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HK1061973A1 - Lactam-containing compounds and derivatives thereof as factor xa inhibitors - Google Patents

Lactam-containing compounds and derivatives thereof as factor xa inhibitors Download PDF

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Publication number
HK1061973A1
HK1061973A1 HK04105041.4A HK04105041A HK1061973A1 HK 1061973 A1 HK1061973 A1 HK 1061973A1 HK 04105041 A HK04105041 A HK 04105041A HK 1061973 A1 HK1061973 A1 HK 1061973A1
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HK
Hong Kong
Prior art keywords
compound
mmol
phenyl
substituted
treating
Prior art date
Application number
HK04105041.4A
Other languages
German (de)
English (en)
Chinese (zh)
Other versions
HK1061973B (en
Inventor
Wei Han
Michael J. Orwat
Donald Pinto
Mimi Quan
Yun-Long Li
X. Qiao Jennifer
Patrick Lam
Stephanie Koch
Original Assignee
Bristol-Myers Squibb Holdings Ireland Unlimited Company
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Publication date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=23262376&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HK1061973(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bristol-Myers Squibb Holdings Ireland Unlimited Company filed Critical Bristol-Myers Squibb Holdings Ireland Unlimited Company
Publication of HK1061973A1 publication Critical patent/HK1061973A1/en
Publication of HK1061973B publication Critical patent/HK1061973B/en

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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyrrole Compounds (AREA)

Claims (29)

