUHBGQZSBC-BDYUSTAISA-N (4s)-4-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-[(1-ethoxycarbonylpiperidin-4-yl)amino]-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCC1NC(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 JUFWUUHBGQZSBC-BDYUSTAISA-N 0.000 claims 1
BZZBQDSQFCPKKX-PWMMPXSUSA-N (4s)-4-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-[(2r)-4-ethoxycarbonyl-2-methylpiperazin-1-yl]-5-oxopentanoic acid Chemical compound C[C@@H]1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 BZZBQDSQFCPKKX-PWMMPXSUSA-N 0.000 claims 1
BZZBQDSQFCPKKX-LNBJVWSJSA-N (4s)-4-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-[(2s)-4-ethoxycarbonyl-2-methylpiperazin-1-yl]-5-oxopentanoic acid Chemical compound C[C@H]1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 BZZBQDSQFCPKKX-LNBJVWSJSA-N 0.000 claims 1
ASSNEGLNYGDZRV-PWMMPXSUSA-N (4s)-4-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-[(3r)-4-ethoxycarbonyl-3-methylpiperazin-1-yl]-5-oxopentanoic acid Chemical compound C1[C@@H](C)N(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 ASSNEGLNYGDZRV-PWMMPXSUSA-N 0.000 claims 1
ASSNEGLNYGDZRV-LNBJVWSJSA-N (4s)-4-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-[(3s)-4-ethoxycarbonyl-3-methylpiperazin-1-yl]-5-oxopentanoic acid Chemical compound C1[C@H](C)N(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 ASSNEGLNYGDZRV-LNBJVWSJSA-N 0.000 claims 1
GIKIIOPLMWUVJL-SMCANUKXSA-N (4s)-4-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-[4-(3-methoxyphenyl)piperazin-1-yl]-5-oxopentanoic acid Chemical compound COC1=CC=CC(N2CCN(CC2)C(=O)[C@H](CCC(O)=O)NC(=O)C2=NN(C(OCC(=O)N3[C@@H](CCC3)C(=O)NC3CCC3)=C2)C=2C=CC=CC=2)=C1 GIKIIOPLMWUVJL-SMCANUKXSA-N 0.000 claims 1
DKNNFADSGJARAT-JDXGNMNLSA-N (4s)-4-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxo-5-(4-phenoxycarbonylpiperazin-1-yl)pentanoic acid Chemical compound O=C([C@@H]1CCCN1C(=O)COC1=CC(=NN1C=1C=CC=CC=1)C(=O)N[C@@H](CCC(=O)O)C(=O)N1CCN(CC1)C(=O)OC=1C=CC=CC=1)NC1CCC1 DKNNFADSGJARAT-JDXGNMNLSA-N 0.000 claims 1
DUHQLWJEMNMRRC-BDYUSTAISA-N (4s)-4-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxo-5-(4-propoxycarbonylpiperazin-1-yl)pentanoic acid Chemical compound C1CN(C(=O)OCCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 DUHQLWJEMNMRRC-BDYUSTAISA-N 0.000 claims 1
BXWGANDXCUPEHZ-BDYUSTAISA-N (4s)-4-[[5-[2-[(2s)-2-(cyclobutylmethylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NCC2CCC2)=C1 BXWGANDXCUPEHZ-BDYUSTAISA-N 0.000 claims 1
RKMBNFRQEXWRGK-BDYUSTAISA-N (4s)-4-[[5-[2-[(2s)-2-(cyclopentylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCCC2)=C1 RKMBNFRQEXWRGK-BDYUSTAISA-N 0.000 claims 1
ZBRQCDCFJYGZLX-UPVQGACJSA-N (4s)-4-[[5-[2-[(2s)-2-(cyclopropylcarbamoyl)azetidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CC2)C(=O)NC2CC2)=C1 ZBRQCDCFJYGZLX-UPVQGACJSA-N 0.000 claims 1
WKXIUXDYHFBXHE-ZCYQVOJMSA-N (4s)-4-[[5-[2-[(2s)-2-(cyclopropylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-(3-fluorophenyl)pyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=C(F)C=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CC2)=C1 WKXIUXDYHFBXHE-ZCYQVOJMSA-N 0.000 claims 1
COIKTPDPNIFSEY-ZCYQVOJMSA-N (4s)-4-[[5-[2-[(2s)-2-(cyclopropylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CC2)=C1 COIKTPDPNIFSEY-ZCYQVOJMSA-N 0.000 claims 1
JWSWMMLJENVXRX-AHWVRZQESA-N (4s)-4-[[5-[2-[(2s)-2-(cyclopropylmethylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NCC2CC2)=C1 JWSWMMLJENVXRX-AHWVRZQESA-N 0.000 claims 1
GTWNSMGLSKONLG-PWMMPXSUSA-N (4s)-4-[[5-[2-[(2s)-2-(cyclopropylmethylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-[(3r)-4-ethoxycarbonyl-3-methylpiperazin-1-yl]-5-oxopentanoic acid Chemical compound C1[C@@H](C)N(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NCC2CC2)=C1 GTWNSMGLSKONLG-PWMMPXSUSA-N 0.000 claims 1
RUHJNPVHHSFMBQ-JDXGNMNLSA-N (4s)-4-[[5-[2-[(2s)-2-(cyclopropylmethylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxo-5-(4-phenoxycarbonylpiperazin-1-yl)pentanoic acid Chemical compound O=C([C@@H]1CCCN1C(=O)COC1=CC(=NN1C=1C=CC=CC=1)C(=O)N[C@@H](CCC(=O)O)C(=O)N1CCN(CC1)C(=O)OC=1C=CC=CC=1)NCC1CC1 RUHJNPVHHSFMBQ-JDXGNMNLSA-N 0.000 claims 1
AQQRQVVDXBPLAG-SMCANUKXSA-N (4s)-4-[[5-[2-[(2s)-2-(cyclopropylmethylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxo-5-(4-phenylmethoxycarbonylpiperazin-1-yl)pentanoic acid Chemical compound O=C([C@@H]1CCCN1C(=O)COC1=CC(=NN1C=1C=CC=CC=1)C(=O)N[C@@H](CCC(=O)O)C(=O)N1CCN(CC1)C(=O)OCC=1C=CC=CC=1)NCC1CC1 AQQRQVVDXBPLAG-SMCANUKXSA-N 0.000 claims 1
PPEVADRKIKQWMG-ZCYQVOJMSA-N (4s)-4-[[5-[2-[(2s)-2-(tert-butylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC(C)(C)C)=C1 PPEVADRKIKQWMG-ZCYQVOJMSA-N 0.000 claims 1
YNZNAIQWEFWQIV-GXBCDIMNSA-N (4s)-4-[[5-[2-[(2s)-2-[(2,2-difluorocyclopropyl)carbamoyl]pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2C(C2)(F)F)=C1 YNZNAIQWEFWQIV-GXBCDIMNSA-N 0.000 claims 1
IEACTJWJCQIDST-BDYUSTAISA-N (4s)-4-[[5-[2-[(2s)-2-[cyclobutyl(methyl)carbamoyl]pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)N(C)C2CCC2)=C1 IEACTJWJCQIDST-BDYUSTAISA-N 0.000 claims 1
BATFERYXLOIMMT-UNMCSNQZSA-N (4s)-4-[[5-[2-[(2s)-2-carbamoylpyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(N)=O)=C1 BATFERYXLOIMMT-UNMCSNQZSA-N 0.000 claims 1
IDIXRYQQQCMUIP-GPXNEJASSA-N (4s)-4-[[5-[2-[(2s,4r)-2-ethoxycarbonyl-4-hydroxypyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound CCOC(=O)[C@@H]1C[C@@H](O)CN1C(=O)COC1=CC(C(=O)N[C@@H](CCC(O)=O)C(=O)N2CCN(CC2)C(=O)OCC)=NN1C1=CC=CC=C1 IDIXRYQQQCMUIP-GPXNEJASSA-N 0.000 claims 1
DKMKIQXKLMTUQS-IAXKEJLGSA-N (4s)-4-[[5-[2-[3-(2,2-difluoroethylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2CC(CC2)C(=O)NCC(F)F)=C1 DKMKIQXKLMTUQS-IAXKEJLGSA-N 0.000 claims 1
