JP6464176B2 - 芳香族ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環 - Google Patents

芳香族ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環 Download PDF

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JP6464176B2
JP6464176B2 JP2016549277A JP2016549277A JP6464176B2 JP 6464176 B2 JP6464176 B2 JP 6464176B2 JP 2016549277 A JP2016549277 A JP 2016549277A JP 2016549277 A JP2016549277 A JP 2016549277A JP 6464176 B2 JP6464176 B2 JP 6464176B2
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JP2017504641A (ja
JP2017504641A5 (enExample
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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
アンドリュー・ケイ・ディルガー
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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    • 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
    • C07D471/02—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 two hetero rings
    • C07D471/08—Bridged 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
    • A61K31/41—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
    • A61K31/4192—1,2,3-Triazoles
    • 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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • 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
    • 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
    • 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
    • C07D403/06—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 only aliphatic carbon atoms
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Compression Or Coding Systems Of Tv Signals (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
JP2016549277A 2014-01-31 2015-01-30 芳香族ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環 Active JP6464176B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201461933942P 2014-01-31 2014-01-31
US61/933,942 2014-01-31
US201462058293P 2014-10-01 2014-10-01
US62/058,293 2014-10-01
PCT/US2015/013652 WO2015116885A1 (en) 2014-01-31 2015-01-30 Macrocycles with aromatic p2' groups as factor xia inhibitors

Related Child Applications (1)

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JP2019000516A Division JP6630004B2 (ja) 2014-01-31 2019-01-07 芳香族ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環

Publications (3)

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JP2017504641A JP2017504641A (ja) 2017-02-09
JP2017504641A5 JP2017504641A5 (enExample) 2018-03-08
JP6464176B2 true JP6464176B2 (ja) 2019-02-06

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JP2016549277A Active JP6464176B2 (ja) 2014-01-31 2015-01-30 芳香族ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環
JP2016549279A Active JP6505727B2 (ja) 2014-01-31 2015-01-30 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
JP2019000516A Active JP6630004B2 (ja) 2014-01-31 2019-01-07 芳香族ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環
JP2019060181A Active JP6854067B2 (ja) 2014-01-31 2019-03-27 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
JP2021039989A Active JP7325464B2 (ja) 2014-01-31 2021-03-12 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
JP2023125512A Pending JP2023133468A (ja) 2014-01-31 2023-08-01 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
JP2025166031A Pending JP2025185049A (ja) 2014-01-31 2025-10-02 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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JP2016549279A Active JP6505727B2 (ja) 2014-01-31 2015-01-30 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
JP2019000516A Active JP6630004B2 (ja) 2014-01-31 2019-01-07 芳香族ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環
JP2019060181A Active JP6854067B2 (ja) 2014-01-31 2019-03-27 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
JP2021039989A Active JP7325464B2 (ja) 2014-01-31 2021-03-12 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
JP2023125512A Pending JP2023133468A (ja) 2014-01-31 2023-08-01 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
JP2025166031A Pending JP2025185049A (ja) 2014-01-31 2025-10-02 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

Country Status (32)

Country Link
US (2) US20170002006A1 (enExample)
EP (4) EP3392249B1 (enExample)
JP (7) JP6464176B2 (enExample)
KR (3) KR102413453B1 (enExample)
CN (4) CN106132962B (enExample)
AU (5) AU2015210904C1 (enExample)
BR (1) BR112016015717B1 (enExample)
CA (1) CA2937739C (enExample)
CL (1) CL2016001933A1 (enExample)
CY (1) CY1120702T1 (enExample)
DK (1) DK3099687T3 (enExample)
EA (1) EA030222B1 (enExample)
ES (3) ES2687498T3 (enExample)
HR (1) HRP20181339T1 (enExample)
HU (1) HUE040226T2 (enExample)
IL (5) IL298983B2 (enExample)
LT (1) LT3099687T (enExample)
MX (2) MX377545B (enExample)
MY (1) MY190429A (enExample)
NZ (2) NZ723762A (enExample)
PE (2) PE20161069A1 (enExample)
PH (2) PH12016501249B1 (enExample)
PL (1) PL3099687T3 (enExample)
PT (1) PT3099687T (enExample)
RS (1) RS57659B1 (enExample)
SG (2) SG10201908467RA (enExample)
SI (1) SI3099687T1 (enExample)
SM (1) SMT201800505T1 (enExample)
TW (4) TWI688564B (enExample)
UY (3) UY35971A (enExample)
WO (2) WO2015116886A1 (enExample)
ZA (1) ZA201606011B (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Families Citing this family (47)

