JP2015528022A5 - - Google Patents
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- Publication number
- JP2015528022A5 JP2015528022A5 JP2015525622A JP2015525622A JP2015528022A5 JP 2015528022 A5 JP2015528022 A5 JP 2015528022A5 JP 2015525622 A JP2015525622 A JP 2015525622A JP 2015525622 A JP2015525622 A JP 2015525622A JP 2015528022 A5 JP2015528022 A5 JP 2015528022A5
- Authority
- JP
- Japan
- Prior art keywords
- oxo
- methyl
- nonadeca
- tetrahydropyridin
- 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.)
- Granted
Links
- -1 amino, substituted amino Chemical group 0.000 claims 214
- 125000000217 alkyl group Chemical group 0.000 claims 137
- 125000000623 heterocyclic group Chemical group 0.000 claims 135
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 102
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 54
- 229910052736 halogen Inorganic materials 0.000 claims 52
- 150000002367 halogens Chemical class 0.000 claims 52
- 229910052739 hydrogen Inorganic materials 0.000 claims 50
- 229910052799 carbon Inorganic materials 0.000 claims 49
- 150000003839 salts Chemical class 0.000 claims 41
- 125000003118 aryl group Chemical group 0.000 claims 36
- 229910052731 fluorine Inorganic materials 0.000 claims 36
- 125000003545 alkoxy group Chemical group 0.000 claims 30
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 28
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 27
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 25
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 24
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical group FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims 22
- 229910052801 chlorine Inorganic materials 0.000 claims 19
- 125000000753 cycloalkyl group Chemical group 0.000 claims 18
- 125000001188 haloalkyl group Chemical group 0.000 claims 16
- 229910052760 oxygen Inorganic materials 0.000 claims 16
- 229910052794 bromium Inorganic materials 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 15
- OKAUTHXMCHAZTR-UHFFFAOYSA-N carbamic acid;2,2,2-trifluoroacetic acid Chemical compound NC(O)=O.OC(=O)C(F)(F)F.OC(=O)C(F)(F)F OKAUTHXMCHAZTR-UHFFFAOYSA-N 0.000 claims 12
- 125000003342 alkenyl group Chemical group 0.000 claims 11
- 125000002837 carbocyclic group Chemical group 0.000 claims 11
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 10
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 10
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 8
- 229910052757 nitrogen Inorganic materials 0.000 claims 8
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 208000035475 disorder Diseases 0.000 claims 7
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 7
- 125000004438 haloalkoxy group Chemical group 0.000 claims 7
- 230000009424 thromboembolic effect Effects 0.000 claims 7
- JFDZBHWFFUWGJE-UHFFFAOYSA-N benzenecarbonitrile Natural products N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 claims 6
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 6
- 101100516554 Caenorhabditis elegans nhr-5 gene Proteins 0.000 claims 5
- 229910052740 iodine Inorganic materials 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 125000003831 tetrazolyl group Chemical group 0.000 claims 5
- 125000001425 triazolyl group Chemical group 0.000 claims 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 5
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000003386 piperidinyl group Chemical group 0.000 claims 4
- DLFVBJFMPXGRIB-UHFFFAOYSA-N thioacetamide Natural products CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 4
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 3
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- 208000007536 Thrombosis Diseases 0.000 claims 3
