MA38071A1 - Formes cristallines d'un inhibiteur de facteur xia - Google Patents
Formes cristallines d'un inhibiteur de facteur xiaInfo
- Publication number
- MA38071A1 MA38071A1 MA38071A MA38071A MA38071A1 MA 38071 A1 MA38071 A1 MA 38071A1 MA 38071 A MA38071 A MA 38071A MA 38071 A MA38071 A MA 38071A MA 38071 A1 MA38071 A1 MA 38071A1
- Authority
- MA
- Morocco
- Prior art keywords
- crystalline forms
- factor xia
- xia inhibitor
- inhibitor
- compositions
- Prior art date
Links
- 229940122036 Factor XIa inhibitor Drugs 0.000 title 1
- 238000000034 method Methods 0.000 abstract 2
- WYFCZWSWFGJODV-MIANJLSGSA-N 4-[[(1s)-2-[(e)-3-[3-chloro-2-fluoro-6-(tetrazol-1-yl)phenyl]prop-2-enoyl]-5-(4-methyl-2-oxopiperazin-1-yl)-3,4-dihydro-1h-isoquinoline-1-carbonyl]amino]benzoic acid Chemical compound O=C1CN(C)CCN1C1=CC=CC2=C1CCN(C(=O)\C=C\C=1C(=CC=C(Cl)C=1F)N1N=NN=C1)[C@@H]2C(=O)NC1=CC=C(C(O)=O)C=C1 WYFCZWSWFGJODV-MIANJLSGSA-N 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 230000009424 thromboembolic effect Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- 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
- A61K9/0043—Nose
-
- 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
- A61K9/007—Pulmonary tract; Aromatherapy
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4816—Wall or shell material
- A61K9/4825—Proteins, e.g. gelatin
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Otolaryngology (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Compounds Of Unknown Constitution (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La présente invention concerne des formes cristallines de l'acide(s,e)-4-(2-(3-(3-chloro-2-fluoro-6-(1h-tétrazol-1-yl)phényl)acryloyl)-5-(4-méthyl-2-oxopipérazin-1-yl)-1,2,3,4-tétrahydroisoquinoline-1-carboxamido)benzoïque et ses solvates ; des procédés pour la production de telles formes cristallines ; des compositions comportant de telles formes cristallines ; et des procédé de traitement de troubles thromboemboliques avec lesdites formes cristallines ou lesdites compositions pharmaceutiques.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261712850P | 2012-10-12 | 2012-10-12 | |
PCT/US2013/064423 WO2014059203A1 (fr) | 2012-10-12 | 2013-10-11 | Formes cristallines d'un inhibiteur de facteur xia |
Publications (2)
Publication Number | Publication Date |
---|---|
MA38071A1 true MA38071A1 (fr) | 2016-06-30 |
MA38071B1 MA38071B1 (fr) | 2017-01-31 |
Family
ID=49474724
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MA38071A MA38071B1 (fr) | 2012-10-12 | 2015-05-07 | Formes cristallines d'un inhibiteur de facteur xia |
Country Status (34)
Country | Link |
---|---|
US (1) | US9920034B2 (fr) |
EP (1) | EP2906551B1 (fr) |
JP (1) | JP6154473B2 (fr) |
KR (1) | KR102143257B1 (fr) |
CN (1) | CN104837833B (fr) |
AU (1) | AU2013329125B2 (fr) |
BR (1) | BR112015007937A2 (fr) |
CA (1) | CA2888100A1 (fr) |
CL (1) | CL2015000916A1 (fr) |
CO (1) | CO7350621A2 (fr) |
CY (1) | CY1120238T1 (fr) |
DK (1) | DK2906551T3 (fr) |
EA (1) | EA032092B1 (fr) |
ES (1) | ES2668318T3 (fr) |
HK (1) | HK1212333A1 (fr) |
HR (1) | HRP20180465T1 (fr) |
HU (1) | HUE038272T2 (fr) |
IL (1) | IL238089B (fr) |
LT (1) | LT2906551T (fr) |
MA (1) | MA38071B1 (fr) |
MX (1) | MX351848B (fr) |
MY (1) | MY173058A (fr) |
NO (1) | NO2819265T3 (fr) |
NZ (1) | NZ707990A (fr) |
PE (1) | PE20150639A1 (fr) |
PH (1) | PH12015500678A1 (fr) |
PL (1) | PL2906551T3 (fr) |
PT (1) | PT2906551T (fr) |
RS (1) | RS57039B1 (fr) |
SG (1) | SG11201502605PA (fr) |
SI (1) | SI2906551T1 (fr) |
TR (1) | TR201807316T4 (fr) |
WO (1) | WO2014059203A1 (fr) |
ZA (1) | ZA201503238B (fr) |
Families Citing this family (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
