JP2010514681A5 - - Google Patents
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- Publication number
- JP2010514681A5 JP2010514681A5 JP2009543158A JP2009543158A JP2010514681A5 JP 2010514681 A5 JP2010514681 A5 JP 2010514681A5 JP 2009543158 A JP2009543158 A JP 2009543158A JP 2009543158 A JP2009543158 A JP 2009543158A JP 2010514681 A5 JP2010514681 A5 JP 2010514681A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- phenyl
- ring
- heterocycle
- 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.)
- Withdrawn
Links
- 125000000217 alkyl group Chemical group 0.000 claims 50
- 125000000623 heterocyclic group Chemical group 0.000 claims 47
- 229910052739 hydrogen Inorganic materials 0.000 claims 46
- 229910052799 carbon Inorganic materials 0.000 claims 38
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 34
- 229910052760 oxygen Inorganic materials 0.000 claims 32
- 125000005842 heteroatom Chemical group 0.000 claims 28
- 229910052717 sulfur Inorganic materials 0.000 claims 25
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 20
- 125000004432 carbon atom Chemical group C* 0.000 claims 18
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims 16
- 125000003342 alkenyl group Chemical group 0.000 claims 16
- 125000000304 alkynyl group Chemical group 0.000 claims 16
- 150000001721 carbon Chemical group 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 12
- 208000035475 disorder Diseases 0.000 claims 12
- 230000009424 thromboembolic effect Effects 0.000 claims 12
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 11
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 11
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 10
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 10
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 8
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims 8
- 125000004076 pyridyl group Chemical group 0.000 claims 8
- -1 methoxy, ethoxy, cyclopropyl Chemical group 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 6
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 5
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 5
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 5
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 5
- 208000007536 Thrombosis Diseases 0.000 claims 4
- 206010047249 Venous thrombosis Diseases 0.000 claims 4
- 125000004429 atom Chemical group 0.000 claims 4
- 230000002526 effect on cardiovascular system Effects 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000003831 tetrazolyl group Chemical group 0.000 claims 4
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 3
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims 3
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 3
- 125000002837 carbocyclic group Chemical group 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims 3
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 3
- 229920002554 vinyl polymer Polymers 0.000 claims 3
- 125000000530 1-propynyl group Chemical group [H]C([H])([H])C#C* 0.000 claims 2
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 2
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 2
- 206010002388 Angina unstable Diseases 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 206010003658 Atrial Fibrillation Diseases 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- 206010008088 Cerebral artery embolism Diseases 0.000 claims 2
- 206010008092 Cerebral artery thrombosis Diseases 0.000 claims 2
- 206010011091 Coronary artery thrombosis Diseases 0.000 claims 2
- 206010051055 Deep vein thrombosis Diseases 0.000 claims 2
- 206010014513 Embolism arterial Diseases 0.000 claims 2
- 208000032382 Ischaemic stroke Diseases 0.000 claims 2
- 208000030831 Peripheral arterial occlusive disease Diseases 0.000 claims 2
- 208000010378 Pulmonary Embolism Diseases 0.000 claims 2
- 208000006011 Stroke Diseases 0.000 claims 2
- 208000007814 Unstable Angina Diseases 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 239000008280 blood Substances 0.000 claims 2
- 210000004369 blood Anatomy 0.000 claims 2
- 208000002528 coronary thrombosis Diseases 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 239000007943 implant Substances 0.000 claims 2
- 201000004332 intermediate coronary syndrome Diseases 0.000 claims 2
