CN104080772B - 抗凝血逆转剂 - Google Patents
抗凝血逆转剂 Download PDFInfo
- Publication number
- CN104080772B CN104080772B CN201280060950.2A CN201280060950A CN104080772B CN 104080772 B CN104080772 B CN 104080772B CN 201280060950 A CN201280060950 A CN 201280060950A CN 104080772 B CN104080772 B CN 104080772B
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- CN
- China
- Prior art keywords
- dap
- compound
- anticoagulant
- pharmaceutically acceptable
- factor
- 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.)
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- UAWMAVPSNYFQBS-UHFFFAOYSA-N CNC(N=C)=[N]=C Chemical compound CNC(N=C)=[N]=C UAWMAVPSNYFQBS-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
-
- 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
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- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Physiology (AREA)
- Nutrition Science (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Investigating Or Analysing Biological Materials (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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 CN104080772A (zh) | 2014-10-01 |
| CN104080772B true 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 (34)
Families Citing this family (12)
| 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 |
| JP7034084B2 (ja) | 2016-03-28 | 2022-03-11 | インサイト・コーポレイション | Tam阻害剤としてのピロロトリアジン化合物 |
| CA3077308A1 (en) | 2017-09-27 | 2019-04-04 | Incyte Corporation | Salts of pyrrolotriazine derivatives useful as tam inhibitors |
| BR112019027735A8 (pt) * | 2017-11-13 | 2020-10-13 | Maximum Fidelity Surgical Simulations Llc | reconstituição de circulação pós-morte, métodos e procedimentos especializados |
| EA202190153A1 (ru) | 2018-06-29 | 2021-04-09 | Инсайт Корпорейшн | Составы ингибитора 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 |
| 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 |
| AU2021230385A1 (en) | 2020-03-06 | 2022-09-22 | Incyte Corporation | Combination therapy comprising AXL/MER and PD-1/PD-L1 inhibitors |
| WO2024199096A1 (zh) * | 2023-03-24 | 2024-10-03 | 陕西麦科奥特科技有限公司 | 一种抗凝逆转剂及其制备方法和应用 |
| CN117624137A (zh) * | 2023-12-04 | 2024-03-01 | 中国药科大学 | 三嗪骨架小分子肝素逆转剂及其制备方法与用途 |
| EP4667582A1 (en) * | 2024-06-20 | 2025-12-24 | Instrumentation Laboratory Company | Factor xa reagent |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| EP0932615A1 (en) | 1996-10-11 | 1999-08-04 | 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 |
| CA2373610A1 (en) | 1999-05-19 | 2000-11-23 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents |
| 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 |
| EP1274676A2 (en) | 2000-04-17 | 2003-01-15 | Pharmacia Corporation | Polycyclic aryl and heteroaryl substituted 1,4-quinones useful for selective inhibition of the coagulation cascade |
| CA2462305A1 (en) | 2001-10-03 | 2003-04-10 | Michael S. South | 6-membered heterocyclic compounds useful for selective inhibition of the coagulation cascade |
| WO2003082809A1 (en) * | 2002-03-27 | 2003-10-09 | Glaxo Group Limited | Diaminoacid-aminoacid-polyamine based gemini surfactant compounds |
| JPWO2003099324A1 (ja) * | 2002-05-23 | 2005-09-22 | 中外製薬株式会社 | 組織因子阻害剤中和剤及び活性型血液凝固第vii因子製剤中和剤 |
| GB0214122D0 (en) * | 2002-06-19 | 2002-07-31 | Eastman Kodak Co | High contrast photographic element containing a polyhydrazide nucleating agent |
| US20060045865A1 (en) | 2004-08-27 | 2006-03-02 | Spherics, Inc. | Controlled regional oral delivery |
| KR102069498B1 (ko) * | 2007-09-28 | 2020-01-23 | 포톨라 파마슈티컬스, 인코포레이티드 | 인자 Xa 저해제에 대한 안티도트 및 그것을 사용하는 방법 |
| GB2476643B (en) | 2009-12-23 | 2012-11-14 | Haomamedica Ltd | 1,4-Dihydro-1,4-dioxonaphtalene derivatives as anticoagulants |
| AR079944A1 (es) | 2010-01-20 | 2012-02-29 | Boehringer Ingelheim Int | Anticuerpo neutralizante de la actividad de un anticoagulante |
| AP2013007046A0 (en) | 2011-03-30 | 2013-08-31 | Boehringer Ingelheim Int | Anticoagulant antidotes |
-
2012
- 2012-11-29 KR KR1020147016304A patent/KR101892330B1/ko active Active