NEOPAGBOYFPYRC-DEOSSOPVSA-N (4s)-4-[[5-[2-[3-(cyclobutylcarbamoyl)azetidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2CC(C2)C(=O)NC2CCC2)=C1 NEOPAGBOYFPYRC-DEOSSOPVSA-N 0.000 claims 1
POCASLQMEDGEJT-TUXUZCGSSA-N (4s)-4-[[5-[2-[3-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2CC(CC2)C(=O)NC2CCC2)=C1 POCASLQMEDGEJT-TUXUZCGSSA-N 0.000 claims 1
OHTXBUKWZOGHTN-QHCPKHFHSA-N (4s)-4-[[5-[2-[3-(cyclopropylcarbamoyl)azetidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2CC(C2)C(=O)NC2CC2)=C1 OHTXBUKWZOGHTN-QHCPKHFHSA-N 0.000 claims 1
QZOFQSPPOHIQEI-FHZUCYEKSA-N (4s)-4-[[5-[2-[3-(cyclopropylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2CC(CC2)C(=O)NC2CC2)=C1 QZOFQSPPOHIQEI-FHZUCYEKSA-N 0.000 claims 1
ACNLRNGYQFTYAW-YNMFNDETSA-N (4s)-4-[[5-[2-[3-(cyclopropylmethylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2CC(CC2)C(=O)NCC2CC2)=C1 ACNLRNGYQFTYAW-YNMFNDETSA-N 0.000 claims 1
WLWKSKVKTSCNFR-ZCYQVOJMSA-N (4s)-5-(4-butoxycarbonylpiperazin-1-yl)-4-[[5-[2-[(2s)-2-(2,2-difluoroethylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NCC(F)F)=C1 WLWKSKVKTSCNFR-ZCYQVOJMSA-N 0.000 claims 1
DNSBPAYHLJPUTF-AHWVRZQESA-N (4s)-5-(4-butoxycarbonylpiperazin-1-yl)-4-[[5-[2-[(2s)-2-(2-fluoroethylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NCCF)=C1 DNSBPAYHLJPUTF-AHWVRZQESA-N 0.000 claims 1
BEORAWYIKRCZKI-XCZPVHLTSA-N (4s)-5-(4-butoxycarbonylpiperazin-1-yl)-4-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 BEORAWYIKRCZKI-XCZPVHLTSA-N 0.000 claims 1
MUCGVSSPQSPCKI-BDYUSTAISA-N (4s)-5-(4-butoxycarbonylpiperazin-1-yl)-4-[[5-[2-[(2s)-2-(cyclopropylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CC2)=C1 MUCGVSSPQSPCKI-BDYUSTAISA-N 0.000 claims 1
MSWGOCULYQIDGP-XCZPVHLTSA-N (4s)-5-(4-butoxycarbonylpiperazin-1-yl)-4-[[5-[2-[(2s)-2-(cyclopropylmethylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NCC2CC2)=C1 MSWGOCULYQIDGP-XCZPVHLTSA-N 0.000 claims 1
FJKJLHMLWNGTPE-YTMVLYRLSA-N (4s)-5-(4-butoxycarbonylpiperazin-1-yl)-4-[[5-[2-[(2s)-2-[cyclobutyl(methyl)carbamoyl]pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)N(C)C2CCC2)=C1 FJKJLHMLWNGTPE-YTMVLYRLSA-N 0.000 claims 1
GJMKFKODRQXIGG-ZCYQVOJMSA-N (4s)-5-(4-butoxycarbonylpiperazin-1-yl)-5-oxo-4-[[5-[2-oxo-2-[(2s)-2-(2,2,2-trifluoroethylcarbamoyl)pyrrolidin-1-yl]ethoxy]-1-phenylpyrazole-3-carbonyl]amino]pentanoic acid Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NCC(F)(F)F)=C1 GJMKFKODRQXIGG-ZCYQVOJMSA-N 0.000 claims 1
KMFRPHHUPZJQSJ-KEKNWZKVSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-4-[[5-[2-(3-methylsulfonylpyrrolidin-1-yl)-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2CC(CC2)S(C)(=O)=O)=C1 KMFRPHHUPZJQSJ-KEKNWZKVSA-N 0.000 claims 1
MXDWLFKHNAHHSM-QHCPKHFHSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-4-[[5-[2-(4-ethylpiperazin-1-yl)-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2CCN(CC)CC2)=C1 MXDWLFKHNAHHSM-QHCPKHFHSA-N 0.000 claims 1
KPIARWRTUDDWFT-QFIPXVFZSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-4-[[5-[2-(4-hydroxypiperidin-1-yl)-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2CCC(O)CC2)=C1 KPIARWRTUDDWFT-QFIPXVFZSA-N 0.000 claims 1
NGFWLABDAKLJLN-UPVQGACJSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-4-[[5-[2-[(2s)-2-(2-fluoroethylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NCCF)=C1 NGFWLABDAKLJLN-UPVQGACJSA-N 0.000 claims 1
VVTJJEFPRVMTQO-ZCYQVOJMSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-4-[[5-[2-[(2s)-2-(2-methylsulfanylethylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NCCSC)=C1 VVTJJEFPRVMTQO-ZCYQVOJMSA-N 0.000 claims 1
FKIOCEBFXLRUFO-UPVQGACJSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-4-[[5-[2-[(2s)-2-(3-methyl-1,2,4-oxadiazol-5-yl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C=2ON=C(C)N=2)=C1 FKIOCEBFXLRUFO-UPVQGACJSA-N 0.000 claims 1
GZWBBCZIZDUAMU-ZCYQVOJMSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-4-[[5-[2-[(2s)-2-(3-methyl-1,2-oxazol-5-yl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C=2ON=C(C)C=2)=C1 GZWBBCZIZDUAMU-ZCYQVOJMSA-N 0.000 claims 1
DTFCIYPCWQLZMS-ZCYQVOJMSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-4-[[5-[2-[(2s)-2-(4-methyl-1,3-oxazol-2-yl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C=2OC=C(C)N=2)=C1 DTFCIYPCWQLZMS-ZCYQVOJMSA-N 0.000 claims 1
LHSSKYXYIJQMHP-ZCYQVOJMSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-4-[[5-[2-[(2s)-2-(5-methyl-1h-imidazol-2-yl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C=2NC=C(C)N=2)=C1 LHSSKYXYIJQMHP-ZCYQVOJMSA-N 0.000 claims 1
KWCKTXOCWXSWQQ-UPVQGACJSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-4-[[5-[2-[(2s)-2-(ethylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound CCNC(=O)[C@@H]1CCCN1C(=O)COC1=CC(C(=O)N[C@@H](CCC(O)=O)C(=O)N2CCN(CC2)C(=O)OCC)=NN1C1=CC=CC=C1 KWCKTXOCWXSWQQ-UPVQGACJSA-N 0.000 claims 1
WKTGDAXCYAFQKO-FUDKSRODSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-4-[[5-[2-[(2s,4s)-4-hydroxy-2-methoxycarbonylpyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](C[C@H](O)C2)C(=O)OC)=C1 WKTGDAXCYAFQKO-FUDKSRODSA-N 0.000 claims 1
NYKNIJKWPCYBKO-RTWAWAEBSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-4-[[5-[2-[(3r)-3-hydroxypyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2C[C@H](O)CC2)=C1 NYKNIJKWPCYBKO-RTWAWAEBSA-N 0.000 claims 1
UGUNAIGOTVMNIG-QSAPEBAKSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-4-[[5-[2-[2-(5-methylfuran-2-yl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2C(CCC2)C=2OC(C)=CC=2)=C1 UGUNAIGOTVMNIG-QSAPEBAKSA-N 0.000 claims 1
