BR112012014475A2 - derivados de glp-acilados. - Google Patents

derivados de glp-acilados.

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Publication number
BR112012014475A2
BR112012014475A2 BR112012014475A BR112012014475A BR112012014475A2 BR 112012014475 A2 BR112012014475 A2 BR 112012014475A2 BR 112012014475 A BR112012014475 A BR 112012014475A BR 112012014475 A BR112012014475 A BR 112012014475A BR 112012014475 A2 BR112012014475 A2 BR 112012014475A2
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BR
Brazil
Prior art keywords
integer
glp
range
chemical
residue
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BR112012014475A
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English (en)
Other versions
BR112012014475A8 (pt
Inventor
Spetzler Jane
Lau Jesper
Tibor Kodra János
Linderoth Lars
William Garibay Patrick
Sauerberg Per
Original Assignee
Novo Nordisk As
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Publication of BR112012014475A2 publication Critical patent/BR112012014475A2/pt
Publication of BR112012014475A8 publication Critical patent/BR112012014475A8/pt

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    • 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
    • C07K14/65—Insulin-like growth factors (Somatomedins), e.g. IGF-1, IGF-2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A61K38/26—Glucagons
    • 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
    • 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
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
    • 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
    • A61K47/56—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • 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
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • 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
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/575—Hormones
    • G01N2333/605—Glucagons

Abstract

derivados de glp-1 duplo-acilados - a presente invenção refere-se a um derivado de um análogo de glp-1, cujo análogo compreende um primeiro resíduo k em uma posição correspondente à posição 37 de glp-1(7-37) (seq id no:1), um segundo resíduo k em uma posição correspondente à posição 26 de glp-1(7-37), e um máximo de vez modificações de aminoácidos em comparação com glp-1(7-37), em que o primeiro resíduo k é designado k ^37^, e segundo resíduo k é designado k ^26^, cujo derivado compreende duas porções de ligação de albumina anexadas a k ^26^ e k ^37^, respectivamente, em que a porção de ligação de albumina compreende uma porção de protração selecionada entre: produto químico 1: hooc-(ch ~2~)~-co-* produto químico 2: hooc-c~6~h ~4~-o-(ch ~2~)~-co-* produto químico 3: r ~1~c~h~-(ch ~2~)~-co-* produto químico 4: hooc- c ~4~sh~ 2~-(ch~ 2~)~ w~-co-* na qual x é um inteiro na faixa d 6 a 18, y é um inteiro na faixa de 3 a 17, z é um inteiro na faixa de 1 a 5, r ~1~ é um grupamento tendo uma massa molar não maior do que 150 da, e w é um inteiro na faixa de 6 a 18; com a condição de que quando a porção de protração é o produto químico 1, a porção de ligação de albumina compreende adicionalmente um encadeador de fórmula do produto químico 5: *-nh-(ch ~)~- (o- (ch~)~)~-o-o(ch~)~-co-*, em que k é um inteiro na faixa de 1 a 5, e n é um inteiro na faixa de 1 a 5; ou um sinal, amida, ou éster farmaceuticamente aceitável do mesmo. a invenção também se refere à aplicação farmacêutica do mesmo, por exemplo do tratamento e/ou na prevenção de todas as formas de diabetes e doenças relacionadas bem como a novos peptídeos correspondentes e intermediários de cadeia lateral. os derivados são adequados para administração oral.
BR112012014475A 2009-12-16 2010-12-16 derivados de glp-1 duplo-acilados. BR112012014475A8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09179390 2009-12-16
US28860109P 2009-12-21 2009-12-21
PCT/EP2010/069932 WO2011080103A1 (en) 2009-12-16 2010-12-16 Double-acylated glp-1 derivatives

Publications (2)

Publication Number Publication Date
BR112012014475A2 true BR112012014475A2 (pt) 2018-04-24
BR112012014475A8 BR112012014475A8 (pt) 2018-07-03

Family

ID=41800497

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BR112012014475A BR112012014475A8 (pt) 2009-12-16 2010-12-16 derivados de glp-1 duplo-acilados.

