TWI847981B - 類升糖素肽1 (glp-1)融合肽偶合環狀酪酪肽接合物及其用途 - Google Patents

類升糖素肽1 (glp-1)融合肽偶合環狀酪酪肽接合物及其用途 Download PDF

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TWI847981B
TWI847981B TW108114084A TW108114084A TWI847981B TW I847981 B TWI847981 B TW I847981B TW 108114084 A TW108114084 A TW 108114084A TW 108114084 A TW108114084 A TW 108114084A TW I847981 B TWI847981 B TW I847981B
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peptide
glp
conjugate
seq
fusion
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TW108114084A
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Chinese (zh)
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TW202014433A (zh
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越梅 章
勞爾 卡瑪裘
馬丁 卡斯
友善 戚
蘇珊娜 艾達維托
威爾森 愛德華茲
麗莎 諾奎
馬克 沃爾
張瑞
松茂 鄭
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比利時商健生藥品公司
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    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/66—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid the modifying agent being a pre-targeting system involving a peptide or protein for targeting specific cells
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A61K47/645—Polycationic or polyanionic oligopeptides, polypeptides or polyamino acids, e.g. polylysine, polyarginine, polyglutamic acid or peptide TAT
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • 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
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575—Hormones
    • C07K14/57545—Neuropeptide Y
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575—Hormones
    • C07K14/605—Glucagons
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/52—Constant or Fc region; Isotype
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/52—Constant or Fc region; Isotype
    • C07K2317/53—Hinge
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2319/00—Fusion polypeptide
    • C07K2319/30—Non-immunoglobulin-derived peptide or protein having an immunoglobulin constant or Fc region, or a fragment thereof, attached thereto

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Endocrinology (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Toxicology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Cell Biology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
TW108114084A 2018-04-25 2019-04-23 類升糖素肽1 (glp-1)融合肽偶合環狀酪酪肽接合物及其用途 TWI847981B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201862662313P 2018-04-25 2018-04-25
US62/662,313 2018-04-25
WOPCT/US18/29284 2018-04-25
US2018029284 2018-04-25

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TW202014433A TW202014433A (zh) 2020-04-16
TWI847981B true TWI847981B (zh) 2024-07-11

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EP (2) EP4640701A3 (https=)
JP (2) JP7676148B2 (https=)
KR (2) KR20250142942A (https=)
CN (2) CN112004822B (https=)
AU (2) AU2019259790B2 (https=)
BR (1) BR112020021562A2 (https=)
CA (1) CA3096792A1 (https=)
CL (1) CL2020002718A1 (https=)
CO (1) CO2020013221A2 (https=)
CR (1) CR20200487A (https=)
DO (1) DOP2020000192A (https=)
EC (1) ECSP20067968A (https=)
ES (1) ES3049134T3 (https=)
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JO (1) JOP20200265A1 (https=)
MA (1) MA52361A (https=)
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MY (1) MY207588A (https=)
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PE (1) PE20211457A1 (https=)
PH (1) PH12020551659A1 (https=)
SA (1) SA520420401B1 (https=)
SG (1) SG11202009844SA (https=)
TW (1) TWI847981B (https=)
UY (1) UY38200A (https=)
WO (1) WO2019207505A1 (https=)

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JOP20190095A1 (ar) * 2016-10-27 2019-04-28 Janssen Pharmaceutica Nv مركبات ببتيد تيروسين-تيروسين الحلقية كمعدلات لمستقبلات الببتيد العصبي y
CR20220206A (es) 2019-11-11 2022-06-16 Boehringer Ingelheim Int Agonistas del receptor npy2
MX2022006861A (es) * 2019-12-04 2022-07-11 Scripps Research Inst Agonistas del receptor glp2 y metodos de uso.
JP7661478B2 (ja) 2020-08-07 2025-04-14 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 可溶性ｎｐｙ２受容体アゴニスト
CN119638849A (zh) * 2021-10-18 2025-03-18 深圳科兴药业有限公司 一种生长激素融合蛋白及其应用
JP2025504612A (ja) * 2021-12-31 2025-02-13 サンシャイン・レイク・ファーマ・カンパニー・リミテッド Ｇｌｐ－１及びｇｄｆ１５の融合タンパク質並びにその使用
JP2025526148A (ja) 2022-08-18 2025-08-07 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 長時間作用型ｇｌｐ－１／グルカゴン受容体アゴニスト及びｎｐｙ２受容体アゴニストを含む組合せ治療
CN117327200B (zh) * 2023-11-28 2024-02-09 西宝生物科技（上海）股份有限公司 一种调控糖脂代谢和抗衰老的双功能重组蛋白gik及其制备方法
WO2025247862A1 (en) * 2024-05-27 2025-12-04 Numaferm Gmbh Methods for the c-terminal modification of (poly)peptides

