CN104080772A - 抗凝血逆转剂 - Google Patents
抗凝血逆转剂 Download PDFInfo
- Publication number
- CN104080772A CN104080772A CN201280060950.2A CN201280060950A CN104080772A CN 104080772 A CN104080772 A CN 104080772A CN 201280060950 A CN201280060950 A CN 201280060950A CN 104080772 A CN104080772 A CN 104080772A
- Authority
- CN
- China
- Prior art keywords
- compound
- dap
- experimenter
- methods
- acceptable salt
- 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.)
- Granted
Links
- 0 *NC(NICN1CC(CINC(I*)=O)NCC1)=O Chemical compound *NC(NICN1CC(CINC(I*)=O)NCC1)=O 0.000 description 1
- XUSNPFGLKGCWGN-UHFFFAOYSA-N NCCCN1CCN(CCCN)CC1 Chemical compound NCCCN1CCN(CCCN)CC1 XUSNPFGLKGCWGN-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/12—Ketones
- A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
- C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/13—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
Abstract
Description
LMWH | 平均分子量 | 抗-Xa/抗-IIa活性比率 |
贝米肝素 | 3600 | 9.7 |
舍托肝素 | 5400 | 2.4 |
达肝素钠 | 6000 | 2.5 |
依诺肝素 | 4500 | 3.9 |
那屈肝素 | 4300 | 3.3 |
帕肝素 | 5000 | 2.3 |
瑞维肝素 | 4400 | 4.2 |
亭扎肝素 | 6500 | 1.6 |
Claims (37)
Applications Claiming Priority (9)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201161564559P | 2011-11-29 | 2011-11-29 | |
US61/564,559 | 2011-11-29 | ||
US201261614292P | 2012-03-22 | 2012-03-22 | |
US61/614,292 | 2012-03-22 | ||
US201261641698P | 2012-05-02 | 2012-05-02 | |
US61/641,698 | 2012-05-02 | ||
US201261666291P | 2012-06-29 | 2012-06-29 | |
US61/666,291 | 2012-06-29 | ||
PCT/US2012/066938 WO2013082210A1 (en) | 2011-11-29 | 2012-11-29 | Anticoagulant reversal agents |
Publications (2)
Publication Number | Publication Date |
---|---|
CN104080772A true CN104080772A (zh) | 2014-10-01 |
CN104080772B CN104080772B (zh) | 2016-10-05 |
Family
ID=47430065
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201280060950.2A Active CN104080772B (zh) | 2011-11-29 | 2012-11-29 | 抗凝血逆转剂 |
Country Status (35)
Country | Link |
---|---|
US (4) | US9522892B2 (zh) |
EP (1) | EP2785700B1 (zh) |
JP (1) | JP6134731B2 (zh) |
KR (1) | KR101892330B1 (zh) |
CN (1) | CN104080772B (zh) |
AP (1) | AP2014007662A0 (zh) |
AR (1) | AR089020A1 (zh) |
AU (1) | AU2012345975B2 (zh) |
BR (1) | BR112014012892B1 (zh) |
CA (1) | CA2856540C (zh) |
CL (1) | CL2014001399A1 (zh) |
CO (1) | CO6990738A2 (zh) |
CR (1) | CR20140310A (zh) |
CY (1) | CY1117414T1 (zh) |
DK (1) | DK2785700T3 (zh) |
EA (1) | EA027603B1 (zh) |
EC (1) | ECSP14006696A (zh) |
ES (1) | ES2569674T3 (zh) |
HK (1) | HK1202858A1 (zh) |
HR (1) | HRP20160513T1 (zh) |
HU (1) | HUE027452T2 (zh) |
IL (1) | IL232788B (zh) |
ME (1) | ME02424B (zh) |
MX (1) | MX349514B (zh) |
PE (1) | PE20141295A1 (zh) |
PH (1) | PH12014501176A1 (zh) |
PL (1) | PL2785700T3 (zh) |
PT (1) | PT2785700E (zh) |
RS (1) | RS54738B1 (zh) |
SG (1) | SG11201402713WA (zh) |
SI (1) | SI2785700T1 (zh) |
SM (1) | SMT201600161B (zh) |
UA (1) | UA116336C2 (zh) |
WO (1) | WO2013082210A1 (zh) |
ZA (1) | ZA201404793B (zh) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN112010930A (zh) * | 2019-05-28 | 2020-12-01 | 首都医科大学 | Rgd修饰的五环哌嗪二酮及其制备和应用 |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US9999690B2 (en) | 2013-11-08 | 2018-06-19 | Perosphere Pharmaceuticals Inc. | Labeled compounds and methods of imaging, diagnosing cartilage disorders and diseases, and monitoring cartilage health using labeled and unlabeled compounds |
BR112019027735A8 (pt) * | 2017-11-13 | 2020-10-13 | Maximum Fidelity Surgical Simulations Llc | reconstituição de circulação pós-morte, métodos e procedimentos especializados |
MX2021000127A (es) | 2018-06-29 | 2021-03-29 | Incyte Corp | Formulaciones de un inhibidor de axl/mer. |