JGBNSEJWSZGPAU-LFQPHHBNSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-4-[[5-[2-[2-(furan-2-yl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2C(CCC2)C=2OC=CC=2)=C1 JGBNSEJWSZGPAU-LFQPHHBNSA-N 0.000 claims 1
FXKWIQMWWCEJHH-YANBTOMASA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-4-[[5-[2-[3-(2-fluoroethylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2CC(CC2)C(=O)NCCF)=C1 FXKWIQMWWCEJHH-YANBTOMASA-N 0.000 claims 1
WGRZKOAGMIWRQR-QHCPKHFHSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-4-[[5-[2-[4-(2-hydroxyethyl)piperazin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2CCN(CCO)CC2)=C1 WGRZKOAGMIWRQR-QHCPKHFHSA-N 0.000 claims 1
UJPNXGVZSCCCDK-NRFANRHFSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxo-4-[[5-(2-oxo-2-pyrrolidin-1-ylethoxy)-1-phenylpyrazole-3-carbonyl]amino]pentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2CCCC2)=C1 UJPNXGVZSCCCDK-NRFANRHFSA-N 0.000 claims 1
BTRSCHURPZANJE-LFQPHHBNSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxo-4-[[5-[2-oxo-2-(2-thiophen-2-ylpyrrolidin-1-yl)ethoxy]-1-phenylpyrazole-3-carbonyl]amino]pentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2C(CCC2)C=2SC=CC=2)=C1 BTRSCHURPZANJE-LFQPHHBNSA-N 0.000 claims 1
SUNXWUQJCHCXIV-FQEVSTJZSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxo-4-[[5-[2-oxo-2-(3-oxopiperazin-1-yl)ethoxy]-1-phenylpyrazole-3-carbonyl]amino]pentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2CC(=O)NCC2)=C1 SUNXWUQJCHCXIV-FQEVSTJZSA-N 0.000 claims 1
RMJDGQZTKDWHEZ-GMAHTHKFSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxo-4-[[5-[2-oxo-2-[(2s)-2-(2,2,2-trifluoroethylcarbamoyl)pyrrolidin-1-yl]ethoxy]-1-phenylpyrazole-3-carbonyl]amino]pentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NCC(F)(F)F)=C1 RMJDGQZTKDWHEZ-GMAHTHKFSA-N 0.000 claims 1
LQRKDJIASVQXFQ-BDYUSTAISA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxo-4-[[5-[2-oxo-2-[(2s)-2-(piperidine-1-carbonyl)pyrrolidin-1-yl]ethoxy]-1-phenylpyrazole-3-carbonyl]amino]pentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)N2CCCCC2)=C1 LQRKDJIASVQXFQ-BDYUSTAISA-N 0.000 claims 1
VSFXRBVCYLPUQF-ZCYQVOJMSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxo-4-[[5-[2-oxo-2-[(2s)-2-(propan-2-ylcarbamoyl)pyrrolidin-1-yl]ethoxy]-1-phenylpyrazole-3-carbonyl]amino]pentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC(C)C)=C1 VSFXRBVCYLPUQF-ZCYQVOJMSA-N 0.000 claims 1
FDVYOFZFOFXCOF-ZCYQVOJMSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxo-4-[[5-[2-oxo-2-[(2s)-2-(propylcarbamoyl)pyrrolidin-1-yl]ethoxy]-1-phenylpyrazole-3-carbonyl]amino]pentanoic acid Chemical compound CCCNC(=O)[C@@H]1CCCN1C(=O)COC1=CC(C(=O)N[C@@H](CCC(O)=O)C(=O)N2CCN(CC2)C(=O)OCC)=NN1C1=CC=CC=C1 FDVYOFZFOFXCOF-ZCYQVOJMSA-N 0.000 claims 1
KFUNMCRSFZOQBO-AHWVRZQESA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxo-4-[[5-[2-oxo-2-[(2s)-2-(pyrrolidine-1-carbonyl)pyrrolidin-1-yl]ethoxy]-1-phenylpyrazole-3-carbonyl]amino]pentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)N2CCCC2)=C1 KFUNMCRSFZOQBO-AHWVRZQESA-N 0.000 claims 1
SJJFTMOQIHGUBG-XCZPVHLTSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxo-4-[[5-[2-oxo-2-[(2s)-2-phenylpyrrolidin-1-yl]ethoxy]-1-phenylpyrazole-3-carbonyl]amino]pentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C=2C=CC=CC=2)=C1 SJJFTMOQIHGUBG-XCZPVHLTSA-N 0.000 claims 1
BRKWDYUEUIYDSA-IAXKEJLGSA-N (4s)-5-(4-ethoxycarbonylpiperazin-1-yl)-5-oxo-4-[[5-[2-oxo-2-[3-(2,2,2-trifluoroethylcarbamoyl)pyrrolidin-1-yl]ethoxy]-1-phenylpyrazole-3-carbonyl]amino]pentanoic acid Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2CC(CC2)C(=O)NCC(F)(F)F)=C1 BRKWDYUEUIYDSA-IAXKEJLGSA-N 0.000 claims 1
MBPGDWGWTGFAIG-VTZPFEBOSA-N (4s)-5-[(3r)-4-ethoxycarbonyl-3-methylpiperazin-1-yl]-4-[[5-[2-[(2s)-2-(2-fluoroethylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1[C@@H](C)N(C(=O)OCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NCCF)=C1 MBPGDWGWTGFAIG-VTZPFEBOSA-N 0.000 claims 1
CXGURSKICFDPQR-FKIMBDHASA-N (4s)-5-[3-(butoxycarbonylamino)pyrrolidin-1-yl]-4-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1C(NC(=O)OCCCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 CXGURSKICFDPQR-FKIMBDHASA-N 0.000 claims 1
KMJHAAYPFIJIOB-SMCANUKXSA-N (4s)-5-[4-(3-chlorobenzoyl)piperidin-1-yl]-4-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound O=C([C@@H]1CCCN1C(=O)COC1=CC(=NN1C=1C=CC=CC=1)C(=O)N[C@@H](CCC(=O)O)C(=O)N1CCC(CC1)C(=O)C=1C=C(Cl)C=CC=1)NC1CCC1 KMJHAAYPFIJIOB-SMCANUKXSA-N 0.000 claims 1
SQHJPPLBQIFBAG-YTMVLYRLSA-N (4s)-5-[4-(butoxycarbonylamino)piperidin-1-yl]-4-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoic acid Chemical compound C1CC(NC(=O)OCCCC)CCN1C(=O)[C@H](CCC(O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 SQHJPPLBQIFBAG-YTMVLYRLSA-N 0.000 claims 1
MIZSMGGDTHDBST-SANMLTNESA-N 2-ethoxyethyl 4-[2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]acetyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCOCC)CCN1C(=O)CNC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 MIZSMGGDTHDBST-SANMLTNESA-N 0.000 claims 1
KZLXLGRXTDPOFG-VWLOTQADSA-N 2-methoxyethyl 4-[2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]acetyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCOC)CCN1C(=O)CNC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 KZLXLGRXTDPOFG-VWLOTQADSA-N 0.000 claims 1
PGGCCJGZCSPOPC-DEOSSOPVSA-N 3,3,3-trifluoropropyl 4-[2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]acetyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCC(F)(F)F)CCN1C(=O)CNC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 PGGCCJGZCSPOPC-DEOSSOPVSA-N 0.000 claims 1
125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 1