Country Status (19)

Country Link
US (4) US20120329711A1 (pt)
EP (4) EP2513140B1 (pt)
JP (5) JP6006118B2 (pt)
KR (1) KR101817607B1 (pt)
CN (6) CN111560060A (pt)
AU (1) AU2010338387B2 (pt)
BR (1) BR112012014475A8 (pt)
CA (1) CA2784757A1 (pt)
DK (1) DK2513140T3 (pt)
ES (2) ES2561658T3 (pt)
HU (1) HUE027229T2 (pt)
IL (1) IL219945A (pt)
MX (1) MX2012006634A (pt)
PL (1) PL2513140T3 (pt)
PT (1) PT2513140E (pt)
RU (1) RU2559540C2 (pt)
TW (1) TWI484974B (pt)
WO (3) WO2011073328A1 (pt)
ZA (1) ZA201204436B (pt)

Families Citing this family (114)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2240155B1 (en) 2008-02-13 2012-06-06 Intarcia Therapeutics, Inc Devices, formulations, and methods for delivery of multiple beneficial agents
PE20121130A1 (es) 2009-07-13 2012-08-30 Zealand Pharma As Analogos de glucagon acilados
EP3323423B1 (en) 2009-09-28 2020-06-17 Intarcia Therapeutics, Inc Rapid establishment and/or termination of substantial steady-state drug delivery
JP6006118B2 (ja) * 2009-12-16 2016-10-12 ノヴォ ノルディスク アー／エス Ｇｌｐ−１アナログ及び誘導体
JP6039569B2 (ja) 2010-11-09 2016-12-07 ノヴォ ノルディスク アー／エス 二重アシル化されたｇｌｐ−１誘導体
KR101925620B1 (ko) 2010-12-16 2018-12-05 노보 노르디스크 에이/에스 Ｇｌｐ-1 아고니스트 및 ｎ-(8-(2-히드록시벤조일)아미노)카프릴산의 염을 포함하는 고체 조성물
US20120208755A1 (en) * 2011-02-16 2012-08-16 Intarcia Therapeutics, Inc. Compositions, Devices and Methods of Use Thereof for the Treatment of Cancers
US9266940B2 (en) 2011-04-12 2016-02-23 Novo Nordisk A/S Double-acylated GLP-1 derivatives
CN103930134B (zh) 2011-07-18 2016-12-21 阿茨生物股份有限公司 长效促黄体激素(lh)化合物
EP2753642B8 (en) * 2011-09-06 2017-12-13 Novo Nordisk A/S Glp-1 derivatives
CN104011064A (zh) 2011-12-29 2014-08-27 诺沃—诺迪斯克有限公司 包含非成蛋白质性的氨基酸的二肽
ES2810153T3 (es) * 2012-03-01 2021-03-08 Novo Nordisk As Profármacos de GLP-1
DK2827845T3 (en) 2012-03-22 2019-04-01 Novo Nordisk As COMPOSITIONS INCLUDING A PROCEDURE AND PREPARING THEREOF
EP2827885B1 (en) 2012-03-22 2018-08-15 Novo Nordisk A/S Compositions of glp-1 peptides and preparation thereof
US10100097B2 (en) 2012-05-03 2018-10-16 Zealand Pharma A/S GIP-GLP-1 dual agonist compounds and methods
JP6366575B2 (ja) * 2012-05-08 2018-08-01 ノヴォ ノルディスク アー／エス 二重アシル化されたｇｌｐ−１誘導体
JP6250034B2 (ja) * 2012-05-08 2017-12-20 ノヴォ ノルディスク アー／エス 二重アシル化されたｇｌｐ−１誘導体
US9745359B2 (en) 2012-05-18 2017-08-29 Adda Biotech Inc. Protein and protein conjugate for diabetes treatment, and applications thereof