- 125000004450 alkenylene group Chemical group 0.000 claims 3
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 150000001721 carbon Chemical group 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 3
- 125000003373 pyrazinyl group Chemical group 0.000 claims 3
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 3
- UMGDCJDMYOKAJW-UHFFFAOYSA-N thiourea Chemical compound NC(N)=S UMGDCJDMYOKAJW-UHFFFAOYSA-N 0.000 claims 3
- 125000001607 1,2,3-triazol-1-yl group Chemical group [*]N1N=NC([H])=C1[H] 0.000 claims 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 2
- 206010047249 Venous thrombosis Diseases 0.000 claims 2
- 230000002526 effect on cardiovascular system Effects 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- GLAXWKVTVJLVKU-UHFFFAOYSA-N guanidine 2,2,2-trifluoroacetic acid Chemical compound NC(N)=N.OC(=O)C(F)(F)F.OC(=O)C(F)(F)F GLAXWKVTVJLVKU-UHFFFAOYSA-N 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 125000004306 triazinyl group Chemical group 0.000 claims 2
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 claims 1
- 125000001359 1,2,3-triazol-4-yl group Chemical group [H]N1N=NC([*])=C1[H] 0.000 claims 1
- 125000003626 1,2,4-triazol-1-yl group Chemical group [*]N1N=C([H])N=C1[H] 0.000 claims 1
- AAILEWXSEQLMNI-UHFFFAOYSA-N 1h-pyridazin-6-one Chemical compound OC1=CC=CN=N1 AAILEWXSEQLMNI-UHFFFAOYSA-N 0.000 claims 1
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])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
- 125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims 1
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000004207 3-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(OC([H])([H])[H])=C1[H] 0.000 claims 1
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims 1
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims 1
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 206010002388 Angina unstable 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
- 208000005189 Embolism Diseases 0.000 claims 1
- 206010014513 Embolism arterial Diseases 0.000 claims 1
- 208000032382 Ischaemic stroke Diseases 0.000 claims 1
- 208000010378 Pulmonary Embolism Diseases 0.000 claims 1
- 206010037437 Pulmonary thrombosis Diseases 0.000 claims 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 239000007983 Tris buffer Substances 0.000 claims 1
- 208000007814 Unstable Angina Diseases 0.000 claims 1
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Natural products NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 1
- 125000003668 acetyloxy group Chemical group [H]C([H])([H])C(=O)O[*] 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
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 210000005242 cardiac chamber Anatomy 0.000 claims 1
- 208000002528 coronary thrombosis Diseases 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 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
- 210000003734 kidney Anatomy 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- LVWZTYCIRDMTEY-UHFFFAOYSA-N metamizole Chemical compound O=C1C(N(CS(O)(=O)=O)C)=C(C)N(C)N1C1=CC=CC=C1 LVWZTYCIRDMTEY-UHFFFAOYSA-N 0.000 claims 1
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 230000000414 obstructive effect Effects 0.000 claims 1
- 229940049964 oleate Drugs 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 230000003836 peripheral circulation Effects 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 1
- 125000002206 pyridazin-3-yl group Chemical group [H]C1=C([H])C([H])=C(*)N=N1 0.000 claims 1
- PBMFSQRYOILNGV-UHFFFAOYSA-N pyridazine Chemical compound C1=CC=NN=C1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 claims 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 1
