CA2651303A1 - Factor xa inhibitors - Google Patents
Factor xa inhibitors Download PDFInfo
- Publication number
- CA2651303A1 CA2651303A1 CA002651303A CA2651303A CA2651303A1 CA 2651303 A1 CA2651303 A1 CA 2651303A1 CA 002651303 A CA002651303 A CA 002651303A CA 2651303 A CA2651303 A CA 2651303A CA 2651303 A1 CA2651303 A1 CA 2651303A1
- Authority
- CA
- Canada
- Prior art keywords
- mmol
- alkyl
- compound
- group
- methyl
- 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.)
- Abandoned
Links
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- 150000001875 compounds Chemical class 0.000 claims abstract description 224
- 150000003839 salts Chemical class 0.000 claims abstract description 55
- 238000000034 method Methods 0.000 claims abstract description 42
- 239000000651 prodrug Substances 0.000 claims abstract description 35
- 229940002612 prodrug Drugs 0.000 claims abstract description 35
- 150000002148 esters Chemical class 0.000 claims abstract description 34
- 208000007536 Thrombosis Diseases 0.000 claims abstract description 20
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- 238000005345 coagulation Methods 0.000 claims abstract description 5
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- 229910052739 hydrogen Inorganic materials 0.000 claims description 124
- -1 -NH-C(O)-C1-8 alkyl Chemical group 0.000 claims description 92
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- 125000001424 substituent group Chemical group 0.000 claims description 44
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims description 39
- 150000002431 hydrogen Chemical class 0.000 claims description 33
- 125000001072 heteroaryl group Chemical group 0.000 claims description 31
- 125000003545 alkoxy group Chemical group 0.000 claims description 27
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 26
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 25
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 24
- 125000000623 heterocyclic group Chemical group 0.000 claims description 21
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 19
- 125000004043 oxo group Chemical group O=* 0.000 claims description 18
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 17
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- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 22
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Classifications
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
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- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
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| US88366707P | 2007-01-05 | 2007-01-05 | |
| US60/883,667 | 2007-01-05 | ||
| PCT/US2007/068262 WO2007131179A1 (en) | 2006-05-05 | 2007-05-04 | Factor xa inhibitors |
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| BRPI0512273A (pt) | 2004-06-18 | 2008-02-19 | Millennium Pharm Inc | inibidores do fator xa |
| US7696352B2 (en) * | 2004-06-18 | 2010-04-13 | Millennium Pharmaceuticals, Inc. | Factor Xa inhibitors |
| PT1928454E (pt) | 2005-05-10 | 2014-12-04 | Intermune Inc | Derivativos da piridona para modulação do sistema de proteína quinase ativada pelo stress |
| US20080214495A1 (en) * | 2005-07-08 | 2008-09-04 | Astrazeneca Ab | Heterocyclic Sulfonamide Derivatives as Inhibitors of Factor Xa |
| US20080200431A1 (en) * | 2005-07-08 | 2008-08-21 | Astrazeneca Ab | Heterocyclic Sulfonamide Derivatives as Inhibitors of Factor Xa |
