MX2017009534A - Conjugados de acidos grasos y apelina sintetica con mayor vida media. - Google Patents

Conjugados de acidos grasos y apelina sintetica con mayor vida media.

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Publication number
MX2017009534A
MX2017009534A MX2017009534A MX2017009534A MX2017009534A MX 2017009534 A MX2017009534 A MX 2017009534A MX 2017009534 A MX2017009534 A MX 2017009534A MX 2017009534 A MX2017009534 A MX 2017009534A MX 2017009534 A MX2017009534 A MX 2017009534A
Authority
MX
Mexico
Prior art keywords
fatty acid
conjugates
heart failure
life
diabetes
Prior art date
Application number
MX2017009534A
Other languages
English (en)
Inventor
Zecri Frederic
Kanter Aaron
Richardson Usera Aimee
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 MX2017009534A publication Critical patent/MX2017009534A/es

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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
    • C07K14/46—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
    • 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
    • A61K47/54—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
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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

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

Abstract

La invención proporciona un conjugado, o una sal farmacéuticamente aceptable del mismo, que comprende un polipéptido sintético de Fórmula I: Q-R-P-R-L-C*-H-K-G-P-(Nle)-C*- F (I) o una amida o éster del mismo; y un ácido graso seleccionado de: 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. La invención también se refiere a un método para la fabricación de los conjugados de la invención y sus usos terapéuticos, tales como el tratamiento o la prevención de insuficiencia cardíaca aguda descompensada (ICAD), insuficiencia cardíaca crónica; hipertensión pulmonar, fibrilación atrial, síndrome de Brugada, taquicardia ventricular, aterosclerosis, hipertensión, restenosis, enfermedades isquémicas cardiovasculares, cardiomiopatía, fibrosis cardíaca, 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 invención proporciona además una combinación de agentes farmacológicamente activos y una composición farmacéutica.
MX2017009534A 2015-01-23 2016-01-15 Conjugados de acidos grasos y apelina sintetica con mayor vida media. MX2017009534A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562107040P 2015-01-23 2015-01-23
PCT/IB2016/050206 WO2016116842A1 (en) 2015-01-23 2016-01-15 Synthetic apelin fatty acid conjugates with improved half-life

Publications (1)

Publication Number Publication Date
MX2017009534A true MX2017009534A (es) 2018-04-10

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MX2017009534A MX2017009534A (es) 2015-01-23 2016-01-15 Conjugados de acidos grasos y apelina sintetica 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
EP3684414A4 (en) * 2017-09-19 2021-06-09 Immunwork Inc. PHARMACEUTICAL CONSTRUCTIONS WITH IMPROVED BINDING AFFINITY WITH ALBUMIN
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 (84)

* 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
US4617307A (en) 1984-06-20 1986-10-14 Ciba-Geigy Corporation Substituted imidazo[1,5-A]pyridine derivatives as aromatase inhibitors
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
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
AU660930B2 (en) 1991-06-21 1995-07-13 Novo Nordisk A/S (S)(+)-2-ethoxy-4-(N-(1-(2-piperidinophenyl)-3-methyl-1- butyl)aminocarbonylmethyl)benzoic acid
DE69217762T2 (de) 1991-07-30 1997-10-09 Ajinomoto Kk Kristalle von N-(Trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanin und Verfahren zu ihrer Herstellung
EP0618803A4 (en) 1991-12-19 1995-03-22 Southwest Found Biomed Res POLYPEPTIDE INHIBITING PROTEIN TRANSFER TO CHOLESTERYL ESTERS, ANTIBODIES AGAINST SYNTHETIC POLYPEPTIDE AND ANTI-ATHEROSCLEROSIS PROPHYLACTIC AND THERAPEUTIC TREATMENTS.
DK0712389T3 (da) * 1993-08-02 2001-06-05 Commw Scient Ind Res Org Terapeutisk forbindelse - fedtsyrekonjugater
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
DE69838986T2 (de) 1997-12-24 2009-01-08 Takeda Pharmaceutical Co. Ltd. Polypeptide, deren herstellung und verwendung
AU2605099A (en) * 1998-02-25 1999-09-15 Micrologix Biotech, Inc. Indolicidin and cationic peptides conjugated with polymers
US6197786B1 (en) 1998-09-17 2001-03-06 Pfizer Inc 4-Carboxyamino-2-substituted-1,2,3,4-tetrahydroquinolines
GT199900147A (es) 1998-09-17 1999-09-06 1, 2, 3, 4- tetrahidroquinolinas 2-sustituidas 4-amino sustituidas.
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
US6677341B2 (en) 1999-09-23 2004-01-13 Pharmacia Corporation (R)-Chiral halogenated substituted heteroaryl benzyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
CN1419563A (zh) 2000-03-23 2003-05-21 武田药品工业株式会社 肽衍生物
NZ521855A (en) 2000-04-12 2004-10-29 Novartis Ag Use of an aldosterone synthase inhibitor in combination with an angiotensin I receptor antagonist or an angiotensin I receptor antagonist plus a dirruretic to treat various conditions
CA2444098C (en) 2001-04-19 2016-06-21 The Scripps Research Institute Methods and composition for the production of orthogonal trna-aminoacyltrna synthetase pairs
KR100913714B1 (ko) 2001-11-08 2009-08-24 패시트 바이오테크 코포레이션 Ｉｇｇ 항체의 안정한 액상 약학 제형물
AR040441A1 (es) 2002-06-07 2005-04-06 Glaxo Group Ltd Compuesto de tiol, composicion farmaceutica que lo comprende, su uso para la fabricacion de un medicamento, procedimiento para prepararlo y compuesto intermediario de utilidad en dicho procedimiento
ATE335744T1 (de) 2002-08-07 2006-09-15 Novartis Pharma Gmbh Organische verbindungen als mittel zur behandlung von aldosteronbedingten zuständen
JP2006508970A (ja) 2002-11-18 2006-03-16 ノバルティス アクチエンゲゼルシャフト イミダゾ［１，５ａ］ピリジン誘導体およびアルデステロンにより仲介される疾患の処置方法
WO2004078777A2 (en) * 2003-03-04 2004-09-16 Biorexis Pharmaceutical Corporation Dipeptidyl-peptidase protected proteins
DE602005014955D1 (de) 2004-03-26 2009-07-30 Lilly Co Eli Verbindungen und verfahren zur behandlung von dyslipidämie
UA90269C2 (ru) 2004-04-02 2010-04-26 Мицубиси Танабе Фарма Корпорейшн Тетрагидрохинолиновые производные и способ их получения
AR050251A1 (es) 2004-05-28 2006-10-11 Speedel Experimenta Ag Compuestos heterociclicos con nitrogeno heteroatomico y composicion farmaceutica en base al compuesto
BRPI0510410A (pt) 2004-05-28 2007-10-23 Speedel Experimenta Ag compostos orgánicos
CA2568159A1 (en) 2004-05-28 2005-12-15 Speedel Experimenta Ag Tetrahydro-imidazo [1,5-a] pyridin derivatives as aldosterone synthase inhibitors
WO2006005726A2 (en) 2004-07-09 2006-01-19 Speedel Experimenta Ag Heterocyclic compounds
TW200716634A (en) 2005-05-31 2007-05-01 Speedel Experimenta Ag Heterocyclic spiro-compounds
TW200716105A (en) 2005-05-31 2007-05-01 Speedel Experimenta Ag Imidazole 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