* Cited by examiner, † Cited by third party
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GB201116559D0 (en) 2011-09-26 2011-11-09 Univ Leuven Kath Novel viral replication inhibitors
CN103974938B (zh) 2011-10-14 2016-11-09 百时美施贵宝公司 作为因子xia抑制剂的经取代的四氢异喹啉化合物
ES2712699T3 (es) 2013-03-25 2019-05-14 Bristol Myers Squibb Co Tetrahidroisoquinolinas que contienen azoles sustituidos como inhibidores del factor XIa
NO2760821T3 (enExample) 2014-01-31 2018-03-10
EP2913330A1 (en) * 2014-02-27 2015-09-02 Laboratoire Biodim Condensed derivatives of imidazole useful as pharmaceuticals
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
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JP6662865B2 (ja) 2014-10-01 2020-03-11 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ ボロン酸誘導体
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
ES2762987T3 (es) 2015-06-19 2020-05-26 Bristol Myers Squibb Co Macrociclos de diamida como inhibidores del factor XIA
JO3703B1 (ar) 2015-07-09 2021-01-31 Bayer Pharma AG مشتقات أوكسوبيريدين مستبدلة
ES2871111T3 (es) 2015-07-29 2021-10-28 Bristol Myers Squibb Co Inhibidores macrocíclicos del factor XIa que contienen un grupo P2' no aromático
KR102086934B1 (ko) * 2015-07-29 2020-03-09 브리스톨-마이어스 스큅 컴퍼니 알킬 또는 시클로알킬 P2' 모이어티를 갖는 인자 XIa 마크로시클릭 억제제
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
AU2016344476B2 (en) * 2015-10-29 2020-08-13 Merck Sharp & Dohme Llc Factor XIa inhibitors
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
KR20180117156A (ko) 2016-03-02 2018-10-26 브리스톨-마이어스 스큅 컴퍼니 인자 XIa 억제 활성을 갖는 디아미드 마크로사이클
CR20180496A (es) 2016-03-31 2018-12-06 Univ Leuven Kath Derivados de indolina sustituidos como inhibidores de la replicación vírica de dengue
WO2017167950A1 (en) 2016-03-31 2017-10-05 Janssen Pharmaceuticals, Inc. Substituted indole derivatives as dengue viral replication inhibitors
CN109069482B (zh) 2016-04-01 2022-04-05 杨森制药公司 作为登革热病毒复制抑制剂的经取代的吲哚化合物衍生物
JOP20170069B1 (ar) 2016-04-01 2021-08-17 1 Janssen Pharmaceuticals Inc مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
AR109304A1 (es) 2016-08-10 2018-11-21 Sumitomo Chemical Co Compuesto de oxadiazol y su uso
WO2018039094A1 (en) 2016-08-22 2018-03-01 Merck Sharp & Dohme Corp. Pyridine-1-oxide derivatives and their use as factor xia inhibitors
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
PE20200342A1 (es) 2017-05-22 2020-02-14 Janssen Pharmaceuticals Inc Derivados de indolina sustituidos como inhibidores de la replicacion virica de dengue
MX393586B (es) 2017-05-22 2025-03-24 Janssen Pharmaceuticals Inc Derivados de indolina sustituidos como inhibidores de la replicacion virica de dengue
WO2019011166A1 (zh) * 2017-07-14 2019-01-17 四川科伦博泰生物医药股份有限公司 大环酰胺化合物及其药物组合物和用途
EA202192807A1 (ru) 2019-04-11 2022-02-24 Бристол-Маерс Сквибб Компани НОВЫЕ СИНТЕТИЧЕСКИЕ ВОЗМОЖНОСТИ ДЛЯ ПРОИЗВОДСТВА (6R,10S)-10-{4-[5-ХЛОРО-2-(4-ХЛОРО-1Н-1,2,3-ТРИАЗОЛ-1-ИЛ)ФЕНИЛ]-6-ОКСО-1(6Н)-ПИРИМИДИНИЛ}-1-(ДИФТОРОМЕТИЛ)-6-МЕТИЛ-1,4,7,8,9,10-ГЕКСАГИДРО-11,15-(МЕТЕНО)ПИРАЗОЛО[4,3-b][1,7]ДИАЗАЦИКЛОТЕТРАДЕЦИН-5(6Н)-ОНА
CA3132530A1 (en) * 2019-04-11 2020-10-15 Robert J. GARMISE Enhanced performance of amorphous solid and solubilized formulations for achieving therapeutic plasma concentrations
EP3957638B1 (en) * 2019-04-16 2025-01-08 China Resources Biopharmaceutical Company Limited Macrocyclic derivatives acting as xia factor inhibitor
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BR112016015717A8 (pt) 2018-05-02
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