ES2871328T3 (es) 2012-06-20 2021-10-28 Novo Nordisk As Formulación de comprimido que comprende un péptido y un agente de suministro
RS60432B1 (sr) * 2012-07-01 2020-07-31 Novo Nordisk As Upotreba glp-1 peptida sa dugim dejstvom
DK2875043T3 (en) 2012-07-23 2017-03-27 Zealand Pharma As glucagon
FR2994848B1 (fr) 2012-08-30 2014-08-22 Univ Paris Curie Traitement de l'arthrose par les hormones incretines ou leurs analogues
TWI608013B (zh) 2012-09-17 2017-12-11 西蘭製藥公司 升糖素類似物
UA116217C2 (uk) 2012-10-09 2018-02-26 Санофі Пептидна сполука як подвійний агоніст рецепторів glp1-1 та глюкагону
US9637517B2 (en) 2012-10-31 2017-05-02 Hybio Pharmaceutical Co., Ltd. Method for preparing exenatide
UA116553C2 (uk) 2012-12-21 2018-04-10 Санофі Пептидна сполука - агоніст рецептора glp-1 i glp
KR20210086717A (ko) * 2013-05-02 2021-07-08 노보 노르디스크 에이/에스 Glp-1 화합물의 경구 투여
ES2646538T3 (es) * 2013-06-20 2017-12-14 Novo Nordisk A/S Derivados de GLP-1 y sus usos
CN105377884B (zh) * 2013-07-04 2021-07-20 诺和诺德股份有限公司 Glp-1样肽的衍生物和其用途
US10266577B2 (en) 2013-08-15 2019-04-23 Novo Nordisk A/S GLP-1 derivatives, and uses thereof
US10286078B2 (en) 2013-09-13 2019-05-14 The California Institute For Biomedical Research Modified therapeutic agents and compositions thereof
US9988429B2 (en) 2013-10-17 2018-06-05 Zealand Pharma A/S Glucagon analogues
EA034322B1 (ru) 2013-10-17 2020-01-28 Зилэнд Фарма А/С Ацилированные аналоги глюкагона
WO2015067716A1 (en) 2013-11-06 2015-05-14 Zealand Pharma A/S Glucagon-glp-1-gip triple agonist compounds
TWI670281B (zh) 2013-11-06 2019-09-01 西蘭製藥公司 Ｇｉｐ－ｇｌｐ－１雙重促效劑化合物及方法
EP3077008B1 (en) 2013-12-06 2023-10-04 Jie Han Bioreversable promoieties for nitrogen-containing and hydroxyl-containing drugs
TW201609796A (zh) 2013-12-13 2016-03-16 賽諾菲公司 非醯化之艾塞那肽－４（ｅｘｅｎｄｉｎ－４）胜肽類似物
TW201609799A (zh) 2013-12-13 2016-03-16 賽諾菲公司 雙重ｇｌｐ－１／ｇｉｐ受體促效劑
EP3080150B1 (en) 2013-12-13 2018-08-01 Sanofi Exendin-4 peptide analogues as dual glp-1/gip receptor agonists
TW201609797A (zh) 2013-12-13 2016-03-16 賽諾菲公司 雙重ｇｌｐ－１／升糖素受體促效劑
US10039809B2 (en) 2013-12-18 2018-08-07 The California Institute For Biomedical Research Modified therapeutic agents, stapled peptide lipid conjugates, and compositions thereof
CN106132985B (zh) * 2014-04-07 2020-10-13 诺和诺德股份有限公司 双酰化glp-1化合物
TW201625668A (zh) 2014-04-07 2016-07-16 賽諾菲公司 作為胜肽性雙重ｇｌｐ－１／昇糖素受體激動劑之艾塞那肽－４衍生物
TW201625670A (zh) 2014-04-07 2016-07-16 賽諾菲公司 衍生自ｅｘｅｎｄｉｎ－４之雙重ｇｌｐ－１／升糖素受體促效劑
TW201625669A (zh) 2014-04-07 2016-07-16 賽諾菲公司 衍生自艾塞那肽－４（Ｅｘｅｎｄｉｎ－４）之肽類雙重ＧＬＰ－１／升糖素受體促效劑
