JP2004520290A5 - - Google Patents
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- JP2004520290A5 JP2004520290A5 JP2002546515A JP2002546515A JP2004520290A5 JP 2004520290 A5 JP2004520290 A5 JP 2004520290A5 JP 2002546515 A JP2002546515 A JP 2002546515A JP 2002546515 A JP2002546515 A JP 2002546515A JP 2004520290 A5 JP2004520290 A5 JP 2004520290A5
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- 150000001875 compounds Chemical class 0.000 claims 22
- 150000003839 salts Chemical class 0.000 claims 12
- 239000011780 sodium chloride Substances 0.000 claims 12
- 239000004480 active ingredient Substances 0.000 claims 4
- 230000002429 anti-coagulation Effects 0.000 claims 4
- 239000003146 anticoagulant agent Substances 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 239000002671 adjuvant Substances 0.000 claims 3
- 230000000240 adjuvant Effects 0.000 claims 3
- 239000000969 carrier Substances 0.000 claims 3
- 239000003085 diluting agent Substances 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- NKCXQMYPWXSLIZ-PSRDDEIFSA-N (2S)-2-[[(2S)-1-[(2S)-5-amino-2-[[2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-amino-3-hydroxybutanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]propanoyl]amino]-4-oxobutanoyl]amino]-3-m Chemical compound O=C([C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@@H](N)[C@@H](C)O)[C@@H](C)O)C(C)C)N1CCC[C@H]1C(=O)N[C@@H](CO)C(O)=O NKCXQMYPWXSLIZ-PSRDDEIFSA-N 0.000 claims 2
- 108090000190 Thrombin Proteins 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- 229960004072 thrombin Drugs 0.000 claims 2
- 210000004369 Blood Anatomy 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 239000011159 matrix material Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 201000005665 thrombophilia Diseases 0.000 claims 1
- 210000001519 tissues Anatomy 0.000 claims 1
Claims (17)
- Ph(3-Cl)(5-OCHF2)-(R)CH(OH)C(O)-Aze-Pab；
Ph(3-Cl)(5-OCHF2)-(R)CH(OH)C(O)-Aze-Pab(OMe)；または
Ph(3-Cl)(5-OCHF2)-(R)CH(OH)C(O)-Aze-Pab(OH)；
から選択される化合物またはその医薬用として許容しうる塩。 - 請求項１に記載の化合物Ph(3-Cl)(5-OCHF 2 )-(R)CH(OH)C(O)-Aze-Pab(OMe)またはその医薬用として許容しうる塩。
- 請求項１に記載の化合物又は前記化合物の医薬用として許容しうる塩のいずれかを、医薬用として許容しうるアジュバント、希釈剤、もしくはキャリヤーと混合した状態で含む医薬製剤。
- 請求項２に記載の化合物又は前記化合物の医薬用として許容しうる塩を、医薬用として許容しうるアジュバント、希釈剤、もしくはキャリヤーと混合した状態で含む、請求項３に記載の医薬製剤。
- アジュバント、希釈剤、及び／又はキャリヤーが、化合物の放出調節を生じる、請求項３または４に記載の医薬製剤
- 経口投与に使用すべく造られている、請求項３または４に記載の医薬製剤。
- 親水性のゲル化成分と活性成分とを含んだゲル化マトリックス放出調節システムの形態をとっている、請求項５または６に記載の医薬製剤。
- 医薬として使用するための、請求項１または２に記載の化合物又は前記化合物の医薬用として許容しうる塩。
- トロンビンの阻害が必要とされる状態の処置において使用するための、請求項１または２に記載の化合物又は前記化合物の医薬用として許容しうる塩。
- 抗凝固療法が適応とされる状態の処置において使用するための、請求項１または２に記載の化合物又は前記化合物の医薬用として許容しうる塩。
- 血栓の処置において使用するための、請求項１または２に記載の化合物又は前記化合物の医薬用として許容しうる塩。
- 抗凝固薬として使用するための、請求項１または２に記載の化合物又は前記化合物の医薬用として許容しうる塩。
- 請求項１または２に記載の化合物又は前記化合物の医薬用として許容しうる塩の、トロンビンの阻害が必要とされる状態を処置するための薬物を製造するための活性成分としての使用。
- 請求項１または２に記載の化合物又は前記化合物の医薬用として許容しうる塩の、抗凝固療法が適応とされる状態を処置するための医薬を製造するための活性成分としての使用。
- 前記状態が血栓である、請求項１３または１４に記載の使用。
- 前記状態が血液及び／又は組織における凝固能亢進である、請求項１３または１４に記載の使用。
- 請求項１または２に記載の化合物又は前記化合物の医薬用として許容しうる塩の、抗凝固薬を製造するための活性成分としての使用。
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE0004458A SE0004458D0 (sv) | 2000-12-01 | 2000-12-01 | Pharmaceutically useful compounds |
| SE0100965A SE0100965D0 (sv) | 2001-03-19 | 2001-03-19 | Pharmaceutically-useful compounds |
| SE0101239A SE0101239D0 (sv) | 2001-04-06 | 2001-04-06 | Pharmaceutically useful compounds |
| SE0102921A SE0102921D0 (sv) | 2001-08-30 | 2001-08-30 | Pharmaceutically useful compounds |
| PCT/SE2001/002657 WO2002044145A1 (en) | 2000-12-01 | 2001-11-30 | New mandelic acid derivatives and their use as throbin inhibitors |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008006608A Division JP2008156362A (ja) | 2000-12-01 | 2008-01-16 | 新規マンデル酸誘導体とそれらのトロンビン阻害剤としての使用 |
| JP2008006611A Division JP2008138009A (ja) | 2000-12-01 | 2008-01-16 | 新規マンデル酸誘導体とそれらのトロンビン阻害剤としての使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2004520290A JP2004520290A (ja) | 2004-07-08 |
| JP2004520290A5 true JP2004520290A5 (ja) | 2008-03-06 |
| JP4177101B2 JP4177101B2 (ja) | 2008-11-05 |
Family
ID=27484527
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002546515A Expired - Fee Related JP4177101B2 (ja) | 2000-12-01 | 2001-11-30 | 新規マンデル酸誘導体とそれらのトロンビン阻害剤としての使用 |
| JP2008006611A Pending JP2008138009A (ja) | 2000-12-01 | 2008-01-16 | 新規マンデル酸誘導体とそれらのトロンビン阻害剤としての使用 |
| JP2008006608A Pending JP2008156362A (ja) | 2000-12-01 | 2008-01-16 | 新規マンデル酸誘導体とそれらのトロンビン阻害剤としての使用 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008006611A Pending JP2008138009A (ja) | 2000-12-01 | 2008-01-16 | 新規マンデル酸誘導体とそれらのトロンビン阻害剤としての使用 |
| JP2008006608A Pending JP2008156362A (ja) | 2000-12-01 | 2008-01-16 | 新規マンデル酸誘導体とそれらのトロンビン阻害剤としての使用 |
Country Status (30)
| Country | Link |
|---|---|
| US (4) | US7803954B2 (ja) |
| EP (2) | EP2186800A1 (ja) |
| JP (3) | JP4177101B2 (ja) |
| KR (4) | KR100914016B1 (ja) |
| CN (1) | CN1291975C (ja) |
| AR (2) | AR035216A1 (ja) |
| AT (1) | ATE461171T1 (ja) |
| AU (2) | AU2007203520B2 (ja) |
| BG (1) | BG66261B1 (ja) |
| BR (1) | BR0115861A (ja) |
| CA (1) | CA2436220C (ja) |
| CY (1) | CY1113487T1 (ja) |
| CZ (1) | CZ303708B6 (ja) |
| DE (1) | DE60141603D1 (ja) |
| DK (1) | DK1347955T3 (ja) |
| EE (1) | EE05382B1 (ja) |
| ES (1) | ES2341318T3 (ja) |
| HK (1) | HK1057214A1 (ja) |
| HU (1) | HU228814B1 (ja) |
| IL (1) | IL156096A0 (ja) |
| IS (1) | IS2755B (ja) |
| MX (1) | MXPA03004794A (ja) |
| MY (1) | MY136133A (ja) |
| NO (3) | NO325228B1 (ja) |
| NZ (1) | NZ526205A (ja) |
| PL (1) | PL207045B1 (ja) |
| PT (1) | PT1347955E (ja) |
| SI (1) | SI1347955T1 (ja) |
| SK (1) | SK287692B6 (ja) |
| WO (1) | WO2002044145A1 (ja) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| AR034517A1 (es) | 2001-06-21 | 2004-02-25 | Astrazeneca Ab | Formulacion farmaceutica |
| SE0201662D0 (sv) * | 2002-05-31 | 2002-05-31 | Astrazeneca Ab | Pharmaceutical combination |
| SE0201658D0 (sv) * | 2002-05-31 | 2002-05-31 | Astrazeneca Ab | Immediate release pharmaceutical formulation |
| SE0201659D0 (sv) * | 2002-05-31 | 2002-05-31 | Astrazeneca Ab | Modified release pharmaceutical formulation |
| SE0201661D0 (sv) | 2002-05-31 | 2002-05-31 | Astrazeneca Ab | New salts |
| JP4697962B2 (ja) | 2003-02-13 | 2011-06-08 | ウェルスタット セラピューティクス コーポレイション | 代謝性障害の処置のための化合物 |
| GB0306615D0 (en) * | 2003-03-22 | 2003-04-30 | Astrazeneca Ab | New use |
| US7781424B2 (en) * | 2003-05-27 | 2010-08-24 | Astrazeneca Ab | Modified release pharmaceutical formulation |
| SE0303220D0 (sv) * | 2003-11-28 | 2003-11-28 | Astrazeneca Ab | New process |
| US7550499B2 (en) | 2004-05-12 | 2009-06-23 | Bristol-Myers Squibb Company | Urea antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions |
| ATE499370T1 (de) | 2005-01-19 | 2011-03-15 | Bristol Myers Squibb Co | 2-phenoxy-n-(1,3,4-thiadizol-2-yl)pyridin-3- aminderivate und verwandte verbindungen als p2y1- rezeptor-hemmer zur behandlung thromboembolischer erkrankungen |
| GB0503672D0 (en) * | 2005-02-23 | 2005-03-30 | Astrazeneca Ab | New process |
| GB0510546D0 (en) * | 2005-05-24 | 2005-06-29 | Astrazeneca Ab | New process |
| DE602006020871D1 (de) | 2005-06-27 | 2011-05-05 | Bristol Myers Squibb Co | Lineare harnstoffmimetika-antagonisten des p2y1-rezeptors zur behandlung von thromboseleiden |
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| US7728008B2 (en) | 2005-06-27 | 2010-06-01 | Bristol-Myers Squibb Company | N-linked heterocyclic antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions |
| WO2007087505A2 (en) | 2006-01-25 | 2007-08-02 | Wellstat Therapeutics Corporation | Compounds for the treatment of metabolic disorders |
| WO2007087504A2 (en) | 2006-01-25 | 2007-08-02 | Wellstat Therapeutics Corporation | Compounds for the treatment of metabolic disorders |
| CA2639939A1 (en) | 2006-02-02 | 2007-08-16 | Wellstat Therapeutics Corporation | Compounds for the treatment of metabolic disorders |
| US8044242B2 (en) | 2006-03-09 | 2011-10-25 | Bristol-Myers Squibb Company | 2-(aryloxy) acetamide factor VIIa inhibitors useful as anticoagulants |
| CN101500993A (zh) | 2006-06-08 | 2009-08-05 | 百时美施贵宝公司 | 作为凝血因子Ⅶa抑制剂用作抗凝血药的2-氨基羰基苯基氨基-2-苯基乙酰胺 |
| DE102006033572A1 (de) | 2006-07-20 | 2008-01-24 | Bayer Cropscience Ag | N'-Cyano-N-halogenalkyl-imidamid Derivate |
| US7960569B2 (en) | 2006-10-17 | 2011-06-14 | Bristol-Myers Squibb Company | Indole antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions |
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| CN101605779B (zh) | 2006-12-15 | 2013-11-20 | 百时美施贵宝公司 | 作为凝血因子xia抑制剂的芳基丙酰胺、芳基丙烯酰胺、芳基丙炔酰胺或芳基甲基脲类似物 |
| PE20081775A1 (es) | 2006-12-20 | 2008-12-18 | Bristol Myers Squibb Co | Compuestos macrociclicos como inhibidores del factor viia |
| AU2008241091B2 (en) | 2007-04-23 | 2013-05-09 | Sanofi-Aventis | Quinoline-carboxamide derivatives as P2Y12 antagonists |
| TW200900033A (en) * | 2007-06-21 | 2009-01-01 | Wen-Qing Li | Automatic brewing machine |
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| WO2009080226A2 (en) | 2007-12-26 | 2009-07-02 | Sanofis-Aventis | Heterocyclic pyrazole-carboxamides as p2y12 antagonists |
| JP5841547B2 (ja) | 2010-02-11 | 2016-01-13 | 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マクロ環 |
| 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 |
| 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 |
| EP2899183B1 (en) | 2011-10-14 | 2018-09-19 | Bristol-Myers Squibb Company | Substituted Tetrahydroisoquinoline Compounds as Factor Xia Inhibitors |
| IN2014CN02805A (ja) | 2011-10-14 | 2015-07-03 | Bristol Myers Squibb Co | |
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| NO2721243T3 (ja) | 2014-10-01 | 2018-10-20 | ||
| JP6742348B2 (ja) | 2015-06-19 | 2020-08-19 | 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ジアミド大員環 |
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-
2001
- 2001-11-28 AR ARP010105543A patent/AR035216A1/es active IP Right Grant
- 2001-11-29 MY MYPI20015470A patent/MY136133A/en unknown
- 2001-11-30 KR KR1020037007353A patent/KR100914016B1/ko not_active IP Right Cessation
- 2001-11-30 EP EP10152378A patent/EP2186800A1/en not_active Withdrawn
- 2001-11-30 BR BR0115861-9A patent/BR0115861A/pt active Search and Examination
- 2001-11-30 ES ES01998535T patent/ES2341318T3/es not_active Expired - Lifetime
- 2001-11-30 AT AT01998535T patent/ATE461171T1/de active
- 2001-11-30 WO PCT/SE2001/002657 patent/WO2002044145A1/en active Application Filing
- 2001-11-30 DE DE60141603T patent/DE60141603D1/de not_active Expired - Lifetime
- 2001-11-30 PT PT01998535T patent/PT1347955E/pt unknown
- 2001-11-30 EE EEP200300259A patent/EE05382B1/xx not_active IP Right Cessation
- 2001-11-30 EP EP01998535A patent/EP1347955B1/en not_active Expired - Lifetime
- 2001-11-30 NZ NZ526205A patent/NZ526205A/en not_active IP Right Cessation
- 2001-11-30 PL PL362917A patent/PL207045B1/pl unknown
- 2001-11-30 SK SK651-2003A patent/SK287692B6/sk not_active IP Right Cessation
- 2001-11-30 SI SI200130965T patent/SI1347955T1/sl unknown
- 2001-11-30 KR KR1020087014402A patent/KR100914535B1/ko not_active IP Right Cessation
- 2001-11-30 KR KR1020087014404A patent/KR100914537B1/ko not_active IP Right Cessation
- 2001-11-30 CA CA2436220A patent/CA2436220C/en not_active Expired - Fee Related
- 2001-11-30 DK DK01998535.7T patent/DK1347955T3/da active
- 2001-11-30 KR KR1020097002806A patent/KR100947296B1/ko not_active IP Right Cessation
- 2001-11-30 CZ CZ20031514A patent/CZ303708B6/cs not_active IP Right Cessation
- 2001-11-30 IL IL15609601A patent/IL156096A0/xx not_active IP Right Cessation
- 2001-11-30 CN CNB018223168A patent/CN1291975C/zh not_active Expired - Fee Related
- 2001-11-30 HU HU0302487A patent/HU228814B1/hu not_active IP Right Cessation
- 2001-11-30 MX MXPA03004794A patent/MXPA03004794A/es active IP Right Grant
- 2001-11-30 JP JP2002546515A patent/JP4177101B2/ja not_active Expired - Fee Related
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2003
- 2003-05-19 BG BG107825A patent/BG66261B1/bg unknown
- 2003-05-27 IS IS6828A patent/IS2755B/is unknown
- 2003-05-30 NO NO20032465A patent/NO325228B1/no not_active IP Right Cessation
-
2004
- 2004-01-06 HK HK04100090.5A patent/HK1057214A1/xx not_active IP Right Cessation
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2006
- 2006-09-13 US US11/520,063 patent/US7803954B2/en not_active Expired - Fee Related
- 2006-09-13 US US11/520,052 patent/US20070218136A1/en not_active Abandoned
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2007
- 2007-05-04 US US11/797,656 patent/US7645751B2/en not_active Expired - Fee Related
- 2007-07-27 AU AU2007203520A patent/AU2007203520B2/en not_active Expired - Fee Related
- 2007-07-27 AU AU2007203509A patent/AU2007203509A1/en not_active Abandoned
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2008
- 2008-01-03 NO NO20080031A patent/NO20080031L/no not_active Application Discontinuation
- 2008-01-03 NO NO20080030A patent/NO20080030L/no not_active Application Discontinuation
- 2008-01-16 JP JP2008006611A patent/JP2008138009A/ja active Pending
- 2008-01-16 JP JP2008006608A patent/JP2008156362A/ja active Pending
-
2009
- 2009-06-25 US US12/491,456 patent/US20100087651A1/en not_active Abandoned
- 2009-07-31 AR ARP090102945A patent/AR072331A2/es unknown
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2010
- 2010-05-17 CY CY20101100436T patent/CY1113487T1/el unknown
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