- 2012-11-29 DK DK12806229.6T patent/DK2785700T3/en 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 HR HRP20160513TT patent/HRP20160513T1/hr unknown
- 2012-11-29 AP AP2014007662A patent/AP2014007662A0/xx unknown
- 2012-11-29 AR ARP120104474A patent/AR089020A1/es active IP Right Grant
- 2012-11-29 WO PCT/US2012/066938 patent/WO2013082210A1/en not_active Ceased
- 2012-11-29 SI SI201230558A patent/SI2785700T1/sl unknown
- 2012-11-29 AU AU2012345975A patent/AU2012345975B2/en active Active
- 2012-11-29 PE PE2014000763A patent/PE20141295A1/es active IP Right Grant
- 2012-11-29 EP EP12806229.6A patent/EP2785700B1/en active Active
- 2012-11-29 EA EA201490823A patent/EA027603B1/ru unknown
- 2012-11-29 CN CN201280060950.2A patent/CN104080772B/zh active Active
- 2012-11-29 US US13/688,442 patent/US9522892B2/en active Active
- 2012-11-29 ME MEP-2016-95A patent/ME02424B/me unknown
- 2012-11-29 BR BR112014012892-8A patent/BR112014012892B1/pt active IP Right Grant
- 2012-11-29 ES ES12806229.6T patent/ES2569674T3/es active Active
- 2012-11-29 JP JP2014544857A patent/JP6134731B2/ja active Active
- 2012-11-29 PL PL12806229.6T patent/PL2785700T3/pl unknown
- 2012-11-29 SG SG11201402713WA patent/SG11201402713WA/en unknown
- 2012-11-29 PT PT128062296T patent/PT2785700E/pt unknown
- 2012-11-29 UA UAA201404997A patent/UA116336C2/uk unknown
- 2012-11-29 HU HUE12806229A patent/HUE027452T2/en unknown
- 2012-11-29 RS RS20160318A patent/RS54738B1/sr unknown
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2014
- 2014-05-26 PH PH12014501176A patent/PH12014501176B1/en unknown
- 2014-05-26 IL IL232788A patent/IL232788B/en active IP Right Grant
- 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
-
2016
- 2016-04-25 CY CY20161100338T patent/CY1117414T1/el 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
-
2023
- 2023-12-15 US US18/541,391 patent/US20240366592A1/en active Pending
Patent Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CN1198748A (zh) * | 1995-10-02 | 1998-11-11 | 赫彻斯特马里恩鲁斯公司 | 多氟烷基色氨酸三肽凝血酶抑制剂 |
| 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 |
|---|
| Bleeding risk and the management of bleeding complications in patients undergoing anticoagulant therapy: focus on new anticoagulant agents;Mark A. Crowther,等;《BLOOD》;20080515;第111卷(第10期);第4874页表2 * |
| Guanidines with Antihypertensive Activity.II;Robert P. Mull,等;《Journal of medicinal and pharmaceutical chemistry》;19621231;第5卷;第948页表III * |
| Heterocyclic Quinones VIII. Synthesis and spectra of new carbazoloquinone derivatives of naturally occurring amino acids;Ahmed Sabet Hammam;《Journal of Applied Chemistry and Biotechnology》;19761231;第26卷(第1期);第670页 * |
| Potent Dibasic GPIIb/IIIa Antagonists with Reduced Prolongation of Bleeding Time: Synthesis and Pharmacological Evaluation of 2-Oxopiperazine Derivatives;Shuji Kitamura,等;《Journal of Medicinal Chemistry》;20010621;第44卷(第15期);第2443页表3 * |
| Preparation of some substituted guanidines;Fritz Bischoff;《The Journal of Biological Chemistry》;19281231;第80卷;第347页 * |
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Effective date of registration: 20230626 Address after: Swiss Express Patentee after: Kravis Pharmaceuticals Co.,Ltd. Address before: Connecticut USA Patentee before: Peiros Phil pharmaceutical Co. |
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| CP03 | Change of name, title or address |
Address after: Switzerland Patentee after: Sila Patra Holding Limited Country or region after: Switzerland Address before: Switzerland Patentee before: Kewei Medical Holding Co., Ltd. Country or region before: Switzerland Address after: Luxembourg Patentee after: Xirapathe Holding Co., Ltd. Country or region after: Luxembourg Address before: Switzerland Patentee before: Sila Patra Holding Limited Country or region before: Switzerland |
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| TR01 | Transfer of patent right |
Effective date of registration: 20251216 Address after: Switzerland Patentee after: Kewei Medical Holding Co., Ltd. Country or region after: Switzerland Address before: Chug, Switzerland Patentee before: Kravis Pharmaceuticals Co.,Ltd. Country or region before: Switzerland |