BR112016029076B1 (pt) 2014-06-12 2024-02-15 Ra Pharmaceuticals, Inc Polipeptídeo e composição compreendendo o mesmo para inibir a clivagem de c5 em um sistema celular
US9932381B2 (en) 2014-06-18 2018-04-03 Sanofi Exendin-4 derivatives as selective glucagon receptor agonists
US9889085B1 (en) 2014-09-30 2018-02-13 Intarcia Therapeutics, Inc. Therapeutic methods for the treatment of diabetes and related conditions for patients with high baseline HbA1c
MX2017005457A (es) 2014-10-29 2017-07-04 Zealand Pharma As Metodos y compuestos agonistas de gip.
ES2739289T3 (es) * 2014-11-27 2020-01-30 Novo Nordisk As Derivados de GLP-1 y sus usos
JP6691125B2 (ja) 2014-12-17 2020-04-28 ノヴォ ノルディスク アー／エス Ｇｌｐ−１誘導体及びその使用
PL3250230T3 (pl) 2015-01-28 2022-02-14 Ra Pharmaceuticals, Inc. Modulatory aktywności dopełniacza
CN107205948B (zh) * 2015-01-29 2021-12-14 诺和诺德股份有限公司 包含glp-1激动剂和肠溶衣的片剂
WO2016120380A1 (en) * 2015-01-29 2016-08-04 Novo Nordisk A/S Pharmaceutical composition for oral glp-1 administration comprising a tablet core and immediate release coating
KR20170137198A (ko) 2015-04-16 2017-12-12 질랜드 파마 에이/에스 아실화된 글루카곤 유사체
AU2016270984B2 (en) 2015-06-03 2021-02-25 Intarcia Therapeutics, Inc. Implant placement and removal systems
EP3302465A1 (en) 2015-06-05 2018-04-11 Vertex Pharmaceuticals Incorporated Triazoles for the treatment of demyelinating diseases
AR105319A1 (es) 2015-06-05 2017-09-27 Sanofi Sa Profármacos que comprenden un conjugado agonista dual de glp-1 / glucagón conector ácido hialurónico
SI3319959T1 (sl) 2015-07-06 2022-02-28 Alkermes, Inc. Hetero-halo inhibitorji histonske deacetilaze
US10421756B2 (en) 2015-07-06 2019-09-24 Rodin Therapeutics, Inc. Heterobicyclic N-aminophenyl-amides as inhibitors of histone deacetylase
AR105284A1 (es) 2015-07-10 2017-09-20 Sanofi Sa Derivados de exendina-4 como agonistas peptídicos duales específicos de los receptores de glp-1 / glucagón
CN106496322A (zh) * 2015-09-07 2017-03-15 江苏恒瑞医药股份有限公司 人胰岛素或其类似物的酰化衍生物的制备方法
CN108473547A (zh) * 2015-10-28 2018-08-31 塔夫茨大学 具有改良的蛋白质分解安定性的新颖多肽，以及制备与使用该新颖多肽的方法
CA3007772A1 (en) 2015-12-16 2017-06-22 Ra Pharmaceuticals, Inc. Modulators of complement activity
GB2551945B (en) * 2015-12-18 2021-09-08 Heptares Therapeutics Ltd Novel GLP-1 receptor agonist peptides
ES2835033T3 (es) 2016-03-03 2021-06-21 Novo Nordisk As Derivados de GLP-1 y sus usos
KR20240037175A (ko) 2016-05-16 2024-03-21 인타르시아 세라퓨틱스 인코포레이티드 글루카곤-수용체 선택적 폴리펩티드 및 이들의 이용 방법