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 1
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 150000003536 tetrazoles Chemical class 0.000 claims 1
- 201000005060 thrombophlebitis Diseases 0.000 claims 1
- 230000001052 transient effect Effects 0.000 claims 1
- 150000003852 triazoles Chemical class 0.000 claims 1
- 0 Cc1c(*)[n]c(C)n1 Chemical compound Cc1c(*)[n]c(C)n1 0.000 description 65
- CYTDIDQGTYBGRI-UHFFFAOYSA-N Cc(cc1)cc(C)[n+]1OC Chemical compound Cc(cc1)cc(C)[n+]1OC CYTDIDQGTYBGRI-UHFFFAOYSA-N 0.000 description 3
- UZOFELREXGAFOI-UHFFFAOYSA-N CC1CCNCC1 Chemical compound CC1CCNCC1 UZOFELREXGAFOI-UHFFFAOYSA-N 0.000 description 2
- JYYNAJVZFGKDEQ-UHFFFAOYSA-N Cc1ccnc(C)c1 Chemical compound Cc1ccnc(C)c1 JYYNAJVZFGKDEQ-UHFFFAOYSA-N 0.000 description 2
- QYMGRIFMUQCAJW-UHFFFAOYSA-N C1NC=CN=C1 Chemical compound C1NC=CN=C1 QYMGRIFMUQCAJW-UHFFFAOYSA-N 0.000 description 1
- OGBZELSUKYODHJ-UHFFFAOYSA-N CC(C)(C)c1nccc(C)c1 Chemical compound CC(C)(C)c1nccc(C)c1 OGBZELSUKYODHJ-UHFFFAOYSA-N 0.000 description 1
- FNRZUEIDSCTPBY-UHFFFAOYSA-N Cc(cc1C=C)c(C)cc1N Chemical compound Cc(cc1C=C)c(C)cc1N FNRZUEIDSCTPBY-UHFFFAOYSA-N 0.000 description 1
- NURQLCJSMXZBPC-UHFFFAOYSA-N Cc1c(C)cncc1 Chemical compound Cc1c(C)cncc1 NURQLCJSMXZBPC-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261679197P | 2012-08-03 | 2012-08-03 | |
| US61/679,197 | 2012-08-03 | ||
| US201361787081P | 2013-03-15 | 2013-03-15 | |
| US61/787,081 | 2013-03-15 | ||
| PCT/US2013/053416 WO2014022767A1 (en) | 2012-08-03 | 2013-08-02 | Dihydropyridone p1 as factor xia inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015528022A JP2015528022A (ja) | 2015-09-24 |
| JP2015528022A5 true JP2015528022A5 (OSRAM) | 2016-04-14 |
| JP6082463B2 JP6082463B2 (ja) | 2017-02-15 |
Family
ID=48949290
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015525622A Active JP6082463B2 (ja) | 2012-08-03 | 2013-08-02 | 第ｘｉａ因子阻害剤としてのジヒドロピリドンｐ１ |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US9409908B2 (OSRAM) |
| EP (1) | EP2880026B1 (OSRAM) |
| JP (1) | JP6082463B2 (OSRAM) |
| KR (1) | KR20150038372A (OSRAM) |
| CN (2) | CN108250199B (OSRAM) |
| AR (1) | AR091981A1 (OSRAM) |
| AU (1) | AU2013296259A1 (OSRAM) |
| BR (1) | BR112015002081A2 (OSRAM) |
| CA (1) | CA2880866A1 (OSRAM) |
| CY (1) | CY1119004T1 (OSRAM) |
| DK (1) | DK2880026T3 (OSRAM) |
| EA (1) | EA028581B1 (OSRAM) |
| ES (1) | ES2623175T3 (OSRAM) |
| HR (1) | HRP20170506T1 (OSRAM) |
| HU (1) | HUE032622T2 (OSRAM) |
| IL (1) | IL237011A0 (OSRAM) |
| LT (1) | LT2880026T (OSRAM) |
| MX (1) | MX361759B (OSRAM) |
| PL (1) | PL2880026T3 (OSRAM) |
| PT (1) | PT2880026T (OSRAM) |
| RS (1) | RS55975B1 (OSRAM) |
| SG (1) | SG11201500271UA (OSRAM) |
| SI (1) | SI2880026T1 (OSRAM) |
| SM (1) | SMT201700240T1 (OSRAM) |
| TW (1) | TW201410667A (OSRAM) |
| UY (1) | UY34960A (OSRAM) |
| WO (1) | WO2014022767A1 (OSRAM) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| PL2766346T3 (pl) | 2011-10-14 | 2017-09-29 | Bristol-Myers Squibb Company | Podstawione związki tetrahydroizochinoliny jako inhibitory czynnika XIA |
| IN2014CN02806A (OSRAM) | 2011-10-14 | 2015-07-03 | Bristol Myers Squibb Co | |
| JP6033318B2 (ja) | 2011-10-14 | 2016-11-30 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | 第ＸＩａ因子阻害剤としての置換テトラヒドロイソキノリン化合物 |
| EP2906541B1 (en) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| US9315519B2 (en) | 2012-10-12 | 2016-04-19 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors |
| EA032092B1 (ru) | 2012-10-12 | 2019-04-30 | Бристол-Майерс Сквибб Компани | Кристаллические формы ингибитора фактора xia |
| JP6479763B2 (ja) | 2013-03-25 | 2019-03-06 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | 第ｘｉａ因子阻害剤としての置換アゾール含有のテトラヒドロイソキノリン |
