JP2017504642A5 - - Google Patents
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- JP2017504642A5 JP2017504642A5 JP2016549279A JP2016549279A JP2017504642A5 JP 2017504642 A5 JP2017504642 A5 JP 2017504642A5 JP 2016549279 A JP2016549279 A JP 2016549279A JP 2016549279 A JP2016549279 A JP 2016549279A JP 2017504642 A5 JP2017504642 A5 JP 2017504642A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- independently selected
- substituted
- cycloalkyl
- heterocyclyl
- 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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- 125000000217 alkyl group Chemical group 0.000 claims 190
- 125000000623 heterocyclic group Chemical group 0.000 claims 122
- 229910052739 hydrogen Inorganic materials 0.000 claims 75
- 229910052799 carbon Inorganic materials 0.000 claims 53
- 229910052731 fluorine Inorganic materials 0.000 claims 51
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 claims 48
- 229910052736 halogen Inorganic materials 0.000 claims 43
- 150000002367 halogens Chemical class 0.000 claims 43
- 125000003118 aryl group Chemical group 0.000 claims 37
- 229910052801 chlorine Inorganic materials 0.000 claims 33
- 125000004452 carbocyclyl group Chemical group 0.000 claims 31
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 30
- 229910052760 oxygen Inorganic materials 0.000 claims 26
- 229910052757 nitrogen Inorganic materials 0.000 claims 21
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 21
- 125000003545 alkoxy group Chemical group 0.000 claims 19
- 125000000753 cycloalkyl group Chemical group 0.000 claims 19
- 125000001188 haloalkyl group Chemical group 0.000 claims 19
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 19
- 229910052794 bromium Inorganic materials 0.000 claims 17
- -1 —S (═O) 2 NH 2 Chemical group 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 13
- 150000001875 compounds Chemical class 0.000 claims 10
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 9
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 8
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 7
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 7
- 125000004432 carbon atom Chemical group C* 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 208000035475 disorder Diseases 0.000 claims 7
- 230000009424 thromboembolic effect Effects 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 125000005842 heteroatom Chemical group 0.000 claims 5
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 4
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 4
- 229910052805 deuterium Inorganic materials 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000004438 haloalkoxy group Chemical group 0.000 claims 3
- 125000006809 haloalkylaminocarbonyl group Chemical group 0.000 claims 3
- 229910052740 iodine Inorganic materials 0.000 claims 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 2
- 101100516554 Caenorhabditis elegans nhr-5 gene Proteins 0.000 claims 2
- 208000007536 Thrombosis Diseases 0.000 claims 2
- 206010047249 Venous thrombosis Diseases 0.000 claims 2
- 125000004450 alkenylene group Chemical group 0.000 claims 2
- 125000005099 aryl alkyl carbonyl group Chemical group 0.000 claims 2
- 125000001769 aryl amino group Chemical group 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 230000002526 effect on cardiovascular system Effects 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000005221 halo alkyl carbonyl amino group Chemical group 0.000 claims 2
- 125000005241 heteroarylamino group Chemical group 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 230000000069 prophylactic effect Effects 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 1
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 claims 1
- 125000006706 (C3-C6) carbocyclyl group Chemical group 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
- 206010014513 Embolism arterial Diseases 0.000 claims 1
- 208000032382 Ischaemic stroke Diseases 0.000 claims 1
- 208000010378 Pulmonary Embolism Diseases 0.000 claims 1
- 206010063544 Renal embolism Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000007814 Unstable Angina Diseases 0.000 claims 1
