KR102143257B1 - 인자 XIa 억제제의 결정질 형태 - Google Patents

인자 XIa 억제제의 결정질 형태 Download PDF

Info

Publication number
KR102143257B1
KR102143257B1 KR1020157011941A KR20157011941A KR102143257B1 KR 102143257 B1 KR102143257 B1 KR 102143257B1 KR 1020157011941 A KR1020157011941 A KR 1020157011941A KR 20157011941 A KR20157011941 A KR 20157011941A KR 102143257 B1 KR102143257 B1 KR 102143257B1
Authority
KR
South Korea
Prior art keywords
compound
crystalline form
crystalline
methyl
tetrahydroisoquinoline
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.)
Expired - Fee Related
Application number
KR1020157011941A
Other languages
English (en)
Korean (ko)
Other versions
KR20150065189A (ko
Inventor
마르타 다브로스
첸코우 웨이
Original Assignee
브리스톨-마이어스 스큅 컴퍼니
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 브리스톨-마이어스 스큅 컴퍼니 filed Critical 브리스톨-마이어스 스큅 컴퍼니
Publication of KR20150065189A publication Critical patent/KR20150065189A/ko
Application granted granted Critical
Publication of KR102143257B1 publication Critical patent/KR102143257B1/ko
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical 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)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Otolaryngology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Hematology (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)
KR1020157011941A 2012-10-12 2013-10-11 인자 XIa 억제제의 결정질 형태 Expired - Fee Related KR102143257B1 (ko)

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 (2)

Publication Number Publication Date
KR20150065189A KR20150065189A (ko) 2015-06-12
KR102143257B1 true KR102143257B1 (ko) 2020-08-10

Family

ID=49474724

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020157011941A Expired - Fee Related KR102143257B1 (ko) 2012-10-12 2013-10-11 인자 XIa 억제제의 결정질 형태

Country Status (34)

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

Families Citing this family (18)

* Cited by examiner, † Cited by third party
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
PH12014500625B1 (en) 2011-10-14 2018-12-12 Bristol Myers Squibb Co Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
EP2906541B1 (en) 2012-10-12 2017-11-22 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
WO2014059202A1 (en) 2012-10-12 2014-04-17 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
WO2014160668A1 (en) 2013-03-25 2014-10-02 Bristol-Myers Squibb Company Tetrahydroisoquinolines containing substituted azoles as factor xia inhibitors
SG10201908467RA (en) 2014-01-31 2019-10-30 Bristol Myers Squibb Co Macrocycles with hetrocyclic p2' groups as factor xia inhibitors
NO2760821T3 (enExample) 2014-01-31 2018-03-10
WO2016036893A1 (en) 2014-09-04 2016-03-10 Bristol-Myers Squibb Company Diamide macrocycles that are fxia inhibitors
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
US10160750B2 (en) 2015-06-19 2018-12-25 Bristol-Myers Squibb Company Diamide macrocycles as factor XIa inhibitors
CN107849026B (zh) 2015-07-29 2021-01-01 百时美施贵宝公司 携带烷基或环烷基p2′部分的因子xia大环抑制剂
KR102729666B1 (ko) 2015-07-29 2024-11-12 브리스톨-마이어스 스큅 컴퍼니 비-방향족 P2' 기를 갖는 인자 XIa 신규 마크로사이클
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 (en) 2015-10-29 2022-01-26 Merck Sharp & Dohme Corp. Macrocyclic spirocarbamate derivatives as factor xia inhibitors, pharmaceutically acceptable compositions and their use
WO2018039094A1 (en) 2016-08-22 2018-03-01 Merck Sharp & Dohme Corp. Pyridine-1-oxide derivatives and their use as factor xia inhibitors
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
EP3778597B1 (en) 2018-03-28 2025-05-28 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Tetrahydroisoquinoline derivative, preparation method therefor and uses thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007054453A2 (en) 2005-11-11 2007-05-18 F. Hoffmann-La Roche Ag Carbocyclic fused cyclic amines as inhibitors of the coagulation factor xa
KR101937514B1 (ko) 2011-10-14 2019-01-10 브리스톨-마이어스 스큅 컴퍼니 인자 xia 억제제로서의 치환된 테트라히드로이소퀴놀린 화합물

