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AR056888A1 - Derivados de heterociclil imidazol - Google Patents

Derivados de heterociclil imidazol

Info

Publication number
AR056888A1
AR056888A1 ARP060105413A ARP060105413A AR056888A1 AR 056888 A1 AR056888 A1 AR 056888A1 AR P060105413 A ARP060105413 A AR P060105413A AR P060105413 A ARP060105413 A AR P060105413A AR 056888 A1 AR056888 A1 AR 056888A1
Authority
AR
Argentina
Prior art keywords
substituted
aryl
unsubstituted
heterocyclyl
alkoxycarbonyl
Prior art date
Application number
ARP060105413A
Other languages
English (en)
Original Assignee
Speedel Experimenta 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 Speedel Experimenta Ag filed Critical Speedel Experimenta Ag
Publication of AR056888A1 publication Critical patent/AR056888A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/42Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of mineralocorticosteroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/08Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12Antidiuretics, e.g. drugs for diabetes insipidus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Derivados de heterociclil imidazol, un proceso para prepararlos y con el uso de estos compuestos como medicamentos, especialmente como inhibidores de la aldosterona sintasa. Reivindicacion 1: Un compuesto de la formula general (1), en la cual (A) R1 es fenilo o piridilo si R, R2, R3 y R4 son hidrogeno y n es 0, por lo cual fenilo o piridilo está sustituido con 1-4 alcoxi C1-8, alcoxicarbonilo C1-8, alquilo C1-8, alquilcarbonilo C0-8, alquilsulfonilo C1-8, arilo no sustituido o sustituido, aril-alcoxicarbonilo C0-4, ciano, halogeno, heterociclilo no sustituido o sustituido, hidroxilo, trialquilsililo C1-4, trifluorometoxi o trifluorometilo, donde por lo menos un sustituyente está situado en la posicion ôparaö (con respecto al sistema de anillos 6,7-dihidro-5H-pirrolo[1,2-c]imidazol-7-ilo); o (B) R1 es fenilo o heterociclilo insaturado si R, R2, R3 y R4 son hidrogeno y n es 1, por lo cual el fenilo o heterociclilo insaturado está sustituido con 3-4 alcoxi C1-8, alcoxicarbonilo C1- 8, alquilo C1-8, alquilcarbonilo C0-8, alquilsulfonilo C1-8, arilo no sustituido o sustituido, aril-alcoxicarbonilo C0-4, ciano, halogeno, heterociclilo no sustituido o sustituido, trialquilsililo C1-4, trifluorometoxi o trifluorometilo; o (C) R1 es arilo o heterociclilo insaturado, radicales que están sustituidos con 1-4 alcoxi C1-8, alcoxicarbonilo C1-8, alquilo C1-8, alquilcarbonilo C0-8, alquilsulfanilo C1-8, alquilsulfonilo C1-8, arilo no sustituido o sustituido, arilalcoxicarbonilo C0-4, ciano, halogeno, heterociclilo no sustituido o sustituido, hidroxilo, nitro, oxido, oxo, trialquilsililo C1-4, trifluorometoxi o trifluorometilo, donde por lo menos un sustituyente es alquilsulfanilo C1-8, hidroxilo, nitro u oxido; o (D) R1 es arilo o heterociclilo insaturado si R3 y R4 no son simultáneamente deuterio o hidrogeno, por lo cual arilo o heterociclilo insaturado está sustituido con 1-4 alcoxi C1-8, alcoxicarbonilo C1-8, alquilo C1-8, alquilcarbonilo C0-8, alquilsulfonilo C1-8, arilo no sustituido o sustituido, aril-alcoxicarbonilo C0-4, ciano, halogeno, heterociclilo no sustituido o sustituido, oxo, trialquilsililo C1-4, trifluorometoxi o trifluorometilo; o (E) R1 es arilo o heterociclilo insaturado si R2 es hidroxilo o alcoxi C1-8, donde el arilo o heterociclilo insaturado está sustituido con 1-4 alcoxi C1-8, alcoxicarbonilo C1-8, alquilo C1-8, alquilcarbonilo C0-8, alquilsulfonilo C1-8, arilo no sustituido o sustituido, aril-alcoxicarbonilo C0-4, ciano, halogeno, heterociclilo no sustituido o sustituido, oxo, trialquilsililo C1-4, trifluorometoxi o trifluorometilo; R a) es deuterio, halogeno, trialquilsililo C1-4, trifluorometoxi, trifluorometilo o hidrogeno; o b) es alcoxi C1-8 o alquilo C1-8; R2 a) es deuterio, halogeno, hidroxilo o hidrogeno; o b) es alquenilo C2-8, alquinilo C2-8, alcoxi C1-8, alcoxicarbonilo C1-4-alquilo C1-4, alquilo C1-8, alquilcarbonilo C0-4, arilalquilo C0-4, carboxialquilo C1-4, cicloalquilo C3-8 o heterociclilo insaturado-alquilo C0-4, radicales éstos que pueden estar sustituidos con 1-4 alcoxi C1-8, alcoxicarbonilo, alquilo C1-8, alquilcarbonilo C0-8, alquilsulfonilo C1-8, arilo no sustituido o sustituido, aril-alcoxicarbonilo C0-4, ciano, halogeno, heterociclilo no sustituido o sustituido, hidroxilo, nitro, oxido, oxo, trialquilsililo C1-4, trifluorometoxi o trifluorometilo; R3 a) es deuterio, halogeno, hidroxilo, trifluorometoxi, trifluorometilo o hidrogeno; o b) es alcoxi C1-8 o alquilo C1- 8; R4 a) es deuterio, halogeno, trifluorometoxi, trifluorometilo o hidrogeno; o b) es alcoxi C1-8 o alquilo C1-8; n es un numero 0, 1 o 2; y las sales del mismo, preferentemente las sales adecuadas para uso farmacéutico de los mismos, donde si R2 es hidrogeno, R1 no es carbazolilo, fluorenilo ni naftilo; si R es hidrogeno y R2 es hidroxilo, R1 no es alcoxi C1-8 ni halobenzotiofen-2-ilo, bifenilo no sustituido o sustituido ni 4-bromofenilo.
ARP060105413A 2005-12-09 2006-12-07 Derivados de heterociclil imidazol AR056888A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP05111907 2005-12-09