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 125000004103 aminoalkyl group Chemical group 0.000 claims 1
- 125000005125 aryl alkyl amino carbonyl group Chemical group 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 1
- 125000004104 aryloxy 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
- 210000005242 cardiac chamber Anatomy 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 208000002528 coronary thrombosis Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 1
- 125000005143 heteroarylsulfonyl group Chemical group 0.000 claims 1
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 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
- 238000004519 manufacturing process Methods 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 230000000414 obstructive effect Effects 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
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 229940124530 sulfonamide Drugs 0.000 claims 1
- 150000003456 sulfonamides Chemical class 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 201000005060 thrombophlebitis Diseases 0.000 claims 1
- 230000001052 transient effect Effects 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461933942P | 2014-01-31 | 2014-01-31 | |
| US61/933,942 | 2014-01-31 | ||
| US201462058293P | 2014-10-01 | 2014-10-01 | |
| US62/058,293 | 2014-10-01 | ||
| PCT/US2015/013654 WO2015116886A1 (en) | 2014-01-31 | 2015-01-30 | Macrocycles with hetrocyclic p2' groups as factor xia inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019060181A Division JP6854067B2 (ja) | 2014-01-31 | 2019-03-27 | ヘテロ環式ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017504642A JP2017504642A (ja) | 2017-02-09 |
| JP2017504642A5 true JP2017504642A5 (cg-RX-API-DMAC10.html) | 2018-06-07 |
| JP6505727B2 JP6505727B2 (ja) | 2019-04-24 |
Family
ID=52484570
Family Applications (7)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016549277A Active JP6464176B2 (ja) | 2014-01-31 | 2015-01-30 | 芳香族ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環 |
| JP2016549279A Active JP6505727B2 (ja) | 2014-01-31 | 2015-01-30 | ヘテロ環式ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環 |
| JP2019000516A Active JP6630004B2 (ja) | 2014-01-31 | 2019-01-07 | 芳香族ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環 |
| JP2019060181A Active JP6854067B2 (ja) | 2014-01-31 | 2019-03-27 | ヘテロ環式ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環 |
| JP2021039989A Active JP7325464B2 (ja) | 2014-01-31 | 2021-03-12 | ヘテロ環式ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環 |
| JP2023125512A Pending JP2023133468A (ja) | 2014-01-31 | 2023-08-01 | ヘテロ環式ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環 |
| JP2025166031A Pending JP2025185049A (ja) | 2014-01-31 | 2025-10-02 | ヘテロ環式ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016549277A Active JP6464176B2 (ja) | 2014-01-31 | 2015-01-30 | 芳香族ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環 |
Family Applications After (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019000516A Active JP6630004B2 (ja) | 2014-01-31 | 2019-01-07 | 芳香族ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環 |
| JP2019060181A Active JP6854067B2 (ja) | 2014-01-31 | 2019-03-27 | ヘテロ環式ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環 |
| JP2021039989A Active JP7325464B2 (ja) | 2014-01-31 | 2021-03-12 | ヘテロ環式ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環 |
| JP2023125512A Pending JP2023133468A (ja) | 2014-01-31 | 2023-08-01 | ヘテロ環式ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環 |
| JP2025166031A Pending JP2025185049A (ja) | 2014-01-31 | 2025-10-02 | ヘテロ環式ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環 |
Country Status (32)
Families Citing this family (48)
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| ES2893251T3 (es) | 2014-01-31 | 2022-02-08 | Bristol Myers Squibb Co | Macrociclos con grupos P2 heterocíclicos como inhibidores del factor XIa |
| NO2760821T3 (cg-RX-API-DMAC10.html) | 2014-01-31 | 2018-03-10 | ||
| EP2913330A1 (en) * | 2014-02-27 | 2015-09-02 | Laboratoire Biodim | Condensed derivatives of imidazole useful as pharmaceuticals |
