PE20231071A1 - Formas cristalinas de (9r,13s)-13-{4-[5-cloro-2-(4-cloro-1h-1,2,3-triazol-1- il)fenil]-6-oxo-1,6-dihidropirimidin-1-il}-3-(difluorometil)-9-metil-3,4,7,15- tetraazatriciclo[12.3.1.02,6]octadeca-1(18),2(6),4,14,16-pentaen-8-ona - Google Patents

Formas cristalinas de (9r,13s)-13-{4-[5-cloro-2-(4-cloro-1h-1,2,3-triazol-1- il)fenil]-6-oxo-1,6-dihidropirimidin-1-il}-3-(difluorometil)-9-metil-3,4,7,15- tetraazatriciclo[12.3.1.02,6]octadeca-1(18),2(6),4,14,16-pentaen-8-ona

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Publication number
PE20231071A1
PE20231071A1 PE2022002222A PE2022002222A PE20231071A1 PE 20231071 A1 PE20231071 A1 PE 20231071A1 PE 2022002222 A PE2022002222 A PE 2022002222A PE 2022002222 A PE2022002222 A PE 2022002222A PE 20231071 A1 PE20231071 A1 PE 20231071A1
Authority
PE
Peru
Prior art keywords
chloro
crystalline forms
forms
tetraazatricyclo
pentaen
Prior art date
Application number
PE2022002222A
Other languages
English (en)
Inventor
Andrew K Dilger
Michael A Galella
Daniel Smith
Theresa M Ziemba
David Ludeker
Christos Xiouras
Dipali Ahuja
Dirk Angelina J Cleeren
Original Assignee
Bristol Myers Squibb Co
Janssen Pharmaceutica Nv
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 Bristol Myers Squibb Co, Janssen Pharmaceutica Nv filed Critical Bristol Myers Squibb Co
Publication of PE20231071A1 publication Critical patent/PE20231071A1/es

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Classifications

    • 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
    • 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
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Abstract

Refiere a formas cristalinas del compuesto (I), las cuales se seleccionan de las formas A, B, C, D, E, F, G, H, I y J. Dichas formas se caracterizan por presentar al menos un patron de difraccion de rayos X en polvo, que comprende uno o mas valores 2? seleccionados de 5.0±0.2, 24.5±0.2, entre otros, o aquellos observados sustancialmente en las figuras 1A, 5A, 6A, 7A, 8A, 9A, 10A, 11A, 12 y 13A; un espectro infrarrojo (IR), que tiene uno o mas picos seleccionados de 1678+-2, 1610+-2, entre otros, o aquellos de las figuras 1B, 5B, 6B, 7B, 8B, 9B, 10B, 11B y 13B; un termograma de calorimetria de barrido diferencial (DSC) con una temperatura de inicio de 266°C, un termograma de analisis termogravimetrico (TGA) y una isoterma de sorcion dinamica de vapor (DVS). Asimismo, refiere a una composicion farmaceutica a base de dichas formas cristalinas de formula (I), un portador o diluyente farmaceuticamente aceptables; y a la utilidad de dichas formas cristalinas como agentes anti-tromboembolicos en el tratamiento de enfermedades cardiovasculares.
PE2022002222A 2020-04-10 2021-04-09 Formas cristalinas de (9r,13s)-13-{4-[5-cloro-2-(4-cloro-1h-1,2,3-triazol-1- il)fenil]-6-oxo-1,6-dihidropirimidin-1-il}-3-(difluorometil)-9-metil-3,4,7,15- tetraazatriciclo[12.3.1.02,6]octadeca-1(18),2(6),4,14,16-pentaen-8-ona PE20231071A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202063008161P 2020-04-10 2020-04-10
PCT/US2021/026663 WO2021207659A1 (en) 2020-04-10 2021-04-09 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

Publications (1)

Publication Number Publication Date
PE20231071A1 true PE20231071A1 (es) 2023-07-17

Family

ID=75690727

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2022002222A PE20231071A1 (es) 2020-04-10 2021-04-09 Formas cristalinas de (9r,13s)-13-{4-[5-cloro-2-(4-cloro-1h-1,2,3-triazol-1- il)fenil]-6-oxo-1,6-dihidropirimidin-1-il}-3-(difluorometil)-9-metil-3,4,7,15- tetraazatriciclo[12.3.1.02,6]octadeca-1(18),2(6),4,14,16-pentaen-8-ona

Country Status (14)

Country Link
US (1) US20230151010A1 (es)
EP (1) EP4132930A1 (es)
JP (1) JP2023521411A (es)
KR (1) KR20230008742A (es)
CN (1) CN115916780A (es)
AU (1) AU2021253946A1 (es)
BR (1) BR112022020243A2 (es)
CA (1) CA3179957A1 (es)
CL (1) CL2022002786A1 (es)
CO (1) CO2022016067A2 (es)
IL (1) IL297206A (es)
MX (1) MX2022012523A (es)
PE (1) PE20231071A1 (es)
WO (1) WO2021207659A1 (es)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024030409A1 (en) 2022-08-01 2024-02-08 Bristol-Myers Squibb Company Use of milvexian for treating or preventing ischemic stroke

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NO2721243T3 (es) * 2014-10-01 2018-10-20
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors

Also Published As

Publication number Publication date
CO2022016067A2 (es) 2023-01-26
US20230151010A1 (en) 2023-05-18
KR20230008742A (ko) 2023-01-16
CA3179957A1 (en) 2021-10-14
CN115916780A (zh) 2023-04-04
MX2022012523A (es) 2022-11-07
AU2021253946A1 (en) 2022-12-15
IL297206A (en) 2022-12-01
JP2023521411A (ja) 2023-05-24
CL2022002786A1 (es) 2023-04-14
BR112022020243A2 (pt) 2022-11-22
WO2021207659A1 (en) 2021-10-14
EP4132930A1 (en) 2023-02-15

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