HIZRNYDPELXOIA-UIOOFZCWSA-N 4-[(2S)-2-[[5-[2-[(2S)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-3-(cyclopropanecarbonylamino)propanoyl]piperazine-1-carboxylic acid Chemical compound C1CN(C(=O)O)CCN1C(=O)[C@@H](NC(=O)C1=NN(C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1)C=1C=CC=CC=1)CNC(=O)C1CC1 HIZRNYDPELXOIA-UIOOFZCWSA-N 0.000 claims 1
JRVZJXLSCJPMLV-YTMVLYRLSA-N 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-[(3-ethyloxetan-3-yl)methoxy]-5-oxopentanoyl]piperazine-1-carboxylic acid Chemical compound C([C@H](NC(=O)C1=NN(C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1)C=1C=CC=CC=1)C(=O)N1CCN(CC1)C(O)=O)CC(=O)OCC1(CC)COC1 JRVZJXLSCJPMLV-YTMVLYRLSA-N 0.000 claims 1
HQFYIMYBLSATJC-XCZPVHLTSA-N 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-[(3-methyloxetan-3-yl)methoxy]-5-oxopentanoyl]piperazine-1-carboxylic acid Chemical compound C([C@H](NC(=O)C1=NN(C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1)C=1C=CC=CC=1)C(=O)N1CCN(CC1)C(O)=O)CC(=O)OCC1(C)COC1 HQFYIMYBLSATJC-XCZPVHLTSA-N 0.000 claims 1
KNNFNZMYFIINRV-NAUKPKSFSA-N 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxo-5-(oxolan-2-ylmethoxy)pentanoyl]piperazine-1-carboxylic acid Chemical compound C1CN(C(=O)O)CCN1C(=O)[C@@H](NC(=O)C1=NN(C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1)C=1C=CC=CC=1)CCC(=O)OCC1OCCC1 KNNFNZMYFIINRV-NAUKPKSFSA-N 0.000 claims 1
QBRLGDYNWJSQKS-TXJYOHDVSA-N 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxo-5-(oxolan-3-ylmethoxy)pentanoyl]piperazine-1-carboxylic acid Chemical compound C1CN(C(=O)O)CCN1C(=O)[C@@H](NC(=O)C1=NN(C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1)C=1C=CC=CC=1)CCC(=O)OCC1COCC1 QBRLGDYNWJSQKS-TXJYOHDVSA-N 0.000 claims 1
YWTVXSBBHDZSKW-SANMLTNESA-N 4-[2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]acetyl]-n-(2-ethoxyethyl)piperazine-1-carboxamide Chemical compound C1CN(C(=O)NCCOCC)CCN1C(=O)CNC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 YWTVXSBBHDZSKW-SANMLTNESA-N 0.000 claims 1
FFUJUQFJSQEMPD-SANMLTNESA-N 4-[2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]acetyl]-n-(2-methoxyethyl)-n-methylpiperazine-1-carboxamide Chemical compound C1CN(C(=O)N(C)CCOC)CCN1C(=O)CNC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 FFUJUQFJSQEMPD-SANMLTNESA-N 0.000 claims 1
KWXDHSXWVVINGH-VWLOTQADSA-N 4-[2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]acetyl]-n-(2-methoxyethyl)piperazine-1-carboxamide Chemical compound C1CN(C(=O)NCCOC)CCN1C(=O)CNC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 KWXDHSXWVVINGH-VWLOTQADSA-N 0.000 claims 1
TXUPMQNJQSMNGC-VWLOTQADSA-N 4-[2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]acetyl]-n-cyclopropylpiperazine-1-carboxamide Chemical compound N1([C@@H](CCC1)C(=O)NC1CCC1)C(=O)COC1=CC(C(=O)NCC(=O)N2CCN(CC2)C(=O)NC2CC2)=NN1C1=CC=CC=C1 TXUPMQNJQSMNGC-VWLOTQADSA-N 0.000 claims 1
VWSRVFXVRYHIKV-QFIPXVFZSA-N 4-[2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]acetyl]piperazine-1-carboxylic acid Chemical compound C1CN(C(=O)O)CCN1C(=O)CNC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 VWSRVFXVRYHIKV-QFIPXVFZSA-N 0.000 claims 1
RRJZVUGWLSNIST-HLADLETHSA-N 5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-n-[(2r)-1-[4-(3-methoxyphenyl)piperazin-1-yl]-1-oxopropan-2-yl]-1-phenylpyrazole-3-carboxamide Chemical compound COC1=CC=CC(N2CCN(CC2)C(=O)[C@@H](C)NC(=O)C2=NN(C(OCC(=O)N3[C@@H](CCC3)C(=O)NC3CCC3)=C2)C=2C=CC=CC=2)=C1 RRJZVUGWLSNIST-HLADLETHSA-N 0.000 claims 1
RRJZVUGWLSNIST-NGQVCNFZSA-N 5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-n-[(2s)-1-[4-(3-methoxyphenyl)piperazin-1-yl]-1-oxopropan-2-yl]-1-phenylpyrazole-3-carboxamide Chemical compound COC1=CC=CC(N2CCN(CC2)C(=O)[C@H](C)NC(=O)C2=NN(C(OCC(=O)N3[C@@H](CCC3)C(=O)NC3CCC3)=C2)C=2C=CC=CC=2)=C1 RRJZVUGWLSNIST-NGQVCNFZSA-N 0.000 claims 1
OWDHCBIUWSZWCS-LSQMVHIFSA-N 5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-n-[2-[4-[(1r,2s)-2-fluorocyclopropanecarbonyl]piperazin-1-yl]-2-oxoethyl]-1-phenylpyrazole-3-carboxamide Chemical compound F[C@H]1C[C@@H]1C(=O)N1CCN(C(=O)CNC(=O)C2=NN(C(OCC(=O)N3[C@@H](CCC3)C(=O)NC3CCC3)=C2)C=2C=CC=CC=2)CC1 OWDHCBIUWSZWCS-LSQMVHIFSA-N 0.000 claims 1
PIGQUDCPVKXIPM-SANMLTNESA-N 5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-n-[2-oxo-2-(4-pentanoylpiperazin-1-yl)ethyl]-1-phenylpyrazole-3-carboxamide Chemical compound C1CN(C(=O)CCCC)CCN1C(=O)CNC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 PIGQUDCPVKXIPM-SANMLTNESA-N 0.000 claims 1
RWYGVTPKGMPOJB-SANMLTNESA-N 5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-n-[2-oxo-2-[4-(pyrrolidine-1-carbonyl)piperazin-1-yl]ethyl]-1-phenylpyrazole-3-carboxamide Chemical compound N1([C@@H](CCC1)C(=O)NC1CCC1)C(=O)COC1=CC(C(=O)NCC(=O)N2CCN(CC2)C(=O)N2CCCC2)=NN1C1=CC=CC=C1 RWYGVTPKGMPOJB-SANMLTNESA-N 0.000 claims 1
PPACOILQDYMUGM-FLBADVGZSA-N 5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-n-[2-oxo-2-[4-[(1r,2r)-2-phenylcyclopropanecarbonyl]piperazin-1-yl]ethyl]-1-phenylpyrazole-3-carboxamide Chemical compound N1([C@@H](CCC1)C(=O)NC1CCC1)C(=O)COC1=CC(C(=O)NCC(=O)N2CCN(CC2)C(=O)[C@H]2[C@@H](C2)C=2C=CC=CC=2)=NN1C1=CC=CC=C1 PPACOILQDYMUGM-FLBADVGZSA-N 0.000 claims 1
KBJQIRQMXQNRIG-FTBISJDPSA-N C(CCC)(=O)N.C1(CCC1)NC(=O)[C@H]1N(CCC1)C(COC1=CC(=NN1C1=CC=CC=C1)C(=O)NCC(=O)N1CCN(CC1)C(=O)O)=O Chemical compound C(CCC)(=O)N.C1(CCC1)NC(=O)[C@H]1N(CCC1)C(COC1=CC(=NN1C1=CC=CC=C1)C(=O)NCC(=O)N1CCN(CC1)C(=O)O)=O KBJQIRQMXQNRIG-FTBISJDPSA-N 0.000 claims 1
125000002947 alkylene group Chemical group 0.000 claims 1
ZRZOOWJFUWBFPM-LJAQVGFWSA-N benzyl 4-[2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]acetyl]piperazine-1-carboxylate Chemical compound N1([C@@H](CCC1)C(=O)NC1CCC1)C(=O)COC1=CC(C(=O)NCC(=O)N2CCN(CC2)C(=O)OCC=2C=CC=CC=2)=NN1C1=CC=CC=C1 ZRZOOWJFUWBFPM-LJAQVGFWSA-N 0.000 claims 1
