JP2017530132A - Ｎ−（２，６−ビス（１−メチルエチル）フェニル）−ｎ’−（（１−（４−（ジメチルアミノ）フェニル）シクロペンチル）メチル）尿素塩酸塩の固体薬物形態ならびにこれに関係する組成物、方法、およびキット - Google Patents

Ｎ−（２，６−ビス（１−メチルエチル）フェニル）−ｎ’−（（１−（４−（ジメチルアミノ）フェニル）シクロペンチル）メチル）尿素塩酸塩の固体薬物形態ならびにこれに関係する組成物、方法、およびキット Download PDF

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JP2017530132A
JP2017530132A JP2017516764A JP2017516764A JP2017530132A JP 2017530132 A JP2017530132 A JP 2017530132A JP 2017516764 A JP2017516764 A JP 2017516764A JP 2017516764 A JP2017516764 A JP 2017516764A JP 2017530132 A JP2017530132 A JP 2017530132A
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atr
solid
phenyl
pharmaceutical composition
unit dosage
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JP2017530132A5 (enExample
Inventor
ロバート マツナス，
ロバート マツナス，
ハーマン チェン，
ハーマン チェン，
アイメスター ベタンクール，
アイメスター ベタンクール，
チャールズ ウザラマ，
チャールズ ウザラマ，
ロッシュ ティベール，
ロッシュ ティベール，
スティーブン ワレン ザ サード ハント，
スティーブン ワレン ザ サード ハント，
マーティン ダグラス フィリップス，
マーティン ダグラス フィリップス，
Original Assignee
ミレンド セラピューティクス， インコーポレイテッド
ミレンド セラピューティクス， インコーポレイテッド
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Publication of JP2017530132A publication Critical patent/JP2017530132A/ja
Publication of JP2017530132A5 publication Critical patent/JP2017530132A5/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • 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
    • A61K31/17—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
    • 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
    • A61K9/205—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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • A61K9/2081—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets with microcapsules or coated microparticles according to A61K9/50
    • 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
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5084—Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C273/00—Preparation of urea or its derivatives, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C273/18—Preparation of urea or its derivatives, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups of substituted ureas
    • C07C273/1809—Preparation of urea or its derivatives, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups of substituted ureas with formation of the N-C(O)-N moiety
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C273/00—Preparation of urea or its derivatives, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C273/18—Preparation of urea or its derivatives, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups of substituted ureas
    • C07C273/1809—Preparation of urea or its derivatives, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups of substituted ureas with formation of the N-C(O)-N moiety
    • C07C273/1818—Preparation of urea or its derivatives, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups of substituted ureas with formation of the N-C(O)-N moiety from -N=C=O and XNR'R"
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2017516764A 2014-09-26 2015-09-25 Ｎ−（２，６−ビス（１−メチルエチル）フェニル）−ｎ’−（（１−（４−（ジメチルアミノ）フェニル）シクロペンチル）メチル）尿素塩酸塩の固体薬物形態ならびにこれに関係する組成物、方法、およびキット Pending JP2017530132A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201462055964P 2014-09-26 2014-09-26
US62/055,964 2014-09-26
US201462086153P 2014-12-01 2014-12-01
US62/086,153 2014-12-01
PCT/US2015/052338 WO2016049518A1 (en) 2014-09-26 2015-09-25 Solid drug form of n-(2,6-bis(1-methylethyl)phenyl)-n'-((1-(4-(dimethylamino)phenyl)cyclopentyl) methyl)urea hydrochloride and compositions, methods and kits related thereto

Publications (2)

Publication Number Publication Date
JP2017530132A true JP2017530132A (ja) 2017-10-12
JP2017530132A5 JP2017530132A5 (enExample) 2018-11-08

