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TWI799680B - 製備gip/glp1雙重促效劑之方法 - Google Patents

製備gip/glp1雙重促效劑之方法 Download PDF

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Publication number
TWI799680B
TWI799680B TW109102657A TW109102657A TWI799680B TW I799680 B TWI799680 B TW I799680B TW 109102657 A TW109102657 A TW 109102657A TW 109102657 A TW109102657 A TW 109102657A TW I799680 B TWI799680 B TW I799680B
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TW
Taiwan
Prior art keywords
gip
preparing
dual agonist
glp1 dual
glp1
Prior art date
Application number
TW109102657A
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English (en)
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TW202043260A (zh
Inventor
麥可 奥利弗 弗雷德里克
尼爾 約翰 柯曼
麥克 尤金 柯帕克
凱文 戴爾 賽貝特
謝爾蓋 拉迪米羅維奇 處卡若夫
史蒂芬妮 盧斯 科芬
安庫爾 賈藍
Original Assignee
美商美國禮來大藥廠
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Publication of TW202043260A publication Critical patent/TW202043260A/zh
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575Hormones
    • C07K14/645Secretins
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C7/00Purification; Separation; Use of additives
    • C07C7/04Purification; Separation; Use of additives by distillation
    • C07C7/05Purification; Separation; Use of additives by distillation with the aid of auxiliary compounds
    • C07C7/06Purification; Separation; Use of additives by distillation with the aid of auxiliary compounds by azeotropic distillation
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575Hormones
    • C07K14/605Glucagons
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/08Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K1/00General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
    • C07K1/113General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides without change of the primary structure
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/001Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof by chemical synthesis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/45Carboxylic 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
    • C07C233/46Carboxylic 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 an acyclic carbon atom
    • C07C233/47Carboxylic 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 an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Toxicology (AREA)
  • Endocrinology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Analytical Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Water Supply & Treatment (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Epoxy Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
TW109102657A 2019-01-29 2020-01-22 製備gip/glp1雙重促效劑之方法 TWI799680B (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201962797963P 2019-01-29 2019-01-29
US62/797,963 2019-01-29
US201962815053P 2019-03-07 2019-03-07
US62/815,053 2019-03-07
US201962818342P 2019-03-14 2019-03-14
US62/818,342 2019-03-14

Publications (2)

Publication Number Publication Date
TW202043260A TW202043260A (zh) 2020-12-01
TWI799680B true TWI799680B (zh) 2023-04-21

Family

ID=69724140

Family Applications (1)

Application Number Title Priority Date Filing Date
TW109102657A TWI799680B (zh) 2019-01-29 2020-01-22 製備gip/glp1雙重促效劑之方法

Country Status (18)