  1. Composé qui est représenté par la formule (1): ou sel pharmaceutiquement acceptable de celui-ci.
  2. Composé selon la revendication 1, qui est représenté par la formule (1).
  3. Composition pharmaceutique, comprenant: un support pharmaceutiquement acceptable et une quantité thérapeutiquement efficace du composé de la formule (1) selon la revendication 1 ou d'un sel pharmaceutiquement acceptable de celui-ci.
  4. Composition pharmaceutique, comprenant: le support pharmaceutiquement acceptable et une quantité thérapeutiquement efficace du composé selon la revendication 2.
  5. Composé selon la revendication 1 ou 2 pour une utilisation dans une thérapie.
  6. Composition pharmaceutique selon la revendication 3 ou 4 pour une utilisation dans une thérapie.
  7. Composé selon la revendication 1 ou 2 pour une utilisation dans le traitement d'un trouble thromboembolique.
  8. Composition pharmaceutique selon la revendication 3 ou 4 pour une utilisation dans le traitement d'un trouble thromboembolique.
  9. Utilisation d'un composé selon la revendication 1 ou 2 dans la fabrication d'un médicament pour une utilisation dans le traitement d'un trouble thromboembolique.
  10. Utilisation d'une composition pharmaceutique selon la revendication 3 ou 4 dans la fabrication d'un médicament pour une utilisation dans le traitement d'un trouble thromboembolique.
  11. Composé pour une utilisation dans le traitement d'un trouble thromboembolique selon la revendication 7 ou utilisation d'un composé selon la revendication 9, où le trouble thromboembolique est choisi dans le groupe constitué de troubles thromboemboliques cardiovasculaires artériels, de troubles thromboemboliques cardiovasculaires veineux et de troubles thromboemboliques dans les cavités du coeur.
  12. Composé pour une utilisation dans le traitement d'un trouble thromboembolique selon la revendication 7 ou utilisation d'un composé selon la revendication 9, où le trouble thromboembolique est choisi parmi un angor instable, un syndrome coronaire aigu, un premier infarctus du myocarde, un infarctus du myocarde récurrent, une mort subite ischémique, un accident ischémique transitoire, une attaque, une athérosclérose, une maladie artérielle occlusive périphérique, une thrombose veineuse, une thrombose veineuse profonde, une thrombophlébite, une embolie artérielle, une thrombose artérielle coronaire, une thrombose artérielle cérébrale, une embolie cérébrale, une embolie rénale, une embolie pulmonaire et une thrombose résultant (a) de valves prothétiques ou d'autres implants, (b) de cathéters à demeure, (c) de tuteurs, (d) d'un pontage cardio-pulmonaire, (e) d'une hémodialyse ou (f) d'autres procédures dans lesquelles le sang est exposé à une surface artificielle qui favorise une thrombose.
  13. Composé pour une utilisation dans le traitement d'un trouble thromboembolique selon la revendication 12 ou utilisation d'un composé selon la revendication 12, où le trouble thromboembolique est un syndrome coronaire aigu.
  14. Composé pour une utilisation dans le traitement d'un trouble thromboembolique selon la revendication 12 ou utilisation d'un composé selon la revendication 12, où le trouble thromboembolique est une mort subite ischémique, un accident ischémique transitoire ou une attaque.
  15. Composé pour une utilisation dans le traitement d'un trouble thromboembolique selon la revendication 12 ou utilisation d'un composé selon la revendication 12, où le trouble thromboembolique est une thrombose veineuse profonde.
  16. Composé pour une utilisation dans le traitement d'un trouble thromboembolique selon la revendication 12 ou utilisation d'un composé selon la revendication 12, où le trouble thromboembolique est une embolie pulmonaire.
  17. Composition pharmaceutique pour une utilisation dans le traitement d'un trouble thromboembolique selon la revendication 8 ou utilisation d'une composition pharmaceutique selon la revendication 10, où le trouble thromboembolique est choisi dans le groupe constitué de troubles thromboemboliques cardiovasculaires artériels, de troubles thromboemboliques cardiovasculaires veineux et de troubles thromboemboliques dans les cavités du coeur.
  18. Composition pharmaceutique pour une utilisation dans le traitement d'un trouble thromboembolique selon la revendication 8 ou utilisation d'une composition pharmaceutique selon la revendication 10, où le trouble thromboembolique est choisi parmi un angor instable, un syndrome coronaire aigu, un premier infarctus du myocarde, un infarctus du myocarde récurrent, une mort subite ischémique, un accident ischémique transitoire, une attaque, une athérosclérose, une maladie artérielle occlusive périphérique, une thrombose veineuse, une thrombose veineuse profonde, une thrombophlébite, une embolie artérielle, une thrombose artérielle coronaire, une thrombose artérielle cérébrale, une embolie cérébrale, une embolie rénale, une embolie pulmonaire et une thrombose résultant (a) de valves prothétiques ou d'autres implants, (b) de cathéters à demeure, (c) de tuteurs, (d) d'un pontage cardio-pulmonaire, (e) d'une hémodialyse ou (f) d'autres procédures dans lesquelles le sang est exposé à une surface artificielle qui favorise une thrombose.
  19. Composition pharmaceutique pour une utilisation dans le traitement d'un trouble thromboembolique selon la revendication 18 ou utilisation d'une composition pharmaceutique selon la revendication 18, où le trouble thromboembolique est un syndrome coronaire aigu.
  20. Composition pharmaceutique pour une utilisation dans le traitement d'un trouble thromboembolique selon la revendication 18 ou utilisation d'une composition pharmaceutique selon la revendication 18, où le trouble thromboembolique est une mort subite ischémique, un accident ischémique transitoire ou une attaque.
  21. Composition pharmaceutique pour une utilisation dans le traitement d'un trouble thromboembolique selon la revendication 18 ou utilisation d'une composition pharmaceutique selon la revendication 18, où le trouble thromboembolique est une thrombose veineuse profonde.
  22. Composition pharmaceutique pour une utilisation dans le traitement d'un trouble thromboembolique selon la revendication 18 ou utilisation d'une composition pharmaceutique selon la revendication 18, où le trouble thromboembolique est une embolie pulmonaire.
  23. Un composé et un deuxième agent thérapeutique, pour une utilisation dans le traitement d'un trouble thrombolytique, où le composé est un composé selon la revendication 2 et le deuxième agent thérapeutique est au moins un agent choisi parmi un deuxième inhibiteur du facteur Xa, un agent anti-coagulant, un agent anti-plaquettaire, un agent d'inhibition de la thrombine, un agent thrombolytique et un agent fibrinolytique.
  24. Utilisation d'un composé et d'un deuxième agent thérapeutique dans la fabrication d'un médicament pour une utilisation dans le traitement d'un trouble thrombolytique, où le composé est un composé selon la revendication 2 et le deuxième agent thérapeutique est au moins un agent choisi parmi un deuxième inhibiteur du facteur Xa, un agent anti-coagulant, un agent anti-plaquettaire, un agent d'inhibition de la thrombine, un agent thrombolytique et un agent fibrinolytique.
  25. Un composé et un deuxième agent thérapeutique, pour une utilisation dans le traitement d'un trouble thrombolytique selon la revendication 23 ou utilisation d'un composé et d'un deuxième agent thérapeutique selon la revendication 24, où le deuxième agent thérapeutique est au moins un agent choisi parmi la warfarine, une héparine non fractionnée, une héparine à bas poids moléculaire, un pentasaccharide synthétique, l'hirudine, l'argatroban, l'aspirine, l'ibuprofène, le naproxène, le sulindac, l'indométhacine, le méfénamate, le droxicam, le diclofénac, la sulfinpyrazone, le piroxicam, la ticlopidine, le clopidogrel, le tirofiban, l'eptifibatide, l'abciximab, le mélagatran, la disulfatohirudine, l'activateur tissulaire du plasminogène, un activateur tissulaire du plasminogène modifié, l'anistréplase, l'urokinase et la streptokinase.
  26. Un composé et un deuxième agent thérapeutique, pour une utilisation dans le traitement d'un trouble thrombolytique selon la revendication 23 ou utilisation d'un composé et d'un deuxième agent thérapeutique selon la revendication 24, où le deuxième agent thérapeutique est au moins un agent anti-plaquettaire.
  27. Un composé et un deuxième agent thérapeutique, pour une utilisation dans le traitement d'un trouble thrombolytique selon la revendication 26 ou utilisation d'un composé et d'un deuxième agent thérapeutique selon la revendication 26, où le deuxième agent thérapeutique est au moins un parmi l'aspirine et le clopidogrel.
  28. Un composé et un deuxième agent thérapeutique, pour une utilisation dans le traitement d'un trouble thrombolytique selon la revendication 27 ou utilisation d'un composé et d'un deuxième agent thérapeutique selon la revendication 27, où l'agent anti-plaquettaire est le clopidogrel.
  29. Un composé et un deuxième agent thérapeutique, pour une utilisation dans le traitement d'un trouble thrombolytique selon la revendication 27 ou utilisation d'un composé et d'un deuxième agent thérapeutique selon la revendication 27, où l'agent anti-plaquettaire est l'aspirine.
HK04105041.4A 2001-09-21 2002-09-17 Lactam-containing compounds and derivatives thereof as factor xa inhibitors HK1061973B (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US32416501P 2001-09-21 2001-09-21
US324165 2001-09-21
PCT/US2002/029491 WO2003026652A1 (fr) 2001-09-21 2002-09-17 Composes contenant du lactame et leurs derives en tant qu'inhibiteurs du facteur xa