Family Cites Families (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR7155E (fr) 1906-03-16 1907-05-23 Rene Gabriel Poncet Séchoir rotatif
FR1525186A (fr) 1967-03-29 1968-05-17 Roussel Uclaf Nouvelles pénicillines et procédé de préparation
ATA937274A (de) 1973-12-17 1978-02-15 Thomae Gmbh Dr K Verfahren zur herstellung neuer araliphatischer ketone
DE4034829A1 (de) 1990-11-02 1992-05-07 Merck Patent Gmbh Cyclopeptide
JP3190431B2 (ja) 1991-07-01 2001-07-23 三菱化学株式会社 ケトン誘導体
GB9206757D0 (en) 1992-03-27 1992-05-13 Ferring Bv Novel peptide receptor ligands
WO1996034010A2 (en) 1995-03-29 1996-10-31 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5624936A (en) 1995-03-29 1997-04-29 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5869682A (en) 1996-04-03 1999-02-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
EP0891352A4 (en) 1996-04-03 2001-08-16 Merck & Co Inc INHIBITORS OF FARNESYL PROTEIN TRANSFERASE
TW557297B (en) 1997-09-26 2003-10-11 Abbott Lab Rapamycin analogs having immunomodulatory activity, and pharmaceutical compositions containing same
TR200103406T2 (tr) 1998-03-19 2002-06-21 Vertex Pharmaceuticals Incorporated Kaspaz inhibitörleri.
SK17532000A3 (sk) 1998-05-26 2002-08-06 Warner-Lambert Company Prípadne substituované 3,4-dihydrogenované pyrimidíny, ich použitie a farmaceutické formulácie na ich báze
US6307049B1 (en) 1998-09-30 2001-10-23 The Procter & Gamble Co. Heterocyclic 2-substituted ketoamides
CA2358578A1 (en) 1999-01-02 2000-07-13 Aventis Pharma Deutschland Gmbh Novel malonic acid derivatives, processes for their preparation, their use and pharmaceutical compositions containing them (inhibition of factor xa activity)
EP1016663A1 (en) 1999-01-02 2000-07-05 Aventis Pharma Deutschland GmbH Novel malonic acid derivatives, processes for their preparation, their use and pharmaceutical compositions containing them (inhibition of factor Xa activity)
HK1045846A1 (zh) 1999-04-09 2002-12-13 巴斯福股份公司 低分子量补体蛋白酶抑制剂
EP1125925A1 (en) 2000-02-15 2001-08-22 Applied Research Systems ARS Holding N.V. Amine derivatives for the treatment of apoptosis
ATE310728T1 (de) 2000-05-11 2005-12-15 Bristol Myers Squibb Co Tetrahydroisochinolin-analoga als wachstumshormon-sekretagoga
SV2003000617A (es) 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
WO2003011222A2 (en) 2001-07-27 2003-02-13 Merck & Co., Inc. Thrombin inhibitors
US6649606B1 (en) 2001-11-09 2003-11-18 Bristol-Myers Squibb Co. Tetrahydroisoquinoline analogs as modulators of chemokine receptor activity
US7138412B2 (en) 2003-03-11 2006-11-21 Bristol-Myers Squibb Company Tetrahydroquinoline derivatives useful as serine protease inhibitors
US7129264B2 (en) 2003-04-16 2006-10-31 Bristol-Myers Squibb Company Biarylmethyl indolines and indoles as antithromboembolic agents
JP2007501844A (ja) 2003-08-08 2007-02-01 トランス　テック　ファーマ，インコーポレイテッド アリール及びヘテロアリール化合物、組成物並びに使用方法
US7417063B2 (en) 2004-04-13 2008-08-26 Bristol-Myers Squibb Company Bicyclic heterocycles useful as serine protease inhibitors
US7453002B2 (en) 2004-06-15 2008-11-18 Bristol-Myers Squibb Company Five-membered heterocycles useful as serine protease inhibitors
US7429604B2 (en) 2004-06-15 2008-09-30 Bristol Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
EP2457895A1 (en) 2004-07-12 2012-05-30 Idun Pharmaceuticals, Inc. Tetrapeptide analogs
EP1841504B1 (en) 2005-01-13 2014-11-19 Bristol-Myers Squibb Company Substituted biaryl compounds as factor xia inhibitors