Country Link
US (2) US20220135639A1 (zh)
EP (1) EP3917950A1 (zh)
JP (2) JP7315683B2 (zh)
KR (1) KR20210110349A (zh)
CN (1) CN113330024A (zh)
AU (4) AU2020216922A1 (zh)
BR (1) BR112021012368A2 (zh)
CA (2) CA3224820A1 (zh)
CL (2) CL2021001905A1 (zh)
CO (1) CO2021009662A2 (zh)
EC (1) ECSP21056124A (zh)
IL (1) IL284446A (zh)
MA (1) MA54862A (zh)
MX (1) MX2021008965A (zh)
PE (1) PE20211992A1 (zh)
SG (1) SG11202107123TA (zh)
TW (1) TWI799680B (zh)
WO (1) WO2020159949A1 (zh)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110642935A (zh) * 2019-09-25 2020-01-03 成都奥达生物科技有限公司 一种替瑞帕肽类似物
EP4257597A1 (en) * 2020-12-02 2023-10-11 Dongbao Purple Star (Hangzhou) Biopharmaceutical Co., Ltd. Lactam-modified polypeptide compounds
MX2023008330A (es) * 2021-01-20 2024-01-18 Viking Therapeutics Inc Agonistas del receptor dual gip/glp-1 de molécula pequeña, composiciones farmacéuticas y preparación de las mismas para usarse en el tratamiento de trastornos metabólicos y hepáticos.
BR112023019389A2 (pt) * 2021-03-25 2023-11-28 Brightgene Bio Medical Tech Co Ltd Compostos, agonista de receptor duplo de gip e glp-1, composição farmacêutica compreendendo os mesmos, uso dos mesmos e método para prevenir e/ou tratar doenças associadas a distúrbios metabólicos
TWI827077B (zh) * 2021-05-28 2023-12-21 大陸商廣東眾生睿創生物科技有限公司 多肽的製備及其應用
WO2023089594A1 (en) 2021-11-22 2023-05-25 Sun Pharmaceutical Industries Limited Process for the preparation of tirzepatide or pharmaceutically acceptable salt thereof
TW202404996A (zh) 2022-04-04 2024-02-01 美商美國禮來大藥廠 製備glp-1/升糖素雙重促效劑之方法
CN116023444B (zh) * 2022-08-12 2023-08-01 重庆宸安生物制药有限公司 一种gip和glp-1双受体激动剂多肽化合物及其应用
WO2024077149A2 (en) * 2022-10-05 2024-04-11 Eli Lilly And Company Peptides for incretin synthesis
WO2024112617A2 (en) 2022-11-21 2024-05-30 Eli Lilly And Company Process for preparing a gip/glp1 dual agonist
WO2024134676A1 (en) * 2022-12-19 2024-06-27 Dr. Reddy’S Laboratories Limited Process for the preparation of tirzepatide
WO2024133236A2 (en) * 2022-12-19 2024-06-27 Forschungsverbund Berlin E.V. Peptide conjugates for labelling endogenous gipr and glp-1r
WO2024136573A1 (ko) * 2022-12-23 2024-06-27 한미약품 주식회사 신규한 glp-1, gip, 및 글루카곤 수용체 모두에 활성을 갖는 삼중 활성체 및 이를 포함하는 비만의 예방 또는 치료용 약학적 조성물
WO2024145638A2 (en) * 2022-12-29 2024-07-04 Eli Lilly And Company Processes and intermediates for preparing tirzepatide
WO2024184352A1 (en) 2023-03-06 2024-09-12 Ascendis Pharma A/S Drug compounds comprising albumin-binding moieties
CN116731154A (zh) * 2023-08-14 2023-09-12 苏州金顶生物有限公司 一种全液相法制备替西帕肽的方法
CN117736273B (zh) * 2023-12-08 2024-05-07 广东省卓肽医药有限公司 一种替尔泊肽的纯化方法

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1076066A1 (en) * 1999-07-12 2001-02-14 Zealand Pharmaceuticals A/S Peptides for lowering blood glucose levels
JP2012525348A (ja) 2009-05-01 2012-10-22 エフ.ホフマン−ラ ロシュ アーゲー 固相及び溶液相の組み合わせ技術を用いたインスリン分泌促進ペプチド合成
JOP20200119A1 (ar) 2015-01-09 2017-06-16 Lilly Co Eli مركبات مساعد مشترك من gip وglp-1
CN106928086B (zh) * 2015-12-31 2019-05-31 深圳翰宇药业股份有限公司 一种长链化合物的制备方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
期刊 Mroz P.A., et al., "Optimized GIP analogs promote body weight lowering in mice through GIPR agonism not antagonism" Molecular metabolism, 20 2019 (Available online: 5 December 2018), page 51–62.

Also Published As

Publication number Publication date
JP2022517834A (ja) 2022-03-10
AU2020216922A1 (en) 2021-07-15
CA3128023A1 (en) 2020-08-06
MA54862A (fr) 2022-05-04
AU2024201004A1 (en) 2024-03-07
IL284446A (en) 2021-08-31
CN113330024A (zh) 2021-08-31
CL2023003709A1 (es) 2024-06-07
US20240368240A1 (en) 2024-11-07
SG11202107123TA (en) 2021-08-30
AU2023203001A1 (en) 2023-06-08
TW202043260A (zh) 2020-12-01
JP7315683B2 (ja) 2023-07-26
MX2021008965A (es) 2021-08-24
CA3224820A1 (en) 2020-08-06
US20220135639A1 (en) 2022-05-05
KR20210110349A (ko) 2021-09-07
AU2024205812A1 (en) 2024-09-05
BR112021012368A2 (pt) 2021-09-14
CL2021001905A1 (es) 2022-03-11
WO2020159949A1 (en) 2020-08-06
AU2023203001B2 (en) 2024-03-28
JP2023078130A (ja) 2023-06-06
PE20211992A1 (es) 2021-10-18
CO2021009662A2 (es) 2021-08-09
ECSP21056124A (es) 2021-08-31
EP3917950A1 (en) 2021-12-08

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