Publications (1)

Publication Number Publication Date
AR056888A1 true AR056888A1 (es) 2007-10-31

Family

ID=36284061

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060105413A AR056888A1 (es) 2005-12-09 2006-12-07 Derivados de heterociclil imidazol

Country Status (10)

Country Link
US (2) US8008334B2 (es)
EP (1) EP1957489A2 (es)
JP (1) JP5258573B2 (es)
CN (2) CN102115473A (es)
AR (1) AR056888A1 (es)
BR (1) BRPI0619536A2 (es)
CA (1) CA2629137A1 (es)
IL (1) IL191844A0 (es)
TW (1) TW200804378A (es)
WO (1) WO2007065942A2 (es)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR056888A1 (es) 2005-12-09 2007-10-31 Speedel Experimenta Ag Derivados de heterociclil imidazol
TW200808813A (en) * 2006-04-12 2008-02-16 Speedel Experimenta Ag Imidazo compounds
KR20120041702A (ko) 2009-05-28 2012-05-02 노파르티스 아게 네프릴리신 억제제로서의 치환된 아미노부티르산 유도체
AU2010251967B9 (en) 2009-05-28 2014-04-03 Novartis Ag Substituted aminopropionic derivatives as neprilysin inhibitors
JO2967B1 (en) 2009-11-20 2016-03-15 نوفارتس ايه جي Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors
PL2523731T3 (pl) 2010-01-14 2019-04-30 Novartis Ag Zastosowanie środka modyfikującego hormon nadnerczy
US8877815B2 (en) 2010-11-16 2014-11-04 Novartis Ag Substituted carbamoylcycloalkyl acetic acid derivatives as NEP
US8673974B2 (en) 2010-11-16 2014-03-18 Novartis Ag Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors
TWI627167B (zh) 2011-07-08 2018-06-21 諾華公司 用於高三酸甘油酯個體治療動脈粥狀硬化之方法
UY35144A (es) 2012-11-20 2014-06-30 Novartis Ag Miméticos lineales sintéticos de apelina para el tratamiento de insuficiencia cardiaca
CU24330B1 (es) 2013-02-14 2018-03-13 Novartis Ag Derivados del ácido 4-((1,1) bifenil-4-il)-3-(3-fosfonopropanamido) butanoico, activos como inhibidores de nep (endopeptidasa neutral)
CA2918074A1 (en) 2013-07-25 2015-01-29 Novartis Ag Cyclic polypeptides for the treatment of heart failure
TW201518323A (zh) 2013-07-25 2015-05-16 Novartis Ag 合成apelin多肽之生物結合物
KR20170103970A (ko) 2015-01-23 2017-09-13 노파르티스 아게 개선된 반감기를 갖는 합성 아펠린 지방산 접합체
JOP20190086A1 (ar) 2016-10-21 2019-04-18 Novartis Ag مشتقات نافثيريدينون جديدة واستخدامها في معالجة عدم انتظام ضربات القلب
UY38072A (es) 2018-02-07 2019-10-01 Novartis Ag Compuestos derivados de éster butanoico sustituido con bisfenilo como inhibidores de nep, composiciones y combinaciones de los mismos
WO2020110008A1 (en) 2018-11-27 2020-06-04 Novartis Ag Cyclic pentamer compounds as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorder
UY38485A (es) 2018-11-27 2020-06-30 Novartis Ag Compuestos tetrámeros cíclicos como inhibidores de proproteína convertasa subtilisina/kexina tipo 9 (pcsk9), método de tratamiento, uso y su preparación
US20220024981A1 (en) 2018-11-27 2022-01-27 Novartis Ag Cyclic peptides as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorders
TW202333563A (zh) 2021-11-12 2023-09-01 瑞士商諾華公司 用於治療疾病或障礙之二胺基環戊基吡啶衍生物
AR127698A1 (es) 2021-11-23 2024-02-21 Novartis Ag Derivados de naftiridinona para el tratamiento de una enfermedad o un trastorno

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Also Published As

Publication number Publication date
JP5258573B2 (ja) 2013-08-07
WO2007065942A3 (en) 2007-07-26
JP2009518365A (ja) 2009-05-07
CA2629137A1 (en) 2007-06-14
US20090197909A1 (en) 2009-08-06
BRPI0619536A2 (pt) 2011-10-04
CN101326184A (zh) 2008-12-17
US8263615B2 (en) 2012-09-11
US20110028512A1 (en) 2011-02-03
IL191844A0 (en) 2008-12-29
CN102115473A (zh) 2011-07-06
EP1957489A2 (en) 2008-08-20
US8008334B2 (en) 2011-08-30
TW200804378A (en) 2008-01-16
WO2007065942A2 (en) 2007-06-14
CN101326184B (zh) 2011-11-23

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