AU2012250890B2 - Amorphous solid salts - Google Patents

Amorphous solid salts Download PDF

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Publication number
AU2012250890B2
AU2012250890B2 AU2012250890A AU2012250890A AU2012250890B2 AU 2012250890 B2 AU2012250890 B2 AU 2012250890B2 AU 2012250890 A AU2012250890 A AU 2012250890A AU 2012250890 A AU2012250890 A AU 2012250890A AU 2012250890 B2 AU2012250890 B2 AU 2012250890B2
Authority
AU
Australia
Prior art keywords
amorphous solid
compound
hiv
formula
inhibitors
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
AU2012250890A
Other languages
English (en)
Other versions
AU2012250890A1 (en
Inventor
Joanna M. Koziara
Anne LUNONG
Keiko Sujino
Richard Yu
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Gilead Sciences Inc
Original Assignee
Gilead Sciences Inc
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 Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of AU2012250890A1 publication Critical patent/AU2012250890A1/en
Application granted granted Critical
Publication of AU2012250890B2 publication Critical patent/AU2012250890B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/145—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/15—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/008—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
    • 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
    • A61K9/10—Dispersions; Emulsions
    • A61K9/12—Aerosols; Foams
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • 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
    • 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
    • A61P31/18—Antivirals for RNA viruses for HIV
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/28—Radicals substituted by nitrogen atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Dispersion Chemistry (AREA)
  • Virology (AREA)
  • Molecular Biology (AREA)
  • Dermatology (AREA)
  • Otolaryngology (AREA)
  • Communicable Diseases (AREA)
  • Pulmonology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Biophysics (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2012250890A 2011-05-02 2012-04-30 Amorphous solid salts Ceased AU2012250890B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161481509P 2011-05-02 2011-05-02
US61/481,509 2011-05-02
PCT/US2012/035871 WO2012151165A1 (en) 2011-05-02 2012-04-30 Amorphous solid salts

Publications (2)

Publication Number Publication Date
AU2012250890A1 AU2012250890A1 (en) 2013-05-02
AU2012250890B2 true AU2012250890B2 (en) 2015-05-28

Family

ID=46086061

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2012250890A Ceased AU2012250890B2 (en) 2011-05-02 2012-04-30 Amorphous solid salts

Country Status (8)

Country Link
US (1) US20140187771A1 (enExample)
EP (1) EP2705027B1 (enExample)
JP (1) JP2014513123A (enExample)
AU (1) AU2012250890B2 (enExample)
CA (1) CA2836768A1 (enExample)
ES (1) ES2543923T3 (enExample)
PT (1) PT2705027E (enExample)
WO (1) WO2012151165A1 (enExample)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013130766A1 (en) * 2012-03-01 2013-09-06 Gilead Sciences, Inc. Spray dried formulations
NZ706223A (en) 2012-10-23 2018-11-30 Cipla Ltd Pharmaceutical antiretroviral composition
US20160200716A1 (en) 2012-12-26 2016-07-14 Assia Chemical Industries Ltd. Cobicistat dichlohydrate salt
WO2015079415A1 (en) * 2013-11-29 2015-06-04 Mylan Laboratories Ltd. Amorphous cobicistat solid dispersion
CN105732538B (zh) * 2014-12-09 2018-04-13 杭州普晒医药科技有限公司 可比司他帕莫酸盐及其制备方法、药物组合物和用途
WO2016094011A1 (en) * 2014-12-11 2016-06-16 Merck Sharp & Dohme Corp. Crystal forms of a ccr5 antagonist
CN118286245A (zh) 2014-12-26 2024-07-05 埃莫里大学 N4-羟基胞苷和衍生物及与其相关的抗病毒用途
WO2016132378A2 (en) * 2015-02-18 2016-08-25 Msn Laboratories Private Limited Novel process for the preparation of 1,3-thiazol-5-ylmethyl [(2r,5r)-5-{[(2s)-2- [(methyl{[2-(propan-2-yl)- 1,3-thiazol-4-yl] methyl} carbamoyl) amino] -4-(morpholin-4-yl)butanoyl]amino}-1,6-diphenylhexan-2-yl] carbamate
TW201728582A (zh) * 2016-01-28 2017-08-16 基利科學股份有限公司 結晶型
ES2944958T3 (es) 2016-06-29 2023-06-27 Kezar Life Sciences Sales cristalinas de inhibidor del inmunoproteasoma de epoxicetona peptídico
TWI751177B (zh) 2016-06-29 2022-01-01 美商基澤生命科學公司 製備肽環氧酮免疫蛋白酶體抑制劑及其前驅體之方法
RS66222B1 (sr) 2017-12-07 2024-12-31 Univ Emory N4-hidroksicitidin i derivati i antivirusne upotrebe povezane sa njim
CN110368370B (zh) * 2018-04-12 2022-08-12 湖南千金湘江药业股份有限公司 一种无定形半富马酸替诺福韦二吡呋酯片及其制备方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008103949A1 (en) * 2007-02-23 2008-08-28 Gilead Sciences, Inc. Modulators of pharmacokinetic properties of therapeutics
WO2009135179A2 (en) * 2008-05-02 2009-11-05 Gilead Sciences, Inc. The use of solid carrier particles to improve the processability of a pharmaceutical agent
WO2010115000A2 (en) * 2009-04-03 2010-10-07 Gilead Sciences, Inc. Methods and intermediates for preparing pharmaceutical agents

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2049506T5 (pl) * 2006-07-07 2024-09-09 Gilead Sciences, Inc. Modulatory farmakokinetycznych właściwości leków

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008103949A1 (en) * 2007-02-23 2008-08-28 Gilead Sciences, Inc. Modulators of pharmacokinetic properties of therapeutics
WO2009135179A2 (en) * 2008-05-02 2009-11-05 Gilead Sciences, Inc. The use of solid carrier particles to improve the processability of a pharmaceutical agent
WO2010115000A2 (en) * 2009-04-03 2010-10-07 Gilead Sciences, Inc. Methods and intermediates for preparing pharmaceutical agents

Also Published As

Publication number Publication date
EP2705027B1 (en) 2015-06-03
AU2012250890A1 (en) 2013-05-02
US20140187771A1 (en) 2014-07-03
EP2705027A1 (en) 2014-03-12
CA2836768A1 (en) 2012-11-08
PT2705027E (pt) 2015-09-11
NZ617351A (en) 2015-09-25
JP2014513123A (ja) 2014-05-29
ES2543923T3 (es) 2015-08-25
HK1195770A1 (en) 2014-11-21
WO2012151165A1 (en) 2012-11-08

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Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired