CA2686203A1 - Intravenous and oral dosing of a direct-acting and reversible p2y12 inhibitor - Google Patents
Intravenous and oral dosing of a direct-acting and reversible p2y12 inhibitor Download PDFInfo
- Publication number
- CA2686203A1 CA2686203A1 CA002686203A CA2686203A CA2686203A1 CA 2686203 A1 CA2686203 A1 CA 2686203A1 CA 002686203 A CA002686203 A CA 002686203A CA 2686203 A CA2686203 A CA 2686203A CA 2686203 A1 CA2686203 A1 CA 2686203A1
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- Prior art keywords
- compound
- composition
- platelet aggregation
- unit dose
- subject
- Prior art date
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- 229960001148 rivaroxaban Drugs 0.000 description 1
- 238000002390 rotary evaporation Methods 0.000 description 1
- 238000005070 sampling Methods 0.000 description 1
- 108010073863 saruplase Proteins 0.000 description 1
- 150000003335 secondary amines Chemical class 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 229910052938 sodium sulfate Inorganic materials 0.000 description 1
- 235000011152 sodium sulphate Nutrition 0.000 description 1
- 239000011877 solvent mixture Substances 0.000 description 1
- 238000003797 solvolysis reaction Methods 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 238000002336 sorption--desorption measurement Methods 0.000 description 1
- 230000002269 spontaneous effect Effects 0.000 description 1
- 238000013112 stability test Methods 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 230000000087 stabilizing effect Effects 0.000 description 1
- 238000010186 staining Methods 0.000 description 1
- 239000008174 sterile solution Substances 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 125000001424 substituent group Chemical group 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 150000005846 sugar alcohols Chemical class 0.000 description 1
- 229960003329 sulfinpyrazone Drugs 0.000 description 1
- MLKXDPUZXIRXEP-MFOYZWKCSA-N sulindac Chemical compound CC1=C(CC(O)=O)C2=CC(F)=CC=C2\C1=C/C1=CC=C(S(C)=O)C=C1 MLKXDPUZXIRXEP-MFOYZWKCSA-N 0.000 description 1
- 230000000153 supplemental effect Effects 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- XUTLOCQNGLJNSA-RGVLZGJSSA-N terbogrel Chemical compound CC(C)(C)\N=C(/NC#N)NC1=CC=CC(C(=C/CCCC(O)=O)\C=2C=NC=CC=2)=C1 XUTLOCQNGLJNSA-RGVLZGJSSA-N 0.000 description 1
- 229950006665 terbogrel Drugs 0.000 description 1
- KZZHPWMVEVZEFG-UHFFFAOYSA-N tert-butyl n-phenylcarbamate Chemical compound CC(C)(C)OC(=O)NC1=CC=CC=C1 KZZHPWMVEVZEFG-UHFFFAOYSA-N 0.000 description 1
- 150000003512 tertiary amines Chemical class 0.000 description 1
- HWEOXFSBSQIWSY-UHFFFAOYSA-N terutroban Chemical compound C1CC2=C(CCC(O)=O)C(C)=CC=C2CC1NS(=O)(=O)C1=CC=C(Cl)C=C1 HWEOXFSBSQIWSY-UHFFFAOYSA-N 0.000 description 1
- 229960004559 theobromine Drugs 0.000 description 1
- 229930192474 thiophene Natural products 0.000 description 1
- 239000003856 thrombin receptor antagonist Substances 0.000 description 1
- 230000002885 thrombogenetic effect Effects 0.000 description 1
- 230000002537 thrombolytic effect Effects 0.000 description 1
- 201000005665 thrombophilia Diseases 0.000 description 1
- 239000003768 thromboxane synthase inhibitor Substances 0.000 description 1
- OEKWJQXRCDYSHL-FNOIDJSQSA-N ticagrelor Chemical compound C1([C@@H]2C[C@H]2NC=2N=C(N=C3N([C@H]4[C@@H]([C@H](O)[C@@H](OCCO)C4)O)N=NC3=2)SCCC)=CC=C(F)C(F)=C1 OEKWJQXRCDYSHL-FNOIDJSQSA-N 0.000 description 1
- 229960002528 ticagrelor Drugs 0.000 description 1
- 229940028869 ticlid Drugs 0.000 description 1
- 229960005001 ticlopidine Drugs 0.000 description 1
- 229960001060 tioclomarol Drugs 0.000 description 1
- WRGOVNKNTPWHLZ-UHFFFAOYSA-N tioclomarol Chemical compound C=1C=C(Cl)C=CC=1C(O)CC(C=1C(OC2=CC=CC=C2C=1O)=O)C1=CC=C(Cl)S1 WRGOVNKNTPWHLZ-UHFFFAOYSA-N 0.000 description 1
- 229960003425 tirofiban Drugs 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- 150000004684 trihydrates Chemical class 0.000 description 1
- YFTHZRPMJXBUME-UHFFFAOYSA-N tripropylamine Chemical compound CCCN(CCC)CCC YFTHZRPMJXBUME-UHFFFAOYSA-N 0.000 description 1
- 229910052722 tritium Inorganic materials 0.000 description 1
- 229960005356 urokinase Drugs 0.000 description 1
- 238000005292 vacuum distillation Methods 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
- 208000004043 venous thromboembolism Diseases 0.000 description 1
- 229940063674 voltaren Drugs 0.000 description 1
- 238000010792 warming Methods 0.000 description 1
- 239000011534 wash buffer Substances 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 239000011701 zinc Substances 0.000 description 1
- 229910052725 zinc Inorganic materials 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Emergency Medicine (AREA)
- Engineering & Computer Science (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91564907P | 2007-05-02 | 2007-05-02 | |
| US60/915,649 | 2007-05-02 | ||
| US94792107P | 2007-07-03 | 2007-07-03 | |
| US60/947,921 | 2007-07-03 | ||
| PCT/US2008/062518 WO2008137753A2 (en) | 2007-05-02 | 2008-05-02 | Intravenous and oral dosing of a direct-acting and reversible p2y12 inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2686203A1 true CA2686203A1 (en) | 2008-11-13 |
Family
ID=39587015
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002686203A Abandoned CA2686203A1 (en) | 2007-05-02 | 2008-05-02 | Intravenous and oral dosing of a direct-acting and reversible p2y12 inhibitor |
Country Status (17)
| Country | Link |
|---|---|
| US (2) | US20090048216A1 (enExample) |
| EP (1) | EP2079464A2 (enExample) |
| JP (1) | JP2010526101A (enExample) |
| KR (1) | KR20100029746A (enExample) |
| CN (1) | CN101795682A (enExample) |
| AU (1) | AU2008247483A1 (enExample) |
| BR (1) | BRPI0811476A2 (enExample) |
| CA (1) | CA2686203A1 (enExample) |
| CO (1) | CO6241104A2 (enExample) |
| EA (1) | EA200901473A1 (enExample) |
| EC (1) | ECSP099778A (enExample) |
| GT (1) | GT200900284A (enExample) |
| IL (1) | IL201834A0 (enExample) |
| MA (1) | MA31663B1 (enExample) |
| MX (1) | MX2009011843A (enExample) |
| TN (1) | TN2009000451A1 (enExample) |
| WO (1) | WO2008137753A2 (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2627719C (en) * | 2005-11-03 | 2016-07-12 | Portola Pharmaceuticals, Inc. | [4-(6-halo-7-substituted-2,4-dioxo-1,4-dihydro-2h-quinazolin-3-yl)-phenyl]-5-chloro-thiophen-2-yl-sulfonylureas and forms and methods related thereto |
| CN101622234B (zh) * | 2007-03-06 | 2013-08-07 | 诺瓦提斯公司 | 适于治疗炎性或变应性病症的二环有机化合物 |
| US20090156620A1 (en) * | 2007-05-02 | 2009-06-18 | Portola Pharmaceuticals, Inc. | [4-(6-fluoro-7-methylamino-2,4-dioxo-1,4-dihydro-2h-quinazolin-3-yl)-phenyl]-5-chloro-thiophen-2-yl-sulfonylurea salts, forms and methods related thereto |
| CA2686221A1 (en) * | 2007-05-02 | 2008-11-13 | Portola Pharmaceuticals, Inc. | [4-(6-fluoro-7-methylamino-2,4-dioxo-1,4-dihydro-2h-quinazolin-3-yl)-phenyl]-5-chloro-thiophen-2-yl-sulfonylurea salts, forms and methods related thereto |
| US9427448B2 (en) * | 2009-11-11 | 2016-08-30 | The Medicines Company | Methods of treating, reducing the incidence of, and/or preventing ischemic events |
| CN102271685A (zh) * | 2008-12-30 | 2011-12-07 | 斯若姆博洛捷克有限公司 | 鉴定发展成器官功能衰竭的风险提高的危重患者的方法及用于其治疗的化合物 |
| US10376532B2 (en) | 2009-11-11 | 2019-08-13 | Chiesi Farmaceutici, S.P.A. | Methods of treating, reducing the incidence of, and/or preventing ischemic events |
