JP2015510947A - 小分子ｇｌｐ１ｒアゴニストのトリス（ヒドロキシメチル）アミノメタン塩ならびにその医薬組成物および使用 - Google Patents

小分子ｇｌｐ１ｒアゴニストのトリス（ヒドロキシメチル）アミノメタン塩ならびにその医薬組成物および使用 Download PDF

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JP2015510947A
JP2015510947A JP2015501876A JP2015501876A JP2015510947A JP 2015510947 A JP2015510947 A JP 2015510947A JP 2015501876 A JP2015501876 A JP 2015501876A JP 2015501876 A JP2015501876 A JP 2015501876A JP 2015510947 A JP2015510947 A JP 2015510947A
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solid composition
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salt
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JP2015510947A5 (OSRAM
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アルマリエゴ，ダニロ
ポリセッティ，ダルマ・ラオ
ベンジャミン，エリック
エル・アブデラウイ，ハッサン
サフー，ソーミャ・ピー
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トランステック・ファーマ，エルエルシー
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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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • 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
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J2/00—Processes or devices for granulating materials, e.g. fertilisers in general; Rendering particulate materials free flowing in general, e.g. making them hydrophobic
    • B01J2/02—Processes or devices for granulating materials, e.g. fertilisers in general; Rendering particulate materials free flowing in general, e.g. making them hydrophobic by dividing the liquid material into drops, e.g. by spraying, and solidifying the drops
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • 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
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Inorganic Chemistry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2015501876A 2012-03-22 2013-03-20 小分子ｇｌｐ１ｒアゴニストのトリス（ヒドロキシメチル）アミノメタン塩ならびにその医薬組成物および使用 Ceased JP2015510947A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261614265P 2012-03-22 2012-03-22
US61/614,265 2012-03-22
PCT/US2013/033091 WO2013142569A1 (en) 2012-03-22 2013-03-20 Tris(hydroxymethyl)aminomethane salts of a small-molecule glp1r agonist and pharmaceutical compositions and uses thereof

Publications (2)

Publication Number Publication Date
JP2015510947A true JP2015510947A (ja) 2015-04-13
JP2015510947A5 JP2015510947A5 (OSRAM) 2016-05-19

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JP2015501876A Ceased JP2015510947A (ja) 2012-03-22 2013-03-20 小分子ｇｌｐ１ｒアゴニストのトリス（ヒドロキシメチル）アミノメタン塩ならびにその医薬組成物および使用

Country Status (16)

Country Link
US (1) US9198901B2 (OSRAM)
EP (1) EP2854526B1 (OSRAM)
JP (1) JP2015510947A (OSRAM)
KR (1) KR102158992B1 (OSRAM)
CN (1) CN104202977A (OSRAM)
AU (1) AU2013235167B2 (OSRAM)
CA (1) CA2868033A1 (OSRAM)
EA (1) EA201491749A1 (OSRAM)
ES (1) ES2674951T3 (OSRAM)
HK (1) HK1199371A1 (OSRAM)
IL (1) IL234615B (OSRAM)
IN (1) IN2014DN07867A (OSRAM)
MX (1) MX352804B (OSRAM)
NZ (1) NZ629203A (OSRAM)
SG (1) SG11201405353VA (OSRAM)
WO (1) WO2013142569A1 (OSRAM)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021523877A (ja) * 2018-05-08 2021-09-09 ブイティーブイ・セラピューティクス・エルエルシー Ｇｌｐ１ｒアゴニストの治療的使用

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4141008A4 (en) 2020-04-01 2024-04-17 Hangzhou Zhongmei Huadong Pharmaceutical Co., Ltd. PHARMACEUTICALLY ACCEPTABLE ACID SALT OF GLP-1 RECEPTOR AGONIST FREE BASE, AND PREPARATION METHOD THEREFOR
JP2023528565A (ja) 2020-04-01 2023-07-05 ハンジョウ ジョンメイ フアドン ファーマシューティカル シーオー．，エルティーディー． Ｇｌｐ－１受容体アゴニストの結晶形ａおよびその調製法
AU2024340407A1 (en) 2023-09-14 2026-04-23 Ascletis Pharma (China) Co., Limited Glp-1r agonist and therapeutic method thereof
WO2025109387A1 (en) 2023-11-24 2025-05-30 Ascletis Pharma (China) Co., Limited Glp-1r agonist and therapeutic method thereof
WO2025158275A1 (en) 2024-01-24 2025-07-31 Pfizer Inc. Combination therapy using glucose-dependent insulinotropic polypeptide receptor antagonist compounds and glp-1 receptor agonist compounds