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| EP2016072B1 (en) | 2006-05-05 | 2014-07-16 | Millennium Pharmaceuticals, Inc. | Factor xa inhibitors |
| WO2008057972A1 (en) * | 2006-11-02 | 2008-05-15 | Millennium Pharmaceuticals, Inc. | Methods of synthesizing pharmaceutical salts of a factor xa inhibitor |
| US20080293704A1 (en) * | 2007-01-05 | 2008-11-27 | Millennium Pharmaceuticals, Inc. | FACTOR Xa INHIBITORS |
| WO2008127682A2 (en) | 2007-04-13 | 2008-10-23 | Millennium Pharmaceuticals, Inc. | Combination anticoagulant therapy with a compound that acts as a factor xa inhibitor |
| EA020045B1 (ru) * | 2007-05-02 | 2014-08-29 | Портола Фармасьютиклз, Инк. | Комбинированная терапия соединением, проявляющим активность ингибитора рецептора адф на тромбоцитах |
| WO2009063029A2 (en) * | 2007-11-16 | 2009-05-22 | Boehringer Ingelheim International Gmbh | Substituted amides, manufacturing and use thereof as medicaments |
| US8304413B2 (en) | 2008-06-03 | 2012-11-06 | Intermune, Inc. | Compounds and methods for treating inflammatory and fibrotic disorders |
| CN104774176A (zh) | 2009-12-17 | 2015-07-15 | 米伦纽姆医药公司 | 合成Xa因子抑制剂的方法 |
| JP5796872B2 (ja) * | 2009-12-17 | 2015-10-21 | ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． | 第Ｘａ因子阻害剤の結晶性塩 |
| WO2011075602A1 (en) | 2009-12-17 | 2011-06-23 | Millennium Pharmaceuticals, Inc. | Methods of preparing factor xa inhibitors and salts thereof |
| WO2011084653A1 (en) | 2009-12-17 | 2011-07-14 | Millennium Pharmaceuticals, Inc. | Crystalline forms of the mesylate salt of a factor xa inhibitor |
| TW201240664A (en) | 2010-09-01 | 2012-10-16 | Portola Pharm Inc | Methods and formulations of treating thrombosis with betrixaban and a P-glycoprotein inhibitor |
| AR082804A1 (es) | 2010-09-01 | 2013-01-09 | Portola Pharm Inc | Formas cristalinas de un inhibidor del factor xa |
| US20150224091A1 (en) | 2011-08-31 | 2015-08-13 | Portola Pharmaceuticals, Inc. | Prevention and treatment of thrombosis in medically ill patients |
| CN103242310A (zh) * | 2012-02-10 | 2013-08-14 | 苏州迈泰生物技术有限公司 | 吡唑并吡啶酮类化合物及其在制备抗凝血药物中的用途 |
| MX2015000830A (es) | 2012-07-18 | 2015-10-26 | Sunshine Lake Pharma Co Ltd | Derivados heterociclicos nitrogenosos y su aplicacion en farmacos. |
| AR092742A1 (es) | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
| CA2896057C (en) * | 2012-12-24 | 2023-03-14 | Maxine Bauzon | Short-acting factor vii polypeptides |
| TWI633089B (zh) | 2013-03-28 | 2018-08-21 | 拜耳製藥股份有限公司 | 經取代的酮基吡啶衍生物 |
| US9902712B2 (en) | 2013-12-19 | 2018-02-27 | Sunshine Lake Pharma Co., Ltd. | Nitrogenous heterocyclic derivatives and their application in drugs |
| KR102373700B1 (ko) | 2014-04-02 | 2022-03-11 | 인터뮨, 인크. | 항섬유성 피리디논 |
| CA2961981A1 (en) * | 2014-09-24 | 2016-03-31 | Bayer Pharma Aktiengesellschaft | Substituted oxopyridine derivatives |
| CA2979937A1 (en) * | 2015-03-19 | 2016-09-22 | Bayer Pharma Aktiengesellschaft | Oxo-pyridine-derivatives as factor xia inhibitors for the treatment of thrombosis |
| EP3078378B1 (en) | 2015-04-08 | 2020-06-24 | Vaiomer | Use of factor xa inhibitors for regulating glycemia |
| AR105322A1 (es) * | 2015-07-06 | 2017-09-27 | Bayer Cropscience Ag | Heterociclos nitrogenados como pesticidas |
| JO3703B1 (ar) | 2015-07-09 | 2021-01-31 | Bayer Pharma AG | مشتقات أوكسوبيريدين مستبدلة |
| US10148678B2 (en) | 2015-10-01 | 2018-12-04 | The Boeing Company | Cybersecurity system with differentiated capacity to deal with complex cyber attacks |
| SI3395801T1 (sl) * | 2015-12-16 | 2021-08-31 | Nippon Soda Co., Ltd. | Arilazolna spojina in sredstvo za zatiranje škodljivcev |
