SG10201804024VA - Formulations of azaindole compounds - Google Patents

Formulations of azaindole compounds

Info

Publication number
SG10201804024VA
SG10201804024VA SG10201804024VA SG10201804024VA SG10201804024VA SG 10201804024V A SG10201804024V A SG 10201804024VA SG 10201804024V A SG10201804024V A SG 10201804024VA SG 10201804024V A SG10201804024V A SG 10201804024VA SG 10201804024V A SG10201804024V A SG 10201804024VA
Authority
SG
Singapore
Prior art keywords
compound
pharmaceutical composition
formulations
hcl salt
composition comprises
Prior art date
Application number
SG10201804024VA
Inventor
Eric Simone
Tapan Sanghvi
Alamelu Banda
Katherine Stavropoulos
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=52001095&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=SG10201804024V(A) "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 SG10201804024VA publication Critical patent/SG10201804024VA/en

Links

Classifications

    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Pulmonology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Emergency Medicine (AREA)
  • Inorganic Chemistry (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

FORMULATIONS OF AZAINDOLE COMPOUNDS A pharmaceutical composition comprises: a) wt% to 9 5 wt% of a HCl salt of Compound (l) -xH2 0 by the weight of the pharmaceutical composition, wherein x is from 0 to 3; and b) 5 wt% to 9 5 wt% of a filler by the weight of the pharmaceutical composition. Another pharmaceutical composition comprises: a) 1 mg/ mL to 2 0 mg/ mL of Compound (1 ) in water; and b) 0 .0 1 M to0 .1 M of a pharmaceutically acceptable pH modifier. A method of preparing a pharmaceutical composition, comprising providing a mixture of Compound (1 ) that includes the HCl salt of Compound (l)-xH2 0 and the filler. Another method of preparing a pharmaceutical composition comprises mixing the HCl salt of Compound (l)' X3/ 4 0 and the pH modifier to form 1 mg/ mL to 2 0 mg/ mL of Compound (1 ) in water. Methods of reducing the amount of influenza viruses, inhibiting the replication of influenza viruses, andtreating influenza each independently employ such pharmaceutical compositions. No Suitable Figure
SG10201804024VA 2013-11-13 2014-11-12 Formulations of azaindole compounds SG10201804024VA (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361903840P 2013-11-13 2013-11-13

Publications (1)

Publication Number Publication Date
SG10201804024VA true SG10201804024VA (en) 2018-07-30

Family

ID=52001095

Family Applications (1)

Application Number Title Priority Date Filing Date
SG10201804024VA SG10201804024VA (en) 2013-11-13 2014-11-12 Formulations of azaindole compounds

Country Status (13)

Country Link
US (3) US20160250213A1 (en)
EP (1) EP3068434A1 (en)
JP (2) JP2016537347A (en)
KR (1) KR20160084465A (en)
CN (1) CN105848683A (en)
AU (1) AU2014348762A1 (en)
CA (1) CA2930105A1 (en)
CL (1) CL2016001111A1 (en)
IL (2) IL245587A0 (en)
MX (1) MX2016006197A (en)
RU (1) RU2685730C1 (en)
SG (1) SG10201804024VA (en)
WO (1) WO2015073491A1 (en)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GEP20156325B (en) 2009-06-17 2015-07-10 Vertex Pharma Inhibitors of influenza viruses replication
UA118010C2 (en) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед INFLUENCES OF INFLUENZA VIRUS REPLICATION
EP3421468B1 (en) 2013-11-13 2020-11-04 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
RS59144B1 (en) 2013-11-13 2019-09-30 Vertex Pharma Inhibitors of influenza viruses replication
WO2016183120A1 (en) 2015-05-13 2016-11-17 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
WO2016183116A1 (en) 2015-05-13 2016-11-17 Vertex Pharmaceuticals Incorporated Methods of preparing inhibitors of influenza viruses replication
AU2016368317B2 (en) 2015-12-09 2019-05-23 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication, application methods and uses thereof
CN107759571B (en) 2016-08-16 2021-03-02 广东东阳光药业有限公司 Inhibitors of influenza virus replication and methods of use and uses thereof
CN109641868B (en) 2016-08-30 2021-12-03 广东东阳光药业有限公司 Inhibitors of influenza virus replication and methods of use and uses thereof
AU2017376541B2 (en) 2016-12-15 2021-08-05 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication and uses thereof
WO2018127096A1 (en) 2017-01-05 2018-07-12 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication and uses thereof
US10815232B2 (en) 2017-01-24 2020-10-27 Crystal Pharmaceutical (Suzhou) Co., Ltd. Crystalline forms of viral-protein inhibitor drug VX-787, processes for preparation thereof and use thereof
WO2018157830A1 (en) 2017-03-02 2018-09-07 Sunshine Lake Pharma Co., Ltd. Inhibitors of influenza virus replication and uses thereof
EP3609502A1 (en) * 2017-04-12 2020-02-19 Vertex Pharmaceuticals Incorporated Combination therapies for treating influenza virus infection
WO2019043614A1 (en) * 2017-08-31 2019-03-07 Novartis Ag Method for preparing granules
US20210147413A1 (en) * 2018-04-06 2021-05-20 Janssen Pharmaceuticals, Inc. Isothermal reactive crystallisation process for the preparation of a crystalline form of pimodivir hydrochloride hemihydrate
WO2020058745A1 (en) * 2018-09-18 2020-03-26 Shionogi & Co., Ltd. Treating influenza using substituted polycyclic pyridone derivatives and prodrugs thereof
BR112021009254A2 (en) * 2018-11-13 2021-08-10 Cocrystal Pharma, Inc. formulations for influenza therapeutics
KR20200106607A (en) * 2019-03-05 2020-09-15 주식회사 코아팜바이오 A pharmaceutical composition comprising oseltamivir
US20200397784A1 (en) * 2019-06-20 2020-12-24 Janssen Pharmaceuticals, Inc. Formulations of azaindole compounds
CN112578034B (en) * 2020-11-04 2022-02-11 广东众生睿创生物科技有限公司 Quality control method of chiral amine micromolecules and salts thereof

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5681815A (en) * 1993-06-28 1997-10-28 Sophie Chen Antiviral and antitumor agents
ES2704482T3 (en) * 2004-11-24 2019-03-18 Meda Pharmaceuticals Inc Compositions comprising azelastine and its methods of use
US20120093738A1 (en) * 2009-06-11 2012-04-19 Rubicon Research Private Limited Taste-masked oral formulations of influenza antivirals
GEP20156325B (en) * 2009-06-17 2015-07-10 Vertex Pharma Inhibitors of influenza viruses replication

Also Published As

Publication number Publication date
RU2016122609A (en) 2017-12-18
US20180318301A1 (en) 2018-11-08
IL245587A0 (en) 2016-06-30
EP3068434A1 (en) 2016-09-21
US20160250213A1 (en) 2016-09-01
WO2015073491A1 (en) 2015-05-21
RU2685730C1 (en) 2019-04-23
CL2016001111A1 (en) 2017-06-09
KR20160084465A (en) 2016-07-13
AU2014348762A1 (en) 2016-05-26
JP2021191796A (en) 2021-12-16
CA2930105A1 (en) 2015-05-21
JP2016537347A (en) 2016-12-01
US20210008072A1 (en) 2021-01-14
CN105848683A (en) 2016-08-10
IL278214A (en) 2020-11-30
MX2016006197A (en) 2016-08-08

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