US11716989B2 (en) | 2019-04-16 | 2023-08-08 | Maximum Fidelity Surgical Simulations, LLC | Cadaver preservation systems and methods |
US11915610B2 (en) | 2019-05-15 | 2024-02-27 | Maximum Fidelity Surgical Simulations, LLC | Cadaverous heart model |
Citations (6)
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WO1996010022A1 (en) * | 1994-09-26 | 1996-04-04 | Zeneca Limited | Aminoheterocyclic derivatives as antithrombotic or anticoagulant agents |
WO1997012904A1 (en) * | 1995-10-02 | 1997-04-10 | Hoechst Marion Roussel, Inc. | Polyfluoroalkyl tryptophan tripeptide thrombin inhibitors |
CN1314895A (zh) * | 1998-07-17 | 2001-09-26 | L·拉峰试验公司 | 取代的哌嗪酮及其治疗应用 |
US20020022614A1 (en) * | 2000-06-29 | 2002-02-21 | Pinto Donald J.P. | Thrombin or factor Xa inhibitors |
US6403583B1 (en) * | 1998-12-23 | 2002-06-11 | Patrick Y. S. Lam | Thrombin or factor Xa inhibitors |
CN1905883A (zh) * | 2004-01-08 | 2007-01-31 | 阿斯利康(瑞典)有限公司 | 6-{4-[4-(1h-吲哚-2-磺酰基)-哌嗪-1-羰基-苯基]}哒嗪-3-酮的新衍生物 |
Family Cites Families (16)
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US3678157A (en) * | 1968-10-23 | 1972-07-18 | Oreal | Hair treatment compositions containing polycondensable compounds |
US6080852A (en) | 1996-06-27 | 2000-06-27 | The Perkin-Elmer Corporation | 4,7-dichlororhodamine dyes |
WO1998016547A1 (en) | 1996-10-11 | 1998-04-23 | Cor Therapeutics, Inc. | SELECTIVE FACTOR Xa INHIBITORS |
CA2285454A1 (en) * | 1997-04-07 | 1998-10-15 | Axys Pharmaceuticals Corporation | Compounds and compositions for treating diseases associated with serine protease, particularly tryptase, activity |
CN1152023C (zh) | 1999-05-19 | 2004-06-02 | 法玛西雅公司 | 作为抗凝血剂的取代的多环芳基与杂芳基尿嘧啶 |
EP1377554A1 (en) * | 1999-06-16 | 2004-01-07 | University Of Iowa Research Foundation | Antagonism of immunostimulatory cpg-oligonucleotides by 4-aminoquinolines and other weak bases |
JP2004501077A (ja) | 2000-04-17 | 2004-01-15 | ファルマシア・コーポレーション | 凝固カスケードの選択的阻害に有用な多環式アリールおよびヘテロアリール置換1,4−キノン |
US6969715B2 (en) | 2001-10-03 | 2005-11-29 | Pharmacia Corporation | 6-membered heterocyclic compounds useful for selective inhibition of the coagulation cascade |
AU2003217028A1 (en) * | 2002-03-27 | 2003-10-13 | Cambridge University Technical Services Ltd | Diaminoacid-aminoacid-polyamine based gemini surfactant compounds |
US20060233786A1 (en) * | 2002-05-23 | 2006-10-19 | Chugai Seiyaku Kabushiki Kaisha | Agent neutralizint tissue factor inhibitor and agent neutralizing activated blood coagulation factor viii preparation |
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US20060045865A1 (en) | 2004-08-27 | 2006-03-02 | Spherics, Inc. | Controlled regional oral delivery |
ES2849426T3 (es) * | 2007-09-28 | 2021-08-18 | Alexion Pharma Inc | Antídotos para inhibidores del factor Xa y procedimientos de uso de los mismos |
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TWI513466B (zh) | 2010-01-20 | 2015-12-21 | Boehringer Ingelheim Int | 抗凝血劑解毒劑 |
WO2012130834A1 (en) | 2011-03-30 | 2012-10-04 | Boehringer Ingelheim International Gmbh | Anticoagulant antidotes |
-
2012
- 2012-11-29 AP AP2014007662A patent/AP2014007662A0/xx unknown
- 2012-11-29 AU AU2012345975A patent/AU2012345975B2/en active Active
- 2012-11-29 PT PT128062296T patent/PT2785700E/pt unknown
- 2012-11-29 PL PL12806229.6T patent/PL2785700T3/pl unknown
- 2012-11-29 PE PE2014000763A patent/PE20141295A1/es active IP Right Grant
- 2012-11-29 EA EA201490823A patent/EA027603B1/ru unknown
- 2012-11-29 SI SI201230558A patent/SI2785700T1/sl unknown
- 2012-11-29 CN CN201280060950.2A patent/CN104080772B/zh active Active
- 2012-11-29 AR ARP120104474A patent/AR089020A1/es active IP Right Grant
- 2012-11-29 KR KR1020147016304A patent/KR101892330B1/ko active IP Right Grant
- 2012-11-29 ME MEP-2016-95A patent/ME02424B/me unknown
- 2012-11-29 UA UAA201404997A patent/UA116336C2/uk unknown
- 2012-11-29 SG SG11201402713WA patent/SG11201402713WA/en unknown
- 2012-11-29 RS RS20160318A patent/RS54738B1/sr unknown
- 2012-11-29 ES ES12806229.6T patent/ES2569674T3/es active Active
- 2012-11-29 MX MX2014006349A patent/MX349514B/es active IP Right Grant
- 2012-11-29 CA CA2856540A patent/CA2856540C/en active Active
- 2012-11-29 DK DK12806229.6T patent/DK2785700T3/en active
- 2012-11-29 BR BR112014012892-8A patent/BR112014012892B1/pt active IP Right Grant
- 2012-11-29 US US13/688,442 patent/US9522892B2/en active Active
- 2012-11-29 EP EP12806229.6A patent/EP2785700B1/en active Active
- 2012-11-29 HU HUE12806229A patent/HUE027452T2/en unknown
- 2012-11-29 WO PCT/US2012/066938 patent/WO2013082210A1/en active Application Filing
- 2012-11-29 JP JP2014544857A patent/JP6134731B2/ja active Active
-
2014
- 2014-05-26 IL IL232788A patent/IL232788B/en active IP Right Grant
- 2014-05-26 PH PH12014501176A patent/PH12014501176A1/en unknown
- 2014-05-27 CL CL2014001399A patent/CL2014001399A1/es unknown
- 2014-06-26 CR CR20140310A patent/CR20140310A/es unknown
- 2014-06-26 EC ECIEPI20146696A patent/ECSP14006696A/es unknown
- 2014-06-26 CO CO14137450A patent/CO6990738A2/es unknown
- 2014-06-27 ZA ZA2014/04793A patent/ZA201404793B/en unknown
-
2015
- 2015-04-01 HK HK15103329.9A patent/HK1202858A1/zh unknown
-
2016
- 2016-04-25 CY CY20161100338T patent/CY1117414T1/el unknown
- 2016-05-13 HR HRP20160513TT patent/HRP20160513T1/hr unknown
- 2016-06-08 SM SM201600161T patent/SMT201600161B/it unknown
- 2016-11-10 US US15/348,348 patent/US9877961B2/en active Active
-
2017
- 2017-10-06 US US15/726,497 patent/US20180207152A1/en not_active Abandoned
-
2020
- 2020-12-10 US US17/117,559 patent/US20210169874A1/en not_active Abandoned
Patent Citations (7)
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WO1996010022A1 (en) * | 1994-09-26 | 1996-04-04 | Zeneca Limited | Aminoheterocyclic derivatives as antithrombotic or anticoagulant agents |
WO1997012904A1 (en) * | 1995-10-02 | 1997-04-10 | Hoechst Marion Roussel, Inc. | Polyfluoroalkyl tryptophan tripeptide thrombin inhibitors |
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CN1314895A (zh) * | 1998-07-17 | 2001-09-26 | L·拉峰试验公司 | 取代的哌嗪酮及其治疗应用 |
US6403583B1 (en) * | 1998-12-23 | 2002-06-11 | Patrick Y. S. Lam | Thrombin or factor Xa inhibitors |
US20020022614A1 (en) * | 2000-06-29 | 2002-02-21 | Pinto Donald J.P. | Thrombin or factor Xa inhibitors |
CN1905883A (zh) * | 2004-01-08 | 2007-01-31 | 阿斯利康(瑞典)有限公司 | 6-{4-[4-(1h-吲哚-2-磺酰基)-哌嗪-1-羰基-苯基]}哒嗪-3-酮的新衍生物 |
Non-Patent Citations (5)
Title |
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AHMED SABET HAMMAM: "Heterocyclic Quinones VIII. Synthesis and spectra of new carbazoloquinone derivatives of naturally occurring amino acids", 《JOURNAL OF APPLIED CHEMISTRY AND BIOTECHNOLOGY》 * |
FRITZ BISCHOFF: "Preparation of some substituted guanidines", 《THE JOURNAL OF BIOLOGICAL CHEMISTRY》 * |
MARK A. CROWTHER,等: "Bleeding risk and the management of bleeding complications in patients undergoing anticoagulant therapy: focus on new anticoagulant agents", 《BLOOD》 * |
ROBERT P. MULL,等: "Guanidines with Antihypertensive Activity.II", 《JOURNAL OF MEDICINAL AND PHARMACEUTICAL CHEMISTRY》 * |
SHUJI KITAMURA,等: "Potent Dibasic GPIIb/IIIa Antagonists with Reduced Prolongation of Bleeding Time: Synthesis and Pharmacological Evaluation of 2-Oxopiperazine Derivatives", 《JOURNAL OF MEDICINAL CHEMISTRY》 * |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN112010930A (zh) * | 2019-05-28 | 2020-12-01 | 首都医科大学 | Rgd修饰的五环哌嗪二酮及其制备和应用 |
CN112010930B (zh) * | 2019-05-28 | 2022-08-02 | 首都医科大学 | Rgd修饰的五环哌嗪二酮及其制备和应用 |
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