JP2014513123A - 無定形固体の塩 - Google Patents

無定形固体の塩 Download PDF

Info

Publication number
JP2014513123A
JP2014513123A JP2014509345A JP2014509345A JP2014513123A JP 2014513123 A JP2014513123 A JP 2014513123A JP 2014509345 A JP2014509345 A JP 2014509345A JP 2014509345 A JP2014509345 A JP 2014509345A JP 2014513123 A JP2014513123 A JP 2014513123A
Authority
JP
Japan
Prior art keywords
amorphous solid
compound
present
formula
solid according
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.)
Pending
Application number
JP2014509345A
Other languages
English (en)
Japanese (ja)
Other versions
JP2014513123A5 (enExample
Inventor
ジョアンナ エム． コジアラ，
アン ロン，
ケイコ スジノ，
リチャード ユー，
Original Assignee
ギリアード サイエンシーズ， インコーポレイテッド
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 ギリアード サイエンシーズ， インコーポレイテッド filed Critical ギリアード サイエンシーズ， インコーポレイテッド
Publication of JP2014513123A publication Critical patent/JP2014513123A/ja
Publication of JP2014513123A5 publication Critical patent/JP2014513123A5/ja
Pending legal-status Critical Current

Links

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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Dispersion Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Otolaryngology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Biophysics (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dermatology (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)
JP2014509345A 2011-05-02 2012-04-30 無定形固体の塩 Pending JP2014513123A (ja)

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
JP2014513123A true JP2014513123A (ja) 2014-05-29
JP2014513123A5 JP2014513123A5 (enExample) 2015-06-25

Family

ID=46086061

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2014509345A Pending JP2014513123A (ja) 2011-05-02 2012-04-30 無定形固体の塩

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)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019508393A (ja) * 2016-01-28 2019-03-28 ギリアード サイエンシーズ， インコーポレイテッド １，３−チアゾール−５−イルメチル［（２ｒ，５ｒ）−５−｛［（２ｓ）−２−［（メチル｛［２−（プロパン−２−イル）−１，３−チアゾール−４−イル］メチル｝カルバモイル）アミノ］−４−（モルホリン−４−イル）ブタノイル］アミノ｝−１，６−ジフェニルヘキサン−２−イル］カルバメートまたはコビシスタットの結晶形態

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HK1204980A1 (en) * 2012-03-01 2015-12-11 Gilead Sciences, Inc. Spray dried formulations
EP2911674A1 (en) 2012-10-23 2015-09-02 Cipla Limited Pharmaceutical antiretroviral composition
WO2014105777A1 (en) 2012-12-26 2014-07-03 Assia Chemical Industries Ltd. Cobicostat dichlohydrate salt
JP2016538312A (ja) * 2013-11-29 2016-12-08 マイラン ラボラトリーズ リミテッドＭｙｌａｎ Ｌａｂｏｒａｔｏｒｉｅｓ Ｌｉｍｉｔｅｄ 非晶質のコビシスタットの固体分散体
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
WO2016106050A1 (en) 2014-12-26 2016-06-30 Emory University N4-hydroxycytidine and derivatives and anti-viral uses related thereto
US10351556B2 (en) 2015-02-18 2019-07-16 Msn Laboratories Private Limited Process for the preparation of 1,3-thiazol-5-ylmethyl [(2R,5R)-5-{[(2s)-2-[(methyl{[2-(propan-2-yl)-1,3-thiazol-4YL] methyl} carbamoyl) amino]-4-(morpholin-4-yl)butanoyl]amino)-1,6-diphenylhexan-2-yl]carbamate
CA3029032C (en) 2016-06-29 2024-10-29 Kezar Life Sciences CRYSTAL SALTS OF AN IMMUNOPROTEASOME PEPTIDE INHIBITOR EPOXYCETONE
WO2018005781A1 (en) 2016-06-29 2018-01-04 Kezar Life Sciences Process of preparing a peptide epoxyketone immunoproteasome inhibitor, and precursors thereof
RU2020116571A (ru) 2017-12-07 2021-11-22 Эмори Юниверсити N4-гидроксицитидин и производные и связанные с этим противовирусные применения
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 (2)

* 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

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101477822B1 (ko) * 2006-07-07 2015-01-02 길리애드 사이언시즈, 인코포레이티드 치료제의 약동학 특성의 모듈레이터
UA108738C2 (uk) * 2009-04-03 2015-06-10 Спосіб одержання інгібітора цитохром р450 монооксигенази та залучені проміжні сполуки

Patent Citations (2)

* 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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019508393A (ja) * 2016-01-28 2019-03-28 ギリアード サイエンシーズ， インコーポレイテッド １，３−チアゾール−５−イルメチル［（２ｒ，５ｒ）−５−｛［（２ｓ）−２−［（メチル｛［２−（プロパン−２−イル）−１，３−チアゾール−４−イル］メチル｝カルバモイル）アミノ］−４−（モルホリン−４−イル）ブタノイル］アミノ｝−１，６−ジフェニルヘキサン−２−イル］カルバメートまたはコビシスタットの結晶形態

Also Published As

Publication number Publication date
CA2836768A1 (en) 2012-11-08
PT2705027E (pt) 2015-09-11
AU2012250890B2 (en) 2015-05-28
EP2705027B1 (en) 2015-06-03
NZ617351A (en) 2015-09-25
HK1195770A1 (en) 2014-11-21
AU2012250890A1 (en) 2013-05-02
US20140187771A1 (en) 2014-07-03
WO2012151165A1 (en) 2012-11-08
EP2705027A1 (en) 2014-03-12
ES2543923T3 (es) 2015-08-25

Similar Documents

Publication Publication Date Title
EP2705027B1 (en) Amorphous solid salts of Cobicistat (GS-9350)
AU2014221210C1 (en) The use of solid carrier particles to improve the processability of a pharmaceutical agent
AU2009242451B2 (en) The use of solid carrier particles to improve the processability of a pharmaceutical agent
US20150004239A1 (en) Pharmaceutical compositions and methods for their preparation
US20150045366A1 (en) Spray dried formulations
HK1195770B (en) Amorphous solid salts of cobicistat (gs-9350)
NZ617351B2 (en) Amorphous solid salts of cobicistat (gs-9350)
HK1222553A1 (en) The use of solid carrier particles to improve the processability of a pharmaceutical agent
HK1153670B (en) The use of solid carrier particles to improve the processability of a pharmaceutical agent

Legal Events

Date Code Title Description
A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20150428

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20150507

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20151126

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20160129

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20160907