JP6462865B2 - 第ｘｉａ因子阻害剤としてのピリミジノン - Google Patents

第ｘｉａ因子阻害剤としてのピリミジノン Download PDF

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JP6462865B2
JP6462865B2 JP2017517766A JP2017517766A JP6462865B2 JP 6462865 B2 JP6462865 B2 JP 6462865B2 JP 2017517766 A JP2017517766 A JP 2017517766A JP 2017517766 A JP2017517766 A JP 2017517766A JP 6462865 B2 JP6462865 B2 JP 6462865B2
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mmol
pharmaceutically acceptable
methyl
chloro
tautomer
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JP2017530157A (ja
Inventor
アンドリュー・ケイ・ディルガー
ジェイムズ・アール・コート
インダワティ・デ・ルッカ
ファン・ティアナン
ウー・ヤン
ワン・ユーフェン
クマール・バラシャンムガ・パビセッティ
ウィリアム・アール・ユーイング
イェヘン・ジュー
ルース・アール・ウェクスラー
ドナルド・ジェイ・ピー・ピント
マイケル・ジェイ・オーワット
レオン・エム・スミス・ザ・セカンド
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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
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/18—Bridged systems
    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/61—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2017517766A 2014-10-01 2015-07-29 第ｘｉａ因子阻害剤としてのピリミジノン Active JP6462865B2 (ja)

Priority Applications (1)

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JP2018244086A JP6937734B2 (ja) 2014-10-01 2018-12-27 第ｘｉａ因子阻害剤としてのピリミジノン

Applications Claiming Priority (3)

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US201462058316P 2014-10-01 2014-10-01
US62/058,316 2014-10-01
PCT/US2015/042576 WO2016053455A1 (en) 2014-10-01 2015-07-29 Pyrimidinones as factor xia inhibitors

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JP2017530157A JP2017530157A (ja) 2017-10-12
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JP2018244086A Active JP6937734B2 (ja) 2014-10-01 2018-12-27 第ｘｉａ因子阻害剤としてのピリミジノン
JP2021140618A Active JP7317905B2 (ja) 2014-10-01 2021-08-31 第ｘｉａ因子阻害剤としてのピリミジノン
JP2023117409A Pending JP2023134734A (ja) 2014-10-01 2023-07-19 第ｘｉａ因子阻害剤としてのピリミジノン

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JP2023117409A Pending JP2023134734A (ja) 2014-10-01 2023-07-19 第ｘｉａ因子阻害剤としてのピリミジノン

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JP (4) JP6462865B2 (enExample)
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Cited By (3)

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JP2018525368A (ja) * 2015-07-29 2018-09-06 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ アルキルまたはシクロアルキルＰ２’基を担持する大員環の第ＸＩａ因子阻害剤
JP2019069989A (ja) * 2014-10-01 2019-05-09 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ピリミジノン
JP2019094354A (ja) * 2014-01-31 2019-06-20 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ヘテロ環式ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環