- 201000010849 intracranial embolism Diseases 0.000 claims 2
- 208000010125 myocardial infarction Diseases 0.000 claims 2
- 230000003836 peripheral circulation Effects 0.000 claims 2
- 230000000069 prophylactic effect Effects 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000006413 ring segment Chemical group 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 201000005060 thrombophlebitis Diseases 0.000 claims 2
- 230000001052 transient effect Effects 0.000 claims 2
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 claims 1
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- 125000004066 1-hydroxyethyl group Chemical group [H]OC([H])([*])C([H])([H])[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
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- 125000001960 7 membered carbocyclic group Chemical group 0.000 claims 1
- 208000005189 Embolism Diseases 0.000 claims 1
- 206010063544 Renal embolism Diseases 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 230000003796 beauty Effects 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([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
- 125000005045 dihydroisoquinolinyl group Chemical group C1(NC=CC2=CC=CC=C12)* 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000004672 ethylcarbonyl group Chemical group [H]C([H])([H])C([H])([H])C(*)=O 0.000 claims 1
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 1
- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 125000004458 methylaminocarbonyl group Chemical group [H]N(C(*)=O)C([H])([H])[H] 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 125000004287 oxazol-2-yl group Chemical group [H]C1=C([H])N=C(*)O1 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 230000003449 preventive effect Effects 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- AVBPTIYKXNVKNJ-UHFFFAOYSA-N Cc(cc1)cc(C=CN2)c1C2=O Chemical compound Cc(cc1)cc(C=CN2)c1C2=O AVBPTIYKXNVKNJ-UHFFFAOYSA-N 0.000 description 1
- APPHSAIPZPYEGB-UHFFFAOYSA-N Cc(cc1)cc(N=CN2)c1C2=O Chemical compound Cc(cc1)cc(N=CN2)c1C2=O APPHSAIPZPYEGB-UHFFFAOYSA-N 0.000 description 1
- MKVWWULERWAKBU-UHFFFAOYSA-N Cc1cc(C=CNC2=O)c2nc1 Chemical compound Cc1cc(C=CNC2=O)c2nc1 MKVWWULERWAKBU-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US87086406P | 2006-12-20 | 2006-12-20 | |
| US98446007P | 2007-11-01 | 2007-11-01 | |
| PCT/US2007/088032 WO2008079836A2 (en) | 2006-12-20 | 2007-12-19 | Macrocyclic factor viia inhibitors useful as anticoagulants |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010514681A JP2010514681A (ja) | 2010-05-06 |
| JP2010514681A5 true JP2010514681A5 (OSRAM) | 2010-09-16 |
Family
ID=39430763
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009543158A Withdrawn JP2010514681A (ja) | 2006-12-20 | 2007-12-19 | 抗凝血剤として有用な大環状第ｖｉｉａ因子阻害剤 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8420830B2 (OSRAM) |
| EP (1) | EP2102176A2 (OSRAM) |
| JP (1) | JP2010514681A (OSRAM) |
| AR (1) | AR064471A1 (OSRAM) |
| AU (1) | AU2007337025A1 (OSRAM) |
| CA (1) | CA2673598A1 (OSRAM) |
| CL (1) | CL2007003718A1 (OSRAM) |
| MX (1) | MX2009006689A (OSRAM) |
| NO (1) | NO20092279L (OSRAM) |
| PE (1) | PE20081775A1 (OSRAM) |
| TW (1) | TW200836735A (OSRAM) |
| WO (1) | WO2008079836A2 (OSRAM) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101631784A (zh) | 2006-12-20 | 2010-01-20 | 百时美施贵宝公司 | 用作抗凝血药的二环内酰胺凝血因子viia抑制剂 |
| PH12012501153A1 (en) * | 2009-12-08 | 2012-10-22 | Boehringer Ingelheim Int | Process for synthesis of intermediates useful for making substituted indazole and azaindazole compounds |
| PH12012501589A1 (en) * | 2010-02-11 | 2012-10-22 | Bristol Myers Squibb Co | Macrocycles as factor xia inhibitors |
| CN102993065B (zh) * | 2011-09-13 | 2015-07-29 | 中国科学院上海药物研究所 | 含手性叔丁基亚磺酰基的α-芳基氨基酸酯类化合物、其制备方法及用途 |
| HRP20170784T8 (hr) | 2011-10-14 | 2018-05-18 | Bristol-Myers Squibb Company | Supstituirani spojevi tetrahidroizohinolina kao inhbitori xia faktora |
| EP2797881B1 (en) * | 2011-12-27 | 2018-11-14 | Bio-Pharm Solutions Co., Ltd. | Phenyl alkyl carbamate derivative compound and pharmaceutical composition containing the same |
| EP2858977A1 (en) | 2012-06-08 | 2015-04-15 | Bristol-Myers Squibb Company | Macrocyclic factor viia inhibitors |
