AU2015320358B2 - 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 - Google Patents

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 Download PDF

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Publication number
AU2015320358B2
AU2015320358B2 AU2015320358A AU2015320358A AU2015320358B2 AU 2015320358 B2 AU2015320358 B2 AU 2015320358B2 AU 2015320358 A AU2015320358 A AU 2015320358A AU 2015320358 A AU2015320358 A AU 2015320358A AU 2015320358 B2 AU2015320358 B2 AU 2015320358B2
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Australia
Prior art keywords
phenyl
atr
methyl
pharmaceutical composition
cyclopentyl
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Expired - Fee Related
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AU2015320358A
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English (en)
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AU2015320358A1 (en
Inventor
Aimesther BETANCOURT
Herman CHEN
Stephen Warren Hunt III
Robert MATUNAS
Martin Douglas Phillips
Roch Thibert
Charles UZARAMA
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Millendo Therapeutics Inc
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Millendo Therapeutics Inc
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Priority to AU2020202784A priority Critical patent/AU2020202784A1/en
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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
    • 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
    • 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
    • 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)
AU2015320358A 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 Expired - Fee Related AU2015320358B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2020202784A AU2020202784A1 (en) 2014-09-26 2020-04-27 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

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2020202784A Division AU2020202784A1 (en) 2014-09-26 2020-04-27 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
AU2015320358A1 AU2015320358A1 (en) 2017-05-11
AU2015320358B2 true AU2015320358B2 (en) 2020-05-14

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Family Applications (2)

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AU2015320358A Expired - Fee Related AU2015320358B2 (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
AU2020202784A Abandoned AU2020202784A1 (en) 2014-09-26 2020-04-27 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

Family Applications After (1)

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AU2020202784A Abandoned AU2020202784A1 (en) 2014-09-26 2020-04-27 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

Country Status (9)

Country Link
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 (2)

* 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
WO2013142214A1 (en) * 2012-03-22 2013-09-26 The Regents Of The University Of Michigan Compounds and methods for treating aberrant adrenocartical cell disorders

Family Cites Families (3)

* 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
CA2793533C (en) * 2010-03-23 2019-02-26 Siga Technologies, Inc. Polymorphic forms of st-246 and methods of preparation
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

Patent Citations (2)

* 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
WO2013142214A1 (en) * 2012-03-22 2013-09-26 The Regents Of The University Of Michigan Compounds and methods for treating aberrant adrenocartical cell disorders

Also Published As

Publication number Publication date
MX2017003916A (es) 2017-06-30
US20160090354A1 (en) 2016-03-31
US12151998B2 (en) 2024-11-26
AU2020202784A1 (en) 2020-05-14
BR112017006287A2 (pt) 2017-12-12
CA2962597A1 (en) 2016-03-31
CN107205941A (zh) 2017-09-26
EP3197435A1 (en) 2017-08-02
US20200255372A1 (en) 2020-08-13
US20170305843A1 (en) 2017-10-26
US20220162160A1 (en) 2022-05-26
US9546135B2 (en) 2017-01-17
US10059660B2 (en) 2018-08-28
WO2016049518A1 (en) 2016-03-31
AU2015320358A1 (en) 2017-05-11
JP2017530132A (ja) 2017-10-12

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