JP2014521701A5 - - Google Patents
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- Publication number
- JP2014521701A5 JP2014521701A5 JP2014524152A JP2014524152A JP2014521701A5 JP 2014521701 A5 JP2014521701 A5 JP 2014521701A5 JP 2014524152 A JP2014524152 A JP 2014524152A JP 2014524152 A JP2014524152 A JP 2014524152A JP 2014521701 A5 JP2014521701 A5 JP 2014521701A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- alkyl
- oxo
- chloro
- fluorophenyl
- 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.)
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- -1 methoxy, ethoxy Chemical group 0.000 claims 125
- 125000000217 alkyl group Chemical group 0.000 claims 118
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 80
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 67
- 229910052739 hydrogen Inorganic materials 0.000 claims 58
- 229910052799 carbon Inorganic materials 0.000 claims 37
- 229910052736 halogen Inorganic materials 0.000 claims 37
- 150000002367 halogens Chemical class 0.000 claims 37
- 150000003839 salts Chemical class 0.000 claims 32
- 125000000623 heterocyclic group Chemical group 0.000 claims 31
- 229910052731 fluorine Inorganic materials 0.000 claims 25
- 150000001875 compounds Chemical class 0.000 claims 20
- 229910052757 nitrogen Chemical group 0.000 claims 19
- 239000012453 solvate Substances 0.000 claims 16
- 125000004432 carbon atom Chemical group C* 0.000 claims 15
- 125000005842 heteroatom Chemical group 0.000 claims 15
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 15
- 125000003545 alkoxy group Chemical group 0.000 claims 14
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 14
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 12
- 229910052760 oxygen Inorganic materials 0.000 claims 12
- 229910052801 chlorine Inorganic materials 0.000 claims 11
- 125000002947 alkylene group Chemical group 0.000 claims 7
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 6
- 208000001435 Thromboembolism Diseases 0.000 claims 6
- 125000004450 alkenylene group Chemical group 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 6
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims 5
- 125000001188 haloalkyl group Chemical group 0.000 claims 5
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 4
- 239000003795 chemical substances by application Substances 0.000 claims 4
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 4
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 3
- 125000002837 carbocyclic group Chemical group 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Chemical group COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 3
- 208000007536 Thrombosis Diseases 0.000 claims 2
- 206010047249 Venous thrombosis Diseases 0.000 claims 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 230000002526 effect on cardiovascular system Effects 0.000 claims 2
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- LVWZTYCIRDMTEY-UHFFFAOYSA-N metamizole Chemical group O=C1C(N(CS(O)(=O)=O)C)=C(C)N(C)N1C1=CC=CC=C1 LVWZTYCIRDMTEY-UHFFFAOYSA-N 0.000 claims 2
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical group C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 claims 2
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 1
- 125000001414 1,2,4-triazol-5-yl group Chemical group [H]N1N=C([H])N=C1[*] 0.000 claims 1
- 125000004509 1,3,4-oxadiazol-2-yl group Chemical group O1C(=NN=C1)* 0.000 claims 1
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 1
- 125000004938 5-pyridyl group Chemical group N1=CC=CC(=C1)* 0.000 claims 1
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 206010002388 Angina unstable Diseases 0.000 claims 1
- 200000000007 Arterial disease Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010003658 Atrial Fibrillation Diseases 0.000 claims 1
- 206010008088 Cerebral artery embolism Diseases 0.000 claims 1
- 206010008092 Cerebral artery thrombosis Diseases 0.000 claims 1
- 206010011091 Coronary artery thrombosis Diseases 0.000 claims 1
- 206010051055 Deep vein thrombosis Diseases 0.000 claims 1
- 206010014513 Embolism arterial Diseases 0.000 claims 1
- 208000010378 Pulmonary Embolism Diseases 0.000 claims 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical group C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 1
- 206010063544 Renal embolism Diseases 0.000 claims 1
- 208000007814 Unstable Angina Diseases 0.000 claims 1
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 230000002490 cerebral effect Effects 0.000 claims 1
- 208000002528 coronary thrombosis Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 210000002837 heart atrium Anatomy 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 239000007943 implant Substances 0.000 claims 1
- 201000004332 intermediate coronary syndrome Diseases 0.000 claims 1
