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AR104479A1 - Conjugados de ácidos grasos y apelina sintética con mayor vida media - Google Patents

Conjugados de ácidos grasos y apelina sintética con mayor vida media

Info

Publication number
AR104479A1
AR104479A1 ARP160100180A ARP160100180A AR104479A1 AR 104479 A1 AR104479 A1 AR 104479A1 AR P160100180 A ARP160100180 A AR P160100180A AR P160100180 A ARP160100180 A AR P160100180A AR 104479 A1 AR104479 A1 AR 104479A1
Authority
AR
Argentina
Prior art keywords
conjugates
heart failure
fatty acid
formula
synthetic
Prior art date
Application number
ARP160100180A
Other languages
English (en)
Inventor
Zecri Frdric
Richardson Usera Aimee
Kanter Aaron
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR104479A1 publication Critical patent/AR104479A1/es

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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
    • A61K47/54—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
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • 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
    • A61K47/50—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
    • 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
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/0402—Organic compounds carboxylic acid carriers, fatty acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • 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
    • C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64—Cyclic peptides containing only normal peptide links

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Zoology (AREA)
  • Toxicology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Neurology (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Child & Adolescent Psychology (AREA)

Abstract

La solicitud proporciona un conjugado o una sal farmacéuticamente aceptable del mismo, que comprende un polipéptido sintético de fórmula (1): Q-R-P-R-L-C*-H-K-G-P-(NIe)-C*-F (1) o una amida o éster del mismo; y un ácido graso seleccionado de los compuestos de fórmula (2) y (3), en el que dicho ácido graso está unido covalentemente al extremo N-terminal del péptido a través de una de sus funcionalidades de ácido carboxílico, opcionalmente a través de un enlazador de polietilenglicol y en el que los dos aminoácidos de cisteína marcados con * forman un enlace disulfuro entre las funcionalidades tiol de su cadena lateral. Los conjugados son agonistas del receptor APJ. También se refiere a un método para la fabricación de los conjugados de la presente y sus usos terapéuticos, tales como el tratamiento o la prevención de insuficiencia cardíaca aguda descompensada (ICAD), insuficiencia cardiaca crónica, hipertensión pulmonar, fibrilación atrial, síndrome de Brugada, taquicardia ventricular, aterosclerosis, hipertensión, restenosis, enfermedades isquémicas cardiovasculares, cardiomiopatía. fibrosis cardiaca, arritmias, retención de agua, diabetes (incluyendo diabetes gestacional), obesidad. enfermedad arterial periférica, accidentes cerebrovasculares, ataques isquémicos transitorios, lesiones cerebrales traumáticas, esclerosis lateral amiotrófica, quemaduras (incluyendo quemaduras de sol) y preeclampsia. La presente proporciona además una combinación de agentes farmacológicamente activos y una composición farmacéutica.
ARP160100180A 2015-01-23 2016-01-22 Conjugados de ácidos grasos y apelina sintética con mayor vida media AR104479A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201562107040P 2015-01-23 2015-01-23

Publications (1)

Publication Number Publication Date
AR104479A1 true AR104479A1 (es) 2017-07-26

Family

ID=55229773

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP160100180A AR104479A1 (es) 2015-01-23 2016-01-22 Conjugados de ácidos grasos y apelina sintética con mayor vida media

Country Status (22)

Country Link
US (1) US9931372B2 (es)
EP (1) EP3247405B1 (es)
JP (1) JP2018507187A (es)
KR (1) KR20170103970A (es)
CN (1) CN107406490A (es)
AR (1) AR104479A1 (es)
AU (1) AU2016209968B2 (es)
BR (1) BR112017014194A2 (es)
CA (1) CA2972871A1 (es)
CO (1) CO2017007244A2 (es)
CR (1) CR20170338A (es)
CU (1) CU20170093A7 (es)
EA (1) EA201791668A1 (es)
IL (1) IL253105A0 (es)
MA (1) MA41580A (es)
MX (1) MX2017009534A (es)
PE (1) PE20171328A1 (es)
PH (1) PH12017501112A1 (es)
SG (1) SG11201704758XA (es)
TW (1) TW201632197A (es)
UY (1) UY36523A (es)
WO (1) WO2016116842A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10588980B2 (en) 2014-06-23 2020-03-17 Novartis Ag Fatty acids and their use in conjugation to biomolecules
JP6984923B2 (ja) * 2017-09-19 2021-12-22 イミュンワーク インク.Immunwork Inc. アルブミンとの強化された結合親和性を有する医薬構築物
WO2019229242A1 (en) 2018-05-31 2019-12-05 Novo Nordisk A/S Derivatives comprising an apelin analogue and uses thereof
TW202304500A (zh) * 2021-04-21 2023-02-01 瑞士商諾華公司 升糖素樣肽化合物