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JP6526796B2 (ja) 2014-09-04 2019-06-05 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｆｘｉａ阻害剤であるジアミドマクロ環
AU2015327345B9 (en) 2014-10-01 2020-06-18 Merck Patent Gmbh Boronic acid derivatives
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
JOP20160086B1 (ar) 2015-05-08 2021-08-17 2 Katholieke Univ Leuven Ku Leuven Research And Development مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
US10160750B2 (en) 2015-06-19 2018-12-25 Bristol-Myers Squibb Company Diamide macrocycles as factor XIa inhibitors
ES2871111T3 (es) 2015-07-29 2021-10-28 Bristol Myers Squibb Co Inhibidores macrocíclicos del factor XIa que contienen un grupo P2' no aromático
JOP20160198B1 (ar) 2015-09-16 2022-03-14 Janssen Pharmaceuticals Inc مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
JO3633B1 (ar) 2015-09-16 2020-08-27 Katholieke Univ Leuven Ku Leuven Research & Development مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
CN109195973A (zh) 2016-03-02 2019-01-11 百时美施贵宝公司 具有因子xia抑制活性的二酰胺大环类化合物
WO2017167953A1 (en) 2016-03-31 2017-10-05 Janssen Pharmaceuticals, Inc. Substituted indoline derivatives as dengue viral replication inhibitors
HRP20210847T1 (hr) 2016-03-31 2021-07-23 Janssen Pharmaceuticals, Inc. Supstituirani derivati indola kao inhibitori replikacije denga virusa
JOP20170069B1 (ar) 2016-04-01 2021-08-17 1 Janssen Pharmaceuticals Inc مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
EA201892200A1 (ru) 2016-04-01 2019-03-29 Янссен Фармасьютикалз, Инк. Замещенные производные соединений индола в качестве ингибиторов репликации вирусов денге
CN110062757B (zh) * 2017-01-18 2022-03-04 广东东阳光药业有限公司 凝血因子XIa抑制剂及其用途
JOP20180025B1 (ar) 2017-03-31 2021-08-17 Janssen Pharmaceuticals Inc مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
JOP20180026A1 (ar) 2017-03-31 2019-01-30 Univ Leuven Kath مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
CA3060583C (en) 2017-05-22 2024-06-04 Janssen Pharmaceuticals, Inc. Substituted indoline derivatives as dengue viral replication inhibitors
CR20190531A (es) 2017-05-22 2020-03-05 Janssen Pharmaceuticals Inc Derivados de indolina sustituidos como inhibidores de la replicación vírica de dengue
EP4234555A3 (en) * 2019-04-11 2024-01-03 Bristol-Myers Squibb Company Novel synthetic options towards the manufacture of (6r,10s)-10- {4-[5-chloro-2-(4-chloro-1h-1,2,3-triazol-1-yl)phenyl]-6-oxo-1(6h)- pyrimidinyl}- 1-(difluoromethyl)-6-methyl-1,4,7,8,9,10-hexahydro-11,15 -(metheno)pyrazolo [4,3-b] [1,7] diazacyclotetradecin-5(6h)-one
KR20210151183A (ko) * 2019-04-11 2021-12-13 브리스톨-마이어스 스큅 컴퍼니 치료 혈장 농도를 달성하기 위한 무정형 고체 및 가용화된 제제의 증진된 성능
CN113677682B (zh) * 2019-04-16 2023-05-30 华润生物医药有限公司 作为XIa因子抑制剂的大环衍生物
WO2021013209A1 (zh) 2019-07-23 2021-01-28 南京明德新药研发有限公司 作为XIa因子抑制剂的大环衍生物
EP4036087A4 (en) * 2019-09-27 2023-09-20 Shenzhen Salubris Pharmaceuticals Co. Ltd FXA INHIBITORS AND METHODS OF PRODUCTION THEREOF AND PHARMACEUTICAL USE THEREOF
PH12022551160A1 (en) 2019-11-15 2023-09-25 Janssen Pharmaceuticals Inc Treatment and prevention of dengue disease
WO2021207659A1 (en) * 2020-04-10 2021-10-14 Bristol-Myers Squibb Company Crystalline forms of (9r, 135s)-13- {4-[5-chloro-2-(4-chloro-1h,2,3- triazol- 1 -yl)phenyl] -6-oxo- 1,6-dihydropyrimidin- 1-yl}-3-(difluoromethyl)-9-methyl-3,4,7,15- tetraazatricyclo [ 12.3.1.02·6] octadeca- 1(18), 2(6), 4, 14, 16-pentaen-8-one
CN119552111B (zh) * 2020-07-29 2026-01-02 上海柯君医药科技有限公司 抗血小板药物和其用途
EP4225757A1 (en) * 2020-10-12 2023-08-16 Bristol-Myers Squibb Company A process toward the manufacture of (6r,10s)-10-{4-[5-chloro-2-(4-chloro-1h-1,2,3-triazol-1-yl)phenyl]-6-oxo-1(6h)-pyrimidinyl}-1-(difluoromethyl)-6-methyl-1,4,7,8,9,10-hexahydro-11,15-(metheno)pyrazolo[4,3-b] [1,7]diazacyclotetradecin-5(6h)-one
TW202241964A (zh) * 2021-01-08 2022-11-01 美商必治妥美雅史谷比公司 因子xia抑制劑之抗體及抗原結合肽及其用途
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TW202515882A (zh) * 2023-06-30 2025-04-16 大陸商深圳信立泰藥業股份有限公司 一種多取代的大環化合物及其製備方法與應用
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JP2019094354A (ja) * 2014-01-31 2019-06-20 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ヘテロ環式ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環
JP2021088610A (ja) * 2014-01-31 2021-06-10 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ヘテロ環式ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環
JP7325464B2 (ja) 2014-01-31 2023-08-14 ブリストル－マイヤーズ スクイブ カンパニー ヘテロ環式ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環
JP2023133468A (ja) * 2014-01-31 2023-09-22 ブリストル－マイヤーズ スクイブ カンパニー ヘテロ環式ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環
JP2019069989A (ja) * 2014-10-01 2019-05-09 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ピリミジノン
JP2021185182A (ja) * 2014-10-01 2021-12-09 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ピリミジノン
JP7317905B2 (ja) 2014-10-01 2023-07-31 ブリストル－マイヤーズ スクイブ カンパニー 第ｘｉａ因子阻害剤としてのピリミジノン
JP2018525368A (ja) * 2015-07-29 2018-09-06 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ アルキルまたはシクロアルキルＰ２’基を担持する大員環の第ＸＩａ因子阻害剤

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