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CO2019007129A2 - Modulador del regulador de conductancia transmembrana de fibrosis quística, composiciones farmacéuticas, métodos de tratamiento y proceso para producir el modulador - Google Patents

Modulador del regulador de conductancia transmembrana de fibrosis quística, composiciones farmacéuticas, métodos de tratamiento y proceso para producir el modulador

Info

Publication number
CO2019007129A2
CO2019007129A2 CONC2019/0007129A CO2019007129A CO2019007129A2 CO 2019007129 A2 CO2019007129 A2 CO 2019007129A2 CO 2019007129 A CO2019007129 A CO 2019007129A CO 2019007129 A2 CO2019007129 A2 CO 2019007129A2
Authority
CO
Colombia
Prior art keywords
modulator
pharmaceutical compositions
cystic fibrosis
produce
treatment methods
Prior art date
Application number
CONC2019/0007129A
Other languages
English (en)
Inventor
Timothy Alcacio
Ruah Sara Sabina Hadida
Robert M Hughes
Ali Keshavarz-Shokri
Jason Mccartney
Mark Thomas Miller
Corey Anderson
Thomas Cleveland
Haripada Khatuya
Pramod Virupax Joshi
Paul John Krenitsky
Fabrice Jean Denis Pierre
Andreas P Termin
Johnny Uy
Jinglan Zhou
Alexander Russell Abela
Prasuna Paraselli
David Andrew Siesel
Paul Timothy Angell
Minson Baek
Jeremy J Clemens
Lori Ann Ferris
Peter Diederik Jan Grootenhuis
Raymond Stanley Gross
Anton Gulevich
Clara Kuang-Ju Hsia
Ping Kang
Yi Shi
Muna Shrestha
Kathy Stavropoulos
Goor Fredrick F Van
Timothy John Young
Original Assignee
Vertex Pharma
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=60953944&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CO2019007129(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of CO2019007129A2 publication Critical patent/CO2019007129A2/es

Links

Classifications

    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/455Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5365Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/18One oxygen or sulfur atom
    • C07D231/20One oxygen atom attached in position 3 or 5
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D471/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Se describen compuestos de Fórmula (I): (I), sales farmacéuticamente aceptables de este, derivados deuterados de cualquiera de los que anteceden y metabolitos de cualquiera de los anteceden. También se describen composiciones farmacéuticas que los comprenden, métodos para el tratamiento de la fibrosis quística mediante el uso de estos y métodos para confeccionarlos. Se describen además las formas en estado sólido del Compuesto 1 y sales y solvatos de este.
CONC2019/0007129A 2016-12-09 2019-07-03 Modulador del regulador de conductancia transmembrana de fibrosis quística, composiciones farmacéuticas, métodos de tratamiento y proceso para producir el modulador CO2019007129A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662432537P 2016-12-09 2016-12-09
PCT/US2017/065425 WO2018107100A1 (en) 2016-12-09 2017-12-08 Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator

Publications (1)

Publication Number Publication Date
CO2019007129A2 true CO2019007129A2 (es) 2019-07-31

Family

ID=60953944

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2019/0007129A CO2019007129A2 (es) 2016-12-09 2019-07-03 Modulador del regulador de conductancia transmembrana de fibrosis quística, composiciones farmacéuticas, métodos de tratamiento y proceso para producir el modulador

Country Status (37)

