KR102350156B1 - 피롤리딘 유도체의 경구 제형 - Google Patents

피롤리딘 유도체의 경구 제형 Download PDF

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KR102350156B1
KR102350156B1 KR1020167018856A KR20167018856A KR102350156B1 KR 102350156 B1 KR102350156 B1 KR 102350156B1 KR 1020167018856 A KR1020167018856 A KR 1020167018856A KR 20167018856 A KR20167018856 A KR 20167018856A KR 102350156 B1 KR102350156 B1 KR 102350156B1
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methyl
biphenyl
carbonyl
hydroxymethyl
methyloxime
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Korean (ko)
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KR20160097359A (ko
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앙드레 숄레
올리비에 폴
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옵스에파 에스에이
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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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/401—Proline; Derivatives thereof, e.g. captopril
    • 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
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/40—Cyclodextrins; Derivatives thereof
    • 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
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • 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
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • 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
    • 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
    • A61K9/2009—Inorganic 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
    • A61K9/20—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
    • A61K9/2027—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
    • A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Inorganic Chemistry (AREA)
  • Reproductive Health (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Zoology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
KR1020167018856A 2013-12-17 2014-12-15 피롤리딘 유도체의 경구 제형 Active KR102350156B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13197606.0A EP2886107A1 (en) 2013-12-17 2013-12-17 Oral formulations of pyrrolydine derivatives
EP13197606.0 2013-12-17
PCT/EP2014/077767 WO2015091365A1 (en) 2013-12-17 2014-12-15 Oral formulations of pyrrolidine derivatives

Publications (2)

Publication Number Publication Date
KR20160097359A KR20160097359A (ko) 2016-08-17
KR102350156B1 true KR102350156B1 (ko) 2022-01-11

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Country Link
US (5) US20170065556A1 (enExample)
EP (4) EP2886107A1 (enExample)
JP (2) JP6479800B2 (enExample)
KR (1) KR102350156B1 (enExample)
CN (2) CN106029057B (enExample)
AU (1) AU2014364962B2 (enExample)
CA (1) CA2931592C (enExample)
CY (1) CY1119728T1 (enExample)
DK (1) DK3082773T3 (enExample)
EA (2) EA201892033A3 (enExample)
ES (2) ES2726730T3 (enExample)
HK (1) HK1249050B (enExample)
HU (1) HUE035212T2 (enExample)
IL (2) IL245855B (enExample)
MX (2) MX363697B (enExample)
PT (1) PT3082773T (enExample)
SI (1) SI3082773T1 (enExample)
UA (1) UA116824C2 (enExample)
WO (1) WO2015091365A1 (enExample)

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EP2845850A1 (en) 2013-09-10 2015-03-11 ObsEva S.A. Pyrrolidine derivatives as oxytocin/vasopressin V1a receptors antagonists
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AU2015283133B2 (en) 2014-07-02 2019-05-16 ObsEva SA Crystalline (3Z,5S)-5-(hydroxymethyl)-1-[(2'-methyl-1,1'-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methyloxime useful in methods of treating conditions related to the OT-R activity
TWI829098B (zh) 2015-01-02 2024-01-11 美商梅拉洛伊卡公司 細菌組成物
SG10202009723PA (en) 2016-01-04 2020-11-27 ObsEva SA Alpha-amino esters of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof
WO2018015497A2 (en) 2016-07-21 2018-01-25 ObsEva S.A. Oxytocin antagonist dosing regimens for promoting embryo implantation and preventing miscarriage
IT201600101413A1 (it) 2016-10-10 2018-04-10 Sofar Swiss S A Composizione liquida per uso nel trattamento del reflusso gastroesofageo
IT201700124434A1 (it) * 2017-10-31 2019-05-01 Sofar Swiss Sa Compressa da succhiare e/o sciogliere in bocca a base di acido ialuronico e condroitina solfato e loro sali per uso nel trattamento di una sottopopolazione di pazienti GERD.
IT201700124424A1 (it) 2017-10-31 2019-05-01 Sofar Swiss Sa Compressa da succhiare e/o sciogliere in bocca a base di acido ialuronico e condroitina solfato e loro sali
GB201910125D0 (en) * 2019-07-15 2019-08-28 Kalvista Pharmaceuticals Ltd Treatments of angioedema
GB201910116D0 (en) * 2019-07-15 2019-08-28 Kalvista Pharmaceuticals Ltd Treatments of hereditary angioedema
US20220323410A1 (en) * 2019-09-03 2022-10-13 ObsEva S.A. Oxytocin antagonist dosing regimens for promoting embryo implantation and preventing miscarriage
CN115380122A (zh) 2020-02-10 2022-11-22 奥布赛瓦股份公司 用于催产素受体拮抗剂疗法的生物标志物
CN121265577A (zh) 2020-05-18 2026-01-06 奥瑞克索股份公司 用于药物递送的药物组合物
TW202333658A (zh) 2021-11-25 2023-09-01 瑞典商奥瑞克索股份公司 包含腎上腺素之新穎醫藥組合物
GB202117016D0 (en) 2021-11-25 2022-01-12 Orexo Ab New pharmaceutical device

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EP2886107A1 (en) 2013-12-17 2015-06-24 ObsEva S.A. Oral formulations of pyrrolydine derivatives
AU2015283133B2 (en) 2014-07-02 2019-05-16 ObsEva SA Crystalline (3Z,5S)-5-(hydroxymethyl)-1-[(2'-methyl-1,1'-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methyloxime useful in methods of treating conditions related to the OT-R activity
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US20180311211A1 (en) 2018-11-01
WO2015091365A1 (en) 2015-06-25
US20170065556A1 (en) 2017-03-09
EA201691061A1 (ru) 2016-11-30
EP3266449A1 (en) 2018-01-10
AU2014364962A1 (en) 2016-07-28
EA201892033A2 (ru) 2019-02-28
EA031530B1 (ru) 2019-01-31
UA116824C2 (uk) 2018-05-10
CN106029057B (zh) 2019-09-03
EP3494967A1 (en) 2019-06-12
SI3082773T1 (en) 2018-02-28
IL245855A0 (en) 2016-07-31
EP3082773B1 (en) 2017-10-04
IL245855B (en) 2019-02-28
EA201892033A3 (ru) 2019-03-29
US20230226021A1 (en) 2023-07-20
EP3082773A1 (en) 2016-10-26
US9962367B2 (en) 2018-05-08
MX363697B (es) 2019-03-29
HK1249050B (en) 2020-01-17
CY1119728T1 (el) 2018-06-27
HUE035212T2 (en) 2018-05-02
DK3082773T3 (en) 2018-01-08
US20150164859A1 (en) 2015-06-18
KR20160097359A (ko) 2016-08-17
JP2019108336A (ja) 2019-07-04
EP3266449B1 (en) 2019-02-27
US11419851B2 (en) 2022-08-23
CN106029057A (zh) 2016-10-12
MX2016007930A (es) 2016-09-19
PT3082773T (pt) 2018-01-09
IL264259A (en) 2019-02-28
US10478420B2 (en) 2019-11-19
JP2016540758A (ja) 2016-12-28
CN110960495A (zh) 2020-04-07
ES2726730T3 (es) 2019-10-08
CA2931592A1 (en) 2015-06-25
EP2886107A1 (en) 2015-06-24
JP6479800B2 (ja) 2019-03-06
ES2654927T3 (es) 2018-02-15
MX2019003598A (es) 2019-07-15
CA2931592C (en) 2021-12-07
AU2014364962B2 (en) 2020-03-26
CN110960495B (zh) 2022-05-10
US20200281892A1 (en) 2020-09-10

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