| CN107074821B (zh) | 2014-09-04 | 2020-05-22 | 百时美施贵宝公司 | 为fxia抑制剂的二酰胺大环化合物 |
| NO2721243T3 (cg-RX-API-DMAC10.html) * | 2014-10-01 | 2018-10-20 | ||
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| WO2016050358A1 (en) | 2014-10-01 | 2016-04-07 | Merck Patent Gmbh | Boronic acid derivatives |
| JOP20160086B1 (ar) | 2015-05-08 | 2021-08-17 | 2 Katholieke Univ Leuven Ku Leuven Research And Development | مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
| WO2016205482A1 (en) | 2015-06-19 | 2016-12-22 | Bristol-Myers Squibb Company | Diamide macrocycles as factor xia inhibitors |
| JO3703B1 (ar) | 2015-07-09 | 2021-01-31 | Bayer Pharma AG | مشتقات أوكسوبيريدين مستبدلة |
| WO2017019821A1 (en) | 2015-07-29 | 2017-02-02 | Bristol-Myers Squibb Company | Factor xia new macrocycle bearing a non-aromatic p2' group |
| EP3328851B1 (en) | 2015-07-29 | 2020-04-22 | Bristol-Myers Squibb Company | Factor xia macrocyclic inhibitors bearing alkyl or cycloalkyl p2' moieties |
| JO3633B1 (ar) | 2015-09-16 | 2020-08-27 | Katholieke Univ Leuven Ku Leuven Research & Development | مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
| JOP20160198B1 (ar) | 2015-09-16 | 2022-03-14 | Janssen Pharmaceuticals Inc | مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
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| EP3423458A1 (en) | 2016-03-02 | 2019-01-09 | Bristol-Myers Squibb Company | Diamide macrocycles having factor xia inhibiting activity |
| DK3436435T3 (da) | 2016-03-31 | 2021-08-09 | Janssen Pharmaceuticals Inc | Substituerede indolderivater som inhibitorer af replikation af denguevirus |
| SG11201808270PA (en) | 2016-03-31 | 2018-10-30 | Janssen Pharmaceuticals Inc | Substituted indoline derivatives as dengue viral replication inhibitors |
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| MX2018011786A (es) | 2016-04-01 | 2019-05-20 | Janssen Pharmaceuticals Inc | Derivados de compuestos de indol sustituidos como inhibidores de la replicacion virica del dengue. |
| AR109304A1 (es) | 2016-08-10 | 2018-11-21 | Sumitomo Chemical Co | Compuesto de oxadiazol y su uso |
| US10143681B2 (en) | 2016-08-22 | 2018-12-04 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| WO2018133793A1 (zh) * | 2017-01-18 | 2018-07-26 | 广东东阳光药业有限公司 | 凝血因子XIa抑制剂及其用途 |
| JOP20180026A1 (ar) | 2017-03-31 | 2019-01-30 | Univ Leuven Kath | مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
| JOP20180025B1 (ar) | 2017-03-31 | 2021-08-17 | Janssen Pharmaceuticals Inc | مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
| WO2018215316A1 (en) | 2017-05-22 | 2018-11-29 | Janssen Pharmaceuticals, Inc. | Substituted indoline derivatives as dengue viral replication inhibitors |
| WO2018215315A1 (en) | 2017-05-22 | 2018-11-29 | Janssen Pharmaceuticals, Inc. | Substituted indoline derivatives as dengue viral replication inhibitors |
| 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 |
| US12378246B2 (en) | 2019-04-11 | 2025-08-05 | Bristol-Myers Squibb Company | Synthetic options towards the manufacture of (6R,10S)-10-{4-[5-chloro-2-(4-chloro-1H-1,2,3-triazol-1-yl)phenyl]-6-oxo-1(6H)-pyrimidinyl} - 1-(difluoromethyl)-6-methyl-1,4,7,8,9,10-hexahydro-11,15-(metheno)pyrazolo[4,3-b][1,7]diazacyclotetradecin-5(6H)-one |
| WO2020210629A1 (en) * | 2019-04-11 | 2020-10-15 | Bristol-Myers Squibb Company | Enhanced performance of amorphous solid and solubilized formulations for achieving therapeutic plasma concentrations |
| US12018027B2 (en) | 2019-04-16 | 2024-06-25 | China Resources Biopharmaceutical Company Limited | Macrocyclic derivatives acting as XIa factor inhibitor |
| 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 |
| TWI749881B (zh) * | 2019-11-21 | 2021-12-11 | 大陸商深圳信立泰藥業股份有限公司 | 二氧代哌類衍生物、其製備方法及其在醫藥上的應用 |
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| TW202229280A (zh) * | 2020-10-12 | 2022-08-01 | 美商必治妥美雅史谷比公司 | （６ｒ，１０ｓ）－１０－｛４－［５－氯－２－（４－氯－１ｈ－１，２，３－三唑－１－基）苯基］－６－側氧基－１（６ｈ）－嘧啶基｝－１－（二氟甲基）－６－甲基－１，４，７，８，９，１０－六氫－１１，１５－（亞甲橋基）吡唑并［４，３－ｂ］［１，７］二氮雜環十四炔－５（６ｈ）－酮之製備方法 |
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