CN103189053A - 用于体重控制的5-ht2c激动剂的调节释放剂型 - Google Patents

用于体重控制的5-ht2c激动剂的调节释放剂型 Download PDF

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Publication number
CN103189053A
CN103189053A CN2011800525606A CN201180052560A CN103189053A CN 103189053 A CN103189053 A CN 103189053A CN 2011800525606 A CN2011800525606 A CN 2011800525606A CN 201180052560 A CN201180052560 A CN 201180052560A CN 103189053 A CN103189053 A CN 103189053A
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China
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methyl
chloro
tetrahydro
benzazepine
salt
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CN2011800525606A
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Chinese (zh)
Inventor
Z.J.邵
A.C.布拉克本
A.J.格罗迪克
M.摩根
J.K.鲁特
A.希弗里纳
S.斯蒂尔恩
L.杨
W.H.尹
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Arena Pharmaceuticals Inc
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Arena Pharmaceuticals Inc
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Priority to CN201710915541.0A priority Critical patent/CN107669687A/zh
Publication of CN103189053A publication Critical patent/CN103189053A/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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23P—SHAPING OR WORKING OF FOODSTUFFS, NOT FULLY COVERED BY A SINGLE OTHER SUBCLASS
    • A23P20/00—Coating of foodstuffs; Coatings therefor; Making laminated, multi-layered, stuffed or hollow foodstuffs
    • A23P20/10—Coating with edible coatings, e.g. with oils or fats
    • A23P20/12—Apparatus or processes for applying powders or particles to foodstuffs, e.g. for breading; Such apparatus combined with means for pre-moistening or battering
    • 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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • 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
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • A61K9/2846—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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/45—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/53—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C07C233/54—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of a saturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/16—Benzazepines; Hydrogenated benzazepines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/557—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms, e.g. orotic acid

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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Oil, Petroleum & Natural Gas (AREA)
  • Food Science & Technology (AREA)
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  • Diabetes (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN2011800525606A 2010-09-01 2011-08-31 用于体重控制的5-ht2c激动剂的调节释放剂型 Pending CN103189053A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201710915541.0A CN107669687A (zh) 2010-09-01 2011-08-31 用于体重控制的5‑ht2c激动剂的调节释放剂型

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US40257810P 2010-09-01 2010-09-01
US61/402,578 2010-09-01
US40314310P 2010-09-10 2010-09-10
US61/403,143 2010-09-10
PCT/US2011/049914 WO2012030927A2 (en) 2010-09-01 2011-08-31 Modified-release dosage forms of 5-ht2c agonists useful for weight management

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CN103189053A true CN103189053A (zh) 2013-07-03

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US (3) US20130315994A1 (enExample)
EP (2) EP3485878A1 (enExample)
JP (4) JP6272695B2 (enExample)
KR (2) KR101913442B1 (enExample)
CN (2) CN103189053A (enExample)
AU (1) AU2011296003B2 (enExample)
CA (2) CA2808912C (enExample)
ES (1) ES2704455T3 (enExample)
IL (1) IL224829B (enExample)
SG (2) SG10201506874UA (enExample)
WO (1) WO2012030927A2 (enExample)

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WO2015161730A1 (zh) * 2014-04-21 2015-10-29 杭州普晒医药科技有限公司 一种氯卡色林共晶及其制备方法、药物组合物和用途
CN105873905A (zh) * 2013-11-05 2016-08-17 斯洛文尼亚莱柯制药股份有限公司 稳定的无定形的盐酸氯卡色林
CN109952301A (zh) * 2016-08-19 2019-06-28 艾尼纳制药公司 5-ht2c受体激动剂和组合物及使用方法
CN110354088A (zh) * 2019-07-23 2019-10-22 南京昂谷医药科技有限公司 盐酸氯卡色林缓释片及其制备方法

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JP2016525576A (ja) * 2013-07-29 2016-08-25 アデア ファーマシューティカルズ，インコーポレイテッド 安定化された修飾放出型葉酸誘導体組成物、その治療用途および製造方法
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EA022748B1 (ru) * 2014-06-02 2016-02-29 Делкростон Менеджмент Лимитед Способы получения двойных солей лоркасерина (варианты), продукты способов, двойные соли, фармацевтические композиции для лечения и/или профилактики нарушений, связанных с ожирением, их применение и способ лечения и/или профилактики нарушений, связанных с ожирением
RU2704749C2 (ru) * 2014-09-29 2019-10-30 Зодженикс Интернэшнл Лимитед Система управления для управления распределением лекарственных продуктов
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EP3273967A4 (en) * 2015-03-24 2018-09-12 Aurobindo Pharma Limited A process for the preparation of lorcaserin hydrochloride
SG11201804811WA (en) 2015-12-22 2018-07-30 Zogenix International Ltd Fenfluramine compositions and methods of preparing the same
KR20180095674A (ko) 2015-12-22 2018-08-27 조게닉스 인터내셔널 리미티드 대사 저항성 펜플루라민 유사체 및 그 사용 방법
RU2746000C2 (ru) 2016-08-24 2021-04-05 Зодженикс Интернэшнл Лимитед Состав для ингибирования образования агонистов 5-ht2b и способы его применения
TW202510891A (zh) 2017-01-31 2025-03-16 美商基利科學股份有限公司 替諾福韋埃拉酚胺(tenofovir alafenamide)之晶型
US10682317B2 (en) 2017-09-26 2020-06-16 Zogenix International Limited Ketogenic diet compatible fenfluramine formulation
WO2019131902A1 (ja) 2017-12-27 2019-07-04 武田薬品工業株式会社 腹圧性尿失禁および便失禁の治療薬
JP2021526507A (ja) 2018-05-11 2021-10-07 ゾゲニクス インターナショナル リミテッド 発作により誘発される突然死を処置するための組成物および方法
WO2020072675A1 (en) 2018-10-02 2020-04-09 Northwestern University Beta-carbolines as positive allosteric modulators of the human serotonin receptor 2c (5-ht2c)
US12144787B2 (en) 2018-11-19 2024-11-19 Zogenix International Limited Method of treating patients with a mutation in cyclin-dependent kinase-like 5 (CDKL5)
US11612574B2 (en) 2020-07-17 2023-03-28 Zogenix International Limited Method of treating patients infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2)
CN113974568B (zh) * 2021-11-09 2024-03-26 重庆火后草科技有限公司 基于斜率去干扰的睡眠过程的代谢率的计算方法

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