| FR3010076B1 (fr) * | 2013-09-02 | 2016-12-23 | Centre Nat De La Rech Scient - Cnrs - | Inhibiteurs de metalloproteases, leurs procedes de preparation et leurs utilisations therapeutiques |
| ES2687498T3 (es) * | 2014-01-31 | 2018-10-25 | Bristol-Myers Squibb Company | Macrociclos con grupos P2¿ heterocíclicos como inhibidores del factor XIa |
| NO2760821T3 (OSRAM) * | 2014-01-31 | 2018-03-10 | ||
| ES2714283T3 (es) | 2014-09-04 | 2019-05-28 | Bristol Myers Squibb Co | Macrociclos de diamida que son inhibidores de FXIa |
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| NO2721243T3 (OSRAM) | 2014-10-01 | 2018-10-20 | ||
| US10160750B2 (en) * | 2015-06-19 | 2018-12-25 | Bristol-Myers Squibb Company | Diamide macrocycles as factor XIa inhibitors |
| JO3703B1 (ar) * | 2015-07-09 | 2021-01-31 | Bayer Pharma AG | مشتقات أوكسوبيريدين مستبدلة |
| CN107849026B (zh) * | 2015-07-29 | 2021-01-01 | 百时美施贵宝公司 | 携带烷基或环烷基p2′部分的因子xia大环抑制剂 |
| CN107922393A (zh) * | 2015-07-29 | 2018-04-17 | 百时美施贵宝公司 | 携带非芳族p2,基团的因子xia新大环 |
| US10336730B2 (en) | 2015-08-05 | 2019-07-02 | Bristol-Myers Squibb Company | Substituted glycine derived FXIA inhibitors |
| WO2017074833A1 (en) | 2015-10-29 | 2017-05-04 | Merck Sharp & Dohme Corp. | Macrocyclic spirocarbamate derivatives as factor xia inhibitors, pharmaceutically acceptable compositions and their use |
| CA2998902C (en) * | 2015-10-29 | 2024-03-26 | Merck Sharp & Dohme Corp. | Macrocyclic compounds as factor xia inhibitors |
| WO2017151746A1 (en) | 2016-03-02 | 2017-09-08 | Bristol-Myers Squibb Company | Diamide macrocycles having factor xia inhibiting activity |
| WO2018039094A1 (en) | 2016-08-22 | 2018-03-01 | Merck Sharp & Dohme Corp. | Pyridine-1-oxide derivatives and their use as factor xia inhibitors |
| CN110062757B (zh) * | 2017-01-18 | 2022-03-04 | 广东东阳光药业有限公司 | 凝血因子XIa抑制剂及其用途 |
| WO2019011166A1 (zh) * | 2017-07-14 | 2019-01-17 | 四川科伦博泰生物医药股份有限公司 | 大环酰胺化合物及其药物组合物和用途 |
| CN113677682B (zh) | 2019-04-16 | 2023-05-30 | 华润生物医药有限公司 | 作为XIa因子抑制剂的大环衍生物 |
| WO2021013209A1 (zh) | 2019-07-23 | 2021-01-28 | 南京明德新药研发有限公司 | 作为XIa因子抑制剂的大环衍生物 |
| CN113004286B (zh) * | 2019-12-20 | 2022-08-12 | 成都康弘药业集团股份有限公司 | 作为血浆激肽释放酶抑制剂的三环类化合物及其用途 |
| CN113004284B (zh) * | 2019-12-20 | 2022-08-12 | 成都康弘药业集团股份有限公司 | 作为血浆激肽释放酶抑制剂的四环类化合物及其用途 |
| US20230312560A1 (en) * | 2020-07-22 | 2023-10-05 | Janssen Pharmaceutica Nv | Compounds useful as factor xia inhibitors |
| WO2022164735A1 (en) | 2021-01-28 | 2022-08-04 | Merck Sharp & Dohme Llc | Factor xia inhibitors |
| WO2025002297A1 (zh) * | 2023-06-30 | 2025-01-02 | 深圳信立泰药业股份有限公司 | 一种多取代的大环化合物及其制备方法与应用 |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
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| EP0028489B1 (en) | 1979-11-05 | 1983-10-05 | Beecham Group Plc | Enzyme derivatives, and their preparation |
| PE121699A1 (es) | 1997-02-18 | 1999-12-08 | Boehringer Ingelheim Pharma | Heterociclos biciclicos disustituidos como inhibidores de la trombina |
| ZA985247B (en) | 1997-06-19 | 1999-12-17 | Du Pont Merck Pharma | Guanidine mimics as factor Xa inhibitors. |
| WO2000076970A2 (en) | 1999-06-14 | 2000-12-21 | Eli Lilly And Company | Serine protease inhibitors |
| DE19962924A1 (de) | 1999-12-24 | 2001-07-05 | Bayer Ag | Substituierte Oxazolidinone und ihre Verwendung |
| AR035216A1 (es) | 2000-12-01 | 2004-05-05 | Astrazeneca Ab | Derivados de acido mandelico ,derivados farmaceuticamente aceptables, uso de estos derivados para la fabricacion de medicamentos, metodos de tratamiento ,procesos para la preparacion de estos derivados, y compuestos intermediarios |
| GEP20074098B (en) | 2001-09-21 | 2007-05-10 | Bristol Myers Squibb Co | Lactam-containing compounds and derivatives thereof as factor xa inhibitors |