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JP2017516764A Pending JP2017530132A (ja) 2014-09-26 2015-09-25 Ｎ−（２，６−ビス（１−メチルエチル）フェニル）−ｎ’−（（１−（４−（ジメチルアミノ）フェニル）シクロペンチル）メチル）尿素塩酸塩の固体薬物形態ならびにこれに関係する組成物、方法、およびキット

Country Status (9)

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US (4) US9546135B2 (enExample)
EP (1) EP3197435A1 (enExample)
JP (1) JP2017530132A (enExample)
CN (1) CN107205941A (enExample)
AU (2) AU2015320358B2 (enExample)
BR (1) BR112017006287A2 (enExample)
CA (1) CA2962597A1 (enExample)
MX (1) MX2017003916A (enExample)
WO (1) WO2016049518A1 (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2573085A1 (en) 2011-09-26 2013-03-27 AiCuris GmbH & Co. KG N-[5-(aminosulfonyl)-4methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl] acetamide mesylate monohydrate having a specific particle size distribution range and a specific surface area range
WO2016164476A2 (en) * 2015-04-06 2016-10-13 Millendo Therapeutics, Inc. Combination therapy for treating disorders associated with excess cortisol production
CN112441941B (zh) * 2020-12-03 2022-08-02 浙江荣耀生物科技股份有限公司 一种1-(4-氨基苯基)环戊基甲腈的制备方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5015644A (en) * 1987-06-02 1991-05-14 Warner-Lambert Company Antihyperlipidemic and antiatherosclerotic urea and carbamate compounds
WO2013045491A1 (en) * 2011-09-26 2013-04-04 Aicuris Gmbh & Co. Kg N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-n-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mesylate monohydrate having a specific particle size distribution range and a specific surface area range for use in pharmaceutical formulations.
JP2013522371A (ja) * 2010-03-23 2013-06-13 シガ・テクノロジーズ・インコーポレーテッド Ｓｔ−２４６の多形型および調製方法

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005068066A (ja) * 2003-08-25 2005-03-17 Air Water Chemical Inc ２，６−ジイソプロピルアニリンの精製方法
CN106236741A (zh) * 2012-03-22 2016-12-21 密歇根大学董事会 用于治疗异常肾上腺皮质细胞疾病的化合物和方法

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5015644A (en) * 1987-06-02 1991-05-14 Warner-Lambert Company Antihyperlipidemic and antiatherosclerotic urea and carbamate compounds
JP2013522371A (ja) * 2010-03-23 2013-06-13 シガ・テクノロジーズ・インコーポレーテッド Ｓｔ−２４６の多形型および調製方法
WO2013045491A1 (en) * 2011-09-26 2013-04-04 Aicuris Gmbh & Co. Kg N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-n-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mesylate monohydrate having a specific particle size distribution range and a specific surface area range for use in pharmaceutical formulations.

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
JOURNAL OF MEDICINAL CHEMISTRY, vol. 37, no. 11, JPN6019022966, 1994, pages 1652 - 1659, ISSN: 0004362941 *
TOXICOLOGY AND APPLIED PHARMACOLOGY, vol. 118, no. 1, JPN6019022968, 1993, pages 30 - 38, ISSN: 0004362942 *

Also Published As

Publication number Publication date
US12151998B2 (en) 2024-11-26
AU2015320358B2 (en) 2020-05-14
US9546135B2 (en) 2017-01-17
US20220162160A1 (en) 2022-05-26
AU2020202784A1 (en) 2020-05-14
US20160090354A1 (en) 2016-03-31
MX2017003916A (es) 2017-06-30
EP3197435A1 (en) 2017-08-02
US20200255372A1 (en) 2020-08-13
WO2016049518A1 (en) 2016-03-31
US10059660B2 (en) 2018-08-28
US20170305843A1 (en) 2017-10-26
AU2015320358A1 (en) 2017-05-11
CA2962597A1 (en) 2016-03-31
BR112017006287A2 (pt) 2017-12-12
CN107205941A (zh) 2017-09-26

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