Publications (2)

Publication Number Publication Date
HK1061973A1 true HK1061973A1 (en) 2004-10-15
HK1061973B HK1061973B (en) 2010-02-05

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LTPA2011012I1 (lt) 2012-07-25
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HU228195B1 (hu) 2013-01-28
EP2105436A1 (fr) 2009-09-30
IL203533A (en) 2011-12-29
ATE544750T1 (de) 2012-02-15
US7691846B2 (en) 2010-04-06
ES2329881T3 (es) 2009-12-02
CY2011016I1 (el) 2017-11-14
AU2002341693B2 (en) 2008-05-29
RU2345993C2 (ru) 2009-02-10
RU2004112191A (ru) 2005-10-10
KR100909141B1 (ko) 2009-07-23
US20200140436A1 (en) 2020-05-07
CN104744461A (zh) 2015-07-01
FR11C0042I1 (fr) 2011-04-11
CA2461202A1 (fr) 2003-04-03
MEP58108A (bs) 2011-05-10
LU91888I2 (fr) 2011-12-19
ME00090B (fr) 2010-10-10
HUS1300014I1 (hu) 2017-10-30
AR037092A1 (es) 2004-10-20
CN102617567A (zh) 2012-08-01
MY137830A (en) 2009-03-31
PT1427415E (pt) 2009-10-29
AR067965A2 (es) 2009-10-28
CN1578660A (zh) 2005-02-09
AU2008207537B8 (en) 2011-12-08
CN110894196A (zh) 2020-03-20
JP4249621B2 (ja) 2009-04-02
CO5560567A2 (es) 2005-09-30
JP4889705B2 (ja) 2012-03-07
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US9975891B2 (en) 2018-05-22
PL204263B1 (pl) 2009-12-31
CY1110509T1 (el) 2015-04-29
US20100119510A1 (en) 2010-05-13
LU91888I9 (fr) 2019-01-03
CN1578660B (zh) 2010-11-24
SI1427415T1 (sl) 2009-12-31
PL204653B1 (pl) 2010-01-29
KR20080075927A (ko) 2008-08-19
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US20140113892A1 (en) 2014-04-24
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US20170050964A1 (en) 2017-02-23
FR11C0042I2 (fr) 2013-01-11
EP1427415A4 (fr) 2005-11-02
US8188120B2 (en) 2012-05-29
US20080090807A1 (en) 2008-04-17
US7531535B2 (en) 2009-05-12
US20120201816A1 (en) 2012-08-09
HUP0402463A3 (en) 2011-07-28
HRP20040280A2 (hr) 2007-09-30
US7960411B2 (en) 2011-06-14
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US20090176758A1 (en) 2009-07-09
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JP2005507889A (ja) 2005-03-24
BRPI0212726B8 (pt) 2021-05-25
KR20040041167A (ko) 2004-05-14
AU2008207537A1 (en) 2008-09-18
BE2011C034I2 (fr) 2021-11-22
CH1427415H1 (de) 2023-12-21
IL160693A0 (en) 2004-08-31
HRP20040280B1 (hr) 2013-09-30
WO2003026652A1 (fr) 2003-04-03
PL373299A1 (pl) 2005-08-22
US20180244673A1 (en) 2018-08-30
LTC1427415I2 (lt) 2023-10-10
US7338963B2 (en) 2008-03-04
NO328558B1 (no) 2010-03-22
IS7184A (is) 2004-03-16
CL2008002717A1 (es) 2009-01-09
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NO2011021I2 (no) 2012-06-25
CY2011016I2 (el) 2017-11-14
US20150210691A1 (en) 2015-07-30
EP1427415A1 (fr) 2004-06-16
US8470854B2 (en) 2013-06-25
CN101357914A (zh) 2009-02-04
BR0212726A (pt) 2004-08-03
IL160693A (en) 2011-06-30
HRP20080382A2 (en) 2008-12-31
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ZA200402184B (en) 2005-07-27
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US20050267097A1 (en) 2005-12-01
IS3006B (is) 2018-11-15
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DK1427415T3 (da) 2009-11-23
KR100908176B1 (ko) 2009-07-16
JP2009079059A (ja) 2009-04-16
UA78232C2 (uk) 2007-03-15
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