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.)
- Granted
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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 (enExample) | 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)
| Country | Link |
|---|---|
| US (4) | US9221818B2 (enExample) |
| EP (1) | EP2739628B1 (enExample) |
| JP (1) | JP6158181B2 (enExample) |
| CN (1) | CN103857681B (enExample) |
| AR (1) | AR088748A1 (enExample) |
| BR (1) | BR112014002202A2 (enExample) |
| CA (1) | CA2844254A1 (enExample) |
| CY (1) | CY1119281T1 (enExample) |
| DK (1) | DK2739628T3 (enExample) |
| EA (1) | EA024791B1 (enExample) |
| ES (1) | ES2635088T3 (enExample) |
| HR (1) | HRP20171122T1 (enExample) |
| HU (1) | HUE034487T2 (enExample) |
| LT (1) | LT2739628T (enExample) |
| MX (1) | MX345763B (enExample) |
| PL (1) | PL2739628T3 (enExample) |
| PT (1) | PT2739628T (enExample) |
| RS (1) | RS56244B1 (enExample) |
| SI (1) | SI2739628T1 (enExample) |
| SM (1) | SMT201700413T1 (enExample) |
| TW (1) | TW201311689A (enExample) |
| WO (1) | WO2013022818A1 (enExample) |
Families Citing this family (49)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ602266A (en) | 2010-02-11 | 2014-05-30 | Bristol Myers Squibb Co | 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 |
| EP2766347B1 (en) | 2011-10-14 | 2016-05-04 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| JP6033319B2 (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 |
| WO2013055984A1 (en) | 2011-10-14 | 2013-04-18 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| AU2013296259A1 (en) * | 2012-08-03 | 2015-03-19 | Bristol-Myers Squibb Company | Dihydropyridone P1 as factor XIa inhibitors |
| US9376444B2 (en) | 2012-08-03 | 2016-06-28 | Bristol-Myers Squibb Company | Dihydropyridone P1 as factor XIa inhibitors |
| US9403774B2 (en) | 2012-10-12 | 2016-08-02 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| TR201807316T4 (tr) | 2012-10-12 | 2018-06-21 | Bristol Myers Squibb Co | Bir faktör XIa inhibitörünün kristalli formları. |
| EP2906552B1 (en) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| WO2014160668A1 (en) | 2013-03-25 | 2014-10-02 | Bristol-Myers Squibb Company | Tetrahydroisoquinolines containing substituted azoles as factor xia inhibitors |
| WO2014160592A2 (en) | 2013-03-27 | 2014-10-02 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| 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 |
| NO2760821T3 (enExample) | 2014-01-31 | 2018-03-10 | ||
| SG10201908467RA (en) * | 2014-01-31 | 2019-10-30 | Bristol Myers Squibb Co | Macrocycles with hetrocyclic p2' groups as factor xia inhibitors |
| WO2015123093A1 (en) | 2014-02-11 | 2015-08-20 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| WO2015123091A1 (en) | 2014-02-11 | 2015-08-20 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| EP3134408B1 (en) | 2014-04-22 | 2020-08-12 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| WO2016015593A1 (en) | 2014-07-28 | 2016-02-04 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| ES2714283T3 (es) | 2014-09-04 | 2019-05-28 | Bristol Myers Squibb Co | Macrociclos de diamida que son inhibidores de FXIa |
| NO2721243T3 (enExample) * | 2014-10-01 | 2018-10-20 | ||
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| ES2762987T3 (es) * | 2015-06-19 | 2020-05-26 | Bristol Myers Squibb Co | Macrociclos de diamida como inhibidores del factor XIA |
| JP6629958B2 (ja) | 2015-07-29 | 2020-01-15 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | アルキルまたはシクロアルキルＰ２’基を担持する大員環の第ＸＩａ因子阻害剤 |
| CN114874222B (zh) | 2015-07-29 | 2025-06-06 | 百时美施贵宝公司 | 携带非芳族p2,基团的因子xia新大环 |
| DK4019022T3 (en) | 2015-10-01 | 2024-02-19 | Biocryst Pharm Inc | Human plasma kallikrein inhibitors |
| EP3371162B1 (en) | 2015-10-29 | 2022-01-26 | Merck Sharp & Dohme Corp. | Macrocyclic spirocarbamate derivatives as factor xia inhibitors, pharmaceutically acceptable compositions and their use |
| EP3368036B1 (en) | 2015-10-29 | 2022-07-20 | Merck Sharp & Dohme LLC | Macrocyclic pyridine-n-oxide derivatives as factor xia inhibitors |
| KR20180117156A (ko) | 2016-03-02 | 2018-10-26 | 브리스톨-마이어스 스큅 컴퍼니 | 인자 XIa 억제 활성을 갖는 디아미드 마크로사이클 |
| EP3455211A1 (en) * | 2016-05-10 | 2019-03-20 | Solvay SA | Composition comprising 3-(haloalkyl or formyl)-1h-pyrazole-4-carboxylic acids or esters, its manufacture and its use for the preparation of carboxamides |
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| EP3309143A1 (en) * | 2016-10-17 | 2018-04-18 | Solvay SA | Method for producing fluoroformate compounds |
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| CN107011275A (zh) * | 2017-03-31 | 2017-08-04 | 深圳市众康动保科技有限公司 | 一种1,4,5‑三取代‑1,2,3‑三氮唑类化合物的合成方法 |
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| CN114008047B (zh) | 2019-07-23 | 2023-03-21 | 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 |
| TW202132316A (zh) | 2019-11-04 | 2021-09-01 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| IL322454A (en) | 2019-11-04 | 2025-09-01 | Revolution Medicines Inc | ras inhibitors |
| EP4146205A4 (en) | 2020-05-05 | 2024-05-29 | Nuvalent, Inc. | HETEROAROMATIC MACROCYCLIC ETHERS AS CHEMOTHERAPEUTIC AGENTS |
| IL297832A (en) | 2020-05-05 | 2023-01-01 | Nuvalent Inc | Macrocyclic heteroaromatic chemotherapeutic agents |
| CA3194067A1 (en) | 2020-09-15 | 2022-03-24 | Revolution Medicines, Inc. | Ras inhibitors |
| CN112920005B (zh) * | 2021-01-31 | 2022-06-14 | 上海李氏化学科技有限公司 | 一种(r)-3-(3-氯-2-氟苯)-4,5-二氢异噁唑-5-羧酸的制备方法 |
| KR20240017811A (ko) | 2021-05-05 | 2024-02-08 | 레볼루션 메디슨즈, 인크. | 암의 치료를 위한 ras 억제제 |
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