USD840030S1 (en) 2016-06-02 2019-02-05 Intarcia Therapeutics, Inc. Implant placement guide
USD860451S1 (en) 2016-06-02 2019-09-17 Intarcia Therapeutics, Inc. Implant removal tool
CN107561168A (zh) * 2016-06-30 2018-01-09 山东新时代药业有限公司 一种聚乙二醇化促胰岛素分泌肽类似物的分析检测方法
ES2828526T3 (es) 2016-11-07 2021-05-26 Novo Nordisk As Esteres activos DCHBS de compuestos PEG y sus usos
WO2018106643A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Heterocyclic azoles for the treatment of demyelinating diseases
WO2018106641A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Pyrazoles for the treatment of demyelinating diseases
WO2018106646A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Aminotriazoles for the treatment of demyelinating diseases
MX2019006527A (es) 2016-12-07 2019-08-01 Ra Pharmaceuticals Inc Moduladores de la actividad del complemento.
IL307966A (en) 2017-01-03 2023-12-01 Intarcia Therapeutics Inc Methods involving continuous administration of a GLP-1 receptor agonist and co-administration of a drug
MD3570834T2 (ro) 2017-01-11 2022-04-30 Alkermes Inc Inhibitori biciclici ai histon deacetilazei
FR3061715B1 (fr) * 2017-01-12 2021-07-30 Institut National Univ Jean Francois Champollion Peptide immunomodulateur
WO2018165462A1 (en) * 2017-03-08 2018-09-13 Intarcia Therapeutics, Inc Apparatus and methods for administration of a nauseogenic compound from a drug delivery device
TWI797133B (zh) 2017-06-09 2023-04-01 丹麥商諾佛 儂迪克股份有限公司 用於經口投予的固體組成物
MA49839B1 (fr) 2017-08-07 2022-05-31 Alkermes Inc Inhibiteurs bicycliques de la histone déacétylase
AU2018321157B2 (en) 2017-08-24 2024-03-28 Novo Nordisk A/S GLP-1 compositions and uses thereof
CN117018216A (zh) * 2017-09-19 2023-11-10 免疫功坊股份有限公司 与白蛋白具有较佳结合亲和力的药物分子
PL3746111T3 (pl) 2018-02-02 2024-01-15 Novo Nordisk A/S Stałe kompozycje zawierające agonistę glp-1 i sól kwasu n-(8-(2- hydroksybenzoilo)amino kaprylowego i substancję poślizgową
CA3095988A1 (en) 2018-04-05 2019-10-10 Sun Pharmaceutical Industries Limited Novel glp-1 analogues
US10604555B2 (en) * 2018-05-04 2020-03-31 Novo Nordisk A/S GIP derivatives and uses thereof
TWI829687B (zh) 2018-05-07 2024-01-21 丹麥商諾佛 儂迪克股份有限公司 包含glp-1促效劑與n-(8-(2-羥基苯甲醯基)胺基)辛酸之鹽的固體組成物
CN109111361A (zh) * 2018-10-08 2019-01-01 扬州工业职业技术学院 一种一步法高效制备十二烷基二酸单叔丁酯的方法
CN109134257A (zh) * 2018-10-08 2019-01-04 扬州工业职业技术学院 一种两步法制备高纯度十二烷基二酸单叔丁酯的方法
WO2020118843A1 (zh) * 2018-12-12 2020-06-18 四川利通科创生物医药科技有限公司 一种glp-1突变体及其制备方法和用途