Country Link
US (3) US10793547B2 (es)
EP (2) EP3551622B1 (es)
JP (3) JP6916285B2 (es)
KR (1) KR102269492B1 (es)
CN (2) CN117843619A (es)
AR (1) AR110346A1 (es)
AU (3) AU2017371200B2 (es)
CA (1) CA3046086A1 (es)
CL (1) CL2019001553A1 (es)
CO (1) CO2019007129A2 (es)
CY (1) CY1123736T1 (es)
DK (1) DK3551622T3 (es)
EA (2) EA039280B1 (es)
EC (1) ECSP19048759A (es)
ES (1) ES2837431T3 (es)
GE (1) GEP20247634B (es)
HR (1) HRP20201946T1 (es)
HU (1) HUE052205T2 (es)
IL (3) IL277491B (es)
JO (1) JOP20190125B1 (es)
LT (1) LT3551622T (es)
MA (2) MA49235B1 (es)
MD (1) MD3551622T2 (es)
MX (2) MX388103B (es)
NZ (1) NZ795112A (es)
PE (2) PE20241131A1 (es)
PT (1) PT3551622T (es)
RS (1) RS61150B1 (es)
SA (1) SA519401947B1 (es)
SG (1) SG10201913606VA (es)
SI (1) SI3551622T1 (es)
SM (1) SMT202000617T1 (es)
TW (1) TWI774712B (es)
UA (1) UA128449C2 (es)
UY (2) UY37513A (es)
WO (1) WO2018107100A1 (es)
ZA (2) ZA201904062B (es)

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JOP20190042B1 (ar) 2016-09-30 2021-08-17 Vertex Pharma مُعدِّل‏ لمنظم موصلية التليف الكيسي عبر الغشاء، وتركيبات صيدلانية، وطرق للعلاج، وعملية لتصنيع المُعدِّل
UY37513A (es) 2016-12-09 2018-07-31 Vertex Pharma Modulador del regulador de conductancia transmembrana de fibrosis quística, composiciones farmacéuticas, métodos de tratamiento y proceso para producir el modulador
US11253509B2 (en) 2017-06-08 2022-02-22 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
BR112020000941A2 (pt) * 2017-07-17 2020-07-21 Vertex Pharmaceuticals Incorporated métodos de tratamento para fibrose cística
AU2018309043B2 (en) * 2017-08-02 2022-03-31 Vertex Pharmaceuticals Incorporated Processes for preparing pyrrolidine compounds
CA3078893A1 (en) 2017-10-19 2019-04-25 Vertex Pharmaceuticals Incorporated Crystalline forms and compositions of cftr modulators
US11465985B2 (en) * 2017-12-08 2022-10-11 Vertex Pharmaceuticals Incorporated Processes for making modulators of cystic fibrosis transmembrane conductance regulator
TWI810243B (zh) * 2018-02-05 2023-08-01 美商維泰克斯製藥公司 用於治療囊腫纖化症之醫藥組合物
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AU2023215272A1 (en) 2022-02-03 2024-08-15 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
KR20240155228A (ko) 2022-02-03 2024-10-28 버텍스 파마슈티칼스 인코포레이티드 (6a,12a)-17-아미노-12-메틸-6,15-비스(트리플루오로메틸)-13,19-디옥사-3,4,18-트리아자트리시클로[12.3.1.12,5]노나데카-1(18),2,4,14,16-펜타엔-6-올의 결정질 형태를 제조하는 방법
WO2023154291A1 (en) 2022-02-08 2023-08-17 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
CN119731183A (zh) 2022-05-16 2025-03-28 弗特克斯药品有限公司 大环化合物作为cftr调节剂的固体形式和其制备
CN119947720A (zh) 2022-05-16 2025-05-06 弗特克斯药品有限公司 治疗囊性纤维化的方法
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WO2024056798A1 (en) 2022-09-15 2024-03-21 Idorsia Pharmaceuticals Ltd Macrocyclic cftr modulators
JP2025530377A (ja) 2022-09-15 2025-09-11 イドルシア・ファーマシューティカルズ・リミテッド 大環状cftr調節剤とcftrコレクター及び/又はcftrポテンシエーターとの合剤
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WO2026006653A1 (en) 2024-06-28 2026-01-02 Vertex Pharmaceuticals Incorporated Combination comprising exacaftor/tezacaftor/ivacaftor for use in treating cystic fibrosis where the patient has at least one cftr mutation

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