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JP2004520393A (ja) * 2001-02-05 2004-07-08 ドクター・レディーズ・ラボラトリーズ・リミテッド ヘテロ環化号物の薬学的に許容可能な塩
JP2005511558A (ja) * 2001-10-30 2005-04-28 アプライド リサーチ システムズ エーアールエス ホールディング ナームロゼ フェンノートシャップ タンパク質チロシンホスファターゼのオキシンドールヒドラジンモジュレータ
JP2006523724A (ja) * 2003-04-18 2006-10-19 インサイト サン ディエゴ インコーポレイテッド 代謝障害、癌および他の疾患の治療のための置換イソクロマン化合物
WO2009111700A2 (en) * 2008-03-07 2009-09-11 Transtech Pharma, Inc. Oxadiazoanthracene compounds for the treatment of diabetes
WO2009123241A1 (ja) * 2008-03-31 2009-10-08 株式会社レナサイエンス プラスミノーゲンアクチベーターインヒビター－１阻害剤
WO2009148052A1 (ja) * 2008-06-05 2009-12-10 旭化成ファーマ株式会社 スルホンアミド化合物及びその用途
WO2010068581A1 (en) * 2008-12-08 2010-06-17 Glaxosmithkline Llc Novel compounds
US20110064806A1 (en) * 2009-09-11 2011-03-17 Transtech Pharma, Inc. Solid compositions comprising an oxadiazoanthracene compound and methods of making and using the same

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JP2004520393A (ja) * 2001-02-05 2004-07-08 ドクター・レディーズ・ラボラトリーズ・リミテッド ヘテロ環化号物の薬学的に許容可能な塩
JP2005511558A (ja) * 2001-10-30 2005-04-28 アプライド リサーチ システムズ エーアールエス ホールディング ナームロゼ フェンノートシャップ タンパク質チロシンホスファターゼのオキシンドールヒドラジンモジュレータ
JP2006523724A (ja) * 2003-04-18 2006-10-19 インサイト サン ディエゴ インコーポレイテッド 代謝障害、癌および他の疾患の治療のための置換イソクロマン化合物
WO2009111700A2 (en) * 2008-03-07 2009-09-11 Transtech Pharma, Inc. Oxadiazoanthracene compounds for the treatment of diabetes
US20100324033A1 (en) * 2008-03-07 2010-12-23 Transtech Pharma, Inc. Oxadiazoanthracene compounds for the treatment of diabetes
JP2011513431A (ja) * 2008-03-07 2011-04-28 トランス テック ファーマ，インコーポレイテッド 糖尿病の治療のためのオキサジアゾアントラセン化合物
WO2009123241A1 (ja) * 2008-03-31 2009-10-08 株式会社レナサイエンス プラスミノーゲンアクチベーターインヒビター－１阻害剤
WO2009148052A1 (ja) * 2008-06-05 2009-12-10 旭化成ファーマ株式会社 スルホンアミド化合物及びその用途
WO2010068581A1 (en) * 2008-12-08 2010-06-17 Glaxosmithkline Llc Novel compounds
US20110064806A1 (en) * 2009-09-11 2011-03-17 Transtech Pharma, Inc. Solid compositions comprising an oxadiazoanthracene compound and methods of making and using the same

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021523877A (ja) * 2018-05-08 2021-09-09 ブイティーブイ・セラピューティクス・エルエルシー Ｇｌｐ１ｒアゴニストの治療的使用
JP2024112903A (ja) * 2018-05-08 2024-08-21 ブイティーブイ・セラピューティクス・エルエルシー Ｇｌｐ１ｒアゴニストの治療的使用

Also Published As

Publication number Publication date
WO2013142569A1 (en) 2013-09-26
EA201491749A1 (ru) 2015-01-30
AU2013235167B2 (en) 2017-03-30
ES2674951T8 (es) 2018-08-23
AU2013235167A1 (en) 2014-09-18
HK1199371A1 (en) 2015-07-03
KR102158992B1 (ko) 2020-09-23
IN2014DN07867A (OSRAM) 2015-04-24
US20150005339A1 (en) 2015-01-01
KR20140138758A (ko) 2014-12-04
IL234615B (en) 2018-02-28
MX352804B (es) 2017-12-08
US9198901B2 (en) 2015-12-01
CA2868033A1 (en) 2013-09-26
MX2014010366A (es) 2015-05-15
EP2854526B1 (en) 2018-04-25
SG11201405353VA (en) 2014-09-26
ES2674951T3 (es) 2018-07-05
EP2854526A4 (en) 2016-02-24
EP2854526A1 (en) 2015-04-08
CN104202977A (zh) 2014-12-10
NZ629203A (en) 2015-12-24

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