LLTFAFXLMIEDEU-KCWPFWIISA-N butyl 4-[(2r)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]propanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@@H](C)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 LLTFAFXLMIEDEU-KCWPFWIISA-N 0.000 claims 1
QPZWWHAIOXFYAR-VBTAUBHQSA-N butyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-2-cyclohexylacetyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H](C1CCCCC1)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 QPZWWHAIOXFYAR-VBTAUBHQSA-N 0.000 claims 1
XYJPJAQRAKGULG-IZEXYCQBSA-N butyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-2-cyclopropylacetyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H](C1CC1)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 XYJPJAQRAKGULG-IZEXYCQBSA-N 0.000 claims 1
TYQZULRHPXOIPO-LQJZCPKCSA-N butyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-3-cyclohexylpropanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@@H](NC(=O)C1=NN(C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1)C=1C=CC=CC=1)CC1CCCCC1 TYQZULRHPXOIPO-LQJZCPKCSA-N 0.000 claims 1
QWOGUAIISZQHQX-VMPREFPWSA-N butyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-3-ethoxypropanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H](COCC)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 QWOGUAIISZQHQX-VMPREFPWSA-N 0.000 claims 1
UOGYIEUQOHJXRR-BHBYDHKZSA-N butyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-3-hydroxy-3-methylbutanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H](C(C)(C)O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 UOGYIEUQOHJXRR-BHBYDHKZSA-N 0.000 claims 1
JVSPRVGHPCGHKZ-IZEXYCQBSA-N butyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-3-methylbutanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H](C(C)C)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 JVSPRVGHPCGHKZ-IZEXYCQBSA-N 0.000 claims 1
KSSYMYSUFHKISE-SVBPBHIXSA-N butyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-4,4,4-trifluorobutanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H](CC(F)(F)F)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 KSSYMYSUFHKISE-SVBPBHIXSA-N 0.000 claims 1
ZSTJSSFWPGSNAI-XCZPVHLTSA-N butyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-4-(2h-tetrazol-5-yl)butanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@@H](NC(=O)C1=NN(C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1)C=1C=CC=CC=1)CCC1=NNN=N1 ZSTJSSFWPGSNAI-XCZPVHLTSA-N 0.000 claims 1
APSJKQMVMSMTOQ-KYJUHHDHSA-N butyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-4-methylpentanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H](CC(C)C)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 APSJKQMVMSMTOQ-KYJUHHDHSA-N 0.000 claims 1
XDHANRKAQCNWSC-JDXGNMNLSA-N butyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-ethoxy-5-oxopentanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H](CCC(=O)OCC)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 XDHANRKAQCNWSC-JDXGNMNLSA-N 0.000 claims 1
UGNHUJFAFONAEO-YTMVLYRLSA-N butyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-methoxy-5-oxopentanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H](CCC(=O)OC)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 UGNHUJFAFONAEO-YTMVLYRLSA-N 0.000 claims 1
KLMSWVPDZWWLJR-JDXGNMNLSA-N butyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-6-hydroxyhexanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H](CCCCO)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 KLMSWVPDZWWLJR-JDXGNMNLSA-N 0.000 claims 1
NHBFIZVJDYDSKE-JSXFGMRASA-N butyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-6-phenylmethoxyhexanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@@H](NC(=O)C1=NN(C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1)C=1C=CC=CC=1)CCCCOCC1=CC=CC=C1 NHBFIZVJDYDSKE-JSXFGMRASA-N 0.000 claims 1
CWOVXLRFCDHETC-YTMVLYRLSA-N butyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]pentanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H](CCC)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 CWOVXLRFCDHETC-YTMVLYRLSA-N 0.000 claims 1
LLTFAFXLMIEDEU-HOFKKMOUSA-N butyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]propanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H](C)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 LLTFAFXLMIEDEU-HOFKKMOUSA-N 0.000 claims 1
IWUFZGFZZBSTMS-SMCANUKXSA-N butyl 4-[(2s)-5-acetyloxy-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]pentanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H](CCCOC(C)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 IWUFZGFZZBSTMS-SMCANUKXSA-N 0.000 claims 1
YCLXHHUAQZAENB-ISXOHIFFSA-N butyl 4-[(2s,3r)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-3-methylpentanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H]([C@H](C)CC)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 YCLXHHUAQZAENB-ISXOHIFFSA-N 0.000 claims 1
YCLXHHUAQZAENB-PKLKWBPYSA-N butyl 4-[(2s,3s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-3-methylpentanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)[C@H]([C@@H](C)CC)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 YCLXHHUAQZAENB-PKLKWBPYSA-N 0.000 claims 1
ZVTDRVAULRZHMS-KCWPFWIISA-N butyl 4-[2-[[5-[(2r)-1-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-1-oxopropan-2-yl]oxy-1-phenylpyrazole-3-carbonyl]amino]acetyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)CNC(=O)C1=NN(C=2C=CC=CC=2)C(O[C@H](C)C(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 ZVTDRVAULRZHMS-KCWPFWIISA-N 0.000 claims 1
