JP6154473B2 - 第ＸＩａ因子阻害剤の結晶形 - Google Patents

第ＸＩａ因子阻害剤の結晶形 Download PDF

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Publication number
JP6154473B2
JP6154473B2 JP2015536906A JP2015536906A JP6154473B2 JP 6154473 B2 JP6154473 B2 JP 6154473B2 JP 2015536906 A JP2015536906 A JP 2015536906A JP 2015536906 A JP2015536906 A JP 2015536906A JP 6154473 B2 JP6154473 B2 JP 6154473B2
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Prior art keywords
crystals
tetrahydroisoquinoline
acryloyl
methyl
fluoro
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Expired - Fee Related
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Japanese (ja)
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JP2015533168A5 (OSRAM
JP2015533168A (ja
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マルタ・ダブロス
チェンコウ・ウェイ
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Hematology (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)
JP2015536906A 2012-10-12 2013-10-11 第ＸＩａ因子阻害剤の結晶形 Expired - Fee Related JP6154473B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261712850P 2012-10-12 2012-10-12
US61/712,850 2012-10-12
PCT/US2013/064423 WO2014059203A1 (en) 2012-10-12 2013-10-11 Crystalline forms of a factor xia inhibitor

Publications (3)

Publication Number Publication Date
JP2015533168A JP2015533168A (ja) 2015-11-19
JP2015533168A5 JP2015533168A5 (OSRAM) 2016-07-07
JP6154473B2 true JP6154473B2 (ja) 2017-06-28

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JP2015536906A Expired - Fee Related JP6154473B2 (ja) 2012-10-12 2013-10-11 第ＸＩａ因子阻害剤の結晶形

Country Status (34)

Country Link
US (1) US9920034B2 (OSRAM)
EP (1) EP2906551B1 (OSRAM)
JP (1) JP6154473B2 (OSRAM)
KR (1) KR102143257B1 (OSRAM)
CN (1) CN104837833B (OSRAM)
AU (1) AU2013329125B2 (OSRAM)
BR (1) BR112015007937A2 (OSRAM)
CA (1) CA2888100A1 (OSRAM)
CL (1) CL2015000916A1 (OSRAM)
CO (1) CO7350621A2 (OSRAM)
CY (1) CY1120238T1 (OSRAM)
DK (1) DK2906551T3 (OSRAM)
EA (1) EA032092B1 (OSRAM)
ES (1) ES2668318T3 (OSRAM)
HR (1) HRP20180465T1 (OSRAM)
HU (1) HUE038272T2 (OSRAM)
IL (1) IL238089B (OSRAM)
LT (1) LT2906551T (OSRAM)
MA (1) MA38071B1 (OSRAM)
MX (1) MX351848B (OSRAM)
MY (1) MY173058A (OSRAM)
NO (1) NO2819265T3 (OSRAM)
NZ (1) NZ707990A (OSRAM)
PE (1) PE20150639A1 (OSRAM)
PH (1) PH12015500678A1 (OSRAM)
PL (1) PL2906551T3 (OSRAM)
PT (1) PT2906551T (OSRAM)
RS (1) RS57039B1 (OSRAM)
SG (1) SG11201502605PA (OSRAM)
SI (1) SI2906551T1 (OSRAM)
SM (1) SMT201800262T1 (OSRAM)
TR (1) TR201807316T4 (OSRAM)
WO (1) WO2014059203A1 (OSRAM)
ZA (1) ZA201503238B (OSRAM)

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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
RS56168B1 (sr) 2011-10-14 2017-11-30 Bristol Myers Squibb Co Supstituisana jedinjenja tetrahidroizohinolina kao inhibitori xia faktora
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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 (zh) 2018-03-28 2019-10-03 四川科伦博泰生物医药股份有限公司 四氢异喹啉类衍生物及其制备方法和用途

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PH12015500678A1 (en) 2015-05-18
TR201807316T4 (tr) 2018-06-21
PL2906551T3 (pl) 2018-07-31
US20150266855A1 (en) 2015-09-24
CA2888100A1 (en) 2014-04-17
CN104837833A (zh) 2015-08-12
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