| EP2498731B1 (en) | 2009-11-11 | 2020-01-22 | Chiesi Farmaceutici S.p.A. | Methods of treating or preventing stent thrombosis |
| ES2550033T3 (es) * | 2009-12-23 | 2015-11-04 | Ratiopharm Gmbh | Forma de dosificación farmacéutica sólida de ticagrelor |
| WO2011088152A1 (en) | 2010-01-12 | 2011-07-21 | Portola Pharmaceuticals, Inc. | Pharmaceutical composition and dosage forms of elinogrel and methods of use thereof |
| WO2011137459A1 (en) * | 2010-04-30 | 2011-11-03 | Portola Pharmaceuticals, Inc. | Dosage forms of elinogrel and methods of injectable administration thereof |
| US9029095B2 (en) | 2010-12-01 | 2015-05-12 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Method and kits for determining platelet susceptibility to activation in a patient |
| JP2013544271A (ja) * | 2010-12-03 | 2013-12-12 | ポートラ ファーマシューティカルズ， インコーポレイテッド | 式（ｉ）の化合物の薬学的組成物、投薬形態、および新規の形態、ならびにその使用方法 |
| SG11201908128YA (en) | 2017-03-15 | 2019-10-30 | Idorsia Pharmaceuticals Ltd | Subcutaneous administration of a p2y12 receptor antagonist |
| ES3067885T3 (en) | 2017-06-23 | 2026-05-26 | Chiesi Farm Spa | Cangrelor for the treatment and/or prevention of shunt or stent thrombosis |
| CN107462648B (zh) * | 2017-08-21 | 2019-09-27 | 盐城锦明药业有限公司 | 一种Cangrelor中间体腺苷-2-硫酮的高效液相色谱检测方法 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6906063B2 (en) | 2000-02-04 | 2005-06-14 | Portola Pharmaceuticals, Inc. | Platelet ADP receptor inhibitors |
| CA2627719C (en) | 2005-11-03 | 2016-07-12 | Portola Pharmaceuticals, Inc. | [4-(6-halo-7-substituted-2,4-dioxo-1,4-dihydro-2h-quinazolin-3-yl)-phenyl]-5-chloro-thiophen-2-yl-sulfonylureas and forms and methods related thereto |
-
2008
- 2008-05-02 US US12/114,630 patent/US20090048216A1/en not_active Abandoned
- 2008-05-02 AU AU2008247483A patent/AU2008247483A1/en not_active Abandoned
- 2008-05-02 CN CN200880023071A patent/CN101795682A/zh active Pending
- 2008-05-02 MX MX2009011843A patent/MX2009011843A/es not_active Application Discontinuation
- 2008-05-02 EA EA200901473A patent/EA200901473A1/ru unknown
- 2008-05-02 KR KR1020097025059A patent/KR20100029746A/ko not_active Withdrawn
- 2008-05-02 EP EP08747561A patent/EP2079464A2/en not_active Withdrawn
- 2008-05-02 JP JP2010506688A patent/JP2010526101A/ja not_active Withdrawn
- 2008-05-02 CA CA002686203A patent/CA2686203A1/en not_active Abandoned
- 2008-05-02 BR BRPI0811476-5A2A patent/BRPI0811476A2/pt not_active IP Right Cessation
- 2008-05-02 WO PCT/US2008/062518 patent/WO2008137753A2/en not_active Ceased
-
2009
- 2009-10-29 IL IL201834A patent/IL201834A0/en unknown
- 2009-10-30 TN TNP2009000451A patent/TN2009000451A1/fr unknown
- 2009-10-30 GT GT200900284A patent/GT200900284A/es unknown
- 2009-11-26 MA MA32377A patent/MA31663B1/fr unknown
- 2009-12-02 EC EC2009009778A patent/ECSP099778A/es unknown
- 2009-12-02 CO CO09137697A patent/CO6241104A2/es not_active Application Discontinuation
-
2011
- 2011-09-16 US US13/235,305 patent/US20120009172A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| US20120009172A1 (en) | 2012-01-12 |
| EA200901473A1 (ru) | 2010-06-30 |
| JP2010526101A (ja) | 2010-07-29 |
| KR20100029746A (ko) | 2010-03-17 |
| IL201834A0 (en) | 2010-06-16 |
| WO2008137753A3 (en) | 2009-02-12 |
| EP2079464A2 (en) | 2009-07-22 |
| CO6241104A2 (es) | 2011-01-20 |
| ECSP099778A (es) | 2010-01-29 |
| US20090048216A1 (en) | 2009-02-19 |
| BRPI0811476A2 (pt) | 2014-11-04 |
| CN101795682A (zh) | 2010-08-04 |
| GT200900284A (es) | 2012-01-31 |
| WO2008137753A2 (en) | 2008-11-13 |
| TN2009000451A1 (en) | 2011-03-31 |
| MX2009011843A (es) | 2010-04-22 |
| MA31663B1 (fr) | 2010-09-01 |
| AU2008247483A1 (en) | 2008-11-13 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |
Effective date: 20140502 |