LCYUXAQLZJAFLT-OFNKIYASSA-N butyl 4-[2-[[5-[(2r)-1-oxo-1-[(2s)-2-(2h-tetrazol-5-yl)pyrrolidin-1-yl]propan-2-yl]oxy-1-phenylpyrazole-3-carbonyl]amino]acetyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)CNC(=O)C1=NN(C=2C=CC=CC=2)C(O[C@H](C)C(=O)N2[C@@H](CCC2)C=2NN=NN=2)=C1 LCYUXAQLZJAFLT-OFNKIYASSA-N 0.000 claims 1
CRTZZHVVDACDKB-VTIINTLQSA-N butyl 4-[2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-3-fluorobutanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)C(C(C)F)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 CRTZZHVVDACDKB-VTIINTLQSA-N 0.000 claims 1
QCKRRHRHLONWIP-SANMLTNESA-N butyl 4-[2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]acetyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)CNC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 QCKRRHRHLONWIP-SANMLTNESA-N 0.000 claims 1
FVLQNMNUVCRIPC-RSXGOPAZSA-N butyl 4-[2-[[5-[2-[(2s,4r)-2-(cyclobutylcarbamoyl)-4-hydroxypyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]acetyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)CNC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](C[C@@H](O)C2)C(=O)NC2CCC2)=C1 FVLQNMNUVCRIPC-RSXGOPAZSA-N 0.000 claims 1
GXDNRLLMLIHVIG-QFIPXVFZSA-N butyl 4-[2-[[5-[2-oxo-2-[(2s)-2-(2h-tetrazol-5-yl)pyrrolidin-1-yl]ethoxy]-1-phenylpyrazole-3-carbonyl]amino]acetyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCCC)CCN1C(=O)CNC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C=2NN=NN=2)=C1 GXDNRLLMLIHVIG-QFIPXVFZSA-N 0.000 claims 1
ZZQTYZKSQUYAGK-SHUZPENHSA-N butyl n-[1-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-2-cyclohexylacetyl]piperidin-4-yl]carbamate Chemical compound C1CC(NC(=O)OCCCC)CCN1C(=O)[C@H](C1CCCCC1)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 ZZQTYZKSQUYAGK-SHUZPENHSA-N 0.000 claims 1
WLEPRAKNSVNNTC-HEVIKAOCSA-N butyl n-[1-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-3-cyclohexylpropanoyl]piperidin-4-yl]carbamate Chemical compound C1CC(NC(=O)OCCCC)CCN1C(=O)[C@@H](NC(=O)C1=NN(C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1)C=1C=CC=CC=1)CC1CCCCC1 WLEPRAKNSVNNTC-HEVIKAOCSA-N 0.000 claims 1
HREPBSLCKMIREZ-CONSDPRKSA-N butyl n-[1-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-4-methylpentanoyl]piperidin-4-yl]carbamate Chemical compound C1CC(NC(=O)OCCCC)CCN1C(=O)[C@H](CC(C)C)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 HREPBSLCKMIREZ-CONSDPRKSA-N 0.000 claims 1
MWJQCQJPYQNLQA-JDXGNMNLSA-N butyl n-[1-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]pentanoyl]piperidin-4-yl]carbamate Chemical compound C1CC(NC(=O)OCCCC)CCN1C(=O)[C@H](CCC)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 MWJQCQJPYQNLQA-JDXGNMNLSA-N 0.000 claims 1
VFMYMXHZXSYKEB-DYMXRVJRSA-N butyl n-[1-[(2s,3s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-3-methylpentanoyl]piperidin-4-yl]carbamate Chemical compound C1CC(NC(=O)OCCCC)CCN1C(=O)[C@H]([C@@H](C)CC)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 VFMYMXHZXSYKEB-DYMXRVJRSA-N 0.000 claims 1
AVASDUAUMSQGEW-MHZLTWQESA-N butyl n-[1-[2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]acetyl]piperidin-4-yl]carbamate Chemical compound C1CC(NC(=O)OCCCC)CCN1C(=O)CNC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 AVASDUAUMSQGEW-MHZLTWQESA-N 0.000 claims 1
LTPCPJABFUVFHQ-AMGIVPHBSA-N cyclobutyl 4-[(2r)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]propanoyl]piperazine-1-carboxylate Chemical compound O=C([C@@H]1CCCN1C(=O)COC1=CC(=NN1C=1C=CC=CC=1)C(=O)N[C@H](C)C(=O)N1CCN(CC1)C(=O)OC1CCC1)NC1CCC1 LTPCPJABFUVFHQ-AMGIVPHBSA-N 0.000 claims 1
ADRMDUXHWXZXQS-YTMVLYRLSA-N cyclobutyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-methoxy-5-oxopentanoyl]piperazine-1-carboxylate Chemical compound O=C([C@@H]1CCCN1C(=O)COC1=CC(=NN1C=1C=CC=CC=1)C(=O)N[C@@H](CCC(=O)OC)C(=O)N1CCN(CC1)C(=O)OC1CCC1)NC1CCC1 ADRMDUXHWXZXQS-YTMVLYRLSA-N 0.000 claims 1
MBQXCJHEIBQRIZ-JDXGNMNLSA-N cyclobutyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-6-hydroxyhexanoyl]piperazine-1-carboxylate Chemical compound O=C([C@@H]1CCCN1C(=O)COC1=CC(=NN1C=1C=CC=CC=1)C(=O)N[C@@H](CCCCO)C(=O)N1CCN(CC1)C(=O)OC1CCC1)NC1CCC1 MBQXCJHEIBQRIZ-JDXGNMNLSA-N 0.000 claims 1
ICKSHNVVCYUMQC-JSXFGMRASA-N cyclobutyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-6-phenylmethoxyhexanoyl]piperazine-1-carboxylate Chemical compound N1([C@@H](CCC1)C(=O)NC1CCC1)C(=O)COC1=CC(C(=O)N[C@@H](CCCCOCC=2C=CC=CC=2)C(=O)N2CCN(CC2)C(=O)OC2CCC2)=NN1C1=CC=CC=C1 ICKSHNVVCYUMQC-JSXFGMRASA-N 0.000 claims 1
LTPCPJABFUVFHQ-CUNXSJBXSA-N cyclobutyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]propanoyl]piperazine-1-carboxylate Chemical compound O=C([C@@H]1CCCN1C(=O)COC1=CC(=NN1C=1C=CC=CC=1)C(=O)N[C@@H](C)C(=O)N1CCN(CC1)C(=O)OC1CCC1)NC1CCC1 LTPCPJABFUVFHQ-CUNXSJBXSA-N 0.000 claims 1
MQYZUGQPPZXHDX-SMCANUKXSA-N cyclobutyl 4-[(2s)-2-[[5-[2-[(2s)-2-[cyclobutyl(methyl)carbamoyl]pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-6-hydroxyhexanoyl]piperazine-1-carboxylate Chemical compound O=C([C@H]1N(CCC1)C(=O)COC=1N(N=C(C=1)C(=O)N[C@@H](CCCCO)C(=O)N1CCN(CC1)C(=O)OC1CCC1)C=1C=CC=CC=1)N(C)C1CCC1 MQYZUGQPPZXHDX-SMCANUKXSA-N 0.000 claims 1
JFEQEDZFHRXLSQ-SANMLTNESA-N cyclobutyl 4-[2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]acetyl]piperazine-1-carboxylate Chemical compound N1([C@@H](CCC1)C(=O)NC1CCC1)C(=O)COC1=CC(C(=O)NCC(=O)N2CCN(CC2)C(=O)OC2CCC2)=NN1C1=CC=CC=C1 JFEQEDZFHRXLSQ-SANMLTNESA-N 0.000 claims 1
125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
WTQOCNBRHHFOCW-DQEYMECFSA-N ethyl 4-[(2r)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-3-fluoropropanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CF)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 WTQOCNBRHHFOCW-DQEYMECFSA-N 0.000 claims 1
LRSVBIQNGGSYIV-BWKNWUBXSA-N ethyl 4-[(2r)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]propanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@@H](C)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 LRSVBIQNGGSYIV-BWKNWUBXSA-N 0.000 claims 1
OBWDOVYUKIBORC-XCZPVHLTSA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-(3,4-difluorophenyl)pyrazole-3-carbonyl]amino]-5-ethoxy-5-oxopentanoyl]piperazine-1-carboxylate Chemical compound O=C([C@@H]1CCCN1C(=O)COC1=CC(=NN1C=1C=C(F)C(F)=CC=1)C(=O)N[C@@H](CCC(=O)OCC)C(=O)N1CCN(CC1)C(=O)OCC)NC1CCC1 OBWDOVYUKIBORC-XCZPVHLTSA-N 0.000 claims 1
DJHCDKZCEKXPIU-XCZPVHLTSA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-(3-fluorophenyl)pyrazole-3-carbonyl]amino]-5-ethylperoxy-5-oxopentanoyl]piperazine-1-carboxylate Chemical compound O=C([C@@H]1CCCN1C(=O)COC1=CC(=NN1C=1C=C(F)C=CC=1)C(=O)N[C@@H](CCC(=O)OOCC)C(=O)N1CCN(CC1)C(=O)OCC)NC1CCC1 DJHCDKZCEKXPIU-XCZPVHLTSA-N 0.000 claims 1
LFMKSBWMXKCPAZ-NYDCQLBNSA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-2-cyclohexylacetyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](C1CCCCC1)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 LFMKSBWMXKCPAZ-NYDCQLBNSA-N 0.000 claims 1
QYFBHRVKSQDRCF-UIOOFZCWSA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-3-(methanesulfonamido)propanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CNS(C)(=O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 QYFBHRVKSQDRCF-UIOOFZCWSA-N 0.000 claims 1
BLMWXCNEZOAUDY-CONSDPRKSA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-3-cyclohexylpropanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@@H](NC(=O)C1=NN(C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1)C=1C=CC=CC=1)CC1CCCCC1 BLMWXCNEZOAUDY-CONSDPRKSA-N 0.000 claims 1
FJAAHTPEVCAROF-WNJJXGMVSA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-3-methylbutanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](C(C)C)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 FJAAHTPEVCAROF-WNJJXGMVSA-N 0.000 claims 1
MCAVZSQLMDFOHN-AXJMSPCVSA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-4,5-dihydroxypentanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CC(O)CO)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 MCAVZSQLMDFOHN-AXJMSPCVSA-N 0.000 claims 1
MHGWYEUCPODGRK-YTMVLYRLSA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-4-(2-methylpropanoylamino)butanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCNC(=O)C(C)C)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 MHGWYEUCPODGRK-YTMVLYRLSA-N 0.000 claims 1
WWQPPZJEYLRXEO-BDYUSTAISA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-4-(methanesulfonamido)butanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCNS(C)(=O)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 WWQPPZJEYLRXEO-BDYUSTAISA-N 0.000 claims 1
KMIZZPXVINTZPC-BDYUSTAISA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-4-(methoxycarbonylamino)butanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCNC(=O)OC)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 KMIZZPXVINTZPC-BDYUSTAISA-N 0.000 claims 1
LCBRGTYHHYDBEL-AHWVRZQESA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-4-(trifluoromethylsulfonylamino)butanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCNS(=O)(=O)C(F)(F)F)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 LCBRGTYHHYDBEL-AHWVRZQESA-N 0.000 claims 1
ARBAHZWLLWIEGT-AHWVRZQESA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-4-hydroxybutanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCO)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 ARBAHZWLLWIEGT-AHWVRZQESA-N 0.000 claims 1
DVIVWRMDYPINTI-NSOVKSMOSA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-4-methylpentanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CC(C)C)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 DVIVWRMDYPINTI-NSOVKSMOSA-N 0.000 claims 1
BFYYXHPVXAOVGB-JDXGNMNLSA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-(2-methylpropoxy)-5-oxopentanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(=O)OCC(C)C)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 BFYYXHPVXAOVGB-JDXGNMNLSA-N 0.000 claims 1
UAVCDFLXSPTEDK-JDXGNMNLSA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-cyclobutyloxy-5-oxopentanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@@H](NC(=O)C1=NN(C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1)C=1C=CC=CC=1)CCC(=O)OC1CCC1 UAVCDFLXSPTEDK-JDXGNMNLSA-N 0.000 claims 1
GSKQUAOEOZMZRT-CDZUIXILSA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-cyclohexyloxy-5-oxopentanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@@H](NC(=O)C1=NN(C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1)C=1C=CC=CC=1)CCC(=O)OC1CCCCC1 GSKQUAOEOZMZRT-CDZUIXILSA-N 0.000 claims 1
YQZRBXMVSDTDEZ-SMCANUKXSA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-cyclopentyloxy-5-oxopentanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@@H](NC(=O)C1=NN(C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1)C=1C=CC=CC=1)CCC(=O)OC1CCCC1 YQZRBXMVSDTDEZ-SMCANUKXSA-N 0.000 claims 1
OUURAPUWSPNPLN-XCZPVHLTSA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-ethoxy-5-oxopentanoyl]piperazine-1-carboxylate Chemical compound O=C([C@@H]1CCCN1C(=O)COC1=CC(=NN1C=1C=CC=CC=1)C(=O)N[C@@H](CCC(=O)OCC)C(=O)N1CCN(CC1)C(=O)OCC)NC1CCC1 OUURAPUWSPNPLN-XCZPVHLTSA-N 0.000 claims 1
BHNVPGVBMQIGJR-BDYUSTAISA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-methoxy-5-oxopentanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(=O)OC)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 BHNVPGVBMQIGJR-BDYUSTAISA-N 0.000 claims 1