| CN105753804A (zh) * | 2016-04-15 | 2016-07-13 | 大连信科化工有限公司 | 一种制备3-吗啉酮的方法 |
| WO2019105871A1 (de) | 2017-11-29 | 2019-06-06 | Bayer Aktiengesellschaft | Stickstoffhaltige heterocyclen als schädlingsbekämpfungsmittel |
| WO2019215076A1 (de) * | 2018-05-08 | 2019-11-14 | Bayer Aktiengesellschaft | Verfahren zur herstellung stickstoffhaltiger heterocyclen |
| CN108715584B (zh) * | 2018-06-22 | 2021-06-25 | 四川大学华西医院 | 以n-吡啶-2-(1h)-腈亚氨为母核的荧光分子及其制备与应用 |
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-
2007
- 2007-05-04 EP EP07761905.4A patent/EP2016072B1/en active Active
- 2007-05-04 CN CN200780015911XA patent/CN101490036B/zh not_active Expired - Fee Related
- 2007-05-04 CA CA002651303A patent/CA2651303A1/en not_active Abandoned
- 2007-05-04 NZ NZ572418A patent/NZ572418A/en not_active IP Right Cessation
- 2007-05-04 AR ARP070101952A patent/AR060768A1/es unknown
- 2007-05-04 WO PCT/US2007/068262 patent/WO2007131179A1/en not_active Ceased
- 2007-05-04 TW TW096115906A patent/TW200813017A/zh unknown
- 2007-05-04 MX MX2008014193A patent/MX2008014193A/es active IP Right Grant
- 2007-05-04 JP JP2009510100A patent/JP5227311B2/ja not_active Expired - Fee Related
- 2007-05-04 AU AU2007247928A patent/AU2007247928B2/en not_active Ceased
- 2007-05-04 US US11/744,735 patent/US7763608B2/en not_active Expired - Fee Related
- 2007-05-04 BR BRPI0711296-3A patent/BRPI0711296A2/pt not_active Application Discontinuation
- 2007-05-04 EA EA200802288A patent/EA015942B1/ru not_active IP Right Cessation
- 2007-05-04 KR KR1020087029729A patent/KR20090010098A/ko not_active Ceased
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2008
- 2008-07-02 US US12/166,944 patent/US7767697B2/en not_active Expired - Fee Related
- 2008-10-23 IL IL194891A patent/IL194891A/en active IP Right Grant
- 2008-10-31 ZA ZA2008/09362A patent/ZA200809362B/en unknown
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2010
- 2010-05-11 US US12/777,956 patent/US8063077B2/en not_active Expired - Fee Related
- 2010-10-05 ZA ZA2010/07095A patent/ZA201007095B/en unknown
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- 2011-10-10 US US13/270,170 patent/US8349873B2/en not_active Expired - Fee Related
Also Published As
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| IL194891A (en) | 2014-06-30 |
| MX2008014193A (es) | 2009-03-31 |
| US8063077B2 (en) | 2011-11-22 |
| NZ572418A (en) | 2011-08-26 |
| EP2016072A1 (en) | 2009-01-21 |
| US7763608B2 (en) | 2010-07-27 |
| WO2007131179A1 (en) | 2007-11-15 |
| BRPI0711296A2 (pt) | 2011-08-23 |
| EA015942B1 (ru) | 2011-12-30 |
| US20100249117A1 (en) | 2010-09-30 |
| US7767697B2 (en) | 2010-08-03 |
| CN101490036B (zh) | 2013-07-17 |
| AU2007247928B2 (en) | 2013-06-13 |
| JP2009536218A (ja) | 2009-10-08 |
| US8349873B2 (en) | 2013-01-08 |
| EP2016072B1 (en) | 2014-07-16 |
| EA200802288A1 (ru) | 2009-04-28 |
| AU2007247928A1 (en) | 2007-11-15 |
| US20120088795A1 (en) | 2012-04-12 |
| US20090030045A1 (en) | 2009-01-29 |
| JP5227311B2 (ja) | 2013-07-03 |
| IL194891A0 (en) | 2009-08-03 |
| HK1126490A1 (en) | 2009-09-04 |
| CN101490036A (zh) | 2009-07-22 |
| ZA201007095B (en) | 2011-06-29 |
| AR060768A1 (es) | 2008-07-10 |
| US20070259924A1 (en) | 2007-11-08 |
| TW200813017A (en) | 2008-03-16 |
| ZA200809362B (en) | 2012-01-25 |
| US20110118244A2 (en) | 2011-05-19 |
| KR20090010098A (ko) | 2009-01-28 |
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| EEER | Examination request | ||
| FZDE | Discontinued |
Effective date: 20141104 |