CN107205941A - N‑(2,6‑二(1‑甲基乙基)苯基)‑n′‑((1‑(4‑(二甲基氨基)苯基)环戊基)甲基)脲盐酸盐的固体药物形式以及涉及其的组合物、方法和试剂盒 - Google Patents

N‑(2,6‑二(1‑甲基乙基)苯基)‑n′‑((1‑(4‑(二甲基氨基)苯基)环戊基)甲基)脲盐酸盐的固体药物形式以及涉及其的组合物、方法和试剂盒 Download PDF

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Publication number
CN107205941A
CN107205941A CN201580063601.XA CN201580063601A CN107205941A CN 107205941 A CN107205941 A CN 107205941A CN 201580063601 A CN201580063601 A CN 201580063601A CN 107205941 A CN107205941 A CN 107205941A
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China
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solid pharmaceutical
atr
phenyl
pharmaceutical composition
unit dosage
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Pending
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CN201580063601.XA
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English (en)
Chinese (zh)
Inventor
史蒂芬·沃伦·亨特三世
马丁·道格拉斯·菲利普
罗伯特·玛图纳斯
陈中冰
艾麦斯瑟尔·贝坦科特
查尔斯·乌兹拉玛
罗奇·蒂贝尔
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Milunduo Treatment Co
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Milunduo Treatment Co
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Publication of CN107205941A publication Critical patent/CN107205941A/zh
Pending legal-status Critical Current

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    • 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
    • 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
    • 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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Biophysics (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)
CN201580063601.XA 2014-09-26 2015-09-25 N‑(2,6‑二(1‑甲基乙基)苯基)‑n′‑((1‑(4‑(二甲基氨基)苯基)环戊基)甲基)脲盐酸盐的固体药物形式以及涉及其的组合物、方法和试剂盒 Pending CN107205941A (zh)

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 (1)

Publication Number Publication Date
CN107205941A true CN107205941A (zh) 2017-09-26

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CN201580063601.XA Pending CN107205941A (zh) 2014-09-26 2015-09-25 N‑(2,6‑二(1‑甲基乙基)苯基)‑n′‑((1‑(4‑(二甲基氨基)苯基)环戊基)甲基)脲盐酸盐的固体药物形式以及涉及其的组合物、方法和试剂盒

Country Status (9)

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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112441941A (zh) * 2020-12-03 2021-03-05 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

Families Citing this family (2)

* 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

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
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
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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG184201A1 (en) * 2010-03-23 2012-10-30 Siga Technologies Inc Polymorphic forms 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 (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
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
WO2013142214A1 (en) * 2012-03-22 2013-09-26 The Regents Of The University Of Michigan Compounds and methods for treating aberrant adrenocartical cell disorders

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
BHARAT K. TRIVEDI等: "Inhibitors of Acyl-CoA:Cholesterol Acyltransferase (ACAT). 7. Development of a Series of Substituted N-Phenyl- N′-[(l-phenylcyclopentyl)methyl]ureas with Enhanced Hypocholesterolemic Activity", 《J. MED. CHEM.》 *
HANS-JOACHIM KNOLKER等: "A Novel Method for the Synthesis of Isocyanates Under Mild Conditions**", 《ANGEWANDTE CHEMIE INTERNATIONAL EDITION》 *
VERNETTI LA等: "ATP Depletion Is Associated with Cytotoxicity of a Novel Lipid Regulator in Guinea Pig Adrenocortical Cells", 《TOXICOLOGY AND APPLIED PHARMACOLOGY》 *
李晓天、赵永星: "《生物药剂学与药物动力学》", 31 October 2006 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112441941A (zh) * 2020-12-03 2021-03-05 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
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

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Publication number Publication date
MX2017003916A (es) 2017-06-30
US20220162160A1 (en) 2022-05-26
US20170305843A1 (en) 2017-10-26
AU2015320358A1 (en) 2017-05-11
EP3197435A1 (en) 2017-08-02
CA2962597A1 (en) 2016-03-31
BR112017006287A2 (pt) 2017-12-12
US20160090354A1 (en) 2016-03-31
US9546135B2 (en) 2017-01-17
AU2020202784A1 (en) 2020-05-14
US10059660B2 (en) 2018-08-28
US20200255372A1 (en) 2020-08-13
US12151998B2 (en) 2024-11-26
AU2015320358B2 (en) 2020-05-14
WO2016049518A1 (en) 2016-03-31
JP2017530132A (ja) 2017-10-12

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