ALWPZAAYKBLOQV-WEZIJMHWSA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxo-5-phenylmethoxypentanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@@H](NC(=O)C1=NN(C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1)C=1C=CC=CC=1)CCC(=O)OCC1=CC=CC=C1 ALWPZAAYKBLOQV-WEZIJMHWSA-N 0.000 claims 1
DQQLQKWXUHZQGH-YTMVLYRLSA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxo-5-propan-2-yloxypentanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCC(=O)OC(C)C)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 DQQLQKWXUHZQGH-YTMVLYRLSA-N 0.000 claims 1
IXZWJDAELHXPOS-YTMVLYRLSA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxo-5-propoxypentanoyl]piperazine-1-carboxylate Chemical compound O=C([C@@H]1CCCN1C(=O)COC1=CC(=NN1C=1C=CC=CC=1)C(=O)N[C@@H](CCC(=O)OCCC)C(=O)N1CCN(CC1)C(=O)OCC)NC1CCC1 IXZWJDAELHXPOS-YTMVLYRLSA-N 0.000 claims 1
SGVVXXNCQPFEJU-BDYUSTAISA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]pentanoyl]piperazine-1-carboxylate Chemical compound O=C([C@@H]1CCCN1C(=O)COC1=CC(=NN1C=1C=CC=CC=1)C(=O)N[C@@H](CCC)C(=O)N1CCN(CC1)C(=O)OCC)NC1CCC1 SGVVXXNCQPFEJU-BDYUSTAISA-N 0.000 claims 1
LRSVBIQNGGSYIV-OFVILXPXSA-N ethyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]propanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](C)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 LRSVBIQNGGSYIV-OFVILXPXSA-N 0.000 claims 1
RLSRGSAWLGNGIU-SVBPBHIXSA-N ethyl 4-[(2s)-3-acetamido-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]propanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CNC(C)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 RLSRGSAWLGNGIU-SVBPBHIXSA-N 0.000 claims 1
APIFTIXALFFAGR-XCZPVHLTSA-N ethyl 4-[(2s)-4-acetamido-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]butanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H](CCNC(C)=O)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 APIFTIXALFFAGR-XCZPVHLTSA-N 0.000 claims 1
FRORZHNCDBMCJG-JDXGNMNLSA-N ethyl 4-[(2s)-5-butoxy-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-oxopentanoyl]piperazine-1-carboxylate Chemical compound O=C([C@@H]1CCCN1C(=O)COC1=CC(=NN1C=1C=CC=CC=1)C(=O)N[C@@H](CCC(=O)OCCCC)C(=O)N1CCN(CC1)C(=O)OCC)NC1CCC1 FRORZHNCDBMCJG-JDXGNMNLSA-N 0.000 claims 1
PGUGGZIJQQNIHB-VZPHFUHGSA-N ethyl 4-[(2s,3s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-3-methylpentanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)[C@H]([C@@H](C)CC)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 PGUGGZIJQQNIHB-VZPHFUHGSA-N 0.000 claims 1
UDUMLBQHGUPVHT-DEOSSOPVSA-N ethyl 4-[2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]acetyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCC)CCN1C(=O)CNC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 UDUMLBQHGUPVHT-DEOSSOPVSA-N 0.000 claims 1
LNOQURRKNJKKBU-UHFFFAOYSA-N ethyl piperazine-1-carboxylate Chemical compound CCOC(=O)N1CCNCC1 LNOQURRKNJKKBU-UHFFFAOYSA-N 0.000 claims 1
125000005843 halogen group Chemical group 0.000 claims 1
VKECJWZCWDOKCR-PMERELPUSA-N n-benzyl-4-[2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]acetyl]-n-methylpiperazine-1-carboxamide Chemical compound C1CN(C(=O)CNC(=O)C2=NN(C(OCC(=O)N3[C@@H](CCC3)C(=O)NC3CCC3)=C2)C=2C=CC=CC=2)CCN1C(=O)N(C)CC1=CC=CC=C1 VKECJWZCWDOKCR-PMERELPUSA-N 0.000 claims 1
YSKIJSPVFQBJOP-MHZLTWQESA-N n-butyl-4-[2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]acetyl]-n-methylpiperazine-1-carboxamide Chemical compound C1CN(C(=O)N(C)CCCC)CCN1C(=O)CNC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 YSKIJSPVFQBJOP-MHZLTWQESA-N 0.000 claims 1
125000004430 oxygen atom Chemical group O* 0.000 claims 1
239000008194 pharmaceutical composition Substances 0.000 claims 1
NAKFXPXVMCUGMH-GJZUVCINSA-N propyl 4-[(2r)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]propanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCC)CCN1C(=O)[C@@H](C)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 NAKFXPXVMCUGMH-GJZUVCINSA-N 0.000 claims 1
FWLXTUWSNZRATD-UIOOFZCWSA-N propyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-4,4,4-trifluorobutanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCC)CCN1C(=O)[C@H](CC(F)(F)F)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 FWLXTUWSNZRATD-UIOOFZCWSA-N 0.000 claims 1
FFSONOWVFLOWCG-XCZPVHLTSA-N propyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-5-methoxy-5-oxopentanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCC)CCN1C(=O)[C@H](CCC(=O)OC)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 FFSONOWVFLOWCG-XCZPVHLTSA-N 0.000 claims 1
NAKFXPXVMCUGMH-NVQXNPDNSA-N propyl 4-[(2s)-2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]propanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCC)CCN1C(=O)[C@H](C)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 NAKFXPXVMCUGMH-NVQXNPDNSA-N 0.000 claims 1
RJPKFEVUYCAIEM-GDWJQBMWSA-N propyl 4-[2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]-3-fluorobutanoyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCC)CCN1C(=O)C(C(C)F)NC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 RJPKFEVUYCAIEM-GDWJQBMWSA-N 0.000 claims 1
XISVTHUQQNHZAZ-VWLOTQADSA-N propyl 4-[2-[[5-[2-[(2s)-2-(cyclobutylcarbamoyl)pyrrolidin-1-yl]-2-oxoethoxy]-1-phenylpyrazole-3-carbonyl]amino]acetyl]piperazine-1-carboxylate Chemical compound C1CN(C(=O)OCCC)CCN1C(=O)CNC(=O)C1=NN(C=2C=CC=CC=2)C(OCC(=O)N2[C@@H](CCC2)C(=O)NC2CCC2)=C1 XISVTHUQQNHZAZ-VWLOTQADSA-N 0.000 claims 1
125000003226 pyrazolyl group Chemical group 0.000 claims 1
125000006413 ring segment Chemical group 0.000 claims 1
DCKVNWZUADLDEH-UHFFFAOYSA-N sec-butyl acetate Chemical compound CCC(C)OC(C)=O DCKVNWZUADLDEH-UHFFFAOYSA-N 0.000 claims 1

JP2010540046A 2007-12-26 2008-12-12 Ｐ２ｙ１２アンタゴニストとしてのヘテロサイクリックピラゾール−カルボキサミド Expired - Fee Related JP5504171B2 (ja)