US20220072493A1 (en) 2019-01-24 2022-03-10 Novo Nordisk A/S Roller compactor and method of dry granulation using a roller compactor
WO2020180534A1 (en) 2019-03-01 2020-09-10 President And Fellows Of Harvard College Methods and compositions for protein delivery
CN113939273A (zh) 2019-04-03 2022-01-14 哈佛大学校长及研究员协会 用于药物递送的离子液体
WO2021070202A1 (en) * 2019-10-09 2021-04-15 Prasad Alaparthi Lakshmi A method for preparing glp-1 analogue by solid-phase peptide synthesis
MX2022004779A (es) 2019-11-06 2022-06-14 Novo Nordisk As Agonistas del receptor del péptido 1 similar al glucagón (glp-1) en demencia.
JP2023502004A (ja) 2019-11-07 2023-01-20 ノヴォ ノルディスク アー／エス Ｇｌｐ－１作動薬、ｓｇｌｔ２阻害剤、およびｎ－（８－（２－ヒドロキシベンゾイル）アミノ）カプリル酸の塩を含む固形組成物
IL293145A (en) 2019-11-22 2022-07-01 Harvard College Ionic liquids for drug delivery
CN116925237A (zh) 2019-12-31 2023-10-24 北京质肽生物医药科技有限公司 Glp-1和gdf15的融合蛋白以及其缀合物
IL294520A (en) 2020-02-18 2022-09-01 Novo Nordisk As Pharmaceutical formulations
JP2023524695A (ja) 2020-04-29 2023-06-13 ノヴォ ノルディスク アー／エス Ｇｌｐ－１作動薬およびヒスチジンを含む固形組成物
CA3180215A1 (en) * 2020-05-29 2021-12-02 Beijing Tuo Jie Biopharmaceutical Co. Ltd. Dual-agonist compound for both glp-1 and gip receptors and application thereof
EP4181946A1 (en) * 2020-07-18 2023-05-24 Dr. Reddy's Laboratories Ltd. Improved purification process of semaglutide
EP4185607A1 (en) 2020-07-22 2023-05-31 Novo Nordisk A/S Co-agonists at glp-1 and gip receptors suitable for oral delivery
CA3193453A1 (en) 2020-09-30 2022-04-07 Beijing Ql Biopharmaceutical Co., Ltd. Polypeptide conjugates and methods of uses
AU2021374823A1 (en) 2020-11-06 2023-05-25 Novo Nordisk A/S Glp-1 prodrugs and uses hereof
TW202227474A (zh) * 2020-12-18 2022-07-16 丹麥商諾佛 儂迪克股份有限公司 Ｇｌｐ－１及澱粉素受體之共促效劑
CN114685644A (zh) * 2020-12-29 2022-07-01 苏州康宁杰瑞生物科技有限公司 一种人glp-1多肽变体及其应用
WO2022175384A1 (en) * 2021-02-17 2022-08-25 Fundación Universidad Católica De Valencia San Vicente Mártir Small-molecule agents with antiviral activity against rna viruses
WO2023012263A1 (en) 2021-08-04 2023-02-09 Novo Nordisk A/S Solid oral peptide formulations
CA3233824A1 (en) 2021-10-08 2023-04-13 Samir Mitragotri Ionic liquids for drug delivery
TW202330584A (zh) 2022-01-20 2023-08-01 丹麥商諾佛 儂迪克股份有限公司 前藥及其用途
TW202346324A (zh) 2022-05-10 2023-12-01 丹麥商諾佛 儂迪克股份有限公司 前藥及其用途
WO2024003313A1 (en) 2022-06-30 2024-01-04 Sanofi New peptides as selective il-23 receptor antagonists
CN115785249B (zh) * 2022-10-13 2023-07-21 江苏师范大学 一类glp-1类似物及其应用