TW200804378A (en) 2005-12-09 2008-01-16 Speedel Experimenta Ag Organic compounds
AR058567A1 (es) 2005-12-20 2008-02-13 Bristol Myers Squibb Co Formulaciones de proteinas estables
WO2007116908A1 (ja) 2006-04-04 2007-10-18 Taiyo Nippon Sanso Corporation メタン分離方法、メタン分離装置及びメタン利用システム
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
MX2009000646A (es) 2006-07-20 2009-01-29 Novartis Ag Derivados de amino-piperidina como inhibidores de la proteina de transferencia de colesteril-ester (cetp).
WO2008027284A1 (en) 2006-08-25 2008-03-06 Novartis Ag Fused imidazole derivatives for the treatment of disorders mediated by aldosterone synthase and/or 11-beta-hydroxylase and/or aromatase
PE20081140A1 (es) * 2006-10-25 2008-09-22 Amgen Inc Agentes terapeuticos a base de peptidos derivados de toxinas
EP2213668A3 (en) 2006-12-18 2010-11-24 Novartis AG Imidazoles as aldosterone synthase inhibitors
MX2009006630A (es) 2006-12-18 2009-06-30 Novartis Ag Derivados de 4-imidazolil-1,2,3,4-tetrahidro-quinola y su uso como inhibidores de aldosterona / 11-beta-hidroxilasa.
WO2008076862A2 (en) 2006-12-18 2008-06-26 Novartis Ag 1-substituted imidazole derivatives and their use as aldosterone synthase inhibitors
US8324235B2 (en) 2007-03-29 2012-12-04 Novartis Ag Heterocyclic spiro-compounds
TWI448284B (zh) 2007-04-24 2014-08-11 Theravance Inc 雙效抗高血壓劑
US7834041B2 (en) 2007-09-07 2010-11-16 Theravance, Inc. Dual-acting antihypertensive agents
AU2008324243B2 (en) 2007-11-05 2012-03-08 Novartis Ag 4-benzylamino-1-carboxyacyl-piperidine derivatives as CETP inhibitors useful for the treatment of diseases such as hyperlipidemia or arteriosclerosis
EP2404901B1 (en) 2007-12-03 2013-05-22 Novartis AG 1,2-Disubstituted 4-benzylamino-pyrrolidine derivatives as CETP inhibitors useful for the treatment of diseases such as hyperlipidemia or arteriosclerosis
JP2011518884A (ja) 2008-04-29 2011-06-30 セラヴァンス， インコーポレーテッド 二重活性抗高血圧剤
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.
MX342677B (es) 2008-10-24 2016-10-07 Novartis Ag * Pirrolin-carboxi-lisina biosintéticamente generada y modificaciones de proteínas específicas del sitio por medio de la derivación química de residuos de pirrolin-carboxi-lisina y pirrolisina.
WO2010053545A2 (en) * 2008-11-04 2010-05-14 Anchor Therapeutics, Inc. Apj receptor compounds
MA33358B1 (fr) 2009-05-15 2012-06-01 Novartis Ag Arylpyridine en tant qu'inhibiteurs de l'aldostérone synthase
ME01923B (me) 2009-05-28 2015-05-20 Novartis Ag Supstituisani derivati aminopropionske kiseline kao inhibitori neprilizina
SG176010A1 (en) 2009-05-28 2011-12-29 Novartis Ag Substituted aminobutyric derivatives as neprilysin inhibitors
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
TW201138808A (en) 2010-05-03 2011-11-16 Bristol Myers Squibb Co Serum albumin binding molecules
EP2568993A4 (en) 2010-05-13 2014-02-19 Univ Indiana Res & Tech Corp GLUCAGON SUPERFAMILY PEPTIDES EXPRESSING G PROTEIN-COUPLED RECEPTOR ACTIVITY
US20140142049A1 (en) 2011-03-11 2014-05-22 Zhiqiang Jia Pegylated apelin and uses thereof
CA2860740A1 (en) * 2012-01-09 2013-07-18 Anchor Therapeutics, Inc. Apj receptor compounds
EP3907237A1 (en) 2012-12-20 2021-11-10 Amgen Inc. Apj receptor agonists and uses thereof
AU2014236451B2 (en) 2013-03-14 2018-08-09 Regeneron Pharmaceuticals, Inc. Apelin fusion proteins and uses thereof
EP3024845A1 (en) * 2013-07-25 2016-06-01 Novartis AG Cyclic polypeptides for the treatment of heart failure
CN105705167A (zh) 2013-07-25 2016-06-22 诺华股份有限公司 合成的apelin多肽的生物缀合物
US10941182B2 (en) 2014-06-10 2021-03-09 Amgen Inc. Apelin polypeptides
US10588980B2 (en) * 2014-06-23 2020-03-17 Novartis Ag Fatty acids and their use in conjugation to biomolecules
WO2016102648A1 (en) 2014-12-23 2016-06-30 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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