MA38071B1 - Formes cristallines d'un inhibiteur de facteur xia - Google Patents

Formes cristallines d'un inhibiteur de facteur xia

Info

Publication number
MA38071B1
MA38071B1 MA38071A MA38071A MA38071B1 MA 38071 B1 MA38071 B1 MA 38071B1 MA 38071 A MA38071 A MA 38071A MA 38071 A MA38071 A MA 38071A MA 38071 B1 MA38071 B1 MA 38071B1
Authority
MA
Morocco
Prior art keywords
crystalline forms
factor xia
xia inhibitor
inhibitor
compositions
Prior art date
Application number
MA38071A
Other languages
English (en)
Other versions
MA38071A1 (fr
Inventor
Marta Dabros
Chenkou Wei
Original Assignee
Bristol Myers Squibb Co
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of MA38071A1 publication Critical patent/MA38071A1/fr
Publication of MA38071B1 publication Critical patent/MA38071B1/fr

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0043Nose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4816Wall or shell material
    • A61K9/4825Proteins, e.g. gelatin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Otolaryngology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Compounds Of Unknown Constitution (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (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.
MA38071A 2012-10-12 2015-05-07 Formes cristallines d'un inhibiteur de facteur xia MA38071B1 (fr)

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 MA38071A1 (fr) 2016-06-30
MA38071B1 true 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)

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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
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
LT2766346T (lt) 2011-10-14 2017-06-12 Bristol-Myers Squibb Company Pakeistieji tetrahidroizochinolino junginiai, kaip faktoriaus xia inhibitoriai
EP2906541B1 (fr) 2012-10-12 2017-11-22 Bristol-Myers Squibb Company Composés de tetrahydroisoquinoline substitués par guanidine et amine en tant qu'inhibiteurs de factor xia
WO2014059202A1 (fr) 2012-10-12 2014-04-17 Bristol-Myers Squibb Company Composés de tétrahydroisoquinoléine substitués par guanidine comme inhibiteurs du facteur xia
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
NO2760821T3 (fr) 2014-01-31 2018-03-10
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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
JP7458984B2 (ja) 2018-03-28 2024-04-01 四川科倫博泰生物医薬股▲フン▼有限公司 テトラヒドロイソキノリン系誘導体、その製造方法及び用途

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Also Published As

Publication number Publication date
PL2906551T3 (pl) 2018-07-31
ES2668318T3 (es) 2018-05-17
EA201590548A1 (ru) 2015-07-30
AU2013329125B2 (en) 2017-03-30
EP2906551B1 (fr) 2018-02-28
KR102143257B1 (ko) 2020-08-10
AU2013329125A1 (en) 2015-05-28
MX2015004328A (es) 2015-06-10
EA032092B1 (ru) 2019-04-30
CL2015000916A1 (es) 2015-08-14
ZA201503238B (en) 2017-11-29
CN104837833A (zh) 2015-08-12
HUE038272T2 (hu) 2018-10-29
KR20150065189A (ko) 2015-06-12
BR112015007937A2 (pt) 2017-07-04
SG11201502605PA (en) 2015-05-28
US9920034B2 (en) 2018-03-20
NO2819265T3 (fr) 2018-07-28
HK1212333A1 (en) 2016-06-10
PT2906551T (pt) 2018-05-10
CA2888100A1 (fr) 2014-04-17
WO2014059203A1 (fr) 2014-04-17
CN104837833B (zh) 2017-07-14
PE20150639A1 (es) 2015-05-11
US20150266855A1 (en) 2015-09-24
JP2015533168A (ja) 2015-11-19
NZ707990A (en) 2018-07-27
LT2906551T (lt) 2018-04-25
MA38071A1 (fr) 2016-06-30
IL238089B (en) 2019-03-31
EP2906551A1 (fr) 2015-08-19
MY173058A (en) 2019-12-23
JP6154473B2 (ja) 2017-06-28
MX351848B (es) 2017-10-31
PH12015500678A1 (en) 2015-05-18
DK2906551T3 (en) 2018-05-22
CO7350621A2 (es) 2015-08-10
RS57039B1 (sr) 2018-05-31
HRP20180465T1 (hr) 2018-05-04
TR201807316T4 (tr) 2018-06-21
SI2906551T1 (en) 2018-05-31
CY1120238T1 (el) 2019-07-10

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