DK3089979T3 - PYRIMIDINONES AS A FACTOR XIA INHIBITORS - Google Patents

PYRIMIDINONES AS A FACTOR XIA INHIBITORS Download PDF

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Publication number
DK3089979T3
DK3089979T3 DK15747721.7T DK15747721T DK3089979T3 DK 3089979 T3 DK3089979 T3 DK 3089979T3 DK 15747721 T DK15747721 T DK 15747721T DK 3089979 T3 DK3089979 T3 DK 3089979T3
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mmol
pharmaceutically acceptable
independently selected
methyl
chloro
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DK15747721.7T
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Danish (da)
English (en)
Inventor
Andrew K Dilger
James R Corte
Lucca Indawati De
Tianan Fang
Yufeng Wang
Kumar Balashanmuga Pabbisetty
William R Ewing
Yeheng Zhu
Ruth R Wexler
Donald J P Pinto
Michael J Orwat
Ii Leon M Smith
Wu Yang
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Bristol Myers Squibb Co
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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
    • C07D471/18Bridged systems
    • 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
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • A61K31/41621,2-Diazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/61Halogen atoms or nitro radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/34One oxygen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/10Heterocyclic 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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (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)
DK15747721.7T 2014-10-01 2015-07-29 PYRIMIDINONES AS A FACTOR XIA INHIBITORS DK3089979T3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462058316P 2014-10-01 2014-10-01
PCT/US2015/042576 WO2016053455A1 (en) 2014-10-01 2015-07-29 Pyrimidinones as factor xia inhibitors

Publications (1)

Publication Number Publication Date
DK3089979T3 true DK3089979T3 (en) 2018-01-15

Family

ID=53784023

Family Applications (2)

Application Number Title Priority Date Filing Date
DK15747721.7T DK3089979T3 (en) 2014-10-01 2015-07-29 PYRIMIDINONES AS A FACTOR XIA INHIBITORS
DK17189935.4T DK3293186T3 (da) 2014-10-01 2015-07-29 Pyrimidinoner som faktor xia-hæmmere

Family Applications After (1)

Application Number Title Priority Date Filing Date
DK17189935.4T DK3293186T3 (da) 2014-10-01 2015-07-29 Pyrimidinoner som faktor xia-hæmmere

Country Status (34)

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EP (4) EP3089979B1 (enExample)
JP (4) JP6462865B2 (enExample)
KR (2) KR101921436B1 (enExample)
CN (3) CN114957255A (enExample)
AR (1) AR101367A1 (enExample)
AU (3) AU2015324530B2 (enExample)
CA (1) CA2963395C (enExample)
CL (1) CL2017000712A1 (enExample)
CO (1) CO2017003833A2 (enExample)
CY (2) CY1119678T1 (enExample)
DK (2) DK3089979T3 (enExample)
EA (1) EA031590B1 (enExample)
ES (3) ES2655884T3 (enExample)
HR (2) HRP20171950T1 (enExample)
HU (2) HUE038061T2 (enExample)
IL (2) IL251434B (enExample)
LT (2) LT3293186T (enExample)
MA (1) MA40123A1 (enExample)
MX (2) MX376056B (enExample)
MY (2) MY201397A (enExample)
NO (1) NO2721243T3 (enExample)
PE (2) PE20210922A1 (enExample)
PH (2) PH12017500580B1 (enExample)
PL (1) PL3089979T3 (enExample)
PT (2) PT3293186T (enExample)
RS (2) RS56786B1 (enExample)
SG (2) SG10201911652TA (enExample)
SI (2) SI3293186T1 (enExample)
SM (2) SMT202000667T1 (enExample)
TN (2) TN2018000229A1 (enExample)
TW (3) TWI834182B (enExample)
UY (1) UY36244A (enExample)
WO (1) WO2016053455A1 (enExample)
ZA (1) ZA201702478B (enExample)

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NO2721243T3 (enExample) * 2014-10-01 2018-10-20
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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
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JOP20180026A1 (ar) 2017-03-31 2019-01-30 Univ Leuven Kath مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
JOP20180025B1 (ar) 2017-03-31 2021-08-17 Janssen Pharmaceuticals Inc مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
EA039702B1 (ru) 2017-05-22 2022-03-01 Янссен Фармасьютикалз, Инк. Замещенные производные индолина в качестве ингибиторов репликации вирусов денге
EA201992782A1 (ru) 2017-05-22 2020-03-24 Янссен Фармасьютикалз, Инк. Замещенные производные индолина в качестве ингибиторов репликации вирусов денге
EP3953334B1 (en) 2019-04-11 2023-11-22 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
EA202192753A1 (ru) * 2019-04-11 2022-01-11 Бристол-Маерс Сквибб Компани Повышенная эффективность аморфных твердых и солюбилизированных составов для достижения терапевтических концентраций в плазме
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EP4036087A4 (en) * 2019-09-27 2023-09-20 Shenzhen Salubris Pharmaceuticals Co. Ltd Fxia inhibitors and preparation method therefor and pharmaceutical use thereof
IL297206A (en) * 2020-04-10 2022-12-01 Bristol Myers Squibb Co 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
TW202229280A (zh) * 2020-10-12 2022-08-01 美商必治妥美雅史谷比公司 (6r,10s)-10-{4-[5-氯-2-(4-氯-1h-1,2,3-三唑-1-基)苯基]-6-側氧基-1(6h)-嘧啶基}-1-(二氟甲基)-6-甲基-1,4,7,8,9,10-六氫-11,15-(亞甲橋基)吡唑并[4,3-b][1,7]二氮雜環十四炔-5(6h)-酮之製備方法
EP4274854A4 (en) 2021-01-08 2025-03-26 Bristol-Myers Squibb Company Antibodies and antigen binding peptides for factor xia inhibitors and uses thereof
TWI877478B (zh) * 2021-04-21 2025-03-21 大陸商上海美悦生物科技發展有限公司 FXIa抑制劑及其藥物組合物、製備方法和用途
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AU2021245098A1 (en) 2021-10-28
TWI692478B (zh) 2020-05-01
RS61183B1 (sr) 2021-01-29
AU2021245098B2 (en) 2023-11-23
MY183987A (en) 2021-03-17
JP2019069989A (ja) 2019-05-09
ZA201702478B (en) 2019-06-26
MX376056B (es) 2025-03-07
AU2020200376B2 (en) 2021-07-08
CO2017003833A2 (es) 2017-07-11
EP3089979A1 (en) 2016-11-09
TW202310844A (zh) 2023-03-16
RS56786B1 (sr) 2018-04-30
JP6937734B2 (ja) 2021-09-22
TW201613923A (en) 2016-04-16
SMT202000667T1 (it) 2021-01-05
CL2017000712A1 (es) 2017-11-03
CA2963395C (en) 2023-03-14
CN110734435A (zh) 2020-01-31
SMT201800021T1 (it) 2018-03-08
NO2721243T3 (enExample) 2018-10-20
KR20170057431A (ko) 2017-05-24
PL3089979T3 (pl) 2018-02-28
TW202043228A (zh) 2020-12-01
TN2017000112A1 (en) 2018-07-04
AU2015324530A1 (en) 2017-05-18
KR101921436B1 (ko) 2018-11-22
MX2017003695A (es) 2017-05-30
WO2016053455A1 (en) 2016-04-07
IL251434A0 (en) 2017-05-29
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