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WO2006059106A2 (en) * 2004-12-02 2006-06-08 Domantis Limited Bispecific domain antibodies targeting serum albumin and glp-1 or pyy
WO2008021560A2 (en) * 2006-08-17 2008-02-21 Amylin Pharmaceuticals, Inc. Dpp-iv resistant gip hybrid polypeptides with selectable properties
WO2017075505A2 (en) * 2015-10-28 2017-05-04 Tufts University Novel polypeptides with improved proteolytic stability, and methods of preparing and using same

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JOP20190095A1 (ar) 2016-10-27 2019-04-28 Janssen Pharmaceutica Nv مركبات ببتيد تيروسين-تيروسين الحلقية كمعدلات لمستقبلات الببتيد العصبي y

Patent Citations (3)

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Publication number Priority date Publication date Assignee Title
WO2006059106A2 (en) * 2004-12-02 2006-06-08 Domantis Limited Bispecific domain antibodies targeting serum albumin and glp-1 or pyy
WO2008021560A2 (en) * 2006-08-17 2008-02-21 Amylin Pharmaceuticals, Inc. Dpp-iv resistant gip hybrid polypeptides with selectable properties
WO2017075505A2 (en) * 2015-10-28 2017-05-04 Tufts University Novel polypeptides with improved proteolytic stability, and methods of preparing and using same

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KR20250142942A (ko) 2025-09-30
CO2020013221A2 (es) 2020-11-10
DOP2020000192A (es) 2021-04-30
CN112004822A (zh) 2020-11-27
ES3049134T3 (en) 2025-12-15
JP2025118735A (ja) 2025-08-13
WO2019207505A1 (en) 2019-10-31
CR20200487A (es) 2021-03-11
IL278197B1 (en) 2025-03-01
AU2019259790B2 (en) 2023-08-31
IL319050A (en) 2025-04-01
CN112004822B (zh) 2025-01-14
CA3096792A1 (en) 2019-10-31
JOP20200265A1 (ar) 2020-10-21
IL278197A (en) 2020-11-30
EP3784692A1 (en) 2021-03-03
KR102865076B1 (ko) 2025-09-25
MY207588A (en) 2025-03-05
EP4640701A2 (en) 2025-10-29
KR20210005674A (ko) 2021-01-14
ECSP20067968A (es) 2020-11-30
IL278197B2 (en) 2025-07-01
AU2023274117A1 (en) 2023-12-21
JP2021522258A (ja) 2021-08-30
MX2025014917A (es) 2026-02-03
EP3784692C0 (en) 2025-08-27
SG11202009844SA (en) 2020-11-27
SA520420401B1 (ar) 2023-01-26
UY38200A (es) 2019-10-31
TW202014433A (zh) 2020-04-16
CN119708256A (zh) 2025-03-28
PE20211457A1 (es) 2021-08-05
AU2023274117B2 (en) 2025-04-10
MX2020011293A (es) 2020-11-13
JP7676148B2 (ja) 2025-05-14
MA52361A (fr) 2021-03-03
CL2020002718A1 (es) 2021-01-29
BR112020021562A2 (pt) 2021-03-02
EP4640701A3 (en) 2025-12-17
PH12020551659A1 (en) 2021-07-26
EP3784692B1 (en) 2025-08-27
AU2019259790A1 (en) 2020-10-22
NI202000071A (es) 2021-01-21

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