| CN104507924B (zh) * | 2012-08-03 | 2018-01-23 | 百时美施贵宝公司 | 二氢吡啶酮p1作为凝血因子xia抑制剂 |
| WO2014022766A1 (en) * | 2012-08-03 | 2014-02-06 | Bristol-Myers Squibb Company | Dihydropyridone p1 as factor xia inhibitors |
| HRP20180465T1 (hr) | 2012-10-12 | 2018-05-04 | Bristol-Myers Squibb Company | Kristalni oblici inhibitora faktora xia |
| 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 |
| 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 |
| US9657006B2 (en) | 2013-06-13 | 2017-05-23 | Bristol-Myers Squibb Company | Macrocyclic factor VIIa inhibitors |
| UY35971A (es) | 2014-01-31 | 2015-07-31 | Bristol Myers Squibb Company Una Corporación Del Estado De Delaware | Macrociclos con grupos p2? aromáticos como inhibidores del factor xia |
| NO2760821T3 (OSRAM) | 2014-01-31 | 2018-03-10 | ||
| 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 |
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| EP3072943B1 (en) | 2015-03-26 | 2018-05-02 | Idemitsu Kosan Co., Ltd. | Dibenzofuran/carbazole-substituted benzonitriles |
| 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 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3065190D1 (en) | 1979-11-05 | 1983-11-10 | Beecham Group Plc | Enzyme derivatives, and their preparation |
| US5023236A (en) | 1988-04-07 | 1991-06-11 | Corvas, Inc. | Factor VII/VIIA active site inhibitors |
| US5843442A (en) | 1990-10-22 | 1998-12-01 | Corvas International, Inc. | Blood coagulation protein antagonists and uses therefor |
| US5866542A (en) | 1994-10-18 | 1999-02-02 | Corvas International, Inc. | Nematode-extracted anticoagulant protein |
| 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 |
| HUP0400651A2 (hu) * | 2000-11-07 | 2004-06-28 | Bristol-Myers Squibb Company | Szerin proteáz inhibitorokként alkalmazható savszármazékok és ezeket tartalmazó gyógyszerkészítmények |
| 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 |
| WO2003011222A2 (en) | 2001-07-27 | 2003-02-13 | Merck & Co., Inc. | Thrombin inhibitors |
| SI1427415T1 (sl) | 2001-09-21 | 2009-12-31 | Bristol Myers Squibb Co | Sestavine, ki vsebujejo laktame in njihovi derivati kot inhibitorji faktorja xa |
| US7122559B2 (en) * | 2003-02-11 | 2006-10-17 | Bristol-Myers Squibb Company | Phenylglycine derivatives useful as serine protease inhibitors |
| WO2004072102A2 (en) * | 2003-02-11 | 2004-08-26 | Bristol-Myers Squibb Company | Benzene acetamide compounds useful as serine protease inhibitors |
| ATE479676T1 (de) * | 2005-01-10 | 2010-09-15 | Bristol Myers Squibb Co | Als antikoagulanzien verwendbare phenylglycinamid-derivate |
| JP2008538102A (ja) * | 2005-03-03 | 2008-10-09 | ザ バーナム インスティテュート フォー メディカル リサーチ | バーチャルドッキングアプローチを適用したプロテインキナーゼｂ阻害剤のスクリーニング方法並びにそれにより見出された化合物及び組成物 |
| DE602006011752D1 (de) * | 2005-06-24 | 2010-03-04 | Bristol Myers Squibb Co | Als antikoagulationsmittel geeignete phenylglycinamid- und pyridylglycinamidderivate |
| TW200745062A (en) * | 2005-12-23 | 2007-12-16 | Bristol Myers Squibb Co | Macrocyclic factor VIIA inhibitors useful as anticoagulants |
| US8044242B2 (en) | 2006-03-09 | 2011-10-25 | Bristol-Myers Squibb Company | 2-(aryloxy) acetamide factor VIIa inhibitors useful as anticoagulants |
| CN101631784A (zh) | 2006-12-20 | 2010-01-20 | 百时美施贵宝公司 | 用作抗凝血药的二环内酰胺凝血因子viia抑制剂 |
-
2007
- 2007-12-14 PE PE2007001814A patent/PE20081775A1/es not_active Application Discontinuation
- 2007-12-19 JP JP2009543158A patent/JP2010514681A/ja not_active Withdrawn
- 2007-12-19 WO PCT/US2007/088032 patent/WO2008079836A2/en not_active Ceased
- 2007-12-19 CL CL200703718A patent/CL2007003718A1/es unknown
- 2007-12-19 AU AU2007337025A patent/AU2007337025A1/en not_active Abandoned
- 2007-12-19 TW TW096148731A patent/TW200836735A/zh unknown
- 2007-12-19 CA CA002673598A patent/CA2673598A1/en not_active Abandoned
- 2007-12-19 EP EP07869479A patent/EP2102176A2/en not_active Withdrawn
- 2007-12-19 AR ARP070105750A patent/AR064471A1/es not_active Application Discontinuation
- 2007-12-19 MX MX2009006689A patent/MX2009006689A/es not_active Application Discontinuation
- 2007-12-19 US US12/519,376 patent/US8420830B2/en active Active
-
2009
- 2009-06-12 NO NO20092279A patent/NO20092279L/no not_active Application Discontinuation
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