- 201000010849 intracranial embolism Diseases 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- SXQFCVDSOLSHOQ-UHFFFAOYSA-N lactamide Chemical compound CC(O)C(N)=O SXQFCVDSOLSHOQ-UHFFFAOYSA-N 0.000 claims 1
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 230000003836 peripheral circulation Effects 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 1
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 1
- FPOLWERNILTNDK-UHFFFAOYSA-N pyruvamide Chemical compound CC(=O)C(N)=O FPOLWERNILTNDK-UHFFFAOYSA-N 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 201000005060 thrombophlebitis Diseases 0.000 claims 1
- 230000001052 transient effect Effects 0.000 claims 1
- 230000002861 ventricular Effects 0.000 claims 1
- 0 CC(CCCC(*(C(C(*=*1)=C(*)*1c1c(*=C)c(*)ccc1)=O)=C)C(C)=*C(c1ccc(*)cc1*1)=C(*)*)C1=O Chemical compound CC(CCCC(*(C(C(*=*1)=C(*)*1c1c(*=C)c(*)ccc1)=O)=C)C(C)=*C(c1ccc(*)cc1*1)=C(*)*)C1=O 0.000 description 14
- RYNDLQHJFGSRDC-IBGZPJMESA-N COC(Nc(cc1)cc(NC(CCCC[C@@H]2NC(c3c[n](-c4cc(Cl)ccc4)nn3)=O)=O)c1-c1c[nH]c2n1)=O Chemical compound COC(Nc(cc1)cc(NC(CCCC[C@@H]2NC(c3c[n](-c4cc(Cl)ccc4)nn3)=O)=O)c1-c1c[nH]c2n1)=O RYNDLQHJFGSRDC-IBGZPJMESA-N 0.000 description 1
- PRPMIMZGWAQTMC-IBGZPJMESA-N COC(Nc(cc1)cc(NC(CCCC[C@@H]2NC(c3cc(-c4cc(Cl)ccc4)n[o]3)=O)=O)c1-c1c[nH]c2n1)=O Chemical compound COC(Nc(cc1)cc(NC(CCCC[C@@H]2NC(c3cc(-c4cc(Cl)ccc4)n[o]3)=O)=O)c1-c1c[nH]c2n1)=O PRPMIMZGWAQTMC-IBGZPJMESA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161515401P | 2011-08-05 | 2011-08-05 | |
| US61/515,401 | 2011-08-05 | ||
| PCT/US2012/049706 WO2013022818A1 (en) | 2011-08-05 | 2012-08-06 | Novel macrocycles as factor xia inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014521701A JP2014521701A (ja) | 2014-08-28 |
| JP2014521701A5 true JP2014521701A5 (cg-RX-API-DMAC7.html) | 2015-09-24 |
| JP6158181B2 JP6158181B2 (ja) | 2017-07-05 |
Family
ID=46889416
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014524152A Active JP6158181B2 (ja) | 2011-08-05 | 2012-08-06 | 第ｘｉａ因子阻害剤としての新規大環状分子 |
Country Status (22)
Families Citing this family (49)
| Publication number | Priority date | Publication date | Assignee | Title |
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| TWI577665B (zh) | 2010-02-11 | 2017-04-11 | 必治妥美雅史谷比公司 | 作為因子ｘｉａ抑制劑之巨環類 |
| TW201311689A (zh) | 2011-08-05 | 2013-03-16 | 必治妥美雅史谷比公司 | 作為因子ｘｉａ抑制劑之新穎巨環化合物 |
| TW201319068A (zh) | 2011-08-05 | 2013-05-16 | 必治妥美雅史谷比公司 | 作為ｘｉａ因子抑制劑之環狀ｐ１接合劑 |
| WO2013056034A1 (en) | 2011-10-14 | 2013-04-18 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| EP2766345B1 (en) | 2011-10-14 | 2016-03-16 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| RS56168B1 (sr) | 2011-10-14 | 2017-11-30 | Bristol Myers Squibb Co | Supstituisana jedinjenja tetrahidroizohinolina kao inhibitori xia faktora |
| BR112015002081A2 (pt) * | 2012-08-03 | 2017-07-04 | Bristol Myers Squibb Co | di-hidropiridona p1 como inibidores de fator xia |
| US9376444B2 (en) * | 2012-08-03 | 2016-06-28 | Bristol-Myers Squibb Company | Dihydropyridone P1 as factor XIa inhibitors |
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| WO2014059202A1 (en) | 2012-10-12 | 2014-04-17 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| AU2013329125B2 (en) | 2012-10-12 | 2017-03-30 | Bristol-Myers Squibb Company | Crystalline forms of a factor XIa inhibitor |
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| HRP20220059T1 (hr) | 2015-10-01 | 2022-04-15 | Biocryst Pharmaceuticals, Inc. | Inhibitori kalikreina humane plazme |
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| TWI577665B (zh) | 2010-02-11 | 2017-04-11 | 必治妥美雅史谷比公司 | 作為因子ｘｉａ抑制劑之巨環類 |
| TW201311689A (zh) | 2011-08-05 | 2013-03-16 | 必治妥美雅史谷比公司 | 作為因子ｘｉａ抑制劑之新穎巨環化合物 |
| TW201319068A (zh) | 2011-08-05 | 2013-05-16 | 必治妥美雅史谷比公司 | 作為ｘｉａ因子抑制劑之環狀ｐ１接合劑 |
| EP2766345B1 (en) | 2011-10-14 | 2016-03-16 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| WO2013056034A1 (en) | 2011-10-14 | 2013-04-18 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| RS56168B1 (sr) | 2011-10-14 | 2017-11-30 | Bristol Myers Squibb Co | Supstituisana jedinjenja tetrahidroizohinolina kao inhibitori xia faktora |
| BR112015002081A2 (pt) | 2012-08-03 | 2017-07-04 | Bristol Myers Squibb Co | di-hidropiridona p1 como inibidores de fator xia |
| US9376444B2 (en) | 2012-08-03 | 2016-06-28 | Bristol-Myers Squibb Company | Dihydropyridone P1 as factor XIa inhibitors |
| AU2013329125B2 (en) | 2012-10-12 | 2017-03-30 | Bristol-Myers Squibb Company | Crystalline forms of a factor XIa inhibitor |
| US9403774B2 (en) | 2012-10-12 | 2016-08-02 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| WO2014059202A1 (en) | 2012-10-12 | 2014-04-17 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
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2015
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