CA2851810C (fr) | 2011-10-14 | 2020-01-07 | Bristol-Myers Squibb Company | Composes de tetrahydroisoquinoleine substitues comme inhibiteurs du facteur xia |
EP2906552B1 (fr) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Composés de tetrahydroisoquinoline substitués par guanidine en tant qu'inhibiteurs de factor xia |
US9403774B2 (en) | 2012-10-12 | 2016-08-02 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
JP6479763B2 (ja) | 2013-03-25 | 2019-03-06 | 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置換アゾール含有のテトラヒドロイソキノリン |
WO2015116886A1 (fr) | 2014-01-31 | 2015-08-06 | Bristol-Myers Squibb Company | Macrocycles à groupes hétérocycliques p2' servant d'inhibiteurs du facteur xia |
NO2760821T3 (fr) | 2014-01-31 | 2018-03-10 | ||
WO2016036893A1 (fr) | 2014-09-04 | 2016-03-10 | Bristol-Myers Squibb Company | Diamides macrocycliques qui sont des inhibiteurs de fxia |
US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
WO2016205482A1 (fr) | 2015-06-19 | 2016-12-22 | Bristol-Myers Squibb Company | Macrocycles diamides utilisés en tant qu'inhibiteurs du facteur xia |
EP3328852B1 (fr) | 2015-07-29 | 2021-04-28 | Bristol-Myers Squibb Company | Composés macrocycliques portant un groupe p2' non aromatique en tant qu'inhibiteurs de facteur xia |
ES2803659T3 (es) | 2015-07-29 | 2021-01-28 | Bristol Myers Squibb Co | Inhibidores macrocíclicos del factor xia que contienen restos alquilo o cicloalquilo p2 |
CN106496249B (zh) * | 2015-09-07 | 2019-12-13 | 江苏恒瑞医药股份有限公司 | 噁唑并吲哚类衍生物、其制备方法及其在医药上的应用 |
EP3371162B1 (fr) | 2015-10-29 | 2022-01-26 | Merck Sharp & Dohme Corp. | Dérivé spirocarbamate macrocyclique comme inhibiteurs du facteur xia, compositions pharmaceutiquement acceptables et leur utilisation |
EP3500556B1 (fr) | 2016-08-22 | 2023-08-02 | Merck Sharp & Dohme LLC | Dérivés pyridine-1-oxyde et leur utilisation en tant qu'inhbiteurs du facteur xia |
CN109867660A (zh) * | 2017-12-01 | 2019-06-11 | 四川科伦博泰生物医药股份有限公司 | 含季铵离子的四氢异喹啉酰胺化合物及其药物用途 |
WO2019184744A1 (fr) | 2018-03-28 | 2019-10-03 | 四川科伦博泰生物医药股份有限公司 | Dérivé de tétrahydro-isoquinoline, son procédé de préparation et ses applications |
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WO2006076575A2 (fr) | 2005-01-13 | 2006-07-20 | Bristol-Myers Squibb Company | Composes de biaryle substitue en tant qu'inhibiteurs du facteur xia |
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EP2899183B1 (fr) | 2011-10-14 | 2018-09-19 | Bristol-Myers Squibb Company | Composés de tétrahydroisiquinoline substitués en tant qu'inhibiteurs du facteur Xia |
CA2851810C (fr) * | 2011-10-14 | 2020-01-07 | Bristol-Myers Squibb Company | Composes de tetrahydroisoquinoleine substitues comme inhibiteurs du facteur xia |
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KR20150038369A (ko) | 2012-08-03 | 2015-04-08 | 브리스톨-마이어스 스큅 컴퍼니 | 인자 XIa 억제제로서의 디히드로피리돈 P1 |
CN104507924B (zh) | 2012-08-03 | 2018-01-23 | 百时美施贵宝公司 | 二氢吡啶酮p1作为凝血因子xia抑制剂 |
US9403774B2 (en) | 2012-10-12 | 2016-08-02 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
EP2906552B1 (fr) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Composés de tetrahydroisoquinoline substitués par guanidine en tant qu'inhibiteurs de factor xia |
US9708308B2 (en) | 2012-12-19 | 2017-07-18 | Merck Sharp Dohme Corp. | Factor IXa inhibitors |
GB201300304D0 (en) | 2013-01-08 | 2013-02-20 | Kalvista Pharmaceuticals Ltd | Benzylamine derivatives |
GB2510407A (en) | 2013-02-04 | 2014-08-06 | Kalvista Pharmaceuticals Ltd | Aqueous suspensions of kallikrein inhibitors for parenteral administration |
JP6479763B2 (ja) | 2013-03-25 | 2019-03-06 | 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置換アゾール含有のテトラヒドロイソキノリン |
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