Family Cites Families (86)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2951135A1 (de) 1979-12-19 1981-06-25 Hoechst Ag, 6230 Frankfurt Sulfonylharnstoffe, verfahren zu ihrer herstellung, pharmazeutische praeparate auf basis dieser verbindungen und ihre verwendung
US4889861A (en) 1982-12-21 1989-12-26 Ciba-Geigy Corp. Substituted imidazo[1,5-a]pyridine derivatives and other substituted bicyclic derivatives and their use as aromatase inhibitors
US4617307A (en) 1984-06-20 1986-10-14 Ciba-Geigy Corporation Substituted imidazo[1,5-A]pyridine derivatives as aromatase inhibitors
DE3347565A1 (de) 1983-12-30 1985-07-11 Thomae Gmbh Dr K Neue phenylessigsaeurederivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
JPS6354321A (ja) 1985-03-27 1988-03-08 Ajinomoto Co Inc 血糖降下剤
US5120712A (en) 1986-05-05 1992-06-09 The General Hospital Corporation Insulinotropic hormone
US5118666A (en) 1986-05-05 1992-06-02 The General Hospital Corporation Insulinotropic hormone
ES2113879T3 (es) 1990-01-24 1998-05-16 Douglas I Buckley Analogos de glp-1 utiles para el tratamiento de diabetes.
AU654331B2 (en) 1991-03-30 1994-11-03 Kissei Pharmaceutical Co. Ltd. Succinic acid compounds
US5155100A (en) 1991-05-01 1992-10-13 Ciba-Geigy Corporation Phosphono/biaryl substituted dipeptide derivatives
RU2086544C1 (ru) 1991-06-13 1997-08-10 Хоффманн-Ля Рош АГ Бензолсульфонамидные производные пиримидина или их соли, фармацевтическая композиция для лечения заболеваний, связанных с активностью эндотелина
SG43036A1 (en) 1991-06-21 1997-10-17 Thomae Gmbh Dr K (S) (+) -2-ethoxy-4-[N-[1-(2-piperidino-phenyl)-3-methyl- 1-buthyl]aminocarbony methyl] - benzoic a cid
DE10199058I2 (de) 1991-07-30 2006-04-27 Alcm Co Kristalle von N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanin und Verfahren zu ihrer Herstellung
WO1993011782A1 (en) 1991-12-19 1993-06-24 Southwest Foundation For Biomedical Research Cetp inhibitor polypeptide, antibodies against the synthetic polypeptide and prophylactic and therapeutic anti-atherosclerosis treatments
DE69426629T2 (de) * 1993-08-02 2001-08-02 Commonwealth Scientific And Industrial Research Organisation, Campbell Therapeutische verbindung - fettsäurekonjugate
IL111785A0 (en) 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
US5705483A (en) 1993-12-09 1998-01-06 Eli Lilly And Company Glucagon-like insulinotropic peptides, compositions and methods
US5512549A (en) 1994-10-18 1996-04-30 Eli Lilly And Company Glucagon-like insulinotropic peptide analogs, compositions, and methods of use
TW313568B (es) 1994-12-20 1997-08-21 Hoffmann La Roche
DE122010000020I1 (de) 1996-04-25 2010-07-08 Prosidion Ltd Verfahren zur Senkung des Blutglukosespiegels in Säugern
TW492957B (en) 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
AU1685499A (en) 1997-12-24 1999-07-19 Takeda Chemical Industries Ltd. Polypeptide, their production and use
WO1999043357A1 (en) * 1998-02-25 1999-09-02 Micrologix Biotech Inc. Indolicidin and cationic peptides conjugated with polymers
GT199900147A (es) 1998-09-17 1999-09-06 1, 2, 3, 4- tetrahidroquinolinas 2-sustituidas 4-amino sustituidas.
US6197786B1 (en) 1998-09-17 2001-03-06 Pfizer Inc 4-Carboxyamino-2-substituted-1,2,3,4-tetrahydroquinolines
CO5150173A1 (es) 1998-12-10 2002-04-29 Novartis Ag Compuestos n-(glicilo sustituido)-2-cianopirrolidinas inhibidores de peptidasa de dipeptidilo-iv (dpp-iv) los cuales son efectivos en el tratamiento de condiciones mediadas por la inhibicion de dpp-iv
US6683113B2 (en) 1999-09-23 2004-01-27 Pharmacia Corporation (R)-chiral halogenated substituted N,N-Bis-benzyl aminioalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
KR20020081466A (ko) 2000-03-23 2002-10-26 다케다 야쿠힌 고교 가부시키가이샤 펩티드 유도체
EP1282410A2 (en) 2000-04-12 2003-02-12 Novartis AG Novel medical use of aldosterone synthase inhibitors alone or in combination with at1-receptor antagonists
DK1456360T3 (en) 2001-04-19 2015-08-31 Scripps Research Inst Methods and Composition for Preparation of Orthogonal TRNA-Aminoacyl-TRNA Synthetase Pairs
ATE556591T1 (de) 2001-11-08 2012-05-15 Abbott Biotherapeutics Corp Stabile pharmazeutische flüssigformulierung von igg-antikörpern
AU2003232941A1 (en) 2002-06-07 2003-12-22 Glaxo Group Limited N-mercaptoacyl phenyalanine derivatives, process for their preparation, and pharmaceutical compositions containing them
AU2003253387A1 (en) 2002-08-07 2004-02-25 Novartis Ag Organic compounds as agents for the treatment of aldosterone mediated conditions
PT1565463E (pt) 2002-11-18 2008-09-10 Novartis Ag Derivados de imidazo[1,5-a]piridina e métodos para tratar doenças mediadas pela aldosterona
WO2004078777A2 (en) * 2003-03-04 2004-09-16 Biorexis Pharmaceutical Corporation Dipeptidyl-peptidase protected proteins
ES2326326T3 (es) 2004-03-26 2009-10-07 Eli Lilly And Company Compuestos y procedimientos para tratar la dislipidemia.
UA90269C2 (ru) 2004-04-02 2010-04-26 Мицубиси Танабе Фарма Корпорейшн Тетрагидрохинолиновые производные и способ их получения
WO2005118557A2 (en) 2004-05-28 2005-12-15 Speedel Experimenta Ag Heterocyclic compounds and their use as aldosterone synthase inhibitors
WO2005118541A2 (en) 2004-05-28 2005-12-15 Speedel Experimenta Ag Heterocyclic compounds and their use as aldosterone synthase inhibitors
JP2008500997A (ja) 2004-05-28 2008-01-17 シュペーデル・エクスペリメンタ・アーゲー アロマターゼ阻害剤としての二環式の窒素含有複素環
AR049711A1 (es) 2004-07-09 2006-08-30 Speedel Experimenta Ag Compuestos heterociclicos condensados como inhibidores de la aldosterona sintasa; composiciones farmaceuticas que los contienen y su uso en la preparacion de un medicamento para el tratamiento o prevencion de enfermedades relacionadas con el hiperaldosterismo y por una liberacion excesiva de cortiso
TW200716105A (en) 2005-05-31 2007-05-01 Speedel Experimenta Ag Imidazole compounds
TW200716634A (en) 2005-05-31 2007-05-01 Speedel Experimenta Ag Heterocyclic spiro-compounds
TW200716636A (en) 2005-05-31 2007-05-01 Speedel Experimenta Ag Heterocyclic spiro-compounds
GT200600381A (es) 2005-08-25 2007-03-28 Compuestos organicos
US8673848B2 (en) 2012-01-27 2014-03-18 Novartis Ag Synthetic apelin mimetics for the treatment of heart failure
AR056888A1 (es) 2005-12-09 2007-10-31 Speedel Experimenta Ag Derivados de heterociclil imidazol
WO2007076354A2 (en) 2005-12-20 2007-07-05 Bristol-Myers Squibb Company Stable protein formulations
US20090156875A1 (en) 2006-04-04 2009-06-18 Takafumi Tomioka Methane separation method, methane separation apparatus, and methane utilization system
TW200808813A (en) 2006-04-12 2008-02-16 Speedel Experimenta Ag Imidazo compounds
TW200808812A (en) 2006-04-12 2008-02-16 Speedel Experimenta Ag Imidazo compounds
WO2007128568A1 (en) 2006-05-10 2007-11-15 Novartis Ag Bicyclic derivatives as cetp inhibitors
EP1886695A1 (en) 2006-06-27 2008-02-13 Speedel Experimenta AG Pharmaceutical combination of an aldosterone synthase inhibitor and a glucocorticoid receptor antagonist or a cortisol synthesis inhibitor or a corticotropin releasing factor antagonist
EP2049517B1 (en) 2006-07-20 2013-11-27 Novartis AG Amino-piperidine derivatives as cetp inhibitors