Family Cites Families (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5545618A (en) 1990-01-24 1996-08-13 Buckley; Douglas I. GLP-1 analogs useful for diabetes treatment
ATE164852T1 (de) * 1990-01-24 1998-04-15 Douglas I Buckley Glp-1-analoga verwendbar in der diabetesbehandlung
US5336782A (en) 1991-04-24 1994-08-09 Kuraray Co., Ltd. Long chain carboxylic acid imide ester
US5512549A (en) 1994-10-18 1996-04-30 Eli Lilly And Company Glucagon-like insulinotropic peptide analogs, compositions, and methods of use
US5869602A (en) 1995-03-17 1999-02-09 Novo Nordisk A/S Peptide derivatives
PT944648E (pt) 1996-08-30 2007-06-26 Novo Nordisk As Derivados do glp-1.
US6458924B2 (en) 1996-08-30 2002-10-01 Novo Nordisk A/S Derivatives of GLP-1 analogs
JP2002506792A (ja) 1998-02-27 2002-03-05 ノボ ノルディスク アクティーゼルスカブ Ｎ末端修飾ｇｌｐ−１誘導体
DE69942306D1 (de) * 1998-02-27 2010-06-10 Novo Nordisk As Abkömmlinge von glp-1 analogen
AU2610599A (en) 1998-02-27 1999-09-15 Novo Nordisk A/S N-terminally truncated glp-1 derivatives
EP1932535A3 (en) 1998-07-31 2008-10-29 Novo Nordisk A/S Stimulation of beta cell profileration
MY155270A (en) 1998-09-24 2015-09-30 Lilly Co Eli Use of glp-1 or analogs in treatment of stroke
US20050148497A1 (en) 2002-02-20 2005-07-07 Khan Mohammed A. Method for administering glp-1 molecules
WO2004067548A2 (en) 2003-01-31 2004-08-12 Theratechnologies Inc. Chemically modified metabolites of regulatory peptides and methods of producing and using same
UA92451C2 (en) 2003-03-19 2010-11-10 Эли Лилли Энд Компани Polyethelene glycol link glp-1 compounds
US20070161087A1 (en) 2003-05-29 2007-07-12 Wolfgang Glaesner Glp-1 fusion proteins
EP1654004A2 (en) * 2003-08-08 2006-05-10 Novo Nordisk A/S Synthesis and application of new structural well defined branched polymers as conjugating agents for peptides
KR101241862B1 (ko) 2003-09-19 2013-03-13 노보 노르디스크 에이/에스 신규 ｇｌｐ-1 유도체
DE602004026113D1 (de) 2003-12-18 2010-04-29 Novo Nordisk As Glp-1-verbindungen
CN1893980A (zh) 2003-12-18 2007-01-10 诺沃挪第克公司 与白蛋白样物质相连的新glp－1类似物
US20060286129A1 (en) 2003-12-19 2006-12-21 Emisphere Technologies, Inc. Oral GLP-1 formulations
WO2005121090A1 (en) 2004-06-02 2005-12-22 Abbott Laboratories Substituted piperidines that have antiangiogenic activity
WO2006005667A2 (en) 2004-07-08 2006-01-19 Novo Nordisk A/S Polypeptide protracting tags comprising a tetrazole moiety
WO2006082204A1 (en) 2005-02-02 2006-08-10 Novo Nordisk A/S Insulin derivatives
WO2006096515A2 (en) 2005-03-04 2006-09-14 Biorexis Pharmaceutical Corporation Modified transferrin fusion proteins
TWI362392B (en) * 2005-03-18 2012-04-21 Novo Nordisk As Acylated glp-1 compounds
US8603972B2 (en) * 2005-03-18 2013-12-10 Novo Nordisk A/S Extended GLP-1 compounds
EA012442B1 (ru) 2005-05-13 2009-10-30 Эли Лилли Энд Компани Пегилированные соединения glp-1
AU2006249869A1 (en) * 2005-05-26 2006-11-30 Bristol-Myers Squibb Company N-terminally modified GLP-1 receptor modulators
CA2649751A1 (en) 2006-04-20 2007-11-01 Amgen Inc. Glp-1 compound/glucagon antibody compositions
US8796205B2 (en) 2006-05-09 2014-08-05 Novo Nordisk A/S Insulin derivative
WO2007128817A2 (en) * 2006-05-09 2007-11-15 Novo Nordisk A/S Insulin derivative
US20090098130A1 (en) * 2007-01-05 2009-04-16 Bradshaw Curt W Glucagon-like protein-1 receptor (glp-1r) agonist compounds
EP2514406A1 (en) 2007-06-01 2012-10-24 Novo Nordisk A/S Spontaneously dispersible preconcentrates including a peptide drug in a solid or semisolid carrier
WO2008154619A1 (en) * 2007-06-12 2008-12-18 Smithkline Beecham Corporation Methods for detecting protein in plasma
ES2672770T3 (es) 2007-09-05 2018-06-18 Novo Nordisk A/S Derivados del péptido-1 similar al glucagón y su uso farmacéutico
JP5606314B2 (ja) * 2007-09-05 2014-10-15 ノボ・ノルデイスク・エー／エス Ａ−ｂ−ｃ−ｄ−で誘導体化されたペプチドとその治療用途
US20100317057A1 (en) * 2007-12-28 2010-12-16 Novo Nordisk A/S Semi-recombinant preparation of glp-1 analogues
EP2340049B1 (en) 2008-09-12 2015-11-11 Novo Nordisk A/S Method of acylating a peptide or protein
US8865759B2 (en) 2008-10-15 2014-10-21 Bayer Intellectual Property Gmbh Use of dithiine-tetracarboximides for controlling phytopathogenic fungi
CN101463081B (zh) * 2009-01-12 2012-07-04 华东师范大学 一种glp-1衍生物
AR077956A1 (es) 2009-09-14 2011-10-05 Bayer Cropscience Ag Combinaciones de compuestos activos
JP6006118B2 (ja) 2009-12-16 2016-10-12 ノヴォ ノルディスク アー／エス Ｇｌｐ−１アナログ及び誘導体
US9266940B2 (en) 2011-04-12 2016-02-23 Novo Nordisk A/S Double-acylated GLP-1 derivatives

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