WO2006089005A2 (en) 2005-02-17 2006-08-24 Bristol-Myers Squibb Company Combination of selective factor viia and/or xia and plasma kallikrein inhibitors
JP2009519966A (ja) 2005-12-14 2009-05-21 ブリストル−マイヤーズ スクイブ カンパニー セリンプロテアーゼ阻害剤として有用な６員ヘテロ環
WO2007070816A2 (en) 2005-12-14 2007-06-21 Bristol-Myers Squibb Company Thiophene derivatives as factor xia inhibitors
EA014245B1 (ru) 2005-12-14 2010-10-29 Бристол-Маерс Сквибб Компани Аналоги арилпропионамида, арилакриламида, арилпропинамида или арилметилмочевины в качестве ингибиторов фактора xia
AR058380A1 (es) 2005-12-23 2008-01-30 Bristol Myers Squibb Co Inhibidores del factor viia macrociclicos utiles como anticoagulantes
ES2546815T3 (es) 2006-12-15 2015-09-28 Bristol-Myers Squibb Company Análogos de arilpropilamida, arilacrilamida, arilpropinamida o arilmetilurea como inhibidores del factor XIa
PE20081775A1 (es) 2006-12-20 2008-12-18 Bristol Myers Squibb Co Compuestos macrociclicos como inhibidores del factor viia
PE20091002A1 (es) 2007-06-13 2009-07-15 Bristol Myers Squibb Co Analogos dipeptidos como inhibidores del factor de coagulacion
WO2009114677A1 (en) * 2008-03-13 2009-09-17 Bristol-Myers Squibb Company Pyridazine derivatives as factor xia inhibitors
WO2010151317A1 (en) 2009-06-22 2010-12-29 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
WO2011002520A2 (en) 2009-07-02 2011-01-06 Angion Biomedica Corp. Small molecule inhibitors of parp activity
AR077695A1 (es) 2009-08-04 2011-09-14 Schering Corp Derivados de pirimidina como inhibidores del factor ixa
WO2011100401A1 (en) 2010-02-11 2011-08-18 Bristol-Myers Squibb Company Macrocycles as factor xia inhibitors
US9161924B2 (en) 2011-07-08 2015-10-20 Merck Sharp & Dohme Corp. Factor IXa inhibitors
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
CN103987696B (zh) 2011-10-14 2016-12-21 百时美施贵宝公司 作为因子xia抑制剂的取代的四氢异喹啉化合物
CN103987697B (zh) 2011-10-14 2017-04-26 百时美施贵宝公司 作为因子xia抑制剂的取代的四氢异喹啉化合物
IN2014CN04676A (enExample) 2011-12-21 2015-09-18 Ono Pharmaceutical Co
WO2013111108A1 (en) 2012-01-27 2013-08-01 Novartis Ag 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
EP2807156A1 (en) 2012-01-27 2014-12-03 Novartis AG Aminopyridine derivatives as plasma kallikrein inhibitors
JP2015083542A (ja) 2012-02-08 2015-04-30 大日本住友製薬株式会社 ３位置換プロリン誘導体
CA2872926C (en) 2012-05-10 2022-07-05 Bayer Pharma Aktiengesellschaft Antibodies capable of binding to the coagulation factor xi and/or its activated form factor xia and uses thereof
GB201209138D0 (en) 2012-05-24 2012-07-04 Ono Pharmaceutical Co Compounds
US9758480B2 (en) 2012-07-19 2017-09-12 Sumitomo Dainippon Pharma Co., Ltd. 1-(cycloalkyl-carbonyl)proline derivative
HRP20161378T1 (hr) 2012-08-03 2016-12-02 Bristol-Myers Squibb Company Dihidropiridon kao faktor xia inhibitora
HUE032622T2 (en) 2012-08-03 2017-10-30 Bristol Myers Squibb Co Dihydropyridone p1 as factor xia inhibitors
EP2906541B1 (en) 2012-10-12 2017-11-22 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
WO2014059202A1 (en) 2012-10-12 2014-04-17 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
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
WO2014160668A1 (en) 2013-03-25 2014-10-02 Bristol-Myers Squibb Company Tetrahydroisoquinolines containing substituted azoles as factor xia inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007054453A2 (en) 2005-11-11 2007-05-18 F. Hoffmann-La Roche Ag Carbocyclic fused cyclic amines as inhibitors of the coagulation factor xa
KR101937514B1 (ko) 2011-10-14 2019-01-10 브리스톨-마이어스 스큅 컴퍼니 인자 xia 억제제로서의 치환된 테트라히드로이소퀴놀린 화합물