| US20040180855A1 (en) | 2003-02-19 | 2004-09-16 | Schumacher William A. | Methods of treating thrombosis with reduced risk of increased bleeding times |
| US7138412B2 (en) | 2003-03-11 | 2006-11-21 | Bristol-Myers Squibb Company | Tetrahydroquinoline derivatives useful as serine protease inhibitors |
| US7129264B2 (en) | 2003-04-16 | 2006-10-31 | Bristol-Myers Squibb Company | Biarylmethyl indolines and indoles as antithromboembolic agents |
| US7417063B2 (en) | 2004-04-13 | 2008-08-26 | Bristol-Myers Squibb Company | Bicyclic heterocycles useful as serine protease inhibitors |
| US7429604B2 (en) | 2004-06-15 | 2008-09-30 | Bristol Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| US7453002B2 (en) | 2004-06-15 | 2008-11-18 | Bristol-Myers Squibb Company | Five-membered heterocycles useful as serine protease inhibitors |
| CN101137412B (zh) | 2005-01-13 | 2012-11-07 | 布里斯托尔-迈尔斯·斯奎布公司 | 用作凝血因子XIa抑制剂的取代的二芳基化合物 |
| US20060183771A1 (en) | 2005-02-17 | 2006-08-17 | Seiffert Dietmar A | Novel combination of selective factor VIIa and/or factor XIa inhibitors and selective plasma kallikrein inhibitors |
| WO2007070816A2 (en) | 2005-12-14 | 2007-06-21 | Bristol-Myers Squibb Company | Thiophene derivatives as factor xia inhibitors |
| WO2007070826A1 (en) | 2005-12-14 | 2007-06-21 | Bristol-Myers Squibb Company | Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors |
| EP1966141A1 (en) | 2005-12-14 | 2008-09-10 | Brystol-Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| WO2008076805A2 (en) | 2006-12-15 | 2008-06-26 | Bristol-Myers Squibb Company | Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors |
| PE20081775A1 (es) * | 2006-12-20 | 2008-12-18 | Bristol Myers Squibb Co | Compuestos macrociclicos como inhibidores del factor viia |
| JP5318094B2 (ja) | 2007-06-13 | 2013-10-16 | ブリストル−マイヤーズ スクイブ カンパニー | 凝固因子阻害剤としてのジペプチド類似体 |
| CN102026996B (zh) | 2008-03-13 | 2015-01-07 | 百时美施贵宝公司 | 作为凝血因子xia抑制剂的哒嗪衍生物 |
| US8828983B2 (en) | 2010-02-11 | 2014-09-09 | Bristol-Myers Squibb Company | Macrocycles as factor XIa inhibitors |
| 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 |
| IN2014CN02806A (OSRAM) | 2011-10-14 | 2015-07-03 | Bristol Myers Squibb Co | |
| JP6033318B2 (ja) | 2011-10-14 | 2016-11-30 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | 第ＸＩａ因子阻害剤としての置換テトラヒドロイソキノリン化合物 |
| PL2766346T3 (pl) | 2011-10-14 | 2017-09-29 | Bristol-Myers Squibb Company | Podstawione związki tetrahydroizochinoliny jako inhibitory czynnika XIA |
| DK2794597T3 (en) | 2011-12-21 | 2018-01-15 | Ono Pharmaceutical Co | PYRIDINON AND PYRIMIDINON DERIVATIVES AS FACTOR XIA INHIBITORS |
| JP2015083542A (ja) | 2012-02-08 | 2015-04-30 | 大日本住友製薬株式会社 | ３位置換プロリン誘導体 |
| GB201209138D0 (en) | 2012-05-24 | 2012-07-04 | Ono Pharmaceutical Co | Compounds |
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- 2013-08-02 CN CN201810051705.4A patent/CN108250199B/zh active Active
- 2013-08-02 PT PT137476255T patent/PT2880026T/pt unknown
- 2013-08-02 AR ARP130102764A patent/AR091981A1/es unknown
- 2013-08-02 CA CA2880866A patent/CA2880866A1/en not_active Abandoned
- 2013-08-02 ES ES13747625.5T patent/ES2623175T3/es active Active
- 2013-08-02 AU AU2013296259A patent/AU2013296259A1/en not_active Abandoned
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- 2013-08-02 KR KR1020157004963A patent/KR20150038372A/ko not_active Withdrawn
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- 2013-08-02 EA EA201590277A patent/EA028581B1/ru not_active IP Right Cessation
- 2013-08-02 PL PL13747625T patent/PL2880026T3/pl unknown
- 2013-08-02 SM SM20170240T patent/SMT201700240T1/it unknown
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2015
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