US20090264420A1 (en) 2006-08-25 2009-10-22 Gary Michael Ksander Organic compounds
WO2008088422A2 (en) * 2006-10-25 2008-07-24 Amgen Inc. Toxin peptide therapeutic agents
US8143278B2 (en) 2006-12-18 2012-03-27 Novartis Ag Organic compounds
EA200900811A1 (ru) 2006-12-18 2009-12-30 Новартис Аг Имидазолы в качестве ингибиторов альдостеронсинтазы
JP2010513560A (ja) 2006-12-18 2010-04-30 ノバルティス アーゲー １−置換イミダゾール誘導体およびアルドステロン合成阻害剤としてのその使用
ATE484507T1 (de) 2007-03-29 2010-10-15 Novartis Ag Heterocyclische spiroverbindungen
TWI448284B (zh) 2007-04-24 2014-08-11 Theravance Inc 雙效抗高血壓劑
WO2009035543A1 (en) 2007-09-07 2009-03-19 Theravance, Inc. Dual-acting antihypertensive agents
ES2381518T3 (es) 2007-11-05 2012-05-29 Novartis Ag Derivados del 4-bencilamino-1-carboxi acil-piperidina como inhibidores de CETP útiles para el tratamiento de enfermedades tales como hiperlipidemia o arteroesclerosis
CN101878199B (zh) 2007-12-03 2013-09-18 诺瓦提斯公司 用于治疗例如高血脂或动脉硬化疾病的作为cetp抑制剂的1，2-二取代的-4-苄基氨基-吡咯烷衍生物
WO2009134741A1 (en) 2008-04-29 2009-11-05 Theravance, Inc. Dual-acting antihypertensive agents
AR072297A1 (es) 2008-06-27 2010-08-18 Novartis Ag Derivados de indol-2-il-piridin-3-ilo, composicion farmaceutica que los comprende y su uso en medicamentos para el tratamiento de enfermedades mediadas por la sintasa aldosterona.
RU2526804C2 (ru) * 2008-08-06 2014-08-27 Ново Нордиск Хелс Кеа Аг Конъюгированные белки с пролонгированным действием in vivo
AU2009308163B2 (en) 2008-10-24 2013-01-10 Novartis Ag Biosynthetically generated pyrroline-carboxy-lysine and site specific protein modifications via chemical derivatization of pyrroline-carboxy-lysine and pyrrolysine residues
CN103396474A (zh) * 2008-11-04 2013-11-20 安科治疗公司 Apj受体化合物
SG175925A1 (en) 2009-05-15 2011-12-29 Novartis Ag Aryl pyridine as aldosterone synthase inhibitors
EA201101672A1 (ru) 2009-05-28 2012-06-29 Новартис Аг Замещенные производные аминомасляной кислоты в качестве ингибиторов неприлизина
SI2435409T1 (sl) 2009-05-28 2014-12-31 Novartis Ag Substituirani aminopropionski derivati kot inhibitorji neprilizina
US9345661B2 (en) 2009-07-31 2016-05-24 Genentech, Inc. Subcutaneous anti-HER2 antibody formulations and uses thereof
JO2967B1 (en) 2009-11-20 2016-03-15 نوفارتس ايه جي Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors
TWI508737B (zh) * 2010-01-22 2015-11-21 諾佛 儂迪克股份有限公司 具有延長的活體內功效的生長激素
TW201138808A (en) 2010-05-03 2011-11-16 Bristol Myers Squibb Co Serum albumin binding molecules
JP6050746B2 (ja) 2010-05-13 2016-12-21 インディアナ ユニバーシティー リサーチ アンド テクノロジー コーポレーションIndiana University Research And Technology Corporation Ｇタンパク質共役受容体活性を示すグルカゴンスーパーファミリーのペプチド
US20140142049A1 (en) 2011-03-11 2014-05-22 Zhiqiang Jia Pegylated apelin and uses thereof
WO2013106437A1 (en) * 2012-01-09 2013-07-18 Anchor Therapeutics, Inc. Apj receptor compounds
EP2935311B1 (en) 2012-12-20 2021-03-31 Amgen Inc. Apj receptor agonists and uses thereof
HK1220466A1 (zh) 2013-03-14 2017-05-05 Regeneron Pharmaceuticals, Inc. 爱帕琳融合蛋白和其用途
JP2016527249A (ja) 2013-07-25 2016-09-08 ノバルティス アーゲー 合成アペリンポリペプチドのバイオコンジュゲート
AU2014293386B2 (en) 2013-07-25 2016-11-17 Novartis Ag Cyclic polypeptides for the treatment of heart failure
MX370689B (es) 2014-06-10 2019-12-19 Amgen Inc Polipeptidos apelina.
US10588980B2 (en) 2014-06-23 2020-03-17 Novartis Ag Fatty acids and their use in conjugation to biomolecules
US20170355734A1 (en) 2014-12-23 2017-12-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Metabolically Stable Apelin Analogs in the Treatment of Disease Mediated by the Apelin Receptor

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