Also Published As

Publication number Publication date
JP6154473B2 (ja) 2017-06-28
US9920034B2 (en) 2018-03-20
AU2013329125B2 (en) 2017-03-30
CN104837833A (zh) 2015-08-12
AU2013329125A1 (en) 2015-05-28
EP2906551A1 (en) 2015-08-19
CL2015000916A1 (es) 2015-08-14
PH12015500678A1 (en) 2015-05-18
WO2014059203A1 (en) 2014-04-17
CA2888100A1 (en) 2014-04-17
MX2015004328A (es) 2015-06-10
SG11201502605PA (en) 2015-05-28
US20150266855A1 (en) 2015-09-24
SI2906551T1 (en) 2018-05-31
JP2015533168A (ja) 2015-11-19
HK1212333A1 (en) 2016-06-10
PT2906551T (pt) 2018-05-10
TR201807316T4 (tr) 2018-06-21
MX351848B (es) 2017-10-31
RS57039B1 (sr) 2018-05-31
EA201590548A1 (ru) 2015-07-30
HRP20180465T1 (hr) 2018-05-04
MA38071B1 (fr) 2017-01-31
EP2906551B1 (en) 2018-02-28
NZ707990A (en) 2018-07-27
CO7350621A2 (es) 2015-08-10
NO2819265T3 (enExample) 2018-07-28
PE20150639A1 (es) 2015-05-11
CN104837833B (zh) 2017-07-14
MY173058A (en) 2019-12-23
SMT201800262T1 (it) 2018-07-17
ZA201503238B (en) 2017-11-29
ES2668318T3 (es) 2018-05-17
BR112015007937A2 (pt) 2017-07-04
PL2906551T3 (pl) 2018-07-31
KR20150065189A (ko) 2015-06-12
IL238089B (en) 2019-03-31
MA38071A1 (fr) 2016-06-30
HUE038272T2 (hu) 2018-10-29
EA032092B1 (ru) 2019-04-30
DK2906551T3 (en) 2018-05-22
CY1120238T1 (el) 2019-07-10
LT2906551T (lt) 2018-04-25

Similar Documents

Publication Publication Date Title
KR102143257B1 (ko) 인자 XIa 억제제의 결정질 형태
JP2019135258A (ja) 第Ｘａ因子阻害剤の結晶形態
EP2138482A1 (en) Bicyclic heterocyclic compound
JP2023521411A (ja) （９ｒ，１３ｓ）－１３－｛４－［５－クロロ－２－（４－クロロ－１ｈ－１，２，３－トリアゾール－１－イル）フェニル］－６－オキソ－１，６－ジヒドロピリミジン－１－イル｝－３－（ジフルオロメチル）－９－メチル－３，４，７，１５－テトラアザトリシクロ［１２．３．１．０２，６］オクタデカ－１（１８），２（６），４，１４，１６－ペンタエン－８－オンの結晶体
US20080188517A1 (en) Crystalline forms of a factor xa inhibitor
JP4177663B2 (ja) 新規な結晶形のＸａ因子阻害剤
JP5796872B2 (ja) 第Ｘａ因子阻害剤の結晶性塩
US7388096B2 (en) Crystalline forms of a factor Xa inhibitor
HK1212333B (en) Crystalline forms of a factor xia inhibitor

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

R18-X000 Changes to party contact information recorded

St.27 status event code: A-3-3-R10-R18-oth-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

P22-X000 Classification modified

St.27 status event code: A-2-2-P10-P22-nap-X000

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

R18-X000 Changes to party contact information recorded

St.27 status event code: A-5-5-R10-R18-oth-X000

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 4

PC1903 Unpaid annual fee

St.27 status event code: A-4-4-U10-U13-oth-PC1903

Not in force date: 20240805

Payment event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

PC1903 Unpaid annual fee

St.27 status event code: N-4-6-H10-H13-oth-PC1903

Ip right cessation event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

Not in force date: 20240805